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US 2010/0075985 A1Published application
Benzo[d]isoxazol-3-yl-piperazin derivatives useful as modulators of dopamine d3 receptors
AssigneeHoffman-La Roche Inc.
InventorsKimberly J. Prior, Georg Jaeschke, Rosa Maria Rodriguez Sarmiento, Lucinda Steward
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Abstract
The present invention provides compounds of the general formula (I), having affinity and selectivity for the dopamine D3 receptors, their manufacture, pharmaceutical compositions containing them and their use for the therapeutic and/or prophylactic treatment of cognitive disorders.
Claims59
A compound of formula (I):
- wherein:
- X is independently fluorine or chlorine;
- n is 1 or 2;
- Z is —NH— or —O—;
- R is C1-6-alkyl, wherein C1-6-alkyl is optionally substituted by —CONH2, 3 to 6 membered monocyclic cycloalkyl or 4 to 6 membered monocyclic heterocycloalkyl;
- C1-6-hydroxyallyl;
- C1-6-alkoxy;
- 3 to 6 membered monocyclic cycloalkyl;
- or
- 4 to 6 membered monocyclic heterocycloalkyl;
- wherein 3 to 6 membered monocyclic cycloalkyl and 4 to 6 membered monocyclic heterocycloalkyl are optionally substituted by one or more substituents selected from the group consisting of halo, hydroxy, C1-6-alkyl, C1-6-haloalkyl, C1-6-hydroxyalkyl and C1-6-alkoxy;
- or a pharmaceutically acceptable salt thereof.
9 more elements
A pharmaceutical composition comprising a therapeutically effective amount of a compound of formula I
- wherein:
- X is independently fluorine or chlorine;
- n is 1 or 2;
- Z is —NH— or —O—;
- R is C1-6-alkyl, wherein C1-6-allyl is optionally substituted by —CONH2, 3 to 6 membered monocyclic cycloalkyl or 4 to 6 membered monocyclic heterocycloalkyl;
- C1-6-hydroxyalkyl;
- C1-5-alkoxy;
- 3 to 6 membered monocyclic cycloalkyl;
- or
- 4 to 6 membered monocyclic heterocycloalkyl;
- wherein 3 to 6 membered monocyclic cycloalkyl and 4 to 6 membered monocyclic heterocycloalkyl are optionally substituted by one or more substituents selected from the group consisting of halo, hydroxy, C1-6-alkyl, C1-6-haloalkyl, C1-6-hydroxyallyl and C1-6-alkoxy;
- or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier.
9 more elements
Dependencies are inferred from the claim text.