Camptothecin analogues, process for their preparat

专利名称：Camptothecin analogues, process for their

preparation and pharmaceuticalcompositions containing them

发明人：LAVIELLE, GILBERT,HAUTEFAYE,

PATRICK,PIERRE, ALAIN,ATASSI,GHANEM,HICKMAN, JOHN,CIMETIERE,BERNARD

申请号：EP00403108.4申请日：20001109公开号：EP1101765A2公开日：20010523

摘要：Camptothecin analogs (I), their enantiomers, diastereoisomers, and salts withacids and bases are new. Camptothecin analogs of formula (I), their enantiomers,diastereoisomers, and salts are new. n = 0-2; R1-R5 = H, halogen, alkyl, alkenyl, alkynyl,perhaloalkyl, 3-11C cycloalkyl, 3-11C cycloalkyl-alkyl, OH, hydroxyalkyl, alkoxy,

alkoxyalkyl, alkoxycarbonyl, acyloxy, NO2, CN, aminocarbonyl (optionally substituted onthe N by one or two alkyl groups), -(CH2)p-NRaRb, or -O-CO- NRaRb; or two adjacentgroups of R2-R5 = -O-(CH2)t-O-; p = 0 - 6; Ra, Rb = H, alkyl, 3-11C cycloalkyl, 3-11Ccycloalkyl-alkyl, acyl, optionally substituted aryl or optionally substituted arylalkyl; orNRaRb = pyrrolyl, piperidinyl, or piperazinyl each of the cyclic groups being optionallysubstituted; t = 1-3; R60, R70n, R80, and R90 = H, OH, alkoxy, or -O-CO-X or -O-CO-NXW;X, W = alkyl, alkenyl, alkynyl, 3-11C cycloalkyl, 3-11C cycloalkyl-alkyl, optionallysubstituted aryl, or optionally substituted aryl alkyl; R61, R71n, R81, and R91 = H, alkyl,

alkenyl or alkynyl; or vicinal pairs may together form a bond or an oxirane group; orR60+R61, R70n+R71n, R80+R81n and/or R90+R91 = oxo or -O-(CH2)t1-O-; t1 = 1-3 withthe proviso that R60, R70n, R80, R90, R61, R71n, R81, and R91 are not all H. Alkyl, alkoxyand acyl groups have 1-6C; alkenyl have 2-6C and 1-3 double bonds; alkynyl have 2-6Cand 1-3 triple bonds; aryl = phenyl or naphthyl; 'substituted' on aryl or aryl alkyl groupsmeans by one or more halogens, alkyl, alkoxy, OH, CN, NO2, amino or mono- ordialkylamino groups; 'substituted' on heterocyclic groups means by one or more alkyl,alkoxy, aryl, aryl alkyl, aryloxy and/or aryloxy alkyl groups. An Independent claim isincluded for the preparation of (I).

申请人：LES LABORATOIRES SERVIER

地址：1 rue Carle Hébert 92415 Courbevoie Cédex FR

国籍：FR

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