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US 2019/0337894 A1Published application
Hsp90b n-terminal isoform-selective inhibitors
AssigneeUniversity of Kansas
InventorsBrian S.J. Blagg, Caitlin Nicole Kent, Anuj Khandelwal, Sanket Jaiprakash Mishra
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Abstract
The present technology provides compounds according to Formula (I) as well as compositions including such compounds useful for the treatment of cancers such as non-small cell lung cancer, bladder cancer, or colon cancer.
Claims25
A compound according to Formula I
- or a pharmaceutically acceptable salt and/or solvate thereof, wherein
- X1, X2, X3, and X4 are each independently selected from H, F, Cl, Br, I, sulfoxide, sulfone, nitro, pentafluorosulfanyl, C(O)OH, amide, or ester;
- R1 is OH, C1-C3 alkyl, C2-C4 alkenyl, or —CH2OH;
- R2 is CH2—X5 or OH, where X5 is OH, F, Cl, Br, CN, —C(O)—NR4R5, —NR6—C(O)H, —NR7—C(O)-alkyl, C(O)H, C(O)OH, sulfonamido, sulfoxide, sulfone, or S(O)2OH;
- or R1 and R2 together are (moving in the direction from R2 to R1) —C(X6)—CH2—, —C(X7)—CH(R8)—CH(R9)—, —C(X8)—N(R10)—CH(R11)—, —C(X9)—CH(R12)—CH(R13)—CH(R14)—, —C(X10)—N(R15)—CH(R16)—CH(R17)—, —O—CH═CH—, —O—N═CH—, —NH—CH═N—, or —CH═N—NH—;
- X6, X7, X8, X9, and X10 are each independently selected from O, CH2, and CF2;
- R3 is alkyl, —CH(CH3)2, CF3, Br, sulfonamido, sulfoxide, sulfone, nitro, pentafluorosulfanyl, C(O)OH, amide, or ester;
- R4, R5, R6, and R7 are each independently H or alkyl;
- R8, R9, R11, R12, R13, R14, R16, and R17 are each independently selected from H, C1-C3 alkyl, F, Cl, Br, I, or CF3;
- and
- R10 and R15 are each independently H or C1-C3 alkyl.
8 more elements
(canceled)
-13. (canceled)
-19. (canceled)
-24. (canceled)
-30. (canceled)
A compound according to Formula I
- or a pharmaceutically acceptable salt and/or solvate thereof, wherein
- X1, X2, X3, and X4 are each independently selected from H, F, Cl, Br, I, sulfoxide, sulfone, nitro, pentafluorosulfanyl, C(O)OH, amide, or ester;
- R1 is H, OH, C1-C3 alkyl, C2-C4 alkenyl, or —CH2OH;
- R2 is CH2—X5, where X5 is OH, F, Cl, Br, CN, —C(O)—NR4R5, —NR6—C(O)H, —NR7—C(O)-alkyl, C(O)H, C(O)OH, sulfonamido, sulfoxide, sulfone, or S(O)2OH;
- X6, X7, X8, X9, and X10 are each independently selected from O, CH2, and CF2;
- R3 is alkyl, —CH(CH3)2, CF3, Br, sulfonamido, sulfoxide, sulfone, nitro, pentafluorosulfanyl, C(O)OH, amide, or ester;
- and
- R4, R5, R6, and R7 are each independently H or alkyl.
5 more elements
Dependencies are inferred from the claim text.