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1. 发明授权

US08633227B2 Synthesis and novel salt forms of (R)-3-((E)-pyrrolidin-3-yl)vinyl)-5-tetrahydropyran-4-yloxy)pyridine 有权
标题翻译：（R）-3 - （（E） - 吡咯烷-3-基）乙烯基）-5-四氢吡喃-4-基氧基）吡啶的合成和新型盐形式
公开(公告)号：US08633227B2
公开(公告)日：2014-01-21
申请号：US13125892
申请日：2009-11-30
申请人： Srinivasa Rao Akireddy , Scott R. Breining , Timothy J. Cuthbertson , Gary Maurice Dull , Gregory J. Gatto , John Genus , Philip S. Hammond , Joesph Pike Mitchener, Jr. , Julio A. Munoz , Pieter Albert Otten , Daniel Yohannes , Nikolai Fedorov
发明人： Srinivasa Rao Akireddy , Scott R. Breining , Timothy J. Cuthbertson , Gary Maurice Dull , Gregory J. Gatto , John Genus , Philip S. Hammond , Joesph Pike Mitchener, Jr. , Julio A. Munoz , Pieter Albert Otten , Daniel Yohannes , Nikolai Fedorov
IPC分类号： A61K31/4433 , C07D405/14
CPC分类号： A61K31/4439 , C07D405/14
摘要： The present invention relates to (R)-3-((E)-2-(pyrrolidin-3-yl)vinyl)-5-(tetrahydropyran-4-yloxy)pyridine, its salt forms, and to processes for the commercial-scale production of these compounds in sufficient purity and quality for use in pharmaceutical compositions.
摘要翻译：本发明涉及（R）-3 - （（E）-2-（吡咯烷-3-基）乙烯基）-5-（四氢吡喃-4-基氧基）吡啶及其盐形式，这些化合物的大规模生产具有足够的纯度和质量用于药物组合物。

2. 发明申请

US20120015983A1 Synthesis and Novel Salt Forms of (R)-3-((E)-pyrrolidin-3-yl)vinyl)-5-tetrahydropyran-4-yloxy)pyridine 有权
标题翻译：（R）-3 - （（E） - 吡咯烷-3-基）乙烯基）-5-四氢吡喃-4-基氧基）吡啶的合成和新型盐形式
公开(公告)号：US20120015983A1
公开(公告)日：2012-01-19
申请号：US13125892
申请日：2009-11-30
申请人： Srinivasa Rao Akireddy , Scott R. Breining , Timothy J. Cuthbertson , Gary Maurice Dull , Gregory J. Gatto , John Genus , Philip S. Hammond , Joseph Pike Mitchener , Julio A. Munoz , Pieter Albert Otten , Daniel Yohannes , Nikolai Fedorov
发明人： Srinivasa Rao Akireddy , Scott R. Breining , Timothy J. Cuthbertson , Gary Maurice Dull , Gregory J. Gatto , John Genus , Philip S. Hammond , Joseph Pike Mitchener , Julio A. Munoz , Pieter Albert Otten , Daniel Yohannes , Nikolai Fedorov
IPC分类号： A61K31/4439 , A61P29/00 , A61P25/18 , A61P25/28 , A61P31/12 , A61P25/04 , A61P3/00 , C07D405/14 , A61P31/04
CPC分类号： A61K31/4439 , C07D405/14
摘要： The present invention relates to (R)-3-((E)-2-(pyrrolidin-3-yl)vinyl)-5-(tetrahydropyran-4-yloxy)pyridine, its salt forms, and to processes for the commercial-scale production of these compounds in sufficient purity and quality for use in pharmaceutical compositions.
摘要翻译：本发明涉及（R）-3 - （（E）-2-（吡咯烷-3-基）乙烯基）-5-（四氢吡喃-4-基氧基）吡啶及其盐形式，这些化合物的大规模生产具有足够的纯度和质量用于药物组合物。

