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1. 发明授权

US08980923B2 Compositions and methods for selective inhibition of nicotine acetylcholine receptors 有权
标题翻译：用于选择性抑制尼古丁乙酰胆碱受体的组合物和方法
公开(公告)号：US08980923B2
公开(公告)日：2015-03-17
申请号：US13526076
申请日：2012-06-18
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
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αb亚基的烟碱乙酰胆碱受体的方法。选择性抑制缺乏α5亚基的烟碱型乙酰胆碱受体的方法可以在体内或体外进行。

2. 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。

3. 发明申请

US20120329783A1 COMPOSITIONS AND METHODS FOR SELECTIVE INHIBITION OF NICOTINE ACETYLCHOLINE RECEPTORS 有权
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：US20120329783A1
公开(公告)日：2012-12-27
申请号：US13526076
申请日：2012-06-18
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 , A61K31/4515 , A61K31/454 , A61P25/14 , A61K31/55 , A61P25/34 , A61P25/00 , C07D211/46 , C12N5/071
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αb亚基的烟碱乙酰胆碱受体的方法。选择性抑制缺乏α5亚基的烟碱型乙酰胆碱受体的方法可以在体内或体外进行。

4. 发明授权

US07531555B2 Compositions and methods for selective inhibition of nicotine acetylcholine receptors 失效
标题翻译：用于选择性抑制尼古丁乙酰胆碱受体的组合物和方法
公开(公告)号：US07531555B2
公开(公告)日：2009-05-12
申请号：US10956957
申请日：2004-09-30
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： A61K31/445 , C07D211/40
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。

5. 发明授权

US06673800B2 4,5,-dihydroisoxazolylakylpiperazine 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4,5'-二氢异恶唑烷基哌嗪衍生物及其制备
公开(公告)号：US06673800B2
公开(公告)日：2004-01-06
申请号：US09838253
申请日：2001-04-20
申请人： Hun Yeong Koh , Kyung Il Choi , Yong Seo Cho , Ae Nim Pae , Jae Yang Kong , Dae Young Jeong , Sun Ho Jung , Ji Young Jung , Hee-Yoon Lee
发明人： Hun Yeong Koh , Kyung Il Choi , Yong Seo Cho , Ae Nim Pae , Jae Yang Kong , Dae Young Jeong , Sun Ho Jung , Ji Young Jung , Hee-Yoon Lee
IPC分类号： A61K31496
CPC分类号： C07D413/04 , C07D261/08
摘要： The present invention relates to 4,5-dihydroisoxazolylalkylpiperazine derivatives having selective biological activity at dopamine D3 and 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和D4受体中具有选择性生物活性的4,5-二氢异恶唑基烷基哌嗪衍生物及其还原胺还原胺化反应的制备方法，其中R1，R2， X和n与说明书中定义的相同。

