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1. 发明授权

US06376665B1 Amide derivatives as inhibitors of matrix metalloproteinases, TNF-&agr;, and aggrecanase 有权
标题翻译：酰胺衍生物作为基质金属蛋白酶，TNF-α和聚集蛋白聚糖蛋白聚糖酶的抑制剂
公开(公告)号：US06376665B1
公开(公告)日：2002-04-23
申请号：US09540057
申请日：2000-03-31
申请人： Jingwu Duan , Carl P. Decicco , David J. Nelson , Chu-Biao Xue
发明人： Jingwu Duan , Carl P. Decicco , David J. Nelson , Chu-Biao Xue
IPC分类号： C07D41700
CPC分类号： C07D213/30 , C07C259/06 , C07C317/50 , C07C323/59 , C07C2601/02 , C07C2601/08 , C07D207/16 , C07D211/60 , C07D215/14 , C07D249/18 , C07D261/08 , C07D295/185 , C07D401/12 , C07D417/12
摘要： The present application describes novel amides and derivatives thereof of formula I: or pharmaceutically acceptable salt forms thereof, wherein these compounds are useful as inhibitors of matrix metalloproteinases, TNF-&agr;, and aggrecanase.
摘要翻译：本申请描述了式I的新型酰胺及其衍生物或其药学上可接受的盐形式，其中这些化合物可用作基质金属蛋白酶，TNF-α和聚蛋白聚糖蛋白聚糖酶的抑制剂。

2. 发明授权

US06689771B2 Amide derivatives as inhibitors of matrix metalloproteinases, TNF-&agr;, and aggrecanase 有权
标题翻译：酰胺衍生物作为基质金属蛋白酶，TNF-α和聚集蛋白聚糖蛋白聚糖酶的抑制剂
公开(公告)号：US06689771B2
公开(公告)日：2004-02-10
申请号：US10074357
申请日：2002-02-12
申请人： Jingwu Duan , Carl P. DeCicco , David J. Nelson , Chu-Biao Xue
发明人： Jingwu Duan , Carl P. DeCicco , David J. Nelson , Chu-Biao Xue
IPC分类号： A61K3133
CPC分类号： C07D213/30 , C07C259/06 , C07C317/50 , C07C323/59 , C07C2601/02 , C07C2601/08 , C07D207/16 , C07D211/60 , C07D215/14 , C07D249/18 , C07D261/08 , C07D295/185 , C07D401/12 , C07D417/12
摘要： The present application describes novel amides and derivatives thereof of formula I: or pharmaceutically acceptable salt forms thereof, wherein these compounds are useful as inhibitors of matrix metalloproteinases, TNF-&agr;, and aggrecanase.
摘要翻译：本申请描述了式I的新型酰胺及其衍生物或其药学上可接受的盐形式，其中这些化合物可用作基质金属蛋白酶，TNF-α和聚蛋白聚糖蛋白聚糖酶的抑制剂。

3. 发明授权

US06989139B2 Matrix metalloproteinase inhibitors 失效
标题翻译：基质金属蛋白酶抑制剂
公开(公告)号：US06989139B2
公开(公告)日：2006-01-24
申请号：US09783248
申请日：2001-02-14
申请人： Carl P. Decicco , David J. Nelson , John A. Barrett , Alan P. Carpenter Jr. , Jingwu Duan , Milind Rajopadhye
发明人： Carl P. Decicco , David J. Nelson , John A. Barrett , Alan P. Carpenter Jr. , Jingwu Duan , Milind Rajopadhye
IPC分类号： A61K31/395 , C07D267/00 , C07D401/12 , C07D413/12 , C07F9/6527
CPC分类号： A61K49/14 , A61K49/0002 , A61K49/085 , A61K49/10 , A61K51/088 , C07D207/26 , C07D213/82 , C07D267/00 , C07D401/12 , C07D401/14 , C07D413/12 , C07F9/6527
摘要： Thus the present invention describes novel compounds comprising 1-10 targeting moieties; a chelator (Ch); and 0-1 linking groups (Ln) between the targeting moiety and chelator; wherein the targeting moiety is a matrix metalloproteinase inhibitor; and wherein the chelator is capable of conjugating to a cytotoxic radioisotope. The present invention also provides novel compositions of the compounds of the invention, kits and their uses in treatment of diseases associated with MMPs.
摘要翻译：因此，本发明描述了包含1-10个靶向部分的新化合物; 螯合剂（Ch）; 和靶向部分和螯合剂之间的0-1个连接基团（Ln）; 其中靶向部分是基质金属蛋白酶抑制剂; 并且其中所述螯合剂能够缀合到细胞毒性放射性同位素。本发明还提供本发明化合物的新组合物，试剂盒及其在治疗与MMP相关的疾病中的用途。

