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21. 发明申请

WO2007038314A3 FUSED HETEROCYCLIC COMPOUNDS USEFUL AS KINASE MODULATORS 审中-公开
公开(公告)号：WO2007038314A3
公开(公告)日：2007-04-05
申请号：PCT/US2006/037056
申请日：2006-09-22
申请人： BRISTOL-MYERS SQUIBB COMPANY , VACCARO, Wayne , CHEN, Zhong , DODD, Dharmpal, S. , HUYNH, Tram, N. , LIN, James , LIU, Chunjian , MUSSARI, Christopher, P. , TOKARSKI, John, S. , TORTOLANI, David, R. , WROBLESKI, Stephen, T.
发明人： VACCARO, Wayne , CHEN, Zhong , DODD, Dharmpal, S. , HUYNH, Tram, N. , LIN, James , LIU, Chunjian , MUSSARI, Christopher, P. , TOKARSKI, John, S. , TORTOLANI, David, R. , WROBLESKI, Stephen, T.
IPC分类号： C07D487/04 , A61K31/437 , A61P29/00
摘要： Compounds having the formula (I), and enantiomers, and diastereomers, pharmaceutically-acceptable salts, and hydrates, thereof, (I) are useful as kinase modulators, including MK2 modulation, wherein one of E and F is a nitrogen atom and the other of E and F is a carbon atom, and Z is N or CR 3 , and R 1 , R 2 , R 3 , X and Y are as defined herein.

22. 发明申请

WO2014074670A1 ALKYL AMIDE-SUBSTITUTED PYRIMIDINE COMPOUNDS USEFUL IN THE MODULATION OF IL-12, IL-23 AND/OR IFNα 审中-公开
标题翻译：用于IL-12，IL-23和/或IFNα调节的ALKYL酰胺取代的吡咯烷酮化合物
公开(公告)号：WO2014074670A1
公开(公告)日：2014-05-15
申请号：PCT/US2013/068866
申请日：2013-11-07
申请人： BRISTOL-MYERS SQUIBB COMPANY
发明人： SANTELLA, Joseph B. , MOSLIN, Ryan M. , WEINSTEIN, David S. , WROBLESKI, Stephen T. , TOKARSKI, John S.
IPC分类号： C07D239/95 , A61K31/513 , A61P35/00 , A61P37/00 , A61P29/00
CPC分类号： C07D239/48 , C07D239/95
摘要： Compounds having the following formula (I): or a stereoisomer or pharmaceutically-acceptable salt thereof, where R 1 , R 2 , R 3 , R 4 , and R 5 are as defined herein, are useful in the modulation of IL-12, IL-23 and/or IFNα by acting on Tyk-2 to cause signal transduction inhibition.
摘要翻译：具有下式（I）的化合物或其立体异构体或药学上可接受的盐，其中R 1，R 2，R 3，R 4和R 5如本文所定义，可用于调节IL-12，IL-23和/ 或通过作用于Tyk-2引起信号转导抑制的IFNα。

23. 发明申请

WO2014074660A1 ALKYL-AMIDE-SUBSTITUTED PYRIDYL COMPOUNDS USEFUL AS MODULATORS OF IL-12, IL-23 AND/OR IFNα RESPONSES 审中-公开
标题翻译：用作IL-12，IL-23和/或IFNα应答的调节剂的烷基酰胺取代的吡啶化合物
公开(公告)号：WO2014074660A1
公开(公告)日：2014-05-15
申请号：PCT/US2013/068842
申请日：2013-11-07
申请人： BRISTOL-MYERS SQUIBB COMPANY
发明人： MOSLIN, Ryan M. , LIN, Shuqun , WEINSTEIN, David S. , WROBLESKI, Stephen T. , ZHANG, Yanlei , TOKARSKI, John S.
IPC分类号： C07D401/14 , C07D405/14 , C07D413/14 , C07D401/12 , C07D417/14 , C07D471/04 , A61K31/444 , A61P35/00 , A61P37/00 , A61P29/00
CPC分类号： C07D413/14 , C07D401/12 , C07D401/14 , C07D405/14 , C07D417/14 , C07D471/04
摘要： Compounds having the following formula (I): or a stereoisomer or pharmaceutically-acceptable salt thereof, where R 1 , R 2 , R 3 , R 4 , and R 5 are as defined herein, are useful in the modulation of IL-12, IL-23 and/or IFNα, by acting on Tyk-2 to cause signal transduction inhibition.
摘要翻译：具有下式（I）的化合物或其立体异构体或药学上可接受的盐，其中R 1，R 2，R 3，R 4和R 5如本文所定义，可用于调节IL-12，IL-23和/ 或IFNα，通过作用于Tyk-2以引起信号转导抑制。

