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12 条记录 (耗时 0.025 秒)

    Pyrimidinone fused bicyclic metalloproteinase inhibitors
    1.
    发明授权
    Pyrimidinone fused bicyclic metalloproteinase inhibitors 失效
    嘧啶酮稠合双环金属蛋白酶抑制剂

    公开(公告)号：US06828326B2

    公开(公告)日：2004-12-07

    申请号：US10634225

    申请日：2003-08-05

    申请人： Joseph Armand Picard ,  Michael William Wilson

    发明人： Joseph Armand Picard ,  Michael William Wilson

    IPC分类号： C07D51304

    CPC分类号： C07D487/04 ,  C07D513/04

    摘要： The present invention relates to fused bicyclic metalloproteinase inhibitors of the formula wherein A, B, X, Y, and R1 are as defined in the specification, and to pharmaceutical compositions and methods of treating arthritis, inflammation, cancer and other disorders.

    摘要翻译： 本发明涉及式I，B，X，Y和R 1的稠合双环金属蛋白酶抑制剂如说明书中所定义，以及治疗关节炎，炎症，癌症和其它病症的药物组合物和方法。

    Alkynylated quinazoline compounds
    2.
    发明授权
    Alkynylated quinazoline compounds 失效
    炔烃基喹唑啉化合物

    公开(公告)号：US06962922B2

    公开(公告)日：2005-11-08

    申请号：US10269197

    申请日：2002-10-11

    申请人： Bernard Gaudilliere ,  Henri Jacobelli ,  Joseph Armand Picard ,  Michael William Wilson

    发明人： Bernard Gaudilliere ,  Henri Jacobelli ,  Joseph Armand Picard ,  Michael William Wilson

    IPC分类号： C07D239/96 ,  C07D403/06 ,  C07D471/04 ,  A61K31/517 ,  A61P19/02 ,  C07D401/10

    CPC分类号： C07D403/06 ,  C07D239/96 ,  C07D471/04

    摘要： A compound selected from those of formula (I): wherein W1 represents O, S, or —NR3 in which R3 represents hydrogen, alkyl, OH or CN; W2 represents a group selected from hydrogen, CF3, NH2, monoalkylamino, dialkylamino, alkyl, alkenyl, alkynyl, aryl, arylalkyl, cycloalkylalkyl, heterocycle, these groups being optionally substituted, or W1 and W2 form together a group of formula —N═X4—W3— as defined in the description, X1, X2 and X3 represent N or C optionally substituted, n is 0 to 8, Z represents —CR12R13, wherein R12 and R13 are as defined in the description, A represents a ring system, the groups R2 represent hydrogen or various chemical groups as defined in the description, q is 0 to 7; R1 represents hydrogen, alkyl, alkenyl, alkynyl, or a ring system, and optionally, its optical isomers, N-oxide, and addition salts thereof with a pharmaceutically-acceptable acid or base, and medicinal products containing the same are useful as specific inhibitors of type-13 matrix metalloprotease.

    摘要翻译： 选自式（I）的化合物的化合物：其中W 1代表O，S或-NR 3，其中R 3表示氢 ，烷基，OH或CN; W 2表示选自氢，CF 3，NH 2，单烷基氨基，二烷基氨基，烷基，烯基，炔基，芳基，芳基烷基， 环烷基烷基，杂环，这些基团任选被取代，或者W 1和W 2 2一起形成式-NX 4 -W 3 < - >如描述中所定义，X 1，X 2和X 3表示N或C任选取代的n 是0至8，Z表示-CR 12 R 13，其中R 12和R 13定义同上 在描述中，A表示环系，基团R 2表示氢或如说明书中定义的各种化学基团，q为0至7; R 1表示氢，烷基，烯基，炔基或环系，并且任选地，其光学异构体，N-氧化物及其与药学上可接受的酸或碱的加成盐和药物产品 含有它们的特异性抑制剂可用作13型基质金属蛋白酶的特异性抑制剂。

    Benzo thiadiazine matrix metalloproteinase inhibitors
    3.
    发明授权
    Benzo thiadiazine matrix metalloproteinase inhibitors 失效
    苯并噻二嗪基质金属蛋白酶抑制剂

