IP Library Granted Patent US 8,012,943
Granted Patent B2
US 8,012,943 · App. 12/430,736 · Granted Sep 6, 2011

Antibacterial agents

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Quick Facts
Patent No.
US 8,012,943
App. No.
12/430,736
Granted
Sep 6, 2011
Kind
B2
Abstract

Described herein are novel macrolides, the preparation of novel macrolides, the use of novel macrolides for preventing, treating, or ameliorating various conditions, and the use of novel macrolides as antibacterial agents.

Claims (38)

1. A compound of the formula

or a pharmaceutically acceptable salt or hydrate thereof, wherein:

A is —CH 2 —;

B is —(CH 2 ) n —, where n is an integer in the range from 0 to 10;

C is aryl or heteroaryl; and

W is H or F.

2. The compound of claim 1 wherein B is —(CH 2 ) n —, and n is an integer from 2-4.

3. The compound of claim 2 wherein n is 3.

4. The compound of claim 1 wherein C is 3-aminophenyl or 3-pyridinyl.

5. The compound of claim 1 wherein W is F.

6. A pharmaceutical composition for treating a disease selected from the group consisting of bacterial infections, protozoal infections, diseases related to bacterial infections or protozoal infections, and combinations thereof, the composition comprising a therapeutically effective amount of one or more compounds of claim 1 .

7. A pharmaceutical composition comprising an anti-bacterially effective amount of one or more compounds of claim 1 .

8. A method for treating a disease selected from the group consisting of bacterial infections, protozoal infections, diseases related to bacterial infections or protozoal infections, and combinations thereof, the method comprising the step of administering a therapeutically effective amount of one or more compounds of claim 1 to a patient in need of relief from the disease.

9. A pharmaceutical composition comprising an anti-bacterially effective amount of a compound of the formula

wherein:

A is —CH 2 —;

B is —(CH 2 ) n —, where n is an integer in the range from 0 to 10;

C is aryl or heteroaryl; and

W is H or F.

10. The composition of claim 9 wherein B is —(CH 2 ) n —, and n is an integer from 2-4.

11. The composition of claim 10 wherein n is 3.

12. The composition of claim 9 wherein C is 3-aminophenyl or 3-pyridinyl.

13. The composition of claim 9 wherein W is F.

14. A method for treating a disease selected from the group consisting of bacterial infections, protozoal infections, diseases related to bacterial infections or protozoal infections, and combinations thereof, the method comprising the step of administering a therapeutically effective amount of the pharmaceutical composition of claim 9 to a patient in need of relief from the disease.

15. A compound of the formula

or a pharmaceutically acceptable salt or hydrate thereof.

16. A pharmaceutical composition for treating a disease selected from the group consisting of bacterial infections, protozoal infections, diseases related to bacterial infections or protozoal infections, and combinations thereof, the composition comprising a therapeutically effective amount of the compound of claim 15 .

17. A pharmaceutical composition comprising an anti-bacterially effective amount of the compound of claim 15 .

18. A method for treating a disease selected from the group consisting of bacterial infections, protozoal infections, diseases related to bacterial infections or protozoal infections, and combinations thereof, the method comprising the step of administering a therapeutically effective amount of the compound of claim 15 to a patient in need of relief from the disease.

19. A pharmaceutical composition comprising an anti-bacterially effective amount of a compound of the formula

20. A method for treating a disease selected from the group consisting of bacterial infections, protozoal infections, diseases related to bacterial infections or protozoal infections, and combinations thereof, the method comprising the step of administering a therapeutically effective amount of the pharmaceutical composition of claim 19 to a patient in need of relief from the disease.

21. A compound of the formula

or a pharmaceutically acceptable salt thereof.

22. A pharmaceutical composition for treating a disease selected from the group consisting of bacterial infections, protozoal infections, diseases related to bacterial infections or protozoal infections, and combinations thereof, the composition comprising a therapeutically effective amount of the compound or salt of claim 21 .

23. A pharmaceutical composition comprising an anti-bacterially effective amount of the compound or salt of claim 21 .

24. A method for treating a disease selected from the group consisting of bacterial infections, protozoal infections, diseases related to bacterial infections or protozoal infections, and combinations thereof, the method comprising the step of administering a therapeutically effective amount of the compound or salt of claim 21 to a patient in need of relief from the disease.

25. A pharmaceutical composition comprising a compound of the formula,

or a pharmaceutically acceptable salt thereof, and a physiologically acceptable carrier or excipient.

Assignments (3)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 14, 2019
From: CEMPRA PHARMACEUTICALS, INC.
To: TETARD, INC.
Reel/Frame 050056/0731 →
NUNC PRO TUNC ASSIGNMENT Recorded Aug 14, 2015
From: OPTIMER PHARMACEUTICALS LLC
To: MERCK SHARP & DOHME CORP.
Reel/Frame 036328/0122 →
CHANGE OF NAME Recorded Aug 12, 2015
From: OPTIMER PHARMACEUTICALS, INC.
To: OPTIMER PHARMACEUTICALS LLC
Reel/Frame 036333/0793 →