Abstract: The invention provides polymorphs of a compound of Formula (X): The invention also provided pharmaceutical compositions containing polymorphs of the compound and methods treating conditions in a subject by providing polymorphs of the compound.
Type:
Grant
Filed:
November 14, 2022
Date of Patent:
September 5, 2023
Assignee:
IMBRIA PHARMACEUTICALS, INC.
Inventors:
Neil Buckley, Dan Belmont, Sarah Bethune, Krista Diaz
Abstract: Compounds of Formula (I): and salts thereof, and methods of use as Janus kinase inhibitors are described herein.
Type:
Grant
Filed:
February 17, 2021
Date of Patent:
August 22, 2023
Assignee:
Genentech, Inc.
Inventors:
James John Crawford, Mark Zak, Terry Kellar, Yun-Xing Cheng, Wei Li, F. Anthony Romero, Paul Gibbons, Guiling Zhao, Gregory Hamilton, Simon Charles Goodacre
Abstract: The 3-substituted quinolin-2-one compounds are antibacterial agents. The emergence of drug-resistant bacteria calls for constant development of new antibacterial agents with the aim of generating medicaments that are potent against drug sensitive and resistant bacteria and are well tolerated. The present compounds are not only new, but have very valuable antimicrobial properties. These compounds showed a broad spectrum of activity against gram-positive and gram-negative bacteria, as well tuberculosis mycobacteria. They also showed potent activity against drug-resistant bacteria, such as MRSA and VRSA. The molecular target of these compounds was identified as DNA Gyrase B. Based on their pharmacological profiles, the present compounds may find important clinical applications for severe infectious diseases and tuberculosis.
Abstract: Herein, is taught a Eumelanin-inspired antimicrobial capable of overcoming methicillin resistant Staphylococcus aureus (MSRA) and Enterococcus faecalis. By ligating quaternary ammonium functionalized “arms” on to a Eumelanin-inspired indole, with intrinsic antimicrobial activity, a cell wall destroying antimicrobial agent was prepared. It also has antifungal effects against Candida albicans. Further, Eumelanin-inspired phenyleneethynylene (EIPE) derivatives EIPE-1 and EIPE-HCl are novel compounds. EIPE structure serves as scaffolding for functional groups that may have antibacterial properties. Both gram-positive and gram-negative organisms are screened against EIPE derivatives using a standardized Kirby Bauer disk agar diffusion assay. These results showed that EIPE-1 has antibacterial properties against some pathogenic gram-positive organisms.
Type:
Grant
Filed:
July 13, 2021
Date of Patent:
August 22, 2023
Assignee:
The Board of Regents for the Oklahoma Agricultural and Mechanical Colleges
Abstract: An improved process can be used for preparing triacetonamine. The process involves performing an absorption step in which acetone present in the crude product is removed from triacetonamine by distillation, and in gaseous form is then absorbed in countercurrent into fresh, liquid acetone. The acetone stream thus obtained is then converted further to triacetonamine. This process enables more energy-efficient reutilization of the unreacted reactants used in the synthesis of triacetonamine, and thus lowers overall both the use of reactants and the energy expenditure.
Abstract: The present disclosure relates to the endothelin receptor antagonist (ERA) zibotentan in combination with the sodium-dependent glucose cotransporter 2 (SGLT-2) inhibitor dapagliflozin for use in the treatment of certain endothelin related diseases.
Type:
Grant
Filed:
July 9, 2021
Date of Patent:
August 22, 2023
Assignee:
ASTRAZENECA AB
Inventors:
Peter Greasley, Christine Ahlström, Stanko Skrtic, Robert Menzies, Anne-Kristina Mercier, Mikael Sunnåker
Abstract: Described are methods for treating or preventing a neurological disease in a subject. The methods include administering a suppressor of hemichannel permeability to a subject having or prone of getting a neurological disease. The methods include the treatment and prevention of amyotrophic lateral sclerosis (ALS).
Abstract: The present disclosure provides methods for the acute treatment of migraine with or without aura, comprising the administration of ubrogepant. In particular, the present disclosure provides methods for the acute treatment of migraine in patients having hepatic impairment; in patients with renal impairment; and in patients concurrently taking CYP3A4 modulators or BCRP and/or P-gp only inhibitors.
Type:
Grant
Filed:
December 22, 2021
Date of Patent:
August 8, 2023
Assignee:
Allergan Pharmaceuticals International Limited
Inventors:
Joel Trugman, Ramesh Boinpally, Abhijeet Jakate, Michelle Finnegan
Abstract: Provided herein are methods for rational design of nicotine haptens. More particularly, provided herein are methods for designing, selecting, and synthesizing nicotine haptens and nicotine hapten conjugates. Also provided herein are novel nicotine haptens and methods for using nicotine haptens to treat nicotine addiction.
