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123 条记录 (耗时 0.043 秒)

    2,5-diazabicyclo[2.2.1]heptane derivatives
    114.
    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。

    Diazabicyclic biaryl derivatives
    115.
    发明授权
    Diazabicyclic biaryl derivatives 失效
    二氮杂双环联芳基衍生物

    公开(公告)号：US07223753B2

    公开(公告)日：2007-05-29

    申请号：US10703556

    申请日：2003-11-10

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

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

    IPC分类号： A61P25/00 ,  A61K31/551 ,  A61K31/495 ,  C07D471/00 ,  C07D243/00

    CPC分类号： C07D471/08 ,  A61K31/551 ,  C07D487/08

    摘要： This invention relates to novel diazabicyclic biaryl 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联芳基衍生物，其被发现是烟碱乙酰胆碱受体的胆碱能配体和单胺受体和转运蛋白的调节剂。 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
    117.
    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
    118.
    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
    119.
    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.

    Spiro-quinuclidine derivatives, their preparation and use
    120.
    发明授权
    Spiro-quinuclidine derivatives, their preparation and use 失效
    螺 - 奎宁环衍生物，其制备和用途

    公开(公告)号：US06352995B1

    公开(公告)日：2002-03-05

    申请号：US09417889

    申请日：1999-10-14

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

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

    IPC分类号： A61K3144

    CPC分类号： C07D491/20

    摘要： The present invention discloses compounds of formula (I), or a pharmaceutically acceptable salt thereof; wherein n is 1 or 2 or 3, A is —O—, —S—, —CH—, —O—CH2—, or —CH2—O—; B is —O—, —S—, —CH2—, —0—CH2—, or —CH2—O—; and C is N, or —CR1—; D is N, or —CR2—; E is N, or —CR3—; and F is N, or —CR4—; wherein R1, R2, R3 and R4 each independently are 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 for the treatment of disorders or diseases responsive to the activity of nicotinic ACh receptor modulators.

    摘要翻译： 本发明公开了式（I）化合物或其药学上可接受的盐; 其中n为1或2或3，A为-O - ， - S - ， - CH - ， - O-CH 2 - 或-CH 2 -O-; B是-O - ， - S - ， - CH 2 - ， - O-CH 2 - 或-CH 2 -O-; 和C是N或-CR1; D是N或-CR 2 - ; E为N或-CR3-; 而F为N或-CR4-; 其中R1，R2，R3和R4各自独立地选自烷基，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，CF3，OCF3，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于治疗对烟碱ACh受体调节剂的活性有反应的病症或疾病。