JP2013504544A5 - - Google Patents

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JP2013504544A5
JP2013504544A5 JP2012528379A JP2012528379A JP2013504544A5 JP 2013504544 A5 JP2013504544 A5 JP 2013504544A5 JP 2012528379 A JP2012528379 A JP 2012528379A JP 2012528379 A JP2012528379 A JP 2012528379A JP 2013504544 A5 JP2013504544 A5 JP 2013504544A5
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  1. 式(I)の化合物、又は、それらの医薬として許容し得る塩、溶媒和物、若しくは、そのすべての互変異性体及び立体異性体を含む多形体：
    Figure 2013504544
     (式中、R1は、ヘテロアリール、-カルボシクリル-ヘテロアリール、-C2-6アルケニルヘテロアリール、-C1-6アルキルヘテロアリール、又は(CH2)aCR5R6(CH2)bヘテロアリールを表し、ここで、a及びbは独立して、0〜5の整数を表し、但し、a＋b＝0〜5であり、かつR5及びR6が、それらの結合する炭素と共にC3-C5シクロアルキル基を形成するアルキレンであり；
    ここで、上記のヘテロアリール基のいずれも、C1-6アルキル、C2-6アルケニル、C2-6アルキニル、C1-6ハロアルキル、-C1-6チオアルキル、-SOC1-4アルキル、-SO2C1-4アルキル、C1-6アルコキシ-、-O-C3-8シクロアルキル、C3-8シクロアルキル、-SO2C3-8シクロアルキル、-SOC3-6シクロアルキル、C3-6アルケニルオキシ-、C3-6アルキニルオキシ-、-C(O)C1-6アルキル、-C(O)OC1-6アルキル、C1-6アルコキシ-C1-6アルキル-、ニトロ、ハロゲン、シアノ、ヒドロキシル、-C(O)OH、-NH2、-NHC1-4アルキル、-N(C1-4アルキル)(C1-4アルキル)、-C(O)N(C1-4アルキル)(C1-4アルキル)、-C(O)NH2、-C(O)NH(C1-4アルキル)、及び-C(O)NH(C3-10シクロアルキル)から選択される1個以上の基によって任意に置換されてもよく；
    かつここで、上記のカルボシクリル基のいずれも、C1-4アルキル、オキソ、ハロゲン、及びC1-4アルコキシから選択される1個以上の基によって任意に置換されてもよく；
    R2は、H、C1-8アルキル、アリール、ヘテロアリール、カルボシクリル、ヘテロシクリル、-C1-4アルキルアリール、-C1-4アルキルヘテロアリール、-C1-4アルキルカルボシクリル、又は-C1-4アルキルヘテロシクリルを表し；
    ここで、上記のアリール基及びヘテロアリール基のいずれも、C1-6アルキル、C2-6アルケニル、C2-6アルキニル、C1-6ハロアルキル、-C1-6チオアルキル、-SOC1-4アルキル、-SO2C1-4アルキル、C1-6アルコキシ-、-O-C3-8シクロアルキル、C3-8シクロアルキル、-SO2C3-8シクロアルキル、-SOC3-6シクロアルキル、C3-6アルケニルオキシ-、C3-6アルキニルオキシ-、-C(O)C1-6アルキル、-C(O)OC1-6アルキル、C1-6アルコキシ-C1-6アルキル-、C1-6アルコキシ-C1-6アルコキシ-、ニトロ、ハロゲン、ハロC1-6アルキル、ハロC1-6アルコキシ、シアノ、ヒドロキシル、-C(O)OH、-NH2、-NHC1-4アルキル、-N(C1-4アルキル)(C1-4アルキル)、-N(C1-4アルキル)(C1-4アルキル)-N(C1-4アルキル)(C1-4アルキル)、-C1-4アルキル-N(C1-4アルキル)(C1-4アルキル)、-C1-4アルコキシ-N(C1-4アルキル)(C1-4アルキル)、-N(C3-8シクロアルキル)(C3-8シクロアルキル)、-N(-C1-6アルキル-C1-6アルコキシ)(-C1-6アルキル-C1-6アルコキシ)、-C(O)N(C1-4アルキル)(C1-4アルキル)、-C(O)NH2、-C(O)NH(C1-4アルキル)、及び-C(O)NH(C3-10シクロアルキル)から選択される1個以上の基によって任意に置換されてもよく；
