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294 条记录 (耗时 0.05 秒)

    Heteroaryl diazacycloalkanes, their preparation and use
    61.
    发明授权
    Heteroaryl diazacycloalkanes, their preparation and use 失效
    杂芳基二氮杂环烷烃，其制备和用途

    公开(公告)号：US07282494B2

    公开(公告)日：2007-10-16

    申请号：US11312574

    申请日：2005-12-21

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

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

    IPC分类号： A61P25/00 ,  A61K31/55 ,  C07D243/08

    CPC分类号： C07D401/14 ,  C07D401/04 ,  C07D403/04 ,  C07D405/14 ,  C07D417/04

    摘要： The present invention relates to novel heteroaryl diazacycloalkane 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： 本发明涉及新颖的杂芳基二氮杂环烷烃衍生物，其在烟碱乙酰胆碱受体中被发现是胆碱能配体。 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。

    8-azabicyclo[3.2.1]oct-2-ene and -octane derivatives
    62.
    发明授权
    8-azabicyclo[3.2.1]oct-2-ene and -octane derivatives 失效
    8-氮杂双环[3.2.1]辛-2-烯和 - 辛烷衍生物

    公开(公告)号：US06680328B2

    公开(公告)日：2004-01-20

    申请号：US09864367

    申请日：2001-05-25

    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： A61K3146

    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 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，与化学物质终止引起的炎症，疼痛和戒断症状有关的疾病或病症。

    2,5-diazabicyclo[2.2.1]heptane derivatives
    65.
    发明授权
    2,5-diazabicyclo[2.2.1]heptane derivatives 失效
    2,5-二氮杂双环[2.2.1]庚烷衍生物

    公开(公告)号：US07329754B2

    公开(公告)日：2008-02-12

    申请号：US10250765

    申请日：2002-02-28

    申请人： Dan Peters ,  Gunnar M. Olsen ,  Elsebet Ostergaard Nielsen ,  Philip K. Ahring ,  Tino Dyhring Jorgensen

    发明人： Dan Peters ,  Gunnar M. Olsen ,  Elsebet Ostergaard Nielsen ,  Philip K. Ahring ,  Tino Dyhring Jorgensen

    IPC分类号： C07D215/38 ,  C07D265/30

    CPC分类号： C07D487/08 ,  A61K31/4995

    摘要： The present invention relates to novel 2,5-diazabicyclo[2.2.1]heptane derivatives, which are found to be potent modulators of the monoamine receptors and transporters.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), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.

    摘要翻译： 本发明涉及新的2,5-二氮杂双环[2.2.1]庚烷衍生物，其被发现是单胺受体和转运蛋白的有效调节剂。 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），周围神经系统（PNS），疾病或病症相关的胆碱能系统相关的疾病或障碍 平滑肌肉收缩，内分泌疾病或病症，与神经变性相关的疾病或病症，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。

    Heteroaryl-diazabicycloalkanes
    67.
    发明授权
    Heteroaryl-diazabicycloalkanes 失效
    杂芳基 - 二氮杂双环烷烃

    公开(公告)号：US06815438B2

    公开(公告)日：2004-11-09

    申请号：US10130099

    申请日：2002-05-14

    申请人： Dan Peters ,  Gunnar M. Olsen ,  Elsebet Ostergaard Nielsen ,  Philip K. Ahring ,  Simon Feldbaek Nielsen ,  Tino Dyhring Jorgensen

    发明人： Dan Peters ,  Gunnar M. Olsen ,  Elsebet Ostergaard Nielsen ,  Philip K. Ahring ,  Simon Feldbaek Nielsen ,  Tino Dyhring Jorgensen

    IPC分类号： A61K3133

    CPC分类号： C07D471/08 ,  C07D487/04 ,  C07D487/08

    摘要： The present invention relates to novel heteroaryl-diazabicycloalkanes 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型杂芳基 - 二氮杂双环烷烃。 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。

    8-azabicyclo(3,2,1)oct-2-ene and octane derivatives as cholinergic ligands at nicotinic ACh receptors
    68.
    发明授权
    8-azabicyclo(3,2,1)oct-2-ene and octane derivatives as cholinergic ligands at nicotinic ACh receptors 失效
    8-氮杂双环（3,2,1）辛-2-烯和辛烷衍生物作为胆碱能配体在烟碱性ACh受体

    公开(公告)号：US06645977B1

    公开(公告)日：2003-11-11

    申请号：US09450637

    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： A61K3146

    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, cycloalklyl, 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）的任何对映体或其任何混合物或其药学上可接受的盐的化合物; 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; 和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; 或可以被选自烷基，环烯基，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，氨基酰基的氨基酰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; 或由与苯环稠合或稠合至其它单环5至6元杂芳基的单环5至6元杂芳基组成的双环杂芳基，所有这些可以被选自以下的取代基取代一次或多次： 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。 本发明的化合物可用作烟碱ACh受体配体。

    Heteroaryl diazabicycloalkanes, their preparation and use
    69.
    发明授权
    Heteroaryl diazabicycloalkanes, their preparation and use 失效

    公开(公告)号：US06552012B2

    公开(公告)日：2003-04-22

    申请号：US09933944

    申请日：2001-08-22

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

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

    IPC分类号： C07D48708

    CPC分类号： C07D471/08 ,  C07D487/08

    摘要： The present invention relates to novel heteroaryl diazabicycloalkane derivatives represented by general formula (I), any of its enantiomers or any mixture thereof, an N oxide thereof, a pharmaceutically acceptable salt thereof, in a labelled or un-labelled form, 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.

    Diazabicyclic aryl derivatives as cholinergic receptor modulators
    70.
    发明授权
    Diazabicyclic aryl derivatives as cholinergic receptor modulators 失效
    二氮杂双环芳基衍生物作为胆碱能受体调节剂

    公开(公告)号：US08236793B2

    公开(公告)日：2012-08-07

    申请号：US12633505

    申请日：2009-12-08

    申请人： Dan Peters ,  Gunnar M. Olsen ,  Elsebet Østergaard Nielsen ,  Tino Dyhring Jørgensen ,  Daniel B Timmermann

    发明人： Dan Peters ,  Gunnar M. Olsen ,  Elsebet Østergaard Nielsen ,  Tino Dyhring Jørgensen ,  Daniel B Timmermann

    IPC分类号： A61K31/55 ,  C07D243/10

    CPC分类号： C07D471/08

    摘要： This invention relates to novel diazabicyclic aryl derivatives which are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. 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), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.

    摘要翻译： 本发明涉及新的二氮杂双环芳基衍生物，其在烟碱乙酰胆碱受体和单胺受体和转运蛋白的调节剂中被发现是胆碱能配体。 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），周围神经系统（PNS），疾病或病症相关的胆碱能系统相关的疾病或障碍 平滑肌肉收缩，内分泌疾病或病症，与神经变性相关的疾病或病症，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。