Adenosine receptor agonists

Details Adenosine receptor agonists Adenosine receptor agonists

C - Chemistry, Metallurgy

07

H

C07H 19/16 (2006.01) A61K 31/7076 (2006.01) A61P 29/00 (2006.01)

Patent

CA 2557285

Use of compounds of general formula (A) as medicaments is described, in particular for the treatment of pain or inflammation; wherein: (I) when X = OH, R2 = NH2, R5 = CH2OH, R6 = H , R1 is C5-C6 alkoxy, OCH2Cyclopropyl, O- (2,2,3,3-tetrafluoro-cycloButyl), phenoxy, substituted phenoxy, OCH2CH2OH, or OCH2CHF2, (5-indanyl)oxy, C1, C2, C5, or C6 alkylamino, (R) or (S)-sec- Butylamino, C5 or C6 cycloalkylamino, exo-norbornane amino, (N-methyl, N- ~isoamylamino), phenylamino, phenylamino with either rnethoxy or fluoro substituents, a C2 sulfone group, a C2 alkyl group, a cyano group, a CONH2 group, or 3,5-dimethylphenyl; or when X = H, R2 = NH2, R5 = CH2OH , R6 = H, R1 is n-hexyloxy; or (II) when X = OH , R1 = H, R5 = CH2OH, R6 = H, R2 is NMe2, N- (2-isopentenyl), piperazinyl, (N-Me, N-benzyl), (N-Me, N-CH2Ph(3-Br)), (N-Me, N-~CH2Ph(3-CF3)), or (N-Me, N-(2-rnethoxyethyl)), or OCH2Cyclopentyl; or (III) when X = OH, R5 = CONHR3, R6 = H: R1 is H, R3 is an isopropyl group, and R2 is either NH2 or a methylamino group (NHMe) or an isoamyl group (CH2CH2CHMe2); or R1 is H, R3 is H, and R2 is NH2; or R1 is OMe, R3 is Ph, and R2 is NH2; or R1 is NHCH2CH2CH2CH2CH2Me, R3 is CH2CH2CH2Me, and R2 is NH2; or (IV) when X = OH, R1 = H, R2 = NH2, R5 = CH2NHCOR.4, R6 = H, R4 is n-propyl or NHCH2CH3; or (V) when X = OH, R5 = CH2OH, R6 = H: R1 is NHCyclohexyl when R2 is NMe2; or R1 is OMe when R2 is NHBenzyl; or (VI) when X = OH , R2 = NH2, R5 = CH2OH, R6 = Me, R1 is NHCyclohexyl or NHCyclopentyl.

La présente invention porte sur des composés représentés par la formule (A) utilisés comme médicaments, en particulier pour le traitement de la douleur ou de l'inflammation. Selon cette formule: (I) lorsque X = OH, R2 = NH2, R5 = CH2OH, R6 = H, R1 désigne alcoxy C5-C6, OCH2Cyclopropyle, O-(2,2,3,3-tétrafluoro-cycloButyle), phénoxy, phénoxy substitué, OCH2CH2OH, ou OCH2CHF2, (5-indanyl)oxy, C1, C2, C5, ou C6 alkylamino, (R) ou (S)-sec-Butylamino, C5 ou C6 cycloalkylamino, exo-norbornane amino, (N-méthyl, N-isoamylamino), phénylamino, phénylamino à substituants méthoxy ou fluoro, un groupe C2 sulfone, un groupe C7 alkyle, un groupe cyano, un groupe CONH2, ou 3,5-diméthylphényle; ou lorsque X = H, R2 = NH2, R5 = CH2OH, R6 = H, R1 désigne n-hexyloxy; ou (II) lorsque X = OH, R1 = H, R5 = CH2OH, R6 = H, R2 désigne NMe2, N-(2-isopentényle), pipérazinyle, (N-Me, N-benzyle), (N-Me, N-CH2Ph(3-Br)), (N-Me, N-CH2Ph(3-CF3)), ou (N-Me, N-(2-méthoxyéthyle)), ou OCH2Cyclopentyle; ou (III) lorsque X = OH, R5 = CONHR3, R6 = H: R1 désigne H, R3 désigne un groupe isopropyle et R2 désigne soit NH2 soit un groupe méthylamino (NHMe) soit un groupe isoamyle (CH2CH2CHMe2); ou R1 désigne H, R3 désigne H, et R2 désigne NH2; ou R1 désigne OMe, R3 désigne Ph, et R2 désigne NH2; ou R1 désigne NHCH2CH2CH2CH2CH2Me, R3 désigne CH2CH2CH2Me, et R2 désigne NH2; ou (IV) lorsque X = OH, R1 = H, R2 = NH2, R5 = CH2NHCOR.4, R6 = H, R4 désigne n-propyle ou NHCH2CH3; ou (V) lorsque X = OH, R5 = CH2OH, R6 = H: R1 désigne NHCyclohexyle lorsque R2 désigne NMe2; ou R1 désigne OMe lorsque R2 désigne NHBenzyle; ou (VI) lorsque X = OH, R2 = NH2, R5 = CH2OH, R6 = Me, R1 désigne NHCyclohexyle ou NHCyclopentyle.

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