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    NOVEL ENZYME INHIBITORS, THEIR SYNTHESIS, AND METHODS FOR USE
    15.
    发明公开
    NOVEL ENZYME INHIBITORS, THEIR SYNTHESIS, AND METHODS FOR USE 失效
    新的酶抑制剂，其使用的合成和方法

    公开(公告)号：EP0725641A1

    公开(公告)日：1996-08-14

    申请号：EP94929398.0

    申请日：1994-09-30

    申请人： El Kouni, Mahmoud H. ,  Naguib, Fardos N. M. ,  Schinazi, Raymond F.

    发明人： El Kouni, Mahmoud H. ,  Naguib, Fardos N. M. ,  Schinazi, Raymond F.

    IPC分类号： A61K31 ,  A61P31 ,  A61P33 ,  A61P35 ,  A61P43 ,  C07D239

    CPC分类号： C07D239/24 ,  C07D239/60

    摘要： Novel compounds are provided that are effective to inhibit the activity of DHUDase or UrdPase. Such compounds have general formula (I) or (II), where X is S or Se; Y is I, F, Cl, Br, methoxy, benzyl, selenenylphenyl, or thiophenyl, and R1 is an acyclo tail having general formula (III), where R2 is H, CH2OH or CH2NH2; R3 is OH, NH2, or OCOCH2CH2CO2H; and R4 is O, S, or CH2. The compounds can be used in pharmaceutical compositions, along with various chemotherapeutic agents to increase the efficacy of the treatment. These compounds can also be used in methods of treating patients by coadministering or sequentially administering the enzyme inhibiting compounds with a chemotherapeutic agent effective to treat cancers, or viral, fungal, bacterial, or parasitic infections. The compounds have further utility in enhancing imaging. Further, they can be administered alone to prevent and/or treat disorders of pyrimidine catabolism and other physiological disorders.

    New heterocyclic derivatives
    16.
    发明公开
    New heterocyclic derivatives 失效
    Heterozyklische Derivate。

    公开(公告)号：EP0309425A2

    公开(公告)日：1989-03-29

    申请号：EP88830377.3

    申请日：1988-09-19

    申请人： ISTITUTO DE ANGELI S.p.A.

    发明人： Nicola, Massimo ,  Donetti, Arturo ,  Cereda, Enzo ,  Turconi, Marco ,  Schiavi, Giovanni Battista ,  Micheletti, Rosamaria

    IPC分类号： C07D239/06 ,  C07D239/14 ,  C07D233/48 ,  C07D233/06 ,  A61K31/505 ,  A61K31/415

    CPC分类号： C07D239/06 ,  C07D233/48 ,  C07D239/24

    摘要： New pharmacologically active heterocyclic derivatives as muscarinic receptor blocking agents, useful for the treatment of gastrointestinal disorders of the following formula
    wherein
    R is hydrogen atom or C₁₋₉ alkyl optionally substituted by 2 or 3 radicals, which may be identical or different from each other, selected from aryl, cycloalkyl, hydroxy and carboxamide;
    R₁ may be any group indicated for R, or NHR₄, in which R₄ is hydrogen atom, C₁₋₄ alkyl substituted by -OOCR₅, in which R₅ is methyl sub­stituted by 2 or 3 radicals, which may be identical or different from each other, selected from aryl, cycloalkyl and hydroxy, or a cycloalkyl substituted by another cycloalkyl;
    R₂ is hydrogen atom, C₁₋₄ alkyl, a radical -OOCR₅, in which R₅ is as hereinbefore defined;
    R₃ is hydrogen atom or C₁₋₄ alkyl;
    n is 0, 1 or 2
    provided that at least one among R, R₁, R₂ and R₃ is different from hydrogen atom.
    The tautomers of the compounds of formula (I) and acid addition salts thereof, as well as the processes for their preparation and pharmaceu­tical compositions containing them are also described

    摘要翻译： 新的药物活性杂环衍生物作为毒蕈碱受体阻断剂，可用于治疗下列化学式的胃肠道疾病，其中R是氢原子或任选被2或3个基团取代的C1-9烷基，其可以相同或不同 彼此，选自芳基，环烷基，羟基和甲酰胺; R1可以是R或NHR4表示的任何基团，其中R 4是氢原子，被-OOCR 5取代的C 1-4烷基，其中R 5被2或3个可被相同或不同的基团取代的甲基， 选自芳基，环烷基和羟基，或被另一环烷基取代的环烷基; R 2是氢原子，C 1-4烷基，基团-OOCR 5，其中R 5如上所定义; R3是氢原子或C1-4烷基; n是0,1或2，条件是R，R 1，R 2和R 3中的至少一个不同于氢原子。 还描述了式（I）化合物及其酸加成盐的互变异构体及其制备方法和含有它们的药物组合物