Abstract: Use of colchicine to inhibit tumor growth and metastases in mammalian subjects comprising the administration of the compositions and formulations are provided. The described colchicine compositions and formulations include sustained release, and multimodal release compositions and formulations suitable for alone or in combination with additional pharmaceutically active agents useful in treating tumor growth and metastases.
Abstract: The present invention relates to an injection for protecting ischemic myocardium, and preparation method for the injection. The emulsion for injection comprises, in parts by weight: 1-5 parts of N-suberoylanilide hydroxamic acid, 0.2-12.5 parts of n emulsifying agent, 2-100 parts of oil for injection, 0.02-5 parts of a solubilizer, 0.03-0.4 part of oleic acid, 0.4-12.5 parts of glycerinum, and the balance being water for injection. The emulsion for injection can effectively be used for increasing local drug concentration of the N-suberoylanilide hydroxamic acid in lipophilic organs such as angiocarpy and/or tissues before a cardiac interventional operation, increasing the bioavailability of the N-suberoylanilide hydroxamic acid, reducing general side effects of the N-suberoylanilide hydroxamic acid, realizing effective protection on myocardium under an ischemic or reperfusion injury state, and reducing or avoiding the occurrence of myocardial infarction.
Abstract: The invention relates to compounds exhibiting kallikrein inhibitory activity, and to compositions comprising at least one of these compounds for use in the treatment of diseases or disorders in which kallikrein activity is dysregulated, particularly neurodegenerative and inflammatory diseases.
Type:
Application
Filed:
February 13, 2019
Publication date:
February 18, 2021
Inventors:
CHAHRAZADE EL AMRI, FERYEL SOUALMIA, NICOLAS MASURIER, SABRINA AÏT AMIRI, BRAHIM NAIT OUMESMAR, CYRILLE DEBOUX
Abstract: The disclosure discloses a fatty acid synthase inhibitor and application thereof and belongs to the technical field of medical biology. The fatty acid synthase inhibitor of the disclosure can significantly inhibit the activity of fatty acid synthase without affecting normal expression, and adjust the ratio of fatty acids in cells. The fatty acid synthase inhibitor of the disclosure has a good tumor proliferation inhibitory effect, can arrest the growth cycle of tumor cells in the interphase, prevent tumor cell division, inhibit tumor cell proliferation, promote tumor cell apoptosis and exert a tumor treatment effect, can be used to treat tumors and metabolism related diseases, and has an important clinical application prospect.
Abstract: Compositions including small molecule mitofusin activators are described. The mitofusin activators are useful for treating diseases or disorders associated with a mitochondria-associated disease, disorder, or condition such as diseases or disorders associated with mitofusin 1 (MFN1) and/or mitofusin 2 (MFN2), or mitochondrial dysfunction. Methods of treatment, pharmaceutical formulations, and screening methods for identifying compounds that activate mitochondrial fusion are also described.
Abstract: The present disclosure relates to (a) an improved pharmaceutical composition comprising a levodopa active agent and a carbidopa active agent (b) methods of producing the pharmaceutical composition and (c) methods of treating Parkinson's disease and associated conditions comprising administering the pharmaceutical composition to a subject with Parkinson's disease.
Type:
Application
Filed:
March 18, 2020
Publication date:
February 18, 2021
Inventors:
Rajkumar CONJEEVARAM, Alexandru DEAC, Ye HUANG, Sean E. MACKEY, Randy A. MENGES, Jayne ZIMMERMAN
Abstract: Compounds of Formula (I), and pharmaceutically effective salts thereof; wherein R1-R14, m, n, o, p, q and r are as defined herein, are provided for treatment of for increasing insulin sensitivity, reducing insulin resistance, preventing insulin resistance and treating insulin resistance disorders.
Type:
Application
Filed:
July 17, 2020
Publication date:
February 18, 2021
Inventors:
Salim Merali, Carlos A. Barrero, Wayne e. Childers, George c. Morton
Abstract: The present disclosure provides for treatments of restless legs syndrome (RLS) or one or more symptoms associated with RLS comprising administering leucine, acetyl-leucine or a pharmaceutically acceptable salt thereof.
