abstract |
The present invention relates to 3-substituted-2- (arylalkyl) -1-azabicycloalkanes of the formula their pharmaceutically acceptable salts, where m is 2 and n is 1, p is 1; X is oxygen or NR ', Y is oxygen or sulfur, Z is NR', a covalent bond or linker moiety A, A is -CR '= CR'- where, if Z is a covalent bond or A, X should be NR' , Ar is an unsubstituted or substituted group including phenyl, pyridinyl, thienyl, pyrrolyl, indolyl, benzimidazolyl, benzothiophenyl, benzofuranyl, naphthofuranyl, naphthalenyl; Cy is pyridinyl. The invention also relates to said compounds labeled with a radioactive isotope, pharmaceutical compositions containing said compounds, pharmaceutical and diagnostic compositions containing labeled with a radioactive isotope, the use of such compositions for diagnosing a disease of the central nervous system or for monitoring a patient's subtypes of selective nicotinic receptors and methods treatments using these compounds. The compounds affect nicotinic acetylcholine receptors (nAChRs), especially the nAChR α7 subtype, and can be used to modulate neurotransmission and release ligands involved in neurotransmission. Also disclosed is the use of these compounds in the treatment of conditions and diseases, including diseases of the central nervous system (CNS), which are characterized by a change in normal neurotransmission, as well as in the treatment of inflammation, autoimmune diseases, pain and excessive revascularization, such as revascularization associated with tumor growth . |