Pyrimidine derivatives and their application as receptor p2y12 antagonists

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to derivatives of 4-aminocarbonylpyrimidine of formula (I).

EFFECT: invention is applicable as P2Y12 receptor antagonists for treatment and/or prevention of diseases or disease states of peripheral vessels, as well as vessels, supplying internal organs, vessels of liver and kidneys, in treatment and/or prevention of cardiovascular and cerebrovascular diseases and states, associated with aggregation of platelets, including thrombosis in humans and mammals.

26 cl, 500 ex

 

The text descriptions are given in facsimile form.

1. A compound selected from the group consisting of compounds of the formula I:

where R1represents phenyl, optionally substituted 1-3 times by substituents, each of which is independently selected from the group consisting of halogen, methyl and methoxy;
W represents a simple bond, and
R2represents a (C1-C7)alkyl; halogen(C1-C7)alkyl; cyano; hydroxy(C1-C7)alkyl; hydroxy(C1-C7)alkyl, substituted in the alkyl chain unsubstituted phenyl group; a (C1-C6)alkoxy(C1-C7)al the sludge; heterocyclyl where heterocyclyl represents an unsubstituted saturated monocyclic fragment of 3-7 ring members, containing 1-2 heteroatoms selected from nitrogen, oxygen and sulfur; heterocyclyl(C1-C7)alkyl, where heterocyclyl predstavlyaet an unsubstituted saturated monocyclic fragment of 3-7 ring members, containing 1-2 heteroatoms selected from nitrogen, oxygen and sulfur; cycloalkyl where cycloalkyl represents a saturated cyclic hydrocarbon fragment of 3-7 carbon atoms which may be substituted once hydroxy, hydroxymethyl, (C1-C6)alkoxy or (C1-C6)alkoxycarbonyl; and (C6-C10)aryl, possibly substituted by a group selected from halogen, (C1-C7)alkyl, (C1-C6)alkoxy, hydroxymethyl, acetyl, methanesulfonyl, trifloromethyl, carboxy, (C1-C6)alkoxycarbonyl and cyano; biphenyl-4-yl; benzo[1,3]dioxole; heteroaryl where heteroaryl represents a mono - or bicyclic aromatic ring system containing up to 10 ring atoms and where at least one of the rings contains at least one heteroatom independently selected from the group comprising nitrogen, oxygen and sulfur; 1-oxypyridine; or one of the radicals
,,img src="https://img.russianpatents.com/1070/10702999-s.jpg" height="15" width="17" /> ,
where m is 0 and n is 2 or 3, or m is 1 and n is 2,
p is 0 and q is 2 or 3, or p is 1 and q is 2, or
also p is 2 or 3, and q is 0;
Q represents-CO - or-CH(ORa)-, Rarepresents hydrogen, and Q' represents-CO-; or
W represents-CH2-, and R2represents-NR7R8, -SR9or SO2R10;
W represents-O - or-S-, and R2is a (C1-7)alkyl; carboxy(C1-C7)alkyl, (C1-C6)alkoxycarbonyl(C1-C7)alkyl; hydroxy(C1-C7)alkyl; cycloalkyl where cycloalkyl represents a saturated cyclic hydrocarbon fragment of 3-7 carbon atoms; cycloalkyl(C1-C7)alkyl, where cycloalkyl represents a saturated cyclic hydrocarbon fragment of 3-7 carbon atoms; and (C6-C10)aryl; and (C6-C10)aryl(C1-C7)alkyl; heteroaryl where heteroaryl represents a mono - or bicyclic aromatic ring system containing up to 10 ring atoms and where at least one of the rings contains at least one heteroatom independently selected from the group comprising nitrogen, oxygen and sulfur; or heteroaryl(C1-C7)alkyl, where heteroaryl p is ecstasy a mono - or bicyclic aromatic ring system, containing up to 10 ring atoms and where at least one of the rings contains at least one heteroatom independently selected from the group comprising nitrogen, oxygen and sulfur;
W represents-NR3-, and R2represents hydrogen; and (C1-C7)alkyl; di(C1-C7)alkylamino(C1-C7)alkyl, (C1-C6)alkoxycarbonyl(C1-C7)alkyl; carboxy(C1-C7)alkyl; carboxy(C1-C7)alkyl, substituted in its alkyl part unsubstituted phenyl group; hydroxy(C1-C7)alkyl, (C1-C6)alkoxy(C1-C7)alkyl; heterocyclyl where heterocyclyl represents an unsubstituted saturated monocyclic fragment of 3-7 ring members, containing 1-2 heteroatoms selected from nitrogen, oxygen and sulfur; heterocyclyl(C1-C7)alkyl, where heterocyclyl represents an unsubstituted saturated monocyclic fragment of 3-7 ring members, containing 1-2 heteroatoms selected from nitrogen, oxygen and sulfur; cycloalkyl where cycloalkyl represents a saturated cyclic hydrocarbon fragment of 3-7 carbon atoms which may be substituted once hydroxy; cycloalkyl(C1-C7)alkyl, where cycloalkyl represents a saturated cyclic hydrocarbon fragment from 3-7 the volume of carbon; (C6-C10)aryl which may be substituted with halogen: indenyl; 2-vinylcyclopropyl, (C6-C10)aryl; and (C1-C7)alkyl; diphenyl(C1-C7)alkyl; heteroaryl(C1-C7)alkyl, where heteroaryl represents a monocyclic (C5)heteroaryl containing 1-2 heteroatoms that are independently selected from the group comprising nitrogen, oxygen and sulfur; -COR11or-SO2R12;
W represents-CH=CH-, and R2is a (C1-C7)alkyl, hydroxy(C1-C7)alkyl, (C1-C6)alkoxycarbonyl, phenyl or-CO-NR13R14; or
W represents-C≡C -, and R2represents hydrogen, hydroxy(C1-C7)alkyl; or
W represents-CO - and R2is a (C1-C7)alkyl;
R3represents hydrogen or (C1-C7)alkyl;
R7is a (C1-C7)alkyl or (C6-C10)aryl(C1-C7)alkyl;
R8is a (C1-C7)alkyl;
or R7and R8together with the nitrogen atom to which they are attached, form a heterocyclic ring system containing from 4 to 7 members, where each member needed to complete the build of the specified heterocyclic ring system, independently vibrant-CH 2-,-CH(CH3)-, -CHRy-, -O-, -S-, -CO - and-NRz-if this is specified heterocyclic ring system contains no more than one member selected from the group consisting of-CHRy-, -O-, -S-, -CO - and-NRz-, Ryrepresents hydroxy, hydroxymethyl or (C1-C6)alkoxycarbonyl, and Rzrepresents hydrogen, (C1-C7)alkyl or (C1-C6)alkoxycarbonyl;
R9is cycloalkyl where cycloalkyl represents a saturated cyclic hydrocarbon fragment of 3-7 carbon atoms, or (C6-C10)aryl;
R10is a (C1-C7)alkyl, cycloalkyl where cycloalkyl represents a saturated cyclic hydrocarbon fragment of 3-7 carbon atoms, or (C6-C10)aryl;
R11is a (C1-C7)alkyl, (C1-C6)alkoxy(C1-C7)alkyl; cycloalkyl where cycloalkyl represents a saturated cyclic hydrocarbon fragment of 3-7 carbon atoms; cycloalkyl(C1-C7)alkyl, where cycloalkyl represents a saturated cyclic hydrocarbon fragment of 3-7 carbon atoms; and (C6-C10)aryl; monocyclic (C5)heteroaryl containing 1-2 heteroatoms that are independently selected from the group comprising nitrogen, Ki is oxygen and sulfur; or (C6-C10)aryl(C1-C7)alkyl;
R12is a (C1-C7)alkyl or (C6-C10)aryl;
R13is a (C1-C7)alkyl;
R14is a (C1-C7)alkyl;
or W represents-NR3-, and R2and R3together with the nitrogen atom to which they are attached, form a heterocyclic ring system containing from 4 to 7 members, where each member needed to complete the build of the specified heterocyclic ring system is independently selected from-CH2-, -CHRx-, -O-, -S-, -CO - and-NR4-if this is specified heterocyclic ring system contains no more than one member selected from the group consisting of-CHRx-, -O-, -S-, -CO - and-NR4-, Rxrepresents hydroxy, hydroxymethyl, (C1-C6)alkoxymethyl or (C1-C6)alkoxy, and R4represents hydrogen or (C1-C7)alkyl;
or W represents-NR3-, and R2and R3together with the nitrogen atom to which they are attached, form or imidazolidine, pyrazolidine, 1,2,3-triazoline or 1,2,4-triazoline ring, and the specified ring may be substituted (C1-C7)alkyl group, or 4-oxo-4H-pyridin-1-ilen, 4,5-dihydropyrazol-1-ilen, 2-methyl,5-dihydroimidazole-1-ilen, or 3-methyl-5-oxo-2,5-dihydropyrazol-1-ilen ring;
each of R5aand R5brepresents independently hydrogen or methyl;
X represents-CO - and R6is a (C1-C7)alkyl; cycloalkyl where cycloalkyl represents a saturated cyclic hydrocarbon fragment of 3-7 carbon atoms; and (C1-C6)alkoxy; and (C2-C6)alkyloxy; and (C6-C10)aryloxy; and (C6-C10)aryl(C1-C6)alkoxy; and (C6-C10)aryl; monocyclic (C5)heteroaryl containing 1-2 heteroatoms that are independently selected from the group comprising nitrogen, oxygen and sulfur, or NR15R16or X represents-SO2-, and R6is a (C1-C7)alkyl;
R15is a (C1-C7)alkyl;
R16represents hydrogen or (C1-C7)alkyl; or
R15and R16together with the nitrogen atom to which they are attached, form a heterocyclic ring system containing from 4 to 7 members, where each member needed to complete the build of the specified heterocyclic ring system represents a-CH2-; and
Y represents a simple bond, and Z represents hydrogen or (C6-10)aryl, substituted carboxy(C1-C6)alkoxy; or
Y represents a (C1-C6)alkylen (C 1-C6)alkoxy(C1-C6)alkylene, phenyl(C1-C6)alkylene, (C1-C6)alkoxyphenyl or (C1-C6)alkoxyphenyl(C1-C6)alkylene, and Z represents hydrogen, -OH, -NH2, -COOH, tetrazolyl, -CO-NH2, -COOR17,-NH-CO-R17,-NH-COOR17or-NH-SO2-R17, R17is a (C1-C7)alkyl;
or its pharmaceutically acceptable salt.

