IP Library › Granted Patent US 9,682,050
Granted Patent B2
US 9,682,050 · App. 14/394,916 · Granted Jun 20, 2017

Methods of treating lactose intolerance

Inventors: Sergio Baroni (Villa D'adda, IT); Salvatore Bellinvia (Balerna, CH); Francesca Viti (Salorino, CH)
Assignee: Nogra Pharma Limited
A61K31/196A23C9/152A23C9/20A23C13/12A23C19/09A23C21/08A61K31/195A61K31/4439A61K31/606A61K31/635
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Quick Facts
Patent No.
US 9,682,050
App. No.
14/394,916
Granted
Jun 20, 2017
Kind
B2
Abstract

Disclosed herein are methods for treating lactose intolerance, including compounds that may be specific or modulate PPARγ receptors.

Claims (20)

1. A method for treating and/or ameliorating lactose intolerance or lactase deficiency in a patient in need thereof, comprising administering an effective amount of a PPARγ agonist compound to said patient, wherein the PPARγ agonist is represented by Formula I:

or a pharmaceutically acceptable salt, an N-oxide, and/or a stereoisomer thereof, wherein:

R 1 and R 2 , are each independently selected from the group consisting of H and C 1-6 alkyl; or R 1 and R 2 together with the nitrogen atom they are bonded to form an aromatic or aliphatic ring with 5 or 6 atoms which may be optionally substituted;

Y and Z are each independently selected from the group consisting of H, OH, COOH, —OR 3 , —CH(OR 3 )COOH; and

R 3 is selected from the group consisting of H, phenyl, benzyl, vinyl, allyl, C 1-6 alkyl or C 1-6 alkyl substituted by one, two, three or more halogens.

2. The method of claim 1 , wherein the PPARγ agonist is selected from the group consisting of: (±)-2-hydroxy-3-(3′-aminophenyl) propionic acid; (±)-2-methoxy-2-(4′-aminophenyl) acetic acid; (±)-2-ethoxy-2-(3′-aminophenyl) acetic acid; (±)-2-ethoxy-2-(4′-aminophenyl) acetic acid; (±)-2-methoxy-3-(4′-aminophenyl) propionic acid; (±)-2-ethoxy-3-(4′-aminophenyl) propionic acid; (±)-2-ethoxy-3-(3′-aminophenyl) propionic acid, and (R,S)-2-methoxy-3-(4-aminophenyl)propionic acid, or a pharmaceutically acceptable salt thereof.

3. The method of claim 1 , wherein the PPARγ agonist is (R)-2-methoxy-3-(4-aminophenyl) propionic acid or a pharmaceutically acceptable salt thereof.

4. A method for treating and/or ameliorating lactose intolerance or lactase deficiency in a patient in need thereof, comprising administering an effective amount of a PPARγ agonist compound to said patient, wherein the PPARγ agonist is a compound represented by Formula I′:

wherein X is C 1 -C 3 alkylene, optionally substituted with one, two or three substituents selected from halogen or hydroxyl;

R 1 is selected from the group consisting of C 1 -C 6 alkyl, C 3 -C 6 cycloalkyl, C 2 -C 6 alkenyl, and C 2 -C 6 alkynyl;

R 2 is selected from the group consisting of hydrogen and C 1 -C 6 alkyl;

R 3 is independently selected, for each occurrence from the group consisting of hydrogen, C 1 -C 6 alkoxy, C 1 -C 6 alkyl, cyano, C 3 -C 6 cycloalkyl, halogen, hydroxyl, and nitro;

R 4 is selected from the group consisting of hydrogen and C 1 -C 6 alkyl; and

R 5 is hydrogen C 1 -C 6 alkyl;

or a pharmaceutically acceptable salt or an N-oxide thereof.

5. The method of claim 4 , wherein the compound is N-acetyl-(R)-3-(4-aminophenyl)-2-methoxypropionic acid or a pharmaceutically acceptable salt thereof.

6. The method of claim 4 , wherein the compound is N-acetyl-(S)-3-(4-aminophenyl)-2-methoxypropionic acid or a pharmaceutically acceptable salt thereof.

7. The method of claim 1 , wherein the PPARγ agonist is (S)-2-methoxy-3-(4-aminophenyl) propionic acid or a pharmaceutically acceptable salt thereof.

8. The method of claim 1 , wherein the PPARγ agonist is 2-methoxy-3-(4-aminophenyl) propionic acid or a pharmaceutically acceptable salt or a stereoisomer thereof.

9. The method of claim 4 , wherein the compound is N-acetyl-3-(4-aminophenyl)-2-methoxypropionic acid or a pharmaceutically acceptable salt or a stereoisomer thereof.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 21, 2015
From: BARONI, SERGIO; BELLINVIA, SALVATORE; VITI, FRANCESCA
To: NOGRA PHARMA LIMITED
Reel/Frame 034774/0177 →
Priority Claims (1)
EP 12425073 · Apr 18, 2012 · regional
Continuity (2)
Provisional Application 61672931 · Jul 18, 2012
Related Publication 20150087678A1 · Mar 26, 2015