426829-61-0Relevant articles and documents
DIHYDROQUINOLINE-2-ONE DERIVATIVES
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Paragraph 0617; 0618; 0619; 0620, (2013/03/28)
The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6, R7, A1, A2 and A3 are as described herein, compositions including the compounds and methods of using the compounds. These compounds are useful for therapy or prophylaxis in a mammal, and in particular as aldosterone synthase (CYP11B2 or CYP11B1) inhibitors for the treatment or prophylaxis of chronic kidney disease, congestive heart failure, hypertension, primary aldosteronism and Cushing syndrome.
NEW DIHYDROQUINOLINE-2-ONE DERIVATIVES
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Page/Page column 92, (2013/03/28)
The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4? R5, R6, R7, A1, A2 and A3 are as described herein, compositions including the compounds and methods of using the compounds.
Novel inhibitors of B-RAF based on a disubstituted pyrazine scaffold. Generation of a nanomolar lead
Niculescu-Duvaz, Ion,Roman, Esteban,Whittaker, Steven R.,Friedlos, Frank,Kirk, Ruth,Scanlon, Ian J.,Davies, Lawrence C.,Niculescu-Duvaz, Dan,Marais, Richard,Springer, Caroline J.
, p. 407 - 416 (2007/10/03)
B-RAF, a serine/threonine kinase, plays an important role in the development of certain classes of cancer, especially melanoma. As a result of high-throughput screening of a 23,000 compound library, 2-(3,4,5- trimethoxyphenylamino)-6-(3-acetamidophenyl)pyrazine, 1, was identified as a low micromolar (IC50 = 3.5 μM) B-RAF inhibitor. This compound was chosen as the starting point of a program aimed at producing potent inhibitors of B-RAF. We have synthesized a series of 40 novel compounds, which involved extensive modifications to the 2-(3,4,5-trimethoxyphenylamino) moiety (ring A) of 1. Their biological profiles against isolated B-RAF and mutated B-RAF in a cellular assay have been determined. These efforts led to the identification of two compounds exhibiting activities lower than 800 nM against B-RAF.
KINASE INHIBITORS
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Page 33, (2008/06/13)
A compound of the general formula (I) or pharmaceutically acceptable salts, hydrates, solvates, crystal forms or diastereomers thereof is described. A method of treating protein kinase-associated disease states using the compound of formula (I) is also de
Novel compounds and their use
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, (2008/06/13)
A compound of the general formula (I): wherein R1, R2, X, Y and Z are as described in the specification.