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：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。

公开(公告)号：US08637510B2

公开(公告)日：2014-01-28

申请号：US13512464

申请日：2010-11-25

申请人： Gregor James Macdonald ,  Benoit Christian Albert Ghislain De Boeck ,  Joseph Elisabeth Leenaerts

发明人： Gregor James Macdonald ,  Benoit Christian Albert Ghislain De Boeck ,  Joseph Elisabeth Leenaerts

IPC分类号： A61K31/535 ,  C07D413/14

CPC分类号： C07D417/14

摘要： The present invention relates to morpholinothiazole derivatives and pharmaceutically acceptable salts thereof, processes for preparing them, pharmaceutical compositions containing them and their use in therapy. The invention particularly relates to positive allosteric modulators of nicotinic acetylcholine receptors, such positive allosteric modulators having the capability to increase the efficacy of nicotinic receptor agonists.

摘要翻译： 本发明涉及吗啉代噻唑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。 本发明特别涉及烟碱乙酰胆碱受体的正变构调节剂，这种正性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：US20130197019A1

公开(公告)日：2013-08-01

申请号：US13803267

申请日：2013-03-14

申请人： Jose Maria CID-NUNEZ ,  Andres Avelino Trabanco-Suarez ,  Gregor James Macdonald ,  Guillaume Albert Jacques Duvey ,  Robert Johannes Lütjens ,  Terry Patrick Finn

发明人： Jose Maria CID-NUNEZ ,  Andres Avelino Trabanco-Suarez ,  Gregor James Macdonald ,  Guillaume Albert Jacques Duvey ,  Robert Johannes Lütjens ,  Terry Patrick Finn

IPC分类号： C07D401/04 ,  C07D491/107 ,  A61K31/444 ,  A61K45/06 ,  A61K31/4545

CPC分类号： A61K31/4545 ,  A61K9/0014 ,  A61K9/0019 ,  A61K9/08 ,  A61K9/10 ,  A61K9/2009 ,  A61K9/2013 ,  A61K9/2018 ,  A61K9/2059 ,  A61K31/444 ,  A61K31/5377 ,  A61K45/06 ,  A61K47/10 ,  A61K47/44 ,  C07D211/86 ,  C07D401/04 ,  C07D491/107 ,  C07D493/10 ,  A61K2300/00

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。

公开(公告)号：US07531558B2

公开(公告)日：2009-05-12

申请号：US10545283

申请日：2004-02-12

申请人： Gregor James Macdonald ,  Darren Jason Mitchell ,  Harshad Kantilal Rami ,  Mervyn Thompson ,  Leontine Saskia Trouw ,  Susan Marie Westaway

发明人： Gregor James Macdonald ,  Darren Jason Mitchell ,  Harshad Kantilal Rami ,  Mervyn Thompson ,  Leontine Saskia Trouw ,  Susan Marie Westaway

IPC分类号： A61K31/4436 ,  C07D417/12

CPC分类号： C07D401/12 ,  C07D417/12

摘要： Compounds of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein P, W, X, Y, R2, R3, r and s are as defined in the specification, processes for preparing such compounds, pharmaceutical compositions comprising such compounds and their use in therapy.

摘要翻译： 式（I）化合物或其药学上可接受的盐或溶剂合物，其中P，W，X，Y，R 2，R 3，r和s如本说明书中所定义，制备此类化合物的方法，包含这些化合物的药物组合物 及其在治疗中的应用。

公开(公告)号：US20080227791A1

公开(公告)日：2008-09-18

申请号：US12091219

申请日：2006-10-24

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

IPC分类号： A61K31/501 ,  C07D401/12

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：US08993591B2

公开(公告)日：2015-03-31

申请号：US13883818

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 ,  C07D515/02 ,  A61K31/498 ,  A61K31/542 ,  A61K45/06 ,  C07D471/02 ,  C07D471/04 ,  A61K9/20 ,  A61K31/437 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/5377 ,  A61K9/00 ,  A61K47/06 ,  A61K47/10 ,  A61K47/26 ,  A61K9/06 ,  A61K47/38

CPC分类号： A61K31/498 ,  A61K9/0014 ,  A61K9/0019 ,  A61K9/0095 ,  A61K9/06 ,  A61K9/2009 ,  A61K9/2018 ,  A61K9/2059 ,  A61K31/437 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/542 ,  A61K45/06 ,  A61K47/06 ,  A61K47/10 ,  A61K47/26 ,  A61K47/38 ,  C07D471/02 ,  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.

