# US 4,399,144 A · Pyridinium salts

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- Number: US 4,399,144 A
- Document ID: US4399144A
- Status: Granted
- Kind: A
- Application number: 06/342,542
- Filed: 1981-01-25
- Granted: 1983-08-16
- Earliest claimed: 1980-04-30
- Assignees: John Wyeth & Brother Limited
- Inventors: Roger Crossley
- Web page: https://patentgrep.com/patent/US4399144A

## CPC

- C07D 417/12: linked by a chain containing hetero atoms as chain links
- C07D 401/12: linked by a chain containing hetero atoms as chain links
- Y02P 20/55: Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- Y02P: CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS

## Abstract

The invention concerns compounds of formula ##STR1## wherein the sulphur is bonded to the pyridinium ring at position 2 or 4, Y is --S--or --CH.sub.2 --, R represents hydrogen, or a lower alkyl group, or other carboxylic protecting group; R.sup.1 represents hydrogen or lower alkyl; R.sup.2 represents lower alkyl, aryl of 6 to 10 carbon atoms or aralkyl of 7 to 11 carbon atoms; R.sup.3 represents hydrogen or a substituent selected from lower alkyl, halogen and lower alkoxy; q and r are each 1 or 2; and X.sup..crclbar. represents a halide ion or an organosulphonate ion, which are antihypertensive agents and are useful as intermediates to captopril and analogous compounds.

## Claims

### Claim 1

A compound of formula ##STR14## wherein the sulphur is bonded to the pyridinium ring at position 2 or 4, Y is --S--, R represents hydrogen or lower alkyl group; R.sup.1 represents hydrogen or lower alkyl; R.sup.2 represents lower alkyl, aryl of 6 to 10 carbon atoms or aralkyl of 7 to 11 carbon atoms; R.sup.3 represents hydrogen or a substituent selected from lower alkyl, halogen and lower alkoxy; q and r are each 1 or 2; and X.sup..crclbar. represents a halide ion or p-toluenesulphonate or methanesulphonate.

### Claim 2 (depends on 1)

A compound of formula I according to claim 1 wherein R is hydrogen, R.sup.2 is lower alkyl and R.sup.3 is hydrogen.

### Claim 3 (depends on 1)

A compound of formula I according to claim 1 wherein the sulphur is bonded to the pyridinium ring at position 2.

### Claim 4 (depends on 1)

A pharmaceutical composition comprising an anti-hypertensive effective amount of a compound of formula I as claimed in claim 1 and a pharmaceutically acceptable carrier.