[4-(3-(S)-hydroxypiperidin-1-yl)phenyl]amine | 1042917-57-6

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 哌啶类
• 英文名称: [4-(3-(S)-hydroxypiperidin-1-yl)phenyl]amine
• 英文别名: (3S)-1-(4-Aminophenyl)-3-piperidinol；(3S)-1-(4-aminophenyl)piperidin-3-ol
• CAS: 1042917-57-6
• 化学式: C₁₁H₁₆N₂O
• 分子量: 192.261
• InChiKey: GFPPPMAWVWTROZ-NSHDSACASA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.2
• 重原子数：
  14
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.45
• 拓扑面积：
  49.5
• 氢给体数：
  2
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  [4-(3-(S)-hydroxypiperidin-1-yl)phenyl]amine 在 氢溴酸 、 sodium nitrite 、 copper(I) bromide 、 sodium hydroxide 作用下， 以 水 、 乙酸乙酯 为溶剂， 反应 2.25h， 以84%的产率得到4-bromo-1-(3-(S)-hydroxypiperidin-1-yl)benzene
  参考文献：
  名称：

  WO2008/90181

  摘要：

  公开号：

文献信息

• [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。
• [EN] PYRAZOLO[4,3-D]PYRIMIDINES AS KINASE INHIBITORS<br/>[FR] PYRAZOLO[4,3-D]PYRIMIDINES UTILES EN TANT QU'INHIBITEURS DE KINASES
  申请人：ORIGENIS GMBH

  公开号：WO2014060112A1

  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.

  本发明涉及具有式（I）的新化合物，其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多种疾病。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。
• 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。
• [EN] NOVEL PHENYLAMINOPYRIMIDINE COMPOUND HAVING INHIBITORY ACTIVITY AGAINST LRRK2 AND USE THEREOF<br/>[FR] NOUVEAU COMPOSÉ DE PHÉNYLAMINOPYRIMIDINE AYANT UNE ACTIVITÉ INHIBITRICE CONTRE LRRK2 ET SON UTILISATION<br/>[KO] LRRK2에 대해 저해 활성을 갖는 신규한 페닐아미노피리미딘 화합물 및 이의 용도
  申请人：STANDIGM INC

  公开号：WO2022203466A1

  公开（公告）日：2022-09-29

  본 발명은 화학식 1의 피리미딘 화합물, 이를 포함하는 LRRK2에 의해 매개되거나 이와 관련된 질병(예컨대, 파킨슨병)의 예방 또는 치료용 약학적 조성물, 및 이를 이용한 질병 또는 질환의 치료 및 예방 방법을 제공한다. 본 발명에 따른 피리미딘 화합물은 LRRK2 저해 활성이 우수하여 LRRK2와 관련된 질병(예컨대, 파킨슨병)의 예방 또는 치료에 효과적으로 사용될 수 있다.

  本发明提供了一种化学式为1的嘧啶化合物，以及包含该化合物的用于预防或治疗由LRRK2介导或与之相关的疾病（例如帕金森病）的药物组合物，以及使用该组合物治疗和预防疾病或疾病的方法。根据本发明，嘧啶化合物具有优异的LRRK2抑制活性，可有效用于预防或治疗与LRRK2相关的疾病（例如帕金森病）。