3-氟-5-甲氧基吡啶-2-胺 | 1211589-70-6

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡啶及其衍生物
• 中文名称: 3-氟-5-甲氧基吡啶-2-胺
• 英文名称: 3-fluoro-5-methoxypyridin-2-amine
• CAS: 1211589-70-6
• 化学式: C₆H₇FN₂O
• 分子量: 142.133
• InChiKey: XDOHJTASOZCWFE-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.6
• 重原子数：
  10
• 可旋转键数：
  1
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.17
• 拓扑面积：
  48.1
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  2-[1-(4-fluorophenyl)-3-[2-(4-methoxyphenyl)ethyl]-5-oxo-2-sulfanylideneimidazolidin-4-yl]acetic acid 、 3-氟-5-甲氧基吡啶-2-胺 在 草酰氯 、 N,N-二甲基甲酰胺 、 吡啶 作用下， 以 二氯甲烷 为溶剂， 反应 18.0h， 以14%的产率得到N-(3-fluoro-5-methoxypyridin-2-yl)-2-[1-(4-fluorophenyl)-3-[2-(4-methoxyphenyl)ethyl]-5-oxo-2-sulfanylideneimidazolidin-4-yl]acetamide
  参考文献：
  名称：

  [EN] HYDANTOIN AND THIOHYDANTOIN DERIVATIVES AS ANTIVIRAL DRUGS
  [FR] DÉRIVÉS D'HYDANTOÏNE ET DE THIOHYDANTOÏNE UTILISÉS COMME MÉDICAMENTS ANTIVIRAUX

  摘要：

  本发明涉及以下式（I）的化合物，或其盐、溶剂合物、互变异构体、对映异构体、顺反异构体或混合物，以及其作为药物的用途，特别是在治疗丙型肝炎方面的用途，其制备过程以及含有这种化合物的药物组合物。

  公开号：

  WO2013171281A1
• 作为产物：
  描述：

  3,5-difluoro-2-nitropyridine 在 甲醇 、 palladium 10% on activated carbon 、 氢气 作用下， 以 甲醇 为溶剂， 反应 18.0h， 生成 3-氟-5-甲氧基吡啶-2-胺
  参考文献：
  名称：

  [EN] HYDANTOIN AND THIOHYDANTOIN DERIVATIVES AS ANTIVIRAL DRUGS
  [FR] DÉRIVÉS D'HYDANTOÏNE ET DE THIOHYDANTOÏNE UTILISÉS COMME MÉDICAMENTS ANTIVIRAUX

  摘要：

  本发明涉及以下式（I）的化合物，或其盐、溶剂合物、互变异构体、对映异构体、顺反异构体或混合物，以及其作为药物的用途，特别是在治疗丙型肝炎方面的用途，其制备过程以及含有这种化合物的药物组合物。

  公开号：

  WO2013171281A1

文献信息

• [EN] COMPOUNDS AND METHODS FOR KINASE MODULATION, AND INDICATIONS THEREFOR<br/>[FR] COMPOSÉS ET MÉTHODES UTILISÉS POUR LA MODULATION DES KINASES ET INDICATIONS À CET EFFET
  申请人：PLEXXIKON INC

  公开号：WO2011063159A1

  公开（公告）日：2011-05-26

  Compounds and salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof and uses thereof are described. In certain aspects and embodiments, the described compounds or salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof are active on at least one Raf protein kinase. In certain aspects and embodiments, the described compounds are active in inhibiting proliferation of a Ras mutant cell line. Also described are methods of use thereof to treat diseases and conditions, including diseases and conditions associated with activity of B-Raf V600E mutant protein kinase, including melanoma, glioma, glioblastoma multiforme, pilocytic astrocytoma, colorectal cancer, thyroid cancer, lung cancer, ovarian cancer, prostate cancer, liver cancer, gallbladder cancer, gastrointestinal stromal tumors, biliary tract cancer, and cholangiocarcinoma. Also described are methods of use thereof to treat diseases and conditions, including diseases and conditions associated with activity of c-Raf-1 protein kinase, including acute pain, chronic pain or polycystic kidney disease.

  描述了化合物及其盐、配方、共轭物、衍生物、形式和用途。在某些方面和实施例中，所述化合物或其盐、配方、共轭物、衍生物、形式对至少一种Raf蛋白激酶具有活性。在某些方面和实施例中，所述化合物在抑制Ras突变细胞系增殖方面具有活性。还描述了使用这些方法来治疗疾病和病况，包括与B-Raf V600E突变蛋白激酶活性相关的疾病和病况，包括黑色素瘤、胶质瘤、胶质母细胞瘤、乳头状星形细胞瘤、结直肠癌、甲状腺癌、肺癌、卵巢癌、前列腺癌、肝癌、胆囊癌、胃肠间质瘤、胆道癌和胆管癌。还描述了使用这些方法来治疗与c-Raf-1蛋白激酶活性相关的疾病和病况，包括急性疼痛、慢性疼痛或多囊肾病。
• TYK2 INHIBITORS AND USES THEREOF
  申请人：Nimbus Lakshmi, Inc.

