Novel compound and medical use thereof

Abstract

Provided is a levodopa prodrug that overcomes the problems attributed to the blood kinetics of levodopa such as large number of doses and the incidence of side effects due to frequent dosing. (2S)-2-Amino-3-(3,4-bis((2-(benzoyloxy)-2-methylpropanoyl)oxy)phenyl)propanoic acid, a salt thereof, or a solvate thereof is a levodopa prodrug, and provides a flat blood concentration-time profile of levodopa through oral administration, and therefore is useful as a preventive and/or therapeutic agent for Parkinson's disease and/or Parkinson's syndrome that overcomes the problems associated with pharmaceutical preparations of levodopa.

1 . A method for preventing hyperkinetic child syndrome, toxemia of pregnancy, malignant hypertension, or epilepsy, comprising administering to a subject in need thereof an effective amount of an amorphous solvate of an ornithine salt of (2S)-2-Amino-3-(3,4-bis((2-(benzoyloxy)-2-methylpropanoyl)oxy)phenyl)propanoic acid. 
     
     
         2 . A method for preventing orthostatic hypotension, subarachnoid hemorrhage, cerebral infarction, bronchospasm accompanying bronchial asthma or whooping cough, hypoglycemic symptoms due to insulin injection, or iris adhesion in iridocyclitis, comprising administering to a subject in need thereof an effective amount of an amorphous solvate of an ornithine salt of (2S)-2-amino-3-(3,4-bis((2-(benzoyloxy)-2-methylpropanoyl)oxy)phenyl)propanoic acid. 
     
     
         3 . A method according to  claim 1 , wherein hyperkinetic child syndrome is prevented. 
     
     
         4 . A method according to  claim 1 , wherein toxemia of pregnancy is prevented. 
     
     
         5 . A method according to  claim 1 , wherein malignant hypertension is prevented. 
     
     
         6 . A method according to  claim 1 , wherein epilepsy is prevented. 
     
     
         7 . A method according to  claim 2 , wherein subarachnoid hemorrhage is prevented. 
     
     
         8 . A method according to  claim 2 , wherein cerebral infarction is prevented. 
     
     
         9 . A method according to  claim 2 , wherein bronchospasm accompanying bronchial asthma is prevented. 
     
     
         10 . A method according to  claim 2 , wherein bronchospasm accompanying whooping cough is prevented. 
     
     
         11 . A method according to  claim 2 , wherein hypoglycemic symptoms due to insulin injection is prevented. 
     
     
         12 . A method according to  claim 2 , wherein iris adhesion in iridocyclitis is prevented. 
     
     
         13 . A method according to  claim 2 , wherein orthostatic hypotension is prevented. 
     
     
         14 . A medicament kit containing an effective amount of an amorphous solvate of an ornithine salt of (2S)-2-Amino-3-(3,4-bis((2-(benzoyloxy)-2-methylpropanoyl)oxy)phenyl)propanoic acid and instructions to administer it to a subject in need of prevention of hyperkinetic child syndrome, toxemia of pregnancy, malignant hypertension, epilepsy, orthostatic hypotension, subarachnoid hemorrhage, cerebral infarction, bronchospasm accompanying bronchial asthma or whooping cough, hypoglycemic symptoms due to insulin injection, or iris adhesion in iridocyclitis. 
     
     
         15 - 39 . (canceled)