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1.发明公开6,7-DIHYDROPYRAZOLO[1,5-A]PYRAZIN-4(5H)-ONE COMPOUNDS AND THEIR USE AS NEGATIVE ALLOSTERIC MODULATORS OF MGLUR2 RECEPTORS 审中-公开6,7-二氢吡唑并[1,5-a]吡嗪-4（5H） - 酮化合物及其作为受体的mGluR2的负变构调节剂的用途
公开(公告)号：EP3174880A1
公开(公告)日：2017-06-07
申请号：EP15742317.9
申请日：2015-07-30
发明人： ANDRÉS-GIL, José Ignacio , VAN GOOL, Michiel Luc Maria , TRABANCO-SUÁREZ, Andrés Avelino , DE LUCAS OLIVARES, Ana Isabel , ALONSO-DE DIEGO, Sergio-Alvar , DELGADO-GONZÁLEZ, Óscar
IPC分类号： C07D487/04 , A61K31/4985 , A61P25/00
CPC分类号： C07D487/04 , A61P25/18 , A61P25/26
摘要： The present invention relates to novel 6,7-dihydropyrazolo[1,5-a]pyrazin-4(5H)-one derivatives as negative allosteric modulators (NAMs) of the metabotropic glutamate receptor subtype 2 (“mGluR2”). 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 or treatment of disorders in which the mGluR2 subtype of metabotropic receptors is involved.
摘要翻译： 本发明涉及代谢型谷氨酸受体亚型2（“mGluR2的”）的新颖的6,7-二氢吡唑并[1,5-a]吡嗪-4（5H） - 酮衍生物作为负变构调节剂（NAM）。 因此，本发明涉及药物组合物，其包括测试的化合物，以用于制备测试和组合物的化合物，并涉及用于疾病的预防或治疗其中代谢型受体的mGluR2的亚型参与测试的化合物和组合物。
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2.发明授权6,7-DIHYDROPYRAZOLO[1,5-A]PYRAZIN-4(5H)-ONE COMPOUNDS AND THEIR USE AS NEGATIVE ALLOSTERIC MODULATORS OF MGLUR2 RECEPTORS 有权6,7-二氢吡唑并[1,5-a]吡嗪-4（5H） - 酮化合物及其作为受体的mGluR2的负变构调节剂的用途
公开(公告)号：EP3004107B1
公开(公告)日：2017-05-10
申请号：EP14727824.6
申请日：2014-06-03
发明人： VAN GOOL, Michiel, Luc, Maria , ALONSO-DE DIEGO, Sergio-Alvar , CID-NÚÑEZ, José, Maria , DELGADO-GONZÁLEZ, Óscar , DECORTE, Annelies, Marie, Antonius , MACDONALD, Gregor, James , MEGENS, Antonius, Adrianus, Hendrikus, Petrus , TRABANCO-SUÁREZ, Andrés, Avelino , GARCÍA-MOLINA, Aránzazu , ANDRÉS-GIL, José, Ignacio
IPC分类号： C07D487/04 , A61K31/4985 , A61P25/00
CPC分类号： C07D487/04
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3.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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4.发明公开2,3,4,5-TETRAHYDROPYRIDIN-6-AMINE AND 3,4-DIHYDRO-2H-PYRROL-5-AMINE COMPOUND INHIBITORS OF BETA-SECRETASE 审中-公开β-分泌酶的2,3,4,5-四氢吡啶-6-胺和3,4-二氢-2H-吡咯-5-胺化合物抑制剂
公开(公告)号：EP3233834A1
公开(公告)日：2017-10-25
申请号：EP15820456.0
申请日：2015-12-16
发明人： TRABANCO-SUÁREZ, Andrés, Avelino , DELGADO-GONZÁLEZ, Óscar , GIJSEN, Henricus, Jacobus, Maria , VAN GOOL, Michiel, Luc, Maria , VAN BRANDT, Sven, Franciscus, Anna , DE CLEYN, Michel, Anna, Jozef , FUSTERO LARDIÉS, Santos , MATEU SANCHÍS, Natalia
IPC分类号： C07D403/12 , C07D401/10 , C07D401/12 , C07D403/10 , C07D413/12 , A61K31/506 , A61P25/28
摘要： wherein the radicals are as defined in the specification. 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 beta-secretase is involved, such as Alzheimer's disease (AD), mild cognitive impairment, senility, dementia, dementia with Lewy bodies, Down's syndrome, dementia associated with stroke, dementia associated with Parkinson's disease, dementia associated with beta-amyloid, age-related macular degeneration, type 2 diabetes or metabolic disorders.
