US2014275616A1PendingUtilityA1
Salts of treprostinil
Est. expiryMar 15, 2033(~6.6 yrs left)· nominal 20-yr term from priority
C07C 51/412C07C 59/72C07C 51/41A61K 31/19A61P 9/12C07C 51/418C07C 59/13
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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-modifiedWhat is claimed is:
1 . A treprostinil salt compound according to the following formula:
that is produced by a process comprising:
alkylating a starting compound of the formula:
to form an O-alkylated compound that is not isolated; followed by optional base hydrolysis and contacting the resulting compound with a base or a base salt in situ;
wherein X is a pharmaceutically acceptable salt counterion and the treprostinil salt is isolated as at least 98% pure.
2 . The compound of claim 1 , wherein the treprostinil salt comprises a Group IA or IIA metal.
3 . The compound of claim 1 , wherein the treprostinil salt is K, Ca, Na, Ba, Li, Mg or Cs salt.
4 . The compound of claim 1 , wherein the treprostinil salt is isolated is at least 99% pure.
5 . The compound of claim 1 , wherein the treprostinil salt is isolated is at least 99.5% pure.
6 . A treprostinil salt compound according to the following formula:
wherein X is a pharmaceutically acceptable salt counterion and the treprostinil salt is isolated as at least 99% pure.
7 . The compound of claim 6 , wherein the salt comprises a Group IA or IIA metal.
8 . The compound of claim 6 , wherein the salt is K, Ca, Na, Ba, Li, Mg or Cs.
9 . The compound of claim 6 , wherein the compound is at least 99.5% pure.
10 . The compound of claim 6 , wherein the treprostinil salt is isolated is at least 99.95% pure.
11 . A treprostinil salt compound according to the following formula:
that is produced by a process comprising:
alkylating a starting compound of the formula:
to form an O-alkylated compound that is not isolated; followed by hydrogenolysis and contacting the resulting compound with a base or base salt in situ;
wherein X is a pharmaceutically acceptable salt counterion and the treprostinil salt is isolated as at least 98% pure.
12 . The compound of claim 11 , wherein the treprostinil salt comprises a Group IA or IIA metal.
13 . The compound of claim 11 , wherein the salt is K, Ca, Na, Ba, Li, Mg or Cs salt.
14 . The compound of claim 11 , wherein the treprostinil salt is isolated is at least 99% pure.
15 . The compound of claim 11 , wherein the treprostinil salt is isolated is at least 99.5% pure.
16 . A method for making a treprostinil salt compound according to the following formula:
comprising alkylating a starting compound of the formula:
to form an O-alkylated compound that is not isolated; followed by optional base hydrolysis and contacting the resulting compound with a base or a base salt in situ;
wherein X is a pharmaceutically acceptable salt counterion and the treprostinil salt is isolated as at least 98% pure.
17 . The method of claim 16 , wherein the treprostinil salt comprises a Group IA or IIA metal.
18 . The method of claim 16 , wherein the treprostinil salt is K, Ca, Na, Ba, Li, Mg or Cs salt.
19 . The method of claim 16 , wherein the treprostinil salt is isolated is at least 99% pure.
20 . The method of claim 16 , wherein the treprostinil salt is isolated is at least 99.5% pure.
21 . A method for making a treprostinil salt compound according to the following formula:
comprising alkylating a starting compound of the formula:
to form an O-alkylated compound that is not isolated; followed by hydrogenolysis and contacting the resulting compound with a base or a base salt in situ;
wherein X is a pharmaceutically acceptable salt counterion and the treprostinil salt as isolated has at least 98% purity.
22 . The method of claim 21 , wherein the treprostinil salt comprises a Group IA or IIA metal.
23 . The method of claim 21 , wherein the treprostinil salt is a K, Ca, Na, Ba, Li, Mg or Cs salt.
24 . The method of claim 21 , wherein the treprostinil salt is isolated is at least 99% pure.
25 . The method of claim 21 , wherein the treprostinil salt is isolated is at least 99.5% pure.Join the waitlist — get patent alerts
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