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51. 发明授权

US08389513B2 2-amino-5,5-difluoro-5,6-dihydro-4H-[1,3]oxazin-4-yl)-phenyl]-amides 失效
标题翻译： 2-氨基-5,5-二氟-5,6-二氢-4H- [1,3]恶嗪-4-基） - 苯基] - 酰胺
公开(公告)号：US08389513B2
公开(公告)日：2013-03-05
申请号：US12959412
申请日：2010-12-03
申请人： David Banner , Wolfgang Guba , Hans Hilpert , Harald Mauser , Alexander V. Mayweg , Robert Narquizian , Emmanuel Pinard , Eoin Power , Mark Rogers-Evans , Thomas Woltering , Wolfgang Wostl
发明人： David Banner , Wolfgang Guba , Hans Hilpert , Harald Mauser , Alexander V. Mayweg , Robert Narquizian , Emmanuel Pinard , Eoin Power , Mark Rogers-Evans , Thomas Woltering , Wolfgang Wostl
IPC分类号： C07D265/04 , A61K31/33
CPC分类号： C07D265/08 , C07D413/12
摘要： The present invention relates to 2-Amino-5,5-difluoro-5,6-dihydro-4H-[1,3]oxazin-4-yl)-phenyl]-amides 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2-氨基-5,5-二氟-5,6-二氢-4H- [1,3]恶嗪-4-基） - 苯基] - 酰胺，它们的制造，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。

52. 发明申请

US20120225858A1 1,4 THIAZEPINES/SULFONES AS BACE1 AND/OR BACE2 INHIBITORS 有权
标题翻译： 1,4 THIAZEPINES / SULFONES AS BACE1和/或BACE2抑制剂
公开(公告)号：US20120225858A1
公开(公告)日：2012-09-06
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 , A61P25/28 , 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。

53. 发明申请

US20120035195A1 1,4,5,6-TETRAHYDRO-PYRIMIDIN-2-YLAMINE COMPOUNDS 有权
标题翻译： 1,4,5,6-四氢吡啶-2-基胺化合物
公开(公告)号：US20120035195A1
公开(公告)日：2012-02-09
申请号：US13196933
申请日：2011-08-03
申请人： David Banner , Emanuele Gabellieri , Wolfgang Guba , Hans Hilpert , Benoit Hornsperger , Roland Humm , Harald Mauser , Alexander V. Mayweg , Robert Narquizian , Emmanuel Pinard , Mark Rogers-Evans , Thomas Woltering , Wolfgang Wostl
发明人： David Banner , Emanuele Gabellieri , Wolfgang Guba , Hans Hilpert , Benoit Hornsperger , Roland Humm , Harald Mauser , Alexander V. Mayweg , Robert Narquizian , Emmanuel Pinard , Mark Rogers-Evans , Thomas Woltering , Wolfgang Wostl
IPC分类号： A61K31/513 , A61P3/10 , C07D239/47
CPC分类号： C07D417/12 , A61K31/513 , C07D239/22 , C07D239/70 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12
摘要： This invention relates to compounds of the formula wherein R1 to R9 are as described below, or to pharmaceutically acceptable salts thereof. These compounds are BACE2 inhibitors and can be used as medicaments for the therapeutic and/or prophylactic treatment of diseases such as diabetes, particularly type 2 diabetes, and other metabolic disorders.
摘要翻译：本发明涉及下式化合物或其药学上可接受的盐：其中R 1至R 9如下所述。这些化合物是BACE2抑制剂，可用作治疗和/或预防性治疗诸如糖尿病，特别是2型糖尿病和其它代谢疾病的药物。

54. 发明申请

US20110312937A1 2,5,6,7-TETRAHYDRO-[1,4]OXAZEPIN-3-YLAMINE OR 2,3,6,7-TETRAHYDRO-[1,4]OXAZEPIN-5-YLAMINE COMPOUNDS 失效
标题翻译： 2,5,6,7-四氢 - [1,4]氧杂环己烯-3-基胺或2,3,6,7-四氢 - [1,4]氧杂环己烯-5-胺化合物
公开(公告)号：US20110312937A1
公开(公告)日：2011-12-22
申请号：US13096059
申请日：2011-04-28
申请人： David Banner , Wolfgang Guba , Hans Hilpert , Roland Humm , Harald Mauser , Alexander V. Mayweg , Robert Narquizian , Eoin Power , Mark Rogers-Evans , Didier Rombach , Thomas Woltering , Wolfgang Wostl
发明人： David Banner , Wolfgang Guba , Hans Hilpert , Roland Humm , Harald Mauser , Alexander V. Mayweg , Robert Narquizian , Eoin Power , Mark Rogers-Evans , Didier Rombach , Thomas Woltering , Wolfgang Wostl
IPC分类号： A61K31/553 , A61P3/10 , C07D417/12 , A61P25/28 , C07D413/12 , C07D267/10
CPC分类号： C07D267/10 , C07D413/12 , C07D417/12
摘要： This invention relates to compounds of the formula wherein A, B and R1 to R7 are as described below, or to pharmaceutically acceptable salts thereof. These compounds are BACE1 and/or BACE2 inhibitors and can be used as medicaments for the therapeutic and/or prophylactic treatment of diseases such as Alzheimer's disease, diabetes, particularly type 2 diabetes, and other metabolic disorders.
摘要翻译：本发明涉及下式化合物，其中A，B和R 1至R 7如下所述，或其药学上可接受的盐。这些化合物是BACE1和/或BACE2抑制剂，可用作治疗和/或预防性治疗诸如阿尔茨海默病，糖尿病，特别是2型糖尿病和其它代谢紊乱的药物。

