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1. 发明公开

EP1986645A1 GLUCOKINASE ACTIVATORS 有权
标题翻译：葡糖激酶活化剂
公开(公告)号：EP1986645A1
公开(公告)日：2008-11-05
申请号：EP07716991.0
申请日：2007-01-24
申请人： Array Biopharma, Inc. , Aicher, Thomas Daniel , BOYD, Steven Armen , Chicarelli, Mark Joseph , Condroski, Kevin Ronald , Hinklin, Ronald Jay , Singh, Ajay , Turner, Timothy Mark , Rustam, Ferdinand Garrey
发明人： AICHER, Thomas, Daniel , BOYD, Steven, Armen , CHICARELLI, Mark, Joseph , CONDROSKI, Kevin, Ronald , HINKLIN, Ronald, J. , SINGH, Ajay , TURNER, Timothy, Mark , RUSTAM, Ferdinand, Garrey
IPC分类号： A61K31/427 , C07D417/12 , C07D417/14 , C07D471/04 , C07D487/04 , C07D495/04 , C07D498/04 , C07D513/04 , A61P3/10 , A61K31/428
CPC分类号： C07D417/12 , C07D417/14 , C07D471/04 , C07D487/04 , C07D495/04 , C07D513/04
摘要： Provided are compounds of formula I that are useful in the treatment and/or prevention of diseases mediated by deficient levels of glucokinase activity, such as diabetes mellitus. Also provided are methods of treating or preventing diseases and disorders characterized by underactivity of glucokinase or which can be treated by activating glucokinase. (Formula I) wherein R2, L, Z, Y, G and R1 are as defined in the claims.
摘要翻译：提供可用于治疗和/或预防由葡萄糖激酶活性水平不足（例如糖尿病）介导的疾病的式I化合物。还提供治疗或预防葡萄糖激酶活性降低或可通过激活葡萄糖激酶进行治疗的疾病和病症的方法。（式I）其中R2，L，Z，Y，G和R1如权利要求中所定义。

2. 发明申请

WO2009042435A8 PYRIDIN-2 -YL-AMINO-I, 2, 4 -THIADIAZOLE DERIVATIVES AS GLUCOKINASE ACTIVATORS FOR THE TREATMENT OF DIABETES MELLITUS 审中-公开
标题翻译：吡啶-2-基氨基-1,2,4-噻二唑衍生物作为用于治疗糖尿病的葡糖激酶活化剂
公开(公告)号：WO2009042435A8
公开(公告)日：2009-10-08
申请号：PCT/US2008076401
申请日：2008-09-15
申请人： ARRAY BIOPHARMA INC , AICHER THOMAS DANIEL , BOYD STEVEN ARMEN , CHICARELLI MARK JOSEPH , CONDROSKI KEVIN RONALD , FELL JAY BRADFORD , FISCHER JOHN P , GUNAWARDANA INDRANI W , HINKLIN RONALD JAY , SINGH AJAY , TURNER TIMOTHY M , WALLACE ELI M
发明人： AICHER THOMAS DANIEL , BOYD STEVEN ARMEN , CHICARELLI MARK JOSEPH , CONDROSKI KEVIN RONALD , FELL JAY BRADFORD , FISCHER JOHN P , GUNAWARDANA INDRANI W , HINKLIN RONALD JAY , SINGH AJAY , TURNER TIMOTHY M , WALLACE ELI M
IPC分类号： C07D417/12 , A61K31/433 , A61P3/10 , C07D417/14
CPC分类号： C07D401/14 , C07D213/75 , C07D401/12 , C07D417/12 , C07D417/14
摘要： Provided are compounds of Formula (I): wherein R2, R3, R13, L and D2 are as defined in the specification, which are useful in the treatment and/or prevention of diseases or disorders mediated by deficient levels of glucokinase activity or which can be treated by activating glucokinase including, but not limited to, diabetes mellitus, impaired glucose tolerance, IFG (impaired fasting glucose) and IFG (impaired fasting glycemia), as well as other diseases and disorders such as those discussed herein.
摘要翻译：提供了式（I）的化合物：其中R 2，R 3，R 13，L和D 2如说明书中所定义，其可用于治疗和/或预防由葡萄糖激酶活性水平不足所介导的疾病或病症，通过激活包括但不限于糖尿病，葡萄糖耐量降低，IFG（空腹葡萄糖受损）和IFG（空腹血糖受损）以及其他疾病和病症（例如本文讨论的那些）的葡萄糖激酶来治疗。

