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1. 发明申请

US20100144741A1 ETHANOLAMINE DERIVATIVES USEFUL AS BACE INHIBITORS 审中-公开
标题翻译：乙酰胺衍生物可用作BACE抑制剂
公开(公告)号：US20100144741A1
公开(公告)日：2010-06-10
申请号：US12515521
申请日：2007-11-22
申请人： Mathias Frederiksen , Rainer Martin Luond , Clive McCarthy , Henrik Moebitz , Jean-Michel Rondeau , Bernard Lucien Roy , Heinrich Rueeger
发明人： Mathias Frederiksen , Rainer Martin Luond , Clive McCarthy , Henrik Moebitz , Jean-Michel Rondeau , Bernard Lucien Roy , Heinrich Rueeger
IPC分类号： A61K31/4402 , C07D401/02 , C07D239/42 , C07C233/40 , C07D213/72 , C07D405/10 , C07D237/20 , C07D487/04 , A61K31/505 , A61K31/506 , A61K31/4418 , A61K31/50 , A61K31/5025 , A61P25/00
CPC分类号： C07D401/12 , C07C233/40 , C07C2601/02 , C07D213/74 , C07D231/38 , C07D237/20 , C07D239/42 , C07D239/47 , C07D239/52 , C07D261/14 , C07D487/04
摘要： The invention relates to novel cyclic compounds of the formula (I), in free base form or in acid addition salt form, to their preparation, to their use as medicaments and to medicaments comprising them.
摘要翻译：本发明涉及以游离碱形式或以酸加成盐形式的式（I）的新型环状化合物，其制备方法，其用作药物和包含它们的药物。

2. 发明申请

US20090099207A1 Cyclic sulfones useful as BACE inhibitors 审中-公开
标题翻译：可用作BACE抑制剂的环状砜
公开(公告)号：US20090099207A1
公开(公告)日：2009-04-16
申请号：US12279388
申请日：2007-02-14
申请人： Heinrich Rueeger , Clive McCarthy , Henrik Moebitz , Jean-Michel Rondeau , Marina Tintelnot-Blomley
发明人： Heinrich Rueeger , Clive McCarthy , Henrik Moebitz , Jean-Michel Rondeau , Marina Tintelnot-Blomley
IPC分类号： A61K31/506 , C07D335/02 , A61K31/382 , C07D409/02 , A61K31/427 , A61P9/00 , A61P25/00 , C07D417/02 , C07D413/02 , A61K31/422 , A61K31/4436
CPC分类号： C07D335/02 , C07D409/12 , C07D413/10 , C07D413/12 , C07D417/12
摘要： The invention relates to novel heterocyclic compounds of the formula in which all of the variables are as defined in the specification, in free base form or in acid addition salt form, to their preparation, to their use as medicaments and to medicaments comprising them.
摘要翻译：本发明涉及下式的新型杂环化合物，其中所有变量如本说明书中所定义，游离碱形式或酸加成盐形式，其制备方法，用作药物和包含它们的药物。

3. 发明申请

US20100056490A1 Cyclic sulfones with aminobenzyl substitution useful as BACE inhibitors 失效
标题翻译：具有氨基苄基取代基的环砜用作BACE抑制剂
公开(公告)号：US20100056490A1
公开(公告)日：2010-03-04
申请号：US12500093
申请日：2009-07-09
申请人： Emmanuelle Briard , Rainer Martin Lueoend , Rainer Machauer , Henrik Moebitz , Olivier Rogel , Jean-Michel Rondeau , Heinrich Rueeger , Marina Tintelnot-Blomley , Siem Jacob Veenstra
发明人： Emmanuelle Briard , Rainer Martin Lueoend , Rainer Machauer , Henrik Moebitz , Olivier Rogel , Jean-Michel Rondeau , Heinrich Rueeger , Marina Tintelnot-Blomley , Siem Jacob Veenstra
IPC分类号： A61K31/397 , C07D401/12 , C07D205/02 , C07D335/02 , A61K31/4535 , A61K31/382 , A61P25/00 , A61P9/10
CPC分类号： C07D335/02 , C07D409/10 , C07D409/12 , C07D413/12 , C07F7/0812
摘要： The invention relates to novel heterocyclic compounds of the formula in which all of the variables are as defined in the specification, in free form or in salt form, to their preparation, to their use as medicaments and to medicaments comprising them.
摘要翻译：本发明涉及下式的新型杂环化合物，其中所有变量如本说明书中所定义，以游离形式或盐形式，其制备方式，其用作药物和包含它们的药物。

