公开(公告)号：US20180297983A1

公开(公告)日：2018-10-18

申请号：US15575583

申请日：2016-05-19

Applicant: GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED

Inventor： Dominique Amans ,  Stephen John Atkinson ,  Michael David Barker ,  Matthew Campbell ,  Hawa Diallo ,  Clement Douault ,  Neil Stuart Garton ,  John Liddle ,  Jessica Fanny Renaux ,  Robert John Sheppard ,  Ann Louise Walker ,  Christopher Roland Wellaway ,  David Matthew Wilson

IPC: C07D401/14 ,  C07D498/04 ,  C07D405/14 ,  C07D413/14 ,  C07D403/14

CPC classification number: C07D401/14 ,  C07D403/14 ,  C07D405/14 ,  C07D413/14 ,  C07D498/04 ,  C07D498/06

Abstract: Compounds of formula (I): wherein X, Y, R1 and R3-R11 are as herein defined, and salts thereof are PAD4 inhibitors and may be useful in the treatment of various disorders, for example rheumatoid arthritis, vasculitis, systemic lupus erythematosus, ulcerative colitis, cancer, cystic fibrosis, asthma, cutaneous lupus erythematosis, and psoriasis.

公开(公告)号：US10815218B2

公开(公告)日：2020-10-27

申请号：US16515735

申请日：2019-07-18

Applicant: GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED

Inventor： Dominique Amans ,  Stephen John Atkinson ,  Michael David Barker ,  Matthew Campbell ,  Hawa Diallo ,  Clement Douault ,  Neil Stuart Garton ,  John Liddle ,  Jessica Fanny Renaux ,  Robert John Sheppard ,  Ann Louise Walker ,  Christopher Roland Wellaway ,  David Matthew Wilson

IPC: C07D401/14 ,  C07D403/14 ,  C07D405/14 ,  C07D498/04 ,  C07D498/06 ,  C07D413/14

Abstract: Compounds of formula (I): wherein X, Y, R1 and R3-R11 are as herein defined, and salts thereof are PAD4 inhibitors and may be useful in the treatment of various disorders, for example rheumatoid arthritis, vasculitis, systemic lupus erythematosus, ulcerative colitis, cancer, cystic fibrosis, asthma, cutaneous lupus erythematosis, and psoriasis.

公开(公告)号：US10407407B2

公开(公告)日：2019-09-10

申请号：US15575583

申请日：2016-05-19

Applicant: GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED

Inventor： Dominique Amans ,  Stephen John Atkinson ,  Michael David Barker ,  Matthew Campbell ,  Hawa Diallo ,  Clement Douault ,  Neil Stuart Garton ,  John Liddle ,  Jessica Fanny Renaux ,  Robert John Sheppard ,  Ann Louise Walker ,  Christopher Roland Wellaway ,  David Matthew Wilson

IPC: C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D403/14 ,  C07D498/06 ,  C07D498/04

Abstract: Compounds of formula (I): wherein X, Y, R1 and R3-R11 are as herein defined, and salts thereof are PAD4 inhibitors and may be useful in the treatment of various disorders, for example rheumatoid arthritis, vasculitis, systemic lupus erythematosus, ulcerative colitis, cancer, cystic fibrosis, asthma, cutaneous lupus erythematosis, and psoriasis.

公开(公告)号：US09624219B2

公开(公告)日：2017-04-18

申请号：US15132274

申请日：2016-04-19

Applicant: GlaxoSmithKline Intellectual Property Development Limited

Inventor： Jose-Miguel Coteron Lopez ,  Esther Pilar Fernandez Velando ,  Jorge Fernandez-Molina ,  Maria Luisa Leon-Diaz ,  David Matthew Wilson

IPC: C07D471/04 ,  A61K31/519 ,  A61K45/06

CPC classification number: C07D471/04 ,  A61K31/519 ,  A61K45/06

Abstract: The present invention relates to a compound of Formula (I) having pharmacological activity, processes for its preparation, pharmaceutical compositions and their use in the treatment of certain parasitic certain parasitic protozoal infections such as malaria, in particular infection by Plasmodium falciparum. (S)—N-(2-fluoropyridin-4-yl)-3-methyl-2-(5-methyl-2,4-dioxo-1,2-dihydropyrido[3,4-d]pyrimidin-3(4H)-yl)butanamide.