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71. 发明授权

US08796311B2 3-cyano-4-(4-tetrahydropyran-phenyl)-pyridin-2-one derivatives 有权
公开(公告)号：US08796311B2
公开(公告)日：2014-08-05
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
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.

72. 发明授权

US08772504B2 Substituted benzoxazole, benzimidazole, oxazolopyridine and imidazopyridine derivatives as gamma secretase modulators 有权
标题翻译：取代的苯并恶唑，苯并咪唑，恶唑并吡啶和咪唑并吡啶衍生物作为γ分泌酶调节剂
公开(公告)号：US08772504B2
公开(公告)日：2014-07-08
申请号：US13144557
申请日：2010-02-15
申请人： Henricus Jacobus Maria Gijsen , François Paul Bischoff , Wei Zhuang , Sven Franciscus Anna Van Brandt , Michel Surkyn , Mirko Zaja , Didier Jean-Claude Berthelot , Michel Anna Jozef De Cleyn , Gregor James MacDonald , Daniel Oehlrich
发明人： Henricus Jacobus Maria Gijsen , François Paul Bischoff , Wei Zhuang , Sven Franciscus Anna Van Brandt , Michel Surkyn , Mirko Zaja , Didier Jean-Claude Berthelot , Michel Anna Jozef De Cleyn , Gregor James MacDonald , Daniel Oehlrich
IPC分类号： C07D235/00 , C07D403/02
CPC分类号： C07D413/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/14 , C07D413/14 , C07D471/04
摘要： The present invention is concerned with novel substituted benzoxazole, benzimidazole, oxazolopyridine and imidazopyridine derivatives of Formula (I) wherein R1, R2, R3, R4, X, A1, A2, A3, A4, Y1, Y2, Y3 and Z have the meaning defined in the claims. The compounds according to the present invention are useful as gamma secretase modulators. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.
摘要翻译：本发明涉及式（I）的新的取代苯并恶唑，苯并咪唑，恶唑并吡啶和咪唑并吡啶衍生物，其中R1，R2，R3，R4，X，A1，A2，A3，A4，Y1，Y2，Y3和Z具有含义在权利要求中限定。根据本发明的化合物可用作γ-分泌酶调节剂。本发明还涉及制备这种新化合物的方法，包含所述化合物作为活性成分的药物组合物以及所述化合物作为药物的用途。

73. 发明授权

US08710074B2 Dihydronaphthyridinyl(organo)methanone analogs as positive allosteric mGluR5 modulators 失效
标题翻译：二氢萘并（甲氧基）甲酮类似物作为正变构mGluR5调节剂
公开(公告)号：US08710074B2
公开(公告)日：2014-04-29
申请号：US13349476
申请日：2012-01-12
申请人： P. Jeffrey Conn , Craig W. Lindsley , Shaun R. Stauffer , Jason Manka , Jon Jacobs , Ya Zhou , José Manuel Bartolomé-Nebreda , Gregor James MacDonald , Susana Conde-Ceide , Eric S. Dawson
发明人： P. Jeffrey Conn , Craig W. Lindsley , Shaun R. Stauffer , Jason Manka , Jon Jacobs , Ya Zhou , José Manuel Bartolomé-Nebreda , Gregor James MacDonald , Susana Conde-Ceide , Eric S. Dawson
IPC分类号： A61K31/4375 , A61P25/00 , A61P25/28 , A61P25/18 , A61P25/08 , A61P35/00 , A61P29/00 , A61P3/10 , A61P3/04 , C07D471/04 , A61P25/06
CPC分类号： C07D471/04
摘要： In one aspect, the invention relates to dihydronaphthyridinyl(organo)methanone analogs, 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，本发明涉及二氢硫吡啶基（有机）甲酮类似物，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。

74. 发明申请

US20130338185A1 1,2,4-TRIAZOLO[4,3-a]PYRIDINE DERIVATIVES AND THEIR USE AS POSITIVE ALLOSTERIC MODULATORS OF MGLUR2 RECEPTORS 有权
公开(公告)号：US20130338185A1
公开(公告)日：2013-12-19
申请号：US13883906
申请日：2011-11-08
申请人： José Maria Cid-Núñez , Andrés Avelino Trabanco-Suärez , Juan Antonio Vega Ramiro , Daniel Oehlrich , Gary John Tresadern , Gregor James MacDonald
发明人： José Maria Cid-Núñez , Andrés Avelino Trabanco-Suärez , Juan Antonio Vega Ramiro , Daniel Oehlrich , Gary John Tresadern , Gregor James MacDonald
IPC分类号： C07D471/04 , A61K45/06 , A61K31/437
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.

