Pfizer Corporation

Robert M Wallis

Peter E Cross

David Alker

Brian Frank Johnson

Michael John Allen

Brian Robert Leaker

Darifenacin, and its pharmaceutically acceptable salts, are useful in the treatment of cognitive impairment. The invention also discloses the use of combinations of darifenacin, or a pharmaceutically acceptable salt thereof, with an acetylcholinesterase inhibitor, in the treatment of cognitive impairment.

Method of enhancing cognition

Synthetic intermediates of 1-arylethyl-3-substituted piperidines. The Intermediates include the 3R,S- and 3R-forms of the compounds having the following formulae: ##STR1##

1-arylethyl-3-substituted piperidines

Synthetic intermediates of 1-arylethyl-3-substituted piperidines. The Intermediates includes the 3R,S- and 3R-forms of the compounds having the following formulae: ##STR1##

A series of novel 1-(phenethyl) and 1-(2-heteroarylethyl)-3-substituted piperidine derivatives have been prepared, including their pharmaceutically acceptable salts and various novel key intermediates therefor. The 3-substituent present in these compounds is an unsubstituted or substituted diphenylmethoxy group or a diphenylmethoxy-derived group, while the 1-substituent is unsubstituted or substituted phenethyl or 1-(2-heteroarylethyl) wherein the heteroaryl moiety is thienyl, pyridyl or pyrazinyl. These compounds in the form of both their racemates and 3R-isomers, are useful in therapy as smooth muscle muscarinic receptor antagonists and therefore, are of value in the treatment diseases associated with altered motility and/or smooth muscle tone.

A series of novel 1-(phenethyl) and 1-(1-heteroarylethyl)-3-substituted piperidine derivatives have been prepared, including their pharmaceutically acceptable salts and various novel key intermediates therefor. The 3-substituent present in these compounds is an unsubstituted or substituted diphenylmethoxy group or a diphenylmethoxy-derived group, while the 1-substituent is unsubstituted or substituted phenethyl or 1-(2-heteroarylethyl) wherein the heteroaryl moiety is thienyl, pyridyl or pyrazinyl. These compounds in the form of both their racemates and 3R-isomers, are useful in therapy as smooth muscle muscarinic receptor antagonists and therefore, are of value in the treatment diseases associated with altered motility and/or smooth muscle tone. The most preferred compound is (3R)-diphenylmethoxy-1-(3,4-methylenedioxyphenethyl)piperidine. Methods for preparing these compounds from known starting materials are provided.

Growing community of inventors

Ramsgate, United Kingdom

Robert M Wallis