Patent classifications
C07D207/48
PROTEIN-PROTEIN INTERACTION STABILIZERS
- Michelle R. Arkin ,
- Lucas Brunsveld ,
- Christian Ottmann ,
- Adam R. Renslo ,
- R. Jeffrey Neitz ,
- Mengqi Zhong ,
- Kenneth K. Hallenbeck ,
- Priyadarshini Jaishankar ,
- Shubhankar Dutta ,
- John K. Morrow ,
- Eline Sijbesma ,
- Bente Aminhan Somsen ,
- Galen Patrick Miley ,
- Emira Josien Visser ,
- Peter James Cossar ,
- Madita Wolter ,
- Thorsten Genski ,
- Laura Mariana Levy ,
- Torsten Hoffmann ,
- Dimitrios Tzalis ,
- Dario Valenti ,
- Markella Konstantinidou
Provided herein, inter alia, are stabilizers of protein-protein interactions and methods of identifying and using the same.
3-DIARYLMETHYLENES AND USES THEREOF
3-Diarylmethylenes are disclosed. The compounds activate PP2A, suppress oncogenic kinase signaling, and negatively regulate MYC and MYCN in cancer. The compounds also induce FOXO transcription factor translocation to the nucleus by modulating PP2A and, as a consequence, exhibit anti-proliferative effects. They are useful in the treatment of a variety of disorders, including as a monotherapy in cancer treatment, or used in combination with other drugs to restore sensitivity to chemotherapy where resistance has developed.
3-DIARYLMETHYLENES AND USES THEREOF
3-Diarylmethylenes are disclosed. The compounds activate PP2A, suppress oncogenic kinase signaling, and negatively regulate MYC and MYCN in cancer. The compounds also induce FOXO transcription factor translocation to the nucleus by modulating PP2A and, as a consequence, exhibit anti-proliferative effects. They are useful in the treatment of a variety of disorders, including as a monotherapy in cancer treatment, or used in combination with other drugs to restore sensitivity to chemotherapy where resistance has developed.
ANTI-ARRHYTHMICITY AGENTS
Agents, compositions, and methods for regulating cardiac rhythmicity are disclosed.
ANTI-ARRHYTHMICITY AGENTS
Agents, compositions, and methods for regulating cardiac rhythmicity are disclosed.
NOVEL IMAGING COMPOSITION AND USES THEREOF
The invention discussed in this application relates to hydroxamic acid-based compounds that are useful as imaging agents when bound to an appropriate metal centre, particularly for the imaging of tumours.
NOVEL IMAGING COMPOSITION AND USES THEREOF
The invention discussed in this application relates to hydroxamic acid-based compounds that are useful as imaging agents when bound to an appropriate metal centre, particularly for the imaging of tumours.
TRPV4 antagonists
The present invention relates to pyrrolidine sulfonamide analogs, pharmaceutical compositions containing them and their use as TRPV4 antagonists.
TRPV4 antagonists
The present invention relates to pyrrolidine sulfonamide analogs, pharmaceutical compositions containing them and their use as TRPV4 antagonists.
SULFINYLAMINOBENZAMIDE AND SULFONYLAMINOBENZAMIDE DERIVATIVES
Provided is a compound of Formula (I):
##STR00001## wherein the variable groups are defined herein.