公开(公告)号：US20160244479A1

公开(公告)日：2016-08-25

申请号：US14913366

申请日：2014-08-27

Applicant: YEDA RESEARCH AND DEVELOPMENT CO. LTD.

Inventor： Steven J.D. KARLISH ,  Adriana KATZ ,  Daniel M. TAL

IPC: C07J43/00

CPC classification number: C07J43/003 ,  C07J19/005

Abstract: The present invention relates to digoxin and digitoxin derivatives that are selective inhibitors of the α2 isoform of Na,K-ATPase, and that reduce intra-ocular pressure. The invention further relates to uses of these derivatives for treating disorders associated with elevated intraocular pressure, such as glaucomas, and/or as cardiotonic agents.

Abstract translation: 本发明涉及作为Na，K-ATP酶的α2同种型的选择性抑制剂的地高辛和洋地黄毒苷衍生物，并且降低眼内压。 本发明进一步涉及这些衍生物用于治疗与眼内压升高相关的疾病，例如青光眼，和/或作为强心剂。

公开(公告)号：US20180207189A1

公开(公告)日：2018-07-26

申请号：US15745441

申请日：2016-07-19

Applicant: Yeda Research and Development Co., Ltd.

Inventor： Steven J.D. KARLISH ,  Adriana KATZ ,  Daniel M. TAL ,  Arie MARCOVICH

IPC: A61K31/7052 ,  A61P27/06 ,  A61P9/00

Abstract: Provided herein are alpha2-selective Na,K-ATPase inhibitors and prodrugs thereof, characterized by having a cyclic moiety attached to a digoxin or digitoxin derivative, as well as uses thereof in lowering intraocular pressure and in treating glaucoma and heart conditions.

公开(公告)号：US20200297748A1

公开(公告)日：2020-09-24

申请号：US16847737

申请日：2020-04-14

Applicant: Yeda Research and Development Co. Ltd.

Inventor： Steven J.D. KARLISH ,  Adriana KATZ ,  Daniel M. TAL ,  Arie MARCOVICH

IPC: A61K31/7052 ,  C07H17/00 ,  C07J43/00 ,  A61P27/06 ,  A61P9/00

Abstract: Provided herein are alpha2-selective Na,K-ATPase inhibitors and prodrugs thereof, characterized by having a cyclic moiety attached to a digoxin or digitoxin derivative, as well as uses thereof in lowering intraocular pressure and in treating glaucoma and heart conditions.