公开(公告)号：US10781175B2

公开(公告)日：2020-09-22

申请号：US15650773

申请日：2017-07-14

申请人： AM Chemicals LLC

发明人： Andrei Pavel Guzaev ,  Vladimir Y. Vvedenskiy ,  Khirud Gogoi

IPC分类号： C07D211/22 ,  C07F9/59 ,  C07F9/6561 ,  C07F9/6558 ,  C07F9/568 ,  C07F9/24 ,  C07D205/04 ,  C07D401/12 ,  C07D409/06 ,  C07D491/18 ,  C07D493/10 ,  C07D495/04 ,  C07H1/00 ,  C07H15/26 ,  C07H21/00 ,  C07J43/00

摘要： Novel non-nucleoside solid supports and phosphoramidite building blocks for preparation of synthetic oligonucleotides containing at least one non-nucleosidic moiety conjugated to a ligand of practical interest and synthetic processes for making the same are disclosed. Furthermore, oligomeric compounds are prepared using said solid supports and phosphoramidite building blocks, preferably followed by removal of protecting groups to provide oligonucleotides conjugated to ligands of interest.

公开(公告)号：US20200291057A1

公开(公告)日：2020-09-17

申请号：US16464291

申请日：2017-11-30

申请人： NOXXON Pharma AG

发明人： Lucas Bethge

IPC分类号： C07H21/00 ,  C12N15/113

摘要： The present invention is related to a method for the preparation of a modified nucleic acid molecule comprising a nucleic acid moiety and a non-nucleic acid moiety by reacting a first reactant and a second reactant, wherein the first reactant comprises the non-nucleic acid moiety and a carboxyl group, and wherein the second reactant is an amino-modified nucleic acid molecule comprising the nucleic acid moiety and an amino modification comprising an amino group which is attached to the nucleic acid moiety, wherein the method comprises the following steps: a) activating the first reactant, preferably the carboxyl group of the first reactant, by a condensation reagent in a water miscible organic solvent, and b) reacting the activated first reactant, preferably the activated carboxyl group of the first reactant, of step a) and the second reactant, preferably the amino group of the amino modification of the amino-modified nucleic acid molecule which has been dissolved in water or a mixture of a water miscible organic solvent and water, whereby the modified nucleic acid molecule is formed.

公开(公告)号：US10760078B2

公开(公告)日：2020-09-01

申请号：US16225909

申请日：2018-12-19

申请人： Sarepta Therapeutics, Inc.

发明人： Gunnar J. Hanson ,  Alexander Charles Rudolph ,  Bao Zhong Cai ,  Ming Zhou ,  Dwight D. Weller

IPC分类号： C12N15/113 ,  C07F9/59 ,  C07F9/572 ,  C07F9/6558 ,  C07F9/6561 ,  C07F9/6584 ,  C07H21/00 ,  A61K31/496 ,  A61K31/5377 ,  C07D265/30 ,  C07D295/108 ,  C07F9/22 ,  C07F9/26 ,  C07F9/6544

摘要： Oligonucleotide analogues comprising modified intersubunit linkages and/or modified 3′ and/or 5′-end groups are provided. The disclosed compounds are useful for the treatment of diseases where inhibition of protein expression or correction of aberrant mRNA splice products produces beneficial therapeutic effects.

公开(公告)号：US10759825B2

公开(公告)日：2020-09-01

申请号：US15886568

申请日：2018-02-01

申请人： Merck Sharp & Dohme Corp.

发明人： Michael D. Altman ,  Brian Andresen ,  Wonsuk Chang ,  Matthew Lloyd Childers ,  Jared N. Cumming ,  James P. Jewell ,  Jongwon Lim ,  Alan B. Northrup ,  Ryan D. Otte ,  Benjamin Wesley Trotter ,  Quang T. Truong ,  Shawn P. Walsh ,  Kake Zhao

IPC分类号： A01N43/04 ,  A61K31/70 ,  C07H21/04 ,  C07H21/02 ,  A61K39/39 ,  C07H19/20 ,  C07H19/23 ,  C07H21/00 ,  A61P35/00 ,  A61K31/7064 ,  A61K31/7084 ,  A61K31/708 ,  A61K31/706 ,  A61K31/7076

摘要： A class of polycyclic compounds of general formula (I), of general formula (I′), or of general formula (I″), wherein Base1, Base2, Y, Ya, Xa, Xa1, Xb, Xb1, Xc, Xc1, Xd, Xd1, R1, R1a, R2, R2a, R3, R4, R4a, R5, R6, R6a, R7, R7a, R8, and R8a are defined herein, that may be useful as inductors of type I interferon production, specifically as STING active agents, are provided. Also provided are processes for the synthesis and use of compounds.

公开(公告)号：US10752939B2

公开(公告)日：2020-08-25

申请号：US15656541

申请日：2017-07-21

申请人： LUMINEX CORPORATION

发明人： Scott C. Johnson ,  Nicolas Arab ,  Doug Whitman

IPC分类号： C12Q1/68 ,  C07H21/00 ,  C12Q1/6818 ,  C12Q1/6816 ,  C12Q1/6823

摘要： Methods and compositions for the detection and quantification of nucleic acids are provided. In certain embodiments, methods involve the use of cleavable probes that comprise a ribonucleotide position that is susceptible to endoribonuclease (e.g., RNase H) cleavage in the presence of target nucleic acid molecules. Probes of the embodiments may also comprise non-natural nucleotide linked to a reporter and/or quenching moiety.

