发明名称 6-ACETYLMORPHINE ANALOGS, AND METHODS FOR THEIR SYNTHESIS AND USE
摘要 The present invention relates to novel 6-acetylmorphine analogs, and methods for their synthesis and use. Such analogs are designed to provide a convenient linkage chemistry for coupling under mild conditions to a suitable group on a target protein, polypeptide, solid phase or detectable label.
申请公布号 US2016022809(A1) 申请公布日期 2016.01.28
申请号 US201414775644 申请日期 2014.03.14
申请人 ALERE SAN DIEGO, INC. 发明人 BANASZCZYK Mariusz;HÉBERT Normand;STOWE Neil
分类号 A61K39/385;C07D489/02;C07F9/6561;C08L25/06;A61K39/39;C07K16/06;C07K16/44;G01N33/94;C07D489/00;A61K39/00 主分类号 A61K39/385
代理机构 代理人
主权项 1. A compound or salt thereof, said compound having a general formula selected from (I), (II), (III) or (IV):where R1, R3, R4, or R5 is a linkage chemistry which provides a terminal functional moiety selected from the group consisting of protected or unprotected sulfhydryl moieties, protected or unprotected amine moieties, primary amine-reactive moieties, sulfhydryl-reactive moieties, photoreactive moieties, carboxyl-reactive moieties, arginine-reactive moieties, and carbonyl-reactive moieties; each Z is independently optionally substituted C1-4 alkyl, C1-4 alkoxy, N, O, S, and aryl, wherein substitution(s), when present, may be independently selected from the group consisting of C1-6 alkyl straight or branched chain, benzyl, halogen, trihalomethyl, C1-6 alkoxy, —NO2, —NH2, —OH, ═O, —COOR′ where R′ is H or lower alkyl, —CH2OH, and —CONH2, and where Z is preferably O, S, N, NH, CH3, CH2, CH, CHF or CF2, and where Z is most preferably —C(O)—, —N(H)— or —O—. each Y is independently selected from the group consisting of  wherein each R2 is independently optionally substituted C1-4 alkyl, C1-4 alkoxy, OH, N, O, S, and aryl, wherein substitution(s), when present, may be independently selected from the group consisting of C1-6 alkyl straight or branched chain, benzyl, halogen, trihalomethyl, C1-6 alkoxy, —NO2, —NH2, —OH, ═O, —COOR′ where R′ is H or lower alkyl, —CH2OH, and —CONH2, and where each R2 is preferably CH3, CF3, CHF2, CH2F or NH2; and each X is H or together form a covalent bond.
地址 San Diego CA US