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1.发明申请Azabicyclic, azatricyclic and azaspirocyclic derivatives of aminocyclohexane NMDA, 5HT3 and neuronal nicotinic receptor antagonists 审中-公开氨基环己烷NMDA，5HT3和神经元烟碱受体拮抗剂的Azabicyclic，azatricyclic和azaspirocyclic衍生物公开(公告)号：US20070185151A1
公开(公告)日：2007-08-09
申请号：US11732764
申请日：2007-04-04
申请人： Christopher Parsons , Markus Henrich , Wojciech Danysz , Ivars Kalvinsh , Valerjans Kauss , Aigars Jirgensons , Markus Gold , Maksims Vanejevs
发明人： Christopher Parsons , Markus Henrich , Wojciech Danysz , Ivars Kalvinsh , Valerjans Kauss , Aigars Jirgensons , Markus Gold , Maksims Vanejevs
IPC分类号： A61K31/44
CPC分类号： C07D221/20 , A61K31/44 , C07D209/54 , C07D221/22 , C07D471/08 , C07D487/08 , Y02A50/411
摘要： Azabicyclic, azatricyclic and azaspirocyclic derivatives of aminocyclohexanes which are systemically-active as NMDA, 5HT3, and nicotinic receptor antagonists, pharmaceutical compostions comprising the same, method of preparation thereof, and method of treating CNS disorders which involve disturbances of glutamatergic, serotoninergic, and nicotinic transmission, treating immunomodulatory disorders, and antimalaria, antitrypanosomal, anti-Borna virus, anti-HSV and anti-Hepatitis C virus activity.
摘要翻译： 作为NMDA，5HT 3和烟碱型受体拮抗剂具有全身活性的氨基环己烷的氮杂双环，氮杂环和azaspirocyclic衍生物，包含其的药物组合物，其制备方法和治疗CNS病症的方法，涉及 治疗谷氨酸能，血清素能和烟碱传播的紊乱，治疗免疫调节障碍和抗疟疾，抗睾丸激素，抗牛痘病毒，抗HSV和抗丙型肝炎病毒活性。
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2.发明授权Azabicyclic, azatricyclic and azaspirocyclic derivatives of aminocyclohexane NMDA, 5HT3, and neuronal nicotinic receptor antagonists 失效氨基环己烷NMDA，5HT3和神经元烟碱受体拮抗剂的Azabicyclic，azatricyclic和azaspirocyclic衍生物公开(公告)号：US07022729B2
公开(公告)日：2006-04-04
申请号：US10394670
申请日：2003-03-21
申请人： Christopher Graham Raphael Parsons , Markus Henrich , Wojciech Danysz , Ivars Kalvinsh , Valerjans Kauss , Aigars Jirgensons , Markus Gold , Maksims Vanejevs
发明人： Christopher Graham Raphael Parsons , Markus Henrich , Wojciech Danysz , Ivars Kalvinsh , Valerjans Kauss , Aigars Jirgensons , Markus Gold , Maksims Vanejevs
IPC分类号： A61K31/40 , C07D209/02
CPC分类号： C07D221/20 , A61K31/44 , C07D209/54 , C07D221/22 , C07D471/08 , C07D487/08 , Y02A50/411
摘要： Azabicyclic, azatricyclic and azaspirocyclic derivatives of aminocyclohexanes which are systemically-active as NMDA, 5HT3, and nicotinic receptor antagonists, pharmaceutical compositions comprising the same, method of preparation thereof, and method of treating CNS disorders which involve disturbances of glutamatergic, serotoninergic, and nicotinic transmission, treating immunomodulatory disorders, and antimalaria, antitrypanosomal, anti-Borna virus, anti-HSV and anti-Hepatitis C virus activity.
摘要翻译： 作为NMDA，5HT 3和烟碱型受体拮抗剂具有全身活性的氨基环己烷的氮杂环，氮杂环和azaspirocyclic衍生物，包含它们的药物组合物，其制备方法和治疗CNS疾病的方法，涉及 治疗谷氨酸能，血清素能和烟碱传播的紊乱，治疗免疫调节障碍和抗疟疾，抗睾丸激素，抗牛痘病毒，抗HSV和抗丙型肝炎病毒活性。
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公开(公告)号：US06602862B1
公开(公告)日：2003-08-05
申请号：US09664629
申请日：2000-09-19
IPC分类号： A61K3133
CPC分类号： A61K31/13
摘要： Certain 1-aminoalkylcyclohexanes are anti-trypanosomiasis agents and trypanocides. Pharmaceutical compositions thereof for such purpose and method of making same, as well as a method-of-treating trypanosomiasis therewith.
