Abstract: The present invention relates to a quinoline derivative of formula (I) or anyone of its pharmaceutically acceptable salt, or anyone of its metabolites, for use for treating or preventing a viral infection, in particular a HIV infection or a HIV-related condition in a patient; and then terminating said treatment when: the viral load is low or undetectable; and/or the level of CD4+ cell count is maintained or restored.
Abstract: The present invention provides alkaloids with formula I, II, III, IV, or V and their pharmaceutically acceptable salts, their preparation and their uses as antivirus drugs, for example, for treatment of HSV-1 infection. The alkaloids with formula I were isolated from the fermentation of marine fungus Scopulariopsis sp.(TA01-33) by means of column chromatography, such as positive phase silica gel column chromatography, etc. Alkaloids with formula II, III, IV and V were semisynthesized from compounds with formula I.
Abstract: Provided herein are quinolinone derivatives and their uses as antiviral drugs, for example, for treatment of HSV-1 infection. Also provided herein are pharmaceutically acceptable compositions comprising the quinolinone derivatives and the uses of the composition in the treatment of diseases caused by HSV-1 virus.
Abstract: Provided herein are compounds and methods for achieving a sustained therapeutic effect of small molecule anti-cancer agents when administered in vivo.
Type:
Application
Filed:
October 3, 2017
Publication date:
February 1, 2018
Inventors:
Michael A. Eldon, Shibani S. Harite, Tamra L. Barker
Abstract: The present invention relates to nalmefene for use in the reduction of alcohol consumption in a patient with alcohol dependence who has a high drinking risk level. The present invention also relates to nalmefene for use in the reduction of alcohol consumption in a patient with alcohol dependence who maintains a high DRL after an observation period following initial assessment.
Type:
Application
Filed:
March 22, 2017
Publication date:
February 1, 2018
Inventors:
Lars TORUP, Afsaneh ABBARIKI, Anna BLADSTROM, Christine PERSSON, Didier MEULIEN, Per SORENSEN, Thomas Jon JENSEN, Jette Buch OSTERGAARD
Abstract: This invention relates a therapeutic pharmaceutical composition comprising: a mixture including an opioid; polyethylene oxide in an amount of about 3 to about 40 wt % of the composition; a disintegrant; and a surfactant; wherein the disintegrant is present in an amount sufficient to cause the pharmaceutical composition to exhibit an immediate release profile.
Type:
Application
Filed:
October 5, 2017
Publication date:
February 1, 2018
Applicant:
Acura Pharmaceuticals, Inc.
Inventors:
Vijai KUMAR, David DIXON, Divya TEWARI, Dilip B. WADGAONKAR
Abstract: An abuse-deterrent pharmaceutical composition has been developed to reduce the likelihood of improper administration of drugs, especially drugs such as opiods. In the preferred embodiment, a drug is modified to increase its lipophilicity. In preferred embodiments the modified drug is homogeneously dispersed within microparticles composed of a material that is either slowly soluble or not soluble in water. In some embodiments the drug containing microparticles or drug particles are coated with one or more coating layers, where at least one coating is water insoluble and preferably organic solvent insoluble, but enzymatically degradable by enzymes present in the human gastrointestinal tract. The abuse-deterrent composition retards the release of drug, even if the physical integrity of the formulation is compromised (for example, by chopping with a blade or crushing) and the resulting material is placed in water, snorted, or swallowed.
Type:
Application
Filed:
October 5, 2017
Publication date:
February 1, 2018
Inventors:
Jane Hirsh, Alexander M. Klibanov, Timothy M. Swager, Stephen L. Buchwald, Whe Yong Lo, Alison B. Fleming, Roman V. Rariy
Abstract: An abuse-deterrent pharmaceutical composition has been developed to reduce the likelihood of improper administration of drugs, especially drugs such as opioids. In a preferred embodiment, a drug is modified to increase its lipophilicity. In some embodiments the modified drug is homogeneously dispersed within spherical microparticles composed of a material that is either slowly soluble or not soluble in water. In some embodiments the drug containing microparticles or drug particles are coated with one or more coating layers, where at least one coating is water insoluble and/or organic solvent insoluble. The abuse-deterrent composition retards the release of drug, even if the physical integrity of the formulation is compromised (for example, by chopping with a blade or crushing) and the resulting material is placed in water, snorted, or swallowed. However, when administered as directed, the drug is slowly released from the composition as the composition is passes through the GI tract.
