Abstract: Aerosol formulations of granisetron useful for pulmonary delivery are provided. The formulations are useful in the reduction, elimination or prevention of nausea and vomiting associated with chemotherapy, radiation therapy, and surgery. Also provided are novel methods to treat chemotherapy-induced nausea and vomiting (CINV), radiation-induced nausea and vomiting (RINV), and post-operative nausea and vomiting (PONV) using the inhalation formulations.
Abstract: The present invention relates to a method for predicting susceptibility to sorafenib treatment by using an SULF2 gene, and a composition for treatment of sorafenib-resistant cancer using the SULF2 expression inhibition. The method for predicting susceptibility to sorafenib treatment by using the SULF2 gene according to the present invention can enable achievement of an optimal therapeutic effect by administering a drug suitable for cancer patients, and the composition for treatment of sorafenib-resistant cancer using the SULF2 inhibition has a very excellent anticancer treatment effect.
Type:
Application
Filed:
March 20, 2018
Publication date:
March 19, 2020
Applicant:
AJOU UNIVERSITY INDUSTRY-ACADEMIC COOPERATION FOUNDATION
Abstract: The present invention relates to a pharmaceutical composition the prevention or treatment of DYRK-related diseases containing a pyridine-based compound as an active ingredient, a pyridine-based compound of the present invention which is used as an active ingredient of the pharmaceutical composition inhibits the activity of DYRK1A with very high efficacy and selectivity, thereby can be used effectively in the prevention or treatment of DYRK-related diseases, such as Down syndrome, degenerative brain diseases, cancer, and metabolic diseases.
Type:
Application
Filed:
December 15, 2017
Publication date:
March 19, 2020
Applicants:
KOREA RESEARCH INSTITUTE OF BIOSCIENCE AND BIOTECHNOLOGY, KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY
Abstract: A composition for preventing or treating glaucoma or ocular hypertension including a combination of isopropyl (6-{[4-(pyrazol-1-yl)benzyl](pyridin-3-ylsulfonyl) aminomethyl} pyridin-2-ylamino) acetate and at least one other drug for preventing or treating glaucoma or ocular hypertension, with the proviso that tafluprost is excluded.
Abstract: The invention relates to a method of treating a type of cancer related to activation of an RAS gene in a subject, and belongs to the field of pharmaceuticals. The method of treating cancer related to activation of an RAS gene involves administering to the subject a therapeutically effective amount of 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine, a pharmaceutically acceptable salt thereof, or a solvate thereof. 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine was found to reduce the level of RAS mRNA. 24 mM of 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine is capable of reducing RAS mRNA level by 3.5 folds. The compound of the present invention also has a significant tumor suppressive effect on a Drosophila tumor model. Clinical anti-tumor products that exploit the intervention and treatment of tumors by 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine have immense potential.
Abstract: The invention relates to a mucoadhesive oromucosal formulation comprising a nicotine complex, said nicotine complex comprising nicotine in ionic complex with at least one mucoadhesive water-soluble anionic polymer.
Abstract: The invention relates to a new administration form for the oral application of the active substance ethyl 3-[(2-{[4-(hexyloxycarbonylamino-imino-methyl)-phenylamino]-methyl}-1-methyl-1H-benzimidazole-5-carbonyl)-pyridin-2-yl-amino]-propionate and the pharmacologically acceptable salts thereof.
Type:
Application
Filed:
November 25, 2019
Publication date:
March 19, 2020
Inventors:
Ulrich BRAUNS, Norbert HAUEL, Peter SIEGER
Abstract: Methods of use, formulations, and devices for delivering therapeutic drugs locally to the region of the spleen are described herein. A method for treating sepsis and other inflammatory disease conditions can include inserting a drug delivery system inside the body, advancing the device to the spleen through the splenic artery, splenic vein or other blood vessel adjacent to the splenic nerves, or within a ligament associated with the spleen, such as the splenorenal or gastrosplenic ligaments.
