申请人:Savage Paul B.
公开号:US20160096864A1
公开(公告)日:2016-04-07
Prodrugs or pharmaceutically acceptable salts, stereoisomers, solvates, or polymorphs thereof include a pharmaceutically and/or diagnostically active cationic steroidal antimicrobial (hereinafter “CSA”) compound or pharmaceutically acceptable salt, stereoisomer, solvate, or polymorph thereof, and one or more cleavable groups (C.G.). Some embodiments include a CSA compound prepared in an inactive or less active form and that is capable of conversion to a fully active form upon administration to a subject, upon preparation of a pharmaceutical formulation containing the CSA composition, and/or upon exposure to physiological conditions. Pharmaceutical compositions include the prodrug or pharmaceutically acceptable salt, stereoisomer, solvate, or polymorph thereof and one or more pharmaceutically acceptable excipients. Methods of treatment of bacterial infections in a patient in need utilize prodrugs or pharmaceutically acceptable salts, stereoisomers, solvates, polymorphs thereof and/or the pharmaceutical compositions described herein.
前药或药学上可接受的盐、立体异构体、溶剂化物或其多晶体包括一种药学上和/或诊断上活性的阳离子类固醇抗微生物化合物(以下简称“CSA”)化合物或药学上可接受的盐、立体异构体、溶剂化物或其多晶体,以及一个或多个可裂解基团(C.G.)。一些实施例包括以不活性或较不活性形式制备的CSA化合物,该化合物能够在给予受试者、制备含有CSA组分的制药配方和/或暴露于生理条件下时转化为完全活性形式。制药组合物包括前药或药学上可接受的盐、立体异构体、溶剂化物或其多晶体以及一个或多个药学上可接受的辅料。需要治疗细菌感染的患者的治疗方法利用前药或药学上可接受的盐、立体异构体、溶剂化物、多晶体和/或本文所述的制药组合物。