89540-41-0Relevant articles and documents
Compounds - 801
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Page/Page column 24-25, (2011/04/14)
Spirocyclic amide derivatives of formula I wherein ArCH2CH2NH— represents a β-adrenoceptor binding group, processes for their preparation, pharmaceutical compositions containing them, a process for preparing such pharmaceutical compo
2,3,4-trinor-1,5-inter-meta-phenylene-prostacyclin compounds useful in inhibiting thrombocyte aggregation
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, (2008/06/13)
The invention relates to new 2,3,4-trinor-1,5-inter-m-phenylene-PGI2 derivatives of the formula (I) STR1 wherein A stands for carboxy, cyano, tetrazolyl or --COOR3 or --CONR1 R2 ; R3 is C1-4 alkyl or an equivalent of a pharmacologically acceptable cation: R1 and R2 each stands for hydrogen, phenyl; C1-5 alkyl, optionally substituted by carboxy, hydroxy, phenyl or C2-5 alkoxycarbonyl; or C1-4 alkylsulfonyl; or R1 and R2 together form an α,ω-alkylene chain containing 3-6 carbon atoms; B stands for oxygen or methylene; Y is optionally bromo-substituted vinylene or a --C C-- group: R4 stands for hydrogen or tetrahydro-pyran-2-yl; R5 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 phenyoxymethyl group optionally substituted by halogen or trifluoromethyl; or an alkenoyloxymethyl group containing 3-5 carbon atoms; R6 is hydrogen or C1-4 alkyl; R7 stands for hydrogen, halogen, cyano, C1-4 alkyl or C1-4 alkoxy; R8 is hydrogen, halogen, cyano, nitro, hydroxy or C2-5 alkanoylamido; with the proviso that if R5 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 phenyoxymethyl group optionally substituted by halogen or trifluoromethyl, then either R7 or R8 is other than hydrogen, or A is other than carboxy or --COOR3 and a process for the preparation thereof. The new compounds of the 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.