Alpha-substituted hydrazides having calpain inhibitory activity

Details Alpha-substituted hydrazides having calpain inhibitory activity Alpha-substituted hydrazides having calpain inhibitory activity

C - Chemistry, Metallurgy

07

D

C07D 241/44 (2006.01) A61K 31/495 (2006.01) C07D 401/00 (2006.01) C07D 403/00 (2006.01)

Patent

CA 2208073

The invention covers a novel series of .alpha.-substituted hydrazides that inhibit both calpain I and calpain II. They are non-peptide irreversible active site inhibitors of calpain. The compounds are useful in the treatment of neurodegenerative disorders including cerebrovascular disorders, brain injury, spinal cord, and peripheral nerve injury, cardiac infarction, cataracts, inflammation, restenosis, muscular dystrophy, and platelet aggregation. Pharmaceutical compositions, methods of using processes for preparing and novel intermediates useful in the processes are also disclosed.

L'invention concerne une nouvelle série d'hydrazides alpha-substitués qui inhibent à la fois la calpaïne I et la calpaïne II. Il s'agit d'inhibiteurs non peptidiques irréversibles du site actif de la calpaïne. Ces composés sont utiles dans le traitement des maladies neurodégénératives, dont les affections cérébro-vasculaires, les lésions cérébrales, les lésions de la moelle épinière et des nerfs périphériques, l'infarctus cardiaque, les cataractes, l'inflammation, la resténose, la dystrophie musculaire et l'agrégation plaquettaire. On divulgue également des compositions pharmaceutiques, des méthodes pour utiliser les procédés de préparation et de nouveaux intermédiaires utiles dans les procédés.

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