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公开(公告)号:US06610733B2
公开(公告)日:2003-08-26
申请号:US10149748
申请日:2002-06-13
申请人: SungDae Park , HeeAn Kwon , HongKi Kim , PilSu Ho , Kazumi Morikawa , Yoshitake Kanbe , Masahiro Nishimoto , MyungHwa Kim
发明人: SungDae Park , HeeAn Kwon , HongKi Kim , PilSu Ho , Kazumi Morikawa , Yoshitake Kanbe , Masahiro Nishimoto , MyungHwa Kim
IPC分类号: A61K31385
CPC分类号: C07D335/06 , C07D311/38 , C07D311/58
摘要: The present invention includes a compound having the following general formula (1): in which x represents an oxygen atom or a sulfur atom, m represents an integer of 2 to 14, and n represents an integer of 2 to 7, or hydrates or pharmaceutically acceptable salts thereof. The compound of general formula (1) is advantageous in pharmaceutical use because of its far superior anti-estrogenic activity over the corresponding racemic mixture.
摘要翻译: 本发明包括具有以下通式(1)的化合物:其中x表示氧原子或硫原子,m表示2〜14的整数,n表示2〜7的整数,或水合物或药学上可接受的盐 其中。 由于其相对于相应的外消旋混合物具有优异的抗雌激素活性,通式(1)的化合物在药物应用中是有利的。
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公开(公告)号:US06737417B2
公开(公告)日:2004-05-18
申请号:US10149752
申请日:2002-06-13
申请人: JaeChon Jo , HeeAn Kwon , HyunSuk Lim , JaeYoung Choi , Kazumi Morikawa , Yoshitake Kanbe , Masahiro Nishimoto , MyungHwa Kim , Yoshikazu Nishimura
发明人: JaeChon Jo , HeeAn Kwon , HyunSuk Lim , JaeYoung Choi , Kazumi Morikawa , Yoshitake Kanbe , Masahiro Nishimoto , MyungHwa Kim , Yoshikazu Nishimura
IPC分类号: C07J100
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): in 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.
摘要翻译: 本发明提供由部分和化学键合到所述部分的基团组成的化合物,其中所述部分含有口服后具有低活性的化合物或其母体支架,并且所述基团具有以下通式(1):其中R 1表示 氢原子等,R2表示C1-C7卤代烷基等,m表示2〜14的整数,n表示2〜7的整数,或该化合物的对映异构体或其水合物或药学上可接受的盐 其化合物或其对映异构体。 上述化合物在药物用途中是有利的,因为通式(1)的基团允许化合物如抗雌激素的化合物在连接到化合物的母体支架上时在口服给药后显示出显着增加的活性。
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公开(公告)号:US07196081B2
公开(公告)日:2007-03-27
申请号:US10281990
申请日:2002-10-29
申请人: JaeChon Jo , HeeAn Kwon , HyunSuk Lim , JaeYoung Choi , Kazumi Morikawa , Yoshitake Kanbe , Masahiro Nishimoto , MyungHwa Kim , Yoshikazu Nishimura
发明人: JaeChon Jo , HeeAn Kwon , HyunSuk Lim , JaeYoung Choi , Kazumi Morikawa , Yoshitake Kanbe , Masahiro Nishimoto , MyungHwa Kim , Yoshikazu Nishimura
IPC分类号: C07D265/36 , C07D303/18 , C07D209/12 , C07D333/56 , A61K31/20 , A61K31/538 , A61P35/00 , A61K31/565 , A61K31/381 , C07D311/60
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): in 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.
摘要翻译: 本发明提供由部分和化学键合到所述部分的基团组成的化合物,其中所述部分含有口服后具有低活性的化合物或其母体支架,并且所述基团具有以下通式(1):
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公开(公告)号:US20050192449A1
公开(公告)日:2005-09-01
申请号:US11115134
申请日:2005-04-27
申请人: JaeChon Jo , HeeAn Kwon , HyunSuk Lim , JaeYoung Choi , Kazumi Morikawa , Yoshitake Kanbe , Masahiro Nishimoto , MyungHwa Kim , Yoshikazu Nishimura
发明人: JaeChon Jo , HeeAn Kwon , HyunSuk Lim , JaeYoung Choi , Kazumi Morikawa , Yoshitake Kanbe , Masahiro Nishimoto , MyungHwa Kim , Yoshikazu Nishimura
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): in 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.
摘要翻译: 本发明提供了由部分和化学键合到所述部分的基团组成的化合物,其中所述部分含有口服后具有低活性的化合物或其母体支架,所述基团具有以下通式(1):其中R R 1表示氢原子等,R 2表示C 1 -C 7卤代烷基等 m表示2〜14的整数,n表示2〜7的整数,或该化合物的对映异构体,或其化合物或其对映异构体的水合物或药学上可接受的盐。 上述化合物在药物用途中是有利的,因为通式(1)的基团允许化合物如抗雌激素的化合物在连接到化合物的母体支架上时在口服给药后显示出显着增加的活性。
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