Derivatives of 3-oxo-10?-hydroxy-17?-cyanomethyl(oxy/thio) carbonyl-androsta-1,4-diene-17alpha- carboxylic acid esters and pharmaceutical
compositions comprising them
申请(专利)号： IL20050172776
专利号： IL172776A 主分类号： A61K
申请权利人： GLAXO GROUP
LIMITED 公开国代码： IL 优先权国家： GB;
EP
摘 要：
A process for preparing a compound of formula (I): wherein
X represents O or S;
R 1 represents C 1-6 alkyl, C 3-8
cycloalkyl, C 3-8 cycloalkylmethyl or C 3-8 cycloalkenyl any of which optionally may be substituted by one or more methyl groups or halogen atoms or R 1 represents aryl, 4-(diethylamino)sulphonylphenyl, 2,6-
申请日： 2005-12-22 公开公告日： 2015-05-31
分类号： A61K;
A61P; A61P5/44; C07D215/26; C07D233/54; C07D451/02; C07J; C07J1; C07J3 发明设计人： 申请国代码： IL
优先权： 20030711 GB
0316290; 20040709 EP 2004007819
摘 要 附 图：
difluorophenyl, 4-methoxyphenyl, 3-difluoromethylthiophenyl, 4-cyanophenyl, heteroaryl, 5-chloro-4-methoxy-thiophene-3-yl, 2-isopropyl-1,3-thiazol-4-yl, 5-trifluoromethylfuran-2-yl, 5-methylsulphonyl-thiophene-2-yl, 5-methylthio-thiophene-2-yl or 5-ethyl-isoxazol-3-yl;
R 2 represents hydrogen, methyl, which may be in either the ± or 2 configuration, or methylene;
R 3 and R 4 are the same or different and each independently represents hydrogen, halogen or a methyl group; and represents a single or a double bond;
or a physiologically acceptable salt or solvate thereof;
comprising the reaction of a carboxylic acid (X=O) or carbothioic acid (X=S) of formula (II)
wherein R 1 , R 2 , R 3 , R 4 , X and are as defined for formula (I) above;
with a compound of formula L-CH 2 CN wherein L represents a leaving group. 主权项：
权 利 要 求 说 明 书
【Derivatives of 3-oxo-10?-hydroxy-17?-cyanomethyl(oxy/thio) carbonyl-androsta-1,4-diene-17alpha- carboxylic acid esters and pharmaceutical compositions comprising them】的权利说明书内容是......请下载后查看
Derivatives of 3-oxo-10
