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Discovery of N-(piperidin-3-yl)-N-(pyridin-2-yl)piperidine/piperazine-1-carboxamides as small molecule inhibitors of PCSK9 |
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| Authors: | Allyn T Londregan Gary Aspnes Chris Limberakis Paula M Loria Kim F McClure Donna N Petersen Brian Raymer Roger B Ruggeri Liuqing Wei Jun Xiao David W Piotrowski |
| Institution: | Pfizer Medicinal Chemistry, Pfizer Inc., Eastern Point Road, Groton, CT 06340, United States |
| 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. |
| Keywords: | PCSK9 SAR Medchem Parallel synthesis Urea |
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