4. 发明授权

US06984648B2 Cyclic β-amino acid derivatives as inhibitors of matrix metalloproteases and TNF-α 有权
标题翻译：环状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：US06984648B2
公开(公告)日：2006-01-10
申请号：US10779539
申请日：2004-02-13
申请人： Zhonghui Lu , Thomas P. Maduskuie, Jr. , Matthew E. Voss , Chu-Biao Xue , Jingwu Duan , Gregory Ott , Lihua Chen , Carl Decicco
发明人： Zhonghui Lu , Thomas P. Maduskuie, Jr. , Matthew E. Voss , Chu-Biao Xue , Jingwu Duan , Gregory Ott , Lihua Chen , Carl Decicco
IPC分类号： A61K31/47 , A61K31/445 , C07D215/02 , C07D413/00 , C07D211/68
CPC分类号： C07D417/14 , C07C259/08 , C07C2601/08 , C07D213/56 , C07D213/82 , C07D215/12 , C07D215/14 , C07D261/02 , C07D307/24 , C07D401/06 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/14 , C07D413/04 , C07D417/12
摘要： The present application describes novel cyclic β-amino acid derivatives of formula I: or pharmaceutically acceptable salt forms thereof, wherein ring B is a 5-7 membered cyclic system containing from 0-2 heteroatoms selected from O, N, NRa, and S(O)p, and 0-1 carbonyl groups and the other variables are defined in the present specification, which are useful as metalloprotease and/or as TNF-α inhibitors.
摘要翻译：本申请描述了式I的新型环状β-氨基酸衍生物或其药学上可接受的盐形式，其中环B是含有0-2个选自O，N，NR a的杂原子的5-7元环系和/或S（O）p，和0-1个羰基，其它变量在本说明书中定义，其可用作金属蛋白酶和/或作为TNF-α抑制剂。

5. 发明申请

US20050171096A1 Hydantoins and related heterocycles as inhibitors of matrix metalloproteinases and/or TNF-alpha converting enzyme (TACE) 有权
公开(公告)号：US20050171096A1
公开(公告)日：2005-08-04
申请号：US11093670
申请日：2005-03-30
申请人： James Sheppeck , Jingwu Duan , Chu-Biao Xue , Zelda Wasserman
发明人： James Sheppeck , Jingwu Duan , Chu-Biao Xue , Zelda Wasserman
IPC分类号： A61K31/4166 , A61K31/4184 , A61K31/4188 , A61K31/437 , A61K31/4439 , A61K31/454 , A61K31/4709 , A61K31/4725 , A61K31/4741 , A61K31/5415 , A61K45/06 , A61P1/00 , A61P1/02 , A61P1/04 , A61P1/14 , A61P1/16 , A61P3/00 , A61P7/00 , A61P7/02 , A61P7/04 , A61P9/04 , A61P9/08 , A61P9/10 , A61P11/00 , A61P11/06 , A61P17/00 , A61P17/02 , A61P17/06 , A61P19/00 , A61P19/02 , A61P19/06 , A61P19/08 , A61P21/00 , A61P21/04 , A61P25/00 , A61P25/04 , A61P27/02 , A61P27/06 , A61P29/00 , A61P31/00 , A61P31/04 , A61P31/18 , A61P35/00 , A61P37/02 , A61P37/08 , A61P43/00 , C07D233/76 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/14 , C07D409/14 , C07D417/12 , C07D417/14 , C07D471/10 , C07D487/10 , C07D491/10 , C07D491/107 , C07D519/00 , A61K31/541 , A61K31/5377 , A61K31/496 , A61K31/4178 , A61K31/4164 , C07D417/02 , C07D413/02 , C07D43/02
CPC分类号： C07D401/06 , A61K31/4709 , A61K45/06 , C07D233/76 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/14 , C07D409/14 , C07D417/12 , C07D417/14 , C07D471/10 , C07D487/10 , C07D491/10 , Y02A50/401 , A61K2300/00
摘要： The present application describes novel hydantoin derivatives of formula (I): or pharmaceutically acceptable salt or prodrug forms thereof, wherein A, B, R1, R2, R3, R4, R5, R6, R7, R11, and n are defined in the present specification, which are useful as inhibitors of matrix metalloproteinases (MMP), TNF-α converting enzyme (TACE), aggrecanase, or a combination thereof.

