US2023119470A1PendingUtilityA1

PYRAZINO[2,3-b]PYRAZINE mTOR KINASE INHIBITORS FOR ONCOLOGY INDICATIONS AND DISEASES ASSOCIATED WITH THE mTOR/PI3K/AKT PATHWAY

Assignee: SIGNAL PHARM LLCPriority: Oct 27, 2008Filed: Feb 25, 2022Published: Apr 20, 2023
Est. expiryOct 27, 2028(~2.3 yrs left)· nominal 20-yr term from priority
C07D 487/04A61P 29/00A61P 9/00A61P 25/28A61P 21/04C07D 519/00A61P 43/00C07D 471/14A61P 25/16A61P 11/02A61P 1/16A61P 35/00A61P 25/14C07D 487/10A61P 1/04C07D 498/14A61P 1/00A61P 17/02A61P 1/18A61P 3/04A61P 37/02A61P 37/06A61P 37/00A61P 3/10A61P 25/00A61P 35/02A61P 3/00A61K 31/4985A61P 25/08C07F 5/025C07D 241/20C07D 471/04A61P 13/12A61P 9/10A61P 11/06A61P 19/02A61P 19/06A61P 11/00A61P 17/06C07D 487/14
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Claims

Abstract

Provided herein are Heteroaryl Compounds having the following structure: wherein R 1 -R 4 are as defined herein, compositions comprising an effective amount of a Heteroaryl Compound and methods for treating or preventing cancer, inflammatory conditions, immunological conditions, neurodegenerative diseases, diabetes, obesity, neurological disorders, age-related diseases, or cardiovascular conditions, comprising administering an effective amount of a Heteroaryl Compound to a patient in need thereof.

Claims

exact text as granted — not AI-modified
1 - 20 . (canceled) 
     
     
         21 . A method for preparing a compound of formula (III), 
       
         
           
           
               
               
           
         
         the method comprising contacting a compound of formula (IV) 
       
       
         
           
           
               
               
           
         
         with R 2 —NH 2  in a solvent, in the presence of a base, wherein 
         R 2  is substituted or unsubstituted C 1-8  alkyl, 
         R 3  and R 4  are H, 
         X is a halogen, 
         Hal is a halogen, and 
         Hal 2  is Br or I. 
       
     
     
         22 . The method of claim  1 , wherein the solvent as acetonitrile or tetrahydrofuran. 
     
     
         23 . The method of claim  1 , wherein the base is triethylamine or diisopropylethylamine. 
     
     
         24 . The method of claim  1 , wherein halogen is Br 
     
     
         25 . The method of claim  1 , wherein Hal 2  is Br.

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