US 2026/0257992 A1 · AGONISTS OF SMALL HETERODIMER PARTNER FOR CANCER THERAPY

Abstract

Novel compounds that are improved analogs and mimetics of DSHN and methods to treat or inhibit cancer using the compounds. The methods can require lower doses than for DSHN and the compounds can have a larger biological maximum than DSHN. Nuclear receptor NR0B2 is activated by the disclosed compounds to reduce immune-suppressive Tregs, thereby attenuating tumor growth and metastasis. The therapy disclosed herein results in an inhibition of Treg expansion and an expansion of cytotoxic T cells. This therapy can significantly reduce tumor growth with lower doses compared to other available treatments.

Claims22

Dependent claims

A compound of formula I:

wherein
R1 is (C1-C8)alkyl or H;
R2 is ethyl, (C1-C8)alkyl, or H;
R3 is ethyl, (C1-C8)alkyl, or H;
or
R2 and R3 taken together with the nitrogen atom to which they are attached form a 3- to 9-membered ring heterocycle provided that R1 is (C1-C8)alkyl;
and
R4 is H or (C1-C8)alkyl;
wherein the naphthalene moiety of formula I and each (C1-C8)alkyl are optionally substituted with one or more substituents;
or a pharmaceutically acceptable salt thereof;
provided that R1 is (C1-C8)alkyl when R2 and R3 are both ethyl and R4 is H;
and
provided that R1, R2, R3, and R4 are not all H.

10 more elements

Dependencies are inferred from the claim text.

Facts

Application

19/474,194Filed 11 Apr 2024

Priority

12 Apr 2023

Published

3 Sep 2026

Term ends

Not estimatedThe source records don’t support an estimate.

Classification9 codes

C07C 311/29
Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound oxygen atoms: having the sulfur atom of at least one…
A61K 31/24
Having an aromatic ring attached to a carboxyl group: having an amino or nitro group
A61K 31/403
Having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil: condensed with…
A61P 35/00
Antineoplastic agents

Agonists of small heterodimer partner for cancer therapy

Life of this patent

Agonists of small heterodimer partner for cancer therapy

Life of this patent

Abstract

Claims22