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1. 发明授权

US06441023B1 N-hydroxy-2-(alkyl, aryl, or heteroaryl sulfanyl, sulfinyl or sulfonyl)-3-substituted alkyl, aryl or heteroarylamides as matrix metalloproteinase inhibitors 失效
标题翻译： N-羟基-2-（烷基，芳基或杂芳基硫烷基，亚磺酰基或磺酰基）-3-取代的烷基，芳基或杂芳基酰胺作为基质金属蛋白酶抑制剂
公开(公告)号：US06441023B1
公开(公告)日：2002-08-27
申请号：US09898604
申请日：2001-07-03
申请人： Aranapakam Mudumbai Venkatesan , Jannie Lea Baker , Jeremy Ian Levin
发明人： Aranapakam Mudumbai Venkatesan , Jannie Lea Baker , Jeremy Ian Levin
IPC分类号： A61K31382
CPC分类号： C07D209/48 , A61K31/165 , A61K31/192 , A61K31/341 , A61K31/351 , A61K31/381 , A61K31/40 , A61K31/4418 , A61K31/445 , A61K31/451 , A61K31/495 , A61K31/5375 , C07C317/44 , C07C317/46 , C07C323/60 , C07C2601/08 , C07C2601/18 , C07D207/12 , C07D211/20 , C07D211/54 , C07D211/62 , C07D211/66 , C07D213/32 , C07D213/56 , C07D213/70 , C07D213/71 , C07D213/74 , C07D213/89 , C07D215/14 , C07D215/36 , C07D231/18 , C07D233/64 , C07D233/78 , C07D233/84 , C07D235/28 , C07D239/26 , C07D257/04 , C07D263/58 , C07D277/36 , C07D277/74 , C07D285/14 , C07D295/088 , C07D307/10 , C07D307/38 , C07D307/64 , C07D309/12 , C07D333/18 , C07D333/28 , C07D333/34 , C07D409/04
摘要： Matrix metalloproteinases (MMPs) are a group of enzymes that have been implicated in the pathological destruction of connective tissue and basement membranes. These zinc containing endopeptidases consist of several subsets of enzymes including collagenases, stromelysins and gelatinases. TNF-&agr; converting enzyme (TACE), a pro-inflmatory cytokine, catalyzes the formation of TNF-&agr; from membrane bound TNF-&agr; precursor protein. It is expected that small molecule inhibitors of MMPs and TACE therefore have the potential for treating a variety of disease states. The present invention provides low molecular weight, non-peptide inhibitors of matrix metalloproteinases (MMPs) and TNF-&agr; converting enzyme (TACE) for the treatment of arthritis, tumor metastasis, tissue ulceration, abnormal wound healing, periodontal disease, bone disease, diabetes (insulin resistance) and HIV infection having the formula wherein R2 and R3 form a heterocyclic ring and A is S, S(O), or S(O)2, and R1 and R4 are defined herein.
摘要翻译：基质金属蛋白酶（MMPs）是一组涉及结缔组织和基底膜的病理破坏的酶。这些含锌的内肽酶由几种酶组成，包括胶原酶，基质溶胶蛋白和明胶酶。 TNF-α转化酶（TACE）是促炎细胞因子，从膜结合的TNF-α前体蛋白催化TNF-α的形成。预期MMP和TACE的小分子抑制剂具有治疗各种疾病状态的潜力。本发明提供用于治疗关节炎，肿瘤转移，组织溃疡，异常伤口愈合，牙周病，骨病，糖尿病的基质金属蛋白酶（MMP）和TNF-α转换酶（TACE）的低分子量非肽抑制剂（胰岛素抵抗）和具有式R 2和R 3的HIV感染形成杂环，A是S，S（O）或S（O）2，并且R 1和R 4在本文中定义。

