4-phenyl-coumarin derivatives, processes for their preparation and uses thereof for the treatment of cancer
AssigneesLead Discovery Center GmbH, Max-Planck-Gesellschaft Zur FöRderung Der Wissenschaften E. V.
InventorsRaffaella Di Lucrezia, Tim Bergbrede, Peter Nussbaumer, Uwe Koch, Bert Klebl, Axel Choidas, Anke Unger, Nils-Göran Larsson, Maria Falkenberg-Gustafsson, Claes M. Gustafsson
Life of this patent
Estimating the term…
Abstract
The invention provides novel 4-phenyl-coumarin derivatives, processes for their preparation and uses thereof as specific mitochondrial RNA polymerase inhibitors for the treatment of cancer.
Claims14
A method of inhibiting POLRMT comprising administering a therapeutically effective amount of a compound of the general formula (I)
- wherein
- R is —H or —C1-C4-alkyl;
- R1 is —H or -methyl;
- R2 is —H;
- n=0, 1 or 2;
- X is -halogen, —C1-C4-alkyl, —OMe or —CN, with n=1 or 2;
- Y is —NR3R4 with
- R3 is —H, or —C1-C4-alkyl, and
- R4 is —H, —C1-C4-alkyl or —C3-C8-cycloalkyl;
- an unsubstituted or substituted pyridine residue;
- an unsubstituted or substituted pyridinylmethyl residue;
- an unsubstituted or substituted morpholinylethyl residue;
- an unsubstituted or substituted furanylmethyl residue;
- an unsubstituted or substituted phenyl residue;
- an unsubstituted or substituted benzyl residue;
- an unsubstituted or substituted phenethyl residue;
- the group;
- or
- the group
- or
- Y is —NR3R4 with N, R3 and R4 forming an unsubstituted or substituted 5- or 6-membered saturated heterocycle,
- or
- Y is —OR11, with R11 is —H or —C1-C4-alkyl, phenyl, benzyl or 2-ethoxyethyl;
- and
- W1, W2, and W3 are identical or different, and are —H, -halogen, or —C1-C4-alkyl;
- or a pharmaceutically or veterinary acceptable salt, hydrate or solvate thereof
- to a patient in need thereof.
A method of treating cancer by inhibiting POLRMT comprising administering a therapeutically effective amount of a compound of the general formula (I)
- wherein
- R is —H or —C1-C4-alkyl;
- R1 is —H or -methyl;
- R2 is —H;
- n=0, 1 or 2;
- X is -halogen, —C1-C4-alkyl, —OMe or —CN, with n=1 or 2;
- Y is —NR3R4 with
- R3 is —H, or —C1-C4-alkyl, and
- R4 is —H, —C1-C4-alkyl or —C3-C8-cycloalkyl;
- an unsubstituted or substituted pyridine residue;
- an unsubstituted or substituted pyridinylmethyl residue;
- an unsubstituted or substituted morpholinylethyl residue;
- an unsubstituted or substituted furanylmethyl residue;
- an unsubstituted or substituted phenyl residue;
- an unsubstituted or substituted benzyl residue;
- an unsubstituted or substituted phenethyl residue;
- the group
- or
- the group
- or
- Y is —NR3R4 with N, R3 and R4 forming an unsubstituted or substituted 5- or 6-membered saturated heterocycle,
- or
- Y is —OR1, with R11 is —H or —C1-C4-alkyl, phenyl, benzyl or 2-ethoxyethyl;
- and
- W1, W2, and W3 are identical or different, and are —H, -halogen, or —C1-C4-alkyl;
- or a pharmaceutically or veterinary acceptable salt, hydrate or solvate thereof
- to a patient in need thereof.
Dependencies are inferred from the claim text.