Addition/Correction pubs.acs.org/jmc
Identification, Synthesis, and Biological Evaluation of 6‑[(6R)‑2-(4-Fluorophenyl)-6-(hydroxymethyl)-4,5,6,7tetrahydropyrazolo[1,5‑a]pyrimidin-3-yl]-2(2-methylphenyl)pyridazin-3(2H)‑one (AS1940477), a Potent p38 MAP Kinase Inhibitor Toru Asano,* Hitoshi Yamazaki, Chiyoshi Kasahara, Hirokazu Kubota, Toru Kontani, Yu Harayama, Kazuki Ohno, Hidekazu Mizuhara, Masaharu Yokomoto, Keiji Misumi, Tomohiko Kinoshita, Mitsuaki Ohta, and Makoto Takeuchi J. Med. Chem. 2012, 55 (17), 7772−7785. DOI: 10.1021/jm3008008 Page 7776. In Table 3, footnotes in this table should be following table. That is to say, doses of 3d, 3e, 3f, and 3g should be 0.32 mg/kg instead of 1.0 mg/kg. Table 3. Pharmacokinetic Parameters of Selected TNFα Release Inhibitors in Rata ivb
2ac 3d 3e 3f 3g 3jc
pob
CLtot (mL/min/kg)
Vss (L/kg)
t1/2 (h)
AUC (ng·h/mL)
F (%)
20.64 4.80 9.53 2.17 4.56 3.80
0.65 1.23 4.21 0.77 1.11 0.98
0.66 3.89 9.01 5.15 3.82 5.95
235 763 457 1518 1217 4502
28.6 67.7 81.0 61.8 103.6 100.5
a
Pharmacokinetics were determined at a dose of 0.32 mg/kg iv and po in SD rats for 3d−3g. bResults expressed as the mean ± SD of n = 3. cPharmacokinetics were determined at a dose of 1.0 mg/kg iv and po in SD rats for 2a and 3j.
Published: August 19, 2014 © 2014 American Chemical Society
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dx.doi.org/10.1021/jm501222p | J. Med. Chem. 2014, 57, 7143−7143
