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    Aminoacyl and oligopeptidyl derivatives of allopurinol exhibiting immunostimulatory activity, and pharmaceutical formulations containing these substances
    5.
    发明公开
    Aminoacyl and oligopeptidyl derivatives of allopurinol exhibiting immunostimulatory activity, and pharmaceutical formulations containing these substances 失效
    氨基酰基和具有免疫刺激作用和含有它们的药物组合物别嘌呤醇Oligopeptidylderivate。

    公开(公告)号：EP0506628A2

    公开(公告)日：1992-09-30

    申请号：EP92830136.5

    申请日：1992-03-20

    申请人： Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.

    发明人： Marzi, Mauro ,  Minetti, Patrizia ,  Foresta, Piero ,  Tinti, Maria Ornella

    IPC分类号： C07K5/04 ,  C07K7/06 ,  C07D487/04 ,  A61K31/505

    CPC分类号： C07K5/06026 ,  A61K38/00 ,  C07K5/04

    摘要： The present invention concerns aminoacyl and oligopeptidyl derivatives of allopurinol (1,5-dihydro-4H-pyrazolo-[3,4-d]-pyrimidin-4-one) of general formula (I), and related salts with

    pharmacologically-acceptable cations, in which n is an integer between 2 and 6, preferably 5, Y is H or CO-A, in which A is a racemic or chiral amino acid, dipeptide, tripeptide, tetrapeptide, or pentapeptide chosen, respectively, from the goups consisting of:

    a) arginine, aspartic acid, lysine, leucine ;
    b) glycylaspartate, glycylglycine, aspartylarginine, leucylarginine, alanylglycine ;
    c) arginyllysylaspartate, aspartyllysylarginine, lysylprolylarginine, prolylprolylarginine, lysylhis- tidylglycinamide, prolylphenylalanylarginine, phenylalanylprolylarginine ;
    d) arginyllysylaspartylvaline, valylaspartyllysylarginine, threonylvalylleucylhistidine ;
    e) arginyllysylaspartylvalyltyrosine.

    摘要翻译： 本发明涉及别嘌醇的氨基酰基和oligopeptidyl衍生物（1,5-二氢-4H-吡唑并[3,4-d]嘧啶-4-酮）的通式（I）中，并用相关的盐的药理学 -acceptable阳离子，其中n为2和6，优选5之间的整数，Y是H或CO-A，其中A是外消旋或手性氨基酸，二肽，三肽，四肽，五肽或选择，分别从 所述goups组成为：A）精氨酸，天门冬氨酸，赖氨酸，亮氨酸; b）中glycylaspartate，甘氨酰甘氨酸，aspartylarginine，leucylarginine，alanylglycine; c）中arginyllysylaspartate，aspartyllysylarginine，lysylprolylarginine，prolylprolylarginine，lysylhistidylglycinamide，prolylphenylalanylarginine，phenylalanylprolylarginine; D）arginyllysylaspartylvaline，valylaspartyllysylarginine，threonylvalylleucylhistidine; E）arginyllysylaspartylvalyltyrosine。 升

    Oligopeptide derivatives of ipoxantine endowed with immunomodulating activity and pharmaceutical compositions containing same
    8.
    发明公开
    Oligopeptide derivatives of ipoxantine endowed with immunomodulating activity and pharmaceutical compositions containing same 失效
    配备Ipoxantin寡肽具有免疫调节活性和含有它们的药物组合物。

    公开(公告)号：EP0464009A2

    公开(公告)日：1992-01-02

    申请号：EP91830284.5

    申请日：1991-06-26

    申请人： Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.

    发明人： Marzi, Mauro ,  Foresta, Piero ,  Minetti, Patrizia ,  Tinti, Maria Ornella

    IPC分类号： C07K5/00 ,  A61K37/02

    CPC分类号： C07K7/06 ,  A61K38/00 ,  C07K5/06026 ,  C07K5/06043 ,  C07K5/06113 ,  C07K5/0812 ,  C07K5/0815 ,  C07K5/0819 ,  C07K5/0823 ,  C07K5/101 ,  C07K5/1019

    摘要： Ipoxantine derivatives of general formula (I):

    both as racemate and chiral forms and the salts thereof with pharmacologically acceptable cations, wherein n is an integer comprised between 2 and 6, and A is the residue of a dipeptide, tripeptide, tetrapeptide and pentapeptide selected, respectively, from the groups consisting of:

    (a) glycyl-aspartate, alanyl-glycine, glycyl-glycine, aspartyl-arginine, leucyl-arginine;
    (b) arginyl-lysyl-aspartate, aspartyl-lysyl-arginine, lysyl-prolyl-arginine, prolyl-prolyl-arginine, lysyl-histidyl-glycinamide, prolyl-phenilalanyl-arginine, phenylalanyl-prolyl-arginine;
    (c) arginyl-lysyl-aspartyl-valine, valyl-aspartyl-lysyl-arginine, threonylvalyl-leucyl-histidyne; and
    (d) arginyl-lysyl-aspartyl-valyl-tyrosine; are endowed with immunomodulating activity and can be formulated in orally or parenterally administrable pharmaceutical compositions.

    摘要翻译： 通式（I）的Ipoxantine衍生物：既可作为外消旋体和手性形式和其与药理学上可接受的阳离子的盐，worin n是2和6，以及A之间包含的整数是二肽，三肽，四肽的残基 和五肽选择的，分别从组由以下组成：（A）甘氨酰天冬氨酸盐，丙氨酰 - 甘氨酸，甘氨酰 - 甘氨酸，天冬氨酰精氨酸，亮氨酰 - 精氨酸; （B）精氨酰 - 赖氨酰 - 天冬氨酸，天冬氨酰赖氨酰 - 精氨酸，赖氨酰 - 脯氨酰 - 精氨酸，脯氨酰 - 脯氨酰 - 精氨酸，赖氨酰 - 组氨酰 - 甘氨酸酰胺，脯氨酰 - phenilalanyl精氨酸，苯丙氨酰脯氨酰 - 精氨酸; （C）精氨酰 - 赖氨酰 - 天冬氨酰缬氨酸，缬氨酰 - 天冬氨酰基赖氨酰 - 精氨酸，threonylvalyl亮氨酰histidyne; 和（d）精氨酰 - 赖氨酰 - 天冬氨酰缬氨酰 - 酪氨酸; 赋有免疫调节活性，并且可以被配制成口服或肠胃外给药的药物组合物。 我