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1. 发明申请

WO2018083247A1 4,4A,5,7-TETRAHYDRO-3H-FURO[3,4-B]PYRIDINYL COMPOUNDS 审中-公开
标题翻译： 4,4A，5,7-四氢-3H-呋喃并[3,4-B]吡啶基化合物
公开(公告)号：WO2018083247A1
公开(公告)日：2018-05-11
申请号：PCT/EP2017/078200
申请日：2017-11-03
申请人： JANSSEN PHARMACEUTICA NV
发明人： VAN BRANDT, Sven, Franciscus, Anna , GIJSEN, Henricus, Jacobus, Maria , ROMBOUTS, Frederik, Jan, Rita
IPC分类号： C07D491/048 , A61K31/4355 , A61P25/28
摘要： The present invention relates to 4,4a,5,7-tetrahydro-3H-furo[3,4-b]pyridinyl compound inhibitors of beta-site APP-cleaving enzyme having the structure shown in Formula (I) 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-site APP- cleaving enzyme is involved, such as Alzheimer's disease (AD), mild cognitive impairment, preclinical Alzheimer's disease, senility, dementia, dementia with Lewy bodies, Down's syndrome, dementia associated with stroke, dementia associated with Parkinson's disease, and dementia associated with beta-amyloid.
摘要翻译：本发明涉及具有式（I）所示结构的β位APP剪切酶的4,4a，5,7-四氢-3H-呋喃并[3,4-b]吡啶基化合物抑制剂。（I）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其中涉及β位APP裂解酶的疾病的用途，例如阿尔茨海默病（AD），轻度认知障碍，临床前阿尔茨海默氏病，衰老，痴呆，路易体痴呆，唐氏综合症，与中风相关的痴呆，与帕金森氏病有关的痴呆和与β-淀粉样蛋白相关的痴呆。

2. 发明申请

WO2014198851A1 4-AMINO-6-PHENYL-5,6-DIHYDROIMIDAZO[1,5-A]PYRAZIN-3(2H)-ONE DERIVATIVES AS INHIBITORS OF BETA-SECRETASE (BACE) 审中-公开
标题翻译：作为β-分泌酶（BACE）的抑制剂的4-氨基-6-苯基-5,6-二氢吲哚并[1,5-a]吡嗪-3（2H） - 酮衍生物
公开(公告)号：WO2014198851A1
公开(公告)日：2014-12-18
申请号：PCT/EP2014/062283
申请日：2014-06-12
申请人： JANSSEN PHARMACEUTICA NV
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：本发明涉及新的5,6-二氢咪唑并[1,5-a]吡嗪-3（2H） - 酮衍生物作为β-分泌酶的抑制剂，也称为β-位淀粉样蛋白切割酶BACE，特别是BACE1和 /或BACE2（其中BACE1，也称为Asp2，或memapsin2和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病的用途（例如， 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 2型糖尿病等代谢紊乱。

3. 发明申请

WO2017050978A1 2,3,4,5-TETRAHYDROPYRIDIN-6-AMINE DERIVATIVES 审中-公开
标题翻译： 2,3,4,5-四氢吡啶-6-胺衍生物
公开(公告)号：WO2017050978A1
公开(公告)日：2017-03-30
申请号：PCT/EP2016/072710
申请日：2016-09-23
申请人： JANSSEN PHARMACEUTICA NV
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
CPC分类号： C07D401/12
摘要： The present invention relates to 2,3,4,5-tetrahydropyridin-6-amine compound inhibitors of beta-secretase having the structure shown in Formula (I) 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.
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病的用途（例如， 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或与β-淀粉样蛋白相关的痴呆。

