公开(公告)号：US20110130408A1

公开(公告)日：2011-06-02

申请号：US13056287

申请日：2009-07-29

申请人： José Manuel l Bartolmé-Nebreda ,  Gregor James Macdonald ,  Michiel Luc,Maria Van Gool

发明人： José Manuel l Bartolmé-Nebreda ,  Gregor James Macdonald ,  Michiel Luc,Maria Van Gool

IPC分类号： A61K31/496 ,  A61P25/16 ,  A61P25/18 ,  A61P25/22 ,  A61P25/30 ,  A61P25/28 ,  C07D401/04

CPC分类号： C07D213/74 ,  C07D213/84

摘要： The present invention relates to piperazin-1-yl-trifluoromethyl-substituted-pyridines that are fast dissociating dopamine 2 receptor antagonists, processes for preparing these compounds, pharmaceutical compositions comprising these compounds as an active ingredient. The compounds find utility as medicines for treating or preventing central nervous system disorders, for example schizophrenia, by exerting an antipsychotic effect without motor side effects.

摘要翻译： 本发明涉及快速解离多巴胺2受体拮抗剂的哌嗪-1-基 - 三氟甲基取代的吡啶，制备这些化合物的方法，包含这些化合物作为活性成分的药物组合物。 该化合物可用作治疗或预防中枢神经系统疾病（例如精神分裂症）的药物，通过发挥抗精神病作用而没有运动副作用。

公开(公告)号：US20110269752A1

公开(公告)日：2011-11-03

申请号：US13096545

申请日：2011-04-28

申请人： Joaquin Pastor-Fernández ,  José Manuel Bartolomé-Nebreda ,  Gregor James Macdonald ,  Susana Conde-Ceide ,  Óscar Delgado-González ,  Greta Constantia Peter Vanhoof ,  Michiel Luc Maria Van Gool ,  María Luz Martin-Martín ,  Sergio-Alvar Alonso-de Diego ,  Kelly Ann Swinney ,  Carina Leys ,  Johan Erwin Edmond Weerts ,  Stijn Wuyts

发明人： Joaquin Pastor-Fernández ,  José Manuel Bartolomé-Nebreda ,  Gregor James Macdonald ,  Susana Conde-Ceide ,  Óscar Delgado-González ,  Greta Constantia Peter Vanhoof ,  Michiel Luc Maria Van Gool ,  María Luz Martin-Martín ,  Sergio-Alvar Alonso-de Diego ,  Kelly Ann Swinney ,  Carina Leys ,  Johan Erwin Edmond Weerts ,  Stijn Wuyts

IPC分类号： A61K31/5377 ,  C07D471/04 ,  A61K31/5025 ,  A61P25/18 ,  A61P3/00 ,  A61P25/14 ,  A61P25/28 ,  A61P25/30 ,  A61P25/00 ,  C07D413/14 ,  A61P25/22

CPC分类号： C07D487/04

摘要： The present invention relates to novel imidazo[1,2-b]pyridazine derivatives which are inhibitors of the phosphodiesterase 10 enzyme (PDE10) and which are useful for the treatment or prevention of neurological, psychiatric and metabolic disorders in which the PDE10 enzyme is involved. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes to prepare such compounds and compositions, to the use of such compounds or pharmaceutical compositions for the prevention or treatment of neurological, psychiatric and metabolic disorders and diseases.

摘要翻译： 本发明涉及作为磷酸二酯酶10酶（PDE10）的抑制剂的新的咪唑并[1,2-b]哒嗪衍生物，它们可用于治疗或预防涉及PDE10酶的神经，精神和代谢紊乱 。 本发明还涉及包含这些化合物的药物组合物，以制备这些化合物和组合物以使用这些化合物或药物组合物来预防或治疗神经，精神和代谢疾病和疾病。

公开(公告)号：US08716282B2

公开(公告)日：2014-05-06

申请号：US13096545

申请日：2011-04-28

申请人： Joaquin Pastor-Fernández ,  José Manuel Bartolomé-Nebreda ,  Gregor James Macdonald ,  Susana Conde-Ceide ,  Óscar Delgado-González ,  Greta Constantia Peter Vanhoof ,  Michiel Luc Maria Van Gool ,  María Luz Martín-Martín ,  Sergio-Alvar Alonso-de Diego ,  Kelly Ann Swinney ,  Carina Leys ,  Johan Erwin Edmond Weerts ,  Stijn Wuyts

发明人： Joaquin Pastor-Fernández ,  José Manuel Bartolomé-Nebreda ,  Gregor James Macdonald ,  Susana Conde-Ceide ,  Óscar Delgado-González ,  Greta Constantia Peter Vanhoof ,  Michiel Luc Maria Van Gool ,  María Luz Martín-Martín ,  Sergio-Alvar Alonso-de Diego ,  Kelly Ann Swinney ,  Carina Leys ,  Johan Erwin Edmond Weerts ,  Stijn Wuyts

