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2,4-DISUBSTITUTED TRIAZINE DERIVATIVES

机译:2,4-二取代的三嗪衍生物

摘要

The invention concerns the use of the compounds of formula the N-oxides, the pharmaceutically acceptable addition salts, quaternary amines and the stereochemically isomeric forms thereof, wherein -a1=a2-a3=a4- forms a phenyl, pyridinyl, pyrimidinyl, pyridazinyl or pyrazinyl with the attached group; n is 0 to 4; and where possible 5; R1 is hydrogen, aryl, formyl, C1-6 alkylcarbonyl, C1-6 alkyl, C1-6alkyloxycarbonyl or substituted C1-6 alkyl; each R2 independently is hydroxyl, halo, optionally substituted C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-7cycloalkyl, C1-6 alkyloxy, C1-6 alkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono- or di(C1-6 alkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, -S(=O)pR4, -NH-S(=O)pR4, -C(=O)R4, -NHC(O)H, -C(=O)NHNH2, -NHC(=O)R4, -C(=NH)R4 or a 5-membered heterocyclic ring; p is 1 or 2; L is optionally substituted C1-1) alkyl, C2-10 alkenyl, C2-10 alkynyl or C3-7 cycloalkyl; or L is -X-R3 wherein R 3 is optionally substituted phenyl, pyridnyl, pyrimidinyl, pyrazinyl or pyridazinyl; X is -NR1-, -NH-NH-, -N=N-, -O-, -C(=O)-, -S-, -CHOH-,-S-, -S(=O)- or -S(=O)2-; aryl is optionally substituted phenyl; for the manufacture of a medicine for the treatment of subjects suffering from HIV (Human Immunodeficiency Virus) infection. 13 claims, 1 figure
机译:本发明涉及式N-氧化物,其药学上可接受的加成盐,季胺及其立体化学异构体形式的用途,其中-a1 = a2-a3 = a4-形成苯基,吡啶基,嘧啶基,哒嗪基或吡嗪基及其连接基团; n为0至4;并在可能的情况下5; R1是氢,芳基,甲酰基,C1-6烷基羰基,C1-6烷基,C1-6烷氧羰基或取代的C1-6烷基;每个R 2独立地为羟基,卤素,任选取代的C 1-6烷基,C 2-6烯基,C 2-6炔基,C 3-7环烷基,C 1-6烷氧基,C 1-6烷氧基羰基,羧基,氰基,硝基,氨基,单或二(C1-6烷基)氨基,多卤代甲基,多卤代甲氧基,多卤代甲硫基,-S(= O)pR4,-NH-S(= O)pR4,-C(= O)R4,-NHC(O)H,-C (= O)NHNH 2,-NHC(= O)R 4,-C(= NH)R 4或5元杂环; p是1或2; L为任选取代的C1-1)烷基,C2-10链烯基,C2-10炔基或C3-7环烷基; L为-X-R3,其中R 3为任选取代的苯基,吡啶基,嘧啶基,吡嗪基或哒嗪基;或X是-NR1-,-NH-NH-,-N = N-,-O-,-C(= O)-,-S-,-CHOH-,-S-,-S(= O)-或-S(= O)2-;芳基是任选取代的苯基;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。 13个索赔,1个数字

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