Abstract: The present disclosure provides methods of treatment using ophthalmic compositions comprising semifluorinated alkanes for keratoconjunctivitis sicca and/or Meibomian gland dysfunction, which methods provide for the enrichment of an ophthalmic tissue in the semifluorinated alkane, and optionally methods of delayed release of the semifluorinated alkane from the enriched ophthalmic tissue to the surface of the cornea and/or conjunctiva, and/or to the Meibomian gland.
Type:
Application
Filed:
October 3, 2018
Publication date:
August 27, 2020
Inventors:
Bernhard GÜNTHER, Frank LÖSCHER, Hartmut VOSS, Sonja KRÖSSER, Kirsten EICKHOFF, Daniela WILLEN, Markus BEIER, Thomas SCHLÜTER
Abstract: A high-throughput screening methods for identifying candidate anticancer medicinal agents is described herein. The candidate anticancer medicinal agents are arylfluorosulfate compounds derived from phenolic compounds. The method involves in situ generation of the arylfluorosulfate compounds in multi-well plates by reaction of phenolic compounds in DMSO with a saturated solution of SO2F2 dissolved in a solvent such as acetonitrile, in the presence of an organic base, followed by reaction of generated fluoride ion with trimethylsilyl chloride to form volatile trimethylsilyl fluoride. Solvents, organic base, and silyl compounds are then removed, in vacuo, to afford the arylfluorosulfate compounds suitable for biological screening in cancer cell lines without further purification.
Type:
Application
Filed:
May 11, 2020
Publication date:
August 27, 2020
Applicant:
THE SCRIPPS RESEARCH INSTITUTE
Inventors:
Jie LI, Zilei LIU, Suhua LI, Peng WU, K. Barry SHARPLESS
Abstract: The present invention relates generally to compositions and methods of use that include compounds that treat and prevent neurological disorders including Alzheimer's disease, neuroinflammation, and diseases and conditions associated with protein misfolding and/or protein aggregation.
Type:
Application
Filed:
December 16, 2016
Publication date:
August 27, 2020
Inventors:
Joshua M COSTIN, John M WILLIAMS, Norman RELKIN, Dan LI
Abstract: The present invention provides pharmaceutical compositions given once daily containing at least one therapeutically active ingredient selected from the group consisting of memantine and a pharmaceutically acceptable salt of memantine, and a pharmaceutically acceptable polymeric matrix carrier. The dosage forms of the invention sustain the release of the therapeutically active agent from about 4 to about 24 hours when said dosage form is exposed to aqueous solutions. following entry of said form into a use environment, wherein said dosage form has a dissolution rate of more than about 80% after passage of about 6 hours to about 12 hours following said entry into said use environment.
Type:
Application
Filed:
April 17, 2020
Publication date:
August 27, 2020
Inventors:
Suneel K. Rastogi, Niranjan Rao, Antonia Periclou, Wattanaporn Abramowitz, Mahendra G. Dedhiya, Shashank Mahashabde
Abstract: Provided are processes for the prevention or treatment of viral infection in a subject. Some aspects provide administration of a sphingoid compound, optionally sphingosine, an active ingredient that activates generation of a sphingoid base, optionally of sphingosine; or an active agent that inhibits the degradation of a sphingoid base, optionally of sphingosine, to a subject such as a human. By increasing the local concentration of sphingosine in a subject or an area of a subject to which the composition is administered such as the nose or interior of the nose or portion thereof, the ability of viruses to infect the subject or cells thereof is reduced thereby treating of preventing infection by the virus.
Type:
Application
Filed:
May 11, 2020
Publication date:
August 27, 2020
Inventors:
Erich Gulbins, Karl Sebastian Lang, Judith Bezgovsek
Abstract: There is herein provided a compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein X, R1, R2, R3, R4 and n have meanings as provided in the description.
Abstract: The disclosure herein relates to the innovative epinephrine formulations in aqueous solution of medicinal products that enhance the physicochemical stabilities of epinephrine and extend the product shelf life. In some instances, the formulations comprise epinephrine or a salt thereof, a complexing agent, and a “non-sulfite” antioxidant. The epinephrine formulations substantially demonstrated the superior physicochemical stabilities to conventional sulfite formulation of commercial medications currently available. In some instances, sulfite-free formulations further provide further benefit (e.g., safety benefits) to sulfite-sensitive patients. The compositions, methods for preparing the formulations, and methods of using the same (e.g., in the treatment of anaphylaxis) are also provided.
