4-氨基-3-甲氧基-2-甲基吡啶 | 1559064-12-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡啶及其衍生物
• 中文名称: 4-氨基-3-甲氧基-2-甲基吡啶
• 英文名称: 3-methoxy-2-methylpyridin-4-amine
• 英文别名: 3-Methoxy-2-methyl-4-pyridinamine
• CAS: 1559064-12-8
• 化学式: C₇H₁₀N₂O
• mdl: MFCD22397888
• 分子量: 138.169
• InChiKey: BJQUFRZNXLGEGF-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.5
• 重原子数：
  10
• 可旋转键数：
  1
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.29
• 拓扑面积：
  48.1
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  二碳酸二叔丁酯 、 4-氨基-3-甲氧基-2-甲基吡啶 在 N,N-二异丙基乙胺 作用下， 以 四氢呋喃 为溶剂， 生成 tert-butyl N-(3-methoxy-2-methyl-4-pyridyl)carbamate
  参考文献：
  名称：

  [EN] NOVEL COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS THEREOF FOR THE TREATMENT OF INFLAMMATORY DISORDERS
  [FR] NOUVEAUX COMPOSÉS ET COMPOSITIONS PHARMACEUTIQUES DE CEUX-CI POUR LE TRAITEMENT DE TROUBLES INFLAMMATOIRES

  摘要：

  本发明公开了化合物的公式(I)：(I)。其中R1、R2、R5和Cy的定义如本文所述。本发明涉及化合物、制备该化合物的方法、包含该化合物的药物组合物以及通过给予该化合物进行预防和/或治疗炎症性疾病、自身免疫性疾病、疼痛、纤维化和/或增殖性疾病的方法。

  公开号：

  WO2020200900A1

文献信息

• [EN] PYRAZOLO[1,5-D][1,2,4]TRIAZINE-5(4H)-ACETAMIDES AS INHIBITORS OF THE NLRP3 INFLAMMASOME PATHWAY<br/>[FR] PYRAZOLO[1,5-D][1,2,4]TRIAZINE-5(4H)-ACÉTAMIDES UTILISÉS COMME INHIBITEURS DE LA VOIE DE L'INFLAMMASOME NLRP3
  申请人：JANSSEN PHARMACEUTICA NV

  公开号：WO2021209552A1

  公开（公告）日：2021-10-21

  The invention relates to novel compounds for use as inhibitors of NLRP3 inflammasone production, wherein such compounds are as defined by compounds of formula (I) and wherein the integers R1, R2 and R3 are defined in the description, and where the compounds may be useful as medicaments, for instance for use in the treatment of a disease or disorder that is associated with NLRP3 inflammasome activity.

  这项发明涉及用作NLRP3炎症小体产生抑制剂的新化合物，其中这些化合物由式(I)的化合物定义，并且整数R1、R2和R3在描述中有定义，这些化合物可能作为药物有用，例如用于治疗与NLRP3炎症小体活性相关的疾病或紊乱。
• [EN] MITOCHONDRIAL INHIBITORS FOR THE TREATMENT OF PROLIFERATION DISORDERS<br/>[FR] INHIBITEURS MITOCHONDRIALES POUR LE TRAITEMENT DE TROUBLES PROLIFÉRATIFS
  申请人：BASILEA PHARM INT AG

  公开号：WO2019115709A1

  公开（公告）日：2019-06-20

  The invention provides compounds of formula I or pharmaceutically acceptable salt thereof wherein Bl, B2, B3 and B4 represent independently C(R3); X represents -CH(R5)-, -C(R5)= or -(C=0)-, and wherein when X represents -CH(R5)- or -(C=0)- the dotted line represents a single bond, and when X represents -C(R5)= the dotted line represents a double bond; R1 represents independently at each occurrence methy, ethyl, methoxy or ethoxy; R2 represents halogen, cyano, hydroxyl, methyl, ethyl, methoxy, ethoxy, -N(R6a)(R6b) or -methylene- N(R6a)(R6b); R3 represents independently at each occurrence hydrogen, halogen, cyano or methyl; R4a represents methyl or ethyl; R4b represents halogen, Cl-C4alkyl, Cl-C4alkoxy or -0-Cl-C4alkylene-Cycle-Q; R5 represents hydrogen or methyl; R6a represents hydrogen or methyl; R6b represents hydrogen or methyl; Cycle-Q represents independently at each occurrence phenyl optionally substituted by 1 to 3 R7; R7 represents independently at each occurrence cyano, methyl, halomethyl, methoxy or halomethoxy; n is 1 or 2; and q is 0, 1 or 2; as well as methods of using the compounds to treat proliferation diseases, in particular cancer.

  该发明提供了公式I的化合物或其药用可接受的盐，其中Bl、B2、B3和B4分别独立地代表C（R3）；X代表-CH（R5）-、-C（R5）=或-(C=0)-，当X代表-CH（R5）-或-(C=0)-时，虚线代表单键，当X代表-C（R5）=时，虚线代表双键；R1在每次出现时独立地代表甲基、乙基、甲氧基或乙氧基；R2代表卤素、氰基、羟基、甲基、乙基、甲氧基、乙氧基、-N（R6a）（R6b）或-亚甲基-N（R6a）（R6b）；R3在每次出现时独立地代表氢、卤素、氰基或甲基；R4a代表甲基或乙基；R4b代表卤素、Cl-C4烷基、Cl-C4烷氧基或-0-Cl-C4烷基环-Q；R5代表氢或甲基；R6a代表氢或甲基；R6b代表氢或甲基；环-Q在每次出现时独立地代表苯环，可选择地被1至3个R7取代；R7在每次出现时独立地代表氰基、甲基、卤甲基、甲氧基或卤甲氧基；n为1或2；q为0、1或2；以及使用这些化合物治疗增殖性疾病，特别是癌症的方法。
• NOVEL COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS THEREOF FOR THE TREATMENT OF INFLAMMATORY DISORDERS
  申请人：Galapagos NV

  公开号：US20220218679A1

  公开（公告）日：2022-07-14

  The present invention discloses compounds according to Formula I: Wherein R 1 , R 2 , R 5 and Cy are as defined herein. The present invention relates to compounds, methods for the production of said compounds, pharmaceutical compositions comprising said compounds and methods for the prophylaxis and/or treatment of inflammatory diseases, autoimmune diseases, pain, fibrosis and/or proliferative diseases by administering said compounds.
• [EN] NOVEL COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS THEREOF FOR THE TREATMENT OF INFLAMMATORY DISORDERS<br/>[FR] NOUVEAUX COMPOSÉS ET COMPOSITIONS PHARMACEUTIQUES DE CEUX-CI POUR LE TRAITEMENT DE TROUBLES INFLAMMATOIRES
  申请人：GALAPAGOS NV

  公开号：WO2020200900A1

  公开（公告）日：2020-10-08

  The present invention discloses compounds according to Formula (I): (I). Wherein R1, R2, R5 and Cy are as defined herein. The present invention relates to compounds, methods for the production of said compounds, pharmaceutical compositions comprising said compounds and methods for the prophylaxis and/or treatment of inflammatory diseases, autoimmune diseases, pain, fibrosis and/or proliferative diseases by administering said compounds.

  本发明公开了化合物的公式(I)：(I)。其中R1、R2、R5和Cy的定义如本文所述。本发明涉及化合物、制备该化合物的方法、包含该化合物的药物组合物以及通过给予该化合物进行预防和/或治疗炎症性疾病、自身免疫性疾病、疼痛、纤维化和/或增殖性疾病的方法。