发明名称 Modified creatine compounds
摘要 The invention discloses creatine derivatives that are represented by Formula (I), Formula (II), and Formula (III); wherein Z is a functional group; Y is a mitochondrial targeting agent, a cationic ammonium group, or a polypeptide containing at least one positively charged amino acid residue; each R1 is independently hydrogen, alkyl, or a phosphate group; R2 a linker; R3 is a spacer group; R4 is hydrogen, alkyl, aryl, or heterocyclic; or R4 and R1, or R4 and R3, together with the nitrogen atoms to which they are attached form a heterocyclic ring, and W is hydrogen or alkyl.;
申请公布号 US9434753(B2) 申请公布日期 2016.09.06
申请号 US201214345503 申请日期 2012.09.18
申请人 Gencia Corporation 发明人 Khan Shaharyar M.;Gadwood Robert;Romero Arthur Glenn
分类号 C07F9/54;C07F9/655;C07F9/6506;C07F9/22 主分类号 C07F9/54
代理机构 Honigman Miller Shwartz and Cohn LLP 代理人 Honigman Miller Shwartz and Cohn LLP ;Yang Lucy X.;O'Brien Jonathan P.
主权项 1. A compound of Formula Ior a pharmaceutically acceptable salt thereof wherein Z is —C(═O)NR5—; wherein R5 is hydrogen, alkyl, aryl, or heterocyclic; Y is a phosphonium group; each R1 is independently hydrogen, alkyl, or a phosphate group; R2 is alkyl; R3 is alkyl, cycloalkyl, alkylcycloalkyl, heterocycloalkyl, or alkylheterocycloalkyl; R4 is hydrogen, or alkyl; at each occurrence, an alkyl is optionally substituted with 1-3 substituents independently selected from halo, haloalkyl, hydroxyl, amino, thio, ether, ester, oxo, aldehyde, cycloalkyl, nitrile, urea, amide, carbamate and aryl; at each occurrence, an aryl is optionally substituted with 1-5 substituents independently selected from halogen, azide, alkyl, haloalkyl, aralkyl, alkenyl, alkynyl, cycloalkyl, hydroxyl, alkoxyl, amino, nitro, sulfhydryl, imino, amido, phosphonate, phosphinate, carbonyl, carboxyl, silyl, ether, alkylthio, sulfonyl, sulfonamide, ketone, aldehyde, ester, heterocyclyl, and CN; W is hydrogen or alkyl; and with the provisos that Z and Y are not substituted on the same R2 carbon; and that Z and the —NR4— moiety are not substituted on the same R3 carbon.
地址 Charlottesville VA US