6. 发明授权

US08299072B2 Pyrazolylmethylamine compounds as calcium channel modulators and preparation method thereof 有权
标题翻译：吡唑基甲胺化合物作为钙通道调节剂及其制备方法
公开(公告)号：US08299072B2
公开(公告)日：2012-10-30
申请号：US12568243
申请日：2009-09-28
申请人： Ghilsoo Nam , Kyung Il Choi , Hye Ran Kim , Seon Hee Seo , Yoon Jee Kim , Hee Sup Shin , Dong Jin Kim , Ae Nim Pae , Hye Jin Chung , Hyunah Choo , Hyewhon Rhim , Yong Seo Cho , Eun Joo Roh , Gyo Chang Keum , Kee Hyun Choi , Kye Jung Shin , Hoh Gyu Hahn , Chan Seong Cheong , Jae Kyun Lee , Kee Dal Nam , Yong Koo Kang , Youngsoo Kim , Woong Seo Park , Eunice Eun-Kyeong Kim , Key-Sun Kim , Hesson Chung , Dong Yun Shin , Chi man Song
发明人： Ghilsoo Nam , Kyung Il Choi , Hye Ran Kim , Seon Hee Seo , Yoon Jee Kim , Hee Sup Shin , Dong Jin Kim , Ae Nim Pae , Hye Jin Chung , Hyunah Choo , Hyewhon Rhim , Yong Seo Cho , Eun Joo Roh , Gyo Chang Keum , Kee Hyun Choi , Kye Jung Shin , Hoh Gyu Hahn , Chan Seong Cheong , Jae Kyun Lee , Kee Dal Nam , Yong Koo Kang , Youngsoo Kim , Woong Seo Park , Eunice Eun-Kyeong Kim , Key-Sun Kim , Hesson Chung , Dong Yun Shin , Chi man Song
IPC分类号： A61K31/496 , A61K31/506 , A61K31/5377 , C07D231/12 , C07D401/04 , C07D403/12 , C07D405/12 , C07D405/14 , C07D413/10
CPC分类号： C07D231/12 , C07D401/04 , C07D405/04 , C07D405/10 , C07D405/12
摘要： The present invention relates to pyrazolylmethylamine-piperazine derivatives and their pharmaceutically acceptable salts effective as calcium channel modulators and a method of manufacturing the same. The present invention also relates to the medicinal use of the above compounds as therapeutic treatment of diseases due to their effect as calcium channel modulators.
摘要翻译：本发明涉及作为钙通道调节剂有效的吡唑基甲胺 - 哌嗪衍生物及其药学上可接受的盐及其制备方法。本发明还涉及由于其作为钙通道调节剂的作用而使上述化合物作为疾病的治疗性治疗的药物用途。

7. 发明授权

US07939672B2 Phenylacetate derivatives or pharmaceutically acceptable salts thereof, preparation method thereof and composition for prevention or treatment of diseases induced by activation of T-type calcium ion channel containing the same as an active ingredient 有权
标题翻译：苯乙酸衍生物或其药学上可接受的盐，其制备方法和预防或治疗由含有其作为活性成分的T型钙离子通道激活引起的疾病的组合物
公开(公告)号：US07939672B2
公开(公告)日：2011-05-10
申请号：US12429004
申请日：2009-04-23
申请人： Kye Jung Shin , Hyung Kook Lee , Eun Joo Roh , Dong Jin Kim , Kyung Il Choi , Hyewhon Rhim , Hye Jin Chung , Seon Hee Seo
发明人： Kye Jung Shin , Hyung Kook Lee , Eun Joo Roh , Dong Jin Kim , Kyung Il Choi , Hyewhon Rhim , Hye Jin Chung , Seon Hee Seo
IPC分类号： C07D235/08
CPC分类号： C07D211/34 , C07D211/14 , C07D211/18 , C07D211/22 , C07D211/70 , C07D235/14 , C07D235/16 , C07D295/145 , C07D295/15
摘要： Disclosed herein are a new phenylacetate derivative represented by Chemical Formula 1 or pharmaceutically acceptable salt thereof, a preparation method thereof, and a composition for prevention or treatment of diseases induced by the activation of T-type calcium ion channels containing the same. The composition containing the phenylacetate derivative according to the present invention effectively inhibits the activation of T-type calcium ion channels and may be useful in the prevention or treatment of diseases such as hypertension, cancer, epilepsy, and neurogenic pains induced by the activation of T-type calcium ion channels. wherein, X, R1, and R3 are as defined herein.
摘要翻译：本文公开了由化学式1表示的新的苯乙酸酯衍生物或其药学上可接受的盐，其制备方法，以及用于预防或治疗由含有其的T型钙离子通道活化引起的疾病的组合物。含有本发明的苯乙酸酯衍生物的组合物有效地抑制T型钙离子通道的活化，并且可用于预防或治疗诸如高血压，癌症，癫痫和T激活诱导的神经源性疼痛等疾病型钙离子通道。其中X，R 1和R 3如本文所定义。

