Abstract: The present invention is directed to oral, therapeutically effective modified release pharmaceutical compositions of (?)-17-(cyclobutylmethyl)morphinan-3,14-diol and it pharmaceutically acceptable salts and the use thereof, including delayed onset and extended release dosage forms. The present invention is also directed at modified release dosage forms of oral (?)-17-(cyclobutylmethyl)morphinan-3,14-dial which provide robust efficacy and reduced potential for abuse and misuse.
Abstract: Dextromethorphan is used to lower blood pressure in a subject suffering from hypertension, alone or in combination with another anti-hypertensive agent. In particular, dextromethorphan acts synergistically with a calcium channel blocker, such as amlodipine, to result in a major improvement in the treatment of hypertension, with no or little adverse effects.
Abstract: Disclosed herein are compounds, compositions, and methods for preventing and treating proliferative diseases associated with aberrant receptor tyrosine kinase (RTK) activity. The therapeutic indications described herein more specifically relate to the non-selective inhibition of RTKs associated with vascular and pulmonary disorders.
Abstract: Disclosed herein are non-platinum-based (NPB) anti-cancer compounds useful for targeted chemotherapy, e.g., to generate anti-cancer effects for the treatment of cancer and other disorders while having no or minimal toxicity. The compounds N have the general formula I: (I) wherein A represents an aromatic core; at least one of Ra and Rb is an electron transfer promoter as defined herein, e.g., NH2; and at least one of Rc is a leaving group as defined herein, e.g., halogen; and the remainder of the molecule is as defined herein. Pharmaceutical compositions, methods, uses, kits and commercial packages comprising the anti-cancer compounds are also disclosed.
Abstract: The invention relates to new pyridopyrazine derivative compounds, to pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.
Type:
Application
Filed:
February 9, 2016
Publication date:
August 18, 2016
Applicant:
ASTEX THERAPEUTICS LIMITED
Inventors:
Valerio BERDINI, Gordon SAXTY, Patrick Rene ANGIBAUD, Olivier Alexis Georges QUEROLLE, Virginie Sophie PONCELET, Bruno ROUX, Lieven MEERPOEL
Abstract: The present invention describes new amino pyrimidine derivatives and pharmaceutically acceptable salts thereof which appear to interact with Bruton's tyrosine kinase (Btk). Accordingly, the novel amino pyrimidines may be effective in the treatment of autoimmune disorders, inflammatory diseases, allergic diseases, airway diseases, such as asthma and chronic obstructive pulmonary disease (COPD), transplant rejection, cancers e.g. of hematopoietic origin or solid tumors.
Type:
Application
Filed:
April 21, 2016
Publication date:
August 18, 2016
Applicant:
NOVARTIS AG
Inventors:
Daniela Angst, François Gessier, Anna Vulpetti
Abstract: A compound, or a pharmaceutically acceptable salt or ester thereof, having a structure of: wherein X is a divalent linking moiety; and R1-R10 are each individually H, optionally-substituted alkyl, optionally-substituted alkoxy, optionally-substituted aryl, optionally-substituted cycloalkyl, optionally-substituted heterocyclic, halogen, amino, or hydroxy, provided that at least one of R3 or R8 is an optionally-substituted alkyl, a substituted alkoxy, optionally-substituted aryl, optionally-substituted cycloalkyl, optionally-substituted heterocyclic, or halogen.
Type:
Application
Filed:
April 25, 2016
Publication date:
August 18, 2016
Applicants:
University of Pittsburgh - Of the Commonwealth System of Higher Education, The United States Government as represented by the Department of Veterans Affairs
Abstract: The invention provides compounds and pharmaceutically acceptable salts and esters and compositions thereof, for treating viral infections. The compounds and compositions are useful for treating Pneumovirinae virus infection including Human respiratory syncytial virus infections.
Type:
Application
Filed:
January 19, 2016
Publication date:
August 18, 2016
Inventors:
Constantine G. Boojamra, Hon Chung Hui, Petr Jansa, Richard L. Mackman, Jay P. Parrish, Michael Sangi, Dustin Siegel, David Sperandio, Hai Yang
Abstract: The present disclosure provides controlled-release delivery systems for oral delivery of active agents, e.g. lopinavir, comprising micro-particulated with enhanced oral bioavailability and efficacy, which may be used for treating HIV.
