Abstract: The present invention relates to methods of treating and/or ameliorating the severity of inflammation and autoimmunity in the central nervous system (CNS). In one embodiment, the present invention provides a method of treating multiple sclerosis by administering a therapeutically effective dosage of nicotine, or a pharmaceutical equivalent, analog, derivative, or salt thereof.
Type:
Application
Filed:
January 5, 2017
Publication date:
May 4, 2017
Applicant:
DIGNITY HEALTH
Inventors:
Fu-Dong Shi, Ronald J. Lukas, Timothy Vollmer
Abstract: Compounds of formula I, defined herein, act both as muscarinic receptor antagonists and beta2 adrenergic receptor agonists and are useful for treating broncho-obstructive and inflammatory diseases.
Type:
Application
Filed:
January 12, 2017
Publication date:
May 4, 2017
Applicant:
CHIESI FARMACEUTICI S.p.A.
Inventors:
Fabio RANCATI, Andrea RIZZI, Laura CARZANIGA, Ian LINNEY, Chris KNIGHT, Wolfgang SCHMIDT
Abstract: A method of providing a patient with controlled release of ketone-containing opioid using a prodrug capable, upon enzymatic activation and intramolecular cyclization, of releasing the ketone-containing opioid is disclosed. The disclosure also provides such prodrug compounds and pharmaceutical compositions comprising such compounds. Such pharmaceutical compositions can optionally include an enzyme inhibitor that interacts with the enzyme(s) to mediate the enzymatically-controlled release of the ketone-containing opioid from the prodrug so as to modify enzymatic cleavage of the prodrug. Also included are methods to use such compounds and pharmaceutical compositions.
Type:
Application
Filed:
October 5, 2016
Publication date:
May 4, 2017
Inventors:
Thomas E. Jenkins, Craig O. Husfeld, Julie D. Seroogy, Jonathan W. Wray
Abstract: The present invention provides a pharmaceutical composition comprising naltrexone or an analogue thereof for use in the treatment of a subject having a tumour/cancer; wherein the naltrexone or the analogue thereof is to be administered to the subject in a first treatment phase, followed by a recovery phase; wherein, following the recovery phase, a small molecule signalling inhibitor selected from the group consisting of PI3-kinase inhibitors, AKT inhibitors, taxanes, antimetabolites, alkylating agents and cell cycle inhibitors is to be administered to the subject in a second treatment phase; the recovery phase being characterised by the absence of administration of the naltrexone or the analogue thereof and the small molecule signalling inhibitor.
Abstract: Disclosed in certain embodiments is an oral dosage form comprising a therapeutically effective amount of a drug susceptible to abuse; and an effective amount of an irritant to impart an irritating sensation to an abuser upon administration of said dosage form after tampering.
Abstract: The present invention relates to the discovery of a novel opioid modulator effective in reducing pharmacologically induced weight gain associated with atypical antipsychotic use. The present invention provides methods of reducing antipsychotic induced weight gain, methods for suppressing food intake and reducing ghrelin levels induced by atypical antipsychotic medications in a patient.
Abstract: The present invention provides for a derivative of monoterpene or sesquiterpene, such as a perillyl alcohol derivative. For example, the perillyl alcohol derivative may be a perillyl alcohol carbamate. The perillyl alcohol derivative may be perillyl alcohol conjugated with a therapeutic agent such as a chemotherapeutic agent. The present invention also provides for a method of treating a disease such as cancer, comprising the step of delivering to a patient a therapeutically effective amount of a derivative of monoterpene for sesquiterpene). The route of administration may vary, and can include, inhalation, intranasal, oral, transdermal, intravenous, subcutaneous or intramuscular injection.
Type:
Application
Filed:
January 18, 2017
Publication date:
May 4, 2017
Inventors:
Thomas CHEN, Daniel LEVIN, Satish PUPALLI
Abstract: There are provided pharmaceutical compositions comprising a compound of Formula (I) as defined herein and an amount of an alkaline effervescent agent that is sufficient to provide satisfactory in vitro dissolution; and further comprising one or more pharmaceutically acceptable ingredients; and to processes for obtaining them.