Abstract: The invention relates to supramolecular metal coordinated liothyronine (triiodothyronine, T3) compositions, methods of preparing such compositions, methods of purifying and formulating supramolecular metal coordinated liothyronine, and methods of treating hypothyroidism and other disease states using such compositions.
Type:
Application
Filed:
April 4, 2019
Publication date:
February 18, 2021
Inventors:
John D. PRICE, Thomas PICCARIELLO, Michaela E. MULHARE
Abstract: The present disclosure is directed to pharmaceutical compositions comprising a nitrogen mustard and a cyclodextrin derivative, and methods of making and using the same.
Abstract: Compositions including odd chain saturated fatty acids, and salts and derivatives thereof, and methods for treatment or prophylaxis of conditions related to aging are provided, including compositions and methods for treating conditions related to aging, including hypercholesterolemia, thrombosis, fibrosis, wound healing, hyperglobulinemia, and hypersensitivity disorders.
Abstract: Pharmaceutical combinations and methods for using such combinations to treat depression are disclosed. In various embodiments (he pharmaceutical combinations include combinations of omega-3 fatty acids, pharmacological sleep agents, and non-pharmacological sleep therapies, and may include other ingredients such as antidepressants. The present invention relates pharmaceutical combinations and methods for their use to treat depression.
Abstract: In various embodiments, the present invention provides methods of treating and/or preventing cardiovascular-related disease and, in particular, a method of blood lipid therapy comprising administering to a subject in need thereof a pharmaceutical composition comprising eicosapentaenoic acid or a derivative thereof.
Type:
Application
Filed:
September 1, 2020
Publication date:
February 18, 2021
Inventors:
Mehar Manku, Ian Osterloh, Pierre Wicker, Rene Braeckman, Paresh Soni
Abstract: This invention concerns a dosage form comprising a therapeutically effective amount of A19-144 or A2-73 and a therapeutically effective amount of at least one AED. This invention further encompasses a method of treating a subject in need of such treatment comprising administering a therapeutically effective amount of A19-144 or A2-73 in conjunction with any therapeutically effective amount of an AED.
Type:
Application
Filed:
October 26, 2020
Publication date:
February 18, 2021
Applicant:
ANAVEX LIFE SCIENCES CORP.
Inventors:
Christopher U. Missling, Cameron Durrant
Abstract: This invention discloses a medicinal composition of matter that effectively provide a nootropic effect beyond the effects simple obtain by cannabinoids alone. And, effectively reduce anxiety due to ingestion of xanthines containing oral products.
Abstract: Described herein are compositions for topical use comprising active agents to provide pain relief. The compositions comprise a magnesium salt, a cannabinoid and at least one additional topical analgesic agent. Additionally described herein are methods for treating pain comprising administering to a person in need thereof a composition comprising a pharmaceutically effective amount of a cannabinoid, a magnesium salt and at least one of: methyl salicylate, and menthol.
Abstract: This disclosure pertains to devices and methods for administering one or more active ingredients, e.g., cannabinoids, terpenes, etc. In particular, the devices and methods disclosed herein administer one or more cannabinoids in a mist for transmucosal and transdermal absorption. In one embodiment, the device contains compositions comprising purified active ingredients (e.g., cannabinoids, terpenes, etc.) and/or unique combinations thereof for delivery via a mist for transmucosal and transdermal adsorption. In one embodiment, the device contains two separate compositions in separate chambers, wherein each composition comprises one or more of the active ingredients. In one embodiment, a composition in one chamber comprises a purified cannabinoid and the composition in the other chamber comprises a purified terpene. In an embodiment, the device operates without heating the active ingredients.
Abstract: The present invention relates to the use of Luteolin 2-(3,4-dihydroxyphenyl)-, 5,7dihydroxy-4-chromenone in a method for the treatment of endometriosis and symptoms thereof. The present invention further relates to compositions comprising Luteolin according to any administration route, alone or associated to other substances, such as for example antiandrogens, antiprogestins, progestins.
