摘要 |
Carbacycline derivs. of formula (I) and (when R2 is H) their salt with physiologically tolerable bases are new. n = 1 or 3; R1 = (II), (III), -COCH3, -COOR2 or -CONHR3; R2 = H, 1-10C alkyl, (opt. substd. by halogen, phenyl, 1-4C alkoxy or 1-4C dialkyl-amino), cycloalkyl, aryl or a heterocyclic residue; R3 = H, 1-10C alkanoyl or 1-10C alkylsulphonyl; R4 = 1-10C alkyl, 3-10C cycloalkyl, opt. substd. 6-10C aryl or a heterocyclic group; R5 = free or functionally modified OH; R9 = 1-10C alkyl or -C=C-(CH2)m-R6 (m = 1-16, R6 = H, OH, amino or trimethylsilyl); X = O or (when R9 = 5-10C alkyl) CH2; Y = H or F; A = -CH2CH2-, trans-CH=CH- or ethynylene; W = free or functionally modified hydroxymethylene -C(CH3)(OH)-; D = -C(CH2)0-CH2- (0 = 1-3), unbranched saturated 1-5C alkylene, or branched saturated or opt. branched unsaturated 2-5C alkylene opt. substd. by F atoms; E = direct bond, ethynylene, or -CH=CR7- (R7 = H, 1-5C alkyl or halogen).
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