3. 发明申请

US20140288169A1 NICOTINIC RECEPTOR NON-COMPETITIVE ANTAGONISTS 审中-公开
标题翻译： NICOTINIC RECEPTOR非竞争性拮抗剂
公开(公告)号：US20140288169A1
公开(公告)日：2014-09-25
申请号：US13978583
申请日：2012-01-05
申请人： Srinivasa Rao Akireddy , Scott R. Breining , Matt S. Melvin , Srinivasa V. Murthy , Anatoly A. Mazurov , Balwinder Singh Bhatti , Jon-Paul Strachan , Ronald Joseph Heemstra , Todd Showalter , Yunde Xiao , Philip S. Hammond , Lan Miao , David Kombo , Daniel Yohannes , Jason Speake
发明人： Srinivasa Rao Akireddy , Scott R. Breining , Matt S. Melvin , Srinivasa V. Murthy , Anatoly A. Mazurov , Balwinder Singh Bhatti , Jon-Paul Strachan , Ronald Joseph Heemstra , Todd Showalter , Yunde Xiao , Philip S. Hammond , Lan Miao , David Kombo , Daniel Yohannes , Jason Speake
IPC分类号： C07D493/08 , C07C211/38
CPC分类号： C07D493/08 , C07C211/38 , C07C2602/40 , C07C2602/42 , C07C2602/44
摘要： The present invention relates to compounds that modulate nicotinic receptors as non-competitive antagonists, methods for their synthesis, methods for their use, and their pharmaceutical compositions.
摘要翻译：本发明涉及将烟碱受体调节为非竞争性拮抗剂的化合物，其合成方法，其使用方法及其药物组合物。

4. 发明申请

US20110071180A1 SUB-TYPE SELECTIVE AMIDES OF DIAZABICYCLOALKANES 审中-公开
标题翻译：亚类型的亚型选择性氨基酸
公开(公告)号：US20110071180A1
公开(公告)日：2011-03-24
申请号：US12919970
申请日：2009-03-04
申请人： Srinivasa Rao Akireddy , Balwinder Singh Bhatti , Scott R. Breining , Philip S. Hammond , Ronald Joseph Heemstra , Anatoly A. Mazurov , Matt S. Melvin , Lan Miao , V. Srinivasa Murthy , Jon-Paul Strachan , Yunde Xiao
发明人： Srinivasa Rao Akireddy , Balwinder Singh Bhatti , Scott R. Breining , Philip S. Hammond , Ronald Joseph Heemstra , Anatoly A. Mazurov , Matt S. Melvin , Lan Miao , V. Srinivasa Murthy , Jon-Paul Strachan , Yunde Xiao
IPC分类号： A61K31/439 , C07D487/04 , C07D471/08 , A61K31/407 , A61K31/4439 , A61P25/00 , A61P25/28 , A61P25/18
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。

5. 发明授权

US07754708B2 N-aryl azaspiroalkene and azaspiroalkane compounds and methods of preparation and use thereof 失效
标题翻译： N-芳基氮杂螺烯和氮杂环烷烃化合物及其制备方法和用途
公开(公告)号：US07754708B2
公开(公告)日：2010-07-13
申请号：US12117946
申请日：2008-05-09
申请人： Balwinder Bhatti , Scott R. Breining , Philip S. Hammond , Jozef Klucik , Yun-De Xiao
发明人： Balwinder Bhatti , Scott R. Breining , Philip S. Hammond , Jozef Klucik , Yun-De Xiao
IPC分类号： A61K31/4406 , A61K31/4418 , A61K31/397 , A61P25/22 , A61P25/24
CPC分类号： C07D413/04 , C07D401/04
摘要： Compounds, pharmaceutical compositions including the compounds, and methods of preparation and use thereof are disclosed. The compounds are N-aryl or heteroaryl azaspiroalkene/alkane compounds, prodrugs or metabolites of these compounds, or pharmaceutically acceptable salts thereof. The aryl group can be a phenyl ring or a five- or six-membered heterocyclic ring (heteroaryl). The compounds and compositions can be used to treat and/or prevent a wide variety of conditions or disorders, particularly those disorders characterized by dysfunction of nicotinic cholinergic neurotransmission, including disorders involving neuromodulation of neurotransmitter release, such as dopamine release. CNS disorders, which are characterized by an alteration in normal neurotransmitter release, are another example of disorders that can be treated and/or prevented. The compounds and compositions can also be used to alleviate pain. 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 gastro-intestinal 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。化合物是N-芳基或杂芳基氮杂螺烯/烷烃化合物，这些化合物的前药或代谢物，或其药学上可接受的盐。芳基可以是苯环或五元或六元杂环（杂芳基）。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，特别是以烟碱型胆碱能神经传递功能障碍为特征的疾病，包括涉及神经递质释放神经调节的疾病，如多巴胺释放。其特征在于正常神经递质释放的改变的CNS疾病是可以治疗和/或预防的疾病的另一个例子。化合物和组合物也可用于缓解疼痛。化合物可以：（i）改变患者脑部烟碱性胆碱能受体的数量，（ii）表现出神经保护作用，和（iii）当以有效量使用时，不会产生明显的不利副作用（例如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以及对骨骼肌的显着影响）。

