Compounds, compositions, and methods of use to inhibit protein aggregation
AssigneePurdue Research Foundation
InventorJessica Sonia FORTIN
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Abstract
The disclosure relates to, among other things, benzisothiazoles, benzisoxazoles, and indazoles; a pharmaceutical composition comprising such compounds; and a method of inhibiting protein aggregation in a subject having, or at risk for, aggregation of a protein prone to aggregate in a state of disease, which method comprises administering to the subject the composition in an amount effective to inhibit protein aggregation.
Claims26
A compound comprising a benzisothiazole linked to an amide, a formamide, an amine, or a urea, or a pharmaceutically acceptable salt thereof, wherein at least one carbon on the benzyl ring of the benzisothiazole is substituted with a substituent selected from the group consisting of a C1-C6 alkyl, —NO2, and a halo.
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A compound of the formula:
- or a pharmaceutically acceptable salt thereof;
- wherein:
- X is O, NR3, or S, wherein R3 is H or alkyl;
- R4 is an electron withdrawing group, and
- each R5 and R6 is independently selected from hydrogen, alkyl, cycloalkyl, aryl, heteroaryl, —SO2R, —C(O)NHR, and —C(NR7)NHR, wherein R5 and R6 can each be independently optionally substituted with an alkyl, a nitro, a cyano, a halo, an amino, a hydroxy, an alkoxy, an aryl, or a heteroaryl, and R is an alkyl, an alkenyl, an alkynyl, a cycloalkyl, a heterocycloalkyl, an aryl, or a heteroaryl, and wherein R can be optionally substituted with a halo, an amino, a nitro, a cyano, a hydroxy, an alkoxy, an aryl, or a heteroaryl group.
A compound of the formula:
- or a pharmaceutically acceptable salt thereof;
- wherein:
- X is O, NR3, or S, wherein R3 is H or alkyl;
- R4 is an electron withdrawing group;
- and
- each R7 and R8 is independently selected from H, —C(O)NHR, alkylaminoalkyl, aminoalkyl, arylamino, heteroarylamino, alkyl substituted with at least one group comprising a hydrogen atom capable of hydrogen bonding with at least one hydrogen bonding acceptor, aryl substituted with at least one group comprising a hydrogen atom capable of hydrogen bonding with a hydrogen bonding acceptor, heteroaryl substituted with at least one group comprising a hydrogen atom capable of hydrogen bonding with a hydrogen bonding acceptor, and heteroaryl comprising at least one hydrogen atom capable of hydrogen bonding with a hydrogen bonding acceptor, each of which can independently optionally be substituted with an alkyl, a nitro, a cyano, a halo, an amino, a hydroxy, an alkoxy, an aryl, or a heteroaryl, and R is an alkyl, an alkenyl, an alkynyl, a cycloalkyl, a heterocycloalkyl, an aryl, or a heteroaryl and wherein R can be optionally substituted with a halo, an amino, a nitro, a cyano, a hydroxy, an alkoxy, an aryl, or a heteroaryl group.
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Dependencies are inferred from the claim text.