Triazaspiro[5.5]undecane derivatives, quaternary ammonium salts thereof, N-oxides thereof, non-toxic salts thereof, or pharmaceutical compositions comprising them, as an active ingredient. ##STR00001## So the compounds of the formula (I) regulate the effect of chemokine/chemokine receptor, they are used for prevention and treatment of various inflammatory diseases, asthma, atopic dermatitis, urticaria, allergic diseases, nephritis, nephropathy, hepatitis, arthritis or rheumatoid arthritis etc.

Ono Pharmaceutical Co., Ltd.

Triazaspiro[5.5]undecane derivatives and pharmaceutical compositions comprising thereof, as an active ingredient

Triazaspiro[5.5]undecane derivatives of the formula (I), quaternary ammonium salts thereof, N-oxides thereof, non-toxic salts thereof, or pharmaceutical compositions comprising them, as active ingredients (wherein R.sup.1 is formula (II) or formula (III); R.sup.2 is alkyl or alkynyl etc.; R.sup.3, R.sup.4 is H, (substituted) alkyl etc., or R.sup.3 and R.sup.4 together to form formula (IV); R.sup.5 is H or alkyl). ##STR00001## Therefore the compounds of the formula (I) regulate the effect of chemokine/chemokine receptor, they are used for prevention and treatment of various inflammatory diseases, asthma, atopic dermatitis, urticaria, allergic diseases, nephritis, nephropathy, hepatitis, arthritis or rheumatoid arthritis etc.

Triazaspiro[5.5]undecane derivative and pharmaceutical composition comprising the same as active ingredient

Triazaspiro[5.5]undecane derivatives and drugs containing the same as the active ingredient

The present invention relates to a new crystal of triazaspiro[5.5]undecane derivatives. The crystal of a non-solvate of (3R)-1-butyl-2,5-dioxo-3-[(1R)-1-hydroxy-1-cyclohexylmethyl]-9-[4-(4-carb- oxyphenyloxy)phenylmethyl]-1,4,9-triazaspiro[5.5]undecane hydrochloride have safety as drug substance, and have possibility to supply at large scale. And the crystal have an antagonistic activity against the interaction between chemokine and chemokine receptor, therefore, it is useful for manufacture of an agent for treating and/or preventing diseases such as various inflammatory diseases, asthma, atopic dermatitis, nettle rash, allergy disease, nephritis, nephropathy, hepatitis, arthritis, chronic rheumatoid arthritis, autoimmune disease, transplanted organ rejection reactions, acquired immunodeficiency syndrome and the like.

undecane/hepatitas

Triazaspiro[5.5]undecane derivatives and pharmaceutical compositions comprising thereof, as an active ingredient

Triazaspiro[5.5]undecane derivative and pharmaceutical composition comprising the same as active ingredient

Triazaspiro[5.5]undecane derivatives and drugs containing the same as the active ingredient

Crystals of triazaspiro[5.5]undecane derivative

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