AR063930A1 - NEW DERIVATIVES OF BENZOTIAZINONA ITS PREPARATION AND USE AS ANTIBACTERIALS - Google Patents

Abstract

This refers to new benzothiazinone derivatives according to the general formula (1), their use as antibacterial agents in the treatment of infectious diseases of mammals caused by bacteria and pharmaceutical compositions comprising them, as well as the methods for its preparation. The new benzothiazinone derivatives are appropriate for the clinical treatment, for example, of tuberculosis (TB) and leprosy caused by microbacteria. Claim 1: A compound of formula (1) in which R1 and R2 are independently selected from NO2, CN, CONR7R8, COOR9, CHO, fluoride, chloride, bromide, iodide, NR7R8, SO2NR7R8, SR9, OCF3, mono-, di or trifluoromethyl; R3 and R4 are independently selected from H, a linear or branched, saturated or unsaturated C1-7 aliphatic radical, a C3-6 cycloalkyl radical, benzyl, SR9 or OR9; R5 and R6 are independently selected from a linear or branched, halogenated or non-halogenated, saturated or unsaturated C1-8 aliphatic radical, a C3-6 cycloalkyl radical or phenyl, or r5 and R6 together represent a radical - (CR92) m- or R5 and R6 together represent the radicals of formulas (2) in which m is 1-4 or R5 and R6 represent bivalent saturated or unsaturated heterocycles containing one or more heteroatoms selected from N, S or O; which are also substituted by (R10) x, where x is 1-4; R7, R8 and R9 are independently selected from H or a linear or branched, halogenated or non-halogenated, saturated or unsaturated C1-7 aliphatic radical, fluoride, chloride, bromide, iodide or phenyl, preferably from mono-, di or trifluoromethyl; R10 is H or a linear or branched aliphatic radical, halogenated or non-halogenated, saturated or unsaturated C1-7, NO2, NR7R8, CN, CONR7R8, COOR9, CHO, fluoride, bromide, iodide, SO2NR7R8, SR9, OR9, benzyl or phenyl, preferably between OCF3 or mono-, di- or trifluoromethyl; or its pharmaceutically acceptable salt, solvate or hydrate.