Abstract: A method of treating HIV in a subject, comprising administering to a subject in need thereof a therapeutically effective amount of a compound having a general Formula 1, or a pharmaceutically acceptable salt or ester thereof: wherein R1 is selected from H, optionally-substituted aryl, optionally-substituted heteroaryl, or optionally-substituted aliphatic; each R2 is independently selected from H, halogen, cyano, thioether, oxo, optionally-substituted amino, optionally-substituted heteroaryl, optionally-substituted aryl, or optionally-substituted aliphatic; a is 3 to 7; and the ring designates a heterocyclic or heteroaryl structure.
Type:
Application
Filed:
February 11, 2016
Publication date:
August 18, 2016
Applicant:
University of Pittsburgh - of the Commonwealth Sys tem of Higher Education
Abstract: The disclosure provides an extended release formulation of 5-fluorocytosine. In another aspect, a method of treating a fungal disease is provided. The method comprises administering to a subject in need thereof a fungus-treating effective amount of a composition comprising 5-fluorocytosine. In yet another aspect, a method of treating a cancer is provided. The method comprises administering to a subject in need thereof a sufficient amount of an expression vector to induce expression of cytosine deaminase which is capable of converting 5-fluorocytosine to 5-fluorourcail in cells of the cancer and a cancer-treating effective amount of a composition comprising 5-fluorocytosine.
Type:
Application
Filed:
April 22, 2016
Publication date:
August 18, 2016
Inventors:
Harry E. Gruber, Douglas J. Jolly, Kay Olmstead
Abstract: Embodiments of the present disclosure provide for compositions including an antimicrobial agent, pharmaceutical compositions including the antimicrobial agent, methods of treatment of an infection, methods of treatment using compositions or pharmaceutical compositions, and the like.
Type:
Application
Filed:
September 29, 2014
Publication date:
August 18, 2016
Applicants:
University of New Orleans, Board of Supervisors of Louisiana State University And Agricultural and Mechanical College
Abstract: Described herein are compounds of Formula (I)-(III), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Also provided are particles (e.g., nanoparticles) comprising compounds of Formula (I)-(III) and pharmaceutical compositions thereof that are mucus penetrating. Methods of using the compounds or pharmaceutical compositions thereof for treating and/or preventing diseases are also provided.
Type:
Application
Filed:
April 26, 2016
Publication date:
August 18, 2016
Inventors:
Winston Zapanta Ong, Pawel Wojciech Nowak, Ben C. Askew, Jinsoo Kim
Abstract: The present invention provides compounds, including resolved enantiomers, resolved diastereomers, solvates and pharmaceutically acceptable salts thereof, comprising the Formula Also provided are methods of using the compounds of this invention as AKT protein kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer.
Type:
Application
Filed:
April 28, 2016
Publication date:
August 18, 2016
Applicants:
Array BioPharma Inc., Genentech, Inc.
Inventors:
Ian S. Mitchell, James F. Blake, Rui Xu, Nicholas C. Kallan, Dengming Xiao, Keith Lee Spencer, Josef R. Bencsik, Eli M. Wallace, Stephen T. Schlachter, Anna L. Leivers, Jun Liang, Brian Safina, Birong Zhang, Christine Chabot, Steven Do
Abstract: Disclosed herein are new heterocyclic compounds and compositions and their application as pharmaceuticals for the treatment of disease. Methods of inhibiting PAS Kinase (PASK) activity in a human or animal subject are also provided for the treatment of diseases such as diabetes mellitus.
Type:
Application
Filed:
January 29, 2016
Publication date:
August 18, 2016
Inventors:
John McCall, Robert C. Kelly, Donna L. Romero
Abstract: {4-[5-(3-chloro-phenoxy)-oxazolo[5,4-d]pyrimidin-2-yl]-2,6-dimethyl-phenoxy}-acetic acid or a pharmaceutically acceptable salt thereof for use in the prevention or treatment of AKI (acute kidney injury). Medicament and pharmaceutical composition thereof.
