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

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1. A method for treating Parkinson's Disease in warmblooded animals which comprises administering thereto, an antiParkinsonism effective amount of a compound having the formula: ##SPC9##

wherein R represents a member selected from the group consisting of hydrogen, --COCH.sub.3, --COC.sub.2 H.sub.5, --COOC.sub.2 H.sub.5, and --CO--C(CH.sub.3).sub.3 ; wherein R.sub.1 represents a member selected from the group consisting of hydroxyl and --OM, wherein M represents a member selected from the group consisting of an alkali metal and an ammonium ion; and wherein R.sub.2 represents --(R.sub.5)CO--CH=C(R.sub.4)--, wherein R.sub.4 represents methyl or ethoxy, and wherein R.sub.5 represents a member selected from the group consisting of methyl, --C.sub.6 H.sub.5, and --OC.sub.2 H.sub.5.

2. The method of claim 1, wherein said compound is administered in combination with a pharmaceutically acceptable inert carrier material.

3. The method of claim 1, wherein said compound is 3,4-diacetyloxy-N[1-methyl-2-acetylvinyl]-L-phenylalanine and its alkali metal salt.

4. The method of claim 1, wherein said compound is 3,4-dihydroxy-N[1-methyl-2-acetylvinyl]-L-phenylalanine and its M salt, wherein M represents an alkali metal.

5. The method of claim 1, wherein said compound is 3,4-dipivalyloxy-N[1-methyl-2-acetylvinyl]-L-phenylalanine and its M salt, wherein M represents an alkali metal.

6. The method of claim 1, wherein said compound is 3,4-dihydroxy-N[1-ethoxy-2-acetylvinyl]-L-phenylalanine and its M salt, wherein M represents an alkali metal.

7. The method of claim 1, wherein said compound is 3,4-diacetyloxy-N[1-ethoxy-2-acetylvinyl]-L-phenylalanine and its M salt, wherein M represents an alkali metal.

8. The method of claim 1, wherein said compound is 3,4-dipivalyloxy-N[1-ethoxy-2-acetylvinyl]-L-phenylalanine and its M salt, wherein M represents an alkali metal.

9. A pharmaceutical composition for use in the treatment of Parkinson's Disease, comprising a pharmaceutically acceptable inert carrier material in combination with an anti-Parkinsonism effective amount of a compound having the formula: ##SPC10##

wherein R represents a member selected from the group consisting of hydrogen, --COCH.sub.3, --COC.sub.2 H.sub.5, --COOC.sub.2 H.sub.5, and --CO--C(CH.sub.3).sub.3 ; wherein R.sub.1 represents a member selected from the group consisting of hydroxyl and --OM, wherein M represents a member selected from the group consisting of an alkali metal and an ammonium ion; and wherein R.sub.2 represents -- (R.sub.5)CO--CH=C(R.sub.4)--, wherein R.sub.4 represents methyl or ethoxy, and wherein R.sub.5 represents a member selected from the group consisting of methyl, --C.sub.6 H.sub.5, and --OC.sub.2 H.sub.5.

10. The composition of claim 9, wherein said compound is 3,4-diacetyloxy-N[1-methyl-2-acetylvinyl]-L-phenylalanine and its alkali metal salt.

11. The composition of claim 9, wherein said compound is 3,4-dihydroxy-N[1-methyl-2-acetylvinyl]-L-phenylalanine and its M salt, wherein M represents an alkali metal.

12. The composition of claim 9, wherein said compound is 3,4-dipivalyloxy-N[1-methyl-2-acetylvinyl]-L-phenylalanine and its M salt, wherein M represents an alkali metal.

13. The composition of claim 9, wherein said compound is 3,4-dihydroxy-N[1-ethoxy-2-acetylvinyl]-L-phenylalanine and its M salt, wherein M represents an alkali metal.

14. The composition of claim 9, wherein said compound is 3,4-diacetyloxy-N[1-ethoxy-2-acetylvinyl]-L-phenylalanine and its M salt, wherein M represents an alkali metal.

15. The composition of claim 9, wherein said compound is 3,4-dipivalyloxy-N[1-ethoxy-2-acetylvinyl]-L-phenylalanine and its M salt, wherein M represents an alkali metal.
Other info:

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.