HETEROARYL CARBOXAMIDE COMPOUNDS AS INHIBITORS OF RIPK2
The present invention relates to compounds of formula (I): or pharmaceutically acceptable salts thereof, wherein R1, R2, X, Y, and HET are as defined herein. The invention also relates to pharmaceutical compositions comprising these
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Paragraph 0316
(2018/03/25)
PYRIDINE AND PYRAZINE COMPOUNDS AS INHIBITORS OF RIPK2
The present invention relates to compounds of formula (I): or pharmaceutically acceptable salts thereof, wherein R1, R2, X, Y, and HET are as defined herein. The invention also relates to pharmaceutical compositions comprising these
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Paragraph 0248; 0249
(2018/05/03)
PYRROLO[2,3-D]PYRIMIDINE DERIVATIVES, PROCESS FOR THEIR PREPARATION AND THEIR USE AS KINASE INHIBITORS
The present invention relates to 6-amino-7-deaza-purine derivatives which modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity, in particular RET family kinases. The present
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Page/Page column 48; 49
(2014/12/12)
p38α mitogen-activated protein kinase inhibitors: Optimization of a series of biphenylamides to give a molecule suitable for clinical progression
p38α MAP kinase is a key anti-inflammatory target for rheumatoid arthritis, influencing biosynthesis of pro-inflammatory cytokines TNFα and IL-1β at a translational and transcriptional level. In this paper, we describe how we have optimized a series of no
Aston, Nicola M.,Bamborough, Paul,Buckton, Jacqueline B.,Edwards, Christopher D.,Holmes, Duncan S.,Jones, Katherine L.,Patel, Vipulkumar K.,Smee, Penny A.,Somers, Donald O.,Vitulli, Giovanni,Walker, Ann L.
experimental part
p. 6257 - 6269
(2010/03/31)
Biphenyl amide p38 kinase inhibitors 3: Improvement of cellular and in vivo activity
The biphenyl amides (BPAs) are a novel series of p38α MAP kinase inhibitor. The optimisation of the series to give compounds that are potent in an in vivo disease model is discussed. SAR is presented and rationalised with reference to the crystallographic binding mode.
Angell, Richard,Aston, Nicola M.,Bamborough, Paul,Buckton, Jacky B.,Cockerill, Stuart,deBoeck, Suzanne J.,Edwards, Chris D.,Holmes, Duncan S.,Jones, Katherine L.,Laine, Dramane I.,Patel, Shila,Smee, Penny A.,Smith, Kathryn J.,Somers, Don O.,Walker, Ann L.
scheme or table
p. 4428 - 4432
(2009/04/06)
BICYCLIC DERIVATIVES AS P38 KINASE INHIBITORS
New bicyclic derivatives of formula (I), wherein the meanings for the various substituents are as disclosed in the description. These compounds are useful as p38 kinase inhibitors.
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Page/Page column 51
(2008/06/13)
HETEROARYL-SUBSTITUTED ALKYNE COMPOUNDS AND METHOD OF USE
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Page/Page column 95-96
(2010/11/08)
P-38 kinase inhibitors
Compounds and compositions for modulating the activity of p38 kinases are provided, including p38α and p38β kinase. Methods for treating, preventing or ameliorating one or more symptoms of a p38 kinase mediated disease or disorder are also provided.
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Page/Page column 16
(2008/06/13)
HETEROARYL SUBSTITUTED BIPHENYL DERIVATIVES AS P38 KINASE INHIBITORS
Compounds of formula (I) are inhibitors of p38 kinase and are useful in the treatment of conditions or disease states mediated by p38 kinase activity or mediated by cytokines produced by the activity of p38.
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Page/Page column 26
(2010/02/07)
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