Ester compounds and their using in medicine


FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to novel ester compounds represented by the formula (1): wherein values for R1, R2, A, X, R3, R4, Alk1, Alk2, l, m, D, R8 and R9 are determined in the invention claim. Also, invention relates to inhibitor of matrix metalloproteinase (MTP), a pharmaceutical composition able to inhibit activity of MTP selectively, agents used in treatment or prophylaxis of hyperlipidemia, arteriosclerosis, coronary artery diseases, obesity, diabetes mellitus or hypertension wherein the pharmaceutical composition is prepared in capsulated formulation, and to a biphenyl compound of the formula (100) given in the invention description.

EFFECT: valuable medicinal properties of compounds.

53 cl, 78 tbl, 17 ex

 

The scope of the invention

The present invention relates to a new ester compound, and also relates to a pharmaceutical composition that includes a new ester compound that selectively inhibits microsomal protein triglyceride transfer (MTP) in the small intestine, or its prodrug, or pharmaceutically acceptable salt of any of them. In addition, the present invention relates to an agent for treatment or prophylaxis of hyperlipidemia, arteriosclerosis, coronary artery disease, obesity, diabetes or high blood pressure (hypertension), comprising as active ingredient new ester compound that selectively inhibits MTP in the small intestine, or its prodrug or pharmaceutically acceptable salt of any of them. In addition, the present invention relates to an agent for treatment or prophylaxis of hyperlipidemia, arteriosclerosis, coronary artery disease, obesity, diabetes or hypertension, which has a new feature that was previously unknown.

Prior this area

It was found that hyperlipidemia, diabetes, hypertension or the like are one of the risk factors for arteriosclerosis. Hyperlipidemia is a condition in which the concentration of whether the IDA, such as cholesterol, abnormally increased in the blood. Types of hyperlipidemia, depending on the causes include primary hyperlipidemia caused by a genetic abnormality of the enzyme, protein, lipoprotein, and the like, which are involved in the metabolism of low density lipoprotein (LDL), secondary hyperlipidemia due to various diseases or taking drugs and acquired hyperlipidemia, mainly resulting from overeating.

Meanwhile, a lipid obtained from the food is absorbed in the small intestine under the action of bile acids and excreted (secreted) in the form of chylomicrons in the blood via the lymphatic vessels. Triglyceride fragment of secreted chylomicrons hydrolyzed to free fatty acids under the action of lipoprotein lipase (LPL), available in the capillary vessels, becoming the remains of chylomicron having a high content cholesterolemia of ester (CE), which is then absorbed in the liver through receptor chylomicronemia residue in the liver. In addition, in the liver absorbed the remainder of chylomicron and free fatty acid into CE and TG, respectively, which are then linked to apolipoprotein B, synthesized on the rough surface of the endoplasmic reticulum with the formation of lipoprotein very low density (VLDL). VLDL p is ranoside in the Golgi apparatus, modified and secreted outside the cells, and becomes a lipoprotein, intermediate density (IDL) under the action of LPL. ILD becomes LDL under the action of hepatic triacylglycerols (HTGL), and lipids are distributed to peripheral tissues.

For a long time it was stated that during the above-mentioned formation of chylomicrons in the small intestine or VLDV liver, microsomal fractions of the small intestine or the liver there is a protein having TG - or CE-transferring activity. Meanwhile, protein, i.e. inventory (microsome protein transfer triglycerides), was purified and isolated from microsomal fractions of bovine liver Wetterau et al., in 1985 (J. R. Wetterau et al., Chem.Phys. Lipids, 38, 205-222 (1985)). Inventory, however, began to attract much attention in the field of clinical medicine only after a report in 1993 that the cause of abetalipoproteinemia is the shortage of materials and equipment. In other words, the disease is characterized by the fact that although genes related to apolipoprotein B, are normal, apolipoprotein In hardly detectable in the blood serum cholesterol level in serum is approximately 50 mg/DL or below, the level of triglyceride in the serum is extremely low, and, moreover, lipoproteins, including apolipoprotein B, such as chylomicrons, VLDL, LDL, etc. generally are not present in the blood. Using this fact, it was shown that the TR is an integral protein involved in the Association of apolipoprotein b with TG or CE, i.e. in the formation of VLDL or chylomicron, and plays a significant role in their secretion.

Because lipid is inherently insoluble in water, the lipid in the blood combined with the hydrophilic protein known as apolipoprotein, and exists in the form of so-called lipoprotein. All VLDL, IDL, LDL or chylomicrons, etc. related to hyperlipidemia, are lipoproteins.

Inventory exists in microsome fractions of hepatocytes and epithelial cells of the small intestine and catalyzes the transfer of TG or CE in the cells. In the liver and small intestine, along with the synthesis of apolipoprotein (apolipoprotein B100 in the liver and apolipoprotein B in the small intestine), TG and CE obyedinayutsya with the corresponding apolipoprotein In due to the activity of MTP transfer, and thus is formed VLDL or chylomicrons. In the external environment of the cells are secreted such lipoproteins like VLDL in the liver or chylomicrons in the small intestine. It should be noted that MTP is required for the formation of these lipoproteins. Namely, if the activity of MTP is blocked, inhibited the migration of lipids such as TG and CE, etc. to apolipoprotein, and, thus, inhibited the formation of lipoprotein.

On the other hand, it was found that LDL is generally closely associated with the development of arteriosclero the and. That is, LDL-permeable endothelium of blood vessels is located on the extracellular matrix of the vessel walls, where oxidative decomposition, and lipid peroxides or denatured proteins induce a series of inflammatory reactions. This results in the invasion of macrophages, leading to fat deposition or the formation of foam cells, migration or proliferation of smooth muscle cells, and there is an increase in the intercellular matrix, etc. that leads to the development arteriosclerotic plaques. Based on the above, it is assumed that it is possible to prevent or to treat arteriosclerosis, coronary artery disease or hypertension by reducing LDL levels.

As already mentioned, it is possible to inhibit the formation of lipoproteins, such as chylomicrons, VLDL, LDL, and so on, by inhibiting the action of RTMS. Accordingly, it was expected that it should be possible to control the level of lipoprotein, such as TG, cholesterol and LDL, etc. in the blood and control the lipids in the cells by regulating the activity of MTP, and, therefore, was to develop a new agent for the treatment or prophylaxis of hyperlipidemia, arteriosclerosis, coronary artery disease, diabetes, obesity or hypertension and, in addition, the agent for the treatment or prevention of pancreatitis, hypercholesterolemia, hypergly is epidemie etc.

However, with the development of the MTP inhibitors began to report the number of cases of fatty liver disease and problems related hepatotoxicity.

For these reasons, it would be highly desirable new MTP inhibitor, which does not cause side effects, such as fatty liver, etc.

The usual way was tested combination therapy with various combinations of different antihyperlipidemic drugs. However, when given together, for example, drug Statesboro type and drug resinous type, was observed unwanted side effects, such as improved GTO and GPT, constipation, blocking the absorption of vitamins a, D, E and K, and the like. On the other hand, when given together medicine Statesboro type and fibrous medicine, observed side effects such as rhabdomyolysis or elevated IBS (CPK). Thus, with regard to combination therapy for hyperlipidemia, it would be desirable to develop a drug for the combined introduction, which could be introduced in conjunction with regular antihyperlipidemic drug, without causing any of the above side effects.

Meanwhile, examples of known compounds with MTP-inhibiting activity, the structure, analogichnoi compounds of the present invention, described below.

The following connection is described in WO98/26240.

The following compound described in WO97/43257

The following connection is described in WO98/23593

The following connection is described in WO99/63929

The following compound described in WO2000/5201

The following compound described in J.Med.Chem. (2001), 44(6), p.851-856

The following compound described in EP 1099701

The following compound described in WO2001/77077

The following compound described in J.Med.Chem. (2001), 44(6), p.4677-4687

The following compound described in WO2002/4403

However, in the above literature, there is no description of the compounds comprising ester as an essential structure as described in the present invention, much less described data indicating that, when the compound has the structure presented in the present invention, it selectively inhibits MTP in the small intestine, while it rarely affects MTP in the liver.

Description of the invention

Although the development of new antihyperlipidemics is their medicines, working due to their MTP-inhibiting activity, are strongly moved to the present time, these medicines are not satisfactory in regard to the level of action and the accompanying side effects such as fatty liver, etc. Thus, it became highly desirable to develop antihyperlipidemic drugs, does not cause side effects in the liver, which is observed in the case of conventional MTP inhibitors, as well as possessing excellent MTP-inhibiting activity.

The authors of the present invention conducted intensive studies on the creation of a new MTP inhibitor that does not cause the above side effects, such as fatty liver. In the result, it was found that the MTP inhibitor that selectively inhibits MTP in the small intestine, but essentially did not inhibit MTP in the liver, significantly reduces the level of unwanted TG or cholesterol without causing side effects such as fatty liver, etc. Unexpectedly found that the compound having the ester structure represented by the following formula (1), immediately metaboliziruet in the small intestine, blood or liver, which makes the connection the ability to selectively act on MTP in the small intestine, essentially no inhibition of MTP in the liver.

For the information of specificity, in accordance with the usual concept of obtaining prodrugs when creating medicines, carboxylic acid, which is an active early, atrificial to improve the rate of absorption in the small intestine and immediately metabolized in the blood, producing carbonic acid, which is an active early. On the other hand, in the present invention uses the concept of drug development, which differs from the above-mentioned concepts of obtaining prodrugs. Namely, when the introduction of at least one of ester in the molecular skeleton compounds with MTP-inhibiting activity, connection, after it shows MTP-inhibitory activity on the mucous membrane of the small intestine, immediately metabolized by the action of esterase or metabolic enzyme, etc. in the small intestine, portal vein (the blood) and liver by conversion to the corresponding carboxylic acid and alcohol, which does not have MTP-inhibiting activity. This is a completely new concept, according to which the MTP in the liver is essentially not exposed to, and MTP in the small intestine selectively inhibited. In addition, the compounds of the present invention exhibit strong MTP-inhibitory activity in vitro, thus strongly inhibit MTP in the small intestine and C is acetelyne reduce the level of triglycerides and cholesterol in the blood. In addition, the compounds of the present invention significantly reduced non-HDL cholesterol and unexpectedly increase HDL-cholesterol in plasma.

Accordingly, the authors of the present invention found that when the connection includes ester structure represented by the following formula (1), the connection is immediately metabolized in the small intestine, blood or liver after he strongly inhibits MTP in the small intestine, and, therefore, MTP in the liver is inhibited is not significant, the result of which was accomplished the present invention.

Thus, the present invention relates to:

(1) Ester compound represented by formula (1)

where

each of R1and R2represents hydrogen, C1-C6-alkyl, C3-With7-cycloalkyl,1-C6-alkoxy, halogen-C1-C6-alkyl, halogen-C1-C6-alkyloxy, optionally substituted C6-C14aryl, optionally substituted C7-C16-aralkyl, optionally substituted C6-C14-aryloxy, optionally substituted C7-C16-aralkylated, optionally substituted C7-C15-arylcarbamoyl, optionally substituted heterocycle, With2-C7-alkoxycarbonyl, halogen, C2-C6 alkenyl, -N(R40)(R41), where each of R40and R41independently represents hydrogen or optionally substituted C6-C14-aryl;

ring a represents a C6-C14aryl, heterocycle or

X represents-COO-(CH2)n-, -CON(R10)-(CH2)n- or-N(R10)-CO-(CH2)n-where R10represents hydrogen, C1-C6-alkyl or C3-C7-cycloalkyl, and n is an integer from 0 to 3;

each of R3and R4independently represents hydrogen, hydroxy, halogen, optionally substituted C1-C6-alkyl, C1-C6-alkoxy, halogen With1-C6-alkyl, C7-C16-aralkylated,1-C6-acyl, optionally substituted heterocycle, -CON(R11)(R12) (where each of R11and R12independently represents hydrogen, C1-C6-alkyl, optionally substituted C6-C14aryl, optionally substituted C7-C16-aralkyl,1-C6-alkoxy, or R11and R12taken together with the nitrogen atom to which they are attached, form

where p is an integer from 0 to 2), -(CH2)q-N(R13)(R14) (where each of R13 and R 14independently represents hydrogen, C1-C6-alkyl, C2-C7-alkoxycarbonyl,1-C6-acyl, or R13and R14taken together with the nitrogen atom to which they are attached, form

where R has the same meaning as defined above, and q is an integer from 0 to 3), or-CO(R15) (where R15represents hydroxy, C1-C6-alkoxy, optionally substituted C6-C14-aryloxy, optionally substituted C7-C16-aralkylated or1-C6-alkyl);

the ring is a

where K is an integer from 0 to 2, or a ring, taken together with R3, R10and nitrogen associated with R10forms

Alkl1represents alcander or alkerdeel;

Alkl2represents alcander or alkerdeel;

l represents an integer from 0 to 3;

m is an integer from 0 to 3;

D represents C1-C6-alkyl, C2-C6alkenyl,2-C7-alkoxycarbonyl, -N(R42)-CO(R43) (where R42represents hydrogen or C1-C6-alkyl, and R43represents a C6-C14-aryl or C7 16-aralkyl) or a group represented by the following formula

(where each of R5, R6and R7independently represents hydrogen, C1-C6-alkyl, C1-C6-alkoxy, C2-C7-alkoxycarbonyl, carboxyl, halogen, cyano, nitro, halogen-C1-C6-alkyl, C1-C6-acyl, hydroxy, amino, optionally substituted C6-C14-aryl or -(CH2)r-CON(R16)(R17) (where each of R16and R17independently represents hydrogen, C1-C6-alkyl or halogen-C1-C6-alkyl, and r is an integer from 0 to 3);

the ring represents a C6-C14-aryl, C7-C15-arylcarboxamide,8-C17-aralkylamines, heterocyclic residue, With3-C7-cycloalkyl or7-C16-aralkyl, or ring, taken together with R7and R8forms

; and

each of R8and R9independently represents hydrogen, C1-C6-alkyl, optionally substituted C6-C14aryl, hydroxy-C1-C6-alkyl, -CON(R18)(R19) (where each of R18and R19independently represents hydrogen, C1-C6-alkyl, C3-C7-cycloalkyl,halogen-C 1-C6-alkyl, C2-C12-alkoxyalkyl or optionally substituted C6-C14aryl), -COO(R20or -(CH2)s-OCO(R20) (where R20represents hydrogen, C1-C6-alkyl or C3-C7-cycloalkyl; s is an integer from 0 to 3), -N(R21)(R22) (where each of R21and R22independently represents hydrogen, C1-C6-alkyl, C1-C6-acyl, C1-C6-alkylsulfonyl, or R21and R22taken together with the nitrogen to which they are connected, form

or

R8and R9taken together, may form With3-C7-cycloalkyl, or its prodrug, or pharmaceutically acceptable salt of any of them;

(2) the Ester compound or its prodrug, or pharmaceutically acceptable salt of any of them in accordance with the above paragraph 1, where D represents C1-C6-alkyl, C2-C6alkenyl,2-C7-alkoxycarbonyl or-N(R42)-CO(R43), where each of R42and R43has the same meaning as defined above;

(3) the Ester compound or its prodrug, or pharmaceutically acceptable salt of any of them in accordance with the above paragraph 1, where D is a group, p is redstavlennye formula

in which each of R5, R6and R7has the same meaning as defined above;

(4) the Ester compound or its prodrug, or pharmaceutically acceptable salt of any of them in accordance with the above paragraph 3, where the ring is a

where q is an integer from 0 to 3;

(5) the Ester compound or its prodrug, or pharmaceutically acceptable salt of any of them in accordance with the above paragraph 2 or paragraph 4, where the ring is a

(6) the Ester compound or its prodrug, or pharmaceutically acceptable salt of any of them in accordance with the above paragraph 5, where the ring And represents a

(7) the Ester compound or its prodrug, or pharmaceutically acceptable salt of any of them in accordance with the above paragraph 6, where X represents-CON(R10)-(CH2)n-, where each R10and n have the same meanings as defined above;

(8) the Ester compound or its prodrug, or pharmaceutically acceptable salt of any of them in accordance with the above paragraph 6, where X represents-COO-(CH2)n -, where n has the same meaning as defined above;

(9) the Ester compound or its prodrug, or pharmaceutically acceptable salt of any of them in accordance with the above paragraph 7 or paragraph 8, where n is 0;

(10) the Ester compound or its prodrug, or pharmaceutically acceptable salt of any of them in accordance with the above paragraph (1)represented by the formula (1')

where each of R2'and R2"independently represents hydrogen, C1-C6-alkyl, C3-C7-cycloalkyl,1-C6-alkoxy, halogen, halogen-C1-C6-alkyl, C1-C6-acyl, C2-C6alkenyl or cyano;

X1represents-O - or-NR10-where R10represents hydrogen, C1-C6alkyl or C3-C7cycloalkyl; and

each of R1, R3, R4, R5, R6, R7, R8, R9, ring C, l, and m have the same meanings as defined above,

or its prodrug, or pharmaceutically acceptable salt of any of them;

(11) the Ester compound or its prodrug, or pharmaceutically acceptable salt of any of them in accordance with the above paragraph (10), where the ring is a

where q PR is dstanley an integer from 0 to 3;

(12) the Ester compound or its prodrug, or pharmaceutically acceptable salt of any of them in accordance with the above paragraph (11), where X1represents-N(R10)-, where R10has the same meaning as defined above;

(13) the Ester compound or its prodrug, or pharmaceutically acceptable salt of any of them in accordance with the above paragraph (11), where X1represents-O-.

(14) the Ester compound or its prodrug, or pharmaceutically acceptable salt of any of them in accordance with the above paragraphs (10)-(13), where the group -(CH2)l- located in the h-position of the benzene ring in the formula (1');

(15) the Ester compound or its prodrug, or pharmaceutically acceptable salt of any of them in accordance with the above paragraphs (10)-(13), where the group -(CH2)l- located in the i-position of the benzene ring in the formula (1');

(16) the Ester compound or its prodrug, or pharmaceutically acceptable salt of any of them in accordance with the above paragraphs (10)-(15), where each of R8and R9independently represents-CON(R18)(R19)-, where each R18and R19has the same meaning as defined above;

(17) the Ester compound or its prodrug, Il the pharmaceutically acceptable salt of any of them in accordance with the above paragraphs (10)-(15), where each of R8and R9independently represents-COO(R20)-, where R20has the same meaning as defined above;

(18) the Ester compound or its prodrug, or pharmaceutically acceptable salt of any of them in accordance with the above paragraphs (12)-(17), where the ring is a6-C14-aryl;

(19) the Ester compound or its prodrug, or pharmaceutically acceptable salt of any of them in accordance with the above paragraph 18, where C6-C14aryl represents phenyl;

(20) the Ester compound or its prodrug, or pharmaceutically acceptable salt of any of them in accordance with the above paragraphs (12)-(17), where the ring is a3-C7-cycloalkyl;

(21) the Ester compound or its prodrug, or pharmaceutically acceptable salt of any of them in accordance with the above paragraphs (12)-(17), where the ring is a

(22) the Ester compound or its prodrug, or pharmaceutically acceptable salt of any of them in accordance with the above paragraph (1), which is chosen from the group including

2,2-bis-ethylcarboxyl-2-phenethyl ester {4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

detroyer 2-phenyl-2-{2-[4-(4'-triptorelin-2-carbonyloxy)phenyl]acetoxymethyl}malonic acid,

diethyl ether 2-(2-{3-methyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{4-[methyl-(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-ethyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

9-(2,2,2-triptoreline)-9H-fluoren-9-ymetray ester {4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

9-(2,2,2-triptoreline)-9H-fluoren-9-ymetray ester 2-{4-[(4'-triptorelin-2-carbonyl)amino]phenyl}propionic acid,

2-phenyl-2-(2,2,2-triptoreline)ethyl ester {4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ester of 2-phenyl-2-(2-{4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

1-(2,2,2-triptoreline)cyclopentylmethyl ester {4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diisopropyl ether 2-phenyl-2-(2-{4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

2-phenyl-2,2-bis-(2,2,2-triptoreline)ethyl ester {4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

dimethyl 2-phenyl-2-(2-{4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)is the responsibility of the howling acid,

diethyl ether 2-cyclopentyl-2-(2-{4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

1-(2,2,2-triptoreline)cyclohexylmethyl ester {4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ester of 2-phenyl-2-{2-[4-(2-trifluoromethyl-benzoylamine)phenyl]acetoxymethyl}malonic acid,

diethyl ether 2-{2-[4-(2-phenoxyethylamine)phenyl]acetoxymethyl}-2-phenylmalonate acid,

diethyl ether 2-{2-[4-(2-butoxycarbonylamino)phenyl]acetoxymethyl}-2-phenylmalonate acid,

diethyl ester of 2-phenyl-2-{2-[4-(2-triftormetilfosfinov)phenyl]acetoxymethyl}malonic acid,

diethyl ether 2-{2-[4-(2-benzoylbenzoate)phenyl]acetoxymethyl}-2-phenylmalonate acid,

diethyl ether 2-{2-[4-(2-benzoylmethylene)phenyl]acetoxymethyl}-2-phenylmalonate acid,

dicyclohexylamine ester 2-phenyl-2-(2-{4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

2,2-bis-cyclohexylcarbonyl-2-phenethyl ester {4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2-phenyl-2,2-bis-phenylcarbamoyloxy ester {4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-isopropylcarbamate-2-phenethyl ester {4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl EF the R 2-benzyl-2-(2-{4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diethyl ether 2-(2-{2-methyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

4-[2-phenyl-2,2-bis-(2,2,2-triptoreline)ethoxycarbonylmethyl]phenyl ester of 4'-triptorelin-2-carboxylic acid,

4-[2-phenyl-2,2-bis-(2,2,2-triptoreline)ethoxycarbonylmethyl]phenyl ether-biphenyl-2-carboxylic acid,

4-[2-phenyl-2,2-bis-(2,2,2-triptoreline)ethoxycarbonylmethyl]phenyl ester 2-butoxybenzoic acid,

diethyl ether of 2-cyclohexyl-2-(2-{4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

2-phenyl-2,2-bis-(2,2,2-triptoreline)ethyl ester {4-[(biphenyl-2-carbonyl)amino]phenyl}acetic acid,

2-phenyl-2,2-bis-(2,2,2-triptoreline)ethyl ester [4-(2-phenoxy-benzoylamine)phenyl]acetic acid,

diethyl ester of 2-phenyl-2-(2-{2-trifluoromethyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

2-phenyl-2,2-bis-propellerblades-ethyl ester {4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-methylcarbamoyl-2-phenethyl ester {4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ether 2-pyridin-2-yl-2-(2-{4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diethyl ether 2-pyridin-3-yl-2-(2-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

4-(2,2-bis-ethylcarboxyl-2-phenyl-ethoxycarbonylmethyl)phenyl ether 4'-triptorelin-2-carboxylic acid,

diethyl ester of 2-phenyl-2-(2-{3-trifluoromethyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

2-phenyl-2,2-bis-(2,2,2-triptoreline)ethyl ester [4-(2-butoxy-benzoylamine)phenyl]acetic acid,

2,2-bis-butylcarbamoyl-2-phenethyl ester {4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ether 2-(2-{4-[(9-oxo-9h-fluoren-1-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{4-[(9h-fluoren-1-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-methyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ether 2-(2-{4-[(4'-methylbiphenyl-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{4-[(4'-methoxybiphenyl-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

3,3-bis-ethylcarbazole-3-phenylpropionic ester {4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

3-phenyl-3,3-bis-propellerblades-propyl ester {4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ester {4-[(biphenyl-2-carbonyl)amino]phenyl}uksu the Noah acid,

2,2-bis-ethylcarboxyl-2-phenethyl ester [4-(2-phenoxy-benzoylamine)phenyl]acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ester [4-(2-butoxy-benzoylamine)phenyl]acetic acid,

diethyl ester of 2-phenyl-2-(2-{4-[(3'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diethyl ether 2-(2-{4-[2-(4-fluoro-benzoyl)benzoylamine]phenyl}acetoxymethyl)-2-phenylmalonate acid,

4-(2,2-bis-ethylcarboxyl-2-phenyl-ethoxycarbonylmethyl)-2-hlorfenilovy ether 4'-triptorelin-2-carboxylic acid,

diethyl ester of 2-phenyl-2-{2-[4-(2-thiophene-3-yl-benzoylamine)phenyl]acetoxymethyl}malonic acid,

diethyl ether 2-(2-{4-[(biphenyl-3-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{4-[isopropyl-(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{4-[cyclohexyl-(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-{2-[4-(2-isopropyl-benzoylamine)phenyl]acetoxymethyl}-2-phenylmalonate acid,

diethyl ether 2-{2-[4-(2-benzyl-benzoylamine)phenyl]acetoxymethyl}-2-phenylmalonate acid,

dipropionyl ester 2-phenyl-2-(2-{4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diisobutylamine ester 2-phenyl-2-(2-{4[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diethyl ester of 2-phenyl-2-{2-[4-(2-triptoreline-benzoylamine)phenyl]acetoxymethyl}malonic acid,

diethyl ether 2-{2-[4-(2-butoxycarbonyl-benzoylamine)phenyl]acetoxymethyl}-2-phenylmalonate acid,

2,2-bis-isobutylamino-2-phenethyl ester {4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-(3-methyl-butylcarbamoyl)-2-phenethyl ester {4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ether 2-(2-{4-[ethyl-(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

2,2-bis-ethylcarboxyl-2-phenethyl ester [4-(2-cyclohexyl-benzoylamine)phenyl]acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ester {4-[(4'-chlorobiphenyl-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ester {4-[(3',4'-dichlorobiphenyl-2-carbonyl)amino]phenyl}acetic acid,

2-phenyl-2,2-bis-propellerblades-ethyl ester {3-methyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis(2-methoxy-ethylcarbamate)-2-phenethyl ester {4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ether 2-[2-(4-{[2-methyl-4-(4-trifluoromethyl-phenyl)thiazole-5-carbonyl]amino}phenyl)acetoxymethyl]-2-phenylmalonate acid,

2,2-bis-ethylcarboxyl-2-phenethyl ester (4-{[2-methyl-4-(4-cryptomite is-phenyl)thiazole-5-carbonyl]amino}phenyl)acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ester (4-{[2-(4-trifluoromethyl-phenyl)pyridine-3-carbonyl]amino}phenyl)acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ester (3-methyl-4-{[2-(4-trifluoromethyl-phenyl)pyridine-3-carbonyl]amino}phenyl)acetic acid,

diethyl ether 2-(2-{3-ethyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-isopropyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ether 2-(2-{3-isopropyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

3,3-bis-ethylcarbazole-3-phenylpropionyl ether {3-ethyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-isobutyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ether 2-(2-{3-isobutyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-chloro-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-bromo-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-Carbo who yl)amino]phenyl}acetic acid,

2-phenyl-2,2-bis-propellerblades-ethyl ester {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-methylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

3,3-bis-ethylcarbazole-3-phenylpropionyl ether {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-benzylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

4,4-bis-ethylcarbamate-4-privately ether {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-diethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-diisopropylamino-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ether 2-(2-{3-diethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-diisopropylamino-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-(isopropylaminocarbonyl)-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ether 2-(2-{3-(ethylmethylamino)-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-(ethylmethylamino)-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

3,3-bis-ethylcarbazole-3-phenylpropionyl ether {3-(ethylmethylamino)-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-(piperidine-1-carbonyl)-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-(pyrrolidin-1-carbonyl)-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-(pyrrolidin-1-carbonyl)-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-(methylpropanoyl)-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

3,3-bis-ethylcarbazole-3-phenylpropionyl ether {3-(methylpropanoyl)-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2-ethylcarboxyl-2-phenethyl ester (3-dimethylcarbamoyl-4-[(4'-triptorelin the-2-carbonyl)amino]phenyl}acetic acid,

diethyl ester of 2-phenyl-2-(2-{3-(pyrrolidin-1-carbonyl)-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diethyl ester of 2-phenyl-2-(2-{3-(piperidine-1-carbonyl)-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

2-phenyl-2-propionylcarnitine ether {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2-phenyl-2-propionylcarnitine ether {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2-(2,5-dioxo-pyrrolidin-1-yl)-2-phenethyl ether {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2-ethylcarbamate-benzyl ether {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2-ethylcarboxylate-benzyl ether {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

hydrochloride of 2-isopropylamino-2-phenethyl ester {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ester [3-dimethylcarbamoyl-4-(2-trifluoromethyl-benzoylamine)phenyl]acetic acid,

diethyl ether 2-{2-[3-dimethylcarbamoyl-4-(2-trifluoromethyl-benzoylamine)phenyl]acetoxymethyl}-2-phenylmalonate acid,

diethyl EF the R 2-[2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxy)ethyl]-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-forbiden-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{4-[(4'-bromobiphenyl-2-carbonyl)amino]-3-dimethylcarbamoyl}acetoxymethyl)-2-phenylmalonate acid,

2-acetylamino-2-phenethyl ether {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2 Butylimino-2-phenethyl ether {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ester [4-(2-benzoyl-benzoylamine)-3-dimethylcarbamoyl]acetic acid,

diethyl ether 2-{2-[4-(2-benzoyl-benzoylamine)-3-dimethylcarbamoyl]acetoxymethyl}-2-phenylmalonate acid,

dimethyl 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-cyclopentyl-2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diethyl ether of 2-cyclohexyl-2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diethyl ether 2-(2-{4-[(4'-chlorobiphenyl-2-carbonyl)amino]-3-dimethylcarbamoyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{4-[(4'-acetyl-biphenyl-2-carbonyl)AMI is about]-3-dimethylcarbamoyl}acetoxymethyl)-2-phenylmalonate acid,

2,2-bis-ethylcarboxyl-2-phenethyl ester [3-dimethylcarbamoyl-4-(2-phenoxy-benzoylamine)phenyl]acetic acid,

diethyl ether 2-{2-[3-dimethylcarbamoyl-4-(2-phenoxy-benzoylamine)phenyl]acetoxymethyl}-2-phenylmalonate acid,

diethyl ether 2-(2-{4-[(4'-cyanobiphenyl-2-carbonyl)amino]-3-dimethylcarbamoyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4-methyl-4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(5-methyl-4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

2 methanesulfonamido-2-phenethyl ether {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

ethyl ester of 3-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxy)-2-phenylpropionic acid,

2-(methylpropionamide)-2-phenethyl ether {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ether 2-[3-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxy)propyl]-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(5-methoxy-4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

Dyatlov the th ether 2-(2-{4-[(5-chloro-4'-triptorelin-2-carbonyl)amino]-3-dimethylcarbamoyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(6-methyl-4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

di-2,2,2-triptoreline ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(2'-fluoro-4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{5-dimethylcarbamoyl-2-fluoro-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-bromo-5-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-chloro-5-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(3'-fluoro-4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{4-[(3'-chloro-4'-triptorelin-2-carbonyl)amino]-3-dimethylcarbamoyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-(5-nitropyridine-2-yl)malonic acid,

diethyl ether 2-(5-aminopyridine-2-yl)-2-(2-{3-dimetilan moil-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-pyridin-2-elmaloglou acid,

diethyl ether 2-(2-{3-chloro-5-dimethylcarbamoyl-2-fluoro-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-bromo-5-dimethylcarbamoyl-2-fluoro-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-o-tolyl-malonic acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-m-tolyl-malonic acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-p-tolyl-malonic acid,

diethyl ether 2-(2-chlorophenyl)-2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diethyl ether 2-(3-chlorophenyl)-2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diethyl ether 2-(4-chlorophenyl)-2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-ka is bonyl)amino]phenyl}acetoxymethyl)-2-phenylethanol acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-(2-methoxyphenyl)malonic acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-(3-methoxyphenyl)malonic acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-(4-methoxyphenyl)malonic acid,

diethyl ether 2-(2-{4-[(5,4'-bis-triptorelin-2-carbonyl)amino]-3-dimethylcarbamoyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{4-[(6-chloro-4'-triptorelin-2-carbonyl)amino]-3-dimethylcarbamoyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(6-fluoro-4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-[2-(2-{3-dimethylcarbamoyl-4-[(5-methyl-4'-triptorelin-2-carbonyl)amino]phenyl}acetoxy)ethyl]-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(5-ethoxy-4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(5-isopropoxy-4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-[2-(2-{4-[(5',4'-bis-trifloromethyl the Nile-2-carbonyl)amino]-3-dimethylcarbamoyl}acetoxy)ethyl]-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(6-methoxy-4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(3-methyl-4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-{2-[4-(2,4-bis-trifluoromethyl-benzoylamine)-3-dimethylcarbamoyl]acetoxymethyl}-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-methylbiphenyl-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether with 2-ethyl-4-trifluoromethyl-benzoylamine)phenyl]acetoxymethyl}-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-ethylbiphenyl-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-isopropyl-biphenyl-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-isopropyl-biphenyl-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-{2-[3-dimethylcarbamoyl-4-(2-Isopropenyl-4-trifluoromethyl-benzoylamine)phenyl]acetoxymethyl}-2-phenylmalonate acid,

diethyl ether 2-{2-[3-dimethylcarbamoyl-4-(2-isopropyl-4-trifluoromethyl-benzoylamine)phenyl]acetoxymethyl}-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethyl who carbamoyl-4-[2-(3-trifluoromethyl-phenylamino)benzoylamine]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-{2-[3-dimethylcarbamoyl-4-(4'-triptorelin-2-carbonyloxy)phenyl]acetoxymethyl}-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[2-(3-triptoreline)benzoylamine]phenyl}acetoxymethyl)-2-phenylmalonate acid,

2-ethyl-2-privately ether {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[2-(4-triptoreline)benzoylamine]phenyl}acetoxymethyl)-2-phenylmalonate acid,

1-phenyl-cyclopropylmethyl ether {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-definiately ether {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

1-phenyl-cyclopentylmethyl ether {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

3-hydroxy-2-hydroxymethyl-2-phenylpropionyl ether {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

3-acetoxy-2-acetoxymethyl-2-phenylpropionyl ether {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-thiophene-2-elmaloglou acid,

diethyl ether 2-(2-{3-DIMET carbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-thiophene-3-elmaloglou acid,

diethyl ether 2-(2-{4-dimethylcarbamoyl-5-[(4'-triptorelin-2-carbonyl)amino]pyridin-2-yl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-(3-methylthiophene-2-yl)malonic acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-(5-methylthiophene-2-yl)malonic acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-thiazol-2-elmaloglou acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-isopropylmalonic acid,

diethyl ether 2-terbutyl-2-(2-{3-dimethylcarbamoyl-4-[(4-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-isobutylamino acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-propylmalonic acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-ethylmalonic acid,

diethyl ester of 2-butyl-2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-CT is of IMT)amino]phenyl}acetoxymethyl)malonic acid,

diethyl ether 2-allyl-2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

ethyl ester of 3-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxy)-2,2-bis-ethoxycarbonylpyrimidine acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-(1-methylbutyl)malonic acid,

diethyl ether 2-(2-{3-ethoxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-hydroxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-methoxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ether 2-(2-{3-methoxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

2-phenyl-2,2-bis-propellerblades-ethyl ester {3-methoxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

3,3-bis-ethylcarbazole-3-phenylpropionyl ether {3-methoxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-ethoxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

3,3-bis-ethylcarbazole-3-phenylpropionyl e is Il - {3-ethoxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ether 2-(2-{3-isopropoxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-isopropoxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

3,3-bis-ethylcarbazole-3-phenylpropionyl ether {3-isopropoxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-propoxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-benzyloxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ether 2-(2-{3-benzyloxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-hydroxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-{2-[3-methoxy-4-(4'-triptorelin-2-carbonyloxy)phenyl]acetoxymethyl}-2-phenylmalonate acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-dimethylamino-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-piperidine-1-yl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-pyrrolidin-1-yl-4-[4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ester of 2-phenyl-2-(2-{3-piperidine-1-yl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diethyl ester of 2-phenyl-2-(2-{3-pyrrolidin-1-yl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diethyl ether 2-(2-{3-dimethylamino-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-morpholine-4-yl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-diethylamino-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-[2-(2-{2-methyl-3-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxy)ethyl]-2-phenylmalonate acid,

diethyl ester of 2-phenyl-2-(2-{3-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diethyl ester of 2-phenyl-2-[2-(2-{3-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxy)ethyl]malonic acid,

3,3-bis-ethylcarbazole-3-phenylpropionyl ether {3-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

3-phenyl-3,3-bis-propellerblades-propyl ether {3-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ether 2-[2-(2-{4-methyl-3-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxy)ethyl]-2-f is nirmaladevi acid,

diethyl ether 2-[2-(2-{2-methyl-5-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxy)ethyl]-2-phenylmalonate acid,

3,3-bis-isopropylcarbamate-3-phenylpropionyl ether {3-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

3,3-bis-ethylcarbazole-3-phenylpropionyl ether {2-methyl-3-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

4,4-bis-ethylcarbamate-4-privately ether {2-methyl-3-[(4'-triptorelin-2-carbonyl)amino]phenyl)acetic acid,

3-phenyl-3,3-bis-propyltetrahydropyran ether {2-methyl-3-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

3,3-bis-ethylcarbazole-3-phenylpropionyl ether {2-methoxy-3-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ether 2-[2-(2-{2-methoxy-3-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxy)ethyl]-2-phenylmalonate acid,

3,3-bis-ethylcarbazole-3-phenylpropionyl ether {2-ethoxy-3-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ether 2-[2-(2-{2-ethoxy-3-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxy)ethyl]-2-phenylmalonate acid,

diethyl ether 2-[2-(2-{2-isopropoxy-3-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxy)ethyl]-2-phenylmalonate acid,

diethyl ether 2-[2-(2-{2-methoxycarbonyl-3-[(4'-triptorelin-2-carbonyl)amino]FeNi is}acetoxy)ethyl]-2-phenylmalonate acid,

diethyl ether 2-[2-(2-{2-ethoxy-5-methyl-3-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxy)ethyl]-2-phenylmalonate acid,

2-[9-(2,2,2-Cryptor-ethylcarbamate)-9h-fluoren-9-yl]ethyl ester 4-[(4'-triptorelin-2-carbonyl)amino]benzoic acid,

2-(9h-fluoren-9-yl)ethyl ester 4-[(4'-triptorelin-2-carbonyl)amino]benzoic acid,

2-[9-(2,2,2-triptoreline)-9h-fluoren-9-yl]ethyl ester of n-biphenyl-2-literaturenobel acid,

2-[(biphenyl-2-carbonyl)amino]ethyl ester 4-[(4'-triptorelin-2-carbonyl)amino]benzoic acid,

2-(2-biphenyl-2-yl-acetylamino)ethyl ester 4-[(4'-triptorelin-2-carbonyl)amino]benzoic acid,

3-naphthalene-1-yl-3-(2,2,2-Cryptor-ethylcarbamate)propyl ether of 4-[(4'-triptorelin-2-carbonyl)amino]benzoic acid,

3-[2-(2,2,2-Cryptor-ethylcarbamate)naphthalene-1-yl]propyl ester 4-[(4'-triptorelin-2-carbonyl)amino]benzoic acid,

3,3-diphenyl-3-(2,2,2-Cryptor-ethylcarbamate)propyl ether of 4-[(4'-triptorelin-2-carbonyl)amino]benzoic acid,

3-biphenyl-2-yl-3-(2,2,2-triptoreline)propyl ether of 4-[(4'-triptorelin-2-carbonyl)amino]benzoic acid,

3-phenyl-3-(2,2,2-triptoreline)propyl ether of 4-[(4'-triptorelin-2-carbonyl)amino]benzoic acid,

2-[8-(2,2,2-triptoreline)naphthalene-1-yl]E. the silt ester 4-[(4'-triptorelin-2-carbonyl)amino]benzoic acid,

3-(2,6-dichlorophenyl)-3-(2,2,2-triptoreline)propyl ether of 4-[(4'-triptorelin-2-carbonyl)amino]benzoic acid,

3-(2-chlorophenyl)-3-(2,2,2-triptoreline)propyl ether of 4-[(4'-triptorelin-2-carbonyl)amino]benzoic acid,

diethyl ester of 2-phenyl-2-(2-{4-[(4'-triptorelin-2-carbonyl)amino]benzoyloxy}ethyl) - malonic acid,

diethyl ether 2-(2-{3-methyl-4-[(4'-triptorelin-2-carbonyl)amino]benzoyloxy}ethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{2-chloro-4-[(4'-triptorelin-2-carbonyl)amino]benzoyloxy}ethyl)-2-phenylmalonate acid,

diethyl ester of 2-phenyl-2-{2-[4-(4'-triptorelin-2-carbonyloxy)benzoyloxy]ethyl}malonic acid,

diethyl ether 2-{2-[4-(2-benzoyl-benzoyloxy)benzoyloxy]ethyl}-2-phenylmalonate acid,

3,3-bis-ethylcarbazole-3-phenylpropionic ester 4-[(4'-triptorelin-2-carbonyl)amino]benzoic acid,

4-(3,3-bis-ethylcarbazole-3-phenylpropionyl)-2-hlorfenilovy ether 4'-triptorelin-2-carboxylic acid,

4-(3,3-bis-ethylcarbazole-3-phenyl-propoxycarbonyl)phenyl ether 4'-triptorelin-2-carboxylic acid,

4-(3,3-bis-ethylcarbazole-3-phenylpropionyl)-2,6-dichlorphenoxy ether 4'-triptorelin-2-carboxylic acid,

2-[9-(2,2,2-triptoreline)-9h-fluoren-9-yl]ethyl ester 4-methyl-[(4'-triptorelin-2-carbonyl)amino]cyclohexanecarboxylic acid,

2-[9-(2,2,2-Cryptor-ethylcarbamate)-9h-fluoren-9-yl]ethyl ester 4-[(4'-triptorelin-2-carbonyl)amino]cyclohexanecarboxylic acid,

3-phenyl-3-(2,2,2-triptoreline)propyl ether of 4-[(4'-triptorelin-2-carbonyl)amino]cyclohexanecarboxylic acid,

diethyl ester of 2-phenyl-2-{4-[(4'-triptorelin-2-carbonyl)amino]cyclohexanecarboxylate}malonic acid,

diethyl ester of 2-phenyl-2-(2-{4-[(4'-triptorelin-2-carbonyl)amino]cyclohexanecarbonyl}ethyl) - malonic acid,

diethyl ester of 2-phenyl-2-(2-{4-[(4'-triptorelin-2-carbonyl)amino]piperidine-1-yl}acetoxymethyl)malonic acid,

diethyl ester of 2-phenyl-2-(2-{4-[(4'-triptorelin-2-carbonyl)amino]indol-1-yl}acetoxymethyl)malonic acid,

diethyl ether 2-(2-{2-methyl-4-[(4'-triptorelin-2-carbonyl)amino]benzimidazole-1-yl}acetoxymethyl)-2-phenylmalonate acid,

2,2-bis-ethylcarboxyl-2-phenethyl ester [2-oxo-3-(4'-triptorelin-2-carbonyl)-2,3-dihydro-benzoxazol-6-yl]acetic acid,

diethyl ether 2-(2-{3-etoxycarbonyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(3-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}propionyloxy)-2-phenylmalonate acid,

2,2-bis-ethylcarboxyl-2-phenylethyl the new ether 4-{[(4'-triptorelin-2-carbonyl)amino]methyl}benzoic acid,

ethylcarbodiimide ester 3-{4-[(4'-triptorelin-2-carbonyl)amino]phenyl}propionic acid,

benzyl ether of 5-(2,2-bis-ethylcarboxyl-2-phenyl-ethoxycarbonylmethyl)-2-[(4'-triptorelin-2-carbonyl)amino]benzoic acid,

5-(2,2-bis-ethylcarboxyl-2-phenyl-ethoxycarbonylmethyl)-2-[(4'-triptorelin-2-carbonyl)amino]benzoic acid,

ethyl ester of 5-(2,2-bis-ethylcarboxyl-2-phenyl-ethoxycarbonylmethyl)-2-[(4'-triptorelin-2-carbonyl)amino]benzoic acid,

diethyl ester of 2-phenyl-2-(2-{4-[(4'-triptorelin-2-carbonyl)amino]benzoimidazol-1-yl}acetoxymethyl)malonic acid,

3-{[(4'-triptorelin-2-carbonyl)amino]methyl}benzoic acid 3,3-bis-ethylcarbazole-3-phenylpropionyl ether acid,

methyl ester 5-(2,2-bis-ethylcarboxyl-2-phenyl-ethoxycarbonylmethyl)-2-[(4'-triptorelin-2-carbonyl)amino]benzoic acid,

diethyl ether 2-(2-{3-benzyloxycarbonyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-carboxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-{2-[2-oxo-3-(4'-triptorelin-2-carbonyl)-2,3-dihydroisoxazole-6-yl]acetoxymethyl}-2-phenylmalonate acid,

diethyl ether 2-{2-[8-oxo-7-(4'-triptorelin-2-Carbo who yl)-7-azabicyclo[4.2.0]OCTA-1(6),2,4-triene-3-yl]acetoxymethyl}-2-phenylmalonate acid,

diethyl ether 2-(2-{3-isopropoxycarbonyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-methoxycarbonyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-[2-(3-dimethylcarbamoyl-4-{[1-(2-nitrol-4-trifluoromethyl-phenyl)pyrrolidin-2-carbonyl]amino}phenyl)acetoxymethyl]-2-phenylmalonate acid,

diethyl ether 2-(2-{3-acetylamino-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-methoxycarbonylamino-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-(4-methyl-thiazol-2-yl)-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ester of 2-phenyl-2-(2-{6-[(4'-triptorelin-2-carbonyl)amino]biphenyl-3-yl}acetoxymethyl)malonic acid,

diethyl ether 2-(2-{3-formyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylaminomethyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-(methoxymethylethoxy)-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate is islote,

diethyl ether 2-(2-{3-isobutyryl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid, and

diethyl ether 2-(2-{3-(1-hydroxy-2-methylpropyl)-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acids;

(23) the Ester compound or its prodrug, or pharmaceutically acceptable salt of any of them in accordance with the above paragraph (1), which is chosen from the group including

2,2-bis-ethylcarboxyl-2-phenethyl ester 4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ester of 2-phenyl-2-{2-[4-[(4'-triptorelin-2-carbonyloxy)phenyl]acetoxymethyl}malonic acid,

diethyl ether 2-(2-{3-methyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{4-[methyl-(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-ethyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

9-(2,2,2-triptoreline)-9h-fluoren-9-ymetray ether (4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

9-(2,2,2-triptoreline)-9h-fluoren-9-ymetray ester {4-[(4'-triptorelin-2-carbonyl)amino]phenyl}propionic acid,

2-phenyl-2-(2,2,2-crypto ethylcarbitol)ethyl ester {4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ester of 2-phenyl-2-(2-{4-[4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diisopropyl ether 2-phenyl-2-(2-{4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

2-phenyl-2,2-bis-(2,2,2-triptoreline)ethyl ester {4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

dimethyl 2-phenyl-2-(2-{4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diethyl ether 2-cyclopentyl-2-(2-{4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

dicyclohexylamine ester 2-phenyl-2-(2-{4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

2,2-bis-cyclohexylcarbonyl-2-phenethyl ester {4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2-phenyl-2,2-bis-phenylcarbamoyl-ethyl ester {4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-isopropylcarbamate-2-phenethyl ester {4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ether 2-benzyl-2-(2-{4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxylation acid,

diethyl ether 2-(2-{2-methyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl-2-phenylmalonate acid,

4-[2-phenyl-2,2-bis-(2,2,2-referencemanual)ethoxycarbonylmethyl]phenyl ester of 4'-triptorelin-2-carboxylic acid,

4-[2-phenyl-2,2-bis-(2,2,2-triptoreline)ethoxycarbonylmethyl]phenyl ether-biphenyl-2-carboxylic acid,

diethyl ether of 2-cyclohexyl-2-(2-{4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

2-phenyl-2,2-bis-(2,2,2-triptoreline)ethyl ester {4-[(biphenyl-2-carbonyl)amino]phenyl}acetic acid,

diethyl ester of 2-phenyl-2-(2-{2-trifluoromethyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

2,2-bis-methylcarbamoyl-2-phenethyl ester {4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ether 2-pyridin-2-yl-2-(2-{4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxylation acid,

diethyl ether 2-pyridin-3-yl-2-(2-{4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

4-(2,2-bis-ethylcarboxyl-2-phenyl-ethoxycarbonylmethyl)phenyl ether 4'-triptorelin-2-carboxylic acid,

diethyl ester of 2-phenyl-2-(2-{3-trifluoromethyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

2,2-bis-butylcarbamoyl-2-phenethyl ester {4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-methyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ether 2-2-{4-[(4'-methylbiphenyl-2-carbonyl}-amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{4-[(4'-methoxybiphenyl-2-carbonyl}amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

3,3-bis-ethylcarbazole-3-phenylpropionic ester {4-[(4'-triptorelin-2-carbonyl}amino]phenyl}acetic acid,

3-phenyl-3,3-bis-propyltetrahydropyran ester {4-[(4'-triptorelin-2-carbonyl}amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ester {4-[(biphenyl-2-carbonyl)amino]phenyl}acetic acid,

diethyl ester of 2-phenyl-2-(2-{4-[(3'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

4-(2,2-bis-ethylcarboxyl-2-phenyl-ethoxycarbonylmethyl)-2-hlorfenilovy ether 4'-triptorelin-2-carboxylic acid,

diethyl ether 2-(2-{4-[isopropyl-(4'-triptorelin-2-carbonyl}amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{4-[cyclohexyl-(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

dipropionyl ester 2-phenyl-2-(2-{4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diisobutylamine ester 2-phenyl-2-(2-{4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

2,2-bis-isobutylamino-2-phenethyl ester {4-[(4'-triptorelin-2-carbonyl}amino]phenyl}acetic acid,

2,2-bis(3-methyl-butylcarbamoyl)-2-phenylethylene the ester {4-[(4'-triptorelin-2-carbonyl}amino]phenyl}acetic acid,

diethyl ether 2-(2-{4-[ethyl-(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

2,2-bis(ethylcarbamate-2-phenyl)ethyl ester {4-[(4'-chlorobiphenyl-2-carbonyl)amino]phenyl}acetic acid,

{2,2-bis(ethylcarbamate-2-phenethyl ester 4-[(3',4'-dichlorobiphenyl-2-carbonyl)amino]phenyl}acetic acid,

2-phenyl-2,2-bis-propellerblades-ethyl ester {3-methyl-4-[(4'-triptorelin-2-carbonyl}amino]phenyl}acetic acid,

2,2-bis-(2-methoxyethanol)-2-phenethyl ester 4-[(4'-triptorelin-2-carbonyl}amino]phenyl}acetic acid,

diethyl ether 2-(2-{3-ethyl-4-[(4'-triptorelin-2-carbonyl}amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-isopropyl-4-[(4'-triptorelin-2-carbonyl}amino]phenyl}acetic acid,

diethyl ether 2-(2-{3-isopropyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

3,3-bis-ethylcarbazole-3-phenylpropionyl ether {3-ethyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-isobutyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl)acetic acid,

diethyl ether 2-(2-{3-isobutyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

dieti the new ester 2-(2-{3-chloro-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-bromo-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

2-phenyl-2,2-bis-profilerenumeration ether {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-methylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

3,3-bis-ethylcarbazole-3-phenethyl ether {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ether 2-(2-{3-diethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-benzylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

4,4'-bis-ethylcarbamate-4-privately ether {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-diethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-diisopropylamino-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

dieti the new ester 2-(2-{3-diethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-diisopropylamino-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-(isopropylaminocarbonyl)-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ether 2-(2-{3-(ethylmethylamino)-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-(ethylmethylamino)-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

3,3-bis-ethylcarbazole-3-phenylpropionyl ether {3-(ethylmethylamino)-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-(piperidine-1-carbonyl)-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-(pyrrolidin-1-carbonyl)-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-(methylpropanoyl)-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

3,3-bis-ethylcarbazole-3-phenethyl ether {3-(methylpropanoyl)-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2-ethyl-carbarnoyl-2-phenethyl ether {3-(dimethylcarbamoyl)-4-[(4'-triptorelin-carbonyl)amino]phenyl}acetic acid,

diethyl ester of 2-phenyl-2-(2-{3-(pyrrolidin-1-carbonyl)-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diethyl ester of 2-phenyl-2-(2-{3-(piperidine-1-carbonyl)-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

2-phenyl-2-propionamido-ethyl ester {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2-phenyl-2-propionamido-ethyl ester {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2-(2,5-dioxopiperidin-1-yl)-2-phenethyl ether {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2-ethylcarbamate-benzyl ether {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2-ethylcarboxylate-benzyl ether {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

hydrochloride of 2-isopropylamino-2-phenethyl ester {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ether 2-[2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxy)ethyl]-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-fluoro-biphenyl-2-carbonyl)amino]phenyl}acetoxymethyl}-2-phenylmalonate acid,

diethyl ether 2-(2-{4-[(4'-bromo-biphenyl-2-carbonyl)amino]-3-dimethylcarbamoyl}acetoxymethyl)-2-phenylmalonate acid,

2-acetylamino-2-phenethyl ether {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2 Butylimino-2-phenethyl ether {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

dimethyl 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-cyclopentyl-2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diethyl ether of 2-cyclohexyl-2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-malonic acid,

diethyl ether 2-(2-{4-[(4'-chlorobiphenyl-2-carbonyl)amino]-3-dimethylcarbamoyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{4-[(4'-acetyl-biphenyl-2-carbonyl)amino]-3-dimethylcarbamoyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{4-[(4'-cyano-biphenyl-2-carbonyl)amino]-3-dimethylcarbamoyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4-methyl-4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether -(2-{3-dimethylcarbamoyl-4-[(5-methyl-4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

2 methanesulfonamido-2-phenethyl ether {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

ethyl ester of 3-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxy)-2-phenylpropionic acid,

2-(methylpropionamide)-2-phenethyl ether {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ether 2-[3-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxy)propyl]-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(5-methoxy-4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{4-[5-chloro-4'-triptorelin-2-carbonyl)amino]-3-dimethylcarbamoyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(6-methyl-4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

di-2,2,2-triptoreline ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(2'-fluoro-4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{5-dimethylcarbamoyl-2-fluoro-4-[(4'-triptorelin-2-carbonyl)am is but]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-bromo-5-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-chloro-5-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(3'-fluoro-4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{4-(3'-chloro-4'-triptorelin-2-carbonyl)amino]-3-dimethylcarbamoyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-(5-nitro-pyridin-2-yl)malonic acid,

diethyl ether 2-(5-aminopyridine-2-yl)-2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-pyridin-2-elmaloglou acid,

diethyl ether 2-(2-{3-chloro-5-dimethylcarbamoyl-2-fluoro-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-bromo-5-dimethylcarbamoyl-2-fluoro-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[('-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-o-tolyl-malonic acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-m-tolyl-malonic acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-p-tolyl-malonic acid,

diethyl ether 2-(2-chlorophenyl)-2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diethyl ether 2-(3-chlorophenyl)-2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diethyl ether 2-(4-chlorophenyl)-2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylethanol acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-(2-methoxyphenyl)malonic acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-(3-methoxyphenyl)malonic acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-(4-methoxyphenyl)malonic acid,

diethyl ether 2-(2-{4-(5,4'-bis-triptorelin-2-carbonyl)amino]-3-dim is talkability}acetoxymethyl)-2-phenyl}malonic acid,

diethyl ether 2-(2-{4-(6-chloro-4'-triptorelin-2-carbonyl)amino]-3-dimethylcarbamoyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(6-fluoro-4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-[2-(2-{3-dimethylcarbamoyl-4-[(5-methyl-4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(5-ethoxy-4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(5-isopropoxy-4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-[2-(2-{4-[(5,4'-bis-4'-triptorelin-2-carbonyl)amino]-3-dimethylcarbamoyl}acetoxy)ethyl]-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(6-methoxy-4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(3-methyl-4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-{2-[4-(2,4-bis-trifluoromethyl-benzoylamine)-3-dimethylcarbamoyl]acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-methylbiphenyl-2-carbon is l)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-{2-[3-dimethylcarbamoyl-4-(2-ethyl-4-trifluoromethyl-benzoylamine)phenyl]acetoxymethyl}-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-ethylbiphenyl-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-isopropyl-biphenyl-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-isopropyl-biphenyl-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-{2-[3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyloxy)phenyl]acetoxymethyl}-2-phenylmalonate acid,

2-ethyl-2-privately ether {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

1-phenyl-cyclopropylmethyl ether {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-definiately ether {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

1-phenyl-cyclopentylmethyl ether {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

3-hydroxy-2-hydroxymethyl-2-phenylpropionyl ether {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

3-acetoxy-2-acetoxymethyl-2-phenylpropionyl ether {3-metilcarbamat-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-thiophene-2-elmaloglou acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-thiophene-3-elmaloglou acid,

diethyl ether 2-(2-{4-dimethylcarbamoyl-5-[(4'-triptorelin-2-carbonyl)amino]pyridin-2-yl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-(3-methylthiophene-2-yl)malonic acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-(5-methylthiophene-2-yl)malonic acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-thiazol-2-elmaloglou acid,

diethyl ether 2-(2-{3-ethoxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-hydroxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-methoxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ether 2-(2-{3-methoxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate,

2-phenyl-2,2-bis-propellerblades-ethyl ester {3-methoxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

3,3-bis-ethylcarbazole-3-phenylpropionyl ether {3-methoxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-ethoxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

3,3-bis-ethylcarbazole-3-phenylpropionyl ether {3-ethoxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ether 2-(2-{3-isopropoxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-isopropoxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

3,3-bis-ethylcarbazole-3-phenylpropionyl ether {3-isopropoxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-propoxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-benzyloxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ether 2-(2-{3-benzyloxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-hydroxy-4-[(4'-triptorelin-2-carbonyl)and the eno]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-{2-[3-methoxy-4-[(4'-triptorelin-2-carbonyloxy)phenyl]acetoxymethyl}-2-phenylmalonate acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-dimethylamino-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-piperidine-1-yl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-pyrrolidin-1-yl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ester of 2-phenyl-2-(2-{3-piperidine-1-yl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diethyl ester of 2-phenyl-2-(2-{3-pyrrolidin-1-yl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diethyl ether 2-(2-{3-dimethylamino-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether (2-{3-morpholine-4-yl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-diethylamino-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-[2-(2-{2-methyl-3-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxy)ethyl]-2-phenylmalonate acid,

diethyl ester of 2-phenyl-2-(2-{3-[(4'-triptorelin the l-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diethyl ester of 2-phenyl-2-[2-(2-{3-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxy)ethyl]malonic acid,

3,3-bis-ethylcarbazole-3-phenylpropionyl ether {3-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

3-phenyl-3,3-bis-propellerblades-propyl ether {3-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ether 2-[2-(2-{4-methyl-3-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxyethyl)-2-phenylmalonate acid,

diethyl ether 2-[2-(2-{2-methyl-5-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxy)ethyl]-2-phenylmalonate acid,

3,3-bis-isopropylcarbamate-3-phenylpropionyl ether {3-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

3,3-bis-ethylcarbazole-3-phenylpropionyl ether {2-methyl-3-[(4'-triptorelin-2-carbonyl)amino]phenyl)acetic acid,

4,4-bis-ethylcarbamate-4-privately ether {2-methyl-3-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

3-phenyl-3,3-bis-propellerblades-propyl ether (2-methyl-3-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

3,3-bis-ethylcarbazole-3-phenylpropionyl ether {2-methoxy-3-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

di is tilby ester 2-[2-(2-{2-methoxy-3-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxy)ethyl]-2-phenylmalonate acid,

3,3-bis-ethylcarbazole-3-phenylpropionyl ether {2-ethoxy-3-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ether 2-[2-(2-{2-ethoxy-3-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxy)ethyl]-2-phenylmalonate acid,

diethyl ether 2-[2-(2-{2-isopropoxy-3-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxy)ethyl]-2-phenylmalonate acid,

diethyl ether 2-[2-(2-{2-methoxycarbonyl-3-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxy)ethyl]-2-phenylmalonate acid,

diethyl ether 2-[2-(2-{2-ethoxy-5-methyl-3-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxy)ethyl]-2-phenylmalonate acid,

2-[9-(2,2,2-triptoreline)-9h-fluoren-9-yl]ethyl ester 4-[(4'-triptorelin-2-carbonyl)amino]benzoic acid,

2-[9h-fluoren-9-yl]ethyl ester 4-[(4'-triptorelin-2-carbonyl)amino]benzoic acid,

2-[9-(2,2,2-triptoreline)-9h-fluoren-9-yl]ethyl ester of n-biphenyl-2-literaturenobel acid,

2-[(biphenyl-2-carbonyl)amino]ethyl ester 4-[(4'-triptorelin-2-carbonyl)amino]benzoic acid,

2-(2-biphenyl-2-yl-acetylamino)ethyl ester 4-[(4'-triptorelin-2-carbonyl)amino]benzoic acid,

3-naphthalene-1-yl-3-(2,2,2-triptoreline)propyl ether of 4-[(4'-triptorelin-2-carbonyl)amino]benzoic acid,

3-[2-(2,2,2-triptorelin email)naphthalene-1-yl]propyl ester 4-[(4'-triptorelin-2-carbonyl)amino]benzoic acid,

3,3-diphenyl-3-(2,2,2-triptoreline)propyl ether of 4-[(4'-triptorelin-2-carbonyl)amino]benzoic acid,

3-biphenyl-2-yl-3-(2,2,2-triptoreline)propyl ether of 4-[(4'-triptorelin-2-carbonyl)amino]benzoic acid,

3-phenyl-3-(2,2,2-triptoreline)propyl ether of 4-[(4'-triptorelin-2-carbonyl)amino]benzoic acid,

2-[8-(2,2,2-triptoreline)naphthalene-1-yl]ethyl ester 4-[(4'-triptorelin-2-carbonyl)amino]benzoic acid,

3-[(2,6-dichlorophenyl)-3-(2,2,2-triptoreline)propyl ether of 4-[(4'-triptorelin-2-carbonyl)amino]benzoic acid,

3-(2-chlorophenyl)-3-(2,2,2-triptoreline)propyl ether of 4-[(4'-triptorelin-2-carbonyl)amino]benzoic acid,

diethyl ester of 2-phenyl-2-(2-{4-[(4'-triptorelin-2-carbonyl)amino]benzoyloxy}ethyl) - malonic acid,

diethyl ether 2-(2-{3-methyl-4-[(4'-triptorelin-2-carbonyl)amino]benzoyloxy}ethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{2-chloro-4-[(4'-triptorelin-2-carbonyl)amino]benzoyloxy}ethyl)-2-phenylmalonate acid,

diethyl ester of 2-phenyl-2-{2-[4-[(4'-triptorelin-2-carbonyloxy)benzoyloxy]ethyl}malonic acid,

3,3-bis-ethylcarbazole-3-phenylpropionic ester 4-[(4'-triptorelin-2-carbonyl)amino]benzoic acid,

4-(3,3-bis-ethylcarbazole-3-f the Nile-propoxycarbonyl)-2-hlorfenilovy ether 4'-triptorelin-2-carboxylic acid,

4-(3,3-bis-ethylcarbazole-3-phenyl-propoxycarbonyl)phenyl ether 4'-triptorelin-2-carboxylic acid,

4-(3,3-bis-ethylcarbazole-3-phenyl-propoxycarbonyl)-2,6-dichlorphenoxy ether 4'-triptorelin-2-carboxylic acid,

