公开(公告)号：US20100216780A1

公开(公告)日：2010-08-26

申请号：US12297333

申请日：2007-05-29

申请人： Dan Peters ,  Gunnar M. Olsen ,  Elsebet Østergaard Nielsen ,  Daniel B. Timmermann ,  Steven Charles Loechel ,  Jens Damsgaard Mikkelsen ,  Henrik Björk Hansen ,  John Paul Redrobe ,  Jeppe Kejser Christensen ,  Timo Dyhring

发明人： Dan Peters ,  Gunnar M. Olsen ,  Elsebet Østergaard Nielsen ,  Daniel B. Timmermann ,  Steven Charles Loechel ,  Jens Damsgaard Mikkelsen ,  Henrik Björk Hansen ,  John Paul Redrobe ,  Jeppe Kejser Christensen ,  Timo Dyhring

IPC分类号： A61K31/551 ,  C07D471/08 ,  A61P25/00 ,  A61P25/28 ,  A61P25/24 ,  A61P25/18 ,  A61P25/22 ,  A61P29/00 ,  A61P17/10 ,  A61P11/06 ,  A61P1/00

CPC分类号： C07D471/08

摘要： This invention relates to novel 1,4-diaza-bicyclo[3.2.2]nonyl oxadiazolyl derivatives and their use in the manufacture of pharmaceutical compositions. The compounds of the invention 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1,4-二氮杂 - 双环[3.2.2]壬基恶二唑基衍生物及其在制备药物组合物中的用途。 发现本发明的化合物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。

公开(公告)号：US08372832B2

公开(公告)日：2013-02-12

申请号：US13420071

申请日：2012-03-14

申请人： Dan Peters ,  Gunnar M. Olsen ,  Elsebet Østergaard Nielsen ,  Daniel B. Timmermann ,  Steven Charles Loechel ,  Jens Damsgaard Mikkelsen ,  Henrik Björk Hansen ,  John Paul Redrobe ,  Jeppe Kejser Christensen ,  Tino Dyhring

发明人： Dan Peters ,  Gunnar M. Olsen ,  Elsebet Østergaard Nielsen ,  Daniel B. Timmermann ,  Steven Charles Loechel ,  Jens Damsgaard Mikkelsen ,  Henrik Björk Hansen ,  John Paul Redrobe ,  Jeppe Kejser Christensen ,  Tino Dyhring

IPC分类号： A61P25/00 ,  A61K31/551 ,  C07D471/08

CPC分类号： C07D471/08

摘要： This invention relates to novel 1,4-diaza-bicyclo[3.2.2]nonyl oxadiazolyl derivatives and their use in the manufacture of pharmaceutical compositions. The compounds of the invention 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1,4-二氮杂 - 双环[3.2.2]壬基恶二唑基衍生物及其在制备药物组合物中的用途。 发现本发明的化合物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。

公开(公告)号：US20120172353A1

公开(公告)日：2012-07-05

申请号：US13420071

申请日：2012-03-14

申请人： Dan PETERS ,  Gunnar M. Olsen ,  Elsebet Østergaard Nielsen ,  Daniel B. Timmermann ,  Steven Charles Loechel ,  Jens Damsgaard Mikkelsen ,  Henrik Björk Hansen ,  John Paul Redrobe ,  Jeppe Kejser Christensen ,  Tino Dyhring

发明人： Dan PETERS ,  Gunnar M. Olsen ,  Elsebet Østergaard Nielsen ,  Daniel B. Timmermann ,  Steven Charles Loechel ,  Jens Damsgaard Mikkelsen ,  Henrik Björk Hansen ,  John Paul Redrobe ,  Jeppe Kejser Christensen ,  Tino Dyhring

IPC分类号： A61K31/551 ,  A61P25/28 ,  A61P25/00 ,  A61P25/18 ,  A61P25/24 ,  A61P25/22 ,  A61P25/08 ,  A61P29/00 ,  A61P25/06 ,  A61P9/06 ,  A61P21/02 ,  A61P15/06 ,  A61P15/10 ,  A61P11/06 ,  A61P1/12 ,  A61P1/00 ,  A61P17/10 ,  A61P25/36 ,  A61P25/34 ,  A61P25/32 ,  C07D471/08

CPC分类号： C07D471/08

摘要： This invention relates to novel 1,4-diaza-bicyclo[3.2.2]nonyl oxadiazolyl derivatives and their use in the manufacture of pharmaceutical compositions. The compounds of the invention 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1,4-二氮杂 - 双环[3.2.2]壬基恶二唑基衍生物及其在制备药物组合物中的用途。 发现本发明的化合物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。

