JP2012162541A - 癌を処置するための化合物 - Google Patents
癌を処置するための化合物 Download PDFInfo
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- JP2012162541A JP2012162541A JP2012072925A JP2012072925A JP2012162541A JP 2012162541 A JP2012162541 A JP 2012162541A JP 2012072925 A JP2012072925 A JP 2012072925A JP 2012072925 A JP2012072925 A JP 2012072925A JP 2012162541 A JP2012162541 A JP 2012162541A
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- methanone
- trimethoxyphenyl
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- 0 COc1cc(C(C2N=C(c3ccccc3)SC2)=O)cc(*)c1* Chemical compound COc1cc(C(C2N=C(c3ccccc3)SC2)=O)cc(*)c1* 0.000 description 4
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Abstract
Description
QはS、N、またはOであり;
Xは任意に、かつO=、S=、=N−NH2、=N−OH、または−OHであることができ;
Yは任意に−N(H)−、O、またはC1〜C20の炭化水素であり;
R1およびR2は、互いに独立して、置換されたもしくは未置換の単環式、縮環式、多環式のアリールまたはヘテロ環系であり、飽和もしくは不飽和のN−ヘテロ環、飽和もしくは不飽和のS−ヘテロ環、および飽和もしくは不飽和のO−ヘテロ環、飽和もしくは不飽和の環状炭化水素、飽和もしくは不飽和の混合ヘテロ環、および脂肪族直鎖状または分枝状C1〜C30炭化水素を含む。化合物はその薬学的に許容される塩、水和物、またはプロドラッグとして提供され得る。
QはS、N、またはOであり;
Xは任意にS=、O=、=N−NH2、=N−OH、または−OHであることができ;
Yは任意に−N(H)−、O、またはC1〜C20の炭化水素であり;
R1およびR2は、互いに独立して、置換されたもしくは未置換の単環式、縮環式、多環式のアリールまたはヘテロ環系であり、飽和もしくは不飽和のN−ヘテロ環、飽和もしくは不飽和のS−ヘテロ環、および飽和もしくは不飽和のO−ヘテロ環、飽和もしくは不飽和の環状炭化水素、飽和もしくは不飽和の混合ヘテロ環、および脂肪族直鎖状または分枝状C1〜C30炭化水素を含む。
ル)イミダゾリジン−4−イル)メタノン;(2−(3,4−ジメトキシフェニル)−チアゾール−4−イル)(3,4,5−トリメトキシフェニル)メタノン(化合物8o);(4,5−ジヒドロ−2−(3,4−ジメトキシフェニル)チアゾール−4−イル)(3,4,5−トリメトキシフェニル)メタノン;(3,4,5−トリメトキシフェニル)(2−(3,4−ジメトキシフェニル)チアゾリジン−4−イル)メタノン;(2−(3,4−ジメトキシフェニル)オキサゾール−4−イル)(3,4,5−トリメトキシフェニル)メタノン;(4,5−ジヒドロ−2−(3,4−ジメトキシフェニル)オキサゾール−4−イル)(3,4,5−トリメトキシフェニル)メタノン;(3,4,5−トリメトキシフェニル)(2−(3,4−ジメトキシフェニル)オキサゾリジン−4−イル)メタノン;(2−(3,4−ジメトキシフェニル)−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;(4,5−ジヒドロ−2−(3,4−ジメトキシフェニル)−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;(3,4,5−トリメトキシフェニル)(2−(3,4−ジメトキシフェニル)イミダゾリジン−4−イル)メタノン;(2−(4−ニトロフェニル)−チアゾール−4−イル)(3,4,5−トリメトキシフェニル)メタノン(化合物8p);(4,5−ジヒドロ−2−(4−ニトロフェニル)チアゾール−4−イル)(3,4,5−トリメトキシフェニル)メタノン;(3,4,5−トリメトキシフェニル)