The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.

The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.

Date of Patent:
Sep. 15, 2026

Filed:

Apr. 09, 2022
Applicant:

Universität Basel, Basel, CH;

Inventors:

Chiara Borsari, Basel, CH;

Matthias Wymann, Bern, CH;

Assignee:

UNIVERSITÄT BASEL, Basel, CH;

Attorney:
Primary Examiner:
Int. Cl.
CPC ...
C07D 413/14 (2006.01); A61K 31/5377 (2006.01); A61P 35/02 (2006.01); C07D 401/14 (2006.01); C07D 403/14 (2006.01);
U.S. Cl.
CPC ...
C07D 413/14 (2013.01); A61K 31/5377 (2013.01); A61P 35/02 (2018.01); C07D 401/14 (2013.01); C07D 403/14 (2013.01);
Abstract

Our invention relates to novel triazine compounds, containing chemical reactive groups (warheads) and behaving as reversible and irreversible covalent inhibitors. Linkers have been introduced to target a solvent exposed, distal cysteine at >10 Å from the core reversible inhibitor. Different exit vectors have been investigated to modulate inhibitor intrinsic reactivity and efficiency in covalent bond formation. We disclose novel, optimized covalent modifiers of phosphoinositide 3-kinase alpha (PI3Kα), an enzyme frequently altered in human malignancies. The compounds of the invention could be exploited as therapeutic agents and chemical probes useful for the investigation of the role of PI3K isoforms in cancer and metabolism, and for treatment of PI3Kα-driven cancers and malformations.


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