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US 2001/0037023 A1Published application
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.
Claims19
A compound of formula
- 5
- 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, arylsulfonylmethyl, 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 the carbon atom of (CH2)n group can be replaced by oxygen, nitrogen, or sulphur.
5 more elements
A compound selected from
- 2-(3,4-Dichlorophenyl)-5-(tetrahydro-pyran-4-yloxy)-pentanenitrile;
- 4-Cyano-4-(3,4-dichlorophenyl)-7-(tetrahydropyran-4-yloxy)-heptanoic acid ethyl ester;
- 5-(3,4-Dichlorophenyl)-5-[3-(tetrahydropyran-4-yloxy)-propyl]-piperidine;
- (R)-3-[3-(3,4-Dichlorophenyl)-piperidin-3-yl]-propan-1-ol(1s)-7,7-dimethyl-2-oxobicyclo[2.2.1]heptane-1-methanesulfonate (1:1) salt;
- [3-(3,4-Dichlorophenyl)-3-(3-hydroxy-propyl)-piperidin-1-yl]-phenyl-methanone;
- (R)-Methanesulfonic acid 3-[1-benzoyl-3-(3,4-dichloro-phenyl)-piperidin-3-yl]-propyl ester;
- (R)-[3-(3,4-Dichlorophenyl)-3-(3-iodopropyl)-piperidin-1-yl]-phenyl-methanone;
- and
- 4-Benzensulfonylmethyl-4-hydroxy-piperidine TFA.
6 more elements
Dependencies are inferred from the claim text.