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：US20110144008A1

公开(公告)日：2011-06-16

申请号：US12957916

申请日：2010-12-01

申请人： Bjarne Due LARSEN ,  Jens Damsgaard Mikkelsen ,  Søren Neve

发明人： Bjarne Due LARSEN ,  Jens Damsgaard Mikkelsen ,  Søren Neve

IPC分类号： A61K38/26 ,  C07K14/605 ,  A61P3/10 ,  A61P3/04

CPC分类号： C07K14/605 ,  A61K38/00 ,  A61K38/26 ,  A61K47/62 ,  C07K14/57563

摘要： Novel peptide agonists of GLP-1 activity useful for lowering blood glucose levels. The novel peptides comprise variants of the GLP-1 or the exendin-4 polypeptide sequence and are pharmacologically active and stable. These peptides are useful in the treatment of diseases that benefit from regulation of excess levels of blood glucose and/or regulation of gastric emptying, such as diabetes and eating disorders.

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：US20100317572A1

公开(公告)日：2010-12-16

申请号：US12809365

申请日：2008-12-18

申请人： Jens Damsgaard Mikkelsen

发明人： Jens Damsgaard Mikkelsen

IPC分类号： A61K38/22 ,  A61K31/46 ,  A61K31/397 ,  A61K38/26 ,  A61K31/55 ,  A61K31/485 ,  A61K31/5375 ,  A61K38/28 ,  A61P1/04

CPC分类号： A61K45/06 ,  A61K31/46 ,  A61K2300/00

摘要： This invention relates to novel pharmaceutical compositions comprising a therapeutically effective combination of a compound of Formula I and an anti-obesity compound. The pharmaceutical compositions for use according to the invention are contemplated particularly useful for combating obesity or an obesity associated disease.

摘要翻译： 本发明涉及包含式I化合物和抗肥胖化合物的治疗有效组合的新型药物组合物。 预期根据本发明使用的药物组合物特别可用于抵抗肥胖症或肥胖相关疾病。

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：US20110118304A1

公开(公告)日：2011-05-19

申请号：US12743546

申请日：2008-11-19

申请人： Jens Damsgaard Mikkelsen ,  Naheed Mirza

发明人： Jens Damsgaard Mikkelsen ,  Naheed Mirza

IPC分类号： A61K31/439 ,  A61P25/30

CPC分类号： A61K31/46

摘要： A method for treating over-eating disorders, in particular Bulimia nervosa, Binge Eating Disorder (BED), and Compulsive Over-Eating. The invention furthermore relates to novel pharmaceutical compositions for the treatment of over-eating disorders comprising a therapeutically effective amount of a compound of formula I.

摘要翻译： 一种治疗过度饮食障碍的方法，特别是神经性惊厥症，BED饮食障碍（BED）和强迫性过度饮食。 本发明还涉及用于治疗过度进食障碍的新型药物组合物，其包含治疗有效量的式I化合物。

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。