Tricyclic compounds with pharmaceutical activity
    2.
    发明授权
    Tricyclic compounds with pharmaceutical activity 失效
    具有药物活性的三环化合物

    公开(公告)号:US5789417A

    公开(公告)日:1998-08-04

    申请号:US432161

    申请日:1995-06-28

    摘要: The invention relates to tricyclic compounds of formula (I) ##STR1## wherein R.sup.1 is hydrogen, amino, (1-4C)alkyl, (1-4C)alkoxy, hydroxy-(1-4C)alkyl or fluoro-(1-4C)alkyl; R.sup.2 is hydrogen, (1-4C)alkyl, (3-4C)alkenyl, (3-4C)alkynyl, hydroxy-(2-4C)alkyl, halogeno-(2-4C)alkyl or cyano-(1-4C)alkyl; Ar is optionally-substituted phenylene, thiophenediyl, thiazolediyl, pyridinediyl or pyrimidinediyl; and R.sup.3 includes a group of the formula --NHCH(CO.sub.2 H)--A.sup.1 --Y.sup.1 wherein A.sup.1 is (1-6C)alkylene and Y.sup.1 is carboxy, tetrazol-5-yl, N-�(1-4C)alkylsulphonyl!carbamoyl, N(phenylsulphonyl)carbamoyl, tetrazol-5-ylthio, tetrazol-5-ylsulphinyl or tetrazol-5-ylsulphonyl; or pharmaceutically-acceptable salts or esters thereof; to processes for their manufacture; to pharmaceutical compositions containing them; and to their use as anti-cancer agents.

    摘要翻译: PCT No.PCT / GB93 / 02281 Sec。 371日期:1995年6月28日 102(e)日期1995年6月28日PCT提交1993年11月4日PCT公布。 出版物WO94 / 11354 日期:1994年5月26日本发明涉及式(I)的三环化合物其中R 1为氢,氨基,(1-4C)烷基,(1-4C)烷氧基,羟基 - (1-4C)烷基 或氟 - (1-4C)烷基; R2是氢,(1-4C)烷基,(3-4C)烯基,(3-4C)炔基,羟基 - (2-4C)烷基,卤代 - (2-4C)烷基或氰基 - (1-4C) 烷基; Ar是任选取代的亚苯基,噻吩二基,噻唑二基,吡啶二基或嘧啶二基; 并且R 3包括式-NHCH(CO 2 H)-A1-Y1的基团,其中A 1为(1-6C)亚烷基且Y 1为羧基,四唑-5-基,N - [(1-4C)烷基磺酰基]氨基甲酰基,N (苯基磺酰基)氨基甲酰基,四唑-5-基硫代,四唑-5-基亚磺酰基或四唑-5-基磺酰基; 或其药学上可接受的盐或酯; 制造过程; 含有它们的药物组合物; 并将其用作抗癌剂。