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1. 发明申请

WO2011006074A1 SUBSTITUTED PYRAZOLO[1,5-a]PYRIMIDINE COMPOUNDS AS TRK KINASE INHIBITORS 审中-公开
标题翻译：取代的吡唑并[1,5-a]吡嗪化合物作为TRK激酶抑制剂
公开(公告)号：WO2011006074A1
公开(公告)日：2011-01-13
申请号：PCT/US2010/041538
申请日：2010-07-09
申请人： ARRAY BIOPHARMA INC. , ALLEN, Shelley , ANDREWS, Steven S. , CONDROSKI, Kevin Ronald , HAAS, Julia , HUANG, Lily , JIANG, Yutong , KERCHER, Timothy , SEO, Jeongbeob
发明人： ALLEN, Shelley , ANDREWS, Steven S. , CONDROSKI, Kevin Ronald , HAAS, Julia , HUANG, Lily , JIANG, Yutong , KERCHER, Timothy , SEO, Jeongbeob
IPC分类号： C07D487/04 , A61K31/519 , C07D519/00
CPC分类号： C07D487/04 , A61K31/519 , A61K31/5377 , C07D453/02 , C07D471/22 , C07D498/22 , C07D519/00
摘要： Compounds of Formula (I) and salts thereof in which R 1 , R 2 , R 3 , R 4 , X, Y and n have the meanings given in the specification, are inhibitors of Trk kinases and are useful in the treatment of diseases which can be treated with a Trk kinase inhibitor such as pain, cancer, inflammation, neurodegenerative diseases and certain infectious diseases.
摘要翻译：其中R1，R2，R3，R4，X，Y和n具有本说明书中给出的含义的式（I）化合物及其盐是Trk激酶的抑制剂，可用于治疗可用一种Trk激酶抑制剂，如疼痛，癌症，炎症，神经变性疾病和某些传染病。

2. 发明申请

WO2009042435A1 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：作为用于治疗糖尿病的GLUCOKINASE激活剂的吡啶-2-基氨基-1,2,4-噻二唑衍生物
公开(公告)号：WO2009042435A1
公开(公告)日：2009-04-02
申请号：PCT/US2008/076401
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 , C07D417/14 , A61K31/433 , A61P3/10
CPC分类号： C07D401/14 , C07D213/75 , C07D401/12 , C07D417/12 , C07D417/14
摘要： Provided are compounds of Formula (I): wherein R 2 , R 3 , R 13 , L and D 2 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：提供式（I）的化合物：其中R2，R3，R13，L和D2如说明书中所定义，其可用于治疗和/或预防由缺乏葡萄糖激酶水平的活性介导的疾病或病症，或可以通过激活葡糖激酶，包括但不限于糖尿病，葡萄糖耐量降低，IFG（空腹血糖受损）和IFG（空腹血糖受损））以及其它疾病和病症如本文讨论的疾病和病症。

3. 发明申请

WO2005037214A2 MACROCYCLIC CARBOXYLIC ACIDS AND ACYLSULFONAMIDES AS INHIBITORS OF HCV REPLICATION 审中-公开
标题翻译：作为HCV复制抑制剂的大环羧酸和乙酰磺胺
公开(公告)号：WO2005037214A2
公开(公告)日：2005-04-28
申请号：PCT/US2004/033970
申请日：2004-10-13
申请人： INTERMUNE, INC. , ARRAY BIOPHARMA INC.
发明人： BLATT, Lawrence M. , WENGLOWSKY, Steven Mark , ANDREWS, Steven Wade , JIANG, Yutong , KENNEDY, April Layne , CONDROSKI, Kevin Ronald , JOSEY, John Anthony , STENGEL, Peter John , MADDURU, Machender R. , DOHERTY, George Andrew , WOODARD, Benjamin T. (deceased)
IPC分类号： A61K
CPC分类号： C07D487/04 , A61K38/00 , C07K5/0804
摘要： The present invention provides compounds of the general formulas I-IX, as well as compositions, including pharmaceutical compositions, comprising a subject compound. The present invention further provides treatment methods, including methods of treating a hepatitis C virus infection and methods of treating liver fibrosis, the methods generally involving administering to an individual in need thereof an effective amount of a subject compound or composition.
摘要翻译：本发明提供了通式I-IX的化合物，以及包含药物组合物的组合物，其包含主题化合物。本发明进一步提供了治疗方法，包括治疗丙型肝炎病毒感染的方法和治疗肝纤维化的方法，所述方法通常包括向有需要的个体施用有效量的主题化合物或组合物。

