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DERIVATIVES OF PROPANOIC ACID INHIBITING THE UNION OF INTEGRINS TO ITS RECEPTORS.

机译:禁止整合素与其受体结合的丙酸的衍生物。

摘要

A compound selected from the group consisting of: (3S) -3 - {[(2S) -2- (3-benzyl-5-methyl-2-oxopyridin-1 (2H) -yl) hexanoyl] -amino} - 3- (3 '', 4 '' - dimethoxy-1-, 1 '' - biphenyl-4-yl) propanoic acid, (3S) -3 - ({(2S) -2- [3- (2-chlorobenzyl ) -5-methyl-2-oxopyridin-1 (2H) -yl] -hexanoyl} amino) -3- (3 '', 4 '' - dimethoxy-1,1''biphenyl-4-yl) propanoic acid, acid (3S) -3- (1,1 '' - biphenyl-4-yl) -3 - ({(2S) -2- [3- (2-chloro-6-methylbenzyl) -5-methyl-2-oxopyridin -1 (2H) -yl] hexanoyl} amino) propanoic acid, (3S) -3 - {[(2S) -2- (3-benzyl-5-methyl-2-oxopyridin-1 (2H) -yl) hexanoyl ] -amino} -3- (1,1 '' - biphenyl-4-yl) propanoic acid, (3S) -3- (1,1 '' - biphenyl-4-yl) -3 - ({(2S) -2- [3- (2-Chlorobenzyl) -5-methyl-2-oxopyridin-1 (2H) -yl] hexanoyl} amino) propanoic acid, (3S) -3 - {[(2S) -2- (3 -benzyl-5-methyl-2-oxopyridin-1 (2H) -yl) hexanoyl] -amino} -3- (4 '' - methyl-1,1 '' - biphenyl-4-yl) propanoic acid, (3S ) -3 - ({(2S) -2- [3- (2-Chlorobenzyl) -5-methyl-2-oxopyridin-1 (2H) -yl] -hexanoyl} amino) -3- (4 '' - methyl -1,1-biphenyl- 4-yl) propanoic acid, (3S) -3 - ({(2S) -2- [3- (2-chloro-6-methylbenzyl) -5-m ethyl-2-oxopyridin-1 (2H) -yl] hexanoyl} amino) -3- (4 '' - methyl- 1,1 '' - biphenyl-4-yl) propanoic acid, (3S) -3 - {[ (2S) -2- (3-Benzyl-5-methyl-2-oxopyridin-1 (2H) -yl) hexanoyl] -amino} -3- (2``, 6 '' - dimethoxy-1,1 '' -biphenyl-4-yl) propanoic acid, (3S) -3 - ({(2S) -2- [3- (2-chlorobenzyl) -5-methyl-2-oxopyridin-1 (2H) -yl] -hexanoyl} amino ) -3- (2``, 6 '' - dimethoxy-1,1''biphenyl-4-yl) propanoic acid, (3S) -3 - ({(2S) -2- [3- (2-chloro -6-methylbenzyl) -5-methyl-2-oxopyridin-1 (2H) -yl] hexanoyl} amino) -3- (2 '', 6 '' - dimethoxy-1,1 '' - biphenyl-4-yl ) propanoic acid (3S) -3 - {[(2S) -2- (3-benzyl-5-methyl-2-oxopyridin-1 (2H) -yl) hexanoyl] -amino} -3- (1,1 '' -biphenyl-3-yl) propanoic acid (3S) -3- (1,1 '' - biphenyl-3-yl) -3 - ({(2S) -2- [3- (2-chlorobenzyl- 5-methyl-2-oxopyridin- (2H) -yl] hexanoyl} amino) propanoic acid, (3S) -3- (1,1 '' - biphenyl-3-yl) -3 - ({(2S) -2 - [3- (2-Chloro-6-methylbenzyl) -5-methyl-2-oxopyridin-1 (2H) -yl] hexanoyl} amino) propanoic acid, (3S) -3 - [(2S) -2- ( 3-Benzyl-5-methyl-2-oxopyridin-1 (2H) -yl) hexanoyl] -amino} -3- (2 '' - methoxy-1,1 '' - biphenyl-3-yl) propanoic acid (3S) -3 - ({(2S) -2- [3- (2-Chlorobenzyl) -5-methyl-2-oxopyridin-1 (2H) -yl] -hexanoyl} amino) -3- (2 '' -methoxy-1,1 '' - biphenyl-3-yl) propanoic acid, (3S) -3 - ({(2S) -2- [3- (2-chloro-6-methylbenzyl) -5-methyl-2 -oxopyridin-1 (2H) -yl] hexanoyl} amino) -3- (2 '' - methoxy-1,1-biphenyl-3-yl) propanoic acid (3S) -3 - ({(2S) -2 - [3- (2-Fluoro-6-methoxybenzyl) -5-methyl-2-oxopyridin-1 (2H) -yl] hexanoyl} amino) -3- (4-methylphenyl) propanoic acid, (3S) -3- ({(2S) -2- [3- (2,6-Dimethylbenzyl) -5-methyl-2-oxopyridin-1 (2H) -yl] hexanoyl} amino) -3- (4-methylphenyl) propanoic acid, ( 3S) -3 - ({(2S) -2- [3- [3,5-dimethylbenzyl) -5-methyl-2-oxopyridin-1 (2H) -yl] -hexanoyl} amino) -3- (4- methylphenyl) propanoic acid, (3S) -3 - ({(2S) -2- [3- [2,6-dichlorobenzyl) -5-methyl-2-oxopyridin-1 (2H) -yl] hexanoyl} amino) - 3- (4-methylphenyl) propanoic acid, 39 null ES 2 321 059 T3 (3S) -3 - ({(2S) -2- [3- (2-chloro-6-fluorobenzyl) -5-methyl-2- oxopyridin-1 (2H) -yl] hexanoyl} amino) -3- (4-methylphenyl) propanoic acid (3S) -3 - ({(2S) -2- [3- (2,6-difluorobenzyl) -5 -methyl-2-oxopyridin-1 (2H) -yl] -hexanoyl} amino) -3- (4-methylphenyl) propanoic acid, (3S) -3- (1,3-benzodioxol-5-yl) -3 - ({(2S) -2- [3- (2,6-difluorobenzyl) -5-methyl -2-oxopyridin-1 (2H) -yl] hexanoyl} amino) propanoic acid, (3S) -3- (1,3-benzodioxol-5-yl) -3 - ({(2S) -2- [3- (2-Chloro-6-fluorobenzyl) -5-methyl-2-oxopyridin-1 (2H) -yl] hexanoyl} amino) propanoic acid, (3S) -3- (1,3-benzodioxol-5-yl) - 3 - ({(2S) -2- [3- [2,6-dichlorobenzyl) -5-methyl-2-oxopyridin-1 (2H) -yl] hexanoyl} amino) propanoic acid, (3S) -3- ( 1,3-benzodioxol-5-yl) -3 - ({(2S) -2- [3- (2,6-dimethylbenzyl) -5-methyl-2-oxopyridin-1 (2H) -yl] hexanoyl} amino ) propanoic acid (3S) -3- (1,3-benzodioxol-5-yl) -3 - ({(2S) -2- [3- (3,5-dimethylbenzyl) -5-methyl-2-oxopyridin -1 (2H) -yl] hexanoyl} amino) propanoic acid, (3S) -3- (1,3-benzodioxol-5-yl) -3 - ({(2S) -2- [3- (2-fluoro -6-methoxybenzyl) -5 methyl-2-oxopyridin-1 (2H) -yl] hexanoyl} amino) propanoic acid, (3S) -3 - ({(2S) -2- [3- (2-chlorobenzyl) - 5-methyl-2-oxopyridin-1 (2H) -yl] -hexanoyl} amino) -3- (3,4-diethoxyphenyl) propanoic acid (3S) -3- (3,4-diethoxyphenyl) -3- ( {(2S) -2- [3- (2,6-difluorobenzyl) -5-me til-2-oxopyridin-1 (2H) -yl] hexanoyl} amino) propanoic acid, (3S) -3 - ({(2S) -2- [3- (2,6-difluorobenzyl) -5-methyl-2 -oxopyridin-1 (2H) -yl] hexanoyl} amino) -3- (3-ethoxyphenyl) propanoic acid, (3S) -3 - ({(2S) -2- [3- (2-chloro-6-fluorobenzyl ) -5-methyl-2-oxopyridin-1 (2H) -yl] hexanoyl} amino) -3- (3-ethoxyphenyl) propanoic acid, (3S) -3 - ({(2S) -2- [3- ( 2-Chlorobenzyl) -5-methyl-2-oxopyridin-1 (2H) -yl] -3-methylbutanoyl} amino) -3- (4-methylphenyl) propanoic acid, (3S) -3 - ({(2S) - 2 [3- (2-Chlorobenzyl) -5-methyl-2-oxopyridin-1 (2H) -yl] -4-methylpentanoyl} -amino) -3- (4-methylphenyl) propanoic acid, (3S) -3- (1,3-benzodioxol-5-yl) -3 - ({(2S) -2- [3- (2-chlorobenzyl) -5-methyl-2-oxopyridin-1 (2H) -yl] -4-methylpentanoyl } amino) propanoic acid, (3S) -3- (1,3-benzodioxol-5-yl) -3 - ({(2S) -2- [3- (2-chlorobenzyl) -5-methyl-2-oxopyridine -1 (2H) -yl] -3-methylbutanoyl} amino) propanoic acid, (3S) -3- (1,3-benzodioxol-5-yl) -3 - ({(2S) -2- [3- ( 2-Chlorobenzyl) -5-methyl-2-oxopyridin-1 (2H) -yl] -3-phenylpropanoyl} amino) propanoic