Back to results
US 7,119,109 B2Granted
Heteroarylheteroalkylamine derivatives and their use as inhibitors of nitric oxide synthase
AssigneeAstraZeneca AB
InventorsDeborah Chen, David Cheshire, Stephen Connolly, Antonio Mete
Life of this patent
Estimating the term…
Abstract
There are provided novel compounds of formula (I) wherein R1, R2, R3, T, U, X, Y, V and W are as defined in the specification, and pharmaceutically acceptable salts thereof; together with processes for their preparation, compositions containing them and their use in therapy. The compounds are inhibitors of nitric oxide synthase and are thereby particularly useful in the treatment or prophylaxis of inflammatory disease, CNS disorders and pain.
Claims15
A compound of formula (I)
- or a racemate, stereoisomer, or tautomer thereof, wherein:
- X is selected from the group consisting of H, C1 to C4 alkyl, C1 to C4 alkoxy, halogen, OH, CN, C═CH, NO2, CHO, COCH3 and NHCHO, wherein the alkyl or alkoxy group is unsubstituted or optionally substituted by one or more fluorine atoms or by an OH group;
- Y is selected from the group consisting of C1 to C4 alkyl, C1 to C4 alkoxy, halogen, OH, CN, C═CH, NO2, CHO, COCH3 and NHCHO, wherein the alkyl or alkoxy group is unsubstituted or optionally substituted by one or more fluorine atoms;
- one of T, U and W is N and the other two are independently CR4, wherein each R4 group is independently selected from the group consisting of H, F, and CH3;
- V is O or S(O)n;
- n is an integer 0, 1 or 2;
- R1 is selected from the group consisting of C1 to C4 alkyl, C2 to C4 alkenyl, C2 to C4 alkynyl, C3 to C6 cycloalkyl, and a 4 to 8 membered saturated heterocyclic ring incorporating one heteroatom selected from O, S and N, wherein any of the said R1 groups is unsubstituted or optionally substituted by a substituent selected from the group consisting of C1 to C4 alkyl, C1 to C4 alkoxy, C1 to C4 alkylthio, C3 to C6 cycloalkyl, one or more halogens, and phenyl, wherein the phenyl group is unsubstituted or optionally substituted by one or more substituents selected independently from the group consisting of halogen, C1 to C4 alkyl, C1 to C4 alkoxy, CF3, OCF3, CN and NO2;
- R2 and R3 are independently selected from the group consisting of H, C1 to C4 alkyl and C3 to C6 cycloalkyl, wherein the alkyl group is unsubstituted or optionally substituted by a substituent selected from the group consisting of C1 to C4 alkoxy, halogen, hydroxy, -Z-NR7R8, phenyl, and a five or six membered aromatic or saturated heterocyclic ring containing 1 to 3 heteroatoms independently selected from O, S and N, wherein the phenyl or aromatic heterocyclic ring is unsubstituted or optionally substituted by one or more groups selected from halogen, C1 to C4 alkyl, C1 to C4 alkoxy, CF3, OCF3, CN, and NO2;
- Z is —CO— or a bond;
- and
- R7 and R8 arc independently H or C1 to C4 alkyl, wherein the compound, racemate, stereoisomer, or tautomer thereof may exist in the form of a pharmaceutically acceptable salt thereof.
8 more elements
Dependencies are inferred from the claim text.