US2006199793A1PendingUtilityA1

Sterol absorption inhibitor compounds

50
Assignee: CHO WING-KEE PPriority: Jan 26, 2001Filed: Jun 22, 2005Published: Sep 7, 2006
Est. expiryJan 26, 2021(expired)· nominal 20-yr term from priority
A61P 9/04A61P 3/06A61P 43/00A61P 3/10A61P 9/00A61P 9/10A61P 3/04A61K 31/216A61P 3/00A61K 45/06A61K 31/397A61K 31/165A61K 31/055A61K 31/03
50
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Claims

Abstract

The present invention provides compositions, therapeutic combinations and methods including: (a) at least one peroxisome proliferator-activated receptor activator; and (b) at least one substituted azetidinone or substituted β-lactam sterol absorption inhibitor which can be useful for treating vascular conditions, diabetes, obesity and lowering plasma levels of sterols.

Claims

exact text as granted — not AI-modified
1 - 101 . (canceled)  
   
   
       102 . A pharmaceutical composition consisting of:  
     
       
         
               
               
               
             
                   
                   
               
                   
                   
               
                   
                   
                 Weight 
               
                   
                   
                 percent of 
               
                   
                 Ingredient 
                 ingredient 
               
                   
                   
               
                   
               
               
               
               
             
                   
                 Compound of Formula (II) 
                 10 
               
                   
                 Lactose monohydrate 
                 55 
               
                   
                 Microcrystalline cellulose 
                 20 
               
                   
                 Povidone 
                 4 
               
                   
                 Croscarmellose sodium 
                 8 
               
                   
                 Sodium lauryl sulfate 
                 2 
               
                   
                 Magnesium stearate 
                 1 
               
                   
                 Total 
                 100 
               
                   
                   
               
                   
                   
               
           
              
              
              
              
              
              
             
             
              
             
          
           
              
              
              
              
              
              
              
              
              
              
             
          
         
       
     
     wherein the compound represented by Formula (II) below is:  
     
       
         
         
             
             
         
       
     
     and wherein the pharmaceutical composition is effective for treating a vascular condition in a mammal.  
   
   
       103 . A pharmaceutical composition consisting of:  
     
       
         
               
               
               
             
                   
                   
               
                   
                   
               
                   
                   
                 Weight 
               
                   
                   
                 percent of 
               
                   
                 Ingredient 
                 ingredient 
               
                   
                   
               
                   
               
               
               
               
             
                   
                 Compound of Formula (II) 
                 10 
               
                   
                 Lactose monohydrate 
                 55 
               
                   
                 Microcrystalline cellulose 
                 20 
               
                   
                 Povidone 
                 4 
               
                   
                 Croscarmellose sodium 
                 8 
               
                   
                 Sodium lauryl sulfate 
                 2 
               
                   
                 Magnesium stearate 
                 1 
               
                   
                 Total 
                 100 
               
                   
                   
               
                   
                   
               
           
              
              
              
              
              
              
             
             
              
             
          
           
              
              
              
              
              
              
              
              
              
              
             
          
         
       
     
     wherein the compound represented by Formula (II) below is:  
     
       
         
         
             
             
         
       
     
     and wherein the pharmaceutical composition is effective for treating diabetes in a mammal.  
   
   
       104 . A pharmaceutical composition consisting of:  
     
       
         
               
               
               
             
                   
                   
               
                   
                   
               
                   
                   
                 Weight 
               
                   
                   
                 percent of 
               
                   
                 Ingredient 
                 ingredient 
               
                   
                   
               
                   
               
               
               
               
             
                   
                 Compound of Formula (II) 
                 10 
               
                   
                 Lactose monohydrate 
                 55 
               
                   
                 Microcrystalline cellulose 
                 20 
               
                   
                 Povidone 
                 4 
               
                   
                 Croscarmellose sodium 
                 8 
               
                   
                 Sodium lauryl sulfate 
                 2 
               
                   
                 Magnesium stearate 
                 1 
               
                   
                 Total 
                 100 
               
                   
                   
               
                   
                   
               
           
              
              
              
              
              
              
             
             
              
             
          
           
              
              
              
              
              
              
              
              
              
              
             
          
         
       
     
     wherein the compound represented by Formula (II) below is:  
     
       
         
         
             
             
         
       
     
     and wherein the pharmaceutical composition is effective for treating obesity in a mammal.  
   
   
       105 . A pharmaceutical composition consisting of:  
     
       
         
               
               
               
             
                   
                   
               
                   
                   
               
                   
                   
                 Weight 
               
                   
                   
                 percent of 
               
                   
                 Ingredient 
                 ingredient 
               
                   
                   
               
                   
               
               
               
               
             
                   
                 Compound of Formula (II) 
                 10 
               
                   
                 Lactose monohydrate 
                 55 
               
                   
                 Microcrystalline cellulose 
                 20 
               
                   
                 Povidone 
                 4 
               
                   
                 Croscarmellose sodium 
                 8 
               
                   
                 Sodium lauryl sulfate 
                 2 
               
                   
                 Magnesium stearate 
                 1 
               
                   
                 Total 
                 100 
               
                   
                   
               
                   
                   
               
           
              
              
              
              
              
              
             
             
              
             
          
           
              
              
              
              
              
              
              
              
              
              
             
          
         
       
     
     wherein the compound represented by Formula (II) below is:  
     
       
         
         
             
             
         
       
     
     and wherein the pharmaceutical composition is effective for lowering a plasma sterol concentration of a mammal.  
   
