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    Triazolo-pyridines anti-inflammatory compounds
    1.
    发明授权
    Triazolo-pyridines anti-inflammatory compounds 失效
    三唑并吡啶抗炎化合物

    公开(公告)号：US06696464B2

    公开(公告)日：2004-02-24

    申请号：US10094760

    申请日：2002-03-11

    申请人： Kim F. McClure ,  Michael A. Letavic ,  Mark A. Dombroski ,  Allen J. Duplantier ,  Ellen R. Laird

    发明人： Kim F. McClure ,  Michael A. Letavic ,  Mark A. Dombroski ,  Allen J. Duplantier ,  Ellen R. Laird

    IPC分类号： A61K3144

    CPC分类号： C07D471/04

    摘要： The present invention relates to novel triazolo-pyridines 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.

    摘要翻译： 本发明涉及式I的新型三唑并 - 吡啶，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; R 2， 选自氢，（C 1 -C 6）烷基或其它合适的取代基; R 3选自氢，（C 1 -C 6）烷基或其它合适的取代基; s是0的整数 -5;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。

    Benzotriazoles anti-inflammatory compounds
    2.
    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

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

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

    IPC分类号： C07D40304

    CPC分类号： C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D413/04

    摘要： 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.

    摘要翻译： 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。

    Three dimensional structure of a ZAP tyrosine protein kinase fragment and modeling methods
    4.
    发明授权
    Three dimensional structure of a ZAP tyrosine protein kinase fragment and modeling methods 失效
    ZAP酪氨酸蛋白激酶片段的三维结构和建模方法

    公开(公告)号：US06251620B1

    公开(公告)日：2001-06-26

    申请号：US08975040

    申请日：1997-11-18

    申请人： Marcos H. Hatada ,  Xiaode Lu ,  Ellen R. Laird ,  Jennifer L. Karas ,  Mark J. Zoller ,  Dennis A. Holt

    发明人： Marcos H. Hatada ,  Xiaode Lu ,  Ellen R. Laird ,  Jennifer L. Karas ,  Mark J. Zoller ,  Dennis A. Holt

    IPC分类号： C12Q148

    CPC分类号： C12N9/1205

    摘要： The invention relates to human ZAP-70, and in particular, to the region of ZAP-70 containing the tandem Src homology-2 (“SH2”) domains, to crystalline forms thereof, liganded or unliganded, which are particularly useful for the determination of the three-dimensional structure of the protein. The three dimensional structure of the tandem SH2 region of ZAP provides information useful for the design of pharmaceutical compositions which inhibit the biological function of ZAP and other members of the ZAP family of SH2 domain-containing proteins, particularly those biological functions mediated by molecular interactions involving one or both SH2 domains.

    摘要翻译： 本发明涉及人ZAP-70，特别涉及含有串联Src同源性-2（“SH2”）结构域的ZAP-70区域，其结构形式为配体或非配体，其特别可用于测定 的蛋白质的三维结构。 ZAP的串联SH2区域的三维结构提供了有用的药物组合物的设计信息，该药物组合物抑制ZAP和包含SH2结构域的蛋白质的ZAP家族的其他成员的生物学功能，特别是那些通过分子相互作用介导的那些生物学功能 一个或两个SH2结构域。