2-(2-{3-etoxycarbonyl-4-[(4'-triptorelin-2-carbonyl)amino]phenylacetonitrile)-2-phenylmalonate acid,

diethyl ether 2-(3-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}propionyloxy)-2-phenylmalonate acid,

ethylcarbamate-methyl ester 2-{4-[(4'-triptorelin-2-carbonyl)amino]phenyl}propionic acid,

benzyl ether of 5-(2,2-bis-ethylcarboxyl-2-phenyl-ethoxycarbonylmethyl)-2-4-[(4'-triptorelin-2-carbonyl)amino]benzoic acid,

5-(2,2-bis-ethylcarboxyl-2-phenyl-ethoxycarbonylmethyl)-2-[(4'-triptorelin-2-carbonyl)amino]benzoic acid,

ethyl ester of 5-(2,2-bis-ethylcarboxyl-2-phenyl-ethoxycarbonylmethyl)-2-[(4'-triptorelin-2-carbonyl)amino]benzoic acid,

methyl ester 5-(2,2-bis-ethylcarboxyl-2-phenyl-ethoxycarbonylmethyl)-2-[(4'-triptorelin-2-carbonyl)amino]benzoic acid,

diethyl ether 2-(2-{3-benzyloxycarbonyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl}-2-phenylmalonate acid,

diethyl ether 2-(2-{3-carboxy-4-[(4'-triptorelin-2-carbonyl) - Amin is]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-isopropoxycarbonyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-methoxycarbonyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-acetylamino-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-methoxycarbonylamino-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-(4-methylthiazole-2-yl)-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ester of 2-phenyl-2-(2-{6-[(4'-triptorelin-2-carbonyl)amino]biphenyl-3-yl}acetoxymethyl)malonic acid,

diethyl ether 2-(2-{3-formyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylaminomethyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}-3-acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-methoxy-methylcarbamoyl)-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}-3-acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-isobutyryl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}-3-acetoxymethyl)-2-phenylmalonate acid and

diethyl-the new ester 2-(2-{3-(1-hydroxy-2-methylpropyl)-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid;

(24) the Ester compound or its prodrug, or pharmaceutically acceptable salt of any of them in accordance with the above paragraph (1), which is chosen from the group including

2,2-bis(ethylcarbamate)-2-phenethyl ester {4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ester of 2-phenyl-2-{2-[4-[(4'-triptorelin-2-carbonyloxy)phenyl]acetoxymethyl}malonic acid,

diethyl ether 2-(2-{3-methyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{4-[methyl-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

2,2-bis-etilcaprilatului ether {3-ethyl-4-[(4'-triptorelin-2-carbonyl)amino]-2-phenyl}acetic acid,

diethyl ester of 2-phenyl-2-(2-{4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diisopropyl ether 2-phenyl-2-(2-{4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

2-phenyl-2,2-bis-(2,2,2-triptoreline)ethyl ester {4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

dimethyl 2-phenyl-2-(2-{4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diethyl ether 2-cyclopentyl-2-(2-{4-[(4'-triptorelin-2-carbonyl)is Mino]phenyl}acetoxymethyl)malonic acid,

dicyclohexylamine ester 2-phenyl-2-(2-{4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

2,2-bis-cyclohexylcarbonyl-2-phenethyl ester {4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2-phenyl-2,2-bis-phenylcarbamoyl-ethyl ester {4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-isopropylcarbamate-2-phenethyl ester {4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ether 2-benzyl-2-(2-{4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diethyl ether 2-(2-{2-methyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

4-[2-phenyl-2,2-bis-(2,2,2-triptoreline)ethoxycarbonylmethyl]phenyl ester of 4'-triptorelin-2-carboxylic acid,

4-[2-phenyl-2,2-bis-(2,2,2-triptoreline)ethoxycarbonylmethyl]phenyl ether-biphenyl-2-carboxylic acid,

diethyl ether of 2-cyclohexyl-2-(2-{4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

2-phenyl-2,2-bis-(2,2,2-triptoreline)ethyl ester {4-[(biphenyl-2-carbonyl)amino]phenyl}acetic acid,

diethyl ester of 2-phenyl-2-(2-{2-trifluoromethyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

2,2-bis-mate the carbarnoyl-2-phenethyl ester {4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ether 2-pyridin-2-yl-2-(2-{4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diethyl ether 2-pyridin-3-yl-2-(2-{4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

4-(2,2-bis-ethylcarbamate)-2-phenyl-ethoxycarbonylmethyl)phenyl ether 4'-triptorelin-2-carboxylic acid,

diethyl ester of 2-phenyl-2-(2-{3-trifluoromethyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

2,2-bis-butylcarbamoyl-2-phenethyl ester {4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ester (3-methyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ether 2-(2-{4-[(4'-methylbiphenyl-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{4-[(4'-methoxybiphenyl-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

3,3-bis-ethylcarbazole-3-phenylpropionic ester {4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

3-phenyl-3,3-bis-propellerblades-propyl ester {4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ester {4-[(biphenyl-2-carbonyl)amino]phenyl}acetic acid,

diethyl ester of 2-phenyl-2-(2-{4-[(3'-triptorelin-2-CT is of IMT)amino]phenyl}acetoxymethyl)malonic acid,

4-(2,2-bis-ethylcarbamate)-2-phenyl-ethoxycarbonylmethyl)-2-hlorfenilovy ether 4'-triptorelin-2-carboxylic acid,

diethyl ether 2-(2-{4-[isopropyl-(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{4-[cyclohexyl-(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

dipropionyl ester 2-phenyl-2-(2-{4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diisobutylamine ester 2-phenyl-2-(2-{4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

2,2-bis-isobutylamino-2-phenethyl ester {4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-(3-methyl-butylcarbamoyl)-2-phenethyl ester {4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ether 2-(2-{4-[ethyl-(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

2,2-bis-ethylcarboxyl-2-phenethyl ester {4-[(4'-chlorobiphenyl-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ester {4-[(3',4'-dichlorobiphenyl-2-carbonyl)amino]phenyl}acetic acid,

2-phenyl-2,2-bis-propellerblades-ethyl ester {3-methyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-(2-methoxy-ethyl is carbamoyl)-2-phenethyl ester {4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ether 2-(2-{3-ethyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-isopropyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ether 2-(2-{3-isopropyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

3,3-bis-ethylcarbazole-3-phenylpropionyl ether {3-ethyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-isobutyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ether 2-(2-{3-isobutyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-chloro-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-bromo-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

2-phenyl-2,2-bis-propellerblades-ethyl ester {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-methylcarbamoyl-4-[(4'-triptime biphenyl-2-carbonyl)amino]phenyl}acetic acid,

3,3-bis-ethylcarbazole-3-phenylpropionyl ether {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ether 2-(2-{3-diethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-benzylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

4,4-bis-ethylcarbamate-4-privately ether {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-diethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-diisopropylamino-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ether 2-(2-{3-diethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-diisopropylamino-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-(isopropylaminocarbonyl)-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ether 2-(2-{3-(ethylmethylamino)-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-FeNi is malonic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-(ethylmethylamino)-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

3,3-bis-ethylcarbazole-3-phenylpropionyl ether (3-(ethylmethylamino)-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-(piperidine-1-carbonyl)-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-(pyrrolidin-1-carbonyl)-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-(methylpropanoyl)-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

3,3-bis-ethylcarbazole-3-phenylpropionyl ether (3-(methylpropanoyl)-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2-ethylcarboxyl-2-phenethyl ether {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ester of 2-phenyl-2-(2-{3-pyrrolidin-1-carbonyl)-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl]malonic acid,

diethyl ester of 2-phenyl-2-(2-{3-piperidine-1-carbonyl)-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

2-phenyl-2-propionamido-ethyl ester {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)is Mino]phenyl}acetic acid,

2-(2,5-dioxo-pyrrolidin-1-yl)-2-phenethyl ether {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl)acetic acid,

ethylcarbitol-benzyl ether {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2-ethylcarboxylate-benzyl ether {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2 isopropylamino-2-phenethyl ester hydrochloride {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ether 2-[2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxy)ethyl]-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-fluoro-biphenyl-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{4-[(4'-bromo-biphenyl-2-carbonyl)amino]-3-dimethylcarbamoyl}acetoxymethyl)-2-phenylmalonate acid,

2-acetylamino-2-phenethyl ether {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2 Butylimino-2-phenethyl ether {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

dimethyl 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-qi is lipantil-2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diethyl ether of 2-cyclohexyl-2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diethyl ether 2-(2-{4-[(4'-chlorobiphenyl-2-carbonyl)amino]-3-dimethylcarbamoyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{4-[(4'-acetyl-biphenyl-2-carbonyl)amino]-3-dimethylcarbamoyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{4-[(4'-cyano-biphenyl-2-carbonyl)amino]-3-dimethylcarbamoyl)acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4-methyl-4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(5-methyl-4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

2 methanesulfonamido-2-phenethyl ether {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

ethyl ester of 3-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxy)-2-phenylpropionic acid,

2-(methylpropionamide)-2-phenethyl ether {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ether 2-[3-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxy)propyl]-2-phenylmalonate sour is you,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(5-methoxy-4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{4-[(5-chloro-4'-triptorelin-2-carbonyl)amino]-3-dimethylcarbamoyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(6-methyl-4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

di-2,2,2-triptoreline ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(2'-fluoro-4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{5-dimethylcarbamoyl-2-fluoro-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-bromo-5-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-chloro-5-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(3'-fluoro-4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{4-[(3'-chloro-4'-triptorelin-2-Carbo who yl)amino]-3-dimethylcarbamoyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-(5-nitro-pyridin-2-yl)malonic acid,

diethyl ether 2-(5-amino-pyridin-2-yl)-2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-pyridin-2-elmaloglou acid,

diethyl ether 2-(2-{3-chloro-5-dimethylcarbamoyl-2-fluoro-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-bromo-5-dimethylcarbamoyl-2-fluoro-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-o-tolyl-malonic acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-m-tolyl-malonic acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-p-tolyl-malonic acid,

diethyl ether 2-(2-chlorophenyl)-2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diethyl ether 2-(3-chlorophenyl)-2-(2-{3-dimethylcarbamoyl-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diethyl ether 2-(4-chlorophenyl)-2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylethanol acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-(2-methoxyphenyl)malonic acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-(3-methoxyphenyl)malonic acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-(4-methoxyphenyl)malonic acid,

diethyl ether 2-(2-{4-[(5,4'-bis-triptorelin-2-carbonyl)amino]-3-dimethylcarbamoyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{4-[(6-chloro-4'-triptorelin-2-carbonyl)amino]-3-dimethylcarbamoyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(6-fluoro-4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-[2-(2-{3-dimethylcarbamoyl-4-[(5-methyl-4'-triptorelin-2-carbonyl)amino]phenyl}acetoxy)ethyl]-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(5-ethoxy-4'-cryptomite is biphenyl-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(5-isopropoxy-4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-[2-(2-{4-(5,4'-bis-triptorelin-2-carbonyl)amino]-3-dimethylcarbamoyl}acetoxy)ethyl]-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-(6-methoxy-4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(3-methyl-4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-{2-[4-(2,4-bis-trifluoromethyl-benzoylamine)-3-dimethylcarbamoyl]acetoxymethyl}-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-methylbiphenyl-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-{2-[3-dimethylcarbamoyl-4-[(2-ethyl-4-trifluoromethyl-benzoylamine)phenyl]acetoxymethyl}-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-ethyl-biphenyl-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-isopropyl-biphenyl-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-isopropyl-biphenyl-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate is islote,

diethyl ether 2-{2-[3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyloxy)phenyl]acetoxymethyl}-2-phenylmalonate acid,

2-ethyl-2-privately ether {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

1-phenyl-cyclopropylmethyl ether {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-definiately ether {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

1-phenyl-cyclopentylmethyl ether {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

3-hydroxy-2-hydroxymethyl-2-phenylpropionyl ether {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

3-acetoxymethyl-2-phenylpropionyl ether {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl]-2-thiophene-2-elmaloglou acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl]-2-thiophene-3-elmaloglou acid,

diethyl ether 2-(2-{4-dimethylcarbamoyl-5-[(4'-triptorelin-2-carbonyl)amino]pyridin-2-yl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-metilcarbamat-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl]-2-(3-methyl-thiophene-2-yl)malonic acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-(5-methyl-thiophene-2-yl)malonic acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-thiazol-2-elmaloglou acid,

diethyl ether 2-(2-{3-ethoxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-hydroxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-methoxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ether 2-(2-{3-methoxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

2-phenyl-2,2-bis-propellerblades-ethyl ester {3-methoxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

3,3-bis-ethylcarbazole-3-phenylpropionyl ether {3-methoxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-ethoxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

3,3-bis-ethylcarbazole-3-phenylpropionyl ether {3-ethoxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ether 2-(2-{3-isopropoxy-4-[(4'-trifluoromethyl shall iphenyl-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-isopropoxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

3,3-bis-ethylcarbazole-3-phenylpropionyl ether {3-isopropoxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-propoxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-benzyloxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ether 2-(2-{3-benzyloxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-hydroxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-{2-[3-methoxy-4-(4'-triptorelin-2-carbonyloxy)phenyl]acetoxymethyl}-2-phenylmalonate acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-dimethylamino-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-piperidine-1-yl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-pyrrolidin-1-yl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ester of 2-phenyl-2-(2-{3-piperidine-1-yl-4-[(4'-cryptomite is biphenyl-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diethyl ester of 2-phenyl-2-(2-{3-pyrrolidin-1-yl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diethyl ether 2-(2-{3-dimethylamino-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-morpholine-4-yl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-diethylamino-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-[2-(2-{2-methyl-3-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxy)ethyl]-2-phenylmalonate acid,

diethyl ester of 2-phenyl-2-(2-{3-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diethyl ester of 2-phenyl-2-[2-(2-{3-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxy)ethyl]malonic acid,

3,3-bis-ethylcarbazole-3-phenylpropionyl ether {3-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

3-phenyl-3,3-bis-propellerblades-propyl ether {3-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ether 2-[2-(2-{4-methyl-3-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxy)ethyl]-2-phenylmalonate acid,

diethyl ether 2-[2-(2-{2-methyl-5-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxy)ethyl]-2-phenylal the new acid,

3,3-bis-isopropylcarbamate-3-phenylpropionyl ether {3-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

3,3-bis-ethylcarbazole-3-phenylpropionyl ether {2-methyl-3-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

4,4-bis-ethylcarbamate-4-privately ether {2-methyl-3-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

3-phenyl-3,3-bis-propellerblades-propyl ether {2-methyl-3-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

3,3-bis-ethylcarbazole-3-phenylpropionyl ether {2-methoxy-3-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ether 2-[2-(2-{2-methoxy-3-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxy)ethyl]-2-phenylmalonate acid,

3,3-bis-ethylcarbazole-3-phenylpropionyl ether {2-ethoxy-3-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ether 2-[2-(2-{2-ethoxy-3-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxy)ethyl]-2-phenylmalonate acid,

diethyl ether 2-[2-(2-{2-isopropoxy-3-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxy)ethyl]-2-phenylmalonate acid,

diethyl ether 2-[2-(2-{2-methoxycarbonyl-3-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxy)ethyl]-2-phenylmalonate acid,

diethyl ether 2-[2-(2-{2-ethoxy-5-methyl-3-[(4'-triptorelin-2-carbonyl)and the eno]phenyl}acetoxy)ethyl]-2-phenylmalonate acid,

2-[(biphenyl-2-carbonyl)amino]ethyl ester 4-[(4'-triptorelin-2-carbonyl)amino]benzoic acid,

2-(2-biphenyl-2-yl-acetylamino)ethyl ester 4-[(4'-triptorelin-2-carbonyl)amino]benzoic acid,

3-naphthalene-1-yl-3-(2,2,2-triptoreline)propyl ether of 4-[(4'-triptorelin-2-carbonyl)amino]benzoic acid,

3-[2-(2,2,2-triptoreline)naphthalene-1-yl]propyl ester 4-[(4'-triptorelin-2-carbonyl)amino]benzoic acid,

3,3-diphenyl-3-(2,2,2-triptoreline)propyl ether of 4-[(4'-triptorelin-2-carbonyl)amino]benzoic acid,

3-biphenyl-2-yl-3-(2,2,2-triptoreline)propyl ether of 4-[(4'-triptorelin-2-carbonyl)amino]benzoic acid,

3-phenyl-3-(2,2,2-triptoreline)propyl ether of 4-[(4'-triptorelin-2-carbonyl)amino]benzoic acid,

2-[8-(2,2,2-triptoreline)naphthalene-1-yl]ethyl ester 4-[(4'-triptorelin-2-carbonyl)amino]benzoic acid,

3-(2,6-dichlorophenyl)-3-(2,2,2-triptoreline)propyl ether of 4-[(4'-triptorelin-2-carbonyl)amino]benzoic acid,

3-(2-chlorophenyl)-3-(2,2,2-triptoreline)propyl ether of 4-[(4'-triptorelin-2-carbonyl)amino]benzoic acid,

diethyl ester of 2-phenyl-2-(2-{4-[(4'-triptorelin-2-carbonyl)amino]benzoyloxy}ethyl) - malonic acid,

diethyl EF the p 2-(2-{3-methyl-4-[(4'-triptorelin-2-carbonyl)amino]benzoyloxy}ethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{2-chloro-4-[(4'-triptorelin-2-carbonyl)amino]-benzoyloxy}ethyl)-2-phenylmalonate acid,

diethyl ester of 2-phenyl-2-{2-[4-(4'-triptorelin-2-carbonyloxy)benzoyloxy]ethyl}malonic acid,

3,3-bis-ethylcarbazole-3-phenylpropionic ester 4-[(4'-triptorelin-2-carbonyl)amino]benzoic acid,

4-(3,3-bis-ethylcarbazole-3-phenyl-propoxycarbonyl)-2-hlorfenilovy ether 4'-triptorelin-2-carboxylic acid,

4-(3,3-bis-ethylcarbazole-3-phenylpropionyl)phenyl ether 4'-triptorelin-2-carboxylic acid,

4-(3,3-bis-ethylcarbazole-3-phenyl-propoxycarbonyl)-2,6-dichlorphenoxy ether 4'-triptorelin-2-carboxylic acid,

diethyl ether 2-(2-{3-etoxycarbonyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(3-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}propionyloxy)-2-phenylmalonate acid,

ethylcarbodiimide ester 3-{4-[(4'-triptorelin-2-carbonyl)amino]phenyl}propionic acid,

benzyl ether of 5-(2,2-bis-ethylcarboxyl-2-phenyl-ethoxycarbonylmethyl)-2-4-[(4'-triptorelin-2-carbonyl)amino]benzoic acid,

5-(2,2-bis-ethylcarboxyl-2-phenyl-ethoxycarbonylmethyl)-2-4-[(4'-triptorelin-2-carbonyl)amino]benzoic acid,

methyl ester 5-(2,2-bis-ethylcarboxyl-2-phenyl-ethoxycarbonylmethyl)-2-[(4'-triptorelin-2-carbonyl)amino]benzoic acid,

diethyl ether 2-(2-{3-benzyloxycarbonyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-carboxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-isopropoxycarbonyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-methoxycarbonyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-acetylamino-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-methoxycarbonylamino-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-(4-methyl-thiazol-2-yl)-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ester of 2-phenyl-(2-{6-[(4'-triptorelin-2-carbonyl)amino]-biphenyl-3-yl}acetoxymethyl)malonic acid,

diethyl ether 2-(2-{3-formyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-emailmyname-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-(methoxy-methylcarbamoyl)-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-isobutyryl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid and

diethyl ether 2-(2-{3-(1-hydroxy-2-methylpropyl)-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acids;

(25) the Ester compound or its prodrug, or pharmaceutically acceptable salt of any of them in accordance with the above paragraph (1), which is chosen from the group including

2,2-bis-ethylcarboxyl-2-phenethyl ester {4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-ethyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2-phenyl-2,2-bis-(2,2,2-triptoreline)ethyl ester {4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-cyclohexylcarbonyl-2-phenethyl ester {4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2-phenyl-2,2-bis-phenylcarbamoyl-ethyl ester {4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-isopropylcarbamate-2-phenethyl ester {4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

4-[2-phenyl-2,2-is IP-(2,2,2-triptoreline)ethoxycarbonylmethyl]phenyl ester of 4'-triptorelin-2-carboxylic acid,

4-[2-phenyl-2,2-bis-(2,2,2-triptoreline)ethoxycarbonylmethyl]phenyl ether-biphenyl-2-carboxylic acid,

2-phenyl-2,2-bis-(2,2,2-triptoreline)ethyl ester {4-[(biphenyl-2-carbonyl)amino]phenyl}acetic acid,

diethyl ester of 2-phenyl-2-(2-{2-trifluoromethyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

2,2-bis-methylcarbamoyl-2-phenethyl ester {4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

4-(2,2-bis-ethylcarboxyl-2-phenyl-ethoxycarbonylmethyl)phenyl ether 4'-triptorelin-2-carboxylic acid,

2,2-bis-butylcarbamoyl-2-phenethyl ester {4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-methyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

3,3-bis-ethylcarbazole-3-phenylpropionic ester {4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

3-phenyl-3,3-bis-propellerblades-propyl ester {4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ester {4-[(biphenyl-2-carbonyl)amino]phenyl}acetic acid,

4-(2,2-bis-ethylcarboxyl-2-generatestarparameter)-2-hlorfenilovy ether 4'-triptorelin-2-carboxylic acid,

2,2-bis-isobutylamino-2-phenethyl ester {4-[(4'-t is iformative-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-(3-methyl-butylcarbamoyl)-2-phenethyl ester {4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ester {4-[(4'-chlorobiphenyl-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarbamate)-2-phenethyl ester {4-[(3',4'-dichlorobiphenyl-2-carbonyl)amino]phenyl}acetic acid,

2-phenyl-2,2-bis-propellerblades)ethyl ester {3-methyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-(2-methoxy-ethylcarbamate)-2-phenethyl ester {4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-etilcaprilatului ether {3-isopropyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

3,3-bis-ethylcarbazole-3-phenylpropionyl ether {3-ethyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-isobutyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2-phenyl-2,2-bis-propellerblades-ethyl ester {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-methylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

3,3-bis-ethylcarbazole-3-phenylpropionyl ether {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]enyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-benzylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

4,4-bis-ethylcarbamate-4-privately ether {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-diethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-diisopropylamino-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-(isopropylaminocarbonyl)-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-(ethylmethylamino)-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

3,3-bis-ethylcarbazole-3-phenylpropionyl ether {3-(ethylmethylamino)-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-(piperidine-1-carbonyl)-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-(pyrrolidin-1-carbonyl)-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-(methylpropanoyl)-4-[(4'-triptorelin-2-Carbo who yl)amino]phenyl}acetic acid,

3,3-bis-ethylcarbazole-3-phenylpropionyl ether {3-(methylpropanoyl)-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-hydroxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-methoxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2-phenyl-2,2-bis-propellerblades-ethyl ester {3-methoxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

3,3-bis-ethylcarbazole-3-phenylpropionyl ether {3-methoxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-ethoxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

3,3-bis-ethylcarbazole-3-phenylpropionyl ether {3-ethoxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-isopropoxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

3,3-bis-ethylcarbazole-3-phenylpropionyl ether {3-isopropoxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-propoxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-benzyloxy-4-[(4'-t is iformative-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-dimethylamino-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-piperidine-1-yl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-pyrrolidin-1-yl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

3,3-bis-ethylcarbazole-3-phenylpropionyl ether (3-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

3-phenyl-3,3-bis-propellerblades-propyl ether {3-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

3,3-bis-isopropylcarbamate-3-phenylpropionyl ether {3-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

3,3-bis-ethylcarbazole-3-phenylpropionyl ether {2-methyl-3-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

4,4-bis-ethylcarbamate-4-privately ether {2-methyl-3-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

3-phenyl-3,3-bis-propellerblades-propyl ether {2-methyl-3-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

3,3-bis-ethylcarbazole-3-phenylpropionyl ether {2-methoxy-3-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

3,3-bis-ethylcarbazole-3-phenylpropionyl ether {2-ethoxy-3-[(4'-triptorelin-2-Carboni is)amino]phenyl}acetic acid,

3,3-bis-ethylcarbazole-3-phenylpropionic ester 4-[(4'-triptorelin-2-carbonyl)amino]benzoic acid,

4-(3,3-bis-ethylcarbazole-3-phenylpropionyl)-2-hlorfenilovy ether 4'-triptorelin-2-carboxylic acid,

4-(3,3-bis-ethylcarbazole-3-phenylpropionyl)phenyl ether 4'-triptorelin-2-carboxylic acid,

4-(3,3-bis-ethylcarbazole-3-phenylpropionyl)-2,6-dichlorphenoxy ether 4'-triptorelin-2-carboxylic acid,

benzyl ether of 5-(2,2-bis-ethylcarboxyl-2-phenyl-ethoxycarbonylmethyl)-2-[(4'-triptorelin-2-carbonyl)amino]benzoic acid,

5-(2,2-bis-ethylcarboxyl-2-phenyl-ethoxycarbonylmethyl)-2-[(4'-triptorelin-2-carbonyl)amino]benzoic acid,

5-(2,2-bis-ethylcarboxyl-2-phenyl-ethoxycarbonylmethyl)-2-[(4'-triptorelin-2-carbonyl)amino]benzoic acid ethyl ester and

methyl ester 5-(2,2-bis-ethylcarboxyl-2-phenyl-ethoxycarbonylmethyl)-2-[(4'-triptorelin-2-carbonyl)amino]benzoic acid;

(26) the Ester compound or its prodrug, or pharmaceutically acceptable salt of any of them in accordance with the above paragraph (1), which is chosen from the group including

diethyl ester of 2-phenyl-2-{2-[4-(4'-triptorelin-2-carbonyloxy)phenyl]acetoxymethyl}malonic acid,

diethyl ether 2-(2-{3-methyl-4-[(4'-triform tilbehor-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{4-[methyl-(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ester of 2-phenyl-2-(2-{4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diisopropyl ether 2-phenyl-2-(2-{4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

dimethyl 2-phenyl-2-(2-{4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diethyl ether 2-cyclopentyl-2-(2-{4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

dicyclohexylamine ester 2-phenyl-2-(2-{4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diethyl ether 2-benzyl-2-(2-{4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diethyl ether 2-(2-{2-methyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether of 2-cyclohexyl-2-(2-{4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diethyl ester of 2-phenyl-2-(2-{2-trifluoromethyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diethyl ether 2-pyridin-2-yl-2-(2-{4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

dietro the initial ester 2-pyridin-3-yl-2-(2-{4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diethyl ester of 2-phenyl-2-(2-{3-trifluoromethyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diethyl ether 2-(2-{4-[(4'-methylbiphenyl-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{4-[(4'-methoxybiphenyl-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ester of 2-phenyl-2-(2-{4-[(3'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diethyl ether 2-(2-{4-[isopropyl-(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{4-[cyclohexyl-(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

dipropionyl ester 2-phenyl-2-(2-{4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diisobutylamine ester 2-phenyl-2-(2-{4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diethyl ether 2-(2-{4-[ethyl-(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-ethyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-isopropyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2(2-{3-isobutyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-chloro-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-bromo-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-diethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-diisopropylamino-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-(ethylmethylamino)-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-(pyrrolidin-1-carbonyl)-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ester of 2-phenyl-2-(2-{3-(pyrrolidin-1-carbonyl)-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diethyl ester of 2-phenyl-2-(2-{3-(piperidine-1-carbonyl)-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diethyl ether 2-[2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxy)ethyl]-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{4-[(4'-bromo-biphenyl-2-carbonyl)amino]-3-dimethylcarbamoyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-cyclopentyl-2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diethyl ether of 2-cyclohexyl-2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diethyl ether 2-(2-{4-[(4'-chlorobiphenyl-2-carbonyl)amino]-3-dimethylcarbamoyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{4-[(4'-acetyl-biphenyl-2-carbonyl)amino]-3-dimethylcarbamoyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{4-[(4'-cyano-biphenyl-2-carbonyl)amino]-3-dimethylcarbamoyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4-methyl-4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(5-methyl-4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-[3-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxy)propyl]-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(5-methoxy-4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{4-[(5-chloro-4'-triptorelin-2-carbonyl)amino]-3-dimethylcarbamoyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(6-methyl-4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

di-2,2,2-triptoreline ether 2-(2-{3-dimethylcarbamoyl-4-[4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(2'-fluoro-4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{5-dimethylcarbamoyl-2-fluoro-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-bromo-5-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-chloro-5-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(3'-fluoro-4'-trifloromethyl enyl-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{4-[(3'-chloro-4'-triptorelin-2-carbonyl)amino]-3-dimethylcarbamoyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-(5-nitro-pyridin-2-yl)malonic acid,

diethyl ether 2-(5-amino-pyridin-2-yl)-2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl]malonic acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-pyridin-2-elmaloglou acid,

diethyl ether 2-(2-{3-chloro-5-dimethylcarbamoyl-2-fluoro-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-bromo-5-dimethylcarbamoyl-2-fluoro-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-o-tolyl-malonic acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-m-tolyl-malonic acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-p-tolyl-malonic acid,

diethyl ether 2-(3-chlorophenyl)-2-(2-{3-dimethylcarbamoyl--[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diethyl ether 2-(3-chlorophenyl)-2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diethyl ether 2-(4-chlorophenyl)-2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylethanol acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-(2-methoxyphenyl)malonic acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-(3-methoxyphenyl)malonic acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-(4-methoxyphenyl)malonic acid,

diethyl ether 2-(2-{4-[(5,4'-bis-triptorelin-2-carbonyl)amino]-3-dimethylcarbamoyl)acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{4-[(6-chloro-4'-triptorelin-2-carbonyl)amino]-3-dimethylcarbamoyl}acetoxymethyl)-2-phenyl)malonic acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(6-fluoro-4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenyl)malonic acid,

diethyl ether 2-[2-(2-{3-dimethylcarbamoyl-4-[(5-methyl-4'-cryptomite is biphenyl-2-carbonyl)amino]phenyl}acetoxy)ethyl]-2-phenyl)malonic acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(5-ethoxy-4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenyl)malonic acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(5-isopropoxy-4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenyl)malonic acid,

diethyl ether 2-[2-(2-{4-[(5,4'-bis-triptorelin-2-carbonyl)amino]-3-dimethylcarbamoyl}acetoxy)ethyl]-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(6-methoxy-4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(3-methyl-4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-{2-[4-(2,4-bis-trifluoromethyl-benzoylamine)-3-dimethylcarbamoyl]acetoxymethyl}-2-phenyl)malonic acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-methylbiphenyl-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-{2-[3-dimethylcarbamoyl-4-[(2-ethyl-4-trifluoromethyl-benzoylamine)phenyl]acetoxymethyl}-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-ethylbiphenyl-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-isopropylphenyl-2-carbonyl)amino]phenyl}acetoxymethyl)-2-dryer is Lanovoy acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-isopropyl-biphenyl-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-{2-[3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyloxy)phenyl]acetoxymethyl}-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-thiophene-2-elmaloglou acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-thiophene-3-elmaloglou acid,

diethyl ether 2-(2-{4-dimethylcarbamoyl-5-[(4'-triptorelin-2-carbonyl)amino]pyridin-2-yl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-(3-methylthiophene-2-yl)malonic acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-(5-methyl-thiophene-2-yl)malonic acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-thiazol-2-elmaloglou acid,

diethyl ether 2-(2-{3-ethoxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-methoxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-phenylmalonic acid,

diethyl ether 2-(2-{3-isopropoxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-benzyloxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-hydroxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-{2-[3-methoxy-4-[(4'-triptorelin-2-carbonyloxy)phenyl]acetoxymethyl}-2-phenylmalonate acid,

diethyl ester of 2-phenyl-2-(2-{3-piperidine-1-yl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diethyl ester of 2-phenyl-2-(2-{3-pyrrolidin-1-yl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diethyl ether 2-(2-{3-dimethylamino-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-morpholine-4-yl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-diethylamino-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-[2-(2-{2-methyl-3-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxy)ethyl]-2-phenylmalonate acid,

diethyl ester of 2-phenyl-2-(2-{3-[(4'-triptorelin-2-CT is of IMT)amino]phenyl}acetoxymethyl)malonic acid,

diethyl ester of 2-phenyl-2-[2-(2-{3-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxy)ethyl]malonic acid,

diethyl ether 2-[2-(2-{4-methyl-3-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxy)ethyl]-2-phenylmalonate acid,

diethyl ether 2-[2-(2-{2-methyl-5-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxy)ethyl]-2-phenylmalonate acid,

diethyl ether 2-[2-(2-{2-methoxy-3-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxy)ethyl]-2-phenylmalonate acid,

diethyl ether 2-[2-(2-{2-ethoxy-3-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxy)ethyl]-2-phenylmalonate acid,

diethyl ether 2-[2-(2-{2-isopropoxy-3-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxy)ethyl]-2-phenylmalonate acid,

diethyl ether 2-[2-(2-{2-methoxycarbonyl-3-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxy)ethyl]-2-phenylmalonate acid,

diethyl ether 2-[2-(2-{2-ethoxy-5-methyl-3-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxy)ethyl]-2-phenylmalonate acid,

diethyl ester of 2-phenyl-2-(2-{4-[(4'-triptorelin-2-carbonyl)amino]benzoyloxy}ethyl]malonic acid,

diethyl ether 2-(2-{3-methyl-4-[(4'-triptorelin-2-carbonyl)amino]benzoyloxy}ethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{2-chloro-4-[(4'-triptorelin-2-carbonyl)amino]benzoyloxy}ethyl)-2-phenylal the new acid,

diethyl ester of 2-phenyl-2-{2-[4-(4'-triptorelin-2-carbonyloxy)benzoyloxy]ethyl}malonic acid,

diethyl ether 2-(2-{3-etoxycarbonyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(3-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}propionyloxy)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-benzyloxycarbonyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-carboxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-isopropoxycarbonyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-methoxycarbonyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-acetylamino-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-methoxycarbonylamino-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-(4-methyl-thiazol-2-yl)-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-enyl-2-(2-{6-[(4'-triptorelin-2-carbonyl)amino]biphenyl-3-yl}acetoxymethyl)malonic acid,

diethyl ether 2-(2-{3-formyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylaminomethyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-(methoxy-methylcarbamoyl)-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-isobutyryl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid and

diethyl ether 2-(2-{3-(1-hydroxy-2-methylpropyl)-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acids;

(27) the Ester compound or its prodrug, or pharmaceutically acceptable salt of any of them in accordance with the above paragraph (1), which is chosen from the group including

2,2-bis-ethylcarboxyl-2-phenethyl ester {4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-ethyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2-phenyl-2,2-bis-(2,2,2-triptoreline)ethyl ester {4-[(4'-triptorelin-2-carbonyl)amino]phenyl)acetic acid,

2,2-bis-cyclohexylcarbonyl-2-phenethyl ester {4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid to the slots,

2-phenyl-2,2-bis-phenylcarbamoyl-ethyl ester {4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-isopropylcarbamate-2-phenethyl ester {4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2-phenyl-2,2-bis(2,2,2-triptoreline)ethyl ester {4-[(biphenyl-2-carbonyl)amino]phenyl}acetic acid,

diethyl ester of 2-phenyl-2-(2-{2-trifluoromethyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

2,2-bis-methylcarbamoyl-2-phenethyl ester {4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-butylcarbamoyl-2-phenethyl ester {4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethyl-carbarnoyl-2-phenethyl ether {3-methyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

3,3-bis-ethylcarbazole-3-phenylpropionic ester {4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

3-phenyl-3,3-bis-propellerblades-propyl ester {4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ester {4-[(biphenyl-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-isobutylamino-2-phenethyl ester {4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis(3-methyl-butylcarbamoyl)-2-phenethyl ether {-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ester {4-[(4'-chlorobiphenyl-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ester {4-[(3',4'-dichlorobiphenyl-2-carbonyl)amino]phenyl}acetic acid,

2-phenyl-2,2-bis-profilerenumeration ether {3-methyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis(2-methoxy-ethylcarbamate)-2-phenethyl ester {4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-isopropyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

3,3-bis-ethylcarbazole-3-phenylpropionyl ether {3-ethyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-isobutyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2-phenyl-2,2-bis-propellerblades-ethyl ester {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-methylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

3,3-bis-ethylcarbazole-3-phenylpropionyl ether {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-benzylcarbamoyl-4-[(4'-triptorelin-2-carbon is l)amino]phenyl}acetic acid,

4,4-bis-ethylcarbamate-4-privately ether {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-diethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-diisopropylamino-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-(isopropylaminocarbonyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

3,3-bis-ethylcarbazole-3-phenylpropionyl ether {3-(ethylmethylamino-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-(piperidine-1-carbonyl)-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-(pyrrolidin-1-carbonyl)-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-(methylpropanoyl)-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

3,3-bis-ethylcarbazole-3-phenylpropionyl ether {3-(methylpropanoyl)-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-hydroxy-4-[(4'-triptorelin-2-carbonyl)and the eno]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-methoxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2-phenyl-2,2-bis-propellerblades-ethyl ester {3-methoxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl)acetic acid,

3,3-bis-ethylcarbazole-3-phenylpropionyl ether {3-methoxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-ethoxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

3,3-bis-ethylcarbazole-3-phenylpropionyl ether {3-ethoxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-isopropoxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

3,3-bis-ethylcarbazole-3-phenylpropionyl ether {3-isopropoxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-propoxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-benzyloxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-dimethylamino-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-piperidine-1-yl-4-[(4'-triform tilbehor-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-pyrrolidin-1-yl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl)acetic acid,

3,3-bis-ethylcarbazole-3-phenylpropionic ester 4-[(4'-triptorelin-2-carbonyl)amino]benzoic acid,

benzyl ether of 5-(2,2-bis-ethylcarboxyl-2-phenyl-ethoxycarbonylmethyl)-2-[(4'-triptorelin-2-carbonyl)amino]benzoic acid,

5-(2,2-bis-ethylcarboxyl-2-phenyl-ethoxycarbonylmethyl)-2-[(4'-triptorelin-2-carbonyl)amino]benzoic acid,

ethyl ester of 5-(2,2-bis-ethylcarboxyl-2-phenyl-ethoxycarbonylmethyl)-2-[(4'-triptorelin-2-carbonyl)amino]benzoic acid and

methyl ester 5-(2,2-bis-ethylcarboxyl-2-phenyl-ethoxycarbonylmethyl)-2-[(4'-triptorelin-2-carbonyl)amino]benzoic acid;

(28) the Ester compound or its prodrug, or pharmaceutically acceptable salt of any of them in accordance with the above paragraph (1), which is chosen from the group including

diethyl ether 2-(2-{3-methyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{4-[methyl-(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ester of 2-phenyl-2-(2-{4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diisopropyl EF the R 2-phenyl-2-(2-{4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

dimethyl 2-phenyl-2-(2-{4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diethyl ether 2-cyclopentyl-2-(2-{4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

dicyclohexylamine ester 2-phenyl-2-(2-{4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diethyl ether 2-benzyl-2-(2-{4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diethyl ether 2-(2-{2-methyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether of 2-cyclohexyl-2-(2-{4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diethyl ester of 2-phenyl-2-(2-{2-trifluoromethyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diethyl ether 2-pyridin-2-yl-2-(2-{4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diethyl ether 2-pyridin-3-yl-2-(2-{4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diethyl ester of 2-phenyl-2-(2-{3-trifluoromethyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diethyl ether 2-(2-{4-[(4'-methylbiphenyl-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl-the new ester 2-(2-{4-[(4'-methoxybiphenyl-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ester of 2-phenyl-2-(2-{4-[(3'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diethyl ether 2-(2-{4-[isopropyl-(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{4-[cyclohexyl-(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

dipropionyl ester 2-phenyl-2-(2-{4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diisobutylamine ester 2-phenyl-2-(2-{4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diethyl ether 2-(2-{4-[ethyl-(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-ethyl-4-(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-isopropyl-4-(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-isobutyl-4-(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-chloro-4-(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-bromo-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

<> diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-diethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-diisopropylamino-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-(ethylmethylamino)-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-(ethylmethylamino)-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-(pyrrolidin-1-carbonyl)-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ester of 2-phenyl-2-(2-{3-(pyrrolidin-1-carbonyl)-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diethyl ester of 2-phenyl-2-(2-{3-(piperidine-1-carbonyl)-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diethyl ether 2-[2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxy)ethyl]-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-fluoro-biphenyl-2-carbonyl)amino]phenyl}acetoxymethyl)-2-Fenella is about acid,

diethyl ether 2-(2-{4-[(4'-bromo-biphenyl-2-carbonyl)amino]}-3-dimethylcarbamoyl}acetoxymethyl)-2-phenylmalonate acid,

dimethyl 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-cyclopentyl-2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diethyl ether of 2-cyclohexyl-2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diethyl ether 2-(2-{4-[(4'-chlorobiphenyl-2-carbonyl)amino]-3-dimethylcarbamoyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{4-[(4'-acetyl-biphenyl-2-carbonyl)amino]-3-dimethylcarbamoyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{4-[(4'-cyano-biphenyl-2-carbonyl)amino]-3-dimethylcarbamoyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4-methyl-4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(5-methyl-4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-[3-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxy)propyl]-2-phenylmalonate key is lots

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(5-methoxy-4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{4-[(5-chloro-4'-triptorelin-2-carbonyl)amino]-3-dimethylcarbamoyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(6-methyl-4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

2,2,2-triptoreline ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(2'-fluoro-4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{5-dimethylcarbamoyl-2-fluoro-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-bromo-5-dimethylcarbamoyl-4-[(2'-fluoro-4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-chloro-5-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl)acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(3'-fluoro-4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{4-[(3'-chloro-4'-triptorelin-2-ka is bonyl)amino]-3-dimethylcarbamoyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-(5-nitropyridine-2-yl)malonic acid,

diethyl ether 2-(5-aminopyridine-2-yl)-2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-pyridin-2-elmaloglou acid,

diethyl ether 2-(2-{3-chloro-5-dimethylcarbamoyl-2-fluoro-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-bromo-5-dimethylcarbamoyl-2-fluoro-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-o-tolyl-malonic acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-m-tolyl-malonic acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-p-tolyl-malonic acid,

diethyl ether 2-(2-chlorophenyl)-2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diethyl ether 2-(3-chlorophenyl)-2-(2-{3-dimethylcarbamoyl-4-(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diethyl ether 2-(4-chlorophenyl)-2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylethanol acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-(2-methoxyphenyl)malonic acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-(3-methoxyphenyl)malonic acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-(4-methoxyphenyl)malonic acid,

diethyl ether 2-(2-{4-[(5,4'-bis-triptorelin-2-carbonyl)amino]-3-dimethylcarbamoyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{4-[(6-chloro-4'-triptorelin-2-carbonyl)amino]-3-dimethylcarbamoyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(6-fluoro-4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-[2-(2-{3-dimethylcarbamoyl-4-[(5-methyl-4'-triptorelin-2-carbonyl)amino]phenyl}acetoxy)ethyl]-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(5-ethoxy-4'-cryptomite is biphenyl-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(5-isopropoxy-4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-[2-(2-{4-(5,4'-bis-triptorelin-2-carbonyl)amino]-3-dimethylcarbamoyl}acetoxy)ethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-(6-methoxy-4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-(3-methyl-4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-{2-{4-(2,4-bis-trifluoromethyl-benzoylamine)-3-dimethylcarbamoyl]acetoxymethyl}-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-methylbiphenyl-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-{2-[3-dimethylcarbamoyl-4-(2-ethyl-4-trifluoromethyl-benzoylamine)phenyl]acetoxymethyl}-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-ethylbiphenyl-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-isopropyl-biphenyl-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-isopropyl-biphenyl-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate key is lots

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-thiophene-2-elmaloglou acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-thiophene-3-elmaloglou acid,

diethyl ether 2-(2-{4-dimethylcarbamoyl-5-[(4'-triptorelin-2-carbonyl)amino]-pyridine-2-yl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-(3-methylthiophene-2-yl)malonic acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-(5-methylthiophene-2-yl)malonic acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-thiazol-2-elmaloglou acid,

diethyl ether 2-(2-{3-ethoxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-methoxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-isopropoxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-benzyloxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-fenil is Lanovoy acid,

diethyl ether 2-(2-{3-hikkoshi-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ester of 2-phenyl-2-(2-{3-piperidine-1-yl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diethyl ester of 2-phenyl-2-(2-{3-pyrrolidin-1-yl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diethyl ether 2-(2-{3-dimethylamino-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-morpholine-4-yl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-diethylamino-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{2-chloro-4-[(4'-triptorelin-2-carbonyl)amino]benzoyloxy}ethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-etoxycarbonyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(3-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}propionyloxy)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-benzyloxycarbonyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-carboxy-4-[(4-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-isopropoxycarbonyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-methoxycarbonyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-acetylamino-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-methoxycarbonylamino-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-(4-methylthiazole-2-yl)-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ester of 2-phenyl-2-(2-{6-[(4'-triptorelin-2-carbonyl)amino]biphenyl-3-yl}acetoxymethyl)malonic acid,

diethyl ether 2-(2-{3-formyl-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylaminomethyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-(methoxymethylethoxy)-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-isobutyryl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid and

diethyl e is Il-2-(2-{3-(1-hikkoshi-2-methylpropyl)-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid;

(29) the Ester compound or its prodrug, or pharmaceutically acceptable salt of any of them in accordance with the above paragraph (1), which is chosen from the group including

4-[2-phenyl-2,2-bis-(2,2,2-triptoreline)-ethoxycarbonylmethyl]phenyl ester of 4'-triptorelin-2-carboxylic acid,

4-[2-phenyl-2,2-bis-(2,2,2-triptoreline)ethoxycarbonylmethyl]phenyl ether-biphenyl-2-carboxylic acid,

4-(2,2-bis-ethylcarboxyl-2-phenyl-ethoxycarbonylmethyl)phenyl ether 4'-triptorelin-2-carboxylic acid,

4-(2,2-bis-ethylcarboxyl-2-phenyl-ethoxycarbonylmethyl)-2-hlorfenilovy ether 4'-triptorelin-2-carboxylic acid,

4-(3,3-bis-ethylcarbazole-3-phenyl-propoxycarbonyl)-2-hlorfenilovy ether 4'-triptorelin-2-carboxylic acid,

4-(3,3-bis-ethylcarbazole-3-phenyl-propoxycarbonyl)phenyl ether 4'-triptorelin-2-carboxylic acid and

4-(3,3-bis-ethylcarbazole-3-phenyl-propoxycarbonyl)-2,6-dichlorphenoxy ether 4'-triptorelin-2-carboxylic acid;

(30) the Ester compound or its prodrug, or pharmaceutically acceptable salt of any of them in accordance with paragraph (1) above, which is selected from the group including

diethyl ester of 2-phenyl-2-{2-[4-(4'-triptorelin-2-carbonyloxy)phenyl]acetoxymethyl}malonic acid,

p> diethyl ether 2-{2-[3-dimethylcarbamoyl-4-(4'-triptorelin-2-carbonyloxy)phenyl]acetoxymethyl}-2-phenylmalonate acid,

diethyl ether 2-{2-[3-methoxy-4-(4'-triptorelin-2-carbonyloxy)phenyl]acetoxymethyl}-2-phenylmalonate acid and

3-[2-(2,2,2-triptoreline)naphthalene-1-yl]propyl ester 4-[(4'-triptorelin-2-carbonyl)amino]benzoic acid;

(31) the Ester compound or its prodrug, or pharmaceutically acceptable salt of any of them in accordance with paragraph (1) above, which is selected from the group including

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-isopropylmalonic acid,

diethyl ether 2-terbutyl-2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-malonic acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-isobutylamino acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-propylmalonic acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-ethylmalonic acid,

diethyl ester of 2-butyl-2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl) - Amin is]phenyl}acetoxymethyl)malonic acid,

diethyl ether 2-allyl-2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

ethyl ester of 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxy)-2,2-bis-ethoxycarbonylpyrimidine acid and

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-(1-methylbutyl)malonic acid;

(32) a Pharmaceutical composition comprising the ester compound or its prodrug, or pharmaceutically acceptable salt of any of them on any of the above items (1)to(31) and a pharmaceutically acceptable carrier;

(33) the Inhibitor of MTP (microsomal protein transfer triglycerides), comprising as an active ingredient ester compound or its prodrug, or pharmaceutically acceptable salt of any of them in accordance with any of the above points(1)-(31);

(34) Agent for the treatment or prophylaxis of hyperlipidemia, comprising as an active ingredient ester compound or its prodrug, or pharmaceutically acceptable salt of any of them in accordance with any of the above points(1)-(31);

(35) the Agent for the treatment or prevention of arteriosclerosis, comprising as an active ingredient ester compound or its Strait is carstvo, or pharmaceutically acceptable salt of any of them in accordance with any of the above points(1)-(31);

(36) the Agent for the treatment or prevention of coronary artery disease, comprising as an active ingredient ester compound or its prodrug, or pharmaceutically acceptable salt of any of them in accordance with any of the above points(1)-(31);

(37) the Agent for treating or preventing obesity, comprising as an active ingredient ester compound or its prodrug, or pharmaceutically acceptable salt of any of them in accordance with any of the above points(1)-(31);

(38) the Agent for treating or preventing diabetes, comprising as an active ingredient ester compound or its prodrug, or pharmaceutically acceptable salt of any of them in accordance with any of the above points(1)-(31);

(39) the Agent for treating or preventing hypertension comprising as an active ingredient ester compound or its prodrug, or pharmaceutically acceptable salt of any of them in accordance with any of the above points(1)-(31);

(40) Agent for the treatment or prophylaxis of hyperlipidemia, arteriosclerosis, coronary artery disease, obesity, diabetes or hypertension, comprising an inhibitor of M Is R, selectively inhibiting MTP (microsomal protein transfer triglycerides) in the small intestine, and a pharmaceutically acceptable carrier;

(41) Agent for the treatment or prophylaxis according to the above item (40), where the inhibitor of MTP almost did not inhibit MTP in the liver, but to a significant extent only inhibits MTP in the small intestine;

(42) Agent for the treatment or prophylaxis according to the above item (41), where after entered the MTP inhibitor inhibits MTP in the small intestine, it is metabolized in the small intestine, liver and blood to the amount at which the remaining liver MTP inhibitor practically did not inhibit MTP in the liver;

(43) Agent for the treatment or prophylaxis according to the above item (42), where the remaining MTP inhibitor in the liver is metabolized to a state at which TG-releasing activity of the liver remains at the level of about 80% or more from the normal level;

(44) the Agent for treatment or prevention in accordance with the above paragraphs (40)through(43), where the MTP inhibitor is a compound having at least one ester linkage;

(45) the Agent for the treatment or prophylaxis according to the above item (44), where after the connection having at least one ester bond, the times, the t MTP-inhibitory activity, ester fragment compounds metabolized in the blood, turning into an inactive substance;

(46) Agent for the treatment or prophylaxis according to the above paragraphs (40)-(45), where the MTP inhibitor is an ester compound or its prodrug, or pharmaceutically acceptable salt of any of them mentioned in any of the above items(1)-(31);

(47) the Method of treatment or prophylaxis of hyperlipidemia, arteriosclerosis, coronary artery disease, obesity, diabetes or hypertension, including the introduction of a compound that selectively inhibits MTP (microsomal protein transfer triglycerides) in the small intestine;

(48) the Method according to the above item (47), where after the compound inhibits MTP in the small intestine, it is metabolized in the small intestine, liver and blood to the amount at which the remaining liver the specified connection does not inherently inhibits MTP in the liver;

(49) the Method according to the above item (47), where the remainder of the compound is metabolized in the liver to a state in which the TG-releasing activity of the liver remains at the level of about 80% or more from the normal level;

(50) the Method in accordance with the above paragraphs (47)-(49), where the compound has at least one ester linkage;

(51) the Method according to the above item (50), where after the connection having at least one ester linkage, shows MTP-inhibitory activity, ester fragment of the compound is metabolized in the blood, becoming inactive;

(52) the Method in accordance with the above paragraphs (47)-(52), where the compound is an ester compound or its prodrug, or pharmaceutically acceptable salt of any of them mentioned in any of the above items(1)-(31);

(53) Agent for the treatment or prophylaxis according to the above paragraphs (40)-(46), where the agent is an agent for the treatment or prophylaxis of hyperlipidemia, which is used in combination with other antihyperlipidemic drug(s) agent(s);

(54) Agent for the treatment or prophylaxis according to the above item (53), where other antihyperlipidemic drug is a drug Statesboro type;

(55) Agent for the treatment or prophylaxis according to the above item (54), where the drug Statesboro type represents one or more drugs selected from the group consisting of lovastatin, simvastatin, pravastatin, fluvastatin, atorvastatin and zerowaste the ina;

(56) Agent for the treatment or prophylaxis according to the above paragraphs (40)-(46), where the agent is an agent for treatment or prevention of obesity, which is used in combination with other drug(s) agent(s) against obesity;

(57) Agent for the treatment or prophylaxis according to the above item (56), where another drug against obesity is a mazindol and/or orlistat;

(58) Agent for the treatment or prophylaxis according to the above paragraphs (40)-(46), where the agent is an agent for treatment or prevention of diabetes, which is used in combination with other antidiabetics(s) of drug(s) agent(s);

(59) Agent for the treatment or prophylaxis according to the above item (58), where another antidiabetic medicine represents one or more drugs selected from the group consisting of insulin preparations, medicines on the basis of sulfonylureas, which stimulate the production of insulin medicines sulfonamidnuyu medicines, biguanide drugs, inhibitors α-glucosidase and improves insulin resistance medication;

(60) Agent for the treatment or prophylaxis under the above paragraph 59, where other antidiabetic drug is one or more drugs selected from the group consisting of insulin, glibenclamide, tolbutamide, glyclopyramide, acetohexamide, glimepiride, tolazamide, gliklazida, nateglinide, glybuzole, Metformin hydrochloride, the hydrochloride of buformin, voglibose, acarbose hydrochloride and pioglitazone;

(61) Agent for the treatment or prophylaxis according to the above paragraphs (40)-(46), where the agent is an agent for treatment or prevention of hypertension, which is used in combination with other antihypertensive(s) of drug(s) agent(s);

(62) Agent for the treatment or prophylaxis according to the above item (61), where another antihypertensive drug is one or more drugs selected from the group consisting of loop diuretics, inhibitors of angiotensin converting enzyme, receptor antagonists angiotensin II, calcium antagonists, β-blockers, α,β-blockers and α-blockers;

(63) Agent for the treatment or prophylaxis according to the above item (62), where another antihypertensive drug is one or more drugs selected from the group is s, including furosemide delayed release, captopril, captopril sustained-release, enalapril maleate, alacepril, delapril hydrochloride, cilazapril, lisinopril, benazepril hydrochloride, imidapril hydrochloride, temocapril hydrochloride, inapril hydrochloride, trandolapril, perindopril erbumine, losartan potassium, candesartan, cilexetil, nicardipine hydrochloride, nicardipine hydrochloride sustained release, nilvadipine, nifedipine, nifedipine slow release, benidipine hydrochloride, diltiazem hydrochloride, diltiazem hydrochloride sustained release, nisoldipine, nitrendipin, manidipine hydrochloride, barnidipine hydrochloride, efonidipine hydrochloride, amlodipine, besylate, felodipine, cilnidipine, aranidipine, propranolol hydrochloride, propranolol hydrochloride slow release, pindolol, pindolol slow release, indenolol hydrochloride, carteolol hydrochloride, carteolol hydrochloride sustained release, bunitrolol hydrochloride, bunitrolol hydrochloride sustained release, atenolol, acebutolol hydrochloride, metoprolol tartrate, metoprolol tartrate sustained release, nipradilol, penbutolol sulfate, tilisolol hydrochloride, carvedilol, bisoprolol fumarate, betaxolol hydrochloride, celiprolol hydrochloride, bopindolol malonate, bevanda the ol hydrochloride labetalol hydrochloride, arotinolol hydrochloride, amosulalol hydrochloride, prazosin hydrochloride, terazosin hydrochloride, doxazosin mesilate, bunazosin hydrochloride, bunazosin hydrochloride sustained release, urapidil and phentolamine mesilate;

(64) the Use of an agent for treatment or prevention in accordance with the above paragraphs (34)-(46), and other(s), antihyperlipidemic(s) of drug(s) drug for treatment or prevention of hyperlipidemia;

(65) the Application in accordance with paragraph (64), where other antihyperlipidemic drug is a drug Statesboro type;

(66) used in accordance with the above paragraph (64), where the drug Statesboro type represents one or more drugs selected from the group consisting of lovastatin, simvastatin, pravastatin, fluvastatin, atorvastatin and tseriwastatina;

(67) the Use of an agent for treatment or prevention in accordance with the above paragraphs (34)-(46), and other(s) of drug(s) anti-obesity treatment or prevention of obesity;

(68) used in accordance with the above paragraph (67), where another drug against obesity is a mazindol and/or orlistat;

(69) the Use of an agent DL the treatment or prevention in accordance with the above paragraphs (34)-(46), and other(their) antidiabetics(s) of drug(s) drug for treatment or prevention of diabetes;

(70) used in accordance with the above paragraph (69)where other antidiabetic medicines represent one or more drugs selected from the group consisting of insulin preparations, medicines on the basis of sulfonylureas, which stimulate the production of insulin medicines sulfonamidnuyu medicines, biguanide drugs, inhibitors α-glucosidase and improves insulin resistance medication;

(71) the Application in accordance with the above paragraph (70), where another antidiabetic medicine represents one or more drugs selected from the group consisting of insulin, glibenclamide, tolbutamide, glyclopyramide, acetohexamide, glimepiride, tolazamide, gliklazida, nateglinide, glybuzole, Metformin hydrochloride, the hydrochloride of buformin, voglibose, acarbose hydrochloride and pioglitazone;

(72) the Use of an agent for treatment or prevention in accordance with the above paragraphs (34)-(46), and other(their) antihypertensive(s) of drug(s) drug for treatment or prevention of hypertension;

(73) the Application in accordance with the above paragraph (72), where another antihypertensive drug is Soboh the one or more drugs, selected from the group consisting of loop diuretics, inhibitors of angiotensin converting enzyme, receptor antagonists angiotensin II, calcium antagonists, beta-blockers, alpha/beta blockers and alpha blockers;

(74) the Application in accordance with the above paragraph (73), where another antihypertensive drug is one or more drugs selected from the group comprising furosemide delayed release, captopril, captopril sustained-release, enalapril maleate, alacepril, delapril hydrochloride, cilazapril, lisinopril, benazepril hydrochloride, imidapril hydrochloride, temocapril hydrochloride, inapril hydrochloride, trandolapril, perindopril erbumine, losartan potassium, candesartan, cilexetil, nicardipine hydrochloride, nicardipine hydrochloride sustained release, nilvadipine, nifedipine, nifedipine slow release, benidipine hydrochloride, diltiazem hydrochloride, diltiazem hydrochloride slow release, nisoldipine, nitrendipin, manidipine hydrochloride, barnidipine hydrochloride, efonidipine hydrochloride, amlodipine, besylate, felodipine, cilnidipine, aranidipine, propranolol hydrochloride, propranolol hydrochloride sustained-release, pindolol, pindolol slow release, indenolol hydro is lurid, carteolol hydrochloride, carteolol hydrochloride sustained release, bunitrolol hydrochloride, bunitrolol hydrochloride sustained release, atenolol, acebutolol hydrochloride, metoprolol tartrate, metoprolol tartrate sustained release, nipradilol, penbutolol sulfate, tilisolol hydrochloride, carvedilol, bisoprolol fumarate, betaxolol hydrochloride, celiprolol hydrochloride, bopindolol malonate, bevantolol hydrochloride, labetalol hydrochloride, arotinolol hydrochloride, amosulalol hydrochloride, prazosin hydrochloride, terazosin hydrochloride, doxazosin mesilate, bunazosin hydrochloride, bunazosin hydrochloride sustained release, urapidil and phentolamine mesilate;

(75) a Pharmaceutical composition comprising an effective amount of the ester compound or its prodrug, or pharmaceutically acceptable salt of any of them on any of the above items (1)to(31), pharmaceutically acceptable an appropriate amount of ethanol and ether complex of propylene glycol and fatty acids;

(76) the Pharmaceutical composition according to the above item (75)comprising from 25 to 35% by weight of ethanol and from 65 to 75% by weight of ester of propylene glycol and fatty acids;

(77) Encapsulated preparative form comprising the pharmaceutical composition in accordance with visheukazannim the points (75) or (76);

(78) Encapsulated preparative form in accordance with the above paragraph (77), where the encapsulated preparative form is a hard capsule or soft capsule;

(79) the Compound biphenyl represented by formula (100)

where

R1'represents hydrogen, C1-C6-alkyl, halogen, halogen With1-C6-alkyl or C1-C6-alkoxy;

R2"'represents hydrogen, C1-C6-alkyl, halogen, halogen-C1-C6-alkyl or C2-C6alkenyl;

R3"represents-CON(R11a)(R12a), where each of R11aand R12aindependently represents hydrogen, C1-C6-alkyl, optionally substituted C6-C14aryl, optionally substituted C7-C16-aralkyl,1-C6-alkoxy, or R11aand R12ataken together with the nitrogen to which they are attached, may form

(where p is an integer from 0 to 2);

R4'represents hydrogen, halogen, C1-C6-alkyl or halogen-C1-C6-alkyl;

R50represents hydrogen, C1-C6-alkyl, optionally substituted C6-C14aryl or optionally substituted C7-C 16-aralkyl; and

la is an integer from 1 to 3,

or its prodrug, or pharmaceutically acceptable salt of any of them; and

(80) Connection biphenyl in accordance with the above paragraph (79), where

R1'represents hydrogen,

R2"'represents a halogen With1-C6-alkyl,

R3"represents-CON(R11b)(R12b), where each of R11band R12bindependently represents hydrogen or C1-C6-alkyl, or R11band R12btaken together with the nitrogen to which they are attached, may form

(where p is an integer from 0 to 2);

R4'represents hydrogen, and

R50represents hydrogen or C1-C6-alkyl,

or its prodrug, or pharmaceutically acceptable salt of any of them.

Definitions of each of the substituents used in the present invention are as follows.

The term "C1-C6-alkyl" refers to linear or branched alkyl group containing from 1 to 6 carbon atoms, and examples include methyl, ethyl, propyl, isopropyl, butyl, isobutyl, sec-butyl, tert-butyl, pentyl, isopentyl, neopentyl, tert-pentyl, or hexyl, etc., preferably a linear or branched alkyl group containing 1-4 carbon atoms, more preferably it stands, ethyl or isopropyl. Preferable examples in the case of R1, R2, R2'and R2"include methyl, ethyl, or isopropyl; preferable examples in the case of R3and R4include methyl, ethyl, propyl, isopropyl, butyl or isobutyl; a preferred example in the case of R5, R6and R7includes methyl; preferred examples in the case of R8and R9include methyl or ethyl; preferred examples in the case of R10include methyl, ethyl, or isopropyl; preferable examples in the case of R11and R12include methyl, ethyl, propyl or isopropyl; preferable examples in the case of R13and R14include methyl or ethyl; preferred example in the case of R15includes isopropyl; preferable examples in the case of R16and R17include methyl or ethyl; preferred examples in the case of R18and R19include methyl, ethyl, propyl, isopropyl, butyl, isobutyl, sec-butyl, tert-butyl, pentyl or isopentyl, more preferably ethyl; preferred examples in the case of R20include methyl, ethyl, propyl, isopropyl or isobutyl, preferably ethyl; preferred example in the case of R21and R22includes methyl; and preferable examples for D include ethyl, propyl, isopropyl, butyl, isobutyl, sec-bout the l, Deut-pentyl etc.