4. 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。

5. 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。

6. 发明申请

WO2014078408A1 BICYCLIC HETEROARYL UREA, THIOUREA, GUANIDINE AND CYANOGUANIDINE COMPOUNDS AS TRKA KINASE INHIBITORS 审中-公开
标题翻译：作为TRKA激酶抑制剂的双相异构尿素，硫脲，胍和氰基化合物
公开(公告)号：WO2014078408A1
公开(公告)日：2014-05-22
申请号：PCT/US2013/069886
申请日：2013-11-13
申请人： ARRAY BIOPHARMA INC. , ALLEN, Shelley , BRANDHUBER, Barbara J. , CONDROSKI, Kevin Ronald , HUANG, Lily , KERCHER, Timothy , WINSKI, Shannon L.
发明人： ALLEN, Shelley , BRANDHUBER, Barbara J. , CONDROSKI, Kevin Ronald , HUANG, Lily , KERCHER, Timothy , WINSKI, Shannon L.
IPC分类号： C07D231/56 , C07D471/04 , C07D487/04 , C07D491/048 , C07D495/04 , A61K31/4985 , A61K31/437 , A61K31/416 , A61P29/00 , A61P35/00 , A61P25/00 , A61P31/00
CPC分类号： C07D487/04 , C07D231/56 , C07D403/12 , C07D471/04 , C07D491/048 , C07D495/04 , C07D519/00
摘要： Compounds of Formula I or stereoisomers, tautomers, or pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein Ring A, Ring C and X are as defined herein, are inhibitors of TrkA kinase and are useful in the treatment of diseases which can be treated with a TrkA kinase inhibitor such as pain, cancer, inflammation/inflammatory diseases, neurodegenerative diseases, certain infectious diseases, Sjogren's syndrome, endometriosis, diabetic peripheral neuropathy, prostatitis and pelvic pain syndrome.
摘要翻译：其中环A，环C和X如本文所定义的式I或其立体异构体，互变异构体或其药学上可接受的盐，溶剂合物或前药的化合物是TrkA激酶的抑制剂，并且可用于治疗可以用一种TrkA激酶抑制剂，如疼痛，癌症，炎症/炎性疾病，神经变性疾病，某些传染病，干燥综合征，子宫内膜异位症，糖尿病性周围神经病变，前列腺炎和骨盆疼痛综合征。

7. 发明申请

WO2013066869A1 PIPERIDINYL-SUBSTITUTED LACTAMS AS GPR119 MODULATORS 审中-公开
标题翻译：作为GPR119调节剂的哌啶取代的LACTAMS
公开(公告)号：WO2013066869A1
公开(公告)日：2013-05-10
申请号：PCT/US2012/062576
申请日：2012-10-30
申请人： ARRAY BIOPHARMA INC. , AICHER, Thomas Daniel , BENSCIK, Josef Roland , BOYD, Steven Armen , CONDROSKI, Kevin Ronald , FELL, Jay Bradford , FISCHER, John Peter , HINKLIN, Ronald Jay , PRATT, Scott , SINGH, Ajay , TURNER, Timothy M.
发明人： AICHER, Thomas Daniel , BENSCIK, Josef Roland , BOYD, Steven Armen , CONDROSKI, Kevin Ronald , FELL, Jay Bradford , FISCHER, John Peter , HINKLIN, Ronald Jay , PRATT, Scott , SINGH, Ajay , TURNER, Timothy M.
IPC分类号： C07D413/14 , C07D417/14 , A61K31/422 , A61K31/4245 , A61K31/427 , A61K31/433 , A61P3/04 , A61P3/06 , A61P3/10 , A61P9/12 , A61P9/00 , A61P25/28 , A61P25/18
CPC分类号： C07D417/14 , C07D413/14
摘要： Compounds of Formula (I) and pharmaceutically acceptable salts thereof in which X 1 , X 2 , X 3 , L, R 3 , R 4 , R 5 , R 7 and n have the meanings given in the specification, are modulators of GPR119 and are useful in the treatment or prevention of diseases such as such as, but not limited to, type 2 diabetes, diabetic complications, symptoms of diabetes, metabolic syndrome, obesity, dyslipidemia, and related conditions.
摘要翻译：其中X1，X2，X3，L，R3，R4，R5，R7和n具有本说明书中给出的含义的式（I）化合物及其药学上可接受的盐是GPR119的调节剂，可用于治疗或预防的疾病，例如但不限于2型糖尿病，糖尿病并发症，糖尿病症状，代谢综合征，肥胖症，血脂异常和相关病症。