Abstract: A mast cell inhibitor, a pharmaceutical composition and a method for treating patients afflicted with Progressive Supranuclear Palsy (PSP), wherein the patients are treated with a tyrosine kinase inhibitor, c-Kit inhibitor or mast cell inhibitor, in particular masitinib or a pharmaceutically acceptable salt or solvate thereof, optionally in combination with at least one pharmaceutically active ingredient.
Type:
Application
Filed:
October 28, 2016
Publication date:
May 4, 2017
Inventors:
Alain MOUSSY, Jean-Pierre KINET, Colin MANSFIELD
Abstract: The invention relates to disubstituted 3-benzofuranyl-indol-2-one-3-acetamidopiperazine derivatives of the general formula (I) where R1, R2, R3, R4, R5, R6, R7, R8, R9 and n are such as defined in claim 1, to a method for preparing same, and to the therapeutic use of said compounds.
Abstract: Provided are compounds that target the lanthionine synthetase C-like protein 2 pathway. The compounds can be used to treat a number of conditions, including infectious disease, autoimmune disease, diabetes, and a chronic inflammatory disease.
Type:
Application
Filed:
December 9, 2016
Publication date:
May 4, 2017
Applicant:
Biotherapeutics, Inc.
Inventors:
Josep Bassaganya-Riera, Adria Carbo Barrios, Richard Gandour, Julian D. Cooper, Raquel Hontecillas
Abstract: The invention relates to a combination of a first compound selected from N-(3,5-dimethoxyphenyl)-N?-(1-methylethyl)-N-[3-(1-methyl-1H-pyrazol-4-yl)quinoxalin-6-yl]ethane-1,2-diamine or a pharmaceutically acceptable salt thereof or a solvate thereof, and N-(2-fluoro-3,5-dimethoxyphenyl)-N-(1H-imidazol-2-ylmethyl)-3-(1-methyl-1H-pyrazol-4-yl)pyrido[2,3-b]pyrazin-6-amine or a pharmaceutically acceptable salt thereof or a solvate thereof; and a second compound which is a cMet inhibitor. The combination is for use in the treatment of a proliferative disorder, in particular for use in the treatment of cancer.
Type:
Application
Filed:
March 26, 2015
Publication date:
May 4, 2017
Applicant:
ASTEX THERAPEUTICS LTD
Inventors:
Eleonora JOVCHEVA, Timothy Pietro Suren PERERA
Abstract: Compounds for use in the treatment of human immunodeficiency virus (HIV) infection are disclosed. The compounds have the following Formula (Ia): including stereoisomers and pharmaceutically acceptable salts thereof, wherein A?, R1, R2 and R3 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
Type:
Application
Filed:
November 11, 2016
Publication date:
May 4, 2017
Inventors:
Elizabeth M. Bacon, Zhenhong R. Cai, Jeromy J. Cottell, Mingzhe Ji, Haolun Jin, Scott E. Lazerwith, Philip Anthony Morganelli, Hyung-Jung Pyun
Abstract: 2-(2-methylamino-pyrimidin-4-yl)-1H-indole-5-carboxylic acid [(S)-1-carbamoyl-2-(phenyl-pyrimidin-2-yl-amino)-ethyl]-amide for use in the treatment of pain associated with osteoarthritis in the knee.
Type:
Application
Filed:
June 30, 2015
Publication date:
May 4, 2017
Inventors:
Tobias Paehler, Klaus Flechsenhar, Kirsten Grothe, Martin Lunnon, Christelle Jan
Abstract: The present invention provides methods of treating cancer using pyrimidine and pyridine compounds which are inhibitors of Bruton's tyrosine kinase (BTK).
Type:
Application
Filed:
November 4, 2016
Publication date:
May 4, 2017
Inventors:
Bayard R. HUCK, Samantha M. GOODSTAL, Claude GIMMI-MCKIM
Abstract: The present disclosure relates to novel solid pharmaceutical formulations and process for their preparation. The present disclosure also provides, in part, methods of using the pharmaceutical formulations for regulating the expression of apolipoprotein A-I (ApoA-I), and their use for the treatment and prevention of cardiovascular disease and related disease states, including cholesterol- or lipid-related disorders, such as, for example, atherosclerosis.
