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1. 发明申请

US20070259884A1 4,5-Dihydro-1H-pyrazole derivatives having potent CB1-antagonistic activity 失效
标题翻译：具有强的CB1拮抗活性的4,5-二氢-1H-吡唑衍生物
公开(公告)号：US20070259884A1
公开(公告)日：2007-11-08
申请号：US11265090
申请日：2005-11-03
申请人： Josephus Lange , Cornelis Kruse , Jacobus Tipker , Herman van Stuivenberg , Arnoldus Herremans
发明人： Josephus Lange , Cornelis Kruse , Jacobus Tipker , Herman van Stuivenberg , Arnoldus Herremans
IPC分类号： A61K31/415 , A61K31/454 , A61K31/497 , A61P25/00 , C07D231/06 , C07D401/12 , C07D403/12
CPC分类号： C07D231/06 , C07D401/04 , C07D401/12 , C07D409/04
摘要： The present invention relates to a group of novel 4,5-dihydro-1H-pyrazole derivatives which are potent cannabinoid (CB1) receptor antagonists with utility for the treatment of diseases connected with disorders of the cannabinoid system. The compounds have the general formula (Ia) or (Ib) wherein the symbols have the meanings given in the specification. The invention also relates to methods for the preparation of these compounds, and to pharmaceutical compositions containing one or more of these compounds as an active component.
摘要翻译：本发明涉及一组新的4,5-二氢-1H-吡唑衍生物，它们是用于治疗与大麻素系统紊乱相关的疾病的有效大麻素（CB 1）受体拮抗剂。化合物具有通式（Ia）或（Ib），其中符号具有说明书中给出的含义。本发明还涉及制备这些化合物的方法，以及含有一种或多种这些化合物作为活性组分的药物组合物。

2. 发明申请

US20070275977A1 N-OXIDES OF PYRIDYLMETHYL -PIPERAZINE AND -PIPERIDINE DERIVATIVES 审中-公开
标题翻译：吡咯并吡啶和哌啶衍生物的N-氧化物
公开(公告)号：US20070275977A1
公开(公告)日：2007-11-29
申请号：US11743049
申请日：2007-05-01
申请人： Marcel Van Aar , Peter Van Amsterdam , Gerrit Barf , Johan Bakker , Cathaline Den Besten , Arnoldus Herremans , Jan Zorgdrager
发明人： Marcel Van Aar , Peter Van Amsterdam , Gerrit Barf , Johan Bakker , Cathaline Den Besten , Arnoldus Herremans , Jan Zorgdrager
IPC分类号： A61K31/496 , C07D405/14
CPC分类号： C07D405/12
摘要： N-oxides of certain pyridylmethylpiperazine and -piperidine derivatives are provided as alternatives to or as “prodrugs” of their respective parent compounds, as well as pharmaceutical compositions containing these N-oxides, methods for preparing them, and compositions comprising them. The N-oxides have the formula (a) wherein the substituents have the meanings given in the description, and wherein the oxidized nitrogen atom can be the nitrogen atom in the pyridyl ring of R5, or the nitrogen atom in the piperidine ring (when Z is carbon) or either one of the nitrogen atoms in the piperazine ring (when Z is nitrogen), or both the nitrogen atom connected to R5 via a methylene group, and the nitrogen atom in the pyridyl ring of R5, and tautomers, stereoisomers, pharmacologically acceptable salts, hydrates, and solvates thereof. In addition, the N-oxides and compositions can be used as medicaments useful in the treatment of affections or diseases of the central nervous system caused by disturbances in either the dopaminergic or serotinergic systems.
摘要翻译：提供某些吡啶基甲基哌嗪和哌啶衍生物的N-氧化物作为其各自母体化合物的“前体药物”的替代物或含有这些N-氧化物的药物组合物，其制备方法和包含它们的组合物。 N-氧化物具有式（a），其中取代基具有本说明书中给出的含义，其中氧化的氮原子可以是R 5的吡啶环中的氮原子，或氮哌啶环中的一个原子（当Z为碳时）或哌嗪环中的氮原子之一（当Z为氮时），或通过亚甲基与R 5连接的氮原子，和R 5的吡啶环中的氮原子，以及互变异构体，立体异构体，药理学上可接受的盐，水合物和溶剂化物。此外，N-氧化物和组合物可以用作治疗由多巴胺能或血清素能系统中的紊乱引起的中枢神经系统的情感或疾病的药物。

3. 发明申请

US20050054679A1 1 H-imidazole derivatives having CB1 agonistic, CB1 partial agonistic or CB1-antagonistic activity 有权
标题翻译：具有CB1激动性，CB1部分激动性或CB1拮抗活性的1 H-咪唑衍生物
公开(公告)号：US20050054679A1
公开(公告)日：2005-03-10
申请号：US10912171
申请日：2004-08-06
申请人： Cornelis Kruse , Josephus Lange , Arnoldus Herremans , Herman Van Stuivenberg
发明人： Cornelis Kruse , Josephus Lange , Arnoldus Herremans , Herman Van Stuivenberg
IPC分类号： C07C257/18 , C07D233/90 , C07D295/30 , C07D401/04 , C07D403/04 , C07D405/04 , A61K31/454 , C07D43/02
CPC分类号： C07D295/30 , C07C257/18 , C07D233/90 , C07D401/04 , C07D403/04 , C07D405/04
摘要： The present invention relates to a group of novel 1H-imidazole derivatives, to methods for the preparation of these compounds, and to pharmaceutical compositions containing one or more of these compounds as an active component. These 1H-imidazole derivatives are potent cannabinoid-CB1 receptor agonists, partial agonists or antagonists, useful for the treatment of psychiatric and neurological disorders, as well as and other diseases involving cannabinoid neurotransmission. The compounds have the general formula (I) wherein R and R1-R4 have the meanings given in the specification.
摘要翻译：本发明涉及一组新的1H-咪唑衍生物，制备这些化合物的方法，以及含有一种或多种这些化合物作为活性组分的药物组合物。这些1H-咪唑衍生物是有效的大麻素-CB1受体激动剂，部分激动剂或拮抗剂，可用于治疗精神病和神经障碍，以及涉及大麻素神经传递的其它疾病。这些化合物具有通式（I），其中R和R 1 -R 4具有说明书中给出的含义。

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