800401-54-1Relevant academic research and scientific papers
BICYCLIC HETEROARYLS AS KINASE INHIBITORS
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, (2011/05/06)
The invention is directed to heteroaryl compounds useful as inhibitors of various kinase enzymes. In various embodiments, the invention provides a heteroaryl compound having inhibitory bioactivity with respect to a Rho kinase, an AKT kinase, a p70S6K kinase, a LIM kinase, an IKK kinase, a Flt kinase, an Aurora kinase, or a Src kinase, or any combination thereof. Compounds of the invention include bicyclic heteroaryl compounds of formula (I), which can contain a bridging nitrogen atom at a ring junction. The invention further provides methods of synthesis of compounds of the invention, pharmaceutical compositions, pharmaceutical combinations, and methods of treatment of malconditions using compounds of the invention.
Discovery and optimization of indoles and 7-azaindoles as Rho kinase (ROCK) inhibitors (part-I)
Chowdhury, Sarwat,Sessions, E. Hampton,Pocas, Jennifer R.,Grant, Wayne,Schr?ter, Thomas,Lin, Li,Ruiz, Claudia,Cameron, Michael D.,Schürer, Stephan,Lograsso, Philip,Bannister, Thomas D.,Feng, Yangbo
, p. 7107 - 7112 (2012/01/05)
Rho kinase (ROCK) inhibitors are potential therapeutic agents to treat disorders such as hypertension, multiple sclerosis, cancers, and glaucoma. Here, we disclose the synthesis, optimization, biological evaluation of potent indole and 7-azaindole based ROCK inhibitors that have high potency on ROCK (IC 50 = 1 nM) with 740-fold selectivity over PKA (47). Moreover, 47 showed very good DMPK properties making it a good candidate for further development. Finally, docking studies with a homology model of ROCK-II were performed to rationalize the binding mode of these compounds and showed the compounds bound in both orientations to take advantage to H-bonds with Lys-121 of ROCK-II.
PYRROLOPYRIDINE-2-CARBOXYLIC ACID AMIDES
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Page/Page column 24, (2008/06/13)
Compounds represented by Formula (I) or pharmaceutically acceptable salts thereof, are useful in the prophylactic or therapeutic treatment of diabetes, hyperglycemia, hypercholesterolemia, hyperinsulinemia, hyperlipidemia, hypertension, atherosclerosis or tissue ischemia e.g. myocardial ischemia, and as cardioprotectants.
G-PROTEIN COUPLED RECEPTOR AGONISTS
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Page/Page column 18, (2008/06/13)
Compounds of Formula (I) or pharmaceutically acceptable salts or N-oxides thereof, are agonists of GPR116 and are useful for the treatment of obesity, and for the treatment of diabetes.
PYRROLOPYRIDINE-2-CARBOXYLIC ACID AMIDE INHIBITORS OF GLYCOGEN PHOSHORYLASE
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, (2008/06/13)
Compounds represented by Formula (I): or pharmaceutically acceptable salts thereof, are inhibitors of glycogen phosphorylase and are useful in the prophylactic or therapeutic treatment of diabetes, hyperglycemia, hypercholesterolemia, hyperinsulinemia, hyperlipidemia, hypertension, atherosclerosis or tissue ischemia e.g. myocardial ischemia, and as cardioprotectants.
