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1. 发明申请

WO2008121686A1 SUB-TYPE SELECTIVE AZABICYCLOALKANE DERIVATIVES 审中-公开
标题翻译：亚型选择性亚硫酰胆碱衍生物
公开(公告)号：WO2008121686A1
公开(公告)日：2008-10-09
申请号：PCT/US2008/058384
申请日：2008-03-27
申请人： TARGACEPT, INC. , HAMMOND, Philip, S. , MAZUROV, Anatoly, A. , XIAO, Yun-De , MURTHY, Srinivasa, V. , AKIREDDY, Srinivasa, Rao
发明人： HAMMOND, Philip, S. , MAZUROV, Anatoly, A. , XIAO, Yun-De , MURTHY, Srinivasa, V. , AKIREDDY, Srinivasa, Rao
IPC分类号： C07D209/52 , C07D221/22 , C07D401/06 , C07D401/12 , C07D403/06 , C07D405/06 , C07D405/12 , C07D413/06 , A61K31/403 , A61K31/439 , A61K31/4439 , A61K31/5355 , A61K31/541 , A61P25/00
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 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, 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，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病症是可以治疗和/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）。

2. 发明申请

WO2008112734A1 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：WO2008112734A1
公开(公告)日：2008-09-18
申请号：PCT/US2008/056607
申请日：2008-03-12
申请人： TARGACEPT, INC. , HAMMOND, Philip, S. , MAZUROV, Anatoly, A. , MIAO, Lan , XIAO, Yun-De , BHATTI, Balwinder , STRACHAN, Jon-Paul , MURTHY, V. Srinivasa , KOMBO, David, C. , AKIREDDY, Srinivasa Rao
发明人： HAMMOND, Philip, S. , MAZUROV, Anatoly, A. , MIAO, Lan , XIAO, Yun-De , BHATTI, Balwinder , STRACHAN, Jon-Paul , MURTHY, V. Srinivasa , KOMBO, David, C. , AKIREDDY, Srinivasa Rao
IPC分类号： C07D471/02 , C07D487/02 , A61K31/407 , A61K31/4353 , A61K31/437 , 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 heteroaryi 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- diazbicyclo [4.3.0]壬烷; 2,8- diazbicyclo [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是一个杂种组; 该化合物对中枢神经系统（CNS）中a402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。

3. 发明申请

WO2004076449A2 3-SUBSTITUTED-2(ARYLALKYL)-1-AZABICYCLOALKANES AND METHODS OF USE THEREOF 审中-公开
标题翻译： 3-取代-2（芳基）-1-氮杂环十二烷及其使用方法
公开(公告)号：WO2004076449A2
公开(公告)日：2004-09-10
申请号：PCT/US2004/005044
申请日：2004-02-20
申请人： TARGACEPT, INC. , MAZUROV, Anatoly, A. , KLUCIK, Jozef , MIAO, Lan , SEAMANS, Angela, S. , PHILLIPS, Teresa, Youngpeter , SCHMITT, Jeffrey, Daniel , MILLER, Craig, Harrison
发明人： MAZUROV, Anatoly, A. , KLUCIK, Jozef , MIAO, Lan , SEAMANS, Angela, S. , PHILLIPS, Teresa, Youngpeter , SCHMITT, Jeffrey, Daniel , MILLER, Craig, Harrison
IPC分类号： C07D453/00
CPC分类号： C07D471/08 , A61K51/0455 , C07D453/02 , C07D487/08
摘要： The present invention relates to 3-substituted-2-(arylalkyl)-1-azabicycloalkanes, methods of preparing the compounds and methods of treatment using the compounds. The azabicycloalkanes generally are azabicycloheptanes, azabicyclooctanes, or azabicyclononanes. The aryl group in the arylalkyl moiety is a 5- or 6-membered ring heteroaromatic, preferably 3-pyridinyl and 5-pyrimidinyl moieties, and the alkyl group is typically a C1-4 alkyl. The substituent at the 3-position of the 1-azabicycloalkane is a carbonyl group-containing moiety, such as an amide, carbamate, urea, thioamide, thiocarbamate, thiourea or similar functionality. The compounds exhibit activity at nicotinic acetylcholine receptors (nAChRs), particularly the a7 nAChR subtype, and are useful towards modulating neurotransmission and the release of ligands involved in neurotransmission. Methods for preventing or treating conditions and disorders, including central nervous system (CNS) disorders, which are characterized by an alteration in normal neurotransmission, are also disclosed. Also disclosed are methods for treating inflammation, autoimmune disorders, pain and excess neovascularization, such as that associated with tumor growth.
摘要翻译：本发明涉及3-取代-2-（芳基烷基）-1-氮杂双环烷烃，制备该化合物的方法和使用该化合物的治疗方法。氮杂双环烷烃通常是氮杂二环庚烷，氮杂二环辛烷或氮杂二环壬烷。芳基烷基部分中的芳基是5或6元环杂芳族，优选3-吡啶基和5-嘧啶基部分，并且烷基典型地为C 1-4烷基。 1-氮杂双环烷烃3-位上的取代基是含羰基的部分，如酰胺，氨基甲酸酯，脲，硫代酰胺，硫代氨基甲酸酯，硫脲或类似的官能团。这些化合物对烟碱型乙酰胆碱受体（nAChRs），特别是a7 nAChR亚型表现出活性，并且可用于调节神经传递和参与神经传递的配体的释放。还公开了预防或治疗以正常神经传递改变为特征的包括中枢神经系统（CNS）障碍的病症和障碍的方法。还公开了用于治疗炎症，自身免疫病症，疼痛和过量新血管形成的方法，例如与肿瘤生长有关的方法。

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