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    • 98. 发明公开
    • Fumagillol derivatives
    • 马洁林衍。
    • EP0359036A1
    • 1990-03-21
    • EP89116052.5
    • 1989-08-31
    • Takeda Chemical Industries, Ltd.
    • Kishimoto, ShojiFujita, Takeshi
    • C07D303/22C07D303/28C07D303/36C07D405/12C07D417/12
    • C07D303/22A61K31/335A61K31/336C07D231/12C07D233/56C07D249/08C07D303/28C07D405/14C07D407/14C07D417/14
    • The present invention is related to a compound of the formula
      wherein R' is a 2-methyl-1-propenyl or isobutyl group which may be substituted and R 2 is (1) a substituted alkanoyl group, (2) a substituted aroyl group having at least one substituent selected from the group consisting of C 2 - 6 alkyl, amino, halogen, hydroxyl, lower alkoxy, cyano, carbamoyl and carboxyl, (3) an aromatic heterocycle-carbonyl, which may optionally be substituted, (4) a carbamoyl group, which may optionally be substituted, (5) an alkyl group, which may optionally be substituted, (6) a benzenesulfonyl group, which may optionally be substituted, (7) an alkylsulfonyl group, which may optionally be substituted, (8) a sulfamoyl group, which may optionally be substituted, (9) an alkoxycarbonyl group, which may optionally be substituted or (10) a phenoxycarbonyl group, which may optionally be substituted; or a salt thereof.
      The compound (I) has a strong angiogenesis inhibitory activity.
    • 本发明涉及式CHEM的化合物,其中R 1是可被取代的2-甲基-1-丙烯基或异丁基,R 2是(1)取代的烷酰基( 2)具有至少一个选自C 2-6烷基,氨基,卤素,羟基,低级烷氧基,氰基,氨基甲酰基和羧基的取代基的取代的芳酰基,(3)芳族杂环羰基,其可任选地为 (4)可任选被取代的氨基甲酰基,(5)可任选被取代的烷基,(6)可任选被取代的苯磺酰基,(7)烷基磺酰基,其可以 (8)可以任选被取代的氨磺酰基,(9)可任选被取代的烷氧基羰基,或可任意被取代的(10)苯氧基羰基; 或其盐。 化合物(I)具有强的血管生成抑制活性。