Gagliardi Stefania, Dondio Giulio, Giardina Giuseppe A M
NiKem Research Srl, Via Zambeletti 25, 20021 - Baranzate di Bollate, Milan, Italy.
IDrugs. 2003 Feb;6(2):129-37.
Alkaloids extracted from the Papaverum somniferum are among the most powerfully acting and clinically used drugs for diseases of the central nervous system, in particular for pain. The basic ring system, common to these opiate alkaloids, is the morphinan skeleton, which in the last 50 years has been chemically manipulated to obtain compounds with improved potency and increased selectivity toward different populations of opioid receptors. Despite a huge amount of research, interest surrounding these compounds is still high. This review will discuss the patent applications published from January 2001 to June 2002, focusing on new chemical entities that could become drugs over the next few years, new chemical processes for the production of the morphinans currently used in therapy, novel formulations and combined compositions.
从罂粟中提取的生物碱是作用最强且临床上用于治疗中枢神经系统疾病,尤其是疼痛的药物之一。这些阿片类生物碱共有的基本环系是吗啡喃骨架,在过去50年里,人们对其进行了化学处理,以获得效力更强、对不同阿片受体群体选择性更高的化合物。尽管进行了大量研究,但围绕这些化合物的关注度仍然很高。本综述将讨论2001年1月至2002年6月期间公布的专利申请,重点关注未来几年可能成为药物的新化学实体、目前用于治疗的吗啡喃类化合物的新生产工艺、新型制剂和复方组合物。