2. The compound according to claim 1, where W represents a simple bond, or its pharmaceutically acceptable salt.

3. The compound according to claim 1, where W represents-CH2or its pharmaceutically acceptable salt.

4. The compound according to claim 1, where W represents-O-, or its pharmaceutically acceptable salt.

5. The compound according to claim 1, where W represents-S-, or its pharmaceutically acceptable salt.

6. The compound according to claim 1, where W represents-NR3or its pharmaceutically acceptable salt.

7. The compound according to claim 1, where W represents-CH=CH-, or its pharmaceutically acceptable salt.

8. The compound according to claim 1, where W represents-C≡C-, or its pharmaceutically acceptable salt.

9. The compound according to claim 1, where Y is a (C1-C4)alkylene, (C1-C6)alkoxy(C1-C4)alkylene or phenyl(C1-C4)alkylene, or its pharmaceutically acceptable salt./p>

10. The compound according to claim 1, where R1represents unsubstituted phenyl, or its pharmaceutically acceptable salt.

11. The compound according to claim 1, where each of R5aand R5brepresents hydrogen, or its pharmaceutically acceptable salt.

12. The compound according to claim 1, where X represents-CO - and R6is a (C1-C6)alkoxy, (C2-C6)alkyloxy monocyclic or (C5)heteroaryl containing 1-2 heteroatoms that are independently selected from the group comprising nitrogen, oxygen and sulfur, or its pharmaceutically acceptable salt.

