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11. 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。

12. 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。

13. 发明申请

US20130281463A1 DIAZA-SPIRO[5.5]UNDECANES USEFUL AS OREXIN RECEPTOR ANTAGONISTS 审中-公开
标题翻译： DIAZA-SPIRO [5.5]有机质作为OREXIN受体拮抗剂
公开(公告)号：US20130281463A1
公开(公告)日：2013-10-24
申请号：US13880994
申请日：2011-10-25
申请人： Sangamesh Badiger , Dirk Behnke , Claudia Betschart , Simona Cotesta , Samuel Hintermann , Silvio Ofner , Chetan Pandit , Bernard Lucien Roy
发明人： Sangamesh Badiger , Dirk Behnke , Claudia Betschart , Simona Cotesta , Samuel Hintermann , Silvio Ofner , Chetan Pandit , Bernard Lucien Roy
IPC分类号： C07D471/10 , A61K45/06 , A61K31/444 , A61K31/506
CPC分类号： C07D471/10 , A61K31/444 , A61K31/506 , A61K45/06 , C07D519/00
摘要： The invention relates to compound of the formula (I), in which the substituents are as defined in the specification; in free form or in salt form; to its preparation, to its use as medicament and to medicaments comprising it.
摘要翻译：本发明涉及式（I）化合物，其中取代基如说明书中所定义; 以游离形式或盐形式; 作为其制备，用作药物和包含它的药物。

14. 发明授权

US08530648B2 Diaza-spiro[5.5]undecanes 失效
标题翻译：丹参螺[5.5]十一烷
公开(公告)号：US08530648B2
公开(公告)日：2013-09-10
申请号：US13517111
申请日：2010-12-20
申请人： Sangamesh Badiger , Dirk Behnke , Claudia Betschart , Vinod Chaudhari , Simona Cotesta , Jürgen Hans-Hermann Hinrichs , Silvio Ofner , Chetan Pandit , Jürgen Wagner
发明人： Sangamesh Badiger , Dirk Behnke , Claudia Betschart , Vinod Chaudhari , Simona Cotesta , Jürgen Hans-Hermann Hinrichs , Silvio Ofner , Chetan Pandit , Jürgen Wagner
IPC分类号： C07D471/10 , A61P3/00 , A61P25/00 , A61P25/28 , A61P25/30
CPC分类号： C07D471/10
摘要： The invention relates to compound of the formula (I), in which the substituents are as defined in the specification; in free form or in salt form; to its preparation, to its use as medicament and to medicaments comprising it.
摘要翻译：本发明涉及式（I）化合物，其中取代基如说明书中所定义; 以游离形式或盐形式; 作为其制备，用作药物和包含它的药物。

15. 发明申请

US20110257131A1 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：US20110257131A1
公开(公告)日：2011-10-20
申请号：US13141249
申请日：2009-12-21
申请人： Simona Cotesta , Wolfgang Jahnke , Jean-Michel Rondeau , Sven Weiler , Leo Widler
发明人： Simona Cotesta , Wolfgang Jahnke , Jean-Michel Rondeau , Sven Weiler , Leo Widler
IPC分类号： A61K31/675 , A61P19/00 , A61P43/00 , C07F9/572
CPC分类号： C07F9/6506
摘要： (Unsubstituted or substituted phenyl)-alkyl-substituted [(imidazol-1-yl)-1-hydroxy-1-phosphono-ethyl]-phosphonic, 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 R1 and R2 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] - 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，它们在疾病治疗中的应用，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。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化合物，其中R 1和R 2之一如说明书中所定义，并且可以为酯的形式的游离形式和/或盐。

