Abstract: The present invention provides compounds of formula (I) and/or salt thereof and/or geometric isomer thereof and/or stereoisomer thereof and/or enantiomer thereof and/or racemate thereof and/or diastereomer thereof and/or biologically active metabolite thereof and/or prodrug thereof and/or solvate thereof and/or hydrate thereof and/or polymorph thereof having affinity and selectivity for the gamma-aminobutyric acid A receptor subunit alpha 5 and act as GABAA ?5 negative allosteric modulators, thereby useful in the treatment or prevention of diseases related to the GABAA ?5 receptor, process for the preparation thereof, pharmaceutical compositions comprising them alone or in combination with one or more other active ingredients and their use as medicaments.

Abstract: The invention relates to new N-hydroxy-4-(3-phenyl-5-methyl-isoxazole-4-yl)-benzenesulfonamide solvates of formula (I). wherein n represents 0 or 1 mol, [solvate] represents water, C1-C4 alcohol, C1-C4 alkylester of C1-C3 carboxylic acid or dioxane, and the mixture of solvated (wherein n=1) and solvat-free forms (wherein n=0). Furthermore, the invention relates their process for production and use for the treatment of osteoarthritis and rheumatoid arthritis and surgical and primary dysmenorrheal pains, based on anti-inflammatory and analgesic pharmacological model experiments.