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11. 发明申请

WO2010105179A3 INHIBITORS OF BETA-SECRETASE 审中-公开
公开(公告)号：WO2010105179A3
公开(公告)日：2010-09-16
申请号：PCT/US2010/027173
申请日：2010-03-12
申请人： VITAE PHARMACEUTICALS, INC. , BOEHRINGER INGELHEIM INTERNATIONAL GMBH , CACATIAN, Salvacion , CLAREMON, David, A. , DILLARD, Lawrence, W. , FUCHS, Klaus , HEINE, Niklas , JIA, Lanqi , LEFTHERIS, Katerina , MCKEEVER, Brian , MORALES-RAMOS, Angel , SINGH, Suresh , VENKATRAMAN, Shankar , WU, Guosheng , WU, Zhongren , XU, Zhenrong , YUAN, Jing , ZHENG, Yajun
发明人： CACATIAN, Salvacion , CLAREMON, David, A. , DILLARD, Lawrence, W. , FUCHS, Klaus , HEINE, Niklas , JIA, Lanqi , LEFTHERIS, Katerina , MCKEEVER, Brian , MORALES-RAMOS, Angel , SINGH, Suresh , VENKATRAMAN, Shankar , WU, Guosheng , WU, Zhongren , XU, Zhenrong , YUAN, Jing , ZHENG, Yajun
IPC分类号： C07D277/60 , C07D271/12 , C07D235/02 , C07D239/70 , C07D491/10 , C07D487/10 , C07D403/06 , C07D405/12 , C07D498/10 , A61K31/4245 , A61K31/4184 , A61K31/4188 , A61K31/517 , A61K31/519 , A61K31/428
摘要： The present invention is directed to a compound represented by the following structural formula or a pharmaceutically acceptable salt thereof. Pharmaceutical compositions and method of use of the compounds are also described.

12. 发明申请

WO2004099156A1 ARYL-SUBSTITUTED PYRAZOLE-AMIDE COMPOUNDS USEFUL AS KINASE INHIBITORS 审中-公开
标题翻译： ARYL替代的吡唑酰胺化合物可用作激酶抑制剂
公开(公告)号：WO2004099156A1
公开(公告)日：2004-11-18
申请号：PCT/US2004/013604
申请日：2004-05-03
申请人： BRISTOL-MYERS SQUIBB COMPANY , DYCKMAN, Alaric , DAS, Jagabandhu , LEFTHERIS, Katerina , LIU, Chunjian , ZHAO, Rulin , CHEN, Bang-Chi , WROBLESKI, Stephen, T.
发明人： DYCKMAN, Alaric , DAS, Jagabandhu , LEFTHERIS, Katerina , LIU, Chunjian , ZHAO, Rulin , CHEN, Bang-Chi , WROBLESKI, Stephen, T.
IPC分类号： C07D231/18
CPC分类号： C07D231/14 , C07D231/12 , C07D231/40 , C07D401/12 , C07D413/12
摘要： The present invention relates to compounds having the formula (I), and pharmaceutically-acceptable salts, prodrugs, solvates, isomers, and/or hydrates thereof, wherein Q is an optionally-substituted phenyl, pyridyl, pyridazinyl, pyrimidinyl, or pyrazinyl ring; R 2 is alkyl or an amino group as defined herein; and Z is optionally-substituted oxadiazolyl or -C(=O)NR 6 , wherein R 6 is lower alkyl or cyclopropyl. The compounds are surprisingly advantageous in preparing medicaments for treating p38 kinase related conditions and/or in preparing medicaments for use in treating inflammatory disorders or conditions in a patient.
摘要翻译：本发明涉及具有式（I）的化合物及其药学上可接受的盐，前体药物，溶剂合物，异构体和/或水合物，其中Q是任选取代的苯基，吡啶基，哒嗪基，嘧啶基或吡嗪基; R2是如本文所定义的烷基或氨基; Z为任选取代的恶二唑基或-C（= O）NR 6，其中R 6为低级烷基或环丙基。该化合物在制备用于治疗p38激酶相关病症的药物和/或制备用于治疗患者的炎性疾病或病症的药物方面令人惊奇地有利。

