发明名称 Adamantane analogs
摘要 Provided are compounds that are capable of modulating the activity of the influenza A virus via interaction with the M2 transmembrane protein. Also provided are methods for treating an influenza A-affected disease state or infection comprising administering a composition comprising one or more compounds that have been identified as being capable of interaction with the M2 protein.
申请公布号 US9301950(B2) 申请公布日期 2016.04.05
申请号 US201013391519 申请日期 2010.07.30
申请人 The Trustees Of The University of Pennsylvania 发明人 DeGrado William F.;Wang Jun
分类号 A61K31/438;A61K31/439;C07D209/56;C07D209/96;C07D233/61;A61K31/44;C07D339/08;C07D471/08 主分类号 A61K31/438
代理机构 Baker & Hostetler LLP 代理人 Baker & Hostetler LLP
主权项 1. A compound having the formula (I): wherein X is carbon, —NH(H+Cl−), alkylene, or alkyleneamino; R1 is hydrogen, deuterium, halo, hydroxyl, nitro, guanidinyl, —(R6)-guanidine, fonnamidinyl, carbonyl, oxime, amino, aminocarbonyl, aminooxy, aralkoxy, or aralkylaminooxy; R2 and R3 are each independently hydrogen, deuterium, hydroxyl, carbonyl, amino, nitro, alkyl, trifluoromethyl, aryl, aminocarbonyl, or —C(═Y)—Z, or R2 and R3 taken together along with the atom to which they are both attached form a six-membered carbocyclic ring or a dithanyl ring optionally substituted with up to three substituents independently selected from alkyl, aryl, aralkyl, hydroxyl, nitro, amino, andcarbonyl; Y is O, S, or NH; Z is amino, —NH—NH2, methyloxy, or methylthio; R4 is hydrogen, deuterium, or amino; R5 is hydrogen or carbonyl; and, R6 is —CH(CH3)— or —NH—C(═NH)—; or a stereoisomer, partial stereoisomer, prodrug, pharmaceutically acceptable salt, hydrate, solvate, acid hydrate, or N-oxide thereof, with the proviso that if R1 is amino and X is methylene or ethylene, R2, R3, R4, and R5 cannot all be hydrogen.
地址 Philadelphia PA US