Abstract: The invention provides a compound of Formula I, Pharmaceutical compositions comprising such compounds and the use of such compounds in the treatment of phosphoinositide 3-kinase related diseases and disorders such as cancer. The instant application further relates to the treatment of histone deacetylase related disorders and diseases related to both histone deacetylase and phosphoinositide 3-kinase.
Abstract: One aspect of the present disclosure is a pharmaceutical composition which includes (R)—N-[1-(3,5-difluoro-4-methansulfonylamino-phenyl)-ethyl]-3-(2-propyl-6-trifluoromethyl-pyridin-3-yl)-acrylamide as a first component and a cellulosic polymer as a second component, wherein the composition of one aspect of the present disclosure has a formulation characteristic in which crystal formation is delayed for a long time.
Type:
Application
Filed:
August 10, 2018
Publication date:
July 9, 2020
Applicant:
AMOREPACIFIC CORPORATION
Inventors:
Joon Ho CHOI, Won Kyung CHO, Kwang-Hyun SHIN, Byoung Young WOO, Ki-Wha LEE, Min-Soo KIM, Jong Hwa ROH, Mi Young PARK, Young-Ho PARK, Eun Sil PARK, Jae Hong PARK
Abstract: A novel function for the p53 gene related to resolution of deep venous thrombosis is disclosed herein. Lack of the p53 gene results in impaired thrombus resolution in a clinically relevant in vivo model of deep venous thrombus resolution. It is further shown that augmentation of p53 activity with quinacrine accelerates thrombus resolution in vivo, and that this beneficial effect is completely dependent on p53. p53-based therapy is therefore provided to accelerate thrombus resolution in patients, and to prevent or ameliorate the debilitating long-term complications of deep venous thrombosis such as post-thrombotic syndrome.
Abstract: Disclosed herein is a compound of formula (I), or a pharmaceutically acceptable salt thereof: (I). Also disclosed herein are uses of the compounds disclosed herein in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising a compound disclosed herein. Further disclosed herein are uses of the compositions in the potential treatment or prevention of an IDO-associated disease or disorder.
Abstract: Provided are methods of treating a patient diagnosed with Fabry disease and methods of enhancing ?-galactosidase A in a patient diagnosed with or suspected of having Fabry disease. Certain methods comprise administering to a patient a therapeutically effective dose of a pharmacological chaperone for ?-galactosidase A, wherein the patient has a splice site mutation in intron 4 of the nucleic acid sequence encoding ?-galactosidase A. Also described are uses of pharmacological chaperones for the treatment of Fabry disease and compositions for use in the treatment of Fabry disease.
Abstract: The present invention relates to a method of treating PIK3CA-Related Overgrowth Spectrum (PROS) more particularly, Congenital, Lipomatous, Overgrowth, Vascular Malformations, Epidermal Nevi and Spinal/Skeletal Anomalies and/or Scoliosis (CLOVES) 10 syndrome. To date, there are no specific treatments for patients and no animal models of PROS to better understand the physiopathology of the disorder. Inventors developed a genetic mouse model of PROS that recapitulates the human disease and demonstrated the efficacy of BYL719. Based on these results they treated two patients, one adult and one child, with severe CLOVES syndrome using BYL719. The drug had a robust efficiency on disease in the 15 two patients inducing quick recovery of all affected organs. Thus, the invention relates to a method of treating PROS in a subject in need thereof comprising the step of administrating the subject with a therapeutically effective amount of BYL719.
Abstract: A pharmaceutical composition containing isomyosmine or a pharmaceutically acceptable salt thereof is administered to an individual in need thereof for treating a substance addiction, inclusive of addiction to heroin (diacetylmorphine), cocaine, opioids, methadone, d-methamphetamine, barbiturates, alcohol, benzodiazepines, amphetamines, or buprenorphine. The isomyosmine, along with optional additional therapeutic agent(s), may be administered in a capsule, tablet, or lozenge.
Abstract: A therapeutic agent or a preventive agent for alopecia areata has an ROR? antagonistic activity, and, there is a therapeutic agent or a preventive agent for alopecia areata, including a cyclic amine derivative typified by the following compound or a pharmacologically acceptable salt thereof as an active ingredient.
Abstract: Compounds and methods for modulating the activity of receptors are disclosed. Some of the compounds modulate the activity of glycine receptors. Certain embodiments of the compounds are useful for treatment of pain, treatment of opioid addiction, and/or reduction of side effects attributable to opioid use.
