Aminopiperidine indazoles as orally efficacious melanin concentrating hormone receptor-1 antagonists

Bioorganic and Medicinal Chemistry Letters

Volumn 15, Issue 23, 2005, Pages 5293-5297

  Vasudevan, Anil ^a   Souers, Andrew J ^a   Freeman, Jennifer C ^a   Verzal, Mary K ^a   Gao, Ju ^a   Mulhern, Mathew M ^a   Wodka, Derek ^a   Lynch, John K ^a   Engstrom, Kenneth M ^a   Wagaw, Seble H ^a   Brodjian, Sevan ^a   Dayton, Brian ^a   Falls, Doug H ^a   Bush, Eugene ^a   Brune, Michael ^a   Shapiro, Robin D ^a   Marsh, Kennan C ^a   Hernandez, Lisa E ^a   Collins, Christine A ^a   Kym, Philip R ^a  

^a ABBOTT LABORATORIES   (United States)

Author keywords

Aminoindazoles; Melanin concentrating hormone; Obesity; Palladium amination

Indexed keywords

3 AMINOINDAZOLE MELANIN CONCENTRATING HORMONE RECEPTOR 1 ANTAGONIST; HORMONE RECEPTOR BLOCKING AGENT; INDAZOLE DERIVATIVE; MELANIN CONCENTRATING HORMONE; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; BIOLOGICAL ACTIVITY; BRAIN; BRAIN LEVEL; DIET; DRUG DISTRIBUTION; DRUG EFFICACY; DRUG MECHANISM; DRUG POTENCY; DRUG POTENTIATION; DRUG SCREENING; DRUG STRUCTURE; MOUSE; NONHUMAN; OBESITY;

ADMINISTRATION, ORAL; ANIMALS; ANTI-OBESITY AGENTS; HUMANS; INDAZOLES; MICE; PIPERIDINES; RECEPTORS, SOMATOSTATIN; TISSUE DISTRIBUTION;

ANIMALIA;

EID: 26844531187     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2005.08.049     Document Type: Article

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12. In certain cases, a significant disconnect between MCHr1-binding affinity and activity in the functional assay was observed. Studies are underway to determine the cause of this phenomenon and results will be reported elsewhere.
13. Compound 25 was also evaluated for efficacy in a DIO mouse model and was found to cause robust weight-loss (data not shown).