Type:
Application
Filed:
October 15, 2014
Publication date:
August 18, 2016
Applicant:
Sanofi
Inventors:
Véronique BRIAND, Sabine GRATZER, Thomas HUEBSCHLE, Philip JANIAK, Dieter KADEREIT, Ashfaq PARKAR, Bruno POIRIER, Matthias SCHAEFER, Paulus WOHLFART
Abstract: Disclosed are topical preparations for inhibiting tyrosine kinase and preparation methods thereof, and especially topical pharmaceutical compositions for inhibiting tyrosine kinase and preparation methods thereof. The active ingredient of the topical preparations is Icotinib or a pharmaceutically acceptable salt thereof. The preparations are suitable for topical application, with minimal skin irritation, no adverse reactions such as pruritus, burning sensations, tingling, dry skin, erythema and rashes, without parahormone-related side effects such as skin atrophy, pigmentation or hypopigmentation for long-term use, as well as no related dermatological symptoms after drug withdrawal. The preparation methods are easily understood, operable, and controllable, and are suitable for industrialization.
Abstract: The present invention provides for a method for treating a disease condition associated with PI3-kinase ? and/or mTOR in a subject. In another aspect, the invention provides for a method for treating a disease condition associated with PI3-kinase ? and/or mTOR in a subject. In yet another aspect, a method of inhibiting phosphorylation of both Akt (S473) and Akt (T308) in a cell is set forth.
Type:
Application
Filed:
February 11, 2016
Publication date:
August 18, 2016
Inventors:
Pingda Ren, Yi Liu, Katayoun Jessen, Xin Guo, Christian Rommel, Troy Edward Wilson
Abstract: The invention is directed to a method of treatment for chronic pain, the method comprising administering to a mammal in need of such treatment a therapeutically effective amount of a compound of formula I, or a pharmaceutically acceptable salt thereof.
Type:
Application
Filed:
April 21, 2016
Publication date:
August 18, 2016
Applicant:
MediSynergics, LLC
Inventors:
Dennis Michael Godek, Harry Ralph Howard
Abstract: This invention pertains to methods of treating systemic lupus erythematosus and Sjogren's Syndrome with compounds that selectively inhibit the activity of Bcl-2 anti-apoptotic proteins.
Type:
Application
Filed:
April 22, 2016
Publication date:
August 18, 2016
Inventors:
Steven Elmore, Andrew Souers, Lichun Wang, Tariq Ghayur, Stuart J. Perper
Abstract: Described herein are compounds of Formula (I) or Formula (VI), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Also provided are particles (e.g., nanoparticles) comprising compounds of Formula (I) or Formula (VI) and pharmaceutical compositions thereof that are mucus penetrating. Methods of using the compounds or pharmaceutical compositions thereof for treating diseases are also provided.
Type:
Application
Filed:
April 26, 2016
Publication date:
August 18, 2016
Inventors:
Winston Zapanta Ong, Pawel Wojciech Nowak, Ben C. Askew, Jinsoo Kim
Abstract: The invention relates to 7-zminocephalosporanic acid derivative, Cefazolin, for use as the inhibitor of IL-15 and IL-2 receptors in the prevention and treatment of IL-15 and IL-2 overproduction related diseases.
Type:
Application
Filed:
September 29, 2014
Publication date:
August 18, 2016
Inventors:
Katarzyna Koziak, Barbara Zyzynska-Granica, Slawomir Filipek, Szymon Niewieczerzal, Bartosz Trzaskowski, Oliwia Zegrocka-Stendel, Malgorzata Dutkiewicz, Piotr Krzeczynski, Elzbieta Kaczmarek, Magdalena Winiarska
Abstract: Disclosed are methods and pharmaceutical compositions for treating diseases, disorders, and conditions associated with glucocorticoid receptor (GR) expression and activity. The disclosed methods typically include administering to a patient in need thereof a glucocorticoid receptor (GR) agonist and administering to the patient in need thereof a REDD1 inhibitor that inhibits expression or activity of REDD1, wherein the REDD1 inhibitor is administered before, concurrently with, or after the GR agonist is administered.