6. 发明授权

US06890915B2 Hydantoins and related heterocycles as inhibitors of matrix metalloproteinases and/or TNF-α converting enzyme (TACE) 有权
公开(公告)号：US06890915B2
公开(公告)日：2005-05-10
申请号：US10155575
申请日：2002-05-23
申请人： James E. Sheppeck , Jingwu Duan , Chu-Biao Xue , Zelda Wasserman
发明人： James E. Sheppeck , Jingwu Duan , Chu-Biao Xue , Zelda Wasserman
IPC分类号： A61K31/4166 , A61K31/4184 , A61K31/4188 , A61K31/437 , A61K31/4439 , A61K31/454 , A61K31/4709 , A61K31/4725 , A61K31/4741 , A61K31/5415 , A61K45/06 , A61P1/00 , A61P1/02 , A61P1/04 , A61P1/14 , A61P1/16 , A61P3/00 , A61P7/00 , A61P7/02 , A61P7/04 , A61P9/04 , A61P9/08 , A61P9/10 , A61P11/00 , A61P11/06 , A61P17/00 , A61P17/02 , A61P17/06 , A61P19/00 , A61P19/02 , A61P19/06 , A61P19/08 , A61P21/00 , A61P21/04 , A61P25/00 , A61P25/04 , A61P27/02 , A61P27/06 , A61P29/00 , A61P31/00 , A61P31/04 , A61P31/18 , A61P35/00 , A61P37/02 , A61P37/08 , A61P43/00 , C07D233/76 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/14 , C07D409/14 , C07D417/12 , C07D417/14 , C07D471/10 , C07D487/10 , C07D491/10 , C07D491/107 , C07D519/00 , A61K31/33 , C07D487/00 , C07D233/00 , C07D221/00 , C07D215/00
CPC分类号： C07D401/06 , A61K31/4709 , A61K45/06 , C07D233/76 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/14 , C07D409/14 , C07D417/12 , C07D417/14 , C07D471/10 , C07D487/10 , C07D491/10 , Y02A50/401 , A61K2300/00
摘要： The present application describes novel hydantoin derivatives of formula (I): or pharmaceutically acceptable salt or prodrug forms thereof, wherein A, B, R1, R2, R3, R4, R5, R6, R7, R11, and n are defined in the present specification, which are useful as inhibitors of matrix metalloproteinases (MMP), TNF-α converting enzyme (TACE), aggrecanase, or a combination thereof.

