Penicillaminamide derivatives

Details Penicillaminamide derivatives Penicillaminamide derivatives

C - Chemistry, Metallurgy

07

D

C07D 207/16 (2006.01) A61K 31/40 (2006.01) A61K 31/445 (2006.01) C07D 211/60 (2006.01) C07K 5/06 (2006.01) C07K 5/065 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2227607

Compounds represented by the general formula (I) wherein n represents 1 or 2, R1 represents, for example, a C1-C10 alkyl group which may be substituted with a C3-C10 cycloalkyl group or carboxyl group; R2 represents hydrogen atom, a C1- C10 alkyl group or other; and R3 represents amino group or amidino group, whose example include trans-4-amino-[(S)-N-[(S)-2-propoxycarbonylamino-3-isopropylthio-3- methyl--butanoyl] prolyl]aminomethylcyclohexane. The compounds have potent inhibitory activity against thrombin, and are useful as anticoagulants.

L'invention concerne des composés représentés par la formule générale (I). Dans cette formule, n est 1 ou 2; R<1> est un cycloalkyle en C3-10, un alkyle en C1-10 éventuellement carboxylé, etc; R<2> représente un hydrogène, un alkyle en C1-10, etc; et R<3> représente un amino ou un amidino. Le trans-4-amino[(S)-N-[(S)-2-propoxycarbonylamino-3-isopropylthio-3-méthyl-butanoyl]propyl]aminométhylcyclohexane constitue un composé typique. Ces dérivés sont de puissants inhibiteurs de la thrombine et sont donc utiles comme anticoagulants.

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