Abstract: The present invention aims to provide a composition for promoting lipid metabolism, a composition for suppressing fat accumulation, and the like, which contain, as an active ingredient, a substance that is thermally stable and adequately water-soluble and that has lipid metabolism-promoting action. The present invention relates to a composition for promoting lipid metabolism containing isoxanthohumol.
Abstract: This disclosure is directed to non-aromatic difluoro analogues of resorcylic acid lactones, pharmaceutical compositions comprising non-aromatic difluoro analogues of resorcylic acid lactones, and methods of treatment comprising non-aromatic difluoro analogues of resorcylic acid lactones.
Type:
Application
Filed:
August 30, 2019
Publication date:
December 19, 2019
Inventors:
Mitchell P. Croatt, Lara Fakhouri, Nicholas H. Oberlies, Cedric Pearce
Abstract: A pharmaceutical composition having an analgesic, anaesthetic and antiseptic action, a method for producing the pharmaceutical composition and a method for treatment of otitis and other ear injuries. The group of inventions relates to medicine and can be used in the treatment of otitis and other ear injuries. The invention relates to a pharmaceutical composition in the form of ear drops, containing 4 wt. % phenazone or propyphenazone, 2 wt. % articaine and 0.05-0.2 wt. % benzalkonium chloride.
Abstract: The present invention relates to compounds, compositions, and methods for modulating skin pigmentation and treating or preventing UV-induced skin damage, erythema, aging of the skin, sunburn, and hyperpigmentation in a subject. The compounds, compositions, and methods of the present invention generally involve Malassezia-derived compounds, including malassezin and indirubin, and/or chemical analogs thereof. Other applications of the compounds and compositions disclosed herein include, but are not limited to, improving hyperpigmentation caused by a hyperpigmentation disorder, inducing melanocyte apoptosis, and modulating arylhydrocarbon receptor (AhR) activity, melanogenesis, melanin production, melanosome biogenesis, melanosome transfer, melanocyte activity, and melanin concentration.
Abstract: A method is provided for lowering blood sugar in a subject in need thereof by administering a dipeptidyl peptidase-4 inhibitor pharmaceutical composition to a subject qualified for over-the-counter access to the dipeptidyl peptidase-4 inhibitor pharmaceutical composition. In some embodiments, the dipeptidyl peptidase-4 inhibitor pharmaceutical composition includes saxagliptin, sitagliptin, linagliptin, alogliptin, or a pharmaceutically acceptable salt thereof. In some embodiments, the dipeptidyl peptidase-4 inhibitor pharmaceutical composition includes (1S,3S,5S)-2-[(2S)-2-amino-2-(3-hydroxy-1-adamantyl)acetyl]-2-azabicyclo[3.1.0]hexane-3-carbonitrile or a pharmaceutically acceptable salt thereof.
Abstract: The present disclosure relates provides compounds according to Formula I or Formula II as well as compositions including such compounds useful for the prevention of schistosomiasis infection and/or swimmer's itch.
Type:
Application
Filed:
June 19, 2019
Publication date:
December 19, 2019
Inventors:
PHILLIP A. NEWMARK, Jonathan V. Sweedler, Ning Yang, Jiarong Gao, Peter Yau
Abstract: The invention includes an amount of (3aR)-1,3a,8-trimethyl-1,2,3,3a,8,8a-hexahydropyrrolo[2,3-b]indol-5-yl phenylcarbamate for administering to a subject and also a method of preventing or treating neurotoxicity or neurodegenerative processes in a subject in need thereof using the amount thereof.
Abstract: Methods for treatment of wAMD with an active CNV lesion of less than 50% of the total lesion size and pharmaceutical compositions for the use therein are disclosed.
Abstract: The present invention relates to the use of DBH inhibitors (e.g., disulfiram and Nepicastat), and pharmaceutical compositions thereof, for treating subjects with certain types of memory loss, for instance memory loss associated with a neurodegenerative disease, disorder, or condition, such as Alzheimer's Disease.
