Abstract: The invention relates to the combined use and to a combination of either a microtubule targeting agent or a Src kinase inhibitor, a Raf-MEK-ERK pathway inhibitor and an EGFR and/or ERBB2 inhibitor for use in the treatment of RAS-mutant cancer. The invention further relates to a method of treating RAS-mutant cancers and to a method of testing a combination comprising of a either microtubule targeting agent or a Src inhibitor, a Raf-MEK-ERK pathway inhibitor and an EGFR and/or ERBB2 inhibitor on a tumor organoid. In particular, the invention relates to the combined use of either a microtubule targeting agent or a Src kinase inhibitor with: an inhibitor of the Raf-MEK-ERK pathway and at least one of an inhibitor of both EGFR and ERBB2 and a combination of an EGFR inhibitor and an ERBB2 inhibitor in the treatment of RAS mutant cancer.
Type:
Application
Filed:
April 12, 2019
Publication date:
December 9, 2021
Applicant:
UMC Utrecht Holding B.V.
Inventors:
Hugo Johannes Gerhardus Snippert, Alexander Eduard Edgar Mertens, Carla Sofia Leiria Verissimo, Johannes Lukas Bos
Abstract: One embodiment of the invention provides a method for administering tasimelteon to a human patient that comprises orally administering an effective dose of tasimelteon under fasted conditions. Fasted conditions may comprise administering the tasimelteon without food, no food at least ½ hour prior to administration, no food at least 1 hour prior to administration, no food at least 1½ hours prior to administration, no food at least 2 hours prior to administration, no food at least 2½ hours prior to administration, or no food at least 3 hours prior to administration. According to such embodiments, tasimelteon may be administered, for example, at a dose of 20 mg/d. Tasimelteon may be administered where, for example, the patient is being treated for a circadian rhythm disorder or for a sleep disorder, including, for example, Non-24 Disorder.
Type:
Application
Filed:
August 20, 2021
Publication date:
December 9, 2021
Inventors:
Marlene Michelle Dressman, Mihael H. Polymeropoulos, Paolo Baroldi
Abstract: Provided is an antibacterial drug for an enterobacterium that causes an infection in humans, such as Clostridioides difficile. An antibacterial agent against an enterobacterium, comprising equol as an active ingredient.
Abstract: The invention provides compositions comprising at least one cannabinoid compound, for use in the method of treating and preventing a disease, condition or symptom caused by, or associated with fungi, bacteria and microbes.
Type:
Application
Filed:
October 30, 2019
Publication date:
December 9, 2021
Applicant:
Yissum Research Development Company of The Hebrew University of Jerusalem Ltd.
Abstract: A topical composition includes a cannabinoid, a terpenoid, and a skin penetration system that includes dimethyl sulfoxide (DMSO) and at least one compatibilizer. The composition may be in the form of an emulsion that further contains water and at least one fatty component. The composition can be used to reduce or eliminate pain by topical application to an affected region of the body. The composition provides localized pain relief by providing a focused quantity of cannabinoid in the region of the pain instead of distributing the cannabinoid systemically and/or delivering it to the brain or central nervous system.
Abstract: A novel chromane derivative, (3?-hydroxy-4?-ethoxybenzyl)-5,6,7-trimethoxy-2H-1-benzopyran (SH-17059 (1)) is disclosed herein. This chromane derivative has been found to inhibit blood vessel cell growth and proliferation, providing a promising treatment for ocular angiogenesis-mediated diseases.
Type:
Application
Filed:
April 29, 2019
Publication date:
December 9, 2021
Inventors:
Timothy W. Corson, Seung-Yong SEO, Bit Lee, Sianne SCHWIKKARO, Dulcie MULHOLLAND, Hannah WHITMORE
Abstract: The present invention is drawn to novel topiramate compositions as well as methods for effecting weight loss, e.g., in the treatment of obesity and related conditions, including conditions associated with and/or caused by obesity per se. The present invention features an escalating dosing regimen adapted for the administration of topiramate and optionally a sympathomimetic agent such as phentermine or bupropion, in the treatment of obesity and related conditions.