Abstract: The present disclosure provides a novel topical composition comprising at least one active agent and method for making the composition. Certain compounds have been combined to make a stable composition comprising at least one active agent such as selective estrogen receptor modulators and aromatase inhibitors. The present disclosure also provides methods for treatment of hormone-dependent breast and hormone-dependent reproductive tract disorders.
Type:
Application
Filed:
September 10, 2018
Publication date:
August 27, 2020
Applicant:
Atossa Therapeutics, Inc.
Inventors:
Steven C. Quay, Avadhesh S. Kushwaha, Edward T. Kisak, John M. Newsam
Abstract: The present disclosure provides the use of compounds of Formulae (I), (II), (III), (III-A), and (III-B) (e.g., metformin) in treating a neurological disease associated with repeat expansions and/or RAN protein accumulation, reducing the level of one or more repeat associated non-ATG (RAN) proteins, and reducing the accumulation of RAN proteins in a subject and/or biological sample. Also provided is the use of compounds of Formulae (I), (II), (III), (III-A), and (III-B) (e.g., metformin) in inhibiting RAN protein translation in a subject and in a biological sample (e.g., cells, tissue). Also provided in the present disclosure are pharmaceutical compositions, Skits, and uses of compounds of Formulae (I), (II), (III), (III-A), and (III-B) (e.g., metformin) for treating diseases associated with repeat expansions.
Type:
Application
Filed:
September 26, 2018
Publication date:
August 27, 2020
Applicant:
University of Florida Research Foundation, Incorporated
Abstract: The invention features methods for the treatment of cystinosis and other cysteamine sensitive disorders in a subject including administration of a disulfide convertible to cysteamine in vivo. The methods can include the separate administration of a reducing agent to the subject to increase the bioavailablity and extend the plasma pharmacokinetic profile of the cysteamine produced following administration of the disulfide. The methods permit sustained cysteamine plasma concentrations in a subject.
Type:
Application
Filed:
September 20, 2018
Publication date:
August 27, 2020
Inventors:
Vincent P. STANTON, Jr., Patrice P. RIOUX, Piotr BARSKI, Dariusz WITT
Abstract: Disclosed are methods for the prevention or treatment of a disease or infection caused by or associated with H. Pylori in a subject infected by H. Pylori, the method comprising orally administering a halogenated salicylanilide such as niclosamide to the subject. The method may be used for the prevention or treatment of, for example dyspepsia, gastritis, peptic ulcer disease, premalignant gastric lesions, gastric cancer and gastric mucosa-associated lymphoid tissue (MALT) lymphoma.
Abstract: This disclosure features chemical entities (e.g., a compound exhibiting activity as a mitochondrial uncoupling agent or a pharmaceutically acceptable salt and/or hydrate and/or cocrystal thereof; e.g., a compound, such as niclosamide or a pharmaceutically acceptable salt and/or hydrate and/or cocrystal thereof; e.g., a compound, such as a niclosamide analog, or a pharmaceutically acceptable salt and/or hydrate and/or cocrystal thereof) that are useful, e.g., for treating one or more symptoms of a pathology characterized by an abnormal inflammatory response (e.g., inflammatory bowel diseases) in a subject (e.g., a human). This disclosure also features compositions as well as other methods of using and making the same.
Abstract: A non-enzymatic debridement agent that is less expensive, less cytotoxic, and more effective than enzymatic and sharp surgical debridement of eschar material. The non-enzymatic debridement agent is based on a formulation of detergent with a high critical micelle concentration and a denaturing agent along with an optional optimized buffer. The non-enzymatic wound debriding agent is able to dissolve eschar material in under one week. The buffer or ointment may contain an optimized pH, salt concentration, reducing agent, and other components that aid in the debridement of eschar material from chronic wounds and burn wounds. The non-enzymatic debridement agent can be formulated as an ointment, liquid rinse under pressure, and/or as a combination product with an advanced wound dressing that can act as a sink to remove the solubilized eschar material from the surface of the wound to assist in the debridment and proper healing of wounds.
Abstract: A method for treating a fibrous mass associated with a condition such as Morton's neuroma, plantar fibroma, or Achilles tendinopathy. The method comprises identifying a location of the fibrous mass and non-surgically delivering electromagnetic energy to the fibrous mass.
Abstract: Methods and compositions for controlling parasitic nematodes and treating or preventing a parasitic nematode infection are described herein. The methods include the use of compositions containing an autophagy inhibitor and/or a DCAR-1 inhibitor as anthelmintic agents.
