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1. 发明授权

US4740523A Interfuranylene prostacyclins 失效
标题翻译：二烯呋喃前列环素
公开(公告)号：US4740523A
公开(公告)日：1988-04-26
申请号：US820434
申请日：1986-01-17
申请人： Geza Galambos , Jozsef Ivanics , Gyorgy Dorman , Karoly Kanay , Istvan Tomoskozy , Gabor Kovacs , Istvan Stadler , Peter Kormoczi , Pal Hadhazy , Sandor Virag , Miklos Kiss
发明人： Geza Galambos , Jozsef Ivanics , Gyorgy Dorman , Karoly Kanay , Istvan Tomoskozy , Gabor Kovacs , Istvan Stadler , Peter Kormoczi , Pal Hadhazy , Sandor Virag , Miklos Kiss
IPC分类号： C07C405/00 , A61K31/35 , A61K31/557 , A61K31/5585 , A61P7/02 , A61P9/12 , A61P9/14 , A61P11/08 , A61P35/00 , C07D307/935 , C07D311/02 , C07D407/04 , C07D407/14 , C07D311/00
CPC分类号： C07D407/04
摘要： The invention relates to novel interfuranylene-prostacyclin derivatives of the general formula (I) ##STR1## wherein R.sup.1 stands for hydrogen or a straight or branched chain C.sub.1-6 alkyl group, an inorganic cation or for the protonated form of a base containing an amino group;R.sup.2 stands for hydrogen, a C.sub.1-4 alkanoyl or benzoyl group, a monosubstituted benzoyl, trialkylsilyl or an alkoxyalkyl group;R.sup.3 stands for a straight or branched chain C.sub.1-6 alkyl group, a phenyl group optionally substituted by halogen or by a C.sub.1-4 alkyl group, a heteroaryl group optionally substituted by halogen or by a C.sub.1-4 alkyl group or a cycloalkyl group;A stands for an ethylene or for a cis- or trans-vinylene or --C.tbd.C-- group;B means a chemical bond, a --CHR.sup.5 --, --CHR.sup.5 --CH.sub.2 -- or a --CH.sub.2 --O-- group: andR.sup.5 means hydrogen or a C.sub.1-4 alkyl group.The compounds of the formula (I) can be used therapeutically as platelet aggregation inhibiting, anti-thrombotic, hypotensive and anti-antherosclerotic agents; they are much more stable than the natural prostacyclin derivatives.
摘要翻译：本发明涉及通式（I）的新型二亚呋喃基 - 前列环素衍生物，其中R1代表氢或直链或支链C 1-6烷基，无机阳离子或质子化形式的碱含有氨基; R2代表氢，C1-4烷酰基或苯甲酰基，单取代的苯甲酰基，三烷基甲硅烷基或烷氧基烷基; R3代表直链或支链C 1-6烷基，任意被卤素取代的苯基或被C 1-4烷基任选取代的杂芳基，或被卤素或C1-4烷基或环烷基任选取代的杂芳基; A代表乙烯或顺式 - 或反式 - 亚乙烯基或-C 3位C基团; B表示化学键，-CHR5-，-CHR5-CH2-或-CH2-O-基，R5表示氢或C1-4烷基。式（I）化合物可以治疗性地用作血小板聚集抑制剂，抗血栓形成剂，降压药和抗动脉粥样硬化剂; 它们比天然前列环素衍生物更稳定。

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