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Discovery of MK-4409, a Novel Oxazole FAAH Inhibitor for the Treatment of Inflammatory and Neuropathic Pain.
Chobanian, Harry R; Guo, Yan; Liu, Ping; Chioda, Marc D; Fung, Selena; Lanza, Thomas J; Chang, Linda; Bakshi, Raman K; Dellureficio, James P; Hong, Qingmei; McLaughlin, Mark; Belyk, Kevin M; Krska, Shane W; Makarewicz, Amanda K; Martel, Elliot J; Leone, Joseph F; Frey, Lisa; Karanam, Bindhu; Madeira, Maria; Alvaro, Raul; Shuman, Joyce; Salituro, Gino; Terebetski, Jenna L; Jochnowitz, Nina; Mistry, Shruti; McGowan, Erin; Hajdu, Richard; Rosenbach, Mark; Abbadie, Catherine; Alexander, Jessica P; Shiao, Lin-Lin; Sullivan, Kathleen M; Nargund, Ravi P; Wyvratt, Matthew J; Lin, Linus S; DeVita, Robert J.
Afiliação
  • Chobanian HR; Departments of Medicinal Chemistry, Process Chemistry, Drug Metabolism and Pharmacokinetics, Preclinical Development, Pharmacology, and Immunology, Merck Research Laboratories , Kenilworth, New Jersey 07033, United States.
  • Guo Y; Departments of Medicinal Chemistry, Process Chemistry, Drug Metabolism and Pharmacokinetics, Preclinical Development, Pharmacology, and Immunology, Merck Research Laboratories , Kenilworth, New Jersey 07033, United States.
  • Liu P; Departments of Medicinal Chemistry, Process Chemistry, Drug Metabolism and Pharmacokinetics, Preclinical Development, Pharmacology, and Immunology, Merck Research Laboratories , Kenilworth, New Jersey 07033, United States.
  • Chioda MD; Departments of Medicinal Chemistry, Process Chemistry, Drug Metabolism and Pharmacokinetics, Preclinical Development, Pharmacology, and Immunology, Merck Research Laboratories , Kenilworth, New Jersey 07033, United States.
  • Fung S; Departments of Medicinal Chemistry, Process Chemistry, Drug Metabolism and Pharmacokinetics, Preclinical Development, Pharmacology, and Immunology, Merck Research Laboratories , Kenilworth, New Jersey 07033, United States.
  • Lanza TJ; Departments of Medicinal Chemistry, Process Chemistry, Drug Metabolism and Pharmacokinetics, Preclinical Development, Pharmacology, and Immunology, Merck Research Laboratories , Kenilworth, New Jersey 07033, United States.
  • Chang L; Departments of Medicinal Chemistry, Process Chemistry, Drug Metabolism and Pharmacokinetics, Preclinical Development, Pharmacology, and Immunology, Merck Research Laboratories , Kenilworth, New Jersey 07033, United States.
  • Bakshi RK; Departments of Medicinal Chemistry, Process Chemistry, Drug Metabolism and Pharmacokinetics, Preclinical Development, Pharmacology, and Immunology, Merck Research Laboratories , Kenilworth, New Jersey 07033, United States.
  • Dellureficio JP; Departments of Medicinal Chemistry, Process Chemistry, Drug Metabolism and Pharmacokinetics, Preclinical Development, Pharmacology, and Immunology, Merck Research Laboratories , Kenilworth, New Jersey 07033, United States.
  • Hong Q; Departments of Medicinal Chemistry, Process Chemistry, Drug Metabolism and Pharmacokinetics, Preclinical Development, Pharmacology, and Immunology, Merck Research Laboratories , Kenilworth, New Jersey 07033, United States.
  • McLaughlin M; Departments of Medicinal Chemistry, Process Chemistry, Drug Metabolism and Pharmacokinetics, Preclinical Development, Pharmacology, and Immunology, Merck Research Laboratories , Kenilworth, New Jersey 07033, United States.
  • Belyk KM; Departments of Medicinal Chemistry, Process Chemistry, Drug Metabolism and Pharmacokinetics, Preclinical Development, Pharmacology, and Immunology, Merck Research Laboratories , Kenilworth, New Jersey 07033, United States.
  • Krska SW; Departments of Medicinal Chemistry, Process Chemistry, Drug Metabolism and Pharmacokinetics, Preclinical Development, Pharmacology, and Immunology, Merck Research Laboratories , Kenilworth, New Jersey 07033, United States.
  • Makarewicz AK; Departments of Medicinal Chemistry, Process Chemistry, Drug Metabolism and Pharmacokinetics, Preclinical Development, Pharmacology, and Immunology, Merck Research Laboratories , Kenilworth, New Jersey 07033, United States.
  • Martel EJ; Departments of Medicinal Chemistry, Process Chemistry, Drug Metabolism and Pharmacokinetics, Preclinical Development, Pharmacology, and Immunology, Merck Research Laboratories , Kenilworth, New Jersey 07033, United States.
  • Leone JF; Departments of Medicinal Chemistry, Process Chemistry, Drug Metabolism and Pharmacokinetics, Preclinical Development, Pharmacology, and Immunology, Merck Research Laboratories , Kenilworth, New Jersey 07033, United States.
  • Frey L; Departments of Medicinal Chemistry, Process Chemistry, Drug Metabolism and Pharmacokinetics, Preclinical Development, Pharmacology, and Immunology, Merck Research Laboratories , Kenilworth, New Jersey 07033, United States.
  • Karanam B; Departments of Medicinal Chemistry, Process Chemistry, Drug Metabolism and Pharmacokinetics, Preclinical Development, Pharmacology, and Immunology, Merck Research Laboratories , Kenilworth, New Jersey 07033, United States.
