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1. 发明申请

WO2007093621A1 CYCLIC SULFONES USEFUL AS BACE INHIBITORS 审中-公开
标题翻译：循环硫磺有效用作BACE抑制剂
公开(公告)号：WO2007093621A1
公开(公告)日：2007-08-23
申请号：PCT/EP2007/051454
申请日：2007-02-14
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , RUEEGER, Heinrich , MCCARTHY, Clive , MOEBITZ, Henrik , RONDEAU, Jean-Michel , TINTELNOT-BLOMLEY, Marina
发明人： RUEEGER, Heinrich , MCCARTHY, Clive , MOEBITZ, Henrik , RONDEAU, Jean-Michel , TINTELNOT-BLOMLEY, Marina
IPC分类号： C07D335/02
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 (I), 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：本发明涉及式（I）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，用作药物和药物包括他们。

2. 发明申请

WO2008062044A1 2-HYDROXY-1,3-DIAMINOPROPANE DERIVATIVES 审中-公开
标题翻译： 2-羟基-1,3-二氨基嘌呤衍生物
公开(公告)号：WO2008062044A1
公开(公告)日：2008-05-29
申请号：PCT/EP2007/062701
申请日：2007-11-22
申请人： NOVARTIS AG , FREDERIKSEN, Mathias , LÜÖND, Rainer Martin , MCCARTHY, Clive , MOEBITZ, Henrik , RONDEAU, Jean-Michel , ROY, Bernard Lucien , RUEEGER, Heinrich
发明人： FREDERIKSEN, Mathias , LÜÖND, Rainer Martin , MCCARTHY, Clive , MOEBITZ, Henrik , RONDEAU, Jean-Michel , ROY, Bernard Lucien , RUEEGER, Heinrich
IPC分类号： C07C233/40 , C07D213/74 , C07D231/38 , C07D237/20 , C07D239/42 , C07D239/46 , C07D239/52 , C07D261/14 , C07D401/12 , C07D487/04 , A61K31/505 , A61K31/44 , A61K31/165 , A61P25/28
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。

3. 发明申请

WO2010076258A1 PHENYLALKYL-IMIDAZOLE-BISPHOSPHONATE COMPOUNDS 审中-公开
标题翻译：苯基 - 咪唑 - 二磷酸酯化合物
公开(公告)号：WO2010076258A1
公开(公告)日：2010-07-08
申请号：PCT/EP2009/067679
申请日：2009-12-21
申请人： NOVARTIS AG , COTESTA, Simona , JAHNKE, Wolfgang , RONDEAU, Jean-Michel , WEILER, Sven , WIDLER, Leo
发明人： COTESTA, Simona , JAHNKE, Wolfgang , RONDEAU, Jean-Michel , WEILER, Sven , WIDLER, Leo
IPC分类号： C07F9/6506 , A61K31/663
CPC分类号： C07F9/65061
摘要： (Unsubstituted or substituted phenyl)-alkyl-substituted [(imidazol-1-yl)-1-hydroxy-1- phosphono-ethyl]-phosρhonic, 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 disclosed. The compounds are able to inhibit excessive or inappropriate bone resorption. The compounds are of the formula (I), wherein one of R 1 and R 2 are as defined in the specification, and can be in free form, in the form of an ester, and/or of a salt.
摘要翻译：（未取代或取代的苯基） - 烷基取代的[（咪唑-1-基）-1-羟基-1-膦酰基 - 乙基] - 苯基，以及其制备方法或方法，它们在制备公开了其在治疗疾病中的用途，用于治疗疾病的方法，包含它们的药物制剂和/或用于治疗疾病的化合物。这些化合物能够抑制过量或不适当的骨吸收。化合物是式（I）的化合物，其中R 1和R 2之一如本说明书中所定义，并且可以为酯的形式的游离形式和/或盐。

