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1.发明公开IMIDAZO [1, 2 -A]PYRAZINE DERIVATIVES AND THEIR USE FOR THE PREVENTION OR TREATMENT OF NEUROLOGICAL, PSYCHIATRIC AND METABOLIC DISORDERS AND DISEASES 有权咪唑并[1,2-A]哒嗪衍生物及其在神经，精神和代谢病症和疾病的预防或治疗
公开(公告)号：EP2545055A1
公开(公告)日：2013-01-16
申请号：EP11707172.0
申请日：2011-03-08
发明人： BARTOLOMÉ-NEBREDA, José, Manuel , CONDE-CEIDE, Susana , MACDONALD, Gregor, James , PASTOR-FERNÁNDEZ, Joaquin , VAN GOOL, Michiel, Luc, Maria , MARTÍN-MARTÍN, María, Luz , VANHOOF, Greta, Constantia, Peter
IPC分类号： C07D487/04 , A61K31/4985 , A61P3/00 , A61P25/00
CPC分类号： C07D487/04 , A61K31/5377
摘要： The present invention relates to novel imidazo[1,2-a]pyrazine 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： 本发明涉及新的咪唑并[1,2-a]吡嗪衍生物，其是磷酸二酯酶10（PDE10）并且其抑制剂可用于其中PDE10酶参与神经，精神和代谢性疾病的治疗或预防有用的 ， 因此，本发明涉及药物组合物，包含测试化合物，以处理，以制备测试化合物和组合物，涉及使用测试的化合物或药物组合物用于治疗神经，精神和代谢病症和疾病的预防或治疗的。
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2.发明授权Imidazo[1,2-a]pyrazine derivatives and their use for the prevention or treatment of neurological, psychiatric and metabolic disorders and diseases 有权咪唑并[1,2-a]吡嗪衍生物及其用于预防或治疗神经，精神和代谢疾病和疾病的用途
公开(公告)号：EP2545055B1
公开(公告)日：2017-08-09
申请号：EP11707172.0
申请日：2011-03-08
发明人： BARTOLOMÉ-NEBREDA, José, Manuel , CONDE-CEIDE, Susana , MACDONALD, Gregor, James , PASTOR-FERNÁNDEZ, Joaquin , VAN GOOL, Michiel, Luc, Maria , MARTÍN-MARTÍN, María, Luz , VANHOOF, Greta, Constantia, Peter
IPC分类号： C07D487/04 , A61K31/4985 , A61P3/00 , A61P25/00
CPC分类号： C07D487/04 , A61K31/5377
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公开(公告)号：EP2513118B1
公开(公告)日：2013-09-18
申请号：EP10790989.7
申请日：2010-12-16
发明人： MACDONALD, Gregor, James , TRESADERN, Gary, John , TRABANCO-SUÁREZ, Andrés, Avelino , PASTOR-FERNÁNDEZ, Joaquin
IPC分类号： C07D277/60 , C07D417/04 , C07D417/06 , C07D417/12 , C07D513/04
CPC分类号： C07D277/60 , A61K31/4365 , C07D417/04 , C07D417/06 , C07D417/12 , C07D513/04
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4.发明授权SUBSTITUTED PYRAZINONE DERIVATIVES AS ALPHA2C-ADRENORECEPTOR ANTAGONISTS 有权取代PYRADINON衍生物作为ALPHA2阻断剂
公开(公告)号：EP1966191B1
公开(公告)日：2010-03-17
申请号：EP06841410.1
申请日：2006-12-18
发明人： ANDRÉS-GIL, José, Ignacio , ALCÁZAR-VACA, Manuel, Jesús , LINARES DE LA MORENA, Maria Lourdes , MARTINEZ GONZALEZ, Sonia , OYARZABAL SANTAMARINA, Julen , PASTOR-FERNÁNDEZ, Joaquin , VEGA RAMIRO, Juan, Antonio , DRINKENBURG, Wilhelmus, Helena, Ignatius, Maria
IPC分类号： C07D401/12 , A61K31/497 , A61P25/00
CPC分类号： C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14
摘要： The present invention concerns substituted pyrazinone derivatives according to the general Formula (I) a pharmaceutically acceptable acid or base addition salt thereof, a stereo- chemically isomeric form thereof, an N-oxide form thereof or a quaternary ammonium salt thereof, wherein the variables are defined in Claim 1, having se- lective α2C-adrenoceptor antagonist activity. It further relates to their preparation, compositions comprising them and their use as a medicine. The compounds according to the invention are usefull for the prevention and/or treatment of central nervous system disorders, mood disorders, anxiety disorders, stress-related disorders associated with depression and/or anxiety, cognitive disorders, personality disorders, schizoaffective disorders, Parkinson's disease, dementia of the Alzheimer's type, chronic pain conditions, neurodegenerative diseases, addiction disorders, mood disorders and sexual dysfunction.
