Methods of treating lactose intolerance

Patent metadata

Field	Value
Publication number	US-9682050-B2
Application number	US-201314394916-A
Country	US
Kind code	B2
Filing date	Apr 12, 2013
Priority date	Apr 18, 2012
Publication date	Jun 20, 2017
Grant date	Jun 20, 2017

Abstract

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

First claim

What is claimed is:

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.

Assignees

• Nogra Pharma Ltd

Inventors

• Baroni Sergio
• Bellinvia Salvatore
• Viti Francesca

Classifications

• A61P43/00

  Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00 · CPC title

• A61P3/00

  Drugs for disorders of the metabolism (of the blood or the extracellular fluid A61P7/00) · CPC title

• A61K31/196 Primary

  the amino group being directly attached to a ring, e.g. anthranilic acid, mefenamic acid, diclofenac, chlorambucil · CPC title

• A61K31/4402

  only substituted in position 2, e.g. pheniramine, bisacodyl · CPC title

• A61K31/4439

  containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole (nicotine A61K31/465) · CPC title