4. 发明申请

WO2014096212A1 NOVEL TRICYCLIC 3,4-DIHYDRO-2H-PYRIDO[1,2-α]PYRAZINE-1,6-DIONE DERIVATIVES AS GAMMA SECRETASE MODULATORS 审中-公开
标题翻译：作为GAMMA分泌酶调节剂的新型三环3,4-二氢-2H-吡啶并[1,2-α]吡嗪-1,6-二酮衍生物
公开(公告)号：WO2014096212A1
公开(公告)日：2014-06-26
申请号：PCT/EP2013/077425
申请日：2013-12-19
申请人： JANSSEN PHARMACEUTICA NV
发明人： BISCHOFF, François, Paul , GIJSEN, Henricus, Jacobus, Maria , VAN DEN KEYBUS, Frans, Alfons, Maria , ROMBOUTS, Frederik, Jan, Rita
IPC分类号： C07D471/14 , A61K31/4985 , A61P25/28
CPC分类号： C07D471/14
摘要： The present invention is concerned with novel tricyclic 3,4-dihydro-2H-pyrido[l,2-a]pyrazine-l,6-dione derivatives of Formula (I) wherein R 1 , R 2 , R 3 , R 4 , L, Y, Z and X 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 for the treatment of i.a. Alzheimer's disease.
摘要翻译：本发明涉及式（I）的新型三环3,4-二氢-2H-吡啶并[1,2-a]吡嗪-1,6-二酮衍生物，其中R1，R2，R3，R4，L，Y， Z和X具有权利要求中限定的含义。根据本发明的化合物可用作γ-分泌酶调节剂。本发明进一步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治疗药物的用途。阿尔茨海默氏病。

5. 发明申请

WO2011154431A1 5,6-DIHYDRO-2H-[1,4]OXAZIN-3-YL-AMINE DERIVATIVES USEFUL AS INHIBITORS OF BETA-SECRETASE (BACE) 审中-公开
标题翻译：作为β-分泌酶（BACE）的抑制剂有用的5,6-二氢-2H- [1,4]氧杂-3-氨基胺衍生物
公开(公告)号：WO2011154431A1
公开(公告)日：2011-12-15
申请号：PCT/EP2011/059441
申请日：2011-06-08
申请人： JANSSEN PHARMACEUTICA NV , 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
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
摘要： The present invention relates to novel 5,6-dihydro-2H-[1,4]oxazin-3-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 and dementia associated with beta- amyloid.
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-2H- [1,4]恶嗪-3-基胺衍生物，也称为β位点淀粉样蛋白切割酶，BACE，BACE1，Asp2或memapsin2 。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病的用途（例如， 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和与β-淀粉样蛋白相关的痴呆。

6. 发明申请

WO2018083101A1 [1,2,4]TRIAZOLO[1,5-A]PYRIMIDINE COMPOUNDS AS PDE2 INHIBITORS 审中-公开
标题翻译： [1,2,4] TRIAZOLO [1,5-A]嘧啶化合物作为PDE2抑制剂
公开(公告)号：WO2018083101A1
公开(公告)日：2018-05-11
申请号：PCT/EP2017/077918
申请日：2017-10-31
申请人： JANSSEN PHARMACEUTICA NV
发明人： VAN ROOSBROECK, Yves, Emiel, Maria , VAN DEN KEYBUS, Frans, Alfons, Maria , VELTER, Adriana, Ingrid , BUIJNSTERS, Peter, Jacobus, Johannes, Antonius , TRESADERN, Gary, John , GIJSEN, Henricus, Jacobus, Maria
IPC分类号： C07D487/04 , A61K31/519 , A61P25/00 , C07D451/02
摘要： The present invention relates to novel [1,2,4]triazolo[1,5-a]pyrimidin-yl derivatives as inhibitors of phosphodiesterase 2 (PDE2). The invention is also directed to pharmaceutical compositions comprising the 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, such as neurological and psychiatric disorders.
摘要翻译：本发明涉及作为磷酸二酯酶2（PDE2）抑制剂的新型[1,2,4]三唑并[1,5-a]嘧啶 - 基衍生物。本发明还涉及包含所述化合物的药物组合物，涉及用于制备所述化合物和组合物的方法，并且涉及所述化合物和组合物用于预防和治疗其中涉及PDE2的疾病如神经和精神疾病的用途。

