Abstract: The present invention relates to a stable oral formulation comprising 1-(3-cyano-1-isopropyl-indol-5-yl)pyrazol-4-carboxylic acid or a pharmaceutically acceptable salt thereof as an API. The stable oral formulation according to the present invention has the characteristics of maintaining stability even if it does not comprise a stabilizer as an excipient, and does not comprise a stabilizer but has increased API content, and thus the convenience of administration can be increased.
Type:
Application
Filed:
November 30, 2021
Publication date:
January 4, 2024
Applicant:
LG CHEM, LTD.
Inventors:
Seok Cheol YOO, Sun LEE, Duck Il YUN, Junghong PARK, Hyun Ji SUN
Abstract: The present invention refers to a microsuspension against parasites in animals and its method of preparation, more particularly intended for the veterinary industry. The microsuspension against parasites comprises macrocyclic lactone and albendazole sulfoxide having an average particle size of D50?250 ?m.
Abstract: The present disclosure relates to methods and compositions for increasing or extending lifespan and/or healthspan and/or delaying aging using agents which mimic the effects of time-restricted feeding and/or activate or enhance circadian-regulated autophagy. In particular, the present disclosure relates to increasing certain proteins including UNC-51-like kinase (ULK1), adenosine monophosphate protein kinase (AMPK) and microtubule-associated protein, light chain 3 (LC3), and decreasing other certain proteins including ribosomal protein S6 kinase beta-1 (S6K) protein in order to increase lifespan and/or healthspan and delay aging.
Type:
Application
Filed:
July 19, 2021
Publication date:
January 4, 2024
Inventors:
Mimi Shirasu-Hiza, Julie Canman, Matt Ulgherait
Abstract: The present application relates to a pharmaceutical composition comprising sulbactam or a pharmaceutically acceptable salt thereof, avibactam or a pharmaceutically acceptable salt thereof, and optionally a pharmaceutically acceptable carrier, wherein unit dose ratio of said sulbactam or the pharmaceutically acceptable salt thereof and said avibactam or the pharmaceutically acceptable salt thereof is about 8:1 to about 4:1, unit dose of said sulbactam or the pharmaceutically acceptable salt thereof is about 1 g-4 g, and unit dose of said avibactam or the pharmaceutically acceptable salt thereof is about 0.125 g-1 g. The present application also relates to methods of treating bacterial infections using said pharmaceutical composition.
Abstract: The present invention concerns a pharmaceutical composition for topical administration, comprising sirolimus, solvent, thickener and glycol ether. The invention further concerns a pharmaceutical composition for use in the treatment of skin diseases or skin manifestations of diseases, especially of skin manifestations of tuberous sclerosis complex (TSC). The invention further concerns a method for producing a pharmaceutical composition comprising the steps of (i) providing sirolimus and (ii) forming the present composition.
Abstract: The present disclosure provides methods of increasing mitochondrial biogenesis, function, or both in a tissue of a subject by administering to the subject an amount of a 15-PGDH inhibitor effective to inhibit 15-PGDH activity and/or reduce 15-PGDH levels in the subject. The methods described herein are useful for treating diseases, disorders, or conditions associated with dysfunctional mitochondria and/or increased oxidative stress including mitochondrial diseases.
Type:
Application
Filed:
October 22, 2021
Publication date:
January 4, 2024
Applicant:
The Board of Trustees of the Leland Stanford Junior University
Inventors:
Helen M. BLAU, Adelaida Rosa PALLA, Meenakshi RAVICHANDRAN
Abstract: The invention provides antibiotic combination therapies for treating an A. baumannii infection in a subject. The combination therapies include rifabutin and a second antibiotic, such as colistin and cefiderocol.
Type:
Application
Filed:
September 12, 2023
Publication date:
January 4, 2024
Inventors:
Vincent Trebosc, Christian Kemmer, Glenn E. Dale, Sergio Lociuro, Marc Gitzinger
Abstract: An improved a method of treating a patient having a disorder responsive to PDE-4 inhibition by administering roflumilast. The improvement involves administering the roflumilast topically in a composition having a roflumilast release profile that produces in the patient a flattened plasma concentration time curve and a reduced Cmax relative to oral administration of a PDE4-inhibiting amount of roflumilast. Such disorders include inflammatory disorders such as inflammatory dermatoses, including psoriasis, atopic dermatitis and seborrheic dermatitis. Such disorders also include inflammatory diseases in a variety of organs, especially the lungs (asthma, COPD). Because of reduced side effects with topical administration due to the improved pharmacokinetics (PK) characteristics, it may be possible to provide higher systemic exposures (AUCs) with topical administration, resulting in greater therapeutic efficacy than with the oral route of administration.