Type:
Application
Filed:
July 13, 2018
Publication date:
July 9, 2020
Applicant:
University of Pittsburgh - Of the Commonwealth System of Higher Education
Abstract: Methods and compositions for treating disorders of the nail and nail bed. Such compositions contain a vehicle in which all components of the composition are dissolved, suspended, dispersed, or emulsified, a non-volatile solvent, a wetting agent, and a pharmaceutically active ingredient that is soluble in the non-volatile solvent and/or a mixture of the vehicle and the non-volatile solvent, and which composition is effective in treating a disorder of the nail or nail bed.
Abstract: The present invention relates to methods for treating chronic inflammatory conditions using a mast cell stabilizing compound. The invention further relates to compositions and dosage forms comprising mast cell stabilizing agents.
Abstract: The present invention addresses the problem of providing a therapeutic agent for abdominal aortic aneurysms, with which pharmacotherapy is possible. The present invention provides a therapeutic agent for an aortic aneurysm comprising, as an active component, (?)-6-[3-[3-cyclopropyl-3-[(1R,2R)-2-hydroxycyclohexyl]ureido]propoxy]-2(1H)-quinolinone or a salt thereof, or a solvate of these.
Abstract: This disclosure relates to a nebulization composition comprising tiotropium, or a pharmaceutically acceptable salt thereof, and indacaterol, or a pharmaceutically acceptable salt thereof. This disclosure also relates to a process for preparing such a composition and to methods of treating inflammatory and/or obstructive airway diseases using such a composition.
Abstract: The invention provides an oral dosage form comprising (i) an amount of oxycodone and (ii) an amount of buprenorphine, wherein the weight ratio of the amount of buprenorphine to the amount of oxycodone is greater than 1:40 calculated with the amount of buprenorphine in the dosage form expressed as the equimolar amount of buprenorphine base (Mw=467.64 g/mol) in mg, and the amount of oxycodone in the dosage form expressed as the equimolar amount of oxycodone hydrochloride (Mw=351.82 g/mol) in mg. The invention also provides combinations of an opioid agonist and buprenorphine for use to treat pain, wherein the combination achieves a reduction of adverse pharmacodynamic responses (such as, respiratory depression), compared with a corresponding stand-alone opioid therapy. The invention also includes methods of treatment and dosage forms thereof comprising such combinations.
Type:
Application
Filed:
June 29, 2018
Publication date:
July 9, 2020
Inventors:
Alessandra CIPRIANO, Salvatore COLUCCI, Stephen HARRIS, Michelle HUMMEL, Donald KYLE, Garth WHITESIDE
Abstract: The invention relates to a dosage form that is thermoformed without discoloration and is safeguarded from abuse, comprising at least one synthetic or natural polymer having a breaking strength of at least 500 N in addition to one or more active substances that could be subject to abuse. The invention also relates to a corresponding method for producing said dosage form.
Type:
Application
Filed:
February 21, 2020
Publication date:
July 9, 2020
Applicant:
GRÜNENTHAL GMBH
Inventors:
Elisabeth ARKENAU-MARIC, Johannes BARTHOLOMAEUS, Heinrich KUGELMANN
Abstract: The present invention relates to methods and compositions for treating pain in a subject and safely transitioning a subject from a full ?-opioid receptor agonist to a partial ?-opioid receptor agonist.
Type:
Application
Filed:
March 16, 2020
Publication date:
July 9, 2020
Applicant:
BioDelivery Sciences International, Inc.
Inventors:
Andrew Finn, Todd Kirby, Lynn R. Webster
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: 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: 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: Provided herein are methods of using 4-(4-(4-(((2-(2,6-dioxopiperidin-3-yl)-1-oxoisoindolin-4-yl)oxy)methyl)benzyl)piperazin-1-yl)-3-fluorobenzonitrile, or an enantiomer, a mixture of enantiomers, a tautomer, or a pharmaceutically acceptable salt thereof, in combination with a second active agent for treating, preventing or managing multiple myeloma. The second active agent is one or more of a BTK inhibitor, an mTOR inhibitor, a PIM inhibitor, an IGF-1R inhibitor, an MEK inhibitor, an XPO1 inhibitor, a DOT1L inhibitor, an EZH2 inhibitor, a JAK2 inhibitor, a BRD4 inhibitor, a PLK 1 inhibitor, an NEK2 inhibitor, an AURKB inhibitor, a BIRC5 inhibitor, a BET inhibitor, or a DNA methyltransferase inhibitor.
