Abstract: Methods are disclosed herein for administering a oncogenic Src homology-2 domain containing protein tyrosine phosphatase-2 (SHP2) inhibitor for treating autoimmune and/or glomerulonephritis-associated diseases, and in particular, Systemic Lupus Erythematosus (SLE).
Type:
Application
Filed:
September 10, 2018
Publication date:
January 3, 2019
Inventors:
Zhong-Yin ZHANG, Maria KONTARIDIS, Li-Fan ZENG, Jianxun WANG
Abstract: The invention provides preparations, formulations, kits and other products of manufacture (e.g., blister packs) comprising combinations of beneficial ingredients that are serviceable as therapies for improving states and disease symptoms such as involving inflammation, excessive sympathoneural drive, cachexia, anorexia, and anorexia-cachexia, as well as stress or anxiety related thereto, and methods of making and using them. The invention provides compositions and therapies comprising use of a beta adrenergic antagonist (also called “beta blockers”, e.g., propranolol) in combination with an anti-inflammatory agent, e.g., a nonsteroidal anti-inflammatory drug (NSAID), an angiotensin-converting enzyme (ACE) inhibitor, an angiotensin receptor blocker (ARB), an anabolic steroid, a natural oil or fatty acid or any combination thereof.
Type:
Application
Filed:
May 22, 2017
Publication date:
January 3, 2019
Inventors:
Newell Bascomb, John Maki, Fredric Young
Abstract: The present invention relates to the use of chondroitin as a transdermal carrier and slow-release system for active ingredients in pharmaceutical and cosmeceutical compositions.
Abstract: Stereomerically pure (+)-2-[1-(3-Ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-acetylaminoisoindoline-1,3-dione, substantially free of its (?) isomer, and prodrugs, metabolites, polymorphs, salts, solvates, hydrates, and clathrates thereof are discussed. Also discussed are methods of using and pharmaceutical compositions comprising the (+) enantiomer of 2-[1-(3-Ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-acetylaminoisoindoline-1,3-dione are disclosed. The methods include methods of treating and/or preventing disorders ameliorated by the reduction of levels of TNF-? or the inhibition of PDE4.
Type:
Application
Filed:
September 7, 2018
Publication date:
January 3, 2019
Inventors:
George W. Muller, Peter H. Schafer, Hon-Wah Man, Chuansheng GE
Abstract: Disclosed herein are compounds and compositions thereof which find use in increasing stability of proteins particularly proteins that tend to misfold and form aggregates. Also provided herein are methods for using these compounds and compositions for increasing stability of proteins and thereby decreasing aggregate formation by these proteins. Also disclosed herein are heterobifunctional compounds that include a TTR binding compound connected to a targeting moiety via a linker, for use in disrupting PPIs of a target protein.
Type:
Application
Filed:
January 30, 2018
Publication date:
January 3, 2019
Inventors:
Isabella A. Graef, Mamoun M. Alhamadsheh
Abstract: This invention relates to novel compounds. The compounds of the invention are tyrosine kinase inhibitors. Specifically, the compounds of the invention are useful as inhibitors of Bruton's tyrosine kinase (BTK). The invention also contemplates the use of the compounds for treating conditions treatable by the inhibition of Bruton's tyrosine kinase, for example cancer, lymphoma, leukemia and immunological diseases.
Abstract: The present invention relates to certain PDE2 inhibitory compounds, in free or salt form, pharmaceutical compositions containing such compounds and methods for the treatment of PDE2 mediated disorders.
Type:
Application
Filed:
September 7, 2018
Publication date:
January 3, 2019
Applicant:
INTRA-CELLULAR THERAPIES, INC.
Inventors:
Peng LI, Hailin ZHENG, Gretchen SNYDER, Lawrence P. WENNOGLE, Joseph HENDRICK
Abstract: The present invention relates to compositions and methods for the treatment and prevention of ptosis and more specifically to compositions and methods for the non-surgical treatment and prevention of ptosis and methods for the improvement of night vision, administering a combination of pilocarpine and oxymetazoline.
