Yissum - Research Development Company of the Hebrew University

New CNS-Active Carbamate Derivatives for Epilepsy

Posted by Yissum - Research Development Company of the Hebrew UniversityResponsive · Innovative Products and Technologies · Israel

Summary of the technology

New CNS-active carbamate derivatives of branched aliphatic carboxylic acids with 4-aminobenzensulfonamide with a broad potent antiepileptic activity
Project ID : 6-2017-4419

Yissum - Research Development Company of the Hebrew University

Description of the technology

Keywords

Antiepileptic drugs, 4-Aminobenzensulfonamides. Teratogenicity. Carbonic Anhydrase Inhibition

Current development stage

TRL4 - POC & Safety of candidate drug formulation is demonstrated in defined animal model

Application

Epilepsy therapy is based on the use of antiepileptic drugs (AEDs). However, approximately 30% of patients with epilepsy are not seizure-free with the existing medications.

Furthermore, the clinical use of the existing AEDs is restricted by their side-effects, including the teratogenicity associated with valproic acid that restricts its use in women of child-bearing age.

Therefore, there is an unmet clinical need to develop new, effective AEDs.

Our Innovation

  • Novel CNS-active carbamate derivatives of branched aliphatic carboxylic acids with 4-aminobenzensulfonamide with a broad potent antiepileptic activity
  • Better anticonvulsant activity
  • Better protective index than valproic acid (VPA)
  • Potent inhibitors of Carbonic anhydrase (CA) isoforms I, II and VII

Technology

The researchers conducted comparative analysys of the anticonvulsant activity, neurotoxicity, teratogenicity and carbonic anhydrase (CA) inhibition of 10 new carbamate derivatives of 4-aminobenzenesulfonamide possessing 6–9 carbons in the aliphatic side chain of the carbamate moieties

The teratogenicity of the most potent anticonvulsant compounds was evaluated in mice and their CA inhibition of four human-CA isoforms was tested in vitro compared to that of acetazolamide.

Three of the ten newly synthesized carbamates showed anticonvulsant activity in the maximal-electroshock (MES) and 6 Hz tests in rodents. They induced neural tube defects only at doses markedly exceeding their anticonvulsant ED50 values.

Fig. 1: Structures of the synthesized and tested sulfonebenzene carbamates

Opportunity

  • New potent and safe antiepileptic drugs
  • New CNS (Central Nervous System) drugs

Project manager

Mel Larrosa
VP Business Development Healthcare

Project researchers

Meir Bialer
HUJI, School of Medicine - IMRIC
School of Pharmacy- Institute for Drug Research

Hafiz Mawasi
HUJI, School of Medicine - IMRIC

David BIBI
,

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About Yissum - Research Development Company of the Hebrew University

Technology Transfer Office from Israel

Yissum Research Development Company of the Hebrew University of Jerusalem Ltd. Founded in 1964 to protect and commercialize the Hebrew University’s intellectual property. Ranked among the top technology transfer companies, Yissum has registered over 8,900 patents covering 2,500 inventions; has licensed out 800 technologies and has spun-off 90 companies. Products that are based on Hebrew University technologies and were commercialized by Yissum generate today over $2 Billion in annual sales.

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