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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

WO2009158380A1 CYCLOPENTATHIOPHENE MODULATORS OF THE GLUCOCORTICOID RECEPTOR, AP-1, AND/OR NF-KAPPA B ACTIVITY AND USE THEREOF 审中-公开
标题翻译： GLUCOCORTICOID受体，AP-1和/或NF-KAPPA B活性及其用途的环磷酰胺调节剂
公开(公告)号：WO2009158380A1
公开(公告)日：2009-12-30
申请号：PCT/US2009/048396
申请日：2009-06-24
申请人： BRISTOL-MYERS SQUIBB COMPANY , YANG, Bingwei, Vera
发明人： YANG, Bingwei, Vera
IPC分类号： C07D417/12 , A61K31/433 , A61P29/00
CPC分类号： C07D417/12
摘要： A compound of Formula( I ) and enantiomers, diastereomers and pharmaceutically-acceptable salts thereof, wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 and R 8 are as defined herein. Also disclosed are pharmaceutical compositions and combinations containing compounds of Formula I and methods of treating diseases or disorders including metabolic and inflammatory or immune associated diseases or disorders.
摘要翻译：式（I）的化合物及其对映异构体，非对映异构体和药学上可接受的盐，其中R 1，R 2，R 3，R 4，R 5，R 6，R 7和R 8如本文所定义。还公开了含有式I化合物的药物组合物和组合以及治疗包括代谢和炎症或免疫相关疾病或病症的疾病或病症的方法。

3. 发明申请

WO2008057859A3 MODULATORS OF GLUCOCORTICOID RECEPTOR, AP-I AND/OR NF-KAPPAB ACTIVITY AND USE THEREOF 审中-公开
公开(公告)号：WO2008057859A3
公开(公告)日：2008-05-15
申请号：PCT/US2007/083090
申请日：2007-10-31
申请人： BRISTOL-MYERS SQUIBB COMPANY , YANG, Bingwei, Vera , DOWEYKO, Lidia, M.
发明人： YANG, Bingwei, Vera , DOWEYKO, Lidia, M.
IPC分类号： C07D417/12 , C07D417/14 , A61K31/433 , A61P29/00
摘要： Novel non-steroidal compounds are provided which are useful in. treating diseases associated with modulation of the glucocorticoid receptor AP-I and/or NF- kB activity, including metabolic and inflammatory or immune associated diseases or disorders havin the structure of formula I or an enantiomer, diastereomer, tautomer, or a pharmaceutically-acceptable salt, thereof, wherein: A is a 5-, 6-, or 7-membered heterocyclo or heteroaryl, each containing 1, 2, or 3 heteroatoms selected from N, O, and S and substituted with one to four groups R 1 , R 2 , R 3 , and/or R 4 ; M is selected from alky!, cycloalkyl, aryl, heterocyclo, and heteroaryl; Z is selected from alkyl, CF3, OH, cycloalkyl, heterocyclo, aryl, heteroaryl, -CC=O)NR 8 R 9 , -CC=O)R 8 , -C(NCN)NR 8 R 9 , -CC=O)OR 8 , -SO 2 R 8 , and -SO 2 NR 8 R 9 . Also provided are pharmaceutical compositions, combinations and methods of treating metabolic and inflammatory or immune associated diseases or disorders using said compounds.

