Page last updated: 2024-08-21

thiazoles and amg 221

thiazoles has been researched along with amg 221 in 6 studies

Research

Studies (6)

TimeframeStudies, this research(%)All Research%
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's1 (16.67)29.6817
2010's5 (83.33)24.3611
2020's0 (0.00)2.80

Authors

AuthorsStudies
Caille, S; Cui, S; Faul, MM; Hwang, TL; Wang, X1
Adams, J; Bartberger, MD; Chen, MM; Cupples, R; Emery, MG; Fotsch, C; Gahm, K; Hague, A; Hale, C; Henriksson, MA; Hungate, RW; Johansson, L; Jona, J; Jordan, S; Joseph, S; Kim, KW; Komorowski, R; Li, V; Moniz, G; St Jean, DJ; Syed, R; Vallgårda, J; Véniant, MM; Wang, M; Williams, M; Zhang, J1
Akrami, A; Bautista, E; Daniels, O; Emery, MG; Gastonguay, MR; Gibbs, JP; Gibbs, MA; McCaffery, I; Paweletz, K; Perfetti, R; Rossi, J; Smith, B; Wang, M1
Davis, JA; Deane, MR; Emery, MG; Greene, RJ; Slatter, JG; Subramanian, R1
Akrami, A; Deane, MR; Emery, MG; Hickman, D; Skiles, GL; Slatter, JG; Subramanian, R; Zhang, X; Zhu, X1
Amore, BM; Emery, MG; Gao, Q; Greg Slatter, J; Hickman, D; Kimura, RE; Nam, J; Zhang, X1

Trials

1 trial(s) available for thiazoles and amg 221

ArticleYear
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.
    Journal of clinical pharmacology, 2011, Volume: 51, Issue:6

    Topics: 11-beta-Hydroxysteroid Dehydrogenase Type 1; Administration, Oral; Adult; Biomarkers, Pharmacological; Dose-Response Relationship, Drug; Female; Humans; Inhibitory Concentration 50; Male; Models, Biological; Obesity; Subcutaneous Fat, Abdominal; Thiazoles

2011

Other Studies

5 other study(ies) available for thiazoles and amg 221

ArticleYear
Two asymmetric syntheses of AMG 221, an inhibitor of 11beta-hydroxysteroid dehydrogenase type 1.
    The Journal of organic chemistry, 2009, May-15, Volume: 74, Issue:10

    Topics: 11-beta-Hydroxysteroid Dehydrogenase Type 1; Alcohols; Chlorides; Cyclization; Enzyme Inhibitors; Solvents; Stereoisomerism; Substrate Specificity; Thiazoles

2009
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).
    Journal of medicinal chemistry, 2010, Jun-10, Volume: 53, Issue:11

    Topics: 11-beta-Hydroxysteroid Dehydrogenase Type 1; Administration, Oral; Animals; Dogs; Drug Discovery; Enzyme Inhibitors; Humans; Male; Mice; Models, Molecular; Protein Conformation; Rats; Thiazoles

2010
Regiospecific and stereospecific triangulation of the structures of metabolites formed by sequential metabolism at multiple prochiral centers.
    Drug metabolism and disposition: the biological fate of chemicals, 2012, Volume: 40, Issue:5

    Topics: 11-beta-Hydroxysteroid Dehydrogenase Type 1; Administration, Oral; Animals; Bile; Biotransformation; Chromatography, High Pressure Liquid; Dogs; Enzyme Inhibitors; Feces; Female; Hydroxylation; Male; Microsomes, Liver; Molecular Structure; Oxidation-Reduction; Rats; Rats, Sprague-Dawley; Sex Factors; Species Specificity; Stereoisomerism; Tandem Mass Spectrometry; Thiazoles

2012
Activity-based exposure comparisons among humans and nonclinical safety testing species in an extensively metabolized drug candidate.
    Xenobiotica; the fate of foreign compounds in biological systems, 2013, Volume: 43, Issue:7

    Topics: 11-beta-Hydroxysteroid Dehydrogenase Type 1; Animals; Area Under Curve; Chromatography, Liquid; Dogs; Humans; Male; Microsomes, Liver; Rats; Species Specificity; Tandem Mass Spectrometry; Thiazoles

2013
Intestinal and hepatic first-pass extraction of the 11β-HSD1 inhibitor AMG 221 in rats with chronic vascular catheters.
    Xenobiotica; the fate of foreign compounds in biological systems, 2014, Volume: 44, Issue:3

    Topics: 11-beta-Hydroxysteroid Dehydrogenase Type 1; Administration, Oral; Animals; Biological Availability; Carbon Radioisotopes; Intestinal Mucosa; Liver; Molecular Structure; Rats; Thiazoles; Vascular Access Devices

2014