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Claims for Patent: 6,756,393

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Claims for Patent: 6,756,393

Title: Azacyclic compounds
Abstract:Compounds and methods are provided for the treatment of disease conditions in which modification of serotonergic receptor activity has a beneficial effect. In the method, an effective amount of a compound is adminstered to a patient in need of such treatment.
Inventor(s): Andersson; Carl-Magnus A. (Glostrup, DK), Croston; Glenn (San Diego, CA), Hansen; Eva L. (Glostrup, DK), Uldam; Allan Kjaersgaard (Glostrup, DK)
Assignee: Acadia Pharmaceuticals, Inc. (San Diego, CA)
Application Number:10/409,782
Patent Claims: 1. A compound of formula (I) ##STR10##

wherein Z is ##STR11## wherein R is a lower alkyl group, wherein said lower alkyl group is a methyl; and n is 1; X.sub.1 is methylene, vinylene, or an NH or N(lower alkyl) group; and X.sub.2 is methylene; or, when X.sub.1 is methylene or vinylene, X.sub.2 is methylene or a bond; or when X.sub.1 is methylene, X.sub.2 is O, S, NH, or N(lower alkyl) or a bond; Y.sub.1 is methylene and Y.sub.2 is methylene, vinylene, ethylene, propylene, or a bond; or Y.sub.1 is a bond and Y.sub.2 is vinylene; or Y.sub.1 is ethylene and Y.sub.2 is O, S, NH, or N(lower alkyl); Ar.sub.1 and Ar.sub.2 independently are unsubstituted or substituted aryl or heteroaryl groups, provided that Ar.sub.1 and Ar.sub.2 are not simultaneously unsubstituted phenyl; and W is oxygen; or a pharmaceutically acceptable salt or prodrug thereof.

2. A compound of formula (I) ##STR12##

wherein Z is ##STR13## wherein R is a hydrogen, a cyclic or straight-chained or branched acyclic organyl group, a lower hydroxyalkyl group, a lower aminoalkyl group, or an aralkyl or heteroaralkyl group; and n is 1; X.sub.1 is an NH, and X.sub.2 is methylene; Y.sub.1 is methylene and Y.sub.2 is methylene, vinylene, ethylene, propylene, or a bond; or Y.sub.1 is a bond and Y.sub.2 is vinylene; or Y.sub.1 is ethylene and Y.sub.2 is O, S, NH, or N(lower alkyl); Ar.sub.1 and Ar.sub.2 independently are unsubstituted or substituted aryl or heteroaryl groups, provided that Ar.sub.1 and Ar.sub.2 are not simultaneously unsubstituted phenyl; and W is oxygen; or a pharmaceutically acceptable salt or prodrug thereof.

3. A compound of formula (I) ##STR14##

wherein Z is ##STR15## wherein R is a hydrogen, a cyclic or straight-chained or branched acyclic organyl group, a lower hydroxyalkyl group, a lower aminoalkyl group, or an aralkyl or heteroaralkyl group; and n is 1; X.sub.1 is methylene, vinylene, or an NH or N(lower alkyl) group; and X.sub.2 is methylene, or, when X.sub.1 is methylene or vinylene, X.sub.2 is methylene or a bond; or when X.sub.1 is methylene, X.sub.2 is O, S, NH, or N(lower alkyl) or a bond; Y.sub.1 is methylene and Y.sub.2 is a bond; Ar.sub.1 and Ar.sub.2 independently are unsubstituted or substituted aryl or heteroaryl groups, provided that Ar.sub.1 and Ar.sub.2 are not simultaneously unsubstituted phenyl; and W is oxygen; or a pharmaceutically acceptable salt or prodrug thereof.

4. A compound of formula (I) ##STR16##

wherein Z is ##STR17## wherein R is a hydrogen, a cyclic or straight-chained or branched acyclic organyl group, a lower hydroxyalkyl group, a lower aminoalkyl group, or an aralkyl or heteroaralkyl group; and n is 1; X.sub.1 is methylene, vinylene, or an NH or N(lower alkyl) group; and X.sub.2 is methylene, or, when X.sub.1 is methylene or vinylene, X.sub.2 is methylene or a bond; or when X.sub.1 is methylene, X.sub.2 is O, S, NH, or N(lower alkyl) or a bond; Y.sub.1 is methylene and Y.sub.2 is methylene, vinylene, ethylene, propylene, or a bond; or Y.sub.1 is a bond and Y.sub.2 is vinylene; or Y.sub.1 is ethylene and Y.sub.2 is O, S, NH, or N(lower alkyl); Ar.sub.1 is a 4-haloaryl, wherein said aryl is phenyl and said halo is a fluoro; Ar.sub.2 is a 4-substituted aryl, wherein said aryl is phenyl, and said phenyl is substituted with a lower alkoxy group, wherein the alkyl group of said lower alkoxy group is an isobutyl; and W is oxygen; or a pharmaceutically acceptable salt or prodrug thereof.

5. A tartrate salt of a compound of formula (I) ##STR18##

wherein Z is ##STR19## wherein R is a hydrogen, a cyclic or straight-chained or branched acyclic organyl group, a lower hydroxyalkyl group, a lower aminoalkyl group, or an aralkyl or heteroaralkyl group; and n is 1; X.sub.1 is methylene, vinylene, or an NH or N(lower alkyl) group; and X.sub.2 is methylene, or, when X.sub.1 is methylene or vinylene, X.sub.2 is methylene or a bond; or when X.sub.1 is methylene, X.sub.2 is O, S, NH, or N(lower alkyl) or a bond; Y.sub.1 is methylene and Y.sub.2 is methylene, vinylene, ethylene, propylene, or a bond; or Y.sub.1 is a bond and Y.sub.2 is vinylene; or Y.sub.1 is ethylene and Y.sub.2 is O, S, NH, or N(lower alkyl); Ar.sub.1 and Ar.sub.2 independently are unsubstituted or substituted aryl or heteroaryl groups, provided that Ar.sub.1 and Ar.sub.2 are not simultaneously unsubstituted phenyl; and W is oxygen.
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