JP2021512078A - Gcn2阻害剤およびその使用 - Google Patents
Gcn2阻害剤およびその使用 Download PDFInfo
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- JP2021512078A JP2021512078A JP2020541375A JP2020541375A JP2021512078A JP 2021512078 A JP2021512078 A JP 2021512078A JP 2020541375 A JP2020541375 A JP 2020541375A JP 2020541375 A JP2020541375 A JP 2020541375A JP 2021512078 A JP2021512078 A JP 2021512078A
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- 229940033942 zoladex Drugs 0.000 description 1
- CGTADGCBEXYWNE-JUKNQOCSSA-N zotarolimus Chemical compound N1([C@H]2CC[C@@H](C[C@@H](C)[C@H]3OC(=O)[C@@H]4CCCCN4C(=O)C(=O)[C@@]4(O)[C@H](C)CC[C@H](O4)C[C@@H](/C(C)=C/C=C/C=C/[C@@H](C)C[C@@H](C)C(=O)[C@H](OC)[C@H](O)/C(C)=C/[C@@H](C)C(=O)C3)OC)C[C@H]2OC)C=NN=N1 CGTADGCBEXYWNE-JUKNQOCSSA-N 0.000 description 1
- 229950009819 zotarolimus Drugs 0.000 description 1
- 229940039925 zyprexa Drugs 0.000 description 1
- 229940051084 zytiga Drugs 0.000 description 1
- 239000002076 α-tocopherol Substances 0.000 description 1
- 235000004835 α-tocopherol Nutrition 0.000 description 1
- 235000019145 α-tocotrienol Nutrition 0.000 description 1
- 150000003773 α-tocotrienols Chemical class 0.000 description 1
- 239000002478 γ-tocopherol Substances 0.000 description 1
- QUEDXNHFTDJVIY-DQCZWYHMSA-N γ-tocopherol Chemical compound OC1=C(C)C(C)=C2O[C@@](CCC[C@H](C)CCC[C@H](C)CCCC(C)C)(C)CCC2=C1 QUEDXNHFTDJVIY-DQCZWYHMSA-N 0.000 description 1
- 235000019150 γ-tocotrienol Nutrition 0.000 description 1
- 150000003786 γ-tocotrienols Chemical class 0.000 description 1
- 239000002446 δ-tocopherol Substances 0.000 description 1
- 235000019144 δ-tocotrienol Nutrition 0.000 description 1
- 150000003790 δ-tocotrienols Chemical class 0.000 description 1
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Abstract
Description
本願は、米国特許法第119条第(e)項の下で、米国仮出願第62/623,312号(2018年1月29日出願)の利益を主張する。この米国仮出願の内容は、その全体が本明細書中に参考として援用される。
発明の技術分野
GCN2(一般アミノ酸制御必須2)は、真核生物でのアミノ酸欠損への細胞応答に関与する、遍在的に発現されるプロテインキナーゼである(Castilho et al.,2014)。細胞での、1つまたはそれより多くのアミノ酸の欠損は、非荷電のコグネイト転移RNA(tRNA)の蓄積を引き起こし、これらは、GCN2により直接結合されて、キナーゼの活性化、および真核生物開始因子2α(eIF2α)のセリン51でのリン酸化をもたらす(Wek et al.,1989;Dong et al.,2000)。eIF2αのリン酸化は、タンパク質翻訳の開始をもたらし、これは、大部分のmRNAの翻訳の減少を引き起こして、アミノ酸の全体的な利用の低下をもたらす。同時に、eIF2αリン酸化は、mRNAの、特定の上流オープンリーディングフレームをそれらの5’未翻訳領域(5’−UTR)に含む特定のサブセット(例えば、哺乳動物の転写因子ATF4(Vattem and Wek,2004))の翻訳を増大させ、これは、タンパク質ホメオスタシスの修復を促進する。従って、GCN2は、アミノ酸消耗に応答する細胞の発生運命の重大な決定因子である。
本発明の化合物およびその薬学的に受容可能な組成物は、GCN2キナーゼの阻害剤として有効であることが、ここで見出された。このような化合物は、一般式I:
1.本発明の特定の実施形態の一般的な説明:
本発明の化合物およびその組成物は、GCN2プロテインキナーゼの阻害剤として有用である。いくつかの実施形態において、提供される化合物は、GCN2を阻害する。
環Aは、3員〜8員の飽和もしくは部分不飽和の単環式炭素環式環、フェニル、8員〜10員の二環式芳香族炭素環式環、窒素、酸素、もしくは硫黄から独立して選択される0個〜4個のヘテロ原子を有する5〜6員の芳香環と必要に応じて縮合し、窒素、酸素、もしくは硫黄から独立して選択される1個〜2個のヘテロ原子を有する、4員〜8員の部分不飽和単環式複素環式環、窒素、酸素、もしくは硫黄から独立して選択される1個〜2個のヘテロ原子を有する7員〜12員の部分不飽和スピロ環式複素環式環、窒素、酸素、もしくは硫黄から独立して選択される1個〜4個のヘテロ原子を有する7員〜12員の部分不飽和二環式複素環式環、窒素、酸素、もしくは硫黄から独立して選択される1個〜2個のヘテロ原子を有する7員〜12員の部分不飽和架橋二環式複素環式環、窒素、酸素、もしくは硫黄から独立して選択される1個〜4個のヘテロ原子を有する5員〜6員の単環式ヘテロ芳香環、窒素、酸素、もしくは硫黄から独立して選択される1個〜5個のヘテロ原子を有する8員〜10員の二環式ヘテロ芳香環、または
Hetから選択され、ここでHetは、窒素、酸素、もしくは硫黄から独立して選択される1個〜2個のヘテロ原子を有する4員〜8員の飽和単環式複素環式環、窒素、酸素、もしくは硫黄から独立して選択される1個〜4個のヘテロ原子を有する7員〜12員の飽和スピロ環式複素環式環、窒素、酸素、もしくは硫黄から独立して選択される1個〜3個のヘテロ原子を有する7員〜12員の飽和二環式複素環式環、または窒素、酸素、もしくは硫黄から独立して選択される1個〜2個のヘテロ原子を有する7員〜12員の飽和架橋二環式複素環式環であり;
環Bは、
各Rは独立して、水素であるか、またはC1〜6脂肪族、3員〜8員の飽和もしくは部分不飽和の単環式炭素環式環、フェニル、8員〜10員の二環式芳香族炭素環式環、窒素、酸素、もしくは硫黄から独立して選択される1個〜2個のヘテロ原子を有する4員〜8員の飽和もしくは部分不飽和の単環式複素環式環、窒素、酸素、もしくは硫黄から独立して選択される1個〜4個のヘテロ原子を有する5員〜6員の単環式ヘテロ芳香環、または窒素、酸素、もしくは硫黄から独立して選択される1個〜5個のヘテロ原子を有する8員〜10員の二環式ヘテロ芳香環から選択される必要に応じて置換された基であるか;あるいは
2個のR基は必要に応じて一緒になって、二価C2〜4アルキレン鎖を形成し;
2個のR基は、これらの間にある原子と必要に応じて一緒になって、窒素、酸素もしくは硫黄から独立して選択される0個〜4個のヘテロ原子を有する必要に応じて置換された3員〜7員の飽和もしくは部分不飽和の単環式環を形成し;
各R’は独立して、水素、またはハロゲンで必要に応じて置換されたC1〜3脂肪族基であり;
R1の各々は独立して、水素、ハロゲン、−CN、−NO2、−C(O)R、−C(O)OR、−C(O)NR2、−C(O)NRS(O)2R、−C(O)N=S(O)R2、−NR2、−NRC(O)R、−NRC(O)NR2、−NRC(O)OR、−NRS(O)2R、−NRS(O)2NR2、−OR、−ON(R)SO2R、−P(O)R2、−SR、−S(O)R、−S(O)2R、−S(O)(NH)R、−S(O)2N(R)2、−S(NH2)2(O)OH、−N=S(O)R2、−CH3、−CH2OH、−CH2NHSO2CH3、−CH3、−CH2OH、−CH2NHSO2CH3、−CD3、−CD2NRS(O)2R、またはRであるか;あるいは:
2個のR1基は必要に応じて一緒になって、=Oまたは=NHを形成するか;あるいは
2個のR1基は必要に応じて一緒になって、二価C2〜4アルキレン鎖を形成し;
R2の各々は独立して、水素、ハロゲン、−CN、−C(O)N(R’)2、−OR’、−N(R’)2、−S(O)2R、−S(O)2N(R)2、−O−フェニル、または必要に応じて置換された基であり、この必要に応じて置換された基は、C1〜3脂肪族、フェニル、窒素、酸素、もしくは硫黄から独立して選択される1個〜4個のヘテロ原子を有する5員〜6員の単環式ヘテロ芳香環、または窒素、酸素、もしくは硫黄から独立して選択される1個〜4個のヘテロ原子を有する4員〜8員の飽和単環式複素環から選択され;
R3は、水素、ハロゲン、−CN、−OR’、−N(R’)2、または必要に応じて置換された基であり、この必要に応じて置換された基は、C1〜3脂肪族、フェニル、または窒素、酸素、もしくは硫黄から独立して選択される1個〜4個のヘテロ原子を有する5員〜6員の単環式ヘテロ芳香環から選択され;
R4は、水素、ハロゲン、−CN、−OR、−N=S(O)R2、−N(R)2、または必要に応じて置換された基であり、この必要に応じて置換された基は、C1〜3脂肪族、窒素、酸素、もしくは硫黄から独立して選択される1個〜2個のヘテロ原子を有する4員〜8員の飽和もしくは部分不飽和の単環式複素環式環、または窒素、酸素、もしくは硫黄から独立して選択される1個〜2個のヘテロ原子を有する7員〜12員の飽和もしくは部分不飽和のスピロ環式複素環式環から選択され;
mは、0、1、2、3、4または5であり;
nは、0、1、または2であり;
pは、0または1であり;そして
qは、0または1である。
2.化合物および定義:
3.例示的な実施形態の説明:
環Aは、3員〜8員の飽和もしくは部分不飽和の単環式炭素環式環、フェニル、8員〜10員の二環式芳香族炭素環式環、窒素、酸素、もしくは硫黄から独立して選択される0個〜4個のヘテロ原子を有する5〜6員の芳香環と必要に応じて縮合し、窒素、酸素、もしくは硫黄から独立して選択される1個〜2個のヘテロ原子を有する、4員〜8員の部分不飽和単環式複素環式環、窒素、酸素、もしくは硫黄から独立して選択される1個〜2個のヘテロ原子を有する7員〜12員の部分不飽和スピロ環式複素環式環、窒素、酸素、もしくは硫黄から独立して選択される1個〜4個のヘテロ原子を有する7員〜12員の部分不飽和二環式複素環式環、窒素、酸素、もしくは硫黄から独立して選択される1個〜2個のヘテロ原子を有する7員〜12員の部分不飽和架橋二環式複素環式環、窒素、酸素、もしくは硫黄から独立して選択される1個〜4個のヘテロ原子を有する5員〜6員の単環式ヘテロ芳香環、窒素、酸素、もしくは硫黄から独立して選択される1個〜5個のヘテロ原子を有する8員〜10員の二環式ヘテロ芳香環、または
Hetから選択され、ここでHetは、窒素、酸素、もしくは硫黄から独立して選択される1個〜2個のヘテロ原子を有する4員〜8員の飽和単環式複素環式環、窒素、酸素、もしくは硫黄から独立して選択される1個〜4個のヘテロ原子を有する7員〜12員の飽和スピロ環式複素環式環、窒素、酸素、もしくは硫黄から独立して選択される1個〜3個のヘテロ原子を有する7員〜12員の飽和二環式複素環式環、または窒素、酸素、もしくは硫黄から独立して選択される1個〜2個のヘテロ原子を有する7員〜12員の飽和架橋二環式複素環式環であり;
環Bは、
各Rは独立して、水素であるか、またはC1〜6脂肪族、3員〜8員の飽和もしくは部分不飽和の単環式炭素環式環、フェニル、8員〜10員の二環式芳香族炭素環式環、窒素、酸素、もしくは硫黄から独立して選択される1個〜2個のヘテロ原子を有する4員〜8員の飽和もしくは部分不飽和の単環式複素環式環、窒素、酸素、もしくは硫黄から独立して選択される1個〜4個のヘテロ原子を有する5員〜6員の単環式ヘテロ芳香環、または窒素、酸素、もしくは硫黄から独立して選択される1個〜5個のヘテロ原子を有する8員〜10員の二環式ヘテロ芳香環から選択される必要に応じて置換された基であるか;あるいは
2個のR基は必要に応じて一緒になって、二価C2〜4アルキレン鎖を形成し;
2個のR基は、これらの間にある原子と必要に応じて一緒になって、窒素、酸素もしくは硫黄から独立して選択される0個〜4個のヘテロ原子を有する必要に応じて置換された3員〜7員の飽和もしくは部分不飽和の単環式環を形成し;
各R’は独立して、水素、またはハロゲンで必要に応じて置換されたC1〜3脂肪族基であり;
R1の各々は独立して、水素、ハロゲン、−CN、−NO2、−C(O)R、−C(O)OR、−C(O)NR2、−C(O)NRS(O)2R、−C(O)N=S(O)R2、−NR2、−NRC(O)R、−NRC(O)NR2、−NRC(O)OR、−NRS(O)2R、−NRS(O)2NR2、−OR、−ON(R)SO2R、−P(O)R2、−SR、−S(O)R、−S(O)2R、−S(O)(NH)R、−S(O)2N(R)2、−S(NH2)2(O)OH、−N=S(O)R2、−CH3、−CH2OH、−CH2NHSO2CH3、−CD3、−CD2NRS(O)2R、またはRであるか;あるいは:
2個のR1基は必要に応じて一緒になって、=Oまたは=NHを形成するか;あるいは
2個のR1基は必要に応じて一緒になって、二価C2〜4アルキレン鎖を形成し;
R2の各々は独立して、水素、ハロゲン、−CN、−C(O)N(R’)2、−OR’、−N(R’)2、−S(O)2R、−S(O)2N(R)2、−O−フェニル、または必要に応じて置換された基であり、この必要に応じて置換された基は、C1〜3脂肪族、フェニル、窒素、酸素、もしくは硫黄から独立して選択される1個〜4個のヘテロ原子を有する5員〜6員の単環式ヘテロ芳香環、または窒素、酸素、もしくは硫黄から独立して選択される1個〜4個のヘテロ原子を有する4員〜8員の飽和単環式複素環から選択され;
R3は、水素、ハロゲン、−CN、−OR’、−N(R’)2、または必要に応じて置換された基であり、この必要に応じて置換された基は、C1〜3脂肪族、フェニル、または窒素、酸素、もしくは硫黄から独立して選択される1個〜4個のヘテロ原子を有する5員〜6員の単環式ヘテロ芳香環から選択され;
R4は、水素、ハロゲン、−CN、−OR、−N=S(O)R2、−N(R)2、または必要に応じて置換された基であり、この必要に応じて置換された基は、C1〜3脂肪族、窒素、酸素、もしくは硫黄から独立して選択される1個〜2個のヘテロ原子を有する4員〜8員の飽和もしくは部分不飽和の単環式複素環式環、または窒素、酸素、もしくは硫黄から独立して選択される1個〜2個のヘテロ原子を有する7員〜12員の飽和もしくは部分不飽和のスピロ環式複素環式環から選択され;
mは、0、1、2、3、4または5であり;
nは、0、1、または2であり;
pは、0または1であり;そして
qは、0または1である。
4.本化合物を得る一般的な方法:
5.使用、製剤化および投与
a.薬学的に受容可能な組成物
b.化合物および薬学的に受容可能な組成物の使用
c. 併用療法
[0100]
用語「生物学的サンプル」には、本明細書で使用する場合、非限定的に、細胞培養物またはその抽出物;哺乳動物またはその抽出物から得られた生検物質;および血液、唾液、尿、大便、精液、涙液もしくは他の体液またはその抽出物が含まれる。
例示的な腫瘍免疫剤
例示的な免疫チェックポイント阻害剤
以下の実施例に図示されている通り、ある種の例示的な実施形態において、化合物は、以下の一般手順に従い調製する。一般的方法は、本発明のある種の化合物の合成を図示しているが、以下の一般的方法および当業者に公知の他の方法を、本明細書に記載されているようなすべての化合物、ならびにこれらの化合物の各々の部分クラスおよび種に適用することができることが理解されよう。
調製1: 3−(4−メチルスルファニルピリミジン−2−イル)−6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン
6−クロロ−3−(4−メチルスルファニルピリミジン−2−イル)イミダゾ[1,2−a]ピリジン、5−クロロピリジン−2−アミンを使用;
6−クロロ−7−フルオロ−3−(4−メチルスルファニルピリミジン−2−イル)イミダゾ[1,2−a]ピリジン、5−クロロ−4−フルオロ−ピリジン−2−アミンを使用;
6−ブロモ−7−フルオロ−3−(4−メチルスルファニルピリミジン−2−イル)イミダゾ[1,2−a]ピリジン、5−ブロモ−4−フルオロ−ピリジン−2−アミンを使用;
6−クロロ−7−フルオロ−3−(4−(メチルチオ)ピリミジン−2−イル)イミダゾ[1,2−a]ピリジン、5−クロロ−4−フルオロピリジン−2−アミンを使用。
調製2: 3−(4−クロロピリミジン−2−イル)−6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン
6−クロロ−3−(4−クロロピリミジン−2−イル)イミダゾ[1,2−a]ピリジン、6−クロロ−3−(4−メチルスルファニルピリミジン−2−イル)イミダゾ[1,2−a]ピリジンを使用;
6−クロロ−3−(4−クロロピリミジン−2−イル)−7−フルオロ−イミダゾ[1,2−a]ピリジン、6−クロロ−7−フルオロ−3−(4−メチルスルファニルピリミジン−2−イル)イミダゾ[1,2−a]ピリジンを使用;
6−ブロモ−3−(4−クロロピリミジン−2−イル)−7−フルオロ−イミダゾ[1,2−a]ピリジン、6−ブロモ−7−フルオロ−3−(4−メチルスルファニルピリミジン−2−イル)イミダゾ[1,2−a]ピリジンを使用;
6−クロロ−3−(4−クロロピリミジン−2−イル)−7−フルオロ−イミダゾ[1,2−a]ピリジン、6−クロロ−7−フルオロ−3−(4−(メチルチオ)ピリミジン−2−イル)イミダゾ[1,2−a]ピリジンを使用。
4−クロロ−2−{6−フェノキシイミダゾ[1,2−a]ピリジン−3−イル}ピリミジン
4−クロロ−2−{6−メタンスルホニルイミダゾ[1,2−a]ピリジン−3−イル}ピリミジン
3−(4−クロロピリミジン−2−イル)−N−シクロプロピルイミダゾ[1,2−a]ピリジン−6−スルホンアミド
3−(4−クロロピリミジン−2−イル)イミダゾ[1,2−a]ピリジン−6−スルホンアミド
調製3: 3−ブロモ−6−(ジフルオロメチル)イミダゾ[1,2−a]ピリジン
調製4: 2−[6−(ジフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル]ピリミジン−4−オール
工程2: 2−[6−(ジフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル]ピリミジン−4−オール
調製5: 3−(2−クロロピリミジン−4−イル)−6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン
調製6: N−[[(2S)−モルホリン−2−イル]メチル]メタンスルホンアミド
工程2: N-[[(2S)-モルホリン-2-イル]メチル]メタンスルホンアミド
調製7: 2-(1H-ピラゾール-4-イル)モルホリン
工程2: 2-(1H-ピラゾール-4-イル)モルホリン
調製8: 2-メチル-6-(1H-ピラゾール-4-イル)モルホリン。
調製9: イミノ(メチル)(ピペリジン-3-イルメチル)-λ6-スルファノン
調製10: イミノ(メチル)(ピペリジン-3-イルメチル)-λ6-スルファノン
調製11: 2,5-ジメチル-3-((メチルスルフィニル)メチル)ピペリジン
工程2: 3-(ヒドロキシメチル)-2,5-ジメチルピペリジン-1-カルボン酸tert-ブチル
工程3: 2,5-ジメチル-3-(((メチルスルホニル)オキシ)メチル)ピペリジン-1-カルボン酸tert-ブチル
工程4: 2,5-ジメチル-3-((メチルチオ)メチル)ピペリジン-1-カルボン酸tert-ブチル
工程5: 2,5-ジメチル-3-((メチルスルフィニル)メチル)ピペリジン-1-カルボン酸tert-ブチル
工程6: 2,5-ジメチル-3-((メチルスルフィニル)メチル)ピペリジン
調製12: 2-(1H-ピラゾール-4-イル)ピペラジン
調製13: 2,5-ジメチル-3-(1H-ピラゾール-4-イル)ピペラジン
2-メチル-6-(1H-ピラゾール-4-イル)ピペラジン;
3-(1H-イミダゾール-4-イル)-2,5-ジメチルピペラジン。
調製14: ジメチル((5-メチルピペリジン-3-イル)イミノ)-λ6-スルファノン
工程2: 1-ベンジル-3-((ジメチル(オキソ)-λ6-スルファニリデン)アミノ)-5-メチルピリジン-1-イウムブロミド
工程3: ((1-ベンジル-,5-メチル-1,2,5,6-テトラヒドロピリジン-3-イル)イミノ)ジメチル-λ6-スルファノン
工程4: ジメチル((5-メチルピペリジン-3-イル)イミノ)-λ6-スルファノン
ジメチル((ピペリジン-3-イル)イミノ)-λ6-スルファノン。
調製15: 2,5-ジメチルピペリジン-3-カルボキサミド
