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Discovery of a new series of potent prostacyclin receptor agonists with in vivo activity in rat.
Tran, Thuy-Anh; Shin, Young-Jun; Kramer, Bryan; Choi, Juyi; Zou, Ning; Vallar, Pureza; Martens, Peter; Boatman, P Douglas; Adams, John W; Ramirez, Juan; Shi, Yunqing; Morgan, Michael; Unett, David J; Chang, Steve; Shu, Hsin-Hui; Tung, Shiu-Feng; Semple, Graeme.
Afiliação
  • Tran TA; Arena Pharmaceuticals, 6154, Nancy Ridge Drive, San Diego, CA 92121, USA.
  • Shin YJ; Arena Pharmaceuticals, 6154, Nancy Ridge Drive, San Diego, CA 92121, USA.
  • Kramer B; Arena Pharmaceuticals, 6154, Nancy Ridge Drive, San Diego, CA 92121, USA.
  • Choi J; Arena Pharmaceuticals, 6154, Nancy Ridge Drive, San Diego, CA 92121, USA.
  • Zou N; Arena Pharmaceuticals, 6154, Nancy Ridge Drive, San Diego, CA 92121, USA.
  • Vallar P; Arena Pharmaceuticals, 6154, Nancy Ridge Drive, San Diego, CA 92121, USA.
  • Martens P; Arena Pharmaceuticals, 6154, Nancy Ridge Drive, San Diego, CA 92121, USA.
  • Boatman PD; Arena Pharmaceuticals, 6154, Nancy Ridge Drive, San Diego, CA 92121, USA.
  • Adams JW; Arena Pharmaceuticals, 6154, Nancy Ridge Drive, San Diego, CA 92121, USA.
  • Ramirez J; Arena Pharmaceuticals, 6154, Nancy Ridge Drive, San Diego, CA 92121, USA.
  • Shi Y; Arena Pharmaceuticals, 6154, Nancy Ridge Drive, San Diego, CA 92121, USA.
  • Morgan M; Arena Pharmaceuticals, 6154, Nancy Ridge Drive, San Diego, CA 92121, USA.
  • Unett DJ; Arena Pharmaceuticals, 6154, Nancy Ridge Drive, San Diego, CA 92121, USA.
  • Chang S; Arena Pharmaceuticals, 6154, Nancy Ridge Drive, San Diego, CA 92121, USA.
  • Shu HH; Arena Pharmaceuticals, 6154, Nancy Ridge Drive, San Diego, CA 92121, USA.
  • Tung SF; Arena Pharmaceuticals, 6154, Nancy Ridge Drive, San Diego, CA 92121, USA.
  • Semple G; Arena Pharmaceuticals, 6154, Nancy Ridge Drive, San Diego, CA 92121, USA. Electronic address: gsemple@arenapharm.com.
Bioorg Med Chem Lett ; 25(5): 1030-5, 2015 Mar 01.
Article em En | MEDLINE | ID: mdl-25666818
ABSTRACT
The design and synthesis of two closely related series of prostacyclin receptor agonist compounds that showed excellent human IP receptor potency and efficacy is described. Compounds from this series showed in vivo activity after SC dosing in the monocrotaline model of PAH in rat.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Receptores de Prostaglandina / Descoberta de Drogas / Hipertensão Pulmonar Limite: Animals / Humans Idioma: En Revista: Bioorg Med Chem Lett Assunto da revista: BIOQUIMICA / QUIMICA Ano de publicação: 2015 Tipo de documento: Article País de afiliação: Estados Unidos

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Receptores de Prostaglandina / Descoberta de Drogas / Hipertensão Pulmonar Limite: Animals / Humans Idioma: En Revista: Bioorg Med Chem Lett Assunto da revista: BIOQUIMICA / QUIMICA Ano de publicação: 2015 Tipo de documento: Article País de afiliação: Estados Unidos