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公开(公告)号：US09067924B2
公开(公告)日：2015-06-30
申请号：US13405398
申请日：2012-02-27
申请人： Hans Hilpert , Mark Rogers-Evans , Didier Rombach
发明人： Hans Hilpert , Mark Rogers-Evans , Didier Rombach
IPC分类号： A61K31/554 , C07D417/10 , C07D513/04 , C07D417/12
CPC分类号： C07D417/12 , A61K31/554 , C07D513/04
摘要： The present invention relates to 1,4 Thiazepines/Sulfones of formula I having BACE1 and/or BACE2 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease and type 2 diabetes.
摘要翻译： 本发明涉及具有BACE1和/或BACE2抑制活性的式I的1,4噻嗪类/砜类，其制备方法，含有它们的药物组合物及其作为治疗活性物质的用途。 本发明的活性化合物可用于例如治疗和/或预防性治疗。 阿尔茨海默病和2型糖尿病。
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![NOVEL [1,2,3]TRIAZOLO[4,5-D]PYRIMIDINE DERIVATIVES](/abs-image/US/2014/09/25/US20140288046A1/abs.jpg.150x150.jpg)
公开(公告)号：US20140288046A1
公开(公告)日：2014-09-25
申请号：US14250781
申请日：2014-04-11
申请人： Jean-Michel Adam , Caterina Bissantz , Uwe Grether , Atsushi Kimbara , Matthias Nettekoven , Stephan Roever , Mark Rogers-Evans
发明人： Jean-Michel Adam , Caterina Bissantz , Uwe Grether , Atsushi Kimbara , Matthias Nettekoven , Stephan Roever , Mark Rogers-Evans
IPC分类号： C07D487/04 , C07D491/107
CPC分类号： C07D487/04 , A61K9/0019 , A61K9/2054 , A61K9/4866 , A61K31/519 , A61K47/10 , C07D491/107
摘要： The invention relates to a compound of formula (I) wherein A, R1 and R2 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.
摘要翻译： 本发明涉及式（I）化合物，其中A，R 1和R 2如在说明书和权利要求书中所定义。 式（I）化合物可以用作药物。
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公开(公告)号：US08748418B2
公开(公告)日：2014-06-10
申请号：US13415873
申请日：2012-03-09
申请人： Emanuele Gabellieri , Wolfgang Guba , Hans Hilpert , Harald Mauser , Alexander V. Mayweg , Mark Rogers-Evans , Didier Rombach , Andrew Thomas , Thomas Woltering , Wolfgang Wostl
发明人： Emanuele Gabellieri , Wolfgang Guba , Hans Hilpert , Harald Mauser , Alexander V. Mayweg , Mark Rogers-Evans , Didier Rombach , Andrew Thomas , Thomas Woltering , Wolfgang Wostl
IPC分类号： A61K31/553 , C07D413/02 , C07D267/10
CPC分类号： C07D267/10 , C07D413/12
摘要： The present invention relates to 1,4-Oxazepines of formula I having BACE1 and/or BACE2 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease and type 2 diabetes.
摘要翻译： 本发明涉及具有BACE1和/或BACE2抑制活性的式I的1,4-氧氮杂，其制备方法，含有它们的药物组合物及其作为治疗活性物质的用途。 本发明的活性化合物可用于例如治疗和/或预防性治疗。 阿尔茨海默病和2型糖尿病。
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公开(公告)号：US08207220B2
公开(公告)日：2012-06-26
申请号：US12958440
申请日：2010-12-02
IPC分类号： A61K31/38
CPC分类号： C07D413/12 , C07D403/12 , C07D413/14 , C07D417/12
摘要： The present invention is concerned with novel sulfonamides of formula I wherein R1, R2, Ar, Hetaryl, m and n are as described in the description and claims. The compounds are orexin receptor antagonists, useful in the treatment of disorders, in which orexin pathways are involved.
