Di-and tri-peptide mimetic compounds for Parkinson's disease
AssigneeDepartment of Health, the Executive Yuan, Republic of China
InventorsHui-Po Wang, Jia-Shuai Lee, Ming-Cheng Tsai, Hsiao-Hwa Lu, Oliver Yoa-Pu Hu, Wen-Lin Luo
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Abstract
A series of di- and tri-peptide mimetic dopamine prodrugs are synthesized in which D-phenylglycine or D-p-hydroxyphenylglycine is attached as tools for delivery of L-dopa through the intestine via the intestinal dipeptide-mediated carrier transport system. These compounds are found useful as an active ingredient for the treatment of Parkinson's disease.
Claims16
A di- or tri-peptide derivative of 2-amino-3-(3,4-dihydroxyphenyl)propanoic acid having the following formula:
- ##STR16## wherein n is 0 or 1;
- R is hydrogen or hydroxyl;
- R.sub.1 is hydrogen;
- and
- R.sub.2 is hydrogen, alkyl of from one to four carbon atoms, alkyl of from one to four carbon atoms substituted with one --OH, --SH, --SCH.sub.3, --NH.sub.2, --NHC(.dbd.NH)NH.sub.2, --COOH, phenyl, hydroxyphenyl, indolyl or imidazolyl group, alkyl from one to four carbon atoms substituted with one carboalkoxyl group of from one to six carbon atoms;
- or
- R.sub.1 and R.sub.2 together is trimethylene.
A pharmaceutical composition for the treatment of Parkinson's disease, which comprises a therapeutically effective amount of a di- or tri-peptide derivative of 2-amino-3-(3,4-dihydroxyphenyl)propanoic acid having the following formula or a pharmaceutically acceptable salt thereof, as an active ingredient, in combination with a pharmaceutically acceptable carrier or diluent for the active ingredient:
- ##STR17## wherein n is 0 or 1;
- R is hydrogen or hydroxyl;
- R.sub.1 is hydrogen;
- and
- R.sub.2 is hydrogen, alkyl of from one to four carbon atoms, alkyl of from one to four carbon atoms substituted with one --OH, --SH, --SCH.sub.3, --NH.sub.2, --NHC(.dbd.NH)NH.sub.2, --COOH, phenyl, hydroxyphenyl, indolyl or imidazolyl group, alkyl from one to four carbon atoms substituted with one carboalkoxyl group of from one to six carbon atoms;
- or
- R.sub.1 and R.sub.2 together is trimethylene.
A di-peptide derivative of 2-amino-3-(3,4-dihydroxyphenyl)propanoic acid having the following formula:
- ##STR18## wherein R.sub.3 is hydrogen;
- and R.sub.4 is phenyl or hydroxyphenyl;
- or R.sub.3 and R.sub.4 together is trimethylene.
A pharmaceutical composition for the treatment of Parkinson's disease, which comprises a therapeutically effective amount of a di-peptide derivative of 2-amino-3-(3,4-dihydroxyphenyl)propanoic acid having the following formula or a pharmaceutically acceptable salt thereof, as an active ingredient, in combination with a pharmaceutically acceptable carrier or diluent for the active ingredient:
- ##STR19## wherein R.sub.3 is hydrogen;
- and R.sub.4 is phenyl or hydroxyphenyl;
- or R.sub.3 and R.sub.4 together is trimethylene.
Dependencies are inferred from the claim text.