US2015232439A1PendingUtilityA1

Process for the preparation of c-fms kinase inhibitors

Assignee: JANSSEN PHARMACEUTICA NVPriority: Aug 7, 2012Filed: May 6, 2015Published: Aug 20, 2015
Est. expiryAug 7, 2032(~6 yrs left)· nominal 20-yr term from priority
A61P 9/10A61P 37/06A61P 3/10A61P 35/04A61P 43/00A61P 25/04A61P 3/00A61P 31/18A61P 35/02A61P 31/00A61P 25/18A61P 27/02A61P 35/00A61P 29/00A61P 25/28A61P 25/00A61P 19/10C07D 405/14A61P 19/00C07D 493/18C07D 493/08C07F 7/10A61P 13/12A61P 19/02A61P 11/06C07D 309/30A61P 17/06C07D 409/14C07D 409/12C07D 451/06A61P 15/00A61P 1/04A61P 1/18A61P 13/08C07D 405/12A61P 11/00
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Claims

Abstract

The present invention is directed to a process for the preparation of heterocyclic derivatives of formula I wherein J, X, Z, and R 2 are as defined herein. Such compounds are useful as protein tyrosine kinase inhibitors, more particularly inhibitors of c-fms kinase.

Claims

exact text as granted — not AI-modified
1 - 75 . (canceled) 
     
     
         76 . A process for the preparation of a compound of formula (XX) 
       
         
           
           
               
               
           
         
         comprising 
       
       
         
           
           
               
               
           
         
       
       reacting a compound of formula (XXII) is reacted with NfsulphF, in the presence of DBU; in an organic solvent; at a temperature of from about 0° C. to about room temperature; to yield the corresponding compound of formula (XX). 
     
     
         77 . A process according to  claim 76 , wherein the NfsulphF is present in an amount of form about 1.0 molar equivalents to about 1.5 molar equivalents. 
     
     
         78 . A process according to  claim 77 , wherein the NfsulphF is present in an amount of form about 1.1 molar equivalents to about 1.3 molar equivalents. 
     
     
         79 . A process according to  claim 78 , wherein the NfsulphF is present in an amount of about 1.2 molar equivalents. 
     
     
         80 . A process according to  claim 76 , wherein the DBU is present in an amount in the range of from about 1.1 molar equivalents to about 4.0 molar equivalents. 
     
     
         81 . A process according to  claim 80 , wherein the DBU is present in an amount of from about 1.5 molar equivalents to about 2.5 molar equivalents. 
     
     
         82 . A process according to  claim 81 , wherein the DBU is present in an amount of about 2.0 molar equivalents. 
     
     
         83 . A process according to  claim 76 , wherein the organic solvent is selected from the group consisting of 2-methyl-THF, THF and toluene. 
     
     
         84 . A process according to  claim 83 , wherein the organic solvent is 2-methyl-THF. 
     
     
         85 . A process according to  claim 76 , wherein the compound of formula (XXII) is reacted with NfsulphF at a temperature of from about 0° C. to about room temperature. 
     
     
         86 . A process according to  claim 85 , wherein the compound of formula (XXII) is reacted with NfsulphF at about room temperature.

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