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1. 发明申请

US20120214767A1 TRICYCLIC HETEROCYCLIC COMPOUNDS 有权
标题翻译：三元杂环化合物
公开(公告)号：US20120214767A1
公开(公告)日：2012-08-23
申请号：US13504541
申请日：2010-10-29
申请人： T.G. Murali Dhar , Hai-Yun Xiao , Scott Hunter Watterson , Soo S. Ko , Alaric J. Dyckman , Charles M. Langevine , Jagabandhu Das
发明人： T.G. Murali Dhar , Hai-Yun Xiao , Scott Hunter Watterson , Soo S. Ko , Alaric J. Dyckman , Charles M. Langevine , Jagabandhu Das
IPC分类号： A61K31/423 , C07D498/04 , A61K31/454 , C07D413/04 , A61P37/00 , A61K31/5377 , C07F9/09 , A61K31/675 , A61P35/00 , A61P7/00 , C07D413/14 , A61K31/506
CPC分类号： C07D413/04 , C07D231/54 , C07D261/20 , C07D277/84 , C07D403/06 , C07D413/06 , C07D413/14 , C07D417/04 , C07D417/14 , C07D419/04 , C07D487/10 , C07D498/04
摘要： Disclosed are compounds of Formula (I) or stereoisomers or salts thereof, wherein: X1, X2, X3, W, Q1, Q2, and G2 are defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein-coupled receptor S1P1, 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）的化合物或其立体异构体或其盐，其中：X1，X2，X3，W，Q1，Q2和G2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（例如自身免疫性疾病和血管疾病）中的疾病或病症的进展。

2. 发明授权

US08067447B2 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：US08067447B2
公开(公告)日：2011-11-29
申请号：US12513192
申请日：2007-10-31
申请人： James E. Sheppeck , John L. Gilmore , T. G. Murali Dhar , Hai-Yun Xiao
发明人： James E. Sheppeck , John L. Gilmore , T. G. Murali Dhar , Hai-Yun Xiao
IPC分类号： A61K31/433 , A61K31/416 , C07D285/135 , C07D231/56 , C07D231/40
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-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.
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，和/或AP-1和/或NF-κB活性相关的疾病，包括炎性和免疫疾病，肥胖症和糖尿病，其结构为式（I），其对映异构体，非对映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。

3. 发明申请

US20100113532A1 MODULATORS OF THE 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：US20100113532A1
公开(公告)日：2010-05-06
申请号：US12631179
申请日：2009-12-04
申请人： T.G. Murali Dhar , Hai-Yun Xiao , Bingwei Yang
发明人： T.G. Murali Dhar , Hai-Yun Xiao , Bingwei Yang
IPC分类号： A61K31/4196 , C07D249/14 , C07D401/10 , C07D417/10 , A61K31/4439 , A61P19/02 , A61P3/10 , A61P11/06
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-κB activity including obesity, diabetes, inflammatory and immune diseases, and have the structure of formula (I) or (II): including a stereoisomer thereof, a tautomer thereof, 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, C2-6alkyl, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, halo, or alkoxy; and A, B, R, Ra, Rb, Rc and Rd 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，包括肥胖症，糖尿病，炎症和免疫疾病，并且具有式（I）或（II）的结构：包括其立体异构体，其互变异构体，其前体药物或其药学上可接受的盐，其中Q选自N，O和S; 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A，B，R，Ra，Rb，Rc和Rd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。

4. 发明申请

US20100076014A1 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：US20100076014A1
公开(公告)日：2010-03-25
申请号：US12513192
申请日：2007-10-31
申请人： James E. Sheppeck , John l. Gilmore , T.G. Murali Dhar , Hai-Yun Xiao
发明人： James E. Sheppeck , John l. Gilmore , T.G. Murali Dhar , Hai-Yun Xiao
IPC分类号： A61K31/427 , C07D417/12 , C07D417/14 , C07D401/12 , C07D471/04 , A61K31/433 , A61K31/4439 , A61K31/454 , A61K31/437 , A61P3/00 , A61P29/00 , A61P37/00
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-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.
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，和/或AP-1和/或NF-κB活性相关的疾病，包括炎性和免疫疾病，肥胖症和糖尿病，其结构为式（I），其对映异构体，非对映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。

5. 发明授权

US06639074B2 Process for preparing azacycloalkanoylaminothiazoles 有权
标题翻译：制备氮杂环烷酰氨基噻唑的方法
公开(公告)号：US06639074B2
公开(公告)日：2003-10-28
申请号：US10100129
申请日：2002-03-18
申请人： Bang-Chi Chen , Kyoung S. Kim , S. David Kimball , Raj N. Misra , Mark E. Salvati , Joseph E. Sundeen , Hai-Yun Xiao , Rulin Zhao
发明人： Bang-Chi Chen , Kyoung S. Kim , S. David Kimball , Raj N. Misra , Mark E. Salvati , Joseph E. Sundeen , Hai-Yun Xiao , Rulin Zhao
IPC分类号： C07D47100
CPC分类号： C07D417/12 , A61K31/427 , A61K31/454 , C07D231/12 , C07D233/56 , C07D249/08 , C07D417/14
摘要： The present invention relates to new, efficient processes for the preparation of 5-(2-oxazolylalkylthio)-2-azacycloalkanoylaminothiazole compounds of formula I or a pharmaceutically acceptable salt thereof, wherein: R is alkyl, aryl or heteroaryl; R1, R2, R3, R4 and R5 are each independently hydrogen, alkyl, aryl or heteroaryl; R6 and R7 are each independently hydrogen, alkyl, aryl, heteroaryl, halogen, hydroxy or alkoxy; R8 is hydrogen, alkyl, aryl, heteroaryl, CONR9R10, COR11 or COOR12; R9, R10, R11 and R12 are each independently hydrogen, alkyl or aryl; m equals 0 to 5; and n equals 0 to 5, which are novel, potent inhibitors of cyclin dependent kinases (cdks). The present invention further concerns new key intermediate compounds, a quaternary ammonium salt of formula III′ and a 2-oxazolylalkyl derivative of formula IX.
摘要翻译：本发明涉及制备式I的5-（2-恶唑基烷硫基）-2-氮杂环烷酰氨基噻唑化合物或其药学上可接受的盐的新的，有效的方法，其中：R是烷基，芳基或杂芳基; R 1，R 2 R 3，R 4和R 5各自独立地为氢，烷基，芳基或杂芳基; R 6和R 7各自独立地为氢，烷基，芳基，杂芳基，卤素，羟基或烷氧基; R 8是氢，烷基，芳基，杂芳基，CONR 9 R 10，COR 11或COOR 12; R 9，R 10，R 11 且R 12各自独立地为氢，烷基或芳基; m等于0至5; 和等于0至5，这是细胞周期蛋白依赖性激酶（cdks）的新型有效抑制剂。本发明还涉及新的关键中间体化合物，式III'的季铵盐和式IX的2-恶唑基烷基衍生物。

