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1. 发明公开

EP3353163A1 2,3,4,5-TETRAHYDROPYRIDIN-6-AMINE DERIVATIVES 审中-公开
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
申请人： Janssen Pharmaceutica, N.V.
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.

2. 发明授权

EP2788346B1 6-DIFLUOROMETHYL-5,6-DIHYDRO-2H-[1,4]OXAZIN-3-AMINE DERIVATIVES 有权
标题翻译： 6-二氟甲基-5,6-二氢-2H- [1,4]恶嗪-3-胺衍生物
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
申请人： Janssen Pharmaceutica, N.V.
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

3. 发明公开

EP2788335A1 5-(3-AMINOPHENYL)-5-ALKYL-5,6-DIHYDRO-2H-[1,4]OXAZIN-3-AMINE DERIVATIVES 有权
标题翻译： 5-（3-氨基苯基）-5-烷基-5,6-二氢-2H- [1,4]恶嗪-3-胺衍生物对病症的治疗β-分泌酶涉及
公开(公告)号：EP2788335A1
公开(公告)日：2014-10-15
申请号：EP12794730.7
申请日：2012-12-04
申请人： Janssen Pharmaceutica, N.V.
发明人： GIJSEN, Henricus, Jacobus, Maria , VAN BRANDT, Sven, Franciscus, Anna
IPC分类号： C07D265/30 , C07D413/12 , A61K31/5377 , A61P25/00
CPC分类号： C07D413/12 , C07D265/30
摘要： The present invention relates to novel 5-(3-aminophenyl)-5-alkyl-5,6-dihydro- 2
H -[1,4]oxazin-3-amine derivatives as inhibitors of beta-secretase, also known as beta- site amyloid cleaving enzyme, BACE, BACE 1, 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, cerebral amyloid angiopathy, multi-infarct dementia, Down's syndrome, dementia associated with stroke, dementia associated with Parkinson's disease and dementia associated with beta-amyloid. (Formula I)

4. 发明公开

EP2234984A1 FLUOROALKYL SUBSTITUTED BENZIMIDAZOLE CANNABINOID AGONISTS 有权
标题翻译：氟烷基的苯并咪唑作为大麻素受体激动剂
公开(公告)号：EP2234984A1
公开(公告)日：2010-10-06
申请号：EP08862464.8
申请日：2008-12-16
申请人： Janssen Pharmaceutica, N.V.
发明人： GIJSEN, Henricus, Jacobus, Maria , VERBIST, Bie, Maria, Pieter , SURKYN, Michel
IPC分类号： C07D235/08 , C07D401/12 , C07D403/12 , A61K31/4184
CPC分类号： C07D235/08 , C07D401/12 , C07D403/12
摘要： The present invention is related to benzimidazole compounds of formula (I) having cannabinoid receptor agonistic properties, pharmaceutical compositions comprising these compounds, chemical processes for preparing these compounds and their use in the treatment of diseases linked to the mediation of the cannabinoid receptors in animals, in particular humans.

5. 发明公开

EP3008067A1 4-AMINO-6-PHENYL-5,6-DIHYDROIMIDAZO[1,5-A]PYRAZIN-3(2H)-ONE DERIVATIVES AS INHIBITORS OF BETA-SECRETASE (BACE) 有权
标题翻译： 4-氨基-6-苯基-5,6-二氢吲哚并[1,5-a]吡嗪-3（2H） - 衍生物ALS抑制剂β-谷维素（BACE）
公开(公告)号：EP3008067A1
公开(公告)日：2016-04-20
申请号：EP14732131.9
申请日：2014-06-12
申请人： Janssen Pharmaceutica N.V.
发明人： OEHLRICH, Daniel , GIJSEN, Henricus, Jacobus, Maria
IPC分类号： C07D487/04 , A61K31/4985 , A61P25/28
CPC分类号： C07D487/04
摘要： The present invention relates to novel 5,6-dihydroimidazo[1,5-a]pyrazin-3(2
H )-one derivatives as inhibitors of beta-secretase, also known as beta-site amyloid cleaving enzyme, BACE, in particular BACE1 and/or BACE2 (wherein BACE1, is also known as Asp2, or memapsin2 and BACE2 is also known as Asp1, Memapsin 1 or DRAP). 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 of the Alzheimer's type, dementia associated with beta-amyloid, age-related macular degeneration, type 2 diabetes and other metabolic disorders.
摘要翻译：本发明涉及作为β-分泌酶抑制剂的新的5,6-二氢咪唑并[1,5-a]吡嗪-3（2H） - 酮衍生物，也称为β位点淀粉样蛋白切割酶BACE，特别是BACE1和 /或BACE2（其中BACE1，也称为Asp2或memapsin2，BACE2也称为Asp1，Memapsin 1或DRAP）。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，以及这些化合物和组合物用于预防和治疗其中涉及β-分泌酶的疾病如阿尔茨海默氏病的用途（ AD），轻度认知障碍，衰老，痴呆，路易体痴呆，唐氏综合征，与中风相关的痴呆，与帕金森病相关的痴呆，阿尔茨海默氏型痴呆，与β-淀粉样变性相关的痴呆，年龄相关性黄斑变性，类型 2型糖尿病等代谢紊乱。

