Abstract: For the prevention of parasite infestation of animals, an isoxazoline can be administered by drinking water route. However the inventors have found that when the drinking water is sanitized, for instance by using hypochlorite, the isoxazoline becomes degraded. Surprisingly, the isoxazoline can be protected from degradation by the use of a vitamin E. A pharmaceutical composition can now be prepared containing a concentrated solution of the isoxazoline in a solvent and co-solvent, with vitamin E. The composition can be diluted in drinking water, even when sanitized, to prepare medicated drinking water for animals. This way an anti-parasitic treatment can be mass-administered, leading to a highly effective reduction of the parasite infestation of an animal, and its surroundings.
Abstract: Disclosed are compounds of Formula (I) N-oxides, or salts thereof, wherein G, A, R1, R5, and n are defined herein. Also disclosed are methods of using such compounds as inhibitors of signaling through Toll-like receptor 7, or 8, or 9, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating inflammatory and autoimmune diseases.
Type:
Grant
Filed:
December 18, 2018
Date of Patent:
January 23, 2024
Assignee:
Bristol-Myers Squibb Company
Inventors:
Alaric J. Dyckman, Dharmpal S. Dodd, Christopher P. Mussari, John L. Gilmore, Tasir Shamsul Haque, Trevor C. Sherwood, Brian K. Whiteley, Shoshana L. Posy, Sreekantha Ratna Kumar, Laxman Pasunoori, Srinivasan Kunchithapatham Duraisamy, Subramanya Hegde, Rushith Kumar Anumula, Pitani Veera Venkata Srinivas
Abstract: Methods of treating subjects having disorders associated with mutations in the FXN gene and/or having reduced expression of frataxin protein, e.g., Friedreich ataxia (FA). Generally, the methods include administering a therapeutically effective amount of an agent that increases expression of frataxin protein as described herein, e.g., an inhibitor of a FXN Repressing Factor (FXN-RF).
Abstract: A topical cyclooxygenase (COX) inhibitor formulation comprising an inhibitor of COX-1 and/or COX-2, one or more long chain monounsaturated fatty acids, long chain monounsaturated fatty alcohols, terpenes, or combinations thereof; and a solvent mixture comprising ethanol, propylene glycol, 2-(2-Ethoxyethoxy)ethanol, and optionally dimethylsulfoxide.
Abstract: The present invention provides triazolotriazine derivatives of formula (1) as A2A receptor antagonists. Compounds of formula (1) and pharmaceutical compositions including the compounds can be used for the treatment of disorders related to A2A receptor hyperfunctioning, such as certain types cancers. Compounds of formula (1) and methods of preparing the compounds are disclosed in the invention.
Type:
Grant
Filed:
June 26, 2018
Date of Patent:
January 2, 2024
Assignee:
ZHEJIANG VIMGREEN PHARMACEUTICALS, LTD.
Inventors:
Sanxing Sun, Jinqi Ye, Long Zhao, Chongbo Hu, Zhengshu Chen
Abstract: This invention provides compounds that are inhibitors of HDAC2. The compounds (e.g., compounds according to Formula I, II or any of Compounds 100-128 or any of those in Tables 2 or 3) accordingly are useful for treating, alleviating, or preventing a condition in a subject such as a neurological disorder, memory or cognitive function disorder or impairment, extinction learning disorder, fungal disease or infection, inflammatory disease, hematological disease, or neoplastic disease, or for improving memory or treating, alleviating, or preventing memory loss or impairment.
Type:
Grant
Filed:
December 28, 2020
Date of Patent:
January 2, 2024
Assignee:
Alkermes, Inc.
Inventors:
Martin R. Jefson, John A. Lowe, III, Fabian Dey, Andreas Bergmann, Andreas Schoop, Nathan Oliver Fuller
Abstract: The present invention provides triazolotriazine derivatives of formula (1) as A2A receptor antagonists. Compounds of formula (1) and pharmaceutical compositions including the compounds can be used for the treatment of disorders related to A2A receptor hyperfunctioning, such as certain types cancers. Compounds of formula (1) and methods of preparing the compounds are disclosed in the invention.
Type:
Grant
Filed:
June 26, 2018
Date of Patent:
December 19, 2023
Assignee:
ZHEJIANG VIMGREEN PHARMACEUTICALS, LTD.
