JP2010513447A5 - - Google Patents
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- JP2010513447A5 JP2010513447A5 JP2009542223A JP2009542223A JP2010513447A5 JP 2010513447 A5 JP2010513447 A5 JP 2010513447A5 JP 2009542223 A JP2009542223 A JP 2009542223A JP 2009542223 A JP2009542223 A JP 2009542223A JP 2010513447 A5 JP2010513447 A5 JP 2010513447A5
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- Prior art keywords
- alkyl
- aryl
- group
- heterocyclyl
- optionally substituted
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- 125000000217 alkyl group Chemical group 0.000 claims 24
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 22
- 150000001875 compounds Chemical class 0.000 claims 21
- 125000000623 heterocyclic group Chemical group 0.000 claims 14
- 125000003118 aryl group Chemical group 0.000 claims 12
- 229910052739 hydrogen Inorganic materials 0.000 claims 11
- 239000001257 hydrogen Substances 0.000 claims 11
- 229910052757 nitrogen Inorganic materials 0.000 claims 11
- 125000003545 alkoxy group Chemical group 0.000 claims 9
- 150000002431 hydrogen Chemical class 0.000 claims 9
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 8
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 8
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 7
- 229910052736 halogen Inorganic materials 0.000 claims 7
- 125000001475 halogen functional group Chemical group 0.000 claims 7
- 150000002367 halogens Chemical class 0.000 claims 7
- -1 -O- (CH 2 ) n -OR x Chemical group 0.000 claims 6
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 6
- 125000004093 cyano group Chemical group *C#N 0.000 claims 5
- 239000008194 pharmaceutical composition Substances 0.000 claims 4
- 229910052799 carbon Inorganic materials 0.000 claims 3
