57659-03-7Relevant articles and documents
Boronic acid-containing aminopyridine- and aminopyrimidinecarboxamide CXCR1/2 antagonists: Optimization of aqueous solubility and oral bioavailability
Schuler, Aaron D.,Engles, Courtney A.,Maeda, Dean Y.,Quinn, Mark T.,Kirpotina, Liliya N.,Wicomb, Winston N.,Mason, S. Nicholas,Auten, Richard L.,Zebala, John A.
, p. 3793 - 3797 (2015/08/24)
Abstract The chemokine receptors CXCR1 and CXCR2 are important pharmaceutical targets due to their key roles in inflammatory diseases and cancer progression. We have previously identified 2-[5-(4-fluoro-phenylcarbamoyl)-pyridin-2-ylsulfanylmethyl]-phenylboronic acid (SX-517) and 6-(2-boronic acid-5-trifluoromethoxy-benzylsulfanyl)-N-(4-fluoro-phenyl)-nicotinamide (SX-576) as potent non-competitive boronic acid-containing CXCR1/2 antagonists. Herein we report the synthesis and evaluation of aminopyridine and aminopyrimidine analogs of SX-517 and SX-576, identifying (2-{(benzyl)[(5-boronic acid-2-pyridyl)methyl]amino}-5-pyrimidinyl)(4-fluorophenylamino)formaldehyde as a potent chemokine antagonist with improved aqueous solubility and oral bioavailability.
6-SUBSTITUTED- 2,3,4,5-TETRAHYDRO-1H-BENZO[D]AZEPINES AS 5-HT2C RECEPTOR AGONISTS
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Page/Page column 65, (2008/06/13)
The present invention provides 6-substituted 2,3,4,5-tetrahydro-lH- benzo[d]azepines of Formula (I) as selective 5-HT2C receptor agonists for the treatment of 5-HT2c associated disorders including obesity, obsessive/compulsive disorder, depression, and anxiety: R6 D R? N-R" R* where R6 is -(CrC3)alkyl-S-(C0-C3)alkyl-R10, -(C1-C3)alkyl-NR11R12, -(CrC3)alkyl-O- R 13. and other substituents are as defined in the specification.
NOVEL CYANOGUANIDINE COMPOUNDS
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Page/Page column 20, (2008/06/13)
Novel pyridyl cyanoguanidien compounds of general formula I (I) wherein R1, X, R2 and R3 are as defined herein, exhibit a high antiproliferative activity and may be used in the treatment of hyperproliferative and neoplastic diseases.