Methods for treating resistant diseases using triazole containing macrolides
View Patent ↗Described herein are macrolide and ketolide antibiotics and pharmaceutical compositions, methods, and uses thereof for treating diseases caused at least in party by resistant bacteria.
1. A method for treating a disease in a host animal, where the disease is a gonococcal infection or community-acquired bacterial pneumonia caused at least in part by one or more bacteria resistant to azithromycin or clarithromycin, or both, the method comprising the step of administering an effective amount to the host animal of a compound of the formula
or a salt thereof, wherein:
R 10 is hydrogen or acyl;
W is H or F;
A is CH 2 ;
B is C 0 -C 10 alkyl, C 2 -C 10 alkenyl, or C 4 -C 10 alkynyl, or C 4 -C 10 alkenylalkynyl; and
C is aryl, heteroaryl, arylalkyl, or heteroarylalkyl, each of which is optionally substituted.
2. The method of claim 1 wherein C is optionally substituted aryl or optionally substituted heteroaryl.
3. The method of claim 1 wherein C is aminophenyl.
4. The method of claim 1 wherein C is pyridinyl.
5. The method of claim 1 wherein C is 3-aminophenyl.
6. The method of claim 1 wherein C is 3-pyridinyl.
7. The method of claim 1 wherein R 10 is hydrogen.
8. The method of claim 1 wherein A and B are taken together to form butylene or pentylene.
9. The method of claim 1 wherein A is CH 2 and B is (CH 2 )n and n is an integer from 2-4.
10. The method of claim 9 wherein n is 3.
11. The method of claim 1 wherein W is F.
12. The method of claim 1 wherein the compound recited in claim 1 is of the formula
13. The method of claim 1 wherein the compound recited in claim 1 is of the formula
where HX is a pharmaceutically acceptable salt forming acid.
14. The method of claim 13 wherein HX is selected from the group consisting of hydrochloric acid, tartaric acid, and combinations thereof.
15. The method of claim 1 wherein the disease is a gonococcal infection.
16. The method of claim 1 wherein the disease is community-acquired bacterial pneumonia.
17. The method of claim 1 wherein the bacteria is also resistant to a quinolone.
18. The method of claim 1 wherein the bacteria is also resistant to vancomycin.
19. The method of claim 1 wherein the host animal is a human.
20. The method of claim 1 wherein the bacteria is Neisseria gonorrhoeae .
21. The method of claim 1 wherein the bacteria is a Streptococcus, Staphylococcus, Mycoplasma, Legionella pneumophila, Moraxella catarrhalis , or Haemophilus influenzae , or a combination thereof.
22. The method of claim 16 wherein the bacteria is a Streptococcus, Staphylococcus , or Mycoplasma , or a combination thereof.
23. The method of claim 22 wherein the bacteria is resistant to azithromycin.
24. The method of claim 22 wherein the bacteria is resistant to clarithromycin.
25. The method of claim 1 wherein the disease is urethritis.
26. The method of claim 1 wherein the disease is pelvic inflammatory disease.
27. The method of claim 1 wherein the disease is pharyngitis.