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    • 103. 发明授权
    • 1H-IMIDAZO{8 1,2a{9 {8 1,4{9 BENZO-DIAZEPINE-1,2(3H)-DIONES
    • 1H-1MIDAZO {8,12a {9 {8 1,4 {9苯并二氮杂-1,2(3H) - 酮
    • US3846443A
    • 1974-11-05
    • US36461673
    • 1973-05-29
    • UPJOHN CO
    • MOFFETT R
    • A23K1/16A61K31/55A61P21/02A61P25/08A61P25/20C07D487/04C07D57/02
    • C07D487/04
    • This invention relates to 1H-imidazo(1,2-a)(1,4)-benzodiazepine1,2(3H)-diones of the formula WHEREIN R is selected from the group consisting of hydrogen, lower alkyl of 1 through 4 carbon atoms and lower alkenyl of 3 through 4 carbon atoms; R1 is selected from the group consisting of hydrogen and lower alkyl of 1 through 3 carbon atoms; R2 is selected from the group consisting of 2-pyridyl, 3-pyridyl, 4pyridyl, 2-pyrimidyl, furyl, pyrryl, thienyl, lower alkyl of 1 through 3 carbon atoms, lower alkenyl of 2 through 4 carbon atoms, cycloalkyl of 5 through 7 carbon atoms, cycloalkenyl of 5 through 7 carbon atoms and WHEREIN R5 and R6 are selected from the group consisting of hydrogen, lower alkyl of 1 through 3 carbon atoms, halogen, nitro, cyano, trifluoromethyl, lower alkoxy of 1 through 3 carbon atoms, lower alkylthio of 1 through 3 carbon atoms, lower alkylsulfinyl of 1 through 3 carbon atoms, lower alkylsulfonyl of 1 through 3 carbon atoms, lower alkanoylamino having lower alkyl moieties of 1 through 3 carbon atoms and lower dialkylamino having lower alkyl moieties of 1 through 3 carbon atoms; R3 and R4 have the same meaning as R5 and R6, above; and a pharmacologically acceptable acid addition salt thereof. The new products of Formula 1 are useful as sedatives, hypnotics, tranquilizers, muscle relaxants and anti-convulsants in mammals and birds.
    • 本发明涉及式WHEREIN R的1H-咪唑并[1,2-a] [1,4]苯并二氮杂-1,2(3H) - 二酮,其选自氢,1至4的低级烷基 碳原子和3至4个碳原子的低级烯基; R1选自氢和1至3个碳原子的低级烷基; R2选自2-吡啶基,3-吡啶基,4-吡啶基,2-嘧啶基,呋喃基,吡啶基,噻吩基,1至3个碳原子的低级烷基,2至4个碳原子的低级链烯基, 5至7个碳原子,5至7个碳原子的环烯基和WHEREIN R5和R6选自氢,1至3个碳原子的低级烷基,卤素,硝基,氰基,三氟甲基,1至3的低级烷氧基 碳原子数1〜3个碳原子的低级烷硫基,1〜3个碳原子的低级烷基亚磺酰基,1〜3个碳原子的低级烷基磺酰基,1〜3个碳原子的低级烷基部分的低级烷酰基氨基, 1至3个碳原子; R3和R4具有与上述R5和R6相同的含义; 及其药理学上可接受的酸加成盐。 式1的新产品可用作哺乳动物和鸟类中的镇静剂,催眠药,镇定剂,肌肉松弛剂和抗惊厥药。