Abstract: Provided herein are antibacterial compounds, wherein the compounds in some embodiments have broad spectrum bioactivity. In various embodiments, the compounds act by inhibition of bacterial type 1 signal peptidases SpsB and/or LepB, an essential protein in bacteria. Pharmaceutical compositions and methods for treatment using the compounds described herein are also provided.
Type:
Grant
Filed:
May 27, 2020
Date of Patent:
December 28, 2021
Assignee:
Genentech, Inc.
Inventors:
Michael F. T. Koehler, Peter Andrew Smith, Dana Winter, Boubacar Sow, Claudio Sturino, Guillaume Pelletier, Jonathan Boudreault
Abstract: A preserved liquid aqueous pharmaceutical composition includes one or more etherified cyclodextrin derivatives, at least one water-soluble preservative, and at least one pharmaceutically active compound which is poorly water-soluble, very poorly water-soluble or water-insoluble. The liquid aqueous pharmaceutical composition provides an acceptable solubility of the pharmaceutically active compound, such as pimobendan, in aqueous solution whereby the water-soluble preservatives retain their effectiveness in the presence of the etherified cyclodextrin derivatives allowing the use in an oral administration form.
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: The present invention relates to a pharmaceutical combination comprising LSZ102 and ribociclib; pharmaceutical compositions comprising the same; and methods of using such combinations and compositions in the treatment or prevention of conditions in which degradation of estrogen receptors combined with CDK4/6 inhibition is beneficial in, for example, the treatment of cancers.
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 8, 2017
Date of Patent:
November 9, 2021
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: An injectable hyaluronic acid composition including a hyaluronic acid; a local anesthetic selected from the group of amide and ester type local anesthetics or a combination thereof; and an ascorbic acid derivative in an amount which prevents or reduces the effect on the viscosity and/or elastic modulus G? of the composition caused by the local anesthetic upon sterilization by heat. Further, the medical and non-medical, such as cosmetic, use of such a composition, and to a method of manufacturing such a composition.
Abstract: Described herein are uses of the CB1 inhibitors (e.g., antagonists, neutral antagonists, inverse agonists) and various methods of using and administering a CB1 inhibitor to a patient, especially patients showing symptoms of drug overdose or suspected of a drug overdose. Further described herein are uses wherein the CB1 inhibitor is ANEB-001. Further described herein are treatments with a CB1 inhibitor for THC or synthetic cannabinoid overdose.
Type:
Grant
Filed:
November 20, 2020
Date of Patent:
October 12, 2021
Assignee:
ANEBULO PHARMACEUTICALS, INC.
Inventors:
Joseph Fenton Lawler, Daniel Pawel Schneeberger
Abstract: The present invention relates to a pharmaceutical composition for preventing or treating AIDS, comprising a rhodanine derivative and a nucleoside reverse transcriptase inhibitor. A complex composition of the present invention exhibits a synergistic effect in terms of anti-HIV activity as compared with a case where each of the compounds is used as a single drug. Thus, the composition provides sufficient anti-HIV activity and exhibits an excellent effect of decreasing side effects such as toxicity even in a case where each compound is administered in a small amount. Accordingly, the present invention is expected to greatly contribute to treatment of AIDS patients.
Type:
Grant
Filed:
September 17, 2020
Date of Patent:
October 12, 2021
Assignee:
AVIXGEN INC.
Inventors:
Min Jung Kim, Jun Sub Choi, Hye Cheong Koo, Yi Yong Baek
Abstract: Dosage forms, drug delivery systems, and methods related to sustained release of dextromethorphan or improved therapeutic effects are disclosed. Typically, bupropion or a related compound is orally administered to a human being to be treated with, or being treated with, dextromethorphan.
Abstract: Dosage forms, drug delivery systems, and methods related to sustained release of dextromethorphan or improved therapeutic effects are disclosed. Typically, bupropion or a related compound is orally administered to a human being to be treated with, or being treated with, dextromethorphan.
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: Dosage forms, drug delivery systems, and methods related to sustained release of dextromethorphan or improved therapeutic effects are disclosed. Typically, bupropion or a related compound is orally administered to a human being to be treated with, or being treated with, dextromethorphan.
Abstract: Disclosed herein are compositions comprising fixed doses of ETC-1002 and one or more statins. Also disclosed herein are methods for using fixed doses of ETC-1002 and one or more statins. Uses include methods of treating cardiovascular disease or reducing the risk of cardiovascular disease in a subject. Uses also include methods of treating hypercholesterolemia in a subject.
Type:
Grant
Filed:
March 16, 2016
Date of Patent:
September 14, 2021
Inventors:
Roger Schofield Newton, Noah Laban Rosenberg, Diane Elaine MacDougall
Abstract: The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula I: or a pharmaceutically acceptable salt, wherein the variables are as devined herein. Moreover, The compounds of this invention have formula I-A: or a pharmaceutically acceptable salt, wherein the variables are as defined herein.
Type:
Grant
Filed:
August 6, 2019
Date of Patent:
September 14, 2021
Assignee:
VERTEX PHARMACEUTICALS INCORPORATED
Inventors:
Nadia Ahmad, Dean Boyall, Jean-Damien Charrier, Chris Davis, Rebecca Davis, Steven Durrant, Gorka Etxebarria I Jardi, Damien Fraysse, Juan-Miguel Jimenez, David Kay, Ronald Knegtel, Donald Middleton, Michael O'Donnell, Maninder Panesar, Francoise Pierard, Joanne Pinder, David Shaw, Pierre-Henri Storck, John Studley, Heather Twin
Abstract: The present invention provides compositions and methods for delivery of therapeutic agents across an barrier. The compositions include a therapeutic agent (e.g., antimicrobial agent, antibiotic, or anesthetic agent), a permeation enhancer which increases the flux of the therapeutic agent across the barrier, and a matrix forming agent. The matrix forming agent forms a gel at a suitable gelation temperature and rheological properties for use in drug delivery, and in some cases, the gelation temperature and rheological properties are not significantly changed from those of the composition without the permeation enhancer. The invention also provides a matrix forming agent and compositions thereof. Such compositions are particularly useful in the treatment of otitis media. Methods of treatment, methods of delivery, and kits for the compositions described herein are also provided.
Type:
Grant
Filed:
August 5, 2016
Date of Patent:
September 7, 2021
Assignees:
Children's Medical Center Corporation, Massachusetts Institute of Technology
Inventors:
Daniel S. Kohane, Rong Yang, Lily Yun Lin
Abstract: Pharmaceutical compositions for co-administering estradiol and progesterone to a human subject in need thereof are provided. In some embodiments, the pharmaceutical composition comprises solubilized estradiol, suspended progesterone, and a solubilizing agent comprising a medium chain (C6-C12) oil.
Type:
Grant
Filed:
May 27, 2020
Date of Patent:
August 31, 2021
Assignee:
TherapeuticsMD
Inventors:
Brian A. Bernick, Peter H. R. Persicaner, Julia M. Amadio
Abstract: The present disclosure is directed to compositions comprising oxymetazoline and methods of stabilizing oxymetazoline compositions for long term storage.
Abstract: The present invention includes a novel method of treating or preventing a disease or disorder associated with low levels of branched N-glycans in a subject in need thereof, the method comprising administering to the subject an effective amount of a compound of the invention. In one embodiment, the subject is further administered at least one additional therapeutic agent.
Type:
Grant
Filed:
April 23, 2015
Date of Patent:
August 31, 2021
Assignee:
THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
Inventors:
Michael Demetriou, James Dennis, Ani Oganesyan