Type:
Application
Filed:
February 17, 2016
Publication date:
August 18, 2016
Applicant:
Northwestern University
Inventors:
Irina Budunova, Gleb Baida, Joel Dudley
Abstract: This invention relates to dosage forms for the delivery of drugs across the oral mucosa having improved transmucosal permeability. More specifically, the invention relates to an oral transmucosal dosage form comprising a primary vehicle comprising a crystallization inhibition agent (CIA) system and a drug, and a secondary vehicle. It also relates to methods of designing and making this dosage form, methods of administering this dosage form and methods of packaging the dosage forms.
Type:
Application
Filed:
April 29, 2016
Publication date:
August 18, 2016
Applicant:
ABON PHARMACEUTICALS, LLC
Inventors:
Salah U. AHMED, Yanming ZU, Karunakar NEELAM, Saad MUNTAZIM, Tahseen A. CHOWDHURY, Shiying TIAN
Abstract: This disclosure relates to methods of managing eye pain, for example, due to eye surgery. In certain embodiments, the disclosure relates to methods comprising administering a local anesthetic in combination with a steroid to the space around the eye in a subject in need thereof.
Abstract: The present invention relates to propellant-free topical spray compositions of halobetasol comprising halobetasol, an emollient, and a non-aqueous solvent. It also relates to a process for the preparation of the propellant-free topical spray compositions. It further relates to a method of treating topical skin condition by administering said 5 propellant-free topical spray compositions.
Abstract: The application provides formulations for the topical administration of an active agent comprising at least one steroid, in the form of topical sprays that are propellant-free, and/or substantially non-foaming, and/or alcohol-free. The present application also provides processes for preparing such compositions and methods of using them in management of skin diseases or disorders such as psoriasis, dermatoses, and other associated skin diseases or disorders.
Abstract: The application provides formulations for the topical administration of an active agent comprising at least one steroid, in the form of topical sprays that are propellant-free, and/or substantially non-foaming, and/or alcohol-free. The present application also provides processes for preparing such compositions and methods of using them in management of skin diseases or disorders such as psoriasis, dermatoses, and other associated skin diseases or disorders.
Abstract: Provided herein are methods for treating the symptoms of and inflammation associated with gastroesophageal reflux disease (GERD) and other conditions. Also provided herein are pharmaceutical compositions useful for the methods of the present invention.
Abstract: Oral and topical pharmaceutical compositions, kits and methods of treatment thereof for treating various skin disorder including acne, psoriasis, ichthyosis, photoaging, photodamaged skin, and, skin cancer.
Type:
Application
Filed:
April 22, 2016
Publication date:
August 18, 2016
Inventors:
Margaret Clagett-Dame, Hector F. DeLuca, Nircaq J. Nieves, Lori A. Plum, Mary E. Kaiser
Abstract: Inositol trisphosphate (ITPP) causes normalization of tumor vasculature and is a particularly effective cancer therapy when a second chemotherapeutic agent is administered following partial vascularization. ITPP also treats, alone or in combination, multi-drug resistant cancers. ITPP can also be used to reduce the amount of a second chemotherapeutic drug required for anticancer activity. In addition, ITPP enhances immune response and treats hyperproliferative disorders.
Type:
Application
Filed:
May 3, 2016
Publication date:
August 18, 2016
Inventors:
Yves Claude Nicolau, Jean-Marie Lehn, Claudine Kieda
Abstract: The combined use of 1,2-dilinoleoyl-sn-glycero-3-phosphocholine and 1-palmitoyl-2-oleoyl-sn-glycero-3-phosphocholine affords a superior anti-depressive action, an improving effect on the cognitive function associated with depression, an improving effect on the stress-induced suppression of Akt activation, and a suppressive action on the stress-induced GSK-3? activation. Therefore, the present invention can provide an antidepressant combination drug, an agent for improving cognitive function associated with depression, an agent for improving stress-induced suppression of Akt activation and an agent for suppressing stress-induced GSK-3? activation.
Type:
Application
Filed:
October 14, 2014
Publication date:
August 18, 2016
Applicant:
NISHIZAKI BIOINFORMATION RESEARCH INSTITUTE
Abstract: Described herein are compositions comprising shortened fibers of poly-N-acetylglucosamine and/or a derivative thereof (“sNAG nanofibers”) and anti-bacterial applications of such compositions. The sNAG nanofibers may be formulated into compositions for the prevention and/or treatment of bacterial infections and diseases associated with such infections. Regimens employing such compositions are also described.
