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US 12,435,067 B2Granted
Truncated itraconazole analogues and methods of use thereof
AssigneeUniversity of Connecticut
InventorMatthew Kyle Hadden
Life of this patent
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Abstract
Disclosed herein are analogues of itraconazole that are potent hedgehog signaling pathway inhibitors. The compounds are expected to be useful in the treatment of cell proliferation disorders such as cancer, particularly cancers that are dependent upon the hedgehog signaling pathway such as basal cell carcinoma and medulloblastoma.
Claims15
A compound having the structure of Formula (Ia-1), (Ia-2), (Ia-3), or (Ia-4)
- wherein
- Q is O;
- R1 is methyl;
- R4 is chloro;
- n is 2;
- and
- one of a), b), or c):
- a) J1 and J2 are absent and R3 is H;
- b) J1 is —C(═O)— or —C(═O)NH—N═CH—;
- J2 is absent, C1-4 alkyl, or C2-4 alkenyl;
- and
- R3 is unsubstituted or substituted phenyl or pyridyl;
- or
- c) J1 is absent;
- J2 is C3-4 alkyl;
- and R3 is unsubstituted or substituted phenyl;
- wherein each substituted phenyl or pyridyl individually is substituted with 1, 2, or 3 substituents, each substituent is independently C1-6 alkyl, halo, —OH, —COOH, cyano, nitro, amino, C1-6 monoalkylamine, C1-6 dialkylamine, C1-6 haloalkyl, or C1-6 haloalkoxy;
- or
- a pharmaceutically acceptable salt, a stereoisomeric form thereof, or a combination thereof.
16 more elements
Dependencies are inferred from the claim text.