Abstract: The present invention is directed to pyrazole derivatives, pharmaceutical compositions comprising the compounds and the use of the compounds or the compositions in the treatment of various diseases.
Type:
Application
Filed:
February 27, 2018
Publication date:
December 19, 2019
Inventors:
Stephen John ATKINSON, Emmanuel Hubert DEMONT, Lee Andrew HARRISON, Gemma Michele LIWICKI, Simon Christopher Cranko LUCAS, Alexander G. PRESTON, Jonathan Thomas SEAL, Ian David WALL, Robert J. WATSON
Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
Type:
Application
Filed:
December 21, 2018
Publication date:
December 19, 2019
Inventors:
Kamlesh Jagdis BALA, Andrew BREARLEY, James DALE, Anne-Marie EDWARDS, Mahbub AHMED, David PORTER, Robert Alexander PULZ, Lisa Ann ROONEY, David Andrew SANDHAM, Duncan SHAW, Nichola SMITH, Jessica Louise TAYLOR, Roger John TAYLOR, Thomas Josef Troxler, Joe WRIGGLESWORTH
Abstract: Disclosed are compounds, compositions and methods for treating of diseases, syndromes, conditions, and disorders that are affected by the modulation of MALT1. Such compounds are represented by Formula (I) as follows: wherein R1, R2, R3, R4, R5, R6, R7, G1 and G2, are defined herein.
Type:
Application
Filed:
June 13, 2019
Publication date:
December 19, 2019
Inventors:
Tianbao LU, Peter J. CONNOLLY, Maxwell David CUMMINGS, Gaston Stanislas Marcella DIELS, Jan Willem THURING, Ulrike PHILIPPAR, James Patrick EDWARDS, Didier Jean-Claude BERTHELOT, Tongfei WU
Abstract: Disclosed is an isoquinolinone compound as shown in Formula (I) or a stereoisomer, pharmaceutically acceptable salt, solvate or crystal thereof, and a preparation method thereof, and use thereof in the preparation of drugs for treating or preventing viral infectious diseases caused by the hepatitis B virus (HBV) and other viruses, in particular, use thereof in drugs as HBV surface antigen inhibitors and HBV DNA production inhibitors. The compound has a significant activity in inhibiting hepatitis B surface antigen and hepatitis B DNA, and is possible to significantly improve the probability of curing hepatitis B by administration in combination with nucleoside drugs or other drugs in the future, and has good clinical application prospects.
Type:
Application
Filed:
July 28, 2017
Publication date:
December 19, 2019
Inventors:
Li Chen, Peibin Zhai, Qing Shao, Jin Wu, Xiaowen Li
Abstract: An application of berberine in preparation of drugs for prevention and treatment of pulmonary hypertension, cardiac failure caused by pulmonary hypertension and in-stent restenosis and antithrombotic drugs. Berberine can inhibit stimulation of noradrenaline to pulmonary arterial smooth muscle cells, improve right ventricular function, reduce mean pulmonary arterial pressure, and prevent and treat in-stent restenosis and stent thrombosis.
Abstract: Provided are methods of administering a vesicular monoamine transport 2 (VMAT2) inhibitor chosen from valbenazine and (+)-?-3-isobutyl-9,10-dimethoxy-1,3,4,6,7,11b-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 10, 2017
Publication date:
December 19, 2019
Inventors:
Christopher F. O`Brien, Haig P. Bozigian
Abstract: The present technology is directed to one or more compositions comprising serdexmethylphenidate conjugates and unconjugated d-methylphenidate and/or a pharmaceutically acceptable salt thereof. The present technology also relates to one or more compositions and oral formulations comprising serdexmethylphenidate conjugates and unconjugated d-methylphenidate and/or a pharmaceutically acceptable salt thereof. The present technology also relates to one or more methods of using compositions comprising serdexmethylphenidate conjugates and unconjugated d-methylphenidate and/or a pharmaceutically acceptable salt thereof. The present technology additionally relates to one or more pharmaceutical kits containing a composition comprising serdexmethylphenidate conjugates and unconjugated d-methylphenidate and/or a pharmaceutically acceptable salt thereof.
