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.

公开(公告)号：US20090118266A1

公开(公告)日：2009-05-07

申请号：US12300060

申请日：2007-05-29

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

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

IPC分类号： A61K31/5513 ,  C07D471/08 ,  A61P25/28 ,  A61P25/00 ,  A61P25/36 ,  A61P25/34 ,  A61P25/32 ,  A61P9/12 ,  A61P17/06 ,  A61P17/10 ,  A61P17/00 ,  A61P15/12 ,  A61P15/10 ,  A61P15/06 ,  A61P11/06 ,  A61P1/00 ,  A61P25/14 ,  A61P25/24 ,  A61P25/18 ,  A61P25/22 ,  A61P25/06

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：US20090099153A1

公开(公告)日：2009-04-16

申请号：US12298290

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： A61K31/55 ,  C07D487/08

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：US20080242668A1

公开(公告)日：2008-10-02

申请号：US10586838

申请日：2005-02-01

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

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

IPC分类号： A61K31/498 ,  C07D221/02 ,  A61K31/4375 ,  A61P9/00 ,  A61P29/00 ,  A61P25/00 ,  C07D403/02

摘要： This invention relates to azacyclic derivatives according of formula (I) and their use as pharmaceuticals. 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. Formula (I) Aza-X′-A′-Y′-L-Y-A″-X″-Aza Aza:Azabicyclic group A′,A″:Aromatic monocyclic and/or polycyclic, carbocyclic and/or heterocyclic group Y′,Y″: Linker or absent (covalent bond) L: Monocyclic or polycyclic, carbocyclic or heterocyclic group or is absent X′,X″: Linker or absent (covalent bond)

摘要翻译： 本发明涉及式（I）的氮杂环十二烷基衍生物及其作为药物的用途。 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，内分泌疾病或疾病，疾病或。 与“终止化学物质的滥用”引起的与炎症，疼痛和戒断症状有关的神经变性，疾病或病症相关的疾病。 式（I）Aza-X'-A'-Y'-LY-A“-X” - 氮杂氮杂：氮杂双环基A'，A“：芳族单环和/或多环，碳环和/或杂环基 Y'，Y“：连接体或不存在（共价键）L：单环或多环，碳环或杂环基团或不存在X'，X”：连接基或不存在（共价键）

公开(公告)号：US20080227772A1

公开(公告)日：2008-09-18

申请号：US10586749

申请日：2005-02-01

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

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

IPC分类号： A61K31/551 ,  C07D243/10 ,  A61P1/00 ,  A61P25/02 ,  A61P29/00 ,  A61P37/02

CPC分类号： C07D471/08 ,  C07D487/08

摘要： This invention relates to novel diazabicyclic aryl 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： 本发明涉及在尼古丁乙酰胆碱受体中被发现是胆碱能配体的新的二氮杂双环芳基衍生物。 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），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：US20110263577A1

公开(公告)日：2011-10-27

申请号：US13123539

申请日：2009-10-08

申请人： Dan Peters ,  Daniel B. Timmermann ,  Gunnar M. Olsen ,  Elsebet Østergaard Nielsen ,  Philip K. Ahring ,  Tino Dyhring ,  Jeppe Kejser Christensen

发明人： Dan Peters ,  Daniel B. Timmermann ,  Gunnar M. Olsen ,  Elsebet Østergaard Nielsen ,  Philip K. Ahring ,  Tino Dyhring ,  Jeppe Kejser Christensen

IPC分类号： A61K31/551 ,  A61P25/00 ,  A61P25/28 ,  A61P25/18 ,  A61P25/24 ,  A61P25/22 ,  A61P3/04 ,  A61P25/20 ,  A61P25/08 ,  A61P25/16 ,  A61P25/14 ,  A61P25/02 ,  A61P25/04 ,  A61P25/06 ,  A61P29/00 ,  A61P9/06 ,  A61P21/00 ,  A61P1/00 ,  A61P1/12 ,  A61P11/06 ,  A61P43/00 ,  A61P15/00 ,  A61P9/12 ,  A61P17/00 ,  A61P17/10 ,  A61P25/30 ,  A61P25/34 ,  A61P25/36 ,  A61P25/32 ,  C07D471/08

CPC分类号： C07D471/08

摘要： This invention relates to novel oxadiazolyl-diazabicyclononane 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： 本发明涉及新的恶二唑基 - 二氮杂双环壬烷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：US20110118268A1

公开(公告)日：2011-05-19

申请号：US12921931

申请日：2009-03-09

申请人： Dan Peters ,  Daniel B. Timmermann ,  Elsebet Østergaard Nielsen ,  Gunnar M. Olsen ,  Tino Dyhring ,  Jeppe Kejser Christensen ,  Philip K. Ahring ,  John Paul Redrobe

发明人： Dan Peters ,  Daniel B. Timmermann ,  Elsebet Østergaard Nielsen ,  Gunnar M. Olsen ,  Tino Dyhring ,  Jeppe Kejser Christensen ,  Philip K. Ahring ,  John Paul Redrobe

IPC分类号： A61K31/4995 ,  C07D487/08 ,  A61P25/18 ,  A61P25/22 ,  A61P25/24 ,  A61P25/08 ,  A61P25/14 ,  A61P15/10 ,  A61P1/12 ,  A61P11/06 ,  A61P9/12 ,  A61P17/10 ,  A61P25/32 ,  A61P25/30 ,  A61P25/34 ,  A61P25/36

CPC分类号： C07D487/08

摘要： This invention relates to novel 1,4-diaza-bicyclo[3.2.1]octane 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. (formula)

摘要翻译： 本发明涉及新的1,4-二氮杂双环[3.2.1]辛烷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。 （式）

公开(公告)号：US20110112078A1

公开(公告)日：2011-05-12

申请号：US12997053

申请日：2009-06-09

申请人： Dan Peters ,  Daniel B. Timmermann ,  Elsebet Ostergaard Nielsen ,  Gunnar M. Olsen ,  Philip K. Ahring ,  Tino Dyhring ,  Jeppe Kejser Christensen ,  John Paul Redrobe ,  Jens Damsgaard Mikkelsen

发明人： Dan Peters ,  Daniel B. Timmermann ,  Elsebet Ostergaard Nielsen ,  Gunnar M. Olsen ,  Philip K. Ahring ,  Tino Dyhring ,  Jeppe Kejser Christensen ,  John Paul Redrobe ,  Jens Damsgaard Mikkelsen

IPC分类号： A61K31/551 ,  C07D487/08 ,  A61P25/00 ,  A61P25/28 ,  A61P25/18 ,  A61P25/16 ,  A61P25/22 ,  A61P25/08 ,  A61P29/00 ,  A61P11/06 ,  A61P17/10 ,  A61P9/12

CPC分类号： C07D487/08

摘要： This invention relates to novel oxadiazolyl-diazabicyclononane derivatives and their use in the manufacture of pharmaceutical compositions. The compounds of the invention are found to be cholinergic ligands at the nicotinic acetylcholin 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： 本发明涉及新的恶二唑基 - 二氮杂双环壬烷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酰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。