工程2: 2,5-ジメチルピペリジン-3-カルボキサミド
調製16: N-(((3S,5S)-4,4-ジフルオロ-5-メチルピペリジン-3-イル)メチル)メタンスルホンアミド
工程2: (3R,5S)-3-[(1,3-ジオキソイソインドリン-2-イル)メチル]-4,4-ジフルオロ-5-メチル-ピペリジン-1-カルボン酸ベンジル
工程3: (3R,5S)-3-(アミノメチル)-4,4-ジフルオロ-5-メチル-ピペリジン-1-カルボン酸ベンジル
工程4: (3S,5S)-4,4-ジフルオロ-3-(メタンスルホンアミドメチル)-5-メチル-ピペリジン-1-カルボン酸ベンジル
工程5: N−(((3S,5S)−4,4−ジフルオロ−5−メチルピペリジン−3−イル)メチル)メタンスルホンアミド
調製17: N−(ピロリジン−3−イルメチル)メタンスルホンアミド
工程2: N−(ピロリジン−3−イルメチル)メタンスルホンアミド
調製18: 4−ピロリジン−3−イル−1H−ピラゾール
工程2および3: 4−ピロリジン−3−イル−1H−ピラゾール
調製19: (E)−2−(2−エトキシビニル)−4−(メチルチオ)ピリミジン
調製20: 2−クロロ−4−{6−シクロプロピルイミダゾ[1,2−a]ピリジン−3−イル}ピリミジン
2−クロロ−4−{6−クロロイミダゾ[1,2−a]ピリジン−3−イル}ピリミジン
調製22: 2−クロロ−4−[6−(3,3−ジフルオロアゼチジン−1−イル)イミダゾ[1,2−a]ピリジン−3−イル]−6−メチルピリミジン
2−クロロ−4−[6−(3−フルオロアゼチジン−1−イル)イミダゾ[1,2−a]ピリジン−3−イル]ピリミジン
調製23: 5−[6−(アゼチジン−1−イル)イミダゾ[1,2−a]ピリジン−3−イル]−2−クロロピリミジン
調製24: 5−(3−メチル−1H−ピラゾール−4−イル)ピペリジン−3−オール
3−(3−フルオロ−1H−ピラゾール−4−イル)−5−メチルピペリジン
8−メチルスルホニル−1−[2−[6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル]ピリミジン−4−イル]−1,8−ジアザスピロ[4.5]デカン、I−7
N−[[−4,4−ジフルオロ−5−メチル−1−[2−[6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル]ピリミジン−4−イル]−3−ピペリジル]メチル]メタンスルホンアミド、I−8
N−[[(2S)−4−[2−(6−クロロイミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル]モルホリン−2−イル]メチル]メタンスルホンアミド、I−19(6−クロロ−3−(4−クロロピリミジン−2−イル)イミダゾ[1,2−a]ピリジンを使用)
4−[2−(6−クロロイミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル]−2−(1H−ピラゾール−4−イル)モルホリン、I−20(6−クロロ−3−(4−クロロピリミジン−2−イル)イミダゾ[1,2−a]ピリジンを使用)
6−クロロ−3−(4−(3−((メチルスルホンイミドイル)メチル)ピペリジン−1−イル)ピリミジン−2−イル)イミダゾ[1,2−a]ピリジン、I−21(6−クロロ−3−(4−クロロピリミジン−2−イル)イミダゾ[1,2−a]ピリジンを使用)
4−[2−(6−クロロ−7−フルオロ−イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル]−2−(1H−ピラゾール−4−イル)モルホリン、I−23(6−クロロ−3−(4−クロロピリミジン−2−イル)−7−フルオロ−イミダゾ[1,2−a]ピリジンを使用)
4−[2−(6−ブロモ−7−フルオロ−イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル]−2−(1H−ピラゾール−4−イル)モルホリン、I−24(6−ブロモ−7−フルオロ−3−(4−メチルスルファニルピリミジン−2−イル)イミダゾ[1,2−a]ピリジンを使用)
N−[[1−[2−(6−ブロモ−7−フルオロ−イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル]ピロリジン−3−イル]メチル]メタンスルホンアミド I−25(6−ブロモ−7−フルオロ−3−(4−メチルスルファニルピリミジン−2−イル)イミダゾ[1,2−a]ピリジンを使用)
1−[2−(6−クロロイミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル]−1,4−ジアゼパン−5−オン I−26(6−クロロ−3−(4−クロロピリミジン−2−イル)イミダゾ[1,2−a]ピリジンを使用);
6−クロロ−3−[4−[3−(1H−ピラゾール−4−イル)ピロリジン−1−イル]ピリミジン−2−イル]イミダゾ[1,2−a]ピリジン I−27(6−クロロ−3−(4−クロロピリミジン−2−イル)イミダゾ[1,2−a]ピリジンを使用)
6−クロロ−3−[4−[3−(1H−ピラゾール−4−イル)ピペラジン−1−イル]ピリミジン−2−イル]イミダゾ[1,2−a]ピリジン I−28(6−クロロ−3−(4−クロロピリミジン−2−イル)イミダゾ[1,2−a]ピリジンを使用)
6−クロロ−3−[4−[3−ジメチルホスホリル−5−(1H−ピラゾール−4−イル)−1−ピペリジル]ピリミジン−2−イル]イミダゾ[1,2−a]ピリジン I−29(6−クロロ−3−(4−クロロピリミジン−2−イル)イミダゾ[1,2−a]ピリジンを使用)
((1−(2−(6−クロロイミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペリジン−3−イル)イミノ)ジメチル−λ6−スルファノン I−30(6−クロロ−3−(4−クロロピリミジン−2−イル)イミダゾ[1,2−a]ピリジンを使用)
N−[[−1−[4−[6−(ジフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル]ピリミジン−2−イル]−4,4−ジフルオロ−5−メチル−3−ピペリジル]メチル]メタンスルホンアミド、I−41(3−(2−クロロピリミジン−4−イル)−6−(ジフルオロメチル)イミダゾ[1,2−a]ピリジンを使用);
6−クロロ−7−フルオロ−3−[4−[3−(1H−イミダゾール−4−イル)−2,5−ジメチル−ピペラジン−1−イル]ピリミジン−2−イル]イミダゾ[1,2−a]ピリジン I−42(6−クロロ−3−(4−クロロピリミジン−2−イル)−7−フルオロ−イミダゾ[1,2−a]ピリジンを使用)
7−[2−[6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル]ピリミジン−4−イル]−1,2,5,6,8,8a−ヘキサヒドロイミダゾ[1,5−a]ピラジン−3−オン I−43(3−(4−クロロピリミジン−2−イル)−6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジンを使用)
2−(1H−ピラゾール−4−イル)−4−[4−[6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル]ピリミジン−2−イル]モルホリン I−44(3−(2−クロロピリミジン−4−イル)−6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジンを使用)
(3S)−1−[2−(6−クロロ−7−フルオロ−イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル]ピペリジン−3−カルボキサミド I−48(6−クロロ−3−(4−クロロピリミジン−2−イル)−7−フルオロ−イミダゾ[1,2−a]ピリジンを使用)
((1−(2−(6−クロロ−7−フルオロイミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペリジン−3−イル)イミノ)ジメチル−λ6−スルファノン I−49(6−クロロ−3−(4−クロロピリミジン−2−イル)−7−フルオロ−イミダゾ[1,2−a]ピリジンを使用)
1−[2−(6−クロロイミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル]−2,5−ジメチル−ピペリジン−3−カルボキサミド I−50(6−クロロ−3−(4−クロロピリミジン−2−イル)イミダゾ[1,2−a]ピリジンを使用);
1−[2−(6−クロロイミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル]−2,5−ジメチル−ピペリジン−3−カルボキサミド I−51(6−クロロ−3−(4−クロロピリミジン−2−イル)イミダゾ[1,2−a]ピリジンを使用)
1−[2−(6−クロロ−7−フルオロ−イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル]−2,5−ジメチル−ピペリジン−3−カルボキサミド I−52および1−[2−(6−クロロ−7−フルオロ−イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル]−2,5−ジメチル−ピペリジン−3−カルボキサミド I−53
実施例2: 1H−ピラゾール−4−イル−4−[2−[6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル]ピリミジン−4−イル]モルホリンおよび1H−ピラゾール−4−イル−4−[2−[6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル]ピリミジン−4−イル]モルホリン、I−2およびI−3
7−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ヘキサヒドロイミダゾ[1,5−a]ピラジン−3(2H)−オン I−5
7−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ヘキサヒドロイミダゾ[1,5−a]ピラジン−3(2H)−オン、I−6
2−(1H−ピラゾール−4−イル)−4−(4−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−2−イル)モルホリン、I−9
2−(1H−ピラゾール−4−イル)−4−(4−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−2−イル)モルホリン、I−10
ジメチル((5−メチル−1−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペリジン−3−イル)イミノ)−λ6−スルファノン I−31およびジメチル((5−メチル−1−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペリジン−3−イル)イミノ)−λ6−スルファノン I−32
3−[2−[2,5−ジメチル−3−(1H−ピラゾール−4−イル)ピペラジン−1−イル]ピリミジン−4−イル]−6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン I−33および3−[2−[2,5−ジメチル−3−(1H−ピラゾール−4−イル)ピペラジン−1−イル]ピリミジン−4−イル]−6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン I−34
6−クロロ−3−[4−[2,5−ジメチル−3−(1H−ピラゾール−4−イル)ピペラジン−1−イル]ピリミジン−2−イル]イミダゾ[1,2−a]ピリジン I−35および6−クロロ−3−[4−[2,5−ジメチル−3−(1H−ピラゾール−4−イル)ピペラジン−1−イル]ピリミジン−2−イル]イミダゾ[1,2−a]ピリジン I−36
3−[4−[2,5−ジメチル−3−(1H−ピラゾール−4−イル)ピペラジン−1−イル]ピリミジン−2−イル]−6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン I−37および3−[4−[2,5−ジメチル−3−(1H−ピラゾール−4−イル)ピペラジン−1−イル]ピリミジン−2−イル]−6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン I−38
3−[4−[3−メチル−5−(1H−ピラゾール−4−イル)ピペラジン−1−イル]ピリミジン−2−イル]−6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン I−39および3−[4−[3−メチル−5−(1H−ピラゾール−4−イル)ピペラジン−1−イル]ピリミジン−2−イル]−6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン I−40
実施例3: N−[[(2S)−4−[2−[6−(ジフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル]ピリミジン−4−イル]モルホリン−2−イル]メチル]メタンスルホンアミド、I−13
N−[[(2S)−4−[2−[6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル]ピリミジン−4−イル]モルホリン−2−イル]メチル]メタンスルホンアミド、I−1(2−[6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル]−1H−ピリミジン−6−オンを使用)
1−[4−[2−[6−(ジフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル]ピリミジン−4−イル]ピペラジン−1−イル]エタノン、I−14
4−[2−[6−(ジフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル]ピリミジン−4−イル]−2−(1H−ピラゾール−4−イル)モルホリン、I−15
N−(((3S,5S)−1−(2−(6−(ジフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)−4,4−ジフルオロ−5−メチルピペリジン−3−イル)メチル)メタンスルホンアミド、I−16
2−(1H−ピラゾール−4−イル)−4−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)モルホリン、I−45
実施例4: N−[[(2S)−4−[4−[6−(ジフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル]ピリミジン−2−イル]モルホリン−2−イル]メチル]メタンスルホンアミド、I−17
4−[4−[6−(ジフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル]ピリミジン−2−イル]−2−(1H−ピラゾール−4−イル)モルホリン、I−18
実施例5: 1−[4−[6−[6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル]−2−ピリジル]ピペラジン−1−イル]エタノン、I−11
工程2: 3−(6−ピペラジン−1−イル−2−ピリジル)−6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン
工程3: 1−[4−[6−[6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル]−2−ピリジル]ピペラジン−1−イル]エタノン
実施例6: 2−(1H−ピラゾール−4−イル)−4−[6−[6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル]−2−ピリジル]モルホリン、I−12
実施例7: 4−[4−(6−クロロイミダゾ[1,2−a]ピリジン−3−イル)−1,3,5−トリアジン−2−イル]−2−(1H−ピラゾール−4−イル)モルホリン、I−22
工程2: 4−[4−[(E)−2−エトキシビニル]−1,3,5−トリアジン−2−イル]−2−(1H−ピラゾール−4−イル)モルホリン
工程3: 4−[4−(6−クロロイミダゾ[1,2−a]ピリジン−3−イル)−1,3,5−トリアジン−2−イル]−2−(1H−ピラゾール−4−イル)モルホリン
実施例8: ((1−(2−(6−クロロイミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)−2,5−ジメチルピペリジン−3−イル)メチル)(イミノ)(メチル)−λ6−スルファノン(transジアステレオマー)、I−46
工程2: ((1−(2−(6−クロロイミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)−2,5−ジメチルピペリジン−3−イル)メチル)(イミノ)(メチル)−λ6−スルファノン(transジアステレオマー)
((1−(2−(6−クロロイミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)−2,5−ジメチルピペリジン−3−イル)メチル)(イミノ)(メチル)−λ6−スルファノン(cisジアステレオマー)、I−47
実施例9: 6−クロロ−3−{4−cis−2−メチル−6−(3−メチル−[1,2,4]オキサジアゾール−5−イル)−モルホリン−4−イル]−ピリミジン−2−イル}−イミダゾ[1,2−a]ピリジン、I−54
6−クロロ−3−{4−[3−(1H−イミダゾール−4−イル)−ピペリジン−1−イル]−ピリミジン−2−イル}−イミダゾ[1,2−a]ピリジン、I−55
3−(2−((3R,5R)−3−メチル−5−(1H−ピラゾール−4−イル)ピペリジン−1−イル)ピリミジン−4−イル)−6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン、I−136(キラル分離後)
3−(2−((3S,5S)−3−メチル−5−(1H−ピラゾール−4−イル)ピペリジン−1−イル)ピリミジン−4−イル)−6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン、I−137(キラル分離後)
5−メチル−1−[2−(6−トリフルオロメチル−イミダゾ[1,2−a]ピリジン−3−イル)−ピリミジン−4−イル]−ピペリジン−3−カルボン酸アミド、I−149
(S)−1−[2−(6−トリフルオロメチル−イミダゾ[1,2−a]ピリジン−3−イル)−ピリミジン−4−イル]−ピペリジン−3−カルボン酸アミド、I−154
5,5−ジフルオロ−1−[2−(6−トリフルオロメチル−イミダゾ[1,2−a]ピリジン−3−イル)−ピリミジン−4−イル]−ピペリジン−3−カルボン酸メチルエステル、I−570
実施例10: 6−クロロ−7−フルオロ−3−{4−[cis−2−メチル−6−(3−メチル−[1,2,4]オキサジアゾール−5−イル)−モルホリン−4−イル]−ピリミジン−2−イル}−イミダゾ[1,2−a]ピリジン、I−56
6−クロロ−7−フルオロ−3−{4−[3−(1H−イミダゾール−4−イル)−ピペリジン−1−イル]−ピリミジン−2−イル}−イミダゾ[1,2−a]ピリジン、I−57
3−{4−[(3S,5S)−3−メチル−5−(1−メチル−1H−ピラゾール−4−イル)−ピペリジン−1−イル]−ピリミジン−2−イル}−6−トリフルオロメチル−イミダゾ[1,2−a]ピリジン(ラセミ混合物)、I−60
3−{4−[(3R,5S)−3−メチル−5−(1−メチル−1H−ピラゾール−4−イル)−ピペリジン−1−イル]−ピリミジン−2−イル}−6−トリフルオロメチル−イミダゾ[1,2−a]ピリジン(ラセミ混合物)、I−61
1−[2−(6−クロロ−イミダゾ[1,2−a]ピリジン−3−イル)−ピリミジン−4−イル]−3−(3−メチル−[1,2,4]オキサジアゾール−5−イル)−ピロリジン−3−オール、I−64
6−クロロ−3−[4−(3−イソオキサゾール−4−イル−ピペリジン−1−イル)−ピリミジン−2−イル]−イミダゾ[1,2−a]ピリジン、I−65
6−クロロ−3−[4−(3−イソオキサゾール−3−イル−ピペリジン−1−イル)−ピリミジン−2−イル]−イミダゾ[1,2−a]ピリジン、I−66
3−[2−(6−クロロ−イミダゾ[1,2−a]ピリジン−3−イル)−ピリミジン−4−イル]−3−アザ−ビシクロ[4.1.0]ヘプタン−6−オール、I−67
4−{1−[2−(6−クロロ−イミダゾ[1,2−a]ピリジン−3−イル)−ピリミジン−4−イル]−ピペリジン−3−イル}−4−メチル−オキサゾリジン−2−オン、I−68
1−メチル−4−[2−(6−トリフルオロメチル−イミダゾ[1,2−a]ピリジン−3−イル)−ピリミジン−4−イル]−[1,4]ジアゼパン−2−オン、I−69
3−{4−[(3aR,6aR)−3a−(3−イソプロピル−[1,2,4]オキサジアゾール−5−イル)−ヘキサヒドロ−シクロペンタ[c]ピロール−2−イル]−ピリミジン−2−イル}−6−トリフルオロメチル−イミダゾ[1,2−a]ピリジン、I−70
3−[4−(3−メチル−ピペリジン−1−イル)−ピリミジン−2−イル]−6−トリフルオロメチル−イミダゾ[1,2−a]ピリジン、I−71
1−[2−(6−クロロ−イミダゾ[1,2−a]ピリジン−3−イル)−ピリミジン−4−イル]−3−(1−イソプロピル−1H−[1,2,3]トリアゾール−4−イル)−ピロリジン−3−オール、I−72
6−クロロ−3−{4−[(2S,3S)−2−(3−クロロ−フェニル)−3−メチル−モルホリン−4−イル]−ピリミジン−2−イル}−7−フルオロ−イミダゾ[1,2−a]ピリジン(ラセミ混合物)、I−73
