7-([1,4]dioxan-2-yl)-benzothiazole derivative as adenosine...

Details 7-([1,4]dioxan-2-yl)-benzothiazole derivative as adenosine... 7-([1,4]dioxan-2-yl)-benzothiazole derivative as adenosine...

C - Chemistry, Metallurgy

07

D

C07D 417/14 (2006.01) A61K 31/428 (2006.01) A61P 25/00 (2006.01) C07D 417/04 (2006.01)

Patent

CA 2520852

The present invention relates to compounds of the general formula wherein R1 is a dioxan group as described in claim 1 and R2 is unsubstituted or substituted -(CH2)n-pyridin-2,3 or 4-yl; or is unsubstituted or mono- or di- substituted -(CH2)n-PiPeridine- 1-yl; or is unsubstituted or mono-or di- substituted -(CH2)n-phenyl; or is benzof [1.3] dioxol-5-yl; or -(CH2)n- morpholinyl; or -(CH2)n -tetrahydropyran-4-yl; or -(CH2)n -O-lower alk-yl; or - (CH2)n,-cycloalkyl; or -(CH2)n -C(0)-NR'R"; or -(CH2)n -2-oxo-pyrrolidin-1-yl; or -(CH2)n NRR"; or -2-oxa-5-aza-icyclo[2.2.1]heptane 5-yl; or -l-oxa-8-aza- spiro[4.5]decane-8-yl; and R'and R" are independently from each other lower alkyl, '(CH2)o -O-lower alkyl, mono- or di~substituted cycloalkyl; and n is 0, 1, 2 or 3; m is 0 or 1; and o is 1 or 2; and to pharmaceutically acceptable acid addition salts thereof It has been found that the compounds of general formula I are adenosine receptor ligands with a good affinity to the A2A- receptor and a high selectivity to the A1- and A3 receptors.

L'invention concerne des composés de formule générale?¿(I), dans laquelle R?1¿ représente un groupe dioxane tel qu'il est décrit dans la revendication 1 et R?2¿ représente -(CH¿2?)¿n?-pyridin-2,3 ou 4-yle substitué ou non ; ou -(CH¿2?)¿n?-pipéridin-1-yle non substitué ou monosubstitué ou disubstitué ; -(CH¿2?)¿n?-phényle non substitué ou monosubstitué ou disubstitué ; ou benzo[1.3] dioxol-5-yle; ou -(CH¿2?)¿n?-morpholinyle; ou -(CH¿2?)¿n?-tétrahydropyran-4-yle; ou -(CH¿2?)¿n?-O-alkyle inférieur ; ou -(CH¿2?)¿n?-cycloalkyle; ou -(CH¿2?)¿n?-C(O)-NR'R''; ou -(CH¿2?)¿n?-2-oxo-pyrrolidin-1-yle; ou -(CH¿2?)¿n?NR'R''; ou -2-oxa-5-aza-icyclo[2.2.1]heptan-5-yle; ou -1-oxa-8-aza-spiro[4.5]décan-8-yle ; et R' et R'' représentent indépendamment l'un de l'autre alkyle inférieur, -(CH¿2?)¿o?-O-alkyle inférieur, cycloalkyle monosubstitué ou disubstitué ; et n vaut 0, 1, 2 ou 3 ; m vaut 0 ou 1 ; et o vaut 1 ou 2. L'invention concerne également les sels d'addition d'acide pharmaceutiquement acceptables desdits composés. On a découvert que les composés de la formule générale (I) constituaient des ligands des récepteurs de l'adénosine présentant une bonne affinité pour le récepteur A¿2A ?et une sélectivité élevée vis-à-vis des récepteurs A¿1? et A¿3?.

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