Children's Medical Center Corporation

Celgene Corporation

Glenn M Swartz

Robert J D'Amato

Jamshed H Shah

Anthony Treston

Kimberly A Hunsucker

John Rougas

Barry P Conner

Victor Pribdula

Shawn J Green

Adonia E Papathanassiu

John W Madsen

William E Fogler

Victor S Pribluda

Robert J D'amato

Victor Pribluda

The invention provides new and useful analogs of 4-amino-thalidomide. These analogs include S(&#x2212;)-4-amino-thalidomide and R(+)-4-amino-thalidomide. The invention also provides processes for making these analogs. Further, the invention provides methods for inhibiting angiogenesis and treating angiogenesis-associated diseases, including cancer and macular degeneration, by administering these compounds.

Synthesis of 4-amino-thalidomide enantiomers

Method of synthesis of 4-amino-thalidomide enantiomers

The present invention comprises a group of compounds that effectively inhibit angiogenesis. More specifically, nitrogen-substituted thalidomide analogs and di-substituted thalidomide analogs have been shown to inhibit angiogenesis. Importantly, these compounds can be administered orally.

Use of nitrogen substituted thalidomide analogs for the treatment of macular degenerator

The invention provides new and useful analogs of 2-phthalimidinoglutaric acid. These analogs include DL-2-methyl-2-phthalimidinoglutaric acid and hydroxylated analogs of 2-phthalimidinoglutaric. The invention also provides processes for making these analogs. The invention also provides the two individual enantiomers of DL-2-methyl-2-phthalimidinoglutaric acid, (R)-(+)-2-methyl-2-phthalimidinoglutaric acid and (S)-(&#x2212;)-2-methyl-2-phthalimidinoglutaric acid, and processes for separating these individual enantiomers from the racemate. Further, the invention provides methods for inhibiting angiogenesis and treating angiogenesis-associated diseases, including cancer and macular degeneration, by administering one or more of these compounds.

Methods of treating undesired angiogenesis with 2-methyl-EM-138

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Mt. Airy, MD, United States of America

Glenn M Swartz