2,4,6-Triaminopyrimidines for the treatment of depression and/or anxiety
This invention is directed to pyrimidine derivatives which are selective antagonists for the GalR3 receptor. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a pharmaceutical composition made by combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a method of treating a subject suffering from depression and/or anxiety which comprises administering to the subject an amount of a compound of the invention effective to treat the subject's depression and/or anxiety. This invention also provides a method of treating depression and/or anxiety in a subject which comprises administering to the subject a composition comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of a GalR3 receptor antagonist.
1. A compound having the structure:
2. A compound having the structure:
3. A compound having the structure:
4. A compound having the structure:
5. A compound having the structure:
6. A compound having the structure:
wherein the methyl groups off the morpholine are trans to each other.
7. The compound of claim 6 , wherein the compound is enantiomerically pure.
8. A pharmaceutical composition comprising a therapeutically effective amount of the compound of claim 6 and a pharmaceutically acceptable carrier.
9. The pharmaceutical composition of claim 8 , wherein the amount of the compound is from about 0.01 mg to about 1000 mg.
10. The pharmaceutical composition of claim 9 , wherein the amount of the compound is from about 0.1 mg to about 500 mg.
11. The pharmaceutical composition of claim 10 , wherein the amount of the compound is from about 1 mg to about 200 mg.
12. The pharmaceutical composition of claim 11 , wherein the amount of the compound is from about 10 mg to about 100 mg.
13. The pharmaceutical composition of claim 12 , wherein the carrier is a liquid and the composition is a solution.
14. The pharmaceutical composition of claim 8 , wherein the carrier is a solid and the composition is a tablet.
15. The pharmaceutical composition of claim 8 , wherein the carrier is a gel and the composition is a suppository.
16. A process of making a pharmaceutical composition comprising admixing a therapeutically effective amount of the compound of claim 6 and a pharmaceutically acceptable carrier.
17. A method of treating a subject suffering from depression, which comprises administering to the subject a dose of the compound of claim 6 effective to treat the subject's depression.
18. A method of treating a subject suffering from anxiety, which comprises administering to the subject a dose of the compound of claim 6 effective to treat the subject's anxiety.
19. The method of claim 17 , wherein the therapeutically effective amount is between about 0.01 and about 1000 mg per day.
20. The method of claim 19 , wherein the therapeutically effective amount is between about 0.10 and about 500 mg per day.
21. The method of claim 20 , wherein the therapeutically effective amount is between about 1.0 and about 200 mg per day.
22. The method of claim 21 , wherein the therapeutically effective amount is between about 10 and about 100 mg per day.
23. The method of claim 17 , wherein the compound can be administered orally.
24. The method of claim 17 , wherein the subject is a vertebrate, a mammal, a canine or a human.
25. The method of claim 17 , wherein the compound is administered in combination with food.