Abstract: The present invention includes a method and compositions for preventing primary or acquired resistance of epidermal growth factor receptors (EGFR) inhibitors in a cancer with deregulated EGFR comprising: identifying a subject suspected of needing treatment for primary or acquired resistance to epidermal growth factor receptor (EGFR) inhibitors of the cancer with deregulated EGFR; and providing the subject with a therapeutically effective amount of a chromosome region maintenance 1 (CRM1) inhibitor and an inhibitor of EGFR in an amount sufficient to reduce or eliminate the cancer.
Abstract: A pharmaceutical composition comprising lidocaine N-oxide (LNO), or a pharmaceutically acceptable salt thereof, for use in a method of treatment, said method being a prophylactic treatment to prevent, or decrease the likelihood of, sudden cardiac death associated with ventricular fibrillation (VF) in a subject, whereby the composition is provided to the subject's bloodstream via the oral mucous membrane or via pulmonary absorption in the lungs or by IV administration.
Abstract: Formulations of tegavivint and related compounds, methods of making such formulations and methods of treating various conditions utilizing such formulations.
Type:
Grant
Filed:
May 31, 2019
Date of Patent:
March 8, 2022
Inventors:
Steven David Dykstra, Henry Havel, Stephen Horrigan, Roger Harrison, Jeffrey Larson, Jonathan Northrup, Theodore Laslo, Garry Gwozdz
Abstract: Improved methods of causing vasodilation in a human subject are disclosed. In one implementation, the human subject is administered a dose of a nitrate salt of arginine, norvaline, or ornithine, wherein the dose of the nitrate salt of the amino acid in moles of the amino acid is less than a molar amount of the amino acid needed to cause vasodilation in the human subject. In another implementation, the human subject is administered a composition comprising a dose of a nitrate salt and an amount of an amino acid, wherein the dose of the nitrate salt in the composition in moles of the nitrate salt is less than a molar amount of the nitrate salt that needs be administered alone in order to induce vasodilation in the human subject. The amino acid in the composition is selected from the group consisting of: arginine, citrulline, creatine, glutamine, leucine, norvaline, and ornithine.
Abstract: A tumescent composition including a cannabinoid dissolved in a tumescent solution, wherein the tumescent solution includes a local anesthetic; a vasoconstrictor; and a pharmaceutically acceptable carrier, wherein a tumescent concentration of the cannabinoid is 1-2000 ?g/kg and is simultaneously: below a threshold for local, subcutaneous tissue toxicity, above a threshold for positive local therapeutic effect, and above a concentration safely achievable by intravenous (IV), intramuscular (IM) or oral (PO) delivery. Also disclosed are methods of subcutaneous delivery of a cannabinoid to a subject including administering to the subject the tumescent composition.
Abstract: Compositions are described including a combination of hydroxytyrosol and 3-O-acetyl-11-keto-?-boswellic acid. The hydroxytyrosol may be sourced from an olive extract and the 3-O-acetyl-11-keto-?-boswellic acid may be sourced from a Boswellia serrata extract. The compositions may be formulated for oral administration to a mammalian or an avian subject. Methods for preventing or reducing an inflammatory response in connective tissue are provided, the methods comprising orally administering the compositions to a subject in need thereof.
Abstract: The invention relates to pharmaceutical compositions comprising a statin and a cannabinoid, and their use for the treatment of hypercholesterolemia and atherosclerosis. It has been found that compositions combining a statin and a cannabinoid are improved over existing statin formulations. The compositions of the invention for example allow for a lower effective dose of statin and a reduction of the adverse effects seen with statins taken alone. Dosing ranges and formulations suitable for oral, buccal, and sublingual administration are disclosed. Various specific cannabinoids such as cannabidiol and synthetic cannabidiols selected for their anti-inflammatory, antioxidant, and anti-atherosclerotic effect are shown to be particularly advantageous.
Abstract: The present invention relates to a solid dispersion containing a compound represented by General Formula (I): wherein R1 is an unsubstituted phenyl group or a phenyl group substituted with a substituent; the substituent is an alkyl group having 1 to 8 carbon atoms, an alkyl group having 1 to 8 carbon atoms substituted with a halogen atom, an alkoxy group having 1 to 8 carbon atoms, an alkoxycarbonyl group having 2 to 8 carbon atoms, a formyl group, a carboxyl group, a halogen atom, a phenyl group or a phenoxy group; R2 is a cyano group or a nitro group; R3 is a hydroxyl group; X is an oxygen atom or —S(O)n—; n is an integer of 0 to 2; Y is an oxygen atom or a sulfur atom, or a pharmaceutically acceptable salt thereof and a hypromellose derivative.
Type:
Grant
Filed:
November 28, 2018
Date of Patent:
February 1, 2022
Assignees:
Shizuoka Prefectural University Corporation, Nippon Chemiphar Co., Ltd.
Abstract: The present invention provides compounds of formula (I), wherein: R1 is unsubstituted C1-C6 alkyl; La is substituted or unsubstituted C1-C6 alkyl linker, substituted or unsubstituted C3-C10 carbocycle, substituted or unsubstituted heterocycle comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S, or substituted or unsubstituted heteroaryl comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S; and R2 and R3 are each, independently, H, substituted or unsubstituted C1-C6 alkyl, or substituted or unsubstituted C6-C10 aryl; or alternatively, R2 and R3, together with the nitrogen atom to which they are attached, form a substituted or unsubstituted heteroaryl comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S or a substituted or unsubstituted heterocycle comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S.