6. 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。

7. 发明申请

US20100190820A1 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：US20100190820A1
公开(公告)日：2010-07-29
申请号：US12513228
申请日：2007-10-31
申请人： T. G. Murali Dhar , Hai-Yun Xiao , James E. Sheppeck
发明人： T. G. Murali Dhar , Hai-Yun Xiao , James E. Sheppeck
IPC分类号： A61K31/437 , C07D471/04 , A61P37/02
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-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 (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，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）：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 - ， - SO 2 - 或-CR 2 - ; 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S-S或S-O键， E，F和G中的至少一个是杂原子; 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

US20070179189A1 Modulators of the glucocorticoid receptor, AP-1, and/or NF-kB activity and use thereof 有权
标题翻译：糖皮质激素受体，AP-1和/或NF-kB活性的调节剂及其用途
公开(公告)号：US20070179189A1
公开(公告)日：2007-08-02
申请号：US11330749
申请日：2006-01-12
申请人： T.G. Dhar , Hai-Yun Xiao , Bingwei Yang
发明人： T.G. Dhar , Hai-Yun Xiao , Bingwei Yang
IPC分类号： A61K31/4439 , A61K31/426 , A61K31/4184 , C07D403/02
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-κB activity including obesity, diabetes, inflammatory and immune diseases, and have the structure of formula (I) or (II): including a stereoisomer thereof, a tautomer thereof, 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, C2-6alkyl, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, halo, or alkoxy; and A, B, R, Ra, Rb, Rc and Rd 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）或（II）：其中Q选自N，O和S;其包括其立体异构体，其互变异构体，其前药或其药学上可接受的盐; 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。

9. 发明申请

US20070088029A1 Tricycloundecane compounds useful as modulators of nuclear hormone receptor function 有权
标题翻译：三环十二烷化合物可用作核激素受体功能的调节剂
公开(公告)号：US20070088029A1
公开(公告)日：2007-04-19
申请号：US11581873
申请日：2006-10-17
申请人： James Balog , David Fairfax , Gregory Martin , Mark Salvati , Hai-Yun Xiao
发明人： James Balog , David Fairfax , Gregory Martin , Mark Salvati , Hai-Yun Xiao
IPC分类号： A61K31/5383 , A61K31/4745 , C07D491/14 , C07D471/14
CPC分类号： C07D498/18 , C07D471/18
摘要： Tricycloundecanes compounds, methods of using such compounds in the treatment of nuclear hormone receptor-associated conditions such as cancer and immune disorders, and pharmaceutical compositions containing such compounds are disclosed.
摘要翻译：公开了三环十四烷化合物，使用这些化合物治疗核激素受体相关病症如癌症和免疫疾病的方法，以及含有这些化合物的药物组合物。

10. 发明授权

US07141578B2 Fused heterocyclic succinimide compounds and analogs thereof, modulators of nuclear hormone receptor function 有权
公开(公告)号：US07141578B2
公开(公告)日：2006-11-28
申请号：US10974049
申请日：2004-10-25
申请人： Mark E. Salvati , James Aaron Balog , Dacia A. Pickering , Sören Giese , Aberra Fura , Wenying Li , Ramesh N. Patel , Ronald L. Hanson , Toomas Mitt , Jacques Y. Roberge , James R. Corte , Steven H. Spergel , Richard A. Rampulla , Raj N. Misra , Hai-Yun Xiao
发明人： Mark E. Salvati , James Aaron Balog , Dacia A. Pickering , Sören Giese , Aberra Fura , Wenying Li , Ramesh N. Patel , Ronald L. Hanson , Toomas Mitt , Jacques Y. Roberge , James R. Corte , Steven H. Spergel , Richard A. Rampulla , Raj N. Misra , Hai-Yun Xiao
IPC分类号： A61K31/44 , A61K31/40 , C07D491/00 , C07D487/00
CPC分类号： C07D487/18 , A61K31/00 , A61K31/403 , A61K31/407 , A61K31/655 , A61K31/675 , A61K45/06 , C07B2200/11 , C07D401/08 , C07D471/08 , C07D487/08 , C07D491/08 , C07D491/18 , C07D491/22 , C07D495/08 , C07D495/18 , C07D519/00 , C40B40/00 , A61K2300/00
摘要： Fused cyclic compounds, methods of using such compounds in the treatment of nuclear hormone receptor-associated conditions such as cancer and immune disorders, and pharmaceutical compositions containing such compounds.

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