3−[2−(6−トリフルオロメチル−イミダゾ[1,2−a]ピリジン−3−イル)−ピリミジン−4−イル]−3−アザ−ビシクロ[4.1.0]ヘプタン−1−オール、I−74
6−クロロ−3−{4−[(3aR,6aR)−3a−(3−イソプロピル−[1,2,4]オキサジアゾール−5−イル)−ヘキサヒドロ−シクロペンタ[c]ピロール−2−イル]−ピリミジン−2−イル}−イミダゾ[1,2−a]ピリジン(ラセミ混合物)、I−75
1−[2−(6−クロロ−イミダゾ[1,2−a]ピリジン−3−イル)−ピリミジン−4−イル]−3−(1−イソプロピル−1H−[1,2,3]トリアゾール−4−イル)−ピペリジン−3−オール、I−76
(S)−1−[2−(6−クロロ−7−フルオロ−イミダゾ[1,2−a]ピリジン−3−イル)−ピリミジン−4−イル]−ピペリジン−3−カルボン酸(1−メチル−1H−ピラゾール−4−イル)−アミド、I−77
5−[2−(6−クロロ−イミダゾ[1,2−a]ピリジン−3−イル)−ピリミジン−4−イル]−5−アザ−スピロ[2.5]オクタン−1−カルボン酸、I−78
6−クロロ−3−[4−(7,7−ジフルオロ−6−メチル−3−アザ−ビシクロ[4.1.0]ヘプタ−3−イル)−ピリミジン−2−イル]−イミダゾ[1,2−a]ピリジン、I−79
4−[2−(6−トリフルオロメチル−イミダゾ[1,2−a]ピリジン−3−イル)−ピリミジン−4−イル]−[1,4]ジアゼパン−2−オン、I−80
1−[2−(6−クロロ−7−フルオロ−イミダゾ[1,2−a]ピリジン−3−イル)−ピリミジン−4−イル]−3−フェニル−ピペリジン−3−オール、I−81
1−{1−[2−(6−クロロ−イミダゾ[1,2−a]ピリジン−3−イル)−ピリミジン−4−イル]−3−ヒドロキシ−ピペリジン−3−イル}−シクロブタンカルボン酸メチルエステル、I−82
{1−[2−(6−クロロ−7−フルオロ−イミダゾ[1,2−a]ピリジン−3−イル)−ピリミジン−4−イル]−3−フェニル−ピペリジン−4−イル}−メタノール、I−83
6−クロロ−3−[4−(1−フェニル−3−アザ−ビシクロ[3.1.0]ヘキサ−3−イル)−ピリミジン−2−イル]−イミダゾ[1,2−a]ピリジン、I−84
{1−[2−(6−クロロ−7−フルオロ−イミダゾ[1,2−a]ピリジン−3−イル)−ピリミジン−4−イル]−3−フェニル−ピペリジン−3−イル}−メタノール、I−85
実施例11: (S)−1−[2−(6−クロロ−7−フルオロ−イミダゾ[1,2−a]ピリジン−3−イル)−ピリミジン−4−イル]−ピペリジン−3−カルボン酸、I−58
工程2: (S)−1−[2−(6−クロロ−7−フルオロ−イミダゾ[1,2−a]ピリジン−3−イル)−ピリミジン−4−イル]−ピペリジン−3−カルボン酸(1H−ピラゾール−4−イル)−アミド
(S)−1−[2−(6−クロロ−7−フルオロ−イミダゾ[1,2−a]ピリジン−3−イル)−ピリミジン−4−イル]−ピペリジン−3−カルボン酸(1−メチル−1H−ピラゾール−4−イル)−アミド、I−59
(S)−1−[2−(6−クロロ−7−フルオロ−イミダゾ[1,2−a]ピリジン−3−イル)−ピリミジン−4−イル]−ピペリジン−3−カルボン酸ピリジン−4−イルアミド、I−86
実施例12: (3S)−1−(2−{6−クロロイミダゾ[1,2−a]ピリジン−3−イル}ピリミジン−4−イル)ピペリジン−3−アミン、I−87
工程2: (3S)−1−(2−{6−クロロイミダゾ[1,2−a]ピリジン−3−イル}ピリミジン−4−イル)ピペリジン−3−アミン
実施例13: 6−クロロ−7−フルオロ−3−[4−(2−ピリジン−2−イル−モルホリン−4−イル)−ピリミジン−2−イル]−イミダゾ[1,2−a]ピリジン、I−88
cis−2−メチル−6−(5−メチル−1,3,4−オキサジアゾール−2−イル)−4−{2−[6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル]ピリミジン−4−イル}モルホリン、I−93(3−(4−クロロピリミジン−2−イル)−6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジンを使用)
3−{4−[cis−2−メチル−6−(5−メチル−1,3,4−オキサジアゾール−2−イル)モルホリン−4−イル]ピリミジン−2−イル}イミダゾ[1,2−a]ピリジン−6−カルボニトリル、I−94(3−(4−クロロピリミジン−2−イル)イミダゾ[1,2−a]ピリジン−6−カルボニトリルを使用)
cis−4−(2−{6−クロロイミダゾ[1,2−a]ピリジン−3−イル}ピリミジン−4−イル)−2−メチル−6−(5−メチル−1,3,4−オキサジアゾール−2−イル)モルホリン、I−95(4−クロロ−2−{6−クロロイミダゾ[1,2−a]ピリジン−3−イル}ピリミジンを使用)
2−(2−{6−クロロイミダゾ[1,2−a]ピリジン−3−イル}ピリミジン−4−イル)−オクタヒドロ−1H−ピラジノ[1,2−c]ピリミジン−6−オン、I−96(4−クロロ−2−{6−クロロイミダゾ[1,2−a]ピリジン−3−イル}ピリミジンを使用)
7−(2−{6−クロロイミダゾ[1,2−a]ピリジン−3−イル}ピリミジン−4−イル)−オクタヒドロイミダゾ[1,5−a]ピラジン−3−オン、I−97(4−クロロ−2−{6−クロロイミダゾ[1,2−a]ピリジン−3−イル}ピリミジンを使用)
2−(2−{6−クロロイミダゾ[1,2−a]ピリジン−3−イル}ピリミジン−4−イル)−オクタヒドロピラジノ[1,2−c][1,3]オキサジン−6−オン、I−98(4−クロロ−2−{6−クロロイミダゾ[1,2−a]ピリジン−3−イル}ピリミジンを使用)
7−(2−{6−クロロイミダゾ[1,2−a]ピリジン−3−イル}ピリミジン−4−イル)−ヘキサヒドロ−1H−[1,3]オキサゾロ[3,4−a]ピラジン−3−オン、I−99(4−クロロ−2−{6−クロロイミダゾ[1,2−a]ピリジン−3−イル}ピリミジンを使用)
2−{6−クロロイミダゾ[1,2−a]ピリジン−3−イル}−4−[3−(1H−ピラゾール−4−イル)ピペリジン−1−イル]ピリミジン、I−100(4−クロロ−2−{6−クロロイミダゾ[1,2−a]ピリジン−3−イル}ピリミジンを使用)
4−[3−(1H−ピラゾール−4−イル)ピペリジン−1−イル]−2−[6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル]ピリミジン、I−101(3−(4−クロロピリミジン−2−イル)−6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジンを使用)
実施例14: 2−メチル−6−(3−メチル−1,2,4−オキサジアゾール−5−イル)−4−{2−[6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル]ピリミジン−4−イル}モルホリン、I−89およびI−90
3−{4−[(2S,6S)−2−メチル−6−(3−メチル−1,2,4−オキサジアゾール−5−イル)モルホリン−4−イル]ピリミジン−2−イル}イミダゾ[1,2−a]ピリジン−6−カルボニトリル、I−91、および3−{4−[(2R,6R)−2−メチル−6−(3−メチル−1,2,4−オキサジアゾール−5−イル)モルホリン−4−イル]ピリミジン−2−イル}イミダゾ[1,2−a]ピリジン−6−カルボニトリル、I−92
実施例15: 例示的な化合物I−102〜I−113。
(S)−1−(2−(6−クロロイミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペリジン−3−カルボキサミド、I−102
N−(((3S,5S)−1−(3−(6−(ジフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)−1,2,4−チアジアゾール−5−イル)−4,4−ジフルオロ−5−メチルピペリジン−3−イル)メチル)メタンスルホンアミド、I−103
2−(1H−ピラゾール−4−イル)−4−(3−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)−1,2,4−チアジアゾール−5−イル)モルホリン、I−104
4−(3−(6−(ジフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)−1,2,4−チアジアゾール−5−イル)−2−(1H−ピラゾール−4−イル)モルホリン、I−105
(S)−N−((4−(3−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)−1,2,4−チアジアゾール−5−イル)モルホリン−2−イル)メチル)メタンスルホンアミド、I−106
(S)−N−((4−(3−(6−(ジフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)−1,2,4−チアジアゾール−5−イル)モルホリン−2−イル)メチル)メタンスルホンアミド、I−107
2−(1H−ピラゾール−4−イル)−4−(5−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)−1,2,4−チアジアゾール−3−イル)モルホリン、I−108
(S)−N−((4−(5−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)−1,2,4−チアジアゾール−3−イル)モルホリン−2−イル)メチル)メタンスルホンアミド、I−109
N−((1−(5−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)−1,2,4−チアジアゾール−3−イル)ピペリジン−3−イル)メチル)メタンスルホンアミド、I−110
(S)−N−((4−(4−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)チアゾール−2−イル)モルホリン−2−イル)メチル)メタンスルホンアミド、I−111
N−((1−(3−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)−1,2,4−チアジアゾール−5−イル)ピペリジン−3−イル)メチル)メタンスルホンアミド、I−112
(S)−N−((4−(6−(6−クロロイミダゾ[1,2−a]ピリジン−3−イル)ピラジン−2−イル)モルホリン−2−イル)メチル)メタンスルホンアミド、I−113
実施例16: 6−クロロ−3−{4−cis−2−メチル−6−(3−メチル−[1,2,4]オキサジアゾール−5−イル)−モルホリン−4−イル]−ピリミジン−2−イル}−イミダゾ[1,2−a]ピリジン、I−114
cis−2−メチル−6−(3−メチル−1H−ピラゾール−4−イル)−4−{4−[6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル]ピリミジン−2−イル}モルホリン、I−115
cis−2−メチル−6−(1H−ピラゾール−4−イル)−4−{4−[6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル]ピリミジン−2−イル}モルホリン、I−117
3−{4−[cis−2−メチル−6−(3−メチル−1H−ピラゾール−4−イル)−モルホリン−4−イル]−ピリミジン−2−イル}−6−トリフルオロメチル−イミダゾ[1,2−a]ピリジン、I−119
表2:式Iの化合物についての分析データ
表3:式Iの化合物についての酵素活性
表5:式Iの化合物についての細胞活性(バイオマーカーアッセイ)
実施例20: 5,5−ジフルオロ−1−[2−(6−トリフルオロメチル−イミダゾ[1,2−a]ピリジン−3−イル)−ピリミジン−4−イル]−ピペリジン−3−カルボン酸アミド、I−202
実施例21: 3−{2−[(2R,6S)−2−メチル−6−(1H−ピラゾール−4−イル)−モルホリン−4−イル]−ピリミジン−4−イル}−6−トリフルオロメチル−イミダゾ[1,2−a]ピリジン I−127および(2S,6R)−2−メチル−6−(1H−ピラゾール−4−イル)−4−{4−[6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル]ピリミジン−2−イル}モルホリン I−126
実施例22: 3−{4−[(S)−4−(3−メタンスルホニル−シクロブチル)−3−(1H−ピラゾール−4−イル)−ピペラジン−1−イル]−ピリミジン−2−イル}−6−トリフルオロメチル−イミダゾ[1,2−a]ピリジン I−495および3−{4−[(R)−4−(3−メタンスルホニル−シクロブチル)−3−(1H−ピラゾール−4−イル)−ピペラジン−1−イル]−ピリミジン−2−イル}−6−トリフルオロメチル−イミダゾ[1,2−a]ピリジン I−490
実施例23: 4−[4−({6−オキサスピロ[2.5]オクタン−1−イル}メチル)−3−(1H−ピラゾール−4−イル)ピペラジン−1−イル]−2−[6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル]ピリミジン I−476
実施例25: 例示的な化合物I−122〜I−563。
6−クロロ−3−(4−(2,5−ジメチル−3−(1H−ピラゾール−4−イル)ピペラジン−1−イル)ピリミジン−2−イル)イミダゾ[1,2−a]ピリジン、I−122
ジメチル(((3R,5S)−5−メチル−1−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペリジン−3−イル)イミノ)−λ6−スルファノン、I−123
3−{4−[(2S,6R)−2−メチル−6−(3−メチル−1H−ピラゾール−4−イル)−モルホリン−4−イル]−ピリミジン−2−イル}−6−トリフルオロメチル−イミダゾ[1,2−a]ピリジン、I−124
(2R,6S)−2−メチル−6−(5−メチル−1H−ピラゾール−4−イル)−4−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)モルホリン、I−125
(((3R,5S)−1−(2−(6−クロロイミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)−5−メチルピペリジン−3−イル)イミノ)ジメチル−λ6−スルファノン、I−128
(2R,6S)−6−メチル−4−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)モルホリン−2−カルボキサミド、I−129
N,N−ジメチル−1−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペリジン−3−カルボキサミド、I−130
ピロリジン−1−イル(1−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペリジン−3−イル)メタノン、I−131
5−(2−(6−クロロイミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)−5−アザスピロ[2.5]オクタン−1−カルボキサミド、I−132
5−(2−(6−クロロイミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)−5−アザスピロ[2.5]オクタン−1−カルボン酸メチル、I−133
(2S,6S)−2−メチル−6−(1H−ピラゾール−4−イル)−4−(4−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−2−イル)モルホリン、I−134
(2R,6R)−2−メチル−6−(1H−ピラゾール−4−イル)−4−(4−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−2−イル)モルホリン、I−135
3−(2−((3R,5R)−3−メチル−5−(1H−ピラゾール−4−イル)ピペリジン−1−イル)ピリミジン−4−イル)−6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン、I−136(キラル分離後)。
3−(2−((3S,5S)−3−メチル−5−(1H−ピラゾール−4−イル)ピペリジン−1−イル)ピリミジン−4−イル)−6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン、I−137(キラル分離後)。
(2S,6R)−2−メチル−6−(1H−ピラゾール−3−イル)−4−(4−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−2−イル)モルホリン、I−138
3−(2−((3R,5S)−3−(1,3−ジメチル−1H−ピラゾール−4−イル)−5−メチルピペリジン−1−イル)ピリミジン−4−イル)−6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン、I−139
3−(2−((3S,5R)−3−(1,3−ジメチル−1H−ピラゾール−4−イル)−5−メチルピペリジン−1−イル)ピリミジン−4−イル)−6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン、I−140
3−(2−((3S,5S)−3−(1,3−ジメチル−1H−ピラゾール−4−イル)−5−メチルピペリジン−1−イル)ピリミジン−4−イル)−6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン、I−141
3−(2−((3R,5R)−3−(1,3−ジメチル−1H−ピラゾール−4−イル)−5−メチルピペリジン−1−イル)ピリミジン−4−イル)−6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン、I−142
3−(2−((3R,5R)−3−(1−(2−メトキシエチル)−1H−ピラゾール−4−イル)−5−メチルピペリジン−1−イル)ピリミジン−4−イル)−6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン、I−143
3−(2−((3R,5S)−3−(1−(2−メトキシエチル)−1H−ピラゾール−4−イル)−5−メチルピペリジン−1−イル)ピリミジン−4−イル)−6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン、I−144
3−(2−((3S,5R)−3−(1−(2−メトキシエチル)−1H−ピラゾール−4−イル)−5−メチルピペリジン−1−イル)ピリミジン−4−イル)−6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン、I−145
3−(2−((3S,5S)−3−(1−(2−メトキシエチル)−1H−ピラゾール−4−イル)−5−メチルピペリジン−1−イル)ピリミジン−4−イル)−6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン、I−146
(2S,6S)−2−メチル−6−(5−メチル−1H−ピラゾール−4−イル)−4−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)モルホリン、I−147
(3R,5S)−5−メチル−1−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペリジン−3−カルボキサミド、I−148
5−メチル−1−[2−(6−トリフルオロメチル−イミダゾ[1,2−a]ピリジン−3−イル)−ピリミジン−4−イル]−ピペリジン−3−カルボン酸アミド、I−149
(S)−4−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)モルホリン−2−カルボキサミド、I−150
(R)−4−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)モルホリン−2−カルボキサミド、I−151
(R)−1−(4−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−2−イル)ピペリジン−3−カルボキサミド、I−152
(S)−1−(4−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−2−イル)ピペリジン−3−カルボキサミド、I−153
(S)−1−[2−(6−トリフルオロメチル−イミダゾ[1,2−a]ピリジン−3−イル)−ピリミジン−4−イル]−ピペリジン−3−カルボン酸アミド、I−154
(2R,6R)−2−(1,3−ジメチル−1H−ピラゾール−4−イル)−6−メチル−4−(4−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−2−イル)モルホリン、I−155
(2S,6S)−2−(1,3−ジメチル−1H−ピラゾール−4−イル)−6−メチル−4−(4−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−2−イル)モルホリン、I−156
(2R,6S)−2−(1,3−ジメチル−1H−ピラゾール−4−イル)−6−メチル−4−(4−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−2−イル)モルホリン、I−157
(2S,6R)−2−(1,3−ジメチル−1H−ピラゾール−4−イル)−6−メチル−4−(4−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−2−イル)モルホリン、I−158
(((3R,5S)−1−(4−(6−クロロイミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−2−イル)−5−メチルピペリジン−3−イル)イミノ)ジメチル−λ6−スルファノン、I−159