  • Madeira M; Departments of Medicinal Chemistry, Process Chemistry, Drug Metabolism and Pharmacokinetics, Preclinical Development, Pharmacology, and Immunology, Merck Research Laboratories , Kenilworth, New Jersey 07033, United States.
  • Alvaro R; Departments of Medicinal Chemistry, Process Chemistry, Drug Metabolism and Pharmacokinetics, Preclinical Development, Pharmacology, and Immunology, Merck Research Laboratories , Kenilworth, New Jersey 07033, United States.
  • Shuman J; Departments of Medicinal Chemistry, Process Chemistry, Drug Metabolism and Pharmacokinetics, Preclinical Development, Pharmacology, and Immunology, Merck Research Laboratories , Kenilworth, New Jersey 07033, United States.
  • Salituro G; Departments of Medicinal Chemistry, Process Chemistry, Drug Metabolism and Pharmacokinetics, Preclinical Development, Pharmacology, and Immunology, Merck Research Laboratories , Kenilworth, New Jersey 07033, United States.
  • Terebetski JL; Departments of Medicinal Chemistry, Process Chemistry, Drug Metabolism and Pharmacokinetics, Preclinical Development, Pharmacology, and Immunology, Merck Research Laboratories , Kenilworth, New Jersey 07033, United States.
  • Jochnowitz N; Departments of Medicinal Chemistry, Process Chemistry, Drug Metabolism and Pharmacokinetics, Preclinical Development, Pharmacology, and Immunology, Merck Research Laboratories , Kenilworth, New Jersey 07033, United States.
  • Mistry S; Departments of Medicinal Chemistry, Process Chemistry, Drug Metabolism and Pharmacokinetics, Preclinical Development, Pharmacology, and Immunology, Merck Research Laboratories , Kenilworth, New Jersey 07033, United States.
  • McGowan E; Departments of Medicinal Chemistry, Process Chemistry, Drug Metabolism and Pharmacokinetics, Preclinical Development, Pharmacology, and Immunology, Merck Research Laboratories , Kenilworth, New Jersey 07033, United States.
  • Hajdu R; Departments of Medicinal Chemistry, Process Chemistry, Drug Metabolism and Pharmacokinetics, Preclinical Development, Pharmacology, and Immunology, Merck Research Laboratories , Kenilworth, New Jersey 07033, United States.
  • Rosenbach M; Departments of Medicinal Chemistry, Process Chemistry, Drug Metabolism and Pharmacokinetics, Preclinical Development, Pharmacology, and Immunology, Merck Research Laboratories , Kenilworth, New Jersey 07033, United States.
  • Abbadie C; Departments of Medicinal Chemistry, Process Chemistry, Drug Metabolism and Pharmacokinetics, Preclinical Development, Pharmacology, and Immunology, Merck Research Laboratories , Kenilworth, New Jersey 07033, United States.
  • Alexander JP; Departments of Medicinal Chemistry, Process Chemistry, Drug Metabolism and Pharmacokinetics, Preclinical Development, Pharmacology, and Immunology, Merck Research Laboratories , Kenilworth, New Jersey 07033, United States.
  • Shiao LL; Departments of Medicinal Chemistry, Process Chemistry, Drug Metabolism and Pharmacokinetics, Preclinical Development, Pharmacology, and Immunology, Merck Research Laboratories , Kenilworth, New Jersey 07033, United States.
  • Sullivan KM; Departments of Medicinal Chemistry, Process Chemistry, Drug Metabolism and Pharmacokinetics, Preclinical Development, Pharmacology, and Immunology, Merck Research Laboratories , Kenilworth, New Jersey 07033, United States.
  • Nargund RP; Departments of Medicinal Chemistry, Process Chemistry, Drug Metabolism and Pharmacokinetics, Preclinical Development, Pharmacology, and Immunology, Merck Research Laboratories , Kenilworth, New Jersey 07033, United States.
  • Wyvratt MJ; Departments of Medicinal Chemistry, Process Chemistry, Drug Metabolism and Pharmacokinetics, Preclinical Development, Pharmacology, and Immunology, Merck Research Laboratories , Kenilworth, New Jersey 07033, United States.
  • Lin LS; Departments of Medicinal Chemistry, Process Chemistry, Drug Metabolism and Pharmacokinetics, Preclinical Development, Pharmacology, and Immunology, Merck Research Laboratories , Kenilworth, New Jersey 07033, United States.
  • DeVita RJ; Departments of Medicinal Chemistry, Process Chemistry, Drug Metabolism and Pharmacokinetics, Preclinical Development, Pharmacology, and Immunology, Merck Research Laboratories , Kenilworth, New Jersey 07033, United States.
ACS Med Chem Lett ; 5(6): 717-21, 2014 Jun 12.
Article em En | MEDLINE | ID: mdl-24944750
We report herein the identification of MK-4409, a potent and selective fatty acid amide hydrolase (FAAH) inhibitor. Starting from a high throughput screening (HTS) hit, medicinal chemistry efforts focused on optimizing of FAAH inhibition in vitro potency, improving the pharmacokinetic (PK) profile, and increasing in vivo efficacy in rodent inflammatory and neuropathic pain assays.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Idioma: En Revista: ACS Med Chem Lett Ano de publicação: 2014 Tipo de documento: Article País de afiliação: Estados Unidos
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PubMed Links
Buscar no Google

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Idioma: En Revista: ACS Med Chem Lett Ano de publicação: 2014 Tipo de documento: Article País de afiliação: Estados Unidos