8-Azabicyclo[3.2.1]octane derivatives
AssigneeN.V. Organon
InventorsSusan Napier, Matilda Bingham, Neil Dunbar
Life of this patent
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Abstract
The present invention relates to a 8-azabicyclo[3.2.1]octane derivative of Formula I, wherein each of the substituents is given the definition as set forth in the specification and claims, or a pharmaceutically acceptable salt thereof or solvate thereof. The present invention also relates to a pharmaceutical composition comprising an 8-azabicyclo[3.2.1]octane derivative in admixture with one or more pharmaceutically acceptable auxiliaries and to the use of the 8-azabicyclo[3.2.1]octane derivative in therapy.
Claims11
A 8-azabicyclo[3.2.1]octane derivative of Formula I,
- wherein
- R1 is H or C1-5alkyl;
- Y is O, S or O(CH2)m;
- m is 1 or 2;
- n is 0 or 1;
- Ar1 is phenylene or pyridylene, said phenylene and pyridylene being 1,3-linked with respect to O and when n is 1 with Y and when n is 0 with Ar2,said phenylene or pyridylene being optionally substituted with one or two substituents independently selected from halogen, C1-5alkyl, C1-5alkoxy, C3-6cycloalkyl, C2-5alkenyl, C2-5alkynlphenyl, CN and hydroxy, wherein said C1-5alkyl and C1-5alkoxy are optionally substituted with one to three halogens and wherein the oxygen of said hydroxy is optionally bonded to Ar2 to form a 5-membered ring;
- Ar2 is phenyl or a 5-6 membered heteroaryl, said phenyl or 5-6 membered heteroaryl being optionally substituted with one to three substituents independently selected from halogen, C1-5alkyl, C1-5alkoxy, CN, CONR2R3, CO2R4, NHCOR5 and hydroxy, wherein said C1-5alkyl and C1-5alkoxy are optionally substituted with one to three halogens and wherein the oxygen of said hydroxy is optionally bonded to Ar1 to form a 5-membered ring;
- R2-R4 are independently H or C1-5alkyl and
- R5 is C1-5alkyl
- or a pharmaceutically acceptable salt or solvate thereof.
A 8-azabicyclo[3.2.1]octane derivative selected from:
- 3-exo-(5-chlorobiphenyl-3-yloxy)-8-azabicyclo[3.2.1]octane;
- exo 5-(8-azabicyclo[3.2.1]oct-3-yloxy)biphenyl-3-carbonitrile;
- exo 3-(8-azabicyclo[3.2.1]oct-3-yloxy)-5-phenoxybenzonitrile;
- 3-exo-(4′-methoxybiphenyl-3-yloxy)-8-azabicyclo[3.2.1]octane;
- exo 3′-(8-azabicyclo[3.2.1]oct-3-yloxy)biphenyl-4-carbonitrile;
- 3-exo-(3-pyridin-4-ylphenoxy)-8-azabicyclo[3.2.1]octane;
- exo 2-{6-(8-azabicyclo[3.2.1]oct-3-yloxy)-4-chloropyridin-2-yl}benzonitrile;
- exo 2-(8-azabicyclo[3.2.1]oct-3-yloxy)-6-(2-cyanophenyl)isonicotinonitrile;
- exo 3-[(8-azabicyclo[3.2.1]oct-3-yl)oxy]-5-(3-chloropyridin-2-yl)benzonitrile;
- exo 3-(8-azabicyclo[3.2.1]oct-3-yloxy)-5-cyanophenyl)nicotinonitrile;
- exo 3-(8-azabicyclo[3.2.1]oct-3-yloxy)-5-(3-fluoropyridin-2-yl)benzonitrile;
- exo 3′-(8-azabicyclo[3.2.1]oct-3-yloxy)biphenyl-2-carbonitrile;
- exo 2-[6-(8-azabicyclo[3.2.1]oct-3-yloxy)pyridin-2-yl]benzonitrile;
- 3′-(8-azabicyclo[3.2.1]oct-3-exo-yloxy)-2′-fluorobiphenyl-4-carbonitrile and
- 2-(8-azabicyclo[3.2.1]oct-3-exo-yloxy)-6-phenylisonicotinonitrile
- or a pharmaceutically acceptable salt or solvate thereof.
Dependencies are inferred from the claim text.