公开(公告)号：US11179395B2

公开(公告)日：2021-11-23

申请号：US15923244

申请日：2018-03-16

Applicant: GEORGETOWN UNIVERSITY

Inventor： Sivanesan Dakshanamurthy ,  Stephen W. Byers ,  Dean Rosenthal

IPC: A61K31/519 ,  A61P35/00 ,  A61K31/4184 ,  C12Q1/6886

Abstract: Provided herein are methods for treating melanoma in a subject.

公开(公告)号：US20180263987A1

公开(公告)日：2018-09-20

申请号：US15923244

申请日：2018-03-16

Applicant: GEORGETOWN UNIVERSITY

Inventor： Sivanesan Dakshanamurthy ,  Stephen W. Byers ,  Dean Rosenthal

IPC: A61K31/519 ,  A61P35/00 ,  A61K31/4184 ,  C12Q1/6886

CPC classification number: A61K31/519 ,  A61K31/4184 ,  A61P35/00 ,  C12Q1/6886 ,  C12Q2600/106 ,  C12Q2600/156

Abstract: Provided herein are methods for treating melanoma in a subject.

公开(公告)号：US20150119250A1

公开(公告)日：2015-04-30

申请号：US14390743

申请日：2013-03-15

Applicant: Howard University ,  Georgetown University

Inventor： Sivanesan Dakshanamurthy ,  Hemayet Ullah

IPC: A01N43/653 ,  A01N43/38

CPC classification number: A01N43/653 ,  A01N43/38

Abstract: Compounds and methods are described herein that are effective to modulate plant response (e.g., plant susceptibility) to environmentally-induced stress. The compounds and methods described herein advantageously may be used to modulate environmental stress resistance in a wide variety of plants. Environmental stresses include, for example, high light intensity (UV exposure), temperature (e.g., high heat), high soil salinity, and low soil moisture (e.g., drought). As used herein, environmental stresses include any conditions that result in increased generation of reactive oxygen species (ROS) and accumulation of ROS in the plant cells. The compounds described herein that are effective to modulate resistance to the stress prevent, directly or indirectly, or increase phosphorylation of Tyr248 of the RACK1A protein.

Abstract translation: 本文描述了有效调节植物对环境胁迫的响应（例如，植物敏感性）的化合物和方法。 本文所述的化合物和方法有利地可用于调节各种植物中的耐环境胁迫性。 环境胁迫包括例如高光强度（UV暴露），温度（例如高热），高土壤盐分和低土壤湿度（例如干旱）。 如本文所用，环境应力包括导致活性氧（ROS）的产生增加和ROS在植物细胞中积累的任何条件。 本文所述的有效调节抗原的化合物直接或间接地阻止或增加RACK1A蛋白的Tyr248的磷酸化。

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：US20180157786A1

公开(公告)日：2018-06-07

申请号：US15577719

申请日：2016-06-03

Applicant: GEORGETOWN UNIVERSITY

Inventor： Sivanesan Dakshanamurthy ,  Stephen W. Byers

IPC: G06F19/16 ,  G06F5/01 ,  G06F17/11

CPC classification number: G16B15/00 ,  G06F5/01 ,  G06F17/11 ,  G06F2217/16 ,  G16B15/30

Abstract: Described herein are methods of predicting drug-target interactions and methods of using the information for drug repurposing. The methods described herein combine different descriptors, including, for example, atom pair similarity, shape, topology and chemical signatures, physico-chemical functional descriptors, contact points of the ligand and the target protein, chemical similarity, and docking score.

公开(公告)号：US09889131B2

公开(公告)日：2018-02-13

申请号：US15017040

申请日：2016-02-05

Applicant: Georgetown University

Inventor： Stephen W. Byers ,  Sivanesan Dakshanamurthy ,  Jaime M. Guidry Auvil ,  Milton L. Brown

IPC: A61K31/498 ,  C07D241/42 ,  C07D213/30 ,  A61K31/343 ,  A61K31/44 ,  A61K31/473 ,  A61K45/06 ,  C07D215/14 ,  C07D307/77 ,  C07K16/18

CPC classification number: A61K31/498 ,  A61K31/343 ,  A61K31/44 ,  A61K31/473 ,  A61K45/06 ,  C07D213/30 ,  C07D215/14 ,  C07D241/42 ,  C07D307/77 ,  C07K16/18

Abstract: Cadherin-11 inhibitors and methods for the prevention and treatment of cadherin-11 related diseases are described herein. Cadherin-11 related diseases include cancer and rheumatoid arthritis.

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。

公开(公告)号：US09284368B2

公开(公告)日：2016-03-15

申请号：US14323374

申请日：2014-07-03

Applicant: Georgetown University

Inventor： Stephen W. Byers ,  Sivanesan Dakshanamurthy ,  Jaime M. Guidry Auvil ,  Milton L. Brown

IPC: C07D241/12 ,  C07K16/18 ,  C07D213/30 ,  C07D241/42 ,  A61K31/343 ,  A61K31/44 ,  A61K31/473 ,  A61K31/498 ,  A61K45/06 ,  C07D215/14 ,  C07D307/77

CPC classification number: A61K31/498 ,  A61K31/343 ,  A61K31/44 ,  A61K31/473 ,  A61K45/06 ,  C07D213/30 ,  C07D215/14 ,  C07D241/42 ,  C07D307/77 ,  C07K16/18

Abstract: This invention provides for a method of preventing or treating a cadherin-11 related disease in a subject, which includes administering to the subject an effective amount of a compound of the following formula: or a pharmaceutically acceptable salt or prodrug thereof, where R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, X1 and X2 are as defined herein.

Abstract translation: 本发明提供了预防或治疗受试者中钙粘蛋白-11相关疾病的方法，其包括向受试者施用有效量的下式化合物或其药学上可接受的盐或前药，其中R1，R2 ，R 3，R 4，R 5，R 6，R 7，R 8，R 9，R 10，R 11，R 12，X 1和X 2如本文所定义。