C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 495/04 (2006.01) A61K 31/505 (2006.01) A61P 25/14 (2006.01) C07D 239/00 (2006.01) C07D 333/00 (2006.01) C07D 491/04 (2006.01)
Patent
CA 2370344
A compound of formula (I) wherein X is O or S; R1 and R2 are independently selected from hydrogen, alkyl, aryl, hydroxy, alkoxy, aryloxy, cyano, nitro, CO,R7, COR7, OCOR7CONR7R8, CONR7NR8R9, OCONR7R8, NR7R8, NR7COR8, NR7CONR8R9, NR7CO2R8, NR7SO2R8, NR7CONR8NR9R10, NR7NR8CO2R9, NR7NR8CONR9R10, NR7SO2NR8R9, SO2R7, SOR7, SR7 and SO2NR7R8, or R1 and R2 together form a carbonyl group (C=O), an oxime group (C=NOR11), an imine group (C=NR11) or a hydrazone group (C=NNR11R12), or R1 and R2 together form a 5, 6 or 7 membered carbocyclic or heterocyclic ring; R3 is alkyl or aryl; R4, R5 and R6 are independently selected from hydrogen, alkyl, aryl, halogen, hydroxy, nitro, cyano, alkoxy, aryloxy, COR7, OCOR7, CO2R7, SR7, SOR7, SO,R7, SO2NR7R8, CONR7R8, CONR7NR8R9, OCONR7R8, NR7R8, NR7COR8, NR7CONR8R9, NR7CO2R8, NR7SO2R8, CR7=NOR8, NR7CONR8NR9R10, NR7NR8CO2R9, NR7NR8CONR9R10, SO2NR7NR8R9, NR7SO2NR8R9, NR7NR8SO2R9, NR7NR8COR9, NR7NR8R9 and NR7CSNR8R9, or R5 and R6 together form a 5, 6 or 7 membered carbocyclic or heterocyclic ring; and R7, R8, R9, R10, R11 and R12 are independently selected from hydrogen, alkyl and aryl, or a pharmaceutically acceptable salt thereof or prodrug thereof, and the use thereof in therapy, particularly in the therapy of a disorder in which the blocking of purine receptors may be beneficial, such as Parkinson's Disease.
Divulgation d'un composé de formule (I) dans laquelle X représente O ou S; R1 et R2 sont indépendamment l'un de l'autre sélectionnés parmi un hydrogène, un alkyle, un aryle, un hydroxyle, un alcoxy, un aryloxy, un cyano, un nitro, CO2R7, COR7, CONR7R8, CONR7NR8R9, OCONR7R8, NR7R8, NR7COR8, NR7CONR8R9, NR7CO2R8, NR7SO2R8, NR7CONR8NR9R10, NR7NR8CO2R9, NR7NR8CONR9R10, NR7SO2NR8R9, SO2R7, SOR7, SR7 et SO2NR7R8, ou bien R1 et R2 ensemble constituent un groupe carbonyle (C=O), un groupe oxime (C=NOR11), un groupe imine (C=NR11) ou un groupe hydrazone (C=NNR11R12), ou encore R1 et R2 ensemble forment un hétérocycle ou carbocycle a 5, 6 ou 7 atomes; R3 est alkyle ou aryle; R4, R5 et R6 sont, indépendamment l'un de l'autre, sélectionnés parmi un hydrogène, un alkyle, un aryle, un halogène, un hydroxyla, un nitro, un cyano, un alcoxy, un aryloxy, COR7, OCOR7, CO2R7, SR7, SOR7, SO2R7, SO2NR7R8, CONR7R8, CONR7NR8R9, OCONR7R8, NR7R8, NR7COR8, NR7CONR8R9, NR7CO2R8, NR7SO2R8, CR7=NOR8, NR7CONR8NR9R10, NR7NR8CO2R9, NR7NR8CONR9R10, SO2NR7NR8R9, NR7SO2NR8R9, NR7NR8SO2R9, NR7NR8COR9, NR7NR8R9 et NR7CSNR8R9, ou bien R5 et R6 forment ensemble un hétérocycle ou carbocycle à 5, 6 ou 7 atomes; R7, R8, R9, R10, R11 et R12 sont indépendamment l'un de l'autre sélectionnés parmi un hydrogène, un alkyle et un aryle, ou d'un sel pharmaceutiquement acceptable ou un promédicament de ce composé. L'invention a aussi pour objet l'utilisation thérapeutique de ces composés, en particulier pour le traitement de troubles dans lesquels le blocage des récepteurs de la purine peut être avoir un effet bénéfique, comme la maladie de Parkinson.
Bebbington David
Dawson Claire Elizabeth
Giles Paul Richard
Gillespie Roger John
Lerpiniere Joanne
Kirby Eades Gale Baker
Vernalis Research Limited
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