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:
May 5, 2020
Publication date:
November 12, 2020
Inventors:
Bart Rudolf Romanie KESTELEYN, Jan Martin BERKE, Erwin COESEMANS, Sandrine Céline GROSSE, Edgar JACOBY, Tim Hugo Maria JONCKERS, Stefaan Julien LAST, Wim Gaston VERSCHUEREN, Michel OBRINGER, Christelle Catherine Cecile DOEBELIN
Abstract: Described herein are methods of treating non-metastatic castrate-resistant prostate cancer using an approved drug product comprising apalutamide, enzalutamide or darolutamide. Also described here are drug products containing apalutamide enzalutamide or darolutamide, and methods of selling or offering for sale an anti-androgen drug product.
Abstract: Described herein are methods of administering the non-steroidal anti-inflammatory drug norketotifen, an isomer, an isomeric mixture, a prodrug, or a pharmaceutically acceptable salt thereof for the treatment of a respiratory disorders such as COPD and asthma to human patient in need of such treatment, without exposing said patient to adverse immune-suppressive effects. Methods include treating acute and potentially life-threatening exacerbations of COPD and asthma with norketotifen.
Type:
Application
Filed:
July 30, 2020
Publication date:
November 12, 2020
Inventors:
A.K. Gunnar Aberg, Vincent B. Ciofalo, Kresimir Pucaj
Abstract: The inventive subject matter is directed to compositions and methods for sterile and storage stable low-dose atropine formulations with improved stability. Most preferably, the compositions presented herein are substantially preservative free and exhibit less than 0.35% tropic acid from degradation of atropine. Advantageously, contemplated formulations are also substantially free of preservatives.
Type:
Application
Filed:
July 20, 2020
Publication date:
November 12, 2020
Inventors:
Navneet Puri, Prem Sagar Akasapu, Irfan A. Mohammed, Kumaresh Soppimath, Iouri V. Ilitchev
Abstract: An oral product includes a body that is wholly receivable in an oral cavity. The body includes a mouth-stable polymer matrix, cellulosic fibers embedded in the mouth-stable polymer matrix, and a mouth-soluble binder dispersed in the mouth-stable polymer matrix.
Type:
Application
Filed:
July 29, 2020
Publication date:
November 12, 2020
Applicant:
Altria Client Services LLC
Inventors:
Feng GAO, Frank Scott ATCHLEY, Gregory James GRISCIK, Christopher Joseph DINOVI, Phillip M. HULAN, Diane L. GEE, Jason FLORA, Shuzhong ZHUANG
Abstract: The present invention relates to solid state forms of N-[2,4-bis(1,1-diethylethyl)-5-hydroxyphenyl]-1,4-dihydro-1-oxoquinoline-3-carboxamide (Compound 1), pharmaceutical compositions thereof and methods therewith.
Type:
Application
Filed:
December 5, 2019
Publication date:
November 12, 2020
Applicant:
Vertex Pharmaceuticals Incorporated
Inventors:
Patricia Hurter, William Rowe, Christopher R. Young, Adriana Costache, Patrick R. Connelly, Mariusz Krawiec, Yuchuan Gong, Yushi Feng, Martin Trudeau
Abstract: The present invention relates to novel compounds which act as modulators of indoleamine 2,3-dioxygenase (IDO1) and to the use of said compounds in the prophylaxis and/or treatment of diseases or conditions mediated by indoleamine 2,3-dioxygenase. The invention further relates to pharmaceutical compositions comprising the novel compounds.
Type:
Application
Filed:
December 12, 2018
Publication date:
November 12, 2020
Applicant:
PHENEX DISCOVERY VERWALTUNGS-GMBH
Inventors:
Christoph Steeneck, Olaf Kinzel, Simon Anderhub, Martin Hornberger, Marta Czekanska, Thomas Hoffmann
Abstract: The present invention provides a quinoline derivative for the treatment of nasopharyngeal carcinoma and use thereof in preparation of a pharmaceutical composition for tumor treatment.
