Muscarinic antagonists

US6458812B1 · kind B1 · utility

Assignee

• SCHERING CORPORATION · US

Inventors

• Brian McKittrick · New Vernon, US
• Guihua Guo · Plainsboro, US
• Zhaoning Zhu · Plainsboro, US
• Yuanzan C. Ye · New Brunswick, US

Key dates

• Filing date: Dec 17, 2001
• Grant date: Oct 1, 2002
• Expiry date: Dec 17, 2021

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D405/04
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

Amide derivatives of 1,4 di-substituted piperidine compounds of the formula: or a pharmaceutically acceptable salt, ester or solvate thereof, whereinR1 is optionally substituted cycloalkyl, cycloalkylalkyl, aryl, arylalkyl or heteroaryl;R2 is H, alkyl, or optionally substituted cycloalkyl, cycloalkylalkyl, heterocycloalkyl, bridged cycloalkyl, or bridged heterocycloalkyl;R3 is alkyl or —CH2OH; andR4 is H or alkyl;are muscarinic antagonists useful for treating cognitive disorders such as Alzheimer's disease. Pharmaceutical compositions and methods of preparation are also disclosed.