4. 发明申请

WO2010043584A1 SALICYLIC ACID DERIVATIVES BEING FARNESYL PYROPHOSPHATE SYNTHASE ACTIVITY INHIBITORS 审中-公开
标题翻译：磷酸酯合成酶活性抑制剂的脂肪酸衍生物
公开(公告)号：WO2010043584A1
公开(公告)日：2010-04-22
申请号：PCT/EP2009/063257
申请日：2009-10-12
申请人： NOVARTIS AG , COTESTA, Simona , GLICKMAN, Joseph Fraser , JAHNKE, Wolfgang , MARZINZIK, Andreas , OFNER, Silvio , RONDEAU, Jean-Michel , ZOLLER, Thomas
发明人： COTESTA, Simona , GLICKMAN, Joseph Fraser , JAHNKE, Wolfgang , MARZINZIK, Andreas , OFNER, Silvio , RONDEAU, Jean-Michel , ZOLLER, Thomas
IPC分类号： C07C65/21 , C07C229/64 , C07D207/06 , C07D207/08 , C07D209/08 , C07D211/22 , C07D213/74 , C07D231/38 , C07D295/10 , C07D307/14 , C07D319/08 , C07D333/20 , A61P43/00 , A61K31/192
CPC分类号： C07D207/26 , C07C65/24 , C07C229/64 , C07C233/54 , C07C255/58 , C07C2601/02 , C07C2601/04 , C07C2601/14 , C07C2601/18 , C07D207/09 , C07D207/327 , C07D209/18 , C07D211/22 , C07D211/58 , C07D213/36 , C07D213/64 , C07D213/74 , C07D231/38 , C07D243/08 , C07D295/155 , C07D295/185 , C07D307/14 , C07D307/54 , C07D307/79 , C07D317/60 , C07D319/18 , C07D333/20 , C07D333/60
摘要： The invention relates to the use of and mainly novel compounds of the formula (I) wherein the moieties are as defined in the description, which are useful as farnesyl pyrophosphate synthase modulators and e.g. in the treatment of proliferative diseases.
摘要翻译：本发明涉及式（I）的新型化合物和主要新颖化合物，其中部分如说明书中所定义，其可用作法呢基焦磷酸合酶调节剂，在治疗增殖性疾病。

5. 发明申请

WO2010003976A1 CYCLIC SULFONES WITH AMINOBENZYL SUBSTITUTION USEFUL AS BACE INHIBITORS 审中-公开
标题翻译：具有氨基取代基的循环磺化作为空白抑制剂有用
公开(公告)号：WO2010003976A1
公开(公告)日：2010-01-14
申请号：PCT/EP2009/058661
申请日：2009-07-08
申请人： NOVARTIS AG , BRIARD, Emmanuelle , LUEOEND, Rainer, Martin , MACHAUER, Rainer , MOEBITZ, Henrik , ROGEL, Olivier , RONDEAU, Jean-Michel , RUEEGER, Heinrich , TINTELNOT-BLOMLEY, Marina , VEENSTRA, Siem, Jacob
发明人： BRIARD, Emmanuelle , LUEOEND, Rainer, Martin , MACHAUER, Rainer , MOEBITZ, Henrik , ROGEL, Olivier , RONDEAU, Jean-Michel , RUEEGER, Heinrich , TINTELNOT-BLOMLEY, Marina , VEENSTRA, Siem, Jacob
IPC分类号： C07D335/02 , C07D409/12 , A61K31/382 , A61P25/28
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 (I); 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：本发明涉及式（I）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，用作药物和包含它们的药物。

