ANTIPARASITIC AGENTS

التفاصيل البيبلوغرافية
العنوان: ANTIPARASITIC AGENTS
Document Number: 20080194694
تاريخ النشر: August 14, 2008
Appl. No: 12/028192
Application Filed: February 08, 2008
مستخلص: The present invention relates to compounds of the formula (I) [chemical expression included] or a tautomer or prodrug thereof, or a pharmaceutically acceptable salt of said compound, tautomer or prodrug, wherein: R1, R2, R3, R4 and R5 are each independently selected from H, halo, CN, CF3 and CONH2; compositions containing such compounds and the uses of such compounds as antiparasitic agents.
Inventors: Comlay, Stuart Nicholas (Sandwich, GB); Hannam, Joanne Clare (Sandwich, GB); Howson, William (Sandwich, GB); Lauret, Christelle (Sandwich, GB); Sabnis, Yogesh Anil (Sandwich, GB)
Assignees: PFIZER LIMITED (Sandwich, UK)
Claim: 1. A compound of the formula [chemical expression included] or a tautomer or prodrug thereof, or a pharmaceutically acceptable salt of said compound, tautomer or prodrug, wherein: R1, R2, R3, R4 and R5 are each independently selected from H, halo, CN, CF3 and CONH2.
Claim: 2. A compound according to claim 1 wherein R1, R2, R3, R4 and R5 are each independently selected from H, F, Cl, Br, CN and CF3.
Claim: 3. A compound according to claim 2 wherein at least one of R1,R2, R3, R4 and R5 is CN and at least two of R1, R2, R3, R4 and R5 are H.
Claim: 4. A compound according to claim 2 wherein R1 and R4 are H, one of R2 and R3 is H and the other is CN, and R5 is selected from F, Cl, Br and CF3.
Claim: 5. A compound according to claim 4 wherein R3 is CN and R5 is CF3.
Claim: 6. A compound according to claim 1 selected from: N-{1-cyano-2-[5-cyano-2-(trifluoromethyl)phenoxy]-1-methylethyl}-4-pentafluorothiobenzamide, N-{(1R)-1-cyano-2-[5-cyano-2-(trifluoromethyl)phenoxy]-1-methylethyl}-4-pentafluorothiobenzamide, N-{(1S)-1-cyano-2-[5-cyano-2-(trifluoromethyl)phenoxy]-1-methylethyl}-4-pentafluorothiobenzamide, N-[2-(2-chloro-5-cyanophenoxy)-1-cyano-1-methylethyl]-4-pentafluorothiobenzamide, N-[2-(2-chloro-5-cyanophenoxy)-(1R)-1-cyano-1-methylethyl]-4-pentafluorothiobenzamide, N-[2-(2-chloro-5-cyanophenoxy)-(1S)-1-cyano-1-methylethyl]-4-pentafluorothiobenzamide, N-{1-cyano-2-[4-cyano-2-(trifluoromethyl)phenoxy]-1-methylethyl}-4-pentafluorothiobenzamide, N-{(1R)-1-cyano-2-[4-cyano-2-(trifluoromethyl)phenoxy]-1-methylethyl}-4-pentafluorothiobenzamide, N-{(1S)-1-cyano-2-[4-cyano-2-(trifluoromethyl)phenoxy]-1-methylethyl}-4-pentafluorothiobenzamide, N-{2-[2-chloro-5-cyano-3-(trifluoromethyl)phenoxy]-1-cyano-1-methylethyl}-4-pentafluorothiobenzamide, N-{2-[2-chloro-5-cyano-3-(trifluoromethyl)phenoxy]-(1R)-1-cyano-1-methylethyl}-4-pentafluorothiobenzamide, N-{2-[2-chloro-5-cyano-3-(trifluoromethyl)phenoxy]-(1S)-1-cyano-1-methylethyl}-4-pentafluorothiobenzamide, N-[2-(2-chloro-4,5-dicyanophenoxy)-1-cyano-1-methylethyl]-4-pentafluorothiobenzamide, N-[2-(2-chloro-4,5-dicyanophenoxy)-(1R)-1-cyano-1-methylethyl]-4-pentafluorothiobenzamide, N-[2-(2-chloro-4,5-dicyanophenoxy)-(1S)-1-cyano-1-methylethyl]-4-pentafluorothiobenzamide, N-(1-cyano-2-[4-cyano-2-(trifluoromethyl)phenoxy]-1-methylethyl)-4-pentafluorothiobenzamide, N-{(1R)-1-cyano-2-[4-cyano-2-(trifluoromethyl)phenoxy]-1-methylethyl}-4-pentafluorothiobenzamide, and N-{(1S)-1-cyano-2-[4-cyano-2-(trifluoromethyl)phenoxy]-1-methylethyl}-4-pentafluorothiobenzamide, or a pharmaceutically acceptable salt thereof.
Claim: 7. A pharmaceutical composition comprising a compound of formula (I) of claim 1, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier.
Claim: 8. The pharmaceutical composition according to claim 7 further comprising a second therapeutic agent.
Claim: 9. The pharmaceutical composition according to claim 8 wherein the second therapeutic agent is selected from ivermectin, avermectin, abamectin, emamectin, eprinomectin, doramectin, selamectin, moxidectin, nemadectin, milbemycin oxime, albendazole, cambendazole, fenbendazole, flubendazole, mebendazole, oxfendazole, oxibendazole, parbendazole, tetramisole, levamisole, pyrantel pamoate, oxantel, morantel, closantel, triclabendazole, clorsulon, rafoxanide, niclosamide, praziquantel, epsiprantel, 2-desoxoparaherquamide, fipronil, pyriprole, pyrafluprole, lufenuron, spiromesifen, tebufenozide, tebufenozide, spinosad, spinetoram, imidacloprid, dinotefuran, metaflumizone, flubendiamide, chlorantraniliprole, indoxacarb, pyridalyl, pyrimidifen and pyrifluquinazon.
Claim: 10. A method of treatment of a parasitic infestation in a host animal, comprising treating said host animal with an effective amount of a compound of formula (I), or with a pharmaceutically acceptable salt or composition thereof, as defined in claim 1.
Claim: 11. The method according to claim 10 wherein the host animal is a non-human animal.
Claim: 12. The method according to claim 10 wherein the parasite is a nematode.
Current U.S. Class: 514/618
Current International Class: 61; 07; 61
رقم الانضمام: edspap.20080194694
قاعدة البيانات: USPTO Patent Applications