Type:
Application
Filed:
July 6, 2016
Publication date:
January 3, 2019
Inventors:
Charles F. BOSWORTH, Houman D. HEMMATI, David A. HOLLANDER
Abstract: The present invention provides, among other things, methods and compositions for treating brain conditions. In some embodiments, the methods include administering to a subject suffering from or susceptible to a brain condition an angiotensin (1-7) peptide via either an intravenous or subcutaneous route of administration.
Abstract: An ointment is provided. The ointment stably comprises an oxazole compound that has specific inhibitory activity against PDE4 and that is represented by the following formula (11). The ointment can be efficiently absorbed into the skin.
Abstract: Disclosed herein, inter alia, are compounds and methods for increasing spine density in a neuron, and for treatment of neuronal diseases and cancer.
Abstract: The invention provides pharmaceutical compositions comprising a compound of formula (I) or (II) and an additional therapeutic agent Also provided is the HCI salt and crystalline form of the compound of formula (I). The compounds inhibit the prostaglandin F receptor (PGF2alpha) and thus useful in the treatment of disorders such as preterm labor at the early gestational stage.
Type:
Application
Filed:
January 4, 2017
Publication date:
January 3, 2019
Inventors:
Patrick Naxos PAGE, Matthias SCHWARZ, Catherine JORAND-LEBRUN, Anna QUATTROPANI, Vincent POMEL, Ernest LOUMAYE, Oliver POHL, Jean-Pierre GOTTELAND
Abstract: The present invention relates to the compound [2-[(5-nitro-1,3-thiazol-2-yl)carbamoyl]phenyl]ethanoate (Nitazoxanide) 2-hydroxy-N-(5-nitro-2-thiazolyl)benzamide (Tizoxanide) for treating cholestatic and fibrotic diseases.
Type:
Application
Filed:
September 19, 2018
Publication date:
January 3, 2019
Inventors:
Raphael DARTEIL, Robert WALCZAK, Carole BELANGER, Emilie NEGRO, Pierre DAUBERSIES, Philippe DELATAILLE
Abstract: The technical field of the invention is in pharmaceutical compounds and methods. In an aspect, the disclosure provides macrolide compounds suitable for use as antifungal agents, as well as methods for their use and compositions containing the same.
Type:
Application
Filed:
May 1, 2018
Publication date:
January 3, 2019
Applicant:
Amplyx Pharmaceuticals, Inc.
Inventors:
Jonathan A. Covel, Mitchell Mutz, Peter J. Webb, Robert Remme Webb
Abstract: A formulation, especially one that is topically administered, comprising a combination of rapamcycin and metformin in a molar ratio of about 20:1, 10:1, 5:1, 4:1, 3:1, or 1:1. The topical formulation may be a gel, an ointment, a cream or a lotion. The topical formulation may be used to treat a condition or disease of the skin or eye, wherein the condition or disease is associated with mTORC1 activation.
Abstract: The invention provides derivatives of cyclopamine having the following formula:
Type:
Application
Filed:
March 27, 2018
Publication date:
January 3, 2019
Inventors:
Brian Austad, Mark L. Behnke, Alfredo C. Castro, Michael J. Grogan, Somarajannair Janardanannair, Andre Lescarbeau, Stephane Peluso, Andre B. Charette, Martin R. Tremblay
Abstract: Provided are methods and compositions for identifying candidate agents for treatment of obesity, liver disease, and/or diabetes. Such methods include, e.g., contacting a mammalian cell or cell population with a test agent, and measuring an expression level and/or activity level of ClpP in the mammalian cell or in cells of the cell population. Also provided are methods and compositions for treating an individual (e.g., one who is obese and/or has diabetes). Treatment methods include administering an inhibitor of ClpP to the individual (e.g., to prevent or reduce weight gain, to increase insulin sensitivity, and/or to increase glucose tolerance).
