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公开(公告)号：US07579375B2
公开(公告)日：2009-08-25
申请号：US10564720
申请日：2004-07-14
申请人： Haruo Imawaka , Tomoyuki Hasegawa , Shigeru Sakuyama , Yasufumi Kawanaka , Tsutomu Akiyama , Masamitsu Hoshikawa , Saiko Matsuda
发明人： Haruo Imawaka , Tomoyuki Hasegawa , Shigeru Sakuyama , Yasufumi Kawanaka , Tsutomu Akiyama , Masamitsu Hoshikawa , Saiko Matsuda
CPC分类号： C07C59/185 , C07C59/01
摘要： The present invention relates to a compound represented by formula (I) wherein R1 represents optionally protected hydroxy or oxo, indicates α-configuration, β-configuration or a mixture of these in an arbitrary proportion, n represents an integer of 1 to 3, and m represents 0 or an integer of 1 to 10; and wherein two or more R1's are not bound to the same carbon atom other than the terminal carbon atom, a salt thereof or a prodrug thereof. The compounds represented by formula (I) have an ability to improve astrocyte function, and they are useful as a preventive and/or therapeutic agent for a brain infarction, neuronal dysfunction by brain infarction, Parkinson's disease, Parkinson's syndrome, amyotrophic lateral sclerosis or Alzheimer's disease.
摘要翻译： 本发明涉及由式（I）表示的化合物，其中R 1表示任选保护的羟基或氧代，
表示alpha配置，beta配置或其任意比例的混合，n表示整数 为1〜3，m为0或1〜10的整数， 并且其中两个或更多个R1不与除了末端碳原子之外的相同碳原子，其盐或其前药结合。 由式（I）表示的化合物具有改善星形胶质细胞功能的能力，并且它们可用作脑梗塞的预防和/或治疗剂，脑梗死的神经元功能障碍，帕金森病，帕金森综合征，肌萎缩性侧索硬化或阿尔茨海默病 疾病。
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公开(公告)号：US20070167522A1
公开(公告)日：2007-07-19
申请号：US10564720
申请日：2004-07-14
申请人： Haruo Imawaka , Tomoyuki Hasegawa , Shigeru Sakuyama , Yasufumi Kawanaka , Tsutomu Akiyama , Masamitsu Hoshikawa , Saiko Matsuda
发明人： Haruo Imawaka , Tomoyuki Hasegawa , Shigeru Sakuyama , Yasufumi Kawanaka , Tsutomu Akiyama , Masamitsu Hoshikawa , Saiko Matsuda
IPC分类号： A61K31/20
CPC分类号： C07C59/185 , C07C59/01
摘要： The present invention relates to a compound represented by formula (I) wherein R1 represents optionally protected hydroxy or oxo, indicates α-configuration, β-configuration or a mixture of these in an arbitary proportion, n represents an integer of 1 to 3, and m represents 0 or an integer of 1 to 10; and wherein two or more R1's are not bound to the same carbon atom other than the terminal carbon atom, a salt thereof or a prodrug thereof. The compounds represented by formula (I) have an ability to improve astrocyte function, and they are useful as a preventive and/or therapeutic agent for a brain infarction, neuronal dysfunction by brain infarction, Parkinson's disease, Parkinson's syndrome, amyotrophic lateral sclerosis or Alzheimer's disease.
摘要翻译： 本发明涉及由式（I）表示的化合物，其中R 1表示任选保护的羟基或氧代，
表示alpha配置，beta配置或这些 任意比例，n表示1〜3的整数，m表示0或1〜10的整数， 并且其中两个或更多个R 1不与除了末端碳原子之外的相同碳原子，其盐或其前药结合。 由式（I）表示的化合物具有改善星形胶质细胞功能的能力，并且它们可用作脑梗塞的预防和/或治疗剂，脑梗死的神经元功能障碍，帕金森病，帕金森综合征，肌萎缩性侧索硬化或阿尔茨海默病 疾病。
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公开(公告)号：US08273916B2
公开(公告)日：2012-09-25
申请号：US12872384
申请日：2010-08-31
IPC分类号： C07B57/00
CPC分类号： C07C53/128
摘要： According to the present invention, crystals comprising (2R)-2-propyloctanoic acid and an amine, which can be used as bulk drugs for safely orally administrable solid preparations with keeping the pharmacological effect, are provided. Among these crystals, the crystal with dibenzylamine per se is particularly useful as bulk drug for pharmaceuticals and can be used as an intermediate to produce (2R)-2-propyloctanoic acid having an optical purity of more than 99.5% e.e. which has not been obtained.
