title: Benzimidazole-2-pyrazole HIF Prolyl 4-Hydroxylase Inhibitors as Oral Erythropoietin Secretagogues.
abstract: HIF prolyl 4-hydroxylases (PHD) are a family of enzymes that mediate key physiological responses to hypoxia by modulating the levels of hypoxia inducible factor 1-α (HIF1α). Certain benzimidazole-2-pyrazole carboxylates were discovered to be PHD2 inhibitors using ligand- and structure-based methods and found to be potent, orally efficacious stimulators of erythropoietin secretion in vivo.
authors.affiliation: Johnson & Johnson Pharmaceutical Research and Development, L.L.C, 3210 Merryfield Row, San Diego, California 92121, United States.
authors.forename: Mark D
authors.initials: MD
authors.lastname: Rosen
authors.affiliation: Johnson & Johnson Pharmaceutical Research and Development, L.L.C, 3210 Merryfield Row, San Diego, California 92121, United States.
authors.forename: Hariharan
authors.initials: H
authors.lastname: Venkatesan
authors.affiliation: Johnson & Johnson Pharmaceutical Research and Development, L.L.C, 3210 Merryfield Row, San Diego, California 92121, United States.
authors.forename: Hillary M
authors.initials: HM
authors.lastname: Peltier
authors.affiliation: Johnson & Johnson Pharmaceutical Research and Development, L.L.C, 3210 Merryfield Row, San Diego, California 92121, United States.
authors.forename: Scott D
authors.initials: SD
authors.lastname: Bembenek
authors.affiliation: Johnson & Johnson Pharmaceutical Research and Development, L.L.C, 3210 Merryfield Row, San Diego, California 92121, United States.
authors.forename: Kimon C
authors.initials: KC
authors.lastname: Kanelakis
authors.affiliation: Johnson & Johnson Pharmaceutical Research and Development, L.L.C, 3210 Merryfield Row, San Diego, California 92121, United States.
authors.forename: Lucy X
authors.initials: LX
authors.lastname: Zhao
authors.affiliation: Johnson & Johnson Pharmaceutical Research and Development, L.L.C, 3210 Merryfield Row, San Diego, California 92121, United States.
authors.forename: Barry E
authors.initials: BE
authors.lastname: Leonard
authors.affiliation: Johnson & Johnson Pharmaceutical Research and Development, L.L.C, 3210 Merryfield Row, San Diego, California 92121, United States.
authors.forename: Frances M
authors.initials: FM
authors.lastname: Hocutt
authors.affiliation: Johnson & Johnson Pharmaceutical Research and Development, L.L.C, 3210 Merryfield Row, San Diego, California 92121, United States.
authors.forename: Xiaodong
authors.initials: X
authors.lastname: Wu
authors.affiliation: Johnson & Johnson Pharmaceutical Research and Development, L.L.C, 3210 Merryfield Row, San Diego, California 92121, United States.
authors.forename: Heather L
authors.initials: HL
authors.lastname: Palomino
authors.affiliation: Johnson & Johnson Pharmaceutical Research and Development, L.L.C, 3210 Merryfield Row, San Diego, California 92121, United States.
authors.forename: Theresa I
authors.initials: TI
authors.lastname: Brondstetter
authors.affiliation: Johnson & Johnson Pharmaceutical Research and Development, L.L.C, 3210 Merryfield Row, San Diego, California 92121, United States.
authors.forename: Peter V
authors.initials: PV
authors.lastname: Haugh
authors.affiliation: Johnson & Johnson Pharmaceutical Research and Development, L.L.C, 3210 Merryfield Row, San Diego, California 92121, United States.
authors.forename: Laurence
authors.initials: L
authors.lastname: Cagnon
authors.affiliation: Johnson & Johnson Pharmaceutical Research and Development, L.L.C, 3210 Merryfield Row, San Diego, California 92121, United States.
authors.forename: Wen
authors.initials: W
authors.lastname: Yan
authors.affiliation: Johnson & Johnson Pharmaceutical Research and Development, L.L.C, 3210 Merryfield Row, San Diego, California 92121, United States.
authors.forename: Lisa A
authors.initials: LA
authors.lastname: Liotta
authors.affiliation: Johnson & Johnson Pharmaceutical Research and Development, L.L.C, 3210 Merryfield Row, San Diego, California 92121, United States.
authors.forename: Andrew
authors.initials: A
authors.lastname: Young
authors.affiliation: Johnson & Johnson Pharmaceutical Research and Development, L.L.C, 3210 Merryfield Row, San Diego, California 92121, United States.
authors.forename: Tara
authors.initials: T
authors.lastname: Mirzadegan
authors.affiliation: Johnson & Johnson Pharmaceutical Research and Development, L.L.C, 3210 Merryfield Row, San Diego, California 92121, United States.
authors.forename: Nigel P
authors.initials: NP
authors.lastname: Shankley
authors.affiliation: Johnson & Johnson Pharmaceutical Research and Development, L.L.C, 3210 Merryfield Row, San Diego, California 92121, United States.
authors.forename: Terrance D
authors.initials: TD
authors.lastname: Barrett
authors.affiliation: Johnson & Johnson Pharmaceutical Research and Development, L.L.C, 3210 Merryfield Row, San Diego, California 92121, United States.
authors.forename: Michael H
authors.initials: MH
authors.lastname: Rabinowitz
keywords: HIF; PHD inhibitors; Prolyl 4-hydroxylase inhibitors; anemia; epo; erythropoietin; erythropoietin stimulating agents; hypoxia inducible factor