公开(公告)号：US11542274B1

公开(公告)日：2023-01-03

申请号：US17483731

申请日：2021-09-23

Applicant: AGENCY FOR SCIENCE, TECHNOLOGY AND RESEARCH (A*STAR)

Inventor： Wei Hung ,  Thomas Hugo Keller ,  Wei Ling Wang ,  Gang Wang ,  Congbao Kang

IPC: C07D495/14 ,  C07D519/00

Abstract: There are provided new heterobifunctional agents designed to mediated formation of protein-protein dimers and promote ubiquitination of a protein of the dimer. Also provided are methods of synthesizing the agents, pharmaceutical formulations including the agents, and methods of using the agents to treat, ameliorate or cure diseases characterized by protein over-expression or malfunction.

公开(公告)号：US20190071416A1

公开(公告)日：2019-03-07

申请号：US15767129

申请日：2016-10-10

Applicant: Agency For Science, Technology and Research

Inventor： Klement Jihao Foo ,  Anders Poulsen ,  Thomas Hugo Keller ,  Si Si Liew ,  Cheng San Brian Chia ,  Jin Yan Melgious Ang ,  Chuhul Huang

IPC: C07D401/06 ,  A61P35/00 ,  C07D401/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/08 ,  C07D405/14

Abstract: Compounds For Inhibition Of Cancer and Epigenesis. The present invention relates to quinolines and 5,6,7,8-tetrahydroacridines of the formula (I) wherein Z1, Z2, X, R1 to R8 and Y are defined as described in the specification, or a pharmaceutically acceptable form or prodrug thereof, that are inhibitors of methyl transferases such as protein lysine methyltransferases and more particularly SMYD3. The present invention also relates to the methods for their preparation, pharmaceutical compositions containing these compounds and uses of these compounds in the treatment of disorders/conditions/diseases involving, relating to or associated with enzymes having methyl transferase activities/functions and/or via unspecified/multi-targeted mechanisms.

公开(公告)号：US11834430B2

公开(公告)日：2023-12-05

申请号：US16646693

申请日：2018-09-12

Applicant: AGENCY FOR SCIENCE, TECHNOLOGY AND RESEARCH

Inventor： Soo Yei Ho ,  Anders Poulsen ,  Sum Wai Eldwin Tan ,  Shi Hua Ang ,  Thomas Hugo Keller

IPC: C07D401/04 ,  C07D231/12 ,  C07D233/12 ,  C07D249/08 ,  C07D401/12 ,  C07D401/14 ,  A61P35/00 ,  C07D233/06 ,  C07D233/60 ,  C07D261/08 ,  C07D277/24 ,  C07D403/12

CPC classification number: C07D401/04 ,  A61P35/00 ,  C07D231/12 ,  C07D233/06 ,  C07D233/60 ,  C07D249/08 ,  C07D261/08 ,  C07D277/24 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12

Abstract: The present invention relates to compounds of general Formula (I), and/or tautomers, enantiomers, solvates, hydrates, and pharmaceutically acceptable salts thereof. The present invention also relates to compounds of Formula (I) for use in therapy, methods of treating isoprenylcysteine carboxyl methyltransferase (ICMT) related disorders or uses of compounds of Formula (I) in the manufacture of a medicament for the treatment of ICMT-related disorders, wherein the disorder is cancer and/or progeria. The present invention further relates to processes for synthesizing compounds of Formula (I).

公开(公告)号：US20210147441A1

公开(公告)日：2021-05-20

申请号：US17028574

申请日：2020-09-22

Applicant: AGENCY FOR SCIENCE, TECHNOLOGY AND RESEARCH (A*STAR)

Inventor： Wei Hung ,  Thomas Hugo Keller ,  Wei Ling Wang ,  Gang Wang ,  Congbao Kang

IPC: C07D495/14 ,  C07D519/00

Abstract: There are provided new heterobifuctional agents designed to mediated formation of protein-protein dimers and promote ubiqutination of a protein of the dimer. Also provided are methods of synthesizing the agents, pharmaceutical formulations including the agents, and methods of using the agents to treat, ameliorate or cure diseases characterized by protein over-expression or malfunction.

公开(公告)号：US20210130317A1

公开(公告)日：2021-05-06

申请号：US16646693

申请日：2018-09-12

Applicant: AGENCY FOR SCIENCE, TECHNOLOGY AND RESEARCH

Inventor： Soo Yei Ho ,  Anders Poulsen ,  Sum Wai Eldwin Tan ,  Shi Hua Ang ,  Thomas Hugo Keller

IPC: C07D401/04 ,  C07D249/08 ,  C07D233/60 ,  C07D277/24 ,  C07D401/12 ,  C07D231/12 ,  C07D233/06 ,  C07D261/08 ,  C07D401/14 ,  C07D403/12 ,  A61P35/00

Abstract: The present invention relates to compounds of general Formula (I), and/or tautomers, enantiomers, solvates, hydrates, and pharmaceutically acceptable salts thereof. The present invention also relates to compounds of Formula (I) for use in therapy, methods of treating isoprenylcysteine carboxyl methyltransferase (ICMT) related disorders or uses of compounds of Formula (I) in the manufacture of a medicament for the treatment of ICMT-related disorders, wherein the disorder is cancer and/or progeria. The present invention further relates to processes for synthesizing compounds of Formula (I).