BORON-CONTAINING SMALL MOLECULES

摘要

598441 Disclosed are 1,3-dihydro-1-hydroxy-2,1-benzoxaborole derivatives as represented by the general formula (I), wherein R1b and R7b are hydrogen, and R11b and R10b are as defined herein; and wherein the compounds are 5-(4-cyanophenoxy)-1,3-dihydro-1-hydroxy-2,1-benzoxaborole, 6-(4-cyanophenoxy)-1,3-dihydro-1-hydroxy-2,1-benzoxaborole, 6-(3-cyanophenoxy)-1,3-dihydro-1-hydroxy-2,2-benzoxaborole, 6-(4-chlorophenoxy)-1,3-dihydro-1-hydroxy-2,1-benzoxaborole, 5-(4-cyanobenzyloxy)-1,3-dihydro-1-hydroxy-2,1-benzoxaborole, 5-(2-cyanophenoxy)-1,3-dihydro-1-hydroxy-2,1-benzoxaborole, 5-[4-(N,N-diethylcamamoyl)phenoxy]-1,3-dihydro-1-hydroxy-2,1-benzoxaborole, 1,3-dihydro-1-hydroxy-5-[4-(morpholinocarbonyl)phenoxy]-2,1-benzoxaborole, 5-(3,4-dicyanophenoxy)-1,3-dihydro-1-hydroxy-2,1-benzoxaborole, 6-phenylthio-1,3-dihydro-1-hydroxy-2,1-benzoxaborole, 6-(4-trifluoromethoxyphenoxy)-1,3-dihydro-1-hydroxy-2,1-benzoxaborole, 6-(4-methoxyphenoxy)-1,3-dihydro-1-hydroxy-2,1-benzoxaborole, 6-(4-methoxyphenyithio)-1,3-dihydro-1-hydroxy-2,1-benzoxaborole, 5-(3-cyanophenoxy)-1,3-dihydro-1-hydroxy-2,1-benzoxaborole, 5-(4-carboxyphenoxy)-1-hydroxy-2,1-benzoxaborole, and 1-hydroxy-5-[4-(tetrazole-1-yl)phenoxy]-2,1-benzoxaborole. Further disclosed is a pharmaceutical formulation comprising a compound as defined above and a pharmaceutically acceptable excipient, for the treatment of inflammation, and wherein said formulation may be formulated for administration to a site which is skin, nail, hair or skin surrounding the nail or hair.