Abstract: Provided is a composition for increasing muscle mass in a mammal, the composition including citric acid, a salt of citric acid, a hydrate thereof, or a mixture thereof.
Abstract: The present invention relates to PD-0184264 for use in a method for the prophylaxis and/or treatment of a co-infection comprising a bacterial infection and an influenza virus infection or a viral or bacterial infection alone. Also provided are compositions comprising such inhibitors for use in the prophylaxis and/or treatment of a co-infection comprising a bacterial infection and an influenza virus infection or a bacterial or viral infection alone.
Abstract: The disclosure is directed to methods of treating Parkinson's disease comprising administration of a capsule comprising an anti-parkinsonian medication and where the capsule's length is at least about 29 mm and the capsule's width at least about 9.5 mm.
Abstract: Disclosed are compounds, compositions and methods for antagonizing fibroblast activation. Particularly disclosed are compounds, methods and compositions for treating and/or preventing scar formation with a retinoid.
Type:
Application
Filed:
January 25, 2024
Publication date:
July 25, 2024
Inventors:
David Michael Dolivo, Adrian E. Rodrigues, Seok Jong Hong, Thomas A. Mustoe, Robert D. Galiano
Abstract: The present invention relates to a pharmaceutical composition for preventing or treating diabetes mellitus in an animal of the family Canidae, including enavogliflozin as an active ingredient. The pharmaceutical composition, of the present invention, including enavogliflozin as an active ingredient exhibits an excellent blood glucose level control effect and thus can be effectively used for treating diabetes mellitus in an animal of the family Canidae.
Type:
Application
Filed:
May 20, 2022
Publication date:
July 25, 2024
Inventors:
Wan Huh, Hyun Woo Lim, Ji Soo Choi, Ju Mi Han, Joon Seok Park
Abstract: Apparatuses, methods, and systems for extraction, isolation, purification, and conversion of various cannabinoids, and modifications of whole-plant hemp extracts therewith are presented. A method for preparing a whole-plant hemp extract based product includes extracting cannabinoids from plant materials, such as one or more hemp varieties of Cannabis sativa. The method also includes separating and purifying CBD from the extracted cannabinoids, converting purified CBD to ?9-THC and ?8-THC and concurrently converting ?9-THC to CBN, purifying and separating the CBN, and combining the purified CBN with a whole-plan hemp extract. Products and supplements related to the method are also described.
Type:
Application
Filed:
September 15, 2023
Publication date:
July 25, 2024
Inventors:
Alexander Michael MCCORKLE, Graham Taylor CARLSON, Shelby Renee SHEAHAN
Abstract: The present invention relates to the recognition that inhibition of the base excision repair pathway is selectively lethal in cells which are deficient in HR dependent DNA DSB repair. Methods and means relating to the treatment of cancers which are deficient in HR dependent DNA DSB repair using inhibitors which target base excision repair components, such as PARP, is provided herein.
Type:
Application
Filed:
September 22, 2023
Publication date:
July 25, 2024
Inventors:
Alan Ashworth, Stephen Jackson, Niall Martin, Graeme Cameron Murray Smith
Abstract: A pharmacological method for treating the expressive language deficit in an autistic human child or adult is provided. A therapeutically effective dose of a succinimide anticonvulsant, e.g., ethosuximide, methsuximide, phensuximide, or a pharmaceutically acceptable salt thereof, is administered to a patient suffering from expressive language deficit, preferably over an extended period, e.g., six months or longer. Language gains are retained even after treatment is discontinued.
Abstract: Provided herein are small molecule inhibitors of ASH1L activity and small molecules that facilitate ASH1L degradation and methods of use thereof for the treatment of disease, including acute leukemia, solid cancers and other diseases dependent on activity of ASH1L.
Type:
Application
Filed:
January 8, 2024
Publication date:
July 25, 2024
Inventors:
Jolanta GREMBECKA, Tomasz CIERPICKI, David ROGAWSKI, Dmitry BORKIN, Szymon KLOSSOWSKI, Zhuang JIN, Deanna MONTGOMERY, Jing DENG, Marta KROTOSKA, Hao LI
Abstract: The present invention is directed to a method for preventing and/or treating aging-related cognitive impairment in the central nervous system. The method comprises administering to a subject in need thereof a Ppangela activator 2-(4-tert-butylphenyl)-1H-benzimidazole, 2-[4-(1,1-dimethylethyl)phenyl]-1H-benzimidazole, in an effective amount. A preferred route of administration is oral administration.
