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Publication No: EP4346786 [Europe] Application No: EP2022815524
Title: Small molecule modulator targeting a rare histone modification regulating adipogenesis and pharmaceutical formulation thereof
Publication Date: 30-07-2025 File Date: 02-06-2022
Inventor(s): Kundu, Tapas Kumar; Bhattacharya, Aditya; Chatterjee, Sourav; Koneni, Venkata Sashidhara; Singh, Suriya Pratap; Mishra, Prabhat Ranjan; Nazir, Aamir; Guha, Rajdeep
IPC Classification: A61K0031122, C07D031178
Abstract: The present invention relates to substituted benzophenones of structural Formula I employed as small molecule inhibitor for controlling obesity. The present invention further relates to screening of small molecule inhibitors against p300 which selectively targets histone butyrylation thereby specifically inhibiting adipogenesis further aiding to prevention of weight gain. The present invention reveals that histone butyrylation increases during adipogenesis. Hence, inhibition of histone butyrylation by a small molecule inhibitor would be a promising therapeutic strategy to control obesity. Significantly, besides inhibiting adipogenesis in cellular model, it also prevents weight gain in high fat diet based mouse model system, indicating the possible use of the scaffold for obesity control.
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Industrial Applications Animals [Biological Science] Biomolecules [Biological Science] Diagnostics [Medical Devices and Diagnostics]