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1. 发明申请

WO2008057855A2 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：WO2008057855A2
公开(公告)日：2008-05-15
申请号：PCT/US2007083083
申请日：2007-10-31
申请人： SQUIBB BRISTOL MYERS CO , DHAR T G MURALI , XIAO HAI-YUN , SHEPPECK JAMES E
发明人： DHAR T G MURALI , XIAO HAI-YUN , SHEPPECK JAMES E
CPC分类号： C07D471/04
摘要： Novel non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, and/or AP-1 and/or NF-?B 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 the group X is O or (R x )(R y ); is heterocyclo or heteroaryl; E is -N-, -NR 1 -, -O-, -C(=O), -S-, -SO 2 -, or -CR 2 -; F is -N-, -NR 1a , -O-, -C(=O), -S-, -SO 2 -, or -CR 2a -; G is independently N, -NR 1b -, -O-, -C(=O), -S-, -SO 2 - or -CR 2b - provided that the heterocyclic ring formed does not contain a S-S or S-O bond and at least one of E, F and G is a hetero atom; and Ma, R x , R y , R 1 , R 1a , R 1b , R 2 , R 2a , R 2b , R 4 , R 5a , R 6 , R 7 , X, Z a and Z are as defined herein. Also provided are pharmaceutical compositions and methods of treating inflammatory- or immune-associated diseases employing said compounds.
摘要翻译：提供了新的非甾体化合物，其可用于治疗与糖皮质激素受体的调节有关的疾病和/或AP-1和/或NF-κB活性，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，其中基团X为O或（R x x）O（R y）; 是杂环基或杂芳基; E是-N-，-NR 1 - ， - O - ， - C（= O），-S - ， - SO 2 - 或-CR _{2 - ; F是-N，-NR 1a，-O - ， - C（= O）， - S - ， - SO 2 - 或-CR 图2a - ; G独立地为N，-NR1B1 - ， - O - ， - C（= O），-S-，-SO2-或-CR2b - 条件是所形成的杂环不含有SS或SO键，并且E，F和G中的至少一个为杂原子; 和M a，R x，R y，R 1，R 1a，R 1b， R 2，R 2，R 2a，R 2b，R 4，R 5a， R 6，R 6，R 7，X，Z a a和Z如本文所定义。还提供了使用所述化合物治疗炎性或免疫相关疾病的药物组合物和方法。}

2. 发明申请

WO0110890A2 SYNTHESIS OF PROTEASE SUBSTRATES 审中-公开
标题翻译：蛋白质底物的合成
公开(公告)号：WO0110890A2
公开(公告)日：2001-02-15
申请号：PCT/US0021710
申请日：2000-08-08
申请人： CHEMRX ADVANCED TECHNOLOGIES I , COLLINS NATHAN , GOSINK LUKE J , SHEPPECK JAMES E II
发明人： COLLINS NATHAN , GOSINK LUKE J , SHEPPECK JAMES E II
IPC分类号： C07K1/04 , C07K5/09 , C07K1/00
CPC分类号： C40B50/14 , C07B2200/11 , C07K1/04 , C07K1/047 , C07K5/0815
摘要： The present invention provides a process for synthesizing a compound or an array of compounds of Formula (I) and Formula (-6) wherein peptidal substrates are bound to a solid support and a fluorescent moiety. Also provided is a process for synthesizing compounds of Formula (II) wherein peptidal substrates are bound to a fluorescent moiety. These related processes afford said peptidal substrates having a varied structural order.
摘要翻译：本发明提供了合成式（I）和式（-6）的化合物或阵列的方法，其中肽基底与固体支持物和荧光部分结合。还提供了合成式（II）化合物的方法，其中肽基底与荧光部分结合。这些相关过程提供了具有不同结构顺序的所述肽基底。

