Abstract: The invention provides compositions, formulations, and methods for treatment of malignancies via activation of an inflammatory response in the subject. Such compositions, formulations, and methods for are preferably used in conjunction with other therapies for the treatment and/or management of malignancies, e.g., chemotherapy and/or radiation. The invention also provides methods of monitoring immune activation in subjects with malignancies.
Abstract: Described herein is the chemical structure of neurosteroid derivative compounds, methods of synthesizing the derivatives, and their uses in treating disorders, including those of the central nervous system. These compounds are readily synthesized and have improved pharmaceutical properties, including water solubility, compared to known neurosteroids.
Abstract: A method of treating Alcohol Use Disorder (AUD), Substance Use Disorder (SUD), tobacco use, pain, or proinflammatory disorders comprising: providing a subject with an effective amount of a modified tetracycline or derivative thereof to ameliorate or eliminate the AUD, SUD, tobacco use, pain, or proinflammatory disorder, and wherein the modified tetracycline or derivative thereof has reduced binding to a microbial ribosome and has the formula wherein R1 is acetyl, R2 is OH or acetyl, R3 is acetyl, R4 is H or acetyl, and R5 is acetyl.
Type:
Grant
Filed:
June 13, 2019
Date of Patent:
January 3, 2023
Assignee:
Texas Tech University System
Inventors:
Susan E. Bergeson, Peter Syapin, Ted W. Reid, Mayank Shashtri, Phat Tran
Abstract: Disclosed herein are novel compounds and methods for the treatment of acute organ injury, including injuries resulting from ischemic events. The compounds may be used to treat organ including the brain, heart, or kidney, which have injured as a result of events such as stroke, cardiac arrest, traumatic brain injury, hemorrhagic shock, or subarachnoid hemorrhage.
Type:
Grant
Filed:
September 26, 2019
Date of Patent:
December 27, 2022
Assignee:
University of Pittsburgh—of the Commonwealth System of Higher Education
Abstract: The invention relates to compounds of general formula (I): wherein R2a, R2b, R3a, R3b, R5, Y and R7 are as defined herein are selective agonists at the FXR receptor and are useful for the treatment or prevention of diseases and conditions including nonalcoholic steatohepatitis (NASH); primary biliary cirrhosis; primary sclerosing cholangitis; biliary atresia; cholestatic liver disease; hepatitis C infection; alcoholic liver disease; fibrosis; and liver damage arising from fibrosis.
Type:
Grant
Filed:
July 30, 2019
Date of Patent:
December 6, 2022
Assignees:
NZP UK LIMITED, THE UNIVERSITY OF SOUTHAMPTON
Inventors:
Alexander Charles Weymouth-Wilson, Gemma Packer, Bruno Jan Pol Linclau, Dannielle Kydd-Sinclair, Kimberly Ann Watson
Abstract: Provided are compositions comprising unequal mixtures of (R)-amisulpride and (S)-amisulpride, or pharmaceutically acceptable salts thereof, where the amount of (R)-amisulpride is greater than the amount of (S)-amisulpride, compositions and medicaments comprising the same used for the treatment of various diseases and disorders, and methods of using same for the treatment of various diseases and disorders, including, but not limited to, dosage regimens. In addition, provided are various formulations thereof, including, but not limited to, formulations employing polymorphs of enantiomeric amisulpride.
Type:
Grant
Filed:
November 13, 2020
Date of Patent:
December 6, 2022
Assignee:
Sunovion Pharmaceuticals Inc.
Inventors:
Seth Cabot Hopkins, Kenneth Stephen Koblan, John R. Snoonian, Harold Scott Wilkinson
Abstract: The present disclosure relates to stereodefined polycyclic (e.g., tetracyclic) compounds that contain quaternary centers at one or multiple ring fusions, synthetic methods for preparing such compounds, and methods of using such compounds to treat a disease, such as a brain tumor and, particularly, a glioma.
Abstract: Described herein are neuroactive steroids of the Formula (I): or a pharmaceutically acceptable salt thereof; wherein -------, R1, R2, R5, A and L are as defined herein. Such compounds are envisioned, in certain embodiments, to behave as GABA modulators. The present invention also provides pharmaceutical compositions comprising a compound of the present invention and methods of use and treatment, e.g., such for inducing sedation and/or anesthesia.
Type:
Grant
Filed:
April 8, 2020
Date of Patent:
November 15, 2022
Assignee:
Sage Therapeutics, Inc.
Inventors:
Gabriel Martinez Botella, Boyd L. Harrison, Albert Jean Robichaud, Francesco G. Salituro, Robert Jason Herr, Robert Borbo Kargbo
Abstract: The present invention relates to a composition comprising 2,4,6-trihydroxyacetophenone (THA) as an effective ingredient for prevention or treatment of prostate cancer. THA in the present invention is a main ingredient of Curcuma comosa. The composition of the present invention effectively inhibits the growth of prostate cancer by regulating in particular the activity of polo-like kinase 1 (PLK1) and thus is expected to find useful applications in use in the prevention, alleviation, and treatment of prostate cancer in future.