Abstract: Provided herein are pharmaceutical compositions (e.g., oral dosage formulations) comprising (S)-4-(4-(4-(((2-(2,6-dioxopiperidin-3-yl)-1-oxoisoindolin-4-yl)oxy)methyl)benzyl)piperazin-1-yl)-3-fluorobenzonitrile, or an enantiomer, mixture of enantiomers, tautomer, isotopolog, or pharmaceutically acceptable salt thereof, and a carrier or diluent. Also provided herein are methods of preparing and methods of using the pharmaceutical compositions.
Type:
Application
Filed:
January 8, 2020
Publication date:
July 9, 2020
Inventors:
Anjali Agrawal, Ming J. Chen, Shyam Babu Karki, Prajwal Gunwanth Thool, Dora Visky, Ruimin Xie
Abstract: Compounds for use in the treatment of human immunodeficiency virus (HIV) infection are disclosed. The compounds have the following Formula (I): including stereoisomers and pharmaceutically acceptable salts thereof, wherein L, R1, R5, W, X, Y1, Y2, and Z are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
Type:
Application
Filed:
September 16, 2019
Publication date:
July 9, 2020
Inventors:
Manoj C. Desai, Mingzhe Ji, Haolun Jin, Hyung-Jung Pyun, Teresa Alejandra Trejo Martin
Abstract: Oral film dosage forms that provide improved solubilization and stabilization of an active ingredient in particle form include at least one primary crystallization inhibitor in an amount that inhibits growth and/or agglomeration of the active ingredient, a polyoxyethylated fatty acid glycerides in an amount that further enhances inhibition of crystallization, growth and agglomeration of the particles of the pharmaceutically active ingredient; and at least one plasticizer present in an amount that is effective to increase flexibility and elasticity of the film dosage form.
Type:
Application
Filed:
March 17, 2020
Publication date:
July 9, 2020
Applicant:
Intelgenx Corp.
Inventors:
Horst G. Zerbe, Nadine Paiement, Angela Angusti, Cormac Long, Rodolphe Obeid, Laetitia Rodes, Billal Tir
Abstract: An Axl inhibitor and one or more immune checkpoint (activity) modulators and/or one or more oncolytic viruses, for use in the prevention, treatment or management of cancer, wherein the Axl inhibitor and the one or more immune checkpoint (activity) modulators and/or the one or more oncolytic viruses are administered concurrently, separately or sequentially; compositions containing such components in combination; and methods of treating cancer in a patient by administering such components in combination.
Abstract: Water-in-hydrocarbon emulsions, preferably comprising a fluorinated or perfluorinated hydrocarbon continuous phase, a discontinuous aqueous phase, and a surfactant or mixture of surfactants. The emulsions contain pharmacologically active agents, such as endothelin receptor antagonists, and are particularly suitable for pulmonary drug delivery. The emulsions are useful for treating pulmonary diseases or disorders, including pulmonary hypertension conditions, such as acute pulmonary arterial hypertension.
Type:
Application
Filed:
July 6, 2018
Publication date:
July 9, 2020
Inventors:
David IRWIN, Thies SCHROEDER, Mark BORDEN, David PAK, Justin HOPKINS
Abstract: The present disclosure provides compositions and methods for the treatment of pathogen-induced and/or chemical-induced lung injury, for regenerating lung epithelial cells following lung injury, for treating cancer, and for sensitizing a subject suffering from cancer to a chemotherapeutic agent.
Abstract: The present invention relates to compounds and pharmaceutically acceptable salts thereof and formulations comprising the compounds or a pharmaceutically acceptable salts thereof that are useful in methods of preventing pancreatic beta cell degeneration or methods of treating a disorder associated with pancreatic beta cell degeneration, such as type I diabetes.
Type:
Application
Filed:
August 21, 2019
Publication date:
July 9, 2020
Inventors:
Andrew G. Reaume, Michael S. Saporito, Alexander R. Ochman
Abstract: The present invention provides methods of treating Type I or Type II diabetes in a mammal by administering an effective amount of insulin and an effective amount of a phenoxypyrimidinone compound to the mammal in need of such treatment, and formulations for carrying out the methods.
Type:
Application
Filed:
January 8, 2020
Publication date:
July 9, 2020
Inventors:
Andrew G. Reaume, Michael S. Saporito, Alexander R. Ochman
Abstract: The present invention provides an agent containing an orotic acid derivative that has high solubility in solvent and has superior physiological activity. The agent of the present invention is a melanin production inhibitor, whitening agent, fibroblast activator, collagen and/or elastin production promoter or wrinkle ameliorant containing as an active ingredient thereof an orotic acid derivative represented by the following general formula (1) or a salt thereof. In formula (1), R preferably represents a side chain of glutamic acid, glycine, histidine or aspartic acid. [In formula (1), R represents a side chain of a naturally-occurring amino acid and R may form, together with a nitrogen atom adjacent thereto through a single carbon atom, a hetero ring.
