BICYCLISCHE FIBRINOGENANTAGONISTEN

摘要

PCT No. PCT/US95/00248 Sec. 371 Date Jul. 3, 1996 Sec. 102(e) Date Jul. 3, 1996 PCT Filed Jan. 9, 1995 PCT Pub. No. WO96/18619 PCT Pub. Date Jul. 13, 1995Certain compounds within formula (I) are inhibitors of platelet aggregation: wherein A1 is NH or CH2; R is H, C1-6alkyl, benzyl or a carboxy protecting group; R3 is C1-6alkyl, Ar-C0-6alkyl, C3-7cycloalkylC0-6alkyl, or Het-C0-6alkyl; R6 is 4-amidino-Ar-N(CH3)CO, [[2-(4-piperidinyl)ethyl](N-methyl)amino]carbonyl, (4,4'-bipiperidin-1-yl)carbonyl, [4-(2-aminoethyl)piperidin-1-yl]carbonyl, [[[3-(4-piperidinyl]propyl]methylamino]carbonyl, 1-[4-(4-pyridyl)piperazinyl]carbonyl, [[2-[(2-amino)pyrid-4-yl]ethyl]methylamino]carbonyl, [[2-(4-piperidinyl)ethyl]carbonyl]amino, [[2-(4-piperidinyl)ethyl]carbonyl]amino, [[2-(1-piperazinyl)ethyl]methylamino]-carbonyl, or [[(1,2,3,4-tetrahydro-7-isoquinolinyl]amino]carbonyl; and X is H, C1-4alkyl, C1-4alkoxy, C1-4alkthio, trifluoroalkyl, N(R')2, CO2R', CON(R')2, OH, F, Cl, Br or I.