3. 发明申请

WO2011017578A1 SPHINGOSINE-1-PHOSPHATE RECEPTOR AGONISTS 审中-公开
标题翻译：丝氨酸1-磷酸酯受体激动剂
公开(公告)号：WO2011017578A1
公开(公告)日：2011-02-10
申请号：PCT/US2010/044627
申请日：2010-08-06
申请人： BRISTOL-MYERS SQUIBB COMPANY , GILMORE, John L. , SHEPPECK, James E.
发明人： GILMORE, John L. , SHEPPECK, James E.
IPC分类号： C07D413/14 , C07D417/14 , A61P29/00 , A61K31/4245 , A61K31/454 , A61K31/5377 , A61K31/496
CPC分类号： C07D413/14 , C07D417/14
摘要： Disclosed are compounds of Formula (I), or a stereoisomer or a pharmaceutically acceptable salt thereof, wherein: A is formula (II) Q is a substituted 5-membered monocyclic heteroaryl group; W is CH 2 , O, or NH; and R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , m, n, t, and x are defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein-coupled receptor S1P 1 , and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.
摘要翻译：公开了式（I）化合物或其立体异构体或其药学上可接受的盐，其中：A为式（II）Q为取代的5元单环杂芳基; W是CH 2，O或NH; 并且R 1，R 2，R 3，R 4，R 5，R 6，m，n，t和x在本文中定义。还公开了使用这种化合物作为G蛋白偶联受体S1P1的选择性激动剂的方法，以及包含这些化合物的药物组合物。这些化合物可用于治疗，预防或减缓各种治疗领域（例如自身免疫疾病和血管疾病）中的疾病或病症的进展。

4. 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。

5. 发明申请

WO2008057856A3 MODULATORS OF GLUCOCORTICOID RECEPTOR, AP-1 AND/OR NF-KAPPAB ACTIVITY AND USE THEREOF 审中-公开
公开(公告)号：WO2008057856A3
公开(公告)日：2008-05-15
申请号：PCT/US2007/083084
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
发明人： SHEPPECK, James E. , GILMORE, John L. , DHAR, T. G. Murali , XIAO, Hai-Yun
IPC分类号： C07D417/12 , C07D231/56 , C07D403/12 , C07D409/12 , C07D417/14 , C07D471/04 , A61K31/427 , A61P29/00
摘要： Novel non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, and/or 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 (Ia) is heterocycle or heteroaryl; J, Ja, E, F, G, Ma, M, Q, Za and Z 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.

6. 发明申请

WO2008057856A2 MODULATORS OF GLUCOCORTICOID RECEPTOR, AP-1, AND/OR NF-?B 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：WO2008057856A2
公开(公告)日：2008-05-15
申请号：PCT/US2007083084
申请日：2007-10-31
申请人： SQUIBB BRISTOL MYERS CO , SHEPPECK JAMES E , GILMORE JOHN L , DHAR T G MURALI , XIAO HAI-YUN
发明人： SHEPPECK JAMES E , GILMORE JOHN L , DHAR T G MURALI , XIAO HAI-YUN
IPC分类号： C07D417/12 , A61K31/427 , A61P29/00 , C07D231/56 , C07D403/12 , C07D409/12 , C07D417/14 , C07D471/04
CPC分类号： C07D231/56 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D417/12 , C07D417/14
摘要： Novel non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, and/or AP-1, and/or NF-?B 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 (Ia) is heterocycle or heteroaryl; J, Ja, E, F, G, Ma, M, Q, Za and Z 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：提供新的非甾体化合物，其可用于治疗与调节糖皮质激素受体，和/或AP-1和/或NF-κB活性相关的疾病，包括具有结构式的炎性和免疫疾病，肥胖症和糖尿病（I）化合物，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（Ia）是杂环或杂芳基; J，Ja，E，F，G，Ma，M，Q，Za和Z如本文所定义。还提供了使用所述化合物治疗炎性或免疫相关疾病和肥胖症和糖尿病的药物组合物和方法。