Type:
Application
Filed:
October 6, 2017
Publication date:
February 1, 2018
Inventors:
Roman V. Rariy, Alison B. Fleming, Jane Hirsh, Alexander M. Klibanov
Abstract: Compositions and therapeutic uses of HEPES and derivatives in the treatment of pain associated with cancers and side-effects including post-chemotherapy cognitive impairment are disclosed herein. HEPES is also used to treat neurodegenerative and neurological diseases, demyelinization injuries, and side-effects and withdrawal symptoms associated with benzodiazepines, anti-depressants, and other neurological agents.
Abstract: Disclosed herein are compositions comprising Plinabulin and one or more immune checkpoint inhibitor for treating cancer. Some embodiments relate to methods of treating cancer by co-administering Plinabulin and one or more immune checkpoint inhibitor to a subject in need thereof.
Abstract: The present invention provides a compound of Formula (I) or a salt thereof; and therapeutic uses of these compounds. The present invention further provides pharmaceutical compositions comprising these compounds, and compositions comprising these compounds with a therapeutic co-agent.
Type:
Application
Filed:
August 9, 2017
Publication date:
February 1, 2018
Applicant:
Novartis AG
Inventors:
Jeffrey T. BAGDANOFF, Yu DING, Wooseok HAN, Zilin HUANG, Qun JIANG, Xianming JIN, Xiang KOU, Patrick LEE, Mika LINDVALL, Zhongcheng MIN, Yue PAN, Sabina PECCHI, Keith Bruce PFISTER, Daniel POON, Vivek RAUNIYAR, Xiaojing Michael WANG, Qiong ZHANG, Jianguang ZHOU, Shejin ZHU
Abstract: The present invention relates generally to a medicinal solution, and more particularly to a medicinal solution which is to be continuously or pulse-delivered for the purpose of treating various ocular diseases, conditions, or maladies, such as keratoconus, infectious keratitis, severe inflammatory conditions, and ocular surface neoplasia. In particular, the medicinal solution comprises the combination of a medication for treating one of the aforenoted or similar diseases, conditions, or maladies, and an anesthetic for rendering the patient comfortable during the treatment procedure.
Abstract: Provided herein are formulations, processes, solid forms and methods of use relating to 2-(tert-butylamino)-4-((1R,3R,4R)-3-hydroxy-4-methylcyclohexylamino)-pyrimidine-5-carboxamide.
Type:
Application
Filed:
October 9, 2017
Publication date:
February 1, 2018
Inventors:
Hon-Wah Man, Marie Georges Beauchamps, Mohit Atul Kothare, Nanfei Zou
Abstract: Various embodiments described herein are directed to compounds of formula (I), (II), (III) or (IV) for use as potent inhibitors of HIV integrase and for treatment of patients afflicted with AIDS. A major challenge of human immunodeficiency virus (HIV) chemotherapy continues to be the inevitable selection of resistance by the virus towards known drug regimens. Treating resistant HIV strains calls for novel antivirals with unique structural cores. Some embodiments are directed to compounds featuring a 3-hydroxypyrimidine-2,4-dione-5-carboxamide core that consistently confers low nanomolar potencies against HIV-1 in cell culture. Biochemical testing and molecular modeling results corroborate an antiviral mechanism of action of inhibiting integrase strand transfer (INST). Preliminary testing against raltegravir-resistant HIVs showed marginal cross resistance, suggesting that the chemotypes of the various embodiments described herein could fit an inhibitory profile of second generation INSTIs.
