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1. 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。

2. 发明授权

US09284284B2 Oxazine derivatives and their use in the treatment of disease 有权
公开(公告)号：US09284284B2
公开(公告)日：2016-03-15
申请号：US14350938
申请日：2012-10-11
申请人： Konstanze Hurth , Sebastien Jacquier , Rainer Machauer , Heinrich Rueeger , Marina Tintelnot-Blomley , Siem Jacob Veenstra , Markus Voegtle
发明人： Konstanze Hurth , Sebastien Jacquier , Rainer Machauer , Heinrich Rueeger , Marina Tintelnot-Blomley , Siem Jacob Veenstra , Markus Voegtle
IPC分类号： C07D265/30 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/12 , C07D471/04 , C07D487/04 , A61K31/5375 , A61K31/5377
CPC分类号： C07D265/30 , A61K31/5375 , A61K31/5377 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/12 , C07D471/04 , C07D487/04
摘要： The invention relates to novel oxazine derivatives of formula (I), and pharmaceutically acceptable salts thereof, in which all of the variables are as defined in the specification, pharmaceutical compositions thereof, combinations thereof, and their use as medicaments, particularly for the treatment of Alzheimer's Disease or diabetes via inhibition of BACE-1 or BACE-2.

3. 发明申请

US20140135330A1 Oxazolidin-2-one-Pyrimidine Derivatives 有权
标题翻译：恶唑烷-2-酮嘧啶衍生物
公开(公告)号：US20140135330A1
公开(公告)日：2014-05-15
申请号：US14069400
申请日：2013-11-01
申请人： Robin Alec Fairhurst , Pascal Furet , Frank Stephan Kalthoff , Andreas Lerchner , Heinrich Rueeger
发明人： Robin Alec Fairhurst , Pascal Furet , Frank Stephan Kalthoff , Andreas Lerchner , Heinrich Rueeger
IPC分类号： C07D413/14 , A61K31/5377 , A61K45/06 , C07D417/14
CPC分类号： C07D417/14 , A61K31/5377 , A61K45/06 , C07D413/14
摘要： The present invention relates to oxazolidin-2-one substituted pyrimidine compounds that act as PI3K (phosphatidylinositol-3-kinase) inhibitors, as well as pharmaceutical compositions thereof, methods for their manufacture and uses for the treatment of conditions, diseases and disorders dependent on PI3K.
摘要翻译：本发明涉及作为PI3K（磷脂酰肌醇-3-激酶）抑制剂的恶唑烷-2-酮取代的嘧啶化合物及其药物组合物，其制备方法和用于治疗依赖于 PI3K。

4. 发明授权

US08338413B1 Oxazine derivatives and their use in the treatment of neurological disorders 有权
公开(公告)号：US08338413B1
公开(公告)日：2012-12-25
申请号：US13414483
申请日：2012-03-07
申请人： Heinrich Rueeger
发明人： Heinrich Rueeger
IPC分类号： A61K31/535
CPC分类号： C07D413/12
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 medical use and to medicaments comprising them.

5. 发明授权

US07910774B2 Alternative synthesis of renin inhibitors and intermediates thereof 失效
标题翻译：肾素抑制剂及其中间体的替代合成
公开(公告)号：US07910774B2
公开(公告)日：2011-03-22
申请号：US11573790
申请日：2005-08-30
申请人： Gottfried Sedelmeier , Stuart John Mickel , Heinrich Rueeger
发明人： Gottfried Sedelmeier , Stuart John Mickel , Heinrich Rueeger
IPC分类号： C07C233/65
CPC分类号： C07D207/26 , C07C271/16 , C07C271/22 , C07D211/76 , C07D307/33
摘要： The present invention relates to synthetic routes to prepare a compound of the formula wherein R1 is halogen, C1-6halogenalkyl, C1-6alkoxy-C1-6alkyloxy or C1-6alkoxy-C1-6alkyl; R2 is halogen, C1-4alkyl or C1-4alkoxy; R3 and R4 are independently branched C3-6alkyl; and R5 is cycloalkyl, C1-6alkyl, C1-6hydroxyalkyl, C1-6alkoxy-C1-6alkyl, C1-6alkanoyloxy-C1-6alkyl, C1-6aminoalkyl, C1-6alkylamino-C1-6alkyl, C1-6dialkylamino-C1-6alkyl, C1-6alkanoylamino-C1-6alkyl, HO(O)C—C1-6alkyl, C1-6alkyl-O—(O)C—C1-6alkyl, H2N—C(O)—C1-6alkyl, C1-6alkyl-HN—C(O)—C1-6alkyl or (C1-6alkyl)2N—C(O)—C1-6alkyl; or a pharmaceutically acceptable salt thereof as well as key intermediates obtained when following these routes as well as their preparation.
摘要翻译：本发明涉及制备下式化合物的合成路线：其中R 1是卤素，C 1-6卤代烷基，C 1-6烷氧基-C 1-6烷氧基或C 1-6烷氧基-C 1-6烷基; R2是卤素，C1-4烷基或C1-4烷氧基; R3和R4独立地是支链的C 3-6烷基; 和R 5是环烷基，C 1-6烷基，C 1-6羟基烷基，C 1-6烷氧基-C 1-6烷基，C 1-6烷酰氧基-C 1-6烷基，C 1-6氨基烷基，C 1-6烷基氨基-C 1-6烷基，C 1-6二烷基氨基-C 1-6烷基，C 1 （O）C 1-6烷基，C 1-6烷基-O-（O）C 1-6烷基，H 2 N-C（O）-C 1-6烷基，C 1-6烷基-NH- C （O）-C 1-6烷基或（C 1-6烷基）2 N -C（O）-C 1-6烷基; 或其药学上可接受的盐以及按照这些途径获得的关键中间体及其制备方法。

6. 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。

7. 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.