2. 发明授权

US06462073B2 N-hydroxy-2-(alkyl, aryl, or heteroaryl sulfanyl, sulfinyl or sulfonyl)-3-substituted alkyl, aryl or heteroarylamides as matrix metalloproteinase inhibitors 失效
标题翻译： N-羟基-2-（烷基，芳基或杂芳基硫烷基，亚磺酰基或磺酰基）-3-取代的烷基，芳基或杂芳基酰胺作为基质金属蛋白酶抑制剂
公开(公告)号：US06462073B2
公开(公告)日：2002-10-08
申请号：US09899641
申请日：2001-07-05
申请人： Aranapakam Mudumbai Venkatesan , George Theodore Grosu , Jamie Marie Davis , Jannie Lea Baker , Jeremy Ian Levin
发明人： Aranapakam Mudumbai Venkatesan , George Theodore Grosu , Jamie Marie Davis , Jannie Lea Baker , Jeremy Ian Levin
IPC分类号： A61K3140
CPC分类号： C07D209/48 , A61K31/165 , A61K31/192 , A61K31/341 , A61K31/351 , A61K31/381 , A61K31/40 , A61K31/4418 , A61K31/445 , A61K31/451 , A61K31/495 , A61K31/5375 , C07C317/44 , C07C317/46 , C07C323/60 , C07C2601/08 , C07C2601/18 , C07D207/12 , C07D211/20 , C07D211/54 , C07D211/62 , C07D211/66 , C07D213/32 , C07D213/56 , C07D213/70 , C07D213/71 , C07D213/74 , C07D213/89 , C07D215/14 , C07D215/36 , C07D231/18 , C07D233/64 , C07D233/78 , C07D233/84 , C07D235/28 , C07D239/26 , C07D257/04 , C07D263/58 , C07D277/36 , C07D277/74 , C07D285/14 , C07D295/088 , C07D307/10 , C07D307/38 , C07D307/64 , C07D309/12 , C07D333/18 , C07D333/28 , C07D333/34 , C07D409/04
摘要： Matrix metalloproteinases (MMPs) are a group of enzymes that have been implicated in the pathological destruction of connective tissue and basement membranes. These zinc containing endopeptidases consist of several subsets of enzymes including collagenases, stromelysins and gelatinases. TNF converting enzyme (TACE), a pro-inflammatory cytokine, catalyzes the formation of TNF-&agr; from membrane bound TNF-&agr; precursor protein. It is expected that small molecule inhibitors of MMPs and TACE therefore have the potential for treating a variety of disease states. The present invention provides low molecular weight, non-peptide inhibitors of matrix metalloproteinases (is) and TNF-&agr; converting enzyme (TACE) for the treatment of arthritis, tumor metastasis, tissue ulceration, abnormal wound healing, periodontal disease, bone disease, diabetes (insulin resistance) and HIV infection having the formula wherein R2 and R3 form a heterocyclic ring and A is S, S(O), or S(O)2, and R1 and R4 are defined herein.
摘要翻译：基质金属蛋白酶（MMPs）是一组涉及结缔组织和基底膜的病理破坏的酶。这些含锌的内肽酶由几种酶组成，包括胶原酶，基质溶胶蛋白和明胶酶。 TNF转导酶（TACE）是促炎细胞因子，从膜结合的TNF-α前体蛋白催化TNF-α的形成。预期MMP和TACE的小分子抑制剂具有治疗各种疾病状态的潜力。本发明提供用于治疗关节炎，肿瘤转移，组织溃疡，异常伤口愈合，牙周病，骨病，糖尿病的基质金属蛋白酶（is）和TNF-α转化酶（TACE）的低分子量非肽抑制剂（胰岛素抵抗）和具有式R 2和R 3的HIV感染形成杂环，A是S，S（O）或S（O）2，并且R 1和R 4在本文中定义。