摘要翻译： 本发明涉及式（I）的新的三唑并[4,3-a]吡啶衍生物，其中所有基团如权利要求中所定义。 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代谢代谢受体的mGluR2亚型 参与。 本发明还涉及包含这种化合物的药物组合物，制备这些化合物和组合物的方法，以及这些化合物用于预防或治疗其中涉及mGluR2的神经和精神疾病和疾病的用途。

公开(公告)号：US20140155393A1

公开(公告)日：2014-06-05

申请号：US13883818

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： C07D471/04 ,  A61K31/498 ,  A61K31/5377 ,  A61K31/496 ,  A61K31/437 ,  A61K45/06

CPC分类号： A61K31/498 ,  A61K9/0014 ,  A61K9/0019 ,  A61K9/0095 ,  A61K9/06 ,  A61K9/2009 ,  A61K9/2018 ,  A61K9/2059 ,  A61K31/437 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/542 ,  A61K45/06 ,  A61K47/06 ,  A61K47/10 ,  A61K47/26 ,  A61K47/38 ,  C07D471/02 ,  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.

摘要翻译： 本发明涉及式（I）的新的三唑并[4,3-a]吡啶衍生物，其中所有基团如权利要求中所定义。 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代谢代谢受体的mGluR2亚型 参与。 本发明还涉及包含这种化合物的药物组合物，制备这些化合物和组合物的方法，以及这些化合物用于预防或治疗其中涉及mGluR2的神经和精神疾病和疾病的用途。

公开(公告)号：US20130252952A1

公开(公告)日：2013-09-26

申请号：US13884149

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： A61K31/5377 ,  A61K45/06 ,  C07D471/04

CPC分类号： A61K31/5377 ,  A61K9/0019 ,  A61K9/06 ,  A61K9/10 ,  A61K9/2009 ,  A61K31/542 ,  A61K45/06 ,  C07D471/04

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.

摘要翻译： 本发明涉及式（I）的新的三唑并[4,3-a]吡啶衍生物，其中所有基团如权利要求中所定义。 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代谢代谢受体的mGluR2亚型 参与。 本发明还涉及包含这种化合物的药物组合物，制备这些化合物和组合物的方法，以及这些化合物用于预防或治疗其中涉及mGluR2的神经和精神疾病和疾病的用途。

公开(公告)号：US20120238561A1

公开(公告)日：2012-09-20

申请号：US13512464

申请日：2010-11-25

申请人： Gregor James Macdonald ,  Benoît Christian Albert Ghislain De Boeck ,  Joseph Elisabeth Leenaerts

发明人： Gregor James Macdonald ,  Benoît Christian Albert Ghislain De Boeck ,  Joseph Elisabeth Leenaerts

IPC分类号： A61K31/5377 ,  A61P25/00 ,  A61P25/22 ,  A61P25/18 ,  A61P25/24 ,  A61P25/16 ,  A61P25/14 ,  A61P25/34 ,  A61P29/00 ,  A61P31/00 ,  A61P11/06 ,  A61P17/06 ,  A61P1/00 ,  A61P9/04 ,  A61P11/00 ,  A61P37/06 ,  C07D417/14 ,  C07D498/08 ,  A61K31/5386 ,  A61P25/28

CPC分类号： C07D417/14

摘要： The present invention relates to morpholinothiazole derivatives and pharmaceutically acceptable salts thereof, processes for preparing them, pharmaceutical compositions containing them and their use in therapy. The invention particularly relates to positive allosteric modulators of nicotinic acetylcholine receptors, such positive allosteric modulators having the capability to increase the efficacy of nicotinic receptor agonists.

摘要翻译： 本发明涉及吗啉代噻唑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。 本发明特别涉及烟碱乙酰胆碱受体的正变构调节剂，这种正性变构调节剂具有增加烟碱受体激动剂功效的能力。