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公开(公告)号：US20190142949A1
公开(公告)日：2019-05-16
申请号：US16244186
申请日：2019-01-10
Inventor： John Alexander BROWN , Katherine Louise Jones , Rabinder Kumar Prinjha , Jason Witherington
IPC: A61K47/54 , A61K31/4709 , A61K31/4439 , C07D405/14 , C07D401/12 , C07D401/04
Abstract: The present invention relates to covalent conjugates of BET inhibitors and alpha amino acid esters, processes for their preparation, compositions containing them, and to their use in the treatment of various disorders in particular inflammatory and autoimmune diseases, such as rheumatoid arthritis; and cancers.
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公开(公告)号：US20180044317A1
公开(公告)日：2018-02-15
申请号：US15559556
申请日：2016-03-17
Inventor： Rino Antonio BIT , John Alexander BROWN , Philip G HUMPHREYS , Katherine Louise JONES
IPC: C07D401/04 , C07D401/14 , C07D413/14 , C07D405/14
Abstract: Compounds of formula (I) and salts thereof: wherein R1, R2, R3, R4 are defined herein. Compounds of formula (I) and salts thereof have been found to inhibit the binding of the BET family of bromodomain 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.
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公开(公告)号：US20180117165A1
公开(公告)日：2018-05-03
申请号：US15559518
申请日：2016-03-17
Inventor： John Alexander BROWN , Katherine Louise JONES , Rabinder Kumar PRINJHA , Jason WITHERINGTON
IPC: A61K47/54 , A61K31/4439 , A61K31/4709
CPC classification number: A61K47/542 , A61K31/4439 , A61K31/4709 , A61K47/54 , C07D401/04 , C07D401/12 , C07D405/14
Abstract: The present invention relates to covalent conjugates of BET inhibitors and alpha amino acid esters, processes for their preparation, compositions containing them, and to their use in the treatment of various disorders in particular inflammatory and autoimmune diseases, such as rheumatoid arthritis; and cancers.
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