Abstract: It is disclosed a compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof: wherein R1 is a linear alkyl group of 3 or 5 carbon atoms, and R2 is: and a pharmaceutical composition comprising the same, for use in the treatment of a disease whose treatment benefits from inhibiting or reducing Notch1 expression levels in cells, and/or benefits from inhibiting or reducing Notch1 levels in cells, and/or benefits from inhibiting or reducing Notch1 signaling dependent proteins levels in cells. As a consequence, present invention also relates to said compound of formula (I), and to the pharmaceutical composition comprising the same, for use in suppressing cancer stem cells, as well as, for use in reducing solid tumor development, metastasis or chemo/radio-resistance, promoted by cancer stem cells.
Type:
Grant
Filed:
October 24, 2022
Date of Patent:
February 21, 2023
Inventors:
Jon Peñarando Sáez, Juan Diego Unciti Broceta, Eduardo Muñoz Blanco
Abstract: The present invention relates to a pharmaceutical composition for treatment of a disease or condition characterized by or associated with stimulation of both DPr2 and TPr signaling, said composition comprising an effective amount of a dual receptor antagonist of DPr2 for prostaglandin D2 and TPr for thromboxane A2 and a pharmaceutically acceptable carrier.
Abstract: Methods for treating prostate cancer, including advanced prostate cancer, in a subject in need thereof, include administering once-daily to the subject, at least 80 mg of N-(4-(1-(2,6-difluorobenzyl)-5-((dimethylamino)methyl)-3-(6-methoxy-3-pyridazinyl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl)phenyl)-N?-methoxyurea, or a corresponding amount of a pharmaceutically acceptable salt thereof.
Type:
Grant
Filed:
August 20, 2020
Date of Patent:
February 21, 2023
Assignees:
Myovant Sciences GmbH, Takeda Pharmaceutical Company Limited
Inventors:
Vijaykumar Reddy Rajasekhar, Brendan Mark Johnson, David B. MacLean, Lynn Seely, Paul N. Mudd, Jr.
Abstract: The present disclosure provides methods of identifying patients who have partial or total resistance to HIF-2 inhibitors or who develop partial or total resistance to HIF-2 inhibitors after treatment and providing suitable treatment to these patients.
Type:
Grant
Filed:
September 23, 2020
Date of Patent:
February 14, 2023
Assignee:
THE BOARD OF REGENTS OF THE UNIVERSITY OF TEXAS SYSTEM
Inventors:
James B. Brugarolas, Haley Hill, Tao Wang
Abstract: Sarcomas are rare malignant tumors arising from the mesenchymal tissues at all body sites. The inventors show that in a mouse model of p16/p19 deficiency prone to tumor development, the absence of the mouse pantetheinase Vnn1 enhances the frequency of aggressive fibrosarcomas. They also show that reintroduction of a catalytically active form of the Vnn1 pantetheinase limits tumor growth in vivo. Interestingly, VNN1 expression in human sarcomas is associated with reduced aggressiveness and lower risk of metastatic relapse in patients. In conclusion, Vnn1 represents a novel marker of sarcoma and may modulate tumor aggressiveness by sustaining myofibroblast cell differentiation, thereby limiting evolution towards undifferentiated tumors. The present invention relates to the use of Vnn1 as a biomarker and a therapeutic target in sarcomas.
Type:
Grant
Filed:
September 25, 2018
Date of Patent:
February 14, 2023
Assignees:
INSERM (Institut National de la Santé et de la Recherche Médicale), Université d'Aix Marseille, Centre National de la Recherche Scientifique (CNRS), Université Claude Bernard, Centre Leon Bernard
Abstract: The present disclosure provides industrially scalable methods of making (Z)-endoxifen or a salt thereof, crystalline forms of endoxifin, and compositions comprising them. The present disclosure also provides methods for treating hormone-dependent breast and hormone-dependent reproductive tract disorders.
Type:
Grant
Filed:
January 20, 2022
Date of Patent:
February 7, 2023
Assignee:
ATOSSA THERAPEUTICS, INC.
Inventors:
Steven C. Quay, Yao-Lin Sun, LungHu Wang, ChangJung Wu, ChuanDer Huang
Abstract: It is provided a catechol-O-methyltransferase (COMT) inhibitor for use in the prevention and/or treatment of transthyretin-associated amyloidosis. It is also provided a catechol-O-methyltransferase (COMT) inhibitor for use in the prevention and/or treatment of transthyretin-associated amyloidosis in combination therapy with another COMT inhibitor, a benzoxazole derivative, iododiflunisal, diflunisal, resveratrol, tauroursodeoxycholic acid, doxocycline, or epigallocatechin-3-gallate.
Abstract: An extended duration anesthetic includes a short duration local anesthetic in a dilute solution and a long duration local anesthetic. The long duration local anesthetic is maintained in a powdered form until the time of administration. Premeasured quantities of the dilute solution and powdered long duration local anesthetic in a kit allow for quick preparation of a solution with desired concentrations of both short duration local anesthetic and long duration local anesthetic at the time of administration.