13. The compound according to claim 1, which is chosen from the group consisting of the following compounds:
ethyl ester of 4-{(S)-4-carboxy-2-[(6-cyclopentyloxy-2-phenylpyrimidine-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-3-carboxy-2-[(6-cyclopentyloxy-2-phenylpyrimidine-4-carbonyl)amino]propionyl}piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-5-carboxy-2-[(6-cyclopentyloxy-2-phenylpyrimidine-4-carbonyl)amino]-pentanoyl}piperazine-1-carboxylic acid;
ethyl ester of 4-{2-[(6-cyclopentyloxy-2-phenylpyrimidine-4-carbonyl)amino]acetyl}piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-2-[(6-cyclopentyloxy-2-phenylpyrimidine-4-carbonyl)amino]-3-methyl-butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-3-carbarnoyl-2-[(6-cyclopen is Naxi-2-phenylpyrimidine-4-carbonyl)amino]propionyl}piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-4-carbarnoyl-2-[(6-cyclopentyloxy-2-phenylpyrimidine-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-3-amino-2-[(6-cyclopentyloxy-2-phenylpyrimidine-4-carbonyl)amino]propionyl}piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-6-amino-2-[(6-cyclopentyloxy-2-phenylpyrimidine-4-carbonyl)amino]-hexanoyl} piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-2-[(6-cyclopentyloxy-2-phenylpyrimidine-4-carbonyl)amino]-3-hydroxypropionic}piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-2-[(6-cyclopentyloxy-2-phenylpyrimidine-4-carbonyl)amino]-4-hydroxy-butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-2-[(6-cyclopentyloxy-2-phenylpyrimidine-4-carbonyl)amino]-5-hydroxy-pentanoyl}piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-2-[(6-cyclopentyloxy-2-phenylpyrimidine-4-carbonyl)amino]-6-hydroxy-hexanoyl}piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-3-acetylamino-2-[(6-cyclopentyloxy-2-phenyl-pyrimidine-4-carbonyl)amino]propionyl}piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-2-[(6-cyclopentyloxy-2-phenylpyrimidine-4-carbonyl)amino]-3-methoxycarbonylaminophenyl}piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-2-[(6-cyclopentyloxy-2-phenylpyrimidine-4-carbonyl)amino]-3-methanesulfonylaminoethyl}piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-carboxymethoxy-2-[(6-cyclopentyloxy-2-phenylpyrimidine-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-[(S)-2-[(6-cyclopentyloxy-2-phenylpyrimidine-4-carbonyl)amino]-3-(1H-tetrazol-5-yl)propionyl]piperazine-1-carboxylic acid;
ethyl ester of 4-[(S)-2-[(6-cyclopentyloxy-2-phenylpyrimidine-4-carbonyl)amino]-4-(1H-tetrazol-5-yl)-butyryl]piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-2-[(6-cyclopentyloxy-2-phenylpyrimidine-4-carbonyl)amino]-3-[4-(1H-tetrazol-5-yl)phenyl]propionyl}piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-3-(4-carboxyphenyl)-2-[(6-cyclopentyloxy-2-phenylpyrimidine-4-carbonyl)amino]propionyl} piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-3-(4-carboxymethoxy)-2-[(6-cyclopentyloxy-2-phenylpyrimidine-4-carbonyl)amino]propionyl}piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-4-carboxy-2-[(6-carboxymethoxy-2-phenylpyrimidine-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-4-carboxy-2-[(2-phenyl-6-propoxyphene-4-carbonyl)amino]butyryl} piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[6-(2-hydroxyethoxy)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-2-[(6-benzyloxy-2-phenylpyrimidine-4-carbonyl)amino]-4-carboxy-butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-4-carboxy-2-[(6-cyclopropylmethoxy-2-phenylpyrimidine-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
acroyear 4-{(S)-4-carboxy-2-[(6-cyclohexyloxy-2-phenylpyrimidine-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-4-carboxy-2-[(6-isopropoxy-2-phenylpyrimidine-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-4-carboxy-2-[(6-methoxy-2-phenylpyrimidine-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-{3-(3-carboxymethoxy)-2-[(6-cyclopentyloxy-2-phenylpyrimidine-4-carbonyl)amino]propionyl}piperazine-1-carboxylic acid;
ethyl ester of 4-{3-(2-carboxymethoxy)-2-[(6-cyclopentyloxy-2-phenylpyrimidine-4-carbonyl)amino]propionyl}piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-2-(4-carboxymethoxy)-2-[(6-cyclopentyloxy-2-phenylpyrimidine-4-carbonyl)amino]acetyl}piperazine-1-carboxylic acid;
prop-2-injuly ester 4-{(S)-4-carboxy-2-[(6-cyclopentyloxy-2-phenylpyrimidine-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
butyl ether 4-{(S)-4-carboxy-2-[(6-cyclopentyloxy-2-phenylpyrimidine-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
isobutyl ether 4-{(S)-4-carboxy-2-[(6-cyclopentyloxy-2-phenylpyrimidine-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
2,2-dimethylpropionic ether 4-{(S)-4-carboxy-2-[(6-cyclopentyloxy-2-phenylpyrimidine-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
isopropyl ester 4-{(S)-4-carboxy-2-[(6-cyclopentyloxy-2-phenylpyrimidine-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid is you;
(S)-4-[(6-cyclopentyloxy-2-phenylpyrimidine-4-carbonyl)amino]-5-[4-(furan-2-carbonyl)piperazine-1-yl]-5-oxopentanoic acid;
phenyl ester 4-{(S)-4-carboxy-2-[(6-cyclopentyloxy-2-phenylpyrimidine-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
(S)-5-(4-benzylpiperazine-1-yl)-4-[(6-cyclopentyloxy-2-phenylpyrimidine-4-carbonyl)amino]-5-oxopentanoic acid;
benzyl ether of 4-{(S)-4-carboxy-2-[(6-cyclopentyloxy-2-phenylpyrimidine-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
(S)-5-(4-butylpiperazine-1-yl)-4-[(6-cyclopentyloxy-2-phenylpyrimidine-4-carbonyl)amino]-5-oxopentanoic acid;
(S)-4-[(6-cyclopentyloxy-2-phenylpyrimidine-4-carbonyl)amino-5-oxo-5-[4-(propane-1-sulfonyl)piperazine-1-yl]pentane acid;
ethyl ester of 4-{(S)-4-carboxy-2-[(6-cyclopentyloxy-2-phenylpyrimidine-4-carbonyl)amino]butyryl}-3-methylpiperazin-1-carboxylic acid;
ethyl ester of 4-{(S)-4-carboxy-2-[(6-cyclopentyloxy-2-phenylpyrimidine-4-carbonyl)amino]butyryl}-2-methylpiperazin-1-carboxylic acid;
ethyl ester of 4-{(S)-4-carboxy-2-[(6-cyclopentyloxy-2-phenylpyrimidine-4-carbonyl)amino]butyryl}-TRANS-2,5-dimethylpiperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-4-carboxy-2-[(6-methylamino-2-phenylpyrimidine-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-4-carboxy-2-[(2-phenyl-6-propylamino-pyrimidine-4-to bonil)amino]butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-4-carboxy-2-[(6-isopropylamino-2-phenylpyrimidine-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-2-[(6-butylamino-2-phenylpyrimidine-4-carbonyl)amino]-4-carboxy-butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-4-carboxy-2-[(6-isobutylamino-2-phenylpyrimidine-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-4-carboxy-2-[(6-cyclopropylamino-2-phenylpyrimidine-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-4-carboxy-2-[(6-cyclopentylamine-2-phenylpyrimidine-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-4-carboxy-2-[(6-cyclohexylamino-2-phenylpyrimidine-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[6-(ethoxycarbonylmethylene)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2- {[6-(carboxymethylamino)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[6-(2-hydroxyethylamino)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[6-(2-ethoxycarbonylmethylene)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[6-(2-what reboxetine)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[6-(3-hydroxypropylamino)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2- {[6-(3-carboxypropyl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester-((S)-4-carboxy-2-{[6-(2-diethylaminoethylamine)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[6-(3-dimethylaminopropylamine)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[6-(2-morpholine-4-ylethylamine)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[6-(3-morpholine-4-yl-propylamino)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-2-[(6-benzylamino-2-phenylpyrimidine-4-carbonyl)amino]-4-carboxybutyl}piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[2-phenyl-6-((S)-1-phenylethylamine)pyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[2-phenyl-6-((R)-1-phenylethylamine)pyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[6-((S)-2-carboxy-1-phenylethylamine)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid is;
ethyl ester of 4-((S)-4-carboxy-2-{[6-((R)-2-carboxy-1-phenylethylamine)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-4-carboxy-2-[(6-phenethylamine-2-phenylpyrimidine-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[2-phenyl-6-(2-phenyl-propylamino)pyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[6-(1,2-diphenylethylamine)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-(4-carboxy-2- {[2-phenyl-6-(TRANS-2-phenyl-cyclopropylamino)pyrimidine-4-carbonyl]amino)butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2- {[6-(indan-1-ylamino)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[6-((R)-indan-1-ylamino)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2- {[6-(indan-2-ylamino)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-4-carboxy-2-[(6-dimethylamino-2-phenylpyrimidine-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-2-[(6-azetidin-1-yl-2-phenylpyrimidine-4-carbonyl)amino]-4-carboxy-butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-4-carboxy-2-[(2-Hairdryer is l-6-pyrrolidin-1-Yeremey-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-4-carboxy-2-[(2-phenyl-6-piperidine-1-Yeremey-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
ethyl ester-2-phenylpyrimidine-4-carbonyl]amino}-4-carboxy-butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-4-carboxy-2-[(2-phenyl-6-phenylamino-pyrimidine-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[6-(4-forgenerating)-2-phenyl-pyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-4-carboxy-2-[(6-methyl-2-phenylpyrimidine-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-4-carboxy-2-[(6-isopropyl-2-phenylpyrimidine-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-2-[(6-butyl-2-phenylpyrimidine-4-carbonyl)amino]-4-carboxy-butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-4-carboxy-2-[(6-isobutyl-2-phenylpyrimidine-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-4-carboxy-2-[(6-cyclopropyl-2-phenylpyrimidine-4-carbonyl)amino]butyryl} piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-4-carboxy-2-[(6-cyclopentyl-2-phenylpyrimidine-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-4-carboxy-2-[(2,6-diphenylpyridine-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-4-Carbo the si-2-[(2-phenyl-6-o-tolylboronic-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-4-carboxy-2-[(2-phenyl-6-m-tolylboronic-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-4-carboxy-2-[(2-phenyl-6-p-tolylboronic-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[6-(3-carboxyphenyl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[6-(4-carboxyphenyl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-([2-(4-forfinal)-6-methylpyrimidin-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[2-(3-forfinal)-6-methylpyrimidin-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[2-(2-forfinal)-6-methylpyrimidin-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[2-(4-chlorophenyl)-6-methylpyrimidin-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[2-(3-chlorophenyl)-6-methylpyrimidin-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[2-(2-chlorophenyl)-6-methylpyrimidin-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-4-carboxy-2-[(6-methyl-2-p-tolylboronic-4-carbonyl)amino]butyryl}piperazine-1-carboxylic KIS is the notes;
ethyl ester of 4-{(S)-4-carboxy-2-[(6-methyl-2-m-tolylboronic-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[2-(4-methoxyphenyl)-6-methylpyrimidin-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[2-(3-methoxyphenyl)-6-methylpyrimidin-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-{2-[(6-isopropylamino-2-phenylpyrimidine-4-carbonyl)amino]acetyl}piperazine-1-carboxylic acid;
ethyl ester of 4-{2-[(6-benzylamino-2-phenylpyrimidine-4-carbonyl)-amino]acetyl}piperazine-1-carboxylic acid;
ethyl ester of 4-{2-[(2,6-diphenylpyridine-4-carbonyl)amino]acetyl}piperazine-1-carboxylic acid;
ethyl ester of 4-{2-[(6-cyclopropyl-2-phenylpyrimidine-4-carbonyl)-amino]acetyl}piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-2-[(6-isopropylamino-2-phenylpyrimidine-4-carbonyl)amino]-3-methyl-butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-2-[(6-benzylamino-2-phenylpyrimidine-4-carbonyl)amino]-3-methyl-butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-2-[(2,6-diphenylpyridine-4-carbonyl)amino]-3-methylbutyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-3-(4-carboxyphenyl)-2-[(6-isopropylamino-2-phenylpyrimidine-4-carbonyl)amino]propionyl}piperazine-1-carboxylic acid;
ethyl ester of 4-[(S)-2-[(6-benzylamino-2-phenylpyrimido the Jn-4-carbonyl)amino]-3-(4-carboxyphenyl)propionyl]piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-3-(4-carboxyphenyl)-2-[(2,6-diphenylpyridine-4-carbonyl)amino]propionyl}piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-3-(4-carboxyphenyl)-2-[(6-cyclopropyl-2-phenylpyrimidine-4-carbonyl)amino]propionyl)piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-5-carboxy-2-[(6-isopropylamino-2-phenylpyrimidine-4-carbonyl)amino]pentanoyl} piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-2-[(6-benzylamino-2-phenylpyrimidine-4-carbonyl)amino]-5-carboxy-pentanoyl}piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-5-carboxy-2-[(2,6-diphenylpyridine-4-carbonyl)amino]-pentanoyl}piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-5-carboxy-2-[(6-cyclopropyl-2-phenylpyrimidine-4-carbonyl)amino]-pentanoyl}piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-2-[(6-benzylamino-2-phenylpyrimidine-4-carbonyl)amino]-3-carbarnoyl-propionyl}piperazine-1-carboxylic acid;