Abstract: The disclosure relates to a pharmaceutical composition including daphnetin, a method for improving aortic endothelial cell function, and use of daphnetin in preparation of a medicine for improving aortic endothelial cell function. The daphnetin is capable of inhibiting inflammatory response of the human aortic endothelial cells caused by a saturated fatty acid, and preventing an occurrence and progression of atherosclerosis. The daphnetin is capable of reducing human aortic endothelial inflammation caused by a saturated fatty acid, for example, reducing the mRNA levels of interleukin-6 (IL-6), and is capable of effectively protecting the function of mitochondria in human aortic endothelium from being damaged by a saturated fatty acid.
Type:
Application
Filed:
October 21, 2019
Publication date:
February 18, 2021
Applicant:
XI'AN JIAOTONG UNIVERSITY
Inventors:
JIAN-GANG LONG, XU-YUN LIU, JIAN-KANG LIU
Abstract: The present invention relates to (+)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane and pharmaceutically acceptable salts thereof, compositions comprising (+)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane or a pharmaceutically acceptable salt thereof, and methods for treating or preventing an alcohol-related or addictive disorder. The (+)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.
Type:
Application
Filed:
May 4, 2020
Publication date:
February 18, 2021
Inventors:
Anthony Alexander McKinney, Franklin Porter Bymaster
Abstract: Some embodiments include compositions and methods of using or identifying compounds that modulate the activity of the granulocyte colony-stimulating factor receptor (GCFR). Some embodiments include use of compounds to treat certain disorders, such as hematopoietic or neurological disorders.
Type:
Application
Filed:
July 10, 2020
Publication date:
February 18, 2021
Inventors:
Lin Zhi, Keith Marschke, Virginia H. Grant, Steven L. Roach, Yixing Shen, Jason C. Pickens, Bijan Pedram, Cornelis Arjan van Oeveren, Lino J. Valdez, Andrew R. Hudson
Abstract: Disclosed herein are self-emulsifying compositions and formulations of Dimdolylmethane (“DIM”) and certain derivatives of DIM, their uses and methods of making. In particular, the disclosed compositions comprise a DIM-related indole as an active agent and a carrier, wherein the carrier comprises a solvent, one or more surfactants with an HLB of greater than 7, and one or more co-surfactants with an HLB equal to or less than 7. In certain aspects of the invention, the compositions disclosed herein show improved bioavailability.
Abstract: Methods of treatment, pharmaceutically acceptable solutions, and implantable devices are provided for the intrathecal treatment of AED-resistant seizures using levetiracetam.
Type:
Application
Filed:
August 12, 2020
Publication date:
February 18, 2021
Inventors:
Augusto Mitidieri, Elisabetta Donati, Clara Bianchi, Barbara Piccagli
Abstract: The present invention generally relates to artemisinin/dihydroartemisinin (DHA) derivatives, and their use for therapy, in particular cancer therapy. These tumor-homing artemisinin derivatives (THAD) comprise three moieties: an artemisinin/DHA or a derivative thereof, a heptamethine carbocyanine dye (HMCD) residue, and a linker that conjugates the HMCD dye residue to the artemisinin residue. The THAD include compounds wherein the linker is linked to one or two DHA residue(s) via one or more ether bonds, and wherein the linker is linked to two DHA residues via two bonds independently selected from ester, carbamate and thiocarbamate. The THAD of the invention provide improved growth inhibition of cancer cells. The present invention also relates to improved methods of cancer therapy wherein a THAD is administered to a cancer patient. In embodiments, one or more THAD may be co-administered in a coordinated administration schedule.
Type:
Application
Filed:
July 10, 2020
Publication date:
February 18, 2021
Applicant:
Da Zen Theranostics, Inc.
Inventors:
Leland W.K. Chung, Gina C.Y. Chu, Yi Zhang
Abstract: The present invention refers to a pharmaceutical composition that comprises the synergistic combination of an antagonist agent of the NMDA receptor, such as the active principle: ketamine and an agonist agent of the MT1 and MT2 melatonin receptors, as is the active principle: melatonin, which are in a pharmaceutical composition, which is indicated for the control and treatment of psychiatric diseases.
