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1. 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）。

2. 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）。

3. 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）。

4. 发明申请

US20100144700A1 HETEROCYCLIC-CARBONYL-DIAZABICYCLOALKANES AS MODULATORS OF THE NEURONAL NICOTINIC ACETYLCHOLINE ALPHA 4 BETA 2, SUBTYPE RECEPTOR FOR THE TREATMENT OF CNS RELATED DISORDERS 审中-公开
标题翻译：作为神经细胞性乙酰胆碱酯酶4β2的调节剂的杂环碳二亚氨基二醇，用于治疗CNS相关疾病的亚型受体
公开(公告)号：US20100144700A1
公开(公告)日：2010-06-10
申请号：US12530997
申请日：2008-03-12
申请人： Philip S. Hammond , Anatoly A. Mazurov , Lan Miao , Yun-De Xiao , Balwinder Singh Bhatti , Jon-Paul Strachan , V. Srinivasa Murthy , David C. Kombo , Srinivisa Rao Akireddy
发明人： Philip S. Hammond , Anatoly A. Mazurov , Lan Miao , Yun-De Xiao , Balwinder Singh Bhatti , Jon-Paul Strachan , V. Srinivasa Murthy , David C. Kombo , Srinivisa Rao Akireddy
IPC分类号： A61K31/439 , C07D471/08 , C07D487/04 , C07D471/04 , A61K31/407 , A61K31/422 , A61K31/437 , A61K31/4353 , A61P25/00 , A61P25/28 , A61P25/18
CPC分类号： C07D487/04 , C07D471/04 , C07D471/08
摘要： A compound of Formula 1: A-C(O)-Cy, wherein A is a diazabicyclic core, containing 7, 8, or 9 ring atoms, and selected from the following: 2,6-diazabicyclo[3.2.0]heptane; 3,6-diazabicyclo[3.ZO]heptane; 2,7-diazabicyclo[4.2.0]octane; 3,7-diazabicyclo[4.2.0]octane; 3,8-diazabicyclo[4.2.0]octane; 2,7-diazabicyclo[3.3.0]octane; 2,7-diazbicyclo[4.3.0]nonane; 2,8-diazbicyclo[4.3.0]nonane; 3,7-diazabicyclo[4.3.0]nonane; 3,8-diazabicyclo[4.3.0]nonane; 3,9-diazabicyclo[4.3.0]nonane; 2,6-diazabicyclo[3.2.1]octane; 3,6-diazabicyclo[3.2.1]octane; wherein the diazabicycle is attached as a radical to the depicted carbonyl via either one of the two ring nitrogen atoms, such that the carbonyl forms an amide bond with the ring nitrogen; Cy is a heteroaryl group; The compounds exhibit selectivity for, and bind with high affinity to, neuronal nicotinic receptors of the α402 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 are believed to: (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, namely 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：式1的化合物：A-C（O）-Cy，其中A是具有7,8或9个环原子的二氮杂双环核心，并且选自以下：2,6-二氮杂双环[3.2.0]庚烷; 3,6-二氮杂双环[3.ZO]庚烷; 2,7-二氮杂双环[4.2.0]辛烷; 3,7-二氮杂双环[4.2.0]辛烷; 3,8-二氮杂双环[4.2.0]辛烷; 2,7-二氮杂双环[3.3.0]辛烷; 2,7-二氮杂双环[4.3.0]壬烷; 2,8-二氮杂双环[4.3.0]壬烷; 3,7-二氮杂双环[4.3.0]壬烷; 3,8-二氮杂双环[4.3.0]壬烷; 3,9-二氮杂双环[4.3.0]壬烷; 2,6-二氮杂双环[3.2.1]辛烷; 3,6-二氮杂双环[3.2.1]辛烷; 其中所述二氮杂双环通过两个环氮原子中的任一个连接到所描绘的羰基上，使得羰基与环氮形成酰胺键; Cy是杂芳基; 该化合物对中枢神经系统（CNS）中α402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。这些化合物被认为是：（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影响如血压和心率显着升高，对胃肠道的显着负面影响，以及对骨骼肌的显着影响。

5. 发明申请

US20100173968A1 SUB-TYPE SELECTIVE AZABICYCLOALKANE DERIVATIVES 失效
标题翻译：亚型选择性亚硫酰胆碱衍生物
公开(公告)号：US20100173968A1
公开(公告)日：2010-07-08
申请号：US12593779
申请日：2008-03-27
申请人： Philip S. Hammond , Anatoly Mazurov , Yun-De Xiao , Srinivasa V. Murthy , Srinivisa Rao Akireddy
发明人： Philip S. Hammond , Anatoly Mazurov , Yun-De Xiao , Srinivasa V. Murthy , Srinivisa Rao Akireddy
IPC分类号： A61K31/403 , C07D209/52 , A61P25/18 , A61P25/28
CPC分类号： C07D209/52 , C07D221/22 , C07D401/06 , C07D401/12 , C07D403/06 , C07D405/06 , C07D405/12 , C07D413/06
摘要： Compounds, pharmaceutical compositions including the compounds, and methods of preparation and use thereof are disclosed. The compounds are amide, ketone, and ester compounds prepared from certain azabicycloalkane carboxylic acids. The resulting 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, such as 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 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。这些化合物是由某些氮杂双环烷烃羧酸制备的酰胺，酮和酯化合物。所得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/或预防各种各样的病症或病症，例如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的神经调节的疾病，例如多巴胺释放。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）。

6. 发明授权

US08198296B2 Sub-type selective azabicycloalkane derivatives 失效
标题翻译：亚型选择性氮杂双环烷烃衍生物
公开(公告)号：US08198296B2
公开(公告)日：2012-06-12
申请号：US12593779
申请日：2008-03-27
申请人： Philip S. Hammond , Anatoly Mazurov , Yun-De Xiao , Srinivasa V. Murthy , Srinivisa Rao Akireddy
发明人： Philip S. Hammond , Anatoly Mazurov , Yun-De Xiao , Srinivasa V. Murthy , Srinivisa Rao Akireddy
IPC分类号： A61K31/439 , C07D221/22 , C07D221/02
CPC分类号： C07D209/52 , C07D221/22 , C07D401/06 , C07D401/12 , C07D403/06 , C07D405/06 , C07D405/12 , C07D413/06
摘要： Compounds, pharmaceutical compositions including the compounds, and methods of preparation and use thereof are disclosed. The compounds are amide, ketone, and ester compounds prepared from certain azabicycloalkane carboxylic acids. The resulting 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, such as 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 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。这些化合物是由某些氮杂双环烷烃羧酸制备的酰胺，酮和酯化合物。所得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/或预防各种各样的病症或病症，例如以烟碱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的神经调节的疾病，例如多巴胺释放。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）。

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