Type:
Grant
Filed:
August 7, 2020
Date of Patent:
January 25, 2022
Assignee:
Alkermes Pharma Ireland Limited
Inventors:
Tarek A. Zeidan, Scott Duncan, Christopher P. Hencken, Thomas Andrew Wynn, Carlos N. Sanrame
Abstract: A pharmaceutical composition is provided for the treatment of systemic infections as well as colonic diseases. The composition comprises a therapeutically effective amount of rifaximin and a therapeutically effective amount of at least one alkaloid or derivative thereof. Methods and kits are also provided.
Abstract: Analogs of (4aS,6R,8aS)-5,6,9,10,11,12-hexahydro-3-methoxy-11-methyl-4aH-[1]benzofuro[3a,3,2-ef][2]benzazepin-6-ol of the formula: wherein R1 carbamate, carbonate or carboxlate group; R2 is alkoxy group of from one to six carbon atoms, a hydroxy group, hydrogen, an alkanoyloxy group or 2 to 10 carbon atoms, a benzoyloxy or substituted benzoyloxy group, a carbonate group of 1 to 10 carbon atoms or a carbamate group such as a mono alkyl or dialkyl or an aryl carbamate wherein the alkyl groups or aryl groups contain from 1 to 10 carbons; and R3 is hydrogen, alkyl of 1 to 10 carbon atoms, benzyl, cyclopropylmethyl group or a substituted or unsubstituted benzoyloxy group are of use in treating persons meeting criteria for having a risk of developing Alzheimer's type dementia, before symptoms of dementia are observed by reducing the decline of A? amyloid CSF.
Abstract: Provided herein, inter alia, are compounds and methods useful for modulating the translational effects of eIF2? phosphorylation, the Integrated Stress Response (ISR), and the unfolded protein response (UPR); for treating diseases; for increasing protein production, and for improving long-term memory.
Type:
Grant
Filed:
May 21, 2019
Date of Patent:
January 11, 2022
Assignee:
THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
Inventors:
Peter Walter, Carmela Sidrauski, Diego Acosta Alvear, Michelle R. Arkin, Christopher G. Wilson, Kean Hooi Ang, Brian R. Hearn, Punitha Vedantham, Adam R. Renslo, Mervyn Maze, Susana Vacas
Abstract: The inventive subject matter provides ready-to-administer, preferably anti-oxidant free, epinephrine compositions with improved stability, and methods for preparing the same. Contemplated compositions can be packaged using blow-fill-seal technology or packaged into flexible IV bags and maintain degradation of the epinephrine at a level of less than 5 wt % when stored over at least one months at between 2-40° C.
Type:
Grant
Filed:
March 17, 2020
Date of Patent:
December 28, 2021
Assignee:
Nevakar Injectables Inc.
Inventors:
Prem Sagar Akasapu, Kumaresh Soppimath, Reema Ajitkumar Puri, Iouri V. Ilitchev, Milan Patel, Pooja H. Tendulkar
Abstract: The present invention relates to liquid pharmaceutical composition suitable for oral administration comprising clonidine or pharmaceutically acceptable salts thereof with at least one buffer and at least one preservative. The present invention also relates to process for preparing the said liquid pharmaceutical composition.
Abstract: Provided are methods of using curcuphenol compounds to increase expression of major histocompatibility complex class I (MHC-I) antigen in cells, particularly on the surface of diseased cells such as cancer cells, and thereby increase the immunogenicity of the cells. Also provided are pharmaceutical compositions that comprise curcuphenol compounds and methods of use thereof, for instance, to treat various cancers, alone or in combination with other therapies.
Type:
Grant
Filed:
August 20, 2020
Date of Patent:
December 14, 2021
Assignee:
Cava Healthcare Inc.
Inventors:
Wilfred Jefferies, Reinhard Gabathuler, Raymond Andersen, Lilian Nohara, David Williams
Abstract: Pharmaceutical compositions of the invention include substituted riluzole pro drugs useful for the treatment of amyotrophic lateral sclerosis (ALS) and related disorders through the release of riluzole, especially to avoid patient to patient variability in first pass, hepatic metabolism promoted by Cyp 1?2. Pro-drugs of riluzole have enhanced stability to hepatic metabolism and are delivered into systemic circulation by oral administration, and then cleaved to release riluzole in the plasma via either an enzymatic or general biophysical release process. The invention further includes pro-drugs of riluzole useful for the treatment of disease states that can be treated with riluzole through the release of riluzole from a pro-drug agent.
Type:
Grant
Filed:
July 22, 2019
Date of Patent:
December 14, 2021
Assignee:
Biohaven Pharmaceutical Holding Company Limited
Abstract: A method for treating a disease or disorder in a patient who is currently taking a cytochrome P450 inhibitor comprising administering to the patient a dose of pimavanserin or a pharmaceutical acceptable salt thereof, wherein the dose is at least 20% lower than a dose of pimavanserin or a pharmaceutical acceptable salt thereof that would otherwise have been recommended to the patient if the patient were not currently taking the cytochrome P450 inhibitor.
Abstract: Methods for treating and/or preventing periodontal disease with arginine silicate are disclosed. Methods may include the steps of identifying an individual in need of treatment for, or in need of prevention of, periodontal disease and administering an effective amount of an arginine-silicate complex to said individual. Arginine silicate may also be used to ameliorate one or more symptoms of periodontal disease. In some aspects, arginine silicate may be used to restore gum health and/or stop or reverse recession of the gums and/or the loss of gum tissue in the oral cavity.