초록

Levodopa dimethyl-substituted diester prodrugs pharmaceutical, compositions comprising levodopa dimethyl-substituted diester prodrugs, and methods of using such prodrugs and pharmaceutical compositions for treating diseases such as Parkinson's disease are provided.

대표청구항 ▼

1. A compound chosen from: (1R,2R)-2-acetyloxy-1-methylpropyl (2S)-2-amino-3-(3,4-dihydroxyphenyl)propanoate hydrochloride;(1R,2R)-1-methyl-2-(2-methylpropanoyloxy)propyl (2S)-2-amino-3-(3,4-dihydroxyphenyl)propanoate mesylate;(1R,2R)-2-ethoxycarbonyloxy-1-methylpropyl (2S)-2-amino-3-(3,4-dihydroxyp

1. A compound chosen from: (1R,2R)-2-acetyloxy-1-methylpropyl (2S)-2-amino-3-(3,4-dihydroxyphenyl)propanoate hydrochloride;(1R,2R)-1-methyl-2-(2-methylpropanoyloxy)propyl (2S)-2-amino-3-(3,4-dihydroxyphenyl)propanoate mesylate;(1R,2R)-2-ethoxycarbonyloxy-1-methylpropyl (2S)-2-amino-3-(3,4-dihydroxyphenyl)propanoate hydrochloride;(1R,2R)-2-isopropoxycarbonyloxy-1-methylpropyl (2S)-2-amino-3-(3,4-dihydroxyphenyl)propanoate hydrochloride;(1R,2R)-1-methyl-2-(2-methylpropoxycarbonyloxy)propyl (2S)-2-amino-3-(3,4-dihydroxyphenyl)propanoate, hydrochloride; and(1R,2R)-1-methyl-2-pentyloxycarbonyloxypropyl (2S)-2-amino-3-(3,4-dihydroxyphenyl)propanoate hydrochloride. 2. The compound of claim 1, wherein the compound is (1R,2R)-1-methyl-2-phenylcarbonyloxypropyl (2S)-2-amino-3-(3,4-dihydroxyphenyl)propanoate mesylate. 3. A pharmaceutical composition comprising at least one pharmaceutically acceptable vehicle and a therapeutically effective amount of at least one compound of claim 1 for treating Parkinson's a disease in a patient. 4. A pharmaceutical composition comprising at least one pharmaceutically acceptable vehicle and a therapeutically effective amount of at least one compound of claim 1 for treating a disease in a patient, wherein the disease is chosen from schizophrenia, cognitive impairment disorders, restless legs syndrome, periodic limb movement disorders, tardive dyskinesia, Huntington's disease, hypertension, stroke, excessive daytime sleepiness, dystonia, and memory and learning deficit or loss. 5. The pharmaceutical composition of claim 3, wherein the pharmaceutical composition is a sustained release oral dosage formulation. 6. The pharmaceutical composition of claim 3, further comprising a pharmaceutical agent chosen from a decarboxylase inhibitor, a catechol-O-methyltransferase inhibitor, and a combination thereof. 7. A method of treating Parkinson's disease in a patient comprising administering to a patient in need of such treatment a therapeutically effective amount of at least one compound of claim 1. 8. A method of treating Parkinson's a disease in a patient comprising administering to a patient in need of such treatment a pharmaceutical composition of claim 3. 9. The method of claim 8, wherein the pharmaceutical composition is a sustained release oral dosage formulation. 10. A method of treating a disease in a patient comprising administering to a patient in need of such treatment a compound of claim 1, wherein the disease is chosen from schizophrenia, cognitive impairment disorders, restless legs syndrome, periodic limb movement disorders, tardive dyskinesia, Huntington's disease, hypertension, stroke, excessive daytime sleepiness, dystonia, and memory and learning deficit or loss. 11. A method of treating a disease in a patient comprising administering to a patient in need of such treatment a pharmaceutical composition of claim 4, wherein the disease is chosen from schizophrenia, cognitive impairment disorders, restless legs syndrome, periodic limb movement disorders, tardive dyskinesia, Huntington's disease, hypertension, stroke, excessive daytime sleepiness, dystonia, and memory and learning deficit or loss. 12. The method of claim 10, wherein the pharmaceutical composition comprises a pharmaceutical agent chosen form a decarboxylase inhibitor, a catechol-O-methyltransferase inhibitor, and a combination thereof. 13. The method of claim 11, wherein the pharmaceutical composition comprises a pharmaceutical agent chosen form a decarboxylase inhibitor, a catechol-O-methyltransferase inhibitor, and a combination thereof. 14. The pharmaceutical composition of claim 4, wherein the pharmaceutical composition is a sustained release oral dosage formulation. 15. The pharmaceutical composition of claim 4, wherein the pharmaceutical composition comprises a pharmaceutical agent chosen form a decarboxylase inhibitor, a catechol-O-methyltransferase inhibitor, and a combination thereof.