摘要翻译： 本发明涉及式I的新型磺酰胺，其中R 1，R 2，Ar，杂芳基，m和n如说明书和权利要求中所述。 这些化合物是食欲素受体拮抗剂，可用于治疗食欲素途径参与的病症。
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公开(公告)号：US08071622B2
公开(公告)日：2011-12-06
申请号：US11947146
申请日：2007-11-29
申请人： Caterina Bissantz , Christophe Grundschober , Raffaello Masciadri , Hasane Ratni , Mark Rogers-Evans , Patrick Schnider
发明人： Caterina Bissantz , Christophe Grundschober , Raffaello Masciadri , Hasane Ratni , Mark Rogers-Evans , Patrick Schnider
IPC分类号： A61K31/454 , C07D403/14
CPC分类号： C07D401/14 , C07D491/04
摘要： The present invention is concerned with novel indol-2-yl-carbonyl-piperidin-benzoimidazolon and indol-2-yl-carbonyl-piperidin-benzoxazolon derivatives as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use for the treatment of anxiety and depressive disorders and other diseases. In particular, the present invention concerns compounds of formula (I) wherein R1 to R11, X and Y are as defined in the specification.
摘要翻译： 本发明涉及新的吲哚-2-基 - 羰基 - 哌啶 - 苯并咪唑酮和吲哚-2-基 - 羰基 - 哌啶 - 苯并恶唑酮衍生物作为V1a受体拮抗剂，其制备方法，含有它们的药物组合物及其用于治疗 焦虑抑郁障碍等疾病。 特别地，本发明涉及其中R 1至R 11，X和Y如说明书中所定义的式（I）化合物。
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公开(公告)号：US20110144098A1
公开(公告)日：2011-06-16
申请号：US12958436
申请日：2010-12-02
IPC分类号： A61K31/5365 , C07D413/12 , A61K31/5355 , C07D413/14 , A61K31/537 , A61P3/10
CPC分类号： C07D413/12 , C07D265/08 , C07D417/12 , C07D495/04 , C07D498/04
摘要： This invention relates to 5,6-dihydro-4H-[1,3]oxazin-2-ylamine compounds of the formula wherein R1 to R5 are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds are BACE2 inhibitors and can be used as medicaments for the treatment or prevention of diseases such as diabetes.
摘要翻译： 本发明涉及下式的5,6-二氢-4H- [1,3]恶嗪-2-基胺化合物，其中R1至R5如说明书和权利要求书中所定义，以及其药学上可接受的盐。 这些化合物是BACE2抑制剂，可用作治疗或预防糖尿病等疾病的药物。
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公开(公告)号：US07803815B2
公开(公告)日：2010-09-28
申请号：US11490305
申请日：2006-07-20
申请人： Caterina Bissantz , Christophe Grundschober , Hasane Ratni , Mark Rogers-Evans , Patrick Schnider
发明人： Caterina Bissantz , Christophe Grundschober , Hasane Ratni , Mark Rogers-Evans , Patrick Schnider
IPC分类号： A61K31/454 , C07D403/14
CPC分类号： C07D401/14 , C07D413/14
摘要： The present invention relates to Indol-3-yl-carbonyl-piperidin-benzoimidazol derivatives which act as V1a receptor antagonists and which are represented by Formula I: wherein the residues R1 to R7 are as defined herein. The invention further relates to pharmaceutical compositions containing such compounds, their use in treating dysmenorrhea, hypertension, chronic heart failure, inappropriate secretion of vasopressin, liver cirrhosis, nephritic syndrome, obsessive compulsive disorder, anxiety and depressive disorders, and methods of preparation thereof.
