[4-(aminophenyl)morpholin-2-yl]methanol | 1229980-07-7

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 恶嗪烷类
• 英文名称: [4-(aminophenyl)morpholin-2-yl]methanol
• 英文别名: [4-(4-Aminophenyl)morpholin-2-yl]methanol
• CAS: 1229980-07-7
• 化学式: C₁₁H₁₆N₂O₂
• 分子量: 208.26
• InChiKey: DOQVQDFDRBYLME-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.4
• 重原子数：
  15
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.45
• 拓扑面积：
  58.7
• 氢给体数：
  2
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  7-chloro-3-(2,6-dichlorophenyl)-4-imino-1-methyl-3,4-dihydropyrimido[4,5-d]pyrimidin-2(1H)-one 、 [4-(aminophenyl)morpholin-2-yl]methanol 在 对甲苯磺酸 作用下， 以 正丁醇 为溶剂， 反应 0.25h， 生成 3-(2,6-dichlorophenyl)-7-({4-[2-(hydroxymethyl)morpholin-4-yl]phenyl}amino)-4-imino-1-methyl-3,4-dihydropyrimido[4,5-d]pyrimidin-2(1H)-one
  参考文献：
  名称：

  [EN] DIHYDROPYRIMIDOPYRIMIDINE DERIVATIVE
  [FR] DÉRIVÉ DE DIHYDROPYRIMIDOPYRIMIDINE

  摘要：

  本发明涉及一种通式（I）的化合物，其中Ar1是一个可选取代的芳基或杂环芳基基团；R1是氢原子，可选取代的C1-C6烷基基团，或可选取代的芳基、芳基烷基或杂环芳基基团；R2是可选取代的芳基、芳基烷基或杂环芳基基团；R3是氢原子或C1-C6烷基基团。本发明的化合物具有出色的Wee1激酶抑制作用，因此在医学领域特别是各种癌症治疗方面非常有用。

  公开号：

  WO2010067886A1

文献信息

• TANK-BINDING KINASE INHIBITOR COMPOUNDS
  申请人：Gilead Sciences, Inc.

  公开号：US20160096827A1

  公开（公告）日：2016-04-07

  Compounds having the following formula (I) and methods of their use and preparation are disclosed:

  具有以下化学式（I）的化合物以及它们的使用和制备方法已被披露：
• [EN] HETEROCYCLIC COMPOUNDS AS KINASE INHIBITORS<br/>[FR] COMPOSÉS HÉTÉROCYCLIQUES EN TANT QU'INHIBITEURS DE KINASES
  申请人：ORIGENIS GMBH

  公开号：WO2012143143A1

  公开（公告）日：2012-10-26

  The present invention relates to novel compounds of formula (I) that are capable of inhibiting one or more kinases, especially SYK (Spleen Tyrosine Kinase), LRRK2 (Leucine-rich repeat kinase 2) and/or MYLK (Myosin light chain kinase) or mutants thereof. The compounds find applications in the treatment of a variety of diseases. These diseases include autoimmune diseases, inflammatory diseases, bone diseases, metabolic diseases, neurological and neurodegenerative diseases, cancer, cardiovascular diseases, allergies, asthma, alzheimer's disease, parkinson's disease, skin disorders, eye diseases, infectious diseases and hormone-related diseases.

  本发明涉及一种能够抑制一个或多个激酶，特别是SYK（脾酪氨酸激酶）、LRRK2（富含亮氨酸重复激酶2）和/或MYLK（肌球蛋白轻链激酶）或其突变体的化合物的新颖化合物（I）的公式。这些化合物在治疗各种疾病中发挥作用。这些疾病包括自身免疫疾病、炎症性疾病、骨疾病、代谢性疾病、神经和神经退行性疾病、癌症、心血管疾病、过敏、哮喘、阿尔茨海默病、帕金森病、皮肤疾病、眼部疾病、传染病和与激素相关的疾病。
• [EN] SYK INHIBITORS<br/>[FR] INHIBITEURS DE SYK
  申请人：GILEAD SCIENCES INC

