Boron-containing small molecules
This invention provides novel compounds of the following formula and pharmaceutical compositions containing such compounds.
1. A compound which has a structure according to the following formula:
wherein
R a is halogen,
R b is H or unsubstituted C 1 -C 4 alkyl,
when R b is unsubstituted C 1 -C 4 alkyl, then R is H or halogen or unsubstituted C 1 -C 4 alkyl,
when R b is H, then R is halogen or unsubstituted C 1 -C 4 alkyl,
or a salt thereof.
2. The compound of claim 1 , or a salt thereof, which has a structure according to the following formula:
wherein
R a is halogen,
R b is unsubstituted C 1 -C 4 alkyl,
R is H or halogen or unsubstituted C 1 -C 4 alkyl.
3. The compound of claim 1 , or a salt thereof, which has a structure which is:
4. The compound of claim 1 , or a salt thereof, in which R is F, Cl, methyl, ethyl, or isopropyl.
5. The compound of claim 1 , or a salt thereof, in which R a is F or Cl.
6. The compound of claim 1 , or a salt thereof, in which R b is methyl.
7. The compound of claim 1 , or a salt thereof, in which R a is F or Cl, and R b is methyl.
8. The compound of claim 1 , or a salt thereof, in which R a is Cl and R b is methyl.
9. The compound of claim 1 , or a salt thereof, in which R a is F or Cl, R b is methyl, and R is methyl.
10. The compound of claim 1 , or a salt thereof, in which R a is F or Cl, R b is methyl, and R is ethyl.
11. The compound of claim 1 , or a salt thereof, in which R a is F or Cl, R b is methyl, and R is isopropyl.
12. A combination comprising:
(a) the compound of claim 1 , or a salt thereof, and
(b) an additional therapeutic agent.
13. A pharmaceutical formulation comprising:
(a) the compound of claim 1 , or a salt thereof, and
(b) a pharmaceutically acceptable excipient.
14. A method of inhibiting a kinase, comprising contacting said kinase with the compound of claim 1 , or a salt thereof, thereby inhibiting said kinase whereby said kinase is ROCK1 or ROCK2.
15. A method of treating a disease, comprising administering to an animal in need of treatment a therapeutically effective amount of the compound of claim 1 , or a salt thereof, thereby treating said disease, wherein the disease is selected from the group consisting of glaucoma, asthma, pulmonary hypertension, angina, heart failure, wound healing, and spinal cord injury.
16. The method of claim 15 , wherein said disease is glaucoma.
17. The method of claim 15 , wherein said disease is pulmonary hypertension.
18. The method of claim 15 , wherein said animal is a human.
19. The method of claim 15 , wherein said disease is glaucoma, and the glaucoma is selected from the group consisting of a primary glaucoma, a developmental glaucoma, a secondary glaucoma and absolute glaucoma.