3. 发明授权

US06197791B1 N-hdroxy-2-(alkyl, aryl, or heteroaryl, sulfanyl, sulfinyl or sulfonyl)-3-substituted alkyl, aryl or heteroarylamides as matrix metalloproteinase inhibitors 失效
标题翻译： N-羟基-2-（烷基，芳基或杂芳基，硫烷基，亚磺酰基或磺酰基）-3-取代的烷基，芳基或杂芳基酰胺作为基质金属蛋白酶抑制剂
公开(公告)号：US06197791B1
公开(公告)日：2001-03-06
申请号：US09140504
申请日：1998-08-26
申请人： Aranapakam Mudumbai Venkatesan , George Theodore Grosu , Jamie Marie Davis , Jannie Lea Baker , Jeremy Ian Levin
发明人： Aranapakam Mudumbai Venkatesan , George Theodore Grosu , Jamie Marie Davis , Jannie Lea Baker , Jeremy Ian Levin
IPC分类号： A61K31445
CPC分类号： C07D209/48 , A61K31/165 , A61K31/192 , A61K31/341 , A61K31/351 , A61K31/381 , A61K31/40 , A61K31/4418 , A61K31/445 , A61K31/451 , A61K31/495 , A61K31/5375 , C07C317/44 , C07C317/46 , C07C323/60 , C07C2601/08 , C07C2601/18 , C07D207/12 , C07D211/20 , C07D211/54 , C07D211/62 , C07D211/66 , C07D213/32 , C07D213/56 , C07D213/70 , C07D213/71 , C07D213/74 , C07D213/89 , C07D215/14 , C07D215/36 , C07D231/18 , C07D233/64 , C07D233/78 , C07D233/84 , C07D235/28 , C07D239/26 , C07D257/04 , C07D263/58 , C07D277/36 , C07D277/74 , C07D285/14 , C07D295/088 , C07D307/10 , C07D307/38 , C07D307/64 , C07D309/12 , C07D333/18 , C07D333/28 , C07D333/34 , C07D409/04
摘要： Matrix metalloproteinases (MMPs) are a group of enzymes that have been implicated in the pathological destruction of connective tissue and basement membranes. These zinc containing endopeptidases consist of several subsets of enzymes including collagenases, stromelysins and gelatinases. TNF-&agr; converting enzyme (TACE), a pro-inflammatory cytokine, catalyzes the formation of TNF-&agr; from membrane bound TNF-&agr; precursor protein. It is expected that small molecule inhibitors of MMPs and TACE therefore have the potential for treating a variety of disease states. The present invention provides low molecular weight, non-peptide inhibitors of matrix metalloproteinases (MMPs) and TNF-&agr; converting enzyme (TACE) for the treatment of arthritis, tumor metastasis, tissue ulceration, abnormal wound healing, periodontal disease, bone disease, diabetes (insulin resistance) and HIV infection having the formula wherein R2 and R3 form a heterocyclic ring and A is S, S(O), or S(O)2, and R1 and R4 are defined herein.
摘要翻译：基质金属蛋白酶（MMPs）是一组涉及结缔组织和基底膜的病理破坏的酶。这些含锌的内肽酶由几种酶组成，包括胶原酶，基质溶胶蛋白和明胶酶。 TNF-α转化酶（TACE）是促炎细胞因子，从膜结合的TNF-α前体蛋白催化TNF-α的形成。预期MMP和TACE的小分子抑制剂具有治疗各种疾病状态的潜力。本发明提供用于治疗关节炎，肿瘤转移，组织溃疡，异常伤口愈合，牙周病，骨病，糖尿病的基质金属蛋白酶（MMP）和TNF-α转换酶（TACE）的低分子量非肽抑制剂（胰岛素抵抗）和具有式R 2和R 3的HIV感染形成杂环，A是S，S（O）或S（O）2，并且R 1和R 4在本文中定义。