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: A compound having the formula (I) R1-COOH. R1 is an alkyl or alkenyl group having a C7-11 backbone, optionally branched with a C1-6 alkyl group at any C position in the backbone, or a pharmaceutically acceptable salt, amide or ester thereof. The backbone of the alkyl or alkenyl group, and/or the branched alkyl groups, are optionally interrupted by one or more heteroatoms, provided that when R1 is an alkyl group having a C7 backbone, the branching does not consist only of a hexyl group at the ? carbon of R1, or only of a methyl group at the ? carbon of R1, or of only single methyl groups at both the ? and ?-1 carbons of R1, and provided that when R1 is an alkyl group having a C8 dor C11 backbone, the branching does not consist only of a propyl group at the ? carbon of R1.
Type:
Application
Filed:
December 20, 2019
Publication date:
August 27, 2020
Inventors:
Robin Simon Brooke Williams, Matthew Walker
Abstract: Methods, compositions and uses for inhibiting the growth in blood cancer cells with one or more of caffeic acid (3,4-dihydroxycinnamic acid) phenethyl ester (CAPE), CAPE analogue MT30, and CAPE analogue GL8. The blood cancer cells can be myeloma, lymphoma and leukemia cells. The methods, compositions and uses can be in conjunction with the use of an IMiD to treat a patient. The compositions can include a pharmaceutically acceptable carrier, adjuvant or vehicle, a pharmaceutically acceptable salt or dietary supplement.
Type:
Application
Filed:
October 22, 2018
Publication date:
August 27, 2020
Inventors:
Alli Murugesan, Anthony Reiman, Mohamed Touaibia
Abstract: Beta-hydroxybutyrate mineral salts in combination with medium chain fatty acids or an ester thereof such as medium chain triglycerides were used to induce ketosis, achieving blood ketone levels of (2-7 mmol/L), with or without dietary restriction. The combination results in substantial improvements in metabolic biomarkers related to insulin resistance, diabetes, weight loss, and physical performance in a short period of time. Further, use of these supplements to achieve ketosis yields a significant elevation of blood ketones and reduction of blood glucose levels. Use of these substances does not adversely affect lipid profiles. By initiating rapid ketosis and accelerating the rate of ketoadaptation, this invention is useful for the avoidance of glucose withdrawal symptoms commonly experienced by individuals initiating a ketogenic diet, and minimizes the loss of lean body mass during dietary restriction.
Type:
Application
Filed:
May 11, 2020
Publication date:
August 27, 2020
Inventors:
Dominic Paul D'Agostino, Patrick Arnold, Shannon Kesl
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:
February 18, 2020
Publication date:
August 27, 2020
Inventors:
Rene Braeckman, William Stirtan, Paresh Soni
Abstract: The present invention relates to a medicine for treating a patient with advanced or recurrent cancer which is non-responsive or non-tolerant to standard chemotherapy and incurable and unresectable, the medicine comprising propagermanium.
Abstract: Provided in some embodiments are titration packages, kits, and methods of treating pulmonary arterial hypertension comprising prescribing and/or administering to a patient in need thereof 2-(((1r,4r)-4-(((4-chlorophenyl)(phenyl)carbamoyloxy)methyl)cyclohexyl)methoxy)acetic acid (Compound 1), or a pharmaceutically acceptable salt, hydrate, or solvate thereof, via a titration scheme that comprises the up-titration of Compound 1, or a pharmaceutically acceptable salt, hydrate, or solvate thereof, over a period of no more than about nine weeks until an optimized dose is administered.
Abstract: The present invention relates to a cabazitaxel composition for injection and a preparation method therefor. The composition comprises the following components in parts by weight: 1 part of cabazitaxel, 1 to 100 parts of cyclodextrin, 10 to 200 parts of a cosolvent, 1 to 60 parts of polyvidone (PVP), and 0.02 to 1.0 part of an additive. The composition does not contain polysorbate and ethanol. The composition of the present invention contains no polysorbate and ethanol, has low histamine release, and does not require the use of antihistamines, corticosteroids and H antagonists before administration. The composition is provided in a single ready-to-use vial, and serves as a new composition preparation that does not require two-step dilution. The preparation has characteristics of cabazitaxel, including high solubility and high stability. The preparation remains stable long after redissolution and is convenient to use clinically.
Abstract: A composition of furosemide, or a pharmaceutically acceptable salt, solvate, or physiologically functional derivative thereof is combined with a steroid, or a pharmaceutically acceptable salt, solvate, or physiologically functional derivative thereof, to provide a topical medication for nasal or pulmonary treatment. The composition can provide, in a single administration or dosing regime, the anti-inflammatory properties of the steroid and the anti-inflammatory properties of furosemide, without any significant interference between the two, or adverse reaction in situ. One of the components is microencapsulated so that the components are released into the patient's bloodstream at different times, even when administered simultaneously.
