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    • 2. 发明授权
    • Sulphonamide derivatives
    • 磺酰胺衍生物
    • US5258399A
    • 1993-11-02
    • US995009
    • 1992-12-22
    • David Waterson
    • David Waterson
    • C07D309/16C07D405/12A61K31/40A61K31/405C07D209/04C07D401/00
    • C07D405/12C07D309/16
    • The invention concerns sulphonamide derivatives of the formula I ##STR1## wherein R.sup.1 includes (1-4C)alkyl; R.sup.2 and R.sup.3 together form --A.sup.2 --X.sup.2 --A.sup.3 --which defines a ring having 5 to 7 ring atoms, wherein A.sup.2 and A.sup.3 each is (1-3C)alkylene and X.sup.2 is oxy, thio, sulphinyl or sulphonyl;A.sup.1 is a direct link to X.sup.1 or is (1-3C)alkylene;X.sup.1 is oxy, thio, sulphinyl, sulphonyl or imino;Ar is optionally substituted phenylene or Ar is pyridylene;Q is nitrogen or of the formula CR.sup.7, wherein R.sup.7 includes hydrogen, halogeno, (1-4C)alkyl and (1-4C)alkoxy;each of R.sup.4 and R.sup.5 is (1-4C)alkyl, (3-4C)alkenyl, (3-4C)alkynyl or optionally substituted phenyl, benzyl or pyridyl, or R.sup.5 may be hydrogen; andR.sup.6 has any of the meanings defined for R.sup.7 ;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的磺酰胺衍生物,其中R 1包括(1-4C)烷基; R2和R3一起形成-A2-X2-A3,其定义具有5至7个环原子的环,其中A 2和A 3各自为(1-3C)亚烷基,X 2为氧基,硫基,亚磺酰基或磺酰基; A1是直接连接到X1或是(1-3C)亚烷基; X1是氧基,硫基,亚磺酰基,磺酰基或亚氨基; Ar是任选取代的亚苯基或Ar是亚吡啶基; Q是氮或式CR7,其中R7包括氢,卤代,(1-4C)烷基和(1-4C)烷氧基; R4和R5各自为(1-4C)烷基,(3-4C)烯基,(3-4C)炔基或任选取代的苯基,苄基或吡啶基,或R5可以是氢; 并且R6具有R7定义的任何含义; 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。