C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 211/46 (2006.01) A61K 31/44 (2006.01) A61P 7/02 (2006.01) A61P 9/10 (2006.01)
Patent
CA 2389156
Benzamidine derivatives of formula (I) or pharmaceutically acceptable salts thereof exhibit excellent inhibitory activity against factor Xa and are useful for treating or preventing blood coagulation disorders: (see formula I) wherein R1 represents a hydrogen atom, a halogen atom, an alkyl group or a hydroxyl group; R2 represents a hydrogen atom, a halogen atom or an alkyl group, R3 represents a hydrogen atom, an optionally substituted alkyl group, an aralkyl group, an optionally substituted alkanoyl group or an optionally substituted alkylsulfonyl group, R4 and R5 are the same as or different from each other and each represent a hydrogen atom, a halogen atom, an optionally substituted alkyl group, an alkoxy group, a carboxyl group, an alkoxycarbonyl group or an optionally substituted carbamoyl group, and R6 represents a substituted pyrrolidine group or substituted piperidine group.
L'invention concerne des dérivés de benzamidine de formule générale (I), ou des sels pharmaceutiquement acceptables desdits composés, présentant une activité inhibitrice efficace contre le facteur X de coagulation sanguine. Ces dérivés sont utilisés comme médicaments thérapeutiques ou préventifs destinés aux maladies liées à la coagulation sanguine. Dans ladite formule, R<1> est hydrogène, halogéno, alkyle ou hydroxyle, R<2> est hydrogène, halogéno ou alkyle, R<3> est hydrogène, éventuellement alkyle, aralkyle, éventuellement alcanoyle, ou éventuellement alkylsulfonyle substitué, R<4> et R<5> sont chacun indépendamment hydrogène, halogéno, éventuellement alkyle substitué, alcoxy, carbonyle, alcoxycarbonyle, ou éventuellement carbamoyle substitué, et R<6> est pyrrolidine substituée ou pipéridine substituée.
Asai Fumitoshi
Fujimoto Koichi
Matsuhashi Hayao
Marks & Clerk
Sankyo Company Limited
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