NOVEL PHARMACEUTICAL SALTS AND POLYMORPHIC FORMS OF AN ERBB AND BTK INHIBITOR

• Main Authors: TSUI, Honchung, ZENG, Qingbei, ZHENG, Jun-Cheng, CHANG, Shih-Ying, JIANG, Jianan, ZHANG, Xiaolin, YANG, Zhenfan, GUO, Qinghai
• Format: Patent
• Language: English; French
• Published: 09.02.2023
• 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

Disclosed are novel pharmaceutical salts and polymorphic forms of (R) -N- (5- ( (4- ( (5-chloro-4-fluoro-2- (2-hydroxypropan-2-yl) phenyl) amino) pyrimidin-2-yl) amino) -2- (3- (dimethylamino) pyrrolidin-1-yl) -4-methoxyphenyl) acrylamide (Compound I) that has inhibitory activities against ErbBs (e.g. EGFR or Her2) and/or BTK, especially mutant forms of ErbBs, and/or BTK. Further disclosed herein are the processes for the preparation of pharmaceutical salts and polymorphic forms of Compound I, and uses of such pharmaceutical salts and polymorphic forms of Compound I in inhibiting the ErbB or BTK. L'invention concerne de nouveaux sels pharmaceutiques et des formes polymorphes de (R) -N- (5- ( (4- ( (5-chloro-4-fluoro-2- (2-hydroxypropan-2-yl) phényl) amino) pyrimidin-2-yl) amino) -2- (3- (diméthylamino) pyrrolidin-1-yl) -4-méthoxyphényl) acrylamide (composé I) qui a des activités inhibitrices contre ErbB (par exemple EGFR ou Her2) et/ou BTK, en particulier des formes mutantes de ErbB et/ou BTK. L'invention concerne en outre les procédés de préparation de sels pharmaceutiques et de formes polymorphes du composé I, et des utilisations de ces sels pharmaceutiques et formes polymorphes du composé I dans l'inhibition de ErbB ou de BTK.