Compositions comprising folic acid derivatives, their preparations and methods of use

• US 10,259,813 B2
• Filed: 03/05/2018
• Issued: 04/16/2019
• Est. Priority Date: 07/27/2012
• Status: Active Grant

• Current Assignee: JSB Pharma Development LLC
• Original Assignee: Chemic Laboratories, Inc. (Solvias AG)
• Inventors: Jones, Jr., Gerald S., St. Laurent, Joseph P., Goodrich, Scott A.
• Primary Examiner(s): Leeser, Erich A
• Application Number:
  US15/912,070
• Publication Number:
  US 20190048011A1
• Time in Patent Office: 407 Days
• CPC Class Codes: A61K 31/519 ortho- or peri-condensed with heterocyclic rings
• CPC Class Codes: C07D 475/04 with a nitrogen atom directly attached in position 2
• CPC Class Codes: C07D 487/14 Ortho-condensed systems

Abstract

Described herein are methods for making folic acid derivatives, intermediates, pharmaceutical compositions and uses thereof.

Claims

1. A method of treating a folic acid deficiency in a subject in need thereof, comprising administering to the subject an oral dosage form comprising a compound of Formula (V):

2. The method of claim 1, wherein R¹ is NH₂.

3. The method of claim 1, wherein R² is OH.

4. The method of claim 1, wherein R³ is H.

5. The method of claim 1, wherein Y is Cl.

6. The method of claim 1, wherein R¹ is NH₂, R² is OH and R³ is H.

7. The method of claim 1, wherein the subject is a pregnant female.

8. A method of providing folic acid to a subject in need thereof, comprising administering to the subject an oral dosage form comprising a compound of Formula (V):

9. The method of claim 8, wherein R¹ is NH₂.

10. The method of claim 8, wherein R² is OH.

11. The method of claim 8, wherein R³ is H.

12. The method of claim 8, wherein Y is Cl.

13. The method of claim 8, wherein R¹ is NH₂, R² is OH and R³ is H.

14. The method of claim 8, wherein the subject is a pregnant female.