Crystalline forms of a TLR7/TLR8 inhibitor

US12084460B2 · kind B2 · utility

Assignee

• Novartis AG · CH

Inventors

• Nicole Bieri · Zürich, CH
• Andreas Kordikowski · Binningen, CH
• Bin Li · Columbus, US
• Philipp Lustenberger · Warthausen, DE
• Rita RAMOS · Allschwil, CH
• Vijay SETHURAMAN · Fremont, US
• Sisi Zhang · Hoherlehmer Straße, CN

Key dates

• Filing date: May 16, 2019
• Grant date: Sep 10, 2024
• Expiry date: Jun 21, 2041

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D487/04
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

This application relates to various crystalline forms of (S)—N-(4-((5-(1,6-dimethyl-1H-pyrazolo[3,4-b]pyridin-4-yl)-3-methyl-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl)methyl)bicyclo[2.2.2]octan-1-yl)morpholine-3-carboxamide in its free form, as well as compositions, method of making and methods of using the same. In some embodiments the crystalline forms also contain water (“hydrates”). These materials are useful in the treatment of various autoimmune diseases, including systemic lupus erythematosus, cutaneous lupus, discoid lupus, mixed connective tissue disease, primary biliary cirrhosis, immune thrombocytopenia purpura, hidradenitis suppurativa, dermatomyositis, polymyositis, Sjögren's syndrome, arthritis, rheumatoid arthritis and psoriasis.