Benzothiophenes as adenosine receptor modulators

C - Chemistry – Metallurgy – 07 – D

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C07D 333/66 (2006.01) A61K 31/38 (2006.01) A61P 25/16 (2006.01) A61P 25/24 (2006.01) A61P 25/28 (2006.01) C07D 409/12 (2006.01)

Patent

CA 2469872

The invention relates to compounds of the general formula (I), wherein R is phenyl, optionally substituted by halogen, or is pyridin 3-or 4-yl, optionally substituted by lower alkyl, or is -NR1R2, wherein Rl and R2 form together with the N atom to which they are attached heterocyclic rings, selected from the group consisting of morpholinyl, thiomorpholinyl, piperidinyl or piperazinyl, optionally substituted by -(CH2) n-hydroxy, lower alkyl or lower alkoxy; n is 0, 1 or 2; and to pharmaceutically acceptable acid addition salts thereof. It has been shown that the compounds of formula (I) have a good affinity to the A2A receptor and they are therefore useful for the treatment of diseases related to this receptor.

L'invention concerne des composés de formule générale (I), dans laquelle R représente un phényle, facultativement substitué par un halogène ou pyridine 3- ou 4-yl, facultativement substitué par un alkyle inférieur ou -NR?1¿R?2¿, R?l¿ et R?2¿ formant ensemble avec l'atome d'azote auquel ils sont attachés des anneaux hétérocycliques, sélectionnés parmi le groupe comprenant morpholinyl, thiomorpholinyl, piperidinyl ou piperazinyl, facultativement substitués par -(CH¿2?)¿n?-hydroxy, un alkyle inférieur ou un alkoxy inférieur, et n est égal à 1, 2 ou 3. Ladite invention a également trait à des sels d'addition acide correspondants acceptables pharmaceutiquement. Selon cette invention, les composés de formule (I) présentent une bonne affinité vis-à-vis du récepteur A2A, et ils sont alors utilisés dans le traitement de maladies liées à ce récepteur.

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