4. 发明授权

US08093406B2 Cyclic sulfones with aminobenzyl substitution useful as BACE inhibitors 失效
标题翻译：具有氨基苄基取代基的环砜用作BACE抑制剂
公开(公告)号：US08093406B2
公开(公告)日：2012-01-10
申请号：US12500093
申请日：2009-07-09
申请人： Emmanuelle Briard , Rainer Martin Lueoend , Rainer Machauer , Henrik Moebitz , Olivier Rogel , Jean-Michel Rondeau , Heinrich Rueeger , Marina Tintelnot-Blomley , Siem Jacob Veenstra
发明人： Emmanuelle Briard , Rainer Martin Lueoend , Rainer Machauer , Henrik Moebitz , Olivier Rogel , Jean-Michel Rondeau , Heinrich Rueeger , Marina Tintelnot-Blomley , Siem Jacob Veenstra
IPC分类号： C07D335/02
CPC分类号： C07D335/02 , C07D409/10 , C07D409/12 , C07D413/12 , C07F7/0812
摘要： The invention relates to novel heterocyclic compounds of the formula in which all of the variables are as defined in the specification, in free form or in salt form, to their preparation, to their use as medicaments and to medicaments comprising them.
摘要翻译：本发明涉及下式的新型杂环化合物，其中所有变量如本说明书中所定义，以游离形式或盐形式，其制备方式，其用作药物和包含它们的药物。

5. 发明申请

US20090054427A1 AMINOBENZYL-SUBSTITUTED CYCLIC SULFONES USEFUL AS BACE INHIBITORS 审中-公开
标题翻译：氨基取代的循环硫磺有效用作BACE抑制剂
公开(公告)号：US20090054427A1
公开(公告)日：2009-02-26
申请号：US12196461
申请日：2008-08-22
申请人： Emmanuelle Briard , Rainer Martin Lueoend , Rainer Machauer , Henrik Moebitz , Olivier Rogel , Jean-Michel Rondeau , Heinrich Rueeger , Marina Tintelnot-Blomley , Siem Jacob Veenstra
发明人： Emmanuelle Briard , Rainer Martin Lueoend , Rainer Machauer , Henrik Moebitz , Olivier Rogel , Jean-Michel Rondeau , Heinrich Rueeger , Marina Tintelnot-Blomley , Siem Jacob Veenstra
IPC分类号： A61K31/5377 , C07D335/02 , A61K31/382 , A61P25/00 , C07D413/08
CPC分类号： C07D335/02 , C07D409/12
摘要： The invention relates to novel heterocyclic compounds of the formula in which all of the variables are as defined in the specification, in free form or in salt form, to their preparation, to their use as medicaments and to medicaments comprising them.
摘要翻译：本发明涉及下式的新型杂环化合物，其中所有变量如本说明书中所定义，以游离形式或盐形式，其制备方式，其用作药物和包含它们的药物。