8. 发明申请

WO2012037393A1 PIPERIDINYL-SUBSTITUTED LACTAMS AS GPR119 MODULATORS 审中-公开
标题翻译：作为GPR119调节剂的哌啶取代的LACTAMS
公开(公告)号：WO2012037393A1
公开(公告)日：2012-03-22
申请号：PCT/US2011/051821
申请日：2011-09-15
申请人： ARRAY BIOPHARMA INC. , AICHER, Thomas Daniel , BENCSIK, Josef R. , BOYD, Steven Armen , CONDROSKI, Kevin Ronald , FELL, Jay Bradford , FISCHER, John P. , HINKLIN, Ronald Jay , PRATT, Scott Alan , SINGH, Ajay , TURNER, Timothy M.
发明人： AICHER, Thomas Daniel , BENCSIK, Josef R. , BOYD, Steven Armen , CONDROSKI, Kevin Ronald , FELL, Jay Bradford , FISCHER, John P. , HINKLIN, Ronald Jay , PRATT, Scott Alan , SINGH, Ajay , TURNER, Timothy M.
IPC分类号： A61K31/4468 , A61K31/454 , A61P3/04 , C07D413/14
CPC分类号： C07D413/14 , A61K31/4468 , A61K31/454 , C07D211/76 , C07D401/04 , C07D401/14
摘要： Compounds of Formula (I) and pharmaceutically acceptable salts thereof in which X 1 , X 2 , L, R 3 , R 4 , R 5 , R 7 and n have the meanings given in the specification, are modulators of GPR119 and are useful in the treatment or prevention of diseases such as such as, but not limited to, type 2 diabetes, diabetic complications, symptoms of diabetes, metabolic syndrome, obesity, dyslipidemia, and related conditions.
摘要翻译：其中X1，X2，L，R3，R4，R5，R7和n具有本说明书中给出的含义的式（I）化合物及其药学上可接受的盐是GPR119的调节剂，可用于治疗或预防疾病例如但不限于2型糖尿病，糖尿病并发症，糖尿病症状，代谢综合征，肥胖症，血脂异常和相关病症。

9. 发明申请

WO2011146335A1 PIPERIDINYL-SUBSTITUTED LACTAMS AS GPR119 MODULATORS 审中-公开
标题翻译：作为GPR119调节剂的哌啶取代的LACTAMS
公开(公告)号：WO2011146335A1
公开(公告)日：2011-11-24
申请号：PCT/US2011/036443
申请日：2011-05-13
申请人： ARRAY BIOPHARMA INC. , AICHER, Thomas Daniel , BENCSIK, Josef Roland , BOYD, Steven Armen , CONDROSKI, Kevin Ronald , FELL, Jay Bradford , FISCHER, John P. , HINKLIN, Ronald Jay , PRATT, Scott Alan , SINGH, Ajay , TURNER, Timothy M.
发明人： AICHER, Thomas Daniel , BENCSIK, Josef Roland , CONDROSKI, Kevin Ronald , FELL, Jay Bradford , FISCHER, John P. , HINKLIN, Ronald Jay , PRATT, Scott Alan , SINGH, Ajay , TURNER, Timothy M.
IPC分类号： C07D401/14 , A61K31/4545 , A61P3/10
CPC分类号： C07D413/14 , C07D401/14 , C07D405/14
摘要： Compounds of Formula (I): and pharmaceutically acceptable salts thereof in which X 1 , X 2 , L, R 3 , R 4 , R 5 , R 6 , R 6a , R 7 , R 9 , R 9a , and n have the meanings given in the specification, are modulators of GPR119 and are useful in the treatment or prevention of diseases such as such as, but not limited to, type 2 diabetes, diabetic complications, symptoms of diabetes, metabolic syndrome, obesity, dyslipidemia, and related conditions.
摘要翻译：其中X1，X2，L，R3，R4，R5，R6，R6a，R7，R9，R9a和n具有本说明书中给出的含义的式（I）化合物及其药学上可接受的盐是GPR119的调节剂并且可用于治疗或预防诸如但不限于2型糖尿病，糖尿病并发症，糖尿病症状，代谢综合征，肥胖症，血脂异常和相关病症等疾病。

10. 发明申请

WO2011029027A1 SUBSTITUTED PYRAZOLO[1,5-a]PYRIMIDINE COMPOUNDS AS mTOR INHIBITORS 审中-公开
标题翻译：取代的吡唑并[1,5-a]吡啶化合物作为mTOR抑制剂
公开(公告)号：WO2011029027A1
公开(公告)日：2011-03-10
申请号：PCT/US2010/047856
申请日：2010-09-03
申请人： ARRAY BIOPHARMA INC. , ANDREWS, Steven W. , CONDROSKI, Kevin Ronald , DE MEESE, Lisa A. , FELL, Jay Bradford , FISCHER, John P. , LE HUEROU, Yvan , JOSEY, John A. , KOCH, Kevin , MIKNIS, Gregory F. , RODRIGUEZ, Martha E. , TOPALOV, George T. , WALLACE, Eli M. , XU, Rui
发明人： ANDREWS, Steven W. , CONDROSKI, Kevin Ronald , DE MEESE, Lisa A. , FELL, Jay Bradford , FISCHER, John P. , LE HUEROU, Yvan , JOSEY, John A. , KOCH, Kevin , MIKNIS, Gregory F. , RODRIGUEZ, Martha E. , TOPALOV, George T. , WALLACE, Eli M. , XU, Rui
IPC分类号： C07D487/04 , A61K31/519
CPC分类号： C07D487/04
摘要： Compounds of Formula I: and salts thereof in which R 1 , R 2 , R 2a , R 3 , n, X and ring B have the meanings given in the specification, are inhibitors of mTOR and are useful in the treatment of diseases which are sensitive to inhibition of mTOR, such as cancers.
摘要翻译：式I化合物及其盐，其中R 1，R 2，R 2a，R 3，n，X和环B具有本说明书中给出的含义，是mTOR的抑制剂，可用于治疗对抑制作用敏感的疾病 mTOR，如癌症。

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