US2019262351A1PendingUtilityA1

Noribogaine compositions

51
Assignee: DEMERX INCPriority: Jul 23, 2010Filed: Jun 3, 2016Published: Aug 29, 2019
Est. expiryJul 23, 2030(~4 yrs left)· nominal 20-yr term from priority
Inventors:Robert M. MoriartyDeborah C. Mash
A61P 25/30A61P 25/04A61K 31/55C07D 487/14
51
PatentIndex Score
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Claims

Abstract

Disclosed are noribogaine compositions comprising a very high level of the 2(R), 4(S), 5(S), 6(S) and 18(R) enantiomer and not more than 0.5 wt % of ibogaine relative to the total amount of noribogaine.

Claims

exact text as granted — not AI-modified
1 .- 12 . (canceled) 
     
     
         13 . Noribogaine or a salt thereof prepared from ibogaine, wherein at least 95% of the noribogaine is its 2(R), 4(S), 5(S), 6(S), and 18(R) enantiomer and no more than 0.5 wt % of the total amount of noribogaine and ibogaine present is ibogaine. 
     
     
         14 . The noribogaine or salt thereof according to  claim 13 , wherein the noribogaine or salt thereof is prepared by a method comprising demethylating ibogaine in solvent using a Lewis acid followed by quenching, to obtain the noribogaine or said salt thereof. 
     
     
         15 . The noribogaine or salt thereof according to  claim 13 , wherein the noribogaine or salt thereof is prepared from ibogaine by a method comprising forming amine-protected ibogaine, demethylating said amine-protected ibogaine in solvent using a Lewis acid to form amine-protected noribogaine and deprotecting said amine-protected noribogaine to obtain the noribogaine or said salt thereof. 
     
     
         16 . The noribogaine or salt thereof according to  claim 13 , wherein the noribogaine or salt thereof is prepared from ibogaine by a method comprising forming amine-protected ibogaine, demethylating said amine-protected ibogaine in solvent using a Lewis acid to form amine-protected noribogaine, appending said amine-protected noribogaine to a solid support, removing the amine-protecting group from the amine-protected noribogaine and removing the resulting noribogaine from said solid support. 
     
     
         17 . The noribogaine or salt thereof according to  claim 14 , wherein said Lewis acid is boron tribromide or boron trichloride. 
     
     
         18 . The noribogaine or salt thereof according to  claim 14 , wherein said Lewis acid is boron trichloride. 
     
     
         19 . The noribogaine or salt thereof according to  claim 14 , wherein said Lewis acid is boron tribromide. 
     
     
         20 . The noribogaine or salt thereof according to  claim 15 , wherein said Lewis acid is boron tribromide or boron trichloride. 
     
     
         21 . The noribogaine or salt thereof according to  claim 15 , wherein said Lewis acid is boron trichloride. 
     
     
         22 . The noribogaine or salt thereof according to  claim 15 , wherein said Lewis acid is boron tribromide. 
     
     
         23 . The noribogaine or salt thereof according to  claim 16 , wherein said Lewis acid is boron tribromide or boron trichloride. 
     
     
         24 . The noribogaine or salt thereof according to  claim 16 , wherein said Lewis acid is boron trichloride. 
     
     
         25 . The noribogaine or salt thereof according to  claim 16 , wherein said Lewis acid is boron tribromide. 
     
     
         26 . The noribogaine or salt thereof according to  claim 13 , wherein the noribogaine is in the form of its hydrochloride salt. 
     
     
         27 . The noribogaine or salt thereof according to  claim 13 , at least 98% of the noribogaine is the 2(R), 4(S), 5(S), 6(S), and 18(R) enantiomer. 
     
     
         28 . The noribogaine or salt thereof according to  claim 13 , wherein the amount of ibogaine present is not more than 0.1 wt %. 
     
     
         29 . A composition comprising noribogaine or a salt thereof and ibogaine, wherein at least 95% of the noribogaine is its 2(R), 4(S), 5(S), 6(S), and 18(R) enantiomer and wherein said composition comprises no more than 0.5 wt % ibogaine of the total amount of noribogaine and ibogaine in the composition. 
     
     
         30 . The composition according to  claim 29 , wherein the noribogaine or salt thereof is in solid farm. 
     
     
         31 . The composition according to  claim 29 , further comprising isopropanol. 
     
     
         32 . The composition according to  claim 29 , wherein the noribogaine is in the form of its hydrochloride salt.

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