75. 发明授权

US08466153B2 Piperidinylamino-pyridazines and their use as fast dissociating dopamine 2 receptor antagonists 有权
标题翻译：哌啶基氨基哒嗪及其作为快速解离多巴胺2受体拮抗剂的用途
公开(公告)号：US08466153B2
公开(公告)日：2013-06-18
申请号：US12516645
申请日：2007-12-05
申请人： Gregor James MacDonald , José Ignacio Andrés-Gil , Frans Alfons Maria Van Den Keybus , José Manuel Bartolomé-Nebreda , Michiel Luc Maria Van Gool
发明人： Gregor James MacDonald , José Ignacio Andrés-Gil , Frans Alfons Maria Van Den Keybus , José Manuel Bartolomé-Nebreda , Michiel Luc Maria Van Gool
IPC分类号： A61K31/501 , C07D237/20 , A61P25/28
CPC分类号： C07D401/12
摘要： The present invention relates to 6-(piperidin-4-ylamino)pyridazin-3-carbonitriles of the general formula (I); or a pharmaceutically acceptable salt thereof, or a stereoisomeric form, that are fast dissociating dopamine 2 receptor antagonists, as well as 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：本发明涉及通式（I）的6-（哌啶-4-基氨基）哒嗪-3-腈：或其药学上可接受的盐或立体异构形式，其是快速解离的多巴胺2受体拮抗剂，以及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。

76. 发明申请

US20130150412A1 1,4-DISUBSTITUTED 3-CYANO-PYRIDONE DERIVATIVES AND THEIR USE AS POSITIVE MGLUR2-RECEPTOR 审中-公开
标题翻译： 1,4-取代的3-氰基 - 吡咯烷酮衍生物及其作为阳性MGLUR2受体的用途
公开(公告)号：US20130150412A1
公开(公告)日：2013-06-13
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： 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。

77. 发明申请

US20120258955A1 BICYCLIC THIAZOLES AS ALLOSTERIC MODULATORS OF MGLUR5 RECEPTORS 有权
公开(公告)号：US20120258955A1
公开(公告)日：2012-10-11
申请号：US13516985
申请日：2010-12-16
申请人： Gregor James MacDonald , Andrés Avelino Trabanco-Suárez , Susana Conde-Ceide , Gary John Tresadern , José Manuel Bartolomé-Nebreda , Joaquin Pastor-Fernández
发明人： Gregor James MacDonald , Andrés Avelino Trabanco-Suárez , Susana Conde-Ceide , Gary John Tresadern , José Manuel Bartolomé-Nebreda , Joaquin Pastor-Fernández
IPC分类号： A61K31/437 , A61K31/55 , A61P25/00 , A61P25/18 , A61K31/444 , A61P25/22 , A61P25/30 , A61P25/28 , A61P25/16 , A61P3/04 , C07D513/04 , A61P25/24
CPC分类号： C07D513/04 , A61K31/4365
摘要： The present invention relates to novel bicyclic thiazoles which are positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (“mGluR5”) and which are useful for the treatment or prevention of disorders associated with glutamate dysfunction and diseases in which the mGluR5 subtype of receptors is involved. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention and treatment of disorders in which mGluR5 is involved.

78. 发明申请

US20120220581A1 IMIDAZO[1,2-b]PYRIDAZINE DERIVATIVES AND THEIR USE AS PDE10 INHIBITORS 审中-公开
标题翻译：咪唑并[1,2-b]吡啶衍生物及其用作PDE10抑制剂
公开(公告)号：US20120220581A1
公开(公告)日：2012-08-30
申请号：US13505187
申请日：2010-10-27
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
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
IPC分类号： A61K31/5377 , A61K31/5025 , A61P25/00 , A61P25/18 , A61P3/00 , A61P25/14 , A61P25/28 , A61P25/30 , A61P25/04 , C07D487/04 , 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。

79. 发明申请

US20120184528A1 7-ARYL-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： 7-ARYL-1,2,4-三唑并[4,3-a]吡啶衍生物及其作为MGLUR2受体的阳性免疫调节剂的用途
公开(公告)号：US20120184528A1
公开(公告)日：2012-07-19
申请号：US13319568
申请日：2010-05-11
申请人： Jose Maria Cic-Nunez , Ana Isabel De Lucas Olivares , Andres Avelino Trabanco-Suarez , Gregor James MacDonald
发明人： Jose Maria Cic-Nunez , Ana Isabel De Lucas Olivares , Andres Avelino Trabanco-Suarez , Gregor James MacDonald
IPC分类号： A61K31/553 , A61K31/437 , A61K31/5377 , A61K31/496 , A61P25/00 , A61P25/22 , A61P25/18 , A61P25/30 , A61P3/00 , A61P25/06 , A61P25/08 , A61P25/28 , A61P9/10 , A61P25/24 , C07D471/04
CPC分类号： C07D471/04 , A61K9/0014 , A61K9/0019 , A61K9/0095 , A61K9/06 , A61K9/2009 , A61K9/2018 , A61K9/2059 , A61K31/437 , A61K31/444 , A61K31/4545 , A61K31/5377 , A61K45/06 , A61K47/06 , A61K47/10 , A61K47/26 , A61K47/38 , 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。

