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31. 发明授权

US08835429B2 Pyrimidine compounds, their use as mTOR kinase and Pl3 kinase inhibitors, and their syntheses 有权
标题翻译：嘧啶化合物，它们作为mTOR激酶和Pl3激酶抑制剂的用途及其合成
公开(公告)号：US08835429B2
公开(公告)日：2014-09-16
申请号：US13264776
申请日：2010-04-15
申请人： Kevin Joseph Curran , Joshua Aaron Kaplan , David James Richard , Jeroen Cunera Verheijen , Arie Zask
发明人： Kevin Joseph Curran , Joshua Aaron Kaplan , David James Richard , Jeroen Cunera Verheijen , Arie Zask
IPC分类号： C07D498/08 , A61K31/5386
CPC分类号： C07D498/08
摘要： The invention relates to pyrimidine compounds of the Formula I: or a pharmaceutically acceptable salt thereof, wherein the constituent variables are as defined herein, compositions comprising the compounds, and methods for making and using the compounds.
摘要翻译：本发明涉及式I的嘧啶化合物或其药学上可接受的盐，其中组成变量如本文所定义，包含该化合物的组合物，以及制备和使用该化合物的方法。

32. 发明授权

US06946473B2 Preparation and use of acetylenic ortho-sulfonamido and phosphinic acid amido bicyclic heteroaryl hydroxamic acids as TACE inhibitors 失效
标题翻译：炔基邻氨基磺酰氨基和次膦酸酰胺双环杂芳基异羟肟酸的制备和用途，作为TACE抑制剂
公开(公告)号：US06946473B2
公开(公告)日：2005-09-20
申请号：US10390515
申请日：2003-03-17
申请人： Jeremy I. Levin , James M. Chen , Xue-Mei Du , Jay D. Albright , Arie Zask
发明人： Jeremy I. Levin , James M. Chen , Xue-Mei Du , Jay D. Albright , Arie Zask
IPC分类号： C07D471/04 , C07D487/04 , C07D491/04 , C07D495/04 , C07D498/04 , C07D513/04 , A61K31/437 , A61P19/02
CPC分类号： C07D471/04 , C07D487/04 , C07D491/04 , C07D495/04 , C07D513/04
摘要： Compounds of the formula which are useful in disease conditions mediated by TNF-α, such as rheumatoid arthritis, osteoarthritis, sepsis, AIDS, ulcerative colitis, multiple sclerosis, Crohn's disease and degenerative cartilage loss.
摘要翻译：可用于TNF-α介导的疾病状态的化合物，例如类风湿性关节炎，骨关节炎，败血症，AIDS，溃疡性结肠炎，多发性硬化，克罗恩病和退行性软骨损失。

33. 发明授权

US06326516B1 Acetylenic &bgr;-sulfonamido and phosphinic acid amide hydroxamic acid TACE inhibitors 失效
标题翻译：乙酰β-亚磺酰氨基和次膦酸酰胺异羟肟酸TACE抑制剂
公开(公告)号：US06326516B1
公开(公告)日：2001-12-04
申请号：US09492980
申请日：2000-01-27
申请人： Jeremy I. Levin , James M. Chen , Arie Zask
发明人： Jeremy I. Levin , James M. Chen , Arie Zask
IPC分类号： C07C31129
CPC分类号： C07C311/29 , C07C2601/08 , C07C2601/14 , C07C2602/42
摘要： The invention discloses hydroxamide acids of the formula: which are useful in treating disease conditions mediated by TNF-&agr;, such as rheumatoid arthritis, osteoarthritis, sepsis, AIDS, ulcerative colitis, multiple sclerosis, Crohn's disease and degenerative cartilage loss.
摘要翻译：本发明公开了下式的羟基酰胺酸：其可用于治疗TNF-α介导的疾病状况，例如类风湿性关节炎，骨关节炎，败血症，AIDS，溃疡性结肠炎，多发性硬化，克罗恩病和退行性软骨损失。