4−(4−(6−クロロイミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−2−イル)−2−メチル−6−(3−メチル−1H−ピラゾール−4−イル)モルホリン、I−160
2−(1−(2−(6−クロロイミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペリジン−3−イル)酢酸、I−161
2−(1−(2−(6−クロロイミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペリジン−3−イル)アセトアミド、I−162
4−(2−(6−クロロイミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)モルホリン−2−カルボキサミド、I−163
(R)−1−(2−(6−クロロイミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペリジン−3−カルボキサミド、I−164
2−(1−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペリジン−3−イル)酢酸、I−165
2−(1−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペリジン−3−イル)アセトアミド、I−166
(((3S,5R)−1−(4−(6−クロロイミダゾ[1,2−a]ピリジン−3−イル)−5−メチルピリミジン−2−イル)−5−メチルピペリジン−3−イル)イミノ)ジメチル−λ6−スルファノン、I−167
(((3S,5R)−1−(4−(6−クロロイミダゾ[1,2−a]ピリジン−3−イル)−6−メチルピリミジン−2−イル)−5−メチルピペリジン−3−イル)イミノ)ジメチル−λ6−スルファノン、I−168
ジメチル(((3S,5R)−5−メチル−1−(4−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−2−イル)ピペリジン−3−イル)イミノ)−λ6−スルファノン、I−169
3−(2−((2S,5S)−2,5−ジメチル−3−(1H−ピラゾール−4−イル)ピペラジン−1−イル)ピリミジン−4−イル)−6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン、I−170
3−(2−((2R,5R)−2,5−ジメチル−3−(1H−ピラゾール−4−イル)ピペラジン−1−イル)ピリミジン−4−イル)−6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン、I−171
3−(2−((2S,5S)−2,5−ジメチル−3−(5−メチル−1H−ピラゾール−4−イル)ピペラジン−1−イル)ピリミジン−4−イル)−6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン、I−172
3−(2−((2R,5R)−2,5−ジメチル−3−(5−メチル−1H−ピラゾール−4−イル)ピペラジン−1−イル)ピリミジン−4−イル)−6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン、I−173
(S)−1−(4−(6−クロロイミダゾ[1,2−a]ピリジン−3−イル)−5−メチルピリミジン−2−イル)ピペリジン−3−カルボキサミド、I−174
(2S,6S)−4−(2−(6−クロロイミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)−2−(5−フルオロ−1H−ピラゾール−4−イル)−6−メチルモルホリン、I−175
(2R,6S)−4−(2−(6−クロロイミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)−2−(5−フルオロ−1H−ピラゾール−4−イル)−6−メチルモルホリン、I−176
(2S,6R)−4−(2−(6−クロロイミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)−6−メチルモルホリン−2−カルボキサミド、I−177
(2R,6R)−4−(2−(6−クロロイミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)−6−メチルモルホリン−2−カルボキサミド、I−178
(2S,6R)−4−(4−(6−クロロイミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−2−イル)−2−メチル−6−(5−メチル−1H−ピラゾール−4−イル)モルホリン、I−179
(2R,6S)−4−(4−(6−クロロイミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−2−イル)−2−メチル−6−(5−メチル−1H−ピラゾール−4−イル)モルホリン、I−180
(2S,6S)−4−(4−(6−クロロイミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−2−イル)−2−メチル−6−(5−メチル−1H−ピラゾール−4−イル)モルホリン、I−181
(2R,6R)−4−(4−(6−クロロイミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−2−イル)−2−メチル−6−(5−メチル−1H−ピラゾール−4−イル)モルホリン、I−182
(S)−1−(4−(6−クロロイミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−2−イル)ピペリジン−3−カルボキサミド、I−183
6−クロロ−3−(5−メチル−2−((3R,5S)−3−メチル−5−(1H−ピラゾール−4−イル)ピペリジン−1−イル)ピリミジン−4−イル)イミダゾ[1,2−a]ピリジン、I−184
6−クロロ−3−(5−メチル−2−((3R,5R)−3−メチル−5−(1H−ピラゾール−4−イル)ピペリジン−1−イル)ピリミジン−4−イル)イミダゾ[1,2−a]ピリジン、I−185
6−クロロ−3−(5−メチル−2−((3S,5S)−3−メチル−5−(1H−ピラゾール−4−イル)ピペリジン−1−イル)ピリミジン−4−イル)イミダゾ[1,2−a]ピリジン、I−186
N−(1−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペリジン−3−イル)アセトアミド、I−187
4−メチル−1−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペリジン−4−カルボキサミド、I−188
(2S,6S)−2−メチル−6−(2H−テトラゾール−5−イル)−4−(4−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−2−イル)モルホリン、I−189
(2R,6R)−2−メチル−6−(2H−テトラゾール−5−イル)−4−(4−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−2−イル)モルホリン、I−190
(((3S,5R)−1−(2−(6−クロロ−7−フルオロイミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)−5−メチルピペリジン−3−イル)イミノ)ジメチル−λ6−スルファノン、I−191
3−メチル−1−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペリジン−3−カルボキサミド、I−192
3−(4−(2−(5−(ジフルオロメチル)−1H−ピラゾール−4−イル)モルホリノ)ピリミジン−2−イル)イミダゾ[1,2−a]ピリジン−6−カルボニトリル、I−193
6−クロロ−3−(2−((3R,5S)−3−メチル−5−(1H−ピラゾール−4−イル)ピペリジン−1−イル)ピリミジン−4−イル)イミダゾ[1,2−a]ピリジン、I−195
6−クロロ−3−(2−((3R,5R)−3−メチル−5−(1H−ピラゾール−4−イル)ピペリジン−1−イル)ピリミジン−4−イル)イミダゾ[1,2−a]ピリジン、I−196
6−クロロ−3−(5−メチル−2−((3S,5R)−3−メチル−5−(1H−ピラゾール−4−イル)ピペリジン−1−イル)ピリミジン−4−イル)イミダゾ[1,2−a]ピリジン、I−197
6−クロロ−3−(2−((3S,5R)−3−メチル−5−(1H−ピラゾール−4−イル)ピペリジン−1−イル)ピリミジン−4−イル)イミダゾ[1,2−a]ピリジン、I−198
6−クロロ−3−(2−((3S,5S)−3−メチル−5−(1H−ピラゾール−4−イル)ピペリジン−1−イル)ピリミジン−4−イル)イミダゾ[1,2−a]ピリジン、I−199
6−メチル−1−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペリジン−3−カルボキサミド、I−200
6−メチル−1−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペリジン−3−カルボン酸、I−201
(2S,6R)−4−(4−(6−クロロイミダゾ[1,2−a]ピリジン−3−イル)−5−メチルピリミジン−2−イル)−2−メチル−6−(5−メチル−1H−ピラゾール−4−イル)モルホリン、I−203
(2R,6S)−4−(4−(6−クロロイミダゾ[1,2−a]ピリジン−3−イル)−5−メチルピリミジン−2−イル)−2−メチル−6−(5−メチル−1H−ピラゾール−4−イル)モルホリン、I−204
5,5−ジフルオロ−1−[2−(6−トリフルオロメチル−イミダゾ[1,2−a]ピリジン−3−イル)−ピリミジン−4−イル]−ピペリジン−3−カルボン酸、I−205
5−フルオロ−1−[2−(6−トリフルオロメチル−イミダゾ[1,2−a]ピリジン−3−イル)−ピリミジン−4−イル]−ピペリジン−3−カルボン酸、I−206
2−カルバモイル−4−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペラジン−1−カルボン酸tert−ブチル、I−207
6−クロロ−3−(6−メチル−2−((3S,5S)−3−メチル−5−(1H−ピラゾール−4−イル)ピペリジン−1−イル)ピリミジン−4−イル)イミダゾ[1,2−a]ピリジン、I−208
6−クロロ−3−(6−メチル−2−((3R,5R)−3−メチル−5−(1H−ピラゾール−4−イル)ピペリジン−1−イル)ピリミジン−4−イル)イミダゾ[1,2−a]ピリジン、I−209
6−クロロ−3−(6−メチル−2−((3S,5R)−3−メチル−5−(1H−ピラゾール−4−イル)ピペリジン−1−イル)ピリミジン−4−イル)イミダゾ[1,2−a]ピリジン、I−210
6−クロロ−3−(6−メチル−2−((3R,5S)−3−メチル−5−(1H−ピラゾール−4−イル)ピペリジン−1−イル)ピリミジン−4−イル)イミダゾ[1,2−a]ピリジン、I−211
3−ヒドロキシ−1−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペリジン−3−カルボン酸tert−ブチル、I−212
3−ヒドロキシ−1−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペリジン−3−カルボキサミド、I−213
3−ヒドロキシ−1−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペリジン−3−カルボン酸、I−214
4−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペラジン−2−カルボキサミド、I−217
(2R,6R)−4−(4−(6−クロロイミダゾ[1,2−a]ピリジン−3−イル)−6−メチルピリミジン−2−イル)−2−メチル−6−(5−メチル−1H−ピラゾール−4−イル)モルホリン、I−218
(S)−1−(5−フルオロ−4−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−2−イル)ピペリジン−3−カルボキサミド、I−219
(2S,6S)−4−(4−(6−クロロイミダゾ[1,2−a]ピリジン−3−イル)−6−メチルピリミジン−2−イル)−2−メチル−6−(5−メチル−1H−ピラゾール−4−イル)モルホリン、I−220
(2S,6R)−4−(4−(6−クロロイミダゾ[1,2−a]ピリジン−3−イル)−6−メチルピリミジン−2−イル)−2−メチル−6−(5−メチル−1H−ピラゾール−4−イル)モルホリン、I−221
(2R,6S)−4−(4−(6−クロロイミダゾ[1,2−a]ピリジン−3−イル)−6−メチルピリミジン−2−イル)−2−メチル−6−(5−メチル−1H−ピラゾール−4−イル)モルホリン、I−222
(R)−1−(5−フルオロ−4−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−2−イル)ピペリジン−3−カルボキサミド、I−223
3−(4−(3,3−ジフルオロピペリジン−1−イル)ピリミジン−2−イル)−6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン、I−224
2−(ジフルオロメチル)−4−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)モルホリン、I−225
3−(4−(3−フルオロ−3−メチルピペリジン−1−イル)ピリミジン−2−イル)−6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン、I−226
(S)−1−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペリジン−3−カルボニトリル、I−227
1−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)アゼチジン−3−カルボキサミド、I−228
5−フルオロ−1−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペリジン−3−カルボキサミド、I−229
2−(1−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)アゼチジン−3−イル)アセトアミド、I−230
3−(4−(3,5−ジメチルピペラジン−1−イル)ピリミジン−2−イル)−6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン、I−231
(S)−4−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)モルホリン−2−カルボニトリル、I−232
(S)−6−(トリフルオロメチル)−3−(4−(3−(トリフルオロメチル)ピペリジン−1−イル)ピリミジン−2−イル)イミダゾ[1,2−a]ピリジン、I−233
3−(4−(3,5−ジメチル−4−(オキセタン−3−イル)ピペラジン−1−イル)ピリミジン−2−イル)−6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン、I−234
6−シクロプロピル−3−(2−((3S,5R)−3−メチル−5−(1H−ピラゾール−4−イル)ピペリジン−1−イル)ピリミジン−4−イル)イミダゾ[1,2−a]ピリジン、I−235
6−シクロプロピル−3−(2−((3R,5S)−3−メチル−5−(1H−ピラゾール−4−イル)ピペリジン−1−イル)ピリミジン−4−イル)イミダゾ[1,2−a]ピリジン、I−236
((3S,5S)−5−ヒドロキシ−1−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペリジン−3−イル)カルバミン酸tert−ブチル、I−237
(3R,5S)−1−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペリジン−3,5−ジオール、I−238
(3S,5S)−5−アミノ−1−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペリジン−3−オール、I−239
3−(4−((3R,4R)−3−フルオロ−4−メチルピペリジン−1−イル)ピリミジン−2−イル)−6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン、I−240
3−(ヒドロキシメチル)−1−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペリジン−4−オール、I−241
1−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペリジン−3−スルホンアミド、I−242
((3R,4R)−1−(2−(6−クロロイミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)−4−ヒドロキシピペリジン−3−イル)カルバミン酸tert−ブチル、I−243
(((3S,5R)−1−(4−(6,7−ジクロロイミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−2−イル)−5−メチルピペリジン−3−イル)イミノ)ジメチル−λ6−スルファノン、I−244
4−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)−1−(3,3,3−トリフルオロプロピル)ピペラジン−2−カルボキサミド、I−245
(2S,6S)−4−(4−(6−クロロイミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−2−イル)−2−メチル−6−(1H−ピラゾール−4−イル)モルホリン、I−246
6−クロロ−3−{2−[(2S,6R)−2−メチル−6−(1H−ピラゾール−4−イル)−モルホリン−4−イル]−ピリミジン−4−イル}−イミダゾ[1,2−a]ピリジン、I−247
6−クロロ−3−{2−[(2R,6S)−2−メチル−6−(1H−ピラゾール−4−イル)−モルホリン−4−イル]−ピリミジン−4−イル}−イミダゾ[1,2−a]ピリジン、I−248
6−シクロプロピル−3−{2−[(3R,5R)−3−メチル−5−(1H−ピラゾール−4−イル)−ピペリジン−1−イル]−ピリミジン−4−イル}−イミダゾ[1,2−a]ピリジン、I−249
6−シクロプロピル−3−{2−[(3S,5S)−3−メチル−5−(1H−ピラゾール−4−イル)−ピペリジン−1−イル]−ピリミジン−4−イル}−イミダゾ[1,2−a]ピリジン、I−250
(2R,6R)−4−(4−(6−クロロイミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−2−イル)−2−メチル−6−(1H−ピラゾール−4−イル)モルホリン、I−251
((3R,5R)−1−(2−(6−クロロイミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)−5−メチルピペリジン−3−イル)カルバミン酸tert−ブチル、I−252
2−ヒドロキシ−N−((3S,5S)−5−ヒドロキシ−1−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペリジン−3−イル)アセトアミド、I−253
2−ヒドロキシ−N−((3S,5S)−5−ヒドロキシ−1−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペリジン−3−イル)プロパンアミド、I−254
(3R,4R)−3−アミノ−1−(2−(6−クロロイミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペリジン−4−オール、I−255
(3R,5R)−1−(2−(6−クロロイミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)−5−メチルピペリジン−3−アミン、I−256
N−((3S,5S)−5−ヒドロキシ−1−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペリジン−3−イル)−1H−ピラゾール−4−カルボキサミド、I−257
1−(2−メトキシエチル)−4−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペラジン−2−カルボキサミド、I−258
6−(3,3−ジフルオロアゼチジン−1−イル)−3−(2−((3S,5R)−3−メチル−5−(1H−ピラゾール−4−イル)ピペリジン−1−イル)ピリミジン−4−イル)イミダゾ[1,2−a]ピリジン、I−259
(R)−1−(3−フルオロ−6−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリジン−2−イル)ピペリジン−3−カルボキサミド、I−260
6−(3,3−ジフルオロアゼチジン−1−イル)−3−(2−((3R,5S)−3−メチル−5−(1H−ピラゾール−4−イル)ピペリジン−1−イル)ピリミジン−4−イル)イミダゾ[1,2−a]ピリジン、I−261
3−(4−((3S,5R)−3−((ジメチル(オキソ)−λ6−スルファニリデン)アミノ)−5−メチルピペリジン−1−イル)ピリミジン−2−イル)イミダゾ[1,2−a]ピリジン−6−カルボニトリル(3−(4−((3S,5R)−3−((dimethyl(oxo)−λ6−sulfaneylidene)amino)−5−methylpiperidin−1−yl)pyrimidin−2−yl)imidazo[1,2−a]pyridine−6−carbonitrile)、I−262