Type:
Application
Filed:
August 23, 2021
Publication date:
December 9, 2021
Inventors:
Thomas NAJARIAN, Peter Y. TAM, Leland F. WILSON
Abstract: Pharmaceutical compositions and kits including a tyrosine hydroxylase inhibitor; melanin, a melanin promoter, or a combination thereof; a p450 3A4 promoter; and a leucine aminopeptidase inhibitor are provided. Also provided are methods of treating cancer in a subject, comprising administering an effective amount of a tyrosine hydroxylase inhibitor, a melanin promoter, a p450 3A4 promoter, and a leucine aminopeptidase inhibitor to the subject in need thereof.
Abstract: Provided are a feed additive composition for cattle including N-acetyl-L-tryptophan (NALT) as an active ingredient, and more particularly, a feed additive composition including N-acetyl-L-tryptophan as an active ingredient for reducing temperature stress of cattle, increasing average daily gain of cattle, and increasing feed intake of cattle; a feed including the feed additive composition for cattle; and methods of reducing temperature stress of cattle, increasing average daily gain of cattle, and increasing feed intake of cattle, the methods including feeding the cattle with the feed additive composition or feed for cattle including N-acetyl-L-tryptophan as an active ingredient.
Type:
Application
Filed:
November 12, 2019
Publication date:
December 9, 2021
Inventors:
Jin Seung PARK, Jin Woo JEON, Jun Ok MOON, Joo Young LEE, Hong-Gu LEE, Jae-Sung LEE
Abstract: Therapeutics and methods of treating one of an angiotensin-converting enzyme 2 (ACE2) associated condition and an ACE2 associated pre-condition patient comprising administering to the patient a pharmaceutically therapeutic dose of a therapeutic, wherein the therapeutic includes either a Sigmar1 antagonist or any pharmaceutically acceptable salt, solvate, or prodrug thereof, or a Sigmar1 enhancer, or any pharmaceutically acceptable salt, solvate, or prodrug thereof. A method of treating coronavirus disease 2019 (COVID-19) patient comprising administering to the patient a pharmaceutically therapeutic dose of a therapeutic, wherein the therapeutic includes a Sigmar1 enhancer, or any pharmaceutically acceptable salt, solvate, or prodrug thereof.
Type:
Application
Filed:
June 7, 2021
Publication date:
December 9, 2021
Applicant:
Board of Supervisors of Louisiana State University and Agricultural and Mechanical College
Inventors:
Shenuarin BHUIYAN, Christopher KEVIL, Anthony Wayne ORR, Chowdhury S ABDULLAH, Richa Aishwarya
Abstract: Disclosed herein are novel drug combinations comprising a glutathione peroxidase (GPx) mimic compound and an antipsychotic agent, pharmaceutical compositions comprising one or more of such combinations, methods of preparing pharmaceutical compositions comprising one or more such combinations, and methods of treatment, prevention, inhibition or amelioration of one or more diseases associated with GPx mediated disorders, psychotic disorders or complications from administering an antipsychotic agent at high dose or long term using such combination or pharmaceutical compositions. Furthermore, a method is disclosed for reducing the antipsychotic agent's dosages that comprises co-administering a therapeutically effective amount of a glutathione peroxidase mimic compound.
Abstract: The present invention relates to a use to be used for the purpose of preventing, alleviating or treating diabetic peripheral neuropathy or chemotherapy-induced peripheral neuropathy by administering a pharmaceutical composition containing a carbamate compound of chemical formula 1.
Abstract: Provided herein is a method of treating, preventing, or ameliorating one or more symptoms of a glucokinase-mediated disorder, disease, or condition in a renally impaired subject with a glucokinase activator (GKA), for example, dorzagliatin. Also provided herein is a method of treating, preventing, or ameliorating one or more symptoms of a diabetes in a renally impaired subject with a GKA. Additionally, provided herein is a method of treating, preventing, or ameliorating one or more symptoms of a chronic kidney disease with a GKA.
Type:
Application
Filed:
June 3, 2021
Publication date:
December 9, 2021
Inventors:
Li CHEN, Shuang REN, Chengfeng JIAO, Yaohui WANG
Abstract: The present invention provides methods of treating malaria by administration of a compound of Formula (I): or a pharmaceutically acceptable salt of said compound, to a subject in need thereof, wherein the variables X, R1, R3, R4, R5, A, B, L, m and n are as defined herein. The invention also provides uses of the compounds of Formula (I), as defined herein, for inhibiting plasmepsin V activity, for treating a Plasmodium infection, and for treating malaria. Also provided are methods of treatment further comprising administration of one or more additional anti-malarial compounds.
