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US 9,850,216 B2Granted
Inhibitors of ACK1/TNK2 tyrosine kinase
AssigneeH. Lee Moffitt Cancer Center and Research Institute, Inc.
InventorsNupam P. Mahajan, Kiran N. Mahajan, Nicholas J. Lawrence, Harshani R. Lawrence
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Abstract
Described are cancer therapies and anti-cancer compounds. In particular, disclosed are inhibitors of Ack1 tyrosine kinase and their use in the treatment of cancer. Methods of screening for new Ack1 tyrosine kinase inhibitors are also disclosed. In specific example, compound having Formula I through IV are disclosed.
Claims6
A compound having Formula IA:
- wherein
- R1 is Cl, Br, F, CH3, or C2H5;
- m is 1 or 2;
- and
- at least one R4 is a cycloalkyl or heterocycloalkyl that is unsubstituted or substituted with R6, and, if present, the other R4 is OH, Cl, Br, F, C1-C6 alkyl, CN, NO2, or OR5 where
- R5 is C1-C6 alkyl, heteroalkyl, cycloalkyl, heterocycloalkyl, or heteroaryl;
- and
- R6 is OH, Cl, Br, F, C1-C6 alkyl, CO2H, CO2R5, OC(O)R5, (CH2)1-6CO2H, C(O)(CH2)1-6CO2H, (CH2)1-6CO2R5, C(O)(CH2)1-6CO2R5, OR5, C(O)R5, C(O)NH2, C(O)NHR5, SO2NH2, SO2NHR5, C(O)NHSO2R5, 4-morpholinyl, 4-piperazinyl, 1-piperidinyl, 4-piperadinyl group, or PEG-sterol,
- or a pharmaceutically acceptable salt thereof.
6 more elements
Dependencies are inferred from the claim text.