4. 发明申请

WO2006076632A1 SUBSTITUTED HETEROARYL AMIDE MODULATORS OF GLUCOCORTICOID RECEPTOR, AP-1, AND/OR NFκB ACTIVITY AND USE THEREOF 审中-公开
标题翻译：替代的胆固醇受体，AP-1和/或NF-κB活性的异构体调节剂及其用途
公开(公告)号：WO2006076632A1
公开(公告)日：2006-07-20
申请号：PCT/US2006/001328
申请日：2006-01-13
申请人： BRISTOL-MYERS SQUIBB COMPANY , SHEPPECK, James E. , DHAR, T. G. Murali , DOWEYKO, Arthur M. P. , DOWEYKO, Lidia M. , GILMORE, John L. , WEINSTEIN, David S. , XIAO, Hai-Yun , YANG, Bingwei Vera
发明人： SHEPPECK, James E. , DHAR, T. G. Murali , DOWEYKO, Arthur M. P. , DOWEYKO, Lidia M. , GILMORE, John L. , WEINSTEIN, David S. , XIAO, Hai-Yun , YANG, Bingwei Vera
CPC分类号： C07D233/91 , C07D277/46 , C07D417/06
摘要： The present invention relates to new class of non-steroidal compounds which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NFκB activity including obesity, diabetes, inflammatory- and immune-associated diseases, and have the structure (I) including all stereoisomers thereof, tautomers thereof, or a prodrug thereof, or a pharmaceutically acceptable salt thereof, wherein X is selected from N, O, and S; Y is N or CR 6 ; Z is a ring; and where R, R a , R b , R c , R d , R 1 , R 2 , R 3 , R 4 , and R 5 are as 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：本发明涉及新类型的非甾体化合物，其可用于治疗与糖皮质激素受体，AP-1和/或NF-B活性的调节相关的疾病，包括肥胖症，糖尿病，炎性和免疫相关疾病，并且具有包括其所有立体异构体，其互变异构体或其前药或其药学上可接受的盐的结构（I），其中X选自N，O和S; Y是N或CR 6; Z是一个戒指并且其中R，R a，R b，R b，R c，R d，R 1， R 2，R 3，R 4和R 5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。

5. 发明申请

WO2004009017A3 MODULATORS OF THE GLUCOCORTICOID RECEPTOR AND METHOD 审中-公开
标题翻译：糖皮质激素受体的调节因子和方法
公开(公告)号：WO2004009017A3
公开(公告)日：2004-07-08
申请号：PCT/US0322300
申请日：2003-07-17
申请人： SQUIBB BRISTOL MYERS CO , VACCARO WAYNE , YANG BINGWEI VERA , KIM SOONG-HOON , HUYNH TRAM , TORTOLANI DAVID R , LEAVITT KENNETH J , LI WENYING , DOWEYKO ARTHUR M , CHEN XIAO-TAO , DOWEYKO LIDIA
发明人： VACCARO WAYNE , YANG BINGWEI VERA , KIM SOONG-HOON , HUYNH TRAM , TORTOLANI DAVID R , LEAVITT KENNETH J , LI WENYING , DOWEYKO ARTHUR M , CHEN XIAO-TAO , DOWEYKO LIDIA
IPC分类号： A61K31/403 , A61K31/415 , A61K31/425 , A61K31/473 , A61K31/495 , A61K45/06 , C07D207/34 , C07D209/48 , C07D213/40 , C07D213/75 , C07D213/82 , C07D215/38 , C07D217/22 , C07D231/16 , C07D233/88 , C07D235/10 , C07D235/14 , C07D235/30 , C07D239/42 , C07D239/94 , C07D241/20 , C07D261/12 , C07D261/14 , C07D263/48 , C07D277/46 , C07D277/64 , C07D285/06 , C07D307/58 , C07D317/58 , C07D333/20 , C07D333/34 , C07D401/04 , C07D405/04 , C07D417/04 , C07D417/10 , C07D417/12 , C07D471/04 , C07D471/08 , C07D487/04 , C07D495/04 , A61K31/50
CPC分类号： C07D495/04 , A61K31/403 , A61K31/473 , A61K45/06 , C07D207/34 , C07D209/48 , C07D213/40 , C07D213/75 , C07D213/82 , C07D215/38 , C07D217/22 , C07D231/16 , C07D233/88 , C07D235/14 , C07D235/30 , C07D239/42 , C07D239/94 , C07D241/20 , C07D261/12 , C07D261/14 , C07D263/48 , C07D277/46 , C07D277/64 , C07D285/06 , C07D307/58 , C07D317/58 , C07D333/20 , C07D333/34 , C07D401/04 , C07D405/04 , C07D417/04 , C07D417/10 , C07D417/12 , C07D471/04 , C07D471/08 , C07D487/04 , A61K2300/00
摘要： Novel non-steroidal compounds are provided which are glucocorticoid receptor modulators which are useful in treating diseases requiring glucocorticoid receptor agonist or antagonist therapy such as obesity, diabetes, inflammatory and immune disorders, and have the structure formula (I), where Z is CONR R or CH NR R and where R, R , R , R , R , Z, A and B are defined herein.
摘要翻译：提供了新的非类固醇化合物，其为糖皮质激素受体调节剂，其可用于治疗需要糖皮质激素受体激动剂或拮抗剂治疗如肥胖症，糖尿病，炎症和免疫疾病的疾病，并且具有结构式（I），其中Z是CONR < 其中R 1，R 2，或CH 2 NR 1 R 2和其中R，R a，R b，R c，R d，Z，A和B被定义为于此。

