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    • 9. 发明授权
    • Oxime derivatives
    • 肟衍生物
    • US5482966A
    • 1996-01-09
    • US240464
    • 1994-06-13
    • Thomas G. C. BirdPatrick Ple
    • Thomas G. C. BirdPatrick Ple
    • A61K31/425A61K31/505A61P29/00A61P37/08A61P43/00C07D239/42C07D307/20C07D309/08C07D309/10C07D317/22C07D405/04C07D409/02C07D409/04C07D409/12C07D417/04C07D417/12A61K31/35A61K31/34
    • C07D405/04C07D307/20C07D309/10C07D317/22C07D409/04C07D417/04
    • The invention concerns oxime derivatives of the formula I ##STR1## wherein R.sup.4 includes hydrogen, carboxy, carbamoyl, amino, cyano, trifluoromethyl, (1-4C)alkylamino, di-(1-4C)alkylamino and (1-4C)alkyl;R.sup.5 includes hydrogen, (1-4C)alkyl, (3-4C)alkenyl, (3-4C)alkynyl, (2-5C)alkanoyl, halogeno-(2-4C)alkyl and hydroxy-(2-4C)alkyl;Ar.sup.1 is phenylene or a heteroaryl diradical;A.sup.1 is a direct link to X.sup.1, or A.sup.1 is (1-4C)alkylene;X.sup.1 is oxy, thio, sulphinyl or sulphonyl;Ar.sup.2 is phenylene or a heteroaryl diradical;R.sup.1 is (1-4C)alkyl, (3-4C)alkenyl or (3-4C)alkynyl; andR.sup.2 and R.sup.3 together form a group of the formula --A.sup.2 --X.sup.2 --A.sup.3 -- which together with the carbon atom to which A.sup.2 and A.sup.3 are attached define a ring having 5 or 6 ring atoms, wherein each of A.sup.2 and A.sup.3 is (1-3C)alkylene and X.sup.2 is oxy, thio, sulphinyl, sulphonyl or imino;or a pharmaceutically-acceptable salt thereof;processes for their manufacture; pharmaceutical compositions containing them and their use as 5-lipoxygenase inhibitors.
    • 本发明涉及式I的肟衍生物,其中R 4包括氢,羧基,氨基甲酰基,氨基,氰基,三氟甲基,(1-4C)烷基氨基,二(1-4C)烷基氨基和(1-4C)烷基 ; R5包括氢,(1-4C)烷基,(3-4C)烯基,(3-4C)炔基,(2-5C)烷酰基,卤代 - (2-4C)烷基和羟基 - (2-4C)烷基; Ar1是亚苯基或杂芳基双基; A1是直接连接到X1,或A1是(1-4C)亚烷基; X1是氧基,硫基,亚磺酰基或磺酰基; Ar 2是亚苯基或杂芳基双基; R1是(1-4C)烷基,(3-4C)烯基或(3-4C)炔基; 并且R2和R3一起形成式-A2-X2-A3-的基团,其与A2和A3所连接的碳原子一起形成具有5或6个环原子的环,其中A2和A3各自为(1 -3C)亚烷基,X 2为氧基,硫基,亚磺酰基,磺酰基或亚氨基; 或其药学上可接受的盐; 制造过程; 含有它们的药物组合物及其作为5-脂肪氧合酶抑制剂的用途。