Claims for Patent: 8,283,369

Summary for Patent: 8,283,369

Title:	Compounds and compositions and methods of use
Abstract:	Described herein are compounds useful in the modulation of blood uric acid levels, formulations containing them and methods of using them. In some embodiments, the compounds described herein are used in the treatment or prevention of disorders related to aberrant levels of uric acid.
Inventor(s):	Quart; Barry D. (Encinitas, CA), Girardet; Jean-Luc (San Diego, CA), Gunic; Esmir (San Diego, CA), Yeh; Li-Tain (Irvine, CA)
Assignee:	Ardea Biosciences. Inc. (San Diego, CA)
Application Number:	13/174,522
Patent Claims:	1. A method of treating gout in a human, the method comprising administering to the human a compound of formula (III): ##STR00173## wherein X is N; W is S or O; R.sup.1 is Cl, Br, I, optionally substituted methyl, CF.sub.3, CHF.sub.2 or CH.sub.2F; R.sup.3 and R.sup.3' are independently selected from H and lower alkyl; R.sup.2 is: ##STR00174## wherein represents a carbon-carbon double bond; R.sup.P is cyclopropyl; R.sup.8, R.sup.9 and R.sup.10 are H or a pharmaceutically acceptable salt, ester, or tautomer thereof. 2. The method of claim 1, wherein W is S. 3. The method of claim 1, wherein R.sup.3 and R.sup.3' are H. 4. The method of claim 2, wherein R.sup.3 and R.sup.3' are H. 5. The method of claim 1, wherein R.sup.1 is Br. 6. The method of claim 4, wherein R.sup.1 is Br. 7. The method of claim 1, wherein a compound of formula (IV): ##STR00175## or a pharmaceutically acceptable salt, ester, or tautomer thereof, is administered to the human. 8. The method of claim 1, wherein the pharmaceutically acceptable salt is administered to the human, and wherein the pharmaceutically acceptable salt is an ammonium, a primary amine, a secondary amine, a tertiary amine, a lithium, a sodium, a potassium, a calcium, a magnesium, or an aluminum salt. 9. The method of claim 8, wherein the pharmaceutically acceptable salt is a sodium salt. 10. The method of claim 1, wherein said administering is orally. 11. The method of claim 1, wherein said compound is administered in combination with a pharmaceutically acceptable carrier, excipient, or diluent, in a pharmaceutical composition. 12. The method of claim 11, wherein the pharmaceutical composition is a tablet or capsule. 13. The method of claim 12, wherein the pharmaceutical composition is a tablet. 14. The method of claim 13, wherein the pharmaceutical composition is a coated tablet. 15. The method of claim 13, wherein the tablet comprises lactose. 16. The method of claim 13, wherein the tablet comprises microcrystalline cellulose. 17. The method of claim 13, wherein the tablet comprises sodium croscarmellose. 18. The method of claim 12, wherein the tablet or capsule comprises gelatin. 19. The method of claim 13, wherein the tablet comprises magnesium stearate. 20. The method of claim 13, wherein the tablet comprises hydroxypropylcellulose or hydroxypropylmethyl-cellulose. 21. The method of claim 1, further comprising administering to the human a second agent effective for treatment of gout. 22. The method of claim 21, wherein the second agent is a URAT 1 inhibitor, a xanthine oxidase inhibitor, a xanthine dehydrogenase, a xanthine oxidoreductase inhibitor, or a combination thereof. 23. The method of claim 22, wherein the second agent is allopurinol, febuxostat, FYX-051, or a combination thereof. 24. The method of claim 23, wherein the second agent is allopurinol. 25. A method of treating gout in a human, the method comprising administering to the human a compound of formula (IV): ##STR00176## 26. A method of achieving a therapeutic benefit in a human with gout, the method comprising administering to the human a compound of formula (III): ##STR00177## wherein X is N; W is S or O; R.sup.1 is Cl, Br, I, optionally substituted methyl, CF.sub.3, CHF.sub.2 or CH.sub.2F; R.sup.3 and R.sup.3' are independently selected from H and lower alkyl; R.sup.2 is: ##STR00178## wherein represents a carbon-carbon double bond; R.sup.P is cyclopropyl; R.sup.8, R.sup.9 and R.sup.10 are H or a pharmaceutically acceptable salt, ester, or tautomer thereof. 27. The method of claim 26, wherein W is S. 28. The method of claim 26, wherein R.sup.3 and R.sup.3' are H. 29. The method of claim 27, wherein R.sup.3 and R.sup.3' are H. 30. The method of claim 26, wherein R.sup.1 is Br. 31. The method of claim 29, wherein R.sup.1 is Br. 32. The method of claim 26, wherein a compound of formula (IV): ##STR00179## or a pharmaceutically acceptable salt, ester, or tautomer thereof, is administered to the human. 33. The method of claim 26, wherein the pharmaceutically acceptable salt is administered to the human, and wherein the pharmaceutically acceptable salt is an ammonium, a primary amine, a secondary amine, a tertiary amine, a lithium, a sodium, a potassium, a calcium, a magnesium, or an aluminum salt. 34. The method of claim 33, wherein the pharmaceutically acceptable salt is a sodium salt. 35. The method of claim 26, wherein said administering is orally. 36. The method of claim 26, wherein said compound is administered in combination with a pharmaceutically acceptable carrier, excipient, or diluent, in a pharmaceutical composition. 37. The method of claim 36, wherein the pharmaceutical composition is a tablet or capsule. 38. The method of claim 37, wherein the pharmaceutical composition is a tablet. 39. The method of claim 38, wherein the pharmaceutical composition is a coated tablet. 40. The method of claim 38, wherein the tablet comprises lactose. 41. The method of claim 38, wherein the tablet comprises microcrystalline cellulose. 42. The method of claim 38, wherein the tablet comprises sodium croscarmellose. 43. The method of claim 37, wherein the tablet or capsule comprises gelatin. 44. The method of claim 38, wherein the tablet comprises magnesium stearate. 45. The method of claim 38, wherein the tablet comprises hydroxypropylcellulose or hydroxypropylmethyl-cellulose. 46. The method of claim 26, further comprising administering to the human a second agent effective for treatment of gout. 47. The method of claim 46, wherein the second agent is a URAT 1 inhibitor, a xanthine oxidase inhibitor, a xanthine dehydrogenase, a xanthine oxidoreductase inhibitor, or a combination thereof. 48. The method of claim 47, wherein the second agent is allopurinol, febuxostat, FYX-051, or a combination thereof. 49. The method of claim 48, wherein the second agent is allopurinol. 50. A method of achieving a therapeutic benefit in a human with gout, the method comprising administering to the human a compound of formula (IV): ##STR00180##