Amino acid derivatives

Abstract

Compounds of formula (I) or formula (II) have dopaminergic activity: wherein: R1 is a carboxyl, carboxyl ester, or carboxamide group; R2 is a group - C(=O)-NR3R4, or -S(=O)2-NR3R4; R3 and R4 are independently selected from hydrogen, optionally substituted C1-C6 alkyl, (C1-C5 fluoroalkyl)-CH2-, -Q, and -CH2Q, wherein Q is an optionally substituted monocyclic carbocyclic or heterocyclic ring of (3) to (6) ring atoms; or R3 and R4 together with the nitrogen to which they are attached form an optionally substituted monocyclic cycloalkyl or non-aromatic heterocyclic ring of (3) to (8) ring atoms; R5 is hydrogen, or a natural or non-natural alpha amino acid residue linked via a peptide bond; R6 is hydrogen or a group R7C(=O)-; and R7 is C1- C6 alkyl, C1-C6 fluoroalkyl or cyclopropyl.

Description

technical field The present invention relates to substituted phenylalanine derivatives capable of alleviating the symptoms of dopamine deficiency. Background technique Dopamine is a substance naturally produced by neurons in the basal ganglia of the brain, which enables smooth and coordinated control of voluntary movements. Loss or damage to dopamine-producing neurons in the brain heralds Parkinson's disease and the related Parkinson-plus syndrome. These diseases respond to dopamine replacement therapy. Other disorders, such as restless leg syndrome (RLS), also respond to dopamine replacement therapy. Parkinson's disease is a progressive neurodegenerative disorder that affects neuronal cells in the substantia nigra of the midbrain. It is an age-related disorder of the central nervous system that primarily affects patients over the age of 60. About 1 in every 500 people is infected with the disease, and about 1 in every 100 people over the age of 60 has the disease. As ...

AI Technical Summary

Problems solved by technology

L-dopa is highly effective in reversing motor symptoms of disease, but less effective with long-term treatment and disease progression

Images