5307. Ketotifen

Nomenclature

CAS number: 34580-13-7
4,9-Dihydro-4-(1-methyl-4-piperidinylidene)-10H-benzo[4,5]cyclohepta[1,2-b]thiophen-10-one.
C19H19NOS; mol wt 309.43.
C 73.75%, H 6.19%, N 4.53%, O 5.17%, S 10.36%.

Description and references

Prepn: J. P. Bourquin et al., DE 2111071; eidem, US 3682930 (1971, 1972 both to Sandoz); E. Waldvogel et al., Helv. Chim. Acta 59, 866 (1976). Pharmacology: U. Martin, D. Roemer, Arzneim.-Forsch. 28, 770 (1978). Clinical studies: B. Wüthrick, P. Radielovic, Dtsch. Med. Wochenschr. 103, 1865 (1978); H. Gmür, M. Scherrer, Schweiz. Med. Wochenschr. 109, 881 (1979). Review: U. Martin et al., in Pharmacological and Biochemical Properties of Drug Substances vol. 3, M. E. Goldberg, Ed. (Am. Pharm. Assoc., Washington, DC, 1981) pp 424-460. Review of clinical experience in asthma and allergy: S. M. Grant et al., Drugs 40, 412-448 (1990).

Chemical structure

Properties

Crystals from ethyl acetate, mp 152-153°.

Derivative

Fumarate.

Nomenclature

CAS number: 34580-14-8
HC-20511; Totifen (Chiesi); Zaditen (Novartis); Zaditor (Novartis); Zasten (Novartis).
C19H19NOS.C4H4O4; mol wt 425.50.
C 64.92%, H 5.45%, N 3.29%, O 18.80%, S 7.54%.

Properties

Crystals, mp 192° (dec).

Therapeutic Category

Antiasthmatic; antiallergic.

Keywords

Antiasthmatic (Nonbronchodilator); Antiallergic