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JP2013521281A5
JP2013521281A5 JP2012556056A JP2012556056A JP2013521281A5 JP 2013521281 A5 JP2013521281 A5 JP 2013521281A5 JP 2012556056 A JP2012556056 A JP 2012556056A JP 2012556056 A JP2012556056 A JP 2012556056A JP 2013521281 A5 JP2013521281 A5 JP 2013521281A5
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  1. 下記の構造式(II)で表される化合物。
    Figure 2013521281
    式中、B環は、
    Figure 2013521281
    であり、
    、R、R、R、R、およびRは、互いに独立して、水素、O−アルキル、O−ハロアルキル、F、Cl、Br、I、ハロアルキル、CF、CN、−CHCN、NH、ヒドロキシル、−(CHNHCH、−(CHNH、−(CHN(CH、−OC(O)CF、炭素数1〜5の直鎖もしくは分岐鎖のアルキル、ハロアルキル、アルキルアミノ、アミノアルキル、−OCHPh、−NHCO−アルキル、COOH、−C(O)Ph、C(O)O−アルキル、C(O)H、−C(O)NH、またはNOであり;
    10およびR11は、互いに独立して、水素、O−アルキル、O−ハロアルキル、F、Cl、Br、I、ハロアルキル、CF、CN、−CHCN、NH、ヒドロキシル、−(CHNHCH、−(CHNH、−(CHN(CH、−OC(O)CF、炭素数1〜5の直鎖もしくは分岐鎖のアルキル、ハロアルキル、アルキルアミノ、アミノアルキル、−OCHPh、−NHCO−アルキル、COOH、−C(O)Ph、C(O)O−アルキル、C(O)H、−C(O)NH、またはNOであり;
    Xは、単結合、炭素数1〜5の炭化水素、またはOであり;
    Yは、単結合、−C=O、−C=S、−C=N−NH、−C=N−OH、−CH−OH、−C=CH−CN、−C=N−CN、−CH=CH−、−C=C(CH、−C=N−OMe、−(C=O)−NH、−NH−(C=O)、-(C=O)−O、−O−(C=O)、−(CH1−5−(C=O)、(C=O)−(CH1−5、−(SO)−NH−、−NH−(SO)−、SO、SO、またはSであり;
    iは、0〜5の整数であり;
    lは、1〜2の整数であり;
    nは、1〜3の整数であり;
    mは、1〜3の整数である。
  2. 請求項1に記載の化合物であって、
    下記の構造式Vで表される化合物であることを特徴とする化合物。
    Figure 2013521281
    式中、B環は、
    Figure 2013521281
    であり、
    、R、およびRは、互いに独立して、水素、O−アルキル、O−ハロアルキル、F、Cl、Br、I、ハロアルキル、CF、CN、−CHCN、NH、ヒドロキシル、−(CHNHCH、−(CHNH、−(CHN(CH、−OC(O)CF、炭素数1〜5の直鎖もしくは分岐鎖のアルキル、ハロアルキル、アルキルアミノ、アミノアルキル、−OCHPh、−NHCO−アルキル、COOH、−C(O)Ph、C(O)O−アルキル、C(O)H、−C(O)NH、またはNOであり;
    nは、1〜3の整数である。
  3. 請求項1に記載の化合物であって、
    下記の構造式XVIで表される化合物であることを特徴とする化合物。
    Figure 2013521281
    式中、RおよびRは、互いに独立して、H、O−アルキル、I、Br、Cl、F、アルキル、ハロアルキル、アミノアルキル、−(CHNHCH、−(CHNH、−(CHN(CH、OCHPh、OH、CN、NO、−NHCO−アルキル、COOH、C(O)O−アルキル、またはC(O)Hであり;
    は、I、Br、Cl、またはFであり;
    iは、0〜5の整数であり;
    nは、1〜4である。
  4. 請求項3に記載の化合物であって、
    前記RまたはClであることを特徴とする化合物。
  5. 請求項3に記載の化合物であって、
    前記RClまたはOCH であることを特徴とする化合物。
  6. 請求項3に記載の化合物であって、
    前記Rが水素であることを特徴とする化合物。
  7. 請求項に記載の化合物であって、
    2−(4−クロロフェニル)−1H−イミダゾール−4−イル)(3,4,5−トリメトキシフェニル)メタノン(12fa)
    Figure 2013521281
    2−(p−トリル)−1H−イミダゾール−4−イル)(3,4,5−トリメトキシフェニル)メタノン(12da)
    Figure 2013521281
    2−(4−ブロモフェニル)−1H−イミダゾール−4−イル)(3,4,5−トリメトキシフェニル)メタノン(34)
    Figure 2013521281
    または、(1−メチル−2−(p−トリル)−1H−イミダゾール−4−イル)(3,4,5−トリメトキシフェニル)メタノン(12dab)
    Figure 2013521281
    であることを特徴とする化合物。
  8. 請求項1〜のいずれかに記載の化合物、またはその異性体、薬学的に許容される塩、医薬品、互変異性体、水和物、N−酸化物あるいはそれらの組み合わせ。
  9. 請求項に記載の化合物および薬学的に許容される担体を含む医薬組成物。
  10. 請求項に記載の化合物を、癌の処置に有効な条件の下で癌を患う被検体に投与することを含む、癌の処置、抑制、重症度軽減、リスク軽減、または阻害の方法。
  11. 請求項10に記載の方法であって、
    前記癌が、前立腺癌、乳癌、卵巣癌、皮膚癌、メラノーマ、肺癌、大腸癌、白血病、腎臓癌、CNS癌、およびそれらの組み合わせからなる群から選択されることを特徴とする方法。
  12. 請求項11に記載の方法であって、
    前記癌がメラノーマ癌転移性メラノーマ癌、前立腺癌または卵巣癌であることを特徴とする方法。
  13. 請求項10に記載の方法であって、
    前記投与が別の癌治療との併用で行われることを特徴とする方法。
  14. 請求項に記載の化合物を、薬剤耐性腫瘍の処置に有効な条件の下で癌を患う被検体に投与することを含む、薬剤耐性腫瘍を処置する方法。
  15. 請求項14に記載の方法であって、
    前記腫瘍がメラノーマ癌腫瘍転移性メラノーマ腫瘍、前立腺癌腫または卵巣癌腫瘍であることを特徴とする方法。
  16. 請求項14に記載の方法であって、
    前記投与が別の癌治療との併用で行われることを特徴とする方法。
  17. 請求項に記載の化合物を提供すること、および癌細胞の死滅に有効な条件の下で癌細胞を化合物に接触させることを含む、癌性細胞を破壊する方法。
JP2012556056A 2010-03-01 2010-12-29 癌を処置するための化合物 Expired - Fee Related JP5879273B2 (ja)

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US30936010P 2010-03-01 2010-03-01
US61/309,360 2010-03-01
US31579010P 2010-03-19 2010-03-19
US61/315,790 2010-03-19
US37667510P 2010-08-24 2010-08-24
US61/376,675 2010-08-24
PCT/US2010/062418 WO2011109059A1 (en) 2010-03-01 2010-12-29 Compounds for treatment of cancer

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