55. 发明授权

US07964594B1 Amino oxazine derivatives 有权
标题翻译：氨基恶嗪衍生物
公开(公告)号：US07964594B1
公开(公告)日：2011-06-21
申请号：US12958436
申请日：2010-12-02
申请人： David Banner , Hans Hilpert , Harald Mauser , Alexander V. Mayweg , Mark Rogers-Evans
发明人： David Banner , Hans Hilpert , Harald Mauser , Alexander V. Mayweg , Mark Rogers-Evans
IPC分类号： C07D265/04 , A61K31/33
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。

56. 发明申请

US20080132562A1 TETRONIC AND TETRAMIC ACIDS 审中-公开
标题翻译：四面体和四面体酸
公开(公告)号：US20080132562A1
公开(公告)日：2008-06-05
申请号：US12023063
申请日：2008-01-31
申请人： Thierry Godel , Hans Hilpert , Roland Humm , Mark Rogers-Evans , Didier Rombach , Christopher Martin Stahl , Peter Weiss , Wolfgang Wostl
发明人： Thierry Godel , Hans Hilpert , Roland Humm , Mark Rogers-Evans , Didier Rombach , Christopher Martin Stahl , Peter Weiss , Wolfgang Wostl
IPC分类号： A61K31/40 , A61P25/28 , A61K31/34
CPC分类号： C07D401/06 , C07D207/38 , C07D307/60 , C07D403/06 , C07D405/06 , C07D409/06 , C07D417/06 , C07D495/06
摘要： This invention relates to new tetronic and tetramic acid derivatives with beta-secretase inhibitory activity of formula I: wherein R1, R2, R3, R4, R5, R5′, R6 and R6′ are as defined hereinabove, to processes for their preparation, compositions containing said tetronic and tetramic acid derivatives and their use in the treatment and prevention of diseases modulated by an inhibitor of β-secretase, such as Alzheimer's disease.
摘要翻译：本发明涉及具有式I的β-分泌酶抑制活性的新的tetronic和tetramic acid衍生物：其中R1，R2，R3，R4，R5，R5'，R6和R6'如上文所定义，其制备方法，组合物含有所述的tetron和四聚酸衍生物及其在治疗和预防由β-分泌酶抑制剂如阿尔茨海默病调节的疾病中的用途。

57. 发明申请

US20050107341A1 Phosphinic acids 失效
标题翻译：次膦酸
公开(公告)号：US20050107341A1
公开(公告)日：2005-05-19
申请号：US10983363
申请日：2004-11-08
申请人： Hans Hilpert , Roland Humm , Dietmar Knopp , Peter Weiss
发明人： Hans Hilpert , Roland Humm , Dietmar Knopp , Peter Weiss
IPC分类号： C07F9/30 , C07F9/572 , C07F9/58 , C07F9/60 , C07F9/653 , A61K31/675 , A61K31/661 , C07F9/141
CPC分类号： C07F9/301 , C07F9/572 , C07F9/5728 , C07F9/58 , C07F9/60 , C07F9/653
摘要： The present invention relates to phosphinic acid derivatives of formula I wherein R1, R2, R3 and R4 are described hereinabove. These compounds can be used in the treatment or prevention of a disease related to the inhibition of β-secretase, inter alia for the treatment of Alzheimer's disease.
摘要翻译：本发明涉及式Ⅰ的次膦酸衍生物，其中R 1，R 2，R 3和R 4， >如上所述。这些化合物可用于治疗或预防与β-分泌酶的抑制相关的疾病，特别是用于治疗阿尔茨海默氏病。