Examples of substituents for "optionally substituted C1-C6-alkyl" include halogen, carboxyl, hydroxy, amino, nitro, cyano, C1-C6-alkoxy, C7-C16-aralkylated,2-C7-alkoxycarbonyl,6-C14-aryl, C1-C6-alkylthio,1-C6-alkylsulfonyl,1-C6-alkylsulfonyl, C1-C6-alkylamino, acylamino and the like, among which a hydroxyl group is preferred. The number of substituents is from 1 to 5, preferably 1-3.

The term "C3-C7-cycloalkyl" refers to cycloalkyl containing from 3 to 7 carbon atoms, specifically, for cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, 1-methylcyclohexyl or cycloheptyl. Preferred examples include cycloalkyl containing from 3 to 6 carbon atoms, specifically, cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl. More preferred examples include cyclopropyl or cyclohexyl. A preferred example in the case of R1and R2includes cyclohexyl; a preferred example in the case of R10includes cyclohexyl; a preferred example in the case of R18and R19includes cyclohexyl; a preferred example in the case of R20includes cyclohexyl; and preferable examples for Kohl is and include cyclopentyl or cyclohexyl. Also is preferred that R8and R9taken together, formed cyclopentyl or cyclohexyl.

The term "C1-C6-alkoxy" refers to a linear or branched CNS group containing from 1 to 6 carbon atoms, and examples include methoxy, ethoxy, propoxy, isopropoxy, butoxy, tert-butoxy, pentyloxy, tert-pentyloxy or hexyloxy etc., preferably to the CNS group containing from 1 to 4 carbon atoms, such as methoxy, ethoxy, isopropoxy, butoxy or tert-butoxy, and more preferably methoxy or ethoxy. Preferable examples in the case of R1, R2, R2'and R2"include methoxy, isopropoxy or butoxy; preferable examples in the case of R3and R4include methoxy, ethoxy, propoxy or isopropoxy; preferable examples in the case of R5, R6and R7include methoxy or ethoxy; a preferred example in the case of R11and R12includes methoxy; and preferable examples for R15include methoxy, ethoxy, propoxy or isopropoxy.

The term "halogen" refers to chlorine, bromine, fluorine or the like. Preferable examples in the case of R1include fluorine or chlorine; preferable examples for R2'and R2"include fluorine, chlorine or bromine; preferable examples in the case of R and R4include chlorine or bromine; and preferable examples for R5, R6and R7include fluorine or chlorine.

The term "halogen-C1-C6-alkyl" refers to a specified With1-C6-alkyl, substituted specified halogen, and its examples include chloromethyl, methyl bromide, vermeil, trifluoromethyl, trichloromethyl, tribromoethyl, trichlorethyl, pentafluoropropyl or chlorobutyl etc., preferably chloromethyl, methyl bromide, vermeil, trifluoromethyl, triptorelin or trichloromethyl and, more preferably trifluoromethyl. A preferred example for R1, R2, R2'and R2"includes trifluoromethyl; a preferable example for R3and R4includes trifluoromethyl; a preferable example for R5, R6and R7includes trifluoromethyl; preferable examples for R16and R17include trifluoromethyl or triptorelin; and preferable examples for R18and R19include trifluoromethyl or triptorelin.

The term "halogen-C1-C6-alkyloxy" includes, for example, chloromethoxy, bromatology, formations, cryptometrics, trichlorethylene, tribromomethane, trichlorethylene, pentafluoropropionic or chlorobutyrate etc., preferably chloromethoxy, bromatology, formations, cryptometrics or trichlorethylene and more site is preferably cryptometrics. A preferred example for the case R1, R2, R2'and R2"includes cryptometrics.

The term "C2-C12-alkoxyalkyl" refers to alkoxyalkyl, in which CNS fragment has the same meaning as defined above, alkoxy, and alkyl fragment has the same meaning as the above alkyl, and its examples include methoxymethyl, ethoxymethyl, propoxymethyl, butoxymethyl, petrochemical, hexyloxymethyl, ethoxyethyl or methoxyethyl etc. Preferred example for R18and R19includes methoxyethyl.

The term "C2-C7-alkylaryl" refers to acetyl, propionyl, butyryl or pivaloyl, etc. and preferred example for R21and R22includes acetyl.

The term "C1-C7-alkylsulfonyl" refers to methanesulfonyl, econsultancy, propylsulfonyl, butylsulfonyl, pentasulphide or hexylsilane etc., and a preferred example for R21and R22includes methylsulphonyl.

The term "C2-C7-alkoxycarbonyl" refers to alkoxycarbonyl, in which the alkyl fragment contains from 1 to 6 carbon atoms, such as methoxycarbonyl, etoxycarbonyl, propoxycarbonyl, isopropoxycarbonyl, butoxycarbonyl, isobutoxide, tert-butoxycarbonyl, pentyloxybenzoyl, tert-pentyloxy arbonyl or hexyloxybenzoyl etc. Preferred examples include methoxycarbonyl, etoxycarbonyl, propoxycarbonyl butoxycarbonyl. A preferred example in the case of R2includes butoxycarbonyl; a preferable example for R5, R6and R7includes methoxycarbonyl; a preferred example in the case of R13and R14includes methoxycarbonyl; a preferred example in the case D includes etoxycarbonyl.

The term "C1-C6-acyl refers to formyl, containing one carbon atom, or alkanoyl containing from 2 to 6 carbon atoms, such as acetyl, propanol, butyryl or pivaloyl, etc., and its preferred examples include formyl, acetyl or pivaloyl. A preferred example for R2and R2"includes acetyl; a preferable example for R3includes formyl; a preferable example for R5, R6and R7includes acetyl; a preferable example for R13and R14includes acetyl; and a preferred example for R21and R22includes acetyl.

The term "alcander" means the group having preferably 1-6 carbon atoms, and examples include the methylene, ethane-1,2-diyl, ethane-1,1-diyl, propane-1,3-diyl, butane-1,4-diyl, pentane-1,5-diyl, hexane-1,6-diyl, 1,1-dimethylether-1,2-diyl, 1,1-diethylether-1,2-diyl, 2,2-dimethylated-1,2-diyl, 2,2-diethylether-1,2-diyl, 1,1-DIMETHYLPROPANE-1,3-Hai who, 1,1-diethylpropane-1,3-diyl, 2,2-DIMETHYLPROPANE-1,3-diyl, 2,2-diethylpropane-1,3-diyl, 3,3-DIMETHYLPROPANE-1,3-diyl or 3.3-diethylpropane-1,3-diyl etc. Preferred examples for Alk1and Alk2include methylene, ethane-1,2-diyl, ethane-1,1-diyl, propane-1,3-diyl etc.

The term "alcander" preferably means a group containing from 2 to 6 carbon atoms, and its examples include ethylene-1,2-diyl, 1-propene-1,3-diyl, 2-propene-1,3-diyl, 1-butene-1,4-diyl, 2-butene-1,4-diyl, 3-butene-1,4-diyl or 1,3-butadiene-1,4-diyl etc. Preferred examples for Alk1and Alk2include ethylene-1,2-diyl, 1-propene-1,3-diyl, 2-propene-1,3-diyl etc.

The term "C6-C14aryl" refers to phenyl, naphthyl or biphenyl, etc., preferably for phenyl.

In the "optionally substituted C6-C14the aryl" substituent(s) is/are not specifically limited, and they may be the same or different from each other and can be placed arbitrarily. The number of substituents is not limited specifically as long as they are chemically acceptable, although preferably the number of substituents is from 1 to 3. Specifically, examples of the substituent include1-C6-alkyl (e.g. methyl, ethyl, propyl, isopropyl, butyl, tert-butyl etc), hydroxy, C1-C6-alkoxy (e.g. methoxy, ethoxy, propoxy, butoxy etc.), g is lågen (for example, fluorine, chlorine, bromine, etc.), nitro, cyano, C1-C6-acyl (e.g. formyl, acetyl, propionyl etc.)1-C6-acyloxy (for example, formyloxy, acetoxy, propionyloxy etc), mercapto, C1-C6-alkylthio (for example, methylthio, ethylthio, propylthio, butylthio, isobutyric, etc), amino, C1-C6-alkylamino (for example, methylamino, ethylamino, propylamino, butylamino and so on), di(C1-C6-alkyl)amino (e.g. dimethylamino, decylamine, dipropylamino, dibutylamino etc), carboxyl,2-C7-alkoxycarbonyl (for example, methoxycarbonyl, etoxycarbonyl, propoxycarbonyl etc), amido, trifluoromethyl, C1-C6-alkylsulfonyl (for example, methylsulphonyl, ethylsulfonyl etc), aminosulfonyl,3-C7-cycloalkyl (for example, cyclopentyl, cyclohexyl, etc.), phenyl, acylamino (for example, acetamido, propionamido etc) and the like, among which hydroxy, C1-C6-alkyl, C1-C6-alkoxy, mercapto, C1-C6-alkylthio, halogen, trifluoromethyl, C1-C6-acyl, C2-C7-alkoxycarbonyl, acylamino are preferred.

A preferred example for R1and R2includes phenyl which may be substituted by halogen With1-C6-alkyl (e.g. trifluoromethyl, etc.)1-C6-alkyl (n is an example, the stands, ethyl, etc.), halogen (e.g. fluorine, chlorine, bromine, etc.)1-C6-alkoxy (e.g. methoxy, etc.)1-C6-acyl (e.g. acetyl), C2-C6-alkenyl (for example, isopropanol etc) or cyano; a preferable example for R5, R6and R7includes phenyl which may be substituted With halogen1-C6-alkyl (e.g. trifluoromethyl, etc.)1-C6the alkyl (for example, stands etc), halogen (e.g. chlorine, etc.) or (C1-C6-alkoxy (e.g. methoxy, etc.); a preferable example for R8and R9includes phenyl; a preferable example for R11and R12includes phenyl; a preferable example for R18and R19includes phenyl; a preferable example for R43includes biphenyl; a preferable example for ring And includes phenyl; and preferred examples of the rings include phenyl or naphthyl.

The term "C7-C16-aralkyl" refers to arylalkyl, in which the aryl fragment represents phenyl (which may be substituted by 1-3 substituents mentioned above in the description of the aryl), alkyl fragment is an alkyl containing from 1 to 6 carbon atoms. Examples include benzyl, phenetyl, phenylpropyl, phenylbutyl or phenylhexa and so on, among which benzyl Il is phenylethyl are preferred. A preferred example for R1and R2includes benzyl; a preferable example for R11and R12includes benzyl, and a preferred example for rings includes benzyl.

The term "C6-C14-aryloxy" refers to phenoxy, naphthyloxy etc. (where the phenyl group or naftalina group can be substituted by 1-3 substituents mentioned above in the description of the aryl), preferably to phenoxy. A preferred example for R1and R2includes phenoxy, and a preferred example for R15includes phenoxy.

The term "C7-C16-aralkylated" refers to aralkylated, in which CNS fragment has from 1 to 4 carbon atoms (where the aryl group may be substituted by 1-3 substituents mentioned above in the description of the aryl), and its examples include benzyloxy, penetrate, phenylpropoxy, phenylbutyrate etc., preferably benzyloxy. A preferred example for R1and R2includes benzyloxy, a preferred example for R3includes benzyloxy; and a preferred example for R15includes benzyloxy.

The term "C7-C15-arylcarbamoyl" refers to benzoyl, Naftoli etc. (where the phenyl group or naftalina group can be substituted by 1-3 substituents mentioned above in the description of the aryl), preferably the benzoyl. Suppose the equipment example for R 1and R2includes benzoyl.

The term "C7-C15-arylcarboxamide" refers to phenylcarbonylamino, nattermannallee etc. (where the phenyl group or naftalina group can be substituted by 1-3 substituents mentioned above in the description of the aryl), preferably the benzoyl. A preferred example in the case of rings includes phenylcarbonylamino.

The term "C8-C16-aralkylamines" refers to benzylmorphine, nattermannallee etc. (where the phenyl group or naftalina group can be substituted by 1-3 substituents mentioned above in the description of the aryl), preferably to benzylmorphine. A preferred example in the case of rings includes benzylmorphine.

The term "heterocycle" refers to a 5-6-membered heteroaromatic ring, a 5-6-membered saturated heterocycle, or a 5-6-membered unsaturated heterocycle, each of which contains from 1 to 3 heteroatoms selected from nitrogen, oxygen and sulfur, as atoms constituting the ring and different from carbon, or a condensed heterocyclic ring, where the heterocycle and a benzene ring are condensed. Specifically, its examples include thiophene-2-yl, thiophene-3-yl, furan-2-yl, furan-3-yl, pyrrol-1-yl, pyrrol-2-yl, pyrrol-3-yl, imidazol-1-yl, imidazol-2-yl, imidazol-4-the l imidazol-5-yl, pyrazole-1-yl, pyrazole-3-yl, pyrazole-4-yl, thiazol-2-yl, thiazol-4-yl, thiazol-5-yl, oxazol-2-yl, oxazol-4-yl, oxazol-5-yl, isoxazol-3-yl, isoxazol-4-yl, isoxazol-5-yl, pyrimidine-2-yl, pyrimidine-4-yl, pyrimidine-5-yl, pyridine-2-yl, pyridin-3-yl, pyridine-4-yl, pyrrolidin-2-yl, pyrrolidin-3-yl, benzothiophen-2-yl, benzothiophen-3-yl, benzofuran-2-yl, bontfaen-3-yl, indol-2-yl, indol-3-yl, benzimidazole-1-yl, benzimidazole-2-yl, benzothiazol-2-yl, benzoxazol-2-yl, quinoline-2-yl, quinoline-3-yl, quinoline-4-yl, isoquinoline-1-yl, isoquinoline-3-yl, isoquinoline-4-yl, 1,3,4-thiadiazole-2-yl, morpholine-4-yl, etc.

Preferred examples of R1and R2include thiophene-3-yl; preferred examples of ring a include imidazole-5-yl, thiazol-5-yl, pyridin-3-yl or pyrrolidin-2-yl; a preferable example for R3includes thiazol-2-yl; and preferred examples of the rings include pyridine-2-yl, pyridin-3-yl, thiophene-2-yl, thiophene-3-yl or thiazol-2-yl.

As for the substituent in the "optionally substituted heterocycle", there can be mentioned the same substituents listed above in the description of the aryl. The number of substituents does not specifically limited, as long as they are chemically acceptable, although preferably the number of substituents is about 1-3.

"C2-C6alkenyl" refers to a linear or razvetvlenno the th alkenylphenol group, containing from 2 to 6 carbon atoms, and its examples include vinyl, n-propenyl, Isopropenyl, n-butenyl, Isobutanol, second-butenyl, tert-butenyl, n-pentenyl, isopentenyl, neopentyl, 1-methylpropenyl, n-hexenyl, isohexyl, 1,1-dimethylbutyl, 2,2-dimethylbutyl, 3,3-dimethylbutyl, 3,3-dimethylpropyl, 2-ethylbutyl etc. Preferred example for the cases R2and R2'includes n-propenyl, and a preferred example for D includes n-propenyl.

The term "prodrug" of a compound refers to a derivative of the compound of the present invention, which has a group capable of chemically or metabolically developing, and manifests pharmaceutical activity after hydrolysis or solvolysis, or conversion under physiological conditions.

For example, it may be listed derivative, in which the Deputy, such as-CO-C1-C6-alkyl, -CO2-C1-C6-alkyl, -CONH-C1-C6-alkyl, -CO-C2-C6alkenyl, -CO2-C2-C6alkenyl, -CONH-C2-C6alkenyl, -CO-C6-C14-aryl, -CO2-C6-C14-aryl, -CONH-C6-C14-aryl, -CO-heterocycle, -CO2-heterocycle, -CONH-heterocycle, etc. where any of the above With1-C6-alkyl, C2-C6-alkenyl,6-C14-aryl and heterocycle may be substituted with halogen, C1-the 6-alkyl, hydroxy, C1-C6-alkoxy, carboxyla, amino, amino acid residue, RHO3H2, -SO3H, residue-CO-poly (ethylene glycol), residue-CO2-glycol-CO-polietilenglikoli balance monoalkylated simple ester or-CO2-polietilenglikoli balance monoalkylated simple ether)attached to the hydroxyl group of the connection.

Can also be illustrated by the derivative, in which the Deputy, such as-CO-C1-C6-alkyl, -CO2-C1-C6-alkyl, -CO-C2-C6alkenyl, -CO2-C2-C6alkenyl, -CO2-C6-C14-aryl, -CO-C6-C14-aryl, -CO-heterocycle, -CO2-heterocycle, etc. where any of the above With1-C6-alkyl, C2-C6-alkenyl,6-C14-aryl and heterocycle may be substituted with halogen, C1-C6-alkyl, hydroxy, C1-C6-alkoxy, carboxyla, amino, amino acid residue, RHO3H2, -SO3H, residue-CO-poly (ethylene glycol), residue-CO2-glycol-CO-polietilenglikoli balance monoalkylated simple ester or-CO2-polietilenglikoli balance monoalkylated simple ester or RHO3H2etc)attached to the amino group of the connection.

In addition, there may be proil utrirovanno derivative, in which Deputy, such as1-C6-alkoxy, C6-C14-aryloxy etc. (where any of these With1-C6-alkoxy or C6-C14-aryloxy may be substituted with halogen, C1-C6-alkyl, hydroxy, C1-C6-alkoxy, carboxyla, amino, amino acid residue, RHO3H2, -SO3H, a residue of polyethylene glycol or polietilenglikoli balance monoalkylated simple ether and so on)attached to the carboxyl group of the connection.

The term "pharmaceutically acceptable salt" includes various additive salts of inorganic acids such as hydrochloride, hydrobromide, sulfate, phosphate or nitrate, etc.; various additive salts of organic acids such as acetate, propionate, succinate, glycolate, lactate, malate, oxalate, tartrate, citrate, maleate, fumarate, methanesulfonate, bansilalpet, p-toluensulfonate or ascorbate, etc.; or salts with amino acids such as aspartate or glutamate and so on, though not limited to the above. This can be a hydrated compound, hydrate or MES depending on the circumstances.

The expression "MTP in the small intestine" refers to materials existing in the epithelial cells of the small intestine.

The expression "MTP in the liver" refers to materials existing in the liver cells.

The expression "with the collective inhibits MTP in the small intestine" means, the level of inhibition of at least about 5 times higher, preferably about 10 times higher than the inhibition of MTP in other parts of the body such as the liver and heart, especially in the liver. For greater specificity, on the basis of a test of metabolic stability S9 this means that in the test using S9 human or hamster residual fraction unmodified form 10 minutes after the processing of S9 of the small intestine approximately 10 times or more that in the case of the processing of S9 liver (see example test 7).

The expression is metabolized to a number, in which the remaining MTP inhibitor in the liver essentially did not inhibit MTP in the liver means that almost all oral introduced MTP inhibitors are metabolized to the inactive metabolite before it enters the liver or in the time of exposure in the liver and essentially do not show MTP-inhibiting activity in the liver; i.e. inhibitors of materials and equipment into such compounds, which essentially does not inhibit the release of TG from the liver. More specifically, this means the condition under which the TG-releasing activity of the liver remains at the level of about 80% or more, preferably about 90% or more, more preferably 100% of the normal level. In terms of metabolism this means that the ratio of the inactive metabolite to unmodified formed blood of the portal vein is about 8 or more to one one hour after oral administration to hamsters, i.e. about 80% or more agent (connection) is metabolized before entering the liver (see example test 6), or on the basis of a test of metabolic stability in liver S9 this means that 10 minutes after I tested with S9 human or hamster residual velocity unmodified form is about 20% or less, preferably about 10% or less, more preferably about 8% or less (see example test 7).

The expression "the MTP inhibitor is not essentially inhibits MTP in the liver" has essentially the same meaning as the above expression is "metabolized to a number, in which the remaining MTP inhibitor in the liver essentially did not inhibit MTP in the liver", and means the condition under which the TG-releasing activity of the liver is maintained at about 80% or more, preferably about 90% or more, more preferably 100% of the normal level.

As a "pharmaceutically acceptable carrier" used various organic and inorganic materials-carriers, which are usually used as materials preparative forms and enter the formula as excipients, lubricants, binders, dezintegriruetsja agent, solvent, solubilizer, suspending agent, isotonicity agent, puff the RA, sedative, etc. If desired, you can also use pharmaceutical additives such as preservative, antioxidant, colorant, sweetener, etc. Preferred examples of the specified excipient include lactose, sucrose, D-mannitol, starch, crystalline cellulose, light anhydrous silicic acid, etc. are Preferable examples of the specified lubricants include magnesium stearate, calcium stearate, talc, colloidal silicon dioxide, etc. Preferred examples of the specified coupling agent include crystalline cellulose, sucrose, D-mannitol, dextrin, hydroxypropylcellulose, hypromellose, polyvinylpyrrolidone, etc. Preferred examples of the specified dezintegriruetsja agent include starch, carboxymethylcellulose, calcium carboxymethylcellulose, croscarmellose sodium, carboximetilkrahmal sodium, etc. Preferred examples of the specified solvent include water for injection, alcohol, propylene glycol, macrogol, sesame oil, corn oil, ether of propylene glycol and fatty acid, etc. are Preferable examples of the specified solubilizer include polyethylene glycol, propylene glycol, D-mannitol, benzyl benzoate, ethanol, trilaminate, cholesterol, triethanolamine, sodium carbonate, sodium citrate, etc. Preferred examples indicated the data of a suspending agent include surfactants (e.g., steartrimonium, sodium lauryl sulfate, lauramidopropyl acid, lecithin, sodium chloride benzalconia, chloride benzene, glycerylmonostearate etc), polyvinyl alcohol, polyvinylpyrrolidone, carboxymethylcellulose sodium, methylcellulose, hydroxymethylcellulose, etc. preferred examples of the specified isotonicity agent include sodium chloride, glycerin, D-mannitol, etc. Preferred examples of the specified buffer include phosphate, acetate, carbonate, citrate, etc. Preferred examples of the specified sedative include benzyl alcohol, etc. Preferred examples of the specified preservative include esters of para-oksibenzoynoy acid, chlorbutanol, benzyl alcohol, finitely alcohol, along with dehydroacetic acid, sorbic acid etc. Preferred examples of the specified antioxidant include sulfites, ascorbic acid, etc. are Preferable examples of the specified sweeteners include aspartame, saccharin sodium, stevia, etc.

Preferred examples of these dyes include food dyes such as food yellow No. 5, food red No. 2 and food blue No. 2, replace for food, iron oxide, etc.

The best way of carrying out the invention

Below is a detailed description of the different substituents.

R1preference is sustained fashion represents hydrogen, With1-C6-alkyl, such as methyl, ethyl, etc.; C1-C6-alkoxy, such as methoxy, isopropoxy etc.; halogen, such as fluorine, chlorine, etc.; halogen-C1-C6-alkyl, such as trifluoromethyl, etc.; or (C2-C6alkenyl, such as Isopropenyl etc.

R2preferably represents phenyl (which may be substituted by halogen With1-C6-alkyl, such as trifluoromethyl, etc.; C1-C6-alkyl, such as methyl, ethyl, etc.; halogen, such as fluorine, chlorine, bromine, etc.; C1-C6-alkoxy, such as methoxy, etc.; C1-C6-acyl, such as acetyl, etc.; C2-C6-alkenyl, such as Isopropenyl etc.; or cyano);1-C6-alkyl, such as ethyl, isopropyl, etc.; C3-C7-cycloalkyl, such as cyclohexyl and so on;1-C6-alkoxy, such as butoxy etc.; halogen-C1-C6-alkyl, such as trifluoromethyl, etc.; halogen-C1-C6-alkyloxy, such as triptoreline etc.; C7-C16-aralkyl, such as benzyl, etc.; C6-C14-aryloxy, such as phenoxy (in which the aryl part may be substituted With1-C6-alkyl, such as trifluoromethyl, etc. and so on;7-C15-arylcarbamoyl, such as benzoyl (in which the aryl part may be substituted by halogen, still is as chlorine, etc. and so on; a heterocycle such as thiophene-3-yl and so on;2-C7-alkoxycarbonyl, such as butoxycarbonyl etc.; -N(R40)(R41) (where each of R40and R41independently represents hydrogen or optionally substituted phenyl).

R2'preferably represents hydrogen or halogen, such as chlorine, etc.

R2"preferably represents hydrogen, halogen-C1-C6-alkyl, such as trifluoromethyl, etc.; C1-C6-alkyl, such as methyl, ethyl, etc.; halogen, such as fluorine, chlorine, bromine, etc.; C1-C6-alkoxy, such as methoxy, etc.; C1-C6-acyl, such as methylcarbamyl etc.; C2-C6alkenyl, such as Isopropenyl etc.; or cyano.

Ring And preferably represents

among which phenyl is especially preferred.

X preferably represents-COO-, -N(R10)CO -, or-CON(R10) (where R10represents hydrogen; C1-C6-alkyl, such as methyl, isopropyl, etc.; or (C3-C7-cycloalkyl, such as cyclohexyl and so on), among which-COO - or-CONH - are especially preferred.

The ring preferably is a

or more preferably

or most preferably

R3preferably represents hydrogen; hydroxy; halogen, such as chlorine, bromine, etc.; C1-C6-alkyl, such as methyl, ethyl, isopropyl, isobutyl, etc.; substituted C1-C6-alkyl, such as isobutyl, substituted hydroxy, etc.; C1-C6-alkoxy, such as methoxy, ethoxy, propoxy, isopropoxy etc.; halogen-C1-C6-alkyl, such as trifluoromethyl, etc.; C7-C16-aralkylated, such as benzyloxy, etc.; C1-C6-acyl such as formyl, etc.; optionally substituted heterocycle such as 4-methylthiazole-2-yl, etc.; -CON(R11)(R12) (where each of R11and R12independently represents hydrogen; C1-C6-alkyl, such as methyl, ethyl, propyl, isopropyl, etc.; C6-C14-aryl, such as phenyl and so on;7-C16-aralkyl, such as benzyl, etc.; C1-C6-alkoxy, such as methoxy, etc.; or R11and R12taken together with the nitrogen can form

(where p is an integer from 0 to 1); -N(R13)(R14or-CH2-N(R13)(R14) (where each of R13and R14independently represents hydrogen; C1-C6-alkyl, such as methyl, ethyl, etc.; 2-C7-alkoxycarbonyl, such as methoxycarbonyl etc.; C1-C6-acyl, such as acetyl, etc.; or R13and R14taken together with the nitrogen can form

(where R has the same meaning as defined above); or,- COR15(where R15represents a C1-C6-alkyl, such as isopropyl, etc.; C1-C6-alkoxy, such as methoxy, ethoxy, propoxy, isopropoxy etc.; C7-C16-Allakaket, such as benzyloxy, etc.; or hydroxy). Alternative, R3and R10can be taken together with the nitrogen atom that is attached to R10and ring In education

R4preferably represents hydrogen or halogen, such as fluorine, chlorine, bromine, etc.

Alk1preferably represents methylene or ethane-1,1-diyl.

l preferably represents 0, 1 or 2.

Alk2preferably represents methylene.

m preferably represents 0 or an integer from 1 to 3.

D preferably represents a C1-C6-alkyl, such as ethyl, propyl, isopropyl, butyl, isobutyl, sec-butyl, sec-pentyl etc.; C2-C6alkenyl, such as n-propanol etc.; C2-C7-alkoxycarbonyl, such as ethoxycarbonyl and so on; -N(R42)-COR43(where R42represents hydrogen or C1-C6-alkyl; R43represents a C6-C14-aryl, such as biphenyl, etc.; or (C7-C16-aralkyl); or a group represented by the below formula:

(where each of the rings, R5, R6and R7has the same meaning as defined above).

The ring preferably is a C6-C14-aryl, such as phenyl, naphthyl and so on;3-C7-cycloalkyl, such as cyclopentyl, cyclohexyl and so on;7-C16-aralkyl, such as benzyl, etc.; or a heterocycle, such as pyridine-3-yl, thiophene-3-yl, thiazol-2-yl etc. Alternative, the ring, taken together with R7and R8may form

R5preferably represents hydrogen; C1-C6-alkyl, such as methyl, etc.; C1-C6-alkoxy, such as methoxy, etc.; halogen, such as chlorine, etc.; nitro; amino; C6-C14-aryl, such as phenyl and so on; or-CON(R16)(R17or-CH2-CON(R16)(R17) (where each of R16and R17independently represents hydrogen; C1-C6-alkyl, such as ethyl, etc. or halogen-C1-C6-alkyl, such as 2,2,2-triptorelin etc).

R6predpochtitel is but represents hydrogen or halogen, such as chlorine, etc.

R7preferably represents hydrogen.

Preferably, each of R8and R9independently represents hydrogen, C1-C6-alkyl, such as ethyl and so on;6-C14-aryl, such as phenyl, etc.; hydroxy-C1-C6-alkyl, such as hydroxymethyl, etc.; -CON(R18)(R19) (where each of R18and R19independently represents hydrogen; C1-C6-alkyl, such as methyl, ethyl, propyl, isopropyl, butyl, isobutyl, etc.; C3-C7-cycloalkyl, such as cyclohexyl, etc.; halogen-C1-C6-alkyl, such as 2,2,2-triptorelin etc.; C2-C12-alkoxyalkyl, such as methoxyethyl etc.; or (C6-C14-aryl, such as phenyl and so on); -COOR20or -(CH2)n-OCO(R20) (where R20represents hydrogen; C1-C6-alkyl, such as methyl, ethyl, propyl, isopropyl, isobutyl, etc.; or (C3-C7-cycloalkyl, such as cyclohexyl, etc. and n is an integer equal to 0 or 1); -N(R21)(R22) (where each of R21and R22independently represents hydrogen, C1-C6-alkyl, such as methyl, isopropyl, etc.; C1-C6-acyl, such as acetyl, propionyl, butyryl etc.; C1-C6-alkylsulfonyl, such as methylsulphonyl and so what.; or R21and R22taken together with the nitrogen atom to which they are attached, may form

or R8and R9taken together, may form With3-C7-cycloalkyl, such as cyclopropyl, cyclohexyl, etc.

Preferred variants of the embodiment of deputies and designated replacement will be illustrated below.

R1preferably represents hydrogen, halogen-C1-C6-alkyl or C1-C6-alkyl, among which hydrogen is especially preferred.

R2preferably represents phenyl (which may be substituted by halogen With1-C6-alkyl, such as trifluoromethyl, etc.; C1-C6-alkyl, such as methyl, etc.; halogen, such as chlorine, etc.; or (C1-C6-alkoxy, such as methoxy and so on).

R2'preferably represents hydrogen.

R2"preferably represents hydrogen, halogen-C1-C6-alkyl, halogen, C1-C6-alkyl or C1-C6-alkoxy, and trifluoromethyl is particularly preferred.

X preferably represents-COO - or-CON(R10)- (R10has the same meaning as defined above), among which the-CONH - is especially preferred.

Ring In predpochtite is correctly represents phenyl.

R3preferably represents C1-C6-alkyl, C1-C6-alkoxy, -CON(R11)(R12) (where preferably each of R11and R12represents hydrogen or C1-C6-alkyl), or-COR15(where R15preferably represents C1-C6-alkoxy).

R3preferably represents hydrogen or methyl and, particularly preferably, methyl.

Alk1preferably represents methylene.

Alk2preferably represents methylene.

l is preferably 0 or 1, especially 1.

m is preferably equal to 1 or 2, especially 1 or 2.

D preferably represents a C1-C6-alkyl or a group represented by the following formula:

(where each of the rings, R5, R6and R7has the same meaning as defined above).

The ring preferably is a phenyl, pyridine-3-yl, thiophene-3-yl, thiophene-2-yl and thiazol-2-yl, among which phenyl is especially preferred.

Each of R5, R6and R7preferably represents hydrogen, halogen or1-C6-alkyl, among which hydrogen is especially preferred.

R8and R9each preferably represents bodoro is, With1-C6-alkyl, C6-C14-aryl, -CON(R18)(R19) (where each of R18and R19preferably represents hydrogen or C1-C6-alkyl) or -- COO(R20) (where R20preferably represents hydrogen or C1-C6-alkyl), among which-CON(R18)(R19) (where each of R18and R19preferably represents hydrogen or C1-C6-alkyl) or -- COO(R20) (where R20preferably represents hydrogen or C1-C6-alkyl) are more preferred, and-COO(R20) (where R20preferably represents C1-C6-alkyl) is particularly preferred.

Place the replacement by the group -(CH2)l- the benzene ring in the formula (1') is preferably an i-position.

Compounds of the present invention may include a hydrate or solvate, as the case may be, and may additionally include their metabolites. In addition, the compounds of the present invention include the racemates and optically active compounds. Optically active compounds preferred are such compounds where one of the enantiomers is in enantiomeric excess of about 90% or higher, more preferably in an enantiomeric excess of about 99% or above.

When the compounds of the present invention is used as an agent for the treatment or prophylaxis of hyperlipidemia or arteriosclerosis, they can be administered systemically or locally and orally or parenterally. Although the dose may vary depending on age, body weight, symptoms, therapeutic activities, and so on, the daily dose for an adult is in the range from 0.1 mg to 1 g per dose, which you can enter from one to several times a day. Also compounds of the present invention can introduce people and animals are different from humans, in particular a mammal, for the treatment or prophylaxis of these diseases. Compounds of the present invention can be used in the same way, for the treatment or prevention of coronary artery disease, obesity, diabetes or hypertension.

In the manufacture of formulations of the compounds of the present invention into the corresponding solid compositions and liquid compositions for oral administration or in compositions for injection, etc. for parenteral administration may be added suitable adjuvants such as diluents, dispersing agents, adsorbents, soljubilizatory etc. in Addition, the compositions of the present invention may be a known form, such as tablets, sawing and, powders, granules, suppositories, injectable preparations, eye drops, solutions, capsules, lozenges, aerosols, elixirs, suspensions, emulsions, syrups, etc.

When the compounds of the present invention is introduced into the composition of solid preparations such as tablets, pills, powders, granules, etc. are examples of such additives include lactose, mannitol, glucose, hydroxypropylcellulose, microcrystalline cellulose, starch, polyvinylpyrrolidone, alumosilicate magnesium or powdered silicic acid anhydride. In the case where the compounds of the present invention receive in the form of tablets or pills, they can be covered with a film cover, soluble in the stomach, or intersolubility film-coated, containing such substance such as sucrose, gelatin, hydroxypropylcellulose or phthalate of hydroxymethylcellulose. In addition, tablets or pills may be a multilayer tablet comprising two or more layers.

Illustrative examples of pharmaceutical compositions according to the present invention are also capsules that are filled with liquid, semi-solid or solid content, obtained by dissolving the compounds of the present invention in a solvent and added to a solution of auxiliary additives. Examples of these solvents are water, ethanol, flora is the second oil etc, among them, preferably used are ethanol, or a mixture of purified water and ethanol. Any adjuvants which are usually used to obtain the capsules can be used without any specific limitations. Such additives include, for example, esters of propylene glycol and fatty acids; low molecular weight glycols such as polyethylene glycol 200-600, and so on; esters of glycerol and fatty acids and triglycerides of fatty acids with medium chain length; alcohols/polyols, such as stearyl alcohol, cetanol, polyethylene glycol, etc. or their esters; fats such as sesame oil, soybean oil, peanut oil, corn oil, gidrirovannoe oil, paraffin oil, bleached wax; fatty acids, such as triethylcitrate, triacetin, stearic acid, palmitic acid, myristic acid, etc. and their derivatives. Such auxiliary additives are suitable for the production of liquid or semi-solid contents. Capsules of the present invention is preferable as such auxiliary additives are esters of propylene glycol and fatty acids. Examples : esters of propylene glycol and fatty acids are propilenglikolmonostearata (Capmul PG-8 (trade mark), Sefol 218 (trade mark), Capryo 190 (trade mark)), impregnated englishliterature (Lauroglycol FCC (trade mark)), propilenglikolmonostearata (Myverol P-06 (trade mark)), propilenglikolstearat, propilenglikolmonostearata, propilenglikolstearat (Propymuls (trade mark)), propilenglikolstearat/dicaprate (Captex (trade mark) 200 (trade name), propilenglikolstearat, propilenglikolstearat and propilenglikolmonostearata (Captex (trade mark) 800 (trade name)). Although there are no specific limitations to the material constituting the capsule of the present invention, they include, for example, polysaccharides derived from natural products, such as agar, alginic acid salts, starch, xanthan gum, dextrin, etc.; proteins such as gelatin, casein, etc.; chemically processed foods, such as hydroxyacyl, pullulan, hydroxypropylcellulose, hypromellose, polyvinyl alcohol or its derivatives, polyacrylic derivatives, polyvinylpyrrolidone or its derivatives, polyethylene glycol, etc.

In that case, when the pharmaceutical compositions of the present invention are liquid formulation for oral administration, such as pharmaceutically acceptable emulsions, soljubilizatory, suspensions, syrups or elixirs, etc. used diluents include, for example, purified water, ethanol, vegetable oils, emulsifiers, etc. In addition to this RA is basicaly to the above preparative liquid formulations can be added auxiliary agents, such as wetting agents, suspendresume agents, sweeteners, flavoring seasonings, flavorings or preservatives.

In that case, when the pharmaceutical compositions of the present invention are parenteral formulation, such as injectable preparations are sterilized aqueous and non-aqueous solutions, solubilization, suspendresume agents, emulsifiers, etc. are Examples of the aqueous solutions of solubilization and suspendida agents include distilled water for injection, saline solution, cyclodextrin and its derivatives; organic amines such as triethanolamine, diethanolamine, monoethanolamine, triethylamine, etc. and inorganic alkaline solutions. When using aqueous solutions, may be optionally added to the propylene glycol or vegetable oils, such as olive oil, or alcohols, such as ethanol. Additionally, as a solubilizer can be used surfactants (for the formation of mixed micelles), such as polyoxyethylene hydrogenated castor oil, esters of sucrose and fatty acids or lecithin or hydrogenated lecithin (for the formation of liposomes). In addition, as for parenteral preparative forms of the present invention, they can be obtained in the de emulsions, including nonaqueous soljubilizatory, such as vegetable oil with lecithin, polyoxyethylene gidrirovannoe castor oil or polyoxyethylene-polyoxypropylene glycol, etc.

In addition, the present invention relates to a new agent for the treatment or prophylaxis of hyperlipidemia, arteriosclerosis, coronary artery disease, obesity, diabetes or hypertension with new features that previously were not known. The agents according to the present invention for the treatment or prophylaxis of these diseases are different in that they selectively inhibit MTP (microsomal protein transfer triglycerides) in the small intestine. Among such agents is desirable agent, which essentially did not inhibit MTP in the liver, inhibiting only MTP in the small intestine. Specifically, it is preferable that the inhibition of MTP agent in the liver was approximately 1/3 or less, preferably 1/100 or less, when compared with such option to the small intestine when assessing translated into ED50or ED20. With regard to one preferred variant implementation of therapeutic or prophylactic agents of the present invention for these diseases, they inhibit MTP in the small intestine, and then they are metabolized in the small intestine, liver and blood is of such quantity, when the residual agent appearing in the liver, is not essentially inhibits MTP in the liver. Especially preferably by oral administration of 300 mg/kg of the compounds of the present invention the percentage of inhibition reaching the liver residual connection release TG in the liver was approximately 20% or less, preferably less than about 10%, more preferably about 0. Specifically, it is desirable that the agent showed percentage inhibition of the release of TG in the liver at the level of 40% or less, preferably about 20% or less, in the analysis using the method described in example test 4, which will be described next.

Pharmaceutical compositions or agents of the present invention can be used in combination with other pharmaceutical compositions or agents. As other agents can be illustrated by the medicinal product for the treatment or prophylaxis of hyperlipidemia, arteriosclerosis, coronary artery disease, obesity, diabetes or hypertension, and can be used individually or in combination of two or more kinds of these medicines. Examples of the antihyperlipidemic drugs include medicines Statesboro type, more specifically lovastatin, simvastatin, pravastatin, fluvastatin is, atorvastatin or tseriwastatina. Examples of drugs anti-obesity include musical or olistat. Examples of antidiabetic drugs include insulin preparations, medicines on the basis of sulfonylureas, which stimulate the production of insulin medicines sulfonamidnuyu medicines biguanide drugs, inhibitors α-glucosidase and improves insulin resistance drugs, etc. and, more specifically, insulin, glibenclamide, tolbutamide, glyclopyramide, acetohexamide, glimepiride, tolazamide, gliclazide, nateglinide, glybuzole, Metformin hydrochloride, the hydrochloride of buformin, voglibose, acarbose and pioglitazone hydrochloride etc. are Examples of antihypertensive drugs include loop diuretics, inhibitors of angiotensin-converting enzyme, receptor antagonists angiotensin II, calcium antagonists, β-blockers, α,β-blockers and α-blockers, and, more specifically, furosemide delayed release, captopril, captopril sustained-release, enalapril maleate, alacepril, delapril hydrochloride, cilazapril, lisinopril, benazepril hydrochloride, imidapril hydrochloride, temocapril hydrochloride, inapril hydrochloride, trandolapril, perindopril erbumine, losartan potassium, kandisa the tan cilexetil, nicardipine hydrochloride, nicardipine hydrochloride sustained release, nilvadipine, nifedipine, nifedipine slow release, benidipine hydrochloride, diltiazem hydrochloride, diltiazem hydrochloride sustained release, nisoldipine, nitrendipin, manidipine hydrochloride, barnidipine hydrochloride, efonidipine hydrochloride, amlodipine, besylate, felodipine, cilnidipine, aranidipine, propranolol hydrochloride, propranolol hydrochloride sustained-release, pindolol, pindolol slow release, indenolol hydrochloride, carteolol hydrochloride, carteolol hydrochloride sustained release, bunitrolol hydrochloride, bunitrolol hydrochloride sustained release, atenolol, acebutolol hydrochloride, metoprolol tartrate, metoprolol tartrate sustained release, nipradilol, penbutolol sulfate, tilisolol hydrochloride, carvedilol, bisoprolol fumarate, betaxolol hydrochloride, celiprolol hydrochloride, bopindolol malonate, bevantolol hydrochloride, labetalol hydrochloride, arotinolol hydrochloride, amosulalol hydrochloride, prazosin hydrochloride, terazosin hydrochloride, doxazosin mesilate, bunazosin hydrochloride, bunazosin hydrochloride sustained release, urapidil and phentolamine mesilate, etc.

There are no specific limitations to the timing in which edenia pharmaceutical compositions or agents and other drugs for combined application in accordance with the present invention, and they can be administered simultaneously or alternately.

The number of such drugs for the combined application can be determined on the basis of their clinical dosages and may be selected depending on age, weight, condition, treatment time, preparative dosage form, route of administration, combination type, etc. there are No special restrictions for preparative dosage forms of medicines for the combined application, and may be enough to pharmaceutical compositions or agents and other drugs for combined application in accordance with the present invention were United during the injection.

Following example will illustrate the methods of obtaining the ester compound represented by formula (1), but the method of the present invention is not restricted by them. In the following way D is a group of formula (2):

(where each of the rings, R5, R6and R7has the same meaning as defined above), and when D represents C1-C6-alkyl, C2-C6alkenyl,2-C7-alkoxycarbonyl or-N(R42)-CO(R43) (each of R42and R43has the same meaning as defined above), the connection can be is obtained similarly.

In addition, functional groups, other than those that will interact, can be optionally protected on the previous stage, and the protection can be removed at an appropriate stage.

In addition, the reaction at each stage can be performed in the usual way, and separation and purification can be performed using the appropriate selection or combination of conventional methods such as crystallization, recrystallization, column chromatography, preparative HPLC, etc.

Method 1

Among the compounds represented by formula (1)below is illustrated the method of producing compounds in which X represents-CONH(CH2)n-.

Method 1

In the above reaction scheme, each of R1, R2, R3, R4, R5, R6, R7, R8, R9, l, m, n, Alk1, Alk2, ring A, ring b and ring C has the same meaning as defined above, and R23represents a C1-C6-alkyl.

Stage 1-1

Carboxylic acid of the formula (2) reacts with oxalylamino or chloride tiomila in the solvent, giving the acid chloride of the acid of formula (3).

The solvent used in this reaction includes, for example, ethers such as diethyl ether, tetrahydrofuran, dioxane, 1,2-dimethoxyethane,diglyme etc; hydrocarbons, such as benzene, toluene, hexane, xylene and so on; halogenated hydrocarbons such as methylene chloride, chloroform, carbon tetrachloride, 1,2-dichloroethane, etc.; and esters such as ethyl acetate, methyl acetate, butyl acetate and so on; and they can be used individually or in combination. Preferred solvents used in this reaction include methylene chloride, chloroform or toluene, each of which contains a catalytic amount of N,N-dimethylformamide.

The reaction temperature is about -20°to 120°C, preferably from approximately 0°C to room temperature.

The reaction time is from about 10 minutes to 8 hours, preferably from about 30 minutes to 4 hours.

Stage 1-2

This stage is a normal restore of the nitro group attached directly to aromatic ring. Nitrosoaniline formula (4) hydronaut in a solvent in the presence of a catalyst, to obtain the compounds of formula (5).

The solvent used in this reaction includes, for example, ethers such as tetrahydrofuran, dioxane, 1,2-dimethoxyethane, and so on; alcohols such as methanol, ethanol, isopropyl alcohol, tert-butanol, etc.; and esters such as ethyl acetate, methyl acetate, butyl acetate and so on; and they can use the with separately or in combination. Preferred solvents used in this reaction include alcohols such as methanol, ethanol, isopropyl alcohol, tert-butanol, etc.; and a mixture of specified alcoholic solvent and tetrahydrofuran and/or water.

The catalyst used in the reaction includes, for example, palladium-on-carbon, palladium hydroxide, Raney Nickel, platinum oxide, among which palladium-on-carbon or reduced iron are preferred.

The reaction temperature is from approximately 0°to 120°C, preferably from about room temperature to 100°C.

The reaction time is from about 30 minutes to 8 hours, preferably from about 1 hour to 96 hours.

Stage 1-3

This stage is a conventional condensation reaction between anhydrides of acids and amines. The acid chloride of the acid of formula (3) is condensed with an amine of formula (5) in a solvent in the presence of a base, receiving the compound of formula (6).

The solvent used in the reaction includes, for example, ethers such as diethyl ether, tetrahydrofuran, dioxane, 1,2-dimethoxyethane, diglyme, etc.; hydrocarbons, such as benzene, toluene, hexane, xylene and so on; halogenated hydrocarbons such as methylene chloride, chloroform, carbon tetrachloride, 1,2-dichloroethane, etc.; and esters such as this is latitat, methyl acetate, butyl acetate and so on; and they can be used individually or in combination. Preferred solvents used in this reaction include methylene chloride, chloroform, toluene, ethyl acetate or tetrahydrofuran.

Examples of bases used in the present invention include organic bases such as triethylamine, pyridine, N-methylmorpholine etc.; hydroxides of alkali metals such as lithium hydroxide, sodium hydroxide, potassium hydroxide, etc; and carbonates of alkali metals such as sodium carbonate, potassium carbonate, sodium bicarbonate, potassium bicarbonate, etc.; among which triethylamine, sodium hydroxide or sodium bicarbonate are preferred.

The reaction temperature is from approximately 0°C to 80°C, preferably from approximately 0°C to room temperature.

The reaction time is from about 10 minutes to 48 hours, preferably from about 30 minutes to 24 hours.

In the case of the compounds of formula (5), where R23represents hydrogen, the compound of formula (7) can be obtained by condensation in a single phase between aminocarbonyl acid and acid chloride of acid (reaction Schotten's-Bauman).

Alternatively, the compound of formula (6) can be obtained using a condensing agent (for example, WSC-HOBT, DCC-HOBT) for compounds of formula 2 and the compound of formula (5). In addition, the compound of formula (6) can be obtained by transformation of a compound of the formula (2) in its mixed andrid followed by reaction in the presence of a base.

Stage 1-4

This stage represents the overall hydrolysis reaction of ester with the use of alkali. The compound of formula (6) hydrolyzing in a solvent in the presence of a base, receiving the compound of formula (7).

The solvent used in this reaction includes, for example, ethers such as diethyl ether, tetrahydrofuran, dioxane, 1,2-dimethoxyethane, diglyme etc; and alcohols, such as methanol, ethanol, isopropyl alcohol, etc; and can be used separately or in combination. Preferred solvents in the present reaction include a mixture of tetrahydrofuran and ethanol or methanol. Examples of bases are aqueous solutions of carbonates of alkali metals such as sodium carbonate, potassium carbonate, etc. or aqueous solutions of hydroxides of alkali metals such as lithium hydroxide, sodium hydroxide, potassium hydroxide and so on, among which sodium hydroxide or lithium hydroxide are preferred.

The reaction temperature is from approximately 0°to 120°C, preferably from about room temperature up to 80°C.

The reaction time is from about 1 hour to 24 hours, preferably approx the RNO from 2.5 hours to 12 hours.

Stage 1-5

This stage is a conventional condensation reaction of carboxylic acid with alcohol.

Carboxylic acid of the formula (7) condense with alcohol of the formula (8) in a solvent in the presence of a base and a condensing agent, receiving the compound of formula (1-1), which is one of the target compounds.

The solvent used in the reaction includes, for example, ethers such as diethyl ether, tetrahydrofuran, dioxane, 1,2-dimethoxyethane, diglyme, etc.; hydrocarbons, such as benzene, toluene, hexane, xylene and so on; halogenated hydrocarbons such as methylene chloride, chloroform, carbon tetrachloride, 1,2-dichloroethane and so on; esters such as ethyl acetate, methyl acetate, butyl acetate, etc.; polar solvents such as acetone, N,N-dimethylformamide, dimethyl sulfoxide and so on; and they can be used individually or in combination. Preferred solvents used in this reaction include tetrahydrofuran, acetone, methylene chloride or N,N-dimethylformamide.

Examples of the bases used in this reaction include organic bases such as triethylamine, pyridine, dimethylaminopyridine, N-methylmorpholine and so on, among which dimethylaminopyridine is preferred.

Examples of the condensing agent used in this reaction, including the Ute hydrochloride of 1-ethyl-3-(3'-dimethylaminopropyl)carbodiimide (WSC• HCl), dicyclohexylcarbodimide (DCC) and so on, among which the hydrochloride of 1-ethyl-3-(3'-dimethylaminopropyl)carbodiimide is preferred.

The reaction temperature is from approximately 0°C to 80°C, preferably from approximately 0°C to room temperature.

The reaction time is from about 1 hour to 48 hours, preferably from about 3 hours to 24 hours.

As an alternative way of carboxylic acid of the formula (7) can be converted to its mixed anhydride, and then subjected to interaction with alcohol of the formula (8) in the presence of a base.

Method 1A

Method 1A, as shown below, is an alternative to method 1.

Method 1A

In the above reaction scheme, each of R1, R2, R3, R4, R5, R6, R7, R8, R9, R23, l, m, n, Alk1, Alk2, ring A, ring b and ring C has the same meaning as defined above.

Stage 1A-1

The compound of the formula (105) can be obtained from compounds of formula (4) in a manner analogous to stages 1-4 method 1.

Stage 1A-2

The compound of formula (106) can be obtained by condensation of the carboxylic acid of the formula (105) with an alcohol of the formula (8) in a manner analogous to stages 1-5 method 1.

Stage 1A-3

The compound of formula (107) can be obtained from the soedineniya formula (106), similar stages 1-2 of method 1.

Stage 1A-4

The compound of formula (1-1), which represents one of the compounds which are the object of the invention may be obtained by condensation of an amine of the formula (107) with the acid chloride of the acid of formula (3) in a manner analogous to stages 1-3 method 1.

Method 2

Among the compounds represented by formula (1)below is illustrated the method of producing compounds in which X represents-COO-(CH2)n-.

Method 2

In the above reaction scheme, each of R1, R2, R3, R4, R5, R6, R7, R8, R9, l, m, n, Alk1, Alk2, ring A, ring b and ring C has the same meaning as defined above, and R24represents a protective group of hydroxyl (for example, benzyl, p-methoxybenzyl, tert-butyl, trialkylsilyl etc).

Stage 2-1

This stage represents the condensation reaction of carboxylic acid with alcohol, similar to stages 1-5 of method 1. The compound of formula (10) can be obtained by condensation of the carboxylic acid of formula (9) with an alcohol of the formula (8) in a solvent in the presence of a base and a condensing agent.

The solvent used in the reaction includes, for example, ethers such as diethyl ether, tetrahydrofuran, dioxane, 2-dimethoxyethane, diglyme, etc.; hydrocarbons, such as benzene, toluene, hexane, xylene and so on; halogenated hydrocarbons such as methylene chloride, chloroform, carbon tetrachloride, 1,2-dichloroethane and so on; esters such as ethyl acetate, methyl acetate, butyl acetate, etc.; polar solvents such as acetone, N,N-dimethylformamide, dimethylsulfoxide, water and so on; and they can be used individually or in combination. Preferred solvents used in this reaction include tetrahydrofuran, methylene chloride or N,N-dimethylformamide.

Examples of the bases used in this reaction include organic bases such as triethylamine, pyridine, dimethylaminopyridine, N-methylmorpholine and so on, among which dimethylaminopyridine is preferred.

Examples of the condensing agent used in this reaction include hydrochloride, 1-ethyl-3-(3'-dimethylaminopropyl)carbodiimide (WSC•HCl), dicyclohexylcarbodimide (DCC) and so on, among which the hydrochloride of 1-ethyl-3-(3'-dimethylaminopropyl)carbodiimide is preferred.

The reaction temperature is from approximately 0°C to 80°C, preferably from approximately 0°C to room temperature.

The reaction time is from about 2 hours to 48 hours, preferably from about 6 hours to 24 hours.

Stage 2-2

This stage p is ecstasy a common way to remove protection for the hydroxyl groups. For example, when R24represents benzyl in the compound of formula (10), the compound of formula (10) hydronaut in a solvent in the presence of a catalyst, obtaining the compound of formula (11).

The solvent used in this reaction includes, for example, ethers such as tetrahydrofuran, dioxane, 1,2-dimethoxyethane, diglyme and so on; alcohols such as methanol, ethanol, isopropyl alcohol, tert-butanol, etc.; and esters such as ethyl acetate, methyl acetate, butyl acetate and so on; and they can be used individually or in combination. Preferred solvents used in this reaction include alcohols such as methanol, ethanol, isopropyl alcohol, tert-butanol, etc.

Examples of the catalyst used in the reaction include, for example, palladium-on-carbon, palladium hydroxide, Raney Nickel, platinum oxide, among which palladium-on-carbon are preferred.

The reaction temperature is from approximately 0°C to 80°C, preferably from approximately 0°C to room temperature.

The reaction time is from about 1 hour to 16 hours, preferably from about 2 hours to 8 hours.

Stage 2-3

This stage represents the condensation reaction of carboxylic acid with alcohol, similar to stages 1-5 of method 1. The compound of the formula (11) condense with alcohol Faure the uly (2) in a solvent in the presence of a base and a condensing agent, receiving the compound of formula (1-2), which represents one of the target compounds.

The solvent used in the reaction includes, for example, ethers such as diethyl ether, tetrahydrofuran, dioxane, 1,2-dimethoxyethane, diglyme, etc.; hydrocarbons, such as benzene, toluene, hexane, xylene and so on; halogenated hydrocarbons such as methylene chloride, chloroform, carbon tetrachloride, 1,2-dichloroethane and so on; esters such as ethyl acetate, methyl acetate, butyl acetate, etc.; and polar solvents such as acetone, N,N-dimethylformamide, dimethylsulfoxide, etc; and you can use them separately or in combination. Preferred solvents for this reaction are tetrahydrofuran, methylene chloride, dimethylformamide, etc.

Examples of the bases used in this reaction include organic bases such as triethylamine, pyridine, dimethylaminopyridine, N-methylmorpholine and so on, among which dimethylaminopyridine is preferred.

Examples of the condensing agent used in this reaction include hydrochloride, 1-ethyl-3-(3'-dimethylaminopropyl)carbodiimide (WSC•HCl), dicyclohexylcarbodimide (DCC) and so on, among which the hydrochloride of 1-ethyl-3-(3'-dimethylaminopropyl)carbodiimide is preferred.

The reaction temperature is primer is from 0° With up to 80°C, preferably from approximately 0°C to room temperature.

The reaction time is from about 2 hours to 48 hours, preferably from about 6 hours to 24 hours.

As an alternative method 2, the phenol or alcohol derivative obtained from the compounds of formula (9) (where R24represents the p-methoxybenzyl and the carboxyl group is protected benzyl ester group), remove the p-methoxybenzyloxy group using 2,3-dichloro-5,6-dicyanobenzoquinone (DDQ) and so on, followed by condensation with the compound of the formula (2). After removal of the benzyl group of the compounds obtained unprotected compound condensed with the compound of the formula (8), obtaining the compound of formula (1-2), which is one of the objects of the invention.

Method And

Below is an example of the method of obtaining the compounds of formula (1), where the ring is a

(where R4has the same meaning as defined above, R31represents a C1-C6-alkyl, and l' is 1).

Method And

In the above reaction scheme, each of R31and R4has the same meaning as defined above, R25represents a C1-C6alkyl, each X2and X3the present is the focus of a halogen, and Et represents ethyl.

Stage a-1

The compound of formula (14) can be obtained by the coupling of compounds of formula (12) with an ester of malonic acid of the formula (13) in a solvent in the presence of a base.

The solvent used in this reaction includes, for example, ethers such as diethyl ether, tetrahydrofuran, dioxane, 1,2-dimethoxyethane, diglyme, etc.; hydrocarbons, such as benzene, toluene, hexane, xylene and so on; alcohols such as methanol, ethanol, isopropyl alcohol, tert-butanol, etc.; and polar solvents such as N,N-dimethylformamide, dimethyl sulfoxide and so on; and they can be used individually or in combination. The preferred solvent for this reaction is N,N-dimethylformamide.

Examples of bases used in the reaction include hydrides of alkali metals, such as sodium hydride, potassium hydride, etc.; alkoxides of alkali metals, such as ethoxide sodium, sodium methoxide, tert-piperonyl potassium and so on; amides of alkali metals such as sodium amide, bestremembered lithium, etc.; and carbonates of alkali metals such as sodium carbonate, potassium carbonate and so on, among which sodium hydride is preferred.

The reaction temperature is from approximately 0°to 120°C, preferably from about room temperature to 100°C.

Time the I reaction is from about 30 minutes to 24 hours, preferably from about 1 hour to 12 hours.

Stage a-2

This stage represents the reaction of hydrolysis of complex ester followed by decarboxylation. The compound of formula (15) can be obtained by mixing the compounds of formula (14) by heating in a solvent in the presence of a base.

The solvent used in this reaction includes, for example, ethers such as diethyl ether, tetrahydrofuran, dioxane, 1,2-dimethoxyethane, diglyme and so on; alcohols such as methanol, ethanol, isopropyl alcohol, tert-butanol, etc.; and water, and can be used separately or in combination. Preferred solvents for this reaction are a mixture of alcohol and water.

Examples of bases used in the reaction include carbonates of alkali metals such as sodium carbonate, potassium carbonate, etc. and hydroxides of alkali metals such as lithium hydroxide, sodium hydroxide, potassium hydroxide, etc., among which sodium hydroxide or potassium hydroxide are preferred.

The reaction temperature is from approximately 0°to 150°C, preferably from about 60°to 120°C.

The reaction time is from about 10 minutes to 12 hours, preferably from about 30 minutes to 6 hours.

In accordance with the stages 1A-2, 1A-3 and 1A-4 method 1A connection this is subramania can be obtained from compounds of formula (15), obtained in the above stage a-2.

Below is illustrated an example of a case where Alk1represents a branched alcander or alcander.

Stage a-3

The compound of formula (17) can be obtained by the coupling of compounds of formula (14) with the compound of the formula (16) in a solvent in the presence of a base.

The solvent used in this reaction includes, for example, ethers such as diethyl ether, tetrahydrofuran, dioxane, 1,2-dimethoxyethane, diglyme, etc.; hydrocarbons, such as benzene, toluene, hexane, xylene and so on; alcohols such as methanol, ethanol, isopropyl alcohol, tert-butanol, etc.; and polar solvents such as N,N-dimethylformamide, dimethyl sulfoxide and so on; and they can be used individually or in combination. The preferred solvent for this reaction is N,N-dimethylformamide, etc.

Examples of bases used in the reaction include hydrides of alkali metals, such as sodium hydride, potassium hydride, etc.; alkoxides of alkali metals, such as ethoxide sodium, sodium methoxide, tert-piperonyl potassium, etc.; carbonates of alkali metals such as sodium carbonate, potassium carbonate, sodium bicarbonate, potassium bicarbonate, etc.; hydroxides of alkali metals such as lithium hydroxide, sodium hydroxide, potassium hydroxide, etc.; carboxylates of shelo the different metals, such as sodium acetate, potassium acetate, etc.; phosphates of alkali metals such as sodium phosphate, potassium phosphate, etc. among which sodium hydride is preferred.

The reaction temperature is from approximately 0°to 120°C, preferably from about room temperature to 100°C.

The reaction time is from about 10 minutes to 24 hours, preferably from about 30 minutes to 12 hours.

Stage a-4

In a manner analogous to stages a-2, a compound of formula (18) can be obtained from compounds of formula (17).

In accordance with the stages 1A-2, 1A-3 and 1A-4 method 1A compounds of the present invention can be obtained from compounds of formula (18)obtained in the above stage a-4.

Method In

Below is an example of the method of obtaining the compounds of formula (1), where the ring is a

(where each of R3and R4has the same meaning as defined above, and l is 2 or 3).

Method In

In the case of l=2

In the case of l=3

In the above reaction scheme, each of R3and R4has the same meaning as defined above, Me represents methyl, and Bn is benzyl.

Stage-1

The compound of formula (20) can be obtained cooperation is the interaction of the compounds of formula (19) with brainwashin agent in a solvent in the presence of a radical initiator (for example, 2,2'-azobisisobutyronitrile or benzoyl peroxide).

The solvent used in this reaction includes, for example, hydrocarbons, such as benzene, etc. and halogenated hydrocarbons such as methylene chloride, chloroform, carbon tetrachloride, 1,2-dichloroethane, etc., and can be used separately or in combination. The preferred solvent for this reaction is methylene chloride or carbon tetrachloride.

Pomeroyi agent used in this reaction includes, for example, bromine, N-bromosuccinimide, and so on, among which N-bromosuccinimide is preferred.

The reaction temperature is from about room temperature to 120°C, preferably from about 60°to 100°C.

The reaction time is from about 10 minutes to 8 hours, preferably from about 30 minutes to 4 hours.

Stage-2

Similarly, stage a-1 of method a compound of formula (22) can be obtained by the coupling of compounds of formula (20) with the compound of the formula (21).

Stage B-2'

Similarly, stage a-1 of method a compound of formula (22') can be obtained by the coupling of compounds of formula (20') (obtained from the compounds of formula (15) and the compounds of formula (22) in several stages) with the compound of the formula (21).

