US2020323827A1PendingUtilityA1

Ite for cancer intervention and eradication

Assignee: ARIAGEN INCPriority: Nov 2, 2009Filed: Jun 22, 2020Published: Oct 15, 2020
Est. expiryNov 2, 2029(~3.3 yrs left)· nominal 20-yr term from priority
Inventors:Jiasheng Song
Y02E10/50A61P 43/00E04D 1/20A61K 31/475C08L 75/04A61P 35/00C07D 417/06C08G 2101/00A61K 31/40A61K 31/425E04D 1/28H02S 20/25Y02B10/10E04D 1/30A61K 31/427A61K 45/06
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Claims

Abstract

A method of cancer intervention or eradication by administering an effective amount of an endogenous ligand for the aryl hydrocarbon (Ah) receptor (AhR) named ITE or one of its analogs (the active ingredient) to a subject with cancer is disclosed. An effective dose and dosing frequency of the active ingredient are determined by measuring its blood levels of the subject after dosing. The active ingredient formulated with a carrier system is applied topically, enterally, or parenterally to the subject. The formulated drug can also be administered together with one or more of other cancer therapeutic agents. A maintenance dosing is provided after the subject is free of cancer to insure the cancer eradication. Subjects with cancers of prostate, liver, lung, ovarian, and breast are preferably accepted for treatment.

Claims

exact text as granted — not AI-modified
1 . A method of stimulating the immune system in a human patient in need thereof, comprising administering a therapeutically effective amount of a compound of structural formula 4: 
       
         
           
           
               
               
           
         
         wherein:
 X and Y are independently selected from the group consisting of O (oxygen) and S (sulfur); 
 R N  is selected from the group consisting of hydrogen, halo, cyano, formyl, alkyl, haloalkyl, alkenyl, alkynyl, alkanoyl, haloalkanoyl, and a nitrogen protective group; 
 R 1 , R 2 , R 3 , R 4 , and R 5  are independently selected from the group consisting of hydrogen, halo, hydroxy, thiol, cyano, formyl, alkyl, haloalkyl, alkenyl, alkynyl, amino, nitro, alkoxy, haloalkoxy, thioalkoxy, alkanoyl, haloalkanoyl, and carbonyloxy; 
 R 6  is 
 
       
       
         
           
           
               
               
           
         
         
           wherein R 10  is amino; and 
           R 7  is selected from the group consisting of hydrogen, halo, hydroxy, thiol, cyano, formyl, alkyl, haloalkyl, alkenyl, alkynyl, amino, nitro, alkoxy, haloalkoxy, and thioalkoxy. 
         
       
     
     
         2 . The method of  claim 1 , wherein the amino of R 10  has the formula —NR a R b , wherein R a  and R b  are independently selected from the group consisting of hydrogen and alkyl. 
     
     
         3 . The method of  claim 2 , wherein R a  and R b  are each hydrogen. 
     
     
         4 . The method of  claim 2 , wherein R a  and R b  are each alkyl. 
     
     
         5 . The method of  claim 4 , wherein R a  and R b  are each methyl. 
     
     
         6 . The method of  claim 1 , wherein R N , R 1 , R 2 , R 3 , R 4 , R 5 , and R 7  are each independently selected from the group consisting of hydrogen, halo, and alkyl. 
     
     
         7 . The method of  claim 6 , wherein the amino of R 10  has the formula —NR a R b , wherein R a  and R b  are independently selected from the group consisting of hydrogen and alkyl. 
     
     
         8 . The method of  claim 7 , wherein R a  and R b  are each hydrogen. 
     
     
         9 . The method of  claim 8 , wherein R N , R 1 , R 2 , R 3 , R 4 , R 5 , and R 7  are each hydrogen. 
     
     
         10 . The method of  claim 7 , wherein R a  and R b  are each alkyl. 
     
     
         11 . The method of  claim 10 , wherein R a  and R b  are each methyl. 
     
     
         12 . The method of  claim 11 , wherein R N , R 1 , R 2 , R 3 , R 4 , R 5 , and R 7  are each hydrogen. 
     
     
         13 . The method of  claim 1 , wherein the patient has an increased count of white blood cells after the administering step. 
     
     
         14 . The method of  claim 1 , wherein the patient has an increased count of neutrophils after the administering step. 
     
     
         15 . The method of  claim 1 , wherein the patient has an increased count of lymphocytes after the administering step. 
     
     
         16 . The method of  claim 1 , wherein the patient has an increased count of platelets after the administering step.

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