Seven-membered ring compounds as inhibitors of cytidine deaminase

US4275057A · kind A · utility

Assignee

• The United States of America as represented by the Department of Health, Education and Welfare · US

Inventors

• Victor E. Marquez · Gaithersburg, US
• Paul S. Liu · Bethesda, US
• John S. Driscoll · Rockville, US

Key dates

• Filing date: Jan 28, 1980
• Grant date: Jun 23, 1981
• Expiry date: Jan 28, 2000

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07H19/052
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

Seven-membered heterocyclic nucleosides used to inhibit the deamination enzyme responsible for the inactivation of arabinosylcytosine (ara--C). Preferred nucleosides containing a seven-member aglycone are as follows: ##STR1## Preferred aglycones are as follows: ##STR2## Active components utilized against pyrimidine deaminases from mammalian tissues (mouse kidney and human liver) showed optimum advantage when compared with tetrahydrouridine (THU).