Non-steroidal (hetero) cyclically substd. acylanilides with mixed gestagen and androgen activity

• Main Authors: MANFRED LEHMANN, KLAUS SCHAELLKOPF, PETER STREHLKE
• Format: Patent
• Language: Chinese; English
• Published: 24.12.2008
• Subjects: ACYCLIC OR CARBOCYCLIC COMPOUNDS; CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

The invention relates to non-steroidal gestagens of general formula (I), wherein R and R 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 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 , an alkenyl group -CR =CR R , an alkinyl group -CCR 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 endometriosi