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135- Trisubstituted 135-triazine derivatives for treatment of HIV infections

机译:135-三取代的135-三嗪衍生物用于治疗HIV感染

摘要

The present invention relates to the use of compounds of formula (I), their N-oxides, pharmaceutically acceptable salts and stereochemically isomeric forms for the manufacture of medicaments for the treatment of HIV (human immunodeficiency virus) infected patients.;In this formula,;A is CH, CR4Or N;;n is 0, 1, 2, 3 or 4;;ROneAnd R2Each independently represent 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 the above-mentioned C1-12Each of the alkyl groups may be optionally and individually substituted;;ROneAnd R2Together are pyrrolidinyl, piperidinyl, morpholinyl, azido or mono-or di (C1-12Alkyl) amino C1-4Alkylidene;;R3Is hydrogen, aryl, C1-6Alkylcarbonyl, optionally substituted C RTI ID = 0.0 1-6Alkyl,;Each R4Are independently selected from the group consisting of hydroxy, halo, C1-6Alkyl, C1-6Alkyloxy, cyano, aminocarbonyl, nitro, amino, trihalomethyl or trihalomethyloxy;;L is-X-R5Or-X-Alk-R6;Here, R5And R6Are each independently indanyl, indolyl or phenyl; Wherein each of said indanyl, indolyl or phenyl is substituted;;X is-NR3(= O)-or-S (= O)-,-NH-NH-,-N = N-,-O-,-S-,2-;;Aryl is optionally substituted phenyl;;Het is an optionally substituted aliphatic or aromatic heterocyclic radical.;The present invention also relates to novel compounds which are subgroups of compounds of formula (I), processes for their preparation and pharmaceutical compositions containing them.
机译:本发明涉及式(I)化合物,其N-氧化物,药学上可接受的盐和立体化学异构形式在制备用于治疗HIV(人免疫缺陷病毒)感染患者的药物中的用途。 ; A为CH,CR 4 或N ;; n为0、1、2、3或4 ;; R 1 和R 2 各自独立地表示氢,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(C 1-12 烷基)氨基羰基,其中上述C 1-12 烷基中的每个可任选地和单独地被取代;; R One 和R 2 一起是吡咯烷基,哌啶基,吗啉基,叠氮基或单或二(C 1-12 烷基)氨基C 1-4 亚烷基;; R 3 < / Sup>是氢,芳基,C 1-6 烷基羰基,可选被取代的C < RTIID 0.0> 1-6 烷基,;每个R 4 独立地选自羟基,卤素,C 1-6 烷基,C 1-6 烷氧基,氰基,氨基羰基,硝基,氨基,三卤甲基或三卤甲氧基;; L is-XR 5 Or-X-Alk-R 6 <;这里,R 5 和R 6 分别独立地是茚满基,吲哚基或苯基;其中每个所述的茚满基,吲哚基或苯基均被取代;; X为-NR 3 (= O)-或-S(= O)-,-NH-NH-,-N = N- ; -O-,-S-, 2 -;;芳基是任选取代的苯基;; Het是任选取代的脂族或芳族杂环基。;本发明还涉及属于亚组的新型化合物式(I)化合物的制备,其制备方法和包含它们的药物组合物。

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