Stage-3

The compound of formula (23) can be obtained Hider is of the compounds of formula (22) to dibenzylamine in a solvent with subsequent decarboxylation.

The solvent used in this reaction includes, for example, ethers such as diethyl ether, tetrahydrofuran, dioxane, 1,2-dimethoxyethane, diglyme and so on; alcohols such as methanol, ethanol, isopropyl alcohol, tert-butanol, etc.; and water; and they can be used individually or in combination. Preferred solvents for this reaction are alcohols.

Examples of the catalyst used for dibenzylamine include palladium-on-carbon, palladium hydroxide, Raney Nickel, platinum oxide, etc. among which palladium-on-carbon are preferred.

The reaction temperature when dibenzylamine is preferably from about room temperature up to 80°and the reaction temperature when the decarboxylation is preferably from about 10°to 150°C.

The response time dibenzylamine is about from 1 hour to 16 hours, preferably from about 2 hours to 8 hours, and the reaction time decarboxylation is approximately from 5 minutes to 4 hours, preferably about from 10 minutes to 2 hours.

Stage-3'

Similarly, stage-3 of the method, the compound of formula (23') can be obtained from compounds of formula (22').

In accordance with the stages 1-3, 1-4 and 1-5 method 1 compounds of the present invention can be obtained from the connected to the second formula (23) or (23'), obtained at stages b-3 or b-3'.

Way

Below is an example of the method of obtaining the compounds of formula (1), where the ring is a

(where R4has the same meaning as defined above, R32represents-CON(R11)(R12), where each of R11and R12has the same meaning as defined above, and l' is 1).

Way

In the above reaction scheme, each of R4, R11and R12has the same meaning as defined above, Me represents methyl, and t-Bu represents tert-butyl.

Stage s-1

The acid chloride of the acid can be obtained from compounds of formula (24) in a manner analogous to stage 1-1 method 1. The obtained acid chloride acid is subjected to interaction with the compound of the formula (25) is similar stages 1-3 of method 1, when receiving the connection formula (25).

The compound of formula (26) can be obtained by condensation of compounds of formula (24) with the compound of the formula (25) using a condensing agent (for example, 1-ethyl-3-(3'-dimethylaminopropyl)carbodiimide (WSC), 1-hydroxybenzotriazole (HOBT)). Alternatively, the compound of formula (24) is transformed into a mixed anhydride, followed by interaction with the compound of the formula (25) in the presence of a base, receiving soy is inane formula (26).

Stage C-2

Similarly, stage a-1 of method a compound of formula (28) can be obtained by the coupling of compounds of formula (26) with the compound of the formula (27).

Stage S-3

The compound of the formula (29) can be obtained by treating compounds of formula (28) acid (triperoxonane acid, toluensulfonate acid, methanesulfonic acid, etc. in the presence or in the absence of a solvent under heating or at room temperature for the conversion of tert-Putilkovo ester fragment in the fragment of the carboxylic acid, followed by decarboxylation.

The solvent used in the reaction includes, for example, ethers such as diethyl ether, tetrahydrofuran, dioxane, 1,2-dimethoxyethane, diglyme, etc.; hydrocarbons, such as benzene, toluene, hexane, xylene and so on; alcohols such as methanol, ethanol, isopropyl alcohol, tert-butanol and so on; halogenated hydrocarbons such as methylene chloride, chloroform, carbon tetrachloride, 1,2-dichloroethane, etc.; and water, and can be used separately or in combination. Preferred solvents for this reaction are methylene chloride, chloroform or toluene.

The reaction temperature is from approximately 0°to 120°C, preferably from about room temperature to 100°C.

The reaction time with the is from about 1 hour to 24 hours, preferably from about 2 hours to 12 hours.

Stage C-4

Similarly, stage 1-2 of method 1, the compound of formula (30) can be obtained from compounds of formula (29).

In accordance with the stages 1-3, 1-4 and 1-5 method 1 compounds of the present invention can be obtained from compounds of formula (30), obtained above in stage-4.

Method D

Below is an example of the method of obtaining the compounds of formula (1), where the ring is a

(where R4has the same meaning as defined above, R33represents a C1-6-alkoxy or C7-16-aralkylated, and l' is 1).

Method D

In the above reaction scheme, each of R4, X2, Me and Et, R11and R12has the same meaning as defined above, and R26represents a C1-6-alkyl or C7-16-aralkyl.

Stage D-1

The compound of formula (32) can be obtained by the coupling of compounds of formula (31) with the compound of the formula (16) in a solvent in the presence of a base.

The solvent used in the reaction includes, for example, ethers such as diethyl ether, tetrahydrofuran, dioxane, 1,2-dimethoxyethane, diglyme, etc.; hydrocarbons, such as benzene, toluene, hexane, xylene and so on; esters such as ethyl is Etat, methyl acetate, butyl acetate, etc.; and polar solvents such as acetone, N,N-dimethylformamide, dimethylsulfoxide, etc; and can be used separately or in combination. The preferred solvent for this reaction is N,N-dimethylformamide.

Examples of bases used in the reaction include hydrides of alkali metals, such as sodium hydride, potassium hydride, etc.; and carbonates of alkali metals such as sodium carbonate, potassium carbonate, sodium bicarbonate, potassium bicarbonate, etc.; among which sodium hydride is preferred.

The reaction temperature is from approximately 0°to 100°C, preferably from about room temperature up to 80°C.

The reaction time is from about 2 hours to 48 hours, preferably from about 6 hours to 24 hours.

Stage D-2

The compound of formula (33) can be obtained by hydrolysis of the ester fragment in the compound of formula (32) in a solvent in the presence of a base.

The solvent used in this reaction includes, for example, ethers such as diethyl ether, tetrahydrofuran, dioxane, 1,2-dimethoxyethane, diglyme and so on; alcohols such as methanol, ethanol, isopropyl alcohol, etc.; and water, and can be used separately or in combination. Preferred solvents for this reaction I have are tetrahydrofuran, or a mixture of tetrahydrofuran, ethanol or methanol.

Examples of bases used in the reaction include carbonates of alkali metals such as sodium carbonate, potassium carbonate, etc., aqueous solutions of hydroxides of alkali metals such as lithium hydroxide, sodium hydroxide, potassium hydroxide and so on, among which sodium hydroxide is preferred.

The reaction temperature is from approximately 0°to 120°C, preferably from about room temperature up to 80°C.

The reaction time is from about 1 hour to 24 hours, preferably from about 2.5 hours to 12 hours.

Stage D-3

In a manner analogous to stage 1-1 method 1, a compound of formula (34) can be obtained from compounds of formula (33).

Stage D-4

This method represents a reaction conversion of acid chlorides acid diazo ketones. The compound of the formula (35) can be obtained by the coupling of compounds of formula (34) with diazomethane in a solvent in the presence of a base.

The solvent used in this reaction includes, for example, ethers such as diethyl ether, tetrahydrofuran, dioxane, 1,2-dimethoxyethane, diglyme etc; and can be used separately or in combination. Preferred solvents for this reaction are diethyl ether or tetrahydrofuran.

Examples of the bases used in this reaction, R is t organic bases, such as triethylamine, pyridine, dimethylaminopyridine, N-methylmorpholine and so on, among which triethylamine is preferred.

The reaction temperature is about -20°C to 50°C, preferably from approximately 0°C to room temperature.

The reaction time is from about 2 hours to 48 hours, preferably from about 6 hours to 24 hours.

Stage D-5

This method represents one carbon homologation (synthesis Arndt-Eistert) due to the rearrangement α-diazoketone (Wolff rearrangement). The compound of the formula (35) is subjected to interaction with the use of a silver catalyst (for example, silver benzoate, silver oxide) in alcohol in the presence of a base, receiving the compound of formula (36).

The solvent also acts as the reaction reagent used in this reaction includes, for example, alcohols such as methanol, ethanol, isopropyl alcohol, tert-butanol, etc. and can be used separately or in combination. Preferred solvents (also acting as the reaction reagent for this reaction are methanol or ethanol.

Examples of the bases used in this reaction include organic bases such as triethylamine, pyridine, dimethylaminopyridine, N-methylmorpholine etc. among the cat is where the triethylamine is preferred.

The reaction temperature is from about room temperature to 120°C, preferably from about 60°to 120°C.

The reaction time is from about 2 hours to 36 hours, preferably from about 4 hours to 18 hours.

Stage D-6

Similarly, stage 1-2 of method 1, the compound of formula (37) can be obtained from compounds of formula (36).

In accordance with the stages 1-3, 1-4 and 1-5 of the above method 1, the compounds of the present invention can be obtained from compounds of formula (37)obtained above in stage D-6. The compound obtained by the present invention is additionally subjected to reaction stage 2-2 method 2, with the Deputy OR26can be turned into a " HE.

Method E

Below is an example of the method of obtaining the compounds of formula (1), where the ring is a

(where R4has the same meaning as defined above, R34represents-N(R13)(R14), where each of R13and R14has the same meaning as defined above, and l' is 1).

Method E

In the above reaction scheme, each of R4, R13, R14That IU and t-Bu has the same meaning as defined above.

Stage E-1

Similarly, stage a-1 of method a compound of formula(39) can be obtained by the coupling of compounds of formula (38) with the compound of the formula (27).

Stage E-2

Similarly, stage-3 method With the compound of formula (40) can be obtained from compounds of formula (39).

Stage E-3

The compound of formula (42) can be obtained by the coupling of compounds of formula (40) with the compound of the formula (41) without solvent or in a solvent and in the presence of a base.

The solvent used in the reaction includes, for example, ethers such as diethyl ether, tetrahydrofuran, dioxane, 1,2-dimethoxyethane, diglyme, etc.; hydrocarbons, such as benzene, toluene, hexane, xylene and so on; halogenated hydrocarbons such as methylene chloride, chloroform, carbon tetrachloride, 1,2-dichloroethane and so on; alcohols such as methanol, ethanol, isopropyl alcohol, tert-butanol and so on; esters such as ethyl acetate, methyl acetate, butyl acetate, etc.; polar solvents such as N,N-dimethylformamide, dimethylsulfoxide, etc; and can be used separately or in combination. The preferred solvent for this reaction is tetrahydrofuran.

Examples of the bases used in this reaction include organic bases such as triethylamine, pyridine, dimethylaminopyridine, N-methylmorpholine and so on, among which triethylamine or a mixture of triethylamine and dimethylaminopyridine are preferred.

The reaction temperature is in the Arno 0° With up to 120°C, preferably from about room temperature to 100°C.

The reaction time is from about 2 hours to 48 hours, preferably from about 6 hours to 24 hours.

Stage E-4

In a manner analogous to stage 1-2 of method 1, a compound of formula (43) can be obtained from compounds of formula (42).

In accordance with the stages 1-3, 1-4 and 1-5 of the above method 1, the compounds of the present invention can be obtained from compounds of formula (43)obtained above in stage E-4.

Method F

Below is an example of the method of obtaining the compounds of formula (1), where the ring is a

(where R4has the same meaning as defined above, and R35represents-COO(R25), where R25represents a C1-C6-alkyl, and l' is 1).

Method F

In the above reaction scheme, each of R4, R25and Bn has the same meaning as defined above.

Stage F-1

Similarly, stage 1-1 method 1 for the compound of formula (45) can be obtained from compounds of formula (44).

Stage F-2

The compound of formula (47) can be obtained by the coupling of compounds of formula (45) with the compound of the formula (46) in a solvent in the presence of a base.

The solvent used in the reactions is, includes, for example, ethers such as diethyl ether, tetrahydrofuran, dioxane, 1,2-dimethoxyethane, diglyme, etc.; hydrocarbons, such as benzene, toluene, hexane, xylene and so on; halogenated hydrocarbons such as methylene chloride, chloroform, carbon tetrachloride, 1,2-dichloroethane, etc.; and esters such as ethyl acetate, methyl acetate, butyl acetate and so on; and they can be used individually or in combination. The preferred solvent for this reaction is tetrahydrofuran.

Examples of the bases used in this reaction include organic bases such as triethylamine, pyridine, dimethylaminopyridine, N-methylmorpholine and so on, among which triethylamine is preferred.

The reaction temperature is from about -30°C to 80°C, preferably from approximately -20°C to room temperature.

The reaction time is from about 2 hours to 48 hours, preferably from about 6 hours to 24 hours.

Stage F-3

Similarly, stage a-1 of method a compound of formula (49) can be obtained by the coupling of compounds of formula (47) with the compound of the formula (48).

Stage F-4

The compound of formula (49) interacts similarly, stage 1-2 of method 1 followed by dibenzylammonium and decarboxylation, yielding the compound of formula (50).

In accordance to an alternative method, described in stage 1-3 and stage 1-5 method 1, the compounds of the present invention can be obtained from compounds of formula (50)obtained above in stage F-4.

Method G

Below is an example of the method of obtaining the compounds of formula (1), where the ring is a

(where each of R3and R4has the same meaning as defined above, and l' is 1).

Method G

In the above reaction scheme, each of R3, R4and Et has the same meaning as defined above.

Stage G-1

Similarly, stage 1-1 method 1 for the compound of formula (52) can be obtained from compounds of formula (51).

Stage G-2

Analogichnye stage D-4 method D, compound of formula (53) can be obtained from compounds of formula (52).

Stage G-3

Similarly, stage D-5 way D compound of formula (54) can be obtained from compounds of formula (53).

Stage G-4

Similarly, stage D-6 way D compound of formula (55) can be obtained from compounds of formula (54).

In accordance with the stages 1-3, 1-4 and 1-5 of the above method 1, the compounds of the present invention can be obtained from compounds of formula (55)obtained above in stage (G-4.

Stage G-5

Similarly, stages 1-4 of the above method 1, the compound of formula (55') can be the ü obtained from the compounds of formula (54).

In accordance with the stages 1A-2, 1A-3 and 1A-4 of the above method 1A compounds of the present invention can be obtained from compounds of formula (55')obtained above in stage G-5.

Way N

Below is an example of the method of obtaining the compounds of formula (1), where the ring is a

(where each of R3andR4has the same meaning as defined above, and l3 is 0).

Way N

In the above reaction scheme, each of R1, R2, R3, R4, R5, R6, R7, R8, R9, R23, Alk2, ring A, ring B, ring C, m and n has the same meaning as defined above.

Stage N-1

Similarly, stage 1-2 of method 1, the compound of formula (57) can be obtained from compounds of formula (56).

Stage N-2

Similarly, stages 1-3 of method 1, the compound of formula (58) can be obtained by the coupling of compounds of formula 57, obtained at stage N-1 (or commercially available product), with the compound of the formula (3).

Stage H-3

Similarly, stages 1-4 of method 1, the compound of formula (59) can be obtained from compounds of formula (58).

Stage N-4

Similarly, stages 1-5 of method 1, the compound of formula (1-3), which is a connection, which is the subject of the crust is asego of the invention, can be obtained by the coupling of compounds of formula (59) with the compound of the formula (8).

The way I

Below is an example of the method of obtaining the compounds of formula (1), where the ring is a

(where each of R3and R4has the same meaning as defined above and l4 is 1-3).

The way I

In the above reaction scheme, each of R1, R2, R3, R4, R5, R6, R7, R8, R9, l4, m, n, ring A, ring C, Bn, Me, Alk1, Alk2and X2has the same meaning as defined above.

Stage I-1

Similarly, stages 1-3 of method 1, the compound of formula (61) can be obtained by the coupling of compounds of formula (60) with the compound of the formula (3).

Stage I-2

In conditions similar to stage 1-2 of method 1, provided that the catalyst is palladium hydroxide, the compound of formula (62) can be obtained from compounds of formula (61).

Stage I-3

The compound of formula (64) can be obtained by the coupling of compounds of formula (62) with the compound of the formula (63) in a solvent in the presence of a base. Alternatively, X2-(Alk1)l4-COOEt (in the formula, each of X2, Alk1, l4 and Et has the same meaning as defined above) can be used instead of the on compounds of formula (63).

The solvent used in the reaction includes, for example, ethers such as diethyl ether, tetrahydrofuran, dioxane, 1,2-dimethoxyethane, diglyme, etc.; hydrocarbons, such as benzene, toluene, hexane, xylene and so on; alcohols such as methanol, ethanol, isopropyl alcohol, tert-butanol and so on; esters such as ethyl acetate, methyl acetate, butyl acetate, etc.; polar solvents such as acetone, N,N-dimethylformamide, dimethylsulfoxide, etc; and you can use them individually or in the combination of the two. The preferred solvent for this reaction is N,N-dimethylformamide.

Examples of bases used in the reaction include hydrides of alkali metals, such as sodium hydride, potassium hydride, etc.; alkoxides of alkali metals, such as ethoxide sodium, sodium methoxide, tert-piperonyl potassium, etc.; carbonates of alkali metals such as sodium carbonate, potassium carbonate, etc.; hydroxides of alkali metals such as lithium hydroxide, sodium hydroxide, potassium hydroxide, etc.; carboxylates of alkali metals such as sodium acetate, potassium acetate, etc.; phosphates of alkali metals such as sodium phosphate, potassium phosphate, etc., among which potassium carbonate or sodium hydride are preferred.

The reaction temperature is from approximately 0°to 150°C, preferably from approximately to the room temperature to 100° C.

The reaction time is from about 1 hour to 48 hours, preferably from about 2 hours to 24 hours.

Stage I-4

Similarly, stages 1-4 of method 1, the compound of formula (65) can be obtained from compounds of formula (64).

Stage I-5

Similarly, stages 1-5 of method 1, the compound of formula (1-4), which represents one of the target compounds, can be obtained by the coupling of compounds of formula (65) with the compound of the formula (8).

Method J

Below is an example of the method of obtaining the compounds of formula (1), where the ring is a

(where each of R3, R4and Alk1has the same meaning as defined above and l4 is 1-3).

Method J

In the above reaction scheme, each of R3, R4Me, Alk1, l4 and X2has the same meaning as defined above.

Stage J-1

Similarly, stage I-3 method I, compound of formula (67) can be obtained by the coupling of compounds of formula (66) with the compound of the formula (63). Alternatively, X2-(Alk1)l4-COOEt (in the formula, each of X2, Alk1, l4 and Et has the same meaning as defined above) can be used instead of the compounds of formula (63).

Stage J-2

In accordance with stage I-4 ways I compound of the formula (68) can the t can be obtained from the compounds of formula (67).

Similarly, stages 1A-2, 1A-3 and 1A-4 method 1A compounds of the present invention can be obtained from compounds of formula (68)obtained above in stage J-2.

Method K

Below is an example of the method of obtaining the compounds of formula (1), where the ring is a

(where each of R3, R4, l4and Alk1has the same meaning as defined above).

Method K

In the above reaction scheme, each of R3, R4Me, l4, Alk1and X2has the same meaning as defined above.

Stage K-1

Similarly, stage I-3 ways I compound of formula (70) can be obtained by the coupling of compounds of formula (69) with the compound of the formula (63). Alternatively, instead of the compounds of formula (63) can be used X2-(Alk1)l4-COOEt (in the formula, each of X2, Alk1, l4 and Et has the same meaning as defined above).

Stage K-2

Similarly, stage I-4 ways I compound of the formula (71) can be obtained from compounds of formula (70).

In accordance with the stages 1A-2, 1A-3 and 1A-4 method 1A compounds of the present invention can be obtained from compounds of formula (71)obtained above in stage J-2.

Method L

Below is an example of a method for obtaining compounds of the forms of the crystals (1), where R3in the ring, and R10in the group X are taken together with education

(where each of R3,l4 and Alk1has the same meaning as defined above).

Method L

In the above reaction scheme, each of R1, R2, R4, R5, R6, R7, R8, R9, l4, m, ring A, ring S, Alk1and Alk2has the same meaning as defined above.

Stage L-1

The compound of the formula (1-5)obtained by dibenzylammonium compounds (where R26represents benzyl)obtained in method 1 and method D, is subjected to the interaction with the equivalent poganovo reagent (for example, triphosgene or diphosgene etc) in a solvent in the presence of a base, receiving the compound of the formula (1-6).

The solvent used in the reaction includes, for example, ethers such as diethyl ether, tetrahydrofuran, dioxane, 1,2-dimethoxyethane, diglyme, etc.; hydrocarbons, such as benzene, toluene, hexane, xylene and so on; halogenated hydrocarbons such as methylene chloride, chloroform, carbon tetrachloride, 1,2-dichloroethane, etc. and can be used separately or in combination. The preferred solvent for this reaction is chloroform.

Examples of bases used in the used in this reaction, include organic bases such as triethylamine, pyridine, dimethylaminopyridine, N-methylmorpholine and so on, among which triethylamine is preferred.

The reaction temperature is about -20°to 100°C, preferably from approximately 0°C to room temperature.

The reaction time is from about 10 minutes to 4 hours, preferably from about 30 minutes to 2 hours.

Method M

Below is an example of the method of obtaining the compounds of formula (1), where R10different from hydrogen.

Method M

In the above reaction scheme, each of R1, R2, R3, R4, R23, l, n, X2, ring A, ring b and Alk1have the same meaning as defined above.

Stage M-1

The compound of formula (73) can be obtained by the coupling of compounds of formula (6)obtained in stage 1-3 method 1, with a compound of formula (73) in a solvent in the presence of a base.

The solvent used in the reaction includes, for example, ethers such as diethyl ether, tetrahydrofuran, dioxane, 1,2-dimethoxyethane, diglyme, etc.; hydrocarbons, such as benzene, toluene, hexane, xylene and so on; esters such as ethyl acetate, methyl acetate, butyl acetate, etc.; polar solvents such as N,N-dimethylformamide, dimethyl shall sulfoxide, and so on; and they can be used individually or in combination. The preferred solvent for this reaction is N,N-dimethylformamide.

Examples of bases used in the reaction include hydrides of alkali metals, such as sodium hydride, potassium hydride, etc.; alkoxides of alkali metals, such as ethoxide sodium, sodium methoxide, tert-piperonyl potassium, etc.; carbonates of alkali metals such as sodium carbonate, potassium carbonate, etc.; carboxylates of alkali metals such as sodium acetate, potassium acetate, etc.; phosphates of alkali metals such as sodium phosphate, potassium phosphate, etc. among which sodium hydride is preferred.

The reaction temperature is from approximately 0°to 100°C, preferably from about room temperature up to 80°C.

The reaction time is from about 1 hour to 24 hours, preferably from about 2 hours to 8 hours.

In accordance with the above stages 1-4 and 1-5 of the compounds of the present invention can be obtained from compounds of formula (73)obtained at stage M-1 above.

Way N

Below is an example of the method of obtaining the compounds of formula (1), where each of R8and R9represents a-CONH(R19') (where R19'represents a C1-C6alkyl).

Way N

In the above reaction scheme, each of R5, R6, R7, R25and the ring has the same meaning as defined above.

Stage N-1

The compound of formula (75) can be obtained by interaction of the compound (74) c chloride tiomila or oxalylamino in the solvent.

The solvent used in the reaction includes, for example, ethers such as diethyl ether, tetrahydrofuran, dioxane, 1,2-dimethoxyethane, diglyme, etc.; hydrocarbons, such as benzene, toluene, hexane, xylene and so on; halogenated hydrocarbons such as methylene chloride, chloroform, carbon tetrachloride, 1,2-dichloroethane, etc.; and esters such as ethyl acetate, methyl acetate, butyl acetate and so on; and they can be used individually or in combination. The preferred solvent for this reaction is toluene containing catalytic amount of N,N-dimethylformamide.

The reaction temperature is from about room temperature to 120°C, preferably from about 50°to 100°C.

The reaction time is from about 10 minutes to 6 hours, preferably from about 30 minutes to 3 hours.

Stage N-2

The compound of formula (77) can be obtained by interaction of the compound (75) with a compound of formula (76) in a solvent in the presence of a base.

The solvent used in isoamyl in the reaction, includes, for example, ethers such as diethyl ether, tetrahydrofuran, dioxane, 1,2-dimethoxyethane, diglyme, etc.; hydrocarbons, such as benzene, toluene, hexane, xylene and so on; halogenated hydrocarbons such as methylene chloride, chloroform, carbon tetrachloride, 1,2-dichloroethane, etc.; and esters such as ethyl acetate, methyl acetate, butyl acetate and so on; and they can be used individually or in combination. Preferred solvents for this reaction are methylene chloride or tetrahydrofuran.

Examples of the bases used in this reaction include organic bases such as triethylamine, pyridine, dimethylaminopyridine, N-methylmorpholine and so on, among which triethylamine is preferred.

The reaction temperature is from about -40°C to 60°C, preferably from about -30°C to room temperature.

The reaction time is from about 2 hours to 48 hours, preferably from about 6 hours to 24 hours.

Stage N-3

The compound of formula (78) can be obtained by the interaction of the compounds (77) with paraformaldehyde or formalin in the absence of solvent or in a solvent in the presence of catalytic amounts of base.

The solvent used in the reaction includes, for example, ethers, such as detroyer, tetrahydrofuran, dioxane, 1,2-dimethoxyethane, diglyme, etc.; hydrocarbons, such as benzene, toluene, hexane, xylene and so on; halogenated hydrocarbons such as methylene chloride, chloroform, carbon tetrachloride, 1,2-dichloroethane and so on; alcohols such as methanol, ethanol, isopropyl alcohol, tert-butanol and so on; esters such as ethyl acetate, methyl acetate, butyl acetate, etc.; polar solvents such as N,N-dimethylformamide, dimethyl sulfoxide and so on; and they can be used individually or in combination. The preferred solvent for this reaction is tetrahydrofuran.

Examples of bases used in the reaction include hydrides of alkali metals, such as sodium hydride, potassium hydride, etc.; alkoxides of alkali metals, such as ethoxide sodium, sodium methoxide, tert-piperonyl potassium, etc.; hydroxides of alkali metals such as sodium hydroxide, potassium hydroxide, lithium hydroxide, etc.; carbonates of alkali metals such as sodium carbonate, potassium carbonate, etc.; and organic bases such as triethylamine, diethylamine, pyridine, etc.; among whom tert-piperonyl potassium, ethoxide sodium or potassium hydroxide are preferred.

The reaction temperature is from approximately 0°to 100°C, preferably from about room temperature up to 80°C.

Time is eacli is approximately from 10 minutes to 24 hours, preferably from about 30 minutes to 12 hours.

In accordance with the above methods 1, 1A and 2, the compounds of the present invention can be obtained using the compounds of formula (78)obtained above in stage N-3, instead of the compounds of formula (8).

How About

Below is an example of the method of obtaining the compounds of formula (1), where each of R8and R9is a-COOR25(where R25represents a C1-C6alkyl).

How About

In the above reaction scheme, each of R5, R6, R7, R25and the ring has the same meaning as defined above.

Stage-1

Similarly, stage N-3 way N the compound of formula (80) can be obtained from compound (79).

In accordance with the above methods 1, 1A and 2, the compounds of the present invention can be obtained using the compounds of formula (80)obtained above in stage-1, instead of the compounds of formula (8).

How R

Below is an example of the method of obtaining the compounds of formula (1), where m is 2 or 3. In this way instead of benzyl (Bn) can be used tert-butyldimethylsilyl (TBS).

How R

In the above reaction scheme, each of R5, R6, R7, R8 , R9, X2, m, Bn, and rings has the same meaning as defined above.

Stage R-1

The compound of formula (83) can be obtained by the coupling of compounds of formula (81) with the compound of the formula (82) in the presence of a base.

The solvent used in the reaction includes, for example, ethers such as diethyl ether, tetrahydrofuran, dioxane, 1,2-dimethoxyethane, diglyme, etc.; hydrocarbons, such as benzene, toluene, hexane, xylene and so on; halogenated hydrocarbons such as methylene chloride, chloroform, carbon tetrachloride, 1,2-dichloroethane and so on; alcohols such as methanol, ethanol, isopropyl alcohol, tert-butanol and so on; esters such as ethyl acetate, methyl acetate, butyl acetate, etc.; and polar solvents such as N,N-dimethylformamide, dimethyl sulfoxide and so on; and they can be used individually or in combination. Preferred solvents for this reaction are N,N-dimethylformamide or tetrahydrofuran.

Examples of bases used in the reaction include hydrides of alkali metals, such as sodium hydride, potassium hydride, etc.; alkoxides of alkali metals, such as ethoxide sodium, sodium methoxide, tert-piperonyl potassium, etc.; carbonates of alkali metals such as sodium carbonate, potassium carbonate, etc.; and organic compounds of alkali metals, such to the to diisopropylamide lithium, etc., among which sodium hydride or diisopropylamide lithium are preferred.

The reaction temperature is from approximately 0°to 100°C, preferably from about room temperature up to 80°C.

The reaction time is from about 30 minutes to 24 hours, preferably from about 2 hours to 24 hours.

Stage R-2

Similarly, stage 2-2 method 2 compound of formula (84) can be obtained from compounds of formula (83).

In accordance with the above methods 1, 1A and 2, the compounds of the present invention can be obtained using the compounds of formula (84), obtained above in stage R-2, instead of the compounds of formula (8).

Examples

The present invention is illustrated in more detail using the following examples, but stipulating that the present invention is not limited. In the examples, Me represents methyl, Et represents ethyl, tBu represents tert-butyl and TBS represents a tert-butylmethylether.

Example 1

2,2-Bisericani-2-phenethyl ester 4-[{4'-triptorelin-2-carbonyl)amino]phenylacetic acid

a) Dichlorohydrin phenylmalonate acid

Chloride thionyl (13,7 ml) was added dropwise to a mixture of phenylmalonate acid (11,31 g), dimethylformamide (230 ml) and toluene (27 ml) with cooling gap is the situation with ice. The mixture was stirred at 80°C for 70 minutes and the solvent was removed by evaporation. After azeotropic distillation with toluene the residue was dried in vacuum, obtaining specified in the header connection (to 11.61).

b) Diethylamid phenylmalonate acid

To a mixed solution of ethylamine in tetrahydrofuran (2 M, with 45.5 ml), triethylamine (13,9 ml) and methylene chloride (80 ml) was added dropwise dichlorohydrin phenylmalonate acid (8,99 g)obtained in example 1-(a) at -20°C. the Mixture was stirred overnight while the temperature was increased to room, and then after adding the chlorine-hydrogen acid was diluted with ethyl acetate. The organic layer was washed with saturated salt solution, saturated aqueous sodium bicarbonate and saturated salt solution, dried over sodium sulfate and concentrated. The obtained solid was washed with ethyl acetate and hexane, obtaining specified in the header connection (4,85 g) as a white powder.

(C) Diethylamid 2-hydroxymethyl-2-phenylmalonate acid

Diethylamid phenylmalonate acid (2,34 g)obtained in example 1-b), and parathormone (390 mg) suspended in tetrahydrofuran (20 ml)and to this suspension was added potassium hydroxide (catalytic amount) at 60°C. the Mixture was stirred in ECENA 5 hours and concentrated to remove solvent. The residue was chromatographically on a column of silica gel using a mixture of ethyl acetate:hexane=1:1, receiving specified in the header connection (2,31 g).

d) the acid chloride of 4'-triptorelin-2-carboxylic acid

To a mixture of 4'-triptorelin-2-carboxylic acid (of 5.06 g), dimethylformamide (catalytic amount) and methylene chloride (30 ml) was added dropwise oxalicacid (2,43 ml) under cooling with ice. The mixture was stirred at room temperature for 100 minutes and the solvent was removed by evaporation. After azeotropic distillation with toluene the residue was dried in vacuum, obtaining specified in the header of the connection (of 5.40 g).

e) Ethyl ester 4-[(4'-triptorelin-2-carbonyl)amino]phenylacetic acid

To a mixture of ethyl ester of 4-aminophenylarsonic acid (3,41 g), triethylamine (3.2 ml) and methylene chloride (30 ml) was added dropwise a solution of acid chloride of 4'-triptorelin-2-carboxylic acid (5,40 g)obtained in example 1-d) in methylene chloride (10 ml) under ice cooling, and the mixture was stirred at room temperature overnight. After addition of 1 N. hydrochloric acid, the reaction mixture was diluted with ethyl acetate and the organic layer was washed with saturated salt solution, saturated aqueous sodium bicarbonate and Ishenim salt solution, was dried over sodium sulfate and then concentrated, receiving specified in the header connection (8,12 g).

f) 4-[(4'-Triptorelin-2-carbonyl)amino]phenylacetic acid

Ethyl ester of 4-[(4'-triptorelin-2-carbonyl)amino]phenylacetic acid (8,12 g)obtained in example 1-e), was dissolved in 40 ml of tetrahydrofuran and 20 ml of ethanol. After addition of 4 n sodium hydroxide (5 ml) the solution was stirred at room temperature for 5 hours and concentrated. The powder formed by the addition of 1 N. hydrochloric acid, collected by filtration and dried in vacuum, obtaining specified in the header of the connection (of 7.48 g).

g) 2,2-Bisericani-2-phenethyl ester 4-[{4'-triptorelin-2-carbonyl)amino]phenylacetic acid

4-[(4'-Triptorelin-2-carbonyl)amino]phenylacetic acid (519 mg)obtained in example 1-f), diethylamid 2-hydroxymethyl-2-phenylmalonate acid (317 mg)obtained in example 1-C), dimethylaminopyridine (171 mg), and hydrochloride of 1-ethyl-3-(3'-dimethylaminopropyl)carbodiimide (WSC.HCl) (268 mg) was dissolved in methylene chloride (5 ml). The solution was stirred at room temperature for 6 hours, and the solvent was removed by evaporation. The residue was purified column chromatography on silica gel using a mixture etilize is at:hexane=1:1 to 3:2, getting listed in the title compound (725 mg) (see table 1).

Example 1-2

Diethyl ester of 2-phenyl-2-{2-[4-(4'-triptorelin-2-carbonyloxy)phenyl]acetoxymethyl}malonic acid

a) Diethyl ester of 2-hydroxymethyl-2-phenylmalonate acid

Paraformaldehyde (720 mg) suspended in diethyl ether phenylmalonate acid (4,73 g) was added to this mixture, a catalytic amount of potassium hydroxide at 60°C. After stirring for 1.5 hours the reaction mixture was purified column chromatography on silica gel using a mixture of ethyl acetate:hexane=1:5 to 1:2, receiving specified in the header connection (4,96 g).

(b) Diethyl ester 2-[2-(4-benzyloxyphenyl)acetoxymethyl]-2-phenylmalonate acid

4-Benzyloxyaniline acid (1,09 g) suspended in methylene chloride (50 ml) and the suspension was dissolved by adding dimethylaminopyridine (0,511 g). To the solution was added diethyl ether 2-hydroxymethyl-2-phenylmalonate acid (1.20 g)obtained in example 1-2A), was added in portions to this mixture of the hydrochloride of 1-ethyl-3-(3'-dimethylaminopropyl)carbodiimide (0,864 g). The mixture was stirred at room temperature overnight and then concentrated. The residue was purified column chromatography on silica gel using the m mixture of ethyl acetate:hexane=1:4, getting listed in the title compound (1,95 g) as a colourless oil.

C) Diethyl ether 2-[2-(4-hydroxyphenyl)acetoxymethyl]-2-phenylmalonate acid

Diethyl ether 2-[2-(4-benzyloxyphenyl)acetoxymethyl]-2-phenylmalonate acid (1,95 g)obtained in example 1-2b), was dissolved in methanol (2.5 ml). The solution was first made in the presence of 7.5% palladium-on-carbon (0,200 g) at normal pressure for 4 hours. The reaction solution was filtered through a layer of celite and concentrated, obtaining specified in the header connection (1,71 g) as a colourless oil.

d) Diethyl ester of 2-phenyl-2-{2-[4-(4'-triptorelin-2-carbonyloxy)phenyl]acetoxymethyl}malonic acid

4'-Triptorelin-2-carboxylic acid (0,266 g) suspended in methylene chloride (10 ml), and the suspension was dissolved by addition of 4-dimethylaminopyridine (0,122 g). To the solution was added diethyl ether 2-[2-(4-hydroxyphenyl)acetoxymethyl]-2-phenylmalonate acid (0.400 g)obtained in example 1-2C), and was added in portions to this mixture of the hydrochloride of 1-ethyl-3-(3'-dimethylaminopropyl)carbodiimide (0,192 g). The mixture was stirred at room temperature overnight and then concentrated. The residue was purified column chromatography on silica gel using a mixture of ethyl acetate:hexane=1:3, p is the ray specified in the title compound (0.55 g) as an amorphous powder (see table 1).

Example 1-3

Diethyl ether 2-(2-{3-methyl-[4-(4'-triptorelin-2-carbonyl)amino]phenyl]acetoxymethyl}-2-phenylmalonate acid

a) Diethyl ether 2-(3-methyl-4-nitrophenyl)malonic acid

Sodium hydride (60%in mineral oil; 0,599 g) suspended in dimethylformamide (10 ml) and was added to the suspension dropwise with ice cooling diethyl ester of malonic acid (2.00 g) in dimethylformamide. After the termination of the foam to the reaction mixture was added a solution of 4-fluoro-2-methylnitrobenzene (1,94 g) in dimethylformamide (5 ml) and the reaction temperature was raised to 100°C, followed by stirring for 6 hours. The reaction mixture was concentrated, acidified 1 N. hydrochloric acid and was extracted with ethyl acetate. The extract was washed successively with water and saturated salt solution, dried over sodium sulfate and concentrated. The residue was purified column chromatography on silica gel using a mixture of ethyl acetate:hexane=1:5, getting mentioned in the title compound (1.65 g) as a yellow oil.

b) (3-Methyl-4-nitrophenyl)acetic acid

Potassium hydroxide (has 0.168 g) was dissolved in 7 ml of methanol and 1 ml of water, and this solution was dissolved in diethyl ether 2-(3-methyl-4-nitrophenyl)malonic acid (0,250 g)obtained in example 1-a). The solution was stirred at 100°C for 2 hours and concentrated. The residue was acidified using 2 N. hydrochloric acid and was extracted with ethyl acetate. The extract was washed with saturated salt solution, dried over sodium sulfate and concentrated, obtaining specified in the header connection (0,143 g) as a yellow solid.

C) Diethyl ether 2-[2-(3-methyl-4-nitrophenyl)acetoxymethyl]-2-phenylmalonate acid

(3-Methyl-4-nitrophenyl)acetic acid (0,143 g)obtained in example 1-3b), was dissolved in methylene chloride (5 ml). To the solution was added diethyl ether 2-hydroxymethyl-2-phenylmalonate acid (of € 0.195 g)obtained in example 1-2A, 4-dimethylaminopyridine (0,090 g) and the hydrochloride of 1-ethyl-3-(3'-dimethylaminopropyl)carbodiimide (0,141 g)and the mixture was stirred at room temperature overnight. The reaction mixture was concentrated, and the residue was purified column chromatography on silica gel using a mixture of ethyl acetate:hexane=1:4, receiving specified in the header connection (0,219 g) as a yellow oil.

d) Diethyl ester 2-[2-(4-amino-3-were)acetoxymethyl]-2-phenylmalonate acid

Diethyl ether 2-[2-(3-methyl-4-nitrophenyl)acetoxymethyl]-2-phenylmalonate acid (0,219 g)obtained in example 1-3C), was dissolved in methanol (3 ml). The solution is selective is Ali in the presence of 7.5% palladium-on-carbon (0,030 g) at normal pressure, getting listed in the title compound (0,197 g) as a yellow oil.

e) Diethyl ether 2-(2-{3-methyl-[4-(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid

By the way, is similar to that described in example 1d), 4'-trifluoromethyl-2-biphenylcarbonic acid (0.124 g) is transformed into the corresponding acid chloride acid. On the other hand, is specified in the header connection (0,215 g) was obtained as a colorless amorphous product from diethyl ether 2-[2-(4-amino-3-were)acetoxymethyl]-2-phenylmalonate acid (0,197 g)obtained in example 1-3d), in a manner analogous to example 1E) (see table 1).

Example 1-4

Diethyl ether 2-(2-{4-[methyl-(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid

a) Ethyl ester {4-[methyl-(4'-triptorelin-2-carbonyl)amino]phenylacetic acid

Sodium hydride (51 mg) was dissolved in dimethylformamide (5 ml)and the solution was cooled to 0°C. To the solution was added ethyl ester 4-[(4'-triptorelin-2-carbonyl)amino]phenylacetic acid (500 mg)obtained in example 1E), and the mixture was stirred for one hour. After adding iodomethane (183 mg) and the mixture was stirred at room temperature for 3 hours and then added water. Reaktionarsten concentrated, was diluted with ethyl acetate and washed with water. The resulting solution was dried over sodium sulfate and purified column chromatography on silica gel using a mixture of hexane:ethyl acetate=4:1, getting mentioned in the title compound (141 mg).

(b) Diethyl ether 2-(2-{4-[methyl-(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid

Ethyl ester {4-[methyl-(4'-triptorelin-2-carbonyl)amino]phenylacetic acid (141 mg)obtained in example 1-4A)were subjected to interactions, similar to those described in examples 1f) and 1g), getting mentioned in the title compound (56 mg) (see table 1).

Example 1-5

2,2-Bisericani-2-phenethyl ether {3-ethyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid

a) Ethyl ester of 3-ethyl-4-nitrophenylarsonic acid

To a solution of ethyl ester of 4-nitrophenylarsonic acid (1.63 g) in tetrahydrofuran (100 ml) was added dropwise a 2 M solution of ethylmagnesium in tetrahydrofuran (3 ml) at -15°C in an atmosphere of argon, and the mixture was stirred at the same temperature for 30 minutes. After further adding dropwise 2 M solution of ethylmagnesium in tetrahydrofuran (3 ml) and the mixture was stirred at -15°C for one hour and was added to a mixture of 2,3-dichlor,6-dicyano-1,4-benzoquinone (3.0 g). The mixture was stirred overnight and added to her water (300 ml) followed by extraction with chloroform (150 ml x 3). The organic layers were combined, washed with saturated salt solution, dried over sodium sulfate and purified column chromatography on silica gel using a mixture of hexane:ethyl acetate=10:1, receiving specified in the header connection (1,09 g).

b) 2,2-Bisericani-2-phenethyl ether {3-ethyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid

Ethyl ester 3-ethyl-4-nitrophenylarsonic acid (1,05 g)obtained in example 1-5A)were subjected to interactions, similar to that described in example 1-3d), example 1E), example 1f and example 1g), getting mentioned in the title compound (1.60 g) (see table 1).

Examples 1-6 on 1-85

The compounds of examples 1-6 on 1-85 was obtained by methods similar to those described in examples 1 to 1-5. The compounds obtained are presented in tables 2-17.

Table 1
ExampleStructureNMR (δ, 300MHz, CDC13)
1< / br>
TPL 88,4-91,2
of 1.05 (6H, t, J=7,3 Hz), 3,18 to be 3.29 (4H, m), 3,53 (2H, s), a 4.83 (2H, s), to 6.95 (1H, users), 7,02-of 7.23 (8H, m), 7,27 was 7.36 (3H, m), 7,41-7,47 (1H, m), 7,49-7,63 (4H, m), 7,65-7,72 (2H, m), to 7.77-to 7.84 (1H, m)
1-2to 1.19 (6H, t, J=9,2 Hz), 3,53 (2H, s), 4,18 (4H, q, J=9,2 Hz), 4,82 (2H, s), 6,79 (2H, d, J=12hz), 7,14 (2H, d, J=12hz), 7,29 (5H, users), 7,38-7,73 (7H, m), of 8.09 (1H, DD, J=1,2, J=7,5 Hz)
1-3to 1.21 (6H, t, J=7,1Hz), to 1.67 (3H, c), 3,47 (2H, s), 4,20 (4H, q, J=7,1Hz), 4,82 (2H, c), 6,89 ((1H, users), 6,92 (1H, users), 7,00 (1H, d, J=10,GC). 7,30 (5H, users), 7,42-to 7.84 (9H, m)
1-4to 1.22 (6H, t, J=7,2 Hz), 3,23 (3H, s), 3,40 (2H, s), is 4.21 (4H, q, J=7,2Hz), a 4.83 (2H, s), 6,10 (2H, d, J=8,3 Hz), 6,70 (2H, d, J=8,3 Hz), 7,07-to 7.61(13H, m)
1-5< / br>
TPL 105-109
of 0.93 (3H, t, J=7,5 Hz), of 1.05 (6H, t, J=7,3 Hz), was 1.94 (2H, q, J=7,5 Hz), 3,13 of 3.28 (4H, m), 3,53 (2H, s), a 4.83 (2H, s), 6,80-7,84 (19H, m)

to 3.50 (2H, s), 3,68-4,00 (3H, m), 4,42 (1H, DD, J=6,0, and 11.0 Hz), to 4.62 (1H, DD, J=7,9, 11,0 Hz), of 5.68 (1H, t, J=6,8gts), to 6.95 (1H, s), 7.03 is-7,17 (4H, m), 7,17 and 7.36(5H, m), 7,44 (1H, DD, J=1,5, 7,GC), of 7.48-to 7.64 (4H, m), 7,65-7,71 (2H, m), 7,80 (1H, DD, J=1,5, 7,GC)
Table 2
ExampleStructureNMR (δ, 300MHz, CDC13)
1-6of 3.56 (2H, c), 3,65-of 3.78 (2H, c), 4,55 (2H, c), 5,49 (1H, usher.), 7,01 (1H, users), 7,05-7,83 (20H, m)
1-7of 1.39 (3H, d, J=7,2 Hz), 3,48-3,68 (2H, m), 3,70-to 3.89 (2H, m), of 4.44 (1H, d, J=10,GC), of 4.66 (1H, d, J=10,GC), 5,46 (1H, usher.), of 6.96 (1H, users), 7,02-7,84 (20H, m)
1-8
1-9of 1.20 (6H, t, J=7,2 Hz), 3,51 (2H, s), 4,20 (4H, q, J=7,2Hz), to 4.81 (2H, s), 6,92 (1H, users),? 7.04 baby mortality-to 7.18 (4H, m), 7.24 to to 7.35 (5H, m), 7,44 (1H, DD, J=1,5, 7,1 Hz), of 7.48-to 7.64 (4H, m), 7,65-7,73 (2H, m), 7,81 (1H DD, J=1,5, 7,1 Hz)
1-101,47 to 1.76 (6H, m), 1,90-2,03 (2H, m), of 3.60 (2H, s), 3,71-of 3.85 (2H, m), 4,10 (2H, s)6,94 (1H, users), 7,12-7,20 (4H, m), 7,44 (1H, DD, J=1,2, 7,4 Hz), 7,49-to 7.64 (4H, m), 7,65-7,72 (2H, m), 7,80 (1H, DD, J=1,2, 7,4 Hz)

Table 3
ExampleStructureNMR (δ, 300MHz, CDC13)
1-11of 1.18 (6H, d, J=6,4 Hz), of 1.20 (6H, d, J=6,0 Hz), 3,50 (2H, s), 4,80 (2H, s)5,08 (1H, Sept, J=6,4 Hz), to 5.08 (1H, Sept, J=6,0 Hz), 6,92 (1H, s), 7,05-7,16 (4H, m), 7,27-to 7.32 (5H, m), 7,41-7,47 (1H, m), 7,49-7,63 (4H, m), 7,65-7,72 (2H, m), 7,80 (1H, DD, J=1,5, 7,1 Hz)
1-12of 3.53 (2H, s), 3,74-of 3.97 (4H, m), to 4.87 (2H, s)6,94 (1H, s), 7,00-7,07 (2H, m), 7,09-7,20 (4H, m), 7,31-7,47 (6H, m), 7,49-to 7.64 (4H, m), 7,65-7,72 (2H, m), 7,80 (1H, DD, J=1,5, 7,5Hz)
1-133,5 (H, C), and 3.7 (6H, s), to 4.81 (2H, s), 6,92 (1H, users) 7,05-7,16 (4H, m), 7,22-to 7.35 (5H, m), 7,41-7,46 (1H, m), 7,49-7,63 (4H, m), 7,65-7,71 (2H, m), 7,81 (1H, DD, J=1,5, 7,2 Hz)
1-14of 1.20 (6H, t, J=7,1Hz), 1,29-of 1.81 (10H, usher.), 2,40 of $ 2.53 (1H, m), 3,52 (2H, s), of 4.13 (4H, q, J=7,1Hz), 4,48 (2H, s), 6,93 (1H, users), 7,14 (4H, users), 7,39-7,83 (8H, m)
1-15< / br>
TPL 108,8 - to 112.4
1,27-of 1.44 (5H, m), 1,46-to 1.61 (3H, m), 1,79-1,90 (2H, m), of 3.57 (2H, s), 3.72 points-a 3.87 (2H, m), 4,07 (2H, S), 5,71-of 5.81 (1H, m)6,94 (1H, users), 7,10-7,21 (4H, m), 7,40-7,47 (1H, m), 7,49-7,63 (4H, m), 7,65-7,72 (2H, m,), to 7.77-7,83 (1H, m)

Table 4
ExampleStructureNMR (δ, 300MHz, CDC13)
1-16< / br>
TPL 93-95
to 1.22 (6H, t, J=7,2 Hz), of 3.57 (2H, s), is 4.21 (4H, q, J=7,2Hz), a 4.83 (2H, s), 7,20 (1H, d, J=8,5Hz), 7,28-to 7.67 (12H, m), 7,76 (1H, d, J=7,4)
1-17TPL 99-103of 1.20 (6H, t, J=7,1Hz), 3,53 (2H, s), 4,19 (4H, q, J=7,1Hz), 4,82 (2H, with),6,91 (1H, d, J=8,3 Hz), 7,11-7,56 (16H, m), with 8.33 (1H, DD, J=7,8, 1,8gts), 9,62(1H, users)
1-18of 1.05 (3H, m)to 1.22 (6H, t, J=7,2Hz), was 1.58 (2H, m)to 1.99 (2H, m), of 3.57 (2H, s), 4,21 (6H, m), is 4.85 (2H, s),? 7.04 baby mortality-of 7.60 (12H, m), 8,30 (1H, m), 10,07 (1H, users)
1-19to 1.22 (6H, t, J=6,9G is), of 3.60 (2H, s), 4,20 (4H, sq J=6,GC), is 4.85 (2H, s), 7,12-7,37 (9H, m), 7,63-7,73 (2H, m), 7,79-7,86 (1H, m), of 7.90-8,00 (1H, m)
1-20of 1.18 (6H, t, J=6,8gts), 3,51 (2H, s), 4,17 (4H, q, J=6,8gts), 4,80 (2H, s)6,70 (2H, d, J=12hz), to 7.09 (2H, d, J=12hz), 7,27 (5H, users), 7,41-7,83 (8H, m), 8,21 (1H, d, J=10Hz)

Table 5
ExampleStructureNMR (δ, 300MHz, CDC13)
1-21of 1.18 (6H, t, J=7,2 Hz), 3,49 (2H, s), is 4.15 (4H, q, J=7,2 Hz), 4,80 (2H, s), 7,07 (1H, d, J=8,Hz), 7,27-7,54 (17H, m), 7,88 (1H, d, J=6,2 Hz)
1-221,16-1,83 (20H, m), 3,50 (2H, s), 4.80 to 4,91 (2H, m), 4,82 (2H, s), 6,93 (1H, users), 7,05-7,17 (4H, m), 7,27-7,34 (5H, m), 7,41-7,47 (1H, 7,49-7,63 (4H, m), 7,65-7,72 (2H, m), 7,80 (1H, DD, J=1,5, 7,2 Hz)
1-230,95-1,22 (6H, m), 1,23 was 1.43 (4H, m), 1,50-1,71 (6H, m), 1,71-1,90 (4H, m), 3,52 (2H, s), 3,69-a 3.83 (2H, m), 4,84 (2H, s), to 6.95 (1H, users),? 7.04 baby mortality-to 7.35 (11H, m), 7,41-of 7.48 (1H, m), 7,49-the 7.65 (4H, m), 7,66-7,73 (2H, m,), to 7.77-to 7.84 (1H, m)
1-24to 3.58 (2H, s), is 5.06 (2H, s), for 6.81 (1H, users), 6,99-7,05 (4H, m), 7,08-7,16 (2H, m), 7.24 to 7,47 (14H, m), 7,50-to 7.67 (6H, m), 7,80 (1H, DD, J=1.5 and 7.5 Hz), the remaining 9.08 (2H, users)
1-25the 1.04 (6H, d, J=6,4 Hz, of 1.09 (6H, d, J=6,8gts), 3,52 (2H, s), 3.95 to 4.09 to (2H, m), a 4.83 (2H, s), 6,92-7,03 (3H, m), 7.03 is-7,10 (2H, m), 7,11-of 7.23 (4H, m), 7,27 was 7.36 (3H, m), 7,41-7,47 (1H, m), 7,49-to 7.64 (4H, m), 7,65-7,72 (2H, m), 7,80 (1H, DD, J=1,5, 7,5Hz)

Table 6
ExampleStructureNMR (δ, 300MHz, CDC13)
1-26to 1.19 (6H, t, J=7,1Hz), 3,24 (2H, s)and 3.59 (2H, s), is 4.15 (4H, q, J=7,1Hz), 4,32 (2H, s), 6,80-to 6.88 (2H, m), 6,93 (1H, users), 7,11-7,28 (7H, m), 7,39-7,83 (8H, m)
1-27to 1.21 (6H, t, J=7,1Hz), and 2.14 (3H, s), 3,51 (2H, s), 4,19 (4H, q, J=7,1Hz), 4,80 (2H, s), 6.87 in (1H, users), 6,91-7,02 (3H, m), 7,19-7,34 (5H, m), 7,40-a 7.85 (8H, m)
1-28of 3.56 (2H, s), 3,71-of 3.95 (4H, m), to 4.87 (2H, s),

6,75-6,83 (2H, m)

7,05-7,19 (4H, m)

7,29-7,44 (6H, m)

7,47-of 7.60 (3H, m)

a 7.62-7,73 (3H, m)

8,05-to 8.12 (1H, m)
1-293,55 (2H, s), 3,70-of 3.94 (4H, m), a 4.86 (2H, s)of 6.71-6,79 (2H, m), 7,01-to 7.09 (2H, m), 7,11-to 7.18 (2H, m), 7,27-7,54 (N, m), EUR 7.57-7,66 (1H, m), 7,94 shed 8.01 (1H, m)
1-30of 0.95 (3H, t, J=7,4 Hz), 1,45-to 1.60 (2H, m), 1,76-of 1.88 (2H, m), 3,62 (2H, s), 3,79-of 3.97 (4H, m), 4,08 (2H, t, J=6,4 Hz), the 4.90 (2H, s), 6,99-7,06 (2H, m), 7,10-7,21 (6H, m), 7,31-7,41 (5H, m), of 7.48-7,56 (1H, m)of 7.96 (1H, DD, J=1,8, 8,0 Hz)

Table 7
ExampleStructureNMR (δ, 300MHz, CDC13)
1-310,97-of 1.10 (6H, m)of 1.12 (6H, t, J=6,8gts), 1,54-of 1.78 (4H, m), 2.05 is-2,17 (1H, m), of 3.54(2H, s), of 4.13 (4H, q, J=6,8gts), 4,50 (2H, s), 6,93 (1H, users), 7,14 (4H, users), 7,40-of 7.82 (8H, m)
1-323,51 (2H, s), 3,85 (4H, m), a 4.86 (2H, s), to 6.88 (1H, s), 7,00-7,54 (19H, m), 7,89 (1H, m)
1-33of 3.56 (2H, s), a-3.84 (4H, m), a 4.86 (2H, s)6,91 (1H, d, J=8,3 Hz), 7,07-7,55 (18H, m), 8,32 (1H, DD, J=7,9, 1,GZ), for 9.64 (1H, s)
1-34of 1.23 (6H, t, J=7,1Hz), 3,70 (2H,s), 4,22 (4H, t, J=7,1Hz), to 4.81 (2H, s), 7,02 (1H, users), 7,13-7,97 (16H, m)
1-35< / br>
TPL 100,5-104,0
of 0.85 (6H, t, J=7,5 Hz), 1,37-is 1.51 (4H, m), 3,13-up 3.22 (4H, m), 3,53 (2H, s), 4,84 (2H, s), of 6.96 (1H, users), 7,02-to 7.09 (2H, m), 7,10-7,24 (6H, m), 7,27-to 7.35 (3H, m), 7,41-7,47 (1H, m), 7,49-7,63 (4H, m), 7,65-7,72 (2H, m), 7,80 (1H, DD, J=1,6, 8,0 Hz)

Table 8
ExampleStructureNMR (δ, 300MHz, CDC13)
1-36by 2.73 (6H, d, J=4,Hz), 3,53 (2H, s), to 4.81 (2H, s)6,94 (1H, users), 701-7,09 (4H, m), 7,11-7,21 (4H, m), 7,27-to 7.35 (3H, m), 7,41-7,47 (1H, m), 7,49-7,63 (4H, m), 7,66-7,72 (2H,m), 7,81 (1H, DD, J=1,5, 7,5Hz)
1-37of 1.20 (6H, t, J=7,0 Hz), 3,50 (2H, s), is 4.21 (4H, q, J=7,0 Hz), the 4.90 (2H, s), 6,93 (1H, users),? 7.04 baby mortality-to 7.15 (4H, m), 7,15-7,21 (1H, m), 7,38-7,47 (2H, m), 7,49-to 7.64 (5H, m), 7,66-7,72 (2H, m), 7,81 (1H, DD, J=1,5, 7,5Hz), 8,46-8,51 (1H, m)
1-38to 1.22 (6H, t, J=7,2 Hz), 3,51 (2H, s), is 4.21 (4H, q, J=7,2 Hz), 4,82 (2H, s), 6,98 (1H, users), 7,03-7,17 (4H, m), 7,22 (1H, DD, J=5,0, 8,5Hz), 7,41-7,47 (1H, m), of 7.48-7,63 (5H, m), of 7.64-7,72 (2H, m), to 7.77-7,83 (1H, m), 8,50-to 8.57 (2H, m)
1-39the 1.04 (6H, t, J=7,4 Hz), 3,16 to be 3.29 (4H, m), 3,55 (2H, s), 4,84 (2H, s), 6.75 in-6,83 (2H, m),? 7.04 baby mortality-7,14 (4H, m), 7,17-7,22 (2H, m), 7,27-to 7.35 (3H, m), 7,41 (1H, DD, J=1,1, 7,GC), 7,47-rate of 7.54 (2H, m), 7,56 (1H, DD, J=1,5, 7,GC), to 7.61-7,72 (3H, m), 8,08 (1H, DD, J=1,1, 7,GC)
1-40of 1.20 (6H, t, J=7,1Hz), 3,55 (2H, s), is 4.21 (4H, q, J=7,1Hz), 4,84 (2H, s), 7,20-to 7.77 (16H, m), 8,16(1H, user.)

