公开(公告)号：US20240092821A1

公开(公告)日：2024-03-21

申请号：US17916064

申请日：2021-03-30

申请人： JANSSEN BIOPHARMA, INC.

发明人： Minghong Zhong ,  Yi Jin ,  Dinesh Gala ,  Marija Prhavc

IPC分类号： C07H21/02 ,  C07H19/067 ,  C07H19/167

CPC分类号： C07H21/02 ,  C07H19/067 ,  C07H19/167

摘要： Methods of synthesizing oligonucleotides via new intermediates on a cleavable support having an azidomethyl moiety are disclosed. The method comprises multiple reaction cycles, each of which comprises sequential coupling a nucleoside or oligonucleotide subunit on a cleavable support having an azidomethyl moiety and a nucleoside phosphoramidite or an oligonucleotide phosphoramidite, capping, oxidation/thiolation and deblocking; followed by orthogonal cleavage of the azidomethyl support while keeping all other protecting groups intact. The method can be used in combination with a support moiety for either solid phase or liquid phase oligo synthesis. The soluble support facilitates homogeneous reactions and efficient separations by simple precipitation. The methods also provide novel intermediates useful in the synthesis of oligonucleotide conjugates.

公开(公告)号：US10745427B2

公开(公告)日：2020-08-18

申请号：US16090715

申请日：2017-03-09

申请人： Janssen BioPharma, Inc.

发明人： Leonid Beigelman ,  Guangyi Wang ,  Minghong Zhong

IPC分类号： A61K31/683 ,  A61K31/675 ,  C07F9/6561 ,  C07D487/04 ,  A61P31/18 ,  A61P31/20 ,  A61F13/511 ,  A61F13/513 ,  A61F13/512 ,  A61F13/514 ,  A61F13/51

摘要： Disclosed herein are nucleotide analogs, methods of synthesizing nucleotide analogs and methods of treating diseases and/or conditions such as a HBV and/or HDV and/or HIV infection with one or more nucleotide analogs.