The present invention discloses (1) phenolic ester hybrids of niacin with m-methoxy-p-hydroxy phenyl compounds like eugenol, vanillin, apocynin, ferulic acid, isoferulic acid and eugenol epoxide and (2) cocrystals of hybrids as above, particularly cocrystal of niacin-eugenol hybrid with cocrystal former like eugenol and oxalic acid (3) novel pharmaceutical compositions comprising a combination of niacin and one or more small molecule/potentiating agent like eugenol, curcumin, cinnamic acid, meclofenamic acid, and their use in the treatment of a disorder or a disease caused by excess production of amyloid beta peptide-42 (Aβ42), its deposition, accumulation, and plaque formation including Alzheimer's Disease, dementia and mild cognitive impairment as well as other neurodegenerative diseases such as Parkinson's Disease and ischemic stroke.
本发明披露了(1)
烟酸与m-甲氧基-p-羟基苯基化合物(如
丁香酚、
香草醛、阿波替宁、
香豆酸、异
香豆酸和
丁香酚环氧化物)的
酚酯杂化物,以及(2)上述杂化物的共晶体,特别是
烟酸-
丁香酚杂化物与
丁香酚和
草酸等共晶体形成剂的共晶体;(3)新型药物组合物,包括
烟酸和一种或多种小分子/增效剂,如
丁香酚、
姜黄素、
肉桂酸、美克洛
酚酸,以及它们在治疗由淀粉样β肽42(Aβ42)过度产生、沉积、积累和斑块形成引起的疾病或紊乱,包括阿尔茨海默病、痴呆症和轻度认知障碍,以及其他神经退行性疾病,如帕
金森病和缺血性中风的用途。