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US 7,816,386 B2Granted
Cinnamic, phenylpropiolic and phenylpropanoic acid derivatives useful as anti-tumor agents
AssigneeSigma-Tau Industrie Farmaceutiche Riunite S.p.A.
InventorsClaudio Pisano, Gianfranco Battistuzzi, Maria Di Marzo, Giuseppe Giannini, Mauro Marzi, Loredana Vesci, Franco Zunino, Riccardo Pezzi
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Abstract
Cinnamic and phenylpropiolic acid derivatives of formula (I) having antitumour and chemo sensitizing activity are described. Also described are pharmaceutical compositions containing the above-mentioned compounds, for the treatment of tumours.
Claims9
A compound of the following formula I:
- wherein:
- n is 0;
- A is a monovalent group and is selected from the group consisting of:
- NH—OG and, the group
- where G and G′ are H,
- Y is a group selected among HC═CH, CH2—CH2 and C≡C;
- R is the group:
- where X is either O, NH;
- or
- R is the group:
- Z is H;
- R1 is H;
- or:
- R and R1, taken together with the aromatic group, form a polycyclic group having the following formula:
- R2 is selected from the group consisting of:
- H;
- (C6-C12) aryl or (C6-C12) aryl substituted with nitro, halogen, (C1-C4) alkoxycarbonyl;
- (C1-C4) alkyl, (C2-C4) alkenyl;
- (C6-C12) aryl-(CH2)n″, where aryl is substituted with nitro halogen, (C1-C4) alkoxycarbonyl, where n″=0-3;
- (C6-C12) aryl-CO, where aryl is substituted with halogen (C1-C4);
- and
- (C6) heterocyclyl-(C1-C3) alkylene where at least one of the CH2 of the heterocycle is substituted by O;
- R3 is H;
- R4 is H;
- R5 is H;
- its tautomers, geometrical isomers, optically active forms as enantiomers, diastereomers and racemate forms, as well as its pharmaceutically acceptable salts.
23 more elements
Dependencies are inferred from the claim text.