Abstract: The present invention relates to phenylcyclopropylamine derivatives. In particular, pharmaceutical compositions comprising phenylcyclopropylamine derivatives are provided. The compounds of this invention can, inter alia, be used for the treatment and the prevention of cancer as well as neurodegenerative diseases or disorders.
Type:
Grant
Filed:
January 21, 2010
Date of Patent:
March 31, 2015
Assignee:
Oryzon Genomics, S.A.
Inventors:
Nathalie Guibourt, Alberto Ortega Munoz, Julio Castro-Palomino Laria
Abstract: Provided herein are macrocyclic serine protease inhibitor compounds, for example, of Formula Ia or Ib, pharmaceutical compositions comprising the compounds, and processes of preparation thereof. Also provided are methods of their use for the treatment of an HCV infection in a host in need thereof.
Type:
Grant
Filed:
January 10, 2013
Date of Patent:
March 31, 2015
Assignee:
Idenix Pharmaceuticals, Inc.
Inventors:
Christophe Claude Parsy, Francois-Rene Alexandre, Michel Derock, Frederic Leroy, Jean-Christophe Meillon, Thierry Convard, Dominique Surleraux
Abstract: A pharmaceutical composition in multilayer-coated form including an omega-3 fatty acid or an alkyl ester thereof and a statin-based drug, and more particularly, a pharmaceutical composition for oral administration including: (a) a gelatin capsule core containing an omega-3 fatty acid or an alkyl ester thereof; (b) a first coating layer formed by coating, on the gelatin capsule core, hydroxypropyl methylcellulose and a copolymer of butyl methacrylate, (2-demethylaminoeethyl) methacrylate, and methyl methacrylate at a weight ratio of 1:2:1; and (c) a second coating layer formed by coating, on the first coating layer, a coating solution containing a statin-based drug.
Type:
Application
Filed:
May 21, 2013
Publication date:
March 26, 2015
Applicant:
KUHNIL PHARM. CO., LTD.
Inventors:
Jae-Pyoung Cho, Pung-Sok Lee, Seul-A Lee, Min-Ho Jeong, Mase Lee
Abstract: Novel hetarylaminoquinoline derivatives of formula (I) wherein X, Z, Het, R1, R2, R3 and R4 have the meaning according to claim 1, are inhibitors of ATP consuming proteins, and can be employed, inter alia, for the treatment of tumors.
Type:
Grant
Filed:
October 12, 2010
Date of Patent:
March 24, 2015
Assignee:
Merck Patent GmbH
Inventors:
Alfred Jonczyk, Christiane Amendt, Frank Zenke
Abstract: The present invention relates to compounds and compositions and their application as pharmaceuticals for treating, preventing, or reversing injury to skeletal or cardiac muscles, for treating or preventing diseases relating to the structure and function of skeletal or cardiac muscle, and for inducing regeneration or restructuring of skeletal or cardiac muscle as a means of treating diseases relating to abnormalities in skeletal or cardiac muscle structure and function in a human or animal subject.
Type:
Application
Filed:
March 22, 2013
Publication date:
March 19, 2015
Inventors:
Francisco Villarreal, George F. Schreiner, Guillermo Ceballos
Abstract: The present invention is directed to novel quinoline compounds useful as S-nitrosoglutathione reductase (GSNOR) inhibitors, pharmaceutical compositions comprising such compounds, and methods of making and using the same.
Abstract: The present invention relates to a medicament for treating occlusive and/or ischemic vascular disorder comprising a carbostyril derivative and carnitine.
Abstract: The invention is directed to methods of treating organ specific infections in a host organism by administering compounds that target host receptors and/or host cellular signaling molecules to prevent a pathogen from infecting the organ. For example, the administration of a compound to prevent a pathogen from crossing the blood-brain barrier to prevent a brain infection.