ethyl ester of 4-[(S)-2-[(6-benzylamino-2-phenylpyrimidine-4-carbonyl)amino]-3-(2H-tetrazol-5-yl)propionyl]piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-3-(4-hydroxyphenyl)-2-[(6-isopropylamino-2-phenylpyrimidine-4-carbonyl)amino]propionyl}piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-4-tert-butoxycarbonyl-2-[(6-cyclopentyloxy-2-phenylpyrimidine-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-3-tert-butoxycarbonyl-2-[(6-cyclo is enyloxy-2-phenylpyrimidine-4-carbonyl)amino]propionyl}piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-5-tert-butoxycarbonyl-2-[(6-cyclopentyloxy-2-phenylpyrimidine-4-carbonyl)amino]pentanoyl}piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-2-[(6-cyclopentyloxy-2-phenylpyrimidine-4-carbonyl)amino]-4-ethoxycarbonylmethoxy-butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-[(S)-2-[(6-cyclopentyloxy-2-phenylpyrimidine-4-carbonyl)amino]-3-(4-ethoxycarbonylphenyl)propionyl]piperazine-1-carboxylic acid;
ethyl ester of 4-[(S)-2-[(6-cyclopentyloxy-2-phenylpyrimidine-4-carbonyl)amino]-3-(4-methoxycarbonylaminophenyl)propionyl]piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-4-tert-butoxycarbonyl-2-[(6-carboxymethoxy-2-phenylpyrimidine-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-4-tert-butoxycarbonyl-2-[(2-phenyl-6-propoxyphene-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-tert-butoxycarbonyl-2-{[6-(2-hydroxyethoxy)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-2-[(6-benzyloxy-2-phenylpyrimidine-4-carbonyl)amino]-4-tert-butoxycarbonylmethyl}piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-4-tert-butoxycarbonyl-2-[(6-cyclopropylmethoxy-2-phenylpyrimidine-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-4-tert-butoxycarbonyl-2-[(6-cyclohexyloxy-phenylpyrimidine-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-4-tert-butoxycarbonyl-2-[(6-isopropoxy-2-phenylpyrimidine-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid:
ethyl ester of 4-{(S)-4-tert-butoxycarbonyl-2-[(6-methoxy-2-phenylpyrimidine-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-[2-[(6-cyclopentyloxy-2-phenylpyrimidine-4-carbonyl)amino]-3-(3-ethoxycarbonylmethoxy)propionyl]piperazine-1-carboxylic acid;
ethyl ester of 4-[2-[(6-cyclopentyloxy-2-phenylpyrimidine-4 carbonyl)amino]-3-(2-ethoxycarbonylmethoxy)propionyl]piperazine-1-carboxylic acid;
ethyl ester of 4-[(S)-2-[(6-cyclopentyloxy-2-phenylpyrimidine-4-carbonyl)amino]-2-(4-ethoxycarbonylmethoxy)acetyl]piperazine-1-carboxylic acid;
prop-2-injuly ester 4-{(S)-4-tert-butoxycarbonyl-2-[(6-cyclopentyloxy-2-phenylpyrimidine-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
butyl ether 4-{(S)-4-tert-butoxycarbonyl-2-[(6-cyclopentyloxy-2-phenylpyrimidine-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
isobutyl ether 4-{(S)-4-tert-butoxycarbonyl-2-[(6-cyclopentyloxy-2-phenylpyrimidine-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
2,2-dimethylpropionic ether 4-{(S)-4-tert-butoxycarbonyl-2-[(6-cyclopentyloxy-2-phenylpyrimidine-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
isopropyl ester 4-{(S)-4-tre is-butoxycarbonyl-2-[(6-cyclopentyl-hydroxy-2-phenylpyrimidine-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
tert-butyl ester 4-[(S)-(6 cyclopentyloxy-2-phenylpyrimidine-4-carbonyl)amino]-5-[4-(furan-2-carbonyl)piperazine-1-yl]-5-oxopentanoic acid;
phenyl ester 4-{(S)-4-tert-butoxycarbonyl-2-[(6-cyclopentyloxy-2-phenylpyrimidine-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
tert-butyl ester 5-((S)-4-benzylpiperazine-1-yl)-4-[(6-cyclopentyloxy-2-phenylpyrimidine-4-carbonyl)amino]-5-oxopentanoic acid;
benzyl ether of 4-{(S)-4-tert-butoxycarbonyl-2-[(6-cyclopentyloxy-2-phenylpyrimidine-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
tert-butyl ester 5-((S)-4-butylpiperazine-1-yl)-4-[(6-cyclopentyloxy-2-phenylpyrimidine-4-carbonyl)amino]-5-oxopentanoic acid;
tert-butyl ether (S)-4-[(6-cyclopentyloxy-2-phenylpyrimidine-4-carbonyl)amino]-5-oxo-5-[4-(propane-1-sulfonyl)piperazine-1-yl]-pentanol acid;
ethyl ester of 4-{(S)-4-tert-butoxycarbonyl-2-[(6-cyclopentyloxy-2-phenylpyrimidine-4-carbonyl)amino]butyryl}-3-methylpiperazin-1-carboxylic acid;
ethyl ester of 4-{(S)-4-tert-butoxycarbonyl-2-[(6-cyclopentyloxy-2-phenylpyrimidine-4-carbonyl)amino]butyryl}-2-methylpiperazin-1-carboxylic acid;
ethyl ester of 4-{(S)-4-tert-butoxycarbonyl-2-[(6-cyclopentyloxy-2-phenylpyrimidine-4-carbonyl)amino]butyryl}-TRANS-2,5-dimethylpiperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-4-tert-butoxycarbonyl the l-2-[(6-methylamino-2-phenylpyrimidine-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid:
ethyl ester of 4-{(S)-4-tert-butoxycarbonyl-2-[(2-phenyl-6-propylamino-pyrimidine-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-tert-butoxycarbonyl-2-[(6-isopropylamino-2-phenylpyrimidine-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-4-tert-butoxycarbonyl-2-[(6-butylamino-2-phenylpyrimidine-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-4-tert-butoxycarbonyl-2-[(6-isobutylamino-2-phenylpyrimidine-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-4-tert-butoxycarbonyl-2-[(6-cyclopropylamino-2-phenylpyrimidine-4-carbonyl)amino]butyryl]piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-4-tert-butoxycarbonyl-2-[(6-cyclopentylamine-2-phenylpyrimidine-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-4-tert-butoxycarbonyl-2-[(6-cyclohexylamino-2-phenylpyrimidine-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-tert-butoxycarbonyl-2-{[6-(etoxycarbonyl-methylamino)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-tert-butoxycarbonyl-2-{[6-(2-hydroxyethyl-amino)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-tert-butoxycarbonyl-2-{[6-(2-etoxycarbonyl-atrami is about)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-tert-butoxycarbonyl-2-{[6-(3-hydroxy-propylamino)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-tert-butoxycarbonyl-2-{[6-(3-tert-butoxy-carbonylcyanide)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-tert-butoxycarbonyl-2-{[6-(2-dimethylamino-ethylamino)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-tert-butoxycarbonyl-2-{[6-(3-dimethylamino-propylamino)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-tert-butoxycarbonyl-2-{[6-(2-morpholine-4-ylethylamine)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-tert-butoxycarbonyl-2-{[6-(3-morpholine-4-yl-propylamino)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-2-[(6-benzylamino-2-phenylpyrimidine-4-carbonyl)amino]-4-tert-butoxycarbonyl-butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-tert-butoxycarbonyl-2-{[2-phenyl-6-((S)-1-phenylethylamine)pyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-tert-butoxycarbonyl-2-{[2-phenyl-6-((K)-1 phenylethylamine)pyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl is a new ester of 4-((S)-4-tert-butoxycarbonyl-2-{[6-((S)-2-tert-butoxycarbonyl-1 phenylethylamine)-2-phenylpyrimidine-4-carbonyl]-amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-tert-butoxycarbonyl-2-{[6-((R)-2-tert-butoxycarbonyl-1 phenylethylamine)-2-phenylpyrimidine-4-carbonyl]-amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-4-tert-butoxycarbonyl-2-[(6-phenethylamine-2-phenylpyrimidine-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-tert-butoxycarbonyl-2-{[2-phenyl-6-(2-phenylpropylamine)pyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-tert-butoxycarbonyl-2-{[6-1,2-diphenyl-ethylamino)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-tert-butoxycarbonyl-2-{[2-phenyl-6-(TRANS-2-phenyl-cyclopropylamino)pyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-tert-butoxycarbonyl-2-{[6-(indan-1-ylamino)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-tert-butoxycarbonyl-2-{[6-((R)-indan-1-ylamino)-2-FeNi pyrimidin-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-tert-butoxycarbonyl-2-{[6-(indan-2-ylamino)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-4-tert-butoxycarbonyl-2-[(6-dimethylamino-2-phenylpyrimidine-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-2-[(6-azetidin the-1-yl-2-phenylpyrimidine-4-carbonyl)amino]-4-tert-butoxycarbonylmethyl}piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-4-tert-butoxycarbonyl-2-[(2-phenyl-6-pyrrolidin-1-Yeremey-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-4-tert-butoxycarbonyl-2-[(2-phenyl-6-piperidine-1-Yeremey-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-tert-butoxycarbonyl-2-{[6-(butylmethylamine)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-4-tert-butoxycarbonyl-2-[(2-phenyl-6-phenylamino-pyrimidine-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-tert-butoxycarbonyl-2-{[6-(4-forgenerating)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-4-tert-butoxycarbonyl-2-[(6-methyl-2-phenylpyrimidine-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-4-tert-butoxycarbonyl-2-[(6-isopropyl-2-phenylpyrimidine-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-{4-tert-butoxycarbonyl-2-[(6-butyl-2-phenylpyrimidine-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-4-tert-butoxycarbonyl-2-[(6-isobutyl-2-phenylpyrimidine-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-4-tert-butoxycarbonyl-2-[(6-cyclopropyl-2-phenylpyrimidine-4-carbonyl)amino]butyryl}piperazine-1-carbon is th acid;
ethyl ester of 4-{(S)-4-tert-butoxycarbonyl-2-[(6-cyclopentyl-2-phenylpyrimidine-4-carbonyl)amino]butyryl{piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-4-tert-butoxycarbonyl-2-[(2,6-diphenylpyridine-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-4-tert-butoxycarbonyl-2-[(2-phenyl-6-o-tolyl-pyrimidine-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-4-tert-butoxycarbonyl-2-[(2-phenyl-6-m-tolyl-pyrimidine-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-4-tert-butoxycarbonyl-2-[(2-phenyl-6-p-tolyl-pyrimidine-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-tert-butoxycarbonyl-2-{[6-(3-carboxyphenyl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-tert-butoxycarbonyl-2-{[6-(4-carboxyphenyl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-tert-butoxycarbonyl-2-{[2-(4-forfinal)-6-methylpyrimidin-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-tert-butoxycarbonyl-2-{[2-(3-forfinal)-6-methylpyrimidin-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-tert-butoxycarbonyl-2-{[2-(2-forfinal)-6-methylpyrimidin-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid is;
ethyl ester of 4-((S)-4-tert-butoxycarbonyl-2-{[2-(4-chlorophenyl)-6-methylpyrimidin-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-tert-butoxycarbonyl-2-{[2-(3-chlorophenyl)-6 methyl pyrimidine-4-carbonyl] amino} butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-tert-butoxycarbonyl-2-{[2-(2-chlorophenyl)-6-methylpyrimidin-4-carbonyl]amino }butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-4-tert-butoxycarbonyl-2-[(6-methyl-2-p-tolyl-pyrimidine-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-4-tert-butoxycarbonyl-2-[(6-methyl-2-m-tolyl-pyrimidine-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-tert-butoxycarbonyl-2-{[2-(4-methoxyphenyl)-6-methylpyrimidin-4-carbonyl]amino} butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-tert-butoxycarbonyl-2-{[2-(3-methoxyphenyl)-6-methylpyrimidin-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-[(S)-2-[(6-isopropylamino-2-fenspiride-4-carbonyl)amino]-3-(4-ethoxycarbonylphenyl)propionyl]piperazine-1-carboxylic acid;
ethyl ester of 4-[(S)-2-[(6-benzylamino-2-phenylpyrimidine-4-carbonyl)amino]-3-(4-ethoxycarbonylphenyl)propionyl]piperazine-1-carboxylic acid;
ethyl ester of 4-(S)-[2-[(2,6-diphenylpyridine-4-carbonyl)amino]-3-(4-ethoxycarbonylphenyl)propionyl]piperaz the n-1-carboxylic acid;
ethyl ester of 4-[(S)-2-[(6-cyclopropyl-2-phenylpyrimidine-4-carbonyl)amino]-3-(4-ethoxycarbonylphenyl)propionyl]piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-5-tert-butoxycarbonyl-2-[(6-isopropylamino-2-phenylpyrimidine-4-carbonyl)amino]pentanoyl}piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-2-[(6-benzylamino-2-phenylpyrimidine-4-carbonyl)amino]-5-tert-butoxycarbonylmethyl }piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-5-tert-butoxycarbonyl-2-[(2,6-diphenylpyridine-4-carbonyl)amino]pentanoyl}piperazine-1-karbonovoi acid;
ethyl ester of 4-{(S)-5-tert-butoxycarbonyl-2-[(6-cyclopropyl-2-phenylpyrimidine-4-carbonyl)amino]pentanoyl}piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[6-(2-methoxy-1-methylethylamine)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[6-(isopropylethylene)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-4-carboxy-2-[(6-morpholine-4-yl-2-phenylpyrimidine-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-4-carboxy-2-[(2-phenyl-6-thiazolidin-3-Yeremey-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[6-(4-hydroxypiperidine-1-yl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid is;
ethyl ester of 4-((S)-4-carboxy-2-{[6-(piperazine-1-yl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[6-(2-hydroxy-1-methylethylamine)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[6-(4-hydroxy-butylamino)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[6-(2-hydroxypropylamino)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-[(S)-4-carboxy-2-({2-phenyl-6-[(tetrahydro-furan-2-ylmethyl)amino]pyrimidine-4-carbonyl}amino)butyryl]piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[6-((R)-2-hydroxyethylpyrrolidine-1-yl)-2-phenylpyrimidine-4-carbonyl]amino)butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[6-((S)-2-hydroxyethylpyrrolidine-1-yl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[6-((R)-3-hydroxypyrrolidine-1-yl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[6-((R)-3-hydroxypyrrolidine-1-yl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-[(S)-4-carboxy-2-({2-phenyl-6-[(R)-(tetrahydro-furan-3-yl)amino]pyrimidine-4-carbonyl}amino)-butyryl]piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-4-carboxy-2-[(6-imidazol-1-yl-2-phenylpyrimidine-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-4-carboxy-2-[(2-phenyl-6-pyrazole-1-Yeremey-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[6-((S)-2-hydroxy-1-methylethylamine)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[6-((R)-2-hydroxy-1-
