专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

21. 发明授权

US07569689B2 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活性的调节剂及其用途
公开(公告)号：US07569689B2
公开(公告)日：2009-08-04
申请号：US11034652
申请日：2005-01-13
申请人： Jingwu Duan , Bin Jiang , James Sheppeck , John L. Gilmore
发明人： Jingwu Duan , Bin Jiang , James Sheppeck , John L. Gilmore
IPC分类号： A61K31/498 , C07D417/14
CPC分类号： C07D403/12 , C07D241/36 , C07D417/12 , C07D417/14
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 prodrug thereof, or a pharmaceutically acceptable salt thereof, where Z is CONR1R2 or CH2NR1R2 and where at least two of X1-X4 and/or X5-X8 is N or NR18, and R, Ra, Rb, Rc, Rd, R1, R2 and R18 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）其立体异构体，或其溶剂合物，或其前药，或其药学上可接受的盐，其中Z为CONR1R2或CH2NR1R2，并且其中X1-X4和/或X5-X8中的至少两个为N或NR18 ，R，R a，R b，R c，R d，R 1，R 2和R 18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。

22. 发明申请

US20050182082A1 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：US20050182082A1
公开(公告)日：2005-08-18
申请号：US11034822
申请日：2005-01-13
申请人： Jingwu Duan , James Sheppeck , Bin Jiang , John Gilmore
发明人： Jingwu Duan , James Sheppeck , Bin Jiang , John Gilmore
IPC分类号： A61K31/439 , A61K31/473 , A61K31/4748 , C07D221/28 , C07D401/12 , C07D401/14 , C07D417/12 , C07D417/14 , C07D471/08
CPC分类号： C07D471/08 , C07D401/12 , C07D401/14 , C07D417/12 , C07D417/14
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 prodrug thereof, or a pharmaceutically acceptable salt thereof, where Z is CONR1R2 or CH2NR1R2 and where at least one of X1-X8 is N, and 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）其立体异构体，或其溶剂化物，或其前药，或其药学上可接受的盐，其中Z为CONR 1，R 2或CH 2 > 2 1 2 其中X 1 -X 8中的至少一个为 N和R，R a，O，R b，R c和R d都在本文中定义。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。

23. 发明授权

US08304539B2 Fused heteroaryl 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活性的融合杂芳基调节剂及其用途
公开(公告)号：US08304539B2
公开(公告)日：2012-11-06
申请号：US12866270
申请日：2009-02-05
申请人： Jingwu Duan , David S. Weinstein , Bin Jiang
发明人： Jingwu Duan , David S. Weinstein , Bin Jiang
IPC分类号： C07D491/147 , C07D413/00
CPC分类号： C07D491/147
摘要： Novel non-steroidal compounds are provided which are useful in treating diseases or disorders associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-κB activity, including metabolic and inflammatory and immune diseases or disorders, having the structure of formula (I): an enantiomer, diastereomer, or taυtomer thereof, or a prodrug ester thereof, or a pharmaceutically-acceptable salt thereof, in which: Z is heterocyclo or heteroaryl; •A is a S- to 8-membered carbocyclic ring or a S- to 8-membered heterocyclic ring; B1 and B2 rings are pyridyl rings, wherein the B1 and B2 rings are each fused to the A ring and the B1 ring is optionally substituted by one to three groups which are the same or different and are independently selected from R1, R2, and R4, and the B2 ring is optionally substituted by one to three groups which are the same or different and are independently selected from R5, R7, and R3 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, C1-3 alkylene, substituted C1-3 alkylene, C2-4 alkenylene, and substituted C2-4 alkenylene, 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.
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，AP-1和/或NF-κB活性相关的疾病或病症，包括具有结构的代谢和炎症和免疫疾病或病症式（I）的化合物：其对映异构体，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是杂环基或杂芳基; A是5至8元碳环或5至8元杂环; B1和B2环是吡啶环，其中B1和B2环各自与A环稠合，B1环任选被一至三个相同或不同并且独立地选自R 1，R 2和R 4的基团取代并且B2环任选被一至三个相同或不同并且独立地选自R5，R7和R8的基团取代，J1，J2和J3在每次出现时相同或不同，并且独立地为-A 1 QA 2 - ; 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A1和A2被选择为该环A为5-至8-元碳环或杂环; R1至R11如本文所定义。

