Leukotriene B4 derivs. with a cyclohexane ring - with antiinflammatory, antiallergic, antiproliferative and antimycotic properties for treating e.g. eczema, asthma, colitis

摘要

Leukotriene B4 derivs. of formula (I) and, if R5, their salts, bases, and cyclodextrin clathrates are new: R1 = CH2OH, Me, CF3, COOR5, CONR6R7; or R1 and R2 =C = O; R2, R3 = H or 1-15C organic acid gp.; R4 = H, opt. mono- or poly-substd. 1-14C alkyl, 3-10C alkyl, etc.; R5 = H, 1-10C alkyl, 3-10C cycloalkyl etc.; A = trans, trans-CH=CH-CH=CH etc.; B = 1-10C opt. branched alkylene (opt. substd. with F) or a gp. of formula (a) or (b); D = a direct bond, O, S, C=C, CH=CR8 or together with B also forms a direct bond; R6, R7 = H or 1-4C alkyl; or R7 = H and R6 = 1-15C alkanoyl or 1-10C alkanesulphonyl, opt. substd. with OH; R8 = H, 1-5C alkyl, Cl or Br; n = 2-5. USE - (I) are LTB4 antagonists and have antiinflammatory, antiallergic, antiproliferative and antimycotic properties. (I) are esp. useful for topical local treatment of skin diseases, such as contact dermatitis, various forms of eczema etc.. (I) are also suitable for use as inhalants in the treatment of respiratory disorders such as bronchial asthma and rhinitis etc. and can be used orally or rectally for the treatment of allergic disorders of the gastro intestinal tract, e.g. colitis ulcerosa, etc.. (I) can be used to treat diseases in which leukotrienes cause increased growth and prodn. of cells, e.g. leukaemia etc., and atherosclerosis (increased growth of smooth muscle cells of blood vessels).