6. 发明申请

WO1992021677A1 bibNUCLIDINE DERIVATIVES 审中-公开
标题翻译： bibNUCLIDINE衍生物
公开(公告)号：WO1992021677A1
公开(公告)日：1992-12-10
申请号：PCT/US1992003317
申请日：1992-04-28
申请人： PFIZER INC. , ITO, Fumitaka , KONDO, Hiroshi , SHIMADA, Kaoru , NAKANE, Masami , LOWE, John, Adams, III , ROSEN, Terry, Jay , YANG, Bingwei, Vera
发明人： PFIZER INC.
IPC分类号： C07D453/02
CPC分类号： C07D453/02
摘要： Compounds of formula (I), wherein R is methoxy and R is selected from the group consisting of methyl, ethyl, isopropyl, sec-butyl and tert-butyl; and the pharmaceutically acceptable salts of such compounds. These compounds are substance P antagonists and useful in the treatment of gastrointestinal disorders, inflammatory disorders, central nervous system disorders and pain.
摘要翻译：式（I）化合物，其中R 1是甲氧基，R 2选自甲基，乙基，异丙基，仲丁基和叔丁基; 和这些化合物的药学上可接受的盐。这些化合物是物质P拮抗剂，可用于治疗胃肠道疾病，炎性疾病，中枢神经系统疾病和疼痛。

7. 发明申请

WO2008057862A2 MODULATORS OF GLUCOCORTICOID RECEPTOR, AP-1, AND/OR NF-κB 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：WO2008057862A2
公开(公告)日：2008-05-15
申请号：PCT/US2007/083094
申请日：2007-10-31
申请人： BRISTOL-MYERS SQUIBB COMPANY , YANG, Bingwei Vera , DOWEYKO, Lidia M. , VACCARO, Wayne , HUYNH, Tram N. , TORTOLANI, David R. , DHAR, T.g. Murali
发明人： YANG, Bingwei Vera , DOWEYKO, Lidia M. , VACCARO, Wayne , HUYNH, Tram N. , TORTOLANI, David R. , DHAR, T.g. Murali
IPC分类号： C07C235/36 , C07D213/75 , C07D231/40 , C07D233/88 , C07D239/42 , C07D241/20
CPC分类号： C07D211/58 , C07C235/36 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07D213/75 , C07D231/40 , C07D233/88 , C07D239/42 , C07D277/46 , C07D277/82 , C07D285/08 , C07D285/135 , C07D417/04 , C07D417/10 , C07D417/12
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-κB activity including inflammatory and immune diseases, obesity and diabetes having the structure of formula (I) an enantiomer, diastereomer, tautomer, solvate (e.g. a hydrate), or a pharmaceutically-acceptable salt, thereof, wherein: M is selected from alkyl, substituted alkyl, cycloalkyl, aryl, heterocyclo, and heteroaryl, provided that if M is alkyl then R 6 and R 7 taken together with the carbon atom to which they are both attached are selected from a group other than cycloalkyl; Q is selected from (i) hydrogen, C 1 -C 4 alkyl, and substituted C 1 -C 4 alkyl; or (ii) Q and R 6 are combined with the carbon atoms to which they are attached to form a 3- to 6-membered cycloalkyl; or (iii) Q and M a M are combined with the carbon atom(s) to which they are attached to form a 3- to 7-membered ring containing 1-2 heteroatoms which are independently selected from the group consisting of O, S, SO 2 , and N which ring may be optionally substituted with 0-2 R 5 groups or carbonyl; Z is selected from cycloalkyl, heterocyclo, aryl, or heteroaryl; and M a , Z a , R 1 , R 2 , R 3 , R 4 , R 6 , R 7 , and R 22 are as defined herein. Also provided are pharmaceutical compositions and methods of treating metabolic and inflammatory- or immune-associated diseases or disorders using 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）结构的炎性和免疫疾病，肥胖症和糖尿病，对映体，非对映异构体，互变异构体，溶剂化物（例如水合物）或其药学上可接受的盐，其中：M选自烷基，取代的烷基，环烷基，芳基，杂环和杂芳基，条件是如果M是烷基，则 R 6和R 7与它们所连接的碳原子一起选自除环烷基之外的基团; Q选自（i）氢，C 1 -C 4烷基和取代的C 1 -C 4烷基烷基; 或（ii）Q和R 6与它们所连接的碳原子结合形成3-至6-元环烷基; 或（iii）Q和M a a M与它们所连接的碳原子一起形成含有1-2个杂原子的3-至7-元环，其独立地选自由O，S，SO 2和N组成的基团可以任选地被0-2个R 5基团或羰基取代; Z选自环烷基，杂环基，芳基或杂芳基; 和M a a，Z a，R 1，R 2，R 3， R 4，R 6，R 7和R 22如本文所定义。还提供了使用所述化合物治疗代谢和炎症或免疫相关疾病或病症的药物组合物和方法。