    かつここで、上記のカルボシクリル基及びヘテロシクリル基のいずれも、C1-4アルキル、オキソ、ハロゲン、-C(O)C1-6アルキル、及びC1-4アルコキシから選択される1個以上の基によって任意に置換されてもよく；
    或いはR2は、フェニルによって置換されたフェニル、単環式ヘテロアリール基によって置換されたフェニル、フェノキシによって置換されたフェニル、ヘテロシクリルによって置換されたフェニル、ヘテロシクリルがフェニルによって置換されている該ヘテロシクリルにより置換されたフェニル、-O-C1-4アルキル-ヘテロシクリルにより置換されたフェニル、ベンジルオキシによって置換されたフェニル、カルボシクリルにより置換されたフェニル、カルボシクリルがヘテロシクリルにより置換されている該カルボシクリルにより置換されたフェニル、-O-カルボシクリルにより置換されたフェニル、フェニルにより置換されたヘテロシクリル、フェニルにより置換されたカルボシクリル、カルボシクリルに縮合されたフェニル、ヘテロシクリルに縮合されたフェニル、-C1-4アルキル(フェニルによって置換されたフェニル)、-C1-4アルキル(単環式ヘテロアリール基によって置換されたフェニル)、-C1-4アルキル(単環式ヘテロシクリル基によって置換されたフェニル)、-C1-4アルキル(-O-カルボシクリル基によって置換されたフェニル)、-C1-4アルキル(ベンジルオキシによって置換されたフェニル)、-C1-4アルキル(任意に置換されたカルボシクリルに縮合された任意に置換されたフェニル)、又はC1-4アルキル(任意に置換されたヘテロシクリルに縮合された任意に置換されたフェニル)を表し；
    ここで、上記のフェニル基、ベンジルオキシ基、及びヘテロアリール基のいずれも、C1-4アルキル、ハロゲン、及びC1-4アルコキシから選択される1個以上の基によって任意に置換されてもよく、かつここで、上記のカルボシクリル基及びヘテロシクリル基のいずれも、メチル、フェニル、オキソ、ハロゲン、ヒドロキシル、及びC1-4アルコキシから選択される1個以上の基によって任意に置換されてもよく；
    R3は、H、-C1-4アルキル、又はアリールを表し；
    ここで、上記のアリールは、C1-6アルキル、C2-6アルケニル、C2-6アルキニル、C1-6ハロアルキル、-C1-6チオアルキル、-SOC1-4アルキル、-SO2C1-4アルキル、C1-6アルコキシ-、-O-C3-8シクロアルキル、C3-8シクロアルキル、-SO2C3-8シクロアルキル、-SOC3-6シクロアルキル、C3-6アルケニルオキシ-、C3-6アルキニルオキシ-、-C(O)C1-6アルキル、-C(O)OC1-6アルキル、C1-6アルコキシ-C1-6アルキル-、ニトロ、ハロゲン、シアノ、ヒドロキシル、-C(O)OH、-NH2、-NHC1-4アルキル、-N(C1-4アルキル)(C1-4アルキル)、-C(O)N(C1-4アルキル)(C1-4アルキル)、-C(O)NH2、-C(O)NH(C1-4アルキル)、及び-C(O)NH(C3-10シクロアルキル)から選択される1個以上の基によって任意に置換されてもよく；,
    或いは、R2及びR3は、1個以上のC1-2アルキル基によって任意に置換されたカルボシクリル環を形成するよう結合し；
    或いは、R2及びR3は、フェニルに縮合されたカルボシクリル環を形成するよう結合し、ここで、上記のカルボシクリル及び／又はフェニルは、C1-4アルキル、ハロゲン、及びC1-4アルコキシから選択される1個以上の基によって任意に置換されてもよく；
    或いは、R2及びR3は、単環式ヘテロアリールに縮合されたカルボシクリル環を形成するよう結合し、ここで、上記のカルボシクリル及び／又はヘテロアリールは、C1-4アルキル、ハロゲン、及びC1-4アルコキシから選択される1個以上の基によって任意に置換されてもよく；
