Salts and crystals

• Main Authors: REICH, THOMAS, LAWRENCE R MICHAEL, ALSOP HERVE
• Format: Patent
• Language: Chinese; English
• Published: 12.09.2023
• Subjects: ACYCLIC OR CARBOCYCLIC COMPOUNDS; 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 solid forms of 1-methyl-1, 4, 5, 10-tetrahydropyrazolo [3, 4-b] [1, 5] benzodiazepine free base having desirable pharmacokinetic properties, such as low hygroscopicity and improved thermal stability. These solid forms include crystalline forms of the 1-methyl-1, 4, 5, 10-tetrahydropyrazolo [3, 4-b] [1, 5] benzodiazepine 5 free base and the phosphate and L-tartrate of the 1-methyl-1, 4, 5, 10-tetrahydropyrazolo [3, 4-b] [1, 5] benzodiazepine free base. Pharmaceutical compositions, medicaments and kits comprising these solid forms are also described. Methods of using these forms to treat various diseases, disorders, and conditions are also provided. 本发明涉及1-甲基-1,4,5,10-四氢吡唑并[3,4-b][1,5]苯二氮卓游离碱的固体形式，其具有理想的药代动力学特性，例如低吸湿性和改进的热稳定性。这些固体形式包括1-甲基-1,4,5,10-四氢吡唑并[3,4-b][1,5]苯二氮卓5游离碱和1-甲基-1,4,5,10-四氢吡唑并[3,4-b][1,5]苯二氮卓游离碱的磷酸盐和L-酒石酸盐的结晶形式。还描述了包含这些固体形式的药物组合物、药物和试剂盒。还提供了使用这些形式治疗各种疾病、病症和病况的方法。