13. 发明申请

WO2007016392A2 BENZOTHIAZOLE AND AZABENZOTHIAZOLE COMPOUNDS USEFUL AS KINASE INHIBITORS 审中-公开
标题翻译：苯并噻唑和氰基苯并噻唑化合物可用作激酶抑制剂
公开(公告)号：WO2007016392A2
公开(公告)日：2007-02-08
申请号：PCT/US2006/029520
申请日：2006-07-28
申请人： BRISTOL-MYERS SQUIBB COMPANY , LIU, Chunjian , LEFTHERIS, Katerina , LIN, James
发明人： LIU, Chunjian , LEFTHERIS, Katerina , LIN, James
IPC分类号： C07D417/04 , C07D513/04 , A61K31/428
CPC分类号： C07D513/04 , C07D417/04
摘要： A compound of Formula (I), or an enantiomer, diastereomer or a pharmaceutically-acceptable salt thereof, wherein A is independently selected from: (a); (b); (c); or (d), further wherein R1, R2, R3, R4, R5, R6, R7, and W are as described herein. Also disclosed is a compound of Formula (II), or an enantiomer, diastereomer, or a pharmaceutically-acceptable salt thereof, wherein each of G, X and Y are independently CH or N, wherein at each occurrence at least one of G, X or Y is N and the other two of G, X or Y are CH; and B is independently selected from: (a); (b); (c); (d); or (e), further wherein R1, R2, R3, R4, R5, R8, R9 and Z are as described herein. Also disclosed are pharmaceutical compositions containing compounds of Formula (I) and Formula (II), and methods of treating conditions associated with the activity of p38 kinase.
摘要翻译：式（I）的化合物或其对映异构体，非对映异构体或药学上可接受的盐，其中A独立地选自：（a）; （B）; （C）; 或（d）中，进一步地，其中R 1，R 2，R 3，R 4，R 5，R 6，R 7和W如本文所述。还公开了式（II）的化合物或其对映异构体，非对映异构体或药学上可接受的盐，其中G，X和Y各自独立地为CH或N，其中在每次出现时，G，X 或者Y是N而G，X或Y中的另外两个是CH; 和B独立地选自：（a）; （B）; （C）; （d）; 或（e）中，进一步其中R 1，R 2，R 3，R 4，R 5，R 8，R 9和Z如本文所述。还公开了含有式（I）和式（II）化合物的药物组合物，以及治疗与p38激酶活性相关的病症的方法。

14. 发明申请

WO2006017054A2 TRICYCLIC-HETEROARYL COMPOUNDS USEFUL AS KINASE INHIBITORS 审中-公开
标题翻译： TRICYCLIC-HETEROARYL化合物作为激酶抑制剂有用
公开(公告)号：WO2006017054A2
公开(公告)日：2006-02-16
申请号：PCT/US2005/023683
申请日：2005-06-30
申请人： BRISTOL-MYERS SQUIBB COMPANY , LIN, James , WROBLESKI, Stephen T. , LIU, Chunjian , LEFTHERIS, Katerina
发明人： LIN, James , WROBLESKI, Stephen T. , LIU, Chunjian , LEFTHERIS, Katerina
IPC分类号： A61K31/53 , A61K31/675 , C07D487/14
CPC分类号： C07D487/14
摘要： The present invention relates to compounds having the formula (I) wherein, Q is optionally substituted aryl or heteroaryl, R 1 is hydrogen or C 1-4 alkyl, and R 2 , R 3 , R 4 and R 5 are hydrogen or optional substituents as defined in the specification.
摘要翻译：本发明涉及具有式（I）的化合物，其中Q是任选取代的芳基或杂芳基，R 1是氢或C 1-4烷基， R 3，R 3，R 4和R 5是氢或任选的如说明书中所定义的取代基。

