首页> 外国专利> poly 4 - aminopyrrool - 2 - carboxamidoderivaten, method for preparation thereof, pharmaceutical preparations containing these derivatives and process for the preparation of the pharmaceutical preparations.

poly 4 - aminopyrrool - 2 - carboxamidoderivaten, method for preparation thereof, pharmaceutical preparations containing these derivatives and process for the preparation of the pharmaceutical preparations.

机译:聚4-氨基吡咯-2-烷基羧酰胺衍生物,其制备方法,含有这些衍生物的药物制剂以及该药物制剂的制备方法。

摘要

The invention relates to poly-4-aminopyrrole-2-carboxamido derivatives of the following formula IMAGE wherein, subject to certain provisos, n is zero or an integer of 1 to 4; R is a) -NHR3, wherein R3 is a') -CON(NO)R4, in which R4 is C1-C4 alkyl either unsubstituted or substituted by halogen; or b') -CO(CH2)m-R5, in which R5 is halogen, oxiranyl, methyloxiranyl, aziridinyl, cyclopropyl or the residue of alicyclic, alpha , beta -unsaturated ketone or lactone, and m is zero or an integer of 1 to 4; b IMAGE wherein either R6 and R7 are the same and are each oxiranemethyl, aziridinemethyl, or C2-C4 alkyl 2-substituted by halogen or by a group -OSO2R8, wherein R8 is C1-C4 alkyl or phenyl, or one of R6 and R7 is hydrogen and the other is as defined above; c) -NO2; d) -NH2; or e) -NH-CHO; each group R1 is, independently, hydrogen or C1-C4 alkyl; R2 is a C1-C6 alkyl group terminating with a basic or acidic moiety or with a free or glycosilated hydroxy group; and the pharmaceutically acceptable salts thereof. The scope of the invention includes also pharmaceutical compositions comprising compounds of the above formula and a process for preparing same. The compounds of the invention can be useful antiviral and antineoplastic agents.
机译:本发明涉及下式的聚-4-氨基吡咯-2-羧酰胺基衍生物,其中,在一定条件下,n为零或1-4的整数; R是a)-NHR3,其中R3是a')-CON(NO)R4,其中R4是未被取代或被卤素取代的C1-C4烷基;或b')-CO(CH 2)m -R 5,其中R 5为卤素,氧杂环丁烷基,甲基环氧乙烷基,叠氮基,环丙基或脂环族残基,α,β-不饱和酮或内酯,且m为零或1的整数至4; b> <图像>,其中R6和R7相同,并且各自为被卤素或被-OSO2R8基团2-取代的环氧乙烷基甲基,氮丙啶基甲基或C2-C4烷基,其中R8为C1-C4烷基或苯基,或R6和R7是氢,另一个如上定义。 c)-NO 2; d)-NH 2;或e)-NH-CHO;每个基团R 1独立地是氢或C 1 -C 4烷基; R 2为C 1 -C 6烷基,其末端为碱性或酸性部分或游离或糖基化的羟基。及其药学上可接受的盐。本发明的范围还包括包含上式化合物的药物组合物及其制备方法。本发明的化合物可以是有用的抗病毒和抗肿瘤药。

著录项

  • 公开/公告号NL8601837A

    专利类型

  • 公开/公告日1987-02-16

    原文格式PDF

  • 申请/专利权人 FARMITALIA CARLO ERBA S.P.A. TE MILAAN ITALIE.;

    申请/专利号NL19860001837

  • 发明设计人

    申请日1986-07-14

  • 分类号C07K5/02;C07K7/02;A61K37/02;

  • 国家 NL

  • 入库时间 2022-08-22 07:20:00

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