{1-[2-(4-amino-phenoxy)-ethyl]-piperidin-4-yl}-methanol | 1099658-14-6

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯酚醚
• 英文名称: {1-[2-(4-amino-phenoxy)-ethyl]-piperidin-4-yl}-methanol
• 英文别名: 1-[2-(4-Aminophenoxy)ethyl]-4-piperidinemethanol；[1-[2-(4-aminophenoxy)ethyl]piperidin-4-yl]methanol
• CAS: 1099658-14-6
• 化学式: C₁₄H₂₂N₂O₂
• mdl: MFCD11551891
• 分子量: 250.341
• InChiKey: JUJUWXOAZRFAGX-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.3
• 重原子数：
  18
• 可旋转键数：
  5
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.571
• 拓扑面积：
  58.7
• 氢给体数：
  2
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  {1-[2-(4-nitro-phenoxy)-ethyl]-piperidin-4-yl}-methanol 在 palladium 10% on activated carbon 氢气 作用下， 以 甲醇 为溶剂， 以95.5%的产率得到{1-[2-(4-amino-phenoxy)-ethyl]-piperidin-4-yl}-methanol
  参考文献：
  名称：

  [EN] 2, 4 -DIAMINOPYRIMIDINE DERIVATIVES AS PROTEIN KINASE INHIBITORS
  [FR] DÉRIVÉS DE 2,4-DIAMINOPYRIMIDINE EN TANT QU'INHIBITEURS DE PROTÉINE KINASES

  摘要：

  本发明涉及一种新型的式（I）的嘧啶衍生物，其作为激酶抑制剂具有用途。更具体地，本发明涉及新型嘧啶化合物、其制备方法、含有这些化合物的药物组合物以及这些化合物在治疗增殖性疾病中的用途。

  公开号：

  WO2012059932A1

文献信息

• NOVEL KINASE INHIBITORS
  申请人：ORIGENIS GMBH

  公开号：US20150259340A1

  公开（公告）日：2015-09-17

  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.

  本发明涉及式（I）的新型化合物，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。这些化合物可用于治疗各种疾病。这些疾病包括自身免疫性疾病、炎症性疾病、骨病、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。
• PYRAZOLO[4,3-D]PYRIMIDINES AS KINASE INHIBITORS
  申请人：ORIGENIS GMBH

  公开号：US20150266882A1

  公开（公告）日：2015-09-24

  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.

  本发明涉及化合物(I)的新型化合物，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方面有应用。这些疾病包括自身免疫疾病、炎症性疾病、骨病、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、眼病、传染病和激素相关疾病。
• Kinase inhibitors
  申请人：Origenis GmbH

  公开号：US10000482B2

  公开（公告）日：2018-06-19

  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.

  本发明涉及能够抑制一种或多种激酶，特别是 SYK（脾酪氨酸激酶）、LRRK2（富亮氨酸重复激酶 2）和/或 MYLK（肌球蛋白轻链激酶）或其突变体的新型式（I）化合物。这些化合物可用于治疗多种疾病。这些疾病包括自身免疫性疾病、炎症性疾病、骨病、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、老年痴呆症、帕金森病、皮肤病、眼病、传染病和激素相关疾病。
• US9637491B2
  申请人：——

  公开号：US9637491B2

  公开（公告）日：2017-05-02
• [EN] 2, 4 -DIAMINOPYRIMIDINE DERIVATIVES AS PROTEIN KINASE INHIBITORS<br/>[FR] DÉRIVÉS DE 2,4-DIAMINOPYRIMIDINE EN TANT QU'INHIBITEURS DE PROTÉINE KINASES
  申请人：AURIGENE DISCOVERY TECH LTD

  公开号：WO2012059932A1

  公开（公告）日：2012-05-10

  The present invention relates to novel pyrimide derivatives of formula (I): that are useful as kinase inhibitors. More particularly, the present invention relates to novel pyrimidine compounds, methods for their preparation, pharmaceutical compositions containing these compounds and uses of these compounds in the treatment of proliferative disorders.

  本发明涉及一种新型的式（I）的嘧啶衍生物，其作为激酶抑制剂具有用途。更具体地，本发明涉及新型嘧啶化合物、其制备方法、含有这些化合物的药物组合物以及这些化合物在治疗增殖性疾病中的用途。