Abstract: A novel therapeutic drug for malignant tumors, cancer stem cells, or fibrosis is obtained. A therapeutic drug for malignant tumors or cancer stem cells is used that includes at least one compound selected from the group consisting of compounds represented by formulas (1), (2), and (5), a salt thereof, or a solvate thereof. Alternatively, a therapeutic drug for fibrosis can be used that includes at least one compound selected from the group consisting of compounds represented by formulas (1), (2), and (5), a salt thereof, or a solvate thereof.
Abstract: Described herein is the Bruton's tyrosine kinase (Btk) inhibitor 1-((R)-3-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one, including novel pharmaceutical formulations thereof. Also disclosed are pharmaceutical compositions that include the Btk inhibitor, as well as methods of using the Btk inhibitor, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.
Type:
Application
Filed:
March 17, 2017
Publication date:
February 1, 2018
Inventors:
Harisha Atluri, Ching Wah Chong, Robert Kuehl, Cassandra Shu, Pearl Shwe-Cho Tay, James Francis Hulvat, Alexander Jacob McVey, Ryan Mitchell Minikis
Abstract: The present invention relates to a novel pharmaceutical composition free of gastric coating comprising anagrelide hydrochloride in combination with a non-pH dependent polymer and a pharmaceutically acceptable water soluble acid and its use for the treatment of essential thrombocythemia.
Abstract: Provided are crystalline forms of 2-Methyl-1-[(4-[6-(trifluoromethyl) pyridin-2-yl]-6-{[2-(trifluoromethyl)pyridin-4-yl]amino}-1,3,5-triazin-2-yl)amino]propan-2-ol mesylate useful for treating cancer and methods of treating cancer, comprising administering to a subject in need thereof said compound.
Abstract: The present invention relates to compositions containing a PIKfyve inhibitor, preferably apilimod, APY0201 or YM-201636, most preferably apilimod, for use in treating or preventing viral infections, preferably Ebola or Marburg virus infections. It also relates to a pharmaceutical pack or kit comprising apillimod and at least one additional anti-viral agent.
Type:
Application
Filed:
January 21, 2016
Publication date:
February 1, 2018
Inventors:
Henri LICHENSTEIN, Jonathan M. ROTHBERG, Neil BEEHARRY, Paul BECKETT, Sean LANDRETTE, Chris CONRAD
Abstract: The present disclosure relates to methods for treating bronchiectasis, for example, non-cystic fibrosis bronchiectasis with compositions comprising an effective amount of certain (2S)—N-[(1S)-1-cyano-2-phenylethyl]-1,4-oxazepane-2-carboxamide compounds of Formula (I), including pharmaceutically acceptable salts thereof, that inhibit dipeptidyl peptidase 1 (DPP1) activity. Methods provided herein are useful for prophylaxis, increasing the lung function in a patient, and/or and/or decreasing the rate of pulmonary exacerbation in a patient. In one embodiment, the compound of Formula (I) is (2S)—N-{(1S)-1-cyano-2-[4-(3-methyl-2-oxo-2,3-dihydro-1,3-benzoxazol-5-yl)phenyl]ethyl}-1,4-oxazepane-2-carboxamide.
Type:
Application
Filed:
July 28, 2017
Publication date:
February 1, 2018
Applicants:
AstraZeneca AB, Insmed Incorporated
Inventors:
Hans Roland LONN, Stephen CONNOLLY, Steven SWALLOW, Reinilde HEYRMAN, Eugene SULLIVAN, Carlos FERNANDEZ
Abstract: A drug delivery system for oral administration of hydrophobic drugs with enhanced and extended absorption and improved pharmacokinetics is provided. In one embodiment, formulations comprising testosterone and testosterone esters, e.g., testosterone palmitate, are disclosed. Methods of treating a hormone deficiency or effecting male contraception with the inventive formulations are also provided.
