filgotinib maleate | 1802998-75-9

• 物质功能分类: 医药中间体 - 原料药中间体
• 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
• 英文名称: filgotinib maleate
• 英文别名: (Z)-but-2-enedioic acid;N-[5-[4-[(1,1-dioxo-1,4-thiazinan-4-yl)methyl]phenyl]-[1,2,4]triazolo[1,5-a]pyridin-2-yl]cyclopropanecarboxamide
• CAS: 1802998-75-9
• 化学式: C₄H₄O₄*C₂₁H₂₃N₅O₃S
• 分子量: 541.585
• InChiKey: BFENHEAPFWQJFL-BTJKTKAUSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.69
• 重原子数：
  38
• 可旋转键数：
  7
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.32
• 拓扑面积：
  180
• 氢给体数：
  3
• 氢受体数：
  10

反应信息

• 作为产物：
  描述：

  非戈替尼 、 顺丁烯二酸 以 甲醇 、 二氯甲烷 为溶剂， 反应 1.0h， 生成 filgotinib maleate
  参考文献：
  名称：

  [EN] CRYSTALLINE FILGOTINIB SULFONIC ACID ADDITION SALTS
  [FR] SELS D'ADDITION D'ACIDE SULFONIQUE DE FILGOTINIB CRISTALLIN

  摘要：

  本发明涉及菲洛替尼磺酸加盐物、它们的多晶型、制备方法以及包含它们的药物组合物。

  公开号：

  WO2017012771A1

文献信息

• [EN] PHARMACEUTICAL COMPOSITIONS COMPRISING A JAK INHIBITOR<br/>[FR] COMPOSITIONS PHARMACEUTIQUES COMPRENANT UN INHIBITEUR DE JAK
  申请人：GILEAD SCIENCES INC

  公开号：WO2018169875A1

  公开（公告）日：2018-09-20

  Pharmaceutical compositions comprising filgotinib maleate Form I and uses thereof are described herein.

  本文描述了包含Filgotinib Maleate Form I的制药组合物及其用途。
• [EN] SOLID FORMS OF FILGOTINIB MALEATE AND PROCESSES THEREOF<br/>[FR] FORMES SOLIDES DE MALÉATE DE FILGOTINIB ET PROCÉDÉS ASSOCIÉS
  申请人：DR REDDYS LABORATORIES LTD

  公开号：WO2021044327A1

  公开（公告）日：2021-03-11

  Aspects of the present application relate to solid forms of Filgotinib maleate and pharmaceutical compositions thereof. Specific aspects of the present application relate to crystalline forms FM1, FM2 and FM3 of Filgotinib maleate characterized by X-ray diffraction patterns. Further aspect of the present application related to processes for the preparation of said crystalline forms of Filgotinib maleate.

  本申请的方面涉及Filgotinib maleate的固态形式及其制药组合物。本申请的具体方面涉及Filgotinib maleate的晶体形式FM1、FM2和FM3，其具有X射线衍射图案特征。本申请的另一个方面涉及制备所述Filgotinib maleate晶体形式的方法。
• NOVEL COMPOUND USEFUL FOR THE TREATMENT OF DEGENERATIVE AND INFLAMMATORY DISEASES
  申请人：Menet Christel Jeanne Marie

  公开号：US20120142678A1

  公开（公告）日：2012-06-07

  A novel compound able to inhibit JAK is disclosed, this compound may be prepared as a pharmaceutical composition, 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, inflammatory conditions, autoimmune diseases, proliferative diseases, transplantation rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6.

  本发明揭示了一种能够抑制JAK的新化合物，该化合物可以制备为药物组合物，并可用于哺乳动物包括人类的多种疾病的预防和治疗，例如，炎症性疾病、自身免疫疾病、增殖性疾病、移植排斥、涉及软骨周转障碍的疾病、先天性软骨畸形以及与IL6过度分泌相关的疾病，仅为举例。
• AMINOTRIAZOLOPYRIDINE FOR USE IN THE TREATMENT OF INFLAMMATION, AND PHARMACEUTICAL COMPOSITIONS THEREOF
  申请人：van 't Klooster Gerben Albert Eleutherius

  公开号：US20130345209A1

  公开（公告）日：2013-12-26

  The present invention relates to the compound according to Formula I, and to its use in medicine, in particular in the treatment of inflammatory conditions, autoimmune diseases, proliferative diseases, allergy, transplant rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6 or interferons. In particular, the compound inhibits JAK a family of tyrosine kinases, and more particularly JAK1. The present invention also provides pharmaceutical compositions comprising the compound, methods for the prophylaxis and/or treatment of diseases involving inflammatory conditions, autoimmune diseases, proliferative diseases, allergy, transplant rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6 or interferons by administering the compound.

  本发明涉及公式I所示的化合物及其在医学上的应用，特别是在治疗炎症状况、自身免疫性疾病、增殖性疾病、过敏、移植排斥、涉及软骨周转障碍的疾病、先天性软骨畸形和/或与IL6或干扰素过度分泌相关的疾病中的应用。特别地，该化合物抑制酪氨酸激酶家族JAK，更具体地抑制JAK1。本发明还提供了包含该化合物的药物组合物，通过给予该化合物进行预防和/或治疗涉及炎症状况、自身免疫性疾病、增殖性疾病、过敏、移植排斥、涉及软骨周转障碍的疾病、先天性软骨畸形和/或与IL6或干扰素过度分泌相关的疾病的方法。
• PHARMACEUTICAL COMPOSITIONS COMPRISING A JAK INHIBITOR
  申请人：Gilead Sciences, Inc

  公开号：US20180263997A1

  公开（公告）日：2018-09-20

  Pharmaceutical compositions comprising filgotinib maleate Form I and uses thereof are described herein.