Abstract: There are provided isotope-enriched compounds containing stable heavy isotope-enriched amide functional groups for modulating the pharmacokinetic profile, metabolic profile, and/or delivery efficiency of a drug or prodrug, as well as its therapeutic or prophylactic efficacy and/or adverse effects. Use of the isotope-enriched amide-containing drugs and prodrugs for the treatment or prevention of disease states and conditions is also provided.
Type:
Application
Filed:
March 25, 2021
Publication date:
January 4, 2024
Inventors:
Jiasheng LU, Jiamin GU, Xiang JI, Dongqing ZHU, Xiaolin HE, Xianqi KONG
Abstract: Opicapone for use as adjunctive therapy to preparations of levodopa and a DOPA decarboxylase inhibitor (DDCI) in the treatment of Parkinson's disease; characterised in that a patient with Parkinson's disease is treatable with preparations of levodopa and a DDCI without clinically diagnosed motor complications.
Type:
Application
Filed:
September 19, 2023
Publication date:
January 4, 2024
Inventors:
Patrício Manuel Vieira Araujo Soares Da Silva, José Francisco Da Costa De Pinho Rocha
Abstract: Provided is a pharmaceutical preparation for treatment or prevention of glaucoma or ocular hypertension, comprising 0.0003 to 0.01% (w/v) of isopropyl (6-{[4-(pyrazol-1-yl)benzyl] (pyridin-3-ylsulfonyl)aminomethyl}pyridin-2-ylamino)acetate, or a salt thereof.
Abstract: Provided is an anesthetic composition for locally administrating an amide-type anesthetic into a subject in need thereof. The anesthetic composition has multilamellar vesicles with entrapped amide-type anesthetic prepared by hydrating a highly entrapped lipid structure comprising an amide-type anesthetic and a lipid mixture with an aqueous buffer solution at a pH higher than 5.5. Also provided is a method to prepare an anesthetic composition using a simpler and more feasible process for large-scale manufacture and for providing a high molar ratio of amide-type anesthetic to phospholipid content as compared to the prior art. This anesthetic composition has a prolonged duration of efficacy adapted to drug delivery.
Type:
Application
Filed:
September 13, 2023
Publication date:
January 4, 2024
Inventors:
Keelung HONG, Hao-Wen KAO, Yi-Yu LIN, Luke S.S. GUO
Abstract: Provided herein are methods for treating liver disorders, including non-alcoholic steatohepatitis, and symptoms and manifestations thereof, in a patient which utilize, among others, a combination treatment of an FXR agonist and a THR? agonist.
Type:
Application
Filed:
January 20, 2023
Publication date:
January 4, 2024
Inventors:
Martijn FENAUX, Kevin KLUCHER, Christopher T. JONES, Thorsten A. KIRSCHBERG
Abstract: The present invention relates to a combination of selective blockers of TASK-1 and TASK-3 channels, in particular substituted imidazo [1,2-a]pyrimidine and substituted imidazo [1,2-a]pyridine derivatives of formula (II) and ?2-Adrenoceptor subtype C (alpha-2C) antagonists, in particular substituted heterocyclic carboxamides of formula (I) for the treatment and/or prophylaxis of sleep-related breathing disorders, preferably obstructive and central sleep apneas and snoring.
Abstract: A method for a treatment of individuals suffering from diseases associated with sulfatase deficiencies including lysosomal storage disease includes administering at least once a therapeutically effective amount of at least one retinoid. In particular, the compounds tazarotene and bexarotene have beneficial effects on these individuals. Pharmaceutical compositions comprising both active agents namely, tazarotene and bexarotene compounds, or similar compounds, provides for ready treatment of such individuals, and enhanced treatment is achieved with at least two active agents.
