Triazolo[4,5-d]pyrimidine derivatives and their use as...

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 487/04 (2006.01) A61K 31/198 (2006.01) A61K 31/519 (2006.01) A61K 45/06 (2006.01) A61P 25/00 (2006.01) A61P 25/14 (2006.01) A61P 25/16 (2006.01) A61P 25/28 (2006.01)

Patent

CA 2433453

The use of a compound of formula (I): wherein R1 is selected from H, alkyl, aryl, alkoxy, aryloxy, alkylthio, arylthio, halogen, CN, NR5R6, NR4COR5, NR4CONR5R6,NR4CO2R7 and NR4SO2R7; R2 is selected from aryl attached via an unsaturated carbon; R3 is selected from H, alkyl, COR5, CO2 R7, CONR5R6, CONR4NR5R6 and SO2R7; R4, R5 and R6 are independently selected from H, alkyl and aryl or where R5 and R6 are in an NR5R6 group, R5 and R6 may be linked to form a heterocyclic group, or where R4,R5 and R6 are in a (CONR4NR5R6) group, R4 and R5 may be linked to form a heterocyclic group; and R7 is selected from alkyl and aryl, or a pharmaceutically acceptable salt thereof or prodrug thereof, in the treatment or prevention of a disorder in which the blocking of purine receptors, particularly adenosine receptors and more particularly A2A receptors, may be beneficial, particularly wherein said disorder is a movement disorder such as Parkinson's disease or said disorder is depression, cognitive or memory impairment, acute or chronic pain, ADHD or narcolepsy, or for neuroprotection in a subject; compounds of formula (I) for use in therapy; and novel compounds of formula (I) per se.

L'invention concerne l'utilisation d'un composé de formule (I), dans laquelle R¿1? est choisi parmi H, alkyle, aryle, alcoxy, aryloxy, alkylthio, arylthio, halogène, CN, NR¿5?R¿6?, NR¿4?COR¿5?, NR¿4?CONR¿5?R¿6?,NR¿4?CO¿2?R¿7? et NR¿4?SO¿2?R¿7?; R¿2? est choisi parmi un aryle attaché via un carbone non saturé; R¿3? est choisi parmi H, alkyle, COR¿5?, CO¿2? R¿7?, CONR¿5?R¿6?, CONR¿4?NR¿5?R¿6? et SO¿2?R¿7?; R¿4?, R¿5? et R¿6? sont choisis, de façon indépendante, parmi H, alkyle et aryle, ou R¿5? et R¿6? sont dans un groupe NR¿5?R¿6?, R¿5? et R¿6? pouvant être liés de manière à former un groupe hétérocyclique, ou R¿4?,R¿5? et R¿6? sont dans un groupe (CONR¿4?NR¿5?R¿6?); R¿4? et R¿5? pouvant être liés de manière à former un groupe hétérocyclique; et R¿7? est choisi parmi alkyle et aryle, ou un de leur sel ou promédicament acceptable sur le plan pharmaceutique. Le composé de l'invention s'utilise dans le traitement ou la prévention d'un trouble dans lequel le blocage des récepteurs de purine, notamment les récepteurs d'adénosine et plus particulièrement les récepteurs A¿2A?, peut être bénéfique, notamment lorsque le trouble est un trouble du mouvement, tel que la maladie de Parkinson, ou une dépression, une altération de la mémoire, une déficience cognitive, des douleurs chronique ou aiguë, un THADA, une narcolepsie, ou dans la neuroprotection d'un sujet. L'invention concerne également des composés de formule (I) utilisés en thérapie, ainsi que des nouveaux composés de formule (I) per se.

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