- OKTJSMMVPCPJKN-UHFFFAOYSA-N carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 3
- 125000004122 cyclic group Chemical group 0.000 claims 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 2
- 125000004356 hydroxy functional group Chemical group O* 0.000 claims 2
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 1
- 125000004890 (C1-C6) alkylamino group Chemical group 0.000 claims 1
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 1
- 125000006553 (C3-C8) cycloalkenyl group Chemical group 0.000 claims 1
- UGUHFDPGDQDVGX-UHFFFAOYSA-N 1,2,3-thiadiazole Chemical group C1=CSN=N1 UGUHFDPGDQDVGX-UHFFFAOYSA-N 0.000 claims 1
- PIGSMPOINQICAJ-UHFFFAOYSA-N 1-[2-fluoro-4-[6-(1-tritylpyrazol-4-yl)imidazo[1,2-a]pyridin-3-yl]phenyl]-3-propan-2-ylurea Chemical compound C1=C(F)C(NC(=O)NC(C)C)=CC=C1C1=CN=C2N1C=C(C1=CN(N=C1)C(C=1C=CC=CC=1)(C=1C=CC=CC=1)C=1C=CC=CC=1)C=C2 PIGSMPOINQICAJ-UHFFFAOYSA-N 0.000 claims 1
- KWAOMFSRFDBBRI-UHFFFAOYSA-N 1-[2-fluoro-4-[6-(1H-pyrazol-4-yl)imidazo[1,2-a]pyridin-3-yl]phenyl]-3-propan-2-ylurea Chemical compound C1=C(F)C(NC(=O)NC(C)C)=CC=C1C1=CN=C2N1C=C(C1=CNN=C1)C=C2 KWAOMFSRFDBBRI-UHFFFAOYSA-N 0.000 claims 1
- TUEVVYKIUZPSKK-UHFFFAOYSA-N 1-cyclohexyl-3-[2-fluoro-4-[6-(1-tritylpyrazol-4-yl)imidazo[1,2-a]pyridin-3-yl]phenyl]urea Chemical compound FC1=CC(C=2N3C=C(C=CC3=NC=2)C2=CN(N=C2)C(C=2C=CC=CC=2)(C=2C=CC=CC=2)C=2C=CC=CC=2)=CC=C1NC(=O)NC1CCCCC1 TUEVVYKIUZPSKK-UHFFFAOYSA-N 0.000 claims 1
- LTIBDLOGEYRZBY-UHFFFAOYSA-N 1-cyclohexyl-3-[2-fluoro-4-[6-(1H-pyrazol-4-yl)imidazo[1,2-a]pyridin-3-yl]phenyl]urea Chemical compound FC1=CC(C=2N3C=C(C=CC3=NC=2)C2=CNN=C2)=CC=C1NC(=O)NC1CCCCC1 LTIBDLOGEYRZBY-UHFFFAOYSA-N 0.000 claims 1
- 125000003349 3-pyridyl group Chemical group N1=C([H])C([*])=C([H])C([H])=C1[H] 0.000 claims 1