摘要翻译： 本发明涉及具有式（I）所示结构的β-分泌酶的2,3,4,5-四氢吡啶-6-胺和3,4-二氢-2H-吡咯-5-胺化合物抑制剂，其中 基团如说明书中所定义。 本发明还涉及包含此类化合物的药物组合物，涉及用于制备此类化合物和组合物的方法，并且涉及此类化合物和组合物用于预防和治疗涉及β-分泌酶的疾病如阿尔茨海默病（ AD），轻度认知障碍，衰老，痴呆，路易体痴呆，唐氏综合症，与中风相关的痴呆，与帕金森病相关的痴呆，与β-淀粉样蛋白相关的痴呆，年龄相关性黄斑变性，2型糖尿病或代谢紊乱。
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5.发明公开IMIDAZO[1,2-b]PYRIDAZINE DERIVATIVES AND THEIR USE AS PDE10 INHIBITORS 有权咪唑并[1,2-B]吡啶并[DEREN] DEREN VERWENDUNG ALS PDE10-INHIBITOREN
公开(公告)号：EP2493889A1
公开(公告)日：2012-09-05
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
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，其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。
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6.发明公开6,7-DIHYDROPYRAZOLO[1,5-a]PYRAZIN-4(5H)-ONE COMPOUNDS AND THEIR USE AS NEGATIVE ALLOSTERIC MODULATORS OF MGLUR2 RECEPTORS 审中-公开6,7-二氢吡唑并[1,5-a]吡嗪-4（5H）酮化合物及其作为MGLur2受体的阴性调节剂的用途
公开(公告)号：EP3177623A1
公开(公告)日：2017-06-14
申请号：EP15750666.8
申请日：2015-07-30
发明人： ALONSO-DE DIEGO, Sergio-Alvar , VAN GOOL, Michiel Luc Maria , DELGADO-GONZÁLEZ, Óscar , ANDRÉS-GIL, José Ignacio , TRABANCO-SUÁREZ, Andrés Avelino
IPC分类号： C07D487/04 , A61K31/4985 , A61P25/00
CPC分类号： C07D487/04 , A61K31/4985 , A61K31/506
摘要： The present invention relates to novel 6,7-dihydropyrazolo[1,5-a]pyrazin-4(5H)-one derivatives as negative allosteric modulators (NAMs) of the metabotropic glutamate receptor subtype 2 (“mGluR2”). 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 or treatment of disorders in which the mGluR2 subtype of metabotropic receptors is involved.
摘要翻译： 本发明涉及作为代谢型谷氨酸受体亚型2（“mGluR2”）的负变构调节剂（NAM）的新型6,7-二氢吡唑并[1,5-a]吡嗪-4（5H） - 酮衍生物。 本发明还涉及包含此类化合物的药物组合物，涉及制备此类化合物和组合物的方法，以及涉及这些化合物和组合物用于预防或治疗涉及代谢型受体的mGluR2亚型的疾病的用途。
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7.发明公开6,7-DIHYDROPYRAZOLO[1,5-A]PYRAZIN-4(5H)-ONE COMPOUNDS AND THEIR USE AS NEGATIVE ALLOSTERIC MODULATORS OF MGLUR2 RECEPTORS 审中-公开6,7-二氢吡唑并[1,5-A]吡嗪-4（5H）酮化合物及其作为MGLur2受体的阴性调节剂的用途
公开(公告)号：EP3174883A1
公开(公告)日：2017-06-07
申请号：EP15744915.8
申请日：2015-07-30
发明人： ALONSO-DE DIEGO, Sergio-Alvar , VAN GOOL, Michiel Luc Maria , MARTÍN-MARTÍN, María Luz , CONDE-CEIDE, Susana , ANDRÉS-GIL, José Ignacio , DELGADO-GONZÁLEZ, Óscar , TRESADERN, Gary John , TRABANCO-SUÁREZ, Andrés Avelino
IPC分类号： C07D487/04 , A61K31/4985 , A61P25/00
CPC分类号： C07D487/04 , A61K9/0019 , A61K9/06 , A61K9/10 , A61K9/20 , A61K31/4985 , A61K31/501 , A61K31/506
摘要： The present invention relates to novel 6,7-dihydropyrazolo[1,5-a]pyrazin-4(5H)-one derivatives as negative allosteric modulators (NAMs) of the metabotropic glutamate receptor subtype 2 (“mGluR2”). 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 or treatment of disorders in which the mGluR2 subtype of metabotropic receptors is involved.
摘要翻译： 本发明涉及作为代谢型谷氨酸受体亚型2（“mGluR2”）的负变构调节剂（NAM）的新型6,7-二氢吡唑并[1,5-a]吡嗪-4（5H） - 酮衍生物。 本发明还涉及包含此类化合物的药物组合物，涉及制备此类化合物和组合物的方法，以及涉及这些化合物和组合物用于预防或治疗涉及代谢型受体的mGluR2亚型的疾病的用途。
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8.发明公开6,7-DIHYDROPYRAZOLO[1,5-a]PYRAZIN-4(5H)-ONE COMPOUNDS AND THEIR USE AS NEGATIVE ALLOSTERIC MODULATORS OF MGLUR2 RECEPTORS 有权6,7-二氢吡唑并[1,5-a]吡嗪-4（5H） - 酮化合物及其作为受体的mGluR2的负变构调节剂的用途
公开(公告)号：EP3004107A1
公开(公告)日：2016-04-13
申请号：EP14727824.6
申请日：2014-06-03
发明人： VAN GOOL, Michiel, Luc, Maria , ALONSO-DE DIEGO, Sergio-Alvar , CID-NÚÑEZ, José, Maria , DELGADO-GONZÁLEZ, Óscar , DECORTE, Annelies, Marie, Antonius , MACDONALD, Gregor, James , MEGENS, Antonius, Adrianus, Hendrikus, Petrus , TRABANCO-SUÁREZ, Andrés, Avelino , GARCÍA-MOLINA, Aránzazu , ANDRÉS-GIL, José, Ignacio
IPC分类号： C07D487/04 , A61K31/4985 , A61P25/00
CPC分类号： C07D487/04
摘要： The present invention relates to novel 6,7-dihydropyrazolo[1,5-a]pyrazin-4(5H)-one derivatives of Formula (I) as negative allosteric modulators (NAMs) of the metabotropic glutamate receptor subtype 2 ("mGluR2"). 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 or treatment of disorders in which the mGluR2 subtype of metabotropic receptors is involved, especially CNS disorders.
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