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1. 发明授权

US08937060B2 1,2,4-triazolo [4,3-A] pyridine derivatives and their use for the treatment of prevention of neurological and psychiatric disorders 有权
标题翻译： 1,2,4-三唑并[4,3-A]吡啶衍生物及其用于治疗神经和精神疾病的用途
公开(公告)号：US08937060B2
公开(公告)日：2015-01-20
申请号：US13319541
申请日：2010-05-11
申请人： Jose Maria Cid-Nunez , Daniel Oehlrich , Andres Avelino Trabanco-Suarez , Gary John Tresadern , Juan Antonio Vega Ramiro , Gregor James MacDonald
发明人： Jose Maria Cid-Nunez , Daniel Oehlrich , Andres Avelino Trabanco-Suarez , Gary John Tresadern , Juan Antonio Vega Ramiro , Gregor James MacDonald
IPC分类号： C07D487/04 , C07D241/04 , C07D265/30 , A61K31/5375 , A61K31/5377 , A61K31/496
CPC分类号： A61K31/496 , A61K9/0019 , A61K9/0095 , A61K9/06 , A61K9/10 , A61K9/2059 , A61K31/437 , A61K31/438 , A61K31/4545 , A61K31/506 , A61K31/5377 , A61K45/06 , C07D471/04 , C07D519/00 , 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。

2. 发明授权

US08906939B2 3-cyano-4-(4-tetrahydropyran-phenyl)-pyridin-2-one derivatives 有权
标题翻译： 3-氰基-4-（4-四氢吡喃 - 苯基） - 吡啶-2-酮衍生物
公开(公告)号：US08906939B2
公开(公告)日：2014-12-09
申请号：US12529568
申请日：2008-03-07
申请人： Jose Maria Cid-Nunez , Andres Avelino Trabanco-Suarez , Gregor James MacDonald , Guillaume Albert Jacques Duvey
发明人： Jose Maria Cid-Nunez , Andres Avelino Trabanco-Suarez , Gregor James MacDonald , Guillaume Albert Jacques Duvey
IPC分类号： C07D405/12 , A61K31/4433
CPC分类号： C07D405/12
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化物，其中所有基团在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。

3. 发明申请

US20110275624A1 INDOLE AND BENZOMORPHOLINE DERIVATIVES AS MODULATORS OF METABOTROPIC GLUTAMATE RECEPTORS 有权
标题翻译：作为代谢型谷氨酸盐受体的调节剂的吲哚和苯并吡喃衍生物
公开(公告)号：US20110275624A1
公开(公告)日：2011-11-10
申请号：US13123984
申请日：2009-10-15
申请人： Jose Maria Cid-Nunez , Andres Avelino Trabanco-Suarez
发明人： Jose Maria Cid-Nunez , Andres Avelino Trabanco-Suarez
IPC分类号： A61K31/538 , C07D401/10 , A61K31/4439 , A61P25/28 , A61P25/24 , A61P25/08 , A61P25/18 , C07D413/14 , A61P25/00
CPC分类号： C07D413/04 , C07D401/04 , C07D405/14 , C07D413/14
摘要： The present invention relates to novel compounds, in particular novel indole and benzomorpholine 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：本发明涉及新的化合物，特别是根据式（I）的新的吲哚和苯并吗啉衍生物，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。

4. 发明申请

US20100240706A1 1,3-DISUBSTITUTED-4-PHENYL-1H-PYRIDIN-2-ONES 有权
标题翻译： 1,3-苯并噻唑-4-基] - 吡啶-2-酮
公开(公告)号：US20100240706A1
公开(公告)日：2010-09-23
申请号：US12677628
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： A61K31/436 , C07D405/12 , C07D405/14 , A61P25/00 , A61P25/22 , A61P25/18 , A61P25/06 , A61P25/30 , A61P25/32 , A61P25/36
CPC分类号： C07D405/12 , C07D213/64 , C07D405/14
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。

5. 发明授权

US08946205B2 1,2,4-triazolo[4,3-a]pyridine derivatives and their use as positive allosteric modulators of mGluR2 receptors 有权
标题翻译： 1,2,4-三唑并[4,3-a]吡啶衍生物及其作为mGluR2受体的正变构调节剂的用途
公开(公告)号：US08946205B2
公开(公告)日：2015-02-03
申请号：US13319558
申请日：2010-05-11
申请人： Jose Maria Cid-Nunez , Ana Isabel De Lucas Olivares , Andres Avelino Trabanco-Suarez , Gregor James MacDonald
发明人： Jose Maria Cid-Nunez , Ana Isabel De Lucas Olivares , Andres Avelino Trabanco-Suarez , Gregor James MacDonald
IPC分类号： A61K31/553 , A61K31/437 , A61K31/538 , A61K31/506 , C07D471/04 , C07D519/00 , A61K45/06 , A61K31/444 , A61K9/00 , A61K9/06 , A61K9/08 , A61K9/10 , A61K9/20
CPC分类号： C07D471/04 , A61K9/0014 , A61K9/0095 , A61K9/06 , A61K9/08 , A61K9/10 , A61K9/2009 , A61K9/2059 , A61K31/437 , A61K31/444 , A61K31/553 , A61K45/06 , C07D519/00 , 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。

