Boron-containing small molecules
This invention provides, among other things, novel compounds useful for treating inflammatory conditions, pharmaceutical compositions containing such compounds, as well as combinations of these compounds with at least one additional therapeutically effective agent.
1. A compound which has a structure according to the following formula:
wherein
R is halogen or unsubstituted alkoxy,
or a salt thereof.
2. A combination comprising:
(a) the compound of claim 1 or
(b) an additional therapeutic agent.
3. The combination of claim 2 , wherein the additional therapeutic agent is selected from the group consisting of a beta-antagonist, a prostaglandin, an alpha2 adrenoreceptor agonist, a carbonic anhydrase inhibitor and a miotic.
4. The combination of claim 3 , wherein the additional therapeutic agent is a beta-antagonist, and the beta-antagonist is selected from the group consisting of timolol betaxolol hydrochloride, metipranolol and carteolol.
5. The combination of claim 3 , wherein the additional therapeutic agent is a prostaglandin, and the prostaglandin is selected from the group consisting of latanoprost, unoprostone isopropyl, travoprost and bimatoprost.
6. The combination of claim 3 , wherein the additional therapeutic agent is an alpha2-adrenoreceptor agonist, and the alpha2-adrenoreceptor agonist is selected from the group consisting of brimonidine tartrate, apraclonidine and dipivefrin.
7. The combination of claim 3 , wherein the additional therapeutic agent is a carbonic anhydrase inhibitor, and the carbonic anhydrase inhibitor is selected from the group consisting of dorzolamide hydrochloride and brinzolamide.
8. The combination of claim 3 , wherein the additional therapeutic agent is a miotic, and the miotic is selected from the group consisting of physostigmine, carbacol and piolocarpine.
9. A pharmaceutical formulation comprising:
(a) the compound of claim 1 , or
(b) a pharmaceutically acceptable excipient.
10. The compound of claim 1 , having a structure which is
11. The compound of claim 1 , having a structure which is
12. The compound of claim 1 , having a structure which is
13. The compound of claim 1 , wherein R is F.
14. The compound of claim 1 , wherein R is Cl.
15. The compound of claim 1 , wherein R is unsubstituted C 1 or C 2 or C 3 or C 4 or C 5 or C 6 alkoxy.
16. The compound of claim 1 , wherein R is unsubstituted C 1 or C 2 or C 3 alkoxy.
17. The compound of claim 1 , having a structure which is
or a salt thereof.
18. The compound of claim 1 , having a structure which is
or a salt thereof.
19. The compound of claim 1 , having a structure which is
or a salt thereof.
20. The compound of claim 1 , having a structure which is
or a salt thereof.
21. The combination of claim 2 , wherein the compound of part a) has a structure which is
or a salt thereof.
22. The combination of claim 2 , wherein the compound of part a) has a structure which is
or a salt thereof.
23. The combination of claim 2 , wherein the compound of part a) has a structure which is
or a salt thereof.
24. The combination of claim 2 , wherein the compound of part a) has a structure which is
or a salt thereof.
25. The pharmaceutical formulation of claim 9 , wherein the compound of part a) has a structure which is
or a salt thereof.
26. The pharmaceutical formulation of claim 9 , wherein the compound of part a) has a structure which is
or a salt thereof.
27. The pharmaceutical formulation of claim 9 , wherein the compound of part a) has a structure which is
or a salt thereof.
28. The pharmaceutical formulation of claim 9 , wherein the compound of part a) has a structure which is
or a salt thereof.