7. 发明授权

US06743807B2 Cyclic &bgr;-amino acid derivatives as inhibitors of matrix metalloproteases and TNF-&agr; 有权
标题翻译：环状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：US06743807B2
公开(公告)日：2004-06-01
申请号：US09811233
申请日：2001-03-16
申请人： Jingwu Duan , Gregory Ott , Lihua Chen , Carl Decicco , Zhonghui Lu , Thomas P. Maduskuie, Jr. , Chu-Biao Xue
发明人： Jingwu Duan , Gregory Ott , Lihua Chen , Carl Decicco , Zhonghui Lu , Thomas P. Maduskuie, Jr. , Chu-Biao Xue
IPC分类号： A61K3147
CPC分类号： C07D417/14 , C07C259/08 , C07C2601/08 , C07D213/56 , C07D213/82 , C07D215/12 , C07D215/14 , C07D261/02 , C07D307/24 , C07D401/06 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/14 , C07D413/04 , C07D417/12
摘要： The present application describes novel cyclic &bgr;-amino acid derivatives of formula I: or pharmaceutically acceptable salt forms thereof, wherein ring B is a 5-7 membered cyclic system containing from 0-2 heteroatoms selected from O, N, NRa, and S(O)p, and 0-1 carbonyl groups and the other variables 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的新的环状β-氨基酸衍生物或其药学上可接受的盐形式，其中环B是含有0-2个选自O，N，NR a，和S（O）p和0-1个羰基，其他变量在本说明书中定义，其可用作金属蛋白酶和/或作为TNF-α抑制剂。

8. 发明授权

US07482372B2 Hydantoins and related heterocycles as inhibitors of matrix metalloproteinases and/or TNF-α converting enzyme (TACE) 有权
标题翻译：乙内酰脲和相关杂环作为基质金属蛋白酶和/或TNF-α转换酶（TACE）的抑制剂
公开(公告)号：US07482372B2
公开(公告)日：2009-01-27
申请号：US11093670
申请日：2005-03-30
申请人： James E. Sheppeck , Jingwu Duan , Chu-Biao Xue , Zelda Wasserman
发明人： James E. Sheppeck , Jingwu Duan , Chu-Biao Xue , Zelda Wasserman
IPC分类号： C07D487/00 , C07D233/00 , C07D221/00 , C07D215/00
CPC分类号： C07D401/06 , A61K31/4709 , A61K45/06 , C07D233/76 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/14 , C07D409/14 , C07D417/12 , C07D417/14 , C07D471/10 , C07D487/10 , C07D491/10 , Y02A50/401 , A61K2300/00
摘要： The present application describes novel hydantoin derivatives of formula (I): or pharmaceutically acceptable salt or prodrug forms thereof, wherein A, B, R1, R2, R3, R4, R5, R6, R7, R11, and n are defined in the present specification, which are useful as inhibitors of matrix metalloproteinases (MMP), TNF-α converting enzyme (TACE), aggrecanase, or a combination thereof.
摘要翻译：本申请描述了式（I）的新型乙内酰脲衍生物或其药学上可接受的盐或前药形式，其中A，B，R 1，R 2，R 3，R 4，R 5，R 6，R 7，R 11和n在本文中定义规范，其可用作基质金属蛋白酶（MMP），TNF-α转化酶（TACE），聚蛋白聚糖蛋白聚糖酶或其组合的抑制剂。

9. 发明授权

US07015217B2 Cyclic sulfone 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转换酶（TACE）的抑制剂的环状砜衍生物
公开(公告)号：US07015217B2
公开(公告)日：2006-03-21
申请号：US10265876
申请日：2002-10-07
申请人： Jingwu Duan , Chu-Biao Xue
发明人： Jingwu Duan , Chu-Biao Xue
IPC分类号： C07D279/12 , C07D279/06 , A61K31/54 , A61P7/02 , A61P3/04
CPC分类号： C07D265/30 , C07D327/06 , C07D413/12
摘要： The present application describes novel cyclic sulfone derivatives of formula I: or pharmaceutically acceptable salt or prodrug forms thereof, which are useful as inhibitors of matrix metalloproteinases (MMP), TNF-α converting enzyme (TACE), aggrecanase, or a combination thereof. In formula I, A is selected from —COR5, —CO2H, —CO2R6, —C(O)NHOH, —C(O)NHOR5, —C(O)NHOR6, —NHRa, —N(OH)COR5, —N(OH)CHO, —SH, —CH2SH, —S(O)(═NH)Ra, —S(═NH)2Ra, —SC(O)Ra, —PO(OH)2, and —PO(OH)NHRa; B is a thiomorpholine ring; X is absent or is CR3R4; and Ua, Xa, Ya, Za, R1, R2, Rb, and q are defined in the present specification.
摘要翻译：本申请描述了式I的新型环状砜衍生物或其药学上可接受的盐或前药形式，其可用作基质金属蛋白酶（MMP），TNF-α转化酶（TACE），聚蛋白聚糖蛋白聚糖酶或其组合的抑制剂。在式I中，A选自-COR 5，-CO 2 H，-CO 2 R 6，，-C（O）NHOH，-C（O）NHOR 5，-C（O）NHOR 6，-NHR a， N（OH）COR 5，-N（OH）CHO，-SH，-CH 2 SH，-S（O）（ - NH）R a -S（-NH）2 R a，-SSC（O）R a，-PO（OH） SUB＆gt;和＆lt; 2＆gt;和-PO（OH）NHR a B是硫代吗啉环; X不存在或者是CR 3，R 4，和一个或多个，一个或多个，一个，一个，一个，一个，一个，一个，一个，一个，一个，一个，在本说明书中定义了R 2，R 2，B和Q。

