Fluorinated diaminobutane derivatives

US4435425A · kind A · utility

Assignee

• Merrell Toraude et Compagnie · FR

Inventors

• Albert Sjoerdsma · Cincinnati, US
• Philippe Bey · Cincinnati, US
• Michel Jung · Illkirch-Graffenstaden, FR
• Fritz Gerhart · Kehl, DE
• Daniel Schirlin · Schiltigheim, FR

Key dates

• Filing date: Apr 9, 1982
• Grant date: Mar 6, 1984
• Expiry date: Apr 9, 2002

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07C57/76
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

Fluorinated diaminobutane compounds in vivo are inhibitors of gamma-aminobutyric acid transaminase and have the following formula: ##STR1## wherein: R.sub.1 represents hydrogen, C.sub.1 -C.sub.6 alkyl, or phenyl-(C.sub.1 -C.sub.4 alkyl); PA1 R.sub.2 represents hydrogen, C.sub.1 -C.sub.6 alkyl, phenyl-(C.sub.1 -C.sub.4 alkyl), or R.sub.4, where R.sub.4 is as defined below; PA1 R.sub.3 represents hydrogen, or, except when R.sub.2 represents R.sub.4, R.sub.4, where R.sub.4 is as defined below; PA1 each R.sub.4, independently, represents C.sub.2 -C.sub.5 alkylcarbonyl, phenylcarbonyl, phenyl-(C.sub.1 -C.sub.4 alkyl) carbonyl, or an aminocarboxylic acid residue derived by removal of an hydroxy group from the carboxy moiety of an L-aminocarboxylic acid; and PA1 p represents 1 or 2, PA1 and pharmaceutically acceptable acid addition salts thereof.