| abstract |
THEY REFER TO COMPOUNDS OF FORMULA (I), WHERE: "Q" IS A REST HETEROCICLO; "Z" IS N or -CH =; R1 AND R2 ARE H, OY, WHERE "Y" IS AN EASILY HYDROLYSABLE GROUP LIKE -COR5 or -OP (R6O) 2; R3 AND R4 ARE H, HALOGEN, LOWER ALKYL, LOWER ALKOXYL, LOWER ALKYL, (LOWER ALKYL CARBONYL) THYOMETHYL, CARBOXYL or METOXYCARBONYL; R5 IS H, LOWER ALCOXYL, LOWER ALKYL; R6 IS H or LOWER ALKYL; X- IT IS A PHARMACEUTICALLY ACCEPTABLE ANION. A PREFERRED COMPOUND (I) IS THE SALT OF HYDROCHLORIC ACID OF BROMIDE OF 1 - [(2R, 3R) -3- [4- (4-CIANO-FENIL) -TIAZOL-2-IL] -2- (2,4 -DIFLUORO-PHENYL) -2-HYDROXY-BUTYL] -4- (3,5-DIMETHYL-4-METHYLAMINOACETOXY-BENCIL] -1H- [1,2,4] TRIAZOL-4-ILO. IT ALSO REFERS TO THE PROCEDURE OF PREPARATION OF (I), WHICH INCLUDES: REACTING A COMPOUND THAT POSSESSES ANTIFUNGAL ACTIVITY OF FORMULA (II) WITH A COMPOUND OF FORMULA (III), WHERE: R1 AND R2 ARE OH; FOLLOWED BY THE REACTION OF THE RESULTING COMPOUND WITH R5COL or (R6O) 2POL, WHERE: R5CO IS AN ACID WASTE OF A PROTECTED AMINO ACID; "L" IS A GROUP OF LOSS. THE COMPOUNDS OF FORMULA (I) ARE SOLUBLE IN WATER SO THAT THEIR FORMULATION IS FACILITATED, BEING USEFUL FOR TOPICAL AND SYSTEMIC TREATMENT OF MYCOSIS IN ANIMALS AS WELL AS IN HUMANS |