Derivatives of .beta.-adrenergic antagonists

US4687873A · kind A · utility

Assignee

• The Regents of the University of California · US

Inventors

• Murray Goodman · Village of La Jolla, US
• Debra Marr-Leisy · Village of La Jolla, US
• Roberto P. Rosenkranz · Menlo Park, US
• Kenneth L. Melmon · Woodside, US
• Michael S. Verlander · Del Mar, US

Key dates

• Filing date: May 10, 1985
• Grant date: Aug 18, 1987
• Expiry date: May 10, 2005

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D405/12
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

Molecular structures of .beta.-adrenergic antagonists are modified to produce biologically active compounds. The .beta.-antagonists are modified to form molecules of the general structure: ##STR1## wherein R is most generally R"--OCH.sub.2 --, and in some instances is R"--, and R"=an aryl or substituted aryl moiety; R'=--H, --CH.sub.3, or a short chain alkyl moiety; and Y=--OH, or more usually, --OAX or --NHAX, where A=an alkyl, aryl, or aralkyl moiety, and X=a terminal grouping, such as --CH.sub.3, --CF.sub.3 or --(CH.sub.2).sub.n COOH; or AX may be a carrier moiety consisting of a defined peptide or protein.