Type:
Application
Filed:
May 26, 2023
Publication date:
January 4, 2024
Inventors:
Lars SCHLOTAWA, Matthias KETTWIG, Karthikeyan RADHAKRISHNAN, Thomas DIERKS, Jutta GARTNER, Matthias BAUD
Abstract: The present invention relates to solid dispersions of amorphous compound of formula (I), and a polymer matrix, their processes of preparation and their uses in therapy.
Abstract: This disclosure relates to dosage forms comprising bupropion hydrochloride, another salt form of bupropion, or the free base form of bupropion; dextromethorphan hydrobromide, another salt form of dextromethorphan, or the free base form of dextromethorphan, and a polymer. In some embodiments, the dosage form has no significant dose dumping of bupropion in the presence of ethanol in vitro. In some embodiments, the dosage form does not have a food effect for bupropion or dextromethorphan when taken with a high-fat meal in human subjects. Some embodiments include a method of treating a nervous system condition (such as depression, e.g.
Abstract: This disclosure relates to dosage forms comprising bupropion hydrochloride, another salt form of bupropion, or the free base form of bupropion; dextromethorphan hydrobromide, another salt form of dextromethorphan, or the free base form of dextromethorphan, and a polymer. In some embodiments, the dosage form has no significant dose dumping of bupropion in the presence of ethanol in vitro. In some embodiments, the dosage form does not have a food effect for bupropion or dextromethorphan when taken with a high-fat meal in human subjects. Some embodiments include a method of treating a nervous system condition (such as depression, e.g.
Abstract: Certain embodiments described herein include methods and formulations for treating or preventing symptoms and conditions associated with sepsis. The methods and formulations include, but are not limited to, methods and formulations for delivering effective concentrations of levocetirizine and montelukast to a patient in need. The methods and formulations can comprise conventional and/or modified-release elements, providing for drug delivery to the patient.
Abstract: Methods of using small molecule inhibitors of fatty acid oxidation (FAO) as antimicrobials against intracellular Mycobacteria are disclosed. FAO inhibitors including etomoxir, trimetazidine, oxfenicine perhexeline and/or can be used alone, or in combination with known as antimycobacterial agents against intracellular Mycobacteria.
Type:
Application
Filed:
June 21, 2023
Publication date:
January 4, 2024
Inventors:
Jennifer A. Philips, Kathryn Moore, Pallavi Chandra, Mireille Ouimet
Abstract: The invention provides methods of treatment of heart failure with preserved ejection fraction (HFpEF) using modified forms of trimetazidine, such as CV-8972 and CV-8814.
Abstract: The present invention is directed to a combination therapy involving a type II anti-CD20 antibody and a selective Bcl-2 inhibitor for the treatment of a patient suffering from cancer, particularly, a CD20-expressing cancer.
Type:
Application
Filed:
September 7, 2023
Publication date:
January 4, 2024
Applicants:
GENENTECH, INC., HOFFMANN-LA ROCHE INC., ABBVIE INC.
Inventors:
Deepak Sampath, Christian Klein, Wayne John Fairbrother, Sari L. Heitner Enschede, Rod A. Humerickhouse, Andrew W. Roberts, John F. Seymour
Abstract: The invention relates to the use of an ERK inhibitor in the treatment of myelofibrosis (MF). The invention also relates to a pharmaceutical combination comprising a) an ERK inhibitor and b) at least one further therapeutic agent, preferably ruxolitinib or a pharmaceutically acceptable salt thereof.
Type:
Application
Filed:
October 7, 2021
Publication date:
January 4, 2024
Inventors:
Sime BRKIC, Hans MENSSEN, Sara MEYER, Thomas RADIMERSKI, Simona STIVALA
Abstract: The invention relates to pharmaceutical compositions comprising N-(3,5-dimethoxyphenyl)-N?-(1-methylethyl)-N-[3-(1-methyl-1H-pyrazol-4-yl)quinoxalin-6-yl]ethane-1,2-diamine, or a pharmaceutically acceptable salt thereof or a solvate thereof; to processes for the preparation of said compositions and to the use of said compositions for the manufacture of a medicament for the prophylaxis of or the treatment, in particular the treatment, of diseases, e.g.