Type:
Application
Filed:
November 29, 2023
Publication date:
July 25, 2024
Applicant:
THE BOARD OF TRUSTEES OF THE LELAND STANFORD JUNIOR UNIVERSITY
Abstract: The present disclosure provides a compound having the structure:
Type:
Application
Filed:
December 18, 2023
Publication date:
July 25, 2024
Applicants:
The Trustees of Columbia University in the City of New York, Albany College of Pharmacy and Health Sciences in the City of Albany, The Board of Regents of the University of Oklahoma
Inventors:
Konstantin Petrukhin, Christopher L. Cioffi, Yuhong Wang, Jian-xing Ma, Gennadiy Moiseyev
Abstract: Among others, the present invention provides methods and compositions for mimicking one or more biological benefits of caloric restriction in a mammal, including administering to the mammal an effective amount of Ergothioneine, an analog or derivative thereof, or a pharmaceutically acceptable salt, ester, polymer, acid, analog or derivative thereof.
Abstract: Disclosed herein are methods of administering relatively high doses of dexmedetomidine or a pharmaceutically acceptable salt thereof to a human subject, without also inducing significant sedation. The disclosed methods are particularly suitable for the treatment of agitation, especially when associated with neurodegenerative and/or neuropsychiatric diseases such as schizophrenia, bipolar illness such as bipolar disorder or mania, dementia, depression, or delirium.
Type:
Application
Filed:
February 28, 2023
Publication date:
July 25, 2024
Applicant:
BioXcel Therapeutics, Inc.
Inventors:
Vasukumar KAKUMANU, David Christian HANLEY, Frank YOCCA, Chetan Dalpatbhai LATHIA, Lavanya RAJACHANDRAN, Robert RISINGER
Abstract: Disclosed herein are methods of administering relatively high doses of dexmedetomidine or a pharmaceutically acceptable salt thereof to a human subject, without also inducing significant sedation. The disclosed methods are particularly suitable for the treatment of agitation, especially when associated with neurodegenerative and/or neuropsychiatric diseases such as schizophrenia, bipolar illness such as bipolar disorder or mania, dementia, depression, or delirium.
Type:
Application
Filed:
March 8, 2024
Publication date:
July 25, 2024
Applicant:
BioXcel Therapeutics, Inc.
Inventors:
Vasukumar KAKUMANU, David Christian HANLEY, Frank YOCCA, Chetan Dalpatbhai LATHIA, Lavanya RAJACHANDRAN, Robert RISINGER
Abstract: Aspects of the invention include methods of managing pain in a subject by applying a transdermal delivery device containing a dexmedetomidine composition formulated to deliver a pain relieving effective amount of dexmedetomidine to a subject experiencing pain. In practicing methods according to certain embodiments, a transdermal delivery device having a dexmedetomidine composition is applied to a subject and is maintained in contact with the subject in a manner sufficient to deliver an amount of dexmedetomidine effective to manage pain in the subject. Also provided are transdermal delivery devices configured to deliver dexmedetomidine sufficient for practicing the subject methods, as well as kits containing the transdermal delivery devices.
Abstract: A formulation comprising dantrolene, or a pharmaceutically acceptable salt thereof, and a cyclodextrin in a molar ratio of 1:3 to 1:12 and also comprising polyethylene glycol (PEG) with an average molecular weight in the range 1500 to 6000.
Type:
Application
Filed:
May 6, 2022
Publication date:
July 25, 2024
Applicant:
SPEPHARM AG
Inventors:
Samuel SMITH, Luke EDWARDS, Susanna SAUNDERS, Lorenzo MENCUCCINI
Abstract: There is provided adjunctive D-cycloserine (DCS) augmentation of transcranial magnetic stimulation (TMS) therapy for Major Depressive Disorder (MDD). There is also provided combination therapies and therapeutic methods that include intermittent or continuous theta-burst stimulation (iTBS or cTBS), high- or low-frequency stimulation or combinations thereof with D-cycloserine (DCS) to treat MDD in a patient and/or to improve and/or alleviate and/or reduce frequency of one or more symptoms of MDD as well as complications of MDD, including anxiety, cognitive function, and suicide.