24. 发明申请

US20090325961A1 INDANE MODULATORS OF GLUCOCORTICOID RECEPTOR, AP-1, AND/OR NF-kB ACTIVITY AND USE THEREOF 有权
标题翻译：葡萄糖激素受体，AP-1和/或NF-kB活性及其用途的印度调节剂
公开(公告)号：US20090325961A1
公开(公告)日：2009-12-31
申请号：US12542762
申请日：2009-08-18
申请人： Jingwu Duan , Bin Jiang
发明人： Jingwu Duan , Bin Jiang
IPC分类号： A61K31/5377 , A61K31/4439 , A61K31/41 , A61K31/425 , C07D417/12 , C07D417/10 , C07D285/12 , C07D277/00 , C07D417/14
CPC分类号： C07D285/135 , C07D233/76 , C07D249/12 , C07D277/46 , C07D285/08
摘要： Novel non-steroidal compounds are provided that 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 having the structure of formula (I): or enantiomers, diastereomers, or a pharmaceutically-acceptable salt, or hydrate, thereof, where X is A1QA2-; Q is a bond, —C(═O)—, —OC(O)—, —C(═O)NR5—, —SOp—, —SOpNR5—, —C(O)O—, —NR5C(O)—, —OC(O)NR5—, —NR5C(O)O—, —S(O)pNR5C(O)—, —C(O)NR5S(O)p— —NR5S(O)p—, or —NR5C(═O)NR6—. Y is selected from hydrogen, C1-6alkyl, OR16, substituted C1-6alkyl, cycloalkyl, aryl, heterocyclo and heteroaryl. A1 and A2 are independently selected from a bond, C1-3alkylene, or C1-3alkenylene, and R1-R11 are defined herein. Also provided are pharmaceutical compositions, combinations, and methods of treating obesity, diabetes and inflammatory- or immune-associated diseases comprising said compounds.
摘要翻译：提供了新型非甾体化合物，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，包括具有式（I）结构的肥胖症，糖尿病，炎症和免疫疾病：或对映异构体，非对映异构体或其药学上可接受的盐或水合物，其中X为AlQA2-; Q是键，-C（-O） - ， - OC（O） - ， - C（-O）NR5-，-SOp-，-SOpNR5-，-C（O） - （O）NR5 - ， - NR5C（O）O-，-S（O）pNR5C（O） - ， - C（O）NR5S（O） NR5C（-O）NR6-。 Y选自氢，C 1-6烷基，OR 16，取代的C 1-6烷基，环烷基，芳基，杂环和杂芳基。 A1和A2独立地选自键，C1-3亚烷基或C1-3亚烯基，R1-R11在本文中定义。还提供了治疗包含所述化合物的肥胖症，糖尿病和炎性或免疫相关疾病的药物组合物，组合和方法。