Abstract: The present invention relates to pharmaceutical compositions for inhalation comprising a therapeutically effective dose of clofazimine wherein the clofazimine is provided in the form of a suspension, and processes for their preparation. Furthermore, the present invention provides pharmaceutical combinations comprising clofazimine in the form of an aerosol for pulmonary inhalation. The combinations and compositions provided by the present invention may be used in the treatment and/or prophylaxis of pulmonary infections caused by mycobacteria and other gram-positive bacteria, and of pulmonary fungal infections.
Type:
Application
Filed:
September 19, 2023
Publication date:
January 4, 2024
Inventors:
Thomas Hofmann, Stefan Ufer, Kevin Stapleton
Abstract: A chewable composition comprising an active pharmaceutical ingredient (API) composition, a surfactant composition, a binding composition, and a gelling composition in a sufficient amount to provide a cohesive gelled product. The API composition comprises a PED5 inhibitor; the surfactant composition and the API composition have a weight ration from about 0.1 to about 15; and the binding composition comprises a mono- or di-saccharide, a sugar alcohol, an oligosaccharide, or a combination thereof. In one embodiment, the API composition comprises tadalafil, sildenafil, vardenafil, avanafil, or a combination thereof.
Abstract: The disclosure provides new, stable, pharmaceutically acceptable amorphous solid dispersions of 1-(4-fluoro-phenyl)-4-((6bR,10aS)-3-methyl-2,3,6b,9,10,10a-hexahydro-1H,7H-pyrido[3?,4?:4,5]pyrrolo[1,2,3-de]quinoxalin-8-yl)-butan-1-one, together with methods of making and using them, and pharmaceutical compositions comprising them.
Abstract: Therapeutic methods and pharmaceutical compositions for treating an ophthalmic condition including dry eye syndrome and uveitis in a human subject are described. In certain embodiments, the disclosure includes therapeutic methods using a BTK inhibitor.
Abstract: This invention relates to combination therapies comprising a cyclin dependent kinase 4 (CDK4) inhibitor of Formula (I) or a pharmaceutically acceptable salt thereof, and an antiandrogen, optionally in further combination with an additional anti-cancer agent, and associated methods of treatment, pharmaceutical compositions, and uses thereof.
Type:
Application
Filed:
August 10, 2021
Publication date:
January 4, 2024
Applicants:
Pfizer Inc., Astellas Pharma Inc.
Inventors:
Lars ANDERS, Kimberly Hyunjung KIM, Danan LI, Elizabeth Anne MCMILLAN, Robert Andrew ROLLINS, Brendan Ayers VEENEMAN
Abstract: Disclosed herein are RNA methyltransferase inhibitors and methods of using the same. The inhibitors may be used in a method for the treatment of a subject in need of a treatment for a cancer by administering an effective amount of an RNA methyl-transferase inhibitor to the subject.
Abstract: The invention provides compositions and methods for reducing the volume of menstrual blood loss in a patient, such as a human patient, for instance, that has uterine fibroids, by administration of a gonadotropin-releasing hormone (GnRH) antagonist. Suitable GnRH antagonists useful in conjunction with the compositions and methods described herein include thieno[3,4d]pyrimidine derivatives, such as 3-[2-fluoro-5-(2,3-difluoro-6-methoxybenzyloxy)-4-methoxyphenyl]-2,4-dioxo-1,2,3,4-tetrahydrothieno[3,4d]pyrimidine-5-carboxylic acid and the choline salt thereof.
Type:
Application
Filed:
September 11, 2023
Publication date:
January 4, 2024
Inventors:
Ernest LOUMAYE, Jean-Pierre GOTTELAND, Oliver POHL
Abstract: The present invention discloses a pharmaceutical composition comprising 1-{3-[9-methoxy-7-(2-methoxyphenyl)-2,3,4,5-tetrahydro-1,4-benzoxazepine-4-carbonyl]phenyl}imidazolidin-2-one; N-tert-butyl-2-{N-[(furan-2-yl)methyl]-2-[5-(4-methylphenyl)-2H-1,2,3,4-tetrazol-2-yl]acetamido}-2-(4-hydroxyphenyl)acetamide; 3-[2-(2-{[(6-hydroxy-2,4-dioxo-1,2,3,4-tetrahydropyrimidin-5-yl)(4hydroxyphenyl) methyl]amino}-4-oxo-4,5-dihydro-1,3-thiazol-5-yl) acetamido]benzoic acid; 2-oxo-2-(1H-pyrrol-2-yl)ethyl 2-[(4-fluorophenyl)methoxy]benzoate; and 5-(3-{[(3-bromo-4-hydroxy-5 methoxyphenyl) methylidene]amino}-2 (butylimino)-2,3-dihydro-1,3-thiazol-4-yl)-2-hydroxybenzamide. The components are small molecule antagonists that increase the intracellular nitric oxide level by inhibiting the interaction between Nitric oxide synthase interacting proteins and inducible Nitric oxide synthase.
