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DERIVATIVES OF 9α ESTRATRIENE AS ER-B SELECTIVE LIGANDS FOR PREVENTION OF INTESTINAL CANCER
专利权人:
БАЙЕР ШЕРИНГ ФАРМА АКЦИЕНГЕЗЕЛЬШАФТ (DE)
发明人:
ФРИТЕЦМАЙЕР Карл-Генрих (DE),ДИЛЬ Патрик (DE),ХЕРТРАМПФ Торстен (DE)
申请号:
RU2011104569/15
公开号:
RU2011104569A
申请日:
2009.07.09
申请国别(地区):
RU
年份:
2012
代理人:
摘要:
1. The use of derivatives of 9α-estra-1,3,5 (10) -triene of the formula (I)! ! in which the radicals R3, R9, R16, R17 and R17 independently of one another have the following meanings:! R3 means a hydrogen atom or a group R18 in which! R18 means a straight or branched, saturated or unsaturated C1-C6 alkyl radical, a trifluoromethyl group, an aryl, heteroaryl or aralkyl radical, a substituted aryl, heteroaryl radical with at least one radical independently selected from methyl, ethyl, trifluoromethyl, pentafluoroethyl , trifluoromethylthio, methoxy, ethoxy, nitro, cyano, halo (fluoro, chloro, bromo, iodo), hydroxy, amino,! mono (C1-8-alkyl) or di (C1-8-alkyl) amino, where both alkyl groups are identical or different, di (aralkyl) amino, where both aralkyl groups are identical or different, carboxyl, carboxyalkoxy,! C1-C20-acyl groups or C1-C20-acyloxy as substituents, the acyl radical —C (= O) R19, in which R19 is a straight or branched hydrocarbon radical containing up to 10 carbon atoms, which is saturated or unsaturated in up to three positions and is partially or fully halogenated, or! R18 means a group R20SO2 in which! R20 represents a group R21R22N, where R21 and R22 independently represent a hydrogen atom, a C1-C5 alkyl radical, a C (O) R23 group in which R23 means an unsubstituted or substituted, unbranched or branched hydrocarbon radical containing up to 10 carbon atoms, which is saturated or unsaturated in up to three positions and is partially or fully halogenated, the cyclopropyl group, cyclobutyl, cyclopentyl1. Применение производных 9α-эстра-1,3,5(10)-триена формулы (I) ! ! в которой радикалы R3, R9, R16, R17 и R17 независимо друг от друга имеют следующие значения: ! R3 означает атом водорода или группу R18, в которой ! R18 означает неразветвленный или разветвленный, насыщенный или ненасыщенный радикал C1-C6-алкила, группу трифторметила, радикал арила, гетероарила или аралкила, радикал замещенного арила, гетероарила, по крайней мере, с одним радик
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