| 摘要 |
The present invention relates to 3-substituted-2-(arylalkyl)-1-azabicycloalkanes of formula:pharmaceutically acceptable salts thereof, wherein: m is 2 and n is 1 and p is 1; X is oxygen or NR', Y is oxygen or sulfur, Z is NR', a covalent bond or a linker species A, A is -CR'= CR'-, wherein when Z is a covalent bond or A, X must be NR' nitrogen, Ar is an unsubstituted or substituted, comprising: phenyl, pyridinyl, thienyl, pyrrolyl, indolyl, benzimidazolyl, benzothiephenyl, benzofuranyl, naphthofuranyl, naphthalenyl; Cy is pyridinyl. The invention also relates to said compounds, radiolabelled, pharmaceutical compositions comprising said compounds, pharmaceutical and diagnostic compositions, comprising radiolabelled compounds, use of such compositions for diagnosis of CNS disorders or for monitoring in patients subtypes of selective nicotinic receptors and to methods of treatment using said compounds.The compounds exhibit activity at nicotinic acetylcholine receptors (nAChRs), particularly the a7 nAChR subtype, and are useful towards modulating neurotransmission and the release of ligands involved in neurotransmission. Methods for preventing or treating conditions and disorders, including central nervous system (CNS) disorders, which are characterized by an alteration in normal neurotransmission, are also disclosed. Also disclosed are methods for treating inflammation, autoimmune disorders, pain and excess neovascularization, such as that associated with tumor growth. |
