TREATMENTS FOR AMYOTROPHIC LATERAL SCLEROSIS USING DAZUCORILANT

    公开(公告)号:US20240156806A1

    公开(公告)日:2024-05-16

    申请号:US18496134

    申请日:2023-10-27

    摘要: Applicant discloses methods and compositions for treating a patient suffering from amyotrophic lateral sclerosis (ALS) comprising administration of a heteroaryl ketone fused azadecalin compound. In embodiments, the heteroaryl ketone fused azadecalin compound is dazucorilant: (R)-(1-(4-fluorophenyl)-6-((4-(trifluoromethyl)phenyl) sulfonyl)-4, 4a, 5,6,7,8-hexahydro-1-H-pyrazolo[3,4-g]isoquinolin-4a-yl) (pyridin-2-yl)methanone, having the chemical structure illustrated as




    Suitable doses include daily administration of 150 milligrams and 300 milligrams of dazucorilant. Suitable doses include daily administration of dazucorilant with food, or with water, or with food and water. Daily administration of dazucorilant is effective to increase dazucorilant exposure up to about 2-fold when continued for seven days or more. Administration of such a heteroaryl ketone fused azadecalin compound may comprise oral administration, enteral administration, or other administration. Pharmaceutical compositions comprising dazucorilant are useful in the treatment of patients suffering from ALS. Suitable pharmaceutical compositions comprising dazucorilant include, e.g., pharmaceutical compositions for oral administration and pharmaceutical compositions for enteral administration.

    USE OF COMPOSITION CONTAINING CILOSTAZOL IN CEREBROVASCULAR DISEASES

    公开(公告)号:US20240122917A1

    公开(公告)日:2024-04-18

    申请号:US18263191

    申请日:2022-01-26

    摘要: Disclosed is the use of a composition containing cilostazol or a pharmaceutically acceptable salt thereof and edaravone in the preparation of a drug for treating cerebrovascular diseases, especially ischemic cerebrovascular diseases. The experiment result shows that the tail vein administration of 1-15 mg/kg of cilostazol or 1.67-8.33 mg/kg of edaravone on rats with a focal cerebral ischemia-reperfusion injury can significantly ameliorate neurological defects in rats with an MCAO and reduce a cerebral infarction area; and performing compound combination within the dosage range (the mass ratio of cilostazol:edaravone is 1:5 to 5:1) can be synergistic. The tail vein administration of 3.33-16.67 mg/kg of cilostazol or 3.33-16.67 mg/kg of edaravone on mice with a focal cerebral ischemia-reperfusion injury can significantly ameliorate neurological defects in mice with an MCAO and reduce a cerebral infarction area.