8. 发明授权

US08492384B2 Imidazolylalkylcarbonyl derivatives as calcium channel modulators and preparation method thereof 有权
标题翻译：咪唑烷基羰基衍生物作为钙通道调节剂及其制备方法
公开(公告)号：US08492384B2
公开(公告)日：2013-07-23
申请号：US12492615
申请日：2009-06-26
申请人： Kyung Il Choi , Ghilsoo Nam , Hye Ran Kim , Hyewhon Rhim , Seon Hee Seo , Yoon Jee Kim , Hee Sup Shin , Dong Jin Kim , Ae Nim Pae , Hye Jin Chung , Yong Seo Cho , Hyunah Choo , Eun Joo Roh , Soon Bang Kang , Kye Jung Shin , Hoh Gyu Hahn , Dong Yun Shin , Chan Seong Cheong , Kee Dal Nam , Yong Koo Kang , Jae Kyun Lee , Woong Seo Park , Youngsoo Kim , Eunice Eun-Kyeong Kim , Key-Sun Kim , Hesson Chung , Gyo Chang Keum , Cheolju Lee , Kee Hyun Choi
发明人： Kyung Il Choi , Ghilsoo Nam , Hye Ran Kim , Hyewhon Rhim , Seon Hee Seo , Yoon Jee Kim , Hee Sup Shin , Dong Jin Kim , Ae Nim Pae , Hye Jin Chung , Yong Seo Cho , Hyunah Choo , Eun Joo Roh , Soon Bang Kang , Kye Jung Shin , Hoh Gyu Hahn , Dong Yun Shin , Chan Seong Cheong , Kee Dal Nam , Yong Koo Kang , Jae Kyun Lee , Woong Seo Park , Youngsoo Kim , Eunice Eun-Kyeong Kim , Key-Sun Kim , Hesson Chung , Gyo Chang Keum , Cheolju Lee , Kee Hyun Choi
IPC分类号： A61K31/496 , C07D233/64
CPC分类号： C07D233/60 , C07D209/48 , C07D233/54 , C07D233/61 , C07D403/06
摘要： Disclosed are novel imidazolylalkylcarbonyl derivatives useful as calcium channel modulators and a preparation method of the same. Also disclosed is a method for the treatment of diseases by administering the above compounds based on their inhibitory activity against calcium channel.
摘要翻译：公开了可用作钙通道调节剂的新型咪唑烷基羰基衍生物及其制备方法。还公开了通过基于其对钙通道的抑制活性施用上述化合物来治疗疾病的方法。

9. 发明授权

US08383631B2 1,6-disubstituted-3-amino-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-C]pyridin-7-one compounds and preparation thereof 有权
标题翻译： 1,6-二取代-3-氨基-4,5,6,7-四氢-1H-吡唑并[3,4-C]吡啶-7-酮化合物及其制备
公开(公告)号：US08383631B2
公开(公告)日：2013-02-26
申请号：US12883987
申请日：2010-09-16
申请人： Ghilsoo Nam , Ae Nim Pae , Kyung Il Choi , Hyunah Choo , Vani Nelamane Devegowda , Seon Hee Seo
发明人： Ghilsoo Nam , Ae Nim Pae , Kyung Il Choi , Hyunah Choo , Vani Nelamane Devegowda , Seon Hee Seo
IPC分类号： C07D471/04 , A61K31/496
CPC分类号： C07D471/04
摘要： Provided are a novel 1,6-disubstituted-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridin-7-one compound, a pharmaceutically acceptable salt compound thereof, a method for preparing the compound, and an anticancer pharmaceutical composition including the compound as an effective ingredient.
摘要翻译：提供了新颖的1,6-二取代-4,5,6,7-四氢-1H-吡唑并[3,4-c]吡啶-7-酮化合物，其药学上可接受的盐化合物，制备化合物的方法，以及包含该化合物作为有效成分的抗癌药物组合物。

10. 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。

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