New phenylene-substd. 2-oxa-bicyclo(2.2.1)heptane TXA2 antagonists
Phenylene-substd. 2-oxa-bicyclo(2.2.1.)heptane derivs. of formula (I) and their salts and alpha-, beta- and gamma-cyclodextrin clathrates as well as their liposome-encapsulated forms are new. R1 = COOR5; -CONHR7; oxazolin-2-yl; 1H-tetrazol-5-yl; 5,5-dimethyl-1,3-dioxolan-2-yl; or a gp. of formula (a...
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Zusammenfassung: | Phenylene-substd. 2-oxa-bicyclo(2.2.1.)heptane derivs. of formula (I) and their salts and alpha-, beta- and gamma-cyclodextrin clathrates as well as their liposome-encapsulated forms are new. R1 = COOR5; -CONHR7; oxazolin-2-yl; 1H-tetrazol-5-yl; 5,5-dimethyl-1,3-dioxolan-2-yl; or a gp. of formula (a); R5 = H; 1-10C alkyl opt. substd. by halo, OH, 6-12C aryl, 1-4C alkoxy or di(1-4C) alkyl)amino; 3-10C cycloalkyl; 7-16C aralkyl; phenylacyl or 6-12C aryl substd. by X; R5- or 6-membered heterocyclyl contg. at least 1 N, O or S atom; R7 = H; 1-10C alkanoyl; or 1-10C alkanesulphonyl; r = 0-3; R2 = -(CH2)s-; (E) or (Z) -CH=CH-; or -CC-; s = 0-5; A = -(CH2)n-; (E) or (Z) -CH=CH- or -CC-; n = 0-7 (but 1-7 when B = H); B = H, 1-10C alkyl; halo; CN; N3; HN2; OH; CO2R3; Ph opt. mono-, di or tri-substd. by X; 4-Ph1=Ph2; 1- or 2-naphthyl opt. mono- or di-substd. by X in the other ring; or 5-7C cycloalkyl; PH1 = phenyl opt. mono- or di-substd. by X; Ph2 = phenyl opt. mono-substd. by X; R3 = H; halo; N3; NH2; CF3; OR6; NO2; COOR6; or 1-10C alkyl; R6 = H; 1-10C alkyl; or 6-12C aryl or 7-16C aralkyl opt. substd. by halo; Z = direct bond; -(CH2)m-; (E) or (Z) -CH=CH; or -CC-; -CH=N-; -CH=N-O-; or a gp. of the formula (i) or (ii); m = 0-5; R9 H or 1-10C alkyl; Y, Z = H or Y and Z together form a bond; W = direct bond; alpha- or beta-OH (opt. functionally modified); or -NHSO2; D = satd. or unsatd. alkylene with up to 5C opt. substd. by F; or a gp. of the formula (iii) or (iv); or W and D together form a direct bond; t = 0-3; E = direct bond; -CC-; or -CH=CR8-; R8 = H; 1-10C alkyl; halo; or CF3; R4 = H; 1-10C alkyl; 3-10C cycloalkyl; 6-12C aryl or 7-16C aralkyl opt. substd. by X; %- or 6-membered heterocyclyl contg. at least 1 N, O or S atom; Ph opt. mono-; di- or tri-substd. by X; 1- or 2-naphthyl opt. mono-substd. by X in the linking ring and opt. mono- or di-substd. by X in the other ring; or pyridyl opt. mono-, di- or tri-substd. by X. |
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