Chemokine-binding heterocyclic compound salts, and methods of use thereof
View Patent ↗The present invention relates to chemokine-binding heterocyclic compound salts, methods of use thereof, and methods for preparing the same.
1. A crystalline pharmaceutically acceptable salt of a compound of Formula I
wherein said salt is benzoate, 4-aminobenzoate, 4-hydroxybenzoate, orotate, 4-hydroxybenzenesulfonate, or 4-aminobenzenesulfonate.
2. The salt of claim 1 , wherein said salt is 4-aminobenzoate, 4-hydroxybenzenesulfonate, 4-aminobenzenesulfonate, or orotate.
3. The salt of claim 1 , wherein said salt is 4-hydroxybenzoate.
4. A pharmaceutical composition comprising a crystalline pharmaceutically acceptable salt of a compound of Formula I
wherein said salt is benzoate, 4-aminobenzoate, 4-hydroxybenzoate, orotate, 4-hydroxybenzenesulfonate, or 4-aminobenzenesulfonate, and a pharmaceutically acceptable diluent.
5. The composition of claim 4 , wherein said salt is 4-aminobenzoate, 4-hydroxybenzenesulfonate, 4-aminobenzenesulfonate, or orotate.
6. The composition of claim 4 , wherein said salt is 4-hydroxybenzoate.
7. A crystalline benzoate salt of a compound of Formula I
having less hydroscopicity than the hydrobromide or hydrochloric salt of said compound of Formula I.
8. The salt of claim 7 , wherein said benzoate is 4-hydroxybenzoate.
9. The salt of claim 7 , wherein said salt is more stable in storage than the hydrobromide or hydrochloride salt of said compound of Formula I.
10. The salt of claim 7 , wherein said salt has an improved stability as compared to the free base at about 30 degrees Celsius and above; at about 40 degrees Celsius and above; or at about 70 degrees Celsius and above.