868049-68-7Relevant academic research and scientific papers
Discovery of Potent Benzolactam IRAK4 Inhibitors with Robust in Vivo Activity
Rajapaksa, Naomi S.,Gobbi, Alberto,Drobnick, Joy,Do, Steven,Kolesnikov, Aleksandr,Liang, Jun,Chen, Yongsheng,Sujatha-Bhaskar, Swathi,Huang, Zhiyu,Brightbill, Hans,Francis, Ross,Yu, Christine,Choo, Edna F.,Dement, Kevin,Ran, Yingqing,An, Le,Emson, Claire,Maher, Jonathan,Wai, John,McKenzie, Brent S.,Lupardus, Patrick J.,Zarrin, Ali A.,Kiefer, James R.,Bryan, Marian C.
, p. 327 - 333 (2020)
IRAK4 kinase activity transduces signaling from multiple IL-1Rs and TLRs to regulate cytokines and chemokines implicated in inflammatory diseases. As such, there is high interest in identifying selective IRAK4 inhibitors for the treatment of these disorders. We previously reported the discovery of potent and selective dihydrobenzofuran inhibitors of IRAK4. Subsequent studies, however, showed inconsistent inhibition in disease-relevant pharmacodynamic models. Herein, we describe application of a human whole blood assay to the discovery of a series of benzolactam IRAK4 inhibitors. We identified potent molecule 19 that achieves robust in vivo inhibition of cytokines relevant to human disease.
PYRAZOLO[1,5a]PYRIMIDINE DERIVATIVES AS IRAK4 MODULATORS
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Page/Page column 243, (2019/01/10)
Compounds of Formula (I), Formula (II), Formula (III), Formula (IV), Formula (V), Formula (VI), Formula (VII), Formula (VIII), and methods of use as lnterleukin-1 Receptor Associated Kinase (IRAK4) inhibitors are described herein.
PYRAZOLO[1,5a]PYRIMIDINE DERIVATIVES AS IRAK4 MODULATORS
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, (2017/07/14)
Compounds of Formula (0), Formula (I), and Formula (II) and methods of use as Interleukin-1 Receptor Associated Kinase (IRAK4) inhibitors are described herein.
Novel medicaments for the treatment of respiratory diseases
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Page/Page column 11, (2008/06/13)
The present invention relates to the use of the compounds of general formula 1 wherein the groups R1, R2 and R3 may have the meanings given in the claims and in the specification, for preparing a pharmaceutical composition
Aerosol formulation for the inhalation of beta-agonists
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Page/Page column 14, (2008/06/13)
The present invention relates to a propellant-free aerosol formulation which [contains] one or more compounds of general formula 1 wherein the groups R1, R2, R3 and X? may have the meanings given in the claims a
Novel medicament combinations for the treatment of respiratory diseases
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Page/Page column 36, (2008/06/13)
The present invention relates to new medicament combinations which contain in addition to one or more, preferably one, compound of general formula 1 wherein the groups R1, R2 and R3 may have the meanings given in the claim
