专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

11. 发明申请

US20110224173A1 C2-C5-Alkyl-Imidazole-Bisphosphonates 审中-公开
标题翻译： C2-C5-烷基 - 咪唑 - 二膦酸酯
公开(公告)号：US20110224173A1
公开(公告)日：2011-09-15
申请号：US13116671
申请日：2011-05-26
申请人： Sven Weiler , Leo Widler , Jean-Michel Rondeau , Simona Cotesta , Wolfgang Jahnke
发明人： Sven Weiler , Leo Widler , Jean-Michel Rondeau , Simona Cotesta , Wolfgang Jahnke
IPC分类号： A61K31/675 , C07F9/6506 , A61P19/00
CPC分类号： C07F9/6506
摘要： C2-C5-Alkyl-substituted [imidazol-1-yl)-1-hydroxy-1-phosphono-ethyl]-phosphonic acids, as well as methods or processes for their manufacture, their use in the manufacture of pharmaceutical formulations, their use in the treatment of diseases, methods of using them in the treatment of diseases, pharmaceutical formulations encompassing them and/or the compounds for use in the treatment of diseases, are described. The compounds are able to inhibit excessive or inappropriate bone resorption and for the treatment of other diseases which are caused by excessive prenylation of target proteins, such as Hutchinson-Gilford progeria syndrome. The compounds are of the formula I, wherein one of R1 and R2 is hydrogen and the other is C2-C5-alkyl that is branched or unbranched, and can be in free form, in the form of an ester, and/or of a salt.
摘要翻译： C2-C5-烷基取代的[咪唑-1-基] -1-羟基-1-膦酰基 - 乙基]膦酸，以及其制备方法或方法，它们在制备药物制剂中的用途，它们的用途在治疗疾病方面，使用它们治疗疾病的方法，包括它们的药物制剂和/或用于治疗疾病的化合物。该化合物能够抑制过度或不适当的骨吸收和用于治疗由靶向蛋白过度异戊二烯化引起的其他疾病，例如Hutchinson-Gilford progeria综合征。该化合物具有式I化合物，其中R 1和R 2之一是氢，另一个是支链或非支链的C 2 -C 5 - 烷基，并且可以是酯的游离形式，和/或盐。

12. 发明授权

US5701636A Adjustable door hinge 失效
标题翻译：可调门铰链
公开(公告)号：US5701636A
公开(公告)日：1997-12-30
申请号：US489486
申请日：1995-06-12
申请人： Wolfgang Jahnke
发明人： Wolfgang Jahnke
IPC分类号： E05D7/04
CPC分类号： E05D7/0423 , E05D2003/025 , E05D2007/0461 , E05D2007/0469 , E05D2007/0476 , E05D2007/0484 , E05Y2900/132 , Y10T16/5322 , Y10T16/53225
摘要： An adjustable hinge for mounting a movable door element to a frame element has a plain leaf adapted to be secured to one of the elements and having at least one knuckle, a pintle passing through the knuckle along a pintle axis, and an adjustable leaf. This adjustable leaf has a plate formed with at least one knuckle aligned with the knuckle of the plain leaf and also traversed by the pintle, and a housing adapted to be secured to the other of the elements and formed with a slot receiving the plate. The slot forms a fulcrum for pivoting of the plate relative to the housing about an adjustment axis parallel to but offset from the pintle axis through a multiplicity of angularly offset positions. An adjustable element is provided for fixing the plate in the slot in any of the angularly offset positions. In addition the plate is displaceable parallel to the axis in the housing. The hinge further has at least one axially extending screw braced between the plate and the housing and rotatable for axially displacing the plate in the housing parallel to the axes. This additional axial adjustability can be provided in addition to or instead of the front-to-back transverse adjustability.
摘要翻译：用于将可移动门元件安装到框架元件的可调节铰链具有适于被固定到元件之一的平板叶片，并且具有至少一个转向节，沿枢轴轴线穿过转向节的枢轴和可调叶片。该可调叶片具有形成有至少一个转向节的板，该转向节与平叶的转向节对准，并且也被枢轴穿过，以及适于固定到另一个元件并且形成有容纳板的狭槽的壳体。狭槽形成一个支点，用于使板相对于壳体绕枢轴转动，该调节轴线平行于但是从枢转轴线偏移多个角度偏移位置。提供了可调元件，用于在任何角度偏移位置中将板固定在槽中。此外，板可平行于壳体中的轴线移动。铰链还具有支撑在板和壳体之间的至少一个轴向延伸的螺钉，并且可旋转以使平行于轴线的壳体中的板轴向移位。除了前后的横向可调节性之外，还可以提供这种另外的轴向可调节性。

