Back to results
US 2003/0166582 A1Published application
Aryl fused azapolycyclic compounds
AssigneePfizer Inc.
InventorsAnne E. Hagen, R. Scott Obach
Life of this patent
Estimating the term…
Abstract
This invention is directed to compounds of the formula (I): 1 and their pharmaceutically acceptable salts, wherein R1, R2, and R3 are as defined herein; intermediates for the synthesis of such compounds, pharmaceutical compositions containing such compounds; and methods of using such compounds in the treatment of nicotine addiction/withdrawal and CNS disorders.
Claims8
A compounds of formula (I)
- 19
- wherein R1 is independently hydrogen or —COOR4 wherein R4 is a group of formula
- 20
- R2 and R3, together with the benzo ring to which they are attached, form a bicyclic ring system selected from the following:
- 21
- wherein one of the carbon atoms of ring A can optionally be replaced with oxygen or N(C1-C6)alkyl;
- wherein R11 and R12 are selected, independently, from hydrogen, (C1-C6)alkyl;
- and (C1-C6)alkoxy-(C0-C6)alkyl- wherein the total number of carbon atoms does not exceed six and wherein any of the alkyl moieties may optionally be substituted with from one to seven fluorine atoms;
- nitro, cyano, halo, amino, (C1-C6)alkylamino-, ((C1-C6)alkyl)2amino-, —CO2R5, —CONR6R7, —SO2NR8R9, —C(═O)R10, —XC(═O)R11, phenyl, monocyclic heteroaryl, or when attached to a nitrogen atom, a group of formula:
- 22
- each R5, R6, R7, R8, R9 and R10 is selected, independently, from hydrogen and (C1-C6)alkyl, or
- R6 and R7, or R8 and R9 together with the nitrogen to which they are attached, form a pyrrolidine, piperidine, morpholine, azetidine, piperazine, —N—(C1-C6)alkylpiperazine or thiomorpholine ring, or a thiomorpholine ring wherein the ring sulfur is replaced with a sulfoxide or sulfone;
- and each X is, independently, (C1-C6)alkylene;
- with the proviso that when R1 is H, then at least one of R11 or R12 must be a group of formula:
- 23
- attached to a nitrogen atom in the ring formed by groups R2 and R3, and forming an ammonium ion center on that nitrogen atom if necessary to accommodate the existing bonding relationships;
- and pharmaceutically acceptable salts thereof.
14 more elements
Dependencies are inferred from the claim text.