34. 发明授权

US5068342A 5-[(1- and 2-naphthalenyl)thio and sulfonyl]-2,4-thiazolidinediones and derivatives thereof 失效
标题翻译： 5 - [（1-和2-萘基）硫基和磺酰基] -2,4-噻唑烷二酮类及其衍生物
公开(公告)号：US5068342A
公开(公告)日：1991-11-26
申请号：US596818
申请日：1990-10-12
申请人： Arie Zask , Ivo Jirkovsky
发明人： Arie Zask , Ivo Jirkovsky
IPC分类号： C07D277/36
CPC分类号： C07D277/36
摘要： Disclosed herein are 1- or 2-thio, thiomethylene, and sulfonylnaphthalene derivatives of formulas I and II ##STR1## or a pharmaceutically acceptable cationic salt thereof, wherein n is 0 or 1R.sub.5 is hydrogen, bromo, chloro, trifluoromethyl or difluoroethyl;R.sub.6 is hydrogen, hydroxy, methoxy or ethoxy; andR.sub.7 is hydrogen or R.sub.7 and R.sub.6 are both methyl or ethyl carbonate,provided that, when S(O).sub.2 is in the 2 position of the naphthalene ring, R.sub.5, R.sub.6 and R.sub.7 are each hydrogen. The disclosed compounds possess blood-glucose lowering actions and are useful in the treatment of diabetes mellitus.
摘要翻译：本文公开的是式I和II的1-或2-硫代，亚甲基亚甲基和磺酰基萘衍生物或其药学上可接受的阳离子盐，其中n是0或1个R 5是氢，溴，氯，三氟甲基或二氟乙基; R6是氢，羟基，甲氧基或乙氧基; 并且R 7是氢或R 7和R 6都是甲基或碳酸乙酯，条件是当S（O）2在萘环的2位时，R 5，R 6和R 7各自为氢。所公开的化合物具有降血糖作用，可用于治疗糖尿病。

35. 发明授权

US06548524B2 Preparation and use of ortho-sulfonamido bicyclic heteroaryl hydroxamic acids as matrix metalloproteinase and TACE inhibitors 失效
标题翻译：邻氨基磺酰氨基双环杂芳基异羟肟酸作为基质金属蛋白酶和TACE抑制剂的制备和应用
公开(公告)号：US06548524B2
公开(公告)日：2003-04-15
申请号：US09734140
申请日：2000-12-11
申请人： Jeremy I. Levin , Arie Zask , Yansong Gu , Jay D. Albright , Xuemei Du
发明人： Jeremy I. Levin , Arie Zask , Yansong Gu , Jay D. Albright , Xuemei Du
IPC分类号： A61K3159
CPC分类号： C07D215/54 , C07D401/12 , C07D409/14 , C07D471/04 , C07D487/04 , C07D495/04 , C07D513/04
摘要： This invention provides, non-peptide inhibitors of matrix metalloproteinases (e.g. gelatinases, stromelysins and collagenases) and TNF-&agr; converting enzyme (TACE. tumor necrosis factor-&agr; converting enzyme) which arc useful for the treatment of diseases in which these enzymes are implicated.
摘要翻译：本发明提供了可用于治疗这些酶涉及的疾病的基质金属蛋白酶（例如明胶酶，基质溶胶蛋白和胶原酶）和TNF-α转化酶（TACE。肿瘤坏死因子-α转化酶）的非肽抑制剂。

36. 发明授权

US06429214B1 Bicyclic antagonists selective for the &agr;v&bgr;3 integrin 失效
标题翻译：双环拮抗剂对alphavbeta3整联蛋白有选择性
公开(公告)号：US06429214B1
公开(公告)日：2002-08-06
申请号：US09620381
申请日：2000-07-20
申请人： Arie Zask , Diane Barbara Hauze , Kenneth Lewis Kees , Richard Dale Coghlan , John Yardley
发明人： Arie Zask , Diane Barbara Hauze , Kenneth Lewis Kees , Richard Dale Coghlan , John Yardley
IPC分类号： A61K3147
CPC分类号： C07D215/227 , A61K31/4709 , A61K31/495 , A61K31/496 , A61K31/537 , A61K31/5377 , A61K31/54 , A61K31/541 , C07D215/26 , C07D239/14
摘要： This invention provides novel bicyclic compounds of Formula (I): wherein u, v, m, Y, G, A—B, R1, R1a, R2, R4, R5, R5a, and R5b are defined in the specification which compounds exhibit activity as inhibitors of bone resorption and compounds of Formula (II) wherein u, v, m, Y, G, D, A—B, R1, R1a, R2, R3, R4, R5, R5a, and R5b are defined in the specification which compounds exhibit activity as inhibitors of bone resorption.
摘要翻译：本发明提供新的式（I）双环化合物：其中u，v，m，Y，G，AB，R 1，R 1a，R 2，R 4，R 5，R 5a和R 5b在本说明书中定义，（II）的化合物，其中u，v，m，Y，G，D，AB，R 1，R 1a，R 2，R 3，R 4，R 5，R 5a和R 5b在本说明书中定义，作为骨吸收抑制剂。

