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US 2026/0217667 A1Published application
Amyloid targeting agents
AssigneeAmydis, Inc.
InventorsStella Sarraf, Gerald Swiss
Life of this patent
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Abstract
Provided herein is the design and synthesis of novel molecular rotor fluorophores useful for detection of amyloid or amyloid like proteins. The fluorophores are designed to exhibit enhanced fluorescence emission upon associating with amyloid or amyloid like proteins as compared to unbound compound. Also disclosed herein are the methods for treating of diseases associated with an amyloid or amyloid like proteins.
Claims36
A compound of formula:
- or a pharmaceutically acceptable salt, tautomer or a prodrug thereof wherein:
- W1 is O, N(R14), or C(R4)2;
- R14 is hydrogen, alkyl, halomethyl having 1 to 3 halo groups, —COOH, —CONH2, substituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl;
- R1 is selected from hydrogen, halo, haloalkyl having 1 to 3 halo groups, or cyano;
- R2, R3, R4, R5, and R6 are each independently hydrogen, halo, haloalkyl having 1 to 3 halo groups, —CN, —C(O)R1A, —C(O)OR1A, —C(O)NR1AR1B, —OR1A, —NHC(O)NR1AR1B, —NR1AR1B, —NHNR1AR1B, —NR1AC(O)R1B, —NR1AC(O)OR1B, —NR1AOR1B, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl;
- R1A and R1B are each independently hydrogen, halo, haloalkyl having 1 to 3 halo groups, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl;
- Z is —C(O)— or —SO2—;
- and
- Y is CH2, NH, or S;
- and
- WSG is a water soluble group;
- with the proviso that:
- when Z is —C(O)—, then Y is not NH,
- when Y is CH2, W1 is O, N(CH3), or CH2 for formula I, then R2 is not hydrogen or C1-10 alkyl, and
- when Y is CH2, W1 is O, N(CH3), or CH2, and R3, R5, R6 are hydrogen for formula II, then R2 is not hydrogen or C1-10 alkyl.
12 more elements
A compound selected from the group consisting of:
- or a pharmaceutically acceptable salt, tautomer or prodrug thereof.
Dependencies are inferred from the claim text.