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    8-Azabicyclo[3.2.1]oct-2-ene and -octane derivatives technical field
    57.
    发明授权
    8-Azabicyclo[3.2.1]oct-2-ene and -octane derivatives technical field 失效
    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：US07045522B2

    公开(公告)日：2006-05-16

    申请号：US10726680

    申请日：2003-12-04

    申请人： Dan Peters ,  Gunnar M. Olsen ,  Simon Feldbaek Nielsen ,  Elsebet Ostergaard Nielsen

    发明人： Dan Peters ,  Gunnar M. Olsen ,  Simon Feldbaek Nielsen ,  Elsebet Ostergaard Nielsen

    IPC分类号： A61K31/46 ,  A61K31/4709 ,  C07D451/02

    CPC分类号： A61K31/46 ,  C07D451/02

    摘要： The present invention relates to novel 8-azabicyclo[3.2.1]oct-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。

    9-azobicyclo[3.3.1] non-2-ene derivatives as cholinergic ligands at nicotinic ACH receptors
    60.
    发明授权
    9-azobicyclo[3.3.1] non-2-ene derivatives as cholinergic ligands at nicotinic ACH receptors 失效
    9-偶氮双环[3.3.1]壬-2-烯衍生物作为烟碱型ACH受体上的胆碱能配体

    公开(公告)号：US06392045B1

    公开(公告)日：2002-05-21

    申请号：US09450635

    申请日：1999-11-29

    申请人： Dan Peters ,  Gunnar M. Olsen ,  Simon Feldbaek Nielsen ,  Elsebet Ostergaard Nielsen

    发明人： Dan Peters ,  Gunnar M. Olsen ,  Simon Feldbaek Nielsen ,  Elsebet Ostergaard Nielsen

    IPC分类号： C07D40304

    CPC分类号： C07D451/14

    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; 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-membered heteroaryl 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.

    摘要翻译： 本发明公开了式（1）的化合物，其任何对映体或其任何混合物或其药学上可接受的盐，其中----是单键或双键; R是氢，烷基，烯基，炔基，环烷基，环烷基烷基，芳基或芳烷基; 并且R 1是（a），其中R 2是氢，烷基，烯基，炔基，环烷基，环烷基烷基，氨基; 可以被选自烷基，环烷基，环烷基烷基烯基，炔基，烷氧基，环烷氧基，硫代烷氧基，硫代环烷氧基，亚甲二氧基，芳氧基，卤素，CF 3，OCF 3，CN，氨基，氨基酰基等的取代基取代一次或多次的芳基， 硝基，芳基和单环5至6元杂芳基; 可以被选自烷基，环烷基，环烷基烷基烯基，炔基，烷氧基，环烷氧基，硫代烷氧基，硫代环烷氧基，亚甲二氧基，芳氧基，卤素，CF 3， OCF 3，CN，氨基，硝基，芳基和单环5至6元杂芳基; 或由与苯环稠合或与另一个单环5至6元杂芳基稠合的单环5至6元杂芳基组成的双环杂芳基，所有这些可以与选自以下的取代基取代一次或多次：烷基 烷氧基，环烷氧基，硫代烷氧基，硫代环烷氧基，亚甲二氧基，芳氧基，卤素，CF 3，OCF 3，CN，氨基，硝基，芳基和单环5至6元杂芳基。 本发明的化合物可用作烟碱ACh受体配体。