Type:
Application
Filed:
August 11, 2021
Publication date:
December 9, 2021
Applicants:
Merck Sharp & Dohme Corp., The Walter and Eliza Hall Institute of Medical Research
Inventors:
Tanweer A. Khan, Jared N. Cumming, David B. Olsen, Justin A. Boddey, Alan F. Cowman, Brad E. Sleebs
Abstract: The present invention is directed to an improved method for preparing bisantrene, specifically bisantrene dihydrochloride, for intravenous administration, as well as to preparations of bisantrene dihydrochloride for intravenous administration. The present invention is also directed to methods for treatment of malignancies treatable by administration of bisantrene, which can include administration of additional anti-neoplastic agents, wherein the bisantrene is prepared by a method according to the present invention.
Abstract: The present invention relates to a pharmaceutical composition for preventing or treating cancer, a radiosensitizer composition for treating cancer, and a health functional food for preventing or improving cancer, which comprise N-1H-benzimidazol-2-yl-3-(1H-pyrrol-1-yl) benzamide, a derivative thereof, or a pharmaceutically acceptable salt thereof as an active ingredient. The pharmaceutical composition comprising N-1H-benzimidazol-2-yl-3-(1H-pyrrol-1-yl) benzamide or a derivative thereof as an active ingredient according to the present invention arrests the mitosis of cancer cells to prevent proliferation and at the same time, to exhibit low toxicity in normal cell lines and induce apoptosis only in cancer cell lines, so it can be used as an effective anticancer agent. In addition, the N-1H-benzimidazol-2-yl-3-(1H-pyrrol-1-yl) benzamide of the present invention can increase the sensitivity of the treated cancer cells to radiation, so it can be used as a radiosensitizer composition for cancer treatment.
Type:
Application
Filed:
September 3, 2019
Publication date:
December 9, 2021
Applicant:
KOREA INSTITUTE OF RADIOLOGICAL & MEDICAL SCIENCES
Inventors:
Jae Sung KIM, Ah Young KIM, Sang Gu HWANG, Jie Young SONG, Yi Na YOON
Abstract: The invention describes a long-acting composition comprising a spiro-azetidine isoxazoline of Formula (1) or (2) wherein R1a, R1b, R1c and R2 are as described herein, and stereoisomers thereof. The composition is a veterinary composition and also comprises a glycol ether and at least one veterinarily acceptable solvent, and optionally, at least one precipitation inhibitor, antioxidant and additional veterinary agent, and any mixture thereof. The invention also includes a method of treating an animal with a parasitic infestation by administering the long-acting composition to the animal in need thereof.
Type:
Application
Filed:
August 3, 2021
Publication date:
December 9, 2021
Inventors:
Guy Francis de Rose, Nathan Anthony Logan Chubb, Patrick F. M. Meeus, Tom L. McTier
Abstract: The present invention relates to method of modulating TIGIT signaling pathway and PD-1 signaling pathway. The invention also encompasses the use of the compound of formula (I) or a stereoisomer thereof or a pharmaceutically acceptable salt thereof for the treatment of diseases or disorders mediated by both TIGIT signaling pathway and PD-1 signaling pathway.
Abstract: Disclosed herein are pharmaceutical compositions for the treatment of cytokine storm syndrome, and methods of administering such compositions for the treatment of acute respiratory distress syndrome, and the prevention of multiple organ failure in patients with cytokine storm syndrome and/or acute respiratory distress syndrome, comprising an effective amount of one or more mTor inhibitors.
Abstract: The present invention includes methods and compositions for preventing, ameliorating, and treating certain skin disorders caused due to UV-induced, age-related, and post-inflammatory cutaneous changes. The skin disorders include, in non-limiting examples, static wrinkles, fine wrinkles, loss of skin tone, ephelides, melasma, senile purpura, UV-damage to the skin, static rhytides, prominent hand veins, field cancerization of epithelium such as in squamous cell carcinoma in situ, keloids, and imbalance in ratio of collagen isoforms. In certain embodiments, the compositions useful within the invention comprise a therapeutically effective amount of a rapamycin and a dermatologically acceptable carrier.
