- AMINOTETRALIN COMPOUNDS AS MU OPIOID RECEPTOR ANTAGONISTS
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The invention provides aminotetralin compounds of formula (I): wherein R1, R2, R3, R4, R5, R6, R7, n, and m are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.
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Page/Page column 20
(2009/06/27)
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- Synthesis of 2,5-thiazole butanoic acids as potent and selective αvβ3 integrin receptor antagonists with improved oral pharmacokinetic properties
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We describe a series of 2,5 thiazole containing compounds, which are potent antagonists of the integrin αvβ3 and show selectivity relative to the other integrins, such as αIIbβ 3 and αvβ6. These analogs were demonstrated to have high bioavailability relative to other relative heterocyclic analogs.
- Wendt, John A.,Wu, Hongwei,Stenmark, Heather G.,Boys, Mark L.,Downs, Victoria L.,Penning, Thomas D.,Chen, Barbara B.,Wang, Yaping,Duffin, Tiffany,Finn, Mary Beth,Keene, Jeffery L.,Engleman, V. Wayne,Freeman, Sandra K.,Hanneke, Melanie L.,Shannon, Kristen E.,Nickols, Maureen A.,Steininger, Christina N.,Westlin, Marissa,Klover, Jon A.,Westlin, William,Nickols, G. Allen,Russell, Mark A.
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p. 845 - 849
(2007/10/03)
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- Enzymatic desymmetrization of 3-arylglutaric acid anhydrides
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Optically active (R)- and (S)-3-arylglutaric acid monoesters 3 were synthesized in quantitative yields and good stereoselectivities by lipase-catalyzed desymmetrization of the corresponding 3-arylglutaric anhydrides 2 with alcohols. It was observed that the stereochemical outcome of the reaction was influenced by the substituents present on the aromatic ring. The influence of the enzyme, alcohol, and solvent was systematically examined. Absolute configurations of the monoesters 3 were assigned by chemical correlation to corresponding lactones 4.
- Fryszkowska, Anna,Komar, Marta,Koszelewski, Dominik,Ostaszewski, Ryszard
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p. 2475 - 2485
(2007/10/03)
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- One-pot enzymatic desymmetrization and Ugi MCR
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A new approach to the synthesis of chiral peptidomimetics is reported. It combines an enzymatic desymmetrization of 3-phenylglutaric anhydrides with a subsequent Ugi multi-component reaction in a one-pot, two-step procedure. NMR and CD spectroscopy was used to assign the configurations of obtained products. Our synthetic method is very efficient and it can easily be extended to other types of multi-component reactions and can be used for the preparation of chiral peptidomimetic libraries.
- Fryszkowska, Anna,Frelek, Jadwiga,Ostaszewski, Ryszard
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p. 6064 - 6072
(2007/10/03)
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