Abstract: A method of modulating protein exocytosis is provided. The method comprising contacting a cell with an agent that modulates the ubiquitin pathway in the Golgi, thereby modulating protein secretion.
Abstract: The present invention provides compositions for delivering cannabinoids to the nasal cavity. The subject invention utilizes a composition comprising one or more cannabinoids and an adjuvant mixture to enhance the delivery of the cannabinoid, benefitting the subject to whom the cannabinoid is delivered.
Abstract: Compounds capable of, or usable in, killing cancer cells, and/or modulating a biological activity of a chemokine, and/or inhibiting a kinase, and/or treating diseases and disorders associated with a biological activity of a chemokine and/or cell migration, and/or treating disease and disorders such as cancer and inflammatory diseases and disorders, are provided herein. The compounds are listed in Tables 2, 4 and 5, and/or are represented by Formulae I, IV, V and VI, as defined in the specification. Methods utilizing these compounds are also provided.
Type:
Application
Filed:
May 7, 2020
Publication date:
August 27, 2020
Applicant:
Biokine Therapeutics Ltd.
Inventors:
Amnon PELED, Michal ABRAHAM KARNI, Orly EIZENBERG
Abstract: The current methods and compositions relate to treatment of atrial fibrillation with bucindolol in patients, including patientswith heart failure, after being determined to be homozygous Arg389 in the ?1 adrenergic receptor gene.
Abstract: The present invention relates to a use of a carbamate compound represented by chemical formula 1, or a pharmaceutically acceptable salt, a solvate or a hydrate thereof for reducing or treating developmental disorders including fragile X syndrome, Angelman syndrome or Rett syndrome.
Abstract: Described herein are compounds that are autotaxin inhibitors, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders associated with autotaxin activity.
Abstract: Disclosed herein are spirocyclic compounds, together with pharmaceutical compositions and methods of ameliorating and/or treating a cancer described herein with one or more of the compounds described herein.
Type:
Application
Filed:
January 6, 2020
Publication date:
August 27, 2020
Inventors:
Peter Qinhua Huang, Mehmet Kahraman, Deborah Helen Slee, Kevin Duane Bunker, Chad Daniel Hopkins, Joseph Robert Pinchman, Sunny Abraham, Rakesh Kumar Sit, Daniel Lee Severance
Abstract: The present invention relates to tetracaine based anesthetic formulations and methods of use thereof. The invention further relates to topical formulations of tetracaine and methods of topically anesthetizing body tissues. The present invention also relates to tetracaine based dental anesthetic formulations and methods for anesthetizing the maxillary dental arch using these formulations.
Abstract: An anti-Acanthamoeba agent contains luliconazole crystal as an active ingredient. The luliconazole has a crystal habit in which a ratio of I (20-2) to a total sum of I (001), I (100), I (10-1), I (011), I (110), I (11-1), I (10-2), I (11-2), I (020), I (021), I (20-2), I (121), I (013), I (11-3), and I (221) is 12% or more and/or a ratio of I (10-2) to a total sum of I (001), I (100), I (10-1), I (011), I (110), I (11-1), I (10-2), I (11-2), I (020), I (021), I (20-2), I (121), I (013), I (11-3), and I (221) is 20% or more.
Abstract: A method of lowering cholesterol and/or PCSK9 levels in a subject in need thereof includes administering to the subject an ADH inhibitor, AKR inhibitor, and/or SNO-CoAR inhibitor at an amount(s) effective to reduce serum cholesterol and/or PCSK9 levels.
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:
May 14, 2020
Publication date:
August 27, 2020
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: There is provided an activator of peroxisome proliferator-activated receptor ? which contains: a compound represented by the following Formula (I); a tautomer or stereoisomer of the compound; or a pharmaceutically acceptable salt or solvate thereof (where, in a case where R1, R2, R3, and R8 do not constitute a ring, in the Formula, R1, R2, R3, R6, R7, and R8 may be the same as or different from each other and represent a hydrogen atom, a halogen atom, an alkyl group having 1 to 8 carbon atoms, an alkoxy group having 1 to 8 carbon atoms, an alkyl group having 1 to 8 carbon atoms substituted with 1 to 3 halogen atoms, an alkoxy group having 1 to 8 carbon atoms substituted with 1 to 3 halogen atoms, a hydroxy group, an amino group, a carboxyl group, a mercapto group, an alkylsulfanyl group having 1 to 8 carbon atoms, a nitro group, or a cyano group).