4. 发明授权

US5929097A Preparation and use of ortho-sulfonamido aryl hydroxamic acids as matrix metalloproteinase and tace inhibitors 失效
标题翻译：邻氨基磺酰氨基芳基异羟肟酸作为基质金属蛋白酶和止血抑制剂的制备和应用
公开(公告)号：US5929097A
公开(公告)日：1999-07-27
申请号：US944593
申请日：1997-10-06
申请人： Jeremy Ian Levin , Mila T. Du , Aranapakam Mudumbai Venkatesan , Frances Christy Nelson , Arie Zask , Yansong Gu
发明人： Jeremy Ian Levin , Mila T. Du , Aranapakam Mudumbai Venkatesan , Frances Christy Nelson , Arie Zask , Yansong Gu
IPC分类号： C07C311/21 , C07C311/29 , C07D211/20 , C07D213/30 , C07D213/38 , C07D213/55 , C07D213/56 , C07D213/68 , C07D267/14 , C07D267/22 , C07D307/16 , C07D333/20 , C07D333/24 , C07D405/12 , C07D409/04 , C07D409/12 , C07D413/04 , C07D413/14 , C07D521/00 , C07D213/02 , A61K31/18 , A61K31/44 , C07C311/08
CPC分类号： C07D213/30 , C07C311/21 , C07C311/29 , C07D211/20 , C07D213/38 , C07D213/55 , C07D213/56 , C07D213/68 , C07D231/12 , C07D233/56 , C07D249/08 , C07D267/14 , C07D267/22 , C07D307/16 , C07D333/20 , C07D333/24 , C07D405/12 , C07D409/04 , C07D409/12 , C07D413/04 , C07D413/14
摘要： The present invention relates to the discovery of novel, low molecular weight, non-peptide inhibitors of matrix metalloproteinases (e.g. gelatinases, stromelysins and collagenases) and TNF-.alpha. converting enzyme (TACE, tumor necrosis factor-.alpha. converting enzyme) which are useful for the treatment of diseases in which these enzymes are implicated such as arthritis, tumor growth and metastasis, angiogenesis, tissue ulceration, abnormal wound healing, periodontal disease, bone disease, proteinuria, aneurysmal aortic disease, degenerative cartilage loss following traumatic joint injury, demyelinating diseases of the nervous system, graft rejection, cachexia, anorexia, inflammation, fever, insulin resistance, septic shock, congestive heart failure, inflammatory disease of the central nervous system, inflammatory bowel disease, HIV infection, age related macular degeneration, diabetic retinopathy, proliferative vitreoretinopathy, retinopathy of prematurity, ocular inflammation, keratoconus, Sjogren's syndrome, myopia, ocular tumors, ocular angiogenesis/neovascularization.The TACE and MMP inhibiting ortho-sulfonamido aryl hydroxamic acids of the present invention are represented by the formula ##STR1## where the hydroxamic acid moiety and the sulfonamido moiety are bonded to adjacent carbons on group A.
摘要翻译：本发明涉及基因金属蛋白酶（例如明胶酶，基质溶质蛋白和胶原酶）和TNF-α转换酶（TACE，肿瘤坏死因子-α转化酶）的新型低分子量非肽抑制剂的发现，其可用于这些酶涉及的疾病如关节炎，肿瘤生长和转移，血管生成，组织溃疡，伤口愈合异常，牙周病，骨病，蛋白尿，动脉瘤主动脉疾病，创伤性关节损伤后退行性软骨损失，脱髓鞘疾病的神经系统，移植排斥反应，恶病质，厌食，炎症，发烧，胰岛素抵抗，脓毒性休克，充血性心力衰竭，中枢神经系统炎性疾病，炎症性肠病，HIV感染，年龄相关性黄斑变性，糖尿病性视网膜病变，增殖性玻璃体视网膜病变，早产儿视网膜病变，眼部炎症，角蛋白职业，干燥综合征，近视眼眼肿瘤，眼血管生成/新生血管形成。本发明的TACE和MMP抑制邻氨基磺酰氨基芳基异羟肟酸由下式表示，其中异羟肟酸部分和亚磺酰氨基部分与A组上的相邻碳键合。

