(6-氯-2-甲氧基-嘧啶-4-基)-[2-(2,4-二氯-苯基)-乙基]-胺 | 1016644-41-9

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 中文名称: (6-氯-2-甲氧基-嘧啶-4-基)-[2-(2,4-二氯-苯基)-乙基]-胺
• 英文名称: (6-chloro-2-methoxy-pyrimidin-4-yl)-[2-(2,4-dichloro-phenyl)-ethyl]-amine
• 英文别名: 6-chloro-N-[2-(2,4-dichlorophenyl)ethyl]-2-methoxypyrimidin-4-amine
• CAS: 1016644-41-9
• 化学式: C₁₃H₁₂Cl₃N₃O
• 分子量: 332.617
• InChiKey: WNAHJCXIYGECCP-UHFFFAOYSA-N

物化性质

• 沸点：
  513.6±60.0 °C(Predicted)
• 密度：
  1.431±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  5
• 重原子数：
  20
• 可旋转键数：
  5
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.23
• 拓扑面积：
  47
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  (6-氯-2-甲氧基-嘧啶-4-基)-[2-(2,4-二氯-苯基)-乙基]-胺 在 4-二甲氨基吡啶 、 potassium carbonate 、 盐酸-N-乙基-Nˊ-(3-二甲氨基丙基)碳二亚胺 作用下， 以 N-甲基吡咯烷酮 、 二氯甲烷 为溶剂， 反应 5.0h， 生成 N-(1-(6-(2-(2,4-dichlorophenyl)ethylamino)-2-methoxy-pyrimidin-4-yl)piperidin-3-carbonyl)-methanesulfonamide
  参考文献：
  名称：

  WO2007/121280

  摘要：

  公开号：
• 作为产物：
  描述：

  2,4-二氯苯酚呋喃 、 4,6-二氯-2-甲氧基嘧啶 在 碳酸氢钠 作用下， 以 乙醇 为溶剂， 反应 3.0h， 生成 (6-氯-2-甲氧基-嘧啶-4-基)-[2-(2,4-二氯-苯基)-乙基]-胺
  参考文献：
  名称：

  DIHYDROGEN PHOSPHATE SALT OF A PROSTAGLANDIN D2 RECEPTOR ANTAGONIST

  摘要：

  本发明涉及公式（III）的二氢磷酸盐2-（3-{6-[2-（2,4-二氯苯基）-乙基氨基]-2-甲氧基嘧啶-4-基}-苯基）-2-甲基丙酸，以及包含该化合物的药物组合物，其中药物组合物包含药学上有效量的化合物（III）和药学上可接受的载体；以及通过向患有PGD2介导的疾病的患者（包括但不限于过敏性疾病（如过敏性鼻炎，过敏性结膜炎，特应性皮炎，支气管哮喘和食物过敏），全身性肥大细胞增多症，伴随全身性肥大细胞激活的疾病，过敏性休克，支气管痉挛，支气管炎，荨麻疹，湿疹，伴随瘙痒的疾病（如特应性皮炎和荨麻疹），由于瘙痒行为（如抓挠和敲打）而次生产生的疾病（如白内障，视网膜脱离，炎症，感染和睡眠障碍），炎症，慢性阻塞性肺疾病，缺血再灌注损伤，脑血管意外，慢性类风湿性关节炎，胸膜炎，溃疡性结肠炎等）中，向该患者投予药学上有效量的化合物（III）的方法。

