首页> 外国专利> REPLACED DERIVATIVES OF INDOLIC ACID AS INHIBITORS OF THE INHIBITOR OF THE PLASMINOGEN-1 ACTIVATOR (PAI-1).

REPLACED DERIVATIVES OF INDOLIC ACID AS INHIBITORS OF THE INHIBITOR OF THE PLASMINOGEN-1 ACTIVATOR (PAI-1).

机译:取代的吲哚酸衍生物是纤溶酶原1活化剂(PAI-1)抑制剂的抑制剂。

摘要

Use of a compound of formula (I): in which: X is a chemical bond, -CH2- or -C (O) -; R1 is selected from C1-C8 alkyl, - (CH2) n-C3-C6 cycloalkyl in which n is an integer from 0 to 6, pyridinyl, -CH2-pyridinyl, phenyl and benzyl, the group rings being cycloalkyl, pyridinyl, phenyl and benzyl optionally substituted by 1 to 3 substituents independently selected from halogen, C1-C4 alkyl, C1-C4 perfluoroalkyl, -O-perfluoroalkyl C1-C4, C1-C4 alkoxy, -OH, -NH2, and -NO2; R2 is selected from H, C1-C6 alkyl, C3-C6 cycloalkyl, -CH2-C3-C6 cycloalkyl, C1-C4 perfluoroalkyl, CH2OH and CH2O (CO) CH3; R3 is selected from H, halogen, C1-C6 alkyl, perfluoroalkyl C1-C4, alkoxy C1-C6, cycloalkyl C3-C6, -CH2-cycloalkyl C3-C6, cycloalkenyl C3-C6, -CH2-cycloalkenyl C3-C6, -NH2, and -NO2; R4 is selected from C3-C6 cycloalkyl, -CH2-C3-C6 cycloalkyl, C3-C6 cycloalkenyl, -CH2-C3-C6 cycloalkenyl, phenyl, benzyl, benzyloxy, pyridinyl, and -CH2-pyridinyl, the rings thereof groups optionally substituted by 1 to 3 substituents independently selected from halogen, C1-C4 alkyl, C1-C4 perfluoroalkyl, C1-C4 perfluoroalkyl, C1-C4 alkoxy, -OH, -NH2, -NO2, and (CO ) -C1-C6 alkyl; or a pharmaceutically acceptable salt or ester form thereof, for the preparation of a medicament for the treatment of Alzheimer's disease.
机译:式(I)化合物的用途:其中:X为化学键,-CH 2-或-C(O)-; R1选自C1-C8烷基,-(CH2)n-C3-C6环烷基,其中n为0至6的整数,吡啶基,-CH2-吡啶基,苯基和苄基,基团环为环烷基,吡啶基,苯基苄基,其任选地被1-3个独立地选自卤素,C 1 -C 4烷基,C 1 -C 4全氟烷基,-O-全氟烷基C 1 -C 4,C 1 -C 4烷氧基,-OH,-NH 2和-NO 2的取代基取代。 R2选自H,C1-C6烷基,C3-C6环烷基,-CH2-C3-C6环烷基,C1-C4全氟烷基,CH2OH和CH2O(CO)CH3; R3选自H,卤素,C1-C6烷基,全氟烷基C1-C4,烷氧基C1-C6,环烷基C3-C6,-CH2-环烷基C3-C6,环烯基C3-C6,-CH2-环烯基C3-C6,- NH2和-NO2; R4选自C3-C6环烷基,-CH2-C3-C6环烷基,C3-C6环烯基,-CH2-C3-C6环烯基,苯基,苄基,苄氧基,吡啶基和-CH2-吡啶基,其环基团任选地被取代1-3个独立地选自卤素,C 1 -C 4烷基,C 1 -C 4全氟烷基,C 1 -C 4全氟烷基,C 1 -C 4烷氧基,-OH,-NH 2,-NO 2和(CO)-C 1 -C 6烷基的取代基;或其药学上可接受的盐或酯形式,用于制备治疗阿尔茨海默氏病的药物。

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