US2019256449A1PendingUtilityA1

Salts of treprostinil

Assignee: UNITED THERAPEUTICS CORPPriority: Mar 15, 2013Filed: Apr 30, 2019Published: Aug 22, 2019
Est. expiryMar 15, 2033(~6.6 yrs left)· nominal 20-yr term from priority
C07C 51/41C07C 51/412C07C 59/72A61K 31/19A61P 9/12
78
PatentIndex Score
0
Cited by
0
References
0
Claims

Abstract

Provided are novel treprostinil salts as well as methods for making treprostinil salts.

Claims

exact text as granted — not AI-modified
1 - 15 . (canceled) 
     
     
         16 . A salt of treprostinil, wherein the salt is a tromethamine salt, an arginine salt, an L-Lysine salt, an N-methylglucamine salt, a magnesium salt or an ammonium salt. 
     
     
         17 . The salt of  claim 16 , wherein the salt is a tromethamine salt of treprostinil. 
     
     
         18 . The salt of  claim 16 , wherein the salt is an arginine salt of treprostinil 
     
     
         19 . The salt of  claim 16 , wherein the salt is an L-Lysine salt of treprostinil. 
     
     
         20 . The salt of  claim 16 , wherein the salt is an N-methylglucamine salt of treprostinil. 
     
     
         21 . The salt of  claim 16 , wherein the salt is a magnesium salt of treprostinil. 
     
     
         22 . The salt of  claim 16 , wherein the salt is an ammonium salt of treprostinil 
     
     
         23 . A pharmaceutical formulation comprising the salt of  claim 16  and a pharmaceutically acceptable excipient. 
     
     
         24 . The pharmaceutical formulation of  claim 23 , which is a solid dose formulation. 
     
     
         25 . A method of making a salt of treprostinil, comprising reacting treprostinil with a base, which is selected from tromethamine, arginine, L-Lysine, N-methylglucamine, choline hydroxide, calcium hydroxide, magnesium hydroxide or ammonia to form a salt and
 crystallizing the formed salt.   
     
     
         26 . The method of  claim 25 , wherein a solvent for the reacting and a solvent for said crystallizing is the same. 
     
     
         27 . The method of  claim 25 , wherein a solvent for the reacting is different from a solvent for said crystallizing. 
     
     
         28 . The method of  claim 25 , wherein a solvent for the reacting comprises an alcohol. 
     
     
         29 . The method of  claim 28 , wherein the solvent for the reacting further comprises water. 
     
     
         30 . The method of  claim 29 , wherein the reacting comprises heating a mixture comprising the solvent, the base and the treprostinil to a temperature greater than 50° C. 
     
     
         31 . The method of  claim 25 , wherein the base is tromethamine. 
     
     
         32 . The method of  claim 30 , wherein a solvent for the reacting comprises isopropanol and methyl t-butyl ether. 
     
     
         33 . The method of  claim 25 , wherein the base is arginine. 
     
     
         34 . The method of  claim 33 , wherein a solvent for the reacting comprises isopropanol and ethyl acetate. 
     
     
         35 . The method of  claim 33 , wherein a solvent for the crystallizing comprises ethanol. 
     
     
         36 . The method of  claim 25 , wherein the base is L-lysine. 
     
     
         37 . The method of  claim 36 , wherein a solvent for the reacting comprises isopropanol and ethyl acetate. 
     
     
         38 . The method of  claim 25 , wherein the base is N-methylglucamine. 
     
     
         39 . The method of  claim 38 , wherein a solvent for the reacting comprises isopropanol, methyl t-butyl ether and hexanes. 
     
     
         40 . The method of  claim 25 , wherein the base is magnesium hydroxide. 
     
     
         41 . The method of  claim 40 , wherein a solvent for the reacting comprises ethanol, methyl t-butyl ether and hexanes. 
     
     
         42 . The method of  claim 25 , wherein the base is ammonia. 
     
     
         43 . The method of  claim 42 , wherein a solvent for the reacting comprises isopropanol, methyl t-butyl ether and hexanes. 
     
     
         44 . The method of  claim 25 , wherein the base is choline hydroxide. 
     
     
         45 . The method of  claim 44 , wherein a solvent for the reacting comprises isopropanol and methyl t-butyl ether. 
     
     
         46 . The method of  claim 25 , wherein the base is calcium hydroxide. 
     
     
         47 . The method of  claim 46 , wherein a solvent for the reacting comprises ethanol.

Join the waitlist — get patent alerts

Track US2019256449A1 — get alerts on status changes and closely related new filings.

We store only your email — no account needed. See our privacy policy.