6-amino-5-[1-(2,6-dichloro-3-fluoro-phenyl)-ethoxy]-N-methyl-nicotinamidine

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: 6-amino-5-[1-(2,6-dichloro-3-fluoro-phenyl)-ethoxy]-N-methyl-nicotinamidine
• 英文别名: 6-amino-5-[1-(2,6-dichloro-3-fluorophenyl)ethoxy]-N'-methylpyridine-3-carboximidamide
• 化学式: C₁₅H₁₅Cl₂FN₄O
• 分子量: 357.215
• InChiKey: BDXZDWNJDGDWIQ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.8
• 重原子数：
  23
• 可旋转键数：
  4
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.2
• 拓扑面积：
  86.5
• 氢给体数：
  2
• 氢受体数：
  5

反应信息

• 作为产物：
  描述：

  Methyl 6-amino-5-[1-(2,6-dichloro-3-fluorophenyl)ethoxy]pyridine-3-carboximidate 、 甲胺 以 四氢呋喃 、 甲醇 为溶剂， 生成 6-amino-5-[1-(2,6-dichloro-3-fluoro-phenyl)-ethoxy]-N-methyl-nicotinamidine
  参考文献：
  名称：

  [EN] AMINOHETEROARYL COMPOUNDS AS PROTEIN TYROSINE KINASE INHIBITORS
  [FR] COMPOSES AMINOHETEROARYLES EN TANT QU'INHIBITEURS DES PROTEINES TYROSINE KINASES

  摘要：

  提供了氨基杂环芳基化合物，以及它们的合成和使用方法。优选化合物是c-Met蛋白激酶的强效抑制剂，并且在治疗异常细胞生长紊乱，如癌症方面具有用处。

  公开号：

  WO2006021886A1

文献信息

• [EN] AMINOHETEROARYL COMPOUNDS AS PROTEIN TYROSINE KINASE INHIBITORS<br/>[FR] COMPOSES AMINOHETEROARYLES EN TANT QU'INHIBITEURS DES PROTEINES TYROSINE KINASES
  申请人：PFIZER

  公开号：WO2006021886A1

  公开（公告）日：2006-03-02

  Aminoheteroaryl compounds are provided, as well as methods for their synthesis and use. Preferred compounds are potent inhibitors of the c-Met protein kinase, and are useful in the treatment of abnormal cell growth disorders, such as cancers.

  提供了氨基杂环芳基化合物，以及它们的合成和使用方法。优选化合物是c-Met蛋白激酶的强效抑制剂，并且在治疗异常细胞生长紊乱，如癌症方面具有用处。
• ENANTIOMERICALLY PURE AMINOHETEROARYL COMPOUNDS AS PROTEIN KINASE INHIBITORS
  申请人：CUI Jingrong Jean

  公开号：US20140288086A1

  公开（公告）日：2014-09-25

  Enantiomerically pure compound of formula 1 are provided, as well as methods for their synthesis and use. Preferred compounds are potent inhibitors of the c-Met protein kinase, and are useful in the treatment of abnormal cell growth disorders, such as cancers.

  本发明提供了公式1的对映纯化合物，以及它们的合成和使用方法。首选化合物是c-Met蛋白激酶的强效抑制剂，可用于治疗异常细胞增生性疾病，例如癌症。
• Aminoheteroaryl compounds as protein kinase inhibitors
  申请人：Cui Jean Jingrong

  公开号：US20050009840A1

  公开（公告）日：2005-01-13

  Aminopyridine and aminopyrazine compounds of formula (1), compositions including these compounds, and methods of their use are provided. Preferred compounds of formula 1 have activity as protein kinase inhibitors, including as inhibitors of c-MET.

  提供了公式（1）的氨基吡啶和氨基吡嗪化合物、包括这些化合物的组合物以及它们的使用方法。公式1的优选化合物具有作为蛋白激酶抑制剂的活性，包括作为c-MET的抑制剂。
• AGENT FOR PREVENTING AND/OR TREATING AMYOTROPHIC LATERAL SCLEROSIS
  申请人：Kyoto University