    Xは、C=O、O、S、CR7R8、-O-CH2-、又は-CH2-CH2-を表し；
    Yは、CHR9、C=O、又はC=Sを表し；
    Zは、-N-R4、O、又はCHR10を表し、その結果、XがO又はSを表す場合、ZはCHR10を表さなければならず；
    或いは、X及びZは、その位置で縮合されかつ1個以上のハロゲン又はC1-2アルキル基により任意に置換されているフェニル環の2個の隣接炭素原子を表し；
    R4は、H、-C1-8アルキル、-C(O)C1-6アルキル、又はNH2を表し；
    R7及びR8は独立して、H、-C1-4アルキル、又はアリールを表し；
    ここで、上述のアリールは、C1-6アルキル、C2-6アルケニル、C2-6アルキニル、C1-6ハロアルキル、-C1-6チオアルキル、-SOC1-4アルキル、-SO2C1-4アルキル、C1-6アルコキシ-、-O-C3-8シクロアルキル、C3-8シクロアルキル、-SO2C3-8シクロアルキル、-SOC3-6シクロアルキル、C3-6アルケニルオキシ-、C3-6アルキニルオキシ-、-C(O)C1-6アルキル、-C(O)OC1-6アルキル、C1-6アルコキシ-C1-6アルキル-、ニトロ、ハロゲン、シアノ、ヒドロキシル、-C(O)OH、-NH2、-NHC1-4アルキル、-N(C1-4アルキル)(C1-4アルキル)、-C(O)N(C1-4アルキル)(C1-4アルキル)、-C(O)NH2、-C(O)NH(C1-4アルキル)、及び-C(O)NH(C3-10シクロアルキル)により、任意に置換されてよく；
    R9及びR10は独立して、H又はメチルを表し；
    但し、-Y-Z-X-の部分は、-C(=O)-N(-R4)-C(=O)-又は-C(=S)-N(-R4)-C(=O)-以外を表す。)。
  2. 前記R1が、非置換のヘテロアリール、又は任意に1個以上のC1-6アルキル基(例えばメチル)、ハロゲン(例えばフッ素)、又はC1-6ハロアルキル基(例えばトリフルオロメチル)により置換されたヘテロアリールを表す、請求項1記載の化合物。
  3. 前記R1が、5-員ヘテロアリール環に縮合されたフェニル環を表し、ここでR1が、フェニル環を介して式(I)のコアに連結されている、請求項2記載の化合物。
  4. 前記R1が、
    Figure 2013504544
     を表し、ここで、Bが、結合、-CH2-、-CH2-CH2-、-CH(Me)-、-CH(Me)-CH2-、又は-CH2-CH(Me)-を表し、かつ
    R14及びR15が独立して、H又はC1-2アルキルを表す、請求項2又は3記載の化合物。
  5. 前記R1が、
    Figure 2013504544
     を表す、請求項4記載の化合物。
  6. 前記R2が、アリール、ヘテロアリール、フェニルによって置換されたフェニル、ヘテロシクリルに縮合されたフェニルを表し、又はR2及びR3が結合して、フェニルに縮合されたカルボシクリル環を形成し；上記のアリール、ヘテロアリール、フェニル、ヘテロシクリル、及びカルボシクリルが任意に置換されている、請求項1〜5のいずれか一項記載の化合物。
  7. 前記R2が、C1-6アルキル、C1-6アルコキシ、ヒドロキシル、ハロC1-6アルキル、ハロC1-6アルコキシ、ハロゲン、C1-6アルコキシ-C1-6アルキル-、C1-6アルコキシ-C1-6アルコキシ-、-N(C1-4アルキル)(C1-4アルキル)-N(C1-4アルキル)(C1-4アルキル)、-N(C1-4アルキル)(C1-4アルキル)、-N(C3-8シクロアルキル)(C3-8シクロアルキル)、-C1-4アルキル-N(C1-4アルキル)(C1-4アルキル)、-C1-4アルコキシ-N(C1-4アルキル)(C1-4アルキル)、-N(-C1-6アルキル-C1-6アルコキシ)(-C1-6アルキル-C1-6アルコキシ)から選択された1個以上の基により任意に置換されたフェニルを表す、請求項6記載の化合物。
  8. 前記R2が、1個以上のC1-6アルコキシ基により任意に置換されたフェニルを表す、請求項7記載の化合物。
  9. 前記R2が、プロポキシ基により任意に置換されたフェニルを表す、請求項8記載の化合物。
  10. 前記R3がHを表す、請求項1〜9のいずれか一項記載の化合物。
