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    • 1. 发明授权
    • Camptothecin derivatives
    • 喜树碱衍生物
    • US06617456B1
    • 2003-09-09
    • US09624012
    • 2000-07-21
    • Kenji TsujiharaTakayuki KawaguchiSatoshi OkunoToshiro Yano
    • Kenji TsujiharaTakayuki KawaguchiSatoshi OkunoToshiro Yano
    • C07D49800
    • C08B37/0018A61K47/61A61K47/65C08B37/0021
    • A camptothecin derivative comprising a compound of the formula [I]: wherein R1, R2, R3, R4 and R5 are (A) adjacent two groups combine to form alkylene, or both are H, and one of the remaining three groups is —Xn-Alkm-R6, 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 —Xn-Alkm-R6, and the remaining three groups are H, alkyl or a halogen, and one or two —CH2— of the alkylene in (A) or (B) may optionally be replaced by —O—, —S— or —NH—, X is —O— or —NH—, Alk is alkylene, 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.
    • 包含式[I]化合物的喜树碱衍生物:其中R1,R2,R3,R4和R5是(A)相邻的两个基团结合形成亚烷基,或两者都是H,其余三个基团之一是-Xn -Alkm-R6,另外两个为H,烷基或卤素,或(B)相邻的两个基团结合形成亚烷基,所述亚烷基的一个碳原子被-Xn-Alkm-R6取代,并且 剩余的三个基团是H,烷基或卤素,并且(A)或(B)中的一个或两个亚烷基的-CH 2可以任选地被-O - , - S-或-NH-替代,X是-O - 或-NH-,Alk为亚烷基或-OH,m和n均为0或1,或m为1,n为0,喜树碱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。 所述喜树碱衍生物显示出增强的抗肿瘤活性,但副作用很少,可用作药物。
    • 2. 发明授权
    • Camptothecin derivatives
    • 喜树碱衍生物
    • US06512118B1
    • 2003-01-28
    • US09227158
    • 1999-01-08
    • Kenji TsujiharaTakayuki KawaguchiSatoshi OkunoToshiro Yano
    • Kenji TsujiharaTakayuki KawaguchiSatoshi OkunoToshiro Yano
    • C07D47100
    • C08B37/0018A61K47/61A61K47/65C08B37/0021
    • A camptothecin derivative comprising a compound of the formula [I] is disclosed: wherein R1, R2, R3, R4 and R5 are (A) adjacent two groups combine to form alkylene, or both are H, and one of the remaining three groups is —Xn-Alkm-R6, 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 —Xn-Alkm-R6, and the remaining three groups are H, alkyl or a halogen, and one or two —CH2— of the alkylene in (A) or (B) may optionally be replaced by —O—, —S— or —NH—, X is —O— or —NH—, Alk is alkylene, R6 is —NH2, 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.
    • 公开了包含式[I]化合物的喜树碱衍生物:其中R1,R2,R3,R4和R5是(A)相邻的两个基团结合形成亚烷基,或两者都是H,其余三个基团之一是 -Xn-Alkm-R6,另外两个为H,烷基或卤素,或(B)相邻的两个基团结合形成亚烷基,所述亚烷基的一个碳原子被-Xn-Alkm-R6取代, 并且其余三个基团是H,烷基或卤素,并且(A)或(B)中亚烷基的一个或两个-CH 2可以任选地被-O - , - S-或-NH-代替,X是 -O-或-NH-,Alk为亚烷基,R6为-NH2或-OH,m和n均为0或1,或m为1,n为0,喜树碱化合物与具有羧基的多糖结合 通过氨基酸或肽,或其药学上可接受的盐。 所述喜树碱衍生物显示出增强的抗肿瘤活性,但副作用很少,可用作药物。
    • 3. 发明授权
    • Camptothecin derivatives
    • 喜树碱衍生物
    • US5892043A
    • 1999-04-06
    • US773182
    • 1996-12-27
    • Kenji TsujiharaTakayuki KawaguchiSatoshi OkunoToshiro Yano
    • Kenji TsujiharaTakayuki KawaguchiSatoshi OkunoToshiro Yano
    • A61K47/48C08B37/00C08B37/02C07D471/00
    • C08B37/0018A61K47/4823A61K47/48338C08B37/0021
    • A camptothecin derivative comprising a compound of the formula �I!: ##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.
    • 包含式[I]化合物的喜树碱衍生物:其中R 1,R 2,R 3,R 4和R 5是(A)相邻的两个基团结合形成亚烷基,或两者都是H,并且其中之一 其余三个为-Xn-Alkm-R6,另外两个为H,烷基或卤素,或(B)相邻的两个基团结合形成亚烷基,所述亚烷基的一个碳原子被-Xn- Al-C-R6,其余三个基团是H,烷基或卤素,并且(A)或(B)中亚烷基的一个或两个-CH 2可以任选地被-O - , - S-或-NH - ,X为-O-或-NH-,Alk为亚烷基,R6为-NH2,或IMA为-OH,m和n均为0或1,或m为1,n为0,喜树碱化合物为 通过氨基酸或肽或其药学上可接受的盐与具有羧基的多糖结合。 所述喜树碱衍生物显示出增强的抗肿瘤活性,但副作用很少,可用作药物。