Invention Grant
EP0986545B1 NICHTSTEROIDALE (HETERO)ZYKLISCH-SUBSTITUIERTE ACYLANILIDE MIT GEMISCHTER GESTAGENER UND ANDROGENER WIRKSAMKEIT
失效
NICHTSTEROIDALE(HETERO)ZYKLISCH-SUBSTITUIERTE ACYLANILIDE MIT GEMISCHTER GERMAGENER UND ANDROGENER WIRKSAMKEIT
- Patent Title: NICHTSTEROIDALE (HETERO)ZYKLISCH-SUBSTITUIERTE ACYLANILIDE MIT GEMISCHTER GESTAGENER UND ANDROGENER WIRKSAMKEIT
- Patent Title (English): Non-steroidal (hetero) cyclically substituted acylanilides with mixed gestagen and androgen activity
- Patent Title (中): NICHTSTEROIDALE(HETERO)ZYKLISCH-SUBSTITUIERTE ACYLANILIDE MIT GEMISCHTER GERMAGENER UND ANDROGENER WIRKSAMKEIT
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Application No.: EP98928338.7Application Date: 1998-06-02
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Publication No.: EP0986545B1Publication Date: 2004-12-29
- Inventor: LEHMANN, Manfred , SCHÖLLKOPF, Klaus , STREHLKE, Peter , HEINRICH, Nikolaus , FRITZEMEIER, Karl-Heinrich , MUHN, Hans-Peter , KRATTENMACHER, Rolf
- Applicant: SCHERING AKTIENGESELLSCHAFT
- Applicant Address: Müllerstrasse 170/178 13353 Berlin DE
- Assignee: SCHERING AKTIENGESELLSCHAFT
- Current Assignee: SCHERING AKTIENGESELLSCHAFT
- Current Assignee Address: Müllerstrasse 170/178 13353 Berlin DE
- Priority: DE19723722 19970530
- International Announcement: WO1998054159 19981203
- Main IPC: C07D249/18
- IPC: C07D249/18 ; A61K31/41 ; C07D271/12 ; C07D285/10 ; C07C235/26 ; A61K31/16 ; C07D307/88 ; A61K31/365 ; C07D333/72 ; A61K31/38 ; C07D311/76 ; C07D265/02 ; A61K31/535 ; C07D237/32 ; A61K31/50
Abstract:
The invention relates to non-steroidal gestagens of general formula (I), wherein R?1 and R2¿ are the same or different and stand for a hydrogen atom, a C¿1?-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 C¿1?-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 -CR5=CR6R7, an alkinyl group -C CR5 or for a partially or fully fluorinated C¿1?-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.
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