- ORALLY AVAILABLE SPHINGOSINE 1-PHOSPHATE RECEPTOR AGONISTS AND ANTAGONISTS
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The present invention relates to S1P analogs that have activity as S1Preceptor modulating agents and the use of such compounds to treat diseases associated with inappropriate S1P receptor activity. The compounds have the general structure (I) wherein R11 is C5-C18 alkyl or C5-C18 alkenyl; Q is selected from the group consisting of C3-C6 optionally substituted cycloalkyl, C3-C6 optionally substituted heterocyclic, C3-C6 optionally substituted aryl C3-C6 optionally substituted heteroaryl and; R2 is selected from the group consisting of H, C1-C4 alkyl, (C1-C4 alkyl)OH and (C1-C4 alkyl)NH2; R23 is H or C1-C4 alkyl, and R15 is a phosphonate ester or a phosphate ester or a pharmaceutically acceptable salt or tautomer thereof.
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Page/Page column 114; 115
(2008/06/13)
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- Synthesis of benzimidazole based analogues of sphingosine-1-phosphate: Discovery of potent, subtype-selective S1P4 receptor agonists
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We report the synthesis and potencies of several selective S1P4 receptor agonists. Sphingosine-1-phosphate (S1P) is a biologically active lysophospholipid with the capacity to induce a broad range of cellular responses via its interaction with
- Clemens, Jeremy J.,Davis, Michael D.,Lynch, Kevin R.,Macdonald, Timothy L.
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p. 4903 - 4906
(2007/10/03)
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- Nouveaux diamino-3,4 phenylalcanes et leur transformation en benzimidazolemethanethiols-2
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We report five o-phenylenediamines which are substituted by an aliphatic chain containing n carbon atoms (n = 4, 6, 8, 10, 12).We describe a well adapted general synthetic method using Schmidt's reaction.The diamines were then transformed into 2-benzimidazolemethanethiols and their related S-methyl derivatives which structures were checked by (1)H NMR.
- Krati, Noureddine,Roizard, Denis,Brembilla, Alain,Lochon, Pierre
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p. 443 - 448
(2007/10/02)
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