Phosphonic acid derivative having inhibitory activity...

C - Chemistry – Metallurgy – 07 – F

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C07F 9/30 (2006.01) A61K 31/662 (2006.01) A61P 7/02 (2006.01) A61P 43/00 (2006.01) C07F 9/40 (2006.01) C07F 9/50 (2006.01) C07F 9/58 (2006.01) C07F 9/59 (2006.01) C07F 9/6533 (2006.01) C07F 9/655 (2006.01)

Patent

CA 2381801

A compound represented by the following general formula (I) and a pharmacologically acceptable salt thereof: (see formula I) wherein R1 represents hydrogen atom, an alkyl group, a substituted alkyl group and the like; R2 and R3 represent hydrogen atom, an alkyl group, a substituted alkyl group, an alkoxyl group and the like; X represents -CH2-, -O-, or -NH-; A represents the following group (II): (see formula II) [in which R7 and R8 represent hydrogen atom, an alkyl group, an acyl group, an alkoxycarbonyl group and the like; R9 and R10 represents hydrogen atom, a halogen atom, hydroxyl group, phenyl group, an alkyl group and the like] and the like; and E represents hydrogen atom and the like, which has inhibitory activity against carboxypeptidase B and is useful for therapeutic and/or preventive treatment of a thrombotic disease.

L'invention concerne des composés de formule générale (I) [dans laquelle R<1> représente un hydrogène, alkyle, alkyle substitué, etc.; R<2> et R<3> représentent chacun un hydrogène, alkyle, alkyle substitué, alcoxy, etc.; X représente -CH2-, -O-, ou -NH-; A représente un groupe de formule (II) (dans laquelle R<7> et R<8> représentent chacun un hydrogène, alkyle, acyle, alcoxycarbonyle, etc.; et R<9> et R<10> représentent chacun un hydrogène, halogène, hydroxy, phényle, alkyle, etc.), etc.; et E représente un hydrogène, etc.]. L'invention concerne également leurs sels acceptables sur le plan pharmaceutique. Ces composés présentent une activité inhibitrice de carboxypeptidase B et sont utiles dans le traitement et/ou la prévention d'affections thrombotiques.

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