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1. 发明申请

WO2012125886A1 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：WO2012125886A1
公开(公告)日：2012-09-20
申请号：PCT/US2012/029334
申请日：2012-03-16
申请人： BRISTOL-MYERS SQUIBB COMPANY , WROBLESKI, Stephen T. , BROWN, Gregory D. , DOWEYKO, Lidia M. , DUAN, Jingwu , GUO, Junqing , HYNES, John , JIANG, Bin , KEMPSON, James , LIN, Shuqun , LU, Zhonghui , SPERGEL, Steven, H. , TOKARSKI, John S. , WU, Hong , YANG, Bingwei Vera
发明人： WROBLESKI, Stephen T. , BROWN, Gregory D. , DOWEYKO, Lidia M. , DUAN, Jingwu , GUO, Junqing , HYNES, John , JIANG, Bin , KEMPSON, James , LIN, Shuqun , LU, Zhonghui , 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 , C07D519/00 , C07D487/04
CPC分类号： C07D487/04 , C07D471/04 , C07D519/00
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。

2. 发明申请

WO2003053941A3 BARBITURIC ACID DERIVATIVES AS INHIBITORS OF TNF-ALPHA CONVERTING ENZYME (TACE) AND/OR MATRIX METALLOPROTEINASES 审中-公开
公开(公告)号：WO2003053941A3
公开(公告)日：2003-07-03
申请号：PCT/US2002/040458
申请日：2002-12-17
申请人： BRISTOL-MYERS SQUIBB COMPANY , DUAN, Jingwu , JIANG, Bin , CHEN, Lihua , LU, Zhonghui , BARBOSA, Joseph , PITTS, William
发明人： DUAN, Jingwu , JIANG, Bin , CHEN, Lihua , LU, Zhonghui , BARBOSA, Joseph , PITTS, William
IPC分类号： C07D239/54
摘要： The present application describes novel barbituric acid derivatives of formula (I) or pharmaceutically acceptable salt or prodrug forms thereof, wherein A, B, L, R1, R2, R3, R4, R5, n, W, U, X, Y, Z, Ua, Xa, Ya, and Za are defined in the present specification, which are useful as TNF-a converting enzyme (TACE) and matrix metalloproteinases (MMP) inhibitors.

3. 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。

4. 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，

5. 发明申请

WO2011019780A1 AZAINDAZOLES AS BTK KINASE MODULATORS AND USE THEREOF 审中-公开
标题翻译： AZAINDAZOLES作为BTK激酶调节剂及其用途
公开(公告)号：WO2011019780A1
公开(公告)日：2011-02-17
申请号：PCT/US2010/045109
申请日：2010-08-11
申请人： BRISTOL-MYERS SQUIBB COMPANY , DUAN, Jingwu , JIANG, Bin , LU, Zhonghui
发明人： DUAN, Jingwu , JIANG, Bin , LU, Zhonghui
IPC分类号： C07D471/04 , A61K31/437 , A61K31/519 , A61P29/00 , A61P35/00
CPC分类号： C07D471/04
摘要： Compounds having the formula (I), and enantiomers, and diastereomers, pharmaceutically-acceptable salts, thereof, (I) are useful as kinase modulators, including Btk modulation, wherein A 1 , A 2 , A 3 , R 4 , 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，（I）可用作激酶调节剂，包括Btk调节，其中A1，A2，A3，R4如本文所定义。

