JP5784909B2 - スプライシング異常からもたらされる疾患を処置する為のスライスする機構を阻害する化学分子 - Google Patents
スプライシング異常からもたらされる疾患を処置する為のスライスする機構を阻害する化学分子 Download PDFInfo
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- JP5784909B2 JP5784909B2 JP2010541800A JP2010541800A JP5784909B2 JP 5784909 B2 JP5784909 B2 JP 5784909B2 JP 2010541800 A JP2010541800 A JP 2010541800A JP 2010541800 A JP2010541800 A JP 2010541800A JP 5784909 B2 JP5784909 B2 JP 5784909B2
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- benzamide
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- phenylamino
- phenyl
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Description
ここで、
X1は、CR10基を表し、R10は、水素原子である;
R1は、NR11R12基を表し、R11及びR12は、互に独立に、C1〜C3アルキル基を表す、又は、
R1は、OR12基を表し、R12はC1〜C3アルキル基又はトリフルオロメチル基を表す;
Y1は、窒素原子又はCR13基を表し、R13は、水素原子である;
R2は、NR14R15基を表し、R14は水素原子であり且つR15は直鎖状若しくは分枝状のC1〜C10アルキル基を表し、ここで1つの炭素原子が窒素原子により置き換えられていてもよく、及び、1つの炭素原子が窒素原子により置き換えられていない場合、該アルキル基は1つの−OH基又は、置換された又は置換されていない、
の基により置換されている;
R3は、水素原子を表す;
R21は、水素原子を表す;
又は、
ここで、
X1は、窒素原子又はCR10基を表し、R10は水素原子である;
R1は、水素原子又はOR12基を表し、R12はC1〜C3アルキル基を表し、X 1 がCH基を表す場合にR1がOR12基を表す;
Y1は、窒素原子又はCR13基を表し、R13は水素原子である;
R2は、NR14R15基を表し、R14は水素原子であり且つR15は直鎖状若しくは分枝状のC1〜C10アルキル基を表し、ここで1つの炭素原子が窒素原子により置き換えられていてもよく、及び、1つの炭素原子が窒素原子により置き換えられていない場合、該アルキル基は1つの−OH基又は、置換された又は置換されていない、
の基により置換されている;
R3は、水素原子を表す;
R21は、水素原子を表す;
又は、
ここで、
R7は、NR11R12基を表し、R11及びR12は互に独立にC1〜C3アルキル基であり、又は、R7は、OR12基を表し、R12はC1〜C3アルキル基又はトリフルオロメチル基である;
X2は、CR16基を表し、R16は水素原子である;
R4は、水素原子、C1〜C3アルキル基、又はC(=O)NR14R15基を表し、R14は水素原子であり且つR15は直鎖状若しくは分枝状のC1〜C10アルキル基であり、ここで1つの炭素原子が窒素原子により置き換えられており、R4は、R5又はR6が水素原子と異なる場合に、水素原子又はC1〜C3アルキル基を表す;
R5は、水素原子、C(=O)NR14R15基、ここでR14は水素原子であり且つR15は直鎖状若しくは分枝状のC1〜C10アルキル基であり、ここで1つの炭素原子が窒素原子により置き換えられていてもよい、又は、
基、ここでR15は直鎖状若しくは分枝状のC1〜C10アルキル基であり、ここで1つの炭素原子が窒素原子により置き換えられていてもよく、該アルキル基は1つのOH基により置換されていてもよい、を表し、R5は、R4又はR6が水素原子と異なる場合に、水素原子を表す;
R6は、
水素原子、
C(=O)NR14R15基、R14は水素原子であり且つR15は直鎖状若しくは分枝状のC1〜C10アルキル基であり、ここで1つの炭素原子が窒素原子により置き換えられていてもよい、又は
の基、ここでR15は直鎖状若しくは分枝状のC1〜C10アルキル基であり、ここで1つの炭素原子が窒素原子により置き換えられていてもよく、該アルキル基は1つのOH基により置換されていてもよい、
を表し、且つ、R6は、R5が水素原子と異なる場合に又はR4が水素原子又はC1〜C3アルキル基と異なる場合に、水素原子を表す;
R21は、水素原子を表す;
又は
ここで、
X1は、窒素原子又はCR10基を表し、R10はOR11基であり、R11はC1〜C3アルキル基を表す;
R1は、水素原子を表す;
Y2は、CR11基を表し、R11は、
水素原子、
基、ここでR4は、水素原子又はC1〜C3アルキル基を表す;R5は、水素原子、C(=O)NR14R15基、ここでR14は水素原子であり且つR15は直鎖状若しくは分枝状のC1〜C10アルキル基であり、ここで1つの炭素原子が窒素原子により置き換えられていてもよい、又は
基、ここでR15は直鎖状若しくは分枝状のC1〜C10アルキル基であり、ここで1つの炭素原子が窒素原子により置き換えられていてもよく、該アルキル基は1つのOH基により置換されていてもよい、を表し、R5は、R4又はR6が水素原子と異なる場合に、水素原子を表す;R6は、水素原子、C(=O)NR14R15基、ここでR14は水素原子であり且つR15は直鎖状若しくは分枝状のC1〜C10アルキル基であり、ここで1つの炭素原子が窒素原子により置き換えられていてもよい、又は
基、ここでR15は直鎖状若しくは分枝状のC1〜C10アルキル基であり、該アルキル基は1つのOH基により置換されている、を表し、且つ、R6は、R5が水素原子と異なる場合に、水素原子を表す;又は
の基を含む群のうちから選ばれ、ここでR17は直鎖状若しくは分枝状のC1〜C3アルキル基を表し、該アルキル基は1つの−OH基により置換されていてもよい;
R8及びR8’は、
水素原子
基、ここで
R4は、水素原子又はC1〜C3アルキル基を表す;
R5は、水素原子、C(=O)NR14R15基、ここでR14は水素原子であり且つR15は直鎖状若しくは分枝状のC1〜C10アルキル基であり、ここで1つの炭素原子が窒素原子により置き換えられていてもよい、又は
基、ここでR15は直鎖状若しくは分枝状のC1〜C10アルキル基であり、ここで1つの炭素原子が窒素原子により置き換えられていてもよく、該アルキル基は1つのOH基により置換されていてもよい、を表し、R5は、R4又はR6が水素原子と異なる場合に、水素原子を表す;
R6は、水素原子又はC(=O)NR14R15基、ここでR14は水素原子であり且つR15は直鎖状若しくは分枝状のC1〜C10アルキル基であり、ここで1つの炭素原子が窒素原子により置き換えられていてもよい、を表し、且つ、R6は、R5が水素原子と異なる場合に、水素原子を表す;又は
C(=O)NR18R19基、ここでR18は水素原子を表し且つR19は(CH2)4−OHを表す、を表し、
R8は、Y2 がCH基と異なる場合およびR8’が水素原子と異なる場合に、水素原子を表す;且つ
R8’は、Y2 がCH基と異なる場合およびR8が水素原子と異なる場合に、水素原子を表す;
