Discovery of 5-phenoxy-1,3-dimethyl-1H-pyrazole-4-carboxamides as potent agonists of TGR5 via sequential combinatorial libraries

Autor: Londregan, Allyn T., Piotrowski, David W., Futatsugi, Kentaro, Warmus, Joseph S., Boehm, Markus, Carpino, Philip A., Chin, Janice E., Janssen, Ann M., Roush, Nicole S., Buxton, Joanne, Hinchey, Terri

Publikováno v: In Bioorganic & Medicinal Chemistry Letters 1 March 2013 23(5):1407-1411

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Identification of Tetrahydropyrido[4,3-d]pyrimidine Amides as a New Class of Orally Bioavailable TGR5 Agonists.

Autor: Piotrowski DW; Pfizer Worldwide Research and Development , Groton, Connecticut 06340, United States., Futatsugi K; Pfizer Worldwide Research and Development , Groton, Connecticut 06340, United States., Warmus JS; Pfizer Worldwide Research and Development , Groton, Connecticut 06340, United States., Orr ST; Pfizer Worldwide Research and Development , Groton, Connecticut 06340, United States., Freeman-Cook KD; Pfizer Worldwide Research and Development , Groton, Connecticut 06340, United States., Londregan AT; Pfizer Worldwide Research and Development , Groton, Connecticut 06340, United States., Wei L; Pfizer Worldwide Research and Development , Groton, Connecticut 06340, United States., Jennings SM; Pfizer Worldwide Research and Development , Groton, Connecticut 06340, United States., Herr M; Pfizer Worldwide Research and Development , Groton, Connecticut 06340, United States., Coffey SB; Pfizer Worldwide Research and Development , Groton, Connecticut 06340, United States., Jiao W; Pfizer Worldwide Research and Development , Groton, Connecticut 06340, United States., Storer G; Pfizer Worldwide Research and Development , Groton, Connecticut 06340, United States., Hepworth D; Pfizer Worldwide Research and Development , Groton, Connecticut 06340, United States., Wang J; Pfizer Worldwide Research and Development , Groton, Connecticut 06340, United States., Lavergne SY; Pfizer Worldwide Research and Development , Groton, Connecticut 06340, United States., Chin JE; Pfizer Worldwide Research and Development , Groton, Connecticut 06340, United States., Hadcock JR; Pfizer Worldwide Research and Development , Groton, Connecticut 06340, United States., Brenner MB; Pfizer Worldwide Research and Development , Groton, Connecticut 06340, United States., Wolford AC; Pfizer Worldwide Research and Development , Groton, Connecticut 06340, United States., Janssen AM; Pfizer Worldwide Research and Development , Groton, Connecticut 06340, United States., Roush NS; Pfizer Worldwide Research and Development , Groton, Connecticut 06340, United States., Buxton J; Pfizer Worldwide Research and Development , Groton, Connecticut 06340, United States., Hinchey T; Pfizer Worldwide Research and Development , Groton, Connecticut 06340, United States., Kalgutkar AS; Pfizer Worldwide Research and Development , Groton, Connecticut 06340, United States., Sharma R; Pfizer Worldwide Research and Development , Groton, Connecticut 06340, United States., Flynn DA; Pfizer Worldwide Research and Development , Groton, Connecticut 06340, United States.

Publikováno v: ACS medicinal chemistry letters [ACS Med Chem Lett] 2012 Nov 09; Vol. 4 (1), pp. 63-8. Date of Electronic Publication: 2012 Nov 09 (Print Publication: 2013).