Prodrug 1,3-diamino-2-hydroxypropane derivatives

FIELD: chemistry.

SUBSTANCE: invention relates to the compounds of the formula and their pharmaceutically acceptable salts used as inhibiting agent in the relation of fermentative beta-secretase and it also relates to pharmaceutical compositions based on the formula. In general formula one of RN and RN' represents hydrogen, and another represents - C(=O)-(CRR')0-6R100, or where R4 is chosen from the group including H; NH2; -NR50CO2R51; -(C1-C4)-alkyl-NR50CO2R51; where n7 is equal to 0, 1, 2 or 3; R50 represents H or C1-C6alkyl; R51 is chosen from the group including phenyl-(C1-C4)-alkyl and (C1-C6)-alkyl; X is chosen from the group including -(C1-C6)-alkylidenyl optionally substituted with 1, 2 or 3 metal groups; Z is chosen from the group including bond, SO2, SO and S; Y stands for (C1-C10)-alkyl; R1 represents -(C1-C6)-alkylphenyl where phenyl ring is optionally substituted by 1, 2, 3 or 4 halogen atoms; R and R' independently represent hydrogen or (C1-C6)-alkyl; R2 represents hydrogen; R3 represents hydrogen; Rc represents - (CR245R250)0-4-aryl; where aryl is optionally substituted by 1, 2 or 3 R200; R200 is chosen from the group including (C1-C6)-alkyl optionally substituted with 1, 2 or 3 groups R205; halogen; C=N; R205 stands for halogen; R245 and R250 in each case stands for H; either R245 or R250 are taken together with carbon atom whereto attached to form carbocycle from 3, 4, 5, 6 or 7 carbon atoms; R100 represents 5-6-merous heteroaryl with 1-2 heteroatoms chosen from nitrogen and sulphur, -phenyl-W-heteroaryl where heteroaryl is 5-6-merous ring containing 1-2 heteroatoms, chosen from nitrogen and oxygen and where cyclic parts of each group are optionally substituted by 1, 2 or 3 groups independently chosen among C1-C6alkyl, -(CH2)0-4-CO2-NR105R'105, -(CH2)0-4-SO2-NR105R'105, -(CH2)0-4-N(R150)-CO-R105, -(CH2)0-4-N(R150)-SO2-R105; W represents -(CH2)0-4; R105 and R'105 independently represent (C1-C6)-alkyl optionally substituted with -NH2 or halogen; R150 represents hydrogen.

EFFECT: compounds can be applied to prevent and treat diseases mediated by excess activity of beta-secretase such as Alzheimer's disease.

11 cl, 12 tbl, 3 dwg, 1729 ex

 

Cross-reference to related applications

This application discloses the priority of provisional patent application U.S. No. 60/408783 registered 6 September 2002, included in this description by reference.

The technical field

The invention relates to proletarienne derived 1,3-diamino-2-hydroxypropane and to such compounds that are useful in the treatment of Alzheimer's disease and related diseases. More specifically, it relates to such compounds that are able to give or generate, or in vitro, or in vivo, compounds inhibiting beta secretase - the enzyme that breaks down amyloid protein precursor with the formation of amyloid beta-peptide (A-beta), a major component of amyloid plaques formed in the brain of patients suffering from Alzheimer's disease.

Background of invention

Alzheimer's disease (AD) is a progressive, degenerative brain disease associated mainly with aging. The clinical picture of AD is characterized by memory loss, cognitive abilities, the ability to reason and orientation. As the disease progresses, motor, sensory and linguistic ability also affects up to the overall deterioration of many cognitive functions. Such loss of cognitive functions etc which come gradually, but typically lead to severe deterioration and, ultimately, to death in a period of four to twelve years.

Alzheimer's disease is characterized by two main pathological paintings in the brain: neurofibrillary plexuses and beta-amyloid (or trigeminus) plaques composed mainly of units of the peptide fragment, known as A-beta. Individuals with AD are detected characteristic of beta-amyloid deposits in the brain (beta-amyloid plaques) in the blood vessels of the brain (beta-amyloid angiopathy), and neurofibrillary plexus. Neurofibrillary plexus are not only in Alzheimer's disease, but also other disorders that cause dementia. According to the autopsy, a large number of such damage typically found in areas of the human brain important for memory and cognitive abilities.

A smaller number of such injuries with more limited anatomical distribution found in the brain of elderly people who do not have clinical manifestations of AD. Amyloidogenic plaques and vascular amyloid angiopathy also characterize the brain of individuals with trisomy 21 (down syndrome), hereditary cerebral hemorrhage with amyloidosis-type Dutch (Dutch-Type, HCHWA-D) and other neurodegener the tive disorders. Beta-amyloid is the defining characteristic of AD and is believed to now, a causal predecessor or factor in the development of the disease. The deposition of a-beta in the brain regions responsible for cognitive activity, is a major factor in the development of AD. Beta-amyloid plaques are composed mainly of amyloid beta-peptide (A-beta, also sometimes called beta-A4). Beta-peptide is formed by proteolysis of the amyloid protein precursor (APP) and consists of 39-42 amino acids. In the processing of APP involves some protease called secretase.

Cleavage of APP at the N end of the peptide A-beta beta secretases and on the C-end of one or more gamma secretase is beta amelogenic a cascade of reactions, i.e. the cascade, which is formed of a-beta. Cleavage of APP alpha secretases produces alpha-sAPP - secreterial form of ADR, which does not lead to the formation of beta-amyloid plaques. Such an alternative cascade eliminates the formation of peptide A-beta. Description fragments proteolytic processing includes, for example, in U.S. patent No. 5441870, 5721130 and 5942400.

Asparaginase identified as the enzyme responsible for the processing of APP at the site of cleavage of beta-secretases. The enzyme beta-secretase describe using a variety of items, including VASA, Asp and Melepsin. With the., for example, Sinha et al., 1999, Nature, 402:537-554 (p.501) and published PCT application WO00/17369.

Some data shows that progressive cerebral deposition of beta-amyloid peptide (A-beta) plays a fundamental role in the pathogenesis of AD and can precede cognitive symptoms by years or decades. See, for example, Selkoe, 1991, Neuron, 6:487. Shows the release of A-beta from neurons grown in culture, and the presence of A-beta in the cerebrospinal fluid (CSF) of both healthy individuals and patients with AD. See, for example, Seubert et al., 1992, Nature, 359:325-327.

The assumption was made that the peptide A-beta accumulates in the processing of APP by beta secretases, so it is advisable inhibition of this enzymatic activity in the treatment of AD. Suppose that the processing of APP in vivo at the site of cleavage of beta-secretases is the stage that limits the rate of production of A-beta, and is thus a therapeutic target in the case of treatment of AD. See, for example, Sabbagh M. et al., 1997, Alz. Dis. Rev., 3, 1-19.

Mouse amazed VASE cannot produce A-beta and represent the normal phenotype. When crossed with transgenic mice, sverkhekspressiya RDAs, the offspring shows reduced amount of A-beta in the brain extracts compared with the control animals (Luo et al., 2001, Nature Neuroscience, 4:231-232). These data also support the suppose the s, that ingibirovanie activity of beta-secretase and reduced levels of a-beta in the brain provides a therapeutic method for the treatment of AD and other beta-amyloid disorders.

There are currently no effective treatments to stop, prevent or reverse the development of Alzheimer's disease. Therefore, there is an urgent need for pharmaceuticals that can slow the progression of Alzheimer's disease and/or in the first place, to warn her.

Compounds that are effective inhibitors of beta-secretase that inhibit mediated beta-secretases cleavage of APP, which are effective inhibitors of the production of A-beta and/or effective to reduce deposition of amyloid-beta or plaques that are required for the treatment and prevention of diseases characterized by deposits of amyloid-beta or plaques, such as AD.

Summary of the invention

The invention encompasses compounds of formula (AA), (I) and (X)below, pharmaceutical compositions containing such compounds, and methods of using such compounds or compositions in the treatment of Alzheimer's disease, and more specifically, compounds capable of inhibiting beta-secretase - the enzyme that breaks down amyloid protein precursor, with formation of peptide A-beta, the main components the NTA amyloid plaques, detected in the brain of patients suffering from Alzheimer's disease.

In one aspect the invention relates to compounds of formula AA

and their pharmaceutically acceptable salts, where in the formula one of RNand RN'represents hydrogen and the other represents-C(=O)-(CRR')0-6R100-C(=O)-(CRR')1-6-O-R'100-C(=O)-(CRR')1-6-S-R'100-C(=O)-(CRR')1-6-C(=O)-R100-C(=O)-(CRR')1-6-SO2-R100-C(=O)-(CRR')1-6-NR100-R'100or

where

R4selected from the group consisting of H; NH2; -NH-(CH2)n6-R4-1; -Other8;

-NR50C(O)R5; And (C1-C4)-alkyl-NHC(O)R5; -(CH2)0-4-R8; -O-(C1-C4)-alkanoyl; HE; and (C6-C10)-aryloxy, optionally substituted 1, 2, or 3 groups that represent, independently, halogen, (C1-C4)-alkyl, -CO2H, -C(O)-(C1-C4)-alkoxy or (C1-C4)-alkoxy, (C1-C6)-alkoxy; aryl-(C1-C4)-alkoxy; -NR50CO2R51; -(C1-C4)-alkyl-NR50CO2R51;

-C=N; -CF3; -CF2-CF3; -C≡H; -CH2-CH=CH2; -(CH2)1-4-R4-1; -(CH2)1-4-NH-R4-1;

-O-(CH2)n6 -R4-1; -S-(CH2)n6-R4-1; -(CH2)0-4-NHC(O)-(CH2)0-6-R52; -(CH2)0-4-R53-(CH2)0-4-R54;

where

n6is 0, 1, 2 or 3;

n7is 0, 1, 2 or 3;

R4-1selected from the group consisting of-SO2-((C1-C8)-alkyl), -SO-((C1-C8)-alkyl), -S-((C1-C8)-alkyl), -S-CO-((C1-C6)-alkyl), -SO2-NR4-2R4-3, -CO-(C1-C2)-alkyl, -CO-NR4-3R4-4;

R4-2and R4-3represent, independently, H, (C1-C3)-alkyl or (C3-C6-cycloalkyl;

R4-4represents alkyl, arylalkyl, alkanoyl or arylalkyl;

R4-6represents H or (C1-C6)-alkyl;

R5selected from the group consisting of (C3-C7)-cycloalkyl; and (C1-C6)-alkyl, optionally substituted by 1, 2 or 3 groups which are, independently, halogen, -NR6R7, (C1-C4)-alkoxy, (C5-C6-heteroseksualci, (C5-C6-heteroaryl,

(C6-C10)-aryl, (C3-C7-cycloalkyl-(C1-C4)-alkyl, -S-(C1-C4)-alkyl, -SO2-(C1-C4)-alkyl, -CO2N, -CONR6R7, -CO2-(C1-C4)-alkyl, (C6-C10)-aryloxy; heteros is aryl, optionally substituted by 1, 2 or 3 groups which are, independently, (C1-C4)-alkyl, (C1-C4)-alkoxy, halogen, (C1-C4-halogenated or HE; geterotsiklicheskie, optionally substituted by 1, 2 or 3 groups which are, independently, (C1-C4)-alkyl, (C1-C4)-alkoxy, halogen or (C2-C4-alkanoyl; aryl, optionally substituted 1, 2, 3, or 4 groups that represent, independently, halogen, HE, (C1-C4)-alkyl, (C1-C4)-alkoxy or (C1-C4-halogenated; and-NR6R7; where

R6and R7chosen, independently, from the group consisting of H, (C1-C6)-alkyl, (C2-C6)-alkanoyl, phenyl, -SO2-(C1-C4)-alkyl, phenyl-(C1-C4)-alkyl;

R8selected from the group consisting of-SO2-heteroaryl, -SO2-aryl, -SO2-geterotsiklicheskie, -SO2-(C1-C10)-alkyl, -C(O)other9, geterotsiklicheskie, -S-(C1-C6)-alkyl, -S-(C2-C4)-alkanoyl, where

R9represents aryl-(C1-C4)-alkyl, (C1-C6)-alkyl or H;

R50represents H or (C1-C6)-alkyl;

R51selected from the group consisting of aryl-(C1-C4)-alkyl, (C1-C6)-alkyl, optionally substituted by 1, 2 or 3 groups which are, independently, halogen, cyano, heteroaryl, -NR6R7-C(O)NR6R7, (C3-C7-cycloalkyl or -(C1-C4)-alkoxy; geterotsiklicheskie, optionally substituted 1 or 2 groups that represent, independently, (C1-C4)-alkyl, (C1-C4)-alkoxy, halogen, (C2-C4-alkanoyl, aryl-(C1-C4)-alkyl and-SO2-(C1-C4)-alkyl; alkenyl; quinil; heteroaryl, optionally substituted 1, 2, or 3 groups that represent, independently, HE, (C1-C4)-alkyl, (C1-C4)-alkoxy, halogen, NH2, NH((C1-C6)-alkyl) or N((C1-C6)-alkyl)((C1-C6)-alkyl); heteroaromatic, optionally substituted by 1, 2 or 3 groups which are, independently, (C1-C4)-alkyl, (C1-C4)-alkoxy, halogen, NH2, NH((C1-C6)-alkyl) or N((C1-C6)-alkyl)((C1-C6)-alkyl); aryl; geterotsiklicheskie; and (C3-C8)-cycloalkyl and cycloalkenyl; where the aryl, heterocytolysine, (C3-C8)cycloalkyl and cycloalkenyl group substituted by optionally 1, 2, 3, 4, or 5 groups that represent, independently, halogen, CN, NO2, (C1-C6)-alkyl (C 1-C6)-alkoxy, (C2-C6-alkanoyl, (C1-C6-halogenated, (C1-C6)-halogenoalkane, hydroxy, (C1-C6-hydroxyalkyl, (C1-C6)-alkoxy-(C1-C6)-alkyl, (C1-C6)-dialkoxy, (C1-C6)-dialkoxy-(C1-C6)-alkyl or (C1-C6)-alkoxy-(C1-C6)-alkoxy;

R52is heteroseksualci, heteroaryl, aryl, cycloalkyl, -S(O)0-2-

(C1-C6)-alkyl, CO2H, -C(O)NH2, -C(O)NH(alkyl), C(O)N(alkyl)(alkyl), -CO2-alkyl, -NHS(O)0-2-(C1-C6)-alkyl, -N(alkyl)S(O)0-2-(C1-C6)-alkyl, -S(O)0-2-heteroaryl, -S(O)0-2-aryl, -NH(arylalkyl), -N(alkyl)(arylalkyl), dialkoxy or alkoxy, each of which is optionally substituted by 1, 2, 3, 4, or 5 groups that represent, independently, alkyl, alkoxy, dialkoxy, halogen, halogenated, halogenoalkane, alkanoyl, NO2CN, alkoxycarbonyl or aminocarbonyl;

R53is absent or represents-O-, -C(O)-, -NH-, -N(alkyl)-, -NH-S(O)0-2-, -N(alkyl)-S(O)0-2, -S(O)0-2-NH-, -S(O)0-2-N(alkyl)-, -NH-C(S) -, or-N(alkyl)-C(S)-;

R54is heteroaryl, aryl, arylalkyl, heteroseksualci, CO2H, -CO2-alkyl, -C(O)NH(alkyl), -C(O)N(alkyl)(alkyl), -C(O)NH2, (C1-C8)-Ala is l, HE aryloxy, alkoxy, Allakaket, NH2, NH(alkyl), N(alkyl)(alkyl), or -(C1-C6)-alkyl-CO2-(C1-C6)-alkyl, each of which is optionally substituted by 1, 2, 3, 4, or 5 groups that represent, independently, alkyl, alkoxy, CO2H, -CO2-alkyl, dialkoxy, halogen, halogenated, halogenoalkane, hydroxyalkyl, alkanoyl, NO2CN, alkoxycarbonyl or aminocarbonyl;

X is chosen from the group consisting of -(C1-C6)-alkylidene, optionally substituted by 1, 2 or 3 methyl groups, and-NR4-6; or

R4and R4-6combined with education -(CH2)n10-where

n10is 1, 2, 3 or 4;

Z is chosen from the group consisting of communication, SO2SO, S and S(Oh);

Y is chosen from the group consisting of H, (C1-C4)-halogenoalkane; and (C5-C6)-geterotsiklicheskie; and (C6-C10)-aryl; HE; -N(Y1)(Y2); And (C1-C10)-alkyl, optionally substituted by 1-3 substituents, which may be the same or different and are selected from the group consisting of halogen, hydroxy, alkoxy, dialkoxy, halogenoalkane; and (C3-C8)-cycloalkyl, optionally substituted by 1, 2 or 3 groups selected, independently, from (C1-C3)-alkyl and halogen; alkoxy; aryl, optionally substituted with halogen, alkyl, ALK is XI, CN or NO2; arylalkyl, optionally substituted with halogen, alkyl, alkoxy, CN or NO2; where

Y1and Y2are the same or different and represent H; and (C1-C10)-alkyl, optionally substituted by 1, 2 or 3 substituents selected from the group consisting of halogen, (C1-C4)-alkoxy, (C3-C8)-cycloalkyl and IT; and (C2-C6)-alkenyl; and (C2-C6-alkanoyl; phenyl; -SO2-(C1-C4)-alkyl; phenyl-(C1-C4)-alkyl or (C3-C8-cycloalkyl-(C1-C4)-alkyl; or

Y1, Y2and the nitrogen atom to which they are attached, form a cycle selected from the group consisting of piperazinil, piperidinyl, morpholinyl and pyrrolidinyl, where each cycle is optionally substituted by 1, 2, 3, or 4 groups that represent, independently, (C1-C6)-alkyl, (C1-C6)-alkoxy, (C1-C6)-alkoxy-(C1-C6)-alkyl or halogen;

R1represents -(CH2)1-2-S(O)0-2-(C1-C6)-alkyl or

(C1-C10)-alkyl, optionally substituted by 1, 2 or 3 groups selected, independently, from halogen, HE, =O, -SH, -C≡N, -CF3-(C1-C3)-alkoxy, amino, mono - or dialkylamino, -N(R)C(O)R',- OC(=O)-amino and-OC(=O)-mono - or-dialkylamino, or

(C2/sub> -C6)-alkenyl or (C2-C6)-quinil, each of which is optionally substituted by 1, 2 or 3 groups selected, independently, from halogen, -OH, -SH, -C≡N, -CF3, (C1-C3)-alkoxy, amino and mono - or dialkylamino, or

aryl, heteroaryl, heterocyclyl -(C1-C6-alkylaryl -(C1-C6-alkylglycerol or -(C1-C6)-Alkylglucoside, where the cyclical part of each substituent optionally substituted by 1, 2, 3 or 4 groups selected, independently, from halogen, -OH, -SH, -C≡N, -NR105R'105, -CO2R, -N(R)COR', or-N(R)SO2R', -C(=O)-(C1-C4)-alkyl, -SO2-amino, -SO2-mono - or-dialkylamino, -C(=O)-amino, -C(=O)-mono - or-dialkylamino, -SO2-(C1-C4)-alkyl, or

-(C1-C6)-alkoxy, optionally substituted 1, 2, or 3 groups that represent, independently, halogen, or

(C3-C7-cycloalkyl, optionally substituted by 1, 2 or 3 groups selected, independently, from halogen, -OH, -SH, -C≡N, -CF3, (C1-C3)-alkoxy, amino, -(C1-C6)-alkyl and mono - or dialkylamino, or

(C1-C10)-alkyl, optionally substituted by 1, 2 or 3 groups selected, independently, from halogen, -OH, -SH, -C≡N, -CF3, (C1-C3)-alkoxy, amino, mono - or dialkylamino and -(C1-C 3)-alkyl, or

(C2-C10)-alkenyl or (C2-C10)-quinil, each of which is optionally substituted by 1, 2 or 3 groups selected, independently, from halogen, -OH, -SH, -C≡N, -CF3, (C1-C3)-alkoxy, amino, (C1-C6)-alkyl and mono - or dialkylamino; and

heterocycla the group is also optionally substituted by oxo;

R and R' represent, independently, hydrogen or (C1-C10)-alkyl;

R2selected from the group consisting of H; and (C1-C6)-alkyl, optionally substituted by 1, 2 or 3 substituents selected, independently, from the group consisting of (C1-C3)-alkyl, halogen, -OH, -SH, -C≡N, -CF3, (C1-C3)-alkoxy and

-NR1-aR1-b; where R1-aand R1-brepresent-H or (C1-C6)-alkyl; -(CH2)0-4-aryl; -(CH2)0-4-heteroaryl; and (C2-C6-alkenyl; and (C2-C6)-quinil; -CO-NRN-2RN-3; -SO2-NRN-2RN-3; -CO2H and-CO2-((C1-C4)-alkyl);

R3selected from the group consisting of H; and (C1-C6)-alkyl, optionally substituted by 1, 2 or 3 substituents selected, independently, from the group consisting of (C1-C3)-alkyl, halogen, -OH, -SH, -C≡N, -CF3, (C1-C3)-alkoxy and

-NR1-aR1-b; -(CH2)0-4-aryl; -(CH2)0-4-heteroaryl; and (C2-C6-alkenyl; and (C2-C6)-quinil; -CO-NRN-2RN-3; -SO2-NRN-2RN-3; -CO2H and-CO-O-((C1-C4)-alkyl);

or

R2, R3and the carbon atom to which they are attached, form carbocycle from three to seven carbon atoms, where one carbon atom is optionally replaced by a group selected from among-O-, -S-, -SO2- or-NRN-2-;

Rwithselected from the group consisting of (C1-C10)-alkyl, optionally substituted by 1, 2 or 3 groups selected, independently, from the group consisting of

R205, -OC=ONR235R240, -S(=O)0-2((C1-C6)-alkyl), -SH, -NR235C=ONR235R240, -C=ONR235R240and-S(=O)2NR235R240; -(CH2)0-3-(C3-C8)-cycloalkyl where cycloalkyl optionally substituted by 1, 2 or 3 groups selected, independently, from the group consisting of R205, -CO2H and CO2-((C1-C4)-alkyl); -(CR245R250)0-4-aryl;

-(CR245R250)0-4-heteroaryl; -(CR245R250)0-4-geterotsiklicheskie; -(CR245R250)0-4-arylheteroacetic; -(CR245R250)0-4-analgeticalkie; -(CR245R250)0-4-Ariella; -(CR245R250)0-4heteroallyl; -(CR245R250)0-4-heterooligomerization; -(CR245R250)0-4-heteroarylboronic; -(CR245R250)0-4-geterotsiklicheskikh; -(CR245R250)0-4-geterotsiklicheskikh; -(CR245R250)0-4-geterotsiklicheskikh; -[C(R255)(R260)]1-3-CO-N(R255)2; -CH(aryl)2; -CH(heteroaryl)2; -CH(heteroseksualci)2; -CH(aryl)(heteroaryl); cyclopentene, tsiklogeksilnogo or cycloheptyl rings, condensed with aryl, heteroaryl or heterocyclization, where one carbon atom of cyclopentyl, cyclohexyl or cycloheptyl optionally replaced with NH, NR215, O, or S(=O)0-2and where cyclopentamine, tsiklogeksilnogo or cycloheptyl group may be optionally substituted 1 or 2 groups that represent, independently, R205or =O; -CO-NR235R240; -SO2-(C1-C4)-alkyl, (C2-C10-alkenyl, optionally substituted by 1, 2 or 3 groups R205; And (C2-C10)-quinil, optionally substituted by 1, 2 or 3 groups R205; -(CH2)0-1-CH((CH2)0-6-OH)-(CH2)0-1-aryl; -(CH2)0-1-CHRS-6-(CH2)0-1-heteroaryl; -CH(-aryl or-heteroaryl)-CO-O((C1-C4)-alkyl); -CH(-CH2-On the Sabbath.)-CH(OH)-phenyl-NO 2; ((C1-C6)-alkyl)-O-((C1-C6)-alkyl) -;- CH2-NH-CH2-CH(-O-CH2-CH3)2; -N and -(CH2)0-6-C(=NR235)(NR235R240); where

each aryl optionally substituted by 1, 2 or 3 R200;

each heteroaryl optionally substituted by 1, 2, 3 or 4 R200;

each heteroseksualci optionally substituted by 1, 2, 3 or 4 R210;

R200in each case chosen, independently, from the group consisting of (C1-C6)-alkyl, optionally substituted by 1, 2 or 3 groups R205; HE; -NO2; halogen; -CO2N; C≡N; -(CH2)0-4-CO-NR220R225; -(CH2)0-4-CO-((C1-C12)-alkyl);

-(CH2)0-4-CO-((C2-C12-alkenyl); -(CH2)0-4-CO-((C2-C12)-quinil); -(CH2)0-4-CO-((C3-C7)-cycloalkyl); -(CH2)0-4-CO-aryl; -(CH2)0-4-CO-heteroaryl; -(CH2)0-4-CO-geterotsiklicheskie; -(CH2)0-4-CO2R215; -(CH2)0-4-SO2-NR220R225;

-(CH2)0-4-SO-(C1-C8)-alkyl; -(CH2)0-4-SO2-(C1-C12)-alkyl; -(CH2)0-4-SO2-(C3-C7)-cycloalkyl; -(CH2)0-4-N(H or R215)-CO2R215; -(CH2)0-4-N(H or R215)-CO-N(R215 )2; -(CH2)0-4-N-CS-N(R215)2; -(CH2)0-4-N(-H or R215)-CO-R220; -(CH2)0-4-NR220R225; -(CH2)0-4-O-CO-(C1-C6)-alkyl; -(CH2)0-4-O-P(O)-(OR240)2;

-(CH2)0-4-O-CO-N(R215)2; -(CH2)0-4-O-CS-N(R215)2; -(CH2)0-4-O-(R215)2; -(CH2)0-4-O-(R215)2-COOH; -(CH2)0-4-S-(R215)2; -(CH2)0-4-O-((C1-C6)-alkyl, optionally substituted by 1, 2, 3, or 5-F); and (C3-C7)-cycloalkyl; and (C2-C6-alkenyl, optionally substituted 1 or 2 groups R205; And (C2-C6)-quinil, optionally substituted 1 or 2 groups R205; -(CH2)0-4-N(H or R215)-SO2-R220and -(CH2)0-4-(C3-C7)-cycloalkyl; where each aryl group in each case is optionally substituted by 1, 2, or 3 groups that represent, independently, R205, R210or (C1-C6)-alkyl, substituted 1, 2, or 3 groups that represent, independently, R205or R210;

where each heterocytolysine group in each case is optionally substituted by 1, 2, or 3 groups that represent, independently, R210;

where each gets rohilla group in each case is optionally substituted 1, 2 or 3 groups which are, independently, R205, R210or (C1-C6)-alkyl, substituted 1, 2, or 3 groups that represent, independently, R205or R210;

R205in each case chosen, independently, from the group consisting of (C1-C6)-alkyl, halogen, -OH, -O-phenyl, -SH, -C≡N, -CF3, (C1-C6)-alkoxy, NH2,

NH((C1-C6)-alkyl) and N((C1-C6)-alkyl)((C1-C6)-alkyl);

R210in each case chosen, independently, from the group consisting of (C1-C6)-alkyl, optionally substituted by 1, 2 or 3 groups R205; And (C2-C6-alkenyl, optionally substituted by 1, 2 or 3 groups R205; And (C2-C6)-quinil, optionally substituted by 1, 2 or 3 groups R205; halogen; (C1-C6)-alkoxy, (C1-C6)-halogenoalkane; -NR220R225; OH; C≡N; and (C3-C7)-cycloalkyl, optionally substituted by 1, 2 or 3 groups R205; -CO-((C1-C4)-alkyl);

-SO2-NR235R240; -CO-NR235R240; -SO2-((C1-C4)-alkyl) and =O, where

R215in each case chosen, independently, from the group consisting of (C1-C6)-alkyl, (CH2)0-2-aryl, (C2-C6-alkenyl, (C2-C6)-quinil, (C3-C 7)-cycloalkyl, (CH2)0-2-heteroaryl and (CH2)0-2-geterotsiklicheskie, where the aryl group in each case is optionally substituted by 1, 2, or 3 groups that represent, independently, R205or R210; where heterocytolysine group in each case is optionally substituted by 1, 2 or 3 R210; where each heteroaryl group in each case is optionally substituted by 1, 2 or 3 R210;

R220and R225in each case chosen, independently, from the group consisting of-H,

-(C1-C6)-alkyl, hydroxy-(C1-C6)-alkyl, amino-(C1-C6)-alkyl, halogen-(C1-C6)-alkyl, (C3-C7)-cycloalkyl, -((C1-C2)-alkyl)-((C3-C7)-cycloalkyl), -((C1-C6)-alkyl)-O-((C1-C3)-alkyl), -(C2-C6-alkenyl -(C2-C6)-quinil -(C1-C6)-alkyl chain with one double bond and one triple bond, -aryl, -heteroaryl and-geterotsiklicheskie, where the aryl group in each case is optionally substituted by 1, 2 or 3 groups R270where

R270in each case represents, independently, R205, (C1-C6)-alkyl, optionally substituted by 1, 2 or 3 groups R205; And (C2-C6)-alkenyl, not necessarily for ewenny 1, 2 or 3 groups R205; And (C2-C6)-quinil, optionally substituted by 1, 2 or 3 groups R205; halogen; (C1-C6)-alkoxy, (C1-C6)-halogenoalkane; NR235R240; OH; C≡N; and (C3-C7-cycloalkyl, optionally substituted by 1, 2 or 3 groups R205; -CO-((C1-C4)-alkyl); -SO2-NR235R240; -CO-NR235R240; -SO2-((C1-C4)-alkyl) and =O, where heterocytolysine group in each case is optionally substituted by 1, 2 or 3 groups R205; where each heteroaryl group in each case is optionally substituted by 1, 2 or 3 groups R205;

R235and R240in each case represent, independently, H or (C1-C6)-alkyl;

R245and R250in each case chosen, independently, from the group consisting of H, (C1-C4)-alkyl, (C1-C4)-hydroxyalkyl, (C1-C4)-alkoxy, (C1-C4)-halogenoalkane,

-(CH2)0-4-(C3-C7)-cycloalkyl, (C2-C6-alkenyl, (C2-C6)-quinil, aryl-(C1-C4)-alkyl, heteroaryl-(C1-C4)-alkyl and phenyl; or

R245and R250taken together with the carbon atom to which they are attached, to form carbocycle of 3, 4, 5, 6 or 7 carbon atoms, g is e optionally one carbon atom is replaced by a heteroatom, selected from the group consisting of-O-, -S-,

-SO2- , and-NR220-;

R255and R260in each case chosen, independently, from the group consisting of H; and (C1-C6)-alkyl, optionally substituted by 1, 2 or 3 groups R205; And (C2-C6-alkenyl, optionally substituted by 1, 2 or 3 groups R205; And (C2-C6)-quinil, optionally substituted by 1, 2 or 3 groups R205;

-(CH2)1-2-S(O)0-2-((C1-C6)-alkyl), -(CH2)0-4-(C3-C7)-cycloalkyl, optionally substituted by 1, 2 or 3 groups R205; -((C1-C4)-alkyl)aryl; -((C1-C4)-alkyl)heteroaryl; -((C1-C4)-alkyl)geterotsiklicheskie; -aryl; -heteroaryl; -geterotsiklicheskie;

-(CH2)1-4-R265-(CH2)0-4-aryl; -(CH2)1-4-R265-(CH2)0-4-heteroaryl and -(CH2)1-4-R265-(CH2)0-4-geterotsiklicheskie; where

R265in each case represents, independently, -O-, -S - or-N((C1-C6)-alkyl)-;

each aryl or phenyl optionally substituted by 1, 2, or 3 groups that represent, independently, R205, R210or (C1-C6)-alkyl, substituted 1, 2, or 3 groups that represent, independently, R205or R210;

each heteroaryl is what I optionally substituted 1, 2, 3, or 4 R200each heteroseksualci is optionally substituted by 1, 2, 3 or 4 R210;

R100and R'100represent, independently, aryl, heteroaryl, heterocyclyl, -aryl-W-aryl, -aryl-W-heteroaryl, -aryl-W-heterocyclyl-heteroaryl-W-aryl, -heteroaryl-W-heteroaryl-heteroaryl-W-heterocyclyl, -heterocyclyl-W-aryl, -heterocyclyl-W-heteroaryl, -heterocyclyl-W-heterocyclyl, -CH[(CH2)0-2-O-R150]-

(CH2)0-2-aryl, -CH[(CH2)0-2-O-R150]-(CH2)0-2-heterocyclyl or-CH[(CH2)0-2-O-R150]-

(CH2)0-2-heteroaryl, where the cyclical part of each group optionally substituted by 1, 2 or 3 groups selected, independently, from

-OR, -NO2, (C1-C6)-alkyl, halogen, -CN, -OCF3, -CF3, -(CH2)0-4-O-P(=O)(OR)(OR'), -(CH2)0-4-CO-NR105R'105, -(CH2)0-4-O-(CH2)0-4-CONR102R102', -(CH2)0-4-CO-((C1-C12)-alkyl), -(CH2)0-4-CO-((C2-C12-alkenyl), -(CH2)0-4-CO-((C2-C12)-quinil), -(CH2)0-4-CO-(CH2)0-4-((C3-C7)-cycloalkyl), -(CH2)0-4-R110, -(CH2)0-4-R120, -(CH2)0-4-R130, -(CH2)0-4-CO-R110, -(CH2)0-4-CO-R120, -(CH2)0-4-What about the-R 130, -(CH2)0-4-CO-

R140, -(CH2)0-4-CO-O-R150, -(CH2)0-4-SO2-NR105R'105, -(CH2)0-4SO is((C1-C8)-alkyl), -(CH2)0-4-SO2-((C1-C12)-alkyl), -(CH2)0-4-SO2-(CH2)0-4-((C3-C7)-cycloalkyl), -(CH2)0-4-N(R150)-CO-O-R150, -(CH2)0-4-N(R150)-CO-N(R150)2, -(CH2)0-4-N(R150)-CS-

N(R150)2, -(CH2)0-4-N(R150)-CO-R105, -(CH2)0-4-NR105R'105, -(CH2)0-4-R140, -(CH2)0-4-O-CO-((C1-C6)-alkyl), -(CH2)0-4-O-P(O)-(O-R110)2, -(CH2)0-4-O-CO-N(R150)2, -(CH2)0-4-O-CS-N(R150)2, -(CH2)0-4-O-(R150), -(CH2)0-4-O-R150'-COOH, -(CH2)0-4-S-(R150), -(CH2)0-4-N(R150)-SO2-R105, -(CH2)0-4-

((C3-C7)-cycloalkyl), (C2-C10-alkenyl and (C2-C10)-quinil, or

R100is a (C1-C10)-alkyl, optionally substituted by 1, 2 or 3 groups R115or

R100represents -((C1-C6)-alkyl)-O-((C1-C6)-alkyl) or -((C1-C6)-alkyl)-S-((C1-C6)-alkyl), to whom gdy of which is optionally substituted 1, 2 or 3 groups R115or

R100is a (C3-C8-cycloalkyl, optionally substituted by 1, 2 or 3 groups R115;

W represents -(CH2)0-4-, -O-, -S(O)0-2, -N(R135)-, -CR(OH)- or-C(O)-;

R102and R102' represent, independently, hydrogen or (C1-C10)-alkyl, optionally substituted by 1, 2 or 3 groups which are, independently, halogen, aryl or-R110;

R105and R'105represent, independently, -H, -R110, -R120, (C3-C7-cycloalkyl, -((C1-C2)-alkyl)-((C3-C7-cycloalkyl), -((C1-C6)-alkyl))-((C1-C3)-alkyl), (C2-C6)-alkenyl, (C2-C6)-quinil or (C1-C6)-alkyl chain with one double bond and one triple bond, or

(C1-C6)-alkyl, optionally substituted-HE or-NH2; or

(C1-C6)-alkyl, optionally substituted by 1, 2 or 3 groups selected, independently, from halogen, or

R105and R'105together with the atom to which they are attached, form a 3-7-membered carbocyclic ring in which one member is an optional heteroatom selected from-O-, -S(O)0-2- , and-NR135-and the cycle is optionally substituted by 1, 2 or 3 groups selected, independently researched the mo, from among the groups R140;

R115in each case represents, independently, halogen, -OH, -CO2R102-(C1-C6)-dialkoxy, -CO2-phenyl, -NR105R'135, -SO2-((C1-C8)-alkyl), -C(=O)R180, R180, -CONR105R'105, -SO2-NR105R'105, -NH-CO-((C1-C6)-alkyl), -NH-C(=O)-OH, -NH-C(=O)-OR, -NH-C(=O)-O-phenyl, -O-C(=O)-((C1-C6)-alkyl), -O-C(=O)amino, -O-C(=O)mono - or dialkylamino, -O-C(=O)phenyl, -O-((C1-C6)-alkyl)CO2N, -NH-SO2-((C1-C6)-alkyl), (C1-C6)-alkoxy or (C1-C6)-halogenoalkane;

R135is a (C1-C6)-alkyl, (C2-C6)-alkenyl, (C2-C6)-quinil, (C3-C7-cycloalkyl, -(CH2)0-2-aryl, -(CH2)0-2-heteroaryl or -(CH2)0-2-heterocyclyl;

R140represents heterocyclyl, optionally substituted 1, 2, 3 or 4 groups selected, independently, from (C1-C6)-alkyl, (C1-C6)-alkoxy, halogen, hydroxy, cyano, nitro, amino, mono(C1-C6)alkylamino, di(C1-C6)alkylamino, (C2-C6-alkenyl, (C2-C6)-quinil, (C1-C6)-halogenoalkane,

(C1-C6)-halogenoalkane, amino(C1-C6)alkyl, mono(C1-C6)is alkylamino(C 1-C6)alkyl,

di(C1-C6)alkylamino(C1-C6)alkyl and =On;

R145is a (C1-C6)-alkyl or CF3;

R150represents hydrogen, (C3-C7-cycloalkyl, -((C1-C2)-alkyl)-((C3-C7-cycloalkyl), (C2-C6)-alkenyl, (C2-C6)-quinil, (C1-C6)-alkyl with one double bond and one triple bond, -R110, -R120or

(C1-C6)-alkyl, optionally substituted by 1, 2, 3 or 4 groups selected, independently, from among-OH, -NH2, (C1-C3)-alkoxy, R110and halogen;

R150' is a (C3-C7-cycloalkyl, -((C1-C3)-alkyl)-((C3-C7-cycloalkyl), (C2-C6)-alkenyl, (C2-C6)-quinil, (C1-C6)-alkyl with one double bond and one triple bond, -R110, -R120or

(C1-C6)-alkyl, optionally substituted by 1, 2, 3 or 4 groups selected, independently, from among-OH, -NH2, (C1-C3)-alkoxy, R110and halogen;

R155is a (C3-C7-cycloalkyl, -((C1-C2)-alkyl)-((C3-C7-cycloalkyl), (C2-C6)-alkenyl, (C2-C6)-quinil, (C1-C6)-alkyl with one double bond and one triple SV is su, -R110, -R120or

(C1-C6)-alkyl, optionally substituted by 1, 2, 3 or 4 groups selected, independently, from among-OH, -NH2, (C1-C3)-alkoxy and halogen;

R180choose from a number of morpholinyl, thiomorpholine, piperazinil, piperidinyl, homomorpholine, homotaurine, homotaurine-S-oxide, homotaurine-S,S-dioxide, pyrrolidine and pyrrolidinyl, each of which is optionally substituted by 1, 2, 3 or 4 groups selected, independently, from (C1-C6)-alkyl, (C1-C6)-alkoxy, halogen, hydroxy, cyano, nitro, amino, mono(C1-C6)alkylamino, di(C1-C6)alkylamino, (C2-C6-alkenyl, (C2-C6)-quinil, (C1-C6)-halogenoalkane, (C1-C6)-halogenoalkane, amino(C1-C6)-alkyl, mono(C1-C6)alkylamino(C1-C6)alkyl, di(C1-C6)alkylamino

(C1-C6)alkyl and =On;

R110represents aryl, optionally substituted 1 or 2 groups R125;

R125in each case represents, independently, halogen, amino, mono - or dialkylamino, -OH, -C≡N, -SO2-NH2, -SO2-NH-((C1-C6)-alkyl), -SO2-N((C1-C6)-alkyl)2, -SO2-((C1-C4)-alkyl), -CO-NH2, -CO-NH-((C1-C6 )-alkyl) or-CO-N((C1-C6)-alkyl)2or

(C1-C6)-alkyl, (C2-C6)-alkenyl or (C2-C6)-quinil, each of which is optionally substituted by 1, 2 or 3 groups selected, independently, from (C1-C3)-alkyl, halogen, -OH, -SH, -C≡N, -CF3, (C1-C3)-alkoxy, amino, and mono - and dialkylamino, or

(C1-C6)-alkoxy, optionally substituted with one, two or three galactography;

R120is heteroaryl, optionally substituted 1 or 2 groups

R125; and

R130represents heterocyclyl, optionally substituted 1 or 2 groups R125.

The invention also relates to compounds of formula I

and their pharmaceutically acceptable salts, where in the formula, R1, R2, R3and RChave the meanings specified for formula (AA), and

RNrepresents-C(=O)-(CRR')0-6R100-C(=O)-

(CRR')1-6-O-R'100-C(=O)-(CRR')1-6-S-R'100-C(=O)-(CRR')1-6-C(=O)-R100-C(=O)-(CRR')1-6-SO2-R100-C(=O)-(CRR')1-6-NR100-R'100or

RNrepresents a

where

R4selected from the group consisting of H; NH2; -NH-(CH2)n6-R4-1; -Other8;

-NR 50C(O)R5; And (C1-C4)-alkyl-NHC(O)R5; -(CH2)0-4R8; -O-(C1-C4)-alkanoyl; HE; and (C6-C10)-aryloxy, optionally substituted 1, 2, or 3 groups that represent, independently, halogen, (C1-C4)-alkyl, -CO2H, -C(O)-(C1-C4)-alkoxy or (C1-C4)-alkoxy, (C1-C6)-alkoxy; aryl-(C1-C4)-alkoxy; -NR50CO2R51; -(C1-C4)-alkyl-NR50CO2R51; -C≡N; -CF3; -CF2-CF3; -C≡CH; -CH2-CH=CH2; -(CH2)1-4-R4-1; -(CH2)1-4-NH-R4-1;

-O-(CH2)n6-R4-1; -S-(CH2)n6-R4-1; -(CH2)0-4-NHC(O)-(CH2)0-6-R52; -(CH2)0-4-R53-(CH2)0-4-R54;

where

n6is 0, 1, 2 or 3;

n7is 0, 1, 2 or 3;

R4-1selected from the group consisting of-SO2-((C1-C8)-alkyl), -SO-((C1-C8)-alkyl), -S-((C1-C8)-alkyl), -S-CO-((C1-C6)-alkyl), -SO2-NR4-2R4-3;- ((C1-C2)-alkyl), -CO-NR4-3R4-4;

R4-2and R4-3represent, independently, H, (C1-C3)-alkyl or (C3-C6-cycloalkyl;

R4-4represents alkyl, arylalkyl, alkanoyl or arylalkyl;

R represents H or (C1-C6)-alkyl;

R5selected from the group consisting of (C3-C7)-cycloalkyl; (C1-C6)-alkyl, optionally substituted by 1, 2 or 3 groups which are, independently, halogen, -NR6R7, (C1-C4)-alkoxy, (C5-C6-heteroseksualci, (C5-C6-heteroaryl, (C6-C10)-aryl, (C3-C7-cycloalkyl-(C1-C4)-alkyl, -S-(C1-C4)-alkyl, -SO2-(C1-C4)-alkyl, -CO2H, -CO-NR6R7, -CO2-(C1-C4)-alkyl, (C6-C10)-aryloxy; heteroaryl, optionally substituted by 1, 2 or 3 groups which are, independently, (C1-C4)-alkyl, (C1-C4)-alkoxy, halogen, (C1-C4-halogenated or HE; geterotsiklicheskie, optionally substituted by 1, 2 or 3 groups which are, independently, (C1-C4)-alkyl, (C1-C4)-alkoxy, halogen or

(C2-C4-alkanoyl; aryl, optionally substituted 1, 2, 3, or 4 groups that represent, independently, halogen, (C1-C4)-alkyl, (C1-C4)-alkoxy or (C1-C4-halogenated; and-NR6R7where R6and R7chosen, independently, from the group consisting of H, (C1-C6)-alkyl, (C2-C6 )-alkanoyl, phenyl, -SO2-(C1-C4)-alkyl, phenyl-(C1-C4)-alkyl;

R8selected from the group consisting of-SO2-heteroaryl, -SO2-aryl, -SO2-geterotsiklicheskie, -SO2-(C1-C10)-alkyl, -C(O)other9, geterotsiklicheskie, -S-(C1-C6)-alkyl, -S-(C2-C4)-alkanoyl, where

R9represents aryl-(C1-C4)-alkyl, (C1-C6)-alkyl or H;

R50represents H or (C1-C6)-alkyl;

R51selected from the group consisting of aryl-(C1-C4)-alkyl, (C1-C6)-alkyl, optionally substituted by 1, 2 or 3 groups which are, independently, halogen, cyano, heteroaryl, -NR6R7-C(O)-NR6R7, (C3-C7-cycloalkyl or -(C1-C4)-alkoxy; geterotsiklicheskie, optionally substituted 1 or 2 groups that represent, independently, (C1-C4)-alkyl, (C1-C4)-alkoxy, halogen, (C2-C4-alkanoyl, aryl-(C1-C4)-alkyl and-SO2-(C1-C4)-alkyl; alkenyl; quinil; heteroaryl, optionally substituted by 1, 2 or 3 groups which are, independently, (C1-C4)-alkyl, (C1-C4)-alkoxy, halogen, NH2, NH((C1-C6)-alkyl) or N((C1-C6)-alkyl)((C1 -C6)-alkyl); heteroaromatic, optionally substituted by 1, 2 or 3 groups which are, independently, (C1-C4)-alkyl, (C1-C4)-alkoxy, halogen, NH2, NH((C1-C6)-alkyl) or N((C1-C6)-alkyl)((C1-C6)-alkyl); aryl; geterotsiklicheskie; (C3-C8)-cycloalkyl and cycloalkenyl; where the aryl, heterocytolysine, (C3-C8)-cycloalkyl and cycloalkenyl group optionally substituted by 1, 2, 3, 4, or 5 groups that represent, independently, halogen, CN, NO2, (C1-C6)-alkyl, (C1-C6)-alkoxy, (C2-C6-alkanoyl, (C1-C6-halogenated, (C1-C6)-halogenoalkane, hydroxy, (C1-C6-hydroxyalkyl, (C1-C6)-alkoxy-(C1-C6)-alkyl, (C1-C6)-dialkoxy,

(C1-C6)-dialkoxy-(C1-C6)-alkyl or (C1-C6)-alkoxy-(C1-C6)-alkoxy;

R52is heteroseksualci, heteroaryl, aryl, cycloalkyl, -S(O)0-2-

(C1-C6)-alkyl, CO2H, -C(O)NH2, -C(O)NH(alkyl), -C(O)N(alkyl)(alkyl), -CO2-alkyl, -NHS(O)0-2-(C1-C6)-alkyl, -N(alkyl)S(O)0-2-(C1-C6)-alkyl, -S(O)0-2-heteroaryl, -S(O)0-2-aryl, -NH(arylalkyl), -N(alkyl)(arylalkyl), dialkoxy or Alcock and, each of which is optionally substituted by 1, 2, 3, 4, or 5 groups that represent, independently, alkyl, alkoxy, dialkoxy, halogen, halogenated, halogenoalkane, alkanoyl, NO2CN, alkoxycarbonyl or aminocarbonyl;

R53is absent or represents-O-, -C(O)-, -NH-, -N(alkyl)-, -NH-S(O)0-2-, -N(alkyl)-S(O)0-2-, -S(O)0-2-NH-, -S(O)0-2-N(alkyl)-, -NH-C(S) -, or-N(alkyl)-C(S)-;

R54is heteroaryl, aryl, arylalkyl, heteroseksualci, CO2H, -CO2-alkyl, -C(O)NH(alkyl), -C(O)N(alkyl)(alkyl), -C(O)NH2, (C1-C8)-alkyl, HE aryloxy, alkoxy, Allakaket, NH2, NH(alkyl), N(alkyl)(alkyl), or -(C1-C6)-alkyl-CO2-(C1-C6)-alkyl, each of which is optionally substituted by 1, 2, 3, 4, or 5 groups that represent, independently, alkyl, alkoxy, CO2H, -CO2-alkyl, dialkoxy, halogen, halogenated, halogenoalkane, hydroxyalkyl, alkanoyl, NO2CN, alkoxycarbonyl or aminocarbonyl;

X is chosen from the group consisting of -(C1-C6)-alkylidene, optionally substituted by 1, 2 or 3 methyl groups, and-NR4-6or

R4and R4-6combined with education -(CH2)n10-where

n10is 1, 2, 3 or 4;

Z is chosen from the group consisting of communication, SO2SO, S and S(Oh);

Y is chosen from the group consisting the th of N; (C1-C4)-halogenoalkane; (C5-C6)-geterotsiklicheskie; (C6-C10)-aryl; IT; N(Y1)(Y2); (C1-C10)-alkyl, optionally substituted by 1-3 substituents, which may be the same or different and are selected from the group consisting of halogen, hydroxy, alkoxy, dialkoxy, halogenoalkane; (C3-C8)-cycloalkyl, optionally substituted by 1, 2 or 3 groups independently selected from among (C1-C3)-alkyl and halogen; alkoxy; aryl, optionally substituted with halogen, alkyl, alkoxy, CN or NO2; arylalkyl, optionally substituted with halogen, alkyl, alkoxy, CN or NO2; where

Y1and Y2are the same or different and represent H; (C1-C10)-alkyl, optionally substituted by 1, 2 or 3 substituents selected from the group consisting of halogen, (C1-C4)-alkoxy, (C3-C8)-cycloalkyl and HE; (C2-C6)-alkenyl; (C2-C6-alkanoyl; phenyl; -SO2-(C1-C4)-alkyl, phenyl-(C1-C4)-alkyl or (C3-C8-cycloalkyl-(C1-C4)-alkyl; or

Y1and Y2and the nitrogen atom to which they are attached, form a cycle selected from the group consisting of piperazinil, piperidinyl, morpholinyl and pyrrolidinyl, where each cycle is long is correctly substituted 1, 2, 3, or 4 groups that represent, independently, (C1-C6)-alkyl, (C1-C6)-alkoxy, (C1-C6)-alkoxy-(C1-C6)-alkyl or halogen;

R100and R'100represent, independently, aryl, heteroaryl, heterocyclyl, -aryl-W-aryl, -aryl-W-heteroaryl, -aryl-W-heterocyclyl-heteroaryl-W-aryl, -heteroaryl-W-heteroaryl-heteroaryl-W-heterocyclyl, -heterocyclyl-W-aryl, -heterocyclyl-W-heteroaryl, -heterocyclyl-W-heterocyclyl, -CH[(CH2)0-2-O-R150]-(CH2)0-2-aryl, -CH[(CH2)0-2-O-R150]-(CH2)0-2-heterocyclyl or-CH[(CH2)0-2-O-R150]-(CH2)0-2-heteroaryl, where the cyclical part of each substituent optionally substituted by 1, 2 or 3 groups selected, independently, from

-OR, -NO2, (C1-C6)-alkyl, halogen, -C≡N, -OCF3, -CF3, -(CH2)0-4-O-P

(=)(OR)(OR'), -(CH2)0-4-CO-NR105R'105, -(CH2)0-4-O-(CH2)0-4-CO-NR102R102', -(CH2)0-4-CO-((C1-C12)-alkyl), -(CH2)0-4-CO-((C2-C12-alkenyl), -(CH2)0-4-CO-((C2-C12)-quinil), -(CH2)0-4-CO-(CH2)0-4-((C3-C7)-cycloalkyl), -(CH2)0-4-R110, -(CH2)0-4-R120,

-(CH2)0-4-R130, -(CH2 )0-4-CO-R110, -(CH2)0-4-CO-R120, -(CH2)0-4-CO-R130, -(CH2)0-4-CO-R140,

-(CH2)0-4-CO-O-R150, -(CH2)0-4-SO2-NR105R'105, -(CH2)0-4SO is((C1-C8)-alkyl), -(CH2)0-4-SO2-

((C1-C12)-alkyl), -(CH2)0-4-SO2-(CH2)0-4-((C3-C7)-cycloalkyl), -(CH2)0-4-N(R150)-CO-O-

R150, -(CH2)0-4-N(R150)-CO-N(R150)2, -(CH2)0-4-N(R150)-CS-N(R150)2, -(CH2)0-4-N(R150)-CO-R105, -(CH2)0-4-NR105R'105, -(CH2)0-4-R140, -(CH2)0-4-O-CO-((C1-C6)-alkyl), -(CH2)0-4-O-P(O)-(O-R110)2, -(CH2)0-4-O-CO-N(R150)2, -(CH2)0-4-O-CS-N(R150)2, -(CH2)0-4-O-(R150), -(CH2)0-4-O-R150'-COOH, -(CH2)0-4-S-(R150), -(CH2)0-4-N(R150)-SO2-R105, -(CH2)0-4-((C3-C7)-cycloalkyl), (C2-C10-alkenyl and (C2-C10)-quinil, or

R100is a (C1-C10)-alkyl, optionally substituted by 1, 2 or 3 groups R115or

R100represents -((C1-C6)-alkyl)-O-(C1 -C6)-alkyl) or -((C1-C6)-alkyl)-S-

((C1-C6)-alkyl), each of which is optionally substituted by 1, 2 or 3 groups R115or

R100is a (C3-C8-cycloalkyl, optionally substituted by 1, 2 or 3 groups R115;

W represents -(CH2)0-4-, -O-, -S(O)0-2, -N(R135)-, -CR(OH)- or-C(O)-;

R102and R102' represent, independently, hydrogen or

(C1-C10)-alkyl, optionally substituted by 1, 2 or 3 groups which are, independently, halogen, aryl or-R110;

R105and R'105represent, independently, -H, -R110, -R120, (C3-C7-cycloalkyl, -((C1-C2)-alkyl)-((C3-C7-cycloalkyl), -((C1-C6)-alkyl))-((C1-C3)-alkyl), (C2-C6)-alkenyl, (C2-C6)-quinil or (C1-C6)-alkyl chain with one double bond and one triple bond, or

(C1-C6)-alkyl, optionally substituted-HE or-NH2; or

(C1-C6)-alkyl, optionally substituted by 1, 2 or 3 groups selected, independently, from halogen, or

R105and R'105together with the atom to which they are attached, form a 3-7-membered carbocyclic ring in which one member is neobyazatel the heteroatom, selected from among-O-, -S(O)0-2- , and-NR135-and the cycle is optionally substituted by 1, 2 or 3 groups selected independently from among the groups R140;

R115in each case represents, independently, halogen, -OH, -CO2R102-(C1-C6)-dialkoxy, -CO2-phenyl, -NR105R'135, -SO2-((C1-C8)-alkyl), -C(=O)R180, R180, -CONR105R'105, -SO2-NR105R'105, -NH-CO-((C1-C6)-alkyl), -NH-C(=O)-OH, -NH-C(=O)-OR, -NH-C(=O)-O-phenyl, -O-C(=O)-((C1-C6)-alkyl), -O-C(=O)amino, -O-C(=O)mono - or dialkylamino, -O-C(=O)phenyl, -O-((C1-C6)-alkyl)-CO2N, -NH-SO2-((C1-C6)-alkyl), (C1-C6)-alkoxy or (C1-C6)-halogenoalkane;

R135is a (C1-C6)-alkyl, (C2-C6)-alkenyl, (C2-C6)-quinil, (C3-C7-cycloalkyl, -(CH2)0-2-aryl, -(CH2)0-2-heteroaryl or -(CH2)0-2-heterocyclyl;

R140represents heterocyclyl, optionally substituted 1, 2, 3 or 4 groups selected, independently, from (C1-C6)-alkyl, (C1-C6)-alkoxy, halogen, hydroxy, cyano, nitro, amino, mono(C1-C6)alkylamino, di(C1-C6)alkylamino, (C2-C6-alkenyl, (C2-C6)-quinil, ( 1-C6)-halogenoalkane,

(C1-C6)-halogenoalkane, amino(C1-C6)alkyl, mono(C1-C6)alkylamino(C1-C6)alkyl,

di(C1-C6)alkylamino(C1-C6)alkyl and =On;

R145is a (C1-C6)-alkyl or CF3;

R150represents hydrogen, (C3-C7-cycloalkyl, -((C1-C2)-alkyl)-((C3-C7-cycloalkyl), (C2-C6)-alkenyl, (C2-C6)-quinil, (C1-C6)-alkyl with one double bond and one triple bond, -R110, -R120or

(C1-C6)-alkyl, optionally substituted by 1, 2, 3 or 4 groups selected, independently, from among-OH, -NH2, (C1-C3)-alkoxy, R110and halogen;

R150' is a (C3-C7-cycloalkyl, -((C1-C3)-alkyl)-((C3-C7-cycloalkyl), (C2-C6)-alkenyl, (C2-C6)-quinil, (C1-C6)-alkyl with one double bond and one triple bond, -R110, -R120or

(C1-C6)-alkyl, optionally substituted by 1, 2, 3 or 4 groups selected, independently, from among-OH, -NH2, (C1-C3)-alkoxy, R110and halogen;

R155is a (C3-C7-cycloalkyl, -((C1-C2)-alkyl)-((C3-C72-C6)-alkenyl, (C2-C6)-quinil, (C1-C6)-alkyl with one double bond and one triple bond, -R110, -R120or

(C1-C6)-alkyl, optionally substituted by 1, 2, 3 or 4 groups selected, independently, from among-OH, -NH2, (C1-C3)-alkoxy and halogen;

R180choose from a number of morpholinyl, thiomorpholine, piperazinil, piperidinyl, homomorpholine, homotaurine, homotaurine-S-oxide, homotaurine-S,S-dioxide, pyrrolidine and pyrrolidinyl, each of which is optionally substituted by 1, 2, 3 or 4 groups selected, independently, from (C1-C6)-alkyl, (C1-C6)-alkoxy, halogen, hydroxy, cyano, nitro, amino, mono(C1-C6)alkylamino, di(C1-C6)alkylamino, (C2-C6-alkenyl, (C2-C6)-quinil, (C1-C6)-halogenoalkane, (C1-C6)-halogenoalkane, amino(C1-C6)-alkyl, mono(C1-C6)alkylamino(C1-C6)alkyl, di(C1-C6)alkylamino

(C1-C6)alkyl and =On;

R110represents aryl, optionally substituted 1 or 2 groups R125;

R125in each case represents, independently, halogen, amino, mono - or dialkylamino, -OH, -C≡N, -SO2-NH2, -SO2-NH-(C1-C )-alkyl, -SO2-N((C1-C6)-alkyl)2, -SO2-((C1-C4)-alkyl), -CO-NH2, -CO-NH-(C1-C6)-alkyl or-CO-N((C1-C6)-alkyl)2or

(C1-C6)-alkyl, (C2-C6)-alkenyl or (C2-C6)-quinil, each of which is optionally substituted by 1, 2 or 3 groups selected, independently, from (C1-C3)-alkyl, halogen, -OH, -SH, -C≡N, -CF3, (C1-C3)-alkoxy, amino, and mono - and dialkylamino, or

(C1-C6)-alkoxy, optionally substituted with one, two or three galactography;

R120is heteroaryl, optionally substituted 1 or 2 groups

R125; and

R130represents heterocyclyl, optionally substituted 1 or 2 groups R125.

The invention also relates to compounds of the formula X

and their pharmaceutically acceptable salts, where in the formula, R1, R2, R3, RNand RChave the meanings specified for formula (I).

The invention also relates to a process for the production of compounds of formula (AA), (I) or (X) compounds of formula (Y)

where R1, R2, R3, RNand RChave the meanings specified for formula (I). The formation of compounds of formula (Y) is connected to the second formula (AA), (I) or (X) may occur in vivo or in vitro. The compounds of formula (Y) is suitable for the treatment and/or prevention of Alzheimer's disease.

The invention also relates to methods for the transformation of compounds of formula AA, I or X in the compounds of formula y-Transformation and/or obtaining compounds of formula Y comprises bringing into contact of the compounds of formulas I and/or X with the aquatic environment. The conversion can occur in vitro or in vivo.

The invention also relates to methods of treating or preventing Alzheimer's disease, moderate cognitive impairment, down's syndrome, hereditary cerebral hemorrhage with amyloidosis (Dutch-Type, cerebral amyloid angiopathy, other degenerative dementias, dementias of mixed vascular and degenerative origin, dementia associated with Parkinson's disease, dementia associated with progressive supranuclear palsy, dementia associated with cortical basal degeneration, Alzheimer's-type diffusion Taurus levy, including the introduction of a patient in need, a therapeutically effective amount of the compounds of formula AA, I or X or its salts.

Preferably the patient is a man.

Preferably the disease is an Alzheimer's disease.

Preferably the disease is a dementia.

The invention targetnode to pharmaceutical compositions, containing the compound of formula AA, I or X or its salt and at least one pharmaceutically acceptable carrier, solvent, adjuvant or diluent.

The invention also relates to the use of compounds of formula AA, I or X or its salt to obtain the drug.

The invention also relates to the use of compounds of formula (AA), (I) or (X) for treating or preventing Alzheimer's disease, moderate cognitive impairment, down's syndrome, hereditary cerebral hemorrhage with amyloidosis (Dutch-Type, cerebral amyloid angiopathy, other degenerative dementias, dementias of mixed vascular and degenerative origin, dementia associated with Parkinson's disease, dementia associated with progressive supranuclear palsy, dementia associated with cortical basal degeneration or Alzheimer's-type diffusion Taurus Levi.

The invention also relates to compounds, pharmaceutical compositions, kits and methods of inhibition mediated beta-secretases cleavage of amyloid protein precursor (APP). More specifically, the compounds, compositions and methods of the invention are effective for inhibiting the production of peptide A-beta for the treatment or prevention of any disease or condition of a person or animal that is associated with PA the ideological form of the peptide A-beta.

The invention also relates to methods of preparing compounds of the invention and intermediate compounds used in these methods.

Compounds, compositions and methods of the invention are suitable for the treatment of people with Alzheimer's disease (AD), to promote the prevention or delay the occurrence of AD, for treating patients with mild cognitive impairment (MCI) and preventing or delaying the occurrence of AD in these patients, which otherwise can be expected progression from MCI to AD, for treating down's syndrome, for the treatment of hereditary cerebral hemorrhage with amyloidosis (Dutch-Type, for treating cerebral beta-amyloid angiopathy and preventing its potential consequences, such as single and recurring lobes hemorrhages, for treating other degenerative dementias, including dementias of mixed vascular and degenerative origin, for the treatment of dementia associated with Parkinson's disease, dementia associated with progressive supranuclear palsy, dementia associated with cortical basal degeneration, and AD-type diffusion Taurus Levi, and for the treatment of fronto-temporal dementia with parkinsonism (FTDP).

The compounds of formula Y have activity of inhibiting beta-secretase. Inhibiting activity of the compounds of the invention are easily demonstrated on the example, using one or more assays described herein or known in the art.

If the substituents for formula not defined specifically for this formula, we mean that they have the definitions stated in connection with the previous formula, which is given reference.

Detailed description of the invention

As noted above, the invention relates to compounds of formula (AA), (I) and (X), suitable for the treatment and prevention of Alzheimer's disease. These compounds can be considered as prodrugs of the active compounds of the formula Y, as they form such active compound in vivo and in vitro.

Compounds of formula AA, I and X are undergoing migration of the acyl group RNupon contact with water, as shown in scheme I. the Migration related to compounds of formula (I), herein referred to as "N-acyl migration". Migration-related compounds of formula (X), in this description referred to as "O-acyl migration.

Migration, shown in figure 1, can occur either in vitro or in vivo and occur when the compound is introduced into contact with the water environment, including the water. Water environment can be neutral, acidic or alkaline. Preferably, the medium had a pH of from about 2 to about 10, preferably from about 3 to p is IMEMO 7. The amount of water required for migration is not a critical parameter. A catalytic amount of aqueous medium is sufficient to cause migration. Aqueous buffer solutions and gastric fluid are good environments for migration occurred.

Products rearrangements of compounds of formula AA, of the formula I and/or formula X are compounds of formula (Y). The substituents R1, R2, R3, RNand RCin the compounds of formula (Y) have the values specified above for compounds of formula (I).

Scheme 1

Preferred compounds of formula AA are the compounds of formula AA-1, i.e. the compounds of formula AA where

R1represents aryl, heteroaryl, heterocyclyl -(C1-C6-alkylaryl -(C1-C6-alkylglycerol or -(C1-C6)-Alkylglucoside, where the cyclical part of each substituent optionally substituted by 1, 2, 3 or 4 groups selected, independently, from halogen, -OH, -SH, -C≡N, -NO2, -NR105R'105, -CO2R, -N(R)COR', or-N(R)SO2R', -C(=O)-(C1-C4)-alkyl, -SO2-amino, -SO2-mono - or-dialkylamino, -C(=O)-amino, -C(=O)-mono - or-dialkylamino, -SO2-(C1-C4)-alkyl, or

(C1-C6)-Ala is XI, optionally substituted by 1, 2 or 3 groups selected, independently, from halogen, or

(C3-C7-cycloalkyl, optionally substituted by 1, 2 or 3 groups selected, independently, from halogen, -OH, -SH, -C≡N, -CF3, (C1-C3)-alkoxy, amino, -(C1-C6)-alkyl and mono - or dialkylamino, or

(C1-C10)-alkyl, optionally substituted by 1, 2 or 3 groups selected, independently, from halogen, -OH, -SH, -C≡N, -CF3, (C1-C3)-alkoxy, amino, mono - or dialkylamino and -(C1-C3)-alkyl, or

(C2-C10)-alkenyl or (C2-C10)-quinil, each of which is optionally substituted by 1, 2 or 3 groups selected, independently, from halogen, -OH, -SH, -C≡N, -CF3, (C1-C3)-alkoxy, amino, (C1-C6)-alkyl and mono - or dialkylamino; and heterocyclyl the group is also optionally substituted by oxo.