- ZAKUXPKAPWYKQK-UHFFFAOYSA-N 3H-oxathiadiazole Chemical group N1SOC=N1 ZAKUXPKAPWYKQK-UHFFFAOYSA-N 0.000 claims 1
- 102000027757 FGF receptors Human genes 0.000 claims 1
- 108091008101 FGF receptors Proteins 0.000 claims 1
- YDJQQPMRODCRSH-UHFFFAOYSA-N N-[4-[6-[3-(4-fluorophenyl)-1-tritylpyrazol-4-yl]imidazo[1,2-a]pyridin-3-yl]phenyl]methanesulfonamide Chemical compound C1=CC(NS(=O)(=O)C)=CC=C1C1=CN=C2N1C=C(C=1C(=NN(C=1)C(C=1C=CC=CC=1)(C=1C=CC=CC=1)C=1C=CC=CC=1)C=1C=CC(F)=CC=1)C=C2 YDJQQPMRODCRSH-UHFFFAOYSA-N 0.000 claims 1
- XWEKHLNARXFFBD-UHFFFAOYSA-N N-[4-[6-[5-(4-fluorophenyl)-1H-pyrazol-4-yl]imidazo[1,2-a]pyridin-3-yl]phenyl]methanesulfonamide Chemical compound C1=CC(NS(=O)(=O)C)=CC=C1C1=CN=C2N1C=C(C=1C(=NNC=1)C=1C=CC(F)=CC=1)C=C2 XWEKHLNARXFFBD-UHFFFAOYSA-N 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 125000002837 carbocyclic group Chemical group 0.000 claims 1
- 125000004452 carbocyclyl group Chemical group 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 230000001404 mediated Effects 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- WCPAKWJPBJAGKN-UHFFFAOYSA-N oxadiazole Chemical group C1=CON=N1 WCPAKWJPBJAGKN-UHFFFAOYSA-N 0.000 claims 1
- ZCQWOFVYLHDMMC-UHFFFAOYSA-N oxazole Chemical group C1=COC=N1 ZCQWOFVYLHDMMC-UHFFFAOYSA-N 0.000 claims 1
- 125000001037 p-tolyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1*)C([H])([H])[H] 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- LDIJKUBTLZTFRG-UHFFFAOYSA-N pyrazolo[1,5-a]pyrimidine Chemical compound N1=CC=CN2N=CC=C21 LDIJKUBTLZTFRG-UHFFFAOYSA-N 0.000 claims 1
- 125000004076 pyridyl group Chemical group 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 239000011780 sodium chloride Substances 0.000 claims 1
