Pharmaceutically active morpholinol

Abstract

Disclosed is the compound (+)-(2S,3S)-2-(3-chlorophenyl)-3,5,5-trimethyl-2-morpholinol and pharmaceutically acceptable salts and solvates thereof, pharmaceutical compositions comprising them, and processes for their preparation and use; also disclosed is a method of treating depression, attention deficit hyperactivity disorder (ADHD), obesity, migraine, pain, sexual dysfunction, Parkinson's disease, Alzheimer's disease, or addiction to cocaine or nicotine-containing (especially tobacco) products using such compound, salts, solvates or compositions.

1 . A method of treating pain in a mammal comprising the administration to said mammal of an effective amount of (+)-(2S,3S)-2-(3-chlorophenyl)-3,5,5-trimethyl-2-morpholinol or pharmaceutically acceptable salts and solvates thereof.  
     
     
         2 . A method as claimed in  claim 1  wherein the treatment is of neuropathic pain.  
     
     
         3 . A method as claimed in  claim 1  comprising the administration of the compound (+)-(2S,3S)-2-(3-chlorophenyl)-3,5,5-trimethyl-2-morpholinol hydrochloride.  
     
     
         4 . A method as claimed in  claim 2  wherein said compound has an optical rotation [α] 20   D  at c=0.64 in 95% EtOH of +31.9°.  
     
     
         5 . A method of treating sexual dysfunction in a mammal comprising the administration to said mammal of an effective amount of (+)-(2S,3S)-2-(3-chlorophenyl)-3,5,5-trimethyl-2-morpholinol or pharmaceutically acceptable salts and solvates thereof.  
     
     
         6 . A method as claimed in  claim 5  wherein the sexual dysfunction is psychosexual dysfunction.  
     
     
         7 . A method as claimed in  claim 6  wherein the psychosexual dysfunction is HSDD or FSD.  
     
     
         8 . A method as claimed in  claim 5  wherein the sexual dysfunction is a side-effect induced by treatment of the said mammal with an SSRI-class antidepressant.  
     
     
         9 . A method as claimed in  claim 5  comprising the administration of the compound (+)-(2S,3S)-2-(3-chlorophenyl)-3,5,5-trimethyl-2-morpholinol hydrochloride.  
     
     
         10 . A method as claimed in  claim 9  wherein said compound has an optical rotation [α] 20   D  at c=0.64 in 95% EtOH of +31.9°.  
     
     
         11 . A method of treating Parkinson's disease in a mammal comprising the administration to said mammal of an effective amount of (+)-(2S,3S)-2-(3-chlorophenyl)-3,5,5-trimethyl-2-morpholinol or pharmaceutically acceptable salts and solvates thereof.  
     
     
         12 . A method as claimed in  claim 11  wherein the treatment is for symptoms of locomotor deficit, motor disability, or both symptoms.  
     
     
         13 . A method as claimed  claim 11  wherein comprising the administration of the compound (+)-(2S,3S)-2-(3-chlorophenyl)-3,5,5-trimethyl-2-morpholinol hydrochloride.  
     
     
         14 . A method as claimed in  claim 13  wherein said compound has an optical rotation [α] 20   D  at c=0.64 in 95% EtOH of +31.9°.  
     
     
         15 . A method of treating migraine in a mammal comprising the administration to said mammal of an effective amount of (+)-(2S,3S)-2-(3-chlorophenyl)-3,5,5-trimethyl-2-morpholinol or pharmaceutically acceptable salts and solvates thereof.  
     
     
         16 . A method as claimed in  claim 15  wherein the treatment is prophylactic.  
     
     
         17 . A method as claimed in  claim 15  wherein comprising the administration of the compound (+)-(2S,3S)-2-(3-chlorophenyl)-3,5,5-trimethyl-2-morpholinol hydrochloride.  
     
     
         18 . A method as claimed in  claim 17  wherein said compound has an optical rotation [α] 20   D  at c=0.64 in 95% EtOH of +31.9°.  
     
     
         19 . A method of treating addiction to nicotine-containing products comprising the administration to a mammal of an effective amount of (+)-(2S,3S)-2-(3-chlorophenyl)-3,5,5-trimethyl-2-morpholinol or pharmaceutically acceptable salts and solvates thereof.  
     
     
         20 . A method as claimed in  claim 19  wherein comprising the administration of the compound (+)-(2S,3S)-2-(3-chlorophenyl)-3,5,5-trimethyl-2-morpholinol hydrochloride.  
     
     
         21 . A method as claimed in  claim 20  wherein said compound has an optical rotation [α] 20   D  at c=0.64 in 95% EtOH of +31.9°.