Abstract: The present invention provides methods to determine whether a patient with a lysosomal storage disorder will benefit from treatment with a specific pharmacological chaperone. The present invention exemplifies an in vitro method for determining ?-galactosidase A responsiveness to a pharmacological chaperone such as 1-deoxygalactonojirimycin in a cell line expressing a mutant from of ?-galactosidase A. The invention also provides a method for diagnosing Fabry disease in patients suspected of having Fabry disease.
Type:
Application
Filed:
July 26, 2018
Publication date:
January 3, 2019
Inventors:
Elfrida Benjamin, Hung V. Do, Xiaoyang Wu, John Flanagan, Brandon Alan Wustman
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: Disclosed herein are methods and compositions related to the durable use of aminopyridines, such as 4-aminopyridine, to improve impairments of patients with a demyelinating condition, such as MS.
Abstract: The invention relates to methods for decreasing adverse events associated with pirfenidone (5-methyl-1-phenyl-2-(1H)-pyridone) therapy. The invention discloses an optimized dose escalation scheme that results in the patient having increased tolerance to adverse events associated with the administration of pirfenidone. The invention also discloses a starter pack that may be used in conjunction with the dose escalation scheme.
Abstract: The present invention relates to chlorine or bromine salts of cetylpyridinium for use in the treatment of porphyrias and psoriasis, as well as methods of treatment of these diseases in human patients by using hydro-alcoholic solutions of cetylpyridinium chloride or bromide.
Abstract: The present invention is directed to compounds of formula (I) which are inhibitors of the BACE1 enzyme. Separate aspects of the invention are directed to pharmaceutical compositions comprising said compounds and uses of the compounds to treat disorders for which the reduction of A? deposits is beneficial such as Alzheimer's disease.
Type:
Application
Filed:
August 9, 2018
Publication date:
January 3, 2019
Inventors:
Karsten Juhl, Lena Tagmose, Mauro Marigo
Abstract: The present invention is directed to pyrazol-4-yl-pyridine compounds which are allosteric modulators of the M4 muscarinic acetylcholine receptor. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which M4 muscarinic acetylcholine 5 receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which M4 muscarinic acetylcholine receptors are involved.
Type:
Application
Filed:
December 19, 2016
Publication date:
January 3, 2019
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
John J. Acton, III, Jianming Bao, Melissa Egbertson, Xiaolei Gao, Scott T. Harrison, Sandra L. Knowles, Chunsing Li, Michael Man-Chu Lo, Robert D. Mazzola, Jr., Zhaoyang Meng, Michael T. Rudd, Oleg B. Selyutin, David M. Tellers, Ling Tong, Jenny Miu-Chun Wai
Abstract: Synergistic compositions and medical devices for use in treatment during gynecological procedures are provided. A gynecological device for treatment of cervical blockages without general anesthesia thereby suitable for out-patient service, saving time and money to the patients is provided. Synergistic compositions that enable the practioners to perform gynecological procedures without pain or bleeding to the patients are provided.
Abstract: The present invention relates to a pharmaceutical composition comprising propiverine, trospium or glycopyrrolate; and a non-anticholinergic antiemetic agent. It is also related to a pharmaceutical composition comprising a high dose of solifenacin or a pharmaceutically acceptable salts thereof; and a non-anticholinergic antiemetic agent. Pharmaceutical compositions containing high dose of nsPAChA for use for increasing the AChEI blood concentrations and for combating neurodegeneration are also described. The invention also relates to a method for inducing neuroprotection and combating neurodegeneration in a patient suffering from Alzheimer type dementia as well as to a method for increasing the blood levels of an acetyl choline esterase inhibitor (AChEI) in a human subject treated with an AChEI dose.
