首页> 外国专利> NOVEL 1,2,5-TRISUBSTITUTED 1,2-DIHYDRO-INDAZOL-3-ONES WITH ANTI-ASTHMATIC, ANTI-ALLERGIC, ANTI-INFLAMMATORY, IMMUNO-MODULATING AND NEURO-PROTECTIVE EFFECT, METHOD FOR THE PRODUCTION THEM AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM

NOVEL 1,2,5-TRISUBSTITUTED 1,2-DIHYDRO-INDAZOL-3-ONES WITH ANTI-ASTHMATIC, ANTI-ALLERGIC, ANTI-INFLAMMATORY, IMMUNO-MODULATING AND NEURO-PROTECTIVE EFFECT, METHOD FOR THE PRODUCTION THEM AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM

机译:新型1,2,5-三取代1,2-二氢吲哚-3-酮,具有抗吸入性,抗过敏,抗炎,免疫调节和神经保护作用,其制备方法和包含药物的药物成分他们

摘要

The present invention provides novel 1,2,5-substituted 1,2-dihydroindazol-3-one derivatives of formula (I) wherein X is -SO2-, -SO-, - (CH2) p-, - (CH2) pO-, - (CH2) p- (C = O) -, - (CH2) p- (C = O) -NH-, - (CH2) p-CHOH-, -CHOH- (CH2) p -, - (CH 2) p -CH = CH-, -CH = CH- (CH 2) p - where p is 1, 2, 3 or 4, Y is - (C = O) -, - (C = O). ) -NH-, - (C = O) -NH- (CH 2) p -, - (C = O) - (CH 2) p -, - (CH 2) p O -, - (CH 2) p - (C = O). ) -, - (CH 2) p - (C = O) -NH-, - (CH 2) p - (C = O) -NH- (CH 2) p -, - (CH 2) p -CHOH-, -CHOH - (CH2) p-, - (CH2) p-CH = CH-, -CH = CH- (CH2) p-, wherein p is 1, 2, 3 or 4, Z is -O-, -O- ( CH 2) p - (p = 1, 2, 3 or 4) or -NH-, -NH- (C = O) -, -NH- (C = O) -NH-, -NH- (C = O) -O-, -NH-CH 2 - (C = O) - or -NH- (C = O) -CH 2, R 1, R 2 and R 3 are the same or different and can be selected from the group consisting of 5-14 ring members, mono-, bi- or tricyclic, saturated or singly or multiply unsaturated carbocycle, preferably phenyl, naphthyl, anthranil, fluorenyl, mono-, bi- or tricyclic, saturated, 5-15 ring members or a single or polyunsaturated heterocyclic group containing from 1 to 6 heteroatoms, preferably N, O and / or S, preferably thienyl, pyridinyl, isoxazolyl, benzomidazolyl, benz [1,3] dioxolyl, pyrimidinyl; , quinolyl, quinazolinyl, morpholinyl, pyrrolidinyl, pyrrolyl, phenyl [1,2,4] oxadiazolyl or phenylthiazolyl, and acarbocyclic and heterocyclic groups may be singly or multiply substituted, respectively, for their preparation and their use as therapeutic agents. The compounds have anti-asthmatic, anti-allergic, anti-inflammatory and immunomodulatory properties. SHE
机译:本发明提供了式(I)的新的1,2,5-取代的1,2,5-二氢吲唑-3-酮衍生物,其中X是-SO 2-,-SO-,-(CH 2)p-,-(CH 2)pO。 -,-(CH2)p-(C = O)-,-(CH2)p-(C = O)-NH-,-(CH2)p-CHOH-,-CHOH-(CH2)p-,-( CH 2)p -CH = CH-,-CH = CH-(CH 2)p-其中p为1,2,3或4,Y为-(C = O)-,-(C = O)。 )-NH-,-(C = O)-NH-(CH 2)p-,-(C = O)-(CH 2)p-,-(CH 2)p O-,-(CH 2)p -(C = O)。 )-,-(CH 2)p-(C = O)-NH-,-(CH 2)p-(C = O)-NH-(CH 2)p-,-(CH 2)p -CHOH- ,-CHOH-(CH 2)p-,-(CH 2)p-CH = CH-,-CH = CH-(CH 2)p-,其中p是1、2、3或4,Z是-O-,- O-(CH 2)p-(p = 1,2,3或4)或-NH-,-NH-(C = O)-,-NH-(C = O)-NH-,-NH-( C = O)-O-,-NH-CH 2-(C = O)-或-NH-(C = O)-CH 2,R 1,R 2和R 3相同或不同,可以选择选自单环,双环或三环,饱和或单或多不饱和碳环的5-14个环成员,优选苯基,萘基,蒽基,芴基,单环,双环或三环,饱和的5-15环含有1至6个杂原子,优选N,O和/或S,优选噻吩基,吡啶基,异恶唑基,苯并咪唑基,苯并[1,3]二恶唑基,嘧啶基的成员或单个或多不饱和杂环基;为了它们的制备和用作治疗剂,可以分别将一个或多个取代基,喹啉基,喹唑啉基,吗啉基,吡咯烷基,吡咯基,苯基[1,2,4]恶二唑基或苯基噻唑基以及碳环和杂环基团取代。这些化合物具有抗哮喘,抗过敏,抗炎和免疫调节的特性。她

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