  公开号：

  US20080194600A1

文献信息

• 2,6-SUBSTITUTED-4-MONOSUBSTITUTEDAMINO-PYRIMIDINE AS PROSTAGLANDIN D2 RECEPTOR ANTAGONISTS
  申请人：Lim Sungtaek

  公开号：US20070244131A1

  公开（公告）日：2007-10-18

  The present invention is directed to a compound of Formula (I) wherein Cy 1 , Cy 2 , L 1 , L 2 , and R 1 are as defined herein, a pharmaceutical composition comprising a pharmaceutically effective amount of one or more compounds according to Formula (I) in admixture with a pharmaceutically acceptable carrier, and a method of treating a patient suffering from a PGD2-mediated disorder including, but not limited to, allergic disease (such as allergic rhinitis, allergic conjunctivitis, atopic dermatitis, bronchial asthma and food allergy), systemic mastocytosis, disorders accompanied by systemic mast cell activation, anaphylaxis shock, bronchoconstriction, bronchitis, urticaria, eczema, diseases accompanied by itch (such as atopic dermatitis and urticaria), diseases (such as cataract, retinal detachment, inflammation, infection and sleeping disorders) which is generated secondarily as a result of behavior accompanied by itch (such as scratching and beating), inflammation, chronic obstructive pulmonary diseases, ischemic reperfusion injury, cerebrovascular accident, chronic rheumatoid arthritis, pleurisy, ulcerative colitis and the like by administering to said patient a pharmaceutically effective amount of a compound according to Formula (I).

  本发明涉及一种式（I）的化合物，其中Cy1，Cy2，L1，L2和R1如本文所定义，一种制药组合物，包括一种或多种按照式（I）的化合物的药物有效量与药学可接受载体的混合物，以及一种治疗患有PGD2介导的疾病的患者的方法，包括但不限于过敏性疾病（如过敏性鼻炎，过敏性结膜炎，特应性皮炎，支气管哮喘和食物过敏），全身性肥大细胞病，伴随全身性肥大细胞激活的疾病，过敏性休克，支气管收缩，支气管炎，荨麻疹，湿疹，伴随瘙痒的疾病（如特应性皮炎和荨麻疹），疾病（如白内障，视网膜脱落，炎症，感染和睡眠障碍），这些疾病是由于伴随瘙痒的行为（如搔抓和敲打）而次生产生的，炎症，慢性阻塞性肺疾病，缺血再灌注损伤，脑血管意外，慢性类风湿性关节炎，胸膜炎，溃疡性结肠炎等，通过向该患者注射按照式（I）的化合物的药物有效量。
• 2,6-SUBSTITUTED-4-MONOSUBSTITUTED AMINO-PYRIMIDINE AS PROSTAGLANDIN D2 RECEPTOR ANTAGONISTS
  申请人：STEFANY David

  公开号：US20090036469A1

  公开（公告）日：2009-02-05

  The present invention is directed to a compound of formula (I), wherein R 1 and R 2 are as defined herein, a pharmaceutical composition comprising a pharmaceutically effective amount of one or more compounds of the invention in admixture with a pharmaceutically acceptable carrier, and a method of treating a patient suffering from a PGD2-mediated disorder by administering to said patient a pharmaceutically effective amount of a compound of the invention.

  本发明涉及一种式（I）的化合物，其中R1和R2如本文所定义，以及一种制药组合物，该组合物包含一种或多种本发明化合物的药效量与药物可接受载体混合，并通过向患有PGD2介导的疾病的患者投与本发明化合物的药效量来治疗患者的方法。
• NEW PROCESS FOR PREPARING 2-(3--PHENYL)-2-METHYLPROPRIONIC ACID
  申请人：HANNA Reda G.

  公开号：US20100184979A1

  公开（公告）日：2010-07-22

  This invention is directed to a process for preparing 2-(3-6-[2-(2,4-dichloro-phenyl)-ethylamino]-2-methoxy-pyrimidin-4-yl}-phenyl)-2-methyl-propionic acid.

  本发明涉及一种制备2-(3-6-[2-(2,4-二氯苯基)-乙基氨基]-2-甲氧基嘧啶-4-基}-苯基)-2-甲基-丙酸的方法。
• 2,6-substituted-4-monosubstitutedamino-pyrimidine as prostaglandin D2 receptor antagonists
  申请人：Aventis Pharmaceuticals, Inc.

