US2018064667A1PendingUtilityA1

Methods of treating lactose intolerance

Assignee: NOGRA PHARMA LTDPriority: Apr 18, 2012Filed: May 12, 2017Published: Mar 8, 2018
Est. expiryApr 18, 2032(~5.6 yrs left)· nominal 20-yr term from priority
A61P 43/00A61P 3/00A23C 21/08A61K 31/195A23C 9/20A23C 13/12A61K 31/635A23C 9/152A61K 31/196A61K 31/44A61K 31/606A61K 31/4439A23C 19/09A61K 31/4402A61P 1/12A61P 1/04
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Claims

Abstract

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

Claims

exact text as granted — not AI-modified
1 - 10 . (canceled) 
     
     
         11 . A food product comprising a dairy component and a PPAR agonist represented by Formula I: 
       
         
           
           
               
               
           
         
         wherein R 1  and R 2 , are each independently selected from the group consisting of H and a —C 1 -C 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 , and —CH(OR 3 )COOH; and 
         R 3  is selected from the group consisting of H, phenyl, benzyl, vinyl, allyl, a —C 1 -C 6  alkyl, and a —C 1 -C 6  alkyl substituted by one, two, three, or more halogens; 
       
       or a pharmaceutically acceptable salt and/or a stereoisomer thereof. 
     
     
         12 . The food product of  claim 11 , wherein the dairy component is whey, milk, cheese or cream. 
     
     
         13 - 15 . (canceled) 
     
     
         16 . The food product of  claim 11 , wherein the PPAR agonist is 2-methoxy-3-(4′-aminophenyl)propionic acid, or a pharmaceutically acceptable salt and/or a stereoisomer thereof. 
     
     
         17 . The food product of  claim 11 , wherein the PPAR agonist is (S)-2-methoxy-3-(4′-aminophenyl)propionic acid, or a pharmaceutically acceptable salt thereof. 
     
     
         18 . A method for treating and/or ameliorating lactose intolerance or lactase deficiency in a patient in need thereof, the method comprising administering the food product of  claim 11  to the patient. 
     
     
         19 . A method for stimulating lactase gene expression in a patient in need thereof, the method comprising administering the food product of  claim 11  to the patient. 
     
     
         20 . A food product comprising a dairy component and a PPAR agonist, wherein the PPAR 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, 2-methoxy-3-(4′-aminophenyl)propionic acid, 5-aminosalicylo-hydroxamic acid (compound 5), 3-dimethylaminosalicylic acid, 2-methoxy-4-aminobenzoic acid, 2-methoxy-5-aminobenzoic acid, 5-methylaminosalicylic acid, 4-methylaminosalicylic acid, 4-acetylaminosalicylic acid, 2-ethoxy-4-aminobenzoic acid, 2-ethoxy-5-aminobenzoic acid, 4-dimethylaminosalicylic acid, 2-ethoxy-4-aminobenzoylhydroxamic acid, 6-hydroxyquinoline-5-carboxylic acid, 2-(2-propyl)oxy-4-aminobenzoic acid, 4-(1-piperazinyl)salicylic acid, 5-oxa-quinoline-6-carboxylic acid, 6-methoxy quinoline-5-carboxylic acid, 6-methoxy-1,2,3,4-tetrahydroquinoline-5-carboxylic acid, 5-diisopropylaminosalicylic acid, and 4-diisopropylaminosalicylic acid;
 or a pharmaceutically acceptable salt and/or a stereoisomer thereof. 
 
     
     
         21 . The food product of  claim 20 , wherein the dairy component is whey, milk, cheese or cream. 
     
     
         22 . A method for treating and/or ameliorating lactose intolerance or lactase deficiency in a patient in need thereof, the method comprising administering the food product of  claim 20  to the patient. 
     
     
         23 . A method for stimulating lactase gene expression in a patient in need thereof, the method comprising administering the food product of  claim 20  to the patient. 
     
     
         24 . A food product comprising a dairy component and a PPAR agonist represented by Formula I′: 
       
         
           
           
               
               
           
         
         wherein X is a —C 1 -C 3 alkylene, optionally substituted with one, two, or three substituents selected from a halogen or a hydroxyl; 
         R 1  is selected from the group consisting of a —C 1 -C 6 alkyl, a —C 3 -C 6 cycloalkyl, a —C 2 -C 6 alkenyl, and a —C 2 -C 6 alkynyl; 
         R 2  is selected from the group consisting of hydrogen and a —C 1 -C 6 alkyl; 
         R 3  is independently selected, for each occurrence, from the group consisting of hydrogen, a —C 1 -C 6 alkoxy, a —C 1 -C 6 alkyl, cyano, a —C 3 -C 6 cycloalkyl, a halogen, hydroxyl, and nitro; 
         R 4  is selected from the group consisting of hydrogen and a —C 1 -C 6 alkyl; and 
         R 5  is hydrogen or a —C 1 -C 6 alkyl; 
       
       or a pharmaceutically acceptable salt thereof, an N-oxide thereof, and/or a stereoisomer thereof. 
     
     
         25 . The food product of  claim 24 , wherein the dairy component is whey, milk, cheese or cream. 
     
     
         26 . The food product of  claim 24 , wherein the PPAR agonist is N-acetyl-3-(4′-aminophenyl)-2-methoxypropionic acid, or a pharmaceutically acceptable salt and/or a stereoisomer thereof. 
     
     
         27 . The food product of  claim 24 , wherein the PPAR agonist is N-acetyl-(S)-3-(4′-aminophenyl)-2-methoxypropionic acid, or a pharmaceutically acceptable salt thereof. 
     
     
         28 . A method for treating and/or ameliorating lactose intolerance or lactase deficiency in a patient in need thereof, the method comprising administering the food product of  claim 24  to the patient. 
     
     
         29 . A method for stimulating lactase gene expression in a patient in need thereof, the method comprising administering the food product of  claim 24  to the patient.

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