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1. 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。

2. 发明申请

WO2006076633A1 MODULATORS OF THE 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：WO2006076633A1
公开(公告)日：2006-07-20
申请号：PCT/US2006/001329
申请日：2006-01-13
申请人： BRISTOL-MYERS SQUIBB COMPANY , YANG, Bingwei Vera , DOWEYKO, Lidia M. , DOWEYKO, Arthur M.
发明人： YANG, Bingwei Vera , DOWEYKO, Lidia M. , DOWEYKO, Arthur M.
IPC分类号： C07D277/56 , C07D233/90 , A61K31/426 , A61K31/4168 , A61P37/00
CPC分类号： C07D277/46 , C07D233/90 , C07D277/56
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), where X is S, O or N; Z is -T-COOR 1 or çT-COR 1 ;and T, R, R 1 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：提供了一类新型非甾体化合物，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，包括肥胖，糖尿病，炎症和免疫疾病，并具有结构式（I）的化合物，其中X是S，O或N; Z是-T-COOR 1或çT-COR 1;以及T，R，R 1，R 2， 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。

3. 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。

4. 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。

5. 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。

6. 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。

7. 发明申请

WO2005072132A3 TRICYCLIC MODULATORS OF THE GLUCOCORTICOID RECEPTOR, AP-1, AND/OR NF-κB ACTIVITY AND USE THEREOF 审中-公开
公开(公告)号：WO2005072132A3
公开(公告)日：2005-08-11
申请号：PCT/US2005/001180
申请日：2005-01-14
申请人： BRISTOL-MYERS SQUIBB COMPANY , WEINSTEIN, David, S. , YANG, Bingwei Vera , KIM, Soong-Hoon , VACCARO, Wayne , SHEPPECK, James , GILMORE, John
发明人： WEINSTEIN, David, S. , YANG, Bingwei Vera , KIM, Soong-Hoon , VACCARO, Wayne , SHEPPECK, James , GILMORE, John
IPC分类号： C07C233/58
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 obesity, diabetes, inflammatory and immune diseases, and have the structure of formula (I): or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein B, J, K, Z, R, R a , R b , R c , R d , R q , R w , m 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.

8. 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。

9. 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，

10. 发明申请

WO2006076702A1 MODULATORS OF THE GLUCOCORTICOID RECEPTOR, AP-1, AND/OR NF-ĸB 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：WO2006076702A1
公开(公告)日：2006-07-20
申请号：PCT/US2006/001482
申请日：2006-01-13
申请人： BRISTOL-MYERS SQUIBB COMPANY , DHAR, T., G., Murali , XIAO, Hai-yun , YANG, Bingwei Vera
发明人： DHAR, T., G., Murali , XIAO, Hai-yun , YANG, Bingwei Vera
IPC分类号： C07D249/14 , C07D403/10 , C07D401/10 , C07D401/04 , C07D277/46 , C07D417/10 , A61K31/4196 , A61K31/4436 , A61K31/4439
CPC分类号： C07D401/10 , C07D249/14 , C07D277/46 , C07D401/04 , C07D401/14 , C07D403/10 , C07D417/10
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) or (II): [INSERT CHEMICAL STRUCTURE HERE] including all stereoisomers thereof, tautomers thereof, or a prodrug thereof, or a pharmaceutically acceptable salt thereof, where Q is selected from N, O, and S; Y is aryl or heteroaryl; Z is H, C 2-6 alkyl, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, halo, or alkoxy; and A, B, 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：提供了一类新型非甾体化合物，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，包括肥胖，糖尿病，炎症和免疫疾病，并具有结构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，其中Q选自N，O和S;（I）或（II）的化合物： Y是芳基或杂芳基; Z是H，C 2-6烷基，环烷基，杂环烷基，芳基，杂芳基，卤素或烷氧基; 并且本文定义了A，B，R，R a，R b，R b，R c和R d。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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