公开(公告)号：US20210206783A1

公开(公告)日：2021-07-08

申请号：US17056351

申请日：2019-05-16

Applicant: NOVARTIS AG

Inventor： Nicole BIERI ,  Andreas KORDIKOWSKI ,  Bin LI ,  Pilipp LUSTENBERGER ,  Rita RAMOS ,  Vijay SETHURAMAN ,  Sisi ZHANG

IPC: C07D519/00 ,  A61K45/06

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.

公开(公告)号：US20240245694A1

公开(公告)日：2024-07-25

申请号：US18483651

申请日：2023-10-10

Applicant: Novartis AG

Inventor： Vincent BORDAS ,  Markus FUREGATI ,  Jacques HAMON ,  Jürgen Hans-Hermann HINRICHS ,  Ziyue HONG ,  Fabio LIMA ,  Fatma LIMAM ,  Henrik MOEBITZ ,  Sandro NOCITO ,  Niko SCHMIEDEBERG ,  Joseph SCHOEPFER ,  Ross Sinclair STRANG ,  Frédéric ZECRI ,  Huangchao YU ,  Yong ZHANG ,  Xinkan YANG ,  Sisi ZHANG ,  Wei LI

IPC: A61K31/5377 ,  A61K31/519 ,  C07D487/14 ,  C07D519/00

CPC classification number: A61K31/5377 ,  A61K31/519 ,  C07D487/14 ,  C07D519/00

Abstract: The present invention provides a compound, or a pharmaceutically acceptable salt thereof, of formula (I):




wherein R1, R2, R3, x, R4, R5, y, R, M, W, L, V, T, Y, J, K and A are as described herein, therapeutic uses of said compounds, uses of said compounds as research chemicals, a pharmaceutical composition and combinations comprising said compounds, and methods for manufacturing the compounds of the invention.

公开(公告)号：US20240391938A1

公开(公告)日：2024-11-28

申请号：US18795371

申请日：2024-08-06

Applicant: Novartis AG

Inventor： Nicole BIERI ,  Andreas KORDIKOWSKI ,  Bin LI ,  Philipp LUSTENBERGER ,  Rita RAMOS ,  Vijay SETHURAMAN ,  Sisi ZHANG

IPC: C07D519/00 ,  A61K31/4162 ,  A61K31/437 ,  A61K31/5377 ,  A61K45/06 ,  C07D231/00 ,  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.

公开(公告)号：US20240360118A1

公开(公告)日：2024-10-31

申请号：US18506164

申请日：2023-11-10

Applicant: Novartis AG

Inventor： Vincent BORDAS ,  Jvan BRUN ,  Andrea DECKER ,  Markus FUREGATI ,  Geoffrey GOGNIAT ,  Wanben GONG ,  Jacques HAMON ,  Jürgen Hans-Hermann HINRICHS ,  Philipp HOLZER ,  Fatma LIMAM ,  Henrik MÖBITZ ,  Sandro NOCITO ,  Simone PLATTNER ,  Niko SCHMIEDEBERG ,  Joseph SCHOEPFER ,  Jessica SOTO ,  Ross Sinclair STRANG ,  Shuping YAO ,  Huangchao YU ,  Frédéric ZECRI ,  Sisi ZHANG

IPC: C07D413/14 ,  C07D401/14 ,  C07D405/14

CPC classification number: C07D413/14 ,  C07D401/14 ,  C07D405/14 ,  C07B2200/13

Abstract: The present invention provides a compound, or a pharmaceutically acceptable salt thereof, of formula (I):




wherein R1, R2, R3, R4, R5, R26, R27, y, R, M, W, L, V, T, Y, J, K and A are as described herein, therapeutic uses of said compounds, uses of said compounds as research chemicals, a pharmaceutical composition and combinations comprising said compounds, and methods for manufacturing the compounds of the invention.

公开(公告)号：US20230046859A1

公开(公告)日：2023-02-16

申请号：US17824407

申请日：2022-05-25

Applicant: NOVARTIS AG

Inventor： Vincent BORDAS ,  Jvan BRUN ,  Andrea DECKER ,  Markus FUREGATI ,  Geoffrey GOGNIAT ,  Wanben GONG ,  Jacques HAMON ,  Jürgen Hans-Hermann HINRICHS ,  Philipp HOLZER ,  Fatma LIMAM ,  Henrik MÖBITZ ,  Sandro NOCITO ,  Simone PLATTNER ,  Niko SCHMIEDEBERG ,  Joseph SCHOEPFER ,  Jessica SOTO ,  Ross Sinclair STRANG ,  Shuping YAO ,  Huangchao YU ,  Frédéric ZECRI ,  Sisi ZHANG

IPC: C07D413/14 ,  C07D401/14 ,  C07D405/14

Abstract: The present invention provides a compound, or a pharmaceutically acceptable salt thereof, of formula (I): wherein R1, R2, R3, R4, R5, R26, R27, y, R, M, W, L, V, T, Y, J, K and A are as described herein, therapeutic uses of said compounds, uses of said compounds as research chemicals, a pharmaceutical composition and combinations comprising said compounds, and methods for manufacturing the compounds of the invention.