methylethylamine)-2-phenylpyrimidine-4-carbonyl]amino)butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[6-(2-hydroxy-1,1-dimethylethylamine)-2-vanillylamide-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[6-(TRANS-4-hydroxy-cyclohexylamino)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[6-(3-hydroxypiperidine-1-yl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[6-(2-hydroxyethylpiperazine-1-yl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[6-(TRANS-2-hydroxy-cyclohexylamino)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-4-carboxy-2-[(2-phenyl-6-propylsulfonyl-pyrimidine-4-carbonyl)amino]butyryl}is piperazin-1-carboxylic acid;
ethyl ester of 4-{(S)-4-carboxy-2-[(6-isopropylphenyl-2-phenylpyrimidine-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-4-carboxy-2-[(6-cyclopentylmethyl-2-phenylpyrimidine-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-4-carboxy-2-[(6-isopropylphenyl-2-phenylpyrimidine-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-4-carboxy-2-[(6-cyclohexylsulfamic-2-phenylpyrimidine-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-4-carboxy-2-[(6-ethoxycarbonylmethyl-2-phenylpyrimidine-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[6-(2-ethoxycarbonylethyl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-4-carboxy-2-[(6-carboxymethylchitin-2-phenylpyrimidine-4-carbonyl)amino]butyryl{piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[6-(2-carboxyethylidene)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-4-carboxy-2-[(2-phenyl-6-phenylsulfanyl-LinkedIn-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-2-[(6-benzylmethyl-2-phenylpyrimidine-4-carbonyl)amino]-4-carboxy-butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[6-(3-hydroxyprop-1-inyl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[6-(3-hydroxy-but-1-inyl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[6-(3-hydroxyben-1-inyl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[6-(3-hydroxy-3-methyl-but-1-inyl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[6-(3-hydroxypropyl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[6-(3-hydroxy-butyl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[6-(3-hydroxyphenyl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[6-(3-hydroxy-3-methyl-butyl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[6-((E)-3-hydroxy-but-1-enyl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-tert-butoxycarbonyl-2-{[6-(2-methoxy-1-methylethylamine)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid
ethyl ester of 4-((S)-4-tert-butoxycarbonyl-2-{[6-(isopropylethylene)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)-piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-4-tert-butoxycarbonyl-2-[(6-morpholine-4-yl-2-phenylpyrimidine-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-4-tert-butoxycarbonyl-2-[(2-phenyl-6-thiazolidin-3-Yeremey-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-tert-butoxycarbonyl-2-{[6-(4-hydroxypiperidine-1-yl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-tert-butoxycarbonyl-2-{[6-(piperazine-1-yl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-tert-butoxycarbonyl-2-{[6-(2-hydroxy-1-methylethylamine)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-tert-butoxycarbonyl-2-{[6-(4-hydroxy-butylamino)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-tert-butoxycarbonyl-2-{[6-(2-hydroxypropylamino)-2-phenylpyrimidine-4-carbonyl]amino}-butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-[(S)-4-tert-butoxycarbonyl-2-({2-phenyl-6-[(tetrahydro-furan-2-ylmethyl)amino]pyrimidine-4-carbonyl}amino)butyryl]piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-tert-bout xianbei-2-{[6-((R)-2-hydroxymethyl-pyrrolidin-1-yl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-tert-butoxycarbonyl-2-{[6-((S)-2-hydroxymethyl-pyrrolidin-1-yl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-tert-butoxycarbonyl-2-{[6-((S)-3-hydroxy-pyrrolidin-1-yl)-2-phenylpyrimidine-4-carbonyl]amino)butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-tert-butoxycarbonyl-2-{[6-((R)-3-hydroxy-pyrrolidin-1-yl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-[(S)-4-tert-butoxycarbonyl-2-({2-phenyl-6-[(R)-(tetrahydro-furan-3-yl)amino]pyrimidine-4-carbonyl}-amino)-butyryl]piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-4-tert-butoxycarbonyl-2-[(6-imidazol-1-yl-2-phenylpyrimidine-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-4-tert-butoxycarbonyl-2-[(2-phenyl-6-pyrazole-1-Yeremey-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-tert-butoxycarbonyl-2-{[6-((S)-2-hydroxy-1-methylethylamine)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-tert-butoxycarbonyl-2-{[6-((R)-2-hydroxy-1-methylethylamine)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-tert-butoxycarbonyl-2-{[6-(2-hydroxy-1,1-dimethylethylamine)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carbon is howling acid;
ethyl ester of 4-((S)-4-tert-butoxycarbonyl-2-{[6-(TRANS-4-hydroxy-cyclohexylamino)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-tert-butoxycarbonyl-2-{[6-(3-hydroxypiperidine-1-yl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-tert-butoxycarbonyl-2-{[6-(2-hydroxy-methylpiperidin-1-yl)-2-phenylpyrimidine-4-carbonyl]amino}-butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-tert-butoxycarbonyl-2-{[6-(TRANS-2-hydroxy-cyclohexylamino)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-4-tert-butoxycarbonyl-2-[(2-phenyl-6-propylsulfonyl-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-4-tert-butoxycarbonyl-2-[(6-isopropylphenyl-2-phenylpyrimidine-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-4-tert-butoxycarbonyl-2-[(6-cyclopentyl-effect-free remedy 2-phenylpyrimidine-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-4-tert-butoxycarbonyl-2-[(6-isopropylphenyl-2-phenylpyrimidine-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-4-tert-butoxycarbonyl-2-[(6-cyclohexyl-effect-free remedy 2-phenylpyrimidine-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid is;
ethyl ester of 4-{(S)-4-tert-butoxycarbonyl-2-[(6-etoxycarbonyl-methylsulfanyl-2-phenylpyrimidine-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-tert-butoxycarbonyl-2-{[6-(2-etoxycarbonyl-ethylsulfanyl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-4-tert-butoxycarbonyl-2-[(2-phenyl-6-phenyl-sulfanilamide-4-carbonyl)amino]butyryl} piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-2-[(6-benzylmethyl-2-phenylpyrimidine-4-carbonyl)amino]-4-tert-butoxycarbonylmethyl}piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-4-tert-butoxycarbonyl-2-[(6-ethinyl-2-phenylpyrimidine-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-tert-butoxycarbonyl-2-{[6-(3-hydroxy-prop-1-inyl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-tert-butoxycarbonyl-2-{[6-(3-hydroxy-but-1-inyl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-tert-butoxycarbonyl-2-{[6-(3-hydroxy-Penta-1-inyl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-tert-butoxycarbonyl-2-{[6-(3-hydroxy-3-methyl-but-1-inyl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-tert-BU is oxycarbonyl-2-{[6-(3-hydroxypropyl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-tert-butoxycarbonyl-2-{[6-(3-hydroxy-butyl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-tert-butoxycarbonyl-2-{[6-(3-hydroxy-pentyl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-tert-butoxycarbonyl-2-{[6-(3-hydroxy-3-methyl-butyl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-tert-butoxycarbonyl-2-{[6-((2)-3-hydroxy-but-1-enyl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[6-(4-oxo-cyclohex-1-enyl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[6-(4-oxo-cyclohexyl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[6-(4-hydroxy-cyclohex-1-enyl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[6-(4-hydroxy-cyclohexyl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-tert-butoxycarbonyl-2-{[6-(4-oxo-cyclohex-1-enyl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-tert-butoxycarbonyl-2-{[6-(4-oxo-cyclohexyl)-2-Fenrir midin-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[6-((S)-3-ethoxypyrrolidine-1-yl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[6-((5)-2-methoxy-1-methylethylamine)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[6-(4-methoxypiperidine-1-yl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[6-((R)-3-ethoxypyrrolidine-1-yl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[6-((R)-2-methoxy-1-methylethylamine)-2-phenylpyrimidine-4-carbonyl]amino[butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[6-(2-methoxypiperidine-1-yl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[6-((S)-2-methoxypiperidine-1-yl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[6-((R)-2-methoxypiperidine-1-yl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[6-(2-methoxy-1,1-dimethylethylamine)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[6-(4,5-dihydro-pyrazole-1-yl)-2-phenylpyrimidine-4-ka is bonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[6-(2-methyl-4,5-dihydro-imidazol-1-yl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazin-1-carboxylic acid;
ethyl ester of 4-{(S)-4-carboxy-2-[(2-phenyl-6-[1,2,4]triazole-1-Yeremey-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[6-(4-methylpyrazole-1-yl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[6-(3-methylpyrazole-1-yl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-4-carboxy-2-[(2-phenyl-6-[1,2,3]triazole-1-Yeremey-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-2-([6-(4-butyl-[1,2,3]triazole-1-yl)-2-phenylpyrimidine-4-carbonyl]amino}-4-carboxybutyl)piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-2-[(6-amino-2-phenylpyrimidine-4-carbonyl)amino]-4-carboxy-butyryl} piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[6-(cyclohexanecarbonyl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-[(S)-4-carboxy-2-({2-phenyl-6-[(thiophene-2-carbonyl)amino]pyrimidine-4-carbonyl}-amino)-butyryl]piperazine-1-carboxylic acid;
ethyl ester of 4-[(S)-4-carboxy-2-({6-[(furan-2-carbonyl)amino]-2-phenylpyrimidine-4-carbonyl}-amino)-butyryl]piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-carboxy-2-[(2-phenyl-6-phenylacetylamino-pyrimidine-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[2-phenyl-6-(3-phenyl-propionamido)pyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[6-(3-cyclopentyl-propionamido)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[6-(2,2-dimethyl-propionamido)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[2-phenyl-6-(2-propyl-pentanediamine)pyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-2-[(6-benzoylamine 2-phenylpyrimidine-4-carbonyl)amino]-4-carboxy-butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[6-(2-cyclopentyl-acetylamino)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[6-(2-methoxy-acetylamino)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[6-(cyclobutanecarbonyl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[6-(cyclopentanecarbonyl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-4-carboxy-2-[(6-pentanediamine-2-phenylpyrimidine-4-carbonyl)amino]butyryl}piperazine-1-carboxylic to the slots;
ethyl ester of 4-((S)-4-carboxy-2-{[6-(3-methylbutylamine)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[6-(cyclopropanecarbonyl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-2-[(6-acetylamino-2-phenylpyrimidine-4-carbonyl)amino]-4-carboxybutyl}piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-2-[(6-Butylimino-2-phenylpyrimidine-4-carbonyl)amino]-4-carboxy-butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-4-carboxy-2-[(6-isobutylamino-2-phenylpyrimidine-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-4-carboxy-2-[(2-phenyl-6-propionamido-pyrimidine-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[2-phenyl-6-(propane-1-sulfonylamino)pyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-4-carboxy-2-[(6-ethanolamine-2-phenylpyrimidine-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-2-[(6-benzosulfimide-2-phenylpyrimidine-4-carbonyl)amino]-4-carboxy-butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[2-phenyl-6-(propane-2-sulfonylamino)pyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2{[6-(4-oxo-4H-pyridin-1-yl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[6-(3-methyl-5-oxo-2,5-dihydro-pyrazole-1-yl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[6-(2-hydroxy-1-methyl-propyl an sulfanyl)-2-phenyl pyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[6-(2-hydroxypropanesulfonic)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-[(S)-2-({6-[(benzylmethylamine)methyl]-2-phenylpyrimidine-4-carbonyl}amino)-4-carboxy-butyryl]piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[6-(4-ethoxycarbonylpyrimidine-1-ylmethyl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[6-((S)-2-hydroxyethylpyrrolidine-1-ylmethyl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-]-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[6-(4-ethoxycarbonylpyrimidine-1-ylmethyl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[6-(3-hydroxypiperidine-1-ylmethyl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[6-(2-hydroxyethylpiperazine-1-ylmethyl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-4-carboxy-2-[(-morpholine-4-ylmethyl-2-phenylpyrimidine-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[6-((R)-3-hydroxypyrrolidine-1-ylmethyl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-4-carboxy-2-[(2-phenyl-6-piperidine-1-iletilerimde-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[6-(2,6-dimethyl-morpholine-4-ylmethyl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-[(S)-4-carboxy-2-({6-[(ethylmethylamino)methyl]-2-phenylpyrimidine-4-carbonyl}-amino)-butyryl]piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-4-carboxy-2-[(6-diethylaminomethyl-2-phenylpyrimidine-4-carbonyl)amino]butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-4-carboxy-2-[(2-phenyl-6-pyrrolidin-1-iletilerimde-4-carbonyl)amno]butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-4-carboxy-2-[(6-ethanallenhotel-2-phenylpyrimidine-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-4-carboxy-2-[(2-phenyl-6-phenylsulfanyl-methylpyrimidin-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-2-[(6-benzosulfimide-2-phenylpyrimidine-4-carbonyl)amino]-4-carboxybutyl } piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-4-carboxy-2-[(6-cyclopentylmethyl-2-phenylpyrimidine-4-carbonyl)amino]butyryl)piperazine-1-carboxylic key is lots;
