A Pd-catalyzed asymmetric allylic substitution cascade: Via an asymmetric desymmetrization for the synthesis of bicyclic dihydrofurans
A Pd-catalyzed asymmetric allylic substitution cascade of allylic meso-dicarbonates with 3-oxo-nitriles has been developed for the synthesis of chiral bicyclic dihydrofurans bearing two vicinal carbon stereocenters. The reaction proceeds via an asymmetric desymmetrization process with the desired products being obtained in high yields and with up to 97% ee. The reaction was performed on a gram-scale and the corresponding bicyclic dihydrofurans could undergo several transformations. The methodology provides an efficient synthetic route to biologically active chiral bicyclic dihydrofurans derivatives.
The instant invention provides for substituted fused naphthyridine derivatives that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer.
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(2010/10/03)
5-CYANO-2-AMINOPYRIMIDINE DERIVATIVES
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(2008/06/13)
Combinations of agents which give enhanced anti-inflammatory activity
This disclosure describes compatible additive anti-inflammatory compositions comprising certain novel anti-arthritic agents and the known non-steroidal anti-inflammatory agents.
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(2008/06/13)
β-oxo-3-thiophene propionitrile and β-amino-2-(3)-thiophene acrylonitriles
This disclosure describes new compounds and compositions of matter useful as anti-inflammatory agents and as inhibitors of the progressive joint deterioration characteristic of arthritic disease and the methods of meliorating inflammation and of inhibiting joint deterioration in mammals therewith, the active ingredients of said compositions of matter being β-oxo-3-thiophenepropionitrile, β-amino-2-thiopheneacrylonitrile, and/or β-amino-3-thiopheneacrylonitrile.
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(2008/06/13)
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