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：US20210155606A1

公开(公告)日：2021-05-27

申请号：US17170690

申请日：2021-02-08

Applicant: NOVARTIS AG

Inventor： Luca ARISTA ,  Sreehari BABU ,  Jianwei BIAN ,  Kai CUI ,  Michael Patrick DILLON ,  Rene LATTMANN ,  Jialiang LI ,  Lv LIAO ,  Dimitrios LIZOS ,  Rita RAMOS ,  Nikolaus Johannes STIEFL ,  Thomas ULLRICH ,  Peggy USSELMANN ,  Xiaoyang WANG ,  Liladhar Murlidhar WAYKOLE ,  Sven WEILER ,  Yubo ZHANG ,  Yizong ZHOU ,  Tingying ZHU

IPC: C07D401/14 ,  C07D405/14 ,  C07D401/10 ,  C07D401/12 ,  C07D409/14 ,  C07D213/82 ,  C07D411/14 ,  C07D491/107 ,  A61P19/00 ,  C07D417/00 ,  C07D413/00 ,  C07D419/00 ,  A61P19/08 ,  C07D413/10 ,  C07D413/12 ,  C07D413/14 ,  C07D491/20

Abstract: The invention relates to a compound of formula (1) in free form or in pharmaceutically acceptable salt form to pharmaceutical compositions comprising said compound and to the use of said compound in the treatment of heterotopic ossification and fibrodysplasia ossificans progressiva.

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：US20200299265A1

公开(公告)日：2020-09-24

申请号：US16884666

申请日：2020-05-27

Applicant: NOVARTIS AG

Inventor： Luca ARISTA ,  Sreehari BABU ,  Jianwei BIAN ,  Kai CUI ,  Michael Patrick DILLON ,  Rene LATTMANN ,  Jialiang LI ,  Lv LIAO ,  Dimitrios LIZOS ,  Rita RAMOS ,  Nikolaus Johannes STIEFL ,  Thomas ULLRICH ,  Peggy USSELMANN ,  Xiaoyang WANG ,  Liladhar Murlidhar WAYKOLE ,  Sven WEILER ,  Yubo ZHANG ,  Yizong ZHOU ,  Tingying ZHU

IPC: C07D401/14 ,  C07D405/14 ,  C07D401/10 ,  C07D401/12 ,  C07D409/14 ,  C07D213/82 ,  C07D411/14 ,  C07D491/107 ,  A61P19/00 ,  C07D417/00 ,  C07D413/00 ,  C07D419/00 ,  A61P19/08 ,  C07D413/10 ,  C07D413/12 ,  C07D413/14 ,  C07D491/20

Abstract: The invention relates to a compound of formula (I) in free form or in pharmaceutically acceptable salt form to pharmaceutical compositions comprising said compound and to the use of said compound in the treatment of heterotopic ossification and fibrodysplasia ossificans progressiva.

公开(公告)号：US20190161474A1

公开(公告)日：2019-05-30

申请号：US16318250

申请日：2017-07-18

Applicant: NOVARTIS AG

Inventor： Luca ARISTA ,  Sreehari BABU ,  Jianwei BIAN ,  Kai CUI ,  Michael Patrick DILLON ,  Rene LATTMANN ,  Jialiang LI ,  Lv LIAO ,  Dimitrios LIZOS ,  Rita RAMOS ,  Nikolaus Johannes STIEFL ,  Thomas ULLRICH ,  Peggy USSELMANN ,  Xiaoyang WANG ,  Liladhar Murlidhar WAYKOLE ,  Sven WEILER ,  Yubo ZHANG ,  Yizong ZHOU ,  Tingying ZHU

IPC: C07D401/14 ,  C07D401/10 ,  C07D401/12 ,  C07D491/20 ,  C07D405/14 ,  C07D409/14 ,  C07D413/10 ,  C07D413/12 ,  C07D413/14 ,  A61P19/08

Abstract: The invention relates to a compound of formula (I) in free form or in pharmaceutically acceptable salt form (I) to pharmaceutical compositions comprising said compound and to the use of said compound in the treatment of heterotopic ossification and fibrodysplasia ossificans progressiva.