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    • 4. 发明申请
    • THIOAMIDES DERIVATES AND THEIR USE AS INHIBITORS OF HYPER-PROLIFERATIVE CELL GROWTH
    • 噻唑衍生物及其作为高增殖细胞生长抑制剂的用途
    • WO1996033179A1
    • 1996-10-24
    • PCT/US1996005470
    • 1996-04-19
    • SUGEN, INC.TANG, Peng, Cho
    • SUGEN, INC.
    • C07D261/18
    • C07D213/75C07C327/44C07D213/85C07D261/10C07D261/18C07D413/12
    • The present invention features compounds and methods for inhibiting hyper-proliferative cell growth. The compounds and method are preferably used to treat patients having a hyper-proliferative cell disorder. The compounds are preferably of formulas (I.A) and (I.B) wherein T is carbon or nitrogen; if T is carbon m is either 0, 1, 2, 3, 4 or 5; and if T is nitrogen m is either 0, 1, 2, 3 or 4; each X is independently selected from the group consisting of: SH, OH, lower alkyl, lower alkenyl, lower alkoxy, haloalkoxy, halogen, haloalkyl, cyano, sulfonyl-aryl, amino, aminosulfonyl, and NO2; R1 is hydrogen or lower alkyl; R3 is selected from the group consisting of: hydrogen, carboxy, alkoxy, and carbalkoxy; R4 is selected from the group consisting of: alkyl, alkenyl, alkyl-aryl, alkenyl-aryl, and alkynyl-aryl; R5 is hydrogen or a group which is cleavable in vivo; and pharmaceutically acceptable salts thereof.
    • 本发明的特征在于抑制高增殖细胞生长的化合物和方法。 化合物和方法优选用于治疗患有高增殖性细胞病症的患者。 所述化合物优选为式(ⅠA)和(ⅠB),其中T为碳或氮; 如果T是碳,则m为0,1,2,3,4或5; 如果T是氮,则m为0,1,2,3或4; 每个X独立地选自:SH,OH,低级烷基,低级烯基,低级烷氧基,卤代烷氧基,卤素,卤代烷基,氰基,磺酰基 - 芳基,氨基,氨基磺酰基和NO 2; R1是氢或低级烷基; R3选自:氢,羧基,烷氧基和烷氧羰基; R 4选自:烷基,烯基,烷基 - 芳基,烯基 - 芳基和炔基 - 芳基; R5是氢或体内可切割的基团; 及其药学上可接受的盐。