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公开(公告)号:US4638002A
公开(公告)日:1987-01-20
申请号:US576399
申请日:1983-12-30
申请人: Istvan Szekely , Sandor Botar , Krisztina Dolgos nee Kekesi , Bela Bertok , Antal Gajary , Tamas Szabolcsi , Gabor Kovacs , Marianna Lovasz nee Gaspar
发明人: Istvan Szekely , Sandor Botar , Krisztina Dolgos nee Kekesi , Bela Bertok , Antal Gajary , Tamas Szabolcsi , Gabor Kovacs , Marianna Lovasz nee Gaspar
IPC分类号: C07C69/76 , A61K31/343 , A61K31/5585 , A61P1/04 , A61P39/00 , C07C51/363 , C07C51/367 , C07C63/04 , C07C63/70 , C07C65/03 , C07C65/21 , C07C67/00 , C07C69/88 , C07C201/00 , C07C205/58 , C07C231/00 , C07C231/12 , C07C253/00 , C07C405/00 , C07D209/42 , C07D257/04 , C07D307/00 , C07D307/935 , C07D307/937 , C07D405/00 , C07D405/10 , C07F9/40 , C07F9/535 , C07F9/54 , A61K31/44
CPC分类号: C07D257/04 , C07C205/58 , C07C255/00 , C07C405/00 , C07C405/0041 , C07C405/0083 , C07C65/03 , C07C65/21 , C07D307/935 , C07D307/937 , C07D405/10 , C07F9/4015 , C07F9/5352 , C07F9/5456
摘要: The invention relates to new 2,3,4-trinor-1,5-inter-m-phenylene-PGI.sub.2 derivatives of the formula (I) ##STR1## wherein A stands for carboxy, cyano, tetrazolyl or --COOR.sup.3 or --CONR.sup.1 R.sup.2 ;R.sup.3 is C.sub.1-4 alkyl or an equivalent of a pharmacologically acceptable cation:R.sup.1 and R.sup.2 each stands for hydrogen, phenyl; C.sub.1-5 alkyl, optionally substituted by carboxy, hydroxy, phenyl or C.sub.2-5 alkoxycarbonyl; or C.sub.1-4 alkylsulfonyl; orR.sup.1 and R.sup.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.tbd.C-- group:R.sup.4 stands for hydrogen or tetrahydro-pyran-2-yl;R.sup.5 represents an alkyl group containing 5-9 carbon atoms, which can be optionally interrupted by one or more oxygen atom(s) or --CH.dbd.CH-- or --C.tbd.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;R.sup.6 is hydrogen or C.sub.1-4 alkyl;R.sup.7 stands for hydrogen, halogen, cyano, C.sub.1-4 alkyl or C.sub.1-4 alkoxy;R.sup.8 is hydrogen, halogen, cyano, nitro, hydroxy or C.sub.2-5 alkanoylamido;with the proviso that ifR.sup.5 stands for an alkyl group containing 5-9 carbon atoms which is unsubstituted or not interrupted by an oxygen atom or a --CH.dbd.CH-- or --C.tbd.C-- group; or a phenyoxymethyl group optionally substituted by halogen or trifluoromethyl, theneither R.sup.7 or R.sup.8 is other than hydrogen, or A is other than carboxy or --COOR.sup.3 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.