Abstract: The present invention provides compositions and methods for treating and preventing an A?-modulated disease and/or a Tauopathy. In certain embodiments, the invention provides an inhibitor of Fyn tyrosine kinase, and methods of using the same. In certain embodiments, the inhibitor of the invention inhibits A? oligomer induced signaling and reduces or halts the progression of Alzheimer's Disease.
Abstract: Combination therapies for treatment of cancer are provided. The disclosed methods comprise administration of a cyclin-dependent kinase inhibitor and a DNA methyltransferase S inhibitor to a mammal in need thereof.
Type:
Application
Filed:
March 17, 2020
Publication date:
July 9, 2020
Applicant:
TOLERO PHARMACEUTICALS, INC.
Inventors:
David J. Bearss, Steven L. Warner, Adam Siddiqui-Jain, Clifford J. Whatcott, Wontak Kim
Abstract: The present disclosure is directed to a method of treating prediabetes or type 1 or type 2 diabetes mellitus comprising administering to a subject in need thereof an effective amount of imeglimin, wherein the subject has chronic kidney disease.
Type:
Application
Filed:
March 9, 2020
Publication date:
July 9, 2020
Inventors:
Bill SYMONDS, Steve PISCITELLI, Karen SEGAL, Ruby HOLDER, Sophie BOZEC, Sebastien BOLZE, Pascale FOUQUERAY, Christophe ARBET-ENGELS, Julie DUBOURG, Paul STRUMPH, Brandon Dale SWIFT, Margaret Smith FLETCHER
Abstract: Phenoxy acetic acids and phenyl propionic acids and their use in improving mitochondrial energy output in a subject are provided herein. The present compounds are activators of PPAR? and may be useful for treating conditions mediated by the same.
Type:
Application
Filed:
November 8, 2019
Publication date:
July 9, 2020
Inventors:
Per SAUERBERG, Pavel PIHERA, Zdenek POLIVKA, Miroslav HAVRANEK, Ingrid PETTERSON, John Patrick MOGENSEN
Abstract: Disclosed herein are methods for treating cancer in a subject in need thereof by administering an agent or pharmaceutically acceptable derivative thereof, optionally with another agent, induces prostate apoptosis response-4 (Par-4) production by non-cancerous normal cells, to promote apoptosis in cancer cells.
Abstract: The present disclosure is directed, among other things, to the surprising and unexpected efficacy provided by select V2R antagonists in significantly reducing the cell proliferation levels of clear cell renal cell carcinoma. Thus, the present disclosure provides methods, uses, and medicaments that include such select V2R antagonists for utility in treating clear cell renal cell carcinoma.
Abstract: A method of forming a dietary supplement can include steps of creating a composition of matter comprising tianeptine, kava, and optionally, at least one of CDP Choline, and Alpha GPC; and providing the composition of matter in a liquid or solid form. The ingredient of tianeptine can be tianeptine sodium, tianeptine free acid, or both. Providing the composition of matter can include filling a container with the composition of matter.
Abstract: Methods and kits for treating oral mucositis are disclosed. The treatment comprises administering to a patient in need thereof a Reactive Oxygen Species scavenger in a pharmaceutically acceptable formulation.
Type:
Application
Filed:
February 27, 2020
Publication date:
July 9, 2020
Inventors:
David M. Rothstein, Chris Murphy, Vivien Wong, Glenn Kazo
Abstract: Provided are compositions comprising a benzodiazepine and a neurosteroid, containing one or both of the benzodiazepine and the neurosteroid in a subtherapeutic dose, and administration of such compositions for mitigation of an epileptic seizure. Further provided are compositions comprising a benzodiazepine, a neurosteroid, and an NMDA blocker, and administration of such compositions for mitigation of an epileptic seizure.
Type:
Application
Filed:
August 19, 2019
Publication date:
July 9, 2020
Inventors:
Michael A. ROGAWSKI, Isaac N. PESSAH, Zhengyu CAO, Pamela J. LEIN
Abstract: The present invention relates to certain cortexolone derivatives of formula (I) and the use of the same as antitumor active ingredients for the curative or adjuvant, or neoadjuvant or palliative treatment of precancerous lesions, dysplasias, metaplasias and tumor diseases, including malignant neoplasias and metastasis. The present invention also relates to pharmaceutical compositions comprising cortexolone derivatives of formula (I) as active ingredients and at least one physiologically acceptable excipient, and to the use of the pharmaceutical compositions as antitumor medicinal products.
