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21. 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。

22. 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。

23. 发明申请

US20120082702A1 NICOTINAMIDE COMPOUNDS USEFUL AS KINASE MODULATORS 有权
标题翻译： NICOTINAMIDE化合物作为激酶调节剂有用
公开(公告)号：US20120082702A1
公开(公告)日：2012-04-05
申请号：US13377157
申请日：2010-06-10
申请人： George V. DeLucca , Qing Shi , Chunjian Liu , Jingwu Duan , Andrew J. Tebben
发明人： George V. DeLucca , Qing Shi , Chunjian Liu , Jingwu Duan , Andrew J. Tebben
IPC分类号： A61K47/22 , A61K31/5377 , C07D401/14 , A61K31/497 , A61P37/08 , C07D401/04 , A61K31/4545 , A61K31/438 , A61P35/00 , A61P37/06 , C07D413/14 , C07D401/12
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。

24. 发明授权

US07595317B2 Barbituric acid derivatives as inhibitors of TNF-α converting enzyme (TACE) and/or matrix metalloproteinases 有权
标题翻译：巴比妥酸衍生物作为TNF-α转化酶（TACE）和/或基质金属蛋白酶的抑制剂
公开(公告)号：US07595317B2
公开(公告)日：2009-09-29
申请号：US11696847
申请日：2007-04-05
申请人： Jingwu Duan , Bin Jiang , Lihua Chen , Zhonghui Lu , Joseph Barbosa , William J. Pitts
发明人： Jingwu Duan , Bin Jiang , Lihua Chen , Zhonghui Lu , Joseph Barbosa , William J. Pitts
IPC分类号： A01N43/58 , A61K31/50 , C07D237/00 , C07D239/02
CPC分类号： C07D239/54 , C07D239/62 , C07D239/70 , C07D401/12 , C07D403/12 , C07D417/12 , C07D471/10 , C07D487/10 , C07D491/10
摘要： The present application describes novel barbituric acid derivatives of formula I: or pharmaceutically acceptable salt or prodrug forms thereof, wherein A, B, L, R1, R2, R3, R4, R5, n, W, U, X, Y, Z, Ua, Xa, Ya, and Za are defined in the present specification, which are useful as TNF-α converting enzyme (TACE) and matrix metalloproteinases (MMP) inhibitors.
摘要翻译：本申请描述了式I的新型巴比妥酸衍生物或其药学上可接受的盐或前药形式，其中A，B，L，R 1，R 2，R 3，R 4，R 5，n，W，U，X，Y， Ua，Xa，Ya和Za在本说明书中定义，其可用作TNF-α转化酶（TACE）和基质金属蛋白酶（MMP）抑制剂。

25. 发明申请

US20070167451A1 BARBITURIC ACID DERIVATIVES AS INHIBITORS OF TNF-alpha CONVERTING ENZYME (TACE) AND/OR MATRIX METALLOPROTEINASES 有权
标题翻译：作为TNF-α转化酶（TACE）和/或基质金属蛋白酶抑制剂的巴比妥酸衍生物
公开(公告)号：US20070167451A1
公开(公告)日：2007-07-19
申请号：US11696847
申请日：2007-04-05
申请人： Jingwu Duan , Bin Jiang , Lihua Chen , Zhonghui Lu , Joseph Barbosa , William Pitts
发明人： Jingwu Duan , Bin Jiang , Lihua Chen , Zhonghui Lu , Joseph Barbosa , William Pitts
IPC分类号： A61K31/53 , A61K31/517 , A61K31/515 , C07D413/02 , C07D403/02
CPC分类号： C07D239/54 , C07D239/62 , C07D239/70 , C07D401/12 , C07D403/12 , C07D417/12 , C07D471/10 , C07D487/10 , C07D491/10
摘要： The present application describes novel barbituric acid derivatives of formula I: or pharmaceutically acceptable salt or prodrug forms thereof, wherein A, B, L, R1, R2, R3, R4, R5, n, W, U, X, Y, Z, Ua, Xa, Ya, and Za are defined in the present specification, which are useful as TNF-α converting enzyme (TACE) and matrix metalloproteinases (MMP) inhibitors.
摘要翻译：本申请描述了式I的新型巴比妥酸衍生物或其药学上可接受的盐或前药形式，其中A，B，L，R 1，R 2， R 4，R 4，R 5，n，W，U，X，Y，Z，U a，在本说明书中定义，其可用作TNF-α转化酶（TACE）和/或基质金属蛋白酶（MMP）抑制剂。

26. 发明申请

US20070129400A1 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活性的调节剂及其用途
公开(公告)号：US20070129400A1
公开(公告)日：2007-06-07
申请号：US11451660
申请日：2006-06-13
申请人： Jingwu Duan , Zhonghui Lu , David Weinstein , Bin Jiang
发明人： Jingwu Duan , Zhonghui Lu , David Weinstein , Bin Jiang
IPC分类号： A61K31/4709 , A61K31/4439 , A61K31/428 , A61K31/427 , A61K31/416 , C07D417/02 , C07D403/02 , C07D405/02 , C07D409/02
CPC分类号： C07D401/04 , C07D231/56 , C07D401/06 , C07D403/04 , C07D405/04 , C07D405/06 , C07D409/06 , C07D417/06 , C07D417/12
摘要： 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 an enantiomer, a diastereomer, a pharmaceutically acceptable salt, or hydrate thereof, where J is selected from NR1 or C(R4)(R4a); K is selected from NR2 or C(R5)(R5a); L is selected from NR3 or C(R6)(R6a); and A, X, Y, R1, R2, R3, R4, R4a, R5, R5a, R6, R6a, R8, R10, R11, 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（包括肥胖症，糖尿病，炎症和免疫疾病）的调节相关的疾病，并且具有式（I）的结构，或其对映异构体，非对映异构体，药学上可接受的盐或水合物，其中J选自NR 1或C（R 4 S 4）（R 4a） / SUB>）; K选自NR 2或C（R 5）（R 5a）; L选自NR 3或C（R 6 S）（R 6a）; 和A，X，Y，R 1，R 2，R 3，R 4，R SUB R 4a，R 5，R 5a，R 6，R 6a，R SUB， R 8，R 11，R 11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。

