发明名称 5-{2-HYDROXY-3-[1-(3-TRIFLUOROMETHYLPHENYL)CYCLOPROPYL]-PROPIONYLAMINO}-PHTHALIDE AND RELATED COMPOUNDS POSSESSING MODULATING ACTIVITY WITH RESPECT TO PROGESTERONE RECEPTOR FOR USING IN CONTROL OF REPRODUCTIVE FUNCTION AND HORMONE-SUBSTITUTION THERAPY
摘要 FIELD: organic chemistry, medicine. ^ SUBSTANCE: invention relates to compound of the general formula (I) wherein R1 and R2 mean independently of on another hydrogen atom (H) or fluorine atom (F); R3 means -CH3 or -CF3 ; Ar means structural formulae (a) or (b) Invention relates also to a pharmaceutical composition possessing the modulating activity with respect to progesterone receptor and containing compound of the formula (I), adjuvants, carriers and excipents. Compounds of the formula (I) are used in preparing a medicinal agent designated for selective modulation of processes in organ-targets mediated by progesterone receptor, such as uterus/breast and for selective activation of transcription of progesterone receptor isoform A as compared with transcription of progesterone receptor isoform B, selective enhancing processes mediated by progesterone receptor isoform A as compared with processes mediated by progesterone receptor isoform B and as a contraceptive. Invention provides a compound using as a medicinal agent in hormone-substitution therapy and for control of reproductive function. ^ EFFECT: valuable medicinal and biological properties of compound and pharmaceutical composition. ^ 45 cl, 4 dwg, 5 tbl, 6 ex
申请公布号 RU2314299(C2) 申请公布日期 2008.01.10
申请号 RU20040130430 申请日期 2003.03.10
申请人 SHERING AKTSIENGEZEL'SHAFT 发明人 SHMEES NORBERT;LEMANN MANFRED;FURMANN UL'RIKE;MUN PETER;KHEGELE-KHARTUNG KRISTA;KLOTTSBJUKHER MIKHAEHL'
分类号 C07D265/02;A61K31/343;A61K31/365;A61K31/535;A61K31/536;A61K31/565;A61P5/30;A61P15/08;A61P15/18;A61P43/00;C07D307/88 主分类号 C07D265/02
代理机构 代理人
主权项
地址