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Structure-activity-relationship of amide and sulfonamide analogs of omarigliptin.
Chen, Ping; Feng, Dennis; Qian, Xiaoxia; Apgar, James; Wilkening, Robert; Kuethe, Jeffrey T; Gao, Ying-Duo; Scapin, Giovanna; Cox, Jason; Doss, George; Eiermann, George; He, Huaibing; Li, Xiaohua; Lyons, Kathryn A; Metzger, Joseph; Petrov, Aleksandr; Wu, Joseph K; Xu, Shiyao; Weber, Ann E; Yan, Youwei; Roy, Ranabir Sinha; Biftu, Tesfaye.
Afiliação
  • Chen P; Department of Discovery Chemistry, Merck Research Laboratories, 2015 Galloping Hill Road, Kenilworth, NJ 07033, United States.
  • Feng D; Department of Discovery Chemistry, Merck Research Laboratories, 2015 Galloping Hill Road, Kenilworth, NJ 07033, United States.
  • Qian X; Department of Discovery Chemistry, Merck Research Laboratories, 2015 Galloping Hill Road, Kenilworth, NJ 07033, United States.
  • Apgar J; Department of Discovery Chemistry, Merck Research Laboratories, 2015 Galloping Hill Road, Kenilworth, NJ 07033, United States.
  • Wilkening R; Department of Discovery Chemistry, Merck Research Laboratories, 2015 Galloping Hill Road, Kenilworth, NJ 07033, United States.
  • Kuethe JT; Department of Discovery Chemistry, Merck Research Laboratories, 2015 Galloping Hill Road, Kenilworth, NJ 07033, United States.
  • Gao YD; Department of Discovery Chemistry, Merck Research Laboratories, 2015 Galloping Hill Road, Kenilworth, NJ 07033, United States.
  • Scapin G; Department of Discovery Chemistry, Merck Research Laboratories, 2015 Galloping Hill Road, Kenilworth, NJ 07033, United States.
  • Cox J; Department of Discovery Chemistry, Merck Research Laboratories, 2015 Galloping Hill Road, Kenilworth, NJ 07033, United States.
  • Doss G; Department of Pharmacokinetics, Pharmacodynamics & Drug Metabolism, Merck Research Laboratories, 2015 Galloping Hill Road, Kenilworth, NJ 07033, United States.
  • Eiermann G; Department of Pharmacology, Screening & Protein Sciences, Merck Research Laboratories, 2015 Galloping Hill Road, Kenilworth, NJ 07033, United States.
  • He H; Department of Pharmacokinetics, Pharmacodynamics & Drug Metabolism, Merck Research Laboratories, 2015 Galloping Hill Road, Kenilworth, NJ 07033, United States.
  • Li X; Department of Pharmacokinetics, Pharmacodynamics & Drug Metabolism, Merck Research Laboratories, 2015 Galloping Hill Road, Kenilworth, NJ 07033, United States.
  • Lyons KA; Department of Pharmacokinetics, Pharmacodynamics & Drug Metabolism, Merck Research Laboratories, 2015 Galloping Hill Road, Kenilworth, NJ 07033, United States.
  • Metzger J; Department of Cardiometabolic Diseases, Merck Research Laboratories, 2015 Galloping Hill Road, Kenilworth, NJ 07033, United States.
  • Petrov A; Department of Pharmacology, Screening & Protein Sciences, Merck Research Laboratories, 2015 Galloping Hill Road, Kenilworth, NJ 07033, United States.
  • Wu JK; Department of Cardiometabolic Diseases, Merck Research Laboratories, 2015 Galloping Hill Road, Kenilworth, NJ 07033, United States.
  • Xu S; Department of Pharmacokinetics, Pharmacodynamics & Drug Metabolism, Merck Research Laboratories, 2015 Galloping Hill Road, Kenilworth, NJ 07033, United States.
  • Weber AE; Department of Discovery Chemistry, Merck Research Laboratories, 2015 Galloping Hill Road, Kenilworth, NJ 07033, United States.
  • Yan Y; Department of Discovery Chemistry, Merck Research Laboratories, 2015 Galloping Hill Road, Kenilworth, NJ 07033, United States.
  • Roy RS; Department of Cardiometabolic Diseases, Merck Research Laboratories, 2015 Galloping Hill Road, Kenilworth, NJ 07033, United States.
  • Biftu T; Department of Discovery Chemistry, Merck Research Laboratories, 2015 Galloping Hill Road, Kenilworth, NJ 07033, United States.
Bioorg Med Chem Lett ; 25(24): 5767-71, 2015 Dec 15.
Article em En | MEDLINE | ID: mdl-26546218
ABSTRACT
A series of novel substituted-[(3R)-amino-2-(2,5-difluorophenyl)]tetrahydro-2H-pyran analogs have been prepared and evaluated as potent, selective and orally active DPP-4 inhibitors. These efforts lead to the discovery of a long acting DPP-4 inhibitor, omarigliptin (MK-3102), which recently completed phase III clinical development and has been approved in Japan.
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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Piranos / Sulfonamidas / Inibidores da Dipeptidil Peptidase IV / Amidas / Compostos Heterocíclicos com 2 Anéis Limite: Animals Idioma: En Ano de publicação: 2015 Tipo de documento: Article
Texto completo
Imprimir
XML
PubMed Links
Buscar no Google

Texto completo: 1 Base de dados: MEDLINE Assunto principal: Piranos / Sulfonamidas / Inibidores da Dipeptidil Peptidase IV / Amidas / Compostos Heterocíclicos com 2 Anéis Limite: Animals Idioma: En Ano de publicação: 2015 Tipo de documento: Article