JP2013545749A5 - - Google Patents
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- JP2013545749A5 JP2013545749A5 JP2013538894A JP2013538894A JP2013545749A5 JP 2013545749 A5 JP2013545749 A5 JP 2013545749A5 JP 2013538894 A JP2013538894 A JP 2013538894A JP 2013538894 A JP2013538894 A JP 2013538894A JP 2013545749 A5 JP2013545749 A5 JP 2013545749A5
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- 0 C*C1=CCNc2ccn[n]12 Chemical compound C*C1=CCNc2ccn[n]12 0.000 description 8
- GIMWHCHOTWSKAK-KRWDZBQOSA-N CC(C)N(CC1)CCC1Oc1nc([C@H](C)Nc2ccnc3ccn[n]23)cc2cccc(Cl)c12 Chemical compound CC(C)N(CC1)CCC1Oc1nc([C@H](C)Nc2ccnc3ccn[n]23)cc2cccc(Cl)c12 GIMWHCHOTWSKAK-KRWDZBQOSA-N 0.000 description 1
- JLSAEIAARXOSFT-UHFFFAOYSA-N CCc1cc2cccc(C)c2c(OC(CC2)CCN2C(C)C)n1 Chemical compound CCc1cc2cccc(C)c2c(OC(CC2)CCN2C(C)C)n1 JLSAEIAARXOSFT-UHFFFAOYSA-N 0.000 description 1
- NSZKMHUXDXFLAZ-UHFFFAOYSA-N CCc1cc2cccc(Cl)c2c(C(N2CCOCC2)=O)n1 Chemical compound CCc1cc2cccc(Cl)c2c(C(N2CCOCC2)=O)n1 NSZKMHUXDXFLAZ-UHFFFAOYSA-N 0.000 description 1
- DDKXTXUMGTXWCX-INIZCTEOSA-N C[C@@H](c1cc(cccc2Cl)c2c(OCCN2CCCC2)n1)Nc1ccnc2ccn[n]12 Chemical compound C[C@@H](c1cc(cccc2Cl)c2c(OCCN2CCCC2)n1)Nc1ccnc2ccn[n]12 DDKXTXUMGTXWCX-INIZCTEOSA-N 0.000 description 1
- GYPPLWOLWPZVKS-AWEZNQCLSA-N C[C@@H](c1cc2cccc(C)c2c(C(N(C)C)=O)n1)Nc1c2ncccc2ncn1 Chemical compound C[C@@H](c1cc2cccc(C)c2c(C(N(C)C)=O)n1)Nc1c2ncccc2ncn1 GYPPLWOLWPZVKS-AWEZNQCLSA-N 0.000 description 1
- WNHZZCIYDFPHME-AWEZNQCLSA-N C[C@@H](c1cc2cccc(C)c2c(C(N2CCOCC2)=O)n1)Nc1c2nc[nH]c2ncn1 Chemical compound C[C@@H](c1cc2cccc(C)c2c(C(N2CCOCC2)=O)n1)Nc1c2nc[nH]c2ncn1 WNHZZCIYDFPHME-AWEZNQCLSA-N 0.000 description 1
- GCSIYFMLLDMJTR-HNNXBMFYSA-N C[C@@H](c1cc2cccc(C)c2c(C(N2CCOCC2)=O)n1)Nc1c2ncccc2nc(N)n1 Chemical compound C[C@@H](c1cc2cccc(C)c2c(C(N2CCOCC2)=O)n1)Nc1c2ncccc2nc(N)n1 GCSIYFMLLDMJTR-HNNXBMFYSA-N 0.000 description 1