3. 发明申请

WO2008118718A3 2-AMINOPYRIDINE ANALOGS AS GLUCOKINASE ACTIVATORS 审中-公开
标题翻译： 2-氨基吡啶类似物作为GLUCOKINASE激活剂
公开(公告)号：WO2008118718A3
公开(公告)日：2008-11-13
申请号：PCT/US2008057543
申请日：2008-03-19
申请人： ARRAY BIOPHARMA INC , AICHER THOMAS DANIEL , BOYD STEVEN ARMEN , CHICARELLI MARK JOSEPH , CONDROSKI KEVIN RONALD , HINKLIN RONALD JAY , SINGH AJAY
发明人： AICHER THOMAS DANIEL , BOYD STEVEN ARMEN , CHICARELLI MARK JOSEPH , CONDROSKI KEVIN RONALD , HINKLIN RONALD JAY , SINGH AJAY
IPC分类号： C07D417/14 , A61K31/427 , A61K31/4427 , A61P3/10 , C07D471/04 , C07D495/04 , C07D498/04
CPC分类号： C07D417/14 , C07D471/04 , C07D495/04 , C07D498/04
摘要： Provided are compounds of formula (I) that are useful in the treatment and/or prevention of diseases mediated by deficient levels of glucokinase activity, such as diabetes mellitus. Also provided are methods of treating or preventing diseases and disorders characterized by underactivity of glucokinase or which can be treated by activating glucokinase.
摘要翻译：提供式（I）化合物，其可用于治疗和/或预防由缺乏水平的葡糖激酶活性（例如糖尿病）介导的疾病。还提供了治疗或预防以葡萄糖激酶不足活性为特征的疾病和病症的方法，或者可以通过激活葡糖激酶治疗。

4. 发明申请

WO2006049952A1 CYCLOALKYL LACTAM DERIVATIVES AS INHIBITORS OF 11-BETA-HYDROXYSTEROID DEHYDROGENASE 1 审中-公开
标题翻译：作为11-羟基脱氢酶脱氢酶1的抑制剂的环丙基乳糖衍生物
公开(公告)号：WO2006049952A1
公开(公告)日：2006-05-11
申请号：PCT/US2005/038369
申请日：2005-10-26
申请人： ELI LILLY AND COMPANY , AICHER, Thomas, D. , CHICARELLI, Mark, Joseph , HINKLIN, Ronald, Jay , TIAN, Hongqi , WALLACE, Owen, Brendan , CHEN, Zhaogen , MABRY, Thomas, Edward , MCCOWAN, Jefferson, Ray , SNYDER, Nancy, June , WINNEROSKI, Leonard, Larry, Junior , ALLEN, John, Gordon
发明人： AICHER, Thomas, D. , CHICARELLI, Mark, Joseph , HINKLIN, Ronald, Jay , TIAN, Hongqi , WALLACE, Owen, Brendan , CHEN, Zhaogen , MABRY, Thomas, Edward , MCCOWAN, Jefferson, Ray , SNYDER, Nancy, June , WINNEROSKI, Leonard, Larry, Junior , ALLEN, John, Gordon
IPC分类号： A61K31/4015 , C07D207/27 , C07D211/76 , C07D401/10 , C07D403/10 , C07D409/10 , A61K31/4025 , A61K31/4412 , A61P3/04
CPC分类号： C07D403/12 , C07D207/26 , C07D207/267 , C07D207/273 , C07D211/76 , C07D401/10 , C07D401/12 , C07D403/10 , C07D405/04 , C07D409/04 , C07D409/10
摘要： The present invention discloses compounds of Formula I: (I) having 11beta -HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I, as well as the use of the Fomula I and compositions as medicaments to treat diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, Syndrome X, and other conditions associated with hyperglycemia.
摘要翻译：本发明公开了具有11β-HSD 1型拮抗剂活性的式I化合物：（I），以及制备这些化合物的方法。在另一个实施方案中，本发明公开了包含式I化合物的药物组合物，以及作为药物用于治疗糖尿病，高血糖症，肥胖症，高血压，高脂血症，综合征X和与高血糖相关的其它病症的组合物I和组合物的用途。

