公开(公告)号：US12084460B2

公开(公告)日：2024-09-10

申请号：US17056351

申请日：2019-05-16

Applicant: NOVARTIS AG

Inventor： Nicole Bieri ,  Andreas Kordikowski ,  Bin Li ,  Philipp Lustenberger ,  Rita Ramos ,  Vijay Sethuraman ,  Sisi Zhang

IPC: A61K31/4162 ,  A61K31/5377 ,  A61K45/06 ,  C07D231/00 ,  C07D519/00 ,  A61K31/437 ,  C07D265/30 ,  C07D487/04

CPC classification number: C07D519/00 ,  A61K31/4162 ,  A61K31/5377 ,  A61K45/06 ,  C07D231/00 ,  A61K31/437 ,  C07B2200/13 ,  C07D265/30 ,  C07D487/04

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.