Oligopeptide derivatives of ipoxantine endowed with immunomodulating
activity and pharmaceutical compositions containing same
    4.
    发明授权
    Oligopeptide derivatives of ipoxantine endowed with immunomodulating activity and pharmaceutical compositions containing same 失效
    具有免疫调节活性的异辛胺的寡肽衍生物和含有它们的药物组合物

    公开(公告)号:US5298621A

    公开(公告)日:1994-03-29

    申请号:US723418

    申请日:1991-06-28

    摘要: Ipoxantine derivatives of general formula (I): ##STR1## 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 (SEQ ID NO: 1), valyl-aspartyl-lysyl-arginine (SEQ ID NO: 2), threonylvalyl-leucyl-histidyne (SEQ ID NO: 3); and(d) arginyl-lysyl-aspartyl-valyl-tyrosine (SEQ ID NO: 4);are endowed with immunomodulating activity and can be formulated in orally or parenterally administrable pharmaceutical compositions.

    摘要翻译: 作为外消旋物和手性形式的通式(I)的碘醇衍生物:(*化学结构*)及其与药理学上可接受的阳离子的盐,其中n是2和6之间的整数,A是二肽的残基, 分别选自:(a)甘氨酰 - 天冬氨酸,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;三肽,四肽和五肽; (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 - 甘氨酰胺,脯氨酰 - 苯丙氨酰 - 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(SEQ ID NO:1),缬氨酰天冬氨酰赖氨酰 - 精氨酸(SEQ ID NO:2),苏氨酰缬氨酰 - 亮氨酰 - 组氨酸(SEQ ID NO:3); 和(d)精氨酰 - 赖氨酰 - 天冬氨酰 - 缬氨酰 - 酪氨酸(SEQ ID NO:4); 具有免疫调节活性,并可配制成口服或非肠道给药的药物组合物。

    Process for the preparation of 9-amino substituted 9,10-dihydropyrrolo[2,1-b][1,3]benzotiazepines
    10.
    发明授权
    Process for the preparation of 9-amino substituted 9,10-dihydropyrrolo[2,1-b][1,3]benzotiazepines 失效
    制备9-氨基取代的9,10-二氢吡咯并[2,1-b] [1,3]苯并氮杂的方法

    公开(公告)号:US07078521B2

    公开(公告)日:2006-07-18

    申请号:US10343629

    申请日:2001-07-20

    IPC分类号: C07D513/04

    CPC分类号: C07D513/04

    摘要: A process is described for the preparation of compounds with the following formula where the groups are as defined below; in particular, R1 is a substituted amine; said process includes essentially the reaction of pyrrolobenzothiazepin-9-one with amine R1H to give the corresponding enamine, which is subsequently transformed into the final compound

    摘要翻译: 描述了用于制备具有下式的化合物的方法,其中基团如下所定义; 特别地,R 1是取代的胺; 所述方法基本上包括吡咯并苯并硫氮杂-9-酮与胺R 1 H的反应,得到相应的烯胺,随后将其转化为最终化合物