专利名称:14beta-H-, 14- and 15-EN-11beta -aryl-4-estrenes
发明人:WOLFGANG SCHWEDE,ECKHARD
OTTOW,GUNTER NEEF,ARWEDCLEVE,KRZYSZTOF CHWALISZ,HORSTMICHNA,ULRIKE FUHRMANN
申请号:AU9111091申请日:19911221公开号:AU659118B2公开日:19950511
摘要:PCT No. PCT/EP91/02494 Sec. 371 Date Jun. 22, 1993 Sec. 102(e) Date Nov. 1,1993 PCT Filed Dec. 21, 1991 PCT Pub. No. WO92/11278 PCT Pub. Date Jul. 9, 1992.Novelcompounds of the general formula I (I) and the pharmacologically tolerable additionsalts thereof with acids are described, in which either Ia) R11 represents a hydrogen atomin the beta -configuration and each of R12 and R13 represents a hydrogen atom, or Ib)R11 represents a hydrogen atom in the beta -configuration and R12 and R13 togetherrepresent a second bond, or Ic) R11 and R12 together represent a second bond and R13represents a hydrogen atom, or Id) R11 represents a hydrogen atom in the alpha -configuration and R12 and R13 together represent a second bond, and in Ia), Ib), Ic) or Id)X represents an oxygen atom, the hydroxyimino grouping >N DIFFERENCE OH or twohydrogen atoms, R1 represents a hydrogen atom or a methyl group, R2 represents ahydroxy group, a C1-C10-alkoxy group or a C1-C10-acyloxy group, and R3 and R4 havethe meanings customary for competitive progesterone antagonists specified in the
description. The invention relates also to processes for the preparation of the novelcompounds, to pharmaceutical compositions containing those compounds, to their usefor the manufacture of medicaments, and to the novel intermediates required for theprocess. The novel compounds have a strong affinity for the gestagen receptor andexhibit pronounced antigestagenic and also antiglucocorticoid, antimineralocorticoid andantiandrogenic properties.
申请人:SCHERING AKTIENGESELLSCHAFT
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