CN102850328A - 吡啶类化合物、其制备方法、包含该化合物的药物组合物及其用途 - Google Patents
吡啶类化合物、其制备方法、包含该化合物的药物组合物及其用途 Download PDFInfo
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- CN102850328A CN102850328A CN2011101832745A CN201110183274A CN102850328A CN 102850328 A CN102850328 A CN 102850328A CN 2011101832745 A CN2011101832745 A CN 2011101832745A CN 201110183274 A CN201110183274 A CN 201110183274A CN 102850328 A CN102850328 A CN 102850328A
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- PLUVJGUMODTQQX-QGZVFWFLSA-N CCNC(Nc(ncc(-c1c[n](C(CC2)CCN2C(OC(C)(C)C)=O)nc1)c1)c1O[C@H](C)c(c(Cl)c(cc1)F)c1Cl)=S Chemical compound CCNC(Nc(ncc(-c1c[n](C(CC2)CCN2C(OC(C)(C)C)=O)nc1)c1)c1O[C@H](C)c(c(Cl)c(cc1)F)c1Cl)=S PLUVJGUMODTQQX-QGZVFWFLSA-N 0.000 description 1
- HKXNFTAKLYMKDM-CQSZACIVSA-N CCNC(Nc(ncc(-c1c[n](C2CCNCC2)nc1)c1)c1O[C@H](C)c(c(Cl)ccc1F)c1Cl)=S Chemical compound CCNC(Nc(ncc(-c1c[n](C2CCNCC2)nc1)c1)c1O[C@H](C)c(c(Cl)ccc1F)c1Cl)=S HKXNFTAKLYMKDM-CQSZACIVSA-N 0.000 description 1
- DIMBEDHLPXGRDB-QGZVFWFLSA-N CCOC(Nc(ncc(-c1c[n](C(CC2)CCN2C(OC(C)(C)C)=O)nc1)c1)c1O[C@H](C)c(c(Cl)c(cc1)F)c1Cl)=O Chemical compound CCOC(Nc(ncc(-c1c[n](C(CC2)CCN2C(OC(C)(C)C)=O)nc1)c1)c1O[C@H](C)c(c(Cl)c(cc1)F)c1Cl)=O DIMBEDHLPXGRDB-QGZVFWFLSA-N 0.000 description 1
- PWRXUPONCFVMOY-CQSZACIVSA-N CCOC(Nc(ncc(-c1c[n](C2CCNCC2)nc1)c1)c1O[C@H](C)c(c(Cl)ccc1F)c1Cl)=O Chemical compound CCOC(Nc(ncc(-c1c[n](C2CCNCC2)nc1)c1)c1O[C@H](C)c(c(Cl)ccc1F)c1Cl)=O PWRXUPONCFVMOY-CQSZACIVSA-N 0.000 description 1
- XRUQLGJNOWNRKE-MRXNPFEDSA-N C[C@H](c(c(Cl)ccc1F)c1Cl)Oc1c(NC(N2CCOCC2)=O)ncc(-c2c[n](C3CCNCC3)nc2)c1 Chemical compound C[C@H](c(c(Cl)ccc1F)c1Cl)Oc1c(NC(N2CCOCC2)=O)ncc(-c2c[n](C3CCNCC3)nc2)c1 XRUQLGJNOWNRKE-MRXNPFEDSA-N 0.000 description 1
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Abstract
Description
化合物 | 抑制率 | IC50(μM) | 化合物 | 抑制率 | IC50(μM) |
IA-1 | 94.8%10μM | <0.1 | ID-1 | 96.4%10μM | <0.1 |
IA-2 | 95.2%10μM | <0.1 | ID-2 | 92.0%10μM | <0.1 |
IA-3 | 94.0%10μM | <0.1 | ID-3 | 98.4%10μM | <0.01 |
IA-4 | 94.2%10μM | <1 | ID-4 | 67.2%10μM | <1 |
IB-1 | 58.5%10μM | <1 | ID-5 | 96.7%10μM | <0.1 |
IB-2 | 98.4%10μM | <0.01 | ID-6 | 95.5%10μM | <1 |
IB-3 | 72.7%10μM | <1 | IE-1 | 83.9%10μM | <0.1 |
IB-4 | 74.9%10μM | <1 | IE-2 | 83.7%10μM | <1 |
IC-1 | 99.0%10μM | <0.01 | IF-1 | 91.0%10μM | <1 |
IC-2 | 64.8%10μM | <10 | IF-2 | 91.0%10μM | <1 |
