Abstract: The present intervention identifies the antiglycating inhibitors from a series of carbazole-linked 1,2,3 triazole derivatives through in vitro MGO-mediated glycating BSA model. Derivatives 12, and 13 established a remarkable antiglycation activity at the receptor level in human monocytes. These compounds were found non-toxic, and possess the potential to halt AGE-RAGE/ROS-mediated NF-kB-dependent COX-2, and its proinflammatory product, PGE2, production in monocytes. Hence, carbazole-linked 1,2,3 triazole derivatives provide treatment modalities to delay or prevent the onset of late diabetic micro- and macro-vascular complications in diabetic patients.
Type:
Grant
Filed:
August 20, 2021
Date of Patent:
March 12, 2024
Inventors:
Humera Jahan, Mohammad Iqbal Choudhary, Nimra Naz Siddiqui, Fatima Z. Basha, Shazia Iqbal
Abstract: This patent document relates to the crystalline forms of a quinazoline compound and the hydrochloride salts thereof. More particularly, this patent document relates to a preparation method of the crystalline forms of 1-(4-(4-(3,4-dichloro-2-fluorophenylamino)-7-methoxyquinazolin-6-yloxy)piperidin-1-yl)prop-2-en-1-one and its hydrochloride salts.
Type:
Grant
Filed:
September 12, 2019
Date of Patent:
January 30, 2024
Assignees:
Hanmi Pharmaceutical Co., Ltd., Spectrum Pharmaceuticals, Inc.
Inventors:
Jong Ouk Baek, Hee Cheol Kim, Tae Hee Ha, Kweehyun Suh, Guru Reddy
Abstract: To provide a medicament for safely treating a patient in need of treatment with pemafibrate, a salt thereof, or a solvate of any of these (hereinafter also referred to as pemafibrate therapy). A medicament for treating a patient in need of pemafibrate therapy, the medicament comprising the step of avoiding or suspending concomitant use of pemafibrate, a salt thereof, or a solvate of any of these as an active ingredient in order to suppress an increase in plasma concentration of pemafibrate when the treatment is combined with a medicament containing an OATP1B inhibitor, or the step of reducing the dose of pemafibrate, a salt thereof, or a solvate of any of these.
Abstract: The present invention provides oral solutions containing sotalol hydrochloride which advantageously avoid swallowing while providing with improved stability. The present invention also relates to methods of using the oral solutions for treatment of diseases and disorders, such as delay in reoccurrence of atrial fibrillation/atrial flutter and/or ventricular arrhythmias.
Abstract: A method is provided for identifying a patient having a respiratory illness and administering to the patient a combination of an anti-inflammatory agent and a leukotriene inhibitor. The method may include treating respiratory illness associated with a coronavirus, and may it may further include reducing or preventing an inflammatory response or cytokine storm for those patients without impairing their immune response against the underlying pathogen.
Abstract: Disclosed are bruceolides for the treatment of cancer, and other diseases, selectively targeting unwanted cells. The disclosed bruceolides may include a site specific cleavable moiety inhibiting the chemotoxic activity until cleaved, i.e., removed, within and/or near a cancer to be treated. As to facilitate selective delivery to cancer tumors, the disclosed bruceolides may be loaded into, attached to or otherwise carried by nanoparticles.
Abstract: Provided are a pharmaceutical composition for preventing or treating inflammatory disease, autoimmune disease, graft rejection responses, or combinations thereof, the pharmaceutical composition including a compound represented by Formula 1, or a stereoisomer, derivative, solvate, or pharmaceutically acceptable salt thereof, and a method using the pharmaceutical composition. The pharmaceutical composition and the method can be used to effectively prevent or treat inflammatory disease, autoimmune disease, graft rejection responses, or combinations thereof.
Type:
Grant
Filed:
December 18, 2020
Date of Patent:
November 28, 2023
Assignees:
INDUSTRY-ACADEMIC COOPERATION FOUNDATION, YONSEI UNIVERSITY, IMMUNOMET THERAPEUTICS INC.
Inventors:
Jungsik Song, Beom Seok Kim, Sang Jun Ha, Ji Min Son
Abstract: [Problem] To provide a composition for external skin use that has anti-inflammatory and antiallergic activity, and is very safe. [Solution] A composition for external skin use for inflammatory diseases contains dihomo-gamma-linolenic acid (DGLA) as the active ingredient thereof. It is preferable for the DGLA to be present as a glyceride, a phospholipid, or an alkyl ester. The amount of DGLA contained in the composition for external use is 0.1-50 wt %.
Abstract: This invention relates to compounds, pharmaceutical compositions comprising them, and methods of using the compounds and compositions for treating diseases related to translesion synthesis (TLS) pathway. More particularly, this disclosure relates to small molecule inhibitors of TLS, methods of inhibiting TLS pathway with these compounds, and methods of treating diseases related to the TLS pathway.
Abstract: The present invention concerns the compound aprocitentan, {5-(4-bromo-phenyl)-6-[2-(5-bromo-pyrimidin-2-yloxy)-ethoxy]-pyrimidin-4-yl}-sulfamide, and its use as endothelin receptor antagonist, in combination with other active ingredients or therapeutic agents including an angiotenin receptor blocker, and/or a calcium channel blocker, and preferably a diuretic which is a thiazide-like diuretic, in the prophylaxis or treatment of certain endothelin related diseases. The invention further relates to pharmaceutical compositions comprising aprocitentan in combination with said other active ingredients or therapeutic agents. The invention further relates to such pharmaceutical compositions comprising novel crystalline forms of aprocitentan.
