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Sulfonamides: a patent review (2008 - 2012)
Fabrizio Carta1, Andrea Scozzafava, Claudiu T Supuran
1Università degli Studi di Firenze, Laboratorio di Chimica Bioinorganica, Rm. 188, Via della Lastruccia 3, I-50019 Sesto Fiorentino (Florence), Italy.
Expert Opinion on Therapeutic Patents
|June 16, 2012
Summary
Sulfonamides are versatile drug components, with recent research focusing on antiglaucoma and anticancer applications. This review covers sulfonamide-based carbonic anhydrase inhibitors and tyrosine kinase inhibitors patented between 2008-2012.
Area of Science:
- Medicinal Chemistry
- Drug Discovery
- Organic Chemistry
Background:
- The sulfonamide functional group is a key component in numerous established pharmaceuticals, including diuretics, carbonic anhydrase inhibitors (CAIs), antiepileptics, and COX2 inhibitors.
- Recent drug development has introduced novel sulfonamide-containing agents like apricoxib and pazopanib, highlighting the continued relevance of this chemical scaffold.
Purpose of the Study:
- To review the scientific and patent literature on sulfonamides investigated between 2008 and 2012.
- To focus on carbonic anhydrase inhibitors (CAIs), COX2 inhibitors, and pazopanib (a multi-targeted receptor tyrosine kinase inhibitor).
Main Methods:
- Literature review of scientific publications and patents.
- Analysis of research trends in sulfonamide drug development within the specified timeframe.
- Identification of key drug classes and their therapeutic targets.
Main Results:
- Patents predominantly feature sulfonamide CAIs with NO-donating moieties for antiglaucoma applications and compounds targeting tumor-associated carbonic anhydrase isoforms (CA IX/XII).
- Antidandruff properties of sulfonamides inhibiting yeast CAs were also patented.
- Significant antitumor activity was reported for apricoxib (COX2 inhibitor) and pazopanib (tyrosine kinase inhibitor), with related patents.
Conclusions:
- There is an ongoing demand for novel sulfonamides as selective antiglaucoma agents (targeting CA II) and antitumor therapeutics/diagnostic tools (targeting CA IX/XII).
- The sulfonamide motif is recognized for its potential in developing drugs for various diseases.
- This privileged structure is expected to feature in future pharmaceutical innovations.
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