Preferred compounds of formula AA-1 are also connections

R1represents -(C1-C6-alkylaryl -(C1-C6-alkylglycerol or -(C1-C6)-Alkylglucoside, where the cyclical part of each substituent optionally substituted by 1, 2, 3 or 4 groups selected, independently, from halogen, -OH, -SH, -C≡N, -NO2, -NR105R'105, -CO2R, -N(R)COR' what if-N(R)SO 2R', -C(=O)-(C1-C4)-alkyl, -SO2-amino, -SO2-mono - or-dialkylamino, -C(=O)-amino, -C(=O)-mono - or-dialkylamino, -SO2-(C1-C4)-alkyl, or

(C1-C6)-alkoxy, optionally substituted by 1, 2 or 3 groups selected, independently, from halogen, or

(C3-C7-cycloalkyl, optionally substituted by 1, 2 or 3 groups selected, independently, from halogen, -OH, -SH, -C≡N, -CF3, (C1-C3)-alkoxy, amino, -(C1-C6)-alkyl and mono - or dialkylamino, or

(C1-C10)-alkyl, optionally substituted by 1, 2 or 3 groups selected, independently, from halogen, -OH, -SH, -C≡N, -CF3, (C1-C3)-alkoxy, amino, mono - or dialkylamino and -(C1-C3)-alkyl, or

(C2-C10)-alkenyl or (C2-C10)-quinil, each of which is optionally substituted by 1, 2 or 3 groups selected, independently, from halogen, -OH, -SH, -C≡N, -CF3, (C1-C3)-alkoxy, amino, (C1-C6)-alkyl and mono - or dialkylamino; and heterocyclyl the group is also optionally substituted by oxo.

Preferred compounds of formula AA-1 are also connections

R1represents -(CH2)-aryl, -(CH2-heteroaryl or -(CH2)-heterocyclyl, where the cyclic portion of each is the first Deputy optionally substituted 1, 2, 3, or 4 groups selected, independently, from halogen, -OH, -SH, -C≡N, -NO2, -NR105

R'105, -CO2R, -N(R)COR', or-N(R)SO2R', -C(=O)-(C1-C4)-alkyl, -SO2-amino, -SO2-mono - or-dialkylamino, -C(=O)-amino, -C(=O)-mono - or-dialkylamino, -SO2-(C1-C4)-alkyl, or

(C1-C6)-alkoxy, optionally substituted by 1, 2 or 3 groups selected, independently, from halogen, or

(C3-C7-cycloalkyl, optionally substituted by 1, 2 or 3 groups selected, independently, from halogen, -OH, -SH, -C≡N, -CF3, (C1-C3)-alkoxy, amino, -(C1-C6)-alkyl and mono - or dialkylamino, or

(C1-C10)-alkyl, optionally substituted by 1, 2 or 3 groups selected, independently, from halogen, -OH, -SH, -C≡N, -CF3, (C1-C3)-alkoxy, amino, mono - or dialkylamino and -(C1-C3)-alkyl, or

(C2-C10)-alkenyl or (C2-C10)-quinil, each of which is optionally substituted by 1, 2 or 3 groups selected, independently, from halogen, -OH, -SH, -C≡N, -CF3, (C1-C3)-alkoxy, amino, (C1-C6)-alkyl and mono - or dialkylamino; and heterocyclyl the group is also optionally substituted by oxo.

Preferred compounds of formula AA-1 are also connections to the verge

R1represents-CH2-phenyl or-CH2-pyridinyl, where the cyclical part of each substituent optionally substituted by 1, 2, 3 or 4 groups selected, independently, from halogen, (C1-C4)-alkoxy, hydroxy, -NO2and

(C1-C4)-alkyl, optionally substituted by 1, 2 or 3 substituents selected, independently, from halogen, HE, SH, NH2, NH((C1-C6)-alkyl), N-((C1-C6)-alkyl)((C1-C6)-alkyl, -C≡N, -CF3.

Preferred compounds of formula AA-1 are also connections

R1represents-CH2-phenyl or-CH2-pyridinyl where the phenyl or pyridinoline parts, each optionally substituted by 1 or 2 groups selected, independently, from halogen, (C1-C2)-alkyl, (C1-C2)-alkoxy, hydroxy, -CF3and-NO2.

Preferred compounds of formula AA-1 are compounds in which

R1represents-CH2-phenyl, where the phenyl portion is optional substituted 2 groups selected, independently, from halogen, (C1-C2)-alkyl, (C1-C2)-alkoxy, hydroxy, and-NO2.

Preferred compounds of formula AA-1 are also compounds in which R1represents benzyl or 3,5-gifthorse the ZIL.

Preferred compounds of formula AA and AA-1 are the compounds of formula AA-2, i.e. compounds of formula AA or AA-1, in which

R2and R3chosen, independently, from the group consisting of H or (C1-C6)-alkyl, optionally substituted by 1, 2 or 3 substituents selected from the group consisting of (C1-C3)-alkyl, halogen, -OH, -SH, -C≡N, -CF3, (C1-C3)-alkoxy and

-NR1-aR1-b.

Preferred compounds of formula AA-2 are compounds in which

Rwithselected from the group consisting of (C1-C10)-alkyl, optionally substituted by 1, 2 or 3 groups selected, independently, from the group consisting of

R205, -OC=ONR235R240, -S(=O)0-2((C1-C6)-alkyl), -SH, -NR235C=ONR235R240, -C=ONR235R240and-S(=O)2NR235R240; -(CH2)0-3-(C3-C8)-cycloalkyl where cycloalkyl optionally substituted by 1, 2 or 3 groups selected, independently, from the group consisting of R205, -CO2H and CO2-((C1-C4)-alkyl); -(CR245R250)0-4-aryl;

-(CR245R250)0-4-heteroaryl; -(CR245R250)0-4-geterotsiklicheskie; -[C(R255)(R260)]1-3-CO-N(R255)2; -CH(aryl)2; -CH(heteroaryl)2; -CH(heterocyclic is) 2; -CH(aryl)(heteroaryl); -CO-NR235R240; -(CH2)0-1-CH((CH2)0-6-OH)-(CH2)0-1-aryl; -(CH2)0-1-CHRS-6-(CH2)0-1-heteroaryl; -CH(-aryl or-heteroaryl)-CO-O((C1-C4)-alkyl); -CH(-CH2-OH)-CH(OH)-phenyl-NO2; ((C1-C6)-alkyl)-O-((C1-C6)-alkyl) -;- CH2-NH-CH2-CH(-O-CH2-CH3)2; -N and -(CH2)0-6-C(=NR235)(NR235R240); where

each aryl optionally substituted by 1, 2 or 3 R200;

each heteroaryl optionally substituted by 1, 2, 3 or 4 R200;

each heteroseksualci optionally substituted by 1, 2, 3 or 4 R210;

R200in each case chosen, independently, from the group consisting of (C1-C6)-alkyl, optionally substituted by 1, 2 or 3 groups R205; HE; -NO2; halogen; -CO2N; C≡N; -(CH2)0-4-CO-NR220R225; -(CH2)0-4-CO-((C1-C12)-alkyl);

-(CH2)0-4-CO2R215and -(CH2)0-4-O-((C1-C6)-alkyl, optionally substituted by 1, 2, 3, or 5-F);

where each aryl group in each case is optionally substituted by 1, 2, or 3 groups that represent, independently, R205, R210or (C1-C6)-alkyl, substituted 1, 2, or 3 groups that represent what they themselves independently, R205or R210;

where each heterocytolysine group in each case is optionally substituted by 1, 2, or 3 groups that represent, independently, R210;

where each heteroaryl group in each case is optionally substituted by 1, 2, or 3 groups that represent, independently, R205, R210or (C1-C6)-alkyl, substituted 1, 2, or 3 groups that represent, independently, R205or R210;

R205in each case chosen, independently, from the group consisting of (C1-C6)-alkyl, halogen, -OH, -O-phenyl, -SH, -C≡N, -CF3, (C1-C6)-alkoxy, NH2,

NH((C1-C6)-alkyl) and N((C1-C6)-alkyl)((C1-C6)-alkyl);

R210in each case chosen, independently, from the group consisting of (C1-C6)-alkyl, optionally substituted by 1, 2 or 3 groups R205; halogen; (C1-C6)-alkoxy, (C1-C6)-halogenoalkane; -NR220R225; OH; C≡N; and (C3-C7)-cycloalkyl, optionally substituted by 1, 2 or 3 groups R205; -CO-((C1-C4)-alkyl);

-SO2-NR235R240; -CO-NR235R240; -SO2-((C1-C4)-alkyl) and =O, where

R215in each case chosen, independently, from the group consisting of (C1 -C6)-alkyl, (CH2)0-2-aryl, (C3-C7)-cycloalkyl, (CH2)0-2-heteroaryl and (CH2)0-2-geterotsiklicheskie, where the aryl group in each case is optionally substituted by 1, 2, or 3 groups that represent, independently, R205or R210; where heterocytolysine group in each case is optionally substituted by 1, 2 or 3 R210; where each heteroaryl group in each case is optionally substituted by 1, 2 or 3 R210;

R220and R225in each case chosen, independently, from the group consisting of-H,

-(C1-C6)-alkyl, hydroxy-(C1-C6)-alkyl, amino-(C1-C6)-alkyl, halogen-(C1-C6)-alkyl, (C3-C7)-cycloalkyl, -((C1-C6)-alkyl)-O-((C1-C3)-alkyl), -aryl, -heteroaryl and-geterotsiklicheskie, where the aryl group in each case is optionally substituted by 1, 2 or 3 groups R270each heteroaryl is optionally substituted by 1, 2, 3 or 4 R200each heteroseksualci is optionally substituted by 1, 2, 3 or 4 R210where

R270in each case represents, independently, R205, (C1-C6)-alkyl, optionally substituted by 1, 2 or 3 groups R205; halogen; (C1-C6)-alkoxy (C 1-C6)-halogenoalkane; NR235R240; OH; C≡N; -CO-((C1-C4)-alkyl) and =O, where heterocytolysine group in each case is optionally substituted by 1, 2 or 3 groups R205; where each heteroaryl group in each case is optionally substituted by 1, 2 or 3 groups R205;

R235and R240in each case represent, independently, H or (C1-C6)-alkyl;

R245and R250in each case chosen, independently, from the group consisting of H, (C1-C4)-alkyl, (C1-C4)-hydroxyalkyl, (C1-C4)-alkoxy, (C1-C4)-halogenoalkane, or

R245and R250taken together with the carbon atom to which they are attached, to form carbocycle of 3, 4, 5, 6 or 7 carbon atoms, where carbocycle optionally substituted 1 or 2 groups that represent, independently, HE, methyl, Cl, F, och3, CF3, NO2or CN;

R255and R260in each case chosen, independently, from the group consisting of H; and (C1-C6)-alkyl, optionally substituted by 1, 2 or 3 groups R205; -(CH2)0-4-(C3-C7)-cycloalkyl, optionally substituted by 1, 2 or 3 groups R205; -((C1-C4)-alkyl)aryl; -((C1-C4)-alkyl)heteroaryl; -((C1-C4)-alkyl)het is of recycleable; aryl; heteroaryl; geterotsiklicheskie; -(CH2)1-4-R265-(CH2)0-4-aryl; -(CH2)1-4-R265-(CH2)0-4-heteroaryl and -(CH2)1-4-R265-(CH2)0-4-geterotsiklicheskie; where

R265in each case represents, independently, -O-, -S - or-N((C1-C6)-alkyl)-;

each aryl or phenyl optionally substituted by 1, 2, or 3 groups that represent, independently, R205, R210or (C1-C6)-alkyl, substituted 1, 2, or 3 groups that represent, independently, R205or R210.

Preferred compounds of formula AA-2 are compounds in which

Rwithrepresents -(CR245R250)0-4-aryl or -(CR245R250)0-4-heteroaryl, where aryl and heteroaryl optionally substituted by 1, 2 or 3 groups R200.

Preferred compounds of formula AA-2 are also connections

Rwithrepresents -(CR245R250)-aryl or -(CR245R250-heteroaryl, where each aryl and heteroaryl optionally substituted by 1, 2 or 3 groups R200.

Preferred compounds of formula AA-2 are also connections

Rwithrepresents -(CH2)-aryl or -(CH2-heteroaryl, where each aryl and heteroaryl optional what about the substituted 1, 2 or 3 groups selected from HE, " NO2, halogen, -CO2N, C≡N, -(CH2)0-4-CO-NR220R225, -(CH2)0-4-CO-((C1-C12)-alkyl) and -(CH2)0-4-SO2-NR220R225.

Preferred compounds of formula AA-2 are also connections

Rwithrepresents -(CH2)-aryl, where aryl optionally substituted by 1, 2 or 3 groups selected from HE, " NO2, halogen, -CO2N and C≡N.

Preferred compounds of formula AA-2 are also connections

Rwithrepresents -(CH2)-phenyl, where phenyl optionally substituted by 1, 2 or 3 groups selected from HE, " NO2, halogen, -CO2N and C≡N.

Preferred compounds of formula AA-2 are also compounds in which Rwithrepresents benzyl.

Other preferred compounds of formula AA, AA-1 and AA-2 are the compounds of formula AA-3, i.e. compounds of formula AA, AA-1 and AA-2, in which

one of RNand RN' represents hydrogen and the other represents a

where

R4represents NH2, -NH-(CH2)n6-R4-1-The other8, -NR50C(O)R5or-NR50CO2R51,

where

n6is 0, 1, 2 or 3;

n7is 0, 1, 2 is 3;

R4-1selected from the group consisting of-SO2-((C1-C8)-alkyl), -SO-((C1-C8)-alkyl), -S-((C1-C8)-alkyl), -S-CO-((C1-C6)-alkyl), -SO2-NR4-2R4-3; -CO-(C1-C2)-alkyl, -CO-NR4-3R4-4;

R4-2and R4-3represent, independently, H, (C1-C3)-alkyl or (C3-C6-cycloalkyl;

R4-4represents alkyl, phenylalkyl, (C2-C4-alkanoyl or phenylalkanoic;

R5is cyclopropyl, cyclobutyl, cyclopentyl and cyclohexyl, where each cycloalkyl group optionally substituted by one or two groups representing a (C1-C6)-alkyl, preferably - (C1-C2)-alkyl, (C1-C6)-alkoxy, preferably - (C1-C2)-alkoxy, CF3, OH, NH2, NH((C1-C6)-alkyl), N((C1-C6)-alkyl)((C1-C6)-alkyl), halogen, CN or NO2; or cycloalkyl group substituted by 1 or 2 groups that represent, independently, CF3, Cl, F, methyl, ethyl or cyano; (C1-C6)-alkyl, optionally substituted by 1, 2 or 3 groups which are, independently, halogen,

-NR6R7, (C1-C4)-alkoxy, (C5-C6-heteroseksualci, (C5-C6-heteroaryl, Fe is Il, (C3-C7-cycloalkyl, -S-(C1-C4)-alkyl, -SO2-(C1-C4)-alkyl, -CO2N, -CONR6R7, -CO2-(C1-C4)-alkyl or phenyloxy; heteroaryl, optionally substituted by 1, 2 or 3 groups which are, independently, (C1-C4)-alkyl, (C1-C4)-alkoxy, halogen, (C1-C4-halogenated or HE; heteroseksualci, optionally substituted by 1, 2 or 3 groups which are, independently, (C1-C4)-alkyl, (C1-C4)-alkoxy, halogen or (C2-C4-alkanoyl; phenyl, optionally substituted by 1, 2, 3, or 4 groups that represent, independently, halogen, HE, (C1-C4)-alkyl, (C1-C4)-alkoxy or (C1-C4-halogenated; and-NR6R7; where

R6and R7chosen, independently, from the group consisting of H, (C1-C6)-alkyl, (C2-C6)-alkanoyl, phenyl, -SO2-(C1-C4)-alkyl and phenyl-(C1-C4)-alkyl;

R8selected from the group consisting of-SO2-heteroaryl, optionally substituted 1 or 2 groups that represent, independently, (C1-C4)-alkyl or halogen; -SO2-aryl, -SO2-geterotsiklicheskie, -C(O)other9, geterotsiklicheskie, -S-(C2-C4)-alkanoyl, where

R9depict is to place a phenyl-(C 1-C4)-alkyl, (C1-C6)-alkyl or H;

R50represents H or (C1-C6)-alkyl;

R51selected from the group consisting of phenyl-(C1-C4)-alkyl, (C1-C6)-alkyl, optionally substituted by 1, 2 or 3 groups which are, independently, halogen, cyano, -NR6R7-C(O)NR6R7, (C3-C7-cycloalkyl or -(C1-C4)-alkoxy; geterotsiklicheskie, optionally substituted 1 or 2 groups that represent, independently, (C1-C4)-alkyl, (C1-C4)-alkoxy, halogen, (C2-C4-alkanoyl, phenyl-

(C1-C4)-alkyl and-SO2-(C1-C4)-alkyl; geterotsiklicheskikh, optionally substituted 1 or 2 groups that represent, independently, (C1-C4)-alkyl,

(C1-C4)-alkoxy, halogen, (C2-C4-alkanoyl, phenyl-(C1-C4)-alkyl and-SO2-(C1-C4)-alkyl; alkenyl; quinil; heteroaryl, optionally substituted 1, 2, or 3 groups that represent, independently, HE, (C1-C4)-alkyl, (C1-C4)-alkoxy, halogen, NH2, NH(C1-C6)-alkyl or N((C1-C6)-alkyl)((C1-C6)-alkyl); heteroaromatic, optionally substituted 1, 2, or 3 groups that represent what they themselves independently, (C1-C4)-alkyl, (C1-C4)-alkoxy, halogen, NH2, NH(C1-C6)-alkyl or N((C1-

With6)-alkyl)((C1-C6)-alkyl); phenyl; and (C3-C8)cycloalkyl and cycloalkenyl, where phenyl, (C3-C8)cycloalkyl and cycloalkenyl group substituted by optionally 1, 2, 3, 4, or 5 groups that represent, independently, halogen, CN, NO2, (C1-C6)-alkyl, (C1-C6)-alkoxy, (C2-C6-alkanoyl, (C1-C6-halogenated, (C1-C6)-halogenoalkane, hydroxy, (C1-C6-hydroxyalkyl, (C1-C6)-alkoxy-(C1-C6)-alkyl, (C1-C6)-dialkoxy, (C1-C6)-dialkoxy-(C1-C6)-alkyl or (C1-C6)-alkoxy-(C1-C6)-alkoxy.

Preferred compounds of formula AA-3 are compounds in which

one of RNand RN' represents hydrogen and the other represents a

where

X is a (C1-C4)-alkylidene, optionally substituted by 1, 2 or 3 methyl groups, or-NR4-6; or

R4and R4-6combined with education -(CH2)n10-where

n10is 1, 2, 3 or 4;

Z is chosen from among communication, SO2SO, S IS C(O);

Y is chosen from among N, (C1-C4)-halogenoalkane; and (C5-C6)-geterotsiklicheskie containing at least one N, O or S; phenyl; HE; -N(Y1)(Y2); And (C1-C10)-alkyl, optionally substituted by 1-3 substituents, which may be the same or different and are selected from among halogen, hydroxy, alkoxy, dialkoxy, halogenoalkane; and (C3-C8)-cycloalkyl, optionally substituted by 1, 2 or 3 groups selected, independently, from (C1-C3)-alkyl and halogen; alkoxy; phenyl, optionally substituted with halogen, (C1-C4)-alkyl, (C1-C4)-alkoxy, CN or NO2; phenyl-(C1-C4)-alkyl, optionally substituted with halogen, (C1-C4)-alkyl, (C1-C4)-alkoxy, CN or NO2; where

Y1and Y2are the same or different and represent H; and (C1-C10)-alkyl, optionally substituted by 1, 2 or 3 substituents selected from the group consisting of halogen, (C1-C4)-alkoxy, (C3-C8)-cycloalkyl and IT; and (C2-C6)-alkenyl; and (C2-C6-alkanoyl; phenyl; -SO2-(C1-C4)-alkyl; phenyl-(C1-C4)-alkyl and (C3-C8-cycloalkyl-(C1-C4)-alkyl; or

-N(Y1)(Y2) to form a cycle selected from a number of the and piperazinil, piperidinyl, morpholinyl and pyrrolidinyl, where each cycle is optionally substituted by 1, 2, 3, or 4 groups that represent, independently, (C1-C6)-alkyl, (C1-C6)-alkoxy, (C1-C6)-alkoxy-(C1-C6)-alkyl or halogen.

Preferred compounds of formula AA-3 are compounds in which

X is a (C1-C4)-alkylidene, optionally substituted by 1, 2 or 3 methyl groups;

Z is chosen from among SO2SO, S and S(Oh);

Y is chosen from among N, (C1-C4)-halogenoalkane; and (C5-C6)-geterotsiklicheskie containing at least one N, O or S; phenyl; HE; -N(Y1)(Y2); And (C1-C10)-alkyl, optionally substituted by 1-3 substituents, which may be the same or different and are selected from the group consisting of halogen, hydroxy, alkoxy, dialkoxy, halogenoalkane; and (C3-C8)-cycloalkyl, optionally substituted by 1, 2 or 3 groups selected, independently, from (C1-C3)-alkyl and halogen; alkoxy; phenyl, optionally substituted with halogen, (C1-C4)-alkyl,

(C1-C4)-alkoxy, CN or NO2; phenyl-(C1-C4)-alkyl, optionally substituted with halogen, (C1-C4)-alkyl, (C1-C4)-alkoxy, CN or NO2; where

Y 1and Y2are the same or different and represent H; and (C1-C6)-alkyl, optionally substituted by 1, 2 or 3 substituents selected from the group consisting of halogen, (C1-C4)-alkoxy, (C3-C8)-cycloalkyl and IT; and (C2-C6)-alkenyl; and (C2-C6-alkanoyl; phenyl; -SO2-(C1-C4)-alkyl; phenyl-(C1-C4)-alkyl or (C3-C8-cycloalkyl-(C1-C4)-alkyl; or

-N(Y1)(Y2) to form a cycle selected from the piperazinil, piperidinyl, morpholinyl and pyrrolidinyl, where each cycle is optionally substituted by 1, 2, 3, or 4 groups that represent, independently, (C1-C6)-alkyl, (C1-C6)-alkoxy, (C1-C6)-alkoxy-(C1-C6)-alkyl or halogen.

Preferred compounds of formula AA-3 are compounds in which one of RNand RN' represents hydrogen and the other represents a

where R4represents NH2, -NH-(CH2)n6-R4-1-The other8, -NR50C(O)R5or-NR50CO2R51where

n6is 0, 1, 2 or 3;

n7is 0, 1, 2 or 3;

R4-1selected from the group consisting of-SO2-((C1-C8)-alkyl), -SO-((C1-C8)-alkyl), -S-((C1 -C8)-alkyl), -S-CO-((C1-C6)-alkyl), -SO2-NR4-2R4-3; -CO-(C1-C2)-alkyl, -CO-NR4-3R4-4;

R4-2and R4-3represent, independently, H, (C1-C3)-alkyl or (C3-C6-cycloalkyl;

R4-4represents alkyl, phenylalkyl, (C2-C4-alkanoyl or phenylalkanoic;

R5is cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl, where each cycloalkyl group optionally substituted by one or two groups representing a (C1-C6)-alkyl, preferably - (C1-C2)-alkyl, (C1-C6)-alkoxy, preferably - (C1-C2)-alkoxy, CF3, OH, NH2, NH((C1-C6)-alkyl), N((C1-C6)-alkyl)((C1-C6)-alkyl), halogen, CN or NO2; or cycloalkyl group substituted by 1 or 2 groups that represent, independently, CF3, Cl, F, methyl, ethyl or cyano; (C1-C6)-alkyl, optionally substituted by 1, 2 or 3 groups which are, independently, halogen,

-NR6R7, (C1-C4)-alkoxy, (C5-C6-heteroseksualci, (C5-C6-heteroaryl, phenyl, (C3-C7-cycloalkyl, -S-(C1-C4)-alkyl, -SO2-(C1-C4)-alkyl, -CO2N, -CONR6R , -CO2-(C1-C4)-alkyl or phenyloxy; heteroaryl, optionally substituted by 1, 2 or 3 groups which are, independently, (C1-C4)-alkyl, (C1-C4)-alkoxy, halogen, (C1-C4-halogenated or HE; heteroseksualci, optionally substituted by 1, 2 or 3 groups which are, independently, (C1-C4)-alkyl, (C1-C4)-alkoxy, halogen or (C2-C4-alkanoyl; phenyl, optionally substituted by 1, 2, 3, or 4 groups that represent, independently, halogen, HE, (C1-C4)-alkyl, (C1-C4)-alkoxy or (C1-C4-halogenated; and-NR6R7; where

R6and R7chosen, independently, from the group consisting of H, (C1-C6)-alkyl, (C2-C6)-alkanoyl, phenyl, -SO2-(C1-C4)-alkyl and phenyl-(C1-C4)-alkyl;

R8selected from the group consisting of-SO2-heteroaryl, optionally substituted 1 or 2 groups that represent, independently, (C1-C4)-alkyl or halogen; -SO2-aryl, -SO2-geterotsiklicheskie, -C(O)other9, geterotsiklicheskie, -S-(C2-C4)-alkanoyl, where

R9represents phenyl-(C1-C4)-alkyl, (C1-C6)-alkyl or H;

R50represents H or (C1-the 6)-alkyl; and

R51selected from the group consisting of phenyl-(C1-C4)-alkyl, (C1-C6)-alkyl, optionally substituted by 1, 2 or 3 groups which are, independently, halogen, cyano, -NR6R7-C(O)NR6R7, (C3-C7-cycloalkyl or -(C1-C4)-alkoxy; geterotsiklicheskie, optionally substituted 1 or 2 groups that represent, independently, (C1-C4)-alkyl, (C1-C4)-alkoxy, halogen, (C2-C4-alkanoyl, phenyl-

(C1-C4)-alkyl and-SO2-(C1-C4)-alkyl; geterotsiklicheskikh, optionally substituted 1 or 2 groups that represent, independently, (C1-C4)-alkyl,

(C1-C4)-alkoxy, halogen, (C2-C4-alkanoyl, phenyl-(C1-C4)-alkyl and-SO2-(C1-C4)-alkyl; alkenyl; quinil; heteroaryl, optionally substituted 1, 2, or 3 groups that represent, independently, HE, (C1-C4)-alkyl, (C1-C4)-alkoxy, halogen, NH2, NH(C1-C6)-alkyl or N((C1-C6)-alkyl)((C1-C6)-alkyl); heteroaromatic, optionally substituted by 1, 2 or 3 groups which are, independently, (C1-C4)-alkyl, (C1-C4)-alkoxy, halogen, NH2, NH(C1 -C6)-alkyl or N((C1-

With6)-alkyl)((C1-C6)-alkyl); phenyl; and (C3-C8)cycloalkyl and cycloalkenyl, where phenyl, (C3-C8)cycloalkyl and cycloalkenyl group substituted by optionally 1, 2, 3, 4, or 5 groups that represent, independently, halogen, CN, NO2, (C1-C6)-alkyl, (C1-C6)-alkoxy, (C2-C6-alkanoyl, (C1-C6-halogenated, (C1-C6)-halogenoalkane, hydroxy, (C1-C6-hydroxyalkyl, (C1-C6)-alkoxy-(C1-C6)-alkyl, (C1-C6)-dialkoxy, (C1-C6)-dialkoxy-(C1-C6)-alkyl or (C1-C6)-alkoxy-(C1-C6)-alkoxy; and

Y represents a (C1-C10)-alkyl, optionally substituted by 1-3 substituents, which may be the same or different and are selected from among halogen, hydroxy, alkoxy, dialkoxy, halogenoalkane.

Preferred compounds of formula AA-3 are also connections

Rwithis a (C1-C8)-alkyl, optionally substituted by 1, 2 or 3 groups selected, independently, from the group consisting of R205, -OC=ONR235R240, -S(=O)0-2((C1-C6)-alkyl), -SH, -C=ONR235R240and-S(=O)2NR235R240; -(The h 2)0-3-(C3-C8-cycloalkyl where cycloalkyl optionally substituted by 1, 2 or 3 groups selected, independently, from the group consisting of R205, -CO2H and CO2-((C1-C4)-alkyl); -(CR245R250)0-4-phenyl; -(CR245R250)0-4-heteroaryl;

-(CR245R250)0-4-heteroseksualci; -(CH2)0-1-CH((CH2)0-4-OH)-(CH2)0-1-phenyl; -(CH2)0-1-CHRS-6-(CH2)0-1-heteroaryl; -CH(-CH2-OH)-CH(OH)-phenyl-NO2; ((C1-C6)-alkyl)-O-((C1-C6)-alkyl)-or -(CH2)0-6-C(=NR235)(NR235R240); where

each aryl optionally substituted by 1, 2 or 3 R200;

each heteroaryl optionally substituted by 1, 2, 3 or 4 R200;

each heteroseksualci optionally substituted by 1, 2, 3 or 4 R210;

R200in each case represents, independently, (C1-C6)-alkyl, optionally substituted by 1, 2 or 3 groups R205; HE; -NO2; halogen; -CO2N; C≡N; -(CH2)0-4-CO-NR220R225; -(CH2)0-4-CO-((C1-C12)-alkyl); -(CH2)0-4-CO2R215or -(CH2)0-4-O-((C1-C6)-alkyl, optionally substituted by 1, 2, 3, or 5-F);

R205in each case represents, independently, (C -C6)-alkyl, halogen, -OH, -O-phenyl, -SH, -C≡N, -CF3, (C1-C6)-alkoxy, NH2, NH((C1-C6)-alkyl) or N((C1-C6)-alkyl)((C1-C6)-alkyl);

R210in each case represents, independently, (C1-C6)-alkyl, optionally substituted by 1, 2 or 3 groups R205; halogen; (C1-C6)-alkoxy, (C1-C6)-halogenoalkane; -NR220R225; OH; C≡N; and (C3-C7-cycloalkyl, optionally substituted by 1, 2 or 3 groups R205; -CO-((C1-C4)-alkyl); -SO2-NR235R240; -CO-NR235R240; -SO2-((C1-C4)-alkyl) and =O, where

R215in each case represents, independently, (C1-C6)-alkyl, (CH2)0-2-phenyl, (C3-C7-cycloalkyl, (CH2)0-2-heteroaryl and (CH2)0-2-heteroseksualci, where the phenyl group in each case is optionally substituted by 1, 2, or 3 groups that represent, independently, R205or R210; where heterocytolysine group in each case is optionally substituted by 1, 2 or 3 R210; where each heteroaryl group in each case is optionally substituted by 1, 2 or 3 R210;

R220and R225in each case represent, independently, -H, -(C1-C6)-Alki is, hydroxy-(C1-C6)-alkyl, halogen-(C1-C6)-alkyl, -(C3-C7-cycloalkyl and((C1-C6)-alkyl)-O-((C1-C3)-alkyl);

R235and R240in each case represent, independently, H or (C1-C6)-alkyl;

R245and R250in each case represent, independently, H, (C1-C4)-alkyl, (C1-C4-hydroxyalkyl, (C1-C4)-alkoxy, (C1-C4)-halogenoalkane, or

R245and R250taken together with the carbon atom to which they are attached, form carbocycle of 3, 4, 5, 6 or 7 carbon atoms.

Preferred compounds of formula AA-3 are also connections

R1represents benzyl, optionally substituted by 1, 2, 3 or 4 groups selected, independently, from halogen, (C1-C4)-alkoxy, hydroxy and (C1-C4)-alkyl, optionally substituted by 1, 2 or 3 substituents from halogen, HE, SH, NH2, NH((C1-C6)-alkyl), N((C1-C6)-alkyl)((C1-C6)-alkyl), C≡N, CF3;

R2and R3chosen, independently, from H or (C1-C4)-alkyl, optionally substituted by 1 Deputy, selected from among halogen, -OH, -SH, -C≡N, -CF3, (C1-C3)-alkoxy, NH2, NH((C1-C6)-is Lila) and N((C 1-C6)-alkyl)((C1-C6)-alkyl);

Rwithis a (C1-C8)-alkyl, optionally substituted by 1, 2 or 3 groups selected, independently, from the group consisting of R205, -SH, -C=ONR235

R240and-S(=O)2NR235R240; -(CH2)0-3-(C3-C6-cycloalkyl where cycloalkyl optionally substituted by 1, 2 or 3 groups selected, independently, from among the R205, -CO2H and CO2-((C1-C4)-alkyl); -(CR245R250)0-4is phenyl, optionally substituted by 1, 2 or 3 R200; -(CR245R250)0-3-pyridyl; -(CR245R250)0-3-pyridazinyl; -(CR245R250)0-3-pyrimidinyl; -(CR245R250)0-3-pyrazinyl; -(CR245R250)0-3-furyl;

-(CR245R250)0-3-indolyl; -(CR245R250)0-3-thienyl; -(CR245R250)0-3-pyrrolyl; -(CR245R250)0-3-pyrazolyl; -(CR245R250)0-3-benzoxazolyl; -(CR245R250)0-3-imidazolyl; each of the above heteroaryl groups is optionally substituted by 1, 2, 3 or 4 R200; -(CR245

R250)0-3-imidazolidinyl; (CR245R250)0-3-tetrahydrofuryl; (CR245R250)0-3-tetrahydropyranyl; (CR245R250)0-3-piperazinil; (CR245R250) 0-3-pyrrolidinyl; (CR245R250)0-3-piperidinyl; (CR245R250)0-3-indolinyl; each of the above geterotsiklicheskikh group optionally substituted by 1, 2, 3 or 4 R210; (CH2)0-1-CH((CH2)0-4-OH)-(CH2)0-1-phenyl; -(CH2)0-1-CH((C1-C4-hydroxyalkyl)-

(CH2)0-1-pyridyl;

R200in each case represents, independently, (C1-C6)-alkyl, optionally substituted by 1, 2 or 3 groups R205; HE; -NO2; halogen; -CO2N; C≡N; -(CH2)0-4-CO-NR220R225; -(CH2)0-4-CO-((C1-C8)-alkyl); -(CH2)0-4-CO2R215and -(CH2)0-4-O-((C1-C6)-alkyl, optionally substituted by 1, 2, 3, or 5-F);

R205in each case represents, independently, (C1-C6)-alkyl, halogen, -OH, -O-phenyl, -SH, -C≡N, -CF3, (C1-C6)-alkoxy, NH2, NH((C1-C6)-alkyl) and N((C1-C6)-alkyl)((C1-C6)-alkyl);

R210in each case represents, independently, (C1-C6)-alkyl, optionally substituted 1 or 2 groups R205; halogen; (C1-C4)-alkoxy, (C1-C4)-halogenoalkane; -NR220R225; OH; C≡N; and (C3-C7-cycloalkyl, not necessarily samewe the hydrated 1 or 2 groups R 205; -CO-((C1-C4)-alkyl); -SO2-NR235R240; -CO-NR235R240; -SO2-((C1-C4)-alkyl) and =O, where

R215in each case represents, independently, (C1-C6)-alkyl, (CH2)0-2-phenyl, (C3-C6-cycloalkyl, -(CH2)0-2-pyridyl, -(CH2)0-2-pyrrolyl, -(CH2)0-2-imidazolyl, -(CH2)0-2pirimidil, -(CH2)0-2-pyrrolidinyl, -(CH2)0-2-imidazolidinyl, -(CH2)0-2-piperazinil, -(CH2)0-2-piperidinyl and (CH2)0-2-morpholinyl, where the phenyl group in each case is optionally substituted 1 or 2 groups that represent, independently, R205or R210; where each heterocytolysine group in each case is optionally substituted by 1 or 2 R210; where each heteroaryl group in each case is optionally substituted by 1 or 2 R210;

R220and R225in each case represent, independently, -H, -(C1-C4)-alkyl, hydroxy-(C1-C4)-alkyl, halogen-(C1-C4)-alkyl, -(C3-C6-cycloalkyl and((C1-C4)-alkyl)-O-((C1-C2)-alkyl);

R235and R240in each case represent, independently, H or (C1-C6)-alkyl;

R 245and R250in each case represent, independently, H, (C1-C4)-alkyl, (C1-C4-hydroxyalkyl, (C1-C4)-alkoxy, (C1-C4)-halogenoalkane, or

R245and R250taken together with the carbon atom to which they are attached, to form carbocycle of 3, 4, 5 or 6 carbon atoms.

Other preferred compounds of formula AA-3 are compounds in which

X is a (C1-C3)-alkylidene, optionally substituted by 1 or 2 methyl groups;

Z represents SO2, SO, S, or C(O);

Y represents a (C1-C4-halogenated; HE; -N(Y1)(Y2); And (C1-C10)-alkyl, optionally substituted by 1 or 2 substituents, which may be the same or different and are selected from among halogen, hydroxy, (C1-C4)-alkoxy, (C1-C4)-dialkoxy and (C1-C4)-halogenoalkane; and (C1-C4)-alkoxy; phenyl, optionally substituted with halogen, (C1-C4)-alkyl, (C1-C4)-alkoxy, CN or NO2; and benzyl, optionally substituted with halogen, (C1-C4)-alkyl, (C1-C4)-alkoxy, CN or NO2; where

Y1and Y2are the same or different and represent H; and (C1-C6)-alkyl, optional the nutrient substituted 1, 2 or 3 substituents selected from among halogen, (C1-C2)-alkoxy, (C3-C6)-cycloalkyl and IT; and (C2-C6-alkanoyl; phenyl; -SO2-(C1-C4)-alkyl; benzyl and (C3-C6-cycloalkyl-(C1-C2)-alkyl; or

-N(Y1)(Y2) to form a cycle selected from the piperazinil, piperidinyl, morpholinyl and pyrrolidinyl, where each cycle is optionally substituted by 1, 2, 3, or 4 groups that represent, independently, (C1-C6)-alkyl, (C1-C6)-alkoxy, (C1-C6)-alkoxy-(C1-C6)-alkyl or halogen.

Preferred compounds of formula AA-3 are also the compounds of formula AA-4, i.e. the compounds of formula AA-3, in which

X is a (C1-C3)-alkylidene, optionally substituted 1 methyl group;

Z represents SO2, SO, S, or C(O);

Y is HE, -N(Y1)(Y2), phenyl, benzyl or (C1-C10)-alkyl, optionally substituted by 1 or 2 substituents, which may be the same or different and are selected from among halogen, hydroxy, methoxy, ethoxy, dimethoxy, diethoxy and CF3; where

Y1and Y2are the same or different and represent H; and (C1-C4)-alkyl, optionally substituted by 1 or 2 substituents, selected and from among halogen, methoxy, ethoxy, cyclopropyl and HE; or

-N(Y1)(Y2) to form a cycle selected from the piperazinil, piperidinyl, morpholinyl and pyrrolidinyl, where each cycle is optionally substituted 1 or 2 groups that represent, independently, (C1-C4)-alkyl, (C1-C4)-alkoxy or halogen;

R1represents benzyl, optionally substituted by 1, 2 or 3 groups selected independently from among methyl, ethyl, n-propyl, isopropyl, hydroxymethyl, monohalogenated, dehalogenating, trihalomethyl, -CH2CF3, methoxymethyl, halogen, methoxy, ethoxy, n-propyloxy, isopropoxy and HE;

R2and R3represent, independently, H or (C1-C4)-alkyl,

Rwithis a (C1-C6)-alkyl, optionally substituted by 1, 2 or 3 groups R205; cyclopropyl, cyclopropylmethyl, cyclopentyl, cyclopentylmethyl, cyclohexyl, cyclohexylmethyl; -(CR245R250)0-3is phenyl, optionally substituted 1 or 2 groups R200; -(CR245R250)0-3-pyridyl, optionally substituted by 1 or 2 R200; -(CR245R250)0-3-piperazinil; -(CR245R250)0-3-pyrrolidinyl or -(CR245R250)0-3-piperidinyl; each of the above geterotsiklicheskikh group optionally substituted by 1, and the 2 groups of R 210;

R200in each case chosen, independently, from (C1-C4)-alkyl, optionally substituted 1 or 2 groups R205; HE and halogen;

R205in each case chosen, independently, from (C1-C4)-alkyl, halogen, -OH, -SH, -C≡N, -CF3and (C1-C4)-alkoxy;

R210in each case chosen, independently, from (C1-C4)-alkyl, optionally substituted 1 or 2 groups R205; halogen; (C1-C4)-alkoxy; OCF3; NH2; NH((C1-C6)-alkyl); NH((C1-C6)-alkyl)((C1-C6)-alkyl); and HE CO- ((C1-C4)-alkyl); where

R245and R250in each case chosen, independently, from H, (C1-C4)-hydroxyalkyl, (C1-C4)-alkoxy, or

R245and R250taken together with the carbon atom to which they are attached, to form carbocycle of 3, 5 or 6 carbon atoms.

Preferred compounds of formula AA, AA-1 and AA-2 are the compounds of formula AA-5, i.e. compounds of formula AA, AA-1 and AA-2, in which

one of RNand RN' represents hydrogen and the other represents-C(=O)-(CRR')0-6R100; and

R100represents aryl, heteroaryl or heterocyclyl, where the cyclical part of each group optionally substituted by 1, 2 or 3 FCU is the groups, selected, independently, from

-OR, -NO2, (C1-C6)-alkyl, halogen, -C≡N, -OCF3, -CF3, -(CH2)0-4-O-P(=O)(OR)(OR'), -(CH2)0-4-CO-NR105R'105, -(CH2)0-4-O-(CH2)0-4-CONR102R102', -(CH2)0-4-CO-((C1-C12)-alkyl), -(CH2)0-4-CO-((C2-C12-alkenyl), -(CH2)0-4-CO-((C2-C12)-quinil), -(CH2)0-4-CO-(CH2)0-4-((C3-C7)-cycloalkyl), -(CH2)0-4-R110, -(CH2)0-4-R120, -(CH2)0-4-R130, -(CH2)0-4-CO-R110, -(CH2)0-4-CO-R120, -(CH2)0-4-CO-R130, -(CH2)0-4-CO-

R140, -(CH2)0-4-CO-O-R150, -(CH2)0-4-SO2-NR105R'105, -(CH2)0-4SO is((C1-C8)-alkyl), -(CH2)0-4-SO2-((C1-C12)-alkyl), -(CH2)0-4-SO2-(CH2)0-4-((C3-C7)-cycloalkyl), -(CH2)0-4-N(R150)-CO-O-R150, -(CH2)0-4-N(R150)-CO-N(R150)2, -(CH2)0-4-N(R150)-CS-N

(R150)2, -(CH2)0-4-N(R150)-CO-R105, -(CH2)0-4-NR105R'105, -(CH2)0-4-R140, -(CH2)0-4-O-CO-((C1-C6)-alkyl), -(CH2) 0-4-O-P(O)-(O-R110)2, -(CH2)0-4-O-CO-N(R150)2, -(CH2)0-4-O-CS-N(R150)2, -(CH2)0-4-O-(R150), -(CH2)0-4-O-R150'-COOH, -(CH2)0-4-S-(R150), -(CH2)0-4-N(R150)-SO2-R105, -(CH2)0-4-((C3-C7)-cycloalkyl), (C2-C10-alkenyl or (C2-C10)-quinil.

Preferred compounds of formula AA-5 are compounds in which

one of RNand RN' represents hydrogen and the other represents-C(=O)-

R100; and

R100represents aryl or heteroaryl, where the cyclical part of each group optionally substituted by 1, 2 or 3 groups selected, independently, from

-OR, -NO2, (C1-C6)-alkyl, halogen, -C≡N, -OCF3, -CF3, -(CH2)0-4-O-P(=O)(OR)(OR'), -(CH2)0-4-CO-NR105R'105, -(CH2)0-4-O-(CH2)0-4-CONR102R102', -(CH2)0-4-CO-((C1-C12)-alkyl), -(CH2)0-4-CO-((C2-C12-alkenyl), -(CH2)0-4-CO-((C2-C12)-quinil), -(CH2)0-4-CO-(CH2)0-4-((C3-C7)-cycloalkyl), -(CH2)0-4-R110, -(CH2)0-4-R120, -(CH2)0-4-R130, -(CH2)0-4-CO-R110, -(CH2)04 -CO-R120, -(CH2)0-4-CO-R130, -(CH2)0-4-CO-

R140, -(CH2)0-4-CO-O-R150, -(CH2)0-4-SO2-NR105R'105, -(CH2)0-4SO is((C1-C8)-alkyl), -(CH2)0-4-SO2-((C1-C12)-alkyl), -(CH2)0-4-SO2-(CH2)0-4-((C3-C7)-cycloalkyl), -(CH2)0-4-N(R150)-CO-O-R150, -(CH2)0-4-N(R150)-CO-N(R150)2, -(CH2)0-4-N(R150)-CS-N

(R150)2, -(CH2)0-4-N(R150)-CO-R105, -(CH2)0-4-NR105R'105, -(CH2)0-4-R140, -(CH2)0-4-O-CO-((C1-C6)-alkyl), -(CH2)0-4-O-P(O)-(O-R110)2, -(CH2)0-4-O-CO-N(R150)2, -(CH2)0-4-O-CS-N(R150)2, -(CH2)0-4-O-(R150), -(CH2)0-4-O-R150'-COOH, -(CH2)0-4-S-(R150), -(CH2)0-4-N(R150)-SO2-R105, -(CH2)0-4-((C3-C7)-cycloalkyl), (C2-C10-alkenyl or (C2-C10)-quinil.

Preferred compounds of formula AA-5 are also connections

one of RNand RN' represents hydrogen and the other represents-C(=O)-aryl or-C(=O)-heteroaryl, where the cyclic portion of each is a group optionally substituted by 1, 2 or 3 groups selected, independently, from

-OR, -NO2, (C1-C6)-alkyl, halogen, -C≡N, -OCF3, -CF3, -(CH2)0-4-CO-NR105R'105, -(CH2)0-4-O-(CH2)0-4-CONR102R102', -(CH2)0-4-CO-((C1-C12)-alkyl), -(CH2)0-4-CO-((C2-C12-alkenyl), -(CH2)0-4-CO-((C2-C12)-quinil), -(CH2)0-4-R110, -(CH2)0-4-R120, -(CH2)0-4-R130,

-(CH2)0-4-CO-R110, -(CH2)0-4-CO-R120, -(CH2)0-4-CO-R130, -(CH2)0-4-CO-R140, -(CH2)0-4-CO-O-

R150, -(CH2)0-4-SO2-NR105R'105, -(CH2)0-4SO is((C1-C8)-alkyl), -(CH2)0-4-SO2-((C1-C12)-alkyl), -(CH2)0-4-N(R150)-CO-O-R150, -(CH2)0-4-N(R150)-CO-N(R150)2, -(CH2)0-4-N(R150)-CO-R105, -(CH2)0-4-NR105R'105,

-(CH2)0-4-R140, (CH2)0-4-O-CO-((C1-C6)-alkyl), -(CH2)0-4-O-CO-N(R150)2, -(CH2)0-4-O-(R150), -(CH2)0-4-N(R150)-SO2-R105, -(CH2)0-4-((C3-C7)-cycloalkyl), (C2-C10-alkenyl or (C2-C10)-quinil.

Other preferred compounds of formula AA-5 are compounds in which

one of RNand RN' represents hydrogen and the other represents-C(=O)-aryl or-C(=O)-heteroaryl, where the cyclical part of each group optionally substituted by 1 or 2 groups selected, independently, from

(C1-C6)-alkyl, halogen, -(CH2)0-4-CO-NR105R'105, -(CH2)0-4-O-CO-N(R150)2,

-(CH2)0-4-N(R150)-SO2-R105, -(CH2)0-4-SO2-NR105R'105-(C3-C7)-cycloalkyl, (C2-C10-alkenyl, -(CH2)0-4-R110, -(CH2)0-4-R120, -(CH2)0-4-R130or (C2-C10)-quinil.

Other preferred compounds of formula AA-5 are compounds in which

one of RNand RN' represents hydrogen and the other represents-C(=O)-phenyl, where the phenyl cycle optionally substituted 1 or 2 groups selected, independently, from

(C1-C6)-alkyl, halogen, -(CH2)0-4-CO-NR105R'105, -(CH2)0-4-O-CO-N(R150)2,

-(CH2)0-4-N(R150)-SO2-R105, -(CH2)0-4-SO2-NR105R'105-(C3-C7)-cycloalkyl, (C2-C10-alkenyl, -(CH )0-4-R110, -(CH2)0-4-R120, -(CH2)0-4-R130or (C2-C10)-quinil.

Other preferred compounds of formula AA-5 are compounds in which one of RNand RN' represents hydrogen and the other represents a

where sub is a hydrogen or a (C1-C6)-alkyl, halogen, -(CH2)0-4-CO-NR105R'105, -(CH2)0-4-O-CO-N(R150)2, -(CH2)0-4-N(R150)-SO2-R105, -(CH2)0-4-SO2-NR105R'105-(C3-C7-cycloalkyl -(C2-C10)-alkenyl, -(CH2)0-4-R110,

-(CH2)0-4-R120, -(CH2)0-4-R130or (C2-C10)-quinil.

The preferred stereocilia compounds of formula AA is

Preferred compounds of formula I are the compounds of formula I-1, i.e. the compounds of formula I, in which

R1represents aryl, heteroaryl, heterocyclyl -(C1-C6-alkylaryl -(C1-C6-alkylglycerol or -(C1-C6)-Alkylglucoside, where the cyclical part of each substituent optionally substituted by 1, 2, 3 or 4 groups selected, independently, from halogen, -OH, -H, -C≡N, -NO2, -NR105R'105, -CO2R, -N(R)COR', or-N(R)SO2R', -C(=O)-(C1-C4)-alkyl, -SO2-amino, -SO2-mono - or-dialkylamino, -C(=O)-amino, -C(=O)-mono - or-dialkylamino, -SO2-(C1-C4)-alkyl, or

(C1-C6)-alkoxy, optionally substituted by 1, 2 or 3 groups selected, independently, from halogen, or

(C3-C7-cycloalkyl, optionally substituted by 1, 2 or 3 groups selected, independently, from halogen, -OH, -SH, -C≡N, -CF3, (C1-C3)-alkoxy, amino, -(C1-C6)-alkyl and mono - or dialkylamino, or

(C1-C10)-alkyl, optionally substituted by 1, 2 or 3 groups selected, independently, from halogen, -OH, -SH, -C≡N, -CF3, (C1-C3)-alkoxy, amino, mono - or dialkylamino and -(C1-C3)-alkyl, or

(C2-C10)-alkenyl or (C2-C10)-quinil, each of which is optionally substituted by 1, 2 or 3 groups selected, independently, from halogen, -OH, -SH, -C≡N, -CF3, (C1-C3)-alkoxy, amino, (C1-C6)-alkyl and mono - or dialkylamino; and heterocyclyl the group is also optionally substituted by oxo.

Preferred compounds of formula I-1 are also connections

R1represents -(C1-C6-alkylaryl,- ( 1-C6-alkylglycerol or -(C1-C6)-Alkylglucoside, where the cyclical part of each substituent optionally substituted by 1, 2, 3 or 4 groups selected, independently, from halogen, -OH, -SH, -C≡N, -NO2, -NR105R'105, -CO2R, -N(R)COR', or-N(R)SO2R', -C(=O)-(C1-C4)-alkyl, -SO2-amino, -SO2-mono - or-dialkylamino, -C(=O)-amino, -C(=O)-mono - or-dialkylamino, -SO2-(C1-C4)-alkyl, or

(C1-C6)-alkoxy, optionally substituted by 1, 2 or 3 groups selected, independently, from halogen, or

(C3-C7-cycloalkyl, optionally substituted by 1, 2 or 3 groups selected, independently, from halogen, -OH, -SH, -C≡N, -CF3, (C1-C3)-alkoxy, amino, -(C1-C6)-alkyl and mono - or dialkylamino, or

(C1-C10)-alkyl, optionally substituted by 1, 2 or 3 groups selected, independently, from halogen, -OH, -SH, -C≡N, -CF3, (C1-C3)-alkoxy, amino, mono - or dialkylamino and -(C1-C3)-alkyl, or

(C2-C10)-alkenyl or (C2-C10)-quinil, each of which is optionally substituted by 1, 2 or 3 groups selected, independently, from halogen, -OH, -SH, -C≡N, -CF3, (C1-C3)-alkoxy, amino, (C1-C6)-alkyl and mono - or dialkylamino; and GE is eroticline the group is also optionally substituted by oxo.

Preferred compounds of formula I-1 are also connections

R1represents -(CH2)-aryl, -(CH2-heteroaryl or -(CH2)-heterocyclyl, where the cyclical part of each substituent optionally substituted by 1, 2, 3 or 4 groups selected, independently, from halogen, -OH, -SH, -C≡N, -NO2, -NR105

R'105, -CO2R, -N(R)COR', or-N(R)SO2R', -C(=O)-(C1-C4)-alkyl, -SO2-amino, -SO2-mono - or-dialkylamino, -C(=O)-amino, -C(=O)-mono - or-dialkylamino, -SO2-(C1-C4)-alkyl, or

(C1-C6)-alkoxy, optionally substituted by 1, 2 or 3 groups selected, independently, from halogen, or

(C3-C7-cycloalkyl, optionally substituted by 1, 2 or 3 groups selected, independently, from halogen, -OH, -SH, -C≡N, -CF3, (C1-C3)-alkoxy, amino, -(C1-C6)-alkyl and mono - or dialkylamino, or

(C1-C10)-alkyl, optionally substituted by 1, 2 or 3 groups selected, independently, from halogen, -OH, -SH, -C≡N, -CF3, (C1-C3)-alkoxy, amino, mono - or dialkylamino and -(C1-C3)-alkyl, or

(C2-C10)-alkenyl or (C2-C10)-quinil, each of which is optionally substituted by 1, 2 or 3 groups selected, independently, from among halog is on, -OH, -SH, -C≡N, -CF3, (C1-C3)-alkoxy, amino, (C1-C6)-alkyl and mono - or dialkylamino; and heterocyclyl the group is also optionally substituted by oxo.

Preferred compounds of formula I-1 are also connections

R1represents-CH2-phenyl or-CH2-pyridinyl, where the cyclical part of each substituent optionally substituted by 1, 2, 3 or 4 groups selected, independently, from halogen, (C1-C4)-alkoxy, hydroxy, -NO2and

(C1-C4)-alkyl, optionally substituted by 1, 2 or 3 substituents selected, independently, from halogen, HE, SH, NH2, NH((C1-C6)-alkyl), N-((C1-C6)-alkyl)((C1-C6)-alkyl, -C≡N, -CF3.

Preferred compounds of formula I-1 are also connections

R1represents-CH2-phenyl or-CH2-pyridinyl where the phenyl or pyridinoline cycles, each optionally substituted by 1 or 2 groups selected, independently, from halogen, (C1-C2)-alkyl, (C1-C2)-alkoxy, hydroxy, -CF3and-NO2.

Preferred compounds of formula I-1 are compounds in which

R1represents-CH2-phenyl, where the phenyl cycle optionally substituted 2 groups, select the tion, independently from halogen, (C1-C2)-alkyl, (C1-C2)-alkoxy, hydroxy, and-NO2.

Preferred compounds of formula I-1 are compounds in which R1represents benzyl or 3,5-diferensial.

Preferred compounds of formulas I and I-1 are the compounds of formula I-2, i.e. compounds of formula I or I-1 in which

R2and R3chosen, independently, from H or (C1-C6)-alkyl, optionally substituted by 1, 2 or 3 substituents selected from the group consisting of (C1-C3)-alkyl, halogen, -OH, -SH, -C≡N, -CF3, (C1-C3)-alkoxy and-NR1-aR1-b.

Preferred compounds of formula I-2 are compounds in which

Rwithselected from the group consisting of (C1-C10)-alkyl, optionally substituted by 1, 2 or 3 groups selected, independently, from the group consisting of

R205, -OC=ONR235R240, -S(=O)0-2((C1-C6)-alkyl), -SH, -NR235C=ONR235R240, -C=ONR235R240and-S(=O)2NR235R240; -(CH2)0-3-(C3-C8)-cycloalkyl where cycloalkyl optionally substituted by 1, 2 or 3 groups selected, independently, from the group consisting of R205, -CO2H and CO2-((C1-C4)-alkyl); -(CR245R250)0-4 -aryl;

-(CR245R250)0-4-heteroaryl; -(CR245R250)0-4-geterotsiklicheskie; -[C(R255)(R260)]1-3-CO-N(R255)2; -CH(aryl)2; -CH(heteroaryl)2; -CH(heteroseksualci)2; -CH(aryl)(heteroaryl); -CO-NR235R240; -(CH2)0-1-CH((CH2)0-6-OH)-(CH2)0-1-aryl; -(CH2)0-1-CHRS-6-(CH2)0-1-heteroaryl; -CH(-aryl or-heteroaryl)-CO-O((C1-C4)-alkyl); -CH(-CH2-OH)-CH(OH)-phenyl-NO2; ((C1-C6)-alkyl)-O-((C1-C6)-alkyl) -;- CH2-NH-CH2-CH(-O-CH2-CH3)2; -N and -(CH2)0-6-C(=NR235)(NR235R240); where

each aryl optionally substituted by 1, 2 or 3 R200;

each heteroaryl optionally substituted by 1, 2, 3 or 4 R200;

each heteroseksualci optionally substituted by 1, 2, 3 or 4 R210;

R200in each case chosen, independently, from the group consisting of (C1-C6)-alkyl, optionally substituted by 1, 2 or 3 groups R205; HE; -NO2; halogen; -CO2N; C≡N; -(CH2)0-4-CO-NR220R225; -(CH2)0-4-CO-((C1-C12)-alkyl);

-(CH2)0-4-CO2R215and -(CH2)0-4-O-((C1-C6)-alkyl, optionally substituted by 1, 2, 3, or 5-F);

the de each aryl group in each case is optionally substituted 1, 2 or 3 groups which are, independently, R205, R210or (C1-C6)-alkyl, substituted 1, 2, or 3 groups that represent, independently, R205or R210;

where each heterocytolysine group in each case is optionally substituted by 1, 2, or 3 groups that represent, independently, R210;

where each heteroaryl group in each case is optionally substituted by 1, 2, or 3 groups that represent, independently, R205, R210or (C1-C6)-alkyl, substituted 1, 2, or 3 groups that represent, independently, R205or R210;

R205in each case chosen, independently, from the group consisting of (C1-C6)-alkyl, halogen, -OH, -O-phenyl, -SH, -C≡N, -CF3, (C1-C6)-alkoxy, NH2,

NH((C1-C6)-alkyl) and N((C1-C6)-alkyl)((C1-C6)-alkyl);

R210in each case chosen, independently, from the group consisting of (C1-C6)-alkyl, optionally substituted by 1, 2 or 3 groups R205; halogen; (C1-C6)-alkoxy, (C1-C6)-halogenoalkane; -NR220R225; OH; C≡N; and (C3-C7)-cycloalkyl, optionally substituted by 1, 2 or 3 groups R205; -CO-((C1-C4)-alkyl); -SO2-

NR235R240 ; -CO-NR235R240; -SO2-((C1-C4)-alkyl) and =O, where

R215in each case chosen, independently, from the group consisting of (C1-C6)-alkyl, (CH2)0-2-aryl, (C3-C7)-cycloalkyl, (CH2)0-2-heteroaryl and (CH2)0-2-geterotsiklicheskie, where the aryl group in each case is optionally substituted by 1, 2, or 3 groups that represent, independently, R205or R210; where heterocytolysine group in each case is optionally substituted by 1, 2 or 3 R210; where each heteroaryl group in each case is optionally substituted by 1, 2 or 3 R210;

R220and R225in each case chosen, independently, from the group consisting of-H,

-(C1-C6)-alkyl, hydroxy-(C1-C6)-alkyl, amino-(C1-C6)-alkyl, halogen-(C1-C6)-alkyl, (C3-C7)-cycloalkyl, -((C1-C6)-alkyl)-O-((C1-C3)-alkyl), -aryl, -heteroaryl and-geterotsiklicheskie, where the aryl group in each case is optionally substituted by 1, 2 or 3 groups R270each heteroaryl is optionally substituted by 1, 2, 3 or 4 R200each heteroseksualci is optionally substituted by 1, 2, 3 or 4 R210where

R270in each case, before the hat is, independently, R205, (C1-C6)-alkyl, optionally substituted by 1, 2 or 3 groups R205; halogen; (C1-C6)-alkoxy, (C1-C6)-halogenoalkane; NR235R240; OH; C≡N; -CO-((C1-C4)-alkyl) and =O, where heterocytolysine group in each case is optionally substituted by 1, 2 or 3 groups R205; where each heteroaryl group in each case is optionally substituted by 1, 2 or 3 groups R205;

R235and R240in each case represent, independently, H or (C1-C6)-alkyl;

R245and R250in each case chosen, independently, from the group consisting of H, (C1-C4)-alkyl, (C1-C4)-hydroxyalkyl, (C1-C4)-alkoxy, (C1-C4)-halogenoalkane, or

R245and R250taken together with the carbon atom to which they are attached, to form carbocycle of 3, 4, 5, 6 or 7 carbon atoms, where carbocycle optionally substituted 1 or 2 groups that represent, independently, HE, methyl, Cl, F, och3, CF3, NO2or CN;

R255and R260in each case chosen, independently, from the group consisting of H; and (C1-C6)-alkyl, optionally substituted by 1, 2 or 3 groups R205; -(CH2)0-4-(C3-C7)-cycloalkyl, neobyazatel is substituted 1, 2 or 3 groups R205; -((C1-C4)-alkyl)aryl; -((C1-C4)-alkyl)heteroaryl; -((C1-C4)-alkyl)geterotsiklicheskie; aryl; heteroaryl; geterotsiklicheskie; -(CH2)1-4-R265-(CH2)0-4-aryl; -(CH2)1-4-R265-(CH2)0-4-heteroaryl and -(CH2)1-4-R265-(CH2)0-4-geterotsiklicheskie; where

R265in each case represents, independently, -O-, -S - or-N((C1-C6)-alkyl)-;

each aryl or phenyl optionally substituted by 1, 2, or 3 groups that represent, independently, R205, R210or (C1-C6)-alkyl, substituted 1, 2, or 3 groups that represent, independently, R205or R210.

Preferred compounds of formula I-2 are compounds in which

Rwithrepresents -(CR245R250)0-4-aryl or -(CR245R250)0-4-heteroaryl, where aryl and heteroaryl optionally substituted by 1, 2 or 3 groups R200.

Preferred compounds of formula I-2 are also connections

Rwithrepresents -(CR245R250)-aryl or -(CR245R250-heteroaryl, where each aryl and heteroaryl optionally substituted by 1, 2 or 3 groups R200.

Preferred compounds of formula I-2 are also with the unity, in which

Rwithrepresents -(CH2)-aryl or -(CH2-heteroaryl, where each aryl and heteroaryl optionally substituted by 1, 2 or 3 groups selected from HE, " NO2, halogen, -CO2N, C≡N, -(CH2)0-4-CO-NR220R225, -(CH2)0-4-CO-((C1-C12)-alkyl) and -(CH2)0-4-SO2-NR220R225.

Preferred compounds of formula I-2 are also connections

Rwithrepresents -(CH2)-aryl, where aryl optionally substituted by 1, 2 or 3 groups selected from HE, " NO2, halogen, -CO2N and C≡N.

Preferred compounds of formula I-2 are also connections

Rwithrepresents -(CH2)-phenyl, where phenyl optionally substituted by 1, 2 or 3 groups selected from HE, " NO2, halogen, -CO2N and C≡N.

Preferred compounds of formula I-2 also include compounds in which Rwithrepresents benzyl.

Other preferred compounds of formulas I, I-1 and I-2 are the compounds of formula I-3, i.e. compounds of formulas I, I-1 or I-2, in which

RNrepresents a

where

R4represents NH2, -NH-(CH2)n6-R4-1-The other8, -NR50C(O)R5or-NR50CO2 51,

where

n6is 0, 1, 2 or 3;

n7is 0, 1, 2 or 3;

R4-1selected from the group consisting of-SO2-((C1-C8)-alkyl), -SO-((C1-C8)-alkyl), -S-((C1-C8)-alkyl), -S-CO-((C1-C6)-alkyl), -SO2-NR4-2R4-3; -CO-(C1-C2)-alkyl, -CO-NR4-3R4-4;

R4-2and R4-3represent, independently, H, (C1-C3)-alkyl or (C3-C6-cycloalkyl;

R4-4represents alkyl, phenylalkyl, (C2-C4-alkanoyl or phenylalkanoic;

R5is cyclopropyl, cyclobutyl, cyclopentyl and cyclohexyl, where each cycloalkyl group optionally substituted by one or two groups representing a (C1-C6)-alkyl, preferably - (C1-C2)-alkyl, (C1-C6)-alkoxy, preferably - (C1-C2)-alkoxy, CF3, OH, NH2, NH((C1-C6)-alkyl), N((C1-C6)-alkyl)((C1-C6)-alkyl), halogen, CN or NO2; or cycloalkyl group substituted by 1 or 2 groups that represent, independently, CF3, Cl, F, methyl, ethyl or cyano; (C1-C6)-alkyl, optionally substituted by 1, 2 or 3 groups which are, independently, halogen,

-NR6R7, (C1-C4)-alkoxy, (the 5-C6-heteroseksualci, (C5-C6-heteroaryl, phenyl, (C3-C7-cycloalkyl, -S-(C1-C4)-alkyl, -SO2-(C1-C4)-alkyl, -CO2N, -CONR6R7, -CO2-(C1-C4)-alkyl or phenyloxy; heteroaryl, optionally substituted by 1, 2 or 3 groups which are, independently, (C1-C4)-alkyl, (C1-C4)-alkoxy, halogen, (C1-C4-halogenated or HE; heteroseksualci, optionally substituted by 1, 2 or 3 groups which are, independently, (C1-C4)-alkyl, (C1-C4)-alkoxy, halogen or (C2-C4-alkanoyl; phenyl, optionally substituted by 1, 2, 3, or 4 groups that represent, independently, halogen, HE, (C1-C4)-alkyl, (C1-C4)-alkoxy or (C1-C4-halogenated; and-NR6R7; where

R6and R7chosen, independently, from the group consisting of H, (C1-C6)-alkyl, (C2-C6)-alkanoyl, phenyl, -SO2-(C1-C4)-alkyl and phenyl-(C1-C4)-alkyl;

R8selected from the group consisting of-SO2-heteroaryl, optionally substituted 1 or 2 groups that represent, independently, (C1-C4)-alkyl or halogen; -SO2-aryl, -SO2-geterotsiklicheskie, -C(O)other9that gets the rockleesmile, -S-(C2-C4)-alkanoyl, where

R9represents phenyl-(C1-C4)-alkyl, (C1-C6)-alkyl or H;

R50represents H or (C1-C6)-alkyl;

R51selected from the group consisting of phenyl-(C1-C4)-alkyl, (C1-C6)-alkyl, optionally substituted by 1, 2 or 3 groups which are, independently, halogen, cyano, -NR6R7-C(O)NR6R7, (C3-C7-cycloalkyl or -(C1-C4)-alkoxy; geterotsiklicheskie, optionally substituted 1 or 2 groups that represent, independently, (C1-C4)-alkyl, (C1-C4)-alkoxy, halogen, (C2-C4-alkanoyl, phenyl-

(C1-C4)-alkyl and-SO2-(C1-C4)-alkyl; geterotsiklicheskikh, optionally substituted 1 or 2 groups that represent, independently, (C1-C4)-alkyl,

(C1-C4)-alkoxy, halogen, (C2-C4-alkanoyl, phenyl-(C1-C4)-alkyl and-SO2-(C1-C4)-alkyl; alkenyl; quinil; heteroaryl, optionally substituted 1, 2, or 3 groups that represent, independently, HE, (C1-C4)-alkyl, (C1-C4)-alkoxy, halogen, NH2, NH((C1-C6)-alkyl) or N((C1-C6)-alkyl)((C1-C6)-al is Il); heteroaromatic, optionally substituted by 1, 2 or 3 groups which are, independently, (C1-C4)-alkyl, (C1-C4)-alkoxy, halogen, NH2, NH((C1-C6)-alkyl) or N((C1-C6)-alkyl)((C1-C6)-alkyl); phenyl; and (C3-C8)-cycloalkyl and cycloalkenyl, where phenyl, (C3-C8)-cycloalkyl and cycloalkenyl group substituted by optionally 1, 2, 3, 4, or 5 groups that represent, independently, halogen, CN, NO2, (C1-C6)-alkyl, (C1-C6)-alkoxy, (C2-C6-alkanoyl, (C1-C6-halogenated, (C1-C6)-halogenoalkane, hydroxy, (C1-C6-hydroxyalkyl, (C1-C6)-alkoxy-(C1-C6)-alkyl, (C1-C6)-dialkoxy, (C1-C6)-dialkoxy-(C1-C6)-alkyl or (C1-C6)-alkoxy-(C1-C6)-alkoxy.

