Derivatives of phosphinic acid useful as endothelin converting enzyme inhibitors
US5476847A · kind A · utility
Assignee
Inventors
Key dates
| Filing date | Jun 29, 1994 |
| Grant date | Dec 19, 1995 |
| Priority date | — |
| Expiry date | Jun 29, 2014 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07F9/5728
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
Abstract
Phosphinic acid derivatives of the structural formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein R is H, alkyl or alkanoyloxymethylene; PA1 R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are H, alkyl, alkenyl, alkenylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, hydroxyalkyl, carboxyalkyl, thioalkyl, alkoxythioalkyl, aminoalkyl, alkylaminoalkyl, cycloalkyl-substituted alkyl or heterocycloalkyl; or R.sub.1 and R.sub.2 form a cycloalkyl ring of 3-8 members and R.sub.3 and R.sub.4 are as defined; or R.sub.3 and R.sub.4 form a cycloalkyl ring of 3-7 members and R.sub.1 and R.sub.2 are as defined; or R.sub.1 and R.sub.2 together, and R.sub.3 and R.sub.4 together, each form a cycloalkyl ring; PA1 R.sub.5 is --OR.sub.9 or --NHR.sub.9, wherein R.sub.9 is hydrogen or alkyl; PA1 n is 0 or 1; PA1 A.sub.1 is p-aminobenzoyl or p-aminobenzenesulfonyl, or A.sub.1 and R.sub.5 together form a radical of an .alpha.-aminoacyl derivative; and PA1 R.sub.6 is phenylmethoxycarbonyl, arylcarbonyl, heteroarylcarbonyl or --A.sub.2 --R.sub.7, wherein A.sub.2 is a divalent .alpha.-aminoacyl radical, and R.sub.7 is a substituent on the .alpha.-amino atom selected from H, R.sub.8 OCO--, R.sub…
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.