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    ACETYLENIC (BETA)-SULFONAMIDO AND PHOSPHINIC ACID AMIDE HYDROXAMIC ACID TACE INHIBITORS
    13.
    发明公开
    ACETYLENIC (BETA)-SULFONAMIDO AND PHOSPHINIC ACID AMIDE HYDROXAMIC ACID TACE INHIBITORS 审中-公开
    磷酸二氢钠（BETA）-SULFONAMIDO UNDPHOSPHINSÄUREAMIDHYDROXAMSÄURETACE INHIBITOREN

    公开(公告)号：EP1147078A1

    公开(公告)日：2001-10-24

    申请号：EP00904570.9

    申请日：2000-01-27

    申请人： American Cyanamid Company

    发明人： LEVIN, Jeremy, Ian ,  CHEN, James, Ming ,  ZASK, Arie

    IPC分类号： C07C311/29 ,  C07F9/53 ,  A61K31/18 ,  A61K31/664 ,  A61P19/02

    CPC分类号： C07C309/87 ,  C07C309/42 ,  C07C311/29 ,  C07C2601/08 ,  C07C2601/14

    摘要： The invention discloses hydroxamide acids of formula (B) which are useful in treating disease conditions mediated by TNF-α, such as rheumatoid arthritis, osteoarthritis, sepsis, AIDS, ulcerative colitis, multiple sclerosis, Crohn's disease and degenerative cartilage loss. In the above formula, the dotted line represents an optional double bond, and R5, R6, R7, R8, R11, R12, X, Y and Z have the meanings given in the specification.

    摘要翻译： 本发明公开了式（B）的羟基酰胺酸，其可用于治疗由TNF-α介导的疾病状态，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。 在上式中，虚线表示任选的双键，R5，R6，R7，R8，R11，R12，X，Y和Z具有说明书中给出的含义。

    THE PREPARATION AND USE OF ORTHO-SULFONAMIDO BICYCLIC HETEROARYL HYDROXAMIC ACIDS AS MATRIX METALLOPROTEINASE AND TACE INHIBITORS
    15.
    发明公开
    THE PREPARATION AND USE OF ORTHO-SULFONAMIDO BICYCLIC HETEROARYL HYDROXAMIC ACIDS AS MATRIX METALLOPROTEINASE AND TACE INHIBITORS 失效
    生产和基质金属蛋白酶与TACE抑制剂ORTHO磺酰胺基二环杂芳基异羟肟酸衍生物的使用

    公开(公告)号：EP1021413A1

    公开(公告)日：2000-07-26

    申请号：EP98915523.9

    申请日：1998-04-14

    申请人： American Cyanamid Company

    发明人： LEVIN, Jeremy, Ian ,  ZASK, Arie ,  GU, Yansong ,  ALBRIGHT, Jay, Donald ,  DU, Xuemei

    IPC分类号： C07D215/54 ,  A61K31/63 ,  A61K31/47 ,  A61K31/44 ,  C07D401/12 ,  C07D471/04 ,  C07D513/04 ,  C07D498/04 ,  C07D495/04 ,  C07F9/547 ,  A61K31/66

