Substituted 4-(Indol-3-yl)quinazolines and Their Use and Preparation

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

This patent discloses a new class of substituted 4-(indol-3-yl)quinazoline compounds and their salts, which are potent inhibitors of specific protein kinases, particularly the EGFR and HER-2 receptor tyrosine kinases. These compounds can be used in pharmaceutical compositions for treating diseases associated with abnormal kinase activity, like cancers, osteoporosis, and certain skin disorders. Additionally, these compounds can be applied in plant protection as components of agrochemicals, such as fungicides, herbicides, or insecticides. The patent also describes methods for synthesizing these novel compounds.

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

• Development of targeted anti-cancer drugs, particularly for tumors overexpressing EGFR or HER-2 (e.g., certain lung and breast cancers).
• Pharmaceutical treatment for osteoporosis and proliferative skin diseases like psoriasis.
• Diagnostic tools for identifying ATP binding sites in EGFR due to the compounds' fluorescence properties.
• Formulation of new plant protection products, including fungicides, herbicides, and insecticides, for agriculture.
• Research tools for studying protein kinase activity in biochemical and cellular assays.

BenefitsContent extracted from patent full text and abstract with AI.

• Improved specificity and potency for inhibiting EGFR and HER-2 tyrosine kinases, which may lead to better cancer therapies with fewer side effects than conventional chemotherapy.
• Potential to treat a wider range of diseases linked to kinase activity, including both oncology and non-oncology indications.
• Compounds with unique fluorescent properties that can facilitate diagnostics and research applications.
• Versatile utility in both medical and agricultural sectors, enhancing crop protection and human health.
• Novel synthetic methods provide routes to obtain these compounds efficiently and with potentially higher yields.

Technical Classifications (CPCs)

Inventors & Applicants

Patent Abstract

The present invention relates to the use of substituted 4-(indol-3- yl)quinazolines or a salt thereof for inhibiting protein kinase activity, in particular of EGFR and HER-2 receptor-specific protein tyrosinkinases, for treatment of tumor illnesses, osteoporosis or proliferative epidermis illnesses, and novel substituted 4-(indol-3-yl)quinazolines or a salt thereof and a method for the production thereof. The invention further relates to the use of substituted 4-(indol-3- yl)quinazoline derivatives or a salt thereof for inhibiting protein kinase activity, in particular in plant protection for the development of fungicidal, herbicidal and insecticidal active ingredients, and relates to novel substituted 4-(indol-3-yl)quinazolines or a salt thereof.