Inventors:
Sanxing Sun, Long Zhao, Chongbo Hu, Zhengshu Chen, Jinqi Ye
Abstract: The polymeric clotrimazole biofilm for the treatment of otomycosis contains clotrimazole or a pharmaceutically acceptable salt thereof as the active pharmaceutical ingredient in a polymer biofilm thug delivery vehicle. The polymer may be a bio compatible polymer, such as hydroxypropylmethylcellulose (HPMC). Propylene glycol may be added to the mixture as a plasticizer to promote formation of the film. The drug and the polymer may be solvated in a casting solvent and then mixed in a 1:3 ratio of drug:polymer. About 15% propylene glycol may be added to the mixture, which is then heated at 40° C. until a thin, flexible film forms. A round, knife-thick patch of the biofilm may be applied to the patient's ear through the external canal and over the tympanic membrane.
Type:
Grant
Filed:
July 12, 2023
Date of Patent:
December 19, 2023
Assignee:
KING FAISAL UNIVERSITY
Inventors:
Mai Mostafa Khalaf Ali, Hany Mohamed Abd El-Lateef Ahmed, Ahmed Mohammed Abu-Dief Mohammed, Amr Embaby Elsayed Karamany, Mahmoud Ibrahim Mahmoud Abdelmagid, Mohammed Sherif Saddik Ibrahim, Ali Khames Abd Eltwab Morsy
Abstract: Pharmaceutical compositions for topical application to skin are provided. In some embodiments, the pharmaceutical compositions comprise a corticosteroid and further comprise a liquid oil component comprising one or more dicarboxylic acid esters and/or monocarboxylic acid esters.
Abstract: The invention provides compositions and methods for the induction of cell death, for example, cancer cell death. Combinations of compounds and related methods of use are disclosed, including the use of compounds in therapy for the treatment of cancer and selective induction of apoptosis in cells. The disclosed drug combinations can have lower neurotoxicity effects than other compounds and combinations of compounds.
Type:
Grant
Filed:
January 8, 2021
Date of Patent:
December 5, 2023
Assignees:
Vanquish Oncology, Inc., The Board of Trustees of the University of Illinois
Inventors:
Paul J. Hergenrother, Rachel C. Botham, Timothy M. Fan, Mark J. Gilbert, Michael K. Handley, Howard S. Roth, Theodore M. Tarasow
Abstract: Small molecule inhibitors (SMIs) of the Prolactin receptor, pharmaceutical compositions of the SMIs, and methods for treating patients suffering from disorders characterized increased expression or excitation of the Prolactin receptor, including breast cancer, prostate cancer and nociceptive pain disorders such as migraine headache, by administering pharmaceutical compositions of SMIs are provided.
Type:
Grant
Filed:
September 30, 2021
Date of Patent:
December 5, 2023
Assignees:
University of Cincinnati, University of Texas System, The Hebrew University of Jerusalem
Inventors:
Nira Ben-Jonathan, Eric R. Hugo, Edward J. Merino, Abraham J. Domb, Armen N. Akopian
Abstract: Described are methods of treating or preventing a disease in a subject treatable by modulating cell mechanics. The method includes administering to a subject having or at risk for such a disease a pharmaceutical composition.
Type:
Grant
Filed:
July 6, 2020
Date of Patent:
December 5, 2023
Assignee:
THE JOHNS HOPKINS UNIVERSITY
Inventors:
Douglas Robinson, Alexandra Surcel, Win Pin Ng, Caren L. Freel Meyers
Abstract: A method for relieving menstrual pain and reducing menstrual blood loss in a female is provided. The method comprises administering to the female an oral combination drug formulation comprising a first therapeutically effective dose of a non-steroidal anti-inflammatory drug (NSAID) and a second complementary low dose of tranexamic acid, wherein the NSAID is formulated to relieve the menstrual pain and to reduce a volume of menstrual blood loss of the female, wherein the dose of tranexamic acid ranges from 200 mg to 250 mg per oral combination drug formulation.
Abstract: The polymeric clotrimazole biofilm for the treatment of otomycosis contains clotrimazole or a pharmaceutically acceptable salt thereof as the active pharmaceutical ingredient in a polymer biofilm drug delivery vehicle. The polymer may be a biocompatible polymer, such as hydroxypropylmethylcellulose (HPMC). Propylene glycol may be added to the mixture as a plasticizer to promote formation of the film. The drug and the polymer may be solvated in a casting solvent and then mixed in a 1:3 ratio of drug:polymer. About 15% propylene glycol may be added to the mixture, which is then heated at 40° C. until a thin, flexible film forms. A round, knife-thick patch of the biofilm may be applied to the patient's ear through the external canal and over the tympanic membrane.
