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US 2022/0087967 A1Published application
Sulfopropanoic acid derivatives for treating neurodegenerative disorders
AssigneeAlzheon, Inc.
InventorsPetr Kocis, John Hey, Martin Tolar
Life of this patent
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Abstract
Provided herein is the use of a compound of Formula (I) or a pharmaceutically acceptable salt thereof, for treating a disease characterized by amyloid and amyloid-like aggregates, e.g., Alzheimer's disease.
Claims22
A method of treating a subject suffering from Alzheimer's disease, comprising the step of administering to the subject an effective amount of a compound of Formula I:
- or a pharmaceutically acceptable salt thereof, wherein:
- R1 is selected from —O—R3, —O—R4—CH(NHR6)—C(O)—R5, and —[N(R6)—CH(R7)—C(O)]1-2—R5;
- R2 is selected from hydrogen, R3, and R4—CH(NHR6)—C(O)—O—R5;
- each R3 is independently selected from C1-C20 alkyl, —C2-C20 alkenyl, —C2-C20 alkynyl, —(C0-C20 alkylene)-aryl, —(C0-C20 alkylene)-carbocyclyl, —(C0-C20 alkylene)-heterocyclyl, —(C0-C20 alkylene)-heteroaryl, —(C2-C20 alkenylene)-aryl, —(C2-C20 alkenylene)-carbocyclyl, —(C2-C20 alkenylene)-heterocyclyl, —(C2-C20 alkenylene)-heteroaryl, —(C2-C20 alkynylene)-aryl, —(C2-C20 alkynylene)-carbocyclyl, —(C2-C20 alkynylene)-heterocyclyl, and —(C2-C20 alkynylene)-heteroaryl;
- each R4 is an independently selected derivatized side chain of a natural or unnatural α-amino acid wherein the side chain has been derivatized through a free —OH group present on the side chain prior to derivatization;
- each R5 is independently selected from —OH, —O—C1-C4 alkyl and —NH2;
- each R6 is independently selected from hydrogen and —C(O)R8;
- R7 is a side chain of an α-amino acid;
- and
- each R8 is independently selected from hydrogen, C1-C4 alkyl, —O—C1-C4 alkyl, —(C1-C4 alkylene)-aryl, and (C1-C4 alkoxy)-aryl;
- wherein:
- each alkyl, alkylene, alkenyl, alkenylene, alkynyl or alkynylene portion of R3 is optionally substituted with up to 6 substituents independently selected from halo, —OH, —O—(C1-C4 alkyl), —O—(C1-C4 haloalkyl), carbocyclyl, aryl, heterocyclyl, and heteroaryl;
- each carbocyclyl, aryl, heterocyclyl, or heteroaryl portion of R3 is optionally substituted with up to four substituents independently selected from halo, —OH, —O—(C1-C4 alkyl), —O—(C1-C4 haloalkyl), C1-C18 alkyl, C2-C18 alkenyl, and C2-C18 alkynyl, wherein the alkyl, alkenyl, or alkynyl portions of the C1-C18 alkyl, C2-C18 alkenyl, or C2-C18 alkynyl, respectively, are optionally substituted with up to six substituents independently selected from halo, —OH, —O—(C1-C4 alkyl), and —O—(C1-C4 haloalkyl);
- R1 comprises no more than 2 cyclic moieties;
- and
- R2 comprises no more than 2 cyclic moieties.
13 more elements
Dependencies are inferred from the claim text.