R21及びR22は、水素原子を表す。
N-(4-メトキシ-フェニル)-2-[6-(N'-(4-メトキシ-フェニルニコチンアミド)-ピリジン-2-イルアミノ)-ヘキシルアミノ]-ニコチンアミド;
2-(2-ジメチルアミノ-エチルアミノ)-N-(4-トリフルオロメトキシ-フェニル)-ニコチンアミド;
2-(3-ジメチルアミノ-プロピルアミノ)-N-(4-トリフルオロメトキシ-フェニル)-ニコチンアミド;
2-(3-ジエチルアミノ-プロピルアミノ)-N-(4-トリフルオロメトキシ-フェニル)-ニコチンアミド;
2-(4-ヒドロキシ-ブチルアミノ)-N-(4-トリフルオロメトキシ-フェニル)-ニコチンアミド;
N-(4-トリフルオロメトキシ-フェニル)-2-[6-(N'-(4-トリフルオロメトキシ-フェニルニコチンアミド)-ピリジン-2-イルアミノ)-ヘキシルアミノ]-ニコチンアミド;
N-(3-ジエチルアミノ-プロピル)-3-[3-(3-メトキシベンズアミド)-フェニルアミノ]-ベンズアミド;
N-(3-メチル-ブチル)-3-メチル-4-[3-(4-メトキシベンズアミド)-フェニルアミノ]-ベンズアミド;及び
(N-ジエチルアミノ)-3-(1-{3-[4(4-メトキシベンズアミド)-フェニルアミノ]-フェニル}-1H-1,2,3-トリアゾール-4-イル)-メチルアミン;
2-ブロモ-N-(4-ジメチルアミノ-フェニル)-ベンズアミド;
2-クロロ-N-(4-ジメチルアミノ-フェニル)-ニコチンアミド;
2-(2-ジメチルアミノ-エチルアミノ)-N-(4-メトキシ-フェニル)-ニコチンアミド ;
2-(2-ジメチルアミノ-エチルアミノ)-N-(4-メトキシ-フェニル)-ベンズアミド;
2-(3-ジエチルアミノ-エチルアミノ)-N-(4-メトキシ-フェニル)-ベンズアミド;
2-(3-ジメチルアミノ-プロピルアミノ)-N-(4-メトキシ-フェニル)-ベンズアミド;
2-(4-ヒドロキシ-ブチルアミノ)-N-(4-メトキシ-フェニル)-ベンズアミド;
2-(3-イミダゾール-1-イル-プロピルアミノ)-N-(4-メトキシ-フェニル)-ベンズアミド;
2-クロロ-N-(4-トリフルオロメトキシ-フェニル)-ニコチンアミド;
2-ブロモ-N-(4-トリフルオロメトキシ-フェニル)-ベンズアミド;
2-(3-イミダゾール-1-イル-プロピルアミノ)-N-(4-トリフルオロメトキシ-フェニル)-ニコチンアミド;
2-(2-ジエチルアミノ-エチルアミノ)-N-(4-トリフルオロメトキシ-フェニル)-ベンズアミド;
2-(3-ジメチルアミノ-プロピルアミノ)-N-(4-トリフルオロメトキシ-フェニル)-ベンズアミド;
2-(3-ジエチルアミノ-プロピルアミノ)-N-(4-トリフルオロメトキシ-フェニル)-ベンズアミド;
2-(4-ヒドロキシ-ブチルアミノ)-N-(4-トリフルオロメトキシ-フェニル)-ベンズアミド;
2-(6-アミノ-ヘキシルアミノ)-N-(4-トリフルオロメトキシ-フェニル)-ベンズアミド;
2-(3-イミダゾール-1-イル-プロピルアミノ)-N-(4-トリフルオロメトキシ-フェニル)-ベンズアミド;及び
2-(4-ジエチルアミノ-1-メチル-ブチルアミノ)-N-(4-トリフルオロメトキシ-フェニル)-ベンズアミド。
2-(2-ジメチルアミノ-エチルアミノ)-N-(4-メトキシ-フェニル)-ニコチンアミド ;
2-(2-ジメチルアミノ-エチルアミノ)-N-(4-メトキシ-フェニル)-ベンズアミド;
2-(3-イミダゾール-1-イル-プロピルアミノ)-N-(4-トリフルオロメトキシ-フェニル)-ベンズアミド、
のうちから選ばれる。
4-ベンゾイルアミノ-N-(2-ジエチルアミノ-エチル)-ベンズアミド;
N-(3-メチル-ブチル)-3-[3-(4-メトキシ-ベンゾイルアミノ)-フェニルアミノ]-ベンズアミド;
N-{3-[3-(4-ジエチルアミノメチル-[1,2,3]トリアゾール-1-イル)-フェニルアミノ]-フェニル}-4-メトキシ-ベンズアミド;
N-(3-{4-[4-(3-ヒドロキシ-プロピル)-[1,2,3]トリアゾール-1-イル]-フェニルアミノ}-フェニル)-4-メトキシ-ベンズアミド;及び
N-(3-メチル-ブチル)-4-[3-(4-メトキシベンズアミド)-フェニルアミノ]-ベンズアミド。
2-(3-ジメチルアミノ-プロピルアミノ)-N-ピリジン-3-イル-ベンズアミド;
2-(3-イミダゾール-1-イル-プロピルアミノ)-N-ピリジン-3-イル-ベンズアミド;
2-(2-ジメチルアミノ-エチルアミノ)-N-ピリジン-3-イル-ニコチンアミド;
2-(2-ジエチルアミノ-エチルアミノ)-N-ピリジン-3イル-ニコチンアミド;
2-(3-ジメチルアミノ-プロピルアミノ)-N-ピリジン-3-イル-ニコチンアミド;
2-(3-ジエチルアミノ-プロピルアミノ)-N-ピリジン-3-イル-ニコチンアミド;
2-(3-イミダゾール-1-イル-プロピルアミノ)-N-ピリジン-3-イル-ニコチンアミド;
2-ブロモ-N-ピリジン-3-イル-ベンズアミド ;
2-ブロモ-N-(4-メトキシ-フェニル)-ベンズアミド ;
2-クロロ-N-(4-メトキシ-フェニル)-ニコチンアミド ;
2-クロロ-N-ピリジン-3-イル-ニコチンアミド ;及び
2-(3-ジエチルアミノ-プロピルアミノ)-N-ピリジン-3-イル-ベンズアミド。
N-(4-ピリジル)-2-[6-(N'-(4-ピリジルベンズアミド)-フェニルアミノ)-1-ヒドロキシブチルアミノ]-ベンズアミド;
2-(3-ジエチルアミノ-プロピルアミノ)-N-ピリジン-4-イル-ニコチンアミド;
2-(3-イミダゾール-1-イル-プロピルアミノ)-N-ピリジン-4イル-ニコチンアミド;
N-(3-ジエチルアミノ-プロピル)-3-[3-(3-メトキシベンズアミド)-フェニルアミノ]-ベンズアミド;
3-(1-{3-[3-メトキシベンズアミド)-フェニルアミノ]-フェニル}-1H-1,2,3-トリアゾール-4-イル)-プロパン-1-オール;
N-(3-ジエチルアミノ-プロピル)-3-メチル-4-[3-(3-メトキシベンズアミド)-フェニルアミノ]-ベンズアミド;
N-(3-メチル-ブチル)-4-[3-(3-メトキシベンズアミド)-フェニルアミノ]-ベンズアミド;
3-(1-{4-[3-メトキシベンズアミド)-フェニルアミノ]-フェニル}-1H-1,2,3-トリアゾール-4-イル)-プロパン-1-オール;
(N-ジエチルアミノ)-3-(1-{3-[3-メトキシベンズアミド)-フェニルアミノ]-フェニル}-1H-1,2,3-トリアゾール-4-イル)-メチルアミン;
3-(1-{4-[3-メトキシベンズアミド)-フェニルアミノ]-フェニル}-1H-1,2,3-トリアゾール-4-イル)-プロパン-1-オール;
N-(3-ジエチルアミノ-プロピル)-4-[4-(3-メトキシベンズアミド)-フェニルアミノ]-ベンズアミド;
N-(3-ジエチルアミノ-プロピル)-3-メチル-4-[4-(3-メトキシベンズアミド)-フェニルアミノ]-ベンズアミド;
N-(3-メチル-ブチル)-3-メチル-4-[4-(3-メトキシベンズアミド)-フェニルアミノ]-ベンズアミド;
(N-ジエチルアミノ)-3-(1-{4-[4-(3-メトキシベンズアミド)-フェニルアミノ]-フェニル}-1H-1,2,3-トリアゾール-4-イル)-メチルアミン;
