Abstract: A pharmaceutical composition for modified release comprising (R)-2-(2-aminothiazol-4-yl)-4?-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetic acid anilide or a pharmaceutically acceptable salt thereof, and a carrier for a sustained release pharmaceutical composition, wherein a maximum blood drug concentration (Cmax) when administered in a fasted state is 400 ng/mL or less, is disclosed.
Abstract: The present invention relates to substituted dihydroimidazopyridinedione compounds of general formula (I) as described and defined herein, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyperproliferative, angiogenesis disorders, inflammatory diseases or diseases associated with inflammatory pain, as a sole agent or in combination with other active ingredients.
Abstract: The present invention relates to stable pharmaceutical compositions of dihydroergotamine mesylate or other pharmaceutically acceptable salts thereof and methods for preparing the compositions particularly for the treatment of migraine headaches. The invention further relates to stable injectable composition comprising dihydroergotamine or its pharmaceutically acceptable salts thereof, wherein the composition has a pH from about 5.0 to about 6.0. Further, the present invention relates to a method of treating migraine comprising providing a stable pharmaceutical composition for parenteral administration comprising dihydroergotamine mesylate, wherein the pH of the composition ranges from 5.0 to 6.0 and, wherein the composition comprises no greater than 3% of total impurities as determined by HPLC.
Abstract: A pyridone derivative compound and a pharmaceutically acceptable salt, isomer, solvate or hydrate thereof, and a preventive or therapeutic pharmaceutical composition for cognitive disorders that includes the pyridone derivative compound or a pharmaceutically acceptable salt, isomer, solvate or hydrate thereof.
Type:
Application
Filed:
December 1, 2020
Publication date:
March 25, 2021
Inventors:
Cheol Young MAENG, Young Koo JANG, Su Bong CHA, Hye Won SHIN, Chan Mi JOUNG, Eun Jung YI
Abstract: A first aspect of the invention relates to betahistine, or a pharmaceutically acceptable salt thereof, and a monoamine oxidase inhibitor, for use in the treatment or prevention of one or more symptoms of vertigo in a subject. A second aspect of the invention relates to a method of treating or preventing one or more symptoms of vertigo in a subject, said method comprising administering to the subject (i) betahistine, or a pharmaceutically acceptable salt thereof, and (ii) a monoamine oxidase inhibitor.
Abstract: Provided are methods for treatment of Fabry disease in patients having HEK assay amenable mutations in ?-galactosidase A. Certain methods comprise administering migalastat or a salt thereof every other day, such as administering about 150 mg of migalastat hydrochloride every other day.
Abstract: Provided are methods for treatment of Fabry disease in patients having HEK assay amenable mutations in ?-galactosidase A. Certain methods comprise administering migalastat or a salt thereof every other day, such as administering about 150 mg of migalastat hydrochloride every other day.
Abstract: The inventors surprisingly found that FXR plays a determinant role in the maintenance of viral episome in cells from tissues that are not specialized in bile salt synthesis and transport as the liver or the intestine. In particular, the inventors show that FXR agonist could be suitable for inhibiting the replication of viruses (e.g. BKV and HIV-1) that persist in the cell in an episomal and extrachromosomal form of DNA. Accordingly the present invention relates to a method of reducing persistence and expression of an episomal virus in a subject in need thereof comprising administrating to the subject a therapeutically effective amount of a FXR agonist.
Abstract: The present invention provides, inter alia, methods, pharmaceutical compositions, and kits for treating or ameliorating the effects of a cancer in a subject, which harbors an atypical BRAF mutation (i.e. a non-V600E/K BRAF mutation), comprising an ERK inhibitor. Also provided are methods for identifying a subject having an atypical BRAF mutant cancer who would benefit from therapy comprising an ERK inhibitor.
