Esters of cyproheptadine-3-carboxylic acid and structurally...

C - Chemistry – Metallurgy – 07 – D

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260/201.1

C07D 401/12 (2006.01) C07D 211/34 (2006.01) C07D 405/14 (2006.01) C07D 409/14 (2006.01) C07D 521/00 (2006.01)

Patent

CA 1203798

TITLE OF THE INVENTION Esters of Cyproheptadine-3-Carhoxylic Acid and Structurally Related Compounds ABSTRACT OF THE DISCLOSURE Certain esters of cvproheptadine-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, radio- therapy 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 etioloqy.

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