80. 发明申请

US20110269748A1 2-ANILINE-4-ARYL SUBSTITUTED THIAZOLE DERIVATIVES 有权
标题翻译： 2-苯胺-4-芳基取代的噻唑衍生物
公开(公告)号：US20110269748A1
公开(公告)日：2011-11-03
申请号：US12063689
申请日：2008-02-13
申请人： Johannes Wilhelmus John F. Thuring , Gregor James MacDonald , Christopher James Grantham , Theodorus Dinklo , Anne Simone Josephine Lesage
发明人： Johannes Wilhelmus John F. Thuring , Gregor James MacDonald , Christopher James Grantham , Theodorus Dinklo , Anne Simone Josephine Lesage
IPC分类号： A61K31/426 , C07D417/04 , C07D417/14 , A61K31/4439 , A61K31/444 , A61K31/506 , A61K31/437 , A61K31/429 , A61K31/5377 , A61K31/519 , A61K31/5513 , A61P25/00 , A61P25/18 , A61P25/22 , A61P25/20 , A61P25/24 , C07D277/42
CPC分类号： C07D471/04 , C07D277/42 , C07D417/04 , C07D417/12 , C07D417/14 , C07D513/04
摘要： This invention concerns the use of a compound of formula (I) a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochemically isomeric form thereof, wherein Z is hydrogen, halo, C1-6alkyl, Het1, HO—C1-6alkyl-, cyano-C1-6alkyl-, amino-C(═O)—C1-6alkyl-, formylamino-C1-6alkyl-, C1-6alkyl-C(═O)—NH—C1-6alkyl-, mono- or di(C1-6alkyl)amino-C(═O)—C1-6alkyl-, phenyl-C1-6alkyl-, or Het4-C1-6alkyl-; Q is phenyl, pyridyl, benzofuranyl, 2,3-dihydro-benzofuranyl, pyrazolyl, isoxazolyl or indazolyl wherein each of said ring systems is optionally being substituted with up to three substituents each independently selected from halo, cyano, C1-6alkyl, C1-6alkyl-O—, C1-6alkylthio, Ar or polyhaloC1-6alkyl; L is phenyl, pyridyl, pyrimidazolyl, 8-Azapyrimidazolyl, pyridazinyl, imidazothiazolyl or furanyl wherein each of said ring systems may optionally be substituted with one or two or more substituents, each substituent independently being selected from halo, hydroxy, amino, cyano, C1-6alkyl or C1-6alkyl-O—; Het1 represents morpholinyl; pyrazolyl or imidazolyl; Het4 represents morpholinyl, pyrazolyl or imidazolyl; Ar represents phenyl optionally substituted with halo, C1-6alkyl, C1-6alkyl-O— or polyhaloC1-6alkyl; for the manufacture of a medicament for the prevention or the treatment or prophylaxis of psychotic disorders, intellectual impairment disorders or diseases or conditions in which modulation of the α7 nicotinic receptor is beneficial.
摘要翻译：本发明涉及式（I）化合物的N-氧化物，药学上可接受的加成盐，季胺及其立体化学异构体形式的用途，其中Z是氢，卤素，C 1-6烷基，Het 1，HO-C 1 C 1-6烷基 - ，氰基-C 1-6烷基 - ，氨基-C（= O）-C 1-6烷基 - ，甲酰基氨基-C 1-6烷基 - ，C 1-6烷基-C（= O）-NH-C 1-6烷基 - 或二（C 1-6烷基）氨基-C（= O）-C 1-6烷基 - ，苯基-C 1-6烷基 - 或Het 4 -C 1-6烷基 - ; Q是苯基，吡啶基，苯并呋喃基，2,3-二氢 - 苯并呋喃基，吡唑基，异恶唑基或吲唑基，其中每个所述环系统任选地被至多三个独立地选自卤素，氰基，C 1-6烷基， C 1-6烷基-O-，C 1-6烷硫基，Ar或多卤代C 1-6烷基; L是苯基，吡啶基，嘧唑基，8-氮杂唑基，哒嗪基，咪唑并噻唑基或呋喃基，其中每个所述环系可任选地被一个或两个或多个取代基取代，每个取代基独立地选自卤素，羟基，氨基，氰基，C 1 -6-烷基或C 1-6烷基-O-; Het1表示吗啉基; 吡唑基或咪唑基; Het4表示吗啉基，吡唑基或咪唑基; Ar表示任选被卤素，C 1-6烷基，C 1-6烷基-O-或多卤代C 1-6烷基取代的苯基; 用于制备用于预防或治疗或预防精神病，智力障碍或其中α7烟碱受体的调节有益的疾病或病症的药物。

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