SUCCINIC ACID ESTERS OF 5-HYDROXYADAMANTAN-2-ONE, IMPROVING BLOOD SUPPLY TO ISCHEMIC BRAIN Russian patent published in 2018 - IPC C07C69/40 A61K31/225 A61P9/10 

FIELD: chemistry.

SUBSTANCE: invention relates to succinic acid esters of 5-hydroxyadamantan-2-one and to their study on local blood flow in the cerebral cortex in conditions of transient global ischemia. It has been found that compound Ia and, to a lesser extent, compound Ib, improve blood supply to the brain in rats subjected to transient global ischemia. It was also shown that compound Ia has a lower toxicity than compound Ib. GABAergic mechanism of the cerebrovascular effect of these substances was revealed via in vivo experiments. Therefore, compound Ia has significant cerebrovascular anti-ischemic activity and, unlike 5-hydroxyadamantan-2-one and nimodipine, does not decrease, and in fact within the first 30 minutes slightly increases the level of blood pressure. It is important to emphasise that the ability of drugs to lower the level of blood pressure, i.e. weaken cerebrovascular perfusion pressure, is an important factor limiting their use for the treatment of patients in the acute phase of ischemic stroke.

I a, b, where: Ia R=H; Ib R=5-adamantan-2-one.

EFFECT: disclosed are succinic acid esters of 5-hydroxyadamantan-2-one, which improve blood supply of the ischemic brain.

1 cl