Type:
Grant
Filed:
September 16, 2020
Date of Patent:
January 31, 2023
Assignee:
Ventis Pharma
Inventors:
Jeremy Poulsen, Louis Stanfield, Lawrence Volz
Abstract: The present invention relates to the field of cancer therapy. Specifically, provided are methods of treating cancer, for example, peripheral T-cell lymphoma (“PTCL”), with a farnesyltransferase inhibitor (FTI) that include determining whether the subject is likely to be responsive to the FTI treatment based on gene expression characteristics.
Type:
Grant
Filed:
February 21, 2018
Date of Patent:
January 3, 2023
Assignee:
Kura Oncology, Inc.
Inventors:
Antonio Gualberto, Catherine Rose Scholz
Abstract: Disclosed are methods for the removal of plaques containing amyloid beta, protecting the brain from amyloid beta toxicity, and restoring neurological function by the expansion of neural stem cell pools and improving mitochondrial health.
Abstract: The present invention includes methods for treating TRKA, TRKB, and/or TRKC driven proliferative disorder in a subject comprising administering to the subject a therapeutically effective amount of crenolanib, wherein the subject has a proliferative disorder with overexpression, activation, amplification, or mutation of TRKA, TRKB, and/or TRKC kinase.
Abstract: The disclosure provides compounds with warheads and their use in treating medical diseases or disorders, such as viral infections. Pharmaceutical compositions and methods of making various compounds with warheads are provided. The compounds are contemplated to inhibit proteases, such as the 3C, CL- or 3CL-like protease.
Type:
Grant
Filed:
November 12, 2021
Date of Patent:
December 13, 2022
Assignee:
Pardes Biosciences, Inc.
Inventors:
Lee D. Arnold, Andy Jennings, Walter Keung
Abstract: The invention concerns gene signatures obtained from microvesicles and a method of applying these gene signatures in helping to determine a biological condition. The determination of a biological condition may aid, for example, the diagnosis, prognosis, and therapy treatment selection for disease in a subject.
Type:
Grant
Filed:
July 23, 2019
Date of Patent:
December 6, 2022
Assignee:
THE GENERAL HOSPITAL CORPORATION
Inventors:
Mikkel Noerholm, Johan Karl Olov Skog, Xandra O. Breakefield, Bob Carter
Abstract: A formulation, including: (a) a first medicament, wherein the first medicament includes an isothiocyanate functional compound/surfactant; and (b) a second medicament, wherein the second medicament includes an antineoplastic agent, such as a cytotoxic antineoplastic agent and/or a targeted antineoplastic agent.
Abstract: The present invention relates to a crystalline form of Compound I, a salt, a solvate, or a solvate salt thereof or an amorphous form of Compound I, a salt, a solvate, or a solvate salt thereof. The present invention also provides compositions comprising the crystalline form and/or the amorphous form, therapeutic uses of the crystalline forms and/or the amorphous forms, and the compositions thereof.
Abstract: This disclosure relates to new compositions and methods for making cannabinoid formulations. In one embodiment, this disclosure provides water soluble compositions comprising a first purified cannabinoid and Vitamin E TPGS. In one embodiment, the disclosure herein comprises a method of making powders comprising heatings material to a first temperature and a second temperature.
Abstract: The presently claimed invention is related to compositions and methods for treating H2S related diseases comprising administering a pharmacologically effective amount of pharmaceutical composition containing a first therapeutic, wherein the first therapeutic includes one of an ATR kinase inhibitor and an ATR kinase promotor. According to further embodiments the H2S related disease is one of cancer, cardiovascular disease, acute inflammation, chronic inflammation, and neurological disease.
Type:
Grant
Filed:
November 13, 2019
Date of Patent:
November 29, 2022
Assignee:
Board of Supervisors of Louisiana
State University
Inventors:
Christopher G. Kevil, Rodney Shackelford
Abstract: Provided herein are therapeutic methods, kits, and pharmaceutical compositions for protecting a subject from radiation using a therapeutic agent selected from the group consisting of RRx-OO1 and a pharmaceutically acceptable salt thereof. One exemplary therapeutic method involves administering RRx-OO1 to the subject prior to the subject being exposed to the radiation, in order to protect the subject against radiation, such as ionizing radiation containing ?-rays, ?-rays, ?-rays, neutron radiation, or a combination thereof.
Type:
Grant
Filed:
January 8, 2019
Date of Patent:
November 29, 2022
Assignee:
EpicentRx, Inc.
Inventors:
Bryan T. Oronsky, Arnold Oronsky, Tony R. Reid
Abstract: Provided herein are methods for predicting chemotherapy benefit. The invention predicts chemotherapy benefit based on the expression analysis of biomarkers, e.g., RNA biomarker transcription analysis, taken from a tumor sample. The biomarker expression data can be combined with clinical variables, e.g., tumor size and nodal status, to generate a profile that predicts the benefit of including chemotherapy as a treatment decision.
Type:
Grant
Filed:
March 4, 2020
Date of Patent:
November 22, 2022
Assignee:
MYRIAD GENETICS, INC.
Inventors:
Alexander Gutin, Julia Reid, Ralf Kronenwett, Marsel Scheer