Use of sildenafil and rock inhibitors for treating stroke or sequelae following stroke

Patent metadata

Field	Value
Publication number	US-2022273662-A1
Application number	US-202217744162-A
Country	US
Kind code	A1
Filing date	May 13, 2022
Priority date	Nov 14, 2019
Publication date	Sep 1, 2022
Grant date	—

Abstract

The present invention relates to a use of a pharmaceutical composition for treating stroke or sequelae following stroke, the composition comprising a phosphodiesterase type 5 activity inhibitor and a Rho-associated kinase (ROCK) inhibitor.The present inventors have performed research, based on clinical knowledge related to stroke treatment, in order to use sildenafil and a ROCK inhibitor in combination to treat stroke or sequelae caused by stroke, and as a result, confirmed for the first time that stroke or sequelae caused by stroke were significantly improved when sildenafil and a ROCK inhibitor were co-administered compared to when sildenafil or the ROCK inhibitor was administered by itself. Therefore, it is expected that a pharmaceutical composition according to the present invention will be able to be effectively used for treating or studying stroke or stroke-related sequelae.

First claim

1 . A method for treating an ischemic cerebrovascular disease or sequelae following the ischemic cerebrovascular disease, the method including administering a pharmaceutical composition to an individual, wherein the pharmaceutical composition comprising a phosphodiesterase type 5 activity inhibitor; and a Rho-associated kinase (ROCK) inhibitor.

2 . The pharmaceutical composition of claim 1 , wherein the ischemic cerebrovascular disease is selected from the group consisting of ischemic stroke (cerebral infarction), thrombosis, embolism, transient ischemic attack, leukoplakia and small infarction.

3 . The pharmaceutical composition of claim 1 , wherein the sequelae following the ischemic cerebrovascular disease is any one selected from the group consisting of loss of locomotor activity, an anxiety disorder and cognitive function decline.

4 . The pharmaceutical composition of claim 1 , wherein the phosphodiesterase type 5 activity inhibitor is any one selected from the group consisting of mirodenafil, sildenafil, vardenafil, tadalafil, udenafil, dasantafil, avanafil and pharmaceutically acceptable salts, solvates and hydrates thereof.

5 . The pharmaceutical composition of claim 1 , wherein the ROCK inhibitor is any one selected from the group consisting of fasudil, ripasudil, RKI-1447, Y-27632, GSK429286A, Y-30141 and pharmaceutically acceptable salts, solvates and hydrates thereof.

6 . The pharmaceutical composition of claim 1 , wherein the pharmaceutical composition is for administration before reperfusion after cerebrovascular occlusion, simultaneously with the reperfusion or after the reperfusion.

7 . A method for improving a prognosis of an ischemic cerebrovascular disease, the method including administering a pharmaceutical composition to an individual, wherein the pharmaceutical composition comprising a phosphodiesterase type 5 activity inhibitor; and
a Rho-associated kinase (ROCK) inhibitor.

8 . A method for enhancing a cognitive function, the method including administering a pharmaceutical composition to an individual, wherein the pharmaceutical composition comprising a phosphodiesterase type 5 activity inhibitor; and
a Rho-associated kinase (ROCK) inhibitor.

Assignees

• Univ Soonchunhyang Ind Acad Coop Found

Inventors

• Oh Jae-Sang
• Kim Duk-Soo
• Lee Man-Ryul
• Kang Juhyeon

Classifications

• A61K31/4439 Primary

  containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole (nicotine A61K31/465) · CPC title

• A61K31/519 Primary

  ortho- or peri-condensed with heterocyclic rings · CPC title

• A61P9/10

  for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis · CPC title

• A61P7/02

  Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors · CPC title

• A61K31/551

  having two nitrogen atoms, e.g. dilazep · CPC title