54828-05-6Relevant academic research and scientific papers
AROMATIC DERIVATIVES, PREPARATION METHODS, AND MEDICAL USES THEREOF
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Paragraph 0151; 0153, (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.
SULFONAMIDE DERIVATIVE AND MEDICINAL USE THEREOF
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Paragraph 0166-0167, (2015/02/25)
Provided are sulfonamide derivatives of a specific chemical structure in which a sulfonamide group having, as a substituent, a phenyl group or a heterocyclic group having a hetero atom(s) as a constituent element(s) is present at its terminal, and pharmaceutically acceptable salts thereof. These compounds are novel compounds having excellent α4 integrin-inhibitory action.
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.
Hetaryl imidazoles: A novel dual inhibitors of VEGF receptors I and II
Kiselyov, Alexander S.,Semenova, Marina,Semenov, Victor V.
, p. 1440 - 1444 (2007/10/03)
A novel potent derivatives of hetaryl imidazoles were described as inhibitors of vascular endothelial growth factor receptor II (VEGFR-2). Several compounds display VEGFR-2 inhibitory activity reaching IC50 100 nM in both enzymatic and cellular assays. The compounds also inhibit the related tyrosine kinase, VEGFR-1. By controlling the substitution pattern on the 5-carboxamido functionality, both dual and specific VEGFR-2 thiazoles were identified.
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
MODELS FOR "FAT" NUCLEOSIDES AND NUCLEOTIDES: SYNTHESES OF "FAT" XANTHINE (fX), "FAT" GUANINE (fG), AND "FAT" HYPOXANTHINE (fHx) ANALOGUES OF THE IMIDAZODIAZEPINE SYSTEM
Hosmane, Ramachandra S.,Bhan, Anila,Rauser, Michael E.
, p. 2743 - 2748 (2007/10/02)
Synthetic analogues of xanthine, guanine, and hypoxanthine, possessing the skeletal structure of imidazodiazepine, are reported.