Type:
Application
Filed:
October 3, 2017
Publication date:
February 1, 2018
Inventors:
Robert E. DUDLEY, Panayiotis P. CONSTANTINIDES
Abstract: A composition has ornithine, aspartic acid and vitamin B6, and it is used in preparation of hypolipidemic drugs, health-care products, foods or food additives.
Abstract: Oral dosage forms of osteoclast inhibitors, such as neridronic acid, in an acid or a salt form can be used to treat or alleviate pain or related conditions, such as complex regional pain syndrome.
Abstract: Compositions involving a modified egg yolk extract for use as an effective anti-cancer agent are described. The modified egg yolk extract involves specific fractions of phosphatidylcholines and sphingomyelins modified and produced from a chemical synthesis applied to the extract that produce a beneficial effect on the inhibition of cancerous cell growth. Methods of administering these compositions are also described.
Type:
Application
Filed:
October 6, 2017
Publication date:
February 1, 2018
Inventors:
Jakub STASZAK-JIRKOVSKY, Lukas KOBR, Gregory F. MIKNIS, Colleen HUDSON, Luca MONFREGOLA,, Pavel JIRKOVSKY, Zboncáková MILADA, Jason DUEX, Pitchaimani KANDASAMY
Abstract: The present invention provides the use of a compound of formula I, and compositions comprising such a compound, for improving power output and/or oxygen efficiency in a subject.
Type:
Application
Filed:
February 11, 2016
Publication date:
February 1, 2018
Inventors:
Antonie Johannes VAN DER SAAG, Sam POSSEMIERS
Abstract: A compound from the avermectin family is described for use in treating and/or preventing folliculitis caused by anti-cancer agents and more particularly by agents for targeted therapy.
Abstract: The stable pharmaceutical compositions comprising a compound of Formula (I) or a stereoisomer or a pharmaceutically acceptable derivative thereof are disclosed.
Type:
Application
Filed:
January 12, 2017
Publication date:
February 1, 2018
Applicant:
WOCKHARDT LIMITED
Inventors:
Mohammad Ajmal SHAREEF, Mrutunjaya SAHU, Ajaykumar HANDA
Abstract: The lyophilized solid pharmaceutical compositions comprising a compound of Formula (I) or a stereoisomer or a pharmaceutically acceptable derivative thereof are disclosed.
Abstract: Disclosed is a use of albiflorin or a pharmaceutically acceptable salt for the prevention and/or treatment of irritable bowel syndrome. The experimental results demonstrate that the prevention, remission and/or treatment of irritable bowel syndrome with albiflorin or a pharmaceutically acceptable salt has significant effects and few side effects. This is a preparation derived from a natural plant for the safe, effective and multi-targeted prevention, remission and/or treatment of irritable bowel syndrome.
Abstract: A method of and composition for treating a patient having Mycobacterium avium complex (MAC), and in one embodiment Mycobacterium avium subspecies paratuberculosis (MAP), causing one or more diseases, an embodiment of the method including administering to the patient an effective amount of one or more antibiotics and administering to the patient an effective amount of ultraviolet blood irradtiation (UVBI) treatments, and an embodiment of the composition including an effective amount of one or more antibiotics and an effective amount of UVBI treated blood of the patient.
Abstract: The present disclosure relates to a combination of an inhibitor of human histone methyltransferase DOT1L, such as EPZ-5676 or salts thereof, and one or more DNMT inhibitors, and methods of combination therapy for administering to subjects in need thereof for the treatment of cancer.
Type:
Application
Filed:
February 1, 2016
Publication date:
February 1, 2018
Inventors:
Christine Klaus, Maria Alejandra Raimondi, Scott Richard Daigle, Roy MacFarlane Pollock, Vivek Chopra
Abstract: Methods and compositions for treating cancer by intratumorally administering a stimulator of interferon genes (STING) agonist are disclosed herein.
Type:
Application
Filed:
October 13, 2017
Publication date:
February 1, 2018
Inventors:
Thomas F. Gajewski, Seng-ryong Woo, Leticia Corrales, Thomas W. Dubensky, Jr., David Kanne, Meredith Lai Ling Leong, Laura Hix Glickman, Edward Emile Lemmens
Abstract: The current invention provides oligomers with improved characteristics that enhance clinical applicability for treating, ameliorating, preventing a disorder or disease.