Type:
Application
Filed:
June 6, 2019
Publication date:
December 19, 2019
Inventors:
Sven Guenther, Guochen Chi, Travis Mickle
Abstract: The present technology is directed to one or more compositions comprising serdexmethylphenidate conjugates and unconjugated d-methylphenidate and/or a pharmaceutically acceptable salt thereof. The present technology also relates to one or more compositions and oral formulations comprising serdexmethylphenidate conjugates and unconjugated d-methylphenidate and/or a pharmaceutically acceptable salt thereof. The present technology also relates to one or more methods of using compositions comprising serdexmethylphenidate conjugates and unconjugated d-methylphenidate and/or a pharmaceutically acceptable salt thereof. The present technology additionally relates to one or more pharmaceutical kits containing a composition comprising serdexmethylphenidate conjugates and unconjugated d-methylphenidate and/or a pharmaceutically acceptable salt thereof.
Type:
Application
Filed:
June 6, 2019
Publication date:
December 19, 2019
Inventors:
Sven Guenther, Guochen Chi, Travis Mickle
Abstract: Disclosed are compounds, compositions and methods for treating of diseases, syndromes, conditions, and disorders that are affected by the modulation of MALT 1. Such compounds are represented by Formula (I) as follows: wherein R1, R2, R3, R4, R5, and G, are defined herein.
Type:
Application
Filed:
June 13, 2019
Publication date:
December 19, 2019
Inventors:
Tianbao Lu, Peter J. Connolly, Maxwell David Cummings, Joseph Kent Barbay, Kevin D. Kreutter, Tongfei Wu, Gaston Stanislas Marcella Diels, Jan Willem Thuring, Ulrike Philippar, James Patrick Edwards, Fang Shen
Abstract: A pharmaceutical composition which comprises a therapeutically effective amount of a aminopyridine dispersed in a release matrix, including, for example, a composition that can be formulated into a stable, sustained-release oral dosage formulation, such as a tablet which provides, upon administration to a patient, a therapeutically effective plasma level of the aminopyridine for a period of at least 12 hours, preferably 24 hours or more and the use of the composition to treat various neurological diseases.
Type:
Application
Filed:
August 29, 2019
Publication date:
December 19, 2019
Inventors:
Sean Cunningham, Seamus Mulligan, Michael Myers
Abstract: Disclosed herein is use of one or more aminopyridines in methods and compositions for treatment of impairments in gait or balance in patients with multiple sclerosis.
Type:
Application
Filed:
August 29, 2019
Publication date:
December 19, 2019
Applicant:
Acorda Therapeutics, Inc.
Inventors:
Gabriel Pardo, Gustavo Adolfo Suarez Zambrano, Cecilie Fjeldstad
Abstract: The invention relates to pharmaceutical compositions comprising PPAR agonists and Nrf2 activators and methods of using combinations of PPAR agonists and Nrf2 activators for treating diseases such as psoriasis, asthma, multiple sclerosis, inflammatory bowel disease, and arthritis.
Abstract: This invention relates to a pharmaceutical preparation comprising nicotinamide in combination with phosphate lowering agents (phosphate binders) for the treatment of elevated serum phosphate levels resulting particularly from kidney failure, especially in patients undergoing hemodialysis treatment, as well as to a pharmaceutical composition comprising a pharmaceutically effective amount of a combination of nicotinamide with phosphate binders together with pharmaceutically acceptable carriers.
