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Title:
【発明の名称】抗増殖剤としての縮合複素環式グルタミン酸誘導体
Document Type and Number:
Japanese Patent JPH08505877
Kind Code:
A
Abstract:
Novel compounds of formula (I) wherein n is 0 to 2; A is sulfur, CH2, oxygen, -NH- or selenium, provided that when n is 0, A cannot be CH2, and when n is 1, A cannot be CH2 or NH; X is at least one substituted or unsubstituted C1-C3 alkyl or alkenyl group, a C2-C3 alkynyl group, a substituted or unsubstituted amino group, sulfur or oxygen; Ar is a substituted or unsubstituted monocyclic carbocyclic or heterocyclic ring or fused or nonfuxed carbocyclic or heterocyclic ring system; and R1 and R2 are independently hydrogen or a moiety which forms a readily hydrolyzable ester group or a pharmaceutically acceptable salt thereof are found to inhibit the enzyme glycinamide ribonucleotide formyl transferase (GARFT). A novel method of preparing such compounds is also disclosed, as well as methods and compositions for employing the compounds as antiproliferative agents.

Inventors:
Vernie, Michael Dee
Palmer, Cynthia El
Romins, william h
Application Number:
JP51708294A
Publication Date:
June 25, 1996
Filing Date:
January 18, 1994
Export Citation:
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Assignee:
Agron Pharmaceuticals Incorporated
International Classes:
A61K31/505; A61K31/519; A61P35/00; A61P43/00; C07D471/04; C07D487/04; C07D475/04; C07D498/04; C07D513/04; C07D517/04; (IPC1-7): C07D471/04; A61K31/505; C07D475/04; C07D498/04; C07D513/04; C07D517/04
Attorney, Agent or Firm:
Kyozo Yuasa (6 people outside)