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    • 5. 发明授权
    • 3-amin3-arylpropan-1-ol compounds, their preparation and use
    • 3-氨基-3-芳基丙-1-醇化合物,其制备和用途
    • US06410790B1
    • 2002-06-25
    • US09545371
    • 2000-04-07
    • Bernd SundermannHagen-Heinrich HenniesBabette-Yvonne KoegelHelmut Buschmann
    • Bernd SundermannHagen-Heinrich HenniesBabette-Yvonne KoegelHelmut Buschmann
    • C07C21100
    • C07D295/096C07C215/28C07C215/42C07C215/64C07C215/70C07C217/74C07C229/38C07C255/59C07C323/32C07C2601/14C07D307/52C07D317/58C07D333/20
    • 3-amino-3-arylpropan-1-ol compounds of formula I: R1 and R2 independently denoting C1-6 alkyl, or together denoting a (CH2)2-6 ring optionally substituted by phenyl, R3 denoting C3-6 alkyl, C3-6 cycloalkyl, aryl optionally containing heteroatoms and optionally substituted by R6 to R8, or a substituted C1-3 alkylphenyl of formula XII:  R4 and R5 independently denoting C1-6 alkyl, C3-6 cycloalkyl, phenyl, benzyl, or phenethyl, or together forming a (CH2)3-6 or CH2CH2OCH2CH2 ring, R6 to R8 independently denoting H, F, Cl, Br, CHF2, CF3, OH, OCF3, OR14, NR15R16, SR14, phenyl, SO2CH3, SO2CF3, C1-6 alkyl, CN, COOR14, or CONR15R16, or together forming a OCH2O, OCH2CH2O, CH═CHO, CH═C(CH3)O or (CH2)4 ring, R14 denoting C1-6 alkyl, phenyl, benzyl, or phenethyl, R15 and R16 independently denoting H, C1-6 alkyl, phenyl, benzyl or phenethyl, and A denoting optionally substituted aryl optionally containing heteroatoms, or a diastereomer or enantiomer or pharmaceutically acceptable salt thereof, and their preparation and use in pharmaceutical compositions.
    • 式I的3-氨基-3-芳基丙-1-醇化合物:R 1和R 2独立地表示C 1-6烷基,或一起表示任选被苯基取代的(CH 2)2-6环,R 3表示C 3-6烷基,C 3 -6环烷基,任选含有杂原子并任选被R 6至R 8取代的芳基或式XII的取代的C 1-3烷基苯基:R 4和R 5独立地表示C 1-6烷基,C 3-6环烷基,苯基,苄基或苯乙基,或 一起形成(CH2)3-6或CH2CH2OCH2CH2环,R6至R8独立地表示H,F,Cl,Br,CHF2,CF3,OH,OCF3,OR14,NR15R16,SR14,苯基,SO2CH3,SO2CF3,C1-6烷基 ,CN,COOR 14或CONR 15 R 16,或一起形成OCH 2 O,OCH 2 CH 2 O,CH = CHO,CH = C(CH 3)O或(CH 2)4环,R 14表示C 1-6烷基,苯基,苄基或苯乙基,R 15和 R16独立地表示H,C 1-6烷基,苯基,苄基或苯乙基,A表示任选地含有杂原子的任选取代的芳基,或其非对映异构体或对映异构体或其药学上可接受的盐, 在药物组合物中的应用和用途。