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1. 发明申请

WO2010028033A1 AMIDES OF DIAZABICYCLOOCTANES AND USES THEREOF 审中-公开
标题翻译：双酚A的氨基酸及其用途
公开(公告)号：WO2010028033A1
公开(公告)日：2010-03-11
申请号：PCT/US2009/055718
申请日：2009-09-02
申请人： TARGACEPT, INC. , STRACHAN, Jon-Paul , BHATTI, Balwinder Singh , MAZUROV, Anatoly , KLUCIK, Jozef , XIAO, Yun-De , HAMMOND, Philip S. , KOMBO, David , MIAO, Lan , SPEAKE, Jason Daniel , YOHANNES, Daniel
发明人： STRACHAN, Jon-Paul , BHATTI, Balwinder Singh , MAZUROV, Anatoly , KLUCIK, Jozef , XIAO, Yun-De , HAMMOND, Philip S. , KOMBO, David , MIAO, Lan , SPEAKE, Jason Daniel , YOHANNES, Daniel
IPC分类号： C07D471/08 , A61K31/407 , A61P25/00
CPC分类号： C07D471/08
摘要： The present invention relates to compounds of the following formulae I and II that bind to and modulate the activity of neuronal nicotinic acetylcholine receptors, to processes for preparing these compounds, to pharmaceutical compositions containing these compounds, and to methods of using these compounds for treating a wide variety of conditions and disorders, including those associated with dysfunction of the central nervous system (CNS). Formula (I ), Formula (Il)
摘要翻译：本发明涉及结合并调节神经元烟碱乙酰胆碱受体的活性，制备这些化合物的方法，含有这些化合物的药物组合物的下式I和II的化合物，以及使用这些化合物治疗各种各样的病症和疾病，包括与中枢神经系统（CNS）功能障碍有关的疾病。式（I），式（II）

2. 发明申请

WO2009111550A1 NICOTINIC ACETYLCHOLINE RECEPTOR SUB-TYPE SELECTIVE AMIDES OF DIAZABICYCLOAL KANES 审中-公开
标题翻译： NICOTINIC乙酰胆碱受体亚型选择性氨基酸
公开(公告)号：WO2009111550A1
公开(公告)日：2009-09-11
申请号：PCT/US2009/036009
申请日：2009-03-04
申请人： TARGACEPT, INC. , AKIREDDY, Srinivisa Rao , BHATTI, Balwinder Singh , BREINING, Scott R. , HAMMOND, Philip S. , HEEMSTRA, Ronald Joseph , MAZUROV, Anatoly , MELVIN, Matt S. , MIAO, Lan , MURTHY, V. Srinivasa , STRACHAN, Jon-Paul , XIAO, Yun-De
发明人： AKIREDDY, Srinivisa Rao , BHATTI, Balwinder Singh , BREINING, Scott R. , HAMMOND, Philip S. , HEEMSTRA, Ronald Joseph , MAZUROV, Anatoly , MELVIN, Matt S. , MIAO, Lan , MURTHY, V. Srinivasa , STRACHAN, Jon-Paul , XIAO, Yun-De
IPC分类号： C07D471/08 , A61K31/407 , A61P25/00
CPC分类号： C07D471/08
摘要： The present invention relates to compounds of the following formula (I) that bind to and modulate the activity of neuronal nicotinic acetylcholine receptors, to processes for preparing these compounds, to pharmaceutical compositions containing these compounds, and to methods of using these compounds for treating a wide variety of conditions and disorders, including those associated with dysfunction of the central nervous system (CNS).
摘要翻译：本发明涉及结合并调节神经元烟碱乙酰胆碱受体活性的下式（I）化合物，制备这些化合物的方法，含有这些化合物的药物组合物，以及使用这些化合物治疗各种各样的病症和疾病，包括与中枢神经系统（CNS）功能障碍有关的疾病。