5. 发明申请

WO2008118718A2 2-AMINOPYRIDINE ANALOGS AS GLUCOKINASE ACTIVATORS 审中-公开
标题翻译： 2-氨基吡啶类似物作为GLUCOKINASE激活剂
公开(公告)号：WO2008118718A2
公开(公告)日：2008-10-02
申请号：PCT/US2008/057543
申请日：2008-03-19
申请人： ARRAY BIOPHARMA INC. , AICHER, Thomas, Daniel , BOYD, Steven, Armen , CHICARELLI, Mark, Joseph , CONDROSKI, Kevin, Ronald , HINKLIN, Ronald, Jay , SINGH, Ajay
发明人： AICHER, Thomas, Daniel , BOYD, Steven, Armen , CHICARELLI, Mark, Joseph , CONDROSKI, Kevin, Ronald , HINKLIN, Ronald, Jay , SINGH, Ajay
IPC分类号： C07D417/14 , C07D471/04 , C07D495/04 , C07D498/04 , A61P3/10 , A61K31/427 , A61K31/4427
CPC分类号： C07D417/14 , C07D471/04 , C07D495/04 , C07D498/04
摘要： Provided are compounds that are useful in the treatment and/or prevention of diseases mediated by deficient levels of glucokinase activity, such as diabetes mellitus. Also provided are methods of treating or preventing diseases and disorders characterized by underactivity of glucokinase or which can be treated by activating glucokinase.
摘要翻译：提供了可用于治疗和/或预防由缺乏水平的葡糖激酶活性（例如糖尿病）介导的疾病的化合物。还提供了治疗或预防以葡萄糖激酶不足活性为特征的疾病和病症的方法，或者可以通过激活葡糖激酶治疗。

6. 发明申请

WO2007117381A9 2 -AMINOPYRIDINE ANALOGS AS GLUCOKINASE ACTIVATORS 审中-公开
标题翻译： 2-氨基吡啶类似物作为葡糖激酶活化剂
公开(公告)号：WO2007117381A9
公开(公告)日：2008-03-27
申请号：PCT/US2007007444
申请日：2007-03-23
申请人： ARRAY BIOPHARMA INC , AICHER THOMAS DANIEL , BOYD STEVEN ARMEN , CHICARELLI MARK JOSEPH , CONDROSKI KEVIN RONALD , HINKLIN RONALD JAY , SINGH AJAY
发明人： AICHER THOMAS DANIEL , BOYD STEVEN ARMEN , CHICARELLI MARK JOSEPH , CONDROSKI KEVIN RONALD , HINKLIN RONALD JAY , SINGH AJAY
IPC分类号： C07D417/12 , C07D417/14 , C07D471/04 , C07D487/04 , C07D491/04 , C07D495/04 , C07D498/04 , C07D513/04
CPC分类号： C07D417/12 , C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04 , C07D491/04 , C07D495/04 , C07D513/04
摘要： Provided are compounds of formula I that are useful in the treatment and/or prevention of diseases mediated by deficient levels of glucokinase activity, such as diabetes meilitus. Also provided are methods of treating or preventing diseases and disorders characterized by underactivity of glucokinase or which can be treated by activating glucokinase.
摘要翻译：提供可用于治疗和/或预防由葡萄糖激酶活性水平不足（例如糖尿病）引起的疾病的式I化合物。还提供治疗或预防葡萄糖激酶活性降低或可通过激活葡萄糖激酶进行治疗的疾病和病症的方法。

7. 发明申请

WO2020081848A1 PROTEIN TYROSINE PHOSPHATASE INHIBITORS 审中-公开
公开(公告)号：WO2020081848A1
公开(公告)日：2020-04-23
申请号：PCT/US2019/056786
申请日：2019-10-17
申请人： ARRAY BIOPHARMA INC. , BLAKE, James F. , BOYS, Mark Laurence , CHICARELLI, Mark Joseph , COOK, Adam , ELSAYED, Mohamed S. A. , FELL, Jay B. , FISCHER, John P. , HINKLIN, Ronald Jay , MCNULTY, Oren T. , MEJIA, Macedonio J. , RODRIGUEZ, Martha E. , WONG, Christina E.
发明人： BLAKE, James F. , BOYS, Mark Laurence , CHICARELLI, Mark Joseph , COOK, Adam , ELSAYED, Mohamed S. A. , FELL, Jay B. , FISCHER, John P. , HINKLIN, Ronald Jay , MCNULTY, Oren T. , MEJIA, Macedonio J. , RODRIGUEZ, Martha E. , WONG, Christina E.
IPC分类号： C07D401/04 , C07D471/04 , C07D519/00 , A61P35/00 , A61K31/498 , A61K31/4985
摘要： Compounds of Formula la or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof are provided, which are useful for the treatment of hyperproliferative diseases in the view of their ability to inhibit SHP2. Methods of using compounds of Formula I or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof, for in vitro , in situ , and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.