Type:
Application
Filed:
February 28, 2019
Publication date:
February 18, 2021
Applicant:
INSTITUTO NACIONAL DE PSIQUIATRÍA "RAMÓN DE LA FUENTE MUÑIZ"
Inventors:
Gloria Acacia BENÍTEZ KING, Margarita Lucía DUBOCOVICH JERKOVICH, Citlali TRUETA SEGOVIA, Marcela VALDÉS TOVAR, Brian Daniel QUERO CHÁVEZ, Ana María DORANTES BARRÓN, Rosa ESTRADA REYES
Abstract: The present invention relates to stable amorphous form of sacubitril valsartan trisodium complex and its solid dispersion compounds, processes for their preparation and pharmaceutical composition comprising the same. The present invention also relates to an improved process for the preparation of sacubitril sodium and its use in the preparation of sacubitril valsartan trisodium complex.
Abstract: Methods for treating fecal incontinence by administering tc a subject in need thereof compositions including oxymetazoline as an active ingredient. Kits including compositions of oxymetazoline suitable for topical application, for the treatment of fecal incontinence.
Abstract: The present invention provides a technique that allows a pharmaceutical composition, preferably for external use, containing luliconazole or the like to contain luliconazole or the like at a high concentration, and suppresses the precipitation thereof over time. The present invention uses a polyethylene glycol having an average molecular weight of 380 to 420 represented by a formula HOCH2(CH2OCH2)nCH2OH (where n is an integer), ethanol, benzyl alcohol, lactic acid, propylene carbonate, and acetone in combination with the luliconazole or the like.
Abstract: The present invention provides a new compositions and methods to enable the safe administration of pyridostigmine to mammalian subjects, including those with myasthenic syndromes including Myasthenia Gravis, with said compositions comprising combinations, including fixed-dose combinations, of an antagonist of the 5-hydroxytryptamine subtype-3 receptor (“5HT3-antagonist”) with an effective dose of pyridostigmine. The compositions and methods of the present invention provide for an increase in the tolerable dose of pyridostigmine over that of pyridostigmine when administered alone.
Abstract: An extended release oral dosage form comprising as active substance tacrolimus or a pharmaceutically active analogue thereof for a once daily immunosuppressive treatment of a patient in need thereof, preferable a kidney or liver transplant patient. The dosage form releases the active substance over an extended period of time. It also provides improved pharmacokinetic parameters due to an extended and constant in vivo release including substantial decreased peak concentrations, despite increased bioavailability, substantial extended times for maximal concentration, and higher minimal concentrations when compared with conventional immediate release dosage forms and a recent modified release tacrolimus dosage form.
Type:
Application
Filed:
October 30, 2020
Publication date:
February 18, 2021
Inventors:
Robert D. GORDON, Per HOLM, Anne-Marie LADEMANN, Tomas NORLING
Abstract: An extended release oral dosage form comprising as active substance tacrolimus or a pharmaceutically active analogue thereof for a once daily immunosuppressive treatment of a patient in need thereof, preferable a kidney or liver transplant patient. The dosage form releases the active substance over an extended period of time. It also provides improved pharmacokinetic parameters due to an extended and constant in vivo release including substantial decreased peak concentrations, despite increased bioavailability, substantial extended times for maximal concentration, and higher minimal concentrations when compared with conventional immediate release dosage forms and a recent modified release tacrolimus dosage form.
Type:
Application
Filed:
October 30, 2020
Publication date:
February 18, 2021
Inventors:
Robert D. GORDON, Per HOLM, Anne-Marie LADEMANN, Tomas NORLING
Abstract: The present invention relates to a compound of the following formula (A): or a pharmaceutically acceptable salt or hydrate thereof, for use in the prevention or treatment of a disease associated with a mitochondrial dysfunction.