Preferred compounds of formula I-3 include compounds in which

RNrepresents a

where

X is a (C1-C4)-alkylidene, optionally substituted by 1, 2 or 3 methyl groups, or-NR4-6; or

R4and R4-6combined with education -(CH2)n10-where

n10is 1, 2, 3 or 4;

Z is chosen and the number of communication SO2SO, S and S(Oh);

Y is chosen from among N, (C1-C4)-halogenoalkane; and (C5-C6)-geterotsiklicheskie containing at least one N, O or S; phenyl; HE; -N(Y1)(Y2); And (C1-C10)-alkyl, optionally substituted by 1-3 substituents, which may be the same or different and are selected from among halogen, hydroxy, alkoxy, dialkoxy, halogenoalkane; and (C3-C8)-cycloalkyl, optionally substituted by 1, 2 or 3 groups selected, independently, from (C1-C3)-alkyl and halogen; alkoxy; phenyl, optionally substituted with halogen, (C1-C4)-alkyl, (C1-C4)-alkoxy, CN or NO2; phenyl-(C1-C4)-alkyl, optionally substituted with halogen, (C1-C4)-alkyl, (C1-C4)-alkoxy, CN or NO2; where

Y1and Y2are the same or different and represent H; and (C1-C10)-alkyl, optionally substituted by 1, 2 or 3 substituents selected from the group consisting of halogen, (C1-C4)-alkoxy, (C3-C8)-cycloalkyl and IT; and (C2-C6)-alkenyl; and (C2-C6-alkanoyl; phenyl; -SO2-(C1-C4)-alkyl; phenyl-(C1-C4)-alkyl and (C3-C8-cycloalkyl-(C1-C4)-alkyl; or

-N(Y1)(Y2) forms the CEC is, selected from among piperazinil, piperidinyl, morpholinyl and pyrrolidinyl, where each cycle is optionally substituted by 1, 2, 3, or 4 groups that represent, independently, (C1-C6)-alkyl, (C1-C6)-alkoxy, (C1-C6)-alkoxy-(C1-C6)-alkyl or halogen.

Preferred compounds of formula I-3 include compounds in which

X is a (C1-C4)-alkylidene, optionally substituted by 1, 2 or 3 methyl groups;

Z is chosen from among SO2SO, S and S(Oh);

Y is chosen from among N, (C1-C4)-halogenoalkane; and (C5-C6)-geterotsiklicheskie containing at least one N, O or S; phenyl; HE; -N(Y1)(Y2); And (C1-C10)-alkyl, optionally substituted by 1-3 substituents, which may be the same or different and are selected from the group consisting of halogen, hydroxy, alkoxy, dialkoxy, halogenoalkane; and (C3-C8)-cycloalkyl, optionally substituted by 1, 2 or 3 groups selected, independently, from (C1-C3)-alkyl and halogen; alkoxy; phenyl, optionally substituted with halogen, (C1-C4)-alkyl,

(C1-C4)-alkoxy, CN or NO2; phenyl-(C1-C4)-alkyl, optionally substituted with halogen, (C1-C4)-alkyl, (C1-C4)and is coxi, CN or NO2; where

Y1and Y2are the same or different and represent H; and (C1-C6)-alkyl, optionally substituted by 1, 2 or 3 substituents selected from the group consisting of halogen, (C1-C4)-alkoxy, (C3-C8)-cycloalkyl and IT; and (C2-C6)-alkenyl; and (C2-C6-alkanoyl; phenyl; -SO2-(C1-C4)-alkyl; phenyl-(C1-C4)-alkyl or (C3-C8-cycloalkyl-(C1-C4)-alkyl; or

-N(Y1)(Y2) to form a cycle selected from the piperazinil, piperidinyl, morpholinyl and pyrrolidinyl, where each cycle is optionally substituted by 1, 2, 3, or 4 groups that represent, independently, (C1-C6)-alkyl, (C1-C6)-alkoxy, (C1-C6)-alkoxy-(C1-C6)-alkyl or halogen.

Preferred compounds of formula I-3 include compounds in which RNrepresents a

and where R4represents NH2, -NH-(CH2)n6-R4-1-The other8, -NR50C(O)R5or-NR50CO2R51where

n6is 0, 1, 2 or 3;

n7is 0, 1, 2 or 3;

R4-1selected from the group consisting of-SO2-((C1-C8)-alkyl), -SO-((C1-C8)-alkyl), -S-((C1-C8)-alkyl), -S-CO-(( -C6)-alkyl), -SO2-NR4-2R4-3; -CO-(C1-C2)-alkyl, -CO-NR4-3R4-4;

R4-2and R4-3represent, independently, H, (C1-C3)-alkyl or (C3-C6-cycloalkyl;

R4-4represents alkyl, phenylalkyl, (C2-C4-alkanoyl or phenylalkanoic;

R5is cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl, where each cycloalkyl group optionally substituted by one or two groups representing a (C1-C6)-alkyl, preferably - (C1-C2)-alkyl, (C1-C6)-alkoxy, preferably - (C1-C2)-alkoxy, CF3, OH, NH2, NH((C1-C6)-alkyl), N((C1-C6)-alkyl)((C1-C6)-alkyl), halogen, CN or NO2; or cycloalkyl group substituted by 1 or 2 groups that represent, independently, CF3, Cl, F, methyl, ethyl or cyano; (C1-C6)-alkyl, optionally substituted by 1, 2 or 3 groups which are, independently, halogen,

-NR6R7, (C1-C4)-alkoxy, (C5-C6-heteroseksualci, (C5-C6-heteroaryl, phenyl, (C3-C7-cycloalkyl, -S-(C1-C4)-alkyl, -SO2-(C1-C4)-alkyl, -CO2N, -CONR6R7, -CO2-(C1-C )-alkyl or phenyloxy; heteroaryl, optionally substituted by 1, 2 or 3 groups which are, independently, (C1-C4)-alkyl, (C1-C4)-alkoxy, halogen, (C1-C4-halogenated or HE; heteroseksualci, optionally substituted by 1, 2 or 3 groups which are, independently, (C1-C4)-alkyl, (C1-C4)-alkoxy, halogen or (C2-C4-alkanoyl; phenyl, optionally substituted by 1, 2, 3, or 4 groups that represent, independently, halogen, HE, (C1-C4)-alkyl, (C1-C4)-alkoxy or (C1-C4-halogenated; and-NR6R7; where

R6and R7chosen, independently, from the group consisting of H, (C1-C6)-alkyl, (C2-C6)-alkanoyl, phenyl, -SO2-(C1-C4)-alkyl and phenyl-(C1-C4)-alkyl;

R8selected from the group consisting of-SO2-heteroaryl, optionally substituted 1 or 2 groups that represent, independently, (C1-C4)-alkyl or halogen; -SO2-aryl, -SO2-geterotsiklicheskie, -C(O)other9, geterotsiklicheskie, -S-(C2-C4)-alkanoyl, where

R9represents phenyl-(C1-C4)-alkyl, (C1-C6)-alkyl or H;

R50represents H or (C1-C6)-alkyl; and

R51selected from the group consisting of phenyl-(C1-C4)-alkyl, (C1-C6)-alkyl, optionally substituted by 1, 2 or 3 groups which are, independently, halogen, cyano, -NR6R7-C(O)NR6R7, (C3-C7-cycloalkyl or -(C1-C4)-alkoxy; geterotsiklicheskie, optionally substituted 1 or 2 groups that represent, independently, (C1-C4)-alkyl, (C1-C4)-alkoxy, halogen, (C2-C4-alkanoyl, phenyl-

(C1-C4)-alkyl and-SO2-(C1-C4)-alkyl; geterotsiklicheskikh, optionally substituted 1 or 2 groups that represent, independently, (C1-C4)-alkyl,

(C1-C4)-alkoxy, halogen, (C2-C4-alkanoyl, phenyl-(C1-C4)-alkyl and-SO2-(C1-C4)-alkyl; alkenyl; quinil; heteroaryl, optionally substituted 1, 2, or 3 groups that represent, independently, HE, (C1-C4)-alkyl, (C1-C4)-alkoxy, halogen, NH2, NH(C1-C6)-alkyl or N((C1-C6)-alkyl)((C1-C6)-alkyl); heteroaromatic, optionally substituted by 1, 2 or 3 groups which are, independently, (C1-C4)-alkyl, (C1-C4)-alkoxy, halogen, NH2, NH((C1-C6)-alkyl) or N((C1-C6)-al is silt)((C 1-C6)-alkyl); phenyl; and (C3-C8)-cycloalkyl and cycloalkenyl, where phenyl, (C3-C8)-cycloalkyl and cycloalkenyl group substituted by optionally 1, 2, 3, 4, or 5 groups that represent, independently, halogen, CN, NO2, (C1-C6)-alkyl, (C1-C6)-alkoxy, (C2-C6-alkanoyl, (C1-C6-halogenated, (C1-C6)-halogenoalkane, hydroxy, (C1-C6-hydroxyalkyl, (C1-C6)-alkoxy-(C1-C6)-alkyl, (C1-C6)-dialkoxy, (C1-C6)-dialkoxy-(C1-C6)-alkyl or (C1-C6)-alkoxy-(C1-C6)-alkoxy; and

Y represents a (C1-C10)-alkyl, optionally substituted by 1-3 substituents, which may be the same or different and are selected from among halogen, hydroxy, alkoxy, dialkoxy, halogenoalkane.

Preferred compounds of formula I-3 are also connections

Rwithis a (C1-C8)-alkyl, optionally substituted by 1, 2 or 3 groups selected, independently, from the group consisting of R205, -OC=ONR235R240, -S(=O)0-2((C1-C6)-alkyl), -SH, -C=ONR235R240and-S(=O)2NR235R240; -(CH2)0-3-(C3-C8-cycloalkyl, where qi is loukil optionally substituted 1, 2 or 3 groups selected, independently, from the group consisting of R205, -CO2H and CO2-((C1-C4)-alkyl); -(CR245R250)0-4-phenyl; -(CR245R250)0-4-heteroaryl;

-(CR245R250)0-4-heteroseksualci; -(CH2)0-1-CH((CH2)0-4-OH)-(CH2)0-1-phenyl; -(CH2)0-1-CHRS-6-(CH2)0-1-heteroaryl; -CH(-CH2-OH)-CH(OH)-phenyl-NO2; ((C1-C6)-alkyl)-O-((C1-C6)-alkyl)-or -(CH2)0-6-C(=NR235)(NR235R240); where

each aryl optionally substituted by 1, 2 or 3 R200;

each heteroaryl optionally substituted by 1, 2, 3 or 4 R200;

each heteroseksualci optionally substituted by 1, 2, 3 or 4 R210;

R200in each case represents, independently, (C1-C6)-alkyl, optionally substituted by 1, 2 or 3 groups R205; HE; -NO2; halogen; -CO2N; C≡N; -(CH2)0-4-CO-NR220R225; -(CH2)0-4-CO-((C1-C12)-alkyl); -(CH2)0-4-CO2R215or -(CH2)0-4-O-((C1-C6)-alkyl, optionally substituted by 1, 2, 3, or 5-F);

R205in each case represents, independently, (C1-C6)-alkyl, halogen, -OH, -O-phenyl, -SH, -C≡N, -CF3, (C1-C6-alcox is, NH2, NH((C1-C6)-alkyl) or N((C1-C6)-alkyl)((C1-C6)-alkyl);

R210in each case represents, independently, (C1-C6)-alkyl, optionally substituted by 1, 2 or 3 groups R205; halogen; (C1-C6)-alkoxy, (C1-C6)-halogenoalkane; -NR220R225; OH; C≡N; and (C3-C7-cycloalkyl, optionally substituted by 1, 2 or 3 groups R205; -CO-((C1-C4)-alkyl); -SO2-NR235R240; -CO-NR235R240; -SO2-((C1-C4)-alkyl) and =O, where

R215in each case represents, independently, (C1-C6)-alkyl, (CH2)0-2-phenyl, (C3-C7-cycloalkyl, (CH2)0-2-heteroaryl and (CH2)0-2-heteroseksualci, where the phenyl group in each case is optionally substituted by 1, 2, or 3 groups that represent, independently, R205or R210; where heterocytolysine group in each case is optionally substituted by 1, 2 or 3 R210; where each heteroaryl group in each case is optionally substituted by 1, 2 or 3 R210;

R220and R225in each case represent, independently, -H, -(C1-C6)-alkyl, hydroxy-(C1-C6)-alkyl, halogen-(C1-C6)-alkyl, -(C3-C 7-cycloalkyl and((C1-C6)-alkyl)-O-((C1-C3)-alkyl);

R235and R240in each case represent, independently, H or (C1-C6)-alkyl;

R245and R250in each case represent, independently, H, (C1-C4)-alkyl, (C1-C4-hydroxyalkyl, (C1-C4)-alkoxy, (C1-C4)-halogenoalkane, or

R245and R250taken together with the carbon atom to which they are attached, to form carbocycle of 3, 4, 5, 6 or 7 carbon atoms.

Preferred compounds of formula I-3 are also connections

R1represents benzyl, optionally substituted by 1, 2, 3 or 4 groups selected, independently, from halogen, (C1-C4)-alkoxy, hydroxy and (C1-C4)-alkyl, optionally substituted by 1, 2 or 3 substituents from halogen, HE, SH, NH2, NH((C1-C6)-alkyl), N((C1-C6)-alkyl)((C1-C6)-alkyl), C≡N, CF3;

R2and R3chosen, independently, from H or (C1-C4)-alkyl, optionally substituted by 1 Deputy, selected from among halogen, -OH, -SH, -C≡N, -CF3, (C1-C3)-alkoxy, NH2, NH((C1-C6)-alkyl) and N((C1-C6)-alkyl)((C1-C6)-alkyl);

Rwithis a (C 1-C8)-alkyl, optionally substituted by 1, 2 or 3 groups selected, independently, from among the R205, -SH, -C=ONR235R240and-S(=O)2NR235R240; -(CH2)0-3-(C3-C6-cycloalkyl where cycloalkyl optionally substituted by 1, 2 or 3 groups selected, independently, from among the R205, -CO2H and CO2-((C1-C4)-alkyl); -(CR245R250)0-4is phenyl, optionally substituted by 1, 2 or 3 R200; -(CR245R250)0-3-pyridyl; -(CR245R250)0-3-pyridazinyl; -(CR245R250)0-3-pyrimidinyl; -(CR245R250)0-3-pyrazinyl; -(CR245R250)0-3-furyl;

-(CR245R250)0-3-indolyl; -(CR245R250)0-3-thienyl; -(CR245R250)0-3-pyrrolyl; -(CR245R250)0-3-pyrazolyl; -(CR245R250)0-3-benzoxazolyl; -(CR245R250)0-3-imidazolyl; each of the above heteroaryl groups is optionally substituted by 1, 2, 3 or 4 R200; -(CR245

R250)0-3-imidazolidinyl; (CR245R250)0-3-tetrahydrofuryl; (CR245R250)0-3-tetrahydropyranyl; (CR245R250)0-3-piperazinil; (CR245R250)0-3-pyrrolidinyl; (CR245R250)0-3-piperidinyl; (CR245R250)0-3-indolinyl; to whom each of the above geterotsiklicheskikh groups optionally substituted 1, 2, 3, or 4 R210; (CH2)0-1-CH((CH2)0-4-OH)-(CH2)0-1-phenyl; -(CH2)0-1-CH((C1-C4-hydroxyalkyl)-

(CH2)0-1-pyridyl;

R200in each case represents, independently, (C1-C6)-alkyl, optionally substituted by 1, 2 or 3 groups R205; HE; -NO2; halogen; -CO2N; C≡N; -(CH2)0-4-CO-NR220R225; -(CH2)0-4-CO-((C1-C8)-alkyl); -(CH2)0-4-CO2R215and -(CH2)0-4-O-((C1-C6)-alkyl, optionally substituted by 1, 2, 3, or 5-F);

R205in each case represents, independently, (C1-C6)-alkyl, halogen, -OH, -O-phenyl, -SH, -C≡N, -CF3, (C1-C6)-alkoxy, NH2, NH((C1-C6)-alkyl) and N((C1-C6)-alkyl)((C1-C6)-alkyl);

R210in each case represents, independently, (C1-C6)-alkyl, optionally substituted 1 or 2 groups R205; halogen; (C1-C4)-alkoxy, (C1-C4)-halogenoalkane; -NR220R225; OH; C≡N; and (C3-C7-cycloalkyl, optionally substituted 1 or 2 groups R205; -CO-((C1-C4)-alkyl); -SO2-NR235R240; -CO-NR235R240; -SO2-((C1-C4)-alkyl) and =O, where

R215each of the beam is independently, (C1-C6)-alkyl, (CH2)0-2-phenyl, (C3-C6-cycloalkyl, -(CH2)0-2-pyridyl, -(CH2)0-2-pyrrolyl, -(CH2)0-2-imidazolyl, -(CH2)0-2pirimidil, -(CH2)0-2-pyrrolidinyl, -(CH2)0-2-imidazolidinyl, -(CH2)0-2-piperazinil, -(CH2)0-2-piperidinyl and (CH2)0-2-morpholinyl, where the phenyl group in each case is optionally substituted 1 or 2 groups that represent, independently, R205or R210; where each heterocytolysine group in each case is optionally substituted by 1 or 2 R210; where each heteroaryl group in each case is optionally substituted by 1 or 2 R210;

R220and R225in each case represent, independently, -H, -(C1-C4)-alkyl, hydroxy-(C1-C4)-alkyl, halogen-(C1-C4)-alkyl, -(C3-C6-cycloalkyl and((C1-C4)-alkyl)-O-((C1-C2)-alkyl);

R235and R240in each case represent, independently, H or (C1-C6)-alkyl;

R245and R250in each case represent, independently, H, (C1-C4)-alkyl, (C1-C4-hydroxyalkyl, (C1-C4)-alkoxy, (C1-C4-GoLoG is alkoxy, or

R245and R250taken together with the carbon atom to which they are attached, to form carbocycle of 3, 4, 5 or 6 carbon atoms.

Other preferred compounds of formula I-3 include compounds in which

X is a (C1-C3)-alkylidene, optionally substituted by 1 or 2 methyl groups;

Z represents SO2, SO, S, or C(O);

Y represents a (C1-C4-halogenated; HE; -N(Y1)(Y2); And (C1-C10)-alkyl, optionally substituted by 1 or 2 substituents, which may be the same or different and are selected from among halogen, hydroxy, (C1-C4)-alkoxy, (C1-C4)-dialkoxy and (C1-C4)-halogenoalkane; and (C1-C4)-alkoxy; phenyl, optionally substituted with halogen, (C1-C4)-alkyl, (C1-C4)-alkoxy, CN or NO2; and benzyl, optionally substituted with halogen, (C1-C4)-alkyl, (C1-C4)-alkoxy, CN or NO2; where

Y1and Y2are the same or different and represent H; and (C1-C6)-alkyl, optionally substituted by 1, 2 or 3 substituents selected from among halogen, (C1-C2)-alkoxy, (C3-C6)-cycloalkyl and IT; and (C2-C6-alkanoyl; phenyl; -SO2-(C1- 4)-alkyl; benzyl and (C3-C6-cycloalkyl-(C1-C2)-alkyl; or

-N(Y1)(Y2) to form a cycle selected from the piperazinil, piperidinyl, morpholinyl and pyrrolidinyl, where each cycle is optionally substituted by 1, 2, 3, or 4 groups that represent, independently, (C1-C6)-alkyl, (C1-C6)-alkoxy, (C1-C6)-alkoxy-(C1-C6)-alkyl or halogen.

Preferred compounds of formula I-3 are also the compounds of formula I-4, i.e. the compounds of formula I-3 in which

X is a (C1-C3)-alkylidene, optionally substituted 1 methyl group;

Z represents SO2, SO, S, or C(O);

Y is HE; -N(Y1)(Y2); phenyl; benzyl or (C1-C10)-alkyl, optionally substituted by 1 or 2 substituents, which may be the same or different and are selected from among halogen, hydroxy, methoxy, ethoxy, dimethoxy, diethoxy and CF3; where

Y1and Y2are the same or different and represent H; and (C1-C4)-alkyl, optionally substituted by 1 or 2 substituents selected from halogen, methoxy, ethoxy, cyclopropyl and HE; or

-N(Y1)(Y2) to form a cycle selected from the piperazinil, piperidinyl, morpholinyl and pyrrolidinyl, where ka is every cycle optionally substituted 1 or 2 groups represent, independently, (C1-C4)-alkyl, (C1-C4)-alkoxy or halogen;

R1represents benzyl, optionally substituted by 1, 2 or 3 groups selected independently from among methyl, ethyl, n-propyl, isopropyl, hydroxymethyl, monohalogenated, dehalogenating, trihalomethyl, -CH2CF3, methoxymethyl, halogen, methoxy, ethoxy, n-propyloxy, isopropoxy and HE;

R2and R3represent, independently, H or (C1-C4)-alkyl,

Rwithis a (C1-C6)-alkyl, optionally substituted by 1, 2 or 3 groups R205; cyclopropyl, cyclopropylmethyl, cyclopentyl, cyclopentylmethyl, cyclohexyl, cyclohexylmethyl; -(CR245R250)0-3is phenyl, optionally substituted 1 or 2 groups R200; -(CR245R250)0-3-pyridyl, optionally substituted by 1 or 2 R200; -(CR245R250)0-3-piperazinil; -(CR245R250)0-3-pyrrolidinyl or -(CR245R250)0-3-piperidinyl; each of the above geterotsiklicheskikh group optionally substituted by 1 or 2 groups R210;

R200in each case chosen, independently, from (C1-C4)-alkyl, optionally substituted 1 or 2 groups R205; HE and halogen;

R205in each case, in baraut, regardless of the numbers (1-C4)-alkyl, halogen, -OH, -SH, -C≡N, -CF3and (C1-C4)-alkoxy;

R210in each case chosen, independently, from (C1-C4)-alkyl, optionally substituted 1 or 2 groups R205; halogen; (C1-C4)-alkoxy; OCF3; NH2; NH((C1-C6)-alkyl); NH((C1-C6)-alkyl)((C1-C6)-alkyl); and HE CO- ((C1-C4)-alkyl); where

R245and R250in each case chosen, independently, from H, (C1-C4)-hydroxyalkyl, (C1-C4)-alkoxy, or

R245and R250taken together with the carbon atom to which they are attached, to form carbocycle of 3, 5 or 6 carbon atoms.

Preferred compounds of formulas I, I-1 and I-2 are the compounds of formula I-5, i.e. compounds of formulas I, I-1 or I-2, in which

RNrepresents-C(=O)-(CRR')0-6R100; and

R100represents aryl, heteroaryl or heterocyclyl, where the cyclical part of each group optionally substituted by 1, 2 or 3 groups selected, independently, from

-OR, -NO2, (C1-C6)-alkyl, halogen, -C≡N, -OCF3, -CF3, -(CH2)0-4-O-P(=O)(OR)(OR'), -(CH2)0-4-CO-NR105R'105, -(CH2)0-4-O-(CH2)0-4-CONR102R102', -(CH2)0-4 -CO-((C1-C12)-alkyl), -(CH2)0-4-CO-((C2-C12-alkenyl), -(CH2)0-4-CO-((C2-C12)-quinil), -(CH2)0-4-CO-(CH2)0-4-((C3-C7)-cycloalkyl), -(CH2)0-4-R110, -(CH2)0-4-R120, -(CH2)0-4-R130, -(CH2)0-4-CO-R110, -(CH2)0-4-CO-R120, -(CH2)0-4-CO-R130, -(CH2)0-4-CO-

R140, -(CH2)0-4-CO-O-R150, -(CH2)0-4-SO2-NR105R'105, -(CH2)0-4SO is((C1-C8)-alkyl), -(CH2)0-4-SO2-((C1-C12)-alkyl), -(CH2)0-4-SO2-(CH2)0-4-((C3-C7)-cycloalkyl), -(CH2)0-4-N(R150)-CO-O-R150, -(CH2)0-4-N(R150)-CO-N(R150)2, -(CH2)0-4-N(R150)-CS-

N(R150)2, -(CH2)0-4-N(R150)-CO-R105, -(CH2)0-4-NR105R'105, -(CH2)0-4-R140, -(CH2)0-4-O-CO-((C1-C6)-alkyl), -(CH2)0-4-O-P(O)-(O-R110)2, -(CH2)0-4-O-CO-N(R150)2, -(CH2)0-4-O-CS-N(R150)2, -(CH2)0-4-O-(R150), -(CH2)0-4-O-R150'-COOH, -(CH2)0-4-S-(R150), -(CH2)0-4-N(R150)-SO2-R105,-(CH 2)0-4-((C3-C7)-cycloalkyl), (C2-C10-alkenyl or (C2-C10)-quinil.

Preferred compounds of formula I-5 include compounds in which

RNrepresents-C(=O)-R100; and

R100represents aryl or heteroaryl, where the cyclical part of each group optionally substituted by 1, 2 or 3 groups selected, independently, from

-OR, -NO2, (C1-C6)-alkyl, halogen, -C≡N, -OCF3, -CF3, -(CH2)0-4-O-P(=O)(OR)(OR'), -(CH2)0-4-CO-NR105R'105, -(CH2)0-4-O-(CH2)0-4-CONR102R102', -(CH2)0-4-CO-((C1-C12)-alkyl), -(CH2)0-4-CO-((C2-C12-alkenyl), -(CH2)0-4-CO-((C2-C12)-quinil), -(CH2)0-4-CO-(CH2)0-4-((C3-C7)-cycloalkyl), -(CH2)0-4-R110, -(CH2)0-4-R120, -(CH2)0-4-R130, -(CH2)0-4-CO-R110, -(CH2)0-4-CO-R120, -(CH2)0-4-CO-R130, -(CH2)0-4-CO-

R140, -(CH2)0-4-CO-O-R150, -(CH2)0-4-SO2-NR105R'105, -(CH2)0-4SO is((C1-C8)-alkyl), -(CH2)0-4-SO2-((C1-C12)-alkyl), -(CH2)0-4-SO2-(CH2)0-4- (( 3-C7)-cycloalkyl), -(CH2)0-4-N(R150)-CO-O-R150, -(CH2)0-4-N(R150)-CO-N(R150)2, -(CH2)0-4-N(R150)-CS-N

(R150)2, -(CH2)0-4-N(R150)-CO-R105, -(CH2)0-4-NR105R'105, -(CH2)0-4-R140, -(CH2)0-4-O-CO-((C1-C6)-alkyl), -(CH2)0-4-O-P(O)-(O-R110)2, -(CH2)0-4-O-CO-N(R150)2, -(CH2)0-4-O-CS-N(R150)2, -(CH2)0-4-O-(R150), -(CH2)0-4-O-R150'-COOH, -(CH2)0-4-S-(R150), -(CH2)0-4-N(R150)-SO2-R105, -(CH2)0-4-((C3-C7)-cycloalkyl), (C2-C10-alkenyl or (C2-C10)-quinil.

Preferred compounds of formula I-5 are also connections

RNrepresents-C(=O)-aryl or-C(=O)-heteroaryl, where the cyclical part of each group optionally substituted by 1, 2 or 3 groups selected, independently, from

-OR, -NO2, (C1-C6)-alkyl, halogen, -C≡N, -OCF3, -CF3, -(CH2)0-4-CO-NR105R'105, -(CH2)0-4-O-(CH2)0-4-CONR102R102', -(CH2)0-4-CO-((C1-C12)-alkyl), -(CH2)0-4-CO-((C2-C12-alkenyl), -(CH2)0-4-CO-((C 2-C12)-quinil), -(CH2)0-4-R110, -(CH2)0-4-R120, -(CH2)0-4-R130,

-(CH2)0-4-CO-R110, -(CH2)0-4-CO-R120, -(CH2)0-4-CO-R130, -(CH2)0-4-CO-R140, -(CH2)0-4-CO-O-

R150, -(CH2)0-4-SO2-NR105R'105, -(CH2)0-4SO is((C1-C8)-alkyl), -(CH2)0-4-SO2-((C1-C12)-alkyl), -(CH2)0-4-N(R150)-CO-O-R150, -(CH2)0-4-N(R150)-CO-N(R150)2, -(CH2)0-4-N(R150)-CO-R105, -(CH2)0-4-NR105R'105, -(CH2)0-4-R140, (CH2)0-4-O-CO-((C1-C6)-alkyl), -(CH2)0-4-O-CO-N(R150)2, -(CH2)0-4-O-(R150), -(CH2)0-4-N(R150)-SO2-R105, -(CH2)0-4-((C3-C7)-cycloalkyl), (C2-C10-alkenyl or (C2-C10)-quinil.

Other preferred compounds of formula I-5 include compounds in which

RNrepresents-C(=O)-aryl or-C(=O)-heteroaryl, where the cyclical part of each group optionally substituted by 1 or 2 groups selected, independently, from

(C1-C6)-alkyl, halogen, -(CH2)0-4-CO-NR105R'105, -(CH2) 0-4-O-CO-N(R150)2,

-(CH2)0-4-N(R150)-SO2-R105, -(CH2)0-4-SO2-NR105R'105-(C3-C7)-cycloalkyl, (C2-C10-alkenyl, -(CH2)0-4-R110, -(CH2)0-4-R120, -(CH2)0-4-R130or (C2-C10)-quinil.

Other preferred compounds of formula I-5 include compounds in which

RNrepresents a

where sub is a hydrogen or a (C1-C6)-alkyl, halogen, -(CH2)0-4-CO-NR105R'105, -(CH2)0-4-O-CO-N(R150)2, -(CH2)0-4-N(R150)-SO2-R105, -(CH2)0-4-SO2-NR105R'105-(C3-C7-cycloalkyl -(C2-C10)-alkenyl, -(CH2)0-4-R110,

-(CH2)0-4-R120, -(CH2)0-4-R130or (C2-C10)-quinil.

The preferred stereocilia compounds of the formula I is

(I)

Preferred compounds of formula X are the compounds of formula X-1, i.e. the compounds of formula X, in which

R1represents aryl, heteroaryl, heterocyclyl -(C1-C6-alkylaryl -(C1-C6-alkylglycerol or -(C1- 6)-Alkylglucoside, where the cyclical part of each substituent optionally substituted by 1, 2, 3 or 4 groups selected, independently, from halogen, -OH, -SH, -C≡N, -NO2, -NR105R'105, -CO2R, -N(R)COR', or-N(R)SO2R', -C(=O)-(C1-C4)-alkyl, -SO2-amino, -SO2-mono - or-dialkylamino, -C(=O)-amino, -C(=O)-mono - or-dialkylamino, -SO2-(C1-C4)-alkyl, or

(C1-C6)-alkoxy, optionally substituted by 1, 2 or 3 groups selected, independently, from halogen, or

(C3-C7-cycloalkyl, optionally substituted by 1, 2 or 3 groups selected, independently, from halogen, -OH, -SH, -C≡N, -CF3, (C1-C3)-alkoxy, amino, -(C1-C6)-alkyl and mono - or dialkylamino, or

(C1-C10)-alkyl, optionally substituted by 1, 2 or 3 groups selected, independently, from halogen, -OH, -SH, -C≡N, -CF3, (C1-C3)-alkoxy, amino, mono - or dialkylamino and -(C1-C3)-alkyl, or

(C2-C10)-alkenyl or (C2-C10)-quinil, each of which is optionally substituted by 1, 2 or 3 groups selected, independently, from halogen, -OH, -SH, -C≡N, -CF3, (C1-C3)-alkoxy, amino, (C1-C6)-alkyl and mono - or dialkylamino; and heterocyclyl the group also optional samewe is and oxo.

Preferred compounds of formula X-1 are also connections

R1represents -(C1-C6-alkylaryl -(C1-C6-alkylglycerol or -(C1-C6)-Alkylglucoside, where the cyclical part of each substituent optionally substituted by 1, 2, 3 or 4 groups selected, independently, from halogen, -OH, -SH, -C≡N, -NO2, -NR105R'105, -CO2R, -N(R)COR', or-N(R)SO2R', -C(=O)-(C1-C4)-alkyl, -SO2-amino, -SO2-mono - or-dialkylamino, -C(=O)-amino, -C(=O)-mono - or-dialkylamino, -SO2-(C1-C4)-alkyl, or

(C1-C6)-alkoxy, optionally substituted by 1, 2 or 3 groups selected, independently, from halogen, or

(C3-C7-cycloalkyl, optionally substituted by 1, 2 or 3 groups selected, independently, from halogen, -OH, -SH, -C≡N, -CF3, (C1-C3)-alkoxy, amino, -(C1-C6)-alkyl and mono - or dialkylamino, or

(C1-C10)-alkyl, optionally substituted by 1, 2 or 3 groups selected, independently, from halogen, -OH, -SH, -C≡N, -CF3, (C1-C3)-alkoxy, amino, mono - or dialkylamino and -(C1-C3)-alkyl, or

(C2-C10)-alkenyl or (C2-C10)-quinil, each of which is optionally substituted by 1, 2 or 3 groups, is abusive, independently from halogen, -OH, -SH, -C≡N, -CF3, (C1-C3)-alkoxy, amino, (C1-C6)-alkyl and mono - or dialkylamino; and heterocyclyl the group is also optionally substituted by oxo.

Preferred compounds of formula X-1 are also connections

R1represents -(CH2)-aryl, -(CH2-heteroaryl or -(CH2)-heterocyclyl, where the cyclical part of each substituent optionally substituted by 1, 2, 3 or 4 groups selected, independently, from halogen, -OH, -SH, -C≡N, -NO2, -NR105

R'105, -CO2R, -N(R)COR', or-N(R)SO2R', -C(=O)-(C1-C4)-alkyl, -SO2-amino, -SO2-mono - or-dialkylamino, -C(=O)-amino, -C(=O)-mono - or-dialkylamino, -SO2-(C1-C4)-alkyl, or

(C1-C6)-alkoxy, optionally substituted by 1, 2 or 3 groups selected, independently, from halogen, or

(C3-C7-cycloalkyl, optionally substituted by 1, 2 or 3 groups selected, independently, from halogen, -OH, -SH, -C≡N, -CF3, (C1-C3)-alkoxy, amino, -(C1-C6)-alkyl and mono - or dialkylamino, or

(C1-C10)-alkyl, optionally substituted by 1, 2 or 3 groups selected, independently, from halogen, -OH, -SH, -C≡N, -CF3, (C1-C3)-alkoxy, amino, mono - or dial the laminitis and -(C 1-C3)-alkyl, or

(C2-C10)-alkenyl or (C2-C10)-quinil, each of which is optionally substituted by 1, 2 or 3 groups selected, independently, from halogen, -OH, -SH, -C≡N, -CF3, (C1-C3)-alkoxy, amino, (C1-C6)-alkyl and mono - or dialkylamino; and heterocyclyl the group is also optionally substituted by oxo.

Preferred compounds of formula X-1 are also connections

R1represents-CH2-phenyl or-CH2-pyridinyl, where the cyclical part of each substituent optionally substituted by 1, 2, 3 or 4 groups selected, independently, from halogen, (C1-C4)-alkoxy, hydroxy, -NO2and

(C1-C4)-alkyl, optionally substituted by 1, 2 or 3 substituents selected, independently, from halogen, HE, SH, NH2, NH((C1-C6)-alkyl), N-((C1-C6)-alkyl)((C1-C6)-alkyl, -C≡N, -CF3.

Preferred compounds of formula X-1 are also connections

R1represents-CH2-phenyl or-CH2-pyridinyl where the phenyl or pyridinoline cycles, each optionally substituted by 1 or 2 groups selected, independently, from halogen, (C1-C2)-alkyl, (C1-C2)-alkoxy, hydroxy, -CF3and-NO .

Preferred compounds of formula X-1 are compounds in which

R1represents-CH2-phenyl, where the phenyl cycle optionally substituted 2 groups selected, independently, from halogen, (C1-C2)-alkyl, (C1-C2)-alkoxy, hydroxy, and-NO2.

Preferred compounds of formula X-1 are also compounds in which R1represents benzyl or 3,5-diferensial.

Preferred compounds of formula X or X-1 are the compounds of formula X-2, i.e. compounds of formula X or X-1, in which

R2and R3chosen, independently, from H or (C1-C6)-alkyl, optionally substituted by 1, 2 or 3 substituents selected from the group consisting of (C1-C3)-alkyl, halogen, -OH, -SH, -C≡N, -CF3, (C1-C3)-alkoxy and-NR1-aR1-b.

Preferred compounds of formula X-2 are compounds in which

Rwithselected from the group consisting of (C1-C10)-alkyl, optionally substituted by 1, 2 or 3 groups selected, independently, from the group consisting of

R205, -OC=ONR235R240, -S(=O)0-2((C1-C6)-alkyl), -SH, -NR235C=ONR235R240, -C=ONR235R240and-S(=O)2NR235R240; -(CH2)0-3-(C3-C8)-cyclo is Lila, where cycloalkyl optionally substituted by 1, 2 or 3 groups selected, independently, from the group consisting of R205, -CO2H and CO2-((C1-C4)-alkyl); -(CR245R250)0-4-aryl;

-(CR245R250)0-4-heteroaryl; -(CR245R250)0-4-geterotsiklicheskie; -[C(R255)(R260)]1-3-CO-N(R255)2; -CH(aryl)2; -CH(heteroaryl)2; -CH(heteroseksualci)2; -CH(aryl)(heteroaryl); -CO-NR235R240; -(CH2)0-1-CH((CH2)0-6-OH)-(CH2)0-1-aryl; -(CH2)0-1-CHRS-6-(CH2)0-1-heteroaryl; -CH(-aryl or-heteroaryl)-CO-O((C1-C4)-alkyl); -CH(-CH2-OH)-CH(OH)-phenyl-NO2; ((C1-C6)-alkyl)-O-((C1-C6)-alkyl) -;- CH2-NH-CH2-CH(-O-CH2-CH3)2; -N and -(CH2)0-6-C(=NR235)(NR235R240); where

each aryl optionally substituted by 1, 2 or 3 R200;

each heteroaryl optionally substituted by 1, 2, 3 or 4 R200;

each heteroseksualci optionally substituted by 1, 2, 3 or 4 R210;

R200in each case chosen, independently, from the group consisting of (C1-C6)-alkyl, optionally substituted by 1, 2 or 3 groups R205; HE; -NO2; halogen; -CO2N; C≡N; -(CH2)0-4-CO-NR220R225 ; -(CH2)0-4-CO-((C1-C12)-alkyl);

-(CH2)0-4-CO2R215and -(CH2)0-4-O-((C1-C6)-alkyl, optionally substituted by 1, 2, 3, or 5-F);

where each aryl group in each case is optionally substituted by 1, 2, or 3 groups that represent, independently, R205, R210or (C1-C6)-alkyl, substituted 1, 2, or 3 groups that represent, independently, R205or R210;

where each heterocytolysine group in each case is optionally substituted by 1, 2, or 3 groups that represent, independently, R210;

where each heteroaryl group in each case is optionally substituted by 1, 2, or 3 groups that represent, independently, R205, R210or (C1-C6)-alkyl, substituted 1, 2, or 3 groups that represent, independently, R205or R210;

R205in each case chosen, independently, from the group consisting of (C1-C6)-alkyl, halogen, -OH, -O-phenyl, -SH, -C≡N, -CF3, (C1-C6)-alkoxy, NH2,

NH((C1-C6)-alkyl) and N((C1-C6)-alkyl)((C1-C6)-alkyl);

R210in each case chosen, independently, from the group consisting of (C1-C6)-alkyl, optionally substituted by 1, 2, and 3 groups of R 205; halogen; (C1-C6)-alkoxy, (C1-C6)-halogenoalkane; -NR220R225; OH; C≡N; and (C3-C7)-cycloalkyl, optionally substituted by 1, 2 or 3 groups R205; -CO-((C1-C4)-alkyl);

-SO2-NR235R240; -CO-NR235R240; -SO2-((C1-C4)-alkyl) and =O, where

R215in each case chosen, independently, from the group consisting of (C1-C6)-alkyl, (CH2)0-2-aryl, (C3-C7)-cycloalkyl, (CH2)0-2-heteroaryl and (CH2)0-2-geterotsiklicheskie, where the aryl group in each case is optionally substituted by 1, 2, or 3 groups that represent, independently, R205or R210; where heterocytolysine group in each case is optionally substituted by 1, 2 or 3 R210; where each heteroaryl group in each case is optionally substituted by 1, 2 or 3 R210;

R220and R225in each case chosen, independently, from the group consisting of-H,

-(C1-C6)-alkyl, hydroxy-(C1-C6)-alkyl, amino-(C1-C6)-alkyl, halogen-(C1-C6)-alkyl, (C3-C7)-cycloalkyl, -((C1-C6)-alkyl)-O-((C1-C3)-alkyl), -aryl, -heteroaryl and-geterotsiklicheskie, where the aryl group in each SL is tea is optionally substituted 1, 2 or 3 groups R270each heteroaryl is optionally substituted by 1, 2, 3 or 4 R200each heteroseksualci is optionally substituted by 1, 2, 3 or 4 R210where

R270in each case represents, independently, R205, (C1-C6)-alkyl, optionally substituted by 1, 2 or 3 groups R205; halogen; (C1-C6)-alkoxy, (C1-C6)-halogenoalkane; NR235R240; OH; C≡N; -CO-((C1-C4)-alkyl) and =O, where heterocytolysine group in each case is optionally substituted by 1, 2 or 3 groups R205; where each heteroaryl group in each case is optionally substituted by 1, 2 or 3 groups R205;

R235and R240in each case represent, independently, H or (C1-C6)-alkyl;

R245and R250in each case chosen, independently, from the group consisting of H, (C1-C4)-alkyl, (C1-C4)-hydroxyalkyl, (C1-C4)-alkoxy, (C1-C4)-halogenoalkane, or

R245and R250taken together with the carbon atom to which they are attached, to form carbocycle of 3, 4, 5, 6 or 7 carbon atoms, where carbocycle optionally substituted 1 or 2 groups that represent, independently, HE, methyl, Cl, F, och3, CF3, NO2or CN;

255and R260in each case chosen, independently, from the group consisting of H; and (C1-C6)-alkyl, optionally substituted by 1, 2 or 3 groups R205; -(CH2)0-4-(C3-C7)-cycloalkyl, optionally substituted by 1, 2 or 3 groups R205; -((C1-C4)-alkyl)aryl; -((C1-C4)-alkyl)heteroaryl; -((C1-C4)-alkyl)geterotsiklicheskie; aryl; heteroaryl; geterotsiklicheskie; -(CH2)1-4-R265-(CH2)0-4-aryl; -(CH2)1-4-R265-(CH2)0-4-heteroaryl and -(CH2)1-4-R265-(CH2)0-4-geterotsiklicheskie; where

R265in each case represents, independently, -O-, -S - or-N((C1-C6)-alkyl)-;

each aryl or phenyl optionally substituted by 1, 2, or 3 groups that represent, independently, R205, R210or (C1-C6)-alkyl, substituted 1, 2, or 3 groups that represent, independently, R205or R210.

Preferred compounds of formula X-2 are compounds in which

Rwithrepresents -(CR245R250)0-4-aryl or -(CR245R250)0-4-heteroaryl, where aryl and heteroaryl optionally substituted by 1, 2 or 3 groups R200.

Preferred compounds of formula X-2 are also connections to the verge

Rwithrepresents -(CR245R250)-aryl or -(CR245R250-heteroaryl, where each aryl and heteroaryl optionally substituted by 1, 2 or 3 groups R200.

Preferred compounds of formula X-2 are also connections

Rwithrepresents -(CH2)-aryl or -(CH2-heteroaryl, where each aryl and heteroaryl optionally substituted by 1, 2 or 3 groups selected from HE, " NO2, halogen, -CO2N, C≡N, -(CH2)0-4-CO-NR220R225, -(CH2)0-4-CO-((C1-C12)-alkyl) and -(CH2)0-4-SO2-NR220R225.

Preferred compounds of formula X-2 are also connections

Rwithrepresents -(CH2)-aryl, where aryl optionally substituted by 1, 2 or 3 groups selected from HE, " NO2, halogen, -CO2N and C≡N.

Preferred compounds of formula X-2 are also connections

Rwithrepresents -(CH2)-phenyl, where phenyl optionally substituted by 1, 2 or 3 groups selected from HE, " NO2, halogen, -CO2N and C≡N.

Preferred compounds of formula X-2 are also compounds in which Rwithrepresents benzyl.

Other preferred compounds of formula X, X-1 or X-2 are the joint is of the formula X-3, i.e. compounds of formula X, X-1 or X-2, in which

RNrepresents a

where

R4represents NH2, -NH-(CH2)n6-R4-1-The other8, -NR50C(O)R5or-NR50CO2R51,

where

n6is 0, 1, 2 or 3;

n7is 0, 1, 2 or 3;

R4-1selected from the group consisting of-SO2-((C1-C8)-alkyl), -SO-((C1-C8)-alkyl), -S-((C1-C8)-alkyl), -S-CO-((C1-C6)-alkyl), -SO2-NR4-2R4-3; -CO-(C1-C2)-alkyl, -CO-NR4-3R4-4;

R4-2and R4-3represent, independently, H, (C1-C3)-alkyl or (C3-C6-cycloalkyl;

R4-4represents alkyl, phenylalkyl, (C2-C4-alkanoyl or phenylalkanoic;

R5is cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl, where each cycloalkyl group optionally substituted by one or two groups representing a (C1-C6)-alkyl, preferably - (C1-C2)-alkyl, (C1-C6)-alkoxy, preferably - (C1-C2)-alkoxy, CF3, OH, NH2, NH((C1-C6)-alkyl), N((C1-C6)-alkyl)((C1-C6)-alkyl), halogen, CN or NO2; or cycloalkyl group substituted by 1 the 2 groups, represent, independently, CF3, Cl, F, methyl, ethyl or cyano; (C1-C6)-alkyl, optionally substituted by 1, 2 or 3 groups which are, independently, halogen,

-NR6R7, (C1-C4)-alkoxy, (C5-C6-heteroseksualci, (C5-C6-heteroaryl, phenyl, (C3-C7-cycloalkyl, -S-(C1-C4)-alkyl, -SO2-(C1-C4)-alkyl, -CO2N, -CONR6R7, -CO2-(C1-C4)-alkyl or phenyloxy; heteroaryl, optionally substituted by 1, 2 or 3 groups which are, independently, (C1-C4)-alkyl, (C1-C4)-alkoxy, halogen, (C1-C4-halogenated or HE; heteroseksualci, optionally substituted by 1, 2 or 3 groups which are, independently, (C1-C4)-alkyl, (C1-C4)-alkoxy, halogen or (C2-C4-alkanoyl; phenyl, optionally substituted by 1, 2, 3, or 4 groups that represent, independently, halogen, HE, (C1-C4)-alkyl, (C1-C4)-alkoxy or (C1-C4-halogenated; and-NR6R7; where

R6and R7chosen, independently, from the group consisting of H, (C1-C6)-alkyl, (C2-C6)-alkanoyl, phenyl, -SO2-(C1-C4)-alkyl and phenyl-(C1-C4)-alkyl;

R 8selected from the group consisting of-SO2-heteroaryl, optionally substituted 1 or 2 groups that represent, independently, (C1-C4)-alkyl or halogen; -SO2-aryl, -SO2-geterotsiklicheskie, -C(O)other9, geterotsiklicheskie, -S-(C2-C4)-alkanoyl, where

R9represents phenyl-(C1-C4)-alkyl, (C1-C6)-alkyl or H;

R50represents H or (C1-C6)-alkyl;

R51selected from the group consisting of phenyl-(C1-C4)-alkyl, (C1-C6)-alkyl, optionally substituted by 1, 2 or 3 groups which are, independently, halogen, cyano, -NR6R7-C(O)NR6R7, (C3-C7-cycloalkyl or -(C1-C4)-alkoxy; geterotsiklicheskie, optionally substituted 1 or 2 groups that represent, independently, (C1-C4)-alkyl, (C1-C4)-alkoxy, halogen, (C2-C4-alkanoyl, phenyl-

(C1-C4)-alkyl and-SO2-(C1-C4)-alkyl; geterotsiklicheskikh, optionally substituted 1 or 2 groups that represent, independently, (C1-C4)-alkyl,

(C1-C4)-alkoxy, halogen, (C2-C4-alkanoyl, phenyl-(C1-C4)-alkyl and-SO2-(C1-C4)-alkyl; alkenyl; Alki the sludge; heteroaryl, optionally substituted 1, 2, or 3 groups that represent, independently, HE, (C1-C4)-alkyl, (C1-C4)-alkoxy, halogen, NH2, NH((C1-C6)-alkyl) or N((C1-C6)-alkyl)((C1-C6)-alkyl); heteroaromatic, optionally substituted by 1, 2 or 3 groups which are, independently, (C1-C4)-alkyl, (C1-C4)-alkoxy, halogen, NH2, NH((C1-C6)-alkyl) or N((C1-C6)-alkyl)((C1-C6)-alkyl); phenyl; and (C3-C8)-cycloalkyl and cycloalkenyl, where phenyl, (C3-C8)-cycloalkyl and cycloalkenyl group substituted by optionally 1, 2, 3, 4, or 5 groups that represent, independently, halogen, CN, NO2, (C1-C6)-alkyl, (C1-C6)-alkoxy, (C2-C6-alkanoyl, (C1-C6-halogenated, (C1-C6)-halogenoalkane, hydroxy, (C1-C6-hydroxyalkyl, (C1-C6)-alkoxy-(C1-C6)-alkyl, (C1-C6)-dialkoxy, (C1-C6)-dialkoxy-(C1-C6)-alkyl or (C1-C6)-alkoxy-(C1-C6)-alkoxy.

Preferred compounds of formula X-3 are compounds in which

RNrepresents a

where

X is a (C1-C4)-alkylidene, optionally substituted by 1, 2 or 3 methyl groups, or-NR4-6; or

R4and R4-6combined with education -(CH2)n10-where

n10is 1, 2, 3 or 4;

Z is chosen from among communication, SO2SO, S and S(Oh);

Y is chosen from among N, (C1-C4)-halogenoalkane; and (C5-C6)-geterotsiklicheskie containing at least one N, O or S; phenyl; HE; -N(Y1)(Y2); And (C1-C10)-alkyl, optionally substituted by 1-3 substituents, which may be the same or different and are selected from among halogen, hydroxy, alkoxy, dialkoxy, halogenoalkane; and (C3-C8)-cycloalkyl, optionally substituted by 1, 2 or 3 groups selected, independently, from (C1-C3)-alkyl and halogen; alkoxy; phenyl, optionally substituted with halogen, (C1-C4)-alkyl, (C1-C4)-alkoxy, CN or NO2; phenyl-(C1-C4)-alkyl, optionally substituted with halogen, (C1-C4)-alkyl, (C1-C4)-alkoxy, CN or NO2; where

Y1and Y2are the same or different and represent H; and (C1-C10)-alkyl, optionally substituted by 1, 2 or 3 substituents selected from the group consisting of halogen, (C1-C4)-alkoxy, ( 3-C8)-cycloalkyl and IT; and (C2-C6)-alkenyl; and (C2-C6-alkanoyl; phenyl; -SO2-(C1-C4)-alkyl; phenyl-(C1-C4)-alkyl and (C3-C8-cycloalkyl-(C1-C4)-alkyl; or

-N(Y1)(Y2) to form a cycle selected from the piperazinil, piperidinyl, morpholinyl and pyrrolidinyl, where each cycle is optionally substituted by 1, 2, 3, or 4 groups that represent, independently, (C1-C6)-alkyl, (C1-C6)-alkoxy, (C1-C6)-alkoxy-(C1-C6)-alkyl or halogen.

Preferred compounds of formula X-3 are compounds in which

X is a (C1-C4)-alkylidene, optionally substituted by 1, 2 or 3 methyl groups;

Z is chosen from among SO2SO, S and S(Oh);

Y is chosen from among N, (C1-C4)-halogenoalkane; and (C5-C6)-geterotsiklicheskie containing at least one N, O or S; phenyl; HE; -N(Y1)(Y2); And (C1-C10)-alkyl, optionally substituted by 1-3 substituents, which may be the same or different and are selected from the group consisting of halogen, hydroxy, alkoxy, dialkoxy, halogenoalkane; and (C3-C8)-cycloalkyl, optionally substituted by 1, 2 or 3 groups selected, independently, from (C1-C3)-Ala is La and halogen; alkoxy; phenyl, optionally substituted with halogen, (C1-C4)-alkyl,

(C1-C4)-alkoxy, CN or NO2; phenyl-(C1-C4)-alkyl, optionally substituted with halogen, (C1-C4)-alkyl, (C1-C4)-alkoxy, CN or NO2; where

Y1and Y2are the same or different and represent H; and (C1-C6)-alkyl, optionally substituted by 1, 2 or 3 substituents selected from the group consisting of halogen, (C1-C4)-alkoxy, (C3-C8)-cycloalkyl and IT; and (C2-C6)-alkenyl; and (C2-C6-alkanoyl; phenyl; -SO2-(C1-C4)-alkyl; phenyl-(C1-C4)-alkyl or (C3-C8-cycloalkyl-(C1-C4)-alkyl; or

-N(Y1)(Y2) to form a cycle selected from the piperazinil, piperidinyl, morpholinyl and pyrrolidinyl, where each cycle is optionally substituted by 1, 2, 3, or 4 groups that represent, independently, (C1-C6)-alkyl, (C1-C6)-alkoxy, (C1-C6)-alkoxy-(C1-C6)-alkyl or halogen.

Preferred compounds of formula X-3 are compounds in which

RNrepresents a

and where R4represents NH2, -NH-(CH2)n6-R4-1-The other8, -NR 50C(O)R5or-NR50CO2R51where

n6is 0, 1, 2 or 3;

n7is 0, 1, 2 or 3;

R4-1selected from the group consisting of-SO2-((C1-C8)-alkyl), -SO-((C1-C8)-alkyl), -S-((C1-C8)-alkyl), -S-CO-((C1-C6)-alkyl), -SO2-NR4-2R4-3; -CO-(C1-C2)-alkyl, -CO-NR4-3R4-4;

R4-2and R4-3represent, independently, H, (C1-C3)-alkyl or (C3-C6-cycloalkyl;

R4-4represents alkyl, phenylalkyl, (C2-C4-alkanoyl or phenylalkanoic;

R5is cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl, where each cycloalkyl group optionally substituted by one or two groups representing a (C1-C6)-alkyl, preferably - (C1-C2)-alkyl, (C1-C6)-alkoxy, preferably - (C1-C2)-alkoxy, CF3, OH, NH2, NH((C1-C6)-alkyl), N((C1-C6)-alkyl)((C1-C6)-alkyl), halogen, CN or NO2; or cycloalkyl group substituted by 1 or 2 groups that represent, independently, CF3, Cl, F, methyl, ethyl or cyano; (C1-C6)-alkyl, optionally substituted by 1, 2 or 3 groups which are, independently, halogen,

-NR6 R7, (C1-C4)-alkoxy, (C5-C6-heteroseksualci, (C5-C6-heteroaryl, phenyl, (C3-C7-cycloalkyl, -S-(C1-C4)-alkyl, -SO2-(C1-C4)-alkyl, -CO2N, -CONR6R7, -CO2-(C1-C4)-alkyl or phenyloxy; heteroaryl, optionally substituted by 1, 2 or 3 groups which are, independently, (C1-C4)-alkyl, (C1-C4)-alkoxy, halogen, (C1-C4-halogenated or HE; heteroseksualci, optionally substituted by 1, 2 or 3 groups which are, independently, (C1-C4)-alkyl, (C1-C4)-alkoxy, halogen or (C2-C4-alkanoyl; phenyl, optionally substituted by 1, 2, 3, or 4 groups that represent, independently, halogen, HE, (C1-C4)-alkyl, (C1-C4)-alkoxy or (C1-C4-halogenated; and-NR6R7; where

R6and R7chosen, independently, from the group consisting of H, (C1-C6)-alkyl, (C2-C6)-alkanoyl, phenyl, -SO2-(C1-C4)-alkyl and phenyl-(C1-C4)-alkyl;

R8selected from the group consisting of-SO2-heteroaryl, optionally substituted 1 or 2 groups that represent, independently, (C1-C4)-alkyl or halogen; -SO2-aryl, -SO 2-geterotsiklicheskie, -C(O)other9, geterotsiklicheskie, -S-(C2-C4)-alkanoyl, where

R9represents phenyl-(C1-C4)-alkyl, (C1-C6)-alkyl or H;

R50represents H or (C1-C6)-alkyl; and

R51selected from the group consisting of phenyl-(C1-C4)-alkyl, (C1-C6)-alkyl, optionally substituted by 1, 2 or 3 groups which are, independently, halogen, cyano, -NR6R7-C(O)NR6R7, (C3-C7-cycloalkyl or -(C1-C4)-alkoxy; geterotsiklicheskie, optionally substituted 1 or 2 groups that represent, independently, (C1-C4)-alkyl, (C1-C4)-alkoxy, halogen, (C2-C4-alkanoyl, phenyl-

(C1-C4)-alkyl and-SO2-(C1-C4)-alkyl; geterotsiklicheskikh, optionally substituted 1 or 2 groups that represent, independently, (C1-C4)-alkyl,

(C1-C4)-alkoxy, halogen, (C2-C4-alkanoyl, phenyl-(C1-C4)-alkyl and-SO2-(C1-C4)-alkyl; alkenyl; quinil; heteroaryl, optionally substituted 1, 2, or 3 groups that represent, independently, HE, (C1-C4)-alkyl, (C1-C4)-alkoxy, halogen, NH2, NH(C1-C6)-and the keel or N((C 1-C6)-alkyl)((C1-C6)-alkyl); heteroaromatic, optionally substituted by 1, 2 or 3 groups which are, independently, (C1-C4)-alkyl, (C1-C4)-alkoxy, halogen, NH2, NH((C1-C6)-alkyl) or N((C1-C6)-alkyl)((C1-C6)-alkyl); phenyl; and (C3-C8)-cycloalkyl and cycloalkenyl, where phenyl, (C3-C8)-cycloalkyl and cycloalkenyl group substituted by optionally 1, 2, 3, 4, or 5 groups that represent, independently, halogen, CN, NO2, (C1-C6)-alkyl, (C1-C6)-alkoxy, (C2-C6-alkanoyl, (C1-C6-halogenated, (C1-C6)-halogenoalkane, hydroxy, (C1-C6-hydroxyalkyl, (C1-C6)-alkoxy-(C1-C6)-alkyl, (C1-C6)-dialkoxy, (C1-C6)-dialkoxy-(C1-C6)-alkyl or (C1-C6)-alkoxy-(C1-C6)-alkoxy; and

Y represents a (C1-C10)-alkyl, optionally substituted by 1-3 substituents, which may be the same or different and are selected from among halogen, hydroxy, alkoxy, dialkoxy, halogenoalkane.

Preferred compounds of formula X-3 are also connections

Rwithis a (C1-C8)-Ala is l, optionally substituted by 1, 2 or 3 groups selected, independently, from the group consisting of R205, -OC=ONR235R240, -S(=O)0-2((C1-C6)-alkyl), -SH, -C=ONR235R240and-S(=O)2NR235R240; -(CH2)0-3-(C3-C8-cycloalkyl where cycloalkyl optionally substituted by 1, 2 or 3 groups selected, independently, from the group consisting of R205, -CO2H and CO2-((C1-C4)-alkyl); -(CR245R250)0-4-phenyl; -(CR245R250)0-4-heteroaryl;

-(CR245R250)0-4-heteroseksualci; -(CH2)0-1-CH((CH2)0-4-OH)-(CH2)0-1-phenyl; -(CH2)0-1-CHRS-6-(CH2)0-1-heteroaryl; -CH(-CH2-OH)-CH(OH)-phenyl-NO2; ((C1-C6)-alkyl)-O-((C1-C6)-alkyl)-or -(CH2)0-6-C(=NR235)(NR235R240); where

each aryl optionally substituted by 1, 2 or 3 R200;

each heteroaryl optionally substituted by 1, 2, 3 or 4 R200;

each heteroseksualci optionally substituted by 1, 2, 3 or 4 R210;

R200in each case represents, independently, (C1-C6)-alkyl, optionally substituted by 1, 2 or 3 groups R205; HE; -NO2; halogen; -CO2N; C≡N; -(CH2)0-4-CO-NR220R225; -(CH2)0-4WITH((C 1-C12)-alkyl); -(CH2)0-4-CO2R215or -(CH2)0-4-O-((C1-C6)-alkyl, optionally substituted by 1, 2, 3, or 5-F);

R205in each case represents, independently, (C1-C6)-alkyl, halogen, -OH, -O-phenyl, -SH, -C≡N, -CF3, (C1-C6)-alkoxy, NH2, NH((C1-C6)-alkyl) or N((C1-C6)-alkyl)((C1-C6)-alkyl);

R210in each case represents, independently, (C1-C6)-alkyl, optionally substituted by 1, 2 or 3 groups R205; halogen; (C1-C6)-alkoxy, (C1-C6)-halogenoalkane; -NR220R225; OH; C≡N; and (C3-C7-cycloalkyl, optionally substituted by 1, 2 or 3 groups R205; -CO-((C1-C4)-alkyl); -SO2-NR235R240; -CO-NR235R240; -SO2-((C1-C4)-alkyl) and =O, where

R215in each case represents, independently, (C1-C6)-alkyl, -(CH2)0-2-phenyl, (C3-C7-cycloalkyl, -(CH2)0-2-heteroaryl and -(CH2)0-2-heteroseksualci, where the phenyl group in each case is optionally substituted by 1, 2, or 3 groups that represent, independently, R205or R210; where heterocytolysine group in each case is not necessarily samewe the Noi 1, 2 or 3 R210; where each heteroaryl group in each case is optionally substituted by 1, 2 or 3 R210;

R220and R225in each case represent, independently, -H, -(C1-C6)-alkyl, hydroxy-(C1-C6)-alkyl, halogen-(C1-C6)-alkyl, -(C3-C7-cycloalkyl and((C1-C6)-alkyl)-O-((C1-C3)-alkyl);

R235and R240in each case represent, independently, H or (C1-C6)-alkyl;

R245and R250in each case represent, independently, H, (C1-C4)-alkyl, (C1-C4-hydroxyalkyl, (C1-C4)-alkoxy, (C1-C4)-halogenoalkane, or

R245and R250taken together with the carbon atom to which they are attached, to form carbocycle of 3, 4, 5, 6 or 7 carbon atoms.