Type:
Application
Filed:
May 15, 2018
Publication date:
March 25, 2021
Inventors:
Gary DeCrescenzo, Dean Welsch, Saurabh Saha
Abstract: The present application relates to substituted indazoles, to the use thereof alone or in combinations for treatment and/or prophylaxis of autoimmune disorders, and to the use thereof for production of medicaments for treatment and/or prophylaxis of autoimmune disorders, especially for treatment and/or prophylaxis of arthritides (especially psoriatic arthritis, rheumatoid arthritis, Bekhterev's disease, reactive arthritis, systematic juvenile idiopathic arthritis), systematic lupus erythematosus, multiple sclerosis, psoriasis, atopic dermatitis, allergic eczema and chronic-inflammatory bowel disorders (especially Crohn's disease and ulcerative colitis).
Type:
Application
Filed:
April 30, 2020
Publication date:
March 25, 2021
Applicant:
Bayer Pharma Aktiengesellschaft
Inventors:
Alexandra RAUSCH, Stefan Joachim JODL, Jörn KRÄTZSCHMAR, Ulrich BOTHE, Nicole SCHMIDT
Abstract: Pharmaceutical compositions and single unit dosage forms of 4-amino-2-(2,6-dioxopiperidine-3-yl)isoindoline-1,3-dione, or a pharmaceutically acceptable stereoisomer, prodrug, salt, solvate, hydrate, or clathrate, are provided herein. Also provided are methods of treating, managing, or preventing various disorders, such as cancer or an inflammatory disease.
Abstract: A gel composition is provided, including an alkaloid compound, or a cannabinoid compound, or both an alkaloid compound and a cannabinoid compound; glycerol; a viscosifying agent; a hydrogen-bond crosslinking gelling agent; and an ionic crosslinking gelling agent; and an acid.
Abstract: The present invention relates to tetrahydroquinoline derivatives of the present invention or a pharmaceutically acceptable salt thereof or a prodrug thereof, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders which are mediated via the P2X7 receptor.
Abstract: The present invention derives from the unexpected finding that ADRA2a antagonists decrease fibrosis in non-alcoholic fatty liver disease (NAFLD). Thus, by antagonising ADRA2a, many of the unwanted consequences or symptoms of NAFLD, may be reduced, such as impaired cognitive activity and fibrosis progression. The present invention utilises these findings to identify and provide ADRA2a antagonists that may be used in the treatment of fibrosis in NAFLD.
Abstract: Methods of treating patients diagnosed with AML or MDS harboring mutant IDH-1 include detecting an IDH1 mutation and the therapeutic administration of an inhibitor of a mutant IDH-1 as a single agent, or in combination with azacitidine (AZA) or cytarabine.
Type:
Application
Filed:
December 4, 2020
Publication date:
March 25, 2021
Inventors:
Patrick F. Kelly, Alan Collis, Jeff Davis, Duncan Walker, Susan Ashwell, Blythe Thomson, Wei Lu
Abstract: Methods for treating a subject having a cancerous tumor are disclosed. The methods comprise administering to the subject an effective amount of a non-steroidal selective glucocorticoid receptor modulator (SGRM) and an effective amount of a chemotherapeutic agent. The tumor may be cervical cancer. The SGRM may be a fused azadecalin. In embodiments, the SGRM may be a heteroaryl ketone fused azadecalin or an octahydro fused azadecalin.
Abstract: This disclosure pertains to new compositions and methods comprising a first serotonergic drug and a second serotonergic drug. In one embodiment, the compositions disclosed herein are used for a method of regulating a neurotransmitter receptor, e.g., a serotonin receptor. In one embodiment, the compositions disclosed herein comprise purified compounds, e.g., a purified psilocybin derivative, a purified cannabinoid, a purified terpene, a purified tryptamine, purified LSD, and/or purified MDMA.