Abstract: Disclosed are an anti-abnormal proliferation of angiogenesis compound represented by formula I, use and intermediate thereof. The compound has good effect against abnormal proliferation of angiogenesis, and the activity of the compound is produced by inhibiting VEGFR2. The compound can be used for treating diseases, such as wet macular degeneration, inflammation, malignant tumor and the like, caused by abnormity of angiogenesis and protein kinases such as VEGFR2, FGFR2 and the like.
Abstract: Disclosed herein are methods and compositions for treating, as well as identifying potential therapeutics for, cancers or diabetes, with compounds that inhibit the activity of menin, preferably the compounds are capable of inhibiting MLL binding to menin.
Type:
Application
Filed:
June 10, 2015
Publication date:
May 4, 2017
Applicant:
THE TRUSTEES OF THE UNIVERSITY OF PENNSYLVANIA
Abstract: Compounds of Formula I: and salts thereof in which R1, R2, R3, R4, X, Y and n have the meanings given in the specification, are inhibitors of Trk kinases and are useful in the treatment of diseases which can be treated with a Trk kinase inhibitor such as pain, cancer, inflammation, neurodegenerative diseases and certain infectious diseases.
Type:
Application
Filed:
January 9, 2017
Publication date:
May 4, 2017
Inventors:
Shelley Allen, Steven W. Andrews, Kevin Ronald Condroski, Julia Haas, Lily Huang, Yutong Jiang, Timothy Kercher, Jeongbeob Seo
Abstract: The invention provides methods that relate to a novel therapeutic strategy for the treatment of hematological malignancies and inflammatory diseases. In particular, the method comprises administration of a compound of formula A, wherein R is H, halo, or C1-C6 alkyl; R? is C1-C6 alkyl; or a pharmaceutically acceptable salt thereof; and optionally a pharmaceutically acceptable excipient; and one or more additional therapeutic agents optionally selected from the group consisting of bendamustine, rituximah, and ofatumumab.
Type:
Application
Filed:
June 30, 2016
Publication date:
May 4, 2017
Inventors:
W. Michael GALLATIN, Roger G. ULRICH, Neill A. GIESE, Brian LANNUTTI, Albert YU, Langdon MILLER, Thomas M. JAHN
Abstract: A beverage composition comprising phlorotannin, a ginseng extract and caffeine, and being effective in improving work performance, such as improving concentration and fatigue, preventing sleepiness, relieving hangovers, reducing headaches and improving physical abilities.
Type:
Application
Filed:
August 4, 2016
Publication date:
May 4, 2017
Inventors:
Haeng-Woo LEE, Hyun-Cheol CHEON, Seong-Ho KIM, Hyeon-Cheol SHIN, Ju-Hee KIM, Jae-Keun OH
Abstract: The present invention relates to pharmaceutical compositions comprising fixed dose combinations of a DPP-4 inhibitor drug and a partner drug, processes for the preparation thereof, and their use to treat certain diseases.
Type:
Application
Filed:
January 11, 2017
Publication date:
May 4, 2017
Inventors:
Thomas FRIEDL, Michael BRAUN, Kenji EGUSA, Hikaru FUJITA, Megumi MARUYAMA, Takaaki NISHIOKA
Abstract: This invention is in the area of improved compounds and methods for transiently protecting healthy cells, and in particular hematopoietic stem and progenitor cells (HSPC), from the damage associated with ionizing radiation (IR) exposure using selective radioprotectants.
Type:
Application
Filed:
December 7, 2016
Publication date:
May 4, 2017
Applicant:
G1 Therapeutics, Inc.
Inventors:
Jay Copeland Strum, John Emerson Bisi, Patrick Joseph Roberts, Francis Xavier Tavares
Abstract: The technology provided herein relates to the novel use of compounds for improving cognition, concentration capacity, learning capacity and/or memory retentiveness, in particularly for the treatment and/or prophylaxis of cognitive, concentration capacity, learning capacity and/or memory retentiveness disorders.
Abstract: The present application relates to novel, chiral 2,5-disubstituted cyclopentanecarboxylic acid derivatives, to a method for their preparation, to their use on their own or in combinations for the treatment and/or prevention of diseases, and to their use for producing medicaments for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of diseases of the respiratory tracts, the lung and the cardiovascular system.
