New cyclobutyl derivs. as leukotriene-5-B4 antagonists - used to treat contact dermatitis eczema, neuro-dermatitis etc.

摘要

Leukotriene-B4 derivs. of fomrula (I) and (if R5 = H) their salts with physiologically acceptable bases and their cyclodextrin clathrates are new. R1 = CH2OH, Me, CF3, COOR5, CONR6R7 or R1 and R2 together form a carbonyl gp. R2 and R3 = each H or a 1-15C organic acid gp. R4 = H, opt. mono- or poly-substd. 1-4C alkyl, 3-10C cycloalkyl, 6-10C aryl (opt. mono or polysubstd. with gps. chosen from halogen, Ph, 1-4C alkyl, 1-4C alkoxy, fluoromethyl, chloromethyl, CF3, COOH, or OH) or a 5-6 membered heterocyclic ring contg. at lest 1 heteroatom R5 = H, 1-10C alkyl, 3-10C cycloalkyl, 6-10C aryl (opt. substd. with 1-3 halogen, Ph, 1-4C alkyl, 1-4C alkoxy, fluoromethyl, chloromethyl, CF3, COOH or OH gps) CH2CO (6-10C) aryl or 5-6 membered ring contg. at least 1 heteroatoms; A = trans, trans-CH=CH-CH=CH, CH2CH2CH=CH or tetramethylene; B = 1-10C opt. branched alkylene (opt. substd. with F) or (i), D = a direct bond, O, S, -CC-, CH=OR8 or togehter with B also forms a direct bond; R6 and R7 = each H or 1-4C alkyl, or R7 = H and R6 = 1-15C alkanoyl or 1-10C alkane sulphonyl; R8 = H, 1-5C alkyl, Cl or Br; n = 3-5. USE/ADVANTAGE - (I) have antiinflammatory, antiallergic and anti-mycotic properties. They can be used for topical local treatment of contact dermatitis, eczema of various types, neurodermatoses, erythrodermia, pruritis vulvae et ani, Rosacea, erythemanatodes cutaneus psoriasis, lichen rubber planus et verrocosus and similar skin diseases. (I) can also be used as an inhalant in the therapy of allergic diseases of the respiratory system, e.g. bronchial asthma or rhinitis.