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US 11,718,596 B2Granted
Amyloid targeting agents and methods of using the same
AssigneesThe Regents of the University of California, Amydis, Inc.
InventorsJerry Yang, Emmanuel A. Theodorakis, Stella Sarraf
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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 methods for treating diseases associated with amyloid or amyloid like proteins.
Claims20
A compound of Formula (Ie):
- wherein
- EDG is heterocycloalkyl of no more than 10 carbons optionally substituted with one or more R17;
- each R17 is independently halogen, —OR18, —NR19R20, C1-C10 alkyl, or C1-C10 heteroalkyl;
- each of R18, R19 and R20 is independently hydrogen, C1-C10 alkyl, C1-C10 heteroalkyl, or cycloalkyl of no more than 10 carbon atoms, each of which except for hydrogen is optionally substituted with one or more R21;
- each R21 is independently halogen, —OR22, —NR23R24, C1-C10 alkyl, C1-C10 heteroalkyl, cycloalkyl of no more than 10 carbon atoms, heterocycloalkyl of no more than 10 carbon atoms, aryl of no more than 10 carbon atoms, or heteroaryl of no more than 10 carbon atoms;
- each of R22, R23 and R24 is independently hydrogen or C1-C10 alkyl;
- Ar is naphthylene optionally substituted with one or more R1;
- each R1 is independently halogen, —OR2, —NR3R4, C1-C10 alkyl, or C1-C10 heteroalkyl, each of R2, R3 and R4 is independently hydrogen, C1-C10 alkyl, or C1-C10 heteroalkyl;
- R84 is hydrogen or optionally substituted C1-C10 alkyl;
- EWG is —CN;
- and
- WSG is:
- wherein n is an integer from 2-50, and R81 is hydrogen or C1-C10 alkyl.
10 more elements
Dependencies are inferred from the claim text.