Compounds and methods for treating cancer, viral infections, and allergic conditions
AssigneeWashington University
InventorsJames W. Janetka, Vishnu Damalanka
Life of this patent
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Abstract
The present invention generally relates to compounds that are useful for inhibiting one or more trypsin-like S1 serine proteases, HGFA, matriptase, hepsin, KLK5 and/or TMPRSS2 as well as cysteine proteases including trypsin-like cysteine proteases (e.g. Cathepsin B). The present invention also relates to various methods of using the inhibitor compounds to treat or prevent viral infections, including those caused by coronaviruses and influenza, conditions associated with KLK5, various malignancies, pre-malignant conditions, and cancer.
Claims10
A compound of Formula (IIA), (IIB), (IIC), (IID), (IIE), (IIF), (IIG), or (IIH) a salt thereof, or a stereoisomer thereof:
- wherein:
- each n is independently 1 or 2;
- each P3 is independently hydrogen or a side chain of a natural or unnatural amino acid;
- each X is independently hydrogen or methyl;
- each Y is independently hydrogen, acetyl, tert-butyloxycarbonyl (Boc), benzyloxycarbonyl (Cbz), fluorenylmethyloxycarbonyl (Fmoc), benzyl, —C(O)R, —SOOR, —COOR, —C(O)NHR, substituted or unsubstituted —(CH2)xaryl, substituted or unsubstituted —(CH2)xheteroaryl, substituted or unsubstituted —(CH2)xcycloalkyl, or substituted or unsubstituted —(CH2)xheterocycle;
- each x is independently 0, 1, or 2;
- each R is independently C1 to C6 alkyl, C3 to C6 cycloalkyl, substituted or unsubstituted heterocycle, substituted or unsubstituted alkylheterocycle, aralkyl, or aryl;
- and
- each Z is independently
- R1 is hydrogen,
- R2 and R3 are each independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted aralkyl, substituted or unsubstituted heteroaryl, or substituted or unsubstituted heteroarylalkyl;
- R4 is hydrogen, substituted or unsubstituted alkyl, or a residue of an amino acid, or R3 and R4 can form a ring;
- each R5 is independently hydrogen, substituted or unsubstituted alkyl, or R5 moieties can form a ring;
- and
- each R6 is substituted or unsubstituted aryl.
A compound selected from the group consisting of:
Dependencies are inferred from the claim text.