University of Kansas

The United States of America, As Represented by the Secretary, Department of Health and Human Services

Mediquest Therapeutics, Inc.

U.S. Government Nih Division of Extramural Inventions and Technology Resources (deitr)

Virovax LLC

Sunil Abraham David

Nikunj Shukla

Mark R Burns

Mallesh Beesu

Alex Christopher Salyer

Subbalakshmi Malladi

Giuseppe Caruso

Scott A Jenkins

Alex Salyer

Diptesh Sil

Cassandra Jones

Deepak B Salunke

Cindy S Scott-Watts

Lauren Miranda Fox

Xiaoqiang Guo

Hari Prasad Kokatla

Euna Yoo

Naveen Kumar Rayala

The disclosure provides human toll-like receptor modulators of general Formula (II), wherein R, R, R, R, R, R, R, Rare defined herein.

Human TLR8-selective agonists

A compound can include the structure of Formula 1, derivative thereof, prodrug thereof, salt thereof, stereoisomer thereof, tautomer thereof, polymorph thereof, or solvate thereof, or having any chirality at any chiral center: Rincludes a hydrogen or a substituent; Rincludes a hydroxyl, hydroxyl-forming prodrug, or hydroxyl-leaving chemical moiety; Rincludes a halogen; and Rincludes a heterocycle. The compound can be an antiviral compound used in antiviral therapies.

Antiviral compounds

The disclosure provides human toll-like receptor modulators of general Formula (II), wherein R, R, R, R, R, R, R, Rare defined herein. 

Compounds described herein can be used for therapeutic purposes. The compounds can be TLR agonists, such as TLR8 agonists. The compounds can be included in pharmaceutical compositions and used for therapies were being a TLR8 agonist is useful. The pharmaceutical compositions can include any ingredients, such as carries, diluents, excipients, fillers or the like that are common in pharmaceutical compositions. The compounds can be those illustrated or described herein as well as derivative thereof, prodrug thereof, salt thereof, or stereoisomer thereof, or having any chirality at any chiral center, or tautomer, polymorph, solvate, or combinations thereof. As such, the compounds can be used as adjuvants in vaccines as well as for other therapeutic purposes described herein. The compounds can have any one of the formulae described herein or derivative thereof.

Toll-like receptor 8 agonists

Compounds described herein can be used for therapeutic purposes. The compounds can be TLR agonists, such as TLR7 or TLR8 agonists. The compounds can be included in pharmaceutical compositions and used for therapies were being a TLR agonist is useful. The pharmaceutical compositions can include any ingredients, such as carries, diluents, excipients, fillers or the like that are common in pharmaceutical compositions. The compounds can be those illustrated or described herein as well as derivative thereof, prodrug thereof, salt thereof, or stereoisomer thereof, or having any chirality at any chiral center, or tautomer, polymorph, solvate, or combinations thereof. As such, the compounds can be used as adjuvants in vaccines as well as for other therapeutic purposes described herein. The compounds can have any one of the formulae. Examples of the compounds can be reviewed in Table 1 and Table A1 for activates.

Toll-like receptor agonists

The present disclosure provides novel imidazoquinoline derived compounds, derivatives thereof, analogues thereof, and pharmaceutically acceptable salts thereof, and methods of making and using such compounds. The present disclosure also provides TLR7 agonists and TLR7/TLR8 dual agonists, probes, tissue-specific molecules, adjuvants, immunogenic compositions, therapeutic compositions, and self-adjuvanting vaccines including the imidazoquinoline derived compounds, derivatives thereof, analogues thereof, and pharmaceutically acceptable salts thereof. Derivatives of the imidazoquinoline derived compounds also include dendrimers and dimers of the imidazoquinoline derived compounds, and methods of making and using the dendrimeric and dimeric imidazoquinoline derived compounds. The present disclosure also provides dual TLR2/TLR7 hybrid agonists that include imidazoquinoline derived compounds of the present disclosure.

Toll-like receptor-7 and -8 modulatory 1H imidazoquinoline derived compounds

The present disclosure is directed to a novel class of toll-like receptor 2-agonistic (TLR2) lipopeptide compounds having specific structures, and synthetic methods of making the compounds. These compounds provide high potency of agonistic activities with human, other than murine, TLR2, and are useful as vaccine adjuvants. Vaccines are perhaps one of the most successful medical interventions against infectious disease.

Toll-like receptor 2-agonistic lipopeptides, and method of making the same

The present disclosure provides novel imidazoquinoline derived compounds, derivatives thereof, analogues thereof, and pharmaceutically acceptable salts thereof, and methods of making and using such compounds. The present disclosure also provides TLR7 agonists and TLR7/TLR8 dual agonists, probes, tissue-specific molecules, adjuvants, immunogenic compositions, therapeutic compositions, and self-adjuvanting vaccines including the imidazoquinoline derived compounds, derivatives thereof, analogues thereof, and pharmaceutically acceptable salts thereof. Derivatives of the imidazoquinoline derived compounds also include dendrimers and dimers of the imidazoquinoline derived compounds, and methods of making and using the dendrimeic and dimeric imidazoquinoline derived compounds. The present disclosure also provides dual TLR2/TLR7 hybrid agonists that include imidazoquinoline derived compounds of the present disclosure.

[object Object]

Small molecule polycationic agents are used to modulate or interrupt biological processes by binding to oligosaccharide-based biomolecules. Compounds that inhibit nitric oxide, TNF&#x3b1; or other immunomodulators are provided and are useful for treating immunological disease and disease of an infectious disorder.

Recognition of oligosaccharide molecular targets by polycationic small molecule inhibitors and treatment of immunological disorders and infectious diseases

Certain lipophilic polycationic sulfonamides are provided and are useful for treating various diseases or conditions and particularly sepsis.

Polycationic sulfonamides and use thereof

Recognition of oligiosaccaride molecular targets by polycationic small molecule inhibitors and treatment of immunological disorders and infectious diseases

Growing community of inventors

Lawrence, KS, United States of America

Sunil Abraham David