Type:
Application
Filed:
March 31, 2015
Publication date:
May 4, 2017
Inventors:
Hartmut BECK, Volkhart Min-Jian LI, Andreas TIMMERMANN, Pamela BOGNER, Yolanda CANCHO GRANDE, Dirk BROHM, Michael GERISCH, Hannah JÖRISSEN, Dieter LANG
Abstract: Compounds of formula I wherein: R1 is and R2, R4, and R6-9 are defined herein, and pharmaceutically acceptable salts and esters thereof. These compounds inhibit PI3 kinase and mTOR, and may be used to treat diseases mediated by PI3 kinase and mTOR, such as a variety of cancers. Methods for making and using the compounds of this invention are disclosed. Various compositions containing the compounds of this invention are also disclosed.
Type:
Application
Filed:
October 30, 2015
Publication date:
May 4, 2017
Inventors:
Aranapakam Mudumbai VENKATESAN, Zecheng CHEN, Christoph Martin DEHNHARDT, Osvaldo DOS SANTOS, Efren Guillermo DELOS SANTOS, Arie ZASK, Jeroen Cunera VERHEIJEN, Joshua Aaron KAPLAN, David James RICHARD, Semiramis AYRAL-KALOUSTIAN, Tarek Suhayl MANSOUR, Ariamala GOPALSAMY, Kevin Joseph CURRAN, Mengxiao SHI
Abstract: The present invention relates to a method of treating pre-term labour with retosiban in subjects with conditions resulting in uterine overdistension including polyhydroamnios and multiple gestation. In another aspect, the invention relates to a method of preventing pre-term labour in subjects by the prophylactic administration of retosiban.
Abstract: The present invention relates to aryl- or heteroaryl-substituted benzene compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also relates to the use of such compounds for research or other non-therapeutic purposes.
Type:
Application
Filed:
November 8, 2016
Publication date:
May 4, 2017
Inventors:
Kevin Wayne Kuntz, Richard Chesworth, Kenneth William Duncan, Heike Keilhack, Natalie Warholic, Christine Klaus, Sarah Kathleen Knutson, Timothy James Nelson Wigle, Masashi Seki, Syuji Shirotori, Satoshi Kawano
Abstract: The present invention relates to a pharmaceutical composition comprising poorly soluble compounds such as BSC class II or IV kinase inhibitors, a process for the preparation thereof and its use in the treatment of diseases, in particular cancer, further particularly in non-small lung cancer.
Abstract: The present disclosure relates to bicyclic heterocycles, and pharmaceutical compositions of the same, that are inhibitors of the FGFR4 enzyme and are useful in the treatment of FGFR4-associated diseases such as cancer.
Type:
Application
Filed:
January 17, 2017
Publication date:
May 4, 2017
Inventors:
Liang Lu, Liangxing Wu, Bo Shen, Wenqing Yao
Abstract: A method for treating Alzheimer's Disease (AD) by administering an efficacious amount of artemisone. It is hypothesized that the treatment counters AD by inhibiting the production of the amyloid protein which has been implicated as a contributing factor to the onset of AD and the associated AD dementia and memory loss. Additionally, artemisone acts to reduce inflammation in the brain associated with AD by inhibiting tumor necrosis factor (TNF). Artemisone is a particularly useful AD treatment as it is able to cross the blood-brain barrier whereas many other TNF inhibitors are unable to do so. Artemisone may be administered via the following routes: subcutaneous, intravenous, intrathecal, intramuscular, intranasal, oral, transepidermal, parenteral, by inhalation, or intracerebroventricular.
Abstract: The present invention relates to a new class of cephalosporin derivatives of formula (I), notably having CXCR4 receptor antagonist effect, useful as a therapeutic agent for treating cancer, in particular for treating breast cancer, lung cancer and uveal melanoma. The invention further relates to a pharmaceutical composition comprising a compound of formula (I) and an additional antitumor drug for treating cancer.