- JWRVCHLJBGMISM-HNNXBMFYSA-N C[C@@H](c1cc2cccc(C)c2c(N2CCN(C)CC2)n1)Nc1c2nc[nH]c2ncn1 Chemical compound C[C@@H](c1cc2cccc(C)c2c(N2CCN(C)CC2)n1)Nc1c2nc[nH]c2ncn1 JWRVCHLJBGMISM-HNNXBMFYSA-N 0.000 description 1
- MKLJIPWMFFCVGD-NSHDSACASA-N C[C@@H](c1cc2cccc(C)c2c(OCC(O)=O)n1)Nc1c2nc[nH]c2ncn1 Chemical compound C[C@@H](c1cc2cccc(C)c2c(OCC(O)=O)n1)Nc1c2nc[nH]c2ncn1 MKLJIPWMFFCVGD-NSHDSACASA-N 0.000 description 1
- VMSBTJNDRGOKRP-AWEZNQCLSA-N C[C@@H](c1cc2cccc(Cl)c2c(C(N2CCOCC2)=O)n1)NC(c1cnc2[n]1nccc2)=O Chemical compound C[C@@H](c1cc2cccc(Cl)c2c(C(N2CCOCC2)=O)n1)NC(c1cnc2[n]1nccc2)=O VMSBTJNDRGOKRP-AWEZNQCLSA-N 0.000 description 1
- UWAVFYKYVYMZGT-HNNXBMFYSA-N C[C@@H](c1cc2cccc(Cl)c2c(C(N2CCOCC2)=O)n1)Nc1c(cccc2)c2ncn1 Chemical compound C[C@@H](c1cc2cccc(Cl)c2c(C(N2CCOCC2)=O)n1)Nc1c(cccc2)c2ncn1 UWAVFYKYVYMZGT-HNNXBMFYSA-N 0.000 description 1
- QYUUUMUSOUPFAR-LBPRGKRZSA-N C[C@@H](c1cc2cccc(Cl)c2c(C(N2CCOCC2)=O)n1)Nc1c2nc[s]c2ncn1 Chemical compound C[C@@H](c1cc2cccc(Cl)c2c(C(N2CCOCC2)=O)n1)Nc1c2nc[s]c2ncn1 QYUUUMUSOUPFAR-LBPRGKRZSA-N 0.000 description 1
- NDUZQPPGIGIXQS-ZDUSSCGKSA-N C[C@@H](c1cc2cccc(Cl)c2c(N2CCN(C)CC2)n1)Nc1c2nc[s]c2ncn1 Chemical compound C[C@@H](c1cc2cccc(Cl)c2c(N2CCN(C)CC2)n1)Nc1c2nc[s]c2ncn1 NDUZQPPGIGIXQS-ZDUSSCGKSA-N 0.000 description 1
- AOBIZYSWXCLUGQ-INIZCTEOSA-N C[C@@H](c1cc2cccc(Cl)c2c(OCCN2CCCC2)n1)Nc1c2ncccc2ncn1 Chemical compound C[C@@H](c1cc2cccc(Cl)c2c(OCCN2CCCC2)n1)Nc1c2ncccc2ncn1 AOBIZYSWXCLUGQ-INIZCTEOSA-N 0.000 description 1
- UYNSQOJBUWTJMF-UHFFFAOYSA-N Cc1c2nc[s]c2ncn1 Chemical compound Cc1c2nc[s]c2ncn1 UYNSQOJBUWTJMF-UHFFFAOYSA-N 0.000 description 1
- DGXAOSOMFMODCF-UHFFFAOYSA-N Nc1c2ncccc2ncn1 Chemical compound Nc1c2ncccc2ncn1 DGXAOSOMFMODCF-UHFFFAOYSA-N 0.000 description 1
Description
一態様では、本明細書で記載されるのは、式(I)の化合物、又はその医薬として許容し得るその形態である:
(式中、
W5は、N、CHR4、又はCR4であり;
R4は、水素、アルキル、ハロアルキル、ヘテロアルキル、アルケニル、アルキニル、シクロアルキル、ヘテロシクロアルキル、アリール、アリールアルキル、ヘテロアリール、ヘテロアリールアルキル、アルコキシ、ヘテロシクロアルキルオキシ、アミド、アミノ、アシル、アシルオキシ、アルコキシカルボニル、スルホンアミド、チオ、スルホキシド、スルホン、ハロ、シアノ、ヒドロキシ、ニトロ、ホスフェート、尿素、カルボネート、又はNR'R''であり、ここで、R'及びR''は、窒素と一緒になって、環部分を形成し、
Cyは、R3の0〜4回の出現によって置換されたアリール又はヘテロアリールであり;
R1は-(L)n-R1'であり;
各Lは、独立に、結合、アルキレン、ヘテロアルキレン、-N(R2)-、-S(O)-、-S(O)2-、-S-、-C(=O)-、-P(=O)R2-、又は-O-であり;
R1'は、水素、アルキル、ヘテロアルキル、アルケニル、アルキニル、シクロアルキル、ヘテロシクロアルキル、アリール、アリールアルキル、ヘテロアリール、ヘテロアリールアルキル、アルコキシ、ヘテロシクリルオキシ、アミノ、アミド、アシル、アシルオキシ、アルコキシカルボニル、スルホンアミド、ハロ、シアノ、ヒドロキシ、ニトロ、ホスフェート、尿素、カルボネート、-(C=O)-NRa1Ra2、又はNRa1Ra2であり;
Ra1及びRa2は、各々独立に、水素、アルキル、ヘテロアルキル、アルケニル、アルキニル、シクロアルキル、ヘテロシクロアルキル、アリール、アリールアルキル、ヘテロアリール、ヘテロアリールアルキル、アルコキシ、ヘテロシクロアルキルオキシ、アミド、アミノ、アシル、アシルオキシ、アルコキシカルボニル、スルホンアミド、チオ、スルホキシド、スルホン、ハロ、シアノ、ヒドロキシ、ニトロ、ホスフェート、尿素、カルボネートであるか、又はRa1及びRa2は、窒素と一緒になって、環部分を形成し;
R2は、水素、アルキル、シクロアルキル、ヘテロシクロアルキル、ヘテロアルキル、アリール、又はヘテロアリールであり;
各R3は、独立に、アルキル、ヘテロアルキル、ハロアルキル、アルケニル、アルキニル、シクロアルキル、ヘテロシクロアルキル、アリール、アリールアルキル、ヘテロアリール、ヘテロアリールアルキル、アルコキシ、ヘテロシクロアルキルオキシ、アミド、アミノ、アシル、アシルオキシ、アルコキシカルボニル、スルホンアミド、チオ、スルホキシド、スルホン、ハロ、シアノ、ヒドロキシ、ニトロ、ホスフェート、尿素、カルボネート、又はNR'R''であり、ここで、R'及びR''は、窒素と一緒になって、環部分を形成し;
Xは、存在しないか、又は-(CH(R10))Z-であり;
Yは、非存在、-O-、-S-、-S(=O)-、-S(=O)2-、-N(R9)-、-C(=O)-(CHR10)z-、-C(=O)-、-N(R9)-C(=O)-、-N(R9)-C(=O)NH-、-N(R9)C(R10)2-、-C(=O)-(CHR10)z-、-C(=O)-N(R9)-(CHR10)z-、又は-P(=O)R2-であり;
各zは、1、2、3、又は4の整数であり;
nは、0、1、2、3、又は4の整数であり;
各R9は、独立に、水素、アルキル、シクロアルキル、ヘテロシクロアルキル、ヘテロシクロアルキルアルキル、ヘテロアルキル、アリール、又はヘテロアリールであり;
Wdは、ヘテロシクロアルキル、アリール、シクロアルキル、又はヘテロアリールであり、ここで、Wdは、1以上のRb、R11、R12、及びR13で任意に置換されており;かつ
各Rb、R10、R11、R12、及びR13は、独立に、水素、アルキル、ヘテロアルキル、アルケニル、アルキニル、シクロアルキル、ヘテロシクロアルキル、アリール、アリールアルキル、ヘテロアリール、ヘテロアリールアルキル、アルコキシ、ヘテロシクリルオキシ、アミド、アミノ、アシル、アシルオキシ、アルコキシカルボニル、スルホンアミド、ハロ、ハロアルキル、シアノ、ヒドロキシル、ニトロ、ホスフェート、尿素、カルボネート、又はNR'R''であり、ここで、R'及びR''は、窒素と一緒になって、環部分を形成する)。
W5は、N、CHR4、又はCR4であり;
