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公开(公告)号：EP3353163A1
公开(公告)日：2018-08-01
申请号：EP16770283.6
申请日：2016-09-23
发明人： ROMBOUTS, Frederik, Jan, Rita , GIJSEN, Henricus, Jacobus, Maria , VAN BRANDT, Sven, Franciscus, Anna , TRABANCO-SUÁREZ, Andrés, Avelino
IPC分类号： C07D401/12 , A61K31/4418 , A61P25/16 , 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, or dementia associated with beta-amyloid.
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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
公开(公告)号：EP2788346B1
公开(公告)日：2015-10-28
申请号：EP12794731.5
申请日：2012-12-04
发明人： TRABANCO-SUÁREZ, Andrés, Avelino , GIJSEN, Henricus, Jacobus, Maria , SURKYN, Michel , PROKOPCOVÁ, Hana
IPC分类号： C07D413/10 , C07D413/12 , A61K31/5377 , A61P25/16 , A61P25/28
CPC分类号： C07D413/12 , C07D413/10
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4.发明公开1-ARYL-4-METHYL-[1,2,4]TRIAZOLO[4,3-a]QUINOXALINE DERIVATIVES 有权1-芳基-4-甲基 - [1,2,4]三唑并[4,3-A] -CHINOXALIN衍
公开(公告)号：EP2723744A1
公开(公告)日：2014-04-30
申请号：EP12729637.4
申请日：2012-06-26
发明人： ANDRÉS-GIL, José, Ignacio , ROMBOUTS, Frederik, Jan, Rita , TRABANCO-SUÁREZ, Andrés, Avelino , VANHOOF, Greta, Constantia, Peter , DE ANGELIS, Meri , BUIJNSTERS, Peter, Jacobus, Johannes, Antonius , GUILLEMONT, Jerôme, Emile, Georges , BORMANS, Guy, Maurits R. , CELEN, Sofie, Jeanne, Leopoldine , VLIEGEN, Maarten
IPC分类号： C07D487/04 , A61K31/4985 , A61P25/00
CPC分类号： C07D487/04 , A61K31/4985 , A61K45/06 , A61K51/0463 , G01N33/60
摘要： The present invention relates to novel l-aryl-4-methyl-[l,2,4]triazolo[4,3-a]- quinoxaline derivatives as inhibitors of phosphodiesterase 2 (PDE2) and to a lesser extent of phosphodiesterase 10 (PDE10) or as inhibitors of both, phosphodiesterases 2 and 10. 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 PDE2 is involved, or disorders in which both PDE2 and PDE10 are involved, such as neurological and psychiatric disorders, and endocrinological or metabolic diseases. The present invention also relates to radiolabeled compounds which may be useful for imaging and quantifying the PDE2 enzyme in tissues, using positron- emission tomography (PET). The invention is also directed to compositions comprising such compounds, to processes for preparing such compounds and compositions, to the use of such compounds and compositions for imaging a tissue, cells or a host, in vitro or in vivo and to precursors of said compounds.
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公开(公告)号：EP3353163B1
公开(公告)日：2020-02-05
申请号：EP16770283.6
申请日：2016-09-23
发明人： ROMBOUTS, Frederik, Jan, Rita , GIJSEN, Henricus, Jacobus, Maria , VAN BRANDT, Sven, Franciscus, Anna , TRABANCO-SUÁREZ, Andrés, Avelino
IPC分类号： C07D401/12 , A61K31/4418 , A61P25/16 , A61P25/28
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6.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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7.发明公开1,2,4-TRIAZOLO[4,3-a]PYRIDINE COMPOUNDS AND THEIR USE AS POSITIVE ALLOSTERIC MODULATORS OF MGLUR2 RECEPTORS 有权1,2,4-TRIAZOLO [4,3-A] PYRIDINVERBINDUNGEN UND DEREN VERWENDUNG ALS POSISTIVE ALLOSTERISCHE MODULATOREN DER MGLUR2 -REZEPTOREN
公开(公告)号：EP3041839A1
公开(公告)日：2016-07-13
申请号：EP14758564.0
申请日：2014-09-03
发明人： CID-NÚÑEZ, José, Maria , TRABANCO-SUÁREZ, Andrés, Avelino , LAVREYSEN, Hilde , CEUSTERS, Marc André
IPC分类号： C07D471/04 , A61K31/437
CPC分类号： C07D471/04 , A61K31/198 , A61K31/437
摘要： The present invention relates to novel 1,2,4-triazolo[4,3-a]pyridine compounds of Formula (I) as positive allosteric modulators (PAMs) 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 mGluR2 subtype disorders.
摘要翻译： 本发明涉及作为代谢型谷氨酸受体亚型2（“mGluR2”）的正变构调节剂（PAM）的新型1,2,4-三唑并[4,3-a]吡啶化合物。 本发明还涉及包含这些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3,4-DIHYDRO-PYRROLO[1,2-a]PYRAZIN-1-YLAMINE DERIVATIVES USEFUL AS INHIBITORS OF BETA-SECRETASE (BACE) 有权3,4-二氢吡咯并[1,2-a]吡嗪-1-基 - 胺衍生物作为β-分泌酶抑制剂（BACE）
公开(公告)号：EP2683721A1
公开(公告)日：2014-01-15
申请号：EP12707319.5
申请日：2012-03-07
IPC分类号： C07D487/04 , A61K31/4985 , A61K31/506 , A61P25/28
CPC分类号： C07D487/04
摘要： The present invention relates to novel 3,4-dihydro-pyrrolo[l,2-a]pyrazin-1-ylamine derivatives as inhibitors of beta-secretase, also known as beta-site amyloid cleaving enzyme, BACE, BACE1, Asp2, or memapsin2. 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 or dementia associated with beta-amyloid.
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9.发明公开6,7-DIHYDRO-PYRAZOLO[1,5-A]PYRAZIN-4-YLAMINE DERIVATIVES USEFUL AS INHIBITORS OF BETA-SECRETASE (BACE) 有权6,7-二氢吡唑并[1,5A-]吡嗪-4-基 - AMIN衍生物作为抑制剂的β-分泌酶（BACE）有用的
公开(公告)号：EP2681219A1
公开(公告)日：2014-01-08
申请号：EP12707276.7
申请日：2012-02-29
发明人： TRABANCO-SUÁREZ, Andrés, Avelino , GIJSEN, Henricus, Jacobus, Maria , VAN GOOL, Michiel, Luc, Maria , VEGA RAMIRO, Juan, Antonio , DELGADO-JIMÉNEZ, Francisca
IPC分类号： C07D487/04 , A61K31/4985 , A61P25/28
CPC分类号： C07D487/04
摘要： The present invention relates to novel 6,7-dihydro-pyrazolo[1,5-a]pyrazin-4-yl-amine derivatives as inhibitors of beta-secretase, also known as beta-site amyloid cleaving enzyme, BACE, BACEl, Asp2, or memapsin2. 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 or dementia associated with beta-amyloid.
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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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