Highly potent, orally available anti-inflammatory broad-spectrum chemokine inhibitors
A series of 3-acylaminocaprolactams are inhibitors of chemokine-induced chemotaxis. Branching of the side chain α-carbon provides highly potent inhibitors of a range of CC and CXC chemokines. The most potent compound has an ED50 of 40 pM. Selec
Fox, David J.,Reckless, Jill,Lingard, Hannah,Warren, Stuart,Grainger, David J.
supporting information; experimental part
p. 3591 - 3595
(2010/03/30)
ANTI-INFLAMMATORY AGENTS
The invention relates to the use of 3-aminocaprolactam derivatives for preparing a medicament intended to prevent or treat inflammatory disorders, and uses compounds of general formula (I) or a pharmaceutically acceptable salts thereof; wherein X is -CO-R1 or-S02-R2, and R1 and R2 are carbonaceous substituents.
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Page/Page column 42
(2010/02/11)
Phosphite-Mediated in Situ Carboxyvinylation: A New General Acrylic Acid Synthesis
Sequential treatment of a 2-halo carboxylic acid with a dialkyl phosphite and an aldehyde or ketone in the presence of 3 equiv of sodium hydride in glyme constitutes a new general acrylic acid synthesis superior to conventional methods.An alkoxide-in-alcohol variant may be used with bromo- or chloroacetic acid and aryl aldehydes to produce cinnamic acids conveniently.The scope and other features of the synthesis are discussed.
Brittelli, David R.
p. 2514 - 2520
(2007/10/02)
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