Pharmaceutical compounds
    1.
    发明授权
    Pharmaceutical compounds 失效
    药物化合物

    公开(公告)号:US5663375A

    公开(公告)日:1997-09-02

    申请号:US293786

    申请日:1994-08-22

    摘要: Pharmaceutical compounds of the formula ##STR1## in which n is 0, 1 or 2 and R.sup.1 is attached at any of the positions 7, 8, 9 or 10, and each R.sup.1 is halo, carboxy, trifluoromethyl, hydroxy, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 alkylthio, hydroxy-C.sub.1-4 alkyl, hydroxy-C.sub.1-4 alkoxy, nitrogen-containing heterocyclyl, nitro, trifluoromethoxy, --COOR.sup.5 where R.sup.5 is an ester group, --COR.sup.6, --CONR.sup.6 R.sup.7 or --NR.sup.6 R.sup.7 where R.sup.6 and R.sup.7 are each hydrogen or C.sub.1-4 alkyl;R.sup.2 is phenyl, naphthyl or heteroaryl selected from thienyl, pyridyl, benzothienyl, quinolinyl, benzofuranyl or benzimidazolyl, said phenyl, naphthyl and heteroaryl groups being optionally substituted, or R.sup.2 is furanyl optionally substituted with C.sub.1-4 alkyl;R.sup.3 is nitrile, carboxy, --COOR.sup.8 where R.sup.8 is an ester group, or --CONR.sup.9 R.sup.10 where R.sup.9 and R.sup.10 are each hydrogen or C.sub.1-4 alkyl; andR.sup.4 is --NR.sup.11 R.sup.12, --NR.sup.11 COR.sup.12, --N(COR.sup.11).sub.2 or --N.dbd.CHOCH.sub.2 R.sup.11 where R.sup.11 and R.sup.12 are each hydrogen or C.sub.1-4 alkyl optionally substituted with carboxy, --N.dbd.CH--NR.sup.13 R.sup.14 where R.sup.13 is hydrogen or C.sub.1-4 alkyl and R.sup.14 is C.sub.1-4 alkyl, optionally substituted phenyl or optionally substituted heteroaryl, ##STR2## where X is C.sub.2-4 alkylene, or --NHSO.sub.2 R.sup.15 where R.sup.15 is C.sub.1-4 alkyl, trifluoromethyl or optionally substituted phenyl; and salts thereof.

    摘要翻译: 其中n为0,1或2并且R 1连接在7,8,9或10位的任何位置的式“IMAGE”的药物化合物,并且每个R 1为卤素,羧基,三氟甲基,羟基,C 1-4烷基 C 1-4烷氧基,C 1-4烷硫基,羟基-C 1-4烷基,羟基-C 1-4烷氧基,含氮杂环基,硝基,三氟甲氧基,-COOR 5,其中R5是酯基,-COR6,-CONR6R7或 - NR 6 R 7,其中R 6和R 7各自为氢或C 1-4烷基; R 2是选自噻吩基,吡啶基,苯并噻吩基,喹啉基,苯并呋喃基或苯并咪唑基的苯基,萘基或杂芳基,所述苯基,萘基和杂芳基任选被取代,或R 2是任选被C 1-4烷基取代的呋喃基; R3是腈,羧基,-COOR8,其中R8是酯基,或-CONR9R10,其中R9和R10各自是氢或C1-4烷基; 并且R 4为-NR 11 R 12,-NR 11 COR 12,-N(COR 11)2或-N = CHOCH 2 R 11,其中R 11和R 12各自为氢或任选被羧基取代的C 1-4烷基,-N = CH-NR 13 R 14,其中R 13为氢或C1- 4烷基和R 14是C 1-4烷基,任选取代的苯基或任选取代的杂芳基,其中X是C 2-4亚烷基或-NHSO 2 R 15,其中R 15是C 1-4烷基,三氟甲基或任选取代的苯基; 及其盐。