Preferred compounds of formula X-3 are compounds in which

R1represents benzyl, optionally substituted by 1, 2, 3 or 4 groups selected, independently, from halogen, (C1-C4)-alkoxy, hydroxy and (C1-C4)-alkyl, optionally substituted by 1, 2 or 3 substituents from halogen, HE, SH, NH2, NH((C1-C6)-alkyl), N((C1-C6)-alkyl)((C1-C6)-alkyl), C≡N, CF3;

R2and 3chosen, independently, from H or (C1-C4)-alkyl, optionally substituted by 1 Deputy, selected from among halogen, -OH, -SH, -C≡N, -CF3, (C1-C3)-alkoxy, NH2, NH((C1-C6)-alkyl) and N((C1-C6)-alkyl)((C1-C6)-alkyl);

Rwithis a (C1-C8)-alkyl, optionally substituted by 1, 2 or 3 groups selected, independently, from among the R205, -SH, -C=ONR235R240and-S(=O)2NR235R240; -(CH2)0-3-(C3-C6-cycloalkyl where cycloalkyl optionally substituted by 1, 2 or 3 groups selected, independently, from among the R205, -CO2H and CO2-((C1-C4)-alkyl); -(CR245R250)0-4is phenyl, optionally substituted by 1, 2 or 3 R200; -(CR245R250)0-3-pyridyl; -(CR245R250)0-3-pyridazinyl; -(CR245R250)0-3-pyrimidinyl; -(CR245R250)0-3-pyrazinyl; -(CR245R250)0-3-furyl;

-(CR245R250)0-3-indolyl; -(CR245R250)0-3-thienyl; -(CR245R250)0-3-pyrrolyl; -(CR245R250)0-3-pyrazolyl; -(CR245R250)0-3-benzoxazolyl; -(CR245R250)0-3-imidazolyl; each of the above heteroaryl groups is optionally substituted by 1, 2, 3 or 4 R200/sub> ; -(CR245R250)0-3-imidazolidinyl;

(CR245R250)0-3-tetrahydrofuryl; (CR245R250)0-3-tetrahydropyranyl; (CR245R250)0-3-piperazinil; (CR245R250)0-3-pyrrolidinyl; (CR245R250)0-3-piperidinyl; (CR245R250)0-3-indolinyl; each of the above geterotsiklicheskikh group optionally substituted by 1, 2, 3 or 4 R210; (CH2)0-1-CH((CH2)0-4-OH)-(CH2)0-1-phenyl; -(CH2)0-1-CH((C1-C4-hydroxyalkyl)-

(CH2)0-1-pyridyl;

R200in each case represents, independently, (C1-C6)-alkyl, optionally substituted by 1, 2 or 3 groups R205; HE; -NO2; halogen; -CO2N; C≡N; -(CH2)0-4-CO-NR220R225; -(CH2)0-4-CO-((C1-C8)-alkyl); -(CH2)0-4-CO2R215and -(CH2)0-4-O-((C1-C6)-alkyl, optionally substituted by 1, 2, 3, or 5-F);

R205in each case represents, independently, (C1-C6)-alkyl, halogen, -OH, -O-phenyl, -SH, -C≡N, -CF3, (C1-C6)-alkoxy, NH2, NH((C1-C6)-alkyl) and N((C1-C6)-alkyl)((C1-C6)-alkyl);

R210in each case represents, independently, (C1-C6 )-alkyl, optionally substituted 1 or 2 groups R205; halogen; (C1-C4)-alkoxy, (C1-C4)-halogenoalkane; -NR220R225; OH; C≡N; and (C3-C7-cycloalkyl, optionally substituted 1 or 2 groups R205; -CO-((C1-C4)-alkyl); -SO2-NR235R240; -CO-NR235R240; -SO2-((C1-C4)-alkyl) and =O, where

R215in each case represents, independently, (C1-C6)-alkyl, (CH2)0-2-phenyl, (C3-C6-cycloalkyl, -(CH2)0-2-pyridyl, -(CH2)0-2-pyrrolyl, -(CH2)0-2-imidazolyl, -(CH2)0-2pirimidil, -(CH2)0-2-pyrrolidinyl, -(CH2)0-2-imidazolidinyl, -(CH2)0-2-piperazinil, -(CH2)0-2-piperidinyl and (CH2)0-2-morpholinyl, where the phenyl group in each case is optionally substituted 1 or 2 groups that represent, independently, R205or R210; where each heterocytolysine group in each case is optionally substituted by 1 or 2 R210; where each heteroaryl group in each case is optionally substituted by 1 or 2 R210;

R220and R225in each case represent, independently, -H, -(C1-C4)-alkyl, hydroxy-(C1-C4)-alkyl halogen-(C 1-C4)-alkyl, -(C3-C6-cycloalkyl and((C1-C4)-alkyl)-O-((C1-C2)-alkyl);

R235and R240in each case represent, independently, H or (C1-C6)-alkyl;

R245and R250in each case represent, independently, H, (C1-C4)-alkyl, (C1-C4-hydroxyalkyl, (C1-C4)-alkoxy, (C1-C4)-halogenoalkane, or

R245and R250taken together with the carbon atom to which they are attached, to form carbocycle of 3, 4, 5 or 6 carbon atoms.

Other preferred compounds of formula X-3 are compounds in which

X is a (C1-C3)-alkylidene, optionally substituted by 1 or 2 methyl groups;

Z represents SO2, SO, S, or C(O);

Y represents a (C1-C4-halogenated; HE; -N(Y1)(Y2); And (C1-C10)-alkyl, optionally substituted by 1 or 2 substituents, which may be the same or different and are selected from among halogen, hydroxy, (C1-C4)-alkoxy, (C1-C4)-dialkoxy and (C1-C4)-halogenoalkane; and (C1-C4)-alkoxy; phenyl, optionally substituted with halogen, (C1-C4)-alkyl, (C1-C4)-alkoxy, CN or NO2; and benzyl, it is certainly substituted with halogen, (C1-C4)-alkyl, (C1-C4)-alkoxy, CN or NO2; where

Y1and Y2are the same or different and represent H; and (C1-C6)-alkyl, optionally substituted by 1, 2 or 3 substituents selected from among halogen, (C1-C2)-alkoxy, (C3-C6)-cycloalkyl and IT; and (C2-C6-alkanoyl; phenyl; -SO2-(C1-C4)-alkyl; benzyl and (C3-C6-cycloalkyl-(C1-C2)-alkyl; or

-N(Y1)(Y2) to form a cycle selected from the piperazinil, piperidinyl, morpholinyl and pyrrolidinyl, where each cycle is optionally substituted by 1, 2, 3, or 4 groups that represent, independently, (C1-C6)-alkyl, (C1-C6)-alkoxy, (C1-C6)-alkoxy-(C1-C6)-alkyl or halogen.

Preferred compounds of formula X-3 are also the compounds of formula X-4, i.e. the compounds of formula X-3, in which

X is a (C1-C3)-alkylidene, optionally substituted 1 methyl group;

Z represents SO2, SO, S, or C(O);

Y is HE, -N(Y1)(Y2), phenyl, benzyl or (C1-C10)-alkyl, optionally substituted by 1 or 2 substituents, which may be the same or different and are selected from among halogen, hydroxy, methoxy, e is hydroxy, dimethoxy, diethoxy and CF3; where

Y1and Y2are the same or different and represent H; and (C1-C4)-alkyl, optionally substituted by 1 or 2 substituents selected from halogen, methoxy, ethoxy, cyclopropyl and HE; or

-N(Y1)(Y2) to form a cycle selected from the piperazinil, piperidinyl, morpholinyl and pyrrolidinyl, where each cycle is optionally substituted 1 or 2 groups that represent, independently, (C1-C4)-alkyl, (C1-C4)-alkoxy or halogen;

R1represents benzyl, optionally substituted by 1, 2 or 3 groups selected independently from among methyl, ethyl, n-propyl, isopropyl, hydroxymethyl, monohalogenated, dehalogenating, trihalomethyl, -CH2CF3, methoxymethyl, halogen, methoxy, ethoxy, n-propyloxy, isopropoxy and HE;

R2and R3represent, independently, H or (C1-C4)-alkyl,

Rwithis a (C1-C6)-alkyl, optionally substituted by 1, 2 or 3 groups R205; cyclopropyl, cyclopropylmethyl, cyclopentyl, cyclopentylmethyl, cyclohexyl, cyclohexylmethyl; -(CR245R250)0-3is phenyl, optionally substituted 1 or 2 groups R200; -(CR245R250)0-3-pyridyl, optionally substituted by 1 or 2 R 200; -(CR245R250)0-3-piperazinil; -(CR245R250)0-3-pyrrolidinyl or -(CR245R250)0-3-piperidinyl; each of the above geterotsiklicheskikh group optionally substituted by 1 or 2 groups R210;

R200in each case chosen, independently, from (C1-C4)-alkyl, optionally substituted 1 or 2 groups R205; HE and halogen;

R205in each case chosen, independently, from (C1-C4)-alkyl, halogen, -OH, -SH, -C≡N, -CF3and (C1-C4)-alkoxy;

R210in each case chosen, independently, from (C1-C4)-alkyl, optionally substituted 1 or 2 groups R205; halogen; (C1-C4)-alkoxy; OCF3; NH2; NH((C1-C6)-alkyl); NH((C1-C6)-alkyl)((C1-C6)-alkyl); and HE CO- ((C1-C4)-alkyl); where

R245and R250in each case chosen, independently, from H, (C1-C4)-hydroxyalkyl, (C1-C4)-alkoxy, or

R245and R250taken together with the carbon atom to which they are attached, to form carbocycle of 3, 5 or 6 carbon atoms.

Preferred compounds of formula X, X-1 and X-2 are the compounds of formula X-5, i.e. compounds of formula X, X-1 or X-2, in which

RNnot only is em a-C(=O)-(CRR') 0-6R100; and

R100represents aryl, heteroaryl or heterocyclyl, where the cyclical part of each group optionally substituted by 1, 2 or 3 groups selected, independently, from

-OR, -NO2, (C1-C6)-alkyl, halogen, -C≡N, -OCF3, -CF3, -(CH2)0-4-O-P(=O)(OR)(OR'), -(CH2)0-4-CO-NR105R'105, -(CH2)0-4-O-(CH2)0-4-CONR102R102', -(CH2)0-4-CO-((C1-C12)-alkyl), -(CH2)0-4-CO-((C2-C12-alkenyl), -(CH2)0-4-CO-((C2-C12)-quinil), -(CH2)0-4-CO-(CH2)0-4-((C3-C7)-cycloalkyl), -(CH2)0-4-R110, -(CH2)0-4-R120, -(CH2)0-4-R130, -(CH2)0-4-CO-R110, -(CH2)0-4-CO-R120, -(CH2)0-4-CO-R130, -(CH2)0-4-CO-

R140, -(CH2)0-4-CO-O-R150, -(CH2)0-4-SO2-NR105R'105, -(CH2)0-4SO is((C1-C8)-alkyl), -(CH2)0-4-SO2-((C1-C12)-alkyl), -(CH2)0-4-SO2-(CH2)0-4-((C3-C7)-cycloalkyl), -(CH2)0-4-N(R150)-CO-O-R150, -(CH2)0-4-N(R150)-CO-N(R150)2, -(CH2)0-4-N(R150)-CS-

N(R150)2, -(CH2)0-4-NR 150)-CO-R105, -(CH2)0-4-NR105R'105, -(CH2)0-4-R140, -(CH2)0-4-O-CO-((C1-C6)-alkyl), -(CH2)0-4-O-P(O)-(O-R110)2, -(CH2)0-4-O-CO-N(R150)2, -(CH2)0-4-O-CS-N(R150)2, -(CH2)0-4-O-(R150), -(CH2)0-4-O-R150'-COOH, -(CH2)0-4-S-(R150), -(CH2)0-4-N(R150)-SO2-R105, -(CH2)0-4-((C3-C7)-cycloalkyl), (C2-C10-alkenyl or (C2-C10)-quinil.

Preferred compounds of formula X-5 are compounds in which

RNrepresents-C(=O)-R100; and

R100represents aryl or heteroaryl, where the cyclical part of each group optionally substituted by 1, 2 or 3 groups selected, independently, from

-OR, -NO2, (C1-C6)-alkyl, halogen, -C≡N, -OCF3, -CF3, -(CH2)0-4-O-P(=O)(OR)(OR'), -(CH2)0-4-CO-NR105R'105, -(CH2)0-4-O-(CH2)0-4-CONR102R102', -(CH2)0-4-CO-((C1-C12)-alkyl), -(CH2)0-4-CO-((C2-C12-alkenyl), -(CH2)0-4-CO-((C2-C12)-quinil), -(CH2)0-4-CO-(CH2)0-4-((C3-C7)-cycloalkyl), -(CH2)0-4-R110, -(CH2) -R120, -(CH2)0-4-R130, -(CH2)0-4-CO-R110, -(CH2)0-4-CO-R120, -(CH2)0-4-CO-R130, -(CH2)0-4-CO-

R140, -(CH2)0-4-CO-O-R150, -(CH2)0-4-SO2-NR105R'105, -(CH2)0-4SO is((C1-C8)-alkyl), -(CH2)0-4-SO2-((C1-C12)-alkyl), -(CH2)0-4-SO2-(CH2)0-4-((C3-C7)-cycloalkyl), -(CH2)0-4-N(R150)-CO-O-R150, -(CH2)0-4-N(R150)-CO-N(R150)2, -(CH2)0-4-N(R150)-CS-N

(R150)2, -(CH2)0-4-N(R150)-CO-R105, -(CH2)0-4-NR105R'105, -(CH2)0-4-R140, -(CH2)0-4-O-CO-((C1-C6)-alkyl), -(CH2)0-4-O-P(O)-(O-R110)2, -(CH2)0-4-O-CO-N(R150)2, -(CH2)0-4-O-CS-N(R150)2, -(CH2)0-4-O-(R150), -(CH2)0-4-O-R150'-COOH, -(CH2)0-4-S-(R150), -(CH2)0-4-N(R150)-SO2-R105, -(CH2)0-4-((C3-C7)-cycloalkyl), (C2-C10-alkenyl or (C2-C10)-quinil.

Preferred compounds of formula X-5 are also connections

RNrepresents-C(=O)-aryl or-C(=O)-heteros is aryl, where the cyclical part of each group optionally substituted by 1, 2 or 3 groups selected, independently, from

-OR, -NO2, (C1-C6)-alkyl, halogen, -C≡N, -OCF3, -CF3, -(CH2)0-4-CO-NR105R'105, -(CH2)0-4-O-(CH2)0-4-CONR102R102', -(CH2)0-4-CO-((C1-C12)-alkyl), -(CH2)0-4-CO-((C2-C12-alkenyl), -(CH2)0-4-CO-((C2-C12)-quinil), -(CH2)0-4-R110, -(CH2)0-4-R120, -(CH2)0-4-R130,

-(CH2)0-4-CO-R110, -(CH2)0-4-CO-R120, -(CH2)0-4-CO-R130, -(CH2)0-4-CO-R140, -(CH2)0-4-CO-O-R150, -(CH2)0-4-SO2-NR105R'105, -(CH2)0-4SO is((C1-C8)-alkyl), -(CH2)0-4-SO2-((C1-C12)-alkyl), -(CH2)0-4-N(R150)-CO-O-R150, -(CH2)0-4-N(R150)-CO-N(R150)2, -(CH2)0-4-N(R150)-CO-R105, -(CH2)0-4-NR105R'105,

-(CH2)0-4-R140, (CH2)0-4-O-CO-((C1-C6)-alkyl), -(CH2)0-4-O-CO-N(R150)2, -(CH2)0-4-O-(R150), -(CH2)0-4-N(R150)-SO2-R105, -(CH2)0-4-((C3-C7)-cyclol the sludge), (C2-C10-alkenyl or (C2-C10)-quinil.

Other preferred compounds of formula X-5 are compounds in which

RNrepresents-C(=O)-aryl or-C(=O)-heteroaryl, where the cyclical part of each group optionally substituted by 1 or 2 groups selected, independently, from

(C1-C6)-alkyl, halogen, -(CH2)0-4-CO-NR105R'105, -(CH2)0-4-O-CO-N(R150)2,

-(CH2)0-4-N(R150)-SO2-R105, -(CH2)0-4-SO2-NR105R'105-(C3-C7)-cycloalkyl, (C2-C10-alkenyl, -(CH2)0-4-R110, -(CH2)0-4-R120, -(CH2)0-4-R130or (C2-C10)-quinil.

Other preferred compounds of formula X-5 are compounds in which RNrepresents a

where sub is a hydrogen or a (C1-C6)-alkyl, halogen, -(CH2)0-4-CO-NR105R'105, -(CH2)0-4-O-CO-N(R150)2, -(CH2)0-4-N(R150)-SO2-R105, -(CH2)0-4-SO2-NR105R'105-(C3-C7-cycloalkyl -(C2-C10)-alkenyl, -(CH2)0-4-R110,

-(CH2)0-4-R120, -(CH2)0- -R130or (C2-C10)-quinil.

The preferred stereochemistry of the compounds of the formula X is

In another aspect the invention relates to intermediate compounds of formula (IA)

where R1, R2, R3, RNand RChave the values specified above for compounds of formula I, and PROT represents a protective group for the amino group, the definition of which is given below.

In another aspect the invention relates to intermediate compounds of the formula (XA)

where R1, R2, R3, RNand RChave the values specified above for compounds of formula I, and PROT represents a protective group for the amino group, the definition of which is given below.

The invention also relates to methods for formation of compounds of formula (Y) of the compounds of the formula (AA), formula (I) or formula (X), suitable for the treatment and/or prevention of Alzheimer's disease. The formation of compounds of formula (Y) of the compounds of formula (AA), (I) or (X) may occur in vivo or in vitro.

The invention also relates to methods for the transformation of compounds of formula AA, I or X in the compounds of formula Y when exposed to compounds of formula AA, I, or X aquatic environments. The conversion can occur in vitro or in vivo.

The invention also about what is worn to a method of treatment of a patient, who has a disease or condition, or prevent the acquisition of the patient's disease or condition selected from the group consisting of Alzheimer's disease, contributing to the prevention or delay of onset of Alzheimer's, patients with mild cognitive impairment (MCI) and preventing or delaying the occurrence of Alzheimer's disease in these patients, which may develop from MCI to AD, down syndrome treatment, treatment of people with hereditary cerebral hemorrhage with amyloidosis (Dutch Type), the treatment of cerebral amyloid angiopathy and preventing its potential consequences, i.e. single and recurrent lobes bleeding, treating other degenerative dementias including dementias of mixed vascular and degenerative origin, dementia associated with Parkinson's disease, dementia associated with progressive supranuclear palsy, dementia associated with cortical basal degeneration, or Alzheimer's-type diffusion Taurus levy, including the introduction of those needing such treatment, a therapeutically effective amount of the compounds of formula (AA), (I) or (X) or its pharmaceutically acceptable salts.

In the embodiment of this method of treatment can be used when a disease is a disease of Alzheimer's.

In embodied and this method of treatment may help prevent or delay the appearance of Alzheimer's disease.

In the embodiment of this method of treatment can be applied when the disease is a mild cognitive impairment.

In the embodiment of this method of treatment can be applied when the disease is a syndrome.

In the embodiment of this method of treatment can be used when a disease is a hereditary cerebral hemorrhage with amyloidosis (Dutch Type).

In the embodiment of this method of treatment can be used when a disease is a cerebral amyloid angiopathy.

In the embodiment of this method of treatment can be used when a disease is a degenerative dementia.

In the embodiment of this method of treatment can be applied when the disease is an Alzheimer's-type diffusion Taurus Levi.

In the embodiment of this method of treatment can treat an existing disease.

In the embodiment of this method of treatment can prevent the development of disease.

In the embodiment of this method of treatment can be used therapeutically effective amount, comprising, in the case of oral administration, from about 0.1 mg/day to about 1000 mg/day; in the case of parenteral, sublingual, intranasal, vnutriobolochechnoe of administration is from about 0.5 mg/day to about 100 mg/day; in the case of the introduction method depots and implants - from approximately 05 mg/day to about 50 mg/day; in the case of local administration is from about 0.5 mg/day to about 200 mg/day; in the case of rectal administration is from about 0.5 mg to about 500 mg

In the embodiment of this method of treatment can be used therapeutically effective amount, comprising, in the case of oral administration, from about 1 mg/day to about 100 mg/day; and in the case of parenteral administration is from about 5 to about 50 mg daily.

In the embodiment of this method of treatment can be used therapeutically effective amounts of the components in the case of oral administration from about 5 mg/day to about 50 mg/day.

The invention also relates to pharmaceutical compositions comprising a compound of formula (AA), (I) or (X) or its pharmaceutically acceptable salt.

The invention also relates to the use of compounds of formula (AA), (I) or (X) or its pharmaceutically acceptable salts for obtaining medicines.

The invention also relates to a method of inhibiting beta-secretase activity, inhibiting cleavage of amyloid protein precursor (APP) in the reaction mixture in the website between Met596 and Asp597, the numbering of amino acid isotype of APP-695, or in the corresponding website isotype or mutant; inhibiting production of amyloid beta peptide (A-beta) in a cell; ingibirovany the production of amyloid plaque in an animal, and treating or preventing diseases, characterized by beta-amyloid deposits in the brain. Each of these methods includes the introduction of therapeutically effective amounts of compounds of formula (AA), (I) or (X) or its pharmaceutically acceptable salts.

The invention also relates to a method of inhibiting beta-secretase activity, including effects on specified beta secretshow activity of the compounds of formula (AA), (I) or (X) under conditions when there is an effective inhibitory amount of a compound of formula (Y) or its pharmaceutically acceptable salt.

In the embodiment in this way is used as a compound inhibiting the enzyme activity by 50% at a concentration of less than 50 microns.

In the embodiment in this way is used as a compound inhibiting the enzyme activity by 50% at a concentration of 10 μm or less.

In the embodiment in this way is used as a compound inhibiting the enzyme activity by 50% at a concentration of 1 μm or less.

In the embodiment in this way is used as a compound inhibiting the enzyme activity by 50% at a concentration of 10 nm or less.

In this embodiment the method comprises exposure to the specified connection on the specified beta secretase in vitro.

In this embodiment the method comprises exposure to the specified connection on the specified beta secretase in the cell.

In the embodiment of this method includes the t effect of the compounds on the specified beta secretase in the cage of the animal.

In this embodiment the method comprises exposure to the specified connection on the specified beta secretase in humans.

The invention also relates to a method for inhibiting cleavage of amyloid protein precursor (APP) in the reaction mixture in the website between Met596 and Asp597, the numbering of amino acid isotype of APP-695, or in the corresponding website isotype or mutant, including the impact on the specified reaction mixture an effective inhibitory amount of a compound of formula (AA), (I) or (X) or its pharmaceutically acceptable salt.

In the embodiment in such a way use the site of cleavage between Met652 and Asp653, the numbering of amino acid isotype of APP-751; between Met671 and Asp672, the numbering of amino acid isotype of APP-770; between Leu652 and Asp653 Swedish mutation of APP-751 or between Leu671 and Asp672 Swedish mutation of APP-770.

In the embodiment in this method, the reaction mixture effect in vitro.

In the embodiment in this method, the reaction mixture is exposed in the cell.

In the embodiment in this method, the reaction mixture is exposed in the cell of the animal.

In the embodiment in this method, the reaction mixture is exposed in the cell.

The invention also relates to a method for inhibiting production of amyloid beta peptide (A-beta) in a cell, comprising introducing into the specified cell connection fo the formula (AA), (I) or (X) under conditions when there is an effective inhibitory amount of a compound of formula (Y) or its pharmaceutically acceptable salt.

In the embodiment of this method includes the introduction of the animal.

In this embodiment the method includes administration to a human.

The invention also relates to a method of inhibiting the production of beta-amyloid plaque in an animal, comprising the introduction of a specified animal compounds of the formula (AA), (I) or (X) under conditions when there is an effective inhibitory amount of a compound of formula (Y) or its pharmaceutically acceptable salt.

In this embodiment the method includes administration to a human.

The invention also relates to a method of treating or preventing diseases characterized by beta-amyloid deposits in the brain, including the introduction to the patient an effective therapeutic amount of the compounds of formula (AA), (I) or (X) under conditions when there is an effective inhibitory amount of a compound of formula (Y) or its pharmaceutically acceptable salt.

In the embodiment of this method leads to the compound of formula (Y), the inhibitory activity of the enzyme by 50% at a concentration of less than 50 microns.

In the embodiment of this method leads to the compound of formula (Y), the inhibitory activity of the enzyme by 50% at a concentration of 10 μm or less.

In this embodiment the manual leads to the compound of formula (Y), the inhibitory activity of the enzyme by 50% at a concentration of 1 μm or less.

In the embodiment of this method leads to the compound of formula (Y), the inhibitory activity of the enzyme by 50% at a concentration of 10 nm or less.

In the embodiment of this method of connection is used in a therapeutic quantity in the range of from about 0.1 to about 1500 mg/day.

In the embodiment of this method of connection is used in a therapeutic quantity in the range of from about 15 to about 1000 mg/day.

In the embodiment of this method of connection is used in a therapeutic quantity in the range of from about 1 to about 100 mg/day.

In the embodiment of this method of connection is used in a therapeutic quantity in the range of from about 5 to about 50 mg/day.

In the embodiment of this method can be used when the disease is a disease of Alzheimer's.

In the embodiment of this method can be used when the disease is a mild cognitive impairment, down's syndrome and hereditary cerebral hemorrhage with amyloidosis (Dutch Type).

The invention also relates to a set of components, including components that can be assembled, in which at least one component includes a compound of formula AA, I, or X enclosed in the package.

In the oploschenii this set of components includes liofilizovane connection, and at least one other component comprises a diluent.

The invention also relates to a set of packages that include multiple packages, with each package includes one or more unit doses of the compounds of formula (AA), (I) or (X) or its pharmaceutically acceptable salt.

In this embodiment the set of packages includes packages, each of which is adapted for oral delivery, and includes a tablet, gel or capsule.

In this embodiment the set of packages includes packages, each of which is adapted for parenteral delivery, and includes the product in the form of a depot, syringe, ampoule or vial.

In this embodiment the set of packages includes packages, each of which is adapted for local delivery, and includes a sticker (the patch), pad, ointment or cream.

The invention also relates to a kit comprising a compound of formula (AA), (I) or (X) or its pharmaceutically acceptable salt and one or more therapeutic agents selected from the group consisting of antioxidant, anti-inflammatory agent, an inhibitor of gamma-secretase, neurotrophic means of acetylcholinesterase inhibitor, statin drug (statin), peptide A-beta and antibodies against A-beta.

The invention also relates to compositions containing a compound of the formula (AA), (I) or (X) or its pharmaceutical is acceptable salt and an inert diluent or edible carrier.

In this embodiment the composition comprises a carrier, representing the oil.

The invention also relates to compositions containing a compound of the formula (AA), (I) or (X) or its pharmaceutically acceptable salt and a binder, excipient, disintegrant, lubricant or glidant.

The invention also relates to compositions containing a compound of the formula (AA), (I) or (X) or its pharmaceutically acceptable salt that is included in the cream, ointment or sticker (the patch).

The invention relates to compounds of the formula (AA), formula (I) and (X)that can be used to generate compounds of formula (Y), which is suitable for the treatment and prevention of Alzheimer's disease. Compounds according to the invention is a specialist in the art can obtain, based on knowledge of the chemical structure of the compounds. Chemistry of obtaining compounds of this invention are well-known specialists in this field of technology. In fact, there are several ways to obtain the compounds according to the invention. Specific examples of methods of obtaining can be found in the technique. For example, see J. Org. Chem., 1998, 63, 4898-4906; J. Org. Chem., 1997, 62, 9348-9353; J. Org. Chem., 1996, 61, 5528-5531; J. Med. Chem., 1993, 36, 320-330; J. Am. Chem. Soc., 1999, 121, 1145-1155; and references cited in these works. Cm. also U.S. patent No. 6150530, 5892052, 5696270 and 5362912 included in this description as a reference.

The use of the s different ways, which you can use to obtain the compounds according to the invention, are described below.

General method of preparing compounds of the formula I and X is shown in scheme A. the Chemistry is simple and in the end stage includes the protection of the parent substance of the amino acids (a) N obtaining the appropriate amino acids (II)containing a protective group of the protected amino acid (II)), the interaction of the protected amino acid (II) with diazomethane, followed by processing for adding carbon atoms to obtain the corresponding containing a protective group of the compound (III), the recovery of protected halide to the corresponding alcohol (IV), the formation of the corresponding epoxide (V), the opening of the epoxide (V) With-terminal amine Rc-NH2(VI) to produce the corresponding protected alcohol (VII).

The compounds of formula (I) can be obtained by the interaction of the protected alcohol (VII) with amidoamines agent such as, for example, (RN-)2O or RN-X or RN-OH (IX), with the formation of alcohol (IA). Then of alcohol (IA) remove azatadine group and obtain the corresponding compounds of formula (I).

The compounds of formula (X) can be obtained by additional protection N alcohol (VII) with the formation of alcohol with two protective groups (XB). Alcohol with two protective groups (XB) enter into interaction with amidoamines agent such to the to, for example, (RN-)2O or RN-X or RN-OH (IX), with the formation of compound (HA). Then from the compound (HA) remove the protective group and obtain the corresponding compounds of formula (X).

Specialists in the art it will be clear that all of these interactions are well-known reactions in organic chemistry. Specialist in the field of chemistry, knowing the chemical structure of compounds according to the invention (AA), (I) and (X)will be able to get them by known methods from known starting compounds without any additional information. Therefore, in the explanation below, it is not necessary, but, as expected, will help professionals in the art wishing to obtain compounds of the invention.

The main chain of the intermediate compound (VII)from which you can easily obtain compounds of formula (AA), (I) and (X)can be considered as hydroxyethylamino group-NH-CH(R)-CH(OH)-. These key chains can be obtained by methods described in literature and known to experts in this field of technology. For example, in J. Med. Chem., 36, 288-291 (1993), Tetrahedron Letters, 28, 5569-5572 (1987), J. Med. Chem., 38, 581-584 (1995), Tetrahedron Letters, 38, 619-620 (1997) and WO 02/02506 describes methods of making compounds of the type hydroxyethylamine and/or intermediates for them.

Chart a shows the General method used in the invention to obtain appropriate is Estulin way of substituted amines I and H. Compounds according to the invention receives from the corresponding amino acids (And). Amino acid (S) known to experts in the art or can be easily obtained by methods known to experts in this field of technology. Compounds of the invention have at least two chiral centers, which provide two sets of diastereomers, each of which is a racemic for all of the at least four stereoisomers. Although biologically active end products are obtained from all of the stereoisomers, the preferred configuration (S,R). The first of these chiral centers (carbon bearing R1it derives from the original amino acid (S). Commercially, it is preferable to obtain or produce the desired enantiomer and not enantiomerically impure mixture, followed by the necessary selection of the desired enantiomer. Thus, it is preferable to start the process with enantiomerically pure (S)-amino acids (And) the same configuration as the desired product X.

On the diagram And shows the introduction of a protective group to the free amino acid (A) with the formation of (S)-protected amino acid (II). Group, protection for the amino group, known to experts in the art, and are discussed below. See, for example, "Protecting Groups in Organic Synthesis", John Wiley and sons, New York, N.Y., 1981, Chapter 7; "Protecting Groups in Organic Chemistry", Plenum Press, New York, N.Y., 1973, Chapter 2. F. what nccia group, protective for the amino group, is to protect the free functional amino group (-NH2during subsequent interactions with (S)-amino acid (A), which will not leak or amino groups, which can interact and show functionality on the track or incompatible with the necessity of freedom for subsequent interactions, or a free amino group may intervene in the interaction. When the group, protection for the amino group, then it is not required, it is removed by methods known to experts in this field of technology. By definition, group, protective for amino groups, should be easily removed, as is known to experts in the art by methods known to experts in this field of technology. Suitable protective groups for the amino group are described below.

(S)-Protected amino acid (II) is transformed into the corresponding (S)-protected compound (III) in two different ways, depending on the nature of R2and R3.

R2and R3may be the same or different. Preferably, R2and R3- both were a-N. If R2and R3are not the same, in the molecule, an additional chiral center or stereogenic center. In order to obtain the compounds of formula (III), where R2and R3- both are the a-N, (S)-protected amino acid (II) enter into interaction with diazomethane, as is well known to specialists in this field of technology, with subsequent interaction with the compound of the formula H-X1and get (S)-protected compound (III). X1includes-Cl, -Br, -I, -O-tosylate, -O-mesilate, -O-nosrat and-About-brasilit. Preferably, X1was a-Br or-Cl. Appropriate interaction terms is to carry out the reaction in inert solvents, such as ether, tetrahydrofuran, and other similar solvents. Reactions of transition from (S)-protected amino acid (II) to (S)-protected compound (III) is carried out for a time from 10 minutes to 1 day, and at temperatures ranging from about -78aboutC to about 20-25ºC. It is preferable to conduct the reaction for about 1-4 hours and at temperatures from-30ºC up to-10ºC. This method allows you to add one methylene group.

On the other hand, (S)-protected compound of formula (III) can be obtained by turning the first, (S)-protected amino acid (II) into the corresponding methyl or ethyl ester, according to the methods adopted in the technique, followed by treatment with a reagent of the formula X1-C(R2)(R3)-X1and strong metal base. The reason is to influence the exchange of the halogen-metal, X1undergoing change, made the focus of a halogen, selected from among chlorine, bromine or iodine. Nucleophilic joining ether derivative gives (S)-protected compound (III). Suitable bases are alkality, including, for example, second-utility, n-utility and tert-utility, and other reasons. The reaction is preferably carried out at a low temperature, such as-78ºC. Suitable reaction conditions include carrying out the reaction in inert solvents, such as ether, tetrahydrofuran, and other similar solvents. When R2and R3- both represent hydrogen, then examples X1-C(R2)(R3)-X1are dibromethane, diiodomethane, chloromethane, bromomethane and bromochloromethane. Specialists in this field known in the art, the preferred conditions necessary for such interaction. In addition, if R2and/or R3are not-H, then by adding C(R2)(R3)-X1to the ester (S)-protected amino acid (II) to obtain (S)-protected compound (III) in the reaction product is introduced an additional chiral center, provided that R2and R3are not the same.

Then (S)-protected compound (III) restoring means known to specialists in this field of technology for the recovery of the ketone to the corresponding secondary with the IRT, and receive the corresponding alcohol (IV). Means and conditions of the reduction reaction of (S)-protected compound (III) to the corresponding alcohol (IV) include, for example, sodium borohydride, lithium borohydride, borane, hydride diisobutylaluminum and alumoweld lithium. Sodium borohydride is the preferred reducing agent. The restoration carried out in the period of time from 1 hour to 3 days at temperatures ranging from-78ºC to the temperature increased up to the boiling point of the used solvent. It is preferable to carry out the restoration of the between-78ºC and 0ºC. If using borane, it can be used in the form of a complex such as borane complex-metilsulfate, complex, borane-piperidine or a complex of borane-tetrahydrofuran. Preferred combinations necessary reducing agents and reaction conditions known to experts in the art, see, for example, R.C. Larock, Comprehensive Organic Transformations, VCH Publishers, 1989. Recovery of (S)-protected compound (III) to the corresponding alcohol (IV) gives the second chiral center (third chiral center, if R2and R3are not the same). Recovery of (S)-protected compound (III) gives a mixture of enantiomers according to the second centre (S, R/S)-alcohol (IV). Then this enantiomeric mixture separated by methods known to experts in the field of technology, such as selective the recrystallization at low temperatures or chromatographic separation, for example HPLC, using commercially available chiral columns. Enantiomer, which is then used in the method according to scheme a, is a (S,S)-alcohol (IV), such as enantiomer will give the desired (S,S)-substituted compound I or X.

(S,S)-Alcohol (IV) is transformed into the corresponding epoxide (V) by means known to specialists in this field of technology. The stereochemistry of the centre (S)to(IV) in the formation of the epoxide (V) is retained. The preferred method is the interaction with a base, such as hydroxide ion formed from sodium hydroxide, potassium hydroxide, lithium hydroxide and other similar reasons. Reaction conditions include the use of solvents of alcohols With1-C6; preferred is ethanol. You can also use regular co-solvent, such as, for example, ethyl acetate. The reaction is carried out at temperatures ranging from-45ºC to the boiling point of the used alcohol; the preferred temperature intervals are between-20ºC and 40ºC.

An alternative, and preferred, method of production of the epoxide (V)when R1represents 3,5-diferensial presented in figure D. the First stage of the method is to protect the free amino group (S)-amino acids (A) group, protective for amino - protecting group, previously described for obtaining (S)-Conn is Noah amino acids (II).

In the alternative method (S)-protected amino acid (A) is transformed into the corresponding (S)-protected ester (XVII) one of a number of ways. One method involves the use of lithium hydroxide. Using lithium hydroxide (S)-protected amino acid (a) and lithium hydroxide are mixed and cooled to a temperature of from about -20 to about 10ºC. Then add metymirumi agent selected from the group consisting of dimethylsulfate, under the conditions and metallifere. Preferably, meteorous agent was dimethylsulfate. Followed by heating to a temperature of from about -20 to about 50ºC.

On the other hand, (S)-protected amino acid (A) enter into contact with a weak base, such as bicarbonate or preferably carbonate. Then add metymirumi agent. Heating is not necessary, but it can be used to facilitate interaction. Carbonate method known to specialists in this field of technology. In the case of (S)-protected ester (XVII)in which Z1is not the stands, the specialist in the art, knowing the chemical structure is known how to obtain the necessary connections from known starting materials. In one known method (S)-protected amino acid (A) enter into contact with an activating agent such as DCC, followed by adding suitable the alcohol Z 1-HE. This method works when Z1is a (C1-C4)-alkyl (optionally substituted), -CH2-CH=CH2or phenyl (optionally substituted).

Scheme E illustrates an alternative method of obtaining of ester (II). In the method of scheme E aldehyde (XX), well-known specialists in the field of technology, enter into interaction with the connection phosphorus (XXI), where X3represents an easily removable group, and get olefin (XXII). Phosphorus compounds (XXI) are known to specialists in this field of technology. Preferably, X1was a (C1-C3)-alkyl; preferably, X1represented With1-alkyl. The aldehyde (XX) and phosphate (XXI) are combined in an organic solvent and then cooled to 0ºC. Add a base, such as DBU or TMG, and the contents of the reaction mixture is heated to about 20 ░ to 25 ░ C and stirred until then, until the reaction is complete. Once the reaction is complete, it is preferable to divide the E - and Z-olefin isomers (XXII). The separation is carried out by methods known to experts in the art such as chromatography on silica gel. Then the olefin (XXII) hydronaut using a suitable hydrogenation catalyst and get the desired ester (II). Some hydrogenation reactions will give racemize the cue ester (II). The desired stereochemistry of ester (II) is (S)-and therefore it is preferable to use the Z-olefin (XXII) with a hydrogenation catalyst. Preferably, the hydrogenation catalyst was represented by a compound of the formula [Rh(diene)L]+X-,

where Rh is a rhodium;

where the diene is cyclooctadiene and norbornadiene;

where L represents the DIPMAP, MeDuPhos, EtDuPhos, Bintan, f-Bintan, IU-KetalPhos, IU-f-KetalPhos, BINAP, DIOP, BPPFA, BPPM, CHIRAPHOS, PROPHOS, NORPHOS, CYCLOPHOS, BDPP, DEGPHOS, PNNP, and where X-is a ClO4-BF4-, CF3-SO3-, Cl-, Br-PF6-and SbF6-. Preferably, the hydrogenation catalyst was or DIPMAP or EtDuPhos. Suitable solvents are polar solvents, such as alcohols, preferably alcohols With1-C5and THF, preferably methanol, ethanol, isopropanol and THF. Chiral hydrogenation is carried out in a temperature range from about -20 to about the temperature of education phlegmy. Preferably, the interaction was carried out in the temperature range from about 0 to about room temperature (25ºC). Chiral hydrogenation is carried out at a pressure of from about one atmosphere to about 100 f/d2; preferably, the chiral hydrogenation of implementing Talos at a pressure of from about 10 f/d 2up to about 40 f/d2.

Then (S)-protected ester (II) is transformed into the corresponding (S)-protected ketone (III) interaction with a slight excess of the compound of the formula CH2ClX2where X2is a-Br and-I, one of two different ways. In the same way do not use exogenous nucleophiles. This method requires (1) the presence of three or more equivalents of a strong base with pKbmore than about 30, and then (2) adding acid. The other method requires (1) the presence of from about 2 to about 2.5 equivalents of a strong base with pKbmore than about 30, (2) introducing into contact with the mixture from step (1) with from about 1 to about 1.5 equivalents of exogenous nucleophile and (3) the addition of an acid. Suitable strong bases are bases that have pKbmore than about 30. Preferably, the strong base is selected from the group consisting of LDA, LiHMDS and KHMDS; rather, a strong reason was that the LDA. Suitable acids are acids with pKandless than about 10. Preferably, the acid is selected from the group consisting of acetic, sulfuric, chloroethanol, citric, phosphoric, and benzoic acids; preferably, the acid represented acetic acid. The preferred solvent is THF. Usaimage the dance can be performed in the temperature range from about-80ºC until about-50ºC; it is preferable to carry out the interaction in the temperature range from about-75ºC to about-65ºC. Suitable nucleophiles are alkality, ability, alkyl - and arylesterase Grignard reagents. Preferably, the nucleophile selected from the group consisting of finelite, n-utility, methylacrylamide, methylacrylamide, phenylmagnesium, formanilide; preferably, the nucleophile was n-utility.

Then (S)-protected ketone (III) is reduced to the corresponding (S)-alcohol (IV) by methods known to experts in the art for recovery of the ketone to the corresponding secondary alcohol. Means and reaction conditions for recovery (S)-protected compound (III) to the corresponding alcohol (IV) include, for example, sodium borohydride, lithium borohydride, borane, hydride diisobutylaluminum, zinc borohydride and alumoweld lithium. Sodium borohydride is the preferred reducing agent. The restoration carried out over a period of time from about 1 hour to about 3 days at temperatures ranging from about-78ºC to the temperature increased up to the boiling point of the used solvent. Preferably restoration at a temperature of from about to about 70ºC 0ºC. If using borane, it can be used in the form of sets the KSA, for example, a complex of borane-metilsulfate, complex, borane-piperidine or a complex of borane-tetrahydrofuran. Preferred combinations necessary reducing agents and reaction conditions known to experts in the art, see, for example, R.C. Larock, Comprehensive Organic Transformations, VCH Publishers, 1989. Recovery of (S)-protected compound (III) to the corresponding alcohol (IV) gives the second chiral center. Recovery of (S)-protected compound (III) gives a mixture of diastereomers according to the second centre (S, R/S)-alcohol (IV). Then this diastereomers the mixture is separated by methods known to experts in the field of technology, such as selective recrystallization at low temperatures or chromatographic separation, the most preferred recrystallization or the use of commercially available chiral columns. The diastereoisomer, which is then used in the method according to scheme a, is a (S,S)-alcohol (IV), such as stereochemistry will give the desired epoxide (V).

The alcohol (IV) is transformed into the corresponding epoxide (V) by means known to specialists in this field of technology. The stereochemistry of the centre (S)to(IV) in the formation of the epoxide (V) is retained. The preferred method is the interaction with the base, such as hydroxide ion formed from sodium hydroxide, potassium hydroxide, lithium hydroxide and other similar reasons. Reaction conditions include the use as solvents alcohols With1-C6; preferred is ethanol. You can also use regular co-solvent, such as, for example, ethyl acetate. The reaction is carried out at temperatures ranging from about-45ºC to the boiling point of the used alcohol; the preferred temperature intervals are between about -20 and about 40ºC.

Then the epoxide (V) enter into interaction with the appropriately substituted C-terminal amine Rc-NH2(VI) by methods known to experts in the field of technology, which opens the epoxide with the formation of the desired corresponding enantiomerically pure (S,R)-protected alcohol (VII). Substituted C-terminal amine Rc-NH2(VI) this invention are commercially available or known to experts in the art and can be easily obtained from known compounds. Preferably, Rcwas substituted in position 3 or the provisions of 3.5, when he represents phenyl.

Suitable reaction conditions for opening the epoxide (V) include the reaction takes place in a wide range of conventional and inert solvents. Preferred are alcohols With1-C6and the most preferable isopropyl alcohol. The reaction can be conducted at temperatures to replysize from 20-25 ° C to the boiling point of the used alcohol. The preferred temperature range for the reaction is from 50ºC to the boiling point of the used alcohol. When the substituted C-terminal amine (VI) is 1-amino-3,5-CIS-dimethylcyclopropanecarboxylate, it is preferably prepared as follows. It dimethyl-5-isophthalate in acetic acid and methanol in a thick-walled flask add the rhodium in the aluminum oxide. The contents of the flask is saturated with hydrogen at a pressure of 55 f/d2and shaken for one week. The mixture is then filtered through a thick layer of celite, celite is washed three times with methanol, the solvents are removed under reduced pressure (when heated) and get the concentrate. The concentrate is treated with ether and again filtered and receive the desired C-terminal amine (VI). When the substituted C-terminal amine (VI) is 1-amino-3,5-CIS-dimethoxytoluene, it preferably receive, following the General procedure described above and making non-critical changes, but based on 3,5-dimethoxyaniline.

When the substituted C-terminal amine (VI) contains aminomethyl group, where the substituent in the methyl group is an aryl group, such as, for example, NH2-CH2is aryl, it is not available, and it is obtained preferably as follows. A suitable starting material is a (relevant about what atom substituted) arylalkyl connection. The first stage is the bromination of alkyl substituent methods known to experts in the art, see, for example, R.C. Larock, Comprehensive Organic Transformations, VCH Publishers, 1989, R. Then alkylhalogenide enter into interaction with azide and get aryl(alkyl)azide. Finally, the azide is reduced to the corresponding amine (VI) in the system hydrogen/catalyst and receive a C-terminal amine (VI) of the formula NH2-CH2-Rc-aryl.

Scheme reveals an alternative way of obtaining enantiomerically pure (S,R)-protected alcohol (VII) of (S)-protected compound (III). In this way, (S)-protected compound (III) is first introduced in the interaction with the appropriately substituted C-terminal amine Rc-NH2(VI) using the preferred conditions described above, and receive the corresponding (S)-protected ketone (XI), which is then restored using the preferred conditions described above, and receive the corresponding (S,R)-protected alcohol (VII).

The scheme discloses another alternative method of obtaining enantiomerically pure (S,R)-protected alcohol (VII), but this time of the epoxide (V). In the method according to the scheme With the epoxide (V) enter into interaction with azide and receive the corresponding enantiomerically pure (S,R)-protected azide (XII). Conditions azidopirimidinov disclosure EP is xida well-known specialists in the field of technology see, for example, J. March, Advanced Organic Chemistry, 3rdEdition, John Wiley & Sons Publishers, 1985, p.380. Then (S,R)-protected azide (XII) is reduced to the corresponding amine (XIII) by methods known to experts in this field of technology. The preferred conditions of the recovery (S,R)-protected azide (XII) in the presence of N-protective tert-butoxycarbonyl groups include catalytic hydrogenation, the terms of which are well-known specialists in this field of technology. Alternative terms of recovery, which can be used to avoid removal of the protective group from the N-protected by other protective groups than tert-butoxycarbonyl, known to experts in the art, see, for example, R.C. Larock, Comprehensive Organic Transformations, VCH Publishers, 1989, R. Finally, (S,R)-amine (XIII) is converted into the corresponding protected alcohol (VII) by alkylation of the nitrogen compound of the formula RWith-X3. X3is a corresponding delete the group, such as-Cl, -Br, -I, -O-mesilate, -O-tosylate, -O-triflate etc., and other groups. X3may also be an aldehyde; an appropriate combination of (XIII) by means of known procedures reductive amination gives protected (S,R)-alcohol (VII).

In the formation of compounds of formula (I) - protected alcohol (VII) enter into interaction with accordingly Zam is on aminoaldehydes agent (IX), such as, for example, anhydride, allalone or acid of the formula (RN)2O or RNX or RNOH, respectively, by methods known to experts in the art, and receive the corresponding (S,R)-substituted amine (IA). Conditions of acylation of the nitrogen to the interaction of alcohol (VII) with aminoaldehydes agent (IX) to obtain the corresponding compounds (IA) are known to experts in the art and can be found, for example, in R.C. Larock, Comprehensive Organic Transformations, VCH Publishers, 1989, SS. 981, 979 and 972. From (S,R)-protected amine (IA) remove the protective group with formation of the corresponding compounds (I) by methods known to experts in the art to remove aminosidine group. Suitable means for removing aminosidine group depends on the nature of the protective group. Experts in the art, knowing the specific nature of the protective group, you know, what is the preferred reagent to remove it. For example, it is preferable to remove the preferred protective group BOC, dissolving (S,R)-protected amine (IA) in a mixture triperoxonane acid/dichloromethane (1:1). After removal of the solvents removed under reduced pressure and get the corresponding (S,R)-amine (I) (in the form of a corresponding salt, i.e. salt triperoxonane acid), which is used without further purification. But what if appropriate (S,R)-amine (I) can be cleaned advanced methods, well-known experts in the art, such as, for example, recrystallization. Further, if desired nosoleva form, this form can also be obtained by methods known to experts in the art, such as, for example, to obtain the free base amine by treatment of the salt in a moderately alkaline medium. Other conditions of removal of the protective group BOC and terms of remove other protective groups can be found in T.W. Green and P.G.M. Wuts, "Protective Groups in Organic Chemistry", John Wiley and Sons, 1991, p.309. Chemically suitable salts are triptorelin and salt containing the anion of a mineral acid such as chloride, sulfate, phosphate; preferred is triptorelin.

In the formation of compounds of formula (X) alcohol (VII) also protects as described above, with the formation of desasosiego connection (XB). Then the compound (XB) enter into interaction with an appropriately substituted aminoaldehydes compound (IX) with the formation of compound (HA), as described above for compound (IA). Removing the protective groups from the compound (HA) to form compounds (X) are as described in the case of the conversion of compounds (IA) to the compound (I).

Removing the protective groups of the amines is carried out, if necessary, by methods known to experts in this field of technology. Aminosidine group of renowned experts in the Noah engineering. See, for example, "Protective Groups in Organic Chemistry", John Wiley and Sons, New York, N.Y., 1981, Chapter 7; "Protective Groups in Organic Chemistry", Plenum Press, New York, N.Y., 1973, Chapter 2. When aminosidine group is no longer needed, it is removed by methods known to experts in this field of technology. By definition, aminosidine group should easily be removed. Many different methodologies known to experts in the art; see, for example, also Green and P.G.M. Wuts, "Protective Groups in Organic Chemistry", John Wiley and Sons, 1991. Suitable aminosidine groups are tert-butoxycarbonyl, benzyloxycarbonyl, formyl, trityl, phthalimido, trichloroacetyl, chloroacetyl, bromoacetyl, iodoacetyl, 4-phenylbenzoxazole, 2-methylbenzyloxycarbonyl, 4-ethoxybenzothiazole, 4-forantimicrobial, 4-chlorobenzenesulfonyl, 3-chlorobenzylidene, 2-chlorobenzenesulfonyl, 2,4-dichlorobenzenesulfonyl, 4-bromobenzyloxycarbonyl, 3-bromobenzyloxycarbonyl, 4-nitrobenzenesulfonyl, 4-cyanobenzeneboronic, 2-(4-xenil)isopropoxycarbonyl, 1,1-diffenret-1-jocstarbunny, 1,1-diphenylprop-1-jocstarbunny, 2-phenylprop-2-jocstarbunny, 2-(p-toluyl)prop-2-jocstarbunny, cyclopentanecarbonyl, 1-methylcyclopentadienyl, cyclohexyloxycarbonyl, 1-methylcyclohexanecarboxylic, 2-methylcyclohexanecarboxylic, 2-(4-toluensulfonyl)etoxycarbonyl, 2-(methylsulphonyl)is oxycarbonyl, 2-(triphenylphosphino)etoxycarbonyl, fluorenylmethoxycarbonyl, 2-(trimethylsilyl)etoxycarbonyl, allyloxycarbonyl, 1-(trimethylsilylmethyl)prop-1-relaxerror, 5-benzisothiazolinone, 4-acetoxybenzoic, 2,2,2-trichlorocyanuric, 2-ethinyl-2-propoxycarbonyl, cyclopropanecarbonyl, 4-(decyloxy)benzyloxycarbonyl, isobornylacitate, 1-piperidinylcarbonyl, 9-fluorenylmethoxycarbonyl, -CH-CH=CH2and phenyl-C(=N -).

Preferably, the protective group represented tert-butoxycarbonyl (VOS) and/or benzyloxycarbonyl (CBZ), it is preferable that the protective group represented tert-butoxycarbonyl. Specialist in the art will know the appropriate ways of introducing tert-butoxycarbonyl or benzyloxycarbonyl protective group and may additionally be accessed as a guide to the Green and P.G.M. Wuts, "Protective Groups in Organic Chemistry", John Wiley and Sons, 1991.

Compounds according to the invention can be geometric or optical isomers, and tautomers. Thus, the invention includes all tautomers and pure geometric isomers such as E - and Z-geometric isomers, and mixtures thereof. In addition, the invention includes the pure enantiomers and diastereoisomers, and also mixtures thereof, including racemic mixtures. Single geometric isomer, enantiomer is or diastereomers can be obtained or highlight ways, well-known experts in the art, including chiral chromatography; obtaining diastereomers, separating the diastereomers and converting the diastereoisomers of enantiomers using chiral decomposing agent and other methods.

Compounds of the invention with the planned stereochemistry can log in mixtures, including racemic mixtures, with other enantiomers, diastereomers, geometric isomers or tautomers. In a preferred aspect of compounds of the invention with the stereochemistry of (S, R, R), (S, S, S) or (S, R, S) in such mixtures are present in more than 50%. Preferred compounds of the invention with the planned stereochemistry of these compounds are present in more than 80%. Preferred compounds of the invention with the planned stereochemistry of these compounds are present in more than 90%. More preferred compounds of the invention with the planned stereochemistry of these compounds are present in more than 99%.

The invention encompasses pharmaceutically acceptable salts of compounds of formula (AA), (I) and (X). Pharmaceutically acceptable salts are preferred over the corresponding amines of formula (AA), (I) or (X), as they give compounds which are more water soluble, stable and/or more crystalline. Pharmaceutically who ielemia salt is any salt, which retains the activity of the parent compound and does not produce any harmful or unwanted actions of the entity to which it is administered and in the context in which it is injected. Pharmaceutically acceptable salts include salts of both inorganic and organic acids. Preferred pharmaceutically acceptable salts are acid salts, acetic, aspartic, benzosulfimide, benzoic acid, bicarbonate, bisulfate, bitartrate, butyric acid, calcium salt of ethylenediaminetetraacetic acid, acid Kamilova, coal, chlorbenzene, lemon, ethylenediaminetetraacetic, agisilaou, Astroboy, asilinae, silovoi, formic, fumaric, gluceptate, gluconic, glutamic, picolylamine, examinados, hexylresorcinol, geranamine, Hydrobromic, chloroethanol, iodomethane, hydroxynaphthoic, italianboy, lactic, lactobionic, maleic, malic, malonic, almond, methansulfonate, metolazone, metallernas, mucus, Mukanova, natsiavas, nitric, oxalic, p-micrometeorology, pambou, Pantothenic, phosphoric, disubstituted phosphate, monosubstituted phosphate, phthalic acid, polygalacturonases, propionic, salicylic, stearic, succinic, sulfamic, sulfanilic, sulfonic, sulfuric, tannic, the wine, tolovaj, toloo the sulfonic. About other acceptable salts, see Int. J. Pharm., 33, 201-217 (1986)and J. Pharm. Sci., 66(1), 1 (1977).

The invention relates to compounds, compositions, kits and methods for inhibiting the enzymatic activity of beta-secretase and production of peptide A-beta. Inhibition of the enzymatic activity of beta-secretase stops or reduces the production of A-beta from the RDA and reduces or eliminates the formation of beta-amyloid deposits in the brain.

The methods of the invention

Compounds according to the invention and their pharmaceutically acceptable salts are suitable for the treatment of humans or animals suffering from a condition characterized by a pathological form of beta-amyloid peptide, such as beta-amyloid plaques, and to promote the prevention or delay the emergence of such a state.

Used in this description, the term "treatment" means that the compounds of the invention can be used for people with at least a presumptive diagnosis of the disease. Compounds of the invention will delay or slow the progression of the disease, whereby the individual provides much greater life expectancy.

The term "prevention" means that the compounds of the invention are suitable, when you enter the patient has no diagnosis possible presence of disease at the time of introduction, but whose natural the public to expect the development of the disease or increased risk of disease. Compounds according to the invention will slow the progression of symptoms of the disease, to delay the appearance of the disease or even prevent the individual from developing the disease. Prevention also includes the introduction of compounds of the invention to those individuals suspected of predisposition to disease because of age, family history, genetic or chromosomal abnormalities, and/or because of the presence of one or more biological markers of disease, such as a known genetic mutation of APP or cleavage products of APP in the tissues or fluids of the brain.

In the treatment or prevention of the above diseases, the compounds of the invention are administered in therapeutically effective amounts. therapeutically effective amount will greatly vary depending on the specific compound and the method of administration, which is known to specialists in this field of technology.

When treating a patient who has diagnosed with any of the above conditions, the doctor may prescribe a compound of the invention immediately and continue the introduction of the unlimited, as required. In the treatment of patients who are not diagnosed with Alzheimer's disease, but which, considered to be facing a significant risk of developing Alzheimer's disease, the physician should preferably start the treatment when the patient COI is melting the first early symptoms, prior Alzheimer's disease, such as problems with memory and cognition associated with aging. In addition, there are some patients for whom it is possible to determine that they are in danger of developing Alzheimer's disease through the detection of a genetic marker, such as AREA, or other biological indicators that predict Alzheimer's disease. In such situations, even if the patient has no symptoms of the disease, the introduction of the compounds of the invention can be started before the onset of symptoms, and the treatment can be continued indefinitely to prevent or delay onset of the disease.

Dosage forms and number

Compounds according to the invention can be administered orally, parenterally (IV, IM, depo-IM, SQ, and depo-SQ), sublingual, intranasally (inhalation), vnutriobolochechnoe, topically or rectally. Pharmaceutical form known to the person skilled in the art are suitable for delivery of the compounds according to the invention.

Provide compositions containing therapeutically effective amounts of compounds according to the invention. The connection is preferably introduced into suitable pharmaceutical preparations such as tablets, capsules or elixirs for oral administration or in sterile solutions or suspensions for parenteral administration. Typically, the compounds described above, putting the t into pharmaceutical compositions using techniques and procedures, well known in the art.

About 1-500 mg of the compound or mixture of compounds according to the invention or their physiologically acceptable salts or esters combined with a physiologically acceptable excipient, carrier, excipient, binder, preservative, stabilizer, flavorants, etc. in a unit dosage form by methods accepted pharmaceutical practice. The amount of active substance in these compositions or preparations is such that you are getting the right dosage at the specified interval. The composition is preferably prepared in the form of a unit dosage form, each dosage containing from about 2 to about 100 mg, preferably from about 10 to about 30 mg, of the active ingredient. The term "unit dosage form" refers to physically discrete units suitable as single doses to humans and other mammals, each unit contains a preset amount of the active substance is calculated in order to obtain the desired therapeutic effect, in combination with a suitable pharmaceutical excipient.

In order to obtain compositions, one or more compounds according to the invention is mixed with a suitable pharmaceutically acceptable carrier. After mixing or addition of the compound(s) obtained mixture may be a p is the target, suspension, emulsion or similar form. Liposomal suspensions can also be suitable as pharmaceutically acceptable carriers. They can be obtained according to methods known to experts in this field of technology. The shape of the resulting mixture depends upon a number of factors, including the intended route of administration and the solubility of the compounds in the selected carrier or filler. The effective concentration is the concentration that is sufficient to attenuate or reduce at least one symptom of a disease, disorder or condition which is treatable and can be determined empirically.

Pharmaceutical carriers or excipients suitable for administration of the compounds described herein include any such carriers known to experts in the art as suitable for a particular method of administration. In addition, the active substance can also be mixed with other active materials that do not weaken the desired action, or with substances that Supplement the desired action, or have a different action. Compounds can be introduced into the composition as the sole pharmaceutically active ingredient in the composition or can be combined with other active ingredients.

When the connection detect low solubility, can be used in the th methods of solubilization. Such methods are known and include the use of co-solvents, such as dimethylsulfoxide (DMSO), using surfactants, such as tween®, and dissolution in aqueous solution bicarbonate sodium, and other ways. Derivative compounds, such as salts or prodrugs can also be used to obtain effective pharmaceutical compositions.

The concentration of the compound is effective for delivery after the introduction of a number that weakens or reduces the intensity of at least one symptom of the disorder, which enter the connection. Typically, the compositions have for a single dose.

Compounds of the invention can be introduced into the drug with carriers that protect them against rapid removal from the body, such as the composition with the gradual release of, or coated. Such media include compositions for controlled release, such as microencapsulation delivery systems, and others. Active connection include pharmaceutically acceptable carrier in a quantity sufficient for the manifestation of therapeutically useful effect in the absence of undesirable side effects on the patient treated. therapeutically effective concentration may be determined empirically testing the connection on the well-known m the sensible systems in vitro and in vivo for the disorder, from where they treat.

Compounds and compositions of the invention can be enclosed in packaging one or more techniques. Packed compounds and compositions can be provided in sets, for example, contains elements that can be connected for use. For example, the connection-inhibitor in liofilizovannyh form and a suitable diluent can be provided in the form of separate components to merge before use. The set can include a connection-inhibitor and another therapeutic agent for joint injection. The inhibitor and the second therapeutic agent can be provided in the form of individual components. The set can include several packages, with each package contains one or more standard doses of the compounds of the invention. Packing is preferably adapted for the desired method of administration, including tablets, soft capsules, capsules, delayed release, etc. for oral administration; products of prolonged action, pre-filled syringes, ampoules, vials, etc. for parenteral administration; and labels, patches, creams, etc. for local injection.

The concentration of the active compounds in the composition of the medicinal product will depend on the speed of absorption, inactivation and excretion of the active connection scheme application Lakers the governmental funds and the input quantity, as well as other factors known to specialists in this field of technology.

The active ingredient can be injected once or divided into several smaller doses for insertion through a certain period of time. It should be borne in mind that the precise dosage and duration of treatment depends on the disease that is treatable and can be determined empirically using known testing protocols or by extrapolation of the test results in vivo or in vitro. It should be noted that the concentration and size of doses may also vary due to the severity of the condition with a partial withdrawal symptoms. It should also be borne in mind that for any particular subject, specific patterns of use of the medicinal product must be adjusted over time according to individual needs and professional assessment of the person making the introduction of, or control over the introduction of the compositions, and that the intervals of the concentrations mentioned in this description are only examples and are not intended to limit the scope or the practical application of the inventive compositions.

If it is desirable oral administration, the connection should be provided in a composition that protects it from the active medium in the stomach. For example, it is possible to obtain a composition with intersolubility coating which retains its entirety the guard in the stomach and releases the active compound in the gut. It is also possible to obtain compositions in combination with antacid agent or the other ingredient.

Oral compositions generally will contain an inert diluent or edible carrier and can be compressed into tablets or enclosed in gelatin capsules. For purposes of oral administration for the treatment of active compound or compounds can be combined with excipients and used in the form of tablets, capsules or lozenges. Pharmaceutically compatible binding agents, and adjuvants may be included as part of the composition.

Tablets, pills, capsules, lozenges and the like can contain any of the following ingredients, or compounds of a similar nature: a binder such as tragacanth resin, Arabian gum, corn starch or gelatin, or a similar substance; excipients, such as microcrystalline cellulose, starch or lactose; disintegrant, such as alginic acid, corn starch, or the like; a lubricant such as magnesium stearate or the like; glidants, such as colloidal silicon dioxide, or the like; sweeteners such as sucrose or saccharin; and flavorant, such as peppermint, methyl salicylate or fruit substance.

When the unit dosage form is a capsule, it may contain, in addition to the substances of the above type, a liquid is osiel, such as fatty oil. In addition, the standard dosage forms can contain various other materials which modify the physical form of the dosage form, for example, coatings of sugar and other intersolubility substances. Connections can also be entered as a component of an elixir, suspension, syrup, wafer, chewing gum or the like. A syrup may contain, in addition to the active compounds, sucrose as a sweetener and certain preservatives, dyes and tinted substance and flavorant.

The active substance can also be mixed with other active materials that do not weaken the desired action, or with substances that Supplement the desired action.

Solutions or suspensions used for parenteral, intradermal, subcutaneous, or topical application can include any of the following components: a sterile diluent such as water for injection, saline solution, fixed oil, a naturally occurring vegetable oil such as sesame oil, coconut oil, peanut oil, cottonseed oil and the like, or synthetic fatty filler, such as etiloleat and the like, polyethylene glycol, glycerine, propylene glycol or other synthetic solvent; antimicrobial agents, such as benzyl alcohol and methylparaben; antioxidants, such as ascorbic acid and sodium bisulfite; hepatoblastoma agents such as ethylenediaminetetraacetic acid (edtc); buffering agents such as acetates, citrates and phosphates; and agents to achieve isotonicity, such as sodium chloride and dextrose. Parenteral preparations can be enclosed in ampoules, syringes disposable or vessels in multiple doses, made of glass, plastic or other suitable material. Optionally, you can include buffering agents, preservatives, antioxidants, etc.

For intravenous administration, suitable carriers are saline, phosphate buffered saline (SFR) and solutions containing thickening agents and soljubilizatory, such as glucose, polyethylene glycol, polypropyleneglycol and mixtures thereof. Liposomal suspensions containing darinaparsin liposomes, may also be suitable as pharmaceutically acceptable carriers. They can be obtained according to known methods, for example as described in U.S. patent No. 4522811.

The active compounds can be introduced into the drug with carriers that protect the compound against rapid removal from the body, such as the composition with the gradual release of, or coated. Such media include compositions for controlled release, such as implants and microencapsulation system dostavka the other, and biodegradable, biocompatible polymers, such as collagen, a copolymer of ethylene and vinyl acetate, polyanhydrides, polyglycolic acid, complex poliorcetes, polylactic acid and other Methods of obtaining such compositions are well-known specialists in this field of technology.

The compound of the invention can be administered orally, parenterally (IV, IM, depo-IM, SQ, and depo-SQ), sublingual, intranasally (inhalation), vnutriobolochechnoe, topically or rectally. Pharmaceutical form known to experts in the art and are suitable for delivery of the compounds of the invention.

The compound of the invention can enter interline or parenteral. When administered orally, the compounds of the invention can be introduced in the form of conventional pharmaceutical forms for oral administration are well known to the specialists in this field of technology. Such dosage forms include tablets and capsules) and liquid dosage forms such as solutions, suspensions and elixirs. When using solid dosage forms, preferably so that they are type forms with delayed release, so that compounds of the invention need to enter only once or twice a day.

Oral dosage form is administered to the patient 1, 2, 3 or 4 times a day. Preferably, the connection izobreteny is introduced or three or fewer times, preferably only once or twice a day. Therefore, it is preferable that the compounds of the invention were administered in oral dosage form. Preferably, whatever dosage form is not used, it was created so that the compounds of the invention are protected from the acidic environment of the stomach. Specialists in the art of well-known tablets intersolubility coating. In addition, specialists in the art is also well-known capsules, filled with small spheres coated to protect it from the acidic environment of the stomach.

