Patent · US Expired

Phosphono/biaryl substituted amino acid derivatives

US5250522A · kind A · utility

32Cited by
6References
19Claims
0Family size

Assignee

Inventor

Key dates

Filing dateOct 9, 1992
Grant dateOct 5, 1993
Priority date
Expiry dateOct 9, 2012

Classification

  • Technology area (CPC C)Chemistry; Metallurgy
  • CPC primaryC07F9/4006
  • WIPO fieldOrganic fine chemistry
  • WIPO sectorChemistry

Abstract

The present invention relates to the N-phosphonomethyl-biaryl substituted amino acid derivatives of formula I ##STR1## wherein X represents a direct bond, C.sub.1-4 -alkylene or C.sub.2 -C.sub.4 -alkenylene; R and R' represent independently hydrogen, carbocyclic aryl, 6-tetrahydronaphthyl, 5-indanyl, .alpha.-(trichloromethyl, carboxyl, esterified carboxyl or amidated carboxyl)substituted-(lower alkyl or aryl-lower alkyl), acyloxymethyl optionally monosubstituted on methyl carbon by C.sub.1-20 -alkyl, by C.sub.5 -C.sub.7 -cycloalkyl, by aryl or by aryl-lower alkyl; R.sub.1 represents monocyclic carbocyclic or monocyclic heterocyclic aryl; COR.sub.3 represents carboxyl or carboxyl derivatized in form of a pharmaceutically acceptable ester; R.sub.2 and R.sub.4 represent hydrogen, lower alkyl, trifluoromethyl, lower alkoxy or halogen; and pharmaceutically acceptable salts thereof; pharmaceutical compositions comprising said compounds; methods for preparation of said compounds and for the preparation of intermediates; and methods of treating disorders in mammals which are responsive to the inhibition of neutral endopeptidases by administration of said compounds to mammals in need of suc…

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