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Compounds with hydroxycarbonyl-halogenoalkyl side chains

机译:具有羟羰基-卤代烷基侧链的化合物

摘要

The present invention provides a compound consisting of a moiety and a group chemically bonded to said moiety, wherein said moiety contains a compound having low activity following oral administration or its parent scaffold and said group has the following general formula (1): embedded imagein which R1 represents a hydrogen atom, etc., R2 represents a C1-C7 halogenoalkyl group, etc., m represents an integer of 2 to 14, and n represents an integer of 2 to 7, or enantiomers of the compound, or hydrates or pharmaceutically acceptable salts of the compound or enantiomers thereof. The above compound is advantageous in pharmaceutical use because the group of general formula (1) allows compounds such as anti-estrogenic ones to show a significantly increased activity following oral administration when attached to the parent scaffolds of the compounds.
机译:本发明提供了由部分和与该部分化学键合的基团组成的化合物,其中所述部分包含口服给药后活性低的化合物或其母体支架,并且所述基团具有以下通式(1): <图像alt =“嵌入式图像” file =“ US20050192449A1-20050901-C00001.GIF” he =“ 14.82mm” imgContent =“ chem” imgFormat =“ GIF” wi =“ 60.62mm“ /> 在其中 R 1 代表氢原子等, R 2 表示C 1 -C 7 卤代烷基等,m表示2至14的整数,n表示2至7的整数,或化合物或其化合物或对映体的水合物或药学上可接受的盐。上述化合物在药学上是有利的,因为通式(1)的基团使化合物例如抗雌激素化合物当与化合物的母体支架连接时口服显示出显着增加的活性。

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