首页> 外国专利> use of pyrimidine derivatives for use in the manufacture of the product, which is intended for the treatment of hiv infection, a compound containing pharmaceutical composition.method and composition for use in the manufacture of compound preparation of hiv nakkusera ningkombineeritud

use of pyrimidine derivatives for use in the manufacture of the product, which is intended for the treatment of hiv infection, a compound containing pharmaceutical composition.method and composition for use in the manufacture of compound preparation of hiv nakkusera ningkombineeritud

机译:嘧啶衍生物用于制备用于治疗HIV感染的产品的用途,该化合物包含药物组合物。方法和用于制备HIV的药物制剂的组合物

摘要

This invention concerns the use of the compounds of formula CHEM the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein A is CH, CR4 or N; n is 0 to 4; Q is hydrogen or -NR1R2; R1 and R2 are selected from hydrogen, hydroxy, C1-12alkyl, C1-12alkyloxy, C1-12alkylcarbonyl, C1-12alkyloxycarbonyl, aryl, amino, mono- or di(C1-12alkyl)-amino, mono- or di(C1-12alkyl)aminocarbonyl wherein each C1-12alkyl may optionally be substituted; or R1 and R2 taken together may form pyrrolidinyl, piperidinyl, morpholinyl, azido or mono- or di(C1-12alkyl)aminoC1-4alkylidene; R3 is hydrogen, aryl, C1-6alkylcarbonyl, optionally substituted C1-6alkyl, C1-6alkyloxy-carbonyl,; and R4 is hydroxy, halo, optionally substituted C1-6alkyl, C1-6alkyloxy, cyano, aminocarbonyl, nitro, amino, trihalomethyl, trihalomethyloxy; R5 is hydrogen or C1-4alkyl; L is optionally substituted C1-10alkyl, C3-10alkenyl, C3-10alkynyl, C3-7cycloalkyl; or L is -X1-R6 or -X2-Alk-R7 wherein R6 and R7 are optionally substituted phenyl; X1 and X2 are -NR3-, -NH-NH-, -N=N-, -O-, -S-, -S(=O)- or -S(=O)2-; Alk is C1-4alkanediyl; aryl is potionally substituted phenyl; Het is an optionally substituted aliphatic or aromatic heterocyclic radical; for the manufacture of a medicine for the treatment of subjects suffering from HIV (Human Immunodeficiency Virus) infection. It further relates to new compounds being a subgroup of the compounds of formula (I), their preparation and compositions comprising them.
机译:本发明涉及具有化学式的N-氧化物,其药学上可接受的加成盐及其立体化学异构体形式的用途,其中A为CH,CR 4或N; n为0至4; Q是氢或-NR 1 R 2; R 1和R 2选自氢,羟基,C 1-12烷基,C 1-12烷氧基,C 1-12烷基羰基,C 1-12烷氧基羰基,芳基,氨基,单或二(C 1-12烷基)-氨基,单-或二(C1-12烷基)氨基羰基,其中每个C1-12烷基可任选被取代;或R 1和R 2一起可以形成吡咯烷基,哌啶基,吗啉基,叠氮基或单或二(C1-12烷基)氨基C1-4亚烷基;或R 3为氢,芳基,C 1-6烷基羰基,任选取代的C 1-6烷基,C 1-6烷氧基-羰基; R 4为羟基,卤素,任选取代的C 1-6烷基,C 1-6烷氧基,氰基,氨基羰基,硝基,氨基,三卤甲基,三卤甲氧基。 R 5为氢或C 1-4烷基; L为任选取代的C 1-10烷基,C 3-10烯基,C 3-10炔基,C 3-7环烷基;或L为-X 1 -R 6或-X 2 -Alk-R 7,其中R 6和R 7为任选取代的苯基;或X 1和X 2为-NR 3-,-NH-NH-,-N = N-,-O-,-S-,-S(= O)-或-S(= O )2-;烷基为C 1-4烷二基;芳基是部分取代的苯基; Het是任选取代的脂族或芳族杂环基;制造用于治疗患有HIV(人类免疫缺陷病毒)感染的受试者的药物。它还涉及作为式(I)化合物的子集的新化合物,其制备和包含它们的组合物。

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