    公开(公告)号：US06656932B2

    公开(公告)日：2003-12-02

    申请号：US10074646

    申请日：2002-02-13

    申请人： Joseph Armand Picard ,  Michael William Wilson

    发明人： Joseph Armand Picard ,  Michael William Wilson

    IPC分类号： C07D28522

    CPC分类号： C07D285/22 ,  C07D285/24 ,  C07D417/12

    摘要： Selective MMP-13 inhibitors are benzo thiadiazines of the Formula or a pharmaceutically acceptable salt thereof, wherein R2 is hydrogen or alkyl; R1 and R3 include hydrogen, alkyl, and aryl, with the proviso that R3 is not (CH2)m biphenyl or (CH2)m substituted biphenyl; X is O or NH, n is 0, 1, or 2. The compounds of Formula I, or a pharmaceutically acceptable salt thereof, is useful for treating diseases mediated by an MMP-13 enzyme, including diseases selected from osteoarthritis, rheumatoid arthritis, cancer, inflammation, and heart failure.

    摘要翻译： 选择性MMP-13抑制剂是其配制剂的药学上可接受的盐的苯并噻二嗪，其中R 2是氢或烷基; R 1和R 3包括氢，烷基和芳基，条件是R 3不是（CH 2）m联苯基或（CH 2）m取代的联苯基; X是O或NH，n是0,1或2.式I化合物或其药学上可接受的盐可用于治疗由MMP-13酶介导的疾病，包括选自骨关节炎，类风湿性关节炎， 癌症，炎症和心力衰竭。

    Thiazolidinone compounds useful as chemokine inhibitors
    8.
    发明授权
    Thiazolidinone compounds useful as chemokine inhibitors 有权
    可用作趋化因子抑制剂的噻唑烷酮化合物

    公开(公告)号：US06506751B1

    公开(公告)日：2003-01-14

    申请号：US09705219

    申请日：2000-11-02

    申请人： Stephanie Elizabeth Ault Justus ,  Helen Tsenwhei Lee ,  Jason Keith Pontrello ,  Bruce David Roth ,  Karen Elaine Sexton ,  Michael William Wilson

    发明人： Stephanie Elizabeth Ault Justus ,  Helen Tsenwhei Lee ,  Jason Keith Pontrello ,  Bruce David Roth ,  Karen Elaine Sexton ,  Michael William Wilson

    IPC分类号： C07D41306

    CPC分类号： C07D417/04 ,  C07D277/34 ,  C07D417/06

    摘要： Disclosed are compounds of the Formula I wherein: Z is C or nothing, provided that when Z is nothing, R3 and R4 are nothing; A is S, S═O or O═S═O; R1 and R2 are independently hydrogen, lower alkyl, halogen, hydroxy or lower alkoxy, (un)substituted aryl, (un)substituted arylalkyl, (un)substituted heteroaryl or(un)substituted heteroarylakyl; R3 and R4 independently represent hydrogen, lower alkyl, cycloalkyl, aminoalkyl, mono- or dialkylaminoalkyl, (un)substituted aryl or (un)substituted heteroaryl; R5 represents a (un)substituted carbocyclic group containing from 3-7 members, up to two of which members are optionally hetero atoms; or R5 is (CR6R7)—(CH2)n—XR8R9; X is S or N; R6, R7, R8, R9, and n are as defined in the specification. The compounds are useful in the treatment and prevention of the AIDS virus. Intermediates useful in the preparation of the final products, pharmaceutical compositions containing the final products are also taught.

    摘要翻译： 公开了式I的化合物，其中Z为C或无，条件是当Z不为任何时，R 3和R 4不为任何; A为S，S = O或O = S = O; R 1和R 2独立地为氢，低级烷基 ，卤素，羟基或低级烷氧基，（未）取代的芳基，（未）取代的芳基烷基，（未）取代的杂芳基或（未）取代的杂芳基; R3和R4独立地表示氢，低级烷基，环烷基，氨基烷基， ，（un）取代的芳基或（未）取代的杂芳基; R 5表示含有3-7个成员的（未）取代的碳环基，其中至多两个为任意的杂原子; 或R 5是（CR 6 R 7） - （CH 2）n -XR 8 R 9; X是S或N; R 6，R 7，R 8，R 9和n如说明书中所定义。该化合物可用于治疗和预防艾滋病毒。 还教导了用于制备最终产品的中间体，含有最终产品的药物组合物。