COMBINATION

• US 20080146643A1
• Filed: 12/13/2007
• Published: 06/19/2008
• Est. Priority Date: 06/15/2005
• Status: Abandoned Application

• Current Assignee: Pfizer Limited (Pfizer Inc.)
• Original Assignee: Pfizer Limited (Pfizer Inc.)
• Inventors: Gethin, David Morris, Kyne, Graham Michael, Critcher, Douglas James, Billen, Denis, Hall, Kim Thomas, Boyle, Jessica
• Application Number:
  US11/955,860
• Publication Number:
  US 20080146643A1
• Time in Patent Office: Days
• US Class Current: 514/407
• CPC Class Codes: A61K 2300/00 Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
• CPC Class Codes: A61K 31/415 1,2-Diazoles
• CPC Class Codes: A61K 45/06 Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• CPC Class Codes: A61P 33/00 Antiparasitic agents
• CPC Class Codes: C07D 231/38 Nitrogen atoms nitro radicals C07D231/16
• CPC Class Codes: C07D 231/40 Acylated on said nitrogen atom

Abstract

Compounds of formula (I) are used in combination with a second antiparasitic agent for the treatment of parasitic infestations in a host animal.

Claims

1. A method of treating a parasitic infestation in a host animal, comprising simultaneously, sequentially or separately administering to said host animal:

a) a therapeutically effective amount of a compound of formula (I)

2. The method according to claim 1 wherein the second antiparasitic agent is an anthelmintic agent.

3. The method according to claim 2 wherein the anthelmintic agent is a macrocyclic lactone.

4. The method according to claim 3 wherein the macrocyclic lactone anthelmintic agent is a milbemycin or a derivative thereof.

5. The method according to claim 4 wherein the milbemycin or derivative thereof is milbemycin oxime.

6. A compound of formula I in the method according to claim 1 which is

cyclopropylmethyl {4-[1-(aminocarbonyl)cyclopropyl]-3-cyano-1-[2,6-dichloro-4-pentafluorothiophenyl]-1H-pyrazol-5-yl}carbamate;

1-{5-amino-3-cyano-1-[2,6-dichloro-4-pentafluorothiophenyl]-1H-pyrazol-4-yl}-cyclopropanecarboxamide;

1-{3-cyano-1-[2,6-dichloro-4-pentafluorothiophenyl]-5-[(2-fluoroethyl)amino]-1H-pyrazol-4-yl}cyclopropanecarboxamide;

1-{5-amino-3-cyano-1-[2,6-dichloro-4-pentafluorothiophenyl]-1H-pyrazol-4-yl}-2,2-dichlorocyclopropanecarboxamide;

isopropyl {4-[1-(aminocarbonyl)cyclopropyl]-3-cyano-1-[2,6-dichloro-4-pentafluorothiophenyl]-1H-pyrazol-5-yl}carbamate;

1-{3-cyano-1-[2,6-dichloro-4-pentafluorothiophenyl]-5-(methylamino)-1H-pyrazol-4-yl}-2,2-difluorocyclopropanecarboxamide;

1-{5-amino-3-cyano-1-[2,6-dichloro-4-pentafluorothiophenyl]-1H-pyrazol-4-yl}-2,2-difluorocyclopropanecarboxamide;

1-[3-cyano-1-[2,6-dichloro-4-pentafluorothiophenyl]-5-(methylamino)-1H-pyrazol-4-yl]cyclopropanecarboxamide; and

ethyl {4-[1-(aminocarbonyl)cyclopropyl]-3-cyano-1-[2,6-dichloro-4-pentafluorothiophenyl]-1H-pyrazol-5-yl}carbamate.

7. The method according to claim 6 wherein the second antiparasitic agent is an anthelmintic agent.

8. The method according to claim 7 wherein the anthelmintic agent is a macrocyclic lactone.

9. The method according to claim 8 wherein the macrocyclic lactone anthelmintic agent is a milbemycin or a derivative thereof.

10. The method according to claim 9 wherein the milbemycin or derivative thereof is milbemycin oxime.

11. The method according to claim 1 which is cyclopropylmethyl {4-[1-(aminocarbonyl)cyclopropyl]-3-cyano-1-[2,6-dichloro-4-pentafluorothiophenyl]-1H-pyrazol-5-yl}carbamate.

12. The method according to claim 1 wherein the host animal is a human.

13. The method according to claim 1 wherein the host animal is a non-human mammal.

14. The method according to claim 13 wherein the non-human mammal is selected from dogs, cats, horses, cattle, sheep and pigs.

15. The method according to claim 1 wherein the compound of formula (I), or pharmaceutically acceptable salt or a prodrug thereof, and the second antiparasitic agent, are administered together in a single pharmaceutical composition.

16. The method according to claim 15 wherein the single pharmaceutical composition is adapted for oral administration.

17. A pharmaceutical composition comprising:

a) a compound of formula (I)

18. The pharmaceutical composition according to claim 17 wherein the second antiparasitic agent is an anthelmintic agent.

19. The pharmaceutical composition according to claim 18 wherein the anthelmintic agent is a macrocyclic lactone.

20. The pharmaceutical composition according to claim 19 wherein the macrocyclic lactone is a milbemycin or a derivative thereof.

21. The pharmaceutical composition according to claim 20 wherein the milbemycin or derivative thereof is milbemycin oxime.

22. The pharmaceutical composition according to claim 17 wherein the compound according to formula (i) is cyclopropylmethyl {4-[1-(aminocarbonyl)cyclopropyl]-3-cyano-1-[2,6-dichloro-4-pentafluorothiophenyl]-1H-pyrazol-5-yl}carbamate.

23. A kit for treating a parasitic infestation in a host animal, comprising:

a) a pharmaceutical composition comprising a therapeutically effective amount of a compound of formula (I)

24. The kit of claim 23 wherein the compound according to formula (i) is cyclopropylmethyl {4-[1-(aminocarbonyl)cyclopropyl]-3-cyano-1-[2,6-dichloro-4-pentafluorothiophenyl]-1H-pyrazol-5-yl}carbamate.