Type:
Application
Filed:
October 27, 2016
Publication date:
December 19, 2019
Applicant:
MEDICE Arzneimittel Putter GmbH & Co. KG
Abstract: Provided herein are solid dispersions of (R)—N-((4-methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methy 1)-2-methyl-(1-(1-(2,2,2-trifluoroethyl)piperidin-4-yl)ethyl)-1H indole-3-carboxamide, pharmaceutically acceptable compositions comprising the dispersions, and methods of using said dispersions and compositions in the treatment of various conditions.
Type:
Application
Filed:
January 18, 2018
Publication date:
December 19, 2019
Inventors:
Alisha Arrigo, Donald Corson, Jean-Christophe Harmange
Abstract: In accordance with the present invention, the immunoregulatory activity of low doses of P4N was investigated. Unlike previously described antitumor drugs, low dose P4N, in doses of about 1 to 10 mg/kg, or at concentrations of about 10 to 100 nM, was surprisingly found to contribute to humoral immunity by raising the titers and activities of autoantibodies against GRP78 and F1F0 ATP synthase on the surface of CT26 cells, and inducing B cell proliferation and differentiation of plasma cells. Methods for inducing B cell proliferation, inducing BAFF stimulated B cell proliferation, and suppressing or inhibition growth of a neoplasia are provided.
Type:
Application
Filed:
August 29, 2019
Publication date:
December 19, 2019
Inventors:
Ru Chih C. Huang, David Mold, Tiffany Jackson, Yu-Ling Lin, Kuang-Wen Liao
Abstract: The present invention relates to a method for administering water soluble physiologically active substances, said method comprising intranasally administering to a subject an aqueous composition comprising 0.001-25 wt. % of one or more fully dissolved physiologically active substances, the physiologically active substances having a water solubility in demineralized water of at least 15 mg/mL at 20° C. of, 0.01-10 wt. % nicotinamide, and at least 60 wt. % water. The invention also relates to a kit comprising said composition and to the use of nicotinamide as an enhancer of intranasal absorption of a physiologically active substance from an aqueous solution, wherein the aqueous solution further comprises 0.01-10 wt. % nicotinamide.
Type:
Application
Filed:
August 30, 2019
Publication date:
December 19, 2019
Inventors:
Hubert Clemens PELLIKAAN, Rolf Lourens VISSER
Abstract: Disclosed is a pharmaceutical composition comprising i) a dopamine agonist and ii) a L-DOPA derivative in combination in form of a liquid preparation. The pharmaceutical composition is used for the treatment of Parkinson's disease, restless leg syndrome, dystonia, for inhibiting prolactin secretion, for stimulating the release of growth hormones, for the treatment of neurological symptoms of chronic manganese intoxication, oamyotrophic lateral sclerosis, and multiple system atrophy.
Abstract: New methods of treating schizophrenia and schizoaffective disorder by administration of pharmaceutical compositions comprising an antipsychotic compound and a VMAT2 inhibitor to a subject in need thereof are provided.
Type:
Application
Filed:
January 16, 2019
Publication date:
December 19, 2019
Inventors:
Samuel Roger Jesse Hoare, Dimitri E. Grigoriadis, Neil J. Ashweek
Abstract: The present disclosure is directed to method of treatment for treating or ameliorating various conditions caused by radiation exposure such as RIGS, enteritis, oral mucositis, mucositis, and proctitis by the administration of a compound Yel002/BCN057 or an analog thereof.
Type:
Application
Filed:
October 12, 2018
Publication date:
December 19, 2019
Applicants:
University of Kansas, BCN Biosciences L.L.C.
Abstract: Methods and compositions are described for enhancing tissue regeneration or wound repair in a mammalian subject comprising a composition comprising (a) a proline hydroxylase inhibitor component or molecule that increases or upregulates HIF1a and (b) a carrier component comprising a hydrogel.