5. 发明授权

US06124502A Mercaptoketones and mercaptoalcohols and a process for their preparation 失效
公开(公告)号：US06124502A
公开(公告)日：2000-09-26
申请号：US169661
申请日：1998-10-09
申请人： Jeremy Ian Levin
发明人： Jeremy Ian Levin
IPC分类号： C07C319/20 , C07C323/60 , C07D307/33 , C07C233/05 , C07C321/12
CPC分类号： C07D307/33 , C07C319/20 , C07C323/60
摘要： This invention relates to matrix metalloproteinase (MMP) inhibiting compounds of the formula: ##STR1## where R.sup.1 is C.sub.1 -C.sub.12 alkyl, straight or branched and optionally substituted by halogen, hydroxy, C.sub.1 -C.sub.6 alkoxy, amino, carboxyl, C.sub.1 -C.sub.6 alkoxycarbonyl, carboxamido, nitrile, mono- or di-(C.sub.1 -C.sub.6)alkylamino, thio, C.sub.1 -C.sub.6 alkylthio, aryl, --Oaryl or --OCH.sub.2 aryl where aryl is optionally substituted with C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, carboxy, halogen, cyano, nitro, carboxamido, or hydroxy; and C.sub.1 -C.sub.6 alkanesulfonyloxy. R.sup.2 is .alpha.-OH or .beta.-OH and R.sup.6 is H or R.sup.2 and R.sup.6 together are carbonyl; the chemical intermediates; and processes for the preparation of these compounds and the intermediates thereto.Matrix metalloproteinases (MMP) are a family of zinc-containing calcium dependent proteinases, including stromelysins, collagenases, and gelatinases. These MMP enzymes are capable of degrading the proteinaceous components of connective tissue and appear to be involved in tissue remodeling, i.e., wound healing and connective tissue turnover. Unexpectedly, the mercaptoalcohols with the S-configuration at the hydroxyl-bearing carbon have been found to be at least 4 times more potent than the analogous (R)-alcohols both in vitro and in vivo in inhibiting the MMP enzyme.

6. 发明授权

US06544984B1 2,3,4,5-tetrahydro-1H-(1,4)benzodiazepine-3-hydroxamic acids 失效
标题翻译： 2,3,4,5-四氢-1H-（1,4）苯并二氮杂-异羟肟酸
公开(公告)号：US06544984B1
公开(公告)日：2003-04-08
申请号：US09492622
申请日：2000-01-27
申请人： Jay Donald Albright , Efren Guillermo Delos Santos , Jeremy Ian Levin , James Ming Chen
发明人： Jay Donald Albright , Efren Guillermo Delos Santos , Jeremy Ian Levin , James Ming Chen
IPC分类号： A61K3155
CPC分类号： C07D401/06 , C07D243/14 , C07D409/06
摘要： Compounds having the following formula: are useful in treating disease conditions mediated by matrix metalloproteinases and TACE, such as tumor growth, osteoarthritis, rheumatoid arthritis and degenerative cartilage loss.
摘要翻译：具有下式的化合物可用于治疗由基质金属蛋白酶和TACE介导的疾病状况，例如肿瘤生长，骨关节炎，类风湿性关节炎和退行性软骨损失。

7. 发明申请

US20070219183A1 Dihydropyrazolo[1,5-A]pyrimidine and dihydroimidazo[1,5-A]pyrimidine derivatives and methods of use thereof 审中-公开
标题翻译：二氢吡唑并[1,5-A]嘧啶和二氢咪唑并[1,5-A]嘧啶衍生物及其使用方法
公开(公告)号：US20070219183A1
公开(公告)日：2007-09-20
申请号：US11724489
申请日：2007-03-15
申请人： Jeremy Ian Levin , Zhong Li , Dennis Powell
发明人： Jeremy Ian Levin , Zhong Li , Dennis Powell
IPC分类号： A61K31/554 , A61K31/553 , A61K31/551 , A61K31/541 , A61K31/5377 , A61K31/519 , C07D487/04
CPC分类号： C07D487/04
摘要： The present invention relates to dihydropyrazolo[1,5-a]pyrimidine and dihydroimidazo[1,5-a]pyrimidine derivatives, compositions comprising an effective amount of a dihydropyrazolo[1,5-a]pyrimidine or a dihydroimidazo[1,5-a]pyrimidine derivative and methods for treating or preventing cancer, comprising administering to a subject in need thereof an effective amount of a dihydropyrazolo[1,5-a]pyrimidine or a dihydroimidazo[1,5-a]pyrimidine derivative.
摘要翻译：本发明涉及二氢吡唑并[1,5-a]嘧啶和二氢咪唑并[1,5-a]嘧啶衍生物，包含有效量的二氢吡唑并[1,5-a]嘧啶或二氢咪唑并[ a]嘧啶衍生物和治疗或预防癌症的方法，包括向有需要的受试者施用有效量的二氢吡唑并[1,5-a]嘧啶或二氢咪唑并[1,5-a]嘧啶衍生物。

