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    PYRAZOLE COMPOUNDS THAT MODULATE HSP90 ACTIVITY
    41.
    发明申请
    PYRAZOLE COMPOUNDS THAT MODULATE HSP90 ACTIVITY 审中-公开
    调节HSP90活性的吡咯化合物

    公开(公告)号：US20100069442A1

    公开(公告)日：2010-03-18

    申请号：US12559155

    申请日：2009-09-14

    申请人： Weiwen Ying ,  Shijie Zhang ,  Zhenjian Du ,  Kevin Foley

    发明人： Weiwen Ying ,  Shijie Zhang ,  Zhenjian Du ,  Kevin Foley

    IPC分类号： A61K31/4439 ,  C12N5/00 ,  A61K31/415 ,  A61P35/00

    CPC分类号： C07D231/20 ,  C07D231/18 ,  C07D231/38 ,  C07D403/04

    摘要： Compounds of formula (I), pharmaceutical compositions comprising compounds of formula (I) and methods of inhibiting Hsp90 in a cell, treating or preventing a proliferation disorder in a mammal and treating cancer in a mammal comprising administering a compound of formula (I) to a patient or a cell. Variable R5 is an optionally substituted heteroaryl; an optionally substituted 6 to 14-membered aryl; a bicyclic 9-member heterocycle optionally substituted at any substitutable nitrogen or carbon atoms; or a substituent R18, defined herein. Ring A is an aryl or a heteroaryl optionally further substituted with one or more substituents in addition to R3. Substituent R3 is defined herein.

    摘要翻译： 式（I）化合物，包含式（I）化合物的药物组合物和抑制细胞中Hsp90的方法，治疗或预防哺乳动物中的增殖病症并治疗哺乳动物的癌症，其包括给予式（I）化合物至 患者或细胞。 变量R5是任选取代的杂芳基; 任选取代的6至14元芳基; 任选在任何可取代的氮或碳原子上取代的双环9元杂环; 或本文定义的取代基R18。 环A是除了R3之外任选进一步被一个或多个取代基取代的芳基或杂芳基。 取代基R 3在本文中定义。

    Treatment for cancers
    47.
    发明授权
    Treatment for cancers 失效
    癌症治疗

    公开(公告)号：US07763658B2

    公开(公告)日：2010-07-27

    申请号：US10758589

    申请日：2004-01-15

    申请人： Keizo Koya ,  Lijun Sun ,  Yaming Wu ,  Timothy Korbut ,  Dan Zhou ,  Zhenjian Du ,  Shoujun Chen ,  Noriaki Tatsuta ,  Guiqing Liang ,  Mitsunori Ono

    发明人： Keizo Koya ,  Lijun Sun ,  Yaming Wu ,  Timothy Korbut ,  Dan Zhou ,  Zhenjian Du ,  Shoujun Chen ,  Noriaki Tatsuta ,  Guiqing Liang ,  Mitsunori Ono

    IPC分类号： A61K31/16

    CPC分类号： A61K31/165 ,  A61K31/16 ,  A61K31/277

    摘要： One embodiment of the present invention is a method of treating a subject with a multi-drug resistant cancer. The method comprises administering to the subject an effective amount of a compound represented by Structural Formula (I): Y is a covalent bond or a substituted or unsubstituted straight chained hydrocarbyl group, or, Y, taken together with both >C═Z groups to which it is bonded, is a substituted or unsubstituted aromatic group. R1-R4 are independently —H, an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group, or R1 and R3 taken together with the carbon and nitrogen atoms to which they are bonded, and/or R2 and R4 taken together with the carbon and nitrogen atoms to which they are bonded, form a non-aromatic heterocyclic ring optionally fused to an aromatic ring. Preferably R1 and R2 are the same and R3 and R4 are the same. R5-R6 are independently —H, an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group. Z is ═O or ═S.

    摘要翻译： 本发明的一个实施方案是用多药耐药性癌症治疗受试者的方法。 该方法包括向受试者施用有效量的由结构式（I）表示的化合物：Y是共价键或取代或未取代的直链烃基，或Y与两个> C = Z基团一起加到 其是键合的，是取代或未取代的芳基。 R 1 -R 4独立地为-H，脂族基团，取代的脂族基团，芳基或取代的芳基，或者R 1和R 3与它们所键合的碳原子和氮原子一起，和/或R 2和R 4 与它们所键合的碳原子和氮原子一起形成任选地与芳环稠合的非芳族杂环。 优选地，R 1和R 2相同，并且R 3和R 4相同。 R5-R6独立地是-H，脂族基团，取代的脂族基团，芳基或取代的芳基。 Z为═O或═S。