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    • 1. 发明申请
    • OXIME ETHER DERIVATIVES HAVING LIPOXYGENASE INHIBITORY ACTIVITY
    • 具有LIPOXYGENASE抑制活性的OXIME醚衍生物
    • WO1994014762A1
    • 1994-07-07
    • PCT/US1993012152
    • 1993-12-14
    • ABBOTT LABORATORIESBROOKS, Dee, W.STEWART, Andrew, O.MAKI, Robert, G.
    • ABBOTT LABORATORIES
    • C07C259/06
    • C07D207/335C07C275/64C07D307/58C07D333/22C07D333/58
    • The present invention provides certain substituted oxime ether compounds which inhibit lipoxygenase enzyme activity and are useful in the treatment of allergic and inflammatory disease states. The compounds of this invention have structure (I) where M is hydrogen, a pharmaceutically acceptable cation, or a pharmaceutically acceptable metabolically cleavable group; p and q are independently zero or one, with the proviso that (i) p and q may not both be the same; (ii) when p is one and q is zero, R is selected from the group consisting of hydrogen, straight or branched alkyl of from one to twelve carbon atoms, and cycloalkyl of from three to eight carbon atoms; and (iii) when p is zero and q is one, R is selected from the group consisting of hydrogen, alkyl of from one to twelve carbon atoms, cycloalkyl of from three to eight carbon atoms, and -NR1R2. L1 is a direct bond or is selected from the group consisting of alkyl of from one to six carbon atoms, alkylenyl, of from one to six carbon atoms, and alkynyl of from two to six carbon atoms; L2 is a direct bond or is alkyl of from one to six carbon atoms; Z is selected from the group consisting of hydrogen, alkyl of from one to six carbon atoms, and halosubstituted alkyl of from one to six carbon atoms; and A is optionally substituted carbocyclic or heterocyclic aryl, arylalkyl, or aryloxy.
    • 本发明提供某些抑制脂氧合酶活性的取代的肟醚化合物,可用于治疗过敏性和炎性疾病状态。 本发明的化合物具有结构(I),其中M为氢,药学上可接受的阳离子或药学上可接受的代谢裂解基团; p和q独立为零或一个,条件是(i)p和q不能都相同; (ii)当p为1且q为0时,R选自氢,1至12个碳原子的直链或支链烷基和3至8个碳原子的环烷基; 和(iii)当p为0且q为1时,R选自氢,1至12个碳原子的烷基,3至8个碳原子的环烷基和-NR 1 R 2。 L1是直接键或选自1-6个碳原子的烷基,1至6个碳原子的亚烷基,和2至6个碳原子的炔基; L2是直接键或1-6个碳原子的烷基; Z选自氢,1至6个碳原子的烷基和1至6个碳原子的卤代烷基; 并且A是任选取代的碳环或杂环芳基,芳烷基或芳氧基。