6. 发明申请

US20100081683A1 NICOTINIC ACETYLCHOLINE RECEPTOR SUB-TYPE SELECTIVE AMIDES OF DIAZABICYCLOALKANES 有权
标题翻译： NICOTINIC乙酰胆碱受体亚型选择性氨基酸
公开(公告)号：US20100081683A1
公开(公告)日：2010-04-01
申请号：US12447850
申请日：2007-11-01
申请人： Anatoly Mazurov , Lan Miao , Yun-De Xiao , Philip S. Hammond , Craig H. Miller , Srinivisa Rao Akireddy , V.Srinivasa Murthy , Regina C. Whitaker , Scott R. Breining , Matt S. Melvin
发明人： Anatoly Mazurov , Lan Miao , Yun-De Xiao , Philip S. Hammond , Craig H. Miller , Srinivisa Rao Akireddy , V.Srinivasa Murthy , Regina C. Whitaker , Scott R. Breining , Matt S. Melvin
IPC分类号： A61K31/439 , C07D487/04 , C07D471/04 , A61K31/407 , A61K31/42 , C07D261/18 , A61P25/18
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 a4β2 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, particularly 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）中的a4和bgr2亚型的神经元烟碱受体具有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/或预防多种病症或病症，特别是CNS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

US20080242689A1 N-ARYL AZASPIROALKENE AND AZASPIROALKANE COMPOUNDS AND METHODS OF PREPARATION AND USE THEREOF 失效
标题翻译： N-ARYL AZASPIROALKENE和AZASPIROALKANE化合物及其制备和使用方法
公开(公告)号：US20080242689A1
公开(公告)日：2008-10-02
申请号：US12117946
申请日：2008-05-09
申请人： Balwinder Bhatti , Scott R. Breining , Philip S. Hammond , Jozef Klucik , Yun-De Xiao
发明人： Balwinder Bhatti , Scott R. Breining , Philip S. Hammond , Jozef Klucik , Yun-De Xiao
IPC分类号： A61K31/4427 , A61P25/00 , A61K31/4439
CPC分类号： C07D413/04 , C07D401/04
摘要： Compounds, pharmaceutical compositions including the compounds, and methods of preparation and use thereof are disclosed. The compounds are N-aryl or heteroaryl azaspiroalkene/alkane compounds, prodrugs or metabolites of these compounds, or pharmaceutically acceptable salts thereof. The aryl group can be a phenyl ring or a five- or six-membered heterocyclic ring (heteroaryl). The compounds and compositions can be used to treat and/or prevent a wide variety of conditions or disorders, particularly those disorders characterized by dysfunction of nicotinic cholinergic neurotransmission, including disorders involving neuromodulation of neurotransmitter release, such as dopamine release. CNS disorders, which are characterized by an alteration in normal neurotransmitter release, are another example of disorders that can be treated and/or prevented. The compounds and compositions can also be used to alleviate pain. 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 gastro-intestinal 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。化合物是N-芳基或杂芳基氮杂螺烯/烷烃化合物，这些化合物的前药或代谢物，或其药学上可接受的盐。芳基可以是苯环或五元或六元杂环（杂芳基）。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，特别是以烟碱型胆碱能神经传递功能障碍为特征的疾病，包括涉及神经递质释放神经调节的疾病，如多巴胺释放。其特征在于正常神经递质释放的改变的CNS疾病是可以治疗和/或预防的疾病的另一个例子。化合物和组合物也可用于缓解疼痛。化合物可以：（i）改变患者脑部烟碱性胆碱能受体的数量，（ii）表现出神经保护作用，和（iii）当以有效量使用时，不会产生明显的不利副作用（例如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以及对骨骼肌的显着影响）。

8. 发明授权

US08268860B2 Sub-type selective amides of diazabicycloalkanes 失效
标题翻译：二氮杂双环烷烃的亚型选择性酰胺
公开(公告)号：US08268860B2
公开(公告)日：2012-09-18
申请号：US12723790
申请日：2010-03-15
申请人： Anatoly A. Mazurov , Lan Miao , Yun-De Xiao , Philip S. Hammond , Craig H. Miller , Srinivisa Rao Akireddy , V. Srinivasa Murthy , Regina C. Whitaker , Scott R. Breining , Matt S. Melvin
发明人： Anatoly A. Mazurov , Lan Miao , Yun-De Xiao , Philip S. Hammond , Craig H. Miller , Srinivisa Rao Akireddy , V. Srinivasa Murthy , Regina C. Whitaker , Scott R. Breining , Matt S. Melvin
IPC分类号： A61K43/42 , A01N31/44
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 heteroaryl carboxylic acids and certain diazabicycloalkanes. The compounds exhibit selectivity for, and bind with high affinity to, neuronal nicotinic receptors of the α4β2 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, particularly 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杂芳基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α4和bgr2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/或预防多种病症或病症，特别是CNS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）显示神经保护作用，和（iii）当以有效量使用时，不会产生明显的副作用（例如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）。

