Analogs of 2-phthalimidinoglutaric acid and their use as...

C - Chemistry – Metallurgy – 07 – D

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C07D 209/46 (2006.01) A61K 31/4035 (2006.01)

Patent

CA 2331461

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 wherein each of R3 and R4 are independently H or OH. 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)-(-)-2-methyl-2-phthalimidinoglutaric acid, and processes or 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.

La présente invention concerne des analogues nouveaux et utiles de l'acide 2-phthalimidinoglutarique. Les analogues comprennent l'acide DL-2- méthyl-2- phthalimidinoglutarique et des analogues hydroxylés de 2-phthalimidinoglutarique. L'invention englobe également des procédés de fabrication de ces analogues. Elle concerne également les deux enantiomères de l'acide DL-2- méthyl-2- phthalimidinoglutarique, l'acide (R)-(+)-2- méthyl-2- phthalimidinoglutarique et l'acide (S)-(-)-2-méthyl-2-phthalimidinoglutarique ainsi que les procédés permettant de séparer ces énantiomères individuels du racémique vrai. De plus, cette invention, s'intéresse à des méthodes permettant d'inhiber l'angiogenèse et de traiter des affections en rapport avec l'angiogenèse, dont le cancer et la dégénérescence maculaire, par administration d'un ou de plusieurs de ces composés.

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