摘要翻译： 某些1-氨基烷基环己烷是抗锥虫病和锥虫病。 用于此目的的药物组合物及其制备方法，以及与其进行的锥虫病治疗方法。
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4.发明授权Pyrido-phtalazin diones and their use against neurological disorders associated with excitotoxicity and malfunctioning of glutamatergic neurotransmission 失效吡哆醛 - 酞霉素及其用于与神经功能障碍相关的神经功能障碍，其与兴奋性毒性和谷氨酸能神经传递功能异常有关
公开(公告)号：US5776935A
公开(公告)日：1998-07-07
申请号：US686346
申请日：1996-07-25
申请人： Wojciech Danysz , Markus Gold , Ivars Kalvinsh , Christopher Graham Raphael Parsons , Irene Piskunova , Eugene Rozhkov
发明人： Wojciech Danysz , Markus Gold , Ivars Kalvinsh , Christopher Graham Raphael Parsons , Irene Piskunova , Eugene Rozhkov
IPC分类号： C07D491/147 , A61K31/5025 , A61P25/08 , A61P43/00 , C07D237/26 , C07D471/04 , A61K31/50
CPC分类号： C07D471/04
摘要： Pyridyl-phtalazin diones having the following formula: ##STR1## wherein R1 and R2 are selected from the group consisting of hydrogen, halogen, and methoxy or wherein R1 and R2 together form methylenedioxy, and pharmaceutically-acceptable salts thereof, and pharmaceutical compositions containing an effective glycine.sub.B antagonistic amount thereof, are useful in combatting neurological disorders associated with excitotoxicity and malfunctioning of glutamatergic neurotransmission in a living animal, including a human, in need thereof.
摘要翻译： 具有下式的吡啶基 - 苯达嗪二酮：其中R 1和R 2选自氢，卤素和甲氧基，或其中R 1和R 2一起形成亚甲二氧基及其药学上可接受的盐，以及含有 有效的甘氨酸B拮抗量可用于与有需要的活体动物（包括人）的兴奋性毒性和谷氨酸能神经传递功能异常相关的神经障碍。
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5.发明申请1-Amino-alkyl-cyclohexanes as 5-HT3 and neuronal nicotinic receptor antagonists 审中-公开1-氨基 - 烷基 - 环己烷作为5-HT3和神经元烟碱受体拮抗剂公开(公告)号：US20100298442A1
公开(公告)日：2010-11-25
申请号：US12804610
申请日：2010-07-26
申请人： Christopher Graham Raphael Parsons , Wojciech Danysz , Markus Gold , Ivars Kalvinsh , Valerjans Kauss , Aigars Jirgensons
发明人： Christopher Graham Raphael Parsons , Wojciech Danysz , Markus Gold , Ivars Kalvinsh , Valerjans Kauss , Aigars Jirgensons
CPC分类号： A61K31/13 , A61K31/40 , C07B2200/07 , C07C211/35 , C07C2601/14
摘要： Certain 1-aminoalkylcyclohexanes are systematically-active 5HT3 and nicotinic receptor antagonists and are useful in the inhibition of progression of or alleviation of conditions resulting from disturbances of serotoninergic or nicotinergic transmission giving them a wide range of utility in the treatment of CNS-disorders. Pharmaceutical compositions thereof for such purpose and method of making same, as well as a method-of-treating conditions which are alleviated by the employment of a 5HT3 or neuronal nicotinic receptor antagonist.
摘要翻译： 某些1-氨基烷基环己烷是系统活性的5HT3和烟碱受体拮抗剂，可用于抑制由5-羟色胺能或烟碱能传递紊乱引起的病症的进展或缓解，从而在治疗CNS障碍方面具有广泛的应用。 用于其目的的药物组合物及其制备方法，以及通过使用5HT3或神经元烟碱受体拮抗剂缓解的治疗方法。
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6.发明授权Azabicyclic, azatricyclic and azaspirocyclic derivatives of aminocyclohexane NMDA, 5HT3, and neuronal nicotinic receptor antagonists 失效氨基环己烷NMDA，5HT3和神经元烟碱受体拮抗剂的Azabicyclic，azatricyclic和azaspirocyclic衍生物公开(公告)号：US07238703B2
公开(公告)日：2007-07-03
申请号：US11202012
申请日：2005-08-11
申请人： Christopher G. R. Parsons , Markus Henrich , Wojciech Danysz , Ivars Kalvinsh , Valerjans Kauss , Aigars Jirgensons , Markus Gold , Maksims Vanejevs
发明人： Christopher G. R. Parsons , Markus Henrich , Wojciech Danysz , Ivars Kalvinsh , Valerjans Kauss , Aigars Jirgensons , Markus Gold , Maksims Vanejevs
IPC分类号： A61K31/438 , C07D221/20
CPC分类号： C07D221/20 , A61K31/44 , C07D209/54 , C07D221/22 , C07D471/08 , C07D487/08 , Y02A50/411
摘要： Azabicyclic, azatricyclic and azaspirocyclic derivatives of aminocyclohexanes which are systemically-active as NMDA, 5HT3, and nicotinic receptor antagonists, pharmaceutical compositions comprising the same, method of preparation thereof, and method of treating CNS disorders which involve disturbances of glutamatergic, serotoninergic, and nicotinic transmission, treating immunomodulatory disorders, and antimalaria, antitrypanosomal, anti-Borne virus, anti-HSV and anti-Hepatitis C virus activity.