(2−(4−ニトロフェニル)チアゾリジン−4−イル)メタノン;(2−(4−ニトロフェニル)オキサゾール−4−イル)(3,4,5−トリメトキシフェニル)メタノン;(4,5−ジヒドロ−2−(4−ニトロフェニル)オキサゾール−4−イル)(3,4,5−トリメトキシフェニル)メタノン;(3,4,5−トリメトキシフェニル)(2−(4−ニトロフェニル)オキサゾリジン−4−イル)メタノン;(2−(4−ニトロフェニル)−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;(4,5−ジヒドロ−2−(4−ニトロフェニル)−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;(3,4,5−トリメトキシフェニル)(2−(4−ニトロフェニル)イミダゾリジン−4−イル)メタノン;(2−(4−シアノフェニル)−チアゾール−4−イル)(3,4,5−トリメトキシフェニル)メタノン(化合物8q);(4,5−ジヒドロ−2−(4−シアノフェニル)チアゾール−4−イル)(3,4,5−トリメトキシフェニル)メタノン;(3,4,5−トリメトキシフェニル)(2−(4−シアノフェニル)チアゾリジン−4−イル)メタノン;(2−(4−シアノフェニル)オキサゾール−4−イル)(3,4,5−トリメトキシフェニル)メタノン;(4,5−ジヒドロ−2−(4−シアノフェニル)オキサゾール−4−イル)(3,4,5−トリメトキシフェニル)メタノン;(3,4,5−トリメトキシフェニル)(2−(4−シアノフェニル)オキサゾリジン−4−イル)メタノン;(2−(4−シアノフェニル)−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;(4,5−ジヒドロ−2−(4−シアノフェニル)−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;(3,4,5−トリメトキシフェニル)(2−(4−シアノフェニル)イミダゾリジン−4−イル)メタノン;4−(4−(3,4,5−トリメトキシベンゾイル)−チアゾール−2−イル)−安息香酸(化合物8r);4−(4−(3,4,5−トリメトキシベンゾイル)−(1,3−ジヒドロ)チアゾール−2−イル)−安息香酸;4−(4−(3,4,5−トリメトキシベンゾイル)−チアゾリジン−2−イル)−安息香酸;4−(4−(3,4,5−トリメトキシベンゾイル)−オキサゾール−2−イル)−安息香酸;4−(4−(3,4,5−トリメトキシベンゾイル)−(1,3−ジヒドロ)オキサゾール−2−イル)−安息香酸;4−(4−(3,4,5−トリメトキシベンゾイル)−オキサゾリジン−2−イル)−安息香酸;4−(4−(3,4,5−トリメトキシベンゾイル)−1H−イミダゾール−2−イル)−安息香酸;4−(4−(3,4,5−トリメトキシベンゾイル)−(1,3−ジヒドロ)−1H−イミダゾール−2−イル)−安息香酸;4−(4−(3,4,5−トリメトキシベンゾイル)−イミダゾリジン−2−イル)−安息香酸;メチル−4−(4−(3,4,5−トリメトキシベンゾイル)−チアゾール−2−イル)−ベンゾエート(化合物8s);メチル−4−(4−(3,4,5−トリメトキシベンゾイル)−(1,3−ジヒドロ)チアゾール−2−イル)−ベンゾエート;メチル−4−(4−(3,4,5−トリメトキシベンゾイル)−チアゾリジン−2−イル)−ベンゾエート;メチル−4−(4−(3,4,5−トリメトキシベンゾイル)−オキサゾール−2−イル)−ベンゾエート;メチル−4−(4−(3,4,5−トリメトキシベンゾイル)−(1,3−ジヒドロ)オキサゾール−2−イル)−ベンゾエート;メチル−4−(4−(3,4,5−トリメトキシベンゾイル)−オキサゾリジン−2−イル)−ベンゾエート;メチル−4−(4−(3,4,5−トリメトキシベンゾイル)−1H−イミダゾール−2−イル)−ベンゾエート;メチル−4−(4−(3,4,5−トリメトキシベンゾイル)−(1,3−ジヒドロ)−1H−イミダゾール−2−イル)−ベンゾエート;メチル−4−(4−(3,4,5−トリメトキシベンゾイル)−イミダゾリジン−2−イル)−ベンゾエート;(2−(4−(トリフルオロメチル)−フェニル)−チアゾール−4−イル)(3,4,5−トリメトキシフェニル)メタノン(化合物8t);(4,5−ジヒドロ−2−(4−(トリフルオロメチル)−フェニル)チアゾール−4−イル)(3,4,5−トリメトキシフェニル)メタノン;(3,4,5−トリメトキシフェニル)(2−(4−シアノフェニル)チアゾリジン−4−イル