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Discovery of N-(piperidin-3-yl)-N-(pyridin-2-yl)piperidine/piperazine-1-carboxamides as small molecule inhibitors of PCSK9.
Londregan, Allyn T; Aspnes, Gary; Limberakis, Chris; Loria, Paula M; McClure, Kim F; Petersen, Donna N; Raymer, Brian; Ruggeri, Roger B; Wei, Liuqing; Xiao, Jun; Piotrowski, David W.
Affiliation
  • Londregan AT; Pfizer Medicinal Chemistry, Pfizer Inc., Eastern Point Road, Groton, CT 06340, United States. Electronic address: allyn.t.londregan@pfizer.com.
  • Aspnes G; Pfizer Medicinal Chemistry, Pfizer Inc., Eastern Point Road, Groton, CT 06340, United States.
  • Limberakis C; Pfizer Medicinal Chemistry, Pfizer Inc., Eastern Point Road, Groton, CT 06340, United States.
  • Loria PM; Pfizer Medicinal Chemistry, Pfizer Inc., Eastern Point Road, Groton, CT 06340, United States.
  • McClure KF; Pfizer Medicinal Chemistry, Pfizer Inc., Eastern Point Road, Groton, CT 06340, United States.
  • Petersen DN; Pfizer Medicinal Chemistry, Pfizer Inc., Eastern Point Road, Groton, CT 06340, United States.
  • Raymer B; Pfizer Medicinal Chemistry, Pfizer Inc., Eastern Point Road, Groton, CT 06340, United States.
  • Ruggeri RB; Pfizer Medicinal Chemistry, Pfizer Inc., Eastern Point Road, Groton, CT 06340, United States.
  • Wei L; Pfizer Medicinal Chemistry, Pfizer Inc., Eastern Point Road, Groton, CT 06340, United States.
  • Xiao J; Pfizer Medicinal Chemistry, Pfizer Inc., Eastern Point Road, Groton, CT 06340, United States.
  • Piotrowski DW; Pfizer Medicinal Chemistry, Pfizer Inc., Eastern Point Road, Groton, CT 06340, United States.
Bioorg Med Chem Lett ; 28(23-24): 3685-3688, 2018 12 15.
Article in En | MEDLINE | ID: mdl-30482620
ABSTRACT
A series of N-(piperidin-3-yl)-N-(pyridin-2-yl)piperidine/piperazine-1-carboxamides were identified as small molecule PCSK9 mRNA translation inhibitors. Analogues from this new chemical series, such as 4d and 4g, exhibited improved PCSK9 potency, ADME properties, and in vitro safety profiles when compared to earlier lead structures.
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Full text: 1 Database: MEDLINE Main subject: Piperidines / Protease Inhibitors / Amides / PCSK9 Inhibitors Limits: Animals / Humans Language: En Year: 2018 Type: Article
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Full text: 1 Database: MEDLINE Main subject: Piperidines / Protease Inhibitors / Amides / PCSK9 Inhibitors Limits: Animals / Humans Language: En Year: 2018 Type: Article