Type:
Application
Filed:
January 25, 2018
Publication date:
January 3, 2019
Applicant:
Chase Pharmaceuticals Corporation
Inventors:
Kathleen E. Clarence-Smith, Thomas N. Chase
Abstract: The present disclosure provides methods and compositions for treating fall-related symptoms in patients with neurodegenerative diseases such as Parkinson's disease or Parkinson-related diseases. In some embodiments, the disclosure utilizes nicotine or a salt thereof in combination of dopaminergic agent treatments for reducing fall-related symptoms such as reducing frequency of fall, reducing injuries related to fall, reducing severity of injuries related to fall, freezing of gait, improving posture stability, improving locomotion ability, improving balance and gait. In some embodiments, the methods predict fall frequency and tendency of recurrent falls in patients with Parkinson's disease, in particular, patients with typical Parkinson's disease.
Abstract: The present disclosure provides methods and compositions for treating fall-related symptoms in patients with neurodegenerative diseases such as Parkinson's disease or Parkinson-related diseases. In some embodiments, the disclosure utilizes nicotine or a salt thereof in combination of dopaminergic agent treatments for reducing fall-related symptoms such as reducing frequency of fall, reducing injuries related to fall, reducing severity of injuries related to fall, freezing of gait, improving posture stability, improving locomotion ability, improving balance and gait. In some embodiments, the methods predict fall frequency and tendency of recurrent falls in patients with Parkinson's disease, in particular, patients with typical Parkinson's disease.
Abstract: A therapeutic agent for biliary tract cancer comprising 4-[3-chloro-4-(cyclopropylaminocarbonyl)aminophenoxy]-7-methoxy-6-quinolinecarboxamide or a pharmacologically acceptable salt thereof is provided.
Abstract: The present invention is directed to the use of compounds which are modulators of the G protein-Coupled Estrogen Receptor (GPER) for the inhibition—and/or treatment of Bacterial infections, especially including metMctHin-resistant Staphylococcus aureus (MRSA) infections. Pharmaceutical compositions and methods of treatment of bacterial pathogens, including MRSA are also described.
Type:
Application
Filed:
January 9, 2017
Publication date:
January 3, 2019
Inventors:
Pamela Hall, Eric R. Prossnitz, Helen J. Hathaway
Abstract: The present invention provides compositions and methods for the treatment of drug-tolerant glioblastoma, and in particular glioblastoma stem cells. Specifically, the methods comprise contacting a glioblastoma stem cell with a platelet-derived growth factor receptor alpha inhibitor and one or more of a histone lysine demethylase inhibitor and a Notch inhibitor.
Type:
Application
Filed:
March 24, 2016
Publication date:
January 3, 2019
Applicant:
THE GENERAL HOSPITAL CORPORATION
Inventors:
BRIAN B. LIAU, ANOOP P. PATEL, CEM SIEVERS, BRADLEY E. BERNSTEIN
Abstract: To provide a pharmaceutical, in particular a compound which can be used as a therapeutic agent for irritable bowel syndrome (IBS). It was found that a tetrahydroisoquinolin-1-one derivative having an amide group at the 4-position or a pharmaceutically acceptable salt thereof has an excellent bombesin 2 (BB2) receptor antagonistic action. It is also found that the tetrahydroisoquinolin-1-one derivative is highly effective on bowel movement disorders. From the above, the tetrahydroisoquinolin-1-one derivative of the present invention is useful as a therapeutic agent for diseases associated with a BB2 receptor, in particular IBS.
Abstract: The present invention provides abuse deterrent mucoadhesive devices for delivery of buprenorphine. Each device comprises a mucoadhesive layer and a backing layer, and the pH in each layer is selected, such that absorption of buprenorphine is maximized.
Type:
Application
Filed:
July 9, 2018
Publication date:
January 3, 2019
Applicant:
BioDelivery Sciences International, Inc.