3-(1-{4-[3-メトキシベンズアミド)-フェニルアミノ]-フェニル}-1H-1,2,3-トリアゾール-4-イル)-プロパン-1-オール;
N-(3-ジエチルアミノ-プロピル)-3-[4-(3-メトキシベンズアミド)-フェニルアミノ]-ベンズアミド;
N-(3-メチル-ブチル)-3-[4-(3-メトキシベンズアミド)-フェニルアミノ]-ベンズアミド;
2-クロロ-N-(3-メトキシ-フェニル)-ニコチンアミド;
2-(3-ジメチルアミノ-プロピルアミノ)-N-(3-メトキシ-フェニル)-ニコチンアミド;
2-ブロモ-N-ピリジン-4-イル-ベンズアミド;
2-ブロモ-N-(3-メトキシ-フェニル)-ベンズアミド;
2-クロロ-N-ピリジン-4-イル-ニコチンアミド;
2-(2-ジメチルアミノ-エチルアミノ)-N-(3-メトキシ-フェニル)-ニコチンアミド;
2-(2-ジエチルアミノ-エチルアミノ)-N-(3-メトキシ-フェニル)-ニコチンアミド;
2-(3-ジエチルアミノ-プロピルアミノ)-N-(3-メトキシ-フェニル)-ニコチンアミド;
2-(4-ヒドロキシ-ブチルアミノ)-N-(3-メトキシ-フェニル)-ニコチンアミド;
2-(5-ヒドロキシ-ペンチルアミノ)-N-(3-メトキシ-フェニル)-ニコチンアミド;
2-(6-アミノ-ヘキシルアミノ)-N-(3-メトキシ-フェニル)-ニコチンアミド;
2-(3-イミダゾール-1-イル-プロピルアミノ)-N-(3-メトキシ-フェニル)-ニコチンアミド;
2-(2-ジメチルアミノ-エチルアミノ)-N-(3-メトキシ-フェニル)-ベンズアミド;
2-(2-ジエチルアミノ-エチルアミノ)-N-(3-メトキシ-フェニル)-ベンズアミド;
2-(4-ヒドロキシ-ブチルアミノ)-N-(3-メトキシ-フェニル)-ベンズアミド;
2-(4-ジエチルアミノ-1-メチル-ブチルアミノ)-N-(3-メトキシ-フェニル)-ベンズアミド;
2-(2-ジエチルアミノ-エチルアミノ)-N-ピリジン-4-イル-ベンズアミド;
2-(2-ジエチルアミノ-エチルアミノ)-N-ピリジン-4-イル-ベンズアミド;
2-(3-ジエチルアミノ-プロピルアミノ)-N-ピリジン-4-イル-ベンズアミド;
2-(3-イミダゾール-1-イル-プロピルアミノ)-N-ピリジン-4-イル-ベンズアミド;
2-(2-ジエチルアミノ-エチルアミノ)-N-ピリジン-4-イル-ニコチンアミド ;及び
2-(3-ジメチルアミノ-プロピルアミノ)-N-ピリジン-4-イル-ニコチンアミド。
N-(3-ジエチルアミノ-プロピル)-3-メチル-4-[3-(3-メトキシベンズアミド)-フェニルアミノ]-ベンズアミド;
N-(3-メチル-ブチル)-4-[3-(3-メトキシベンズアミド)-フェニルアミノ]-ベンズアミド;
2-ブロモ-N-(3-メトキシ-フェニル)-ベンズアミド;
2-(6-アミノ-ヘキシルアミノ)-N-(3-メトキシ-フェニル)-ニコチンアミド;及び
2-(3-イミダゾール-1-イル-プロピルアミノ)-N-(3-メトキシ-フェニル)-ニコチンアミド。
N-(3-ジメチルアミノ-プロピル)-3-(4-トリフルオロメトキシ-フェニルアミノ)-ベンズアミド;
4-(4-メトキシ-フェニルアミノ)-3-メチル-N-(3-メチル-ブチル)-ベンズアミド;
3-メチル-N-(3-メチル-ブチル)-4-(4-トリフルオロメトキシ-フェニルアミノ)-ベンズアミド;
N-(2-ジメチルアミノ-エチル)-2-(4-トリフルオロメトキシ-フェニルアミノ)-ベンズアミド;
N-(2-ジエチルアミノ-エチル)-2-(4-トリフルオロメトキシフェニルアミノ)-ベンズアミド;
N-(2-ジエチルアミノ-プロピル)-2-(4-トリフルオロメトキシ-フェニルアミノ)-ベンズアミド;
(N-ジエチルアミノ)-{1-[4-(4-メトキシ-フェニルアミノ)-フェニル]-1H-1,2,3-トリアゾール-4-イル}-メチルアミン;
(N-ジエチルアミノ)-{1-[4-(4-トリフルオロメトキシフェニルアミノ)-フェニル]-1H-1,2,3-トリアゾール-4-イル}-メチルアミン;
(N-ジエチルアミノ)-{1-[4-(4-N-ジメチルアミノ-フェニルアミノ)-フェニル]-1H-1,2,3-トリアゾール-4-イル}-メチルアミン;
N-(3-イミダゾール-1-イル-プロピル)-2-(4-メトキシ-フェニルアミノ)-ベンズアミド;
N-(3-イミダゾール-1-イル-プロピル)-2-(4-トリフルオロメトキシ-フェニルアミノ)-ベンズアミド;
2-(4-ジメチルアミノ-フェニルアミノ)-N-(3-イミダゾール-1-イル-プロピル)-ベンズアミド;
N-(4-ジエチルアミノ-1-メチル-ブチル)-2-(4-ジメチルアミノフェニルアミノ)-ベンズアミド;
N-(2-ジメチルアミノ-エチル)-4-(4-トリフルオロメトキシ-フェニルアミノ)-ベンズアミド;
N-(2-ジメチルアミノ-エチル)-4-(4-ジメチルアミノ-フェニルアミノ)-ベンズアミド;
N-(2-ジメチルアミノ-エチル)-4-(4-メトキシ-フェニルアミノ)-3-メチル-ベンズアミド;
N-(3-ジエチルアミノ-プロピル)-4-(4-メトキシ-フェニルアミノ)-ベンズアミド;
N-(3-ジエチルアミノ-プロピル)-4-(4-メトキシ-フェニルアミノ)-3-メチル-ベンズアミド;
N-(3-ジエチルアミノ-プロピル)-3-メチル-4-(4-トリフルオロメトキシ-フェニルアミノ)-ベンズアミド;
N-(3-ジエチルアミノ-プロピル)-4-(4-ジメチルアミノ-フェニルアミノ)-3-メチル-ベンズアミド;
N-(2-ジメチルアミノ-エチル)-3-メチル-4-(4-トリフルオロメトキシ-フェニルアミノ)-ベンズアミド;
3-{1-[4-(4-メトキシ-フェニルアミノ)-フェニル]-1H-1,2,3-トリアゾール-4-イル}-プロパン-1-オール;
(N-ジエチルアミノ)-{1-[3-(4-メトキシ-フェニルアミノ)-フェニル]-1H-1,2,3-トリアゾール-4-イル}-メチルアミン;
[4-(5-クロロ-1H-イミダゾール-2-イル)-2-メチル-フェニル]-(4-メトキシ-フェニル)-アミン;
N-(2-ジエチルアミノ-エチル)-4-(4-メトキシ-フェニルアミノ)-ベンズアミド;
N-(2-ジメチルアミノ-エチル)-2-(4-メトキシ-フェニルアミノ)-ベンズアミド;
4-(4-メトキシ-フェニルアミノ)-N-(3-メチル-ブチル)-ベンズアミド;
N-(3-イミダゾール-1-イル-プロピル)-4-(4-トリフルオロメトキシ-フェニルアミノ)-ベンズアミド;
[3-(4-ジエチルアミノメチル-[1,2,3]トリアゾール-1-イル)-フェニル]-(4-ジメチルアミノ)-フェニルアミン;
N-(2-ジエチルアミノ-エチル)-2-(4-メトキシ-フェニルアミノ)-ベンズアミド;
3-{1-[3-(4-トリフルオロメトキシ-フェニルアミノ)-フェニル]-1H-[1,2,3]トリアゾール-4-イル}-プロパン-1-オール;及び
3-{1-[3-(4-ジメチルアミノ-フェニルアミノ)-フェニル]-1H-[1,2,3]トリアゾール-4-イル}-プロパン-1-オール。
N-(3-ジメチルアミノ-プロピル)-3-(ピリジン-3-イルアミノ)-ベンズアミド;
3-メチル-N-(3-メチル-ブチル)-4-(ピリジン-3-イルアミノ)-ベンズアミド;
N-(3-メチル-ブチル)-4-(ピリジン-3-イルアミノ)-ベンズアミド;
(N-ジエチルアミノ)-{1-[4-(ピリジン-3-イルアミノ)-フェニル]-1H-1,2,3-トリアゾール-4-イル}-メチルアミン;