Abstract: The invention relates to compositions and methods for regulating hair growth. Specifically, the invention relates to regulating hair growth by regulating the activity one of the prostaglandin D2 (PGD2) receptors, DP-2 (GPR44). Compositions and methods for regulating hair growth include inhibiting hair growth by administering a DP-2 agonist, or stimulating hair growth by administering a DP-2 antagonist.
Type:
Application
Filed:
March 15, 2013
Publication date:
March 12, 2015
Inventors:
George Cotsarelis, Garret Fitzgerald, Luis Garza
Abstract: The invention relates to ROR modulators; compositions comprising an effective amount of a ROR modulator; and methods for treating or preventing diseases associated with ROR.
Type:
Application
Filed:
April 30, 2013
Publication date:
March 12, 2015
Inventors:
Anderson GAWECO, Jefferson TILLEY, John WALKER, Samantha PALMER, James BLINN
Abstract: The present invention describes a method for the treatment of a neurological condition in a subject which comprises administering to a subject in need thereof a therapeutically effect amount of a compound of the formula or pharmaceutically acceptable salts, hydrates, or solvates thereof.
Type:
Grant
Filed:
September 19, 2007
Date of Patent:
March 10, 2015
Assignee:
Prana Biotechnology Limited
Inventors:
Kevin Jeffrey Barnham, Elisabeth Colette Louise Gautier, Gaik Beng Kok, Guy Krippner
Abstract: Compounds of formula (I) wherein R1, R2, R3, and Y are defined in the description are TRPA1 antagonists. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also disclosed.
Type:
Application
Filed:
November 4, 2014
Publication date:
March 5, 2015
Inventors:
Richard J. Perner, Michael E. Kort, Stanley DiDomenico, Jun Chen, Anil Vasudevan
Abstract: Disclosed are substituted quinolines of formula 1 wherein R1 and R2 are defined herein, the processing of making and using the same.
Type:
Application
Filed:
October 30, 2014
Publication date:
March 5, 2015
Inventors:
Matthias HOFFMANN, Daniel BISCHOFF, Georg DAHMANN, Jasna KLICIC, Gerhard SCHAENZLE, Stefan Ludwig Michael WOLLIN, Serge Gaston CONVERS-REIGNIER, Stephen Peter EAST, Frederic Jacques MARLIN, Clive McCARTHY, John SCOTT
Abstract: At least one compound selected from among coumarin and/or derivative thereof, butylated hydroxyanisole, ethoxyquine and mixtures thereof, and admixtures thereof with other active agents selected from among active agents for combating desquamative conditions of the scalp, plant extracts having propigmenting activity and active agents that slow hair loss and/or promote hair regrowth, are useful for preventing and/or limiting and/or stopping the development of canities.
Abstract: The present invention is to provide an inhibitor that inhibits differentiation of T cells into Th1 cells. The inhibitor that inhibits differentiation of T cells into Th1 cells contains, as an active ingredient, pitavastatin or a salt thereof.
Type:
Grant
Filed:
October 31, 2012
Date of Patent:
March 3, 2015
Assignees:
Kowa Co., Ltd., National University Corporation Nagoya University
Abstract: Disclosed herein are systems and methods for contributing to the local treatment of pain. More specifically, the disclosed systems and methods contribute to the local treatment pain by inhibiting the NF?B family of transcription factors.
Type:
Grant
Filed:
February 5, 2010
Date of Patent:
March 3, 2015
Assignee:
Warsaw Orthopedic, Inc.
Inventors:
Eric N. Burright, Lisa L. Shafer, Bill McKay, John Zanella
Abstract: The present invention provides secondary 8-hydroxyquinoline-7-carboxamide derivatives of general formula (I) and pharmaceutically acceptable salts thereof. These compounds are useful as antifungal agents. Specifically, these compounds were tested against Tricophyton Rubrum, Tricophyton Mentagrophytes, Aspergillus Niger and Scopulariopsis Brevicaulis. These compounds are active against Candida species such as Candida Albicans and Candida Glabrata.
