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US 11,634,403 B2Granted
IRE1 small molecule inhibitors
AssigneeCornell University
InventorsJoseph P. Vacca, Dansu Li, Sarah Elizabeth Bettigole
Life of this patent
Estimating the term…
Abstract
Provided herein are small molecule inhibitors for the targeting or IRE1 protein family members. Binding may be direct or indirect. Further provided herein are methods of using IRE1 small molecule inhibitors for use in treating or ameliorating cancer in a subject. Moreover, IRE1 small molecule inhibitors described herein are for the treatment of cancer, where the cancer is a solid or hematologic cancer.
Claims22
A compound of Formula (I), or a pharmaceutically acceptable salt:
- wherein,
- each Z is independently N or CR1, provided that at least one Z is N;
- each R1 is independently halogen, —OR8, or C1-C4alkyl;
- R3 is C1-C4alkyl, or —O—C1-C4alkyl;
- R4 is halogen, or C1-C4alkyl;
- each R5 is independently H, halogen, or C1-C4alkyl;
- each R2 is independently H, or C1-C4alkyl;
- R6 is H, or C1-C4alkyl;
- R7 is C3-C6cyclooalkylalkyl, C1-C4alkyl, —CH2CF3, —CH2-cyclopropyl, or —CH2CH2OCH3;
- each R8 is C1-C4alkyl;
- each R9 is C1-C4alkyl;
- RA1 and RA2 are each independently H, halogen, —OR9, C1-C4alkyl, or C1-C4fluoroalkyl;
- provided that both RA1 and RA2, are not H;
- n is 1,2,3, or 4;
- and
- q is 1, 2, 3, or 4.
13 more elements
A compound, or a pharmaceutically acceptable salt thereof, selected from:
- 2-chloro-N-(5-(8-ethyl-2-(((18,4r)4-(methylamino)cyclohexyl)amino)quinazolin-6yl)-3-fluoro-6-methoxypyridin-2yl)benzenesulfonamide;
- 2-chloro-N-(5-(2-(((11,4r)-4(dimethylamino)cyclohexyl)amino)8-ethylquinazolin-6-yl)-3-fluoro 6-methoxypyridin-2yl)benzenesulfonamide;
- 2-chloro-N-(5-(2-(((18,4s)-4(dimethylamino)cyclohexyl) amino)8-ethylquinazolin-6-yl)-3-fluoro 6-methoxypyridin-2 yl)benzenesulfonamide;
- 2-chloro-N-(5-(2-(((15,4s)-4 (dimethylamino)-4 methylcyclohexyl) amino)-8 ethylquinazolin-6-yl)-3-fluoro-6 methoxypyridin-2 yl) benzenesulfonamide;
- 2-chloro-N-(5-(2-(((11,4r)-4 (dimethylamino)cyclohexyl)amino)8-methylquinazolin-6-yl)-3 fluoro-6-methoxypyridin-2 yl)benzenesulfonamide;
- 2-chloro-N-(5-(2-(((15,4s)-4 (dimethylamino)cyclohexyl)amino)8-methylquinazolin-6-yl)-3 fluoro-6-methoxypyridin-2 yl)benzenesulfonamide;
- 2-chloro-N-(5-(2-(((11,4r)-4 (dimethylamino)cyclohexyl)amino)8-fluoroquinazolin-6-yl)-3-fluoro 6-methoxypyridin-2 yl)benzenesulfonamide;
- 2-chloro-N-(5-(2-(((18,4r)-4 (dirnethylamino)cyclohexyl)amino)8-fluoroquinazolin-6-yl)-3-fluoro 6-methylpyridin-2 yl)benzenesulfonamide;
- and
- 2-chloro-N-(5-(2-(((11,4r)-4 (dimethylamino)cyclohexyl)amino)8-ethyl-7-fluoroquinazolin-6-yl)3-fluoro-6-methylpyridin-2yl)benzenesulfonamide.
7 more elements
Dependencies are inferred from the claim text.