JP2014520888A5 - - Google Patents

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JP2014520888A5
JP2014520888A5 JP2014521731A JP2014521731A JP2014520888A5 JP 2014520888 A5 JP2014520888 A5 JP 2014520888A5 JP 2014521731 A JP2014521731 A JP 2014521731A JP 2014521731 A JP2014521731 A JP 2014521731A JP 2014520888 A5 JP2014520888 A5 JP 2014520888A5
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  1. 式(I)の化合物、又はそのエナンチオマー、エナンチオマーの混合物、もしくは2以上のジアステレオマーの混合物、或いはその医薬として許容し得るその形態:
    Figure 2014520888
    (式中、
    Cyは、0〜1回出現するR3及び0〜3回出現するR5で置換されたアリール又はヘテロアリールであり;
    Wb 5は、CR8、CHR8、又はNであり;
    ここで、Wb 5がNであるとき、X又はYのうちの1以下が非存在であり;
    R8は、水素、アルキル、アルケニル、アルキニル、シクロアルキル、ヘテロアルキル、アルコキシ、アミド、アミノ、アシル、アシルオキシ、スルホンアミド、ハロ、シアノ、ヒドロキシル、又はニトロであり;
    Bは、その各々が0〜4回出現するR2で置換されている、アルキル、アミノ、ヘテロアルキル、シクロアルキル、ヘテロシクリル、ヘテロシクリルアルキル、アリール、又はヘテロアリールであり;
    各々のR2は、独立に、アルキル、ヘテロアルキル、アルケニル、アルキニル、シクロアルキル、ヘテロシクリル、アリール、アリールアルキル、ヘテロアリール、ヘテロアリールアルキル、アルコキシ、アミド、アミノ、アシル、アシルオキシ、アルコキシカルボニル、スルホンアミド、ハロ、シアノ、ヒドロキシル、ニトロ、ホスフェート、尿素、又はカルボネートであり;
    Xは、非存在であるか、又は-(CH(R9))z-であり;
    Yは、非存在、-O-、-S-、-S(=O)-、-S(=O)2-、-N(R9)-、-C(=O)-(CHR9)z-、-C(=O)-、-N(R9)-C(=O)NH-、又は-N(R9)C(R9)2-であり;
    各々のzは、独立に、1、2、3、又は4の整数であり;
    R3は、アルキル、アルケニル、アルキニル、シクロアルキル、ヘテロシクリル、ハロアルキル、ヘテロアルキル、アルコキシ、アミド、アミノ、アシル、アシルオキシ、スルフィニル、スルホニル、スルホキシド、スルホン、スルホンアミド、ハロ、シアノ、アリール、ヘテロアリール、ヒドロキシル、ニトロ、又は-C(=O)R17であり;ここで、上記の置換基の各々は、0、1、2、又は3個のR13で置換されることができ;
    R17は、水素、ヒドロキシル、又はヘテロシクリルであり;
    各々のR5は、独立に、アルキル、アルケニル、アルキニル、シクロアルキル、ヘテロアルキル、アルコキシ、アミド、アミノ、アシル、アシルオキシ、スルホンアミド、ハロ、シアノ、ヒドロキシル、又はニトロであり;
    各々のR9は、独立に、水素、アルキル、シクロアルキル、ヘテロシクリル、又はヘテロアルキルであり;かつ
    Wdは、
    Figure 2014520888
    であり、
    ここで、X1は、N又はCR10であり;かつ
    各々のR10、R11、R12、及びR13は、独立に、水素、アルキル、ヘテロアルキル、アルケニル、アルキニル、シクロアルキル、ヘテロシクリル、アリール、アリールアルキル、ヘテロアリール、ヘテロアリールアルキル、アルコキシ、ヘテロシクリルオキシ、アミド、アミノ、アシル、アシルオキシ、アルコキシカルボニル、スルホンアミド、ハロ、シアノ、ヒドロキシル、ニトロ、ホスフェート、尿素、カルボネート、オキソ、又はNR'R''であり、ここで、R'及びR''は、窒素と一緒に、環状部分を形成する)。
  2. 各々のR5が、独立に、CH3、OCH3、CF3、又はハロである、請求項1記載の化合物。
  3. 式(XV)の化合物が、式(II)、(IIa)、(IIb)、(IIIa)又は(IIIb)の構造:
    Figure 2014520888
    を有する、請求項1記載の化合物。
  4. R3が、アルキル、アルケニル、アルキニル、アリール、シクロアルキル、ヘテロシクリル、フルオロアルキル、ヘテロアルキル、アルコキシ、アミド、アミノ、アシル、アシルオキシ、スルホンアミド、ハロ、シアノ、ヘテロアリール、ヒドロキシル、又はニトロであり;ここで、上記の置換基の各々は、0、1、2、又は3個のR13で置換されることができる、請求項1〜3のいずれか一項記載の化合物。
