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

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 amino acid, With the proviso that simultaneously, R cannot represent a hydrogen atom when R.sub.1 represents a --OCH.sub.3 group or a --OH group and when R.sub.2 represents a hydrogen atom respectively; R cannot represent a hydrogen atom when R.sub.1 represents either a hydroxyl group or a --OCH.sub.3 group and R.sub.2 represents a --COCH.sub.3 group, respectively; R cannot represent a hydrogen atom when R.sub.1 represents a hydroxyl group and R.sub.2 represents a formyl group respectively, R cannot represent a hydrogen atom when R.sub.1 represents a hydroxyl group and R.sub.2 represents a benzoyl group, respectively; and, R cannot represent a hydrogen atom when R.sub.1 represents a hydroxyl group and R.sub.6 represents the residue of L-leucine, respectively. These compounds are useful in the treatment of Parkinson's Disease.


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Inventors: Bodor, Nicolae S. (Lawrence, KS, US)
Sloan, Kenneth B. (Lawrence, KS, US)
Hussain, Anwar A. (Lawrence, KS, US)

Application Number: 566748
Filing Date: 1975-04-10
Publication_date: 1976-02-17
Assignee: Interx Research Corporation (Lawrence, KS)
Primary Class(es): 514/547 514/512, 514/649, 514/650, 514/653
Other Classes:
US Patent Ref:
Other Refs:
Primary Examiner: Friedman, Stanley J.
Assistant Examiner:
Attorney: Blitzer; Charles N.