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US 7,678,807 B2Granted
Isoquinoline and benzo[H] isoquinoline derivatives, preparation and therapeutic use thereof as antagonists of the histamine H3 receptor
AssigneeSanofi-Aventis
InventorsJuan Antonio Diaz Martin, Beatriz Escribano Arenales, Maria Dolores Jimenez Bargueno
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Abstract
The invention concerns a compound of formula (I): Wherein A, l, m, n, R1 and R2 are as defined herein. The compounds of this invention are useful as medicaments, particularly, in the treatment of disorders improved by modulation of the histamine H3 receptor.
Claims18
A compound of formula (I):
- wherein:
- represents a 6-membered unsaturated carbocycle with double bonds which is optionally substituted by one or two substituents chosen, independently of one another, from a halogen atom, a hydroxyl, a nitro, cyano, C1-2 perhaloalkyl or C1-3 alkyl group or a phenyl;
- 1 is 0 to 2;
- m is 0 to 2;
- wherein the aminocycle comprising —(C)l—, —(C)m— and —NR1- forms a pyrrolidine;
- n is 0 to 6;
- —(C)l—, —(C)m— and —(C)n— represent, independently of one another, a —Cx-z— alkylene group, optionally substituted by 1 to 4 substituents chosen from a halogen atom, a hydroxyl, nitro, cyano, amino, C1-2 perhaloalkyl or C1-3 alkyl group or a phenyl;
- and when l, m and n are 0, —(C)0— represents a bond;
- R1 represents
- a hydrogen atom,
- a C1-3 alkyl group,
- a C1-6 alkylcarbonyl,
- a C1-6 alkoxycarbonyl,
- it being possible for each to be substituted by a halogen atom, a hydroxyl, C1-3 alkoxy, nitro, cyano or amino group or aryl;
- a C1-3 alkylaryl group,
- a monocyclic heteroaryl, and
- an aryl;
- the aryl and heteroaryl groups optionally being substituted by 1 to 4 substituents chosen from a halogen atom, a hydroxyl, nitro, cyano, amino, C1-3 monoalkylamino, C2-6 dialkylamino, C1-3 alkyl, C1-2 perhaloalkyl, C1-3 haloalkyl or C1-3 alkoxy group or a alkylidenedioxy group;
- and
- R2 represents
- a C1-6 alkyl group or a C3-6 cycloalkyl group, each optionally being substituted by 1 to 4 substituents chosen from a halogen atom, a hydroxyl, nitro, cyano, amino, C1-3 monoalkylamino, C2-6 dialkylamino, C1-2 perhaloalkyl, C1-3 haloalkyl, C1-3 alkoxy or C3-6 cycloalkyl group, a monocyclic heteroaryl, a bicyclic heteroaryl or an aryl group itself optionally substituted by 1 to 4 substituents chosen from a halogen atom, a hydroxyl, nitro, cyano, amino, C1-3 monoalkylamino, C2-6 dialkylamino, C1-3 alkyl, C1-2 perhaloalkyl, C1-3 haloalkyl or C1-3 alkoxy group or a C1-3 alkylidenedioxy group,
- or a salt thereof.
19 more elements
Dependencies are inferred from the claim text.