When administered orally enter the amount therapeutically effective for inhibiting beta-secretase activity, for inhibiting the production of A-beta, for inhibiting the deposition of A-beta, or for treating or preventing AD is from about 0.1 mg/day to about 1000 mg/day. Preferably, the oral dosage ranged from about 1 mg/day to about 100 mg/day. Preferably, the oral dosage ranged from about 5 mg/day to about 50 mg/day. It should be borne in mind that although the patient may start with one dose, the dose may change over time, so how does the patient's condition.

Compounds according to the invention can also be advantageously Dostal shall be composed of nanocrystalline dispersion. The receipt of such compositions is described, for example, in U.S. patent No. 5145684. Nanocrystalline dispersion of HIV protease inhibitors and method of use are described in U.S. patent No. 6045829. Nanocrystalline compositions generally provide greater bioavailability of the compounds of the medicinal product.

Compounds according to the invention it is possible to enter parenterally, for example, IV, IM, depo-IM, SQ, or depo-SQ method. When parenteral administration should deliver a therapeutically effective amount of about 0.5 mg/day to about 100 mg/day, preferably from about 5 mg/day to about 50 mg/day. When using the composition-depot injections once a month or once every two weeks, the dose should be from about 0.5 mg/day to about 50 mg/day or a monthly dose of about 15 mg to about 1500 mg Partly due to forgetfulness of patients with Alzheimer's disease it is preferable that a parenteral dosage form had the form of a depot composition.

Compounds according to the invention it is possible to enter the hyoid. When the hyoid reception compounds of the invention should be given one to four times a day in amounts described above for IM injection.

Compounds according to the invention it is possible to enter the route. To receive such a manner appropriate drug Faure who s have the form of a nasal spray or dry powder, what is known by the experts in this field of technology. The dosage of the compounds according to the invention for intranasal represents the number described above for IM injection.

Compounds according to the invention it is possible to enter vnutriobolochechnoe. To receive in this way a suitable dosage form can be a parenteral dosage form, well-known specialists in this field of technology. The dosage of the compounds of the invention for vnutriobolochechnoe introduction represents the number described above for IM injection.

Compounds according to the invention can be entered locally. To receive in this way a suitable dosage form can be a cream, ointment or sticker. Due to the insertion amount of the compounds of the invention, it is preferable sticker. The local introduction of the dosage is from about 0.5 mg/day to about 200 mg/day. Because the amount that can deliver the label is limited, you can use two or more labels. The number and size of the labels are not important, and it is important that delivered therapeutically effective amount of the compounds according to the invention, as is well known to specialists in this field of technology. Compounds according to the invention it is possible to enter rectal use suppository, how people know this is the field of technology. With the introduction of using the suppository therapeutically effective amount is from about 0.5 mg to about 500 mg

Compounds according to the invention can be entered with the help of implants, as is well known to specialists in this field of technology. With the introduction with implant therapeutically effective amount is the amount described above for the introduction of the depot.

Specific compounds according to the invention and the desired dosage form specialist in the art will be able to learn how to obtain and enter the appropriate dosage form.

Compounds according to the invention is used in the same way, the same introduction methods using the same pharmaceutical dosage forms and schemes of a medicament which is described above, for prevention or treatment of patients with MCI (mild cognitive impairment) and preventing or delaying the appearance of Alzheimer's disease in those people with MCI may evolve to AD, for treating and preventing down syndrome, for treating humans with hereditary cerebral hemorrhage with amyloidosis (Dutch-Type, for treating cerebral amyloid angiopathy and preventing its potential consequences, i.e. single or repeated lobes hemorrhages, for treating other degeneratively, including dementia of mixed vascular and degenerative origin, dementia associated with Parkinson's disease, dementia associated with progressive supranuclear palsy, dementia associated with cortical basal degeneration, and Alzheimer's disease-type diffusion Taurus Levi.

Compounds according to the invention can be used in combination with each other or with other therapeutic agents or methods used to treat or prevent conditions listed above. To such means or methods include acetylcholinesterase inhibitors such as taken (tetrahydroaminoacridine, marketed as COGNEX®), donepezil hydrochloride (marketed as Aricept®) and rivastigmine (marketed as Exelon®); inhibitors of gamma-secretase; anti-inflammatory agents, such as inhibitors of cyclooxygenase II; antioxidants, such as vitamin E and ginkolide; immunological methods, such as, for example, immunization with peptide A-beta or antibodies against peptide A-beta; statins and acting directly or indirectly neurotropic agents such as Cerebrolysin®, AIT-082 (Emilieu, 2000, Arch. Neurol., 57:454) and other neurotropic tools, which will appear in the future.

In addition, the compounds of formula (AA), (I) or (X) can also be used with inhibitors of P-glycoprotein (P-gp). Inhibitors of P-gp and the use of such compounds is swesty specialists in this field of technology. See, for example, Cancer Research, 53, 4595-4602 (1993), Clin. Cancer Res., 2, 7-12 (1996), Cancer Research, 56, 4171-4179 (1996), international publication WO 99/64001 and WO 01/10387. Importantly, the level of inhibitor of P-gp in the blood is such that it exerts its effect by inhibition of P-gp at lower levels in the blood brain compounds of formula (A). To this end, the inhibitor of P-gp and the compounds of formula (A) can be entered simultaneously in the same or different routes of administration or at different times. It is not the time of introduction, and the presence of an effective level of inhibitor of P-gp in the blood.

Suitable inhibitors of P-gp are cyclosporin a, verapamil, tamoxifen, quinidine, vitamin E TGPS, ritonavir, acetate megestrol, progesterone, rapamycin, 10,11-metasedimentary, phenothiazines, acridine derivatives, such as GF120918, FK506, VX-710, LY335979, PSC-833, GF-102,918 and other steroids. It should be borne in mind that they will find other means having the same function and, therefore, reaching the same result; such compounds are also considered suitable.

Inhibitors of P-gp can be administered orally, parenterally (IV, IM, depo-IM, SQ, or depo-SQ), topical, sublingual, rectal, intranasal, vnutriobolochechnoe and with implant.

A therapeutically effective amount of the inhibitors of P-gp is from about 0.1 to about 300 mg/kg/day, preferably from about 0.1 to about 150mg/kg daily. It should be borne in mind that although the patient can start taking one dose, you may need to change this dose over time, as changing the patient's condition.

When orally administered inhibitors of P-gp can be entered in the usual pharmaceutical forms for oral administration, known to specialists in this field of technology. Such dosage forms include conventional solid and liquid dosage forms - tablets and capsules) and liquid dosage forms such as solutions, suspensions and elixirs. When using solid dosage forms, preferably, they represented a type of delayed release, in order to introduce the P-gp was required only once or twice a day. Oral dosage form is administered to the patient one to four times per day. Preferably, the inhibitors of P-gp was administered three or fewer times per day, preferably once or twice per day. Therefore, preferably, the inhibitors of P-gp was administered in solid dosage form, and also preferably, the solid dosage form was a form of delayed release, allowing the reception once or twice a day. Preferably, whenever the dosage form is not used, it was created so that inhibitors of P-gp was defending himself from what Isla environment of the stomach. Specialists in the art of well-known tablets intersolubility coating. In addition, specialists in the art is also well-known capsules, filled with small spheres coated to protect it from the acidic environment of the stomach.

In addition, inhibitors of P-gp can be entered parenteral. When parenteral they can be administered IV, IM, depo-IM, SQ, or depo-SQ method.

Inhibitors of P-gp you can enter the hyoid. When the hyoid receiving inhibitors of P-gp should be given one to four times per day in the same amount as for IM injection.

Inhibitors of P-gp you can enter the route. To receive this way is suitable dosage forms have the form of a nasal spray or dry powder, which is known to specialists in this field of technology. Dosage of inhibitors of P-gp for intranasal same as for IM injection.

Inhibitors of P-gp can be entered vnutriobolochechnoe. To receive in this way a suitable dosage form can be a parenteral dosage form, well-known specialists in this field of technology.

Inhibitors of P-gp can be entered locally. To receive in this way a suitable dosage form can be a cream, ointment or sticker. Because of the necessary input number of inhibitors of P-gp is preferable NAC the side. However, the amount that can deliver sticker, limited. So you may need two or more labels. The number and size of the labels are not important, and it is important that delivered therapeutically effective amount of the inhibitors of P-gp, as is well known to specialists in this field of technology.

Inhibitors of P-gp can be entered by using a suppository, as is well known to specialists in this field of technology.

Inhibitors of P-gp can be entered with the help of implants, as is well known to specialists in this field of technology.

There is nothing new in no relation to the method of administration, neither in terms of dosage forms for administration of inhibitors of P-gp. Using a specific inhibitor of P-gp and the desired dosage form specialist in the art will be able to learn how to obtain and enter an appropriate dosage form for an inhibitor of P-gp.

For specialists in the art should be obvious that the exact dosage and frequency of injection will depend on the particular input connection of the invention, a specific condition, which are treated, the severity of the condition, which are treated, age, weight, General physical condition of the particular patient, and other medications that can take an individual that is well known to physicians prescribing treatment is, who are specialists in this field of technology.

Inhibition of cleavage of APP

Compounds of the invention inhibit cleavage of APP between Met595 and Asp596 numbered on the isoforms ARR, or its mutant, or in the corresponding website the other isoforms, such as AR or AR, or its mutant (sometimes referred to as the "site beta secretase"). Without going into any theory, under the inhibition of beta-secretase activity understand the inhibition of the production of beta-amyloid peptide (A-beta). Inhibitory activity demonstrated in the analysis of a series of tests on inhibition, in which cleavage of the substrate by the RDA in the presence of the enzyme beta-secretase analyze in the presence of inhibitory compounds in the environment, is usually sufficient to obtain cleavage site cleavage of beta-secretases. The decrease in the cleavage of APP at the site of cleavage of beta-secretases compared with untreated or inaktivirovannye control correlates with inhibitory activity. System tests that can be used to demonstrate the efficacy of compounds for inhibitors of the invention are known. Typical system analyses are described, for example, in U.S. patent No. 5942400 and 5744346, as well as in the examples below.

The enzymatic activity of beta-secretase and the production of A-beta can analizirovat the in vivo or in vitro using natural substrates, the mutated and/or synthetic RDAs, natural, mutated, and/or synthetic enzyme and test compound. In the analysis it is possible to use primary or secondary cells expressing native, mutant, and/or synthetic RDAs and the enzyme, animal models expressing native RDAs and the enzyme, or you can use transgenic animal models expressing the substrate and the enzyme. The detection of the enzymatic activity can be performed by analysis of one or more cleavage products, for example, by immunoassay, fluorometric or chromogenic analysis, HPLC or other methods of detection. Connection-inhibitors are defined as compounds with the ability to reduce the amount of cleavage product of beta-secretases compared with the control, where the cleavage in the reaction system, mediated beta-secretases observed and measured in the absence of compounds inhibitors.

Beta secretase

Various forms of the enzyme beta-secretase known and available and suitable for analysis of enzyme activity and inhibition of enzyme activity. Such forms include native, recombinant and synthetic forms of the enzyme. Human beta-secretase known as an enzyme that breaks down beta-site of APP (VASYA), Asp2 and Melepsin 2, and characterized, n is the sample, in U.S. patent No. 5744346 and published patent applications PCT WO 98/22597, Wo 00/03819, WO 01/23533 and WO 00/17369, as well as in literary publications (Hussain et al., 1999, Mol. Cell. Neurosci., 14:419-427; Vassar et al., 1999, Science 286:735-741; Yan et al., 1999, Nature, 402:533-537; Sinha et al., 1999, Nature, 40:537-540; and Lin et al., 2000, PNAS USA, 97:1456-1460). Synthetic forms of the enzyme have also been described (WO 98/22597 and WO 00/17369). Beta secretase can be extracted and separated into a pure form of the fabric of the human brain and can be obtained in the cells, for example mammalian cells expressing recombinant enzyme.

Preferred subjected to rearrangement compounds are effective for inhibiting the enzymatic activity of beta-secretase to about 50% at a concentration of less than about 50 microns, preferably in a concentration of 1 μm or less, and most preferably at a concentration of 10 nm or less.

The substrate RDAs

In the analyses that demonstrate inhibition mediated beta-secretases cleavage of APP, you can use any of the known forms of ADR, including "normal" isotype of 695 amino acids described by Kang et al., 1987, Nature, 325:733-6, of 770 amino acids described by Kitaguchi et al., 1981, Nature, 31:530-532, and options such as the Swedish mutation (CM-1NL) (APP-SW), the London mutation (V7176F) and others. See, for example, U.S. patent No. 5766846 and Hardy, 1992, Nature Genet., 1:233-234, for an overall view of the known variants of mutations. Other prigodin the mi substrates are modifying dibasic amino acids ARR-ACS, disclosed, for example, in WO 00/17369, fragments of APP and synthetic peptides containing the site of cleavage of beta-secretases, wild type (WT) or mutated form, for example, SW, described, for example, in U.S. patent No. 5942400 and WO 00/03819.

The substrate ARR contains the site cleavage of APP by beta secretases (KM-DA or NL-DA), such as the full peptide of APP or variant, fragment of APP, recombinant or synthetic APP or fused peptide. Preferably fused peptide includes the site of cleavage of beta-secretases, fused with a peptide containing a group suitable for enzymatic analysis, for example, have properties to effect the separation and/or detection. Suitable group may be antigenic epitope for binding of the antibody, a label or other detected group, substrate for binding, etc.

Antibodies

Characteristic cleavage products of APP may be determined by immunoassay using various antibodies, as described, for example, in Pirtilla et al., 1999, Neuro. Lett., 249:21-4, and in U.S. patent No. 5612486. Antibodies suitable for detection of a-beta, are, for example, monoclonal antibodies E (Senetek, St. Louis, MO), which specifically recognize an epitope on amino acids 1-16 of peptide A-beta; antibodies 162 and 164 (New York State Institute for Basic Research, Staten Island, NY), which is specific for human A-beta 1-40 and 1-42, respectively; and antibodies that recognize the region of the junction be the a-amyloid peptide - the site between residues 16 and 17, described in U.S. patent No. 5593846. Antibodies induced against a synthetic peptide residues 591-596 RDAs, and antibodies SW192 induced against 590-596 Swedish mutation, also suitable immunoanalyzer RDAs and fission products, as described in U.S. patent No. 5604102 and 5721130.

System analysis

Analyses to determine the cleavage of APP at the site of cleavage of beta-secretases well known in the art. Examples of analyses are described, for example, in U.S. patent No. 5744346 and 5942400, and are described below in the examples.

Cell-free tests

Examples of analyses that can be used to demonstrate the inhibitory activity of the compounds of the invention are described, for example, in WO 00/17369, WO 00/03819 and in U.S. patent No. 5942400 and 5744346. Such analyses can be performed by incubation in the absence of cells or in the presence of cells, using cells expressing beta-secretase, and substrate RDAs, with the site of cleavage of beta-secretases.

The substrate of APP that contains the site of cleavage of beta-secretases, for example, the full RDA or variant, fragment of APP, or the substrate recombinant or synthetic APP containing the amino acid sequence of KM-DA or NL-DA, incubated in the presence of the enzyme beta-secretase, its fragment or variant synthetic or recombinant polypeptide region is giving beta secretase activity and effective for cleavage site cleavage of beta-secretases RDAs, the incubation conditions suitable for splitting activity of the enzyme. Suitable substrates include optional derivatives, which can be a fused proteins or peptides containing peptide substrate, and modification suitable to facilitate purification or detection of the peptide or products of the cleavage of beta-secretases. Suitable modifications are inserting a known epitope for binding of antibodies; attaching a label or detectable group, joining binding substrate, etc.

Suitable incubation conditions for cell-free in vitro assays are, for example, incubation of a mixture of approximately 200 nm - 10 μm substrate, approximately 10-200 PM enzyme, and approximately 0.1 nm - 10 μm compound inhibitor in aqueous solution at a pH of about 4-7, at approximately 37º during the period of time from about 10 minutes to 3 hours. Such conditions of incubation are only examples, and may require changes to specific components of the analysis and/or need of the measuring system. Optimization of incubation conditions for specific components of the analysis should take account of the used enzyme beta-secretase and its pH optimum, any additional enzyme and/or markers that can be used in the analysis, and similar factors. This optimization is usual the case and does not require additional experiments.

In one suitable analyses using fused peptide containing maltose binding protein (MBP)fused to a C-terminal amino acids of APP-SW. MBP-part captured on the substrate for the analysis of immobilized antibodies against MBP. Incubation of immobilized fused protein in the presence of beta-secretase leads to cleavage of the substrate at the site of cleavage of beta-secretases. Analysis of digestive activity can be performed, for example, by immunoassay products of cleavage. In one such analysis discover a unique epitope at the carboxy-end of the cleaved fused protein, for example, using antibodies SW192. This analysis is described, for example, in U.S. patent No. 5942400.

Cell analysis

Many analyses based cells can be used to analyze beta-secretase activity and/or processing of APP with the release of A-beta. The contact substrate RDAs with the enzyme beta-secretases in the cell in the presence or in the absence of the compound inhibitor of the invention can be used to demonstrate the inhibitory activity of compounds against beta-secretase. Preferably the analysis in the presence of a suitable connection inhibitor gives the inhibition of the enzymatic activity of at least about 30%, most preferably at least about 50%, when compared with control, not p is delavska inhibition.

In one embodiment using cells naturally expressing beta-secretase. On the other hand, cells modify for the expression of recombinant beta-secretase or synthetic version of the enzyme, as described above. The substrate RDAs can be added to the culture medium, and preferably to Express in cells. Cells naturally expressing the RDA, variant or mutant form of APP, or cells that have been transformed for the expression of isoforms of APP, mutant or variant ARR, recombinant or synthetic APP, fragment of APP or synthetic peptide of APP or fused protein containing the site cleavage of APP by beta secretases, can be used, provided that downregulation of APP is allowed to contact with the enzyme and can be analyzed enzymatic splitting activity.

Line of human cells that naturally produce A-beta from the RDA, provide a suitable tool for the analysis of the inhibitory activity of the compounds of the invention. The production and release of A-beta and/or other fission products into the culture medium can be measured, for example, immunoassay methods, such as Western blotting or enzyme immunoassay (EIA), such as ELISA.

Cells expressing the substrate RDAs and active beta-secretase, can be incubated in the presence of the connection is in inhibitor to demonstrate the inhibition of the enzymatic activity when compared with control. The activity of beta-secretase can be measured by analysis of one or more products of the cleavage of the substrate by the RDA. For example, it can be expected that inhibition of beta-secretase activity against substrate RDAs will reduce the release of specific cleavage products of APP, called beta-secretases, such as A-beta.

Although both neural and aneuretinae cells produce and release A-beta, the levels of endogenous beta-secretase activity are low and often barely detectable EIA. Therefore, it is preferable to use types of cells, known as cell-enhancing beta-secretshow activity, enhancing the processing of APP to A-beta and/or enhancing production of A-beta. For example, transfection of cells form the Swedish mutant of APP (APP-SW), ARR-ACS or the RDA-SW-KK, provides cells with enhanced beta-secretase activity and producing amount of A-beta, which can be easily measured.

In such analyses, for example, cells expressing the RDA and beta secretase, incubated in culture medium under conditions suitable for the beta secretase enzymatic activity in her cleavage site on the substrate by the RDA. When exposed to cell connection-inhibiting amount of A-beta, released on Wednesday, and/or the number of fragments CTF99 of APP in cell lysates compared to control. Prod the points of cleavage of APP can be analysed for example, using immune reactions with specific antibodies described above.

The preferred cells for the analysis of beta-secretase activity are the primary neural cells human primary neural cells of transgenic animals, where the transgene is RDAs, and other cells, such as cells of the resistant cell line 293 expressing the RDA, such as the RDA-SW.

Anility in vivo: animal models

Various animal models can be used to analyze beta-secretase activity and/or processing of APP with the release of A-beta, described above. For example, to demonstrate the inhibitory activity of the compounds of the invention can be used transgenic animals expressing the substrate RDAs and the enzyme beta-secretase. Some transgenic animal models are described, for example, in U.S. patents№№ 5877399, 5612486, 5387742, 5720936, 5850003, 5877015 and 5811633, and Ganes et al., 1995, Nature, 373:523. Preferred animals, showing the properties that are associated with the pathophysiology of AD. Introduction compounds are inhibitors of the invention the transgenic mice described herein, is an alternative way to demonstrate inhibitory activity of compounds. Also preferably, the introduction of compounds in pharmaceutically effective carrier and method of administration, which delivers to the target tissue suitable treatment the number.

Inhibition mediated beta-secretases cleavage of APP at the site of cleavage of beta-secretases and the release of A-beta can be analyzed on animals, by measuring the cleavage fragments in body fluids of animals, such as cerebral fluid, or tissues. The preferred analysis of brain tissue to deposition of a-beta or plaques.

Upon contact of the substrate RDAs with the enzyme beta-secretases in the presence of the compound is an inhibitor of the invention and under conditions sufficient to create opportunities mediated by enzyme cleavage of APP and/or release of a-beta from the substrate, the compounds of the invention are effective to reduce mediated beta-secretases cleavage of APP at the site of cleavage of beta-secretases and/or effective to reduce the released amounts of A-beta. When this contact is the introduction of compounds inhibitors of the invention to an animal model, such as described above, the compounds are effective to reduce sediment And-beta in the brain tissue of the animal and to reduce the number and/or size of beta-amyloid plaques. When this introduction is carried out to a person, the compounds are effective for inhibiting or slowing the disease, characterized by increased amounts of A-beta, to slow down the progression of AD and/or to prevent the Oia began the development of AD in patients at risk of such disease.

Unless otherwise stated, terms used in this description have the same values, which usually gives the person skilled in the art to which it pertains to this invention. All patents and publications cited in this specification, are included as references.

Definitions

Definitions and explanations below are for terms used throughout this document, including the description and the claims.

It should be noted that as used in this description and the attached claims the signs of the singular number include the corresponding plural forms, if the content does not indicate clearly otherwise. So, for example, reference to a composition containing "a compound"includes a mixture of two or more compounds. It should also be noted that the term "or" is used generally in its sense including "and/or"unless the content is not clearly indicates otherwise.

The symbol "-" in General represents a bond between two atoms in the chain. So, CH3-About-

CH2-CH(R1)-CH3represents the connection of 2-substituted 1-methoxypropan. In addition, the symbol "-" represents the place of connection of the Deputy to the connection. So, for example, aryl((C1-C6)-alkyl)- shows alkylaryl the group, such as benzyl, attached to the connection in the alkyl part.

When you specify several deputies, acceding to the structure, it should be borne in mind that the substituents may be the same or different. So, for example, Rm, optionally substituted by 1, 2 or 3 groups Rqindicates that Rmsubstituted by 1, 2 or 3 groups Rqwhere the group Rqmay be the same or different.

Amyloid protein precursor of the RDA is defined as any peptide RDAs, including options for RDAs, mutation and isoforms, for example, described in U.S. patent No. 5766846.

Amyloid beta-peptide A-beta is defined as any peptide, the resulting mediated beta-secretases cleavage of APP, including the peptides of 39, 40, 41, 42 and 43 amino acids, and capacity from the site of cleavage of beta-secretases to amino acids 39, 40, 41, 42 or 43.

Beta secretase (VASE, Asp2, Melepsin 2) represents aspirinplease, which mediates cleavage of APP by aminobenzo A-beta. Human beta-secretase described, for example, in WO 00/17369.

The term "pharmaceutically acceptable" refers to those properties and/or substances which are acceptable to the patient from a pharmacological/Toxicological point of view and for a pharmacist / chemist from a physical/chemical point of view when considering the composition, structure, ostoich the stability and acceptance by the patient.

"Therapeutically effective amount" is defined as an amount effective to reduce or ameliorate at least one symptom of the disease, which is treated, or to reduce or delay the appearance of one or more clinical markers or symptoms of the disease.

The terms "alkyl" and "(1-C6)-alkyl" in the present invention denotes an alkyl group with a linear or branched chain with 1-6 carbon atoms, such as methyl, ethyl, propyl, isopropyl, n-butyl, sec-butyl, tert-butyl, pentyl, 2-pentyl, isopentyl, neopentyl, hexyl, 2-hexyl, 3-hexyl, and 3-methylpentyl. It should be borne in mind that in cases where the alkyl chain substituent (e.g. alkyl, alkoxy or Alchemilla group) shorter or longer chain of 6 atoms of carbon, it will also be specified in the second "S", as, for example, "(1-C10indicates a maximum of 10 carbon atoms.

The terms "alkoxy" and "(1-C6)-alkoxy" in the present invention denotes an alkyl group with a linear or branched chain with 1-6 carbon atoms, attached through at least one divalent oxygen atom, such as, for example, methoxy, ethoxy, propoxy, isopropoxy, n-butoxy, sec-butoxy, tert-butoxy, pentox, isopentane, neopentane, hexose and 3 methylpentane.

The term "ha is oven" in the present invention are denoted by fluorine, bromine, chlorine and iodine.

The terms "alkenyl" and "(2-C6)-alkenyl" refers to linear or branched hydrocarbon radical with 2-6 carbon atoms and one to three double bonds and includes, for example, ethynyl, propenyl, 1-but-3-enyl, 1-Penta-3-enyl, 1-Gex-5-enyl and similar groups.

The terms "quinil" and "(2-C6)-quinil" refers to linear or branched hydrocarbon radical with 2-6 carbon atoms and one or two triple bonds and includes ethinyl, PROPYNYL, butynyl, pentyn-2-yl and the like groups.

Used in this description, the term "cycloalkyl" refers to saturated carbocyclic radicals from three to twelve carbon atoms. Cycloalkyl may be single-core or multi-core condensed system. Examples of such radicals are cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl and cycloheptyl. Cycloalkyl group herein are unsubstituted or, as specified, substituted in one or more substitutable positions of different groups. For example, such cycloalkyl groups can be optionally substituted (C1-C6)-alkyl, (C1-C6)-alkoxy, halogen, hydroxy, cyano, nitro, amino, mono(C1-C6)alkylamino, di(C1-C6)alkylamino, (C2-C6-alkenyl, (C2-C6)-alkyne is scrap, (C1-C6-halogenation, (C1-C6)-halogenoalkane, amino(C1-C6)alkyl, mono(C1-C6)alkylamino(C1-C6)-alkyl or di(C1-C6)alkylamino(C1-C6)-alkyl.

The term "aryl" refers to aromatic carbocyclic group of from one cycle (e.g., phenyl), multiple cycles (e.g., biphenyl) or multiple condensed nuclei, of which at least one is aromatic (e.g., 1,2,3,4-tetrahydronaphthyl, naphthyl), which optionally is mono-, di - or tizamidine. Preferred aryl groups of the present invention are phenyl, 1-naphthyl, 2-naphthyl, indanyl, indenyl, dihydronaphtho, tetralinyl or 6,7,8,9-tetrahydro-5H-benzo[a]cyclopentyl. Aryl groups herein are unsubstituted or, as specified, substituted in one or more substitutable positions of different groups. For example, such aryl groups can be optionally substituted, for example, (C1-C6)-alkyl, (C1-C6)-alkoxy, halogen, hydroxy, cyano, nitro, amino, mono(C1-C6)alkylamino, di(C1-C6)alkylamino, (C2-C6-alkenyl, (C2-C6-quinil, (C1-C6-halogenation, (C1-C6)-halogenoalkane, amino(C1 -C6)alkyl, mono(C1-C6)alkylamino(C1-C6)-alkyl, di(C1-C6)alkylamino(C1-C6)-alkyl, -COOH, -C(=O)O((C1-C6)-alkyl), -C(=O)NH2, -C(=O)N(mono - or di((C1-C6)-alkyl), -S-((C1-C6)-alkyl), -SO2-((C1-C6)-alkyl), -O-C(=O)((C1-C6)-alkyl), -NH-C(=O)-((C1-C6)-alkyl), -N((C1-C6)-alkyl)-C(=O)-((C1-C6)-alkyl), -NH-SO2-((C1-C6)-alkyl), -N((C1-C6)-alkyl)-SO2-((C1-C6)-alkyl), -NH-C(=O)NH2, -NH-C(=O)N(mono - or di-(C1-C6)-alkyl), -NH((C1-C6)-alkyl)-C(=O)-NH2or-NH((C1-C6)-alkyl)-C(=O)-N-(mono - or di-(C1-C6)-alkyl).

The term "heteroaryl" refers to a system of one or more aromatic cyclic 5-, 6 - or 7-membered cycles, including the condensed-cyclic systems of 9-11 atoms containing at least one and up to four heteroatoms selected from nitrogen atoms, oxygen or sulfur. Preferred heteroaryl groups of the present invention are pyridinyl, pyrimidinyl, chinoline, benzothiazyl, indolyl, indolinyl, pyridazinyl, pyrazinyl, isoindolyl, ethanolic, hintline, honokalani, phthalazine, imidazolyl, isoxazolyl, pyrazolyl, oxazol is l, thiazolyl, indolizinyl, indazoles, benzothiazoles, benzimidazoles, benzofuranyl, furanyl, thienyl, pyrrolyl, oxadiazolyl, thiadiazolyl, triazolyl, tetrazolyl, oxazolopyridine, imidazopyridines, isothiazolin, naphthyridine, cinnoline, carbazolyl, beta-carbolines, isopropanol, bromanil, tetrahydroisoquinoline, isoindolines, isobenzofuranyl, isobenzofurandione, isobenzofuranyl, benzoxazolyl, pyridopyrimidines, bettererererer, betterregulation, purinol, benzodioxolyl, triazinyl, phenoxazines, phenothiazines, pteridinyl, benzothiazolyl, imidazopyridines, imidazothiazoles, dihydroergotoxine, benzisoxazole, benzoxazine, dihydromethysticin, benzopyranyl, benzothiophene, coumarinyl, isocoumarins, chromones, chromanones, pyridinyl-N-oxide, tetrahydroquinoline, dihydroquinoline, dihydroquinoline, dihydroisoquinoline, dihydrocoumarin, dihydroisocoumarin, isoindolines, benzodioxane, benzoxazolinone, pyrrolyl-N-oxide, pyrimidinyl-N-oxide, pyridazinyl-N-oxide, pyrazinyl-N-oxide, chinoline-N-oxide, indolyl-N-oxide, indolyl-N-oxide, ethanolic-N-oxide, hintline-N-oxide, honokalani-N-oxide, phthalazine-N-oxide, imidazolyl-N-oxide, isoxazolyl-N-oxide, oxazolyl-N-oxide, thiazolyl-N-oxide, indolizinyl-N-oxide, indazolin-N-oxide, benzothiazolyl-N-oxide, gasoline is idazole-N-oxide, pyrrolyl-N-oxide, oxadiazolyl-N-oxide, thiadiazolyl-N-oxide, triazolyl-N-oxide, tetrazolyl-N-oxide, benzothiophene-S-oxide, benzothiophene-S,S-dioxide. Heteroaryl groups herein are unsubstituted or, as specified, substituted in one or more substitutable positions of different groups. For example, such heteroaryl groups can be optionally substituted (C1-C6)-alkyl, (C1-C6)-alkoxy, halogen, hydroxy, cyano, nitro, amino, mono(C1-C6)alkylamino, di(C1-C6)alkylamino, (C2-C6-alkenyl, (C2-C6-quinil, (C1-C6-halogenation, (C1-C6)-halogenoalkane, amino(C1-C6)alkyl, mono(C1-C6)alkylamino(C1-C6)-alkyl or di(C1-C6)alkylamino(C1-C6)-alkyl, -COOH, -C(=O)O((C1-C6)-alkyl), -C(=O)NH2, -C(=O)N(mono - or di((C1-C6)-alkyl), -S-((C1-C6)-alkyl), -SO2-((C1-C6)-alkyl), -O-C(=O)((C1-C6)-alkyl), -NH-C(=O)-((C1-C6)-alkyl), -N((C1-C6)-alkyl)-C(=O)-((C1-C6)-alkyl), -NH-SO2-((C1-C6)-alkyl), -N((C1-C6)-alkyl)-SO2-((C1-C6)-alkyl), -NH-C(=O)NH2, -NH-C(=O)N(mono - or di-(C1-C6 )-alkyl), -NH((C1-C6)-alkyl)-C(=O)-NH2or-NH((C1-C6)-alkyl)-C(=O)-N-(mono - or di-(C1-C6)-alkyl).

The terms "heterocycle", "heteroseksualci" or "heterocyclyl" refers to a system of one or more of 3, 4, 5, 6 - or 7-membered cycles, including the condensed-cyclic systems of 9-11 atoms containing at least one and up to four heteroatoms selected from nitrogen atoms, oxygen or sulfur. Preferred heterocycles of the present invention are morpholinyl, thiomorpholine, thiomorpholine-S-oxide, thiomorpholine-S,S-dioxide, piperazinil, homopiperazine, pyrrolidinyl, pyrrolyl, tetrahydropyranyl, piperidinyl, tetrahydrofuranyl, tetrahydrothieno, homopiperazine, homomorpholine, homotaurine, homotaurine-S,S-dioxide, oxazolidinones, dihydropyrazolo, dihydropyrrole, dihydropyrazine, dihydropyridines, dihydropyrimidines, dihydrofuran, dihydropyran, azepane, diazepan, tetrahydrothieno-S-oxide, tetrahydrothieno-S,S-dioxide and homotaurine-S-oxide. Heterocyclyl group in this description may be unsubstituted or, as specified, substituted in one or more substitutable positions of different groups. For example, such heterocyclyl groups can be optionally substituted (C1-C6)alkyl, (C1-C6)-alkoxy, halogen, hydroxy, cyano, nitro, amino, mono(C1-C6)alkylamino, di(C1-C6)alkylamino, (C2-C6-alkenyl, (C2-C6-quinil, (C1-C6-halogenation, (C1-C6)-halogenoalkane, amino(C1-C6)alkyl, mono(C1-C6)alkylamino(C1-C6)-alkyl, di(C1-C6)alkylamino(C1-C6)-alkyl or =O.

All patents and publications cited in this specification, are included as references.

Patterns are named using the Name Pro IUPAC Naming Software, version 5.09, available from Advanced Chemical Development, Inc., 90 Adelaide Srteet West, Toronto, Ontario, M5H 3V9, Canada.

The present invention can be better understood by referring to the following examples. These examples are intended to be typical examples of specific embodiments of the invention and are not intended to limit the scope of the invention.

Chemical examples

The following detailed examples describe how you can get a variety of compounds and/or to perform various methods of the invention, and such examples should be considered only as a clarification in any way as limitations of the preceding disclosure. Specialists in the art will immediately recognize the corresponding change is to the procedures in respect of reagents, and conditions of interactions and methods.

Preparative example 1

tert-Butyl(1S)-3-bromo-1-(3,5-diferensial)-2-oxopropionate (III)

To (2S)-[(tert-butoxycarbonyl)amino]-3-(3,5-differenl)propanoic acid (II, 15 g, 50 mmol) in THF (100 ml) is added N-methylmorpholine (of 5.83 ml, 53 mmol, of 1.05 equiv.) and the reaction mixture was cooled to-78ºC. Quickly add isobutylparaben (6,87 ml, 53 mmol, of 1.05 EQ.). Then the cooling bath removed and the mixture is stirred for 1 hour. The reaction mixture was checked by TLC in order to ensure the full realization of the reaction, and the mixture is then filtered, washed with dry THF (50 ml) and stored cold in the flask to the filtrate at -20 ºc.

At bath with a mixture of ice and salt is placed 500-ml measuring cylinder containing ether (200 ml) and aqueous solution of potassium hydroxide (40%, 60 ml). Gradually under stirring was added 1-methyl-3-nitro-1-nitrosoguanidine (5.6 g, 106 mmol, 2.1 EQ.) and keep the temperature below zero degrees. The mixture becomes yellow, and bubbling continued for 10 minutes. Stirring is stopped and, without mixing the two layers, the upper diazolidinyl layer is transferred by pipette with the whole tip into the mixture with the mixed anhydride under stirring at-20ºC. The reaction is controlled by TLC (ethyl acetate/hexane, 50/50; Rf=0,69). Then after 1 hour the mixture barbotine is nitrogen. The solvent is removed under reduced pressure (when heated) and the mixture is treated with ether and water. The phases are separated, the organic phase is washed with bicarbonate solution and brine, dried over anhydrous sodium sulfate, filter and remove the solvent under reduced pressure (when heated). The residue is dissolved in ether (100 ml), at -20 ░ C add Hydrobromic acid (48%, 15 ml, 135 mmol, 2.7 equiv.) the cooling bath is removed and the mixture is stirred for another half an hour. The reaction mixture was checked by TLC (ethyl acetate/hexane, 50/50; Rf=0,88). The mixture is treated with ether and water, washed with bicarbonate solution and brine, dried over anhydrous sodium sulfate, filter and remove the solvent. The residue is recrystallized from ethanol and get called in the header connection. TLC (ethyl acetate/hexane, 50/50; Rf=0,88); MS (MH+)=379,3.

Preparative example 2

tert-Butyl(1S,2S)-3-bromo-1-(3,5-diferensial)-2-hydroxypropionate (IV)

To tert-butyl(1S)-3-bromo-1-(3,5-diferensial)-2-oxopropionate (III preparative example 1, 12 g of 31.75 mmol), dissolved in absolute alcohol (500 ml)at-78ºC add sodium borohydride (1,32 g, is 34.9 mmol, 1.1 EQ.). The reaction mixture is stirred for 30 minutes and control TLC (ethyl acetate/hexane, 20/80; Rf=0,2). The mixture was quenched with water (10 ml) and remove the solvent to the ear under reduced pressure with heating (not exceeding 30ºC). The solid is treated with dichloromethane and water and the organic portion washed with brine and dried over anhydrous sodium sulfate. The solvent is removed under reduced pressure and get called in the header connection. TLC (ethyl acetate/hexane, 20/80; Rf=0,2); MS (MH+)=381,2.

Preparative example 3

tert-Butyl(1S)-2-(3,5-diferensial)-1-[(2S)-oxiranyl]ethylcarbamate (V)

tert-Butyl(1S,2S)-3-bromo-1-(3,5-diferensial)-2-hydroxypropionate (IV preparative example 2) is dissolved in absolute alcohol (150 ml) and ethyl acetate (100 ml), at -20 ░ C add potassium hydroxide (2.3 g, is 34.9 mmol, 1.1 EQ.) in absolute alcohol (85%, 5 ml). Then the cooling bath removed and the mixture is stirred for 30 minutes. Reaction control TLC (ethyl acetate/hexane, 20/80). When the reaction is complete, the reaction mixture is diluted with dichloromethane and extragere, the extract washed with water and brine, dried over anhydrous sodium sulfate and remove the solvent under reduced pressure. The crude substance is purified flash chromatography on silica gel and get called in the header connection. TLC (ethyl acetate/hexane, 20/80; Rf=0,2), Rf=0,3; MS (MH+)=300,4.

Preparative example 4

tert-Butyl(1S,2R)-1-(3,5-diferensial)-2-hydroxy-3-[(3-(trifluoromethyl)benzyl)amino]propellernet

tert-Butyl(1S)-2-(5-diferensial)-1-[(2S)-oxiranyl]ethylcarbamate (preparative example 3, 8.5 g, 28.4 mmol) is mixed with isopropanol (145 ml). In a reaction flask is charged with 3-(trifluoromethyl)benzylamine. The reaction mixture is refluxed for 3 hours, analysis by HPLC indicates complete disappearance of the epoxide. The reaction mixture was concentrated under reduced pressure and the residue treated with ethyl acetate and hydrochloric acid. The organic phase is separated and washed with hydrochloric acid, bicarbonate solution and brine and then dried over sodium sulfate. Concentration under reduced pressure and recrystallization from hexane to give the named header connection. MS (MH+) 475.

Preparative example 5

tert-Butyl(1S,2R)-1-(3,5-diferensial)-2-hydroxy-3-{(tert-Butylochka)carbonyl-3-{(trifluoromethyl)benzyl}amino}propellernet

To a solution of tert-butyl(1S,2R)-1-(3,5-diferensial)-2-hydroxy-3-[(3-(trifluoromethyl)benzyl)amino]propylgallate (preparative example 4, 6.2 g, of 13.1 mmol) in THF (70 ml) at 0ºC add di-tert-butylpyrocatechol (6.3 g, of 28.9 mmol). The reaction mixture is stirred at 20 to 25 ° C for 18 hours. The reaction mixture was diluted with diethyl ether and washed with a solution of bicarbonate, 0.5 m citric acid and brine, then dried over sodium sulfate and concentrate and get called in the header connection. MS (MNa+) 597.

Ven is an operational example 6

3-Iodine-5-(methoxycarbonyl)benzoic acid

To commercially available 3-amino-5-(methoxycarbonyl)benzoic acid (5,19 g, 26,59 mmol) in 2n hydrochloric acid (156 ml) under ice cooling and stirring, a solution of sodium nitrite (1.84 g, 26,67 mmol) in water (10,8 ml). Then the resulting mixture under ice cooling and stirring, added dropwise to a solution of potassium iodide (8,84 g, 53,25 mmol) in water (26,2 ml). After stirring for 30 minutes the reaction mixture was diluted with water and extracted with ethyl acetate. The organic layer was washed with 5% aqueous sodium thiosulfate solution and a saturated solution of sodium chloride, dried (sodium sulfate) and concentrated under reduced pressure. Purification column flash chromatography (silica, hexane/ethyl acetate/acetic acid 50:50:2) gives named the title compound (4,48 g, yield 55%) as not quite white solid. ESI-MS (m/z 305 [M+H]+.

Preparative example 7

3-[(Dipropylamino)carbonyl]-5-(1,3-oxazol-2-yl)benzoic acid

To a solution of oxazole (4.0 g, 58 mmol) in tetrahydrofuran (100 ml) at-70ºC add n-utility (1.6 m solution in hexane, 40 ml, 64 mmol). After 30 minutes add zinc chloride (1M solution in diethyl ether, 166 ml, 166 mmol)and the reaction mixture is heated to 0ºC in those which begins 1 hour. To this mixture is added 3-iodine-5-(methoxycarbonyl)benzoic acid (preparative example 6, with 21.4 g, 55 mmol) and tetrakis(triphenylphosphine)palladium(0) (2.7 g, 2.34 mmol). The reaction mixture is refluxed for 1 hour. The reaction mixture was diluted with ethyl acetate (300 ml) and washed with water and saturated sodium chloride solution. The organic layer is dried (sodium sulfate) and concentrated under reduced pressure. Purification on a layer of silica gel (10-33% ethyl acetate/hexane) gives oxazol (17,7 g, 97%) as a pale yellow solid.1H NMR (300 MHz, CDC13) δ 8,73 (t, J=2 Hz, 1H), 8,24 (t, J=2 Hz, 1H), 8,11 (t, J=2 Hz, 1H), to 7.77 (d, J=1 Hz, 1H), 7,28 (d, J=1 Hz, 1H), of 3.97 (s, 3H), 3,49 (m, 2H), 3,19 (m, 2H), 1,71 (m, 2H), 1.57 in (m, 2H), 1,01 (m, 3H), 0.76 to (m, 3H).

To a solution of ester from step 1 (17,7 g, 53.6 mmol) in tetrahydrofuran (50 ml), methanol (25 ml) and water (25 ml) add monohydrate of lithium hydroxide (6,92 g, 165 mmol). The reaction mixture was stirred at room temperature for 2 hours and then concentrated under reduced pressure. The residue is treated with water (100 ml) and diethyl ether (100 ml). The aqueous layer was acidified to pH 4-5 with hydrochloric acid and extracted with ethyl acetate (3×200 ml). The combined organic layers washed with a saturated solution of sodium chloride, dried (sodium sulfate) and concentrated under reduced pressure to half its original volume. Received fallen in about the of ADOC substance is collected by filtration and washed with hexane and get named in the title compound (15.5 g, 91%) as not quite white solid. MP 131-133º;1H NMR (300 MHz, CD3OD) δ 8,72 (s, 1H), they were 8.22 (s, 1H), 8,10 (s, 1H), of 8.06 (d, J=1 Hz, 1H), was 7.36 (d, J=1 Hz, 1H), 3,52 (m, 2H), 3,25 (m, 2H), 1,76 (m, 2H), 1,62 (m, 2H), 1,02 (m, 3H), 0.76 to (m, 3H); APCI MS m/z 317 [M+H]+.

Preparative example 8

The dihydrochloride of (1R,2S)-2-amino-3-(3,5-differenl)-1-({[3-(trifluoromethyl)benzyl]amino}methyl)propyl-3-[(dipropylamino)carbonyl]-5-(1,3-oxazol-2-yl)benzoate

To a solution of tert-butyl(1S,2R)-1-(3,5-diferensial)-2-hydroxy-3-{(tert-Butylochka)carbonyl-3-{(trifluoromethyl)benzyl}amino}propylgallate (preparative example 5, 594 mg, 1.0 mmol) in DMF (2 ml) is added 3-[(dipropylamino)carbonyl]-5-(1,3-oxazol-2-yl)benzoic acid (preparative example 7, 316 mg, 1.0 mmol), hydrochloride of 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide (210 mg, 1.1 mmol) and 4-(dimethylamino)pyridine (146 mg, 1.2 mmol). After ~36 hours, the reaction mixture was diluted with ethyl acetate and washed with bicarbonate solution (2×) and brine (4×), then dried over sodium sulfate, filtered and concentrated under reduced pressure. The concentrate is purified flash chromatography on silica gel using the solvent ethyl acetate/hexane gradient (from 20/80 to 50/50) and receive (1R,2S)-2-[(tert-butoxycarbonyl)amino]-1-({(tert-butoxycarbonyl)[3-(trifluoromethyl)benzyl]amino}methyl)-3-(3,5-differenl)propyl-3-[(dipropylamino)carbonyl]-5-(1-oxazol-2-yl)benzoate, MC (MNa+) 895.

(1R,2S)-2-[(tert-Butoxycarbonyl)amino]-1-({(tert-butoxycarbonyl)[3-(trifluoromethyl)benzyl]amino}methyl)-3-(3,5-differenl)propyl-3-[(dipropylamino)carbonyl]-5-(1,3-oxazol-2-yl)benzoate (482 mg, 0.55 mmol) dissolved in a mixture of hydrogen chloride/dioxane (4n, 3 ml) and stirred for 1 hour at 20-25ºC. Then the solvent is removed under reduced pressure and get called in the header connection. MS (MN+) 673.

Preparative example 9

Hydrochloride N~1~-[(2R,3S)-3-amino-4-(3,5-differenl)-2-hydroxybutyl]-5-(1,3-oxazol-2-yl)-N~3~,N~3~-dipropyl-N~1~-[3-(trifluoromethyl)benzyl]isophthalamide

To a solution of tert-butyl(1S,2R)-1-(3,5-diferensial)-2-hydroxy-3-[(3-(trifluoromethyl)benzyl)amino]propylgallate (preparative example 4, 393 mg, 0.83 mmol) in DMF (2 ml) is added 3-[(dipropylamino)carbonyl]-5-(1,3-oxazol-2-yl)benzoic acid (preparative example 7, 262 mg, 0.83 mmol), hydrochloride of 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide (175 mg, of 0.91 mmol) and 4-(dimethylamino)pyridine (122 mg, 1.0 mmol). After ~18 hours the reaction mixture was diluted with ethyl acetate and washed with bicarbonate solution (2×) and brine (4×), then dried over sodium sulfate, filtered and concentrated under reduced pressure. The concentrate is purified flash chromatography on silica gel using a solvent ethylacetate/hexane gradient (from 50/5 to 70/30) and get tert-butyl(1S,2R)-1-(3,5-diferensial)-3-{[3-[(dipropylamino)carbonyl]-5-(1,3-oxazol-2-yl)benzoyl][3-(trifluoromethyl)benzyl]amino}-2-hydroxypropionate. MC (MH+) 773.

tert-Butyl(1S,2R)-1-(3,5-diferensial)-3-{[3-[(dipropylamino)carbonyl]-5-(1,3-oxazol-2-yl)benzoyl][3-(trifluoromethyl)benzyl]amino}-2-hydroxypropionate (226 mg, 0.29 mmol) dissolved in a mixture of hydrogen chloride/dioxane (4n, 2 ml) and stirred for 20 minutes at 20-25º. Then the solvent is removed under reduced pressure and the crude substance is purified HPLC with reversed phase using a gradient of solvent a acetonitrile/water with 0.5% triperoxonane acid. The obtained Sol triperoxonane acid is converted into the hydrochloride by treatment with HCl in methanol (1,25M, 5 ml). Concentration under reduced pressure gives the named header connection. MS (MN+) 673.

The following compounds get essentially according to the procedures described in the diagrams, charts, examples and formulation examples given in this description.