Type:
Application
Filed:
June 3, 2019
Publication date:
December 19, 2019
Inventors:
Phillip B. Messersmith, Iossif A. Strehin, Ellen Heber-Katz
Abstract: The present invention relates to therapeutic ADCs comprising SN-38 attached to an anti-Trop-2 antibody or antigen-binding antibody fragment. The ADC may be administered at a dosage of between 4 mg/kg and 18 mg/kg, preferably 4, 6, 8, 9, 10, 12, 16 or 18 mg/kg, most preferably 8 to 10 mg/kg. When administered at specified dosages and schedules, the ADC can reduce solid tumors in size, reduce or eliminate metastases and is effective to treat cancers resistant to standard therapies, such as radiation therapy, chemotherapy or immunotherapy. Preferably, the ADC is administered in combination with one or more other therapeutic agents, such as a PARP inhibitor, a microtubule inhibitor, a Bruton kinase inhibitor or a PI3K inhibitor. Most preferably, the ADC is of use for treating a Trop-2 expressing cancer, such as metastatic urothelial cancer.
Type:
Application
Filed:
July 29, 2019
Publication date:
December 19, 2019
Inventors:
Serengulam V. Govindan, David M. Goldenberg
Abstract: The present invention generally relates to processes for preparing highly pure morphinan-6-one products. The processes involve reducing the concentration of alpha, beta unsaturated ketone compounds present as impurities in morphinan 6 one products or reaction mixtures including morphinan 6 one compounds by treatment with a sulfur-containing compound.
Type:
Application
Filed:
August 23, 2019
Publication date:
December 19, 2019
Applicant:
SpecGx LLC
Inventors:
Henry J. Buehler, William E. Dummitt, Anthony Mannino, Dennis C. Aubuchon, Hong Gu
Abstract: The present invention provides a composition and method for treating acute on chronical liver failure or a related disease. The method comprises administering to a subject a composition comprising trimetazidine hydrochloride (1-[2,3,4-trimethoxybenzyl] piperazine dihydrochloride) (Trimetazidine or TMZ) or a pharmaceutically acceptable salt thereof according to a dosage regimen.
Abstract: Provided herein is 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 and a bispecific antibody specifically binding to human B cell maturation antigen (BCMA) and to human CD3? (CD3) provided herein, in treating, preventing or managing multiple myeloma.
Abstract: The present invention relates to sulphate salts of N-(3-(4-(3-(diisobutylamino)propyl)piperazin-1-yl)propyl)-1H-benzo[d]imidazol-2-amine and pharmaceutically acceptable solvates thereof, preparation thereof, pharmaceutical compositions containing them and use of the same in the treatment and/or prevention of neurodegenerative diseases.
Abstract: The present invention relates to compounds of general formula I, wherein the groups R, R1, R2, R3, m and n are defined herein, which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2.
Abstract: The present disclosure relates to methods, uses, pharmaceutical compositions comprising an sGC stimulator or a pharmaceutically acceptable salt thereof, alone or in combination with one or more additional therapeutic agents, for the treatment of an esophageal motility disorder.
Abstract: The present application relates to the use of bicyclic-substituted uracil derivatives, alone or in combinations with other active ingredients for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of inflammatory and fibrotic disorders, for the treatment of endometriosis, of endometriosis-associated fibrosis, of adenomyosis and of pain associated with an endometriosis disorder and also of postoperative peritoneal fibrosis and adhesion formation.
Type:
Application
Filed:
December 13, 2017
Publication date:
December 19, 2019
Applicant:
BAYER PHARMA AKTIENGESELLSCHAFT
Inventors:
Michaele PETERS, Markus KOCH, Thomas ZOLLNER
Abstract: Provided herein are compositions and methods for treating myelofibrosis in a subject. The methods comprise administering to the subject an effective amount of compound which is which is N-tert-butyl-3-[(5-methyl-2-{[4-(2-pyrrolidin-1-ylethoxy)phenyl]amino}pyrimidin-4-yl)amino]benzenesulfonamide or a pharmaceutical salt thereof or a hydrate thereof.