37. 发明授权

US06358980B1 Alkynyl containing hydroxamic acid compounds as matrix metalloproteinase/tace inhibitors 失效
标题翻译：含有异羟肟酸化合物的炔基作为基质金属蛋白酶/抑制剂
公开(公告)号：US06358980B1
公开(公告)日：2002-03-19
申请号：US09492686
申请日：2000-01-27
申请人： Jeremy I. Levin , Aranapakam M. Venkatesan , James M. Chen , Arie Zask , Vincent P. Sandanayaka , Mila T. Du , Jannie L. Baker
发明人： Jeremy I. Levin , Aranapakam M. Venkatesan , James M. Chen , Arie Zask , Vincent P. Sandanayaka , Mila T. Du , Jannie L. Baker
IPC分类号： A61K31445
CPC分类号： C07D309/08 , A61K31/351 , A61K31/435 , A61K31/445 , A61K31/496 , C07D211/60 , C07D211/62 , C07D211/66
摘要： Compounds of the formula: useful in the treatment of arthritis, tumor metastasis, tissue ulceration, abnormal wound healing, periodontal disease, bone disease, diabetes (insulin resistance) and HIV infection.
摘要翻译：下列化合物：可用于治疗关节炎，肿瘤转移，组织溃疡，创伤愈合异常，牙周病，骨病，糖尿病（胰岛素抵抗）和HIV感染。

38. 发明授权

US5977408A Preparation and use of .beta.-sulfonamido hydroxamic acids as matrix metalloproteinase and TACE inhibitors 失效
公开(公告)号：US5977408A
公开(公告)日：1999-11-02
申请号：US944189
申请日：1997-10-06
申请人： Jeremy Ian Levin , Arie Zask , Yansong Gu
发明人： Jeremy Ian Levin , Arie Zask , Yansong Gu
IPC分类号： C07C311/29
CPC分类号： C07C311/29 , C07C2101/14
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 where:A is a 5 to 7 membered, monocyclic, non-aromatic heterocyclic ring having from 1 to 2 heteroatoms independently selected from N, O, and S, optionally substituted by R.sup.1, R.sup.2, R.sup.3 and R.sup.4 ; a --C.sub.3 -C.sub.7 -cycloalkyl containing 0-2 double bonds and optionally substituted with R.sup.1, R.sup.2, R.sup.3 and R.sup.4 ; or --CHR.sup.5 .dbd.CHR.sup.6 --;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.

39. 发明申请

US20120134959A1 PYRIMIDINE COMPOUNDS, THEIR USE AS MTOR KINASE AND PI3 KINASE INHIBITORS, AND THEIR SYNTHESES 有权
标题翻译：哌嗪化合物，它们作为MTOR激酶和PI3激酶抑制剂使用，以及它们的合成
公开(公告)号：US20120134959A1
公开(公告)日：2012-05-31
申请号：US13264776
申请日：2010-04-15
申请人： Kevin Joseph Curran , Joshua Aaron Kaplan , David James Richard , Jeroen Cunera Verheijen , Arie Zask
发明人： Kevin Joseph Curran , Joshua Aaron Kaplan , David James Richard , Jeroen Cunera Verheijen , Arie Zask
IPC分类号： A61K31/5383 , A61K31/655 , A61K31/7068 , A61K31/675 , A61P35/00 , A61K31/7048 , A61K38/50 , A61K39/395 , A61K38/21 , C07D498/08 , A61K33/24
CPC分类号： C07D498/08
摘要： The invention relates to pyrimidine compounds of the Formula I: or a pharmaceutically acceptable salt thereof, wherein the constituent variables are as defined herein, compositions comprising the compounds, and methods for making and using the compounds.
摘要翻译：本发明涉及式I的嘧啶化合物或其药学上可接受的盐，其中组成变量如本文所定义，包含该化合物的组合物，以及制备和使用该化合物的方法。

40. 发明申请

US20050085504A1 Preparation and use of ortho-sulfonamido aryl hydroxamic acids as matrix metalloproteinase 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抑制剂的制备和应用
公开(公告)号：US20050085504A1
公开(公告)日：2005-04-21
申请号：US10980990
申请日：2004-11-04
申请人： Frances Nelson , Arie Zask , James Chen , Dominick Mobilio , Ramaswamy Nilakantan
发明人： Frances Nelson , Arie Zask , James Chen , Dominick Mobilio , Ramaswamy Nilakantan
IPC分类号： C07D307/78 , C07D307/87 , C07D333/52 , C07D217/12 , A61K31/405 , A61K31/47 , C07D213/56
CPC分类号： C07D307/87 , C07D307/78 , C07D333/52
摘要： Ortho-sulfonamido aryl hydroxamic acids are provided which are useful, inter alia, for the inhibition of matrix metalloproteinases and the treatment of conditions associated with overexpression of MMPs.
摘要翻译：提供了邻磺酰氨基芳基异羟肟酸，其尤其可用于抑制基质金属蛋白酶和治疗与MMP过量表达相关的病症。

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