ethyl ester of 4-{(S)-4-carboxy-2-[(6-cyclopentanecarbonyl-2-phenylpyrimidine-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-4-carboxy-2-[(2-phenyl-6-thiophene-3-Yeremey-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[6-(2-methoxyphenyl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[6-(4-methanesulfonyl-phenyl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-2-{[6-(4-acetylphenyl)-2-phenylpyrimidine-4-carbonyl]amino}-4-carboxybutyl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[6-(2-forfinal)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[6-(3-cyano-phenyl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[6-(3-forfinal)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[6-(4-methoxyphenyl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-4-carboxy-2-[(6-furan-3-yl-2-phenylpyrimidine-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-2-[(6-benzo[1,3]dioxol-5-yl-2-phenylpyrimidine-4-carbonyl) - Amin is]-4-carboxy-butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[6-(3-methoxyphenyl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-([6-(4-hydroxymethylene)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-4-carboxy-2-[(2-phenyl-6-thiophene-2-Yeremey-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[6-(4-cyanophenyl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[6-(3-chlorphen yl)-2-phenyl pyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-2-[(6-biphenyl-4-yl-2-phenylpyrimidine-4-carbonyl)amino]-4-carboxy-butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[2-phenyl-6-(1H-pyrazole-4-yl)pyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[2-phenyl-6-((E)-styryl)pyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[2-phenyl-6-(3-triptoreline)pyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-4-carboxy-2-[(2-phenyl-6-pyridin-3-Yeremey-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-4-carboxy-2-[(2-phenyl-6-pyridin-4-Yeremey-4-carbonyl)amino]butir the l}piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-4-carboxy-2-[(2-phenyl-6-thiazol-2-Yeremey-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-2-[(6-acetyl-2-phenylpyrimidine-4-carbonyl)amino]-4-carboxy-butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[6-(1-hydroxyethyl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[6-(1-methoxyethyl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[6-(1-ethoxyethyl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[6-(1-hydroxy-1-methylethyl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-etoxycarbonyl-2-{[6-(1-hydroxy-1-methylethyl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[6-(2-hydroxyethyl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[6-(2-methoxyethyl)-2-phenylpyrimidine-4-carbonyl]amino)butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[6-(2-hydroxy-cyclohexyl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[6-(2-methoxy-cyclohexyl)-2-phenyl shall eremein-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[6-(2-hydroxy-cyclopentyl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[6-(2-hydroxypropyl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[6-(2-methoxypropyl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[6-(3,6-dihydro-2H-Piran-4-yl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[2-phenyl-6-(tetrahydro-Piran-4-yl)pyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[6-(2-etoxycarbonyl-cyclohexyl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[6-(1-oxypyridine-3-yl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[6-((E)-2-etoxycarbonyl-vinyl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[2-phenyl-6-(tetrahydro-furan-2-ylmethyl)pyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[6-((E)-4-hydroxy-but-1-enyl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[2-phenyl-6-(tetrahydro-furan-3-yl)pyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[6-((E)-2-dimethylcarbamoyl-vinyl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-4-carboxy-2-[(6-cyano-2-phenylpyrimidine-4-carbonyl)amino]butyryl} piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[6-(1-hydroxypropyl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[6-(1-hydroxy-butyl)-2-phenylpyrimidine-4-carbonyl]amino}botril)piperazine-1-carboxylic acid;
ethyl ester of 4-({S}-4-carboxy-2- {[6-(hydroxyphenylethyl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[6-(2-hydroxy-2-phenylethyl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-4-carboxy-2-[(6-ethoxymethyl-2-phenylpyrimidine-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-4-carboxy-2-[(2-phenyl-6-cryptomaterial-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-2-[(6-tert-butyl-2-phenylpyrimidine-4-carbonyl)amino]-4-carboxy-butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-4-carboxy-2-[(6-phenoxy-2-phenylpyrimido the-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[2-phenyl-6-(pyridine-3-yloxy)pyrimidine-4-carbonyl]amino[butyryl)piperazine-1-carboxylic acid;
-(S)-5-(4-tert-butylcarbamoyl-1-yl)-4-[(6-cyclopentyloxy-2-phenylpyrimidine-4-carbonyl)amino]-5-oxopentanoic acid;
-(S)-4-[(6-cyclopentyloxy-2-phenylpyrimidine-4-carbonyl)amino]-5-(4-isopropylpiperazine-1-yl)-5-oxo-pentane acid;
-(S)-4-[(6-cyclopentyloxy-2-phenylpyrimidine-4-carbonyl)amino]-5-oxo-5-[4-(thiophene-2-carbonyl)piperazine-1-yl]pentane acid;
-(S)-5-(4-cyclopentanecarbonitrile-1-yl)-4-[(6-cyclopentyloxy-2-phenylpyrimidine-4-carbonyl)amino]-5-oxo-pentane acid;
-(S)-4-[(6-cyclopentyloxy-2-phenylpyrimidine-4-carbonyl)amino]-5-oxo-5-[4-(piperidine-1-carbonyl)piperazine-1-yl]-pentane acid;
ethyl ester of 4-(4-tert-butoxycarbonyl-2-{[6-((S)-3-methoxy-pyrrolidin-1-yl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-tert-butoxycarbonyl-2-{[6-((S)-2-methoxy-1-methylethylamine)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine - 1-carboxylic acid;
ethyl ester of 4-((S)-4-tert-butoxycarbonyl-2-{[6-(4-methoxypiperidine-1-yl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-(4-tert-butoxycarbonyl-2-{[6-((R)-3-ethoxypyrrolidine-1-yl)-2-phenylpyrimidine-4-carbonyl}amino}butyryl)piperazine-1-carb is new acid;
ethyl ester of 4-((S)-4-tert-butoxycarbonyl-2-{[6-((R)-2-methoxy-1-methylethylamine)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-tert-butoxycarbonyl-2-{[6-(2-methoxymethyl-piperidine-1-yl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-tert-butoxycarbonyl-2-{[6-((S)-2-methoxymethyl-pyrrolidin-1-yl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-tert-butoxycarbonyl-2-{[6-((R)-2-methoxymethyl-pyrrolidin-1-yl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-tert-butoxycarbonyl-2-{[6-(2-methoxy-1,1-dimethylethylamine)-2-phenylpyrimidine-4-carbonyl}amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-tert-butoxycarbonyl-2-{[6-(4,5-dihydro-pyrazole-1-yl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-tert-butoxycarbonyl-2-{[6-(2-methyl-4,5-dihydro-imidazol-1-yl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-4-tert-butoxycarbonyl-2-[(2-phenyl-6-[1,2,4]triazole-1-Yeremey-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid:
ethyl ester of 4-((S)-4-tert-butoxycarbonyl-2-{[6-(4-methylpyrazole-1-yl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-to benovoy acid;
ethyl ester of 4-((S)-4-tert-butoxycarbonyl-2-{[6-(3-methylpyrazole-1-yl}-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-2-{[6-(4-butyl-[1,2,3]triazole-1-yl)-2-phenylpyrimidine-4-carbonyl]amino}-4-tert-butoxycarbonyl-butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-2-[(6-amino-2-phenylpyrimidine-4-carbonyl)amino]-4-tert-butoxycarbonyl-butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-tert-butoxycarbonyl-2-{[6-(3-methyl-5-oxo-2,5-dihydro-pyrazole-1-yl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-4-tert-butoxycarbonyl-2-[(6-ethanallenhotel-2-phenylpyrimidine-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-4-tert-butoxycarbonyl-2-[(6-ethylsulfanyl-2-phenylpyrimidine-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-2-[(6-benzosulfimide-2-phenylpyrimidine-4-carbonyl)amino]-4-tert-butoxycarbonyl-butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-4-tert-butoxycarbonyl-2-[(6-cyclopentyl-sulfanilyl-2-phenylpyrimidine-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-4-tert-butoxycarbonyl-2-[(6-cyclopentane-sulfanilyl-2-phenylpyrimidine-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-Tret-butoxycarbonyl-2-[(2-phenyl-6-pyridin-3-Yeremey-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-4-tert-butoxycarbonyl-2-[(2-phenyl-6-pyridin-4-Yeremey-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-4-tert-butoxycarbonyl-2-[(2-phenyl-6-thiazol-2-Yeremey-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-2-[(6-acetyl-2-phenylpyrimidine-4-carbonyl)amino]-4-tert-butoxycarbonyl-butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-tert-butoxycarbonyl-2-{[6-(1-hydroxyethyl)-2-phenylpyrimidine-4-carbonyl]amino} butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-tert-butoxycarbonyl-2-{[6-(1-methoxyethyl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-tert-butoxycarbonyl-2-{[6-(1-ethoxyethyl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-tert-butoxycarbonyl-2-([6-(1-hydroxy-1-methylethyl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-tert-butoxycarbonyl-2-{[6-(2-hydroxyethyl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-tert-butoxycarbonyl-2-{[6-(2-methoxyethyl)-2-phenylpyrimidine-4-carbonyl]amino)butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-tert-butoxycarbonyl-2-{[6-(2-hydroxy-cyclohexyl)-2-phenylpyrimidine-4-carbonyl]and the Ino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-tert-butoxycarbonyl-2-{[6-(2-methoxy-cyclohexyl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-tert-butoxycarbonyl-2-{[6-(2-hydroxy-cyclopentyl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((5)-4-tert-butoxycarbonyl-2-{[6-(2-hydroxypropyl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-tert-butoxycarbonyl-2-{[6-(2-methoxypropyl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-tert-butoxycarbonyl-2-{[6-(3,6-dihydro-2H-Piran-4-yl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-tert-butoxycarbonyl-2-{[2-phenyl-6-(tetrahydro-Piran-4-yl)pyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-tert-butoxycarbonyl-2-{[6-(2-etoxycarbonyl-cyclohexyl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-tert-butoxycarbonyl-2-{[6-(1-oxypyridine-3-yl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-tert-butoxycarbonyl-2-{[6-((E)-2-ethoxycarbonylphenyl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-tre is-butoxycarbonyl-2-{[2-phenyl-6-(tetrahydro-furan-2-ylmethyl)pyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-tert-butoxycarbonyl-2-{[6-(3-hydroxy-2-methyl-propyl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-tert-butoxycarbonyl-2-{[2-phenyl-6-(tetrahydro-furan-3-yl)pyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-tert-butoxycarbonyl-2-{[6-((E)-2-dimethyl-carbarnoyl-vinyl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-tert-butoxycarbonyl-2-{[6-(1-hydroxypropyl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-tert-butoxycarbonyl-2-{[6-(1-hydroxy-butyl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-tert-butoxycarbonyl-2-{[6-(hydroxyphenyl-methyl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-tert-butoxycarbonyl-2-{[6-(2-hydroxy-2-phenylethyl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-4-tert-butoxycarbonyl-2-[(2-phenyl-6-cryptomaterial-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-2-[(6-tert-butyl-2-phenylpyrimidine-4-carbonyl)-amino]-4-tert-butyloxycarbonyl-butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-{(S)-4-tert-butoxycarbonyl-[(6-phenoxy-2-phenyl-pyrimidine-4-carbonyl)amino]butyryl}piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[6-(1-oxypyridine-2-yl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[6-(1-oxypyridine-4-yl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[6-(2-hydroxy-1,1-dimethylethyl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-tert-butoxycarbonyl-2-{[6-(1-oxypyridine-2-yl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-tert-butoxycarbonyl-2-{[6-(1-oxypyridine-4-yl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-tert-butoxycarbonyl-2-{[6-(2-hydroxy-1,1-dimethylethyl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-tert-butoxycarbonyl-2-{[6-{2-hydroxymethyl-cyclopropyl)-2-phenylpyrimidine-4-carbonyl]amino}butyryl)piperazine-1-carboxylic acid;
ethyl ester of 4-((S)-4-carboxy-2-{[6-(2-hydroxymethyl-cyclopropyl)-2-phenylpyrimidine-4-carbonyl]amino} butyryl)piperazine-1-carboxylic acid;
and their pharmaceutically acceptable salts