Abstract: Described herein are solid, pharmaceutical compositions, dosage forms and methods of making and using the same, wherein the solid compositions comprise at least one high viscosity agent. The solid, high viscosity agent-comprising pharmaceutical compositions, when comprised of an opioid drug, can reduce the potential for abuse of such drug. The solid dosage forms are characterized by having a significantly reduced extractability of an opioid drug comprised therein upon contact of the dosage form with a solvent such as a typical household solvent. The solid dosage forms, following contact with a household solvent, such as an aqueous or alcoholic solvent, generate a high viscosity solution, thereby discouraging abuse of the resulting formulation via intravenous (IV) injection.
Type:
Application
Filed:
July 25, 2018
Publication date:
March 25, 2021
Inventors:
Sindhuri Maddineni, Shailendra Mandge, Sourish Mukherjee, Vinod Balakrishnan Nair, Vijaya Srinivas Sekuboyina, Praveen Gaddam, Kevin J. Brodbeck, Ramakrishna Gadiraju, Xue Ge, Michael A. Eldon, Aleksandrs Odinecs, Satyanarayana Goda, Rajendra Tandale, Shiladitya Bhattacharya
Abstract: The present invention provides a method of providing pain relief in a human subject in need thereof comprising administering (R)-dihydroetorphine to said subject, wherein said (R)-dihydroetorphine is administered in a dose of at least 0.01 ?g/kg, preferably at least 0.05 ?g/kg, and the level of respiratory depression in said subject is 65 or less % relative to the baseline level pre-administration of (R)-dihydroetorphine.
Type:
Application
Filed:
September 30, 2020
Publication date:
March 25, 2021
Applicant:
EURO-CELTIQUE S.A.
Inventors:
John WATKINS, Alexander Oksche, Kevin Smith, Heikki Mansikka, Paul Bailey
Abstract: The invention provides new therapeutic uses of 1-[2-(2,4-dimethyl-phenylsulfanyl)phenyl]-piperazine and pharmaceutically acceptable salts thereof.
Abstract: In a hybrid computing system including at least one analog processor and at least one digital processor an embedded problem is repeatedly run or executed on the analog processor(s) to generate a first plurality of candidate solutions to the computational problem, the candidate solutions are returned to the digital processor(s) which determine a value for at least one statistical feature of the candidate solutions, at least one programmable parameter of the plurality of analog devices in the analog processor(s) is adjusted to at least partially compensate for deviations from an expected value of the at least one statistical feature, the expected value of the at least one statistical feature inferred from the structure of the embedded problem, the embedded problem is again repeatedly run or executed on the analog processor(s) to generate a second plurality of candidate solutions to the computational problem.
Type:
Application
Filed:
January 22, 2019
Publication date:
March 25, 2021
Inventors:
Guangrong Zheng, Daohong Zhou, Xuan Zhang, Sajid Khan, Yonghan He, Peiyi Zhang
Abstract: The present invention includes methods and compositions for treating a skeletal muscular atrophy caused by a defect in the function of one or more sarco/endoplasmic reticulum Ca2+-ATPase (SERCA) pumps comprising: identifying a subject having a muscular atrophy caused by a defect in the function of the one or more SERCA pumps, and providing the subject with an effective amount of an activator that enhances an activity of the one or more SERCA pumps.
Abstract: The disclosure is in part directed to crystalline forms of (R)-1?-(3-(3,4-dihydro-1,5-naphthyridin-1(2H)-yl)-1H-pyrazolo[3,4-b]pyrazin-6-yl)-3H-spiro[benzofuran-2,4?-piperidin]-3-amine, its salt, and variants thereof.
Type:
Application
Filed:
September 23, 2020
Publication date:
March 25, 2021
Inventors:
Alexander M. Taylor, André Lescarbeau, Jing Wang, Yanyan Zhang, Gaodeng Lian
Abstract: The present invention provides, inter alia, compositions and methods for using CB1 cannabinoid receptor agonists, or other compounds capable of increasing endocannabinoids or endocannabinoid signaling, for treating and preventing lysosomal storage disorders in which lipid storage occurs (including, e.g., disorders associated with sphingomyelin accumulation). In particular embodiments, the present invention provides compositions and methods for treating such lysosomal storage disorders with one or more fatty acid amide hydrolase inhibitor alone or in combination with one or more additional agent.