公开(公告)号：US08158619B2

公开(公告)日：2012-04-17

申请号：US12297333

申请日：2007-05-29

申请人： Dan Peters ,  Gunnar M. Olsen ,  Elsebet ØStergaard Nielsen ,  Daniel B. Timmermann ,  Steven Charles Loechel ,  Jen Damsgaard Mikkelsen ,  Henrik Björk Hansen ,  John Paul Redrobe ,  Jeppe Kejser Christensen ,  Tino Dyhring

发明人： Dan Peters ,  Gunnar M. Olsen ,  Elsebet ØStergaard Nielsen ,  Daniel B. Timmermann ,  Steven Charles Loechel ,  Jen Damsgaard Mikkelsen ,  Henrik Björk Hansen ,  John Paul Redrobe ,  Jeppe Kejser Christensen ,  Tino Dyhring

IPC分类号： A61P25/00 ,  A61K31/551 ,  C07D471/08

CPC分类号： C07D471/08

摘要： This invention relates to novel 1,4-diaza-bicyclo[3.2.2]nonyl oxadiazolyl derivatives and their use in the manufacture of pharmaceutical compositions. The compounds of the invention 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1,4-二氮杂 - 双环[3.2.2]壬基恶二唑基衍生物及其在制备药物组合物中的用途。 发现本发明的化合物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。

公开(公告)号：US20090197872A1

公开(公告)日：2009-08-06

申请号：US12299108

申请日：2007-05-29

申请人： Dan Peters ,  Gunnar M. Olsen ,  Elsebet Ostergaard Nielsen ,  Daniel B. Timmermann ,  Steven Charles Loechel ,  Jens Damsgaard Mikkelsen ,  Henrik Bjork Hansen ,  John Paul Redrobe ,  Jeppe Kejser Christensen ,  Tino Dyhring

发明人： Dan Peters ,  Gunnar M. Olsen ,  Elsebet Ostergaard Nielsen ,  Daniel B. Timmermann ,  Steven Charles Loechel ,  Jens Damsgaard Mikkelsen ,  Henrik Bjork Hansen ,  John Paul Redrobe ,  Jeppe Kejser Christensen ,  Tino Dyhring

IPC分类号： A61K31/551 ,  C07D243/10 ,  A61P25/00

CPC分类号： C07D471/08

摘要： This invention relates to novel 1,4-diaza-bicyclo[3.2.2]nonyl pyrimidinyl derivatives and their use in the manufacture of pharmaceutical compositions. The compounds of the invention 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1,4-二氮杂 - 双环[3.2.2]壬基嘧啶基衍生物及其在制备药物组合物中的用途。 发现本发明的化合物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。

公开(公告)号：US07910578B2

公开(公告)日：2011-03-22

申请号：US12298290

申请日：2007-05-21

申请人： Dan Peters ,  Gunnar M. Olsen ,  Elsebet Østergaard Nielsen ,  Daniel B. Timmermann ,  Steven Charles Loechel ,  Jeppe Kejser Christensen ,  Tino Dyhring

发明人： Dan Peters ,  Gunnar M. Olsen ,  Elsebet Østergaard Nielsen ,  Daniel B. Timmermann ,  Steven Charles Loechel ,  Jeppe Kejser Christensen ,  Tino Dyhring

IPC分类号： C07D487/08 ,  A61K31/551

CPC分类号： C07D487/08

摘要： This invention relates to novel 8,10-diaza-bicyclo[4.3.1]decane derivatives, which are found to be cholinergic ligands at the nicotinic acetylcholine 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), 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8,10-二氮杂 - 双环[4.3.1]癸烷衍生物，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），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。

公开(公告)号：US07915272B2

公开(公告)日：2011-03-29

申请号：US12299114

申请日：2007-05-29

申请人： Dan Peters ,  Gunnar M. Olsen ,  Elsebet Østergaard Nielsen ,  Daniel B Timmermann ,  Steven Charles Loechel

发明人： Dan Peters ,  Gunnar M. Olsen ,  Elsebet Østergaard Nielsen ,  Daniel B Timmermann ,  Steven Charles Loechel

IPC分类号： A61K31/505

CPC分类号： C07D471/08

摘要： This invention relates to a novel 1,4-diaza-bicyclo[3.2.2]nonyl pyrimidinyl derivative and its use in the manufacture of pharmaceutical compositions. The compound of the invention is found to be a cholinergic ligand at the nicotinic acetylcholine receptors.Due to its pharmacological profile the compound 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1,4-二氮杂双环[3.2.2]壬基嘧啶基衍生物及其在制备药物组合物中的用途。 发现本发明的化合物是烟碱乙酰胆碱受体的胆碱能配体。 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病症多种多样 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。

公开(公告)号：US20100317654A1

公开(公告)日：2010-12-16

申请号：US12861420

申请日：2010-08-23

申请人： Dan Peters ,  Gunnar M. Olsen ,  Elsebet Østergaard Nielsen ,  Daniel B. Timmermann ,  Steven Charles Loechel