6. 发明授权

EP2788335B1 5-(3-AMINOPHENYL)-5-ALKYL-5,6-DIHYDRO-2H-[1,4]OXAZIN-3-AMINE DERIVATIVES FOR THE TREATMENT OF DISORDERS IN WHICH BETA-SECRETASE IS INVOLVED 有权
标题翻译： 5-（3-氨基苯基）-5-烷基-5,6-二氢-2H- [1,4]恶嗪-3-胺衍生物对病症的治疗β-分泌酶涉及
公开(公告)号：EP2788335B1
公开(公告)日：2016-04-13
申请号：EP12794730.7
申请日：2012-12-04
申请人： Janssen Pharmaceutica, N.V.
发明人： GIJSEN, Henricus, Jacobus, Maria , VAN BRANDT, Sven, Franciscus, Anna
IPC分类号： C07D265/30 , C07D413/12 , A61K31/5377 , A61P25/00
CPC分类号： C07D413/12 , C07D265/30

7. 发明授权

EP2234984B1 FLUOROALKYL SUBSTITUTED BENZIMIDAZOLE CANNABINOID AGONISTS 有权
标题翻译：氟烷基的苯并咪唑作为大麻素受体激动剂
公开(公告)号：EP2234984B1
公开(公告)日：2016-03-16
申请号：EP08862464.8
申请日：2008-12-16
申请人： Janssen Pharmaceutica, N.V.
发明人： GIJSEN, Henricus, Jacobus, Maria , VERBIST, Bie, Maria, Pieter , SURKYN, Michel
IPC分类号： C07D235/08 , C07D401/12 , C07D403/12 , A61K31/4184
CPC分类号： C07D235/08 , C07D401/12 , C07D403/12

8. 发明公开

EP1641782A1 HYDROXYCARBONYLPHENYL SUBSTITUTED 4-(AMINOMETHYL)-PIPERIDINE BENZAMIDES AS 5HT4-ANTAGONISTS 有权
标题翻译：羟基羰基苯基取代的4-（氨基甲基）-PIPERIDINBENZAMIDE AS 5HT4拮抗剂
公开(公告)号：EP1641782A1
公开(公告)日：2006-04-05
申请号：EP04739777.3
申请日：2004-06-10
申请人： JANSSEN PHARMACEUTICA N.V.
发明人： BOSMANS, Jean-Paul, René, Marie, André , GIJSEN, Henricus, Jacobus, Maria , MEVELLEC, Laurence, Anne Janssen-Cilag
IPC分类号： C07D405/12 , A61P1/00
CPC分类号： C07D405/12
摘要： The present invention is concerned with novel compounds of formula (I) having 5HT4-antagonistic properties. The invention further relates to methods for preparing such novel compounds, pharmaceutical compositions comprising said novel compounds as well as the use as a medicine of said compounds.

9. 发明授权

EP3008067B1 4-AMINO-6-PHENYL-5,6-DIHYDROIMIDAZO[1,5-A]PYRAZIN-3(2H)-ONE DERIVATIVES AS INHIBITORS OF BETA-SECRETASE (BACE) 有权
标题翻译： 4-氨基-6-苯基-5,6-二氢咪唑并[1,5-a]吡嗪-3（2H） - 酮衍生物以β-分泌酶的抑制剂（BACE）
公开(公告)号：EP3008067B1
公开(公告)日：2017-03-29
申请号：EP14732131.9
申请日：2014-06-12
申请人： Janssen Pharmaceutica N.V.
发明人： OEHLRICH, Daniel , GIJSEN, Henricus, Jacobus, Maria
IPC分类号： C07D487/04 , A61K31/4985 , A61P25/28
CPC分类号： C07D487/04

10. 发明授权

EP2580200B1 5,6-DIHYDRO-2H-[1,4]OXAZIN-3-YL-AMINE DERIVATIVES USEFUL AS INHIBITORS OF BETA-SECRETASE (BACE) 有权
标题翻译： 5,6-二氢-2H- [1,4]恶嗪-3-基 - 胺衍生物作为β-分泌酶抑制剂（BACE）
公开(公告)号：EP2580200B1
公开(公告)日：2016-09-14
申请号：EP11723974.9
申请日：2011-06-08
申请人： Janssen Pharmaceutica, N.V.
发明人： TRABANCO-SUÁREZ, Andrés, Avelino , ROMBOUTS, Frederik, Jan, Rita , TRESADERN, Gary, John , VAN GOOL, Michiel, Luc, Maria , MACDONALD, Gregor, James , MARTINEZ LAMENCA, Carolina , GIJSEN, Henricus, Jacobus, Maria
IPC分类号： C07D265/30 , C07D413/04 , A61K31/535 , A61K31/5355 , A61P25/28 , A61P25/16
CPC分类号： C07D265/30 , C07D413/04 , C07D413/10

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