Drug compsn. contg. 3(5)-(hydroxyaryl)-pyrazole derivs. - for inhibition of lipoxygenase and cyclo:oxygenase in treatment of asthma, allergy, inflammation, skin disorders, myocardial infarction etc.

摘要

A drug compsn. contg. 3(5)-(hydroxyaryl)-pyrazole derivs. (I) is claimed. Ar = opt. susbtd. 2-hydroxyphenyl; R = H, alkyl or opt. substd. phenyl or naphthyl; and R1 = H, alkyl or cycloalkyl; or R+R1 = 3-5C alkylene. Certain cpds. (I) are known from DE856297, DE931284, DE932909, GB707669, J. Chem.Soc. 1952, 1303 and J.Indian Chem.Soc. 65,852(1988), whereas others are new. Pref. opt. substits. on 2-hydroxyphenyl include alkyl, alkoxy, haloalkyl, CF3, F, Cl, Br, CN, NO2, OH, 3-6C alkylene or a fused benzene ring, and opt. substits. on phenyl or naphthyl include alkyl, alkoxy, CF3, F, Cl, Br, CN, NO2 and OH. USE/ADVANTAGE - Cpds. (I) are dual inhibitors of lipoxygenase and cyclooxygenase used for the treatment and prophylaxis of bronchial asthma, allergies, inflammations, shock states, skin disorders, esp. psoriasis and polymorphic photodermatoses, cerebral ischaemia and myocardial infarction, and for the prevention of rejection in organ transplants. Cpds. (I) readily obtainable and have high activity combined with low toxicity. In partic., they inhibit 5-lipoxygenase in the micromolar range. Cpds. (I) are administered by the oral, parenteral, intraperitoneal or rectal route or topically in conventional pharmaceutical dosage forms. Daily dosage is 0.1-50 mg/kg.