An object of the present invention is to find a novel pharmaceutical that has an excellent tryptophanase inhibitory effect, and suppresses worsening of renal function to preserve the kidney by reducing production of indoxyl sulfate in the blood. The prese
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Paragraph 0187
(2019/08/26)
Novel Cyclic Urea Derivatives, Preparation Thereof and Pharmaceutical Use Thereof as Kinase Inhibitors
Compounds of formula (I): wherein Ra, Rb, R, X1 and X2 are as defined in the disclosure, pharmaceutical compositions comprising said compounds, processes for making and methods of using the same are provided.
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Page/Page column 29
(2009/04/24)
New β-alanine derivatives are orally available glucagon receptor antagonists
A weak human glucagon receptor antagonist with an IC50 of 7 μM was initially found by screening of libraries originally targeted to mimic the binding of the glucagon-like peptide (GLP-1) hormone to its receptor. Optimization of this hit for binding affinity for the glucagon receptor led to ligands with affinity in the nanomolar range. In addition to receptor binding, optimization efforts were made to stabilize the molecules against fast metabolic turnover. A potent antagonist of the human human glucagon receptor was obtained that had 17% oral availability in rats with a plasma half-life of 90 min. The major metabolites of this lead were identified and used to further optimize this series with respect to pharmacokinetic properties. This final optimization led to a potent glucagon antagonist that was orally available in rats and dogs and was efficacious in lowering blood glucose levels in a diabetic animal model.
Lau, Jesper,Behrens, Garsten,Sidelmann, Ulla G.,Knudsen, Lotte B.,Lundt, Behrend,Sams, Christian,Ynddal, Lars,Brand, Christian L.,Pridal, Lone,Ling, Anthony,Kiel, Dan,Plewe, Michael,Shi, Shengua,Madsen, Peter
p. 113 - 128
(2007/10/03)
3-(p-Alkylsulfonylphenyl)oxazolidinone derivatives as antibacterial agents
This invention relates to novel 3-(p-alkylsulfonylphenyl)oxazolidinone derivatives, pharmaceutical compositions containing them and methods of using them to alleviate bacterial infections in mammals.
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(2008/06/13)
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