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    • 7. 发明申请
    • 5- (2-HYDROXYPHENYL) TETRAZOLES AS HSP90 INHIBITORS AGAINST CANCER
    • 5-(2-羟基苯基)四氢叶酸作为HSP90抗癌剂抑制剂
    • WO2009049305A3
    • 2009-07-02
    • PCT/US2008079755
    • 2008-10-14
    • ARQULE INCYANG RUI-YANGALI SYED MASHWELL MARK AKELLEHER EUGENEPALMA ROCIOWESTLUND NEIL
    • YANG RUI-YANGALI SYED MASHWELL MARK AKELLEHER EUGENEPALMA ROCIOWESTLUND NEIL
    • C07D257/04A61K31/41A61P35/00C07D401/10C07D403/04C07D403/10C07D403/12
    • C07D257/04C07D401/10C07D403/04C07D403/10C07D403/12
    • The present invention provides tetrazole compounds, and methods of preparation of these compounds. The present invention also relates to pharmaceutical compositions comprising the tetrazole compounds. The present invention provides methods of treating a cell proliferative disorder, such as a cancer, by administering to a subject in need thereof a therapeutically effective amount of a compound of the present invention, formula (I) wherein: R1 is selected from the group consisting of hydrogen, CH3, F, Cl, Br, and I; R2 is selected from the group consisting of hydrogen, OH, SH, CH3, -CONH2, NHR16, -CH2OH, - CH2SH, and -CH2NH2; R16 is hydrogen, CH3, or C2H3; R3 is selected from the group consisting of hydrogen, F, Cl, Br, I, NO2, CN, -(C1-C6) alkyl, -(C1 -C6) substituted alkyl, C2-C6 alkenyl, (C3-C9) cycloalkyl, (C3-C9) substituted cycloalkyl; -OR8, -NR9R10, -C(=O)-, WR11, -C(=O)-NR12R13, and formula (II); R4 is selected from the group consisting of hydrogen, (C1 -C6) alkyl, (C1-C6) substituted alkyl, (C3-C9) cycloalkyl, (C3-C9) substituted cycloalkyl; aryl, substituted aryl, heteroaryl, substituted heteroaryl, heterocyclyl, substituted heterocyciyl, -OR14, and formula (III). The present invention relates to tetrazole compounds and the use of as HSP90 inhibitors for cancer.
    • 本发明提供了四唑化合物,以及这些化合物的制备方法。 本发明还涉及包含四唑化合物的药物组合物。 本发明提供了通过向有需要的受试者施用治疗有效量的本发明化合物式(I)的式(I)化合物,其中:R1选自下组:治疗细胞增殖性疾病如癌症的方法, 的氢,CH3,F,Cl,Br和I; R 2选自氢,OH,SH,CH 3,-CONH 2,NHR 16,-CH 2 OH,-CH 2 SH和-CH 2 NH 2; R 16是氢,CH 3或C 2 H 3; R3选自氢,F,Cl,Br,I,NO2,CN, - (C1-C6)烷基, - (C1-C6)取代的烷基,C2-C6烯基,(C3-C9) ,(C 3 -C 9)取代的环烷基; -OR8,-NR9R10,-C(= O) - ,WR11,-C(= O)-NR12R13和式(Ⅱ); R4选自氢,(C1-C6)烷基,(C1-C6)取代的烷基,(C3-C9)环烷基,(C3-C9)取代的环烷基; 芳基,取代的芳基,杂芳基,取代的杂芳基,杂环基,取代的杂胞基,-OR14和式(III)。 本发明涉及四唑化合物和作为HSP90抑制剂用于癌症的用途。