183247-69-0Relevant academic research and scientific papers
CYCLIC AMINE DERIVATIVES AS EP4 RECEPTOR ANTAGONISTS
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Paragraph 0352; 0353; 0354; 0355, (2015/03/31)
There is described a novel group of cyclic amine derivative compounds, having an EP4 receptor antagonistic activity and specifically pharmaceutical compounds which are useful for the treatment or alleviation of Prostaglandin E mediated diseases. The present invention therefore relates to novel compounds which are selective antagonists of the EP4 subtype of PGE2 receptors with analgesic and antinflammatory activity, processes for their preparation, pharmaceutical compositions containing them and their use as medicaments, inter alia for the treatment or alleviation of Prostaglandin E mediated diseases such as acute and chronic pain, osteoarthritis, inflammation-associated disorder as arthritis, rheumatoid arthritis, cancer, migraine and endometriosis.
CYCLIC AMINE DERIVATIVES AS EP4 RECEPTOR ANTAGONISTS
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Page/Page column 42; 43, (2013/03/26)
There is described a novel group of cyclic amine derivative compounds, having an EP4 receptor antagonistic activity and specifically pharmaceutical compounds which are useful for the treatment or alleviation of Prostaglandin E mediated diseases. The present invention therefore relates to novel compounds which are selective antagonists of the EP 4 sub type of PGE2 receptors with analgesic and antinflammatory activity, processes for their preparation, pharmaceutical compositions containing them and theiruse as medicaments, inter alia for the treatment or alleviation of Prostaglandin E mediated diseases such as acute and chronic pain, osteoarthritis, inflammation-associated disorder as arthritis, rheumatoid arthritis, cancer, migraine and endometriosis.
Aziridine-allylsilane-mediated synthesis of exocyclic γ-amino olefins and azabicyclo[x.y.1]-systems
Lapinsky, David J,Bergmeier, Stephen C
, p. 7109 - 7117 (2007/10/03)
We have shown that connection of C-2 of an allylsilane to a tethered aziridine ring yields exocyclic γ-amino olefins and desilylated azabicyclo[x.2.1]-systems upon cyclization with BF3·OEt2. Furthermore, manipulation of a specific exocyclic γ-amino olefin provided access to an azabicyclo[3.3.1]nonane. This methodology should be useful for the preparation of natural products and pharmacologically active agents containing these bicyclic heterocyclic systems.
A Suzuki cross-coupling route to substituted aziridines
Lapinsky, David J,Bergmeier, Stephen C
, p. 8583 - 8586 (2007/10/03)
We have shown that the Suzuki cross-coupling reaction of olefinic aziridines is an effective route for the synthesis of substituted aziridines. This is the first example of a palladium coupling reaction applied to an aziridine-containing molecule. This method is complementary to other methods of aziridine synthesis utilizing organocuprate reagents.