摘要翻译： 本发明涉及作为V1a受体拮抗剂并由式I表示的吲哚-3-基 - 羰基 - 哌啶 - 苯并咪唑衍生物：其中残基R1至R7如本文所定义。 本发明还涉及含有这些化合物的药物组合物，它们在治疗痛经，高血压，慢性心力衰竭，不适当的血管加压素分泌，肝硬化，肾病综合征，强迫症，焦虑和抑郁障碍中的用途及其制备方法。
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公开(公告)号：US20100222357A1
公开(公告)日：2010-09-02
申请号：US12779099
申请日：2010-05-13
申请人： Caterina Bissantz , Christophe Grundschober , Hasane Ratni , Mark Rogers-Evans , Patrick Schnider
发明人： Caterina Bissantz , Christophe Grundschober , Hasane Ratni , Mark Rogers-Evans , Patrick Schnider
IPC分类号： A61K31/4985 , C07D403/06 , A61K31/497 , C07D495/04 , C07D401/14 , C07D403/14 , C07D487/04 , A61K31/454 , C07D401/06 , A61K31/4545
CPC分类号： C07D209/42 , C07D209/22 , C07D401/06 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/12 , C07D405/14 , C07D417/12 , C07D495/04
摘要： The present invention relates to indol-3-yl-carbonyl-piperidin and piperazin derivatives which act as V1a receptor antagonists and which are represented by Formula I: wherein the residues R1 to R3 are as defined herein. The invention also relates to pharmaceutical compositions containing such compounds, and methods for preparation of the compounds and compositions. The invention further relates to methods for treating dysmenorrhea, hypertension, chronic heart failure, inappropriate secretion of vasopressin, liver cirrhosis, nephrotic syndrome, obsessive compulsive disorder, anxiety and depressive disorders.
摘要翻译： 本发明涉及作为V1a受体拮抗剂并由式I表示的吲哚-3-基 - 羰基 - 哌啶和哌嗪衍生物：其中残基R1至R3如本文所定义。 本发明还涉及含有这些化合物的药物组合物，以及制备化合物和组合物的方法。 本发明还涉及治疗痛经，高血压，慢性心力衰竭，不适当的血管加压素分泌，肝硬化，肾病综合征，强迫症，焦虑和抑郁障碍的方法。
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公开(公告)号：US20100029664A1
公开(公告)日：2010-02-04
申请号：US12506302
申请日：2009-07-21
IPC分类号： A61K31/498 , C07D413/12 , A61K31/423 , C07D417/12 , A61K31/428 , C07D413/14 , C07D417/14 , C07D403/12
CPC分类号： C07D413/12 , C07D403/12 , C07D413/14 , C07D417/12
摘要： The present invention is concerned with novel sulfonamides of formula I wherein R1, R2, Ar, Hetaryl, m and n are as described in the description and claims. The compounds are orexin receptor antagonists, useful in the treatment of disorders, in which orexin pathways are involved.
摘要翻译： 本发明涉及式I的新型磺酰胺，其中R 1，R 2，Ar，杂芳基，m和n如说明书和权利要求中所述。 这些化合物是食欲素受体拮抗剂，可用于治疗食欲素途径参与的病症。
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公开(公告)号：US20090163485A1
公开(公告)日：2009-06-25
申请号：US12334559
申请日：2008-12-15
IPC分类号： A61K31/5365 , C07D263/54 , A61K31/421 , C07D241/36 , A61K31/498 , C07D417/02 , A61K31/428 , C07D221/00 , A61K31/4245 , A61P25/00 , A61K31/501 , C07D403/02 , A61K31/505 , C07D239/24 , C07D271/06 , A61K31/454 , C07D215/38 , A61K31/4709 , C07D239/72 , A61K31/517 , C07D265/12
CPC分类号： C07D413/12 , C07D401/12 , C07D409/14 , C07D413/14 , C07D417/12 , C07D417/14 , C07D498/04
摘要： The present invention relates to compounds of formula wherein Ar, Het, R1 and n are as defined herein and to pharmaceutically suitable acid addition salts, optically pure enantiomers, racemates or diastereomeric mixtures thereof. Compounds of formula I are orexin receptor antagonists and are useful in the treatment of sleep apnea, narcolepsy, insomnia, parasomnia, jet lag syndrome, circadian rhythms disorder and sleep disorders associated with neurological diseases.
摘要翻译： 本发明涉及下式的化合物其中Ar，Het，R 1和n如本文所定义，并且与药学上合适的酸加成盐，光学纯对映异构体，外消旋物或非对映体混合物相关。 式I化合物是食欲蛋白受体拮抗剂，可用于治疗睡眠呼吸暂停，发作性睡病，失眠，睡眠不正，夜间综合征，昼夜节律障碍和与神经疾病相关的睡眠障碍。
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