24. 发明申请

WO2014039595A1 IMIDAZOPYRIDAZINE JAK3 INHIBITORS AND THEIR USE FOR THE TREATMENT OF INFLAMMATORY AND AUTOIMMUNE DISEASES 审中-公开
标题翻译：咪达唑啶酮JAK3抑制剂及其用于治疗炎症和自发性疾病的用途
公开(公告)号：WO2014039595A1
公开(公告)日：2014-03-13
申请号：PCT/US2013/058114
申请日：2013-09-05
申请人： BRISTOL-MYERS SQUIBB COMPANY
发明人： YANG, Bingwei, Vera , BROWN, Gregory, D. , GUPTA, Samayamunthula, Venkata, Satya, Arun, Kumar , PITTS, William, J.
IPC分类号： C07D487/04 , A61K31/5025 , A61P35/00
CPC分类号： C07D487/04 , C07B59/002 , C07B2200/05
摘要： The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase activity of JAK3, thereby making them useful for the treatment of inflammatory and autoimmune diseases.
摘要翻译：本发明提供式（I）化合物及其药学上可接受的盐。式I化合物抑制JAK3的酪氨酸激酶活性，从而使其可用于治疗炎症和自身免疫性疾病。

25. 发明申请

WO2012125893A1 PYRROLOPYRIDAZINE JAK3 INHIBITORS AND THEIR USE FOR THE TREATMENT OF INFLAMMATORY AND AUTOIMMUNE DISEASES 审中-公开
标题翻译：吡咯烷酮JAK3抑制剂及其用于治疗炎症和自身免疫疾病的用途
公开(公告)号：WO2012125893A1
公开(公告)日：2012-09-20
申请号：PCT/US2012/029366
申请日：2012-03-16
申请人： BRISTOL-MYERS SQUIBB COMPANY , WROBLESKI, Stephen T. , DAS, Jagabandhu , DUAN, Jingwu , GUO, Junqing , HYNES, John , JIANG, Bin , KEMPSON, James , LIN, Shuqun , LU, Zhonghui , PITTS, William J. , SPERGEL, Steven H. , WU, Hong , YANG, Bingwei Vera
发明人： WROBLESKI, Stephen T. , DAS, Jagabandhu , DUAN, Jingwu , GUO, Junqing , HYNES, John , JIANG, Bin , KEMPSON, James , LIN, Shuqun , LU, Zhonghui , PITTS, William J. , SPERGEL, Steven H. , WU, Hong , YANG, Bingwei Vera
IPC分类号： C07D487/04 , A61K31/5025 , A61P37/00 , A61P29/00 , A61P17/00 , A61P19/00 , C07D519/00
CPC分类号： C07D487/04 , C07D519/00
摘要： The present invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase activity of JAK3, thereby making them useful for the treatment of inflammatory and autoimmune diseases.
摘要翻译：本发明提供式I化合物及其药学上可接受的盐。式I化合物抑制JAK3的酪氨酸激酶活性，从而使其可用于治疗炎症和自身免疫性疾病。

26. 发明申请

WO2012125887A1 PYRROLOPYRIDAZINE JAK3 INHIBITORS AND THEIR USE FOR THE TREATMENT OF INFLAMMATORY AND AUTOIMMUNE DISEASES 审中-公开
标题翻译：吡咯烷酮JAK3抑制剂及其用于治疗炎症和自发性疾病的用途
公开(公告)号：WO2012125887A1
公开(公告)日：2012-09-20
申请号：PCT/US2012/029337
申请日：2012-03-16
申请人： BRISTOL-MYERS SQUIBB COMPANY , WROBLESKI, Stephen T. , JAGABANDHU, Das , DOWEYKO, Lidia M. , GUO, Junqing , HYNES, John , JIANG, Bin , KEMPSON, James , LIN, Shuqun , SPERGEL, Steven H. , TOKARSKI, John S. , WU, Hong , YANG, Bingwei Vera
发明人： WROBLESKI, Stephen T. , JAGABANDHU, Das , DOWEYKO, Lidia M. , GUO, Junqing , HYNES, John , JIANG, Bin , KEMPSON, James , LIN, Shuqun , SPERGEL, Steven H. , TOKARSKI, John S. , WU, Hong , YANG, Bingwei Vera
IPC分类号： A61K31/5025 , A61P37/00 , A61P29/00 , A61P17/00 , A61P19/00 , C07D487/04 , C07F9/11
CPC分类号： C07D487/04 , C07F9/6561
摘要： Disclosed are compounds of formula (I) and pharmaceutically acceptable salts thereof. The compounds of formula (I) inhibit tyrosine kinase activity of JAK3, thereby making them useful for the treatment of inflammatory and autoimmune diseases.
摘要翻译：公开了式（I）的化合物及其药学上可接受的盐。式（I）化合物抑制JAK3的酪氨酸激酶活性，从而使其可用于治疗炎性和自身免疫性疾病。