Type:
Application
Filed:
October 29, 2015
Publication date:
August 18, 2016
Applicant:
MARINE POLYMER TECHNOLOGIES, INC.
Inventors:
John N. Vournakis, Sergio Finkielsztein
Abstract: The present invention relates to compounds useful for the treatment or prevention of bacteria infections. These compounds have formula I: The invention also provides pharmaceutically acceptable compositions containing the compounds and methods of using the compositions in the treatment of bacteria infections. Finally, the invention provides processes for making compounds of the invention.
Type:
Application
Filed:
April 27, 2016
Publication date:
August 18, 2016
Inventors:
Yeeman K. Ramtohul, Sanjoy Kumar Das, Caroline Cadilhac, Thumkunta Jagadeeswar Reddy, Louis Vaillancourt, Michel Gallant, Bingcan Liu, Evelyne Dietrich, Frederic Vallee, Julien Martel, Carl Poisson
Abstract: The present invention relates to a sustained release composition comprising topiramate and one or more pharmaceutical excipients, wherein the composition comprises a single population of beads, wherein each bead comprises: a) an inert core, b) an inner layer comprising topiramate, c) an outer layer comprising at least one sustained release material and at least one alkalizer. It also relates to methods of preparing such compositions and using those compositions in the treatment of neurological and/or psychiatric condition.
Type:
Application
Filed:
February 9, 2016
Publication date:
August 18, 2016
Applicant:
CADILA HEALTHCARE LIMITED
Inventors:
Sushrut Krishnaji KULKARNI, Ajaykumar HANDA, Amit Om Prakash GUPTA
Abstract: The invention is directed to a method for increasing phosphatidylcholine in the blood of a subject comprising administering to the subject a composition having uridine or a metabolic precursor of uridine; choline or a metabolic precursor of choline; and at least one omega-3 fatty acid and/or omega-6 fatty acid, the phosphatidylcholine has a glycerol portion and the glycerol portion is bonded to two fatty acids and the total amount of carbons in the fatty acids is about 16 to 40 carbon atoms.
Abstract: Methods are presented for treating cancers and hematopoietic stem cell disorders, comprising administering to a subject with a cancer or hematopoietic stem cell disorder who is receiving a treatment regimen, a heparin derivative capable of inhibiting, reducing, abrogating or otherwise interfering with the binding of CXCL12 to CXCR4, wherein the cancer or hematopoietic stem cell disorder is one in which interaction of CXCL12 with CXCR4 privileges the cancer or disordered HSCs against therapeutic intervention. In preferred embodiments, the heparin derivative is a substantially 2-O, 3-O-desulfated heparin derivative.
Abstract: Embodiments described herein relate to formulations for and methods of use for eye drop formulations comprising carboxymethyl cellulose (CMC) and hyaluronic acid (HA) with an improved distribution on the cornea during blinking.
Type:
Application
Filed:
April 27, 2016
Publication date:
August 18, 2016
Inventors:
Bereth J. Beard, Wendy Blanda, David Marsh, Joseph G. Vehige, Peter Simmons, Haixia Liu, Steven Matsumoto
Abstract: Provided are uses of a poloxamer and methods of administering a poloxamer for treating hemo-concentration, such as hemo-concentration resulting from dehydration and/or diuresis in a subject. Administration of a poloxamer prevents, treats or otherwise reduces adverse effects of hemo-concentration, dehydration and/or diuresis.
Abstract: Provided herein are pharmaceutically acceptable sodium thiosulfate and pharmaceutical compositions thereof. Also provided herein are methods for determining the total non-purgeable organic carbon in a sodium thiosulfate-containing sample. Further provided herein are methods for producing pharmaceutically acceptable sodium thiosulfate. Still further provided herein are methods of treatment comprising the administration of pharmaceutically acceptable sodium thiosulfate.