Abstract: An injectable liquid composition for the treatment of a physical addiction includes naltrexone in the amount of 5%-95% of the total weight of the composition; at least two co-polymers in the amount of between 5%-95% of the total weight of the composition; and a biocompatible water miscible organic solvent in the amount of 5% to 50% of the total weight of the composition. The composition is adapted to form a gel-like mass when contacted with an aqueous environment and to dissolve at a predetermined rate to release a therapeutic naltrexone dose over a predetermined period of time.
Abstract: Dosage forms, drug delivery systems, and methods related to sustained release of dextromethorphan or improved therapeutic effects are disclosed. Typically, bupropion or a related compound is orally administered to a human being to be treated with, or being treated with, dextromethorphan.
Abstract: The invention provides new therapeutic uses of 1-[2-(2,4-dimethyl-phenylsulfanyl)phenyl]-piperazine and pharmaceutically acceptable salts thereof.
Abstract: A method of promoting remyelination in a subject in need thereof includes administering to the subject a therapeutically effective amount of at least one (1,3) Diazole compound, wherein the therapeutically effective amount is the amount effective to induce endogenous oligodendrocyte precursor cell (OPC) differentiation in the subject's central nervous system.
Type:
Application
Filed:
May 27, 2015
Publication date:
January 3, 2019
Inventors:
Paul Tesar, Fadi J. Najm, Robert H. Miller
Abstract: Described herein are compounds, compositions and methods for treatment of cancer. Also described are methods and uses for identifying subject with cancer that are suitable for treatment with the compounds, composition and methods are described herein. In one aspect of the present invention, there is provided a method of treating a subject having a cancer deficient in NMT2, comprising: administering to said subject an NMT inhibitor.
Type:
Application
Filed:
July 2, 2018
Publication date:
January 3, 2019
Applicant:
PACYLEX PHARMACEUTICALS INC.
Inventors:
Luc G. Berthiaume, Erwan Beauchamp, Conganige Maneka Anne Perinpanayagam, Chuiyee Yap
Abstract: Disclosed herein are otic product kits for administration of a sterilized formulation. In some embodiments, the otic product kit comprises: an aseptic container containing the sterilized formulation; a syring; and an administration needle connectable to the syringe, wherein the sterilized formulation comprising: from about 5.5 wt % to about 6.5 wt % multiparticulate ciprofloxacin; from about 15 wt % to about 17 wt % poloxamer 407; and water. Also disclosed herein are methods of preparing and administrating the sterilized formulation. In some embodiments, the method comprising (1) transferring the sterilized otic formulation from an aseptic container to a syringe through a preparation needle; (2) replacing the preparation needle with an administration needle; and (3) injecting the sterilized otic formulation from the syringe through the administration needle into the ear of a patient.
Type:
Application
Filed:
December 9, 2016
Publication date:
January 3, 2019
Applicant:
OTONOMY, INC.
Inventors:
Scott H. COLEMAN, Wei-Cheng LIAW, Jerry WROBLEWSKI, Robert SAVEL
Abstract: Described herein are combinations comprising a therapeutically effective amount of a first agent and a therapeutically effective amount of a second agent, wherein the first agent is an inhibitor of ALK, ROS1, TrkA, TrkB, or TrkC activity, or a combination thereof, and methods of using such combinations in the treatment of patients having cancer.
Type:
Application
Filed:
December 15, 2016
Publication date:
January 3, 2019
Applicant:
IGNYTA, INC.
Inventors:
Gang LI, Ge WEI, Zachary D. HORNBY, Jonathan Ee-ren LIM
Abstract: Disclosed herein are methods of treating a brain tumor by administering Plinabulin. Some embodiments relate to treatment of glioblastoma multiforme by administering Plinabulin.
Abstract: The invention relates to the use of flibanserin, or a pharmaceutically acceptable acid addition salt thereof, for the treatment of disorders of sexual desire.
