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1. 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。

2. 发明授权

EP1594869B9 3-SUBSTITUTED-2(ARYLALKYL)-1-AZABICYCLOALKANES AND METHODS OF USE THEREOF 有权
标题翻译： 3-取代的-2（芳基烷基）供其使用-1- azabicycloalkanes AND METHODS
公开(公告)号：EP1594869B9
公开(公告)日：2009-04-01
申请号：EP04713356.6
申请日：2004-02-20
申请人： Targacept, Inc.
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 , C07D453/02
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.

3. 发明授权

EP1594869B1 3-SUBSTITUTED-2(ARYLALKYL)-1-AZABICYCLOALKANES AND METHODS OF USE THEREOF 有权
标题翻译： 3-取代的-2（芳基烷基）供其使用-1- azabicycloalkanes AND METHODS
公开(公告)号：EP1594869B1
公开(公告)日：2007-12-19
申请号：EP04713356.6
申请日：2004-02-20
申请人： Targacept, Inc.
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 , C07D453/02
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.

4. 发明公开

EP1594869A2 3-SUBSTITUTED-2(ARYLALKYL)-1-AZABICYCLOALKANES AND METHODS OF USE THEREOF 有权
标题翻译： 3-取代的-2（芳基烷基）供其使用-1- azabicycloalkanes AND METHODS
公开(公告)号：EP1594869A2
公开(公告)日：2005-11-16
申请号：EP04713356.6
申请日：2004-02-20
申请人： Targacept, Inc.
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 , C07D453/02
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.

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