Type:
Application
Filed:
November 2, 2020
Publication date:
February 18, 2021
Applicant:
Amabiotics
Inventors:
Antoine Danchin, Agnieszka Sekowska, Patrice Garnier
Abstract: Provided are a ?-lactamase inhibitor of formula (I), or an ester, a stereoisomer or a pharmaceutically acceptable salt thereof, and a method of preparing the same. Further provided is a pharmaceutical composition comprising the ?-lactamase inhibitor of formula (I), or the ester, the stereoisomer or pharmaceutically acceptable salt thereof. In addition, the present invention relates to a method for treating diseases caused by bacterial infection, which comprises administering the ?-lactamase inhibitor of formula (I), or the ester, the stereoisomer or the pharmaceutically acceptable salt thereof to a patient or a subject in need.
Type:
Application
Filed:
January 24, 2019
Publication date:
February 18, 2021
Inventors:
Yuchuan WU, Shaoqiang HUANG, Xi CHEN, Yonghan HU, Xiao LIU
Abstract: A macrocycle represented by formula (I) and a pharmaceutical composition comprising the macrocycle, or a crystalline form, pharmaceutically acceptable salt, hydrate or solvent compound, stereoisomer, prodrug, or isotopic variant of the macrocycle. The macrocycle and the composition thereof inhibit a protein kinase.
Abstract: The present disclosure relates to methods of treating gastrointestinal stromal tumors to a subject in need thereof, comprising administering to the subject a therapeutically effective amount of ripretinib or a pharmaceutically acceptable salt thereof.
Type:
Application
Filed:
September 22, 2020
Publication date:
February 18, 2021
Inventors:
Rodrigo Ruiz Soto, Oliver Rosen, Jama Pitman
Abstract: Provided are methods of administering a vesicular monoamine transport 2 (VMAT2) inhibitor chosen from valbenazine and (+)-?-3-isobutyl-9,10-dimethoxy-1, 3,4, 6,7,11 b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-ol, or a pharmaceutically acceptable salt and/or isotopic variant thereof, to a patient in need thereof wherein the patient is a CYP2D6 poor metabolizer.
Type:
Application
Filed:
October 26, 2020
Publication date:
February 18, 2021
Inventors:
Christopher F. O`Brien, Haig P. Bozigian
Abstract: Provided are methods and compositions for the prevention and/or treatment of viral conditions, virally-induced conditions and inflammatory conditions. The methods can comprise administering to a subject a viral inducing agent with an antiviral agent, and optionally an additional agent. The viral inducing agent can be a HDAC inhibitor administered orally.
Abstract: Provided herein are pharmaceutical compositions comprising a class of calcium channel blockers and at least one chelating agent. More specifically, the pharmaceutical compositions comprise at least one 1,4-dihydropyridine (DHP) compound and at least one chelating agent. The chelating agents used in this disclosure can decrease the degradation of the constituent DHPs of the DHP compositions. The DHP compositions can be used to treat cardiovascular disorders and are more stable for prolonged periods of time.
Type:
Application
Filed:
March 11, 2020
Publication date:
February 18, 2021
Inventors:
Daniel Walter Wehring, Meng Zhong, Saral Pinkal Patel, Bindhu Madhavi Rayaprolu
Abstract: The presently-disclosed subject matter generally relates to methods for sensitizing chemotherapy resistant tumors using a synergistic drug combination. The presently-disclosed subject matter further relates to methods for sensitizing a drug resistant cancer cell to chemotherapy, comprising: contacting the drug resistant cancer cell with an effective amount of an agent capable of increasing cell surface expression of GRP78 and an agent capable of increasing soluble prostate apoptosis response 4 (Par-4).
Abstract: The invention is directed to the treatment of tauopathic neurodegenerative conditions and the underlying processes thereof. Based on the discovery that Rhes acts as a negative regulator of normal tau clearance, the compositions and methods of the invention may be applied to inhibit Rhes and reduce pathogenic tau aggregation. Rhes may be disrupted by disrupting RAS2D gene expression or reducing the abundance of Rhes protein in neurons. Additionally, post-translational modifications of Rhes may be targeted, including the disruption of Rhes farnesylation by the administration of farnesyltransferase inhibitors.
