Novel use
AssigneeAstraZeneca AB
InventorsSverker Hanson, Gunnar Nordvall
Life of this patent
Estimating the term…
Abstract
There is disclosed the use of a compound of formula (I) wherein R1, R2, R3, Ar and X are as defined in the specification, and pharmaceutically acceptable salts, enantiomers or racemates thereof, in the manufacture of a medicament, for the treatment or prophylaxis of diseases or conditions in which antagonism of the CX3CR1 receptor is beneficial. Certain novel compounds of formula (Ia) and pharmaceutically acceptable salts thereof, and enantiomers and racemates thereof are disclosed, together with processes for their preparation. The compounds of the formulae (I) and (Ia) are CX3CR1 receptor antagonists and are thereby particularly useful in the treatment or prophylaxis of neurodegenerative disorders, demyclinating disease and pain.
Claims10
Use of a compound of formula (I)
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- wherein:
- R1 represents hydrogen, NR4R5, CONR6R7 or a 4 to 7 membered saturated monoazacyclic ring optionally substituted by C1 to C6 alkyl or C1 to C6 alkyl-OR8;
- R2 represents C3 to C7 alkyl, optionally substituted by OR9 or NR10R11;
- R3 represents hydrogen or C1 to C7 alkyl, optionally substituted by OR12 or NR13R14;
- or R2 and R3 are joined together such that the group R2—C—R3 forms a C3 to C7 cycloalkyl group, optionally substituted by OR9 or NR10R11;
- Ar represents phenyl optionally substituted by one or more groups selected independently from halogen, C1 to C6 alkyl, C1 to C6 alkoxy, methylenedioxy, cyano, nitro, —CO2R15 or —CONR16R17;
- said alkyl group being optionally substituted by one or more fluorine atoms;
- X represents a bond or C1 to C6 alkyl;
- R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16 and R17 independently represent hydrogen or C1 to C6 alkyl;
- or a pharmaceutically acceptable salt, enantiomer or racemate thereof, in the manufacture of a medicament, for the treatment or prophylaxis of diseases or conditions in which antagonism of the CX3CR1 receptor is beneficial.
A compound of formula (Ia)
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- wherein:
- R1 represents hydrogen, NR4R5, CONR6R7 or a 4 to 7 membered saturated monoazacyclic ring optionally substituted by C1 to C6 alkyl or C1 to C6 alkyl-OR8;
- R2 represents C3 to C7 alkyl, optionally substituted by OR9 or NR10R11;
- R3 represents hydrogen or C1 to C7 alkyl, optionally substituted by OR12 or NR13R14;
- or R2 and R3 are joined together such that the group R2—C—R3 forms a C3 to C7 cycloalkyl group, optionally substituted by OR9 or NR10R11;
- Ar represents phenyl optionally substituted by one or more groups selected independently from halogen, C1 to C6 alkyl, C1 to C6 alkoxy, methylenedioxy, cyano, nitro, —CO2R15 or —CONR16R17;
- said alkyl group being optionally substituted by one or more fluorine atoms;
- X represents a bond or C1 to C6 alkyl;
- R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16 and R17 independently represent hydrogen or C1 to C6 alkyl;
- or a pharmaceutically acceptable salt, enantiomer or racemate thereof;
- with the proviso that when R1 and R3 each represent hydrogen and R2 represents iso-butyl, Ar does not represent unsubstituted phenyl or 2,3-difluorophenyl.
Dependencies are inferred from the claim text.