摘要翻译： 作为NMDA，5HT 3和烟碱型受体拮抗剂具有全身活性的氨基环己烷的氮杂环，氮杂环和azaspirocyclic衍生物，包含它们的药物组合物，其制备方法和治疗CNS疾病的方法，涉及 治疗谷氨酸能，血清素能和烟碱传播的紊乱，治疗免疫调节障碍和抗疟疾，抗睾丸激素，抗血清病毒，抗HSV和抗丙型肝炎病毒活性。
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7.发明授权Unsaturated 1-amino-alkylcyclohexane NMDA, 5HT3, and neuronal nicotinic receptor antagonists 失效不饱和的1-氨基 - 烷基环己烷NMDA，5HT3和神经元烟碱受体拮抗剂公开(公告)号：US06828462B2
公开(公告)日：2004-12-07
申请号：US10288819
申请日：2002-11-06
申请人： Markus Henrich , Wojciech Danysz , Christopher Graham Raphael Parsons , Ivars Kalvinsh , Valerjans Kauss , Aigars Jirgensons , Markus Gold
发明人： Markus Henrich , Wojciech Danysz , Christopher Graham Raphael Parsons , Ivars Kalvinsh , Valerjans Kauss , Aigars Jirgensons , Markus Gold
IPC分类号： A61K3133
CPC分类号： C07D295/033 , C07C211/25 , C07C211/40 , C07C2601/14 , C07C2601/16
摘要： Unsaturated 1-Amino-alkylcyclohexane compounds which are systemically-active as NMDA, 5HT3, and nicotinic receptor antagonists, pharmaceutical compositions comprising the same, method of preparation thereof, and method of treating CNS disorders which involve disturbances of glutamatergic, serotoninergic, and nicotinic transmission, treating immunomodulatory disorders, and antimalaria, antitrypanosomal, anti-Borna virus, anti-HSV and anti-Hepatitis C virus activity.
摘要翻译： 作为NMDA，5HT3和烟碱受体拮抗剂具有系统活性的不饱和1-氨基 - 烷基环己烷化合物，包含其的药物组合物，其制备方法和治疗涉及谷氨酸能，血清素能和烟碱传播紊乱的CNS疾病的方法 治疗免疫调节障碍，抗疟疾，抗睾丸激素，抗 - 博尔纳病毒，抗HSV和抗丙型肝炎病毒活性。
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公开(公告)号：US6034134A
公开(公告)日：2000-03-07
申请号：US141381
申请日：1998-08-27
申请人： Markus Gold , Wojciech Danysz , Christopher Graham Raphael Parsons , Ivars Kalvinsh , Valerjans Kauss , Aigars Jirgensons
发明人： Markus Gold , Wojciech Danysz , Christopher Graham Raphael Parsons , Ivars Kalvinsh , Valerjans Kauss , Aigars Jirgensons
IPC分类号： A61P1/16 , A61K31/13 , A61K31/40 , A61P31/12 , A61P33/06 , A61P37/02 , A61P43/00 , C07C211/17 , C07C211/35 , C07D295/135 , A61K33/00
CPC分类号： C07D295/135 , A61K31/40 , C07C211/17 , C07C211/35 , C07C2101/14
摘要： Certain 1-aminoalkylcyclohexanes are systemically-active uncompetitive NMDA receptor antagonists having rapid blocking/unblocking kinetics and strong voltage-dependency and are therefore useful in the alleviation of conditions resulting from disturbances of glutamatergic transmission giving them a wide range of utility in the treatment of CNS disorders involving the same, as well as in non-NMDA indications, due to their immunomodulatory, antimalarial, anti-Borna virus, and anti-Hepatitis C activities and utilities. Pharmaceutical compositions thereof and a method-of-treating conditions which are alleviated by the employment of an NMDA receptor antagonist, as well as the aforementioned non-NMDA indications, and a method for the preparation of the active 1-aminoalkylcyclohexane compounds involved.
