Pyrido[2,3-]pyrimidine derivatives

US5026851A · kind A · utility

Assignee

• THE TRUSTEES OF PRINCETON UNIVERSITY · US

Inventors

• Edward C. Taylor · Princeton, US
• George P. Beardsley · Essex, US
• Peter J. Harrington · Louisville, US
• Stephen Robert Fletcher · Hamilton, CA

Key dates

• Filing date: Apr 21, 1989
• Grant date: Jun 25, 1991
• Expiry date: Apr 21, 2009

Classification

• Technology area (CPC Y): Emerging Cross-Sectional Technologies
• CPC primary: Y02P20/55
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

2,4-Diamino- and 2-amino-4-hydroxy- derivatives of N-(4-[2-(pyrido[2,3-d]pyrimidin-6-yl)alkyl]benzoyl-)-L-glutamic acids, and the corresponding 5,6,7,8-tetrahydro compounds are antineoplastic agents. The compounds are prepared by hydrolytic or hydrogenolytic removal of carboxylic acid protecting groups from the correspondingly protected glutamic acid derivatives. A typical embodiment is N-(4-[2-(2-amino-4-hydroxy-5,6,7,8-tetrahydropyrido[2,3-d]pyrimidin-6-yl)e thyl]benzoyl)-L-glutamic acid.