申请人:Tanabe Seiyaku Co., Ltd.
公开号:US05892043A1
公开(公告)日:1999-04-06
A camptothecin derivative comprising a compound of the formula \x9bI!: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are (A) adjacent two groups combine to form alkylene, or both are H, and one of the remaining three groups is --X.sub.n --Alk.sub.m --R.sup.6, and the other two are H, alkyl or halogen, or (B) adjacent two groups combine to form alkylene, and one of the carbon atoms of said alkylene group is substituted by --X.sub.n --Alk.sub.m --R.sup.6, and the remaining three groups are H, alkyl or a halogen, and one or two --CH.sub.2 -- of the alkylene in (A) or (B) may optionally be replaced by --O--, --S-- or --NH--, X is --O-- or --NH--, Alk is alkylene, R.sup.6 is --NH.sub.2, ##STR2## or --OH, m and n are both 0 or 1, or m is 1 and n is 0, which camptothecin compound is bound to a polysaccharide having carboxyl groups via an amino acid or a peptide, or a pharmaceutically acceptable salt thereof. Said camptothecin derivatives show enhanced antitumor activities but few side effects and are useful as a medicament.
一种紫杉醇衍生物,包括以下式的化合物:##STR1##其中R.sup.1、R.sup.2、R.sup.3、R.sup.4和R.sup.5是(A)相邻两个基团结合形成烷基,或两者均为H,剩下的三个基团中的一个是--X.sub.n--Alk.sub.m--R.sup.6,另外两个是H、烷基或卤素;或者(B)相邻两个基团结合形成烷基,所述烷基中的一个碳原子被--X.sub.n--Alk.sub.m--R.sup.6取代,剩下的三个基团是H、烷基或卤素,而(A)或(B)中的烷基中的一个或两个--CH.sub.2--可以选择地被--O--、--S--或--NH--取代,X为--O--或--NH--,Alk为烷基,R.sup.6为--NH.sub.2、##STR2##或--OH,m和n均为0或1,或m为1且n为0,该紫杉醇化合物通过氨基酸或肽与具有羧基的多糖结合,或其药学上可接受的盐。所述紫杉醇衍生物显示出增强的抗肿瘤活性,但副作用较少,可用作药物。