Chromene derivatives
AssigneeConsejo Superior de Investigaciones Cientificas
InventorsBalbino Jose Alarcon Sanchez, Angel Messeguer Peypoch, Antonio Morreale De Leon, Aldo Jorge Borroto Revuelta, Irene Azahara Arellano Rojo, Almudena Perona Requena, Esther Carrasco Romero
Life of this patent
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Abstract
Derivates of chromene of formula I, where the meanings for the various substituents are as indicated in the description. These compounds are useful as inhibitors of TCR-Nck interaction in T lymphocytes.
Claims20
A compound of formula I:
- or a salt thereof, where:
- each R1 and R3 independently represent hydrogen, C1-4alkyl, C2-4alkenyl, C2-4alkynyl, hydroxyl, C1-4alkoxyl, C1-4alkoxyC1-4alkyl, haloC1-4alkyl, hydroxyC1-4alkyl, cyanoC1-4alkyl, halogen, —CN, —NO2 or Cy2;
- R2 represents hydrogen, C1-4alkyl or Cy2, where C1-4alkyl is optionally substituted by Cy2;
- Cy1 represents a monocyclic heterocycle of 3 to 7 members or bicyclic from 6 to 11 members, saturated or partially unsaturated which can be joined to the rest of the molecule by any available C or N atom, where Cy1 can be optionally merged to a ring of 5 or 6 members carbocyclic or heterocyclic saturated, partly unsaturated or aromatic, where Cy1 can contain from 1 to 4 heteroatoms selected from N, O and S, where one or more atoms of C or S of the ring may be oxidized to form groups CO, SO or SO2, and where Cy1 is optionally replaced by one or more R4;
- each Cy2 independently represents an aromatic ring of 5-7 members which can be joined to the rest of the molecule by any C or N available atom, where Cy2 can be optionally merged to a ring of 5 or 6 members carbocyclic or heterocyclic saturated, partly unsaturated or aromatic, where Cy2 can contain from 1 to 4 heteroatoms in total selected from N, O and S, where one or more atoms of C or S of the ring may be oxidized to form groups CO, SO or SO2, and where Cy2 is optionally replaced by one or more R4;
- each R4 independently represent, C1-4alkyl, C2-4alkenyl, C2-4alkynyl, hydroxyl, C1-4alkoxyl, C1-4alkoxyC1-4alkyl, haloC1-4alkyl, hydroxiC1-4alkyl, cyanoC1-4alkyl, halogen, —CN or —NO2;
- n represents from 0 to 4;
- and
- m represents from 0 to 5.
The compound according to i where each Cy2 independently represents phenyl or an aromatic ring of 5 or 6 members which can be joined to the rest of the molecule by any available C or N atom, where Cy2 contains 1 or 2 heteroatoms selected from N, O and S, where one or more atoms of C or S of the ring may be oxidized to form CO, SO or SO2 groups, and where Cy2 is optionally replaced by one or more R4.
The method according to claim 17 where the disease is selected from rejection of transplants;
- immune, autoimmune and inflammatory diseases;
- neurodegenerative diseases;
- and proliferative diseases.
Dependencies are inferred from the claim text.