Substituted isoquinolines as ultra short acting neuromuscular blockers

US6177445A · kind A · utility

Assignees

• Glaxo Wellcome Inc. · US
• Cornell Research Foundation, Inc. · US

Inventors

• Eric C. Bigham · Chapel Hill, US
• Grady Evan Boswell · Cary, US
• John J. Savarese · Boxford, US
• Roy A. Swaringen, Jr. · Durham, US
• Sanjay Shashikant Patel · Cary, US
• Eric Eugene Boros · Durham, US
• Robert Mook · Chapel Hill, US
• Vincente Samano · Chapel Hill, US

Key dates

• Filing date: Dec 22, 1999
• Grant date: Jan 23, 2001
• Expiry date: Dec 22, 2019

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D217/20
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

Ultra short acting neuromuscular blocking agents of Formula (I) which are useful as skeletal muscle relaxants during emergency intubation procedures, routine surgery and post-operative settings are disclosed, wherein q and t are independently from 0 to 4; X.sup.1 and X.sup.2 are independently halogen; h.sup.a and h.sup.b are independenity from 0 to 2; Z.sup.1 and Z.sup.2 are indepentdently hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl or C.sub.2-6 alkynyl with the proviso that Z.sup.1 and Z.sup.2 are not both hydrogen; Y.sup.1, Y.sup.2, and Y.sup.3 and Y.sup.4 are independently hydrogen, halogen or C.sub.1-3 alkoxy; m and p are independently 1 to 6; n and r are independently 0 to 4; with the proviso the if h.sup.a and h.sup.b are both 0, then r is 0 and n is 0 to 2; R.sup.1 to R.sup.14 are independently hydrogen, halogen, C.sub.1-3 alkoxy, or R.sup.2 and R.sup.3 together with the carbon atoms to which they are bonded, R.sup.5 and R.sup.6 together with the carbon atoms to which they are bonded, R.sup.9 and R.sup.10 together with the carbon atoms to which they are bonded, R.sup.12 and R.sup.13 together with the carbon atoms to which they are bonded, may independently form a methylened…