2. Academic Validation
  3. Synthesis and Antiobesity Properties of 6-(4-Chlorophenyl)-3-(4-((3,3-difluoro-1-hydroxycyclobutyl)methoxy)-3-methoxyphenyl)thieno[3,2-d]pyrimidin-4(3H)-one (BMS-814580): A Highly Efficacious Melanin Concentrating Hormone Receptor 1 (MCHR1) Inhibitor

Synthesis and Antiobesity Properties of 6-(4-Chlorophenyl)-3-(4-((3,3-difluoro-1-hydroxycyclobutyl)methoxy)-3-methoxyphenyl)thieno[3,2-d]pyrimidin-4(3H)-one (BMS-814580): A Highly Efficacious Melanin Concentrating Hormone Receptor 1 (MCHR1) Inhibitor

  • J Med Chem. 2016 Oct 13;59(19):8848-8858. doi: 10.1021/acs.jmedchem.6b00676.
Saleem Ahmad 1,  William N Washburn 1,  Andres S Hernandez 1,  Sharon Bisaha 1,  Khehyong Ngu 1,  Wei Wang 1,  Mary Ann Pelleymounter 1,  Daniel Longhi 1,  Neil Flynn 1,  Anthony V Azzara 1,  Kenneth Rohrbach 1,  James Devenny 1,  Suzanne Rooney 1,  Michael Thomas 1,  Susan Glick 1,  Helen Godonis 1,  Susan Harvey 1,  Hongwei Zhang 1,  Brian Gemzik 1,  Evan B Janovitz 1,  Christine Huang 1,  Lisa Zhang 1,  Jeffrey A Robl 1,  Brian J Murphy 1
Affiliations

Affiliation

  • 1 Metabolic Diseases Chemistry, ‡Metabolic Diseases Biology, §PCO MAP, ∥PCO Discovery Toxicology, and ⊥PCO Bioanalytical Research, Bristol-Myers Squibb Research & Development , P.O. Box 4000, Princeton, New Jersey 08543, United States.
PMID: 27564419 DOI: 10.1021/acs.jmedchem.6b00676
Abstract

The potent MCHR1 in vitro and in vivo antagonist activity of a series of cyclic tertiary alcohols derived from compound 2b is described. Subsequent pharmacokinetic and pharmacodynamic studies identified BMS-814580 (compound 10) as a highly efficacious antiobesity agent with a relatively clean in vitro and in vivo safety profile.

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