公开(公告)号：US20210238173A1

公开(公告)日：2021-08-05

申请号：US16972013

申请日：2019-06-04

Applicant: Yeda Research and Development Co. Ltd.

Inventor： Nir LONDON ,  Amit SHRAGA ,  Evgenia OLSHVANG

IPC: C07D471/04 ,  C07D231/56 ,  C07D491/052 ,  C07D401/04

Abstract: Provided are compounds that act as covalent inhibitors of mitogen-activated protein kinase kinase 7 (MKK7 enzyme), method of preparation and uses thereof.

公开(公告)号：US20190327974A1

公开(公告)日：2019-10-31

申请号：US16476559

申请日：2018-01-09

Applicant: THE AUSTRALIAN NATIONAL UNIVERSITY ,  YEDA RESEARCH AND DEVELOPMENT CO. LTD. ,  THE REGENTS OF THE UNIVERSITY OF CALIFORNIA

Inventor： Colin JACKSON ,  Nir LONDON ,  Galen CORREY ,  Janelle SAN JUAN

IPC: A01N55/08 ,  A01N57/10

Abstract: This invention is directed to synergists for organophosphate (OP), carbamate (CM) and/or pyrethroid/synthetic pesticides (SP). This invention is further directed to a composition comprising organophosphate, carbamate, and/or pyrethroid/synthetic pyrethroid, and at least one boronic acid derivative. This invention further provides methods for killing insect pests.

公开(公告)号：US20240139326A1

公开(公告)日：2024-05-02

申请号：US18258812

申请日：2021-12-23

Applicant: YEDA RESEARCH AND DEVELOPMENT CO. LTD.

Inventor： Nir LONDON ,  Efrat RESNICK ,  Rambabu REDDI ,  Adi ROGEL

IPC: A61K47/55 ,  C09K11/07

CPC classification number: A61K47/55 ,  C09K11/07 ,  C09K2211/1007 ,  C09K2211/1014 ,  C09K2211/1022

Abstract: This invention is directed to substituted a methacrylamide compounds as targeted covalent protein binders and uses thereof.

公开(公告)号：US20230406837A1

公开(公告)日：2023-12-21

申请号：US18334385

申请日：2023-06-14

Applicant: Yeda Research and Development Co., Ltd.

Inventor： Nir LONDON ,  Rambabu Reddi

IPC: C07D333/48

CPC classification number: C07D333/48

Abstract: Provided herein are Sulfamate compounds for use in modulating an activity of peptidyl-prolyl isomerase NIMA-interacting-1 (Pin1).

公开(公告)号：US20210332024A1

公开(公告)日：2021-10-28

申请号：US17370216

申请日：2021-07-08

Applicant: Yeda Research and Development Co. Ltd. ,  Dana-Farber Cancer Institute, Inc. ,  Beth Israel Deaconess Medical Center, Inc.

Inventor： Nir LONDON ,  Daniel ZAIDMAN ,  Christian DUBIELLA ,  Nathanael S. GRAY ,  Benika Joan PINCH ,  Kun Ping LU ,  Alfred Thomas LOOK ,  Shuning HE ,  Xiao Zhen ZHOU ,  Xiaolan LIAN

IPC: C07D333/16

Abstract: Disclosed herein are compounds comprising an electrophilic moiety and rigid moiety for use in modulating an activity of Pin1. The rigid moiety comprises at least one functional group that is capable of forming hydrogen bonds with hydrogen atoms, wherein the electrophilic moiety and the rigid moiety are arranged such that the electrophilic moiety is capable of covalently binding to the Cys113 residue of Pin1, and the rigid moiety is capable of forming hydrogen bonds with the Gln131 and His 157 residues of Pin1. Further disclosed are novel compounds having Formula Id: wherein the dashed line, W, X, Y, Z, Ra-Rc, R1, R2, L1, L2 and n are as defined herein, and libraries comprising such compounds. Further disclosed are methods of identifying a compound capable of modulating an activity of Pin1, by screening a library of compounds.