141519-77-9Relevant articles and documents
ROCK KINASE INHIBITORS
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Paragraph 0091-0093, (2020/05/29)
The present invention relates to compounds that inhibit ROCK activity. In particular, the present invention relates to compounds, pharmaceutical compositions and methods of use, such as methods of inhibiting ROCK activity and methods for treating, for example cerebral cavernous malformation syndrome (CCM) and cardiovascular diseases using the compounds and pharmaceutical compositions of the present invention.
Structure-based design of isoquinoline-5-sulfonamide inhibitors of protein kinase B
Collins, Ian,Caldwell, John,Fonseca, Tatiana,Donald, Alastair,Bavetsias, Vassilios,Hunter, Lisa-Jane K.,Garrett, Michelle D.,Rowlands, Martin G.,Aherne, G. Wynne,Davies, Thomas G.,Berdini, Valerio,Woodhead, Steven J.,Davis, Deborah,Seavers, Lisa C. A.,Wyatt, Paul G.,Workman, Paul,McDonald, Edward
, p. 1255 - 1273 (2007/10/03)
Structure-based drug design of novel isoquinoline-5-sulfonamide inhibitors of PKB as potential antitumour agents was investigated. Constrained pyrrolidine analogues that mimicked the bound conformation of linear prototypes were identified and investigated by co-crystal structure determinations with the related protein PKA. Detailed variation in the binding modes between inhibitors with similar overall conformations was observed. Potent PKB inhibitors from this series inhibited GSK3β phosphorylation in cellular assays, consistent with inhibition of PKB kinase activity in cells.
ISOQUINOLINE-5-SULFONIC ACID AMIDES AS INHIBITORS OF AKT (PROTEIN KINASE B)
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Page 27, (2010/02/09)
The present invention relates to compounds Formula (I): as inhibitors of AKT activity, which are useful for the treatment of susceptible neoplasms and viral infections.
Isoquinolines as urokinase inhibitors
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, (2008/06/13)
Compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein one of R1 and R2 is H and the other is N=C(NH2)2 or NHC(=NH)NH2, and the other substituents are as defined herein, are urokinase (uPA) inhibitors.