Method for the treatment, alleviation of symptoms of, relieving, improving and preventing a cognitive disease, disorder or condition

Abstract

The present invention provides uses of a salt adduct comprising at least one positively charged moiety being a pyridoxine or a derivative thereof and at least one carboxylated 5- to 7-membered lactam ring, optionally additionally substituted, for the preparation of a medicament for the treatment, alleviation of symptoms of relieving, improving and preventing a cognitive disease, disorder or condition in a subject. Additionally, the invention provides use of said salt adducts for the preparation of medicaments for the improvement of cognitive functions in a healthy subject.

1 - 16 . (canceled) 
     
     
         17 . A method of treatment, alleviation of symptoms of, relieving, improving and preventing a cognitive disease, disorder or condition in a subject, comprising administering to said subject a therapeutically effective amount of a salt adduct comprising at least one positively charged moiety being a pyridoxine or a derivative thereof and at least one carboxylated 5- to 7-membered lactam ring, optionally additionally substituted. 
     
     
         18 . A method of improving cognitive functions in a healthy subject comprising administering to said subject an effective amount of a salt adduct comprising at least one positively charged moiety being a pyridoxine or a derivative thereof and at least one carboxylated 5- to 7-membered lactam ring, optionally additionally substituted. 
     
     
         19 . A method according to  claim 17  or  claim 18 , wherein said positively charged moiety is a compound of formula (I): 
       
         
           
           
               
               
           
         
         wherein 
         R 1  is straight or branched C 1 -C 6  alkyl; 
         R 2  is selected from —OH, straight or branched C 1 -C 6  alkoxy, and straight or branched C 1 -C 6  alkoxycarbonyl; 
         R 3  and R 4  are each independently selected from formyl, straight or branched C 1 -C 6  alkyl optionally substituted by at least one halogen, amine, hydroxy, C 1 -C 6  alkoxy, thiol and C 1 -C 6  alkoxycarbonyl. 
       
     
     
         20 . A method according to  claim 17  or  claim 18 , wherein said carboxylated lactam ring is selected from the group consisting of: 
       
         
           
           
               
               
           
         
         wherein 
         R 6  is selected from H, straight or branched C 1 -C 6  alkyl optionally substituted by at least one halogen, straight or branched C 2 -C 6  alkenyl, straight or branched C 2 -C 6  alkynyl, cycloalkyl, aryl and heteroaryl optionally substituted by a C 1 -C 6  alkyl; 
         R 7 , R 8 , R 9 , R 10  R 11 , R 12 , R 13  and R 14  are each independently selected from H, straight or branched C 1 -C 6  alkyl, C 2 -C 6  alkenyl, C 2 -C 6  alkynyl, cycloalkyl, aryl and heteroaryl optionally substituted by at least one group selected from C 1 -C 6  alkyl, halogen, amino, cyano, nitro, thiol, C 1 -C 6  alkoxy, aminocarbonyl, C 1 -C 6  alkoxycarbonyl, C 1 -C 6  carboxyalkyl, C 1 -C 6  alkoxycarbonylalkyl and amidino. 
       
     
     
         21 . A method according to  claim 17  or  claim 18 , wherein said salt adduct is selected from the following: 
       
         
           
           
               
               
           
         
         
           
           
               
               
           
         
       
     
     
         22 . A method according to  claim 17 , wherein said cognitive disease, disorder or condition is selected from Attention Deficit/Hyperactivity Disorder (ADHD/ADD), impaired memory (Amnesia), impaired wakefulness, mental fatigue conditions, Shift Work Sleep Disorder, Narcolepsy, Obstructive Sleep Apnea/Hypopnea Syndrome, poor concentration, and poor focus or any combination thereof. 
     
     
         23 . A method according to  claim 17 , wherein said cognitive disease, disorder or condition is selected from learning disabilities, impairment of memory, cognitive dysfunction, alteration of cognitive function, including Alzheimer's disease, or any type of encephalopathy, including uremic and hepatic encephalopathy. 
     
     
         24 . A method according to  claim 17 , wherein said cognitive disease, disorder or condition is a neurobehavioral disease, disorder or condition. 
     
     
         25 . A method according to  claim 17 , wherein said cognitive disease, disorder or condition is a neurobehavioral disease, disorder or condition selected from Attention Deficit Hyperactivity Disorder (ADHD), Attention Deficit Disorder (ADD), impaired memory, poor concentration, and poor focus. 
     
     
         26 . A method according to  claim 17 , wherein said cognitive disease, disorder or condition is selected from Attention Deficit Disorder (ADD) or Hyperactivity Disorder (ADHD/ADD), impaired memory (Amnesia), impaired wakefulness, mental fatigue conditions, Shift Work Sleep Disorder, Narcolepsy, Obstructive Sleep Apnea/Hypopnea Syndrome, poor concentration, and poor focus or any combination thereof. 
     
     
         27 . A method according to  claim 18 , wherein said cognitive function selected from temporary or long term learning disabilities, temporary or long term impairment of memory, temporary or long term cognitive dysfunction, temporary or long term alteration of cognitive function, temporary or long term concentration impairment, temporary or long term focus impairment, temporary or long term impaired wakefulness, temporary or long term mental fatigue conditions, temporary or long term Shift Work Sleep Disorder, or any combination thereof. 
     
     
         28 . A method according to any one of  claims 17  and  18 , wherein said subject is a child, an adolescent, an adult, or an elderly person. 
     
     
         29 . A method according to any one of  claims 17  and  18 , wherein said salt adduct is formulated in a sustained-, delayed or controlled-release dosage form. 
     
     
         30 . A method according to any one of  claims 17  and  18 , wherein said salt adduct is formulated in a sustained-, delayed or controlled-release dosage form combined with a salt adduct formulated in an immediate or burst effect dosage form. 
     
     
         31 . A method according to any one of  claims 17  and  18 , wherein said salt adduct is formulated to deliver up to 0.1-1000 mg/kg body weight/day of said salt adduct, preferably 1-400 mg/kg body weight of said salt adduct, in a single dose administration or portion thereof. 
     
     
         32 . A method according to any one of  claims 17  and  18 , wherein said salt adduct is formulated together with at least one additional pharmaceutically active agent.