Details for Patent: 8,080,562

Title:	Crystalline pharmaceutical and methods of preparation and use thereof
Abstract:	Novel crystalline polymorphic forms, Forms A, B, C, D, and E of a compound of Formula I, which has been found to be a potent inhibitor of LFA-1, are disclosed. Methods of preparation and uses thereof in the treatment of LFA-1 mediated diseases are also disclosed in this invention. ##STR00001##
Inventor(s):	Burnier; John (Pacifica, CA), Gadek; Thomas (Oakland, CA), Naud; Frederic (Binningen, CH)
Assignee:	Sarcode Bioscience Inc. (Brisbane, CA)
Filing Date:	Apr 15, 2009
Application Number:	12/386,361
Claims:	1. A compound of the formula: ##STR00028## or its pharmaceutically acceptable salts. 2. A compound of the formula: ##STR00029## or its pharmaceutically acceptable salts. 3. A compound of the formula: ##STR00030## 4. A compound of the formula: ##STR00031## or its pharmaceutically acceptable salts. 5. A reaction mixture comprising the compound of claim 1 or 2, a solvent, and a coupling reagent. 6. The reaction mixture of claim 5 further comprising a base. 7. The reaction mixture of claim 6 comprising the compound of ##STR00032## or its pharmaceutically acceptable salts. 8. The reaction mixture of claim 7 wherein a compound of the formula: ##STR00033## is produced. 9. The reaction mixture of claim 5 wherein the solvent is DMF. 10. The reaction mixture of claim 5 wherein the coupling reagent is 2-(7-Aza-1H-benzotriazole-1-yl)-1,1,3,3-tetramethyluronium hexafluorophosphate (HATU). 11. The reaction mixture of claim of claim 6 wherein the base is triethylamine. 12. A compound of the formula: ##STR00034## 13. A reaction mixture comprising the compound of claim 4, a solvent, and an acid. 14. The reaction mixture of claim 4 wherein a compound of the formula: ##STR00035## is produced. 15. The reaction mixture of claim 13 wherein the solvent is dioxane. 16. The reaction mixture of claim 13 wherein the acid is HCl. 17. A reaction mixture comprising the compound of claim 12, a solvent, and a base. 18. The reaction mixture of claim 17 further comprising benzofuranoyl chloride. 19. The reaction mixture of claim 18 wherein a compound of the formula: ##STR00036## is produced. 20. The reaction mixture of claim 17 wherein the solvent is methylene chloride. 21. The reaction mixture of claim 17 wherein the base is diisopropylethylamine.