Type:
Grant
Filed:
February 6, 2023
Date of Patent:
December 5, 2023
Assignee:
KING FAISAL UNIVERSITY
Inventors:
Mai Mostafa Khalaf Ali, Hany Mohamed Abd El-Lateef Ahmed, Ahmed Mohammed Abu-Dief Mohammed, Amr Embaby Elsayed Karamany, Mahmoud Ibrahim Mahmoud Abdelmagid, Mohammed Sherif Saddik Ibrahim, Ali Khames Abd Eltwab Morsy
Abstract: Materials (e.g., particles, hydrogels) that provide extended release of one or more therapeutic agents are useful platforms for drug delivery. In part, the present invention relates to new triblock (ABC) bottlebrush copolymers which can be used in the formulation of particles and hydrogels for the extended release of therapeutic agents. In certain embodiments, the triblock bottlebrush copolymers, particles, and hydrogels described herein are thermally-responsive and gel at physiological temperature (e.g., upon administration to a subject), providing injectable and/or implantable gels which can be used for extended release drug delivery. The present invention also provides methods for extended release drug delivery, and methods of treating and/or preventing a disease or conditions in a subject, using the inventive copolymers, particles, and hydrogels. In addition, the present invention provides methods of preparing the triblock bottlebrush copolymers described herein.
Type:
Grant
Filed:
May 29, 2020
Date of Patent:
November 28, 2023
Assignee:
Massachusetts Institute of Technology
Inventors:
Jeremiah A. Johnson, Qixian Chen, Farrukh Vohidov
Abstract: This disclosure features chemical entities (e.g., a compound or a pharmaceutically acceptable salt, and/or hydrate, and/or cocrystal, and/or drug combination of the compound) that modulate (e.g., agonizes or partially agonizes) NLRP3 that are useful, e.g., for treating a condition, disease or disorder in which an increase in NLRP3 signaling may correct a deficiency in innate immune activity (e.g., a condition, disease or disorder associated with an insufficient immune response) that contributes to the pathology and/or symptoms and/or progression of the condition, disease or disorder (e.g., cancer) in a subject (e.g., a human). This disclosure also features compositions as well as other methods of using and making the same.
Type:
Grant
Filed:
May 6, 2021
Date of Patent:
November 28, 2023
Assignee:
INNATE TUMOR IMMUNITY, INC
Inventors:
Gary D. Glick, Shomir Ghosh, William R. Roush, Edward James Olhava, Daniel O'Malley
Abstract: The invention provides a method of treating a subject afflicted with a dystonia, comprising periodically administering to the subject a pharmaceutical composition comprising an amount of pridopidine effective to treat the subject.
Type:
Grant
Filed:
February 24, 2019
Date of Patent:
November 28, 2023
Assignee:
PRILENIA NEUROTHERAPEUTICS LTD
Inventors:
Michael Hayden, Spyridon Papapetropoulos, Juha-Matti Savola, Eli Eyal, Beth Borowsky, Igor D. Grachev, Mark Forrest Gordon
Abstract: The present invention relates to a compound of the following general formula (I): or a pharmaceutically acceptable salt and/or solvate thereof, for use as drug, particularly intended for inhibiting a programmed cell death route selected from the group consisting of ferroptosis, oxytosis and cellular necroptosis. The present invention also relates to a compound of general formula (I) for use as a drug for neuroprotection as well as for preventing and/or treating disorders associated with cellular necroptosis or ferroptosis. The present invention also relates to a pharmaceutical composition comprising a compound of general formula (I), or a pharmaceutically acceptable salt and/or solvate thereof. The present invention also encompasses the use of a compound of the general formula (I) for organs preservation.
Type:
Grant
Filed:
December 10, 2021
Date of Patent:
November 21, 2023
Assignees:
Institut National de la Sante et de la Recherche Medicale (INSERM), Centre National de la Recherche Scientifique (CNRS), Sorbonne Universite, Universite de Poitiers, Centre Hospitalier Universitaire de Poitiers
Abstract: Novel cromolyn analogs useful as imaging agents for detecting atherosclerotic plaques and for treating atherosclerosis and Alzheimer's Disease, and methods of making the cromolyn analogs, are disclosed. The cromolyn analogs have the general formula: wherein: X is OH, C1-C6 alkoxyl; Y and Z are independently selected form a C1-C6 alkyl, C1-C6 alkoxyl, halogen, un-substituted or C1-C6 substituted amine, 18F, 19F, or H; and n is 1, 2, or 3; and wherein for structure (I), if n are both 1 and Y and Z are both H and X is OH.