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11. 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。

12. 发明授权

US06610731B2 Lactam metalloprotease inhibitors 有权
公开(公告)号：US06610731B2
公开(公告)日：2003-08-26
申请号：US10096619
申请日：2002-03-12
申请人： Jingwu Duan , Carl P. Decicco , Zelda R. Wasserman , Thomas P. Maduskuie, Jr.
发明人： Jingwu Duan , Carl P. Decicco , Zelda R. Wasserman , Thomas P. Maduskuie, Jr.
IPC分类号： A61K3140
CPC分类号： C07D207/267 , C07D205/08 , C07D207/26 , C07D207/27 , C07D209/96 , C07D211/76 , C07D233/32 , C07D233/36 , C07D233/78 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/12 , C07D417/12 , C07D417/14 , C07D471/04 , C07D487/10
摘要： The present application describes novel lactams and derivatives thereof of formula I: or pharmaceutically acceptable salt forms thereof, wherein rings ring B is a 4-8 membered cyclic amide containing from 0-3 additional heteroatoms selected from N, O, and S, which are useful as metalloprotease inhibitors.

13. 发明授权

US06403632B1 Lactam metalloprotease inhibitors 有权
标题翻译：内酰胺金属蛋白酶抑制剂
公开(公告)号：US06403632B1
公开(公告)日：2002-06-11
申请号：US09516709
申请日：2000-03-01
申请人： Jingwu Duan , Carl P. Decicco , Zelda R. Wasserman , Thomas P. Maduskuie, Jr.
发明人： Jingwu Duan , Carl P. Decicco , Zelda R. Wasserman , Thomas P. Maduskuie, Jr.
IPC分类号： A61K3140
CPC分类号： C07D207/267 , C07D205/08 , C07D207/26 , C07D207/27 , C07D209/96 , C07D211/76 , C07D233/32 , C07D233/36 , C07D233/78 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/12 , C07D417/12 , C07D417/14 , C07D471/04 , C07D487/10
摘要： The present application describes novel lactams and derivatives thereof of formula I: or pharmaceutically acceptable salt forms thereof, wherein rings ring B is a 4-8 membered cyclic amide containing from 0-3 additional heteroatoms selected from N, O, and S, which are useful as metalloprotease inhibitors.
摘要翻译：本申请描述了式I的新型内酰胺及其衍生物：或其药学上可接受的盐形式，其中环环B是含有0-3个另外选自N，O和S的杂原子的4-8元环酰胺，其为可用作金属蛋白酶抑制剂。

14. 发明授权

US6057336A Lactam metalloprotease inhibitors 有权
标题翻译：内酰胺金属蛋白酶抑制剂
公开(公告)号：US6057336A
公开(公告)日：2000-05-02
申请号：US165747
申请日：1998-10-02
申请人： Jingwu Duan , Carl P. Decicco , Zelda R. Wasserman , Thomas P. Maduskuie, Jr.
发明人： Jingwu Duan , Carl P. Decicco , Zelda R. Wasserman , Thomas P. Maduskuie, Jr.
IPC分类号： A61K31/397 , A61K31/4015 , A61K31/4025 , A61K31/403 , A61K31/405 , A61K31/407 , A61K31/41 , A61K31/4155 , A61K31/4166 , A61K31/4178 , A61K31/4184 , A61K31/4192 , A61K31/422 , A61K31/4245 , A61K31/427 , A61K31/433 , A61K31/437 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/4439 , A61K31/4465 , A61K31/45 , A61K31/451 , A61K31/4545 , A61K31/4709 , A61K31/506 , A61K31/5377 , A61P1/02 , A61P7/00 , A61P9/00 , A61P17/06 , A61P19/02 , A61P25/00 , A61P27/06 , A61P31/18 , A61P35/00 , A61P37/00 , A61P43/00 , C07D205/08 , C07D207/26 , C07D207/273 , C07D209/96 , C07D211/76 , C07D233/32 , C07D233/78 , C07D401/06 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/12 , C07D403/14 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/06 , C07D409/12 , C07D413/04 , C07D413/10 , C07D413/12 , C07D413/14 , C07D417/10 , C07D417/12 , C07D417/14 , C07D471/04 , C07D487/10 , C07D491/10 , A01N43/42 , A01N57/24 , C07D215/06 , C07D215/20 , C07F9/32
CPC分类号： C07D207/26 , C07D205/08 , C07D209/96 , C07D211/76 , C07D233/32 , C07D233/78 , C07D401/06 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/12 , C07D417/12 , C07D417/14 , C07D471/04 , C07D487/10
摘要： The present application describes novel lactams and derivatives thereof of formula I: ##STR1## or pharmaceutically acceptable salt forms thereof, wherein rings ring B is a 4-8 membered cyclic amide containing from 0-3 additional heteroatoms selected from N, O, and S, which are useful as metalloprotease inhibitors.
摘要翻译：本申请描述了式I的新型内酰胺及其衍生物：或其药学上可接受的盐形式，其中环环B是含有0-3个另外选自N，O和S的杂原子的4-8元环酰胺，其为可用作金属蛋白酶抑制剂。

