(2S)-3-[[5-fluoro-2-(5-fluoro-1H-pyrrolo[2,3-b]pyridin-3-yl)pyrimidin-4-yl]amino]bicyclo[2.2.2]octane-2-carboxylic acid

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: (2S)-3-[[5-fluoro-2-(5-fluoro-1H-pyrrolo[2,3-b]pyridin-3-yl)pyrimidin-4-yl]amino]bicyclo[2.2.2]octane-2-carboxylic acid
• 化学式: C₂₀H₁₉F₂N₅O₂
• 分子量: 399.4
• InChiKey: JGPXDNKSIXAZEQ-ZSFXIKKESA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.8
• 重原子数：
  29
• 可旋转键数：
  4
• 环数：
  6.0
• sp3杂化的碳原子比例：
  0.4
• 拓扑面积：
  104
• 氢给体数：
  3
• 氢受体数：
  8

文献信息

• [EN] FORMULATIONS OF AZAINDOLE COMPOUNDS<br/>[FR] FORMULATIONS DE COMPOSÉS AZAINDOLES
  申请人：JANSSEN PHARMACEUTICALS INC

  公开号：WO2020256820A1

  公开（公告）日：2020-12-24

  The present invention relates to pharmaceutical compositions, each comprising a multitude of granules that make up an intragranular phase of the composition, wherein the granules are produced by fluid bed granulation and comprise a HCI salt of Compound (1) • xH20 wherein x is from 0 to 3 (pimodivir), and one or more excipients selected from a disintegrant, a binder, and a wetting agent. The pharmaceutical composition also comprises one or more excipients that make up an extragranular phase of the composition, selected from a diluent, a disintegrant, a glidant, and a lubricant. The invention also relates to processes for producing the pharmaceutical compositions of the invention. The invention further relates to uses and methods of the pharmaceutical compositions in reducing the amount of influenza viruses in a biolog ica l/n v/trosample or in a subject, inhibiting the replication of influenza viruses in a biolog icalin vitrosample or in a subject, and treating influenza in a subject.

  本发明涉及制药组合物，每种组合物包括构成组合物的多个颗粒，其中颗粒由流化床造粒生产，并包括化合物（1）的HCl盐•xH20，其中x为0至3（pimodivir），以及从可分散剂、粘合剂和润湿剂中选择的一个或多个赋形剂。制药组合物还包括构成组合物的外颗粒相的一个或多个赋形剂，从稀释剂、可分散剂、滑动剂和润滑剂中选择。该发明还涉及制备本发明的制药组合物的方法。此外，本发明涉及在生物体外/体内样本或受试者中减少流感病毒数量、抑制生物体外/体内样本或受试者中流感病毒的复制，以及治疗受试者流感的制药组合物的用途和方法。
• INHIBITORS OF INFLUENZA VIRUSES REPLICATION
  申请人：Vertex Pharmaceuticals Incorporated

  公开号：US20140142119A1

  公开（公告）日：2014-05-22

  Methods of inhibiting the replication of influenza viruses in a biological sample or patient, of reducing the amount of influenza viruses in a biological sample or patient, and of treating influenza in a patient, comprises administering to said biological sample or patient an effective amount of a compound represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof, wherein the values of Structural Formula (IA) are as described herein. A compound is represented by Structural Formula (IA) or a pharmaceutically acceptable salt thereof, wherein the values of Structural Formula (IA) are as described herein. A pharmaceutical composition comprises an effective amount of such a compound or pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, adjuvant or vehicle.

  抑制生物样品或患者中流感病毒复制的方法，减少生物样品或患者中流感病毒的数量，以及治疗患者的流感的方法，包括向所述生物样品或患者投予有效量的由结构式（I）表示的化合物或其药学上可接受的盐，其中结构式（IA）的值如此处所述。所述化合物由结构式（IA）或其药学上可接受的盐表示，其中结构式（IA）的值如此处所述。药物组合物包括有效量的此类化合物或其药学上可接受的盐，以及药学上可接受的载体、佐剂或载体。
• Treatment of cerebral cavernous malformations and cerebral aneurysms with rho kinase inhibitors
  申请人：BioAxone BioSciences, Inc.

  公开号：US10857157B2

  公开（公告）日：2020-12-08

  Provided are methods of treating a cerebral cavernous malformation (CCM) and methods of treating cerebral aneurysm in a mammal with certain rho kinase inhibitors.

  本文提供了用某些 rho 激酶抑制剂治疗脑海绵畸形（CCM）的方法和治疗哺乳动物脑动脉瘤的方法。
• COMBINATION THERAPIES FOR TREATING INFLUENZA VIRUS INFECTION
  申请人：Vertex Pharmaceuticals Incorporated

  公开号：US20200054633A1

  公开（公告）日：2020-02-20

  The present invention relates to mono and combination therapies that are useful for inhibiting influenza virus replication, treating or reducing the severity of influenza infections in patients, and prophylactically preventing or reducing the incidence of influenza infections in patients. The combinations described herein include a compound having the structure
• TREATING INFLUENZA USING SUBSTITUTED POLYCYCLIC PYRIDONE DERIVATIVES AND PRODRUGS THEREOF IN A SUBJECT HAVING INFLUENZA AND A COMPLICATION RISK FACTOR
  申请人：Shionogi & Co., Ltd.

  公开号：US20200289522A1

  公开（公告）日：2020-09-17

  A method for treating an influenza virus infection is described. The disclosed method generally involves administering an effective amount of a compound, for example baloxavir marboxil, to a subject having an influenza virus infection and at least one complication risk factor. Generally, the amount is effective such that a reduction in a time to improvement of at leat one symptom of an influenza virus infection is statistically significant as compared to that of a non-treated subject.