Abstract: The present invention relates to methods of treating various central nervous system disorders using novel triazolo[4,3-a]pyridine derivatives of Formula (I) wherein all radicals are as defined in the claims. The compounds according to the invention are positive allosteric modulators of the metabotropic glutamate receptor subtype 2 (“mGluR2”), which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes to prepare such compounds and compositions, and to the use of such compounds for the prevention or treatment of neurological and psychiatric disorders and diseases in which mGluR2 is involved.
Type:
Application
Filed:
November 19, 2015
Publication date:
March 10, 2016
Inventors:
JOSE MARIA CID-NUNEZ, DANIEL OEHLRICH, ANDRES AVELINO TRABANCO-SUAREZ, GARY JOHN TRESADERN, JUAN ANTONIO VEGA RAMIRO, GREGOR JAMES MACDONALD
Abstract: Described herein are methods of treating muscular dystrophy, including Becker's muscular dystrophy and Duchenne muscular dystrophy. The methods comprise administering a phosodiesterase 5A (PDE5A) inhibitor, such as tadalafil, to a subject in need thereof. Administering the PDE5A inhibitor has beneficial effects such as restoring functional sympatholysis, alleviating ischemic insult to dystrophin-deficient muscle membranes, reducing use-dependent muscle injury, and thus can slow muscular dystrophy disease progression.
Abstract: The present invention is directed to compounds or pharmaceutically acceptable salts thereof for use in the treatment of fibrotic diseases such as idiopathic pulmonary fibrosis (IPF).
Type:
Application
Filed:
November 18, 2015
Publication date:
March 10, 2016
Inventors:
Richard Francis WOOSTER, Pauline Teresa Lukey, Patrick John Thompson Vallance
Abstract: The present invention relates to a method of treating ovarian cancer in a female human and to pharmaceutical combinations useful in such treatment. In particular, the method relates to a ovarian cancer treatment method that includes administering 5-[[4-[(2,3-dimethyl-2H-indazol-6-yl)methylamino]-2-pyrimidinyl]amino]-2-methylbenzenesulfonamide, or a pharmaceutically acceptable salt thereof, and 2-[(5-chloro-2-[[3-methyl-1-(1-methylethyl)-1H-pyrazol-5-yl]amino]-4-pyridinyl)amino]-N-methoxybenzamide, or a pharmaceutically acceptable salt thereof, and optionally 1,7?,10?-trihydroxy-9-oxo-5?,20-epoxytax-11-ene-2?,4,13?-triyl 4-acetate 2-benzoate 13-{(2R,3S)-3-[(tert-butoxycarbonyl)amino]-2-hydroxy-3-phenylpropanoate}, to a human in need thereof.
Type:
Application
Filed:
November 19, 2015
Publication date:
March 10, 2016
Inventors:
Kurt R. AUGER, Justin Bottsford-Miller, Ani Sood
Abstract: The invention relates to novel quinazolinone compounds and their use as inhibitors of PI3 kinases, for example, PI3K?, for treating and/or preventing diseases, disorder, and conditions associated with modulating PI3 kinase activity. Novel 3 -aryl-2-((arylamino)methyl)quinazolin-4(3H)-one derivatives and pharmaceutically acceptable salts or solvates thereof and their use for the treatment or prevention of diseases, disorders, and conditions associated with the activity of one or more PI3 kinase, such as PI3K?, are disclosed.
Abstract: Methods, compounds and kits relating to treating cancer, reducing kinase inhibitor or resistance, and reducing or preventing diminished ectodomain shedding are described.
Type:
Application
Filed:
April 17, 2015
Publication date:
March 10, 2016
Inventors:
Frank B. Gertler, Linda G. Griffith, Douglas A. Lauffenburger, Aaron Samuel Meyer, Miles Aaron Miller, Madeleine Oudin
Abstract: This invention relates to pyrrolopyrimidine derivatives of formula (I): where R1, X, p, R4, R2 and R3 are as defined herein, and their use as pharmaceuticals.