Abstract: The present invention provides a solid preparation comprising, based on 100 parts by weight of the solid preparation, a self-emulsifying composition comprising 0.1 to 0.5 parts by weight of dutasteride, 6 to 110 parts by weight of oil and 6 to 110 parts by weight of a surfactant, and 5 to 185 parts by weight of a coating excipient having pores accommodating the self-emulsifying composition formed in a surface thereof, and a method of manufacturing the solid preparation.
Abstract: The present disclosure is directed to methods of treating cancer comprising administering dihydrotestosterone, a dihydrotestosterone derivative, a dihydrotestosterone promoter, or a combination thereof to a patient in need of treatment.
Abstract: Current therapeutic approach to treating heart allotransplantation rejection focus on immunosuppression protocols that carry harmful side effects after chronic use, which include global immune depression to the patient. The present inventors have discovered alternative and synergistic protocols based on inhibiting NF-?B and NLRP3 inflammasome-dependent IL-1?release with nitrated NSAID derivatives.
Type:
Application
Filed:
March 18, 2020
Publication date:
July 9, 2020
Inventors:
Carlos Batthyány, Gloria Virginia López, Carlos Escande, Williams Arturo Porcal Quinta, Germán Adrian Galliussi López, Marcelo Hill, Mercedes Segovia
Abstract: The present invention includes a composition and method of producing aspirin in situ, the method comprising: identifying a subject in need of aspirin or aspirin-like compounds; and providing the subject with a composition comprising: a source of methyl salicylate, an acetyl donor, and L-Arginine, wherein the composition is effective to produce aspirin-triggered resolvins in the subject without the deleterious effect of the aspirin or aspirin-like compounds in the stomach.
Abstract: Methods for prevention and treatment of asthma attacks involve the administration of one or more TRPV1 antagonists, one or more LPAr antagonists or preferably a combination of one or more TRPV1 antagonists and one or more LPAr antagonists. TRPV1 antagonists and/or LPAr antagonists or a combination of both inhibit or prevent carotid body activation during an acute asthma attack. TRPV1 antagonists, LPAr antagonists or a combination thereof are useful for preventing or ameliorating the symptoms of asthma attacks. Pharmaceutical compositions for use in treating asthma and more specifically for preventing or treating asthma attacks comprise a combination of a TRPV1 antagonist and an LPAr antagonist. Methods for making medicaments for such treatment are provided. Also provided are kits for treating asthma and for preventing or treating asthma attacks in which a TRPV1 antagonist and an LPAr antagonist are separately formulated for administration at the same time.
Type:
Application
Filed:
July 19, 2018
Publication date:
July 9, 2020
Inventors:
Richard J. A. WILSON, Nicholas JENDZJOWSKY, Arijit ROY
Abstract: Compositions and foods which contain (1) histidine and (2) vitamin B6 and/or carnosine are useful for treating, improving, and recovering from fatigue.
Abstract: Various methods and compositions for treating age-associated conditions and other medical conditions, such as muscle diseases, type 2 diabetes, and/or obesity are described. Methods of enhancing cellular uptake of NMN and stimulating NAD+ production are further described. Various mammalian cells and mammalian cell lines are described including those comprising a cDNA encoding a Slc12a8 protein. Gene therapy vectors comprising a nucleic acid encoding Slc12a8 and non-human animals comprising an inactivating mutation in a Slc12a8 gene are also disclosed. Also described are methods for screening a candidate compound to identify compounds that promote NMN transport.
Abstract: The present invention is directed to a dietary supplement comprising palatinose or a derivative thereof. The dietary supplement may be a nutritional product, a sports performance product, a weight loss product or a meal replacement product. The present invention is also directed to a method of increasing the absorption of a compound into the bloodstream, cells and tissue comprising administering palatinose, or a derivative thereof, in combination with the compound. The present invention also relates to a diluent for parenteral compounds. The diluent comprises palatinose or a derivative thereof. Another aspect of the present invention is directed to a method of decreasing the recovery time to pre-performance levels of total adenosine triphosphate (ATP) levels in a mammal comprising administering palatinose, or a derivative thereof, to the mammal. The present invention is further directed to a method of supplying a compound to a diabetic patient, burn victim patient or trauma victim patient.