10 33 N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N',N'-diethyl-N-(3-active compounds)-5-methylisophthalic 1-(3-{[[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl](3-active compounds)amino]carbonyl}-5-methylbenzoyl)-L-prolinamide (1R,2S)-2-Amino-1-[(benzylamino)methyl]-3-(2-thienyl)propyl-3-(aminocarbonyl)-5-[(dipropylamino)carbonyl]benzoate Hydrochloride (1R,2S)-2-amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-(4-methyl-1,3-oxazol-2-yl)benzoate N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-N'-(2-methoxy-5-were)succinamictr> 1583
Conn.No.StructureName(s) of connections[M+H}+
9The dihydrochloride of N1-[(2R,3S)-3-amino-4-(3,5-differenl)-2-hydroxybutyl]-3-(butylsulfonyl)-N1-(3-active compounds)-D-alaninemia526
Triptorelin N1-[(2R,3S)-3-amino-4-(3,5-differenl)-2-hydroxybutyl]-N1-(3-active compounds)-N2-[(benzyloxy)carbonyl]-3-[(1-propinball)sulfonyl]-D-alaninemia702
11The hydrochloride of N1-[(2R,3S)-3-amino-4-(3,5-differenl)-2-hydroxybutyl]-N1-(3-active compounds)-3-[(1-propinball)sulfonyl]-D-alaninemia568
12N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-2-[(methylsulphonyl)amino]-1,3-thiazole-5-carboxamide539
13Bis(triptorelin) N1-[(2R,3S)-3-amino-4-(3,5-differenl)-2-hydroxybutyl]-N1-(3-active compounds)-3-[(1-propinball)sulfonyl]-L-alaninemia568
14The hydrochloride of N-[(2R,3S)-3-amino-4-(3,5-differenl)-2-hydroxybutyl]-(3-butylsulfonyl)-N-(3-active compounds)propanamide 511
15The dihydrochloride of (1R,2S)-2-amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-(butylsulfonyl)propanoate511
16The dihydrochloride of (1R,2S)-2-amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-[(dipropylamino)carbonyl]-5-(1,3-oxazol-2-yl)benzoate633
17The dihydrochloride of (1R,2S)-2-amino-3-(3,5-differenl)-1-({[(3-ethylphenyl)cyclopropyl]amino} methyl)propyl-3-[(dipropylamino)carbonyl]-5-(1,3-oxazol-2-yl)benzoate659
18The dihydrochloride of (1R,2S)-2-amino-3-(3,5-differenl)-1-({[(3-trifluoromethyl)benzyl]amino}
methyl)propyl-3-[(dipropylamino)carbonyl]-5-(1,3-oxazol-2-yl)benzoate
673
19The hydrochloride of N1-[(2R,3S)-3-amino-4-(3,5-differenl)-2-hydroxybutyl]-N(u)1(d)-(3-active compounds)-5-(1,3-oxazol-yl)-N 3N3-dipropylacetamide633
20The hydrochloride of N1-[(2R,3S)-3-amino-4-(3,5-differenl)-2-hydroxybutyl]-5-(1,3-oxazol-2-yl)-N3N3-dipropyl-N1-[3-(trifluoromethyl)benzyl]ISO-phthalamide673
21N1-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-5-(1,3-oxazol-2-yl)-N3N3-dipropyl-N1-[3-(trifluoromethyl)benzyl]ISO-phthalamide673
22(1R,2S)-2-amino-3-(3,5-differenl)-1-({[1-(3-ethynylphenyl)cyclopropyl]amino}methyl)propyl-3-[(dipropylamino)carbonyl]-5-(1,3-oxazol-2-yl)benzoate655
23The dihydrochloride of N1-[(2R,3S)-3-amino-4-(3,5-differenl)-2-hydroxybutyl]-3-(butylsulfonyl)-N1-(3-active compounds)-N2-[(methoxy)carbonyl]-D-alaninemia584
24(1R,2S)-2-Amino-3-(3,5-gift henyl)-1-{[(3-active compounds)amino]methyl}propyl-3-[(dipropylamino)carbonyl]-5-{[(2-hydroxyethyl)amino]sulfonyl}benzoate
26(1R,2S)-2-Amino-3-(3,5-differenl)-1-({[(2-isobutyl-1,3-thiazol-5-yl)methyl]amino}methyl)propyl-3-[(dipropylamino)carbonyl]-5-ethynylbenzoate
28(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-isopropylbenzyl)amino]methyl}propyl-3-[(dipropylamino)carbonyl]-5-ethynylbenzoate
30(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-isopropylbenzyl)amino]methyl}propyl-3-[(dipropylamino)carbonyl]-5-(1,3-oxazol-2-yl)benzoate
32(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-[(dipropylamino)carbonyl]-5-{[(2-hydroxy-1,1-dimethylethyl)amino]sulfonyl}benzoate
34(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-[(dipropylamino)carbonyl]-5-(4-methyl-1,3-oxazol-2-yl)benzoate
36(1R,2S)-2-Amino-3-(3,5-differenl)-1-({[(2-isobutyl-1,3-thiazol-5-yl)methyl]amino}methyl)propyl-3-[(dipropylamino)carbonyl]-5-(1,3-oxazol-2-yl)benzoate
38Hydrochloride (1R,2S)-2-amino-3-(3,5-differenl)-1-{[(3-Ativ nil)amino]methyl}propyl-3-[(dipropylamino)carbonyl]-5-{[(3-hydroxypropyl)amino]sulfonyl}benzoate
40(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-propylbenzyl)amino]methyl}propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
42(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-{[butyl(methyl)amino]carbonyl}-5-methylbenzoate
44(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-ethynylphenyl)amino]methyl}propyl-3-[(dipropylamino)carbonyl]-5-ethynylbenzoate
46(1R,2S)-2-Amino-3-(3,5-differenl)-1-({[(3-isobutylthiazole-5-yl)methyl]amino}methyl)propyl-3-[(dipropylamino)carbonyl]-5-ethynylbenzoate
48(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-[(dimethylamino)sulfonyl]-5-[(dipropylamino)carbonyl]benzoate
50Hydrochloride (1R,2S)-2-amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-[(dipropylamino)carbonyl]-5-(1,3-oxazol-2-yl)benzoate
52 (1R,2S)-2-Amino-3-(3,5-differenl)-1-({[3-(5-formyl-2-thienyl)benzyl]amino}methyl)propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
54(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-iodobenzyl)amino]methyl}propyl-3-bromo-5-[(dipropylamino)carbonyl]benzoate
56(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-[(dipropylamino)carbonyl]-5-({[(1R)-2-hydroxy-1-methylethyl]amino}sulfonyl)benzoate
58(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-isobutylphenyl)amino]methyl}propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
60(1R,2S)-2-Amino-3-(3,5-differenl)-1-({[3-(trifluoromethyl)benzyl]amino}methyl)Pro-drank-3-[(dipropylamino)carbonyl]-5-ethynylbenzoate
62Hydrochloride (1R,2S)-2-amino-3-(3,5-differenl)-1-{[3-active compounds)amino]methyl}propyl-3-{[(2R)-2-(methoxymethyl peer who ridin-1-yl]carbonyl}-5-methylbenzoate
64(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[3-active compounds)amino]methyl}propyl-3-[(dipropylamino)carbonyl]-5-({[(1S)-2-hydroxy-1-methylethyl]amino}sulfonyl)benzoate
66(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[3-active compounds)amino]methyl}propyl-3-{[butyl(propyl)amino]carbonyl}-5-methylbenzoate
68(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[3-active compounds)amino]methyl}propyl-3-[(dibutylamino)carbonyl]-5-methylbenzoate
70(1R,2S)-2-Amino-3-(3,5-differenl)-1-({[3-(3-hydroxyprop-1-Jn-1-yl)benzyl]amino}methyl)propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
72(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[3-active compounds)amino]methyl}propyl-3-[(dipropylamino)carbonyl]-5-{[(2S)-2-(hydroxymethyl)pyrrolidin-1-yl]sulfonyl}benzoate
74(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[3-active compounds)amino]methyl}propyl-3-{[butyl(ethyl)amino]carbonyl}-5-methylbenzoate
76(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[3-ethynylphenyl)amino]methyl}propyl-3-[(dipro is ylamino)carbonyl]-5-(1,3-oxazol-2-yl)benzoate
78(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[3-active compounds)amino]methyl}propyl-3-{[cyclohexyl(methyl)amino]carbonyl}-5-methylbenzoate
80(1R,2S)-2-Amino-1-({[3-(cyclopropylamino)benzyl]amino}methyl)-3-(3,5-differenl)propyl-3-[(dipropylamino)carbonyl]-5-ethynylbenzoate
82(1R,2S)-2-Amino-3-(3,5-differenl)-1-({[3-(3-thienyl)benzyl]amino}methyl)propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
84(1R,2S)-2-Amino-3-(3,5-differenl)-1-({[3-(trifluoromethyl)benzyl]amino}methyl)propyl-3-[(dipropylamino)carbonyl]-5-(1,3-oxazol-2-yl)benzoate
86The dihydrochloride of (1R,2S)-2-amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-[(dipropylamino)carbonyl]-5-(piperazine-1-ylsulphonyl)benzoate
88(1R,2S)-2-Amino-3-(3,5-differenl)-1-({[1-(3-itfeel)cyclopropyl]amino}methyl)propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
90(1R,2S)-2-Amino-1-{[(3-second-butylbenzyl)amino]methyl}-3-(3,5-differenl)propyl-3-[(dipr is palamino)carbonyl]-5-methylbenzoate
92Hydrochloride (1R,2S)-2-amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-[(dipropylamino)carbonyl]-5-(3-methylisoxazol-4-yl)benzoate
94(1R,2S)-2-Amino-3-(3,5-differenl)-1-({[1-(3-isobutylthiazole-5-yl)cyclopropyl]amino}methyl)propyl-3-[(dipropylamino)carbonyl]-5-(1,3-oxazol-2-yl)benzoate
96(1R,2S)-2-Amino-3-(3,5-differenl)-1-({[1-(3-ethylphenyl)cyclopropyl]amino}methyl)propyl-3-[(dipropylamino)carbonyl]-5-(1,3-oxazol-2-yl)benzoate
98(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-2-[(dipropylamino)carbonyl]-6-methylethanolamine
100(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-{[(cyclopropylmethyl)(propyl)amino]carbonyl}-5-methylbenzoate
102(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-methoxybenzyl)amino]methyl}propyl-3-[(dipropylamino)carbonyl]-5-(1,3-oxazol-2-yl)benzoate
104(1R,2S)-2-Amino-3-(3,5-differenl)-1-({[1-(3-ethynylphenyl)is ecoprofile]amino}methyl)propyl-3-[(dipropylamino)carbonyl]-5-(1,3-oxazol-2-yl)benzoate
106(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-(aminosulfonyl)-5-[(dipropylamino)carbonyl]benzoate
108(1R,2S)-2-Amino-3-(3,5-differenl)-1-[({3-[(1Z)-prop-1-EN-1-yl]benzyl}amino)methyl]propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
110Hydrochloride (1R,2S)-2-amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-[(dipropylamino)carbonyl]-5-(1H-pyrazole-4-yl)benzoate
112(1R,2S)-2-Amino-3-(3,5-differenl)-1-({[1-(3-ethylphenyl)-1-methylethyl]amino}methyl)propyl-3-[(dipropylamino)carbonyl]-5-ethynylbenzoate
114(1R,2S)-2-Amino-3-(3,5-differenl)-1-({[3-(trifluoromethyl)benzyl]amino}methyl)propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
116(1R,2S)-1-{[(3-allylbenzene)amino]methyl}-2-amino-3-(3,5-differenl)propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
118(1R,2S)-2-Amino-3-(3,5-differenl)-1-({[1-(3-ethylphenyl)cyclopropyl]amino}methyl)propyl-3-[(dipropylamino carb is Neil]-5-methylbenzoate
120(1R,2S)-2-Amino-3-(3,5-differenl)-1-({[1-(3-ethylphenyl)-1-methylethyl]amino}methyl)propyl-3-[(dipropylamino)carbonyl]-5-(1,3-oxazol-2-yl)benzoate
122(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-{[ethyl(propyl)amino]carbonyl}-5-methylbenzoate
124(1R,2S)-2-Amino-1-({[3-(cyclopropylamino)benzyl]amino}methyl)-3-(3,5-differenl)propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
126(1R,2S)-2-Amino-3-(3,5-differenl)-1-({[1-(3-ethynylphenyl)cyclopropyl]amino}methyl)propyl-3-[(dipropylamino)carbonyl]-5-ethynylbenzoate
128(1R,2S)-2-Amino-3-(3,5-differenl)-1-({[1-(3-isobutylthiazole-5-yl)cyclopropyl]amino}methyl)propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
130(1R,2S)-2-Amino-3-(3,5-differenl)-1-({[3-(5-formyl-4-methyl-2-thienyl)benzyl]amino}methyl)propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
132(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-isopropylbenzyl)amino]methyl}prop is l-5-[(dipropylamino)carbonyl]nicotinate
134(1R,2S)-2-Amino-3-(3,5-differenl)-1-[({3-[(methylsulphonyl)amino]benzyl}amino)methyl]propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
136(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-[(butylamino)carbonyl]-5-methylbenzoate
138(1R,2S)-2-Amino-3-(3,5-differenl)-1-({[3-(3-methylbutyl)benzyl]amino}methyl)propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
140(1R,2S)-2-Amino-1-{[(biphenyl-3-ylmethyl)amino]methyl}-3-(3,5-differenl)propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
142(1R,2S)-2-Amino-3-(3,5-differenl)-1-({[1-(3-ethynylphenyl)cyclopropyl]amino}methyl)propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
144Hydrochloride (1R,2S)-2-amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-[(dipropylamino)carbonyl]-5-({[2-(methylamino)ethyl]amino}sulfonyl)benzoate
146(1R,2S)-2-Amino-3-(3,5-differenl)-1-({[1-(3-isobutylthiazole-5-yl)cyclopropyl]amino}met the l)propyl-3-[(dipropylamino)carbonyl]-5-ethynylbenzoate
148(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-[(diallylamine)carbonyl]-5-methylbenzoate
150(1R,2R)-2-Amino-3-(3,5-differenl)-1-({[1-(2-isobutyl-1,3-thiazol-5-yl)cyclopropyl]amino}methyl)propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
152(1R,2S)-2-Amino-3-(3,5-differenl)-1-({[1-(3-ethylphenyl)-1-methylethyl]amino}methyl)propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
154(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-{[(2-hydroxyethyl)amino]sulfonyl}-5-[(propylamino)carbonyl]benzoate
156(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-methyl-5-{[methyl(propyl)amino]carbonyl}benzoate
158 Hydrochloride (1R,2S)-2-amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-N-(phenylsulfonyl)-3-[(1-propinball)sulfonyl]alaninate
160(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-[(diethylamino)carbonyl]-5-(1,3-oxazol-2-yl)benzoate
162Triptorelin (1R,2S)-2-amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-N-[(benzylamino)carbonyl]-3-[(1-propinball)sulfonyl]alaninate
164(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-pyridin-3-ylbenzyl)amino]methyl}propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
1661-Oxide (1R,2S)-2-amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-5-[(dipropylamino)carbonyl]nicotinate
168(1R,2S)-2-Amino-3-(3,5-differenl)-1-({[3-(3-formyl-2-furyl)benzyl]amino}methyl)propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
170(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-[(dipropylamino)carbonyl]-5-(1-methyl-1H-imidazol-2-yl)benzoate
172(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-[(diethylamino)carbonyl]-5-methylbenzoate
174(1R,2S)-2-Amino-3-(3,5-differenl)-1-({[3-(ethylsulfonyl)benzyl]amino}methyl)propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
176(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-{[butyl(ethyl)amino]sulfonyl}propanoate
178(1R,2S)-2-Amino-1-{[(3-cyanobenzyl)amino]methyl}-3-(3,5-differenl)propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
180Hydrochloride (1R,2S)-2-amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-[(1-propinball)sulfonyl]propanoate
182(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-{[isobutyl(methyl)amino]carbonyl}-5-methylbenzoate
184
186(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-pyridin-2-ylbenzyl)amino]methyl}propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
188(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-iodobenzyl)amino]methyl}propyl-2-[(methylsulphonyl)amino]-1,3-oxazol-4-carboxylate
190(1R,2S)-2-Amino-3-(3,5-differenl)-1-[({3-[methyl - (methylsulphonyl)amino]benzyl}
amino)methyl]propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
192Triptorelin (1R,2S)-2-amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-N-(3-phenylpropenoyl)-3-[(1-propinball)sulfonyl]alaninate
194(1R,2S)-2-Amino-3-(3,5-differenl)-1-({[3-(ethylsulfonyl)benzyl]amino}methyl)propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
196 Hydrochloride (1R,2S)-2-amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-N-[(5-chloro-2-thienyl)sulfonyl]-3-[(1-propinball)sulfonyl]alaninate
198(1R,2S)-1-({[3-(5-Acetyl-2-thienyl)benzyl]amino}methyl)-2-amino-3-(3,5-differenl)propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
200(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-[(Deut-butylamino)carbonyl]-5-methylbenzoate
202Hydrochloride (1R,2S)-2-amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-(1,3-oxazol-2-yl)benzoate
204(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-methyl-5-{[methyl(2-phenylethyl)amino]carbonyl}benzoate
206(1R,2S)-2-Amino-3-(3,5-differenl)-1-({[3-(3,5-dimethylisoxazol-4-yl)benzyl]amino}methyl)propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
208(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-methyl-5-{[methyl(prop-2-in-1-yl)amino]carbonyl}benzoate
210 (1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-{[ethyl(methyl)amino]carbonyl}-5-methylbenzoate
212(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-{[(dimethylamino)carbonyl]oxy}benzyl)amino]methyl}propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
214(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-{[benzyl(methyl)amino]carbonyl}-5-methylbenzoate
216(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-{[Deut-butyl(propyl)amino]carbonyl}-5-methylbenzoate
218(1R,2S)-2-Amino-3-(3,5-differenl)-1-({[3-(4-methyl-2-thienyl)benzyl]amino}methyl)propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
220(1R,2S)-2-Amino-3-(3,5-differenl)-1-[({3-[(methoxycarbonyl)(methyl)amino]benzyl}amino)methyl] propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
222(1R,2S)-2-Amino-1-({[3-(trifluoromethyl)benzyl]amino}methyl)- 3-(2,3,5-tryptophanyl)propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
224 (1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-[(diisobutylamine)carbonyl]-5-methylbenzoate
226(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-methyl-5-{[methyl(2-pyridin-2-retil)amino]carbonyl}benzoate
228Hydrochloride (1R,2S)-2-amino-3-(3-fluoro-5-hydroxyphenyl)-1-{[(3-methoxybenzyl)amino]methyl}propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
230(1R,2S)-2-Amino-3-(3-chloro-5-forfinal)-1-{[(3-methoxybenzyl)amino]methyl}propyl-3-(aminocarbonyl)-5-[(dipropylamino)carbonyl]benzoate
232(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-iodobenzyl)amino]methyl}propyl-4-hydroxy-3-(pyrrolidin-1-ylcarbonyl)benzoate
234Hydrochloride (1R,2S)-2-amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-5-oxo-D-propyl-3-[(1-propinball)sulfonyl]alaninate
236
238 (1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-pyridin-4-ylbenzyl)amino]methyl}propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
240(1R,2S)-2-Amino-3-(3,5-differenl)-1-[({3-[(dimethylamino)sulfonyl]benzyl}amino)methyl]propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
242(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(6-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl)amino]methyl}propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
244(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-N-(phenylacetyl)-3-[(1-propinball)sulfonyl]alanine
246(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-(azepin-1-ylcarbonyl)-5-methylbenzoate
248(1R,2S)-2-Amino-3-(3,5-differenl)-1-[({3-[(methoxycarbonyl)amino]benzyl}amino)methyl]propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
250Hydrochloride (1R,2S)-2-amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-5-oxo-L-prolyl-3-[(1-propinball)su is hanil]alaninate
252(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[3-active compounds)amino]methyl}propyl-3-[(isobutylamino)carbonyl]-5-methylbenzoate
254Triptorelin 4-[((1R,2S)-2-amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl)oxy]-4-oxo-3-{[(1-propinball)sulfonyl]methyl}butane acid
256(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-[methyl - (methylsulphonyl)amino]benzoate
25N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-5-{[(2-hydroxyethyl)amino]sulfonyl}-N',N'-dipropylacetamide
27N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-5-ethinyl-N-[(2-isobutyl-1,3-thiazol-5-yl)methyl]-N',N'-dipropylacetamide
29N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-5-ethinyl-N-(3-isopropylbenzyl)-N',N'-dipropylacetamide
31N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-isopropylbenzyl)-5-(1,3-oxazol-2-yl)-N',N'-dipropylacetamide
N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-5-{[(2-hydroxy-1,1-dimethylethyl)amino]sulfonyl}-N',N'-dipropylacetamide
35N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-5-(4-methyl-1,3-oxazol-2-yl)-N',N'-dipropylacetamide
37N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-[(2-isobutyl-1,3-thiazol-5-yl)methyl]-5-(1,3-oxazol-2-yl)-N',N'-dipropylacetamide
39The hydrochloride of N-[(2R,3S)-3-amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-5-{[(3-hydroxypropyl)amino]sulfonyl}-N',N'-dipropylacetamide
41N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-5-methyl-N',N'-dipropyl-N-(3-propylbenzyl)isophthalamide
43N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N'-butyl-N-(3-active compounds)-N',5-dimethylacetamide
45N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-5-ethinyl-N-(3-ethynylphenyl)-N',N'-dipropylacetamide
47 N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-5-ethinyl-N-[(3-isobutylthiazole-5-yl)methyl]-N',N'-dipropylacetamide
49N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-5-[(dimethylamino)sulfonyl]-N-(3-active compounds)-N',N'-dipropylacetamide
51The hydrochloride of N-[(2R,3S)-3-amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-5-(1,3-oxazol-2-yl)-N',N'-dipropylacetamide
53N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-[3-(5-formyl-2-thienyl)benzyl]-5-methyl-N',N'-dipropylacetamide
55N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-5-bromo-N-(3-iodobenzyl)-N',N'-dipropylacetamide
57N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-5-({[(1R)-2-hydroxy-1-methylethyl]amino}sulfonyl)-N',N'-dipropylacetamide
59N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-isobutylphenyl)-5-methyl-N',N'-dipropylacetamide
61N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-5-ethinyl-N',N'-dipropyl-N-[3-(trifluoromethyl)benzyl]isophthalamide
63The hydrochloride of N-[(2R,3S)-3-amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-3-{[(2R)-2-(methoxymethyl)pyrrolidin-1-yl]carbonyl}-5-methylbenzamide
65N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-5-({[(1S)-2-hydroxy-1-methylethyl]amino}sulfonyl)-N',N'-dipropylacetamide
67N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N'-butyl-N-(3-active compounds)-5-methyl-N'-propylacetamide
69N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N',N'-dibutil-N-(3-active compounds)-5-methylisophthalic
71N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-[3-(3-hydroxyprop-1-Jn-1-yl)benzyl]-5-methyl-N',N'-dipropylacetamide
73N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-5-{[(2S)-2-(hydroxymethyl)pyrrolidin-1-yl]sulfonyl}-N',N'-dipropylacetamide
75N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N'-butyl-N'-ethyl-N-(3-active compounds)-5-methylisophthalic
77N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-5-(1,3-oxazol-2-yl)-N',N'-dipropylacetamide
79N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N'-cyclohexyl-N-(3-active compounds)-N',5-dimethylacetamide
81N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-[3-(cyclopropylamino)benzyl]-5-ethinyl-N',N'-dipropylacetamide
83N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-5-methyl-N',N'-dipropyl-N-[3-(3-thienyl)benzyl]isophthalamide
85N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-5-(1,3-oxazol-2-yl)-N',N'-dipropyl-N-[3-(trifluoromethyl)benzyl]isophthalamide
87The dihydrochloride of N-[(2R,3S)-3-amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-5-(piperazine-1-ylsulphonyl)-N',N'-dipropylacetamide
89N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-[1-(3-itfeel)cyclopropyl]-5-methyl-N',N'-dipropylacetamide
91 N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-second-butylbenzyl)-5-methyl-N',N'-dipropylacetamide
93The hydrochloride of N-[(2R,3S)-3-amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-5-(3-methylisoxazol-4-yl)-N',N'-dipropylacetamide
95N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-[1-(3-isobutylthiazole-5-yl)cyclopropyl]-5-(1,3-oxazol-2-yl)-N',N'-dipropylacetamide
97N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-[1-(3-ethylphenyl)cyclopropyl]-5-(1,3-oxazol-2-yl)-N',N'-dipropylacetamide
99N4-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N4-(3-active compounds)-6-methyl-N2N2-DIPROPYLENE-2,4-dicarboxamide
101N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N'-(cyclopropylmethyl)-N-(3-active compounds)-5-methyl-N'-propylacetamide
103N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-methoxybenzyl)-5-(1,3-oxazol-2-yl)-N',N'-dipropylacetamide
105 N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-[1-(3-ethynylphenyl)cyclopropyl]-5-(1,3-oxazol-2-yl)-N',N'-dipropylacetamide
107N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-5-(aminosulfonyl)-N-(3-active compounds)-N',N'-dipropylacetamide
109N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-5-methyl-N-{3-[(1Z)-prop-1-EN-1-yl]benzyl}-N',N'-dipropylacetamide
111The dihydrochloride of N-[(2R,3S)-3-amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-N',N'-dipropyl-5-(1H-pyrazole-4-yl)isophthalamide
113N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-[1-(3-ethylphenyl)-1-methylethyl]-5-ethinyl-N',N'-dipropylacetamide
115N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-5-m is Teal-N',N'-dipropyl-N-[3-(trifluoromethyl)benzyl]isophthalamide
117N-(3-Allylbenzene)-N-[(2R,3S)-3-amino-4-(3,5-differenl)-2-hydroxybutyl]-5-methyl-N',N'-dipropylacetamide
119N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-[1-(3-ethylphenyl)cyclopropyl]-5-methyl-N',N'-dipropylacetamide
121N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-[1-(3-ethylphenyl)-1-methylethyl]-5-(1,3-oxazol-2-yl)-N',N'-dipropylacetamide
123N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N'-ethyl-N-(3-active compounds)-5-methyl-N'-propylacetamide
125N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-[3-(cyclopropylamino)benzyl]-5-methyl-N',N'-dipropylacetamide
127N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-5-ethinyl-N-[1-(3-ethynylphenyl)cyclopropyl]-N',N'-dipropylacetamide
129N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-[1-(3-isobut isoxazol-5-yl)cyclopropyl]-5-methyl-N',N'-dipropylacetamide
131N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-[3-(5-formyl-4-methyl-2-thienyl)benzyl]-5-methyl-N',N'-dipropylacetamide
133N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-isopropylbenzyl)-N',N'-DIPROPYLENE-3,5-dicarboxamide
135N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-5-methyl-N-{3-[(methylsulphonyl)amino]benzyl}-N',N'-dipropylacetamide
137N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N'-butyl-N-(3-active compounds)-5-methylisophthalic
139N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-5-methyl-N-[3-(3-methylbutyl)benzyl]-N',N'-dipropylacetamide
141N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(biphenyl-3-ylmethyl)-5-methyl-N',N'-dipropylacetamide
143N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-[1-(3-ethynylphenyl)cyclopropyl]-5-methyl-N',N'-dipropylacetamide
145 The hydrochloride of N-[(2R,3S)-3-amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-5-({[2-(methylamino)ethyl]amino}sulfonyl)-N',N'-dipropylacetamide
147N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-5-ethinyl-N-[1-(3-isobutylthiazole-5-yl)cyclopropyl]-N',N'-dipropylacetamide
149N,N-diallyl-N'-[(2R,3S)-3-amino-4-(3,5-differenl)-2-hydroxybutyl]-N'-(3-active compounds)-5-methylisophthalic
151N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-[1-(2-isobutyl-1,3-thiazol-5-yl)cyclopropyl]-5-methyl-N',N'-dipropylacetamide
153N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-[1-(3-ethylphenyl)-1-methylethyl]-5-methyl-N',N'-dipropylacetamide
155N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-5-{[(2-hydroxyethyl)amino]sulfonyl}-N'-propylacetamide
157N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-N,5-dimethyl-N'-propylacetamide
159Hydrochlor the d N 1-[(2R,3S)-3-amino-4-(3,5-differenl)-2-hydroxybutyl]-N1-(3-active compounds)-N2-(phenylsulfonyl)-3-[(1-propinball)sulfonyl]alaninemia
161N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N',N'-diethyl-N-(3-active compounds)-5-(1,3-oxazol-2-yl)isophthalamide
163Triptorelin (Sol) N1-[(2R,3S)-3-amino-4-(3,5-differenl)-2-hydroxybutyl]-N2-[(benzylamino)carbonyl]-N1-(3-active compounds)-3-[(1-propinball)sulfonyl]alaninemia
165N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-5-methyl-N',N'-dipropyl-N-(3-pyridin-3-ylbenzyl)isophthalamide
1671-Oxide N-[(2R,3S)-3-amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-N',N'-DIPROPYLENE-3,5-dicarboxamide
169N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N'-ethyl-N-[3-(3-formyl-2-furyl)benzyl]5-methyl-N'-propylacetamide
171N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-5-(1-methyl-1H-imidazol-2-yl)-N',N'-dipropylacetamide
173
175N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-[3-(ethylsulfonyl)benzyl]-5-methyl-N',N'-dipropylacetamide
177N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-3-{[butyl(ethyl)amino]sulfonyl}-N-(3-active compounds)propanamide
179N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-cyanobenzyl)-5-methyl-N',N'-dipropylacetamide
181The hydrochloride of N-[(2R,3S)-3-amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-3-[(1-propinball)sulfonyl]propanamide
183N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-N'-isobutyl-N',5-dimethylacetamide
185
187N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-5-methyl-N',N'-dipropyl-N-(3-pyridin-2-ILB nil)isophthalamide
189N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-iodobenzyl)-2-[(methylsulphonyl)amino]-1,3-oxazol-4-carboxamid
191N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-5-methyl-N-{3-[methyl - (methylsulphonyl)amino]benzyl}-N',N'-dipropylacetamide
193Triptorelin (Sol) N1-[(2R,3S)-3-amino-4-(3,5-differenl)-2-hydroxybutyl]-N1-(3-active compounds)-N2-(3-phenylpropenoyl)-3-[(1-propinball)sulfonyl]alaninemia
195N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-[3-(ethylsulfonyl)benzyl]-5-methyl-N',N'-dipropylacetamide
197The hydrochloride of N1-[(2R,3S)-3-amino-4-(3,5-differenl)-2-hydroxybutyl]-N2-[(5-chloro-2-thienyl)sulfonyl]-N1-(3-active compounds)-3-[(1-propinball)sulfonyl]alaninemia
199N-[3-(5-Acetyl-2-thienyl)benzyl]-N-[(2R,3S)-3-amino-4-(3,5-differenl)-2-hydroxybutyl]-5-methyl-N',N'-dipropylacetamide
201N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N'-(sec-butyl)-N-(3-active compounds)-5-methylisophthalic
203The hydrochloride of N-[(2R,3S)-3-amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-3-(1,3-oxazol-2-yl)benzamide
205N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-N,5-dimethyl-N'-(2-phenylethyl)isophthalamide
207N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-[3-(3,5-dimethylisoxazol-4-yl)benzyl]-5-methyl-N',N'-dipropylacetamide
209N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-N,5-dimethyl-N'-prop-2-in-1-resoftened
211N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N'-ethyl-N-(3-active compounds)-N',5-dimethylacetamide
2133-[([(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]{3-[(is, dipropylamino)carbonyl]-5-methylbenzoyl}amino)methyl]phenyldimethylsilane
215N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N'-benzyl-N-(3-active compounds)-N',5-dimethylacetamide
217N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N'-(sec-butyl)-N-(3-active compounds)-5-methyl-N'-propylacetamide
219N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-5-methyl-N-[3-(4-methyl-2-thienyl)benzyl]-N',N'-dipropylacetamide
221Methyl-{3-[([(2R,3S)-3-amino-4-(3,5-differenl)-2-hydroxybutyl]{3-[(dipropylamino)carbonyl]-5-methylbenzoyl}amino)methyl]phenyl}methylcarbamate
223N-[(2R,3S)-3-Amino-2-hydroxy-4-(2,3,5-tryptophanyl)butyl]-5-methyl-N',N'-dipropyl-N-[3-(trifluoromethyl)benzyl]isophthalamide
225N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-N',N'-Diisobutyl-5-methylisophthalic
227N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-N,5-dimethyl-N'-(2-pyridin-2-retil)isophthalamide
229 The hydrochloride of N-[(2R,3S)-3-amino-4-(3-fluoro-5-hydroxyphenyl)-2-hydroxybutyl]-N-(3-methoxybenzyl)-5-methyl-N',N'-dipropylacetamide
231N1-[(2R,3S)-3-Amino-4-(3-chloro-5-forfinal)-2-hydroxybutyl]-N1-(3-methoxybenzyl)-N3N3-DIPROPYLENE-1,3,5-tricarboxylic
233N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-4-hydroxy-N-(3-iodobenzyl)-3-(pyrrolidin-1-ylcarbonyl)benzamide
235Hydrochloride 5-oxo-D-prolyl-N1-[(2R,3S)-3-amino-4-(3,5-differenl)-2-hydroxybutyl]-N1-(3-active compounds)-3-[(1-propinball)sulfonyl]alaninemia
237
239N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-5-methyl-N',N'-dipropyl-N-(3-pyridin-4-ylbenzyl)isophthalamide
241N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-{3-[(dimethylamino)sulfonyl]benzyl}-5-methyl-N',N'-dipropyl isophthalamide
243N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(6-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl)-5-methyl-N',N'-dipropylacetamide
245N1-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N1-(3-active compounds)-N2(phenylacetyl)-3-[(1-propinball)sulfonyl]alanine
247N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-3-(azepin-1-ylcarbonyl)-N-(3-active compounds)-5-methylbenzamide
249Methyl-{3-[([(2R,3S)-3-amino-4-(3,5-differenl)-2-hydroxybutyl]{3-[(dipropylamino)carbonyl]-5-methylbenzoyl}amino)methyl]phenyl}carbamate
251Hydrochloride 5-oxo-L-propyl-N1-[(2R,3S)-3-amino-4-(3,5-differenl)-2-hydroxybutyl]-N1-(3-active compounds)-3-[(1-propinball)sulfonyl]alaninemia
253N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-N'-isobutyl-5-methylisophthalic
255Triptorelin (g) 4-[[(2R,3S)-3-the Mino-4-(3,5-differenl)-2-hydroxybutyl]-(3-active compounds)amino]-4-oxo-3-{[(1-propinball)sulfonyl]methyl}butane acid
257N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-3-[methyl - (methylsulphonyl)amino]benzamide
258(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-{[ethyl(isopropyl)amino]carbonyl}-5-methylbenzoate
260(1R,2S)-2-Amino-1-{[(3-methoxybenzyl)amino]methyl}-3-(2-thienyl)propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
262(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-{[(2-hydroxyethyl)(propyl)amino]sulfonyl}propanoate
264(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-{[isopropyl(methyl)amino]carbonyl}-5-methylbenzoate
266(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-2-[(methylsulphonyl)amino]-1,3-thiazole-4-carboxylate
268(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-{[allyl(cyclopentyl)amino]carbonyl}-5-methylbenzoate
270
272(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-[(3-methylbutyl)sulfonyl]propanoic
274(1R,2S)-2-Amino-3-(3,5-differenl)-1-({[3-(5-methyl-2-thienyl)benzyl]amino}methyl)propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
276(1R,2S)-2-Amino-1-{[(3-methoxybenzyl)amino]methyl}-3-(3-methoxyphenyl)propyl-3-(aminocarbonyl)-5-[(dipropylamino)carbonyl]benzoate
278(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(1-etylhexyl)amino]methyl}propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
280(1R,2S)-2-Amino-1-({[1-(aminocarbonyl)cyclohexyl]amino}methyl)-3-(3,5-differenl)propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
282(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(2E)-Gex-2-EN-1-and what amino)methyl]propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
284(1R,2S)-2-Amino-3-(4-forfinal)-1-{[(3-methoxybenzyl)amino]methyl}propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
286(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-hydroxyethoxy-5-carboxylate
288(1R,2S)-2-Amino-3-(3,5-differenl)-1-[({3-[(1E)-Gex-1-EN-1-yl]benzyl}amino)methyl]propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
290(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-[(isopropylamino)carbonyl]-5-methylbenzoate
292(1R,2S)-2-Amino-1-{[(3-methoxybenzyl)amino]methyl}-3-(2-thienyl)propyl-3-(aminocarbonyl)-5-[(dipropylamino)carbonyl]benzoate
294(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-iodobenzyl)amino]methyl}propyl-3-[3-(2-amino-2-oksidoksi)phenyl]acetate
296(1R,2S)-2-Amino-3-(3-bromophenyl)-1-{[(3-methoxybenzyl)amino]methyl}propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
298 (1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(2-ethylhexyl)amino]methyl}propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
300(1R,2S)-2-Amino-3-(3,5-differenl)-1-({[3-(6-methoxypyridine-3-yl)benzyl]amino}methyl)propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
302(1R,2S)-2-Amino-3-(3,5-differenl)-1-({[3-(2,4-dimethoxypyrimidine-5-yl)benzyl]amino}methyl)propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
304(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-(2-ethylbutanol)benzoate
306(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-[(4-hydroxypiperidine-1-yl)carbonyl]-5-methylbenzoate
308(1R,2S)-2-Amino-3-(3-bromophenyl)-1-{[(3-methoxybenzyl)amino]methyl}propyl-3-(aminocarbonyl)-5-[(dipropylamino)carbonyl]benzoate
310(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-iodobenzyl)amino]methyl}propyl-4-[2'-(aminocarbonyl)biphenyl-4-yl]-4-oxobutanoate
312
314(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-[(3-hydroxypiperidine-1-yl)carbonyl]-5-methylbenzoate
316(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-hydroxy-1-phenylpropyl)amino]methyl}propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
318(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-{[[2-(dimethylamino)ethyl](ethyl)amino] carbonyl}-5-methylbenzoate
320(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-4-methyl-4H,6N-pyrrolo[1,2-a][4,1]benzoxazepin-4-carboxylate
322(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl(5-acetyl-2-thienyl)acetate
324(1R,2S)-2-Amino-3-(3,5-dichlorophenyl)-1-{[(3-methoxybenzyl)amino]methyl}propyl-3-(aminocarbonyl)-5-[(dipropylamino)Carboni is]benzoate
326(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-[(diisopropylamino)carbonyl]-5-methylbenzoate
328(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-[(methylsulphonyl)amino]benzoate
330(1R,2S)-2-Amino-3-(4-chlorophenyl)-1-{[(3-methoxybenzyl)amino]methyl}propyl-3-(aminocarbonyl)-5-[(dipropylamino)carbonyl]benzoate
332(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-iodobenzyl)amino]methyl}propyl[4-(2-oxopyrrolidin-1-yl)phenyl]acetate
334(1R,2S)-2-Amino-3-(3-chloro-5-forfinal)-1-{[(3-methoxybenzyl)amino]methyl}propyl-3-[(dipropylamino)sulfonyl]propanoic
336(1R,2S)-2-Amino-3-(3-chloro-5-forfinal)-1-{[(3-methylbutyl)amino]methyl}propyl-3-(aminocarbonyl)-5-[(dipropylamino)carbonyl]benzoate
338
340Trihydrochloride (1R,2S)-2-AMI is about-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-{[(1-methyl-1H-imidazol-4-yl)sulfonyl]amino}benzoate
342(1R,2S)-2-Amino-3-(3,5-differenl)-1-[(pentylamine)methyl]propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
344(1R,2S)-2-Amino-3-(4-forfinal)-1-{[(3-methoxybenzyl)amino]methyl}propyl-3-(aminocarbonyl)-5-[(dipropylamino)carbonyl]benzoate
346(1R,2S)-2-Amino-1-[(benzylamino)methyl]-3-(3-chloro-5-forfinal)propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
348(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-{[cyclohexyl(ethyl)amino]carbonyl}-5-methylbenzoate
350(1R,2S)-2-Amino-3-(3,5-differenl)-1-({[2-({[(2,4-differenl)amino]carbonyl}oxy)ethyl]amino}methyl)propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
352Hydrochloride (1R,2S)-2-amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-{[(2S)-2-(methoxymethyl)pyrrolidin-1-yl]carbonyl}-5-methylbenzoate
354(1R,2S)-2-Amino-3-(3-fluoro-4-were)-1-{[(3-methoxybenzyl)amino]methyl}propyl-3-(aminocarbonyl)-5-[(diprop the laminitis)carbonyl]benzoate
356(1R,2S)-2-Amino-3-(3-bromophenyl)-1-{[(3-methylbutyl)amino]methyl}propyl-3-(aminocarbonyl)-5-[(dipropylamino)carbonyl]benzoate
358(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-2,8-dimethylindoline-3-carboxylate
360(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(6-hydroxyhexyl)amino]methyl}propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
362(1R,2S)-2-Amino-3-(3,5-differenl)-1-({[(2R)-2-hydroxypropyl]amino}methyl)propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
364(1R,2S)-2-Amino-1-{[(3-methoxybenzyl)amino]methyl}-3-phenylpropyl-3-[(1-propinball)sulfonyl]propanoic
366(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-{[(2-hydroxy-1,1-dimethylethyl)amino]sulfonyl}benzoate
368(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(4-phenylbutyl)amino]methyl}propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
370 (1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-iodobenzyl)amino]methyl}propyl-7-(1H-imidazol-1-yl)-5,6-dihydronaphthalene-2-carboxylate
372(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-(acetylamino)-4-methylbenzoate
374(1R,2S)-2-Amino-1-({[2-(aminosulfonyl)ethyl]amino}methyl)-3-(3,5-differenl)propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
376(1R,2S)-2-Amino-3-(3,5-differenl)-1-({[2-(ethylthio)ethyl]amino}methyl)propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
378(1R,2S)-2-Amino-3-cyclohexyl-1-{[(3-methoxybenzyl)amino]methyl}propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
380(1R,2S)-2-Amino-1-{[benzyl(cyanomethyl)amino]methyl}-3-(3,5-differenl)propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
382(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(2-hydroxypropyl)amino]methyl}propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
384(1R,2S)-2-Amino-1-{[(3-butoxypropyl)amino]methyl}-3(3,5-differenl)propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
386(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-{[2-(2-hydroxyethyl)piperidine-1-yl]carbonyl}-5-methylbenzoate
388
390(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-(1-hydroxy-2-propylpentyl)benzoate
392(1R,2S)-2-Amino-1-[(benzylamino)methyl]-3-(3-chloro-5-forfinal)propyl-3-(aminocarbonyl)-5-[(dipropylamino)carbonyl]benzoate
394Triptorelin (1R,2S)-2-amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-4-[(methanesulfonyl)amino]butanoate
396(1R,2S)-2-Amino-1-({[3-(1-benzothieno-2-yl)benzyl]amino}methyl)-3-(3,5-differenl)propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
398(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-(benzyl) - Rev. XI)isoxazol-5-carboxylate
400Triptorelin (1R,2S)-2-amino-1-{[(cyclopropylmethyl)amino]methyl}-3-(3,5-differenl)propyl-N-[(benzyloxy)carbonyl]-3-[(1-propinball)sulfonyl]alaninate
402
404(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-5-(1H-pyrazole-1-yl)pentanoate
406(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-1-(2-furylmethyl)-5-oxopyrrolidin-3-carboxylate
408Hydrochloride (1R,2S)-2-amino-1-{[(3-methoxybenzyl)amino]methyl}-3-phenylpropyl-2-ethylhexanoate
410(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(5-hydroxyphenyl)amino]methyl}propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
412(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-methoxybenzyl)amino]methyl}propyl-3-[(dipropylamino)carbonyl]piperidine-1-carboxylate
414(1R,2S)-2-Amino-(3,5-differenl)-1-{[(3-methoxybenzyl)amino]methyl}propyl-3-[(diethylamino)carbonyl]piperidine-1-carboxylate
416(1R,2S)-2-Amino-3-(pentafluorophenyl)-1-({[3-(trifluoromethyl)benzyl]amino}methyl)propyl-3-bromo-5-[(dipropylamino)carbonyl]benzoate
418(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[3-(active compounds)amino]methyl}propyl-4-[(methylsulphonyl)amino]benzoate
420
422(1R,2S)-2-Amino-3-(3-bromophenyl)-1-{[(3-methoxybenzyl)amino]methyl}propyl-3-[(dipropylamino)sulfonyl]propanoic
424(1R,2S)-2-Amino-1-{[(3-methoxybenzyl)amino]methyl}-3-(2-thienyl)propyl-3-[(dipropylamino)sulfonyl]propanoic
426(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[3-(ethoxypropan)amino]methyl}propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
428(1R,2S)-2-Amino-1-[(benzylamino)methyl]-3-(2-thienyl)propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
430
432Hydrochloride (1R,2S)-2-amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-2-hydroxy-4-(phenylsulfonyl)butanoate
434(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[3-(methylbutyl)amino]methyl}propyl-3-(aminocarbonyl)-5-[(dipropylamino)carbonyl]benzoate
436(1R,2S)-2-Amino-1-{[3-(methoxybenzyl)amino]methyl}-3-[3-(triptoreline)phenyl]propyl-3-(aminocarbonyl)-5-[(dipropylamino)carbonyl]benzoate
259N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N'-ethyl-N-(3-active compounds)-N'-isopropyl-5-methylisophthalic
261N-[(2R,3S)-3-Amino-2-hydroxy-4-(2-thienyl)butyl]-N-(3-methoxybenzyl)-5-methyl-N',N'-dipropylacetamide
263N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-3-{[(2-hydroxyethyl)(propyl)amino]sulfonyl}propanamide
265N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-N'-isopropyl-N',5-dimethylacetamide
267 N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-2-[(methylsulphonyl)amino]-1,3-thiazole-4-carboxamide
269N-Allyl-N'-[(2R,3S)-3-amino-4-(3,5-differenl)-2-hydroxybutyl]-N-cyclopentyl-N'-(3-active compounds)-5-methylisophthalic
271
273N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-3-[(3-methylbutyl)sulfonyl]propanamide
275N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-5-methyl-N-[3-(5-methyl-2-thienyl)benzyl]-N',N'-dipropylacetamide
277N1-[(2R,3S)-3-Amino-2-hydroxy-4-(3-methoxyphenyl)butyl]-N1-(3-methoxybenzyl)-N3N3-DIPROPYLENE-1,3,5-tricarboxylic
279N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-5-methyl-N-(1-etylhexyl)-N',N'-dipropylacetamide
281N-[1-(aminocarbonyl)cyclohexyl]-N-[(2R,3S)-3-amino-4-(3,5-differenl)-2-hydroxybutyl]-5-methyl-N',N'-diprop isoftlimit
283N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-[(2E)-Gex-2-EN-1-yl]-5-methyl-N',N'-dipropylacetamide
285N-[(2R,3S)-3-Amino-4-(4-forfinal)-2-hydroxybutyl]-N-(3-methoxybenzyl)-5-methyl-N',N'-dipropylacetamide
287N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-3-hydroxyethoxy-5-carboxamid
289N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-{3-[(1E)-Gex-1-EN-1-yl]benzyl}-5-methyl-N',N'-dipropylacetamide
291N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-N'-isopropyl-5-methylisophthalic
293N1-[(2R,3S)-3-Amino-2-hydroxy-4-(2-thienyl)butyl]-N1-(3-methoxybenzyl)-N3N3-DIPROPYLENE-1,3,5-tricarboxylic
2952-(3-{2-[[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl](3-iodobenzyl)amino]-2-oxoethyl}phenoxy)ndimethylacetamide
297N-[(2R,3S)-3-Amino-4-(3-what Ravenel)-2-hydroxybutyl]-N-(3-methoxybenzyl)-5-methyl-N',N'-dipropylacetamide
299N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(2-ethylhexyl)-5-methyl-N',N'-dipropylacetamide
301N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-[3-(6-methoxypyridine-3-yl)benzyl]-5-methyl-N',N'-dipropylacetamide
303N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-[3-(2,4-dimethoxypyrimidine-5-yl)benzyl]-5-methyl-N',N'-dipropylacetamide
305N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-3-(2-ethylbutanol)benzamid
307N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-3-[(4-hydroxypiperidine-1-yl)carbonyl]-5-methylbenzamide
309N1-[(2R,3S)-3-Amino-4-(3-bromophenyl)-2-hydroxybutyl]-N1-(3-methoxybenzyl)-N3N3-DIPROPYLENE-1,3,5-tricarboxylic
311(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-iodobenzyl)amino]methyl}propyl-4-[2'-(aminocarbonyl)biphenyl-4-yl]-4-oxobutanoate
313
315N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-3-[(3-hydroxypiperidine-1-yl)carbonyl]-5-methylbenzamide
317N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-hydroxy-1-phenylpropyl)-5-methyl-N',N'-dipropylacetamide
319N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N'-[2-(dimethylamino)ethyl]-N'-ethyl-N-(3-active compounds)-5-methylisophthalic
321N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-4-methyl-4H,6N-pyrrolo[1,2-a][4,1]benzoxazepin-4-carboxamid
3232-(5-Acetyl-2-thienyl)-N-[(2R,3S)-3-amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)ndimethylacetamide
325N1-[(2R,3S)-3-Amino-4-(3,5-dichlorophenyl)-2-hydroxybutyl]-N1-(3-methoxybenzyl)-N3N3-DIPROPYLENE-1,3,5-tricarboxylic
327N-[(2R,3S)-3-Amino-4-(3,5-ditto is phenyl)-2-hydroxybutyl]-N-(3-active compounds)-N',N'-aminobutiramida 5-methylisophthalic
329N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-3-[(methylsulphonyl)amino]benzamide
331N1-[(2R,3S)-3-Amino-4-(4-chlorophenyl)-2-hydroxybutyl]-N1-(3-methoxybenzyl)-N3N3-DIPROPYLENE-1,3,5-tricarboxylic
333N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-iodobenzyl)-2-[4-(2-oxopyrrolidin-1-yl)phenyl]ndimethylacetamide
335N-[(2R,3S)-3-Amino-4-(3-chloro-5-forfinal)-2-hydroxybutyl]-3-[(dipropylamino)sulfonyl]-N-(3-methoxybenzyl)propanamide
337N1-[(2R,3S)-3-Amino-4-(3-chloro-5-forfinal)-2-hydroxybutyl]-N1-(3-methylbutyl)-N3N3-DIPROPYLENE-1,3,5-tricarboxylic
339
341Trihydrochloride N-[(2R,3S)-3-amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-3-{[(1-methyl-1H-imidazol-4-yl)sulfonyl]amino}be Sumida
343N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-5-methyl-N-pentyl-N',N'-dipropylacetamide
345N1-[(2R,3S)-3-Amino-4-(4-forfinal)-2-hydroxybutyl]-N1-(3-methoxybenzyl)-N3N3-DIPROPYLENE-1,3,5-tricarboxylic
347N-[(2R,3S)-3-Amino-4-(3-chloro-5-forfinal)-2-hydroxybutyl]-N-benzyl-5-methyl-N',N'-dipropylacetamide
349N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N'-cyclohexyl-N'-ethyl-N-(3-active compounds)-5-methylisophthalic
3512-([(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]{3-[(dipropylamino)carbonyl]-5-methylbenzoyl}amino)ethyl(2,4-differenl)carbamate
353The hydrochloride of N-[(2R,3S)-3-amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-3-{[(2S)-2-(methoxymethyl)pyrrolidin-1-yl]carbonyl}-5-methylbenzamide
355N1-[(2R,3S)-3-Amino-4-(3-fluoro-4-were)-2-hydroxybutyl]-N1-(3-label benzyl)-N 3N3-DIPROPYLENE-1,3,5-tricarboxylic
357N1-[(2R,3S)-3-Amino-4-(3-bromophenyl)-2-hydroxybutyl]-N1-(3-methylbutyl)-N3N3-DIPROPYLENE-1,3,5-tricarboxylic
359N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-2,8-dimethylindoline-3-carboxamide
361N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(6-hydroxyhexyl)-5-methyl-N',N'-dipropylacetamide
363N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-[(2R)-2-hydroxypropyl]-5-methyl-N',N'-dipropylacetamide
365N-[(2R,3S)-3-Amino-2-hydroxy-4-phenylbutyl]-N-(3-methoxybenzyl)-3-[(1-propinball)sulfonyl]propanamide
367N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-3-{[(2-hydroxy-1,1-dimethylethyl)amino]sulfonyl}benzamide
369N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-5-methyl-N-(4-phenylbutyl)-N',N'-dipropylacetamide
371N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-7-(1H-imidazol-1-yl)-N-(3-iodobenzyl)-5,6-dihydronaphthalene-2-carboxamide
373(3-Acetylamino)-N-[(2R,3S)-3-amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-4-methylbenzamide
375N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-[2-(aminosulfonyl)ethyl]-5-methyl-N',N'-dipropylacetamide
377N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-[2-(ethylthio)ethyl]-5-methyl-N',N'-dipropylacetamide
379N-[(2R,3S)-3-Amino-4-cyclohexyl-2-hydroxybutyl]-N-(3-methoxybenzyl)-5-methyl-N',N'-dipropylacetamide
381
383N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(2-hydroxypropyl)-5-methyl-N',N'-dipropylacetamide
385N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(-butoxypropyl)-5-methyl-N',N'-dipropylacetamide
387N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-3-{[2-(2-hydroxyethyl)piperidine-1-yl]carbonyl}-5-methylbenzamide
389Methyl-N-[(2R,3S)-3-amino-4-(3,5-differenl)-2-hydroxybutyl]-N-{3-[(dipropylamino)carbonyl}-5-methylbenzoyl}-β-alaninate
391N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-3-(1-hydroxy-2-propylpentyl)benzamid
393N1-[(2R,3S)-3-Amino-4-(3-chloro-5-forfinal)-2-hydroxybutyl]-N1-benzyl-N3N3-DIPROPYLENE-1,3,5-tricarboxylic
395Triptorelin (g) N-[(2R,3S)-3-amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-4-[(methylsulphonyl)amino]butanamide
397N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-[3-(1-benzothieno-2-yl)benzyl]-5-methyl-N',N'-dipropylacetamide
399N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-3-(benzyloxy)-N-(3-active compounds)isoxazol-5-carboxamid
401
4031-(3-{[[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl](3-active compounds)amino]carbonyl}-5-methylbenzoyl)-D-prolinamide
405N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-5-(1H-pyrazole-1-yl)pentanone
407N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-1-(2-furylmethyl)-5-oxopyrrolidin-3-carboxamide
409The hydrochloride of N-[(2R,3S)-3-amino-2-hydroxy-4-phenylbutyl]-2-ethyl-N-(3-methoxybenzyl)hexanamide
411N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(5-hydroxyphenyl)-5-methyl-N',N'-dipropylacetamide
413N1-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N1-(3-methoxybenzyl)-N3N3-dipropyltryptamine-1,3-dicarboxamide
415N1-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N3N3diet the l-N 1-(3-methoxybenzyl)piperidine-1,3-dicarboxamide
417N-[(2R,3S)-3-Amino-2-hydroxy-4-(pentafluorophenyl)butyl]-5-bromo-N',N'-dipropyl-N-[3-(trifluoromethyl)benzyl]isophthalamide
419N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-4-[(methylsulphonyl)amino]benzamide
421
423N-[(2R,3S)-3-Amino-4-(3-bromophenyl)-2-hydroxybutyl]-3-[(dipropylamino)sulfonyl]-N-(3-methoxybenzyl)propanamide
425N-[(2R,3S)-3-Amino-2-hydroxy-4-(2-thienyl)butyl]-3-[(dipropylamino)sulfonyl]-N-(3-methoxybenzyl)propanamide
427N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-ethoxypropan)-5-methyl-N',N'-dipropylacetamide
429N-[(2R,3S)-3-Amino-2-hydroxy-4-(2-thienyl)butyl]-N-benzyl-5-methyl-N',N'-dipropylacetamide
431
433The hydrochloride of N-[(2R,3S)-3-amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-2-hydroxy-4-(phenylsulfonyl)butanamide
435N1-[(2R,3S)-3-Amino-4-(3,5-dichlorophenyl)-2-hydroxybutyl]-N1-(3-methylbutyl)-N3N3-DIPROPYLENE-1,3,5-tricarboxylic
437N1-{(2R,3S)-3-Amino-2-hydroxy-4-[3-(triptoreline)phenyl]butyl}-N1-(3-methoxybenzyl)-N3N3-DIPROPYLENE-1,3,5-tricarboxylic
438(1R,2S)-2-Amino-3-(3,5-dichlorophenyl)-1-{[(3,3-dimethylbutyl)amino]methyl}propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
440(1R,2S)-2-Amino-1-[(benzylamino)methyl]-3-(3-bromophenyl)propyl-3-(aminocarbonyl)-5-[(dipropylamino)carbonyl]benzoate
442(1R,2S)-2-Amino-3-(3-chloro-5-forfinal)-1-{[(3-methylbutyl)amino]methyl}propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
444
446(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-diphenylpropyl)amino]methyl}propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
448(1R,2S)-2-Amino-3-(3,5-differenl)-1-({[(1S)-1-hydroxymethyl)propyl]amino}methyl)propyl-3-[(dipropylamino)carbonyl]benzoate
450(1R,2S)-2-Amino-3-(3,5-differenl)-1-({[(3S)-2-oxazepan-3-yl]amino}methyl)propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
452(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino}methyl)propyl-5-(cyclohexylamino)-5-oxopentanoate
454(1R,2S)-2-Amino-1-{[(3-methoxybenzyl)amino]methyl}-3-(3-were)propyl-3-(aminocarbonyl)-5-[(dipropylamino)carbonyl]benzoate
456Triptorelin (1R,2S)-2-amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-N-[(2-propylpentyl)sulfonyl]-β-alaninate
458The dihydrochloride of (1R,2S)-2-amino-3-(3,5-differenl)-1-{[(3-active compounds)amino}methyl)about the Il-3-(1,3-thiazol-2-yl)benzoate
460(1R,2S)-2-Amino-3-(2-furyl)-1-{[(3-methoxybenzyl)amino]methyl}propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
462(1R,2S)-2-Amino-3-(3,5-differenl)-1-[({3-[methyl(phenyl)amino]propyl}amino)methyl]propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
464(1R,2S)-2-Amino-1-{[(3-methoxybenzyl)amino]methyl}-3-(4-were)propyl-3-(aminocarbonyl)-5-[(dipropylamino)carbonyl]benzoate
466(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-5-oxo-1-(2-thienylmethyl)pyrrolidin-3-carboxylate
468(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-4-[(butylthio)methyl]-5-methyl-2-furoate
470(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-{[(2-hydroxyethyl)amino]sulfonyl}benzoate
472(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-N-[3-(trifluoromethyl)benzoyl]glycine is t
474(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-methylcyclohexyl)amino]methyl}propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
476(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-4-(2-oxo-1,3-oxazolidin-3-yl)benzoate
478(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-4-(1H-pyrrol-1-yl)benzoate
480(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(6-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl)amino]methyl}propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
482(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-1,3,4,5-tetrahydropyrido[4,3-b]indole-8-carboxylate
484(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-4-oxo-4-{[2-(trifluoromethyl)phenyl]amino}of butanoate
486(1R,2S)-2-Amino-3-(3-bromophenyl)-1-{[(3-methylbutyl)amino]methyl}propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
488 (1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-4,5-dimethyl-2-(1H-pyrrol-1-yl)thiophene-3-carboxylate
490(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(2,3-dihydroxypropyl)amino]methyl}propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
492(1R,2S)-2-Amino-3-(3,5-differenl)-1-({[(2S)-2-hydroxypropyl]amino}methyl)propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
494(1R,2S)-2-Amino-3-(3,5-differenl)-1-({[(1R)-1-methylpropyl]amino}methyl)propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
496(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-2-chloro-4-(methylsulphonyl)benzoate
498(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(2-hydroxyethyl)amino]methyl}propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
500(1R,2S)-2-Amino-1-{[(3-methoxybenzyl)amino]methyl}-3-(3-methoxyphenyl)propyl-3-[(dipropylamino)sulfonyl]propanoic
502Hydrochloride (1R,2S)-2-amino-3-(3,5-differenl)-1-{[(3-e is ylbenzyl)amino]methyl}propyl-3-{methyl[(trifluoromethyl)sulfonyl]amino}benzoate
504(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-hydroxy-6-(1-hydroxy-2,2-dimethylpropyl)pyridine-2-carboxylate
506(1R,2S)-2-Amino-1-{[(1,3-dicyclohexylphosphino)amino]methyl}-3-(3,5-differenl)propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
508(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-2,2'-Bethoven-5-carboxylate
510(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-4-(1H-imidazol-1-yl)butanoate
512(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-2,3-dihydroxy-4-[(4-methoxyphenyl)amino]-4-oxobutanoate
514(1R,2S)-2-Amino-1-[(benzylamino)methyl]-3-(4-hydroxyphenyl)propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
516(1R,2S)-2-Amino-1-{[(3-methoxybenzyl)amino]methyl}-3-[3-(trifluoromethyl)phenyl]propyl-3-(aminocarbonyl)-5-[(dipropylamino)carbonyl]benzoate
518
520(1R,2S)-2-Amino-1-({[2-(aminocarbonyl)-1H-indol-6-yl]amino}methyl)-3-(3,5-differenl)propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
522(1R,2S)-2-Amino-1-[(benzylamino)methyl]-3-(3-bromophenyl)propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
524(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-N-[4-(trifluoromethyl)benzoyl]glycinate
526(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-2-(1-oxo-1,3-dihydro-2H-isoindole-2-yl)butanoate
528(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-N-(3,4-dichlobenil)glycinate
530(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-chloro-4-(methylsulphonyl)thiophene-2-carboxylate
532(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(1-ethylpropyl)amino]methyl}propyl-3-[(dipropyl is Ino)carbonyl]-5-methylbenzoate
534(1R,2S)-2-Amino-3-(3,5-differenl)-1-[({[(5R)-3-ethyl-2-oxo-1,3-oxazolidin-5-yl]methyl}amino)methyl]propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
536(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-5-methyl-7-(trifluoromethyl)pyrazolo[1,5-a]pyrimidine-2-carboxylate
538Hydrochloride (1R,2S)-2-amino-1-{[(3-methoxybenzyl)amino]methyl}-3-phenylpropyl-N-[(methylthio)acetyl]-3-[(1-propinball)sulfonyl]alaninate
540(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(2,3-dimethylcyclohexyl)amino]methyl}propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
542(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-4,5-dimethoxy-1-benzothiophen-2-carboxylate
544(1R,2S)-2-Amino-3-[(3-fluoro-5-(trifluoromethyl)phenyl]-1-{[(3-methylbutyl)amino]methyl}propyl-3-(aminocarbonyl)-5-[(dipropylamino)carbonyl]benzoate
546(1R,2S)-2-Amino-3-(3,5-differenl)-1-[({[(5S)-3-ethyl-2-oxo-1,3-oxazolidin-5-yl]methyl}is Mino)methyl]propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
548(1R,2S)-2-Amino-3-(1,3-benzodioxol-5-yl)-1-{[(3-methoxybenzyl)amino]methyl}propyl-3-(aminocarbonyl)-5-[(dipropylamino)carbonyl]benzoate
550(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-4-(3,5-dioxo-1,2,4-triazolin-4-yl)benzoate
552Hydrochloride (1R,2S)-2-amino-1-{[(3-methoxybenzyl)amino]methyl}-3-phenylpropyl-2-hydroxy-3-[(3-methoxyphenyl)sulfonyl]propanoate
554
556(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(2-methylcyclohexyl)amino]methyl}propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
558(1R,2S)-2-Amino-1-{[(2-{4-[(3-Chlorobenzyl)oxy]phenyl}ethyl)amino]IU-Tyl}-3-(3,5-differenl)propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
560(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]ethyl}propyl-2-hydroxy-4-oxo-(3-thienyl)butanoic
562(1R,2S)-2-Amino-3-[3-(benzyloxy)-5-forfinal]-1-{[(3-methoxybenzyl)amino]methyl}propyl-3-(aminocarbonyl)-5-[(dipropylamino)carbonyl]benzoate
564(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-2-hydroxy-4-oxo-4-[3-(trifluoromethyl)phenyl]butanoate
566(1R,2S)-2-Amino-1-{[(3-methylbutyl)amino]methyl}-3-[3-(triptoreline)phenyl]propyl-3-(aminocarbonyl)-5-[(dipropylamino)carbonyl]benzoate
568(1R,2S)-2-Amino-3-(3,5-differenl)-1-({[1-(hydroxymethyl)-3-(methylthio)propyl]amino}methyl)propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
570(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-2-(1H-1,2,3-benzotriazol-1-yl)hexanoate
572(1R,2S)-2-Amino-3-(3-fluoro-4-were)-1-{[(3-methylbutyl)amino]methyl}propyl-3-(aminocarbonyl)-5-[(dipropylamino)carbonyl]benzoate
574(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-(4,4-dimethyl-2,5-dioxime solidin-1-yl)2-{[(1-propinball)sulfonyl]methyl}propanoic
576Triptorelin (1R,2S)-2-amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-4-{[(trifluoromethyl)sulfonyl]amino}butanoate
578(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl(5-methyl-1,3-dioxo-1,3-dihydro-2H-isoindole-2-yl)acetate
580(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-hydroxypropyl)amino]methyl}propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
582(1R,2S)-2-Amino-3-(3,5-differenl)-1-({[1-(hydroxymethyl)propyl]amino}methyl)propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
584(1R,2S)-2-Amino-1-[(benzylamino)methyl]-3-(3,5-dichlorophenyl)propyl-3-(aminocarbonyl)-5-[(dipropylamino)carbonyl]benzoate
586Hydrochloride (1R,2S)-2-amino-1-{[(3-methoxybenzyl)amino]methyl}-3-phenylpropyl-3-{[(2-hydroxyethyl)(propyl)amino]sulfonyl}of propanoate
588(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-5-(benzylthio)nicotinate
590(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-1H-pyrazole-5-carboxylate
592(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-6-chloro-3-methyl-2-oxo-2,3-dihydro-1,3-benzoxazol-5-carboxylate
594(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-1H-benzimidazole-2-carboxylate
596(1R,2S)-2-Amino-3-cyclohexyl-1-{[(3-methoxybenzyl)amino]methyl}propyl-3-(aminocarbonyl)-5-[(dipropylamino)carbonyl]benzoate
598(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-6-hydroxy-4,7-dimethoxy-1-benzofuran-5-carboxylate
600(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(4-methylcyclohexyl)amino]methyl}propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
602(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl[1,2,4]triazolo[4,3-a]pyridine-6-carboxylate
604(1R,2S)-2-Amino-3(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-2-hydroxy-4-oxo-4-(2-thienyl)butanoic
606(1R,2S)-2-Amino-1-[(benzylamino)methyl]-3-(3,5-differenl)propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
608(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-4-(2-hydroxy-5-were)-4-oxobutanoate
610(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-phenoxybenzoic
612(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-4-[(aminocarbonyl)amino]benzoate
614(1R,2S)-2-Amino-3-(3,5-differenl)-1-({[(1S)-1-(hydroxymethyl)-3-(methylthio)propyl]amino}methyl)propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
616(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-7-hydroxy-4-exogamy-2-carboxylate
618(1R,2S)-2-Amino-3-(3,5-differenl)-1-({[(1S)-1-(hydroxymethyl)-3-methylbutyl]amino}methyl)propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
620622(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(1-methyl-3-phenylpropyl)amino]methyl}propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
439N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3,3-dimethylbutyl)-5-methyl-N',N'-dipropylacetamide
441N1-[(2R,3S)-3-Amino-4-(3-bromophenyl)-2-hydroxybutyl]-N1-benzyl-N3N3-DIPROPYLENE-1,3,5-tricarboxylic
443N-[(2R,3S)-3-Amino-4-(3-chloro-5-forfinal)-2-hydroxybutyl]-5-methyl-N-(3-methylbutyl)-N',N'-dipropylacetamide
445
447N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(1,3-diphenylpropyl)-5-methyl-N',N'-dipropylacetamide
449 N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-[(1S)-1-(hydroxymethyl)propyl]-N',N'-dipropylacetamide
451N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-5-methyl-N-[(3S)-2-oxazepan-3-yl]-N',N'-dipropylacetamide
453N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N'-cyclohexyl-N-(3-active compounds)pentanedione
455N1-[(2R,3S)-3-Amino-2-hydroxy-4-(3-were)butyl]-N1-(3-methoxybenzyl)-N3N3-DIPROPYLENE-1,3,5-tricarboxylic
457Triptorelin (Sol) N1-[(2R,3S)-3-amino-4-(3,5-differenl)-2-hydroxybutyl]-N1-(3-active compounds)-N3-[(2-propylpentyl)sulfonyl]-β-alaninemia
459The dihydrochloride of N-[(2R,3S)-3-amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-3-(1,3-thiazol-2-yl)benzamide
461N-[(2R,3S)-3-Amino-4-(2-furyl)-2-hydroxybutyl]-N-(3-methoxybenzyl)-5-methyl-N',N'-dipropylacetamide
463N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroc libutil]-5-methyl-N-{3-[methyl(phenyl)amino]propyl}-N',N'-dipropylacetamide
465N1-[(2R,3S)-3-Amino-2-hydroxy-4-(4-were)butyl]-N1-(3-methoxybenzyl)-N3N3-DIPROPYLENE-1,3,5-tricarboxylic
467N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-5-oxo-1-(2-thienylmethyl)pyrrolidin-3-carboxamide
469N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-4-[(butylthio)methyl]-N-(3-active compounds)-5-methyl-2-furamide
471N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-3-{[(2-hydroxyethyl)amino]sulfonyl}benzamide
473
475N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-5-methyl-N-(3-methylcyclohexyl)-N',N'-dipropylacetamide
477N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-4-(2-oxo-1,3-oxazolidin-3-yl)benzamid
479 N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-4-(1H-pyrrol-1-yl)benzamid
481N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(6-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl)-5-methyl-N',N'-dipropylacetamide
483N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-1,3,4,5-tetrahydropyrido[4,3-b]indol-8-carboxamide
485N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-N'-[2-(trifluoromethyl)phenyl]succinamic
487N-[(2R,3S)-3-Amino-4-(3-bromophenyl)-2-hydroxybutyl]-5-methyl-N-(3-methylbutyl)-N',N'-dipropylacetamide
489N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-4,5-dimethyl-2-(1H-pyrrol-1-yl)thiophene-3-carboxamide
491N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(2,3-dihydroxypropyl)-5-methyl-N',N'-dipropylacetamide
493N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-[(2S)-2-hydroxypropyl]-5-methyl-N',N'-dipropyl softlimit
495N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-5-methyl-N-[(1R)-1-methylpropyl]-N',N'-dipropylacetamide
497N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-2-chloro-N-(3-active compounds)-4-(methylsulphonyl)benzamid
499N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(2-hydroxyethyl)-5-methyl-N',N'-dipropylacetamide
501N-[(2R,3S)-3-Amino-2-hydroxy-4-(3-methoxyphenyl)butyl]-3-[(dipropylamino)sulfonyl]-N-(3-methoxybenzyl)propanamide
503The hydrochloride of N-[(2R,3S)-3-amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-3-{methyl[(trifluoromethyl)sulfonyl]amino}benzamide
505N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-3-hydroxy-6-(1-hydroxy-2,2-dimethylpropyl)pyridine-2-carboxamide
507N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(1,3-dicyclohexylphosphino)-5-methyl-N',N'-dipropylacetamide
509 N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-2,2'-Bethoven-5-carboxamid
511N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-4-(1H-imidazol-1-yl)butanamide
513N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-2,3-dihydroxy-N'-(4-methoxyphenyl)succinamic
515N-[(2R,3S)-3-Amino-2-hydroxy-4-(4-hydroxyphenyl)butyl]-N-benzyl-5-methyl-N',N'-dipropylacetamide
517N1-{(2R,3S)-3-Amino-2-hydroxy-4-[3-(trifluoromethyl)phenyl]butyl}-N1-(3-methoxybenzyl)-N3N3-DIPROPYLENE-1,3,5-tricarboxylic
519N1-[(2R,3S)-3-Amino-2-hydroxy-4-(2-thienyl)butyl]-N1-benzyl-N3N3-DIPROPYLENE-1,3,5-tricarboxylic
521N-[2-(Aminocarbonyl)-1H-indol-6-yl]-N-[(2R,3S)-3-amino-4-(3,5-differenl)-2-hydroxybutyl]-5-methyl-N',N'-dipropylacetamide
523N-[(2R,3S)-3-Amino-4-(3-bromophenyl)-2-hydroxybutyl]-N-benzyl-5-methyl-N',N dipropylacetamide
525
527N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-2-(1-oxo-1,3-dihydro-2H-isoindole-2-yl)butanamide
529
531N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-3-chloro-N-(3-active compounds)-4-(methylsulphonyl)thiophene-2-carboxamide
533N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(1-ethylpropyl)-5-methyl-N',N'-dipropylacetamide
535N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-{[(5R)-3-ethyl-2-oxo-1,3-oxazolidin-5-yl]methyl}-5-methyl-N',N'-dipropylacetamide
537N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-5-methyl-7-(trifluoromethyl)pyrazolo[1,5-a]pyrimidine-2-carboxamide
539Hydroch Oric N 1-[(2R,3S)-3-amino-2-hydroxy-4-phenylbutyl]-N1-(3-methoxybenzyl)-N2-[(methylthio)acetyl]-3-[(1-propinball)sulfonyl]alaninemia
541N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(2,3-dimethylcyclohexyl)-5-methyl-N',N'-dipropylacetamide
543N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-4,5-dimethoxy-1-benzothiophen-2-carboxamide
545N1-{(2R,3S)-3-Amino-4-[3-fluoro-5-(trifluoromethyl)phenyl]-2-hydroxybutyl}-N1-(3-methylbutyl)-N3N3-DIPROPYLENE-1,3,5-tricarboxylic
547N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-{[(5S)-3-ethyl-2-oxo-1,3-oxazolidin-5-yl]-5-methyl-N',N'-dipropylacetamide
549N1-[(2R,3S)-3-Amino-4-(1,3-benzodioxol-5-yl)-2-hydroxybutyl]-N1-(3-methoxybenzyl)-N3N3-DIPROPYLENE-1,3,5-tricarboxylic
551N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-4-(3,5-dioxo-1,2,4-triazolin-4-yl)-N-(3-active compounds)benzamid
553 The hydrochloride of N-[(2R,3S)-3-amino-2-hydroxy-4-phenylbutyl]-2-hydroxy-N-(3-methoxybenzyl)-3-[(3-methoxyphenyl)sulfonyl]propanamide
555
557N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-5-methyl-N-(2-methylcyclohexyl)-N',N'-dipropylacetamide
559N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(2-{4-[(3-Chlorobenzyl)oxy]phenyl}ethyl)-5-methyl-N',N'-dipropylacetamide
561N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-2-hydroxy-4-oxo-4-(3-thienyl)butanamide
563N1-{(2R,3S)-3-Amino-4-[3-(benzyloxy)-5-forfinal]-2-hydroxybutyl}-N1-(3-methoxybenzyl)-N3N3-DIPROPYLENE-1,3,5-tricarboxylic
565N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-2-hydroxy-4-oxo-4-[3-(trifluoromethyl)phenyl]butanamide
567N1-{(2R,3S)-3-Am is but-2-hydroxy-4-[3-(triptoreline)phenyl]butyl}-N 1-(3-methylbutyl)-N3N3-DIPROPYLENE-1,3,5-tricarboxylic
569N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-[1-(hydroxymethyl)-3-(methylthio)propyl]-5-methyl-N',N'-dipropylacetamide
571N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-2-(1H-1,2,3-benzotriazol-1-yl)-N-(3-active compounds)hexanamide
573N1-[(2R,3S)-3-Amino-4-(3-fluoro-4-were)-2-hydroxybutyl]-N1-(3-methylbutyl)-N3N3-DIPROPYLENE-1,3,5-tricarboxylic
575N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-3-(4,4-dimethyl-2,5-dioxoimidazolidin-1-yl)-N-(3-active compounds)-2-{[(1-propinball)sulfonyl]methyl}propanamide
577Triptorelin (g) N-[(2R,3S)-3-amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-4-{[(trifluoromethyl)sulfonyl]amino}butanamide
579N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-2-(5-methyl-1,3-dioxo-1,3-dihydro-2H-isoindole-2-yl)ndimethylacetamide
581 N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-hydroxypropyl)-5-methyl-N',N'-dipropylacetamide
583N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-[1-(hydroxymethyl)propyl]-5-methyl-N',N'-dipropylacetamide
585N1-[(2R,3S)-3-Amino-4-(3,5-dichlorophenyl)-2-hydroxybutyl]-N1-benzyl-N3N3-DIPROPYLENE-1,3,5-tricarboxylic
587The hydrochloride of N-[(2R,3S)-3-amino-2-hydroxy-4-phenylbutyl]-3-{[(2-hydroxyethyl)(propyl)amino]sulfonyl}-N-(3-methoxybenzyl)propanamide
589N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-5-(benzylthio)-N-(3-active compounds)nicotinamide
591N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-1H-pyrazole-5-carboxamide
593N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-6-chloro-N-(3-active compounds)-3-methyl-2-oxo-2,3-dihydro-1,3-benzoxazol-5-carboxamid
595N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-ative the ZIL)-1H-benzimidazol-2-carboxamide
597N1-[(2R,3S)-3-Amino-4-cyclohexyl-2-hydroxybutyl]-N1-(3-methoxybenzyl)-N3N3-DIPROPYLENE-1,3,5-tricarboxylic
599N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-6-hydroxy-4,7-dimethoxy-1-benzofuran-5-carboxamide
601N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-5-methyl-N-(4-methylcyclohexyl)-N',N'-dipropylacetamide
603N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)[1,2,4]triazolo[4,3-a]pyridine-6-carboxamide
605N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-2-hydroxy-4-oxo-4-(2-thienyl)butanamide
607N-[(2R,3S)-3-Amino-4-(3,5-dichlorophenyl)-2-hydroxybutyl]-N-benzyl-5-methyl-N',N'-dipropylacetamide
609N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-4-(2-hydroxy-5-were)-4-oxobutanamide
611 N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-3-phenoxybenzamide
6134-[(Aminocarbonyl)amino]-N-[(2R,3S)-3-amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)benzamid
615N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-[(1S)-1-(hydroxymethyl)-3-(methylthio)propyl]-5-methyl-N',N'-dipropylacetamide
617N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-7-hydroxy-4-exogamy-2-carboxamide
619N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-[(1S)-1-(hydroxymethyl)-3-methylbutyl]-5-methyl-N',N'-dipropylacetamide
621N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-[(1R)-1-(hydroxymethyl)propyl]-N',N'-dipropylacetamide
623N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-5-methyl-N-(1-methyl-3-phenylpropyl)-N',N'-dipropylacetamide
624(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-2-(2,3-dihydro-1-benzofuran-5-is)-1,3-thiazole-4-carboxylate
626(1R,2S)-2-Amino-3-[(3-benzyloxy)phenyl]-1-{[(3-methoxybenzyl)amino]methyl}propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
628(1R,2S)-2-Amino-3-(4-chlorophenyl)-1-{[(3-methoxybenzyl)amino]methyl}propyl-3-[(dipropylamino)sulfonyl]propanoic
630(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-oxo-3-(pentylamine)propanoate
632(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-(triptoreline)benzoate
634(1R,2S)-2-Amino-3-(3-fluoro-4-were)-1-{[(3-methoxybenzyl)amino]methyl}propyl-3-[(dipropylamino)sulfonyl]propanoic
636(1R,2S)-2-Amino-3-(3-chloro-5-forfinal)-1-{[(3-methylbutyl)amino]methyl}propyl-3-[(dipropylamino)sulfonyl]propanoic
638(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-(4,4-dimethyl-2,5-dioxoimidazolidin-1-yl)-2-{[(1-propinball)sulfonyl]methyl}propanoic
640 (1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-4-{[4-(acetylamino)phenyl]amino}-4-oxobutanoate
642(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-(1-cyanoethyl)benzoate
644(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-4-oxo-4-[(5-phenyl)-1,3,4-thiadiazole-2-yl)amino]butanoate
646(1R,2S)-2-Amino-1-[(benzylamino)methyl]-3-[3-(triptoreline)phenyl]propyl-3-(aminocarbonyl)-5-[(dipropylamino)carbonyl]benzoate
648(1R,2S)-2-Amino-3-(3,5-differenl)-1-({[2-(2-oxo-2-pyrrolidin-1 ylethoxy)phenyl]amino}methyl)propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
650(1R,2S)-2-Amino-3-(4-chlorophenyl)-1-{[(3-methylbutyl)amino]methyl}propyl-3-(aminocarbonyl)-5-[(dipropylamino)carbonyl]benzoate
652(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl(1,1-dissidocerida-2-thienyl)acetate
654(1R,2S)-2-Amino-1-[(benzylamino)methyl]--(4-chlorophenyl)propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
656(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-5-Gex-1-in-1-incomenet
658(1R,2S)-2-Amino-3-(3-bromophenyl)-1-{[(3-methylbutyl)amino]methyl}propyl-3-[(dipropylamino)sulfonyl]propanoic
660(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-methoxyethoxy-5-carboxylate
662(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-2,3-dimethyl-1H-indole-7-carboxylate
664(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-4-(3-chlorophenyl)-2-hydroxy-4-oxobutanoate
666(1R,2S)-2-Amino-3-(3-fluoro-4-methoxyphenyl)-1-{[(3-methoxybenzyl)amino]methyl}propyl-3-(aminocarbonyl)-5-[(dipropylamino)carbonyl]benzoate
668(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl(1-methyl-1H-indol-3-yl)(oxo)acetate
670(1R,2S)-2-Amino-3-(3-fluoro-4-Mei is phenyl)-1-{[(3-methylbutyl)amino]methyl}propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
672(1R,2S)-2-Amino-1-{[(3-methoxybenzyl)amino]methyl}-3-(4-were)propyl-3-[(dipropylamino)sulfonyl]propanoic
674(1R,2S)-2-Amino-1-[(benzylamino)methyl]-3-(3-fluoro-4-were)propyl-3-(aminocarbonyl)-5-[(dipropylamino)carbonyl]benzoate
676(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl[5-(4-were)-2H-tetrazol-2-yl]acetate
678(1R,2S)-2-Amino-3-(3,5-dichlorophenyl)-1-{[(3-methoxybenzyl)amino]methyl}propyl-3-[(dipropylamino)sulfonyl]propanoic
680(1R,2S)-2-Amino-1-{[(3-methylbutyl)amino]methyl}-3-(2-thienyl)propyl-3-(aminocarbonyl)-5-[(dipropylamino)carbonyl]benzoate
682(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-5-methyl-3-phenylisoxazol-4-carboxylate
684(1R,2S)-2-Amino-1-[(benzylamino)methyl]-3-(4-forfinal)propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
686(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-N-[(methylsulphonyl)acetyl]-N-interglacial
688(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-N-(4-methoxybenzoyl)glycinate
690(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-N-(2,6-differentail)glycinate
692(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-4-(1H-indol-3-yl)-4-oxobutanoate
694(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-4-[(5-benzyl-1,3,4-thiadiazole-2-yl)amino]-4-oxobutanoate
696(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-4-(3-fluoro-4-methoxyphenyl)-4-oxobutanoate
698Ethyl-4-{[(2R,3S)-3-amino-4-(3,5-differenl)-2-({3-[(dipropylamino)carbonyl]-5-methylbenzoyl}oxy)butyl]amino}piperidine-1-carboxylate
700(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-4-(2-perbenzoic)-1H-pyrrole-2-carboxylate
702(1R,2S)-2-Amino--[(benzylamino)methyl]-3-(4-chlorophenyl)propyl-3-(aminocarbonyl)-5-[(dipropylamino)carbonyl]benzoate
704(1R,2S)-2-Amino-1-{[(3-methylbutyl)amino]methyl}-3-[3-(trifluoromethyl)phenyl]propyl-3-(aminocarbonyl)-5-[(dipropylamino)carbonyl]benzoate
706(1R,2S)-2-Amino-3-(4-hydroxyphenyl)-1-{[(3-methylbutyl)amino]methyl}propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
708(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl(4-morpholine-4-ylphenyl)acetate
710(1R,2S)-2-Amino-1-{[(3-methoxybenzyl)amino]methyl}-3-[3-(triptoreline)phenyl]propyl-3-[(dipropylamino)sulfonyl]propanoic
712(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-4-[benzyl(1-cyclopropylethyl)amino]-4-oxobutanoate
714(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-methoxybenzyl)amino]methyl}propyl-3-(2,5-dimethylbenzoyl)-5-methylbenzoate
716(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-4-[(2-methoxy-5-were)amino]-4-oxobutanoate
718 (1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl(3-hydroxyphenyl)acetate
720(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-methoxybenzyl)amino]methyl}propyl-3-[hydroxy(2-were)methyl]-5-methylbenzoate
722(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-5-(ethylthio)nicotinate
724(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-4-[4-(2-furoyl)piperazine-1-yl]-4-oxobutanoate
726(1R,2S)-2-Amino-1-[(benzylamino)methyl]-3-(3-fluoro-4-were)propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
728(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-occaisonaly-1-carboxylate
730(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-(ethylthio)benzoate
732(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propertiee[2,3-b]quinoline-2-carboxylate
734
736(1R,2S)-2-Amino-1-[(benzylamino)methyl]-3-(4-forfinal)propyl-3-(aminocarbonyl)-5-[(dipropylamino)carbonyl]benzoate
738(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-2-[2-furoyl(methyl)amino]benzoate
740(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-2-hydroxy-4-(3-methoxyphenyl)-4-oxobutanoate
742(1R,2S)-2-Amino-1-[(cyclohexylamino)methyl]-3-(3,5-differenl)propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
744(1R,2S)-2-Amino-1-{[(3-methylbutyl)amino]methyl}-3-(4-were)propyl-3-(aminocarbonyl)-5-[(dipropylamino)carbonyl]benzoate
746Hydrochloride (1R,2S)-2-amino-3-(3-fluoro-5-hydroxyphenyl)-1-{[(3-methoxybenzyl)amino]methyl}propyl-3-[(dipropylamino)sulfonyl]propanoate
748(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-ativans the l)amino]methyl}propyl-5-hydroxy-1H-indole-2-carboxylate
750(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-2,2-DIMETHYLPROPANE-8-carboxylate
7524-Oxide, (1R,2S)-2-amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-6-benzylpyridine-2-carboxylate
754(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-methoxybenzyl)amino]methyl}propyl{2-[(dipropylamino)sulfonyl]ethyl}carbamate
756(1R,2S)-2-Amino-3-(3,5-differenl)-1-({[1-(hydroxymethyl)-2-methylpropyl]amino}methyl)propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
758(1R,2S)-2-Amino-1-[(benzylamino)methyl]-3-(3-chloro-5-forfinal)propyl-3-[(dipropylamino)sulfonyl]propanoic
760(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-4-(4-methoxyphenyl)-4-oxobutanoate
762(1R,2S)-2-Amino-1-[(benzylamino)methyl]-3-(4-hydroxyphenyl)propyl-3-(aminocarbonyl)-5-[(dipropylamino)carbonyl]benzoate
764 (1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-methyl-4-oxo-3,4-dihydrophenazine-1-carboxylate
766(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3,4-dihydro-2H-1,5-benzodioxepin-7-carboxylate
768(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl[4-(2,5-dioxopiperidin-1-yl)phenoxy]acetate
770(1R,2S)-2-Amino-3-(2-furyl)-1-{[(3-methoxybenzyl)amino]methyl}propyl-3-(aminocarbonyl)-5-[(dipropylamino)carbonyl]benzoate
772(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-5-methyl-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidine-6-carboxylate
774(1R,2S)-2-Amino-3-(1,3-benzodioxol-5-yl)-1-{[(3-methylbutyl)amino]methyl}propyl-3-(aminocarbonyl)-5-[(dipropylamino)carbonyl]benzoate
776
778(1R,2S)-2-Amino-3(3-chloro-5-forfinal)-1-{[(3-methoxybenzyl)amino]methyl}propyl-5-(dipropylamino)-5-oxopentanoate
780(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-6-fluoro-2-hydroxyquinolin-4-carboxylate
782(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-4-oxo-4-(2-thienyl)butanoic
784
786(1R,2S)-2-Amino-1-{[(3-methoxybenzyl)amino]methyl}-3-(phenylthio)propyl-3-(aminocarbonyl)-5-[(dipropylamino)carbonyl]benzoate
788(1R,2S)-2-Amino-3-(3,5-differenl)-1-({[(1R)-1-(hydroxymethyl)-2-methylpropyl]amino}methyl)propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
790(1R,2S)-2-Amino-3-(3,5-differenl)-1-({[(1R,2S)-1-(hydroxymethyl)-2-methylbutyl]amino}methyl)propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
792(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-2-(proximate the l)benzoate
794(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-5-[(2,4-differenl)amino]-5-oxopentanoate
796(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-5-[(4,6-dimethylpyrimidin-2-yl)amino]-5-oxopentanoate
798(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-methoxybenzyl)amino]methyl}propyl-3-(3-methoxybenzoyl)-5-methylbenzoate
800(1R,2S)-2-Amino-3-[3-(benzyloxy)phenyl]-1-{[(3-methoxybenzyl)amino]methyl}propyl-3-(aminocarbonyl)-5-[(dipropylamino)carbonyl]benzoate
802(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-4-(3,4-dichlorophenyl)-4-oxobutanoate
804(1R,2S)-2-Amino-1-{[(3-methoxybenzyl)amino]methyl}-3-[4-(methoxycarbonyl)phenyl]propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
806(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-5-[(4-acetylphenyl)amino]-5-oxopentanoate
808 (1R,2S)-2-Amino-3-[4-(benzyloxy)phenyl]-1-{[(3-methoxybenzyl)amino]methyl}propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
810(1R,2S)-2-Amino-1-{[(3-methoxybenzyl)amino]methyl}-3-(phenylthio)propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
812(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-({2-[(methylamino)carbonyl]phenyl}thio)propanoate
814Hydrochloride (1R,2S)-2-amino-1-{[(3-methoxybenzyl)amino]methyl}-3-phenylpropyl-3-[(1-propinball)thio]propanoate
816(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-4-[(4-ethoxyphenyl)amino]-4-oxobutanoate
818(1R,2S)-2-Amino-3-[3-(benzyloxy)-5-forfinal]-1-{[(3-methylbutyl)amino]methyl}propyl-3-(aminocarbonyl)-5-[(dipropylamino)carbonyl]benzoate
820(1R,2S)-2-Amino-3-(3,5-differenl)-1-({[2-({[(3-methoxyphenyl)amino]carbonyl}oxy)ethyl]amino}methyl) propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
625N-[(2R,3S)-3-And the Ino-4-(3,5-differenl)-2-hydroxybutyl]-2-(2,3-dihydro-1-benzofuran-5-yl)-N-(3-active compounds)-1,3-thiazole-4-carboxamide
627N-{(2R,3S)-3-Amino-4-[3-(benzyloxy)phenyl]-2-hydroxybutyl}-N-(3-methoxybenzyl)-5-methyl-N',N'-dipropylacetamide
629N-[(2R,3S)-3-Amino-4-(4-chlorophenyl)-2-hydroxybutyl]-3-[(dipropylamino)sulfonyl]-N-(3-methoxybenzyl)propanamide
631N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-N'-internalname
633N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-3-(triptoreline)benzamid
635N-[(2R,3S)-3-Amino-4-(3-fluoro-4-were)-2-hydroxybutyl]-3-[(dipropylamino)sulfonyl]-N-(3-methoxybenzyl)propanamide
637N-[(2R,3S)-3-Amino-4-(3-chloro-5-forfinal)-2-hydroxybutyl]-3-[(dipropylamino)sulfonyl]-N-(3-methylbutyl)propanamide
639N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-3-(4,4-dimethyl-2,5-dioxoimidazolidin-1-yl)-N-(3-active compounds)-2-{[(1-propinball)sulfonyl]methyl}propanamide
641 N'-[4-(Acetylamino)phenyl]-N-[(2R,3S)-3-amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)succinamic
643N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-3-(1-cyanoethyl)-N-(3-active compounds)benzamid
645N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-N'-(5-phenyl-1,3,4-thiadiazol-2-yl)succinamic
647N1-{(2R,3S)-3-Amino-2-hydroxy-4-[3-(triptoreline)phenyl]butyl}-N1-benzyl-N3N3-DIPROPYLENE-1,3,5-tricarboxylic
649N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-5-methyl-N-[2-(2-oxo-2-pyrrolidin-1 ylethoxy)phenyl]-N',N'-dipropylacetamide
651N1-[(2R,3S)-3-Amino-4-(4-chlorophenyl)-2-hydroxybutyl]-N1-(3-methylbutyl)-N3N3-DIPROPYLENE-1,3,5-tricarboxylic
653N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-2-(1,1-dissidocerida-2-thienyl)-N-(3-active compounds)ndimethylacetamide
655N-[(2R,3S)-3-Amino-4-(4-chlorophenyl)-2-hydroxyp the Teal]-N-benzyl-5-methyl-N',N'-dipropylacetamide
657N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-5-Gex-1-in-1-iniatiated
659N-[(2R,3S)-3-Amino-4-(3-bromophenyl)-2-hydroxybutyl]-3-[(dipropylamino)sulfonyl]-N-(3-methylbutyl)propanamide
661N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-3-methoxyethoxy-5-carboxamid
663N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-2,3-dimethyl-1H-indole-7-carboxamide
665N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-4-(3-chlorophenyl)-N-(3-active compounds)-2-hydroxy-4-oxobutanamide
667N1-[(2R,3S)-3-Amino-4-(3-fluoro-4-methoxyphenyl)-2-hydroxybutyl]-N1-(3-methoxybenzyl)-N3N3-DIPROPYLENE-1,3,5-tricarboxylic
669N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-2-(1-methyl-1H-indol-3-yl)-2-oxoacetate
671N-[(2R,3S)-3-Amin is-4-(3-fluoro-4-were)-2-hydroxybutyl]-5-methyl-N-(3-methylbutyl)-N',N'-dipropylacetamide
673N-[(2R,3S)-3-Amino-2-hydroxy-4-(4-were)butyl]-3-[(dipropylamino)sulfonyl]-N-(3-methoxybenzyl)propanamide
675N1-[(2R,3S)-3-Amino-4-(3-fluoro-4-were)-2-hydroxybutyl]-N1-benzyl-N3N3-DIPROPYLENE-1,3,5-tricarboxylic
677N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-2-[5-(4-were)-2H-tetrazol-2-yl]ndimethylacetamide
679N-[(2R,3S)-3-Amino-4-(3,5-dichlorophenyl)-2-hydroxybutyl]-3-[(dipropylamino)sulfonyl]-N-(3-methoxybenzyl)propanamide
681N1-[(2R,3S)-3-Amino-2-hydroxy-4-(2-thienyl)butyl]-N1-(3-methylbutyl)-N3N3-DIPROPYLENE-1,3,5-tricarboxylic
683N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-5-methyl-3-phenylisoxazol-4-carboxamid
685N-[(2R,3S)-3-Amino-4-(4-forfinal)-2-hydroxybutyl]-N-benzyl-5-methyl-N',N'-dipropylacetamide
687 N1-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N1-(3-active compounds)-N2-[(methylsulphonyl)acetyl]-N2-pentylpyridine
689
691
693N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-4-(1H-indol-3-yl)-4-oxobutanamide
695N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N'-(5-benzyl)-1,3,4-thiadiazole-2-yl)-N-(3-active compounds)succinamic
697N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-4-(3-fluoro-4-methoxyphenyl)-4-oxobutanamide
699Ethyl-4-([(2R,3S)-3-amino-4-(3,5-differenl)-2-hydroxybutyl]{3-[(dipropylamino)carbonyl]-5-methylbenzoyl}amino)piperidine-1-carboxylate
701N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-4-(2-forbe the zoilus)-1H-pyrrol-2-carboxamide
703N1-[(2R,3S)-3-Amino-4-(4-chlorophenyl)-2-hydroxybutyl]-N1-benzyl-N3N3-DIPROPYLENE-1,3,5-tricarboxylic
705N1-{(2R,3S)-3-Amino-2-hydroxy-4-[3-(trifluoromethyl)phenyl]butyl}-N1-(3-methylbutyl)-N3N3-DIPROPYLENE-1,3,5-tricarboxylic
707N-[(2R,3S)-3-Amino-2-hydroxy-4-(4-hydroxyphenyl)butyl]-5-methyl-N-(3-methylbutyl)-N',N'-dipropylacetamide
709N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-2-(4-(morpholine-4-ylphenyl)ndimethylacetamide
711N-{(2R,3S)-3-Amino-2-hydroxy-4-[3-(triptoreline)phenyl]butyl}-3-[(dipropylamino)sulfonyl]-N-(3-methoxybenzyl)propanamide
713N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N'-benzyl-N'-(1-cyclopropylethyl)-N-(3-active compounds)succinamic
715N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-3-(2,5-dimethylbenzoyl)-N-(3-methoxybenzyl)-5-methylbenzamide
717
719N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-2-(3-hydroxyphenyl)ndimethylacetamide
721N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-3-[hydroxy(2-were)methyl]-N-(3-methoxybenzyl)-5-methylbenzamide
723N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-5-(ethylthio)nicotinamide
725N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-4-[4-(2-furoyl)piperazine-1-yl]-4-oxobutanamide
727N-[(2R,3S)-3-Amino-4-(3-fluoro-4-were)-2-hydroxybutyl]-N-benzyl-5-methyl-N',N'-dipropylacetamide
729N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-3-occaisonaly-1-carboxamid
731N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-3-(ethylthio)benzamid
733 N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)thieno[2,3-b]quinoline-2-carboxamide
735The hydrochloride of N-[(2R,3S)-3-amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-3-(4-methyl-1,3-oxazol-2-yl)benzamide
737N1-[(2R,3S)-3-Amino-4-(4-forfinal)-2-hydroxybutyl]-N1-benzyl-N3N3-DIPROPYLENE-1,3,5-tricarboxylic
739N-(2-{[[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl](3-active compounds)amino]carbonyl}phenyl)-N-methyl-2-furamide
741N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-2-hydroxy-4-(3-methoxyphenyl)-4-oxobutanamide
743N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-cycloheptyl-5-methyl-N',N'-dipropylacetamide
745N1-[(2R,3S)-3-Amino-2-hydroxy-4-(4-were)butyl]-N1-(3-methylbutyl)-N3N3-DIPROPYLENE-1,3,5-tricarboxylic
747The hydrochloride of N-[(2R,3S)-3-amino-4-(3-fluoro-5-hydroxyphenyl)-hydroxybutyl]-3-[(dipropylamino)sulfonyl]-N-(3-methoxybenzyl)propanamide
749N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-5-hydroxy-1H-indole-2-carboxamide
751N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-2,2-DIMETHYLPROPANE-8-carboxamide
7534-Oxide N-[(2R,3S)-3-amino-4-(3,5-differenl)-2-hydroxybutyl]-6-benzyl-N-(3-active compounds)pyrazin-2-carboxamide
7552-({[[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl](3-methoxybenzyl)amino]carbonyl}amino)-N,N-dipropylacetamide