Type:
Application
Filed:
April 28, 2015
Publication date:
March 10, 2016
Inventors:
David R. WITTY, David Norton, Jason Paul Tierney, Ghislaine Lorthioir, Mairi Sime, Karen Louise Philpott
Abstract: The present invention generally relates to the transdermal delivery of sildenafil and other phosphodiesterase type 5 inhibitors. While transdermal transport of sildenafil in creams and other topical formulations have been previously described, propylene glycol has not previously been recognized as a transdermal enhancer. However, in some aspects of the present invention, certain concentrations of propylene glycol can have a surprising effect on the transdermal delivery of sildenafil and other phosphodiesterase type 5 inhibitors, e.g., doubling the amount of transdermal delivery in some cases.
Abstract: The present invention relates to the Janus kinase (JAK) inhibitors 3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]octanenitrile or 3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]heptanenitrile, as well as its compositions and methods of use, which is useful in the treatment of JAK-associated diseases including, for example, inflammatory and autoimmune disorders, skin disorders, cancer, and other diseases.
Abstract: The present invention is directed to novel substituted bicyclic aromatic compounds useful as S-nitrosoglutathione reductase (GSNOR) inhibitors, pharmaceutical compositions comprising such compounds, and methods of making and using the same.
Abstract: The disclosure describes methods for treating or preventing HIV in a patient using a combination of tenofovir alafenamide and dolutegravir, and to compositions containing such compounds.
Type:
Application
Filed:
September 1, 2015
Publication date:
March 10, 2016
Inventors:
Darius M. Babusis, Adrian S. Ray, Jianhong Wang
Abstract: Methods and compounds for the treatment or prevention of oxidative damage in a mammalian subject. The treatment and/or prevention may be on inhibiting heme-induced lipid peroxidation. Also discloses are methods and compounds for treating or preventing isoprostane-mediated tissue damage.
Type:
Application
Filed:
September 15, 2015
Publication date:
March 10, 2016
Inventors:
John A. Oates, L. Jackson Roberts, Ned A. Porter, Olivier Boutaud
Abstract: The present invention embraces methods for identifying compounds that modulate the activity of telomerase. Compounds of the invention are identified by designing or screening for a compound which binds to at least one amino acid residue of the TRBD, “thumb,” “finger,” and/or “palm” domain; or FP-pocket, PT-pocket or Th-pocket of telomerase and testing the compound for its ability to modulate the activity of telomerase. Compounds selected for interacting with the T-pocket or Fingers-Palm pocket of telomerase are also provided.
Abstract: There is provided a compound of formula I: or a pharmaceutically acceptable salt thereof. There are also provided processes for the manufacture of a compound of Formula 1, and the use of a compound of Formula 1 as a medicament and in the treatment of cancer.
Type:
Application
Filed:
June 8, 2015
Publication date:
March 10, 2016
Inventors:
Heather Mary Ellen Duggan, Frederic Georges Marie Leroux, Karine Fabienne Malagu, Niall Morrison Barr Martin, Keith Menear, Graeme Cameron Murray Smith
Abstract: Provided herein are compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with HDAC activity, particularly diseases or disorders that involve activity of HDAC1 and/or HDAC2. Such diseases include cancer, sickle-cell anemia, beta-thalassemia, and HIV.
Abstract: The present invention relates to methods of treating cell proliferative disorders, such as cancer or Proteus syndrome, by utilizing 3-(3-(4-(1-aminocyclobutyl)phenyl)-5-phenyl-3H-imidazo[4,5-b]pyridin-2-yl)pyridin-2-amine or 3-(3-(4-(1-aminocyclobutyl)phenyl)-5-(3-morpholinophenyl)-3H-imidazo[4,5-b]pyridin-2-yl)pyridin-2-amine or N-(1-(3-(3-(4-(1-aminocyclobutyl)phenyl)-2-(2-aminopyridin-3-yl)-3H-imidazo[4,5-b]pyridin-5-yl)phenyl)piperidin-4-yl)-N-methylacetamide. The methods of the present invention can also relate to methods of treating cell proliferative disorders, such as cancer or Proteus syndrome, by utilizing the above compounds in combination with ((R)-6-(2-fluorophenyl)-N-(3-(2-((2-methoxyethyl)amino)ethyl)phenyl)-5,6-dihydrobenzo[h]quinazolin-2-amine).
