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Design and Synthesis of a Pan-Janus Kinase Inhibitor Clinical Candidate (PF-06263276) Suitable for Inhaled and Topical Delivery for the Treatment of Inflammatory Diseases of the Lungs and Skin.
Jones, Peter; Storer, R Ian; Sabnis, Yogesh A; Wakenhut, Florian M; Whitlock, Gavin A; England, Katherine S; Mukaiyama, Takasuke; Dehnhardt, Christoph M; Coe, Jotham W; Kortum, Steve W; Chrencik, Jill E; Brown, David G; Jones, Rhys M; Murphy, John R; Yeoh, Thean; Morgan, Paul; Kilty, Iain.
Afiliación
  • Jones P; Medicine Design, ‡Pharmacokinetics, Dynamics and Metabolism, and §Inflammation and Immunology Research Unit, Pfizer Inc. , 610 Main Street, Cambridge, Massachusetts 02139, United States.
  • Storer RI; Medicine Design, and ⊥Medicinal Sciences, Pfizer Inc. , 445 Eastern Point Road, Groton, Connecticut 06340, United States.
  • Sabnis YA; Worldwide Medicinal Chemistry, ∇Structural Biology and Biophysics, and ○Pharmaceutical Sciences, Pfizer Ltd. , Ramsgate Road, Sandwich, CT13 9NJ, U.K.
  • Wakenhut FM; Medicine Design, ‡Pharmacokinetics, Dynamics and Metabolism, and §Inflammation and Immunology Research Unit, Pfizer Inc. , 610 Main Street, Cambridge, Massachusetts 02139, United States.
  • Whitlock GA; Medicine Design, and ⊥Medicinal Sciences, Pfizer Inc. , 445 Eastern Point Road, Groton, Connecticut 06340, United States.
  • England KS; Worldwide Medicinal Chemistry, ∇Structural Biology and Biophysics, and ○Pharmaceutical Sciences, Pfizer Ltd. , Ramsgate Road, Sandwich, CT13 9NJ, U.K.
  • Mukaiyama T; Medicine Design, ‡Pharmacokinetics, Dynamics and Metabolism, and §Inflammation and Immunology Research Unit, Pfizer Inc. , 610 Main Street, Cambridge, Massachusetts 02139, United States.
  • Dehnhardt CM; Medicine Design, and ⊥Medicinal Sciences, Pfizer Inc. , 445 Eastern Point Road, Groton, Connecticut 06340, United States.
  • Coe JW; Worldwide Medicinal Chemistry, ∇Structural Biology and Biophysics, and ○Pharmaceutical Sciences, Pfizer Ltd. , Ramsgate Road, Sandwich, CT13 9NJ, U.K.
  • Kortum SW; Medicine Design, ‡Pharmacokinetics, Dynamics and Metabolism, and §Inflammation and Immunology Research Unit, Pfizer Inc. , 610 Main Street, Cambridge, Massachusetts 02139, United States.
  • Chrencik JE; Medicine Design, and ⊥Medicinal Sciences, Pfizer Inc. , 445 Eastern Point Road, Groton, Connecticut 06340, United States.
  • Brown DG; Worldwide Medicinal Chemistry, ∇Structural Biology and Biophysics, and ○Pharmaceutical Sciences, Pfizer Ltd. , Ramsgate Road, Sandwich, CT13 9NJ, U.K.
  • Jones RM; Medicine Design, ‡Pharmacokinetics, Dynamics and Metabolism, and §Inflammation and Immunology Research Unit, Pfizer Inc. , 610 Main Street, Cambridge, Massachusetts 02139, United States.
  • Murphy JR; Medicine Design, and ⊥Medicinal Sciences, Pfizer Inc. , 445 Eastern Point Road, Groton, Connecticut 06340, United States.
  • Yeoh T; Worldwide Medicinal Chemistry, ∇Structural Biology and Biophysics, and ○Pharmaceutical Sciences, Pfizer Ltd. , Ramsgate Road, Sandwich, CT13 9NJ, U.K.
  • Morgan P; Medicine Design, ‡Pharmacokinetics, Dynamics and Metabolism, and §Inflammation and Immunology Research Unit, Pfizer Inc. , 610 Main Street, Cambridge, Massachusetts 02139, United States.
  • Kilty I; Medicine Design, and ⊥Medicinal Sciences, Pfizer Inc. , 445 Eastern Point Road, Groton, Connecticut 06340, United States.
J Med Chem ; 60(2): 767-786, 2017 01 26.
Article en En | MEDLINE | ID: mdl-27983835
ABSTRACT
By use of a structure-based computational method for identification of structurally novel Janus kinase (JAK) inhibitors predicted to bind beyond the ATP binding site, a potent series of indazoles was identified as selective pan-JAK inhibitors with a type 1.5 binding mode. Optimization of the series for potency and increased duration of action commensurate with inhaled or topical delivery resulted in potent pan-JAK inhibitor 2 (PF-06263276), which was advanced into clinical studies.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Enfermedades de la Piel / Inhibidores de Proteínas Quinasas / Quinasas Janus / Compuestos Heterocíclicos con 2 Anillos / Indazoles / Enfermedades Pulmonares / Antiinflamatorios Tipo de estudio: Prognostic_studies Límite: Animals / Humans Idioma: En Revista: J Med Chem Asunto de la revista: QUIMICA Año: 2017 Tipo del documento: Article País de afiliación: Estados Unidos
Texto completo
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Imprimir
XML
PubMed Links
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Enfermedades de la Piel / Inhibidores de Proteínas Quinasas / Quinasas Janus / Compuestos Heterocíclicos con 2 Anillos / Indazoles / Enfermedades Pulmonares / Antiinflamatorios Tipo de estudio: Prognostic_studies Límite: Animals / Humans Idioma: En Revista: J Med Chem Asunto de la revista: QUIMICA Año: 2017 Tipo del documento: Article País de afiliación: Estados Unidos