Type:
Application
Filed:
July 5, 2017
Publication date:
February 1, 2018
Inventors:
Judith Christina Theodora Van DEUTEKOM, Peter Christian de VISSER
Abstract: Compositions comprising first and second oligomers are provided wherein at least a portion of the first oligomer is capable of hybridizing with at least a portion of the second oligomer, at least a portion of the first oligomer is complementary to and capable of hybridizing to a selected target nucleic acid, and at least one of the first or second oligomers includes a modified sugar and/or backbone modification. In some embodiments the modification is a 2?-OCH3 substituent group on a sugar moiety. Oligomer/protein compositions are also provided comprising an oligomer complementary to and capable of hybridizing to a selected target nucleic acid and at least one protein comprising at least a portion of an RNA-induced silencing complex (RISC), wherein at least one nucleotide of the oligomer has a modified sugar and/or backbone modification.
Abstract: The present invention relates to methods for treating optic disorders or for reducing or alleviating the signs, symptoms, or pathological conditions related to such optic disorders. In particular, methods are provided for treating optic disorders, or reducing the symptoms thereof, the methods involving the administration of one or more downstream folate compounds and/or methyl-B12. In one particular embodiment, the method comprises administration of L-methylfolate. In other embodiments, the method involves administering both L-methylfolate and methyl-B12. In still further embodiments, the method further involves reducing dietary intake of folic acid. 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 mutations.
Abstract: Provided herein are hybrid oligonucleotides comprising a region that promotes cleavage of a nucleic acid and a region that protects a nucleic acid from exonuclease activity. Such hybrid oligonucleotides are useful for modulating the expression of genes. Related compositions and methods are also provided. In some embodiments, methods are provided for treating a disease, such as by administering a hybrid oligonucleotide.
Abstract: Described herein are materials and methods useful for the treatment of neurodegenerative disorders as well as bone disorders in a subject. Materials described herein include polysaccharide digestive products resulting from the enzymatic hydrolysis of low acyl gellan gum. Also describe herein are pharmaceutical compositions comprising one or more of such materials, and methods for their preparation and use.
Type:
Application
Filed:
February 12, 2016
Publication date:
February 1, 2018
Applicant:
The University of Toledo
Inventors:
Joshua J. Park, Dong-Shik Kim, Kenneth Hensley, Kevin Christopher, Vishruti Makani
Abstract: The use of selenite- or selenate-containing preparations supplemented with pharmaceutically acceptable or food-compatible acids for the preparation of an agent intended for topical or buccal application or mucosal administration is described.
Type:
Application
Filed:
October 5, 2017
Publication date:
February 1, 2018
Applicant:
SELO MEDICAL GMBH
Inventors:
Bodo KUKLINSKI, Peter KÖSSLER, Norbert FUCHS
Abstract: The use of selenite- or selenate-containing preparations supplemented with pharmaceutically acceptable or food-compatible acids for the preparation of an agent intended for topical or buccal application or mucosal administration is described.
Type:
Application
Filed:
October 5, 2017
Publication date:
February 1, 2018
Applicant:
SELO MEDICAL GMBH
Inventors:
Bodo KUKLINSKI, Peter KÖSSLER, Norbert FUCHS
Abstract: A liposomal rehydration salt formulation comprising phosphatidylcholine liposomes, salts, water, and a percentage inclusion ratio of salts (salts retained within said liposomes/total salts) of at least 40%; and a process for preparing said formulation using tangential ultrafiltration.
Type:
Application
Filed:
October 3, 2017
Publication date:
February 1, 2018
Inventors:
Alcides NICASTRO, Alejandro Luis BARBARINI
Abstract: Provided is a method for preventing or treating inflammation and associated states (e.g. infection, hypersensitivity, pain) by administering a therapeutically effective amount of an oxidative reduction potential (ORP) water solution that is stable for at least about twenty-four hours. The ORP water solution administered in accordance with the invention can be combined with one or more suitable carriers and can be administered in conjunction with one or more additional therapeutic agents.
