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. 20, 2022

Filed:

Jul. 08, 2020
Applicant:

University of Puerto Rico, San Juan, PR (US);

Inventors:

Eliud Hernandez-O'Farrill, San Juan, PR (US);

Cornelis P. Vlaar, San Juan, PR (US);

Suranganie Dharmawardhane Flanagan, San Juan, PR (US);

Linette Castillo-Pichardo, San Juan, PR (US);

Assignee:

UNIVERSITY OF PUERTO RICO, San Juan, PR (US);

Attorneys:
Primary Examiner:
Int. Cl.
CPC ...
C07D 403/12 (2006.01); C07D 403/14 (2006.01); A61K 31/506 (2006.01); C07D 401/14 (2006.01); A61P 35/00 (2006.01); A61K 31/5377 (2006.01);
U.S. Cl.
CPC ...
A61K 31/506 (2013.01); A61K 31/5377 (2013.01); A61P 35/00 (2018.01); C07D 401/14 (2013.01); C07D 403/12 (2013.01); C07D 403/14 (2013.01);
Abstract

A series of novel EHop-016 derivatives is presented herein via designing and synthesizing compounds that mimics its more favorable 'U-shaped' conformation that appears to be critical for inhibitory activity against Rac. Based on modeling studies on EHop-016, compounds with a more rigid structural conformation can mimic this 'U-shaped' conformation and would improve the anti-migration activity against metastatic cells. Compounds are disclosed that inhibit RhoGTPases that are useful for inhibiting hyperprofilerative and neoplastic diseases, for instance compounds of formula Specifically, the compounds inhibit the GTPases Rac and Cdc42 that are overactive or overexpressed in signaling pathways in cancer and metastasis. Methods for treatment of cancer and hyperproliferative diseases are disclosed.


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