1−(オキセタン−3−イル)−4−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペラジン−2−カルボキサミド、I−263
(2S,6S)−6−メチル−4−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)モルホリン−2−カルボキサミド、I−264
(2S,6R)−6−メチル−4−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)モルホリン−2−カルボキサミド、I−265
6−クロロ−3−(4−(3−メチル−5−(1H−ピラゾール−4−イル)ピペラジン−1−イル)ピリミジン−2−イル)イミダゾ[1,2−a]ピリジン、I−266
6−クロロ−3−(4−(3−メチル−5−(5−メチル−1H−ピラゾール−4−イル)ピペラジン−1−イル)ピリミジン−2−イル)イミダゾ[1,2−a]ピリジン、I−267
6−クロロ−3−(4−(3−メチル−5−(5−メチル−1H−ピラゾール−4−イル)−4−(メチルスルホニル)ピペラジン−1−イル)ピリミジン−2−イル)イミダゾ[1,2−a]ピリジン、I−268
(((3S,5R)−1−(2−(6,7−ジクロロイミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)−5−メチルピペリジン−3−イル)イミノ)ジメチル−λ6−スルファノン、I−269
(2S,6R)−4−(4−(6−クロロ−7−フルオロイミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−2−イル)−2−メチル−6−(1H−ピラゾール−4−イル)モルホリン、I−270
6−(アゼチジン−1−イル)−3−(2−((3S,5R)−3−メチル−5−(1H−ピラゾール−4−イル)ピペリジン−1−イル)ピリミジン−4−イル)イミダゾ[1,2−a]ピリジン、I−271
6−(アゼチジン−1−イル)−3−(2−((3R,5R)−3−メチル−5−(1H−ピラゾール−4−イル)ピペリジン−1−イル)ピリミジン−4−イル)イミダゾ[1,2−a]ピリジン、I−272
(2R,6S)−4−(4−(6−クロロ−7−フルオロイミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−2−イル)−2−メチル−6−(1H−ピラゾール−4−イル)モルホリン、I−273
(2R,6R)−4−(4−(6−クロロ−7−フルオロイミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−2−イル)−2−メチル−6−(1H−ピラゾール−4−イル)モルホリン、I−274
(2S,6S)−4−(4−(6−クロロ−7−フルオロイミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−2−イル)−2−メチル−6−(1H−ピラゾール−4−イル)モルホリン、I−275
1−(4−(2−(6−クロロイミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)−2−メチル−6−(3−メチル−1H−ピラゾール−4−イル)ピペラジン−1−イル)エタン−1−オン、I−276
1−(4−(2−(6−クロロイミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)−2−メチル−6−(1H−ピラゾール−4−イル)ピペラジン−1−イル)エタン−1−オン、I−277
(S)−1−(5−フルオロ−2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペリジン−3−カルボキサミド、I−278
6−クロロ−3−(6−メトキシ−2−((3R,5R)−3−メチル−5−(1H−ピラゾール−4−イル)ピペリジン−1−イル)ピリミジン−4−イル)イミダゾ[1,2−a]ピリジン、I−279
6−クロロ−3−(6−メトキシ−2−((3R,5S)−3−メチル−5−(1H−ピラゾール−4−イル)ピペリジン−1−イル)ピリミジン−4−イル)イミダゾ[1,2−a]ピリジン、I−280
6−クロロ−3−(6−メトキシ−2−((3S,5S)−3−メチル−5−(1H−ピラゾール−4−イル)ピペリジン−1−イル)ピリミジン−4−イル)イミダゾ[1,2−a]ピリジン、I−281
(S)−1−(5−フルオロ−2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペリジン−3−カルボキサミド、I−282
N−((1−(2−(6−クロロイミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペリジン−3−イル)メチル)−N−メチルメタンスルホンアミド、I−283
2−(1−(2−(6−クロロイミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペリジン−3−イル)−2−メチルプロパン酸、I−284
6−(2−(6−クロロイミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)−2,6−ジアザスピロ[3.5]ノナン−2−カルボン酸tert−ブチル、I−285
4−(2−(6−クロロイミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)−1−シクロプロピルピペラジン−2−カルボキサミド、I−286
6−(3,3−ジフルオロアゼチジン−1−イル)−3−(6−メチル−2−((3S,5R)−3−メチル−5−(1H−ピラゾール−4−イル)ピペリジン−1−イル)ピリミジン−4−イル)イミダゾ[1,2−a]ピリジン、I−287
6−(3,3−ジフルオロアゼチジン−1−イル)−3−(6−メチル−2−((3R,5R)−3−メチル−5−(1H−ピラゾール−4−イル)ピペリジン−1−イル)ピリミジン−4−イル)イミダゾ[1,2−a]ピリジン、I−288
(((3S,5R)−1−(2−(6−ブロモイミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)−5−メチルピペリジン−3−イル)イミノ)ジメチル−λ6−スルファノン、I−289
ジメチル(((3S,5R)−5−メチル−1−(2−(6−(トリフルオロメトキシ)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペリジン−3−イル)イミノ)−λ6−スルファノン、I−290
ジメチル(((3S,5R)−5−メチル−1−(2−(6−(ジフルオロメトキシ)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペリジン−3−イル)イミノ)−λ6−スルファノン、I−291
6,6−ジメチル−8−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)−5−オキサ−2,8−ジアザスピロ[3.5]ノナン−2−カルボン酸tert−ブチル、I−292
(2R,6S)−2−メチル−6−(1H−ピラゾール−4−イル)−4−(2−(6−(トリフルオロメトキシ)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)モルホリン、I−293
6,6−ジメチル−8−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)−5−オキサ−2,8−ジアザスピロ[3.5]ノナン、I−294
(R)−6−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)−2,6−ジアザスピロ[3.5]ノナン−1−オン、I−295
(S)−6−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)−2,6−ジアザスピロ[3.5]ノナン−1−オン、I−296
1−(1−(2−(6−クロロイミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペリジン−3−イル)シクロプロパン−1−カルボン酸、I−297
2−(4−(2−(6−クロロイミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)モルホリン−2−イル)酢酸、I−298
6−(2−(6−クロロイミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)−2,6−ジアザスピロ[3.5]ノナン、I−299
(((3S,5R)−1−(2−(6−シクロプロピルイミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)−5−メチルピペリジン−3−イル)イミノ)ジメチル−λ6−スルファノン、I−300
6−クロロ−3−(4−(3−メチル−4−(メチルスルホニル)−5−(1−(メチルスルホニル)−1H−ピラゾール−4−イル)ピペラジン−1−イル)ピリミジン−2−イル)イミダゾ[1,2−a]ピリジン、I−301
1−(2−(6−クロロイミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)−5−(3−メチル−1H−ピラゾール−4−イル)ピペリジン−3−オール、I−302
1−(1−(2−(6−クロロイミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペリジン−3−イル)シクロプロパン−1−カルボキサミド、I−303
6,6−ジメチル−2−(メチルスルホニル)−8−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)−5−オキサ−2,8−ジアザスピロ[3.5]ノナン、I−304
2−((6,6−ジメチル−4−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)モルホリン−2−イル)メトキシ)−N,N−ジメチルアセトアミド、I−305
(3S,5R)−5−(5−メチル−1H−ピラゾール−4−イル)−1−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペリジン−3−オール、I−307
(3R,5S)−5−(5−メチル−1H−ピラゾール−4−イル)−1−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペリジン−3−オール、I−308
2−(1−(2−(6−クロロイミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペリジン−3−イル)−2−メチルプロパンアミド、I−309
3−(4−((3R)−2−メチル−3−(1H−ピラゾール−4−イル)ピペラジン−1−イル)ピリミジン−2−イル)−6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン、I−310
1−シクロプロピル−4−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペラジン−2−カルボキサミド、I−311
ジメチル(((3R,5S)−5−メチル−1−(2−(6−(メチルスルホニル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペリジン−3−イル)イミノ)−λ6−スルファノン、I−312
3−(4−(3−(1H−ピラゾール−4−イル)ピペリジン−1−イル)ピリミジン−2−イル)−6−(メチルスルホニル)イミダゾ[1,2−a]ピリジン、I−313
(3S,5S)−5−(3−メチル−1H−ピラゾール−4−イル)−1−[2−(6−トリフルオロメチル−イミダゾ[1,2−a]ピリジン−3−イル)−ピリミジン−4−イル]−ピペリジン−3−オール I−314。
(3R,5R)−5−(3−メチル−1H−ピラゾール−4−イル)−1−[2−(6−トリフルオロメチル−イミダゾ[1,2−a]ピリジン−3−イル)−ピリミジン−4−イル]−ピペリジン−3−オール I−315
(3S,5S)−1−(4−(6−クロロイミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−2−イル)−5−ヒドロキシピペリジン−3−カルボキサミド、I−316
(((3S,5R)−1−(2−(6−ブロモ−7−フルオロイミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)−5−メチルピペリジン−3−イル)イミノ)ジメチル−λ6−スルファノン、I−317
3−(4−(3−(1H−ピラゾール−4−イル)ピペリジン−1−イル)ピリミジン−2−イル)−N−シクロプロピルイミダゾ[1,2−a]ピリジン−6−スルホンアミド、I−318
N−シクロプロピル−3−(4−((3R,5S)−3−((ジメチル(オキソ)−λ6−スルファニリデン)アミノ)−5−メチルピペリジン−1−イル)ピリミジン−2−イル)イミダゾ[1,2−a]ピリジン−6−スルホンアミド、I−319、
3−(4−(3−(1H−ピラゾール−4−イル)ピペリジン−1−イル)ピリミジン−2−イル)イミダゾ[1,2−a]ピリジン−6−スルホンアミド、I−320
3−(4−(2−メチル−3−(5−メチル−1H−ピラゾール−4−イル)ピペラジン−1−イル)ピリミジン−2−イル)−6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン、I−321
(R)−1−シクロプロピル−4−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペラジン−2−カルボキサミド、I−323
(S)−1−シクロプロピル−4−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペラジン−2−カルボキサミド、I−324
ジメチル({[(3S,5R)−5−メチル−1−(2−{6−フェノキシイミダゾ[1,2−a]ピリジン−3−イル}ピリミジン−4−イル)ピペリジン−3−イル]イミノ})−λ6−スルファノン I−325
3−(4−(3−(1H−ピラゾール−4−イル)ピペリジン−1−イル)ピリミジン−2−イル)−6−ブロモ−7−フルオロイミダゾ[1,2−a]ピリジン、I−326
N−(1−(4−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)モルホリン−2−イル)エチル)メタンスルホンアミド、I−327
3−(4−((3R,5S)−3−((ジメチル(オキソ)−λ6−スルファニリデン)アミノ)−5−メチルピペリジン−1−イル)ピリミジン−2−イル)イミダゾ[1,2−a]ピリジン−6−スルホンアミド、I−328
2−{6−フェノキシイミダゾ[1,2−a]ピリジン−3−イル}−4−[3−(1H−ピラゾール−4−イル)ピペリジン−1−イル]ピリミジン I−329
(((3S,5R)−1−(2−(6−(3−フルオロアゼチジン−1−イル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)−5−メチルピペリジン−3−イル)イミノ)ジメチル−λ6−スルファノン、I−330
6−メチル−4−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)モルホリン−2−カルボニトリル、I−331
3−メチル−5−(1−メチル−4−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペラジン−2−イル)−1,2,4−オキサジアゾール、I−332
3−(4−(3,3−ジメチル−4−(2,2,2−トリフルオロエチル)ピペラジン−1−イル)ピリミジン−2−イル)−6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン、I−333
3−(4−(3,3−ジメチルピペラジン−1−イル)ピリミジン−2−イル)−6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン、I−334
3−(4−(4−(2−メトキシエチル)−3,5−ジメチルピペラジン−1−イル)ピリミジン−2−イル)−6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン、I−335
1−(2,2−ジメチル−4−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペラジン−1−イル)エタン−1−オン、I−336
3−(4−(3−(5−メチル−4H−1,2,4−トリアゾール−3−イル)ピペラジン−1−イル)ピリミジン−2−イル)−6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン、I−337
8−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)オクタヒドロピラジノ[2,1−c][1,4]チアジン2,2−ジオキシド、I−338
3−(4−(3,3−ジメチル−4−(メチルスルホニル)ピペラジン−1−イル)ピリミジン−2−イル)−6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン、I−339
(((3S,5R)−1−(2−(6−(ジフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)−5−メチルピペリジン−3−イル)イミノ)ジメチル−λ6−スルファノン、I−340
(2S,6S)−4−(2−(6−シクロプロピル−7−フルオロイミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)−2−メチル−6−(3−メチル−1,2,4−オキサジアゾール−5−イル)モルホリン、I−341
ジメチル(((3R,5R)−5−(5−メチル−1H−ピラゾール−4−イル)−1−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペリジン−3−イル)イミノ)−λ6−スルファノン、I−342
(2R,6R)−2−メチル−6−(5−メチルイソオキサゾール−4−イル)−4−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)モルホリン、I−343
ジメチル(((3S,5R)−5−(5−メチル−1H−ピラゾール−4−イル)−1−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペリジン−3−イル)イミノ)−λ6−スルファノン、I−344
(2S,6S)−2−メチル−6−(5−メチルイソオキサゾール−4−イル)−4−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)モルホリン、I−345
(2S,6R)−2−メチル−6−(5−メチルイソオキサゾール−4−イル)−4−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)モルホリン、I−346
(2R,6S)−2−メチル−6−(5−メチルイソオキサゾール−4−イル)−4−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)モルホリン、I−347
3−(4−(4−(1−エトキシシクロプロピル)−2−メチル−3−(1H−ピラゾール−4−イル)ピペラジン−1−イル)ピリミジン−2−イル)−6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン、I−348
(R)−4−(2−(6−クロロイミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)−1−シクロプロピルピペラジン−2−カルボキサミド、I−349
(s)−4−(2−(6−クロロイミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)−1−シクロプロピルピペラジン−2−カルボキサミド、I−350
3−(4−(3−(1H−ピラゾール−4−イル)ピペラジン−1−イル)ピリミジン−2−イル)−6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン、I−351
3−(2−(1H−ピラゾール−4−イル)−4−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペラジン−1−イル)プロパン−1,2−ジオール、I−352
4−((2−(1H−ピラゾール−4−イル)−4−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペラジン−1−イル)メチル)オキサゾール、I−353
3−(4−(3−(1H−ピラゾール−4−イル)−4−((テトラヒドロ−2H−ピラン−4−イル)メチル)ピペラジン−1−イル)ピリミジン−2−イル)−6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン、I−354
6−(トリフルオロメチル)−3−(4−(3−(3−(トリフルオロメチル)−1H−ピラゾール−1−イル)ピペリジン−1−イル)ピリミジン−2−イル)イミダゾ[1,2−a]ピリジン、I−355
3−(4−(3−(1H−1,2,4−トリアゾール−1−イル)ピペリジン−1−イル)ピリミジン−2−イル)−6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン、I−356
3−(4−(3−フルオロ−5−(3−メチル−1H−ピラゾール−4−イル)ピペリジン−1−イル)ピリミジン−2−イル)−6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン、I−357