公开(公告)号：US10745728B1

公开(公告)日：2020-08-18

申请号：US16113766

申请日：2018-08-27

申请人： Steven A Benner ,  Hyo-Joong Kim ,  Zunyi Yang

发明人： Steven A Benner ,  Hyo-Joong Kim ,  Zunyi Yang

IPC分类号： C07H19/00 ,  C07H21/00 ,  C12P19/34 ,  C12Q1/686 ,  C07H19/04 ,  C07H21/02 ,  C07H21/04

摘要： This invention relates to the use of analogs of purines that have two tautomeric forms, one formally complementary to thymidine, the other formally complementary to cytidine, and analogs of pyrimidines that have two tautomeric forms, one formally complementary to guanosine, the other formally complementary to adenosine. These uses include the polymerase chain reaction amplification of targets having polymorphisms in primer binding sites and ligation.

公开(公告)号：US10738308B2

公开(公告)日：2020-08-11

申请号：US15863578

申请日：2018-01-05

申请人： SIRNA THERAPEUTICS, INC.

发明人： Wonsuk Chang ,  Erin N. Guidry ,  Matthew G. Stanton ,  Daniel Zewge

IPC分类号： C07H21/04 ,  C12N15/113 ,  C12N15/11 ,  C07H21/00 ,  C07H21/02 ,  C07H19/10

摘要： The present invention relates to RNAi molecules, and compositions thereof, comprising a 2′ internucleoside linkage connecting the nucleotide at position 1 and the nucleotide at position 2 at the 5′ end of the antisense strand. Specifically, the invention relates to single- and double-stranded short interfering nucleic acid (siNA) molecules that are capable of mediating RNA interference comprising 5′ modified nucleotides that comprise, among other potential modifications, a 2′ internucleoside linkage. The invention further relates to 5′ modified nucleotides used as reagents to generate the RNAi molecules of the invention and methods of using the disclosed RNAi molecules.

公开(公告)号：US10738074B2

公开(公告)日：2020-08-11

申请号：US15752144

申请日：2016-08-11

申请人： Merck Sharp & Dohme Corp. ,  Michael D. Altman ,  Brian Andresen ,  Wonsuk Chang ,  Matthew Lloyd Childers ,  Jared N. Cumming ,  Andrew Marc Haidle ,  Timothy J. Henderson ,  James P. Jewell ,  Min Lu ,  Alan B. Northrup ,  Ryan D. Otte ,  Tony Siu ,  Benjamin Wesley Trotter ,  Quang T. Truong

发明人： Michael D. Altman ,  Brian Andresen ,  Wonsuk Chang ,  Matthew Lloyd Childers ,  Jared N. Cumming ,  Andrew Marc Haidle ,  Timothy J. Henderson ,  James P. Jewell ,  Min Lu ,  Alan B. Northrup ,  Ryan D. Otte ,  Tony Siu ,  Benjamin Wesley Trotter ,  Quang T. Truong

IPC分类号： A01N43/04 ,  A61K31/70 ,  C07H21/04 ,  C07H21/02 ,  A61K39/39 ,  C07H19/20 ,  C07H19/23 ,  C07H21/00 ,  A61P35/00 ,  A61K31/7064 ,  A61K31/7084 ,  A61K31/708 ,  A61K31/706 ,  A61K31/7076

摘要： A class of polycyclic compounds of general formula (II), of general formula (II′), or of general formula (II″), wherein Base1, Base2, Y, Ya, Xa, Xa1, Xb, Xb1, Xc, Xc1, Xd, Xd1, R1, R1a, R2, R2a, R3a, R4, R4a, R5, R6, R6a, R7, R7a, R8, and R8a are defined herein, that may be useful as inductors of type I interferon production, specifically as STING active agents, are provided. Also provided are processes for the synthesis and use of compounds.

公开(公告)号：US20200224234A1

公开(公告)日：2020-07-16

申请号：US16629211

申请日：2018-07-10

申请人： THE SCRIPPS RESEARCH INSTITUTE

发明人： Floyd E. ROMESBERG ,  Yorke ZHANG ,  Aaron W. FELDMAN ,  Vivian T. DIEN

IPC分类号： C12P19/34 ,  C12N1/20 ,  C07H21/00

摘要： Disclosed herein are in vivo methods, compositions, and kits for producing nucleic acids which comprises at least one unnatural base. Disclosed herein are in vivo methods of producing a nucleic acid with an expanded genetic alphabet, the method comprising incorporatin at least one unnatural base in the nucleic acid. Disclosed herein are semi-synthetic organisms comprising an expanded genetic alphabet, wherein the genetic alphabet comprises at least one unnatural base. Disclosed herein are compositions that include a heterologous or recombinant polymerase and methods of use thereof. Further, disclosed herein are kits that are useful for stably incorporating an unnatural nucleic acid into a nucleic acid molecule, e.g., using the methods provided by the present invention in in vitro condition or under a cell free condition.

公开(公告)号：US10689643B2

公开(公告)日：2020-06-23

申请号：US14892911

申请日：2014-05-22

申请人： Active Motif, Inc.

发明人： Mary Anne Jelinek ,  Brian Stanley Egan ,  Joseph Fernandez

IPC分类号： C12N15/10 ,  C12Q1/6806 ,  C12Q1/6804 ,  C07H21/00

摘要： Disclosed herein are compositions, methods and kits useful for epigenetic analysis based on the use of transposons that are targeted to specific regions of chromatin based on DNA-DNA interactions, protein-protein interactions, RNA-RNA interactions, and nucleic acid-protein interactions.