R4は、水素、アルキル、ハロアルキル、ヘテロアルキル、アルケニル、アルキニル、シクロアルキル、ヘテロシクロアルキル、アリール、アリールアルキル、ヘテロアリール、ヘテロアリールアルキル、アルコキシ、ヘテロシクロアルキルオキシ、アミド、アミノ、アシル、アシルオキシ、アルコキシカルボニル、スルホンアミド、チオ、スルホキシド、スルホン、ハロ、シアノ、ヒドロキシ、ニトロ、ホスフェート、尿素、カルボネート、又はNR'R''であり、ここで、R'及びR''は、窒素と一緒になって、環部分を形成し、
Cyは、R3の0〜4回の出現によって置換されたアリール又はヘテロアリールであり;
R1は-(L)n-R1'であり;
各Lは、独立に、結合、アルキレン、ヘテロアルキレン、-N(R2)-、-S(O)-、-S(O)2-、-S-、-C(=O)-、-P(=O)R2-、又は-O-であり;
R1'は、水素、アルキル、ヘテロアルキル、アルケニル、アルキニル、シクロアルキル、ヘテロシクロアルキル、アリール、アリールアルキル、ヘテロアリール、ヘテロアリールアルキル、アルコキシ、ヘテロシクリルオキシ、アミノ、アミド、アシル、アシルオキシ、アルコキシカルボニル、スルホンアミド、ハロ、シアノ、ヒドロキシ、ニトロ、ホスフェート、尿素、カルボネート、-(C=O)-NRa1Ra2、又はNRa1Ra2であり;
Ra1及びRa2は、各々独立に、水素、アルキル、ヘテロアルキル、アルケニル、アルキニル、シクロアルキル、ヘテロシクロアルキル、アリール、アリールアルキル、ヘテロアリール、ヘテロアリールアルキル、アルコキシ、ヘテロシクロアルキルオキシ、アミド、アミノ、アシル、アシルオキシ、アルコキシカルボニル、スルホンアミド、チオ、スルホキシド、スルホン、ハロ、シアノ、ヒドロキシ、ニトロ、ホスフェート、尿素、カルボネートであるか、又はRa1及びRa2は、窒素と一緒になって、環部分を形成し;
R2は、水素、アルキル、シクロアルキル、ヘテロシクロアルキル、ヘテロアルキル、アリール、又はヘテロアリールであり;
各R3は、独立に、アルキル、ヘテロアルキル、ハロアルキル、アルケニル、アルキニル、シクロアルキル、ヘテロシクロアルキル、アリール、アリールアルキル、ヘテロアリール、ヘテロアリールアルキル、アルコキシ、ヘテロシクロアルキルオキシ、アミド、アミノ、アシル、アシルオキシ、アルコキシカルボニル、スルホンアミド、チオ、スルホキシド、スルホン、ハロ、シアノ、ヒドロキシ、ニトロ、ホスフェート、尿素、カルボネート、又はNR'R''であり、ここで、R'及びR''は、窒素と一緒になって、環部分を形成し;
Xは、存在しないか、又は-(CH(R10))Z-であり;
Yは、非存在、-O-、-S-、-S(=O)-、-S(=O)2-、-N(R9)-、-C(=O)-(CHR10)z-、-C(=O)-、-N(R9)-C(=O)-、-N(R9)-C(=O)NH-、-N(R9)C(R10)2-、-C(=O)-(CHR10)z-、-C(=O)-N(R9)-(CHR10)z-、又は-P(=O)R2-であり;
各zは、1、2、3、又は4の整数であり;
nは、0、1、2、3、又は4の整数であり;
各R9は、独立に、水素、アルキル、シクロアルキル、ヘテロシクロアルキル、ヘテロシクロアルキルアルキル、ヘテロアルキル、アリール、又はヘテロアリールであり;
Wdは、ヘテロシクロアルキル、アリール、シクロアルキル、又はヘテロアリールであり、ここで、Wdは、1以上のRb、R11、R12、及びR13で任意に置換されており;かつ
各Rb、R10、R11、R12、及びR13は、独立に、水素、アルキル、ヘテロアルキル、アルケニル、アルキニル、シクロアルキル、ヘテロシクロアルキル、アリール、アリールアルキル、ヘテロアリール、ヘテロアリールアルキル、アルコキシ、ヘテロシクリルオキシ、アミド、アミノ、アシル、アシルオキシ、アルコキシカルボニル、スルホンアミド、ハロ、ハロアルキル、シアノ、ヒドロキシル、ニトロ、ホスフェート、尿素、カルボネート、又はNR'R''であり、ここで、R'及びR''は、窒素と一緒になって、環部分を形成する)。
Claims (37)
- 式(Ia)の化合物、又はその医薬として許容し得る形態:
W5は、N又はCR4であり;