8. 发明申请

US20160168145A1 OXAZOLIDIN-2-ONE-PYRIMIDINE DERIVATIVES AND THE USE THEREOF AS PHOSPHATIDYLINOSITOL-3-KINASE INHIBITORS 审中-公开
标题翻译：氧杂环丁烷-2-酮嘧啶衍生物及其作为磷酸胆碱-3-激酶抑制剂的用途
公开(公告)号：US20160168145A1
公开(公告)日：2016-06-16
申请号：US15047574
申请日：2016-02-18
申请人： Robin Alec Fairhurst , Pascal Furet , Frank Stephen Kalthoff , Andreas Lerchner , Heinrich Rueeger
发明人： Robin Alec Fairhurst , Pascal Furet , Frank Stephen Kalthoff , Andreas Lerchner , Heinrich Rueeger
IPC分类号： C07D417/14 , A61K31/5377
CPC分类号： C07D417/14 , A61K31/5377 , A61K45/06 , C07D413/14
摘要： The present invention relates to oxazolidin-2-one substituted pyrimidine compounds that act as PI3K (phosphatidylinositol-3-kinase) inhibitors, as well as pharmaceutical compositions thereof, methods for their manufacture and uses for the treatment of conditions, diseases and disorders dependent on PI3K.
摘要翻译：本发明涉及作为PI3K（磷脂酰肌醇-3-激酶）抑制剂的恶唑烷-2-酮取代的嘧啶化合物及其药物组合物，其制备方法和用于治疗依赖于 PI3K。

9. 发明申请

US20140256715A1 Novel Oxazine Derivatives and their use in the Treatment of Disease 有权
标题翻译：新型恶嗪衍生物及其在疾病治疗中的应用
公开(公告)号：US20140256715A1
公开(公告)日：2014-09-11
申请号：US14350938
申请日：2012-10-11
申请人： Konstanze Hurth , Sebastien Jacquier , Rainer Machauer , Heinrich Rueeger , Marina Tintelnot-Blomley , Siem Jacob Veenstra , Markus Voegtle
发明人： Konstanze Hurth , Sebastien Jacquier , Rainer Machauer , Heinrich Rueeger , Marina Tintelnot-Blomley , Siem Jacob Veenstra , Markus Voegtle
IPC分类号： C07D265/30 , A61K31/5377 , C07D487/04 , A61K31/5375 , C07D471/04 , C07D417/12 , C07D413/12
CPC分类号： C07D265/30 , A61K31/5375 , A61K31/5377 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/12 , C07D471/04 , C07D487/04
摘要： The invention relates to novel oxazine derivatives of formula (I), and pharmaceutically acceptable salts thereof, in which all of the variables are as defined in the specification, pharmaceutical compositions thereof, combinations thereof, and their use as medicaments, particularly for the treatment of Alzheimer's Disease or diabetes via inhibition of BACE-1 or BACE-2.
摘要翻译：本发明涉及式（I）的新的恶嗪衍生物及其药学上可接受的盐，其中所有变量如说明书，其药物组合物，其组合，及其作为药物的用途，特别是用于治疗通过BACE-1或BACE-2的抑制来治疗阿尔茨海默病或糖尿病。

10. 发明申请

US20140107118A1 Novel Heterocyclic Derivatives and Their Use in the Treatment of Neurological Disorders 有权
标题翻译：新型杂环衍生物及其在神经障碍治疗中的应用
公开(公告)号：US20140107118A1
公开(公告)日：2014-04-17
申请号：US14136855
申请日：2013-12-20
申请人： Sangamesh BADIGER , Murali CHEBROLU , Konstanze HURTH , Sebastien JACQUIER , Rainer Martin LUEOEND , Rainer MACHAUER , Heinrich RUEEGER , Marina TINTELNOT-BLOMLEY , Siem Jacob VEENSTRA , Markus VOEGTLE
发明人： Sangamesh BADIGER , Murali CHEBROLU , Konstanze HURTH , Sebastien JACQUIER , Rainer Martin LUEOEND , Rainer MACHAUER , Heinrich RUEEGER , Marina TINTELNOT-BLOMLEY , Siem Jacob VEENSTRA , Markus VOEGTLE
IPC分类号： C07D413/14 , C07D487/04 , C07D471/04 , A61K31/5377
CPC分类号： C07D413/14 , A61K31/5377 , C07B59/002 , C07B2200/05 , C07D471/04 , C07D487/04 , A61K2300/00
摘要： The invention relates to novel heterocyclic compounds of the formula in which all of the variables are as defined in the specification, pharmaceutical compositions thereof, combinations thereof, and their use as medicaments, particularly for the treatment of Alzheimer's Disease or diabetes via inhibition of BACE-1 or BACE-2.
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，其药物组合物，其组合及其作为药物的用途，特别是用于通过BACE-抑制剂的抑制治疗阿尔茨海默病或糖尿病， 1或BACE-2。

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