Title: Novel, transient pro-drug forms of L-DOPA to treat Parkinson's disease

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Abstract: There is provided, novel, transient pro-drug forms of L-DOPA (3,4-dihydroxy-L-phenylalanine), having the formula: ##STR1## wherein R represents a hydrogen atom, an acyl group, ##STR2## group, a -CO-pyridyl group, and a -CO-R.sub.3 group, wherein R.sub.3 represents the residue of any N,N-C.sub.1 -C.sub.2 dialkylamino acid or a C.sub.4 -C.sub.6 cycloalkylamino acid (e.g., ##STR3## wherein R.sub.1 represents a member selected from the group consisting of a hydroxyl group and a --OM group, wherein M is an alkali metal (Na, K, etc.) or an ammonium ion; and wherein R.sub.2 represents a member selected from the group consisting of a ##STR4## group, a -CO-pyridyl group, and a --CO-R.sub.3 group, wherein R.sub.3 represents the residue of any N,N-(C.sub.1 -C.sub.2)--dialkylamino acid or a C.sub.4 -C.sub.6 -cycloalkylamino acid (e.g., ##STR5## wherein R represents an acyl group; wherein R.sub.2 represents a hydrogen atom; and wherein R.sub.1 represents a --NHCH(R.sub.4)COOR.sub.5 group, wherein R.sub.4 represents the residue of any naturally occurring amino acid, and wherein R.sub.5 represents a member selected from the group consisting of a hydrogen atom, a C.sub.1 -C.sub.5 alkyl group (e.g., methyl, ethyl, propyl, butyl, pentyl), and a C.sub.1 -C.sub.5 alkylaryl group (e.g., --CH.sub.2 -C.sub.6 H.sub.5, --CH.sub.2 -CH.sub.2 --C.sub.6 H.sub.5, etc.), and the HX salts thereof, wherein X is a conventional pharmaceutically acceptable acid addition salt anion (e.g., chloride, bromide, perchlorate, methanesulfonate, succinate, etc.); ##STR6## wherein R represents an acyl group; wherein R.sub.1 represents a member selected from the group consisting of a hydroxyl group, a --OCH.sub.3 group, a --OC.sub.2 H.sub.5 group, a --OC.sub.3 H.sub.7 group, a --OC.sub.4 H.sub.9 group, and a -OCH.sub.2 -C.sub.6 H.sub.5 group; and wherein R.sub.2 represents an NH.sub.2 CH(R.sub.6)CO-- group, wherein R.sub.6 represents the residue of any naturally occurring amino acid, and the HX salts thereof, wherein X is defined as above; ##STR7## wherein R represents a member selected from the group consisting of an acyl group; wherein R.sub.1 represents a member selected from the group consisting of a hydroxyl group, a --OCH.sub.3 group, a --OC.sub.2 H.sub.5 group, a --OC.sub.3 H.sub.7 group, a --OC.sub.4 H.sub.9 group, and a --OCH.sub.2 -C.sub.6 H.sub.5 group; and wherein R.sub.2 represents an NH.sub.2 -CH(R.sub.7)--CO-- group, wherein R.sub.7 represents the residue of a 3,4-L-diacylphenylalanine group having the formula: ##STR8## wherein R is defined as above, and the HX salts thereof, wherein X is as defined above; and ##STR9## wherein n represents an integer of from 2 to 50 with respect to formula (V-A), and wherein n represents an integer of from 1 to 50 with respect to formula (V-B). These compounds are all useful in the treatment of Parkinson's Disease.


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