6. 发明申请

WO2009068567A1 C2-C5-ALKYL-IMIDAZOLE-BISPHOSPHONATES 审中-公开
标题翻译： C2-C5烷基咪唑双膦酸盐
公开(公告)号：WO2009068567A1
公开(公告)日：2009-06-04
申请号：PCT/EP2008/066245
申请日：2008-11-26
申请人： NOVARTIS AG , WEILER, Sven , WIDLER, Leo , RONDEAU, Jean-Michel , COTESTA, Simona , JAHNKE, Wolfgang
发明人： WEILER, Sven , WIDLER, Leo , RONDEAU, Jean-Michel , COTESTA, Simona , JAHNKE, Wolfgang
IPC分类号： C07F9/6506 , A61K31/663 , A61P19/00
CPC分类号： C07F9/65061
摘要： C 2 -C 5 -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 R 1 and R 2 is hydrogen and the other is C 2 -C 5 -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： C 2 -C 5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。化合物是式（I）的化合物，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/或的盐。

7. 发明申请

WO2009024615A1 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：WO2009024615A1
公开(公告)日：2009-02-26
申请号：PCT/EP2008/061030
申请日：2008-08-22
申请人： NOVARTIS AG , BRIARD, Emmanuelle , LUEOEND, Rainer Martin , MACHAUER, Rainer , MOEBITZ, Henrik , ROGEL, Olivier , RONDEAU, Jean-Michel , RUEEGER, Heinrich , TINTELNOT-BLOMLEY, Marina , VEENSTRA, Siem Jacob
发明人： BRIARD, Emmanuelle , LUEOEND, Rainer Martin , MACHAUER, Rainer , MOEBITZ, Henrik , ROGEL, Olivier , RONDEAU, Jean-Michel , RUEEGER, Heinrich , TINTELNOT-BLOMLEY, Marina , VEENSTRA, Siem Jacob
IPC分类号： C07D335/02 , C07D409/12 , A61K31/382 , A61P25/28
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。

8. 发明申请

WO2007140980A1 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：WO2007140980A1
公开(公告)日：2007-12-13
申请号：PCT/EP2007/004959
申请日：2007-06-04
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , ROGEL, Olivier , RONDEAU, Jean-Michel , RUEEGER, Heinrich , SIMIC, Oliver , SIROCKIN, Finton , TINTELNOT-BLOMLEY, Marina
发明人： ROGEL, Olivier , RONDEAU, Jean-Michel , RUEEGER, Heinrich , SIMIC, Oliver , SIROCKIN, Finton , TINTELNOT-BLOMLEY, Marina
IPC分类号： C07D215/48 , A61K31/47 , A61P25/28
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; the use of a compound of that class in 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（=无序），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; 使用该类化合物治疗依赖于β-分泌酶活性和/或产生β-淀粉样蛋白的疾病，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。

9. 发明申请

WO2006013107A1 IL-17 ANTAGONISTIC ANTIBODIES 审中-公开
标题翻译： IL-17拮抗抗体
公开(公告)号：WO2006013107A1
公开(公告)日：2006-02-09
申请号：PCT/EP2005/008470
申请日：2005-08-04
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , DI PADOVA, Franco, E. , GRAM, Hermann , HOFSTETTER, Hans , JESCHKE, Margit , RONDEAU, Jean-Michel , VAN DEN BERG, Wim
发明人： DI PADOVA, Franco, E. , GRAM, Hermann , HOFSTETTER, Hans , JESCHKE, Margit , RONDEAU, Jean-Michel , VAN DEN BERG, Wim
IPC分类号： A61K39/395
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 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，特别是针对人IL-17的抗体，更优选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。

10. 发明授权

EP2225252B1 C2-C5-ALKYL-IMIDAZOLE-BISPHOSPHONATES 有权
标题翻译： C2-C5-ALKYLIMIDAZOLBISPHOSPHONATE
公开(公告)号：EP2225252B1
公开(公告)日：2012-06-27
申请号：EP08854485.3
申请日：2008-11-26
申请人： Novartis AG
发明人： WEILER, Sven , WIDLER, Leo , RONDEAU, Jean-Michel , COTESTA, Simona , JAHNKE, Wolfgang
IPC分类号： C07F9/6506 , A61K31/663 , A61P19/00
CPC分类号： C07F9/65061
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.

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