公开(公告)号：US20250092053A1

公开(公告)日：2025-03-20

申请号：US18966276

申请日：2024-12-03

Applicant: GlaxoSmithKline Intellectual Property Development Limited

Inventor： Adam K. CHARNLEY ,  Janos Botyanszki ,  Xiaoyang Dong ,  Philip Gareth Humphreys ,  Bryan Wayne King ,  Kimberly Katherine Marcus ,  Joseph Pero ,  Alexander Joseph Reif ,  Daohua Zhang ,  Attiq Rahman ,  Kenneth Allen Newlander ,  Kenneth Wiggall ,  Joshi Ramanjulu

IPC: C07D487/04 ,  C07D403/14 ,  C07D471/04 ,  C07D471/14 ,  C07F9/6561

Abstract: The present invention relates to compounds of Formula (I), compositions containing them, and to their use in the treatment of various disorders, in particular autoimmune, autoinflammatory or immune-mediated conditions, such as systemic lupus erythematosus (SLE), cutaneous lupus erythematosus (CLE) and lupus nephritis.

公开(公告)号：US10975056B2

公开(公告)日：2021-04-13

申请号：US16309121

申请日：2017-06-13

Applicant: GlaxoSmithKline Intellectual Property Development Limited ,  Cancer Research Technology Ltd.

Inventor： Nicholas David Adams ,  Andrew B. Benowitz ,  María Lourdes Rueda Benede ,  Karen Anderson Evans ,  David T Fosbenner ,  Bryan Wayne King ,  Mei Li ,  Juan Ignacio Luengo ,  William Henry Miller ,  Alexander Joseph Reif ,  Stuart Paul Romeril ,  Stanley J. Schmidt ,  Roger J. Butlin ,  Kristin M. Goldberg ,  Allan M. Jordan ,  Christopher S. Kershaw ,  Ali Raoof ,  Bohdan Waszkowycz

IPC: C07D401/12 ,  C07D401/04 ,  C07D213/73 ,  C07D213/74 ,  C07D413/14 ,  C07D417/12 ,  A61P37/00 ,  A61P35/00 ,  C07D401/14

Abstract: The invention is directed to substituted pyridine derivatives. Specifically, the invention is directed to compounds according to Formula (Iar): wherein Yar, X1ar, X2ar, R1ar, R2ar, R3ar, R4ar and R5ar are as defined herein; or a pharmaceutically acceptable salt or prodrug thereof. The compounds of the invention are selective inhibitors of DNMT1 and can be useful in the treatment of cancer, pre-cancerous syndromes, beta hemoglobinopathy disorders, sickle cell disease, sickle cell anemia, and beta thalassemia, and diseases associated with DNMT1 inhibition. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting DNMT1 activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.

公开(公告)号：US12247033B2

公开(公告)日：2025-03-11

申请号：US18586620

申请日：2024-02-26

Applicant: GlaxoSmithKline Intellectual Property Development Limited

Inventor： Adam K. Charnley ,  Janos Botyanszki ,  Xiaoyang Dong ,  Philip Gareth Humphreys ,  Bryan Wayne King ,  Kimberly Katherine Marcus ,  Joseph Pero ,  Alexander Joseph Reif ,  Daohua Zhang ,  Attiq Rahman ,  Kenneth Allen Newlander ,  Kenneth Wiggall ,  Joshi Ramanjulu

IPC: C07D487/04 ,  C07D403/14 ,  C07D471/04 ,  C07D471/14 ,  C07F9/6561

Abstract: The present invention relates to compounds of Formula (I), compositions containing them, and to their use in the treatment of various disorders, in particular autoimmune, autoinflammatory or immune-mediated conditions, such as systemic lupus erythematosus (SLE), cutaneous lupus erythematosus (CLE) and lupus nephritis.