Type:
Application
Filed:
October 30, 2020
Publication date:
February 18, 2021
Applicant:
The Regents of the University of California
Abstract: The present invention relates to the discovery of a novel opioid modulator effective in reducing pharmacologically induced weight gain associated with atypical antipsychotic use. The present invention provides methods of reducing antipsychotic induced weight gain, methods for suppressing food intake and reducing ghrelin levels induced by atypical antipsychotic medications in a patient.
Abstract: The present disclosure provides acetate salts of buprenorphine, and its anhydrates, solvates, hydrates, and crystalline forms thereof, where the acetate salts of buprenorphine are essentially free of impurities. The disclosure further provides method of preparing the acetate salts, buprenorphine free base prepared from the acetate salts, other salts prepared from the free base, and pharmaceutical compositions thereof essentially free of impurities.
Type:
Application
Filed:
October 29, 2020
Publication date:
February 18, 2021
Applicant:
Rhodes Technologies
Inventors:
C. Frederick M. HUNTLEY, Erik Wayne KATAISTO, Helge Alfred REISCH, Archana SHARMA
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: Disclosed herein are methods of reducing or preventing thrombocytopenia, in a clinically relevant manner, that is caused by chemotherapy or radiation therapy by administering plinabulin to a subject.
Type:
Application
Filed:
January 23, 2019
Publication date:
February 18, 2021
Inventors:
Lan Huang, Ramon Mohanlal, George Kenneth Lloyd
Abstract: The present invention relates to a novel pentafluorosulfanyl-substituted amide compound that regulates or inhibits indoleamine 2,3-dioxygenase (IDO) activity, its preparation method and its application in medicine. Specifically, the present invention relates to a compound represented by general formula (I) and pharmaceutically acceptable salt thereof, a pharmaceutical composition containing the compound or pharmaceutically acceptable salt thereof, application of the compound or pharmaceutically acceptable salt thereof for treating and/or preventing related disorders mediated by IDO, especially tumors, and a method for preparing the compound or pharmaceutically acceptable salt thereof. The present invention also relates to the preparation of the compound or pharmaceutically acceptable salt thereof or a pharmaceutical composition containing the compound or pharmaceutically acceptable salt thereof for the treatment and/or prevention of IDO-mediated related disorders, especially for use in tumor treatment.
Abstract: Provided are compounds that target the lanthionine synthetase C-like protein 2 pathway. The compounds can be used to treat a number of conditions, including infectious disease, autoimmune disease, diabetes, and a chronic inflammatory disease.
Type:
Application
Filed:
October 20, 2020
Publication date:
February 18, 2021
Applicant:
Landos Biopharma, Inc.
Inventors:
Josep Bassaganya-Riera, Adria Carbo Barrios, Richard Gandour, Julian D. Cooper, Raquel Hontecillas
Abstract: The present invention includes 2-(4-Methyl-[1,4]diazepan-1-yl)-5-oxo-5H-7-thia-1,11b-diaza-benzo[c]fluorene-6-carboxylic acid (5-methyl-pyrazin-2-ylmethyl)-amide (Compound I) or a pharmaceutically acceptable salt thereof for use in treating cancer with PALB2 mutation and/or BRCA2 mutation.
Abstract: Provided herein is a pharmaceutical combination comprising (a) a poly-(ADP-ribose)-polymerase (PARP) inhibitor and (b) a second agent comprising (i) an inhibitor of glycogen synthase kinase 3 (GSK-3) or (ii) an inhibitor of disrupter of telomeric silencing 1-like (DOT1L). Also provided is a method of treating a subject suffering from acute myeloid leukaemia, comprising administering to the subject a therapeutically effective amount of the pharmaceutical combination.
Abstract: The present invention relates to novel compounds, pharmaceutical compositions containing such compounds and to their use in therapy.
Type:
Application
Filed:
January 7, 2020
Publication date:
February 18, 2021
Inventors:
Dominique Amans, Stephen John Atkinson, Lee Andrew Harrison, David Jonathan Hirst, Robert Peter Law, Matthew Lindon, Alexander Preston, Jonathan Thomas Seal, Christopher Roland Wellaway