711017-40-2Relevant academic research and scientific papers
PYRIMIDINE-2,4,6-TRIONES FOR USE IN THE TREATMENT OF AMYOTROPHIC LATERAL SCLEROSIS
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Page/Page column 109, (2010/11/18)
The present invention relates to the identification of inventive pyrimidine-2,4,6- triones (PYT compounds) and pharmaceutical compositions thereof for treating subjects with amyotrophic lateral sclerosis (ALS) and other neurodegenerative diseases. The invention also provides methods of preparing the inventive PYT compounds.
β,β-Difluoro analogs of α-oxo-β-phenylpropionic acid and phenylalanine
Schlosser, Manfred,Brügger, Nadia,Schmidt, Werner,Amrhein, Nikolaus
, p. 7731 - 7742 (2007/10/03)
A simple three-step procedure converted the readily accessible (2-bromo-1,1-difluoroethyl)arenes (2) into α-aryl-α,α- difluoroacetaldehydes (1). Subsequent hydrocyanation, hydrolysis, oxidation and again hydrolysis afforded β-aryl-β,β-difluoro-α- oxopropionic acids (3). Reductive amination transformed the oxoacids 3 into a separable mixture of α-hydroxyacids 11 and racemic β,β-difluoro- β-phenylalanine derivatives (4). Enantiomerically pure β,β- difluorophenylalanine (L-4a) was obtained when α,α-difluoro-α- phenylacet-aldehyde (1a) was condensed with homochiral 1-phenylethylamine, hydrogen cyanide added to the resulting imine, the diastereomeric mixture thus produced hydrolyzed to the carboxamides (15) which were found to be separable by fractional crystallization or chromatography. The pKa values of the β-aryl-β,β-difluoroalanines (4) were measured and biological profile of the latter probed. 3-(4-Chlorophenyl)-3,3-difluoro-2-oxopropionic acid (4c) proved to be a potent (Ki 27 μM) and selective inhibitor of arogenate dehydratase, a key enzyme catalyzing the last step of the phenylalanine biosynthesis.
PYRROLYDIN-2-ONE DERIVATIVES AS INHIBITORS OF THROMBIN AND FACTOR XA
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Page 51, (2010/02/07)
The invention relates to compounds of formula (I), wherein : R1 represents hydrogen, C1-4 alkyl, -CH2CO2H, -CH2CO2C1-2alkyl, or -CH2CONR7R8; Rsu
