US2019256449A1PendingUtilityA1
Salts of treprostinil
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
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Claims
Abstract
Provided are novel treprostinil salts as well as methods for making treprostinil salts.
Claims
exact text as granted — not AI-modified1 - 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
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