Patent · US Expired

Derivatives of p-guanidinobenzoic acid and pharmaceutical agents containing them as an active ingredient

US5376655A · kind A · utility

21Cited by
6References
2Claims
0Family size

Assignee

Inventors

Key dates

Filing dateJun 2, 1993
Grant dateDec 27, 1994
Priority date
Expiry dateJun 2, 2013

Classification

  • Technology area (CPC C)Chemistry; Metallurgy
  • CPC primaryC07D295/26
  • WIPO fieldOrganic fine chemistry
  • WIPO sectorChemistry

Abstract

A derivative of p-guanidinobenzoic acid of the general formula (IA): ##STR1## wherein Y represents an oxygen atom or a sulfur atom and (a) when Y is an oxygen atom, (R.sup.1).sub.m is selected from the group consisting of: PA1 5-(4-guanidinobenzoyloxy)-3-methoxymethyl, 3,5-dicarboxy, 3,5-bis(isopropoxycarbonyl), 3,5-bistrifluoromethyl, 3-acetyl, 3,5-bis(N-ethylcarbamoyl), and 3,5-bis(N-propylcarbamoyl); PA0 (b) when Y is a sulfur atom, (R.sup.1).sub.m is selected from the group consisting of: PA1 2-methyl, 3-methyl, 4-fluoro, 2-chloro, 3-chloro, 2,5-dichloro 2,6-dichloro, 3,4-dichloro, 2-bromo, 2-methoxycarbonyl, and 4-(N,N-diethylaminosulfonyl); PA1 or an acid addition salt of said derivative. A method for the treatment or prevention of diseases induced by abnormal enhancing of degradation of proteins by the action of elastase in mammals subject to or suffering therefrom, including the step of administering an effective amount of a p-guanidinobenzoic acid as described herein, is also disclosed.

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