发明名称 Oligomer-calcimimetic conjugates and related compunds
摘要 The invention relates to (among other things) oligomer-calcimimetic conjugates and related compounds. A conjugate of the invention, when administered by any of a number of administration routes, exhibits advantages over previously administered compounds.
申请公布号 US9421275(B2) 申请公布日期 2016.08.23
申请号 US201414223572 申请日期 2014.03.24
申请人 Nektar Therapeutics 发明人 Riggs-Sauthier Jennifer;Cheng Lin;Martin David
分类号 A61P5/10;A61K31/137;A61K31/27;C07C271/14;A61K47/48;C07C211/30 主分类号 A61P5/10
代理机构 代理人
主权项 1. A compound according to Formula II-Ce:or a pharmaceutically acceptable salt or solvate thereof, wherein: is 3-methoxyphenyl, 3-chlorophenyl or 1-naphthyl; each R4 is independently —H, —F, —Cl, —Br, —I, phenyl, —CF3, —CF2H, —CFH2, lower alkyl, —O-lower alkyl, —OCH2CF3, —OH, —CN, —NO2, —C(O)-lower alkyl, —C(O)O-lower alkyl, —C(O)NH-lower alkyl, —C(O)N-(lower alkyl)2, —OC(O)-lower alkyl, or —NH—C(O)-lower alkyl; a is an integer from 1 to 5; R5 is lower alkyl; R is a residue of polyol, polythiol or polyamine bearing from 3 to about 50 hydroxyl, thiol or amino groups; POLY is a water-soluble, non-peptidic polymer; each of X and Q is independently —(CRxRy)a′—Kw—(CRxRy)b—(CH2CH2O)c—(CRxRy)d—Kz—, an amino acid residue, or combination thereof; each of Rx and Ry, in each occurrence, is independently H, alkyl substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, aryl or substituted aryl; each of Kw and Kz is independently —NH—, —C(O)—, —C(O)NH—, —NHC(O)—, —O—, —S—, —OC(O)—, —C(O)O—, —OC(O)O—, —OC(O)NH—, or —NHC(O)O—; each a′ is independently an integer from 0 to 12; each b is independently an integer from 0 to 12; each c is independently an integer from 0 to 25; each d is independently an integer from 0 to 12; with the proviso that neither X nor Q is —O—O—, —NH—O—, nor —NH—NH—; and q is an integer from 3 to about 50.
地址 San Francisco CA US