SUBSTITUTED CAMPTOTHECIN DERIVATIVES AND PROCESS F

专利名称：SUBSTITUTED CAMPTOTHECIN

DERIVATIVES AND PROCESS FOR THEIRPREPARATION

发明人：CABRI, Walter,CANDIANI, Ilaria,BEDESCHI,

Angelo,ZARINI, Franco,PENCO, Sergio

申请号：EP96919763.0申请日：19960510公开号：EP0777670A1公开日：19970611

摘要：The present invention relates to substituted camptothecin derivative (I) whereinsymbols ----represent singly-bound or double bond; () or (two) R1, R2 and R3 such asdefined below is as follows: (one) R1 and R2 are each independently hydrogen; C1-C4alkyl; C3-C7 naphthenic base; Phenyl C1-C6 alkyl; The phenyl ring optionally replaced;Wherein one of R5 and R6 are hydrogen, C1-C6 alkyl or benzyls, the other is hydrogento-NR5R6; C1-C6 alkanoyls, the C1-C6 alkoxy carbonyl groups optionally replaced, thebenzoyl arbitrarily replaced; phenyl C1-C6 alkanoyls; the C1-C6 alkoxy carbonyl groupsoptionally replaced, the phenyloxycarbonyl arbitrarily replaced or phenyl C1-C6 alkoxycarbonyls, or-NR5R60 and-NR5R61; it is combined together; nitrogen-atoms connectedto them links together, composition-NR5R62 Yuans saturation, the miscellaneousmonocyclic residue arbitrarily replaced; COOR8, wherein R8 is hydrogen, C1-C6 alkyl, C3-C7 naphthenic base or phenyl C1-C6 alkyl; Or wherein Rg is C1-C6 alkyl, C3-C7 naphthenicbase, phenyl C1-C6 alkyl to COR9, the phenyl ring or NR10R11 optionally replaced,wherein R10 and R11 is each independently hydrogen or C1-C6 alkyl; R3 is hydrogen, C1-

C6 alkyl or the phenyl ring optionally replaced; Or (and) R1 R3 b, combine, to form 5-8members, the carbomonocyclic rings arbitrarily replaced; R2 is hydrogen, C1-C4 alkyl orC3-C7 naphthenic base; R4 is hydrogen, C1-C6 alkyl, C3-C7 naphthenic base or phenyl C1-C6 alkyl; X is hydrogen, C1-C6 alkyl, C3-C7 naphthenic base, C1-C6 alkoxies, C3-C7cycloalkyloxies, C1-C6, alkanoyloxy, benzoyloxy, amino, hydroxyl, nitro, halogen or it bethat methylene-dioxy is linked on the molecule of position 10 and 11 and itspharmaceutically acceptable salt. The compounds of this invention can be used asantitumor agent.

申请人：PHARMACIA & UPJOHN S.p.A.

地址：Via Robert Koch, 1.2 20152 Milano IT

国籍：IT

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