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2. 发明申请

WO2010141273A1 DERIVATIVES OF 6,7-DIHYDRO-5H-IMIDAZO[1,2-a]IMIDAZOLE-3-CARBOXYLIC ACID AMIDES 审中-公开
标题翻译： 6,7-二氢-5H-咪唑并[1,2-a]咪唑-3-羧酸酰胺的衍生物
公开(公告)号：WO2010141273A1
公开(公告)日：2010-12-09
申请号：PCT/US2010/036094
申请日：2010-05-26
申请人： BOEHRINGER INGELHEIM INTERNATIONAL GMBH , LEMIEUX, Rene, Marc , BRUNETTE, Steven, Richard , HORAN, Joshua, Courtney , KOWALSKI, Jennifer, A. , LAWLOR, Michael, David , MCKIBBEN, Bryan , MILLER, Craig, Andrew , BARBOSA, Antonio, J.M.
发明人： LEMIEUX, Rene, Marc , BRUNETTE, Steven, Richard , HORAN, Joshua, Courtney , KOWALSKI, Jennifer, A. , LAWLOR, Michael, David , MCKIBBEN, Bryan , MILLER, Craig, Andrew , BARBOSA, Antonio, J.M.
IPC分类号： C07D471/04 , C07D487/04 , A61K31/4439 , A61K31/501 , A61K31/4375 , A61K31/506 , A61P29/00
CPC分类号： C07D487/04 , C07D519/00
摘要： Derivatives of 6,7-dihydro-5H-imidazo[1,2- a ]imidazole-3-carboxylic acid amide exhibit good inhibitory effect upon the interaction of CAMs and Leukointegrins and are thus useful in the treatment of inflammatory disease.
摘要翻译： 6,7-二氢-5H-咪唑并[1,2-a]咪唑-3-羧酸酰胺的衍生物对CAM和白血球整合素的相互作用表现出良好的抑制作用，因此可用于治疗炎性疾病。

3. 发明申请

WO2006107923A1 SUBSTITUTED BENZYLIMIDAZOLES USEFUL FOR THE TREATMENT OF INFLAMMATORY DISEASES 审中-公开
标题翻译：用于治疗炎症性疾病的替代苄基咪唑
公开(公告)号：WO2006107923A1
公开(公告)日：2006-10-12
申请号：PCT/US2006/012431
申请日：2006-04-04
申请人： BOEHRINGER INGELHEIM INTERNATIONAL GMBH , BOEHRINGER INGELHEIM PHARMA GMBH & CO. KG , KIM, Jin, Mi , LEMIEUX, Rene, Marc , MCKIBBEN, Bryan , TSCHANTZ, Matt, Aaron , YU, Hui
发明人： KIM, Jin, Mi , LEMIEUX, Rene, Marc , MCKIBBEN, Bryan , TSCHANTZ, Matt, Aaron , YU, Hui
IPC分类号： C07D401/12 , C07D401/14 , C07D233/54 , C07D233/88 , C07D233/70 , A61K31/415 , A61K31/454 , A61P29/00
CPC分类号： C07D233/64 , C07D233/70 , C07D233/88 , C07D401/12 , C07D401/14
摘要： The invention comprises a class of derivatives of substituted benzylimidazoles of the formula (I) and methods for making the same. These compounds are useful for the treatment of inflammatory conditions.
摘要翻译：本发明包括一类式（I）的取代苄基咪唑衍生物及其制备方法。这些化合物可用于治疗炎性病症。

4. 发明申请

WO2006014482A1 PYRIMIDINE DERIVATIVES USEFUL AS INHIBITORS OF PKC-THETA 审中-公开
标题翻译：用作PKC-THETA的抑制剂的吡嗪衍生物有用
公开(公告)号：WO2006014482A1
公开(公告)日：2006-02-09
申请号：PCT/US2005/023969
申请日：2005-07-06
申请人： BOEHRINGER INGELHEIM PHARMACEUTICALS, INC. , BARBOSA, Antonio, J.M., Jr. , BRUNETTE, Steven, Richard , HICKEY, Eugene, Richard , KIM, Jin Mi , LAWLOR, Michael, David , LEMIEUX, Rene, Marc , MCKIBBEN, Bryan , TSCHANTZ, Matt, Aaron , YU, Hui
发明人： BARBOSA, Antonio, J.M., Jr. , BRUNETTE, Steven, Richard , HICKEY, Eugene, Richard , KIM, Jin Mi , LAWLOR, Michael, David , LEMIEUX, Rene, Marc , MCKIBBEN, Bryan , TSCHANTZ, Matt, Aaron , YU, Hui
IPC分类号： C07D239/48
CPC分类号： C07D239/48 , C07D401/12 , C07D403/12
摘要： Disclosed are novel compounds of formula: (I); wherein X, Y, R 1 , R 2 and R 3 are as defined herein, which are useful as inhibitors of PKC-theta and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of PKC-theta, including immunological disorders and type II diabetes. This invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
摘要翻译：公开了式（I）的新化合物：其中X，Y，R