Type:
Application
Filed:
April 25, 2016
Publication date:
August 18, 2016
Inventors:
Craig Sherman, Catherine Marie Smith, Kevin Robert Wirtz, Erich Schulze
Abstract: A bioelectronic medical method and system for rapidly destroying living cancer cells and the tumors they create including metastatic off-spring of such tumor(s) regardless of their location within a human or animal body. Calcium ions can be inserted into a nucleus a cancer cell(s). The nucleus of the cancer cell(s) is then fragmented among many cancer cells (e.g., in a tumor) simultaneously with the transmission of a destructive analog electrically encoded signals to provide a medical cancer treatment thereof. A first target of medical cancer treatment is aimed principally into the nucleus and mitochondrion bodies of a malignancy associated with the cancer cell(s).
Abstract: The present invention is anti-itching powder that blocks transmission to stratum corneum and invasion up to epidermal cells by emulsion as a result of further concentration on skin stratum corneum. The emulsion is produced by mixing sweat continuously secreted during rest and sebum. The emulsion becomes a cell disorder composition. Specifically, the anti-itching powder as a fine powder contains main ingredients of aluminum chloride or alum and cyclodextrin. A fine powder as a base is dispersed into and combined with the fine powder. The application of the fine powder over the skin prevents sudden itch without blocking emission and transpiration of water in the sweat from the skin stratum corneum.
Abstract: [Problem] To provide a solid dialysis A agent which is to be used in preparing a bicarbonate dialysis fluid, which enables the setting of a low total acetate ion content in a dialysis fluid, and which exhibits excellent storage stability of glucose or the like and a reduced acetic acid odor. [Solution] A solid dialysis A agent which is to be used in preparing a bicarbonate dialysis fluid, wherein: the solid dialysis A agent contains glucose, acetic acid and an acetate salt; at least a part of a mixture of the acetic acid with the acetate salt is an alkali metal diacetate; and the acetic acid/acetate salt molar ratio is adjusted to 1/0.5 to 1/2. This solid dialysis A agent makes it possible to prepare a bicarbonate dialysis fluid which has a total acetate ion concentration of 2 to less than 6 mEq/L. Further, the dialysis A agent exhibits excellent stability of ingredients and a reduced acetic acid odor.
Abstract: A formulation comprising platelet rich plasma (PRP) for treatment of patients who have experienced brain injury, consisting of a mixture of human autologous plasma, D5W, glutathione, methylcobalamin, and regular insulin. The formulation is infused directly adjacent to a patient's brain through the nostrils or nares of the nasal cavity. Treatment using the formulation may be supplemented with one or more therapies including hyperbaric oxidation therapy (HBOT), cranial osteopathic therapy, intravenous (IV) nutrition, electroencephalographic (EEG) biofeedback, low level laser therapy (LLLT), transcranial magnetic stimulation (TMS), adult stem cell treatments, and a ketogenic diet and medium-chain triglyceride (MCT) oil therapy.
Abstract: The present invention relates to compositions and methods for inducing epitope spreading by administering to a mammal an effective amount of a cell genetically modified to express a chimeric antigen receptor (CAR). The invention also relates to identification of antigens and antibodies involved in the epitope spreading associated with CAR T cells.
Type:
Application
Filed:
July 12, 2013
Publication date:
August 18, 2016
Inventors:
Carl H. June, Bruce L. Levine, Michael D. Kalos, Yangbing Zhao
Abstract: This invention relates to stem cell microparticles and miRNA isolated from these microparticles, their use and production thereof, in particular neural stem cell microparticles and their use in therapy of cancer, typically a nestin-positive cancer. The cancer may be glioma, melanoma, breast cancer, pancreatic cancer or prostate cancer. The stem cell microparticle is typically an exosome or microvesicle and may be derived from a neural stem cell line. The neural stem cell line may be a conditionally-immortalised stem cell line such as CTX0E03 (deposited at the ECACC with Accession No. 04091601).
Type:
Application
Filed:
October 9, 2014
Publication date:
August 18, 2016
Inventors:
Caroline Hicks, John Sinden, Lara Stevanato, Randolph Corteling
Abstract: The present invention provides an isolated population of bone marrow-derived endothelial progenitor cells (EPCs) and uses thereof for the treatment of vascular diseases.