首页> 外国专利> New hydroxy-indole derivatives useful in treatment of degenerative joint disease, viral and parasitic infections, bronchial, dermatological, neurodegenerative and prostate disorders, etc.

New hydroxy-indole derivatives useful in treatment of degenerative joint disease, viral and parasitic infections, bronchial, dermatological, neurodegenerative and prostate disorders, etc.

机译:新的羟基吲哚衍生物可用于治疗退行性关节疾病,病毒和寄生虫感染,支气管,皮肤病学,神经退行性疾病和前列腺疾病等。

摘要

Hydroxyindole derivatives (I) are new. 5- or 6-Hydroxyindole derivatives (I), including optical isomers, racemates and diastereomers, and their addition and base salts are new: A = bond; -(CH2)m-; -(CH2)m-(CH=CH)n-(CH2)p-; -(CHOZ)m-; -C(O)-; -C(S)-; -C(=N-Z)-; -O-; -S-; or -N(Z)-; m and p = 0-3; n = 0-2; Z = H; alkyl; alkenyl; or a heterocycle or carbocycle (each mono-, bi- or tricyclic and saturated or mono- or poly-unsaturated); B = C; S; or S(O); D = O or N-Z or, when B = C, also S or CH2; E = bond; -(CH2)m-; -O-; -S-; or -N(Z)-; R1 and R5 = alkyl, alkenyl, a heterocycle, carbocycle or carbocyclic or heterocyclic spirocycle (each optionally mono- or poly-substituted with Q); Q = OH; SH; NH2; NH(alkyl); N(alkyl)2; NH(aryl); N(aryl)2; N(alkyl)(aryl); NHCOR6; NO2; CN; F; Cl; Br; I; alkoxy; aryloxy; OC(O)R6; alkylthio; arylthio; SOR6; SO3H; SO2R6; alkyl-SO2O; aryl-SO2O; C(S)R6; COOH; C(O)R6; or a heterocycle or carbocycle (aryl, heterocycle and carbocycle are optionally mono- or poly-substituted with R4); R2 and R3 = H or OH, but at least one is OH; R4 = H; OH; SH; NH2; NH(alkyl) N(alkyl)2; NH(aryl); N(aryl)2; N(alkyl)(aryl); NHCOR6; NO2; CN; COOH; C(O)R6; C(S)R6; F: Cl; Br; I; alkoxy; aryloxy; OC(O)R6; alkylthio; arylthio; SOR6; or SO2R6; R6 = H; NH2; NH(alkyl); N(alkyl)2; NH(aryl); N(aryl)2; N(alkyl)(aryl); alkoxy; aryloxy; alkylthio; arylthio; arylthio-alkyl; alkenyl; or a heterocycle or carbocycle. The full definitions are given in the DEFINITIONS (Full Definitions) Field. Independent claims are also included for the preparation of compounds (I).
机译:羟基吲哚衍生物(I)是新的。 5-或6-羟基吲哚衍生物(I),包括旋光异构体,外消旋体和非对映异构体,以及它们的加成盐和碱式盐是新的。 -(CH2)m-; -(CH 2)m-(CH = CH)n-(CH 2)p-; -(CHOZ)m-; -C(O)-; -C(S)-; -C(= N-Z)-; -O- ;; -S-;或-N(Z)-; m和p = 0-3; n = 0-2; Z = H;烷基;烯基或杂环或碳环(各自为单环,双环或三环以及饱和或单不饱和或多不饱和); B = C; S;或者); D = O或N-Z,或者当B = C时也为S或CH2; E =键; -(CH2)m-; -O- ;; -S-;或-N(Z)-; R 1和R 5 =烷基,烯基,杂环,碳环或碳环或杂环螺环(各自任选被Q单或多取代); Q = OH; SH; NH2; NH(烷基); N(烷基)2; NH(芳基); N(芳基)2; N(烷基)(芳基); NHCOR <6>; NO2; CN; F;氯溴一世;烷氧基芳氧基; OC(O)R 6;烷硫基芳硫基; SOR <6>; SO3H; SO 2 R 6;烷基-SO 2 O;芳基-SO 2 O; C(S)R 6; COOH; C(O)R 6;或杂环或碳环(芳基,杂环和碳环任选被R 4单或多取代);或R 2和R 3 = H或OH,但至少一个为OH; R 4 = H;哦; SH; NH2; NH(烷基)N(烷基)2; NH(芳基); N(芳基)2; N(烷基)(芳基); NHCOR <6>; NO2; CN; COOH; C(O)R 6; C(S)R 6; F:Cl;溴一世;烷氧基芳氧基; OC(O)R 6;烷硫基芳硫基; SOR <6>;或SO2R <6>; R 6 = H; NH2; NH(烷基); N(烷基)2; NH(芳基); N(芳基)2; N(烷基)(芳基);烷氧基芳氧基;烷硫基芳硫基;芳硫基烷基;烯基或杂环或碳环。完整定义在“定义(完整定义)”字段中给出。还包括制备化合物(I)的独立权利要求。

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