Type:
Application
Filed:
June 29, 2017
Publication date:
March 19, 2020
Inventors:
Corinne Bright, Kondapavulur T. Venkateswara-Rao, Emily Stein
Abstract: The present disclosure relates to ABCA1 inducer compounds for use in treating kidney disorders, and in particular, chronic kidney diseases, glomerular diseases or proteinuric kidney diseases such as Alport syndrome, focal segmental glomerulosclerosis, and diabetic kidney disease.
Abstract: A method of treating or preventing a neuroinflammatory and/or neurodegenerative disease in a subject by administering a pharmaceutically effective amount of a CB2 receptor agonist is described. The CB2 receptor agonist can be a compound according to formula I or a pharmaceutically acceptable salt thereof, with R1 and R2 as defined herein. Administration of the CB2 receptor agonist activates CB2 receptors in the microglia, can restore syntaptic plasticity, cognition, and memory in subjects having elevated levels of amyloid-?peptide in the brain.
Abstract: The present invention relates to a bioactive agent that increases the intracellular concentration and/or activity of one or more heat shock proteins, including Hsp70, for use in the treatment of frontotemporal disorders.
Type:
Application
Filed:
May 24, 2018
Publication date:
March 19, 2020
Inventors:
Thomas Kirkegaard Jensen, Linda Greensmith
Abstract: Provided herein is an ophthalmic composition. In some embodiments, the ophthalmic composition includes a low concentration of an ophthalmic agent for treatment of an ophthalmic disorder or condition; and an ophthalmically acceptable carrier, wherein the ophthalmic agent is distributed with substantial uniformity throughout the ophthalmically acceptable carrier. Further disclosed herein include an ophthalmic composition including a low concentration of an ophthalmic agent and deuterated water. Also disclosed herein are methods of arresting or preventing myopia development by administering to an eye of an individual in need thereof an effective amount of an ophthalmic composition as described herein.
Type:
Application
Filed:
November 7, 2019
Publication date:
March 19, 2020
Inventors:
Gregory I. OSTROW, Kenneth J. WIDDER, David S. BAKER
Abstract: The present disclosure relates to a pharmaceutical composition comprising two Tyrosine Kinase Inhibitors (TKIs), namely Ceritinib and an EGFR Inhibitor. The present combination can be administered independently or separately, in a quantity which is jointly therapeutically effective for the treatment of a TKI mediated disease, such as cancer. The disclosure also provides the use of such a combination for the manufacture of a medicament; the use of such a combination as a medicine; a kit of part comprising such a combination; and a method of treatment of such a combination.
Type:
Application
Filed:
September 24, 2019
Publication date:
March 19, 2020
Inventors:
Serafino Pantano, Fang Li, Nanxin Li, Anthony Boral
Abstract: The present disclosure reports solid forms of ((S)-5-((1-(6-chloro-2-oxo-1,2-dihydroquinolin-3-yl)ethyl)amino)-1-methyl-6-oxo-1,6-dihydropyridine-2-carbonitrile.
Abstract: The invention features methods and compositions for the treatment of Alzheimer's Disease using lysergic acid diethylamide and pharmaceutically acceptable salts thereof.
Abstract: Potassium chloride cotransporter-2 (KCC2) plays a critical role in brain function, and deficiency in KCC2 has been linked to neurological diseases, psychiatric disorders, and central nervous system injuries. In particular, Rett syndrome (RTT), a severe neurodevelopmental disorder caused by mutations in the X-linked gene Methyl CpG binding Protein 2 (MECP2), has been linked to deficits in KCC2. The disclosure reports the use of CRISPR/Cas9 genome-editing technology to generate stem cell-derived, genetically defined KCC2 reporter human neurons for large-scale compound screening. This screening platform has been utilized to identify a number of small molecule compounds that are capable of enhancing KCC2 expression in both wild-type and RTT neurons, as well as organotypical brain slices cultured from wild-type mice.
Type:
Application
Filed:
May 22, 2018
Publication date:
March 19, 2020
Applicant:
Whitehead Institute for Biomedical Research
Abstract: The present disclosure relates to a film formulation for oral administration, containing tadalafil free base and a method of preparing the same, and a film may be provided with maximized dispersion stability of tadalafil free base in the film by the addition of a dispersion stabilizing agent in small amounts without unique fragrance or favor that may appear when other dispersion stabilizing agents known in the art are used, and an extremely low likelihood that a reagglomeration phenomenon of tadalafil free base particles will occur, and an amount of bubbles generated may be significantly reduced during a production process.