化合物 | 抑制率 | IC50(μM) | 化合物 | 抑制率 | IC50(μM) |
IA-1 | 74.8%10μM | <1 | ID-1 | 73.2%10μM | <1 |
IA-2 | 85.2%10μM | <0.1 | ID-2 | 82.0%10μM | <0.1 |
IA-3 | 64.0%10μM | <1 | ID-3 | 68.4%10μM | <1 |
IA-4 | 74.2%10μM | <1 | ID-4 | 73.2%10μM | <1 |
IB-1 | 70.2%10μM | <1 | ID-5 | 66.7%10μM | <1 |
IB-2 | 73.3%10μM | <1 | ID-6 | 85.5%10μM | <0.1 |
IB-3 | 72.7%10μM | <1 | IE-1 | 63.9%10μM | <1 |
IB-4 | 74.9%10μM | <1 | IE-2 | 73.7%10μM | <1 |
IC-1 | 69.0%10μM | <1 | IF-1 | 71.0%10μM | <1 |
IC-2 | 74.8%10μM | <10 | IF-2 | 81.0%10μM | <0.1 |
Claims (10)
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Cited By (15)
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CN103373986A (zh) * | 2012-04-22 | 2013-10-30 | 东南大学 | 克里唑替尼前药及其制备方法与用途 |
CN103842353A (zh) * | 2011-09-21 | 2014-06-04 | 苏州韬略生物科技有限公司 | 作为激酶抑制剂的吡啶化合物 |
WO2014124594A1 (zh) * | 2013-02-16 | 2014-08-21 | 浙江九洲药业股份有限公司 | 一种克里唑替尼的制备方法 |
WO2014139391A1 (en) * | 2013-03-11 | 2014-09-18 | Teligene Ltd | Substituted pyridine compounds as kinases inhibitors |
CN104059054A (zh) * | 2013-03-19 | 2014-09-24 | 浙江导明医药科技有限公司 | 用于治疗癌症的三级环状胺alk激酶抑制剂 |
CN104230890A (zh) * | 2013-06-19 | 2014-12-24 | 信诺凯(北京)化工有限公司 | 吡啶-2-胺衍生物及其制法和药物组合物与用途 |
CN104557870A (zh) * | 2013-10-25 | 2015-04-29 | 正大天晴药业集团股份有限公司 | 一种吡啶胺化合物的富马酸盐 |
CN105175351A (zh) * | 2014-05-30 | 2015-12-23 | 中国科学院上海药物研究所 | 一类3-氨基-苯并五元杂环化合物及其制备方法和用途 |
WO2016169030A1 (zh) * | 2015-04-23 | 2016-10-27 | 正大天晴药业集团股份有限公司 | 吡啶胺化合物的富马酸盐及其晶体 |
CN107207528A (zh) * | 2014-08-20 | 2017-09-26 | 苏州韬略生物科技有限公司 | 作为激酶抑制剂的经取代大环及其使用方法 |
CN104557869B (zh) * | 2013-10-25 | 2017-09-26 | 正大天晴药业集团股份有限公司 | 一种吡啶胺化合物富马酸盐的晶型 |
CN108191833A (zh) * | 2018-01-17 | 2018-06-22 | 浙江树人学院 | 克唑替尼衍生物及其制备方法和应用 |
WO2020233710A1 (zh) * | 2019-05-22 | 2020-11-26 | 正大天晴药业集团股份有限公司 | 吡啶胺化合物的药物组合物及其在ros1阳性非小细胞肺癌中的应用 |
US11046658B2 (en) | 2018-07-02 | 2021-06-29 | Incyte Corporation | Aminopyrazine derivatives as PI3K-γ inhibitors |
US11926616B2 (en) | 2018-03-08 | 2024-03-12 | Incyte Corporation | Aminopyrazine diol compounds as PI3K-γ inhibitors |
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CN103842353A (zh) * | 2011-09-21 | 2014-06-04 | 苏州韬略生物科技有限公司 | 作为激酶抑制剂的吡啶化合物 |
US20140350050A1 (en) * | 2011-09-21 | 2014-11-27 | Teligene Ltd. | Pyridine compounds as inhibitors of kinase |
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