R4は、水素、アルキル、ハロアルキル、ヘテロアルキル、アルケニル、アルキニル、シクロアルキル、ヘテロシクロアルキル、アリール、アリールアルキル、ヘテロアリール、ヘテロアリールアルキル、アルコキシ、ヘテロシクロアルキルオキシ、アミド、アミノ、アシル、アシルオキシ、アルコキシカルボニル、スルホンアミド、チオ、スルホキシド、スルホン、ハロ、シアノ、ヒドロキシ、ニトロ、ホスフェート、尿素、カルボネート、又はNR'R''であり、ここで、R'及びR''は、窒素と一緒になって、環部分を形成し;
Cyは、R3の0〜4回の出現によって置換されたアリール又はヘテロアリールであり;
R1は-(L)n-R1'であり:
各Lは、独立に、結合、アルキレン、ヘテロアルキレン、-N(R2)-、-S(O)-、-S(O)2-、-S-、-C(=O)-、-P(=O)R2-、又は-O-であり;
R1'は、水素、アルキル、ヘテロアルキル、アルケニル、アルキニル、シクロアルキル、ヘテロシクロアルキル、アリール、アリールアルキル、ヘテロアリール、ヘテロアリールアルキル、アルコキシ、ヘテロシクリルオキシ、ヘテロシクロアルキルオキシ、アミノ、アミド、アシル、アシルオキシ、アルコキシカルボニル、スルホンアミド、ハロ、シアノ、ニトロ、ホスフェート、尿素、カルボネート、-(C=O)-NRa1Ra2、又はNRa1Ra2であり;
Ra1及びRa2は、各々独立に、水素、アルキル、ヘテロアルキル、アルケニル、アルキニル、シクロアルキル、ヘテロシクロアルキル、アリール、アリールアルキル、ヘテロアリール、ヘテロアリールアルキル、アルコキシ、ヘテロシクロアルキルオキシ、アミド、アミノ、アシル、アシルオキシ、アルコキシカルボニル、スルホンアミド、チオ、スルホキシド、スルホン、ハロ、シアノ、ヒドロキシ、ニトロ、ホスフェート、尿素、カルボネートであるか、又はRa1及びRa2は、窒素と一緒になって、環部分を形成し;
R2は、水素、アルキル、シクロアルキル、ヘテロシクロアルキル、ヘテロアルキル、アリール、又はヘテロアリールであり;
各R3は、独立に、アルキル、ヘテロアルキル、ハロアルキル、アルケニル、アルキニル、シクロアルキル、ヘテロシクロアルキル、アリール、アリールアルキル、ヘテロアリール、ヘテロアリールアルキル、アルコキシ、ヘテロシクロアルキルオキシ、アミド、アミノ、アシル、アシルオキシ、アルコキシカルボニル、スルホンアミド、チオ、スルホキシド、スルホン、ハロ、シアノ、ヒドロキシ、ニトロ、ホスフェート、尿素、カルボネート、又はNR'R''であり、ここで、R'及びR''は、窒素と一緒になって、環部分を形成し;
Xは、-(CH(R10))Z-であり;
Yは、非存在、-O-、-S-、-S(=O)-、-S(=O)2-、-N(R9)-、-C(=O)-(CHR10)z-、-C(=O)-、-N(R9)-C(=O)-、-C(=O)-N(R9)-、-N(R9)-C(=O)NH-、-N(R9)C(R10)2-、-C(=O)-N(R9)-(CHR10)z-、又は-P(=O)R2-であり;
各zは、1、2、3、又は4の整数であり;
nは、0、1、2、3、又は4の整数であり;
各R9は、独立に、水素、アルキル、シクロアルキル、ヘテロシクロアルキル、ヘテロシクロアルキルアルキル、ヘテロアルキル、アリール、又はヘテロアリールであり;
Wdは、
各Rbは、独立に、水素、ハロ、ホスフェート、尿素、カルボネート、アルキル、アルケニル、アルキニル、シクロアルキル、ヘテロアルキル、又はヘテロシクロアルキルであり;かつ
各R10、R11、及びR12は、独立に、水素、アルキル、ヘテロアルキル、アルケニル、アルキニル、シクロアルキル、ヘテロシクロアルキル、アリール、アリールアルキル、ヘテロアリール、ヘテロアリールアルキル、アルコキシ、ヘテロシクリルオキシ、アミド、アミノ、アシル、アシルオキシ、アルコキシカルボニル、スルホンアミド、ハロ、ハロアルキル、シアノ、ヒドロキシル、ニトロ、ホスフェート、尿素、カルボネート、又はNR'R''であり、ここで、R'及びR''は、窒素と一緒になって、環部分を形成する)。 - nが、1、2、又は3である、請求項1記載の化合物。
- 各Lが、-O-、-C(O)-、-S(O)-、-S(O)2-、-S-、アルキレン、又は結合である、請求項1記載の化合物。
