Phenyl diamides and a pharmaceutical preparation comprising phenyl diamides

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

The invention relates to a new class of chemical compounds known as phenyl diamides, and their use as active ingredients in pharmaceutical preparations. These compounds inhibit proteins called cytohesins, which are involved in cancer cell signaling through the epidermal growth factor receptor (EGFR) and its variant EGFRvIII. The phenyl diamides demonstrate strong inhibitory effects on the proliferation of glioblastoma cells – a highly aggressive form of primary brain cancer. The patent discloses specific phenyl diamides effective against gliomas and potentially other cancers, as well as claims around their formulation and use in medicinal products.

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

• Development of new targeted drugs for treating glioblastoma, a type of aggressive brain tumor.
• Therapeutic intervention against other EGFR- or cytohesin-driven cancers, such as lung, colorectal, pancreatic, prostate, kidney, or breast cancer.
• Treatment of cancers that are resistant to classical chemotherapy and radiotherapy, particularly those with the EGFRvIII mutation.
• Use in personalized or precision medicine, where patients with specific tumor types or genetic profiles (e.g., EGFRvIII-positive tumors) may benefit.
• Drug development programs focusing on orally or intravenously administered anti-cancer pharmaceuticals.

BenefitsContent extracted from patent full text and abstract with AI.

• Offers a novel treatment option for glioblastoma, a cancer with poor prognosis and limited current therapies.
• Selectivity for mutated forms of EGFR (like EGFRvIII), potentially resulting in targeted action and reduced side effects on healthy tissues.
• Demonstrates strong inhibition of cancer cell proliferation at low concentrations (low IC50 values), indicating high potency.
• Low toxicity in preclinical models, suggesting suitability for long-term therapeutic use.
• Potential for broad cancer application beyond gliomas due to mechanism targeting common cancer-signaling pathways.
• Versatility in formulation—can be delivered orally or intravenously for ease of use in clinical settings.

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Inventors & Applicants

Patent Abstract

The present invention relates to phenyl diamides according to the general formula (1) and their use as a medicament and a pharmaceutical preparation comprising as an active ingredient a phenyl diamide according to the general formula (1). Further, the present invention relates to phenyl diamides according to the formulas (16), (17) and (18) for use in the treatment of gliomas.