13. 发明申请

US20120094958A1 QUINOLINES AS INHIBITORS OF FARNESYL PYROPHOSPHATE SYNTHASE 审中-公开
标题翻译：作为呋喃糖磷酸酯合成酶抑制剂的喹啉
公开(公告)号：US20120094958A1
公开(公告)日：2012-04-19
申请号：US12918880
申请日：2009-02-26
申请人： Rene Amstutz , Guido Bold , Simona Cotesta , Wolfgang Jahnke , Andreas Marzinzik , Juliane Constanze Desiree Hartwieg , Silvio Ofner , Frédérik Stauffer , Johann Zimmermann
发明人： Rene Amstutz , Guido Bold , Simona Cotesta , Wolfgang Jahnke , Andreas Marzinzik , Juliane Constanze Desiree Hartwieg , Silvio Ofner , Frédérik Stauffer , Johann Zimmermann
IPC分类号： A61K31/47 , C07D401/10 , C07F9/60 , C07F9/6558 , C07D417/12 , C07F1/02 , A61K31/4709 , A61K31/4725 , A61K31/675 , A61P19/08 , A61P35/00 , A61P3/06 , A61P31/00 , A61P35/04 , C07D215/48
CPC分类号： C07D215/48 , C07D215/18 , C07D401/04 , C07D409/04 , C07D409/14 , C07D417/12 , C07F9/60 , C07F9/65583 , C07F9/65586
摘要： The invention relates to a compound of formula (I) wherein the substituents are as described in the specification, which are useful as farnesyl pyrophosphate synthase modulators, e.g. in the treatment of proliferative diseases, to methods of manufacturing such compounds and to intermediates thereof.
摘要翻译：本发明涉及式（I）化合物，其中取代基如本说明书所述，其可用作法呢基焦磷酸合酶调节剂，例如，在增殖性疾病的治疗中，涉及制造这些化合物的方法及其中间体。

14. 发明申请

US20090143337A1 C2-C5-Alkyl-Imidazole-Bisphosphonates 有权
标题翻译： C2-C5-烷基 - 咪唑 - 二膦酸酯
公开(公告)号：US20090143337A1
公开(公告)日：2009-06-04
申请号：US12323696
申请日：2008-11-26
申请人： Sven Weiler , Leo Widler , Jean-Michel Rondeau , Simona Cotesta , Wolfgang Jahnke
发明人： Sven Weiler , Leo Widler , Jean-Michel Rondeau , Simona Cotesta , Wolfgang Jahnke
IPC分类号： A61K31/675 , C07F9/40 , A61P19/08
CPC分类号： C07F9/6506
摘要： C2-C5-Alkyl-substituted [(imidazol-1-yl)-1-hydroxy-1-phosphono-ethyl]-phosphonic acids, as well as methods or processes for their manufacture, their use in the manufacture of pharmaceutical formulations, their use in the treatment of diseases, methods of using them in the treatment of diseases, pharmaceutical formulations encompassing them and/or the compounds for use in the treatment of diseases, are described. The compounds are able to inhibit excessive or inappropriate bone resorption and for the treatment of other diseases which are caused by excessive prenylation of target proteins, such as Hutchinson-Gilford progeria syndrome. The compounds are of the formula I, wherein one of R1 and R2 is hydrogen and the other is C2-C5-alkyl that is branched or unbranched, and can be in free form, in the form of an ester, and/or of a salt.
摘要翻译： C2-C5-烷基取代的[（咪唑-1-基）-1-羟基-1-膦酰基 - 乙基] - 膦酸，以及其制备方法或方法，它们在药物制剂的制备中的用途，它们描述了用于治疗疾病，用于治疗疾病的方法，包括它们的药物制剂和/或用于治疗疾病的化合物。该化合物能够抑制过度或不适当的骨吸收和用于治疗由靶向蛋白过度异戊二烯化引起的其他疾病，例如Hutchinson-Gilford progeria综合征。该化合物具有式I化合物，其中R 1和R 2之一是氢，另一个是支链或非支链的C 2 -C 5 - 烷基，并且可以是酯的游离形式，和/或盐。

