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.

公开(公告)号：US20200031824A1

公开(公告)日：2020-01-30

申请号：US16495275

申请日：2018-03-29

Applicant: Novartis AG

Inventor： Fabrice Gallou ,  Philipp Lustenberger ,  Christian Mathes ,  Qiangbiao Pan ,  Benli Zou

IPC: C07D471/04 ,  B01J27/128 ,  B01J23/44

Abstract: This invention relates to novel processes for synthesizing [1-(4-Methanesulfonyl-2-trifluoromethyl-benzyl)-2-methyl-1H-pyrrolo[2,3-b]pyridin-3-yl]-acetic acid and to intermediates that are used in such processes.

公开(公告)号：US10251868B2

公开(公告)日：2019-04-09

申请号：US15876619

申请日：2018-01-22

Applicant: NOVARTIS AG

Inventor： Jun Cao ,  Bernhard Erb ,  Robin Alec Fairhurst ,  Arnaud Grandeury ,  Shinji Hatakeyama ,  Magdalena Koziczak-Holbro ,  Xinzhong Lai ,  Philipp Lustenberger ,  Bernd Ulrich Riebesehl ,  Nicola Tufilli ,  Thomas Ullrich ,  Xiang Wu ,  Jianguang Zhou

IPC: A61K31/428 ,  A61K31/167 ,  C07D277/68 ,  C07C53/10 ,  A61K45/06

Abstract: The present invention provides a compound of formula (I) in free form or in pharmaceutically acceptable salt form a method for manufacturing the compound of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and pharmaceutical compositions.

公开(公告)号：US10723735B2

公开(公告)日：2020-07-28

申请号：US16495275

申请日：2018-03-29

Applicant: Novartis AG

Inventor： Fabrice Gallou ,  Philipp Lustenberger ,  Christian Mathes ,  Qiangbiao Pan ,  Benli Zou

IPC: C07D471/04 ,  B01J23/44 ,  B01J27/128

Abstract: This invention relates to novel processes for synthesizing [1-(4-Methanesulfonyl-2-trifluoromethyl-benzyl)-2-methyl-1H-pyrrolo[2,3-b]pyridin-3-yl]-acetic acid and to intermediates that are used in such processes.

公开(公告)号：US09913828B2

公开(公告)日：2018-03-13

申请号：US15178579

申请日：2016-06-10

Applicant: Novartis AG

Inventor： Jun Cao ,  Bernhard Erb ,  Robin Alec Fairhurst ,  Arnaud Grandeury ,  Shinji Hatakeyama ,  Magdalena Koziczak-Holbro ,  Xinzhong Lai ,  Philipp Lustenberger ,  Bernd Ulrich Riebesehl ,  Nicola Tufilli ,  Thomas Ullrich ,  Xiang Wu ,  Jianguang Zhou

IPC: A61K31/428 ,  C07D277/68 ,  A61K45/06 ,  A61K31/167 ,  C07C53/10

CPC classification number: A61K31/428 ,  A61K31/167 ,  A61K45/06 ,  C07B2200/07 ,  C07C53/10 ,  C07D277/68 ,  Y02P20/55

Abstract: The present invention provides a compound of formula (I) in free form or in pharmaceutically acceptable salt form a method for manufacturing the compound of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and pharmaceutical compositions.

公开(公告)号：US11603363B2

公开(公告)日：2023-03-14

申请号：US17322409

申请日：2021-05-17

Applicant: Novartis AG

Inventor： Zichen Jia ,  Philipp Lustenberger ,  Marie Meyer ,  Massimo Moratto

IPC: C07D401/06

Abstract: Described herein is a crystalline hydrate form of LNP023 hydrochloride and to a process for its preparation. Furthermore, described herein is a pharmaceutical composition comprising the crystalline hydrate form of LNP023 hydrochloride, and at least one pharmaceutically acceptable excipient. The pharmaceutical composition described herein can be used to treat a disease and disorder mediated by complement activation.