Abstract: The disclosure provides drug combinations and methods for treating human bladder cancer. The drug combination may include mitomycin, or an analogue thereof, cisplatin or an alternative platinum drug, and epirubicin or an alternative anthracycline drug and does not include gemcitabine.
Abstract: The present invention relates to methods for preventing or treating infectious diseases caused by extracellular microorganisms, such as bacteria and fungi, by systemically administering to a patient a compound containing gallium. The extracellular microorganisms targeted by the present methods include methicillin-resistant Staphylococcus aureus (MRSA), vancomycin-resistant Enterococcus faecalis (VRE), E. coli O157:H7, fluoroquinolone-resistant Salmonella typhi, and the like. Furthermore, in the present methods, gallium compounds can be co-administered with one or more conventional antimicrobial agents to treat infectious diseases with reduced risks of creating multi-drug resistant pathogens. The methods of the present invention is also applicable to those microorganisms, such as ulcer-causing Helicobacter pylori, complete eradication of which so far has been difficult to achieve.
Abstract: Provided herein are ?? T cell suppressors and methods of using such in detecting and treating solid tumors, as well as detection of solid tumors such as PDA or CRC based on the level of ?? T cells.
Type:
Application
Filed:
July 31, 2017
Publication date:
February 1, 2018
Inventors:
George Miller, Donnele Daley, Constantinos Zambirinis
Abstract: The present invention relates to the transient modification of cells. In particular embodiments, the cells are immune systems, such as PBMC, PBL, T (CD3+ and/or CD8+) and Natural Killer (NK) cells. The modified cells provide a population of cells that express a genetically engineered chimeric receptor which can be administered to a patient therapeutically. The present invention further relates to methods that deliver mRNA coding for the chimeric receptor to unstimulated resting PBMC, PBL, T (CD3+ and/or CD8+) and NK cells and which delivers the mRNA efficiently to the transfected cells and promotes significant target cell killing.
Abstract: A method for the treatment of psoriasis or an autoimmune disease in a subject by administering to said subject an effective amount of a cell-based composition containing a suspension of mesenchymal stem cells in crystalloid with a cellular concentration from 0.01 million to 3.0 million cells/ml.
Type:
Application
Filed:
May 18, 2017
Publication date:
February 1, 2018
Inventors:
Bernard Sze Piaw Chin, Kong Yong Then, Soon Keng Cheong
Abstract: A method of preparation of a solution used for therapeutic and regenerative applications having a concentration of at least about .05 microgram of total protein extract is disclosed. The method comprises the steps of: collecting an umbilical cord; incubating the umbilical cord in a solution containing antibiotics for sterilization; washing the umbilical cord in a buffered salt solution; homogenizing the umbilical cord in the buffered salt solution so as to produce an aqueous solution including the buffered salt solution; applying a sonicator at ultrasonic frequencies to the aqueous solution to further disrupt the aqueous solution; placing the aqueous solution into a centrifuge to separate the aqueous solution into a soluble component and a non-soluble component; filtrating and discarding the non-soluble component of the aqueous solution from the centrifuge through a 0.2 micron filter; and measuring protein concentration of the soluble component to insure at least about 0.05 microgram of total protein extract.
Abstract: The disclosure relates to methods for obtaining angiogenic factors, as well as to methods of treating cardiovascular disease and methods for stimulating angiogenesis.
Abstract: The present invention relates to a method for preventing or treating cancer in an individual comprising administering the individual with a prophylactically or therapeutically effective quantity of a gingival fibroblast-derived product.
Type:
Application
Filed:
October 12, 2017
Publication date:
February 1, 2018
Inventors:
Bruno GOGLY, Antoine LAFONT, Bernard COULOMB, Jean-Jacques LATAILLADE