Abstract: In an aspect, the invention relates to compositions and methods for treating sepsis, including but not limited neonatal sepsis and sepsis related to infection. In an aspect, the invention relates to compositions and methods for attenuating adverse conditions of sepsis resulting from enterovirus infection. In an aspect, the invention relates to improved formulations of antiviral agents such as pleconaril for the treatment, alleviation and prevention of conditions associated with sepsis.
Abstract: Methods of using glucokinase (GK) activators are generally disclosed herein, particularly in combination with insulin or insulin analogs. In certain aspects, the disclosure provides methods of treating type 1 diabetes that include administering a GK activator in combination with insulin or insulin analogs. Uses of GK activators as a medicament are also disclosed herein, as well as the manufacture of a medicament for such uses.
Type:
Application
Filed:
April 5, 2024
Publication date:
July 25, 2024
Inventors:
Jennifer L.R. FREEMAN, Maria Carmen VALCARCE LOPEZ
Abstract: The present invention relates to 2,4-disubstituted thiadiazolidinones of formula (I): or a pharmaceutically acceptable salt or solvate thereof, for its use in the treatment of limb girdle muscular dystrophy.
Type:
Application
Filed:
May 23, 2022
Publication date:
July 25, 2024
Inventors:
Ana MARTÍNEZ GIL, Valle PALOMO RUIZ, Miren Ametsa SÁENZ PEÑA, Adolfo José LÓPEZ DE MUNAIN ARREGI
Abstract: Provided herein is a compound of Formula (I): or a pharmaceutically acceptable salt thereof, wherein values for the variables (e.g., R1, R2, X1, X2, Y1, Y2, Y3, Y4, Y5, Y6, Y7, and Y8) are as disclosed herein. Also provided herein are pharmaceutical compositions comprising a compound of Formula (I), or a pharmaceutically acceptable salt thereof, and methods of using the compounds, pharmaceutically acceptable salts thereof and pharmaceutical compositions of the foregoing, e.g., to treat a neurological or psychiatric disease or disorder.
Abstract: Methods and uses are disclosed for treating a subject suffering from a disorder selected from a liver disorder, Cushing's syndrome, or Cushing's Disease, cancer, an infection, an inflammatory condition, a cardiovascular, endocrine, or kidney disease, and combinations thereof, or other disorder for which they may be administered a drug which may cause liver toxicity, without adverse effects on the liver. Such liver disorders include fatty liver diseases are effective for reducing high levels of liver enzymes with a favorable safety profile. The methods and uses comprise administering to the subject an effective amount of a selective nonsteroidal glucocorticoid receptor modulator such as relacorilant, including methods and uses in combination with another drug, without adverse effects on liver enzyme levels, or on liver function. In embodiments, the other drug may be a drug that may cause liver toxicity, such as drugs that inhibit CYP3A enzymes, e.g., itraconazole or ketoconazole.
Abstract: The present disclosure relates to methods of treating gastrointestinal stromal tumors to a subject in need thereof, comprising administering to the subject a therapeutically effective amount of ripretinib or a pharmaceutically acceptable salt thereof.
Type:
Application
Filed:
December 20, 2023
Publication date:
July 25, 2024
Inventors:
Kam M. Sprott, Matthew L. Sherman, Rodrigo Ruiz Soto
Abstract: Disclosed are agents, compositions, and methods for treating acute kidney injury (AKI). Particularly disclosed are agents, compositions, and methods for treating AKI and reducing the progression from AKI to chronic kidney disease by administering an agent that inhibits or reduces expression of monocarboxylate transporter 4 (MCT4).
Abstract: The present disclosure provides methods for the acute treatment of migraine with or without aura, comprising the administration of ubrogepant. In particular, the present disclosure provides methods for the acute treatment of migraine in patients having hepatic impairment; in patients with renal impairment; and in patients concurrently taking CYP3A4 modulators or BCRP and/or P-gp only inhibitors.
