Patents by Inventor Yu-Lin Leu

Yu-Lin Leu has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).

  • BQC-G, a tumor-selective anti-cancer prodrug
    Patent number: 9353140
    Abstract: The invention relates to the synthesis of a second-generation camptothecin glucuronide prodrug (BQC-G) of a potent anticancer camptothecin derivative 5,6-dihydro-4H-benzo[de]quinoline-camptothecin (BQC). BQC-G was over 4000 times more water soluble than BQC, displayed good stability in human plasma and was an excellent substrate for enzymatic hydrolysis by bacterial and human ?-glucuronidases. BQC-G was about 30 times less toxic than BQC, but was as toxic as BQC after hydrolysis of the glucuronide moiety by ?-glucuronidase. In the presence of human serum albumin, BQC-G displayed lower cytotoxicity (IC50=1080 nM) but could be activated by ?-glucuronidase to display potent activity (IC50=13.3 nM).
    Type: Grant
    Filed: November 24, 2010
    Date of Patent: May 31, 2016
    Assignee: Academia Sinica
    Inventors: Zeljko M. Prijovic, Yu-Lin Leu, Steve R. Roffler
  • BQC-G, A TUMOR-SELECTIVE ANTI-CANCER PRODRUG
    Publication number: 20130012467
    Abstract: The invention relates to the synthesis of a second-generation camptothecin glucuronide prodrug (BQC-G) of a potent anticancer camptothecin derivative 5,6-dihydro-4H-benzo[de]quinoline-camptothecin (BQC). BQC-G was over 4000 times more water soluble than BQC, displayed good stability in human plasma and was an excellent substrate for enzymatic hydrolysis by bacterial and human ?-glucuronidases. BQC-G was about 30 times less toxic than BQC, but was as toxic as BQC after hydrolysis of the glucuronide moiety by ?-glucuronidase. In the presence of human serum albumin, BQC-G displayed lower cytotoxicity (IC50=1080 nM) but could be activated by ?-glucuronidase to display potent activity (IC50=13.3 nM).
    Type: Application
    Filed: November 24, 2010
    Publication date: January 10, 2013
    Applicant: Academia Sinica
    Inventors: Zeljko M. Prijovic, Yu-Lin Leu, Steve R. Roffler