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    NON-SYMMETRICAL BIS-HETEROARYLMETHOXYPHENYLALKYL CARBOXYLATES AS INHIBITORS OF LEUKOTRIENE BIOSYNTHESIS
    5.
    发明申请
    NON-SYMMETRICAL BIS-HETEROARYLMETHOXYPHENYLALKYL CARBOXYLATES AS INHIBITORS OF LEUKOTRIENE BIOSYNTHESIS 审中-公开
    作为紫苏酮生物合成酶的抑制剂的非对称双异吲哚氧基甲基羧酸酯

    公开(公告)号：WO1998004555A1

    公开(公告)日：1998-02-05

    申请号：PCT/US1997012138

    申请日：1997-07-14

    Applicant: ABBOTT LABORATORIES

    Inventor： ABBOTT LABORATORIES ,  BROOKS, Clint, D., W. ,  KOLASA, Teodozyj ,  GUNN, David, E.

    IPC: C07D417/12

    CPC classification number: C07D401/12 ,  C07D215/14 ,  C07D413/12 ,  C07D417/12

    Abstract: Compounds having formula (I) or a pharmaceutically acceptable salt thereof wherein W and Y are independently selected from the group consisting of (a) quinolyl; (b) quinolyl substituted with a substituent selected from the group consisting of (b-1) halogen, (b-2) alkyl of one to six carbon atoms, (b-3) haloalkyl of one to six carbon atoms, and (b-4) alkoxy of one to six carbon atoms; (c) benzothiazolyl; (d) benzothiazolyl substituted with a substituent selected from the group consisting of (d-1) halogen, (d-2) alkyl of one to six carbon atoms, (d-3) haloalkyl of one to six carbon atoms, and (d-4) alkoxy of one to six carbon atoms; (e) benzoxazolyl; (f) benzoxazolyl substituted with a substituent selected from the group consisting of (f-1) halogen, (f-2) alkyl of one to six carbon atoms; (g) benzimidazolyl; (h) benzimidazolyl substituted with a substituent selected from the group consisting of (h-1) halogen, (h-2) alkyl of one to six carbon atoms; (i) quinoxalyl; (j) quinoxalyl substituted with a substituent selected from the group consisting of (j-1) halogen, (j-2) alkyl of one to six carbon atoms; (k) naphthyl; (l) naphthyl substituted with a substituent selected from the group consisting of (l-1) halogen, (1-2) alkyl of one to six carbon atoms, (1-3) alkoxy of one to six carbon atoms; with the proviso that W and Y are not simultaneously the same substituent; R and R are independently selected from the group consisting of (a) hydrogen, (b) alkyl of one to six carbon atoms, (c) haloalkyl of one to six carbon atoms, (d) alkoxy of one to six carbon atoms, and (e) halogen; R is selected from the group consisting of (a) hydrogen and (b) alkyl of one to six carbon atoms; X is absent or is selected from the group consisting of (a) alkylene of one to six carbon atoms, (b) alkenylene of one to six carbon atoms, and (c) alkynylene of one to six carbon atoms; and M is selected from the group consisting of (a) a pharmaceutically acceptable metabolically cleavable group, (b) -OR where R is selected from the group consisting of hydrogen and alkyl of one to six carbon atoms, (c) -NR R where R and R are independently selected from the group consisting of hydrogen, alkyl of one to six carbon atoms, hydroxy, and alkoxy of one to six carbon atoms. These compounds inhibit leukotriene biosynthesis and are useful in the treatment of allergic and inflammatory disease states.

    Abstract translation: 具有式（I）的化合物或其药学上可接受的盐，其中W和Y独立地选自（a）喹啉基; （b）被选自（b-1）卤素，（b-2）1至6个碳原子的烷基，（b-3）1-6个碳原子的卤代烷基取代的喹啉基和（b -4）1至6个碳原子的烷氧基; （c）苯并噻唑基; （d）被选自（d-1）卤素，（c-2）1-6个碳原子的烷基，（d-3）1-6个碳原子的卤代烷基取代的苯并噻唑基和（d -4）1至6个碳原子的烷氧基; （e）苯并恶唑基; （f）被选自（f-1）卤素，（c-2）1-6个碳原子的（f-2）烷基的取代基取代的苯并恶唑; （g）苯并咪唑基; （h）被选自（h-1）卤素，1至6个碳原子的（h-2）烷基的取代基取代的苯并咪唑基; （i）喹喔啉; （j）被选自（j-1）卤素，具有1至6个碳原子的（j-2）烷基）的取代基取代的喹喔啉基; （k）萘基; （I）被选自（I-1）卤素，（1-2）1-6个碳原子的烷基，（1-3）1-6个碳原子的烷氧基的取代基取代的萘基; 条件是W和Y不是同一个取代基; R 1和R 2独立地选自（a）氢，（b）1至6个碳原子的烷基，（c）1至6个碳原子的卤代烷基，（d）一个 至（6）个碳原子，（e）卤素; R 3选自（a）氢和（b）1至6个碳原子的烷基; X不存在或选自（a）1至6个碳原子的亚烷基，（b）1至6个碳原子的亚烯基和（c）1至6个碳原子的亚炔基; 并且M选自（a）药学上可接受的代谢可裂解基团，（b）-OR 4，其中R 4选自氢和1至6个碳原子的烷基（ c）-NR 5 R 6其中R 5和R 6独立地选自氢，1至6个碳原子的烷基，羟基和1至6个碳原子的烷氧基。 这些化合物抑制白细胞三烯生物合成，并且可用于治疗过敏性和炎性疾病状态。

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