  11. 前記R4が、Hを表す、請求項1〜10のいずれか一項記載の化合物。
  12. 前記XがCR7R8を表し、YがC=Oを表し、かつZが-N-R4又はOを表す、請求項1〜11のいずれか一項記載の化合物。
  13. 前記XがC=Oを表し、YがCHR9を表し、かつZが-N-R4を表す、請求項1〜11のいずれか一項記載の化合物。
  14. 前記XがCR7R8を表し、YがCHR9又はC=Oを表し、かつZがCHR10を表す、請求項1〜11のいずれか一項記載の化合物。
  15. 前記XがSを表し、YがC=O又はC=Sを表し、かつZがCHR10を表す、請求項1〜11のいずれか一項記載の化合物。
  16. 前記X及びZが、2,5-ジクロロフェニル若しくは3,4ジクロロフェニルなどの、その位置で縮合されかつ1個以上のハロゲン又はC1-2アルキル基により任意に置換されているフェニル環の2個の隣接炭素原子を表し、かつYがC=Oを表す、請求項1〜11のいずれか一項記載の化合物。
  17. 前記Xが-O-CH2-を表し、YがCOを表し、かつZがCHR10を表す、請求項1〜11のいずれか一項記載の化合物。
  18. 前記Xが-CH2-CH2-を表し、YがCOを表し、かつZがOを表す、請求項1〜11のいずれか一項記載の化合物。
  19. 実施例1〜235のいずれか1つに記載の化合物、又は、すべての互変異性体及び立体異性体を含む、それらの医薬として許容し得る塩、溶媒和物、若しくは多形体：
    Figure 2013504544
    Figure 2013504544
    Figure 2013504544
    Figure 2013504544
    Figure 2013504544
    Figure 2013504544
    Figure 2013504544
    Figure 2013504544
    Figure 2013504544
    Figure 2013504544
    Figure 2013504544
    。
  20. 実施例12〜14のいずれか1つに記載の化合物、又は、すべての互変異性体及び立体異性体を含む、それらの医薬として許容し得る塩、溶媒和物、若しくは多形体：
    Figure 2013504544
     。
  21. 医薬品として使用するための、請求項1〜20のいずれか一項記載の化合物。
  22. 任意に1つ以上の治療上許容し得る希釈剤又は担体との組み合わせで、請求項1〜20のいずれか一項記載の化合物を含む医薬組成物。
  23. 神経保護薬、抗パーキンソン病薬、アミロイドタンパク質沈着阻害剤、βアミロイド合成阻害剤、抗うつ薬、抗不安薬、抗精神病薬、及び抗多発性硬化症薬からなる群から選択される、少なくとも1つの化合物を追加的に含有する、請求項22記載の医薬組成物。
  24. PEP阻害剤、LiCl、DP IV酵素又はDP IV様酵素の阻害剤の阻害剤、アセチルコリンエステラーゼ(ACE)阻害剤、PIMTエンハンサー、βセクレターゼの阻害剤、γセクレターゼの阻害剤、中性エンドペプチダーゼの阻害剤、ホスホジエステラーゼ-4(PDE-4)の阻害剤、TNFα阻害剤、ムスカリン性M1受容体アンタゴニスト、NMDA受容体アンタゴニスト、σ-1受容体阻害剤、ヒスタミンH3アンタゴニスト、免疫調節薬、免疫抑制薬、又はアンテグレン(ナタリズマブ)、Neurelan(ファムプリジン-SR)、カンパス(アレムツズマブ)、IR 208、NBI 5788／MSP771(チプリモチド)、パクリタキセル、Anergix.MS(AG 284)、SH636、ディフェリン(CD 271、アダパレン)、BAY 361677(インターロイキン-4)、マトリックス-メタロプロテイナーゼ-阻害剤、インターフェロン-τ(トロホブラスチン)、及びSAIK-MSからなる群から選択される作用物質からなる群から選択される少なくとも1つの化合物を追加的に含む、請求項22又は請求項23記載の医薬組成物。