IPC分类号： A61K31/5025 ,  A61K31/5377 ,  C07D413/14 ,  C07D403/14 ,  C07D487/04

CPC分类号： C07D487/04

摘要： The present invention relates to novel imidazo[1,2-b]pyridazine derivatives which are inhibitors of the phosphodiesterase 10 enzyme (PDE10) and which are useful for the treatment or prevention of neurological, psychiatric and metabolic disorders in which the PDE10 enzyme is involved. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes to prepare such compounds and compositions, to the use of such compounds or pharmaceutical compositions for the prevention or treatment of neurological, psychiatric and metabolic disorders and diseases.

摘要翻译： 本发明涉及作为磷酸二酯酶10酶（PDE10）的抑制剂的新的咪唑并[1,2-b]哒嗪衍生物，它们可用于治疗或预防涉及PDE10酶的神经，精神和代谢紊乱 。 本发明还涉及包含这些化合物的药物组合物，以制备这些化合物和组合物以使用这些化合物或药物组合物来预防或治疗神经，精神和代谢疾病和疾病。

公开(公告)号：US09067891B2

公开(公告)日：2015-06-30

申请号：US13610000

申请日：2012-09-11

申请人： Jose Maria Cid-Nunez ,  Andres Avelino Trabanco-Suarez ,  Gregor James Macdonald ,  Guillaume Albert Jacques Duvey ,  Robert Johannes Lutjens

发明人： Jose Maria Cid-Nunez ,  Andres Avelino Trabanco-Suarez ,  Gregor James Macdonald ,  Guillaume Albert Jacques Duvey ,  Robert Johannes Lutjens

IPC分类号： A61K31/443 ,  C07D401/04 ,  C07D213/85 ,  A61K31/198 ,  A61K31/444

CPC分类号： C07D213/85 ,  A61K31/198 ,  A61K31/444

摘要： The present invention relates to novel compounds, in particular novel pyridinone derivatives according to Formula (I) including any stereochemically isomeric form thereof, or a pharmaceutically acceptable salt thereof or a solvate thereof, wherein all radicals are defined in the application and claims. The compounds according to the invention are positive allosteric modulators of metabotropic glutamate receptors subtype 2 (“mGluR2”) which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. In particular, such diseases are central nervous system disorders selected from the group of anxiety, schizophrenia, migraine, depression, and epilepsy. The invention is also directed to pharmaceutical compositions and processes to prepare such compounds and such compositions, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR2 is involved.

摘要翻译： 本发明涉及新化合物，特别是包括其任何立体化学异构形式的式（I）的新型吡啶酮衍生物或其药学上可接受的盐或其溶剂合物，其中所有基团在本申请和权利要求书中定义。 根据本发明的化合物是代谢型谷氨酸受体亚型2（“mGluR2”）的正变构调节剂，其可用于治疗或预防与谷氨酸功能障碍相关的神经和精神病学障碍以及涉及代谢型受体的mGluR2亚型的疾病 。 特别地，这些疾病是选自焦虑，精神分裂症，偏头痛，抑郁症和癫痫组的中枢神经系统疾病。 本发明还涉及药物组合物和制备这些化合物和这些组合物的方法，以及这些化合物用于预防和治疗其中涉及mGluR2的疾病的用途。

公开(公告)号：US20170022181A1

公开(公告)日：2017-01-26

申请号：US15264185

申请日：2016-09-13

申请人： Marcel Frans Leopold De Bruyn ,  Gregor James Macdonald ,  Ludo Edmond Josephine Kennis ,  Xavier Jean Michel Langlois ,  Frans Alfons Maria Van den Keytus ,  Yves Emiel Maria Van Roosbroeck

发明人： Marcel Frans Leopold De Bruyn ,  Gregor James Macdonald ,  Ludo Edmond Josephine Kennis ,  Xavier Jean Michel Langlois ,  Frans Alfons Maria Van den Keytus ,  Yves Emiel Maria Van Roosbroeck

IPC分类号： C07D401/12 ,  C07D409/14

CPC分类号： C07D401/12 ,  A61K31/501 ,  C07D409/14

摘要： The present invention relates to compounds that are fast dissociating dopamine 2 receptor antagonists, processes for preparing these compounds, pharmaceutical compositions comprising these compounds as an active ingredient. The compounds find utility as medicines for treating or preventing central nervous system disorders, for example schizophrenia, by exerting an antipsychotic effect without motor side effects.

