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1. 发明授权

US07544808B2 Tricyclic modulators of the glucocorticoid receptor, AP-1, and/or NF-κB activity and use thereof 有权
标题翻译：糖皮质激素受体，AP-1和/或NF-κB活性的三环调节剂及其用途
公开(公告)号：US07544808B2
公开(公告)日：2009-06-09
申请号：US11773506
申请日：2007-07-05
申请人： David S. Weinstein , John L. Gilmore , James Sheppeck , Bingwei Vera Yang , Soong-Hoon Kim , Wayne Vaccaro
发明人： David S. Weinstein , John L. Gilmore , James Sheppeck , Bingwei Vera Yang , Soong-Hoon Kim , Wayne Vaccaro
IPC分类号： C07D277/20 , A61K31/425
CPC分类号： C07D417/12 , A23K20/168 , A23K50/40 , C07D233/88 , C07D277/46 , C07D405/12 , C07D453/06
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, Ra, Rb, Rc, Rd, Rq, Rw, 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.
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，AP-1和/或NF-κB活性的调节相关的疾病，包括肥胖，糖尿病，炎症和免疫疾病，并且具有式（I ）或其立体异构体或前药或其药学上可接受的盐，其中B，J，K，Z，R，Ra，Rb，Rc，Rd，Rq，Rw，m和n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。

2. 发明授权

US07253283B2 Tricyclic modulators of the glucocorticoid receptor, AP-1, and/or NF-κB activity and use thereof 有权
标题翻译：糖皮质激素受体，AP-1和/或NF-κB活性的三环调节剂及其用途
公开(公告)号：US07253283B2
公开(公告)日：2007-08-07
申请号：US11035176
申请日：2005-01-13
申请人： David S. Weinstein , John L. Gilmore , James Sheppeck , Bingwei Vera Yang , Soong-Hoon Kim , Wayne Vaccaro
发明人： David S. Weinstein , John L. Gilmore , James Sheppeck , Bingwei Vera Yang , Soong-Hoon Kim , Wayne Vaccaro
IPC分类号： C07D417/02 , C07D413/02 , A61K31/473
CPC分类号： C07D417/12 , A23K20/168 , A23K50/40 , C07D233/88 , C07D277/46 , C07D405/12 , C07D453/06
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, Ra, Rb, Rc, Rd, Rq, Rw, 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.
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，AP-1和/或NF-κB活性的调节相关的疾病，包括肥胖，糖尿病，炎症和免疫疾病，并且具有式（I ）或其立体异构体或前药或其药学上可接受的盐，其中B，J，K，Z，R，R a，R b，R b， >，R“，R”，“O”，m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。

3. 发明授权

US06995181B2 Modulators of the glucocorticoid receptor and method 有权
标题翻译：糖皮质激素受体的调节剂和方法
公开(公告)号：US06995181B2
公开(公告)日：2006-02-07
申请号：US10621909
申请日：2003-07-17
申请人： Wayne Vaccaro , Bingwei Vera Yang , Soong-Hoon Kim , Tram Huynh , David R. Tortolani , Kenneth J. Leavitt , Wenying Li , Arthur M. Doweyko , Xiao-Tao Chen , Lidia Doweyko
发明人： Wayne Vaccaro , Bingwei Vera Yang , Soong-Hoon Kim , Tram Huynh , David R. Tortolani , Kenneth J. Leavitt , Wenying Li , Arthur M. Doweyko , Xiao-Tao Chen , Lidia Doweyko
IPC分类号： A61K31/426 , C07D277/38
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 where Z is CONR1R2 or CH2NR1R2 and where R, Ra, Rb, Rc, Rd, 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的疾病，例如肥胖症，糖尿病，炎症和免疫疾病，并且具有结构

4. 发明申请

US20090075995A1 MODULATORS OF GLUCOCORTICOID RECEPTOR, AP-1, AND/OR NF-kB ACTIVITY AND USE THEREOF 有权
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：US20090075995A1
公开(公告)日：2009-03-19
申请号：US11835438
申请日：2007-08-08
申请人： David S. Weinstein , Ping Chen , T.G. Murali Dhar , Jingwu Duan , Hua Gong , Bin Jiang , Bingwei Vera Yang , Arthur M. Doweyko
发明人： David S. Weinstein , Ping Chen , T.G. Murali Dhar , Jingwu Duan , Hua Gong , Bin Jiang , Bingwei Vera Yang , Arthur M. Doweyko
IPC分类号： A61K31/5377 , A61K31/436 , C07D491/052 , A61P31/12 , A61K31/427 , C07D417/12
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-κB 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 R5, R6, R7, and R8; J1, J2, and J3 are at each occurrence the same or different and are independently -A1QA2-; Q is a bond, O, S, S(O), or S(O)2; A1 and A2 are the same or different and are at each occurrence independently selected from a bond, C1-3alkylene, substituted C1-3alkylene, C2-4alkenylene, and substituted C2-4alkenylene, provided that A1 and A2 are chosen so that ring A is a 5- to 8-membered carbocyclic or heterocyclic ring; R1 to R11 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）调节相关的疾病：对映异构体，非对映异构体或其互变异构体，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，杂环基或杂芳基环，其中每个环与相邻原子上的A环稠合并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R5，R6， R7和R8; J1，J2和J3各自出现相同或不同，独立地为-A1QA2-; 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，条件是选择A1和A2使得环A为 5-至8-元碳环或杂环; R1至R11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。