Table 9
ExampleStructureNMR (δ, 300MHz, CDC13)
1-41a 1.01 (3H, t, J=7,2 Hz), 1,60 (2H, m), a 1.96 (2H, m)and 3.59 (2H, s), a-3.84 (4H, m), is 4.21 (2H, t, J=6,5 Hz), 4,89 (2H, c), of 7.00 (1H, d, J=8,3 Hz), 7,09-7,16 (5H, m), 7,32-7,58 (8H,m), compared to 8.26 (1H, DD, J=8,0, 1,GC), 10,07 (1H, users)
1-42to 0.88 (6H, t, J=7,1Hz), 1,19 is 1.34 (4H, m), of 1.35 to 1.48 (4H, m), 3,16-3,26 (4H, m), 3,52 (2H, s), 4,84 (2H, s), to 6.95 (1H, users), 7,02-of 7.23 (8H, m), 7,27 was 7.36 (3H, m), 7,40-7,47 (1H, m), 7,49-7,63 (4H, m), of 7.64-7,73 (2H, m), 7,81 (1H, DD, J=1,5, 7,5Hz)
1-43to 1.22 (6H, t, J=7,1Hz), to 3.58 (2H, s), 4,22 (4H, q, J=7,1Hz), is 4.85 (2H, s), 6,23 (2H, d, J=8,5Hz), 7,30-7,73 (10H, m), 7,87 (2H, d, J=8,5Hz), at 8.36 (1H, DD, J=6,8, 2,3 Hz), to 12.3 (1H, users)
1-44to 1.24 (6H, t, J=7,1Hz), to 3.58 (2H, s)to 4.23 (4H, q, J=7,1Hz), 4,27 (2H, s), is 4.85 (2H, s), 7,22 (2H, d, J=8,5Hz), 7,27-7,98 (13H, m), to 7.61 (2H, d, J=8,5Hz)
1-45< / br>
so pl. 175-177
of 1.05 (6H, t, J=7,3 Hz), 1.69 in (3H, s), 3,14-3,30 (4H, m), 3,49 (2H, s), a 4.83(2H, s), 6,77 (1H, users), 6,89 (1H, users), 6,92-a 7.85 (17H, m)

Table 10
ExampleStructureNMR (δ, 300MHz, CDC13)
1-46of 1.20 (6H, t, J=7,1Hz), of 2.38 (3H, s)to 3.49 (2H, s), 4,19 (4H, q, J=7,1Hz), to 4.81 (2H, s), make 6.90 (1H, users), 7,05 (4H, users), 7,19-7,56 (12H, m), 7,88 (1H, d, J=7,1 Hz)
1-47of 1.20 (6H, t, J=7,1Hz), to 3.49 (2H, s), 3,81 (3H, s), 4,19 (4H, q, J=7,1Hz), to 4.81 (2H, s), 6.87 in-7,56 (17H, m), 7,86 (1H, d, J=7,Hz)
1-48of 1.12 (6H, t, J=7,2 Hz), 2,49-of 2.58 (2H, m), 3,30(4H, d of q, J=5,6, 7,2 Hz), of 3.54 (2H, s), 4,07-to 4.15 (2H, m)6,94 (1H, users), 7,11-to 7.18 (4H, m), 7,22-7,37 (5H, m), 7,41-7,46 (1H, m), of 7.48-7,63 (6H, m), 7,65-7,71 (2H,m), 7,80 (1H, DD, J=1,5, 7,5Hz)
1-49of 0.87 (6H, t, J=7,2 Hz)and 1.51 (4H, t kV, J=7,2, 7,2 Hz), 2,50 at 2.59 (2H, m), 3,18-of 3.27 (4H, m), of 3.54 (2H, s), 4,07-to 4.15 (2H, m), to 6.95 (1H, users), 7,12-to 7.18 (4H, m), 7.23 percent and 7.36 (5H, m), 7,41-7,46 (1H, m), of 7.48-7,63 (6H, m), 7,65-7,71 (2H, m), 7,80 (1H, DD, J=1,5, 7,5Hz)
1-50of 1.05 (6H, t, J=7,1Hz), 3,17 of 3.28 (4H, m), 3,51 (2H, s), 4,82 (2H, s), 6.87 in (1H, users), 6,97-7,22 (8H, m), 7,27-to 7.35 (3H, m), 7,39-to 7.59 (8H, m), of 7.90 (1H, DD, J=1,5, 7,5Hz)

Table 11
ExampleStructureNMR (δ, 300MHz, CDC13)
1-51of 1.03 (6H, t, J=7,1Hz), and 3.16 of 3.28 (4H, m), of 3.56 (2H, s), 4,82 (2H, s), 6,88-6,94 (1H, m), 7,02-7,34 (13H, m), 7,39-7,49 (3H, m), 7,51-to 7.59 (2H, m), a 8.34 (1H, DD, J=1,9, 7,GC), 9,63 (1H, users)
1-52of 1.05 (3H, t, J=7,2 Hz), with 1.07 (6H, t, J=7,2 Hz), 1,54 by 1.68 (2H, m), 1,92-of 2.05 (2H, m), 3,19-of 3.31 (4H, m)to 3.58 (2H, s)to 4.23 (2H, q, J=6,4 Hz), is 4.85 (2H, s), 7,02 (1H, d, J=8,3 Hz), 7,06-7,38 (10H, m), 7,44-7,53 (1H, m), EUR 7.57-the 7.65 (2H, m), 8,30(1H, DD, J=1,9,7,GC), 10,08 (1H, users)
1-53 of 1.23 (6H, t, J=7,1Hz), 3,53 (2H, s)to 4.23 (4H, q, J=7,1Hz), 4,84 (2H, s), to 6.95 (1H, users), 7,10 (2H, d, J=8,3 Hz), 7,17 (2H, d, J=8,3 Hz), 7,32 (5H, users), 7,41-7,87 (8H, m)
1-54to 1.19 (6H, t, J=7,1Hz), a 3.50 (2H, s)to 4.16 (2H, sq J=7,1Hz), to 4.17 (2H, q, J=7,1Hz), 4,80 (2H, s), 6,89-of 7.90 (17H, m)
1-55of 1.05 (6H, t, J=7,2 Hz), 3,19-of 3.31 (4H, m), of 3.54(2H, s), a 4.86 (2H, s), make 6.90 (1H, d, J=8,3 Hz), 7,02-7,11 (3H, m), 7,16-of 7.23 (2H, m), 7,25 was 7.36 (4H, m), 7,41 (1H, DD, J=1,2, 7,5Hz), of 7.48-to 7.61 (3H, m), a 7.62-7,71 (3H, m), 8,21 (1H, DD, J=1,5, 7,5Hz)

Table 12
ExampleStructureNMR (δ, 300MHz, CDC13)
1-56to 1.21 (6H, t, J=7,1Hz), 3,51 (2H, s), 4,20 (4H, q, J=7,1Hz), 4,82 (2H, s), 6,99-EUR 7.57 (16H, m), to 7.84 (1H, d, J=7,2 Hz)
1-57of 1.23 (6H, t, J=7,2 Hz), of 3.57 (2H, s), 4,22 (4H, q, J=7,2Hz), is 4.85 (2H, s), 7,19-8,08 (19H, m)
1-58of 0.94 (6H, d, J=6,8gts), to 1.22 (6H, t, J=7,1Hz), 3,40 (2H, s), 4,20 (4H, q, J=7,1Hz), 4,82 (2H, s), 4,99 (1H, m), 6,16 (1H, users), is 6.78 (2H, d, J=8,Hz), was 7.08 (1H, DD, J=8,6, 1,5Hz), 7,20-7,74 (13H m)
1-590,89 (4H, m)to 1.22 (6H, t, J=7,1Hz), 1,28-of 1.78 (6H, m), 3,40 (2H, s), 4,20 (4H, q,J=7,1Hz), to 4.62 (1H, m), 4,82 (2H, s), x 6.15 (1H, users), to 6.75 (2H, m), 7,06-7,74 (14H, m)
1-60of 1.23 (6H, t, J=6,GC), of 1.28 (6H, d, J=6,GC), 3,40 (1H, Sept, J=6,GC), of 3.56 (2H, s), 4,22 (4H, q, J=6,GC), 4,84 (2H, s), 7,12-to 7.61 (14H, m)

Table 13
ExampleStructureNMR (δ, 300MHz, CDC13)
1-61to 1.22 (6H, t, J=7,1Hz), 3,53 (2H, s), 4,22 (4H, q, J=7,1Hz), to 4.23 (2H, s), a 4.83 (2H, s), 6,98-to 7.61 (19H, m)
1-620,86 (6H, t, J=7,3 Hz), 1,50 was 1.69 (4H,m), 3,50 (2H, s), 4,10 (4H, t, J=6,GC), a 4.83 (2H, s), 6,93 (1H, users), was 7.08 (2H, d, J=8,Hz), 7,13 (2H, d, J=8,Hz), 7,29 (5H, users), 7,40-7,83 (8H, m)
1-630,84 (12H, d, J=6,GC), 1,80-of 1.97 (2H, m), 3,50 (2H, s)to 3.92 (4H, d, J=6,GC), 4,84 (2H, s), 6,93 (1H, users), was 7.08 (2H, d, J=5,5Hz), 7,13 (2H, d, J=5,5Hz), 7,29(5H, users), 7,40-to 7.84 (8H, m)
1-64to 1.22 (6H, t, J=7,1Hz), of 3.57 (2H, s), is 4.21 (4H, q, J=7,1Hz), 4,84 (2H, s), 7,21 (2H, d, J=8,5 Hz), 7.23 percent-of 7.60 (8H, m), EUR 7.57 (2H, d, J=8,5Hz), of 8.09 (1H, DD, J=7,8, 1,8gts), compared to 8.26 (1H, users)
1-65from 0.84 (3H, t, J=7,3 Hz), of 1.23 (6H, t, J=7,1Hz), 1,23 of 1.46 (2H, m), 1,50 was 1.69 (2H,m), 3,55 (2H, s)to 4.23 (4H, q, J=7,1Hz), 4,25 (2H, q, J=6,GC), ,84 (2H, C)7,19 (2H, d, J=8,4 Hz), 7,21-7,37 (5H, m), 7,44-to 7.64 (3H, m), 7,56 (2H, d, J=8,4 Hz), to 7.64 (1H, users), 7,95 (1H, d, J=7,Hz)

Table 14
ExampleStructureNMR (δ, 300MHz, CDC13)
1-660,84 (N, d, J=6,8gts), 1,63-to 1.79 (2H, m), 2,97-3,15 (4H, m), 3,52 (2H, s), a 4.86 (2H, s)6,94 (1H, users), 7,01-was 7.08 (2H, m), 7,10-of 7.25 (6H, m), 7,27 was 7.36 (3H, m), 7,40-7,47 (1H, m), of 7.48-7,63 (4H, m), of 7.64-7,72 (2H, m), 7,80 (1H, DD, J=1,5, 8,0 Hz)
1-67of 0.87 (12H, d, J=6,8gts), 1,27-to 1.38 (4H, m), 1,46-to 1.61 (2H, m), 3,18 of 3.28 (4H, m), 3,52 (2H, s), 4,84 (2H, s)6,94 (1H, users), 7,01-7,22 (8H, m), 7,27-to 7.35 (3H, m), 7,41-7,47 (1H, m), 7,49-7,63 (4H, m), 7,65-7,72 (2H, m), 7,80 (1H, DD, J=1,5, 7,5Hz)
1-68of 1.07 (3H, t, J=7,2Hz), to 1.22 (6H, t, J=7,1Hz), 3,40 (2H, s), and 3.72 (2H, q, J=7,2 Hz), 4,20 (4H, q, J=7,1Hz), a 4.83 (2H, s), 6,14 (2H, d, J=8,3 Hz), 6,74 (2H, d, J=8,3 Hz), 7,07 (1H, DD, J=9,1, 1,5 Hz), 7.23 percent-to 7.61 (12H, m)
1-69of 1.09 (6H, t, J=7,1Hz), 1,26 of 1.50 (6H, m), is 1.81 (4H, m), 2,99 (1H, m), 3,26 (4H, d of q, J=1,1,7,1 Hz)and 3.59 (2H, s), is 4.85 (2H, s), 7,10-7,42 (14H, m), 7,56 (2H, d, J=8,3 Hz)
1-70of 1.05 (6H, t, J=7,2 Hz), 3,18-3,30 (4H, m), 3,53 (2H, s), a 4.83 (2H, s), 6,93 (1H, users), 7,02-of 7.23 (8H, m), 7,27 was 7.36 (3H, m), 7,37 was 7.45 (5H, m), 7,45-to 7.59 (2H, m), 7,80(1H, is d, J=1,1,7,5Hz)

Table 15
ExampleStructureNMR (δ, 300MHz, CDC13)
1-71of 1.05( 6H, t, J=7,2 Hz), 3,18-3,30 (4H, m), of 3.54 (2H, s), 4,84 (2H, s), 7,02-7,14 (5H, m), 7,17-to 7.35 (8H, m), 7,37 to 7.62 (5H, m), 7,74 (1H, DD, J=1,5, 7,5Hz)
1-72< / br>
TPL 126,4-127,8
of 0.85 (6H, t, J=7,5 Hz), the 1.44 (4H, t kV, J=7,5, 7,5Hz), by 1.68 (3H, s), 3,12-up 3.22 (4H, m), 3,49 (2H, s), is 4.85 (2H, s), 6,77 (1H, users), 6,87-6,92 (1H, m), 6,94-7,01 (1H, m), 7,11-of 7.25 (4H, m), 7,27 was 7.36 (3H, m), 7,40-7,47 (1H, m), 7,50-7,73 (6H, m), 7,75-a 7.85 (2H, m)
1-733,29 (6H, s), 3,36-of 3.48 (8H, m), 3,53 (2H, s), is 4.85 (2H, s), 6,97 (1H, users),? 7.04 baby mortality-to 7.18 (4H, m), 7,19-7,40 (8H, m), 7,41-7,47 (1H, m), 7,49-to 7.64 (4H, m), 7,66-7,73 (2H, m), to 7.77-to 7.84 (1H, m)
1-74to 1.22 (6H, t, J=7,1Hz), 2,78 (3H, s), 3,52 (2H, s), is 4.21 (4H, q, J=7,1Hz), 4,82 (2H, s), 7,11 (2H, d, J=8,5Hz), 7,19 (2H, d, J=8,5Hz), 7,20-to 7.35 (6H, m), to 7.77 (2H, d, J=8,3 Hz), 7,86 (2H, d, J=8,3 Hz)
1-75of 1.06 (6H, t, J=7,3 Hz), 2,78 (3H, s), 3,20 to be 3.29 (4H, m), 3,55 (2H, s), 4,84 (2H, s), 6,98-7,34 (12H, m), to 7.77 (2H, d, J=8,3 Hz), 7,86 (2H, d, J=8,3 Hz)

Table 16
Example StructureNMR (δ, 300MHz, CDC13)
1-76of 1.06 (6H, t, J=7,3 Hz), 3,19 of 3.28 (4H, m), of 3.54 (2H, s), a 4.83 (2H, s), 6,99-of 7.48 (13H, m), 7,71 (2H, d, J=8,2 Hz), 7,86 (2H, d, J=8,2 Hz), 8,05-8,13 (1H, m), 8,75-8,84 (1H, m)
1-77of 1.06 (6H, t, J=7,2 Hz), of 1.64 (3H, s), 3,12-to 3.33 (4H, m), 3,51 (2H, s), 4,84 (2H, s), at 6.84 (1H, users), 6,91 (1H, users), 6,98-7,98 (12H, m), 8,16 (1H, d, J=8,1 Hz), 8,84 (1H, d, J=4,4 Hz)
1-78to 0.92 (3H, t, J=7,5 Hz), of 1.20 (6H, t, J=7,1Hz), was 1.94 (2H, q, J=7,5 Hz), 3,50 (2H, s), 4,20 (4H, q, J=7,1Hz), 4,82 (2H, s), 6,79-7,83 (17H, m)
1-79of 0.96 (6H, d, J=6,GC), of 1.05 (6H, t, J=7,1Hz), to 2.15 (1H, Sept., J=6,GC), 3,19-3,29 (4H, m), of 3.54 (2H, s), a 4.83 (2H, s), for 6.81-7,84 (19H, m)
1-80< / br>
TPL 91,5-94,8
of 0.96 (6H, d, J=6,8gts), of 1.20 (6H, t, J=7,1Hz), of 2.16 (1H, Sept., J=6,8gts), 4,20 (4H, q, J=7,1Hz), 4,82 (2H, s), 6,79-7,82 (17H, m)

Table 17
ExampleStructureNMR (δ, 300MHz, CDC13)
1-81< / br>
TPL 147-158
of 0.95 (3H, t, J=7,Hz), of 1.13 (6H, t, J=7,2 Hz), 1,99 (2H, q, J=7,Hz), of 2.54 (2H, t, J=7,Hz), 3,20-to 3.38 (4H, m), 3,53 (2H, s), 4,11 (2H, t, J=7,Hz), 6,79-7,84(19H, m)
1-82to 0.72 (6H, d, J=6,GC), of 1.06 (6H, t, J=7,2 Hz), 1,26-of 1.44 (1H, m), 1,89 (2H, d, J=7,3 Hz), 3,20-of 3.27 (4H, m), 3,52(2H, s), a 4.83 (2H, s), 6,82-7,88 (19H, m)
1-83< / br>
TPL 80-86
of 0.71 (6H, d, J=6,5 Hz), to 1.21 (6H, t, J=7,1Hz), 1,26 was 1.43 (1H, m), a 1.88 (2H, d, J=7,3 Hz), 3,49 (2H, s), is 4.21 (4H, q, J=7,1Hz), a 4.83 (2H, s), 6,79-7,87 (17H,m)
1-84to 1.21 (6H, t, J=7,2 Hz), of 3.48 (2H, s), 4,22 (4H, q, J=7,2Hz), a 4.83 (2H, s), was 7.08 (1H, d, J=8,Hz), 7,12 (1H, s), 7,25-to 7.67 (13H, m), to 7.84 (1H, DD, J=1,5, 7,5Hz), of 8.37 (1H, d, J=8,Hz)
1-85to 1.21 (6H, t, J=7,1Hz), of 3.48 (2H, s), 4,22 (4H, q, J=7,1Hz), a 4.83 (2H, s), 7,13 (1H, d, J=7,Hz), 7,28-to 7.67 (14H, m), 7,82 (1H, DD, J=1,5, 7,5Hz), 8,35 (1H, d, J=8,Hz)

Example 2

2,2-Bisericani-2-phenethyl ether {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid

a) 5-Chloro-N,N-dimethyl-2-nitrobenzamide

The acid chloride of the acid was obtained from 5-chloro-2-nitrobenzoic acid (5.0 g), similarly to the method of example 1d)were subjected to interactions, similar to that described in example 1E), getting mentioned in the title compound (5.5 g).

b) tert-Butyl ether methyl ester of 2-(3-dimethylcarbamoyl-4-nitrophenyl)malonic acid

/img>

Sodium hydride (350 mg) was dissolved in dimethylformamide (10 ml)and the solution was cooled to 0°C. After adding tert-butylmalonate (1.52 g) and the mixture was stirred for 1 hour and added to 5-chloro-N,N-dimethyl-2-nitrobenzamide (1.0 g)obtained in example 2A). The mixture was stirred at 70°C for 4.5 hours and was added to her water. The resulting solution was concentrated, diluted with ethyl acetate and washed with water. The organic layer was dried over sodium sulfate and purified column chromatography on silica gel using a mixture of ethyl acetate:hexane=1:1, getting mentioned in the title compound (1.29 g).

C) Methyl ester of (3-dimethylcarbamoyl-4-nitrophenyl)acetic acid

tert-Butyl ether methyl ester of 2-(3-dimethylcarbamoyl-4-nitrophenyl)malonic acid (1.22 g)obtained in example 2b), was dissolved in dichloromethane (10 ml)and the solution was cooled to 0°C. After adding triperoxonane acid (10 ml) and the mixture was stirred at room temperature for 6 hours and then concentrated, followed by azeotropic distillation with toluene. The residue was purified column chromatography on silica gel using a mixture of ethyl acetate:hexane=3:1, getting mentioned in the title compound (712 mg).

d) Methyl ester of (4-amino-3-dimethylcarbamoyl)acetic acid

Methyl ether (3-dimethylcarbamoyl-4-nitrophenyl)acetic acid (683 mg)obtained in example 2C), were subjected to the reactions described in example 1-3d), getting mentioned in the title compound (627 mg).

e) {3-Dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid

Methyl ester of (4-amino-3-dimethylcarbamoyl)acetic acid (627 mg)obtained in example 2d), was subjected to reactions similar to those described in example 1E and example 1f), getting mentioned in the title compound (1.07 g) (see table 65).

f) 2,2-Bisericani-2-phenethyl ether {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid

{3-Dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid (517 mg)obtained in example 2E), were subjected to interaction, similar to that described in example 1g), getting mentioned in the title compound (387 mg) (see table 18).

Examples 2-2 on 2-119

Compounds of examples 2-2 on 2-119 was obtained by methods similar to those described in example 2. Thus obtained compounds are shown in tables 18-41. In addition, the compound of example 2-a) was obtained in a manner analogous to the method of example 2E), and thus obtained the compounds shown in table 65.

Table 18
ExampleStructureNMR (δ, 300MHz, CDC13)
21,07 (6N, t, J=7,2 Hz), 2,85 (3H, users), 2,95 (3H, users), 3,26 (4H, d of q, J=7,2, 7,2 Hz), of 3.54 (2H, s), 4,84 (2H, s),? 7.04 baby mortality-to 7.68 (17H, m), of 8.37 (1H, d, J=8,3 Hz), 9,16 (1H, users)
2-20,86 (6H, t, J=7,2 Hz), of 1.46 (4H, t kV, J=7,2, 7,2 Hz), 2,85 (3H, users), 2,95 (3H, users), 3,19 (4H, dt, J=7,2, 7,2 Hz), of 3.54 (2H, s), is 4.85 (2H, s), 7.03 is-7,68 (17H, m), of 8.37 (1H, d, J=8,Hz), 9,17 (1H, users)
2-3of 1.07 (6H, t, J=7,1Hz), and 2.83 (3H, d, J=4.5 Hz), 3,24 (4H, q, J=7,1, 7,1 Hz)and 3.59 (2H, s), 4,80 (2H, s), 7,10-7,76 (18H, m), 8,53 (1H, d, J=8,3 Hz), for 11.55 (1H, users)
2-4< / br>
TPL 128-129
of 1.12 (6H, t, J=7,3 Hz), 2,53 (2H, t, J=7,Hz), of 2.86 (3H, users), 2,95 (3H, users), 3,20-3,40 (4H, m), of 3.54 (2H, s), of 4.12 (2H, t, J=7,Hz), to 7.09 (1H, users), 7,17-7,75 (14H, m), at 8.36 (1H, d, J=8,4 Hz), 9,24 (1H, users)
2-5< / br>
TPL 114-116
to 1.21 (6H, t, J=7,1Hz), of 2.81 (3H, users), of 2.92 (3H,users), a 3.50 (2H, s), 4,20 (4H, q, J=7,1Hz), 4,82 (2H, s), of 6.99 (1H, users), 7,17-7,71 (14H, m), with 8.33 (1H, d, J=8,5Hz), 9,14 (1H, users)

Table 19
ExampleStructure NMR (δ, 300MHz, CDC13)
2-6of 0.98 (6H, t, J=7,3 Hz), of 3.12 (4H, d of q, J=7,3, 7,3 Hz), to 3.58 (2H, s), 4,50 (2H, d, J=5,GC), 4,79 (2H, s), 7,01-to 7.59 (16H, m), 7,72 (1H, DD, J=7,0, 1,8gts), 8,23 (1H, m), 8,51 (1H, d, J=8,5Hz), 11,49 (1H, users)
2-7of 1.07 (6H, t, J=7,3 Hz), of 1.66 (2H, m), 2,28 (2H, m), 2,87 (3H, users), with 2.93 (3H, users), 3,24 (4H, d of q, J=7,3, 7,3 Hz), of 3.57 (2H, s), 4,11 (2H, t, J=6,GC), 7,13-7,66 (17H, m), at 8.36 (1H, d, J=8,4 Hz), the remaining 9.08 (1H, users)
2-8a 1.08 (6H, t, J=7,2 Hz), 0,98-to 1.21 (6H, userd), 3,26 (4H, d of q, J=7,2, 7,2 Hz), 3,12-3,51 (4H, userd), of 3.56 (2H, s), 4,84 (2H, s), 7,06-7,63 (17H, m), 8,21 (1H, d, J=8,Hz), 8,88 (1H, s)
2-9< / br>
TPL 108-117
of 1.07 (6H, t, J=7,1Hz), 0,93-to 1.59 (6H, userd), 3,26 (4H, d of q, J=7,2, 7,2 Hz), of 3.56 (2H, s), 3,41-of 3.95 (2H, userd), 4,84 (2H, s), 7,01-7,62 (17H, m), 8,08 (1H, d, J=8,3 Hz), to 8.70 (1H, users)
2-10to 1.21 (6H, t, J=7,1Hz), 0,95-of 1.27 (6H, userd), is 3.08-to 3.49 (4H, userd), 3,52 (2H, s), is 4.21 (4H, q, J=7,1Hz), a 4.83 (2H, s),7,06 (1H, d, J=1,GZ), 7,19 (1H, DD, J=8,7, 1,GC), 7,31-7,63 (13H, m), 8,19 (1H, d, J=8,Hz), of 8.90 (1H, users)

Table 20
ExampleStructureNMR (δ, 300MHz, CDC13)
2-11 to 1.21 (6H, t, J=7,1Hz), 1,00-of 1.52 (12H, userd), 3,52 (2H, s), 3,49-to 3.92 (2H, userd), 4,20 (4H, q, J=7,1Hz), 4,82 (2H, s), 7,02 (1H, d, J=1,GZ), 7,17 (1H, DD, J=8,4, 1,GC), 7,31-to 7.64 (13H, m), of 8.06 (1H, d, J=8,4 Hz), 8,72 (1H, users)
2-121,01-to 1.21 (6H, m)of 1.07 (6H, t, J=7,3 Hz), 2,78 (3H, users), 3,20-of 3.31 (4H, m), of 3.56 (2H, s), 3,82-4,27 (1H, m), 4,84 (2H, s), 6,99-7,63 (17H, m), 8,19 (1H, d, J=8,4 Hz), 8,98 (1H, users)
2-13< / br>
TPL,5-119,0
0,98-of 1.27 (3H, usher.), to 1.21 (6H, t, J=7,1Hz), 2,73-2,96 (3H, usher.), 3,05-to 3.49 (2H, usher.), 3,51 (2H, s), is 4.21 (4H, q, J=7,1Hz), 4,82 (2H, s), 7,00-was 7.08 (1H, m), 7,19 (1H, DD, J=1,9, 8,3 Hz), 7,24 and 7.36 (5H, m), 7,39 (1H,DD, J=1,5, 7,GC), 7,43-of 7.70 (7H, m), of 8.28 (1H, d, J=8,Hz), 8,92-9,18(1H, user.)
2-141,00-of 1.23 (3H, usher.), a 1.08 (6H, t, J=7,2 Hz), 2,79-2,96 (3H, usher.), 3,10-to 3.49 (2H, usher.), 3,26 (4H, d of q, J=5,2, 7,2 Hz), 3,55 (2H, s), 4,84 (2H, s),? 7.04 baby mortality (1H, d, J=1,8gts), 7,07-7,14 (2H, m), 7,15-7,24 (3H, m), 7,28-7,37 (3H, m), 7,37-the 7.43 (1H, m), 7,44-7,69 (7H, m), 8,30 (1H, d, J=8,3 Hz), 8,88-9,17 (1H, user.)
2-151,02-of 1.24 (3H, usher.), of 1.12 (6H, t, J=7,2 Hz), 2,47 at 2.59 (2H, m), 2,80-2,96 (3H, usher.), 3,10-3,51 (2H, usher.), 3,30 (4H, d of q, J=5,7, 7,2 Hz), 3,55 (2H, s), 4,07-4,18 (2H, m), to 7.09 (1H, d, J=1,5Hz), 7,22-the 7.43 (7H, m), 7,43-of 7.70 (9H, m), of 8.28(1H, d, J=8,3 Hz), cent to 8.85-9,14 (1H, user.)

Table 21
ExampleStructureNMR (δ, 300MHz, CDC13)
2-16of 1.07 (6H, t, J=7,2 Hz), 1.32 to 1,71 (5H, usher.), 3,10-with 3.79 (8H, m), of 3.54 (2H, s), 4,84 (2H, s), 7.03 is-7,79 (15H, m), of 8.28 (1H, d, J=8,5Hz), 9,04 (1H, users)
2-17of 1.07 (6H, t, J=7,2 Hz), 2,02-2,78 (4H, usher.), 3,21-of 3.53 (8H, m), of 3.54(2H, m), 4,84 (2H, s), 7.03 is-7,72 (15H, m), a 8.34 (1H, d, J=7,2 Hz), 9,83 (1H,users)
2-18< / br>
TPL 106,8-109,4
0,65-a 1.01 (3H, usher.), to 1.21 (6H, t, J=7,2 Hz), 1,43-of 1.66 (2H, usher.), 2,75 are 2.98 (3H, usher.), 3,05-to 3.41 (2H, usher.), 3,51(2H, s), is 4.21 (4H,. kV, J=7,2 Hz), 4,82 (2H, s),? 7.04 baby mortality(1H, users), 7,19 (1H, DD, J=1,9, 8,GC), 7,24-to 7.35 (5H, m), 7,39 (1H, DD, J=1,5, 7,5Hz), 7,43-7,69 (7H, m), 8,18-8,31 (1H, usher.), 8,94-9,18 (1H, user.)
2-190,68 is 0.99 (3H, usher.), a 1.08 (6H, t, J=7,1Hz), 1,42 was 1.69 (2H, usher.), 2,79 are 2.98 (3H, usher.), a 3.06-of 3.42(2H, usher.), 3,26(4H, d of q, J=5,6, 7,1 Hz), 3,55 (2H, s), 4,84 (2H, s),? 7.04 baby mortality (1H, d, J=1,8gts), 7,11 (2H, ushort, J=5,GC), 7,15-7,24 (3H, m), 7,27 was 7.36 (3H,m), 7,37-the 7.43 (1H, m), 7,44-7,69 (7H, m), 8,21-8,35 (1H, user.), 8,92-9,18 (1H, user.)
2-20of 0.67 to 1.00{3H, usher.), of 1.13(6H, t, J=7,1Hz), 1,43-to 1.67(2H, usher.), 2,48 at 2.59(2H, m), 2,82 are 2.98(3H, usher.), a 3.06-3,42{2H, usher.), 3,30(4H, d sq J=5,6, 7,1 Hz), of 3.54(2H, s), 4,07-4,17(2H, m), to 7.09(1H, d, J=2,2 Hz), 7,22-7,42(7H, m), 7,43-of 7.69(9H, m), 8,20-to 8.34(1H, usher.), 8,89-9,14(1H, user.)

Table 22
ExampleStructureNMR (δ, 300MHz, CDC13)
2-21the 1.04 (3H, t, J=7,2 Hz), 2,84 (3H, users), 2,95 (3H, users), 3,16 to be 3.29 (2H, m), 3,50 (2H, s)to 3.64 (1H, DD, J=7,7, 6,5 Hz), 3,91 (1H, DD, J=10,9, 6,5 Hz), with 4.64 (1H, DD, J=10,9, 7,GC), 5,28 is 5.38 (1H, m), 7,00-7,71 (15H, m), a 8.34 (1H, d, J=8,5Hz), to 9.15 (1H, users)
2-22< / br>
t, PL-131
to 1.21 (6H, t, J=7,1Hz), 1,73 is 2.00 (4H, m), 3,22-of 3.53 (4H,m), 3,51 (2H, s), 4,20 (4H, q, J=7,1Hz), a 4.83 (2H, s), 7,15-7,70 (15H, m), with 8.33 (1H, d, J=8,Hz), 9,84 (1H, users),
2-23< / br>
t, pl. 118-120
to 1.21(6H, t, J=7,1Hz), 1,35 is 1.70(6H, user), 3,00 is 3.76(4H, user), 3,51 (2H, s), 4,20 (4H, q, J=7,1Hz), 4,82 (2H, s), 7,03 (1H, d, J=2,0 Hz), 7,12-7,68 (14H, m), compared to 8.26 (1H, d, J=8,5Hz), 9,06 (1H, users),
2-24a 1.11 (3H, t, J=7,Hz), 2,19 (2H, q, J=7,Hz), 2,84 (3H, users), 2,95 3H, users), of 3.54 (2H, s), 4,28 (1H, DD, J=11,3, 4,GC), to 4.41 (1H, DD, J=11,3, 7,0 Hz), 5.25 to 5,33 (1H, m), by 5.87 (1H, d, J=8,3 Hz),? 7.04 baby mortality-7,71 (15H, m), at 8.36 (1H, d, J=8,5Hz), 9,14 (1H, users)
2-25< / br>
TPL 95-98
a 1.11 (3H, t, J=7,5 Hz), 2,19 (2H, q, J=7,5 Hz), 2,84 (3H, users), 2,95 (3H, users), of 3.54 (2H, s), the 4.29 (1H, DD, J=11,3, 4,GC), to 4.41 (1H, DD, J=11,3, 7,0 Hz), 5,26-5,33 (1H, m), 5,86 (1H, d, J=7,Hz),? 7.04 baby mortality-7,71 (15H, m), at 8.36 (1H, d, J=8,Hz), 9,14 (1H, users)

Table 23ExampleStructureNMR (δ, 300MHz, CDC13)2-26< / br>
TPL 152-155of 2.53 (4H, s), 2,89 (3H, users), 2,96 (3H, users), 3,55 (2H, s), of 4.66 (1H, DD, J=10,9, 5,3 Hz), 5,10 (1H, t, J=10,GC), lower than the 5.37 (1H, DD, J=10,9, 5,3 Hz), 7,07-7,69 (15H,m), 8,35 (1H, d, J=8,Hz), 9,17 (1H, users)2-27to 1.19 (3H, t, J=7,2 Hz), 2,70-a 3.01 (6H, usher.), to 3.41 (2H, d, q, J=5,6, 7,2 Hz), of 3.60 (2H, s), 5,32 (2H, s), 6,18 (1H, ushort, J=5,GC),? 7.04 baby mortality (1H, d, J=1,GZ), 7,21-7,29 (1H, m), 7,30-7,56 (7H, m), 7,56-7,66 (4H,m), of 7.69 (1H, DD, J=1,5, 7,1 Hz), 8,35 (1H, d, J=8,Hz), which is 9.09 (1H, users)2-28the 1.04 (3H, t, J=7,1Hz), 2,70-of 3.00 (6H, usher.), up 3.22 (2H, d, q, J=5,7, 7,1 Hz), 3,53 (2H, s), of 3.57(2H, s)to 5.13 (2H, s), 5,43 is 5.54 (1H, usher.), was 7.08 (1H, d, J=1,GZ), 7,21-the 7.43 (6H, m), 7,44-7,66 (6H, m), of 7.69 (1H, DD, J=1,5, 7,2 Hz), a 8.34 (1H, d, J=8,Hz), 9,10 (1H, users)2-291,26 by 1.68 (6H, m), 2,61-of 3.00 (6H, m), 2,93-of 3.12 (1H, m), to 3.58-4,01 (1H, m), 4,28-to 5.03 (3H, m), 7,09-8,32 (17H, m), 9,14 (1H, users), 9,40-10,24 (2H, m)2-30of 1.10 (6H, t, J=7,3 Hz), 3,06 (6H, users), 3,21-of 3.42 (4H, m), 3,61 (2H, s), a 4.86 (2H, s), 7,06-to 7.77 (13H, m), of 8.37 (1H, d, J=8,5Hz), of 9.21 (1H, users)

Table 24
StructureNMR (δ, 300MHz, CDC13)
2-31< / br>
TPL 106-110
of 1.23 (6H, t, J=7,1Hz), 2,98 (3H, users) 3,05 (3H, users), 4,22 (4H, q, J=7,1Hz), is 4.85 (2H, s), 7,11-of 7.75 (11H, m), 8,35 (1H, d, J=8,5Hz), of 9.21 (1H, users)
2-32to 1.24 (6H, t, J=7,2 Hz), 2,61 (2H, t, J=7,1Hz), of 2.86 (3H, users), to 2.94 (3H, users), of 3.46 (2H, s)4,07 (2H, t, J=7,1Hz), to 4.23 (4H, q, J=7,2Hz), was 7.08 (1H, d, J=1,Hz), 7.23 percent-of 7.68 (14H, m), at 8.36 (1H, d, J=8,Hz), to 9.15 (1H, users)
2-33< / br>
TPL 125-128
to 1.22 (6H, t, J=7,2 Hz), and 2.83 (3H, users), to 2.94 (3H, users), 3,51 (2H, s), is 4.21 (4H, q, J=7,2Hz), a 4.83 (2H, s), 7,00-7,51 (14H, m), 7,68 (1H, DD, J=7,6, 1,5Hz), of 8.37 (1H, d, J=8,3 Hz), 8,93 (1H, users)
2-34< / br>
TPL 124 to 128
to 1.22 (6H, t, J=7,2 Hz), 2,86 (3H, users), 2,95 (3H, users), 3,51 (2H, s), is 4.21 (4H, q, J=7,2Hz), a 4.83 (2H, s), 7,01 (1H, d, J=2,2 Hz), 7,19-7,53 (13H, m), 7,68 (1H, DD, J=7,6, 1,5Hz), 8,40 (1H, d, J=8,3 Hz), 9,01 (1H, users)
2-35a 1.96 (3H, s)2,84 (3H, users), 2,95 (3H, users), of 3.54 (2H, s), the 4.29 (1H, DD, J=11,6, 5,0 Hz), 4,39 (1H, DD, J=11,6, 7,1 Hz), 5,23-5,33 (1H, m), 5,90 (1H, d, J=8,1 Hz), 6,99-7,71 (15H, m), at 8.36 (1H, d, J=8,5Hz), 9,14 (1H, users)

Table 25
ExampleArt is ucture NMR (δ, 300MHz, CDC13)
2-36to 0.92 (3H, t, J=7,4 Hz), 1.56 to its 1.68 (2H,m), and 2.14 (2H, t, J=7,5 Hz), 2,84 (3H, users), 2,95 (3H, users), of 3.54 (2H, s), the 4.29 (1H, DD, J=11,4, 4,GC), and 4.40 (1H, DD, J=11,4, 7,1 Hz), 5,23-5,33 (1H, m), 5,90 (1H, d, J=8,1 Hz), 7,05 (1H, d, J=2,0 Hz), 7,15-7,72 (14H, m), at 8.36 (1H, d, J=8,5Hz), to 9.15(1H, users)
2-37of 1.07 (3H, t, J=7,3 Hz), a 1.08 (3H, t, J=7,3 Hz), of 2.97 (3H, s), 3,10 (3H, s), 3,18-of 3.31 (4H, m)and 3.59 (2H, s), to 4.87 (2H, d, J=4,1 Hz), 6,38 (1H, d, J=8,2 Hz), 6,92-to 7.64 (18H, m), 7,83 (1H, d, J=6,8gts)
2-38to 1.21 (6H, t, J=7,1Hz), 2,96 (3H, s), of 3.07 (3H, s), 3,55 (2H, d, J=2,1 Hz), 4,19 (2H, q, J=7,1Hz), 4,20 (2H, q, J=7,1Hz), 4,82 and 4,89 (2H, each d, J=11,2 Hz), 6,36 (1H, d, J=8,2 Hz), 6,93-to 7.59 (16H, m), 7,83 (1H, d, J=6,8gts)
2-39< / br>
TPL 108,8-to 112.4
2,73-of 3.00 (6H, usher.), to 3.52 (2H, s), and 3.72 (6H, s), 4,82 (2H, s), 7,03 (1H, d, J=1,GZ), 7,16 and 7.36 (6H, m), 7,40 (1H, DD, J=1,5, 7,5Hz), 7,45-the 7.65 (6H, m), of 7.69 (1H, DD, J=1,5, 7,2 Hz), 8,35 (1H, d, J=8,Hz), 9,17 (1H, users)
2-40< / br>
TPL 110-111
to 1.21 (6H, t, J=7,1Hz), 1,31-to 1.60 (6H, m), 1,67-to 1.82 (2H, m), 2.40 a-to 2.57 (1H,m), is 2.88 (3H, users), to 2.94 (3H, users), 3,53 (2H, s), 4,14 (4H, q, J=7,1Hz), 4,48 (2H, s), to 7.09 (1H, d, J=1,8gts), 7,21-7,72 (9H, m)of 8.37 (1H, d, J=8,4 Hz), 9,16 (1H, users),

Table 26
ExampleStructureNMR (δ, 300MHz, CDC13)
2-41< / br>
TPL 108-110
0,95-1,19 (6H, m)to 1.21 (6H, t, J=9,5 Hz), 1,60-1,80 (4H, m), 2.00 in to 2.18 (1H, m), is 2.88 (3H, users), 2,95 (3H, users), 3,52 (2H, s), 4,14 (4H, q, J=9,5 Hz), 4,50 (2H, s), to 7.09 (1H, d, J=2,GC), 7,19-7,73 (9H, m), scored 8.38 (1H, d, J=11,3 Hz), 9,18 (1H, users),
2-42< / br>
TPL 121-124
to 1.22 (6H, t, J=7,2 Hz), 2,84 (3H, users), to 2.94 (3H, users), 3,51 (2H, s), is 4.21 (4H, q, J=7,2Hz), a 4.83 (2H, s), 7,01 (1H, d, J=1,GZ), 7,20 (1H, DD,J=8,7, 1,GC), 7,26-7,51 (12H, m), 7,68 (1H, DD, J=7,5,1,5Hz), 8,40 (1H, d, J=8,Hz), of 9.00 (1H, users)
2-43to 1.21 (6H, t, J=7,2Hz), to 2.57 (3H, s)of 2.75 (3H, users), to 2.94 (3H, users), a 3.50 (2H, s), 4,20 (4H, q, J=7,2 Hz), 4,82 (2H, s), 7,00 (1H, d, J=1,GZ), 7,18 (1H, DD, J=8,6, 1,GC), 7,26-to 7.59 (11H, m), 7,70 (1H, DD, J=7,6, 1,5Hz), 7,95 (1H, d, J=8,3 Hz), 8,35 (1H, d, J=8,Hz), 9,13 (1H, users)
2-44of 1.07 (6H, t, J=7,3 Hz), was 2.76 (3H, s), of 2.86 (3H, s), 3,21-3,30 (4H, m), of 3.57 (2H, s), a 4.83 (2H, s), PC 6.82 (1H, d, J=8,3 Hz), 6,98 was 7.45 (16H, m), 8,24 (1H, DD, J=7,8, 1,8gts), 8,44 (1H, d, J=8,5Hz), 10,4 (1H, users)
2-45to 1.22 (6H, t, J=7,1Hz), a 2.75 (3H, s), 2,82 (3H, s), of 3.54 (2H, s), is 4.21 (4H, q, J=7,1Hz), a 4.83 (2H, s), PC 6.82 (1H, d, J=7,Hz), 7,05 (1H, d, J=2,0 Hz), 7,09-7,46 (13H, m), 8,24 (1H, DD, J=7,8, 1,8gts), 8,42 (1H, d, J=8,5Hz), 10,4 (1H, users)

Table 27ExampleStructureNMR (δ, 300MHz, CDC13)2-46to 1.22 (6H, t, J=7,2 Hz), 2,90 (3H, users), of 2.97 (3H, users), 3,52 (2H, S), is 4.21 (4H, q, J=7,2Hz), a 4.83 (2H, s), 7,05 (1H, d, J=1,GZ), 7,20 (1H, DD,J=8,7, 1,GC), 7,29-7,73 (13H, m), with 8.33 (1H, d, J=8,GC), 9,27 (1H, users)2-47to 1.21 (6H, t, J=7,2 Hz), 2,44 (3H, S), 2,77 (3H, users), only 2.91 (3H, users), a 3.50 (2H, s), 4,20 (4H, q, J=7,2 Hz), 4,82 (2H, s), 7,01 (1H, d, J=2,2 Hz), 7,19 (1H, DD,J=8,7, 2,2 Hz), 7,30-to 7.59 (12H, m), 8,35 (1H, d, J=8,Hz), the remaining 9.08 (1H, users)2-48TPL 105-108to 1.21 (6H, t, J=7,1Hz), is 2.44 (3H, S), 2,80 (3H, users), to 2.94 (3H, users), a 3.50 (2H, s), 4,20 (4H, q, J=7,1Hz), 4,82 (2H, s), 7,02 (1H, d, J=2,2 Hz), 7,16-7,30 (8H, m), 7,56-7,63 (5H, m), 8,35 (1H, d, J=8,GC), 9,14 (1H, users)2-49to 2.65 (3H, s), of 2.86 (3H, users), 2,95 (3H, users), 3,6H2H, C), 4,23-4,30 (2H, m), 4,71-rate 4.79 (1H, m), 4,98 ((1H, d, J=7,1Hz), to 7.09 (1H, d, J=1,GZ), 7,18-7,7K14H, m)of 8.37 (1H, d, J=8,Hz), 9,16 (1H, users)2-50to 1.19 (3H, t, J=7,1Hz), of 2.86 (3H, users), 2,95 (3H, users), 3,52 (2H, s)to 3.89 (1H, DD, J=9,1, 6,0 Hz), was 4.02-4,19 (2H, m), 4,34 (1H, DD, J=10,9, 6,0 Hz), 4,58 (1H, DD, J=10,9, 9,1 Hz), 7,06 (1H, d, J=2,3 Hz), 7,18-7,71 (14H, m), at 8.36 (1H, d, J=8,Hz), 9,17 (1H, users)

Table 28
ExampleStructureNMR (δ, 300MHz, CDC13)
2-512,21 is 2.46 (2H, m), 2,64-3,49 (9H, m), 3,55-to 3.58 (2H, m), 4,45-of 5.29 (2H, m), 6,11-to 6.19 (1H, m), 7,12-7,70 (15H, m), 8,33 is 8.38 (1H, m), 9,17 (1H, users ) Conformer
2-52to 1.24 (6H, t, J=7,0 Hz), 1,50-of 1.64 (2H, m), 2,25-of 2.36 (2H, m), 2.77-to to 3.02 (6H, usher.), of 3.54 (2H, s), 3,99-4,08 (2H, m), 4,16-the 4.29 (4H, m), 7,10 (1H, d, J=1,Hz), 7.24 to the 7.43 (7H, m), 7,44-EUR 7.57 (2H, m), to 7.59-to 7.64 (4H, m), 7,68 (1H, DD, J=1,5, 7,2 Hz), at 8.36 (1H, d, J=8,Hz), 9,16 (1H, s)
2-53to 1.21 (6H, t, J=7,0 Hz), 2,82 (3H, users), 2,95 (3H, users), a 3.50 (2H, s), 3,88 (3H, s), is 4.21 (4H, sq J=7,0 Hz), 4,82 (2H, s), 6.87 in (1H, d, J=2,GC), of 6.99 (1H, DD,J=8,5, 2,GC), 7,03 (1H, d, J=1,8gts), to 7.18 (1H, DD, J=8,5, 1,8gts), 7,29-7,69 (10H, m), 8,35 (1H, d, J=8,8gts), 9,17 (1H, users)
2-54to 1.21 (6H, t, J=7,0 Hz), of 2.81 (3H, users), to 2.94 (3H, users), 3,51 (2H, s), 4,20 (4H, q, J=7,0 Hz)of 4.83 (2H, s),? 7.04 baby mortality (1H, d, J=2,2 Hz), 7,19 (1H, DD,J=8,4, 2,2 Hz), 7,30-7,66 (12H, m), with 8.33 (1H, d, J=8,5Hz), 9,29 (1H, users)
2-55< / br>
TPL 102-105
of 1.20 (6H, t, J=7,1Hz), 2,11 (3H, s), is 2.88 (3H, users), totaling 3.04 (3H, users), of 3.48 (2H,s), 4,19 (4H, q, J=7,1Hz), to 4.81 (2H, s),? 7.04 baby mortality (1H, d, J=2,0 Hz), 7,12 (1H, DD, J=2,0 Hz, J=8,5 Hz), 7.24 to to 7.50 (10H, m), 7,60(2H, d, J=8,1 Hz), 8,10 (1H, d, J=8,5Hz), 9,06 (1H, users)

Table 29
ExampleStructureNMR (δ, 300MHz, CDC13)
2-56of 2.81 (3H, users), with 2.93 (3H, users), 3,52 (2H,s), 4,45-4,60 (4H, m), 4,88 (2H, s), 7,02 (1H, d,J=2,0 Hz), 7,19 (1H, DD, J=2,0 Hz, J=8,Hz), 7.23 percent-of 7.64 (12H, m), 7,68 (1H, DD, J=2,0 Hz, J=8,1 Hz), a 8.34 (1H, d, J=8,1 Hz), 9,10 (1H, users)
2-57< / br>
TPL 116,5-119,5
to 1.21 (6H, t, J=7,1Hz), 2,95 (3H, users), a 3.01 (3H, users), 3,52 (2H, s), is 4.21 (4H, q, J=7,1Hz), a 4.83 (2H, s), 7,10 (1H, s), 7,14-7,63 (12H, m) of 7.75 (1H, d, J=6,GC), by 8.22 (1H, d, J=8,Hz), 9,34 (1H, users)
2-58< / br>
TPL 119-121
of 1.23 (6H, t, J=7,1Hz), 2,85 (6H, users), 3,55 (2H, s), 4,22 (4H, q, J=7,1Hz), a 4.83 (2H, s), 7,03 (1H, d, J=7,Hz), 7,24-7,74 (13H, m), at 8.36 (1H, d, J=12,2 Hz), to 9.45 (1H, users)
2-59to 1.22 (6H, t, J=7,1Hz), 2,87 (3H, s), 2,96 (3H, s), 3,51 (2H, s), 4,22 (4H, q, J=7,1Hz), is 4.85 (2H, s), 7,06 (1H, users), 7,25-7,68 (14H, m), to 7.77 (1H, d, J=7,1 Hz)
2-60to 1.22 (6H, t, J=7,1Hz), of 2.86 (3H, users), 2,95 (3H, s), 3,50 (2H, s), 4,22 (4H, q, J=7,1Hz), is 4.85 (2H, s), 7,00 (1H, d, J=1,5Hz), 7,20-7,66 (13H,m), 7,73 (1H, DD, J=1,5 Hz and 7.1 Hz), of 7.97 (1H, users)

ExampleStructureNMR (δ, 300MHz, CDC13)
2-61< / br>
TPL 131-133
to 1.21 (6H, t, J=7,2Hz), is 2.88 (3H, users), of 2.97 (3H, users), 3,52 (2H, s), 4,20 (4H, q, J=7,2Hz), a 4.83 (2H, s), 7,07 (1H, d, J=2,2 Hz), 7.18 in-7,72 (13H, m), with 8.33 (1H, d, J=8,4 Hz), was 9.33 (1H, users)
2-62< / br>
TPL 120-125
to 1.21 (6H, t, J=7,1Hz), 2,87 (3H, users), 2,96 (3H, users), 3,52 (2H, s), is 4.21 (4H, q, J=7,1Hz), a 4.83 (2H, s), 7,07 (1H, d, J=1,8gts), 7,17-7,72 (13H, m), 8,32 (1H, d, J=8,4 Hz), to 9.32(1H, users)
2-63to 1.22 (6H, t, J=7,2 Hz), and 2.83 (3H, users), to 2.94 (3H, users), of 3.48 (2H, s)to 4.23 (4H, q, J=7,Hz), 4,94 (2H, s), 6,98 (1H, d, J=1,GZ), 7,12-7,76 (10H, m), 8,30 (1H, d, J=8,3 Hz), scored 8.38 (1H, DD, J=2,GC, J=8,Hz), the remaining 9.08 (1H, users), which 9.22 (1H, d, J=2,GC)
2-64to 1.21 (6H, t, J=7,2 Hz), and 2.83 (3H, users), to 2.94 (3H, users), of 3.48 (2H, s), 3,49 (1H, users), 3,71 (1H, users), 4,20 (4H, q, J=7,2 Hz), 4,88 (2H, s), 6,83 (1H, DD, J=3,0 Hz, J=8,3 Hz), 7,03 (1H, d, J=1,GZ), 7,11-7,72 (10H, m), 7,83 (1H, d, J=3,1 Hz), of 8.25 (1H, d, J=8,Hz), 9,14 (1H, users)
2-65< / br>
TPL 149-155
to 1.21 (6H, t, J=7,2 Hz), and 2.83 (3H, users), with 2.93 (3H, users), to 3.49 (2H, s), is 4.21 (4H, q, J=7,2Hz), is 4.93 (2H, s), 7,03 (1H, d, J=1,GZ), 7,13-7,73 (12H, m), with 8.33 (1H, d, J=8,Hz), of 8.47 (1H, d, J=3,8gts), 9,17 (1H, users)

Table 31
ExampleStructureNMR (δ, 300MHz, CDC13)
2-66of 1.23 (6H, t, J=7,2Hz), is 2.88 (3H, s), of 2.97 (3H, s), 3,61 (2H, s)to 4.23 (4H, q, J=7,2Hz), is 4.85 (2H, s), 7,03 (1H, d, J=7,1 Hz), 7.23 percent-of 7.68 (12H, m), 7,74 (1H, DD, J=1,1 Hz, J=7,5 Hz),to 7.84 (1H, users)
2-67of 1.23 (6H, t, J=7,2Hz), is 2.88 (3H, s), 2,96 (3H, s), 3,62 (2H, s)to 4.23 (4H, q, J=7,2Hz), is 4.85 (2H, s), to 7.09 (1H, d, J=7,5 Hz), 7.24 to 7,68 (12H, m),7,74-7,80 (2H, m)
2-68to 1.22 (6H, t, J=7,2 Hz), and 2.26 (3H, s)2,84 (3H, users), 2,95 (3H, users), of 3.48 (2H, s), 4,10-br4.61 (4H, m), 4,88 (2H, s), 6,99-7,73 (14H, m), 8,43 (1H, d, J=8,3 Hz), 9,18 (1H, users)
2-69to 1.21 (6H, t, J=7,2 Hz), 2,32 (3H, S), of 2.81 (3H, users), with 2.93 (3H, users), 3,51 (2H, s), 4,20 (4H, q, J=7,2Hz), to 4.81 (2H, s), 7,01-7,74 (14H, m), at 8.36 (1H, d, J=8,3 Hz), 9,19 (1H, users)
2-70to 1.21 (6H, t, J=7,2 Hz), of 2.33 (3H, s), 2,82 (3H, users), to 2.94 (3H, users), 3,51 (2H, s), 4,20 (4H, q, J=7,2Hz), to 4.81(2H, s), 7,01-7,74 (14H, m), 8,35 (1H, d, J=8,3 Hz), 9,19 (1H, users)

Table 32
ExampleStructureNMR (δ, 300MHz, CDC13)
2-71 to 1.24 (6H, t, J=7,2 Hz), 2,84 (3H, users), 2,95 (3H, users), 3,44 (2H, s), 4,12-of 4.35 (4H, m), 4,94 (2H, s), 7,00 (1H, d, J=2,2 Hz), 7,05-7,73 (13H, m), 8,31 (1H, d, J=8,3 Hz), 9,19 (1H, users)
2-72< / br>
TPL 122,2-125,0
to 1.22 (6H, t, J=7,1Hz), of 2.81 (3H, users), to 2.94(3H, users), 3,51 (2H, s), is 4.21 (4H, q, J=7,1Hz), 4,80 (2H, s), 7,03 (1H, d, J=2,2 Hz), 7,14-to 7.64 (12H, m), of 7.70 (1H, DD, J=1,Hz, J=7,2 Hz), at 8.36 (1H, d, J=8,Hz), 9,19 (1H, users)
2-73< / br>
TPL 132,0-RUR 134.4
to 1.21 (6H, t, J=7,2 Hz), 2,80 (3H, users), to 2.94 (3H, users), a 3.50 (2H, s), 4,20 (4H, q, J=7,2 Hz), 4,80 (2H, s), 7,02 (1H, d, J=2,3 Hz), 7.18 in-7,71 (13H, m), at 8.36 (1H, d, J=8,3 Hz), 9,18 (1H, users)
2-74of 1.16 (3H, t, J=7,0 Hz), of 1.18 (3H, t, J=7,2 Hz), 2,82 (3H, users), with 2.93 (3H,users), totaling 3.04 (1H, d, J=16,5 Hz), 3,20 (H, d, J=16,5 Hz), of 3.46 (2H, s), 4.04 the-4,20 (4H, m), and 4.75 (1H, d, J=11,4 Hz), 4,82 (1H, d, J=11,4 Hz), 6,98 (1H, d, J=2,2 Hz), 7,11-7,72 (14H, m), a 8.34 (1H, d, J=8,8gts), 9,17 (1H, users)
2-75TPL to 121.0-124,0to 1.22 (6H, t, J=7,1Hz), 2,84 (3H, users), to 2.94 (3H, users), 3,44 (2H, S), 3,74 (3H, s), 4,22 (4H, q, J=7,1Hz), to 4.81 (2H, s), 6,84-7,71 (14H, m), 8,32 (1H, d, J=8,Hz), 9,18 (1H, users)

Table 33
ExampleStructureNMR (δ, 300MHz, CDC13)
2-76to 1.21 (6H, t, J=7,1Hz), 2,82 (3H, users), to 2.94 (3H, users), 3,51 (2H, s), of 3.77 (3H, s), 4,20 (4H, q, J=7,1Hz), to 4.81 (2H, s), 6,83-6,91 (3H, m),? 7.04 baby mortality (1H, d, J=1,GZ), 7,18-7,71 (10H, m), 8,35 (1H, d, J=8,3 Hz), 9,19 (1H, users)
2-77to 1.21 (6H, t, J=7,1Hz), 2,80 (3H, users), with 2.93 (3H, users), 3,51 (2H, s), with 3.79 (3H, s), 4,20 (4H, q, J=7,1Hz), 4,80 (2H, s), at 6.84 (2H, dt, J=8,Hz, J=3,4 Hz), 7,03 (1H, d, J=1,GZ),7,19-7,71 (11H, m), at 8.36(1H, d, J=8,Hz), 9,18 (1H, users)
2-78TPL 118-119to 1.21 (6H, t, J=7,2 Hz), 2,82 (3H, users), to 2.94 (3H, users), 3,52 (2H, s), is 4.21 (4H, q, J=7,2Hz), a 4.83 (2H, s), 7,05 (1H, s), 7,19-7,30 (6H, m), to 7.61-7,84 (7H, m), a 8.34 (1H, d, J=8,3 Hz), 9,40 (1H, users)
2-79TPL 135-138of 1.20 (6H, t, J=7,2 Hz), 2,86 (3H, users), 3,06 (3H, users), 3,50 (2H,C)4,20 (4H, q, J=7,2 Hz), 4,82 (2H, s), 7,06 (1H, s), to 7.15 (1H, DD, J=2.1 a,8,3 Hz), 7,28-7,63 (12H, m)to 8.14 (1H, d, J=8,3 Hz), a 9.25 (1H, users)
2-80TPL 128-130to 1.21 (6H, t, J=7,0 Hz), and 2.83 (3H, users), of 3.00 (3H, users), 3,51 (2H, s), is 4.21 (4H, q, J=7,0 Hz), 4,82 (2H, s), 7,05 (1H, d, J=2,2 Hz), 7,19 (1H, DD, J=2,2, 8,4 Hz), 7,25-7,65 (12H, m), of 8.27 (1H, d, J=8,4 Hz), 9.28 are (1H, users)

Table 34
ExampleStructureNMR (δ, 300MHz, CDC13)
2-81 to 1.24 (6H, t, J=7,2 Hz), 2,44 (3H, s), 2,61 (3H, t, J=7,1Hz), of 2.86 (3H, users), 2,95 (3H, users), of 3.46 (2H, s)4,07 (2H, t, J=7,1Hz), to 4.23 (4H, q, J=7,2 Hz), 4,82 (2H, s), 7,07-7,63 (14H, m), of 8.37 (1H, d, J=8,Hz), 9,12 (1H, users)
2-82to 1.21 (6H, t, J=7,1Hz), a 1.45 (3H, t, J=7,2 Hz), of 2.81 (3H, users), 2,95 (3H, users), a 3.50 (2H, s), 4,11 (2H, q, J=7,2Hz), is 4.21 (4H, q, J=7,1Hz), 4,82 (2H, s)6,86 (1H, d, J=2,GC), 6,97 (1H, DD, J=2,6, 8,GC), 7,03 (1H, d, J=1,GZ), 7,18 (1H, DD, J=1,9, 8,GC), 7,28-7,30 (5H, m), 7,56-to 7.67 (5H, m), at 8.36(1H, d, J=8,Hz), 9,17 (1H, users)
2-83to 1.21 (6H, t, J=7,2 Hz), of 1.28 (6H, d, J=6,0 Hz), of 2.81 (3H, users), 2,95 (3H, users), is 4.21 (4H, q, J=7,2 Hz), with 4.64 (1H, Sept, J=6,0 Hz), 4,82 (2H, s), 6,85 (1H, d, J=2,2 Hz), of 6.96 (1H, DD,3=2,6,8,GC), 7,03 (1H, d, J=2,2 Hz), 7,18 (1H, DD, J=8,7, 1,GC), 7,28-7,30 (5H, m), 7,56-7,66 (5H, m), at 8.36 (1H, d, J=8,3 Hz), 9,16(1H, users)
2-84to 1.24 (6H, t, J=7,2 Hz), 2,61 (2H, t, J=7,1Hz), 2,89 (3H, users), to 2.94 (3H, users), 3,47 (2H, s)4,08 (2H, t, J=7,1Hz), 4,24 (4H, q, J=7,2 Hz), 7,11-7,39 (7H, m), to 7.61-7,83 (7H, m), a 8.34 (1H, d, J=8,GC), 9,36 (1H, users)
2-85< / br>
TPL 107-109
of 1.20 (6H, t, J=7,2 Hz), of 2.81 (3H, users), to 3.02 (3H, users), to 3.49 (2H, s), of 3.78 (3H, s), 4,20 (4H, q, J=7,2Hz), to 4.81 (2H, s), 7,02 (1H, d, J=1,GZ), 7,07 (1H, d, J=8,3 Hz), to 7.15 (1H, DD, J=2,3, 8,GC), 7,24-7,30 (6H, m), 7,41-of 7.60 (5H, m), by 8.22 (1H, d, J=8,Hz), 9,05 (1H, users)

Table 35
ExampleStructureNMR (δ, 300MHz, CDC13)
2-86< / br>
TPL 125-129
to 1.21 (6H, t, J=7,2 Hz), 2,48 (3H, s), 2,69 (3H, users), only 2.91 (3H, users), a 3.50 (2H, s), is 4.21 (4H, q, J=7,2 Hz), 4,82 (2H, s), of 6.99 (1H, d, J=2,2 Hz), 7,20 (1H, DD, J=1,5, 8,3 Hz), 7,28-7,41 (8H, m), EUR 7.57-to 7.64 (4H, m), 8,18 (1H, d, J=8,Hz), 8,81 (1H, users)
2-87of 1.23 (6H, t, J=7,2 Hz), of 3.00 (3H, users), 3,03 (3H, users), to 3.58(2H, s), 4,22 (4H, q, J=7,2Hz), is 4.85 (2H, s), 7,18 (1H, d, J=1,GZ), 7,28-7,33 (6H, m), 7,79 (1H, d, J=7,Hz), 7,92 (1H, d, J=7,Hz), to 7.99 (1H,C)8,35 (1H, d, J=8,3 Hz), 9,46 (1H, s)
2-88< / br>
t, pl. 129-131
to 1.21 (6H, t, J=7,2 Hz), of 2.33 (3H, s), was 2.76 (3H, users), with 2.93 (3H, users), a 3.50 (2H, s), is 4.21 (4H, sq J=7,2 Hz), 4,82 (2H, s), of 6.99 (1H, d, J=1,2 Hz), 7,14-7,51 (13H, m), the 7.65 (1H, d, J=7,Hz), to 8.34 (1H, d, J=8,Hz), 8,78 (1H, users)
2-89< / br>
TPL 81-82
to 1.24 (6H, t, J=7,2) of 1.29 (3H, t, J=7,GC),

of 2.92 (2H, q, J=7,GC),

3,03 (6H, users),

of 3.57 (2H, s) to 4.23 (4H, kV, 7,2 Hz), is 4.85 (2H, s),

7,18 1H, d, 2,3 Hz),

7,27-7,33 (6H, m)

7,51-of 7.60 (3H, m)

to 8.40 (1H, q, j 8,2 Hz),

of 9.51 (1H, users)
2-90< / br>
TPL 110-112
to 1.21 (6H, t, J=7,1Hz), to 1.22 (3H, t, J=6,GC), 2,64 (H, kV, J=6,GC), a 2.75 (3H, users), with 2.93 (3H, users), 3,5 (2H, C)is 4.21 (4H, q, J=7,1Hz), 4,82 (2H, s), of 6.99 (1H, d, J=1,8gts), 7,17-7,66 (14H, m), 8,30 (1H, d, J=8,3 Hz), 8,76(1H, users)

Table 36
ExampleStructureNMR (δ, 300MHz, CDC13)
2-91to 1.21 (6H, t, J=7,1Hz), to 2.13 (3H, s), 2,71 (3H, users), 2,89 (3H, users), to 3.49 (2H, s), 4,20 (4H, sq J=7,1Hz), 4,82 (2H, s), 5,10 (1H, s), 5,43 (1H, s), 6,98 (1H, d, J=2,2 Hz), 7,19 (1H, DD, J=1,9, 8,3 Hz), 7,28-7,53 (12H, m), to 7.67 (1H, d, J=7,Hz), 8,39 (1H, d, J=8,Hz), 8,87 (1H, users)
2-92< / br>
TPL 107-110
to 1.21 (6H, t, J=7,1Hz), to 1.21 (6H, t, J=7,1Hz), was 2.76 (3H, users), 2,89 (1H, Sept, J=7,1Hz), to 2.94 (3H, users), a 3.50 (2H, s), is 4.21 (4H, sq J=7,1Hz), 4,82 (2H, s), 7,01(1H, d, J=1,GZ), 7,14-7,51 (13H, m), a 7.62 (1H, d, J=6,4 Hz), 8,21 (1H, d, J=8,3 Hz), to 8.70 (1H, users)
2-93of 1.23 (6H, t, J=7,2 Hz), 2,12 (3H, s)to 2.99 (3H, users), totaling 3.04 (3H, users), of 3.56(2H, s)to 4.23 (4H, q, J=7,2Hz), is 4.85 (2H, s), 5,15 (1H, s), 5,23(1H, s), to 7.15 (1H, d, J=1,8gts), 7,25-7,31 (6H, m), 7,55 (1H with), to 7.61 (1H, d, J=7,Hz), 7,73 (1H, d, J=7,Hz), at 8.36 (1H, d, J=8,3 Hz), a 9.35 (1H, m)
2-94to 1.24 (6H, t, J=7,2 Hz), of 1.29 (6H, t, J=6,8gts), 3,03 (6H, users), 3,44 (1H, Sept, J=6,8gts), of 3.57 (2H, s)to 4.23 (4H, q, J=7,2Hz), is 4.85 (2H, s), 7,18 (1H, d, J=1,GZ), 7,26-7,33 (6H, m), 7,52 (2H, ), 7,63 (1H, s), to 8.41 (1H, d, J=8,3 Hz), 9,44 (1H, users)
2-95 of 1.23 (6H, t, J=7,1Hz), a 3.01 (3H, users), 3,10 (3H, users), of 3.57 (2H, s)to 4.23 (4H, q, J=7,1Hz), is 4.85 (2H, s), 6,91-of 6.96 (1H, m), 7,20-7,41 (12H, m), 7,46 (1H, s), 7,66 (1H, d, J=7,Hz), 8,29 (1H, d, J=8,3 Hz), 9,78 (1H, s), 10,17(1H, users)