Type:
Application
Filed:
March 5, 2019
Publication date:
March 25, 2021
Inventors:
Maria Dolores LEDESMA, Adrian BARTOLL, Edward H. SCHUCHMAN
Abstract: The invention provides methods of treating or preventing malaria comprising administering to an animal an effective amount of a compound of formula I: Q-Y—R1—R2??(I), wherein Q, Y, R1, and R2 are as described herein. Methods of inhibiting a plasmodial surface anion channel of a parasite in an animal are also provided. The invention also provides pharmaceutical compositions comprising a compound represented by formula I in combination with any one or more compounds represented by formulas II, V, and VI. Use of the pharmaceutical compositions for treating or preventing malaria or for inhibiting a plasmodial surface anion channel in animals including humans are also provided. Also provided by the invention are clag3 amino acid sequences and related nucleic acids, vectors, host cells, populations of cells, antibodies, and pharmaceutical compositions.
Type:
Application
Filed:
December 8, 2020
Publication date:
March 25, 2021
Applicant:
The United States of America,as represented by the Secretary,Department of Health and Human Services
Abstract: Disclosed herein are methods for treating a subject afflicted with a cancer having an activating RET alteration by administering an effective amount of a selective RET inhibitor, e.g., Compound 1 or pharmaceutically acceptable salts thereof, including, e.g., administering an amount of 60 mg to 400 mg of the selective RET inhibitor once daily.
Abstract: The present disclosure relates to compositions and methods for treating retinal damage and/or retinal degradation. More specifically, this disclosure relates to methods for treating degradation of the retinal pigment epithelium by administering compositions comprising a nucleoside and/or a nucleoside or nucleotide reverse transcriptase inhibitor.
Abstract: The present invention relates to combination therapies for treating KRas G12C cancers. In particular, the present invention relates to methods of treating cancer in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of a combination of a an agent that blocks Programmed Death-1 receptor (PD-1) and Programmed Death Ligand-1 (PD-L1) signaling and a KRAS G12C inhibitor of Formula (I), Formula I-A or Formula I-B, kits comprising the compositions and methods of use therefor.
Type:
Application
Filed:
September 23, 2020
Publication date:
March 25, 2021
Inventors:
David Briere, James Gail Christensen, Pete Olson
Abstract: The present invention relates to PDE9 inhibitors, their synthesis, and their use for treatment of benign prostate hyperplasia, beta thalassemia, and sickle cell disease.
Type:
Application
Filed:
October 9, 2020
Publication date:
March 25, 2021
Inventors:
Niels Svenstrup, Anna I. Parachikova, James McArthur
Abstract: The present invention relates to methods of treating, preventing, and/or improving disorders and conditions related to certain metabolic abnormalities including methods of improving blood lipid profiles and muscle recovery and repair in athletes, methods of treating fibromyalgia, erectile dysfunction, diseases associated with certain HLA-DQ gene alleles and/or gluten intolerance, including Celiac Disease, headaches and migraines, as well as idiopathic neuropathy, inability to sleep, inability to concentrate, and/or neurological development issues in children, the methods involving the administration of one or more downstream folate compounds and optionally methyl-B12. In one particular embodiment, the method comprises administration of L-methylfolate. In certain embodiments, the method further involves identifying a subject organism with a malfunction in one or more of the folate or B4 cycles. In certain embodiments, such a malfunction is one or more of the C677T and A1298C genetic polymorphisms.
