Camptothecin-analog with a novel, "flipped" lactone-stable,...

C - Chemistry – Metallurgy – 07 – F

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Details

C07F 7/10 (2006.01) A61K 31/4745 (2006.01) A61K 31/555 (2006.01) A61K 31/695 (2006.01) A61P 35/00 (2006.01) C07D 491/22 (2006.01) C07F 7/30 (2006.01)

Patent

CA 2648895

The present invention discloses: (i) a novel, lactone-stable, ~flipped~ E-ring camptothecin, pharmaceutically-acceptable salts, and/or analogs thereof; (ii) methods of synthesis of said novel, lactone-stable, ~flipped~ E-ring camptothecin, pharmaceutically-acceptable salts, and/or analogs thereof; (iii) pharmaceutically-acceptable formulations comprising said novel, lactone-stable, ~flipped~ E-ring camptothecin, pharmaceutically-acceptable salts, and/or analogs thereof, and, optionally, one or more additional chemotherapeutic agents; (iv) methods of administration of said novel, lactone-stable, ~flipped~ E-ring camptothecin, pharmaceutically-acceptable salts, and/or analogs thereof, and, optionally, one or more additional chemotherapeutic agents, to subjects in need thereof; and (v) devices for the administration of said novel, lactone-stable, ~flipped~ E-ring camptothecin, pharmaceutically-acceptable salts, and/or analogs thereof, and, optionally, one or more chemotherapeutic agents, to subjects in need thereof.

La présente invention concerne (i) une camptothécine à nouveau noyau en E "retourné" stable à la lactone, des sels pharmaceutiquement acceptables et/ou des analogues de celle-ci, (ii) des procédés de synthèse de cette camptothécine à nouveau noyau en E "retourné" stable à la lactone, de ces sels pharmaceutiquement acceptables et/ou de ces analogues, (iii) des préparations pharmaceutiquement acceptables comprenant cette camptothécine à nouveau noyau en E "retourné" stable à la lactone, ces sels pharmaceutiquement acceptables et/ou ces analogues, et, éventuellement, un ou plusieurs agents chimiothérapeutiques additionnels, (iv) des méthodes destinées à administrer cette camptothécine à nouveau noyau en E "retourné" stable à la lactone, ces sels pharmaceutiquement acceptables et/ou ces analogues, et, éventuellement, un ou plusieurs agents chimiothérapeutiques additionnels, à des sujets nécessitant un tel traitement, et (v) des dispositifs destinés à administrer cette camptothécine à nouveau noyau en E "retourné" stable à la lactone, ces sels pharmaceutiquement acceptables et/ou ces analogues, et, éventuellement, un ou plusieurs agents chimiothérapeutiques, à des sujets nécessitant un tel traitement.

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