25. 发明申请

US20070185056A1 Indane modulators of 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活性的吲哚调节剂及其用途
公开(公告)号：US20070185056A1
公开(公告)日：2007-08-09
申请号：US11642508
申请日：2006-12-20
申请人： Jingwu Duan , Bin Jiang
发明人： Jingwu Duan , Bin Jiang
IPC分类号： A61K31/695 , C07D333/22 , C07F7/02 , A61K31/428 , A61K31/426 , A61K31/433 , A61K31/381
CPC分类号： C07D285/135 , C07D233/76 , C07D249/12 , C07D277/46 , C07D285/08
摘要： Novel non-steroidal compounds are provided that 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 having the structure of formula (I): or enantiomers, diastereomers, or a pharmaceutically-acceptable salt, or hydrate, thereof, where X is -A1QA2-; Q is a bond, —C(═O)—, —OC(O)—, —C(═O)NR5—, —SOp—, —SOpNR5—, —C(O)O—, —NR5C(O)—, —OC(O)NR5—, —NR5C(O)O—, —S(O)pNR5C(O)—, —C(O)NR5S(O)p— —NR5S(O)p—, or —NR5C(═O)NR6—. Y is selected from hydrogen, C1-4alkyl, OR16, substituted C1-6alkyl, cycloalkyl, aryl, heterocyclo and heteroaryl. A1 and A2 are independently selected from a bond, C1-3alkylene, or C1-3alkenylene, and R1-R11 are defined herein. Also provided are pharmaceutical compositions, combinations, and methods of treating obesity, diabetes and inflammatory- or immune-associated diseases comprising said compounds.
摘要翻译：提供了新型非甾体化合物，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，包括具有式（I）结构的肥胖症，糖尿病，炎症和免疫疾病：或对映异构体，非对映异构体或其药学上可接受的盐或水合物，其中X为-A 1 -QA 2 - ; Q是键，-C（-O） - ， - OC（O） - ， - C（-O）NR 5 - ， - SO 2 - C（O）O-，-NR 5 C（O） - ， - OC（O）NR 5 O - ， - NR 5 C（O）O-，-S（O）n NR 5 C （O） - ， - C（O）NR 5 S（O）p - （O） - 或-NR 5 C（-O）NR 6 - 。 Y选自氢，C 1-4烷基，OR 16，取代的C 1-6烷基，环烷基，芳基，杂环和杂芳基。 A 1和A 2个独立地选自键，C 1-3 - 亚烷基或C 1-3 - 亚烷基亚烯基，R 1 -R 11，如本文所定义。还提供了治疗包含所述化合物的肥胖症，糖尿病和炎性或免疫相关疾病的药物组合物，组合和方法。

26. 发明授权

US07132432B2 Hydantoin derivatives as inhibitors of tumor necrosis factor-alpha converting enzyme (TACE) 有权
标题翻译：海因衍生物作为肿瘤坏死因子-α转化酶（TACE）的抑制剂
公开(公告)号：US07132432B2
公开(公告)日：2006-11-07
申请号：US10858978
申请日：2004-06-02
申请人： Jingwu Duan , Chu-Biao Xue , James Sheppeck , Bin Jiang , Lihua Chen
发明人： Jingwu Duan , Chu-Biao Xue , James Sheppeck , Bin Jiang , Lihua Chen
IPC分类号： A61K31/147 , C07D453/02
CPC分类号： C07D413/04 , C07D413/14
摘要： The present invention provides compounds of Formula (I): or a stereoisomer or pharmaceutically acceptable salt form thereof, wherein the variables L, Z0, R1, R4, R5, and R11 are defined are as defined herein, which are useful as inhibitors of matrix metalloproteinases (MMP), TNF-α converting enzyme (TACE), aggrecanase, or a combination thereof.
摘要翻译：本发明提供式（I）化合物或其立体异构体或药学上可接受的盐形式，其中变量L，Z 0，R 1，R 2， 4，R 5和R 11定义如本文所定义，其可用作基质金属蛋白酶（MMP），TNF-α转化酶的抑制剂（TACE），软骨聚集蛋白聚糖酶或其组合。

27. 发明申请

US20050176716A1 Modulators of the glucocorticoid receptor, AP-1, and/or NF-kappaB 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：US20050176716A1
公开(公告)日：2005-08-11
申请号：US11034652
申请日：2005-01-13
申请人： Jingwu Duan , Bin Jiang , James Sheppeck , John Gilmore
发明人： Jingwu Duan , Bin Jiang , James Sheppeck , John Gilmore
IPC分类号： A01N43/58 , A01N43/60 , A61K31/495 , A61K31/498 , A61K31/50 , C07D241/36 , C07D403/12 , C07D417/02 , C07D417/12 , C07D417/14 , C07D43/02
CPC分类号： C07D403/12 , C07D241/36 , C07D417/12 , C07D417/14
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 prodrug thereof, or a pharmaceutically acceptable salt thereof, where Z is CONR1R2 or CH2NR1R2 and where at least two of X1-X4 and/or X5-X8 is N or NR18, and R, Ra, Rb, Rc, Rd, R1, R2 and R18 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）其立体异构体，或其溶剂化物，或其前药，或其药学上可接受的盐，其中Z为CONR 1，R 2或CH 2 > 2个NR 2 R 2，并且其中X 1 -X 4中的至少两个和 /或X 5 -X 8是N或NR 18，R，R a，R SUP R 1，R 2，R 2，R 2，R 2，R 2， > 18 。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。

