Sirna Therapeutics, Inc.

Ribozyme Pharmaceuticals, Incorporated

Alios Biopharma, Inc.

Merck Sharp & Dohme Corporation

Janssen Biopharma, Inc.

Aligos Therapeutics, Inc.

Intermune, Inc.

Other

Janssen Pharmaceutica Nv

Janssen Biotech, Inc.

Katholieke Universiteit Leuven

Vertex Pharmaceuticals, Inc.

Janssen Pharmaceuticals, Inc.

Quark Pharmaceuticals, Inc.

Array Biopharma Inc.

Leonid Beigelman

Anh Truong

James A McSwiggen

David Bernard Smith

Guangyi Wang

Jasenka Matulic-Adamic

Nassim Usman

Jerome Deval

Alexander Karpeisky

Vivek Kumar Rajwanshi

Alex Karpeisky

Lawrence M Blatt

Vladimir Serebryany

David Sweedler

Antitsa Dimitrova Stoycheva

James Mcswiggen

Scott D Seiwert

Chandra Vargeese

Francine E Wincott

Natalia Dyatkina

Marija Prhavc

Koen Vandyck

Karl Kossen

Alex B Burgin

Robert Than Hendricks

Peter Haeberli

Jin Hong

Lech W Dudycz

Julian Alexander Symons

Pierre Jean-Marie Bernard Raboisson

Sergei M Gryaznov

Anthony DiRenzo

Rajendra K Pandey

Santhosh Kumar Thatikonda

Minghong Zhong

Amber Beaudry

James Patrick Edwards

Peter J Connolly

David Craig McGowan

Stuart Emanuel

Ramachandran Radhakrishnan

Gilles C Bignan

Dorothée Alice Marie-Eve Bardiot

Jyanwei Liu

Anh P Truong

Shawn Patrick Zinnen

Tao Hu

Danuta Tracz

Susan Grimm

Arnaud Didier Marie Marchand

Donald Ruhrmund

Mark Richter

Luca Francesco Mario Raveglia

Ivana Bianchi

Laurent Bellon

Carmela Napolitano

Young Chun Jung

Pamela Pavco

Andras Horvath

Luca Francesco Raveglia

Stefania Vallese

Steven Wade Andrews

Haiying He

Thale Jarvis

Daniele Andreotti

Elena Feinstein

Brad Owen Buckman

Timothy S Kercher

Luigi Anzalone

Yi Jin

Markus Hossbach

James D Thompson

Sandrine Vendeville

April L Kennedy

Karin Ann Stein

Yutong Jiang

Tianbao Lu

Julia Haas

Igor Mett

Tod M Woolf

Kevin Ronald Condroski

Bin Wang

Weimin Wang

Hagar Kalinski

Sharon Avkin-Nachum

Williamson Ziegler Bradford

Michael Lyon

Rami Skaliter

Fritz Eckstein

Ronald R Breaker

Peter Jamison Rose

Tongqian Chen

Kathy L Fosnaugh

David Morrissey

Min Jiang

Bharat Chowrira

Yannick Debing

Robert J Kaus

Hua Tan

The present disclosure relates to compounds and compositions containing 5'-phosphoramidite nucleoside monomers, and methods of making and use.

Modified nucleoside phosphoramidites

Provided herein are compounds of Formula (I), or pharmaceutically acceptable salts thereof, pharmaceutical compositions that include a compound described herein (including pharmaceutically acceptable salts of a compound described herein) and methods of synthesizing the same. Also provided herein are methods of treating diseases and/or conditions with a compound of Formula (I), or a pharmaceutically acceptable salt thereof.

Anti-viral compounds

Disclosed herein are nucleotide analogs, methods of synthesizing nucleotide analogs and methods of treating diseases and/or conditions such as a HCV infection with one or more nucleotide analogs.

Substituted nucleosides, nucleotides and analogs thereof

Disclosed herein are short interfering nucleic acid (siNA) molecules comprising modified nucleotides and uses thereof. The siNA molecules may be double stranded and comprise modified nucleotides selected from 2'-O-methyl nucleotides and 2′-fluoro nucleotides. Further disclosed herein are siNA molecules comprising (a) a phosphorylation blocker, conjugated moiety, or 5′-stabilized end cap; and (b) a short interfering nucleic acid (siNA).

Modified short interfering nucleic acid (siNA) molecules and uses thereof

Modified oligonucleotides comprising modifications at the 2' and/or 3′ position(s) along with methods of making and use, e.g., against HBV are disclosed.

Modified oligonucleotides and methods of use

A method of making a compound represented by Formula (I): includes a reducing step, a protecting step, and a phosphitylating step, where X is NH; Y is OCF, —O(CR)CR, —O(CR)OCR, or —O(CR)—CR═CR; Z is H; B is adenine (A), guanine (G), thymine (T), cytosine (C), uracil (U), 5-methylcytosine (5-me-C), or a protected version of A, G, T, C, U, or 5-me-C; each Ris independently Calkyl or cycloalkyl; Ris CHCHCN or Calkyl; or Rand Rtogether form an optionally substituted Ccycloalkyl; Ris H or PG; PG is a protecting group; Ris independently in each instance H or F; a is 1 or 2; and b is 1, 2, or 3.

The present disclosure relates to small interfering RNA (siRNA) molecules directed to mRNA transcripts of CD274 to cause downregulation of programmed death-ligand 1 (PD-L1) expression in humans. The siRNA can be constructed of unmodified nucleotides or modified nucleotides that exhibit modified sugars, nucleobases, linkages, or covalently bound targeting moieties. Also disclosed herein are pharmaceutical compositions of siRNAs and uses of or methods of using the siRNAs for the treatment of PD-L1 related diseases including but not limited to liver diseases, cancer, hepatocellular carcinoma, viral diseases, or hepatitis B.

Methods and compositions for targeting PD-L1

Disclosed herein are compounds of Formula I: or a stereoisomer or a tautomer thereof, or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising such compounds, and methods of treating disease by administering or contacting a subject with one or more of the above compounds.

Bicyclic pyridazinones and methods of use thereof

Disclosed herein are compounds of Formula I': or a stereoisomer or a tautomer thereof, or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising such compounds, and methods of treating disease by administering or contacting a subject with one or more of the above compounds.

Oxindoles and methods of use thereof

Disclosed herein are compounds of Formula I&#x2033;: or a stereoisomer or a tautomer thereof, or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising such compounds, and methods of treating disease by administering or contacting a subject with one or more of the above compounds.

2-pyridones and methods of use thereof

Provided herein are compounds of Formula (I), Formula (II) and/or Formula (III), or pharmaceutically acceptable salts of any of the foregoing, pharmaceutical compositions that include a compound described herein (including pharmaceutically acceptable salts of a compound described herein) and methods of synthesizing the same. Also provided herein are methods of treating diseases and/or conditions with a compound of Formula (I), Formula (II) and/or Formula (III), or a pharmaceutically acceptable salt of any of the foregoing.

Modified cyclic dinucleoside compounds as sting modulators

Pyrrole compounds

Growing community of inventors

San Mateo, CA, United States of America

Leonid Beigelman