MALONATE SALT OF VARLITINIB

• Main Author: MOORE ROBERT
• Format: Patent
• Language: Chinese; English
• Published: 15.06.2021
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

The present disclosure relates to a pharmaceutically acceptable salt of compounds (I), i.e. varlitinib, a method of producing the salt, a purer form of the free base obtainable from the salt, and a pharmaceutical composition comprising any one of the same. Also provided is a salt, free base or composition thereof for use in treatment, in particular the treatment of cancer, including as part of a combination therapy, for example in combination with a chemotherapeutic agent. The disclosure also extends to compositions comprising the same and use of any one of the same in treatment, in particular treatment of cancer. 本公开涉及一种式(I)化合物，即瓦利替尼，的药学上可接受的盐、产生所述盐的方法、可从所述盐获得的较纯形式的游离碱以及包括所述盐和所述游离碱中的任一种的药物组合物。还提供了其盐、游离碱或组合物，所述盐、游离碱或组合物用于治疗，具体地癌症治疗，包含作为组合疗法的一部分，例如与化学治疗剂组合。本公开还扩展到包括以上物质的组合物以及以上物质中的任一种在治疗，具体地癌症治疗中的用途。