摘要翻译： 根据本发明，提供了包含（2R）-2-丙基辛酸和胺的晶体，其可以用作用于安全口服给药的固体制剂的主要药物，并具有药理作用。 在这些晶体中，具有二苄基胺本身的结晶特别可用作药物的大量药物，并且可以用作中间体以产生光学纯度大于99.5％e.e的（2R）-2-丙基辛酸。 尚未获得。
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公开(公告)号：US20100331414A1
公开(公告)日：2010-12-30
申请号：US12872384
申请日：2010-08-31
CPC分类号： C07C53/128
摘要： According to the present invention, crystals comprising (2R)-2-propyloctanoic acid and an amine, which can be used as bulk drugs for safely orally administrable solid preparations with keeping the pharmacological effect, are provided. Among these crystals, the crystal with dibenzylamine per se is particularly useful as bulk drug for pharmaceuticals and can be used as an intermediate to produce (2R)-2-propyloctanoic acid having an optical purity of more than 99.5% e.e. which has not been obtained.
摘要翻译： 根据本发明，提供了包含（2R）-2-丙基辛酸和胺的晶体，其可以用作用于安全口服给药的固体制剂的主要药物，并具有药理作用。 在这些晶体中，具有二苄基胺本身的结晶特别可用作药物的大量药物，并且可以用作中间体以产生光学纯度大于99.5％e.e的（2R）-2-丙基辛酸。 尚未获得。
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公开(公告)号：US07820715B2
公开(公告)日：2010-10-26
申请号：US11579071
申请日：2005-04-27
IPC分类号： A61K31/205 , C07C229/00 , C07B57/00
CPC分类号： C07C53/128
摘要： Crystals comprising (2R)-2-propyloctoic acid and an amine which retain the pharmacological effect of (2R)-2-propyloctoic acid and can be safely used as a medicinal raw drug for peroral solid preparations. Of these crystals, the crystals especially with dibenzylamine are advantageous because not only the crystals themselves are useful as a medicinal raw drug but also use of the crystals as an intermediate can yield (2R)-2-propyloctoic acid having an optical purity exceeding 99.5% e.e., which has not been obtained hitherto.
摘要翻译： 包含（2R）-2-丙基辛酸和维持（2R）-2-丙基辛酸的药理作用的胺的晶体，可以安全地用作口服固体制剂的药用原料药。 在这些晶体中，特别是二苄胺的结晶是有利的，因为不仅晶体本身可用作药用原料，而且使用晶体作为中间体可以产生光学纯度超过99.5％的（2R）-2-丙基辛酸， ee，迄今尚未获得。
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公开(公告)号：US20080090907A1
公开(公告)日：2008-04-17
申请号：US11579071
申请日：2005-04-27
CPC分类号： C07C53/128
摘要： Crystals comprising (2R)-2-propyloctoic acid and an amine which retain the pharmacological effect of (2R)-2-propyloctoic acid and can be safely used as a medicinal raw drug for peroral solid preparations. Of these crystals, the crystals especially with dibenzylamine are advantageous because not only the crystals themselves are useful as a medicinal raw drug but also use of the crystals as an intermediate can yield (2R)-2-propyloctoic acid having an optical purity exceeding 99.5% e.e., which has not been obtained hitherto.
摘要翻译： 包含（2R）-2-丙基辛酸和维持（2R）-2-丙基辛酸的药理作用的胺的晶体，可以安全地用作口服固体制剂的药用原料药。 在这些晶体中，特别是二苄胺的结晶是有利的，因为不仅晶体本身可用作药用原料，而且使用晶体作为中间体可以产生光学纯度超过99.5％的（2R）-2-丙基辛酸， ee，迄今尚未获得。
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