Type:
Application
Filed:
November 19, 2019
Publication date:
March 19, 2020
Inventors:
Hong Ryeol JEON, Do-Woo KWON, Bong-Sang LEE, Su-Jun PARK, Bong-Geun CHA, Jun-Ki KIM, Jiyeong HAN, Myeongcheol KIL
Abstract: Methods for treating Down syndrome and improving cognitive function of a patient with an intellectual disability are disclosed. 5-hydroxytryptamine sub-receptor six (5-HT6) receptor antagonists are provided for improving the cognition of a Down syndrome patient.
Type:
Application
Filed:
November 18, 2019
Publication date:
March 19, 2020
Applicant:
THE UNIVERSITY OF UTAH RESEARCH FOUNDATION
Inventors:
Julie Ruth Korenberg, Karen Sue Wilcox, Peter Jeffrey West, Raymond Pierre Kesner
Abstract: The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized by, caused by or associated with the release of chemical mediators via degranulation and other processes effected by activation of the IgE and/or IgG receptor signaling cascades.
Type:
Application
Filed:
November 21, 2019
Publication date:
March 19, 2020
Applicant:
Rigel Pharmaceuticals, Inc.
Inventors:
Rajinder Singh, Ankush Argade, Donald Payan, Susan Molineaux, Sacha J. Holland, Jeffrey Clough, Holger Keim, Somasekhar Bhamidipati, Catherine Sylvain, Hui Li, Alexander B. Rossi
Abstract: Disclosed are chemical entities which are compounds of formula (I): or pharmaceutically acceptable salts thereof; wherein Y, Ra, Ra?, Rb, Rc, X1, X2, X3, Rd, Z1, and Z2 have the values described herein and stereochemical configurations depicted at asterisked positions indicate absolute stereochemistry. Chemical entities according to the disclosure can be useful as inhibitors of Sumo Activating Enzyme (SAE). Further provided are pharmaceutical compositions comprising a compound of the disclosure and methods of using the compositions in the treatment of proliferative, inflammatory, cardiovascular, and neurodegenerative diseases or disorders.
Type:
Application
Filed:
April 23, 2019
Publication date:
March 19, 2020
Applicant:
Millennium Pharmaceuticals, Inc.
Inventors:
Matthew O. DUFFEY, Dylan ENGLAND, Brian Scott FREEZE, Zhigen HU, Steven LANGSTON, Charles McINTYRE, Hirotake MIZUTANI, Koji ONO, He XU
Abstract: The invention provides a class of compounds as inhibitors of influenza virus replication, preparation methods thereof, pharmaceutical compositions containing these compounds, and uses of these compounds and pharmaceutical compositions thereof in the treatment of influenza.
Type:
Application
Filed:
December 14, 2017
Publication date:
March 19, 2020
Applicants:
SUNSHINE LAKE PHARMA CO., LTD., NORTH & SOUTH BROTHER PHARMACY INVESTMENT COMPANY LIMITED
Abstract: Methods for treating a disease in a subject in need thereof by administering an ACVR1 inhibitor having the following formula (I) are disclosed: including stereoisomers, tautomers, pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R3, and R4 are as defined herein. Subjects that may benefit from treatment may have mutations in their ACVR1 gene. Various diseases may be treated using the described methods, including cancers (e.g., diffuse intrinsic pontine glioma (DIPG)) and genetic disorders (e.g., fibrodysplasia ossificans progressiva (FOP)).
Type:
Application
Filed:
July 26, 2019
Publication date:
March 19, 2020
Inventors:
Steven L. Warner, David J. Bearss, Adam Siddiqui-Jain, Clifford J. Whatcott, Jason Marc Foulks, Stephen Patrick Anthony, Paul Flynn, Yuji Fujiwara, Yuka Arikawa
Abstract: Small molecule regulators of steroid receptor coactivator (SRC) family proteins are provided, as well as methods for their use in treating or preventing SRC-related diseases. The SRC-related diseases can include cancer, metabolic disorders, human immunodeficiency virus, neurodegenerative disorders, and/or inflammatory diseases. Also provided are methods for regulating SRC family proteins in a cell.