8. 发明授权

US06842704B2 Crystalline TNF-α-converting enzyme and uses thereof 失效
标题翻译：结晶TNF-α转化酶及其用途
公开(公告)号：US06842704B2
公开(公告)日：2005-01-11
申请号：US09244984
申请日：1999-02-04
申请人： Roy A. Black , Raymond James Paxton , Wolfram Bode , Klaus Maskos , Carlos Fernandez-Catalan , James Ming Chen , Jeremy Ian Levin
发明人： Roy A. Black , Raymond James Paxton , Wolfram Bode , Klaus Maskos , Carlos Fernandez-Catalan , James Ming Chen , Jeremy Ian Levin
IPC分类号： C12N9/64 , G06N7/00 , C12N9/10 , C12Q1/48
CPC分类号： C12N9/6489
摘要： A tumor necrosis factor-α converting enzyme (TACE) is produced, purified, and crystallized. The three-dimensional coordinates of the crystal are obtained by X-ray diffraction. The coordinates can be recorded on a computer readable medium, or are part of a video memory, where they can be used as part of a system for studying for studying TACE. The coordinates are also used in designing, screening, and developing compounds that associate with TACE.
摘要翻译：产生，纯化和结晶的肿瘤坏死因子-α转化酶（TACE）。通过X射线衍射获得晶体的三维坐标。坐标可以被记录在计算机可读介质上，或者是视频存储器的一部分，它们可以用作用于研究TACE的系统的一部分。坐标也用于设计，筛选和开发与TACE相关的化合物。

9. 发明授权

US06162814A Preparation and use of ortho-sulfonamido heteroaryl hydroxamic acids as matrix metaloproteinase and tace inhibitors 失效
标题翻译：邻氨基磺酰氨基杂芳基异羟肟酸作为基质金属蛋白酶和抑制剂的制备和应用
公开(公告)号：US06162814A
公开(公告)日：2000-12-19
申请号：US330877
申请日：1999-06-11
申请人： Jeremy Ian Levin , Frances Christy Nelson
发明人： Jeremy Ian Levin , Frances Christy Nelson
IPC分类号： C07D213/79 , C07D213/81 , C07D233/90 , C07D333/38 , C07D409/12 , A61K31/381
CPC分类号： C07D213/79 , C07D213/81 , C07D233/90 , C07D333/38 , C07D409/12
摘要： The present invention relates to the discovery of novel, low molecular weight, non-peptide inhibitors of matrix metalloproteinases (e.g. gelatinases, stromelysins and collagenases) and TNF-.alpha. converting enzyme (TACE, tumor necrosis factor-.alpha. converting enzyme) which are useful for the treatment of diseases in which these enzymes are implicated such as arthritis, tumor growth and metastasis, angiogenesis, tissue ulceration, abnormal wound healing, periodontal disease, bone disease, proteinuria, aneurysmal aortic disease, degenerative cartilage loss following traumatic joint injury, demyelinating diseases of the nervous system, graft rejection, cachexia, anorexia, inflammation, fever, insulin resistance, septic shock, congestive heart failure, inflammatory disease of the central nervous system, inflammatory bowel disease, HIV infection, age related macular degeneration, diabetic retinopathy, proliferative vitreoretinopathy, retinopathy of prematurity, ocular inflammation, keratoconus, Sjogren's syndrome, myopia, ocular tumors, ocular angiogenesis/neovascularization. The TACE and MMP inhibiting ortho-sulfonamide aryl hydroxamic acids of the present invention are represented by the formula ##STR1## where the hydroxamic acid moiety and the sulfanamido moiety are bonded to adjacent carbons on group A where A is defined as:a 5-6 membered heteroaryl having from 1 to 3 heteroatoms independently selected from N, O, and S and optionally substituted by R.sup.1, R.sup.2 and R.sup.3 ;and Z, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8 and R.sup.9 are described in the specification,and the pharmaceutically acceptable salts thereof and the optical isomers and diastereomers thereof.
摘要翻译：本发明涉及基因金属蛋白酶（例如明胶酶，基质溶质蛋白和胶原酶）和TNF-α转换酶（TACE，肿瘤坏死因子-α转化酶）的新型低分子量非肽抑制剂的发现，其可用于这些酶涉及的疾病如关节炎，肿瘤生长和转移，血管生成，组织溃疡，伤口愈合异常，牙周病，骨病，蛋白尿，动脉瘤主动脉疾病，创伤性关节损伤后退行性软骨损失，脱髓鞘疾病的神经系统，移植排斥反应，恶病质，厌食，炎症，发烧，胰岛素抵抗，脓毒性休克，充血性心力衰竭，中枢神经系统炎性疾病，炎症性肠病，HIV感染，年龄相关性黄斑变性，糖尿病性视网膜病变，增殖性玻璃体视网膜病变，早产儿视网膜病变，眼部炎症，角蛋白职业，干燥综合征，近视眼眼肿瘤，眼血管生成/新生血管形成。本发明的TACE和MMP抑制邻氨基磺酰基芳基异羟肟酸由下式表示，其中异羟肟酸部分和磺酰氨基部分键合到基团A上的相邻碳上，其中A定义为：5-6元杂芳基，独立地选自N，O和S且任选被R 1，R 2和R 3取代的1至3个杂原子; 并且Z，R 1，R 2，R 3，R 4，R 5，R 6，R 7，R 8和R 9在本说明书及其药学上可接受的盐及其旋光异构体和非对映体中描述。