5. 发明申请

WO2014179186A1 ALDOSTERONE SYNTHASE INHIBITORS 审中-公开
公开(公告)号：WO2014179186A1
公开(公告)日：2014-11-06
申请号：PCT/US2014/035596
申请日：2014-04-28
申请人： BOEHRINGER INGELHEIM INTERNATIONAL GMBH , BALESTRA, Michael , BURKE, Jennifer , CHEN, Zhidong , COGAN, Derek , FADER, Lee , GUO, Xin , MCKIBBEN, Bryan , MARSHALL, Daniel Richard , NEMOTO, Peter Allen , YU, Hui
发明人： BALESTRA, Michael , BURKE, Jennifer , CHEN, Zhidong , COGAN, Derek , FADER, Lee , GUO, Xin , MCKIBBEN, Bryan , MARSHALL, Daniel Richard , NEMOTO, Peter Allen , YU, Hui
IPC分类号： C07D471/04 , A61K31/444 , C07D498/04 , A61P9/00
CPC分类号： C07D498/04 , C07D471/04
摘要： The present invention relates to compounds of formula (I): I and pharmaceutically acceptable salts thereof, wherein R 1 , R 2 , R3, R4, R5, R 6 , R 7 , W, Y, m and n are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of a variety of diseases that are mediated or sustained by aldosterone activity, including renal disease, diabetic nephropathy, cardiovascular diseases and fibrotic disorders, processes for preparing these compounds and intermediates useful in these processes.
摘要翻译：本发明涉及式（I）化合物：I及其药学上可接受的盐，其中R 1，R 2，R 3，R 4，R 5，R 6，R 7，W，Y，本发明还涉及包含这些化合物的药物组合物，使用这些化合物治疗由醛固酮活性介导或维持的各种疾病的方法，包括肾脏疾病，糖尿病性肾病，心血管疾病和纤维化疾病，制备这些化合物的方法在这些方法中有用的化合物和中间体。

6. 发明申请

WO2013191984A1 FUSED THIAZIN-3-ONES AS KCA3.1 INHIBITORS 审中-公开
标题翻译：作为KCA3.1抑制剂加热的THIAZIN-3-ONES
公开(公告)号：WO2013191984A1
公开(公告)日：2013-12-27
申请号：PCT/US2013/045405
申请日：2013-06-12
申请人： BOEHRINGER INGELHEIM INTERNATIONAL GMBH , BURKE, Michael J. , MCKIBBEN, Bryan , TSCHANTZ, Matt Aaron
发明人： BURKE, Michael J. , MCKIBBEN, Bryan , TSCHANTZ, Matt Aaron
IPC分类号： C07D513/04 , A61K31/542 , A61P29/00
CPC分类号： C07D513/04
摘要： The present invention encompasses compounds of the formulas (I) &(II), wherein the groups A, L and Ar are defined as in claim 1, which are suitable for the treatment of diseases related to KCa3.1, process of making, pharmaceutical preparations which contain compounds and their methods of use.
摘要翻译：本发明包括式（I）和（II）的化合物，其中基团A，L和Ar如权利要求1中所定义，其适用于治疗与KCa3.1相关的疾病，制备方法，制剂含有化合物及其使用方法的制剂。

8. 发明公开

EP2225238A1 DERIVATIVES OF 6,7-DIHYDRO-5H-IMIDAZOÝ1,2- ¨IMIDAZOLE-3- CARBOXYLIC ACID AMIDES 有权
标题翻译：衍生物6,7-二氢-5H-咪唑并[1,2-A] - 咪唑烷-3-羧酸钠
公开(公告)号：EP2225238A1
公开(公告)日：2010-09-08
申请号：EP08853791.5
申请日：2008-11-20
申请人： Boehringer Ingelheim International GmbH , Boehringer Ingelheim Pharma GmbH & Co. KG
发明人： LEMIEUX, Rene M. , BARBOSA, Antonio Jose Del Moral , BENTZIEN, Joerg Martin , BRUNETTE, Steven Richard , CHEN, Zhidong , COGAN, Derek , GAO, Donghong A. , HEIM-RIETHER, Alexander , HORAN, Joshua Courtney , KOWALSKI, Jennifer A. , LAWLOR, Michael David , LIU, Weimin , MCKIBBEN, Bryan , MILLER, Craig Andrew , MOSS, Neil , TSCHANTZ, Matt Aaron , XIONG, Zhaoming , YU, Hui , YU, Yang
IPC分类号： C07D471/04 , C07D487/04 , A61K31/519 , A61P29/00
CPC分类号： C07D487/04
摘要： Derivatives of 6,7-dihydro-5H-imidazo[1,2-α]imidazole-3-carboxylic acid amide exhibit good inhibitory effect upon the interaction of CAMs and Leukointegrins and are thus useful in the treatment of inflammatory disease.

