Inhibitors for Bromodomains

Simple SummaryContent extracted from patent full text and abstract with AI.

The invention discloses novel chemical compounds that act as inhibitors of bromodomains, especially targeting the BET protein family (such as BRD2, BRD3, BRD4, and BRDT). These proteins are involved in gene expression regulation and can influence the development and progression of several diseases, particularly cancers like acute myeloid leukemia (AML) and myeloproliferative neoplasms (MPN). The patented compounds, particularly sulfoximines and related structures, have been shown to effectively inhibit cell proliferation in leukemia cell lines and patient samples, with some enantiomers (specifically, the (S)-enantiomer of MF2) outperforming existing inhibitors.

Use CasesContent extracted from patent full text and abstract with AI.

• Development of new cancer therapies, especially for conditions linked to BET proteins like AML and MPN.
• Creating pharmaceutical compositions for the treatment of cancers, autoimmune diseases, and inflammatory disorders associated with bromodomain dysregulation.
• Improvement or replacement of existing bromodomain inhibitors in clinical or preclinical settings.
• Potential for use in combination therapies for hematologic malignancies, including leukemia and other related bone marrow diseases.
• Targeted inhibition in research applications for better understanding gene regulation in cancer.

BenefitsContent extracted from patent full text and abstract with AI.

• Provides potent and selective inhibition of BET family bromodomains, particularly BRD4, which is crucial in certain cancers.
• Novel chemical structures (sulfoximines, sulfondiimides, and sulfonimidamides) offer improved selectivity and potency compared to earlier inhibitors like PFI-1, especially in their (S)-enantiomer forms.
• Demonstrated superior efficacy in patient-derived leukemia cells and selectivity for malignant cells over healthy controls at certain dosages, potentially reducing side effects.
• Chemical diversity and stereochemistry allow for fine-tuning of pharmacological properties and personalized medicine approaches.
• Enables development of more effective, possibly lower-dose treatments for otherwise hard-to-treat or resistant cancers.

Technical Classifications (CPCs)

Inventors & Applicants

Patent Abstract

The invention relates to compounds according to the general formula (1), to their use for producing a medicament, in particular for the treatment of bromodomain-related diseases, such as cancers.