• 专利标题:   Making conjugates involves e.g. conjugating targeting moiety to graphene quantum dot in conjugates to form many first intermediates, comprising reacting each GQD with ammonium hydroxide and hydrogen peroxide and associating active agent.
  • 专利号:   US10493170-B1
  • 发明人:   QIN Y, ZHOU S
  • 专利权人:   UNIV SOUTH FLORIDA, QIN Y, ZHOU S
  • 国际专利分类:   A61B005/00, A61K031/704, A61K047/02, A61K047/22, A61K049/00, A61N005/06
  • 专利详细信息:   US10493170-B1 03 Dec 2019 A61K-049/00 201999 Pages: 45 English
  • 申请详细信息:   US10493170-B1 US747321 23 Jun 2015
  • 优先权号:   US016228P, US747321

▎ 摘  要

NOVELTY - Making many conjugates, where each conjugate comprises graphene quantum dot (GQD), targeting moiety conjugated to the GQD, and active agent associated with the GQD, the targeting moiety is folic acid or derivative, and the active agent is doxorubicin non-covalently associated with the GQD via pi - pi stacking, comprises: conjugating the targeting moiety to each GQD in the conjugates to form many first intermediates, where the targeting moiety is folic acid or a derivative thereof, the conjugating the targeting moiety to each GQD comprises reacting each GQD with ammonium hydroxide and hydrogen peroxide to introduce amine reactive coupling groups onto each of the GQDs and reacting the targeting moiety with crosslinking agents to form a covalent bond with the amine reactive coupling group to form the first intermediates; and associating the active agent to each first intermediate in the first intermediates to form the conjugates. USE - The method is useful for making many conjugates (claimed) for therapeutic, prophylactic, or diagnostic effects to a subject, where the subject is cancer patient and the active agent an anti-cancer agent. No biological data given. DETAILED DESCRIPTION - Making many conjugates, where each conjugate comprises a graphene quantum dot (GQD), a targeting moiety conjugated to the GQD, and an active agent associated with the GQD, the GQDs in the conjugates have an average diameter of 3 nm and a span of less than or equal to 1.5, the targeting moiety is folic acid or a derivative, and the active agent is a doxorubicin non-covalently associated with the GQD via pi - pi stacking, comprises: conjugating the targeting moiety to each GQD in the conjugates to form many first intermediates, where the targeting moiety is folic acid or a derivative thereof, the conjugating the targeting moiety to each GQD comprises reacting each GQD with ammonium hydroxide and hydrogen peroxide to introduce amine reactive coupling groups onto each of the GQDs and reacting the targeting moiety with crosslinking agents to form a covalent bond with the amine reactive coupling group to form the first intermediates; and associating the active agent to each first intermediate in the first intermediates to form the conjugates.