Title: Cilomilast
CAS Registry Number: 153259-65-5
CAS Name: cis-4-Cyano-4-[3-(cyclopentyloxy)-4-methoxyphenyl]cyclohexanecarboxylic acid
Manufacturers' Codes: SB-207499
Trademarks: Ariflo (GSK)
Molecular Formula: C20H25NO4
Molecular Weight: 343.42
Percent Composition: C 69.95%, H 7.34%, N 4.08%, O 18.64%
Literature References: Selective phosphodiesterase 4 (PDE4) inhibitor. Prepn: S. B. Christensen, WO 9319749; idem, US 5552438 (1993, 1996 both to SmithKline Beecham); idem et al., J. Med. Chem. 41, 821 (1998). Anti-inflammatory activity: M. S. Barnette et al., J. Pharmacol. Exp. Ther. 284, 420 (1998); D. E. Griswold et al., ibid. 705. Pharmacology and therapeutic potential in asthma and chronic obstructive pulmonary disease (COPD): T. J. Torphy et al., Pulm. Pharmacol. Ther. 12, 131-135 (1999). Clinical pharmacokinetics and bioavailability: B. D. Zussman et al., Pharmacotherapy 21, 653 (2001). Clinical trial in COPD: C. H. Compton et al., Lancet 358, 265 (2001). Review of pharmacology and clinical experience: M. A. Giembycz, Expert Opin. Invest. Drugs 10, 1361-1379 (2001).
Properties: White solid, mp 157°.
Melting point: mp 157°
Therap-Cat: Antiasthmatic; in treatment of chronic obstructive pulmonary disease.
Keywords: Antiasthmatic (Nonbronchodilator); Phosphodiesterase Inhibitor. |