Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor.

Zeng, Qingbei; Wang, Jiabing; Cheng, Ziqiang; Chen, Kan; Johnström, Peter; Varnäs, Katarina; Li, David Yunzhi; Yang, Zhen Fan; Zhang, Xiaolin

Zeng, Qingbei; Wang, Jiabing; Cheng, Ziqiang; Chen, Kan; Johnström, Peter; Varnäs, Katarina; Li, David Yunzhi; Yang, Zhen Fan; Zhang, Xiaolin.

Afiliação

Zeng Q; Innovation Center China, Asia & Emerging Markets iMed, AstraZeneca Innovative Medicines and Early Development , 199 Liangjing Road, Zhangjiang Hi-Tech Park, Shanghai 201203, China.
Wang J; Innovation Center China, Asia & Emerging Markets iMed, AstraZeneca Innovative Medicines and Early Development , 199 Liangjing Road, Zhangjiang Hi-Tech Park, Shanghai 201203, China.
Cheng Z; Innovation Center China, Asia & Emerging Markets iMed, AstraZeneca Innovative Medicines and Early Development , 199 Liangjing Road, Zhangjiang Hi-Tech Park, Shanghai 201203, China.
Chen K; Innovation Center China, Asia & Emerging Markets iMed, AstraZeneca Innovative Medicines and Early Development , 199 Liangjing Road, Zhangjiang Hi-Tech Park, Shanghai 201203, China.
Johnström P; AstraZeneca Translational Centre, Personal Healthcare and Biomarkers iMed, AstraZeneca R&D, Karolinska Institutet , Department of Clinical Neuroscience, R5:U1 Karolinska University Hospital, SE-171 76 Stockholm, Sweden.
Varnäs K; Karolinska Institutet , Department of Clinical Neuroscience, Centre for Psychiatry Research, R5:02 Karolinska University Hospital, SE-171 76 Stockholm, Sweden.
Li DY; Karolinska Institutet , Department of Clinical Neuroscience, Centre for Psychiatry Research, R5:02 Karolinska University Hospital, SE-171 76 Stockholm, Sweden.
Yang ZF; Innovation Center China, Asia & Emerging Markets iMed, AstraZeneca Innovative Medicines and Early Development , 199 Liangjing Road, Zhangjiang Hi-Tech Park, Shanghai 201203, China.
Zhang X; Innovation Center China, Asia & Emerging Markets iMed, AstraZeneca Innovative Medicines and Early Development , 199 Liangjing Road, Zhangjiang Hi-Tech Park, Shanghai 201203, China.

J Med Chem ; 58(20): 8200-15, 2015 Oct 22.

Article em En | MEDLINE | ID: mdl-26313252

Assuntos

Sistema Nervoso Central/metabolismo; Receptores ErbB/antagonistas & inibidores; Piperazinas/farmacologia; Inibidores de Proteínas Quinases/farmacologia; Proteínas Tirosina Quinases/antagonistas & inibidores; Quinazolinas/farmacologia; Animais; Encéfalo/diagnóstico por imagem; Encéfalo/metabolismo; Neoplasias Encefálicas/tratamento farmacológico; Neoplasias Encefálicas/secundário; Ensaios Clínicos Fase I como Assunto; Cães; Descoberta de Drogas; Macaca fascicularis; Masculino; Camundongos; Piperazinas/síntese química; Piperazinas/uso terapêutico; Tomografia por Emissão de Pósitrons; Inibidores de Proteínas Quinases/síntese química; Inibidores de Proteínas Quinases/uso terapêutico; Quinazolinas/síntese química; Quinazolinas/uso terapêutico; Ratos; Ratos Wistar; Ensaios Antitumorais Modelo de Xenoenxerto

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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Piperazinas / Quinazolinas / Proteínas Tirosina Quinases / Sistema Nervoso Central / Inibidores de Proteínas Quinases / Receptores ErbB Tipo de estudo: Prognostic_studies Limite: Animals Idioma: En Revista: J Med Chem Ano de publicação: 2015 Tipo de documento: Article

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