Type:
Application
Filed:
July 23, 2020
Publication date:
November 12, 2020
Inventors:
Shanchun WANG, Jun SHEN, Xi HAN, Xunqiang WANG, Shaonan TANG, Shuqing CAO, Xiquan Zhang, Hao YU, Maoqiong PAN, Ping XU, Chengqian WANG
Abstract: This disclosure provides pharmaceutical compositions comprising dextromethorphan in combination with quinidine, and methods for treating agitation and/or aggression in subjects with dementia by administering such compositions.
Abstract: The present invention relates to pharmaceutical compositions comprising an opioid antagonist, PG, and an isotonicity agent. The pharmaceutical compositions are stable at temperatures as low as ?5° C. or lower. Methods of using the pharmaceutical compositions are also disclosed.
Type:
Application
Filed:
September 28, 2018
Publication date:
November 12, 2020
Inventors:
Ryan LOUGHLIN, Fintan KEEGAN, Gerard Robert BELL
Abstract: The present invention is directed to a sustained release buprenorphine microsphere (SRBM) formulation capable of delivering buprenorphine, a metabolite, or a prodrug thereof for a duration of about 7 days to about 6 months.
Type:
Application
Filed:
April 23, 2020
Publication date:
November 12, 2020
Applicant:
BioDelivery Sciences International, Inc.
Abstract: The present invention relates to methods of treating or inhibiting keloids in a subject with hypoxia-inducible factor-1 (HIF-1) inhibiting compounds, methods of screening or identifying compounds to induce cell death in keloids, and methods of inducing cell death in keloids.
Abstract: The present disclosure provides pharmaceutical combinations comprising at least one spliceosome modulator and at least one inhibitor chosen from BCL2, BCL2/BCLxL, and BCLxL inhibitors. Also provided are methods of treating cancer comprising administering a therapeutically effective amount of at least one spliceosome modulator and a therapeutically effective amount of at least one inhibitor chosen from BCL2, BCL2/BCLxL, and BCLxL inhibitors.
Type:
Application
Filed:
October 30, 2018
Publication date:
November 12, 2020
Applicant:
Eisai R&D Management Co., Ltd.
Inventors:
Daniel AIRD, Laura CORSON, Ping ZHU, Markus WARMUTH, Silvia BUONAMICI, Peter Gerard SMITH, Peter FEKKES
Abstract: Pharmaceutical compositions for treating presbyopia are described, the compositions comprising choline esterase inhibitor(s) and several other components such as ?-1-adrenergic antagonist(s), non-steroid anti-inflammatory drug(s), and/or adrenergic antagonist(s). Methods for fabricating the compositions and using the compositions are also described.
Abstract: Pharmaceutical compositions containing dihydroergotamine (DHE) and methods in which DHE is administered to patients for treatment of migraine without side effects or adverse effects are disclosed. Methods for rapid treatment of migraine with DHE are disclosed comprising: dampening the peak plasma concentration (Cmax) and slightly delaying the peak such as to avoid activating the dopaminergic and adrenergic receptors, while achieving sufficient active binding to the serotonin receptors to provide relief from migraine symptoms within a timeframe that permits rapid resolution of migraine symptoms. Inhaler devices suitable for the methods are disclosed. Kits for practicing the methods of invention are disclosed.
Type:
Application
Filed:
December 5, 2019
Publication date:
November 12, 2020
Inventors:
Robert O. Cook, Stephen B. Shrewsbury, Nabih N. Ramadan, Thomas A. Armer
Abstract: Provided herein are methods and compositions for increasing muscle strength, and for treating muscle wasting disorders, muscle degenerative disease, or exercise-induced weakness, and cancer.
Abstract: A series of novel EHop-016 derivatives is presented herein via designing and synthesizing compounds that mimics its more favorable “U-shaped” conformation that appears to be critical for inhibitory activity against Rac. Based on modeling studies on EHop-016, compounds with a more rigid structural conformation can mimic this “U-shaped” conformation would improve the anti-migration activity against metastatic cells. Compounds are disclosed that inhibit RhoGTPases that are useful for inhibiting hyperprofilerative and neoplastic diseases, for instance compounds of formula (I) Specifically, the compounds inhibit the GTPases Rac and Cdc42 that are overactive or overexpressed in signaling pathways in cancer and metastasis. Methods for treatment of cancer and hyperproliferative diseases are disclosed.
