# US 5,344,837 A · Platelet aggregation inhibitors

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- Number: US 5,344,837 A
- Document ID: US5344837A
- Status: Granted
- Kind: A
- Application number: 08/126,817
- Filed: 1993-09-23
- Granted: 1994-09-06
- Earliest claimed: 1992-07-02
- Assignees: G.D. Searle & Co.; Monsanto Company
- Inventors: Foe S. Tjoeng; Jeffery A. Zablocki
- Web page: https://patentgrep.com/patent/US5344837A

## CPC

- C07C 275/24: containing six-membered aromatic rings
- C07D 213/55: Acids; Esters
- C07C: ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)

## Abstract

This invention relates to compounds having the following formula ##STR1## or a pharmaceutically acceptable salt thereof which are useful in the inhibition of platelet aggregation, to pharmaceutical compositions including the compounds, and to a method of inhibiting platelet aggregation in mammals by administering such compounds and compositions.

## Claims

### Claim 1

A method of treating a mammal to inhibit platelet aggregation comprising administering a therapeutically effective amount of a compound of the formula ##STR21## or a pharmaceutically acceptable salt thereof wherein Z is selected from the group consisting of H, halogen, hydroxy, alkoxy of from one to six carbon atoms and alkyl of from one to six carbon atoms;
wherein A is selected from the group consisting of alkyl of one to six carbon atoms, alkenyl of two to six carbon atoms and alkynyl of two to six carbon atoms;
wherein R.sub.1 is selected from the group consisting of H, alkyl of from one to six carbon atoms, aralkyl and alkanoyloxyalkyl; and
wherein R.sub.2 is selected from the group consisting of H, alkyl of from one to six carbon atoms, alkenyl of from two to six carbon atoms, alkynyl of from two to six carbon atoms, aryl and heteroaryl wherein the heteroatom is nitrogen optionally substituted by a radical selected from the group consisting of halogen, alkyl of one to six carbon atoms, alkoxy of one to six carbon atoms, carboxyl derivatives, nitro, cyano, azido, ureido, ureylene, alkoxycarbonyloxy, hydroxyl, alkylamino, alkoxycarbonyl, trialkylsilyl, alkoxyimino, alkylsulfonyl, phenylsulfonyl and amino.

### Claim 2 (depends on 1)

A method according to claim 1 wherein the compound is selected from the group consisting of ethyl .beta.-[[[[4-[4-(aminoiminomethyl)phenyl]butyl]amino]carbonyl]amino]3-pyri dinepropanoate; .beta.-[[[[4-[4-(aminoiminomethyl)phenyl]butyl]amino]carbonyl]amino]-3-pyr idinepropanoic acid;ethyl .beta.-[[[[4-[4-(aminoiminomethyl)phenyl]butyl]amino]carbonyl]amino]benzen epropanoate; .beta.-[[[[4-[4-(aminoiminomethyl)phenyl]butyl]amino]carbonyl]amino]benzen epropanoic acid; and 3-[[[[4-[4-(aminoiminomethyl)phenyl]butyl]amino]carbonyl]amino]benzeneprop anoic acid.