Anti-emetic esters of cyproheptadine-3-carboxylic acid and struc

Details Anti-emetic esters of cyproheptadine-3-carboxylic acid and struc Anti-emetic esters of cyproheptadine-3-carboxylic acid and struc

1982-04-14

1983-11-01

Schwartz, Richard A.

Drug, bio-affecting and body treating compositions

Antigen, epitope, or other immunospecific immunoeffector

Parasitic organism or component thereof or substance...

546196, 546199, 546202, 546203, A61K 31445, C07D40112

Patent

active

044129998

ABSTRACT:
Certain esters of cyproheptadine-3-carboxylic acid and its bioisosteres are peripherally selective dopamine antagonists useful in the treatment of emesis caused by stimulation of dopamine receptors of the chemoreceptor trigger zone, as well as emesis and nausea resulting from other causes including post operative emesis, chronic pediatric vomiting, radiotherapy and chemotherapy induced emesis, and nausea associated with migrane attacks and dysmenorrhea or arising idiopathically.
They are also useful in the treatment of gastrointestinal disorders, such as gastro-oesophageal reflux caused by stimulation of dopamine receptors in the stomach or other causes and dyspepsia arising from delayed gastric emptying, post prandial dyspepsia or dyspepsia of unknown etiology.

REFERENCES:
patent: 3014911 (1961-12-01), Engelhardt
patent: 3981877 (1976-09-01), Prugh
patent: 4066772 (1978-01-01), Vandenberk
patent: 4072756 (1978-02-01), Ebnother et al.
patent: 4076714 (1978-02-01), Anderson et al.
patent: 4086350 (1978-04-01), Zirkle
patent: 4160031 (1979-07-01), Remy
March, J., Advanced Organic Chemistry, McGraw Hill, New York, 1968, p. 323.
Postgraduate Medical Journal, 55, (1979), Supplement (1), Hoffrand, B., (editor), pp. 3--4.

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