Propanolaminomethyltetralines, their preparation and pharmaceutical composition comprising same
    3.
    发明申请
    Propanolaminomethyltetralines, their preparation and pharmaceutical composition comprising same 失效
    丙醇氨基甲基四氢萘酯,其制备方法和包含它们的药物组合物

    公开(公告)号:US20050054641A1

    公开(公告)日:2005-03-10

    申请号:US10497379

    申请日:2002-12-02

    CPC分类号: C07C311/08 C07C2602/10

    摘要: The invention concerns compounds of formula (1), wherein A is a group of formula (a) or (b), wherein: R represents a hydrogen or halogen atom, a —S(O)z(C1-C4)Alk wherein z is 0, 1 or 2, a —NHSO2(C1-C4)Alk, —SO2NH(C1-C4)Alk, —NHSO2—(C1-C4)Alk-phenyl or —NHSO2-phenyl group, said phenyl capable of bearing a halogen atom, a (C1-C4)Alk group or a (C1-C6)alkoxy group; R1 represents a hydrogen atom or a —(C1-C4)Alk, —CO(C1-C4)Alk, —(C1-C4)Alk-phenyl or —CO-phenyl group, said phenyl capable of bearing a halogen atom or a —(C1-C4)Alk or (C1-C6)alkoxy group; R2 is a hydrogen atom, a —SO2(C1-C4)Alk, —SO2—(C1-C4)Alk-phenyl, —SO2-phenyl group, or a —(C1-C4)Alk group; X completes a saturated or unsaturated cycle of 5 to 8 atoms, capable of bearing one or two —(C1-C4)Alk groups and/or two carbonyl groups; R3 and R′3 represent each independently a hydrogen or halogen atom, a —(C1-C6)Alk, hydroxy, —CN, —(C1-C6)alkoxy, —COR4 or Y—CR8R9—COR4 group; Y represents O or CH2; R4 represents a hydroxy, (C1-C6)alkoxy or —NR5R6 group; R5 and R6 independently represent a hydrogen atom, a —(C1-C4)Alk, group, aryl or heteroaryl optionally substituted by a R7 group, aralkyl or heteroaralkyl optionally substituted by a R7 group; or R5 and R6, with the nitrogen atom which bears them, form a saturated or unsaturated cycle of 5 to 7 atoms optionally substituted by a R7 group; and R7 represents a hydrogen or halogen atom, a hydroxy, —(C1-C4)Alk, —(C1-C6)alkoxy, —NH(C1-C4)Alk, —N(C1-C4)Alk2, —COO(C1-C4)Alk, aralkyl or heteroaryl group; R8 and R9 independently represent a hydrogen atom or a —(C1-C4)Alk group; their salts or solvates, the pharmaceutical compositions containing them, a method for preparing them and synthesis intermediates.

    摘要翻译: 本发明涉及式(1)的化合物,其中A是式(a)或(b)的基团,其中:R表示氢或卤素原子,-S(O)z(C1-C4) 是0,1或2,-NHSO 2(C 1 -C 4)Alk,-SO 2 NH(C 1 -C 4)Alk,-NHSO 2 - (C 1 -C 4)烷基 - 苯基或-NHSO 2 - 苯基, 卤素原子,(C1-C4)Alk基或(C1-C6)烷氧基; R1表示氢原子或 - (C1-C4)Alk,-CO(C1-C4)Alk, - (C1-C4)Alk-苯基或-CO-苯基,所述能够带有卤素原子或 - (C1-C4)Alk或(C1-C6)烷氧基; R2是氢原子,-SO2(C1-C4)Alk,-SO2-(C1-C4)烷基 - 苯基,-SO2-苯基或 - (C1-C4) X完成5至8个原子的饱和或不饱和的循环,能承载一个或两个 - (C 1 -C 4)Alk基团和/或两个羰基基团; R 3和R'3各自独立地表示氢或卤素原子,α-(C1-C6)Alk,羟基,-CN, - (C1-C6)烷氧基,-COR4或Y-CR8R9-COR4基团; Y表示O或CH 2; R4表示羟基,(C1-C6)烷氧基或-NR5R6基团; R 5和R 6独立地表示氢原子,任选被R 7取代的 - (C 1 -C 4)Alk,基团,芳基或杂芳基

    Propanolaminomethyltetralines, their preparation and pharmaceutical composition comprising same

    公开(公告)号:US07115780B2

    公开(公告)日:2006-10-03

    申请号:US10497379

    申请日:2002-12-02

    CPC分类号: C07C311/08 C07C2602/10

    摘要: The invention concerns compounds of formula (I), wherein A is a group of formula (a) or (b), wherein: R represents a hydrogen or halogen atom, a —S(O)z(C1–C4)Alk wherein z is 0, 1 or 2, a —NHSO2(C1–C4)Alk, —SO2NH(C1–C4)Alk, —NHSO2—(C1–C4)Alk-phenyl or —NHSO2-phenyl group, said phenyl capable of bearing a halogen atom, a (C1–C4)Alk group or a (C1–C6)alkoxy group; R1 represents a hydrogen atom or a —(C1–C4)Alk, —CO(C1–C4)Alk, —(C1–C4)Alk-phenyl or —CO-phenyl group, said phenyl capable of bearing a halogen atom or a —(C1–C4)Alk or (C1–C6)alkoxy group; R2 is a hydrogen atom, a —SO2(C1–C4)Alk, —SO2—(C1–C4)Alk-phenyl, —SO2-phenyl group, or a —(C1–C4)Alk group; X completes a saturated or unsaturated cycle of 5 to 8 atoms, capable of bearing one or two —(C1–C4)Alk groups and/or two carbonyl groups; R3 and R′3 represent each independently a hydrogen or halogen atom, a —(C1–C6)Alk, hydroxy, —CN, —(C1–C6)alkoxy, —COR4 or Y—CR8R9—COR4 group; Y represents O or CH2; R4 represents a hydroxy, (C1–C6)alkoxy or —NR5R6 group; R5 and R6 independently represent a hydrogen atom, a —(C1–C4)Alk, group, aryl or heteroaryl optionally substituted by a R7 group, aralkyl or heteroaralkyl optionally substituted by a R7 group; or R5 and R6, with the nitrogen atom which bears them, form a saturated or unsaturated cycle of 5 to 7 atoms optionally substituted by a R7 group; and R7 represents a hydrogen or halogen atom, a hydroxy, —(C1–C4)Alk, —(C1–C6)alkoxy, —NH(C1–C4)Alk, —N(C1–C4)Alk2, —COO(C1–C4)Alk, aralkyl or heteroaryl group; R8 and R9 independently represent a hydrogen atom or a —(C1–C4)Alk group; their salts or solvates, the pharmaceutical compositions containing them, a method for preparing them and synthesis intermediates