Thrombin inhibitors

Details Thrombin inhibitors Thrombin inhibitors

C - Chemistry, Metallurgy

07

D

C07D 413/12 (2006.01) A61K 31/5365 (2006.01) A61P 7/02 (2006.01) C07D 498/04 (2006.01) C12N 9/99 (2006.01)

Patent

CA 2374654

Compounds of the invention, useful as thrombin inhibitors and having therapeutic value in for example, preventing coronary artery disease, have structure (I) or a pharmaceutically acceptable salt thereof, wherein A is (a), (b) or (c) wherein Y1 and Y2 are independently hydrogen, C1-4 alkyl, C1-4 alkoxy, FuHvC(CH2)0-1 O-, wherein u and v are either 1 or 2, provided that when u is 1, v is 2, and when u is 2, v is 1, C3-7 cycloalkyl, thio C1-4 alkyl, C1-4 sulfinylalkyl, C1-4 sulfonylalkyl, halogen cyano, or trifluoromethyl, and wherein b is 0 or 1.

La présente invention concerne des composés, ou certains de leurs sels pharmaceutiquement admis, convenant comme inhibiteurs de la thrombine et présentant un intérêt thérapeutique, notamment pour la prévention des affections coronariennes. Ces composés sont représentés par la formule générale (I) dans laquelle A est tel que (a), (b) ou (c). En l'occurrence, Y?1¿ et Y?2¿ sont indépendamment hydrogène, C¿1-4? alkyle, C¿1-4? alcoxy, F¿u?H¿v?C(CH¿2?)¿0-1? O-, auquel cas u et v valent 1 ou 2, sous la réserve que lorsque u vaut 1, v vaille 2, et que lorsque u vaut 2, v vaille 1, C¿3-7? cycloalkyle, thio C¿1-4? alkyle, C¿1-4? sulfinylalkyle, C¿1-4? sulfonylalkyle, halogène, cyano, ou trifluorométhyl, b valant 0 ou 1.

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