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公开(公告)号：EP2029553A1
公开(公告)日：2009-03-04
申请号：EP07729335.5
申请日：2007-05-21
发明人： ANDRÉS-GIL, José Ignacio , ALCÁZAR-VACA, Manuel Jesús , LINARES DE LA MORENA, Maria Lourdes , MARTINEZ GONZALEZ, Sonia , OYARZABAL SANTAMARINA, Julen , PASTOR-FERNÁNDEZ, Joaquin , VEGA RAMIRO, Juan, Antonio , DELGADO-JIMÉNEZ, Francisca , DRINKENBURG, Wilhelmus, Helena, Ignatius, Maria
IPC分类号： C07D241/18 , C07D401/12 , C07D401/14 , C07D403/06 , C07D405/14 , A61K31/497 , A61P25/28
CPC分类号： C07D403/06 , C07D241/18 , C07D401/12 , C07D401/14 , C07D405/14
摘要： The present invention concerns substituted pyrazinone derivatives according to the general Formula (I) a pharmaceutically acceptable acid or base addition salt thereof, a stereochemically isomeric form thereof, an N-oxide form thereof or a quaternary ammonium salt thereof, wherein the variables are defined in Claim 1, having selective α2C-adrenoceptor antagonist activity. It further relates to their preparation, compositions comprising them and their use as a medicine. The compounds according to the invention are usefull for the prevention and/or treatment of central nervous system disorders, mood disorders, anxiety disorders, stress-related disorders associated with depression and/or anxiety, cognitive disorders, personality disorders, schizoaffective disorders, Parkinson's disease, dementia of the Alzheimer's type, chronic pain conditions, neurodegenerative diseases, addiction disorders, mood disorders and sexual dysfunction.
摘要翻译： 本发明涉及根据通式（I）的取代的吡嗪酮衍生物，其药学上可接受的酸或碱加成盐，其立体化学异构形式，其N-氧化物形式或其季铵盐，其中变量如 权利要求1，具有选择性α2C肾上腺素受体拮抗剂活性。 它进一步涉及它们的制备，包含它们的组合物以及它们作为药物的用途。 本发明化合物用于预防和/或治疗中枢神经系统病症，情绪障碍，焦虑症，与抑郁症和/或焦虑症相关的压力相关病症，认知障碍，人格障碍，情感分裂性精神障碍，帕金森病 ，阿尔茨海默型痴呆，慢性疼痛症状，神经退行性疾病，成瘾症，情绪障碍和性功能障碍。
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6.发明公开SUBSTITUTED PYRAZINONE DERIVATIVES AS ALPHA2C-ADRENORECEPTOR ANTAGONISTS 有权取代PYRADINON衍生物作为ALPHA2阻断剂
公开(公告)号：EP1966191A1
公开(公告)日：2008-09-10
申请号：EP06841410.1
申请日：2006-12-18
发明人： ANDRÉS-GIL, José, Ignacio , ALCÁZAR-VACA, Manuel, Jesús , LINARES DE LA MORENA, Maria Lourdes , MARTINEZ GONZALEZ, Sonia , OYARZABAL SANTAMARINA, Julen , PASTOR-FERNÁNDEZ, Joaquin , VEGA RAMIRO, Juan, Antonio , DRINKENBURG, Wilhelmus, Helena, Ignatius, Maria
IPC分类号： C07D401/12 , A61K31/497 , A61P25/00
CPC分类号： C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14
摘要： The present invention concerns substituted pyrazinone derivatives according to the general Formula (I) a pharmaceutically acceptable acid or base addition salt thereof, a stereo- chemically isomeric form thereof, an N-oxide form thereof or a quaternary ammonium salt thereof, wherein the variables are defined in Claim 1, having se- lective α2C-adrenoceptor antagonist activity. It further relates to their preparation, compositions comprising them and their use as a medicine. The compounds according to the invention are usefull for the prevention and/or treatment of central nervous system disorders, mood disorders, anxiety disorders, stress-related disorders associated with depression and/or anxiety, cognitive disorders, personality disorders, schizoaffective disorders, Parkinson's disease, dementia of the Alzheimer's type, chronic pain conditions, neurodegenerative diseases, addiction disorders, mood disorders and sexual dysfunction.