15. 发明申请

US20080139449A1 X-Ray Structure of Human Fpps and Use For Selecting Fpps Binding Compounds 审中-公开
标题翻译：人类Fpps的X射线结构和用于选择Fpps结合化合物的用途
公开(公告)号：US20080139449A1
公开(公告)日：2008-06-12
申请号：US11722574
申请日：2006-01-02
申请人： Wolfgang Jahnke , Jean-Michel Rondeau , Martin Geiser , Paul Ramage , Andre Strauss
发明人： Wolfgang Jahnke , Jean-Michel Rondeau , Martin Geiser , Paul Ramage , Andre Strauss
IPC分类号： A61K38/00 , C12N9/10 , C12P21/04 , A61P43/00 , C12Q1/00 , G06G7/48
CPC分类号： C12N9/1085 , C07K2299/00
摘要： The present invention relates to crystalline human farnesyl diphosphate synthase (FPPS), to the three-dimensional structure of free FPPS as well as the three-dimensional structures of FPPS in complex with substrates such as IPP (isopentenyl diphosphate) and/or with inhibitors such as Zometa® or Aredia®. Further, methods for preparing crystals of human FPPS are described. According to the invention the crystals can be used to determine the structures of FPPS homologs mutants, complexes with ligands, FPPS crystal forms and similar molecules of unknown structure. The invention further relates to the use of FPPS crystals to select new FPPS ligands, e.g. by X-ray screening and to design and/or identify inhibitors against FPPS. Furthermore, the invention relates to NMR methods for selecting and/or identifying new low molecular weight binders to FPPS, which represent new therapeutic agents.
摘要翻译：本发明涉及结晶人类法呢基二磷酸合成酶（FPPS），与游离FPPS的三维结构以及FPPS与底物复合物（例如IPP（异戊烯二磷酸酯））和/或与抑制剂的复合物的三维结构作为Zometa或Aredia（R）。此外，描述了制备人FPPS晶体的方法。根据本发明，晶体可用于确定FPPS同系物突变体，配体配合物，FPPS晶体形式和未知结构的类似分子的结构。本发明还涉及使用FPPS晶体来选择新的FPPS配体，例如，通过X射线检查和设计和/或识别针对FPPS的抑制剂。此外，本发明涉及用于选择和/或鉴定新的FPPS的低分子量粘合剂的NMR方法，其代表新的治疗剂。

16. 发明申请

US20160200705A1 BENZAMIDE DERIVATIVES FOR INHIBITING THE ACTIVITY OF ABL1, ABL2 AND BCR-ABL1 审中-公开
标题翻译：用于抑制ABL1，ABL2和BCR-ABL1活性的苯扎明星衍生物
公开(公告)号：US20160200705A1
公开(公告)日：2016-07-14
申请号：US15075620
申请日：2016-03-21
申请人： Pascal FURET , Robert Martin GROTZFELD , Wolfgang JAHNKE , Darryl JONES , Paul William MANLEY , Andreas MARZINZIK , Xavier Francois Andre PELLE , Bahaa SALEM , Joseph SCHOEPFER
发明人： Pascal FURET , Robert Martin GROTZFELD , Wolfgang JAHNKE , Darryl JONES , Paul William MANLEY , Andreas MARZINZIK , Xavier Francois Andre PELLE , Bahaa SALEM , Joseph SCHOEPFER
IPC分类号： C07D401/14 , A61K45/06 , C07D403/10 , A61K31/4155 , A61K31/4439 , C07D487/10
CPC分类号： C07D417/14 , A61K31/4025 , A61K31/4155 , A61K31/427 , A61K31/4439 , A61K31/5377 , A61K45/06 , C07D401/04 , C07D401/14 , C07D403/10 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/10 , C07D487/10
摘要： The present invention relates to compounds of formula (I): in which Y, Y1, R1, R2, R3 and R4 are defined in the Summary of the Invention; capable of inhibiting the tyrosine kinase enzymatic activity of the Abelson protein (ABL1), the Abelson-related protein (ABL2) and related chimeric proteins, in particular BCR-ABL1. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds in the treatment of cancers.
摘要翻译：本发明涉及式（I）化合物：其中Y，Y 1，R 1，R 2，R 3和R 4在本发明概述中定义; 能够抑制Abelson蛋白（ABL1），Abelson相关蛋白（ABL2）和相关嵌合蛋白（特别是BCR-ABL1）的酪氨酸激酶酶活性。本发明还提供了制备本发明化合物的方法，包含这些化合物的药物制剂和使用这些化合物治疗癌症的方法。

