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1. 发明申请

US20040116703A1 8-Azabicyclo[3.2.1]oct-2-ene and -octane derivatives technical field 失效
标题翻译： 8-氮杂双环[3.2.1]辛-2-烯和 - 辛烷衍生物技术领域
公开(公告)号：US20040116703A1
公开(公告)日：2004-06-17
申请号：US10726680
申请日：2003-12-04
申请人： NEUROSEARCH A/S
发明人： Dan Peters , Gunnar M. Olsen , Simon Feldbaek Nielsen , Elsebet Ostergaard Nielsen
IPC分类号： C07D451/02
CPC分类号： A61K31/46 , C07D451/02
摘要： The present invention relates to novel 8-azabicyclonull3.2.1nulloct-2-ene and -octane derivatives which are found to be cholinergic ligands at the nicotinic Acetyl Choline Receptors. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neurodegeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.
摘要翻译：本发明涉及在烟碱乙酰胆碱受体中被发现是胆碱能配体的新的8-氮杂双环[3.2.1]辛-2-烯和 - 辛烷衍生物。由于其药理学特征，本发明的化合物可用于治疗与中枢神经系统（CNS）的胆碱能系统有关的疾病或病症，与平滑肌收缩相关的疾病或病症，内分泌疾病或与神经变性相关的疾病，疾病或病症，与由化学物质的滥用终止引起的炎症，疼痛和戒断症状相关的疾病或病症。

2. 发明申请

US20040019207A1 8-Azabicyclo(3,2,1)oct-2 ene and octane derivatives as cholinergic ligands at nicotinic ACh receptors 失效
公开(公告)号：US20040019207A1
公开(公告)日：2004-01-29
申请号：US10620559
申请日：2003-07-17
申请人： NeuroSearch A/S
发明人： Dan Peters , Gunnar M. Olsen , Simon Feldback Nielsen , Elsebet Ostergaard Nielsen
IPC分类号： C07D417/02 , C07D413/02 , C07D43/02
CPC分类号： C07D451/02
摘要： The present invention discloses compounds of formula (1) any of its enantiomers or any mixture thereof, or a pharmaceutically acceptable salt thereof; wherein is a single or a double bond; R is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, aryl or aralkyl; and R1 is (a), wherein R2 is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, amino; or aryl which may be substituted one or more times with substituents selected from the group consisting of alkyl, cycloalkyl, cycloalkylalkyl alkenyl, alkynyl, alkoxy, cycloalkoxy, thioalkoxy, thiocycloalkoxy, methylenedioxy, aryloxy, halogen, CF3, OCF3, CN, amino, aminoacyl, nitro, aryl and a monocyclic 5 to 6-membered heteroaryl group; a monocyclic 5 to 6-membered heteroaryl group which may be substituted one or more times with substituents selected from the group consisting of alkyl, cycloalkyl, cycloalkylalkyl alkenyl, alkynyl, alkoxy, cycloalkoxy, thioalkoxy, thiocycloalkoxy, methylenedioxy, aryloxy, halogen, CF3, OCF3, CN, amino, nitro, aryl and a monocyclic 5 to 6-membred lieteroaryl group; or a bicyclic heteroaryl group composed of a monocyclic 5 to 6 membered heteroaryl group fused to a benzene ring or fused to another monocyclic 5 to 6-membered heteroaryl, all of which may be substituted one or more times with substituents selected from the group consisting of alkyl, cycloalkyl cycloalkylalkyl alkenyl, alkynyl, alkoxy, cycloalkoxy, thioalkoxy, thiocycloalkoxy methylenedioxy, aryloxy, halogen, CF3, OCF3, CN, amino, nitro, aryl and a monocyclic 5 to 6-membered heteroaryl group. The compounds of the invention are useful as nicotinic ACh receptor ligands. 1

3. 发明申请

US20040242558A1 Pyridylether derivatives, their preparation and use 失效
标题翻译：吡啶醚衍生物，其制备和用途
公开(公告)号：US20040242558A1
公开(公告)日：2004-12-02
申请号：US10848132
申请日：2004-05-19
申请人： NeuroSearch A/S
发明人： Dan Peters , Gunnar M. Olsen , Simon F. Nielsen , Elsebet Ostergaard Nielsen
IPC分类号： A61K031/397 , C07D211/40 , A61K031/445 , A61K031/4015
CPC分类号： C07D401/02 , C07D401/12 , C07D403/12
摘要： The present invention relates to novel pyridylether derivatives which are cholinergic ligands at nicotinic Ach receptors. The compounds of the invention are useful for the treatment of conditions, disorders, or diseases involving the cholinergic system of the central nervous system, pain, inflammatory diseases, diseases caused by smooth muscle contractions and as assistance in the cessation of chemical substance abuse.
摘要翻译：本发明涉及新颖的吡啶基醚衍生物，它们是烟碱型Ach受体的胆碱能配体。本发明的化合物可用于治疗涉及中枢神经系统的胆碱能系统，疼痛，炎性疾病，由平滑肌收缩引起的疾病以及停止化学物质滥用的协助的疾病，病症或疾病。

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