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1. 发明授权

US09890166B2 Imidazopyrrolidine derivatives and their use in the treatment of disease 有权
公开(公告)号：US09890166B2
公开(公告)日：2018-02-13
申请号：US14892616
申请日：2014-05-26
申请人： Jutta Blank , Guido Bold , Simona Cotesta , Vito Guagnano , Heinrich Rueeger , Andrea Vaupel
发明人： Jutta Blank , Guido Bold , Simona Cotesta , Vito Guagnano , Heinrich Rueeger , Andrea Vaupel
IPC分类号： C07D487/04 , C07D471/04 , A61K31/4192 , A61K31/4439 , A61K31/444 , A61K31/5025 , A61K31/513 , A61K31/5377
CPC分类号： C07D487/04 , A61K31/4192 , A61K31/4439 , A61K31/444 , A61K31/5025 , A61K31/513 , A61K31/5377 , C07D471/04
摘要： The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.

2. 发明申请

US20120101110A1 Diaza-spiro[5.5]undecanes 审中-公开
标题翻译：丹参螺[5.5]十一烷
公开(公告)号：US20120101110A1
公开(公告)日：2012-04-26
申请号：US13275837
申请日：2011-10-18
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： A61K31/506 , A61K31/444 , A61K31/497 , A61P25/00 , A61P25/18 , A61P25/28 , A61K31/438 , C07D471/10 , A61P25/30
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。

3. 发明授权

US08975417B2 Pyrazolopyrrolidine derivatives and their use in the treatment of disease 有权
标题翻译：吡唑并吡咯啉衍生物及其在治疗疾病中的应用
公开(公告)号：US08975417B2
公开(公告)日：2015-03-10
申请号：US14282515
申请日：2014-05-20
申请人： Vincent Bordas , Simona Cotesta , Vito Guagnano , Heinrich Rueeger , Andrea Vaupel
发明人： Vincent Bordas , Simona Cotesta , Vito Guagnano , Heinrich Rueeger , Andrea Vaupel
IPC分类号： C07D231/56 , A61K31/506 , C07D487/04 , A61K31/4439 , C07D471/04 , A61K31/437 , A61K31/501 , A61K31/423 , A61K31/4192 , A61K45/06
CPC分类号： A61K31/4439 , A61K31/4192 , A61K31/423 , A61K31/437 , A61K31/501 , A61K31/506 , A61K45/06 , C07D471/04 , C07D487/04
摘要： The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
摘要翻译：本发明提供式（I）化合物或其药学上可接受的盐; 制备本发明化合物的方法及其治疗用途。本发明还提供药理活性剂和药物组合物的组合。

4. 发明申请

US20120264748A1 DIAZA-SPIRO[5.5]UNDECANES 失效
标题翻译： DIAZA-SPIRO [5.5] UNDECANES
公开(公告)号：US20120264748A1
公开(公告)日：2012-10-18
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 , A61K31/438 , A61K31/506 , A61K31/5377 , A61P3/00 , A61K31/5025 , A61P25/00 , A61P25/30 , A61P25/28 , A61K31/502 , A61K31/538
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。

5. 发明授权

US07977323B2 C2-C5-alkyl-imidazole-bisphosphonates 有权
标题翻译： C2-C5-烷基 - 咪唑 - 双膦酸盐
公开(公告)号：US07977323B2
公开(公告)日：2011-07-12
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 , C07F9/02
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。

6. 发明申请

US20160280719A1 PYRROLOPYRROLONE DERIVATIVES AND THEIR USE AS BET INHIBITORS 有权
标题翻译：吡咯烷酮衍生物及其作为抑制剂的用途
公开(公告)号：US20160280719A1
公开(公告)日：2016-09-29
申请号：US15037116
申请日：2014-11-20
申请人： Jutta BLANK , Guido BOLD , Vincent BORDAS , Simona COTESTA , Vito GUAGNANO , Heinrich RUEGER , Andrea VAUPEL
发明人： Jutta BLANK , Guido BOLD , Vincent BORDAS , Simona COTESTA , Vito GUAGNANO , Heinrich RUEGER , Andrea VAUPEL
IPC分类号： C07D519/00 , A61K31/437 , A61K31/444 , A61K31/5025 , A61K31/4439 , A61K31/506 , A61K31/513 , C07D487/04 , A61K31/4192
CPC分类号： C07D519/00 , A61K31/4192 , A61K31/437 , A61K31/4439 , A61K31/444 , A61K31/5025 , A61K31/506 , A61K31/513 , A61P35/00 , C07D487/04
摘要： The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.

7. 发明申请

US20160102107A1 PYRAZOLO-PYRROLIDIN-4-ONE DERIVATIVES AS BET INHIBITORS AND THEIR USE IN THE TREATMENT OF DISEASE 有权
标题翻译：吡唑并吡啶-4-酮衍生物作为抑制剂及其在治疗疾病中的应用
公开(公告)号：US20160102107A1
公开(公告)日：2016-04-14
申请号：US14892623
申请日：2014-05-27
申请人： Jutta BLANK , Guido BOLD , Simona COTESTA , Vito GUAGNANO , Heinrich RUEEGER
发明人： Jutta BLANK , Guido BOLD , Simona COTESTA , Vito GUAGNANO , Heinrich RUEEGER
IPC分类号： C07D519/00 , A61K31/5025 , A61K31/4192 , A61K31/437 , C07D487/04
CPC分类号： C07D519/00 , A61K31/4192 , A61K31/437 , A61K31/5025 , C07D487/04
摘要： The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof; (I) a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
摘要翻译：本发明提供式（I）化合物或其药学上可接受的盐; （I）制备本发明化合物的方法及其治疗用途。本发明还提供药理活性剂和药物组合物的组合。

8. 发明授权

US08742106B2 Disubstituted heteroaryl-fused pyridines 失效
标题翻译：二取代杂芳基稠合吡啶
公开(公告)号：US08742106B2
公开(公告)日：2014-06-03
申请号：US13517115
申请日：2010-12-20
申请人： Sangamesh Badiger , Dirk Behnke , Claudia Betschart , Vinod Chaudhari , Murali Chebrolu , Simona Cotesta , Samuel Hintermann , Arndt Meyer , Chetan Pandit
发明人： Sangamesh Badiger , Dirk Behnke , Claudia Betschart , Vinod Chaudhari , Murali Chebrolu , Simona Cotesta , Samuel Hintermann , Arndt Meyer , Chetan Pandit
IPC分类号： C07D471/04 , C07D498/04 , C07D519/00
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。

9. 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。

10. 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。

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