)メタノン;(2−(4−(トリフルオロメチル)−フェニル)オキサゾール−4−イル)(3,4,5−トリメトキシフェニル)メタノン;(4,5−ジヒドロ−2−(4−(トリフルオロメチル)−フェニル)オキサゾール−4−イル)(3,4,5−トリメトキシフェニル)メタノン;(3,4,5−トリメトキシフェニル)(2−(4−(トリフルオロメチル)−フェニル)オキサゾリジン−4−イル)メタノン;(2−(4−(トリフルオロメチル)−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;(4,5−ジヒドロ−2−(4−(トリフルオロメチル)−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;(3,4,5−トリメトキシフェニル)(2−(4−(トリフルオロメチル)−フェニル)イミダゾリジン−4−イル)メタノン;(2−(4−ブロモフェニル)−チアゾール−4−イル)−(3,4,5−トリメトキシフェニル)メタノン(化合物8u);(4,5−ジヒドロ−2−(4−ブロモフェニル)チアゾール−4−イル)(3,4,5−トリメトキシフェニル)メタノン;(3,4,5−トリメトキシフェニル)(2−(4−ブロモフェニル)チアゾリジン−4−イル)メタノン;(2−(4−ブロモフェニル)オキサゾール−4−イル)(3,4,5−トリメトキシフェニル)メタノン;(4,5−ジヒドロ−2−(4−ブロモフェニル)オキサゾール−4−イル)(3,4,5−トリメトキシフェニル)メタノン;(3,4,5−トリメトキシフェニル)(2−(4−ブロモフェニル)オキサゾリジン−4−イル)メタノン;(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;(4,5−ジヒドロ−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;(3,4,5−トリメトキシフェニル)(2−(4−ブロモフェニル)イミダゾリジン−4−イル)メタノン;(2−(4−エチルフェニル)−チアゾール−4−イル)−(3,4,5−トリメトキシ−フェニル)メタノン(化合物8v);(4,5−ジヒドロ−2−(4−エチルフェニル)チアゾール−4−イル)(3,4,5−トリメトキシフェニル)メタノン;(3,4,5−トリメトキシフェニル)(2−(4−エチルフェニル)チアゾリジン−4−イル)メタノン;(2−(4−エチルフェニル)オキサゾール−4−イル)(3,4,5−トリメトキシフェニル)メタノン;(4,5−ジヒドロ−2−(4−エチルフェニル)オキサゾール−4−イル)(3,4,5−トリメトキシフェニル)メタノン;(3,4,5−トリメトキシフェニル)(2−(4−エチルフェニル)オキサゾリジン−4−イル)メタノン;(2−(4−エチルフェニル)−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;(4,5−ジヒドロ−2−(4−エチルフェニル)−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;(3,4,5−トリメトキシフェニル)(2−(4−エチルフェニル)イミダゾリジン−4−イル)メタノン;(2−(4−アミノフェニル)−チアゾール−4−イル)−(3,4,5−トリメトキシ−フェニル)メタノン(化合物8w);(2−(4−アミノフェニル)チアゾリジン−4−イル)(3,4,5−トリメトキシフェニル)メタノン;(2−(4−アミノフェニル)−4,5−ジヒドロチアゾール−4−イル)(3,4,5−トリメトキシフェニル)メタノン;(2−(4−アミノフェニル)−オキサゾール−4−イル)−(3,4,5−トリメトキシ−フェニル)メタノン;(2−(4−アミノフェニル)オキサゾリジン−4−イル)(3,4,5−トリメトキシフェニル)メタノン;(2−(4−アミノフェニル)−4,5−ジヒドロオキサゾール−4−イル)(3,4,5−トリメトキシフェニル)メタノン;(2−(4−アミノフェニル)−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;(2−(4−アミノフェニル)−1H−イミダゾリジン−4−イル)(3,4,5−トリメトキシフェニル)メタノン;(2−(4−アミノフェニル)−4,5−ジヒドロイミダゾール−4−イル)(3,4,5−トリメトキシフェニル)メタノン;(2−(4−アセトアミドフェニル)チアゾリジン−4−イル)(3,4,5−トリメトキシフェニル)メタノン;(2−(4−アセトアミドフェニル)−4,5−ジヒドロチアゾール−4−イル)(3,4,5−トリメトキシフェニル)メタノン;(2−(4−アセトアミドフェニル)−チアゾール−4−イル)(3,4,5−トリメトキシフェニル)メタノン;(3,4,5−トリメトキシフェニル)(2−(3,4,5−トリメトキシフェニル)チアゾール−4−イル)メタノン;(4,5−ジヒドロ−2−(3,4,5−トリメトキシフェニル)チアゾール−4−イル)(3,4,5−トリメトキシフェニル)メタノン;(3,4,5−トリメトキシフェニル)(2−(3,4,5−トリメトキシフェニル)チアゾリジン−4−イル)メタノン;(3,4,5−トリメトキシフェニル)(2−(3,4−ジメトキシフェニル)チアゾール−4−イル)メタノン;(4,5−ジヒドロ−2−(3,4−ジメトキシフェニル)チアゾール−4−イル)(3,4,5−トリメトキシフェニル)メタノン;(3,4,5−トリメトキシフェニル)(2−(3,4−ジメトキシフェニル)チアゾリジン−4−イル)メタノン;(2−(4−fluornoフェニル)チアゾリジン−4−イル)(3,4,5−トリメトキシフェニル)メタノン;(2−(4−フルオロフェニル)−4,5−ジヒドロチアゾール−4−イル)(3,4,5−トリメトキシフェニル)メタノン;(2−(4−フルオロフェニル)−チアゾール−4−イル)(3,4,5−トリメトキシフェニル)メタノン;(3,4,5−トリメトキシ
フェニル)(2−(2−メトキシフェニル)チアゾール−4−イル)メタノン;(4,5−ジヒドロ−2−(2−メトキシフェニル)チアゾール−4−イル)(3,4,5−トリメトキシフェニル)メタノン;(3,4,5−トリメトキシフェニル)(2−(2−メトキシフェニル)チアゾリジン−4−イル)メタノン;(2−(ピリジン−4−イル)−チアゾール−4−イル)−(3,4,5−トリメトキシフェニル)メタノン(化合物8x);(4,5−ジヒドロ−2−(ピリジン−4−イル)チアゾール−4−イル)(3,4,5−トリメトキシフェニル)メタノン;(3,4,5−トリメトキシフェニル)(2−(ピリジン−4−イル)チアゾリジン−4−イル)メタノン;(2−(ピリジン−4−イル)−オキサゾール−4−イル)−(3,4,5−トリメトキシフェニル)メタノン;(4,5−ジヒドロ−2−(ピリジン−4−イル)オキサゾール−4−イル)(3,4,5−トリメトキシフェニル)メタノン;(3,4,5−トリメトキシフェニル)(2−(ピリジン−4−イル)オキサゾリジン−4−イル)メタノン;(2−(ピリジン−4−イル)−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;(4,5−ジヒドロ−2−(ピリジン−4−イル)−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;(3,4,5−トリメトキシフェニル)(2−(ピリジン−4−イル)イミダゾリジン−4−イル)メタノン;(2−(ピリミジン−2−イル)−チアゾール−4−イル)−(3,4,5−トリメトキシフェニル)メタノン(化合物8y);(4,5−ジヒドロ−2−(ピリミジン−4−イル)チアゾール−4−イル)(3,4,5−トリメトキシフェニル)メタノン;(3,4,5−トリメトキシフェニル)(2−(ピリミジン−4−イル)チアゾリジン−4−イル)メタノン;(2−(ピリミジン−4−イル)−オキサゾール−4−イル)−(3,4,5−トリメトキシフェニル)メタノン;(4,5−ジヒドロ−2−(ピリミジン−4−イル)オキサゾール−4−イル)(3,4,5−トリメトキシフェニル)メタノン;(3,4,5−トリメトキシフェニル)(2−(ピリミジン−4−イル)オキサゾリジン−4−イル)メタノン;(2−(ピリミジン−4−イル)−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;(4,5−ジヒドロ−2−(ピリミジン−4−イル)−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;(3,4,5−トリメトキシフェニル)(2−(ピリミジン−4−イル)イミダゾリジン−4−イル)メタノン;(2−(チオフェン−2−イル)−チアゾール−4−イル)−(3,4,5−トリメトキシフェニル)メタノン(化合物8z);(4,5−ジヒドロ−2−(チオフェン−2−イル)チアゾール−4−イル)(3,4,5−トリメトキシフェニル)メタノン;(3,4,5−トリメトキシフェニル)(2−(チオフェン−2−イル)チアゾリジン−4−イル)メタノン;(2−(チオフェン−2−イル)−オキサゾール−4−イル)−(3,