54828-05-6Relevant articles and documents
AROMATIC DERIVATIVES, PREPARATION METHODS, AND MEDICAL USES THEREOF
-
, (2020/09/19)
The present disclosure relates generally to aromatic derivatives that are inhibitors of FGFR4 and are useful in treating FGFR4-associated diseases or conditions. Compositions containing the compounds of the present disclosure are also provided.
ortho-Substituted azoles as selective and dual inhibitors of VEGF receptors 1 and 2
Kiselyov, Alexander S.,Piatnitski, Evgueni L.,Samet, Alexander V.,Kisliy, Victor P.,Semenov, Victor V.
, p. 1369 - 1375 (2007/10/03)
We have developed a series of novel potent ortho-substituted azole derivatives active against kinases VEGFR-1 and VEGFR-2. Both specific and dual ATP-competitive inhibitors of VEGFR-2 were identified. Kinase activity and selectivity could be controlled by varying the arylamido substituents at the azole ring. The most specific molecule (17) displayed >10-fold selectivity for VEGFR-2 over VEGFR-1. Compound activities in enzymatic and cell-based assays were in the range of activities for reported clinical and development candidates (IC50 30 × 10-5 cm/min) is indicative of their potential for intestinal absorption upon oral administration.
The Synthesis of Ring-expanded Analogues of Xanthine Containing the Imidazodiazepine Ring System
Hosmane, Ramachandra S.,Bhan, Anila
, p. 2189 - 2196 (2007/10/02)
The synthesis of 4,5,7,8-tetrahydro-6H-imidazodiazepine-5,8-dione and its several 1- and 3-alkyl (aralkyl) derivatives 2 has been reported.Mechanistic explorations of the final synthetic step as well as structural confirmation of a final produ