15. 发明申请

WO2004043912A2 METHODS FOR THE PREPARATION OF PYRROLOTRIAZINE COMPOUNDS USEFUL AS KINASE INHIBITORS 审中-公开
标题翻译：用于制备作为激酶抑制剂的吡咯烷酮化合物的方法
公开(公告)号：WO2004043912A2
公开(公告)日：2004-05-27
申请号：PCT/US2003/035220
申请日：2003-11-03
申请人： BRISTOL-MYERS SQUIBB COMPANY , GODFREY, Jollie, Duaine, Jr. , HYNES, John, Jr. , DYCKMAN, Alaric, J. , LEFTHERIS, Katerina , SHI, Zhongping , WROBLESKI, Stephen, T. , DOUBLEDAY, Wendel, William , GROSSO, John, A.
发明人： GODFREY, Jollie, Duaine, Jr. , HYNES, John, Jr. , DYCKMAN, Alaric, J. , LEFTHERIS, Katerina , SHI, Zhongping , WROBLESKI, Stephen, T. , DOUBLEDAY, Wendel, William , GROSSO, John, A.
IPC分类号： C07D
CPC分类号： C07D487/04 , C07D207/50
摘要： Methods of preparing kinase inhibiting pharmaceutical compounds having the formula (I): or a pharmaceutically acceptable salt or solvate thereof, wherein R1 through R6 and Z are as described in the specification. The methods according to the invention utilize an amination process, in which a pyrrole is reacted with a haloamine, preferably chloramine. This step is followed by cyclization to form the pyrrolotriazine core.
摘要翻译：制备具有式（I）的激酶抑制药物化合物或其药学上可接受的盐或溶剂化物的方法，其中R1至R6和Z如说明书所述。根据本发明的方法利用胺化方法，其中吡咯与卤胺，优选氯胺反应。该步骤之后环化形成吡咯并三嗪核心。

16. 发明申请

WO2010011837A1 FUSED HETEROCYCLIC COMPOUNDS USEFUL AS KINASE MODULATORS 审中-公开
标题翻译：熔化的杂环化合物作为激酶调节剂有用
公开(公告)号：WO2010011837A1
公开(公告)日：2010-01-28
申请号：PCT/US2009/051536
申请日：2009-07-23
申请人： BRISTOL-MYERS SQUIBB COMPANY , LIU, Chunjian , LEFTHERIS, Katerina , TEBBEN, Andrew, J.
发明人： LIU, Chunjian , LEFTHERIS, Katerina , TEBBEN, Andrew, J.
IPC分类号： A61K31/53 , C07D487/04 , A61K31/4985 , A61P37/00
CPC分类号： C07D487/04
摘要： Compounds having the formula (I), and enantiomers, and diastereomers, pharmaceutically-acceptable salts, thereof,are useful as kinase modulators, including Btk modulation, wherein R 1 , R 2 , R 3 , R 4 , Q, A and B are as defined herein.
摘要翻译：具有式（I）的化合物及其对映异构体和非对映体药学上可接受的盐可用作激酶调节剂，包括Btk调节，其中R 1，R 2，R 3，R 4，Q，A和B如本文所定义。

17. 发明申请

WO2009015169A1 INDOLE INDANE AMIDE COMPOUNDS USEFUL AS CB2 AGONISTS AND METHOD 审中-公开
标题翻译：单独使用吲哚类化合物作为CB2激发剂和方法有用
公开(公告)号：WO2009015169A1
公开(公告)日：2009-01-29
申请号：PCT/US2008/070810
申请日：2008-07-23
申请人： BRISTOL-MYERS SQUIBB COMPANY , LIU, Chunjian , WROBLESKI, Stephen T. , LEFTHERIS, Katerina , WU, Gang , SHER, Philip M. , ELLSWORTH, Bruce A.
发明人： LIU, Chunjian , WROBLESKI, Stephen T. , LEFTHERIS, Katerina , WU, Gang , SHER, Philip M. , ELLSWORTH, Bruce A.
IPC分类号： C07D209/42 , A61K31/404
CPC分类号： C07D209/42 , C07D413/06
摘要： Indole indane amides which are CB2 agonists are provided which have the structure I wherein R 1 , R 2 , R 3 , R 4 and R 5 are as defined herein, which compounds are useful in treating autoimmune diseases, inflammation, pain, cardiovascular disorders and other diseases mediated by CB2 receptors. A method for preventing or treating such diseases employing the compounds of the invention is also provided.
摘要翻译：提供了CB2激动剂的吲哚二烷酰胺，其具有结构I，其中R 1，R 2，R 3，R 4和R 5如本文所定义，该化合物可用于治疗由CB2介导的自身免疫疾病，炎症，疼痛，心血管疾病和其它疾病受体。还提供了使用本发明化合物预防或治疗这些疾病的方法。