Abstract: The disclosure provides methods of use of certain compounds that are useful for treating certain symptoms of endocrine disturbances, and in particular those associated with hot flashes.
Type:
Application
Filed:
August 26, 2019
Publication date:
December 19, 2019
Inventors:
Michael G. Natchus, Richard Arrendale, Dennis Liotta, Ketan Desai, Hyunsuk Shim
Abstract: The present invention relates to a method of treatment of cancer, said method comprising administering an effective dose of a protein kinase inhibitor to a patient in need thereof having said cancer. The present invention also relates to a method of post-transcriptional control of cancer-related genes comprising administering an effective amount of a protein kinase inhibitor to a subject in need thereof.
Type:
Application
Filed:
June 13, 2018
Publication date:
December 19, 2019
Inventors:
Khalid S. ABU KHABAR, Qamraa Hamad AL-QAHTANI
Abstract: In certain embodiments, the invention includes therapeutic methods of using a BTK inhibitor to treat solid tumor cancers by modulation of the tumor microenvironment, including macrophages, monocytes, mast cells, helper T cells, cytotoxic T cells, regulatory T cells, natural killer cells, myeloid-derived suppressor cells, regulatory B cells, neutrophils, dendritic cells, and fibroblasts.
Type:
Application
Filed:
April 1, 2019
Publication date:
December 19, 2019
Inventors:
Ahmed Hamdy, Wayne Rothbaum, Raquel Izumi, Brian Lannutti, Todd Covey, Roger Ulrich, Dave Johnson, Tjeerd Barf, Allard Kaptein
Abstract: The present invention provides methods of treating, stabilizing or lessening the severity or progression of a non-alcoholic fatty liver disease using an ACC inhibitor alone or with one or more additional therapeutic agents.
Type:
Application
Filed:
May 13, 2019
Publication date:
December 19, 2019
Inventors:
Geraldine C. Harriman, H. James Harwood, Rosana Kapeller-Libermann, William F. Westlin
Abstract: The human body is mediated by a large number of chemicals and chemical processes where imbalances can result in abnormal conditions affecting part or all of the human body. Artificial drugs addressing specific diseases by targeting specific chemical imbalance(s) and/or process(es). For example, tofactinib is a JAK-STAT signaling pathway inhibitor beneficial for treating autoimmune diseases whilst baclofen acts as an agonist of GABA receptors. However, these are each prescribed in oral form leading to reduced efficacy or absorption by other regions of the patient. Accordingly, the inventor has established alternate dosing formats such a topical creams allowing local direct application allowing specific targeted delivery to the appropriate region of the patient's body as well their use, in the instances of tofactinib and baclofen, for the treatment of other diseases or conditions.
Abstract: Methods for decreasing rod gene expression in a retina, methods for decreasing the protein products expressed by rod genes in a retina, methods for treating a disease or condition treatable by decreasing rod gene expression or their protein products in a retina, and methods for treating a retinal disease in a subject.
Type:
Application
Filed:
June 20, 2019
Publication date:
December 19, 2019
Applicants:
University of Washington, The J. David Gladstone Institutes, a Testamentary Trust Established Under the Will of J. David Glads
Inventors:
Thomas A. Reh, Paul Nakamura, Sheng Ding
Abstract: The present disclosure relates to methods and compositions for treating cancer with a diaryl macrocycle in combination with at least one other cancer therapeutic, such as an EGFR inhibitor.
Abstract: The present invention belongs to the pharmaceutical field, and in particular, it relates to a pharmaceutical formulation of palbociclib and a preparation method thereof. The pharmaceutical formulation comprises palbociclib, an acidic auxiliary material, and optionally a hydrophilic high-molecular material, which has better solubility and in vitro dissolution property as compared with the conventional formulation and can be used for enhancing in vivo absorption and bioavailability of palbociclib.