Martin Poe

US Patent:

42580455, Mar 24, 1981

Filed:

Nov 30, 1979

Appl. No.:

6/099167

Inventors:

Martin Poe - Scotch Plains NJ
William V. Ruyle - Scotch Plains NJ

Assignee:

Merck & Co., Inc. - Rahway NJ

International Classification:

A61K 31505
C07D23949
C07D23949

US Classification:

424251

Abstract:

A group of aryl-Z-alkoxy-5-benzylpyrimidines wherein Z is oxy, thio, imino, carbonyl, carbamoyl, sulfonyl, sulfinyl or sulfamoyl has been prepared from 2,4-diamino-5-benzylpyrimidine via alkylation with either an aryl-Z-alkyl halide or a substituted glycidyl ether. These compounds are potent dihydrofolate reductase (DHFR) inhibitors which are useful as antibacterial, anti-protozoal and antitumor agents.