Back to results
US 8,796,284 B2Granted
4-aminopyrimidine derivatives and their as as adenosine A2a receptor antagonists
AssigneePalobiofarma, S.L.
InventorsJuan Alberto Camacho Gomez, Julio Cesar Castro-Palomino Laria
Life of this patent
Estimating the term…
Abstract
New 4-amino-pyrimidine derivatives as potent antagonists of the adenosine A2a receptor formula (I): (I) The invention provides as well a method for preparing such compounds, pharmaceutical compositions comprising an effective amount of these compounds and the use of such compounds in the manufacture of a medicament to treat pathological affections that can be improved by antagonism of the adenosine A2a receptor.
Claims11
A compound of formula (I):
- wherein
- R1 represents a five-membered heteroaryl ring selected from the group consisting of a pyrazole, a thiazole, and a triazole ring optionally substituted by one or two halogen atoms or by one or two methyl groups;
- R2 represents a hydrogen atom;
- R3 represents bromine or chlorine atom;
- R4 represents independently:
- a) a five-membered heteroaryl group optionally substituted by one or more halogen atoms or by one or more groups selected from the group consisting of alkyl, cycloalkyl, alkoxy, alkylthio, amino, mono- or dialkylamino
- b) a group —N(R5)(R6) in which R5 and R6 represent independently:
- a hydrogen atom;
- an alkyl or cycloalkyl group of 3 to 6 carbon atoms, linear or branched, optionally substituted by one or more halogen atoms or by one or more groups selected from the group consisting of cycloalkyl (3-8 carbon atoms), hydroxy, alkoxy, amino, mono- and dialkylamino (1-8 carbon atoms);
- or R5 and R6 form together with the nitrogen atom to that they are attached a saturated heterocyclic group of 4 to 6 members in which further heteroatom may be inserted, which is optionally substituted by one or more halogen atoms or by one or more alkyl groups (1-8 carbon atoms), hydroxy, lower alkoxy, amino, mono- or dialkylamino, or
- c) a group —OR7 or —SR7, where R7 represents independently:
- an alkyl (1-8 carbon atoms) or cycloalkyl (3-8 carbon atoms) group, linear or branched, optionally substituted by one or more halogen atoms or by one or more groups selected from the group consisting of alkyl (1-8 carbon atoms), alkoxy (1-8 carbon atoms), amino, mono- or dialkylamino (1-8 carbon atoms);
- or
- a Phenyl ring optionally substituted with one or more halogen atoms.
11 more elements
Dependencies are inferred from the claim text.