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1,3,5-trisubstituted indazole derivatives having anti-asthmatic, anti-allergic, anti-inflammatory and immunomodulatory effects

机译:1,3,5-三取代的吲唑衍生物具有抗哮喘,抗过敏,抗炎和免疫调节作用

摘要

1,3,5-trisubstituted indazole derivatives of the formula IMAGE (I) wherein R1 is H, (b) a C1-6 straight or branched, substituted or unsubstituted alkyl residue, (c) a C3-7 cycloalkyl residue, (d) an unsustituted or substituted phenyl, naphthyl, anthranyl, or fluorenyl residue, (e) a quinolin-2-ylmethoxy, or pyridin-2-ylmethoxy residue; X is O, or a -NH, -NH-(C=O)-NH-, -NH-(C=O)-O-, -NH-(C=O)-, or -NH-CH2-(C=O)- residue; Y is O, or S; R2 is H; Z is a SO, SO2, -(CH2)p-, -(CH2)p-O-, -O-(CH2)p-, -(CH2)p-(C=O)-, -(C=O)-(CH2)p-, -(CH2)p-(C=O)-NH-, -NH-(C=O)-(CH2)p-, -(CH2)p-CHOH-, -CHOH-(CH2)p-, -(CH2)p-CH=CH-, or -CH=CH-(CH2)p- residue, wherein p is between 1 and 6; A is a phenyl, naphthyl, anthranyl, fluorenyl, thiophenyl, pyridinyl, isoxazolyl, benzimidazolyl, benz[1,3]dioxolyl, pyrimidyl, pyrimidine-2,4-dionyl, quinolinyl, quinoxazolinyl, morpholinyl, or pyrrolidinyl residue; and, R3, R4, and R5, the same or different, are defined in the specification; and pharmaceutically acceptable salts, stereoisomers, racemates, racemic modifications, and enantiomers thereof. The invention also relates to specific compounds, processes for preparing and for treating an allergic, asthmatic, inflamed condition of a host, or for modulating the immune system of a host.
机译:式<图像>的(1)的1,3,5-三取代的吲唑衍生物(I)其中R1为H,(b)C1-6直链或支链,取代或未取代的烷基残基,(c)C3-7环烷基残基, (d)未取代或取代的苯基,萘基,蒽基或芴基残基,(e)喹啉-2-基甲氧基或吡啶-2-基甲氧基残基; X是O或-NH,-NH-(C = O)-NH-,-NH-(C = O)-O-,-NH-(C = O)-或-NH-CH2- C = O)-残基; Y是O或S; R2为H; Z是SO,SO2,-(CH2)p-,-(CH2)pO-,-O-(CH2)p-,-(CH2)p-(C = O)-,-(C = O)- (CH2)p-,-(CH2)p-(C = O)-NH-,-NH-(C = O)-(CH2)p-,-(CH2)p-CHOH-,-CHOH-(CH2 )p-,-(CH2)p-CH = CH-或-CH = CH-(CH2)p-残基,其中p为1-6。 A为苯基,萘基,蒽基,芴基,噻吩基,吡啶基,异恶唑基,苯并咪唑基,苯并[1,3]二氧戊基,嘧啶基,嘧啶-2,4-二硫基,喹啉基,喹喔啉基,吗啉基或吡咯烷基残基;并且,在说明书中定义了相同或不同的R3,R4和R5;及其药学上可接受的盐,立体异构体,外消旋体,外消旋体及其对映异构体。本发明还涉及特定的化合物,用于制备和治疗宿主的过敏性,哮喘性,发炎的病症或调节宿主的免疫系统的方法。

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