27. 发明申请

WO2011159852A1 PIPERIDINYL COMPOUND AS A MODULATOR OF CHEMOKINE RECEPTOR ACTIVITY 审中-公开
标题翻译：作为化合物受体活性的调节剂的哌啶化合物
公开(公告)号：WO2011159852A1
公开(公告)日：2011-12-22
申请号：PCT/US2011/040605
申请日：2011-06-16
申请人： BRISTOL-MYERS SQUIBB COMPANY , CHERNEY, Robert J. , DUNCIA, John V. , GARDNER, Daniel S. , SANTELLA, Joseph B. , WANG, Zhongyu
发明人： CHERNEY, Robert J. , DUNCIA, John V. , GARDNER, Daniel S. , SANTELLA, Joseph B. , WANG, Zhongyu
IPC分类号： C07D211/52 , A61K31/451
CPC分类号： C07D211/52 , A61K31/451
摘要： The present application describes the compound of formula (I): or stereoisomers or pharmaceutically acceptable salts thereof. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and arthrosclerosis using the compound of the invention are disclosed.
摘要翻译：本申请描述了式（I）化合物或其立体异构体或其药学上可接受的盐。此外，公开了使用本发明的化合物治疗和预防炎症性疾病如哮喘和过敏性疾病以及自身免疫病态如类风湿性关节炎和关节病的方法。

28. 发明申请

WO2008021926A2 MODULATORS OF GLUCOCORTICOID RECEPTOR, AP-1, AND/OR NF-KB ACTIVITY AND USE THEREOF 审中-公开
标题翻译： GLUCOCORTICOID受体的调节剂，AP-1和/或NF-κB活性及其用途
公开(公告)号：WO2008021926A2
公开(公告)日：2008-02-21
申请号：PCT/US2007/075543
申请日：2007-08-09
申请人： BRISTOL-MYERS SQUIBB COMPANY , WEINSTEIN, David, S. , GONG, Hua , DUAN, Jingwu , DHAR, T.G. Murali , YANG, Bingwei Vera , CHEN, Ping , JIANG, Bin
发明人： WEINSTEIN, David, S. , GONG, Hua , DUAN, Jingwu , DHAR, T.G. Murali , YANG, Bingwei Vera , CHEN, Ping , JIANG, Bin
CPC分类号： C07D417/12 , C07D277/46 , C07D405/12 , C07D417/14 , C07D491/04
摘要： Novel non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-KB activity, including inflammatory and immune diseases, having the structure of formula (I), an enantiomer, diastereomer, or tautomer thereof, or a prodrug ester thereof, or a pharmaceutically-acceptable salt thereof, in which: Z is heterocyclo or heteroaryl; A is a 5- to 8- membered carbocyclic ring or a 5- to 8-membered heterocyclic ring; B is a cycloalkyl, cycloalkenyl, aryl, heterocyclo, or heteroaryl ring, wherein each ring is fused to the A ring on adjacent atoms and optionally substituted by one to four groups which are the same or different and are independently selected from R 5 , R 6 , R 7 , and R 8 ; J 1 , J 2 , and J3 are at each occurrence the same or different and are independently -A 1 QA 2 -; Q is a bond, O, S, S(O), or S(O)2; A 1 and A 2 are the same or different and are at each occurrence independently selected from a bond, C1-3alkylene, substituted C 1 - 3 alkylene, C 2 -4alkenylene, and substituted C 2 - 4 alkenylene, provided that A 1 and A 2 are chosen so that ring A is a 5- to 8-membered carbocyclic or heterocyclic ring; R 1 to R 11 are as defined herein. Also provided are pharmaceutical compositions and methods of treating inflammatory- or immune-associated diseases and obesity and diabetes employing said compounds.
摘要翻译：提供了新的非甾体化合物，其可用于治疗与式（I）结构的糖皮质激素受体，AP-1和/或NF-κB活性（包括炎症和免疫疾病）的调节相关的疾病，对映异构体，非对映体或其互变异构体，或其前药酯或其药学上可接受的盐，其中：Z是杂环或杂芳基; A是5-至8-元碳环或5-至8-元杂环; B是环烷基，环烯基，芳基，杂环或杂芳基环，其中每个环与相邻原子上的A环稠合，并且任选地被一至四个相同或不同的基团取代，并且独立地选自R 1， R 5，R 6，R 7和R 8; J 1，J 2和J 3在每次出现时相同或不同，并且独立地为-A 1 N 2 QA 2， SUB> - ; Q是键，O，S，S（O）或S（O）2; A 1和A 2各自相同或不同，并且在每次出现时独立地选自键，C 1-3亚烷基，取代的C 1 H 3，