6. 发明申请

US20090247577A1 PYRROLIDINE DERIVATIVES USEFUL AS BACE INHIBITORS 审中-公开
标题翻译：吡咯烷衍生物有效用作BACE抑制剂
公开(公告)号：US20090247577A1
公开(公告)日：2009-10-01
申请号：US12303495
申请日：2007-06-04
申请人： Olivier Rogel , Jean-Michel Rondeau , Heinrich Rueeger , Oliver Simic , Finton Sirockin , Marina Tintelnot-Blomley
发明人： Olivier Rogel , Jean-Michel Rondeau , Heinrich Rueeger , Oliver Simic , Finton Sirockin , Marina Tintelnot-Blomley
IPC分类号： A61K31/4709 , C07D401/12
CPC分类号： C07D215/48
摘要： Novel 3-mono-, 3,4-di- and 3,4,4,-tri-substituted pyrrolidine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (disorder) that depends on the activity of beta-secretase and/or the generation of beta-amyloid and the subsequent aggregation into oligomers and fibrils; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on the activity of beta-secretase and/or the generation of beta-amyloid and the subsequent aggregation into oligomers and fibrils; pharmaceutical formulations comprising a said substituted pyrrolidine compound, and/or a method of treatment comprising administering a said substituted pyrrolidine compound. The substituted pyrrolidine compounds are especially of the formula I, wherein the substituents are as defined in the specification.
摘要翻译：新型3-单，3,4-二和3,4,4-三取代的吡咯烷化合物，用于诊断和治疗温血动物，特别是用于治疗疾病的化合物（紊乱），其取决于β-分泌酶的活性和/或β-淀粉样蛋白的产生，并随后聚集成低聚物和原纤维; 使用该类化合物来制备用于治疗依赖于β-分泌酶的活性和/或产生β-淀粉样蛋白的疾病的药物制剂并随后聚集成低聚物和原纤维; 包含所述取代的吡咯烷化合物的药物制剂和/或包括施用所述取代的吡咯烷化合物的治疗方法。取代的吡咯烷化合物特别是式I，其中取代基如说明书中所定义。

7. 发明授权

US08617552B2 IL-17 antibodies 有权
标题翻译： IL-17抗体
公开(公告)号：US08617552B2
公开(公告)日：2013-12-31
申请号：US13349689
申请日：2012-01-13
申请人： Franco E Di Padova , Hermann Gram , Hans Hofstetter , Margit Jeschke , Jean-Michel Rondeau , Wim Van Den Berg
发明人： Franco E Di Padova , Hermann Gram , Hans Hofstetter , Margit Jeschke , Jean-Michel Rondeau , Wim Van Den Berg
IPC分类号： C07H21/04
CPC分类号： C07K16/244 , C07K2317/21 , C07K2317/55 , C07K2317/76 , C07K2317/92
摘要： An IL-17 binding molecule, in particular an antibody to human IL-17, more preferably a human antibody to human IL-17 is provided, wherein the hypervariable regions of the heavy and light chains have amino acid sequences as defined, for use in the treatment of an IL-17 mediated disease or disorder, e.g. rheumatoid arthritis.
摘要翻译：提供IL-17结合分子，特别是人IL-17的抗体，更优选人IL-17的人抗体，其中重链和轻链的高变区具有如所定义的氨基酸序列，用于治疗IL-17介导的疾病或病症，例如类风湿关节炎。

8. 发明申请

US20120107325A1 IL-17 Antagonistic Antibodies 有权
标题翻译： IL-17拮抗性抗体
公开(公告)号：US20120107325A1
公开(公告)日：2012-05-03
申请号：US13349689
申请日：2012-01-13
申请人： Franco E. Di Padova , Hermann Gram , Hans Hofstetter , Margit Jeschke , Jean-Michel Rondeau , Wim Van Den Berg
发明人： Franco E. Di Padova , Hermann Gram , Hans Hofstetter , Margit Jeschke , Jean-Michel Rondeau , Wim Van Den Berg
IPC分类号： A61K39/395 , C07K16/24 , A61P29/00 , C12N1/19 , C12P21/06 , C12N5/10 , C12N1/21 , C12N15/13 , C12N15/63
CPC分类号： C07K16/244 , C07K2317/21 , C07K2317/55 , C07K2317/76 , C07K2317/92
摘要： An IL-17 binding molecule, in particular an antibody to human IL-17, more preferably a human antibody to human IL-17 is provided, wherein the hypervariable regions of the heavy and light chains have amino acid sequences as defined, for use in the treatment of an IL-17 mediated disease or disorder, e.g. rheumatoid arthritis.
摘要翻译：提供IL-17结合分子，特别是人IL-17的抗体，更优选人IL-17的人抗体，其中重链和轻链的高变区具有如所定义的氨基酸序列，用于治疗IL-17介导的疾病或病症，例如类风湿关节炎。

9. 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。

10. 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。

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