New Invention Profile
| Publication No: | IN202411016656 [India] | Application No: | IN202411016656 |
| Title: | Agonism-antagonism in endosomal TLRS by modulating chemical features in 8-oxopurine: process for preparation and application thereof | ||
| Publication Date: | 09-01-2026 | File Date: | 07-07-2024 |
| Inventor(s): | Talukdar Arindam; Ganguly Dipyaman; Sarkar Dipika; Pattanayak Shrestha; Dastidar Uddipta Ghosh; Bandopadhyay Purbita; Sinha Bishnu Prasad; Roy Shreya; Sarif Jafar; Rozario Ranit D; Ghosh Trisha; Das Rimica | ||
| IPC Classification: | C07D471/04, A61K31/4745, A61K45/06 | ||
| Abstract: | Toll-like receptors (TLRs) are integral components of the innate immune system, serving as key players in the recognition and response to microbial pathogens. TLR7, TLR8 and TLR9 are located inside the cell within the endosomal-lysosomal compartments, subsequently specialized for detecting microbial nucleic acids after microbes get phagocytosed and reach the endosomal compartments. The biological importance of TLR agonists lies in their ability to serve as powerful tools for studying innate immune responses, developing vaccines, and potential therapeutic applications. Additionally, TLR agonists have been explored as immunotherapies, whereas antagonists of these TLRs could serve as novel pathogenic node in different autoimmune disease contexts. Thus, both agonists and antagonists of these endosomal TLRs have therapeutic significance in different clinical context. The previous studies in 8-oxoadenine class depicted that the C-6 position -NH2 group is extremely important for recognition of the agonistic active site and subsequent interferon (IFN) induction. The present invention explores ability of 8-oxopurine derivatives, which does not contain the essential C-6 amine group and was replaced with hydrogen. The replacement of C-6 amino with a hydrogen (H) in 8-oxopurine derivatives provided exciting insight into these endosomal TLR modulation. The ability to modulate the endosomal TLRs by 8-oxopurine derivatives in correlation/interrelation with various substitution at N-7, N-9 and C-2 with all the derivatives containing hydrogen at C-6 were reported. | ||
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