Type:
Application
Filed:
September 4, 2015
Publication date:
March 10, 2016
Inventors:
Daniel T. Dransfield, Sudharshan Eathiraj, Jean-Marc Lapierre, Brian Schwartz, Yi Yu
Abstract: The present invention relates to novel combinations of active ingredients for use in the prevention and/or treatment of tumors. The tumors treated by the composition according to the invention overexpress SEC62 gene and overproduce Sec62 protein. The combination of active ingredients comprises at least a SERCA inhibitor and at least a Calmodulin antagonist.
Type:
Application
Filed:
April 22, 2014
Publication date:
March 10, 2016
Inventors:
Richard Zimmermann, Markus Greiner, Johannes Linxweiler, Maximilian Linxweiler
Abstract: The present invention relates to methods, compositions, kits and reagents for determining the prognosis of a clinical response in a human patient to a medicament which acts in the central nervous system (CNS) and which is a substrate of the ABCB1 protein. Further, the invention relates to a combination of medicaments for the treatment of human patients having specific polymorphisms in the ABCB1 gene.
Type:
Application
Filed:
July 16, 2015
Publication date:
March 10, 2016
Applicant:
Max-Planck-Gesellschaft zur Förderung der Wisenschaften e. V.
Abstract: Described herein are compositions comprising a prostaglandin FP receptor agonist (PFPRA) compound and a fatty acid, e.g., oleic acid, that, when topically applied to the skin, locally delivers a therapeutically effective amount of the PFPRA compound or active metabolite thereof to subcutaneous fat under the skin. The therapeutic effect is, for example, reduction of the subcutaneous fat under the skin. Further provided are methods of reducing body fat in a subject comprising topically administering the composition to the subject. The present invention also provides kits comprising the composition and instructions for use.
Abstract: Disclosed is a diagnostic test to determine suitable therapeutic intervention of subjects suffering from subclinical Cushing's syndrome [SCS] and also agents that antagonise the action of cortisol or inhibit excess cortisol production in the treatment of conditions such as SCS in the presence of an adrenal incidentaloma.
Abstract: Pharmaceutical compositions, including unit dosage forms, comprising fine particle abiraterone acetate with or without an antioxidant and or a sequesting agent as well as methods for producing and using such compositions are described.
Type:
Application
Filed:
August 11, 2015
Publication date:
March 10, 2016
Inventors:
H. William Bosch, Marck Norret, Paul Nemeth, Matt Callahan
Abstract: A storage stable ointment of the present invention comprises a vitamin D compound, a corticosteroid, and an N,N-di(C1-C8) alkylamino substituted, (C4-C18) alkyl (C2-C18) carboxylic ester a (C1-C4)-alkyl (C8-C22) carboxylic ester in a petrolatum ointment base, and optionally containing mineral oil and/or tocopherol. Preferably, the vitamin D compound is calcipotriene, the corticosteroid is selected from the group consisting of clobetasol propionate and betamethasone dipropionate, and the N,N-di(C1-C8) alkylamino substituted, (C4-C18) alkyl (C2-C18) carboxylic ester comprises dodecyl 2-(N,N-dimethylamino)-propionate (DDAIP).
Type:
Application
Filed:
November 13, 2015
Publication date:
March 10, 2016
Applicant:
NEXMED HOLDINGS, INC.
Inventors:
William Shifeng WEI, Yiping WANG, Jianzhen PAN, Sung Hi JO
Abstract: The present invention provides for novel treatments of obesity and overweight and related disorders. The invention provides, in part, method of treatment comprising, or uses of inositol-tripyrophosphate (ITPP) in these disease states.
Type:
Application
Filed:
March 14, 2014
Publication date:
March 10, 2016
Applicant:
NormOxys, Inc.
