34583-83-0Relevant academic research and scientific papers
BENZOLACTAM COMPOUNDS AS PROTEIN KINASE INHIBITORS
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Page/Page column 272; 273, (2017/08/01)
The invention provides a compound of formula (0): or a pharmaceutically acceptable salt, N-oxide or tautomer thereof. The compounds are inhibitors of ERK 1/2 kinases and will be useful in the treatment of ERKl/2-mediated conditions. The compounds are therefore useful in therapy, in particular in the treatment of cancer.
HETEROARYL COMPOUNDS AND USES THEREOF
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Paragraph 00827-00830, (2016/06/28)
The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same. It has now been found that compounds of this invention, and pharmaceutically acceptable compositions thereof, are effective as inhibitors of one or more protein kinases. Such compounds have general formula I or a pharmaceutically acceptable salt thereof, wherein Ring A, Ring B, W, Ry, R3 and R4 are as defined herein.
HETEROCYCLIC COMPOUNDS AS AXL INHIBITORS
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, (2016/01/15)
Compounds of Formula I and their uses of effective AXL inhibitors and for the treatment of physical condition mediated by AXL.
Fragment-based discovery of type i inhibitors of maternal embryonic leucine zipper kinase
Johnson, Christopher N.,Berdini, Valerio,Beke, Lijs,Bonnet, Pascal,Brehmer, Dirk,Coyle, Joseph E.,Day, Phillip J.,Frederickson, Martyn,Freyne, Eddy J. E.,Gilissen, Ron A. H. J.,Hamlett, Christopher C. F.,Howard, Steven,Meerpoel, Lieven,McMenamin, Rachel,Patel, Sahil,Rees, David C.,Sharff, Andrew,Sommen, Franois,Wu, Tongfei,Linders, Joannes T. M.
supporting information, p. 25 - 30 (2015/01/30)
Fragment-based drug design was successfully applied to maternal embryonic leucine zipper kinase (MELK). A low affinity (160 μM) fragment hit was identified, which bound to the hinge region with an atypical binding mode, and this was optimized using structure-based design into a low-nanomolar and cell-penetrant inhibitor, with a good selectivity profile, suitable for use as a chemical probe for elucidation of MELK biology.
BENZAZEPINES AS SEROTONIN 5-HT2C RECEPTOR LIGANDS AND USES THEREOF
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Paragraph 000187, (2014/07/08)
The present invention generally relates to a series of compounds, to pharmaceutical compositions containing the compounds, and to use of the compounds and compositions as therapeutic agents. More specifically, compounds of the present invention are benzaz
Synthesis and SAR of aminothiazole fused benzazepines as selective dopamine D2 partial agonists
Urbanek, Rebecca A.,Xiong, Hui,Wu, Ye,Blackwell, William,Steelman, Gary,Rosamond, Jim,Wesolowski, Steven S.,Campbell, James B.,Zhang, Minli,Brockel, Becky,Widzowski, Daniel V.
, p. 543 - 547 (2013/02/25)
Dopamine (D2) partial agonists (D2PAs) have been regarded as a potential treatment for schizophrenia patients with expected better side effect profiles than currently marketed antipsychotics. Herein we report the synthesis and SAR of a series of aminothiazole fused benzazepines as selective D 2 partial agonists. These compounds have good selectivity, CNS drug-like properties and tunable D2 partial agonism. One of the key compounds, 8h, has good in vitro/in vivo ADME characteristics, and is active in a rat amphetamine-induced locomotor activity model.
Efficient and scalable synthesis of thiazole fused benzazepine as a D2 partial agonist
Xiong, Hui,Wu, Ye,Lehr, Scott G.,Blackwell, William,Steelman, Gary,Hulsizer, Jim,Urbanek, Rebecca A.
, p. 5833 - 5836,4 (2020/07/31)
The development of an efficient and scalable synthetic route to prepare the selective D2 partial agonist (1) is described here. Regioselective nitration of tetrahydrobenzazepine 2, followed by reductive amination, hydrogenation, and oxidative cyclization
2,4-Diaminopyrimidine inhibitors of c-Met kinase bearing benzoxazepine anilines
Zificsak, Craig A.,Theroff, Jay P.,Aimone, Lisa D.,Albom, Mark S.,Angeles, Thelma S.,Brown, Rebecca A.,Galinis, Deborah,Grobelny, Jennifer V.,Herbertz, Torsten,Husten, Jean,Kocsis, Laura S.,Losardo, Christine,Miknyoczki, Sheila J.,Murthy, Seetha,Rolon-Steele, Damaris,Underiner, Ted L.,Wells-Knecht, Kevin J.,Worrell, Candace S.,Zeigler, Kelli S.,Dorsey, Bruce D.
scheme or table, p. 660 - 663 (2011/03/18)
Elaboration of the SAR around a series of 2,4-diaminopyrimidines led to a number of c-Met inhibitors in which kinase selectivity was modulated by substituents appended on the C4-aminobenzamide ring and the nature of the C2-aminoaryl ring. Further lead opt
SUBSTITUTED GLYCINAMIDES, PROCESS FOR THEIR MANUFACTURE AND USE THEREOF AS MEDICAMENTS
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Page/Page column 17, (2010/09/05)
The present invention relates to new substituted glycinamides of general formula (I) wherein D, M, R3, R4 and R5 are defined as in the specification, the tautomers, enantiomers, diastereomers, mixtures and salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties.
7-Sulfonamido-3-benzazepines as potent and selective 5-HT2C receptor agonists: Hit-to-lead optimization
Fish, Paul V.,Brown, Alan D.,Evrard, Edel,Roberts, Lee R.
scheme or table, p. 1871 - 1875 (2009/12/03)
New 7-sulfonamido-3-benzazepines 3 are disclosed as 5-HT2C receptor agonists. Appropriate substitution of the amino group (R1R2N-) gave compounds that were potent 5-HT2C agonists with minimal activation of the 5-HT2A and 5-HT2B receptors. Furthermore, representative examples had excellent in vitro ADME properties and good selectivity over ion channel activity.
