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    • 59. 发明申请
    • OXIME DERIVATIVES
    • OXIME衍生物
    • WO1994017054A1
    • 1994-08-04
    • PCT/EP1994000186
    • 1994-01-25
    • ZENECA LIMITEDZENECA-PHARMA S.A.LARGE, Michael, Stewart
    • ZENECA LIMITEDZENECA-PHARMA S.A.
    • C07D309/10
    • C07D409/04C07D309/10
    • The invention concerns oxime derivatives of formula (I) wherein R includes hydrogen, carboxy, carbamoyl and (1-4C)alkyl; R includes hydrogen, (1-4C)alkyl, (3-4C)alkenyl, (3-4C)alkynyl, (2-5C)alkanoyl and cyano-(1-4C)alkyl; Ar is optionally-substituted phenylene or a heteroaryl diradical; A is a direct link to X , or A is (1-4C)alkylene; X is oxy, thio, sulphinyl or sulphonyl; Ar includes optionally-substituted phenylene and thiophenediyl; R is hydrogen, (2-5C)alkanoyl or benzoyl; and R and R together form a group of the formula -A -X -A - which together with the carbon atom to which A and A are attached define a ring having 5 or 6 ring atoms, each of A and A is (1-3C)alkylene and X includes oxy; 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,氨基甲酰基和(1-4C)烷基; R 5包括氢,(1-4C)烷基,(3-4C)烯基,(3-4C)炔基,(2-5C)烷酰基和氰基 - (1-4C)烷基; Ar 1是任选取代的亚苯基或杂芳基双基; A 1是与X 1的直接键,或A 1是(1-4C)亚烷基; X 1是氧基,硫基,亚磺酰基或磺酰基; Ar 2包括任选取代的亚苯基和噻吩二基; R 1是氢,(2-5C)烷酰基或苯甲酰基; 并且R 2和R 3一起形成式-A 2 -X 2 -A 3的基团 - 与A 2和A 3的碳原子一起 连接的环是具有5或6个环原子的环,A 2和A 3各自为(1-3C)亚烷基且X 2包括氧; 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。