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    • 13. 发明授权
    • Compounds
    • 化合物
    • US5977105A
    • 1999-11-02
    • US793918
    • 1997-03-03
    • David CheshireDavid CladingboelDavid HardernMichael Stocks
    • David CheshireDavid CladingboelDavid HardernMichael Stocks
    • A61K20060101A61K31/00A61K31/44A61P11/00A61P11/08A61P37/00A61P37/08C07D20060101C07D213/30C07D213/32C07D417/12A01N43/66C07D211/70C07D211/72
    • C07D213/30C07D213/32C07D417/12
    • A compound of formula I, ##STR1## wherein--X represents (CH.sub.2).sub.n O, (CH.sub.2).sub.n S or C.sub.2 alkylene;n represents 1 or 2;Ar.sup.1 represents indanyl, tetrahydronaphthyl, naphthyl or phenyl, which latter two groups may be substituted by one or more substituents selected from chloro, fluoro, OR.sup.1, O(CH.sub.2).sub.m CONR.sup.20 R.sup.21, C(O)R.sup.2, C.sub.1-6 alkyl (optionally substituted by one or more fluorine atoms), pyridyl, thiazinyl, phenyl or C.sub.7-9 alkylphenyl which latter two groups are optionally substituted by one or more substituent selected from halo, nitro, OR.sup.3, C.sub.1-6 alkyl (optionally substituted by one or more fluorine atoms), C(O)R.sup.4, C(O)OR.sup.5, C(O)N(R.sup.6)R.sup.7, CN, CH.sub.2 OR.sup.14, CH.sub.2 NR.sup.15 R.sup.16, N(R.sup.8)R.sup.9, N(R.sup.10)SO.sub.2 R.sup.11, N(R.sup.12)C(O)R.sup.13, OC(O)R.sup.19 and SO.sub.2 NR.sup.17 R.sup.18 ;m represents an integer 1 to 3;R.sup.1, R.sup.2 and R.sup.3 independently represent H, C.sub.1-10 alkyl (optionally substituted by one or more fluorine atoms), C.sub.7-9 alkylphenyl or phenyl, which latter group is optionally substituted by hydroxy; andR.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, R.sup.9, R.sup.10, R.sup.11, R.sup.12, R.sup.13, R.sup.14, R.sup.15, R.sup.16, R.sup.17, R.sup.18, R.sup.19, R.sup.20 and R.sup.21 independently represent H, C.sub.1-6 alkyl (optionally substituted by one or more fluorine atoms) or phenyl;in which any alkyl group present may be interrupted by one or more oxygen atoms;provided that when X represents CH.sub.2 CH.sub.2, Ar.sup.1 may not represent phenyl or phenyl substituted with one or more substituents OR.sup.1, in which R.sup.1 represents C.sub.1-10 alkyl;or a pharmaceutically acceptable derivative thereof, may be used for the treatment of a reversible obstructive airways disease or allergic conditions of the skin, nose and eye.
    • PCT No.PCT / SE96 / 01595 Sec。 371日期1997年3月3日 102(e)1997年3月3日PCT 1996年12月4日PCT PCT。 出版物WO97 / 20815 日期:1997年6月12日一种式I化合物,其中-X表示(CH 2)n O,(CH 2)n S或C 2亚烷基; n表示1或2; Ar1表示茚满基,四氢萘基,萘基或苯基,后两个基团可以被一个或多个选自氯,氟,OR 1,O(CH 2)m CONR 20 R 21,C(O)R 2,C 1-6烷基(任选地被 一个或多个氟原子),吡啶基,噻嗪基,苯基或C7-9烷基苯基,后两个基团任选被一个或多个选自卤素,硝基,OR 3,C 1-6烷基(任选被一个或多个氟原子取代) ),C(O)R 4,C(O)OR 5,C(O)N(R 6)R 7,CN,CH 2 OR 14,CH 2 NR 15 R 16,N(R 8)R 9,N(R 10)SO 2 R 11,N(R 12) R13,OC(O)R19和SO2NR17R18; m表示1〜3的整数, R1,R2和R3独立地表示H,C1-10烷基(任选被一个或多个氟原子取代),C7-9烷基苯基或苯基,后一个基团任选被羟基取代; 并且R4,R5,R6,R7,R8,R9,R10,R11,R12,R13,R14,R15,R16,R17,R18,R19,R20和R21独立地表示H,C1-6烷基(任选被一个或 更多的氟原子)或苯基; 其中存在的任何烷基可被一个或多个氧原子中断; 条件是当X表示CH 2 CH 2时,Ar 1可以不表示被一个或多个取代基OR 1取代的苯基或苯基,其中R 1表示C 1-10烷基; 或其药学上可接受的衍生物可用于治疗可逆性阻塞性气道疾病或皮肤,鼻子和眼睛的过敏状况。