227327-85-7Relevant academic research and scientific papers
POLYCYCLIC MOLECULAR COMPOUNDS
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Page/Page column 66-67, (2008/12/06)
This invention relates to compounds of Formula (I), wherein A is a carboaromatic or heteroaromatic ring having one or more substituents; R6 Formula (A) is optionally substituted with one or more substituents; and n is 0, 1 or an integer greater than 1 and when n is 1 or greater the bond or bonds between the carbon atoms may be saturated or unsaturated, which bind the P2X7 receptor with high affinity. This invention also relates to methods for the diagnosis, treatment or monitoring of disorders in which the P2X7 receptor is implicated, in particular the diagnosis, treatment or monitoring of (the progression of) neuroinflammatory and neurodegenerative disorders in a subject.
Cubyl amides: Novel P2X7 receptor antagonists
Gunosewoyo, Hendra,Guo, Jun Liu,Bennett, Maxwell R.,Coster, Mark J.,Kassiou, Michael
supporting information; experimental part, p. 3720 - 3723 (2009/04/06)
Polycyclic amides 2 and 5-9 were successfully synthesised and their lipophilicity profiles were evaluated using reverse-phase HPLC. All synthesised compounds possessed P2X7R antagonistic properties when tested on rat spinal cord microglia cells. Extensive screening for binding to other neuroreceptor subtypes demonstrated their P2X7 selectivity.
Discovery of potent and selective adamantane-based small-molecule P2X 7 receptor antagonists/interleukin-1β inhibitors
Furber, Mark,Alcaraz, Lilian,Bent, Janice E.,Beyerbach, Armin,Bowers, Keith,Braddock, Martin,Caffrey, Moya V.,Cladingboel, David,Collington, John,Donald, David K.,Fagura, Malbinder,Ince, Frank,Kinchin, Elizabeth C.,Laurent, Celine,Lawson, Mandy,Luker, Timothy J.,Mortimore, Michael M. P.,Pimm, Austen D.,Riley, Robert J.,Roberts, Nicola,Robertson, Mark,Theaker, Jill,Thorne, Philip V.,Weaver, Richard,Webborn, Peter,Willis, Paul
, p. 5882 - 5885 (2008/03/30)
A novel series of antagonists of the human P2X7 receptor is described. Modification of substituents enabled identification of compounds selective for the rat P2X7 receptor and provides useful pharmacological tools for evaluation of t
Hit-to-Lead studies: The discovery of potent adamantane amide P2X 7 receptor antagonists
Baxter, Andrew,Bent, Janice,Bowers, Keith,Braddock, Martin,Brough, Steve,Fagura, Malbinder,Lawson, Mandy,McInally, Tom,Mortimore, Mike,Robertson, Mark,Weaver, Richard,Webborn, Peter
, p. 4047 - 4050 (2007/10/03)
A Hit-to-Lead optimisation programme was carried out on the adamantane high throughput screening hit 1 resulting in the discovery of a number of potent P2X7 antagonists.
Adamantane derivatives
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, (2008/06/13)
The invention provides adamantane derivatives, a process for their preparation, pharmaceutical compositions containing them, a process for preparing the pharmaceutical compositions, and their use in therapy.
