Patent · US Expired

Heterocyclic oxophthalazinyl acetic acids

US4939140A · kind A · utility

49Cited by
1References
29Claims
0Family size

Assignee

Inventors

Key dates

Filing dateOct 27, 1988
Grant dateJul 3, 1990
Priority date
Expiry dateOct 27, 2008

Classification

  • Technology area (CPC C)Chemistry; Metallurgy
  • CPC primaryC07D513/04
  • WIPO fieldOrganic fine chemistry
  • WIPO sectorChemistry

Abstract

A heterocyclic oxophthalazinyl acetic acid having aldose reductast inhibitory activity of the formula ##STR1## wherein X is oxygen or sulfur; Z is a covalent bond, O, S, NH or CH.sub.2 or CHR.sub.5 Z is vinyl; R.sub.1 is hydroxy, or a prodrug group; R.sub.2 is a heterocyclic group, R.sub.3 and R.sub.4 are hydrogen or the same or a different substituent, and R.sub.5 is hydrogen, methyl or trifluoromethyl. The pharmaceutically acceptable acid addition salts of the above compounds wherein R.sub.1 is di(C.sub.1 -C.sub.4)alkylamino or (C.sub.1 -C.sub.4)alkoxy substituted by N-morpholino or di(C.sub.1 -C.sub.4)alkylamino and the pharmaceutically active base addition salts of the above compounds wherein R.sub.1 is hydroxy are also aldose reductase inhibitors.

Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.