Inventors:
Ruth Greferath, Jean-Marie Lehn, Yves Claude Nicolau
Abstract: The present invention relates to phosphonate compounds, compositions containing them, processes for obtaining them, and their use for treating a variety of medical disorders, e.g., osteoporosis and other disorders of bone metabolism, cancer, viral infections, and the like.
Abstract: Provided are use of ginsenoside F2 in the prevention, improvement or treatment of liver disease, and a pharmaceutical composition, a health functional food, and a feed composition including ginsenoside F2. Ginsenoside F2 inhibits fat synthesis and accumulation in the liver, and increases distribution of regulatory T cells capable of inhibiting activity of inflammatory cells, thereby preventing hepatitis, and also increases expression of anti-inflammatory cytokine IL-10 in regulatory T cells, and inhibits differentiation of naive T cells into Th17 cells, and is thereby effectively used for the treatment of various liver diseases.
Type:
Application
Filed:
August 27, 2015
Publication date:
March 10, 2016
Inventors:
Won Il Jeong, Ju Yeon Jung, Sun Chang Kim, Wan Taek Im
Abstract: The invention includes methods of treating, preventing, or limiting obesity or weight gain, or reducing or suppressing appetite, by the administration of A2A adenosine receptor pathway agonists. The A2AR pathway agonists may be administered in conjunction with a therapeutic agent having a side effect of weight gain, in order to prevent or limit that weight gain. In some instances, the A2AR pathway agonist is administered as a sleeping pill, and in other instances the A2AR pathway agonist is administered in a non-drowsy formulation.
Abstract: Provided herein are methods for treating or preventing an immune disease in a subject by administering a composition comprising a therapeutically effective amount of NAD+. Also provided herein are methods and assays for diagnosing an immune disease in a subject by measuring the level of NAD+ in a biological sample obtained from the subject.
Abstract: The present invention is related to the field of healing of internal injuries. In particular, the present invention provides compositions and methods comprising molecules and nanoparticles with linked ?-gal epitopes from synthetic origin for induction of recruitment and activation of macrophages within or surrounding injured tissue of treated patients. These macrophages further recruit stem cells into the injured tissues. The recruited macrophages and stem cells promote the repair and regeneration of the treated injured tissue. This invention further teaches methods and compositions comprising molecules and nanoparticles with linked ?-gal epitopes of synthetic origin for inducing recruitment and activation of macrophages into biomaterial implants for improving the conversion of such implants into functional tissues and organs within treated patients.
Abstract: The present invention describes and claims pharmaceutical compositions in gel form for use in the treatment of intervertebral disc degeneration, in particular the forms of dehydration and emptying of the nucleus pulposus known as “black disc disease”. These compositions comprise a hyaluronic acid derivative which forms hydrogels with precise rheological characteristics that make it ideal for filling the nucleus pulposus.
Abstract: Phosphorylated hydrogels obtained by co-cross-linking hyaluronic acid with dextran, a process for preparing same, and a use of the hydrogel for the encapsulation and extended release of active principles as well as cells for use in regenerative human and veterinary medicine.
Abstract: Provided herein are various gas-filled particles having a stabilized membrane that encapsulates the gas. Pharmaceutical compositions, methods of use and treatment, and methods of preparation are also described.
Abstract: The invention relates to a gaseous composition containing xenon as active ingredient for use in preventing or limiting tumour cell migration and/or limiting or preventing metastasis formation in an individual suffering from cancer. The prevention or limitation of tumour cell migration is obtained through the action of the xenon on free cancer cells. The xenon acts on the free cancer cells carried by the blood. The effective volume proportion of xenon is between 5% and 79%, it is preferably at least 50%. The gaseous composition also contains a volume proportion of oxygen (O2) of at least 21%. It is administered by inhalation or insufflation.
Abstract: The invention relates to a dialysis formulation, optionally a citrate containing dialysis formulation, comprising selenium (Se), optionally in combination with further trace elements selected from rubidium (Rb), cobalt (Co), molybdenum (Mo), and zinc (Zn). The dialysis formulation is intended to be used in dialysis treatment.
