Bicyclic fibrinogen antagonists

Details Bicyclic fibrinogen antagonists Bicyclic fibrinogen antagonists

C - Chemistry, Metallurgy

07

D

C07D 401/12 (2006.01) A61K 31/55 (2006.01) C07D 223/16 (2006.01) C07D 243/14 (2006.01) C07D 401/14 (2006.01) C07D 403/12 (2006.01) C07D 405/14 (2006.01) C07D 409/00 (2006.01) C07D 417/14 (2006.01)

Patent

CA 2180441

Certain 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.

Cette invention se rapporte à certains composés de la formule (I), qui sont des inhibiteurs de l'agrégation plaquettaires. Dans cette formule, A?1¿ représente NH ou CH¿2?; R représente H, alkyle C¿1-6?, benzyle ou un groupe protecteur carboxy; R?3¿ représente alkyle C¿1-6?, Ar-alkyle C¿0-6?, cycloalkyle C¿3-7? alkyle C¿0-6? ou Het-alkyle C¿0-6?; R?6¿ représente 4-amidino-Ar-N(CH¿3?)CO, [[2-(4-pipéridinyl)éthyl](N-méthyl)amino]carbonyle, (4,4'-bipipéridine-1-yl)carbonyle, [4-(2-aminoéthyl)pipéridine-1-yl]carbonyle, [[[3-(4-pipéridinyl]propyl]méthylamino]carbonyle, 1-[4-(4-pyridyl)pipérazinyl]carbonyle, [[2-[(2-amino)pyrid-4-yl]éthyl]méthylamino]carbonyle, [[2-(4-pipéridinyl)éthyl]carbonyl]amino, [[2-(4-pipéridinyl)éthyl]carbonyl]amino, [[2-(1-pipérazinyl)éthyl]méthylamino]-carbonyle, ou [[(1,2,3,4-tétrahydro-7-isoquinolinyl]amino]carbonyle; et X représente H, alkyle C¿1-4?, alcoxy C¿1-4?, alkthio C¿1-4?, trifluoroalkyle, N(R')¿2?, CO¿2?R', CON(R')¿2?, OH, F, Cl, Br ou I.

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