8. 发明申请

WO2013130976A1 SERINE/THREONINE KINASE INHIBITORS 审中-公开
标题翻译：丝氨酸/螺旋激酶抑制剂
公开(公告)号：WO2013130976A1
公开(公告)日：2013-09-06
申请号：PCT/US2013/028622
申请日：2013-03-01
申请人： ARRAY BIOPHARMA INC. , GENENTECH, INC. , BLAKE, James F. , CHICARELLI, Mark Joseph , GARREY, Rustam Ferdinand , GAUDINO, John , GRINA, Jonas , MORENO, David A. , MOHR, Peter J. , REN, Li , SCHWARZ, Jacob , CHEN, Huifen , ROBARGE, Kirk , ZHOU, Aihe
发明人： BLAKE, James F. , CHICARELLI, Mark Joseph , GARREY, Rustam Ferdinand , GAUDINO, John , GRINA, Jonas , MORENO, David A. , MOHR, Peter J. , REN, Li , SCHWARZ, Jacob , CHEN, Huifen , ROBARGE, Kirk , ZHOU, Aihe
IPC分类号： C07D401/14 , C07D405/14 , C07D413/14 , C07D401/04 , C07D409/14 , C07D417/14 , C07D471/04 , C07F9/6558 , C07F9/6596 , A61K31/435 , A61K31/506 , A61P29/00 , A61P35/00
CPC分类号： C07D401/04 , A61K31/444 , A61K31/506 , A61K31/513 , A61K31/53 , A61K45/06 , C07D401/14 , C07D403/04 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07F9/65586
摘要： Compounds of Formula I or a stereoisomer, tautomer, prodrug or pharmaceutically acceptable salt thereof are provided, which are useful for the treatment of hyperproliferative, pain and inflammatory diseases. Methods of using compounds of Formula I or a stereoisomer, tautomer, prodrug or pharmaceutically acceptable salt thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.
摘要翻译：提供式I化合物或其立体异构体，互变异构体，前药或其药学上可接受的盐，其可用于治疗过度增生，疼痛和炎性疾病。公开了使用式I化合物或其立体异构体，互变异构体，前药或其药学上可接受的盐在体外，原位和体内诊断，预防或治疗哺乳动物细胞或相关病理状况中的这种病症的方法。