Type:
Application
Filed:
May 8, 2014
Publication date:
March 10, 2016
Applicant:
Gambro Lundia AB
Inventors:
Anna Bryland, Ola Carlsson, Karin Sandin
Abstract: The present invention relates to pharmaceutical compositions of nitrites such as inorganic nitrites, or any pharmaceutically acceptable salts, solvates, or prodrugs thereof, and the medical use of these compositions. The pharmaceutical compositions, which can be formulated for oral administration, can provide immediate release or extended release of the nitrite ion (NO2?). The pharmaceutical compositions of the invention are useful, for example, for the treatment of chronic tissue ischemia.
Type:
Application
Filed:
September 8, 2015
Publication date:
March 10, 2016
Inventors:
Christopher Kevil, Anthony Giordano, Douglas R. Flanagan, Panayiotis P. Constantinides
Abstract: The invention provides a source of sodium thiosulfate via the dialysate used to cleanse the bool of toxic and metabolic waste in the patients undergoing hemodialysis, peritoneal dialysis, or gastro-intestinal dialysis for treatment of end-stage or near end-stage chronic renal disease. In the method of the invention, dialysis solution components contain therapeutic amounts of sodium thiosulfate, which when fully reconstituted for use as a single solution, deliver 20-130 mg/dl of dialysate.
Abstract: A method for manufacturing chlorine dioxide gel includes the following steps: a step of dissolving peg-copolymer bis-decyltetradeceth in hot water to form an aqueous solution of peg-copolymer bis-decyltetradeceth; a step of heating the aqueous solution of peg-copolymer bis-decyltetradeceth obtained in the above step to form a gel like colloid; a step of dissolving pure chlorine dioxide gas in water to form an aqueous solution of chlorine dioxide; and a step of uniformly mixing the aqueous solution of chlorine dioxide and the colloid of peg-copolymer bis-decyltetradeceth to form a chlorine dioxide gel, whereby with the above steps, a method for manufacturing chlorine dioxide gel that stably preserves chlorine dioxide gas in a gel is provided.
Abstract: A pharmaceutical preparation for treating connective tissue damage in man and in animals, comprising a therapeutically effective amount of a glycosaminoglycan composition comprising chondroitin sulfate and hyaluronan, in combination with isolated stem cells. Methods of use and kits containing the glycosaminoglycan composition and materials for isolating stem cells and for treating connective tissue damage and repair of cartilage in man and in animals are also provided.
Abstract: The invention features compositions comprising agents having cardiac protective activity isolated from epicardial progenitor cells and derivatives thereof, and methods for the use of such compositions.
Type:
Application
Filed:
August 14, 2015
Publication date:
March 10, 2016
Applicant:
THE UNIVERSITY OF VERMONT AND STATE AGRICULTURE COLLEGE
Abstract: A sheet-shaped cell culture and method for producing a sheet-shaped cell culture are disclosed having a high activity such as high cytokine productivity and a production method thereof. The method for producing a sheet-shaped cell culture can include freezing cells, thawing the frozen cells and forming a sheet-shaped cell culture. A sheet-shaped cell culture which is produced by the production method and which has a high activity and a method for treating a disease associated with an abnormality of a tissue with the sheet-shaped cell culture.
Abstract: The present invention provides a method for determining the clinical prognosis of a human subject to the administration of a pharmaceutical composition comprising of stem cells (preferably mesenchymal stem cells), stromal cells, regulatory T-cells, fibroblasts and combinations thereof.
Type:
Application
Filed:
March 17, 2014
Publication date:
March 10, 2016
Inventors:
Olga DE LA ROSA, Eleuterio LOMBARDO, Wilfried DALEMANS
Abstract: Disclosed is a formulation for accelerating wound healing, preparation method and administering method of the same. A formulation for accelerating wound healing comprises cell culture medium which is obtained by culturing transfected endothelial progenitor cells which are acquired by transfecting microRNA let-7g into endothelial progenitor cells. And the preparation method of formulation for accelerating wound healing comprises the isolating step, the transfecting step and the culturing step. A method for accelerating wound healing is implemented by administering a therapeutically effective amount of the formulation to an organism's wound.
