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1. 发明申请

WO2009018367A3 SALT FORMS OF (2S)-(4E)-N-METHYL-5-[3-(5-METHOXYPYRIDIN)YL]-4-PENTEN-2-AMINE 审中-公开
标题翻译：（2S） - （4E）-N-甲基-5- [3-（5-甲氧基吡啶）基] -4-苯基-2-胺的盐形式
公开(公告)号：WO2009018367A3
公开(公告)日：2010-05-27
申请号：PCT/US2008071631
申请日：2008-07-30
申请人： TARGACEPT INC , DULL GARY MAURICE , MUNOZ JULIO A , GENUS JOHN , BHATTI BALWINDER SINGH , YOUNG JENNIFER A , BENCHERIF MEROUANE , JAMES JOHN W , WILLIAMS MICHAEL G , JORDAN KRISTEN , LIPPIELLO PATRICK M , FORDHAM-MEIER BETH
发明人： DULL GARY MAURICE , MUNOZ JULIO A , GENUS JOHN , BHATTI BALWINDER SINGH , YOUNG JENNIFER A , BENCHERIF MEROUANE , JAMES JOHN W , WILLIAMS MICHAEL G , JORDAN KRISTEN , LIPPIELLO PATRICK M , FORDHAM-MEIER BETH
IPC分类号： C07D213/62 , A61K31/44 , A61P25/28
CPC分类号： C07D213/62
摘要： Salts of (2S)-(4E)-N-methyl-5-[3-(5-methoxypyridin)yl]-4-penten-2-amine, methods for their preparation, pharmaceutical compositions comprising said salts, and their use are disclosed. The salts can be administered to patients susceptible to or suffering from conditions and disorders, such as central nervous system disorders, to treat or prevent such disorders.
摘要翻译：（2S） - （4E）-N-甲基-5- [3-（5-甲氧基吡啶）基] -4-戊烯-2-胺的盐，其制备方法，包含所述盐的药物组合物及其用途披露。盐可以施用于易患或患有诸如中枢神经系统疾病的病症和障碍的患者，以治疗或预防这些疾病。

2. 发明申请

WO2010096384A3 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：WO2010096384A3
公开(公告)日：2011-01-13
申请号：PCT/US2010024294
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 , A61K31/4985 , A61P25/28 , C07D223/14 , C07D487/04
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。

3. 发明申请

WO2006053039A3 HYDROXYBENZOATE SALTS OF METANICOTINE COMPOUNDS 审中-公开
标题翻译：金属化合物的羟基苯甲酸盐
公开(公告)号：WO2006053039A3
公开(公告)日：2006-12-07
申请号：PCT/US2005040588
申请日：2005-11-09
申请人： TARGACEPT INC , DULL GARY M , MUNOZ JULIO A , GENUS JOHN , MOORE JAMES R
发明人： DULL GARY M , MUNOZ JULIO A , GENUS JOHN , MOORE JAMES R
IPC分类号： C07D213/46 , A61K31/4406
CPC分类号： C07D213/38 , C07D213/65 , C07D213/73 , C07D213/75 , C07D401/12
摘要： Patients susceptible to or suffering from conditions and disorders, such as central nervous system disorders, are treated by administering to a patient in need thereof compositions that are hydroxybenzoate salts of E-metanicotine-type compounds. The formation of hydroxybenzoate salts of the E-metanicotine compounds is also useful in purifying the E-metanicotine compounds, as the hydroxybenzoate salts tend to crystallize out, leaving impurities such as Z-metanicotine compounds, and compounds where the double bond has migrated, in solution. If desired, the hydroxybenzoate salts can be converted to either the free base (the E-metanicotine) or to another pharmaceutically acceptable salt form. E-metanicotine-type compounds that include a five-membered heteroaryl ring linked to an olefinic linker, such as a penten-2-amine linker, which is linked to a terminal amine group, are also disclosed. Patients susceptible to or suffering from conditions and disorders, such as central nervous system disorders, can be treated by administering the compounds, pharmaceutical salts of the compounds, or pharmaceutical compositions including the compounds or their salts, to a patient in need thereof.
摘要翻译：通过向有需要的患者施用作为E-间断脒类化合物的羟基苯甲酸盐的组合物来治疗易患或患有病症和障碍的患者，例如中枢神经系统疾病。 E-间烟碱化合物的羟基苯甲酸盐的形成也可用于纯化E-间烟碱化合物，因为羟基苯甲酸盐倾向于结晶出来，留下杂质如Z-间苯ic啶化合物和双键已经迁移的化合物解。如果需要，羟基苯甲酸盐可以转化为游离碱（E-间烟碱）或另一种药学上可接受的盐形式。还公开了包括与烯属连接体连接的五元杂芳环的E-间断烟碱型化合物，例如与末端胺基连接的戊烯-2-胺连接体。可以通过将化合物，化合物的药物盐或包含该化合物或其盐的药物组合物给予有需要的患者来治疗易患或患有病症和障碍（例如中枢神经系统疾病）的患者。

