Novel, transient pro-drug forms of l-dopa useful in the treatment of parkinson's disease
Patent 3939253 Issued on February 17, 1976. Estimated Expiration Date: 
February 17, 1993. Estimated Expiration Date is calculated based on simple USPTO term provisions. It does not account for terminal disclaimers, term adjustments, failure to pay maintenance fees, or other factors which might affect the term of a patent.
February 17, 1993. Estimated Expiration Date is calculated based on simple USPTO term provisions. It does not account for terminal disclaimers, term adjustments, failure to pay maintenance fees, or other factors which might affect the term of a patent.InventorsAssigneeApplicationNo. 566748 filed on 04/10/1975US Classes:514/547, Compound contains two or more C(=O)O groups514/512, X-C(=X)-X containing (e.g., carbonic acid ester, thiocarbonic acid ester, etc.) (X is chalcogen)514/649, Amino nitrogen attached to aryl ring or aryl ring system by an acyclic carbon or acyclic chain514/650, The aryl ring or aryl ring system is bonded directly to another ring or ring system514/653Hydroxy, bonded directly to carbon, attached directly or indirectly to the acyclic carbon or chain by acyclic nonionic bonding (e.g., beta hydroxy phenethylamines, etc.)ExaminersPrimary: Friedman, Stanley J.Attorney, Agent or FirmAbstractThere 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 --COCH3 group, a --COC2 H5 group, a --COOC2 H5 group, and a --CO--C(CH3)3 group; wherein R1 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 --OCH2 --C6 H5 group, a --OCH3 group, a --OC2 H5 group, and --NH--CH(R3)COOH group, wherein R3 represents the residue of any naturally occurring amino acid; and wherein R2 represents a member selected from the group consisting of a hydrogen atom, a formyl group, a --CO--C6 H5 group, a --CO--pyridyl group, a --CO(R5)--CH=CH(R4) group, and a NH2 --CH(R6)--CO-- group, wherein R4 represents a methyl group and wherein R5 represents a member selected from the group consisting of a methyl group, a --OC2 H5 group, and a C6 H5 -- group, and wherein R6 represents the residue of any naturally occurring amino acid,With the proviso that simultaneously,R cannot represent a hydrogen atom when R1 represents a --OCH3 group or a --OH group and when R2 represents a hydrogen atom respectively;R cannot represent a hydrogen atom when R1 represents either a hydroxyl group or a --OCH3 group and R2 represents a --COCH3 group, respectively;R cannot represent a hydrogen atom when R1 represents a hydroxyl group and R2 represents a formyl group respectively,R cannot represent a hydrogen atom when R1 represents a hydroxyl group and R2 represents a benzoyl group, respectively; and,R cannot represent a hydrogen atom when R1 represents a hydroxyl group and R6 represents the residue of L-leucine, respectively.These compounds are useful in the treatment of Parkinson's Disease. | |