Abstract: The present invention relates to a method of suppressing organ rejection in a patient receiving an organ transplant by initiating oral treatment with a once-daily extended release tacrolimus dosage form, for example, at an initial dose of from about 0.15 to about 0.20 mg/kg/day within 24 or 48 hours following transplantation. The once-daily extended release tacrolimus dosage form (i) provides low fluctuation and/or swing of tacrolimus, (ii) provides a significantly lower Cmax than an immediate release formulation of tacrolimus while providing the same or greater area under the curve (AUC), (iii) releases the tacrolimus substantially in the colon and/or the lower ileum, (iv) releases at most 63.5% of the tacrolimus in the dosage form at the 12 hour time point, or (v) any combination of any of the foregoing.
Abstract: Described is a method for promoting regeneration of hematopoietic stem and progenitor cells in a subject in need thereof. The method comprises administering to the subject a composition comprising a Ca2+/calmodulin (CaM)-dependent protein kinase kinase 2 (CaMKK2) inhibitor. The CaMKK2 inhibitor may be a small molecule inhibitor, such as 7H-benzimidazo(2,1-a)benz(de)isoquinoline-7-one-3-carboxylic acid (STO-609).
Abstract: Methods and compositions are disclosed for diagnosing a patient suspected of suffering from, and for treating a patient suffering from, a disorder such as hypercortisolemia, metabolic syndrome, pre-diabetes, diabetes, Cushing's syndrome, Cushing's Disease, hyperglycemia secondary to hypercortisolemia, a liver disease, a cardiac disorder, high blood pressure, a blood clotting disorder, a cancer, a psychological disorder, weight gain, a disorder of glucose control, a bone disorder (e.g., osteoporosis), hypogonadism, pseudoacromegaly, pituitary tumors, functional hypercortisolism, ACTH secreting tumors, peripheral neuropathy, dyslipidemia and other disorders. The methods and compositions include administration of a heteroaryl-ketone fused azadecalin glucocorticoid receptor modulator (GRM).
Abstract: Provided are methods of administering a vesicular monoamine transport 2 (VMAT2) inhibitor chosen from valbenazine and (+)-a-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 also being administered a strong cytochrome P450 3A4 (CYP3A4) inhibitor.
Type:
Application
Filed:
May 8, 2020
Publication date:
August 27, 2020
Inventors:
Christopher F. O`Brien, Haig P. Bozigian
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:
May 8, 2020
Publication date:
August 27, 2020
Inventors:
Christopher F. O`Brien, Haig P. Bozigian
Abstract: A method of treating liver fibrosis with CCR2 antagonists is provided. The liver fibrosis may be associated with non-alcoholic steatohepatitis (NASH), non-alcoholic fatty liver disease (NAFLD), emerging cirrhosis, non-cirrhotic hepatic fibrosis, type 2 diabetes mellitus (T2DM) or metabolic syndrome (MS).
Abstract: The present invention provides an anti-tumor agent comprising a compound of formula (1) or a pharmaceutically acceptable salt thereof, wherein ring Q1 is optionally-substituted C6-10 aryl, etc.; R1 and R2 are independently hydrogen atom, etc.; W1 is C1-4 alkylene which may be optionally substituted with 1 to 3 fluorine atoms or C3-7 cycloalkyl; W2 is —NR4aC(O)—, etc. wherein R4a is hydrogen atom or C1-6 alkyl; ring Q2 is optionally-substituted C6-10 aryl, etc., in combination with at least one agent selected from the group consisting of an anti-cancer agent, an anti-diabetic agent, an agent for treating dyslipidemia, an agent for treating multiple sclerosis, a steroidal anti-inflammatory agent, a non-steroidal anti-inflammatory agent, an anti-fungal agent, and a pharmaceutically acceptable salt thereof.
Abstract: The application relates to amide derivatives, processes for their preparation, pharmaceutical compositions, and their uses, more particularly their uses in treating chronic hepatitis B virus (HBV) infection.
Type:
Application
Filed:
February 21, 2020
Publication date:
August 27, 2020
Inventors:
Stefaan Julien LAST, Bart Rudolf Romanie KESTELEYN, Sandrine Céline GROSSE, Tim Hugo Maria JONCKERS, Jan Martin BERKE, Geerwin Yvonne Paul HACHÉ, Edgar JACOBY, Carolina MARTINEZ LAMENCA, Morgan Charles R. LECOMTE, Abdellah TAHRI
Abstract: The present disclosure relates generally to compositions and methods for treating, preventing, or slowing the rate of development of a disease or condition mediated by a nonsense mutation in the bone morphogenetic protein receptor type II (Bmpr2) in a subject in need thereof. The method entails administering to the subject a compound of the present disclosure, such as GJ103 and a salt thereof.