Type:
Grant
Filed:
December 28, 2010
Date of Patent:
March 3, 2015
Assignee:
Polichem SA
Inventors:
Stefania Gagliardi, Simone Del Sordo, Federico Mailland, Michela Legora
Abstract: The present specification discloses pharmaceutical compositions, methods of preparing such pharmaceutical compositions, and methods and uses of treating a cardiovascular disease in an individual using such pharmaceutical compositions.
Type:
Application
Filed:
October 21, 2014
Publication date:
February 19, 2015
Applicant:
Infirst Healthcare Limited
Inventors:
Robin Mark Bannister, John Brew, Suzanne Jane Dilly, Gregory Alan Stoloff, Wilson Caparros-Wanderley
Abstract: Embodiments of the invention include methods of treating, preventing, and/or reducing the risk of fibrosis in an individual in need thereof. In some embodiments, particular small molecules are employed for treatment, prevention, and/or reduction of the risk of fibrosis. In at least particular cases, the small molecules are inhibitors of STAT3.
Type:
Application
Filed:
July 18, 2014
Publication date:
February 19, 2015
Inventors:
David J. Tweardy, Moses M. Kasembeli, Marvin X. Xu, Sandeep K. Agarwal, Mesias Pedroza
Abstract: The subject invention is directed to a pharmaceutical composition comprising an open matrix network carrying a pharmaceutically active ingredient, wherein the open matrix network comprises both the polysaccharides levan and inulin.
Abstract: Disclosed herein are methods of diagnosing and treating infectious disease characterized by a pathology that involves hemorrhaging or pathological vascular leakage.
Abstract: The subject invention is directed to a pharmaceutical composition comprising an open matrix network carrying a pharmaceutically active ingredient, wherein the open matrix network comprises levan.
Abstract: Monomeric and dimeric trioxane thioacetals and methods of their use for treating subjects infected with malaria or other parasitic infectious diseases including, but not limited to, toxoplasmic infection; subjects afflicted with psychiatric conditions associated with toxoplasmic infection; and subjects afflicted with cancer.
Type:
Application
Filed:
February 28, 2013
Publication date:
January 29, 2015
Applicant:
THE JOHNS HOPKINS UNIVERSITY
Inventors:
Gary H. Posner, Alexander M. Jacobine, Rachel D. Slack, Jennifer R. Mazzone
Abstract: Embodiments of the invention include methods of preventing and/or reducing the risk or severity of an allergic reaction in an individual. In some embodiments, particular small molecules are employed for prevention and/or reduction in the risk or severity of anaphylaxis. In at least particular cases, the small molecules are inhibitors of STAT3. In some cases, the small molecule comprises N-(1?,2-dihydroxy-1,2?-binaphthalen-4?-yl)-4-methoxybenzenesulfonamide.
Type:
Application
Filed:
July 18, 2014
Publication date:
January 29, 2015
Inventors:
David J. Tweardy, Moses M. Kasembeli, Marvin X. Xu, Josh Milner
Abstract: The invention provides antimicrobial compounds and compositions, and methods of using them. The compounds and compositions include, for example, a compound of any one of Formulas I-X. The invention further provides methods of preparing the compounds, and useful intermediates for their preparation. The compounds can possess highly specific and selective activity, such as antibacterial activity and/or enzymatic inhibitory activity. Accordingly, the compounds and compositions can be used to treat bacterial infections, or to inhibit or kill bacteria, either in vitro or in vivo.
Abstract: The present invention describes a method for the treatment of a neurological condition in a subject which comprises administering to a subject in need thereof a therapeutically effect amount of a compound of the formula or pharmaceutically acceptable salts, hydrates, or solvates thereof.