10. 发明授权

US06906053B2 Hydantoins and related heterocycles as inhibitors of matrix metalloproteinases and/or TNF-α converting enzyme (TACE) 有权
标题翻译：乙内酰脲和相关杂环作为基质金属蛋白酶和/或TNF-α转换酶（TACE）的抑制剂
公开(公告)号：US06906053B2
公开(公告)日：2005-06-14
申请号：US10844219
申请日：2004-05-12
申请人： James E. Sheppeck , Jingwu Duan , Chu-Biao Xue , Zelda Wasserman
发明人： James E. Sheppeck , Jingwu Duan , Chu-Biao Xue , Zelda Wasserman
IPC分类号： A61K31/4166 , A61K31/4184 , A61K31/4188 , A61K31/437 , A61K31/4439 , A61K31/454 , A61K31/4709 , A61K31/4725 , A61K31/4741 , A61K31/5415 , A61K45/06 , A61P1/00 , A61P1/02 , A61P1/04 , A61P1/14 , A61P1/16 , A61P3/00 , A61P7/00 , A61P7/02 , A61P7/04 , A61P9/04 , A61P9/08 , A61P9/10 , A61P11/00 , A61P11/06 , A61P17/00 , A61P17/02 , A61P17/06 , A61P19/00 , A61P19/02 , A61P19/06 , A61P19/08 , A61P21/00 , A61P21/04 , A61P25/00 , A61P25/04 , A61P27/02 , A61P27/06 , A61P29/00 , A61P31/00 , A61P31/04 , A61P31/18 , A61P35/00 , A61P37/02 , A61P37/08 , A61P43/00 , C07D233/76 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/14 , C07D409/14 , C07D417/12 , C07D417/14 , C07D471/10 , C07D487/10 , C07D491/10 , C07D491/107 , C07D519/00 , A61K31/33 , C07D487/00 , C07D233/00 , C07D221/00 , C07D215/00
CPC分类号： C07D401/06 , A61K31/4709 , A61K45/06 , C07D233/76 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/14 , C07D409/14 , C07D417/12 , C07D417/14 , C07D471/10 , C07D487/10 , C07D491/10 , Y02A50/401 , A61K2300/00
摘要： The present application describes novel hydantoin derivatives of formula (I): or pharmaceutically acceptable salt or prodrug forms thereof, wherein A, B, R1, R2, R3, R4, R5, R6, R7, R11, and n are defined in the present specification, which are useful as inhibitors of matrix metalloproteinases (MMP), TNF-α converting enzyme (TACE), aggrecanase, or a combination thereof.
摘要翻译：本申请描述了式（I）的新型乙内酰脲衍生物或其药学上可接受的盐或前药形式，其中A，B，R 1，R 2，R SUP R 3，R 4，R 5，R 6，R 7，R SUP， > 11，并且n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），聚集蛋白聚糖蛋白聚糖酶或其组合的抑制剂。

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