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    • 9. 发明申请
    • COMPOUNDS
    • 化合物
    • WO1997020815A1
    • 1997-06-12
    • PCT/SE1996001595
    • 1996-12-04
    • ASTRA PHARMACEUTICALS LTD.ASTRA AKTIEBOLAGCHESHIRE, DavidCLADINGBOEL, DavidHARDERN, DavidSTOCKS, Michael
    • ASTRA PHARMACEUTICALS LTD.ASTRA AKTIEBOLAG
    • C07D213/28
    • C07D213/30C07D213/32C07D417/12
    • A compound of formula (I), wherein X represents (CH2)nO, (CH2)nS or C2 alkylene; n represents 1 or 2; Ar represents indanyl, tetrahydronaphthyl, naphthyl or phenyl, which latter two groups may be substituted by one or more substituents selected from chloro, fluoro, OR , O(CH2)mCONR R , C(O)R , C1-6 alkyl (optionally substituted by one or more fluorine atoms), pyridyl, thiazinyl, phenyl or C7-9 alkylphenyl which latter two groups are optionally substituted by one or more substituent selected from halo, nitro, OR , C1-6alkyl (optionally substituted by one or more fluorine atoms), C(O)R , C(O)OR , C(O)N(R )R , CN, CH2OR , CH2NR R , N(R )R , N(R )SO2R , N(R )C(O)R , OC(O)R and SO2NR R ; m represents an integer 1 to 3; R , R and R independently represent H, C1-10 alkyl (optionally substituted by one or more fluorine atoms), C7-9 alkylphenyl or phenyl, which latter group is optionally substituted by hydroxy; and R , R , R , R , R , R , R , R , R , R , R , R , R , R , R , R , R and R independently represent H, C1-6 alkyl (optionally substituted by one or more fluorine atoms) or phenyl; in which any alkyl group represent may be interrupted by one or more oxygen atoms; provided that when X represents CH2CH2, Ar may not represent phenyl or phenyl substituted with one or more substituents OR , in which R represents C1-10 alkyl; or a pharmaceutically acceptable derivative thereof, may be used for the treatment of reversible obstructive airways disease or allergic conditions of the skin, nose and eye.
    • 式(I)的化合物,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; Ar 1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,任选被一个或多个氟原子取代的C 1-6烷基,吡啶基,噻嗪基,苯基或C 7-9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 N,R(R 8)R 9,N(R 10)SO 2 R 11,N(R 12) )C(O)R 13,OC(O)R 19和SO 2 NR 17 R 18; m表示1〜3的整数, R 1,R 2和R 3独立地表示H,任选被一个或多个氟原子取代的C 1-10烷基,C 7-9烷基苯基或苯基,后者基团任选被羟基取代; R 4,R 5,R 6,R 7,R 8,R 9,R 10,R 11,R 12,R 13, R 14,R 15,R 16,R 17,R 18,R 19,R 20和R 21独立地代表H,C 1-6烷基(任选地 被一个或多个氟原子取代)或苯基; 其中任何烷基可以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。