8. 发明申请

WO2008057857A1 MODULATORS OF GLUCOCORTICOID RECEPTOR, AP-1, AND/OR NF-κB 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：WO2008057857A1
公开(公告)日：2008-05-15
申请号：PCT/US2007/083085
申请日：2007-10-31
申请人： BRISTOL-MYERS SQUIBB COMPANY , SHEPPECK, James E. , GILMORE, John L. , DHAR, T. G. Murali , XIAO, Hai-Yun , WANG, Jianmin , YANG, Bingwei Vera , DOWEYKO, Lidia M.
发明人： SHEPPECK, James E. , GILMORE, John L. , DHAR, T. G. Murali , XIAO, Hai-Yun , WANG, Jianmin , YANG, Bingwei Vera , DOWEYKO, Lidia M.
IPC分类号： C07D231/56 , C07D401/12 , C07D403/12 , C07D409/12 , A61K31/416 , A61P29/02
CPC分类号： C07D231/56 , C07D401/12 , C07D403/12 , C07D409/12
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-κB activity including inflammatory and immune diseases, obesity and diabetes having the structure of formula (I), its enantiomers, diastereomers, or a pharmaceutically acceptable salt, or hydrate, thereof, wherein X is (Ia); or X is (Ib); or X is (Ic); (Id) is heterocycle or heteroaryl; E is -N-, -NR 1 -, -O-, -S-, -SO 2 - or -CR 2 -; F is -N-, -NR 1a -, -O-, -S-, SO 2 - or -CR 2a -; G is N, -NR 1b -, -O-, -S-, SO 2 - or -CR 2b -, provided that the E-F-G containing heterocyclic ring formed does not contain a S-S or S-O bond, and at least one of E, F and G is a heteroatom; J, J a , M, M a , Q, R x , R y , R 1 , R 1a , R 1b , R 2 , R 2a , R 2b , and R 3 to R 21 , Z, Z a , Z b , and Z c are as defined above.
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）结构的炎性和免疫疾病，肥胖症和糖尿病，，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（Ia）; 或X为（Ib）; 或X为（Ic）; （Id）是杂环或杂芳基; E为-N-，-NR 1 - ， - O - ， - S - ， - SO 2 - 或-CR 2 - 。 F是-N， - NR 1a - ， - O - ， - S - ，SO 2 - 或-CR 2a。 G是N，-NR 1b - ， - O - ， - S - ，SO 2 - 或-CR 2b - ，条件是形成的含有EFG的杂环不含有SS或SO键，E，F和G中的至少一个为杂原子; J，J a，M，M a，Q，R x，R y，R a， R 1，R 1a，R 1b，R 2，R 2a，R 3， 2b和R 3至R 21，Z，Z a，Z B 2和R 3， Z 如上所定义。

