Synthetic methods and intermediates for stereoisomeric compounds useful for the treatment of gastrointestinal and central nervous system disorders

Abstract

The subject invention provides methods and / or processes for making stereoisomeric compounds of formula (X): wherein the variables are as defined herein, and compositions for the safe and effective treatment of various gastrointestinal disorders including, but not limited to, gastroparesis, gastroesophageal reflux and related conditions. The compounds of the subject invention are also useful in treating a variety of conditions involving the central nervous system.

Description

[0001] This application claims priority to US Provisional Application No. 60 / 713,149, filed August 31, 2005, and US Provisional Application No. 60 / 747,762, filed May 19, 2006. Background technique

[0002] Cisapride is one of a class of compounds known as benzamide derivatives, whose parent compound is metoclopramide. US Patent Nos. 4,962,115 and 5,057,525 (collectively "Van Daele" and incorporated herein by reference in their entirety) disclose N-(3-hydroxy-4-piperidinyl)benzamides of cisapride. Van Daele discloses that these compounds and their pharmaceutically acceptable acid addition salts and their stereoisomeric forms stimulate the motility of the gastrointestinal system.

[0003] As a class of compounds, these benzamide derivatives have several remarkable pharmacological effects. The pronounced pharmacological activity of benzamide derivatives is attributed to their effects on the nervous system regulated by the neurotransmitter serotonin. It has been generally accept...

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