公开(公告)号：US20190175571A1

公开(公告)日：2019-06-13

申请号：US16326991

申请日：2017-08-31

Applicant: GLAXOSMITHKLINE INTELLECTUAL PROPERTY (NO.2) LIMITED

Inventor： Andrew BAXTER ,  John Alexander BROWN ,  David HIRST ,  Philip HUMPHREYS ,  Katherine Louise JONES ,  Vipulkumar Kantibhai PATEL

IPC: A61K31/4439 ,  A61P29/00 ,  A61P35/00 ,  A61K31/443 ,  A61K31/4433

Abstract: Compounds of formula (I) and salts thereof: wherein R1, R2, R3 and a are as defined herein. Compounds of formula (I) and salts thereof have been found to inhibit the binding of the BET family of bromodomain containing proteins to, for example, acetylated lysine residues and thus may have use in therapy, for example in the treatment of autoimmune and inflammatory diseases, such as rheumatoid arthritis; and cancers.

公开(公告)号：US20190202799A1

公开(公告)日：2019-07-04

申请号：US16327016

申请日：2017-08-31

Applicant: GLAXOSMITHKLINE INTELLECTUAL PROPERTY (No.2) LIMITED

Inventor： Andrew BAXTER ,  Rino Antonio BIT ,  John Alexander BROWN ,  David HIRST ,  Philip HUMPHREYS ,  Katherine Louise JONES ,  Vipulkumar Kantibhai PATEL

IPC: C07D401/04 ,  C07D401/14 ,  C07D413/14 ,  C07D405/14 ,  A61P29/00 ,  A61P37/02 ,  A61P19/02

CPC classification number: C07D401/04 ,  A61P19/02 ,  A61P29/00 ,  A61P37/02 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14

Abstract: Compounds of formula (I) and salts thereof: wherein R1, R2, R3, a, X1, X2, X3, X4, and X5 are as defined hereinbefore. Compounds of formula (I) and salts thereof have been found to inhibit the binding of the BET family of bromodomain containing proteins to, for example, acetylated lysine residues and thus may have use in therapy, for example in the treatment of autoimmune and inflammatory diseases, such as rheumatoid arthritis; and cancers.

公开(公告)号：US20160016966A1

公开(公告)日：2016-01-21

申请号：US14770922

申请日：2014-03-12

Applicant: GLAXOSMITHKLINE INTELLECTUAL PROPERTY (NO.2) LIMITED

Inventor： Dominique AMANS ,  Paul BAMBOROUGH ,  Michael David BARKER ,  Rino Antonio BIT ,  John Alexander BROWN ,  Matthew CAMPBELL ,  Neil Stuart GARTON ,  Matthew J. LINDON ,  Tracy Jane SHIPLEY ,  Natalie Hope THEODOULOU ,  Christopher Roland WELLAWAY ,  Susan Marie WESTAWAY

IPC: C07D491/048 ,  A61K31/4355 ,  A61K31/4545 ,  A61K31/5377 ,  A61K31/554 ,  A61K31/553 ,  A61K31/541 ,  A61K31/5025 ,  C07D519/00 ,  A61K31/496 ,  A61K31/551

CPC classification number: C07D491/048 ,  A61K31/4355 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/5025 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/551 ,  A61K31/553 ,  A61K31/554 ,  C07D519/00

Abstract: The present invention relates to novel compounds, pharmaceutical compositions containing such compounds and to their use in therapy.

Abstract translation: 本发明涉及新化合物，含有这些化合物的药物组合物及其在治疗中的用途。