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    Novel triazolo-pyridines as anti-inflammatory compounds
    5.
    发明申请
    Novel triazolo-pyridines as anti-inflammatory compounds 失效
    新型三唑并吡啶作为抗炎化合物

    公开(公告)号：US20050075365A1

    公开(公告)日：2005-04-07

    申请号：US10776953

    申请日：2004-02-11

    申请人： John Braganza ,  Michael Letavic ,  Kim McClure

    发明人： John Braganza ,  Michael Letavic ,  Kim McClure

    IPC分类号： A61K31/4745 ,  A61P29/00 ,  C07D471/02 ,  C07D471/04

    CPC分类号： C07D471/04

    摘要： The present invention relates to novel triazolo-pyridines of the formula wherein X is >CH2, >NH, sulfur, >S═O, >SO2 or oxygen; wherein said >CH2 and >NH may optionally be substituted with a suitable substituent; R1 is selected from the group consisting of hydrogen, (C1-C6)alkyl and other suitable substituents; R2 is selected from the group consisting of hydrogen, (C1-C6)alkyl and other suitable substituents; s is an integer from 0-4; R3 is R4, R5—(NR6)—, R5—S—, R5—(S═O)—, R5—(SO2)—, R5—SO2—NR6—, R5—(NR6)—SO2—, R5—O—, R5—(C═O)—, R5—(NR6)—(C═O)—, R5—(C═O)—NR6—, R5—O—(C═O)—, R5—(C═O)—O—, R5—CR7═CR8— or R5—C≡C_; such that the molecular weight of R3 is less than 500 AMU, preferably less than 250 AMU; R4, R5 and R6 are each selected from the group consisting of hydrogen, (C1-C6)alkyl and other suitable substituents; or a pharmaceutically acceptable salt thereof; 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. They are useful in the treatment of inflammation, osteoarthritis, rheumatoid arthritis, cancer, reperfusion or ischemia in stroke or heart attack, autoimmune diseases and other disorders.

    摘要翻译： 本发明涉及下式的新的三唑并 - 吡啶：其中X是> CH2，> NH，硫，> S = O，> SO2或氧; 其中所述> CH 2和> NH可以任选地被合适的取代基取代; R 1选自氢，（C 1 -C 6）烷基和其它合适的取代基; R 2选自氢，（C 1 -C 6）烷基和其它合适的取代基; s是0-4的整数; R 3是R 4，R 5 - （NR 6） - ，R 5 -S-，R 5 - （S = O） - ，R 5 - （SO 2 ） - ，R 5 -SO 2 -NR 6 - ，R 5 - （NR 6）-SO 2 - ，R 5 -O-，R 5 - （C = O） R 5 - （NR 6） - （C = O） - ，R 5 - （C = O）-NR 6 - ，R 5 -O-（C = O） R 5 - （C = O）-O-，R 5 -CR 7 = CR 8 - 或R 5 -C = C = 使得R 3的分子量小于500AMU，优选小于250MAU; R 4，R 5和R 6各自选自氢，（C 1 -C 6）烷基和其它合适的取代基; 或其药学上可接受的盐; 制备中间体，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。 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，自身免疫性疾病和其他疾病。

    C11 carbamates of macrolide antibacterials
    7.
    发明授权
    C11 carbamates of macrolide antibacterials 失效
    C11大环内酯类抗生素的氨基甲酸酯

    公开(公告)号：US6043227A

    公开(公告)日：2000-03-28

    申请号：US320352

    申请日：1999-05-26

    申请人： Hengmiao Cheng ,  Michael Letavic ,  Carl B. Ziegler, Jr. ,  Jason K. Dutra ,  Peter Bertinato ,  Brian S. Bronk

    发明人： Hengmiao Cheng ,  Michael Letavic ,  Carl B. Ziegler, Jr. ,  Jason K. Dutra ,  Peter Bertinato ,  Brian S. Bronk

    IPC分类号： C07H17/08 ,  A61K31/70

    CPC分类号： C07H17/08 ,  Y02P20/55

    摘要： This invention relates to compounds of the formula ##STR1## and to pharmaceutically acceptable salts thereof. The compounds of formula 1 are potent antibacterial agents that may be used to treat various bacterial infections and disorders related to such infections. The invention also relates to pharmaceutical compositions containing the compounds of formula 1 and to methods of treating bacterial infections by administering the compounds of formula 1. The invention also relates to methods of preparing the compounds of formula 1 and to intermediates useful in such preparation.

    摘要翻译： 本发明涉及式的化合物及其药学上可接受的盐。 式1的化合物是可用于治疗各种细菌感染和与这种感染有关的疾病的有效的抗菌剂。 本发明还涉及含有式1化合物的药物组合物和通过施用式1化合物治疗细菌感染的方法。本发明还涉及制备式1化合物的方法和用于此类制备的中间体。