Patent · US Expired

GAR transformylase inhibitor

US4999424A · kind A · utility

1Cited by
0References
17Claims
0Family size

Assignee

Inventors

Key dates

Filing dateNov 10, 1988
Grant dateMar 12, 1991
Priority date
Expiry dateNov 10, 2008

Classification

  • Technology area (CPC C)Chemistry; Metallurgy
  • CPC primaryC07H13/04
  • WIPO fieldOrganic fine chemistry
  • WIPO sectorChemistry

Abstract

The present invention is directed to several multisubstrate adduct inhibitors of glycinamide ribonucleotide transformylase (GAR TFase; E.C. 2.1.2.2), a folate-requiring enzyme of de novo purine biosynthesis. The compounds of the present invention will be useful to provide anti-gout and/or anti-neoplastic therapeutic agents or will serve as potentiators for other such agents. The most prefeffed, potent tight-binding multisubstrate adduct inhibitor of glycinamide ribonucleotide transformylase, is N.sup.10 -[5'-phosphoribosyl-1'-.beta.-aminocarbonylmethyl-1-thioacetyl]-5,8-dideaz afolate, which has the chemical formula: ##STR1##

Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.