摘要翻译： 本发明涉及快速解离多巴胺2受体拮抗剂，制备这些化合物的方法，包含这些化合物作为活性成分的药物组合物。 该化合物可用作治疗或预防中枢神经系统疾病（例如精神分裂症）的药物，通过发挥抗精神病作用而没有运动副作用。

公开(公告)号：US08791144B2

公开(公告)日：2014-07-29

申请号：US13496120

申请日：2010-09-16

申请人： Gregor James Macdonald ,  Johannes Wilhelmus John F. Thuring ,  Frans Alfons Maria Van den Keybus ,  Yves Emiel Maria Van Roosbroeck

发明人： Gregor James Macdonald ,  Johannes Wilhelmus John F. Thuring ,  Frans Alfons Maria Van den Keybus ,  Yves Emiel Maria Van Roosbroeck

IPC分类号： A61K31/4439 ,  C07D401/04

CPC分类号： C07D401/04

摘要： The present invention relates to N-phenyl-1-(4-pyridinyl)-1H-pyrazol-3-amine derivatives and pharmaceutically acceptable salts thereof, processes for preparing them, pharmaceutical compositions containing them and their use in therapy, according to formula (I) Wherein R1, R2, R3, R4, R5, R6 have the meaning defined in the claims. The invention particularly relates to positive allosteric modulators of nicotinic acetylcholine receptors, such positive allosteric modulator having the capability to increase the efficacy of nicotinic receptor agonists.

摘要翻译： 本发明涉及N-苯基-1-（4-吡啶基）-1H-吡唑-3-胺衍生物及其药学上可接受的盐，其制备方法，含有它们的药物组合物及其在治疗中的用途，根据式 I）其中R1，R2，R3，R4，R5，R6具有权利要求中限定的含义。 本发明特别涉及烟碱乙酰胆碱受体的正变构调节剂，这种正变构调节剂具有增加烟碱受体激动剂功效的能力。

公开(公告)号：US20120225844A1

公开(公告)日：2012-09-06

申请号：US13329025

申请日：2011-12-16

申请人： P. Jeffrey Conn ,  Craig W. Lindsley ,  Shaun R. Stauffer ,  José Manuel Bartolomé-Nebreda ,  Susana Conde-Ceide ,  Gregor James Macdonald ,  Han Min Tong ,  Carrie K. Jones ,  Manuel Jesús Alcázar-Vaca ,  José Ignacio Andrés-Gil ,  Chrysa Malosh

发明人： P. Jeffrey Conn ,  Craig W. Lindsley ,  Shaun R. Stauffer ,  José Manuel Bartolomé-Nebreda ,  Susana Conde-Ceide ,  Gregor James Macdonald ,  Han Min Tong ,  Carrie K. Jones ,  Manuel Jesús Alcázar-Vaca ,  José Ignacio Andrés-Gil ,  Chrysa Malosh

IPC分类号： C07D487/04 ,  A61K31/695 ,  C07F7/08 ,  A61P35/04 ,  A61P25/20 ,  A61P25/18 ,  A61P25/08 ,  A61P25/28 ,  A61P25/06 ,  A61K31/4985 ,  A61P25/00

CPC分类号： C07D487/04 ,  A61K31/40 ,  A61K31/4985 ,  A61K31/501 ,  A61K31/506 ,  A61K31/695 ,  A61K45/06 ,  C07F7/1804

摘要： In one aspect, the invention relates to bicyclic triazole and pyrazole lactams, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

摘要翻译： 一方面，本发明涉及双代三唑和吡唑内酰胺，其衍生物和相关化合物，其可用作代谢型谷氨酸受体亚型5（mGluR5）的正变构调节剂; 制备化合物的合成方法; 包含该化合物的药物组合物; 以及使用所述化合物和组合物治疗与谷氨酸官能障碍相关的神经和精神障碍的方法。 该摘要旨在作为用于在特定技术中进行搜索的扫描工具，而不意在限制本发明。

公开(公告)号：US09271967B2

公开(公告)日：2016-03-01

申请号：US13883906

申请日：2011-11-08

申请人： José Maria Cid-Núñez ,  Andrés Avelino Trabanco-Suárez ,  Juan Antonio Vega Ramiro ,  Daniel Oehlrich ,  Gary John Tresadern ,  Gregor James Macdonald

发明人： José Maria Cid-Núñez ,  Andrés Avelino Trabanco-Suárez ,  Juan Antonio Vega Ramiro ,  Daniel Oehlrich ,  Gary John Tresadern ,  Gregor James Macdonald

IPC分类号： A61K31/44 ,  C07D491/02 ,  A61K31/437 ,  A61K45/06 ,  C07D471/04 ,  A61K9/00 ,  A61K9/06 ,  A61K9/20

CPC分类号： A61K31/437 ,  A61K9/0014 ,  A61K9/0019 ,  A61K9/0095 ,  A61K9/06 ,  A61K9/2059 ,  A61K45/06 ,  C07D471/04 ,  A61K2300/00

摘要： The present invention relates to novel triazolo[4,3-a]pyridine derivatives of Formula (I) wherein all radicals are as defined in the claims. The compounds according to the invention are positive allosteric modulators of the metabotropic glutamate receptor subtype 2 (“mGluR2”), which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes to prepare such compounds and compositions, and to the use of such compounds for the prevention or treatment of neurological and psychiatric disorders and diseases in which mGluR2 is involved.

