IP Library Granted Patent US 8,173,669
Granted Patent B2
US 8,173,669 · App. 12/535,156 · Granted May 8, 2012

Azabicycloalkane derivatives, preparation thereof and use thereof in therapy

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Quick Facts
Patent No.
US 8,173,669
App. No.
12/535,156
Granted
May 8, 2012
Kind
B2
Abstract

The invention relates to compounds of the general formula (I): Wherein R, m, n and o are as defined herein. The invention also relates to a method for preparing the same and to the application in therapy.

Claims (31)

1. A compound of the formula (I):

in which:

R represents hydrogen, halogen, hydroxyl, (C 1 -C 6 )alkoxy, (C 3 -C 7 )cycloalkyl-O—, (C 3 -C 7 )cycloalkyl-(C 1 -C 3 )alkylene-O—,

or a heterocycloalkyl, aryl or heteroaryl group; wherein said group is optionally substituted by one or more groups chosen from halogen, (C 1 -C 6 )alkyl, (C 3 -C 7 )cycloalkyl, (C 3 -C 7 )cycloalkyl-(C 1 -C 3 )alkylene, (C 1 -C 6 )alkoxy, (C 3 -C 7 )cycloalkyl-O—, (C 3 -C 7 )cycloalkyl-(C 1 -C 3 )alkylene-O—, (C 1 -C 6 )fluoroalkyl, (C 1 -C 6 )fluoroalkoxy, nitro, cyano, hydroxyl, amino, (C 1 -C 6 )alkylamino, di(C 1 -C 6 )alkylamino, heterocycloalkyl, aryl, aryl-(C 1 -C 6 )alkylene, heteroaryl, heteroaryl-(C 1 -C 6 )alkylene, aryl-O— or —C(O)—(C 1 -C 6 )alkyl groups, the heterocycloalkyl group optionally being substituted by —C(O)O(CH 3 ) 3 ;

n represents 1;

m represents 1; and

o represents 1;

or a salt thereof; and

with the proviso that when n and o are 1 m is not 2; and

the following compounds are excluded:

4-(6-fluoropyridin-3-yl)-1-azabicyclo[2.2.1]heptane;

4-(6-chloropyridin-3-yl)-1-azabicyclo[2.2.1]heptane;

4-(6-bromopyridin-3-yl)-1-azabicyclo[2.2.1]heptane;

4-(pyridin-3-yl)-1-azabicyclo[2.2.1]heptane.

2. The compound of formula (I) according to claim 1 , wherein:

R represents hydrogen, halogen, hydroxyl,

or a heterocycloalkyl, aryl or heteroaryl group; wherein said group is optionally substituted by one or more groups chosen from halogen, (C 1 -C 6 )alkyl, (C 1 -C 6 )alkoxy, (C 1 -C 6 )fluoroalkyl, (C 1 -C 6 )fluoroalkoxy, nitro, cyano, hydroxyl, amino, (C 1 -C 6 )alkylamino, di(C 1 -C 6 )alkylamino, heterocycloalkyl, aryl, aryl-(C 1 -C 6 )alkylene, heteroaryl, aryl-O— or —C(O)—(C 1 -C 6 )alkyl groups, the heterocycloalkyl group optionally being substituted by —C(O)O(CH 3 ) 3 ;

n represents 1;

m represents 1; and

o represents 1;

or a salt thereof.

3. The compound of formula (I) according to claim 1 , wherein:

R represents halogen, hydroxyl,

or a heterocycloalkyl group or an aryl group or a heteroaryl group; wherein said group is optionally substituted by one or more groups chosen from halogen, (C 1 -C 6 )alkyl, (C 1 -C 6 )alkoxy, (C 1 -C 6 )fluoroalkyl, (C 1 -C 6 )fluoroalkoxy, di(C 1 -C 6 )alkylamino, heterocycloalkyl, aryl, aryl-(C 1 -C 6 )alkylene, heteroaryl, aryl-O— or —C(O)—(C 1 -C 6 )alkyl groups; the heterocycloalkyl group optionally being substituted by —C(O)O(CH 3 ) 3 ;

n represents 1;

m represents 1; and

o represents 1;

or a salt thereof.

4. A pharmaceutical composition comprising a compound of formula (I) according to claim 1 or a pharmaceutically acceptable salt thereof and at least one pharmaceutically acceptable excipient.

5. A pharmaceutical composition comprising a compound of formula (I) according to claim 2 or a pharmaceutically acceptable salt thereof and at least one pharmaceutically acceptable excipient.

6. A pharmaceutical composition comprising a compound of formula (I) according to claim 3 or a pharmaceutically acceptable salt thereof and at least one pharmaceutically acceptable excipient.

Assignments (2)
CHANGE OF NAME Recorded Jun 20, 2012
From: SANOFI-AVENTIS
To: SANOFI
Reel/Frame 028413/0927 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 28, 2010
From: BEN AYAD, OMAR; LECLERC, ODILE; LOCHEAD, ALISTAIR; SAADY, MOURAD; SLOWINSKI, FRANCK; VACHE, JULIEN
To: SANOFI-AVENTIS
Reel/Frame 023866/0046 →