5. 发明授权

US08198311B2 Modulators of glucocorticoid receptor, AP-1, and/or NF-κB activity and use thereof 有权
标题翻译：糖皮质激素受体，AP-1和/或NF-κB活性的调节剂及其用途
公开(公告)号：US08198311B2
公开(公告)日：2012-06-12
申请号：US12513232
申请日：2007-10-31
申请人： James E. Sheppeck , John L. Gilmore , T. G. Murali Dhar , Hai-Yun Xiao , Jianmin Wang , Bingwei Vera Yang , Lidia M. Doweyko
发明人： James E. Sheppeck , John L. Gilmore , T. G. Murali Dhar , Hai-Yun Xiao , Jianmin Wang , Bingwei Vera Yang , Lidia M. Doweyko
IPC分类号： A61K31/416 , C07D231/56
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—, —NR1—, —O—, —S—, —SO2— or —CR2—; F is —N—, —NR1a—, —O—, —S—, —SO2— or —CR2a—; G is N, —NR1b—, —O—, —S—, —SO2— or —CR2b—, 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, Ja, M, Ma, Q, Rx, Ry, R1, R1a, R1b, R2, R2a, R2b, and R3 to R21, Z, Za, Zb, and Zc 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是-N-，-NR1 - ， - O - ， - S - ， - SO2-或-CR2-; F是-N-，-NR1 - ， - O - ， - S - ， - SO2-或-CR2a-; G是N，-NR1b - ， - O - ， - S - ， - SO2-或-CR2b-，条件是所形成的含有EFG的杂环不含S-S或S-O键， E，F和G是杂原子; J，Ja，M，Ma，Q，Rx，Ry，R1，R1a，R1b，R2，R2a，R2b和R3至R21，Z，Za，Zb和Zc如上所定义。

6. 发明申请

US20100063051A1 MODULATORS OF GLUCOCORTICOID RECEPTOR, AP-1, AND/OR NF-kB ACTIVITY AND USE THEREOF 有权
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：US20100063051A1
公开(公告)日：2010-03-11
申请号：US12513187
申请日：2007-10-31
申请人： Bingwei Vera Yang , Lidia M. Doweyko , Wayne Vaccaro , Tram N. Huynh , David R. Tortolani , T.G. Murali Dhar
发明人： Bingwei Vera Yang , Lidia M. Doweyko , Wayne Vaccaro , Tram N. Huynh , David R. Tortolani , T.G. Murali Dhar
IPC分类号： A61K31/5377 , C07D277/38 , C07D417/12 , A61K31/426 , A61P37/00 , A61P29/00
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 R6 and R7 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, C1-C4 alkyl, and substituted C1-C4 alkyl; or (ii) Q and R6 are combined with the carbon atoms to which they are attached to form a 3- to 6-membered cycloalkyl; or (iii) Q and MaM 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, SO2, and N which ring may be optionally substituted with 0-2 R5 groups or carbonyl; Z is selected from cycloalkyl, heterocyclo, aryl, or heteroaryl; and Ma, Za, R1, R2, R3, R4, R6, R7, and R22 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，非对映体，互变异构体，溶剂合物（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是烷基那么R6和R7与它们所连接的碳原子一起选自除环烷基以外的基团; Q选自（i）氢，C 1 -C 4烷基和取代的C 1 -C 4烷基; 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MaM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O，S，SO 2 和N，该环可以任选地被0-2个R5基或羰基取代; Z选自环烷基，杂环基，芳基或杂芳基; 并且Ma，Za，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。

7. 发明授权

US08034940B2 Modulators of glucocorticoid receptor, AP-1, and/or NF-κB activity and use thereof 有权
标题翻译：糖皮质激素受体，AP-1和/或NF-κB活性的调节剂及其用途
公开(公告)号：US08034940B2
公开(公告)日：2011-10-11
申请号：US11835438
申请日：2007-08-08
申请人： David S. Weinstein , Ping Chen , T. G. Murali Dhar , Jingwu Duan , Hua Gong , Bin Jiang , Bingwei Vera Yang , Arthur M. Doweyko
发明人： David S. Weinstein , Ping Chen , T. G. Murali Dhar , Jingwu Duan , Hua Gong , Bin Jiang , Bingwei Vera Yang , Arthur M. Doweyko
IPC分类号： C07D491/052 , A61K31/436
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-κB 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 R5, R6, R7, and R8; J1, J2, and J3 are at each occurrence the same or different and are independently -A1QA2-; Q is a bond, O, S, S(O), or S(O)2; A1 and A2 are the same or different and are at each occurrence independently selected from a bond, C1-3alkylene, substituted C1-3alkylene, C2-4alkenylene, and substituted C2-4alkenylene, provided that A1 and A2 are chosen so that ring A is a 5- to 8-membered carbocyclic or heterocyclic ring; R1 to R11 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：其对映异构体，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，杂环基或杂芳基环，其中每个环与相邻原子上的A环稠合并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R5，R6， R7和R8; J1，J2和J3各自出现相同或不同，独立地为-A1QA2-; 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，条件是选择A1和A2使得环A为 5-至8-元碳环或杂环; R1至R11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。