14. The compound of formula I according to claim 1 or its pharmaceutically acceptable salt for use as drugs having antagonistic activity on the wearing of the receptor P2Y 12.

15. Pharmaceutical composition having antagonistic activity against receptor P2Y12including an effective amount of at least one compound of formula I according to claim 1 or its pharmaceutically acceptable salt and a pharmaceutically acceptable carrier, diluent or excipient.

16. The use of the compounds of formula I according to claim 1 or its pharmaceutically acceptable salts for obtaining a medicinal product, which has antagonistic activity against receptor P2Y12.



 

Same patents:

FIELD: chemistry.

SUBSTANCE: method of obtaining compound of the formula VIII where R12 and R13 each are removable protective group where protective group R12 is more resistant to extraction by hydrolysis or hydration than R13. Method involves reaction of compound of the formula IX with relevant R12 donor compound selected out of anhydrides, halogenides, carbamates and N-hydroxysuccinimides.

EFFECT: improved method.

4 cl, 6 ex

FIELD: chemistry; medicine.

SUBSTANCE: invention relates to derivatives of 2-hydroxytetrahydrofurane , of general formula (I) , which possess ability to inhibit calpaines and/or ability to catch active oxygen forms and can be used to obtain medication, intended for inhibiting calpaines and/or lipid peroxidation.

EFFECT: medications possess higher efficiency.

9 cl, 64 ex

FIELD: chemistry; pharmacology.

SUBSTANCE: present invention refers to bioactive compounds of formula (Ic) , pharmaceutical compositions and application at cancer treatment, where R2-R7, X2, R, Q, G, J, L and M represent values estimated in invention formula and description.

EFFECT: production of compounds which can be used for anticancer medical product.

55 cl, 19 ex

FIELD: pharmaceutical chemistry.

SUBSTANCE: invention relates to compounds of general formula: , wherein R1 represents phenyl-С16-alkyl group or 1-naphthyl-С16-alkyl group; R2 biologically labile ether forming group in the form of pharmaceutically acceptable metal salt, which is selected from lithium, calcium, magnesium, and zinc slats; and also to a method for preparing above-defined compounds and to pharmaceutical composition containing salts according to this invention. These compounds are used in treatment cardiac diseases or hypertension, in improvement of gastrointestinal blood circulation, and in treatment and prevention of cardiac disturbances induced by adriamicyn and analogous antitumor agents.

EFFECT: increased assortment of pharmaceutically active compounds of benzazepin series.

15 cl, 2 tbl, 5 ex

Peptide compounds // 2281955

FIELD: chemistry of peptides, medicine, pharmacy.

SUBSTANCE: invention relates to compound of the formula (I): wherein R1 represents benzofuranyl substituted with halogen atom or styryl substituted with halogen atom; R2 represents substituted hydroxyl substituted with mercapto-group or substituted sulfonyl, or its pharmaceutically acceptable salts. Compound of the formula (I) and its pharmaceutically acceptable salts possess the strong inhibitory effect on production of nitrogen oxide (NO) and can be useful in prophylaxis and/or treatment of NO-mediated diseases in humans and animals.

EFFECT: valuable medicinal and biochemical properties of compounds.

The invention relates to a group of compounds of General formula (I) high degree of purification

The invention relates to a derivative of D-Proline General formula

< / BR>
or

< / BR>
where R is SH, benzyl or phenyl, optionally substituted by a hydroxy-group or a lower alkoxygroup, or a group of the formula

< / BR>
R1is hydrogen or halogen; X represents -(CH2)n-; -CH(R2)(CH2)n-; -CH2O(CH2)n-; CH2NH-; benzyl, -C(R2)=CH-; CH2CH (OH)- or thiazol-2,5-diyl; Y represents-S -; (CH2)n; -O-; -NH-; -N (R2)-; -CH=CH-; -NHC(O)NH-; -N(R2)C(O)N(R2)-; -N[CH2WITH6H3(OCH3)2]-; -N(CH2WITH6H5)-; -N(CH2WITH6H5)C(O)N(CH2WITH6H5)-; -N(alkoxyalkyl)-; -N(cyclooctylmethyl)-; 2,6-pyridyl; 2,5-furanyl; 2,5-thienyl; 1,2-cyclohexyl; 1,3-cyclohexyl; 1,4-cyclohexyl; 1,2-naphthyl; 1,4-naphthyl; 1,5-naphthyl; 1,6-naphthyl or diphenylene; 1,2-phenylene; 1,3-phenylene or 1,4-phenylene, where phenylenebis group optionally substituted by 1-4 substituents selected from the group comprising halogen, lower alkyl, lower alkoxygroup, the hydroxy-group, carboxypropyl, -COO-lower thiazolyl, 2-oxo[1,2,3,5] oxadiazolyl, 5-thioxo[1,2,4]oxadiazolyl and 5-tert-butylsulfonyl[1,2,4] oxadiazolyl; X' represents -(CH2)n-; (CH2)nCH(R2)-; -(CH2)nOCH2-; -NHCH2-; benzyl, -CH= C(R2)-; -CH(OH)CH2or thiazol-2,5-diyl; R2denotes lower alkyl, lower alkoxygroup or benzyl and n = 0-3, their pharmaceutically acceptable salts, mono - and diesters, except (R)-1-[(R)- and (R)-1-[(S)-3-mercapto-2-methylpropionyl] pyrrolidin-2-carboxylic acid; medicinal product with amyloidoses activity, and the method of obtaining these derivatives

The invention relates to new derivatives of dipeptides with pharmacological activity, and the way they are received, and may find application in medicine

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to novel amide derivatives of general formula [1] in any of versions (A) or (B), or its pharmaceutically acceptable salt, which possess properties of tyrosinkinase BCR-ABL inhibitor. Amide derivative of general formula [1] represents compound: , where according to Version (A) R1 represents any of the following groups (1)-(3): (1) -) -CH2-R11 [R11 represents saturated 4-6 member nitrogen-containing heterocyclic group, optionally containing additional nitrogen atom; saturated 5-6-member nitrogen-containing heterocyclic group, optionally containing additional nitrogen atom, which is substituted by group selected from group, consisting of oxo, -CH2-R111 (R111 represents saturated 5-member nitrogen-containing heterocyclic group), saturated 5-member nitrogen-containing heterocyclic group, aminomethyl, monoalkylaminomethyl, dialkylaminomethyl and (5-methyl-2-oxo-1,3-Dioxol-4-yl)methyl, and in addition, can be substituted by 1 or 2 similar or different substituents, selected from group, consisting of (C1-C4)alkyl, (C1-C4 alkoxycarbonyl, halogen, halogen(C1-C4)alkyl, hydroxy(C1-C4)alkyl, amino, carbamoyl], (2) -O-R12 [R12 represents saturated 4-6-member nitrogen-containing heterocyclic group]; and (3) - CH=R13 [R13 represents saturated 4-6-member nitrogen-containing heterocyclic group, which can contain additional nitrogen atom, and which can be substituted by 1-3 similar or different substituents, selected from group, consisting of oxo, (C1-C4)alkyl]; R2 represents (C1-C4)alkyl, halogen, halogen(C1-C4)alkyl, hydroxy(C1-C4)alkyl, (C1-C4)alkoxy and carbamoyl; R3 represents hydrogen, halogen; Het1 represents any of groups with the following chemical formulae [4] and [6]: [4] [6] [19] [10] Het2 represents pyridyl or pyrimidinyl. According to Version (B) R1 represents -CH2-R14 [R14 represents saturated 4-6-member nitrogen-containing heterocyclic group, optionally containing additional nitrogen atom; saturated 5-6-member nitrogen-containing heterocyclic group, which can be substituted by 1-3 similar groups, selected from (C1-C4)alkyl] R2 represents (C1-C4)alkyl, halogen, halogen(C1-C4)alkyl, hydroxy(C1-C4)alkyl, (C1-C4)alkoxy, (C1-C4)alkoxy (C1-C4)alkyl, (C1-C4)alkoxycarbonyl, (C1-C4)acyl, amino, mono(C1-C4)alkylamino, di(C1-C4)alkylamino, nitro, carbamoyl, mono(C1-C4)alkylcarbamoyl, di(C1-C4)alkylcarbamoyl or cyano; R3 represents hydrogen or halogen; Het1 represents any of groups with the following chemical formulas [9] and [10], Het2 represents pyridyl.

EFFECT: invention can be applied for treatment of chronic myeloleukosis, acute lymphoblastic leukosis and acute myeloblastic leukosis.

6 cl, 89 ex, 3 tbl

FIELD: chemistry.

SUBSTANCE: invention relates to novel compounds of formula (I) or pharmaceutically acceptable salts thereof, having CRP receptor antagonist activity. In formula (I) R1 denotes C3-C8 alkyl, optionally substituted with hydroxyl; phenyl optionally substituted with 1-3 substitutes selected from halogen, nitro, amino, hydroxyl, C1-C4 alkoxy, C1-C4 alkyl, optionally substituted with hydroxyl or C1-C4 alkylamino; naphthyl; C-bonded 5-6-member heteroaryl with 1-2 heteroatoms selected from S, N or O, optionally substituted with C1-C4 alkyl, C1-C4 alkoxy or acetyl; N-bonded 5-member heteroaryl with 1-2 heteroatoms selected from N, optionally substituted with 1-3 substitutes selected from C1-C4 alkyl or phenyl; R2 denotes phenyl, optionally substituted with 1-3 substitutes selected from C1-C4 alkyl, halogenC1-C4alkyl, C1-C4 alkoxy, halogenC1-C4alkoxy, halogen, hydroxy, di(C1-C4 alkyl)amino or di(C1-C4 alkyl)aminocarbonyl; or a heterocyclic group which is pyridyl, optionally substituted with 1-3 substitutes selected from C1-C4 alkyl, C1-C4 alkoxy or di(C1-C4 alkyl)amino; X denotes -NR3-, where R3 denotes C1-C4 alkyl, optionally substituted with hydroxyl, carboxyl or C1-C4 alkoxycarbonyl; Y1 denotes CR3a, where R3a denotes hydrogen, halogen, cyano, hydroxy, C1-C4 alkyl, optionally substituted with hydroxyl or halogen, C1-C4 alkoxy optionally substituted with halogen; Y2 denotes CR3b, where R3b denotes hydrogen or halogen; Y3 denotes N or CR3c, where R3c denotes hydrogen; and Z denotes O or -NR4-, where R4 denotes hydrogen.

EFFECT: invention also pertains to a method of producing compounds of formula (I), a pharmaceutical composition, an inhibiting method, CRF receptor antagonists and use thereof to prepare a medicinal agent.

25 cl, 9 tbl, 163 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to compounds of formula (Ia) or their pharmaceutically acceptable salts, tautomers, or N-oxides, for use in prevention or treatment of unhealthy conditions or diseases, mediated with cyclin-dependent kinase and glycogen synthase-kinase-3, such as cancerous diseases. In formula (Ia) X stands for group R1-A-NR4; A stands for link, C=O, or NRg(C=O, where R8 stands for hydrogen or C1-3 alkyl; Y stands for link or alkylene chain, made of 1, 2 or 3 atoms of carbon; R1 stands for carbocyclic or heterocyclic group, containing from 3 to 12 circular units; or saturated C1-8hydrocarbyl group, optionally substituted with one or more substituents selected from halogen (for instance, fluorine), hydroxygroups, C1.4alkoxygroups, and carbocyclic or heterocyclic groups, and where 1 or 2 atoms of hydrocarbyl group carbon may be optionally substituted with atom or group selected from O, S, NH, SO, SO2; R2 stands for hydrogen or methyl; R3 is selected from hydrogen and carbocyclic or heterocyclic groups, containing from 3 to 6 circular units; and R4 stands for hydrogen or methyl. Specified carbocyclic and heterocyclic groups are determined in formula of invention and may be optionally substituted with groups specified in invention formula. Objects of invention are also a pharmaceutical composition based on proposed compounds, their application to produce medicinal agents and methods of their application.