Type:
Application
Filed:
December 8, 2020
Publication date:
March 25, 2021
Inventors:
Stephen Albert Lonnie Smith, Jeffrey Lynn Barringer, Craig Jay Brown, Brian Buell, Stephanie Michelle Ott, Gilberto Sanchez
Abstract: The present invention is aimed at a novel composition for use as a medicament; it is also aimed at said composition for use in the treatment of depressive and anxiety syndromes. In particular, said composition is for use in the treatment of: major depression, generalized anxiety disorder, social phobia, panic disorder, mixed depression and anxiety disorder, somatoform disorder, treatment-resistant depression, obsessive-compulsive disorder. The invention also relates to a process for the preparation of said pharmaceutical composition.
Abstract: The application relates to a pharmaceutical combination of an allosteric EGFR inhibitor of Formula Ia or Ib: or a pharmaceutically acceptable salt, hydrate, or solvate thereof, and an ATP-competitive EGFR inhibitor of Formula I?: or a pharmaceutically acceptable salt, hydrate, or solvate thereof, which modulates the activity of EGFR, a pharmaceutical composition comprising the combination, and a method of treating or preventing a disease in which EGFR plays a role.
Type:
Application
Filed:
February 20, 2019
Publication date:
March 25, 2021
Inventors:
NATHANAEL S. GRAY, DRIES DE CLERCQ, JAEBONG JANG, PASI JANNE, CIRIC TO, MICHAEL ECK, EUNYOUNG PARK
Abstract: Prostamide-containing biodegradable intraocular implants, prostamide compounds, prostamide-containing pharmaceutical compositions, and methods for making and using such implants and compositions for the immediate and sustained reduction of intraocular pressure and treatment of glaucoma in an eye of a patient are described.
Type:
Application
Filed:
May 6, 2020
Publication date:
March 25, 2021
Inventors:
Patrick M. Hughes, Jie Shen, Michael R. Robinson, David F. Woodward, Robert M. Burk, Hui Liu, Jinping Wan, Chandrasekar Durairaj, Gyorgy F. Ambrus, Ke Wu, Danny T. Dinh
Abstract: The invention provides a composition comprising one or more hydroxytryptamides and method of its use in the treatment of neurodegenerative disorders. The invention includes embodiments wherein the composition comprises caffeine and chlorogenic acids. The composition finds use in the treatment of Alzheimer's disease and Parkinson's disease, including providing neuroprotection against the advancement of the symptoms of these disorders.
Abstract: Pharmaceutical compositions and methods of use including a benzodiazepine-based compound, an NMDA antagonist, and optionally a ?-blocker, antiemetic, an NSAID, and/or an antihistamine medication.
Abstract: Compositions of Allopregnanolone (Allo), and methods of use thereof for treating and preventing Alzheimer's Disease (AD) or dementia, have been developed. In some embodiments, the amount of Allo effective to treat AD or dementia is between about 2 mg and about 10 mg, preferably 4 mg per dose. Methods for identifying subjects for treatment of AD or dementia are also provided. The methods include selecting a subject having one or more Apo E4 gene alleles. Methods of treating a human subject having AD or at risk of AD or dementia are provided. The methods include administering a dosage of from 2 mg to 6 mg to the subject once within a 24 hour period. The dosing is repeated every seven days, or less frequently. The methods stimulate mitosis of neural progenitor cells, stimulate neurite growth and organization, protect against neural loss, or one or more of these neural processes.
Type:
Application
Filed:
March 13, 2019
Publication date:
March 25, 2021
Applicant:
University of Southern California
Inventors:
Roberta Diaz BRINTON, Kathleen E. ROGERS
Abstract: The invention provides methods for treating a subject afflicted with a memory impairment or a cognitive dysfunction. Additional methods for improving memory and memory related functions in healthy subjects are also provided. The Methods include administration of an inhibitor of Na/K-ATPase.