Type:
Application
Filed:
November 21, 2019
Publication date:
March 19, 2020
Applicant:
BAYLOR COLLEGE OF MEDICINE
Inventors:
Bert W. O'Malley, David Michael Lonard, Jin Wang, Jianming Xu, Jianwei Chen
Abstract: The present invention relates to novel treatments of periodontal disease by administering a suitable formulation of a cyclophilin inhibitor. The present invention further relates to novel pharmaceutical compositions containing said cyclophilin inhibitor compounds.
Abstract: Disclosed herein are compounds for use in lightening skin, treating uneven skin pigmentation and/or improving the appearance of aging skin, as well as methods utilizing the compounds, and anti-aging compositions comprising the compounds and a pharmaceutically acceptable carrier. The compounds have the general Formula I: or a pharmaceutically acceptable salt thereof, wherein the dashed line, X, Y, Z, Ra-Rd, and R1-R3 are as defined herein.
Abstract: The use of methotrexate, e.g., repeated dosing or sustained-release formulations of methotrexate, for treating or reducing risk of proliferative vitreoretinopathy (PVR) or epiretinal membranes (ERM), e.g., after surgical vitrectomy to treat retinal detachment.
Abstract: Disclosed herein are methods and compounds for treating augmenting and enhancing the production of type I IFNs in vivo. In some embodiments, also disclosed herein include methods of activating and enhancing the cGAS-STING response and use of an inhibitor of a phosphodiesterase for the treatment of a microbial infection.
Type:
Application
Filed:
December 21, 2017
Publication date:
March 19, 2020
Inventors:
William Michael GALLATIN, Gregory N. DIETSCH
Abstract: Compositions may include a pharmaceutical active agent, a high viscosity liquid carrier material (HVLCM), a lactic acid-based polymer, and an organic solvent. Related compositions and methods are also disclosed.
Type:
Application
Filed:
August 19, 2019
Publication date:
March 19, 2020
Applicant:
DURECT CORPORATION
Inventors:
Jeremy C. WRIGHT, Wilma TAMRAZ, John J. LEONARD, John W. GIBSON, Keith E. BRANHAM, Stefania SJOBECK, Brooks BOYD, Christopher M. RUBINO
Abstract: The present disclosure is directed to methods and compositions that are useful in combating the spread of Zika virus infections, such as, but not limited to, methods and compositions for treating, preventing or suppressing a Zika virus infection in a subject. The methods comprise administering to the subject an effective amount of a compound of the disclosure, or a composition (such as a pharmaceutical composition) comprising a compound of the disclosure.
Type:
Application
Filed:
November 22, 2019
Publication date:
March 19, 2020
Inventors:
Yarlagadda S. BABU, Pravin L. KOTIAN, Shanta BANTIA
Abstract: Nasal compositions, comprising an aqueous solution containing caffeine and/or theobromine in a total concentration of up to about 0.5 percent (w/v) and an aqueous carrier having a pH of about 6-8 and comprising physiologically acceptable salts of sodium, potassium and calcium. The nasal composition when used as a nasal spray or as nasal drops or irrigation fluid is able to clean the nasal passages and to stimulate nasal mucociliary clearance and, in contrast to nasal decongestants, may be used on a daily-basis for a period longer than 5 days.
Type:
Application
Filed:
November 21, 2019
Publication date:
March 19, 2020
Inventors:
Franciscus Wilhelmus Henricus Maria Merkus, Bart Merkus
Abstract: Provided are deuterated analogs of a compound and methods of using such deuterated analogs for treating a brain tumor in a patient in need thereof; the treatment comprising administering to the patient a deuterated compound described herein. The deuterated compound may be administered in combination with radiation therapy and/or an additional therapeutic agent.
Abstract: The present invention relates to compounds for use in treating a disease that is associated with (related to) CYP7B1 wherein the compound inhibits CYP7B1. The present invention further relates to a method of treating or preventing such a disease by administering an inhibitor of CYP7B1. The present invention also relates to a method of determining whether a compound is effective in treating or preventing a disease associated with the formation of inducible bronchus-associated lymphoid tissue (iBALT).