acid, (3S) -3 - ({(2S) -2- [3- (2- chlorobenzyl) -5-methyl- 2-oxopyridin-1 (2H) -yl] -3-phenylpropanoyl} amino) -3- (4-methylphenyl) propanoic acid, (3S) -3- (1,3-benzodioxol-5-yl) -3- ( ((2R) -2- (1-Benzyl-5-methyl-2-oxo-1,2-dihydropyridin-3-yl) hexanoyl) amino) propanoic acid, (3S) -3- (1,3-benzodioxol- 5-yl) -3 - (((2S) -2- (3-benzyl-5-methyl-2-oxo-1 (2H) pyridinyl) hexanoyl) amino) propanoic acid or one of its pharmaceutically acceptable salts.
机译:选自以下的化合物:(3S)-3-{[((2S)-2-(3-苄基-5-甲基-2-氧代吡啶-1(2H)-基)己酰基]-氨基}-3 -(3'',4''-二甲氧基-1-,1''-联苯-4-基)丙酸,(3S)-3-({(2S)-2- [3-(2-氯苄基) -5-甲基-2-氧杂吡啶-1(2H)-基]-己酰基}氨基)-3-(3'',4''-二甲氧基-1,1''联苯-4-基)丙酸,酸(3S)-3-(1,1''-联苯-4-基)-3-({(2S)-2- [3-(2-氯-6-甲基苄基)-5-甲基-2-氧代吡啶-1(2H)-基]己酰基}氨基)丙酸,(3S)-3-{[(2S)-2-(3-苄基-5-甲基-2-氧代吡啶-1(2H)-基)己酰基]-氨基} -3-(1,1''-联苯-4-基)丙酸,(3S)-3-(1,1''-联苯-4-基)-3-({(2S) -2- [3-(2-氯苄基)-5-甲基-2-氧代吡啶-1(2H)-基]己酰基}氨基)丙酸,(3S)-3-{[((2S)-2-(3 -苄基-5-甲基-2-氧代吡啶-1(2H)-基)己酰基]-氨基} -3-(4''-甲基-1,1''-联苯-4-基)丙酸,(3S )-3-({(2S)-2- [3-(2-氯苄基)-5-甲基-2-氧代吡啶-1(2H )-yl]-己酰基}氨基)-3-(4''-甲基-1,1-联苯-4-基)丙酸,(3S)-3-({(2S)-2- [3-( 2-氯-6-甲基苄基)-5-m乙基-2-氧代吡啶-1(2H)-基]己酰基}氨基)-3-(4''-甲基-1,1''-联苯-4-基)丙酸,(3S)-3-{[((2S)-2-(3-Benzyl-5-methyl-2-oxopyridin-1(2H)-yl)hexanoyl] -amino} -3-(2'' ,6''-二甲氧基-1,1''-联苯-4-基)丙酸,(3S)-3-({(2S)-2- [3-(2-氯苄基)-5-甲基-2 -氧代吡啶-1(2H)-基]-己酰基}氨基)-3-(2'',6''-二甲氧基-1,1''联苯-4-基)丙酸,(3S)-3-( {(2S)-2- [3-(2-氯-6-甲基苄基)-5-甲基-2-氧代吡啶-1(2H)-基]己酰基}氨基)-3-(2'',6'' -二甲氧基-1,1''-联苯-4-基)丙酸(3S)-3-{[((2S))-2-(3-苄基-5-甲基-2-氧代吡啶-1(2H)-基)己基]-氨基} -3-(1,1''-联苯-3-基)丙酸(3S)-3-(1,1''-联苯-3-基)-3-({(2S )-2- [3-(2-氯苄基-5-甲基-2-氧代吡啶-(2H)-基]己酰基}氨基)丙酸,(3S)-3-(1 ,1''-联苯-3-基)-3-({(2S)-2-[3-(2-氯-6-甲基苄基)-5-甲基-2-氧代吡啶-1(2H)-基]己酰基}氨基)丙酸,(3S)-3-[(2S)-2-(3-苄基-5-甲基-2-氧代吡啶-1(2H)-基)己酰基]-氨基} -3-(2 ''-甲氧基-1,1''-联苯-3-基)丙酸(3S)-3-({(2S)-2- [3-(2-氯苄基)-5-甲基-2-氧代吡啶- 1(2H)-基]-己酰基}氨基)-3-(2''-甲氧基-1,1''-联苯-3-基)丙酸,(3S)-3-({(2S)-2 -[3-(2-氯-6-甲基苄基)-5-甲基-2-氧代吡啶-1(2H)-基]己酰基}氨基)-3-(2''-甲氧基-1,1-联苯-3 -yl)丙酸(3S)-3-({(2S)-2-[3-(2-氟-6-甲氧基苄基)-5-甲基-2-氧代吡啶-1(2H)-基]己酰基}氨基)-3-(4-甲基苯基)丙酸,(3S)-3-({(2S)-2- [3-(2,6-二甲基苄基)-5-甲基-2-氧代吡啶-1(2H)-氨基] -3-(4-甲基苯基)丙酸,(3S)-3-({(2S)-2- [3- [3,5-二甲基苄基)-5-甲基-2-氧代吡啶- 1(2H)-基]-己酰基}氨基)-3-(4-甲基苯基)丙酸酸,(3S)-3-({(2S)-2- [3- [2,6-二氯苄基)-5-甲基-2-氧并吡啶-1(2H)-基]己酰基}氨基)-3-( 4-甲基苯基)丙酸,39无ES 2 321 059 T3(3S)-3-({(2S)-2- [3-(2-氯-6-氟苄基)-5-甲基-2-氧代吡啶-1 (2H)-基]己酰基}氨基)-3-(4-甲基苯基)丙酸(3S)-3-({(2S)-2-[[3-(2,6-二氟苄基)-5-甲基-2] -氧吡啶吡啶-1(2H)-基]-己酰基}氨基)-3-(4-甲基苯基)丙酸,(3S)-3-(1,3-苯并二氧杂-5-基)-3-({(2S )-2- [3-(2,6-二氟苄基)-5-甲基-2-氧代吡啶-1(2H)-基]己酰基}氨基)丙酸,(3S)-3-(1,3-苯并二恶唑- 5-基)-3-({((2S)-2- [3-(2-氯-6-氟苄基)-5-甲基-2-氧代吡啶-1(2H)-基]己酰基}氨基)丙酸, (3S)-3-(1,3-苯并二恶唑-5-基)-3-({(2S)-2- [3- [2,6-二氯苄基)-5-甲基-2-氧并吡啶-1(2H )-基]己酰基}氨基)丙酸,(3S)-3-(1,3-苯并二恶唑-5-基)-3-({(2S)-2- [3-(2,6-二甲基苄基)- 5-甲基-2-氧代吡啶-1(2H)-基]己酰基}氨基)丙酸(3S)-3-(1,3-苯并二恶唑-5-基)-3-({(2S)-2- [3-(3,5-二甲基苄基)-5-甲基-2-氧并吡啶-1 (2H)-基]己酰基}氨基)丙酸,(3S)-3-(1,3-苯并二氧杂-5-基)-3-({(2S)-2- [3-(2-氟-6 -甲氧基苄基)-5甲基-2-氧代吡啶-1(2H)-基]己酰基}氨基)丙酸,(3S)-3-({(2S)-2- [3-(2-氯苄基)-5-甲基-2-氧代吡啶-1(2H)-基]-己酰基}氨基)-3-(3,4-二乙氧基苯基)丙酸(3S)-3-(3,4-二乙氧基苯基)-3-({(2S )-2- [3-(2,6-二氟苄基)-5-me til-2-氧嘧啶-1(2H)-基]己酰基}氨基)丙酸,(3S)-3-({(2S)- 2- [3-(2,6-二氟苄基)-5-甲基-2-氧代吡啶-1(2H)-基]己酰基}氨基)-3-(3-乙氧基苯基)丙酸,(3S)-3-( {(2S)-2- [3-(2-氯-6-氟苄基)-5-甲基-2-氧代吡啶-1(2H)-基]己酰基}氨基)-3-(3-乙氧基苯基)丙酸, (3S)-3-({(2S)-2- [3-(2-氯苄基)-5-甲基-2-氧并吡啶-1(2H)-基] -3-甲基丁酰基}氨基)-3-(4 -甲基苯基)丙酸,(3S)-3-({(2S)-2 [3-(2-氯苄基)-5-甲基-2-氧代吡啶-1(2H)-基] -4-甲基戊酰基}-氨基)-3-( 4-甲基苯基)丙酸,(3S)-3-(1,3-苯并二恶唑-5-基)-3-({(2S)-2- [3-(2-氯苄基)-5-甲基-2-氧嘧啶-1(2H)-基] -4-甲基戊酰基}氨基)丙酸,(3S)-3-(1,3-苯并二恶唑-5-基)-3-({(2S)-2- [3- (2-氯苄基)-5-甲基-2-氧吡啶-1(2H)-基] -3-甲基丁酰基}氨基)丙酸,(3S)-3-(1,3-苯并二氧杂-5-基)-3 -({(2S)-2- [3-(2-氯苄基)-5-甲基-2-氧代吡啶-1(2H)-基] -3-苯基丙酰基}氨基)丙酸,(3S)-3-( {(2S)-2- [3-(2-氯苄基)-5-甲基-2-氧代吡啶-1(2H)-基] -3-苯基丙酰基}氨基)-3-(4-甲基苯基)丙酸,( 3S)-3-(1,3-苯并二恶唑-5-基)-3-(((2R)-2-(1-苄基-5-甲基-2-氧-1,2-二氢吡啶-3-基) (3S)-3-(1,3-benzodioxol- 5-yl)-3-((((2S)-2-(3-苄基-5-甲基-2-氧代-1( 2H)吡啶基)己酰基)氨基)丙酸或其一种药学上可接受的盐。

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