10. 发明申请

US20100137298A1 Biaryl Sulfonamides and Methods for Using Same 审中-公开
标题翻译：二芳基磺酰胺及其使用方法
公开(公告)号：US20100137298A1
公开(公告)日：2010-06-03
申请号：US12138752
申请日：2008-06-13
申请人： Jeremy Ian Levin , Thomas Saltmarsh Rush, III , Frank Lovering , Yonghan Hu , Jianchang Li , Wei Li , Jun Jun Wu , Rajeev Hotchandani , Jason Shaoyun Xiang , Xuemei Du , Derek Cecil Cole , Steve Yikkai Tam
发明人： Jeremy Ian Levin , Thomas Saltmarsh Rush, III , Frank Lovering , Yonghan Hu , Jianchang Li , Wei Li , Jun Jun Wu , Rajeev Hotchandani , Jason Shaoyun Xiang , Xuemei Du , Derek Cecil Cole , Steve Yikkai Tam
IPC分类号： A61K31/5377 , G01N33/573 , C12N9/99 , A61K31/4439 , A61K31/425 , A61K31/428 , A61K31/381 , A61K31/343 , C07D413/12 , C07D405/10 , C07D277/02 , C07D275/02 , C07D209/42 , C07D333/52 , C07D307/78 , A61P35/00
CPC分类号： C07D235/24 , C07D209/42 , C07D231/14 , C07D235/12 , C07D261/18 , C07D263/58 , C07D277/56 , C07D277/64 , C07D277/68 , C07D285/01 , C07D307/68 , C07D307/80 , C07D307/81 , C07D307/82 , C07D307/85 , C07D307/92 , C07D333/34 , C07D333/70 , C07D401/12 , C07D405/04 , C07D405/12 , C07D407/04 , C07D409/12 , C07D413/04 , C07D417/04 , C07D491/06 , C07D495/04
摘要： The present invention relates to biaryl sulfonamides and their use as, for example, metalloproteinase inhibitors.
摘要翻译：本发明涉及联芳基磺酰胺及其作为例如金属蛋白酶抑制剂的用途。

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