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    BETA-SULFONAMIDO HYDROXAMIC ACIDS AS MATRIX METALLOPROTEINASE AND TACE INHIBITORS
    1.
    发明授权
    BETA-SULFONAMIDO HYDROXAMIC ACIDS AS MATRIX METALLOPROTEINASE AND TACE INHIBITORS 失效
    阿霉素羟基磷灰石基质金​​属蛋白酶

    公开(公告)号：EP0934259B1

    公开(公告)日：2002-09-18

    申请号：EP97912674.5

    申请日：1997-10-08

    申请人： American Cyanamid Company

    发明人： LEVIN, Jeremy, Ian ,  ZASK, Arie ,  GU, Yansong

    IPC分类号： C07C311/20 ,  A61K31/215

    CPC分类号： C07C311/29 ,  C07C2601/14

    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 formula (1) 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 , R , R and R ; a -C3-C7-cycloalkyl containing 0-2 double bonds and optionally substituted with R , R , R and R ; or -CHR =CHR -; and Z, R , R , R , R , R , R , R , R and R 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转化酶（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 治疗涉及这些酶的疾病如关节炎，肿瘤生长和转移，血管生成，组织溃疡，创伤愈合异常，牙周病，骨病，蛋白尿，动脉瘤主动脉疾病，外伤性关节损伤后退行性软骨损失，脱髓鞘疾病 的神经系统，移植物排斥，恶病质，厌食，炎症，发烧，胰岛素抵抗，败血性休克，充血性心力衰竭，中枢神经系统炎性疾病，炎性肠病，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，角质形成 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式（1）表示，其中异羟肟酸部分和亚磺酰氨基部分与A组的相邻碳键合，其中：A为5至7元单环 具有1至2个独立地选自N，O和S的杂原子的非芳族杂环，任选被R 1，R 2，R 3和R 4取代; 含有0-2个双键并任选被R 1，R 2，R 3和R 4取代的-C 3 -C 7 - 环烷基; 或-CHR 5 = CHR 6 - ; 和Z，R 1，R 2，R 3，R 4，R 5，R 6，R 7，R 8和R 9在 说明书及其药学上可接受的盐及其旋光异构体和非对映异构体。

    METHOD OF TREATING OR INHIBITING NEUTROPENIA
    5.
    发明公开
    METHOD OF TREATING OR INHIBITING NEUTROPENIA 失效
    方法用于治疗或中性粒细胞减少

    公开(公告)号：EP0957918A1

    公开(公告)日：1999-11-24

    申请号：EP97952527.0

    申请日：1997-12-17

    申请人： American Cyanamid Company

    发明人： EPSTEIN, Joseph, William ,  LEVIN, Jeremy, Ian ,  GIBBONS, James, Joseph ,  LUCAS, Judy

    IPC分类号： A61K31 ,  A61P7 ,  A61P43

    CPC分类号： A61K31/5377 ,  A61K31/519

    摘要： The invention is a method of treating or inhibiting neutropenia, or accelerating neutrophil recovery in a mammal in need thereof, which comprises administering to said mammal an effective amount of a compound, or a medicament containing said compound having formula (I) wherein R1 and R2 are each, independently selected from the group consisting of hydrogen, alkyl of 1-6 carbon atoms, optionally substituted benzoyl, (a), (b), (c), (d), (e), (f), and -(CH2)n-R; or R1 and R2 are methylene groups which are taken together to form a 4-7 membered saturated heterocyclic ring; R is hydroxy, 4-morpholinyl, 1H-imidazol-1-yl, -CH(alkoxy of 1-6 carbon atoms)2, α-hydroxybenzyl, or optionally substituted phenyl; R3 is hydrogen or alkyl; R4 is hydrogen, halogen, alkyl, alkoxy, or trifluoromethyl; R5 is hydrogen or alkyl; and n = 1-3, or a pharmaceutically acceptable salt thereof.

    BETA-SULFONAMIDO HYDROXAMIC ACIDS AS MATRIX METALLOPROTEINASE AND TACE INHIBITORS
    6.
    发明公开
    BETA-SULFONAMIDO HYDROXAMIC ACIDS AS MATRIX METALLOPROTEINASE AND TACE INHIBITORS 失效
    BETA-磺酰氨基异羟肟酸如基质金属蛋白酶和AS TACE抑制剂

    公开(公告)号：EP0934259A1

    公开(公告)日：1999-08-11

    申请号：EP97912674.0

    申请日：1997-10-08

    申请人： American Cyanamid Company

    发明人： LEVIN, Jeremy, Ian ,  ZASK, Arie ,  GU, Yansong

    IPC分类号： A61P1 ,  A61K31 ,  A61P9 ,  A61P13 ,  A61P15 ,  A61P17 ,  A61P19 ,  A61P25 ,  A61P27 ,  A61P35 ,  C07C257 ,  C07C311

    CPC分类号： C07C311/29 ,  C07C2601/14

    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-α converting enzyme (TACE, tumor necrosis factor-α 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 formula (1) 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?1, R2, R3 and R4¿; a -C¿3?-C7-cycloalkyl containing 0-2 double bonds and optionally substituted with R?1, R2, R3 and R4¿; or -CHR5=CHR6-; and Z, R?1, R2, R3, R4, R5, R6, R7, R8 and R9¿ are described in the specification, and the pharmaceutically acceptable salts thereof, and the optical isomers and diastereomers thereof.

    THE PREPARATION AND USE OF ORTHO-SULFONAMIDO HETEROARYL HYDROXAMIC ACIDS AS MATRIX METALLOPROTEINASE AND TACE INHIBITORS
    10.
    发明公开
    THE PREPARATION AND USE OF ORTHO-SULFONAMIDO HETEROARYL HYDROXAMIC ACIDS AS MATRIX METALLOPROTEINASE AND TACE INHIBITORS 失效
    生产和邻磺酰HETEROARYLHYDROXAMSÄURENALS基质金属蛋白酶与TACE的使用抑制剂

    公开(公告)号：EP0934300A1

    公开(公告)日：1999-08-11

    申请号：EP97910099.0

    申请日：1997-10-08

    申请人： American Cyanamid Company

    发明人： LEVIN, Jeremy, Ian ,  NELSON, Christy, Frances

    IPC分类号： A61K31 ,  A61P1 ,  A61P9 ,  A61P13 ,  A61P17 ,  A61P19 ,  A61P25 ,  A61P27 ,  A61P29 ,  A61P31 ,  A61P35 ,  A61P37 ,  A61P43 ,  C07D213 ,  C07D231 ,  C07D333 ,  C07D409

    CPC分类号： C07D213/78 ,  C07D231/42 ,  C07D333/38 ,  C07D333/40 ,  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-α converting enzyme (TACE, tumor necrosis factor-α 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 diseases, 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 formula (1) where the hydroxamic acid moiety and the sulfonamido 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?1, R2 and R3¿; and Z, R?1, R2, R3, R4, R5, R6, R7, R8 and R9¿ are described in the specification, and the pharmaceutically acceptable salts thereof and the optical isomers and diastereomers thereof.