US2024002384A1PendingUtilityA1

3,4-dihydro-2,7-naphthyridine-1,6(2h,7h)-diones as mek inhibitors

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Assignee: PFIZERPriority: Mar 31, 2021Filed: Sep 18, 2023Published: Jan 4, 2024
Est. expiryMar 31, 2041(~14.7 yrs left)· nominal 20-yr term from priority
Inventors:Shelley AllenPatrick Michael Doerner BarbourJames F. BlakeSydney Taylor BlancheMark Laurence BoysWesley Dewitt ClarkConnor James CowdreyJoshua Ryan DahlkeAlex Andrew KellumEllen Margaret KnappDavid A. MorenoJacob Matthew O'LearyLi RenFaith WitkosJennifer Fulton
C07D 471/04A61P 35/00A61K 31/4375A61K 45/06
75
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Claims

Abstract

The invention relates to a method of treating a MEK-associated tumor by administering to a subject in need thereof a therapeutically effective amount of a solid form 8-((2-fluoro-4-(methylthio)phenyl)amino)-2-(2-hydroxyethoxy)-7-methyl-3,4-dihydro-2,7-naphthyridine-1,6(2H,7H)-dione.

Claims

exact text as granted — not AI-modified
We claim: 
     
         1 . A method of treating a MEK-associated tumor, the method comprising:
 administering to a subject in need thereof a therapeutically effective amount of a crystalline form of 8-((2-fluoro-4-(methylthio)phenyl)amino)-2-(2-hydroxyethoxy)-7-methyl-3,4-dihydro-2,7-naphthyridine-1,6(2H,7H)-dione.   
     
     
         2 . The method of  claim 1 , where the crystalline form of 8-((2-fluoro-4-(methylthio)phenyl)amino)-2-(2-hydroxyethoxy)-7-methyl-3,4-dihydro-2,7-naphthyridine-1,6(2H,7H)-dione is a monohydrate or anhydrous. 
     
     
         3 . The method of  claim 1 , where the crystalline form of 8-((2-fluoro-4-(methylthio)phenyl)amino)-2-(2-hydroxyethoxy)-7-methyl-3,4-dihydro-2,7-naphthyridine-1,6(2H,7H)-dione is anhydrous and has a PXRD pattern comprising peaks at 5.0, 8.7, 9.3, 10.8, 14.5, 15.3, 18.8, and 20.5 degrees 2-theta (±0.2 degrees 2-theta). 
     
     
         4 . The method of  claim 1 , where the crystalline form of 8-((2-fluoro-4-(methylthio)phenyl)amino)-2-(2-hydroxyethoxy)-7-methyl-3,4-dihydro-2,7-naphthyridine-1,6(2H,7H)-dione is anhydrous and has a PXRD pattern comprising peaks at 7.1, 9.4, 12.4, 12.8, 14.3, 15.6, 16.4, 17.4, 18.5, 18.9, 19.5, 19.9, 21.1, 21.4, 23.2, 23.7, 24.8, 25.6, 27.6, 30.3, 33.2, 33.5, and 37.5 degrees 2-theta (±0.2 degrees 2-theta). 
     
     
         5 . The method of  claim 1 , where the crystalline form of 8-((2-fluoro-4-(methylthio)phenyl)amino)-2-(2-hydroxyethoxy)-7-methyl-3,4-dihydro-2,7-naphthyridine-1,6(2H,7H)-dione is a monohydrate and has a PXRD pattern comprising peaks at 13.7, 18.0, and 18.3 degrees 2-theta (±0.2 degrees 2-theta). 
     
     
         6 . A method of treating a MEK-associated tumor, the method comprising:
 administering to a subject in need thereof a therapeutically effective amount of amorphous 8-((2-fluoro-4-(methylthio)phenyl)amino)-2-(2-hydroxyethoxy)-7-methyl-3,4-dihydro-2,7-naphthyridine-1,6(2H,7H)-dione.   
     
     
         7 . The method of  claim 3 , wherein the MEK-associated tumor has a BRAF V600 mutation selected from V600E, V600K, V600D, V600R and V600S. 
     
     
         8 . The method of  claim 4 , wherein the MEK-associated tumor has a BRAF V600 mutation selected from V600E, V600K, V600D, V600R and V600S. 
     
     
         9 . The method of  claim 5 , wherein the MEK-associated tumor has a BRAF V600 mutation selected from V600E, V600K, V600D, V600R and V600S. 
     
     
         10 . The method of  claim 6 , wherein the MEK-associated tumor has a BRAF V600 mutation selected from V600E, V600K, V600D, V600R and V600S. 
     
     
         11 . The method of  claim 3 , wherein the MEK-associated tumor is a BRAF wild-type tumor. 
     
     
         12 . The method of  claim 4 , wherein the MEK-associated tumor is a BRAF wild-type tumor. 
     
     
         13 . The method of  claim 5 , wherein the MEK-associated tumor is a BRAF wild-type tumor. 
     
     
         14 . The method of  claim 6 , wherein the MEK-associated tumor is a BRAF wild-type tumor. 
     
     
         15 . The method of  claim 3 , wherein the MEK-associated tumor is a CNS tumor. 
     
     
         16 . The method of  claim 4 , wherein the MEK-associated tumor is a CNS tumor. 
     
     
         17 . The method of  claim 5 , wherein the MEK-associated tumor is a CNS tumor. 
     
     
         18 . The method of  claim 6 , wherein the MEK-associated tumor is a CNS tumor. 
     
     
         19 . The method of  claim 3 , wherein the MEK-associated tumor has a BRAF fusion. 
     
     
         20 . The method of  claim 4 , wherein the MEK-associated tumor has a BRAF fusion. 
     
     
         21 . The method of  claim 5 , wherein the MEK-associated tumor has a BRAF fusion. 
     
     
         22 . The method of  claim 6 , wherein the MEK-associated tumor has a BRAF fusion.

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