757N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-[(1R)-1-(hydroxymethyl)-2-methylpropyl]-5-methyl-N',N'-dipropylacetamide
759N-[(2R,3S)-3-Amino-4-(3-chloro-5-forfinal)-2-hydroxybutyl]-N-benzyl-3-[(dipropylamino)sulfonyl]propanamide
761N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-4-(4-methoxyphenyl)-4-oxobutanamide
763N1-[(2R,3S)-3-Am is but-2-hydroxy-4-(4-hydroxyphenyl)butyl]-N 1-benzyl-N3N3-DIPROPYLENE-1,3,5-tricarboxylic
765N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-3-methyl-4-oxo-3,4-dihydrophenazine-1-carboxamid
767N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-3,4-dihydro-2H-1,5-benzodioxepin-7-carboxamid
769N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-2-[4-(2,5-dioxopiperidin-1-yl)phenoxy]-N-(3-active compounds)ndimethylacetamide
771N1-[(2R,3S)-3-Amino-4-(2-furyl)-2-hydroxybutyl]-N1-(3-methoxybenzyl)-N3N3-DIPROPYLENE-1,3,5-tricarboxylic
773N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-5-methyl-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidine-6-carboxamide
775N1-[(2R,3S)-3-Amino-4-(1,3-benzodioxol-5-yl)-2-hydroxybutyl]-N1-(3-methylbutyl)-N3N3-DIPROPYLENE-1,3,5-tricarboxylic
777
779N-[(2R,3S)-3-Amino-4-(3-chloro-5-forfinal)-2-hydroxybutyl]-N-(3-methoxybenzyl)-N',N'-dipropylenetriamine
781N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-6-fluoro-2-hydroxyquinolin-4-carboxamid
783N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-4-oxo-4-(2-thienyl)butanamide
785N3-{[[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl](3-methoxybenzyl)amino]carbonyl}-N1N1-dipropyl-β-alaninemia
787N1-[(2R,3R)-3-Amino-2-hydroxy-4-(phenylthio)butyl]-N1-(3-methoxybenzyl)-N3N3-DIPROPYLENE-1,3,5-tricarboxylic
789N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-[(1R)-1-(hydroxymethyl)-2-methylpropyl]-5-methyl-N',N'-dipropylacetamide
791N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-[(1R,2S)-1-(hydroxymethyl)-2-methylbutyl]-5-methyl-N',N'-dipropylacetamide
793N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-2-(phenoxymethyl)benzamid
795N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N'-(2,4-differenl)-N-(3-active compounds)pentanedione
797N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N'-(4,6-dimethylpyrimidin-2-yl)-N-(3-active compounds)pentanedione
799N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-3-(3-methoxybenzoyl)-N-(3-methoxybenzyl)-5-methylbenzamide
801N1-{(2R,3S)-3-Amino-4-[3-(benzyloxy)phenyl]-2-hydroxybutyl}-N1-(3-methoxybenzyl)-N3N3-DIPROPYLENE-1,3,5-tricarboxylic
803N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-4-(3,4-dichlorophenyl)-N-(3-active compounds)-4-oxobutanamide
805Methyl-4-{(2S,3R)-2-Amino-4-[{3-[(dipropylamino)carbonyl]-5-methylbenzoyl}(3-methoxybenzyl)amino]-3-hydroxybutyl}benzoate
807N'-(4-Acetylphenyl)-N-[(2R,3S)-3-amino-4-(5-differenl)-2-hydroxybutyl]-N-(3-active compounds)pentanedione
809N-{(2R,3S)-3-Amino-4-[4-(benzyloxy)phenyl]-2-hydroxybutyl}-N-(3-methoxybenzyl)-5-methyl-N',N'-dipropylacetamide
811N-[(2R,3R)-3-Amino-2-hydroxy-4-(phenylthio)butyl]-N-(3-methoxybenzyl)-5-methyl-N',N'-dipropylacetamide
8132-({3-[[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl](3-active compounds)amino]-3-oxopropyl}thio)-N-methylbenzamide
815The hydrochloride of N-[(2R,3S)-3-amino-2-hydroxy-4-phenylbutyl]-N-(3-methoxybenzyl)-3-[(1-propinball)thio]propanamide
817N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N'-(4-ethoxyphenyl)-N-(3-active compounds)succinamic
819N1-{(2R,3S)-3-Amino-4-[3-(benzyloxy)-5-forfinal]-2-hydroxybutyl}-N1-(3-methylbutyl)-N3N3-DIPROPYLENE-1,3,5-tricarboxylic
8212-([(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]{3-[(dipropylamino)carbonyl]-5-methylbenzoyl}amino)ethyl(3-methoxyphenyl)carbamate
822 (1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-(benzyloxy)benzoate
824(1R,2S)-2-Amino-3-(3,5-differenl)-1-({[(1S)-2-hydroxy-1-methylethyl]amino}methyl)propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
826(1R,2S)-2-Amino-3-(pentafluorophenyl)-1-({[3-(trifluoromethyl)benzyl]amino}methyl)propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
828(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-4-(4-hydroxyphenyl)-4-oxobutanoate
830(1R,2S)-2-Amino-1-{[(3-methoxybenzyl)amino]methyl}-3-[3-(trifluoromethyl)phenyl]propyl-3-[(dipropylamino)sulfonyl]propanoic
832The dihydrochloride of (1R,2S)-2-amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-(piperidine-3-ylsulphonyl)benzoate
834(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-6-chloro-4-hydroxyquinolin-2-carboxylate
836(1R,2S)-2-Amino-1-{[(3-methoxybenzyl)amino]methyl}-3-(2-thienyl)about the Il-5-(dipropylamino)-5-oxopentanoate
838(1R,2S)-2-Amino-1-{[(3-methoxybenzyl)amino]methyl}-4-methylpentyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
840(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl(6-oxo-3-phenylpyridazin-1(6N)-yl)acetate
842(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-{4-[(methylsulphonyl)amino]phenyl}propanoate
844(1R,2S)-2-Amino-3-(4-fluoro-3-were)-1-{[(3-methoxybenzyl)amino]methyl}propyl-3-(aminocarbonyl)-5-[(dipropylamino)carbonyl]benzoate
846(1R,2S)-2-Amino-1-[(benzylamino)methyl]-3-(4-were)propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
848(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-iodobenzyl)amino]methyl}propyl-3-(2-chlorophenoxy)propanoate
850(1R,2S)-2-Amino-3-(4-forfinal)-1-{[(3-methylbutyl)amino]methyl}propyl-3-(aminocarbonyl)-5-[(dipropylamino)carbonyl]benzoate
852(1R2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-N-(4-chlorobenzoyl)-D-alaninate
854Hydrochloride (1R,2S)-2-amino-3-[3-(benzyloxy)-5-forfinal]-1-{[(3-methoxybenzyl)amino]methyl}propyl-3-[(dipropylamino)sulfonyl]propanoate
856(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-4-(4-were)-4-oxobutanoate
858(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-4-oxo-4-{[3-(trifluoromethyl)phenyl]amino}of butanoate
860(1R,2S)-2-Amino-3-(1,3-benzodioxol-5-yl)-1-{[(3-methoxybenzyl)amino]methyl}propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
862(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl(5-pyridin-2-yl-2H-tetrazol-2-yl)acetate
864
866(1R,2S)-2-Amino-1-{[(3-methoxybenzyl)amino]methyl}-3-(3-were)propyl-3-[(dipropylamino)sulfonyl]propanoic
868 (1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propylenoxide-5-carboxylate
870(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl(3,5-dimethoxyphenoxy)acetate
872(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-4-(2,5-dimethyl-1H-pyrrol-1-yl)-3-hydroxybenzoate
874(1R,2S)-2-Amino-3-(3-bromophenyl)-1-{[(3-methoxybenzyl)amino]methyl}propyl-5-(dipropylamino)-5-oxopentanoate
876(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-4-{[5-(cyclopentylmethyl)-1,3,4-thiadiazole-2-yl]amino}-4-oxobutanoate
878(1R,2S)-2-Amino-1-[(benzylamino)methyl]-3-[3-(trifluoromethyl)phenyl]propyl-3-(aminocarbonyl)-5-[(dipropylamino)carbonyl]benzoate
880(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl(3-oxo-1,2-benzothiazol-2(3H)-yl)acetate
882(1R,2S)-2-Amino-3-(3,5-differenl)-1-({[1-methyl-5-(pyrrolidin-1-ylcarbonyl)-1H-pyrrol-3-ylamino}methyl)propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
884(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-4-(3,4-differenl)-4-oxobutanoate
886(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-4-(2-naphthyl)-4-oxobutanoate
888(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-4,6-detoxification-2-carboxylate
890(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-4-(5-methyl-1H-pyrrol-2-yl)-4-oxobutanoate
892Hydrochloride (1R,2S)-2-amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-({[2-(methylamino)ethyl]amino}sulfonyl)benzoate
894(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-methoxybenzyl)amino]methyl}propyl-3-methyl-5-(4-methylbenzoyl)benzoate
896(1R,2S)-2-Amino-3-(1,3-benzodioxol-5-yl)-1-[(benzylamino)methyl]propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
898Hydrochloride (1R,2S)-amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-(piperazine-1-ylsulphonyl)benzoate
900(1R,2S)-2-Amino-1-[({2-[4-(aminosulfonyl)phenyl]ethyl}amino)methyl]-3-(3,5-differenl)propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
902(1R,2S)-2-Amino-3-(3,5-differenl)-1-({[2-hydroxy-1-(hydroxymethyl)ethyl]amino}methyl)propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
904(1R,2S)-2-Amino-3-(4-fluoro-3-were)-1-{[(3-methylbutyl)amino]methyl}propyl-3-(aminocarbonyl)-5-[(dipropylamino)carbonyl]benzoate
906(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-(3-oxo-2,1-benzisothiazol-1(3H)-yl)propanoate
908(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl(2,6-dihydroxypyrimidine-4-yl)acetate
910(1R,2S)-2-Amino-1-{[(3-methoxybenzyl)amino]methyl}-3-[3-(trifluoromethyl)phenyl]propyl-5-(dipropylamino)-5-oxopentanoate
912(1R,2S)-2-Amino-1-[(benzylamino)methyl]-3-(4-hydroxyphenyl)propyl-3-[(dipropylamino)sulfonyl]propanoic
914(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-4-(3,4-differenl)-2-methyl-4-oxobutanoate
916(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-5-oxo-5-[(2-pyridin-2-retil)amino]pentanoate
918(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl[2-(4-forfinal)-1,3-benzoxazol-5-yl]acetate
920(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-N-(anilinoacrolein)glycinate
922(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-N-(2,6-dimethoxybenzoyl)glycinate
924(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-2-(1,3-dition-2-yl)-3-furoate
9261R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-2-[2-oxo-2-(propylamino)ethyl]benzoate
928(1R,2S)-2-Amino-1-[(benzylamino)methyl]-3-(3-bromophenyl)propyl-3-[(dipropylamino)su is hanil]propanoate
930(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-iodobenzyl)amino]methyl}propyl-3-(2-forfinal)propanoate
932(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-5-methylthiophene-2-carboxylate
934(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-iodobenzyl)amino]methyl}propyl[4-(benzyloxy)phenyl]acetate
936(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl[(5,7-dimethyl[1,2,4]triazolo[4,3-a]pyrimidine-3-yl)thio]acetate
938(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-4-[(1-acetyl-2,3-dihydro-1H-indol-7-yl)amino]-4-oxobutanoate
940(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-5-[(3-acetylphenyl)amino]-5-oxopentanoate
942(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-(4-chlorophenoxy)-2-hydroxypropanoate
944N3-[(1S,2R)-3-(Bensalem the but)-1-(3-fluoro-4-methoxyphenyl)-2-hydroxypropyl]-N 1N1-DIPROPYLENE-1,3,5-tricarboxylic
946(1R,2S)-2-Amino-1-[(benzylamino)methyl]-3-(3-were)propyl-3-(aminocarbonyl)-5-[(dipropylamino)carbonyl]benzoate
948(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-1H-indole-7-carboxylate
950(1R,2S)-2-Amino-1-{[(3-methylbutyl)amino]methyl}-3-(3-were)propyl-3-(aminocarbonyl)-5-[(dipropylamino)carbonyl]benzoate
952(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-4-(1,2,3-thiadiazole-4-yl)benzoate
954(1R,2S)-2-Amino-3-[3-(benzyloxy)-5-forfinal]-1-{[(3-methoxybenzyl)amino]methyl}propyl-3-[(dipropylamino)sulfonyl]propanoic
956(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-(4,4-dimethyl-2,5-dioxoimidazolidin-1-yl)-2-{[(1-propinball)sulfonyl]methyl}propanoic
958(1R,2S)-2-Amino-1-{[(3-methylbutyl)amino]methyl}-3-(4-were)propyl-3-[(dipropylamino)carbonyl]-5-IU is eventout
960(1R,2S)-2-Amino-1-[(benzylamino)methyl]-3-[3-fluoro-5-(trifluoromethyl)phenyl]propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
962(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl[1-methyl-3-(methylthio)-1H-indol-2-yl]acetate
964(1R,2S)-2-Amino-3-(3,5-dichlorophenyl)-1-{[(3-methylbutyl)amino]methyl}propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
966(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl[(2-{[4-(1,3-oxazol-5-yl)phenyl]amino}-2-oxoethyl)thio]acetate
968(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-4-(2-furyl)-4-oxobutanoate
970(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-(3-pyridin-2-yl-1,2,4-oxadiazol-5-yl)propanoate
972(1R,2S)-2-the Mino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl[2-(acetylamino)-1,3-thiazol-4-yl]acetate
974(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl[(4-methyl-4H-1,2,4-triazole-3-yl)thio](phenyl)acetate
976(1R,2S)-2-Amino-3-(4-chlorophenyl)-1-{[(3-methylbutyl)amino]methyl}propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
978(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-4-(1,3-benzothiazol-2-yl)butanoate
980(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-4-[(3-chloro-4-forfinal)amino]-4-oxobutanoate
982(1R,2S)-2-Amino-3-[3-(benzyloxy)-5-forfinal]-1-{[(3-methylbutyl)amino]methyl}propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
984(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl[(2-oxo-2,3-dihydroquinazolin-4-yl)thio]acetate
823N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-3-(benzyloxy)-N-(3-active compounds)benzamid
825N-[(2R,3S)-3-Amino-4(3,5-differenl)-2-hydroxybutyl]-N-[(1S)-2-hydroxy-1-methylethyl]-5-methyl-N',N'-dipropylacetamide
827N-[(2R,3S)-3-Amino-2-hydroxy-4-(pentafluorophenyl)butyl]-5-methyl-N',N'-dipropyl-N-[3-(trifluoromethyl)benzyl]isophthalamide
829N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-4-(4-hydroxyphenyl)-4-oxobutanamide
831N-{(2R,3S)-3-Amino-2-hydroxy-4-[3-(trifluoromethyl)phenyl]butyl}-3-[(dipropylamino)sulfonyl]-N-(3-methoxybenzyl)propanamide
833The dihydrochloride of N-[(2R,3S)-3-amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-3-(piperidine-3-ylsulphonyl)benzamide
835N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-6-chloro-N-(3-active compounds)-4-hydroxyquinolin-2-carboxamide
837N-[(2R,3S)-3-Amino-2-hydroxy-4-(2-thienyl)butyl]-N-(3-methoxybenzyl)-N',N'-dipropylenetriamine
839N-[(2R,3S)-3-Amino-2-hydroxy-5-methylhexan]-N-(3-methoxybenzyl)-5-methyl-N',N'-dipropylacetamide
841N-[(2R,3S)-3-Amino-4-(3,5-differeni is)-2-hydroxybutyl]-N-(3-active compounds)-2-(6-oxo-3-phenylpyridazin-1(6N)-yl)ndimethylacetamide
843N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-3-{4-[(methylsulphonyl)amino]phenyl}propanamide
845N1-[(2R,3S)-3-Amino-4-(4-fluoro-3-were)-2-hydroxybutyl]-N1-(3-methoxybenzyl)-N3N3-DIPROPYLENE-1,3,5-tricarboxylic
847N-[(2R,3S)-3-Amino-2-hydroxy-4-(4-were)butyl]-N-benzyl-5-methyl-N',N'-dipropylacetamide
849N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-3-(2-chlorophenoxy)-N-(3-iodobenzyl)propanamide
851N1-[(2R,3S)-3-Amino-4-(4-forfinal)-2-hydroxybutyl]-N1-(3-methylbutyl)-N3N3-DIPROPYLENE-1,3,5-tricarboxylic
853
855The hydrochloride of N-{(2R,3S)-3-amino-4-[3-(benzyloxy)-5-forfinal]-2-hydroxybutyl}-3-[(dipropylamino)sulfonyl]-N-(3-methoxybenzyl)propanamide
857N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-4-(4-were)-4-oxobutanamide
859(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-4-oxo-4-{[3-(trifluoromethyl)phenyl]amino}of butanoate
861N-[(2R,3S)-3-Amino-4-(1,3-benzodioxol-5-yl)-2-hydroxybutyl]-N-(3-methoxybenzyl)-5-methyl-N',N'-dipropylacetamide
863
865
867N-[(2R,3S)-3-Amino-2-hydroxy-4-(3-were)butyl]-3-[(dipropylamino)sulfonyl]-N-(3-methoxybenzyl)propanamide
869N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)isoxazol-5-carboxamid
871 N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-2-(3,5-dimethoxyphenoxy)-N-(3-active compounds)ndimethylacetamide
873N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-4-(2,5-dimethyl-1H-pyrrol-1-yl)-N-(3-active compounds)-3-hydroxybenzamide
875N-[(2R,3S)-3-Amino-4-(3-bromophenyl)-2-hydroxybutyl]-N-(3-methoxybenzyl)-N',N'-dipropylenetriamine
877N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N'-[5-(cyclopentylmethyl)-1,3,4-thiadiazole-2-yl]-N-(3-active compounds)succinamic
879N1-{(2R,3S)-3-Amino-2-hydroxy-4-[3-(trifluoromethyl)phenyl]butyl}-N1-benzyl-N3N3-DIPROPYLENE-1,3,5-tricarboxylic
881N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-2-(3-oxo-1,2-benzisothiazol-2(3H)-yl)ndimethylacetamide
883N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-5-methyl-N-[1-methyl-5-(pyrrolidin-1-ylcarbonyl)-1H-pyrrol-3-yl]-N',N'-dipropylacetamide
885N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-HYDR shall Sibuti]-4-(3,4-differenl)-N-(3-active compounds)-4-oxobutanamide
887N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-4-(2-naphthyl)-4-oxobutanamide
889N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-4,6-diethoxy-N-(3-active compounds)pyridine-2-carboxamide
891N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-4-(5-methyl)-1H-pyrrol-2-yl)-4-oxobutanamide
893The hydrochloride of N-[(2R,3S)-3-amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-3-({[2-(methylamino)ethyl]amino}sulfonyl)benzamide
895N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-methoxybenzyl)-3-methyl-5-(4-methylbenzoyl)benzamid
897N-[(2R,3S)-3-Amino-4-(1,3-benzodioxol-5-yl)-2-hydroxybutyl]-N-benzyl-5-methyl-N',N'-dipropylacetamide
899The hydrochloride of N-[(2R,3S)-3-amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-3-(piperazine-1-ylsulphonyl)benzamide
901N-[(2R,3S)-3-Amino-4-(3,5-d is forfinal)-2-hydroxybutyl]-N-{2-[4-(aminosulfonyl)phenyl]ethyl}-5-methyl-N',N'-dipropylacetamide
903N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-[2-hydroxy-1-(hydroxymethyl)ethyl]-5-methyl-N',N'-dipropylacetamide
905N1-[(2R,3S)-3-Amino-4-(4-fluoro-3-were)-2-hydroxybutyl]-N1-(3-methylbutyl)-N3N3-DIPROPYLENE-1,3,5-tricarboxylic
907N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-3-(3-oxo-2,1-benzisothiazol-1(3H)-yl)propanamide
909N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-2-(2,6-dihydroxypyrimidine-4-yl)-N-(3-active compounds)ndimethylacetamide
911N-{(2R,3S)-3-Amino-2-hydroxy-4-[3-(trifluoromethyl)phenyl]butyl}-N-(3-methoxybenzyl)-N',N'-dipropylenetriamine
913N-[(2R,3S)-3-Amino-2-hydroxy-4-(4-hydroxyphenyl)butyl]-N-benzyl-3-[(dipropylamino)sulfonyl]propanamide
915N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-4-(3,4-differenl)-N-(3-active compounds)-2-methyl-4-oxobutanamide
917 N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-N'-(2-pyridin-2-retil)pentanedione
919N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-2-[2-(4-forfinal)-1,3-benzoxazol-5-yl]ndimethylacetamide
921N1-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N2(anilinoacrolein)-N1-(3-active compounds)glycinamide
923
925N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-2-(1,3-dition-2-yl)-N-(3-active compounds)-3-furamide
927N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-2-[2-oxo-2-(propylamino)ethyl]benzamide
929N-[(2R,3S)-3-Amino-4-(3-bromophenyl)-2-hydroxybutyl]-N-benzyl-3-[(dipropylamino)sulfonyl]propanamide
931N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydrox the butyl]-3-(2-forfinal)-N-(3-iodobenzyl)propanamide
933N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-5-methylthiophene-2-carboxamide
935N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-2-[4-(benzyloxy)phenyl]-N-(3-iodobenzyl)ndimethylacetamide
937N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-2-[(5,7-dimethyl[1,2,4]triazolo[4,3-a]pyrimidine-3-yl)thio]-N-(3-active compounds)ndimethylacetamide
939N'-(1-Acetyl-2,3-dihydro-1H-indol-7-yl)-N-[(2R,3S)-3-amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)succinamic
941N'-(1-Acetylphenyl)-N-[(2R,3S)-3-amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)pentanedione
943N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-3-(4-chlorophenoxy)-N-(3-active compounds)-2-hydroxypropanoic
945N3-[(1S,2R)-3-Benzylamino-1-(3-fluoro-4-methoxybenzyl)-2-hydroxypropyl]-N1N1-DIPROPYLENE-1,3,5-tricarboxylic
947N1-[(2R,3S)-3-Amino-2-hydroxy-4-(3-were)butyl]-N 1-benzyl-N3N3-DIPROPYLENE-1,3,5-tricarboxylic
949N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-1H-indole-7-carboxamide
951N1-[(2R,3S)-3-Amino-2-hydroxy-4-(3-were)butyl]-N1-(3-methylbutyl)-N3N3-DIPROPYLENE-1,3,5-tricarboxylic
953N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-4-(1,2,3-thiadiazole-4-yl)benzamid
955N-{(2R,3S)-3-Amino-4-[3-(benzyloxy)-5-forfinal]-2-hydroxybutyl}-3-[(dipropylamino)sulfonyl]-N-(3-methoxybenzyl)propanamide
957N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-3-(4,4-dimethyl-2,5-dioxoimidazolidin-1-yl)-N-(3-active compounds)-2-{[(1-propinball)sulfonyl]methyl}propanamide
959N-[(2R,3S)-3-Amino-2-hydroxy-4-(4-were)butyl]-5-methyl-N-(3-methylbutyl)-N',N'-dipropylacetamide
961N-{(2R,3S)-3-Amino-4-[3-fluoro-5-(trifluoromethyl)phenyl]-2-hydroxybutyl}-N-benzyl-5-methyl-N',N'-d is prophylatically
963N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-2-[1-methyl-3-(methylthio)-1H-indol-2-yl]ndimethylacetamide
965N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-5-methyl-N-(3-methylbutyl)-N',N'-dipropylacetamide
9672-({2-[[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl](3-active compounds)amino]-2-oxoethyl}thio)-N-[4-(1,3-oxazol-5-yl)phenyl]ndimethylacetamide
969N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-4-(2-furyl)-4-oxobutanamide
971N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-3-(3-pyridin-2-yl-1,2,4-oxadiazol-5-yl)propanamide
9732-[2-(Acetylamino)-1,3-thiazol-4-yl]-N-[(2R,3S)-3-amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)ndimethylacetamide
975N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-2-[(4-methyl-4H-1,2,4-triazole-3-yl)thio]-2-phenylacetamide
977N-[(2R,3S)-3-the Mino-4-(4-chlorophenyl)-2-hydroxybutyl]-5-methyl-N-(3-methylbutyl)-N',N'-dipropylacetamide
979N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-4-(1,3-benzothiazol-2-yl)-N-(3-active compounds)butanamide
981N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N'-(3-chloro-4-forfinal)-N-(3-active compounds)succinamic
983N-{(2R,3S)-3-Amino-4-[3-(benzyloxy)-5-forfinal]-2-hydroxybutyl}-5-methyl-N-(3-methylbutyl)-N',N'-dipropylacetamide
985N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-2-[(2-oxo-2,3-dihydroquinazolin-4-yl)thio]ndimethylacetamide
986(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-methoxybenzyl)amino]methyl}propyl-3-methyl-5-(2-methylbenzoyl)benzoate
988(1R,2S)-2-Amino-3-(4-hydroxyphenyl)-1-{[(3-methoxybenzyl)amino]methyl}propyl-3-methyl-5-(dipropylamino)-5-oxopentanoate
990(1R,2S)-2-Amino-1-[(benzylamino)methyl]-3-(4-were)propyl-3-(aminocarbonyl)-5-[(dipropylamino)carbonyl]benzoate
992(1R,2S)-2-Amino-3-(3,differenl)-1-{[(3-active compounds)amino]methyl}propyl-4-propoxybenzene
994(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-1-methyl-1H-indole-2-carboxylate
996(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-5-chloro-2-(3-methyl-4H-1,2,4-triazole-4-yl)benzoate
998(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-4-(3,4-differenl)-2-methoxy-4-oxobutanoate
1000(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl[3-(2-thienyl)-1H-pyrazole-1-yl]acetate
1002(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-5-aniline-5-oxopentanoate
1004(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl(2-thioxo-1,3-benzothiazol-3(2H)-yl)acetate
1006(1R,2S)-2-Amino-1-[(benzylamino)methyl]-3-cyclohexylprop-3-[(dipropylamino)carbonyl]-5-methylbenzoate
1008(1R,2S)-2-Amino-1-{[(3-methoxybenzyl)amino]METI the}-3-(4-methoxyphenyl)propyl-3-(aminocarbonyl)-5-[(dipropylamino)carbonyl]benzoate
1010(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl(3-hydroxy-4-were)acetate
1012(1R,2S)-2-Amino-3-[3-fluoro-5-(trifluoromethyl)phenyl]-1-{[(3-methylbutyl)amino]methyl}propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
1014(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-7-fluoro-4H-imidazo[5,1-c][1,4]benzoxazin-3-carboxylate
1016(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-4-(3,4-dihydro-2H-1,5-benzodioxepin-7-yl)-4-oxobutanoate
1018(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-1-benzofuran-3-carboxylate
1020(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-[(3,4-dichlorophenyl)amino]-3-oxopropanoic
1022(1R,2S)-2-Amino-1-[(benzylamino)methyl]-3-[3-fluoro-5-(trifluoromethyl)phenyl]propyl-3-(aminocarbonyl)-5-[(dipropylamino)carbonyl]benzoate
1024 (1R,2S)-2-Amino-3-(3,5-differenl)-1-({[(1R)-2-hydroxy-1-methylethyl]amino}methyl)propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
1026(1R,2S)-2-Amino-1-[(benzylamino)methyl]-3-(3-were)propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
1028(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-5-oxo-5-(pyridine-3-ylamino)pentanoate
1030(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-2-methyl-4-oxo-4H-chromen-6-carboxylate
1032(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl({2-[(5-methylisoxazol-3-yl)amino]-2-oxoethyl}thio)acetate
1034(1R,2S)-2-Amino-3-(3,5-differenl)-1-({[3-(1H-imidazol-1-yl)propyl]amino}methyl)propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
1036(1R,2S)-2-Amino-3-[3-fluoro-5-(trifluoromethyl)phenyl]-1-{[(3-methoxybenzyl)amino]methyl}propyl-3-[(dipropylamino)sulfonyl]propanoic
1038(1R,2S)-2-Amino-3-(4-hydroxyphenyl)-1-{[3-methylbutyl)amino]methyl}propyl-3-[(dipropylamino)sulfonyl]propanoic
1040(1R,2S)-2-Amino-3-(1,3-benzodioxol-5-yl)-1-{[(3-methylbutyl)amino]methyl}propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
1042(1R,2S)-2-Amino-1-{[(3-methylbutyl)amino]methyl}propyl-3-(2-thienyl)propyl-3-[(dipropylamino)sulfonyl]propanoic
1044(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-4-[(2,2-dimethylpropanoyl)amino]-2-hydroxybenzoate
1046(1R,2S)-2-Amino-3-(3-methoxyphenyl)-1-{[(3-methylbutyl)amino]methyl}propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
1048(1R,2S)-2-Amino-3-(4-forfinal)-1-({[3-(trifluoromethyl)benzyl]amino}methyl)propyl-3-{[(3-methoxybenzyl)amino]sulfonyl}benzoate
1050(1R,2S)-2-Amino-1-{[(3-methylbutyl)amino]methyl}-3-[3-(trifluoromethyl)phenyl]propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
1052(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-6-(2-prolamine)hexanoate
1054 (1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl[(1-phenyl-4,5-dihydro-1H-tetrazol-5-yl)thio]acetate
1056(1R,2S)-2-Amino-3-phenyl-1-({[3-(trifluoromethyl)benzyl]amino}methyl)propyl-3-{[(3-methoxybenzyl)amino]sulfonyl}benzoate
1058(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-4-(3,4-dihydro-2H-chromen-6-yl)-4-oxobutanoate
1060(1R,2S)-2-Amino-3-(3-methoxyphenyl)-1-{[(3-methylbutyl)amino]methyl}propyl-3-(aminocarbonyl)-5-[(dipropylamino)carbonyl]benzoate
1062(1R,2S)-2-Amino-3-(3-fluoro-4-were)-1-{[(3-methoxybenzyl)amino]methyl}propyl-5-(dipropylamino)-5-oxopentanoate
1064(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propylenglycol-2-carboxylate
1066(1R,2S)-2-Amino-1-[(benzylamino)methyl]-3-[3-(triptoreline)phenyl]propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
10681-Oxide (1R,2S)-2-amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]METI the}propylenimine
1070(1R,2S)-2-Amino-3-[3-(benzyloxy)-5-forfinal]-1-{[(3-methylbutyl)amino]methyl}propyl-3-[(dipropylamino)sulfonyl]propanoic
1072(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-iodobenzyl)amino]methyl}propyl[(aminocarbonyl)oxy]acetate
1074(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-2,3-dihydro-1H-cyclopent[b]quinoline-9-carboxylate
1076(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-methyl-1H-pyrazole-5-carboxylate
1078(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-5-(benzoylamine)pentanoate
1080(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-4-[(methoxymethyl)thio]benzoate
1082(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-(1,3-benzothiazol-2-yl)-3-methoxypropanol
1084(1R,2S)-2-Amino-3-(3,5-differenl)-1{[(3-active compounds)amino]methyl}propyl-3-{[(methylamino)carbonyl]amino}-3-(3-thienyl)propanoate
1086(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-5-pyridin-2-althofen-2-carboxylate
1088(1R,2S)-2-Amino-1-[(benzylamino)methyl]-3-[3-(benzyloxy)-5-forfinal]propyl-3-(aminocarbonyl)-5-[(dipropylamino)carbonyl]benzoate
1090(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl(5,6-dimethyl-2,4-dioxo-1,2,3,4-tetrahydropyridine-3-yl)acetate
1092(1R,2S)-2-Amino-3-(3-fluoro-4-methoxyphenyl)-1-{[(3-methylbutyl)amino]methyl}propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
1094(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-2-isobutyl-1,3-doxasozin-5-carboxylate
1096(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-5-(acetylamino)-2-furoate
1098(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-N-[(4-methoxyphenyl)acetyl]glycinate
1100 (1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propylethylene-4-carboxylate
1102(1R,2S)-2-Amino-3-[3-(benzyloxy)phenyl]-1-{[(3-methylbutyl)amino]methyl}propyl-3-(aminocarbonyl)-5-[(dipropylamino)carbonyl]benzoate
1104(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl(4-hydroxy-3-methoxyphenyl)acetate
1106(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl[(4-phenyl-4H-1,2,4-triazole-3-yl)thio]acetate
1108(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl(3,5-acid)acetate
1110(1R,2S)-2-Amino-1-[(benzylamino)methyl]-3-(3-methoxyphenyl)propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoate
1112(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl(2-ethyl-4H-[1,2,4]triazolo[1,5-a]benzimidazole-4-yl)acetate
1114(1R,2S)-2-Amino-1-[(benzylamino)methyl]-3-(2-furyl)propyl-3-[(dipropylamino)carbonyl]-5-methylbenzoic/td>
1116(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-7-chloro-1-benzofuran-2-carboxylate
1118(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-2-(1,3-dioxo-1,3-dihydro-2H-isoindole-2-yl)propanoate
1120(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-(2-oxo-2H-1,3-benzoxazin-3(4H)-yl)propanoate
1122(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl(pyrimidine-2-ylthio)acetate
1124(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-4-{[3-(aminocarbonyl)-4,5,6,7-tetrahydro-1-benzothieno-2-yl]amino}-4-oxobutanoate
1126(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl[(5-phenyl-1,3,4-oxadiazol-2-yl)thio]acetate
1128(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propilinian-6-carboxylate
11301R,2S)-2-Amino-1-[(benzylamino)methyl]-3-(2-furyl)propyl-3-(aminocarbonyl)-5-[(dipropylamino)carbonyl]benzoate
1132(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-4-(2,3-dihydro-1,4-benzodioxin-6-yl)-4-oxobutanoate
1134(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-(1H-indol-3-yl)-1H-pyrazole-5-carboxylate
1136(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-2-hydroxy-4-{[(methylamino)carbonothioyl]amino}benzoate
1138(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-6-chloronicotinate
1140(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-4-(3-hydroxyphenyl)-4-oxobutanoate
1142(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl(phthalazine-1 ylthio)acetate
1144(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl[(1-oxidability-2-yl)thio]acetate
1146(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-e is ylbenzyl)amino]methyl}propyl-3-(acetylamino)-5-fluoro-1H-indole-2-carboxylate
1148(1R,2S)-2-Amino-3-phenyl-1-({[3-(trifluoromethyl)benzyl]amino}methyl)propyl-3-{[(3-Chlorobenzyl)amino]sulfonyl}benzoate
1150(1R,2S)-2-Amino-3-[4-(benzyloxy)phenyl]-1-{[(3-methoxybenzyl)amino]methyl}propyl-3-(aminocarbonyl)-5-[(dipropylamino)carbonyl]benzoate
1152(1R,2S)-2-Amino-3-(1,3-benzodioxol-5-yl)-1-[(benzylamino)methyl]propyl-3-(aminocarbonyl)-5-[(dipropylamino)carbonyl]benzoate
1154(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-4-(3,4-dichlorophenyl)-2-hydroxy-3-methyl-4-oxobutanoate
1156(1R,2S)-2-Amino-1-{[(3-methylbutyl)amino]methyl}-3-[3-(triptoreline)phenyl]propyl-3-[(dipropylamino)sulfonyl]propanoic
1158(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-4-[(5-methyl-1,3,4-thiadiazole-2-yl)amino]-4-oxobutanoate
1160(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl(2-ethyl-1H-benzimidazole-1-yl)acetate
(1R,2S)-2-Amino-3-(1,3-benzodioxol-5-yl)-1-{[(3-methoxybenzyl)amino]methyl}propyl-3-[(dipropylamino)sulfonyl]propanoic
1164(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-(2-oxo-1,3-benzoxazol-3(2H)-yl)propanoate
1166(1R,2S)-2-Amino-3-(3,5-dichlorophenyl)-1-{[(3-methylbutyl)amino]methyl}propyl-3-[(dipropylamino)sulfonyl]propanoic
1168(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-4-[(6-methylpyridin-2-yl)amino]-4-oxobutanoate
11704-((1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl)-3-ethyl(4R)-1,3-oxazolidin-3,4, in primary forms
987N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-methoxybenzyl)-3-methyl-5-(2-methylbenzoyl)benzamid
989N-[(2R,3S)-3-Amino-2-hydroxy-4-(4-hydroxyphenyl)butyl]-N-(3-methoxybenzyl)-N',N'-dipropylenetriamine
991 N1-[(2R,3S)-3-Amino-2-hydroxy-4-(4-were)butyl]-N1-benzyl-N3N3-DIPROPYLENE-1,3,5-tricarboxylic
993N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-4-propoxybenzene
995N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-1-methyl-1H-indole-2-carboxamide
997N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-5-chloro-N-(3-active compounds)-2-(3-methyl-4H-1,2,4-triazole-4-yl)benzamid
999N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-4-(3,4-differenl)-N-(3-active compounds)-2-methoxy-4-oxobutanamide
1001N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-2-[3-(2-thienyl-1H-pyrazole-1-yl]ndimethylacetamide
1003N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-N'-phenylenediamine
1005N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-2-(2-thioxo-1,3-benzothiazol-3(2H)-yl)ndimethylacetamide
1007N-[(2R,3S)-3-Amino-4-cyclohexyl-2-hydroxybutyl]-N-benzyl-5-methyl-N',N'-dipropylacetamide
1009N1-[(2R,3S)-3-Amino-2-hydroxy-4-(4-methoxyphenyl)butyl]-N1-(3-methoxybenzyl)-N3N3-DIPROPYLENE-1,3,5-tricarboxylic
1011N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-2-(3-hydroxy-4-were)ndimethylacetamide
1013N-{(2R,3S)-3-Amino-4-[3-fluoro-5-(trifluoromethyl)phenyl]-2-hydroxybutyl}-5-methyl-N-(3-methylbutyl)-N',N'-dipropylacetamide
1015N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-7-fluoro-4H-imidazol[5,1-c][1,4]benzoxazin-3-carboxamide
1017N-[(2R,3S)-3-AMI is about-4-(3,5-differenl)-2-hydroxybutyl]-4-(3,4-dihydro-2H-1,5-benzodioxepin-7-yl)-N-(3-active compounds)-4-oxobutanamide
1019N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-1-benzofuran-3-carboxamide
1021N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N'-(3,4-dichlorophenyl)-N-(3-active compounds)malonamide
1023N1-{(2R,3S)-3-Amino-4-[3-fluoro-5-(trifluoromethyl)phenyl]-2-hydroxybutyl}-N1-benzyl-N3N3-DIPROPYLENE-1,3,5-tricarboxylic
1025N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-[(1R)-2-hydroxy-1-methylethyl]-5-methyl-N',N'-dipropylacetamide
1027N-[(2R,3S)-3-Amino-2-hydroxy-4-(3-were)butyl]-N-benzyl-5-methyl-N',N'-dipropylacetamide
1029N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-N'-pyridine-3-illintentioned
1031(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-2-methyl-4-oxo-4H-chromen-6-carboxylate
10332-({2-[[(2R,3S)-3-Amino-4-(3,5-debtor the Nile)-2-hydroxybutyl](3-active compounds)amino]-2-oxoethyl}thio)-N-(5-methylisoxazol-3-yl)ndimethylacetamide
1035N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-[3-(1H-imidazol-1-yl)propyl]-5-methyl-N',N'-dipropylacetamide
1037N-{(2R,3S)-3-Amino-4-[3-fluoro-5-(trifluoromethyl)phenyl]-2-hydroxybutyl}-3-[(dipropylamino)sulfonyl]-N-(3-methoxybenzyl)propanamide
1039N-[(2R,3S)-3-Amino-2-hydroxy-4-(4-hydroxyphenyl)butyl]-3-[(dipropylamino)sulfonyl]-N-(3-methylbutyl)propanamide
1041N-[(2R,3S)-3-Amino-4-(1,3-benzodioxol-5-yl)-2-hydroxybutyl]-5-methyl-N-(3-methylbutyl)-N',N'-dipropylacetamide
1043N-[(2R,3S)-3-Amino-2-hydroxy-4-(2-thienyl)butyl]-3-[(dipropylamino)sulfonyl]-N-(3-methylbutyl)propanamide
1045N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-4-[(2,2-dimethylpropanoyl)amino]-N-(3-active compounds)-2-hydroxybenzamide
1047N-[(2R,3S)-3-Amino-2-hydroxy-4-(3-methoxyphenyl)butyl]-5-methyl-N-(3-methylbutyl)-N',N'-dipropylacetamide
1049-[(2R,3S)-3-Amino-4-(4-forfinal)-2-hydroxybutyl]-3-{[(3-methoxybenzyl)amino]sulfonyl}-N-[3-(trifluoromethyl)benzyl]benzamide
1051N-{(2R,3S)-3-Amino-2-hydroxy-4-[3-(trifluoromethyl)phenyl]butyl}-5-methyl-N-(3-methylbutyl)-N',N'-dipropylacetamide
1053N-{6-[[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl](3-active compounds)amino]-6-oxohexyl}-2-furamide
1055N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-2-[(1-phenyl-4,5-dihydro-1H-tetrazol-5-yl)thio]ndimethylacetamide
1057N-[(2S,3S)-3-Amino-2-hydroxy-4-phenylbutyl]-3-{[(3-methoxybenzyl)amino]sulfonyl}-N-[3-(trifluoromethyl)benzyl]benzamide
1059N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-4-(3,4-dihydro-2H-chromen-6-yl)-N-(3-active compounds)-4-oxobutanamide
1061N1-[(2R,3S)-3-Amino-2-hydroxy-4-(3-methoxyphenyl)butyl]-N1-(3-methylbutyl)-N3N3-DIPROPYLENE-1,3,5-tricarboxylic
1063N-[(2R,3S)-3-Amino-4-(3-fluoro-4-were)-2-hydroxybutyl]-N-(3-methoxybenzyl)-N',N'-dipropylenetriamine
1065 N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)indolizine-2-carboxamide
1067N-{(2R,3S)-3-Amino-2-hydroxy-4-[3-(triptoreline)phenyl]butyl}-N-benzyl-5-methyl-N',N'-dipropylacetamide
10691-Oxide N-[(2R,3S)-3-amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)nicotinamide
1071N-{(2R,3S)-3-Amino-4-[3-(benzyloxy)-5-forfinal]-2-hydroxybutyl}-3-[(dipropylamino)sulfonyl]-N-(3-methylbutyl)propanamide
10732-[[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl](3-iodobenzyl)amino]-2-oxoethylidene
1075N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-2,3-dihydro-1H-cyclopent[b]quinoline-9-carboxamide
1077N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-3-methyl-1H-pyrazole-5-carboxamide
1079N-{5-[[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl](3-active compounds)amino]-5-oxopent}benzamide
1081 N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-4-[(methoxymethyl)thio]benzamide
1083N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-3-(1,3-benzothiazol-2-yl)-N-(3-active compounds)-3-methoxypropane
1085N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-3-{[(methylamino)carbonyl]amino}-3-(3-thienyl)propanamide
1087N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-5-pyridin-2-althofen-2-carboxamide
1089N1-{(2R,3S)-3-Amino-4-[3-(benzyloxy)-5-forfinal]-2-hydroxybutyl}-N1-benzyl-N3N3-DIPROPYLENE-1,3,5-tricarboxylic
1091N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-2-(5,6-dimethyl-2,4-dioxo-1,2,3,4-tetrahydropyridine-3-yl)-N-(3-active compounds)ndimethylacetamide
1093N-[(2R,3S)-3-Amino-4-(3-fluoro-4-methoxyphenyl)-2-hydroxybutyl]-5-methyl-N-(3-methylbutyl)-N',N'-dipropylacetamide
1095N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydro is libutil]-N-(3-active compounds)-2-isobutyl-1,3-doxasozin-5-carboxamid
10975-(Acetylamino)-N-[(2R,3S)-3-amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-2-furamide
1099N1-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N1-(3-active compounds)-N2-[(4-methoxyphenyl)acetyl]glycinamide
1101N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)isoquinoline-4-carboxamid
1103N1-{(2R,3S)-3-Amino-4-[3-(benzyloxy)phenyl]-2-hydroxybutyl}-N1-(3-methylbutyl)-N3N3-DIPROPYLENE-1,3,5-tricarboxylic
1105N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-2-(4-hydroxy-3-methoxyphenyl)ndimethylacetamide
1107N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-2-[(4-phenyl-4H-1,2,4-triazole-3-yl)thio]ndimethylacetamide
1109N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-2-(3,5-acid)-N-(3-active compounds)ndimethylacetamide
1111N-[(R,3S)-3-Amino-2-hydroxy-4-(3-methoxyphenyl)butyl]-N-benzyl-5-methyl-N',N'-dipropylacetamide
1113N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-2-(2-ethyl-4H-[1,2,4]triazolo[1,5-a]benzimidazole-4-yl)ndimethylacetamide
1115N-[(2R,3S)-3-Amino-4-(2-furyl)-2-hydroxybutyl]-N-benzyl-5-methyl-N',N'-dipropylacetamide
1117N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-7-chloro-N-(3-active compounds)-1-benzofuran-2-carboxamide
1119N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-2-(1,3-dioxo-1,3-dihydro-2H-isoindole-2-yl)-N-(3-active compounds)propanamide
1121N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-3-(2-oxo-2H-1,3-benzoxazin-3(4H)-yl)propanamide
1123N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-2-(pyrimidine-2-ylthio)ndimethylacetamide
1125N'-[3-(Aminocarbonyl)-4,5,6,7-tetrahydro-1-benzothieno-2-yl]-N-[(2R,3S)-3-amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)succinamic
1127N-[(2,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-2-[(5-phenyl-1,3,4-oxadiazol-2-yl)thio]ndimethylacetamide
1129N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)quinoline-6-carboxamide
1131N1-[(2R,3S)-3-Amino-4-(2-furyl)-2-hydroxybutyl]-N1-benzyl-N3N3-DIPROPYLENE-1,3,5-tricarboxylic
1133N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-4-(2,3-dihydro-1,4-benzodioxin-6-yl)-N-(3-active compounds)-4-oxobutanamide
1135N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-3-(1H-indol-3-yl)-1H-pyrazole-5-carboxamide
1137N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-2-hydroxy-4-{[(methylamino)carbonothioyl]amino}benzo-amide
1139N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-6-chloro-N-(3-active compounds)nick is tinamed
1141N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-4-(3-hydroxyphenyl)-4-oxobutanamide
1143N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-2-(phthalazine-1 ylthio)ndimethylacetamide
1145N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-2-[(1-oxidability-2-yl)thio]ndimethylacetamide
11473-(Acetylamino)-N-[(2R,3S)-3-amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-5-fluoro-1H-indole-2-carboxamide
1149N-[(2R,3S)-3-Amino-2-hydroxy-4-phenylbutyl]-3-{[(3-Chlorobenzyl)amino]sulfonyl}-N-[3-(trifluoromethyl)benzyl]benzamide
1151N1-{(2R,3S)-3-Amino-4-[4-(benzyloxy)phenyl]-2-hydroxybutyl}-N1-(3-methoxybenzyl)-N3N3-DIPROPYLENE-1,3,5-tricarboxylic
1153N1-[(2R,3S)-3-Amino-4-(1,3-benzodioxol-5-yl)-2-hydroxybutyl]-N1-benzyl-N3N3-DIPROPYLENE-1,3,5-tricarboxylic
1155N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-4-(3,4-dichlorophenyl)-N-(3-active compounds)-2-hydroxy-3-methyl-4-oxobutanamide
1157N-{(2R,3S)-3-Amino-2-hydroxy-4-[3-(triptoreline)phenyl]butyl}-3-[(dipropylamino)sulfonyl]-N-(3-methylbutyl)propanamide
1159N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-N'-(5-methyl-1,3,4-thiadiazole-2-yl)succinamic
1161N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-2-(2-ethyl-1H-benzimidazole-1-yl)-N-(3-active compounds)ndimethylacetamide
1163N-[(2R,3S)-3-Amino-4-(1,3-benzodioxol-5-yl)-2-hydroxybutyl]-3-[(dipropylamino)sulfonyl]-N-(3-methoxybenzyl)propanamide
1165N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-3-(2-oxo-1,3-benzoxazol-3(2H)-yl)propanamide
1167 N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-3-[(dipropylamino)sulfonyl]-N-(3-methylbutyl)propanamide
1169N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-N'-(6-methylpyridin-2-yl)succinamic
1171Ethyl-(4R)-4-{[[(2R,3S)-3-amino-4-(3,5-differenl)-2-hydroxybutyl](3-active compounds)amino]carbonyl}-1,3-oxazolidin-3-carboxylate
1172(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-(butylsulfonyl)-N-(methoxycarbonyl-D-alaninate
1174(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-S-butyl-N-(methoxycarbonyl-D-cysteinate
1176(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-N-[(benzyloxy)carbonyl]-3-[(4,4,4-trifloromethyl)sulfonyl]-D-alaninate
1178(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-N-[(benzyloxy)carbonyl]-3-[(4,4,4-trifloromethyl)sulfinil]-D-alaninate
1180(1R,2S)-2-Amino-3-(3,5-dif is arvanil)-1-{[(3-active compounds)amino]methyl}propyl-N-[(benzyloxy)carbonyl]-S-[(4,4,4-trifloromethyl)-D-cysteinate
1182(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-(butylsulfonyl)-N-(methoxycarbonyl)-D-alaninate
1184(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-(butylsulfonyl)-N-[(2,2,2-triptoreline)carbonyl]-D-alaninate
1186(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-(butylsulfonyl)-N-[(2-cyanoethoxy)carbonyl]-D-alaninate
1188(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-(butylsulfonyl)-N-{[(3R)-pyrrolidin-3-yloxy]carbonyl}-D-alanine
1190(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-(butylsulfonyl)-N-{[(3S)-tetrahydrofuran-3-yloxy]carbonyl}-D-alanine
1192(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-N-{[(2-acetylamino)ethoxy]carbonyl}-3-(butylsulfonyl)-D-alaninate
1194(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}about the Il-3-(butylsulfonyl)-N-[(pyridine-3-ylethoxy)carbonyl]-D-alaninate
1196(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-(butylsulfonyl)-N-[(pyridine-4-ylethoxy)carbonyl]-D-alaninate
1198(1R,2S)-2-Amino-1-[(cyclopropylamino)methyl]-3-(3,5-differenl)propyl-3-(butylsulfonyl)-N-(methoxycarbonyl)-D-alaninate
1200(1R,2S)-2-Amino-1-[(cyclopropylamino)methyl]-3-(3,5-differenl)propyl-3-(butylsulfonyl)-N-[(2-cyanoethoxy)carbonyl]-D-alaninate
1202(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-methylbutyl)amino]methyl}propyl-N-[(benzyloxy)carbonyl]-3-(butylsulfonyl)-D-alaninate
1204(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-methylbutyl)amino]methyl}propyl-3-(butylsulfonyl)-N-(methoxycarbonyl)-D-alaninate
1206(1R,2S)-2-Amino-1-[(cyclopropylamino)methyl]-3-(3,5-differenl)propyl-N-[(2-cyanoethoxy)carbonyl]-3-[(1-propinball)sulfonyl]-D-alaninate
1208(1R,2S)-2-Amino-1-[(cyclopropylamino)methyl]-3-(3,5-differenl)propyl-N-{[2-(acetylamino)ethoxy]carbon is l}-3-[(1-propinball)sulfonyl]-D-alaninate
1210(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-methylbutyl)amino]methyl}propyl-N-(methoxycarbonyl)-3-[(1-propinball)sulfonyl]-D-alaninate
1212(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-methylbutyl)amino]methyl}propyl-N-[(benzyloxy)carbonyl]-3-[(1-propinball)sulfonyl]-D-alaninate
1214(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-N-{[2-(diethylamino)-2-oksidoksi]carbonyl}-3-[(1-propinball)sulfonyl]-D-alaninate
1216(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-N-(methoxycarbonyl)-3-[(1-propinball)sulfonyl]-D-alaninate
1218(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-N-(isopropoxycarbonyl)-3-[(1-propinball)sulfonyl]-D-alaninate
1220(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-N-[(cyclopropylmethoxy)carbonyl]-3-[(1-propinball)sulfonyl]-D-alaninate
1222(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-what tenbensel)amino]methyl}propyl-N-[(allyloxy)carbonyl]-3-[(1-propinball)sulfonyl]-D-alaninate
1224(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-N-[(2-cyanoethoxy)carbonyl]-3-[(1-propinball)sulfonyl]-D-alaninate
1226(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-N-{[2-(acetylamino)ethoxy]carbonyl}-3-[(1-propinball)sulfonyl]-D-alaninate
1228(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-[(1-propinball)sulfonyl]-N-[(pyridine-3-ylethoxy)carbonyl]-D-alaninate
1230(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-[(1-propinball)sulfonyl]-N-[(pyridine-4-ylethoxy)carbonyl]-D-alaninate
1232(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-(2R)-2-{[(benzyloxy)carbonyl]amino}-4-(methylsulphonyl)butanoate
1234(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-N-[(benzyloxy)carbonyl]-3-(butylsulfonyl)-D-alaninate
1236(1R,2S)-2-Amino-3-(3,5-differenl)-1-{(3-active compounds)amino]methyl}propyl-N-[(benzyloxy)carbonyl]-3-(butylsulfonyl)-L-alaninate
1238(1R,2S)-2-Amino-3-(3,5-differenl)-1-({[(1R)-2-hydroxy-1-phenylethyl]amino}methyl)propyl-N-[(benzyloxy)carbonyl]-3-[(1-propinball)sulfonyl]-D-alaninate
1240(1R,2S)-2-Amino-3-(3,5-differenl)-1-({[(1R)-2-methoxy-1-phenylethyl]amino}methyl)propyl-N-[(benzyloxy)carbonyl]-3-[(1-propinball)sulfonyl]-D-alaninate
1242(1R,2S)-2-Amino-3-(3,5-differenl)-1-({[(1S)-2-methoxy-1-phenylethyl]amino}methyl)propyl-N-[(benzyloxy)carbonyl]-3-[(1-propinball)sulfonyl]-D-alaninate
1244(1R,2S)-2-Amino-3-(3,5-differenl)-1-({[1-(3-ethylphenyl)cyclopropyl]amino}methyl)propyl-N-[(benzyloxy)carbonyl]-3-[(1-propinball)sulfonyl]-D-alaninate
1246(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-[(1-propinball)sulfonyl]-N-[(prop-2-in-1 yloxy)carbonyl]-D-alaninate
1248(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-N-[(2-methoxyethoxy)carbonyl]-3-[(1-propinball)sulfonyl]-D-alaninate
12501252(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-[(1-propinball)sulfonyl]-N-{[(3S)-tetrahydrofuran-3-yloxy]carbonyl}-D-alanine
1254(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-[(1-propinball)sulfonyl]-N-{[(3S)-tetrahydrofuran-3-yloxy]carbonyl}-L-alaninate
1256(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-N-[(benzyloxy)carbonyl]-3-[(1-propinball)sulfonyl]-D-alaninate
1258(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-N-[(benzyloxy)carbonyl]-3-[(1-propinball)sulfonyl]-L-alaninate
1260(1R,2S)-2-Amino-3-(3,5-differenl)-1-({[1-(3-ethylphenyl)cyclopropyl]amino}methyl)propyl-N-[(benzyloxy)carbonyl]-3-[(1-propinball)sulfonyl]alanine
1262(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}p the sawdust-N-[(benzyloxy)carbonyl]-3-[(1-propinball)sulfonyl]alanine
1264(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-methylbutyl)amino]methyl}propyl-N-[(benzyloxy)carbonyl]-3-[(1-propinball)sulfonyl]alanine
1266(1R,2S)-2-Amino-1-[(cyclopropylamino)methyl]-3-(3,5-differenl)propyl-N-[(benzyloxy)carbonyl]-3-[(1-propinball)sulfonyl]alanine
1268(1R,2S)-2-Amino-1-{[(cyclopropylmethyl)amino]methyl}-3-(3,5-differenl)propyl-N-[(benzyloxy)carbonyl]-3-[(1-propinball)sulfonyl]alanine
1270(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-ethylphenyl)amino]methyl}propyl-N-[(benzyloxy)carbonyl]-3-[(1-propinball)sulfonyl]alanine
1272(1R,2S)-2-Amino-3-(3,5-differenl)-1-[({2-[3-(trifluoromethyl)phenyl]amino)ethyl]propyl-N-[(benzyloxy)carbonyl]-3-[(1-propinball)sulfonyl]alanine
1274(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-[(1-propinball)sulfonyl]-N-[(pyridine-3-ylethoxy)carbonyl]alaninate
1276(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-Ativ nil)amino]methyl}propyl-3-[(1-propinball)sulfonyl]-N-{[(3S)-tetrahydrofuran-3-yloxy]carbonyl}alaninate
1278(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-[(1-propinball)sulfonyl]-N-{[(3R)-tetrahydrofuran-3-yloxy]carbonyl}alaninate
1280(1R,2S)-2-Amino-1-{[(3-methoxybenzyl)amino]methyl}-3-phenylpropyl-3-[(1-propinball)sulfonyl]-N-{[(3S)-tetrahydrofuran-3-yloxy]carbonyl}alaninate
1282(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-N-({[(3R)-1-acetylpyrrolidine-3-yl]oxy}carbonyl)-3-[(1-propinball)sulfonyl]alanine
1284(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-[(1-propinball)sulfonyl]-N-{[(3R)-pyrrolidin-3-yloxy]carbonyl}alaninate
1286(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-N-({[(3R)-1-benzylpyrrolidine-3-yl]oxy}carbonyl)-3-[(1-propinball)sulfonyl]alanine
1288(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-N-({[(3R)-1,1-dissidocerida-3-thienyl]oxy}carbonyl)-3-[(1-propinball)sulfonyl]alanine
1290(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-[(1-propinball)sulfonyl]-N-{[(3R)-tetrahydro-3-titilate]carbonyl}alaninate
1292(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-N-[(cyclopentyloxy)carbonyl]-3-[(1-propinball)sulfonyl]alanine
1294(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-N-[(cyclohexyloxy)carbonyl]-3-[(1-propinball)sulfonyl]alanine
1296(1R,2S)-2-Amino-1-[(cyclopropylamino)methyl]-3-(3,5-differenl)propyl-3-[(1-propinball)sulfonyl]-N-[(tetrahydro-2H-Piran-4-yloxy)carbonyl]alaninate
1298
1300(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-N-({[1-(methylsulphonyl)piperidine-4-yl]oxy}carbonyl)-3-[(1-propinball)sulfonyl]alanine
1302 (1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-N-{[(1-acetylpiperidine-4-yl)oxy]carbonyl}-3-[(1-propinball)sulfonyl]alanine
1304(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-N-({[(2R)-5-oxopyrrolidin-2-yl]methoxy}carbonyl)-3-[(1-propinball)sulfonyl]alanine
1306(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-N-({[(2S)-5-oxopyrrolidin-2-yl]methoxy}carbonyl)-3-[(1-propinball)sulfonyl]alanine
1308(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-N-[(2-methoxyethoxy)carbonyl]-3-[(1-propinball)sulfonyl]alanine
1310(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-N-[(benzyloxy)carbonyl]-3-(butylsulfonyl)alaninate
1312(1R,2S)-2-Amino-1-{[(3-methoxybenzyl)amino]methyl}-3-phenylpropyl--[(benzyloxy)carbonyl]-3-[(1-propinball)sulfonyl]alanine
1314The hydrochloride of N-{(1S,2R)-1-benzyl-2-hydroxy-3-[(3-methoxybenzyl)amino]propyl}-2-hydroxy-4-(phenylsulfonyl)butanamide
1316(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-N2-[(benzyloxy)carbonyl]-N5N5-dipropyl-L-glutamine
1318(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-N2-[(benzyloxy)carbonyl]-N5N5-dipropyl-D-glutamine
1320(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-(butylsulfonyl)-N-(3,3,3-tryptophanyl)-D-alaninate
1322(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-(butylsulfonyl)-N-(TRIFLUOROACETYL)-D-alaninate
1324(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-N-acetyl-3-(butylsulfonyl)-D-alaninate
1326(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-(butylsulfonyl)-N-sonicate the oil-D-alaninate
1328(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-(butylsulfonyl)-N-(cyclopropanecarbonyl)-D-alaninate
1330(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-β-alanyl-3-(butylsulfonyl)-D-alaninate
1332(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propylphenyl-3-(butylsulfonyl)-D-alaninate
1334(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-N,N-dimethylglycine-3-(butylsulfonyl)-D-alaninate
1336(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-N,N-dimethyl-β-alanyl-3-(butylsulfonyl)-D-alaninate
1338(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-(butylsulfonyl)-N-(methoxyacetyl)-D-alaninate
1340(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-(butylsulfonyl)-N-(pyridine-3-ylcarbonyl)-D-alaninate
1342 (1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-(butylsulfonyl)-N-[(2,4-dimethyl-1,3-thiazol-5-yl)carbonyl]-D-alaninate
1344(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-(butylsulfonyl)-N-{[3-(trifluoromethyl)-1H-pyrazole-4-yl]carbonyl}-D-alanine
1346(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-(butylsulfonyl)-N-[(3-methyl-1H-pyrazole-5-yl)carbonyl]-D-alaninate
1348(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-(butylsulfonyl)-N-(1H-imidazol-4-ylcarbonyl)-D-alaninate
1350(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-(2R)-5-hydroxy-2-[(methoxycarbonyl)amino]nonanoate
1352(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-(butylsulfonyl)-N-[(6-hydroxypyridine-3-yl)carbonyl]-D-alaninate
1354(1R,2S)-2-Amino-1-[(cyclopropylamino)methyl]-3-(3,5-differenl)propyl-3-(butylsulfonyl)-N-(pyridi the-3-ylcarbonyl)-D-alaninate
1356(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-methylbutyl)amino]methyl}propyl-N-acetyl-3-(butylsulfonyl)-D-alaninate
1358(1R,2S)-2-Amino-1-[(cyclopropylamino)methyl]-3-(3,5-differenl)propyl-N-(cyclopropanecarbonyl)-3-[(1-propinball)sulfonyl]-D-alaninate
1360(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-methylbutyl)amino]methyl}propyl-N-acetyl-3-[(1-propinball)sulfonyl]-D-alaninate
1362(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-N-isonicotinoyl-3-[(1-propinball)sulfonyl]-D-alaninate
1364(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-N-[(5-bromopyridin-3-yl)carbonyl]-3-[(1-propinball)sulfonyl]-D-alaninate
1366(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-N-[(5-chloropyridin-3-yl)carbonyl]-3-[(1-propinball)sulfonyl]-D-alaninate
1368(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-N-(3-perbenzoic)-3-[(1-PR is pivotal)sulfonyl]-D-alaninate
1370(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-N-[(5-methylpyridin-3-yl)carbonyl]-3-[(1-propinball)sulfonyl]-D-alaninate
1372(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-N-phenylglycyl-3-[(1-propinball)sulfonyl]-D-alaninate
1374(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-[(1-propinball)sulfonyl]-N-{[3-(trifluoromethyl)-1H-pyrazole-4-yl]carbonyl}-D-alanine
1376(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-N-[(3-methyl-1H-pyrazole-5-yl)carbonyl]-3-[(1-propinball)sulfonyl]-D-alaninate
1378(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-[(1-propinball)sulfonyl]-N-(1,3-thiazol-4-ylcarbonyl)-D-alaninate
1380(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-N-[(1-acetylpiperidine-4-yl)carbonyl]-3-[(1-propinball)sulfonyl]-D-alaninate
1382(1R,2S)-2-Amino-3(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-N-[4-(acetylamino)butanoyl]-3-[(1-propinball)sulfonyl]-D-alaninate
1384(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-N-acetyl-β-alanyl-3-[(1-propinball)sulfonyl]-D-alaninate
1386(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-N-(chloroacetyl)-3-[(1-propinball)sulfonyl]-D-alaninate
1388(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-N-(methoxyacetyl)-3-[(1-propinball)sulfonyl]-D-alaninate
1390(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-N-(methoxypropanol)-3-[(1-propinball)sulfonyl]-D-alaninate
1392(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-N-(2,2-dimethylpropanoyl)-3-[(1-propinball)sulfonyl]-D-alaninate
1394(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-N-isobutyryl-3-[(1-propinball)sulfonyl]-D-alaninate
1396(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-N-butyryl-3-[(1-propylate is)sulfonyl]-D-alaninate
1398(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-N-acetyl-3-[(1-propinball)sulfonyl]-D-alaninate
1400(1R,2S)-2-Amino-3-(3,5-differenl)-1-({[1-(3-ethylphenyl)cyclopropyl]amino}methyl)propyl-3-[(1-propinball)sulfonyl]-N-(pyridine-3-ylcarbonyl)-D-alaninate
1402(1R,2S)-2-Amino-3-(3,5-differenl)-1-({[1-(3-ethylphenyl)cyclopropyl]amino}methyl)propyl-N-isonicotinoyl-3-[(1-propinball)sulfonyl]-D-alaninate
1404(1R,2S)-2-Amino-3-(3,5-differenl)-1-({[1-(3-ethylphenyl)cyclopropyl]amino}methyl)propyl-N-(3-hydroxybenzoyl)-3-[(1-propinball)sulfonyl]-D-alaninate
1406(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-[(1-propinball)sulfonyl]-N-(pyridine-3-ylcarbonyl)-D-alaninate
1408(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-N-(3-hydroxybenzoyl)-3-[(1-propinball)sulfonyl]-D-alaninate
1410(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-ativan who yl)amino]methyl}propyl-N-(cyclopropanecarbonyl)-3-[(1-propinball)sulfonyl]-D-alaninate
1412(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-N-propionyl 3-[(1-propinball)sulfonyl]-D-alaninate
1414(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-(butylsulfonyl)-N-(pyridine-3-ylcarbonyl)alaninate
1416(1R,2S)-2-Amino-3-(3,5-differenl)-1-({[1-(3-ethylphenyl)cyclopropyl]amino}methyl)propyl-N-(3-hydroxybenzoyl)-3-[(1-propinball)sulfonyl]alanine
1418(1R,2S)-2-Amino-3-(3,5-differenl)-1-({[1-(3-ethylphenyl)cyclopropyl]amino}methyl)propyl-N-isonicotinoyl-3-[(1-propinball)sulfonyl]alanine
1420(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-N-[(6-oxo-1,4,5,6-tetrahydropyrimidin-3-yl)carbonyl]-3-[(1-propinball)sulfonyl]alanine
1422Hydrochloride (1R,2S)-2-amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-5-oxo-D-prolyl-3-[(1-propinball)sulfonyl]alaninate
1424(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-this is benzil)amino]methyl}propyl-5-oxo-L-prolyl-3-[(1-propinball)sulfonyl]alanine
1426(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-N-[3-(4-oxo-2-thioxo-1,3-thiazolidin-3-yl)propanol]-3-[(1-propinball)sulfonyl]alanine
1428(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-N-(piperidine-4-ylcarbonyl)-3-[(1-propinball)sulfonyl]alanine
1430(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-N-[(2,4-dimethyl-1,3-thiazol-5-yl)carbonyl]-3-[(1-propinball)sulfonyl]alanine
1432(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-N-{[2-methyl-4-(trifluoromethyl)-1,3-thiazol-5-yl]carbonyl}-3-[(1-propinball)sulfonyl]alanine
1434(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-N-[(3,5-dimethylisoxazol-4-yl)carbonyl]-3-[(1-propinball)sulfonyl]alanine
1436(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-N-[(3-methyl-1H-pyrazole-5-yl)carbonyl]-3-[(1-propinball)sulfonyl]alanine
1438 (1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-[(1-propinball)sulfonyl]-N-(1H-pyrazole-4-ylcarbonyl)alaninate
1440(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-N-(1H-imidazol-5-ylcarbonyl)-3-[(1-propinball)sulfonyl]alanine
1442(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-N-(1H-imidazol-4-ylacetic)-3-[(1-propinball)sulfonyl]alanine
1444(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-[(1-propinball)sulfonyl]-N-(pyrazin-2-ylcarbonyl)alaninate
1446(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-N-(2,6-dihydroxyethylene)-3-[(1-propinball)sulfonyl]alanine
1448(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-N-[(6-hydroxypyridine-3-yl)carbonyl]-3-[(1-propinball)sulfonyl]alanine
1450(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-N-[(6-chloropyridin-3-yl)carbonyl]-3-[(1-propinball)with Lionel]alaninate
1452(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-N-isonicotinoyl-3-[(1-propinball)sulfonyl]alanine
1454(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-[(1-propinball)sulfonyl]-N-(pyridine-3-ylcarbonyl)alaninate
1456(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-[(1-propinball)sulfonyl]-N-(pyridine-2-ylcarbonyl)alaninate
1458Hydrochloride (1R,2S)-2-amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-N-(1H-indol-6-ylcarbonyl)-3-[(1-propinball)sulfonyl]alaninate
1460(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-[(1-propinball)sulfonyl]-N-(3,4,5-trimethoxybenzoyl)alaninate
1462(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-N-(2-methylbenzoyl)-3-[(1-propinball)sulfonyl]alanine
1464(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}about the Il-N-(3-hydroxybenzoyl)-3-[(1-propinball)sulfonyl]alanine
1466(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-N-(3-methylbenzoyl)-3-[(1-propinball)sulfonyl]alanine
1468(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-N-(3-ethylbenzoyl)-3-[(1-propinball)sulfonyl]alanine
1470(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-N-(3-chlorobenzoyl)-3-[(1-propinball)sulfonyl]alanine
1472(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-[(1-propinball)sulfonyl]-N-[4-(trifluoromethyl)benzoyl]alanine
1474(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-N-(4-methoxybenzoyl)-3-[(1-propinball)sulfonyl]alanine
1476(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-[(1-propinball)sulfonyl]-N-[4-(trifluoromethyl)benzoyl]alanine
1478(1R,2S)-2-Amino-3-(3,5-deltorphin the l)-1-{[(3-active compounds)amino]methyl}propyl-N-(cyclohexylcarbonyl)-3-[(1-propinball)sulfonyl]alanine
1480(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-N-benzoyl-3-[(1-propinball)sulfonyl]alanine
1482(1R,2S)-2-Amino-1-[(cyclopropylamino)methyl]-3-(3,5-differenl)propyl-N-benzoyl-3-[(1-propinball)sulfonyl]alanine
1484(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-N-(phenylacetyl)-3-[(1-propinball)sulfonyl]alanine
1486(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-N-(3-phenylpropenoyl)-3-[(1-propinball)sulfonyl]alanine
1488(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-(benzoylamine)-2-{[(1-propinball)sulfonyl]methyl}propanoic
1490 (1R,2S)-2-Amino-1-{[(3-methoxybenzyl)amino]methyl}-3-phenylpropyl-N-(cyclopropylmethyl)-3-[(1-propinball)sulfonyl]alanine
1492(1R,2S)-2-Amino-1-{[(3-methoxybenzyl)amino]methyl}-3-phenylpropyl-N-[(methylsulphonyl)acetyl]-3-[(1-propinball)sulfonyl]alanine
1494(1R,2S)-2-Amino-1-{[(3-methoxybenzyl)amino]methyl}-3-phenylpropyl-N-[(methylthio)acetyl]-3-[(1-propinball)sulfonyl]alanine
1496
1498(1R,2S)-2-Amino-1-{[(3-methoxybenzyl)amino]methyl}-3-phenylpropyl-N-[4-(methylamino)-4-oxobutanoic]-3-[(1-propinball)sulfonyl]alanine
1500
1502(1R,2S)-2-Amino-1-{[(3-methoxybenzyl)amino]methyl}-3-phenylpropyl-N-(methylsulphonyl)glycyl-3-[(1-propinball)sulfonyl]alanine
1504(1R,2S)-2-Amino-1-{[(3-methoxybenzyl)amino]methyl}-3-phenylpropyl-N-acetyl-3-(phenylsulfonyl)alaninate
1506(1R,2S)-2-Amino-1-{[(3-methoxybenzyl)amino]methyl}-3-phenylpropyl-(2S)-2-[(4-methoxy-4-oxobutanoic)amino]-5-oxo-5-piperidine-1-repentant
1508(1R,2S)-2-Amino-1-{[(3-methoxybenzyl)amino]methyl}-3-phenylpropyl-(2R)-2-{[(benzyloxy)carbonyl]amino}-5-oxo-5-piperidine-1-repentant
1510(1R,2S)-2-Amino-1-{[(3-methoxybenzyl)amino]methyl}-3-phenylpropyl-(2R)-2-[(3-ethoxy-3-oxopropanoic)amino]-5-oxo-5-piperidine-1-repentant
1512(1R,2S)-2-Amino-1-{[(3-methoxybenzyl)amino]methyl}-3-phenylpropyl-N2-(4-methoxy-4-oxobutanoic)-N5N5-dipropyl-D-glutamine
1514(1R,2S)-2-Amino-1-{[(3-methoxybenzyl)amino]methyl}-3-phenylpropyl-(2R)-2-[(4-methoxy-4-oxobutanoic)amino]-5-oxo-5-piperidine-1-repentant
1516(1R,2S)-2-Amino-1-{[(3-methoxybenzyl)amino]methyl}-3-phenylpropyl-(2R)-2-[(5-methoxy-5-oxapentane the l)amino]-5-oxo-5-piperidine-1-repentant
1518(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-2-(atomic charges)-3-(butylsulfonyl)propanoate
1520(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-S-butyl-D-cysteinate
1522(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-(butylsulfonyl)-D-alaninate
1524(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-(butylsulfonyl)-D-alaninate
1526(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-(butylsulfonyl)-L-alaninate
1528(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-methylbutyl)amino]methyl}propyl-3-(butylsulfonyl)-D-alaninate
1530(1R,2S)-2-Amino-3-(3,5-differenl)-1-({[1-(3-ethylphenyl)cyclopropyl]amino}methyl)propyl-3-[(1-propinball)sulfonyl]-D-alaninate
1532(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]m is Teal}propyl-3-[(1-propinball)sulfonyl]-L-alaninate
1534(1R,2S)-2-Amino-1-[(cyclopropylamino)methyl]-3-(3,5-differenl)propyl-3-[(1-propinball)sulfonyl]-D-alaninate
1536(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-methylbutyl)amino]methyl}propyl-3-[(1-propinball)sulfonyl]-D-alaninate
1538(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-[(1-propinball)sulfonyl]-D-alaninate
1540(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-[(1-propinball)sulfonyl]alanine
1542(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-N-(phenoxyacetyl)-3-[(1-propinball)sulfonyl]alanine
1544(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-N-{[(5-chloro-2-thienyl)thio]peroxy}-3-[(1-propinball)sulfonyl]alanine
1546(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-N-(phenylsulfonyl)-3-[(1-propinball)sulfonyl]alanine
548 (1R,2S)-3-(3,5-Differenl)-1-{[(3-active compounds)amino]methyl}-2-(methylamino)propyl-N-[(benzylamino)carbonyl]-3-[(1-propinball)sulfonyl]alanine
15504-{[(1R,2S)-3-(3,5-Differenl)-1-{[(3-active compounds)amino]methyl}-2-(methylamino)propyl]oxy}-4-oxo-3-{[(1-propinball)sulfonyl]methyl}butane acid
15524-[(1R,2S)-2-Amino-1-{[(3-methoxybenzyl)amino]methyl}-3-phenylpropyl)oxy]-3-{[(3-methylbutyl)sulfonyl]methyl}-4-oxobutanoic acid
15541-((1R,2S)-2-Amino-1-{[(3-methoxybenzyl)amino]methyl}-3-phenylpropyl)-4-methyl-2-{[(3-methylbutyl)sulfonyl]methyl}succinate
1556(1R,2S)-2-Amino-1-{[(3-methoxybenzyl)amino]methyl}-3-phenylpropyl-4-amino-2-{[(3-methylbutyl)sulfonyl]methyl}-4-oxobutanoate
1558(1R,2S)-2-Amino-1-{[(3-methoxybenzyl)amino]methyl}-3-phenylpropyl-4-(methylamino)-2-{[(3-methylbutyl)sulfonyl]methyl}-4-oxobutanoate
1560(1R,2S)-2-Amino-1-{[(3-methoxybenzyl)amino]methyl}-3-phenylpropyl-4-(dimethylamino)-2-{[(3-methylbutyl)sulfonyl]methyl}-4-OK who butanoate
1562(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-(4,4-dimethyl-2,5-dioxoimidazolidin-1-yl)-2-{[(1-propinball)sulfonyl]methyl}propanoic
1564(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-(4,4-dimethyl-2,5-dioxoimidazolidin-1-yl)-2-{[(1-propinball)sulfonyl]methyl}propanoic
1566(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-(4,4-dimethyl-2,5-dioxoimidazolidin-1-yl)-2-{[(1-propinball)sulfonyl]methyl}propanoic
1568(1R,2R)-2-Amino-1-{[(3-methoxybenzyl)amino]methyl}-3-phenylpropyl-3-(ethylsulfonyl)-2-{[(isobutylphenyl)amino]methyl}propanoic
1570(1R,2S)-2-Amino-1-{[(3-methoxybenzyl)amino]methyl}-3-phenylpropyl-3-(ethylthio)-2-{[(isobutylphenyl)amino]methyl}propanoic
1572(1R,2S)-2-Amino-1-{[(3-methoxybenzyl)amino]methyl}-3-phenylpropyl-(2S)-2-{[(3-methylbutyl)sulfonyl]amino}-4-(methylsulphonyl)butanoate
1574(1R,2S)-2-AMI is about-1-{[(3-methoxybenzyl)amino]methyl}-3-phenylpropyl-N-[(3-methylbutyl)sulfonyl]-L-methionine
1576(1R,2S)-2-Amino-1-{[(3-methoxybenzyl)amino]methyl}-3-phenylpropyl-3-(acetylthio)-2-{[(3-methylbutyl)sulfonyl]methyl}propanoic
1578(1R,2S)-2-Amino-1-{[(3-methoxybenzyl)amino]methyl}-3-phenylpropyl-2-hydroxy-3-[(1-propinball)sulfonyl]propanoic
1580(1R,2S)-2-Amino-1-{[(3-methoxybenzyl)amino]methyl}-3-phenylpropyl-2-hydroxy-3-[(3-methylbutyl)sulfonyl]propanoic
1582(1R,2S)-2-Amino-1-{[(3-methoxybenzyl)amino]methyl}-3-phenylpropyl-2-hydroxy-3-[(3-methoxyphenyl)sulfonyl]propanoic
1584(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-2-hydroxy-4-(phenylsulfonyl)butanoate
1586(1R,2S)-2-Amino-1-{[(3-methoxybenzyl)amino]methyl}-3-phenylpropyl-2-hydroxy-4-[(3-methylbutyl)sulfonyl]butanoic
1588(1R,2S)-2-Amino-1-{[(3-methoxybenzyl)amino]methyl}-3-phenylpropyl-4-[(3-methylbutyl)sulfonyl]-2-phenoxybutyric
1590 (1R,2S)-2-Amino-1-{[(3-methoxybenzyl)amino]methyl}-3-phenylpropyl-2-(3-methoxyphenoxy)-4-[(3-methylbutyl)sulfonyl]butanoic
15923-{1-{[((1R,2S)-2-Amino-1-{[(3-methoxybenzyl)amino]methyl}-3-phenylpropyl)oxy]carbonyl}-3-[(3-methylbutyl)sulfonyl]propoxy}benzoic acid
1594Methyl-3-{1-{[((1R,2S)-2-amino-1-{[(3-methoxybenzyl)amino]methyl}-3-phenylpropyl)oxy]carbonyl}-3-[(3-methylbutyl)sulfonyl]propoxy}benzoate
1596(1R,2S)-2-Amino-1-{[(3-methoxybenzyl)amino]methyl}-3-phenylpropyl-2-hydroxy-4-(phenylsulfonyl)butanoate
1598(1R,2S)-2-Amino-1-{[(3-methoxybenzyl)amino]methyl}-3-phenylpropyl-2-hydroxy-4-(phenylthio)butanoate
1600(1R,2S)-2-Amino-1-{[(3-methoxybenzyl)amino]methyl}-3-phenylpropyl-2-methoxy-4-(phenylsulfonyl)butanoate
1602(1R,2S)-2-Amino-1-{[(3-methoxybenzyl)amino]methyl}-3-phenylpropyl-2-methoxy-4-(phenylthio)butanoate
1604(1R,2S)-2-Amino-1-{[(3-methoxybenzyl)amino]methyl}-3-phenylpropyl-4-(peninsul who were radioactive)-2-propoxyethanol
1606(1R,2S)-2-Amino-1-{[(3-methoxybenzyl)amino]methyl}-3-phenylpropyl-2-(benzyloxy)-4-(phenylsulfonyl)butanoate
1608(1R,2S)-2-Amino-1-{[(3-methoxybenzyl)amino]methyl}-3-phenylpropyl-N-[(benzyloxy)carbonyl]methionine
1610(1R,2S)-2-Amino-1-{[(3-methoxybenzyl)amino]methyl}-3-phenylpropyl-(2S)-2-amino-5-oxo-5-piperidine-1-repentant
1612(1R,2S)-2-Amino-1-{[(3-methoxybenzyl)amino]methyl}-3-phenylpropyl-(2S)-2-[(2-methoxy-5-oxoethyl)amino]-5-oxo-5-piperidine-1-repentant
1614(1R,2S)-2-Amino-1-{[(3-methoxybenzyl)amino]methyl}-3-phenylpropyl-(2R)-2-amino-5-oxo-5-piperidine-1-repentant
1616(1R,2S)-2-Amino-1-{[(3-methoxybenzyl)amino]methyl}-3-phenylpropyl-(2R)-2-[(2-ethoxy-2-oxoethyl)amino]-5-oxo-5-piperidine-1-repentant
1618(1R,2S)-2-Amino-1-{[(3-methoxybenzyl)amino]methyl}-3-phenylpropyl-(2R)-2-[(4-ethoxy-4-oxobutyl)amino]-5-oxo-5-piperidine-1-repentant
1620 (1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-(2R)-2-[(methoxycarbonyl)amino]-4-oxooctanoate
1622(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-4-butyl-N-(methoxycarbonyl)-D-homoserine
1624(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-(2-butyl-1,3-dioxolane-2-yl)-N-(methoxycarbonyl)-D-alaninate
1626(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-(2-butyl-1,3-dioxane-2-yl)-N-(methoxycarbonyl)-D-alaninate
1628(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-(2R)-4,4-debtor-2-[(methoxycarbonyl)amino]octanoic
1630(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-(2R)-4-fluoro-2-[(methoxycarbonyl)amino]octanoic
1632(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-(2R)-2-[(methoxycarbonyl)amino]-5-exonerat
1634(1R,2S)-2-Amino-3-(3,5-debtor the Nile)-1-{[(3-active compounds)amino]methyl}propyl-(2R)-5-hydroxy-2-[(methoxycarbonyl)amino]nonanoate
1636(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-(2R)-4-(2-butyl-1,3-dioxolane-2-yl)-2-[(methoxycarbonyl)amino]butanoate
1638(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-(2R)-4-(2-butyl-1,3-dioxane-2-yl)-2-[(methoxycarbonyl)amino]butanoate
1640(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-(2R)-5-fluoro-2-[(methoxycarbonyl)amino]nonanoate
1642(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-(2R)-5,5-debtor-2-[(methoxycarbonyl)amino]nonanoate
1644(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-(butylsulfonyl)-N-(methoxycarbonyl)-D-alaninate
1646(1R,2S)-2-Amino-3-(3,5-differenl)-1-({[3-(trifluoromethyl)benzyl]amino}methyl)propyl-3-(butylsulfonyl)-N-(methoxycarbonyl)-D-alaninate
1648(1R,2S)-2-Amino-3-(3,5-differenl)-1-({[3-(ethylphenyl)cyclopropyl]amino}methyl)propyl-3-(butylsulfonyl)-N-(is ethoxycarbonyl)-D-alaninate
1650(1R,2S)-2-Amino-3-(3,5-differenl)-1-({1-[3-(ethynylphenyl)cyclopropyl]amino}methyl)propyl-3-(butylsulfonyl)-N-(methoxycarbonyl)-D-alaninate
1652(1R,2S)-2-Amino-3-(3,5-differenl)-1-[({1-[3-(trifluoromethyl)phenyl]cyclopropyl}amino)methyl]propyl-3-(butylsulfonyl)-N-(methoxycarbonyl)-D-alaninate
1654(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[3-(ethynylphenyl)amino]methyl}propyl-3-(butylsulfonyl)-N-[(3-methyl-1H-pyrazole-5-yl)carbonyl]-D-alaninate
1656(1R,2S)-2-Amino-3-(3,5-differenl)-1-({[3-(trifluoromethyl)benzyl]amino}methyl)propyl-3-(butylsulfonyl)-N-[(3-methyl-1H-pyrazole-5-yl)carbonyl]-D-alaninate
1658(1R,2S)-2-Amino-3-(3,5-differenl)-1-({[1-(3-ethylphenyl)cyclopropyl]amino}methyl)propyl-3-(butylsulfonyl)-N-[(3-methyl-1H-pyrazole-5-yl)carbonyl]-D-alaninate
1660(1R,2S)-2-Amino-3-(3,5-differenl)-1-({[1-(3-ethynylphenyl)cyclopropyl]amino}methyl)propyl-3-(butylsulfonyl)-N-[(3-methyl-1H-pyrazole-5-yl)carbonyl]-D-alaninate
16621664(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-(2R)-2-{[(methylamino)carbonyl]amino}-4-oxooctanoate
1666(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-4-butyl-N-[(methylamino)carbonyl]-D-homoserine
1668(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-(2-butyl-1,3-dioxolane-2-yl)-N-[(methylamino)carbonyl]-D-alaninate
1670(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-(2-butyl-1,3-dioxane-2-yl)-N-[(methylamino)carbonyl]-D-alaninate
1672(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-(2R)-4,4-debtor-2-{[(methylamino)carbonyl]amino}octanoate
1674(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-(2R)-4-fluoro-2-{[(methylamino)carbonyl]amino}octanoate
1676(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-(2R)-2-{[(methylamino)carbonyl]amino}-5-exonerat
1678(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-(2R)-5-hydroxy-2-{[(methylamino)carbonyl]amino}nonanoate
1680(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-(2R)-4-(2-butyl-1,3-dioxolane-2-yl)-2-{[(methylamino)carbonyl]amino}of butanoate
1682(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-(2R)-4-(2-butyl-1,3-dioxane-2-yl)-2-{[(methylamino)carbonyl]amino}of butanoate
1684(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-(2R)-5-fluoro-2-{[(methylamino)carbonyl]amino}nonanoate
1686(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-(2R)-5,5-debtor-2-{[(methylamino)carbonyl]amino}nonanoate
1688(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-ethynylphenyl)amino]methyl}propyl-3-(butylsulfonyl)-N-[(methylamino)carbonyl]-D-Alani is at
1690(1R,2S)-2-Amino-3-(3,5-differenl)-1-({[3-(trifluoromethyl)benzyl]amino}methyl)propyl-3-(butylsulfonyl)-N-[(methylamino)carbonyl]-D-alaninate
1692(1R,2S)-2-Amino-3-(3,5-differenl)-1-({[1-(3-ethylphenyl)cyclopropyl]amino}methyl)propyl-3-(butylsulfonyl)-N-[(methylamino)carbonyl]-D-alaninate
1694(1R,2S)-2-Amino-3-(3,5-differenl)-1-({[1-(3-ethynylphenyl)cyclopropyl]amino}methyl)propyl-3-(butylsulfonyl)-N-[(methylamino)carbonyl]-D-alaninate
1696(1R,2S)-2-Amino-3-(3,5-differenl)-1-[({1-[3-(trifluoromethyl)phenyl]cyclopropyl}amino)methyl]propyl-3-(butylsulfonyl)-N-[(methylamino)carbonyl]-D-alaninate
1698(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-ethynylphenyl)amino]methyl)propyl-3-(butylsulfonyl)-N-[(4-methyl-1H-pyrazole-1-yl)carbonyl]-D-alaninate
1700(1R,2S)-2-Amino-3-(3,5-differenl)-1-({[3-(trifluoromethyl)benzyl]amino}methyl)propyl-3-(butylsulfonyl)-N-[(4-methyl-1H-pyrazole-1-yl)carbonyl]-D-alaninate
1702(1R,2S)-2-Am is but-3-(3,5-differenl)-1-({[1-(3-ethylphenyl)cyclopropyl]amino}methyl)propyl-3-(butylsulfonyl)-N-[(4-methyl-1H-pyrazole-1-yl)carbonyl]-D-alaninate
1704(1R,2S)-2-Amino-3-(3,5-differenl)-1-({[1-(3-ethynylphenyl)cyclopropyl]amino}methyl)propyl-3-(butylsulfonyl)-N-[(4-methyl-1H-pyrazole-1-yl)carbonyl]-D-alaninate
1706(1R,2S)-2-Amino-3-(3,5-differenl)-1-[({1-[3-(trifluoromethyl)phenyl]cyclopropyl}amino)methyl]propyl-3-(butylsulfonyl)-N-[(4-methyl-1H-pyrazole-1-yl)carbonyl]-D-alaninate
1173
1175
1177
1179
1181
1183
1185
1187
1189
1191
1193
1195
1197
1199
1201
1203
1205
1207
1209
1211
1213
1215
1217
1219
1221
1223
1225
1227
1229
1231
1233Benzyl-[(1R)-1-{[[(2R,3S)-3-amino-4-(3,5-differenl)-2-hydroxybutyl](3-active compounds)amino]carbonyl}-3-(methylsulphonyl)propyl]carbamate
1235
1237
1239
1241
1243
1245
1247
1249
1251
1253
1255
1257
1259
1261
1263
1265
1267
1269
1271
1273
1275
1277
1279
1281
1283
1285
1287
1289
1291
1293
1295
1297
1299(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-[(1-propinball)sulfonyl]-N-[(tetrahydro-2H-Piran-4-yloxy)carbonyl]alaninate
1301
1303S-(3-[(2R,3S)-3-Amino-2-hydroxy-4-phenylbutyl](3-methoxybenzyl)amino]-2-{[(3-methylbutyl)sulfonyl]methyl}-3-oxopropyl)attentioin
1305
1307
1309N-[(2R,3S)-3-Amino-2-hydroxy-4-phenylbutyl]-N-(3-methoxybenzyl)-2-(3-methoxyphenoxy)-4-[(3-methylbutyl)sulfonyl]butanamide
1311
1313
1315
1317
1319
1321N1-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-3-(butylsulfonyl)-N1 -(3-active compounds)-N2-(3,3,3-tryptophanyl)-D-alaninate
1323N1-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-3-(butylsulfonyl)-N1-(3-active compounds)-N2-(TRIFLUOROACETYL)-D-alaninate
1325N-[(2R,3S)-3-Amino-2-hydroxy-4-phenylbutyl]-2-methoxy-N-(3-methoxybenzyl)-4-(phenylthio)butanamide
1327
1329N1-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-3-(butylsulfonyl)-N2(cyclopropanecarbonyl)-N1-(3-active compounds)-D-alaninate
1331β-Alanyl-N1-[(2R,3S)-3-amino-4-(3,5-differenl)-2-hydroxybutyl]-3-(butylsulfonyl)-N1-(3-active compounds)-D-alaninate
1333Glycyl-N1-[(2R,3S)-3-amino-4-(3,5-differenl)-2-hydroxybutyl]-3-(butylsulfonyl)-N1-(3-active compounds)-D-alaninate the
1335(1R,2S)-2-Amino-1-{[(3-methoxybenzyl)amino]methyl}-3-phenylpropyl-(2R)-2-[(4-ethoxy-4-oxobutyl)amino]-5-oxo-5-piperidine-1-repentant
1337N,N-Dimethyl-β-alanyl-N1-[(2R,3S)-3-amino-4-(3,5-differenl)-2-hydroxybutyl]-3-(butylsulfonyl)-N1-(3-active compounds)-D-alaninate
1339N1-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-3-(butylsulfonyl)-N1-(3-active compounds)-N2(methoxyacetyl)-D-alaninate
1341
1343
1345(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-(2-butyl-1,3-dioxane-2-yl)-N-(methoxycarbonyl)-D-alaninate
1347
1349
1351
1353
1355
1357N2-Acetyl-N1-[(2R,3S)-3-amino-4-(3,5-differenl)-2-hydroxybutyl]-3-(butylsulfonyl)-N1-(3-methylbutyl)-D-alaninate
1359N1-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N1-cyclopropyl-N2(cyclopropanecarbonyl)-3-[(1-propinball)sulfonyl]-D-alaninate
1361N2-Acetyl-N1-[(2R,3S)-3-amino-4-(3,5-differenl)-2-hydroxybutyl]-N1-(3-methylbutyl)-3-[(1-propinball)sulfonyl]-D-alaninate
1363
1365
1367
1369
1371
1373N-Phenylglycyl-N1-[(2R,3S)-3-amino-4-(3,5-differenl)-2-hydroxybutyl]-N1-(3-active compounds)-3-[(1-propinball)sulfonyl]-D-alaninate
1375
1377
1379
1381
1383
1385N-Acetyl-β-alanyl-N1-[(2R,3S)-3-amino-4-(3,5-differenl)-2-hydroxybutyl]-N1-(3-active compounds)-3-[(1-propinball)sulfonyl]-D-alaninate
1387N1-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N2-(chloroacetyl)-N1-(3-active compounds)-3-[(1-propinball)sulfonyl]-D-alaninate
1389N1-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N1-(3-active compounds)-N2(methoxyacetyl)-3-[(1-propinball)sulfonyl]-D-alaninate
1391N1-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N1-(3-active compounds)-N2(methoxypropanol)-3-[(1-propinball)sulfonyl]-D-alaninate
1393N1-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N2-(2,2-dimethylpropanoyl)-N1-(3-active compounds)-3-[(1-propinball)sulfonyl]-D-alaninate
1395N1-[(2R,3S)-3-Amino-4-(3,5-debtor the Nile)-2-hydroxybutyl]-N 1-(3-active compounds)-N2-isobutyryl-3-[(1-propinball)sulfonyl]-D-alaninate
1397
1399N2-Acetyl-N1-[(2R,3S)-3-amino-4-(3,5-differenl)-2-hydroxybutyl]-N1-(3-active compounds)-3-[(1-propinball)sulfonyl]-D-alaninate
1401
1403
1405
1407
1409
1411N1-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl the]-N 2(cyclopropanecarbonyl)-N1-(3-active compounds)-3-[(1-propinball)sulfonyl]-D-alaninate
1413N1-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N1-(3-active compounds)-N2-propionyl 3-[(1-propinball)sulfonyl]-D-alaninate
1415
1417
1419
1421
1423Hydrochloride 5-oxo-D-prolyl-N1-[(2R,3S)-3-amino-4-(3,5-differenl)-2-hydroxybutyl]-N1-(3-active compounds)-3-[(1-propinball)sulfonyl]alaninemia
14255-Oxo-L-prolyl-N1-[(2R,3S)-3-and the Ino-4-(3,5-differenl)-2-hydroxybutyl]-N 1-(3-active compounds)-3-[(1-propinball)sulfonyl]alanine
1427N1-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N1-(3-active compounds)-N2-[3-(4-oxo-2-thioxo-1,3-thiazolidin-3-yl)propanol]-3-[(1-propinball)sulfonyl]alanine
1429
1431
1433
1435
1437
1439
1441
1443/td> N1-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N1-(3-active compounds)-N2-(1H-imidazol-4-ylacetic)-3-[(1-propinball)sulfonyl]alanine
1445
1447
1449
1451
1453
1455
1457
1459
1461
1463
1465
1467
1469
1471
1473
1475
1477
1479
1481
1483
1485N1-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N1-(3-active compounds)-N2(phenylacetyl)-3-[(1-propinball)sulfonyl]alanine
1487N1-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N1-(3-active compounds)-N2(phenylpropenoyl)-3-[(1-propinball)sulfonyl]alanine
1489N-(3-[[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl](3-active compounds)amino]-3-oxo-2-{[(1-propinball)sulfonyl]methyl}propyl)benzamide
1491N1-[(2R,3S)-3-Amino-2-hydroxy-4-phenylbutyl]-N2(cyclopropylethyl)-N1-(3-methoxybenzyl)-3-[(1-propinball)sulfonyl]alanine
1493N1-[(2R,3S)-3-Amino-2-hydroxy-4-phenylbutyl-N1-(3-methoxybenzyl)-N2-[(methylsulphonyl)acetyl]-3-[(1-propinball)sulfonyl]alanine
1495N1-[(2R,3S)-3-Amino-2-hydroxy-4-phenylbutyl-N1-(3-methoxybenzyl)-N2-[(methylthio)acetyl]-3-[(1-propinball)sulfonyl]alanine
1497
1499
1501
1503N-(Methylsulphonyl)glycyl-N1-[(2R,3S)-3-amino-2-hydroxy-4-phenylbutyl]-N1-(3-methoxybenzyl)-3-[(1-propinball)sulfonyl]alanine
1505N2-Acetyl-N1-[(2R,3S)-3-amino-2-hydroxy-4-phenylbutyl]-N1-(3-methoxybenzyl)-3-(phenylsulfonyl)alaninate
1507
1509
1511
1513
1515
1517
15192-[[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl](3-active compounds)amino]-1-[(butylsulfonyl)methyl]-2-oxoacetate
1521N1-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-S-butyl-N1-(3-active compounds)-D-cysteine
1523N1-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-3-(butylsulfonyl)-N1-(3-active compounds)-D-alaninate
1525N1-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-3-(butylsulfonyl)-N1-(3-active compounds)-D-alaninate
1527N1-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-3-(butylsulfonyl)-N1-3-active compounds)-L-alaninate
1529N1-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-3-(butylsulfonyl)-N1-(3-methylbutyl)-D-alaninate
1531N1-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N1-[1-(3-ethylphenyl)cyclopropyl]-3-[(1-propinball)sulfonyl]-D-alaninate
1533N1-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N1-(3-active compounds)-3-[(1-propinball)sulfonyl]-L-alaninate
1535N1-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N1-cyclopropyl-3-[(1-propinball)sulfonyl]-D-alaninate
1537N1-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N1-(3-methylbutyl)-3-[(1-propinball)sulfonyl]-D-alaninate
1539N1-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N1-(3-active compounds)-3-[(1-propinball)sulfonyl]-D-alaninate
1541N1-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N1-(3-active compounds)-3-[(1-propylate is)sulfonyl]alanine
1543N1-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N1-(3-active compounds)-N2(phenoxyacetyl)-3-[(1-propinball)sulfonyl]alanine
1545N1-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N2-{[(5-chloro-2-thienyl)thio]peroxy}-N1-(3-active compounds)-3-[(1-propinball)sulfonyl]alanine
1547N1-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N1-(3-active compounds)-N2-(phenylsulfonyl)-3-[(1-propinball)sulfonyl]alanine
1549N2-[(Benzylamino)carbonyl]-N1-[(2R,3S)-4-(3,5-differenl)-2-hydroxy-3-(methylamino)butyl]-N1-(3-active compounds)-3-[(1-propinball)sulfonyl]alanine
15514-[[(2R,3S)-4-(3,5-Differenl)-2-hydroxy-3-(methylamino)butyl](3-active compounds)amino]-4-oxo-3-{[(1-propinball)sulfonyl]methyl}butane acid
15534-[[(2R,3S)-3-Amino-2-hydroxy-4-phenylbutyl](3-methoxybenzyl)amino]-3-{[(3-methylbutyl)sulfonyl]methyl}-4-oxobutanoic acid
1555 Methyl-4-[[(2R,3S)-3-amino-2-hydroxy-4-phenylbutyl](3-methoxybenzyl)amino]-3-{[(3-methylbutyl)sulfonyl]methyl}-4-oxobutanoate
1557N1-[(2R,3S)-3-Amino-2-hydroxy-4-phenylbutyl]-N1-(3-methoxybenzyl)-2-{[(3-methylbutyl)sulfonyl]methyl}succinamic
1559N1-[(2R,3S)-3-Amino-2-hydroxy-4-phenylbutyl]-N1-(3-methoxybenzyl)-N4-methyl-2-{[(3-methylbutyl)sulfonyl]methyl}succinamic
1561N1-[(2R,3S)-3-Amino-2-hydroxy-4-phenylbutyl]-N1-(3-methoxybenzyl)-N4N4-dimethyl-2-{[(3-methylbutyl)sulfonyl]methyl}succinamic
1563N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-3-(4,4-dimethyl-2,5-dioxoimidazolidin-1-yl)-N-(3-active compounds)-2-{[(1-propinball)sulfonyl]methyl}propanamide
1565N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-3-(4,4-dimethyl-2,5-dioxoimidazolidin-1-yl)-N-(3-active compounds)-2-{[(1-propinball)sulfonyl]methyl}propanamide
1567(1R,2S)-2-Amino-3-(3,5-differenl)-1-{[(3-active compounds)and the Ino]methyl}propyl-3-(4,4-dimethyl-2,5-dioxoimidazolidin-1-yl)-2-{[(1-propinball)sulfonyl]methyl}propanoic
1569N-[(2R,3S)-3-Amino-2-hydroxy-4-phenylbutyl]-3-(ethylsulfonyl)-2-{[(isobutylphenyl)amino]methyl}-N-(3-methoxybenzyl)propanamide
1571N-[(2R,3S)-3-Amino-2-hydroxy-4-phenylbutyl]-3-(ethylthio)-2-{[(isobutylphenyl)amino]methyl}-N-(3-methoxybenzyl)propanamide
1573(2S)-N-[(2R,3S)-3-Amino-2-hydroxy-4-phenylbutyl]-N-(3-methoxybenzyl)-2-{[(3-methylbutyl)sulfonyl]amino}-4-(methylsulphonyl)butanamide
1575N1-[(2R,3S)-3-Amino-2-hydroxy-4-phenylbutyl]-N1-(3-methoxybenzyl)-N2-(3-methylbutyl)sulfonyl-L-methioninamide
1577S-(3-[[(2R,3S)-3-Amino-2-hydroxy-4-phenylbutyl](3-methoxybenzyl)amino]-2-{(3-methylbutyl)sulfonyl]methyl}-3-oxopropyl)attentioin
1579N-[(2R,3S)-3-Amino-2-hydroxy-4-phenylbutyl]-2-hydroxy-N-(3-methoxybenzyl)-3-[(1-propinball)sulfonyl]propanamide
1581N-[(2R,3S)-3-Amino-2-hydroxy-4-phenylbutyl]-2-hydroxy-N-(3-methoxybenzyl)-3-[(3-methylbutyl)sulfonyl]propanamide
N-[(2R,3S)-3-Amino-2-hydroxy-4-phenylbutyl]-2-hydroxy-N-(3-methoxybenzyl)-3-[(3-methoxyphenyl)sulfonyl]propanamide
1585N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-2-hydroxy-4-(phenylsulfonyl)butanamide
1587N-[(2R,3S)-3-Amino-2-hydroxy-4-phenylbutyl]-2-hydroxy-N-(3-methoxybenzyl)-4-[(3-methylbutyl)sulfonyl]butanamide
1589N-[(2R,3S)-3-Amino-2-hydroxy-4-phenylbutyl]-N-(3-methoxybenzyl)-4-[(3-methylbutyl)sulfonyl]-2-phenoxybutyric
1591N-[(2R,3S)-3-Amino-2-hydroxy-4-phenylbutyl]-N-(3-methoxybenzyl)-2-(3-methoxyphenoxy)-4-[(3-methylbutyl)sulfonyl]butanamide
15933-{1-{[[(2R,3S)-3-Amino-2-hydroxy-4-phenylbutyl](3-methoxybenzyl)amino]carbonyl}-3-[(3-methylbutyl)sulfonyl]propoxy}benzoic acid
1595Methyl-3-{1-{[[(2R,3S)-3-amino-2-hydroxy-4-phenylbutyl](3-methoxybenzyl)amino]carbonyl}-3-[(3-methylbutyl)sulfonyl]propoxy}benzoate
1597 N-[(2R,3S)-3-Amino-2-hydroxy-4-phenylbutyl]-2-hydroxy-N-(3-methoxybenzyl)-4-(phenylsulfonyl)butanamide
1599N-[(2R,3S)-3-Amino-2-hydroxy-4-phenylbutyl]-2-hydroxy-N-(3-methoxybenzyl)-4-(phenylthio)butanamide
1601N-[(2R,3S)-3-Amino-2-hydroxy-4-phenylbutyl]-2-methoxy-N-(3-methoxybenzyl)-4-(phenylsulfonyl)butanamide
1603N-[(2R,3S)-3-Amino-2-hydroxy-4-phenylbutyl]-2-methoxy-N-(3-methoxybenzyl)-4-(phenylthio)butanamide
1605N-[(2R,3S)-3-Amino-2-hydroxy-4-phenylbutyl]-N-(3-methoxybenzyl)-4-(phenylsulfonyl)-2-propoxyethanol
1607N-[(2R,3S)-3-Amino-2-hydroxy-4-phenylbutyl]-2-(benzyloxy)-N-(3-methoxybenzyl)-4-(phenylsulfonyl)butanamide
1609
1611(2S)-2-Amino-N-[(2R,3S)-3-amino-2-hydroxy-4-phenylbutyl]-N-(3-methoxybenzyl)-5-oxo-5-piperidine-1-ilistened
163
1615(2R)-2-Amino-N-[(2R,3S)-3-amino-2-hydroxy-4-phenylbutyl]-N-(3-methoxybenzyl)-5-oxo-5-piperidine-1-ilistened
1617
1619
1621Methyl-((1R)-1-{[[(2R,3S)-3-amino-4-(3,5-differenl)-2-hydroxybutyl](3-active compounds)amino]carbonyl}-3-oxoethyl)carbamate
1623
1625
1627
1629Methyl-((1R)-1-{[[(2R,3S)-3-AMI is about-4-(3,5-differenl)-2-hydroxybutyl](3-active compounds)amino]carbonyl}-3,3-deftarget)carbamate
1631Methyl-((1R)-1-{[[(2R,3S)-3-amino-4-(3,5-differenl)-2-hydroxybutyl](3-active compounds)amino]carbonyl}-3-forgetter)carbamate
1633Methyl-((1R)-1-{[[(2R,3S)-3-amino-4-(3,5-differenl)-2-hydroxybutyl](3-active compounds)amino]carbonyl}-4-oxoethyl)carbamate
1635Methyl-((1R)-1-{[[(2R,3S)-3-amino-4-(3,5-differenl)-2-hydroxybutyl](3-active compounds)amino]carbonyl}-4-hydroxyacyl)carbamate
1637Methyl-[(1R)-1-{[[(2R,3S)-3-amino-4-(3,5-differenl)-2-hydroxybutyl](3-active compounds)amino]carbonyl}-3-(2-butyl-1,3-dioxolane-2-yl)propyl]carbamate
1639Methyl-[(1R)-1-{[[(2R,3S)-3-amino-4-(3,5-differenl)-2-hydroxybutyl](3-active compounds)amino]carbonyl}-3-(2-butyl-1,3-dioxane-2-yl)propyl]carbamate
1641Methyl-((1R)-1-{[[(2R,3S)-3-amino-4-(3,5-differenl)-2-hydroxybutyl](3-active compounds)amino]carbonyl}-4-forochel)carbamate
1643Methyl-((1R)-1-{[[(2R,3S)-3-amino-4-(3,5-differenl)-2-hydroxybutyl](3-active compounds)amino]carbonyl}-4,4-differentil)carbamate/td>
1645
1647
1649
1651
1653
1655
1657
1659
1661
1663
1665(2R)-N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-2-{[(methylamino)carbonyl]amino}-4-oxooctanoate
1667N1-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-4-butyl-N1-(3-active compounds)-N2-[(methylamino)carbonyl]-D-homoserine
1669N1-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-3-(2-butyl-1,3-dioxolane-2-yl)-N1-(3-active compounds)-N2-[(methylamino)carbonyl]-D-alaninate
1671N1-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-3-(2-butyl-1,3-dioxane-2-yl)-N1-(3-active compounds)-N2-[(methylamino)carbonyl]-D-alaninate
1673(2R)-N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-4,4-debtor-2-{[(methylamino)carbonyl]amino}octanamide
1675(2R)-N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-4-fluoro-2-{[(methylamino)carbonyl]amino}octanamide
1677(2R)-N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-Ki is oxybutyl]-N-(3-active compounds)-2-{[(methylamino)carbonyl]amino}-5-econonomic
1679(2R)-N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-5-hydroxy-2-{[(methylamino)carbonyl]amino}nonanamide
1681(2R)-N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-4-(2-butyl-1,3-dioxolane-2-yl)-N-(3-active compounds)-2-{[(methylamino)carbonyl]amino}butanamide
1683(2R)-N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-4-(2-butyl-1,3-dioxane-2-yl)-N-(3-active compounds)-2-{[(methylamino)carbonyl]amino}butanamide
1685(2R)-N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-5-fluoro-2-{[(methylamino)carbonyl]amino}nonanamide
1687(2R)-N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-5,5-debtor-2-{[(methylamino)carbonyl]amino}nonanamide
1689N1-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-3-(butylsulfonyl)-N1-(3-active compounds)-N2-[(methylamino)carbonyl]-D-alaninate
1691N1-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-3-(b is tilsley)-N 2-[(methylamino)carbonyl]-N1-[3-(trifluoromethyl)benzyl]-D-alaninate
1693N1-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-3-(butylsulfonyl)-N1-[1-(3-ethylphenyl)cyclopropyl]-N2-[(methylamino)carbonyl]-D-alaninate
1695N1-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-3-(butylsulfonyl)-N1-[1-(3-ethynylphenyl)cyclopropyl]-N2-[(methylamino)carbonyl]-D-alaninate
1697N1-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-3-(butylsulfonyl)-N2-[(methylamino)carbonyl]-N1-{1-[3-(trifluoromethyl)phenyl]cyclopropyl}-D-alanine
1699
1701
1703
1705
1707

