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    • 5. 发明授权
    • Derivatives of 1,2-dihydro 2-oxo quinoxalines, their preparation and
their use in therapy
    • 1,2-二羟基喹喔啉衍生物的制备及其在治疗中的应用
    • US5198441A
    • 1993-03-30
    • US688536
    • 1991-06-17
    • Guy PitetChristian FaureFrancoise CouretDennis BiggJean-Pierre Tarayre
    • Guy PitetChristian FaureFrancoise CouretDennis BiggJean-Pierre Tarayre
    • A61K31/495A61P11/08C07D241/44C07D401/06
    • C07D401/06C07D241/44
    • New derivatives of 1,2-dihydro 2-oxo quinoxalines corresponding to the general formula I: ##STR1## in which: R is a hydrogen or halogen atomR.sub.1 is a hydrogen atom or a straight or branched C.sub.1 -C.sub.4 alkyl radicalR.sub.2 is:a hydrogen atoma C(O)R.sub.4 radical in which R.sub.4 is a straight or branched C.sub.1 -C.sub.4 alkyl groupa C(O)NHR.sub.5 radical in which R.sub.5 is a straight or branched C.sub.1 -C.sub.4 alkyl radical or a phenyl groupA is a C.sub.1 -C.sub.4 alkaline chainR.sub.3 represents:a hydrogen atom, a C.sub.1 -C.sub.4 alkyl radical, a C.sub.3 -C.sub.6 cycloalkyl radical, an alcynyl, nitrile, hydroxyl, carboxamido, pyridyl, phenyl group, or a phenyl group substituted by a halogen atom, a C.sub.1 -C.sub.4 alkyl group, a C.sub.1 -C.sub.4 alkoxy group or a nitro groupan alkenyl radical of the formula: ##STR2## in which R.sub.6, R.sub.7 may, independently of each other, be a hydrogen atom, a C.sub.1 -C.sub.4 alkyl group, a phenyl group or an alkoxycarbonyl groupa radical of the formula:--OC(O)R.sub.8 in which R.sub.8 represents a C.sub.1 -C.sub.4 alkyl radicala radical of the formula:--OC(O)NHR.sub.9 in which R.sub.9 represents a straight or branched C.sub.1 -C.sub.4 alkyl group, or a phenyl groupmay assume values from 2 to 4.as well as the therapeutically acceptable organic or inorganic salts of these molecules. The compounds are useful in the treatment of respiratory disorders.
    • PCT No.PCT / FR90 / 00752 Sec。 371日期1991年6月17日 102(e)日期1991年6月17日PCT提交1990年10月17日PCT公布。 第WO91 / 05772号公报 日期:1991年5月2日。对应于通式I的1,2-二氢-2-氧代喹喔啉的新衍生物:其中:R为氢或卤素原子,R 1为氢原子或直链或支链C1 -C4烷基R2是:氢原子,C(O)R4基,其中R4是直链或支链C1-C4烷基,C(O)NHR5基,其中R5是直链或支链C1-C4烷基 或苯基A是C1-C4碱基链R3表示:氢原子,C1-C4烷基,C3-C6环烷基,烷酰基,腈,羟基,甲酰氨基,吡啶基,苯基或苯基 被卤素原子取代的基团,C 1 -C 4烷基,C 1 -C 4烷氧基或硝基,下式的链烯基:其中R 6,R 7可以彼此独立地为氢原子 ,C 1 -C 4烷基,苯基或烷氧基羰基,式-OC(O)R 8基团,其中R 8表示C 1 -C 4烷基,式:-OC(O)NHR 9基团在 其中R 9表示直链或支链C 1 -C 4烷基,或苯基可以为2至4的值,以及这些分子的治疗上可接受的有机或无机盐。 该化合物可用于治疗呼吸系统疾病。