6. 发明申请

WO2009100171A1 FUSED HETEROARYL MODULATORS OF GLUCOCORTICOID RECEPTOR, AP-1, AND/OR NF-KB ACTIVITY AND USE THEREOF 审中-公开
标题翻译：葡萄糖激素受体，AP-1和/或NF-κB活性的融合异源调节剂及其用途
公开(公告)号：WO2009100171A1
公开(公告)日：2009-08-13
申请号：PCT/US2009/033134
申请日：2009-02-05
申请人： BRISTOL-MYERS SQUIBB COMPANY , DUAN, Jingwu , WEINSTEIN, David, S. , JIANG, Bin
发明人： DUAN, Jingwu , WEINSTEIN, David, S. , JIANG, Bin
IPC分类号： C07D491/04 , A61P3/00 , A61P29/00 , A61P37/00 , A61K31/436 , C07D491/147
CPC分类号： C07D491/147
摘要： Novel non-steroidal compounds are provided which are useful in treating diseases or disorders associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-κB activity, including metabolic and inflammatory and immune diseases or disorders, having the structure of formula (I): an enantiomer, diastereomer, or taυtomer thereof, or a prodrug ester thereof, or a pharmaceutically-acceptable salt thereof, in which: Z is heterocyclo or heteroaryl; • A is a S- to 8- membered carbocyclic ring or a S- to 8-membered heterocyclic ring; B 1 and B 2 rings are pyridyl rings, wherein the B 1 and B 2 rings are each fused to the A ring and the B 1 ring is optionally substituted by one to three groups which are the same or different and are independently selected from R 1 , R 2 , and R 4 , and the B 2 ring is optionally substituted by one to three groups which are the same or different and are independently selected from R 5 , R 7 , and R 3 J 1 , J 2 , and J 3 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, C 1 - 3 alkylene, substituted C 1-3 alkylene, C 2-4 alkenylene, 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....
摘要翻译：提供了新的非甾体化合物，其可用于治疗与调节糖皮质激素受体，AP-1和/或NF-κB活性（包括代谢和炎症和免疫疾病或病症）相关的疾病或障碍，其具有以下结构：式（I）：其对映异构体，非对映异构体或其衍生物或其前药酯或其药学上可接受的盐，其中：Z是杂环基或杂芳基; A为S-至8-元碳环或S至8-元杂环; B1和B2环是吡啶环，其中B1和B2环各自与A环稠合，B1环任选被一至三个相同或不同并且独立地选自R 1，R 2和R 4的基团取代并且B2环任选地被一至三个相同或不同并且独立地选自R 5，R 7和R 3的基团取代，J 1，J 2和J 3在每次出现时相同或不同，并且独立地为-AlQA2- ; Q是键，O，S，S（O）或S（O）2; A1和A2相同或不同，并且在每次出现时独立地选自键，C1-3亚烷基，取代的C1-3亚烷基，C2-4亚烯基和取代的C2-4亚烯基，条件是A1和A2被选择为该环A为5-至8-元碳环或杂环; R1至R11如本文所定义。

