Synthetic pathway to belzutifan and crystalline phases of synthetic intermediates

US11827614B2 · kind B2 · utility

Assignees

• Merck Sharp & Dohme LLC · US
• Werthenstein Biopharma GMBH · CH

Inventors

• Stephen M. Dalby · Hertford, GB
• Clinton Scott Shultz · Maplewood, US
• Chintal Desai · Flemington, US
• Joshua Lee · Sayreville Junction, US
• Zhiwei Chen · Nanhu, CN
• Jungchul Kim · Berkeley Heights, US
• Nastaran Salehi Marzijarani · Mahwah, US
• Tao Wang · Farmington, US
• Eric M. Phillips · Jersey City, US
• Patrick Larpent
• Het P. Patel · Groton, US
• Haiheng Guo · Shanghai, CN
• Xin Wang · Palo Alto, US
• Kangze Dai · Shanghai, CN
• Lu Chen · Shanghai, CN
• Teng Li · Beijing, CN
• Taotao Lu · Shanghai, CN
• Jianjun Duan · Shanghai, CN

Key dates

• Filing date: May 20, 2022
• Grant date: Nov 28, 2023
• Expiry date: Jun 7, 2042

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07B2200/13
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

The disclosure provides crystalline forms for certain synthetic intermediates for making belzutifan, a HIF-2α inhibitor, useful for the treatment of cancer. The disclosure also provides processes for isolating the crystalline forms.