    CPC分类号： C07D401/12 ,  C07D215/54 ,  C07D409/14 ,  C07D471/04 ,  C07D487/04 ,  C07D495/04 ,  C07D513/04

    摘要： This invention provides, low molecular weight, non-peptide inhibitors of matrix metalloproteinases and TNF-α converting enzyme (TACE, tumor necrosis factor-α converting enzyme) of formula (B) wherein (B) is (1), (2), or (3); P and Q are (4) or (5), provided that when P is (4), Q is (5), and vice versa; T, U, W, and X are each, independently, carbon or nitrogen, provided that when T or U is carbon, either may be optionally substituted with R1; Y is carbon, nitrogen, oxygen or sulfur, provided that at least one of T, U, W, X, and Y is not carbon, and further provided that no more than 2 of T, U, W, and X are nitrogen; (6) is a phenyl ring or is a heteroaryl ring of ring 5-6 atoms which may contain 0-2 heteroatoms selected from nitrogen, oxygen, and sulfur, in addition to any heteroatoms defined by W or X; wherein the phenyl or heteroaryl ring may be optionally mono-, di-, or tri- substituted with R1; Z is a phenyl, naphthyl, heteroaryl, or heteroaryl fused to phenyl, wherein the heteroaryl moiety contains of 5-6 ring atoms and 1-3 heteroatoms selected from nitrogen, oxygen, or sulfur; wherein the phenyl, naphthyl, heteroaryl, or phenyl fused heteroaryl moieties may be optionally mono-, di-, or tri-substituted with R1; R1 is hydrogen, halogen, alkyl of 1-8 carbon atoms, alkenyl of 2-6 carbon atoms, alkynyl of 2-6 carbon atoms, cyclocalkyl of 3-6 carbon atoms, -(CH¿2?)nZ, -OR?2¿, -CN, -COR2, perfluoroalkyl of 1-4 carbon atoms, -CONR2R3, -S(O)¿x?R?2-OPO(OR2)OR3¿, -PO(OR2)R3, -OC(O)NR2R3, -COOR?2, -CONR2R3, -SO¿3H, -NR?2R3, -NR2COR3, -NR2COOR3, -SO¿2NR?2R3, -NR2CONR2R3, -NR2C(=NR3)NR2R3, -SO¿2NHCOR4, -CONHSO¿2R?4, -tetrazol-5-yl, -SO¿2?NHCN, -SO2NHCONR?2R3¿, or Z; V is a saturated or partially unsaturated heterocycloalkyl ring of 5-7 ring atoms having 1-3 heteroatoms selected from N, O, or S, which may be optionally mono-, or di-substituted with R?2; R2 and R3¿ are each, independently, hydrogen, alkyl of 1-8 carbon atoms, alkenyl of 2-6 carbon atoms, alkynyl of 2-6 carbon atoms, cycloalkyl of 3-6 carbon atoms; perfluoroalkyl of 1-4 carbon atoms, Z or V; R4 is alkyl of 1-8 carbon atoms, alkenyl of 2-6 carbon atoms, alkynyl of 2-6 carbon atoms, cycloalkyl of 3-6 carbon atoms; perfluoroalkyl of 1-4 carbon atoms, Z or V; R5 is hydrogen, alkyl of 1-8 carbon atoms, alkenyl of 2-6 carbon atoms, alkynyl of 2-6 carbon atoms, Z, or V; n = 1-6; x = 0-2 or a pharmaceutically acceptable salt thereof.

    THE PREPARATION AND USE OF ORTHO-SULFONAMIDO HETEROARYL HYDROXAMIC ACIDS AS MATRIX METALLOPROTEINASE AND TACE INHIBITORS
    16.
    发明授权
    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：EP0934300B1

    公开(公告)日：2002-12-18

    申请号：EP97910099.7

    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： C07D333/38 ,  C07D231/42 ,  C07D213/78 ,  C07D409/12 ,  A61K31/38 ,  A61K31/44 ,  A61K31/415

    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.

    THE PREPARATION AND USE OF ORTHO-SULFONAMIDO ARYL HYDROXAMIC ACIDS AS MATRIX METALLOPROTEINASE AND TACE INHIBITORS
    17.
    发明授权
    THE PREPARATION AND USE OF ORTHO-SULFONAMIDO ARYL HYDROXAMIC ACIDS AS MATRIX METALLOPROTEINASE AND TACE INHIBITORS 失效
    生产和邻磺酰肟酸芳基质金属蛋白酶和TACE抑制剂的用途

    公开(公告)号：EP0938471B1

    公开(公告)日：2001-12-12

    申请号：EP97946246.2

    申请日：1997-10-08

    申请人： American Cyanamid Company

    发明人： LEVIN, Jeremy, Ian ,  DU, Mila, T. ,  VENKATESAN, Aranapakam, Mudumbai ,  NELSON, Frances, Christy ,  ZASK, Arie ,  GU, Yansong

    IPC分类号： C07C311/00

    CPC分类号： C07D213/42 ,  C07C311/21 ,  C07C311/29 ,  C07D213/68 ,  C07D267/14 ,  C07D273/06 ,  C07D333/20 ,  C07D401/12 ,  C07D405/12 ,  C07D409/04 ,  C07D409/12 ,  C07D413/14 ,  C07F7/1852

    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 (I) where the hydroxamic acid moiety and the sulfonamido moiety are bonded to adjacent carbons on group A where: A is phenyl or naphthyl, optionally substituted by R?1, R2, R3 and R4¿; Z is aryl, heteroaryl, or heteroaryl fused to a phenyl, where aryl is phenyl or naphthyl optionally substituted by R?1, R2, R3 and R4¿; heteroaryl is a 5-6 membered heteroaromatic ring having from 1 to 3 heteroatoms independently selected from N, O and S, and optionally substituted by R?1, R2, R3 and R4¿; and when heteroaryl is fused to phenyl, either or both of the rings can be optionally substituted by R?1, R2, R3 and R4; and R1, 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.