Abstract: The present invention is related to compositions and methods for treating or reducing the likelihood of a migraine, reducing the severity of migraine, reducing the frequency of migraines, reducing the duration of migraine, and ameliorating the symptoms of a migraine. The methods and compositions of the present invention may also be used to treat or prevent condition characterized by increased cardiovascular risk or endothelial dysfunction and musculoskeletal symptoms.
Abstract: An ophthalmic formulation, comprising a chelator (such as EDTA and its salts), and a transport enhancer (such as Methyl Sulfonyl Methane; MSM) and an effective amount of a viscoelastic polymer (such as hydroxymethyl cellulose; HEC) is provided. Together, the combination of the two substances unexpectedly and beneficially reduces discomfort associated with and increases efficacy of chelator/transport enhancer as compared to formulations without the viscoelastic polymer.
Abstract: The present invention relates to a novel use for HDL-ApoM-S1P (a high density lipoprotein in which apolipoprotein M is impregnated with sphingosine-1-phosphate), and more particularly, to using HDL-ApoM-S1P to prevent, improve, or treat degenerative brain disorders (in particular, Alzheimer's disease), cognitive disorders, learning disabilities, and memory disorders, and using HDL-ApoM-S1P to improve cognitive ability, learning ability, and memory. The HDL-ApoM-S1P according to the present invention not only alleviates neuroinflammation but also significantly exhibits improvement effects of cognitive disorder, learning disability, and memory disorder with respect to individuals suffering from degenerative brain disorders (in particular, Alzheimer's disease), and exhibits an effect of greatly reducing amyloid beta and tau deposition. Moreover, increased HDL-ApoM-S1P in the body also has an excellent effect of improving the cognitive, learning, and memory abilities of non-disabled individuals.
Type:
Application
Filed:
July 11, 2018
Publication date:
March 25, 2021
Inventors:
Jae Sung Bae, Hee Kyung Jin, Ju Youn Lee, Min Hee Park
Abstract: The present invention provides improved processes for extracting and preparing lipids from biological sources for use in pharmaceuticals, nutraceuticals and functional foods.
Type:
Application
Filed:
December 9, 2020
Publication date:
March 25, 2021
Inventors:
Finn Myhren, Nils Hoem, Asgeir Saebo, Anil R. Oroskar, Asha A. Oroskar, Anantha Krishna Mallia
Abstract: The present invention provides pharmacological compounds including an effector moiety conjugated to a binding moiety that directs the effector moiety to a biological target of interest. Likewise, the present invention provides compositions, kits, and methods (e.g., therapeutic, diagnostic, and imaging) including the compounds. The compounds can be described as a protein interacting binding moiety-drug conjugate (SDC-TRAP) compounds, which include a protein interacting binding moiety and an effector moiety. For example, in certain embodiments directed to treating cancer, the SDC-TRAP can include an Hsp90 inhibitor conjugated to a cytotoxic agent as the effector moiety.
Type:
Application
Filed:
September 23, 2020
Publication date:
March 25, 2021
Inventors:
Dinesh U. Chimmanamada, Weiwen Ying, Junyi Zhang, Teresa Kowalczyk-Przewloka, Jun Jiang, Sami Osman, Genliang Lu, Dharma Vutukuri, James Loch, Shoujun Chen
Abstract: Disclosed herein are methods, sodium-dependent glucose transporter (SGLT)1 compounds and compositions for the treatment of postprandial hypoglycemia, postprandial hypoglycemia that occurs as a consequence of gastric surgery.
Type:
Application
Filed:
March 28, 2019
Publication date:
March 25, 2021
Inventors:
William WILKISON, Bentley CHEATHAM, James T. GREEN
Abstract: The subject of the present invention is a synthetic polysulfated oligosaccharide having 1 to 4 monosaccharide units, salts thereof, and complexes thereof, for use thereof for treating diabetic foot ulcer in arteriopathic patients.
Type:
Application
Filed:
May 16, 2018
Publication date:
March 25, 2021
Applicant:
Urgot Recherche Innovation et Developpement