Type:
Application
Filed:
October 9, 2014
Publication date:
January 22, 2015
Applicant:
PRANA BIOTECHNOLOGY LIMITED
Inventors:
Kevin Jeffrey BARNHAM, Elisabeth Colette Louise GAUTIER, Gaik Beng KOK, Guy KRIPPNER
Abstract: Embodiments of the invention include methods of treating, preventing, and/or reduce the risk or severity of a condition selected from the group consisting of muscle wasting, muscle weakness, cachexia, and a combination thereof in an individual in need thereof. In some embodiments, particular small molecules are employed for treatment, prevention, and/or reduction in the risk of muscle wasting. In at least particular cases, the small molecules are inhibitors of STAT3.
Type:
Application
Filed:
July 18, 2014
Publication date:
January 22, 2015
Inventors:
David J. Tweardy, Moses M. Kasembeli, Marvin X. Xu, Thomas Kristian Eckols
Abstract: Positive allosteric modulators of melanocortin receptors, especially allosteric potentiators of the receptors MC3R and MC4R are described herein. Also provided are pharmaceutical compositions containing the positive allosteric modulators and methods of treating obesity or an obesity-related disorder such as type 2 diabetes, comprising administering an effective amount of the positive allosteric modulator.
Type:
Application
Filed:
March 6, 2013
Publication date:
January 15, 2015
Inventors:
Roger D. Cone, Julien A. Sebag, Jacques Pantel, Savannah Y. Williams, David C. Weaver, Gary A. Sulikowski, Craig W. Lindsley, Padma S. Portonova, Chao Zhang
Abstract: This invention features vitamin D receptor agonists, and their use in treating bone disorders, cardiovascular disease, hyperparathyroidism, immune disorders, proliferative disease, renal disease, and thrombosis.
Type:
Application
Filed:
July 11, 2012
Publication date:
December 25, 2014
Applicant:
Beth Israel Deaconess Medical Center, In.
Inventors:
Peter Kang, Ananth Karumanchi, Santosh Khedkar, Alan Rigby, Ravi I. Thadhani
Abstract: [Problem] Provided is a compound which is useful as an agent for preventing and/or treating renal diseases. [Means for Solution] The present inventors have conducted extensive studies on compounds having a trypsin inhibitory action, and as a result, they have found that a guanidinobenzoic acid compound has a trypsin inhibitory action, thereby completing the present invention. The guanidinobenzoic acid compound of the present invention can be used as an agent for preventing and/or treating renal disease as an agent which will substitute low-protein diet therapy, and an agent for preventing and/or treating trypsin-related diseases, for example, pancreatitis, gastroesophageal reflux disease, hepatic encephalopathy, influenza, and the like.
Abstract: Compounds are provided that act as potent antagonists of the CCR(9) receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR(9). The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR(9)-mediated diseases, and as controls in assays for the identification of CCR(9) antagonists.
Type:
Grant
Filed:
February 28, 2013
Date of Patent:
December 23, 2014
Assignee:
ChemoCentryx, Inc.
Inventors:
Xi Chen, Junfa Fan, Pingchen Fan, Antoni Krasinski, Lianfa Li, Rebecca M. Lui, Jeffrey P. McMahon, Jay P. Powers, Yibin Zeng, Penglie Zhang
Abstract: A styrylquinoline derivative of structure I or IV or a benzodioxol isoquinoline of structure II or III for use in the treatment of an angiogenesis-related disease or disorder. The invention also provides a composition comprising a styrylquinoline derivative of structure I or IV or a benzodioxol isoquinoline of structure II or III for use as a medicament.
Type:
Grant
Filed:
January 16, 2012
Date of Patent:
December 23, 2014
Assignee:
University College Dublin—National University of Ireland, Dublin
Abstract: Provided are monoquaternary ammonium compounds which are modulators of nicotinic acetylcholine receptors. Also provided are methods of using the compounds for modulating the function of a nicotinic acetylcholine receptor, and for the prevention and/or treatment of central nervous system disorders, substance use and/or abuse, and gastrointestinal tract disorders.
