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1. 发明申请

WO2010019637A1 CHEMICAL COMPOUNDS 审中-公开
标题翻译：化学化合物
公开(公告)号：WO2010019637A1
公开(公告)日：2010-02-18
申请号：PCT/US2009/053504
申请日：2009-08-12
申请人： SMITHKLINE BEECHAM CORPORATION , ATKINSON, Francis, Louis , AXTEN, Jeffrey, Michael , CICHY-KNIGHT, Maria , MOORE, Michael, Lee , PATEI, Vipulkumar, Kantibhai , TIAN, Xinrong , WELLAWAY, Christopher, Roland , DUNN, Allison, K.
发明人： ATKINSON, Francis, Louis , AXTEN, Jeffrey, Michael , CICHY-KNIGHT, Maria , MOORE, Michael, Lee , PATEI, Vipulkumar, Kantibhai , TIAN, Xinrong , WELLAWAY, Christopher, Roland , DUNN, Allison, K.
IPC分类号： A01N43/90
CPC分类号： C07D471/04
摘要： The invention is directed to pyrido[4,3- d ]pyrimidin-5(6 H )-one derivatives. Specifically, the invention is directed to compounds according to Formula (I) wherein R 1 , R 2 , R 3 , and R 4 are defined below. The compounds of the invention are inhibitors of PDK1 and can be useful in the treatment of disorders characterized by constitutively activated ACG kinases such as cancer and more specifically cancers of the breast, colon, and lung. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting PDK1 activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention
摘要翻译：本发明涉及吡啶并[4,3-d]嘧啶-5（6H） - 酮衍生物。具体地，本发明涉及式（I）的化合物，其中R 1，R 2，R 3和R 4定义如下。本发明的化合物是PDK1的抑制剂，可用于治疗特征在于组成型激活的ACG激酶（例如癌症，更特别是乳腺癌，结肠癌和肺癌）的病症。因此，本发明进一步涉及包含本发明化合物的药物组合物。本发明还涉及使用本发明化合物或包含本发明化合物的药物组合物抑制PDK1活性和与之相关疾病的治疗方法

2. 发明申请

WO2006105475A1 NOVEL COMPOUNDS 审中-公开
标题翻译：新型化合物
公开(公告)号：WO2006105475A1
公开(公告)日：2006-10-05
申请号：PCT/US2006/012247
申请日：2006-03-31
申请人： SMITHKLINE BEECHAM CORPORATION , CICHY-KNIGHT, Maria , DUNN, Allison, K. , MARQUIS, Robert, W.
发明人： CICHY-KNIGHT, Maria , DUNN, Allison, K. , MARQUIS, Robert, W.
IPC分类号： C07D409/12
CPC分类号： C07D413/12 , C07D409/12
摘要： This invention relates to novel compounds useful in the treatment of diseases associated with TRPV4 channel receptor. More specifically, this invention relates to certain substituted morpholines and piperidines, according to Formula I wherein: X is O or CH 2 ; R1 is optionally substituted C 3-7 cycloalkyl, C 3-6 cycloalkyl-C 0-6 alkyl, optionally substituted C 4-7 cycloalkenyl, optionally substituted Het-C 0-7 alkyl, optionally substituted Het-C0 -7 alkenyl, optionally substituted aryl, optionally substituted heterocycloalkyl, or optionally substituted heteroaryl- R2 is H, branched or optionally substituted C 1-6 alkyl, C 3-6 cycloalkyl-C 0-6 alkyl, Ar-C 0-6 alkyl, or Het-C 0-6 alkyl; and R3 is optionally substituted heterocycloalkyl, optionally substituted aryl, or optionally substituted heteroaryl; or pharmaceutically acceptable salts, hydrates, solvates and physiologically functional derivatives thereof.
摘要翻译：本发明涉及可用于治疗与TRPV4通道受体相关的疾病的新化合物。更具体地，本发明涉及根据式I的某些取代的吗啉和哌啶，其中：X是O或CH 2; R1是任选取代的C 3-7环烷基，C 3-6环烷基-C 0-6-6烷基，任选取代的C 4 -7个环烯基，任选取代的Het-C 0-7 - 烷基，任选取代的Het-C 0 - 7 - 链烯基，任选取代的芳基，任选取代的杂环烷基，或任选取代的杂芳基-R 2为H，支链或任选取代的C 1-6烷基，C 3-6环烷基-C 0-6-6烷基，Ar-C 0-6-C 1-6烷基或Het-C 0-6-烷基; 并且R 3是任选取代的杂环烷基，任选取代的芳基或任选取代的杂芳基; 或其药学上可接受的盐，水合物，溶剂化物和生理功能衍生物。

3. 发明申请

WO2006052722A1 GLYCOGEN PHOSPHORYLASE INHIBITOR COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS THEREOF 审中-公开
标题翻译： GLYCOGEN PHOSPHORYLASE抑制剂化合物及其药物组合物
公开(公告)号：WO2006052722A1
公开(公告)日：2006-05-18
申请号：PCT/US2005/039956
申请日：2005-11-04
申请人： SMITHKLINE BEECHAM CORPORATION , EVANS, Karen , CICHY-KNIGHT, Maria , COPPO, Frank, Teen , DWORNIK, Kate, Ann , GALE, Jennifer, Paul , GARRIDO, Dulce, Maria , LI, Yue, Hu , PATEL, Mehul, P. , TAVARES, Francis X , THOMSON, Stephen, Andrew , DICKERSON, Scott, Howard , PEAT, Andrew, James , SPARKS, Steven, Meagher , BANKER, Pierette , COOPER, Joel, P.
发明人： EVANS, Karen , CICHY-KNIGHT, Maria , COPPO, Frank, Teen , DWORNIK, Kate, Ann , GALE, Jennifer, Paul , GARRIDO, Dulce, Maria , LI, Yue, Hu , PATEL, Mehul, P. , TAVARES, Francis X , THOMSON, Stephen, Andrew , DICKERSON, Scott, Howard , PEAT, Andrew, James , SPARKS, Steven, Meagher , BANKER, Pierette , COOPER, Joel, P.
IPC分类号： C07C275/28 , C07C275/30 , C07C273/18 , C07C233/87 , C07D221/08 , C07D213/82 , C07D333/38 , A61K31/17 , A61P3/10
CPC分类号： C07C275/42 , C07C237/42 , C07C323/59 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2601/18 , C07C2602/08 , C07D207/16 , C07D209/20 , C07D211/34 , C07D211/56 , C07D211/66 , C07D211/78 , C07D213/56 , C07D213/82 , C07D233/64 , C07D239/26 , C07D261/08 , C07D261/14 , C07D277/56 , C07D307/68 , C07D307/79 , C07D309/14 , C07D317/50 , C07D319/18 , C07D333/24 , C07D333/38 , C07D333/68 , C07D333/70 , C07D335/02 , C07D409/04
摘要： The invention relates to glycogen phosphorylase inhibitor compounds, pharmaceutical compositions of these compounds, methods of treatment using the pharmaceutical compositions to treat diabetes, conditions associated with diabetes, and/or tissue ischemia, including myocardial ischemia, and processes for making the compounds.
摘要翻译：本发明涉及糖原磷酸化酶抑制剂化合物，这些化合物的药物组合物，使用药物组合物治疗糖尿病的方法，与糖尿病有关的病症和/或组织缺血，包括心肌缺血，以及制备该化合物的方法。

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