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    • 10. 发明授权
    • Pharmaceutical pyridine compounds
    • 药物吡啶化合物
    • US5643914A
    • 1997-07-01
    • US356358
    • 1994-12-19
    • Robert A. Daines
    • Robert A. Daines
    • C07D213/65A61K31/435A61K31/44C07D211/72C07D401/00
    • C07D213/65
    • This invention relates to a compound of formula 1 ##STR1## or an N-oxide, or a pharmaceutically acceptable salt, where A is CH.sub.2 and Z is S(O).sub.q where q is 0, 1 or 2, CH.sub.2, CHOH, CO, NR.sub.x, or O, orA is C.dbd.O and Z is NR.sub.x ;m is 0-5;R.sub.x is hydrogen or lower alkyl;R is C.sub.1 to C.sub.20 -aliphatic, unsubstituted or substituted five-membered heteroaryl-C.sub.1 to C.sub.10 -aliphatic-O--, unsubstituted or substituted phenyl-C.sub.1 to C.sub.10 -aliphatic where substituted p from the group consisting of lower alkoxy, lower alkyl, trihalomethyl, and halo, or R is C.sub.1 to C.sub.20 -aliphatic-O--, or R is unsubstituted or substituted phenyl-C.sub.1 to C.sub.10 -aliphatic-O-- where substituted phenyl has one or more radicals selected from the group consisting of lower alkoxy, lower alkyl, trihalomethyl, and halo;R.sub.1 is R.sub.4, --(C.sub.1 to C.sub.5 aliphatic)R.sub.4, --(C.sub.1 to C.sub.5 aliphatic)CHO, --(C.sub.1 to C.sub.5 aliphatic)CH.sub.2 OR.sub.5;R.sub.2 and R.sub.3 are independently, halo, lower alkoxy, CF.sub.3, CN, or lower alkyl;R.sub.4 is tetrazol-5-yl or COOH or an ester or amide thereof; andR.sub.5 is H, lower alkyl, CH.sub.3 (CH.sub.2).sub.0-6 CO or phenyl(CH.sub.2).sub.0-3 CO.This compound is leukotriene antangonist and can be used in treating various diseases associated with leukotrienes.
    • PCT No.PCT / US93 / 06234。 371日期1994年12月19日第 102(e)1994年12月19日日期PCT 1993年6月30日PCT公布。 公开号WO94 / 00437 日本1994年1月6日本发明涉及式1化合物或式I化合物或N-氧化物或其药学上可接受的盐,其中A为CH 2且Z为S(O)q,其中q为0,1或 2,CH 2,CHOH,CO,NR x或O,或A是C = O,Z是NR x; m为0-5; Rx是氢或低级烷基; R是C1至C20脂族,未取代或取代的五元杂芳基-C1至C10-脂族-O-,未取代或取代的苯基-C1至C10-脂族基,其中取代的p由低级烷氧基,低级烷基,三卤甲基 和卤素,或R为C1至C20脂族-O-,或R为未取代或取代的苯基-C1至C10-脂族-O-,其中取代的苯基具有一个或多个选自下列的基团:低级烷氧基,低级 烷基,三卤代甲基和卤素; R1是R4, - (C1〜C5脂肪族)R4, - (C1〜C5脂肪族)CHO, - (C1〜C5脂肪族)CH2OR5; R2和R3独立地为卤素,低级烷氧基,CF3,CN或低级烷基; R 4是四唑-5-基或COOH或其酯或酰胺; 并且R 5是H,低级烷基,CH 3(CH 2)0-6CO或苯基(CH 2)0-3CO。 该化合物为白三烯抗体,可用于治疗与白细胞三烯相关的各种疾病。