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

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

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546196, 546199, 546202, 514322, 514324, 514326, 514872, A61K 31445, C07D40104, C07D40112

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active

045228213

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 migraine 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: 4412999 (1983-11-01), Remy et al.
March, J., Advanced Organic Chemistry, McGraw Hill, New York, 1968, p. 323.

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