2−メチル−6−(3−メチル−1H−ピラゾール−4−イル)−4−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)モルホリン、I−358
(2S,6R)−4−(2−(7−クロロ−6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)−2−メチル−6−(3−メチル−1H−ピラゾール−4−イル)モルホリン、I−359
(2R,6R)−4−(2−(7−クロロ−6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)−2−メチル−6−(3−メチル−1H−ピラゾール−4−イル)モルホリン、I−360
3−(4−((2S,3R)−2−メチル−4−(オキセタン−3−イル)−3−(1H−ピラゾール−4−イル)ピペラジン−1−イル)ピリミジン−2−イル)−6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン、I−361
4−[(2R,3S)−2−メチル−4−(オキセタン−3−イル)−3−(1H−ピラゾール−4−イル)ピペラジン−1−イル]−2−[6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル]ピリミジン、I−362
3−(4−((2R,3R)−2−メチル−4−(オキセタン−3−イル)−3−(1H−ピラゾール−4−イル)ピペラジン−1−イル)ピリミジン−2−イル)−6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン、I−363
3−(4−((2S,3S)−2−メチル−4−(オキセタン−3−イル)−3−(1H−ピラゾール−4−イル)ピペラジン−1−イル)ピリミジン−2−イル)−6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン、I−364
3−(4−(2S,3R)−2−メチル−3−(5−メチル−1H−ピラゾール−4−イル)−4−(オキセタン−3−イル)ピペラジン−1−イル)ピリミジン−2−イル)−6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン、I−365
3−(4−(2R,3S)−2−メチル−3−(5−メチル−1H−ピラゾール−4−イル)−4−(オキセタン−3−イル)ピペラジン−1−イル)ピリミジン−2−イル)−6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン、I−366
3−(4−(2S,3S)−2−メチル−3−(5−メチル−1H−ピラゾール−4−イル)−4−(オキセタン−3−イル)ピペラジン−1−イル)ピリミジン−2−イル)−6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン、I−367
3−(4−(2R,3R)−2−メチル−3−(5−メチル−1H−ピラゾール−4−イル)−4−(オキセタン−3−イル)ピペラジン−1−イル)ピリミジン−2−イル)−6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン、I−368
4−[4−(シクロプロピルメチル)−3−(1H−ピラゾール−4−イル)ピペラジン−1−イル]−2−[6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル]ピリミジン、I−369
3−(4−(4−((3−オキサビシクロ[3.1.0]ヘキサン−6−イル)メチル)−3−(1H−ピラゾール−4−イル)ピペラジン−1−イル)ピリミジン−2−イル)−6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン、I−370
3−(4−(4−((1H−イミダゾール−2−イル)メチル)−3−(1H−ピラゾール−4−イル)ピペラジン−1−イル)ピリミジン−2−イル)−6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン、I−371
3−(4−(4−((2−メチル−1H−イミダゾール−5−イル)メチル)−3−(1H−ピラゾール−4−イル)ピペラジン−1−イル)ピリミジン−2−イル)−6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン、I−372
3−(4−(4−((2−(tert−ブチル)−1H−イミダゾール−5−イル)メチル)−3−(1H−ピラゾール−4−イル)ピペラジン−1−イル)ピリミジン−2−イル)−6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン、I−373
3−(4−(4−(オキセタン−3−イルメチル)−3−(1H−ピラゾール−4−イル)ピペラジン−1−イル)ピリミジン−2−イル)−6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン、I−374
(2R,6R)−4−(2−(6−(ジフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)−2−メチル−6−(3−メチル−1,2,4−オキサジアゾール−5−イル)モルホリン、I−375
(((3S,5R)−1−(2−(6−シクロプロピル−7−フルオロイミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)−5−メチルピペリジン−3−イル)イミノ)ジメチル−λ6−スルファノン、I−376
6−シクロプロピル−7−フルオロ−3−(4−(3−フルオロ−5−(5−メチル−1H−ピラゾール−4−イル)ピペリジン−1−イル)ピリミジン−2−イル)イミダゾ[1,2−a]ピリジン、I−377
4−(2−(6−(ジフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)−3−メチルピペラジン−2−カルボキサミド、I−378
3−(4−(3−メチル−4−(1H−ピラゾール−1−イル)ピペリジン−1−イル)ピリミジン−2−イル)−6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン、I−379
3−メチル−4−{2−[6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル]ピリミジン−4−イル}ピペラジン−2−カルボキサミド、I−380
(1−(1−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペリジン−3−イル)−1H−1,2,3−トリアゾール−4−イル)メタノール、I−382
3−(2−(1H−ピラゾール−4−イル)−4−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペラジン−1−イル)シクロブタン−1−オール、I−383
3−(4−(4−((1−メチル−1H−ピラゾール−4−イル)メチル)−3−(1H−ピラゾール−4−イル)ピペラジン−1−イル)ピリミジン−2−イル)−6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン、I−384
3−(4−(4−((1H−イミダゾール−5−イル)メチル)−3−(1H−ピラゾール−4−イル)ピペラジン−1−イル)ピリミジン−2−イル)−6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン、I−385
8−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)−5−オキサ−2,8−ジアザスピロ[3.5]ノナン−2−カルボン酸tert−ブチル、I−386
6−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)−2,6−ジアザスピロ[3.5]ノナン−2−カルボン酸tert−ブチル、I−387
9,9−ジメチル−8−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)−5−オキサ−2,8−ジアザスピロ[3.5]ノナン−2−カルボン酸tert−ブチル、I−388
4−(2−(6−クロロ−7−フルオロイミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)−1−シクロプロピルピペラジン−2−カルボキサミド、I−389
(3−(2−(1H−ピラゾール−4−イル)−4−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペラジン−1−イル)シクロブチル)メタノール、I−390
(2−(1H−ピラゾール−4−イル)−4−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペラジン−1−イル)(1−イソプロピル−1H−ピラゾール−4−イル)メタノン、I−391
3−(4−(4−シクロプロピル−3,5−ジメチルピペラジン−1−イル)ピリミジン−2−イル)−6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン、I−392
2−(2,6−ジメチル−4−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペラジン−1−イル)アセトニトリル、I−393
N−(((1R,4S)−2−(2−(6−(ジフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)−2−アザビシクロ[2.2.2]オクタン−6−イル)メチル)メタンスルホンアミド、I−394
6−(2−(6−(ジフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)−2−(メチルスルホニル)−2,6−ジアザスピロ[3.5]ノナン、I−395
8−(2−(6−(ジフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)−6,6−ジメチル−2−(メチルスルホニル)−5−オキサ−2,8−ジアザスピロ[3.5]ノナン、I−396
(2−(1H−ピラゾール−4−イル)−4−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペラジン−1−イル)(シクロプロピル)メタノン、I−397
2−{6−フェノキシイミダゾ[1,2−a]ピリジン−3−イル}−4−[(3R)−3−(1H−ピラゾール−4−イル)ピペリジン−1−イル]ピリミジン I−398
2−{6−フェノキシイミダゾ[1,2−a]ピリジン−3−イル}−4−[(3S)−3−(1H−ピラゾール−4−イル)ピペリジン−1−イル]ピリミジン I−399
(2−(1H−ピラゾール−4−イル)−4−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペラジン−1−イル)(2,2−ジフルオロシクロプロピル)メタノン、I−400
(cis−2,6−ジメチル−4−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペラジン−1−イル)(1−イソプロピル−1H−ピラゾール−3−イル)メタノン、I−401
(2−(1H−ピラゾール−4−イル)−4−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペラジン−1−イル)(3,3−ジフルオロシクロブチル)メタノン、I−402
シクロプロピル(cis−2,6−ジメチル−4−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペラジン−1−イル)メタノン、I−403
N−((R)−1−((S)−4−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)モルホリン−2−イル)エチル)メタンスルホンアミド、I−404
N−((S)−1−((R)−4−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)モルホリン−2−イル)エチル)メタンスルホンアミド、I−405
N−((R)−1−((R)−4−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)モルホリン−2−イル)エチル)メタンスルホンアミド、I−406
N−((S)−1−((S)−4−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)モルホリン−2−イル)エチル)メタンスルホンアミド、I−407
3−(4−((3R,5S)−3−メチル−5−(5−メチル−2H−1,2,3−トリアゾール−4−イル)ピペリジン−1−イル)ピリミジン−2−イル)−6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン、I−408
3−(4−((3S,5R)−3−メチル−5−(5−メチル−2H−1,2,3−トリアゾール−4−イル)ピペリジン−1−イル)ピリミジン−2−イル)−6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン、I−409
3−(4−(cis−3,5−ジメチル−4−(2,2,2−トリフルオロエチル)ピペラジン−1−イル)ピリミジン−2−イル)−6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン、I−410
3−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)−3,9−ジアザビシクロ[3.3.1]ノナン−9−カルボン酸tert−ブチル、I−411
8−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)−5−オキサ−2,8−ジアザスピロ[3.5]ノナン、I−412
6−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)−2,6−ジアザスピロ[3.5]ノナン、I−413
1−(cis−2,6−ジメチル−4−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペラジン−1−イル)エタン−1−オン、I−414
(2−(1H−ピラゾール−4−イル)−4−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペラジン−1−イル)(1−(2−ヒドロキシエチル)−1H−ピラゾール−4−イル)メタノン、I−415
(2−(1H−ピラゾール−4−イル)−4−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペラジン−1−イル)(1−(2−メトキシエチル)−1H−ピラゾール−4−イル)メタノン、I−416
(2−(1H−ピラゾール−4−イル)−4−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペラジン−1−イル)(1−(オキセタン−3−イル)−1H−ピラゾール−4−イル)メタノン、I−417
(2−(1H−ピラゾール−4−イル)−4−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペラジン−1−イル)(1−メチル−1H−ピラゾール−4−イル)メタノン、I−418
(2−(1H−ピラゾール−4−イル)−4−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペラジン−1−イル)(1−メチル−1H−ピラゾール−5−イル)メタノン、I−419
1−(2−(1H−ピラゾール−4−イル)−4−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペラジン−1−イル)−2−ヒドロキシプロパン−1−オン、I−420
1−(2−(1H−ピラゾール−4−イル)−4−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペラジン−1−イル)−2−ヒドロキシエタン−1−オン、I−421
1−(2−(1H−ピラゾール−4−イル)−4−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペラジン−1−イル)−3−(1H−イミダゾール−1−イル)プロパン−1−オン、I−422
1−(2−(1H−ピラゾール−4−イル)−4−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペラジン−1−イル)−3−(3,5−ジメチル−1H−ピラゾール−1−イル)プロパン−1−オン、I−423
(S)−4−(2−(6−クロロ−7−フルオロイミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)−1−シクロプロピルピペラジン−2−カルボキサミド、I−424
(R)−4−(2−(6−クロロ−7−フルオロイミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)−1−シクロプロピルピペラジン−2−カルボキサミド、I−425
6−クロロ−7−フルオロ−3−(4−(3−フルオロ−5−(5−メチル−1H−ピラゾール−4−イル)ピペリジン−1−イル)ピリミジン−2−イル)イミダゾ[1,2−a]ピリジン、I−426
4−(2−(6−シクロプロピル−7−フルオロイミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)−3−メチルピペラジン−2−カルボキサミド、I−427
(2S,6S)−4−(2−(6−シクロプロピル−7−フルオロイミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)−2−メチル−6−(5−メチル−1H−ピラゾール−4−イル)モルホリン、I−428
(2S,6R)−4−(2−(6−シクロプロピル−7−フルオロイミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)−2−メチル−6−(5−メチル−1H−ピラゾール−4−イル)モルホリン、I−429
1−(2−(1H−ピラゾール−4−イル)−4−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペラジン−1−カルボニル)シクロプロパン−1−カルボニトリル、I−432
(R)−1−(4−(4−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペラジン−2−イル)−1H−ピラゾール−1−カルボニル)シクロプロパン−1−カルボニトリル、I−433
(2R,3R)−3−メチル−4−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペラジン−2−カルボキサミド、I−434
(2S,3S)−3−メチル−4−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペラジン−2−カルボキサミド、I−435
N−(((2R,3S)−3−メチル−4−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペラジン−2−イル)メチル)メタンスルホンアミド、I−436
(3,3−ジフルオロシクロブチル)(cis−2,6−ジメチル−4−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペラジン−1−イル)メタノン、I−437
(2,2−ジフルオロシクロプロピル)(cis−2,6−ジメチル−4−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペラジン−1−イル)メタノン、I−438
3−(4−(cis−3,5−ジメチル−4−(メチルスルホニル)ピペラジン−1−イル)ピリミジン−2−イル)−6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン、I−439
(1−シクロプロピル−1H−ピラゾール−3−イル)(cis−2,6−ジメチル−4−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペラジン−1−イル)メタノン、I−440
(2−(1H−ピラゾール−4−イル)−4−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペラジン−1−イル)(1,2,5−オキサジアゾール−3−イル)メタノン、I−441
(2−(1H−ピラゾール−4−イル)−4−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペラジン−1−イル)(2H−1,2,3−トリアゾール−4−イル)メタノン、I−442
(2−(1H−ピラゾール−4−イル)−4−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペラジン−1−イル)(オキサゾール−4−イル)メタノン、I−443
(2−(1H−ピラゾール−4−イル)−4−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペラジン−1−イル)(イソオキサゾール−4−イル)メタノン、I−444
(2−(1H−ピラゾール−4−イル)−4−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペラジン−1−イル)(1H−イミダゾール−4−イル)メタノン、I−445
