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    • 6. 发明授权
    • Benzospiroalkene heterocyclic compounds
    • 苯并四氢烯烃杂环化合物
    • US5436261A
    • 1995-07-25
    • US276918
    • 1994-07-19
    • Alex CordiJean-Michel LacosteMichel LaubieTony VerbeurenJean-Jacques Descombes
    • Alex CordiJean-Michel LacosteMichel LaubieTony VerbeurenJean-Jacques Descombes
    • A61K31/415A61K31/4162A61K31/4184A61K31/4188A61K31/42A61K31/423A61K31/424A61K31/425A61K31/429A61P25/02A61P25/04A61P25/06A61P43/00C07D235/02C07D263/52C07D491/10C07D491/107C07D495/10C07D498/10C07D513/10
    • C07D235/02C07D263/52C07D491/10C07D495/10
    • Compounds of formula (I): ##STR1## in which: X represents --CH.sub.2 --, --(CH.sub.2).sub.2 --, --CH.dbd.CH--, --O--CH.sub.2 --, --S--CH.sub.2 --, --SO--CH.sub.2 -- or --SO.sub.2 --CH.sub.2 --,Y represents oxygen or sulfur or --NR.sub.6 --,R.sub.1 represents hydrogen or linear or branched (C.sub.1 -C.sub.6) alkyl,R.sub.2 represents hydrogen or halogen, linear or branched (C.sub.1 -C.sub.6) alkyl, (substituted or unsubstituted), hydroxyl, linear or branched (C.sub.1 -C.sub.6) alkoxy or linear or branched (C.sub.1 -C.sub.6) alkylthio,R.sub.3 represents hydrogen or halogen, linear or branched (C.sub.1 -C.sub.6) alkyl (substituted or unsubstituted), hydroxyl, linear or branched (C.sub.1 -C.sub.6) alkoxy or linear or branched (C.sub.1 -C.sub.6)alkylthio,R.sub.4 represents hydrogen (on condition that, in this case, R.sub.1 represents hydrogen), halogen, linear or branched (C.sub.1 -C.sub.6) alkyl (substituted or unsubstituted) or hydroxyl, or alternativelyR.sub.1 and R.sub.2, R.sub.2 and R.sub.3, R.sub.3 and R.sub.4 or R.sub.4 and X, together with the carbon atoms which bear them, form a benzene ring, on condition that, in the case where R.sub.1 and R.sub.2 form a benzene ring, X is other than --CH.sub.2 -- or --(CH.sub.2).sub.2 --,R.sub.5 represents hydrogen or amino (substituted or unsubstituted),R.sub.6 has the same meaning as R.sub.1,their isomers and also their. addition salts with a pharmaceutically acceptable acid and medicinal product containing the sarne are useful as partial .alpha..sub.1 and .alpha..sub.2 adrenergic agonist in the treatment of venous disease and migraine.
    • 式(I)化合物:其中:X表示-CH 2 - , - (CH 2)2 - , - CH = CH - , - O-CH 2 - , - S-CH 2 - ,-SO- CH2-或-SO2-CH2-,Y表示氧或硫或-NR6-,R1表示氢或直链或支链(C1-C6)烷基,R2表示氢或卤素,直链或支链(C1-C6)烷基,( 取代或未取代的),羟基,直链或支链(C1-C6)烷氧基或直链或支链(C1-C6)烷硫基,R3表示氢或卤素,直链或支链(C1-C6)烷基(取代或未取代的) 直链或支链(C1-C6)烷氧基或直链或支链(C1-C6)烷硫基,R4代表氢(在这种情况下,R1表示氢),卤素,直链或支链(C1-C6)烷基 或未取代的)或羟基,或者R1和R2,R2和R3,R3和R4或R4和X与它们携带的碳原子一起形成苯环,条件是在R1和R2形成 苯环,X不是-CH 2 - 或 - (CH 2)2 - , R5代表氢或氨基(取代或未取代的),R6具有与R1相同的含义,它们的异构体以及它们的含义。 与药学上可接受的酸和含有缬氨酸的药物的加成盐可用作治疗静脉疾病和偏头痛的部分α1和α2肾上腺素能激动剂。