The present invention relates to a novel benzoxazine benzimidazole derivative of formula (1) as an antagonist against a vanilloid receptor-1, a pharmaceutical composition comprising the same as an active ingredient, and a use thereof. The benzoxazine benzimidazole derivative of the present invention may be useful for preventing or treating a disease associated with antagonistic activity of vanilloid receptor-1:wherein, R1, R2, R3, R3, Q1, Q2, Q3 and Q4 have same meanings as defined in the specification.