58. 发明授权

US06310262B1 Process for preparing retiferol derivatives 有权
标题翻译：复方衍生物的制备方法
公开(公告)号：US06310262B1
公开(公告)日：2001-10-30
申请号：US09678866
申请日：2000-10-03
申请人： Hans Hilpert
发明人： Hans Hilpert
IPC分类号： C07C3508
CPC分类号： C12P7/62 , C07B2200/07 , C07C45/29 , C07C45/69 , C07C69/013 , C07C403/08 , C07C2601/14 , C07F7/1804 , C07F7/188 , Y02P20/55 , Y02P20/582 , C07C47/273 , C07C49/175
摘要： A new process prepares retiferol derivatives of formula I: wherein A is —C ≡C— or —CH═CH—, and R1 and R2 are independently of each other lower alkyl or lower perfluoroalkyl, one version couples ketones of formula 1I with compounds of formula III A second version couples phosphinoxides of formula IV with aldehydes of formula V. Compounds of formula I are useful in the treatment or prevention of hyperproliferative skin diseases and for reversing the conditions associated with photodamage.
摘要翻译：新方法制备式I的复方酮衍生物：其中A是-C = C-或-CH = CH-，并且R 1和R 2彼此独立地为低级烷基或低级全氟烷基，一个版本将式II的酮与式IIIA化合物第二版将式IV的膦氧基与式V的醛结合。式I化合物可用于治疗或预防过度增生性皮肤病，并用于逆转与光损伤相关的病症。

59. 发明授权

US6130348A Process for a phenylthiobutyl-isoquinoline and intermediates therefor 失效
标题翻译：苯硫基丁基异喹啉的方法及其中间体
公开(公告)号：US6130348A
公开(公告)日：2000-10-10
申请号：US44439
申请日：1998-03-19
申请人： Hans Hilpert
发明人： Hans Hilpert
IPC分类号： C07D217/04 , A61K31/472 , A61P31/14 , A61P31/18 , C07C319/14 , C07C319/20 , C07C323/43 , C07C323/59 , C07D217/26 , C07D303/36
CPC分类号： C07D303/36 , C07C319/14 , C07C319/20 , C07C323/43 , C07C323/59 , C07D217/26 , C07F7/10 , C07F7/1852 , C07B2200/07
摘要： The present invention relates to a new method for making compounds of formula ##STR1## and intermediates for making compounds of formual II. The compounds of this invention are useful intermediates for the manufacture of pharmacologically active compounds suitable for the treatment of viral infections, particularly, those caused by HIV and other retroviruses.
摘要翻译：本发明涉及一种制备式的化合物和制备式Ⅱ化合物的中间体的新方法。本发明的化合物是制备适用于治疗病毒感染，特别是由HIV和其他逆转录病毒引起的病毒感染的药理学活性化合物的有用中间体。

60. 发明授权

US5744611A Process for the reduction of amino acids and the derivatives thereof 失效
标题翻译：用于还原氨基酸及其衍生物的方法
公开(公告)号：US5744611A
公开(公告)日：1998-04-28
申请号：US793702
申请日：1997-03-03
申请人： Matthias Kottenhahn , Karlheinz Drauz , Hans Hilpert
发明人： Matthias Kottenhahn , Karlheinz Drauz , Hans Hilpert
IPC分类号： C07D263/24 , C07C213/00 , C07C215/02 , C07C215/08 , C07C215/10 , C07C215/28 , C07D263/20
CPC分类号： C07D263/20 , C07C213/00 , C07C215/08 , C07C215/10 , C07C215/28
摘要： A process is disclosed for reducing amino acids and derivatives thereof Compounds of formula (I), in which n=0 or 1 and R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 have the meanings given in the description, are reduced to the corresponding amino alcohols of formula (II): the formula (I) compounds are converted in a first step, in at least one alcohol and with the addition of acid and heat to an ester, this process producing a reaction mixture containing the ester; the ester is converted in a second reaction step with alkali or alkaline earth borohydride to compounds of formula II. By specifying that the second step be carried out without isolating the ester from the reaction mixture and by using alkali or alkaline earth borohydrides which are not activated, the invention facilitates the production from amino acids and their derivatives of the correponding alcohols in a simple "single vessel" process, with high yields and in such a way as to preserve a given centre of chirality. Applications: synthesis components, preparation of optically active compounds splitting of racemic compounds. ##STR1##
摘要翻译： PCT No.PCT / EP95 / 03281 Sec。 371日期1997年3月3日 102（e）1997年3月3日PCT PCT 1996年8月17日PCT公布。出版物WO96 / 07634 日本公开了1996年3月14日公开的用于还原氨基酸及其衍生物的方法式（I）化合物，其中n = 0或1，R1，R2，R3，R4，R5和R6具有说明书中给出的含义，被还原成相应的式（II）的氨基醇：式（I）化合物在第一步中，在至少一种醇中转化，并加酸和加热至酯，该方法产生含有酯; 该酯在与碱金属或碱土金属硼氢化物的第二反应步骤中转化为式II化合物。通过规定第二步在不从反应混合物中分离出酯的情况下进行，并且通过使用未活化的碱金属或碱土金属硼氢化物，本发明便于以简单的“单一”形式从相应的醇的氨基酸及其衍生物生产船只“过程，产量高，并且以保持给定的手性中心的方式。应用：合成成分，外消旋化合物的旋光活性化合物的制备。（I）（II）

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