IP Library › Granted Patent US 11,787,808
Granted Patent B2
US 11,787,808 · App. 17/289,609 · Granted Oct 17, 2023

Folate salts

Inventors: Martin Ulmann (Dachsen, CH); Gerd Wiesler (Lohn, CH); Arthur Bodenmüller (Seltisberg, CH); Markus Müller
Assignee: APROFOL AG
C07D475/04A23L33/10A61K31/519C07B2200/13
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Quick Facts
Patent No.
US 11,787,808
App. No.
17/289,609
Granted
Oct 17, 2023
Kind
B2
Abstract

The invention relates to crystalline folate salts. The salt consists of a folate anion and an organic cation. The folate anion is 5-methyl-(6S)-tetrahydrofolic acid, and the cation is an organic compound which is an alkanolamine selected from the group consisting of choline, N-methylaminoethanol, 2-amino-2-methylpropanol and 2-dimethylaminoethanol.

Claims (6)

1. A crystalline folate salt comprising a tetrahydrofolic acid anion and an organic cation wherein the anion is 5-methyl-(6S)-tetrahydrofolic acid, and the cation is an organic compound wherein the organic compound is choline.

2. The crystalline folate salt according to claim 1 , wherein the folate salts have a solubility of higher than 2 weight-% (w/w) based on a total weight of a solution at 20° C. in organic solvents.

3. The crystalline folate salt according to claim 1 , wherein the organic compound is di-choline.

4. The crystalline folate acid salt according to claim 1 , wherein the tetrahydrofolic acid anion is 5-methyl-(6S)-tetrahydrofolic acid and the organic cation is di-choline.

5. A pharmaceutical composition, comprising at least one folate salt according to claim 1 , as a main active compound and at least a pharmaceutically acceptable excipient.

6. A method for preparing the crystalline folate salt according to claim 1 , comprising crystallizing a folate salt comprising a tetrahydrofolic acid anion and an organic cation from an organic solvent comprising water in a range of 0.2 weight-% to 12 weight-% based on a weight of the organic solvent comprising the water.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 31, 2023
From: WIESLER, GERD; BODENMÜLLER, ARTHUR; MÜLLER, MARKUS; ULMANN, MARTIN
To: APROFOL AG
Reel/Frame 062583/0178 →
Priority Claims (1)
EP 18203849 · Oct 31, 2018 · regional
Continuity (1)
Related Publication 20210403471A1 · Dec 30, 2021