  25. ケネディ病、ヘリコバクターピロリ感染を伴う又は伴わない十二指腸癌、結腸直腸癌、ゾリンジャー・エリソン症候群、ヘリコバクターピロリ感染を伴う又は伴わない胃癌、病原性精神病性容態、統合失調症、不妊、腫瘍、炎症性宿主反応、癌、悪性転移、メラノーマ、乾癬、液性及び細胞仲介性免疫応答障害、内皮内の白血球接着及び遊走プロセス、摂食障害、睡眠-覚醒障害、エネルギー代謝の恒常性調節障害、自律神経機能障害、ホルモン平衡障害又は体液の調節障害、多発性硬化症、ギラン・バレー症候群、慢性炎症性脱髄性多発性神経根症、軽度認知障害、アルツハイマー病、家族性英国型認知症、家族性デンマーク型認知症、ダウン症候群における神経変性、ハンチントン病、関節リウマチ、粥状硬化、膵炎、及び再狭窄からなる群から選択される疾患の治療において使用するための、請求項1〜20のいずれか一項記載の化合物又は請求項22〜23のいずれか一項記載の医薬組成物。
  26. 請求項1〜20のいずれか一項記載の式(I)の化合物の製造方法であって、下記のいずれかを含む、前記方法：
    (a)式(II)の化合物から式(I)の化合物を製造すること：
    Figure 2013504544
     (式中、R2、R3、X、Y及びZは請求項１に定義されるとおりである)；
    (b)式(III)の化合物の水素添加により、式(I)の化合物(式中、R3は水素を表し、YはCOを表し、Zは-N-R4を表し、かつXはCR7R8を表し、かつR8は水素を表す)を製造すること：
    Figure 2013504544
     (式中、R1、R2、R4、及びR7は請求項１に定義されるとおりである)；
    (c)式(IV)の化合物の水素添加により、式(I)の化合物(式中、R3は水素を表し、YはCOを表し、ZはCH2を表し、かつXはCH2を表す)を製造すること：
    Figure 2013504544
     (式中、R1及びR2は請求項１に定義されるとおりである)；
    (d)式(V)の化合物から、式(I)の化合物(式中、R3は水素を表し、YはCOを表し、Zは-N-R4を表し、かつXはCH2を表す)を製造すること：
    Figure 2013504544
     (式中、R1、R2、及びR4は請求項１に定義されるとおりである)；
    (e)式(VI)の化合物から、式(I)の化合物(式中、R3は水素を表し、YはCH2を表し、Zは-N-R4を表し、かつXはCOを表す)を製造すること：
    Figure 2013504544
     (式中、R1、R2、及びR4は請求項１に定義されるとおりである)；
    (f)式(VII)の化合物から、式(I)の化合物(式中、R1は1H-ベンゾ[d]イミダゾール-5-イルを表し、R3は水素を表し、YはCOを表し、Zは-NHを表し、かつXはCH2を表す)を製造すること：
    Figure 2013504544
     (式中、R2は請求項１に定義されるとおりである)；
    (g)式(VIII)の化合物から、式(I)の化合物(式中、R3は水素を表し、YはCOを表し、並びにX及びZは結合し炭素環を形成するか、又はそうでなければX及びZはその位置で縮合されかつ1個以上のハロゲン又はC1-2アルキル基により任意に置換されているフェニル環の2個の隣接炭素原子を表す)を製造すること：
    Figure 2013504544
     (式中、R1、R2、X、及びZは請求項１に定義されるとおりである)；
    (h)XがOを表す対応する化合物から、XはSを表す式(I)の化合物、例えば、式(I)の化合物(式中、R3は水素を表し、YはCOを表し、Zは-CH2を表し、かつXはSを表す)を製造すること：
    (i)R4がHを表す対応する式(I)の化合物から、亜硝酸塩による処理、それに続く還元により、式(I)の化合物(式中、R4は-NH2を表す)を製造すること；
    (j)R4がHを表す対応する式(I)の化合物から、アルキル化剤又はアルカノイル化剤による処理により、式(I)の化合物(式中、R4は-C1-8アルキル又は-C(O)C1-6アルキルを表す)を製造すること；
    (k)式(I)の化合物を相互転換すること；又は
    (i)保護された式(I)の化合物を脱保護すること。
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