Abstract: The invention relates to the treatment of brain tumors, specifically to improved therapy for glioblastoma utilizing specific endocrine modulators and drug combinations. The compositions and uses thereof according to the invention employ androgen receptor (AR) inhibitors, either alone or in combination with receptor tyrosine kinase inhibitors and/or chemotherapeutic agents. According to certain advantageous embodiments, the use of the AR inhibitor enzalutamide, optionally in combination with epidermal growth factor receptor inhibitors such as erlotinib and alkylating agents such as carmustine and temozolomide, is contemplated.
Type:
Grant
Filed:
July 20, 2017
Date of Patent:
October 25, 2022
Assignee:
Hadasit Medical Research Services and Development Ltd.
Inventors:
Iris Lavon Ben Moshe, Tamar Canello Avramovitch
Abstract: The present invention relates to compounds which are intermediates in the synthesis of bile acid derivatives with pharmacological activity. The invention relates to compounds of general formula (I): wherein: , R1, R2, R3, R4, R5, R6 and Y are as defined herein. The compounds are intermediates in the synthesis of synthetic bile acids which are useful in the treatment of conditions such as liver disease. In addition, the invention relates to a method of synthesizing these intermediates and a method of preparing obeticholic acid and obeticholic acid analogues from the compounds of the invention.
Type:
Grant
Filed:
February 26, 2021
Date of Patent:
October 25, 2022
Assignee:
NZP UK Limited
Inventors:
Alexander Weymouth-Wilson, Zofia Komsta, Laura Wallis, Timothy Evans, Ieuan Davies, Carl Otter, Rhys Batchelor
Abstract: Neuroactive steroid anaesthetic agents, methods for their preparation and compositions comprising the same are disclosed. Also provided are scaled up and/or GMP methods for preparing neuroactive steroids, such as alfaxalone, alfadolone and alfadolone acetate.
Abstract: The present invention includes DNP derivatives that are useful for preventing or treating a metabolic disease or disorder in a subject in need thereof. In certain embodiments, the subject is further administered at least one additional therapeutic agent.
Abstract: The present application relates generally to methods for treating, preventing and/or slowing the onset or progression of schizophrenia and/or a related symptom. The methods comprise administering at least one aminosterol or a pharmaceutically acceptable salt or derivative thereof to a subject in need.
Abstract: Described are oxysterols, pharmaceutical compositions including the oxysterols, and methods of using the oxysterols and compositions for treating diseases and/or disorders related to inflammation, such as necrotizing enterocolitis, mesenteric ischemia, inflammatory bowel diseases including Crohn's disease and ulcerative colitis, lymphocytic colitis, Celiac disease. Behcet's disease, rheumatoid arthritis, psoriasis, and autoimmune thyroid disease.
Abstract: The present invention relates to a preparation method of a novel vascular leakage blocker with a high yield. The preparation method is easy to react and more productive and economical than the conventional method by using an intermediate that can easily remove impurities generated during the reaction. In addition, the preparation method can produce a novel vascular leakage blocker with a high yield by using a new reagent that has not been previously used in the step of generating an isomer, and is very advantageous in producing a high-quality active pharmaceutical ingredient.
Type:
Grant
Filed:
July 28, 2020
Date of Patent:
September 27, 2022
Assignee:
CURACLE CO., LTD.
Inventors:
Koo Hyeon Ahn, Myung-Hwa Kim, Jung-Ln Pyo, Chul Su Baek, Sung Hwan Kim
Abstract: This invention relates to methods of stimulating the activity of the human and animal enteric nervous system. The method comprises orally administering an aminoserol, such as squalamine, a naturally occurring aminosterol isolated from Squalus acanthias, or derivatives thereof, to a subject in need.
Abstract: The present disclosure relates to a pharmaceutical composition for treating gallbladder disease containing a gallstone-dissolving agent, and more specifically, to a pharmaceutical composition for treating gallbladder disease containing a gallstone-dissolving agent which dissolves gallstone, a cause of the gallbladder disease, and thus has an excellent effect of alleviating or treating any one or more symptoms selected from the group consisting of asymptomatic cholelithiasis, biliary colic, cholecystitis, choledocholithiasis, and biliary pancreatitis.
Type:
Grant
Filed:
September 19, 2017
Date of Patent:
August 2, 2022
Assignee:
SurgiNex Co., Ltd.
Inventors:
Say June Kim, Kwan Young Jeong, Ok Hee Kim, Seok Jun Jo, Min Jin Yoo
Abstract: An anthraquinone compound of formula I (such as the compounds of formulae II to X) and processes for making the same are provided. Pharmaceutical compositions for use in the treatment of cancer, optionally in combination with an agent capable of reducing the level of oxygenation of a tumour, are also provided. Additionally, an option for combination with chemotherapeutic and radiotherapeutic modalities to enhance overall tumour cell kill is provided. Methods for the detection of cellular hypoxia, both in vivo and in vitro, are additionally provided.
Type:
Grant
Filed:
August 19, 2019
Date of Patent:
August 2, 2022
Assignee:
ONCOTHERICS VENTURES LIMITED
Inventors:
Stefan Ogrodzinski, Paul Smith, Stephanie McKeown, Laurence Patterson, Rachel Jane Errington