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US 6,552,073 B1Granted
Compounds and methods of treating cell proliferative diseases
AssigneeExonhit Therapeutics SA
InventorsVéronique Leblanc, Bertrand Leblond, Dominique Melle-Milovanovic, Maria Luz Lopez Rodriguez, Alma Viso Beronda
Life of this patent
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Abstract
The present invention relates to compounds and their uses, particularly in the pharmaceutical industry. The invention discloses compounds having anti-proliferative activities, as well as methods for treating various diseases associated with abnormal cell proliferation, including cancer, by administering said compounds. It further deals with pharmaceutical compositions comprising said compounds, more particularly useful to treat cancers.
Claims23
A compound having a general formula (I):
- wherein:
- R1 is CH2R3 or COR3;
- R2 represents a hydrogen atom or an alkenyl group containing from 3 to 6 carbon atoms;
- R3 is —OH, —OR4, —SR4, —NR5R6, or
- R4 represents a group selected from alkyl containing from 1 to 6 carbon atoms, aryl, aralkyl, alkanoyl from 2 to 6 carbon atoms and arylcarbonyl;
- R5 and R6, independently from each other, are selected from a hydrogen atom, an alkyl group having from 1 to 10 carbon atoms, an aryl and an aralkyl;
- m is 2 or 3;
- n represents an integer between 1 and 10 inclusive;
- X represents an oxygen atom, a sulfur atom or a radical —NR7—;
- Y represents an oxygen atom;
- R7, identical or different, is selected in a group consisting of a hydrogen atom, an alkyl group having from 1 to 10 carbon atoms, an aryl and an aralkyl;
- A represents either a substituted phenyl group of formula
- in which:
- R8, R9, R10 and R11, independently from each other, are selected from a hydrogen atom, a halogen atom (preferably F, Cl, or Br), a hydroxyl group, a (C1-C10)alkyl group, an (C1-C10)alkanoyl group, a (C1-C10)alkoxy group, an aryl group, an aralkyl group, an arylcarbonyl group, a mono- or poly-cyclic hydrocarbon group, —NO2, —CN, a —NR12R13 group or a trifluoro(C1-C6)alkyl group;
- R8, R9, R10 and R11, not being simultaneously hydrogen atom,
- or alternatively two substituents, R8 and R9, may form together a mono- or poly-cyclic hydrocarbon group with the carbon atoms of the phenyl group they are attached and the two other substituents, R10 and R11, are as defined above;
- or A represents a 5- or 6-membered heterocyclic ring which has 1 to 3 hetero-atoms selected from oxygen, sulfur and nitrogen, said ring is bonded directly to X;
- R12 and R13, independently from each other, are selected in the group consisting of a hydrogen atom, an alkyl group having from 1 to 10 carbon atoms, an aryl and an aralkyl;
- with the provisos that:
- when X is an oxygen atom, R2 is a hydrogen atom, n is 5 and R8 on the ortho position on the phenyl group is n-propyl group, then R9, R10 and R11 are different from hydrogen;
- when X is an oxygen atom, R2 is a hydrogen atom, n is 5, R8 on the ortho position on the phenyl group is n-propyl group, R9 on the meta position is an hydroxyl group, and R10 on the para position is an acetyl group;
- then R11 is different from hydrogen;
- when X is an oxygen atom, R2 is a hydrogen atom, n is 2 or 3, then A is different from a non-substituted naphthalene group;
- its optical isomers, geometrical isomers, salt, or hydrates thereof.
21 more elements
Dependencies are inferred from the claim text.