N-(3-イミダゾール-1-イル-プロピル)-2-(ピリジン-3-イルアミノ)-ベンズアミド;
N-(2-ジメチルアミノ-エチル)-4-(ピリジン-3-イルアミノ)-ベンズアミド;
N-(3-ジエチルアミノ-プロピル)-3-[3-(3-メトキシベンズアミド)-フェニルアミノ]-ベンズアミド;
3-(1-{3-[3-メトキシベンズアミド)-フェニルアミノ]-フェニル}-1H-1,2,3-トリアゾール-4-イル)-プロパン-1-オール;
N-(3-ジエチルアミノ-プロピル)-3-メチル-4-[3-(3-メトキシベンズアミド)-フェニルアミノ]-ベンズアミド;
N-(3-メチル-ブチル)-4-[3-(3-メトキシベンズアミド)-フェニルアミノ]-ベンズアミド;
3-(1-{4-[3-メトキシベンズアミド)-フェニルアミノ]-フェニル}-1H-1,2,3-トリアゾール-4-イル)-プロパン-1-オール;
(N-ジエチルアミノ)-3-(1-{3-[3-メトキシベンズアミド)-フェニルアミノ]-フェニル}-1H-1,2,3-トリアゾール-4-イル)-メチルアミン;
N-(3-ジエチルアミノ-プロピル)-3-メチル-4-(ピリジン-3-イルアミノ)-ベンズアミド;
N-(3-ジエチルアミノ-プロピル)-3-[3-(3-メトキシベンズアミド)-フェニルアミノ]-ベンズアミド;
N-(3-メチル-ブチル)-3-メチル-4-[3-(4-メトキシベンズアミド)-フェニルアミノ]-ベンズアミド;
(N-ジエチルアミノ)-3-(1-{3-[4(4-メトキシベンズアミド)-フェニルアミノ]-フェニル}-1H-1,2,3-トリアゾール-4-イル)-メチルアミン;
4-メチル-N-(3-メチル-ブチル)-3-[3-((E)-2-ピリジン-4-イル-ビニル)-フェニルアミノ]-ベンズアミド;
N-(3-ジエチルアミノ-プロピル)-3-[3-((E)-2-ピリジン-4-イル-ビニル)-フェニルアミノ]-ベンズアミド;
N-(3-メチル-ブチル)-3-[3-((E)-2-ピリジン-4-イル-ビニル)-フェニルアミノ]-ベンズアミド;
(N-ジエチルアミノ)-3-(1-{3-[3-((E)-2-ピリジン-4-イル-ビニル)-フェニルアミノ]-フェニル}-1H-1,2,3-トリアゾール-4-イル)-メチルアミン;
3-(1-{3-[3-((E)-2-ピリジン-4-イル-ビニル)-フェニルアミノ]-フェニル}-1H-1,2,3-トリアゾール-4-イル)-プロパン-1-オール;
N-(2-ジメチルアミノ-エチル)-4-(4-トリフルオロメトキシフェニルアミノ)-ベンズアミド;
N-(3-ジエチルアミノ-プロピル)-3-メチル-4-[3-((E)-2-ピリジン-4-イル-ビニル)-フェニルアミノ]-ベンズアミド;
N-(3-メチル-ブチル)-4-[3-((E)-2-ピリジン-4-イル-ビニル)-フェニルアミノ]-ベンズアミド;
N-(3-ジメチルアミノ-プロピル)-4-(4-メトキシ-フェニルアミノ)-ベンズアミド;
N-(2-ジメチルアミノ-エチル)-2-(ピリジン-3-イルアミノ)-ベンズアミド;
N-(3-ジエチルアミノ-プロピル)-2-(ピリジン-3-イルアミノ)-ベンズアミド;
N-{3-[3-(3-ジエチルアミノ-プロピルカルバモイル)-フェニルアミノ]-フェニル}-ニコチンアミド;
N-(3-ジエチルアミノ-プロピル)-3-[3-(ピリドイル)-フェニルアミノ]-ベンズアミド;
N-{3-[3-(3-メチル-ブチルカルバモイル)-フェニルアミノ]-フェニル}-ニコチンアミド;
N-{3-[3-(4-ジエチルアミノメチル-[1,2,3]トリアゾール-1-イル)-フェニルアミノ]-フェニル}-ニコチンアミド;
N-{3-[4-(3-ジエチルアミノ-プロピルカルバモイル)-フェニルアミノ]-フェニル}-ニコチンアミド;
N-(3-ジメチルアミノ プロピル)-2-(4-メトキシ-フェニルアミノ)-ベンズアミド;及び
N-(3-ジメチルアミノ プロピル)-2-(ピリジン-3-イルアミノ)ベンズアミド。
N-(2-ジメチルアミノ-エチル)-4-(4-トリフルオロメトキシフェニルアミノ)-ベンズアミド;
N-(2-ジメチルアミノ-エチル)-4-(ピリジン-3-イルアミノ)-ベンズアミド;
N-(3-ジエチルアミノ-プロピル)-3-メチル-4-[3-(3-メトキシベンズアミド)-フェニルアミノ]-ベンズアミド;及び
N-(3-メチル-ブチル)-4-[3-(3-メトキシベンズアミド)-フェニルアミノ]-ベンズアミド。
N-(2-ジメチルアミノ-エチル)-2-(ピリジン-4-イルアミノ)-ベンズアミド;
N-(3-ジメチルアミノ-プロピル)-3-(3-メトキシ-フェニルアミノ)-ベンズアミド;
N-(3-ジメチルアミノ-プロピル)-3-(4-メトキシ-フェニルアミノ)-ベンズアミド;
4-(3-メトキシ-フェニルアミノ)-3-メチル-N-(3-メチル-ブチル)-ベンズアミド;
3-メチル-N-(3-メチル-ブチル)-4-(ピリジン-4-イルアミノ)-ベンズアミド;
N-(3-メチル-ブチル)-4-(ピリジン-4-イルアミノ)-ベンズアミド;
(N-ジエチルアミノ)-{1-[4-(3-メトキシ-フェニルアミノ)-フェニル]-1H-1,2,3-トリアゾール-4-イル}-メチルアミン;
N-(2-ジメチルアミノ-エチル)-3-(3-メトキシ-フェニルアミノ)-ベンズアミド;
N-(3-イミダゾール-1-イル-プロピル)-2-(3-メトキシ-フェニルアミノ)-ベンズアミド;
N-(2-ジメチルアミノ-エチル)-4-(3-メトキシ-フェニルアミノ)-ベンズアミド;
N-(3-ジエチルアミノ-プロピル)-4-(3-メトキシ-フェニルアミノ)-3-メチル-ベンズアミド;
3-{1-[4-(3-メトキシ-フェニルアミノ)-フェニル]-1H-1,2,3-トリアゾール-4-イル}-プロパン-1-オール;
N-(3-ジエチルアミノ-プロピル)-3-[4-((E)-2-ピリジン-4-イル-ビニル)-フェニルアミノ]-ベンズアミド;
N-(3-メチル-ブチル)-3-[4-((E)-2-ピリジン-4-イル-ビニル)-フェニルアミノ]-ベンズアミド;
(N-ジエチルアミノ)-3-(1-{3-[4-((E)-2-ピリジン-4-イル-ビニル)-フェニルアミノ]-フェニル}-1H-1,2,3-トリアゾール-4-イル)-メチルアミン;
3-(1-{3-[4-((E)-2-ピリジン-4-イル-ビニル)-フェニルアミノ]-フェニル}-1H-1,2,3-トリアゾール-4-イル)-プロパン-1-オール;
N-(3-ジエチルアミノ-プロピル)-3-メチル-4-[4-((E)-2-ピリジン-4-イル-ビニル)-フェニルアミノ]-ベンズアミド;
3-メチル-N-(3-メチル-ブチル)-4-[4-((E)-2-ピリジン-4-イル-ビニル)-フェニルアミノ]-ベンズアミド;
3-(1-{4-[4-((E)-2-ピリジン-4-イル-ビニル)-フェニルアミノ]-フェニル}-1H-1,2,3-トリアゾール-4-イル)-プロパン-1-オール;
3-(1-{4-[3-メトキシベンズアミド)-フェニルアミノ]-フェニル}-1H-1,2,3-トリアゾール-4-イル)-プロパン-1-オール;
N-(3-ジエチルアミノ-プロピル)-4-[4-(3-メトキシベンズアミド)-フェニルアミノ]-ベンズアミド;
N-(3-ジエチルアミノ-プロピル)-3-メチル-4-[4-(3-メトキシベンズアミド)-フェニルアミノ]-ベンズアミド;