9. 发明申请

WO2005073203A1 MODULATORS OF GLUCOCORTICOID RECEPTOR, AP-1, AND/OR NF-κB 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：WO2005073203A1
公开(公告)日：2005-08-11
申请号：PCT/US2005/001794
申请日：2005-01-14
申请人： BRISTOL-MYERS SQUIBB COMPANY , YANG, Bingwei, Vera
发明人： YANG, Bingwei, Vera
IPC分类号： C07D277/44
CPC分类号： C07D417/12 , C07D277/46 , C07D417/08
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 pharmaceutically acceptable salt thereof, where Z is S, O or NH; and R, R 1 , R 2 R a , R b , R c , R d , Z, A and B 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，或其溶剂合物或其药学上可接受的盐，其中Z为S，O或NH; 并且R，R 1，R 2 R a，R b，R c，R d，Z，A和B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

WO2004009017A2 MODULATORS OF THE GLUCOCORTICOID RECEPTOR AND METHOD 审中-公开
标题翻译： GLUCOCORTICOID受体的调节剂和方法
公开(公告)号：WO2004009017A2
公开(公告)日：2004-01-29
申请号：PCT/US2003/022300
申请日：2003-07-17
申请人： BRISTOL-MYERS SQUIBB COMPANY , VACCARO, Wayne , YANG, Bingwei, Vera , KIM, Soong-Hoon , HUYNH, Tram , TORTOLANI, David, R. , LEAVITT, Kenneth, J. , LI, Wenying , DOWEYKO, Arthur, M. , CHEN, Xiao-Tao , DOWEYKO, Lidia
发明人： VACCARO, Wayne , YANG, Bingwei, Vera , KIM, Soong-Hoon , HUYNH, Tram , TORTOLANI, David, R. , LEAVITT, Kenneth, J. , LI, Wenying , DOWEYKO, Arthur, M. , CHEN, Xiao-Tao , DOWEYKO, Lidia
IPC分类号： A61K
CPC分类号： C07D495/04 , A61K31/403 , A61K31/473 , A61K45/06 , C07D207/34 , C07D209/48 , C07D213/40 , C07D213/75 , C07D213/82 , C07D215/38 , C07D217/22 , C07D231/16 , C07D233/88 , C07D235/14 , C07D235/30 , C07D239/42 , C07D239/94 , C07D241/20 , C07D261/12 , C07D261/14 , C07D263/48 , C07D277/46 , C07D277/64 , C07D285/06 , C07D307/58 , C07D317/58 , C07D333/20 , C07D333/34 , C07D401/04 , C07D405/04 , C07D417/04 , C07D417/10 , C07D417/12 , C07D471/04 , C07D471/08 , C07D487/04 , A61K2300/00
摘要： Novel non-steroidal compounds are provided which are glucocorticoid receptor modulators which are useful in treating diseases requiring glucocorticoid receptor agonist or antagonist therapy such as obesity, diabetes, inflammatory and immune disorders, and have the structure formula (I), where Z is CONR 1 R 2 or CH 2 NR 1 R 2 and where R, R a , R b , R c , R d , Z, A and B are defined herein.
摘要翻译：提供了新型非甾体化合物，其是糖皮质激素受体调节剂，其可用于治疗需要糖皮质激素受体激动剂或拮抗剂治疗如肥胖症，糖尿病，炎症和免疫疾病的疾病，并且具有结构式（I），其中Z为CONR < R 1，R 2或CH 2 NR 1 R 2，并且其中R，R a，R b，R c，R d，Z，A和B定义于此。

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