Muscarinic Agonists as Cognitive Enhancers

Abstract

A method of treating a mental condition in a subject in need thereof, comprising: administering to a subject in need thereof an effective amount of compound CDD-102A.

1 . A composition comprising an effective amount of a CDD-0102 [5-(3-ethyl-1,2,4-oxadiazol-5-yl)-1,4,5,6-tetrahydropyrimidine] compound, or a pharmaceutically acceptable salt or hydrate thereof sufficient to enhance behavioral flexibility by enhancing one or more of executive functioning, reasoning, problem solving, and learning functioning in a subject in need thereof. 
     
     
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         4 . The composition according to  claim 1 , wherein the behavioral flexibility function includes one or more of: perseveration errors, regressive errors and never-reinforced errors. 
     
     
         5 . The composition according to  claim 1 , wherein the administration of the compound gives rise to efficacious treatment without substantially interfering with M 2 , M 3 , M 4  and M 5  receptor activity in the subject. 
     
     
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         9 . The pharmaceutical composition according to  claim 1 , formulated to be administered to a subject in need thereof in a dosage ranging from about 0.001 mg/kg to about 10 mg/kg body weight. 
     
     
         10 . The pharmaceutical composition according to  claim 1 , formulated to be administered to a subject in need thereof in a dosage ranging from about 0.01 to about 10 mg/kg of body weight. 
     
     
         11 . The pharmaceutical composition according to  claim 1 , formulated to be administered to a subject in need thereof in a dosage ranging from about 0.01 mg/kg to about 0.1 mg/kg of body weight. 
     
     
         12 . The pharmaceutical composition according to  claim 1 , formulated to be administered to a subject in need thereof in a daily dosage. 
     
     
         13 . The pharmaceutical composition according to  claim 1 , formulated to be administered to a subject in need thereof in a regimen of 1 to 4 times per day. 
     
     
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         31 . A method of improving and/or modulating a loss of behavioral flexibility in a subject in need thereof, comprising:
 administering to a subject in need thereof an effective amount of CDD-102A [5-(3-ethyl-1,2,4-oxadiazol-5-yl)-1,4,5,6-tetrahydropyrimidine] compound or a pharmaceutically acceptable salt or hydrate thereof,   sufficient to enhance behavioral flexibility by enhancing one or more of: executive function, reasoning and problem solving, a memory function, a learning function.   
     
     
         32 . The method according to  claim 31 , wherein the behavioral flexibility function includes one or more of: perseveration errors, regressive errors and never-reinforced errors. 
     
     
         33 . The method according to  claim 31 , wherein the administration of the compound gives rise to efficacious treatment without substantially interfering with M 2 , M 3 , M 4  and/or M 5  subtype receptor activity in the subject. 
     
     
         34 . The method according to  claim 31 , wherein the mental condition is at least partially due to decreased M 1  receptor activity. 
     
     
         35 . The method according to  claim 31 , wherein the subject has a mental condition selected from the group consisting of one or more of: neurodegenerative diseases, Alzheimer's disease, Parkinson's disease, schizophrenia, age-related cognitive decline, and attention-deficit disorder. 
     
     
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         45 . The method according to  claim 31 , wherein the subject is a human. 
     
     
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         50 . Use of CDD-102A [5-(3-ethyl-1,2,4-oxadiazol-5-yl)-1,4,5,6-tetrahydropyrimidine] compound or a pharmaceutically acceptable salt or hydrate thereof, or a composition comprising CDD-102A [5-(3-ethyl-1,2,4-oxadiazol-5-yl)-1,4,5,6-tetrahydropyrimidine] compound or a pharmaceutically acceptable salt or hydrate thereof in the manufacture of a medicament for use in improving and/or ameliorating a loss of behavioral flexibility in a subject in need thereof. 
     
     
         51 . (canceled) 
     
     
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         54 . Use of CDD-102A compound or a pharmaceutically acceptable salt or hydrate thereof, or a composition comprising CDD-102A compound or a pharmaceutically acceptable salt or hydrate thereof, in the manufacture of a medicament for treating a mental condition affecting behavioral flexibility in a subject. 
     
     
         55 . (canceled) 
     
     
         56 . Use according to  claim 54 ,
 wherein the mental condition is selected from the group consisting of one or more of: neurodegenerative diseases, Alzheimer's disease, Parkinson's disease, schizophrenia, age-related cognitive decline, and attention-deficit disorder.   
     
     
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         73 . Use according to  claim 54 ,
 wherein the use includes preventing the development of the condition, and/or whereby the condition has already developed and the subject is protected against worsening of the condition.   
     
     
         74 . Use according to  claim 54 ,
 wherein the disease or condition results from defective or malfunctioning M 1  receptors in the subject.   
     
     
         75 . Use according to  claim 54 ,
 wherein the treatment disease or condition results from suppressed M 1  receptor transmission in the subject.   
     
     
         76 . Use according to  claim 54 ,
 for use in selectively activating M 1  muscarinic receptor, without substantially interfering with M 2 , M 3 , M 4  and M 5  receptor activity.   
     
     
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         81 . Use according to  claim 54 , wherein the subject is a human.