N-(3-メチル-ブチル)-3-メチル-4-[4-(3-メトキシベンズアミド)-フェニルアミノ]-ベンズアミド;
(N-ジエチルアミノ)-3-(1-{4-[4-(3-メトキシベンズアミド)-フェニルアミノ]-フェニル}-1H-1,2,3-トリアゾール-4-イル)-メチルアミン;
3-(1-{4-[3-メトキシベンズアミド)-フェニルアミノ]-フェニル}-1H-1,2,3-トリアゾール-4-イル)-プロパン-1-オール;
N-(3-ジエチルアミノ-プロピル)-3-[4-(3-メトキシベンズアミド)-フェニルアミノ]-ベンズアミド;
N-(3-メチル-ブチル)-3-[4-(3-メトキシベンズアミド)-フェニルアミノ]-ベンズアミド;
4-(3-メトキシ-フェニルアミノ)-N-(3-メチル-ブチル)-ベンズアミド;
[3-(4-ジエチルアミノメチル-[1,2,3]トリアゾール-1-イル)-フェニル]-(3-メトキシ)-フェニルアミン;
N-(3-ジエチルアミノ-プロピル)-3-[4-(4-メトキシ-ベンゾイルアミノ)-フェニルアミノ]-3-メチル-ベンズアミド;
N-(3-メチル-ブチル)-3-[4-(4-メトキシ-ベンゾイルアミノ)-フェニルアミノ]-ベンズアミド;
(N-ジエチルアミノ)-3-(1-{4-[(4-メトキシベンズアミド)-フェニルアミノ]-フェニル}-1H-1,2,3-トリアゾール-4-イル)-メチルアミン;
3-(1-{4-[(4-メトキシベンズアミド)-フェニルアミノ]-フェニル}-1H-1,2,3-トリアゾール-4-イル)-プロパン-1-オール;
N-(3-ジエチルアミノ-プロピル)-4-[4-(4-メトキシ-ベンゾイルアミノ)-フェニルアミノ]-3-メチル-ベンズアミド;
N-(3-メチル-ブチル)-4-[4-(4-メトキシ-ベンゾイルアミノ)-フェニルアミノ]-ベンズアミド;及び
N-{4-[3-(3-メチル-ブチルカルバモイル)-フェニルアミノ]-フェニル}-ニコチンアミド。
N-(3-ジエチルアミノ-プロピル)-3-[4-(4-メトキシ-ベンゾイルアミノ)-フェニルアミノ]-3-メチル-ベンズアミド;
N-(3-メチル-ブチル)-3-[4-(4-メトキシ-ベンゾイルアミノ)-フェニルアミノ]-ベンズアミド;
3-(1-{4-[(4-メトキシベンズアミド)-フェニルアミノ]-フェニル}-1H-1,2,3-トリアゾール-4-イル)-プロパン-1-オール;
N-(3-ジエチルアミノ-プロピル)-4-[4-(4-メトキシ-ベンゾイルアミノ)-フェニルアミノ]-3-メチル-ベンズアミド;及び
N-(3-メチル-ブチル)-4-[4-(4-メトキシ-ベンゾイルアミノ)-フェニルアミノ]-ベンズアミド。
N-(4-ヒドロキシ-ブチル)-3-((E)-2-ピリジン-2-イル-ビニル)-ベンズアミド;
2-(1-{4-[(E)-2-(4-メトキシ-フェニル)-ビニル]-フェニル}-1H-1,2,3-トリアゾール-4-イル)-プロパン-2-オール;
N-(4-ヒドロキシ-ブチル)-3-[2-(4-メトキシ-フェニル)-ビニル]-ベンズアミド;
N-(3-ジエチルアミノ-プロピル)-3-[4-((E)-2-ピリジン-2-イル-ビニル)-フェニルアミノ]-ベンズアミド;
N-(3-メチル-ブチル)-3-[4-((E)-2-ピリジン-2-イル-ビニル)-フェニルアミノ]-ベンズアミド;
N-(3-ジエチルアミノ-プロピル)-4-[4-((E)-2-ピリジン-2-イル-ビニル)-フェニルアミノ]-ベンズアミド;
N-(3-メチル-ブチル)-4-[4-((E)-2-ピリジン-2-イル-ビニル)-フェニルアミノ]-ベンズアミド;及び
3-(1-{3-[4-((E)-2-ピリジン-2-イルビニル)-フェニルアミノ]-フェニル}-1H-1,2,3-トリアゾール-4-イル)-プロパン-1-オール。
N-(3-ジエチルアミノ-プロピル)-3-[4-((E)-2-ピリジン-4-イル-ビニル)-フェニルアミノ]-ベンズアミド;
N-(3-メチル-ブチル)-3-[4-((E)-2-ピリジン-4-イル-ビニル)-フェニルアミノ]-ベンズアミド;
(N-ジエチルアミノ)-3-(1-{3-[4-((E)-2-ピリジン-4-イル-ビニル)-フェニルアミノ]-フェニル}-1H-1,2,3-トリアゾール-4-イル)-メチルアミン;
3-(1-{3-[4-((E)-2-ピリジン-4-イル-ビニル)-フェニルアミノ]-フェニル}-1H-1,2,3-トリアゾール-4-イル)-プロパン-1-オール;
N-(3-ジエチルアミノ-プロピル)-3-メチル-4-[4-((E)-2-ピリジン-4-イル-ビニル)-フェニルアミノ]-ベンズアミド;
3-メチル-N-(3-メチル-ブチル)-4-[4-((E)-2-ピリジン-4-イル-ビニル)-フェニルアミノ]-ベンズアミド;
3-(1-{4-[4-((E)-2-ピリジン-4-イル-ビニル)-フェニルアミノ]-フェニル}-1H-1,2,3-トリアゾール-4-イル)-プロパン-1-オール;
4-メチル-N-(3-メチル-ブチル)-3-[3-((E)-2-ピリジン-4-イル-ビニル)-フェニルアミノ]-ベンズアミド;
N-(3-ジエチルアミノ-プロピル)-3-[3-((E)-2-ピリジン-4-イル-ビニル)-フェニルアミノ]-ベンズアミド;
N-(3-メチル-ブチル)-3-[3-((E)-2-ピリジン-4-イル-ビニル)-フェニルアミノ]-ベンズアミド;
(N-ジエチルアミノ)-3-(1-{3-[3-((E)-2-ピリジン-4-イル-ビニル)-フェニルアミノ]-フェニル}-1H-1,2,3-トリアゾール-4-イル)-メチルアミン;
3-(1-{3-[3-((E)-2-ピリジン-4-イル-ビニル)-フェニルアミノ]-フェニル}-1H-1,2,3-トリアゾール-4-イル)-プロパン-1-オール;
N-(3-ジエチルアミノ-プロピル)-3-メチル-4-[3-((E)-2-ピリジン-4-イル-ビニル)-フェニルアミノ]-ベンズアミド;
N-(3-メチル-ブチル)-4-[3-((E)-2-ピリジン-4-イル-ビニル)-フェニルアミノ]-ベンズアミド;
N-(3-ジエチルアミノール-プロピル)-3-[3-((E)-(4-メトキシ-スチリル)-フェニルアミノ]-ベンズアミド;
N-(3-メチル-ブチル)-3-[3-((E)-(4-メトキシ-スチリル)-フェニルアミノ]-ベンズアミド;
N-(3-ジエチルアミノール-プロピル)-3-メチル-4-[3-((E)-(4-メトキシ-スチリル)-フェニルアミノ]-ベンズアミド;
N-(3-メチル-ブチル)-3-メチル-4-[3-((E)-(4-メトキシ-スチリル)-フェニルアミノ]-ベンズアミド;
N-(3-メチル-ブチル)-4-[3-((E)-(4-メトキシ-スチリル)-フェニルアミノ]-ベンズアミド;
N-(3-ジエチルアミノ-プロピル)-3-[3-((E)-2-ピリジン-2-イル-ビニル)-フェニルアミノ]-ベンズアミド;
N-(3-メチル-ブチル)-3-[3-((E)-2-ピリジン-2-イル-ビニル)-フェニルアミノ]-ベンズアミド;
3-(1-{3-[4-((E)-2-ピリジン-4-イルビニル)-フェニルアミノ]-フェニル}-1H-1,2,3-トリアゾール-4-イル)-プロパン-1-オール;
N-(3-ジエチルアミノ-プロピル)-4-[3-((E)-2-ピリジン-2-イル-ビニル)-フェニルアミノ]-ベンズアミド;
N-(3-メチル-ブチル)-3-メチル-4-[3-((E)-2-ピリジン-2-イル-ビニル)-フェニルアミノ]-ベンズアミド;及び