Type:
Application
Filed:
October 10, 2019
Publication date:
December 9, 2021
Inventors:
Christina L. Chung, Christian Sell, Ibiyonu O. Lawrence
Abstract: Disclosed herein are pharmaceutical compositions to treat, prevent, reduce the incidence of, or reduce the severity of hepatic steatosis comprising an effective amount of one or more mTOR inhibitors and optionally an effective amount of one or more thyroid hormones. Further disclosed herein are methods of treating, preventing, reducing the incidence of, or reducing the severity of hepatic steatosis comprising administering an effective amount of a pharmaceutical composition of one or more mTOR inhibitors and optionally an effective amount of one or more thyroid hormones.
Abstract: Formulations for treating depressive disorders and methods for treating depressive disorders using gaboxadol or a pharmaceutically acceptable salt thereof are provided.
Abstract: The application provides methods for the treatment of migraine for patients that are poor responders to triptan treatments. Some embodiments provide methods for treating or reducing migraine in patients that do not adequately respond to triptan treatments comprising the step of administering an effective amount of CGRP antagonists; for example, ubrogepant or atogepant, or a pharmaceutically acceptable salt, ester or prodrug thereof.
Abstract: The disclosure provides compounds that inhibit the invasion of host cells by intracellular parasites. These find use, for example, in treating and preventing periodontitis or a periodontitis-related condition or symptom.
Abstract: Provided herein are methods for determining the efficacy of treatment for polycystic kidney disease (PKD) in a patient, diagnosing PKD in a patient, staging PKD in a patient, and monitoring PKD in a patient. These methods include determining a single or multiple levels of AMBP. Also provided are kits that include an antibody specifically binds to AMBP protein and at least one antibody that specifically binds to an additional marker of PKD.
Type:
Application
Filed:
August 17, 2021
Publication date:
December 9, 2021
Applicant:
Genzyme Corporation
Inventors:
Nikolai Bukanov, Sarah Moreno, Timothy E. Weeden
Abstract: The present disclosure generally relates to compounds class I HDAC inhibitors, their production and applications. The compounds possess epigenetic immunomodulatory activities in the tumor microenvironment (TME) and thus inhibit growth of tumor cells.
Abstract: The disclosure relates to aryl hydrocarbon receptor antagonists, such as substituted imidazopyridines and imidazopyrazines, as well as methods of modulating aryl hydrocarbon receptor activity and treating various pathologies, such as cancer, by administration of these aryl hydrocarbon receptor antagonists. Additionally, the disclosure provides methods of synthesizing aryl hydrocarbon receptor antagonists, such as substituted imidazopyridines and imidazopyrazines, as well as compositions and kits containing aryl hydrocarbon receptor antagonists that can be used for the treatment of diseases and disorders.
Abstract: Provided are methods for treatment of Fabry disease in patients having HEK assay amenable mutations in ?-galactosidase A. Certain methods comprise administering migalastat or a salt thereof every other day, such as administering about 150 mg of migalastat hydrochloride every other day.
Abstract: Provided are methods for treatment of Fabry disease in patients having HEK assay amenable mutations in ?-galactosidase A. Certain methods comprise administering migalastat or a salt thereof every other day, such as administering about 150 mg of migalastat hydrochloride every other day.
Abstract: Provided are methods for treatment of Fabry disease in patients having HEK assay amenable mutations in ?-galactosidase A. Certain methods comprise administering migalastat or a salt thereof every other day, such as administering about 150 mg of migalastat hydrochloride every other day.
Abstract: Provided are methods for treatment of Fabry disease in patients having HEK assay amenable mutations in ?-galactosidase A. Certain methods comprise administering migalastat or a salt thereof every other day, such as administering about 150 mg of migalastat hydrochloride every other day.
Abstract: Liquid nicardipine compositions suitable for parenteral administration having improved stability are disclosed. The compositions are aqueous solutions having a pH of at least about 4.8, include nicardipine or a pharmaceutically acceptable salt thereof, sodium benzoate, a surfactant, a buffer and optionally a tonicity adjusting agent such as sorbitol. The liquid nicardipine compositions are preferably stored in a pharmaceutically-acceptable bag-type container. An inert gas such as nitrogen can be included therein if desired.