7. 发明申请

WO2008057855A9 HETEROCYCLIC COMPOUNDS AS MODULATORS OF GLUCOCORTICOID RECEPTOR, AP-I, AND/OR NP-KAPPA-B ACTIVITY 审中-公开
标题翻译：作为GLUCOCORTICOID受体，AP-I和/或NP-KAPPA-B活性的调节剂的杂环化合物
公开(公告)号：WO2008057855A9
公开(公告)日：2009-06-18
申请号：PCT/US2007083083
申请日：2007-10-31
申请人： SQUIBB BRISTOL MYERS CO , DHAR T G MURALI , XIAO HAI-YUN , SHEPPECK JAMES E
发明人： DHAR T G MURALI , XIAO HAI-YUN , SHEPPECK JAMES E
IPC分类号： C07D471/04 , A61K31/437 , A61P3/00 , A61P29/00 , A61P37/00
CPC分类号： C07D471/04
摘要： Novel non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, and/or AP-1 and/or NF-?B 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 the group X is O or (Rx)(Ry); is heterocyclo or heteroaryl; E is -N-, -NR1-, -O-, -C(=O), -S-, -SO2-, or -CR2-; F is -N-, -NR1a, -O-, -C(=O), -S-, -SO2-, or -CR2a-; G is independently N, -NR1b-, -O-, -C(=O), -S-, -SO2- or -CR2b- provided that the heterocyclic ring formed does not contain a S-S or S-O bond and at least one of E, F and G is a hetero atom; and Ma, Rx, Ry, R1, R1a, R1b, R2, R2a, R2b, R4, R5a, R6, R7, X, Za and Z are as defined herein. Also provided are pharmaceutical compositions and methods of treating inflammatory- or immune-associated diseases employing said compounds.
摘要翻译：提供新的非甾体化合物，其可用于治疗与糖皮质激素受体和/或AP-1和/或NF-κB活性相关的疾病，包括具有结构式（1）的炎性和免疫疾病，肥胖症和糖尿病 I）：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，其中基团X为O或（Rx）（Ry）; 是杂环基或杂芳基; E是-N-，-NR1 - ， - O - ， - C（= O），-S-，-SO2-或-CR2-; F是-N-，-NR1a，-O-，-C（= O），-S-，-SO2 - 或-CR2a; G独立地为N，-NR1b - ， - O - ， - C（= O）， - S - ， - SO2-或-CR2b-，条件是所形成的杂环不含有SS或SO键， E，F和G是杂原子; 并且Ma，Rx，Ry，R1，R1a，R1b，R2，R2a，R2b，R4，R5a，R6，R7，X，Za和Z如本文所定义。还提供了使用所述化合物治疗炎性或免疫相关疾病的药物组合物和方法。

8. 发明申请

WO2008057855A3 HETEROCYCLIC COMPOUNDS AS MODULATORS OF GLUCOCORTICOID RECEPTOR, AP-I, AND /OR NP-KAPPA-B ACTIVITY 审中-公开
公开(公告)号：WO2008057855A3
公开(公告)日：2008-05-15
申请号：PCT/US2007/083083
申请日：2007-10-31
申请人： BRISTOL-MYERS SQUIBB COMPANY , DHAR, T.g. Murali , XIAO, Hai-yun , SHEPPECK, James E.
发明人： DHAR, T.g. Murali , XIAO, Hai-yun , SHEPPECK, James E.
IPC分类号： C07D471/04 , A61K31/437 , A61P3/00 , A61P29/00 , A61P37/00
摘要： Novel non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, and/or 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 the group X is O or (R x )(R y ); is heterocyclo or heteroaryl; E is -N-, -NR 1 -, -O-, -C(=O), -S-, -SO 2 -, or -CR 2 -; F is -N-, -NR 1a , -O-, -C(=O), -S-, -SO 2 -, or -CR 2a -; G is independently N, -NR 1b -, -O-, -C(=O), -S-, -SO 2 - or -CR 2b - provided that the heterocyclic ring formed does not contain a S-S or S-O bond and at least one of E, F and G is a hetero atom; and Ma, R x , R y , R 1 , R 1a , R 1b , R 2 , R 2a , R 2b , R 4 , R 5a , R 6 , R 7 , X, Z a and Z are as defined herein. Also provided are pharmaceutical compositions and methods of treating inflammatory- or immune-associated diseases employing said compounds.

9. 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。

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