US2013303534A1PendingUtilityA1

Compounds and methods for kinase modulation, and indications therefor

63
Assignee: PLEXXIKON INCPriority: Jun 22, 2005Filed: Mar 5, 2013Published: Nov 14, 2013
Est. expiryJun 22, 2025(expired)· nominal 20-yr term from priority
Inventors:Prabha N. IbrahimDean R. ArtisRyan BremerGaston HabetsShumeye MamoMarika NespiChao ZhangJiazhong ZhangYong-Liang ZhuRebecca ZuckermanBrian WestYoshisa SuzukiJianming TsaiKlaus-Peter HirthGideon BollagWayne SpevakHanna ChoSamuel J. GilletteGuoxian WuHongyao ZhuShenghua Shi
A61P 9/00A61P 37/00A61P 3/06A61P 9/10A61P 7/00A61P 37/08A61P 7/02A61P 35/02A61P 3/10A61P 9/04A61P 43/00A61P 37/06A61P 37/02A61P 25/16A61P 31/16A61P 25/00A61P 3/04A61P 29/00A61P 25/14A61P 31/04A61P 25/06A61P 25/28A61P 35/00A61P 27/16A61P 3/14A61P 27/02A61P 1/16A61P 1/04A61P 1/00A61P 17/06A61P 17/02A61P 19/02A61P 1/18A61P 11/00A61P 15/08A61P 19/10A61P 21/04A61P 17/00A61P 11/06A61P 13/08A61P 13/12C07C 37/62A61K 31/496A61K 31/5377C07D 209/08C07C 47/575C07C 45/00C07D 471/04A61K 31/437C07C 45/71C07C 45/673C07C 39/27A61K 31/416C07C 47/565A61K 31/435
63
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Claims

Abstract

Compounds active on protein kinases are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases.

Claims

exact text as granted — not AI-modified
That which is claimed is: 
     
         1 . A method of treating a patient diagnosed with metastatic melanoma comprising:
 (a) identifying a metastatic melanoma patient who is positive for a  V600E BRAF mutation; and   (b) administering to the patient identified in step (a) an effective amount of a sulfonamide compound or a pharmaceutically acceptable salt thereof, whose chemical structure includes a Core Moiety I, as shown below:   
       
         
           
           
               
               
           
         
         in which R 112  is amino, substituted amino, aryl, substituted aryl, heteroaryl, substituted heteroaryl, or lower alkyl; 
         R 83  is hydrogen, fluoro, or chloro; and 
       
       
         
           
           
               
               
           
         
       
       represents a carbon-carbon bond connecting the Core Moiety I with the remainder of the compound, which comprises a hydrocarbon having 8-18 carbon atoms and one or more heteroatoms. 
     
     
         2 . The method of  claim 1  in which R 112  is a substituted aryl. 
     
     
         3 . The method of  claim 2  in which the substituted aryl is a fluorobenzene radical. 
     
     
         4 . The method of  claim 2  in which the substituted aryl is a difluorobenzene radical. 
     
     
         5 . The method of  claim 2  in which R 83  is hydrogen. 
     
     
         6 . The method of  claim 1  in which R 112  is a lower alkyl. 
     
     
         7 . The method of  claim 1  in which the lower alkyl is n-propyl. 
     
     
         8 . The method of  claim 7  in which R 83  is fluoro. 
     
     
         9 . The method of  claim 1  in which R 112  is a difluorobenzene radical and R 83  is hydrogen. 
     
     
         10 . The method of  claim 1  in which the remainder of the compound includes a heteroaryl moiety. 
     
     
         11 . The method of  claim 10  in which the heteroaryl moiety includes two nitrogen atoms. 
     
     
         12 . The method of  claim 1  in which the patient's cancer has metastasized to the patient's brain.

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