US2005267208A1PendingUtilityA1

Nordihydroguaiartic derivatives for use in treatment of tumors

53
Assignee: UNIV JOHNS HOPKINSPriority: Oct 15, 1999Filed: May 4, 2005Published: Dec 1, 2005
Est. expiryOct 15, 2019(expired)· nominal 20-yr term from priority
Inventors:Ru Chih C. HuangJonathan Daniel HellerJih Ru HwuKo King
A61P 43/00A61K 31/401A61P 35/04A61K 9/0014A61K 31/405A61K 9/0019A61K 31/22A61K 31/225A61P 31/18A61P 35/00A61K 31/198A61K 31/417
53
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Claims

Abstract

Nordihydroguaiaretic acid derivatives and methods of use thereof for the treatment of tumors.

Claims

exact text as granted — not AI-modified
1 - 16 . (canceled)  
   
   
       17 . A pharmaceutical composition comprising tetra-O-methyl nordihydroguaiaretic acid along with at least one pharmaceutically acceptable excipient or carrier, wherein the tetra-O-methyl nordihydroguaiaretic acid (M 4 N) is present at a concentration of 60 mg/ml or 200 mg/ml.  
   
   
       18 . The composition of  claim 17 , wherein said the excipient or carrier is dimethyl sulfoxide (DMSO).  
   
   
       19 - 21 . (canceled)  
   
   
       22 . A pharmaceutical composition comprising tetraglycinyl nordihydroguaiaretic acid (G 4 N) along with at least one pharmaceutically acceptable excipient or carrier, wherein the tetraglycinyl nordihydroguaiaretic acid (G 4 N) is present at a concentration of 200 m/ml.  
   
   
       23 . The composition of  claim 22 , wherein the excipient or carrier is physiological saline.  
   
   
       24 - 30 . (canceled)  
   
   
       31 . A method for inhibition of HPV-induced unregulated cell growth in a subject comprising the steps of: 
 (a) providing a first composition comprising tetra-O-methyl nordihydroguaiaretic acid (M 4 N); and    (b) applying the first composition to the tumor.    
   
   
       32 . The method of  claim 31 , wherein the step of applying the first composition to the tumor comprises administering the first composition to the subject.  
   
   
       33 . The method of  claim 32 , wherein the subject is a mammal.  
   
   
       34 . The method of  claim 33 , wherein the mammal is a human.  
   
   
       35 . The method of  claim 31 , wherein the HPV-induced unregulated cell growth is benign.  
   
   
       36 . The method of  claim 31 , wherein the HPV-induced unregulated cell growth is a tumor (Supported by specification at, for example, page 2, lines 21 to 23) and the tumor is penile or head and neck cancer.  
   
   
       37 . The method of  claim 31 , wherein the first composition further comprises a first pharmaceutically acceptable excipient or carrier.  
   
   
       38 . The method of  claim 37 , wherein the first pharmaceutically acceptable excipient or carrier comprises dimethylsulfoxide (DMSO).  
   
   
       39 . The method of  claim 31 , wherein the step of applying the first composition to the tumor comprises injecting the first composition into the tumor.  
   
   
       40 . The method of  claim 31 , wherein the step of applying the first composition to the tumor comprises applying the first composition topically.  
   
   
       41 . The method of  claim 31 , wherein the step of applying the first composition to the tumor comprises targeted delivery to the tumor site.  
   
   
       42 . The method of  claim 31 , wherein the first composition comprises tetra-O-methyl nordihydroguaiaretic acid (M 4 N) at a concentration of 200 mg/ml.  
   
   
       43 . The method of  claim 42 , further comprising the step of applying a second composition comprising tetraglycinyl nordihydroguaiaretic acid (G 4 N) to the tumor.  
   
   
       44 . The method of  claim 43 , wherein the second composition comprises tetraglycinyl nordihydroguaiaretic acid (G 4 N) at a concentration of 200 mg/ml.  
   
   
       45 . The method of  claim 31 , wherein the tetra-O-methyl nordihydroguaiaretic acid (M 4 N) is applied at a dose of from 10 mg to 20 mg per gram tumor weight.  
   
   
       46 . The method of  claim 42 , wherein 50 μl to 100 μl of the first composition is applied to the tumor.  
   
   
       47 . A method of treating HSV infected skin in a subject comprising the steps of: 
 (a) providing a composition comprising a NDGA derivative; and    (b) applying the composition to HSV infected skin.    
   
   
       48 . The method of  claim 47 , wherein the composition is applied more than once per day.  
   
   
       49 . The method of  claim 48 , wherein the composition is applied 5 times per day.  
   
   
       50 . The method of  claim 47 , wherein the composition is applied to the skin daily for more than one day.  
   
   
       51 . The method of  claim 50 , wherein the composition is applied to the skin daily for 6 days.  
   
   
       52 . The method of  claim 47 , wherein the NDGA derivative has the formula  
     
       
         
         
             
             
         
       
     
     wherein R 1 , R 2 , R 3 , and R 4  independently represent —OH, —OCH 3 , —O(C═O)CH 3 , or an amino acid residue, but are not each —OH simultaneously.  
   
   
       53 . The method of  claim 52 , wherein the NDGA derivative is tetra-O-methyl nordihydroguaiaretic acid (M 4 N).  
   
   
       54 . The method of  claim 47 , wherein the NDGA derivative is present in the composition at a concentration of 60 mg/ml.  
   
   
       55 . The method of  claim 47 , wherein the composition further comprises a pharmaceutically acceptable carrier.  
   
   
       56 . A pharmaceutical composition for treatment of HSV infected skin comprising a NDGA derivative and a pharmaceutically acceptable carrier, wherein the NDGA derivative is present in the composition at a concentration of 60 mg/ml.  
   
   
       57 . The pharmaceutical composition of  claim 56 , wherein the pharmaceutically acceptable carrier is DMSO.  
   
   
       58 . A method of inhibiting Sp1 binding activity to DNA in a eukaryotic cell comprising the steps of: 
 (a) providing a composition comprising an effective amount of NDGA derivative; and    (b) contacting the cell with the composition to inhibit Sp1 binding to the DNA.    
   
   
       59 . The method of  claim 58 , wherein the NDGA derivative has the formula  
     
       
         
         
             
             
         
       
     
     wherein R 1 , R 2 , R 3 , and R 4  independently represent —OH, —OCH 3 , —O(C═O)CH 3 , or an amino acid residue, but are not each —OH simultaneously.  
   
   
       60 . The method of  claim 59 , wherein the NDGA derivative is G 4 N.  
   
   
       61 . A method of inhibiting Tat transactivation of HIV promoter in a cell comprising the steps of: 
 (a) providing a composition comprising an effective amount of G 4 N; and    (b) exposing the HIV promoter to the composition.    
   
   
       62 . The method of  claim 61 , wherein G 4 N is present at a concentration of about 5 μM to about 100 μM.  
   
   
       63 . A method of down-regulating CDC2 expression in a cell comprising the steps of: 
 (a) providing a composition comprising a NDGA derivative; and    (b) contacting the cell with the composition.    
   
   
       64 . The method of  claim 63 , wherein the NDGA derivative has the formula  
     
       
         
         
             
             
         
       
     
     wherein R 1 , R 2 , R 3 , and R 4  independently represent —OH, —OCH 3 , —O(C═O)CH 3 , or an amino acid residue, but are not each —OH simultaneously.  
   
   
       65 . The method of  63 , wherein the NDGA derivative is M 4 N.

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