4. 发明申请

WO2006053082A3 HYDROXYBENZOATE SALTS OF METANICOTINE COMPOUNDS 审中-公开
标题翻译：金属化合物的羟基苯甲酸盐
公开(公告)号：WO2006053082A3
公开(公告)日：2006-10-19
申请号：PCT/US2005040650
申请日：2005-11-09
申请人： TARGACEPT INC , MUNOZ JULIO A , GENUS JOHN , MOORE JAMES R
发明人： MUNOZ JULIO A , GENUS JOHN , MOORE JAMES R
IPC分类号： C07D213/46 , A61K31/4406
CPC分类号： C07D213/38 , C07D213/65 , C07D213/73 , C07D213/75 , C07D401/12
摘要： Patients susceptible to or suffering from conditions and disorders, such as central nervous system disorders, are treated by administering to a patient in need thereof compositions that are hydroxybenzoate salts of E-metanicotine-type compounds. The formation of hydroxybenzoate salts of the E-metanicotine compounds is also useful in purifying the E-metanicotine compounds, as the hydroxybenzoate salts tend to crystallize out, leaving impurities such as Z-metanicotine compounds, and compounds where the double bond has migrated, in solution. If desired, the hydroxybenzoate salts can be converted to either the free base (the E-metanicotine) or to another pharmaceutically acceptable salt form.
摘要翻译：通过向有需要的患者施用E-间断脒类化合物的羟基苯甲酸盐的组合物来治疗易患或患有病症和障碍的患者，例如中枢神经系统疾病。 E-间烟碱化合物的羟基苯甲酸盐的形成也可用于纯化E-间烟碱化合物，因为羟基苯甲酸盐倾向于结晶出来，留下杂质如Z-间苯ic啶化合物和双键已经迁移的化合物解。如果需要，羟基苯甲酸盐可以转化为游离碱（E-间烟碱）或另一种药学上可接受的盐形式。

5. 发明申请

WO2007134038A3 SALT FORMS OF (2S)-(4E)-N-METHYL-5-[3-(5-ISOPROPOXYPYRIDIN)YL]-4-PENTEN-2-AMINE 审中-公开
标题翻译：（2S） - （4E）-N-甲基-5- [3-（5-异丙氧基吡啶）YL] -4-丁烯-2-胺的盐形式
公开(公告)号：WO2007134038A3
公开(公告)日：2008-03-27
申请号：PCT/US2007068452
申请日：2007-05-08
申请人： ASTRAZENECA AB , TARGACEPT INC , BOHLIN MARTIN HANS , DULL GARY M , ERIKSSON CAROLINE , MILLER CRAIG H , MUNOZ JULIO A , SEBHATU TESFAI
发明人： BOHLIN MARTIN HANS , DULL GARY M , ERIKSSON CAROLINE , MILLER CRAIG H , MUNOZ JULIO A , SEBHATU TESFAI
IPC分类号： C07D213/38
CPC分类号： C07D213/65
摘要： Phosphoric acid, edisylic acid (1,2-ethanedisulfonic acid), citric acid, orotic acid (uracil-6-carboxylic acid), R-mandelic acid, sulfuric acid, 1,5-naphthalenedisulfonic acid, D-aspartic acid, and lysine monohydrochloride salts of (2S)-(4E)-N-methyl-5-[3-(5-isopropoxypyridin)yl]-4-penten-2-amine, and methods for their preparation, pharmaceutical compositions comprising said salts, and use, are disclosed. The salts can be administered to patients susceptible to or suffering from conditions and disorders, such as central nervous system disorders, to treat and/or prevent such disorders.
摘要翻译：磷酸，乙二酸（1,2-乙烷二磺酸），柠檬酸，乳清酸（尿嘧啶-6-羧酸），R-扁桃酸，硫酸，1,5-萘二磺酸，D-天冬氨酸和赖氨酸（2S） - （4E）-N-甲基-5- [3-（5-异丙氧基吡啶）基] -4-戊烯-2-胺的单盐酸盐及其制备方法，包含所述盐的药物组合物和用途，被披露。盐可以施用于易患或患有诸如中枢神经系统障碍的病症和障碍的患者，以治疗和/或预防这些疾病。

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