  公开号：EP3246046A1

  公开（公告）日：2017-11-22

  The present invention provides a prophylactic and/or therapeutic agent for amyotrophic lateral sclerosis (ALS), which contains one or more kinase inhibitors selected from the group consisting of an epithelial cell growth factor receptor (EGFR) inhibitor, a fibroblast growth factor receptor (FGFR) inhibitor, an Aurorakinase inhibitor, a protein kinase A (PKA) inhibitor, a protein kinase C (PKC) inhibitor, an MEK inhibitor, an Met inhibitor, a JNK inhibitor, a Syk inhibitor and a JAK inhibitor, a prostaglandin analogue and an estrogen receptor antagonist, or one or more kinase inhibitors selected from the group consisting of Tivozanib and an analog thereof, SB 216763, Cdk2 Inhibitor II, BUDESONIDE, RIBOFLAVIN, alpha-TOCHOPHEROL, AMODIAQUINE, SU9516, Sunitinib and an analog thereof, GSK-3 Inhibitor XIII, Bisindolylmaleimide I, HYDROQUINONE, FLUNISOLIDE, MGCD-265, Indirubin-3'-monoxime, HYDRASTINE (1R,9S), PIPERINE, BUTAMBEN, Axitinib and an analog thereof, APOMORPHINE, FENBUFEN, Bosutinib (SKI-606) and an analog thereof, a Wee1 Inhibitor, Cdk2 Inhibitor IV, NU6140, 3-hydroxybutyric acid, AT9283, Imatinib, Nilotinib, Rebastinib, and Bafetinib for the prophylaxis and/or treatment of ALS. Particularly, using a compound already on the market as a pharmaceutical product, a pharmaceutical product for the prophylaxis or treatment of ALS can be developed rapidly at a low cost.

  本发明提供了一种肌萎缩性脊髓侧索硬化症（ALS）的预防和/或治疗剂，它含有一种或多种激酶抑制剂，这些激酶抑制剂选自由上皮细胞生长因子受体（EGFR）抑制剂、成纤维细胞生长因子受体（FGFR）抑制剂、Aurorakinase抑制剂、蛋白激酶A（PKA）抑制剂、蛋白激酶C（PKC）抑制剂组成的组、成纤维细胞生长因子受体 (FGFR) 抑制剂、Aurorakinase 抑制剂、蛋白激酶 A (PKA) 抑制剂、蛋白激酶 C (PKC) 抑制剂、MEK 抑制剂、Met 抑制剂、JNK 抑制剂、Syk 抑制剂和 JAK 抑制剂、前列腺素类似物和雌激素受体拮抗剂、或一种或多种激酶抑制剂，这些激酶抑制剂选自以下组别：Tivozanib 及其类似物、SB 216763、Cdk2 抑制剂 II、BUDESONIDE、RIBOFLAVIN、alpha-TOCHOPHEROL、AMODIAQUINE、SU9516、Sunitinib 及其类似物、GSK-3 抑制剂 XIII、Bisindolylmaleimide I、HYDROQUINONE、FLUNISOLIDE、MGCD-265、吲哚啉-3'-monoxime、氢化胱氨酸 (1R,9S)、哌啶、布坦本、阿希替尼及其类似物、阿朴磷、芬布芬、博苏替尼 (SKI-606) 及其类似物、Wee1抑制剂、Cdk2抑制剂IV、NU6140、3-羟基丁酸、AT9283、伊马替尼、尼洛替尼、雷巴替尼和巴非替尼，用于预防和/或治疗ALS。特别是，利用已作为药品上市的化合物，可以低成本快速开发出预防或治疗 ALS 的药品。
• BOSUTINIB, SUNITINIB, TIVOZANIB, IMATINIB, NILOTINIB, REBASTINIB OR BAFETINIB FOR PREVENTING AND/OR TREATING AMYOTROPHIC LATERAL SCLEROSIS
  申请人：KYOTO UNIVERSITY

  公开号：EP3789027A1

  公开（公告）日：2021-03-10

  The present invention provides a compound for use in the prophylaxis and/or treatment of amyotrophic lateral sclerosis (ALS), wherein said compound is selected from the group consisting of bosutinib, sunitinib, tivozanib, imatinib, nilotinib, rebastinib and bafetinib. Particularly, using a compound already on the market as a pharmaceutical product, a pharmaceutical product for the prophylaxis or treatment of ALS can be developed rapidly at a low cost.

  本发明提供了一种用于预防和/或治疗肌萎缩性脊髓侧索硬化症（ALS）的化合物，其中所述化合物选自由博苏替尼、舒尼替尼、替沃扎尼、伊马替尼、尼洛替尼、瑞帕替尼和巴非替尼组成的组。特别是，利用已作为药品上市的化合物，可以低成本快速开发预防或治疗 ALS 的药品。