  公开号：US20190031664A1

  公开（公告）日：2019-01-31

  The present invention provides compounds, compositions thereof, and methods of using the same for the inhibition of TYK2, and the treatment of TYK2-mediated disorders.

  本发明提供了化合物、其组合物以及使用这些化合物来抑制TYK2以及治疗TYK2介导的疾病的方法。
• IMIDAZOLONYLQUINOLINES AND THE USE THEREOF AS ATM KINASE INHIBITORS
  申请人：Merck Patent GmbH

  公开号：US20180072715A1

  公开（公告）日：2018-03-15

  Compounds of the formula (I), which are ATM kinase inhibitors and can be employed, inter alia, for the treatment of cancer.

  式(I)的化合物是ATM激酶抑制剂，可用于治疗癌症。
• Compounds and Methods for Kinase Modulation, and Indications Therefor
  申请人：Ibrahim Prabha N.

  公开号：US20110152258A1

  公开（公告）日：2011-06-23

  Compounds and salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof and uses thereof are described. In certain aspects and embodiments, the described compounds or salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof are active on at least one Raf protein kinase. In certain aspects and embodiments, the described compounds are active in inhibiting proliferation of a Ras mutant cell line. Also described are methods of use thereof to treat diseases and conditions, including diseases and conditions associated with activity of B-Raf V600E mutant protein kinase, including melanoma, glioma, glioblastoma multiforme, pilocytic astrocytoma, colorectal cancer, thyroid cancer, lung cancer, ovarian cancer, prostate cancer, liver cancer, gallbladder cancer, gastrointestinal stromal tumors, biliary tract cancer, and cholangiocarcinoma. Also described are methods of use thereof to treat diseases and conditions, including diseases and conditions associated with activity of c-Raf-1 protein kinase, including acute pain, chronic pain or polycystic kidney disease.

  本文描述了化合物及其盐、制剂、共轭物、衍生物、形式和用途。在某些方面和实施例中，所述的化合物或其盐、制剂、共轭物、衍生物、形式对至少一种Raf蛋白激酶具有活性。在某些方面和实施例中，所述的化合物对抑制Ras突变细胞系的增殖具有活性。还描述了使用这些化合物的方法来治疗与B-Raf V600E突变蛋白激酶活性相关的疾病和病症，包括黑色素瘤、胶质瘤、多形性胶质母细胞瘤、毛细胞星形胶质瘤、结肠直肠癌、甲状腺癌、肺癌、卵巢癌、前列腺癌、肝癌、胆囊癌、胃肠间质瘤、胆道癌和胆管癌。还描述了使用这些化合物的方法来治疗与c-Raf-1蛋白激酶活性相关的疾病和病症，包括急性疼痛、慢性疼痛或多囊肾病。
• COMPOUNDS AND METHODS FOR KINASE MODULATION, AND INDICATIONS THEREFOR
  申请人：Plexxikon Inc.

  公开号：US20140288070A1

  公开（公告）日：2014-09-25

  Compounds and salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof and uses thereof are described. In certain aspects and embodiments, the described compounds or salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof are active on at least one Raf protein kinase. In certain aspects and embodiments, the described compounds are active in inhibiting proliferation of a Ras mutant cell line. Also described are methods of use thereof to treat diseases and conditions, including diseases and conditions associated with activity of B-Raf V600E mutant protein kinase, including melanoma, glioma, glioblastoma multiforme, pilocytic astrocytoma, colorectal cancer, thyroid cancer, lung cancer, ovarian cancer, prostate cancer, liver cancer, gallbladder cancer, gastrointestinal stromal tumors, biliary tract cancer, and cholangiocarcinoma. Also described are methods of use thereof to treat diseases and conditions, including diseases and conditions associated with activity of c-Raf-1 protein kinase, including acute pain, chronic pain or polycystic kidney disease.

  本文描述了化合物及其盐、制剂、共轭物、衍生物、形式和用途。在某些方面和实施例中，所述的化合物或其盐、制剂、共轭物、衍生物、形式至少对一种Raf蛋白激酶具有活性。在某些方面和实施例中，所述的化合物具有抑制Ras突变细胞系增殖的活性。还描述了使用它们治疗疾病和病症的方法，包括与B-Raf V600E突变蛋白激酶活性相关的疾病和病症，包括黑色素瘤、胶质瘤、多形性胶质母细胞瘤、毛细胞星形细胞瘤、结直肠癌、甲状腺癌、肺癌、卵巢癌、前列腺癌、肝癌、胆囊癌、胃肠道间质瘤、胆道癌和胆管癌。还描述了使用它们治疗与c-Raf-1蛋白激酶活性相关的疾病和病症的方法，包括急性疼痛、慢性疼痛或多囊肾病。