6. 发明授权

US08841323B2 1, 4-disubstituted 3-cyano-pyridone derivatives and their use as positive allosteric modulators of MGLUR2-receptors 有权
标题翻译： 1,4-二取代的3-氰基 - 吡啶酮衍生物及其作为MGLUR2受体的正变构调节剂的用途
公开(公告)号：US08841323B2
公开(公告)日：2014-09-23
申请号：US12282663
申请日：2007-03-15
申请人： Jose Maria Cid-Nunez , Jose Ignacio Andres-Gil , Andres Avelino Trabanco-Suarez , Julen Oyarzabal Santamarina , Frank Matthias Dautzenberg , Gregor James MacDonald , Shirley Elizabeth Pullan , Robert Johannes Lutjens , Guillaume Albert Jacques Duvey , Vanthea Nhem , Terry Patrick Finn , Gagik Melikyan , Vincent Mutel
发明人： Hassan Julien Imogai , Jose Maria Cid-Nunez , Jose Ignacio Andres-Gil , Andres Avelino Trabanco-Suarez , Julen Oyarzabal Santamarina , Frank Matthias Dautzenberg , Gregor James MacDonald , Shirley Elizabeth Pullan , Robert Johannes Lutjens , Guillaume Albert Jacques Duvey , Vanthea Nhem , Terry Patrick Finn , Gagik Melikyan
IPC分类号： A61K31/4439 , C07D213/85
CPC分类号： C07D213/85 , C07D213/84 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/12 , C07D401/14 , C07D405/04 , C07D405/06 , C07D405/12 , C07D409/04 , C07D413/04 , C07D413/10 , C07D413/12 , C07D417/04 , C07D417/12 , C07D471/04 , C07D471/10 , C07D487/08 , C07D491/04 , C07D491/10 , C07D495/04
摘要： The present invention relates to novel compounds, in particular novel pyridinone derivatives according to Formula (I) wherein all radicals are 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：本发明涉及新型化合物，特别是根据式（I）的新型吡啶酮衍生物，其中所有基团在申请和权利要求书中定义。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。

7. 发明授权

US08748621B2 1,3-disubstituted 4-(aryl-X-phenyl)-1H-pyridin-2-ones 有权
标题翻译： 1,3-二取代的4-（芳基-N-苯基）-1H-吡啶-2-酮
公开(公告)号：US08748621B2
公开(公告)日：2014-06-10
申请号：US13556547
申请日：2012-07-24
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： A61K31/44 , C07D211/72 , C07D213/64
CPC分类号： C07D213/64 , C07D401/12
摘要： The present invention relates to a method of treating, ameliorating, or controlling a condition in a mammal, including a human, wherein the condition is selected from the group consisting of anxiety disorders, psychotic disorders, substance-dependence related disorders, mood disorders, epilepsy or convulsive disorders, idiopathic Parkinson's disease, and Alzheimer's disease, wherein the method comprises administering to the mammal an effective amount of a compound of Formula (I) wherein all radicals are as defined in the application and claims. In particular, such conditions are central nervous system disorders selected from the group of anxiety, schizophrenia, depression, and epilepsy.
摘要翻译：本发明涉及一种治疗，改善或控制哺乳动物，包括人的病症的方法，其中所述病症选自焦虑症，精神障碍，物质依赖性相关疾病，情绪障碍，癫痫或惊厥性疾病，特发性帕金森病和阿尔茨海默氏病，其中所述方法包括向哺乳动物施用有效量的式（I）化合物，其中所有基团如申请和权利要求中所定义。特别地，这些病症是选自焦虑，精神分裂症，抑郁症和癫痫组的中枢神经系统疾病。

8. 发明授权

US08691813B2 Indole and benzoxazine derivatives as modulators of metabotropic glutamate receptors 有权
标题翻译：吲哚和苯并恶嗪衍生物作为代谢型谷氨酸受体的调节剂
公开(公告)号：US08691813B2
公开(公告)日：2014-04-08
申请号：US13131360
申请日：2009-11-24
申请人： Jose Maria Cid-Nunez , Andres Avelino Trabanco-Suarez , Gregor James MacDonald
发明人： Jose Maria Cid-Nunez , Andres Avelino Trabanco-Suarez , Gregor James MacDonald
IPC分类号： C07D471/04 , A61K31/437
CPC分类号： C07D265/36
摘要： The present invention relates to novel indole and benzoxazine derivatives which are positive allosteric modulators of the metabotropic glutamate receptor subtype 2 (“mGluR2”) and 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 and to the use of such compounds and compositions for the prevention or treatment of neurological and psychiatric disorders and diseases in which mGluR2 is involved.
摘要翻译：本发明涉及新的吲哚和苯并恶嗪衍生物，其是代谢型谷氨酸受体亚型2（“mGluR2”）的正性变构调节剂，其可用于治疗或预防与谷氨酸能力障碍相关的神经和精神障碍及其中涉及代谢型受体的mGluR2亚型。本发明还涉及包含这些化合物的药物组合物以及这些化合物和组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。

9. 发明申请

US20130197019A1 1',3'-DISUBSTITUTED-4-PHENYL-3,4,5,6-TETRAHYDRO-2H,1'H-[1,4']BIPYRIDINYL-2'-ONES 审中-公开
标题翻译： 1'，3'-取代-4-苯基-3,4,5,6-四氢-2H- -2H- 1H，[1,4']联吡啶-2'-酮
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。

10. 发明授权

US08252937B2 1,3-disubstituted 4-(aryl-X-phenyl)-1H-pyridin-2-ones 有权
标题翻译： 1,3-二取代的4-（芳基-N-苯基）-1H-吡啶-2-酮
公开(公告)号：US08252937B2
公开(公告)日：2012-08-28
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： C07D211/72 , A61K31/44
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。

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