IP Library Granted Patent US 10,988,463
Granted Patent B2
US 10,988,463 · App. 16/999,295 · Granted Apr 27, 2021

Substituted 3-azabicyclo[3.1.0]hexanes as ketohexokinase inhibitors

Inventors: Matthew Dowling (Old Lyme, CT); Dilinie Fernando (Jamaica Plain, MA); Kentaro Futatsugi (Quincy, MA); Kim Huard (Berkeley, CA); Thomas Victor Magee (Winchester, MA); Brian Raymer (Holliston, MA); Andre Shavnya (East Lyme, CT); Aaron Smith (North Providence, RI); Benjamin Thuma (Old Lyme, CT); Andy Tsai (Mystic, CT); Meihua Tu (Acton, MA)
Assignee: Pfizer Inc.
C07D403/14A61K31/403C07D401/04C07D401/14C07D403/04
View Patent ↗
Loading inventors, assignments & file history…
Monitor This Case
Get email alerts when status or documents change.
Order Certified Copies
Most orders are placed with the USPTO same day — all within 24 business hours.
Order via The Patent Place →
Pre-filled with this patent's details
Quick Facts
Patent No.
US 10,988,463
App. No.
16/999,295
Granted
Apr 27, 2021
Kind
B2
Abstract

Provided herein are substituted 3-azabicyclo[3.1.0]hexanes as ketohexokinase inhibitors, processes to make said compounds, and methods comprising administering said compounds to a mammal in need thereof.

Claims (8)

1. A method of treating a disease for which an inhibitor of KHK is indicated, the method comprising the administration to a human in need thereof a therapeutically effective amount of a compound, wherein the compound is [(1R,5S,6R)-3-{2-[(2S)-2-methylazetidin-1-yl]-6-(trifluoromethyl)pyrimidin-4-yl}-3-azabicyclo[3.1.0]hex-6-yl]acetic acid, or pharmaceutically acceptable salt thereof, and wherein the disease is selected from any one or a combination of obesity, visceral adipose dysfunction, eating disorders, and excessive sugar craving.

2. The method of claim 1 , wherein the compound is a crystalline form of [(1R,5S,6R)-3-{2-[(2S)-2-methylazetidin-1-yl]-6-(trifluoromethyl)pyrimidin-4-yl}-3-azabicyclo[3.1.0]hex-6-yl]acetic acid.

3. The method of claim 2 , wherein the crystalline form is characterized substantially by the following principal powder x-ray diffraction pattern peaks expressed in terms of 2θ as measured with a copper radiation chosen from 9.0+/−0.2°, 10.4+/−0.2°, 15.0+/−0.2°, and 21.4+/−0.2°.

4. The method of claim 1 , wherein the compound is [(1R,5S,6R)-3-{2-[(2S)-2-methylazetidin-1-yl]-6-(trifluoromethyl)pyrimidin-4-yl}-3-azabicyclo[3.1.0]hex-6-yl]acetic acid.

5. The method of claim 4 , wherein the disease is obesity.

6. The method of claim 4 , wherein the disease is visceral adipose dysfunction.

7. The method of claim 4 , wherein the disease is eating disorders.

8. The method of claim 4 , wherein the disease is excessive sugar craving.

Assignments (1)
ASSIGNEE ADDRESS CORRECTION Recorded Mar 20, 2023
From: PFIZER INC.
To: PFIZER INC.
Reel/Frame 063119/0087 →
Continuity (7)
Continuation 16744283 · Jan 16, 2020
Continuation 16211283 · Dec 6, 2018
Continuation 15729885 · Oct 11, 2017
Continuation 15381295 · Dec 16, 2016
Provisional Application 62423549 · Nov 17, 2016
Provisional Application 62272598 · Dec 29, 2015
Related Publication 20200377482A1 · Dec 3, 2020