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    • 5. 发明授权
    • Antihypertensive 7-trifluoromethyl-4-aminoquinolones
    • 抗高血压7-三氟甲基-4-氨基喹诺酮类
    • US4166853A
    • 1979-09-04
    • US903088
    • 1978-05-05
    • John M. McCall
    • John M. McCall
    • A61K31/4427A61K31/445A61P9/12C07D401/12C07D401/14A61K31/47C07D215/44
    • C07D401/14C07D401/12
    • Antihypertensive compounds of the formula II ##STR1## wherein D is a piperidino or 1,2,5,6-tetrahydropyridino ring; wherein X is chloro or trifluoromethyl; wherein R.sub.1 is hydrogen or hydroxy when the D ring is piperidino, or nothing when the D ring is 1,2,5,6-tetrahydropyridino; and, wherein the moiety Ar is 2-oxo-1-benzimidazolinyl, phenyl, or phenyl substituted by one or two halo, trifluoromethyl, or alkyl, alkoxy, in which the carbon moieties are of 1 to 3 carbon atoms, inclusive, and halo is chloro, bromo, or fluoro, are produced by reacting 4-[[7-(chloro) or (trifluoromethyl)-4-quinolinyl]-amino]benzoic acid with thionyl chloride or a carbonyl diimidazole and subsequent reaction with the selected substituted piperidine or 1,2,5,6-tetrahydropyridine.The pharmacologically acceptable acid addition salts of II can also be used as antihypertensives.
    • 式II的抗高血压化合物其中D是哌啶子基或1,2,5,6-四氢吡啶并环; 其中X是氯或三氟甲基; 当D环为哌啶子基时,其中R 1为氢或羟基,或当D环为1,2,5,6-四氢吡啶子基时,R 1为无。 其中所述部分Ar为2-氧代-1-苯并咪唑啉基,苯基或被一个或两个卤素,三氟甲基或烷基,烷氧基取代的苯基,其中碳部分为1至3个碳原子,包括端基和卤素 是通过使4 - [[7-(氯)或(三氟甲基)-4-喹啉基] - 氨基]苯甲酸与亚硫酰氯或羰基二咪唑反应制备的,随后与选择的取代的哌啶 或1,2,5,6-四氢吡啶。