tert-butyl 3-azido-4-oxopiperidine-1-carboxylate | 1331777-75-3

• 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: tert-butyl 3-azido-4-oxopiperidine-1-carboxylate
• 英文别名: 3-Azido-4-oxo-piperidine-1-carboxylic acid tert-butyl ester
• CAS: 1331777-75-3
• 化学式: C₁₀H₁₆N₄O₃
• 分子量: 240.262
• InChiKey: LHHTYHPVISXCIG-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.8
• 重原子数：
  17
• 可旋转键数：
  3
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.8
• 拓扑面积：
  61
• 氢给体数：
  0
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  tert-butyl 3-azido-4-oxopiperidine-1-carboxylate 在 二乙胺基三氟化硫 作用下， 以 1,2-二氯乙烷 为溶剂， 反应 16.0h， 以55%的产率得到tert-butyl 3-azido-4,4-difluoropiperidine-1-carboxylate
  参考文献：
  名称：

  EP3192791

  摘要：

  公开号：
• 作为产物：
  描述：

  N-BOC-1,2,3,6-四氢吡啶 在 sodium azide 、 戴斯-马丁氧化剂 、 间氯过氧苯甲酸 作用下， 以 二氯甲烷 、 水 、 丙酮 为溶剂， 反应 48.0h， 生成 tert-butyl 3-azido-4-oxopiperidine-1-carboxylate
  参考文献：
  名称：

  EP3192791

  摘要：

  公开号：

文献信息

• [EN] PHENYL-HETEROARYL DERIVATIVES AND METHODS OF USE THEREOF<br/>[FR] DÉRIVÉS DE PHÉNYL-HÉTÉROARYLE ET PROCÉDÉS D'UTILISATION DE CEUX-CI
  申请人：TRANSTECH PHARMA INC

  公开号：WO2011103091A1

  公开（公告）日：2011-08-25

  The present invention provides phenyl-heteroaryl derivatives of Formula (I) and pharmaceutically acceptable salts thereof. These compounds are useful in the treatment of RAGE-mediated diseases such as Alzheimer's Disease. The present invention further relates to methods for the preparation of compounds of Formula (I) and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising such compounds, and the use of such compounds and/or pharmaceutical compositions in treating RAGE-mediated diseases.

  本发明提供了式（I）的苯基-杂环芳基衍生物及其药学上可接受的盐。这些化合物在治疗RAGE介导的疾病，如阿尔茨海默病方面是有用的。本发明还涉及制备式（I）化合物及其药学上可接受的盐的方法，包括含有这些化合物的药物组合物，以及在治疗RAGE介导的疾病中使用这些化合物和/或药物组合物的用途。
• PHENYL-HETEROARYL DERIVATIVES AND METHODS OF USE THEREOF
  申请人：Gohimukkula Devi R.

  公开号：US20110230458A1

  公开（公告）日：2011-09-22

  The present invention provides phenyl-heteroaryl derivatives of Formula (I) and pharmaceutically acceptable salts thereof These compounds are useful in the treatment of RAGE-mediated diseases such as Alzheimer's Disease. The present invention further relates to methods for the preparation of compounds of Formula (I) and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising such compounds, and the use of such compounds and/or pharmaceutical compositions in treating RAGE-mediated diseases.

  本发明提供了式（I）的苯基-杂环取代衍生物及其药学上可接受的盐。这些化合物在治疗RAGE介导的疾病，如阿尔茨海默病中是有用的。本发明还涉及制备式（I）化合物及其药学上可接受的盐的方法，包括这些化合物的制药组合物，以及在治疗RAGE介导的疾病时使用这些化合物和/或制药组合物。
• Phenyl-heteroaryl derivatives and methods of use thereof
  申请人：TransTech Pharma, LLC

  公开号：US09045461B2

  公开（公告）日：2015-06-02

  The present invention provides phenyl-heteroaryl derivatives of Formula (I) and pharmaceutically acceptable salts thereof These compounds are useful in the treatment of RAGE-mediated diseases. The present invention further relates to methods for the preparation of compounds of Formula (I) and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising such compounds, and the use of such compounds and/or pharmaceutical compositions in treating RAGE-mediated diseases.

  本发明提供了式（I）的苯基杂环衍生物及其药学上可接受的盐。这些化合物在治疗RAGE介导的疾病方面是有用的。本发明还涉及制备式（I）化合物及其药学上可接受的盐的方法，包括这些化合物的制药组合物以及在治疗RAGE介导的疾病方面使用这些化合物和/或制药组合物的用途。
• Phenyl-Heteroaryl Derivatives and Methods of Use Thereof
  申请人：TransTech Pharma, Inc.

  公开号：US20130197007A1

  公开（公告）日：2013-08-01

  The present invention provides phenyl-heteroaryl derivatives of Formula (I) and pharmaceutically acceptable salts thereof These compounds are useful in the treatment of RAGE-mediated diseases such as Alzheimer's Disease. The present invention further relates to methods for the preparation of compounds of Formula (I) and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising such compounds, and the use of such compounds and/or pharmaceutical compositions in treating RAGE-mediated diseases.

  本发明提供了式（I）的苯基-杂环芳基衍生物及其药学上可接受的盐。这些化合物可用于治疗RAGE介导的疾病，如阿尔茨海默病。本发明还涉及制备式（I）的化合物及其药学上可接受的盐的方法，包括这种化合物的制药组合物，以及使用这种化合物和/或制药组合物治疗RAGE介导的疾病。
• HETEROCYCLIC COMPOUND
  申请人：Takeda Pharmaceutical Company Limited

  公开号：EP3192791A1

  公开（公告）日：2017-07-19

  The problem of the present invention is to provide a compound having a superior RORγt inhibitory action, and useful as a prophylactic or therapeutic agent for psoriasis, inflammatory bowel disease, ulcerative colitis, Crohn's disease, rheumatoid arthritis, multiple sclerosis, uveitis, asthma, ankylopoietic spondylarthritis, systemic lupus erythematosus, chronic obstructive pulmonary disease or the like. The present invention relates to a compound represented by the formula (I): [wherein each symbol is as described in the DESCRIPTION] or a salt thereof, which has an RORγt inhibitory action, and useful as a prophylactic or therapeutic agent for psoriasis, inflammatory bowel disease, ulcerative colitis, Crohn's disease, rheumatoid arthritis, multiple sclerosis, uveitis, asthma, ankylopoietic spondylarthritis, systemic lupus erythematosus, chronic obstructive pulmonary disease or the like.

  本发明的问题在于提供一种化合物，该化合物具有优异的 RORγt 抑制作用，可用作牛皮癣、炎症性肠病、溃疡性结肠炎、克罗恩病、类风湿性关节炎、多发性硬化症、葡萄膜炎、哮喘、强直性脊柱关节炎、系统性红斑狼疮、慢性阻塞性肺病或类似疾病的预防或治疗药物。本发明涉及一种由式（I）代表的化合物： [其中各符号如说明书所述]或其盐，具有 RORγt 抑制作用，可作为银屑病、炎症性肠病、溃疡性结肠炎、克罗恩病、类风湿性关节炎、多发性硬化症、葡萄膜炎、哮喘、强直性脊柱关节炎、系统性红斑狼疮、慢性阻塞性肺病或类似疾病的预防或治疗剂。