Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221).
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1H-Imidazol-4(5H)-ones and thiazol-4(5H)-ones as emerging pronucleophiles in asymmetric catalysisOptimization of 1,2,4-Triazolopyridines as Inhibitors of Human 11β-Hydroxysteroid Dehydrogenase Type 1 (11β-HSD-1)Discovery of 2-Alkyl-1-arylsulfonylprolinamides as 11β-Hydroxysteroid Dehydrogenase Type 1 Inhibitors11β-Hydroxysteroid dehydrogenase type 1: relevance of its modulation in the pathophysiology of obesity, the metabolic syndrome and type 2 diabetes mellitus.Effects of antisense-mediated inhibition of 11β-hydroxysteroid dehydrogenase type 1 on hepatic lipid metabolismCurrent and future drug targets in weight managementAdamantyl carboxamides and acetamides as potent human 11β-hydroxysteroid dehydrogenase type 1 inhibitors.Crystal structures of 11β-hydroxysteroid dehydrogenase type 1 and their use in drug discovery.New perspectives on the development of antiobesity drugs.Discontinued drugs 2011: endocrine and metabolic.Synthesis and Evaluation of the Metabolites of AMG 221, a Clinical Candidate for the Treatment of Type 2 Diabetes.Synthesis and biological evaluation of cyclic sulfamide derivatives as 11β-hydroxysteroid dehydrogenase 1 inhibitors.Discovery of HSD-621 as a Potential Agent for the Treatment of Type 2 Diabetes.Population pharmacokinetic/pharmacodynamic model of subcutaneous adipose 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) activity after oral administration of AMG 221, a selective 11β-HSD1 inhibitor.Development of supercritical fluid extraction and supercritical fluid chromatography purification methods using rapid solubility screening with multiple solubility chambers.Highly enantioselective construction of tertiary thioethers and alcohols via phosphine-catalyzed asymmetric γ-addition reactions of 5H-thiazol-4-ones and 5H-oxazol-4-ones: scope and mechanistic understandings.Development of a credible 3D-QSAR CoMSIA model and docking studies for a series of triazoles and tetrazoles containing 11β-HSD1 inhibitors.Activity-based exposure comparisons among humans and nonclinical safety testing species in an extensively metabolized drug candidate.Pharmacokinetic characterization of 2-(3-benzoyl)-4-hydroxy-1,1-dioxo-2H-1,2-benzothiazine-2-yl-1-phenylethanone, a novel 11β-hydroxysteroid dehydrogenase type 1 inhibitor in rats.
P2860
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P2860
Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221).
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2010 nî lūn-bûn
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2010年の論文
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2010年学术文章
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2010年学术文章
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2010年学术文章
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2010年学术文章
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2010年学术文章
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name
Discovery of a potent, orally ...... ylthiazol-4(5H)-one (AMG 221).
@en
Discovery of a potent, orally ...... ylthiazol-4(5H)-one (AMG 221).
@nl
type
label
Discovery of a potent, orally ...... ylthiazol-4(5H)-one (AMG 221).
@en
Discovery of a potent, orally ...... ylthiazol-4(5H)-one (AMG 221).
@nl
prefLabel
Discovery of a potent, orally ...... ylthiazol-4(5H)-one (AMG 221).
@en
Discovery of a potent, orally ...... ylthiazol-4(5H)-one (AMG 221).
@nl
P2093
P356
P1476
Discovery of a potent, orally ...... ylthiazol-4(5H)-one (AMG 221).
@en
P2093
Andrew Hague
Christopher Fotsch
Clarence Hale
David J St Jean
George Moniz
Janan Jona
Jeffrey Adams
Jerk Vallgårda
Jiandong Zhang
Ki Won Kim
P304
P356
10.1021/JM100242D
P407
P577
2010-06-01T00:00:00Z