公开(公告)号：US20100305108A1

公开(公告)日：2010-12-02

申请号：US12742595

申请日：2008-11-13

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

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

IPC分类号： A61K31/551 ,  C07D471/08 ,  A61P25/00 ,  A61P25/18 ,  A61P25/24 ,  A61P3/04 ,  A61P25/28 ,  A61P25/22 ,  A61P25/30 ,  A61P29/00

CPC分类号： C07D471/08

摘要： This invention relates to novel 1,4-diaza-bicyclo[3.2.2]nonyl pyrimidine 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：US20110112119A1

公开(公告)日：2011-05-12

申请号：US12994243

申请日：2009-06-09

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 ,  Jens Damsgaard Mikkelsen

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 ,  Jens Damsgaard Mikkelsen

IPC分类号： C07D453/02 ,  A61K31/517 ,  A61P25/00 ,  A61P25/18 ,  A61P25/28 ,  A61P25/08 ,  A61P25/24 ,  A61P9/00 ,  A61P15/06 ,  A61P9/06 ,  A61P11/06 ,  A61P15/10 ,  A61P29/00 ,  A61P1/00 ,  A61P17/10 ,  A61P17/00 ,  A61P25/34 ,  A61P25/36 ,  A61P25/32 ,  A61P25/16

CPC分类号： C07D453/02

摘要： This invention relates to novel azabicyclooctyl-quinazolinone 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： 本发明涉及新的氮杂双环辛基 - 喹唑啉酮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：US20110046118A1

公开(公告)日：2011-02-24

申请号：US12742590

申请日：2008-11-13

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

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

IPC分类号： A61K31/551 ,  C07D487/08 ,  A61P25/00 ,  A61P1/12 ,  A61P1/04 ,  A61P11/06 ,  A61P15/10 ,  A61P15/04 ,  A61P17/10 ,  A61P29/00

CPC分类号： C07D471/08

摘要： This invention relates to novel 1,4-diaza-bicyclo [3.2.2]nonyl pyrimidine derivatives of formula (I) 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： 本发明涉及式（I）的新的1,4-二氮杂 - 双环[3.2.2]壬基嘧啶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：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：US07687523B2

公开(公告)日：2010-03-30

申请号：US12087004

申请日：2007-02-09

申请人： Dan Peters ,  Daniel B. Timmermann ,  Gunnar M. Olsen ,  Elsebet Østergaard Nielsen ,  Jeppe Kejser Christensen

发明人： Dan Peters ,  Daniel B. Timmermann ,  Gunnar M. Olsen ,  Elsebet Østergaard Nielsen ,  Jeppe Kejser Christensen

IPC分类号： A61K31/44

CPC分类号： C07D471/08

摘要： Compounds of the class 3,9-diaza-bicyclo [3.3.1]nonane derivatives. The compounds correspond to structural Formula (I): wherein Ra is hydrogen or optionally substituted alkyl and Rb is a monocyclic heteroaryl group. The compounds are useful in the treatment, prevention, or alleviation of diseases or disorders or conditions that are responsive to modulation of nicotinic acetylcholine receptors, including cognitive disorders, Alzheimer's disease, attention deficit hyperactivity disorder (ADHD), Tourette's syndrome, Bipolar Disorder, obsessive compulsive disorders (OCD), narcolepsy, senile dementia, autism, Parkinson'disease, Amyotrophic Lateral Sclerosis, epilepsy, and diabetic neuropathy.

摘要翻译： 3,9-二氮杂双环[3.3.1]壬烷衍生物的化合物。 化合物对应于结构式（I）：其中R a是氢或任选取代的烷基，R b是单环杂芳基。 这些化合物可用于治疗，预防或缓解对烟碱乙酰胆碱受体调节，包括认知障碍，阿尔茨海默病，注意力缺陷多动障碍（ADHD），Tourette综合征，双相障碍，强迫症的疾病或病症或病症 强迫症（OCD），发作性睡病，老年痴呆，自闭症，帕金森病，肌萎缩性侧索硬化，癫痫和糖尿病性神经病变。

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：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：US20100298307A1

公开(公告)日：2010-11-25

申请号：US12742627

申请日：2008-11-13

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

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

IPC分类号： A61K31/551 ,  C07D471/08 ,  A61P25/00 ,  A61P3/10 ,  A61P9/12 ,  A61P13/12 ,  A61P17/00 ,  A61P15/10 ,  A61P15/04 ,  A61P1/04 ,  A61P1/12 ,  A61P11/06

CPC分类号： C07D471/08

摘要： This invention relates to novel 1,4-diaza-bicyclo[3.2.2]nonyl pyrimidine derivatives of formula (I) 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： 本发明涉及式（I）的新的1,4-二氮杂 - 双环[3.2.2]壬基嘧啶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。