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US 2020/0048198 A1Published application
Modified histone deacetylase inhibitors and uses thereof
AssigneesThe Regents of the University of California, Vybyl Holdings, Inc.
InventorsNathan C Gianneschi, Paul A. Bertin
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Abstract
The present disclosure generally provides compounds useful for treating cancer. In some aspects, the disclosure provides small-molecule histone deacetylase inhibitors (HDIs) that are chemically modified to have one or more moieties that include hydrophobic portions. In some aspects, the disclosure provides compositions that include such modified HDIs and a protein, such as albumin or albumin mimetics. Further, the disclosure provides various uses of these compounds and compositions.
Claims42
A compound of formula (I)
- A1-X1—X2-A2 (I)
- wherein:
- A1 is an organic group;
- or A1 is a hydrophilic group or a hydrogen atom;
- A2 is a histone deacetylase inhibiting moiety;
- X1 is a hydrophobic group;
- and
- X2 is a direct bond, an organic group, —O—, —S—, —S(═O)—, —S(═O)2—, —S—S—, —N═, ═N—, —N(H)—, —N═N—N(H)—, —N(H)—N═N—, —N(OH)—, or —N(═O)—.
5 more elements
A pharmaceutical composition comprising:
- a compound, which comprises a histone deacetylase inhibiting moiety and a protein binding moiety;
- a protein, wherein the protein is human serum albumin or a protein whose sequence is at least 50% equivalent to that of human serum albumin;
- and
- a carrier, which comprises water;
- wherein the compound and the protein are non-covalently associated with each other with a binding constant (Kb) of at least 102 M−1, or at least 103 M−1, or at least 104 M−1, or at least 105 M−1;
- and
- wherein the compound and the protein are solvated by the carrier.
4 more elements
Dependencies are inferred from the claim text.