Abstract: The present invention relates to methods of treating p53 wild type (WT) tumors. In particular, the invention provides novel therapies for p53 WT tumors based on the combination of Mouse Double Minute 2 (MDM2) inhibitors, e.g. HDM201, together with Casein Kinase 1 alpha (CK1?) degrading agents and/or an MDM4 inhibitors, e.g. lenalidomide. The combination may be used in the treatment of solid as well as hematologic p53 WT tumors, e.g. Merkel cell carcinoma (MCC) or myelodysplastic syndrome (MDS).
Type:
Application
Filed:
October 28, 2019
Publication date:
December 9, 2021
Inventors:
Jingwei CHENG, James DECAPRIO, Donglim Esther PARK
Abstract: Provided herein are methods for treating liver disorders, including non-alcoholic steatohepatitis, and symptoms and manifestations thereof, in a patient which utilize, among others, a combination treatment of an FXR agonist and an SSAO inhibitor.
Type:
Application
Filed:
May 12, 2021
Publication date:
December 9, 2021
Inventors:
Martijn FENAUX, Kevin KLUCHER, Christopher T. JONES
Abstract: The present disclosure provides for methods of treating a patient with a CYP3A4 substrate drug, wherein the patient is treated with posaconazole. In some embodiments, the patient stops posaconazole treatment, waits for at least 2 days, and then is treated with the CYP3A4 substrate drug as soon as it is safe to do so. In some embodiments, treatment with the CYP3A4 substrate drug is delayed for about 2-42 days after stopping posaconazole. In some embodiments, the patient is treated with a reduced dose of the CYP3A4 substrate drug for about 2-42 days.
Abstract: Provided herein are methods for monitoring the development of tumor lysis syndrome (TLS) in subjects being treated for cancer with alvocidib, and methods for treating cancer using such monitoring methods. Methods for monitoring a subject for TLS can comprise performing a laboratory TLS panel on the subject about three to about four hours after the end of an alvocidib administration. Methods for treating cancer comprise administering an effective amount of alvocidib to a subject, monitoring the subject being treated with alvocidib for TLS, and administering to the subject an effective amount of one or more TLS therapies if the subject has an elevated serum potassium level or an abnormal laboratory TLS panel.
Type:
Application
Filed:
October 11, 2019
Publication date:
December 9, 2021
Inventors:
Susan Carol SMITH, Stephen Patrick ANTHONY
Abstract: Provided herein are methods for treating liver disorders, including non-alcoholic steatohepatitis, and symptoms and manifestations thereof, in a patient which utilize, among others, a combination treatment of an FXR agonist and a THR? agonist.
Type:
Application
Filed:
May 12, 2021
Publication date:
December 9, 2021
Inventors:
Martijn FENAUX, Kevin KLUCHER, Christopher T. JONES, Thorsten A. KIRSCHBERG
Abstract: The present invention relates to non peptidic, heterobivalent molecules (HBM) that are able to simultaneously bind a surface target protein as well as an endogenous or exogenous human antibody protein and induce immune effector function. More specifically, the present invention relates to agents capable of binding to a chemokine receptor and inducing the depletion of chemokine receptor positive subsets of pathogenic cells in a subject for use in the treatment and/or prevention of cancer, inflammatory, autoimmune and allergic disease.
Type:
Application
Filed:
August 25, 2021
Publication date:
December 9, 2021
Inventors:
James BAILEY, Yao CHEN, Mark HURLE, Craig LEACH, Brandon TURUNEN
Abstract: The disclosed invention provides an antibacterial pro-coagulant formula for assisting in combating the condition of bleeding gums caused by periodontal disease and gingivitis that enhances the natural healing process by assisting in the of cessation of bleeding by providing an “anti-bacterial oral healing environment” accompanied by enhanced blood flow to the affected bleeding area for more rapid blood clotting and increased blood flow to the affected area to assist the body's natural process of rebuilding healthy gum-tissue. Additionally, the disclosed invention with its antibacterial benefits, when used topically, provides for rapid surface skin blood clotting as well as increased blood circulation on the skin surface which greatly aids in the healing of external skin cuts, such as nicks from shaving or against inflammation of the skin from acne vulgaris.
