Process for manufacture of (S)-N-(3-((2-((4-((1-acetylpyrrolidin-3-yl)(methyl)amino)phenyl)amino)-5-methoxypyrimidin-4-yl)oxy)phenyl)acrylamide, and formulations thereof

US12358895B2 · kind B2 · utility

Assignee

• ACEA Therapeutics, Inc. · US

Inventors

• Long Mao · San Diego, US
• Jia Liu · San Diego, US
• Yile CHEN · Zhejiang, CN
• Yuning Hua · Hangzhou City, CN
• Kunhua DONG · Hangzhou City, CN
• Liang CHEN · Shanghai, CN
• Bojie Weng · Zhejiang, CN
• Xiaopeng Mo · Zhejiang, CN
• Kongen Dai · Hangzhou City, CN
• Yimei Bao · Hangzhou City, CN
• Jian WU · Zhengzhou, CN
• Bin Liang · Bositenghu, CN
• Guanglin ZHOU · Hangzhou City, CN
• Zhen Wang · Shanghai, CN

Key dates

• Filing date: Aug 9, 2018
• Grant date: Jul 15, 2025
• Expiry date: Sep 15, 2040

Classification

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

Abstract

The invention relates to solid forms of certain N-(pyrimidinyloxy)acrylamide derivatives that are useful in the treatment of proliferation and immunological disorders and other diseases related to the dysregulation of kinases including EGFR (including HER), Alk, PDGFR, BLK, BMX/ETK, BTK, FLT3 (D835Y), ITK, JAK1, JAK2, JAK3, TEC and TXK. The invention provides methods of making these materials and their salts and polymorphs, and intermediates for preparing these materials, as well as pharmaceutical compositions comprising these materials. The solid forms and pharmaceutical compositions comprising them are useful to treat conditions including a proliferation disorder, a tumor, an inflammatory disease, an autoimmune disease, psoriasis, dry eye, rheumatoid arthritis, or lupus.