公开(公告)号：US12115167B2

公开(公告)日：2024-10-15

申请号：US18444104

申请日：2024-02-16

申请人： Woolsey Pharmaceuticals, Inc.

发明人： Qicai Liu ,  Hemant N. Joshi ,  Thomas Macallister

IPC分类号： A61K31/551 ,  A61K9/00 ,  A61K9/16 ,  A61K47/58

CPC分类号： A61K31/551 ,  A61K9/0053 ,  A61K9/16 ,  A61K47/585

摘要： An oral pharmaceutical composition is provided that can comprise a rho kinase inhibitor, for example, fasudil, a pharmaceutically acceptable salt thereof, a hydrate thereof, a prodrug thereof, a substituted derivative thereof, or a metabolite thereof, or any combination thereof, the rho kinase inhibitor having a bitter taste; and an ion exchange resin. The ion exchange resin can partially or fully mask the bitter taste of the rho kinase inhibitor, making the composition more palatable. The composition can comprise a solid dosage form, and/or a liquid dosage form. The solid dosage form can comprise a powder, granules, a tablet, or a capsule, or any combination thereof. The composition can be present, for example, in a unit dose, in an amount sufficient to treat a neurodegenerative disease. A method of treating the neurodegenerative disease with the oral pharmaceutical composition is provided. The method can ameliorate a symptom of a neurodegenerative disease.

公开(公告)号：US20230405017A1

公开(公告)日：2023-12-21

申请号：US17907185

申请日：2021-01-08

申请人： Woolsey Pharmaceuticals, Inc.

发明人： Thomas MACALLISTER ,  Sven JACOBSON

IPC分类号： A61K31/551

CPC分类号： A61K31/551

摘要： The present invention relates to methods of treating frontotemporal dementia. The methods are preferably accomplished by treatment with a rho kinase inhibitor, such as fasudil or hydroxyfasudil. In particular, the invention contemplates treatment of the behavioral variant frontotemporal dementia and usually treatment begins once symptoms become evident. Usually, patients treated according to the invention have no neuromuscular symptoms and generally have not been diagnosed with amyotrophic lateral sclerosis, corticobasal degeneration, Parkinson's Disease or progressive supranuclear palsy. A preferred method of the invention involves oral treatment with fasudil, administered in a total daily dose of between 70 mg and 140 mg.

公开(公告)号：US11771704B1

公开(公告)日：2023-10-03

申请号：US18175605

申请日：2023-02-28

申请人： Woolsey Pharmaceuticals, Inc.

发明人： Thomas MacAllister ,  Sven Jacobson

IPC分类号： A61K31/5513 ,  A61K9/00 ,  A61P25/28

CPC分类号： A61K31/5513 ,  A61K9/0053 ,  A61P25/28

摘要： Disclosed are methods of treating patients with AD using a rho kinase inhibitor. A preferred rho kinase inhibitor used according to the invention is fasudil, which is typically administered orally in a total daily dose of 70-140 mg. A preferred dosing regimen involves administering the daily dose in three equal portions throughout the day. Preferred methods continue for more than one month and typically at least 2 or 3 months. Some preferred methods do not treat mild cognitive impairment and patients have and MMSE score of≤23 and/or a CDR-SOB score of≥4.5.

公开(公告)号：US11642352B2

公开(公告)日：2023-05-09

申请号：US17144802

申请日：2021-01-08

申请人： WOOLSEY PHARMACEUTICALS, INC.

发明人： Thomas MacAllister ,  Sven Jacobson

IPC分类号： A61K31/551 ,  A61P25/28

CPC分类号： A61K31/551 ,  A61P25/28

摘要： The invention is based on the discovery that rho kinase inhibitors can be used to treat proteinopathy associated wandering. A number of degenerative neurological diseases are thought to be caused, at least in part, by the formation of protein aggregates that cause neurotoxicity and progressive decline in function. The inventive methods related to the use of rho kinase inhibitors in the treatment of patients with proteinopathy-associated wandering. The patients may be suffering from Huntington's disease, a traumatic brain injury, autism spectrum disorder, Down syndrome or a proteinopathy-associated dementia, such as Alzheimer disease or frontotemporal dementia.

公开(公告)号：US20220125799A1

公开(公告)日：2022-04-28

申请号：US17145084

申请日：2021-01-08

申请人： Woolsey Pharmaceuticals, Inc.

发明人： Thomas MACALLISTER ,  Sven JACOBSON

IPC分类号： A61K31/551

摘要： The present invention relates to the treatment patient with a 4-repeat (4R) tauopathy using a therapeutically effect amount of a rho kinase inhibitor. One preferred inhibitor is fasudil and preferred methods involve the daily oral administration of between 20 and 250 mg of fasudil. Preferred 4R tauopathies treatable according to the invention include progressive supranuclear palsy with Richardson syndrome (PSP-RS) and corticobasal syndrome with probable sporadic corticobasal degeneration.

公开(公告)号：US20210401853A1

公开(公告)日：2021-12-30

申请号：US17166733

申请日：2021-02-03

申请人： WOOLSEY PHARMACEUTICALS, INC.

发明人： Thomas MACALLISTER ,  Sven JACOBSON

IPC分类号： A61K31/551

摘要： The invention relates to the treatment of neurodevelopmental disorders using an inhibitor of rho kinase. Preferred methods contemplate the treatment of infants and children. Certain embodiments involve treating a neurodevelopmental disorder is caused by defects of metabolism, including defects of amino acid transport or metabolism, acid-base balance, carbohydrate transport or metabolism, metal homeostasis, neurotransmitter metabolism, or fatty acid transport or metabolism. Methods address a variety of conditions caused by changes in the genetic material that affect the structure and/or expression of certain genes. Preferred methods treat Down syndrome, Fragile X syndrome, oligophrenin 1 deficiency, Rett syndrome, autistic disorder, Asperger's syndrome, pervasive developmental disorder not otherwise specified, and other autism spectrum disorders.

公开(公告)号：US20240299408A1

公开(公告)日：2024-09-12

申请号：US18549237

申请日：2021-01-08

申请人： Woolsey Pharmaceuticals, Inc.

发明人： Thomas MACALLISTER ,  Sven JACOBSON

IPC分类号： A61K31/551

CPC分类号： A61K31/551

摘要： The present invention relates to the treatment patient with a 4-repeat (4R) tauopathy using a therapeutically effect amount of a rho kinase inhibitor. One preferred inhibitor is fasudil and preferred methods involve the daily oral administration of between 20 and 250 mg of fasudil. Preferred 4R tauopathies treatable according to the invention include progressive supranuclear palsy with Richardson syndrome (PSP-RS) and corticobasal syndrome with probable sporadic corticobasal degeneration.

公开(公告)号：US20240261298A1

公开(公告)日：2024-08-08

申请号：US18560760

申请日：2022-05-16

申请人： Woolsey Pharmaceuticals, Inc.

发明人： Thomas MACALLISTER ,  Sven JACOBSON

IPC分类号： A61K31/551

CPC分类号： A61K31/551

摘要： The invention relates to the treatment of patients with depression and or anxiety with high doses of rho kinase inhibitors. The maximum dose of a rho kinase inhibitor, based on fasudil hydrochloride as an exemplary agent, is more than 70 mg per day based on an immediate release formulation. Comparable dosing with other inhibitors is selected based on molar equivalents and/or rho kinase binding affinities. Treatable patients have one or more depressive disorders and/or one or more anxiety disorders.

公开(公告)号：US20230414633A1

公开(公告)日：2023-12-28

申请号：US18462488

申请日：2023-09-07

申请人： Woolsey Pharmaceuticals, Inc.

发明人： Thomas MACALLISTER ,  Sven JACOBSON

IPC分类号： A61K31/551 ,  A61P25/28

CPC分类号： A61K31/551 ,  A61P25/28

摘要： The present invention relates to the treatment of a sporadic ALS patient with oral fausdil at a dose of 180-240 mg/day. This results in an anticipated 25-50% reduction in the average decline over at least three months as measured using the revised ALS Functional Rating Scale.

公开(公告)号：US20230321114A1

公开(公告)日：2023-10-12

申请号：US18042785

申请日：2021-01-08

申请人： Woolsey Pharmaceuticals, Inc.

发明人： Thomas MACALLISTER ,  Sven JACOBSON

IPC分类号： A61K31/551

CPC分类号： A61K31/551

摘要： Methods of treating subjects with age-related cognitive decline with a rho kinase inhibitor are disclosed. In a preferred embodiment, the rho kinase inhibitor is fasudil and it is administered orally in a daily dose of between 70 and 250 mg per day. Subjects have a cognitive impairment on a global cognitive scale, like the MoCA or the MMSE and/or specific impairments related to different cognitive domains. A method of reducing the rate of age-related cognitive decline, comprising administering to a subject with evidence of age-related cognitive decline an effective amount of a rho kinase inhibitor. The inventive methods slow the rate of cognitive decline and/or improve cognition from baseline in treated individuals. The methods may result in enhancing processing speed, increasing attention, improving memory, improving language, improving visual construction skills and/or improving executive function in subjects experiencing age-related cognitive decline.