3-(1-{3-[3-((E)-2-ピリジン-2-イルビニル)-フェニルアミノ]-フェニル}-1H-1,2,3-トリアゾール-4-イル)-プロパン-1-オール。
・インドリンの窒素及びIDC16のD環の窒素が、水素結合の受容体として作用しうること;
・N−メチル化4−ピリジノンモチーフが、該アナログにおいて保存されうること;
・平らな四環系幾何学(geometry)は最適ではなくそしてB環及びC環を他のモチーフにより置き換えてDNA挿入特性を制限することが賢明でありうること。
Claims (25)
- 以下の式(Ia)、(IIIa)、(IV)及び(IX)の一つを有する化合物、該化合物の医薬的に許容できる塩、それらの異性体、及び/又はそれらの混合物、
X1は、CR10基を表し、R10は、水素原子である;
R1は、NR11R12基を表し、R11及びR12は、互に独立に、C1〜C3アルキル基を表す、又は、
R1は、OR12基を表し、R12はC1〜C3アルキル基又はトリフルオロメチル基を表す;
Y1は、窒素原子又はCR13基を表し、R13は、水素原子である;
R2は、NR14R15基を表し、R14は水素原子であり且つR15は直鎖状若しくは分枝状のC1〜C10アルキル基を表し、ここで1つの炭素原子が窒素原子により置き換えられていてもよく、及び、1つの炭素原子が窒素原子により置き換えられていない場合、該アルキル基は1つの−OH基又は、置換された又は置換されていない、
R3は、水素原子を表す;
R21は、水素原子を表す;
又は、
X1は、窒素原子又はCR10基を表し、R10は水素原子である;
R1は、水素原子又はOR12基を表し、R12はC1〜C3アルキル基を表し、X 1 がCH基を表す場合にR1がOR12基を表す;
Y1は、窒素原子又はCR13基を表し、R13は水素原子である;
R2は、NR14R15基を表し、R14は水素原子であり且つR15は直鎖状若しくは分枝状のC1〜C10アルキル基を表し、ここで1つの炭素原子が窒素原子により置き換えられていてもよく、及び、1つの炭素原子が窒素原子により置き換えられていない場合、該アルキル基は1つの−OH基又は、置換された又は置換されていない、
R3は、水素原子を表す;
R21は、水素原子を表す;
又は、
R7は、NR11R12基を表し、R11及びR12は互に独立にC1〜C3アルキル基であり、又は、R7は、OR12基を表し、R12はC1〜C3アルキル基又はトリフルオロメチル基である;
X2は、CR16基を表し、R16は水素原子である;
R4は、水素原子、C1〜C3アルキル基、又はC(=O)NR14R15基を表し、R14は水素原子であり且つR15は直鎖状若しくは分枝状のC1〜C10アルキル基であり、ここで1つの炭素原子が窒素原子により置き換えられており、R4は、R5又はR6が水素原子と異なる場合に、水素原子又はC1〜C3アルキル基を表す;
R5は、水素原子、C(=O)NR14R15基、ここでR14は水素原子であり且つR15は直鎖状若しくは分枝状のC1〜C10アルキル基であり、ここで1つの炭素原子が窒素原子により置き換えられていてもよい、又は、
R6は、
水素原子、
C(=O)NR14R15基、R14は水素原子であり且つR15は直鎖状若しくは分枝状のC1〜C10アルキル基であり、ここで1つの炭素原子が窒素原子により置き換えられていてもよい、又は
を表し、且つ、R6は、R5が水素原子と異なる場合に又はR4が水素原子又はC1〜C3アルキル基と異なる場合に、水素原子を表す;
R21は、水素原子を表す;
又は
X1は、窒素原子又はCR10基を表し、R10はOR11基であり、R11はC1〜C3アルキル基を表す;
R1は、水素原子を表す;
Y2は、CR11基を表し、R11は、
水素原子、
R8及びR8’は、
水素原子
R4は、水素原子又はC1〜C3アルキル基を表す;
R5は、水素原子、C(=O)NR14R15基、ここでR14は水素原子であり且つR15は直鎖状若しくは分枝状のC1〜C10アルキル基であり、ここで1つの炭素原子が窒素原子により置き換えられていてもよい、又は
R6は、水素原子又はC(=O)NR14R15基、ここでR14は水素原子であり且つR15は直鎖状若しくは分枝状のC1〜C10アルキル基であり、ここで1つの炭素原子が窒素原子により置き換えられていてもよい、を表し、且つ、R6は、R5が水素原子と異なる場合に、水素原子を表す;又は
C(=O)NR18R19基、ここでR18は水素原子を表し且つR19は(CH2)4−OHを表す、を表し、
R8は、Y2 がCH基と異なる場合およびR8’が水素原子と異なる場合に、水素原子を表す;且つ
R8’は、Y2 がCH基と異なる場合およびR8が水素原子と異なる場合に、水素原子を表す;
R21及びR22は、水素原子を表す。 - 式(IV)を有する、請求項1の化合物。
- N-(3-ジメチルアミノ-プロピル)-3-(4-メトキシ-フェニルアミノ)-ベンズアミド;
N-(3-ジメチルアミノ-プロピル)-3-(4-トリフルオロメトキシ-フェニルアミノ)-ベンズアミド;
4-(4-メトキシ-フェニルアミノ)-3-メチル-N-(3-メチル-ブチル)-ベンズアミド;
3-メチル-N-(3-メチル-ブチル)-4-(4-トリフルオロメトキシ-フェニルアミノ)-ベンズアミド;
N-(2-ジメチルアミノ-エチル)-2-(4-トリフルオロメトキシ-フェニルアミノ)-ベンズアミド;
N-(2-ジエチルアミノ-エチル)-2-(4-トリフルオロメトキシフェニルアミノ)-ベンズアミド;
N-(2-ジエチルアミノ-プロピル)-2-(4-トリフルオロメトキシ-フェニルアミノ)-ベンズアミド;
(N-ジエチルアミノ)-{1-[4-(4-メトキシ-フェニルアミノ)-フェニル]-1H-1,2,3-トリアゾール-4-イル}-メチルアミン;
(N-ジエチルアミノ)-{1-[4-(4-トリフルオロメトキシフェニルアミノ)-フェニル]-1H-1,2,3-トリアゾール-4-イル}-メチルアミン;
(N-ジエチルアミノ)-{1-[4-(4-N-ジメチルアミノ-フェニルアミノ)-フェニル]-1H-1,2,3-トリアゾール-4-イル}-メチルアミン;
N-(4-ジエチルアミノ-1-メチル-ブチル)-2-(4-ジメチルアミノフェニルアミノ)-ベンズアミド;
N-(2-ジメチルアミノ-エチル)-4-(4-トリフルオロメトキシ-フェニルアミノ)-ベンズアミド;
N-(2-ジメチルアミノ-エチル)-4-(4-ジメチルアミノ-フェニルアミノ)-ベンズアミド;
N-(2-ジメチルアミノ-エチル)-4-(4-メトキシ-フェニルアミノ)-3-メチル-ベンズアミド;
N-(3-ジエチルアミノ-プロピル)-4-(4-メトキシ-フェニルアミノ)-ベンズアミド;
N-(3-ジエチルアミノ-プロピル)-4-(4-メトキシ-フェニルアミノ)-3-メチル-ベンズアミド;
N-(3-ジエチルアミノ-プロピル)-3-メチル-4-(4-トリフルオロメトキシ-フェニルアミノ)-ベンズアミド;
N-(3-ジエチルアミノ-プロピル)-4-(4-ジメチルアミノ-フェニルアミノ)-3-メチル-ベンズアミド;
N-(2-ジメチルアミノ-エチル)-3-メチル-4-(4-トリフルオロメトキシ-フェニルアミノ)-ベンズアミド;
3-{1-[4-(4-メトキシ-フェニルアミノ)-フェニル]-1H-1,2,3-トリアゾール-4-イル}-プロパン-1-オール;
(N-ジエチルアミノ)-{1-[3-(4-メトキシ-フェニルアミノ)-フェニル]-1H-1,2,3-トリアゾール-4-イル}-メチルアミン;