Type:
Application
Filed:
April 2, 2015
Publication date:
May 4, 2017
Inventors:
ARNAUD SINAN KARABOGA, VIOLETA ISABEL PEREZ-NUENO, MICHEL SOUCHET, DIDIER DECAUDIN
Abstract: The present disclosure relates generally to sol-gel polymer composites that comprise chitosan, a hydrophilic polymer, a gelation agent, and optional additional ingredients in a suitable medium. Advantageously, the sol-gel polymer composite can form a durable seal or strong solid in response to one or more physiological stimulus. The disclosure further relates to medical and veterinary uses of the composite, particularly, methods and delivery systems for reducing or preventing the incidence of a mammary disorder in a dairy animal. More particularly, the disclosure includes methods and sol-gel polymer composite compositions for creating a physical barrier on the teat surface or in the teat canal or cistern of a non-human animal for prophylactic treatment of mammary disorders such as mastitis wherein the sol-gel polymer creates a seal in response to one or more physiological stimulus.
Type:
Application
Filed:
November 2, 2016
Publication date:
May 4, 2017
Inventors:
SUMITRA RAJAGOPALAN, WILMS BAILLE, PIOTR KUJAWA, Christopher A. Zook, Rebecca R. Quesnell, Dennis L. Huczek, Stephen L. Secreast, Laibin Luo, Tammy A. Sanders
Abstract: Compounds that are fatty acid synthesis modulators are provided. The compounds may be used to treat disorders characterized by disregulation of the fatty acid synthase function by modulating the function and/or the fatty acid synthase pathway. Methods are provided for treating such disorders including viral infections, such as hepatitis C infection, cancer and metabolic disorders, such as non-alcoholic steatohepatitis (NASH).
Type:
Application
Filed:
November 11, 2016
Publication date:
May 4, 2017
Inventors:
Douglas I. Buckley, Gregory Duke, Allan S. Wagman
Abstract: The present invention relates to a method of modulating production of neurons and/or oligodendrocytes from neural progenitor cells of human white matter and to a method of treating a subject for a condition modulated by underproduction of oligodendrocytes from human white matter. Both of these methods involve administering an agonist or antagonist of one or more molecules set forth in Tables 1 and/or 2 to the neural progenitor cells. Also disclosed is a method of using an inhibitor of sterol synthesis to differentiate oligodendrocyte progenitor cells to oligodendrocytes.
Abstract: Disclosed are compositions comprising topical corticosteroids, such as fluticasone and mometasone, and a biopolymer in a cream base, wherein the cream base comprises a primary and a secondary emulsifier, a waxy material, a co-solvent, a preservative, an acid, a chelating agent, a penetration enhancer, a buffering agent, and water. The biopolymer comprises chitosan. The compositions disclosed herein are suitable for the treatment of dermatological conditions including but not limited to healing wounds and treatment of dermatitis.
Abstract: Methods are provided herein for enhancing the effectiveness of medical therapies by administering agents that suppress a biological damage response that is inducible by the medical therapy administered to a subject. In certain embodiments, a method is provided for administering an anti-senescent cell agent that suppresses a biological response comprising cellular senescence that is induced by the medical therapy.
Abstract: The present invention relates to therapeutic agents for the targeted delivery of an immunosuppressive agent to monocytes and/or monocyte-derived cells comprising a binding moiety with specificity for monocytes and/or monocyte-derived cells and an immunosuppressive agent. In one embodiment, the agent is a glucocorticoid-antibody conjugate. The invention also relates to methods, uses, kits and compositions comprising such agents.
Type:
Application
Filed:
December 1, 2016
Publication date:
May 4, 2017
Inventors:
Niels Jonas Heilskov Graversen, Pia Svendsen, Peter Astrup Christensen, Soren Kragh Moestrup, Holger Jon Moller, Gabriele Anton
Abstract: Disclosed are compositions comprising betamethasone, such as betamethasone dipropionate or betamethasone valerate, and a biopolymer in a cream base, wherein the cream base comprises a primary and a secondary emulsifier, a waxy material, a co-solvent, a preservative, an acid, a chelating agent, a buffering agent, and water. The biopolymer comprises chitosan. The compositions disclosed herein are suitable for the treatment of dermatological conditions including but not limited to healing wounds and treatment of dermatitis.