- 239000012453 solvate Substances 0.000 claims 1
- 150000003536 tetrazoles Chemical group 0.000 claims 1
- 150000003852 triazoles Chemical group 0.000 claims 1
Claims (15)
- 式（Ｉ）の化合物：
Ｘ１、Ｘ２、およびＸ３は、各々独立して、炭素または窒素から選択され、但しＸ１〜Ｘ３の少なくとも一つは窒素を表し、
Ｘ４は、ＣＲ３または窒素を表し、
Ｘ５は、ＣＲ６、窒素、またはＣ＝Ｏを表し、
但し、Ｘ１〜Ｘ５の３以下は、窒素を表し、
------ は、単または二重結合を表し、但し、５員環系内における少なくとも一つの結合は二重結合であり、
Ｒ３は、水素、ハロゲン、Ｃ１‐６アルキル、Ｃ２‐６アルケニル、Ｃ２‐６アルキニル、Ｃ１‐６アルコキシ、Ｃ３‐６シクロアルキル、Ｃ３‐６シクロアルケニル、シアノ、ハロＣ１‐６アルキル、ハロＣ１‐６アルコキシ、または＝Ｏを表し、
Ａは、１以上（例えば、１、２、または３）のＲａ基によって場合により置換される場合もある、芳香族、非芳香族炭素環式、またはヘテロ環式基を表し、
Ｒ１は、‐ＮＨＣＯＮＲ４Ｒ５、‐ＮＨＣＯＯＲ４、‐ＮＨ‐ＣＯ‐（ＣＨ２）ｎ‐ＮＲ４Ｒ５、‐ＮＨ‐（ＣＨ２）ｎ‐ＣＯＮＲ４Ｒ５、‐ＮＨ‐ＣＯ‐（ＣＨ２）ｎ‐ＣＯＯＲ４、‐ＮＨ‐ＣＯ‐（ＣＨ２）ｎ‐ＣＳＯＲ４、‐ＮＨＳＯ２Ｒ４、‐ＮＨＳＯ２ＮＲ４Ｒ５、‐ＮＨＣＳＮＲ４Ｒ５、‐ＮＨＣＯＲ４、‐ＮＨＣＳＲ４、‐ＮＨＣＳＳＲ４、‐ＮＨＣ（＝ＮＲ４）ＮＲ５、‐ＮＨＣ（＝ＮＲ４）Ｒ５、‐ＮＨ‐Ｃ（＝ＮＨ２）‐ＮＨ‐ＣＯ‐Ｒ４、‐ＮＨＣＳＯＲ４、または‐ＮＨＣＯＳＲ４を表し、
Ｒ４およびＲ５は、独立して、水素、Ｃ１‐６アルキル、Ｃ２‐６アルケニル、Ｃ２‐６アルキニル、Ｃ３‐８シクロアルキル、Ｃ３‐８シクロアルケニル、Ｃ１‐６アルカノール、ハロＣ１‐６アルキル、‐（ＣＨ２）ｎ‐ＮＲｘＲｙ、‐（ＣＨ２）ｓ‐ＣＯＯＲｚ、‐（ＣＨ２）ｎ‐Ｏ‐（ＣＨ２）ｍ‐ＯＨ、‐（ＣＨ２）ｎ‐アリール、‐（ＣＨ２）ｎ‐Ｏ‐アリール、‐（ＣＨ２）ｎ‐ヘテロシクリル、または‐（ＣＨ２）ｎ‐Ｏ‐ヘテロシクリルを表し、ここで該Ｃ１‐６アルキル、Ｃ２‐６アルケニル、Ｃ２‐６アルキニル、Ｃ３‐８シクロアルキル、Ｃ３‐８シクロアルケニル、アリール、およびヘテロシクリル基は１以上（例えば、１、２、または３）のＲａ基によって場合により置換される場合もあり、
Ｒｘ、Ｒｙ、およびＲｚは、独立して、水素、Ｃ１‐６アルキル、Ｃ２‐６アルケニル、Ｃ２‐６アルキニル、Ｃ１‐６アルカノール、‐ＣＯＯＣ１‐６アルキル、ヒドロキシ、Ｃ１‐６アルコキシ、ハロＣ１‐６アルキル、‐ＣＯ‐（ＣＨ２）ｎ‐Ｃ１‐６アルコキシ、Ｃ１‐６アルキルアミノ、Ｃ３‐８シクロアルキル、またはＣ３‐８シクロアルケニルを表し、
Ｒ２およびＲ６は、独立して、ハロゲン、水素、Ｃ１‐６アルキル、Ｃ１‐６アルコキシ、Ｃ２‐６アルケニル、Ｃ２‐６アルキニル、‐Ｃ≡Ｎ、Ｃ３‐８シクロアルキル、Ｃ３‐８シクロアルケニル、‐ＮＨＳＯ２Ｒｗ、‐ＣＨ＝Ｎ‐ＯＲｗ、アリール、またはヘテロシクリル基を表し、ここで該Ｃ１‐６アルキル、Ｃ２‐６アルケニル、Ｃ２‐６アルキニル、アリール、およびヘテロシクリル基は１以上のＲｂ基によって場合により置換される場合もあるが、但しＲ２およびＲ６が双方とも水素を表す場合はない、
Ｒｗは、水素またはＣ１‐６アルキルを表し、
Ｒａは、ハロゲン、Ｃ１‐６アルキル、Ｃ２‐６アルケニル、Ｃ２‐６アルキニル、Ｃ３‐８シクロアルキル、Ｃ３‐８シクロアルケニル、‐ＯＲｘ、‐（ＣＨ２）ｎ‐Ｏ‐Ｃ１‐６アルキル、‐Ｏ‐（ＣＨ２）ｎ‐ＯＲｘ、ハロＣ１‐６アルキル、ハロＣ１‐６アルコキシ、Ｃ１‐６アルカノール、＝Ｏ、＝Ｓ、ニトロ、Ｓｉ（Ｒｘ）４、‐（ＣＨ２）ｓ‐ＣＮ、‐Ｓ‐Ｒｘ、‐ＳＯ‐Ｒｘ、‐ＳＯ２‐Ｒｘ、‐ＣＯＲｘ、‐（ＣＲｘＲｙ）ｓ‐ＣＯＯＲｚ、‐（ＣＨ２）ｓ‐ＣＯＮＲｘＲｙ、‐（ＣＨ２）ｓ‐ＮＲｘＲｙ、‐（ＣＨ２）ｓ‐ＮＲｘＣＯＲｙ、‐（ＣＨ２）ｓ‐ＮＲｘＳＯ２‐Ｒｙ、‐（ＣＨ２）ｓ‐ＮＨ‐ＳＯ２‐ＮＲｘＲｙ、‐ＯＣＯＮＲｘＲｙ、‐（ＣＨ２）ｓ‐ＮＲｘＣＯ２Ｒｙ、‐Ｏ‐（ＣＨ２）ｓ‐ＣＲｘＲｙ‐（ＣＨ２）ｔ‐ＯＲｚ、または‐（ＣＨ２）ｓ‐ＳＯ２ＮＲｘＲｙ基を表し、
