Compounds for the prevention and treatment of bleeding and vascular instability

Abstract

Thrombolytic therapy and anticoagulant therapy can induce bleeding and vascular instability. Presented herein, in certain embodiments, are methods for treating and / or preventing bleeding and vascular instability, comprising administering a compound disclosed herein to a subject in need thereof.

Claims

1. Formula IV: For the prevention, reduction, suppression, mitigation, alleviation, or treatment of bleeding in the subject, or for the prevention or treatment of reperfusion injury. 【Chemistry 1】 A composition comprising a compound having the structure or a pharmaceutically acceptable salt, stereoisomer, or tautomer thereof in a therapeutically effective amount, The aforementioned bleeding is induced by thrombolytic therapy, anticoagulant therapy, or intravascular intervention therapy. The bleeding includes internal bleeding or hemorrhagic changes, and the bleeding includes intracerebral hemorrhage. A composition in which the aforementioned reperfusion injury occurs as a result of medical intervention.

2. A composition for the prevention or treatment of reperfusion injury in the subject, wherein the reperfusion injury occurs as a result of thrombolytic therapy, anticoagulant therapy, or intravascular intervention therapy in the brain, according to claim 1.

3. The composition according to claim 1, wherein the prevention of the bleeding, reduction of the risk thereof, suppression, mitigation, alleviation, or treatment thereof includes a reduction in bleeding volume.

4. The composition according to claim 1 or 3, wherein the bleeding is induced by thrombolytic therapy, and the thrombolytic therapy comprises the administration of tissue plasminogen activator (TPA), streptokinase, streptokinase activator, or urokinase.

5. The composition according to claim 4, wherein the tissue plasminogen activator comprises alteplase, reteplase, or tenecteplase (TNKase, Metallyse).

6. The composition according to claim 1, 3, 4, or 5, wherein the bleeding is induced by an endovascular intervention, the endovascular intervention includes mechanical thrombectomy.

7. The subject is a person having an ischemic stroke and receiving administration of tissue plasminogen activator (TPA), and the composition is as described in claim 1 or 2.

8. The composition according to claim 7, which is administered before, during, or after the administration of tissue plasminogen activator (TPA).

Images