4,5−トリメトキシフェニル)メタノン;(4,5−ジヒドロ−2−(チオフェン−2−イル)オキサゾール−4−イル)(3,4,5−トリメトキシフェニル)メタノン;(3,4,5−トリメトキシフェニル)(2−(チオフェン−2−イル)オキサゾリジン−4−イル)メタノン;(2−(チオフェン−2−イル)−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;(4,5−ジヒドロ−2−(チオフェン−2−イル)−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;(3,4,5−トリメトキシフェニル)(2−(チオフェン−2−イル)イミダゾリジン−4−イル)メタノン;(2−(1H−インドール−5−イル)チアゾール−4−イル)(3,4,5−トリメトキシフェニル)メタノン(化合物31);(2−(1H−インドール−5−イル)チアゾリジン−4−イル)(3,4,5−トリメトキシフェニル)メタノン;(4,5−ジヒドロ−2−(1H−インドール−5−イル)チアゾール−4−イル)(3,4,5−トリメトキシフェニル)メタノン;(2−(1H−インドール−5−イル)オキサゾール−4−イル)(3,4,5−トリメトキシフェニル)メタノン;(2−(1H−インドール−5−イル)オキサゾリジン−4−イル)(3,4,5−トリメトキシフェニル)メタノン;(4,5−ジヒドロ−2−(1H−インドール−5−イル)オキサゾール−4−イル)(3,4,5−トリメトキシフェニル)メタノン;(2−(1H−インドール−5−イル)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;(2−(1H−インドール−5−イル)イミダゾリジン−4−イル)(3,4,5−トリメトキシフェニル)メタノン;(4,5−ジヒドロ−2−(1H−インドール−5−イル)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;(2−(1H−インドール−2−イル)チアゾール−4−イル)(3,4,5−トリメトキシフェニル)メタノン(化合物32);(4,5−ジヒドロ−2−(1H−インドール−2−イル)チアゾール−4−イル)(3,4,5−トリメトキシフェニル)メタノン;(2−(1H−インドール−2−イル)チアゾリジン−4−イル)(3,4,5−トリメトキシフェニル)メタノン;(2−(1H−インドール−2−イル)オキサゾール−4−イル)(3,4,5−トリメトキシフェニル)メタノン;(4,5−ジヒドロ−2−(1H−インドール−2−イル)オキサゾール−4−イル)(3,4,5−トリメトキシフェニル)メタノン;(2−(1H−インドール−2−イル)オキサゾリジン−4−イル)(3,4,5−トリメトキシフェニル)メタノン;(2−(1H−インドール−2−イル)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;(4,5−ジヒドロ−2−(1H−インドール−2−イル)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;(2−(1H−インドール−2−イル)イミダゾリジン−4−イル)(3,4,5−トリメトキシフェニル)メタノン;(2−(1H−インドール−1−イル)チアゾール−4−イル)(3,4,5−トリメトキシフェニル)メタノン;(4,5−ジヒドロ−2−(1H−インドール−1−イル)チアゾール−4−イル)(3,4,5−トリメトキシフェニル)メタノン;(2−(1H−インドール−1−イル)チアゾリジン−4−イル)(3,4,5−トリメトキシフェニル)メタノン;(2−(1H−インドール−1−イル)オキサゾール−4−イル)(3,4,5−トリメトキシフェニル)メタノン;(4,5−ジヒドロ−2−(1H−インドール−1−イル)オキサゾール−4−イル)(3,4,5−トリメトキシフェニル)メタノン;(2−(1H−インドール−1−イル)オキサゾリジン−4−イル)(3,4,5−トリメトキシフェニル)メタノン;(2−(1H−インドール−1−イル)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;(4,5−ジヒドロ−2−(1H−インドール−1−イル)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;(2−(1H−インドール−1−イル)イミダゾリジン−4−イル)(3,4,5−トリメトキシフェニル)メタノン;(2−(1H−インドール−3−イル)チアゾール