US2012157441A1PendingUtilityA1

Inhibitors of the mutant form of kit

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Assignee: BUCHDUNGER ELISABETHPriority: Nov 18, 2003Filed: Jan 25, 2012Published: Jun 21, 2012
Est. expiryNov 18, 2023(expired)· nominal 20-yr term from priority
Inventors:Elisabeth BuchdungerDoriano Fabbro
A61P 3/04A61P 35/02A61P 43/00A61P 35/00A61K 31/553A61K 31/506G01N 2800/44A61K 31/502
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Claims

Abstract

The present invention relates to the treatment of KIT dependent diseases that are characterized by a mutant form of KIT whereby the mutant KIT is identified and an appropriate inhibitor of the mutant KIT selected form midostaurin, vatalanib and compound A is administered.

Claims

exact text as granted — not AI-modified
1 . A method of treating a KIT dependent disease in a patient, which comprises: (a) identifying a mutant form of KIT associated with the KIT dependent disease; and (b) administering to said patient an effective mutant KIT inhibiting amount of an inhibitor selected from the group consisting of midostaurin and vatalanib. 
     
     
         2 . A method of  claim 1 , wherein the mutant form of KIT is selected from D816F, D816H, D816N, D816Y, D816V, K642E, Y823D, Del 550-558, Del 557-561, N822K, V654A, N822H, Del 550-558+V654A, Del 557-561+V654A, Ins503AY, V560G, 558NP, Del 557 558, Del W559-560, F522C, Del 579, R634W, K642E, T8011, C809G, D820Y, N822K, N822H, Y823D, Y823C and T6701. 
     
     
         3 . A method of  claim 2 , wherein the mutant form of KIT is selected from D816F, D816H, D816N, D816Y, D816V, K642E, Y823D, Del 550-558, Del 557-561, N822K, V654A, N822H, Del 550-558+V654A, Del 557-561+V654A. 
     
     
         4 . A method of  claim 1 , wherein the KIT dependent disease is resistant to treatment with imatinib. 
     
     
         5 . A method of  claim 3 , wherein the mutant form of KIT is D816F and the inhibitor is selected from the group consisting of midostaurin. 
     
     
         6 . A method of  claim 3 , wherein the mutant form of KIT is D816H and the inhibitor is selected from the group consisting of midostaurin. 
     
     
         7 . A method of  claim 3 , wherein the mutant form of KIT is D816N and the inhibitor is selected from the group consisting of midostaurin. 
     
     
         8 . A method of  claim 3 , wherein the mutant form of KIT is D816Y and the inhibitor is selected from the group consisting of midostaurin. 
     
     
         9 . A method of  claim 3 , wherein the mutant form of KIT is D816V and the inhibitor is selected from the group consisting of midostaurin. 
     
     
         10 . A method of  claim 3 , wherein the mutant form of KIT is K642E and the inhibitor is selected from the group consisting of midostaurin and vatalanib. 
     
     
         11 . A method of  claim 3 , wherein the mutant form of KIT is Y823D and the inhibitor is selected from the group consisting of midostaurin and vatalanib. 
     
     
         12 . A method of  claim 3 , wherein the mutant form of KIT is Del 550-558 and the inhibitor is selected from the group consisting of midostaurin and vatalanib. 
     
     
         13 . A method of  claim 3 , wherein the mutant form of KIT is Del 557-561 and the inhibitor is selected from the group consisting of midostaurin and vatalanib. 
     
     
         14 . A method of  claim 3 , wherein the mutant form of KIT is N822K and the inhibitor is selected from the group consisting of midostaurin and vatalanib. 
     
     
         15 . A method of  claim 3 , wherein the mutant form of KIT is V654A and the inhibitor is selected from the group consisting of midostaurin. 
     
     
         16 . A method of  claim 3 , wherein the mutant form of KIT is N822H and the inhibitor is selected from the group consisting of midostaurin and vatalanib. 
     
     
         17 . A method of  claim 3 , wherein the mutant form of KIT is Del 550-558 V654A and the inhibitor is selected from the group consisting of midostaurin and vatalanib. 
     
     
         18 . A method of  claim 3 , wherein the mutant form of KIT is Del 557-561+V654A and the inhibitor is selected from the group consisting of midostaurin. 
     
     
         19 . A method of  claim 2 , wherein the mutant form of KIT is selected from the group consisting of D816H, D816F, D816N and D816Y and the inhibitor is midostaurin. 
     
     
         20 . A method of  claim 2 , wherein the mutant form of KIT is selected from the group consisting of D816V, K642E, Y823D, De1550-558, Del 557-561, N822K, V654A, N822H, Del 550-558+V654A, and Del 557-561+V654A and the inhibitor is midostaurin. 
     
     
         21 . A method of  claim 2 , wherein the mutant form of KIT is selected from the group consisting of K642E, Y823D, Del 550-558, Del 557-561, N822K and N822H and the inhibitor is vatalanib. 
     
     
         22 . A method according to  claim 1 , wherein the KIT dependent disease is selected from mast cell diseases, acute myelogenous leukemia, gastrointestinal stromal tumors, seminomas and dysgerminomas. 
     
     
         23 . A method of  claim 4 , wherein the inhibitor is midostaurin. 
     
     
         24 . A method of  claim 4 , wherein the inhibitor is vatalanib.

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