Tetracycline derivatives with reduced antibiotic activity...

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 263/52 (2006.01) A61K 31/65 (2006.01) A61P 25/28 (2006.01) A61P 39/00 (2006.01) C07D 498/10 (2006.01)

Patent

CA 2730377

The present disclosure is directed to compositions and methods which utilize the tetracycline scaffold, preferably the scaffold of minocycline, and which significantly lack antibiotic activity. The compounds have neuroprotective attributes without interfering with the drugs capacity to pass through the blood brain barrier. These compounds have neuroprotective activity because of their inhibition of neuronal cell cycle progression. The compounds are characterized m part by a fifth ring joining positions 9 and 10.

La présente invention concerne des compositions et des procédés qui utilisent le squelette de tétracycline, de préférence le squelette de minocycline, et qui manquent significativement dactivité antibiotique. Les composés ont des attributs neuroprotecteurs sans interférer avec la capacité des médicaments de traverser la barrière hémato-encéphalique. Ces composés possèdent une activité neuroprotectrice à cause de leur inhibition de la progression du cycle cellulaire neuronal. Les composés sont caractérisés en partie par un cinquième cycle joignant les positions 9 et 10.

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