US2004044039A1PendingUtilityA1

Antiemetic compositions of optically pure (+) norcisapride

Assignee: SEPRACOR INCPriority: Jul 19, 1996Filed: Sep 3, 2003Published: Mar 4, 2004
Est. expiryJul 19, 2016(expired)· nominal 20-yr term from priority
A61P 1/04A61P 1/10A61P 1/14A61P 1/06A61P 1/00A61K 31/4468A61K 31/495A61K 31/445
57
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Claims

Abstract

Compositons employing and methods utilizing the optically pure (+) isomer of norcisapride are disclosed. This compound has surprisingly been found to be a potent drug for the treatment of disorders of the central nervous system. The compound, (+) norcisapride, has also been found to be a potent antiemetic agent. Finally, the (+) isomer of norcisapride also avoids certain adverse side effects and certain adverse drug interactions.

Claims

exact text as granted — not AI-modified
What is claimed is:  
     
         1 . A method of treating or preventing a disorder caused by gastrointestinal motility dysfunction in a human which comprises administering to said human a therapeutically effective amount of (+) norcisapride, or a pharmaceutically acceptable salt thereof, substantially free of its (−) stereoisomer.  
     
     
         2 . The method of  claim 1 , wherein said disorder is gastro-estophageal reflux disease.  
     
     
         3 . The method of  claim 1 , wherein said disorder is dyspepsia.  
     
     
         4 . The method of  claim 1 , wherein said disorder is gastroparesis.  
     
     
         5 . The method of  claim 1 , wherein said disorder is constipation.  
     
     
         6 . The method of  claim 1 , wherein said disorder is intestinal pseudo-obstruction.  
     
     
         7 . The method of  claim 1 , wherein said (+) norcisapride is administered orally.  
     
     
         8 . The method of  claim 7 , wherein said (+) norcisapride is administered as a tablet.  
     
     
         9 . The method of  claim 1 , wherein said (+) norcisapride is administered parenterally.  
     
     
         10 . The method of  claim 1 , wherein said amount of (+) norcisapride, or a pharmaceutically acceptable salt thereof, is from about 0.5 to about 500 mg per day.  
     
     
         11 . The method of  claim 10 , wherein said amount is from about 1 mg to about 250 mg per day.  
     
     
         12 . The method of  claim 11 , wherein said amount is from about 5 mg to about 100 mg per day.  
     
     
         13 . The method of  claim 10 , wherein said amount is administered in unit doses from one to four times a day.  
     
     
         14 . The method of  claim 1 , wherein said amount of (+) norcisapride, or a pharmaceutically acceptable salt thereof, is at least about 90% by weight of the total weight of norcisapride.  
     
     
         15 . A method of eliciting a prokinetic effect in a human to treat gastro-esophageal reflux disease in said human which comprises administering to said human a therapeutically effective amount of (+) norcisapride, or a pharmaceutically acceptable salt thereof, substantially free of its (−) stereoisomer.  
     
     
         16 . The method of  claim 15 , wherein said (+) norcisapride is administered parenterally or orally as a tablet, a capsule or a liquid suspension.  
     
     
         17 . The method of  claim 16 , wherein said amount of (+) norcisapride, or a pharmaceutically acceptable salt thereof, administered is from about 0.5 to about 500 mg per day.  
     
     
         18 . The method of  claim 17 , wherein the amount administered is from about 1 mg to about 250 mg per day.  
     
     
         19 . The method of  claim 18 , wherein the amount administered is from about 5 mg to 100 mg per day.  
     
     
         20 . The method of  claim 16 , wherein said amount is administered in divided doses from one to four times per day.  
     
     
         21 . The method of  claim 15 , wherein the amount of (+) norcisapride or a pharmaceutically acceptable salt thereof is at least about 90% by weight of the total weight of norcisapride.  
     
     
         22 . The method of  claim 15 , wherein said (+) norcisapride or a pharmaceutically acceptable salt thereof, substantially free of its (−) stereoisomer is administered with a pharmaceutically acceptable carrier.  
     
     
         23 . The method of  claim 15 , wherein said (+) norcisapride or a pharmaceutically acceptable salt thereof, substantially free of its (−) stereoisomer is administered with a pharmaceutically acceptable carrier.  
     
     
         24 . A pharmaceutical composition suitable for administration to a human which comprises (+) norcisapride or a pharmaceutically acceptable salt thereof, substantially free of its (−) stereoisomer; and a pharmaceutically acceptable carrier or excipient.

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