8. 发明授权

US07968577B2 Modulators of glucocorticoid receptor, AP-1, and/or NF-κB activity and use thereof 有权
标题翻译：糖皮质激素受体，AP-1和/或NF-κB活性的调节剂及其用途
公开(公告)号：US07968577B2
公开(公告)日：2011-06-28
申请号：US12513187
申请日：2007-10-31
申请人： Bingwei Vera Yang , Lidia M. Doweyko , Wayne Vaccaro , Tram N. Huynh , David R. Tortolani , T. G. Murali Dhar
发明人： Bingwei Vera Yang , Lidia M. Doweyko , Wayne Vaccaro , Tram N. Huynh , David R. Tortolani , T. G. Murali Dhar
IPC分类号： A61K31/5377 , A61K31/5375 , A61K31/505 , A61K31/50 , A61K31/4965 , A61K31/496 , A61K31/4709 , A61K31/454 , A61K31/4439 , A61K31/433 , A61K31/426 , A61K31/427 , A61K31/428 , A61K31/421 , A61K31/4168 , A61K31/415 , A61K31/165 , C07D417/04 , C07D417/12 , C07D277/46 , C07D285/135 , C07D263/48 , C07D241/20 , C07D239/42 , C07D233/88 , C07D231/44
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 R6 and R7 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, C1-C4 alkyl, and substituted C1-C4 alkyl; or (ii) Q and R6 are combined with the carbon atoms to which they are attached to form a 3- to 6-membered cycloalkyl; or (iii) Q and MaM 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, SO2, and N which ring may be optionally substituted with 0-2 R5 groups or carbonyl; Z is selected from cycloalkyl, heterocyclo, aryl, or heteroaryl; and Ma, Za, R1, R2, R3, R4, R6, R7, and R22 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，非对映体，互变异构体，溶剂合物（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是烷基那么R6和R7与它们所连接的碳原子一起选自除环烷基以外的基团; Q选自（i）氢，C 1 -C 4烷基和取代的C 1 -C 4烷基; 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MaM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O，S，SO 2 和N，该环可以任选地被0-2个R5基或羰基取代; Z选自环烷基，杂环基，芳基或杂芳基; 并且Ma，Za，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。

9. 发明申请

US20100075961A1 MODULATORS OF GLUCOCORTICOID RECEPTOR, AP-1, AND/OR NF-kB ACTIVITY AND USE THEREOF 有权
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：US20100075961A1
公开(公告)日：2010-03-25
申请号：US12513232
申请日：2007-10-31
申请人： James E. Sheppeck , John L. Gilmore , T. G. Murali Dhar , Hai-Yun Xiao , Jianmin Wang , Bingwei Vera Yang , Lidia M. Doweyko
发明人： James E. Sheppeck , John L. Gilmore , T. G. Murali Dhar , Hai-Yun Xiao , Jianmin Wang , Bingwei Vera Yang , Lidia M. Doweyko
IPC分类号： A61K31/416 , C07D231/56 , C07D413/12 , A61K31/5377 , A61P3/00 , A61P29/00 , A61P37/00
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—, —NR1—, —O—, —S—, —SO2— or —CR2—; F is —N—, —NR1a—, —O—, —S—, —SO2— or —CR2a—; G is N, —NR1b—, —O—, —S—, —SO2— or —CR2b—, 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, Ja, M, Ma, Q, Rx, Ry, R1, R1a, R1b, R2, R2a, R2b, and R3 to R21, Z, Za, Zb, and Zc 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是-N-，-NR1 - ， - O - ， - S - ， - SO2-或-CR2-; F是-N-，-NR1 - ， - O - ， - S - ， - SO2-或-CR2a-; G是N，-NR1b - ， - O - ， - S - ， - SO2-或-CR2b-，条件是所形成的含有EFG的杂环不含S-S或S-O键， E，F和G是杂原子; J，Ja，M，Ma，Q，Rx，Ry，R1，R1a，R1b，R2，R2a，R2b和R3至R21，Z，Za，Zb和Zc如上所定义。

10. 发明授权

US08106046B2 Cyclopentathiophene modulators of the glucocorticoid receptor, AP-1, and/or NF-κB activity and use thereof 有权
标题翻译：糖皮质激素受体，AP-1和/或NF-κB活性的环戊噻吩调节剂及其用途
公开(公告)号：US08106046B2
公开(公告)日：2012-01-31
申请号：US12996806
申请日：2009-06-24
申请人： Bingwei Vera Yang
发明人： Bingwei Vera Yang
IPC分类号： C07D413/14 , C07D417/12 , A61K31/433 , A61K31/5377 , A61P19/02 , A61P29/00
CPC分类号： C07D417/12
摘要： A compound of Formula (I) and enantiomers, diastereomers and pharmaceutically-acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6, R7 and R8 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。

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