EFFECT: production of pharmaceutical composition based on proposed compounds for use in prevention or treatment of unhealthy conditions or diseases, mediated with cyclin-dependent kinase and glycogen synthase-kinase-3, such as cancerous diseases.

48 cl, 6 tbl, 254 ex

Chemical compounds // 2405780

FIELD: medicine, pharmaceutics.

SUBSTANCE: present invention refers to new compounds of formula (I): , in which: R1 and R2 are independently specified from hydrogen, C1-6alkyl, C1-6alkoxy and cyclopropyl; X1, X2 and X3 independently represent =N- or =CR10; R3 and R10 are independently specified from hydrogen, halogen, nitro, cyano, amino, carboxy, carbamoyl, C1-6alkyl, N-(C1-6alkyl)amino, N,N(C1-6alkyl)2amino, C1-6alkanoylamino, C1-6alkoxycarbonyl; R4 represents hydrogen; R5 and R6 are independently specified from hydrogen, hydroxy and C1-6alkyl where R5 and R6 independently can be optionally substituted in carbon atom with one or more R16 where R16 represents hydroxy; A represents a single link or C1-2alkylene; where specified C1-2alkylene can be optionally substituted with one or more R18; the ring C represents a saturated, partially saturated or unsaturated mono- or bicyclic ring containing 5 or 6 atoms in which at least one atom can be specified from nitrogen, sulphur or oxygen which can be linked with carbon or nitrogen atom where the -CH2- group can be optionally substituted with -C(O)- and ring sulphur atom can be optionally oxidised to produce S-oxide; R7 is specified from halogen and C1-6alkyl where R7 can be optionally substituted in carbon atom with halogen; n is equal to 0.1 or 2; where R7 values can be equal or different; and R18 is independently specified from halogen and hydroxy; or its pharmaceutically acceptable salt. Also the invention refers to their pharmaceutical compositions and methods for preparation and application thereof for cancer treatment.

EFFECT: preparation of new compounds which can find application for cancer treatment.

23 cl, 96 ex

FIELD: chemistry.

SUBSTANCE: invention describes novel potassium or hydrazinium salts of 4-dinitromethyl-1,2,3-triazoles of general formulae V-VIII: V, VI VII, VIII, where Kat+ =K+ (V,VII), NH2NH3+ (VI;VIII).

EFFECT: higher herbicidal activity.

1 cl, 2 tbl, 4 ex

FIELD: chemistry.

SUBSTANCE: invention relates to pyrrole derivatives of formula (I): , where R1 denotes hydrogen; R2 denotes adamantine which is unsubstituted or substituted with a hydroxy group or halogen; R3 denotes trifluoromethyl, pyrazole, triazole, piperidine, pyrrolidine, hydroxymethylpiperidine, benzylpiperazine, hydroxypyrrolidine, tert-butylpyrrolidine, hydroxyethylpiperazine, hydroxypiperidine or thiomorpholyl group; R4 denotes cyclopropyl, tert-butyl, -CH(CH3)2CH2OH, methyl, -CF3 or -(CH2)nCF3 group, where n equals 1 or 2; R5 denotes hydrogen or lower alkyl which is unsubstituted or substituted with a halogen, as well as pharmaceutically acceptable salts thereof.

EFFECT: compounds and pharmaceutical compositions containing said compounds can inhibit 11β-hydroxysteroid dehydrogenase of the form 1 (11-BETA-HSD-1) and can be used to treat diseases such as type II sugar diabetes type and metabolic syndrome.

17 cl, 99 ex, 1 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to compounds of formula I: and their pharmaceutically acceptable salts, in which R1-R4 have values, given in item 1 of invention formula. Said compounds possess inhibiting activity with respect to 11-beta-hydroxysteroid-dehydrogenase and can be applied for production of medications, intended for treatment and prevention of diabetes, especially, diabetes of II type, obesity, malnutrition and hypertension.

EFFECT: development of efficient method of obtaining formula I compounds and based on them pharmaceutical composition.

25 cl, 1 tbl, 149 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to medication, reducing desire for alcohol, which represents substituted 1H-benzimidazoles of general formula 1 or their pharmaceutically acceptable salts and/or hydrates, pharmaceutical composition, and medication on their basis. Compounds can be applied in treatment of alcohol abuse with application of ethanol-containing products, if necessary, together with antidepressants. In compounds of general formula 1 , where: W represents sulfur atom or group S=O; R1 represents one or more substituents, selected from hydrogen, halogen, C1-C4alkyl, C1-C4alkyloxy, optionally substituted 5-6-member azaheterocyclyl with 1-2 atoms of nitrogen and/or oxygen in cycle; R2 represents atom of hydrogen or optionally substituted C1-C4alkyl; R3 and R4 independently on each other represent optionally similar substituents, selected from hydrogen, optionally substituted C1-C4alkyl, C3-C6cycloalkyl; R5 represents alkyl substituent, selected from hydrogen or optionally substituted C1-C7alkyl, C1-C7alkenyl, C1-C4alkynyl, optionally substituted phenyl, optionally substituted 5-6-member heterocyclyl with 1-3 heteroatoms, selected from nitrogen, oxygen and sulfur, possibly condensed with benzene ring; C1-C4-alkoxycarbonyl, optionally substituted amino carbonyl, or group CR3R4R together stands for group , where Alk stands for C1-C4alkyl.

EFFECT: medication allows to reduce symptoms of alcohol abuse considerably as compared with earlier known compounds and does not produce unfavorable effect on liver function.

12 cl, 3 tbl, 2 ex, 1 dwg

FIELD: chemistry.

SUBSTANCE: invention relates to novel compounds of formula (I), specifically compounds of formula (Ia) which have inhibiting activity during activity of kinase selected from Abl, BCR-AbI, PDGF-R, trkB, c-SRC, BMX, FGFR3, b-RAF, SGK, Tie2, Lck, JNK2a2, MKK4, c-RAF, MKK6, SAPK2a and SAPK2P and pharmaceutical compositions containing such compounds. In the compound of formula I, Ia, m and n are equal to 0; R1 denotes XNR5R6, where X denotes a bond; R5 is selected from hydrogen, C1-6alkyl, phenyl, C5-10heteroaryl-C0-4alkyl, C3-6cycloalkyl and C3-10heterocycloalkyl-C0-4alkyl, where the heteroaryl and heterocycloalkyl contain 1-2 heteroatoms selected from nitrogen and oxygen; and R6 is selected from hydrogen and C1-6alkyl; or R5 and R6 together with the nitrogen atom with which both are bonded form a heteroaryl or heterocycloalkyl; where any of phenyl, heteroaryl, cycloalkyl and heterocycloalkyl, R5 or a combination of R5 and R6 can be optionally substituted with 1-3 radicals independently selected from a halogen group, C1-6alkyl, C1-6alkoxy group, halogen-substituted alkyl, -XNR7R8, -XOR7, -XR8, -XC(O)NR7R8, -XC(O)NR7XNR7R8, -XNR7C(O)R8, -XR9; where X denotes a bond or C1-4alkylene; R7 and R8 are independently selected from a group consisting of hydrogen and C1-4alkyl;and R8 is selected form C5-6heterocycloalkyl and C5-6heteroaryl; where said heterocycloalkyl or heteroaryl contain 1-2 heteroatoms selected from nitrogen and oxygen, and said heterocycloalkyl or heteroaryl in R8 is optionally substituted with a radical selected from a group consisting of C1-4alkyl and XOR7; R3 denotes -NR10R11; where R10 denotes hydrogen; R11 denotes phenyl; where phenyl in R11 is optionally substituted with 1-3 radicals selected from a halogen group, C1-6alkyl, C1-6alkoxy group, halogen-substituted alkyl, halogen-substituted alkoxy group, -NR12C(O)R13, -NR12C(O)NR12R13 and -NR12S(O)0-2R13; where R12 denotes hydrogen; R13 is selected from phenyl, C5-6heteroaryl and C5-6heterocycloalkyl; where any of phenyl, heteroaryl, cycloalkyl or heterocycloalkyl contains 1-2 heteroatoms selected from nitrogen and oxygen, and said heterocycloalkyl or heteroaryl in R13 is substituted with 1-3 radicals independently selected from a halogen group, C1-6alkyl, halogen-substituted C1-6alkyl, C1-6alkoxy group, halogen-substituted C1-6alkoxy group, -XNR7R8, phenyl-C0-4alkyl, C5-6heteroaryl-C0-4alkyl, C5-6heterocycloalkyl-C0-4alkoxy group and C5-6heterocycloalkyl-C0-4alkyl; where X, R7 and R8 are described above, and where any of the phenyl, heteroaryl or heterocycloalkyl fragments contain 1-2 heteroatoms selected from nitrogen and oxygen, and said heterocycloalkyl or heteroaryl in R13 optionally further substituted with 1-3 radicals independently selected from a halogen group, C1-6alkyl, halogen-substituted C1-6alkyl, hydroxy-substituted C1-6alkyl, C1-6alkoxy group; R15 and R16 are selected from phenyl substitutes given in values of R11 and R12 for formula I compounds.

EFFECT: compounds can be used to treat or prevent such diseases as proliferative disorders, and diseases resulting from anomalous activation of the immune and nervous systems.

8 cl, 1 tbl, 1 dwg, 1 ex

FIELD: chemistry.

SUBSTANCE: invention relates to novel 1-substituted-3-[(1E)-1-alkenyl]-4-(5-alkoxy-1,2-dimethyl-1H-indol-3-yl)-1H-pyrrole-2,5-diones of general formula

, where R1=C1-C6alkyl, R2=C1-C6 alkyl, R3=CH2C6H5, C6H5.

EFFECT: obtaining novel compounds which can be used as fluorescent photochromes.

4 cl, 1 tbl, 2 ex

FIELD: chemistry.

SUBSTANCE: invention relates to a method of producing a compound of formula 1a, where X denotes a halogen or C1-C4halogenalkyl; Z denotes N or CR9; each R5 independently denotes halogen or C1-C4halogenalkyl; R9 denotes H, halogen or C1-C4halogenalkyl; R10 denotes H or C1-C4alkyl; and n is an integer from 0 to 3, involving bringing 2-pyrazoline of formula 2a, where X, Z, R5, R9, R10 and n assume values given above, into contact with bromine in a medium of a suitable inert organic solvent at temperature 80-180°C.

EFFECT: obtaining pyrazoles of formula 1a with high output and purity.

7 cl, 2 tbl, 3 ex

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