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US 7,452,883 B2Granted
Dihydro-1,3,5-triazine amine derivatives and their therapeutic uses
AssigneeMerck Sante
InventorsGerard Moinet, Daniel Cravo, Liliane Doare, Micheline Kergoat, Didier Mesangeau
Life of this patent
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Abstract
The invention concerns compounds of general formula (I) wherein: R1, R2, R3, R4, R5 and R6 are as defined in Claim 1. The compounds are useful in the treatment of pathologies related to the insulin-resistance syndrome.
Claims13
A method for inhibiting the formation of advanced glycosylation end products (AGE) in a patient that has and is being treated for atherosclerosis and/or Alzheimer's disease, comprising:
- administering to said patient in need thereof an effective amount of a compound of formula (I)
- in which:
- R1 and R2 are chosen independently from the groups:
- —H,
- —(C1-C20)alkyl,
- wherein R3 and R4 are chosen independently from the groups:
- —H,
- —(C1-C20)alkyl,
- —(C2-C20)alkenyl,
- R3 and R4 can form with the nitrogen atom an n-membered ring (n between 3 and 8) optionally comprising one or more heteroatoms chosen from N, O, S,
- R5 and R6 are chosen independently from the groups:
- H,
- (C1-C20)alkyl optionally substituted with hydroxyl,
- (C3-C8)cycloalkyl optionally substituted with (C6-C14)aryl (C1-C5)alkoxy,
- (C3-C8)heterocycloalkyl carrying one or more heteroatoms chosen from N, O, S,
- (C6-C14)aryl optionally substituted with hydroxyl,
- (C1-C13)heteroaryl carrying one or more heteroatoms chosen from N, O, S,
- (C6C14)aryl (C1-C5)alkyl,
- wherein R5 and R6 can form with the carbon atom to which they are attached an m-membered ring (m between 3 and 8) optionally comprising one or more heteroatoms chosen from N, O, S and being capable of being substituted with hydroxyl, (C1-C5)alkyl, (C6-C14)aryl (C1-C5)alkoxy,
- wherein when R1 and R2 represent a hydrogen, or R3 and R4 represent a hydrogen, then R3 and R4 or R1 and R2 are defined as above with the exception of hydrogen, or a form selected from the group consisting of tautomeric, enantiomeric, diastereoisomeric and epimeric or the pharmaceutically acceptable salt thereof.
17 more elements
A method for treating atherosclerosis or Alzheimer's disease, comprising:
- administering to a patient in the need thereof an effective amount of a compound of formula (I)
- in which:
- R1 and R2 are chosen independently from.the groups:
- H,
- (C1-C20)alkyl,
- wherein R3 and R4 are chosen independently from the groups:
- H,
- (C1-C20)alkyl,
- (C2-C20)alkenyl,
- R3 and R4 can form with the nitrogen atom an n-membered ring (n between 3 and 8) optionally comprising one or more heteroatoms chosen from N, O, S,
- R5 and R6 are chosen independently from the groups:
- H,
- (C1-C20)alkyl optionally substituted with hydroxyl,
- (C3-C8)cycloalkyl optionally substituted with (C6-C14)aryl (C1-C5)alkoxy,
- (C3-C8)heterocycloalkyl carrying one or more heteroatoms chosen from N, O, S,
- (C6-C14)aryl optionally substituted with hydroxyl,
- (C1-C13)heteroaryl carrying one or more heteroatoms chosen from N, O, S,
- (C6-C14)aryl (C1-C5)alkyl,
- wherein R5 and R6 can form with the carbon atom to which they are attached an m-membered ring (m between 3 and 8) optionally comprising one or more heteroatoms chosen from N, O, S and being capable of being substituted with hydroxyl, (C1-C5)alkyl, (C6-C14)aryl (C1-C5)alkoxy,
- wherein when R1 and R2 represent a hydrogen, or R3 and R4 represent a hydrogen, then R3 and R4 or R1 and R2 are defined as above with the exception of hydrogen, or a form selected from the group consisting of tautomeric, enantiomeric, diastereoisomeric and epimeric form or the pharmaceutically acceptable salt thereof.
17 more elements
A method for treating renal complications wherein the formation of advanced glycosylation end products (AGE) is implicated in a patient, comprising administering to said patient in need thereof an effective amount of a compound of formula (I)
- in which:
- R1 and R2 are chosen independently from the groups:
- H,
- (C1-C20)alkyl,
- wherein R3 and R4 are chosen independently from the groups:
- H,
- (C1-C20)alkyl,
- (C2-C20)alkenyl,
- R3 and R4 can form with the nitrogen atom an n-membered ring (n between 3 and 8) optionally comprising one or more heteroatoms chosen from N, O, S,
- R5 and R6 are chosen independently from the groups:
- H,
- (C1-C20)alkyl optionally substituted with hydroxyl,
- (C3-C8)cycloalkyl optionally substituted with (C6-C14)aryl (C1-C5)alkoxy,
- (C3-C8)heterocycloalkyl carrying one or more heteroatoms chosen from N, O, S,
- (C6-C14)aryl optionally substituted with hydroxyl,
- (C1-C13)heteroaryl carrying one or more heteroatoms chosen from N, O, S,
- (C6-C14)aryl (C1-C5)alkyl,
- wherein R5 and R6 can form with the carbon atom to which they are attached an m-membered ring (m between 3 and 8) optionally comprising one or more heteroatoms chosen from N, O, S and being capable of being substituted with hydroxyl, (C1-C5)alkyl, (C6-C14)aryl (C1-C5)alkoxy,
- wherein when R1 and R2 represent a hydrogen, or R3 and R4 represent a hydrogen, then R3 and R4 or R1 and R2 are defined as above with the exception of hydrogen, or a form selected from the group consisting of tautomeric, enantiomeric, diastereoisomeric and epimeric or the pharmaceutically acceptable salt thereof.
16 more elements
Dependencies are inferred from the claim text.