9. 发明申请

WO2008091770A1 2-AMINOPYRIDINE DERIVATIVES AS GLUCOKINASE ACTIVATORS 审中-公开
标题翻译： 2-氨基吡啶衍生物作为GLUCOKINASE激活剂
公开(公告)号：WO2008091770A1
公开(公告)日：2008-07-31
申请号：PCT/US2008/051194
申请日：2008-01-16
申请人： ARRAY BIOPHARMA INC. , AICHER, Thomas Daniel , BOYD, Steven Armen , CHICARELLI, Mark Joseph , CONDROSKI, Kevin Ronald , GARREY, Rustam Ferdinand , HINKLIN, Ronald Jay , SINGH, Ajay , TURNER, Timothy M.
发明人： AICHER, Thomas Daniel , BOYD, Steven Armen , CHICARELLI, Mark Joseph , CONDROSKI, Kevin Ronald , GARREY, Rustam Ferdinand , HINKLIN, Ronald Jay , SINGH, Ajay , TURNER, Timothy M.
IPC分类号： C07D417/14 , C07D495/04 , A61K31/4439
CPC分类号： C07D495/04 , C07D417/14
摘要： Provided are compounds having the Formula (I) or salts thereof, wherein: L is O, S, SO, SO 2 , CHOH, C(O), or CH 2 ; D 2 is CR 12 or N; R 2 is aryl, heteroaryl, saturated or partially unsaturated cycloalkyl, or saturated or partially unsaturated heterocyclyl (optionally substituted with oxo), wherein said aryl, heteroaryl, cycloalkyl and heterocyclyl are monocyclic or bicyclic and are further optionally substituted with one or more groups independently selected from C 1 -C 6 alkyl, F, Cl, Br, I, CF 3 , CN, OR 6 , C(=O)R 6 , C(=O)OR 6 , O(CH 2 ) n C(=O)OR 6 , C(=O)NR 6 R 7 , NO 2 and (1-6C alkyl)OR 6 ; R 3 is H, Br, OR 6 , SR 6 , C(O)OR 6 , C(O)NR 6 R 7 , C(O)R 6 , heteroaryl, or C 1 -C 6 alkyl substituted with one or more groups independently selected from V n -aryl, V n -OR 6 , V n - C(=O)OR 6 and V n -NR 6 R 7 ; R 11 is H or Cl; and R 13 is N-(1 -6C alkanoyl)piperidin-4-yl; that are useful in the treatment and/or prevention of diseases mediated by deficient levels of glucokinase activity, such as diabetes mellitus. Also provided are methods of treating or preventing diseases and disorders characterized by underactivity of glucokinase or which can be treated by activating glucokinase.
摘要翻译：提供具有式（I）或其盐的化合物，其中：L是O，S，SO，SO 2，CHOH，C（O）或CH 2 ; D 是CR 12或N; R 2是芳基，杂芳基，饱和或部分不饱和的环烷基或饱和或部分不饱和的杂环基（任选被氧代取代），其中所述芳基，杂芳基，环烷基和杂环基是单环或双环的，被一个或多个独立地选自C 1 -C 6烷基，F，Cl，Br，I，CF 3 N，CN， C（= O）R 6，C（= O）OR 6，O（CH 2）2， C（= O）OR 6，C（= O）NR 6 R 7，NO 2和（1-6C烷基）OR 6; R 3是H，Br，OR 6，SR 6，C（O）OR 6，C（O） O）NR 6 R 7，C（O）R 6，杂芳基或C 1 -C 6烷基，被一个或多个独立地选自以下的基团取代的亚烷基烷基：V n - 芳基，V n -OR 6，V C（= O）OR 6和V 6和-NR 6 R 7， SUP>; R 11是H或Cl; 和R 13是N-（1-6C烷酰基）哌啶-4-基; 其可用于治疗和/或预防由缺乏水平的葡糖激酶活性（例如糖尿病）介导的疾病。还提供了治疗或预防以葡萄糖激酶不足活性为特征的疾病和病症的方法，或者可以通过激活葡糖激酶治疗。

10. 发明申请

WO2007053345A1 GLUCOKINASE ACTIVATORS 审中-公开
公开(公告)号：WO2007053345A1
公开(公告)日：2007-05-10
申请号：PCT/US2006/041251
申请日：2006-10-24
申请人： ARRAY BIOPHARMA INC. , AICHER, Thomas Daniel , LEE, Wai-Man , HINKLIN, Ronald Jay , CHICARELLI, Mark Joseph , BOYD, Steven Armen , CONDROSKI, Kevin Ronald
发明人： AICHER, Thomas Daniel , LEE, Wai-Man , HINKLIN, Ronald Jay , CHICARELLI, Mark Joseph , BOYD, Steven Armen , CONDROSKI, Kevin Ronald
IPC分类号： C07D417/12 , C07D417/14 , A61K31/4439 , A61P3/10
CPC分类号： C07D417/12 , C07D417/14 , C07D495/04 , C07D513/04
摘要： Provided are compounds of Formula I wherein R 1 , R 2 , Y, Z and G are as defined herein, that are useful in the treatment and/or prevention of diseases mediated by deficient levels of glucokinase activity, such as diabetes mellitus. Also provided are methods of treating or preventing diseases and disorders characterized by underactivity of glucokinase or which can be treated by activating glucokinase.
摘要翻译：提供式I化合物，其中R 1，R 2，Y，Z和G如本文所定义，其可用于治疗和/或预防疾病介导由于葡萄糖激酶活性水平不足，如糖尿病。还提供了治疗或预防以葡萄糖激酶不足活性为特征的疾病和病症的方法，或者可以通过激活葡糖激酶进行治疗。

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