1258595-06-0Relevant articles and documents
Compounds and compositions as TLR activity modulators
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, (2018/05/04)
The invention provides a novel class of compounds, immunogenic compositions and pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with Toll-Like Receptors 7. In one aspect, the compounds are useful as adjuvants for enhancing the effectiveness of a vaccine.
Incorporation of Phosphonate into Benzonaphthyridine Toll-like Receptor 7 Agonists for Adsorption to Aluminum Hydroxide
Cortez, Alex,Li, Yongkai,Miller, Andrew T.,Zhang, Xiaoyue,Yue, Kathy,Maginnis, Jillian,Hampton, Janice,Hall, De Shon,Shapiro, Michael,Nayak, Bishnu,D'Oro, Ugo,Li, Chun,Skibinski, David,Mbow, M. Lamine,Singh, Manmohan,O'Hagan, Derek T.,Cooke, Michael P.,Valiante, Nicholas M.,Wu, Tom Y.-H.
, p. 5868 - 5878 (2016/07/06)
Small molecule Toll-like receptor 7 (TLR7) agonists have been used as vaccine adjuvants by enhancing innate immune activation to afford better adaptive response. Localized TLR7 agonists without systemic exposure can afford good adjuvanticity, suggesting peripheral innate activation (non-antigen-specific) is not required for immune priming. To enhance colocalization of antigen and adjuvant, benzonaphthyridine (BZN) TLR7 agonists are chemically modified with phosphonates to allow adsorption onto aluminum hydroxide (alum), a formulation commonly used in vaccines for antigen stabilization and injection site deposition. The adsorption process is facilitated by enhancing aqueous solubility of BZN analogs to avoid physical mixture of two insoluble particulates. These BZN-phosphonates are highly adsorbed onto alum, which significantly reduced systemic exposure and increased local retention post injection. This report demonstrates a novel approach in vaccine adjuvant design using phosphonate modification to afford adsorption of small molecule immune potentiator (SMIP) onto alum, thereby enhancing co-delivery with antigen.
IMMUNOLOGICALLY USEFUL ARGININE SALTS
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, (2013/09/26)
The invention is in the field of salt forms of an immunopotentiator compound and their formulation for in vivo use. In particular the invention relates to arginine salts.
COMPOUNDS AND COMPOSITIONS AS TLR ACTIVITY MODULATORS
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, (2011/04/14)
The invention provides a novel class of compounds, immunogenic compositions and pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with Toll-Like Receptors 7. In one aspect, the compounds are useful as adjuvants for enhancing the effectiveness of a vaccine.