Abstract: The invention relates to dosage forms for daily administration of compounds of formula (A) and formula (I): or a salt thereof, wherein R1, R2, R10, R11, R12, R13, R14, R15, R16, q and p are as described herein. Compounds of formula (A), formula (I), and pharmaceutical compositions thereof are ?v?6 integrin inhibitors that are useful for treating fibrosis such as idiopathic pulmonary fibrosis (IPF) and nonspecific interstitial pneumonia (NSIP).
Type:
Application
Filed:
April 8, 2020
Publication date:
November 12, 2020
Inventors:
Jacob CHA, Chengguo DONG, Timothy HOM, Lan JIANG, Katerina LEFTHERIS, Hui LI, David J. MORGANS, JR., Manuel MUNOZ, Maureen REILLY, Yajun ZHENG, Martin DECARIS, Scott TURNER
Abstract: A method for preventing, treating and/or improving a prostatic disease or disorder associated with epithelial hyperplasia and/or fibrosis, comprising: administering an effective amount of a multikinase inhibitor to a subject in need thereof, wherein the multikinase inhibitor has a certain spectrum of kinase inhibitory activity. The multikinase inhibitor is sunitinib, regorafenib, ponatinib, pazopanib, nintedanib and/or lenvatinib. The prostatic disease or disorder is selected from the group consisting of benign prostate hyperplasia and its associated lower urinary tract symptoms, fibrosis of ureters and renal pelvis, prostate adenoma, and prostatic intraepithelial neoplasia in animals and humans.
Abstract: The invention relates to a product containing the compound of formula (I) below (I) or a pharmaceutically acceptable salt of this compound, in combination with at least one compound having PDE5-inhibitory properties, or a pharmaceutically acceptable salt thereof, for therapeutic use, simultaneously, separately or over a period of time, in the treatment of a disease wherein vasoconstriction is involved.
Abstract: A compound of formula I or a pharmaceutically acceptable salt or ester thereof is provided for the treatment of cancer wherein (i) the cancer is one that has the characteristic of being a type prone to being or becoming refractory or resistant to platinum drug based therapy and (ii) the treatment is with a dose of between 1 mg/m2 and 30 mg/m2 of compound per patient body surface area per administration. Method of treatment and novel dosage forms are also provided. Particularly treated are ovarian cancers, particularly those expressing a-folate receptors, including epithelial ovarian, fallopian tube or peritoneal cancer.
Abstract: The present disclosure relates to compounds, which are useful for regulating the expression of apolipoprotein A-I (ApoA-I), and their use for treatment and prevention of cardiovascular disease and related disease states, including cholesterol- or lipid-related disorders, such as, for example, atherosclerosis.
Abstract: The present invention relates to the use of serotonergic compounds for the treatment of virus-induced thrombocytopenia. More particularly, the invention relates to methods of treating thrombocytopenia by blocking serotonin activity. For example, inhibitors of receptor 5HT2A and/or receptor 5HT1A and/or inhibitors of mast cell degranulation and/or inhibitors of serotonin uptake may be used. Preferably, the thrombocytopenia is induced by dengue or Japanese Encephalitis virus, and the inhibitors are preferably ketanserin, WAY-100135, sarpogrelate, or fluoxetine.
Type:
Application
Filed:
October 31, 2018
Publication date:
November 12, 2020
Inventors:
Ashley Lauren ST. JOHN, Mohamad Fadhli Bin MASRI, Abhay RATHORE
Abstract: Compounds, compositions, and methods of treatment and prevention of HTV infection are disclosed. The compounds are pyrrolo[2,3-b]pyridines and pyrrolo[2,3-b]pyrimidine JAK inhibitors. Combinations of these JAK inhibitors and additional antiretroviral compounds, such as NRTI, NNRTI, integrase inhibitors, entry inhibitors, protease inhibitors, and the like, are also disclosed. In one embodiment, the combinations include a combination of adenine, cytosine, thymidine, and guanine nucleoside antiviral agents, optionally in further combination with at least one additional antiviral agent that works via a different mechanism than a nucleoside analog. This combination has the potential to eliminate the presence of HIV in an infected patient.
