Novel, transient pro-drug forms of l-dopa useful in the treatment of parkinson's disease

US3939253A · kind A · utility

Assignee

• INTERx Research Corporation · US

Inventors

• Nicolae S. Bodor · Lawrence, US
• Kenneth B. Sloan · Gainesville, US
• Anwar A. Hussain · Lexington, US

Key dates

• Filing date: Apr 10, 1975
• Grant date: Feb 17, 1976
• Expiry date: Apr 10, 1995

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61K38/00
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

There is provided, novel, transient pro-drug forms of L-DOPA (3,4-dihydroxy-L-phenylalanine), having the formula: ##SPC1## Wherein R represents a member selected from the group consisting of a hydrogen atom, a --COCH.sub.3 group, a --COC.sub.2 H.sub.5 group, a --COOC.sub.2 H.sub.5 group, and a --CO--C(CH.sub.3).sub.3 group; wherein R.sub.1 represents a member selected from the group consisting of a hydroxyl group, a --OM group (wherein M represents an alkali metal or an ammonium ion), a --OCH.sub.2 --C.sub.6 H.sub.5 group, a --OCH.sub.3 group, a --OC.sub.2 H.sub.5 group, and --NH--CH(R.sub.3)COOH group, wherein R.sub.3 represents the residue of any naturally occurring amino acid; and wherein R.sub.2 represents a member selected from the group consisting of a hydrogen atom, a formyl group, a --CO--C.sub.6 H.sub.5 group, a --CO--pyridyl group, a --CO(R.sub.5)--CH=CH(R.sub.4) group, and a NH.sub.2 --CH(R.sub.6)--CO-- group, wherein R.sub.4 represents a methyl group and wherein R.sub.5 represents a member selected from the group consisting of a methyl group, a --OC.sub.2 H.sub.5 group, and a C.sub.6 H.sub.5 -- group, and wherein R.sub.6 represents the residue of any naturally occurring…