157701-33-2Relevant academic research and scientific papers
Synthesis of bromoaminoindane and bromoaminoindanone derivatives
Yilmaz, Makbule,Tutar, Ahmet,Erenler, Ramazan
, p. 232 - 235 (2013)
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.
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 (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.
COMPOUNDS AND METHODS FOR IDO AND TDO MODULATION, AND INDICATIONS THEREFOR
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Paragraph 0384, (2019/10/15)
Disclosed are compounds of Formula (I) and (Ia) or a pharmaceutically acceptable salt, a solvate, a tautomer, a stereoisomer or a deuterated analog thereof, wherein R4, R5, R6, and R7 are as described in any of the embodiments described in this disclosure; compositions thereof; and uses thereof.
PYRAZOLO[1,5a]PYRIMIDINE DERIVATIVES AS IRAK4 MODULATORS
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, (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.
COMPOUNDS AND METHODS FOR IDO AND TDO MODULATION, AND INDICATIONS THEREFOR
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Paragraph 0519, (2018/04/20)
Disclosed are compounds of Formula I (a) or a pharmaceutically acceptable salt, a solvate, a tautomer, an isomer or a deuterated analog thereof, wherein R4, R5, R6, R7, G1, G2 and Ring A are as described in any of the embodiments described in this disclosure; compositions thereof; and uses thereof.
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.
BICYCLIC DERIVATIVES AND PHARMACEUTICAL COMPOSITION INCLUDING THE SAME
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, (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
5, 6-RING ANNULATED INDOLE DERIVATIVES AND USE THEREOF
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, (2010/12/31)
The present invention relates to 5,6-ring annulated indole derivatives of the formula (I), compositions comprising at least one 5,6-ring annulated indole derivatives, and methods of using the 5,6-ring annulated indole derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.
A structure-guided approach to an orthogonal estrogen-receptor-based gene switch activated by ligands suitable for in vivo studies
Kinzel, Olaf,Fattori, Daniela,Muraglia, Ester,Gallinari, Paola,Nardi, Maria Chiara,Paolini, Chantal,Roscilli, Giuseppe,Toniatti, Carlo,Gonzalez Paz, Odalys,Laufer, Ralph,Lahm, Armin,Tramontano, Anna,Cortese, Riccardo,De Francesco, Raffaele,Ciliberto, Gennaro,Koch, Uwe
, p. 5404 - 5407 (2007/10/03)
A strategy to obtain a fully orthogonal estrogen-receptor-based gene switch responsive to molecules with acceptable pharmacological properties is presented. From a series of tetrahydrofluorenones active on the wild-type estrogen receptor (ER) an inactive
