Biarylsulfonamide CCR9 inhibitors for inflammatory bowel disease.

Zhang, Jing; Romero, Jan; Chan, Audrey; Goss, Jennifer; Stucka, Sabrina; Cross, Jason; Chamberlain, Brian; Varoglu, Mustafa; Chandonnet, Haoqun; Ryan, Dominic; Lippa, Blaise

Zhang, Jing; Romero, Jan; Chan, Audrey; Goss, Jennifer; Stucka, Sabrina; Cross, Jason; Chamberlain, Brian; Varoglu, Mustafa; Chandonnet, Haoqun; Ryan, Dominic; Lippa, Blaise.

Afiliação

Zhang J; Cubist Pharmaceuticals, 65 Hayden Avenue, Lexington, MA 02421, United States. Electronic address: jackzhang49@yahoo.com.
Romero J; Cubist Pharmaceuticals, 65 Hayden Avenue, Lexington, MA 02421, United States.
Chan A; Cubist Pharmaceuticals, 65 Hayden Avenue, Lexington, MA 02421, United States.
Goss J; Cubist Pharmaceuticals, 65 Hayden Avenue, Lexington, MA 02421, United States.
Stucka S; Cubist Pharmaceuticals, 65 Hayden Avenue, Lexington, MA 02421, United States.
Cross J; Cubist Pharmaceuticals, 65 Hayden Avenue, Lexington, MA 02421, United States.
Chamberlain B; Cubist Pharmaceuticals, 65 Hayden Avenue, Lexington, MA 02421, United States.
Varoglu M; Cubist Pharmaceuticals, 65 Hayden Avenue, Lexington, MA 02421, United States.
Chandonnet H; Cubist Pharmaceuticals, 65 Hayden Avenue, Lexington, MA 02421, United States.
Ryan D; Cubist Pharmaceuticals, 65 Hayden Avenue, Lexington, MA 02421, United States.
Lippa B; Cubist Pharmaceuticals, 65 Hayden Avenue, Lexington, MA 02421, United States.

Bioorg Med Chem Lett ; 25(17): 3661-4, 2015 Sep 01.

Article em En | MEDLINE | ID: mdl-26117562

ABSTRACT

ABSTRACT

Inflammatory bowel disease, including Crohn's disease and ulcerative colitis, affects millions of people worldwide. CCR9 has been shown to be a key chemokine receptor mediating the local inflammatory responses in the GI tract. The CCR9 inhibitor Vercirnon advanced to phase 3 clinical trials, but carries several liabilities which we sought to improve.

Assuntos

Doenças Inflamatórias Intestinais/tratamento farmacológico; Receptores CCR/antagonistas & inibidores; Sulfonamidas/química; Sulfonamidas/farmacologia; Animais; Técnicas de Química Sintética; Avaliação Pré-Clínica de Medicamentos/métodos; Humanos; Concentração Inibidora 50; Camundongos; Relação Estrutura-Atividade

Palavras-chave

CCR9; Crohn's disease; IBD; Sulfonamide; Ulcerative colitis

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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Sulfonamidas / Doenças Inflamatórias Intestinais / Receptores CCR Idioma: En Ano de publicação: 2015 Tipo de documento: Article

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