3. 发明申请

WO2010002971A1 DERIVATIVES OF OXABISPIDINE AS NEURONAL NICOTINIC ACETYLCHOLINE RECEPTOR LIGANDS 审中-公开
标题翻译：奥昔布星作为神经激素乙酰胆碱受体配体的衍生物
公开(公告)号：WO2010002971A1
公开(公告)日：2010-01-07
申请号：PCT/US2009/049373
申请日：2009-07-01
申请人： TARGACEPT, INC. , MAZUROV, Anatoly , MIAO, Lan , XIAO, Yun-de , YOHANNES, Daniel , AKIREDDY, Srinivisa, Rao , BREINING, Scott, R. , KOMBO, David , MURTHY, V. Srinivasa
发明人： MAZUROV, Anatoly , MIAO, Lan , XIAO, Yun-de , YOHANNES, Daniel , AKIREDDY, Srinivisa, Rao , BREINING, Scott, R. , KOMBO, David , MURTHY, V. Srinivasa
IPC分类号： C07D498/04 , A61K31/5386 , A61P25/00
CPC分类号： C07D498/04
摘要： The present invention relates to compounds of formula (I) that bind to and modulate the activity of neuronal nicotinic acetylcholine receptors, to processes for preparing these compounds, to pharmaceutical compositions containing these compounds, and to methods of using these compounds for treating a wide variety of conditions and disorders, including those associated with d sfunction of the central nervous s stem (CNS).
摘要翻译：本发明涉及结合并调节神经元烟碱乙酰胆碱受体的活性，制备这些化合物的方法的式（I）化合物，含有这些化合物的药物组合物，以及使用这些化合物治疗多种多样的方法的病症和障碍，包括与中枢神经干（CNS）功能障碍相关的疾病。

4. 发明申请

WO2010096384A2 FUSED BENZAZEPINES AS NEURONAL NICOTINIC ACETYLCHOLINE RECEPTOR LIGANDS 审中-公开
标题翻译：作为神经烯醇的乙酰胆碱受体配体的熔融苯扎嗪
公开(公告)号：WO2010096384A2
公开(公告)日：2010-08-26
申请号：PCT/US2010/024294
申请日：2010-02-16
申请人： TARGACEPT, INC. , BHATTI, Balwinder Singh , CUTHBERTSON, Timothy, J. , MAZUROV, Anatoly , MITCHENER, Joseph, Pike, Jr. , MUNOZ, Julio, A. , MURTHY, V. Srinivasa , XIAO, Yun-De , YOHANNES, Daniel
发明人： BHATTI, Balwinder Singh , CUTHBERTSON, Timothy, J. , MAZUROV, Anatoly , MITCHENER, Joseph, Pike, Jr. , MUNOZ, Julio, A. , MURTHY, V. Srinivasa , XIAO, Yun-De , YOHANNES, Daniel
IPC分类号： C07D241/36 , C07D223/14 , C07D487/04 , A61P25/28 , A61K31/4985
CPC分类号： C07D487/04 , A61K31/4985 , C07D223/14 , C07D241/36
摘要： The present invention relates to compounds that bind to and modulate the activity of neuronal nicotinic acetylcholine receptors, to processes for preparing these compounds, to pharmaceutical compositions containing these compounds, and to methods of using these compounds for treating a wide variety of conditions and disorders, including those associated with dysfunction of the central nervous system (CNS).
摘要翻译：本发明涉及结合并调节神经元烟碱乙酰胆碱受体的活性，制备这些化合物的方法，含有这些化合物的药物组合物的化合物，以及使用这些化合物治疗各种各样的病症和疾病的方法，包括与中枢神经系统（CNS）功能障碍相关的那些。

5. 发明申请

WO2010028011A1 AMIDES OF DIAZABICYCLONONANES AND USES THEREOF 审中-公开
标题翻译：双酚A的化合物及其用途
公开(公告)号：WO2010028011A1
公开(公告)日：2010-03-11
申请号：PCT/US2009/055687
申请日：2009-09-02
申请人： TARGACEPT, INC. , AKIREDDY, Srinivisa Rao , MAZUROV, Anatoly , YOHANNES, Daniel , MIAO, Lan , SPEAKE, Jason Daniel
发明人： AKIREDDY, Srinivisa Rao , MAZUROV, Anatoly , YOHANNES, Daniel , MIAO, Lan , SPEAKE, Jason Daniel
IPC分类号： C07D471/08 , A61K31/407 , A61P25/00
CPC分类号： C07D471/08
摘要： The present invention relates to compounds of the following formula (I) that bind to and modulate the activity of neuronal nicotinic acetylcholine receptors, to processes for preparing these compounds, to pharmaceutical compositions containing these compounds, and to methods of using these compounds for treating a wide variety of conditions and disorders, including those associated with dysfunction of the central nervous system (CNS).
摘要翻译：本发明涉及结合并调节神经元烟碱乙酰胆碱受体活性的下式（I）化合物，制备这些化合物的方法，含有这些化合物的药物组合物，以及使用这些化合物治疗各种各样的病症和疾病，包括与中枢神经系统（CNS）功能障碍有关的疾病。

