Hongene Biotech Corporation

David Yu

Aldrich N K Lau

Yun-Chiao Yao

Ruiming Zou

Gang Zhao

Wing C Poon

Gengyu Du

Xiaoyang Guan

Gaomai Yang

Jingshe Song

Xiaoling Zheng

Mufa Zou

John Michael Cue

Hongrong Yang

Xiaojun Li

John Liu

Shengdong Wang

Aldrich Nk Lau

Michael Su

Allen Wong

Min Xie

Guijun Yu

Zhixia Li

The present disclosure relates to methods and compounds for liquid phase oligonucleotide synthesis employing the use of small molecules with lipophilic groups. Methods for making an oligonucleotide by liquid phase oligonucleotide synthesis using the compounds described herein are also provided.

Compounds and methods for liquid phase oligonucleotide synthesis

Embodiments of the present application relate to polymers used as polymeric polyvalent hubs for liquid phase oligonucleotide synthesis. Methods for making an oligonucleotide by liquid phase oligonucleotide synthesis using the polymers are also provided.

Compositions and methods for liquid phase oligonucleotide synthesis

Embodiments of the present application relate to functionalized N-acetylgalactosamine analogs, methods of making, and uses of the same. In particular, polyvalent N-acetylgalactosamine analogs may be prepared by utilizing a wide variety of linkers containing functional groups. These functionalized N-acetylgalactosamine analogs may be used in the preparation of targeted delivery of oligonucleotide-based therapeutics.

Functionalized N-acetylgalactosamine analogs

Embodiments of the present disclosure relate to lipid-PEGylated solid support and phosphoramidites derivatives, methods for preparing the same, and their uses in the delivery of oligonucleotide drugs to the cellular targets.

Lipid-pegylated compounds, preparations and uses thereof

Embodiments of the present application relate to polymers used as polymeric polyvalent hub for liquid phase oligonucleotide synthesis. Methods for making an oligonucleotide by liquid phase oligonucleotide synthesis using the polyvalent hub are also provided.

Embodiments of the present application relate to porous polymeric beads solid support for use in oligonucleotide synthesis and the method of producing and using the same. Further embodiments relate to porous polymeric beads and method for preparing and using the same.

Polymeric solid support for oligonucleotide synthesis

Embodiments of the present application relate to functionalized N-acetylgalactosamine-analogs, methods of making, and uses of the same. In particular, mono or trivalent N-acetylgalactosamine analogs may be prepared by utilizing a wide variety of linkers containing functional groups. These functionalized N-acetylgalactosamine-analogs may be used in the preparation of targeted delivery of oligonucleotide-based therapeutics.

Embodiments of the present application relate to the preparation of 2′-O-protected nucleoside phosphoramidites and conjugation of the 2′-O-protected nucleoside to a solid support. More specifically, the present application relates to nucleosides having a hydroxy protecting group at the 2′ position that reduces migration to the 3′ position during RNA (e.g., mRNA) synthesis and can be readily removed under mild conditions without the use of toxic metal-containing reagents. Methods of using the nucleosides described herein in RNA synthesis are also disclosed.

Synthesis of 2′ protected nucleosides

Functionalized n-acetylgalactosamine analogs

Embodiments of the present application relate to polymers for liquid phase oligonucleotide synthesis. Methods for making an oligonucleotide by liquid phase oligonucleotide synthesis, comprising dissolving a polyvalent hub having a plurality of functional groups in a solvent and contacting the polyvalent hub with one or more nucleoside analogs to form a first bioconjugate are also provided.

Embodiments of the present application relate to N-acetylgalactosamine-conjugated nucleosides. In particular, the N-acetylgalactosamine is installed on the nucleobase of the nucleosides through a wide variety of linkers. Methods of making N-acetylgalactosamine-conjugated nucleosides are also disclosed herein. N-acetylgalactosamine is a well-defined liver-targeted moiety and N-acetylgalactosamine-conjugated nucleosides may be used in the preparation of targeted delivery of oligonucleotide-based therapeutics.

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Union City, CA, United States of America

David Yu