Abstract: Solid pharmaceutical dosage forms comprising (S)-ethyl 2-amino-3-(4-(2-amino-6-((R)-1-(4-chloro-2-(3-methyl-1H-pyrazol-1-yl)phenyl)-2,2,2-trifluoroethoxy)pyrimidin-4-yl)phenyl)propanoate (telotristat) are disclosed, as well as methods of making them and compositions useful in their manufacture.
Type:
Application
Filed:
June 5, 2017
Publication date:
January 3, 2019
Inventors:
Jinling CHEN, Matthew S. DEAVER, Richard J. HOLL, Kalyan NUGURU
Abstract: The present description relates to compounds, forms, and pharmaceutical compositions thereof and methods of using such compounds, forms, or compositions thereof for treating or ameliorating Huntington's disease. In particular, the present description relates to substituted monocyclic heteroaryl compounds of Formula (I), forms and pharmaceutical compositions thereof and methods of using such compounds, forms, or compositions thereof for treating or ameliorating Huntington's disease.
Abstract: This invention is directed to a compound of formula (I): wherein R1, R2 and R3 are as defined herein, a pharmaceutical composition comprising the compound, intermediates and processes for making said compounds, and the use of the compound to treat allergic and/or inflammatory disorders, particularly disorders such as allergic rhinitis, asthma, chronic obstructive pulmonary disease (COPD) and age-related macular degeneration (AMD).
Type:
Application
Filed:
February 23, 2018
Publication date:
January 3, 2019
Inventors:
Christopher L. VANDEUSEN, Franz J. WEIBERTH, Harpal S. GILL, George LEE, Andrea HILLEGASS
Abstract: Foamy macrophages with senescence markers accumulate in the subendothelial space at the onset of atherosclerosis where they drive pathology by increasing expression of key atherogenic and inflammatory cytokines and chemokines. This invention provides senolytic agents that remove senescent cells that are present in or around atherosclerotic plaques. The agents inhibit or reverse thinning of the fibrous cap on atherosclerotic plaques. This has the effect of stabilizing the plaques, inhibiting rupture and preventing pathological sequelae that manifest as coronary artery disease. Senolytic agents used in this way complement the action of statins and other drugs that cause plaque regression. Thus, senolytic agents and lipid lowering drugs can be used in combination for enhanced therapeutic effect.
Type:
Application
Filed:
July 2, 2018
Publication date:
January 3, 2019
Inventors:
Jan M.A. van Deursen, Bennett G. Childs, Darren J. Baker, James L. Kirkland, Tamar Tchkonia, Yi Zhu, Nathaniel David, Remi-Martin Laberge, Judith Campisi, Marco Demaria
Abstract: The present invention provides a therapeutic agent for a wound comprising a compound represented by the formula (I) wherein R1 represents a hydroxy C1-C6 alkyl group, a C2-C7 alkanoyl group, a C2-C7 alkanoyl C1-C6 alkyl group, a (C1-C6 alkoxy)carbonyl group, a (C1-C6 alkoxy)carbonyl C1-C6 alkyl group, a carboxy group, or a carboxy C1-C6 alkyl group, or a pharmacologically acceptable salt thereof as an active ingredient.
Abstract: The present invention provides a modulator of Kv3.1 and/or Kv3.2 and/or Kv3.3 channels for use in the prophylaxis or treatment of pain. Modulators for use in the prophylaxis or treatment of pain include compounds of formula (I) or a pharmaceutically acceptable salt and/or solvate thereof and/or derivative thereof: (I).
Abstract: The invention provides compounds of formula (I): Said compounds being modulators of Kv3 channels and of use in the prophylaxis or treatment of related disorders.
Abstract: Described herein, inter alia, are anti-cancer agents, anti-cancer pharmaceutical compositions, combinations of the agents and/or pharmaceutical compositions, and methods of using the same.
Type:
Application
Filed:
February 9, 2016
Publication date:
January 3, 2019
Inventors:
Caius Gabriel Radu, Soumya Poddar, Johannes Czernin, David Nathanson, Thuc Le