UDP GlcNS 、 D-glucosamine 2-sulfate 、 UDP GlcNAc6N3 、 在
amino 作用下,
以
sodium hydroxide 为溶剂,
以Selective acylation of the free amino group of F5-10 using various acyl chlorides produced C-6 modified UDP-GlcNAc的产率得到
参考文献:
名称:
Chemoenzymatic synthesis of heparin and heparan sulfate analogs
[EN] CONJUGATED ANTISENSE COMPOUNDS AND THEIR USE<br/>[FR] COMPOSÉS ANTISENS CONJUGUÉS ET LEUR UTILISATION
申请人:ISIS PHARMACEUTICALS INC
公开号:WO2014179620A1
公开(公告)日:2014-11-06
Provided herein are oligomeric compounds with conjugate groups. In certain embodiments, the oligomeric compounds are conjugated to N-Acetylgalactosamine.
本文提供了具有共轭基团的寡聚化合物。在某些实施例中,这些寡聚化合物与N-乙酰半乳糖结合。
[EN] TARGETED THERAPEUTIC NUCLEOSIDES AND THEIR USE<br/>[FR] NUCLÉOSIDES THÉRAPEUTIQUES CIBLÉES ET LEUR UTILISATION
申请人:ISIS PHARMACEUTICALS INC
公开号:WO2015042447A1
公开(公告)日:2015-03-26
Provided herein are compounds comprising one or more therapeutic nucleosides and one or more targeting groups. In certain embodiments, the compounds further comprise one or more oligonucleotides. In certain embodiments, a targeting group comprises one or more N-Acetylgalactosamine.
[EN] MORPHOLINO MODIFIED OLIGOMERIC COMPOUNDS<br/>[FR] COMPOSÉS OLIGOMÈRES MODIFIÉS PAR MORPHOLINO
申请人:IONIS PHARMACEUTICALS INC
公开号:WO2018165564A1
公开(公告)日:2018-09-13
The present invention provides morpholino modified oligomeric compounds having at least one monomer subunit having Formula III, compounds having Formula I useful for making certain of the morpholino modified oligomeric compounds and methods of using the oligomeric compounds. In certain embodiments, the oligomeric compounds provided herein provide for an improved toxicity profile. Certain such oligomeric compounds are useful for hybridizing to a complementary nucleic acid, including but not limited, to nucleic acids in a cell. In certain embodiments, hybridization results in modulation of the amount of activity or expression of the target nucleic acid in a cell.
[EN] LINKAGE MODIFIED OLIGOMERIC COMPOUNDS<br/>[FR] COMPOSÉS OLIGOMÈRES MODIFIÉS PAR LIAISON
申请人:ISIS PHARMACEUTICALS INC
公开号:WO2015168172A1
公开(公告)日:2015-11-05
The present invention provides oligomeric compounds comprising at least one neutral methoxypropyl phosphonate modified internucleoside linkage. Such oligomeric compounds have one or more improved properties such as selectivity, potency, improved toxicity profile and or improved proinflammatory profile. Such oligomeric compounds have enhanced stability to exposure to base during synthesis. Certain such oligomeric compounds are useful for hybridizing to a complementary nucleic acid, including but not limited, to nucleic acids in a cell. In certain embodiments, hybridization results in modulation of the amount activity or expression of the target nucleic acid in a cell.
Method for synthesis of reactive conjugate clusters
申请人:Ionis Pharmaceuticals, Inc.
公开号:US10098959B2
公开(公告)日:2018-10-16
Provided herein are improved methods for the synthesis of reactive conjugate clusters and intermediates used in such methods. In particular, improvements are provided that enhance the synthesis of reactive conjugate clusters by reducing the number of synthetic steps required. The reactive conjugate clusters prepared using the improved methods don't include any transacylation impurities that are formed using existing methods. The improved methods also provide an increase in overall yield and a cost benefit over existing methods.