公开(公告)号：US10907219B2

公开(公告)日：2021-02-02

申请号：US15119506

申请日：2015-02-18

Applicant: STC.UNM ,  Fu-Sen Liang ,  Wei Wang

Inventor： Fu-Sen Liang ,  Wei Wang

IPC: C12Q1/68 ,  C12Q1/6897

Abstract: This disclosure describes compositions and methods that involve a first modular component and a second modular component. The first modular component includes a first target molecule coupled to a first dimerizing moiety. The second modular component includes a second target molecule coupled to a second dimerizing moiety. The first dimerizing moiety dimerizes with the second dimerizing moiety when the first dimerizing moiety binds a chemical induced proximity (CIP) inducer.

公开(公告)号：US20150087886A1

公开(公告)日：2015-03-26

申请号：US14510476

申请日：2014-10-09

Applicant: STC.UNM

Inventor： Robert Hromas ,  Andrei Leitao ,  Tudor I. Oprea ,  Larry A. Sklar ,  Elizabeth A. Williamson ,  Justin Wray ,  Wei Wang

IPC: C07D215/56 ,  C07D401/06 ,  A61K31/475 ,  A61N5/10 ,  C07D401/12 ,  A61K45/06 ,  C07D401/10 ,  A61K31/7048 ,  A61K31/47 ,  A61K31/496

CPC classification number: C07D215/56 ,  A61K31/47 ,  A61K31/4709 ,  A61K31/475 ,  A61K31/496 ,  A61K31/7048 ,  A61K45/06 ,  A61N5/1001 ,  A61N5/1045 ,  A61N2005/1087 ,  A61N2005/1098 ,  C07D401/06 ,  C07D401/10 ,  C07D401/12 ,  A61K2300/00

Abstract: This invention relates to novel cancer treatment compositions and associated therapeutic methods. More particularly, this invention relates in part to small chemical bifunctional inhibitors of DNA replication and repair proteins Metnase and/or Intnase (also termed Gypsy Integrase, Gypsy Integrease-1, Gypsy Retransposon Integrase 1, or GIN-1) that simultaneously damage DNA, and to a therapeutic method that utilizes the inhibitors to increase the effectiveness of cancer treatment protocols, including radiation therapy.In preferred embodiments, compounds, compositions and methods of treatment of the invention are used to treat a patient suffering from leukemia (e.g. acute myeloid leukemia (AML) and related cancers. In certain aspects of such treatments, compounds, compositions and methods of treatment of the invention are administered as a monotherapy (in some cases, to patients who have exhibited resistance to Topo IIalpha inhibitors such as VP-16), or are co-administered with a Topo IIalpha inhibitor or other anti-cancer agents as otherwise described herein or in combination with radiation therapy.

Abstract translation: 本发明涉及新的癌症治疗组合物和相关的治疗方法。 更具体地说，本发明部分涉及同时损伤DNA的DNA复制和修复蛋白质Metnase和/或Intnase（也称为Gypsy整合酶，Gypsy Integrease-1，Gypsy Retransposon Integrase 1或GIN-1）的小型化学双功能抑制剂， 以及利用抑制剂增加包括放射治疗在内的癌症治疗方案的有效性的治疗方法。 在优选的实施方案中，本发明的化合物，组合物和治疗方法用于治疗患有白血病的患者（例如急性骨髓性白血病（AML）和相关的癌症）。在这些治疗的某些方面，化合物，组合物和治疗方法 本发明作为单一疗法（在某些情况下，对已显示出对Topo IIalpha抑制剂如VP-16具有抗性的患者）施用，或者与本文另有描述的Topo IIal抑制剂或其它抗癌剂共同施用，或 结合放射治疗。

公开(公告)号：US20170226595A1

公开(公告)日：2017-08-10

申请号：US15119506

申请日：2015-02-18

Applicant: STC.UNM

Inventor： Fu-Sen Liang ,  Wei Wang

IPC: C12Q1/68

CPC classification number: C12Q1/6897 ,  C12N2510/00

Abstract: This disclosure describes compositions and methods that involve a first modular component and a second modular component. The first modular component includes a first target molecule coupled to a first dimerizing moiety. The second modular component includes a second target molecule coupled to a second dimerizing moiety. The first dimerizing moiety dimerizes with the second dimerizing moiety when the first dimerizing moiety binds a chemical induced proximity (CIP) inducer.