The present invention relates to 3-amido-1,2-benzoisoxazole derivatives and their salts represented by formula 1, processes for preparation and usees thereof. More particularly, it relates to a method for improving its bioavailability introducing amino acid residue to the amine group of a 3-amido-1,2-benzoisoxazole. The compounds according to the present invention are used as an antagonist against Leukotriene-B-4 receptor, an inhibitor or therapeutics of osteoroposis, thus inhibiting osteolysis and stimulating osteogensis.