公开(公告)号：WO2011094260A2

公开(公告)日：2011-08-04

申请号：PCT/US2011/022508

申请日：2011-01-26

Applicant: STC. UNM ,  HROMAS, Robert ,  LEITAO, Andrei ,  OPREA, Tudor, I. ,  SKLAR, Larry, A. ,  WILLIAMSON, Elizabeth, A. ,  WRAY, Justin ,  WANG, Wei

Inventor： HROMAS, Robert ,  LEITAO, Andrei ,  OPREA, Tudor, I. ,  SKLAR, Larry, A. ,  WILLIAMSON, Elizabeth, A. ,  WRAY, Justin ,  WANG, Wei

IPC: C07D215/233 ,  C07D401/04 ,  C07D401/14 ,  A61K31/47 ,  A61K31/4709 ,  A61P35/00

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-I) 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破坏DNA的DNA复制和修复蛋白Metnase和/或Intnase（也称为Gypsy整合酶，Gypsy Integrease-1，Gypsy Retransposon整合酶1或GIN-1）的小化学双功能抑制剂， 并涉及利用抑制剂来增加包括放射疗法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（例如急性骨髓性白血病（AML）和相关癌症的患者）。在此类治疗的某些方面，本发明化合物，组合物和治疗 本发明作为单一疗法施用（在一些情况下，对展现对TopoIIα抑制剂如VP-16的抗性的患者），或者与本文另有描述的TopoIIα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：WO2020185746A1

公开(公告)日：2020-09-17

申请号：PCT/US2020/021838

申请日：2020-03-10

Applicant: STC. UNM

Inventor： PEREZ, Dominique, Renee ,  SKLAR, Larry, A. ,  CHIGAEV, Alexandre ,  FRANKS, Alison, F.

IPC: A61K8/18 ,  A61K45/08 ,  A61P17/00 ,  A61Q17/04 ,  A61Q19/00

Abstract: The present invention is directed to previously identified inhibitors ofcAMP efflux (ICE) and their use in feaiing/niasking body odor, inhibiting, reducing and/or eliminating hyperhidrosis (excessive sweating), tanning skin or protecting skin before and/or after exposure to the sun as well as.for treating certain skin conditions, in one embodiment, the invention provides a method for inhibiting body odor, a condition that is characterized by an unpleasant odor from the products of the microbial sweat degradation. By inhibiting the efflux of the precursor compounds that are degraded, novel compounds are- capable of preventing unwanted odors. Deodorant compositions that employ this new approach for the control of bodily odor are provided, ICE compounds can also be used as. components, of cosmetic formulations including tanning and after-sun formulations, formulations for skin conditions as described herein and other cosmetic formulations.