Type:
Application
Filed:
March 1, 2024
Publication date:
July 25, 2024
Inventors:
Joel M. Trugman, Ramesh Boinpally, Abhijeet Jakate, Michelle Finnegan
Abstract: The present disclosure relates to pharmaceutical solid forms and pharmaceutical compositions comprising ibutamoren or a pharmaceutically acceptable salt thereof, and methods for administering to a pediatric subject for treating growth hormone deficiency.
Abstract: The present disclosure is generally directed to compositions and methods related to USP15 inhibitors. More particularly, the present disclosure relates to methods of regulating CRL4CRBN-USP15 pathway (previously referred to as the CRL4CRBN-p97 pathway) and glutamine synthetase levels and methods of treating diseases such as cancer via administration of USP15 inhibitors.
Abstract: This invention discloses uses for nicardipine in preparing anti-lung cancer products. This invention provides uses for nicardipine in the preparation of products to treat non-small cell lung cancer. From carrying out cancer drug repositioning for the FDA- and CFDA-approved drug nicardipine, experiments for this invention show, based on screening of non-anti-cancer drugs for various cancer cell lines (tissue types) and mutation sites, that nicardipine has a new use as an anti-small cell lung cancer and/or anti-non small cell lung cancer medication, thus achieving a new purpose for an old drug.
Abstract: The present disclosure relates to dosing regimens and combinations comprising N-[4-(Chlorodifluoromethoxy)phenyl]-6-[(3R)-3-hydroxypyrrolidin-1-yl]-5-(1H-pyrazol-5-yl)pyridine-3-carboxamide or a pharmaceutically acceptable salt thereof, and their use for the treatment of breakpoint cluster region-abelson protein (BCR-ABL) mediated diseases or disorders.
Type:
Application
Filed:
May 10, 2022
Publication date:
July 25, 2024
Inventors:
Stephanie Kay DODD, Florence HOURCADE-POTELLERET, Felix HUTH, Michelle QUINLAN, Julia ZACK
Abstract: Compounds, compositions, and methods useful for inducing cancer cell death via methuosis, autophagy, or a combination thereof, are described. The compounds have a 4-pyridyl group linked by a heterocyclic group to an aryl, heteroaryl, aralkyl, or heteroaryl alkyl.
Type:
Application
Filed:
March 29, 2024
Publication date:
July 25, 2024
Applicant:
The University of Toledo
Inventors:
Amit K. Tiwari, Chandrabose Karthikeyan, Haneen A. Amawi, Paul W. Erhardt, Piyush Trivedi
Abstract: A preventive or therapeutic agent for glaucoma or ocular hypertension includes a combination of isopropyl (6-{[4-(pyrazol-1-yl)benzyl](pyridin-3-ylsulfonyl) aminomethyl}pyridin-2-ylamino)acetate with one or more other preventive or therapeutic drugs for glaucoma or ocular hypertension, with the proviso that tafluprost is excluded.
Abstract: The present disclosure relates to choline salts, and crystalline forms thereof, of a compound which is N—((S)-1-(3-(4-chloro-3-(methylsulfonamido)-1-(2,2,2-trifluoroethyl)-1H-indazol-7-yl)-6-(3-methyl-3-(methylsulfonyl)but-1-yn-1-yl)pyridin-2-yl)-2-(3,5-difluorophenyl)ethyl)-2-((3bS,4aR)-5,5-difluoro-3- (trifluoromethyl)-3b,4,4a,5-tetrahydro-1H-cyclopropa[3,4]cyclopenta[1,2-c]pyrazol-1-yl)acetamide, which is useful in the treatment and prevention of a Retroviridae viral infection including an infection caused by the HIV virus.
Abstract: The present disclosure relates to dosing regimens, formulations, and combinations comprising 3-(1-oxoisoindolin-2-yl)piperidine-2,6-dione compounds or pharmaceutical compositions comprising the same; and methods of using such combinations and compositions in the treatment or prevention IKAROS Family Zinc Finger 2 (IKZF2)-dependent diseases or disorders or where reduction of IKZF2 or IKZF4 protein levels can ameliorate a disease, for example, the treatment of cancers.
