N-Nicotinoyl-3,4-dinicotinoyloxy-L-phenylalanine and derivatives pharmaceutical compositions and methods containing same

摘要

There is provided, novel, transient pro-drug forms of L-DOPA (3,4-dihydroxy-L-phenylalanine), having the formula: (I) wherein R represents a hydrogen atom, an acyl group, a group, a -CO-pyridyl group, and a -CO-R3 group, wherein R3 represents the residue of any N,N-C1-C2 dialkylamino acid or a C4-C6 cycloalkylamino acid wherein R1 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 R2 represents a member selected from the group consisting of a group, a -CO-pyridyl group, and a -CO-R3 group, wherein R3 represents the residue of any N,N-(C1-C2)-dialkylamino acid or a C4-C6-cycloalkylamino acid (II) wherein R represents an acyl group; wherein R2 represents a hydrogen atom; and wherein R1 represents a -NHCH(R4)COOR5 group, wherein R4 represents the residue of any naturally occurring amino acid, and wherein R5 represents a member selected from the group consisting of a hydrogen atom, a C1-C5 alkyl group (e.g., methyl, ethyl, propyl, butyl, pentyl), and a C1-C5 alkylaryl group (e.g., -CH2-C6H5, -CH2-CH2-C6H5, 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.).