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Investigation of piperazine benzamides as human ß3 adrenergic receptor agonists for the treatment of overactive bladder.
Harper, Bart H; Wang, Liping; Zhu, Cheng; Kar, Nam F; Li, Bing; Moyes, Christopher R; Goble, Stephen D; Costa, Melissa; Dingley, Karen; Di Salvo, Jerry; Ha, Sookhee N; Hurley, Amanda; Li, Xiaofang; Miller, Randy R; Nagabukuro, Hiroshi; Salituro, Gino M; Smith, Sean; Struthers, Mary; Hale, Jeffrey J; Edmondson, Scott D; Berger, Richard.
Afiliação
  • Harper BH; Merck & Co., Inc., 126 E. Lincoln Ave., Rahway, NJ 07065, United States. Electronic address: bart_harper@merck.com.
  • Wang L; Merck & Co., Inc., 126 E. Lincoln Ave., Rahway, NJ 07065, United States.
  • Zhu C; Merck & Co., Inc., 126 E. Lincoln Ave., Rahway, NJ 07065, United States.
  • Kar NF; Merck & Co., Inc., 126 E. Lincoln Ave., Rahway, NJ 07065, United States.
  • Li B; Merck & Co., Inc., 126 E. Lincoln Ave., Rahway, NJ 07065, United States.
  • Moyes CR; Merck & Co., Inc., 126 E. Lincoln Ave., Rahway, NJ 07065, United States.
  • Goble SD; Merck & Co., Inc., 126 E. Lincoln Ave., Rahway, NJ 07065, United States.
  • Costa M; Merck & Co., Inc., 126 E. Lincoln Ave., Rahway, NJ 07065, United States.
  • Dingley K; Merck & Co., Inc., 126 E. Lincoln Ave., Rahway, NJ 07065, United States.
  • Di Salvo J; Merck & Co., Inc., 126 E. Lincoln Ave., Rahway, NJ 07065, United States.
  • Ha SN; Merck & Co., Inc., 126 E. Lincoln Ave., Rahway, NJ 07065, United States.
  • Hurley A; Merck & Co., Inc., 126 E. Lincoln Ave., Rahway, NJ 07065, United States.
  • Li X; Merck & Co., Inc., 126 E. Lincoln Ave., Rahway, NJ 07065, United States.
  • Miller RR; Merck & Co., Inc., 126 E. Lincoln Ave., Rahway, NJ 07065, United States.
  • Nagabukuro H; Merck & Co., Inc., 126 E. Lincoln Ave., Rahway, NJ 07065, United States.
  • Salituro GM; Merck & Co., Inc., 126 E. Lincoln Ave., Rahway, NJ 07065, United States.
  • Smith S; Merck & Co., Inc., 126 E. Lincoln Ave., Rahway, NJ 07065, United States.
  • Struthers M; Merck & Co., Inc., 126 E. Lincoln Ave., Rahway, NJ 07065, United States.
  • Hale JJ; Merck & Co., Inc., 126 E. Lincoln Ave., Rahway, NJ 07065, United States.
  • Edmondson SD; Merck & Co., Inc., 126 E. Lincoln Ave., Rahway, NJ 07065, United States.
  • Berger R; Merck & Co., Inc., 126 E. Lincoln Ave., Rahway, NJ 07065, United States.
Bioorg Med Chem Lett ; 27(4): 1094-1098, 2017 02 15.
Article em En | MEDLINE | ID: mdl-28089699
ABSTRACT
The synthesis of a novel class of piperazine benzamide (reverse amides) targeting the human ß3-adrenergic receptor for the treatment of overactive bladder (OAB) is described. The SAR studies directed towards maintaining well established ß3 potency and selectivities while improving the overall pharmacokinetic profile in the reverse amide class will be evaluated. The results and consequences associated with functional activity at the norepinephrine transporter (NET) will also be discussed.
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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Piperazinas / Bexiga Urinária Hiperativa / Agonistas de Receptores Adrenérgicos beta 3 Idioma: En Ano de publicação: 2017 Tipo de documento: Article
Texto completo
Imprimir
XML
PubMed Links
Buscar no Google

Texto completo: 1 Base de dados: MEDLINE Assunto principal: Piperazinas / Bexiga Urinária Hiperativa / Agonistas de Receptores Adrenérgicos beta 3 Idioma: En Ano de publicação: 2017 Tipo de documento: Article