15. 发明授权

US06884806B2 Bicyclic lactam derivatives as inhibitors of matrix metalloproteinases and/or TNF-α converting enzyme (TACE) 有权
标题翻译：作为基质金属蛋白酶和/或TNF-α转化酶（TACE）抑制剂的双环内酰胺衍生物
公开(公告)号：US06884806B2
公开(公告)日：2005-04-26
申请号：US10271441
申请日：2002-10-16
申请人： Carl P. Decicco , Ying Song , Jingwu Duan , Matthew E. Voss
发明人： Carl P. Decicco , Ying Song , Jingwu Duan , Matthew E. Voss
IPC分类号： A61P9/04 , A61P17/06 , C07D455/02 , C07D471/04 , C07D487/04 , C07D498/04 , C07D519/00 , A61K31/47 , A61K31/4745 , A61P19/02
CPC分类号： C07D487/04 , C07D455/02 , C07D471/04
摘要： The present application describes novel bicyclic lactam derivatives of formula I: or pharmaceutically acceptable salt forms thereof, wherein A, B, C, D, R1, and R2 are defined in the present specification, which are useful as metalloprotease, TNF-α, and/or aggrecanase inhibitors.
摘要翻译：本申请描述了式I的新型双环内酰胺衍生物或其药学上可接受的盐形式，其中A，B，C，D，R 1和R 2定义在本说明书中，其可用作金属蛋白酶，TNF-α和/或软骨聚集蛋白聚糖酶抑制剂。

16. 发明授权

US06455522B1 Cyclic sulfonamide derivatives as metalloproteinase inhibitors 有权
标题翻译：环磺酰胺衍生物作为金属蛋白酶抑制剂
公开(公告)号：US06455522B1
公开(公告)日：2002-09-24
申请号：US09247675
申请日：1999-02-10
申请人： Jingwu Duan , Lihua Chen , Robert J. Cherney , Carl P. Decicco , Matthew E. Voss
发明人： Jingwu Duan , Lihua Chen , Robert J. Cherney , Carl P. Decicco , Matthew E. Voss
IPC分类号： A61K3155
CPC分类号： C07D417/06 , C07D279/02 , C07D285/36 , C07D417/12
摘要： The present application describes novel lactams and derivatives thereof of formula I: or pharmaceutically acceptable salt forms thereof, wherein rings ring B is a 4-8 membered cyclic sulfonamide containing from 0-3 additional heteroatoms selected from N, O, and S, which are useful as metalloprotease inhibitors.
摘要翻译：本申请描述了式I的新型内酰胺及其衍生物：或其药学上可接受的盐形式，其中环B是含有0-3个选自N，O和S的杂原子的4-8元环磺酰胺，它们是可用作金属蛋白酶抑制剂。

17. 发明授权

US06281352B1 Macrocyclic compounds as metalloprotease inhibitors 失效
标题翻译：大环化合物作为金属蛋白酶抑制剂
公开(公告)号：US06281352B1
公开(公告)日：2001-08-28
申请号：US08856223
申请日：1997-05-14
申请人： Chu-Bio Xue , Carl P. Decicco , Robert J. Cherney , Elizabeth Arner , William F. DeGrado , Jingwu Duan , Xiaohua He , Irina Cipora Jacobson , Ronald L. Magolda , David Nelson
发明人： Chu-Bio Xue , Carl P. Decicco , Robert J. Cherney , Elizabeth Arner , William F. DeGrado , Jingwu Duan , Xiaohua He , Irina Cipora Jacobson , Ronald L. Magolda , David Nelson
IPC分类号： A61K3133
CPC分类号： C07D231/12 , A61K38/00 , C07D233/56 , C07D245/02 , C07D249/08 , C07D255/02 , C07D267/00 , C07D273/02 , C07D291/02 , C07D401/12 , C07D403/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D419/12 , C07K5/0606 , C07K5/06078 , C07K5/06139 , C07K5/06191 , C12Q1/37
摘要： This invention relates to macrocyclic molecules which inhibit metalloproteinases, including aggrecanase, and the production of tumor necrosis factor (TNF). In particular, the compounds are inhibitors of metalloproteinases involved in tissue degradation and inhibitors of the release of tumor necrosis factor. The present invention also relates to pharmaceutical compositions comprising such compounds and to methods of using these compounds for the treatment of inflammatory diseases.
摘要翻译：本发明涉及抑制金属蛋白酶（包括聚蛋白聚糖蛋白酶）和肿瘤坏死因子（TNF）的产生的大环分子。特别地，化合物是参与组织降解的金属蛋白酶抑制剂和肿瘤坏死因子释放抑制剂。本发明还涉及包含这些化合物的药物组合物和使用这些化合物治疗炎性疾病的方法。

18. 发明申请

US20110002952A1 FUSED HETEROARYL MODULATORS OF GLUCOCORTICOID RECEPTOR, AP-1, AND/OR NF-kappaB ACTIVITY AND USE THEREOF 有权
标题翻译： GLUCOCORTICOID受体，AP-1和/或NF-κB活性的融合血管调节剂及其用途
公开(公告)号：US20110002952A1
公开(公告)日：2011-01-06
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： A61K31/5377 , C07D491/147 , A61K31/4375 , A61K38/26 , A61K38/28 , A61K39/00 , A61P37/00 , A61P29/00 , A61P3/00 , A61P37/06 , A61P19/02 , A61P25/00 , A61P11/06 , A61P1/00 , A61P17/06
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 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; 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 R3, R7, and R3 71, J2, and J3 are at each occurrence the same or different and are independently -AIQA2-; Q is a bond, O, S, S(0), 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, C24 alkenylene, and substituted C24 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环任选地被一至三个相同或不同并且独立地选自R3，R7和R371的基团取代，J2和J3在每次出现时相同或不同，并且独立地为-AIQA2- ; Q是键，O，S，S（0）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，C24亚烯基和取代的C24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。

19. 发明授权

US07294624B2 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：US07294624B2
公开(公告)日：2007-11-13
申请号：US10321144
申请日：2002-12-17
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 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。

20. 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。

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