| 摘要 |
Salts of quinoline derivatives of formula (I) and their solvates are new: Ar = optionally substituted Ph, naphthyl or 5-7C cycloalkdienyl or optionally substituted single or fused ring aromatic heterocyclic group containing 5-12 ring atoms and /- 4 of S, O and N in each ring; R = 1-8C alkyl, 3-7C cycloalkyl, 4-7C cycloalkylalkyl, optionally substituted Ph or Ph(1-6C alkyl), optionally substituted 5-membered heteroaromatic ring comprising /- 4 of O and N, 1-6C hydroxyalkyl, 1-6C aminoalkyl, 1-6C alkylaminoalkyl, di(1-6C alkyl)aminoalkyl, 1-6C acylaminoalkyl, 1- 6C alkoxyalkyl, 1-6C alkylcarbonyl, carboxy, 1-6C alkoxycarbonyl, 1-6C alkoxycarbonyl(1-6C alkyl), aminocarbonyl, 1-6C alkylaminocarbonyl, di(1-6C alkyl)aminocarbonyl, 1-6C haloalkyl or (CH2)p when cyclised onto Ar; p = 2 or 3; R1, R2 = H or 1-6C alkyl, or R1+R2 = (CH2)q-; q = 2-5; R3, R4 = H, 1-6C alkyl, 1-6C alkenyl, aryl, 1-6C alkoxy, OH, halo, NO2, CN, carboxy, carboxamido, sulphonamido, 1-6C alkoxycarbonyl, CF3, acyloxy, phthalimido, NH2, mono- or di- (16C alkyl)amino, -O-(CH2) r-NT2, -O-(CH2) s-OW, hydroxyalkyl, aminoalkyl, mono- or di-alkylaminoalkyl, acylamino, alkylsulphonylamino, aminoacylamino, mono- or di alkylaminoacylamino; or R4 is (CH2)t when cyclised onto R5 as aryl; t = 1-3; n = 1-4 (not drawn in (I)); r, s = 2-4; T = H or 1-6C alkyl or with the adjacent N forms a group of formula (i) or (ii): V, V1 = H or O; u = 0-2; W = H or 1-6C alkyl; R5 = 1-6C alkyl, 3-7C cycloalkyl, 4-7C cycloalkylalkyl, optionally substituted aryl, or optionally substituted single or fused ring aromatic heterocyclic containing 5-12 ring atoms comprising /- 4 of S, O and N in each ring and X = O, S or NCN. (S)-(+)-N-(~a-ethylbenzyl)-3-hydroxy-2-phenyl-4-quinoline carboxamide sodium salt sesquihydrate is specifically claimed. |