摘要翻译： 某些1-氨基烷基环己烷是具有快速阻断/阻断动力学和强电压依赖性的全身活性的非竞争性NMDA受体拮抗剂，因此可用于缓解由谷氨酸能传递紊乱引起的病症，使其在治疗CNS方面具有广泛的用途 由于其免疫调节，抗疟疾，抗 - 博尔纳病毒和抗丙型肝炎活动和功效，涉及相同的疾病以及非NMDA适应症的疾病。 通过使用NMDA受体拮抗剂减轻其药物组合物和治疗方法，以及上述非NMDA适应症，以及涉及制备活性1-氨基烷基环己烷化合物的方法。
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9.发明申请Azabicyclic, azatricyclic and azaspirocyclic derivatives of aminocyclohexane NMDA, 5HT3 and neuronal nicotinic receptor antagonists 失效氨基环己烷NMDA，5HT3和神经元烟碱受体拮抗剂的Azabicyclic，azatricyclic和azaspirocyclic衍生物公开(公告)号：US20060019982A1
公开(公告)日：2006-01-26
申请号：US11202012
申请日：2005-08-11
申请人： Christopher Parsons , Markus Henrich , Wojciech Danysz , Ivars Kalvinsh , Valerjans Kauss , Aigars Jirgensons , Markus Gold , Maksims Vanejevs
发明人： Christopher Parsons , Markus Henrich , Wojciech Danysz , Ivars Kalvinsh , Valerjans Kauss , Aigars Jirgensons , Markus Gold , Maksims Vanejevs
IPC分类号： A61K31/46 , A61K31/407
CPC分类号： C07D221/20 , A61K31/44 , C07D209/54 , C07D221/22 , C07D471/08 , C07D487/08 , Y02A50/411
摘要： Azabicyclic, azatricyclic and azaspirocyclic derivatives of aminocyclohexanes which are systemically-active as NMDA, 5HT3, and nicotinic receptor antagonists, pharmaceutical compositions comprising the same, method of preparation thereof, and method of treating CNS disorders which involve disturbances of glutamatergic, serotoninergic, and nicotinic transmission, treating immunomodulatory disorders, and antimalaria, antitrypanosomal, anti-Borna virus, anti-HSV and anti-Hepatitis C virus activity.
摘要翻译： 作为NMDA，5HT 3和烟碱型受体拮抗剂具有全身活性的氨基环己烷的氮杂环，氮杂环和azaspirocyclic衍生物，包含它们的药物组合物，其制备方法和治疗CNS疾病的方法，涉及 治疗谷氨酸能，血清素能和烟碱传播的紊乱，治疗免疫调节障碍和抗疟疾，抗睾丸激素，抗牛痘病毒，抗HSV和抗丙型肝炎病毒活性。
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10.发明申请1-Amino-alkylcyclohexanes as 5-HT3 and neuronal nicotinic receptor antagonists 审中-公开1-氨基 - 烷基环己烷作为5-HT 3和神经元烟碱受体拮抗剂公开(公告)号：US20070105961A1
公开(公告)日：2007-05-10
申请号：US11643129
申请日：2006-12-21
申请人： Christopher Parsons , Wojciech Danysz , Markus Gold , Ivars Kalvinsh , Valerjans Kauss , Aigars Jirgensons
发明人： Christopher Parsons , Wojciech Danysz , Markus Gold , Ivars Kalvinsh , Valerjans Kauss , Aigars Jirgensons
IPC分类号： A61K31/13
CPC分类号： A61K31/13 , A61K31/40 , C07B2200/07 , C07C211/35 , C07C2601/14
摘要： Certain 1-aminoalkylcyclohexanes are systematically-active 5HT3 and nicotinic receptor antagonists and are useful in the inhibition of progression of or alleviation of conditions resulting from disturbances of serotoninergic or nicotinergic transmission giving them a wide range of utility in the treatment of CNS-disorders. Pharmaceutical compositions thereof for such purpose and method of making same, as a method-of-treating conditions which are alleviated by the employment of a 5HT3 or neuronal nicotinic receptor antagonist.
摘要翻译： 某些1-氨基烷基环己烷是系统活性的5HT3和烟碱受体拮抗剂，可用于抑制由5-羟色胺能或烟碱能传递紊乱引起的病症的进展或缓解，从而在治疗CNS障碍方面具有广泛的应用。 作为其目的的药物组合物及其制备方法，作为通过使用5HT3或神经元烟碱受体拮抗剂缓解的治疗方法。
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