New Inhibitors of Cyclophilins and Uses Thereof
AssigneeInstitut National De La Sante Et De La Recherche Medicale (Inserm)
InventorsJean-Francois Guichou, Lionel Colliandre, Hakim Ahmed-Belkacem, Jean-Michael Pawlotsky
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Abstract
The present invention relates to a compound of formula (I): wherein: n is 0, 1 or 2; A is in particular CH or N; X is in particular CO, SO2, CS, and R1 is in particular H, R2 is a group of formula NR3R4 or OR5, R3 and R4 being in particular H, and R5 an alkyl group, R6 is in particular H or an alkyl group, and R7 is in particular an aryl group, for its use in the prevention and/or the treatment of viral pathologies or infections.
Claims17
1-12. (canceled)
A compound having formula (I-bis):
- wherein:
- R1 is selected from the group consisting of H, alkyl groups, and aralkyl groups, said alkyl or aralkyl groups being possibly substituted;
- R2 is a group of formula NR3R4 or OR5, wherein R3 and R4 are independently selected from the group consisting of H, ORa, alkyl groups, aralkyl groups, and aryl groups, Ra being selected from the group consisting of H, alkyl groups, aryl groups, and aralkyl groups, wherein R3 and R4 may form, together with the nitrogen atom carrying them, a heterocyclyl group comprising from 5 to 20 atoms, possibly substituted, and R5 is selected from the group consisting of alkyl groups, aryl groups, and aralkyl groups, wherein R5 may form, together with the oxygen atom carrying it, a heterocyclyl group from 5 to 20 atoms, possibly substituted;
- A is CH or N, or A is C and form, together with R1 and R2 and CO, a heterocyclyl group comprising from 5 to 20 atoms, possibly substituted;
- X is CO, SO2, or CS;
- R6 is H or an alkyl group, or may form together with R2 a heterocyclyl group from 20 to 30 atoms, or may form together with R1 a heterocyclyl group from 10 to 30 atoms;
- and
- R7 is chosen from the group consisting of aryl groups and heteroaryl groups comprising 5 or 6 ring atoms, substituted by at least one NH2 group,
- or their pharmaceutically acceptable salts, hydrates or hydrated salts or its polymorphic crystalline structures, racemates, diastereomers or enantiomers, with the exclusion of the following compounds:
A method of preventing viral pathologies or infections in a patient in need thereof, comprising the step of
- administering to said patient a therapeutically effective amount of a compound of formula (I):
- wherein:
- n is 0, 1 or 2;
- A is CH or N, or A is C and form, together with R1, R2 and CO, a heterocyclyl group comprising from 5 to 20 atoms, possibly substituted;
- X is CO, SO2 or CS,
- R1 is chosen from the group consisting of:
- H, alkyl groups, and aralkyl groups, said alkyl or aralkyl groups being possibly substituted,
- R2 is a group of formula NR3R4 or OR5, wherein:
- R3 and R4 being each independently chosen from:
- H, ORa, alkyl groups, aralkyl groups, and aryl groups, Ra being chosen from the group consisting of:
- H, alkyl groups, aryl groups, and aralkyl groups;
- wherein R3 and R4 may form, together with the nitrogen atom carrying them, a heterocyclyl group comprising from 5 to 20 atoms, possibly substituted,
- R5 is chosen from:
- alkyl groups, aryl groups, and aralkyl groups,
- wherein R5 may form, together with the oxygen atom carrying it, a heterocyclyl group from 5 to 20 atoms, possibly substituted,
- R6 is H or an alkyl group, or may form together with R2 a heterocyclyl group from 20 to 30 atoms, or may form together with R1 a heterocyclyl group from 10 to 30 atoms,
- R7 is chosen from the group consisting of:
- aryl groups, heteroaryl groups, —NHPh, heterocyclyl groups, and alkyl groups;
- wherein when R7 is aryl, heteroaryl or heterocyclyl, it is substituted by at least one NH2 group,
- wherein, when A is N, R1 and R2 may form, together with A and CO, a heterocyclyl group comprising from 5 to 20 atoms, possibly substituted,
- or its pharmaceutically acceptable salts, hydrates or hydrated salts or its polymorphic crystalline structures, racemates, diastereomers or enantiomers.
Dependencies are inferred from the claim text.