Novel amidinonaphthyl derivative or salt thereof

Details Novel amidinonaphthyl derivative or salt thereof Novel amidinonaphthyl derivative or salt thereof

C - Chemistry, Metallurgy

07

D

C07D 211/44 (2006.01) A61K 31/40 (2006.01) A61K 31/445 (2006.01) A61K 31/495 (2006.01) C07D 207/12 (2006.01) C07D 211/46 (2006.01) C07D 401/12 (2006.01) C07D 403/12 (2006.01) C07D 405/12 (2006.01) C07D 409/12 (2006.01) C07D 413/12 (2006.01) C07D 417/12 (2006.01) C07D 471/04 (2006.01) C07D 498/04 (2006.01) C07D 513/04 (2006.01)

Patent

CA 2206532

An amidinonaphthyl derivative represented by the following general formula (I) which has a platelet aggregation inhibiting action based on the activated blood coagulation factor X inhibiting action and is useful as an anti-thrombus agent and the like, a salt thereof, an intermediate thereof and a pharmaceutical composition which comprises the amidinonaphthyl derivative. An amidinonaphthyl derivative represented by the following general formula (I) or a pharmaceutically acceptable salt thereof. (see formula 1) (symbols in the formula have the following meanings; R1: a hydrogen atom or a group represented by the formula -A-W-R4, A: a group represented by the formula (see formula 2) a group represented by the formula (see formula 3) or a group represented by the formula -SO2-, -184- X: an oxygen atom or a sulfur atom, W: a single bond or a group represented by the formula -NR5-, R4: a hydroxyl group, a lower alkoxy group, etc., R5: a hydrogen atom, a carbamoyl group, a lower alkoxycarbonyl group, etc., R2: a lower alkyl group, R3: a hydrogen atom, a halogen atom, a carboxyl group, B: a lower alkylene group or a carbonyl group, and n: 0 or 1). -185-

L'invention concerne un dérivé d'amidinonaphtyle présentant un effet antiagrégation plaquettaire sur la base de l'effet d'inhibition du facteur X de coagulation sanguine activée, utile en tant qu'agent antithrombotique, etc., et représenté par la formule générale (I), ou un sel pharmaceutiquement acceptable dudit dérivé, un intermédiaire de celui-ci, et une composition médicinale contenant le dérivé d'amidinonaphtyle. Dans ladite formule R<1> représente hydrogène ou -A-W-R<4>; A représente (a), (b) ou -SO2; X représente oxygène ou soufre; W représente une liaison simple ou -NR<5>-; R<4> représente hydroxy, alcoxy inférieur, etc.; R<5> représente hydrogène, carbamyle, alcoxycarbamyle inférieur, etc.; R<2> représente alkyle inférieur; R<3> représente hydrogène, halogéno, carboxy, etc.; B représente alkylène ou carbonyle inférieur; et n représente 0 ou 1.

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