SCHWEDE, WOLFGANG,KLAR, ULRICH,MÖLLER, CARSTEN,ROTGERI, ANDREA,BONE, WILHELM,HUWE, CHRISTOPH
申请号:
ES11702458
公开号:
ES2539715T3
申请日:
2011.02.08
申请国别(地区):
ES
年份:
2015
代理人:
摘要:
17-Hydroxy-17-pentafluoroethyl-estra-4,9 (10) -dien-11-aryl derivatives of the general chemical formula I: ** Formula ** in which R1 and R2 are the same or different and mean hydrogen, a C1-C10 alkyl radical optionally substituted with dimethylamino, a 6-10 membered aryl radical, which is optionally substituted once, twice or multiple times with a halogen (-F, -Cl, -Br, -I), - OH, -O-alkyl, -C (O) OH, -C (O) O-alkyl, -C (O) NH2, -C (O) NH-alkyl, -C (O) N-dialkyl, -C (O) NH-aryl, -C (O) NH-heteroaryl, -NH2, -NH (C1-C10 alkyl), -N (C1-C10 alkyl) 2, in particular with -N (CH3) 2, -NHC (O) -alkyl, -NO2, -N3, -CN, -C1-C10 alkyl, -fluoro-C1-C10 alkyl, -C1-C10 acyl, -C1-C10 acyloxy, -SO2NH2, -SO2NH-alkyl or -SO2N-dialkyl, a 5-10 membered heteroaryl radical, which is optionally substituted once, twice or multiple times with the 6-10 membered aryl radical substituents mentioned above, a arylalkyl radical or C1-C6, which is optionally substituted next to the aryl ring once, twice or multiple times with the 6-10 membered aryl radical substituents mentioned above, or a C1-C6 heteroarylalkyl radical, which is optionally substituted next to the heteroaryl ring once, twice or multiple times with the 6-10 membered aryl radical substituents mentioned above, or else R1 and R2 are in common a component part of a ring of 3-10 members, which is optionally substituted together with carbon with alkyl, carboxyl, alkoxycarbonyl, alkylcarbonyl, aminocarbonyl, arylalkyl, heteroarylalkyl or aminoalkyl or respectively with nitrogen with alkyl, alkanoyl, carboxyl, alkoxycarbonyl, phenyl, phenylalkyl, pyridinyl, pyrimidinyl, pyrazinyl, sulfonyl, benzoyl, alkylsulfonyl, arylsulfonyl, aminocarbonyl, aminocarbonylalkyl, arylalkyl, heterocyclylalkyl, heteroarylalkyl and aminoalkyl or, which eventually contains nitrogen, oxygen or sulfur atoms that may eventually be oxidized to form the sulfoxide or the sulfone, and an aromatic radical may be condensed with the 3- membered ring, X represents an oxygen