[9,10-DIMETHOXY-3-(2-METHYLPROPYL)-1H,2H,3H,4H,6H,7H,11BH-PYRIDO-[2,1-A]ISOQUINOLIN-2-YL]METHANOL AND COMPOUNDS, COMPOSITIONS AND METHODS RELATING THERETO

• Main Authors: ASHWEEK NEIL, HARRIOTT NICOLE
• Format: Patent
• Language: Chinese; English
• Published: 05.12.2017
• 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

Compounds having a structure of formula (I), including stereoisomers and pharmaceutically acceptable salts and solvates thereof: wherein R1 is as defined herein. Such compounds are inhibitors of the vesicular monoamine transporter 2 (VMAT2) and have utility for treating, for example, hyperkinetic disorders. Also disclosed are compositions containing these compounds in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use in a subject in need thereof. 具有式(I)结构的化合物，包括其立体异构体以及药物可接受的盐和溶剂化物：其中R如本文定义。这类化合物是囊泡单胺转运体2(VMAT2)的抑制剂，并且具有治疗例如运动机能亢进性病症的效用。还公开了含有这些化合物结合药物可接受的载体的组合物，以及涉及对有需要的个体使用的方法。