Use of Indole-3-carboxylic Acid Esters for Inhibition of Microsomal Prostaglandin E2 Synthase

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

This patent describes the use of indole-3-carboxylic esters and their derivatives as novel inhibitors of two key enzymes involved in inflammatory and certain neoplastic processes: microsomal prostaglandin E2 synthase-1 (mPGES-1) and 5-lipoxygenase (5-LO). By targeting these enzymes, the compounds selectively block the biosynthesis of prostaglandin E2 (PGE2) and leukotriene products, both of which play major roles in inflammation, pain, fever, and some diseases such as cancer. These inhibitors provide a dual-action approach to treat conditions driven by PGE2 and 5-LO without the broad side effects associated with traditional COX inhibitors.

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

• Pharmaceutical drugs for the treatment of chronic inflammatory diseases such as rheumatoid arthritis and osteoarthritis.
• Therapeutics for cardiovascular diseases where inflammation plays a role, e.g., atherosclerosis, angina, strokes.
• Medications for respiratory inflammatory conditions such as asthma and allergic rhinitis.
• Treatments for autoimmune diseases such as multiple sclerosis.
• Drugs for inflammatory skin conditions like psoriasis and dermatitis.
• Cancer therapeutics targeting inflammation-driven tumor growth.
• Analgesics and antipyretics for pain and fever management where PGE2 and leukotrienes are involved.

BenefitsContent extracted from patent full text and abstract with AI.

• Selectively inhibits pathogenic PGE2 synthesis without disrupting the synthesis of beneficial prostaglandins, potentially resulting in fewer gastrointestinal and renal side effects than traditional NSAIDs.
• Dual inhibition of both mPGES-1 and 5-LO may provide superior efficacy in diseases where both pathways contribute to pathology, possibly achieving additive or synergistic therapeutic effects.
• May reduce or replace the need for steroidal anti-inflammatory drugs and COX inhibitors, thus minimizing associated side effects.
• Potential for use in a wide array of inflammatory and proliferative diseases, increasing therapeutic versatility.
• Oral and parenteral formulations are possible, allowing flexible administration routes.
• Targeted approach could improve patient outcomes in chronic and difficult-to-treat inflammatory and cancer conditions.

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Inventors & Applicants

Patent Abstract

The present invention relates to the use of indole-3-carboxylic esters and derivatives thereof for inhibiting inducible microsomal prostaglandin E2 synthase-1 and/or for inhibiting 5-lipoxygenase. More particularly, the invention relates to the use of derivatives of 3-carboxyaryl[g]indole, in particular of 2-aryl- and 2-arylalkyl­aryl[g]indole-3-carboxylic esters and structural derivatives thereof for inhibiting inducible microsomal prostaglandin E2 synthase-1 and/or for inhibiting 5-lipoxygenase. The invention further relates to the use of indole-3-carboxylic esters for producing a medicament for treatment of PGE2- and/or 5-LO-mediated disorders and pathological states, especially of inflammatory chronic inflammations such as rheumatoid arthritis, osteoarthritis, disorders of the cardiovascular system, asthma, allergic rhinitis, multiple sclerosis, inflammatory skin disorders, osteoporosis and cancer, pain and fever, in which PGE2 and/or 5-LO products are involved.