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

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)-; R<1> and R<5> = 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); NHCOR<6>; NO2; CN; F; Cl; Br; I; alkoxy; aryloxy; OC(O)R<6>; alkylthio; arylthio; SOR<6>; SO3H; SO2R<6>; alkyl-SO2O; aryl-SO2O; C(S)R<6>; COOH; C(O)R<6>; or a heterocycle or carbocycle (aryl, heterocycle and carbocycle are optionally mono- or poly-substituted with R<4>); R<2> and R<3> = H or OH, but at least one is OH; R<4> = H; OH; SH; NH2; NH(alkyl) N(alkyl)2; NH(aryl); N(aryl)2; N(alkyl)(aryl); NHCOR<6>; NO2; CN; COOH; C(O)R<6>; C(S)R<6>; F: Cl; Br; I; alkoxy; aryloxy; OC(O)R<6>; alkylthio; arylthio; SOR<6>; or SO2R<6>; R<6> = 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).