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    Selective inhibition of aggrecanase in osteoarthritis treatment
    7.
    发明授权
    Selective inhibition of aggrecanase in osteoarthritis treatment 失效

    公开(公告)号：US07030242B2

    公开(公告)日：2006-04-18

    申请号：US11120376

    申请日：2005-05-03

    Applicant: Mark C. Noe ,  Michael A. Letavic ,  Louis S. Chupak ,  Kim F. McClure

    Inventor： Mark C. Noe ,  Michael A. Letavic ,  Louis S. Chupak ,  Kim F. McClure

    IPC: C07D295/26 ,  A61K31/495

    CPC classification number: C07D241/04 ,  C07D211/96 ,  C07D241/08

    Abstract: This invention relates to a method of treatment for osteoarthritis involving inhibitors of aggrecanase that demonstrate IC50s of less than 20 nM and demonstrate differential potency against matrix metalloproteinases (MMPs) and a disintegrin and metalloproteinases (ADAMs or reprolysins). This invention also relates to compounds, methods of treatment and composition of Formula I: or a therapeutically acceptable salt thereof, wherein X is carbon or nitrogen; R1 and R2 are independently selected from the group consisting of hydrogen, hydroxy, and methyl, wherein at least one of R1 and R2 is methyl; R3 and R4 are independently selected from the group consisting of hydrogen, hydroxy, and methyl, or R3 and R4 may be taken together to form a carbonyl group; and R5 and R6 are independent substituents in the ortho, meta, or para positions and are independently selected from the group consisting of hydrogen, halogen, cyano, methyl, and ethyl; with the provisos: when X is carbon, then R7 and R8 are both hydrogen and at least one of R1, R2, R3, and R4 is hydroxy; when X is carbon and R5 is para-halo, then at least one of R6, R3, and R4 is not hydrogen; when X is nitrogen, then R8 is not present and R7 is hydrogen or a group of the formula: wherein, Y is —CH2—NH2 or —NH—CH3; and when X is nitrogen and R7 is H, then R3 and R4 are taken together to form a carbonyl group.

    Benzotriazoles anti-inflammatory compounds
    8.
    发明授权
    Benzotriazoles anti-inflammatory compounds 失效
    苯并三唑抗炎化合物

    公开(公告)号：US06664395B2

    公开(公告)日：2003-12-16

    申请号：US10115952

    申请日：2002-04-04

    Applicant: Michael A. Letavic ,  Mark A. Dombroski ,  Kim F. McClure ,  Ellen R. Laird

    Inventor： Michael A. Letavic ,  Mark A. Dombroski ,  Kim F. McClure ,  Ellen R. Laird

    IPC: C07D40304

    CPC classification number: C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D413/04

    Abstract: The present invention relates to novel benzotriazoles of the formula I wherein Het is an optionally substituted 5-membered heterocycle containing one to two heteroatoms selected from nitrogen, sulfur and oxygen wherein at least one of said heteroatoms atoms must be nitrogen; R2 is selected from the group consisting of hydrogen, (C1-C6)alkyl or other suitable substituents; R3 is selected from the group consisting of hydrogen, (C1-C6)alkyl or other suitable substituents; s is an integer from 0-5; to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use. The compounds of the present invention are potent inhibitors of MAP kinases, preferably p38 kinase. They are useful in the treatment of inflammation, osteoarthritis, rheumatoid arthritis, cancer, repurfusion or ischemia in stroke or heart attack, autoimmune diseases and other disorders.

    Abstract translation: 本发明涉及式I的新型苯并三唑，其中Het是含有一至二个选自氮，硫和氧的杂原子的任选取代的五元杂环，其中至少一个所述杂原子必须是氮;选择R 2 由（C 1 -C 6）烷基或其它合适的取代基组成的组; R 3选自氢，（C 1 -C 6）烷基或其它合适的取代基; s为0-5的整数 ;用于制备的中间体，含有它们的药物组合物及其药物用途。 本发明的化合物是MAP激酶的有效抑制剂，优选p38激酶。 它们可用于治疗炎症，骨关节炎，类风湿性关节炎，癌症，中风或心脏病发作中的再灌注或缺血，自身免疫疾病和其他疾病。

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