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US 2022/0008563 A1Published application
Radiolabelled and nonradiolabelled pegylated compounds and uses thereof
AssigneeThe Regents of the University of California
InventorsJogeshwar Mukherjee, Christopher Liang, Phuc Quang Lam, Rommani Mondal, Stephanie Martinez
Life of this patent
Estimating the term…
Abstract
The disclosure provides compounds for detecting neurodegeneration and/or identifying and monitoring the progression of inflammation in neurodegenerative diseases. The disclosure further provides compounds that inhibit the activity of monoamine oxidases, and uses thereof.
Claims20
A compound having the structure of Formula (I) or Formula (II):
- or a pharmaceutically acceptable salt, solvate, polymorph, or prodrug thereof, wherein,
- R1-R4 are each individually selected from H, —OR9, a halogen, a radiohalogen, a hydroxyl, an amino, an alkoxy, an azide, a ketone, a carboxyl, a carboxylate, an aldehyde, a boronic acid, a boronic ester, a haloformyl, an imide, a nitrile, an isonitrile, a nitro, a thiol, a sulfinyl, a sulfo, an optionally substituted (C1-C6)alkyl, an optionally substituted (C1-C6)alkenyl, an optionally substituted (C1-C6)alkynyl, an optionally substituted (C1-C6)hetero-alkyl, an optionally substituted (C1-C6) hetero-alkenyl, an optionally substituted (C1-C6)hetero-alkynyl, an optionally substituted (C4-C12)cycloalkyl, an aryl, and a heterocycle group, wherein at least one of R1-R4 is —OR9;
- R5-R8 are each individually selected from H, —OR9, a halogen, a radiohalogen, a hydroxyl, an alkoxy, an azide, a ketone, a carboxyl, a carboxylate, an aldehyde, a boronic acid, a boronic ester, a haloformyl, an imide, a nitrile, an isonitrile, a nitro, a thiol, a sulfinyl, a sulfo, an optionally substituted (C1-C6)alkyl, an optionally substituted (C1-C6)alkenyl, an optionally substituted (C1-C6)alkynyl, an optionally substituted (C1-C6)hetero-alkyl, an optionally substituted (C1-C6) hetero-alkenyl, an optionally substituted (C1-C6)hetero-alkynyl, an optionally substituted (C4-C12)cycloalkyl, an aryl, and a heterocycle group, wherein at least one of R5-R8 is —OR9 or a radiohalogen;
- R9 is an ether or polyether having the structure of
- X is a halogen, a radiohalogen, or a hydroxyl;
- and
- y is an integer selected from 1, 2, 3, 4, 5, 6, 7, 8, 9 and 10.
4 more elements
A compound having the structure of Formula (III):
- or a pharmaceutically acceptable salt, solvate, polymorph, or prodrug thereof, wherein,
- A1 is selected from N, or CR16;
- R10 and R11 are individually selected from H or a (C1-C6)alkyl;
- R12-R16 are each individually selected from H, —OR17, a halogen, a radiohalogen, a hydroxyl, an amino, an alkoxy, an azide, a ketone, a carboxyl, a carboxylate, an aldehyde, a boronic acid, a boronic ester, a haloformyl, an imide, a nitrile, an isonitrile, a nitro, a thiol, a sulfinyl, a sulfo, an optionally substituted (C1-C6)alkyl, an optionally substituted (C1-C6)alkenyl, an optionally substituted (C1-C6)alkynyl, an optionally substituted (C1-C6)hetero-alkyl, an optionally substituted (C1-C6) hetero-alkenyl, an optionally substituted (C1-C6)hetero-alkynyl, an optionally substituted (C4-C12)cycloalkyl, an aryl, and a heterocycle group, wherein at least one of R1-R4 is —OR17;
- R17 is an ether or polyether having the structure of
- X is a halogen, a radiohalogen or a hydroxyl;
- and
- y is an integer selected from 1, 2, 3, 4, 5, 6, 7, 8, 9 and 10.
5 more elements
Dependencies are inferred from the claim text.