NICOTINIC ACETYLCHOLINE RECEPTOR LIGANDS

Claims

1. Compound of general formula (I): or its pharmaceutically acceptable salt, Where R 1 is an optionally substituted aryl or an optionally substituted heteroaryl; and R 2 is halogen, triflate, optionally substituted aryl, optionally substituted heteroaryl, or absent; or where R 1 and R 2 together form an optionally substituted aryl or an optionally substituted heteroaryl.

2. A compound according to claim 1, wherein said one or each aryl or heteroaryl is a ring with a number of members from 5 to 10, in particular a 5-membered ring or a 6-membered ring.

3. A compound according to claim 1 or 2, wherein one or both aryl or heteroaryl groups are monocyclic.

4. The compound of claim 3, wherein one or both aryl or heteroaryl groups are independently selected from the group consisting of: phenyl, furanyl, pyrrolyl, thienyl, pyridinyl, pyrimidinyl, pyridazinyl, pyrazinyl, oxazolyl, oxadiazolyl, isoxazolyl, pyrazolyl, imidazolyl, thiazolyl, isothiazolyl, and thiadiazolyl.

5. A compound according to claim 1 or 2, wherein one or both aryl or heteroaryl groups are polycyclic.

6. The compound of claim 5, wherein one or both aryl or heteroaryl groups are independently selected from the group consisting of: naphthalenyl, anthracenyl, indolizinyl, indolyl, isoindolyl, benzofuranyl, benzothiophenyl, benzodioxolanyl, indazolyl, pyrrolopyridinyl, benzimidazolyl, benzothiazolyl, benzoisothiazolyl, purinyl, thienopyrazinyl, quinolinyl, isoquinolinyl, cinnolinyl, phthalazinyl, quinazolinyl, quinoxalinyl, 1,8-naphthyridinyl, pteridinyl, carbazolyl, acridinyl, naphthyridinyl, phenazinyl, phenothiazinyl, phenoxazinyl and azulenyl.

7. A compound according to any one of the preceding claims, wherein one or both aryl or heteroaryl groups are substituted, in particular by 1, 2 or 3 substituents, optionally the substituents being independently selected from the group consisting of: alkyl, alkenyl, heterocyclyl, cycloalkyl, aryl, substituted aryl, arylalkyl, substituted arylalkyl, halogen, in particular F, Cl, Br or I; -OR', -NR'R'', -CF3, -CN, -NO2, -SR', -N3, -C(=O)NR'R'', -NR'C(=O)R'', -C(=O)R', -C(=O)OR', -OC(=O)R', -O(CR'R''), -C(=O)R', -SO2R' and -SO2NR'R'', wherein R' and R'' individually represent hydrogen, lower alkyl, in particular straight or branched alkyl, including C1-C8, preferably C1-C5, such as methyl, ethyl or isopropyl; cycloalkyl, heterocyclyl, aryl or arylalkyl, such as benzyl, wherein R' and R'' are optionally combined to form a cyclic functional group.

8. The compound of claim 7, wherein said substituents are independently selected from the group consisting of: cyano, halogen, alkyl, haloalkyl, cycloalkyl, alkoxy, haloalkoxy, and alkylthio.

9. A compound according to any of the preceding claims, in which R 1 selected from 1,3,4-thiadiazolyl, pyridinyl, pyridazinyl, pyrimidinyl and pyrazinyl, and / or characterized in that R 2 selected from indolyl, benzofuranyl, benzothiazolyl and phenyl.

10. A compound according to any one of the preceding claims, wherein said compound is selected from the group consisting of: 4-(3-pyridyl)-1-azabicyclo[3.2.2]non-3-ene; 4-(6-phenyl-3-pyridyl)-1-azabicyclo[3.2.2]non-3-ene; And 4-(6-phenylpyridazin-3-yl)-1-azabicyclo[3.2.2]non-3-ene, in particular, the said compound is 4-(6-phenyl-3-pyridyl)-1-azabicyclo[3.2.2]non-3-ene.

11. A pharmaceutical composition comprising a compound according to any one of claims 1-10 and a pharmaceutically or therapeutically acceptable excipient or carrier.

12. A compound according to any one of claims 1 to 10 for use in the treatment of a disease or disorder.

13. A compound according to any one of claims 1 to 10 for use in the treatment of a disease or disorder mediated by the α7 nicotinic acetylcholine receptor (nAChR).

14. A compound for use according to claim 12 or 13, wherein said treatment is aimed at preventing and / or suppressing cough, progression of cough, alleviating cough symptoms and alleviating recurrence of cough.

15. A method for preparing a compound of general formula (I), as shown in scheme (I): , where R 1 and R 2 are as defined in any of paragraphs 1-14.