  5. R3が、ハロ、アルキル、アルコキシ、又はシクロアルキルである、請求項4記載の化合物。
  6. R3が、CH3、CF3、又はClである、請求項5記載の化合物。
  7. R3が、0、1、2、又は3個のR13で置換された5〜10員ヘテロアリールである、請求項4記載の化合物。
  8. R3が、0、1、2、又は3個のR13で置換された6員ヘテロアリールである、請求項7記載の化合物。
  9. R3が、0、1、2、又は3個のR13で置換されたピリジル又はピリミジルである、請求項8記載の化合物。
  10. 式(IIIb-1)の構造:
    Figure 2014520888
    (式中、X3は、CR13又はNであり;かつpは、0、1、2、又は3である)
    を有する、請求項9記載の化合物。
  11. pが、1又は2である、請求項10記載の化合物。
  12. Bが、その各々が0〜4個のR2で置換されている、アルキル、ヘテロアルキル、シクロアルキル、ヘテロシクリル、アリール、又はヘテロアリールである、請求項1〜11のいずれか一項記載の化合物。
  13. Bがイソオキサゾリルである、請求項12記載の化合物。
  14. Bがイソプロピルである、請求項12記載の化合物。
  15. X1がNである、請求項1〜14のいずれか一項記載の化合物。
  16. R8が水素である、請求項1〜15のいずれか一項記載の化合物。
  17. R9がメチルである、請求項1〜16のいずれか一項記載の化合物。
  18. YがNHである、請求項1〜17のいずれか一項記載の化合物。
  19. 以下のもの:
    Figure 2014520888
    Figure 2014520888
    Figure 2014520888
    Figure 2014520888
    Figure 2014520888
    又はそれらの医薬として許容し得る形態である、請求項1記載の化合物。
  20. 以下のもの:
    Figure 2014520888
    Figure 2014520888
    又はそれらの医薬として許容し得る塩である、請求項1記載の化合物。
  21. 以下のもの:
    Figure 2014520888
    又はその医薬として許容し得る塩である、請求項20記載の化合物。
  22. 以下のもの:
    Figure 2014520888
    又はその医薬として許容し得る塩である、請求項20記載の化合物。
  23. 式(I)の化合物が、式(IVa)、(IVb)、(Va)、(Vb)、(VIa)、(VIb)、(VIIa)、(VIIb)、(VIIIa)、(VIIIb)、(IXa)、又は(IXb)の構造:
    Figure 2014520888
    を有する、請求項1記載の化合物。
  24. R3が、アルキル、シクロアルキル、ハロ、アリール、又はヘテロアリールである、請求項23記載の化合物。
  25. R3が、メチル、クロロ、又はピラゾロである、請求項24記載の化合物。
  26. Bが非置換フェニルである、請求項23〜25のいずれか一項記載の化合物。
  27. 以下のもの:
    Figure 2014520888
    又はそれらの医薬として許容し得る形態である、請求項1記載の化合物。
  28. 式(XI)もしくは(XII)の化合物、又はそのエナンチオマー、エナンチオマーの混合物、もしくは2以上のジアステレオマーの混合物、或いはその医薬として許容し得るその形態:
    Figure 2014520888
    (式中:
    Wb 5は、N、CHR8、又はCR8であり;
    R8は、水素、アルキル、アルケニル、アルキニル、シクロアルキル、ヘテロアルキル、アルコキシ、アミド、アミノ、アシル、アシルオキシ、スルホンアミド、ハロ、シアノ、ヒドロキシル、又はニトロであり;
    Cyは、0〜1回出現するR3及び0〜3回出現するR5で置換されたアリール又はヘテロアリールであり;
    R1は-(L)-R1'であり;
    Lは、結合、-S-、-N(R15)-、-C(=O)-、又は-O-であり;
    R1'は、水素、アルキル、ヘテロアルキル、アルケニル、アルキニル、シクロアルキル、シクロアルキルアルキル、ヘテロシクリル、ヘテロシクリルアルキル、アリール、アリールアルキル、ヘテロアリール、ヘテロアリールアルキル、アルコキシ、ヘテロシクリルオキシ、アミド、アミノ、アシル、アシルオキシ、アルコキシカルボニル、スルホンアミド、ハロ、シアノ、ヒドロキシル、ニトロ、ホスフェート、尿素、カルボネート、置換窒素、又はNR'R''であり、ここで、R'及びR''は、窒素と一緒に、環状部分を形成し;
    各々のR15は、独立に、水素、アルキル、シクロアルキル、又はヘテロアルキルであり;
