| 摘要 |
2-(Hetero)aryloxy-3-(oxoalkoxy or oxoalkylthio)-alkanoic acid derivatives (I) are new. Carboxylic acid derivatives of formula (I) are new. R1 = tetrazolyl or -COR; R = OR9, N-bonded 5-membered heteroaryl, -O(CH2)pS(O)kR10 or -NHSO2R11; R9 = H, alkali(ne earth) metal or organic ammonium cation or (all optionally substituted) cycloalkyl, 1-8C alkyl, alkenyl, alkynyl, benzyl or phenyl; k = 0-2; p = 1-4; R10 = T, cycloalkyl, alkenyl, alkynyl or optionally substituted phenyl; T = 1-4C alkyl; R11 = T, alkenyl, alkynyl or cycloalkyl (all optionally substituted by OT, ST and/or Ph); or optionally substituted phenyl; X, Y = CH or N; Z' = N or CR12; R2, R3 = H, OH, NH2, NHT, N(T)2, halo, T', 2-4C alkenyl, 2-4C alkynyl, OT' or ST; T' = T or 1-4C haloalkyl; R12 = H or T; or R2 + R12 or R3 + R12 = group completing a 5- or 6-membered cycloalkane or cycloalkene ring (optionally substituted and optionally having one or more CH2 replaced by O, S, NH or NT); R4, R5 = phenyl or naphthyl (both optionally substituted; or linked together in the ortho position via a direct bond, CH2, CH2CH2CH=CH, O, S, SO2, NH or N(alkyl)); or optionally substituted cycloalkyl; R6 = cycloalkyl, phenyl, naphthyl or 5- or 6-membered heteroaryl (containing 1-3 N and/or one S or O), all optionally substituted; R7, R8 = H or T; W = O or S; alkenyl or alkynyl moieties have 3-6C and cycloalkyl moieties 3-8C. Independent claims are included for: (1) the use of alcohols of formula (IV) as intermediates for endothelin receptor antagonists; (2) the use of a fragment of formula (IV') or (V) as a structural component of endothelin receptor antagonists; and (3) new intermediates of formula (VI). R18, R19 = T; or R18 + R19 = (CH2)3 or (CH2)4 (both optionally substituted by 1-4 Me).
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