42058-71-9Relevant academic research and scientific papers
ROCK inhibitors 2. Improving potency, selectivity and solubility through the application of rationally designed solubilizing groups
Gao, Huai,Marhefka, Craig,Jacobs, Marc D.,Cao, Jingrong,Bandarage, Upul K.,Green, Jeremy
, p. 2616 - 2621 (2018/06/26)
Solubilizing groups have been frequently appended to kinase inhibitor drug molecules when solubility is insufficient for pharmaceutical development. Such groups are usually located at substitution sites that have minimal impact on target activity. In this report we describe the incorporation of solubilizing groups in a class of Rho kinase (ROCK) inhibitors that not only confer improved solubility, but also enhance target potency and selectivity against a closely related kinase, PKA.
Synthesis and PKCθ inhibitory activity of a series of 4-indolylamino-5-phenyl-3-pyridinecarbonitriles
Dushin, Russell G.,Nittoli, Thomas,Ingalls, Charles,Boschelli, Diane H.,Cole, Derek C.,Wissner, Allan,Lee, Julie,Yang, Xiaoke,Morgan, Paul,Brennan, Agnes,Chaudhary, Divya
scheme or table, p. 2461 - 2463 (2009/12/25)
A series of 4-indolylamino-5-phenyl-3-pyridinecarbonitrile inhibitors of PKCθ were synthesized as potential anti-inflammatory agents. The effects of specific substitution on the 5-phenyl moiety and variations of the positional isomers of the 4-indolylamino substituent were explored. This study led to the discovery of compound 12d, which had an IC50 value of 18 nM for the inhibition of PKCθ.
Substituted Cyanopyridines as protein kinase inhibitors
-
Page/Page column 22, (2008/06/13)
The present teachings provide compounds of formula I and their pharmaceutically acceptable salts, hydrates, and esters, wherein R1, R2, and X are as defined herein. The present teachings also provide methods of making the compounds of formula I, and methods of treating autoimmune and inflammatory diseases by administering a therapeutically effective amount of a compound or compounds of formula I to a mammal including a human.
COMPOSITIONS USEFUL AS INHIBITORS OF ROCK AND OTHER PROTEIN KINASES
-
, (2008/06/13)
The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.
AZAINDOLES USEFUL AS INHIBITORS OF ROCK AND OTHER PROTEIN KINASES
-
Page/Page column 170, (2008/06/13)
The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.
COMPOSITIONS USEFUL AS INHIBITORS OF ROCK AND OTHER PROTEIN KINASES
-
Page 115-116, (2010/02/07)
The present invention relates to substitute thiazole and thiophene derivatives useful as inhibitors of rock and other protein kinaeses. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders, including proliferative, cardiac and neurodegenerative diseases.