[4-(5-クロロ-1H-イミダゾール-2-イル)-2-メチル-フェニル]-(4-メトキシ-フェニル)-アミン;
N-(2-ジエチルアミノ-エチル)-4-(4-メトキシ-フェニルアミノ)-ベンズアミド;
N-(2-ジメチルアミノ-エチル)-2-(4-メトキシ-フェニルアミノ)-ベンズアミド;
4-(4-メトキシ-フェニルアミノ)-N-(3-メチル-ブチル)-ベンズアミド;
[3-(4-ジエチルアミノメチル-[1,2,3]トリアゾール-1-イル)-フェニル]-(4-ジメチルアミノ)-フェニルアミン;
N-(2-ジエチルアミノ-エチル)-2-(4-メトキシ-フェニルアミノ)-ベンズアミド;
3-{1-[3-(4-トリフルオロメトキシ-フェニルアミノ)-フェニル]-1H-[1,2,3]トリアゾール-4-イル}-プロパン-1-オール;
3-{1-[3-(4-ジメチルアミノ-フェニルアミノ)-フェニル]-1H-[1,2,3]トリアゾール-4-イル}-プロパン-1-オール;及び
N-(3-ジメチルアミノ-プロピル)-2-(4-メトキシ-フェニルアミノ)-ベンズアミド
を含む群のうちから選ばれるものである化合物。 - 式(IIIa)を有する、請求項1の化合物。
- N-(4-ピリジル)-2-[6-(N'-(4-ピリジルベンズアミド)-フェニルアミノ)-1-ヒドロキシブチルアミノ]-ベンズアミド;
2-(3-ジエチルアミノ-プロピルアミノ)-N-ピリジン-4-イル-ニコチンアミド;
2-(3-イミダゾール-1-イル-プロピルアミノ)-N-ピリジン-4イル-ニコチンアミド;
2-(3-ジメチルアミノ-プロピルアミノ)-N-(3-メトキシ-フェニル)-ニコチンアミド;
2-(2-ジメチルアミノ-エチルアミノ)-N-(3-メトキシ-フェニル)-ニコチンアミド;
2-(2-ジエチルアミノ-エチルアミノ)-N-(3-メトキシ-フェニル)-ニコチンアミド;
2-(3-ジエチルアミノ-プロピルアミノ)-N-(3-メトキシ-フェニル)-ニコチンアミド;
2-(4-ヒドロキシ-ブチルアミノ)-N-(3-メトキシ-フェニル)-ニコチンアミド;
2-(5-ヒドロキシ-ペンチルアミノ)-N-(3-メトキシ-フェニル)-ニコチンアミド;
2-(6-アミノ-ヘキシルアミノ)-N-(3-メトキシ-フェニル)-ニコチンアミド;
2-(3-イミダゾール-1-イル-プロピルアミノ)-N-(3-メトキシ-フェニル)-ニコチンアミド;
2-(2-ジメチルアミノ-エチルアミノ)-N-(3-メトキシ-フェニル)-ベンズアミド;
2-(2-ジエチルアミノ-エチルアミノ)-N-(3-メトキシ-フェニル)-ベンズアミド;
2-(4-ヒドロキシ-ブチルアミノ)-N-(3-メトキシ-フェニル)-ベンズアミド;
2-(4-ジエチルアミノ-1-メチル-ブチルアミノ)-N-(3-メトキシ-フェニル)-ベンズアミド;
2-(2-ジエチルアミノ-エチルアミノ)-N-ピリジン-4-イル-ベンズアミド;
2-(2-ジメチルアミノ-プロピルアミノ)-N-ピリジン-4-イル-ベンズアミド;
2-(3-ジエチルアミノ-プロピルアミノ)-N-ピリジン-4-イル-ベンズアミド;
2-(3-イミダゾール-1-イル-プロピルアミノ)-N-ピリジン-4-イル-ベンズアミド;
2-(2-ジエチルアミノ-エチルアミノ)-N-ピリジン-4-イル-ニコチンアミド ; 及び
2-(3-ジメチルアミノ-プロピルアミノ)-N-ピリジン-4-イル-ニコチンアミド
を含む群のうちから選ばれるものである、請求項4の化合物。 - 式(Ia)を有する、請求項1の化合物。
- N-(4-メトキシ-フェニル)-2-[6-(N'-(4-メトキシ-フェニルニコチンアミド)-ピリジン-2-イルアミノ)-ヘキシルアミノ]-ニコチンアミド;
2-(2-ジメチルアミノ-エチルアミノ)-N-(4-トリフルオロメトキシ-フェニル)-ニコチンアミド;
2-(3-ジメチルアミノ-プロピルアミノ)-N-(4-トリフルオロメトキシ-フェニル)-ニコチンアミド;
2-(3-ジエチルアミノ-プロピルアミノ)-N-(4-トリフルオロメトキシ-フェニル)-ニコチンアミド;
2-(4-ヒドロキシ-ブチルアミノ)-N-(4-トリフルオロメトキシ-フェニル)-ニコチンアミド;
N-(4-トリフルオロメトキシ-フェニル)-2-[6-(N'-(4-トリフルオロメトキシ-フェニルニコチンアミド)-ピリジン-2-イルアミノ)-ヘキシルアミノ]-ニコチンアミド;
2-(2-ジメチルアミノ-エチルアミノ)-N-(4-メトキシ-フェニル)-ニコチンアミド ;
2-(2-ジメチルアミノ-エチルアミノ)-N-(4-メトキシ-フェニル)-ベンズアミド;
2-(3-ジエチルアミノ-エチルアミノ)-N-(4-メトキシ-フェニル)-ベンズアミド;
2-(3-ジメチルアミノ-プロピルアミノ)-N-(4-メトキシ-フェニル)-ベンズアミド;
2-(4-ヒドロキシ-ブチルアミノ)-N-(4-メトキシ-フェニル)-ベンズアミド;
2-(3-イミダゾール-1-イル-プロピルアミノ)-N-(4-メトキシ-フェニル)-ベンズアミド;
2-(3-イミダゾール-1-イル-プロピルアミノ)-N-(4-トリフルオロメトキシ-フェニル)-ニコチンアミド;
2-(2-ジエチルアミノ-エチルアミノ)-N-(4-トリフルオロメトキシ-フェニル)-ベンズアミド;
2-(3-ジメチルアミノ-プロピルアミノ)-N-(4-トリフルオロメトキシ-フェニル)-ベンズアミド;
2-(3-ジエチルアミノ-プロピルアミノ)-N-(4-トリフルオロメトキシ-フェニル)-ベンズアミド;
2-(4-ヒドロキシ-ブチルアミノ)-N-(4-トリフルオロメトキシ-フェニル)-ベンズアミド;
2-(6-アミノ-ヘキシルアミノ)-N-(4-トリフルオロメトキシ-フェニル)-ベンズアミド;
2-(3-イミダゾール-1-イル-プロピルアミノ)-N-(4-トリフルオロメトキシ-フェニル)-ベンズアミド; 及び
2-(4-ジエチルアミノ-1-メチル-ブチルアミノ)-N-(4-トリフルオロメトキシ-フェニル)-ベンズアミド
を含む群のうちから選ばれるものである、請求項6の化合物。 - 式(IX)を有する、請求項1の化合物。
- 2-(1-(4-((E)-2-(4-メトキシフェニル)ビニル)-フェニル)-1H-1,2,3-トリアゾール-4-イル)-プロパン-2-オール;
N-(3-ジエチルアミノ-プロピル)-3-[4-((E)-2-ピリジン-4-イル-ビニル)-フェニルアミノ]-ベンズアミド;
N-(3-メチル-ブチル)-3-[4-((E)-2-ピリジン-4-イル-ビニル)-フェニルアミノ]-ベンズアミド;
(N-ジエチルアミノ)-3-(1-{3-[4-((E)-2-ピリジン-4-イル-ビニル)-フェニルアミノ]-フェニル}-1H-1,2,3-トリアゾール-4-イル)-メチルアミン;
3-(1-{3-[4-((E)-2-ピリジン-4-イル-ビニル)-フェニルアミノ]-フェニル}-1H-1,2,3-トリアゾール-4-イル)-プロパン-1-オール;
N-(3-ジエチルアミノ-プロピル)-3-メチル-4-[4-((E)-2-ピリジン-4-イル-ビニル)-フェニルアミノ]-ベンズアミド;
3-メチル-N-(3-メチル-ブチル)-4-[4-((E)-2-ピリジン-4-イル-ビニル)-フェニルアミノ]-ベンズアミド;
3-(1-{4-[4-((E)-2-ピリジン-4-イル-ビニル)-フェニルアミノ]-フェニル}-1H-1,2,3-トリアゾール-4-イル)-プロパン-1-オール;
