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21. 发明申请

US20090062339A1 COMPOSITIONS AND METHODS FOR SELECTIVE INHIBITION OF NICOTINE ACETYLCHOLINE RECEPTORS 审中-公开
标题翻译： NICOTINE乙酰胆碱受体选择性抑制的组合物和方法
公开(公告)号：US20090062339A1
公开(公告)日：2009-03-05
申请号：US12264768
申请日：2008-11-04
申请人： Roger L. Papke , Nicole A. Horenstein , Michael M. Francis , Kyung Il Choi
发明人： Roger L. Papke , Nicole A. Horenstein , Michael M. Francis , Kyung Il Choi
IPC分类号： A61K31/4465 , C07D211/44 , C07K14/705
CPC分类号： C07D211/44
摘要： The present invention concerns methods for treating or preventing neurological disorders characterized by dysfunction of nicotinic acetylcholine receptors by administering 2,2,6,6-tetramethylpiperidin-4-yl heptanoate (TMPH), or a pharmaceutically acceptable salt thereof, to the patient. In another aspect, the present invention pertains to pharmaceutical compositions containing TMPH, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier. In another aspect, the present invention pertains to methods for selectively inhibiting nicotinic acetylcholine receptors that lack an α5, α6, or β3 subunit by contacting an effective amount of TMPH, or a pharmaceutically acceptable salt thereof, to the receptor. The method for selectively inhibiting nicotinic acethylcholine receptors that lack an α5 subunit can be carried out in vivo or in vitro.
摘要翻译：本发明涉及通过向患者施用2,2,6,6-四甲基哌啶-4-基庚酸酯（TMPH）或其药学上可接受的盐来治疗或预防特征为烟碱乙酰胆碱受体功能障碍的神经障碍的方法。另一方面，本发明涉及含有TMPH或其药学上可接受的盐和药学上可接受的载体的药物组合物。另一方面，本发明涉及通过使有效量的TMPH或其药学上可接受的盐与受体接触来选择性地抑制缺乏α5，α6或β3亚基的烟碱乙酰胆碱受体的方法。选择性抑制缺乏α5亚基的烟碱乙酰胆碱受体的方法可以在体内或体外进行。

22. 发明授权

US07388101B1 Tetrahydrofuran derivatives having cis substituent, their intermediates, and their preparation method 失效
标题翻译：具有顺式取代基的四氢呋喃衍生物及其制备方法
公开(公告)号：US07388101B1
公开(公告)日：2008-06-17
申请号：US11732602
申请日：2007-04-04
申请人： Yong Seo Cho , Hyunah Choo , Joo Hwan Cha , Ae Nim Pae , Satish N. Chavre , Kyung Il Choi
发明人： Yong Seo Cho , Hyunah Choo , Joo Hwan Cha , Ae Nim Pae , Satish N. Chavre , Kyung Il Choi
IPC分类号： C07D307/02
CPC分类号： C07D307/12
摘要： The present invention relates to a tetrahydrofuran compound having cis substituents, the derivatives thereof and a process for preparing the same, and in particular relates to a dihydrofuran-3-ylidene triflate compound having cis substituents at C2 and C5 positions prepared through Prins-type cyclization using a homopropargylic alcohol derivative as a starting material in the presence of Lewis acid catalyst, a tetrahydrofuran compound having cis substituents at C2, C3 and C5 positions prepared through the hydrolysis of triflate group in the derivatives of the dihydrofuran-3-ylidene triflate compound, and a preparation method thereof.The derivatives and the target tetrahydrofuran compound prepared according to the present invention are hydrofuran compounds with novel structures having cis substituents at C2, C3 and/or C5 positions, which are useful as a derivative for synthesizing drugs such as an antagonist for neurokinin receptor.
摘要翻译：本发明涉及具有顺式取代基的四氢呋喃化合物及其衍生物及其制备方法，特别涉及在C 2上具有顺式取代基的二氢呋喃-3-亚基三氟甲磺酸酯化合物和在路易斯酸催化剂存在下，使用均二炔醇衍生物作为起始原料，在C 2 N 2上具有顺式取代基的四氢呋喃化合物，通过Prins-型环化制备的C 5 H 3位，通过在二氢呋喃-3-亚基三氟甲磺酸酯化合物的衍生物中水解三氟甲磺酸酯基制备的C 3和C 5 H 3位及其制备方法。根据本发明制备的衍生物和目标四氢呋喃化合物是具有在C 2，C 3和/或C 5上具有顺式取代基的新结构的氢呋喃化合物其可用作合成药物的衍生物，例如用于神经激肽受体的拮抗剂。

23. 发明授权

US06723724B2 Isoxazolylalkylpiperazine derivatives having selective biological activity at dopamine D3 or D4 receptor, and preparation thereof 失效
标题翻译：在多巴胺D3或D4受体上具有选择性生物活性的异恶唑基烷基哌嗪衍生物及其制备
公开(公告)号：US06723724B2
公开(公告)日：2004-04-20
申请号：US09839206
申请日：2001-04-23
申请人： Hun Yeong Koh , Kyung Il Choi , Yong Seo Cho , Ae Nim Pae , Kyung Ho Kang , Mi Young Cha , Jae Yang Kong , Dae Young Jeong , Hee-Yoon Lee
发明人： Hun Yeong Koh , Kyung Il Choi , Yong Seo Cho , Ae Nim Pae , Kyung Ho Kang , Mi Young Cha , Jae Yang Kong , Dae Young Jeong , Hee-Yoon Lee
IPC分类号： A61K31496
CPC分类号： C07D413/04 , C07D261/08 , C07D413/14
摘要： The present invention relates to isoxazolylalkylpiperazine derivatives having selective biological activity at dopamine D3 or D4 receptors represented by the following formula (1), and its preparation method through reductive amination reaction in the presence of reducing agent, wherein R1, R2, X and n are the same as defined in the specification.
摘要翻译：本发明涉及在下列通式（1）表示的多巴胺D3或D4受体中具有选择性生物活性的异恶唑基烷基哌嗪衍生物及其还原胺还原反应的制备方法，其中R1，R2，X和n为与说明书中定义的相同。

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