SELECTIVE HISTAMINE H3 ANTAGONIST ACID ADDITION SALTS AND PROCESS FOR THE PREPARATION THEREOF

• Main Authors: MEISZTERICS ANIKO, SEBOK FERENC, DEMETER ADAM
• Format: Patent
• Language: Chinese; English
• Published: 07.01.2022
• 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 invention relates to physically and chemically stable salts of the selective histamine preceptor antagonist compound of l-[4-(4-{3-[(2R)-2-methyl-pyrrolidin-l-yl]-propoxy}-phenoxy)- piperidin-l-yl]-ethanone of formula (1) and/or polymorphs thereof and/or hydrates/solvates thereof, the process for the preparation thereof, pharmaceutical compositions comprising them, and for use in the treatment and/or prevention of conditions requiring the modulation of histamine H3 receptors (e.g. Alzheimer's disease, obesity, schizophrenia, miochardial ischaemia, migraine, autism spectrum disorder). 本发明涉及式(1)的1-[4-(4-{3-[(2R)-2-甲基-吡咯烷-1-基]-丙氧基}-苯氧基)-哌啶-1-基]-乙酮的选择性组胺H3受体拮抗剂化合物的物理和化学稳定的盐，和/或其多晶型物和/或其水合物/溶剂化物、其制备方法、包含它们的药物组合物以及用于治疗和/或预防需要调节组胺H3受体的病症(例如阿尔茨海默病、肥胖症、精神分裂症、心肌缺血、偏头痛、孤独症谱系障碍)。