27. 发明授权

US06936620B2 Barbituric acid derivatives as inhibitors of TNF-α converting enzyme (TACE) and/or matrix metalloproteinases 有权
标题翻译：巴比妥酸衍生物作为TNF-α转化酶（TACE）和/或基质金属蛋白酶的抑制剂
公开(公告)号：US06936620B2
公开(公告)日：2005-08-30
申请号：US10320919
申请日：2003-12-17
申请人： Jingwu Duan , Zhonghui Lu
发明人： Jingwu Duan , Zhonghui Lu
IPC分类号： A61P37/08 , C07D239/54 , C07D239/62 , C07D401/12 , C07D401/14 , C07D239/60 , A61K31/513 , A61K31/515 , A61P19/02
CPC分类号： C07D239/54 , C07D239/62 , C07D401/12 , C07D401/14
摘要： The present application describes novel barbituric acid derivatives of formula I: or pharmaceutically acceptable salt or prodrug forms thereof, wherein A, B, L, R1, W, Z, Ua, Xa, Ya, and Za are defined in the present specification, which are useful as TNF-α converting enzyme (TACE) and matrix metalloproteinases (MMP) inhibitors.
摘要翻译：本申请描述了式I的新型巴比妥酸衍生物或其药学上可接受的盐或前药形式，其中A，B，L，R 1，W，Z，U 在本说明书中定义，其可用作TNF-α转化酶（TACE），其中X，Y，Y，A，Z，）和基质金属蛋白酶（MMP）抑制剂。

28. 发明授权

US06720329B2 Spiro-cyclic &bgr;-amino acid derivatives as inhibitors of matrix metalloproteases and TNF-&agr; converting enzyme (TACE) 有权
标题翻译：作为基质金属蛋白酶和TNF-α转化酶（TACE）的抑制剂的螺环β-氨基酸衍生物
公开(公告)号：US06720329B2
公开(公告)日：2004-04-13
申请号：US10096804
申请日：2002-03-12
申请人： Gregory R. Ott , Xiao Tao Chen , Jingwu Duan , Matthew E. Voss
发明人： Gregory R. Ott , Xiao Tao Chen , Jingwu Duan , Matthew E. Voss
IPC分类号： A61K31443
CPC分类号： C07D317/72 , C07D307/94 , C07D319/08 , C07D339/06 , C07D405/12 , C07D407/12 , C07D409/12 , C07D417/12 , C07D417/14 , C07D491/04
摘要： The present application describes novel spiro-cyclic &bgr;-amino acid derivatives of formula I: or pharmaceutically acceptable salt forms thereof, wherein ring B is a 3-13 membered carbocycle or heterocycle, ring C forms a 3-11 membered spiro-carbocycle or spiro-heterocycleon ring B, and the other variables are defined in the present specification, which are useful as as matrix metalloproteinases (MMP), TNF-&agr; converting enzyme (TACE), and/or aggrecanase inhibitors.
摘要翻译：本申请描述了式I的新型螺环β-氨基酸衍生物或其药学上可接受的盐形式，其中环B是3-13元碳环或杂环，环C形成3-11元螺 - 碳环或螺 - 杂环B，其他变量在本说明书中定义，其可用作基质金属蛋白酶（MMP），TNF-α转化酶（TACE）和/或软骨聚集蛋白聚糖酶抑制剂。

29. 发明授权

US08921368B2 Pyrrolopyridazine JAK3 inhibitors and their use for the treatment of inflammatory and autoimmune diseases 有权
标题翻译：吡咯并哒嗪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：US08921368B2
公开(公告)日：2014-12-30
申请号：US14005570
申请日：2012-03-16
申请人： Stephen T. Wrobleski , Gregory D. Brown , Lidia M. Doweyko , Jingwu Duan , Junqing Guo , John Hynes , Bin Jiang , James Kempson , Shuqun Lin , Zhonghui Lu , Steven H. Spergel , John S. Tokarski , Hong Wu , Bingwei Vera Yang
发明人： Stephen T. Wrobleski , Gregory D. Brown , Lidia M. Doweyko , Jingwu Duan , Junqing Guo , John Hynes , Bin Jiang , James Kempson , Shuqun Lin , Zhonghui Lu , Steven H. Spergel , John S. Tokarski , Hong Wu , Bingwei Vera Yang
IPC分类号： C07D487/04 , C07D471/04 , A01N43/58 , A61K31/50
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。

30. 发明授权

US08324401B2 Indane 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活性的吲哚调节剂及其用途
公开(公告)号：US08324401B2
公开(公告)日：2012-12-04
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： A61K31/4164 , A61K31/426 , C07D233/54
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活性相关的疾病，所述疾病包括具有式（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X为AlQA2-; Q是键，-C（= O） - ， - OC（O） - ， - C（= O）NR5-，-SOp-，-SOpNR5-，-C（O） - （O）NR 5 - ， - NR 5 C（O）O-，-S（O）pNR 5 C（O） - ， - C（O）NR 5 S（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。

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