4-(ethylamino)pyrimidine

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪类
• 英文名称: 4-(ethylamino)pyrimidine
• 英文别名: N-ethylpyrimidin-4-amine
• 化学式: C₆H₉N₃
• 分子量: 123.158
• InChiKey: MFBQWSYPXVVOKF-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.9
• 重原子数：
  9
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.33
• 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：

  bis(2,4,6-trichlorophenyl) ethylmalonate 、 4-(ethylamino)pyrimidine 反应 0.07h， 以85%的产率得到anhydro-(1,3-diethyl-4-oxo-2-hydroxypyrimido[1,6-a]pyrimidinium hydroxide)
  参考文献：
  名称：

  初步研究中离子黄嘌呤类似物作为血小板聚集的抑制剂。

  摘要：

  研究了一系列中离子黄嘌呤（例如，中离子噻唑并嘧啶3，和噻二唑并嘧啶5）和相关类似物作为人类血小板聚集的抑制剂。发现适当取代的化合物可完全抑制血小板凝集，并形成脱水-（6-乙基-8-异戊基-7-氧代-5-羟基-1,3,4-噻二唑[3,2-a]氢氧化嘧啶鎓）（5b ）的效力是与结构相关的黄嘌呤茶碱（1）的4​​0倍。凝胶过滤研究表明，化合物5b不可逆地抑制聚集，这可能是由于其充当潜在的酰化剂的能力。

  DOI：

  10.1016/s0968-0896(00)00123-1

文献信息

• [EN] BENZODIAZEPINE BROMODOMAIN INHIBITOR<br/>[FR] INHIBITEUR DE BROMODOMAINES VIS-À-VIS DE LA BENZODIAZÉPINE
  申请人：GLAXOSMITHKLINE LLC

  公开号：WO2011054845A1

  公开（公告）日：2011-05-12

  Benzodiazepine compounds of formula (I), and salts thereof, pharmaceutical compositions containing such compounds and their use in therapy, in particular in the treatment of diseases or conditions for which a bromodomain inhibitor is indicated.

  苯二氮卓类化合物的化学式（I）及其盐，含有这类化合物的药物组合物以及它们在治疗中的应用，特别是在治疗溴结构域抑制剂适应症的疾病或症状。
• BIARYL AMIDE DERIVATIVE OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF
  申请人：Katayama Seiji

  公开号：US20130116227A1

  公开（公告）日：2013-05-09

  Disclosed is a novel biaryl amide derivative represented by formula (1) and having an affinity for the aldosterone receptor; also disclosed is a pharmaceutically acceptable salt thereof. (In the formula, A is any of the groups represented by formula (a); L is —CONH—, etc.; R 1 is a substitutable aminosulfonyl group, etc.; R 2 is a hydrogen atom, etc.; R 3 is a hydrogen atom, etc.; R 4 is a hydrogen atom, a halogen atom, hydroxy group, a substitutable amino group, a substitutable C 1-6 alkoxy group, a substitutable 4- to 7-membered cyclic amino group, etc.; R 5a , R 5b and R 5c are each independently hydrogen atoms, etc.; R 6 is a halogen atom, a cyano group, etc.; R 7 and R 8 are each independently a hydrogen atom, etc.; and m is an integer such as 0.)

  揭示了一种表示为公式（1）的新型联苯酰胺衍生物，具有与醛固酮受体的亲和力；还揭示了其药用可接受的盐。（在该公式中，A是由公式（a）表示的任何基团之一；L是—CONH—等；R1是可替代的氨基磺酰基等；R2是氢原子等；R3是氢原子等；R4是氢原子、卤原子、羟基、可替代的氨基基团、可替代的C1-6烷氧基、可替代的4-到7-成员环氨基基团等；R5a、R5b和R5c各自独立地是氢原子等；R6是卤原子、氰基等；R7和R8各自独立地是氢原子等；m是整数，例如0。）
• [EN] BICYCLIC ALKYNE DERIVATIVES AND USES THEREOF<br/>[FR] DÉRIVÉS D'ALCYNES BICYCLIQUES ET LEURS UTILISATIONS
  申请人：AGENCY SCIENCE TECH & RES