17. 发明申请

US20150183801A1 COMPOUNDS AND COMPOSITIONS FOR INHIBITING THE ACTIVITY OF ABL1, ABL2 AND BCR-ABL1 有权
标题翻译：抑制ABL1，ABL2和BCR-ABL1活性的化合物和组合物
公开(公告)号：US20150183801A1
公开(公告)日：2015-07-02
申请号：US14400987
申请日：2013-05-09
申请人： Pascal Furet , Robert Martin Grotzfeld , Wolfgang Jahnke , Darryl Brynley Jones , Paul William Manley , Andreas Marzinzik , Xavier Francois Andre Pelle , Bahaa Salem , Joseph Schoepfer , Erich Alois Spieser
发明人： Pascal Furet , Robert Martin Grotzfeld , Wolfgang Jahnke , Darryl Brynley Jones , Paul William Manley , Andreas Marzinzik , Xavier Francois Andre Pelle , Bahaa Salem , Joseph Schoepfer , Erich Alois Spieser
IPC分类号： C07D498/08 , A61K31/506 , C07D401/10 , A61K31/4439 , C07D401/14 , C07D487/04 , C07D487/10 , C07D471/04 , C07D405/14 , A61K31/444 , A61K31/4725 , A61K31/498 , C07D491/107 , A61K31/4545 , A61K31/551 , A61K31/553 , A61K45/06 , A61K31/5025 , C07D403/10
CPC分类号： C07D498/08 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61K31/4725 , A61K31/498 , A61K31/5025 , A61K31/506 , A61K31/551 , A61K31/553 , A61K45/06 , C07D401/04 , C07D401/10 , C07D401/14 , C07D403/10 , C07D405/14 , C07D413/10 , C07D413/14 , C07D471/04 , C07D487/04 , C07D487/10 , C07D491/10 , C07D491/107
摘要： The present invention relates to compounds of formula (I): in which Y, Y, R, R 2, R 3 and R 4 are defined in the Summary of the Invention; capable of inhibiting the activity of BCR-ABL1 and mutants thereof. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds in the treatment of cancers.
摘要翻译：本发明涉及式（I）化合物：其中Y，Y，R，R 2，R 3和R 4在发明概述中定义; 能够抑制BCR-ABL1及其突变体的活性。本发明还提供了制备本发明化合物的方法，包含这些化合物的药物制剂和使用这些化合物治疗癌症的方法。

18. 发明申请

US20140343086A1 COMPOUNDS AND COMPOSITIONS FOR INHIBITING THE ACTIVITY OF ABL1, ABL2 AND BCR-ABL1 审中-公开
标题翻译：抑制ABL1，ABL2和BCR-ABL1活性的化合物和组合物
公开(公告)号：US20140343086A1
公开(公告)日：2014-11-20
申请号：US14448363
申请日：2014-07-31
申请人： Stephanie Kay DODD , Pascal FURET , Robert Martin GROTZFELD , Wolfgang JAHNKE , Darryl Brynley JONES , Paul William MANLEY , Andreas MARZINZIK , Xavier Francois Andre PELLE , Bahaa SALEM , Joseph SCHOEPFER
发明人： Stephanie Kay DODD , Pascal FURET , Robert Martin GROTZFELD , Wolfgang JAHNKE , Darryl Brynley JONES , Paul William MANLEY , Andreas MARZINZIK , Xavier Francois Andre PELLE , Bahaa SALEM , Joseph SCHOEPFER
IPC分类号： C07D213/82 , A61K31/506 , C07D401/14 , C07D401/04 , A61K31/4439 , C07D405/14
CPC分类号： C07D213/82 , A61K31/4439 , A61K31/506 , A61K45/06 , C07D401/04 , C07D401/10 , C07D401/14 , C07D403/10 , C07D405/14 , C07F9/58
摘要： The present invention relates to compounds of formula (I): in which Y, Y1, R1, R2, R3 and R4 are defined in the Summary of the Invention; capable of inhibiting the activity of BCR-ABL1 and mutants thereof. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds in the treatment of cancers.
摘要翻译：本发明涉及式（I）化合物：其中Y，Y 1，R 1，R 2，R 3和R 4在发明概述中定义; 能够抑制BCR-ABL1及其突变体的活性。本发明还提供了制备本发明化合物的方法，包含这些化合物的药物制剂和使用这些化合物治疗癌症的方法。

