发明名称 Non-steroidic (hetero)cyclically substituted acylanides of combined gestagenic and androgenic effectiveness
摘要 The invention relates to non-steroidal gestagens of general formula (I), wherein R<1> and R<2> are the same or different and stand for a hydrogen atom, a C1-C5 alkyl group or a halogen atom, or together with the C atom of the chain stand for a ring with 3-7 units, R<3> means a C1-C5 alkyl group or a partially or fully fluorinated C1-C5 alkyl group, A stands for an optionally substituted mono or bi-cyclic aromatic ring, an ester group -COOR<4>, an alkenyl group -CR<5>=CR<6>R<7>, an alkinyl group -CCR<5> or for a partially or fully fluorinated C1-C5 alkyl group, B means a carbonyl group or a CH2 group and Ar is a ring system selected from the group of general partial formulae (2-11). When B represents a CH2 group in general formula (I), Ar additionally means a phenyl radical of partial general formula (12). The novel compounds display a very strong affinity to the gestagen receptor. They can be used on their own or in combination with oestrogen's in contraceptive preparations. They can also be used in the treatment of endometriosis. They can be used with oestrogen's in preparations for the treatment of gynaecological disorders. They can also be used to treat pre-menstrual complaints and in substitution therapy. Their androgen activity enables them to be used for male fertility control, male HRT and to treat andrological syndromes.
申请公布号 PL197887(B1) 申请公布日期 2008.05.30
申请号 PL19980337088 申请日期 1998.06.02
申请人 SCHERING AKTIENGESELLSCHAFT 发明人 LEHMANN MANFRED;SCHOELLKOPF KLAUS;STREHLKE PETER;HEINRICH NIKOLAUS;FRITZEMEIER KARL-HEINRICH;MUHN HANS-PETER;KRATTENMACHER ROLF
分类号 C07D249/18;A61K31/136;A61K31/16;A61K31/167;A61K31/343;A61K31/365;A61K31/366;A61K31/38;A61K31/381;A61K31/41;A61K31/4245;A61K31/50;A61K31/535;A61K31/536;A61P5/26;A61P5/34;A61P15/00;A61P15/12;A61P15/18;C07C225/22;C07C235/26;C07C235/32;C07C235/38;C07C235/84;C07C255/57;C07D237/28;C07D237/32;C07D265/02;C07D271/08;C07D271/12;C07D285/10;C07D285/14;C07D307/88;C07D307/94;C07D311/76;C07D333/72;C07D409/12 主分类号 C07D249/18
代理机构 代理人
主权项
地址