Back to results
US 12,662,465 B2Granted
EGFR inhibitors
AssigneeBlueprint Medicines Corporation
InventorsOmar Ahmad, John Emmerson Campbell, Thomas A. Dineen, Meredith Suzanne Eno, Dilinie Prasadhini Fernando, Chandrasekhar V. Miduturu
Life of this patent
Estimating the term…
Abstract
The present disclosure provides a compound represented by structural formula (I-0): or a pharmaceutically acceptable salt thereof useful for treating a cancer.
Claims18
A compound of Formula (I-0)
- or a pharmaceutically acceptable salt thereof, wherein
- X1, X2, X3, X4, and X5 is CR3c, N, or N+—O−, provided that at least 3 of X1, X2, X3, X4, and X5 is CR3c;
- X6 is CH;
- X7 and X8 is N
- R1 is C1-C6alkyl, C3-C6cycloalkyl, or 4- to 12-membered heterocyclyl, wherein the alkyl, cycloalkyl, and heterocyclyl represented by R1 is optionally substituted with 1 to 4 groups independently selected from deuterium, halo, C1-C4alkyl, ═O, OH, C1-C4alkoxy, NR1aR1b, and 4 to 8 membered heterocyclyl, wherein the heterocyclyl is optionally substituted with methyl, ethyl, or —(CH2)mNR1aR1b;
- R2 is halo, NR1aR1b, C1-C4alkyl, C1-C4alkoxy, C3-C6cycloalkyl, 4- to 12-membered heterocyclyl, or 5 or 6 membered heteroaryl, wherein the alkyl, alkoxy, cycloalkyl, heterocycyl, and heteroaryl represented by R2 are each optionally substituted with 1 to 4 groups selected from deuterium, halo, ═O (as valence permits), OH, NR1aR1b, C(O)CH3, C1-C4alkyl and C1-C4alkoxy, wherein the C1-C4alkyl and C1-C4alkoxy are each optionally substituted with 1 to 3 groups selected from deuterium, halo, OH, and OCH3;
- R3a is H, deuterium, halo, OH, C1-4alkyl, or C1-C4alkoxy;
- R3b is H, deuterium, halo, OH, C1-4alkyl, or C1-C4alkoxy;
- Each R3c is independently selected from H, deuterium, halo, OH, C1-4alkyl, and C1-C4alkoxy, wherein no more than 3 R3c are halo, OH, C1-4alkyl, or C1-C4alkoxy;
- R1a is H, deuterium, C1-C4alkyl, or C3-C6cycloalkyl;
- R1b is H, deuterium, C1-C4alkyl, or C3-C6cycloalkyl;
- R4 is H or deuterium;
- R5 is H or deuterium;
- and m is 0 or 1.
11 more elements
A compound of Formula (I)
- or a pharmaceutically acceptable salt thereof, wherein
- X1, X2, X3, X4, and X5 is CR3c or N, provided that at least 3 of X1, X2, X3, X4, and X5 is CR3c;
- R1 is C1-C6 alkyl, C3-C6cycloalkyl, 4 to 12 membered heterocyclyl, wherein the alkyl, cycloalkyl, and heterocyclyl represented by R1 is optionally substituted with 1 to 4 groups independently selected from halo, C1-C4alkyl, ═O, OH, C1-C4alkoxy, NR1aR1b, and 4 to 8 membered heterocyclyl, wherein the heterocyclyl is optionally substituted with —(CH2)mNR1aR1b;
- R2 is C1-C4alkoxy, 4 to 12 membered heterocyclyl, 5 or 6 membered heteroaryl, wherein the heterocycyl, and heteroaryl represented by R2 are each optionally substituted with 1 to 4 groups selected from C1-C4alkyl and C1-C4alkoxy, wherein the C1-C4 alkyl and C1-C4alkoxy are each optionally substituted with 1 to 3 groups selected from halo, OH and OCH3;
- R3a is H, halo, OH, C1-4alkyl, or C1-C4alkoxy;
- R3b is H, halo, OH, C1-4alkyl, or C1-C4 alkoxy;
- Each R3c is independently selected from H, halo, OH, C1-4alkyl, and C1-C4 alkoxy, wherein no more than 3 R3c are halo, OH, C1-4alkyl, or C1-C4alkoxy;
- R1a is H, C1-C4alkyl, or C3-C6cycloalkyl;
- R1b is H, C1-C4alkyl, or C3-C6cycloalkyl;
- and
- m is 0 or 1.
8 more elements
Dependencies are inferred from the claim text.