1071017-64-5Relevant academic research and scientific papers
6-6 FUSED BICYCLIC HETEROARYL COMPOUNDS AND THEIR USE AS LATS INHIBITORS
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Page/Page column 303; 304, (2018/11/22)
The present invention is related to 6-6 Fused Bicyclic Heteroaryl Compounds of the Formula A2 or A1 and their Use as LATS Inhibitors, or a salt, stereoisomer or pharmaceutical composition thereof; wherein the variables are as defined herein (A1 and A2). The present invention further relates to a method of LATS inhibition in a cell population using a compound of Formula A1, or a salt, stereoisomer or pharmaceutical composition thereof. The present invention further provides a method for manufacturing compounds of the invention, and its therapeutic uses. The invention further provides methods to their preparation, to their medical use, their use in the treatment and management of diseases or disorders.
Identification of orally available naphthyridine protein kinase D inhibitors
Meredith, Erik L.,Ardayfio, Ophelia,Beattie, Kimberly,Dobler, Markus R.,Enyedy, Istvan,Gaul, Christoph,Hosagrahara, Vinayak,Jewell, Charles,Koch, Keith,Lee, Wendy,Lehmann, HansJoerg,Mckinsey, Timothy A.,Miranda, Karl,Pagratis, Nikos,Pancost, Margaret,Patnaik, Anup,Phan, Dillon,Plato, Craig,Qian, Ming,Rajaraman, Vasumathy,Rao, Chang,Rozhitskaya, Olga,Ruppen, Thomas,Shi, Jie,Siska, Sarah J.,Springer, Clayton,Van Eis, Maurice,Vega, Richard B.,Von Matt, Anette,Yang, Lihua,Yoon, Taeyoung,Zhang, Ji-Hu,Zhu, Na,Monovich, Lauren G.
experimental part, p. 5400 - 5421 (2010/11/18)
A novel 2,6-naphthyridine was identified by high throughput screen (HTS) as a dual protein kinase C/D (PKC/PKD) inhibitor. PKD inhibition in the heart was proposed as a potential antihypertrophic mechanism with application as a heart failure therapy. As PKC was previously identified as the immediate upstream activator of PKD, PKD vs PKC selectivity was essential to understand the effect of PKD inhibition in models of cardiac hypertrophy and heart failure. The present study describes the modification of the HTS hit to a series of prototype pan-PKD inhibitors with routine 1000-fold PKD vs PKC selectivity. Example compounds inhibited PKD activity in vitro, in cells, and in vivo following oral administration. Their effects on heart morphology and function are discussed herein.
[2, 6] NAPHTHYRIDINES USEFUL AS PROTEIN KINASE INHIBITORS
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, (2008/12/04)
The present invention provides a compound of formula I: (formula I) said compound is inhibitor of selective subset of kinases belonging to the AGC or calmodulin kinase family, such as for example MARK1/2/3, PKD-1/2/3, PKN-1/2, CDK-9, CaMKII, ROCK-I/II, inhibitors of histone deacetylase (HDAC) phosphorylation, or inhibitors of other kinases. Finally, the present invention also provides a pharmaceutical composition.
2, 6-NAPHTHYRIDINE DERIVATIVES AS PROTEIN KINASE MODULATORS
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Page/Page column 18, (2008/12/04)
The present invention relates to novel organic compounds comprising a naphthyridine which may be mediators of a selective subset of kinases belonging to the AGC kinase family, such as for example PKC, PKD, PKN-1/2, CDK-9, MRCK-beat, PASK, PRKX, ROCK-I/II or mediators of other kinases, the selectivity of which would be depending on the structural variation thereof.
