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US 2005/0239774 A1Published application
Biaryl diazabicycloalkane amides as nicotinic acetylcholine agonists
OwnerGlen Ernst, Eifion Phillipsinventors
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Abstract
Acetylcholine receptor ligands of formula I wherein A, D, Ar1, E and Ar2 are as described in the specification, diastereoisomers, enantiomers, pharmaceutically-acceptable salts, methods of making, pharmaceutical compositions containing and methods for using the same.
Claims21
A compound of formula I:
- wherein:
- A is a moiety of formula II:
- D is oxygen or sulfur;
- E is a single bond, oxygen, sulfur, or NR3;
- Ar1 is a 5- or 6-membered aromatic heterocyclic ring having 1, 2 or 3 heteroatoms selected from nitrogen, oxygen or sulfur where not more than one of said heteroatoms is oxygen or sulfur, or
- Ar1 is phenyl;
- Ar2 is a 5- or 6-membered aromatic heterocyclic ring having 1, 2 or 3 heteroatoms selected from nitrogen, oxygen or sulfur where not more than one of said heteroatoms is oxygen or sulfur, or
- Ar2 is phenyl, or
- Ar2 is an 8- or 9-, or 10-membered fused aromatic carbocyclic ring or fused aromatic heterocyclic ring having 1, 2 or 3 heteroatoms selected from nitrogen, oxygen or sulfur where not more than one of said heteroatoms is oxygen or sulfur, or an 8- or 9-, or 10-membered aromatic carbocyclic ring;
- the rings Ar1 and Ar2 are substituted with 0, 1, 2 or 3 substituents selected from:
- halogen, C1-4alkyl, C2-4alkenyl, C2-4alkynyl, CN, NO2, CF3NR1R2, CH2NR1R2, OR2, CH2OR2 or CO2R3;
- R1 and R2 at each occurrence are independently selected from hydrogen, C1-4alkyl, aryl, heteroaryl, C(O)R3, C(O)NHR3, CO2R3 or SO2R3, or
- R1 and R2 in combination is —(CH2)jG(CH2)k— wherein G is oxygen, sulfur, NR3, or a bond;
- a, b and c are each 1 or 2;
- j is 2, 3 or 4;
- k is 0, 1 or 2, and
- R3 at each occurrence is independently selected from hydrogen, C1-4alkyl, aryl, or heteroaryl;
- or a diastereoisomer, enantiomer or pharmaceutically-acceptable salt thereof.
15 more elements
16-18. (canceled)
A compound of formula VI:
- wherein:
- Ar1 is a benzene, furan, or thiophene ring;
- J is halogen, or OSO2CF3, provided that when Ar1 is a benzene ring, J may only represent halogen or OSO2CF3 in a position meta or para to the carboxamide group;
- or an enantiomer thereof or pharmaceutically-acceptable salts thereof.
1 more element
Dependencies are inferred from the claim text.