IP Library Granted Patent US 11,866,425
Granted Patent B2
US 11,866,425 · App. 17/345,064 · Granted Jan 9, 2024

Diacylglycerol acyl transferase 2 inhibitors

Inventors: Markus Boehm (Mansfield, MA); Shawn Cabral (Groton, CT); Matthew S. Dowling (Old Lyme, CT); Kentaro Futatsugi (Qunicy, MA); Kim Huard (Berkeley, CA); Esther Cheng Yin Lee (Newton, MA); Allyn T. Londregan (Barrington, RI); Jana Polivkova (Mystic, CT); David A. Price (Concord, MA); Qifang Li (Stonington, CT)
Assignee: Pfizer Inc.
C07D405/14A61K31/506A61K45/06C07D401/14C07D409/14A61P3/00A61P3/06A61P3/10C07B2200/13
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Quick Facts
Patent No.
US 11,866,425
App. No.
17/345,064
Granted
Jan 9, 2024
Kind
B2
Abstract

Compounds of Formula I that inhibit the activity of the diacylglycerol acyltransferase 2 (DGAT2) and their uses in the treatment of diseases linked thereto in animals are described herein.

Claims (29)

1. A method for treating hyperlipidemia, dyslipidemia,

atherosclerosis, hypertriglyceridemia, or hyper apo B lipoproteinemia, in humans comprising the step of administering to a human in need of such treatment a therapeutically effective amount of a compound according to Formula (I) or a pharmaceutically acceptable salt of said compound;

wherein

D 1 and D 2 are each independently N or CH;

R 1 is H, or (C 1 -C 2 )alkyl optionally substituted with one or two substituents each independently selected from fluoro and (C 3 -C 6 )cycloalkyl;

R 2 is H or fluoro;

R 3 is,

R 4 is H, cyano, or (C 1 -C 4 )alkyl optionally substituted with one or two substituents each independently selected from —OH and —S(O) 2 R 6 ;

R 5 is H or —OH, and

R 6 is (C 1 -C 4 )alkyl.

2. A method for treating Type II diabetes mellitus, early-onset Type 2 diabetes (EOD), conditions of impaired glucose tolerance (IGT), conditions of impaired fasting plasma glucose, metabolic acidosis, metabolic syndrome, syndrome X, hyperglycemia, hyperinsulinemia, insulin resistance, or impaired glucose metabolism, in humans comprising the step of administering to a human in need of such treatment a therapeutically effective amount of a compound according to Formula (I) or a pharmaceutically acceptable salt of said compound;

wherein

D 1 and D 2 are each independently N or CH;

R 1 is H, or (C 1 -C 2 )alkyl optionally substituted with one or two substituents each independently selected from fluoro and (C 3 -C 6 )cycloalkyl,

R 2 is H or fluoro;

R 3 is,

R 4 is H, cyano, or (C 1 -C 4 )alkyl optionally substituted with one or two substituents each independently selected from —OH and —S(O) 2 R 6 ;

R 5 is H or —OH; and

R 6 is (C 1 -C 4 )alkyl.

3. The method of claim 1 wherein the compound of Formula (I) is

or a pharmaceutically acceptable salt thereof.

4. The method of claim 2 wherein the compound of Formula (I) is

or a pharmaceutically acceptable salt thereof.

5. The method of claim 1 wherein the compound of Formula (I) is

6. The method of claim 2 wherein the compound of Formula (I) is

7. The method of claim 1 wherein the compound of Formula (I) is 2-(5-((3-ethoxypyridin-2-yl)oxy)pyridin-3-yl)-N-(tetrahydrofuran-3-yl)pyrimidine-5-carboxamide or a pharmaceutically acceptable salt thereof.

8. The method of claim 2 wherein the compound of Formula (I) is 2-(5-((3-ethoxypyridin-2-yl)oxy)pyridin-3-yl)-N-(tetrahydrofuran-3-yl)pyrimidine-5-carboxamide or a pharmaceutically acceptable salt thereof.

9. The method of claim 1 wherein the compound of Formula (I) is 2-(5-((3-ethoxypyridin-2-yl)oxy)pyridin-3-yl)-N-(tetrahydrofuran-3-yl)pyrimidine-5-carboxamide.

10. The method of claim 2 wherein the compound of Formula (I) is 2-(5-((3-ethoxpyridin-2-yl)oxy)pyridin-3-yl)-N-(tetrahydrofuran-3-yl)pyrimidine-5-carboxamide.

Assignments (1)
ASSIGNEE ADDRESS CORRECTION Recorded Mar 20, 2023
From: PFIZER INC.
To: PFIZER INC.
Reel/Frame 063119/0087 →
Cited By (1)
US 12,703,696