Type:
Application
Filed:
December 19, 2019
Publication date:
July 25, 2024
Inventors:
Simone BONAZZI, Adam Crystal, John Scott Cameron, Eva Marie Genevieve D'Hennezel, Glenn Dranoff, Ry Roger Forseth, Dominik Johannes Hainzl, Jacqueline Kinyamu-Akunda, Guiqing Liang, Lilly Mary Petruzzelli
Abstract: The present application belongs to the technical field of proteolysis-targeting chimeras (PROTACs), and discloses a PROTAC molecule and a preparation method and use thereof. A ligand for a target protein in the PROTAC molecule of the present application is a pyridine carboxylic acid-1-oxide derivative. In cell and zebrafish experiments, the PROTAC molecule exhibits no toxic and side effects at a drug concentration allowing a desired effect. At a cellular level, an inhibition level of the PROTAC molecule for human tyrosinase (TYR) reaches less than or equal to 1 ?mol/L. The PROTAC molecule in the present application can significantly reduce the generation of melanin by degrading TYR, and has excellent solubility, safety, and efficacy and a low effective concentration.
Abstract: A pharmaceutical composition, comprising a compound having chemical structural formula I: where R1 is selected from the group consisting of: an alkyl group, a heteroalkyl group, an aryl group, a heteroaryl group, an alkenyl group, a heteroalkenyl group, an alkynyl group, a heteroalkynyl group, a cycloalkyl group, a hetercycloalkyl group, an alkylcycloalkyl group, a heteroalkyl cycloalkyl group, an aralkyl group, a heteroaralkyl group, an alkoxy group, a polar group, an ester and a charged group; a pharmaceutically acceptable hydrolysable, or enzymatically cleavable, prodrug form thereof; and/or a pharmaceutically acceptable salt thereof; where R4? is H or an alkoxy group; where both R5 and R3? are OH, and where one or both OH groups is modified as a pharmaceutically acceptable hydrolysable, or enzymatically cleavable, prodrug form thereof, wherein the prodrug form thereof comprises an ester selected from: an amino acid ester, a phosphate ester, and a sulfonate ester.
Abstract: The invention relates to compounds of Formula (I) and pharmaceutically acceptable salts thereof as defined in the description; to their use in medicine; to compositions containing them; to processes for their preparation; and to intermediates used in such processes. The compounds of Formula (I) may inhibit the activity of papain-like protease (PLpro) and may be useful in the treatment of viral infections, in particular viral infections associated with PLpro activity and/or expression such as coronaviruses infections.
Type:
Application
Filed:
December 7, 2023
Publication date:
July 25, 2024
Applicant:
Pfizer Inc.
Inventors:
James Matthew Frick, Michelle Renee Garnsey, Brian Stephen Gerstenberger, Xinjun Hou, Magdalena Korczynska, Alpha Albert Lee, Luong Tien Nguyen, Usa Reilly, Matthew Christopher Robinson, Alexandria Paige Taylor, Thomas Reynold Vargo, Lei Zhang
Abstract: The present disclosure provides diagnostic methods and compositions usefid in the identification of patients and cancers that are amenable to treatment with cancer therapies, including agonist therapies against cancer targets that exist in normal and cancerous cells and tissues.
Type:
Application
Filed:
May 18, 2022
Publication date:
July 25, 2024
Inventors:
Christopher NATALE, Tina GARYANTES, Patrick MOONEY
Abstract: The present invention features compounds useful in the inhibition of the secretion of proteins. The compounds of the invention can be used in methods for treating diseases associated with protein secretion, and in methods for inhibiting protein secretion.
Type:
Application
Filed:
January 29, 2024
Publication date:
July 25, 2024
Inventors:
Jordi MATA-FINK, Phillip Patrick SHARP, Raman TALWAR
Abstract: Processes for providing depot injections of recrystallized aripiprazole lauroxil in which particles of the aripiprazole lauroxil have a surface area of about 0.50 to about 3.3 m2/g; and crystals of aripiprazole lauroxil produced by such processes.
Type:
Application
Filed:
December 18, 2023
Publication date:
July 25, 2024
Inventors:
Wilfredo Morales, Tarek A. Zeidan, Renato A. Chiarella, Steven G. Wright, Jason M. Perry
Abstract: Selected BRD9 protein degradation compounds and morphic forms thereof are provided for the treatment of disorders mediated by BRD9, including but not limited to abnormal cellular proliferation.