18. 发明申请

WO2006084017A3 PHENYL-SUBSTITUTED PYRIMIDINE COMPOUNDS USEFUL AS KINASE INHIBITORS 审中-公开
公开(公告)号：WO2006084017A3
公开(公告)日：2006-08-10
申请号：PCT/US2006/003659
申请日：2006-02-02
申请人： BRISTOL-MYERS SQUIBB COMPANY , WROBLESKI, Stephen, T. , LIN, Shuqun , LEFTHERIS, Katerina , HE, Liqi , SEITZ, Steven, P. , LIN, Tai-An , VACCARO, Wayne
发明人： WROBLESKI, Stephen, T. , LIN, Shuqun , LEFTHERIS, Katerina , HE, Liqi , SEITZ, Steven, P. , LIN, Tai-An , VACCARO, Wayne
IPC分类号： C07D417/04 , C07D417/14 , C07D401/04 , A61P29/00 , A61P35/00
摘要： Compounds having the formula (I), and pharmaceutically acceptable salts, and solvates thereof, are useful as kinase inhibitors, wherein: two of X 1 , X 2 , and X 3 are N, and the remaining one of X 1 , X 2 , and X 3 is -CR 1 ; R 1 is hydrogen or -CN; and N, G, Z, R 2 , R 3 , R 4 , R 5 , and R 6 are described in the specification. Also disclosed are pharmaceutical compositions containing compounds of formula (I), and methods of treating conditions associated with the activity of p38 kinase and/or conditions associated with the activity of LIM kinase.

19. 发明申请

WO2003099820A1 PYRAZOLO-PYRIMIDINE ANILINE COMPOUNDS 审中-公开
标题翻译：吡唑并吡啶胺类化合物
公开(公告)号：WO2003099820A1
公开(公告)日：2003-12-04
申请号：PCT/US2003/016072
申请日：2003-05-16
申请人： BRISTOL-MYERS SQUIBB COMPANY , DAS, Jagabandhu , LIU, Chunjian , MOQUIN, Robert, V. , LEFTHERIS, Katerina
发明人： DAS, Jagabandhu , LIU, Chunjian , MOQUIN, Robert, V. , LEFTHERIS, Katerina
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： Compounds having the formula (I), where all substituents are as defined herein, and pharmaceutically acceptable salts, prodrugs, and solvates thereof, are useful as kinase inhibitors.
摘要翻译：具有式（I）的化合物，其中所有取代基如本文所定义，及其药学上可接受的盐，前药和溶剂化物，可用作激酶抑制剂。

20. 发明申请

WO2003002542A1 N-HETEROCYCLIC INHIBITORS OF TNF-ALPHA EXPRESSION 审中-公开
标题翻译： TNF-ALPHA表达的N-杂环化合物抑制剂
公开(公告)号：WO2003002542A1
公开(公告)日：2003-01-09
申请号：PCT/US2002/020212
申请日：2002-06-25
申请人： BRISTOL-MYERS SQUIBB COMPANY , PHARMACOPEIA, INC. , MORIARTY, Kevin, J. , SHIMSHOCK, Yvonne , AHMED, Gulzar , WU, Junjun , WEN, James , LI, Wei , ERICKSON, Shawn, D. , LETOURNEAU, Jeffrey, J. , MCDONALD, Edward , LEFTHERIS, Katerina , WROBLESKI, Stephen, T. , HUSSAIN, Zahid , HENDERSON, Ian , METZGER, Axel , BALDWIN, John, J. , DYCKMAN, Alaric
发明人： MORIARTY, Kevin, J. , SHIMSHOCK, Yvonne , AHMED, Gulzar , WU, Junjun , WEN, James , LI, Wei , ERICKSON, Shawn, D. , LETOURNEAU, Jeffrey, J. , MCDONALD, Edward , LEFTHERIS, Katerina , WROBLESKI, Stephen, T. , HUSSAIN, Zahid , HENDERSON, Ian , METZGER, Axel , BALDWIN, John, J. , DYCKMAN, Alaric
IPC分类号： C07D239/32
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D251/52 , C07D251/54 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D405/14
摘要： N-heterocyclic compounds that block cytokine production via inhibition of p38 kinase are disclosed. In one embodiment, compounds of the present invention are represented by Formula (I). Methods of production, pharmaceutical compositions and methods of treating conditions associated with inappropriate p38 kinase activity or TNF-a expression utilizing compounds of the present invention are also disclosed.
摘要翻译：公开了通过抑制p38激酶阻断细胞因子产生的N-杂环化合物。在一个实施方案中，本发明的化合物由式（I）表示。还公开了使用本发明化合物的生产方法，药物组合物和治疗与不适当的p38激酶活性或TNF-α表达相关的病症的方法。

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