29. 发明申请

WO2008014381A3 MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY, CRYSTALLINE FORMS AND PROCESS 审中-公开
公开(公告)号：WO2008014381A3
公开(公告)日：2008-01-31
申请号：PCT/US2007/074438
申请日：2007-07-26
申请人： BRISTOL-MYERS SQUIBB COMPANY , YANG, Michael, G. , CHERNEY, Robert, J. , EASTGATE, Martin, G. , MUSLEHIDDINOGLU, Jale , PRASAD, Siva, Josyula , XIAO, Zili
发明人： YANG, Michael, G. , CHERNEY, Robert, J. , EASTGATE, Martin, G. , MUSLEHIDDINOGLU, Jale , PRASAD, Siva, Josyula , XIAO, Zili
IPC分类号： C07D403/12 , C07D207/273 , A61K31/4025 , C07D317/72
摘要： The present invention provides a novel antagonist or partial agonists/antagonists of MCP-1 receptor activity: N-((1R,2S,5R)-5-(isopropyl(methyl)amino)-2-((S)-2-oxo-3-(6-(trifluoromethyl)quinazolin-4-ylamino)pyrrolidin-1-yl)cyclohexyl)acetamide, or a pharmaceutically acceptable salt, solvate or prodrug, thereof, having an unexpected combination of desirable pharmacological characteristics. Crystalline forms of the present invention are also provided. Pharmaceutical compositions containing the same and methods of using the same as agents for the treatment of inflammatory diseases, allergic, autoimmune, metabolic, cancer and/or cardiovascular diseases is also an objective of this invention. The present disclosure also provides a process for preparing compounds of Formula (I), including N-((1R,2S,5R)-5-(isopropyl(methyl)amino)-2-((S)-2-oxo-3-(6-(trifluoromethyl)quinazolin-4-ylamino)pyrrolidin-1-yl)cyclohexyl)acetamide: wherein R 1 , R 8 , R 9 , R 10 , and structure (a) are as described herein. Compounds that are useful intermediates of the process are also provided herein.

30. 发明申请

WO2008014361A3 CYCLIC DERIVATIVES AS MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY 审中-公开
公开(公告)号：WO2008014361A3
公开(公告)日：2008-01-31
申请号：PCT/US2007/074378
申请日：2007-07-26
申请人： BRISTOL-MYERS SQUIBB COMPANY , CARTER, Percy H. , CHERNEY, Robert J. , HYNES, John , KO, Soo S. , SRIVASTAVA, Anurag , XIAO, Zili , YANG, Michael G.
发明人： CARTER, Percy H. , CHERNEY, Robert J. , HYNES, John , KO, Soo S. , SRIVASTAVA, Anurag , XIAO, Zili , YANG, Michael G.
IPC分类号： C07D401/12 , C07D403/12 , C07D487/04 , A61K31/4025
摘要： This invention relates generally to modulators of chemokine receptor activity having unexpected combination of desirable pharmacological properties. Pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and prevention of inflammatory, allergic, autoimmune, metabolic, cancer and/or cardiovascular diseases, particularly diabetes, Crohn's disease, atherosclerosis, and multiple sclerosis, along with methods of preparing compounds and intermediates therefor. Metabolites of active compounds are also provided herein, pharmaceutical compositions and use thereof are also provided.

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