Geron Corporation

Lynx Therapeutics, Inc.

Northwestern University

Exicure, Inc.

Janssen Biopharma, Inc.

The University of Texas System

Other

Janssen Pharmaceutica Nv

Exicure Operating Company

University of California

University of Rochester

Healthpartners Research Foundation

Perkin-Elmer Corporation, Applied Biosystems, Inc.

Janssen Pharmaceuticals, Inc.

Sergei M Gryaznov

Krisztina Pongracz

Ronald G Schultz

Christopher C Mader

Aleksandar Filip Radovic-Moreno

Leonid Beigelman

Ronald A Pruzan

Jer-Kang Chen

Daria Zielinska

Robert L Letsinger

Vivek Kumar Rajwanshi

Richard Kang

Subbarao Nallagatla

Richard L Tolman

Gregg B Morin

Jerry W Shay

Jin Hong

David H Lloyd

Sarah N McCurdy

Chad A Mirkin

SonBinh T Nguyen

Tracy J Matray

Resham Singh Banga

Natalia Chernyak

Sydney Brenner

Robert B Dubridge

Karen L Fearon

Woodring E Wright

Yi Jin

Antitsa Dimitrova Stoycheva

Glenn Albrecht

Rajendra K Pandey

Weston Daniel

Bernard L Hirschbein

Jeffrey Lindquist

Warefta Hasan

Aaron Love

Lakshmipathi Pandarinathan

Bharat Baral

Tiffany L Halo

William Howard Frey, Ii

Steven Fung

Stephen M Testa

Ilgen Mender

Dennis F Deen

Matthew D Disney

Douglas H Turner

Andreas Ebneth

Saul Martinez Montero

Constantin Van Outryve D'Ydewalle

Saúl Martinez Montero

Jeffery S Nelson

Jeffrey S Nelson

Kimberly Batten

Theodore Yun

Jeffrey N Lindquist

Constantin Van Outryve D'YDEWALLE

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

Modified nucleoside phosphoramidites

This invention relates to compounds useful for inhibiting telomere elongation. More specifically, the invention provides nucleotide analogs that are incorporated into telomeres by telomerase thereby inhibiting elongation of telomeres. The compounds are use in treating cancer and other cell proliferative diseases.

Guanine analogs as telomerase substrates and telomere length affectors

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

The described invention is directed toward pharmaceutical compositions and methods of using 6-mercaptopurine ribosides and analogues thereof for the treatment of cancer and other hyperproliferative diseases. The described compounds can be converted into telomere substrates in vivo and can be recognized by telomerase for incorporation into telomeres of telomerase active cells, leading to induction of cell death of the telomerase active cells.

Treatment of drug resistant proliferative diseases with telomerase mediated telomere altering compounds

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.

Liposomal spherical nucleic acids that function as multivalent immune modulators are provided according to the invention. The liposomal spherical nucleic acids of the invention are useful prophylactic and therapeutic applications as well as research and diagnostic indications.

Multivalent delivery of immune modulators by liposomal spherical nucleic acids for prophylactic or therapeutic applications

Liposomes termed as small unilamellar vesicles (SUVs), can be synthesized in the 20-50 nm size range, but encounter challenges such as instability and aggregation leading to inter-particle fusion. This limits their use as a therapeutic delivery agent. Increasing the surface negative charge of SUVs, via the attachment of anionic entities such as DNA/RNA, increases the colloidal stability of these vesicles. Additionally, the dense spherical arrangement and radial orientation of nucleic acids exhibits unique chemical and biological properties, unlike their linear counterparts. These liposomal particles, are non-toxic and though anionic, can efficiently enter cells without the aid of ancillary cationic transfection agents in a non-immunogenic fashion. These exceptional properties allow their use as delivery agents for gene regulation in different therapies and offer an alternative platform to metal core spherical nucleic acids.

Liposomal particles, methods of making same and uses thereof

Oligonucleotides comprising modifications at the 2' and/or 3&#x2032; positions(s) along with methods of making and use against Alzheimer disease and other tauopathies are disclosed.

Modified oligonucleotides for use in treatment of tauopathies

The present disclosure relates to compounds and compositions containing 5'-phosphoramidite nucleoside monomers of formulae (I) and (II), and methods of making and use, wherein the substituents are as defined in the appended claims. 

Oligodeoxynucleotide-based immunostimulatory Toll-Like Receptor 9 (TLR9) agonists are described. Also described are compositions comprising the TLR9 agonists, methods of making the TLR9 agonists, and methods of using the TLR9 agonists to treat immune diseases, disorders or conditions, such as viral infections or cancer.

Oligonucleotide constructs and uses thereof

Aspects of the invention relate to spherical nucleic acid-based constructs and related methods and compositions thereof. The compositions of the invention are useful for activating agonists of nucleic acid interacting complexes, such as TLRs, stimulating an immune response, and treating diseases such as infectious disease, cancer, allergies, allergic diseases, and autoimmune disease

Spherical nucleic acid-based constructs as immunostimulatory agents for prophylactic and therapeutic use

Aspects of the invention relate to spherical nucleic acid-based constructs and related methods and compositions thereof. The compositions of the invention are useful for activating agonists of nucleic acid interacting complexes, such as TLRs, stimulating an immune response, and treating diseases such as infectious disease, cancer, allergies, allergic diseases, and autoimmune disease.

Growing community of inventors

San Mateo, CA, United States of America

Sergei M Gryaznov