公开(公告)号：US09090632B2

公开(公告)日：2015-07-28

申请号：US13819273

申请日：2011-08-31

申请人： P. Jeffrey Conn ,  Craig W. Lindsley ,  Shaun R. Stauffer ,  Carrie K. Jones ,  Jose Manuel Bartolome-Nebreda ,  Susana Conde-Ceide ,  Gregor James Macdonald ,  Manuel Jesus Alcazar Vaca

发明人： P. Jeffrey Conn ,  Craig W. Lindsley ,  Shaun R. Stauffer ,  Carrie K. Jones ,  Jose Manuel Bartolome-Nebreda ,  Susana Conde-Ceide ,  Gregor James Macdonald ,  Manuel Jesus Alcazar Vaca

IPC分类号： C07D513/04 ,  C07D498/04

CPC分类号： C07D513/04 ,  C07D498/04

摘要： In one aspect, the invention relates to novel bicyclic oxazole and thiazole compounds which are positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (“mGluR5”); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions; and methods for the treatment or prevention of disorders associated with glutamate dysfunction and diseases in which the mGluR5 subtype of receptors is involved. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

摘要翻译： 一方面，本发明涉及作为代谢型谷氨酸受体亚型5（“mGluR5”）的正变构调节剂的新型双环恶唑和噻唑化合物。 制备化合物的合成方法; 包含该化合物的药物组合物; 使用该化合物和组合物治疗与谷氨酸功能障碍相关的神经和精神障碍的方法; 以及用于治疗或预防与谷氨酸功能障碍相关的病症和其中涉及mGluR5亚型亚型的疾病的方法。 该摘要旨在作为用于在特定技术中进行搜索的扫描工具，而不意在限制本发明。

公开(公告)号：US20100286206A1

公开(公告)日：2010-11-11

申请号：US12677691

申请日：2008-09-12

申请人： Jose Maria Cid-Nunez ,  Andres Avelino Trabanco-Suarez ,  Gregor James Macdonald ,  Guillaume Albert Jacques Duvey ,  Robert Johannes Lutjens ,  Patrick Terry Finn

发明人： Jose Maria Cid-Nunez ,  Andres Avelino Trabanco-Suarez ,  Gregor James Macdonald ,  Guillaume Albert Jacques Duvey ,  Robert Johannes Lutjens ,  Patrick Terry Finn

IPC分类号： A61K31/444 ,  C07D401/12 ,  C07D213/64 ,  A61K31/4422 ,  A61P25/28 ,  A61P25/10 ,  A61P25/12 ,  A61P25/18 ,  A61P25/22 ,  A61P9/10 ,  A61P25/30 ,  A61P25/08 ,  A61P25/00 ,  A61P25/32 ,  A61P3/04 ,  A61P25/06 ,  A61P25/24

CPC分类号： C07D213/64 ,  C07D401/12

摘要： The present invention relates to novel compounds, in particular novel pyridinone derivatives according to Formula (I) wherein all radicals are as defined in the application and claims. The compounds according to the invention are positive allosteric modulators of metabotropic receptors—subtype 2 (“mGluR2”) which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. In particular, such diseases are central nervous system disorders selected from the group of anxiety, schizophrenia, migraine, depression, and epilepsy. The invention is also directed to pharmaceutical compositions and processes to prepare such compounds and compositions, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR2 is involved.

摘要翻译： 本发明涉及新化合物，特别是根据式（I）的新型吡啶酮衍生物，其中所有基团如申请和权利要求中所定义。 根据本发明的化合物是代谢型受体亚型2（“mGluR2”）的正性变构调节剂，其可用于治疗或预防与谷氨酸功能障碍相关的神经和精神障碍以及参与代谢型受体的mGluR2亚型的疾病 。 特别地，这些疾病是选自焦虑，精神分裂症，偏头痛，抑郁症和癫痫组的中枢神经系统疾病。 本发明还涉及制备这些化合物和组合物的药物组合物和方法，以及这些化合物用于预防和治疗其中涉及mGluR2的疾病的用途。