US 12,098,119 B2 · Compound used as SIRT6 small-molecule allosteric activator and pharmaceutical composition thereof

Abstract

Disclosed by the present invention are an SIRT6 small-molecule allosteric activator and the application thereof and provided is an SIRT6 small-molecule allosteric activator that contains a derivative as shown in formula (1) or a pharmacologically acceptable salt thereof as the active ingredient. The SIRT6 small-molecule allosteric activator designed and synthesized in the present invention has high efficacy and low toxicity, may significantly activate SIRT6 activity during in vitro experiments, and has great importance in the development of pharmaceuticals for relevant diseases.

Claims3

Dependent claims

A compound or a pharmacologically acceptable salt thereof, as represented by formula (I):

wherein R1, R2, R3, R4, R5, R6, R7, R8, R9 and R10 are independently selected from the group consisting of H, halogen, hydroxyl, nitro, amino, carboxyl, acid ester group, sulfonamide, mercapto, methoxy, ethoxy, benzyloxy, methyl and cyano;
R1, R2, R3, R4, R5, R6, R7, R9 and R10 is halogen;
R11 is
represents substituted or unsubstituted nitrogen-containing heterocyclic ring, and the nitrogen-containing heterocyclic ring is azacyclopropane, azetidine, pyrazole, morpholine, piperidine, piperidine, piperazine, azacycloheptane or azacyclooctane.

1 more element

Dependencies are inferred from the claim text.

Facts

Application

17/293,917Filed 14 May 2018

Priority

CN 201710681498.610 Aug 2017

Published

US 2022/0220069 A114 Jul 2022

Granted

24 Sep 2024

Term ends

Not estimatedThe source records don’t support an estimate.

Classification25 codes

C07C 303/38
Of amides of sulfonic acids: by reaction of ammonia or amines with sulfonic acids, or with esters, anhydrides, or halides thereof
A61K 31/40
Having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins: having five-membered rings with one nitrogen as the only ring hetero atom,…
A61K 31/496
Having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines: non-condensed piperazines…
A61K 31/5375
Having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines: 1,4-Oxazines, e.g. morpholine

Compound used as SIRT6 small-molecule allosteric activator and pharmaceutical composition thereof

Life of this patent

Compound used as SIRT6 small-molecule allosteric activator and pharmaceutical composition thereof

Life of this patent

Abstract

Claims3