| 摘要 |
Heterocyclic derivs. of formula (I) and their salts are new. W = C(R13)Ar1 or C=CHAR1; Y = CO, CS or CH2; Z = NR, O, S or CH2; A = 1-6C alkylene, 3-7C cycloalkylene, phenylene, phenylene(1-6C)alkylene, (1-6C)alkylene-phenylene, phenylene(2-6C)alkyenylene or 5- or 6-membered satd. or unsatd. heterocyclylene contg. 1-2N atoms and opt. mono- or disubstd. by 1-6C alkyl, oxo or thioxo; B = 1-6C alkylene, 2-6C alkenylene, phenylene, phenylene(1-3C)alkylene or (1-3C)alkylene-phenylene; D - CR2R3, NR3 or CH=CR3; E = tetrazolyl, PO(OR8)2, SO3H, SO2NHR9 or COR10; R = H, 1-8C alkyl, 3-8C cycloalkyl or opt. ring-substd. 6-14C aryl or (6-14C)aryl(1-8C)alkyl; R1 = (CH2)pC(NH)NHX or (CH2)pNHX1; p = 0-3; X = H. 1-6C alkyl, 2-7C alkanoyl, 2-7C alkoxycarbonyl, (2-19C)alkanoyloxy(2-7C)alkoxycarbonyl, PO(OR8)2, CN, OH, 1-6C alkoxy, NH2 or opt. ring-substd. 7-15C aroyl, 7-15C aryloxycarbonyl, (6-14C)aryl(2-7C)alkoxycarbonyl or (6-14C)aryl(1-6C)alkoxy; X1 = X or C(NR")NHR'; R' and R" = gps. as defined for X; R2 = H, 1-8C alkyl, 3-8C cycloalkyl or opt. ring-substd. 6-14C aryl or (6-14C)aryl)1-8C)alkyl; R3 = H, 1-8C alkyl, opt. ring-substd. 6-14C aryl or (6-14C)aryl(1-8C)alkyl, 3-8C cycloalkyl, 2-8C alkenyl, 2-8C alkynyl, 3-9C alkenoyl, 3-9C alkanoyl, pyridyl, NHR11, COR4, COOR4, CON(Me)R14, CONHR14 or SCNHR14; R4 = H or 1-28C alkyl (opt. substd. e.g. by OH, COOH, NH2, aminoacid); R8 = H, 1-18C alkyl or opt. ring-substd. 6-14C aryl or (6-14C)aryl(1-8C)alkyl; R9 = H, CONH2, (1-18C alkyl)carbamoyl, (3-8C cycloalkyl)carbamoyl, 1-18C alkyl, opt. substd. 6-14C aryl or 3-8C cycloalkyl; R10 = OH, 1-18C alkoxy, NH2, mono- or di(1-18C alkyl)amino or opt. ring-substd. (6-14C)aryl(1-8C)alkoxy or 6-14C aryloxy; R11 = H, 1-18C alkyl, COR12, 1-18C alkylsulphonyl, SO2NHR9 or opt. substd. 6-14C arylsulphonyl or (6-14C)aryl(1-8C)alkyl; R12 - H, 1-18C alkyl, 2-8C alkenyl, 2-8C alkynyl, 1-18C alkoxy, NH2, mono- or di(1-18C)alkyl)amino or opt. ring-substd. 6-14C aryl, (6-14C)aryl(1-8C)alkoxy or 6-14C aryloxy; R13 = H, 1-6C alkyl, 3-6C cycloalkyl or opt. ring-substd. (6-14C)aryl(1-8C)alkyl; R14 = H or 1-28C alkyl opt. substd. by R'4, sulpho(1-3C)alkyl, R9NHSO2(1-3C)alkyl, R8O)2PO(1-3C)alkyl and/or tetrazolyl(1-3C)alkyl; b,c,d and f = 0 or 1, but not all 0; e, g and h = 0-6; with provisos. |
