Use of lipoxygenase inhibitors for the preparations of cytoprotective pharmaceutical compostions and process for the preparation of a cytoprotective pharmaceutical composition.

摘要

In the prepn. of a cytoprotective pharmaceutical compsn., a lipoxygenase inhibitor (I) is used. The pref. (I) is of formula (Ia). (X = O, S or NR in the 1 or 3 posn.; R = H, 1-6C alkyl, CN or Ph; Y = O, Se, S, SO, SO2 or NR; thr broken line represents an opt. double bond between the 1 and 2 or 2 and 3 posn.; R1, R2, R3 and R4 = H, 1-6C alkyl, 2-6C alkenyl, (CH2)nM or any 2 may be joined to form a 5-6C ring opt. unsatd.; n = 0-6; M = OR5, halogen, CF3, SR5, opt. substd. Ph, COOR6, COR14, tetrazole, NHCOR7, NR8R9, NHSO2R10, COCH2OH, SOR11, CONR8R9, SO2NR8R9, SO2R3, NO2, OCOR14, OCONR8R9, OCOOR, CN or NR15R16; R5 = H, lower alkoxy-lower alkyl, lower acyloxy-lower alkyl, 1-6C alkyl benzyl or opt. substd. Ph; the Ph substit. here and in R1-R4 is 1-3C alkyl, halogen, CN, CF3, COOR6, CH2COOR6, (CH2)mR8R9 1-3C alkoxy, OH, halo-1-6C alkyl, (CH2)pCOOR6, CN, formyl, perfluoroalkyl or CH2R12; m = 0-2; p = 0-6; R6 = H, Ph or 1-6C alkyl; R12 = 1-5C alkyl, Ph or dimethylamino; R14 = H, (CH2)qCOOR6; 1-6C alkyl, CF3 or Ph opt. substd. as in R5; q = 0-4; R7 = 1-6C alkyl, benzyl or Ph; R8, R9 = H, Ph opt. substd. as in R5, 1-4C alkyl, 1-4C alkylamino alkyl, or may be joined through the N to form a 5-8 membered heterocycloalkyl; R10 = OH, 1-6C alkyl, 1-6C alkoxy, Ph or CF3; R11 = 1-6C alkyl, Ph opt. substd. as in R5, (CH2)5COOR6, CN, formyl or perfluoro 1-4C alkyl; s = 1-6; R13 = OH, H, 1-6C alkyl, Ph opt. substd. as in R5; (CH2)5COOR6, CN or perfluoro 1-4C alkyl; R15, R16 are such that NHR15R16 is an essential amino acid; T = H, halogen of CF3.