发明名称 Saccharide structures and methods of making and using such structures
摘要 Described are oligosaccharides having a protecting group at two, a plurality, a majority of, or each position in the oligosaccharide which is amenable to derivatization. Collections, libraries and methods of making and using such oligosaccharides are also described.
申请公布号 US9163047(B2) 申请公布日期 2015.10.20
申请号 US201314075822 申请日期 2013.11.08
申请人 MOMENTA PHARMACEUTICALS, INC. 发明人 Roy Sucharita;Kishimoto Takashi Kei;Kaundinya Ganesh
分类号 A61K31/70;C07H1/00;C07H5/04;C07H9/04;C07H13/04;C07H15/10;C07H15/18;C07H15/203;C07H23/00;C08B37/00;C07H3/06 主分类号 A61K31/70
代理机构 Lando & Anastasi, LLP 代理人 Lando & Anastasi, LLP
主权项 1. A method of making an oligosaccharide with a preselected pattern of sulfation and/or acetylation, the oligosaccharide comprising disaccharide units, wherein the identity of each disaccharide unit is independent of the identity of the other disaccharide units within the oligosaccharide, and wherein the oligosaccharide is a tetrasaccharide, a hexasaccharide, an octasaccharide, or a decasaccharide, the method comprising: providing a protected oligosaccharide comprising disaccharide units, wherein the identity of each disaccharide unit is independent of the identity of the other disaccharide units within the protected oligosaccharide, wherein the protected oligosaccharide is a tetrasaccharide, a hexasaccharide, an octasaccharide, or a decasaccharide, and wherein the protected oligosaccharide comprises:wherein each tetrasaccharide comprises X1, each hexasaccharide comprises X1 and X2, each octasaccharide comprises X1, X2, and X3, and each decasaccharide comprises X1, X2, X3, and X4 ; and wherein each of X1, X2, X3 and X4 is independently A or B, and whereinA isandB is wherein R8 for each occurrence of A or B is independently a hydrogen or an alkyl group, and wherein R5 for each occurrence of A or B is an amine containing protecting group that, independently for each occurrence, is an amine containing protecting group selected from either a first amine containing protecting group that allows sulfation or acetylation or a second amine containing protecting group that does not allow sulfation or acetylation, and wherein R1, R2, R6, and R7 for each occurrence of A or B is a protecting group selected from either a first protecting group that allows sulfation or acetylation, or a second protecting group that does not allow sulfation or acetylation; and deprotecting the first protecting group to form an unprotected moiety or moieties and forming a sulfate or acetyl moiety at the deprotected position or positions, to thereby produce the oligosaccharide with the preselected pattern of sulfation and/or acetylation.
地址 Cambridge MA US