6. 发明申请

WO2008057938A1 NICOTINIC ACETYLCHOLINE RECEPTORSUB-TYPE SELECTIVE AMIDES OF DIAZABICYCLOALKANES 审中-公开
标题翻译： NICOTINIC乙酰胆碱受体类型的选择性氨基酸
公开(公告)号：WO2008057938A1
公开(公告)日：2008-05-15
申请号：PCT/US2007/083330
申请日：2007-11-01
申请人： TARGACEPT, INC. , MAZUROV, Anatoly , MIAO, Lan , XIAO, Yun-de , HAMMOND, Philip, S. , MILLER, Craig, H. , AKIREDDY, Srinivisa, Rao , MURTHY, V. Srinivasa , WHITAKER, Regina C. , BREINING, Scott R. , MELVIN, Matt, S.
发明人： MAZUROV, Anatoly , MIAO, Lan , XIAO, Yun-de , HAMMOND, Philip, S. , MILLER, Craig, H. , AKIREDDY, Srinivisa, Rao , MURTHY, V. Srinivasa , WHITAKER, Regina C. , BREINING, Scott R. , MELVIN, Matt, S.
IPC分类号： C07D471/08 , A61P25/00 , A61K31/407 , C07D487/04
CPC分类号： C07D487/04 , C07D471/08
摘要： Compounds, pharmaceutical compositions including the compounds, and methods of preparation and use thereof are disclosed. The compounds are amide compounds which can be prepared from certain heteoraryl carboxylic acids and certain diazabicycloalkanes. The compounds exhibit selectivity for, and bind with high affinity to, neuronal nicotinic receptors of the a4ß2 subtype in the central nervous system (CNS). The compounds and compositions can be used to treat and/or prevent a wide variety of conditions or disorders, particuarly CNS disorders. The compounds can: (i) alter the number of nicotinic cholinergic receptors of the brain of the patient, (ii) exhibit neuroprotective effects, and (iii) when employed in effective amounts, not result in appreciable adverse side effects (e.g. side effects such as significant increases in blood pressure and heart rate, significant negative effects upon the gastrointestinal tract, and significant effects upon skeletal muscle).
摘要翻译：公开了化合物，包括该化合物的药物组合物，及其制备和使用方法。这些化合物是可以由某些芳香羧酸和某些二氮杂双环烷烃制备的酰胺化合物。该化合物对中枢神经系统（CNS）中a4β2亚型的神经元烟碱受体表现出选择性并且以高亲和力结合。化合物和组合物可用于治疗和/或预防各种各样的病症或病症，特别是中枢神经系统疾病。化合物可以：（i）改变患者脑部烟碱性胆碱能受体的数量，（ii）显示出神经保护作用，和（iii）当以有效量使用时，不会产生明显的不良副作用因为血压和心率的显着增加，对胃肠道的显着的负面影响和对骨骼肌的显着影响）。

7. 发明申请

WO2007024814A1 HETEROARYL-SUBSTiTUTED DIAZATRICYCLOALKANES, METHODS FOR ITS PREPARATION AND USE THEREOF 审中-公开
标题翻译：异丁基二异氰酸酯盐，其制备方法及其用途
公开(公告)号：WO2007024814A1
公开(公告)日：2007-03-01
申请号：PCT/US2006/032685
申请日：2006-08-21
申请人： TARGACEPT, INC. , MAZUROV, Anatoly , MIAO, Lan , KLUCIK, Jozef
发明人： MAZUROV, Anatoly , MIAO, Lan , KLUCIK, Jozef
IPC分类号： C07D471/18 , A61K31/439 , A61P25/00
CPC分类号： C07D471/18 , C07D471/14
摘要： The present invention relates to amide and urea derivatives of heteroaryl- substituted diazatricycloalkanes, of the Formula (I) with the definition as set out in the description pharmaceutical compositions including the compounds, methods of preparing the compounds, and methods of treatment using the compounds. More specifically, the methods of treatment involve modulating the activity of the α7 nAChR subtype by administering one or more of the compounds to treat or prevent disorders mediated by the α7 nAChR subtype. The diazatricycloalkanes typically consist of a 1-azabicyclooctane fused to pyrrolidine ring. The substituent heteroaryl groups are 5- or 6-membered ring heteroaromatics, such as 3-pyridinyl and 5-pyrimidinyl moieties, which are attached directly to the diazatricycloalkane. The secondary nitrogen of the pyrrolidine moiety is substituted with an arylcarbonyl (amide type derivative) or an arylaminocarbonyl (N- arylcarbamoyl) (urea type derivative) group. The compounds are beneficial in therapeutic applications requiring a selective interaction at certain nAChR subtypes. That is, the compounds modulate the activity of certain nAChR subtypes, particularly the α7 nAChR subtype, and do not have appreciable activity toward muscarinic receptors. Radiolabeled versions of the compounds can be used in diagnostic methods.
摘要翻译：本发明涉及式（I）的杂芳基取代的二氮三环环烷烃的酰胺和脲衍生物，其定义如本说明书所述的药物组合物包括化合物，制备化合物的方法和使用该化合物的治疗方法。更具体地，治疗方法包括通过施用一种或多种化合物来治疗或预防由a7 nAChR亚型介导的病症来调节a7 nAChR亚型的活性。二氮杂环烷烃通常由与吡咯烷环稠合的1-氮杂双环辛烷组成。取代基杂芳基是5-或6-元环杂芳族化合物，例如3-吡啶基和5-嘧啶基部分，其直接连接到二氮杂环烷烃上。吡咯烷部分的仲氮被芳基羰基（酰胺型衍生物）或芳基氨基羰基（N-芳基氨基甲酰基）（脲型衍生物）基团取代。这些化合物在需要在某些nAChR亚型选择性相互作用的治疗应用中是有益的。也就是说，化合物调节某些nAChR亚型的活性，特别是a7 nAChR亚型，并且对毒蕈碱受体没有明显的活性。化合物的放射性标记版本可用于诊断方法。

