Pyrazinone thrombin inhibitors

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 401/12 (2006.01) A61K 31/495 (2006.01) C07D 213/00 (2006.01) C07D 241/00 (2006.01) C07D 401/14 (2006.01)

Patent

CA 2373999

Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having structure (I): where A is (II), (III), or (IV) wherein Y1 and Y2 are independently hydrogen, C1-4 alkyl, C1-4 alkoxy, F u H v C(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.

L'invention concerne des composés destinés à être utilisés pour inhiber la thrombine et les occlusions thrombotiques associées, ces composés présentant la structure (I), dans laquelle A représente (II), (III), ou (IV), où Y<1> et Y<2> désignant indépendamment hydrogène, alkyle C1-4, alkoxy C1-4, FuHvC(CH2)0-1O-, u et v étant égaux à 1 ou 2 à condition que lorsque u est égal à 1, v soit égal à 2, et que lorsque u est égal à 2, v soit égal à 1, cycloalkyle C3-7, thioalkyle C1-4, sulfinylalkyle C1-4, sulfonylalkyle C1-4, halogène, cyano, ou trifluorométhyle, et b étant égal à 0 ou 1.

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