16. 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。

17. 发明申请

US20120258973A1 DISUBSTITUTED HETEROARYL-FUSED PYRIDINES 失效
标题翻译：分离的异氟烷基吡啶
公开(公告)号：US20120258973A1
公开(公告)日：2012-10-11
申请号：US13517115
申请日：2010-12-20
申请人： Sangamesh Babiger , Dirk Behnke , Claudia Betschart , Vinod Chaudhari , Murali Chebrolu , Simona Cotesta , Samuel Hintermann , Arndt Meyer , Chetan Pandit
发明人： Sangamesh Babiger , Dirk Behnke , Claudia Betschart , Vinod Chaudhari , Murali Chebrolu , Simona Cotesta , Samuel Hintermann , Arndt Meyer , Chetan Pandit
IPC分类号： A61K31/437 , A61P3/00 , A61P25/30 , A61P25/28 , A61K31/4709 , A61K31/506 , A61K31/497 , C07D519/00 , C07D498/04 , A61K31/444 , A61P25/00 , C07D471/04
CPC分类号： C07D471/04 , C07D498/04 , C07D519/00
摘要： The invention relates to compound of the formula (I′) in which the substituents are as defined in the specification; in free form or in salt form; to its preparation, to its use as medicament and to medicaments comprising it.
摘要翻译：本发明涉及式（I'）的化合物，其中取代基如说明书中所定义; 以游离形式或盐形式; 作为其制备，用作药物和包含它的药物。

18. 发明申请

US20110288057A1 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：US20110288057A1
公开(公告)日：2011-11-24
申请号：US13123681
申请日：2009-10-12
申请人： Simona Cotesta , Joseph Fraser Glickman , Wolfgang Jahnke , Andreas Marzinzik , Silvio Ofner , Jean-Michel Rondeau , Thomas Zoller
发明人： Simona Cotesta , Joseph Fraser Glickman , Wolfgang Jahnke , Andreas Marzinzik , Silvio Ofner , Jean-Michel Rondeau , Thomas Zoller
IPC分类号： A61K31/606 , C07C229/64 , C07D207/26 , C07D295/155 , A61P3/00 , C07D295/185 , C07D243/08 , A61K31/603 , A61K31/625 , A61P35/00 , C07C65/24 , C07D223/04
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）的主要新型化合物，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。

19. 发明申请

US20100222396A1 4-ARYL-BUTANE-1,3-DIAMIDES 审中-公开
公开(公告)号：US20100222396A1
公开(公告)日：2010-09-02
申请号：US12695462
申请日：2010-01-28
申请人： Dirk BEHNKE , Claudia Betschart , Simona Cotesta , Marc Gerspacher , Samuel Hintermann , Bernard Lucien Roy , Anette Von Matt , Jürgen Wagner
发明人： Dirk BEHNKE , Claudia Betschart , Simona Cotesta , Marc Gerspacher , Samuel Hintermann , Bernard Lucien Roy , Anette Von Matt , Jürgen Wagner
IPC分类号： A61K31/44 , C07D207/30 , A61K31/40 , C07D213/81
CPC分类号： C07C233/78 , C07D207/416 , C07D209/08 , C07D213/81 , C07D215/48 , C07D215/50 , C07D217/26 , C07D233/66 , C07D235/24 , C07D277/56 , C07D307/79 , C07D317/68 , C07D401/12 , C07D403/12 , C07D405/12 , C07D413/12 , C07D417/12 , C07D513/04
摘要： The invention relates to compound of the formula I in which the substituents are as defined in the specification; in free form or in salt form; to its preparation, to its use as medicament and to medicaments comprising it.
摘要翻译：本发明涉及式I化合物，其中取代基如说明书中所定义; 以游离形式或盐形式; 作为其制备，用作药物和包含它的药物。

20. 发明申请

US20090099199A1 ORGANIC COMPOUNDS 审中-公开
公开(公告)号：US20090099199A1
公开(公告)日：2009-04-16
申请号：US12251627
申请日：2008-10-15
申请人： Joachim Nozulak , David Orain , Simona Cotesta
发明人： Joachim Nozulak , David Orain , Simona Cotesta
IPC分类号： C07D413/12 , A61K31/4545 , A61K31/454 , A61K31/4523 , A61K31/496 , A61K31/495 , C07D405/12 , C07D405/14 , C07D403/10 , C07D241/04
CPC分类号： C07D261/14 , C07D207/34 , C07D211/14 , C07D211/26 , C07D213/82 , C07D231/14 , C07D235/08 , C07D235/30 , C07D261/18 , C07D295/135 , C07D295/155 , C07D307/24 , C07D401/06 , C07D401/14 , C07D405/04 , C07D405/06 , C07D405/12 , C07D413/04 , C07D413/12
摘要： The invention relates to compound of the formula I wherein the substituents are as defined in the specification; in free base form or in acid addition salt form; to its preparation, to its use as medicament and to medicaments comprising it.

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