Type:
Grant
Filed:
May 12, 2022
Date of Patent:
August 1, 2023
Assignee:
ARIZONA BOARD OF REGENTS ON BEHALF OF ARIZONA STATE UNIVERSITY
Abstract: The present specification provides crystalline forms of 4-[3-(3-[(cyclopropylamino)methyl]azetidine-1-carbonyl)-4-fluorobenzyl]phthalazin-1(2H)-one hydrochloride, methods of preparing the same, and pharmaceutical compositions comprising the same.
Type:
Grant
Filed:
June 2, 2022
Date of Patent:
July 4, 2023
Assignee:
ILDONG PHARMACEUTICAL CO., LTD.
Inventors:
Kunhee Lee, Seoktaek Lee, Keuncheol Ryu, Hanna Seo, Hyeran Yang, Wonje Seong, Jinyoung Yoon
Abstract: Provided herein are compounds, salts, crystalline forms, and pharmaceutical compositions that are related to thiobutyrate compounds, such as Compound (1) and its salts (such as sodium, potassium, and calcium salt), as well as methods of preparing the same. Also provided herein are methods of using the compounds, salts, crystalline forms, and pharmaceutical compositions for the treatment of diseases or disorders, such as gout and hyperuricemia.
Abstract: Methods and compositions are disclosed for diagnosing a patient suspected of suffering from, and for treating a patient suffering from, a disorder such as hypercortisolemia, metabolic syndrome, pre-diabetes, diabetes, Cushing's syndrome, Cushing's Disease, hyperglycemia secondary to hypercortisolemia, a liver disease, a cardiac disorder, high blood pressure, a blood clotting disorder, a cancer, a psychological disorder, weight gain, a disorder of glucose control, a bone disorder (e.g., osteoporosis), hypogonadism, pseudoacromegaly, pituitary tumors, functional hypercortisolism, ACTH secreting tumors, peripheral neuropathy, dyslipidemia and other disorders. The methods and compositions include administration of a heteroaryl-ketone fused azadecalin glucocorticoid receptor modulator (GRM).
Abstract: Provided herein is a compound of Formula (I) or a pharmaceutically acceptable salt thereof, wherein R3a, R5, R6a, R6b, R17, R21a, R21b, Rm, Rn, R16a, R16b, R7a, R7b, R12a, R12b, R11a, R11b, R2a, R2b, R19, R4a, and R4b are defined herein. Also provided herein are pharmaceutical compositions comprising a compound of Formula (I) and methods of using the compounds, e.g., in the treatment of CNS-related disorders.
Type:
Grant
Filed:
December 8, 2021
Date of Patent:
June 6, 2023
Assignee:
Sage Therapeutics, Inc.
Inventors:
Francesco G. Salituro, Albert Jean Robichaud
Abstract: Disclosed herein are adiponectin receptor agonists and methods of using the same for the treatment of inflammation or bone loss in a subject.
Abstract: The disclosure is directed to, in part, compounds, or pharmaceutically acceptable salts or solvates thereof, for modulating the activity of aldehyde dehydrogenase such as ALDH2 and/or methods for treating and/or preventing an alcohol related disorder such as alcohol use disorder, alcohol induced disorder, alcohol abuse, alcohol dependence, alcohol intoxication, alcohol withdrawal, and the like and/or methods for reducing the amount of alcohol consumed, reducing alcoholic cravings, or increasing the percentage of no heavy drinking days for a subject with alcohol use disorder.
Type:
Grant
Filed:
July 8, 2022
Date of Patent:
May 16, 2023
Assignee:
Sophrosyne Pharmaceuticals Limited
Inventors:
Lewis Feldberg, Akram Sabouni, Thomas R. Bailey, Vincent Wing-Fai Tai
Abstract: The present application relates to compounds which are integrin antagonists. Methods of preparing the integrin antagonists and methods of treating diseases and disorders associated with abnormal levels and/or expression of one or more integrins are also provided.
Abstract: The present technology relates to processes, mixtures and intermediates useful for making fungicide, florylpicoxamid. Also disclosed herein are processes for addition reactions which suppress epimerization and/or racemization.
Abstract: Provided herein are small molecules comprising a first domain that binds to ASH1L and a second domain that facilitates ASH1L degradation. In particular, ASH1L-targeting proteolysis targeting chimeras (PROTACs) and methods of use thereof for the treatment of disease (e.g., acute leukemia, solid cancers and other diseases dependent on activity of ASH1L) are provided.
Type:
Grant
Filed:
September 7, 2021
Date of Patent:
April 25, 2023
Assignee:
The Regents of the University of Michigan
Inventors:
Jolanta Grembecka, Szymon Klossowski, Jing Deng, Tomasz Cierpicki, Hao Li, Hongzhi Miao, Trupta Purohit, EunGi Kim, Dong Chen
Abstract: Disclosed herein are compounds for activating the Reelin signaling system for the treatment of neurological disorders Further provided are compounds and methods for activating a lipoprotein receptor, such as ApoER2 or VLDLR.
Type:
Grant
Filed:
April 18, 2022
Date of Patent:
April 18, 2023
Assignee:
UNIVERSITY OF SOUTH FLORIDA
Inventors:
Edwin John Weeber, Qingyou Li, Melinda Marie Peters, Hana Marie Soueidan