Type:
Application
Filed:
March 8, 2024
Publication date:
July 25, 2024
Applicant:
C4 THERAPEUTICS, INC.
Inventors:
Katrina L. Jackson, Christopher G. Nasveschuk, Rhamy Zeid, Ning Yin, Gesine Kerstin Veits, Moses Moustakim, Jeremy L. Yap, Minsheng He, Robert T. Yu, Matthew J. Schnaderbeck, Kathleen Neville, Siyi Jiang, Meiqi Li, Qianwei Liu, Manjie Zheng, Jia Li, Liwei Zhang
Abstract: The invention provides methods of treatment of heart failure with reduced ejection fraction (HFrEF) using modified forms of trimetazidine, such as CV-8972 and CV-8814.
Abstract: This agent for treating coronavirus infectious diseases caused by mutant viruses of SARS-COV-2 contains, as an active ingredient, 6-fluoro-3-hydroxy-2-pyrazinecarboxamide or a salt thereof.
Abstract: The invention relates to methods of treating certain retinal vasculopathies such as diabetic macular edema, diabetic retinopathy and dry and neovascular age-related macular degeneration, among others. In some instances, the method includes treating a patient suffering from a retinal vasculopathy by administering an agent to the patient. The agent can be one or more of the agents as described herein.
Abstract: This invention provides a compound of formula I, their synthesis and their use for treating a SHP2 mediated disorder. More particularly, this invention provides a pharmaceutical composition comprising the said compound.
Type:
Application
Filed:
February 29, 2024
Publication date:
July 25, 2024
Inventors:
Huifeng Han, Panliang Gao, Cunbo Ma, Di Kang
Abstract: The disclosure relates to compounds of formula (A) and formula (I), e.g.: or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, L1, L2, L3, Y, and Q are as described herein. Compounds of formula (A) and formula (I) and pharmaceutical compositions thereof are inhibitors of at least one or more of ?V?8, ?V?1, and ?V?6 integrins. Also disclosed are methods for treating fibrosis such as nonalcoholic steatohepatitis (NASH), idiopathic pulmonary fibrosis (IPF) and nonspecific interstitial pneumonia (NSIP), and cancer comprising administration of the compounds and pharmaceutical compositions thereof.
Type:
Application
Filed:
December 22, 2023
Publication date:
July 25, 2024
Inventors:
Timothy D. MACHAJEWSKI, Darren FINKELSTEIN, Timothy F. HOM, Dennis MONTELEONE, Manuel Angel MUNOZ, Katerina LEFTHERIS
Abstract: Compositions and methods for treatment of cancer according to aspects of the present disclosure comprise compounds comprising or consisting of: structural formula (I) or (II) disclosed herein, or a salt, isomer, or derivative thereof.
Abstract: Nitric oxide releasing phosphodiesterase type 5 (PDE5) inhibitors of formula (I) or (Ib) or (II) or a stereoisomer or a pharmaceutically acceptable salt thereof: useful for the treatment of ocular condition associated with elevated intraocular pressure such as ocular hypertension, glaucoma or retinopathies. Also disclosed are 3-[(2S)-2,3-bis(nitrooxy)propoxy]propanoic acid and 6-(nitrooxy)hexanoic acid for use in the treatment of ocular condition associated with elevated intraocular pressure such as ocular hypertension, glaucoma or retinopathies.
Type:
Application
Filed:
March 22, 2024
Publication date:
July 25, 2024
Inventors:
Nicoletta ALMIRANTE, Stefania BRAMBILLA, Laura STORONI, Francesco IMPAGNATIELLO, Elena BASTIA
Abstract: Combination oral formulations comprising a phosphodiesterase-5 inhibitor and an additional active agent that can reduce or eliminate a side effect associated with phosphodiesterase-5 inhibitor therapy are described. Methods of treatment using the combinations and kit formulations are included.
Type:
Application
Filed:
February 8, 2024
Publication date:
July 25, 2024
Inventors:
Siva Rama Krishna Nutalapati, Victor Chehebar