公开(公告)号：US20190194166A1

公开(公告)日：2019-06-27

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 ,  Kristen M. GOLDBERG ,  Allan M. JORDAN ,  Christopher S. KERSHAW ,  Ali RAOOF ,  Bohdan WASZKOWYCS

IPC: C07D401/12 ,  C07D417/12 ,  A61P35/00 ,  A61P37/00

CPC classification number: C07D401/12 ,  A61P35/00 ,  A61P37/00 ,  C07D213/73 ,  C07D213/74 ,  C07D401/04 ,  C07D401/14 ,  C07D413/14 ,  C07D417/12

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：US20240228503A1

公开(公告)日：2024-07-11

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(Deceased) ,  Kenneth Allen NEWLANDER ,  Kenneth WIGGALL ,  Joshi RAMANJULU

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

CPC classification number: C07D487/04 ,  C07D403/14 ,  C07D471/04 ,  C07D471/14 ,  C07F9/6561

Abstract: The present invention relates to compounds, 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.