Ｒｂは、Ｒａ基または‐Ｙ‐カルボシクリルもしくは‐Ｚ‐ヘテロシクリル基を表し、ここで該カルボシクリルおよびヘテロシクリル基は１以上（例えば、１、２、または３）のＲａ基によって場合により置換される場合もあり、
ＹおよびＺは、独立して、結合、‐ＣＯ‐（ＣＨ２）ｓ‐、‐ＣＯＯ‐、‐（ＣＨ２）ｎ‐、‐ＮＲｘ‐（ＣＨ２）ｎ‐、‐（ＣＨ２）ｎ‐ＮＲｘ‐、‐ＣＯＮＲｘ‐、‐ＮＲｘＣＯ‐、‐ＳＯ２ＮＲｘ‐、‐ＮＲｘＳＯ２‐、‐ＮＲｘＣＯＮＲｙ‐、‐ＮＲｘＣＳＮＲｙ‐、‐Ｏ‐（ＣＨ２）ｓ‐、‐（ＣＨ２）ｓ‐Ｏ‐、‐Ｓ‐、‐ＳＯ‐、または‐（ＣＨ２）ｓ‐ＳＯ２‐を表し、
ｍおよびｎは、独立して、１〜４の整数を表し、
ｓおよびｔは、独立して、０〜４の整数を表す〕
あるいはその薬学上許容される塩、溶媒和物または誘導体、
但し、式（Ｉ）の化合物は：
３‐（３‐アセトアミドフェニル）‐６‐（４‐メチルフェニル）ピラゾロ（１，５ａ）ピリミジン、
３‐（３‐アセトアミドフェニル）‐６‐（４‐メトキシフェニル）ピラゾロ（１，５ａ）ピリミジン、
Ｎ‐〔４‐〔６‐〔３‐（４‐フルオロフェニル）‐１Ｈ‐４‐ピラゾリル〕イミダゾ〔１，２‐ａ〕ピリジン‐３‐イル〕フェニル〕メタンスルホンアミド、
Ｎ‐〔４‐〔６‐〔３‐（４‐フルオロフェニル）‐１‐トリチル‐１Ｈ‐４‐ピラゾリル〕イミダゾ〔１，２‐ａ〕ピリジン‐３‐イル〕フェニル〕メタンスルホンアミド、
Ｎ‐シクロヘキシル‐Ｎ′‐〔２‐フルオロ‐４‐〔６‐（１‐トリチル‐１Ｈ‐４‐ピラゾリル）イミダゾ〔１，２‐ａ〕ピリジン‐３‐イル〕フェニル〕尿素、
Ｎ‐〔２‐フルオロ‐４‐〔６‐（１‐トリチル‐１Ｈ‐４‐ピラゾリル）イミダゾ〔１，２‐ａ〕ピリジン‐３‐イル〕フェニル〕‐Ｎ′‐イソプロピル尿素、
Ｎ‐シクロヘキシル‐Ｎ′‐〔２‐フルオロ‐４‐〔６‐（１Ｈ‐４‐ピラゾリル）イミダゾ〔１，２‐ａ〕ピリジン‐３‐イル〕フェニル〕尿素、
Ｎ‐〔２‐フルオロ‐４‐〔６‐（１Ｈ‐４‐ピラゾリル）イミダゾ〔１，２‐ａ〕ピリジン‐３‐イル〕フェニル〕‐Ｎ′‐イソプロピル尿素、または
Ｎ１‐〔２‐フルオロ‐４‐〔６‐（１Ｈ‐４‐ピラゾリル）イミダゾ〔１，２‐ａ〕ピリジン‐３‐イル〕フェニル〕‐４‐フルオロベンズアミドではない。 - Ｘ１、Ｘ２、およびＸ３は、各々独立して、炭素または窒素から選択され、但しＸ１〜Ｘ３の少なくとも一つは窒素を表し、
Ｘ４は、ＣＲ３または窒素を表し、
Ｘ５は、ＣＨ、窒素、またはＣ＝Ｏを表し、
但しＸ１〜Ｘ５の３以下は窒素を表し、
------ は、単または二重結合を表し、
Ｒ３は、水素または＝Ｏを表し、
Ａは、１以上（例えば、１、２、または３）のＲａ基によって場合により置換される場合もある、芳香族、非芳香族炭素環式、またはヘテロ環式基を表し、
Ｒ１は、‐ＮＨＣＯＮＲ４Ｒ５、‐ＮＨＣＯＯＲ４、‐ＮＨ‐ＣＯ‐（ＣＨ２）ｎ‐ＮＲ４Ｒ５、‐ＮＨ‐ＣＯ‐（ＣＨ２）ｎ‐ＣＯＯＲ４、‐ＮＨＳＯ２Ｒ４、または‐ＮＨＣＳＮＲ４Ｒ５を表し、
Ｒ４およびＲ５は、独立して、水素、Ｃ１‐６アルキル、Ｃ１‐６アルカノール、‐（ＣＨ２）ｎ‐ＮＲｘＲｙ、‐（ＣＨ２）ｎ‐アリール、またはハロＣ１‐６アルキルを表し、
Ｒｘ、Ｒｙ、およびＲｚは、独立して、水素、Ｃ１‐６アルキル、Ｃ１‐６アルカノール、ヒドロキシ、Ｃ１‐６アルコキシ、ハロＣ１‐６アルキル、または‐ＣＯ‐（ＣＨ２）ｎ‐Ｃ１‐６アルコキシを表し、
Ｒ２は、一以上のＲｂ基によって場合により置換されたアリールまたはヘテロシクリル基を表し、
