1-arylethyl-3-substituted piperidines

Details 1-arylethyl-3-substituted piperidines 1-arylethyl-3-substituted piperidines

1989-07-06

1992-02-18

Lee, Mary C.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

514319, 514320, 514324, 514325, 546196, 546197, 546202, 546204, 546205, A61K 31445, A61K 3155, C07D40506, C07D40514

Patent

active

050895052

ABSTRACT:
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.

REFERENCES:
patent: 2745837 (1956-05-01), Papa et al.
patent: 2974146 (1961-03-01), Biel

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