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US 2004/0176422 A1Published application
Heteroarylheteroalkylamine derivatives and their use as inhibitors of nitric oxide synthase
OwnerTimothy Birkinshaw, David Cheshire +3inventors
InventorsTimothy Birkinshaw, David Cheshire, Stephen Connolly, Timothy Luker, Antonio Mete
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Abstract
There are provided novel compounds of formula (I), wherein R1, R2, R3, Q, T, U, X, Y, V and W are as defined in the specification, and pharmaceutically acceptable salts thereof, and enantiomers and racemates 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 and pain.
Claims21
A compound of formula (I)
- 12
- wherein:
- X represents H, C1 to 4 alkyl, C1 to 4 alkoxy, halogen, OH, NHR9, CN, C≡CH, NO2, CHO, COCH3 or NHCHO;
- said alkyl or alkoxy group being optionally further substituted by one or more fluorine atoms or by an OH group;
- Y represents C1 to 4 alkyl, C1 to 4 alkoxy, halogen, OH, CN, C≡CH, NO2, CHO, COCH3 or NHCHO;
- said alkyl or alkoxy group being optionally further substituted by one or more fluorine atoms;
- One of T, U and W represents N and the other two independently represent CR4;
- and each R4 group independently represents H, F or CH3;
- V represents O or S(O)n;
- n represents an integer 0, 1 or 2;
- Q represents CH2 or (CH2)2;
- R1 represents phenyl or a five or six membered aromatic heterocyclic ring containing 1 to 3 heteroatoms independently selected from O, S and N;
- said phenyl or aromatic heterocyclic ring being optionally substituted by one or more substituents selected independently from halogen, C1 to 4 alkyl, C1 to 4 alkoxy, OH, CN, NO2 or NR5R6;
- said alkyl or alkoxy group being optionally further substituted by one or more fluorine atoms;
- R2 and R3 independently represent H, C1 to 4 alkyl or C3 to 6 cycloalkyl;
- said alkyl group being optionally substituted by C1 to 4 alkoxy, halogen, hydroxy, —Z—NR7 R8, phenyl or a five or six membered aromatic or saturated heterocyclic ring containing 1 to 3 heteroatoms independently selected from O, S and N;
- said phenyl or aromatic heterocyclic ring being optionally further substituted by halogen, C1 to 4 alkyl, C1 to 4 alkoxy, CF3, OCF3, OH, CN or NO2;
- Z represents —CO— or a bond;
- R5, R6, R7 and R8 independently represent H or C1 to 4 alkyl;
- R9 represents H or C1 to 4 alkyl;
- said alkyl being optionally further substituted by one or more fluorine atoms;
- or a pharmaceutically acceptable salt thereof.
19 more elements
Dependencies are inferred from the claim text.