Abstract: In aspects, the present disclosure provides a method of treating or preventing a uterine leiomyosarcoma in a female mammal, the method comprising, consisting essentially of, or consisting of administering to the female mammal an effective amount of an inhibitor of bromodomain-containing protein 9 (BRD9).
Abstract: Use of pentoxifylline (PTX) in preparation of a medicament for repairing endothelial glycocalyx damage, and belongs to the technical field of medicine. A chlorine-induced endothelial glycocalyx damage model is established. After the endothelial glycocalyx damage model is successfully established, the PTX is intraperitoneally injected into a rat with endothelial glycocalyx damage. The result shows that the PTX effectively repairs shedding of glycosaminoglycans and syndecans in the endothelial glycocalyx damage and significantly downregulates the expression of inflammatory factors including tumor necrosis factor alpha (TNF-?), interleukin-6 (IL-6), and matrix metallopeptidase 13 (MMP-13). Therefore, the PTX can effectively repair the endothelial glycocalyx damage, providing a new theoretical basis for repairing the endothelial glycocalyx damage. Furthermore, with high safety, the PTX has the prospect of being developed into the medicament for repairing the endothelial glycocalyx damage.
Abstract: The present invention provides a pharmaceutical combination comprising a CRAF inhibitor in combination with (i) an ERK inhibitor or (ii) a MEK inhibitor or (iii) a CDK4/6 inhibitor, each as defined herein, or independently in each case a pharmaceutically acceptable salt thereof, for use in the treatment of NRAS-mutant melanoma and in the treatment of BRAF-mutant melanoma. wherein the melanoma may be unresectable and/or metastatic melanoma.
Type:
Application
Filed:
May 11, 2021
Publication date:
January 4, 2024
Inventors:
Giordano Caponigro, Vesselina Cooke, Uz Martin Stammberger, Darrin Stuart
Abstract: This invention relates to methods comprising administering a FAK inhibitor and an immunotherapeutic agent such as anti-PD-1 or anti-PD-L1; that are useful in the treatment of abnormal cell growth, such as cancer, in mammals, especially humans.
Type:
Application
Filed:
December 21, 2022
Publication date:
January 4, 2024
Inventors:
Jonathan A. Pachter, Jennifer E. Ring, David T. Weaver, Yan Wang
Abstract: The present invention relates to compositions and methods for treating patients with cancer having a RET gene abnormality comprising administering HM06/TAS0953, for example patients with non-small cell lung cancer (NSCLC), and that may also have brain and/or leptomeningeal metastases, or another solid tumor; where the patient is administered an effective amount of HM06/TAS0953, where the HM06/TAS0953 can be formulated in a composition and administered orally in a single or multiple doses; and where the patients may have previously received and/or have developed resistance to another RET-selective or multi-kinase inhibitor.
Type:
Application
Filed:
November 18, 2021
Publication date:
January 4, 2024
Applicants:
Helsinn Healthcare SA, Taiho Pharmaceutical Co., Ltd.
Abstract: Provided herein are compounds, compositions, and methods useful for modulating the integrated stress response (ISR) and for treating related diseases, disorders and conditions.