Ｒａは、ハロゲン、Ｃ１‐６アルキル、Ｃ２‐６アルケニル、Ｃ２‐６アルキニル、Ｃ３‐８シクロアルキル、Ｃ３‐８シクロアルケニル、‐ＯＲｘ、‐Ｏ‐（ＣＨ２）ｎ‐ＯＲｘ、ハロＣ１‐６アルキル、ハロＣ１‐６アルコキシ、Ｃ１‐６アルカノール、＝Ｏ、＝Ｓ、ニトロ、‐（ＣＨ２）ｓ‐ＣＮ、‐Ｓ‐Ｒｘ、‐ＳＯ‐Ｒｘ、‐ＳＯ２‐Ｒｘ、‐ＣＯＲｘ、‐（ＣＲｘＲｙ）ｓ‐ＣＯＯＲｚ、‐（ＣＨ２）ｓ‐ＣＯＮＲｘＲｙ、‐（ＣＨ２）ｓ‐ＮＲｘＲｙ、‐（ＣＨ２）ｓ‐ＮＲｘＣＯＲｙ、‐（ＣＨ２）ｓ‐ＮＲｘＳＯ２‐Ｒｙ、‐ＯＣＯＮＲｘＲｙ、‐（ＣＨ２）ｓ‐ＮＲｘＣＯ２Ｒｙ、‐Ｏ‐（ＣＨ２）ｓ‐ＣＲｘＲｙ‐（ＣＨ２）ｔ‐ＯＲｚ、または‐（ＣＨ２）ｓ‐ＳＯ２ＮＲｘＲｙ基を表し、
Ｒｂは、‐Ｙ‐アリールまたは‐Ｚ‐ヘテロシクリル基を表し、ここで該アリールおよびヘテロシクリル基は一以上（例えば、１、２、または３）のＲａ基によって場合により置換される場合もあり、
但し、Ｒ２が水素以外の基を表す場合、Ｘ５はＣＨまたはＣ＝Ｏを表し、
ＹおよびＺは、独立して、結合、ＣＯ、‐（ＣＨ２）ｎ‐、‐ＮＲｘ‐（ＣＨ２）ｎ‐、‐Ｏ‐、または‐Ｏ‐（ＣＨ２）ｓ‐を表し、
ｍおよびｎは、独立して、１〜４の整数を表し、
ｓおよびｔは、独立して、０〜４の整数を表し、
アリールは、炭素環式環を表し、および
ヘテロシクリルは、ヘテロ環式環を表す、
請求項１に記載の化合物。 - Ａが、１以上のＲａ基によって場合により置換されたフェニルまたはピリジル基を表す、請求項１または２に記載の化合物。
- Ｒ１が‐ＮＨＣＯＮＲ４Ｒ５を表す、先行する請求項のいずれか一項に記載の化合物。
- Ｒ２が、１以上のＲａ基によって場合により置換されたアリールまたはヘテロシクリル基を表す、先行する請求項のいずれか一項に記載の化合物。
- Ｒ２が、ハロゲン、‐Ｚ‐ヘテロシクリル基、または‐（ＣＲｘＲｙ）ｓ‐ＣＯＯＲｚによって場合により置換されたアリール基を表し、該ヘテロシクリル基がＣ１‐６アルキルまたは‐（ＣＲｘＲｙ）ｓ‐ＣＯＯＲｚ基によって場合により置換される場合もあり、またはＲ ２ が、＝Ｏ、＝Ｓ、ハロゲン、Ｃ １‐６ アルキル、ハロＣ １‐６ アルキル、Ｃ ３‐８ シクロアルキル、‐（ＣＨ ２ ） ｓ ‐ＮＲ ｘ Ｒ ｙ 、‐ＯＲ ｘ 、‐（ＣＨ ２ ） ｎ ‐Ｏ‐Ｃ １‐６ アルキル、‐ＣＯＲ ｘ 、‐（ＣＲ ｘ Ｒ ｙ ） ｓ ‐ＣＯＯＲ ｚ 、‐Ｓ‐Ｒ ｘ 、‐ＳＯ ２ ‐Ｒ ｘ 、‐（ＣＨ ２ ） ｓ ‐ＮＲ ｘ Ｒ ｙ 、‐（ＣＨ ２ ） ｓ ‐ＳＯ ２ ＮＲ ｘ Ｒ ｙ 、またはＣ １‐６ アルカノール基によって場合により置換されたヘテロシクリル基を表す、先行する請求項のいずれか一項に記載の化合物。
- Ｒ２が、１以上のメチル、エチル、または‐Ｓ‐メチル基によって場合により置換されたオキサゾール、オキサジアゾール、トリアゾール、テトラゾール、チアジアゾール、またはオキサチアジアゾールを表す、先行する請求項のいずれか一項に記載の化合物。
- ＹおよびＺが、独立して、結合、ＣＯ、‐ＣＨ２‐、‐（ＣＨ２）２‐、‐（ＣＨ２）３‐、または‐Ｏ‐を表す、先行する請求項のいずれか一項に記載の化合物。
- Ｘ１〜Ｘ５が下記環系で定義される通りである、先行する請求項のいずれか一項に記載の化合物：
- 実施例２〜１７、１９、２４、２６〜６２、６４〜６７、７５、７７〜９７、１００〜１０９、１１１〜１１５、１１７、１１９〜１３１、１３３〜１５６、１５８〜１６６、および１６８〜４２２から選択される化合物である、先行する請求項のいずれか一項に記載の化合物。
- 式（Ｉｄ）の化合物：
- 請求項１〜１１のいずれか一項に記載の式（Ｉ）の化合物を含んでなる医薬組成物。
- 癌の予防または治療用の、請求項１２に記載の医薬組成物。
- ＦＧＦＲキナーゼにより媒介される疾患の治療用の、式（II）の化合物を含む、医薬組成物：
ｕは、０〜２の整数を表し、