19. 发明申请

US20050202505A1 Method to identify modulators for human 3alpha-hydroxysteroid dehydrogenase 审中-公开
标题翻译：识别人3α-羟基类固醇脱氢酶调节剂的方法
公开(公告)号：US20050202505A1
公开(公告)日：2005-09-15
申请号：US10486660
申请日：2002-08-21
申请人： Philipp Floersheim , Christian Ostermeier , Doncho Uzunov , Wolfgang Jahnke
发明人： Philipp Floersheim , Christian Ostermeier , Doncho Uzunov , Wolfgang Jahnke
IPC分类号： C12N15/09 , C12N9/04 , C12Q1/32 , G01N33/48 , G01N33/50 , G01N33/53 , G06F19/00
CPC分类号： C12Q1/32 , G01N2500/04
摘要： 3 α-hydroxysteroid dehydrogenase (3a-HSD) plays a central role in the metabolism and action of steroid hormones and neurosteroids (steroids synthesized in the central nervous system). The high resolution structure of human type III 3a-HSD crystallized in complex with cofactor NADP is determined by X-ray diffraction. Furthermore the active site is determined. The structure coordinates of the enzyme may be used to design and select novel classes of modulators to human type III 3a-HSD.
摘要翻译： 3α-羟基类固醇脱氢酶（3a-HSD）在类固醇激素和神经甾体（在中枢神经系统中合成的类固醇）的代谢和作用中起着核心作用。通过X射线衍射测定与辅因子NADP复合结晶的人III型III-HSD的高分辨率结构。此外，确定活性位点。酶的结构坐标可用于设计和选择人类III型3a-HSD的新型调节剂。

20. 发明授权

US09896444B2 Benzamide derivatives for inhibiting the activity of ABL1, ABL2 and BCR-ABL1 有权
公开(公告)号：US09896444B2
公开(公告)日：2018-02-20
申请号：US15075620
申请日：2016-03-21
申请人： Pascal Furet , Robert Martin Grotzfeld , Wolfgang Jahnke , Darryl Jones , Paul William Manley , Andreas Marzinzik , Xavier Francois Andre Pelle , Bahaa Salem , Joseph Schoepfer
发明人： Pascal Furet , Robert Martin Grotzfeld , Wolfgang Jahnke , Darryl Jones , Paul William Manley , Andreas Marzinzik , Xavier Francois Andre Pelle , Bahaa Salem , Joseph Schoepfer
IPC分类号： C07D401/14 , C07D417/14 , A61K31/4155 , C07D487/10 , C07D405/14 , C07D413/14 , C07D401/04 , C07D403/10 , C07D409/14 , C07D417/10 , A61K31/4025 , A61K31/427 , A61K31/4439 , A61K31/5377 , A61K45/06
CPC分类号： C07D417/14 , A61K31/4025 , A61K31/4155 , A61K31/427 , A61K31/4439 , A61K31/5377 , A61K45/06 , C07D401/04 , C07D401/14 , C07D403/10 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/10 , C07D487/10
摘要： The present invention relates to compounds of formula (I): in which Y, Y1, R1, R2, R3 and R4 are defined in the Summary of the Invention; capable of inhibiting the tyrosine kinase enzymatic activity of the Abelson protein (ABL1), the Abelson-related protein (ABL2) and related chimeric proteins, in particular BCR-ABL1. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds in the treatment of cancers.

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式