Novel diazabicyclic aryl derivatives
AssigneeNeuroSearch A/S
InventorsDan Peters, Elsebet Nielsen, Tino Jorgensen, Philip Ahring
Life of this patent
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Abstract
This invention relates to novel diazabicyclic aryl derivatives which are found to be cholinergic ligands at the nicotinic acetylcholine receptors. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.
Claims30
A diazabicyclic aryl derivative represented by Formula I
- any of its enantiomers or any mixture of its enantiomers, or a prodrug, or a pharmaceutically-acceptable addition salt thereof, wherein
- n is 1, 2 or 3;
- and
- X and Y, independently of one another, represents CR2, CR3 and/or N, wherein R2 and R3, independently of one another, represent hydrogen, alkyl, cycloalkyl, cycloalkyl-alkyl, hydroxy, alkoxy, cycloalkoxy, cyanoalkyl, halo, haloalkyl, haloalkoxy, cyano, amino, nitro, aryl, aryloxy, aryl-alkyl, heteroaryl and/or heteroaryloxy, which aryl, aryloxy, aryl-alkyl, heteroaryl and heteroaryloxy may optionally be substituted one or two times with halo, haloalkyl, haloalkoxy, cyano, amino, nitro and/or a group of the formula R′CONH—, wherein R′ represents hydrogen or alkyl;
- and
- R1 represents
- hydrogen, alkyl, cycloalkyl, cycloalkyl-alkyl, hydroxy, alkoxy, cycloalkoxy, cyanoalkyl, halo, haloalkyl, haloalkoxy, cyano, amino, nitro, aryl or heteroaryl, which aryl or heteroaryl may optionally be substituted one or two times with alkyl, halo, haloalkyl, alkoxy, haloalkoxy, cyano, amino, nitro and/or a group of the formula R′CONH—, R′SO2NH— or (R′SO2)2N—, wherein R′ represents hydrogen, alkyl, cycloalkyl, haloalkyl, alkenyl, phenyl or benzyl;
- or
- a group of formula aryl-alkyl-, aryl-Z-(alkyl)m—, aryl-C≡C—, heteroaryl-Z-(alkyl)m— or heteroaryl-C≡C—, wherein
- m is 0 or 1;
- and
- Z represents O or S;
- and wherein the aryl and heteroaryl may optionally be substituted one or two times with alkyl, halo, haloalkyl, hydroxy, alkoxy, haloalkoxy, cyano, amino, nitro and/or a group of the formula R′CONH—, R′SO2NH— or (R′SO2)2N—, wherein R′ represents hydrogen or alkyl;
- or
- R1 and R2, or R1 and R3, together with the carbon atoms to which they are bound, form a benzo-fused aromatic carbocyclic ring, which benzo-fused aromatic carbocyclic ring may optionally be substituted one or two times with alkyl, cycloalkyl, cycloalkyl-alkyl, hydroxy, alkoxy, cycloalkoxy, cyanoalkyl, halo, haloalkyl, haloalkoxy, cyano, amino, nitro and/or a group of the formula R′CONH—, wherein R′ represents hydrogen or alkyl.
(canceled)
Dependencies are inferred from the claim text.