7. 发明申请

WO2014198853A1 4-AMINO-6-PHENYL-5,6-DIHYDROIMIDAZO[1,5-A]PYRAZINE DERIVATIVES AS INHIBITORS OF BETA-SECRETASE (BACE) 审中-公开
标题翻译：作为β-分泌酶（BACE）的抑制剂的4-氨基-6-苯基-5,6-二氢吲哚并[1,5-a]吡啶衍生物
公开(公告)号：WO2014198853A1
公开(公告)日：2014-12-18
申请号：PCT/EP2014/062285
申请日：2014-06-12
申请人： JANSSEN PHARMACEUTICA NV
发明人： OEHLRICH, Daniel , GIJSEN, Henricus, Jacobus, Maria , SURKYN, Michel
IPC分类号： C07D487/04 , A61K31/4985 , A61P25/28
CPC分类号： C07D487/04 , A61K31/4985
摘要： The present invention relates to novel 5,6-dihydroimidazo[1,5-a]pyrazinyl 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]吡嗪衍生物，也称为β-位淀粉样蛋白切割酶BACE，特别是BACE1和/或BACE2（其中BACE1，也称为Asp2，或memapsin2和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病的用途（例如， 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 2型糖尿病等代谢紊乱。

8. 发明申请

WO2014111457A1 NOVEL SUBSTITUTED PYRIDO-PIPERAZINONE DERIVATIVES AS GAMMA SECRETASE MODULATORS 审中-公开
标题翻译：作为GAMMA秘密调节剂的新型取代的吡咯并吡啶酮衍生物
公开(公告)号：WO2014111457A1
公开(公告)日：2014-07-24
申请号：PCT/EP2014/050787
申请日：2014-01-16
申请人： JANSSEN PHARMACEUTICA NV
发明人： BISCHOFF, François, Paul , VELTER, Adriana, Ingrid , ROMBOUTS, Frederik, Jan, Rita , DE CLEYN, Michel, Anna, Jozef , VAN BRANDT, Sven, Franciscus, Anna , GIJSEN, Henricus, Jacobus, Maria , ZAVATTARO, Chiara , VAN DEN KEYBUS, Frans, Alfons, Maria
IPC分类号： C07D471/04 , A61K31/498 , A61P25/28
CPC分类号： C07D471/04
摘要： The present invention is concerned with novel substituted pyrido-piperazinone derivatives of Formula (I) wherein R 1 , R 2 , R 3 , R 4 , R 5 , L, Z and X 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）的新的取代吡啶并哌嗪酮衍生物，其中R 1，R 2，R 3，R 4，R 5，L，Z和X具有权利要求中定义的含义。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。

9. 发明申请

WO2018162444A1 INHIBITORS OF BETA SECRETASE 审中-公开
公开(公告)号：WO2018162444A1
公开(公告)日：2018-09-13
申请号：PCT/EP2018/055402
申请日：2018-03-06
申请人： JANSSEN PHARMACEUTICA NV
发明人： VOS, Ann, Marleen , OEHLRICH, Daniel , GIJSEN, Henricus, Jacobus, Maria , WATTS, Karl, Shawn , BHAT, Sathesh, Pangala , BUIJNSTERS, Peter, Jacobus, Johannes, Antonius , VAN BRANDT, Sven, Franciscus, Anna , ALCÁZAR-VACA, Manuel, Jesús
IPC分类号： C07D513/04 , A61K31/542 , A61P25/28
摘要： The present invention relates to tricyclic inhibitors of beta-secretase having the structure shown in Formula (I) and (II) (I) and (II) and the tautomers and the stereoisomeric forms thereof, 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 and other metabolic disorders.

10. 发明申请

WO2018162443A1 INHIBITORS OF BETA SECRETASE 审中-公开
公开(公告)号：WO2018162443A1
公开(公告)日：2018-09-13
申请号：PCT/EP2018/055401
申请日：2018-03-06
申请人： JANSSEN PHARMACEUTICA NV
发明人： VOS, Ann, Marleen , OEHLRICH, Daniel , GIJSEN, Henricus, Jacobus, Maria , WATTS, Karl, Shawn , BHAT, Sathesh, Pangala , VAN DEN KEYBUS, Frans, Alfons, Maria
IPC分类号： C07D513/04 , C07D498/04 , A61K31/542 , A61P25/28
摘要： The present invention relates to tricyclic inhibitors of beta-secretase having the structure shown in Formula (I) and (II) and the tautomers and the stereoisomeric forms thereof, 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 and other metabolic disorders.

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