发明人： Dan Peters ,  Gunnar M. Olsen ,  Elsebet Østergaard Nielsen ,  Daniel B. Timmermann ,  Steven Charles Loechel

IPC分类号： A61K31/551 ,  A61P25/18 ,  A61P25/28 ,  A61P25/24 ,  A61P25/22 ,  A61P25/16 ,  A61P25/00 ,  A61P25/08 ,  A61P25/06 ,  A61P25/02 ,  A61P29/00 ,  A61P11/06 ,  A61P9/10 ,  A61P15/12 ,  A61P9/12 ,  A61P17/10 ,  A61P1/12 ,  A61P25/30 ,  A61P25/32 ,  A61P25/34 ,  A61P25/36 ,  A61P43/00

CPC分类号： C07D471/08

摘要： This invention relates to novel 1,4-diaza-bicyclo[3.2.2]nonyl oxadiazolyl derivatives and their use in the manufacture of pharmaceutical compositions. The compounds of the invention are found to be cholinergic ligands at the nicotinic acetylcholine 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), 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1,4-二氮杂 - 双环[3.2.2]壬基恶二唑基衍生物及其在制备药物组合物中的用途。 发现本发明的化合物是烟碱乙酰胆碱受体的胆碱能配体。 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。

公开(公告)号：US20100234349A1

公开(公告)日：2010-09-16

申请号：US12303927

申请日：2007-09-04

申请人： Gunnar M. Olsen ,  Dan Peters ,  Bjarne H. Dahl ,  Jeppe Kejser Christensen ,  Steven Charles Loechel ,  Daniel B. Timmermann

发明人： Gunnar M. Olsen ,  Dan Peters ,  Bjarne H. Dahl ,  Jeppe Kejser Christensen ,  Steven Charles Loechel ,  Daniel B. Timmermann

IPC分类号： A61K31/554 ,  A61K31/55 ,  A61K31/551 ,  A61K31/5415 ,  A61K31/4985 ,  A61K31/496 ,  A61K31/497 ,  A61K31/519 ,  A61K31/48 ,  A61K31/473 ,  A61K31/445 ,  A61K31/4525 ,  A61K31/454 ,  A61K31/451 ,  A61K31/4439 ,  A61K31/4406 ,  A61K31/4245 ,  A61K31/428 ,  A61K31/4015 ,  A61K31/38 ,  A61K31/343 ,  A61K31/27 ,  A61K31/195 ,  A61K31/17 ,  A61K31/15 ,  A61K31/136 ,  A61K31/138 ,  A61P25/18 ,  A61K31/465 ,  A61P25/00 ,  A61P25/16 ,  A61P25/24 ,  A61P25/22

CPC分类号： A61K45/06 ,  A61K31/4245 ,  A61K31/4439 ,  A61K31/445 ,  A61K31/4523 ,  A61K31/465 ,  A61K31/497 ,  A61K31/55 ,  A61K31/551 ,  A61K31/5513 ,  A61K2300/00

摘要： This invention relates to novel pharmaceutical compositions comprising therapeutically effective combination of a positive allosteric modulator of nicotine receptors; and a cognitive enhancer selected from the group consisting of a nicotine acetylcholine receptor agonist, an acetylcholine esterase inhibitor, a positive AMPA receptor modulator, an antipsychotic drug, an antidepressant drug and an anti Parkinson drug. The pharmaceutical compositions for use according to the invention are contemplated particularly useful for combating cognitive disorders.

摘要翻译： 本发明涉及包含尼古丁受体的正变构调节剂的治疗有效组合的新型药物组合物; 以及选自尼古丁乙酰胆碱受体激动剂，乙酰胆碱酯酶抑制剂，阳性AMPA受体调节剂，抗精神病药物，抗抑郁药物和抗帕金森药物的认知增强剂。 预期根据本发明使用的药物组合物特别可用于对抗认知障碍。

公开(公告)号：US20090186880A1

公开(公告)日：2009-07-23

申请号：US12299594

申请日：2007-05-21

申请人： Dan Peters ,  Gunnar M. Olsen ,  Elsebet Ostergaard Nielsen ,  Daniel B. Timmermann ,  Steven Charles Loechel ,  Jeppe Kejser Christensen ,  Tino Dyhring

发明人： Dan Peters ,  Gunnar M. Olsen ,  Elsebet Ostergaard Nielsen ,  Daniel B. Timmermann ,  Steven Charles Loechel ,  Jeppe Kejser Christensen ,  Tino Dyhring

IPC分类号： A61K31/551 ,  C07D487/08

CPC分类号： C07D471/08

摘要： This invention relates to novel 1,4-diaza-bicyclo[3.2.2]nonane 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.