| abstract |
New 2,3,4-trinor-1,5-inter-m-phenylene-PGI2 derivatives (wherein A stands for carboxy, cyano, tetrazolyl or -COOR<3> or -CONR<1>R<2>; R<3> is C1-4 alkyl or an equivalent of a pharmacologically acceptable cation: R<1> and R<2> each stands for hydrogen, phenyl; C1-5 alkyl, optionally substituted by carboxy, hydroxy, phenyl or C2-5 alkoxycarbonyl; or C1-4 alkyl-sulfonyl; or R<1> and R<2> together form an alpha , omega -alkylene chain containing 3-6 carbon atoms; B stands for oxygen or methylene; Y is optionally bromo-substituted vinylene or a -C=C- group: R<4> stands for hydrogen or tetrahydro-pyran-2-yl; R<5> represents an alkyl group containing 5-9 carbon atoms, which can be optionally interrupted by one or more oxygen atom(s) or -CH=CH- or -C=C- group(s) and/or optionally substituted by halogen; or a phenoxymethyl group optionally substituted by halogen or trifluoromethyl; or an alkenyloxymethyl group containing 3-5 carbon atoms; R<6> is hydrogen or C1-4 alkyl; R<7> stands for hydrogen, halogen, cyano, C1-4 alkyl or C1-4 alkoxy; R<8> is hydrogen, halogen, cyano, nitro, hydroxy or C2-5 alkanoylamido; with the proviso that if R<5> stands for an alkyl group containing 5-9 carbon atoms which is unsubstituted or not interrupted by an oxygen atom or a -CH=CH- or -C=C- group; or a phenoxymethyl group optionally substituted by halogen or trifluoromethyl, then either R<7> or R<8> is other than hydrogen, or A is other than carboxy or -COOR<3>) and a process for the preparation thereof. The new compounds of the general Formula I exhibit prolonged cytoprotecting and aggregation inhibiting and a low hypotensive effect and are superior to prostacycline in the prolonged duration of their activity. |