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Optimization of physicochemical properties of pyridone-based EP3 receptor antagonists.
Zhang, Xuqing; Zhu, Bin; Guo, Lili; Bakaj, Ivona; Rankin, Matthew; Ho, George; Kauffman, Jack; Lee, Seunghun P; Norquay, Lisa; Macielag, Mark.
Affiliation
  • Zhang X; Discovery Sciences, Discovery Chemistry, Janssen Research & Development, LLC, 1400 McKean Road, Box 776, Spring House, PA 19477, United States. Electronic address: xzhang@proteovanttx.com.
  • Zhu B; Discovery Sciences, Discovery Chemistry, Janssen Research & Development, LLC, 1400 McKean Road, Box 776, Spring House, PA 19477, United States.
  • Guo L; Cardiovascular and Metabolism Research, Janssen Research & Development, LLC, 1400 McKean Road, Box 776, Spring House, PA 19477, United States.
  • Bakaj I; Cardiovascular and Metabolism Research, Janssen Research & Development, LLC, 1400 McKean Road, Box 776, Spring House, PA 19477, United States.
  • Rankin M; Cardiovascular and Metabolism Research, Janssen Research & Development, LLC, 1400 McKean Road, Box 776, Spring House, PA 19477, United States.
  • Ho G; Cardiovascular and Metabolism Research, Janssen Research & Development, LLC, 1400 McKean Road, Box 776, Spring House, PA 19477, United States.
  • Kauffman J; Discovery Sciences, Lead Discovery, Janssen Research & Development, LLC, 1400 McKean Road, Box 776, Spring House, PA 19477, United States.
  • Lee SP; Cardiovascular and Metabolism Research, Janssen Research & Development, LLC, 1400 McKean Road, Box 776, Spring House, PA 19477, United States.
  • Norquay L; Cardiovascular and Metabolism Research, Janssen Research & Development, LLC, 1400 McKean Road, Box 776, Spring House, PA 19477, United States.
  • Macielag M; Discovery Sciences, Discovery Chemistry, Janssen Research & Development, LLC, 1400 McKean Road, Box 776, Spring House, PA 19477, United States.
Bioorg Med Chem Lett ; 47: 128172, 2021 09 01.
Article in En | MEDLINE | ID: mdl-34091043
A novel series of pyridone-based EP3 receptor antagonists was optimized for good physical properties and oral bioavailability in rodents. The lead compounds 3h, 3l and 4d displayed good in vitro profiles, moderate to good metabolic stability and good rodent PK profiles with low clearance, high oral exposure and acceptable half-life.
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Pyridones / Receptors, Prostaglandin E, EP3 Subtype Limits: Humans Language: En Journal: Bioorg Med Chem Lett Year: 2021 Document type: Article
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Pyridones / Receptors, Prostaglandin E, EP3 Subtype Limits: Humans Language: En Journal: Bioorg Med Chem Lett Year: 2021 Document type: Article