Abstract: The present disclosure relates to compounds of Formula I, or their stereoisomers, pharmaceutically acceptable salts, complexes, hydrates, solvates, tautomers, polymorphs, racemic mixtures, optically active forms and pharmaceutically active derivatives thereof, and pharmaceutical compositions containing them as the active ingredient which can be used as medicaments. The aforementioned substances can also be used in the manufacture of medicaments for treatment, prevention or suppression of diseases, and conditions mediated by microbes. The present disclosure also relates to the synthesis and characterization of aforementioned substances.
Abstract: Unit dosage forms of meloxicam containing either 5 mg or 10 mg of meloxicam that provide effective pain relief and have desirable pharmacokinetic properties are described. The unit dosage forms can provide pain relief when a single unit dose is administered to a patient and useful for treating pain such as osteoarthritis pain at a relatively low systemic exposure to meloxicam.
Abstract: This invention is directed to a method of treating alcohol dependence, including acute and post-acute withdrawal symptoms, comprising treating an alcohol dependent patient with ibogaine, ibogaine derivative, or pharmaceutically acceptable salt and/or solvate thereof at a dosage that provides an average serum concentration of about 50 ng/mL to about 850 ng/mL under conditions where the QT interval prolongation does not exceed about 50 milliseconds.
Abstract: The disclosure relates to Prostaglandin receptor EP2 antagonists, derivatives, compositions, and methods related thereto. In certain embodiments, the disclosure relates to methods of treating or preventing conditions and diseases in which EP2 receptor activation has a physiological role, such as but not limited to, brain injury, inflammatory diseases, neuroinflamation after a seizure, pain, endometriosis, cancer, rheumatoid arthritis, skin inflammation, vascular inflammation, colitis, and neurological disorders by administering a pharmaceutical composition comprising a compound disclosed herein to a subject in need thereof.
Type:
Application
Filed:
November 15, 2019
Publication date:
March 19, 2020
Inventors:
Thota Ganesh, Jianxiong Jiang, Raymond Dingledine
Abstract: The present invention is directed to, in part, methods of preventing and/or treating a disease or condition relating to aberrant function of a voltage-gated, sodium ion channel, for example, abnormal late/persistent sodium current. In some embodiments, methods of treating a neurodevelopmental disorder (e.g., epilepsy) comprising administering to a subject in need thereof a compound disclosed herein (e.g., a compound of Formula (I), (I-a), or (I-b), e.g., eleclazine) are provided.
Type:
Application
Filed:
May 16, 2018
Publication date:
March 19, 2020
Inventors:
Gabriel Martinez Botella, Kiran Reddy, Marion Wittmann
Abstract: The present invention provides methods of use for compositions comprising an immunotherapeutic such as chimeric antigen receptor T cells (CAR-T cells), and specifically those that target a tumor antigen cleaved by gamma secretase, in combination with bisfluoroalkyl-1,4-benzodiazepinone compounds, including compounds of Formula (I) or prodrugs thereof; for treating lymphomas.
Abstract: This invention discloses uses for estradiol in preparing anti-small cell lung cancer and/or ovarian cancer and/or osteosarcoma products. This invention provides uses for estradiol in preparing anti-small cell lung cancer and/or ovarian cancer and/or osteosarcoma products. From carrying out cancer drug repositioning for the FDA- and CFDA-approved drug estradiol, experiments for this invention show, based on screening of non-anti-cancer drugs for various cancer cell lines (tissue types) and mutation sites, that estradiol has a new use as an anti-small cell lung cancer and/or ovarian cancer and/or osteosarcoma medication, thus achieving a new purpose for an old drug.
Abstract: Polyethylene glycol (PEG)-conjugated glucocorticoid prodrugs, methods of preparation, and use for the treatment of diseases and disorders are disclosed. In particular, PEG-conjugated dexamethasone compounds and methods of using them for treating inflammatory and autoimmune diseases, including but not limited to lupus, are disclosed.
