Patent ID: 6514949
Filing Date: 2003-02-04
Classification: A61K,Y02A

Abstract:
A method of treating an inflammatory response, comprising administering to a mammal in need thereof an effective anti-inflammatory amount of an agonist of an A2A adenosine receptor having formula (I) wherein X is a group selected from the group consisting of â€”OR1, â€”NR2R3, â€”Câ‰¡Câ€”Z and â€”NHâ€”N&boxH;R4;each Y is individually H, C1-C6 alkyl, C3-C7 cycloalkyl, phenyl or phenyl C1-C3 alkyl; R1 is (a) C1-4-alkyl; (b) C1-4-alkyl substituted with one or more C1-4-alkoxy, halogens (fluorine, chlorine, or bromine), hydroxy, amino, mono(C1-4-alkyl)amino, di(C1-4-alkyl)amino, or C6-10-aryl, wherein aryl may be substituted with one or more halogen, C1-4-alkyl, hydroxy, amino, mono(C1-4-alkyl)amino, or di(C1-4-alkyl)amino; (c) C6-10-aryl; or (d) C6-10-aryl substituted with one or more halogen, hydroxy, amino, mono(C1-4-alkyl)amino, di(C1-4-alkyl)amino, or C1-4-alkyl; one of R2 and R3 has the same meaning as R1 and the other is hydrogen; R4 is a group having the formula: wherein each of R5 and R6 independently may be hydrogen, C3-7-cycloalkyl, or any of the meanings of R1, provided that R5 and R6 are not both hydrogen;R is â€”CH2OH, â€”CH3, â€”CO2R7 or â€”C(&boxH;O)NR8R9; wherein R7 has the same meaning as R2 and wherein R8 and R9 have the same meanings as R5 and R6, or R8 and R9 are both H; Z has one of the following meanings: a) phenyl or naphthyl optionally substituted with one to three halogen atoms, C1-C6 alkyl, C1-C6 haloalkyl, C1-C6 alkoxy, C1-C6 haloalkoxy, C2-C6 alkoxycarbonyl, C2-C6 alkoxyalkyl, C1-C6 alkylthio, thio, CHO, cyanomethyl, nitro, cyano, hydroxy, carboxy, C2-C6 acyl, amino, C1-C3 monoalkylamino, C2-C6 dialkylamino, methylenedioxy; aminocarbonyl; b) a group of formula â€”(CH2)m-Het wherein m is 0 or an integer from 1 to 3 and Het is 5 or 6 membered heterocyclic aromatic or non-aromatic ring, optionally benzocondensed, containing 1 to 3 heteroatoms selected from nonperoxide oxygen, nitrogen or sulphur, linked through a carbon atom or through a nitrogen atom; c) C3-C7 cycloalkyl optionally containig unsaturation or C2-C4 alkenyl; R10 is hydrogen, methyl or phenyl; R12 is hydrogen, C1-C6 linear or branched alkyl, C5-C6 cycloalkyl or C3-C7 cycloalkenyl, phenyl-C1-C2-alkyl or R10 and R12, taken together, form a 5- or 6-membered carbocyclic ring or R3 is hydrogen and R2 and R4, taken together, form an oxo group or a corresponding acetalic derivative; R11 is OH, NH2 dialkylamino, halogen, cyano; n is 0 or 1 to 4; or e) C1-C16 alkyl, optionally comprising 1-2 double bonds, O, S or NY; or a pharmaceutically acceptable salt thereof; provided that the inflammation is not caused by hypertension, thrombosis or atherosclerosis.