3-alkyl-3-phenyl-piperidines
AssigneeWarner-Lambert Company
InventorsMichael Huai Gu Chen, Fu-Zon Chung, Helen Tsenwhei Lee
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Abstract
The small nonpeptides of the instant invention are tachykinin antagonists. The compounds are highly selective and functional NK3 antagonists expected to be useful in the treatment of pain, depression, anxiety, panic, schizophrenia, neuralgia, addiction disorders, inflammatory diseases, gastrointestinal disorders, vascular disorders, and neuropathological disorders.
Claims3
A method of treating anxiety in a mammal suffering therefrom which comprises administering a therapeutically effective amount of a compound of formula
- or a pharmaceutically acceptable salt thereof wherein:
- R1 is straight or branched alkyl of from 5 to 15 carbon atoms, aryl, or heteroaryl;
- R2 is hydrogen, hydroxy, amino, or thiol;
- R3 is aryl or saturated or unsaturated heterocycle;
- R4 is from 1 to 4 groups each independently selected from halogen, alkyl, hydroxy, and alkoxy;
- n is an integer of from 2 to 6;
- and a carbon atom of (CH2)n group can be replaced by oxygen, nitrogen, or sulphur.
A method of treating anxiety in a mammal suffering therefrom which comprises administering a therapeutically effective amount of a compound of formula
- or a pharmaceutically acceptable salt thereof wherein:
- R1 is straight or branched alkyl of from 5 to 15 carbon atoms, aryl, or heteroaryl;
- R2 is hydrogen, hydroxy, amino, or thiol;
- R3 is arylsulfonylmethyl;
- R4 is from 1 to 4 groups each independently selected from halogen, lower alkyl, hydroxy, and lower alkoxy;
- n is an integer of from 2 to 6;
- and the carbon atom of (CH2)n group can be replaced by oxygen, nitrogen, or sulphur.
A method of treating anxiety in a mammal suffering therefrom which comprises administering therapeutically effective amount of a compound selected from:
- (S)-[3-[3-(4-Benzenesulfonylmethyl-4-hydroxy-piperidin-1-yl)-propyl]-3-(3,4-dichlorophenyl)-piperidin-1-yl]-phenyl-methanone monohydrochloride;
- and
- [3-[3-(4-Benzenesulfonylmethyl-4-hydroxy-piperidin-1-yl)propyl]-3-(3,4-dichlorophenyl)-piperidin-1-yl]-phenyl-methanone.
Dependencies are inferred from the claim text.