Ｒ１ａは、‐ＮＨＣＯＮＲ４Ｒ５、‐ＮＨＣＯＯＲ４、‐ＮＨ‐ＣＯ‐（ＣＨ２）ｎ‐ＮＲ４Ｒ５、‐ＮＨ‐（ＣＨ２）ｎ‐ＣＯＮＲ４Ｒ５、‐ＮＨ‐ＣＯ‐（ＣＨ２）ｎ‐ＣＯＯＲ４、‐ＮＨ‐ＣＯ‐（ＣＨ２）ｎ‐ＣＳＯＲ４、‐ＮＨＳＯ２Ｒ４、‐ＮＨＳＯ２ＳＲ４、‐ＮＨＳＯ２ＮＲ４Ｒ５、‐ＮＨＣＳＮＲ４Ｒ５、‐ＮＨＣＯＲ４、‐ＮＨＣＳＲ４、‐ＮＨＣＳＳＲ４、‐ＮＲ４Ｒ５、‐Ｃ（＝ＮＲ４）ＮＲ５、ハロゲン、Ｃ１‐６アルキル、アリール、‐ＣＯ‐アリール、ヘテロシクリル、‐ＣＯ‐ヘテロシクリル、‐ＣＯＮＲ４Ｒ５、‐（ＣＨ２）ｎ‐ＮＲ４ＣＯＲ５、‐（ＣＨ２）ｓ‐ＣＮ、‐ＯＲ４、または‐ＣＯＯＲ４を表し、ここで該アリールおよびヘテロシクリル基は、式（Ｉ）の化合物に関して定義されているような一以上（例えば、１、２、または３）のＲａ基によって場合により置換される場合もあり、
Ｒ４およびＲ５は、式（Ｉ）の化合物に関して定義されている通りであるが、但しＲ４およびＲ５の一方が水素を表す場合、他は‐アリールまたは‐ヘテロシクリル以外の基を表し、
Ｒ２は、式（Ｉ）の化合物に関して定義されている通りである〕。 - 式（II）の化合物が、実施例１、１８、２０〜２３、２５、６３、６８〜６９、７０〜７４、７６、９８〜９９、１１０、１１６、１１８、１３２、１５７、１６７、および２３５から選択される化合物である、請求項１４に記載の医薬組成物。
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| AU2007230911A1 (en) * | 2006-03-23 | 2007-10-04 | Synta Pharmaceuticals Corp. | Benzimidazolyl-pyridine compounds for inflammation and immune-related uses |
| ITVA20060041A1 (it) | 2006-07-05 | 2008-01-06 | Dialectica Srl | Uso di composti derivati amminotiazolici, di loro composizioni farmaceutiche, nel trattamento di malattie caratterizzate dalla anormale repressione della trascrizione genica, particolarmente il morbo di huntington |
| TW200811134A (en) | 2006-07-12 | 2008-03-01 | Irm Llc | Compounds and compositions as protein kinase inhibitors |
| EP1882475A1 (en) | 2006-07-26 | 2008-01-30 | Novartis AG | Method of treating disorders mediated by the fibroblast growth factor receptor |
| US7737149B2 (en) | 2006-12-21 | 2010-06-15 | Astrazeneca Ab | N-[5-[2-(3,5-dimethoxyphenyl)ethyl]-2H-pyrazol-3-yl]-4-(3,5-dimethylpiperazin-1-yl)benzamide and salts thereof |
| US8131527B1 (en) | 2006-12-22 | 2012-03-06 | Astex Therapeutics Ltd. | FGFR pharmacophore compounds |
| US8895745B2 (en) | 2006-12-22 | 2014-11-25 | Astex Therapeutics Limited | Bicyclic heterocyclic compounds as FGFR inhibitors |
| CN101679409B (zh) | 2006-12-22 | 2014-11-26 | Astex治疗学有限公司 | 双环杂环衍生化合物、其医药组合物和其用途 |
| US7977336B2 (en) | 2006-12-28 | 2011-07-12 | Banyu Pharmaceutical Co. Ltd | Aminopyrimidine derivatives as PLK1 inhibitors |