9. 发明授权

US07384929B2 N-aryl azaspiroalkene and azaspiroalkane compounds and methods of preparation and use thereof 失效
标题翻译： N-芳基氮杂螺烯和氮杂环烷烃化合物及其制备方法和用途
公开(公告)号：US07384929B2
公开(公告)日：2008-06-10
申请号：US11230140
申请日：2005-09-19
申请人： Balwinder Bhatti , Scott R. Breining , Philip S. Hammond , Jozef Klucik , Yun-De Xiao
发明人： Balwinder Bhatti , Scott R. Breining , Philip S. Hammond , Jozef Klucik , Yun-De Xiao
IPC分类号： A61K31/397 , A61K33/4402 , A61K33/4406 , A61K33/4409 , C07D211/18 , C07D215/06 , C07D217/04 , C07D219/02 , C07D221/20 , C07D237/08 , C07D239/26 , C07D239/42 , C07D401/04 , C07D261/06 , C07D271/06 , C07D413/04 , C07D498/10 , C07D271/10 , C07D257/02 , C07D417/04 , C07D513/10 , A61K31/501 , A61K31/497 , A61K31/427
CPC分类号： C07D413/04 , C07D401/04
摘要： Compounds, pharmaceutical compositions including the compounds, and methods of preparation and use thereof are disclosed. The compounds are N-aryl or heteroaryl azaspiroalkene/alkane compounds, prodrugs or metabolites of these compounds, or pharmaceutically acceptable salts thereof. The aryl group can be a phenyl ring or a five- or six-membered heterocyclic ring (heteroaryl). The compounds and compositions can be used to treat and/or prevent a wide variety of conditions or disorders, particularly those disorders characterized by dysfunction of nicotinic cholinergic neurotransmission, including disorders involving neuromodulation of neurotransmitter release, such as dopamine release. CNS disorders, which are characterized by an alteration in normal neurotransmitter release, are another example of disorders that can be treated and/or prevented. The compounds and compositions can also be used to alleviate pain. 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 gastro-intestinal 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。化合物是N-芳基或杂芳基氮杂螺烯/烷烃化合物，这些化合物的前药或代谢物，或其药学上可接受的盐。芳基可以是苯环或五元或六元杂环（杂芳基）。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，特别是以烟碱型胆碱能神经传递功能障碍为特征的疾病，包括涉及神经递质释放神经调节的疾病，如多巴胺释放。其特征在于正常神经递质释放的改变的CNS疾病是可以治疗和/或预防的疾病的另一个例子。化合物和组合物也可用于缓解疼痛。化合物可以：（i）改变患者脑部烟碱性胆碱能受体的数量，（ii）表现出神经保护作用，和（iii）当以有效量使用时，不会产生明显的不利副作用（例如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以及对骨骼肌的显着影响）。

10. 发明申请

US20100173932A1 SUB-TYPE SELECTIVE AMIDES OF DIAZABICYCLOALKANES 失效
标题翻译：亚类型的亚型选择性氨基酸
公开(公告)号：US20100173932A1
公开(公告)日：2010-07-08
申请号：US12723790
申请日：2010-03-15
申请人： Anatoly Mazurov , Lan Miao , Yun-De Xiao , Philip S. Hammond , Craig H. Miller , Srinivisa Rao Akireddy , V. Srinivasa Murthy , Regina C. Whitaker , Scott R. Breining , Matt S. Melvin
发明人： Anatoly Mazurov , Lan Miao , Yun-De Xiao , Philip S. Hammond , Craig H. Miller , Srinivisa Rao Akireddy , V. Srinivasa Murthy , Regina C. Whitaker , Scott R. Breining , Matt S. Melvin
IPC分类号： A61K31/407 , C07D487/04 , C07D471/04 , A61K31/4375 , A61K31/4439 , A61K31/422 , A61P25/00 , A61P25/28 , A61P25/18
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 heteroaryl carboxylic acids and certain diazabicycloalkanes. The compounds exhibit selectivity for, and bind with high affinity to, neuronal nicotinic receptors of the α4β2 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, particularly 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杂芳基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α4和bgr2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/或预防多种病症或病症，特别是CNS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）。

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