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US 10,590,157 B2Granted
C-terminal HSP90 inhibitors
AssigneeUniversity of Kansas
InventorsBrian S. J. Blagg, Bhaskar Reddy Kusuma, Teather Sundstrom
Life of this patent
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Abstract
Hsp90 C-terminal inhibitors and pharmaceutical compositions containing such compounds are provided. The compounds of the disclosure are useful for the treatment and/or prevention of neurodegenerative disorders such as diabetic peripheral neuropathy.
Claims20
A method for treating or preventing a neurodegenerative disorder in a subject in need thereof comprising administering to the subject a therapeutically effective amount of a compound of the formula:
- wherein
- R1 is hydrogen, halo, hydroxy, trifluoroalkyl, alkoxy, or sulfanyl;
- R2 is hydrogen, halo, hydroxy, trifluoroalkyl, alkoxy, sulfanyl, or alkyl;
- R3 is hydrogen, halo, hydroxy, trifluoroalkyl, alkoxy, sulfanyl, alkyl;
- X is ═CR21—, or ═N—, wherein R21 is hydrogen, halo, or trifluoromethyl;
- and
- Y is ═CR3— or ═N—.
4 more elements
A compound of the formula:
- wherein:
- R1 is hydrogen, hydroxy, halo, trifluoroalkyl, alkyl, alkenyl, alkynyl, carbocyclic, heterocyclic, aryl, aralkyl, carboxyl, amido, amino, alkoxy, sulfanyl, sulfenyl, sulfonyl, or ether;
- R2 is hydrogen, halo, hydroxy, trifluoromethyl, alkoxy, alkyl, alkenyl, alkynyl, carbocyclic, alkylcarbocyclic, alkylheterocyclic, heterocyclic, or
- —R9—OR10, wherein:
- R9 is a covalent bond or alkylene, and
- R10 is hydrogen, alkyl, C-amido, or acyl;
- or
- R2 together with R3 and the atoms to which they are attached form a carbocyclic ring with 5 to 7 ring members or a heterocyclic ring having 4 to 8 ring members with at least one heteroatom selected from oxygen or nitrogen;
- R3 is hydrogen, hydroxy, halo, trifluoroalkyl, alkyl, alkoxy, sulfanyl, or
- R11—O—R12, wherein:
- R11 is a covalent bond or alkylene, and
- R12 is alkyl, C-amido, or acyl;
- or
- R3 together with R2 and the atoms to which they are attached form a carbocyclic ring with 5 to 7 ring members or a heterocyclic ring having 4 to 8 ring members with at least one heteroatom selected from oxygen or nitrogen;
- or
- R3 is absent when Y is ═N—;
- R′ is H or alkyl;
- R″ is alkyl, alkoxy, haloalkyl, alkylcycloalkyl, or alkylamidoalkyl;
- X is ═CR21— or ═N—, wherein:
- R21 is hydrogen, halo, trifluoromethyl, alkyl, alkenyl, alkynyl, alkoxy, or hydroxy;
- and
- Y is ═CR3— or ═N—;
- or a pharmaceutically acceptable salt thereof.
20 more elements
Dependencies are inferred from the claim text.