8. 发明申请

WO2005037832A3 AZABICYCYCLIC COMPOUNDS FOR RELIEVING PAIN AND TREATING CENTRAL NERVOUS SYSTEM DISORDERS 审中-公开
公开(公告)号：WO2005037832A3
公开(公告)日：2005-04-28
申请号：PCT/US2004/034051
申请日：2004-10-15
申请人： TARGACEPT, INC. , BREINING, Scott R. , BHATTI, Balwinder S. , HAWKINS, Gregory D. , MIAO, Lan , MAZUROV, Anatoly , PHILLIPS, Teresa Y. , MILLER, Craig H.
发明人： BREINING, Scott R. , BHATTI, Balwinder S. , HAWKINS, Gregory D. , MIAO, Lan , MAZUROV, Anatoly , PHILLIPS, Teresa Y. , MILLER, Craig H.
IPC分类号： C07D401/04
摘要： Patients susceptible to or suffering from disorders, such as central nervous system disorders, which are characterized by an alteration in normal neurotransmitter release, such as dopamine release (e.g., Parkinsonism, Parkinson's Disease, Tourette's Syndrome, attention deficient disorder, or schizophrenia), are treated by administering a compound of Formulas (1 or 2), as described herein. The compounds of Formulas (1 and 2) are also useful for treating pain, and treating drug addiction, nicotine addiction, and/or obesity. The compounds can exist as individual stereoisomers, racemic mixtures, diastereomers and the like.

9. 发明申请

WO2010085724A1 PREPARATION AND THERAPEUTIC APPLICATIONS OF (2S,3R)-N-2-((3-PYRIDINYL)METHYL)-1-AZABICYCLO[2.2.2]OCT-3-YL)-3,5-DIFLUOROBENZAMIDE 审中-公开
标题翻译：（2S，3R）-N-2 - （（3-吡啶基）甲基）-1-亚甲基] [2.2.2] OCT-3-YL）-3,5-二氟硼酰胺的制备和治疗应用
公开(公告)号：WO2010085724A1
公开(公告)日：2010-07-29
申请号：PCT/US2010/021926
申请日：2010-01-25
申请人： TARGACEPT, INC. , BENCHERIF, Merouane , FEDOROV, Nikolai , HAUSER, Terry , JORDAN, Kristen , LETCHWORTH, Sharon, Rae , MAZUROV, Anatoly , MUNOZ, Julio, A. , SPEAKE, Jason , YOHANNES, Daniel
发明人： BENCHERIF, Merouane , FEDOROV, Nikolai , HAUSER, Terry , JORDAN, Kristen , LETCHWORTH, Sharon, Rae , MAZUROV, Anatoly , MUNOZ, Julio, A. , SPEAKE, Jason , YOHANNES, Daniel
IPC分类号： C07D453/02 , A61K31/439 , A61P3/00 , A61P25/02 , A61P25/04 , A61P25/06 , A61P25/28 , A61P29/00
CPC分类号： A61K31/444 , C07D453/02
摘要： The present invention relates to compounds that bind to and modulate the activity of neuronal nicotinic acetylcholine receptors, to processes for preparing these compounds, to pharmaceutical compositions containing these compounds, and to methods of using these compounds for treating a wide variety of conditions and disorders, including those associated with dysfunction of the central nervous system (CNS).
摘要翻译：本发明涉及结合并调节神经元烟碱乙酰胆碱受体的活性，制备这些化合物的方法，含有这些化合物的药物组合物的化合物，以及使用这些化合物治疗各种各样的病症和疾病的方法，包括与中枢神经系统（CNS）功能障碍相关的那些。

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