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US 2008/0188518 A1Published application
5-Substituted Imidazoles
AssigneeAstra Zeneca AB
InventorsJames Empfield, Eifion Phillips, Scott Throner
Life of this patent
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Abstract
Compounds of formula I: wherein A and R1 are as defined in the specification, processes for preparing them, pharmaceutical compositions containing them and their use in therapy, especially in the treatment or prophylaxis of psychotic and intellectual impairment disorders.
Claims21
A compound according to formula I:
- wherein:
- A represents:
- where R represents hydrogen or methyl, and
- R1 represents hydrogen or a moiety of Formula VI
- wherein:
- Ar1 is selected from a 5- or 6-membered aromatic or heteroaromatic ring having 0, 1 or 2 nitrogen atoms, 0 or 1 oxygen atoms, and 0 or 1 sulfur atoms, or selected from an 8-, 9- or 10-membered fused aromatic or heteroaromatic ring system having 0, 1, 2 or 3 nitrogen atoms, 0 or 1 oxygen atoms, and 0 or 1 sulfur atoms;
- D is selected from hydrogen, NR2R3, or E-Ar2;
- wherein
- E is a single bond, —O—, —S—, or —NR3—;
- Ar2 is selected from a 5- or 6-membered aromatic or heteroaromatic ring having 0, 1 or 2 nitrogen atoms, 0 or 1 oxygen atoms, and 0 or 1 sulfur atoms;
- where each Ar1 or Ar2 moiety may be unsubstituted or bear 1, 2 or 3 substituents selected from —R3, —C1-C6alkyl, —C2-C6alkenyl, —C2-C6alkynyl, halogen, —CN, —NO2, —CF3, —S(O)nR3, —NR2R3, —CH2NR2R3, —OR3, —CH2OR3 or —CO2R4;
- R2 and R3 are independently selected at each occurrence from hydrogen, —C1-C4alkyl, aryl, heteroaryl, —C(O)R4, —C(O)NHR4, —CO2R4 or —SO2R4, or
- R2 and R3 in combination is —(CH2)jG(CH2)k— wherein G is oxygen, sulfur, NR4, or a bond;
- j is 2, 3 or 4;
- k is 0, 1 or 2;
- n is 0, 1 or 2, and
- R4 is independently selected at each occurrence from hydrogen, —C1-4alkyl, aryl, or heteroaryl;
- and stereoisomers, enantiomers, in vivo-hydrolysable precursors and pharmaceutically-acceptable salts thereof.
15 more elements
21-22. (canceled)
Dependencies are inferred from the claim text.