(2−(1H−ピラゾール−4−イル)−4−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペラジン−1−イル)(1−メチル−1H−イミダゾール−4−イル)メタノン、I−446
2−(メチルスルホニル)−8−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)−5−オキサ−2,8−ジアザスピロ[3.5]ノナン、I−447
2−(メチルスルホニル)−6−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)−2,6−ジアザスピロ[3.5]ノナン、I−448
3−(4−(3−(1H−ピラゾール−4−イル)−4−(3,3,3−トリフルオロプロピル)ピペラジン−1−イル)ピリミジン−2−イル)−6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン、I−449
3−(4−(4−(3,4−ジフルオロベンジル)−3−(1H−ピラゾール−4−イル)ピペラジン−1−イル)ピリミジン−2−イル)−6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン、I−450
4−(2−{6−クロロイミダゾ[1,2−a]ピリジン−3−イル}ピリミジン−4−イル)−3−メチルピペラジン−2−カルボキサミド、I−451
(2−(1H−ピラゾール−4−イル)−4−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペラジン−1−イル)(2−メトキシピリジン−4−イル)メタノン、I−452
(2R,3S)−4−(2−(6−シクロプロピル−7−フルオロイミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)−3−メチルピペラジン−2−カルボキサミド、I−454
4−(2−(6−シクロプロピル−7−フルオロイミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)−3−メチルピペラジン−2−カルボキサミド、I−455
3−(4−(3−(1H−ピラゾール−4−イル)−4−(テトラヒドロ−2H−ピラン−4−イル)ピペラジン−1−イル)ピリミジン−2−イル)−6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン、I−456
3−(4−(4−(4−フルオロベンジル)−3−(1H−ピラゾール−4−イル)ピペラジン−1−イル)ピリミジン−2−イル)−6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン、I−457
3−(4−(4−(3−フルオロベンジル)−3−(1H−ピラゾール−4−イル)ピペラジン−1−イル)ピリミジン−2−イル)−6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン、I−458
3−(4−(4−(2−フルオロベンジル)−3−(1H−ピラゾール−4−イル)ピペラジン−1−イル)ピリミジン−2−イル)−6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン、I−459
3−(4−(4−(4,4−ジフルオロシクロヘキシル)−3−(1H−ピラゾール−4−イル)ピペラジン−1−イル)ピリミジン−2−イル)−6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン、I−460
4−{4−[(1,2,5−オキサジアゾール−3−イル)メチル]−3−(1H−ピラゾール−4−イル)ピペラジン−1−イル}−2−[6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル]ピリミジン、I−461
3−(4−(cis−3,5−ジメチル−4−((テトラヒドロ−2H−ピラン−4−イル)メチル)ピペラジン−1−イル)ピリミジン−2−イル)−6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン、I−462
3−(2−((3R,5S)−3−(3,5−ジメチル−4H−1,2,4−トリアゾール−4−イル)−5−メチルピペリジン−1−イル)ピリミジン−4−イル)−6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン、I−463
1−(cis−2,6−ジメチル−4−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペラジン−1−イル)−2−(テトラヒドロ−2H−ピラン−4−イル)エタン−1−オン、I−464
3−(2−((3S,5S)−3−(3,5−ジメチル−4H−1,2,4−トリアゾール−4−イル)−5−メチルピペリジン−1−イル)ピリミジン−4−イル)−6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン、I−465
3−(2−((3S,5R)−3−(3,5−ジメチル−4H−1,2,4−トリアゾール−4−イル)−5−メチルピペリジン−1−イル)ピリミジン−4−イル)−6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン、I−466
3−(2−((3R,5R)−3−(3,5−ジメチル−4H−1,2,4−トリアゾール−4−イル)−5−メチルピペリジン−1−イル)ピリミジン−4−イル)−6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン、I−467
(2−(1H−ピラゾール−4−イル)−4−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペラジン−1−イル)(スピロ[2.2]ペンタン−1−イル)メタノン、I−468
5−(2−(1H−ピラゾール−4−イル)−4−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペラジン−1−カルボニル)ピロリジン−2−オン、I−469
3−(4−(4−((2,2−ジフルオロシクロプロピル)メチル)−3−(1H−ピラゾール−4−イル)ピペラジン−1−イル)ピリミジン−2−イル)−6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン、I−470
N−(((2S,3S)−3−メチル−4−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペラジン−2−イル)メチル)メタンスルホンアミド、I−471
N−((1−シクロプロピル−4−(2−(6−(ジフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)−3−メチルピペラジン−2−イル)メチル)メタンスルホンアミド、I−472
3−(4−(4−((2−メチルシクロプロピル)メチル)−3−(1H−ピラゾール−4−イル)ピペラジン−1−イル)ピリミジン−2−イル)−6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン、I−473
(S)−6−((S)−2−(1H−ピラゾール−4−イル)−4−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペラジン−1−カルボニル)ピペリジン−2−オン、I−474
3−(4−(3−(1H−ピラゾール−4−イル)−4−(スピロ[2.2]ペンタン−1−イルメチル)ピペラジン−1−イル)ピリミジン−2−イル)−6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン、I−475
3−(4−(4−((2,2−ジメチルシクロプロピル)メチル)−3−(1H−ピラゾール−4−イル)ピペラジン−1−イル)ピリミジン−2−イル)−6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン、I−477
N−(5−(トリフルオロメチル)−1−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペリジン−3−イル)メタンスルホンアミド、I−478
(R)−(1,3−ジメチル−1H−ピラゾール−4−イル)(2−メチル−4−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペラジン−1−イル)メタノン、I−479
(S)−(1,3−ジメチル−1H−ピラゾール−4−イル)(2−メチル−4−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペラジン−1−イル)メタノン、I−480
3−(4−((2S,3R)−2−メチル−4−((3−メチルオキセタン−3−イル)メチル)−3−(1H−ピラゾール−4−イル)ピペラジン−1−イル)ピリミジン−2−イル)−6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン、I−481
3−(4−((2S,3S)−2−メチル−4−((3−メチルオキセタン−3−イル)メチル)−3−(1H−ピラゾール−4−イル)ピペラジン−1−イル)ピリミジン−2−イル)−6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン、I−482
(cis−2,6−ジメチル−4−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペラジン−1−イル)(ピリジン−4−イル)メタノン、I−483
(2−(1H−ピラゾール−4−イル)−4−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペラジン−1−イル)((1R,2R)−2−フルオロシクロプロピル)メタノン、I−485
(cis−2,6−ジメチル−4−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペラジン−1−イル)(1−メチルシクロプロピル)メタノン、I−486
(2−(1H−ピラゾール−4−イル)−4−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペラジン−1−イル)(テトラヒドロ−2H−ピラン−4−イル)メタノン、I−487
(2−(1H−ピラゾール−4−イル)−4−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペラジン−1−イル)(1−(ジフルオロメチル)シクロプロピル)メタノン、I−488
(2−(1H−ピラゾール−4−イル)−4−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペラジン−1−イル)((1R,2R)−2−フルオロシクロプロピル)メタノン、I−489
N−(((2R,3S,6S)−1−シクロプロピル−3,6−ジメチル−4−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペラジン−2−イル)メチル)メタンスルホンアミド、I−491
4−(2,2−ジメチル−4−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペラジン−1−カルボニル)シクロヘキサン−1−オン、I−492
N−(((2R,3R,6R)−1−シクロプロピル−3,6−ジメチル−4−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペラジン−2−イル)メチル)メタンスルホンアミド、I−493
N−(((2S,3R,6R)−1−シクロプロピル−3,6−ジメチル−4−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペラジン−2−イル)メチル)メタンスルホンアミド、I−494
N−((4−(2−(6−(ジフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)−3−(トリフルオロメチル)ピペラジン−2−イル)メチル)メタンスルホンアミド、I−496
(2R,6R)−4−(2−(6−(ジフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)−2−メチル−6−(3−メチル−1,2,4−オキサジアゾール−5−イル)モルホリン、I−497
(2S,6S)−4−(2−(6−(ジフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)−2−メチル−6−(3−メチル−1,2,4−オキサジアゾール−5−イル)モルホリン、I−498
(((3S,5R)−1−(4−(6−(ジフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−2−イル)−5−メチルピペリジン−3−イル)イミノ)ジメチル−λ6−スルファノン、I−499
N−((S)−1−((2S,3S)−1−シクロプロピル−3−メチル−4−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペラジン−2−イル)エチル)メタンスルホンアミド、I−500
1−(cis−2,6−ジメチル−4−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペラジン−1−イル)−2−(オキセタン−3−イル)エタン−1−オン、I−501
(S)−3−(4−(3−(1H−ピラゾール−4−イル)−4−(2−オキサスピロ[3.3]ヘプタン−6−イル)ピペラジン−1−イル)ピリミジン−2−イル)−6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン、I−502
(R)−3−(4−(4−シクロプロピル−3−(1H−ピラゾール−4−イル)ピペラジン−1−イル)ピリミジン−2−イル)−6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン、I−503
(R)−3−(4−(3−(1H−ピラゾール−4−イル)−4−(2−オキサスピロ[3.3]ヘプタン−6−イル)ピペラジン−1−イル)ピリミジン−2−イル)−6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン、I−504
N−((R)−1−((2R,3R)−1−シクロプロピル−3−メチル−4−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペラジン−2−イル)エチル)メタンスルホンアミド、I−505
N−((R)−1−((2S,3S)−1−シクロプロピル−3−メチル−4−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペラジン−2−イル)エチル)メタンスルホンアミド、I−506
N−((S)−1−((2R,3R)−1−シクロプロピル−3−メチル−4−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペラジン−2−イル)エチル)メタンスルホンアミド、I−507
3−{2−[(R)−4−シクロプロピル−3−(1H−ピラゾール−4−イル)−ピペラジン−1−イル]−ピリミジン−4−イル}−6−トリフルオロメチル−イミダゾ[1,2−a]ピリジン、I−508、
(2−(1H−ピラゾール−4−イル)−4−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペラジン−1−イル)(3−ヒドロキシ−3−メチルシクロブチル)メタノン、I−509
3−(4−(4−((1−メチルシクロプロピル)メチル)−3−(1H−ピラゾール−4−イル)ピペラジン−1−イル)ピリミジン−2−イル)−6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン、I−510
4−[(2R,3S)−4−{[1−(メトキシメチル)シクロブチル]メチル}−2−メチル−3−(1H−ピラゾール−4−イル)ピペラジン−1−イル]−2−[6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル]ピリミジン、I−511
4−[(2S,3S)−4−{[1−(メトキシメチル)シクロブチル]メチル}−2−メチル−3−(1H−ピラゾール−4−イル)ピペラジン−1−イル]−2−[6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル]ピリミジン、I−512
(6,7−ジヒドロ−4H−ピラゾロ[5,1−c][1,4]オキサジン−2−イル)(cis−2,6−ジメチル−4−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペラジン−1−イル)メタノン、I−513
1−(2−(1H−ピラゾール−4−イル)−4−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペラジン−1−イル)−2−ヒドロキシ−2−メチルプロパン−1−オン、I−514
(2−(1H−ピラゾール−4−イル)−4−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペラジン−1−イル)(5−メチルイソオキサゾール−4−イル)メタノン、I−515
N−(((2R,3S)−1−シクロプロピル−4−(2−(6−(ジフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)−3−メチルピペラジン−2−イル)メチル)メタンスルホンアミド、I−516
N−(((2S,3R)−1−シクロプロピル−4−(2−(6−(ジフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)−3−メチルピペラジン−2−イル)メチル)メタンスルホンアミド、I−517
(2−(1H−ピラゾール−4−イル)−4−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペラジン−1−イル)(4−メチル−1,2,5−オキサジアゾール−3−イル)メタノン、I−518
(2−(1H−ピラゾール−4−イル)−4−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペラジン−1−イル)(3,5−ジメチルイソオキサゾール−4−イル)メタノン、I−519
3−(4−((R)−4−(((R)−6−オキサスピロ[2.5]オクタン−1−イル)メチル)−3−(1H−ピラゾール−4−イル)ピペラジン−1−イル)ピリミジン−2−イル)−6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン、I−520
3−(4−((S)−4−(((S)−6−オキサスピロ[2.5]オクタン−1−イル)メチル)−3−(1H−ピラゾール−4−イル)ピペラジン−1−イル)ピリミジン−2−イル)−6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン、I−521
3−(4−((S)−4−(((R)−6−オキサスピロ[2.5]オクタン−1−イル)メチル)−3−(1H−ピラゾール−4−イル)ピペラジン−1−イル)ピリミジン−2−イル)−6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン、I−522
3−(4−((R)−4−(((S)−6−オキサスピロ[2.5]オクタン−1−イル)メチル)−3−(1H−ピラゾール−4−イル)ピペラジン−1−イル)ピリミジン−2−イル)−6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン、I−523
((2S,6S)−4−(2−(6−(ジフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)−6−メチルモルホリン−2−イル)メタノール、I−524
N−(1−(4−(6−(ジフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−2−イル)−5−(トリフルオロメチル)ピペリジン−3−イル)メタンスルホンアミド、I−525
3−(4−((R)−4−(((R)−2,2−ジメチルシクロプロピル)メチル)−3−(1H−ピラゾール−4−イル)ピペラジン−1−イル)ピリミジン−2−イル)−6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン、I−526
3−(4−((S)−4−(((S)−2,2−ジメチルシクロプロピル)メチル)−3−(1H−ピラゾール−4−イル)ピペラジン−1−イル)ピリミジン−2−イル)−6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン、I−527
3−(4−((S)−4−(((R)−2,2−ジメチルシクロプロピル)メチル)−3−(1H−ピラゾール−4−イル)ピペラジン−1−イル)ピリミジン−2−イル)−6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン、I−528
3−(4−((R)−4−(((S)−2,2−ジメチルシクロプロピル)メチル)−3−(1H−ピラゾール−4−イル)ピペラジン−1−イル)ピリミジン−2−イル)−6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン、I−529
N−((4−(2−(6−(ジフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)−3−メチル−1−(オキセタン−3−イル)ピペラジン−2−イル)メチル)メタンスルホンアミド、I−530
