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US 2022/0064144 A1Published application
Benzimidazole compounds as c-kit inhibitors
AssigneeARIAD Pharmaceuticals, Inc.
InventorsNicholas E. BENCIVENGA, David C. DALGARNO, Joseph M. GOZGIT, Wei-Sheng HUANG, Anna KOHLMANN, Feng LI, Jiwei QI, William C. SHAKESPEARE, Ranny M. THOMAS, Yihan WANG, Yun ZHANG, Xiaotian ZHU
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Abstract
The invention relates to c-Kit inhibitors useful in the treatment of cancers, and other serine-threonine kinase mediated diseases, having the Formula: (I) where A, L, R1, R2, R3, and n are described herein.
Claims20
-29. (canceled)
A compound having one of the following formulae (Ii) or (Ij):
- or a pharmaceutically acceptable salt thereof, wherein
- R1 is H;
- R2 is —(C(R6a)2)p-heteroaryl wherein the heteroaryl comprises a 5- or 6-membered ring and 1 to 3 heteroatoms selected from N, O, and S, wherein the heteroaryl is optionally substituted with one or more R9;
- R3 is (C1-C6) alkyl or halogen;
- R4 is (C1-C5) haloalkyl;
- R5 is H;
- each R9 is independently at each occurrence (C1-C6) alkyl or 5- to 7-membered heterocycloalkyl ring comprising 1 to 3 heteroatoms selected from N, O and S, wherein the heterocycloalkyl is optionally substituted with one or more substituents each independently selected from (C1-C6) alkyl or —C(Q)H, and wherein the alkyl is optionally substituted with one or more substituents each independently selected from (C1-C5) alkoxy, —OH, or (C1-C6) dialkylamino;
- p is 0;
- and
- n is 0, 1 or 2.
7 more elements
31-32. (canceled)
-38. (canceled)
(canceled)
-49. (canceled)
(canceled)
Dependencies are inferred from the claim text.