Table 37
ExampleStructureNMR (δ, 300MHz, CDC13)
2-96to 1.21 (6H, t, J=7,1Hz), a 2.75 (3H, users), to 3.02 (3H, users), 3,55 (2H, s), 4,20 (4H, q, J=7,1Hz), 4,84 (2H, S),6,92 (1H, d, J=8,3 Hz), 7,15-7,68 (14H, m), 8,07 (1H, DD, J=1,3, 7,GC)
2-97to 1.22 (6H, t, J=7,1Hz), and 2.83 (3H, users), of 2.86 (3H, users), 3,53 (2H, s), is 4.21 (4H, q,J=7,1Hz), a 4.83 (2H, s), 6,85 (1H, d, J=7,Hz), 7,07 (1H, d, J=2,0 Hz), 7,20-7,52 (12H, m), of 8.25 (1H, DD, J=1,8, 7,GC), to 8.41 (1H, d, J=8,5Hz), 10,48 (1H, users)
2-98of 0.65 (6H, t, J=7,4 Hz), 1.69 in (4H, q, J=7,4 Hz), of 2.81 (3H, users), to 2.94 (3H, users), a 3.50 (2H, s), 4,30 (2H, s), 7,02 (1H, d, J=1,8gts), 7,18 to 7.62 (13H, m), of 7.70 (1H, d, J=7,3 Hz), 8,35 (1H, d, J=8,5Hz), to 9.15 (1H, users)
2-99to 1.21 (6H, t, J=7,1Hz), 2,87 (6H, users), 3,53 (2H, s), is 4.21 (4H, q, J=7,1Hz), a 4.83 (2H, s), 6,92 (1H, d, J=7,GC), was 7.08 (1H, d, J=2,1 Hz), 7,20-of 7.48 (10H, m), 7,63 (2H, d, J=8,Hz), 8,23 (1H, DD, J=1,7, 7,GC), 8,35 (1H, d, J=8,5Hz), 10,38 (1H, users)
2-100 0,85-0,93 (4H, m), 2,78 (3H, users), with 2.93 (3H, users), 3,52 (2H, s)to 4.16 (2H, s),? 7.04 baby mortality (1H, d, J=2,1 Hz), 7,17-to 7.61 (13H, m), of 7.70 (1H, DD, J=1,5, 7,2 Hz), 8,35 (1H, d, J=9,0 Hz), to 9.15 (1H, users)

Table 38
ExampleStructureNMR (δ, 300MHz, CDC13)
2-101and 2.79 (3H, users), to 2.94 (3H, users), of 3.45 (2H, s), or 4.31 (1H, t, J=7,Hz), to 4.62 (2H, d, J=7,Hz), of 6.96 (1H, d, J=2,0 Hz), 7,15-7,69 (19H, m), 8,30 (1H, d, J=8,5Hz), to 9.15 (1H, users)
2-102< / br>
MP.. 103,0-109,0
1,62 to 1.76 (4H, m), 1,82 of 1.99 (4H, m), 2,78 (3H, users), with 2.93 (3H, users), 3,44 (2H, s)4,08 (2H, s), 6,97 (1H, d, J=2,0 Hz), 7,09-7,26 (6H, m), 7,35-7,72 (8H, m), a 8.34 (1H, d, J=8,5Hz), to 9.15 (1H, users)
2-103is 2.40 (1H, t, J=5,GC), 2,42 (1H, (2H, t, J=6,3 Hz), 3,53 (2H, s), 2,80 (3H, users), with 2.93 (3H, users), 3,82 (2H, DD, J=6,3, 11,4 Hz), of 3.96 (2H, DD, J=5,7, 11,4 Hz), 4,58 (2H, s), 7,01 (1H, d, J=1,8gts), 7,14-7,71 (14H, m), 8,29 (1H, d, J=8,4 Hz), 9,05 (1H, users)
2-104to 1.98 (6H, s), and 2.83 (3H, users), with 2.93 (3H, users), to 3.49 (2H, s), and 4.40 (4H, s), of 4.44 (2H, s), 7,00 (1H, d, J=2,2 Hz), to 7.15 (1H, DD, J=2,2, 8,4 Hz), 7,22-7,65 (12H, m), of 7.70 (1H, DD, J=1,9, 7,0 Hz), 8,32 (1H, d, J=8,4 Hz), 9,13 (1H, users)
2-105< / br>
TPL 98,8-103,3
of 1.23 (6H, t, J=7,1Hz), and 2.83 (3H, users), to 2.94 (3H, users), 3,51 (2H, S), 4,22 (4H, q,J=7,1Hz),4,82 (2H, s), 6,94? 7.04 baby mortality (3H, m), 7,16-7,71 (10H, m), a 8.34 (1H, d, J=8,5Hz), 9,17 (1H, users)

Table 39
ExampleStructureNMR (δ, 300MHz, CDC13)
2-106MP..116,1-to 121.6to 1.22 (6H, t, J=7,1Hz), of 2.81 (3H, users), with 2.93 (3H, users), a 3.50 (2H, s), 4,20 (4H, q, J=7,1Hz), 4,79 (2H, S), 7,01? 7.04 baby mortality (2H, m), 7,25-7,71 (11H, m), 8,35 (1H, d, J=8,5Hz), 9,17 (1H, users)
2-107of 1.25 (6H, t, J=7,1Hz), a 2.75 (3H, users), of 2.92 (3H, users), of 3.78 (2H, s), 4,22 (4H, q, J=7,1Hz), is 4.85 (2H, S), 6,98 (1H, s), 7,28-7,72 (13H, m)8,71 (1H, s)9,52 (1H, users)
2-108to 1.22 (6H, t, J=7,2Hz), to 2.13 (3H, s), 2,85 (3H, users), with 2.93 (3H, users), a 3.50 (2H, s), 4,16-4.26 deaths (4H, m), 4,80 (2H, s), is 6.78 (1H, d, J=5,1 Hz), 7,05 (1H, d, J=2,2 Hz), to 7.15 (1H, d, J=5,2Hz), 7,16-to 7.64 (8H, m), of 7.69 (1H, DD, J=1,5, 7,3 Hz), with 8.33 (1H, d, J=8,5Hz), 9,16 (1H, users)
2-109< / br>
TPL 104,6-108,3
to 1.22 (6H, t, J=7,2 Hz), 2,44 (3H, s)2,84 (3H, users), to 2.94 (3H, users), 3,52 (2H, s), 4,20 (4H, q, J=7,2 Hz), 4,78 (2H, s), to 6.58 (1H, DD, J=1,2,3,5Hz), 6,76(1H, d,

J=3,5 Hz),? 7.04 baby mortality (1H, d, J=2,0 Hz), 7,20 (1H, DD, J=2.1 a,8,GC), 7,37 to 7.62 (7H, m), 7,68 (1H, DD, J=1,4, 7,GC), with 8.33 (1H, d, J=8,4 Hz), 9,17 (1H, users)
2-110 < / br>
TPL 121,5-of 124.7
to 1.22 (6H, t, J=7,1Hz), 2,85 (3H, users), to 2.94 (3H, users), of 3.46 (2H, s)to 4.23 (4H, q, J=7,1Hz), equal to 4.97 (2H, s), 7,00 (1H, d, J=2,2 Hz), 7,13-7,16 (1H, m), of 7.36 (1H, d, J=3,3 Hz), 7,38-7,71 (8H, m)7,75 (1H, d, J=3,3 Hz), 8,31 (1H, d, J=8,5Hz), 9,16 (1H, users)

Table 40
ExampleStructureNMR (δ, 300MHz, CDC13)
2-111< / br>
TPL 96-98
0,97(6N, d, J=7,2Hz), to 1.21 (6H,t,J=7,2Hz), a 2.45 (1H, Sept, J=7,2Hz), is 2.88 (3H, users), to 2.94 (2H, users), 3,52 (2H, s), is 4.15 (4H, q, J=7,2 Hz), 4,50 (2H, s), to 7.09 (1H, d, J=2,3 Hz), 7,20-7,72 (9H, m), a 8.34 (1H, d, J=8,3 Hz), to 9.15 (1H, users)
2-112< / br>
TPL 100-104,5
of 0.90(3H, t, J=7,2Hz), to 0.92 (3H, t, J=6,5 Hz), 0,95-1,10 (1H, m)to 1.21 (3H, t, J=7,2 Hz), 1,48-of 1.62 (1H, m), 2.05 is-of 2.16 (1H, m), is 2.88 (3H, users), to 2.94 (3H, users), 3,52 (2H, s), 4,14 (4H, q, J=7,2 Hz), 4,51 (2H, s), to 7.09 (1H, d, J=1,GZ), 7,21-7,72 (9H, m), at 8.36 (1H, d, J=8,3 Hz), 9,16 (1H, users)
2-113< / br>
TPL 106-109,5
of 0.83 (6H, d, J=6,4 Hz), to 1.21 (6H, t, J=7,2 Hz), 1,51-of 1.65 (1H, m), a 1.88 (2H, d, J=6,4 Hz), is 2.88 (3H, users), to 2.94 (3H, users), 3,53 (2H, s), is 4.15 (4H, q, J=7,2Hz), to 4.52 (2H, s), was 7.08 (1H, d, J-2,3 Hz), 7,22-7,71 (9H, m), of 8.37 (1H, d, J=8,3 Hz), 9,16 (1H, users)
2-114< / br>
TPL 98-99,5
to 0.88 (3H, t, J=7,2 Hz) of 1.09 to 1.31 (2H, m)to 1.21 (6H, t, J=7,2 Hz), 1,79-of 1.93 (2H, m), 2,89 (3H, users), to 2.94 (3H, users), 3,53 (2H, s), is 4.15 (4H, q, J=7,2 Hz), of 4.49(2H, s), to 7.09 (1H, users), 7,21-7,74 (9H, m), of 8.37 (1H, d, J=8,3 Hz), to 9.15 (1H, users)
2-115< / br>
TPL86,5 to 90.0
of 0.83 (3H,t,J=7,5 Hz), to 1.21 (6H,t,J=7,2Hz), a 1.96 (2H, q, J=7,5 Hz), is 2.88 (3H, users), to 2.94 (3H, users), 3,53 (2H, s)to 4.16 (4H, q, J=7,2 Hz), 4,50 (2H, s), was 7.08 (1H, d, J=1,GZ), 7,21-7,74 (9H, m), at 8.36 (1H, d, J=8,Hz), to 9.15 (1H, users)

Table 41
ExampleStructureNMR (δ, 300MHz, CDC13)
2-116< / br>
TPL 97,5-98,0
0,86 (3H, t, J=7,2 Hz), 1,06-of 1.36 (4H, m)to 1.21 (6H, t, J=7,2 Hz), 1,84-of 1.94 (2H, m), is 2.88 (3H, users), to 2.94 (3H, users), 3,53 (2H, s), is 4.15 (4H, q, J=7,2 Hz), of 4.49 (2H, s), was 7.08(1H, d, J=2,3 Hz), 7,21-7,71 (9H, m), of 8.37 (1H, d, J=8,Hz), 9,16(1H, users)
2-117< / br>
TPL 76,9-82,0
to 1.21 (6H, t, J=7,1Hz), to 2.67 (2H, d, J=7,4 Hz), 2,87(3H, users), 2,95 (3H, users), of 3.54 (2H, s), 4,10-4,20 (4H, m), 4,47(2H, s), 5,00-5,10 (2H, m), 5,56-5,67 (1H, m), to 7.09 (1H, d, J=2,1 Hz), 7,24 (1H, d, J=2,0 Hz), 7,38-to 7.68 (7H, m), of 7.70 (1H, d, J=1,4 Hz), of 8.37 (1H, d, J=8,4 Hz), 9,14 (1H, users)
2-1181,25 (9H, t, J=7,2 Hz), 2,89 (3H, users), 2,95 (3H, users), of 3.56 (2H, s), 4,23 (6H, q, J=7,2 Hz), 4,70 (2H, s), 7,11 (1H, d, J=1,8gts), from 7.24 (1H, d, J=2,2 Hz), 7,28-of 7.70 (8H, m), at 8.36(1H, d, J=8,8gts), 9,16 (1H, users)
2-119< / br>
TPL 72,3-78,6
of 0.87 (3H, t, J=7,2Hz), to 0.92 (3H, t, J=6,8gts), and 1.00-to 1.16 (2H, m)of 1.20 (6H, t, J=7,1Hz), 1,38-of 1.53 (2H, m), 2,18-of 2.23 (1H, m), is 2.88 (3H, users), 2,95 (3H, users), 3,52 (2H, s), 4,08-4,18 (4H, m), 4,50 (2H, d, J=2,1 Hz), was 7.08 (1H, d, J=1,GZ), 7,22-of 7.69 (9H, m), 8,35 (1H, d, J=8,Hz), to 9.15 (1H, users)

Example 3

Diethyl ether 2-(2-{3-ethoxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid

a) Methyl ester of 3-ethoxy-4-nitrobenzoic acid

To a suspension of sodium hydride (60% in mineral oil, 1.20 g) in dimethylformamide (50 ml) was added methyl ether 3-hydroxy-4-nitrobenzoic acid (4,93 g) under ice cooling, and the mixture was stirred at room temperature for 30 minutes. After adding iodine ethyl (4.4 g) the solution was stirred at 60°C overnight, cooled to room temperature, poured into saturated aqueous solution of ammonium chloride and was extracted with a mixture of ethyl acetate-tetrahydrofuran. The organic layer was washed with a saturated aqueous solution of ammonium chloride and a saturated salt solution, dried over sodium sulfate and concentrated, obtaining a solid, which was washed with a mixture of ethyl acetate-hexane, obtaining the methyl ester of 3-ethoxy-4-nitrobenzoic acid (3,30 g) as pale as the addition of a solid substance.

b) the acid chloride of 3-ethoxy-4-nitrobenzoic acid

The acid chloride 3-ethoxy-4-nitrobenzoic acid was obtained in a manner analogous to the one described in example 1f and example 1d), methyl ester 3-ethoxy-4-nitrobenzoic acid obtained in example 3A).

C) 2'-Diazo-3-ethoxy-4-nitroacetophenone

The solution of acid chloride of 3-ethoxy-4-nitrobenzoic acid (2,06g)obtained in example 3b) in diethyl ether (30 ml) was added dropwise to a mixture of diazomethane in diethyl ether (0.35 M, 64 ml) and triethylamine (3.12 ml) under cooling with ice. The mixture was stirred for 2 hours under ice cooling, and the temperature was raised to room, followed by stirring overnight. After adding acetic acid (1 ml) and the mixture was stirred at room temperature for one hour and evaporated to remove solvent. The residue was purified column chromatography on silica gel using a mixture of hexane:ethyl acetate=5:2, getting mentioned in the title compound (1.80 g) as a yellow solid.

d) Ethyl ester of 3-ethoxy-4-nitrophenylarsonic acid

A solution of silver benzoate (270 mg) in triethylamine (2.7 ml) was added dropwise in 10 individual doses to a solution of 2'-diazo-3-ethoxy-4-nitroacetophenone (1,80 g), the scientists in example 3C), in ethanol (25 ml) at boiling under reflux. The mixture was heated at the boil under reflux for 9 hours, and the reaction solution was filtered through a layer of celite. The filtrate was concentrated, and the concentrate was diluted with diethyl ether and washed with 10%aqueous sodium carbonate solution, water and saturated salt solution. The organic layer was dried over sodium sulfate and purified column chromatography on silica gel using a mixture of hexane:ethyl acetate=4:1, getting mentioned in the title compound (1.27 g) as a yellow solid.

e) Ethyl ester of 4-amino-3-ethoxyphenylacetic acid

Ethyl ester of 3-ethoxy-4-nitrophenylarsonic acid (1.27 g)obtained in example 3d), was subjected to reactions similar to those described in example 1-3d), getting mentioned in the title compound (1.12 g) as a brown oil.

Diethyl ether 2-(2-{3-ethoxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid

Ethyl ester of 4-amino-3-ethoxyphenylacetic acid obtained in example 3E), and diethyl ester of 2-hydroxymethyl-2-phenylmalonate acid obtained in example 1-2A)were subjected to interaction method similar to that described in examples 1E), 1f) and 1g), receiving specified in the header with the Association (strength of 0.159 g) (see table 42).

Example 3-2

2,2-Bisericani-2-phenethyl ether {3-hydroxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid

2,2-Bisericani-2-phenethyl ester (3-benzyloxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid (300 mg)obtained by the method similar to that described in example 3, except that the restoration of the nitro group was carried out with the iron powder were subjected to interaction method similar to that described in example 1-2C), getting mentioned in the title compound (244 mg) (see table 42).

Examples 3-3 3-16 on

Connection examples 3-3 3-16 on was obtained by methods similar to those described in examples 3 and 3-2. Thus obtained compounds are shown in tables 42-45.

Table 42
ExampleStructureNMR (δ, 300MHz, CDC13)
3to 1.19 (6H, t, J=7,1Hz), of 1.20 (3H, t, J=7,1Hz), to 3.49 (2H, s), of 3.77 (2H, q, J=7,1Hz), 4,18 (4H, q, J=7,1Hz), a 4.83 (2H, s), 6,59 (1H, d, J=1,5Hz), to 6.75 (1H, DD, J=1,5, 8,2 Hz), 7,25-7,33 (5H, m), 7,44 (1H, DD, J=1,5, 7,2 Hz), 7,49-7,66 (6H, m), 7,70-7,76 (1H, m), 7,80 (1H, DD, J=1,5, 7,2 Hz), 8,35 (1H, d, J=8,0 Hz)
3-2of 1.05 (6H, t, J=7,2 Hz), 3,23 (4H, d to the, J=7,2, 7,2 Hz), of 3.48 (2H, s, a 4.83 (2H, s), 6.48 in (1H, d, J=7,Hz), 6,55 (1H, DD, J=7,9, 1,GC), 6,77 (1H, d, J=1,5Hz), 7,17-7,86 (15H, m),8,58 (1H, )
3-3< / br>
MP..112-114
of 1.05 (6H, t, J=7,2 Hz), 3,23 (4H, d of q, J=7,2, 7,2 Hz), 3,53 (2H, s), 3,55 (3H, s), a 4.83 (2H, s), 6,60 (1H, s), of 6.73 (1H, d, J=7,Hz), 7,10-7,66 (15H, m), a 7.85 (1H, DD, J=7,5, 1,5Hz), with 8.33 (1H, d, J=7,Hz)
3-4to 1.19 (6H, t, J=6,GC), 3,50 (5H, s), 4,17 (4H, q, J=6,GC), a 4.83 (2H, s), to 6.58 (1H, s), of 6.75 (1H, d, J=6,GC), 7,26-the 7.65 (13H, m), a 7.85 (1H, d, J=7,3 Hz), 8,31 (1H, d, J=8,1 Hz)
3-5from 0.84 (6H, t, J=7,2 Hz), USD 1.43 (4H, t kV, J=7,2, 7,2 Hz), and 3.16 (4H, m), 3,52 (2H, s), 3,55 (3H, s), a 4.83 (2H, s), 6,60 (1H, users), 6,72 (1H, DD, J=8,3, 1.5 Hz), 7,12-7,66 (15H, m), to 7.84 (1H, DD, J=7,9, 1,GC), with 8.33 (1H, d, J=7,Hz)

Table 43
ExampleStructureNMR (δ, 300MHz, CDC13)
3-6of 1.13 (6H, t, J=7,2Hz), to 2.55 (2H, t, J=8,0 Hz), 3,30 (4H, d of q, J=7,2, 7,2 Hz), 3,53 (2H, s), of 3.57 (3H, s), of 4.12(2H, t, J=8,0Hz), to 6.67 (1H, users), PC 6.82 (1H, DD, J=8,3, 1,GC), 7,26-7,66 (15H, m), to 7.84 (1H, DD, 3=1,9, 1,GZ), with 8.33(1H, d, J=7,Hz)
3-7of 1.05 (6H, t, J=7,2 Hz), 1,24 (3H, t, J=7,1Hz), 3,17-3,29 (4H, m), 3,52 (2H, s), 3,83 (2H, q, J=7,1Hz), 4,82 (2H, s), 6,60 (1H, d, J=1,5Hz), 6,69-6,76 (1H, m),? 7.04 baby mortality-7,14(2H, m), 7,15-7,22 (2H, m), 7,25-7,34 (3H, m), 7,41-7,47 (1H, m), 7,49-7,66 (6H, m), 7,73 (1H, users), to 7.77-7,83 (1H, m), of 8.37 (1H, d, J=8,3 Hz)
3-8of 1.13 (6H, t, J=7,2 Hz), 1,24 (3H, t, J=7,1Hz), 2,49 at 2.59 (2H, m), and 3.31 (4H, d sq J=5,3, 7,2 Hz), 3,52 (2H, s), a 3.87 (2H, q, J=7,1Hz), 4,07-4,17 (2H, m), of 6.68 (1H, d, J=1,5Hz), 6,78-6,84 (1H, m), of 7.23-7,37 (5H, m), 7,41-7,47 (1H, m), of 7.48-7,66 (8H, m), 7,73 (1H, s), 7,76-of 7.82 (1H, m), of 8.37 (1H, d, J=8,3 Hz)
3-9of 1.10(6H, d, J=6,0 Hz), 1,19 (6H, t, J=7,2 Hz), of 3.48 (2H, s), 4,19 (4H, q, J=7,2 Hz), 4,36 (1H, Sept, J=6,0 Hz), 4,82 (2H, s), 6,62 (1H, d, J=1,5Hz), 6,70-6,77 (1H, m), 7,27-to 7.32 (5H, m), 7,41-7,46 (1H, m), 7,49-to 7.67 (6H, m), 7,72-of 7.82 (2H, m), 8,39 (1H, d, J=8,2 Hz)
3-10of 1.05 (6H, t, J=7,2 Hz), of 1.13 (6H, d, J=6,1 Hz), 3,23 (4H, d of q, J=5,6, 7,2 Hz), 3,52 (2H, s), and 4.40 (1H, Sept, J=6,1 Hz), 4,82 (2H, s), 6,62 (1H, d, J=1,5Hz), 6,67 to 6.75 (1H, m), 7,10 (2H, ushort, J=5,GC), 7,16-of 7.23 (2H, m), 7.24 to to 7.35 (3H, m), 7,44 (1H, DD, J=1,5, 7,GC), 7,50-of 7.70 (6H, m), 7,71-of 7.82 (2H, m), 8,40 (1H, d, J=8,3 Hz)

Table 44
ExampleStructureNMR (δ, 300MHz, CDCl3)
3-11of 1.13 (6H, t, J=7,2 Hz), of 1.13 (6H, d, J=6,1 Hz), 2,48-2,60 (2H, m), and 3.31 (4H, d of q, J=5,1,7,2 Hz), 3,52 (2H, s), 4,07-4,17 (2H, m), 4,43 (1H, Sept, J=6,1 Hz), 6,69 (1H, d, J=1,5Hz), 6,79 (1H, DD, J=1,5, 8,3 Hz), 7.23 percent-7,37 (5H, m), 7,41-7,46 (1H, m), of 7.48-to 7.68 (8H, m), 7,72-of 7.82 (2H, m), 8,40(1H, d, J=8,3 Hz)
3-12of 0.90 (3H, t, J=7,4 Hz), of 1.05 (6H, t, J=7,3 Hz), 1,53 was 1.69 (2H, m), 3,16-3,30 (4H,m), 3,53 (2H, in), 3.75 (2H, t, J=6,GC), 4,82 (2H, s), 6,58-6,74 (2H, m), 7,02-7,78 (16H, m), at 8.36 (1H, d, J=8,2 Hz)
3-13the 1.04 (6H, t, J=7,2 Hz), 3,23 (4H, d of q, J=7,2, 7,2 Hz), 3,52 (2H, c), 4,82-a 4.86 (4H, m), 6,70-7,79 (16H, m), 7,71 (1H, users), 7,78 (1H, DD, J=7,1, 1,GC), 8,40 (1H, d, J=8,3 Hz)
3-14to 1.19 (6H, t, J=7,1Hz), to 3.49 (2H, s), 4,17 (4H, q, J=7,1Hz), 4,78 (2H, s), a 4.83 (2H, s)6,70 (1H, d, J=1,GZ), is 6.78 (1H, DD, J=8,3, 1,5Hz), 7,21-EUR 7.57 (12H, m), of 7.70 (1H, users), to 7.77 (1H, DD, J=7,2, 1,GC), scored 8.38 (1H, d, J=8,3 Hz)
3-15of 1.20 (6H, t, J=7,2 Hz), 3,47 (2H, s), 4,19 (4H, q, J=7,2 Hz), 4,82 (2H, s), of 6.29 (1H, d, J=7,Hz), to 6.57 (1H, DD, J=7,9, 1,GC), 6,79 (1H, d, J=1,GZ), 7,18 (1H, users), 7,28-7,74 (11H, m), 7,86 (1H, DD, J=7,9, 1,5Hz), 8,39 (1H, s)

Table 45
ExampleStructureNMR (δ, 300MHz, CDCl3)
3-161,17 (6N, t, J=7,1 Hz), of 3.54 (2H, s), and 3.72 (3H, s)to 4.16 (4H, q, J=7,1 Hz), a 4.83 (2H, s), 6,72-to 6.80 (3H, m), 7,29-7,66 (N, m)to 8.14 (1H, DD, J=1,3 7,7 Hz)

Example 4

2,2-Bisericani-2-phenethyl ester 2-{3-dimethylamino-4-[(4'-triptorelin-carbonyl)amino]phenyl}acetic acid

a) tert-Butyl ether methyl ester of 2-(3-bromo-4-nitrophenyl)malonic acid

Sodium hydride (60%in mineral oil, 0,985 g) suspended in dimethylformamide (20 ml) and added to it a solution of tert-butylmalonate (4,29 g) in dimethylformamide (5 ml) under cooling with ice. After the termination of foam was added to a mixture solution of 2-bromo-4-fluoro-1-nitrobenzene (2,71 g) in dimethylformamide (5 ml) at the same temperature and the mixture was additionally stirred at 60°C for 3 hours and then concentrated. The residue was neutralized 1 N. hydrochloric acid and was extracted with ethyl acetate. The extract was washed with saturated salt solution, dried over sodium sulfate and concentrated. The residue was purified column chromatography on silica gel using a mixture of ethyl acetate:hexane=1:4 to 1:5, receiving specified in the header connection (7,54 g) in the form of oil.

b) Methyl ester of (3-bromo-4-nitrophenyl)acetic acid

tert-Butyl ether methyl ester of 2-(3-bromo-4-nitrophenyl)malonic acid (1.18 g)obtained in example 4A), was dissolved in chloroform (10 ml), was added to the solution triperoxonane acid (10 g) under ice cooling, and the mixture was stirred at room temperature for 5 hours. The reaction mixture was poured in portions into ice and saturated water is the first sodium bicarbonate solution and was extracted with ethyl acetate. The extract was washed with water and saturated salt solution, dried over sodium sulfate and concentrated, obtaining specified in the header connection (0,820 g) as a pale yellow oil.

C) Methyl ester of (3-dimethylamino-4-nitrophenyl)acetic acid

Methyl ether (3-bromo-4-nitrophenyl)acetic acid (0,320 g)obtained in example 4b), was dissolved in tetrahydrofuran (10 ml). To this solution was added triethylamine (0,237 g) and diethylamine (2 M in tetrahydrofuran, of 0.58 ml) and was stirred overnight while heating. The reaction mixture was concentrated and was purified column chromatography on silica gel using a mixture of ethyl acetate:hexane=1:4, receiving specified in the header connection (0,145 g) as an orange oil.

d) Methyl ester of (4-amino-3-dimethylaminophenyl)acetic acid

Methyl ether (3-dimethylamino-4-nitrophenyl)acetic acid (0,245 g)obtained in example 4C), was introduced in the reaction, similar to that described in example 1-3d), receiving specified in the header connection (0,188 g) as a red oil.

e) 2,2-Bisericani-2-phenethyl ester 2-{3-dimethylamino-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid

Methyl ester of (4-amino-3-dimethylaminophenyl)acetic acid (0,188 g), Paul is obtained in example 4d), introduced in the reaction, similar to that described in example 1E), 1f) and 1g), receiving specified in the header connection (0,058 g) (see table 46).

Examples 4-2 4-8

Compounds of examples 4-2 4-8 were obtained by methods similar to those described in example 4. Thus obtained compounds are shown in tables 46-47.

Table 46
ExampleStructureNMR (δ, 300MHz, CDC13)
4the 1.04 (6H, t, J=7,2 Hz), and 2.26 (6H,C)of 3.23 (4H, m), 3,51 (2H, S), a 4.83 (2H, s), 6,86-7,80 (15H, m), 8, 40 (1H, d, J=8,Hz), to 8.45 (1H, users)
4-2of 1.05 (6H, t, J=7,3 Hz), for 1.49 (6H, users), 2,48 (4H, users), 3,24 (4H, d of q, J=7,3, 7,3 Hz), 3,53 (2H, s), 4,84 (2H, S), 6,93 (2H, m), 7,20-7,70 (15H, m), 8,40 (1H, d, J=9,2 Hz), 8,54 (1H, users)
4-3the 1.04 (6H, t, J=7,3 Hz), of 1.76 (4H, m), 2,59 (4H, t, J=6,2 Hz), 3,23 (4H, d of q, J=7,3, 7,3 Hz), 3,51 (2H, s), a 4.83 (2H, s), 4,82 (2H, m), 7,12-7,63 (14H, m), 7,74 (1H, DD, J=7,3, 1,4 Hz), 8,18 (1H, users), 8,30 (1H, d, J=8,1 Hz)
4-4of 1.20 (6H, t, J=7,1Hz), to 1.48 (6H, users), 2,47 (4H, users), to 3.49 (2H, s), 4,19 (4H, q, J=7,1Hz), a 4.83 (2H, s), 6,92-7,72 (15H, m), 8,39 (1H, d, J=8,3 Hz), 8,56 (1H, users)
4-5 of 1.20 (6H, t, J=7,2 Hz), total 1.74 (4H, m), 2.57 m (4H, m), of 3.48 (2H, s), 4,19 (4H, q, J=7,2 Hz), 4,82 (2H, s), make 6.90 (2H, m), 7,30-7,63 (12H, m), 7,74 (1H, DD, J=7,2, 1,5Hz), to 8.20 (1H, users), 8,29 (1H, d, J=8,GC)

Table 47
ExampleStructureNMR (δ, 300MHz, CDC13)
4-6of 1.20 (6H, t, J=7,1Hz), 2,24 (6H, s), of 3.48 (2H, s), 4,19 (4H, q, J=7,1Hz), 4,82 (2H, s), 6,88-6,98 (2H, m), 7,29 (5H, users),the 7.43 (1H, d, J=7,2 Hz), of 7.48-of 7.60 (2H, m), a 7.62 (4H, s), to 7.77 (1H, d, J=7,5Hz), 8,39 (1H, d, J=8,3 Hz), of 8.47 (1H, users)
4-7to 1.21 (6H, t, J=7,0 Hz), 2,38-2,47 (4H, m), 3,51 (2H, s), 3,53-of 3.60 (4H, m), 4,20 (4H, q, J=7,0 Hz), 4,84 (2H, s), 6,93 (1H, s), 7,00 (1H, DD, J=1,5, 7,4 Hz), 7,29-to 7.35 (5H, m), 7,47-to 7.68 (7H, m), 7,73 (1H, DD, J=1,8, 7,4 Hz), 8,42-8,51 (2H, m)
4-8of 0.67 (6H, t, J=7,0Hz), to 1.21 (6H, t, J=7,2 Hz), of 2.64 (4H, q, J=7,0 Hz), 3,49 (2H, s), is 4.21 (4H, q, J=7,2Hz), a 4.83 (2H, s), 6.90 to-7,01 (2H, m), 7,28-to 7.35 (5H, m), 7,42-the 7.65 (7H, m), of 7.69 (1H, DD, J=1,5, 7,2 Hz), to 8.41 (1H, d, J=8,3 Hz), cent to 8.85 (1H, users)

Example 5

Diethyl ether 2-[2-(2-{2-methyl-3-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxy)ethyl]-2-phenylmalonate acid

a) 2'-Diazo-3-nitro-2-methylacetophenone

2-Methyl-3-nitrobenzoic acid (500 mg) was subjected to interactions, analogues of the figures described in example 3b) and 3C), getting listed in the title compound (377 mg).

b) Ethyl ester of 2-methyl-3-nitrophenylarsonic acid

2'-Diazo-3-nitro-2-methylacetophenone (377 mg)obtained in example 5A)were subjected to interactions, similar to that described in example 3d), getting mentioned in the title compound (363 mg).

C) 2-Methyl-3-nitrophenylarsonic acid

Ethyl ester of 2-methyl-3-nitrophenylarsonic acid (352 mg)obtained in example 5b)were subjected to interactions, similar to that described in example 1f), getting mentioned in the title compound (307 mg).

d) Diethyl ether 2-(2-benzyloxyethyl)-2-methylmalonic acid

Sodium hydride (406 mg) was dissolved in dimethylformamide (20 ml)and the solution was cooled to 0°C. To this solution was added diethyl ether of phenylmalonate acid (2.0 g)and the mixture was stirred at room temperature for 30 minutes. Additionally added to the mixture primatively simple ether (2.0 g), was stirred at 60°C for 4 hours and added water. The reaction mixture was concentrated, diluted with ethyl acetate, washed with water, dried over sodium sulfate and purified column chromatography on silica gel using a mixture of ethyl acetate:hexane=9:1, receiving specified in the header is connected to the e (1.2 g).

e) Diethyl ether 2-(2-hydroxyethyl)-2-phenylmalonate acid

Diethyl ether 2-(2-benzyloxyethyl)-2-methylmalonic acid (1.2 g, purified)obtained in example 5d)were subjected to interactions, similar to that described in example 1-2C), getting mentioned in the title compound (726 mg).

f) Diethyl ether 2-{2-[2-(2-methyl-3-nitrophenyl)acetoxy]ethyl}-2-phenylmalonate acid

2-Methyl-3-nitrophenylazo acid (307 mg)obtained in example 5C), 4-dimethylaminopyridine (217 mg) and diethyl ether 2-(2-hydroxyethyl)-2-phenylmalonate acid (250 mg)obtained in example 5e)were subjected to interactions, similar to that described in example 1-3C), getting mentioned in the title compound (366 mg).

g) Diethyl ester 2-[2-(2-{2-methyl-3-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxy)ethyl]-2-phenylmalonate acid

Diethyl ether 2-{2-[2-(2-methyl-3-nitrophenyl)acetoxy]ethyl}-2-phenylmalonate acid (345 mg)obtained in example 5f)were subjected to interactions, similar to that described in example 1-3d 1-3E), getting mentioned in the title compound (318 mg) (see table 48).

Examples 5-2 5-18 on

Compounds of examples 5-2 5-18 on was obtained by methods similar to those described in example 5. Thus obtained compounds before the taulani in tables 48-51.

Table 48
ExampleStructureNMR (δ, 300MHz, CDC13)
5of 1.23 (6H, t, of 1.70 (3H, s), 2,61 (2H, t, J=7,0 Hz), 3,50 (2H, s)4,07 (2H, t, J=7,0Hz), is 4.21 (4H, q, J=7,0 Hz), at 6.84 (1H, users), 6,98 (1H, d, J=7,Hz), 7,13-7,71 (15H, m), 7,80 (1H, d, J=7,0 Hz)
5-2of 1.17 (6H, t, J=7,1Hz), a 3.50 (2H, s), 4,14 (4H, q, J=7,1Hz), a 4.83 (2H, s), 6,83 (1H, s)6,91(1H, d, J=7,5 Hz), 6,99 (1H, users), 7,16-7,81 (15H, m)
5-3TPL 88-91of 1.23 (6H, t, J=7,2 Hz), 2,62 (2H, t, J=7,2Hz), to 3.41 (2H, s), of 4.13 (2H, t, J=7,2 Hz), 4,20 (4H, q, J=7,2 Hz), 7,05-7,79 (18H, m)
5-4of 1.10 (6H, t, J=7,2 Hz), 2,53-2,61 (2H, m), or 3.28 (4H, d of q, J=5,3, 7,2 Hz), of 3.54 (2H, s), 4,07-4,17 (2H, m), 6,95-7,10 (3H, m), 7,14 and 7.36 (7H, m), 7,40-7,46 (1H, m), 7,46 to 7.62 (6H, m), of 7.64-7,71 (2H, m), to 7.77 (1H, DD, J=1,5, 7,5Hz)
5-5of 0.85 (6H, t, J=7,2 Hz), 1,49 (4H, TCEs, J=7,2, 7,2 Hz), of 2.54 2.63 in (2H, m), 3,16-of 3.25 (4H, m), 3,53 (2H, s), 4,08-4,17 (2H, m), of 6.96-7,01 (1H, m), 7.03 is-7,10 (2H, m) 7,15 and 7.36 (7H, m), 7,40-7,46 (1H, m), 7,47-7,62 (6H, m), 7,65-7,71 (2H, m), to 7.77 (1H,

DD, J=1,5, 7,5Hz)

NMR (δ, 300MHz, CDC13)
Table 49
ExampleStructure
5-6to 1.24 (6H, t, J=7,4 Hz), 1,68 (3H, s)to 2.65 (2H, t, J=7,3 Hz), 3,50 (2H, s), 4.09 to (2H, t, J=7,3 Hz), 4,22 (4H, q, J=7,4 Hz), for 6.81 (1H, users), 6,92-7,83 (16H, m)
5-7of 1.23 (6H, t, J=7,4 Hz), measuring 2.20 (3H, s), 2.63 in (2H, t, J=7,0 Hz), 3,47 (2H, s)4,08 (2H, t, J=7,0Hz), is 4.21 (4H, q, J=7,4 Hz), 6,94 (1H, s), 7,07-7,81 (16H, m)
5-8a 1.11 (6H, d, J=6,4 Hz), of 1.13 (6H, d, J=6,8gts), 2,49-of 2.58 (2H, m), 3,53 (2H, s), 3,98-to 4.15 (4H, m), of 6.96-7,01 (1H, m), 7.03 is-7,16 (3H, m), 7,17-7,37 (8H, m), 7,40-to 7.61 (5H, m), of 7.64-7,71 (2H, m),to 7.77 (1H, DD, J=1,5, 7,GC)
5-91,11 (6N, t, J=7,0 Hz), 1,72 (3H, s), 2,52 (2H, t, J=7,Hz), 3,29 (4H, d of q, J=7,0, 7,0 Hz), of 3.57 (2H, s)4,08 (2H, t, J=7,Hz), 6,85 (1H, users), 6,99-7,81 (18H, m)
5-10of 0.98 (6H, t, J=7,1Hz), of 1.53 (2H, m)to 1.79 (3H, s), of 1.95 (2H, m)to 3.09 (4H, d of q, J=7,1, 7,1 Hz), to 3.64 (2H, s)4,06 (2H, t, J=5,GC), 7,03-7,62 (18H, m), 8,02 (1H, users)

Table 50
ExampleStructureNMR (δ, 300MHz, CDC13)
5-110,86 (6H, t, J=7,1Hz), 1,50 (4H, t kV, J=1,1,7,1Hz), of 2.53 (2H, t, J=7,Hz), 3,21 (4H, m), of 3.57 (2H, s)4,08 (2H, t, J=7,Hz), 6,85 (1H, users), of 7.00 (1H, d, J=7,5 Hz), 7,14-7,80 (17H, m)
5-121,11 (6N, t, J=7,2 Hz), 2,53 (2H, t, J=7,Hz), up 3.22 (3H, d), 3,29 (4H, d of q, J=7,2, 7,2 Hz), 3,55 (2H, s), 4.09 to (2H, t, J=7,Hz), to 6.95 (1H, DD, J=7,5, 1,5Hz),? 7.04 baby mortality-to 7.64 (16H, m), 7,74 (1H, DD, J=7,5, 1,5Hz), to 8.34 (1H, DD, J=8,3, 1,1 Hz)
5-13TPL 78-81of 1.23 (6H, t, J=7,1Hz), 2,61 (2H, t, J=7,2 Hz), up 3.22 (3H, s)to 3.49 (2H, s)4,08 (2H, t, J=7,2Hz), is 4.21 (4H, q, J=7,1Hz), 6,93 (1H, DD, J=7,6, 1,5Hz), 7,28 to 7.75 (14H, m), 7,73 (1H, DD, J=7,6, 1,5Hz), with 8.33 (1H, DD, J=8,3, 1,5Hz)
5-14a 1.11 (6H, t, J=7,4 Hz)and 1.15 (3H, t, J=7,2 Hz), 2,52 (2H, t, J=7,5 Hz), 3,29 (6H, m), of 3.54 (2H, s), 4.09 to (2H, t, J=7,5 Hz), to 6.95 (1H, DD, J=7,9, 1.1 Hz), 7,10 (1H, DD, J=7,9, 7,GC), 7,24-7,73 (16H, m), at 8.36 (1H, d, J=8,3 Hz)
5-15to 1.15(3H, t, J=7,2 Hz), of 1.23 (6H, t, J=7,2 Hz), 2,61 (2H, t, J=7,2 Hz), 3,29 (2H, kV,J=7,2 Hz), 3,49 (2H)4,07 (2H, t, J=7,2Hz), is 4.21 (4H, q, J=7,2 Hz), 6,94 (1H, DD, J=7,5, 1,5Hz), was 7.08 (1H, DD, J=7,9, 7,GC), 7,30-7,73 (14H, m), a 8.34 (1H, DD, J=7,9, 1,5Hz)

Table 51
ExampleStructureNMR (δ, 300MHz, CDC13)
5-161,05 (6N, d, J=6,4 Hz), 1,23 (6N, t, J=7,2 Hz), 2,62 (2H, t, J=7,2 Hz), 3,51 (2H, s), 3,85 (1H, Sept., J=6,4 Hz), 4,10 (2H, t, J=7,2 Hz), 4,20 (4H, q, J=7,2Hz), to 6.95 (1H, DD, J=7,9,1,5Hz), 7,07 (1H, DD, J=7,9, 7,GC), 7,30-to 7.61 (12H, m), 7,68 (1H, DD, J=7,9, 1,5Hz), of 7.75 (1H, users), of 8.28 (1H, DD, J=7,9, 1,5Hz)
5-17of 1.23 (6H, t, J=7,1Hz), 2,61 (2H, t, J=7,1Hz), 3,71 (3H, in), 3.75 (2H, s)4,07 (2H, t, J=7,1Hz), 4,22 (4H, q, J=7,1Hz), 6,94 (1H, d, J=7,Hz), 7,29-7,62 (13H, m), 7,72 (1H, DD, J=1,4, 7,GC), of 8.47 (1H, d, J=8,3 Hz), of 10.25 (1H, users)
5-18of 1.13 (3H, t, J=7,2 Hz), of 1.23 (6H, t, J=7,1Hz), is 2.30 (3H, s), 2,61 (2H, t, J=7,1 Hz)at 3.25 (2H, q, J=7,2 Hz), 3,44 (2H, s)4,07 (2H, t, J=7,1Hz), is 4.21 (4H, q, J=7,1Hz), to 6.75 (1H, s), 7,30-7,69 (14H, m), 8,19 (1H, users)

Example 6

2-[9-(2,2,2-triptoreline)-N-fluoren-9-yl]ethyl ester 4-[(4'-triptorelin-2-carbonyl)amino]benzoic acid

a) Ethyl ester of 4-[(4'-triptorelin-2-carbonyl)amino]benzoic acid

Ethyl ester of 4-aminobenzoic acid (0,568 g) and triethylamine (0,570 g) was dissolved in methylene chloride (20 ml)and to this solution was added dropwise a solution of acid chloride of 4'-triptorelin-2-carboxylic acid, which was obtained from 4'-triptorelin-2-carboxylic acid (1,00 g) by the method similar to that described in example 1d)in methylene chloride under ice cooling. The solution was stirred at room temperature for 2 hours, after which was added methylene chloride (100 ml). The reaction mixture was washed 2 N. hydrochloric Ki is lotay and saturated salt solution, was dried over sodium sulfate and concentrated, obtaining specified in the header connection (1,43 g).

b) 4-[(4'-Triptorelin-2-carbonyl)amino]benzoic acid

Ethyl ester of 4-[(4'-triptorelin-2-carbonyl)amino]benzoic acid (0,700 g)obtained in example 6A)were subjected to interactions, similar to that described in example 1f), receiving specified in the header connection (0,680 g) as a white solid.

(C) (2,2,2-Triptorelin)amide of 9-[2-(tert-butyldimethylsilyloxy)ethyl]-N-fluoren-9-carboxylic acid

(2,2,2-Triptorelin)amide N-fluoren-9-carboxylic acid (3.00 g) was dissolved in tetrahydrofuran (100 ml)and to this solution was added dropwise 1.5 M solution (13,7 ml) diisopropylamide lithium under ice cooling. The mixture was stirred for one hour while cooling with ice, and added to it a solution of tert-butyldimethylchlorosilane (2,46 g) in tetrahydrofuran (5 ml). The temperature is gradually raised from a temperature under cooling with ice to room temperature and the mixture was stirred over night. Was added to the reaction mixture, a saturated aqueous solution of ammonium chloride under cooling with ice and was extracted with a mixture of ethyl acetate (50 ml x 2). The extract was washed with saturated salt solution, dried over sodium sulfate and purified column is a chromatography on silica gel using a mixture of ethyl acetate:hexane=1:2,5, getting listed in the title compound (6,00 g).

d) (2,2,2-Triptorelin)amide of 9-(2-hydroxyethyl)-N-fluoren-9-carboxylic acid

(2,2,2-Triptorelin)amide of 9-[2-(tert-butyldimethylsilyloxy)ethyl]-N-fluoren-9-carboxylic acid (6,00 g)obtained in example 6C), was dissolved in a mixture of tetrahydrofuran (13 ml) - acetic acid (39 ml) - water (13 ml). The solution was stirred at room temperature for 20 hours and concentrated in vacuum. The residue was purified column chromatography on silica gel using a mixture of ethyl acetate:hexane=1:1, getting mentioned in the title compound (3.80 g).

e) 2-[9-(2,2,2-Triptoreline)-N-fluoren-9-yl]ethyl ester 4-[(4'-triptorelin-2-carbonyl)amino]benzoic acid

4-[(4'-Triptorelin-2-carbonyl)amino]benzoic acid (0,345 g)obtained in example 6b), and (2,2,2-triptorelin)amide of 9-(2-hydroxyethyl)-N-fluoren-9-carboxylic acid (0,300 g)obtained in example 3d)were subjected to interaction, similar to that described in example 1g), receiving specified in the header connection (0,390 g) as colorless solids (see table 52).

Examples 6-2 on 6-22

Connection examples 6-2 on 6-22 was obtained by methods similar to those described in examples 6, 1-2b), 1-2C 1-2d). Thus obtained compounds are shown in table is Zach 52-56.

Table 52
ExampleStructureNMR (δ, 300MHz, CDC13)
62,98 (2H, t, J=6,8gts), 3,63-3,71 (2H, m), 3,81 (2H, t, J=6,8gts), 5,27 (1H, usher.), 7,00 (1H, users), 7,12 (2H, m), 7,30-7,84 (18H, m)
6-22,45-of 2.58 (2H, m), 4,10-4,18 (1H, m), is 4.21 (2H, t, J=7,5 Hz), 7,02 (1H, users), 7,14-7,88 (20H, m)
6-3a 3.01 (2H, t, J=6,GC), 3,60-3,74 (2H, m), 3,86 (2H, t, J=6,GC), 5,27 (18H, m), 7,20-to 7.61 (18H, m), of 7.75 (2H, d, J=6,GC), of 7.97 (1H, users), charged 8.52 (1H, d, J=8,4 Hz)
6-4of 3.56 (2H, t, J=5,2Hz), 4,06 (2H, t, J=5,2Hz), 5,52 (1H, usher.), was 7.08 (1H, users), 7,15-7,98 (21H, m)
6-53,42-of 3.54 (2H, m), 3,55 (2H, s), 4.26 deaths (2H, t, J=6,GC), 5,52 (1H, usher.), 7,06 (1H, users), 7,18-7,88 (21H, m)

Table 53
ExampleStructureNMR (δ, 300MHz, CDC13)
6-62,31-to 2.42 (1H, m), 2,80-of 2.93 (1H, m), of 3.73-to 3.89 (2H, m), 4,16-4.26 deaths (1H, m), 4,32-4,43 (2H, m), 5,62 (1H, usher.), to 7.09 (1H, users), 7,26-8,01 (19H, m)
6-72,15-to 2.29 (2H, m)to 3.34 (2H, t, J=7,Hz), 4,01-4,18 (2H, m), and 4.40 (2H, t, J=6,2 Hz), x 6.15 (1H, usher.), was 7.08 (1H, users), 7,18-7,98 (17H, m), 7,92 (1H, d, J=8,4 Hz)
6-8is 2.88 (2H, t, J=8,3 Hz), 3,83-3,93 (2H, m)to 4.23 (2H, t, J=8,3 Hz), 5,90 (1H, t, J=6,4 Hz), 7,01 (1H, users), 7,16-7,86 (22H, m)
6-92,12-to 2.29 (1H, m), 2,56 of 2.68 (1H, m), 3,70-of 3.80 (3H, m), 4.09 to be 4.29 (2H, m), 5,41 (1H, usher.), 7,05 (1H, users), 7,12-7,78 (20H, m), 7,86 (1H, d, J=7,5 Hz)
6-102,16-of 2.30 (2H, m), 2,62-of 2.72 (2H, m), 3,61 (1H, t, J=7,5 Hz), 3,71-3,99 (4H, m), 4,12-4,37 (4H, m), 5,67 (1H, usher.), 7,05 (1H, users), 7,15-to $ 7.91 (17H, m)

Table 54
ExampleStructureNMR (δ, 300MHz, CDC13)
6-11to 3.49 (2H, t, J=6,Hz), 4.09 to be 4.29(2H, m), 4,56 (2H, t, J=6,GC), 6,34 (1H, usher.), was 7.08 (1H, users), 7,12-8,00 (18H, m)
6-122,39-of 2.50 (1H, m), 2.93 which was 3.05 (1H, m), 3,78-4,06 (2H, m), 4,20-to 4.41 (2H, m), of 4.77 (1H, d, J=6,4 Hz, J=9,GC), 5,42 (1H, 1H, t, J=6,4 Hz), 7,07 (1H, users), 7,19-7,88 (15H, m)
6-132,19-of 2.30 (1H, m), 2,62-by 2.73 (1H, m), 3,79-3,82 (2H, m), 4,20-and 4.40 (3H, m), 580 (1H, t, J=6,4 Hz), 7,06(1H, users) 7,16-7,92(16H, m)
6-14to 1.22 (6H, t, J=7,1Hz), 2,77 (2H, t, J=6,GC), is 4.21 (4H, q, J=7,1Hz), 4,30 (2H, t, J=6,GC), 7,06 (1H,users),

7,19-7,88 (17H, m)
6-15of 1.23 (6H, t, J=7,1Hz),

of 1.64 (3H, s), 2,77 (2H, t, J=6,GC), is 4.21 (4H, q,

J=7,1Hz), the 4.29 (2H, t,

J=6,GC), 6,93 (1H, users), 7,20-8,24 (16H, m)

Table 55
ExampleStructureNMR (δ, 300MHz, CDC13)
6-16to 1.22 (3H, t, J=7,1Hz), of 1.23 (3H, t, J=7,1Hz), was 2.76 (2H, t, J=6,GC), 4,20 (2H, q, J=7,1Hz), is 4.21 (2H, q, J=7,1Hz), the 4.29 (2H, t, J=6,GC), 6,95-to $ 7.91 (17H, m)
6-17to 1.22 (6H, t, J=7,1Hz), 2,77 (2H, t, J=6,GC), 4,20 (4H, q, J=7,1Hz), or 4.31 (2H, t, J=6,GC), 6,93 (2H, d, J=8,8gts), 7,26-8,13 (13H, m), 7,92 (2H, d, J=8,8gts)
6-18to 1.22 (6H, t, J=7,1Hz), was 2.76 (2H, t, J=6,GC), 4,20 (4H, q, J=7,1Hz), 4,30 (2H, t, J=6,GC), 6,85 (2H, d, J=8,8gts), 7,21-7,81 (13H, m), 7,88 (2H, d, J=8,8gts), 8,21 (1H, DD, J=7,6,1,3)
6-19to 1.14 (6H, t, J=7,2 Hz), 2,63-a 2.71 (2H, m), and 3.31 (4H, d of q, J=5,6, 7,2 Hz), 4,29-to 4.38 (2H, m), 7,15-7,20 (1H, m), 7.23 percent-7,38 (7H, m) 7,41-7,47 (1H, m), 7,49-7,63 (4H, m), of 7.64 to 7.75 (4H, m), 81 (1H, DD, J=1,5, 7,5Hz), 7,86-to 7.93 (2H, m)
6-20to 1.14 (6H, t, J=7,1Hz), 2,65-to 2.74 (2H, m), and 3.31 (4H, d of q, J=5,7, 7,1 Hz), 4,33-4,43 (2H, m), was 7.08 (1H, d, J=8,3 Hz), 7,27-7,44 (6H, m), 7,47-to 7.61 (5H, m), 7,63-7,72 (3H, m), of 7.90 (1H, DD, J=1,9, 8,GC), 8,07 (1H, d, J=1,GZ), 8,23 (1H, DD, J=1,5, 7,GC)

Table 56
ExampleStructureNMR (δ, 300MHz, CDC13)
6-21to 1.14 (6H, t, J=7,2 Hz), 2,64-by 2.73 (2H, m), 3,32 (4H, d of q, J=5,6, 7,2 Hz), or 4.31-to 4.41 (2H, m), 6,91-6,98 (2H, m), 7,26 and 7.36 (5H, m), 7,41 (1H, DD, J=1,1, 7,5Hz), 7,47-to 7.59 (3H, m), 7,60-7,71 (5H, m), 7,94-8,01 (2H, m), 8,11 (1H, DD, J=1,1, 7,5Hz)
6-22of 1.13 (6H, t, J=7,2 Hz), 2,66 is 2.75 (2H, m), 3,32 (4H, d of q, J=5,3, 7,2 Hz), 4,36 is 4.45 (2H, m), 7,27-7,46 (8H, m), of 7.48-rate of 7.54 (2H, m), 7,55-7,73 (4H, m), to 7.99 (2H, s), 8,32 (1H, DD, J=1,1, 7,GC)

Example 7

2-[9-(2,2,2-Triptoreline)-N-fluoren-9-yl]ethyl ester of TRANS-4-[(4'-triptorelin-2-carbonyl)amino]cyclohexanecarbonyl acid

a) 4-[(4'-Triptorelin-2-carbonyl)amino]cyclohexanecarbonyl acid

4-Aminocyclohexanecarboxylic acid (0,538 g) was dissolved in 4 BC, the sodium hydroxide (0,933 ml)and to this solution under ice cooling were simultaneously added dropwise RA is a creation of the carboxylic acid, obtained from 4'-triptorelin-2-carboxylic acid (1.0 g) by the method similar to that described in example 1d), in tetrahydrofuran (5 ml), and 4 N. aqueous sodium hydroxide solution (0,933 ml). The mixture was stirred at room temperature for one hour, acidified 2 N. hydrochloric acid and was extracted with ethyl acetate. The extract was washed with saturated salt solution and dried over sodium sulfate, getting mentioned in the title compound (1.20 g) as a colorless powdery solid.

b) 2-[9-(2,2,2-Triptoreline)-N-fluoren-9-yl]ethyl ester of TRANS-4-[(4'-triptorelin-2-carbonyl)amino]cyclohexanecarbonyl acid

4-[(4'-Triptorelin-2-carbonyl)amino]cyclohexanecarbonyl acid (0,570 g)obtained in example 7a), and (2,2,2-triptorelin)amide of 9-(2-hydroxyethyl)-N-fluoren-9-carboxylic acid (0,500 g)obtained in example 6d), were treated in a manner analogous to example 1g), getting mentioned in the title compound (0.534 g) as colorless solids (see table 57).

Examples 7-2 through 7-5

Connection examples 7-2 through 7-5 received a manner similar to that described in example 7. Thus obtained compounds are presented in table 57.

Table 57
Example StructureNMR (δ, 300MHz, CDC13)
7< / br>
TPL 156,3-158,0
1,08 is 1.20 (4H, m), 1,28-of 1.42 (4H, m), 1,87-of 1.94 (1H, m), 2,80 (2H, t, J=7,1Hz), 3,52 (2H, t, J=7,1Hz), the 3.65 (1H, m)to 3.89 (1H, usher.), by 5.18 (1H, d, J=8,3 Hz), a 5.25 (1H, t, J=6,4 Hz), 7,29-7,79 (16H, m)
7-20,60-of 0.71 (2H, m), of 1.05 to 1.27 (2H, m), 1,53 is 1.86 (4H, m), 2,82 (2H, t, 6,GC), of 3.54 (2H, t, J=6,GC), 3,56-to 3.73 (2H, m), 4,96 (1H, d, J=8,3 Hz), 5,27 (1H, t, J=7,Hz), 7,30-7,80 (16H, m)
7-31,33-of 1.73 (8H, m), 2.00 in to 2.13 (1H, m), 2,22-is 2.37 (1H, m), 2,45-2,60 (1H, m), 3,52 (1H, t, J=7,0 Hz), 3,66-4,11 (4H, m), and 5.30 (1H, d, J=11,3 Hz), 5,72 (1H, t, J=8,2 Hz), 7,20-7,33 (13H, m)
7-41,09 is 1.20 (2H, m)of 1.24(6H, t, J=7,2 Hz), 1,36-of 1.53 (6H, m), 2,27-of 2.38 (1H, m), 3,82-of 3.95 (1H, m), 4,22 (4H, q, J=7,2 Hz), 4,80 (2H, s), 5,2 1(1H, userd, J=7,Hz), 7,22-7,39 (6H, m), 7,42-EUR 7.57 (4H, m), 7,60-of 7.70 (3H, m)
7-51,12-2,27 (9H, m)of 1.24 (6H, t, J=7,2 Hz), 2,60 (2H, t, J=7,2Hz),

3,59-of 3.78 and 3,90-to 4.15 (1H, m), was 4.02 (2H, t, J=7,2 Hz), 4,22 (4H, q, J=7,2 Hz), 4,98 and and 5.30 (1H, each d, J=8,4 Hz), 7.18 in-7,22 (13H, m) mixture of CIS, TRANS isomers

Example 8

Diethyl ester of 2-phenyl-2-(2-{4-[(4'-triptorelin-2-carbonyl)amino]piperidine-1-yl}acetoxymethyl)malonic acid

a) 1-Benzyl-4-(4'-triptorelin-2-carbylamine)piperidine

4'-triftormetilfullerenov acid (5.0 g) was dissolved in dimethylformamide (950 ml)and to this solution was added at room temperature 4-amino-1-benzylpiperidine (3.55 g), hydrate of 1-hydroxybenzotriazole (3.0 g), and hydrochloride of 1-ethyl-3-(3'-dimethylaminopropyl)carbodiimide (3.58 g). The mixture was stirred at room temperature overnight, and the reaction solution was concentrated in vacuo to precipitate crystals. The crystals are then washed with saturated aqueous sodium bicarbonate solution and water and dried in vacuum, obtaining specified in the header connection (7,42 g).

b) 4-(4'-triptorelin-2-carbylamine)piperidine

To a solution of 1-benzyl-4-(4'-triptorelin-2-carbylamine)piperidine (1.47 g)obtained in example 8A), in a mixture of tetrahydrofuran-methanol (1:1; 50 ml) was added palladium hydroxide (300 mg) in a stream of argon while cooling with ice. The mixture was stirred for one day at normal pressure in an atmosphere of hydrogen and in addition was stirred for one day at normal pressure in a hydrogen atmosphere after the additional added palladium hydroxide (300 mg). The reaction mixture was filtered through a layer of celite and washed with methanol. The filtrate and washing liquid were combined, concentrated in vacuo and was purified column chromatography on what silicagel using a mixture of chloroform:methanol:aqueous ammonia=100:10:1, getting listed in the title compound (1,03 g).

(C) Ethyl ester [4-(4'-triptorelin-2-carbylamine)piperidine-1-yl]acetic acid

To a solution of 4-(4'-triptorelin-2-carbylamine)piperidine (1,03 g)obtained in example 8b), in dimethylformamide (5 ml) was added potassium carbonate (276 mg) and ethyl ether bromoxynil acid (223 μl). The mixture was stirred over night at ambient temperature, component 90°S, and then concentrated in vacuum. The residue was distributed between water and chloroform, and the aqueous layer was additionally extracted with chloroform. The organic layers were combined, washed with saturated salt solution, dried over sodium sulfate, concentrated in vacuo and was purified column chromatography on silica gel using a mixture of chloroform:methanol=30:1, getting mentioned in the title compound (598 mg).

d) [4-(4'-Triptorelin-2-carbylamine)piperidine-1-yl]acetic acid

To a solution of ethyl ester [4-(4'-triptorelin-2-carbylamine)piperidine-1-yl]acetic acid (595 mg)obtained in example 8C), in a mixture of tetrahydrofuran-methanol (1:2; to 10.2 ml) was added 1 M aqueous solution of lithium hydroxide (6.8 ml)and the mixture was stirred at room temperature for 6 hours. The reaction solution which was koncentrirebuli in vacuum and was added to the residue 2 N. hydrochloric acid, bringing the pH to about 3, while in the sediment precipitated crystals. The crystals were collected by filtration, washed with cold water and dried in vacuum, obtaining mentioned in the title compound (411 mg).

e) Diethyl ester of 2-phenyl-2-(2-{4-[(4'-triptorelin-2-carbonyl)amino]piperidine-1-yl}acetoxymethyl)malonic acid

[4-(4'-Triptorelin-2-carbylamine)piperidine-1-yl]acetic acid obtained in example 8d), and diethyl ester of 2-hydroxymethyl-2-phenylmalonate acid obtained in example 1-2A)was subjected to reactions similar to those described in example 1g), receiving specified in the header of the connection (see table 58).

Table 58
ExampleStructureNMR (δ, 300MHz, CDC13)
81,07-1,19 (2H, m), 1,25 (6H, t, J=7,0 Hz), 1,54 by 1.68 (2H, m), 2,10-2,22(2H, m), 2,52-2,62 (2H, m), is 3.08 (2H, s), 3,70-of 3.85 (1H, m), 4,24 (4H, q, J=7,0Hz), is 4.85 (2H, s), 5,07-5,16 (1H, m), 7,28-7,39 (6H, m), 7,42-EUR 7.57 (4H, m), to 7.61-7,71 (3H, m)

Example 9

Diethyl ester of 2-phenyl-2-(2-{4-[(4'-triptorelin-2-carbonyl)amino]indol-1-yl}acetoxymethyl)malonic acid.

a) Ethyl ester of (4-nitroindole-1-yl)acetic acid

The hydride on the rija (60% in mineral oil; 81 mg) was dissolved in dimethylformamide (5 ml)and the solution was cooled to 0°C. After adding 4-nitroindole (300 mg) and the mixture was stirred for one hour and was added to a mixture of ethyl ether bromoxynil acid (340 mg), followed by stirring at 0°C for 4 hours. Added water to the mixture, and the mixture was concentrated, diluted with ethyl acetate, washed with water, dried over sodium sulfate, then concentrated, getting mentioned in the title compound (367 mg).

b) (4-Nitroindole-1-yl)acetic acid

Ethyl ester (4-nitroindole-1-yl)acetic acid obtained in example 9a), were subjected to interactions, similar to that described in example 1f), getting mentioned in the title compound (243 mg).