  公开号：WO2015050505A1

  公开（公告）日：2015-04-09

  The present invention relates to certain compounds (e.g., imidazopyrazine, imidazopyridine, imidazopyridazine and imidazpyrimidine compounds) that act as inhibitors of the MAP kinase interacting kinases MNK2a, MNK2b, MNK1a, and MNK1b. The present invention further relates to pharmaceutical compositions comprising these compounds, and to the use of the compounds for the prevention and treatment of diseases (e.g., proliferative diseases (e.g., cancer), inflammatory diseases, autoimmune diseases, metabolic diseases, and neurodegenerative diseases (e.g. autism, autism spectrum disorders, Alzheimer's disease)), as well as methods of treating these diseases

  本发明涉及某些化合物（例如，咪唑吡嗪、咪唑吡啶、咪唑吡嗪和咪唑嘧啶化合物），这些化合物作为MAP激酶相互作用激酶MNK2a、MNK2b、MNK1a和MNK1b的抑制剂。本发明还涉及包含这些化合物的药物组合物，以及利用这些化合物预防和治疗疾病（例如，增殖性疾病（例如癌症）、炎症性疾病、自身免疫性疾病、代谢性疾病和神经退行性疾病（例如自闭症、自闭症谱系障碍、阿尔茨海默病））的用途，以及治疗这些疾病的方法。
• [EN] COMBINATIONS COMPRISING HISTONE DEACETYLASE INHIBITORS<br/>[FR] ASSOCIATIONS COMPRENANT DES INHIBITEURS D'HISTONE DÉSACÉTYLASE
  申请人：KARUS THERAPEUTICS LTD

  公开号：WO2017208032A1

  公开（公告）日：2017-12-07

  The invention relates to a combination of a compound of formula (I) or a pharmaceutically acceptable salt thereof, and at least one second agent selected from the group consisting of proteasome inhibitors, tumour immunotherapeutics or immunomodulatory agents, signal transduction pathway inhibitors, agents inhibiting the BCL2 family of proteins, agents inhibiting Mcl-1, poly (ADP-ribose) polymerase (PARP) Inhibitors, aromatase inhibitors, conventional cytotoxic agents or a miscellaneous agent selected from abiraterone, ARN-509 and MYC inhibitors.

  该发明涉及公式(I)的化合物或其药用可接受的盐，以及来自蛋白酶体抑制剂、肿瘤免疫治疗剂或免疫调节剂、信号传导途径抑制剂、抑制BCL2蛋白家族的药剂、抑制Mcl-1的药剂、聚(ADP-核糖)聚合酶（PARP）抑制剂、芳香化酶抑制剂、传统细胞毒剂或从阿比特龙、ARN-509和MYC抑制剂中选择的其他药剂中至少一种第二药剂的组合。
• [EN] CARM1 INHIBITORS AND USES THEREOF<br/>[FR] INHIBITEURS DE CARM1 ET LEURS UTILISATIONS
  申请人：EPIZYME INC

  公开号：WO2014144169A1

  公开（公告）日：2014-09-18

  Provided herein are compounds of Formula (I) and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof; wherein X, R1, R1a, R2a, R2b, R2c, R2d, are as defined herein, and Ring HET is a 6-membered monocyclic heteroaryl ring system of Formula (II) wherein L2, R13, G8, G10, G11, and G12 are as defined herein. Compounds of the present invention are useful for inhibiting CARMl activity. Methods of using the compounds for treating CARM1 -mediated disorders are also described.

  本文提供了式（I）的化合物及其药用盐，以及药物组合物；其中X、R1、R1a、R2a、R2b、R2c、R2d如本文所定义，环HET是式（II）的6-成员单环杂环芳基环系统，其中L2、R13、G8、G10、G11和G12如本文所定义。本发明的化合物可用于抑制CARM1活性。还描述了使用这些化合物治疗CARM1介导的疾病的方法。