发明名称 ANTIPROLIFERATIVE SUBSTITUTED TRICYCLIC COMPOUNDS
摘要 Compounds of formula (Q), wherein X and Y form a five- or six-membered heterocyclic ring containing at least one nitrogen; Z is a hydrogen, halogen, carbon, oxygen or nitrogen atom; U is a carbon or nitrogen atom; n is 0 or the integer 1; V is a carbon or nitrogen atom; W is a carbon or nitrogen atom; A is in the 1- or 2-position and is a nitrogen atom, a sulfur atom, or a substituted or unsubstituted alkylene group; Ar is an aryl or heteroaryl group having one or more rings; and B is either (i) an oxygen or nitrogen atom, or a -CO- or -SO2- group, any of which is linked to an amino acid, aryl group, heterocyclic group or alkyl group, or (ii) a substituted or unsubstituted alkyl group, which inhibit the enzyme thymidylate synthase (''TS''), pharmaceutical compositions containing these tricyclic compounds, and the use of these compounds to inhibit TS, including all effects derived from the inhibition of TS. Effects derived from the inhibition of TS include the inhibition of the growth and proliferation of the cells of higher organisms and of microorganisms, such as yeast and fungi. Such effects include antitumor activity.
申请公布号 ZA9107613(B) 申请公布日期 1992.08.26
申请号 ZA19910007613 申请日期 1991.09.24
申请人 AGOURON PHARMACEUTICALS, INC. 发明人 SIEGFRIED H. REICH;MARY ANN M. FUHRY
分类号 A61K31/47;A61K31/495;A61K31/50;A61K31/505;A61P31/04;A61P31/12;A61P35/00;C07D471/04;C12N9/99 主分类号 A61K31/47
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