Compounds useful as antiproliferative agents and GARFT inhibitors
    8.
    发明授权
    Compounds useful as antiproliferative agents and GARFT inhibitors 失效
    可用作抗增殖剂和GARFT抑制剂的化合物

    公开(公告)号:US5723607A

    公开(公告)日:1998-03-03

    申请号:US792572

    申请日:1997-01-30

    CPC分类号: C07D513/04

    摘要: The invention generally relates to compounds of the formula I, which are in equilibrium with their 4-hydroxy tautomers, and their pharmaceutically acceptable salts: ##STR1## where n is 0 to 2; A is S, CH.sub.2, O, NH or Se, and when n is 0, A is not CH.sub.2, and when n is 1, A is not CH.sub.2 or NH; X is a substituted or unsubstituted C.sub.1 -C.sub.3 alkyl, C.sub.2 -C.sub.3 alkenyl, C.sub.2 -C.sub.3 alkynyl or amino, or sulfur or oxygen; Ar is a substituted or unsubstituted monocyclic carbocycle or heterocycle, or fused or nonfused polycyclic carbocycle or heterocycle; and R.sub.1 and R.sub.2 are hydrogen or a moiety that forms together with the attached CO.sub.2 a readily hydrolyzable ester group. These compounds and their salts are useful as inhibitors of GARFT or as antiproliferative agents. The invention also pertains to pharmaceutical compositions and methods employing such compounds as GARFT inhibitors or antiproliferative agents. The invention also relates to compounds useful as intermediates for preparing such compounds, and to their synthesis.

    摘要翻译: 本发明一般涉及与其4-羟基互变异构体平衡的式I化合物及其药学上可接受的盐:其中n为0至2; A是S,CH 2,O,NH或Se,当n是0时,A不是CH2,当n是1时,A不是CH2或NH; X是取代或未取代的C 1 -C 3烷基,C 2 -C 3烯基,C 2 -C 3炔基或氨基,或硫或氧; Ar是取代或未取代的单环碳环或杂环,或稠合或非稠合多环碳环或杂环; 并且R 1和R 2是氢或与所连接的CO 2一起易于水解的酯基的部分。 这些化合物及其盐可用作GARFT的抑制剂或抗增殖剂。 本发明还涉及使用诸如GARFT抑制剂或抗增殖剂的化合物的药物组合物和方法。 本发明还涉及可用作制备这些化合物的中间体的化合物及其合成。

    Novel chemical synthesis
    10.
    发明授权
    Novel chemical synthesis 失效
    新型化学合成

    公开(公告)号:US3926971A

    公开(公告)日:1975-12-16

    申请号:US47227374

    申请日:1974-05-22

    申请人: POLAROID CORP

    CPC分类号: C09B23/06 C07D233/14

    摘要: A method is disclosed for preparing 2- Beta -anilinovinyl derivatives of benzimidazolium salts, useful in the preparation of cyanine dyes and related compounds, which comprises condensing a benzimidazolium salt having a reactive methyl group with an alkyl isoformanilide in a glycol ether medium.

    摘要翻译: 公开了一种用于制备苯并咪唑鎓盐的2-苯乙烯基乙烯基衍生物的方法,其可用于制备花青染料和相关化合物,其包括将具有反应性甲基的苯并咪唑盐与二醇醚介质中的烷基异丙酰苯缩合。