−4−イル)(3,4,5−トリメトキシフェニル)メタノン;(4,5−ジヒドロ−2−(1H−インドール−3−イル)チアゾール−4−イル)(3,4,5−トリメトキシフェニル)メタノン;(2−(1H−インドール−3−イル)チアゾリジン−4−イル)(3,4,5−トリメトキシフェニル)メタノン;(2−(1H−インドール−3−イル)オキサゾール−4−イル)(3,4,5−トリメトキシフェニル)メタノン;(4,5−ジヒドロ−2−(1H−インドール−3−イル)オキサゾール−4−イル)(3,4,5−トリメトキシフェニル)メタノン;(2−(1H−インドール−3−イル)オキサゾリジン−4−イル)(3,4,5−トリメトキシフェニル)メタノン;(2−(1H−インドール−3−イル)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;(4,5−ジヒドロ−2−(1H−インドール−3−イル)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;(2−(1H−インドール−3−イル)イミダゾリジン−4−イル)(3,4,5−トリメトキシフェニル)メタノン;(2−(1H−インドール−4−イル)チアゾール−4−イル)(3,4,5−トリメトキシフェニル)メタノン;(4,5−ジヒドロ−2−(1H−インドール−4−イル)チアゾール−4−イル)(3,4,5−トリメトキシフェニル)メタノン;(2−(1H−インドール−4−イル)チアゾリジン−4−イル)(3,4,5−トリメトキシフェニル)メタノン;(2−(1H−インドール−4−イル)オキサゾール−4−イル)(3,4,5−トリメトキシフェニル)メタノン;(4,5−ジヒドロ−2−(1H−インドール−4−イル)オキサゾール−4−イル)(3,4,5−トリメトキシフェニル)メタノン;(2−(1H−インドール−4−イル)オキサゾリジン−4−イル)(3,4,5−トリメトキシフェニル)メタノン;(2−(1H−インドール−4−イル)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;(4,5−ジヒドロ−2−(1H−インドール−4−イル)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;(2−(1H−インドール−4−イル)イミダゾリジン−4−イル)(3,4,5−トリメトキシフェニル)メタノン;(2−(1H−インドール−6−イル)チアゾール−4−イル)(3,4,5−トリメトキシフェニル)メタノン;(4,5−ジヒドロ−2−(1H−インドール−6−イル)チアゾール−4−イル)(3,4,5−トリメトキシフェニル)メタノン;(2−(1H−インドール−6−イル)チアゾリジン−4−イル)(3,4,5−トリメトキシフェニル)メタノン;(2−(1H−インドール−6−イル)オキサゾール−4−イル)(3,4,5−トリメトキシフェニル)メタノン;(4,5−ジヒドロ−2−(1H−インドール−6−イル)オキサゾール−4−イル)(3,4,5−トリメトキシフェニル)メタノン;(2−(1H−インドール−6−イル)オキサゾリジン−4−イル)(3,4,5−トリメトキシフェニル)メタノン;(2−(1H−インドール−6−イル)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;(4,5−ジヒドロ−2−(1H−インドール−6−イル)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;(2−(1H−インドール−6−イル)イミダゾリジン−4−イル)(3,4,5−トリメトキシフェニル)メタノン;(2−(1H−インドール−7−イル)チアゾール−4−イル)(3,4,5−トリメトキシフェニル)メタノン;(4,5−ジヒドロ−2−(1H−インドール−7−イル)チアゾール−4−イル)(3,4,5−トリメトキシフェニル)メタノン;(2−(1H−インドール−7−イル)チアゾリジン−4−イル)(3,4,5−トリメトキシフェニル)メタノン;(2−(1H−インドール−1−イル)オキサゾール−4−イル)(3,4,5−トリメトキシフェニル)メタノン;(4,5−ジヒドロ−2−(1H−インドール−7−イル)オキサゾール−4−イル)(3,4,5−トリメトキシフェニル)メタノン;(2−(1H−インドール−7−イル)オキサゾリジン−4−イル)(3,4,5−トリメトキシフェニル)メタノン;(2−(1H−インドール−7−イル)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;(4,5−ジヒドロ−2−(1H−インドール−7−イル)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;および(2−(