Type:
Application
Filed:
November 25, 2019
Publication date:
March 19, 2020
Applicant:
Board of Regents of the University of Nebraska
Inventors:
Dong Wang, Fang Yuan, Zhenshan Jia, Xiaobei Wang
Abstract: Bile acids and related compositions and methods of synthesis and use. More specifically, deoxycholic acid and related compositions, said compositions being free of all moieties of animal origin and free of pyrogenic moieties.
Type:
Application
Filed:
September 25, 2019
Publication date:
March 19, 2020
Applicant:
ALLERGAN SALES, LLC
Inventors:
Robert M. Moriarty, Nathaniel E. David, Nadir Ahmeduddin Mahmood
Abstract: A sterol composition in pumpkin seed oil and an application thereof, and a drug for treating benign prostatic hyperplasia are provided, which relate to a technical field of medicine. The sterol composition in the pumpkin seed oil includes components by weight percentage of: 0.2-2 wt % cholesterol, 0.5-5 wt % campesterol, 1.5-5 wt % ?-sitosterol, 15-40 wt % stigmasterol, 20-40 wt % ergosta-7,22-dien-3?-ol, 5-10 wt % lanosterol, and 15-30 wt % cholest-7-en-3?,5?-diol. The sterol composition in the pumpkin seed oil is a pumpkin phytosterol composition extracted from the pumpkin seed oil. Through combining the phytosterol components and controlling a proportion among the components, effects of alleviating and treating prostate diseases are achieved, especially for the benign prostatic hyperplasia.
Abstract: The invention relates to the use of agents that alter the peritumoral environment, specifically non-peptide NK1 receptor antagonists, for the treatment of cancer. The peritumoral environment is formed by the stromal cells, the stromal matrix, intra- and peri-tumoral vascularization and the cells responsible for the inflammatory and/or immune response around the tumor. The result of the alteration to the peritumoral environment is a reduction in the size of the tumor, the prevention of its development and, optionally, the induction of its disappearance. The invention also relates to pharmaceutical compositions containing said peritumoral-environment-altering agents, either alone or combined with at least one other active ingredient, for the treatment of cancer.
Type:
Application
Filed:
November 15, 2019
Publication date:
March 19, 2020
Inventors:
Manuel Vicente SALINAS MARTÍN, María Carmen LARA RUIZ
Abstract: This disclosure provides bioceramic compositions of multiparticulate crystalline multimetallic silicates having silica double tetrahedra structures, such as Strontium-akermanite (Sr2MgSi2O7), Akermanite (Ca2MgSi2O7), Baghdadite (Ca3ZrSi2O9), Hardystonite (Ca2ZnSi2O7), as sources for controlled release of multiple metallic ions, such as Ca2+, Mg2+, Zr4+, Sr2+, Zn2+ for medical and dental use. This disclosure also includes medical and dental uses of the disclosed compositions, for example, in tissue regeneration, including bone tissue.
Type:
Application
Filed:
September 12, 2019
Publication date:
March 19, 2020
Inventors:
CÉSAR EDUARDO BELLINATI, CRISTIANE VILA, WILLIAM PEREIRA DOS SANTOS, MAÍRA BENDLIN CALZAVARA
Abstract: This invention relates to methods and compositions for administering an effective amount of a CDA substrate drug and an effective amount of cedazuridine. In particular, the invention relates to methods for treating cancer, inhibiting degradation of a CDA substrate drug, and reducing DNA methylation in a subject in need thereof comprising administering an effective amount of a CDA substrate drug and an effective amount of cedazuridine.
Type:
Application
Filed:
September 18, 2019
Publication date:
March 19, 2020
Inventors:
Harold Keer, Mohammad Azab, Aram Oganesian
Abstract: Provided herein are methods and compositions related to treating and/or preventing sleep disorders and for improving sleep health in a subject by administering to the subject (e.g., orally administering to the subject) a composition comprising nicotinamide riboside and/or pterostilbene.
Type:
Application
Filed:
May 18, 2018
Publication date:
March 19, 2020
Inventors:
Eric A. Marcotulli, Dan Alminana, Ryan Dellinger, Mark Morris