4-メチル-N-(3-メチル-ブチル)-3-[3-((E)-2-ピリジン-4-イル-ビニル)-フェニルアミノ]-ベンズアミド;
N-(3-ジエチルアミノ-プロピル)-3-[3-((E)-2-ピリジン-4-イル-ビニル)-フェニルアミノ]-ベンズアミド;
N-(3-メチル-ブチル)-3-[3-((E)-2-ピリジン-4-イル-ビニル)-フェニルアミノ]-ベンズアミド;
(N-ジエチルアミノ)-3-(1-{3-[3-((E)-2-ピリジン-4-イル-ビニル)-フェニルアミノ]-フェニル}-1H-1,2,3-トリアゾール-4-イル)-メチルアミン;
3-(1-{3-[3-((E)-2-ピリジン-4-イル-ビニル)-フェニルアミノ]-フェニル}-1H-1,2,3-トリアゾール-4-イル)-プロパン-1-オール;
N-(3-ジエチルアミノ-プロピル)-3-メチル-4-[3-((E)-2-ピリジン-4-イル-ビニル)-フェニルアミノ]-ベンズアミド;
N-(3-メチル-ブチル)-4-[3-((E)-2-ピリジン-4-イル-ビニル)-フェニルアミノ]-ベンズアミド;
N-(4-ヒドロキシ-ブチル)-3-(2-(4-メトキシフェニル)-ビニル)-ベンズアミド;
N-(3-ジエチルアミノール-プロピル)-3-[3-((E)-(4-メトキシ-スチリル)-フェニルアミノ]-ベンズアミド;
N-(3-メチル-ブチル)-3-[3-((E)-(4-メトキシ-スチリル)-フェニルアミノ]-ベンズアミド;
N-(3-ジエチルアミノール-プロピル)-3-メチル-4-[3-((E)-(4-メトキシ-スチリル)-フェニルアミノ]-ベンズアミド;
N-(3-メチル-ブチル)-3-メチル-4-[3-((E)-(4-メトキシ-スチリル)-フェニルアミノ]-ベンズアミド;
N-(3-メチル-ブチル)-4-[3-((E)-(4-メトキシ-スチリル)-フェニルアミノ]-ベンズアミド
を含む群のうちから選ばれるものである、請求項8の化合物。 - 請求項1〜9のいずれか1項の少なくとも1つの化合物を含む医薬組成物。
- 細胞内のプレメッセンジャーRNAをスプライシングするプロセスに関連する疾患を、対象において処置する為の剤であって、請求項1〜9のいずれか1項の少なくとも1つの化合物を含み、該疾患が、スプライシングプロセスの変化からもたらされる遺伝子疾患であり、該疾患がFrasier症候群、17番染色体に関係した前頭側頭型認知症、Leigh症候群、非定型嚢胞性線維症、神経病理、生存運動ニューロン遺伝子に影響する筋萎縮症、セロトニンスプライシングの調節不全に関係したうつ、及び全体のスプライシングプロセスが影響される転移性ガンを含む群のうちから選ばれるものである、前記剤。
- 該疾患がガンであり、該ガンが、乳ガン、大腸ガン、膵臓ガン、肝臓ガン、前立腺ガン及び子宮ガンを含む群において選ばれるものである、請求項11の剤。
- 細胞内のプレメッセンジャーRNAをスプライシングするプロセスに関連する疾患を、対象において処置する為の剤であって、請求項1〜9のいずれか1項の少なくとも1つの化合物を含み、該疾患が老化とともに現れ、該疾患がアテローム性動脈硬化症、インスリン抵抗性II型糖尿病、白内障、骨粗しょう症及び皮膚の老化を含む群のうちから選ばれるものである、前記剤。
- 細胞内のプレメッセンジャーRNAをスプライシングするプロセスに関連する疾患を、対象において処置する為の剤であって、請求項1〜9のいずれか1項の少なくとも1つの化合物を含み、該疾患が、ウィルス由来の疾患である、前記剤。
- 対象において、遺伝子変異に関連した疾患を処置する為の剤であって、請求項1〜9のいずれか1項の少なくとも1つの化合物を含み、該疾患が、エキソンスキッピングにより処置されうる疾患である、前記剤。
- R11及びR12が、互に独立に、メチル基を表す、請求項1の式Ia及びIVの化合物。
- R1がOR12基を表す場合に、X1がCH基を表す、請求項1の式Iaの化合物。
- R1がOCH3基を表す場合に、X1がCH基を表す、請求項1の式Ia及びIIIaの化合物。
- R4が、水素原子又はメチル基又はC(=O)NR14R15基を表す、請求項1の式IVの化合物。
- R6がC(=O)NR14R15基を表す、請求項1の式IV及びIXの化合物。
- 医薬的に許容できる担体を含む、請求項10の医薬組成物。
- 前記神経病理が、Tauタンパク質の変異に関係したアルツハイマー病である、請求項11の剤。
- 前記転移性ガンが、乳ガン、大腸ガン、膵臓ガン、肝臓ガン、前立腺ガン、子宮ガン及び或るリンパ腫を含む上皮ガンにおけるものである、請求項11の剤。
- 該疾患がAIDSである、請求項14の剤。
- 該疾患がデュシェンヌ型筋ジストロフィー(DMD)である、請求項15の剤。
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US8367669B2 (en) | 2005-06-15 | 2013-02-05 | Vanderbilt University | Inhibitors of hemeprotein-catalyzed lipid peroxidation |
US9133212B1 (en) | 2005-06-15 | 2015-09-15 | Vanderbilt University | Inhibitors of hemeprotein-catalyzed lipid peroxidation |
FR2926297B1 (fr) | 2008-01-10 | 2013-03-08 | Centre Nat Rech Scient | Molecules chimiques inhibitrices du mecanisme d'epissage pour traiter des maladies resultant d'anomalies d'epissage. |
TW201103904A (en) | 2009-06-11 | 2011-02-01 | Hoffmann La Roche | Janus kinase inhibitor compounds and methods |
CN106905232B (zh) | 2009-06-12 | 2019-09-27 | Abivax公司 | 用于治疗过早衰老和尤其是早衰的化合物 |
EP2266972A1 (en) * | 2009-06-12 | 2010-12-29 | Splicos | New chemical molecules that inhibit the splicing mechanism for treating diseases resulting from splicing anomalies |
US10253020B2 (en) | 2009-06-12 | 2019-04-09 | Abivax | Compounds for preventing, inhibiting, or treating cancer, AIDS and/or premature aging |
DK2488486T3 (da) * | 2009-10-13 | 2019-11-18 | Ligand Pharm Inc | Småmolekylære forbindelser der efterligner hæmapoetisk vækstfaktor og anvendelse deraf |
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