Type:
Application
Filed:
March 12, 2020
Publication date:
November 12, 2020
Inventors:
Christina Gavegnano, Raymond F. Schinazi
Abstract: The invention relates to particular substituted deuterated heterocycle fused gamma-carbolines, their prodrugs, in free, solid, pharmaceutically acceptable salt and/or substantially pure form as described herein, pharmaceutical compositions thereof, and methods of use in the treatment of diseases involving 5-HT2A receptor, serotonin transporter (SERT) and/or pathways involving dopamine D1/D2 receptor signaling systems, and/or the treatment of residual symptoms.
Abstract: The present invention relates to a novel pharmaceutical composition for the treatment of dystonia or relieving pain caused by myotonic conditions in a subject suffering from dystonia. Particularly, the present invention provides a pharmaceutical composition for treating dystonia or relieving pain caused by dystonia comprising a serotonin receptor 5-HT2A inhibitor as an active ingredient.
Abstract: Methods of using compounds and salts thereof as JAK kinase inhibitors are described herein, including methods of treating or lessening the severity of a disease or condition responsive to the inhibition of a Janus kinase activity in a patient.
Type:
Application
Filed:
July 28, 2020
Publication date:
November 12, 2020
Applicant:
Genentech, Inc.
Inventors:
Mark ZAK, F. Anthony ROMERO, Yun-Xing CHENG
Abstract: A method of treating a bacterial infection of a subject includes topically administering a topical composition that includes ceftriaxone for injection powder combined with a carrier. The topical composition may be administered by contacting a tissue surface of the subject to be treated with the topical composition such as skin or mucosal tissue.
Abstract: A method of alleviating age-related symptoms in a mammal, which comprises a step of administering to a mammal in need thereof, an effective amount of a composition containing an effective amount of at least methylene blue.
Abstract: The present disclosure relates to a process for preparing a pharmaceutical formulation, said process comprises: i) blending chlorpromazine hydrochloride and microcrystalline cellulose under a first set of pre-determined conditions to obtain a first mixture; ii) blending lactose monohydrate with first mixture under a second set of pre-determined conditions to obtain a second mixture; iii) blending pre-gelatinized starch, colloidal silicon dioxide and magnesium stearate with second mixture under a third set of pre-determined conditions to obtain a third mixture; iv) screening the third mixture through #40 Mesh and dry blending under a fourth set of pre-determined conditions to obtain a fourth mixture; and v) directly compressing the fourth mixture to obtain the pharmaceutical formulation.
Abstract: Methods and compositions for potentiating the effect of an opioid analgesic in a patient undergoing or planning to undergo opioid analgesic therapy using a potentiating amount of iboga alkaloid or pharmaceutically acceptable salt and/or solvate thereof that does not prolong the patient's QT interval by more than about 50 milliseconds.
Abstract: The invention provides methods for inducing, enhancing or increasing satellite cell proliferation, and an assay for screening for a candidate compound for inducing, enhancing or increasing satellite cell proliferation. Also provided are methods for repairing or regenerating a damaged muscle tissue of a subject.
Type:
Application
Filed:
May 25, 2020
Publication date:
November 12, 2020
Inventors:
Lee L. Rubin, Amanda Gee, Amy J. Wagers
Abstract: The present invention relates to compositions and methods comprising a retinoic acid receptor inhibitor, a retinoic X receptor inhibitor or an inhibitor of an enzyme in the retinoic acid biosynthesis pathway for treatment of a patient having a solid tumor. In some embodiments, the solid tumor is a sarcoma.
Abstract: The invention provides an orodispersible solid pharmaceutical dosage unit having a weight between 30 and 1,000 mg, said dosage unit comprising: 0.1-25 wt. % of estetrol particles containing at least 80 wt. % of an estetrol component selected from estetrol, estetrol esters and combinations thereof; and 75-99.9 wt. % of one or more pharmaceutically acceptable excipients; the solid dosage unit comprising at least 100 ?g of the estetrol component; and wherein the solid dosage unit can be obtained by a process that comprises compressing a dry blend of estetrol particles and one or more pharmaceutically acceptable excipients into a solid dosage unit. The solid dosage unit is easy to manufacture and perfectly suited for sublingual, buccal or sublabial administration.
