IP Library › Granted Patent US 12,551,484
Granted Patent B2
US 12,551,484 · App. 17/774,657 · Granted Feb 17, 2026

Methods of treatment and/or prevention of major adverse cardiovascular events (MACE) with a combination of a BET bromodomain inhibitor and a sodium dependent glucose transport 2 inhibitor

Inventors: Kenneth Eugene Lebioda (Calgary, CA); Christopher Ross Armstrong Halliday (Calgary, CA); Aziz Naeem Khan (Calgary, CA)
Assignee: Resverlogix Corp.
A61K31/517A61K45/06A61P9/04
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Quick Facts
Patent No.
US 12,551,484
App. No.
17/774,657
Granted
Feb 17, 2026
Kind
B2
Abstract

Described herein are methods of for treating and/or preventing Major adverse cardiovascular events (MACE). by administering to a subject in need thereof, a combination of a sodium-glucose transport protein 2 (SGLT2) inhibitor and a compound of Formula I or a stereoisomer, tautomer, pharmaceutically acceptable salt, or hydrate thereof, wherein the variables of Formula I are as defined herein.

Claims (22)

1 . A method for treating major adverse cardiovascular events (MACE) comprising administering to a subject in need thereof a sodium-glucose transport protein 2 (SGLT2) inhibitor and a compound 2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4 (3H)-one or a stereoisomer, tautomer, pharmaceutically acceptable salt, or hydrate thereof; wherein the subject is a human on statin therapy with type 2 diabetes and low HDL cholesterol, below 40 mg/dL for males and below 45 mg/dL for females, and a recent acute coronary syndrome (ACS) within the preceding 7-90 days; and wherein the SGLT2 inhibitor is selected from empagliflozin, canagliflozin, remogliflozin, ipragliflozin, HM41322, dapagliflozin, bexagliflozin, ertugliflozin, sotagliflozin, luseogliflozin, tofogliflozin.

2 . A method for treating any individual component of major adverse cardiovascular events (MACE) comprising administering to a subject in need thereof a sodium-glucose transport protein 2 (SGLT2) inhibitor and a compound 2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3H)-one or a stereoisomer, tautomer, pharmaceutically acceptable salt, or hydrate thereof, wherein the subject is a human on statin therapy with type 2 diabetes and low HDL cholesterol, below 40 mg/dL for males and below 45 mg/dL for females, and a recent acute coronary syndrome (ACS) within the preceding 7-90 days; and wherein the SGLT2 inhibitor is selected from empagliflozin, canagliflozin, remogliflozin, ipragliflozin, HM41322, dapagliflozin, bexagliflozin, ertugliflozin, sotagliflozin, luseogliflozin, tofogliflozin.

3 . The method according to claim 1 , wherein the subject in need thereof is administered a daily dose of 200 mg of 2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3H)-one or an equivalent amount of a pharmaceutically acceptable salt thereof.

4 . The method according to claim 1 , wherein the subject in need thereof is administered 100 mg of 2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3H)-one or an equivalent amount of a pharmaceutically acceptable salt thereof twice daily.

5 . The method according to claim 1 , wherein the SGLT2 inhibitor is selected from empagliflozin, canagliflozin, remogliflozin, ipragliflozin, HM41322, and dapagliflozin.

6 . The method according to claim 1 , wherein the SGLT2 inhibitor is selected from bexagliflozin, ertugliflozin, sotagliflozin, luseogliflozin, and tofogliflozin.

7 . The method according to claim 1 , wherein the MACE is selected from non-fatal myocardial infarction, cardiovascular death, stroke, and hospitalization for cardiovascular disease events.

8 . The method according to claim 7 , wherein the hospitalization for cardiovascular disease events is hospitalization for congestive heart failure.

9 . The method according to claim 7 , wherein the MACE is selected from non-fatal myocardial infarction, cardiovascular death, and stroke.

10 . The method according to claim 2 , wherein the subject in need thereof is administered a daily dose of 200 mg of 2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3H)-one or an equivalent amount of a pharmaceutically acceptable salt thereof.

11 . The method according to claim 2 , wherein the subject in need thereof is administered 100 mg of 2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3H)-one or an equivalent amount of a pharmaceutically acceptable salt thereof twice daily.

12 . The method according to claim 2 , wherein the SGLT2 inhibitor is selected from empagliflozin, canagliflozin, remogliflozin, ipragliflozin, HM41322, and dapagliflozin.

13 . The method according to claim 2 , wherein the SGLT2 inhibitor is selected from bexagliflozin, ertugliflozin, sotagliflozin, luseogliflozin, and tofogliflozin.

14 . The method according to claim 2 , wherein the MACE is selected from non-fatal myocardial infarction, cardiovascular death, stroke, and hospitalization for cardiovascular disease events.

15 . The method according to claim 14 , wherein the MACE is selected from non-fatal myocardial infarction, cardiovascular death, and stroke.

16 . The method according to claim 14 , wherein the hospitalization for cardiovascular disease events is hospitalization for congestive heart failure.

17 . The method according to claim 1 , wherein the SGLT2 inhibitor is empagliflozin.

18 . The method according to claim 1 , wherein the SGLT2 inhibitor is canagliflozin.

19 . The method according to claim 1 , wherein the SGLT2 inhibitor is dapagliflozin.

20 . The method according to claim 2 , wherein the SGLT2 inhibitor is empagliflozin.

21 . The method according to claim 2 , wherein the SGLT2 inhibitor is canagliflozin.

22 . The method according to claim 2 , wherein the SGLT2 inhibitor is dapagliflozin.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 5, 2022
From: LEBIODA, KENNETH EUGENE; HALLIDAY, CHRISTOPHER ROSS ARMSTRONG; KHAN, AZIZ NAEEM
To: RESVERLOGIX CORP.
Reel/Frame 059832/0335 →
Continuity (2)
Provisional Application 62930860 · Nov 5, 2019
Related Publication 20220370452A1 · Nov 24, 2022
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