MUMBAI, India, Aug. 10 -- Intellectual Property India has published a patent application (202513002027 A) filed by Council Of Scientific And Industrial Research An Indian on January 08, 2025, for A Cost Effective Process For Preparation Of Nintedanib.
Inventors include Gautam Panda; Sabyasachi Halder; Sohini Chatterjee; and Souvik Barman.
The application for the patent was published on July 31, 2026, under issue no. 31/2026.
Abstract: Nintedanib, marketed as Ofev and Vargatev, is an FDA-approved tyrosine kinase inhibitor used to treat idiopathic pulmonary fibrosis and lung cancer. Initially developed by Boehringer Ingelheim and approved in 2014, it was later authorized by the EMA and PMDA for non-small cell lung cancer. The inventio ngn presents an alternative, efficient synthesis of Nintedanib using tandem or domino reaction conditions, reducing synthetic steps and chemical reagents for improved yield and cost- effectiveness. Starting from commercially available materials like methyl 3-amino-4-iodobenzoate and N-(4-aminophenyl)-N-methyl-2-(4-methylpiperazin-1- yl)acetamide, this process offers several advantages: fewer steps, eco-friendly solvents (e.g., toluene, DMF), mild reaction conditions, and cis-selectivity via Pd(0)- catalyzed Heck and Buchwald-Hartwig coupling reactions. This streamlined method addresses the challenges of scalability and low yields in previous approaches, making the production of Nintedanib more efficient and environmentally sustainable.
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