1708
1709
1710
1711
1712
1713
1714
1715
1716
1717
1718
1719
1720
1721
1722
1723
1724
1725
1726
1727
1728
1729

Examples of rearrangement

The following examples illustrate the migration of the acyl group, which occurs in the compounds of the invention. These examples are provided only for purposes of explanation and not intended to limit the scope of the invention.

The General procedure

The compound of formula (I) or (X) (5 mg) dissolved in DMSO-d6(500 ál) and add or buffer solution, pH 4 (500 μl, bufonidae substance hydroptila potassium), or buffer solution, pH 7 (500 μl, bufferer the abuser substance sodium phosphate and potassium). The sample was then heated to 40 ºC. Check O-acyl or N-acyl migration to the N-end, watching the change in chemical shift for the aromatic fluorine using19F-NMR. (Shifts of fluorine atoms associated with the desired migration, confirmed by comparison with authentic analogue.) The sample analyzing method19F-NMR approximately at time 0, 1,5, 3, 24, 48 and 144 hours. The number of On-allstargame prodrugs, N-allstargame prodrugs and the desired product migration in each moment of time estimated by integration of the corresponding NMR signals.

Example 1

A specific example of the NMR

Hydrochloride N~1~-[(2R,3S)-3-amino-4-(3,5-differenl)-2-hydroxybutyl]-5-(1,3-oxazol-2-yl)-N-~3~,N~3~-dipropyl-N~1~-[3-(trifluoromethyl)benzyl]isophthalamide (preparative example 7, 5 mg) is dissolved in DMSO-d6(500 ál) and add buffer solution, pH 4 (500 μl, bufonidae substance hydroptila potassium). The sample was then heated to 40 ºC. Check N-acyl migration of N-acyl N-end, watching the change in chemical shift for the aromatic fluorine using19F-NMR. (Shifts of fluorine atoms to the desired product migration in the presence of buffer is confirmed by comparison with authentic product migration, N1-((1S,2R)-1-(3,5-differenl)-2-hydroxy-3-{[3-(trifluoromethyl)is ensil]amino}propyl)-5-(1,3-oxazol-2-yl)-N 3N3-dipropylacetamide.) These NMR collect at time 0, 1, 3, 25, 48, 96 and 144 hours. The amount of N-allstargame prodrugs and the desired product migration present in each moment of time, estimated by integration of the corresponding NMR signals. The lack of migration to On-allstargame prodrugs see using this method and podverzhdayut by comparison with authentic connection.

The following examples illustrate the migration in a solution of acyl groups of the compounds of formulas (I) and (X), the observed method19F-NMR spectroscopy. The results are collected, as described above in example 1.

Example 2

Rearrangement of (1R,2S)-2-amino-3-(3,5-differenl)-1-({[1-(3-ethynylphenyl)cyclopropyl]amino}methyl)propyl-3-[(dipropylamino)carbonyl]-5-(1,3-oxazol-2-yl)benzoate (22)

Table 1-2 shows the relative concentrations of prodrugs 22 and its rearrangement product as a function of time and the change of the pH value.

Table 1
Concentration at 40 ºC, pH 7
pH 7, -40 ° C
TimeO-Acyl. the prodrugN-Acyl. the prodrug Product NEA1
(h)(% prisutstvie.)(% prisutstvie.)(% prisutstvie.)
010000
0,510010
100100
1NEA = hydroxyethylaminomethyl product migration acyl group

Table 2
Concentration at 40 º C, pH 4
pH 4, -40 ° C
TimeO-Acyl. the prodrugN-Acyl. the prodrugProduct NEA
(h)(% prisutstvie.)(% prisutstvie.)(% prisutstvie.)
010000
0,59307
187013
366027
649042
249078
480086

Example 3

Regrouping dihydrochloride (1R,2S)-2-amino-3-(3,5-differenl)-1-({[1-(3-ethylphenyl)cyclopropyl]amino}methyl)propyl-3-[(dipropylamino)carbonyl]-5-(1,3-oxazol-2-yl)benzoate (17)

Table 3-4 shows the relative concentrations of prodrugs 17 and its rearrangement product as a function of time and the change of the pH value.

Table 3
Concentration at 40 ºC, pH 7
pH 7, -40 ° C
TimeO-Acyl. P is lekarstwo N-Acyl. the prodrugProduct NEA
(h)(% prisutstvie.)(% prisutstvie.)(% prisutstvie.)
010000
1,53097
70
240
480
1440

Table 4
Concentration at 40 º C, pH 4
pH 4, -40 ° C
TimeO-Acyl. the prodrugN-Acyl. the prodrugRead the t NEA
(h)(% prisutstvie.)(% prisutstvie.)(% prisutstvie.)
010000
1,553047
333067
611089
2400100

Example 4

Regrouping hydrochloride N1-[(2R,3S)-3-amino-4-(3,5-differenl)-2-hydroxybutyl]-N(u)1(d)-(3-active compounds)-5-(1,3-oxazol-2-yl)-N3N3-dipropylacetamide (19)

Table 5-6 shows the relative concentrations of prodrugs 19 and its rearrangement product as a function of time and the change of the pH value.

Table 5
Concentration at 40 ºC, pH 7
pH 7, -40 ° C
TimeO-Acyl. the prodrugN-Acyl. the prodrugProduct NEA
(h)(% prisutstvie.)(% prisutstvie.)(% prisutstvie.)
001000
10973
30919
2406040
4803763
9601981

Table 6
Concentration at 40 º C, pH 4
pH 4, -40 ° C
TimeOn-the cyl. the prodrugN-Acyl. the prodrugProduct NEA
(h)(% prisutstvie.)(% prisutstvie.)(% prisutstvie.)
001000
101000
301000
240973
480955
960928

Example 5

Regrouping hydrochloride N1-[(2R,3S)-3-amino-4-(3,5-differenl)-2-hydroxybutyl]-5-(1,3-oxazol-2-yl)-N3N3-dipropyl-N1-[3-(trifluoromethyl)benzyl]isophthalamide (20)

Table 7-8 shows the relative concentrations of prodrugs 20 and prod the KTA its rearrangement as a function of time and the change of the pH value.

Table 7
Concentration at 40 ºC, pH 7
pH 7, -40 ° C
TimeO-Acyl. the prodrugN-Acyl. the prodrugProduct NEA
(h)(% prisutstvie.)(% prisutstvie.)(% prisutstvie.)
001000
10937
308812
2404951
4802773
9601288

Table 8
Concentration at 40 º C, pH 4
pH 4, -40 ° C
TimeO-Acyl. the prodrugN-Acyl. the prodrugProduct NEA
(h)(% prisutstvie.)(% prisutstvie.)(% prisutstvie.)
001000
10973
30964
240937
480928
9608812

Example 6

Regrouping dihydrochloride (1R,2S)-2-amino-3-(3,5-differenl)-1-{[1-(3-active compounds)amino]methyl}propyl-3-[(dipropylamino)carbonyl]-5-(1,3-oxazol-2-is)benzoate (16)

Table 9-10 shows the relative concentrations of prodrugs 16 and its rearrangement product as a function of time and the change of the pH value.

Table 9
Concentration at 40 ºC, pH 7
pH 7, -40 ° C
TimeO-Acyl.