Formulations, salts and polymorphs of transnorsertraline and uses thereof

Abstract

Provided herein are pharmaceutical compositions comprising transnorsertraline, salts and polymorphic forms of transnorsertraline, methods of making the compositions, and methods for their use for the treatment of CNS diseases, including depression.

1 .- 7 . (canceled) 
     
     
         8 . A crystalline hydrochloride salt of transnorsertraline or a hydrate thereof, which has an X-ray powder diffraction pattern comprising peaks at about 14.9, 17.8, 19.2, 23.3, 24.6 and 25.2 degrees 2θ. 
     
     
         9 . The salt of  claim 8  which has an X-ray powder diffraction pattern further comprising peaks at about 5.0 and 21.8 degrees 2θ. 
     
     
         10 . The salt of  claim 9  which has a calculated X-ray powder diffraction pattern comprising peaks at about 5.1, 15.0, 18.0, 19.5, 22.0 23.5, 24.8 and 25.4 degrees 2θ, based on data collected at about 173 K on a single crystal. 
     
     
         11 . The salt of  claim 9  which has the following approximate unit cell dimensions:
 a=16.8 Å, b=5.2 Å, c=19.1 Å, α=90.0 °, β=113.1° and γ=90.0°. 
 
     
     
         12 . The salt of  claim 9  which has the following approximate unit cell dimensions when measured at about 173 K:
 a=16.83 Å, b=5.23 Å, c=19.06 Å, α=90.00°, β=113.10° and γ=90.00°. 
 
     
     
         13 . The salt of  claim 12  wherein the approximate unit cell dimensions are:
 a=16.834 Å, b=5.226 Å, c=19.059 Å, α=90.00°, β=113.10° and γ=90.00°. 
 
     
     
         14 . The salt of  claim 11  which has the space group C2 (no. 5). 
     
     
         15 . The salt of  claim 11  wherein the unit cell contains four transnorsertraline hydrochlorides (Z=4). 
     
     
         16 . The salt of  claim 8  which has a density of about 1.4 g cm −3 . 
     
     
         17 - 18 . (canceled) 
     
     
         19 . A method of treating, preventing, or managing a neurological disorder comprising administering to a patient a therapeutically or prophylactically effective amount of a compound according to  claim 8 . 
     
     
         20 . The method of  claim 19 , wherein the neurological disorder is depression, cognitive deficits, fibromyalgia, pain, a sleep related disorder, chronic fatigue syndrome, attention deficit disorder (ADD), attention deficit hyperactivity disorder (ADHD), restless leg syndrome, schizophrenia, anxiety, obsessive compulsive disorder, posttraumatic stress disorder, seasonal affective disorder (SAD), premenstrual dysphoria, post-menopausal vasomotor symptoms, a neurodegenerative disease, manic conditions, dysthymic disorder, cyclothymic disorder, obesity, or substance abuse or dependency.