公开(公告)号：US20180105505A1

公开(公告)日：2018-04-19

申请号：US15573183

申请日：2016-05-12

Applicant: GEORGETOWN UNIVERSITY

Inventor： Milton L. Brown ,  Yali Kong ,  Jacqueline Smith ,  Kan Wang ,  Shujie Hou

IPC: C07D311/02 ,  C07C271/28 ,  C07C321/14 ,  C07C69/017 ,  C07C69/003 ,  A61K47/69 ,  A61P35/00 ,  G01N21/64

CPC classification number: C07D311/02 ,  A61K31/352 ,  A61K47/6957 ,  A61P35/00 ,  C07C69/003 ,  C07C69/017 ,  C07C271/28 ,  C07C321/14 ,  C07D311/18 ,  C07D311/58 ,  G01N21/64

Abstract: A glutathione-cleavable prodrug is provided herein, as well as methods for its use in treating cancer, including triple negative breast cancer. The prodrug can be cleaved by glutathione under physiological conditions to generate a biologically active agent. The compound described herein is advantageous as the compound is fluorescent and can therefore be monitored within a subject.

公开(公告)号：US10806725B2

公开(公告)日：2020-10-20

申请号：US15155258

申请日：2016-05-16

Applicant: GEORGETOWN UNIVERSITY

Inventor： Sivanesan Dakshanamurthy ,  Milton L. Brown ,  Robert Clarke ,  Ayesha N. Shajahan-Haq ,  Jacqueline Smith

IPC: A61K31/4439 ,  A61K31/426 ,  A61K31/427 ,  C07D401/04 ,  C07D401/14 ,  C07D405/14 ,  C07D417/04 ,  C07D417/14 ,  A61K31/41 ,  C07D213/32 ,  A61K31/444 ,  A61K45/06

Abstract: Small molecule inhibitors of XBP1 splicing by IRE1α are provided, as well as methods for their use in treating or preventing cancer (e.g., endocrine resistant breast cancer), diabetes, and obesity.

公开(公告)号：US10023551B2

公开(公告)日：2018-07-17

申请号：US15573183

申请日：2016-05-12

Applicant: GEORGETOWN UNIVERSITY

Inventor： Milton L. Brown ,  Yali Kong ,  Jacqueline Smith ,  Kan Wang ,  Shujie Hou

IPC: C07D311/58 ,  C07D311/02 ,  A61P35/00 ,  G01N21/64 ,  A61K47/69 ,  C07C321/14 ,  C07C69/017 ,  C07C69/003 ,  C07C271/28

Abstract: A glutathione-cleavable prodrug is provided herein, as well as methods for its use in treating cancer, including triple negative breast cancer. The prodrug can be cleaved by glutathione under physiological conditions to generate a biologically active agent. The compound described herein is advantageous as the compound is fluorescent and can therefore be monitored within a subject.

公开(公告)号：US20170007588A1

公开(公告)日：2017-01-12

申请号：US15155258

申请日：2016-05-16

Applicant: GEORGETOWN UNIVERSITY

Inventor： Sivanesan Dakshanamurthy ,  Milton L. Brown ,  Robert Clarke ,  Ayesha N. Shajahan-Haq ,  Jacqueline Smith

IPC: A61K31/4439

Abstract: Small molecule inhibitors of XBP1 splicing by IRE1α are provided, as well as methods for their use in treating or preventing cancer (e.g., endocrine resistant breast cancer), diabetes, and obesity.

Abstract translation: 提供了通过IRE1α剪接XBP1的小分子抑制剂，以及它们用于治疗或预防癌症（例如内分泌耐药性乳腺癌），糖尿病和肥胖症的方法。