  公开号：WO2016010809A1

  公开（公告）日：2016-01-21

  The present disclosure relates to compounds that are Syk inhibitors and to their use in the treatment of various disease slates, including cancer and inflammatory conditions. In particular embodiments, the structure of the compounds is given by Formula I: wherein R1, R2, R3, and R4 are as described herein. The present disclosure further provides pharmaceutical compositions that include a compound of Formula I, or pharmaceutically acceptable salts thereof, and methods of using these compounds and compositions to treat conditions mediated by Syk. In certain embodiments, also disclosed are methods for treating a cancer in a subject (e.g., a human) in need thereof, comprising administering to the subject a therapeutically effective amount of a compound of formula I, or a pharmaceutically acceptable salt thereof, in combination with a vinca-alkaloid, or a pharmaceutically acceptable salt thereof.

  本公开涉及一类Syk抑制剂化合物及其在治疗各种疾病状态中的应用，包括癌症和炎症性疾病。具体实施例中，该化合物的结构由公式I给出：其中R1、R2、R3和R4如本文所述。本公开还提供包括公式I化合物或其药学上可接受的盐的药物组合物，以及使用这些化合物和组合物治疗Syk介导的疾病的方法。在某些实施例中，还公开了治疗患有癌症的受试者（例如人类）的方法，包括向受试者施用一定量的公式I化合物或其药学上可接受的盐，与长春碱类药物或其药学上可接受的盐结合。
• SYK INHIBITORS
  申请人：Gilead Sciences, Inc.

  公开号：US20150175616A1

  公开（公告）日：2015-06-25

  The present disclosure relates to compounds that are Syk inhibitors and to their use in the treatment of various disease states, including cancer and inflammatory conditions. In particular embodiments, the structure of the compounds is given by Formula I: wherein R 1 , R 2 , R 3 , and R 4 are as described herein. The present disclosure further provides pharmaceutical compositions that include a compound of Formula I, or pharmaceutically acceptable salts or co-crystals thereof, and methods of using these compounds and compositions to treat conditions mediated by Syk.

  本公开涉及一种用于治疗各种疾病状态的Syk抑制剂化合物，包括癌症和炎症性疾病。在特定实施例中，化合物的结构由式I给出：其中R1、R2、R3和R4如本文所述。本公开还提供了包括式I化合物或其药学上可接受的盐或共晶体的药物组合物，以及使用这些化合物和组合物治疗由Syk介导的疾病的方法。
• [EN] NOVEL KINASE INHIBITORS<br/>[FR] NOUVEAUX INHIBITEURS DE KINASES
  申请人：ORIGENIS GMBH

  公开号：WO2014060113A1

  公开（公告）日：2014-04-24

  The present invention relates to novel compounds of formula (I) that are capable of inhibiting one or more kinases, especially SYK (Spleen Tyrosine Kinase), LRRK2 (Leucine-rich repeat kinase 2) and/or MYLK (Myosin light chain kinase) or mutants thereof. The compounds find applications in the treatment of a variety of diseases. These diseases include autoimmune diseases, inflammatory diseases, bone diseases, metabolic diseases, neurological and neurodegenerative diseases, cancer, cardiovascular diseases, allergies, asthma, alzheimer's disease, parkinson's disease, skin disorders, eye diseases, infectious diseases and hormone-related diseases.

  本发明涉及一种具有公式（I）的新化合物，能够抑制一个或多个激酶，特别是SYK（脾酪氨酸激酶）、LRRK2（富含亮氨酸重复的激酶2）和/或MYLK（肌球蛋白轻链激酶）或其突变体。这些化合物在治疗多种疾病中发挥作用。这些疾病包括自身免疫疾病、炎症性疾病、骨疾病、代谢性疾病、神经和神经退行性疾病、癌症、心血管疾病、过敏、哮喘、阿尔茨海默病、帕金森病、皮肤疾病、眼部疾病、传染病和激素相关疾病。