- R1'が、アルキル、ヒドロキシ、アリール、ヘテロアリール、アラルキル、-(C=O)-NRa1Ra2、又はNRa1Ra2であり;任意に、Ra1が、水素又はアルキルであり;任意に、Ra2が、アルキル、シクロアルキル、アリール、アラルキル、ヘテロアリール、ヘテロアラルキル、ヘテロシクロアルキル、アシル、又はヘテロシクロアルキルアルキルであり;任意に、Ra1及びRa2が、それらが結合している窒素と一緒になって、環部分を形成している、請求項1記載の化合物。
- W5がNであるか、又はW5がCR4であり、かつR4が水素である、請求項1記載の化合物。
- Xが-(CH(R10))Z-であり、かつzが1又は2である、請求項1記載の化合物。
- Yが、非存在、-O-、-NH(R9)-、又は-S(=O)2-である、請求項1記載の化合物。
- Cyが、R3の0〜4回の出現によって置換されたフェニルであり;任意に、Cyが、R3の1回の出現によって置換されたフェニルである、請求項1記載の化合物。
- R3が、ハロ、アルキル、ハロアルキル、アシル、又はヘテロアリールである、請求項1記載の化合物。
- R10が水素である、請求項10記載の化合物。
- R12が、水素、ハロ、ハロアルキル、シアノ、アミノ、又はアミドである、請求項10記載の化合物。
- 前記式(Ia)の化合物が、式(II)の化合物、又はその医薬として許容し得る形態である、請求項1記載の化合物:
W1はN又はCR14であり、W2はN又はCR6であり、W3はN又はCR7であり、かつW4はN又はCR8であり、ここで、3個以上のN原子が隣接することはなく;かつ
R6、R7、R8、及びR14は、独立に、水素、アルキル、ハロアルキル、ヘテロアルキル、アルケニル、アルキニル、シクロアルキル、ヘテロシクロアルキル、アリール、アリールアルキル、ヘテロアリール、ヘテロアリールアルキル、アルコキシ、ヘテロシクロアルキルオキシ、アミド、アミノ、アシル、アシルオキシ、アルコキシカルボニル、スルホンアミド、チオ、スルホキシド、スルホン、ハロ、シアノ、ヒドロキシ、ニトロ、ホスフェート、尿素、カルボネート、又はNR'R''であり、ここで、R'及びR''は、窒素と一緒になって、環部分を形成する)。 - R1'が、水素、アミノ、アルコキシ、アルキル、ヘテロシクロアルキル、アリール、又はNRa1Ra2であり、ここで、Ra1及びRa2は、窒素と一緒になって、環部分を形成し;任意に、R1'が、アミノ、アルコキシ、アルキル、又はNRa1Ra2であり、ここで、Ra1及びRa2は、窒素と一緒になって、環部分を形成する、請求項13記載の化合物。
- 前記式(Ia)の化合物が、式(IIIa)の化合物、又はその医薬として許容し得る形態である、請求項1記載の化合物:
W1はN又はCR14であり、W2はN又はCR6であり、W3はN又はCR7であり、かつW4はN又はCR8であり、ここで、3個以上のN原子が隣接することはなく;かつ
R6、R7、R8、及びR14は、独立に、水素、アルキル、ヘテロアルキル、アルケニル、アルキニル、シクロアルキル、ヘテロシクロアルキル、アリール、アリールアルキル、ヘテロアリール、ヘテロアリールアルキル、アルコキシ、ヘテロシクロアルキルオキシ、アミド、アミノ、アシル、アシルオキシ、アルコキシカルボニル、スルホンアミド、チオ、スルホキシド、スルホン、ハロ、シアノ、ヒドロキシ、ニトロ、ホスフェート、尿素、カルボネート、又はNR'R''であり、ここで、R'及びR''は、窒素と一緒になって、環部分を形成する)。 - Ra1及びRa2が窒素と一緒になって、環部分を形成しており;任意に、前記環部分が、5員又は6員である、請求項15記載の化合物。
- nが1であり、かつLがアルキレンであり:任意に、Lが、メチレン又はエチレンである、請求項15記載の化合物。
- Lが、アリール、ヘテロアリール、又はハロによって置換されたアルキレンである、請求項15記載の化合物。
- 前記式(Ia)の化合物が、式(IV)の化合物、又はその医薬として許容し得る形態である、請求項1記載の化合物:
W1はN又はCR14であり、W2はN又はCR6であり、W3はN又はCR7であり、W4はN又はCR8であり、かつW5はN又はCR4であり、ここで、3個以上のN原子が隣接することはなく;かつ
