| 摘要 |
Substituted carbamoylmethyl-azulene derivatives (I) are new. 6-(Substituted carbamoylmethyl)-azulene derivatives of formula (I) and their tautomers, enantiomers, diastereomers, racemates, salts, esters and derivatives which are hydrolysed or metabolized in vivo to compounds (I) are new: R1-R3 = H; OH; NH2; SH; optionally substituted saturated or unsaturated 1-15C aliphatic group; alkoxy; mono- or di-alkylamino; alkylmercapto; alkylsulphinyl; alkylsulphonyl; alkenyl; alkynyl; alkenyloxy; alkenylmercapto; alkynyloxy; alkynylmercapto; mono- or di-alkylcarbonylamino; alkylaminocarbonyl; CHO; alkylcarbonyl; COOH; alkoxycarbonyl; alkenyloxycarbonyl; alkynyloxycarbonyl; carboxyalkyl; alkoxycarbonylalkyl; alkenyloxycarbonylalkyl; alkynyloxycarbonylalkyl; NO2; CN: halo; CF3; N3; optionally substituted phenyl or phenylcarbonyl; 7-15C mono- di- or tricarbocyclyl; or heterocyclyl; R5, R6 = as R1-R3 other than OH, NH2 or SH; R7 = H or alkyl; X = bond; alkylene; CO or alkylenecarbonyl; R8 = alkyl optionally substituted by OH, alkoxy, NH2 or mono- or dialkylamino; 1,3-dioxolan-4-yl optionally substituted in the 2-position; PO(R11)(R12); PO(OR13)(OR14); or, when X is other than a bond, then R8 may also be OH, alkoxy, hydroxyalkoxy, alkanoyloxy, alkylcarbonylamino, alkoxycarbonyloxy, alkanoyloxyalkyl, carboxyvinyl, optionally substituted aminoalkanoyloxy, aminoalkylphenyl or aminoalkylbenzoyloxy; alkanoyloxyalkoxy or NR9R10; R9, R10 = H or alkyl optionally substituted by OH, alkoxy, NH2 or mono- or dialkylamino; or R9 = H and R10 = OH; imidazolin-2-yl; or tetrazol-5-yl; or NR9R10 = heterocyclic ring optionally containing N or O, optionally substituted with alkyl, alkoxy, OH, hydroxyalkyl, oxo, COOH, CONH2 or alkoxycarbonyl and optionally benzo-fused; R11, R12 = alkyl; R13, R14 = H or alkyl. |