   
       106 . A pharmaceutical composition consisting essentially of:  
     
       
         
               
               
               
             
                   
                   
               
                   
                   
               
                   
                   
                 milligrams 
               
                   
                   
                 of 
               
                   
                 Ingredient 
                 ingredient 
               
                   
                   
               
                   
               
               
               
               
             
                   
                 Compound of Formula (II) 
                 10 
               
                   
                 Lactose monohydrate 
                 55 
               
                   
                 Microcrystalline cellulose 
                 20 
               
                   
                 Povidone 
                 4 
               
                   
                 Croscarmellose sodium 
                 8 
               
                   
                 Sodium lauryl sulfate 
                 2 
               
                   
                 Magnesium stearate 
                 1 
               
                   
                 Total 
                 100 
               
                   
                   
               
                   
                   
               
           
              
              
              
              
              
              
             
             
              
             
          
           
              
              
              
              
              
              
              
              
              
              
             
          
         
       
     
     wherein the compound represented by Formula (II) below is:  
     
       
         
         
             
             
         
       
     
     and wherein the pharmaceutical composition is effective for treating a vascular condition in a mammal.  
   
   
       107 . A pharmaceutical composition consisting essentially of:  
     
       
         
               
               
               
             
                   
                   
               
                   
                   
               
                   
                   
                 milligrams 
               
                   
                   
                 of 
               
                   
                 Ingredient 
                 ingredient 
               
                   
                   
               
                   
               
               
               
               
             
                   
                 Compound of Formula (II) 
                 10 
               
                   
                 Lactose monohydrate 
                 55 
               
                   
                 Microcrystalline cellulose 
                 20 
               
                   
                 Povidone 
                 4 
               
                   
                 Croscarmellose sodium 
                 8 
               
                   
                 Sodium lauryl sulfate 
                 2 
               
                   
                 Magnesium stearate 
                 1 
               
                   
                 Total 
                 100 
               
                   
                   
               
                   
                   
               
           
              
              
              
              
              
              
             
             
              
             
          
           
              
              
              
              
              
              
              
              
              
              
             
          
         
       
     
     wherein the compound represented by Formula (II) below is:  
     
       
         
         
             
             
         
       
     
     and wherein the pharmaceutical composition is effective for treating diabetes in a mammal.  
   
   
       108 . A pharmaceutical composition consisting essentially of:  
     
       
         
               
               
               
             
                   
                   
               
                   
                   
               
                   
                   
                 milligrams 
               
                   
                   
                 of 
               
                   
                 Ingredient 
                 ingredient 
               
                   
                   
               
                   
               
               
               
               
             
                   
                 Compound of Formula (II) 
                 10 
               
                   
                 Lactose monohydrate 
                 55 
               
                   
                 Microcrystalline cellulose 
                 20 
               
                   
                 Povidone 
                 4 
               
                   
                 Croscarmellose sodium 
                 8 
               
                   
                 Sodium lauryl sulfate 
                 2 
               
                   
                 Magnesium stearate 
                 1 
               
                   
                 Total 
                 100 
               
                   
                   
               
                   
                   
               
           
              
              
              
              
              
              
             
             
              
             
          
           
              
              
              
              
              
              
              
              
              
              
             
          
         
       
     
     wherein the compound represented by Formula (II) below is:  
     
       
         
         
             
             
         
       
     
     and wherein the pharmaceutical composition is effective for treating obesity in a mammal.  
   
   
       109 . A pharmaceutical composition consisting essentially of:  
     
       
         
               
               
               
             
                   
                   
               
                   
                   
               
                   
                   
                 milligrams 
               
                   
                   
                 of 
               
                   
                 Ingredient 
                 ingredient 
               
                   
                   
               
                   
               
               
               
               
             
                   
                 Compound of Formula (II) 
                 10 
               
                   
                 Lactose monohydrate 
                 55 
               
                   
                 Microcrystalline cellulose 
                 20 
               
                   
                 Povidone 
                 4 
               
                   
                 Croscarmellose sodium 
                 8 
               
                   
                 Sodium lauryl sulfate 
                 2 
               
                   
                 Magnesium stearate 
                 1 
               
                   
                 Total 
                 100 
               
                   
                   
               
                   
                   
               
           
              
              
              
              
              
              
             
             
              
             
          
           
              
              
              
              
              
              
              
              
              
              
             
          
         
       
     
     wherein the compound represented by Formula (II) below is:  
     
       
         
         
             
             
         
       
     
     and wherein the pharmaceutical composition is effective for lowering a plasma sterol concentration of a mammal.

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