28. 发明授权

US06495565B2 &bgr;-amino acid derivatives as inhibitors of matrix metalloproteases and TNF-&agr; 有权
标题翻译： β-氨基酸衍生物作为基质金属蛋白酶和TNF-α的抑制剂
公开(公告)号：US06495565B2
公开(公告)日：2002-12-17
申请号：US09811116
申请日：2001-03-16
申请人： Jingwu Duan , Bryan W. King , Carl Decicco , Thomas P. Maduskuie, Jr. , Matthew E. Voss
发明人： Jingwu Duan , Bryan W. King , Carl Decicco , Thomas P. Maduskuie, Jr. , Matthew E. Voss
IPC分类号： A61K314709
CPC分类号： C07D401/06 , C07D211/34 , C07D211/58 , C07D215/14 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/12 , C07D417/12
摘要： The present application describes novel &bgr;-amino acid derivatives of formula I: or pharmaceutically acceptable salt or prodrug forms thereof, wherein A, X, Z, Ua, Xa, Ya, Za, R1, R2, R3, R4, and R4a are defined in the present specification, which are useful as metalloprotease and/or as TNF-&agr; inhibitors.
摘要翻译：本申请描述了式I的新型β-氨基酸衍生物或其药学上可接受的盐或前药形式，其中A，X，Z，Ua，Xa，Ya，Za，R 1，R 2，R 3，R 4和R 4定义在本说明书中，其可用作金属蛋白酶和/或作为TNF-α抑制剂。

29. 发明授权

US08586751B2 Nicotinamide compounds useful as kinase modulators 有权
标题翻译：可用作激酶调节剂的烟酰胺化合物
公开(公告)号：US08586751B2
公开(公告)日：2013-11-19
申请号：US13377157
申请日：2010-06-10
申请人： George V. De Lucca , Qing Shi , Chunjian Liu , Jingwu Duan , Andrew J. Tebben
发明人： George V. De Lucca , Qing Shi , Chunjian Liu , Jingwu Duan , Andrew J. Tebben
IPC分类号： A61K31/4433 , C07D401/14
CPC分类号： C07D401/04 , C07D213/82 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/04 , C07D417/12 , C07D417/14 , C07D498/10
摘要： Disclosed are nicotinamide compounds of Formula (I): or stereoisomers or pharmaceutically acceptable salts thereof. Also disclosed are methods of using such compounds in the treatment of at least one Btk associated condition, such as, for example, inflammatory disease, and pharmaceutical compositions comprising such compounds.
摘要翻译：公开了式（I）的烟酰胺化合物或其立体异构体或其药学上可接受的盐。还公开了使用这些化合物治疗至少一种Btk相关病症例如炎性疾病的方法和包含这些化合物的药物组合物。

30. 发明申请

US20120295899A1 BENZYLPYRROLIDINONE DERIVATIVES AS MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY 有权
标题翻译：作为化合物受体活性调节剂的苄基吡咯烷酮衍生物
公开(公告)号：US20120295899A1
公开(公告)日：2012-11-22
申请号：US13576706
申请日：2011-02-08
申请人： Ian K. Mangion , Percy H. Carter , Jingwu Duan , Andrew J. Tebben
发明人： Ian K. Mangion , Percy H. Carter , Jingwu Duan , Andrew J. Tebben
IPC分类号： A61K31/5365 , C07D401/06 , A61P37/06 , A61K31/438 , A61P29/00 , A61P37/08 , C07D498/04 , A61K31/454
CPC分类号： C07D498/04 , C07D207/27
摘要： The present application describes modulators of MCP-1 or CCR-2 of formula or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein m, n, W, X, R1 and R6, are defined herein. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and transplant rejection using modulators of formula (I) are disclosed.
摘要翻译：本申请描述了式或其立体异构体或其前药或其药学上可接受的盐的MCP-1或CCR-2的调节剂，其中m，n，W，X，R 1和R 6在本文中定义。此外，公开了使用式（I）的调节剂治疗和预防炎性疾病如哮喘和过敏性疾病以及类风湿性关节炎和移植排斥反应的自身免疫病态的方法。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式