1H−インドール−7−イル)イミダゾリジン−4−イル)(3,4,5−トリメトキシフェニル)メタノンが挙げられる。
Claims (14)
- 前記R1およびR2が、互いに独立して、置換されたもしくは未置換の、フラニル基、インドリル基、ピリジニル基、フェニル基、ビフェニル基、トリフェニル基、ジフェニルメタン基、アダマンタン−イル基またはフルオレン−イル基である、請求項1に記載の化合物。
- 前記R1およびR2が、互いに独立して、置換されたもしくは未置換のフェニル基である、請求項1に記載の化合物。
- 前記QがSまたはNである、請求項1に記載の化合物。
- R3、R4及びR5で置換された前記R2が3,4,5−トリメトキシフェニルである、請求項1に記載の化合物。
- R1が、置換されたもしくは未置換のフェニル基、置換されたもしくは未置換のチオフェン−イル基、または置換されたもしくは未置換のインドリル基であり、
前記置換が、エチル基、フルオロ基、ブロモ基、シアノ基、ニトロ、トリフルオロ基およびアミノ基より成る群から選択される1以上の置換基によりなされる、請求項5に記載の化合物。 - 前記化合物が下記の群から選択される請求項1に記載の化合物。
(3,4,5−トリメトキシフェニル)(2−フェニルチアゾール−4−イル)メタノン、
(2−p−トリルチアゾール−4−イル)(3,4,5−トリメトキシフェニル)メタノン、
(2−(4−フルオロフェニル)−チアゾール−4−イル)(3,4,5−トリメトキシフェニル)メタノン、
(2−(4−ニトロフェニル)−チアゾール−4−イル)(3,4,5−トリメトキシフェニル)メタノン、
(2−(4−シアノフェニル)−チアゾール−4−イル)(3,4,5−トリメトキシフェニル)メタノン、
(2−(4−(トリフルオロメチル)−フェニル)−チアゾール−4−イル)(3,4,5−トリメトキシフェニル)メタノン、
(2−(4−ブロモフェニル)−チアゾール−4−イル)−(3,4,5−トリメトキシフェニル)メタノン、
(2−(4−エチルフェニル)−チアゾール−4−イル)−(3,4,5−トリメトキシ−フェニル)メタノン、
(2−(4−アミノフェニル)−チアゾール−4−イル)−(3,4,5−トリメトキシ−フェニル)メタノン、
(2−(チオフェン−2−イル)−チアゾール−4−イル)−(3,4,5−トリメトキシフェニル)メタノン、
(2−(1H−インドール−5−イル)チアゾール−4−イル)(3,4,5−トリメトキシフェニル)メタノン、
(2−(1H−インドール−2−イル)チアゾール−4−イル)(3,4,5−トリメトキシフェニル)メタノン、
(2−(1H−インドール−1−イル)チアゾール−4−イル)(3,4,5−トリメトキシフェニル)メタノン、
(2−(1H−インドール−3−イル)チアゾール−4−イル)(3,4,5−トリメトキシフェニル)メタノン、
(2−(1H−インドール−4−イル)チアゾール−4−イル)(3,4,5−トリメトキシフェニル)メタノン、
(2−(1H−インドール−6−イル)チアゾール−4−イル)(3,4,5−トリメトキシフェニル)メタノン、および
(2−(1H−インドール−7−イル)チアゾール−4−イル)(3,4,5−トリメトキシフェニル)メタノン。 - 請求項1の化合物と薬学的に許容される担体とを含む薬学的組成物。
- 癌を治療する方法であって、
請求項1の化合物を、癌を有する被験体に対して、その癌の治療に有効な条件下で投与するステップを含み、
前記癌が、前立腺癌、乳癌、卵巣癌、皮膚癌、肺癌、結腸癌、白血病、腎臓癌、CNS癌およびそれらの組み合わせより成る群から選択される、方法。 - 前記投与が、全身的に行われる、請求項9に記載の方法。
- 前記投与が、経口的に、局所的に、経皮的に、非経口的に、皮下に、静脈内に、筋肉内に、腹腔内的に、鼻腔内滴下により、腔内滴下により、膀胱内滴下により、眼内に、動脈内に、病巣内に、または粘膜への塗布により行われる、請求項9に記載の方法。
- 前記化合物が、約0.01〜約100mg/kg体重の用量で投与される、請求項9に記載の方法。
- 前記投与が定期的に行われる、請求項9に記載の方法。
- 前記投与が他の癌治療法と組み合わせて行われる、請求項9に記載の方法。
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