| BRPI0809998B8 (pt) | 2007-04-03 | 2021-05-25 | Array Biopharma Inc | composto de imidazo[1,2-a] piridina como inibidores do receptor tirosina quinase, seus usos, seus processos de preparação e composições farmacêuticas |
| CN107021895A (zh) | 2007-06-12 | 2017-08-08 | 尔察祯有限公司 | 抗菌剂 |
| US20090005374A1 (en) | 2007-06-26 | 2009-01-01 | Melvin Jr Lawrence S | Imidazopyridinyl thiazolyl histone deacetylase inhibitors |
| GB0720038D0 (en) | 2007-10-12 | 2007-11-21 | Astex Therapeutics Ltd | New compounds |
| GB0720041D0 (en) * | 2007-10-12 | 2007-11-21 | Astex Therapeutics Ltd | New Compounds |
| GB0810902D0 (en) | 2008-06-13 | 2008-07-23 | Astex Therapeutics Ltd | New compounds |
| GB0906470D0 (en) | 2009-04-15 | 2009-05-20 | Astex Therapeutics Ltd | New compounds |
| GB0906472D0 (en) | 2009-04-15 | 2009-05-20 | Astex Therapeutics Ltd | New compounds |
-
2007
- 2007-12-21 US US12/520,481 patent/US8895745B2/en active Active
- 2007-12-21 CN CN200780047672.6A patent/CN101679408B/zh active Active
- 2007-12-21 AU AU2007337886A patent/AU2007337886C1/en not_active Ceased
- 2007-12-21 AR ARP070105856A patent/AR064491A1/es active IP Right Grant
- 2007-12-21 JP JP2009542223A patent/JP5442448B2/ja not_active Expired - Fee Related
- 2007-12-21 CA CA2672172A patent/CA2672172C/en active Active
- 2007-12-21 MX MX2009006706A patent/MX2009006706A/es active IP Right Grant
- 2007-12-21 EP EP07848659.4A patent/EP2114941B1/en active Active
- 2007-12-21 WO PCT/GB2007/004934 patent/WO2008078091A1/en active Application Filing
-
2009
- 2009-07-13 NO NO20092657A patent/NO343370B1/no unknown
-
2015
- 2015-06-15 HR HRP20150642TT patent/HRP20150642T1/hr unknown
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