Morpholinone and morpholine derivatives and uses thereof

US6218390A · kind A · utility

Assignee

• Synaptic Pharmaceutical Corporation · US

Inventors

• Bharat Lagu · Maywood, US
• Dhanapalan Nagarathnam · Bethany, US
• Dake Tian · Plainsboro, US
• Charles Gluchowski · Mission Viejo, US

Key dates

• Filing date: Dec 17, 1998
• Grant date: Apr 17, 2001
• Expiry date: Dec 17, 2018

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D413/14
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

This invention is directed to morpholinone and morpholine derivatives which are selective antagonists for human .alpha..sub.1a receptors. This invention is also related to uses of these compounds for lowering intraocular pressure, inhibiting cholesterol synthesis, relaxing lower urinary tract tissue, the treatment of benign prostatic hyperplasia, impotency, cardiac arrhythmia, sympathetic mediated pain, migraine, and for the treatment of any disease where the antagonism of the .alpha..sub.1a receptor may be useful. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.