Abstract: Described herein are compositions composed of micronized placental components and optionally a sealant, and pharmaceutical compositions thereof. Also described are systems, apparatuses, and methods for applying the combination of micronized placental components and adhesives optionally a sealant (e.g., adhesive or gelation agent) for wound care and other medical applications.
Type:
Application
Filed:
September 8, 2015
Publication date:
March 10, 2016
Inventors:
Adam McQueen, Frank Burrows, Thomas Koob
Abstract: A honey based composition is described. The composition includes a mixture of honey, a short chain fatty alcohol and a fatty ester or wax. The composition has applications for use in wound dressings and in one embodiment may be a gel. The composition has a higher than expected storage stability, remaining stable for many weeks when held at elevated temperatures and retains all of the other desirable characteristics including anti-microbial activity.
Abstract: The present invention relates to at least one probiotic strain chosen from Lactobacillus paracasei, or at least one probiotic strain chosen from Lactobacillus paracaseiin combination with at least one probiotic strain chosen from Lactobacillus plantarum, for use in the treatment or prevention of osteoporosis or for use in increasing the absorption of at Ca2+ ions, in a mammal, preferably in a human.
Abstract: Bacteriophages are provided that infect strains of Enterococcus faecalis, an opportunistic bacterial pathogen that causes human disease. Also provided are methods of treating Enterococcus faecalis by therapeutic administration of such bacteriophages.
Type:
Application
Filed:
March 25, 2014
Publication date:
March 10, 2016
Inventors:
Roy H. Stevens, Hongming Zhang, Derrick E. Fouts, Jessica DePew
Abstract: An oral formulation as described herein can comprise pomegranate extract, panax ginseng extract, and c. sinensis, where each is present in an amount effective to counteract and/or prevent effects of aging in a subject when administered to the subject. The effects of aging can include age-related changes in gene expression.
Type:
Application
Filed:
July 7, 2015
Publication date:
March 10, 2016
Applicant:
NSE PRODUCTS, INC.
Inventors:
Angela Mastaloudis, Steve Wood, Richard Weindruch, Tomas Alberto Prolla, Jamie Louis Barger, Mark Bartlett, Scott B. Ferguson, Joseph Chang
Abstract: The present invention discloses the use of a composition comprising an effective amount of an extract of Eurycoma longifolia for the production of a preparation to stimulate and/or enhance the immune system. In a preferred embodiment, the extract comprises active ingredients, which include eurycomanone, protein, polysaccharide and glycosaponin in appropriate amounts. In another preferred embodiment, the extract has an activity selected from the group consisting of: increasing the number of T-cells; improving Scoring of Immunological Vigor (SIV), a comprehensive index of overall immune function; lowering the immunological age, a comprehensible form of immune function based on T-cell number and proliferative activity; reducing fatigue; and alleviating or reducing stress. Also disclosed is a method of for treating an individual to achieve an outcome selected from the group consisting of increasing the number of T-cells, improving SIV (i.e.
Type:
Application
Filed:
August 31, 2015
Publication date:
March 10, 2016
Inventors:
Annie George, Yuuki Kawasaki, Azreena Abas
Abstract: The present invention relates to a food composition comprising Suaeda japonica as an active ingredient for preventing or alleviating diabetes, and to a method for preparing the composition. When Suaeda japonica powder of the present invention is administered to OLETF mice in which obesity and diabetes are naturally induced during growth due to a defect of the CCK-1 gene, an increase in blood glucose and production of glycosylated hemoglobin are inhibited, and the effect of improving glucose tolerance is exhibited. Also, a high blood level of adiponectin, which relates to an improvement in insulin sensitivity and to the recovery of glucose metabolism function, is maintained, and antidiabetic activity, specifically, the effect of alleviating or preventing diabetes, is excellent.
Type:
Application
Filed:
July 23, 2013
Publication date:
March 10, 2016
Inventors:
Kyung Sik HAM, Jeong Yong CHO, Sun Young PARK, Zhangjun HUANG