59856-06-3Relevant articles and documents
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.
supporting information, p. 327 - 333 (2019/12/02)
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 247, (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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Page/Page column 747; 748, (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.
INHIBITORS OF THE RENAL OUTER MEDULLARY POTASSIUM CHANNEL
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Paragraph 0102, (2016/09/26)
no abstract published
Synthesis and biological evaluation of 2-aryliminopyrrolidines as selective ligands for I1 imidazoline receptors: Discovery of new sympatho-inhibitory hypotensive agents with potential beneficial effects in metabolic syndrome
Gasparik, Vincent,Greney, Hugues,Schann, Stephan,Feldman, Josiane,Fellmann, Lyne,Ehrhardt, Jean-Daniel,Bousquet, Pascal
supporting information, p. 878 - 887 (2015/01/30)
New 2-aryliminopyrrolidines (1-18) were synthesized and tested for their binding properties on I1 imidazoline receptors vs α2-adrenergic receptors and their blood pressure effects after both systemic and intracerebral administrations
BICYCLIC DERIVATIVES AND PHARMACEUTICAL COMPOSITION INCLUDING THE SAME
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Page/Page column 22, (2016/04/26)
The present invention relates to a novel bicyclic derivative that has an inhibitory activity against sodium-glucose linked transporters (SGLTs) present in the intestines and kidneys, or a pharmaceutically acceptable salt, isomer, hydrate or solvate thereo
INHIBITORS OF THE RENAL OUTER MEDULLARY POTASSIUM CHANNEL
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Page/Page column 91, (2014/07/08)
The present invention provides compounds of Formula I and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kirl.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and conditions associated with excessive salt and water retention.
Synthesis of bromoaminoindane and bromoaminoindanone derivatives
Yilmaz, Makbule,Tutar, Ahmet,Erenler, Ramazan
, p. 232 - 235 (2013/07/05)
The bromination reactions of 5-aminoindane, 5-acetamidoindane, and 5-acetamidoindan-1-one were investigated using NBS, molecular bromine and photobromination, and the optimum reaction conditions were presented. The reaction of 5-aminoindane with glacial acetic acid at reflux temperature resulted in the formation of 5-acetamidoindane in high yield. 5-Acetamidoindan-1-one was generated by the reaction of 5-acetamidoindane with CrO3 in acetic acid. Selective bromination at C-6 position of 5-acetamidoindane was achieved by treatment of title compound with bromine in acetic acid and thus afforded 5-acetamido-6-bromoindane. Further bromination reactions of bromoindanones were achieved in various reaction conditions.
INHIBITORS OF THE RENAL OUTER MEDULLARY POTASSIUM CHANNEL
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Page/Page column 44; 45, (2013/05/21)
The present invention provides compounds of Formula (I) and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir 1.1) channel. The compounds act as diuretics and natriuretics and are valuable pharmaceutically active compounds for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension and conditions resulting from excessive salt and water retention.