  公开号：US07517889B2

  公开（公告）日：2009-04-14

  The present invention is directed to a compound of Formula (I) wherein Cy1, Cy2, L1, L2, and R1 are as defined herein, a pharmaceutical composition comprising a pharmaceutically effective amount of one or more compounds according to Formula (I) in admixture with a pharmaceutically acceptable carrier, and a method of treating a patient suffering from a PGD2-mediated disorder including, but not limited to, allergic disease (such as allergic rhinitis, allergic conjunctivitis, atopic dermatitis, bronchial asthma and food allergy), systemic mastocytosis, disorders accompanied by systemic mast cell activation, anaphylaxis shock, bronchoconstriction, bronchitis, urticaria, eczema, diseases accompanied by itch (such as atopic dermatitis and urticaria), diseases (such as cataract, retinal detachment, inflammation, infection and sleeping disorders) which is generated secondarily as a result of behavior accompanied by itch (such as scratching and beating), inflammation, chronic obstructive pulmonary diseases, ischemic reperfusion injury, cerebrovascular accident, chronic rheumatoid arthritis, pleurisy, ulcerative colitis and the like by administering to said patient a pharmaceutically effective amount of a compound according to Formula (I).

  本发明涉及一种式(I)化合物，其中Cy1、Cy2、L1、L2和R1的定义如本文所述，一种制药组合物，包括一种或多种式(I)化合物的药物有效量与药物可接受载体混合，以及一种治疗患有PGD2介导的疾病的患者的方法，包括但不限于过敏疾病（如过敏性鼻炎、过敏性结膜炎、特应性皮炎、支气管哮喘和食物过敏）、全身肥大细胞病、伴随全身肥大细胞激活的疾病、过敏性休克、支气管收缩、支气管炎、荨麻疹、湿疹、伴随瘙痒的疾病（如特应性皮炎和荨麻疹）、由于瘙痒行为（如搔抓和打击）引起的疾病（如白内障、视网膜脱落、炎症、感染和睡眠障碍）、炎症、慢性阻塞性肺疾病、缺血再灌注损伤、脑血管意外、慢性类风湿性关节炎、胸膜炎、溃疡性结肠炎等，通过向该患者投予符合式(I)的化合物的药物有效量实施。
• Dihydrogen phosphate salt of a prostaglandin D2 receptor antagonist
  申请人：Aventis Pharmaceuticals Inc.

  公开号：US07642249B2

  公开（公告）日：2010-01-05

  The present invention is directed to dihydrogen phosphate salt 2-(3-6-[2-(2,4-dichloro-phenyl)-ethylamino]-2-methoxy-pyrimidin-4-yl}-phenyl)-2-methyl-propionic acid of Formula (III), a pharmaceutical composition comprising a pharmaceutically effective amount of the compound of Formula (III), and a pharmaceutically acceptable carrier; and a method of treating a patient suffering from a PGD2-mediated disorder including, but not limited to, allergic disease (such as allergic rhinitis, allergic conjunctivitis, atopic dermatitis, bronchial asthma and food allergy), systemic mastocytosis, disorders accompanied by systemic mast cell activation, anaphylaxis shock, bronchoconstriction, bronchitis, urticaria, eczema, diseases accompanied by itch (such as atopic dermatitis and urticaria), diseases (such as cataract, retinal detachment, inflammation, infection and sleeping disorders) which is generated secondarily as a result of behavior accompanied by itch (such as scratching and beating), inflammation, chronic obstructive pulmonary diseases, ischemic reperfusion injury, cerebrovascular accident, chronic rheumatoid arthritis, pleurisy, ulcerative colitis and the like, by administering to said patient a pharmaceutically effective amount of the compound of Formula (III).

  本发明涉及化合物式（III）的二氢磷酸盐2-（3-6-[2-（2,4-二氯苯基）-乙基氨基]-2-甲氧基嘧啶-4-基}-苯基）-2-甲基丙酸，以及包含该化合物的药物组合物，其中药物组合物包含药效学上有效量的化合物（III）和药学上可接受的载体；以及一种治疗患有PGD2介导的疾病的患者的方法，包括但不限于过敏性疾病（如过敏性鼻炎，过敏性结膜炎，特应性皮炎，支气管哮喘和食物过敏），全身性肥大细胞增多症，伴随全身性肥大细胞活化的疾病，过敏性休克，支气管收缩，支气管炎，荨麻疹，湿疹，伴随瘙痒的疾病（如特应性皮炎和荨麻疹），伴随瘙痒行为（如搔抓和敲打）而次生产生的炎症，慢性阻塞性肺疾病，缺血再灌注损伤，脑血管意外，慢性类风湿性关节炎，胸膜炎，溃疡性结肠炎等疾病，通过向该患者投予化合物（III）的药效学上有效量来实现。