N-甲基-n-(4-嘧啶-5-基苄基)胺 | 859850-85-4

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪类
• 中文名称: N-甲基-n-(4-嘧啶-5-基苄基)胺
• 英文名称: N-methyl-N-(4-pyrimidin-5-ylbenzyl)amine
• 英文别名: N-methyl-1-(4-pyrimidin-5-ylphenyl)methanamine
• CAS: 859850-85-4
• 化学式: C₁₂H₁₃N₃
• 分子量: 199.25
• InChiKey: AKANTTBTKVSRKO-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.2
• 重原子数：
  15
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.17
• 拓扑面积：
  37.8
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  5-({[(4-methoxy-2,6-dimethylphenyl)sulfonyl](methyl)amino}methyl)furan-3-carboxylic acid 、 N,N'-羰基二咪唑 、 N-甲基-n-(4-嘧啶-5-基苄基)胺 在 crude product 作用下， 以 四氢呋喃 、 N,N-二甲基甲酰胺 为溶剂， 生成 5-({[(4-methoxy-2,6-dimethylphenyl)sulfonyl](methyl)amino}methyl)-N-methyl-N-(4-pyrimidin-5-ylbenzyl)furan-3-carboxamide
  参考文献：
  名称：

  BRADYKININ B1 ANTAGONISTS

  摘要：

  本发明涉及公式(I)的化合物，其中R1、R1a、R1b、R2、R3和X、X1、X2、X3的含义如描述和权利要求中所述。所述化合物可用作Bradykinin B1拮抗剂。本发明还涉及制药组合物，制备此类化合物以及作为药物的生产和使用。

  公开号：

  US20140073627A1

文献信息

• NOVEL COMPOUNDS USEFUL FOR THE TREATMENT OF DEGENERATIVE AND INFLAMMATORY DISEASES
  申请人：Menet Christel Jeanne Marie

  公开号：US20110190260A1

  公开（公告）日：2011-08-04

  [1,2,4]Triazolo[1,5-a]pyridine compounds are disclosed that have a formula represented by the formula (I). The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, diseases involving cartilage degradation, bone and/or joint degradation, for example osteoarthritis; and/or conditions involving inflammation or immune responses, such as Crohn's disease, rheumatoid arthritis, psoriasis, allergic airways disease (e.g. asthma, rhinitis), juvenile idiopathic arthritis, colitis, inflammatory bowel diseases, endotoxin-driven disease states (e.g. complications after bypass surgery or chronic endotoxin states contributing to e.g. chronic cardiac failure), diseases involving impairment of cartilage turnover (e.g diseases involving the anabolic stimulation of chondrocytes), congenital cartilage malformations, diseases associated with hypersecretion of IL6, transplantation rejection (e.g. organ transplant rejection) and proliferative diseases.

  本文披露了一种具有公式（I）所表示的化学式的[1,2,4]三唑并[1,5-a]吡啶化合物。这些化合物可以制备为药物组合物，并可用于预防和治疗哺乳动物（包括人类）的各种疾病，包括但不限于涉及软骨降解、骨骼和/或关节降解的疾病，例如骨关节炎；以及涉及炎症或免疫反应的疾病，如克隆病、类风湿性关节炎、牛皮癣、过敏性呼吸道疾病（例如哮喘、鼻炎）、少年特发性关节炎、结肠炎、炎性肠病、内毒素驱动的疾病状态（例如旁路手术后的并发症或慢性内毒素状态导致的慢性心力衰竭等）、涉及软骨周转障碍的疾病（例如涉及软骨细胞的合成刺激的疾病）、先天性软骨畸形、与IL6高分泌相关的疾病、移植排斥（例如器官移植排斥）和增生性疾病。
• NEW BRADYKININ B1 ANTAGONISTS
  申请人：Madden James

  公开号：US20110201589A1

  公开（公告）日：2011-08-18

  The invention relates to compounds of formula (I) wherein R 1 , R 1a , R 1b , R 2 , R 3 and X, X 1 , X 2 , X 3 have the meaning as cited in the description and the claims. Said compounds are useful as Bradykinin B1 antagonists. The invention also relates to pharmaceutical compositions, the preparation of such compounds as well as the production and use as medicament.

  本发明涉及式(I)的化合物，其中R1、R1a、R1b、R2、R3和X、X1、X2、X3的含义如描述和权利要求中所述。所述化合物可用作Bradykinin B1受体拮抗剂。本发明还涉及制备这种化合物的药物组合物，以及作为药物的生产和使用。
• Bradykinin B1 antagonists
  申请人：Madden James

  公开号：US08623859B2

  公开（公告）日：2014-01-07

  The invention relates to compounds of formula (I) wherein R1, R1a, R1b, R2, R3 and X, X1, X2, X3 have the meaning as cited in the description and the claims. Said compounds are useful as Bradykinin B1 antagonists. The invention also relates to pharmaceutical compositions, the preparation of such compounds as well as the production and use as medicament.

  该发明涉及式(I)化合物，其中R1、R1a、R1b、R2、R3和X、X1、X2、X3的含义如说明书和权利要求中所述。所述化合物可用作Bradykinin B1拮抗剂。该发明还涉及制备这些化合物的制药组合物，以及作为药物的生产和使用。
• Compounds useful for the treatment of degenerative and inflammatory diseases
  申请人：GALAPAGOS NV

  公开号：US10206907B2

  公开（公告）日：2019-02-19

  [1,2,4]triazolo[1,5-a]pyridine compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, diseases involving cartilage degradation, bone and/or joint degradation, for example osteoarthritis; and/or conditions involving inflammation or immune responses, such as Crohn's disease, rheumatoid arthritis, psoriasis, allergic airways disease (e.g. asthma, rhinitis), juvenile idiopathic arthritis, colitis, inflammatory bowel diseases, endotoxin-driven disease states (e.g. complications after bypass surgery or chronic endotoxin states contributing to e.g. chronic cardiac failure), diseases involving impairment of cartilage turnover (e.g. diseases involving the anabolic stimulation of chondrocytes), congenital cartilage malformations, diseases associated with hypersecretion of IL6 and transplantation rejection (e.g. organ transplant rejection) and proliferative diseases.

  所公开的[1,2,4]三唑并[1,5-a]吡啶化合物具有下式： 这些化合物可制备成药物组合物，并可用于预防和治疗包括人类在内的哺乳动物的各种疾病，包括非限制性实例，涉及软骨退化、骨和/或关节退化的疾病，例如骨关节炎；和/或涉及炎症或免疫反应的疾病，例如克罗恩病、类风湿性关节炎、银屑病、过敏性气道疾病（如哮喘、鼻炎、幼年特发性关节炎、荨麻疹等）。哮喘、鼻炎）、幼年特发性关节炎、结肠炎、肠道炎症性疾病、内毒素驱动的疾病状态（如搭桥手术后的并发症或导致慢性心力衰竭等的慢性内毒素状态）、涉及软骨代谢损伤的疾病（如涉及合成代谢疾病的疾病）、涉及骨质疏松症的疾病（如骨质疏松症）、涉及骨质疏松症的疾病（如骨质疏松症）、涉及骨质疏松症的疾病（如骨质疏松症）。先天性软骨畸形、与 IL6 分泌过多和移植排斥有关的疾病（如器官移植排斥）以及增殖性疾病。
• US8623859B2
  申请人：——

  公开号：US8623859B2

  公开（公告）日：2014-01-07