Phosphoinositide 3-kinase inhibitor with a zinc binding moiety
Inventors
Cai, Xiong • Zhai, Haixiao • Lai, Chengjung • Qian, Changgeng • Bao, Rudi
Assignees
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Publication Number
US-11654136-B2
Publication Date
2023-05-23
Expiration Date
Abstract
The invention provides a compound of Formula I, Pharmaceutical compositions comprising such compounds and the use of such compounds in the treatment of phosphoinositide 3-kinase related diseases and disorders such as cancer. The instant application further relates to the treatment of histone deacetylase related disorders and diseases related to both histone deacetylase and phosphoinositide 3-kinase.
Core Innovation
The disclosed invention centers on a compound referred to as “Compound 1” (Formula I), defined by a specific chemical structure. The concept links the compound to a zinc binding moiety that enables an integrated target profile through interaction with zinc ions, supporting both PI3K inhibition and HDAC inhibition within a single compound concept.
The problem being addressed is the need for therapeutic agents that can inhibit PI3K and inhibit HDAC for diseases associated with those targets. The document characterizes PI3K and HDAC as relevant to cancer and also describes immune/lymphocyte-modulating contexts in connection with the therapeutic use.
Compound 1 is used as part of therapeutic regimens for PI3K- and HDAC-related diseases, including cancer. The document also describes the compound in salt and formulation contexts, including pharmaceutically acceptable salts, and relates the integrated PI3K/HDAC inhibitory activity to pharmacodynamic effects such as tumor growth inhibition and downstream pathway-related changes.
Claims Coverage
The provided claim set includes independent claims focused on specific salt forms of a compound represented by Formula I. The inventive feature is the selection of selected pharmaceutically acceptable salt forms, and the provided claim text also places the salt into pharmaceutical compositions and dosage forms.
Salt forms of a formula-defined compound
A salt of a compound represented by the formula, wherein the salt is a sodium salt, a potassium salt, a choline salt, or a sulfate salt.
Salt in pharmaceutical composition with pharmaceutically acceptable carrier
A pharmaceutical composition including the salt together with a pharmaceutically acceptable carrier.
Oral-adapted pharmaceutical composition
The pharmaceutical composition is adapted for oral administration.
Tablet or capsule dosage form
The pharmaceutical composition is formulated as a tablet or a capsule.
The claim coverage is centered on selected pharmaceutically acceptable salt forms of the compound represented by Formula I, specifically sodium, potassium, choline, or sulfate. The provided claim text further extends to pharmaceutical compositions with a pharmaceutically acceptable carrier, including oral administration and tablet or capsule dosage forms.
Stated Advantages
Potent PI3K/HDAC inhibition.
Oral bioavailability.
Tumor uptake and pharmacodynamic activity in xenograft tumor-bearing mice.
Antitumor efficacy after oral or IV dosing.
Ames-test safety via genotoxicity testing.
Documented Applications
Therapeutic use for PI3K- and HDAC-related diseases, including cancer.
Immune/lymphocyte-modulating uses are described in connection with the therapeutic indications.
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