Phosphinic acid derivatives

C - Chemistry – Metallurgy – 07 – F

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C07F 9/30 (2006.01) A61K 31/66 (2006.01) C07F 9/32 (2006.01) C07F 9/58 (2006.01) C07F 9/6506 (2006.01) C07F 9/6518 (2006.01)

Patent

CA 1327199

Abstract of the Disclosure A phosphinic acid derivative represented by the general formula III, or a pharmaceutically acceptable salt thereof, Image (I) wherein R1 represents an alkyl, cycloalkyl or aralkyl group which may be substituted; R2 and R5 may be identical or different, and each represents a hydrogen atom, or an ester residue capable of forming a non-toxic ester hydro- lyzable in vivo; and A represents a group of the formula Image wherein R3 represents an alkyl group, a group of the formula Image wherein R30 represents a halogen atom, a carboxyl group, a hydroxyl group, a cycloalkyl group which may be substituted, an aryl group which may be substituted, an arylthio group, a heteroarylthio group which may be substituted, an alkylthio group which may be substituted, an amino group which may be substituted, or a lower alkoxycarbonyl group; R31 represents a hydrogen atom or a lower alkyl group; and n represents an integer of 0 to 6, a cycloalkyl group which may be substi- tuted or an aryl group which may be sub- stituted; and the double bond at A has a Z-configuration, or a group of the formula Image wherein R4 represents a cycloalkyl group which may be substituted. Said phosphinic acid derivative is useful for reducing renal toxicity induced by a carbapenem or penem anti- biotic and for inhibiting dipeptidase.

603560

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