Abstract: Provided herein are methods of modulating immune response, including methods of treating a cancer or an infection using a combination of kinase modulators and immunotherapy that promotes immune response. Also provided herein are methods of treating an autoimmune disease or graft-versus-host disease, and methods of reducing the risk of solid organ transplant rejection using a combination of kinase modulators and immunosuppressive therapy.
Type:
Application
Filed:
October 31, 2019
Publication date:
December 9, 2021
Applicant:
Memorial Sloan Kettering Cancer Center
Inventors:
David A. Scheinberg, Claire Y. Oh, Martin Gunther Klatt
Abstract: Pharmaceutical compositions comprising a tyrosine kinase inhibitor and a farnesyltransferase inhibitor, or pharmaceutically acceptable salts thereof, and a pharmaceutically acceptable carrier, as well as methods for preventing or treating cancer by administering the same are disclosed herein.
Abstract: A nicotine lozenge includes a body that is partially or wholly receivable in an oral cavity. The body includes a soluble-fiber matrix and nicotine or a derivative thereof dispersed in the soluble-fiber matrix. A nicotine lozenge may include at least 40 weight percent of soluble fiber. Soluble fiber in a nicotine lozenge may include maltodextrin. The nicotine lozenge is adapted to release the nicotine or a derivative thereof from the body when the body is received within the oral cavity of an adult consumer and exposed to saliva. A method of making nicotine lozenges includes forming a molten mixture of at least 40 weight percent soluble fiber, nicotine, and less than 15 weight percent water while maintaining a mixture temperature of less than 150° C. and portioning the molten mixture into a plurality of nicotine lozenges. The ingredients can be mixed to form the molten mixture in an extruder.
Type:
Application
Filed:
August 25, 2021
Publication date:
December 9, 2021
Applicant:
Altria Client Services LLC
Inventors:
Feng GAO, Diane L. GEE, Phillip M. HULAN, Shuzhong ZHUANG, William J. BURKE
Abstract: Disclosed herein are new dosage regimens for deuterium-substituted benzoquinoline compounds, and methods for the treatment of abnormal muscular activity, movement disorders, and related conditions.
Abstract: Provided is a quinoline derivative having indoleamine-2,3-dioxygenase inhibitory activity, specifically, provided is a compound of general Formula (I) or pharmaceutically acceptable salt thereof, its pharmaceutical composition, preparation method and use in the manufacture of a medicament for immunomodulating and preventing and/or treating of a disease associated with IDO expression abnormality and/or tryptophan metabolism abnormality. Also provided is use of a combination medication of the quinoline derivative and HDAC inhibitor and its use in the manufacture of an anti-tumor drug.
Type:
Application
Filed:
September 25, 2019
Publication date:
December 9, 2021
Inventors:
Jindi YU, Lijun XIN, Song SHAN, Jiangfei ZHU, Lin YANG, Chao FU, Zhibin LI, Xianping LU
Abstract: The present invention relates to a liquid pharmaceutical composition suitable for administration by inhalation comprising: (i) a suspension of particles comprising 9,10-dimethoxy-2-(2,4,6-trimethylphenylimino)-3-(N-carbamoyl-2-aminoethyl)-3,4,6,7-tetrahydro-2H-pyrimido[6,1-a]isoquinolin-4-one (RPL554); and (ii) a diluent which is 1,1,1,2-tetrafluoroethane (HFA-134a), wherein the liquid pharmaceutical composition is substantially free of surfactant. The invention also relates to a pressurised metered dose inhaler comprising the liquid pharmaceutical composition.
Type:
Application
Filed:
October 9, 2019
Publication date:
December 9, 2021
Inventors:
Peter Lionel SPARGO, Phillip A. HAYWOOD
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: The present invention relates to substituted alkynylene compounds represented by the compounds of formula (I), pharmaceutically acceptable salts and stereoisomers thereof. The present invention further provides the therapeutic uses of the compounds of formula (I) as anti-cancer agents.
Abstract: A compound is represented by the following formula I. The compound and stereoisomer, racemate, tautomer, isotope labelled derivative, nitrogen oxide, pharmaceutically acceptable salt or solvate thereof can be prepared and used in the preparation of a medicament for treating a RET kinase-mediated disease.