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US 6,387,927 B1Granted
Epothilone derivatives and their use as antitumor agents
AssigneeNovatis AG
InventorsKarl-Heinz Altmann, Guido Bold, Giorgio Caravatti, Andreas Flörsheimer
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Abstract
The invention relates to anti-tumour-effective compounds of formula (I), wherein the radicals have the meanings given in the description.
Claims16
A compound of formula I
- wherein
- T is O, NH or N(alkyl), wherein alkyl is alkyl;
- A is a radical of formula Ia
- which is bonded to the radical of the molecule according to formula I by one of the two carbon atoms marked with an arrow, and wherein
- X is S;
- O;
- NH;
- N(alk);
- wherein alk is alkyl, hydroxy-lower alkyl, unsubstituted or substituted amino-lower alkyl or carbamoyl-lower alkyl;
- N(ar), wherein ar is aryl;
- C(Rk*)═N, N═C(Rk*) or C(Rk*)═C(Rk**), wherein Rk* and Rk**, independently of one another, are H, alkyl, unsubstituted or substituted amino-lower alkyl, carbamoyl-lower alkyl, halogen-lower alkyl or hydroxy-lower alkyl;
- and
- Rk is H, alkyl, unsubstituted or substituted amino-lower alkyl, carbamoyl-lower alkyl, halogen-lower alkyl or hydroxy-lower alkyl;
- either Y is OH and Y* is hydrogen, or —Y and —Y* together form a bond (so that they form a double bond together with the adjoining bond connecting the two —Y and —Y* bearing carbon atoms);
- R is hydrogen, lower alkyl or halogen-lower alkyl;
- and Z is O, or —Z— is a bond between the two binding carbon atoms;
- or salts thereof.
14 more elements
A compound of formula I, wherein means a radical selected from the radicals of formulae
- R hydrogen, methyl or ethyl;
- is O, or —Z— is a bond between the two binding carbon atoms;
- Y is hydroxy;
- Y* is hydrogen;
- and T is O;
- and the bond indicated by a wavy line is such that the compound of the formula I is present in the cis-form;
- or a pharmaceutically acceptable salt thereof.
4 more elements
Dependencies are inferred from the claim text.