Type:
Application
Filed:
May 26, 2020
Publication date:
November 12, 2020
Applicant:
ESTETRA SPRL
Inventors:
Séverine Francine Isabelle JASPART, Johannes Jan PLATTEEUW, Denny Johan Marijn VAN DEN HEUVEL
Abstract: The invention relates to a new method for the prevention and treatment of wave burst arrhythmia by administering a gestagen having an androgenic effect.
Type:
Application
Filed:
April 18, 2017
Publication date:
November 12, 2020
Inventors:
Joe-Elie SALEM, Christian FUNCK-BRENTANO, Anne BACHELOT, Xavier WAINTRAUB
Abstract: According to various embodiments of this disclosure, pharmaceutical formulations comprising solubilized estradiol are provided. In various embodiments, such formulations are encapsulated in soft capsules which may be vaginally inserted for the treatment of vulvovaginal atrophy.
Type:
Application
Filed:
April 1, 2020
Publication date:
November 12, 2020
Applicant:
TherapeuticsMD, Inc.
Inventors:
Brian A. BERNICK, Julia M. AMADIO, Peter H.R. PERSICANER, Thorsteinn THORSTEINSSON, Janice Louise CACACE, Frederick D. SANCILIO, Neda IRANI
Abstract: The present invention relates to the use of an oxytocin receptor antagonist in females undergoing embryo transfer as part of an assisted reproductive technology. In particular, methods are provided for increasing ongoing implantation rate, increasing ongoing pregnancy rate, increasing clinical pregnancy rate, and/or increasing live birth rate in a female subject undergoing embryo transfer. Specifically, the antagonists are released in the luteal phase when the endometrium is receptive for embryo implantation and/or when the embryo has reached the blastocyst-stage.
Abstract: A unit dose pharmaceutical composition comprising 2.0 to 8.0 mg of a dry powder of one or more glucocorticoid or mineralocorticoid or a therapeutically active analogue, derivative, homolog, pharmaceutically acceptable salt or conjugate thereof; wherein the composition is comprised in a syringe is disclosed. The composition may also comprise a a sterile, liquid carrier suitable for direct injection into an eye and/or 0.6 to 0.75% (w/v) of carboxy methyl cellulose (CMC); and 0.015 to 0.04 (w/v) of a surfactant. Also disclosed is a medical device comprising the unit dose pharmaceutical composition, use of the pharmaceutical composition in the treatment of an eye disease or condition or predisposition thereto and a method of treatment of an eye disease or condition or a predisposition thereto in a subject in need thereof including injecting into the eye the pharmaceutical formulation. The injection may comprise an intravitreal and/or suprachoroidal injection.
Abstract: An ophthalmic aqueous composition comprises levofloxacin, a salt thereof, or a solvate thereof; dexamethasone, an ester thereof, or a salt thereof; and one or at least two isotonic agents. The ophthalmic aqueous composition is substantially free of sodium chloride. This ophthalmic aqueous composition is excellent in drug stability and drug migration and has a clear appearance.
Abstract: The disclosure relates to the field of pharmaceutical technology, in particular, to a compound pharmaceutical composition for treating skin inflammatory diseases, which is characterized in that an active ingredient of the compound pharmaceutical of the disclosure is composed of tofacitinib and crisaborole, and the composition has a stronger therapeutic effect and a lower dosage with a significant synergistic therapeutic effect. The pharmaceutical composition of the disclosure can be used to treat skin inflammatory diseases.
Type:
Application
Filed:
May 9, 2019
Publication date:
November 12, 2020
Inventors:
Guangwei He, Zhaoxing Chu, Qinlong Xu, Jiajia Mo, Yan Zhao, Lincui Bian, Yuanfeng Gu, Li Shao
Abstract: The invention relates to compositions of nicotinamide mononucleotide derivatives and their methods of use. The invention also relates to methods of preparing nicotinamide mononucleotide derivatives. The invention relates to pharmaceutical compositions and nutritional supplements containing a nicotinamide mononucleotide derivative. The invention relates to methods of using nicotinamide mononucleotide derivatives that promote the increase of intracellular levels of nicotinamide adenine dinucleotide (NAD+) in cells and tissues for treating diseases and improving cell and tissue survival.
