公开(公告)号：US06943159B1

公开(公告)日：2005-09-13

申请号：US09641814

申请日：2000-08-18

申请人： Alex Haahr Gouliaev ,  Mogens Larsen ,  Thomas Varming ,  Claus Mathiesen ,  Tina Holm Johansen ,  Jørgen Scheel-Krüger ,  Gunnar M. Olsen ,  Elsebet Østergaard Nielsen

发明人： Alex Haahr Gouliaev ,  Mogens Larsen ,  Thomas Varming ,  Claus Mathiesen ,  Tina Holm Johansen ,  Jørgen Scheel-Krüger ,  Gunnar M. Olsen ,  Elsebet Østergaard Nielsen

IPC分类号： C07D239/90 ,  C07D285/24 ,  C07D285/28 ,  C07D417/04 ,  C07D513/04 ,  A61K31/505 ,  A61K31/54 ,  C07D401/04 ,  C07D403/04

CPC分类号： C07D417/04 ,  C07D239/90 ,  C07D285/24 ,  C07D285/28 ,  C07D513/04

摘要： The invention provides novel compounds represented by general formula (I) wherein the bond represented by the broken line may be a single, double bond or absent; and if the bond is absent, then the nitrogen is substituted with a hydrogen and R2; X represents SO2 or C═O of CH2; Y represents —CH(R4)—, —N(R4)—CH2—, O; and the meaning of R2, R3, R4, R5, R6, R7, and R8 are as defined in the application. The compounds are useful as positive modulators of the AMPA-receptor.

摘要翻译： 本发明提供由通式（I）表示的新型化合物，其中由虚线表示的键可以是单键或双键或不存在; 并且如果该键不存在，则氮被氢和R 2取代; X表示CH 2 2的SO 2或C-O; Y表示-CH（R 4） - ， - N（R 4） - CH 2 - ，O; 并且R 2，R 3，R 4，R 5，R 6，R 6， / SUP>，R 7和R 8如申请中所定义。 该化合物可用作AMPA受体的阳性调节剂。

公开(公告)号：US06617459B2

公开(公告)日：2003-09-09

申请号：US09855630

申请日：2001-05-15

申请人： Dan Peters ,  Jørgen Scheel-Krüger ,  Elsebet Østergaard Nielsen

发明人： Dan Peters ,  Jørgen Scheel-Krüger ,  Elsebet Østergaard Nielsen

IPC分类号： C07D45104

CPC分类号： C07D451/14 ,  A61K51/0455 ,  C07D451/02

摘要： The present invention relates to 8-azabicyclo[3.2.1]oct-2-ene derivatives in their labelled form. Furthermore, the present invention relates to the use of said derivatives in their labelled or unlabelled form in diagnostic methods, in particular for in vivo receptor imaging (neuroimaging).

摘要翻译： 本发明涉及其标记形式的8-氮杂双环[3.2.1]辛-2-烯衍生物。 此外，本发明涉及所述衍生物在其标记或未标记形式的诊断方法中的用途，特别是用于体内受体成像（神经成像）。

公开(公告)号：US08236793B2

公开(公告)日：2012-08-07

申请号：US12633505

申请日：2009-12-08

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

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

IPC分类号： A61K31/55 ,  C07D243/10

CPC分类号： C07D471/08

摘要： This invention relates to novel diazabicyclic aryl 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芳基衍生物，其在烟碱乙酰胆碱受体和单胺受体和转运蛋白的调节剂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：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：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：US20100227869A1

公开(公告)日：2010-09-09

申请号：US12160402

申请日：2007-02-13

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

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

IPC分类号： A61K31/501 ,  C07D403/12 ,  A61P25/00 ,  A61P29/00 ,  A61P1/00 ,  A61P9/12 ,  A61P15/00 ,  A61P17/00

CPC分类号： C07D453/02

摘要： This invention relates to novel enantiopure azabicyclo pyridazinyloxy 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： 本发明涉及新型对映纯氮氮杂双环哒嗪氧基衍生物，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。

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：US20100210625A1

公开(公告)日：2010-08-19

申请号：US12733168

申请日：2008-08-14

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

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

IPC分类号： A61K31/551 ,  C07D487/08 ,  A61P29/00 ,  A61P25/30 ,  A61P17/00 ,  A61P1/00 ,  A61P15/00 ,  A61P25/06 ,  A61P25/18 ,  A61P25/28 ,  A61P25/16 ,  A61P25/08

CPC分类号： C07D471/08

摘要： This invention relates to novel 1,4-diaza-bicyclo[3.2.2]nonyl heteroaryl 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]壬基杂芳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：US07750022B2

公开(公告)日：2010-07-06

申请号：US10568148

申请日：2004-06-29

申请人： Dan Peters ,  Gunnar M. Olsen ,  Elsebet Østergaard Nielsen ,  Philip K. Ahring ,  Tino Dyhring Jørgensen ,  Michael R. Schrimpf ,  Kevin B. Sippy

发明人： Dan Peters ,  Gunnar M. Olsen ,  Elsebet Østergaard Nielsen ,  Philip K. Ahring ,  Tino Dyhring Jørgensen ,  Michael R. Schrimpf ,  Kevin B. Sippy

IPC分类号： A61K31/4745 ,  C07D453/02

CPC分类号： C07D453/02

摘要： This invention relates to novel quinuclidine derivatives 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.

摘要翻译： 本发明涉及新的奎宁环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：US07750011B2

公开(公告)日：2010-07-06

申请号：US11884345

申请日：2006-02-13

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

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

IPC分类号： C07D403/04 ,  C07D401/04 ,  C07D409/04 ,  C07D405/14 ,  A61K31/501 ,  A61K31/497 ,  A61P21/00 ,  A61P5/00 ,  A61P25/00 ,  A61P29/00

CPC分类号： C07D487/08

摘要： This invention relates to novel diazabicyclic aryl 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： 本发明涉及在尼古丁乙酰胆碱受体和单胺受体和转运蛋白的调节剂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。