Azaindole rock inhibitors
This invention provides rho-associated protein kinase (ROCK) inhibiting compounds for therapeutic applications as described further herein.
1. A compound of Formula:
or a pharmaceutically acceptable salt thereof;
wherein:
R 1 and R 2 are independently selected from the group consisting of hydrogen, C 1 -C 4 alkyl, C 1 -C 4 haloalkyl, and halogen.
2. The compound of claim 1 , wherein R 1 is hydrogen.
3. The compound of claim 1 , wherein R 1 is C 1 -C 4 alkyl.
4. The compound of claim 1 , wherein R 1 is methyl.
5. The compound of claim 1 , wherein R 2 is hydrogen.
6. The compound of claim 1 , wherein R 2 is C 1 -C 4 alkyl.
7. The compound of claim 1 , wherein R 2 is methyl.
8. The compound of claim 1 , wherein the compound is of Formula:
or a pharmaceutically acceptable salt thereof.
9. The compound of claim 8 , wherein R 2 is hydrogen or C 1 -C 4 alkyl.
10. The compound of claim 8 , wherein R 2 is hydrogen or methyl.
11. The compound of claim 1 , wherein the compound is of structure:
or a pharmaceutically acceptable salt thereof.
12. A pharmaceutical composition comprising a compound of claim 1 or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable excipient.
13. The pharmaceutical composition of claim 12 , wherein the compound of claim 1 is of structure:
or a pharmaceutically acceptable salt thereof.
14. The pharmaceutical composition of claim 13 , wherein the pharmaceutical composition is in the form of a tablet.
15. The pharmaceutical composition of claim 13 , wherein the pharmaceutical composition is in the form of a capsule.
16. The pharmaceutical composition of claim 13 , wherein the pharmaceutical composition is in the form of an injection or infusion solution.
17. A method of treating a ROCK1 or ROCK2 mediated disorder selected from amyotrophic lateral sclerosis, Parkinson's disease, Huntington's disease, and dementia in a human in need thereof comprising administering an effective amount of a compound of claim 1 or a pharmaceutically acceptable salt thereof, optionally in a pharmaceutical composition, to the human in need thereof.
18. The method of claim 17 , wherein the disorder is mediated by ROCK1.
19. The method of claim 17 , wherein the disorder is mediated by ROCK2.
20. The method of claim 17 , wherein the disorder is amyotrophic lateral sclerosis.
21. The method of claim 17 , wherein the disorder is Parkinson's disease.
22. The method of claim 17 , wherein the compound of claim 1 is a compound of structure:
or a pharmaceutically acceptable salt thereof.
23. The method of claim 22 , wherein the disorder is mediated by ROCK1.
24. The method of claim 22 , wherein the disorder is mediated by ROCK2.
25. The method of claim 22 , wherein the disorder is amyotrophic lateral sclerosis.
26. The method of claim 22 , wherein the disorder is Parkinson's disease.
27. The method of claim 22 , wherein the disorder is Huntington's disease.
28. The method of claim 22 , wherein the disorder is post-traumatic dementia.