    R3は、アルキル、アルケニル、アルキニル、シクロアルキル、ヘテロシクリル、フルオロアルキル、ヘテロアルキル、アルコキシ、アミド、アミノ、アシル、アシルオキシ、スルホンアミド、ハロ、シアノ、ヘテロアリール、アリール、ヒドロキシル、又はニトロであり;ここで、上記の置換基の各々は、0、1、2、又は3個のR13で置換されることができ;
    各々のR5は、独立に、アルキル、ヘテロアルキル、アルケニル、アルキニル、シクロアルキル、ヘテロシクリル、アリール、アリールアルキル、ヘテロアリール、ヘテロアリールアルキル、アルコキシ、ヘテロシクリルオキシ、アミド、アミノ、アシル、アシルオキシ、アルコキシカルボニル、スルホンアミド、ハロ、シアノ、ヒドロキシル、ニトロ、ホスフェート、尿素、カルボネート、又はNR'R''であり、ここで、R'及びR''は、窒素と一緒に、環状部分を形成し;
    Xは、非存在であるか、又は-(CH(R16))zであり;
    Yは、非存在、-O-、-S-、-S(=O)-、-S(=O)2-、-N(R16)-、-C(=O)-(CHR16)z-、-C(=O)-、-N(R16)-C(=O)NH-、又は-N(R16)C(R16)2-であり;
    各々のzは、1、2、3、又は4の整数であり;
    各々のR16は、独立に、水素、アルキル、シクロアルキル、ヘテロシクリル、ヘテロアルキル、アリール、ハロ、又はヘテロアリールであり;かつ
    Wdは、
    Figure 2014520888
    であり、
    X1は、N又はCR10であり;
    ここで、R10、R11 R12、及びR13は、独立に、水素、アルキル、ヘテロアルキル、アルケニル、アルキニル、シクロアルキル、ヘテロシクリル、アリール、アリールアルキル、ヘテロアリール、ヘテロアリールアルキル、アルコキシ、ヘテロシクリルオキシ、アミド、アミノ、アシル、アシルオキシ、アルコキシカルボニル、スルホンアミド、ハロ、シアノ、ヒドロキシル、ニトロ、ホスフェート、尿素、カルボネート、オキソ、又はNR'R''であり、ここで、R'及びR''は、窒素と一緒に、環状部分を形成する)。
  29. 請求項1〜28のいずれか一項記載の化合物を含む医薬組成物。
  30. 対象におけるPI3K媒介性障害を治療するための医薬組成物であって、請求項1〜28のいずれか一項記載の化合物を含む、前記医薬組成物。
  31. 前記障害が、癌、炎症性疾患、又は自己免疫疾患である、請求項30記載の医薬組成物。
  32. 前記障害が、癌である、請求項31記載の医薬組成物。
  33. 前記癌が、白血病又はリンパ腫である、請求項32記載の医薬組成物。
  34. 前記白血病が、急性骨髄性白血病(AML)、急性リンパ球性白血病、成人T細胞白血病、慢性リンパ球性白血病(CLL)、有毛細胞白血病、骨髄異形成、骨髄増殖性障害、慢性骨髄性白血病(CML)、多発性骨髄腫(MM)、骨髄異形成症候群(MDS)、ヒトリンパ球向性ウイルス1型(HTLV-1)白血病、肥満細胞症、及び急性リンパ芽球性白血病から選択される、請求項33記載の医薬組成物。
  35. 前記リンパ腫が、びまん性大細胞型B細胞リンパ腫、B細胞免疫芽球性リンパ腫、小型非切れ込み核細胞性リンパ腫、ヒトリンパ球向性ウイルス1型(HTLV-1) 白血病/リンパ腫、成人T細胞リンパ腫、ホジキン病、非ホジキンリンパ腫、AIDS-関連リンパ腫、T細胞リンパ腫、及び多発性骨髄腫から選択される、請求項33記載の医薬組成物。
  36. 前記障害が、炎症性疾患である、請求項31記載の医薬組成物。
  37. 前記炎症性疾患が、喘息、肺気腫、アレルギー、皮膚炎、関節リウマチ、乾癬、エリテマトーデス、移植片対宿主病、炎症性腸疾患、湿疹、強皮症、クローン病、又は多発性硬化症である、請求項36記載の医薬組成物。
  38. 前記障害が、自己免疫疾患である、請求項31記載の医薬組成物。
  39. 前記自己免疫疾患が、関節炎、喘息、アテローム性動脈硬化症、骨粗鬆症、気管支炎、腱炎、滑液包炎、皮膚疾患、遺尿症、好酸球性疾患、胃腸障害、再発性多発性軟骨炎、又は消化管運動促進剤によって改善される障害である、請求項38記載の医薬組成物。
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US201161509441P 2011-07-19 2011-07-19
US61/509,441 2011-07-19
US201261622251P 2012-04-10 2012-04-10
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PCT/US2012/047190 WO2013012918A1 (en) 2011-07-19 2012-07-18 Heterocyclic compounds and uses thereof

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