The design and synthesis of non-peptide ligands with affinity and selectivity for tachykinin receptors
2,4-disubstituted morpholin-3-one based ligands which show affinity for tachykinin receptors have been designed and synthesised. Variation of the side chains attached to the central template gives rise to selectivity between receptor subtypes. This select
Horwell, David C.,Morrell, Andrew I.,Roberts, Edward
5-MEMBERED HETEROARYLAMINOSULFONAMIDES FOR TREATING CONDITIONS MEDIATED BY DEFICIENT CFTR ACTIVITY
The invention relates to heteroaryl compounds, pharmaceutically acceptable salts thereof, and pharmaceutical preparations thereof. Also described herein are compositions and the use of such compounds in methods of treating diseases and conditions mediated by deficient CFTR activity, in particular cystic fibrosis.
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Page/Page column 442
(2021/05/21)
Efficient synthesis of substituted piperazinones via tandem reductive amination-cyclization
A new strategy for the preparation of substituted piperazinones features a tandem reductive coupling and S(N)2-cyclization of a 2-chloro-N-(2-oxoalkyl)acetamide (1) and a primary amine (2). The method is convenient for diversity-oriented synthesis, since a wide variety of amines may be used in the ring-forming reaction to produce N-substituted piperazinones (3). (C) 2000 Published by Elsevier science Ltd.
Dinsmore,Zartman
p. 6309 - 6312
(2007/10/03)
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