7. 发明申请

WO2007073503A2 INDANE MODULATORS OF GLUCOCORTICOID RECEPTOR, AP-1, AND/OR NF-KB ACTIVITY AND USE THEREOF 审中-公开
标题翻译：葡萄糖激素受体，AP-1和/或NF-κB活性的调节因子及其用途
公开(公告)号：WO2007073503A2
公开(公告)日：2007-06-28
申请号：PCT/US2006/049075
申请日：2006-12-21
申请人： BRISTOL-MYERS SQUIBB COMPANY , DUAN, Jingwu , JIANG, Bin
发明人： DUAN, Jingwu , JIANG, Bin
CPC分类号： C07D285/135 , C07D233/76 , C07D249/12 , C07D277/46 , C07D285/08
摘要： Novel non-steroidal compounds are provided that are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-?B activity including obesity, diabetes, inflammatory and immune diseases having the structure of formula (I): [INSERT CHEMICAL STRUCTURE HERE] (I) or enantiomers, diastereomers, or a pharmaceutically-acceptable salt, or hydrate, thereof, where X is -A1QA2-; Q is a bond, -C(=O)-, -OC(O)-, -C(=O)NR5-, -SOp-, -SOpNR5-, -C(O)O-, - NR5C(O)-, -OC(O)NR5-, -NR5C(O)O-, - S(O)pNR5C(O)-, -C(O)NR5S(O)p- - NR5S(O)p-, or -NR5C(=O)NR6-. Y is selected from hydrogen, C1-6alkyl, OR16, substituted C1-6alkyl, cycloalkyl, aryl, heterocyclo and heteroaryl. A1 and A2 are independently selected from a bond, C1-3alkylene, or C1-3alkenylene, and R1 - R11 are defined herein. Also provided are pharmaceutical compositions, combinations, and methods of treating obesity, diabetes and inflammatory- or immune-associated diseases comprising said compounds.
摘要翻译：提供了新的非甾体化合物，其可用于治疗与调节糖皮质激素受体，AP-1和/或NF-κB活性相关的疾病，包括具有式（I）结构的肥胖症，糖尿病，炎症和免疫疾病，：[INSERT CHEMICAL STRUCTURE HERE]（I）或其对映异构体，非对映异构体或其药学上可接受的盐或水合物，其中X为-A1QA2-; Q是键，-C（= O） - ， - OC（O） - ， - C（= O）NR5-，-SOp-，-SOpNR5-，-C（O）O-，-NR5C（O） - （O）NR 5 - ， - NR 5 C（O）O-，-S（O）pNR 5 C（O） - ， - C（O）NR 5 S（O） NR 5 C（= O）NR 6 - 。 Y选自氢，C 1-6烷基，OR 16，取代的C 1-6烷基，环烷基，芳基，杂环和杂芳基。 A1和A2独立地选自键，C1-3亚烷基或C1-3亚烯基，并且R1-R11在本文中定义。还提供了治疗包含所述化合物的肥胖症，糖尿病和炎性或免疫相关疾病的药物组合物，组合和方法。

8. 发明申请

WO2006138373A2 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-kB活性及其用途
公开(公告)号：WO2006138373A2
公开(公告)日：2006-12-28
申请号：PCT/US2006/023164
申请日：2006-06-14
申请人： BRISTOL-MYERS SQUIBB COMPANY , DUAN, Jingwu , LU, Zhonghui , WEINSTEIN, David, S. , JIANG, Bin
发明人： DUAN, Jingwu , LU, Zhonghui , WEINSTEIN, David, S. , JIANG, Bin
IPC分类号： C07D231/56 , A61K31/416 , A61P29/00
CPC分类号： C07D401/04 , C07D231/56 , C07D401/06 , C07D403/04 , C07D405/04 , C07D405/06 , C07D409/06 , C07D417/06 , C07D417/12
摘要： Non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-?B activity including obesity, diabetes, inflammatory and immune diseases, and have the structure of formula (I) or an enantiomer, a diastereomer, a pharmaceutically acceptable salt, or hydrate thereof, where J is selected from NR 1 or C(R 4 )(R 4a ); K is selected from NR 2 or C(R 5 )(R 5a ); L is selected from NR 3 or C(R 6 )(R 6a ); and A, X, Y, R 1 , R 2 , R 3 , R 4 , R 4a , R 5 , R 5a , R 6 , R 6a , R 8 , R 10 , R 11 , and n are defined herein. Also provided are pharmaceutical compositions and methods of treating obesity, diabetes and inflammatory or immune associated diseases comprising said compounds.
摘要翻译：提供非甾体化合物，其可用于治疗与调节糖皮质激素受体，AP-1和/或NF-κB活性（包括肥胖症，糖尿病，炎症和免疫疾病）相关的疾病，并且具有式（I ）或其对映异构体，非对映异构体，药学上可接受的盐或水合物，其中J选自NR 1或C（R 4）（R 4a））; K选自NR 2或C（R 5）（R 5a）; L选自NR 3或C（R 6 S）（R 6a）; 和A，X，Y，R 1，R 2，R 3，R 4，R SUB R 4a，R 5，R 5a，R 6，R 6a，R SUB， R 8，R 11，R 11和n如本文所定义。还提供了治疗肥胖症，糖尿病和包含所述化合物的炎性或免疫相关疾病的药物组合物和方法。

