BORON-CONTAINING SMALL MOLECULES AS ANTIPROTOZOAL AGENTS

• US 20110207701A1
• Filed: 08/16/2010
• Published: 08/25/2011
• Est. Priority Date: 08/19/2009
• Status: Abandoned Application

• Current Assignee: Anacor Pharmaceuticals, Inc. (Pfizer Inc.)
• Original Assignee: Anacor Pharmaceuticals, Inc. (Pfizer Inc.)
• Inventors: Zhou, Huchen, Ding, Dazhong, Plattner, Jacob J., Zhou, Yasheen, Zhang, Yong-Kang
• Application Number:
  US12/857,305
• Publication Number:
  US 20110207701A1
• Time in Patent Office: Days
• US Class Current: 514/64
• CPC Class Codes: A61P 33/02 Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
• CPC Class Codes: A61P 33/06 Antimalarials
• CPC Class Codes: C07F 5/025 Boronic and borinic acid compounds

Abstract

This invention provides, among other things, novel compounds useful for treating protozoal infections, pharmaceutical compositions containing such compounds, as well as combinations of these compounds with at least one additional therapeutically effective agent.

Claims

1. A compound having a structure according to the following formula:

2. The compound of claim 1, having a structure according to the following formula:

3. The compound of claim 1, which is

9. The method of claim 8, wherein the compound is according to claim 1.

16. The method of claim 15, wherein the compound is according to claim 1.

20. A use of the compound of claim 1 in the manufacture of a medicament for the treatment and/or prophylaxis of protozoal infection.

4. A combination comprising the compound of a preceding claim, together with at least one other therapeutically active agent.

5. A pharmaceutical formulation comprising:

a) the compound of a preceding claim, or a salt thereof; and

b) a pharmaceutically acceptable excipient.

6. The pharmaceutical formulation of claim 5, wherein the pharmaceutical formulation is a unit dosage form.

7. The pharmaceutical formulation of claim 5, wherein the salt of said compound of a preceding claim is a pharmaceutically acceptable salt.

8. A method of killing and/or preventing the growth of a protozoa, comprising:

contacting the protozoa with an effective amount of the compound of the invention, thereby killing and/or preventing the growth of the protozoa.

10. The method of claim 8, wherein the protozoa is a member selected from the trypanosoma genus and the plasmodium genus.

11. The method of claim 8, wherein the protozoa is Trypanosoma brucei.

12. The method of claim 11, wherein the Trypanosoma brucei is a member selected from Trypanosoma brucei brucei, Trypanosoma brucei gambiense and Trypanosoma brucei rhodesiense.

13. The method of claim 8, wherein the protozoa is a member selected from Plasmodium falciparum, Plasmodium vivax, Plasmodium ovale, Plasmodium vivax, Plasmodium malariae and Plasmodium knowlesi.

14. The method of claim 13, wherein the protozoa is Plasmodium falciparum.

15. A method of treating and/or preventing a disease in an animal, comprising:

administering to the animal a therapeutically effective amount of the compound of the invention, thereby treating and/or preventing the disease.

17. The method of claim 15, wherein the disease is African sleeping sickness.

18. The method of claim 15, wherein the disease is malaria.

19. The method of claim 15, wherein the animal is a human.