Type:
Application
Filed:
September 7, 2023
Publication date:
January 4, 2024
Inventors:
Kathleen Ann Martin, Carmela Sidrauski, Jennifer M. Frost, Yunsong Tong, Xiangdong Xu, SeungWon Chung, Qingwei Zhang, Lei Shi, Kathleen J. Murauski, Michael J. Dart, John T. Randolph
Abstract: The present invention relates to a storage-stable pharmaceutical composition for ophthalmic administration in the form of an aqueous solution comprising a therapeutically effective amount of antibiotic levofloxacin or a pharmaceutically acceptable salt or derivative thereof, as a first active ingredient, and a therapeutically effective amount of non-steroidal anti-inflammatory and analgesic ketorolac or a pharmaceutically acceptable salt or derivative thereof, as a second active ingredient, wherein said first active ingredient is from about 0.4 to about 0.9% w/v and said second active ingredient is from about 0.4 to about 0.9% w/v, wherein the weight/volume percentages are expressed as g/100 mL units, in order to prevent the precipitation and improve the stability of the product.
Abstract: Lactam or lactone derivatives of formula Ia: or a pharmaceutically acceptable salt or solvate thereof, wherein X1 is NH or O; X2 is —OH, —O-alkyl, —NH2, an amino acid group or a peptide group, wherein the amino acid group or peptide group is linked to the carbonyl group by its N-terminal residue; Z1 is S, SO, SO2, O, CR3 or NR4; and R1, R2, R3 and R4 each independently are H, alkyl or aryl. Also, the use of lactam or lactone derivatives of formula Ia in treating a disease caused by a viral infection, especially a coronavirus infection and/or a viral respiratory infection, such as COVID-19 caused by SARS-CoV-2.
Abstract: Provided herein are compositions relating to psychedelics and serotonin receptor modulators. Further provided herein are methods of suppressing or halting hallucinogenic effects of a psychedelic and methods of treating a disease or disorder (e.g., depression or diseases or disorders related to depression) comprising administering psychedelics and serotonin receptor modulators.
Abstract: The present invention relates to pharmaceutical compositions comprising flumazenil and naltrexone, especially compositions comprising low-dose flumazenil and low-dose naltrexone. The present invention also relates to methods for the use of a combination of flumazenil and naltrexone in the treatment of depression and/or anxiety and/or post-traumatic stress disorder (PTSD).
Type:
Application
Filed:
November 26, 2021
Publication date:
January 4, 2024
Inventors:
Lee Eric Rodne, Daniel John Zanardo, Julian Chick
Abstract: Disclosed herein are biodegradable poly(lactide-co-glycolide) (PLG) polymer compositions that are administered into the body with syringes or needles and that are utilized to deliver a testosterone into the body over an extended period of time.
Type:
Application
Filed:
September 24, 2021
Publication date:
January 4, 2024
Inventors:
Amy VAN HOVE, Dileep JANAGAM, Gregory FIELDSON
Abstract: A formulation for drug delivery, providing enhanced modulation of solubility, stability, absorption, metabolism, and/or pharmacokinetic profile of a lipophilic therapeutic agent by formulation with sterols and/or sterol esters, resulting in higher bioavailability of a therapeutic agent administered to a subject in need of such therapeutic agent. The formulation contains a therapeutic agent and a sterol or sterol ester, and can, optionally, further contain a solubilizer and/or an enhancing agent. Also described are pharmaceutical compositions containing the formulations and methods of making and methods of using the formulations and pharmaceutical compositions. Formulations of the disclosure can be constituted to minimize the synthesis of dihydrotestosterone when the therapeutic agent includes testosterone or testosterone esters.
Abstract: Provided herein are compositions (e.g., pharmaceutical compositions) comprising deuterated testosterone, deuterated methyltestosterone, deuterated androstenedione, or derivatives thereof. The provided compositions and related methods may be useful for treating and/or preventing various diseases and conditions, such as hypogonadism, delay of growth and puberty, weight loss associated with HIV-associated wasting, vulvar dystrophies, micropenis, breast cancer, and sexual disorders.
Abstract: Polyethylene glycol (PEG)-conjugated glucocorticoid prodrugs, methods of preparation, and use for the treatment of diseases and disorders are disclosed. In particular, PEG-conjugated dexamethasone compounds and methods of using them for treating inflammatory and autoimmune diseases, including but not limited to lupus, are disclosed.
Type:
Application
Filed:
February 21, 2023
Publication date:
January 4, 2024
Inventors:
Dong Wang, Fang Yuan, Zhenshan Jia, Xiaobei Wang