| 摘要 |
Macrocyclic hydroxamic acid derivatives (I), their salts, diastereoisomeric forms and mixtures are new. Macrocyclic hydroxamic acid derivatives of formula (I), their salts, diastereoisomeric forms and mixtures are new. Y = -CH2-, -CH2-CH2-, or -CH=CH-; Z and Z' = -CH2-, or Y-Z or Y-Z' are -CH=CH- ; X = -CH2-, -O- or -S-; R1 = phenyl (optionally substituted by OH, benzyloxy, halo, NH2, mono or dialkylamino, acylamino, or NO2), 5 or 6 membered cycloalkyl, 5-10 membered mono- or bicyclic saturated or unsaturated heterocyclyl that contains 1-3 heteroatoms (O, N, S), (optionally substituted by OH, benzyloxy, halo, NH2, mono or dialkylamino, acylamino, or NO2), and may contain N-oxide, alkyl (optionally substituted by alkyloxycarbonyl, NH2, mono or dialkylamino, alkyloxy carbonyl amino, benzyloxy carbonyl amino, OH, alkyloxy, alkylthio, alkylsulfinyl, alkylsulfonyl, phenyl (itself optionally substituted by OH, alkyloxy, methylenedioxy, benzyloxy, NH2, mono or dialkylamino, acylamino, or NO2), naphthyl, 5 or 6 membered cycloalkyl, 5-10 membered mono- or bicyclic saturated or unsaturated heterocyclyl that contains 1-3 heteroatoms (O, N, S), (optionally substituted by OH, benzyloxy, halo, NH2, mono or dialkylamino, acylamino, or NO2) and that may contain N-oxide, or benzyloxy); R2 = H, alkyl, or hydroxyalkyl (optionally substituted by NH2, mono or dialkylamino, OH, alkylthio, phenyl, saturated or unsaturated 5 or 6 membered heterocycle optionally containing a second hetero atom (O, N, S), and optionally substituted by alkyl, OH, or halogen; R3 = H, alkyl, alkoxycarbonyl, carbamoyl, alkylcarbamoyl, or dialkylcarbamoyl or R2 and R3 together with the atoms to which they are linked, form a 5- or 6-membered heterocycle which may contain another heteroatom (O, N, S), and which may be substituted by alkyl, hydroxyalkyl or OH; and R4 and R'4 = H, OH, alkyl, hydroxyalkyl, or OH. Independent claims are include for (i) intermediates of formula (II) when R4 and R'4 are different; (ii) preparation of (I) and ; (iii) the use of (I) in pharmaceutical compositions together with suitable diluents and/or adjuvants.
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