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7.发明授权IMIDAZO[1,2-b]PYRIDAZINE DERIVATIVES AND THEIR USE AS PDE10 INHIBITORS 有权咪唑并[1,2-b]哒嗪衍生物及其作为PDE10抑制剂的用途
公开(公告)号：EP2493889B1
公开(公告)日：2017-09-06
申请号：EP10768978.8
申请日：2010-10-27
发明人： PASTOR-FERNÁNDEZ, Joaquin , BARTOLOMÉ-NEBREDA, José, Manuel , MACDONALD, Gregor, James , CONDE-CEIDE, Susana , DELGADO-GONZÁLEZ, Óscar , VANHOOF, Greta, Constantia, Peter , VAN GOOL, Michiel, Luc, Maria , MARTÍN-MARTÍN, María, Luz , ALONSO-DE DIEGO, Sergio-Alvar , SWINNEY, Kelly, Ann , LEYS, Carina , WEERTS, Johan, Erwin, Edmond
IPC分类号： C07D487/04 , A61K31/5025 , A61P3/00 , A61P25/00
CPC分类号： C07D487/04
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公开(公告)号：EP2513118A1
公开(公告)日：2012-10-24
申请号：EP10790989.7
申请日：2010-12-16
发明人： MACDONALD, Gregor, James , TRESADERN, Gary, John , TRABANCO-SUÁREZ, Andrés, Avelino , PASTOR-FERNÁNDEZ, Joaquin
IPC分类号： C07D513/04 , A61K31/428 , A61K31/429 , A61P25/18
CPC分类号： C07D277/60 , A61K31/4365 , C07D417/04 , C07D417/06 , C07D417/12 , C07D513/04
摘要： The present invention relates to novel bicyclic thiazoles of formula (I) 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.
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公开(公告)号：EP2513117A1
公开(公告)日：2012-10-24
申请号：EP10790574.7
申请日：2010-12-16
发明人： MACDONALD, Gregor, James , TRABANCO-SUÁREZ, Andrés, Avelino , CONDE-CEIDE, Susana , TRESADERN, Gary, John , BARTOLOMÉ-NEBREDA, José, Manuel , PASTOR-FERNÁNDEZ, Joaquin
IPC分类号： C07D513/04 , A61K31/428 , A61K31/429 , A61P25/18
CPC分类号： C07D513/04 , A61K31/4365
摘要： The present invention relates to novel bicyclic thiazoles of formula (I) 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.
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公开(公告)号：EP2513117B1
公开(公告)日：2013-08-28
申请号：EP10790574.7
申请日：2010-12-16
发明人： MACDONALD, Gregor, James , TRABANCO-SUÁREZ, Andrés, Avelino , CONDE-CEIDE, Susana , TRESADERN, Gary, John , BARTOLOMÉ-NEBREDA, José, Manuel , PASTOR-FERNÁNDEZ, Joaquin
IPC分类号： C07D513/04 , A61K31/428 , A61K31/429 , A61P25/18
CPC分类号： C07D513/04 , A61K31/4365
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