Type:
Grant
Filed:
September 10, 2021
Date of Patent:
October 17, 2023
Assignee:
Idorsia Pharmaceuticals Ltd
Inventors:
Marc Bellet, Martin Bolli, Martine Clozel, Marc Iglarz
Abstract: The disclosure provides compositions comprising amino acids, individually and in combination, and methods of making the compositions and methods of using the compositions as pharmaceutically active agents to, inter alia, treat disease in animals, including humans.
Type:
Grant
Filed:
June 3, 2022
Date of Patent:
October 10, 2023
Assignee:
The Regents of the University of California
Abstract: Provided herein are compositions, systems, and methods for causing weight loss and treating and/or preventing a disease or condition, such as obesity, diabetes, and cancer, with an agent or procedure that inhibits the TMA/FMO3/TMAO pathway in a subject.
Abstract: Disclosed are methods for treating a myelodyspastic syndrome (MDS) and/or an acute myeloid leukemia (AML) in an individual in need thereof. Further disclosed are compositions for use in the disclosed methods, used for treating a myelodyspastic syndrome (MDS) and/or an acute myeloid leukemia (AML) in an individual in need thereof.
Type:
Grant
Filed:
November 21, 2022
Date of Patent:
September 12, 2023
Inventors:
Daniel Starczynowski, William Seibel, Laura Barreyro
Abstract: Diagnostic methods for identifying cancer bearing subjects appropriate for treatment with CPX-351 include genetic and ex vivo testing of cells from a candidate subject. Combination treatment with CPX-351 and FLT-3 inhibitors improve CPX-351 uptake and toxicity.
Type:
Grant
Filed:
February 11, 2021
Date of Patent:
September 5, 2023
Assignees:
CELATOR PHARMACEUTICALS, INC., OREGON HEALTH & SCIENCE UNIVERSITY
Inventors:
Max Gordon, Paul Tardi, Jeffrey Tyner, Lawrence Mayer
Abstract: A compound represented by Formula 1 according to the present disclosure, when used in combination with an anticancer drug, may significantly improve the anticancer effect of the anticancer drug, and may induce the same anticancer effect even when the anticancer drug is used in a significantly smaller amount than the conventionally used amount, thereby reducing the side effects caused by administration of the anticancer drug. Furthermore, the compound represented by Formula 1 makes it possible to effectively prevent, alleviate or treat either anticancer-resistant cancer or cancer which recurs or metastasizes after anticancer drug treatment.
Abstract: Disclosed are compounds of formula (I), wherein X, Y, Z are annular atoms comprised in a five-membered carbocyclic or heterocyclic ring, selected from the group consisting of CH, NH, N, O, S; said carbocyclic or heterocyclic ring being optionally substituted with amino (C1-C4) linear or branched alkyl or guanidine or guanidino (C1-C4) linear or branched alkyl; with the proviso that the heterocycle ring is not furyl; n is 0 or 1; R is H or OH; the dotted line represents an optional double bond C?C; the thick line represents a bond in the ? configuration; the wavy line represents a bond both in the ? and ? configuration; their enantiomeric and/or diastereomeric mixtures, their pharmaceutically acceptable salts, their solvates, hydrates; their metabolite and metabolic precursors. The compounds of formula (I) are for use as medicaments, in particular for the treatment of acute or chronic heart failure. Oral administration is also possible.
Type:
Grant
Filed:
July 17, 2019
Date of Patent:
August 22, 2023
Assignee:
CVie Therapeutics Limited
Inventors:
Alberto Cerri, Giuseppe Bianchi, Patrizia Ferrari, Mara Ferrandi, Paolo Barassi, Antonio Zaza, Marcella Rocchetti, Carlotta Ronchi, Shih-Che Hsu
Abstract: This invention is in the area of improved compounds, compositions and methods of transiently protecting healthy cells, and in particular hematopoietic stem and progenitor cells (HSPC) as well as renal cells, from damage associated with DNA damaging chemotherapeutic agents. In one aspect, improved protection of healthy cells is disclosed using disclosed compounds that act as highly selective and short, transiently-acting cyclin-dependent kinase 4/6 (CDK 4/6) inhibitors when administered to subjects undergoing DNA damaging chemotherapeutic regimens for the treatment of proliferative disorders.
Type:
Grant
Filed:
April 5, 2021
Date of Patent:
August 8, 2023
Assignee:
G1 Therapeutics, Inc.
Inventors:
Jay Copeland Strum, John Emerson Bisi, Patrick Joseph Roberts, Francis Xavier Tavares
Abstract: The invention provides methods, compositions, and kits containing phentolamine for improving visual performance. In particular, the invention provides improvement in visual performance, such as improvement in visual acuity, by daily ophthalmic administration of a phentolamine solution to an eye of a patient at or near the bedtime of the patient for an extended duration while minimizing the occurrence of adverse side effects, such as eye redness during the patient's waking hours.
Abstract: Methods are disclosed for the mobilization of marrow infiltrating cells (MILs) using E-selectin antagonists for the treatment of disorders such as cancer. Methods for treating or preventing cancers using MILs mobilized by E-selectin antagonists are further disclosed.