R6、R7、R8、及びR14は、独立に、水素、アルキル、ヘテロアルキル、アルケニル、アルキニル、シクロアルキル、ヘテロシクロアルキル、アリール、アリールアルキル、ヘテロアリール、ヘテロアリールアルキル、アルコキシ、ヘテロシクロアルキルオキシ、アミド、アミノ、アシル、アシルオキシ、アルコキシカルボニル、スルホンアミド、チオ、スルホキシド、スルホン、ハロ、シアノ、ヒドロキシ、ニトロ、ホスフェート、尿素、カルボネート、又はNR'R''であり、ここで、R'及びR''は、窒素と一緒になって、環部分を形成する)。 - 請求項13、15及び19のいずれか一項記載の化合物であって:
W1がNであり、W2がCR6であり、W3がCR7であり、W4がCR8であるか;
W1がCR14であり、W2がNであり、W3がCR7であり、W4がCR8であるか;
W1がCR14であり、W2がCR6であり、W3がNであり、W4がCR8であるか;
W1がNであり、W2がCR6であり、W3がNであり、W4がCR8であるか;
W1がNであり、W2がNであり、W3がCR7であり、W4がCR8であるか;
W1がNであり、W2がCR6であり、W3がCR7であり、W4がNであるか;
W1がCR14であり、W2がNであり、W3がNであり、W4がCR8であるか;
W1がCR14であり、W2がNであり、W3がCR7であり、W4がNであるか;
W1がCR14であり、W2がCR6であり、W3がNであり、W4がNであるか;又は
W1がCR14であり、W2がCR6であり、W3がCR7であり、W4がCR8である、前記化合物。 - W1がCR14であり、W2がCR6であり、W3がCR7であり、かつW4がCR8である、請求項20記載の化合物。
- R8が、水素、アルキル、ヘテロアルキル、アルケニル、アルキニル、シクロアルキル、ヘテロシクロアルキル、アルコキシ、スルホンアミド、チオ、スルホキシド、スルホン、ハロ、シアノ、ヒドロキシ、又はNR'R''であり、ここで、R'及びR''は、窒素と一緒になって、環部分を形成し;任意に、R8が、水素又はアルキルであり;任意に、R8が、1以上のフルオロで置換されたアルキルである、請求項13、15及び19のいずれか一項記載の化合物。
- Xが、-CH2-、-CH(CH3)-、-CH(C6H5)-、又は-CH(CH2CH3)-であり;任意に、-CH(CH3)-又は-CH(CH2CH3)-のCH炭素が、主に、(S)立体化学配置を有する、請求項1、13、15及び19のいずれか一項記載の化合物。
- Yが、非存在、-O-、-N(R9)-、-N(R9)C(R10)2-、又は-S(=O)2-であり;任意に、R9及びR10が、独立に、水素、メチル、又はエチルである、請求項1、13、15及び19のいずれか一項記載の化合物。
- Xが-(CH(R10))Z-であり、zが1であり、Yが-N(R9)-であり、かつR9が水素である、請求項1、13、15及び19のいずれか一項記載の化合物。
- Yが、-N(CH2CH3)CH2-又は-N(CH3)CH2-である、請求項1、13、15及び19のいずれか一項記載の化合物。
- X-Yが、-CH2-N(CH3)-、又は-CH2-N(CH2CH3)-である、請求項1、13、15及び19のいずれか一項記載の化合物。
- Lが、-O-又はアルキレンであり;かつnが、0、1、又は2である、請求項29記載の化合物。
- 請求項1〜33のいずれか一項記載の化合物を含む医薬組成物。
- 対象のPI3K媒介性障害の治療用医薬の製造における、請求項1〜33のいずれか一項記載の化合物、又は、請求項34記載の医薬組成物の使用。
- 前記医薬が、第2の治療剤と共投与される、請求項35記載の使用。
- 前記障害が、癌、炎症性疾患、又は自己免疫疾患である、請求項35記載の使用。
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KR101758046B1 (ko) | 2009-12-22 | 2017-07-14 | 버텍스 파마슈티칼스 인코포레이티드 | 포스파티딜이노시톨 3-키나제의 이소인돌리논 억제제 |