C) Diethyl ether 2-[2-(3-nitroindole-1-yl)acetoxymethyl]-2-phenylmalonate acid

(4-Nitroindole-1-yl)acetic acid (229 mg)obtained in example 9b), 4-dimethylaminopyridine (143 mg) and diethyl ester of 2-hydroxymethyl-2-phenylmalonate acid (240 mg)obtained in example 1-2A)were subjected to interactions, similar to that described in example 1-3C), getting mentioned in the title compound (301 mg).

d) Diethyl ester 2-[2-(4-aminoindole-1-yl)acetoxymethyl]-2-phenylmalonate acid

Diethyl ether 2-[2-(3-nitroindole-1-the l)acetoxymethyl]-2-phenylmalonate acid (100 mg), obtained in example 9c)was dissolved in tetrahydrofuran (2 ml), ethanol (4 ml) and water (1 ml), and to the solution was added ammonium chloride (57 mg) and reduced iron (60 mg). The mixture was stirred at 100°C for 2 hours, cooled and filtered through a layer of celite. The filtrate was concentrated and diluted with ethyl acetate. The extract was sequentially washed with saturated aqueous sodium bicarbonate solution, water and saturated salt solution, dried over sodium sulfate and concentrated, obtaining mentioned in the title compound (93 mg).

e) Diethyl ester of 2-phenyl-2-(2-{4-[(4'-triptorelin-2-carbonyl)amino]indol-1-yl}acetoxymethyl)malonic acid.

Diethyl ether 2-[2-(4-aminoindole-1-yl)acetoxymethyl]-2-phenylmalonate acid obtained in example 9d), were processed by the method similar to that described in example 1E), receiving specified in the header of the connection (see table 59).

Example 9-2

Diethyl ether 2-(2-{2-methyl-4-[(4'-triptorelin-2-carbonyl}amino]benzimidazole-1-yl}acetoxymethyl)-2-phenylmalonate acid

a) 2-Methyl-4-nitro-1H-benzimidazole

3-Nitrobenzene-1,2-diamine (1.0 g) was dissolved in ethanol (90 ml) and 5 G. hydrochloric acid (24 ml)and to this solution was added 2,4-pentanedione (1.3 g). The mixture was heated at boiling under reflux in those who tell 3 hours was cooled to room temperature and concentrated. To this concentrate was added ethyl acetate, and the mixture is successively washed with saturated aqueous sodium bicarbonate and water and dried over sodium sulfate, getting mentioned in the title compound (1.1 g).

b) Ethyl ester of (2-methyl-4-nitrobenzimidazole-1-yl)acetic acid

2-Methyl-4-nitro-1H-benzimidazole (1.1 g)obtained in example 9-2A)were subjected to interactions, similar to that described in example 9a), getting mentioned in the title compound (1.44 g).

C) Diethyl ether 2-(2-{2-methyl-4-[(4'-triptorelin-2-carbonyl}amino]benzimidazole-1-yl}acetoxymethyl)-2-phenylmalonate acid

Ethyl ester of (2-methyl-4-nitrobenzimidazole-1-yl)acetic acid (500 mg)obtained in example 9-2b)were subjected to interactions described in the examples 9d), 1d), 1e), 1f) and 1g), getting mentioned in the title compound (152 mg) (see table 59).

Example 9-3

2,2-Bisericani-2-phenethyl ester [2-oxo-3-(4'-triptorelin-2-carbonyl)-2,3-dihydroisoxazole-6-yl]acetic acid

2,2-Bisericani-2-phenethyl ether {3-hydroxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid (195 mg)obtained in example 3-2 was dissolved in chloroform (5 ml), which to this solution was added triethylamine (72 mg). The solution was cooled to 0°and added to it triphosgene (35 mg). After stirring for one hour the reaction solution was washed with water, dried over sodium sulfate and purified column chromatography on silica gel using a mixture of hexane:ethyl acetate=1:1, getting mentioned in the title compound (173 mg) (see table 59).

Example 9-4

Diethyl ether 2-(2-{3-etoxycarbonyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid

a) the acid chloride of 5-chloro-2-nitrobenzoic acid

5-Chloro-2-nitrobenzoic acid was subjected to interactions, similar to that described in example 1d), receiving specified in the header of the connection.

b) Ethyl ester of 5-chloro-2-nitrobenzoic acid

To a mixture of ethanol (1.23 ml), triethylamine (3,05 ml) and tetrahydrofuran (35 ml) was added dropwise a solution of acid chloride of 5-chloro-2-nitrobenzoic acid (4.44 g)obtained in example 9-4A)in tetrahydrofuran (10 ml) under cooling with ice. The mixture was stirred at room temperature overnight and then added water. The solution was diluted with ethyl acetate, and the organic layer was washed successively with saturated aqueous sodium bicarbonate solution and saturated salt solution, dried over sodium sulfate and concentrated, is the learn specified in the header connection (4,43 g) as a pale brown solid.

(C) Dimensiony ether 3-etoxycarbonyl-4-nitrophenylarsonic acid

Ethyl ester of 5-chloro-2-nitrobenzoic acid (4,40 g)obtained in example 9-4b), and dibenzylamine ester of malonic acid were subjected to interactions, similar to that described in example 1-3A), getting mentioned in the title compound (4.61 in).

d) 4-Amino-3-ethoxycarbonylmethoxy acid

Dimensiony ether 3-etoxycarbonyl-4-nitrophenylarsonic acid (1.51 g)obtained in example 9-4C)were subjected to interactions, similar to that described in example 1-3d), getting mentioned in the title compound (4.59 g).

e) 3-Etoxycarbonyl-4-[(4'-triptorelin-2-carbonyl)amino]phenylacetic acid

4-Amino-3-ethoxycarbonylmethoxy acid (1.51 g)obtained in example 9-4d), and the acid chloride 4'-triptorelin-2-carboxylic acid (1,99 g) was subjected to interactions, similar to that described in example 7-a), provided that as the basis used sodium bicarbonate, if this is specified in the header connection (1,87 g) was obtained as pale yellow amorphous powder.

f) Diethyl ether 2-(2-{3-etoxycarbonyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid

3-Etoxycarbonyl-4-[(4'-triptorelin-2-carbonyl)amino]phenylacetic acid (0,532 g)obtained in example 9-4E), and diethyl ester of 2-hydroxymethyl-2-phenylmalonate acid (1.04 g)obtained in example 1-2A), were processed by the method similar to that described in example 1g), receiving specified in the header connection (0,524 g) (see table 59).

Example 9-5

Diethyl ether 2-(3-{3-dimethylcarbamoyl-4-[4'-triptorelin-2-carbonyl)amino]phenyl}propionyloxy)-2-phenylmalonate acid

a) the acid chloride of 5-methyl-2-nitrobenzoic acid

5-Methyl-2-nitrobenzoic acid was treated in a manner similar to that described in example 1-d), receiving specified in the header of the connection.

b) 5,N,N-Trimethyl-2-nitrobenzamide

The acid chloride of 5-methyl-2-nitrobenzoic acid obtained in example 9-5A), were processed by the method similar to that described in example 1 (e), receiving specified in the header of the connection.

C) 5-methyl bromide-N,N-dimethyl-2-nitrobenzamide

5,N,N-Trimethyl-2-nitrobenzamide (4,16 g)obtained in example 9-5b), N-bromosuccinimide (of 3.56 g) and 2,2'-azobisisobutyronitrile (328 mg) suspended in carbon tetrachloride (80 ml). The suspension was stirred at 90°C for 2 hours, filtered through a layer of celite and purified colonoscopy because it allows the Noah chromatography on silica gel using a mixture of hexane:ethyl acetate=5:4, getting listed in the title compound (602 mg).

(d) Benzyl ester 3-(3-dimethylcarbamoyl-4-nitrophenyl)-2-methoxycarbonylpropionyl acid

5-methyl bromide-N,N-dimethyl-2-nitrobenzamide (0,597 g)obtained in example 9-5C), and benzyl ether methyl ester of malonic acid was subjected to reactions similar to those described in example 9-4C), receiving specified in the header connection (0,491 g).

e) 3-(4-Amino-3-dimethylcarbamoyl)-2-methoxycarbonylpropionyl acid

Benzyl ester 3-(3-dimethylcarbamoyl-4-nitrophenyl)-2-methoxycarbonylpropionyl acid (0,490 g)obtained in example 9-5d)were subjected to reactions similar to those described in example 1-2C), receiving specified in the header connection (0,353 g).

f) Methyl ether 3-(4-amino-3-dimethylcarbamoyl)propionic acid

3-(4-Amino-3-dimethylcarbamoyl)-2-methoxycarbonylpropionyl acid (347 mg)obtained in example 9-5e), was stirred at 150°C for 40 minutes, cooled to room temperature and was purified column chromatography on silica gel using a mixture of hexane:ethyl acetate (1:1 to 0:1), obtaining mentioned in the title compound (180 mg).

g) Diethyl ether 2-(3-{3-dimethylcarbamoyl-4-[4'-triptorelin-2-carbonyl)amino]phenyl}propion oxymethyl)-2-phenylmalonate acid

Methyl ester of 3-(4-amino-3-dimethylcarbamoyl)propionic acid (was 0.138 g)obtained in example 9-5f)were subjected to reactions similar to those described in examples 1E), 1f) and 1g), receiving specified in the header connection (0,158 g) (see table 59).

Examples 9-6 on 9-29

Connection examples 9-6 on 9-29 got a way similar to that described in examples 9 to 9-5. Thus obtained compounds are shown in tables 59-64.

Table 59
ExampleStructureNMR (δ, 300MHz, CDC13)
9of 1.18 (6H, t, J=7,2Hz), is 4.15 (4H, q, J=7,2Hz), to 4.73 (2H, s), is 4.85 (2H, s)to 5.56 (1H, d, J=3,0 Hz), 6,85 (1H, d, J=3,4 Hz), 6,91 (1H, d, J=8,3 Hz), 7,16-7,78 (16H, m), 7,92 (1H, d, J=6,8gts)
9-2of 1.17 (6H, t, J=7,1Hz), of 2.38(3H, s), of 4.13 (4H, q, J=7,1Hz), 4,70(2H, s), to 4.87(2H, s), at 6.84 (1H, d, J=7,Hz), 7,12-7,63 (13H, m), 7,80 (1H, DD, J=7,5, 1,5Hz), 8,18 (1H, d, J=7,Hz), to 8.41 (1H with)
9-3a 1.08 (6H, t, J=7,2 Hz), with 3.27 (4H, d sq J=7,2, 7,2 Hz), 3,61 (2H, s), 4,88 (2H, s), 6,93 (1H, d, J=1,1 Hz),? 7.04 baby mortality (1H, DD, J=8,3, 1,5Hz), 7,11-7,70 (15H, m), 7,79 (1H, d, J=8,3 Hz)
9-4to 1.21 (6H, t, J=7,1Hz), of 1.35 (3H, t, J=7,1Hz), 3,55 (2H, s) 4,15-4,30 (6H,m), a 4.83 (2H, s), 7.24 to 7,38 (6H, m), 7,41-7,47 (1H, m), of 7.48 to 7.62 (6H, m), 7,76 (1H, DD, J=1,5, 7,5Hz), 7,81 (1H, d, J=1,GZ), 8,68 (1H, d, J=8,Hz), 11,23 (1H, users)
9-5to 1.24 (6H, t, J=7,0 Hz), 2,53 (2H, t, J=7,3 Hz), was 2.76 3.00 for (6H, usher.), of 2.81 (2H, t, J=7,3 Hz), 4,24 (4H, q, J=7,0Hz), to 4.81 (2H, s), of 6.96 (1H, d, J=2,3 Hz), 7,17 (1H, DD, J=1,2, 8,4 Hz), 7,29-7,37 (5H, m), 7,37-7,42 (1H, m), 7,44-EUR 7.57 (2H, m), 7,60-to 7.64 (4H, m), 7,68 (1H, DD, J=1,5, 7,4 Hz), of 8.28 (1H, d, J=8,4 Hz), 9,.05 (1H, users)

Table 60
ExampleStructureNMR (δ, 300MHz, CDC13)
9-6of 1.12 (6H, t, J=7,2 Hz), 3,30(4H, d of q, J=5,7, 7,2 Hz), 4,39 (2H, d, J=6,0 Hz), to 5.08 (2H, s)5,59 (1H, ushort, J=6,0 Hz), 6,97-7,03 (2H, m), 7,28-7,42 (8H, m), 7,43-of 7.55 (4H, m), 7,56-to 7.61 (2H, m), 7,66-7,71 (1H, m), 7,76-7,83 (2H, m)
9-7a 1.08 (3H, t, J=7,2 Hz), 2,64-2,82 (2H, m), 2,86-of 2.97 (2H, m), 3,13-to 3.36 (2H, m), by 5.87 is 5.98 (1H, usher.), 6,03 (1H, s), 7,00 (1H, s),? 7.04 baby mortality-to 7.15 (4H, m), 7,30-7,40 (5H, m), the 7.43 (1H, DD, J=1,1, 7,5Hz), of 7.48-7,63 (4H, m), 7,63-7,71 (2H, m), 7,78 (1H, DD, J=1,5, 7,5Hz)
9-8the 1.04 (6H, t, J=7,2 Hz), 3,23 (4H, d of q, J=5,7, 7,2 Hz), 3,55 (2H, s), is 4.85 (2H, s), 5,23 (2H, s), was 7.08 (2H, ushort, J=5,GC), 7,14-7,22 (2H, m), 7.23 percent-7,47 (10H, m), of 7.48-to 7.64 (6H, m), 7,76 (1H, DD, J=1,5, 7,1 Hz), 7,81 (1H, d, J=2,2 Hz), 8,69 (1H, d, J=8,Hz), 11,17 (1H, users)
9-9 1,05 (6N, t, J=7,2 Hz)at 3.25 (4H, d of q, J=5,6, 7,2 Hz), to 3.58 (2H, s), a 4.86 (2H, s), 7,11-7,63 (15H, m), 7,72 (1H, DD, J=1,5, 7,5Hz), 7,83 (1H, d, J=1,GZ), 8,66 (1H, d, J=8,Hz), 11,10 (1H, users)
9-10of 1.07 (6H, t, J=7,2 Hz), of 1.36 (3H, t, J=7,2 Hz), 3,26 (4H, d of q, J=5,4, 7,2 Hz), to 3.58 (2H, s), 4.26 deaths (2H, q, J=7,2Hz), a 4.86 (2H, s), 7,10 (2H, ushort, J=5,4 Hz), 7,16-7,37 (6H, m), 7,40-to 7.64 (7H, m), to 7.77 (1H, DD, J=1,9, 7,1 Hz), 7,80 (1H, d, J=1,GZ), 8,69 (1H, d, J=8,Hz), 11,22 (1H, users)

Table 61
ExampleStructureNMR (δ, 300MHz, CDC13)
9-11to 1.19 (6H, t, J=7,2 Hz), 4,17 (4H, q, J=7,2 Hz), 4,79 (2H, s), the 4.90 (2H, s)6,94 (1H, d, J=8,0 Hz), 7,15-7,63 (13H, m), 7,82 (1H, d, J=7,5 Hz), of 8.25 (1H, d, J=8,0Hz), of 8.47 (1H, users)
9-12< / br>
TPL 139,4-141,0
to 1.15 (6H, t, J=7,2 Hz), 2,64-by 2.73 (2H,m), 3,32 (4H, d of q, J=5,3, 7,2 Hz), or 4.31-of 4.44 (2H, m)to 4.41 (2H, d, J=6,0 Hz), 5,62 (1H, ushort, J=6,0 Hz), 7,10-7,16 (1H, m), 7.24 to 7,39 (7H, m), 7,42-7,58 (6H, m), a 7.62-7,72 (3H, m), 7,74 for 7.78 (1H, m), a 7.85-a 7.92 (1H, m)
9-13of 1.07 (6H, t, J=7,1Hz), 3,26 (4H, d of q, J=5,7, 7,1 Hz), of 3.57 (2H, s), 3,81 (3H, s), a 4.86 (2H, s), 7,10 (6H, ushort, J=5,GC), 7,16-of 7.23 (2H, m), 7,25-7,37 (4H, m), 7,41-7,63 (7H,m), to 7.77 (1H, DD, J=1,5, 7,5Hz), 7,80 (1H, d, J=2,2 Hz), 8,68 (1H, d, J=8,3 Hz), of 11.15 (1H, users)
9-14 to 1.19 (6H, t, J=7,0 Hz), 3,52 (2H, S), 4,19 (4H, q, J=7,0 Hz), 4,82 (2H, s), 5,23 (2H, s), 7.24 to 7,29 (5H, m), 7,32-7,46 (7H, m), 7,49 to 7.62 (6H, m), 7,74-7,79 (1H, m), 7,82 (1H, d, J=2,2 Hz), 8,67 (1H, d, J=8,8gts), 11,17(1H, users)
9-15to 1.21 (6H, t, J=7,1Hz), of 3.56 (2H, s), is 4.21 (4H, q, J=7,1Hz), is 4.85 (2H, s), 7.23 percent-to 7.32 (5H, m), of 7.36-7,63 (8H, m), to 7.77 (1H, DD, J=1,5, 7,5Hz), 7,86 (1H, d, J=1,GZ), to 8.70 (1H, userd, J=8,3 Hz), 10,89 (1H, users)

Table 62
ExampleStructureNMR (δ, 300MHz, CDC13)
9-16to 1.22 (6H, t, J=7,1Hz), of 3.57 (2H,C)to 4.23 (4H, q, J=7,1Hz), is 4.85 (2H, s), 6,92 (1H, s), 7,03 (1H, d, J=8,3 Hz), 7,30-7,69 (13H, m), to 7.77 (1H, d, J=8,3 Hz)
9-17of 1.23 (6H, t, J=7,1Hz), to 3.67 (2H, s)to 4.23 (4H, q, J=7,1Hz), is 4.85 (2H, s), 7.23 percent-7,34 (6H, m), 7,42-7,49 (3H, m), 7,52-to 7.67 (5H, m), 7,95 (1H, d, J=1,GZ), with 8.05 (1H, DD, J=1,5, 7,5Hz)
9-18to 1.21 (6H, t, J=7,2Hz), is 1.31 (6H, d, J=6,4 Hz), 3,55 (2H, s), is 4.21 (4H, q, J=7,2Hz), a 4.83 (2H, s), 5,09 (1H, Sept, J=6,4 Hz), 7.24 to 7,38 (6H, m), 7,41-7,47 (1H, m), of 7.48 to 7.62 (6H, m), 7,73-7,81 (2H, m,), 8,68 (1H, d, J=8,Hz), 11,33 (1H, users)
9-19to 1.21 (6H, t, J=7,1Hz), of 3.54 (2H, s), of 3.80 (3H, s), is 4.21 (4H, q, J=7,1Hz), a 4.83 (2H, S), 7,247,38 (6H, m), 7,44 (1H, DD, J=1,6, 7,1 Hz), 7,50 to 7.62 (6H, m), to 7.77 (1H, DD, J=1,5, 7,1 Hz), 7,81 (1H, d, J=2,3 Hz), 8,67 (1H, d, J=8,Hz), of 11.15 (1H, users)
9-20to 1.21 (6H, t, J=7,1 Hz), 1.85 to 2,03 (2H, m), 2.05 is-of 2.27(2H, m), 2,50-to 2.67 (1H, m), of 2.81 (3H, users), is 2.88 (3H, users), 3,02-and 3.16 (1H, m), 3,51 (2H, s), 3,71-3,86 (1H, m), 4,20 (4H, q, J=7,1Hz), 4,82 (2H, s), 6,99 (1H, d, J=9,0 Hz), 7,05(1H, d, J=1,8 Hz), 7,18 (1H, DD, J=1,Hz, J=8,3 Hz), 7,22-7,37 (5H, m), 7,56 (1H, DD, J=1,8H, J=9,0 Hz), 8,01 (1H, users), 8,08 (1H, d, J=8,3 Hz), 9,29 (1H, users)

Table 63
ExampleStructureNMR (δ, 300MHz, CDC13)
9-21of 1.18 (6H, t, J=7,1Hz), 2,03 (3H, s), 3.53 (2H, s),to 4.14 (4H, q, J=7,1Hz), a 4.86 (2H, s), 6.97-7.05 (2H, m), 7.24-7.81 (15H, m), 8.35 (1H, users)
9-22< / br>
TPL 146,4-of 148.6
of 1.20 (6H, t, J=7,2 Hz), 3,52 (2H, s), and 3.72 (3H, s),4,18 (4H, q, J=7.2 Hz), a 4.83 (2H, s),6,83 (1H, users), of 4.95 (1H, DD, J=1,8gts, J=8,3 Hz), 7,14 (1H, d, J=8,3 Hz), 7.18 in-7,80 (15H, m)
9-23of 1.20 (6H, t, J=7,1Hz), a 2.36 (3H, s), of 3.57 (2H, s), 4,20 (4H, q, J=7,1 Hz), 4.85 (2H, s), 6,85 (1H, s), 7.18 in-to 7.59 (14H, m), 8,67 (1H, d, J=8,Hz), 12,71 (1H, users)
9-24to 1.19 (6H, t, J=7,2 Hz), 3,53 (2H, s), 4,17 (4H, q, J=7,2 Hz), 4,82 (2H, s), 6,89-of 6.96 (3H, m, 7,17-7,55 (17H, m), to 7.67 (1H, DD, J=1,5, 7,5Hz), to 8.45 (1H, d, J=8,Hz)
9-25to 1.21 (6H, t, J=7,1Hz)and 3.59 (2H, s), is 4.21 (4H, q, J=7,1Hz), to 4.87 (2H, s), 7,27-7,78 (15H, m), 8,67 (1H, d, J=8,3 Hz), being 9.61 (1H, users)and 11.1 (1H, users)

Table 64
ExampleStructureNMR (δ, 300MHz, CDC13)
9-26of 1.20 (6H, t, J=7,0Hz), was 1.94 (6H, s), 3,14 (2H, s), of 3.48 (2H, s), 4,19 (4H, q, J=7,0Hz), to 4.81 (2H, s), 6,83 (1H, d, J=2,0Hz), was 7.08 (1H, DD, J=2.0 a, 8,0 Hz), 7,27-to 7.59 (12H, m), 7,68 (1H, DD, J=1,2, 7,GC), by 8.22 (1H, d, J=8,5Hz)and 10.7 (1H, users)
9-27to 1.21 (6H, t, J=7,1Hz), 3,20 (3H, s)to 3.36 (3H, s), 3,52 (2H, s), is 4.21 (4H, q, J=7,1Hz), 4,82 (2H, s), 7.23 percent-to 7.61 (14H, m), 7,71 (1H, d, J=7,3 Hz), 8,31 (1H, d, J=8,4 Hz), 9,49 (1H, users)
9-28of 1.06 (6H, d, J=6,GC),of 1.20 (6H, t, J=7,2 Hz), 3,42-3,51 (1H, m), of 3.56 (2H, s), 4,20 (4H, q, J=7,2Hz), is 4.85 (2H, s), 7,28-to 7.77 (15H, m), 8,72 (1H, d, J=8,Hz), 11,81 (1H, users)
9-290,49 (3H, d, J=6,GC), of 0.90 (3H, d, J=6,GC), 1,14-1,25 (6H, m), 1,40 is 1.58 (1H, m), 2,41 (1H, d, J=3,GC), 3,51 (2H, d, J=3,GC), 3,81-3,88 (1H, m), as 4.02-4,18 (4H,m), a 4.83 (2H, s), 6,79 (1H, ), 7,05-7,69 (14H, m), 8,19 (1H, d, J=8,1 Hz), 9,01 (1H, users)

tr>
Table 65
ExampleStructureNMR (δ, 300MHz, CDC13)
2e)of 2.86(3H, users), with 2.93 (3H, users), of 3.56 (2H, s), to 7.09 (1H, d, J=2,0 Hz), 7.23 percent-7,71 (9H, m), 8,29 (1H, d, J=8,Hz), 9,06 (1H, users),
2-17 e)a 1.75 of 1.99 (4H, m), 3,32-to 3.52 (4H, m),3,53 (2H, s), 7,20-7,69 (10H, m), by 8.22 (1H, d, J=4,4 Hz), 9,74 (1H, users),

Preparative form

Hereinafter the present invention will be specifically illustrated with reference to the preparative form.

Preparative form 1

Film of controlled thickness were obtained using the composition of the gelatinous shell (a) in accordance with a customary method. Two sheets of film were introduced between the rotating left-right symmetric metal crimping rollers for rolling periodic profiles and molded outer shell soft capsules, whereas the filling solution was injected into the inside of the outer walls of soft capsules and simultaneously melted and sealed the outer wall of the soft capsules rotation of squeeze rollers, and then the film cut capsules. The capsules were dried in a rotary dryer and left to dry for 4 days, getting soft capsules. The following are specific examples of preparative forms.

Preparative Form1-1

(a) composition film
gelatin100 pieces
a solution of sugar alcohol derived from

corn starch
30 parts
purified water100 pieces
(b) filling solution (per capsule)
Ether of propylene glycol and fatty acids295 mg
ethanol105 mg

Preparative form 1-2

(a) composition film
Gelatin100 pieces
a solution of sugar alcohol derived from

corn starch
30 parts
purified water100 pieces
(b) filling solution (per capsule)
The compound of example 2-55 mg
Ether of propylene glycol and fatty acids291 mg
ethanol104 mg

Preparative form 1-3

a solution of sugar alcohol derived from

corn starch
(a) composition film
Gelatin100 pieces
30 parts
purified water100 pieces
(b) filling solution (per capsule)
The compound of example 2-55 mg
Ether of propylene glycol and fatty acids277 mg
ethanol148 mg

Preparative form 2

Connection example 2-22, excipient and binder were mixed in the usual way, getting granular powder. The resulting powder was mixed with baking powder and a lubricant, getting the powder to tablets in a conventional way. Powder alloy preformed, receiving tablets in the usual way. Specific examples of preparative forms below.

Preparative form 2-1

the compound of example 2-225 mg
lactose133,06 mg
crystalline cellulose18 mg
the hypromellose 29105.4 mg
crosspovidone18 mg
magnesium stearate0,54 mg

Preparative form 2-2

connect the tion of example 2-22 5 mg
lactose92,44 mg
corn starch15 mg
the hypromellose 29103.6 mg
carboximetilkrahmal3.6 mg
magnesium stearate0.36 mg

Preparative form 2-3

the compound of example 2-225 mg
D-mannitolto 158.4 mg
the hypromellose 29106 mg
the calcium silicate20 mg
crosspovidone10 mg
magnesium stearate0.6 mg

Pharmacological test

The test example 1

The inhibition activity milliosmoles triglyceride transfer using MTP

Microsome protein transfer of triglycerides (ICTR) from bovine liver was partially purified as described below. To bovine liver to obtain a preparation of homogenate was added to buffer (50 mm Tris, 250 mm sucrose, 1 mm etc, of 0.02% NaN3(pH 7,4)), and the mixture is homogenized under ice cooling, and then was centrifuged at HD (4°C, 30 minutes). The supernatant was brought to a pH of 5.1 with hydrochloric acid and was stirred for 30 minutes. The solution in addition C is was stripperella when HD (4° C, 30 minutes) and to loose the precipitate was added to 1 mm Tris-buffer and brought the pH of the mixture to 8.6 with sodium hydroxide. After adding a 2.7 M solution of ammonium sulfate and the mixture was stirred for 30 minutes, then centrifuged at HD (4°S, 40 minutes). The obtained supernatant served as untreated fractions of the extract materials and equipment stored at -80°in freezing conditions. When it is practical to use a fraction of the crude extract was purified MTP column chromatography on diethylaminoethyl(DEAE)-sepharose using a FPLC system (Liquid chromatography quick resolution) and purified materials used in the test.

Got a small liposome monolabeled vesicles (SUV) (a donor of 0.25 mol.% triolein, 5 mol.% cardiolipin), labeled14C-triolein, and unlabeled SUV-liposome (acceptor, a 0.25 mol.% triolein). A fixed number of donor, acceptor and materials were mixed with the sample dissolved in DMSO, or DMSO. The mixture was incubated in 15 mm Tris-cleaners containing hydrochloride buffer (pH 7.4)containing 40 mm sodium chloride, 1 mm add (ethylenediaminetetraacetic acid), a 0.02% NaN3and 0.5% bovine serum albumin at 37°C for one hour. Upon completion of the incubation to the above solution was added a suspension of DEAE-cellulose (50% vol./about.) in 15 mm Tris-cleaners containing hydrochloride buffer (pH 7.4), and the mixture was centrifuged for having Otdelenia donor and acceptor. The radioactivity of the acceptor was measured by liquid scintillation counter. Determined the value obtained by subtracting the radioactivity of the blank sample from the amount of radioactivity in the acceptor in the DMSO group, as MTP-mediated activity of TG transfer, and it was compared with the value obtained by subtracting the radioactivity of the blank sample from the radioactivity in the group of samples. A blank sample was obtained by adding 15 mm Tris-cleaners containing hydrochloride buffer (pH 7.4) instead of MTP. The degree of inhibition (%) was calculated from the measured values in accordance with the following equation.

The degree of inhibition (%)= 100x (1 minus(the radioactivity of the sample group minus the radioactivity empty groups)/(radioactivity in the DMSO group minus the radioactivity empty groups))).

50% degree of inhibition (IC50) was determined on the basis of the above equations. The results are presented in tables 66-70.

The test example 2

Inhibition of secretion of apolipoprotein b cells HepG2.

The HepG2 cells suspended in modified according to the method of Dulbecco environment Needle (DMEM) containing 10% fetal calf serum, 100 units/ml penicillin and 100 μg/ml streptomycin) and were placed on a 96-well plate (4x104cells/well), then incubated for 24 hours. After you remove the DMEM medium was replaced with medium containing the sample, attoreny in DMSO, or medium containing DMSO (concentration of DMSO: 0.5 percent), and conducted additional incubation for 24 hours, after which the supernatant was isolated and the concentration of APO-b In the supernatant was analyzed using enzyme-linked immunosorbent assay (ELISA).

ELISA was carried out as follows. Monoclonal antibody against APO-man (0.5 μg/well), diluted with a solution of sodium carbonate in strigidaemon buffer (50 ml, pH 9,6), were placed in a 96-well plate for ELISA and left at room temperature for 15 hours. After washing tablet in the hole put a blocking solution (250 μl/well) and left at room temperature for 1.5 hours. After washing tablet in the hole to put the standard and sample (100 µl/well) and left at room temperature for one hour. The standard has received increasing concentrations of purified APO-man with DMEM to 0-1000 ng/ml After washing tablet was added polyclonal antibody against APO-human horseradish peroxidase, which was diluted in the ratio 1:1000 DMEM (100 µl/well) and left at room temperature for one hour. After washing plansheta in the hole was placed a solution of 2,2-azinobis(3-ethylbenzothiazoline-6-sulfonic acid) (100 µl/well) and left at room temperature for one hour. The reaction was stopped by adding 2% of savelianskoy (100 µl/well) and measured the absorbance at 405 nm. The concentration of APO-b In the sample was calculated by using the standard curve for the standard. The degree of inhibition (%) was calculated from the analysis of values in accordance with the following equation.

The degree of inhibition (%)=100x(1 minus (the concentration of APO-group sample/concentration of APO-b In the DMSO group).

Based on the above equation was determined concentration of 50% inhibition (IC50).

The results are shown in tables 66-70.

10
Table 66
ExampleThe test example 1 inhibition of MTP, IC50(nm)Example

test 2 on the inhibition of the secretion of APO-B, IC50(nm)
ExampleExample

tests 1 to the MTP inhibition, IC50(nm)
The test example 2 inhibition of the secretion of APO-B, IC50(nm)
10,65,81-242850
1-3the 4.7of 5.751-43,4190
1-50,660,651-61,25,5
1-7at 7.553301-837,5720
1-9 5,953,21-113222
1-127,6631-135,8170
1-1482551-2266,5179,5
1-2354631-2558,4
1-266306201-27726
1-28356401-3184,561
1-328,67201-3423100
1-351,06,91-362,0150
1-373,5471-386,0320
1-390,661601-406,92,1
1-424,4351-450,390,46
1-474,57501-483,2the 9.7
1-49205,31-510,96530
1-526901-530,43860
1-625,0461-631690
1-66169,31-672728
1-699,1901-701,6270
1-711,81201-720,442,7
1-73-391-74-680

Table 67
ExampleThe test example 1 inhibition of MTP, IC50(nm)Example

test 2 on the inhibition of the secretion of APO-B, IC50(nm)
ExampleExample

tests 1 to the MTP inhibition, IC50(nm)
The test example 2 inhibition of the secretion of APO-B, IC50(nm)
1-75-971-76-120
1-77-3601-78-11
1-79-0,591-80-8,
1-81-0,491-82-0,53
1-83-0,231-84-4,4
1-85-3,2---
20,621,52-21,41,3
2-32,12,02-40,940,29
2-51,40,552-71,10,56
2-8-0,992-10-1,4
2-12-7,02-13-0,74
2-14-1,22-15-0,53
2-16-2,72-18-0,69
2-19-262-20-0,64
2-211,88,92-221,40,44
2-232,70,612-24-28
2-25-6,32-26-8,2
2-29-912-30-27
2-31-432-32-1,7
2-33-132-34-2,0
2-35-382-36-7,4
2-390,740,762-40-0,99
2-41-1,22-42-1,8

Table 68
ExampleThe test example 1 inhibition of MTP, IC50(nm)Example

test 2 on the inhibition of the secretion of APO-B, IC50(nm)
ExampleExample

tests 1 to the MTP inhibition, IC50(nm)
The test example 2 inhibition of the secretion of APO-B, IC50(nm)
2-43-9,02-44-33
2-45-392-46 -2,9
2-47-1,22-48-0,36
2-49-492-50-21
2-51-472-53-4,6
2-54-8,52-55-4,2
2-56-0,932-57-0,56
2-58-1,92-59-0,99
2-60-1,32-61-0,38
2-62-0,372-66-57
2-67-432-68-2,25
2-69-0,912-70-2,34
2-71-0,542-72-0,95
2-73-2,932-74-0,84
2-75-12,542-76- 0,85
2-77-2,742-78-0,14
2-79-1,32-80-0,79
2-81-0,962-82-to 4.41
2-83-8,872-84-2,01
2-85-0,492-86-0,42
2-88-1,922-90-1,74
2-91-0,542-92-1,47
2-93-45,82-95-18

td align="center"> 2,7
Table 69
ExampleThe test example 1 inhibition of MTP, IC50(nm)Example

test 2 on the inhibition of the secretion of APO-B, IC50(nm)
ExampleExample

tests 1 to the MTP inhibition, IC50(nm)
The test example 2 inhibition of the secretion of APO-B, IC50(nm)
2-96-81 2-97-22
2-98-0,972-99-19
2-102-14,632-103-42,6
2-104-to 3.582-105-0,2
2-106-0,442-107-50
2-108-0,822-109-0,93
2-110-0,652-114-3,1
2-115-442-117-38
2-118-49---
3-1,93-2-4,2
3-30,401,03-42,113
3-5-2,23-65,00,63
3-7-0,353-83,70,38
3-9-1,63-100,31
3-11-0,363-12-0,72
3-13-1,93-141364
3-15-to 49.9---
4-0,334-2-16
4-3-7,94-5-5,2
4-6-7,54-7-15
4-8-10---
53,1195-266,5875
5-36,286,55-42,457

td align="center"> -
Table 70
ExampleThe test example 1 inhibition of MTP, IC50(nm)Example

test 2 on the inhibition of the secretion of APO-B, IC50(nm)
ExampleExample

tests 1 to the MTP inhibition, IC50(nm)
The test example 2 inhibi the Finance secretion of APO-B, IC50(nm)
5-54,55,05-6a 3.9260
5-8143405-94,028
5-106,23005-111,35,1
5-12-1,35-13-2,4
5-14-0,345-15-6,4
5-16-3,05-17-5,2
63,4758,36-35,2510
6-8506306-1022870
6-146,3876-152,057
6-162,91706-172,3420
6-193,2356-219,8920
7equal to 4.9760,07-22,4626
7-516,2237--
833595---
9112609-24,2450
9-3-599-4-9,9
9-5-3,19-6-59
9-8-6,99-10-2,3
9-11202109-13-0,53
9-14-419-17-23
9-21-209-22-0,96
9-23-8,779-24-7,86
9-27-0,82---

The test example 3

Example with a load of olive oil

This test used the Syrian hamsters (age 9-11 weeks) without starvation. Previously collected blood from the orbital venous plexus, and the sample suspended in 0.5% methylcellulose (medium), and the suspension forced the nutrient is administered orally to hamsters at a dose of 0.2, 1, 3 or 10 mg/2 ml/kg Control group was injected only carrier in the same volume. Olive oil (2 ml/kg) was forcibly administered orally 30 minutes after injection of the sample, and blood was collected from orbital venous plexus after 4 hours. From blood was isolated plasma and determined the amount of triglycerides (TG) plasma using an automatic analyzer (Hitachi Co.). Data were expressed in units ΔTG(mg/DL)=value at time point 4 hours minus the value before the introduction. The degree of inhibition (%) was calculated from the data obtained on the basis of the following equation.

The degree of inhibition(%)=100x(1 minus ΔTG sample group/ΔTG control group). The results are presented in table 71.

Table 71
Example No.The test example 3. Inhibition of absorption of fat after loading olive oil in hamster ((mg/kg orally)

The degree of inhibition (%)
Example No.The test example 3. Inhibition of absorption of fat after loading olive oil in hamster ((mg/kg orally)

The degree of inhibition (%)
157(100)1-365(100)
1-559(3)1-654(10)
1-35 59(100)1-4571(100)
1-6652(100)1-7254(100)
295(10)2-296(10)
2-368(3)2-478(3)
2-570(3)2-758(3)
2-889(3)2-1370(3)
2-1480(3)2-1581(3)
2-1858(3)2-2261(3)
2-2555(3)2-3968(3)
2-4887(3)--
3-378(10)3-580(10)
3-652(3)3-774(3)
3-860(3)3-1085(3)
3-1175(3)--
5-978(100)5-1164(100)
9-1054(3)9-1370(3)

The test example 4

Test of inhibition of the release of TG in the liver

This test used the Syrian hamsters (age 9-11 weeks), which were not fed during one the day before the test.

Previously collected blood from ocular venous plexus, and the sample forcibly administered orally to hamsters at a dose of 30, 100 or 300 mg/2 ml/kg and the control group was administered the same amount of media. 30 minutes after this injection the rats intravenously injected Triton WR 1339 (2 ml/kg). Two hours later, collected the blood of the ophthalmic venous plexus and the plasma was separated from blood. The amount of TG in plasma were determined using an automatic analyzer (Hitachi Co.). Data were expressed in units of the speed of release of TG (mg/DL/min)=(value after 2 hours minus the value before the introduction)/120. The degree of inhibition was calculated from the data obtained on the basis of the following equation.

The degree of inhibition(%)=100x(1 minus the rate of release of TG for sample/the rate of release of TG for the control group). The results are presented in table 72.

Table 72
Example No.The test example 4. Inhibition of release of TG in the liver of the hamster (()mg/kg orally)

The degree of inhibition (%)
Example No.The test example 4. Inhibition of release of TG in the liver of the hamster (()mg/kg orally)

The degree of inhibition (%)
119(300)1-60(100)
1-359(300)2-50(100)
2-220(30)2-396(100)
3-318(100)-

The test example 5

Test the combined application

White Japanese rabbits (male, age 19 weeks, JW received from Kitayama Labes Co., Ltd) pre-fed so that they could receive food with high cholesterol content (RC-4 with the addition of 0.3% cholesterol +3% peanut oil, a product of Oriental Yeast Co., Ltd) at the rate of 70 g/day before restricting food in one day. Rabbits fed thus used as a model loaded with cholesterol of rabbits, and create groups with this model has been conducted so that no differences (variations) in the amount of cholesterol in blood plasma among each group (five rabbits per group). After sampling blood from the ear artery of the compounds of examples 2-5, simvastatin and compounds of examples 2-5 plus simvastatin was added to the diet with a high content of cholesterol in the dose shown in the table below, and rabbits were fed this diet. The rabbits were 70 g of food each morning. Blood samples were collected from the ear artery after 6 hours after feeding on day 4 of the introduction, and analyzed the level of cholesterol is in the blood plasma. Table 73 shows an increased amount of cholesterol in plasma on day 4, since the formation of groups.

Table 73
Increased total cholesterol (mg/DL)
Control80,0
Simvastatin (1 mg/kg)48,6
Example 2-5 (10 mg/kg)8,6
Example 2-5(10 mg/kg) + Simvastatin (1 mg/kg)2,1

Example test 6

Determination of plasma concentrations

This test used the Syrian hamsters (age 9-11 weeks) without starvation. The sample suspended in 0.5% methylcellulose (medium), and the suspension is forcibly administered orally to hamsters at a dose of from 30 to 100 mg/2 ml/kg After a fixed period of time the blood samples were partly collected from the ophthalmic venous plexus and hamsters were subjected to laparotomy under conditions of anesthesia with ether, and then collected the blood from the portal vein. The blood was immediately cooled on ice for separation of plasma. Part of the blood plasma were extracted with an organic solvent, and provided the supernatant. The concentration of the sample (unmodified form) and metabolites in the supernatant was quantified using high-performance liquid is based chromatography/mass spectrometry (LC/MS) when compared with the chromatogram of synthetic standard.

16,9
Table 74
ConnectionDose (mg/kg)ComponentBlood from the portal vein (µm)Peripheral

blood (µm)
1 h2 hours4 h1H2H4h
1-230unmodified form<0,2<0,2<0,2<0,2<0,2<0,2
metabolite1,62,26,70,91,32,9
1-1230unmodified form<0,2<0,2<0,2<0,2<0,2<0,2
metabolite11,818,224,47,312,115,4
1-1330unmodified form<0,2<0,2<0,2<0,2<0,2<0,2
metabolite11,820,627,310,918,3
2-530unmodified form0,010,030,01<0,2<0,2<0,2
metabolite0,330,730,380,010,010,02

The test example 7

Test metabolic stability in liver S9 and S9 of the small intestine

S9 liver of human and hamster (final concentration: 2 mg protein/ml) and S9 of the small intestine of human and hamster (final concentration: 2 mg protein/ml) suspended in 100 mm califofnia buffer (pH 7.4, containing βnicotinamide dinucleotide phosphate: 1.3 mm, D-glucose-6-phosphate: 3.3 mm magnesium chloride: 3.3 mm glucose-6-phosphate dehydrogenase: a 0.4 u/ml). The suspension was mixed with sample solution (example 2-5) in DMSO. The solutions were incubated at 37°C for 0, 10 and 60 minutes and was added to a mixture of an organic solvent. The solutions were centrifuged and the concentration of the sample (unmodified form) in the supernatant was determined using high-performance liquid chromatography/mass spectrometry (LC/MS). On the basis of the obtained data was calculated percentage of balance (%) in accordance with the following equation.

The percentage of balance (%)= number of sample in 10 minutes or 60 minutes after inquire the project/number of sample in zero time after incubation x 100.

Table 75
PeopleHamster
The percentage of balance (%) after 10 minutesThe percentage of balance (%) after 60 minutesThe percentage of balance (%) after 10 minutesThe percentage of balance (%) after 60 minutes
S9 of the small intestine97,691,529,014,1
S9 liver7,94,32,40

The test example 8

Inhibitory activity against the secretion of materials, equipment and APO-when inhibition by metabolites

Ways, similar to the examples of tests 1 and 2, we analyzed the activity of the metabolites. The results are presented in the table below.

Table 76
ConnectionThe main metaboliteInhibition of MTP IC50(nm)Inhibition of the secretion of APO-IC50(nm)
1>1000>10000
>1000>10000
1-35 >1000>10000
>1000>10000

Table 77
ConnectionThe main metaboliteInhibition of MTP IC50(nm)Inhibition of the secretion of APO-IC50(nm)
2-5>10000>10000
>1000>10000
2-17->10000
>1000>10000

Table 78
ConnectionThe main metaboliteInhibition of MTP IC50(nm)Inhibition of the secretion of APO-IC50(nm)
3-4>1000>10000
>1000>10000

Tests toxi is ness

The following are the test results of the compounds according to the invention for toxicity. The test compound (hereinafter IP) was the compound obtained according to example 2-5 (table).

Test 1

IP disposable administered orally by rats when injected quantity of 200 mg/kg body weight and dogs when the input amount of 50 mg/kg body weight. Symptoms of toxicity was not detected, indicating a lack of toxicity in the IP or its low toxicity. Accordingly, the input dose less than 50 mg/kg body weight in relation to these animals are quite safe.

Test 2

IP disposable was administered by mouth within 1 month rats when injected quantity in 10, 20 or 50 mg/kg body weight and dogs when the input number of 0.2, 2 or 20 mg/kg of body weight. In any case, symptoms of toxicity in the body as a whole, as well as in organs and tissues, including the genitals.

Test 3

IP was subjected to test for reverse mutation using microorganisms. Found no induction of reverse mutations. IP was also subjected to the test chromosome aberration using cell cultures of mammalian species. Found no induction of chromosomal aberrations.

The tests show no toxicity or low toxicness the compounds according to the invention.

Industrial applicability

From the above examples of trials 1-3 it is clear that new compounds and their pharmaceutically acceptable salts according to the present invention have excellent MTP-inhibiting activity and also effectively inhibit the absorption of triglycerides. In addition, the example test 4 it is obvious that, even if the compounds of the present invention is administered at a high dose, the degree of release of TG in the liver is 18-19% or below, more effectively 9% or below, especially now 0% or below and, thus, the compounds of the present invention slightly inhibit the release of TG in the liver. In addition, the example test 6 shows that the active compound after absorption in the small intestine are present in the portal vein in very small quantities, and because most (from 8-fold to 80-fold amount) of such active compounds is metabolites, they do not reach the liver. In addition, the example test 7 shows that a small number of active connections that have reached the liver, rapidly metabolized to metabolites. Additionally, the test example 8 confirms that the ester fragment of these metabolites is cleaved by hydrolysis, and thus they exhibit a slight MTP inhibitory activity or not show it at all. Next, etc which measures test 5 shows that combined use of the compounds of the present invention together with other agents for treatment of hyperlipidemia (agents Statesboro type) can significantly inhibit the increase of cholesterol level and provides an extremely remarkable synergistic effect. These facts show that the compounds of the present invention can be used in combination with other agents, in particular with other agents for treatment of hyperlipidemia, arteriosclerosis, coronary artery disease, obesity, diabetes or hypertension.

From the above facts it is clear that the new compounds of the present invention and their pharmaceutically acceptable salts can inhibit the absorption of fats in the small intestine and, in addition, do not inhibit the release of TG in the liver. This means that the compounds according to this invention do not inhibit MTP in the liver, but selectively inhibit MTP in the small intestine.

Therefore, selective inhibition of MTP activity in the small intestine compounds of the present invention could reduce the absorption of fat that allows you to control the lipoproteins, such as triglyceride, cholesterol and LDL, etc. in the blood or control the fats in the cells. Further, since the compounds of the present invention do not act on MTP in the liver, the accumulation of triglyceride in the liver does not occur is it. Therefore, it can be expected that the development of fatty liver disease as a side effect will be inhibited. Thus, it is possible to say that the compounds of the present invention are new MTP inhibitors, does not exhibit side effects such as fatty liver, etc. or, in other words, they represent new agents for the treatment or prophylaxis of hyperlipidemia, arteriosclerosis, coronary artery disease, obesity, diabetes or hypertension and, in addition, for the treatment or prevention of pancreatitis, hypercholesterolemia, hypertriglyceridemia, etc. that are rarely act on MTP in the liver and essentially only inhibit MTP in the small intestine.

1. Ester compound represented by formula (1)

where each of R1and R2represents hydrogen, C1-C6-alkyl; C3-C7-cycloalkyl; C1-C6-alkoxy; halogen-(C1-C6-alkyl; halogen-(C1-C6-alkyloxy; phenyl which may be substituted by 1-3 substituents selected from the group comprising C1-C6-alkyl, C1-C6-alkoxy, C2-C7alkenyl, halogen, nitro, cyano, C1-C6-acyl and halogen-C1-C6-alkyl; phenylalkyl; phenoxy, which can be substituted by 1-3 substituents, selected the C group, including C1-C6-alkyl, C1-C6-alkoxy, halogen, nitro, cyano, C1-C6-acyl and trifluoromethyl; phenylcarbinol, which can be substituted by 1-3 substituents selected from the group comprising C1-C6-alkyl, C1-C6-alkoxy, halogen, nitro, cyano, and C1-C6-acyl; 5-membered heterocycle containing N and/or S as heteroatoms which can be substituted by 1-3 substituents selected from the group comprising C1-C6-alkyl, C1-C6-alkoxy, halogen, nitro, cyano, and C1-C6-acyl; C2-C7-alkoxycarbonyl; halogen; C2-C6alkenyl; or-N(R40)(R41), where each of R40and R41independently represents hydrogen or phenyl which may be substituted by 1-3 substituents selected from the group comprising C1-C6-alkyl, C1-C6-alkoxy, halogen, nitro, cyano, C1-C6-acyl and trifluoromethyl;

ring a represents a phenyl; 5-membered or 6-membered heterocycle containing N and/or S as heteroatoms; or

or

X represents-COO-(CH2)n- or-CON(R10)-(CH2)n-where R10represents hydrogen, C1-C6-alkyl or C3-C7-cycloalkyl, and n is predstavljaet an integer from 0 to 3;

each of R3and R4independently represents hydrogen; hydroxy; halogen; C1-C6-alkyl which may be substituted by 1-5 substituents selected from the group of hydroxy; C1-C6-alkoxy; halogen-(C1-C6-alkyl; phenylalkylamine; C1-C6-acyl; 5-membered heterocycle containing N and/or S as heteroatoms which can be substituted by 1-3 substituents selected from the group comprising C1-C6-alkyl, C1-C6-alkoxy, halogen, nitro, cyano, and C1-C6-acyl; -CON(R11)(R12) (where each of R11and R12independently represents hydrogen, C1-C6-alkyl; phenylalkyl, which can be substituted by 1-3 substituents selected from the group comprising C1-C6-alkyl, C1-C6-alkoxy, halogen, nitro, cyano, and C1-C6-acyl; or C1-C6-alkoxy; or R11and R12taken together with the nitrogen atom to which they are attached, form

where p is an integer from 0 to 1), - (CH2)q-N(R13)(R14) (where each of R13and R14independently represents hydrogen, C1-C6-alkyl, C2-C7-alkoxycarbonyl or C1-C6-acyl, or R13and R14taken together with economista, to which they are attached, form

where R has the same meaning as defined above, and q is an integer from 0 to 3), or-CO(R15) (where R15represents hydroxy; C1-C6-alkoxy; funeralcare, which can be brewed 1-3 substituents selected from the group comprising C1-C6-alkyl, C1-C6-alkoxy, halogen, nitro, cyano, and C1-C6-acyl; C1-C6-alkylamino; or C1-C6alkyl);

the ring is a

or

where K represents the integer 1; or a ring, taken together with R3, R10and nitrogen associated with R10forms

or

Alkl1represents alcander;

Alkl2represents alcander;

l represents an integer from 0 to 2;

m is an integer from 0 to 3;

D represents C1-C6-alkyl; C2-C6alkenyl; C2-C7-alkoxycarbonyl; -N(R42)-CO(R43(where R 42represents hydrogen or C1-C6-alkyl, and R43is a biphenyl or biphenylyl); or a group represented by the following formula:

(where each of R5, R6and R7independently represents hydrogen, C1-C6-alkyl, C1-C6-alkoxy; halogen; nitro; amino; phenyl which may be substituted by 1-3 substituents selected from the group comprising C1-C6-alkyl, C1-C6-alkoxy, halogen, nitro, cyano, and C1-C6-acyl; or - (CH2)r-CON(R16)(R17) (where each of R16and R17independently represents hydrogen, C1-C6-alkyl or halogen-C1-C6-alkyl, and r is an integer from 0 to 3);

the ring is a phenyl; naphthyl; phenylcarbonylamino; 5-membered or 6-membered heterocycle containing N and/or S as heteroatoms; C3-C7-cycloalkyl; or phenylalkyl; or ring, taken together with R7and R8forms

each of R8and R9independently represents hydrogen, C1-C6-alkyl; phenyl which may be substituted by 1-5 substituents selected from the group comprising C1-C6-alkoxy, halogen, carboxy, guide is hydroxy, amino, nitro and cyano; hydroxy-C1-C6-alkyl; -CON(R18)(R19) (where each of R18and R19independently represents hydrogen, C1-C6-alkyl; C3-C7-cycloalkyl; halogen-(C1-C6-alkyl, C1-C6-alkoxyalkyl;

or phenyl which may be substituted by 1-3 substituents selected from the group comprising C1-C6-alkyl, C1-C6-alkoxy, halogen, nitro, cyano, and C1-C6-acyl; -COO(R20or -(CH2)s-OCO R20) (where R20represents a C1-C6-alkyl or C3-C7-cycloalkyl; s is an integer from 0 to 3), -N(R21)(R22) (where each of R21and R22independently represents hydrogen, C1-C6-alkyl, C1-C6-acyl or C1-C6-alkylsulfonyl, or R21and R22taken together with the nitrogen to which they are connected, form

R8and R9taken together, may form With3-C7-cycloalkyl,

or its pharmaceutically acceptable salt.

2. Ester compound or its pharmaceutically acceptable salt according to claim 1, where D represents C1-C6-alkyl, C2-C6alkenyl,2-C7-alkoxycarbonyl or-N(R42)-CO(R43),where each of R 42and R43has the same meaning as defined above.

3. Ester compound or its pharmaceutically acceptable salt according to claim 1, where D represents a group represented by the formula

where each of R5, R6and R7has the same meaning as defined above.

4. Ester compound or its pharmaceutically acceptable salt according to claim 3, where the ring is a

or

where q is an integer from 0 to 3.

5. Ester compound or its pharmaceutically acceptable salt according to claim 4 in which the ring represents a

or

6. Ester compound or its pharmaceutically acceptable salt according to claim 5, where the ring And represents a

or

7. Ester compound or its pharmaceutically acceptable salt according to claim 6, where X represents the Oh-CON(R 10)-(CH2)n-, where each R10and n have the same meanings as defined above.

8. Ester compound or its pharmaceutically acceptable salt according to claim 6, where X represents-COO-(CH2)n-, where n has the same meaning as defined above.

9. Ester compound or its pharmaceutically acceptable salt according to claim 7, where n is equal to 0.

10. Ester compound or its pharmaceutically acceptable salt according to claim 1, represented by formula (1')

where each of R2'and R2"independently represents hydrogen, C1-C6-alkyl, C3-C7-cycloalkyl, C1-C6-alkoxy, halogen, halogen C1-C6-alkyl, C1-C6-acyl, C2-C6alkenyl or cyano;

X1represents-O - or-NR10-where R10represents hydrogen, C1-C6-alkyl or C3-C7-cycloalkyl; and

each of R1, R3, R4, R5, R6, R7, R8, R9ring With the indices l and m has the same meaning defined above,

or its pharmaceutically acceptable salt.

11. Ester compound or its pharmaceutically acceptable salt of claim 10, where the ring is a

or

where q is an integer from 0 to 3.

12. Ester compound or its pharmaceutically acceptable salt according to claim 11, where X1represents-N(R10)-, where R10has the same meaning as defined above.

13. Ester compound or its pharmaceutically acceptable salt according to claim 11, where X1represents-O-.

14. Ester compound or its pharmaceutically acceptable salt according to any one of PP-13, where the group -(CH2)l- located in the h-position of the benzene ring in the formula (1').

15. Ester compound or its pharmaceutically acceptable salt according to any one of PP-13, where the group -(CH2)1- located in the i-position of the benzene ring in the formula (1').

16. Ester compound or its pharmaceutically acceptable salt according to clause 12, where each of R8and R9independently represents-CON(R18)(R19)-, where each R18and R19has the same meaning as defined above.

17. Ester compound or its pharmaceutically acceptable salt according to clause 12, where each of R8and R9independently represents-COO(R20)-, where R20have the t same value as specified above.

18. Ester compound or its pharmaceutically acceptable salt according to clause 16, where the ring is a phenyl or naphthyl.

