Use of quinoline derivatives with anti-integrase effect and applications thereof
AssigneesBioalliance Pharma, Institut Gustave Roussy, Centre National de la Recherche Scientifique (CNRS), Inserm, Universite De Paris 11-Paris Sud
InventorsAurélie Mousnier, Catherine Dargemont, Sabine Bonnenfant, Hervé Leh, Jean-François Mouscadet, Fatima Zouhiri, Jean D'Angelo, Didier Desmaele
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Abstract
The invention relates to the use of 8-hydroxyquinoline 7-carboxylic acid derivatives in order to produce integrase-inhibiting medicaments, capable of blocking viral replication in the stages preceding integration, and if appropriate at the level of this integration stage, these medicaments being usable for the treatment of retroviral pathologies, in particular for the treatment of AIDS.
Claims9
Method for inhibiting integrase and blocking viral replication in the stages preceding integration, and optionally at the level of this integration stage, for the treatment of retroviral pathologies, comprising administering to an animal or human in need thereof a 8-hydroxyquinoline 7-carboxylic acid derivative of formula III
- or a pharmaceutically acceptable salt thereof, wherein:
- X′ represents O, N, or an —(CH2)n— alkyl chain in which n is equal to 0, 1 or 2;
- Z′ represents an aromatic ring which can comprise heteroatoms selected from the group consisting of O, N and S in substitution of the carbon atoms constituting said aromatic ring, wherein Z′ is substituted by 0-3 Rb′ groups;
- Rb′, if present, at each occurrence is independently selected from the group consisting of —OR, —COOR, —COR, —NRR′, —SR and CN;
- and
- R and R′, identical or different, are selected from the group consisting of H and a linear or branched alkyl chain with 1 to 4 carbon atoms.
Method for inhibiting integrase nuclear import, comprising administering to an animal or human in need thereof a derivative of formula III
- or a pharmaceutically acceptable salt thereof, wherein:
- X′ represents O, N, or an —(CH2)n— alkyl chain in which n is equal to 0, 1 or 2;
- Z′ represents an aromatic ring which can comprise heteroatoms selected from the group consisting of O, N and S in substitution of the carbon atoms constituting said aromatic ring, wherein Z′ is substituted by 0-3 Rb′ groups;
- Rb′, if present, at each occurrence is independently selected from the group consisting of —OR, —COOR, —COR, —NRR′, —SR and CN;
- and
- R and R′, identical or different, are selected from the group consisting of H and a linear or branched alkyl chain with 1 to 4 carbon atoms.
A method for inhibiting integrase nuclear import, comprising administering to an animal or human in need thereof:
Dependencies are inferred from the claim text.