9. 发明申请

WO2005072732A1 MODULATORS OF THE 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：WO2005072732A1
公开(公告)日：2005-08-11
申请号：PCT/US2005/001181
申请日：2005-01-14
申请人： BRISTOL-MYERS SQUIBB COMPANY , DUAN, Jingwu , SHEPPECK, James , JIANG, Bin , GILMORE, John, L.
发明人： DUAN, Jingwu , SHEPPECK, James , JIANG, Bin , GILMORE, John, L.
IPC分类号： A61K31/439
CPC分类号： C07D471/08 , C07D401/12 , C07D401/14 , C07D417/12 , C07D417/14
摘要： A class of novel non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-ĸB activity including obesity, diabetes, inflammatory and immune diseases, and have the structure of formula (I) its stereoisomers thereof, or a solvate thereof, or a prodrug thereof, or a pharmaceutically acceptable salt thereof, where Z is CONR 1 R 2 or CH 2 NR 1 R 2 and where at least one of X 1 - X 8 is N, and R, R a , R b , R c and R d are defined herein. Also provided are pharmaceutical compositions and methods of treating obesity, diabetes and inflammatory or immune associated diseases comprising said compounds.
摘要翻译：提供一类新型非甾体化合物，其可用于治疗与糖皮质激素受体，AP-1和/或NF-kB活性的调节相关的疾病，包括肥胖症，糖尿病，炎症和免疫疾病，并且具有式（I）其立体异构体，或其溶剂合物或其前药，或其药学上可接受的盐，其中Z为CONR 1 R 2或CH 2 NR 1 R 2和其中X1-X8中的至少一个是N，并且R，R a，R b，R c和R d在本文中定义。还提供了治疗肥胖症，糖尿病和包含所述化合物的炎性或免疫相关疾病的药物组合物和方法。

10. 发明申请

WO2005070207A1 MODULATORS OF THE 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：WO2005070207A1
公开(公告)日：2005-08-04
申请号：PCT/US2005/001411
申请日：2005-01-14
申请人： BRISTOL-MYERS SQUIBB COMPANY , DUAN, Jingwu , JIANG, Bin , SHEPPECK, James , GILMORE, John L.
发明人： DUAN, Jingwu , JIANG, Bin , SHEPPECK, James , GILMORE, John L.
IPC分类号： A01N43/58
CPC分类号： C07D403/12 , C07D241/36 , C07D417/12 , C07D417/14
摘要： A class of novel non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-κB activity including obesity, diabetes, inflammatory and immune diseases, and have the structure of formula (I). Its stereoisomers thereof, or a solvate thereof, or a prodrug thereof, or a pharmaceutically acceptable salt thereof, where Z is CONR 1 R 2 or CH 2 NR 1 R 2 and where at least two of X 1 - X 4 and/or X 5 - X 8 is N or NR 18 , and R, R a , R b , R c , R d , R 1 , R 2 and R 18 are defined herein. Also provided are pharmaceutical compositions and methods of treating obesity, diabetes and inflammatory or immune associated diseases comprising said compounds.
摘要翻译：提供一类新型非甾体化合物，其可用于治疗与糖皮质激素受体，AP-1和/或NF-κB活性的调节相关的疾病，包括肥胖症，糖尿病，炎症和免疫疾病，并且具有式（I）。其立体异构体或其溶剂合物或其前药，或其药学上可接受的盐，其中Z为CONR 1 R 2或CH 2 NR 1 R 2，并且其中至少两个的X 1 -X 4和/或X 5 -X 8是N或NR 18，并且R，R a，R b，R c，R d，R 1，R 2，和R 18在本文中定义。还提供了治疗肥胖症，糖尿病和包含所述化合物的炎性或免疫相关疾病的药物组合物和方法。

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