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5 条记录 (耗时 0.019 秒)

    Compounds
    2.
    发明授权
    Compounds 失效
    化合物

    公开(公告)号：US5212163A

    公开(公告)日：1993-05-18

    申请号：US758356

    申请日：1991-09-09

    申请人： Robert W. Ward ,  Roger E. Markwell ,  David J. Hunter

    发明人： Robert W. Ward ,  Roger E. Markwell ,  David J. Hunter

    IPC分类号： C07F9/38 ,  C07F9/40 ,  C07F9/553 ,  C07F9/572 ,  C07K5/06 ,  C07K5/08

    CPC分类号： C07F9/3808 ,  C07F9/4006 ,  C07F9/5532 ,  C07F9/5728 ,  C07K5/06191 ,  C07K5/0827

    摘要： Novel compounds of formula (I) and salts, solvates and hydrates thereof, processes for their preparation and their use in the treatment of conditions in which degradation of connective tissue and other proteinaceous components of the body occurs: ##STR1## in which, R is hydrogen, C.sub.1-6 alkyl or optionally substituted benzyl; R.sub.1 is hydrogen or C.sub.1-6 alkyl; R.sub.2 is C.sub.3-6 alkyl; R.sub.3 is hydrogen, alkyl, --CH.sub.2 --Z where Z is optionally substituted phenyl or heteroaryl, or R.sub.3 is a group ##STR2## where R.sub.7 is hydrogen, alkyl or --CH.sub.2 --Ph where Ph is optionally substituted phenyl and R.sub.8 is hydrogen or alkyl; and R.sub.4 is --CH.sub.2 --(CH.sub.2).sub.n OR.sub.5 or --CH.sub.2 --(CH.sub.2).sub.n OCOR.sub.6 or --CH(R.sub.9)COR.sub.10, where n is an integer from 1 to 6; R.sub.5, R.sub.6 and R.sub.9 are hydrogen or C.sub.1-6 alkyl; and R.sub.10 is hydroxy or --O--C.sub.1-6 alkyl or --NR.sub.5 R.sub.6 (where R.sub.5 and R.sub.6 may be linked to form a heterocyclic ring; or R.sub.3 and R.sub.4 are joined together as --(CH.sub.2).sub.m -- where m is an integer from 4 to 12.

    摘要翻译： 式（I）的新型化合物及其盐，溶剂化物和水合物，其制备方法及其用于治疗结缔组织和身体其它蛋白质成分降解的病症发生：其中（I） ，R为氢，C 1-6烷基或任选取代的苄基; R1是氢或C1-6烷基; R2是C3-6烷基; R3是氢，烷基，-CH2-Z，其中Z是任选取代的苯基或杂芳基，或R3是基团，其中R7是氢，烷​​基或-CH2-Ph，其中Ph是任选取代的苯基，R8是氢或烷基 ; 并且R 4是-CH 2 - （CH 2）nOR 5或-CH 2 - （CH 2）nOCOR 6或-CH（R 9）COR 10，其中n是1至6的整数; R5，R6和R9是氢或C1-6烷基; 并且R 10是羟基或-O-C 1-6烷基或-NR 5 R 6（其中R 5和R 6可以连接形成杂环;或者R 3和R 4连接在一起作为 - （CH 2）m - ，其中m是4的整数 到12岁

    Isoquinolines or benzisoquinoliner having antiinflammatory activity
    3.
    发明授权
    Isoquinolines or benzisoquinoliner having antiinflammatory activity 失效

    公开(公告)号：US4745115A

    公开(公告)日：1988-05-17

    申请号：US789105

    申请日：1985-10-18

    申请人： Roger E. Markwell ,  Stephen A. Smith ,  David J. Hunter

    发明人： Roger E. Markwell ,  Stephen A. Smith ,  David J. Hunter

    IPC分类号： A61K31/435 ,  A61K31/47 ,  A61K31/472 ,  A61K31/473 ,  A61P29/00 ,  A61P37/08 ,  C07D217/22 ,  C07D217/24 ,  C07D221/08 ,  C07D221/10 ,  C07D401/04

    CPC分类号： C07D401/04 ,  C07D217/22 ,  C07D217/24 ,  C07D221/08 ,  C07D221/10

    摘要： Compounds of the general formula I ##STR1## in which: R.sub.1 and R.sub.2 are independently hydrogen, C.sub.1-6 alkyl or together are a group X which is C.sub.3-6 polymethylene optionally in which one carbon atom is replaced by O, S or NR.sub.6 wherein R.sub.6 is hydrogen or C.sub.1-6 alkyl;R.sub.3 is a mono- or fused bi-cyclic heteroaromatic group having up to ten atoms in the aromatic ring(s), not more than four of which are selected from nitrogen, oxygen or sulphur, optionally C-substituted by one or more substituents selected from halogen, CF.sub.3, nitro, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, C.sub.1-6 alkylthio, C.sub.2-7 alkanoyl or cyano; or is phenyl or naphthyl, optionally substituted by one or more substituents selected from halogen, CF.sub.3, nitro, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, C.sub.1-6 alkylthio, C.sub.2-7 alkanoyl, carboxyl, C.sub.1-6 alkoxycarbonyl, cyano, CONR.sub.7 R.sub.8 wherein R.sub.7 and R.sub.8 are selected from hydrogen or C.sub.1-6 alkyl or together are a group X; NR.sub.9 R.sub.10 wherein R.sub.9 and R.sub.10 are selected from hydrogen, C.sub.1-6 alkyl, C.sub.2-7 alkanoyl or C.sub.1-6 alkylsulphonyl or together are a group X; SO.sub.2 NR.sub.11 R.sub.12 wherein R.sub.11 and R.sub.12 are selected from hydrogen or C.sub.1-6 alkyl or together are a group X; or S(O).sub.m R.sub.13 wherein m is 1 or 2 and R.sub.13 is C.sub.1-6 alkyl; Z is naphthyl or a mono- or fused bicyclic heteroaromatic ring having up to ten atoms in the aromatic ring(s), not more than four of which are selected from nitrogen, oxygen or sulphur or (when R.sub.3 is an optionally substituted naphthyl or heteroaromatic group as defined) Z is a phenyl ring; and Z is optionally C-substituted by one or two substituents R.sub.4 and R.sub.5 which are independently selected from C.sub.1-6 alkyl, cyano, amino, aminocarbonyl or aminocarbamoyl optionally substituted by one or two C.sub.1-6 alkyl groups or by a group X, halogen, CF.sub.3, nitro, C.sub.1-6 alkoxy, C.sub.1-6 alkylthio, C.sub.2-7 alkanoyloxy or hydroxy, or together on adjacent carbon atoms are methylenedioxy or C.sub.3-5 polymethylene,are disclosed as an active therapeutic substances for the treatment of inflammatory conditions.