Phosphinic acid derivatives

Details Phosphinic acid derivatives Phosphinic acid derivatives

1989-06-22

1991-01-29

Evans, J. E.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Phosphorus containing other than solely as part of an...

514 94, 514120, 546 24, 548119, 558182, 560125, 560205, 562 11, 562 24, A61K 3166, A61K 31675, C07F 930, C07C 6900

Patent

active

049886819

ABSTRACT:
A phosphinic acid derivative represented by the general formula [I], or a pharmaceutically acceptable salt thereof, ##STR1## wherein R.sup.1 represents an alkyl, cycloalkyl or aralkyl group which may be substituted; R.sup.2 and R.sup.5 may be identical or different, and each represents a hydrogen atom, or an ester residue capable of forming a non-toxic ester hydrolyzable in vivo; and A represents a group of the formula ##STR2## wherein R.sup.3 represents an alkyl group, a group of the formula ##STR3## wherein R.sup.30 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; R.sup.31 represents a hydrogen atom or a lower alkyl group; and n represents an integer of 0 to 6, a cycloalkyl group which may be substituted or an aryl group which may be substituted; and the double bond at A has a Z-configuration, or a group of the formula ##STR4## wherein R.sup.4 represents a cycloalkyl group which may be substituted. Said phosphinic acid derivative is useful for reducing renal toxicity induced by a carbapenem or penem antibiotic and for inhibiting dipeptidase.

REFERENCES:
patent: 4374131 (1983-02-01), Petrillo
patent: 4444765 (1984-04-01), Karanewsky et al.
patent: 4452791 (1984-06-01), Ryono et al.
patent: 4715994 (1987-12-01), Parsons et al.
patent: 4885283 (1989-12-01), Broadhurst et al.
Pitchett et al., "Chem. Abstracts", vol. 107 (11) 97134k (1987).

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