首页> 外国专利> ANTI-VIRAL NUCLEOSIDE ANALOGS AND METHODS FOR TREATING VIRAL INFECTIONS, ESPECIALLY HIV INFECTIONS.

ANTI-VIRAL NUCLEOSIDE ANALOGS AND METHODS FOR TREATING VIRAL INFECTIONS, ESPECIALLY HIV INFECTIONS.

机译:抗病毒核苷类似物和治疗病毒感染(尤其是HIV感染)的方法。

摘要

The present invention relates to novel compounds according to the general Formulae (I, II, III, IV or V); wherein B is nucleoside base according to the structure Formula (VI); R is H, F, Cl, Br, I, C1-C4 alkyl (preferably CH3),-C=N, -C=C-Ra, Formula (VII); X is H, C1-C4 alkyl (preferably, CH3), F, Cl, Br or 1; Z is 0 or CH2, with the proviso that Z is CH2 and not O when the compound is according to general formula II, R3 is -C=C-H and R2 is H or a phosphate, diphosphate, triphosphate or phosphotriester group; R1 is H, an acyl group, a C1-C20 alkyl or an ether group; R2 is H, an acyl group, a CI-C20 alkyl or ether group, a phosphate, diphosphate, triphosphate, phosphodiester group or a Formula;(VIII) or Formula (IX) group; Nu is a radical of a biologically active antiviral compound such that an amino group or hydroxyl group from said biologically active antiviral compound forms a phosphate, phosphoramidate, carbonate or urethane group with the adjacent moiety; R8 is H, or a C1-C20 alkyl or ether group, preferably a C1-C12 alkyl group; k is 0-12, preferably, 0-2; R3 is selected from a C1-C4 alkyl (preferably, CH3), -(CH2)n-C=C-Ra, Formula (X) or Formula (XI); R3a and R3b are independently selected from H, F, C1, Br or I ; R4 and R5 are independently selected from H, F, C1, Br, I, OH, C1-C4 alkyl (preferably, CH3),-(CH2)n-C=C-Ra, Formula(XII) or Formula(XIII) with the proviso that R4 and R5 are not both H; Ra is H, F, Cl, Br, I, or -C1-C4 alkyl, preferably H or CH3; Y is H, F, C1, Br, I or -C1-C4 alkyl, preferably H or CH3; and n is 0, 1, 2,3, 4 or 5, preferably 0, 1 or 2; and their anomers, pharmaceutically acceptable salts, solvates, or polymorphs thereof.
机译:本发明涉及根据通式(I,II,III,IV或V)的新型化合物。其中B是根据结构式(VI)的核苷碱基; R为H,F,Cl,Br,I,C 1 -C 4烷基(优选CH 3),-C = N,-C = C-Ra,式(VII); X是H,C 1 -C 4烷基(优选CH 3),F,Cl,Br或1; Z为0或CH 2,条件是当化合物为通式II时,Z为CH 2而不是O,R 3为-C = C-H且R 2为H或磷酸,二磷酸,三磷酸或磷酸三酯基团; R1为H,酰基,C1-C20烷基或醚基; R 2为H,酰基,C 1 -C 20烷基或醚基,磷酸根,二磷酸根,三磷酸根,磷酸二酯基或式;(VIII)或式(IX)基团; Nu是生物活性抗病毒化合物的基团,使得来自所述生物活性抗病毒化合物的氨基或羟基与相邻部分形成磷酸根,氨基磷酸根,碳酸根或氨基甲酸酯基。 R8是H,或C1-C20烷基或醚基,优选C1-C12烷基; k为0-12,优选0-2; R3选自C1-C4烷基(优选CH3),-(CH2)n-C = C-Ra,式(X)或式(XI); R3a和R3b独立地选自H,F,C1,Br或I; R4和R5独立地选自H,F,C1,Br,I,OH,C1-C4烷基(优选CH3),-(CH2)nC = C-Ra,式(XII)或式(XIII),其中条件是R4和R5都不都是H; Ra为H,F,Cl,Br,I或-C 1 -C 4烷基,优选为H或CH 3; Y为H,F,C1,Br,I或-C1-C4烷基,优选为H或CH3; n为0、1、2、3、4或5,优选为0、1或2;及其异构体,药学上可接受的盐,溶剂化物或多晶型物。

著录项

  • 公开/公告号MXPA05008736A

    专利类型

  • 公开/公告日2005-10-05

    原文格式PDF

  • 申请/专利权人 YALE UNIVERSITY;

    申请/专利号MX2005PA08736

  • 发明设计人 YUNG-CHI CHENG;

    申请日2004-02-18

  • 分类号A61K31/522;A61K31/675;A61K31/7072;A61K31/7076;C07D405/04;C07H19/06;C07H19/10;C07H19/16;C07H19/20;

  • 国家 MX

  • 入库时间 2022-08-21 22:17:15

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