发明名称 NOVEL COMPOUNDS AND USE THEREOF IN THERAPY
摘要 FIELD: chemistry. ^ SUBSTANCE: invention relates to use of tetrahydrobenzo[4,5]thiophene[2,3-d]pyrimidine derivatives, including groups of known compounds, having formula (I), for preparing a medicinal agent for treating and/or preventing diseases and disorders which require inhibition of the 17-hydroxysteroid-dehydrogenase (17-HSD) enzyme, more preferably which require inhbition of type 1 17-HSD enzyme, type 2 17-HSD enzyme or type 3 17-HSD enzyme. In formula X denotes S or SO2, R1 and R2 are separately selected from a group which includes -C1-C12alkyl, where the alkyl can be straight, cyclic, branched or partially unsaturated, and can be optionally substituted with up to three substitutes, independently selected from a group consisting of hydroxyl, C1-C12alkoxy group, thiol, C1-C12alkylthio-, aryloxy group, -CO-aryl, -CO-OR, -O-COR, -O-CO-heteroaryl and a -N(R)2 group; where the said aryl group is phenyl or naphthyl and can be optionally substituted with up to 3 halogen atoms; where the said heteroaryl group is thienyl, furyl or pyridyl; -aryl and arylC1-C12alkyl, where the aryl is selected from a group consisting of phenyl, biphenyl, naphthyl, indanyl, indenyl and fluorenyl. Other values of substitutes are given in the formula of invention. ^ EFFECT: high efficiency of using novel compounds in therapy. ^ 32 cl, 3 tbl, 7 dwg, 151 ex
申请公布号 RU2412190(C2) 申请公布日期 2011.02.20
申请号 RU20060100033 申请日期 2004.06.09
申请人 ZOL'VAJ FARMAS'JUTIKLZ B.V. 发明人 KHIRVELA LEENA;JOKHANSSON NINA;KOSKIMIES PASI;PENTIKAJNEN OLLI TANELI;NIRENEN TOMMI;SALMINEN TIINA ANNAMARIJA;JONSON MARK STUART;LEKHTOVUORI PEKKA
分类号 A61K31/519;A61P15/00;A61P17/02;A61P17/08;A61P17/10;A61P19/02;A61P25/00;A61P25/28;A61P27/12;A61P35/00;C07D495/04 主分类号 A61K31/519
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