JP5951600B2 (ja) * | 2010-05-21 | 2016-07-13 | インフィニティー ファーマシューティカルズ, インコーポレイテッド | キナーゼ調節のための、化合物、組成物および方法 |
AR082799A1 (es) | 2010-09-08 | 2013-01-09 | Ucb Pharma Sa | Derivados de quinolina y quinoxalina como inhibidores de quinasa |
JP2013537861A (ja) * | 2010-09-24 | 2013-10-07 | ケアストリーム ヘルス インク | テストパッチおよび濃度計を用いたインクジェット印刷の較正 |
AU2011323243A1 (en) | 2010-11-04 | 2013-05-23 | Amgen Inc. | Heterocyclic compounds and their uses |
CA2817577A1 (en) | 2010-11-10 | 2012-05-18 | Infinity Pharmaceuticals, Inc. | Heterocyclic compounds and uses thereof |
US8809349B2 (en) | 2011-01-10 | 2014-08-19 | Infinity Pharmaceuticals, Inc. | Processes for preparing isoquinolinones and solid forms of isoquinolinones |
WO2012148548A1 (en) | 2011-02-25 | 2012-11-01 | Takeda Pharmaceutical Company Limited | N-substituted oxazinopteridines and oxazinopteridinones |
AR088218A1 (es) | 2011-07-19 | 2014-05-21 | Infinity Pharmaceuticals Inc | Compuestos heterociclicos utiles como inhibidores de pi3k |
AU2012284088B2 (en) * | 2011-07-19 | 2015-10-08 | Infinity Pharmaceuticals Inc. | Heterocyclic compounds and uses thereof |
EP2751093A1 (en) | 2011-08-29 | 2014-07-09 | Infinity Pharmaceuticals, Inc. | Heterocyclic compounds and uses thereof |
-
2011
- 2011-11-10 CA CA2817577A patent/CA2817577A1/en not_active Abandoned
- 2011-11-10 EP EP11840471.4A patent/EP2637669A4/en not_active Withdrawn
- 2011-11-10 US US13/293,828 patent/US8901133B2/en active Active
- 2011-11-10 AU AU2011326427A patent/AU2011326427B2/en active Active
- 2011-11-10 CN CN201180064613.6A patent/CN103298474B/zh active Active
- 2011-11-10 WO PCT/US2011/060212 patent/WO2012064973A2/en active Application Filing
- 2011-11-10 JP JP2013538894A patent/JP2013545749A/ja active Pending
-
2014
- 2014-10-10 US US14/512,262 patent/US9388183B2/en active Active
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