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17 条记录 (耗时 0.025 秒)

    Compound useful as antiproliferative agents and GARFT inhibitors
    1.
    发明授权
    Compound useful as antiproliferative agents and GARFT inhibitors 失效
    可用作抗增生剂和GARFT抑制剂的化合物

    公开(公告)号：US5610319A

    公开(公告)日：1997-03-11

    申请号：US474764

    申请日：1995-06-07

    申请人： Michael D. Varney ,  William H. Romines ,  Cynthia L. Palmer

    发明人： Michael D. Varney ,  William H. Romines ,  Cynthia L. Palmer

    IPC分类号： C07D475/04 ,  A61K31/505 ,  A61K31/519 ,  A61P35/00 ,  A61P43/00 ,  C07D471/04 ,  C07D487/04 ,  C07D498/04 ,  C07D513/04 ,  C07D517/04 ,  C07D333/38 ,  C07D207/337 ,  C07D307/54

    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。

    Processes for preparing antiproliferative garft-inhibiting compounds
    3.
    发明授权
    Processes for preparing antiproliferative garft-inhibiting compounds 失效
    制备抗增殖性阻滞化合物的方法

    公开(公告)号：US5594139A

    公开(公告)日：1997-01-14

    申请号：US282293

    申请日：1994-07-28

    申请人： Michael D. Varney ,  William H. Romines ,  Cynthia L. Palmer

    发明人： Michael D. Varney ,  William H. Romines ,  Cynthia L. Palmer

    IPC分类号： C07D475/04 ,  A61K31/505 ,  A61K31/519 ,  A61P35/00 ,  A61P43/00 ,  C07D471/04 ,  C07D487/04 ,  C07D498/04 ,  C07D513/04 ,  C07D517/04

    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。

    Antiproliferative substituted 5-thiapyrimidinone and 5-selenopyrimidinone compounds
    4.
    发明授权
    Antiproliferative substituted 5-thiapyrimidinone and 5-selenopyrimidinone compounds 失效
    抗增殖取代的5-硫代嘧啶酮和5-硒代嘧啶酮化合物

    公开(公告)号：US06323210B2

    公开(公告)日：2001-11-27

    申请号：US09782284

    申请日：2001-02-14

    申请人： Michael D. Varney ,  William H. Romines ,  Cynthia L. Palmer ,  Judith G. Deal

    发明人： Michael D. Varney ,  William H. Romines ,  Cynthia L. Palmer ,  Judith G. Deal

    IPC分类号： C07D23936

    CPC分类号： C07D239/56 ,  C07D409/12

    摘要： Novel derivatives of 5-thia- and 5-selenopyrimidinone are sound to inhibit the enzyme glycinamide ribonucleotide formyl transferase (GARFT) and amino imidazole carboxamide ribonucleotide formyl transferase (AICARFT). Novel intermediates of these compounds are also disclosed. A novel method of preparing such compounds is also disclosed, as well as methods and compositions for employing the compounds as antiproliferative agents.

    摘要翻译： 5-硫杂和5-硒代嘧啶酮的新型衍生物有效抑制甘氨酰胺核糖核苷酸甲酰转移酶（GARFT）和氨基咪唑甲酰胺核糖核苷酸甲酰转移酶（AICARFT）。 还公开了这些化合物的新型中间体。 还公开了制备这些化合物的新方法，以及使用该化合物作为抗增殖剂的方法和组合物。

    Compounds useful as antiproliferative agents and garft inhibitors
    9.
    发明授权
    Compounds useful as antiproliferative agents and garft inhibitors 失效
    可用作抗增生剂和绒毛抑制剂的化合物

    公开(公告)号：US5641771A

    公开(公告)日：1997-06-24

    申请号：US483178

    申请日：1995-06-07

    申请人： Michael D. Varney ,  William H. Romines ,  Cynthia L. Palmer

    发明人： Michael D. Varney ,  William H. Romines ,  Cynthia L. Palmer

    IPC分类号： C07D475/04 ,  A61K31/505 ,  A61K31/519 ,  A61P35/00 ,  A61P43/00 ,  C07D471/04 ,  C07D487/04 ,  C07D498/04 ,  C07D513/04 ,  C07D517/04 ,  C07D413/14 ,  A61K31/535 ,  A61K31/54 ,  C07D417/14

    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。