公开(公告)号：US20240228503A1

公开(公告)日：2024-07-11

申请号：US18586620

申请日：2024-02-26

申请人： GlaxoSmithKline Intellectual Property Development Limited

发明人： 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分类号： C07D487/04 ,  C07D403/14 ,  C07D471/04 ,  C07D471/14 ,  C07F9/6561

CPC分类号： C07D487/04 ,  C07D403/14 ,  C07D471/04 ,  C07D471/14 ,  C07F9/6561

摘要： 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.

公开(公告)号：US20240180933A1

公开(公告)日：2024-06-06

申请号：US18358998

申请日：2023-07-26

申请人： GlaxoSmithKline Intellectual Property Development Limited

发明人： Andrew B. BENOWITZ ,  David T. FOSBENNER ,  Bryan Wayne KING ,  Stuart Paul ROMERIL

IPC分类号： A61K31/675 ,  A61K31/44 ,  A61P35/02 ,  C07D213/85 ,  C07F9/58

CPC分类号： A61K31/675 ,  A61K31/44 ,  A61P35/02 ,  C07D213/85 ,  C07F9/58 ,  C07B2200/13

摘要： The invention relates to substituted pyridine derivatives that are inhibitors of the activity of DNA methyltransferase 1 (DNMT1). The invention also relates to pharmaceutical compositions comprising such compounds and methods of using such compounds in the treatment of cancer, pre-cancerous syndromes, beta haemoglobinopathy disorders, and other diseases associated with inappropriate DNMT1 activity.

公开(公告)号：US20170008878A1

公开(公告)日：2017-01-12

申请号：US15271581

申请日：2016-09-21

申请人： GlaxoSmithKline Intellectual Property Development Limited

发明人： Deepak BANDYOPADHYAY ,  Patrick M. EIDAM ,  Peter J. GOUGH ,  Philip Anthony HARRIS ,  Jae U. JEONG ,  Jianxing KANG ,  Bryan Wayne KING ,  Ami LAKDAWALA SHAH ,  Lara Kathryn LEISTER ,  Robert W. MARQUIS, JR. ,  Attiq RAHMAN ,  Joshi M. RAMANJULU ,  Clark A. SEHON ,  Robert SINGHAUS, JR. ,  Daohua ZHANG

IPC分类号： C07D403/12

CPC分类号： A61K31/553 ,  A61K31/55 ,  C07D223/08 ,  C07D267/14 ,  C07D281/10 ,  C07D403/12 ,  C07D403/14 ,  C07D409/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D487/04 ,  C07D498/04

摘要： Disclosed are compounds having the formula: wherein X, Y, Z1, Z2, Z3, Z4, R5, RA, m, A. L, and B are as defined herein, and methods of making and using the same.

摘要翻译： 其中X，Y，Z 1，Z 2，Z 3，Z 4，R 5，RA，m，A L和B如本文所定义，以及制备和使用它们的方法。

公开(公告)号：US20190194166A1

公开(公告)日：2019-06-27

申请号：US16309121

申请日：2017-06-13

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

发明人： 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分类号： C07D401/12 ,  C07D417/12 ,  A61P35/00 ,  A61P37/00

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

摘要： 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：US20150353533A1

公开(公告)日：2015-12-10

申请号：US14763183

申请日：2014-02-14

申请人： GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED

发明人： Deepak BANDYOPADHYAY ,  Patrick M. EIDAM ,  Peter J. GOUGH ,  Philip Anthony HARRIS ,  Jae U. JEONG ,  Jianxing KANG ,  Bryan Wayne KING ,  Ami LAKDAWALA SHAH ,  Lara Kathryn LEISTER ,  Robert W. MARQUIS, JR. ,  Attiq RAHMAN ,  Joshi M. RAMANJULU ,  Clark A. SEHON ,  Robert SINGHAUS, JR. ,  Daohua ZHANG

IPC分类号： C07D413/12 ,  C07D403/12

CPC分类号： A61K31/553 ,  A61K31/55 ,  C07D223/08 ,  C07D267/14 ,  C07D281/10 ,  C07D403/12 ,  C07D403/14 ,  C07D409/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D487/04 ,  C07D498/04

摘要： Disclosed are compounds having the formula: wherein X, Y, Z1, Z2, Z3, Z4, R5, RA, m, A, L, and B are as defined herein, and methods of making and using the same.

摘要翻译： 公开了具有下式的化合物：其中X，Y，Z1，Z2，Z3，Z4，R5，RA，m，A，L和B如本文所定义，以及制备和使用它们的方法。