Discovery of a potent, orally active 11β-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: Identification of (S)-2-((1 S,2 S,4 R)-Bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5 H)-one (AMG 221)

Journal of Medicinal Chemistry

Volumn 53, Issue 11, 2010, Pages 4481-4487

  Véniant, Murielle M ^a   Hale, Clarence ^a   Hungate, Randall W ^a   Gahm, Kyung ^a   Emery, Maurice G ^a   Jona, Janan ^b   Joseph, Smriti ^b   Adams, Jeffrey ^a,c   Hague, Andrew ^a,i   Moniz, George ^a,d   Zhang, Jiandong ^a   Bartberger, Michael D ^a   Li, Vivian ^a   Syed, Rashid ^a   Jordan, Steven ^a   Komorowski, Renée ^a   Chen, Michelle M ^a   Cupples, Rod ^a   Kim, Ki Won ^a   St Jean, David J ^a   Johansson, Lars ^f,g   Henriksson, Martin A ^e,h   Williams, Meredith ^f,i   Vallgårda, Jerk ^f   Fotsch, Christopher ^a   Wang, Minghan ^a   more..

^a Department of Metabolic Disorders ^*  (United States)

^b AMGEN INC   (United States)

^c Ricerca Inc   (United States)

^d EISAI INC   (United States)

^e CALIFORNIA STATE UNIVERSITY   (United States)

^f BIOVITRUM AB   (Sweden)

^g KAROLINSKA INSTITUTE   (Sweden)

^h S BIO   (Singapore)

ⁱ Infinity Pharmaceuticals Inc   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

11BETA HYDROXYSTEROID DEHYDROGENASE 1; 2 (BICYCLO[2.2.1]HEPTAN 2 YLAMINO) 5 ISOPROPYL 5 METHYLTHIAZOL 4(5H) ONE; 2 (BICYCLO[2.2.1]HEPTAN 2 YLAMINO) 5 ISOPROPYLTHIAZOL 4(5H) ONE; AMG 221; ENZYME INHIBITOR; GLUCOSE; INSULIN; ROSIGLITAZONE; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ARTICLE; BODY WEIGHT; DIASTEREOISOMER; DOG; DRUG DOSE COMPARISON; DRUG POTENCY; DRUG SELECTIVITY; DRUG STRUCTURE; ENZYME INHIBITION; EPIMERIZATION; GLUCOSE BLOOD LEVEL; HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; HUMAN; INSULIN BLOOD LEVEL; MASS SPECTROMETRY; MONKEY; MOUSE; NON INSULIN DEPENDENT DIABETES MELLITUS; NONHUMAN; OBESITY; PROTON NUCLEAR MAGNETIC RESONANCE; SPECIES COMPARISON; STRUCTURE ACTIVITY RELATION; TREATMENT OUTCOME;

11-BETA-HYDROXYSTEROID DEHYDROGENASE TYPE 1; ADMINISTRATION, ORAL; ANIMALS; DOGS; DRUG DISCOVERY; ENZYME INHIBITORS; HUMANS; MALE; MICE; MODELS, MOLECULAR; PROTEIN CONFORMATION; RATS; THIAZOLES;

EID: 77953182919     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm100242d     Document Type: Article

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