Roflumilast
Title: Roflumilast
CAS Registry Number: 162401-32-3
CAS Name: 3-(Cyclopropylmethoxy)-N-(3,5-dichloro-4-pyridinyl)-4-(difluoromethoxy)benzamide
Manufacturers' Codes: BY-217
Trademarks: Daxas (Altana)
Molecular Formula: C17H14Cl2F2N2O3
Molecular Weight: 403.21
Percent Composition: C 50.64%, H 3.50%, Cl 17.59%, F 9.42%, N 6.95%, O 11.90%
Literature References: Selective phosphodiesterase 4 (PDE4) inhibitor. Prepn: D. Flockerzi et al., WO 9501338; H. Amschler, US 5712298 (1995, 1998 both to Byk-Gulden). Pharmacology: A. Hatzelmann, C. Schudt, J. Pharmacol. Exp. Ther. 297, 267 (2001); D. S. Bundschuh et al., ibid. 280. Clinical evaluation in allergic rhinitis: B. M. W. Schmidt et al., J. Allergy Clin. Immunol. 108, 530 (2001); in exercise-induced asthma: W. Timmer et al., J. Clin. Pharmacol. 42, 297 (2002); in COPD: K. F. Rabe et al., Lancet 366, 563 (2005). Comparative review with cilomilast: M. A. Giembycz, Monaldi Arch. Chest Dis. 57, 48-64 (2002).
Properties: Crystals from isopropanol, mp 158°.
Melting point: mp 158°
Therap-Cat: Antiasthmatic; in treatment of chronic obstructive pulmonary disease.
Keywords: Antiasthmatic (Nonbronchodilator); Phosphodiesterase Inhibitor.

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