N−(1−(2−(6−(ジフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)−5−(トリフルオロメチル)ピペリジン−3−イル)メタンスルホンアミド、I−531
(R)−3−(4−(3−(1H−ピラゾール−4−イル)ピペラジン−1−イル)ピリミジン−2−イル)−6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン、I−532
(S)−3−(4−(3−(1H−ピラゾール−4−イル)ピペラジン−1−イル)ピリミジン−2−イル)−6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン、I−533
3−(4−((2S,3R)−2−メチル−3−(1H−ピラゾール−4−イル)ピペラジン−1−イル)ピリミジン−2−イル)−6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン、I−534
3−(4−((2S,3S)−2−メチル−3−(1H−ピラゾール−4−イル)ピペラジン−1−イル)ピリミジン−2−イル)−6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン、I−535
3−(4−((2R,3R)−2−メチル−3−(1H−ピラゾール−4−イル)ピペラジン−1−イル)ピリミジン−2−イル)−6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン、I−536
4−[(2R,3S)−2−メチル−3−(1H−ピラゾール−4−イル)ピペラジン−1−イル]−2−[6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル]ピリミジン、I−537
(2R,6R)−4−(2−(6−クロロ−7−フルオロイミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)−2−メチル−6−(5−メチル−1H−ピラゾール−4−イル)モルホリン、I−538
(2S,6S)−4−(2−(6−クロロ−7−フルオロイミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)−2−メチル−6−(5−メチル−1H−ピラゾール−4−イル)モルホリン、I−539
(2R,6S)−4−(2−(6−クロロ−7−フルオロイミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)−2−メチル−6−(5−メチル−1H−ピラゾール−4−イル)モルホリン、I−540
N−(((2R,3S)−1−シクロプロピル−3−メチル−4−(4−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−2−イル)ピペラジン−2−イル)メチル)メタンスルホンアミド、I−541
3−(2−((S)−3−(1H−ピラゾール−4−イル)−4−(((R)−テトラヒドロ−2H−ピラン−3−イル)メチル)ピペラジン−1−イル)ピリミジン−4−イル)−6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン、I−542
N−{(2S,3R)−1−シクロプロピル−3−メチル−4−[4−(6−トリフルオロメチル−イミダゾ[1,2−a]ピリジン−3−イル)−ピリミジン−2−イル]−ピペラジン−2−イルメチル}−メタンスルホンアミド、I−543
3−(2−((R)−3−(1H−ピラゾール−4−イル)−4−(((S)−テトラヒドロ−2H−ピラン−3−イル)メチル)ピペラジン−1−イル)ピリミジン−4−イル)−6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン、I−544
3−(2−((R)−3−(1H−ピラゾール−4−イル)−4−(((R)−テトラヒドロ−2H−ピラン−3−イル)メチル)ピペラジン−1−イル)ピリミジン−4−イル)−6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン、I−545
3−(2−((S)−3−(1H−ピラゾール−4−イル)−4−(((S)−テトラヒドロ−2H−ピラン−3−イル)メチル)ピペラジン−1−イル)ピリミジン−4−イル)−6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン、I−546
(2R,3R)−4−(2−(6−クロロイミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)−1−シクロプロピル−3−メチルピペラジン−2−カルボキサミド、I−547
(2S,3S)−4−(2−(6−クロロイミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)−1−シクロプロピル−3−メチルピペラジン−2−カルボキサミド、I−548
(S)−(2−(1H−ピラゾール−4−イル)−4−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペラジン−1−イル)(5−メチルイソオキサゾール−4−イル)メタノン、I−549
(R)−(2−(1H−ピラゾール−4−イル)−4−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペラジン−1−イル)(5−メチルイソオキサゾール−4−イル)メタノン、I−550
1−(2−(1H−ピラゾール−4−イル)−4−(4−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−2−イル)ピペラジン−1−カルボニル)シクロプロパン−1−カルボニトリル、I−551
3−(4−((R)−3−(1H−ピラゾール−4−イル)−4−(((R)−スピロ[2.2]ペンタン−1−イル)メチル)ピペラジン−1−イル)ピリミジン−2−イル)−6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン、I−552
3−(4−((S)−3−(1H−ピラゾール−4−イル)−4−(((S)−スピロ[2.2]ペンタン−1−イル)メチル)ピペラジン−1−イル)ピリミジン−2−イル)−6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン、I−553
3−(4−((S)−3−(1H−ピラゾール−4−イル)−4−(((R)−スピロ[2.2]ペンタン−1−イル)メチル)ピペラジン−1−イル)ピリミジン−2−イル)−6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン、I−554
3−(4−((R)−3−(1H−ピラゾール−4−イル)−4−(((S)−スピロ[2.2]ペンタン−1−イル)メチル)ピペラジン−1−イル)ピリミジン−2−イル)−6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン、I−555
(S)−6−(2−(1H−ピラゾール−4−イル)−4−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペラジン−1−イル)−2−チアスピロ[3.3]ヘプタン2,2−ジオキシド、I−556
(R)−6−(2−(1H−ピラゾール−4−イル)−4−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペラジン−1−イル)−2−チアスピロ[3.3]ヘプタン2,2−ジオキシド、I−557
(S)−1−(2−(6−クロロ−7−フルオロイミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)ピペリジン−3−カルボキサミド、I−558
6−クロロ−3−(4−((3R,5S)−3−メチル−5−(1H−ピラゾール−4−イル)ピペリジン−1−イル)ピリミジン−2−イル)イミダゾ[1,2−a]ピリジン、I−559
(2S,6R)−2−メチル−6−(1H−ピラゾール−4−イル)−4−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)モルホリン、I−560
(2R,6S)−4−(2−(6−クロロイミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)−2−メチル−6−(5−メチル−1H−ピラゾール−4−イル)モルホリン、I−561
(2S,6S)−6−メチル−4−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)モルホリン−2−カルボキサミド、I−562
6−クロロ−3−(4−((2S,3R,5S)−2,5−ジメチル−3−(1H−ピラゾール−4−イル)ピペラジン−1−イル)ピリミジン−2−イル)イミダゾ[1,2−a]ピリジン、I−563
(2R,6S)−2−メチル−6−(1H−ピラゾール−4−イル)−4−(2−(6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)モルホリン、I−564
3−(4−((2R,3S)−2−メチル−4−(オキセタン−3−イル)−3−(1H−ピラゾール−4−イル)ピペラジン−1−イル)ピリミジン−2−イル)−6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン、I−565
(2R,6S)−4−(2−(6−クロロイミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)−2−メチル−6−(1H−ピラゾール−4−イル)モルホリン、I−566
3−(4−((3R,5S)−3−メチル−5−(1H−ピラゾール−4−イル)ピペリジン−1−イル)ピリミジン−2−イル)−6−(トリフルオロメチル)イミダゾ[1,2−a]ピリジン、I−567
(2S,6R)−4−(2−(6−クロロ−7−フルオロイミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)−2−メチル−6−(1H−ピラゾール−4−イル)モルホリン、I−568
(((3R,5R)−1−(2−(6−(ジフルオロメチル)イミダゾ[1,2−a]ピリジン−3−イル)ピリミジン−4−イル)−5−メチルピペリジン−3−イル)イミノ)ジメチル−λ6−スルファノン、I−569
実施例26:GCN2阻害についてのヒトIL−2アッセイ
表6.T細胞からのIL−2分泌に基づくEC50値
Claims (38)
- 式I:
環Aは、3員〜8員の飽和もしくは部分不飽和の単環式炭素環式環、フェニル、8員〜10員の二環式芳香族炭素環式環、窒素、酸素、もしくは硫黄から独立して選択される0個〜4個のヘテロ原子を有する5〜6員の芳香環と必要に応じて縮合し、窒素、酸素、もしくは硫黄から独立して選択される1個〜2個のヘテロ原子を有する、4員〜8員の部分不飽和単環式複素環式環、窒素、酸素、もしくは硫黄から独立して選択される1個〜2個のヘテロ原子を有する7員〜12員の部分不飽和スピロ環式複素環式環、窒素、酸素、もしくは硫黄から独立して選択される1個〜4個のヘテロ原子を有する7員〜12員の部分不飽和二環式複素環式環、窒素、酸素、もしくは硫黄から独立して選択される1個〜2個のヘテロ原子を有する7員〜12員の部分不飽和架橋二環式複素環式環、窒素、酸素、もしくは硫黄から独立して選択される1個〜4個のヘテロ原子を有する5員〜6員の単環式ヘテロ芳香環、窒素、酸素、もしくは硫黄から独立して選択される1個〜5個のヘテロ原子を有する8員〜10員の二環式ヘテロ芳香環、または
Hetから選択され、ここでHetは、窒素、酸素、もしくは硫黄から独立して選択される1個〜2個のヘテロ原子を有する4員〜8員の飽和単環式複素環式環、窒素、酸素、もしくは硫黄から独立して選択される1個〜4個のヘテロ原子を有する7員〜12員の飽和スピロ環式複素環式環、窒素、酸素、もしくは硫黄から独立して選択される1個〜3個のヘテロ原子を有する7員〜12員の飽和二環式複素環式環、または窒素、酸素、もしくは硫黄から独立して選択される1個〜2個のヘテロ原子を有する7員〜12員の飽和架橋二環式複素環式環であり;
環Bは、
各Rは独立して、水素であるか、またはC1〜6脂肪族、3員〜8員の飽和もしくは部分不飽和の単環式炭素環式環、フェニル、8員〜10員の二環式芳香族炭素環式環、窒素、酸素、もしくは硫黄から独立して選択される1個〜2個のヘテロ原子を有する4員〜8員の飽和もしくは部分不飽和の単環式複素環式環、窒素、酸素、もしくは硫黄から独立して選択される1個〜4個のヘテロ原子を有する5員〜6員の単環式ヘテロ芳香環、または窒素、酸素、もしくは硫黄から独立して選択される1個〜5個のヘテロ原子を有する8員〜10員の二環式ヘテロ芳香環から選択される必要に応じて置換された基であるか;あるいは
2個のR基は必要に応じて一緒になって、二価C2〜4アルキレン鎖を形成し;
2個のR基は、これらの間にある原子と必要に応じて一緒になって、窒素、酸素もしくは硫黄から独立して選択される0個〜4個のヘテロ原子を有する必要に応じて置換された3員〜7員の飽和もしくは部分不飽和の単環式環を形成し;
各R’は独立して、水素、またはハロゲンで必要に応じて置換されたC1〜3脂肪族基であり;
R1の各々は独立して、水素、ハロゲン、−CN、−NO2、−C(O)R、−C(O)OR、−C(O)NR2、−C(O)NRS(O)2R、−C(O)N=S(O)R2、−NR2、−NRC(O)R、−NRC(O)NR2、−NRC(O)OR、−NRS(O)2R、−NRS(O)2NR2、−OR、−ON(R)SO2R、−P(O)R2、−SR、−S(O)R、−S(O)2R、−S(O)(NH)R、−S(O)2N(R)2、−S(NH2)2(O)OH、−N=S(O)R2、−CH3、−CH2OH、−CH2NHSO2CH3、−CD3、−CD2NRS(O)2R、またはRであるか;あるいは:
2個のR1基は必要に応じて一緒になって、=Oまたは=NHを形成するか;あるいは
2個のR1基は必要に応じて一緒になって、二価C2〜4アルキレン鎖を形成し;
R2の各々は独立して、水素、ハロゲン、−CN、−C(O)N(R’)2、−OR’、−N(R’)2、−S(O)2R、−S(O)2N(R)2、−O−フェニル、または必要に応じて置換された基であり、該必要に応じて置換された基は、C1〜3脂肪族、フェニル、窒素、酸素、もしくは硫黄から独立して選択される1個〜4個のヘテロ原子を有する5員〜6員の単環式ヘテロ芳香環、または窒素、酸素、もしくは硫黄から独立して選択される1個〜4個のヘテロ原子を有する4員〜8員の飽和単環式複素環から選択され;
R3は、水素、ハロゲン、−CN、−OR’、−N(R’)2、または必要に応じて置換された基であり、該必要に応じて置換された基は、C1〜3脂肪族、フェニル、または窒素、酸素、もしくは硫黄から独立して選択される1個〜4個のヘテロ原子を有する5員〜6員の単環式ヘテロ芳香環から選択され;
R4は、水素、ハロゲン、−CN、−OR、−N=S(O)R2、−N(R)2、または必要に応じて置換された基であり、該必要に応じて置換された基は、C1〜3脂肪族、窒素、酸素、もしくは硫黄から独立して選択される1個〜2個のヘテロ原子を有する4員〜8員の飽和もしくは部分不飽和の単環式複素環式環、または窒素、酸素、もしくは硫黄から独立して選択される1個〜2個のヘテロ原子を有する7員〜12員の飽和もしくは部分不飽和のスピロ環式複素環式環から選択され;
mは、0、1、2、3、4または5であり;
nは、0、1、または2であり;
pは、0または1であり;そして
qは、0または1である、
化合物。 - 環AはHetである、請求項1に記載の化合物。
- Hetは、窒素、酸素、もしくは硫黄から独立して選択される1個〜2個のヘテロ原子を有する4員〜8員の飽和単環式複素環式環、窒素、酸素、もしくは硫黄から独立して選択される1個〜4個のヘテロ原子を有する7員〜12員の飽和スピロ環式複素環式環、または窒素、酸素、もしくは硫黄から独立して選択される1個〜3個のヘテロ原子を有する7員〜12員の飽和二環式複素環式環である、請求項2に記載の化合物。
- R1の各々は独立して、水素、ハロゲン、−CN、−C(O)R、−C(O)OR、−C(O)NR2、−C(O)NRS(O)2R、−C(O)N=S(O)R2、−NR2、−NRC(O)R、−NRC(O)NR2、−NRC(O)OR、−NRS(O)2R、−NRS(O)2NR2、−OR、−ON(R)SO2R、−P(O)R2、−SR、−S(O)R、−S(O)2R、−S(O)(NH)R、−S(O)2N(R)2、−S(NH2)2(O)OH、−N=S(O)R2、−CH3、−CH2OH、−CH2NHSO2CH3、−CD3、−CD2NRS(O)2R、またはRである、請求項1に記載の化合物。
- R2の各々は独立して、水素、ハロゲン、−CN、−C(O)N(R’)2、−OR’、−N(R’)2、または必要に応じて置換された基であり、該必要に応じて置換された基は、C1〜3脂肪族、または窒素、酸素、もしくは硫黄から独立して選択される1個〜4個のヘテロ原子を有する5員〜6員の単環式ヘテロ芳香環から選択される、請求項1に記載の化合物。
- R3は、水素、ハロゲン、−CN、−OR’、−N(R’)2、または必要に応じて置換された基であり、該必要に応じて置換された基は、C1〜3脂肪族、または窒素、酸素、もしくは硫黄から独立して選択される1個〜4個のヘテロ原子を有する5員〜6員の単環式ヘテロ芳香環から選択される、請求項1に記載の化合物。
- R4は、水素、ハロゲン、−CN、−OR、−N(R)2、または必要に応じて置換された基であり、該必要に応じて置換された基は、C1〜3脂肪族、窒素、酸素、もしくは硫黄から独立して選択される1個〜2個のヘテロ原子を有する4員〜8員の飽和もしくは部分不飽和の単環式複素環式環、または窒素、酸素、もしくは硫黄から独立して選択される1個〜2個のヘテロ原子を有する7員〜12員の飽和もしくは部分不飽和のスピロ環式複素環式環から選択される、請求項1に記載の化合物。
- mは、1、2、3、4または5であり、特に、1、2または3である、請求項1〜23のいずれか1項に記載の化合物。
- 前記化合物は、表1に図示される化合物から選択される、請求項1に記載の化合物。
- 請求項1〜25のいずれか1項に記載の化合物、および薬学的に受容可能なキャリア、アジュバント、またはビヒクルを含有する、薬学的組成物。
- 患者または生物学的サンプルにおいて、GCN2を阻害する方法であって、請求項1〜25のいずれか1項に記載の化合物、またはその薬学的組成物を、該患者に投与する工程、または該生物学的サンプルと接触させる工程を包含する、方法。
- 患者において、GCN2媒介性の障害、疾患、または状態を処置する方法であって、該患者に、請求項1〜25のいずれか1項に記載の化合物、またはその薬学的組成物を投与する工程を包含する、方法。
- 前記GCN2媒介性の障害、疾患、または状態は、炎症状態、免疫学的状態、自己免疫状態、アレルギー状態、リウマチ状態、血栓症状態、がん、感染、神経変性疾患、変性疾患、神経炎症疾患、心血管疾患、および代謝状態.からなる群より選択される、請求項28に記載の方法。
- 前記がんは、固形腫瘍であって、ここで該固形腫瘍は、上皮、膀胱、胃、腎臓、頭頚部、食道、子宮頚部、甲状腺、腸管、肝臓、脳、前立腺、泌尿生殖路、リンパ系、胃、喉頭、軟骨肉腫およびユーイング肉腫が挙げられる骨、胎児組織腫瘍が挙げられる生殖細胞、および/または肺の腫瘍の群、単球性白血病、肺腺癌、小細胞肺癌、膵臓がん、グリア芽細胞腫、神経線維腫、血管肉腫、乳癌および/または悪性黒色腫の群を起源とする、固形腫瘍、ならびに血液および免疫系の腫瘍の群からなる群より選択される、請求項29に記載の方法。
- 前記自己免疫状態は、関節リウマチ、全身性ループス、多発性硬化症、乾癬、シェーグレン症候群または移植器官拒絶である、請求項29に記載の方法。
- 前記代謝状態は糖尿病である、請求項29に記載の方法。
- 前記変性疾患は骨関節症である、請求項29に記載の方法。
- 前記炎症状態は、喘息、炎症性腸疾患、または巨細胞関節炎である、請求項29に記載の方法。
- 前記心血管疾患は虚血傷害である、請求項29に記載の方法。
- 前記神経変性疾患は、アルツハイマー病、ダウン症候群、アミロイドーシスを伴う遺伝性大脳出血−オランダ型、脳のアミロイドアンギオパチー、クロイツフェルト−ヤコブ病、前頭側頭型痴呆、ハンチントン病、またはパーキンソン病である、請求項29に記載の方法。
- 前記感染は、リーシュマニア、らい菌(M.leprae)、結核菌(M.tuberculosis)および/もしくはM.アビウム(M.avium)が挙げられるマイコバクテリア、マラリア原虫、ヒト免疫不全ウイルス、エプスタイン−バーウイルス、単純ヘルペスウイルス、またはC型肝炎ウイルスにより引き起こされる、請求項29に記載の方法。
- 前記GCN2媒介性の障害、疾患、または状態は、がんであり、そして前記方法は、がんの処置のための第二の薬剤を投与する工程をさらに包含する、請求項28に記載の方法。
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CA3089769A1 (en) | 2019-08-01 |
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CN117659010A (zh) | 2024-03-08 |
AR114236A1 (es) | 2020-08-05 |
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MX2020007797A (es) | 2020-09-18 |
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BR112020015396A2 (pt) | 2020-12-08 |
IL276147A (en) | 2020-09-30 |
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