Type:
Application
Filed:
December 13, 2019
Publication date:
November 12, 2020
Inventors:
Karl D. Normington, David A. Sinclair, David J. Livingston, James M. McKearin, Bruce Szczepankiewicz, Jonathan N. Kremsky
Abstract: Provided are methods for treating Arenaviridae and Coronaviridae virus infections by administering nucleosides and prodrugs thereof, of Formula I: wherein the 1? position of the nucleoside sugar is substituted. The compounds, compositions, and methods provided are particularly useful for the treatment of Lassa virus and Junin virus infections.
Type:
Application
Filed:
April 30, 2020
Publication date:
November 12, 2020
Inventors:
Michael O' Neil Hanrahan Clarke, Joy Yang Feng, Robert Jordan, Richard L. Mackman, Adrian S. Ray, Dustin Siegel
Abstract: Provided herein are methods of reducing the weight loss and/or increasing the weight of a feline in need thereof, said methods include administering to a feline in need thereof a total daily dosage of about 2 to 50 mg of Compound 1, having the formula: or a pharmaceutically acceptable form thereof. Also provided herein are methods of managing the disease of a feline with diabetes mellitus and elevated IGF-1 concentration.
Abstract: Nutraceutical composition for the activation of sirtuins in humans, the composition including from 10% by weight to 15% by weight of honokiol; from 12% by weight to 40% by weight of pterostilbene; from 22% by weight to 32% by weight of polydatin; from 25% by weight to 40% by weight of ellagic acid and from 1.5% by weight to 3% by weight of a mixture of zinc, seleniun, chromium and nicotinamide, the composition promoting the inhibition of cell degradation and aging phenomena.
Type:
Application
Filed:
January 8, 2019
Publication date:
November 12, 2020
Inventors:
Giovanni CIALLELLA, Lyudmyla ZAPOROZHETS
Abstract: Disclosed are methods of treating cystic fibrosis using AmB and a sterol or compositions comprising AmB and a sterol. Also disclosed are methods of increasing the pH of airway surface liquid in a patient having cystic fibrosis using AmB and a sterol; and methods of decreasing the viscosity of airway surface liquid in a patient having cystic fibrosis using AmB and a sterol.
Type:
Application
Filed:
October 11, 2018
Publication date:
November 12, 2020
Inventors:
Martin D. Burke, Katrina A. Muraglia, Rajeev S. Chorghade, Michael J. Welsh
Abstract: Provided herein are pharmaceutically acceptable compositions containing macrolide antibiotics, in particular azithromycin. In particular, compositions containing azithromycin with low toxicity, especially for administration to felines, are provided herein.
Type:
Application
Filed:
July 23, 2020
Publication date:
November 12, 2020
Inventors:
Neil E. Paulsen, Gail L. Dempsey, Michael S. Daniel, Tiffany G. Tomlinson, Douglas Hepler, Raymond Petzold
Abstract: Contemplated cancer therapies use aldoxorubicin as an immunomodulator of a tumor microenvironment to increase therapeutic effects of immune therapeutic compositions.
Type:
Application
Filed:
September 5, 2018
Publication date:
November 12, 2020
Inventors:
Patrick SOON-SHIONG, John H. LEE, Shahrooz RABIZADEH, Kayvan NIAZI
Abstract: It is an object of the present invention to provide an antitumor agent for biliary tract cancer that exhibits effects on biliary tract cancer, and a method for treating biliary tract cancer. According to the present invention, provided is an antitumor agent for biliary tract cancer, comprising 1-(2-deoxy-2-fluoro-4-thio-?-D-arabinofuranosyl)cytosine, a salt thereof, or a prodrug thereof.
Abstract: The present disclosure relates to solid dosage forms comprising anti-HCV compounds and methods of using such dosage forms to treat or prevent HCV infection. Direct-acting antiviral agents (DAAs) have a high cure rate, and favorable tolerability in persons infected with hepatitis C virus (HCV). However, shorter courses of therapy can improve adherence, affordability, and increase DAAs accessibility. The addition of an NS3 protease inhibitor to dual NS5A-NS5B (nucleoside) inhibitors enhances antiviral efficacy, and reduces treatment duration to 3 weeks (wks) in individuals with a rapid virologic response (RVR), defined as plasma HCV RNA<500, or <1,000, IU/mL by Day 2 of treatment.