Abstract: Disclosed are compositions comprising topical corticosteroids, such as clobetasol propionate and halobetasol propionate, and a biopolymer in a cream base, wherein the cream base comprises a primary and a secondary emulsifier, a waxy material, a co-solvent, a preservative, an acid, a chelating agent, a buffering agent, and water. The biopolymer comprises chitosan. The compositions disclosed herein are suitable for the treatment of dermatological conditions including but not limited to healing wounds and treatment of dermatitis.
Abstract: The invention described herein pertains to the treatment of infections arising in bones and/or joints. The invention described herein also pertains to the treatment of infections arising from implants and prostheses. Bone and joint infections (BJIs) represent a serious medical condition that, if untreated, can lead to complete loss or loss of use of bones or, joints in the patient, and even death. BJIs include many diseases, such as acute and chronic osteomyelitis, including pediatric osteomyelitis, septic arthritis, and others.
Abstract: Provided herein are methods of treating a variety of disorders related to fat accumulation in humans with pharmaceutical formulations containing deoxycholic acid.
Type:
Application
Filed:
November 4, 2016
Publication date:
May 4, 2017
Applicant:
Kythera Biopharmaceuticals, Inc.
Inventors:
Frederick Beddingfield, Elisabeth Sandoval, Nancy Jorgesen, Serge Lichtsteiner, Paul Lizzul, Todd Gross, Christine Somogyi
Abstract: The present invention discloses fused triterpene compounds, represented by the compounds of Formula I (as described herein), processes for their preparation, pharmaceutical compositions comprising the said compounds, their use as retinoid-related orphan receptors gamma (ROR?) modulators and/or interleukin-17 (IL-17) inhibitors and methods for their use in the treatment of a disease or a disorder mediated by ROR? and/or IL-17.
Abstract: Disclosed herein is a pharmaceutical composition, comprising: (a) spironolactone; (b) a xanthan gum; (c) an anti-foaming agent; (d) a preservative; (f) a dispersing agent; (g) a sweetening agent; (h) a flavoring agent; (i) optionally a buffer to maintain the pH of the pharmaceutical composition within a range described herein; and (j) a sufficient amount of a water vehicle.
Abstract: The present invention relates to a process for preparing a comestible product comprising xylitol said method comprising: (a) subjecting a composition comprising xylitol in an amount ranging from about 60% to about 100% by weight to extrusion treatment inside an extrusion apparatus under conditions sufficient to form and maintain the xylitol in a slurry and (b) then shaping the extruded slurry and cooling the product to form a solid. The present invention additionally is directed to a product produced therefrom.
Type:
Application
Filed:
January 17, 2017
Publication date:
May 4, 2017
Inventors:
Steven M. Kumiega, Thomas J. Carroll, Ashley L. Boldt, Paula M. Gibson, Robert J. Huzinec, Burton Douglas Brown, David M. Stumpf
Abstract: The present invention relates to a stable oral liquid pharmaceutical composition of celecoxib or its pharmaceutically acceptable salts thereof. The celecoxib present in the compositions as described herein do not show any precipitation when subjected in Fasted-State Simulated Gastric Fluid (FaSSGF) at pH 2.0, temperature of 37° C.±0.5° C. and under stirring at a speed of 50 rpm at least for 60 minutes. It also relates to the process of preparing and method of using said composition of celecoxib.
Abstract: This invention relates to a composition that comprises inositol phosphates and/or bisphosphonates, and to the use thereof to prevent the loss of substances of biological interest in the body of patients subjected to dialysis and to maintain sufficient physiological levels of said substances to regulate physiological and/or pathological processes, these substances being inhibitors of pathological crystallisation.
Type:
Application
Filed:
January 18, 2017
Publication date:
May 4, 2017
Inventors:
Félix GRASES FREIXEDAS, Joan PERELLO BESTARD, Fernando TUR ESPINOSA, Antonia COSTA BAUZA, Rafael M. PRIETO ALMIRALL, Isabel GOMILA MUÑIZ
Abstract: The present invention relates to stable pharmaceutical compositions of fosaprepitant or a salt thereof in the form of ready-to-use or ready-to-dilute compositions suitable for parenteral administration.
Abstract: Oral dosage forms of osteoclast inhibitors, such as nitrogen-containing bisphosphonates, such as zoledronic acid in an acid or a salt form, or in a molecular complex can be used to treat or alleviate pain or related conditions, such as complex regional pain syndrome.