| 主权项 |
1. A method of treating a disease or condition in which the stimulation of CB2R is beneficial, the method comprising administering a therapeutically effective amount of a compound of formula I:wherein:
X is —S—, —O—, —SO—, NRa or —CH2—; Ra is hydrogen or (1-3C)alkyl; R1 is selected from hydrogen or a group of the formula:
X0—X1-Q1 whereinX0 is absent or —(CH2)n—;X1 is absent —CO— or —SO2—;n is 1, 2 or 3;when X1 is absent or —CO— then Q1 is selected from (1-5C)alkyl, (3-8C)cycloalkyl, aryl, a carbon-linked heterocyclyl, a carbon-linked heteroaryl or —NR7R8 where R7 and R8 are each independently selected from methyl or ethyl, or R7 and R8 are linked so that, together with the nitrogen atom to which they are attached, they form a 4-7 membered heterocyclic ring optionally comprising one, two or three additional heteroatoms selected from N, O or S;when X1 is —SO2— then Q1 is selected from (1-5C)alkyl, (3-8C)cycloalkyl, phenyl, thiophene or —NR7R8;and wherein Q1 is optionally substituted by one or more substituents selected from halo, trifluoromethyl, trifluoromethoxy, cyano, isocyano, nitro, hydroxy, mercapto, amino, formyl, carboxy, carbamoyl, ureido, (1-4C)alkyl, (2-4C)alkenyl, (2-4C)alkynyl, (1-4C)alkoxy, (1-4C)alkylthio, (1-4C)alkylsulphinyl, (1-4C)alkylsulphonyl, (1-4C)alkylamino, di-[(1-4C)alkyl]amino, (1-4C)alkoxycarbonyl, N-(1-4C)alkylcarbamoyl, N,N-di-[(1-4C)alkyl]carbamoyl, (2-4C)alkanoyl, (2-4C)alkanoyloxy, (2-4C)alkanoylamino, sulphamoyl, N-(1-4C)alkylsulphamoyl, N,N-di-[(1-4C)alkyl]sulphamoyl or a phenyl ring which is optionally further substituted by halo, methoxy, ethoxy, methyl, ethyl, cyano or hydroxy; R2 is selected from the group consisting of: (i) when R1 is hydrogen, R2 is selected from (3-5C)alkyl, (3-5C)alkenyl, (3-5C)alkynyl, aryl, (3-8C)cycloalkyl, thienyl or a group of the formula:
—CH2-Q2 wherein Q2 is selected from:(3-8C)cycloalkyl which is optionally substituted with cyano, nitro, fluoro or methyl;phenyl which is substituted in the ortho or para position (relative to the point of attachment to the —CH2— group) by cyano, nitro, methyl, —CO2H and tetrazole and optionally further substituted with cyano, nitro, fluoro, or methyl;naphthyl which is optionally substituted with cyano, nitro, fluoro or methyl; orthiophene which is optionally substituted with cyano, nitro, fluoro or methyl; and (ii) when R1 is a substituent group other than hydrogen, R2 is selected from (3-5C)alkyl, (3-5C)alkenyl, (3-5C)alkynyl, aryl, (3-8C)cycloalkyl, thienyl or a group of the formula:
—CH2-Q3 wherein Q3 is selected from phenyl, (3-8C)cycloalkyl, naphthyl or a neutral heteroaryl, each of which is optionally substituted by cyano, nitro, halo, methyl, trifluoromethyl, trifluoromethoxy, isocyano, hydroxy, mercapto, amino, carboxy, carbamoyl, methoxy, methylthio, methylsulphinyl, methylsulphonyl, methylamino, or di-methylamino; R3, R4, R5 or R6 are each independently selected from hydrogen, halo, (1-5C)alkyl, (3-6C)cycloalkyl, (3-6C)cycloalkyl(1-2C)alkyl, thiophene or aryl, wherein the aryl ring is optionally substituted by halo, methoxy, ethoxy, methyl, ethyl, cyano or hydroxy; with the proviso that R4, R5 or R6 are all hydrogen when R1 is hydrogen;or a pharmaceutically acceptable salt or solvate thereof. |
