Boron containing small molecules
Novel monosubstituted and disubstutituted oxaboroles and pharmaceutical compositions containing such oxaboroles are provided, which are useful for treating bacterial infections, as well as combinations of these oxaboroles with at least one additional therapeutically effective agent.
1. A compound having a structure according to the formula:
wherein
R* is H;
R 3 is —CH 2 NH 2 ;
R a is H or —YR 5
wherein
Y is O;
R 5 is:
wherein
a is an integer selected from 1, 2, 3, or 4;
each R 10 and each R 11 is H;
R 12 is H;
or a salt thereof.
2. A combination comprising a first therapeutically active agent which is the compound of claim 1 , wherein the salt is a pharmaceutically acceptable salt thereof, together with at least one other therapeutically active agent.
3. A pharmaceutical formulation comprising:
a) the compound of claim 1 or a salt thereof, wherein said salt is a pharmaceutically acceptable salt thereof; and
b) a pharmaceutically acceptable excipient.
4. The pharmaceutical formulation of claim 3 wherein the pharmaceutical formulation is a unit dosage form.
5. A compound having a structure which is:
or a salt thereof.
6. A compound which is
or a salt thereof.
7. A combination comprising a first therapeutically active agent which is the compound of claim 6 or a salt thereof, wherein the salt is a pharmaceutically acceptable salt thereof, together with at least one other therapeutically active agent.
8. A pharmaceutical formulation comprising:
a) the compound of claim 6 or a salt thereof, wherein said salt is a pharmaceutically acceptable salt thereof; and
b) a pharmaceutically acceptable excipient.
9. The compound of claim 6 , which is
or a salt thereof.
10. A combination comprising a first therapeutically active agent which is the compound of claim 9 or a salt thereof, wherein the salt is a pharmaceutically acceptable salt thereof, together with at least one other therapeutically active agent.
11. A pharmaceutical formulation comprising:
a) the compound of claim 9 or a salt thereof, wherein said salt is a pharmaceutically acceptable salt thereof; and
b) a pharmaceutically acceptable excipient.
12. A compound which is
or a salt thereof.
13. A combination comprising a first therapeutically active agent which is the compound of claim 12 , wherein the salt is a pharmaceutically acceptable salt thereof, together with at least one other therapeutically active agent.
14. A pharmaceutical formulation comprising:
a) the compound of claim 12 , wherein said salt is a pharmaceutically acceptable salt thereof; and
b) a pharmaceutically acceptable excipient.
15. The compound of claim 12 , which is
or a salt thereof.
16. A combination comprising a first therapeutically active agent which is the compound of claim 15 or a salt thereof, wherein the salt is a pharmaceutically acceptable salt thereof, together with at least one other therapeutically active agent.
17. A pharmaceutical formulation comprising:
a) the compound of claim 15 or a salt thereof, wherein said salt is a pharmaceutically acceptable salt thereof; and
b) a pharmaceutically acceptable excipient.
18. A compound which is
or a salt thereof.
19. A combination comprising a first therapeutically active agent which is the compound of claim 18 or a salt thereof, wherein the salt is a pharmaceutically acceptable salt thereof, together with at least one other therapeutically active agent.
20. A pharmaceutical formulation comprising:
a) the compound of claim 18 or a salt thereof, wherein said salt is a pharmaceutically acceptable salt thereof; and
b) a pharmaceutically acceptable excipient.
21. The compound of claim 18 , which is
or a salt thereof.
22. A combination comprising a first therapeutically active agent which is the compound of claim 21 or a salt thereof, wherein the salt is a pharmaceutically acceptable salt thereof, together with at least one other therapeutically active agent.
23. A pharmaceutical formulation comprising:
a) the compound of claim 21 or a salt thereof, wherein said salt is a pharmaceutically acceptable salt thereof; and
b) a pharmaceutically acceptable excipient.
24. A compound which is
or a salt thereof.
25. A combination comprising a first therapeutically active agent which is the compound of claim 24 or a salt thereof, wherein the salt is a pharmaceutically acceptable salt thereof, together with at least one other therapeutically active agent.
26. A pharmaceutical formulation comprising:
a) the compound of claim 24 or a salt thereof, wherein said salt is a pharmaceutically acceptable salt thereof; and
b) a pharmaceutically acceptable excipient.
27. The compound of claim 24 , which is
or a salt thereof.
28. A combination comprising a first therapeutically active agent which is the compound of claim 27 or a salt thereof, wherein the salt is a pharmaceutically acceptable salt thereof, together with at least one other therapeutically active agent.
29. A pharmaceutical formulation comprising:
a) the compound of claim 27 or a salt thereof, wherein said salt is a pharmaceutically acceptable salt thereof; and
b) a pharmaceutically acceptable excipient.