Substituted 4-(indol-3-Yl)quinazolines and Their Use

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

The patent discloses new substituted 4-(indol-3-yl)quinazolines and their salts, which act as inhibitors of proteinase and, specifically, tyrosine kinase activities such as the EGF receptor-specific tyrosine protein kinase. These compounds are proposed for the treatment of tumors, osteoporosis, and proliferative epidermal diseases (like psoriasis) in humans. Additionally, the patent covers their use in crop protection as potential fungicides, herbicides, or insecticides, and details methods for synthesizing these compounds. The compounds also exhibit strong fluorescence, making them useful for diagnostic applications in characterizing ATP-binding sites of the EGFR tyrosine kinase.

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

• Development of anti-cancer drugs, especially targeting tumors that overexpress EGFR or HER2 receptors.
• Treatment of bone diseases like osteoporosis by modulating tyrosine kinase-mediated pathways.
• Therapy for proliferative epidermal disorders such as psoriasis.
• Diagnostic reagents for identifying and characterizing ATP-binding sites in cell receptor kinases via their fluorescence.
• Development of advanced agrochemicals for crop protection, including new fungicides, insecticides, and herbicides.

BenefitsContent extracted from patent full text and abstract with AI.

• Targeted inhibition of protein kinases (e.g., EGFR, HER2), potentially leading to more effective and specific cancer therapies with fewer side effects compared to traditional chemotherapy.
• Potential for treating a spectrum of diseases linked to abnormal kinase activity, including cancer, osteoporosis, and skin diseases.
• Dual utility in both human pharmaceuticals and agricultural chemicals, enhancing the versatility of the compounds.
• Strong fluorescence properties enable their use in diagnostics, improving detection and characterization of important biological targets.
• Detailed methods for efficient chemical synthesis allow for easier production and modification of the compounds for diverse applications.

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Inventors & Applicants

Patent Abstract

The invention relates to the use of substituted 4-(indol-3-yl)quinazolines or one of their salts for inhibiting proteinase activity, in particular the EGF receptor-specific tyrosine protein kinase, for treating tumours, osteoporosis or proliferative epidermal diseases, in addition to novel substituted 4-(indol-3-yl)quinazolines or one of their salts and to a method for producing said substances. The invention also relates to the use of substituted 4-(indol-3- yl)quinazoline derivatives or one of their salts for inhibiting protein kinase activity, in particular for crop protection in the development of fungicidal, herbicidal or insecticidal active ingredients.