Your browser doesn't support javascript.
loading
Efforts towards the optimization of a bi-aryl class of potent IRAK4 inhibitors.
Hanisak, Jennifer; Seganish, W Michael; McElroy, William T; Tang, Haiquin; Zhang, Rui; Tsui, Hon-Chung; Fischmann, Theirry; Tulshian, Deen; Tata, James; Sondey, Christopher; Devito, Kristine; Fossetta, James; Garlisi, Charles G; Lundell, Daniel; Niu, Xiaoda.
Afiliação
  • Hanisak J; Discovery Chemistry, Merck Research Laboratories, 2015 Galloping Hill Rd., Kenilworth, NJ 07033, Unites States. Electronic address: jennifer.hanisak@merck.com.
  • Seganish WM; Discovery Chemistry, Merck Research Laboratories, 2015 Galloping Hill Rd., Kenilworth, NJ 07033, Unites States.
  • McElroy WT; Discovery Chemistry, Merck Research Laboratories, 2015 Galloping Hill Rd., Kenilworth, NJ 07033, Unites States.
  • Tang H; Discovery Chemistry, Merck Research Laboratories, 2015 Galloping Hill Rd., Kenilworth, NJ 07033, Unites States.
  • Zhang R; Discovery Chemistry, Merck Research Laboratories, 2015 Galloping Hill Rd., Kenilworth, NJ 07033, Unites States.
  • Tsui HC; Discovery Chemistry, Merck Research Laboratories, 2015 Galloping Hill Rd., Kenilworth, NJ 07033, Unites States.
  • Fischmann T; Discovery Chemistry, Merck Research Laboratories, 2015 Galloping Hill Rd., Kenilworth, NJ 07033, Unites States.
  • Tulshian D; Discovery Chemistry, Merck Research Laboratories, 2015 Galloping Hill Rd., Kenilworth, NJ 07033, Unites States.
  • Tata J; Discovery Chemistry, Merck Research Laboratories, 2015 Galloping Hill Rd., Kenilworth, NJ 07033, Unites States.
  • Sondey C; In Vitro Pharmacology, Merck Research Laboratories, 2015 Galloping Hill Rd., Kenilworth, NJ 07033, United States.
  • Devito K; In Vitro Pharmacology, Merck Research Laboratories, 2015 Galloping Hill Rd., Kenilworth, NJ 07033, United States.
  • Fossetta J; Respiratory and Immunology, Merck Research Laboratories, 2015 Galloping Hill Rd., Kenilworth, NJ 07033, United States.
  • Garlisi CG; In Vitro Pharmacology, Merck Research Laboratories, 2015 Galloping Hill Rd., Kenilworth, NJ 07033, United States.
  • Lundell D; Respiratory and Immunology, Merck Research Laboratories, 2015 Galloping Hill Rd., Kenilworth, NJ 07033, United States.
  • Niu X; In Vitro Pharmacology, Merck Research Laboratories, 2015 Galloping Hill Rd., Kenilworth, NJ 07033, United States.
Bioorg Med Chem Lett ; 26(17): 4250-5, 2016 09 01.
Article em En | MEDLINE | ID: mdl-27476420
ABSTRACT
IRAK4 has been identified as potential therapeutic target for inflammatory and autoimmune diseases. Herein we report the identification and initial SAR studies of a new class of pyrazole containing IRAK4 inhibitors designed to expand chemical diversity and improve off target activity of a previously identified series. These compounds maintain potent IRAK4 activity and desirable ligand efficiency. Rat clearance and a variety of off target activities were also examined, resulting in encouraging data with tractable SAR.
Assuntos
Palavras-chave
Texto completo
Adicionar na Minha BVS
Imprimir
XML
PubMed Links
Buscar no Google

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Pirazóis / Inibidores de Proteínas Quinases / Quinases Associadas a Receptores de Interleucina-1 Limite: Animals / Humans Idioma: En Revista: Bioorg Med Chem Lett Assunto da revista: BIOQUIMICA / QUIMICA Ano de publicação: 2016 Tipo de documento: Article
Texto completo
Adicionar na Minha BVS
Imprimir
XML
PubMed Links
Buscar no Google

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Pirazóis / Inibidores de Proteínas Quinases / Quinases Associadas a Receptores de Interleucina-1 Limite: Animals / Humans Idioma: En Revista: Bioorg Med Chem Lett Assunto da revista: BIOQUIMICA / QUIMICA Ano de publicação: 2016 Tipo de documento: Article