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Publication No: IN202311034982 [India] Application No: IN202311034982
Title: Protacs for ASK1 protein degradation: preparation and use thereof
Publication Date: 22-11-2024 File Date: 18-05-2023
Inventor(s): Arindam Talukdar; Himadri Sekhar Sarkar; Partha Chakrabarti; Israful Hoque; Abhishek Sen; Uddipta Ghosh Dastidar; Anindita Dey
IPC Classification: A61P 1/16, A61P 9/00, C07D 401/14, A61K 45/06, A61P 3/00
Abstract:
The present invention relates to the preparation of substituted triazole-5-yl(pyridine-2-yl)benzamides compounds, having structure I, in free form or an acceptable salt  form for the targeted degradation of Apoptosis Signal-regulating Kinase 1 (ASK 1) as a potential therapeutic target for improves Nonalcoholic Fatty Liver Disease  (NAFLD)/ Nonalcoholic Steatohepatitis (NASH). More particularly, the invention relates to small molecules where R1, R2, and R3 are as defined in the description,  capable of targeted degradation of ASK1, which may ultimately be used to achieve improved human health in patients with hepatic fibrosis. The present disclosure  represents the benchmark of this PROTAC technology for a potential therapeutic target protein ASK1 and will bring a breakthrough in NAFLD/NASH research.
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Industrial Applications Chemistry, Chemical Processes Polymers [Chemistry, Chemical Processes] Synhtesis Procesess [Drugs and Pharmaceuticals]