19. Ester compound or its pharmaceutically acceptable salt 17, where the ring is a phenyl or naphthyl.

20. Ester compound or its pharmaceutically acceptable salt p, where the ring is a phenyl.

21. Ester compound or its pharmaceutically acceptable salt according to claim 19, where the ring is a phenyl.

22. Ester compound or its pharmaceutically acceptable salt according to clause 16, where the ring is a C3-C7-cycloalkyl.

23. Ester compound or its pharmaceutically acceptable salt 17, where the ring is a3-C7-cycloalkyl.

24. Ester compound or its pharmaceutically acceptable salt according to clause 16, where the ring is a

or

25. Ester compound or its pharmaceutically acceptable salt 17, where the ring is a

or

26. Ester compound or its pharmaceutically acceptable the ol according to claim 1, which is chosen from the group including

2,2-bis-ethylcarboxyl-2-phenethyl ester {4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ester of 2-phenyl-2-{2-[4-(4'-triptorelin-2-carbonyloxy)phenyl]acetoxymethyl}malonic acid,

diethyl ether 2-(2-{3-methyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{4-[methyl-(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-ethyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

9-(2,2,2-triptoreline)-N-fluoren-9-ymetray ester {4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

9-(2,2,2-triptoreline)-N-fluoren-9-ymetray ester 2-{4-[(4'-triptorelin-2-carbonyl) amino)phenyl}propionic acid,

2-phenyl-2-(2,2,2-triptoreline)ethyl ester {4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ester of 2-phenyl-2-(2-{4-[(4'-triptoreline-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

1-(2,2,2-triptoreline)cyclopentylmethyl ester {4-[(4'-triptorelin-2-carbonyl)amino]phenyl)acetic acid,

diiso rapelay ester 2-phenyl-2-(2-{4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

2-phenyl-2,2-bis-(2,2,2-triptoreline)ethyl ester {4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

dimethyl 2-phenyl-2-(2-{4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diethyl ether 2-cyclopentyl-2-(2-{4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

1-(2,2,2-triptoreline)cyclohexylmethyl ester {4-[(4'-triptorelin-2-carbonyl)amino] phenyl}acetic acid,

diethyl ester of 2-phenyl-2-{2-[4-(2-trifluoromethyl-benzoylamine)phenyl]acetoxymethyl}malonic acid,

diethyl ether 2-{2-[4-(2-phenoxyethylamine)phenyl]acetoxymethyl}-2-phenylmalonate acid,

diethyl ether 2-{2-[4-(2-butoxycarbonylamino)phenyl]acetoxymethyl}-2-phenylmalonate acid,

diethyl ester of 2-phenyl-2-{2-[4-(2-triftormetilfosfinov)phenyl]acetoxymethyl}malonic acid,

diethyl ether 2-{2-[4-(2-benzoylbenzoate)phenyl]acetoxymethyl}-2-phenylmalonate acid,

diethyl ether 2-{2-[4-(2-benzoylmethylene)phenyl]acetoxymethyl}-2-phenylmalonate acid,

dicyclohexylamine ester 2-phenyl-2-(2-{4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

2,2-bis-cyclohexylcarbonyl-2-phenethyl ester {4-[(4'-is reformative-2-carbonyl)amino]phenyl}acetic acid,

2-phenyl-2,2-bis-phenylcarbamoyloxy ester {4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-isopropylcarbamate-2-phenethyl ester {4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ether 2-benzyl-2-(2-{4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diethyl ether 2-(2-{2-methyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

4-[2-phenyl-2,2-bis-(2,2,2-triptoreline)ethoxycarbonylmethyl]phenyl ester of 4'-triptorelin-2-carboxylic acid,

4-[2-phenyl-2,2-bis-(2,2,2-triptoreline)ethoxycarbonylmethyl]phenyl ether-biphenyl-2-carboxylic acid,

4-[2-phenyl-2,2-bis-(2,2,2-triptoreline)ethoxycarbonylmethyl]phenyl ester 2-butoxybenzoic acid,

diethyl ether of 2-cyclohexyl-2-(2-{4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

2-phenyl-2,2-bis-(2,2,2-triptoreline)ethyl ester {4-[(biphenyl-2-carbonyl)amino]phenyl}acetic acid,

2-phenyl-2,2-bis-(2,2,2-triptoreline) ethyl ester [4-(2-phenoxy-benzoylamine)phenyl]acetic acid,

diethyl ester of 2-phenyl-2-(2-{2-trifluoromethyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}Aceto simetal)malonic acid,

2-phenyl-2,2-bis-profilerenumeration ester {4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-methylcarbamoyl-2-phenethyl ester {4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ether 2-pyridin-2-yl-2-(2-{4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diethyl ether 2-pyridin-3-yl-2-(2-{4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

4-(2,2-bis-ethylcarboxyl-2-phenyl-ethoxycarbonylmethyl)phenyl ether 4'-triptorelin-2-carboxylic acid,

diethyl ester of 2-phenyl-2-(2-{3-trifluoromethyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

2-phenyl-2,2-bis-(2,2,2-triptoreline)ethyl ester [4-(2-butoxy-benzoylamine)phenyl]acetic acid,

2,2-bis-butylcarbamoyl-2-phenethyl ester {4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ether 2-(2-{4-[(9-oxo-9h-fluoren-1-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{4-[(9h-fluoren-1-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-methyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid is you,

diethyl ether 2-(2-{4-[(4'-methylbiphenyl-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{4-[(4'-methoxybiphenyl-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

3,3-bis-ethylcarbazole-3-phenylpropionic ester {4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

3-phenyl-3,3-bis-propellerblades-propyl ester {4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ester {4-[(biphenyl-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ester [4-(2-phenoxy-benzoylamine)phenyl]acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ester [4-(2-butoxy-benzoylamine)phenyl]acetic acid,

diethyl ester of 2-phenyl-2-(2-{4-[(3'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diethyl ether 2-(2-{4-[2-(4-fluoro-benzoyl)benzoylamine]phenyl}acetoxymethyl)-2-phenylmalonate acid,

4-(2,2-bis-ethylcarboxyl-2-phenyl-ethoxycarbonylmethyl)-2-hlorfenilovy ether 4'-triptorelin-2-carboxylic acid,

diethyl ester of 2-phenyl-2-{2-[4-(2-thiophene-3-yl-benzoylamine)phenyl]acetoxymethyl}malonic acid,

diethyl ether 2-(2-{4-[(biphenyl-3-carbonyl)amino]phenyl}acetoxymethyl)-2-dryer is Lanovoy acid,

diethyl ether 2-(2-{4-[isopropyl-(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{4-[cyclohexyl-(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-{2-[4-(2-isopropyl-benzoylamine)phenyl]acetoxymethyl}-2-phenylmalonate acid,

diethyl ether 2-{2-[4-(2-benzyl-benzoylamine)phenyl]acetoxymethyl}-2-phenylmalonate acid,

dipropionyl ester 2-phenyl-2-(2-{4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diisobutylamine ester 2-phenyl-2-(2-{4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diethyl ester of 2-phenyl-2-{2-[4-(2-triptoreline-benzoylamine)phenyl]acetoxymethyl}malonic acid,

diethyl ether 2-{2-[4-(2-butoxycarbonyl-benzoylamine)phenyl]acetoxymethyl}-2-phenylmalonate acid,

2,2-bis-isobutylamino-2-phenethyl ester {4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-(3-methyl-butylcarbamoyl)-2-phenethyl ester {4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ether 2-(2-{4-[ethyl-(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

2,bis-ethylcarboxyl-2-phenethyl ester [4-(2-cyclohexyl-benzoylamine)phenyl]acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ester (4-[(4'-chlorobiphenyl-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ester {4-[(3',4'-dichlorobiphenyl-2-carbonyl)amino]phenyl}acetic acid,

2-phenyl-2,2-bis-propellerblades-ethyl ester {3-methyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis(2-methoxy-ethylcarbamate)-2-phenethyl ester {4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ether 2-[2-(4-{[2-methyl-4-(4-trifluoromethyl-phenyl)thiazole-5-carbonyl]amino}phenyl)acetoxymethyl]-2-phenylmalonate acid,

2,2-bis-ethylcarboxyl-2-phenethyl ester (4-{[2-methyl-4-(4-trifluoromethyl-phenyl)thiazole-5-carbonyl]amino}phenyl)acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ester (4-{[2-(4-trifluoromethyl-phenyl)pyridine-3-carbonyl]amino}phenyl)acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ester (3-methyl-4-{[2-(4-trifluoromethyl-phenyl)pyridine-3-carbonyl]amino}phenyl)acetic acid,

diethyl ether 2-(2-{3-ethyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-isopropyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ether 2-(2-{3-isopropyl-4-[(4'-trifluoromethyl shall iphenyl-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

3,3-bis-ethylcarbazole-3-phenylpropionyl ether {3-ethyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-isobutyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ether 2-(2-{3-isobutyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-chloro-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-bromo-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2-phenyl-2,2-bis-propellerblades-ethyl ester {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-methylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

3,3-bis-ethylcarbazole-3-phenylpropionyl ether {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate is islote,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-benzylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

4,4-bis-ethylcarbamate-4-privately ether {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-diethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-diisopropylamino-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ether 2-(2-{3-diethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-diisopropylamino-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-(isopropylaminocarbonyl)-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ether 2-(2-{3-(ethylmethylamino)-4-[(4'-triptorelin-2-carbonyl) amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

2,2-bis-ethylcarboxyl-2-phenethyl ester (3-(ethylmethylamino)-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

3,3-bis-ethylcarbazole-3-phenylpropionyl ether {-(ethylmethylamino) -4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3- (piperidine-1-carbonyl) -4- [(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-(pyrrolidin-1-carbonyl)-4- [(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-(pyrrolidin-1-carbonyl)-4- [(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-(methylpropanoyl)-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

3,3-bis-ethylcarbazole-3-phenylpropionyl ether {3-(methylpropanoyl)-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2-ethylcarboxyl-2-phenethyl ester (3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ester of 2-phenyl-2-(2-{3-(pyrrolidin-1-carbonyl)-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diethyl ester of 2-phenyl-2-(2-{3-(piperidine-1-carbonyl)-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

2-phenyl-2-propionylcarnitine ether {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2-phenyl-2-propionylcarnitine ether 3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2-(2,5-dioxo-pyrrolidin-1-yl)-2-phenethyl ether {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2-ethylcarbamate-benzyl ether {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2-ethylcarboxylate-benzyl ether {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

hydrochloride of 2-isopropylamino-2-phenethyl ester {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ester [3-dimethylcarbamoyl-4-(2-trifluoromethyl-benzoylamine)phenyl]acetic acid,

diethyl ether 2-{2-[3-dimethylcarbamoyl-4-(2-trifluoromethyl-benzoylamine)phenyl]acetoxymethyl}-2-phenylmalonate acid,

diethyl ether 2-[2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxy)ethyl]-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-forbiden-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{4-[(4'-bromobiphenyl-2-carbonyl)amino]-3-dimethylcarbamoyl}acetoxymethyl)-2-phenylmalonate acid,

2-acetylamino-2-phenethyl ether {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}is kusnoy acid,

2 Butylimino-2-phenethyl ether {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ester [4-(2-benzoyl-benzoylamine)-3-dimethylcarbamoyl]acetic acid,

diethyl ether 2-{2-[4-(2-benzoyl-benzoylamine)-3-dimethylcarbamoyl]acetoxymethyl}-2-phenylmalonate acid,

dimethyl 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-cyclopentyl-2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl) malonic acid,

diethyl ether of 2-cyclohexyl-2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diethyl ether 2-(2-{4-[(4'-chlorobiphenyl-2-carbonyl)amino]-3-dimethylcarbamoyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{4-[(4'-acetyl-biphenyl-2-carbonyl)amino]-3-dimethylcarbamoyl}acetoxymethyl)-2-phenylmalonate acid,

2,2-bis-ethylcarboxyl-2-phenethyl ester [3-dimethylcarbamoyl-4-(2-phenoxy-benzoylamine)phenyl]acetic acid,

diethyl ether 2-{2-[3-dimethylcarbamoyl-4-(2-phenoxy-benzoylamine) phenyl]acetoxymethyl}-2-phenylmalonate acid,

etilogy ether 2-(2-{4-[(4'-cyanobiphenyl-2-carbonyl)amino]-3-dimethylcarbamoyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4-methyl-4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(5-methyl-4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

2 methanesulfonamido-2-phenethyl ether {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

ethyl ester of 3-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxy)-2-phenylpropionic acid,

2-(methylpropionamide)-2-phenethyl ether {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ether 2-[3-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxy)propyl]-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(5-methoxy-4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{4-[(5-chloro-4'-triptorelin-2-carbonyl)amino]-3-dimethylcarbamoyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(6-methyl-4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

di-2,2,2-triptoreline EF the p 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[[2'-fluoro-4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{5-dimethylcarbamoyl-2-fluoro-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-bromo-5-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-chloro-5-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl) amino] phenyl }acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(3'-fluoro-4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{4-[(3'-chloro-4'-triptorelin-2-carbonyl)amino]-3-dimethylcarbamoyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-(5-nitropyridine-2-yl)malonic acid,

diethyl ether 2-(5-aminopyridine-2-yl)-2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-pyridin-2-elmaloglou acid,

diethyl ether 2-(2-{3-chloro-5-dimethylcarbamoyl-2-fluoro-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-bromo-5-dimethylcarbamoyl-2-fluoro-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl) amino]phenyl}acetoxymethyl)-2-o-talismanova acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino] phenyl }acetoxymethyl)-2-m-talismanova acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-p-talismanova acid,

diethyl ether 2-(2-chlorophenyl)-2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diethyl ether 2-(3-chlorophenyl)-2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diethyl ether 2-(4-chlorophenyl)-2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylethanol acid,

diethyl ether 2-(2-{3-di is ethylcarbitol-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-(2-methoxyphenyl)malonic acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-(3-methoxyphenyl)malonic acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl) amino]phenyl}acetoxymethyl)-2-(4-methoxyphenyl)malonic acid,

diethyl ether 2-(2-{4-[(5,4'-bis-triptorelin-2-carbonyl)amino]-3-dimethylcarbamoyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{4-[(6-chloro-4'-triptorelin-2-carbonyl)amino]-3-dimethylcarbamoyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(6-fluoro-4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-[2-(2-{3-dimethylcarbamoyl-4-[(5-methyl-4'-triptorelin-2-carbonyl)amino]phenyl}acetoxy)ethyl]-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(5-ethoxy-4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(5-isopropoxy-4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-[2-(2-{4-[(5',4'-bis-triptorelin-2-carbonyl)amino]-3-dimethylcarbamoyl}acetoxy)ethyl]-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(6-methoxy-4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(3-methyl-4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-{2-[4-(2,4-bis-trifluoromethyl-benzoylamine)-3-dimethylcarbamoyl]acetoxymethyl}-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-methylbiphenyl-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether with 2-ethyl-4-trifluoromethyl-benzoylamine)phenyl]acetoxymethyl}-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-ethyl-biphenyl-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-isopropyl-biphenyl-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-isopropyl-biphenyl-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-{2-[3-dimethylcarbamoyl-4-(2-Isopropenyl-4-trifluoromethyl-benzoylamine)phenyl]acetoxymethyl}-2-phenylmalonate acid,

diethyl ether 2-{2-[3-dimethylcarbamoyl-4-(2-isopropyl-4-trifluoromethyl-benzoylamine)phenyl]acetoxymethyl-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[2-(3-trifluoromethyl-phenylamino)benzoylamine]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-{2-[3-dimethylcarbamoyl-4-(4'-triptorelin-2-carbonyloxy)phenyl]acetoxymethyl}-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[2-(3-trifluoromethyl-phenoxy)benzoylamine]phenyl}acetoxymethyl)-2-phenylmalonate acid,

2-ethyl-2-privately ether {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[2-(4-trifluoromethyl-phenoxy)benzoylamine]phenyl}acetoxymethyl)-2-phenylmalonate acid,

1-phenyl-cyclopropylmethyl ether {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-definiately ether {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

1-phenyl-cyclopentylmethyl ether {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

3-hydroxy-2-hydroxymethyl-2-phenylpropionyl ether {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

3-acetoxy-2-acetoxymethyl-2-phenylpropionyl ether {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)AMI is about]phenyl}acetic acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-thiophene-2-elmaloglou acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-thiophene-3-elmaloglou acid,

diethyl ether 2-(2-{4-dimethylcarbamoyl-5-[(4'-triptorelin-2-carbonyl)amino]pyridin-2-yl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-(3-methylthiophene-2-yl)malonic acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-(5-methylthiophene-2-yl)malonic acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-thiazol-2-elmaloglou acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-isopropylmalonic acid,

diethyl ether 2-terbutyl-2-(2-{3-dimethylcarbamoyl-4-[(4-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-isobutylamino acid,

dieti the new ester 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-propylmalonic acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-ethylmalonic acid,

diethyl ester of 2-butyl-2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diethyl ether 2-allyl-2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

ethyl ester of 3-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxy)-2,2-bis-ethoxycarbonylpyrimidine acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-(1-methylbutyl)malonic acid,

diethyl ether 2-(2-{3-ethoxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-hydroxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-methoxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ether 2-(2-{3-methoxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

2-phenyl-2,2-bis-propellerblades-ethyl ester {3-methoxy-4-[(4'-triptorelin-2-Carboni is)amino]phenyl}acetic acid,

3,3-bis-ethylcarbazole-3-phenylpropionyl ether {3-methoxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-ethoxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

3,3-bis-ethylcarbazole-3-phenylpropionyl ether {3-ethoxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ether 2-(2-{3-isopropoxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-isopropoxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

3,3-bis-ethylcarbazole-3-phenylpropionyl ether {3-isopropoxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-propoxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-benzyloxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ether 2-(2-{3-benzyloxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-hydroxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-{2-[3-methoxy-4-(4'-triptorelin-2-carbonyloxy)phenyl]acetoxymethyl}-2-phenylmalonate acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-dimethylamino-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-piperidine-1-yl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-pyrrolidin-1-yl-4 -[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ester of 2-phenyl-2-(2-{3-piperidine-1-yl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diethyl ester of 2-phenyl-2-(2-{3-pyrrolidin-1-yl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diethyl ether 2-(2-{3-dimethylamino-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-morpholine-4-yl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-diethylamino-4-[(4'-triptorelin-2-carbonyl) amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-[2-(2-{2-methyl-3-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxy)ethyl]-2-phenylmalonate acid,

diethyl ester of 2-phenyl-2-(2-{3-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid

diethyl ester of 2-phenyl-2-[2-(2-{3-[(4'-triptorelin-2-carbonyl) amino] phenyl} acetoxy) ethyl] malonic acid,

3,3-bis-ethylcarbazole-3-phenylpropionyl ether {3-[(4'-triptorelin-2-carbonyl) amino]phenyl}acetic acid,

3-phenyl-3,3-bis-propellerblades-propyl ether {3-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ether 2-[2-(2-{4-methyl-3-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxy)ethyl]-2-phenylmalonate acid,

diethyl ether 2-[2-(2-{2-methyl-5-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxy)ethyl]-2-phenylmalonate acid,

3,3-bis-isopropylcarbamate-3-phenylpropionyl ether {3-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

3,3-bis-ethylcarbazole-3-phenylpropionyl ether {2-metil-3-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

4,4-bis-ethylcarbamate-4-privately ether {2-methyl-3-[(4'-triptorelin-2-carbonyl)amino]phenyl)acetic acid,

3-phenyl-3,3-bis-propellerblades-propyl ether {2-methyl-3-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

3,3-bis-ethylcarbazole-3-phenylpropionyl ether {2-methoxy-3-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ether 2-[2-(2-{2-methoxy-3-[(4'-triform tilbehor-2-carbonyl)amino]phenyl}acetoxy)ethyl]-2-phenylmalonate acid,

3,3-bis-ethylcarbazole-3-phenylpropionyl ether {2-ethoxy-3-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ether 2-[2-(2-{2-ethoxy-3-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxy)ethyl]-2-phenylmalonate acid,

diethyl ether 2-[2-(2-{2-isopropoxy-3-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxy)ethyl]-2-phenylmalonate acid,

diethyl ether 2-[2-(2-{2-methoxycarbonyl-3-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxy)ethyl]-2-phenylmalonate acid,

diethyl ether 2-[2-(2-{2-ethoxy-5-methyl-3-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxy)ethyl]-2-phenylmalonate acid,

2-[9-(2,2,2-Cryptor-ethylcarbamate)-9h-fluoren-9-yl]ethyl ester 4-[(4'-triptorelin-2-carbonyl)amino]benzoic acid,

2-(9h-fluoren-9-yl)ethyl ester 4-[(4'-triptorelin-2-carbonyl)amino]benzoic acid,

2-[9-(2,2,2-triptoreline)-9h-fluoren-9-yl]ethyl ester of n-biphenyl-2-literaturenobel acid,

2-[(biphenyl-2-carbonyl)amino]ethyl ester 4-[(4'-triptorelin-2-carbonyl)amino]benzoic acid,

2-(2-biphenyl-2-yl-acetylamino)ethyl ester 4-[(4'-triptorelin-2-carbonyl)amino]benzoic acid,

3-naphthalene-1-yl-3-(2,2,2-Cryptor-ethylcarbamate)propyl ether of 4-[(4'-trifloromethyl the Nile-2-carbonyl)amino]benzoic acid,

3-[2-(2,2,2-Cryptor-ethylcarbamate)naphthalene-1-yl]propyl ester 4-[(4'-triptorelin-2-carbonyl)amino]benzoic acid,

3,3-diphenyl-3-(2,2,2-Cryptor-ethylcarbamate)propyl ether of 4-[(4'-triptorelin-2-carbonyl)amino]benzoic acid,

3-biphenyl-2-yl-3-(2,2,2-triptoreline)propyl ether of 4-[(4'-triptorelin-2-carbonyl)amino]benzoic acid,

3-phenyl-3-(2,2,2-triptoreline)propyl ether of 4-[(4'-triptorelin-2-carbonyl)amino]benzoic acid,

2-[8-(2,2,2-triptoreline)naphthalene-1-yl]ethyl ester 4-[(4'-triptorelin-2-carbonyl)amino]benzoic acid,

3-(2,6-dichlorophenyl)-3-(2,2,2-triptoreline)propyl ether of 4-[(4'-triptorelin-2-carbonyl)amino]benzoic acid,

3-(2-chlorophenyl)-3-(2,2,2-triptoreline)propyl ether of 4-[(4'-triptorelin-2-carbonyl)amino]benzoic acid,

diethyl ester of 2-phenyl-2-(2-{4-[(4'-triptorelin-2-carbonyl)amino]benzoyloxy}ethyl) - malonic acid,

diethyl ether 2-(2-{3-methyl-4-[(4'-triptorelin-2-carbonyl)amino]benzoyloxy}ethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{2-chloro-4-[(4'-triptorelin-2-carbonyl)amino]benzoyloxy}ethyl)-2-phenylmalonate acid,

diethyl ester of 2-phenyl-2-{2-[4-(4'-triptorelin-carbonyloxy)benzoyloxy]ethyl}malonic acid,

diethyl ether 2-{2-[4-(2-benzoyl-benzoyloxy)benzoyloxy]ethyl}-2-phenylmalonate acid,

3,3-bis-ethylcarbazole-3-phenylpropionic ester 4-[(4'-triptorelin-2-carbonyl)amino]benzoic acid,

4-(3,3-bis-ethylcarbazole-3-phenylpropionyl)-2-hlorfenilovy ether 4'-triptorelin-2-carboxylic acid,

4-(3,3-bis-ethylcarbazole-3-phenyl-propoxycarbonyl)phenyl ether 4'-triptorelin-2-carboxylic acid,

4-(3,3-bis-ethylcarbazole-3-phenylpropionyl)-2,6-dichlorphenoxy ether 4'-triptorelin-2-carboxylic acid,

2-[9-(2,2,2-triptoreline)-9h-fluoren-9-yl]ethyl ester 4-methyl-4-[(4'-triptorelin-2-carbonyl)amino]cyclohexanecarboxylic acid,

2-[9-(2,2,2-Cryptor-ethylcarbamate)-9h-fluoren-9-yl]ethyl ester 4-[(4'-triptorelin-2-carbonyl)amino]cyclohexanecarboxylic acid,

3-phenyl-3-(2,2,2-triptoreline)propyl ether of 4-[(4'-triptorelin-2-carbonyl)amino]cyclohexanecarboxylic acid,

diethyl ester of 2-phenyl-2-{4-[(4'-triptorelin-2-carbonyl)amino]cyclohexanecarboxylate}malonic acid,

diethyl ester of 2-phenyl-2-(2-{4-[(4'-triptorelin-2-carbonyl)amino]cyclohexanecarboxylate)ethyl) - malonic acid,

diethyl ester of 2-phenyl-2-(2-{4-[(4'-cryptomite is biphenyl-2-carbonyl)amino]piperidine-1-yl}acetoxymethyl)malonic acid,

diethyl ester of 2-phenyl-2-(2-{4-[(4'-triptorelin-2-carbonyl)amino]indol-1-yl}acetoxymethyl)malonic acid,

diethyl ether 2-(2-{2-methyl-4-[(4'-triptorelin-2-carbonyl)amino]benzimidazole-1-yl}acetoxymethyl)-2-phenylmalonate acid,

2,2-bis-ethylcarboxyl-2-phenethyl ester [2-oxo-3-(4'-triptorelin-2-carbonyl)-2,3-dihydro-benzoxazol-6-yl]acetic acid,

diethyl ether 2-(2-{3-etoxycarbonyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(3-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}propionyloxy)-2-phenylmalonate acid,

2,2-bis-ethylcarboxyl-2-phenethyl ester 4-{[(4'-triptorelin-2-carbonyl)amino]methyl}benzoic acid,

ethylcarbodiimide ester 3-{4-[(4'-triptorelin-2-carbonyl)amino]phenyl}propionic acid,

benzyl ether of 5-(2,2-bis-ethylcarboxyl-2-phenyl-ethoxycarbonylmethyl)-2-[(4'-triptorelin-2-carbonyl)amino]benzoic acid,

5-(2,2-bis-ethylcarboxyl-2-phenyl-ethoxycarbonylmethyl)-2-[(4'-triptorelin-2-carbonyl)amino]benzoic acid,

ethyl ester of 5-(2,2-bis-ethylcarboxyl-2-phenyl-ethoxycarbonylmethyl)-2-[(4'-triptorelin-2-carbonyl)amino]benzoic acid,

diethyl ester of 2-phenyl-2-(2-{4-[(4'-triptorelin-2-carbonyl)amino]benzoimidazol-1-yl}acetoxymethyl)malonic acid,

3-{[(4'-triptorelin-2-carbonyl)amino]methyl}benzoic acid 3,3-bis-ethylcarbazole-3-phenylpropionyl ether acid,

methyl ester 5-(2,2-bis-ethylcarboxyl-2-phenyl-ethoxycarbonylmethyl)-2-[(4'-triptorelin-2-carbonyl)amino]benzoic acid,

diethyl ether 2-(2-{3-benzyloxycarbonyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-carboxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-{2-[2-oxo-3-(4'-triptorelin-2-carbonyl)-2,3-dihydroisoxazole-6-yl]acetoxymethyl}-2-phenylmalonate acid,

diethyl ether 2-{2-[8-oxo-7-(4'-triptorelin-2-carbonyl)-7-azabicyclo[4.2.0]OCTA-1(6),2,4-triene-3-yl]acetoxymethyl}-2-phenylmalonate acid,

diethyl ether 2-(2-{3-isopropoxycarbonyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-methoxycarbonyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-[2-(3-dimethylcarbamoyl-4-{[1-(2-nitrol-4-trifluoromethyl-phenyl)pyrrolidin-2-CT is of IMT]amino}phenyl)acetoxymethyl]-2-phenylmalonate acid,

diethyl ether 2-(2-{3-acetylamino-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-methoxycarbonylamino-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonic acid,

diethyl ether 2-(2-{3-(4-methyl-thiazol-2-yl)-4-((4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ester of 2-phenyl-2-(2-{6-[(4'-triptorelin-2-carbonyl)amino]biphenyl-3-yl}acetoxymethyl)malonic acid,

diethyl ether 2-(2-{3-formyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylaminomethyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-(methoxymethylethoxy)-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-isobutyryl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid, and

diethyl ether 2-(2-{3-(1-hydroxy-2-methylpropyl)-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid.

27. Ester compound or its pharmaceutically acceptable salt according to claim 1, which is ybiraut from the group including

2,2-bis-ethylcarboxyl-2-phenethyl ester 4-[(4'-triptorelin-2-carbonyl)amino]phenyl} acetic acid,

diethyl ester of 2-phenyl-2-{2-[4-[(4'-triptorelin-2-carbonyloxy)phenyl]acetoxymethyl}malonic acid,

diethyl ether 2-(2-{3-methyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{4-[methyl-(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-ethyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

9-(2,2,2-triptoreline)-9h-fluoren-9-ymetray ether (4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

9-(2,2,2-triptoreline)-9h-fluoren-9-ymetray ester {4-[(4'-triptorelin-2-carbonyl)amino]phenyl}propionic acid,

2-phenyl-2-(2,2,2-triptoreline)ethyl ester {4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ester of 2-phenyl-2-(2-{4-[4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diisopropyl ether 2-phenyl-2-(2-{4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

2-phenyl-2,2-bis-(2,2,2-triptoreline)ethyl the new ester {4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

dimethyl 2-phenyl-2-(2-{4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diethyl ether 2-cyclopentyl-2-(2-{4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

dicyclohexylamine ester 2-phenyl-2-(2-{4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

2,2-bis-cyclohexylcarbonyl-2-phenethyl ester {4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2-phenyl-2,2-bis-phenylcarbamoyl-ethyl ester {4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-isopropylcarbamate-2-phenethyl ester {4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ether 2-benzyl-2-(2-{4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxylation acid,

diethyl ether 2-(2-{2-methyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl-2-phenylmalonate acid,

4-[2-phenyl-2,2-bis-(2,2,2-triptoreline)ethoxycarbonylmethyl]phenyl ester of 4'-triptorelin-2-carboxylic acid,

4-[2-phenyl-2,2-bis-(2,2,2-triptoreline)ethoxycarbonylmethyl]phenyl ether-biphenyl-2-carboxylic acid,

diethyl ether of 2-cyclohexyl-2-(2-{4-[(4'-triptorelin-2-carbonyl)is Mino]phenyl}acetoxymethyl)malonic acid,

2-phenyl-2,2-bis-(2,2,2-triptoreline)ethyl ester {4-[(biphenyl-2-carbonyl)amino]phenyl}acetic acid,

diethyl ester of 2-phenyl-2-(2-{2-trifluoromethyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

2,2-bis-methylcarbamoyl-2-phenethyl ester {4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ether 2-pyridin-2-yl-2-(2-{4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxylation acid,

diethyl ether 2-pyridin-3-yl-2-(2-{4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

4-(2,2-bis-ethylcarboxyl-2-phenyl-ethoxycarbonylmethyl)phenyl ether 4'-triptorelin-2-carboxylic acid,

diethyl ester of 2-phenyl-2-(2-{3-trifluoromethyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

2,2-bis-butylcarbamoyl-2-phenethyl ester {4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-methyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ether 2-(2-{4-[(4'-methylbiphenyl-2-carbonyl}-amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{4-[(4'-methoxybiphenyl-2-carbonyl}amino]phenyl}acetoxymethyl)2-phenylmalonate acid,

3,3-bis-ethylcarbazole-3-phenylpropionic ester {4-[(4'-triptorelin-2-carbonyl}amino]phenyl}acetic acid,

3-phenyl-3,3-bis-propyltetrahydropyran ester {4-[(4'-triptorelin-2-carbonyl}amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ester {4-[(biphenyl-2-carbonyl)amino]phenyl}acetic acid,

diethyl ester of 2-phenyl-2-(2-{4-[(3'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

4-(2,2-bis-ethylcarboxyl-2-phenyl-ethoxycarbonylmethyl)-2-hlorfenilovy ether 4'-triptorelin-2-carboxylic acid,

diethyl ether 2-(2-{4-[isopropyl-(4'-triptorelin-2-carbonyl}amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{4-[cyclohexyl-(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

dipropionyl ester 2-phenyl-2-(2-{4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diisobutylamine ester 2-phenyl-2-(2-{4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

2,2-bis-isobutylamino-2-phenethyl ester {4-[(4'-triptorelin-2-carbonyl}amino]phenyl}acetic acid,

2,2-bis(3-methyl-butylcarbamoyl)-2-phenethyl ester {4-[(4'-triptorelin-2-Carboni is}amino]phenyl}acetic acid,

diethyl ether 2-(2-{4-[ethyl-(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

2,2-bis(ethylcarbamate-2-phenyl)ethyl ester {4-[(4'-chlorobiphenyl-2-carbonyl)amino]phenyl}acetic acid,

{2,2-bis(ethylcarbamate-2-phenethyl ester 4-[(3',4'-dichlorobiphenyl-2-carbonyl)amino]phenyl}acetic acid,

2-phenyl-2,2-bis-propellerblades-ethyl ester {3-methyl-4-[(4'-triptorelin-2-carbonyl}amino]phenyl}acetic acid,

2,2-bis-(2-methoxy-ethylcarbamate)-2-phenethyl ester 4-[(4'-triptorelin-2-carbonyl}amino]phenyl}acetic acid,

diethyl ether 2-(2-{3-ethyl-4-[(4'-triptorelin-2-carbonyl}amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-isopropyl-4-[(4'-triptorelin-2-carbonyl}amino]phenyl}acetic acid,

diethyl ether 2-(2-{3-isopropyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

3,3-bis-ethylcarbazole-3-phenylpropionyl ether {3-ethyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-isobutyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl)acetic acid,

diethyl ether 2-(2-{3-isobutyl-4-[(4'-triptorelin-2-Carbo who yl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-chloro-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-bromo-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

2-phenyl-2,2-bis-propellerblades-ethyl ester {3-dimethylcarbamoyl-4-[{4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-methylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

3,3-bis-ethylcarbazole-3-phenethyl ether {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ether 2-(2-{3-diethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-benzylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

4,4'-bis-ethylcarbamate-4-privately ether {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-diethylcarbamoyl-4-[(4'-triptorelin-2-Carbo who yl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-diisopropylamino-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ether 2-(2-{3-diethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-diisopropylamino-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-(isopropylaminocarbonyl)-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ether 2-(2-{3-(ethylmethylamino)-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-(ethylmethylamino)-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

3,3-bis-ethylcarbazole-3-phenylpropionyl ether {3-(ethylmethylamino)-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-(piperidine-1-carbonyl)-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-(pyrrolidin-1-carbonyl)-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-femilet levy ether {3-(methylpropanoyl)-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

3,3-bis-ethylcarbazole-3-phenethyl ether {3-(methylpropanoyl)-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2-ethyl-carbarnoyl-2-phenethyl ether {3-(dimethylcarbamoyl)-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ester of 2-phenyl-2-(2-{3-(pyrrolidin-1-carbonyl)-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diethyl ester of 2-phenyl-2-(2-{3-(piperidine-1-carbonyl)-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

2-phenyl-2-propionamido-ethyl ester {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2-phenyl-2-propionamido-ethyl ester {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2-(2,5-dioxopiperidin-1-yl)-2-phenethyl ether {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2-ethylcarbamate-benzyl ether {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2-ethylcarboxylate-benzyl ether {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

hydrochloride of 2-isopropylamino-2-phenethyl ester {3-dimethylcarbamoyl the-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ether 2-[2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxy)ethyl]-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-forbiden-2-carbonyl}amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{4-[(4'-bromo-biphenyl-2-carbonyl)amino]-3-dimethylcarbamoyl}acetoxymethyl)-2-phenylmalonate acid,

2-acetylamino-2-phenethyl ether {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2 Butylimino-2-phenethyl ether {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

dimethyl 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-cyclopentyl-2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diethyl ether of 2-cyclohexyl-2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-malonic acid,

diethyl ether 2-(2-{4-[(4'-chlorobiphenyl-2-carbonyl)amino]-3-dimethylcarbamoyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{4-[(4'-acetyl-biphenyl-2-carbonyl)amino]-3-dimethylcarbamoyl}acetic imethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{4-[(4'-cyano-biphenyl-2-carbonyl)amino]-3-dimethylcarbamoyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4-methyl-4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(5-methyl-4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

2 methanesulfonamido-2-phenethyl ether {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

ethyl ester of 3-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxy)-2-phenylpropionic acid,

2-(methylpropionamide)-2-phenethyl ether {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ether 2-[3-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxy)propyl]-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(5-methoxy-4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl]-2-phenylmalonate acid,

diethyl ether 2-(2-{4-[5-chloro-4'-triptorelin-2-carbonyl)amino]-3-dimethylcarbamoyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[6-methyl-4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

di-2,2,2-triptoreline ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(2'-fluoro-4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{5-dimethylcarbamoyl-2-fluoro-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-bromo-5-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-chloro-5-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(3'-fluoro-4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{4-(3'-chloro-4'-triptorelin-2-carbonyl)amino]-3-dimethylcarbamoyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-(5-nitro-pyridin-2-yl)malonic acid,

diethyl ether 2-(5-amino-pyridin-2-yl)-2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic sour is s,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-pyridin-2-elmaloglou acid,

diethyl ether 2-(2-{3-chloro-5-dimethylcarbamoyl-2-fluoro-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-bromo-5-dimethylcarbamoyl-2-fluoro-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-o-talismanova acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-m-talismanova acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-p-talismanova acid,

diethyl ether 2-(2-chlorophenyl)-2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diethyl ether 2-(3-chlorophenyl)-2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diethyl ether 2-(4-chlorophenyl)-2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

Dyatlov the th ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylethanol acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-(2-methoxyphenyl)malonic acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-(3-methoxyphenyl)malonic acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-(4-methoxyphenyl)malonic acid,

diethyl ether 2-(2-{4-(5,4'-bis-triptorelin-2-carbonyl)amino]-3-dimethylcarbamoyl}acetoxymethyl)-2-phenyl}malonic acid,

diethyl ether 2-(2-{4-(6-chloro-4'-triptorelin-2-carbonyl)amino]-3-dimethylcarbamoyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(6-fluoro-4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-[2-(2-{3-dimethylcarbamoyl-4-[(5-methyl-4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(5-ethoxy-4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(5-isopropoxy-4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate sour is s,

diethyl ether 2-[2-(2-{4-[(5,4'-bis-4'-triptorelin-carbonyl)amino]-3-dimethylcarbamoyl}acetoxy)ethyl]-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(6-methoxy-4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(3-methyl-4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-{2-[4-(2,4-bis-trifluoromethyl-benzoylamine)-3-dimethylcarbamoyl]acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-methylbiphenyl-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-{2-[3-dimethylcarbamoyl-4-(2-ethyl-4-trifluoromethyl-benzoylamine)phenyl]acetoxymethyl}-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-ethylbiphenyl-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-isopropyl-biphenyl-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-isopropyl-biphenyl-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-{2-[3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbon is Loxy)phenyl]acetoxymethyl)-2-phenylmalonate acid,

2-ethyl-2-privately ether {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

1-phenyl-cyclopropylmethyl ether {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-definiately ether {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl)acetic acid,

1-phenyl-cyclopentylmethyl ether {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

3-hydroxy-2-hydroxymethyl-2-phenylpropionyl ether {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

3-acetoxy-2-acetoxymethyl-2-phenylpropionyl ether {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-thiophene-2-elmaloglou acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-thiophene-3-elmaloglou acid,

diethyl ether 2-(2-{4-dimethylcarbamoyl-5-[(4'-triptorelin-2-carbonyl)amino]pyridin-2-yl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]enyl)acetoxymethyl)-2-(3-methylthiophene-2-yl)malonic acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-(5-methylthiophene-2-yl)malonic acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-thiazol-2-elmaloglou acid,

diethyl ether 2-(2-{3-ethoxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-hydroxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-methoxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ether 2-(2-{3-methoxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

2-phenyl-2,2-bis-propellerblades-ethyl ester {3-methoxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

3,3-bis-ethylcarbazole-3-phenylpropionyl ether {3-methoxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl)acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-ethoxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

3,3-bis-ethylcarbazole-3-phenylpropionyl ether {3-ethoxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid is you,

diethyl ether 2-(2-{3-isopropoxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-isopropoxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

3,3-bis-ethylcarbazole-3-phenylpropionyl ether {3-isopropoxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-propoxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-benzyloxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ether 2-(2-{3-benzyloxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-hydroxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-{2-[3-methoxy-4-[(4'-triptorelin-2-carbonyloxy)phenyl]acetoxymethyl}-2-phenylmalonate acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-dimethylamino-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-piperidine-1-yl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-pyrrolidin-1-yl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ester of 2-phenyl-2-(2-{3-piperidine-1-yl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diethyl ester of 2-phenyl-2-(2-{3-pyrrolidin-1-yl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diethyl ether 2-(2-{3-dimethylamino-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether (2-{3-morpholine-4-yl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-diethylamino-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-[2-(2-{2-methyl-3-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxy)ethyl]-2-phenylmalonate acid,

diethyl ester of 2-phenyl-2-(2-{3-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diethyl ester of 2-phenyl-2-[2-(2-{3-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxy)ethyl]malonic acid,

3,3-bis-ethylcarbazole-3-phenylpropionyl ether {3-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-Hairdryer is letilly ether {3-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

3-phenyl-3,3-bis-propellerblades-propyl ether {3-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ether 2-[2-(2-{4-methyl-3-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxyethyl)-2-phenylmalonate acid,

diethyl ether 2-[2-(2-{2-methyl-5-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxy)ethyl]-2-phenylmalonate acid,

3,3-bis-isopropylcarbamate-3-phenylpropionyl ether {3-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

3,3-bis-ethylcarbazole-3-phenylpropionyl ether {2-methyl-3-[(4'-triptorelin-2-carbonyl)amino]phenyl)acetic acid,

4,4-bis-ethylcarbamate-4-privately ether {2-methyl-3-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

3-phenyl-3,3-bis-propellerblades-propyl ether (2-methyl-3-[(4'-triptorelin-2-carbonyl)amino]phenyl} acetic acid,

3,3-bis-ethylcarbazole-3-phenylpropionyl ether {2-methoxy-3-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ether 2-[2-(2-{2-methoxy-3-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxy)ethyl]-2-phenylmalonate acid,

3,3-bis-ethylcarbazole-3-phenylpropionyl ether {2-ethoxy-3-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ether 2-[2-(2-{2-ethoxy-3[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxy)ethyl]-2-phenylmalonate acid,

diethyl ether 2-[2-(2-{2-isopropoxy-3-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxy)ethyl]-2-phenylmalonate acid,

diethyl ether 2-[2-(2-{2-methoxycarbonyl-3-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxy)ethyl]-2-phenylmalonate acid,

diethyl ether 2-[2-(2-{2-ethoxy-5-methyl-3-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxy)ethyl]-2-phenylmalonate acid,

2-[9-(2,2,2-triptoreline)-9h-fluoren-9-yl]ethyl ester 4-[(4'-triptorelin-2-carbonyl)amino]benzoic acid,

2-[9h-fluoren-9-yl]ethyl ester 4-[(4'-triptorelin-2-carbonyl)amino]benzoic acid,

2-[9-(2,2,2-triptoreline)-9h-fluoren-9-yl]ethyl ester of N-biphenyl-2-literaturenobel acid,

2-[(biphenyl-2-carbonyl)amino]ethyl ester 4-[(4'-triptorelin-2-carbonyl)amino]benzoic acid,

2-(2-biphenyl-2-yl-acetylamino)ethyl ester 4-[(4'-triptorelin-2-carbonyl)amino]benzoic acid,

3-naphthalene-1-yl-3-(2,2,2-triptoreline)propyl ether of 4-[(4'-triptorelin-2-carbonyl)amino]benzoic acid,

3-[2-(2,2,2-triptoreline)naphthalene-1-yl]propyl ester 4-[(4'-triptorelin-2-carbonyl)amino]benzoic acid,

3,3-diphenyl-3-(2,2,2-triptoreline)propyl ether of 4-[(4'-triptorelin the-2-carbonyl) amino] benzoic acid,

3-biphenyl-2-yl-3-(2,2,2-triptoreline) propyl ether of 4-[(4'-triptorelin-2-carbonyl)amino]benzoic acid,

3-phenyl-3-(2,2,2-triptoreline)propyl ether of 4-[(4'-triptorelin-2-carbonyl)amino]benzoic acid,

2-[8-(2,2,2-triptoreline)naphthalene-1-yl]ethyl ester 4-[(4'-triptorelin-2-carbonyl)amino]benzoic acid,

3-[(2,6-dichlorophenyl)-3-(2,2,2-triptoreline)propyl ether of 4-[(4'-triptorelin-2-carbonyl)amino]benzoic acid,

3-(2-chlorophenyl)-3-(2,2,2-triptoreline)propyl ether of 4-[(4'-triptorelin-2-carbonyl)amino]benzoic acid,

diethyl ester of 2-phenyl-2-(2-{4-[(4'-triptorelin-2-carbonyl)amino]benzoyloxy}ethyl) - malonic acid,

diethyl ether 2-(2-{3-methyl-4-[(4'-triptorelin-2-carbonyl)amino]benzoyloxy}ethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{2-chloro-4-[(4'-triptorelin-2-carbonyl)amino]benzoyloxy}ethyl)-2-phenylmalonate acid,

diethyl ester of 2-phenyl-2-{2-[4-[(4'-triptorelin-2-carbonyloxy)benzoyloxy]ethyl}malonic acid,

3,3-bis-ethylcarbazole-3-phenylpropionic ester 4-[(4'-triptorelin-2-carbonyl)amino]benzoic acid,

4-(3,3-bis-ethylcarbazole-3-phenyl-propoxycarbonyl)-2-hlorfenilovy ether 4'-crypto methylbiphenyl-2-carboxylic acid,

4-(3,3-bis-ethylcarbazole-3-phenyl-propoxycarbonyl)phenyl ether 4'-triptorelin-2-carboxylic acid,

4-(3,3-bis-ethylcarbazole-3-phenyl-propoxycarbonyl)-2,6-dichlorphenoxy ether 4'-triptorelin-2-carboxylic acid,

2-(2-{3-etoxycarbonyl-4-[(4'-triptorelin-2-carbonyl)amino]phenylacetonitrile)-2-phenylmalonate acid,

diethyl ether 2-(3-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}propionyloxy)-2-phenylmalonate acid,

ethylcarbamate-methyl ester 2-{4-[(4'-triptorelin-2-carbonyl)amino]phenyl}propionic acid,

benzyl ether of 5-(2,2-bis-ethylcarboxyl-2-phenyl-ethoxycarbonylmethyl)-2-4-[(4'-triptorelin-2-carbonyl)amino]benzoic acid,

5-(2,2-bis-ethylcarboxyl-2-phenyl-ethoxycarbonylmethyl)-2-[(4'-triptorelin-2-carbonyl)amino]benzoic acid,

ethyl ester of 5-(2,2-bis-ethylcarboxyl-2-phenyl-ethoxycarbonylmethyl)-2-[(4'-triptorelin-2-carbonyl)amino]benzoic acid,

methyl ester 5-(2,2-bis-ethylcarboxyl-2-phenyl-ethoxycarbonylmethyl)-2-[(4'-triptorelin-2-carbonyl)amino]benzoic acid,

diethyl ether 2-(2-{3-benzyloxycarbonyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl}-2-phenylmalonate acid,

IER is silt ether 2-(2-{3-carboxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-isopropoxycarbonyl-4-[(4'-triptorelin-2-carbonyl) amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-methoxycarbonyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-acetylamino-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-methoxycarbonylamino-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-(4-methylthiazole-2-yl)-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ester of 2-phenyl-2-(2-{6-[(4'-triptorelin-2-carbonyl)amino]biphenyl-3-yl}acetoxymethyl)malonic acid,

diethyl ether 2-(2-{3-formyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylaminomethyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}-3-acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-methoxy-methylcarbamoyl)-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}-3-acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-isobutyryl-4-[(4'-triptorelin-2-carbonyl)amino]enyl}-3-acetoxymethyl)-2-phenylmalonate acid and

diethyl ether 2-(2-{3-(1-hydroxy-2-methylpropyl)-4-[(4'-triptorelin-2-carbonyl) amino] phenyl }acetoxymethyl)-2-phenylmalonate acid.

28. Ester compound or its pharmaceutically acceptable salt according to claim 1, which is selected from the group including

2,2-bis(ethylcarbamate)-2-phenethyl ester {4-['4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ester of 2-phenyl-2-{2-[4-[(4'-triptorelin-2-carbonyloxy)phenyl]acetoxymethyl}malonic acid,

diethyl ether 2-(2-{3-methyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl)acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-(4-[methyl-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

2,2-bis-etilcaprilatului ether {3-ethyl-4-[(4'-triptorelin-2-carbonyl)amino]-2-phenyl]acetic acid,

diethyl ester of 2-phenyl-2-(2-{4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diisopropyl ether 2-phenyl-2-(2-{4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

2-phenyl-2,2-bis-(2,2,2-triptoreline)ethyl ester {4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

dimethyl 2-phenyl-2-(2-{4-[(4'-triptorelin-2-arbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diethyl ether 2-cyclopentyl-2-(2-{4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

dicyclohexylamine ester 2-phenyl-2-(2-{4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

2,2-bis-cyclohexylcarbonyl-2-phenethyl ester {4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2-phenyl-2,2-bis-phenylcarbamoyl-ethyl ester {4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-isopropylcarbamate-2-phenethyl ester {4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ether 2-benzyl-2-(2-{4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diethyl ether 2-(2-{2-methyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

4-[2-phenyl-2,2-bis-(2,2,2-triptoreline)ethoxycarbonylmethyl]phenyl ester of 4'-triptorelin-2-carboxylic acid,

4-[2-phenyl-2,2-bis-(2,2,2-triptoreline)ethoxycarbonylmethyl]phenyl ether-biphenyl-2-carboxylic acid,

diethyl ether of 2-cyclohexyl-2-(2-{4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

2-phenyl-2,2-bis-(2,2,2-triptoreline)ethyl ester {4-[(bifen the l-2-carbonyl)amino]phenyl}acetic acid,

diethyl ester of 2-phenyl-2-(2-{2-trifluoromethyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

2,2-bis-methylcarbamoyl-2-phenethyl ester {4-[(4'-triptorelin-2-carbonyl)amino]phenyl} acetic acid,

diethyl ether 2-pyridin-2-yl-2-(2-{4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diethyl ether 2-pyridin-3-yl-2-(2-{4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

4-(2,2-bis-ethylcarbamate)-2-phenyl-ethoxycarbonylmethyl)phenyl ether 4'-triptorelin-2-carboxylic acid,

diethyl ester of 2-phenyl-2-(2-{3-trifluoromethyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

2,2-bis-butylcarbamoyl-2-phenethyl ester {4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-methyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ether 2-(2-{4-[(4'-methylbiphenyl-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{4-[(4'-methoxybiphenyl-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

3,3-bis-ethylcarbazole-3-phenylpropionic ester {4-[(4'-triptorelin-2-carbon is l)amino]phenyl}acetic acid,

3-phenyl-3,3-bis-propellerblades-propyl ether (4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ester {4-[(biphenyl-2-carbonyl)amino]phenyl}acetic acid,

diethyl ester of 2-phenyl-2-(2-{4-[(3'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

4-(2,2-bis-ethylcarbamate)-2-phenyl-ethoxycarbonylmethyl)-2-hlorfenilovy ether 4'-triptorelin-2-carboxylic acid,

diethyl ether 2-(2-{4-[isopropyl-(4'-cryptometrics-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{4-[cyclohexyl-(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

dipropionyl ester 2-phenyl-2-(2-{4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diisobutylamine ester 2-phenyl-2-(2-{4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

2,2-bis-isobutylamino-2-phenethyl ester {4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-(3-methyl-butylcarbamoyl)-2-phenethyl ester {4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ether 2-(2-{4-[ethyl-(4'-triptorelin-2-carbonyl)amino]phenyl}ACET kemetyl)-2-phenylmalonate acid,

2,2-bis-ethylcarboxyl-2-phenethyl ester {4-[(4'-chlorobiphenyl-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ester {4-[(3',4'-dichlorobiphenyl-2-carbonyl)amino]phenyl}acetic acid,

2-phenyl-2,2-bis-propellerblades-ethyl ester {3-methyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-(2-methoxy-ethylcarbamate)-2-phenethyl ester {4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ether 2-(2-{3-ethyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-isopropyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ether 2-(2-{3-isopropyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

3,3-bis-ethylcarbazole-3-phenylpropionyl ether {3-ethyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-isobutyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ether 2-(2-{3-isobutyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-chloro-4-[(4'-triptorelin-2-carb the Nile)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-bromo-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

2-phenyl-2,2-bis-propellerblades-ethyl ester {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-methylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

3,3-bis-ethylcarbazole-3-phenylpropionyl ether {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ether 2-(2-{3-diethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-benzylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

4,4-bis-ethylcarbamate-4-privately ether {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-diethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-diisopropylamino-4-[(4'-triptime iluvenis-2-carbonyl)amino]phenyl}acetic acid,

diethyl ether 2-(2-{3-diethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-diisopropylamino-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-(isopropylaminocarbonyl)-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ether 2-(2-{3-(ethylmethylamino)-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-(ethylmethylamino)-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

3,3-bis-ethylcarbazole-3-phenylpropionyl ether {3-(ethylmethylamino)-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-(piperidine-1-carbonyl)-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-(pyrrolidin-1-carbonyl)-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-(methylpropanoyl)-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

3,3-bis-ethylcarbazole-3-penile opravy ether {3-(methylpropanoyl)-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2-ethylcarboxyl-2-phenethyl ether {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ester of 2-phenyl-2-(2-{3-pyrrolidin-1-carbonyl)-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl]malonic acid,

diethyl ester of 2-phenyl-2-(2-{3-piperidine-1-carbonyl)-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

2-phenyl-2-propionamido-ethyl ester {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2-(2,5-dioxo-pyrrolidin-1-yl)-2-phenethyl ether {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

ethylcarbitol-benzyl ether {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2-ethylcarboxylate-benzyl ether {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2 isopropylamino-2-phenethyl ester hydrochloride {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ether 2-[2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxy)ethyl]-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-fluoro-biphenyl-2-carbon is l)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{4-[(4'-bromo-biphenyl-2-carbonyl)amino]-3-dimethylcarbamoyl}acetoxymethyl)-2-phenylmalonate acid,

2-acetylamino-2-phenethyl ether {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2 Butylimino-2-phenethyl ether {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

dimethyl 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-cyclopentyl-2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diethyl ether of 2-cyclohexyl-2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diethyl ether 2-(2-{4-[(4'-chlorobiphenyl-2-carbonyl)amino]-3-dimethylcarbamoyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{4-[(4'-acetyl-biphenyl-2-carbonyl)amino]-3-dimethylcarbamoyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{4-[(4'-cyano-biphenyl-2-carbonyl)amino]-3-dimethylcarbamoyl)acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4-methyl-4'-triptorelin-2-carbonyl)amino]phenyl}is cacoxenite)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(5-methyl-4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

2 methanesulfonamido-2-phenethyl ether {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

ethyl ester of 3-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxy)-2-phenylpropionic acid,

2-(methylpropionamide)-2-phenethyl ether {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ether 2-[3-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxy)propyl]-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(5-methoxy-4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{4-[(5-chloro-4'-triptorelin-2-carbonyl)amino]-3-dimethylcarbamoyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(6-methyl-4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

di-2,2,2-triptoreline ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-metilcarbamat-4-[(2'-fluoro-4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{5-dimethylcarbamoyl-2-fluoro-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-bromo-5-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-chloro-5-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(3'-fluoro-4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{4-[(3'-chloro-4'-triptorelin-2-carbonyl)amino]-3-dimethylcarbamoyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-(5-nitro-pyridin-2-yl)malonic acid,

diethyl ether 2-(5-amino-pyridin-2-yl)-2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-pyridin-2-elmaloglou acid,

diethyl ether 2-(2-{3-chloro-5-dimethylcarbamoyl-2-fluoro-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-

2-venilale the OIC acid,

diethyl ether 2-(2-{3-bromo-5-dimethylcarbamoyl-2-fluoro-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-o-tolyl-malonic acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-m-tolyl-malonic acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-p-tolyl-malonic acid,

diethyl ether 2-(2-chlorophenyl)-2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diethyl ether 2-(3-chlorophenyl)-2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diethyl ether 2-(4-chlorophenyl)-2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylethanol acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-cryptometrics-2-carbonyl)amino]phenyl}acetoxymethyl)-2-(2-methoxyphenyl)malonic acid,

diethyl ether -(2-{3-dimethylcarbamoyl-4-[(4'-cryptometrics-2-carbonyl)amino]phenyl}acetoxymethyl)-2-(3-methoxyphenyl)malonic acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-(4-methoxyphenyl)malonic acid,

diethyl ether 2-(2-{4-[(5,4'-bis-triptorelin-2-carbonyl)amino]-3-dimethylcarbamoyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{4-[(6-chloro-4'-triptorelin-2-carbonyl)amino]-3-dimethylcarbamoyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(6-fluoro-4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-[2-(2-{3-dimethylcarbamoyl-4-[(5-methyl-4'-triptorelin-2-carbonyl)amino]phenyl}acetoxy)ethyl]-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(5-ethoxy-4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(5-isopropoxy-4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-[2-(2-(4-(5,4'-bis-triptorelin-2-carbonyl)amino]-3-dimethylcarbamoyl}acetoxy)ethyl]-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-(6-methoxy-4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

< num="3034"> diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(3-methyl-4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-{2-[4-(2,4-bis-trifluoromethyl-benzoylamine)-3-dimethylcarbamoyl]acetoxymethyl}-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-methylbiphenyl-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-{2-[3-dimethylcarbamoyl-4-[(2-ethyl-4-trifluoromethyl-benzoylamine)phenyl]acetoxymethyl}-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-ethyl-biphenyl-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-isopropyl-biphenyl-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-isopropyl-biphenyl-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-{2-[3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyloxy)phenyl]acetoxymethyl}-2-phenylmalonate acid,

2-ethyl-2-privately ether {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino] phenyl} acetic acid,

1-phenyl-cyclopropylmethyl ether {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}explicilty,

2,2-definiately ether {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

1-phenyl-cyclopentylmethyl ether {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

3-hydroxy-2-hydroxymethyl-2-phenylpropionyl ether {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

3-acetoxymethyl-2-phenylpropionyl ether {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl]-2-thiophene-2-elmaloglou acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl]-2-thiophene-3-elmaloglou acid,

diethyl ether 2-(2-{4-dimethylcarbamoyl-5-[(4'-triptorelin-2-carbonyl)amino]pyridin-2-yl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl]-2-(3-methyl-thiophene-2-yl)malonic acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl) amino] phenyl}acetoxymethyl)-2-(5-methyl-thiophene-2-yl)malonic acid,

diethyl ether 2-(2-{3-dimethylcarbamoyl-4-[(4 triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-thiazol-2-elmaloglou acid,

diethyl ether 2-(2-{3-ethoxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-hydroxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-methoxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ether 2-(2-{3-methoxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

2-phenyl-2,2-bis-propellerblades-ethyl ester {3-methoxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

3,3-bis-ethylcarbazole-3-phenylpropionyl ether {3-methoxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-ethoxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

3,3-bis-ethylcarbazole-3-phenylpropionyl ether {3-ethoxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ether 2-(2-{3-isopropoxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-isopropoxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

3,3-bis-Amilcar email-3-phenylpropionyl ether {3-isopropoxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-propoxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-benzyloxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ether 2-(2-{3-benzyloxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-hydroxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-{2-[3-methoxy-4-(4'-triptorelin-2-carbonyloxy)phenyl]acetoxymethyl}-2-phenylmalonate acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-dimethylamino-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-piperidine-1-yl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-pyrrolidin-1-yl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ester of 2-phenyl-2-(2-{3-piperidine-1-yl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diethyl ester of 2-phenyl-2-(2-{3-pyrrolidin-1-yl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid

diethyl ether 2-(2-{3-dimethylamino-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-morpholine-4-yl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-diethylamino-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-[2-(2-{2-methyl-3-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxy)ethyl]-2-phenylmalonate acid,

diethyl ester of 2-phenyl-2-(2-{3-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

diethyl ester of 2-phenyl-2-[2-(2-{3-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxy)ethyl]malonic acid,

3,3-bis-ethylcarbazole-3-phenylpropionyl ether {3-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

3-phenyl-3,3-bis-propellerblades-propyl ether {3-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ether 2-[2-(2-{4-methyl-3-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxy)ethyl]-2-phenylmalonate acid,

diethyl ether 2-[2-(2-{2-methyl-5-[(4'-triptorelin-2-carbonyl)amino]phenyl }acetoxy) ethyl]-2-phenylmalonate acid,

3,3-bis-isopropylcarbamate-3-phenylpropyl the th ether {3-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

3,3-bis-ethylcarbazole-3-phenylpropionyl ether (2-methyl-3-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

4,4-bis-ethylcarbamate-4-privately ether {2-methyl-3-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

3-phenyl-3,3-bis-propellerblades-propyl ether {2-methyl-3-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

3,3-bis-ethylcarbazole-3-phenylpropionyl ether {2-methoxy-3-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ether 2-[2-(2-{2-methoxy-3-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxy)ethyl]-2-phenylmalonate acid,

3, 3-bis-ethylcarbazole-3-phenylpropionyl ether {2-ethoxy-3-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

diethyl ether 2-[2-(2-{2-ethoxy-3-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxy)ethyl]-2-phenylmalonate acid,

diethyl ether 2-[2-(2-{2-isopropoxy-3-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxy)ethyl]-2-phenylmalonate acid,

diethyl ether 2-[2-(2-{2-methoxycarbonyl-3-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxy)ethyl]-2-phenylmalonate acid,

diethyl ether 2-[2-(2-{2-ethoxy-5-methyl-3-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxy)ethyl]-2-phenylmalonate acid,

2-[(biphenyl-2-carbonyl)amino]ethyl ester 4-[(4'-triptorelin-2-carbonyl)amino]benzoic acid,

2-(2-biphenyl-2-yl-acetylamino)ethyl ester 4-[(4'-triptorelin-2-carbonyl)amino]benzoic acid,

3-naphthalene-1-yl-3-(2,2,2-triptoreline)propyl ether of 4-[(4'-triptorelin-2-carbonyl)amino]benzoic acid,

3-[2-(2,2,2-triptoreline)naphthalene-1-yl]propyl ester 4-[(4'-triptorelin-2-carbonyl)amino]benzoic acid,

3,3-diphenyl-3-(2,2,2-triptoreline)propyl ether of 4-[(4'-triptorelin-2-carbonyl)amino]benzoic acid,

3-biphenyl-2-yl-3-(2,2,2-triptoreline)propyl ether of 4-[(4'-triptorelin-2-carbonyl)amino]benzoic acid,

3-phenyl-3-(2,2,2-triptoreline)propyl ether of 4-[(4'-triptorelin-2-carbonyl)amino]benzoic acid,

2-[8-(2,2,2-triptoreline)naphthalene-1-yl]ethyl ester 4-[(4'-triptorelin-2-carbonyl)amino]benzoic acid,

3-(2,6-dichlorophenyl)-3-(2,2,2-triptoreline)propyl ether of 4-[(4'-triptorelin-2-carbonyl)amino]benzoic acid,

3-(2-chlorophenyl)-3-(2,2,2-triptoreline)propyl ether of 4-[(4'-triptorelin-2-carbonyl)amino]benzoic acid,

diethyl ester of 2-phenyl-2-(2-{4-[(4'-triptorelin-2-carbonyl)AMI is about]benzoyloxy}ethyl) - malonic acid,

diethyl ether 2-(2-{3-methyl-4-[(4'-triptorelin-2-carbonyl)amino]benzoyloxy}ethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{2-chloro-4-[(4'-triptorelin-2-carbonyl)amino]-benzoyloxy}ethyl)-2-phenylmalonate acid,

diethyl ester of 2-phenyl-2-{2-[4-(4'-triptorelin-2-carbonyloxy)benzoyloxy]ethyl}malonic acid,

3,3-bis-ethylcarbazole-3-phenylpropionic ester 4-[(4'-triptorelin-2-carbonyl)amino]benzoic acid,

4-(3,3-bis-ethylcarbazole-3-phenyl-propoxycarbonyl)-2-hlorfenilovy ether 4'-triptorelin-2-carboxylic acid,

4-(3,3-bis-ethylcarbazole-3-phenylpropionyl)phenyl ether 4'-triptorelin-2-carboxylic acid,

4-(3,3-bis-ethylcarbazole-3-phenyl-propoxycarbonyl)-2,6-dichlorphenoxy ether 4'-triptorelin-2-carboxylic acid,

diethyl ether 2-(2-{3-etoxycarbonyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(3-{3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}propionyloxy)-2-phenylmalonate acid,

ethylcarbodiimide ester 3-{4-[(4'-triptorelin-2-carbonyl)amino]phenyl}propionic acid,

benzyl ether of 5-(2,2-bis-ethylcarboxyl-2-phenyl-ethoxycarbonylmethyl)-2--[(4'-triptorelin-2-carbonyl)amino]benzoic acid,

5-(2,2-bis-ethylcarboxyl-2-phenyl-ethoxycarbonylmethyl)-2-4-[(4'-triptorelin-2-carbonyl) amino] benzoic acid,

ethyl ester of 5-(2,2-bis-ethylcarboxyl-2-phenyl-ethoxycarbonylmethyl)-2-[(4'-triptorelin-2-carbonyl)amino]benzoic acid,

methyl ester 5-(2,2-bis-ethylcarboxyl-2-phenyl-ethoxycarbonylmethyl)-2-[(4'-triptorelin-2-carbonyl)amino]benzoic acid,

diethyl ether 2-(2-{3-benzyloxycarbonyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-carboxy-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-isopropoxycarbonyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-methoxycarbonyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-acetylamino-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-methoxycarbonylamino-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-(4-methyl-thiazol-2-yl)-4-[(4'-triptorelin-2-carbonyl)amino]f the Nile)acetoxymethyl)-2-phenylmalonate acid,

diethyl ester of 2-phenyl-(2-{6-[(4'-triptorelin-2-carbonyl)amino]-biphenyl-3-yl}acetoxymethyl)malonic acid,

diethyl ether 2-(2-{3-formyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-dimethylaminomethyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-(methoxymethylethoxy)-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid,

diethyl ether 2-(2-{3-isobutyryl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)-2-phenylmalonate acid and

diethyl ether 2-(2-{3-(1-hydroxy-2-methylpropyl)-4-[(4'-triptorelin-2-carbonyl)amino]phenyl)acetoxymethyl)-2-phenylmalonate acid.

29. Ester compound or its pharmaceutically acceptable salt according to claim 1, which is selected from the group including

2,2-bis-ethylcarboxyl-2-phenethyl ester {4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-ethyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2-phenyl-2,2-bis-(2,2,2-triptoreline)ethyl ester {4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

22 bis-cyclohexylcarbonyl-2-phenethyl ester {4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2-phenyl-2,2-bis-phenylcarbamoyl-ethyl ester {4-[(4'-triptorelin-2-carbonyl) amino]phenyl}acetic acid,

2,2-bis-isopropylcarbamate-2-phenethyl ester {4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

4-[2-phenyl-2,2-bis-(2,2,2-triptoreline)ethoxycarbonylmethyl]phenyl ester of 4'-triptorelin-2-carboxylic acid,

4-[2-phenyl-2,2-bis-(2,2,2-triptoreline)ethoxycarbonylmethyl]phenyl ether-biphenyl-2-carboxylic acid,

2-phenyl-2,2-bis-(2,2,2-triptoreline)ethyl ester {4-[(biphenyl-2-carbonyl)amino]phenyl}acetic acid,

diethyl ester of 2-phenyl-2-(2-{2-trifluoromethyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetoxymethyl)malonic acid,

2,2-bis-methylcarbamoyl-2-phenethyl ester {4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

4-(2,2-bis-ethylcarboxyl-2-phenyl-ethoxycarbonylmethyl)phenyl ether 4'-triptorelin-2-carboxylic acid,

2,2-bis-butylcarbamoyl-2-phenethyl ester {4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-methyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

3,3-bis-ethylcarbazole-3-phenylpropionic ester {4-[(4'-triptorelin-2-Carbo who yl)amino]phenyl}acetic acid,

3-phenyl-3,3-bis-propellerblades-propyl ester {4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ester {4-[(biphenyl-2-carbonyl)amino]phenyl}acetic acid,

4-(2,2-bis-ethylcarboxyl-2-phenyl-ethoxycarbonylmethyl)-2-hlorfenilovy ether 4'-triptorelin-2-carboxylic acid,

2,2-bis-isobutylamino-2-phenethyl ester {4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-(3-methyl-butylcarbamoyl)-2-phenethyl ester {4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ester {4-[(4'-chlorobiphenyl-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ester {4-[(3',4'-dichlorobiphenyl-2-carbonyl)amino]phenyl}acetic acid,

2-phenyl-2,2-bis-propellerblades)ethyl ester {3-methyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-(2-methoxy-ethylcarbamate)-2-phenethyl ester {4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-etilcaprilatului ether {3-isopropyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

3,3-bis-ethylcarbazole-3-phenylpropionyl ether {3-ethyl-4-[(4'-triptorelin-2-carbonyl) amino]f the Nile}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-isobutyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2-phenyl-2,2-bis-propellerblades-ethyl ester {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-methylcarbamoyl-4-((4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

3,3-bis-ethylcarbazole-3-phenylpropionyl ether {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-benzylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

4,4-bis-ethylcarbamate-4-privately ether {3-dimethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-diethylcarbamoyl-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-diisopropylamino-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-(isopropylaminocarbonyl)-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-(ethylmethylamino is)-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

3,3-bis-ethylcarbazole-3-phenylpropionyl ether {3-(ethylmethylamino)-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethyl ether {3-(piperidine-1-carbonyl)-4-[(4'-triptorelin-2-carbonyl)amino]phenyl}acetic acid,

2,2-bis-ethylcarboxyl-2-phenethy