CN110582483A - 含邻氨基杂芳环炔基的化合物及其制备方法和用途 - Google Patents

含邻氨基杂芳环炔基的化合物及其制备方法和用途 Download PDF

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CN110582483A
CN110582483A CN201880012699.XA CN201880012699A CN110582483A CN 110582483 A CN110582483 A CN 110582483A CN 201880012699 A CN201880012699 A CN 201880012699A CN 110582483 A CN110582483 A CN 110582483A
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胡有洪
耿美玉
任文明
丁健
官晓聪
艾菁
王浪
彭霞
刘杨
戴阳
曾丽敏
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Shanghai Institute of Materia Medica of CAS
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Abstract

含邻氨基杂芳环炔基的化合物及其制备方法和用途，所述含邻氨基杂芳环炔基的化合物的结构如式(I)所示，所述式(I)化合物具有FGFR和RET双靶抑制活性高，并且KDR活性相对较低的优点，而且所述式(I)化合物在人肺癌NCI‑H1581及胃癌细胞株SNU16及RET依赖性敏感细胞株BaF3‑CCDC6‑Ret及突变型均显示出了很强的抑制活性，通过药代数据表明所述含邻氨基杂芳炔基的化合物具有成药性，且在长期的动物药效模型上表现相关的明显抑制相关肿瘤的生长，在药效剂量下，动物状态好。

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PCT国内申请，说明书已公开。

Claims (10)

  1. PCT国内申请，权利要求书已公开。
CN201880012699.XA 2017-02-20 2018-02-12 含邻氨基杂芳环炔基的化合物及其制备方法和用途 Active CN110582483B (zh)

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CN108456163A (zh) * 2017-02-20 2018-08-28 中国科学院上海药物研究所 含邻氨基杂芳环炔基的化合物及其制备方法和用途
CN114075135A (zh) * 2020-08-10 2022-02-22 上海润石医药科技有限公司 含邻氨基吡啶炔基的化合物的盐及其制备方法和应用

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PL2918588T3 (pl) 2010-05-20 2017-10-31 Array Biopharma Inc Związki makrocykliczne jako inhibitory kinazy TRK
EP3571203B1 (en) 2017-01-18 2023-06-07 Array BioPharma Inc. Substituted pyrazolo[1,5-a]pyrazine compounds as ret kinase inhibitors
JOP20190213A1 (ar) 2017-03-16 2019-09-16 Array Biopharma Inc مركبات حلقية ضخمة كمثبطات لكيناز ros1
TWI791053B (zh) 2017-10-10 2023-02-01 美商亞雷生物製藥股份有限公司 6-(2-羥基-2-甲基丙氧基)-4-(6-(6-((6-甲氧基吡啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚-3-基)吡啶-3-基)吡唑并[1,5-a]吡啶-3-甲腈之結晶形式及其醫藥組合物
TWI812649B (zh) 2017-10-10 2023-08-21 美商絡速藥業公司 6-(2-羥基-2-甲基丙氧基)-4-(6-(6-((6-甲氧基吡啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚-3-基)吡啶-3-基)吡唑并[1,5-a]吡啶-3-甲腈之調配物
TWI802635B (zh) 2018-01-18 2023-05-21 美商亞雷生物製藥股份有限公司 作為ｒｅｔ激酶抑制劑之經取代吡咯并[2,3-d]嘧啶化合物
JP6997876B2 (ja) 2018-01-18 2022-02-04 アレイ バイオファーマ インコーポレイテッド Ｒｅｔキナーゼ阻害剤としての置換ピラゾリル［４，３－ｃ］ピリジン化合物
US11524963B2 (en) 2018-01-18 2022-12-13 Array Biopharma Inc. Substituted pyrazolo[3,4-d]pyrimidines as RET kinase inhibitors
WO2020131674A1 (en) 2018-12-19 2020-06-25 Array Biopharma Inc. 7-((3,5-dimethoxyphenyl)amino)quinoxaline derivatives as fgfr inhibitors for treating cancer
CN111662227B (zh) * 2019-03-06 2022-07-05 中国科学院上海药物研究所 邻氨基吡啶炔类化合物及其制备方法和用途
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CN114853739B (zh) * 2021-02-03 2023-09-22 药雅科技(上海)有限公司 一种炔代吡嗪类fgfr抑制剂及其制备方法和用途
CN116730978A (zh) * 2022-03-11 2023-09-12 中国科学院上海药物研究所 一类含杂芳环炔基化合物及其制备方法和用途

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