发明名称 FLUORINATED DERIVATIVES OF 4-AZASTEROID AS ANDROGEN RECEPTOR MODULATORS
摘要 FIELD: organic chemistry, medicine, pharmacy. ^ SUBSTANCE: invention describes compound of the formula (I) or its pharmaceutically acceptable salt, or an enantiomer wherein n = 0 or 1; a - b means -CF=CH or -CHFCH2; R1 represents (C1-C3)-alkyl wherein alkyl is unsubstituted; R2 represents hydrogen atom; R3 is chosen from (C1-C4)-alkyl, (CH2)n-cycloheteroalkyl and (CH2)n-aryl; or R2 and R3 form in common 6-membered saturated ring condensed with 5-membered aromatic ring system comprising 2 heteroatoms chosen from nitrogen atom (N), and pharmaceutical compositions. Compounds of the formula (I) represent modulators of androgen receptors (AR) possessing tissue-selective effect. Proposed compounds are useful as androgen receptors agonists in osseous and/or muscle tissue in antagonizing AR in male patient prostate or in female patient uterus. ^ EFFECT: valuable medicinal properties of compounds and pharmaceutical composition. ^ 36 cl, 2 tbl, 72 ex
申请公布号 RU2320670(C2) 申请公布日期 2008.03.27
申请号 RU20040130452 申请日期 2003.03.07
申请人 MERK EHND KO., INK. 发明人 MEJSSNER ROBERT S.;PERKINS DZHEJMS DZH.
分类号 A61K45/00;C07J73/00;A61K31/138;A61K31/22;A61K31/366;A61K31/40;A61K31/404;A61K31/4418;A61K31/4535;A61K31/47;A61K31/473;A61K31/505;A61K31/56;A61K31/565;A61K31/566;A61K31/567;A61K31/57;A61K31/573;A61K31/58;A61K31/59;A61K31/593;A61K31/661;A61K31/663;A61K31/675;A61K33/16;A61K38/00;A61K38/23;A61K38/27;A61P1/02;A61P3/04;A61P3/06;A61P5/26;A61P7/06;A61P9/10;A61P13/08;A61P15/10;A61P15/12;A61P17/00;A61P19/00;A61P19/02;A61P19/10;A61P21/00;A61P29/00;A61P31/18;A61P35/00;A61P37/02;A61P43/00;C07D221/18 主分类号 A61K45/00
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