9. 发明公开

EP1869012A1 SUBSTITUTED BENZYLIMIDAZOLES USEFUL FOR THE TREATMENT OF INFLAMMATORY DISEASES 审中-公开
标题翻译：取代benzylimidazoles炎症性疾病的治疗
公开(公告)号：EP1869012A1
公开(公告)日：2007-12-26
申请号：EP06740459.0
申请日：2006-04-04
申请人： Boehringer Ingelheim International GmbH , Boehringer Ingelheim Pharma GmbH & Co. KG
发明人： KIM, Jin, Mi , LEMIEUX, Rene, Marc , MCKIBBEN, Bryan , TSCHANTZ, Matt, Aaron , YU, Hui
IPC分类号： C07D401/12 , C07D401/14 , C07D233/54 , C07D233/88 , C07D233/70 , A61K31/415 , A61K31/454 , A61P29/00
CPC分类号： C07D233/64 , C07D233/70 , C07D233/88 , C07D401/12 , C07D401/14
摘要： The invention comprises a class of derivatives of substituted benzylimidazoles of the formula (I) and methods for making the same. These compounds are useful for the treatment of inflammatory conditions.

10. 发明申请

WO2003053366A2 PYRIMIDINE A2B SELECTIVE ANTAGONIST COMPOUNDS, THEIR SYNTHESIS AND USE 审中-公开
标题翻译： PYRIMIDINE A2B选择性拮抗剂化合物，其合成和用途
公开(公告)号：WO2003053366A2
公开(公告)日：2003-07-03
申请号：PCT/US2002/041273
申请日：2002-12-20
申请人： OSI PHARMACEUTICALS, INC. , CASTELHANO, Arlindo , MCKIBBEN, Bryan , STEINIG, Arno , COLLINGTON, Eric, William
发明人： CASTELHANO, Arlindo , MCKIBBEN, Bryan , STEINIG, Arno , COLLINGTON, Eric, William
IPC分类号： A61K
CPC分类号： C07D239/48 , C07D401/12 , C07D403/12
摘要： The subject invention provides compounds having the structure:, wherein R 1 is substituted or unsubstituted phenyl or a 5-6 membered heterocyclic or heteroaromatic ring containing from 1 to 5 heteroatoms; R 2 is hydrogen, or a substituted or unsubstituted alkyl, -C(O)-alkyl, -C(O)-O-alkyl, alkoxy, cycloalkyl, alkenyl, monocyclic or bicyclic aryl, heteroaryl or heterocyclic moiety; R 3 is hydrogen, or a substituted or unsubstituted alkyl, -C(O)-alkyl, -C(O)-O-alkyl, alkoxy, cycloalkyl, alkenyl, monocyclic or bicyclic aryl, heteroaryl or heterocyclic moiety, or R 2 and R 3 are joined to form a heterocyclic ring; wherein the dashed line represents a second bond which may be present or absent, and when present R 3 is oxygen; R 4 and R 5 are each independently substituted or unsubstituted alkyl, -C(O)-alkyl, -C(O)-O-alkyl, alkoxy, cycloalkyl, alkenyl, monocyclic or bicyclic aryl, heteroaryl or heterocyclic moiety, or R 4 NR 5 together form a substituted or unsubstituted monocyclic or bicyclic, heterocyclic or heteroaryl moiety containing from 1 to 6 heteroatoms; R 12 is hydrogen, alkyl, halogen or cyano; and n is 0, 1, 2, 3 or 4, or an enantiomer, or a specific tautomer, or a pharmaceutically acceptable salt thereof and a method for treating a disease associated with the A 2b adenosine receptor by administering a therapeutically effective amount of the compounds of the invention.
摘要翻译：本发明提供具有以下结构的化合物：其中R 1是取代或未取代的苯基或含有1至5个杂原子的5-6元杂环或杂芳族环; R 2是氢或取代或未取代的烷基，-C（O） - 烷基，-C（O）-O-烷基，烷氧基，环烷基，链烯基，单环或双环芳基，杂芳基或杂环部分; R 3是氢或取代或未取代的烷基，-C（O） - 烷基，-C（O）-O-烷基，烷氧基，环烷基，烯基，单环或双环芳基，杂芳基或杂环部分或R 17和R 34连接形成杂环; 其中虚线表示可以存在或不存在的第二键，并且当存在时，R 3是氧; R 4和R 15各自独立地是取代或未取代的烷基，-C（O） - 烷基，-C（O）-O-烷基，烷氧基，环烷基，烯基，单环或双环芳基，杂芳基或杂环部分，或者R 4，R 6，R 15一起形成含有1至6个杂原子的取代或未取代的单环或双环，杂环或杂芳基部分 ; R 12是氢，烷基，卤素或氰基; 和n为0,1,2,3或4，或其对映异构体，或其特异的互变异构体或其药学上可接受的盐，以及通过以下方式治疗与Aβ2b2腺苷受体相关的疾病的方法：施用治疗有效量的本发明化合物。

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