公开(公告)号：US20110137044A1

公开(公告)日：2011-06-09

申请号：US13022243

申请日：2011-02-07

申请人： Gottfried Sedelmeier ,  Stuart John Mickel ,  Heinrich Rueeger

发明人： Gottfried Sedelmeier ,  Stuart John Mickel ,  Heinrich Rueeger

IPC分类号： C07D498/04

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。

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。

公开(公告)号：US08143416B2

公开(公告)日：2012-03-27

申请号：US13022243

申请日：2011-02-07

申请人： Gottfried Sedelmeier ,  Stuart John Mickel ,  Heinrich Rueeger

发明人： Gottfried Sedelmeier ,  Stuart John Mickel ,  Heinrich Rueeger

IPC分类号： C07D263/52

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。

公开(公告)号：US20070208055A1

公开(公告)日：2007-09-06

申请号：US11573790

申请日：2005-08-30

申请人： Gottfried Sedelmeier ,  Stuart Mickel ,  Heinrich Rueeger

发明人： Gottfried Sedelmeier ,  Stuart Mickel ,  Heinrich Rueeger

IPC分类号： A61K31/45 ,  A61K31/165 ,  C07D263/60 ,  C07D211/40

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, C1-4alkanoyloxy-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; R 2是卤素，C 1-4烷基或C 1-4烷氧基; R 3和R 4分别独立地为支链C 3-6烷基; 和R 5是环烷基，C 1-6烷基，C 1-6 1-6羟基烷基，C 1-6烷基， 烷氧基-C 1-6烷基，C 1-4烷酰氧基-C 1-6烷基，C 1-6烷基， 亚氨基烷基，C 1-6烷基氨基-C 1-6烷基，C 1-6二烷基氨基-C 1-6 C 1 -C 6烷基，C 1-6烷酰基氨基-C 1-6烷基，HO（O）C 1-6亚烷基，C C 1 -C 6烷基-O-（O）C 1-6烷基，H 2 NC（O）-C 1 - C 1 -C 6烷基，C 1-6烷基-NH-C（O）-C 1-6烷基或（C 1-6）烷基， （O）-C 1-6烷基;（C 1 -C 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。

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.

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。

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.

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。

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.

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。