Type:
Application
Filed:
August 27, 2014
Publication date:
December 18, 2014
Inventors:
Peter CROOKS, Linda P. DWOSKIN, Guangrong ZHENG, Sangeetha SUMITHRAN, Zhenfa ZHENG
Abstract: The present invention relates to a method of stabilising a tear film in an individual having an ocular surface inflammatory disorder by providing a compound to an ocular surface of the individual to reduce the synthesis of a cholesterol by a meibum-producing tissue.
Type:
Application
Filed:
February 1, 2013
Publication date:
December 18, 2014
Inventors:
Kenneth Gek-Jin Ooi, Stephanie Louise Watson
Abstract: The invention provides specific small molecule compounds that allosterically regulate the activity or modulate protein-protein interactions of AGC protein kinases and the Aurora family of protein kinases, methods for their production, pharmaceutical compositions comprising same, and their use for preparing medicaments for the treatment and prevention of diseases related to abnormal activities of AGC protein kinases or of protein kinases of the Aurora family.
Type:
Grant
Filed:
October 16, 2009
Date of Patent:
December 16, 2014
Assignee:
Universitaet des Saarlandes
Inventors:
Matthias Engel, Wolfgang Fröhner, Adriane Stroba, Ricardo M. Biondi
Abstract: A biodegradable, flexible covering for a breast implant is provided which comprises one or more biodegradable polymer layers dimensioned and shaped to cover at least a portion of the breast implant. The implant can be inserted into an opening of the covering immediately prior to surgery, but alternate configurations and times of insertion are contemplated as well as open or sheet type devices. The coverings can optionally contain one or more drugs for delivery at the surgical site, particularly for treating or preventing infection, pain, inflammation, capsular contracture, scarring or other complications associated with breast augmentation or breast reconstruction.
Abstract: The invention relates to metal-chelating compounds comprising one or more 8-hydroxyquinoline units substituted in position 2 with a nitrogenous group comprising a polyamino chain, wherein the polyamino chain is N-substituted on said nitrogenous group, to the composition containing same, and to the uses thereof in the therapeutic field and in particular in the treatment of diseases associated with an abnormality in the regulation of metal metabolism resulting in a metal overload in human or animal cells.
Type:
Application
Filed:
December 18, 2012
Publication date:
December 11, 2014
Inventors:
Francois Gaboriau, David Deniaud, Vincent Corce, Karine Julienne Aphecetche, Eric Renault
Abstract: The present invention is directed to compounds that modulate the bioactivity of an orexin receptor such as OX1 or OX2, or both; to pharmaceutical compositions and combinations comprising a compound of the invention; to methods of treatment of malconditions in patients wherein modulation of an orexin receptor is medically indicated; and to methods of preparation of compounds of the invention.
Type:
Application
Filed:
February 12, 2014
Publication date:
December 11, 2014
Inventors:
Theodore M. KAMENECKA, Yuanjun HE, William NGUYEN, Rong Jiang, Xinyi Song
Abstract: The present invention provides a method of determining the susceptibility of a subject to treatment with a leukotriene modifier by determining the subject's cysteinyl leukotriene (CysLT) level and the subject's level of eosinophilic airway inflammation and identifying a subject with a high ratio of CysLT levels to eosinophilic airway inflammation as susceptible to treatment with the leukotriene modifier. Also discussed is a method of treatment of subjects who are susceptible to treatment that includes administering a leukotriene modifier to such a subject.
Abstract: A method is disclosed for the in vivo treatment of a breast cancer tumor utilizing a therapeutically effective amount of an agent that inactivates the Rac1 GTPase and results in a reduction in cancer cell invasion, reduced cancer cell motility, and reduced volume and weight of the tumor. Agents that can be used in this treatment include salubrinal, guanabenz, and combinations thereof. The agents additionally have proven useful in reducing the development of osteoclastogenesis and reducing bone metastasis.
Type:
Application
Filed:
June 5, 2014
Publication date:
December 11, 2014
Applicant:
Indiana University Research and Technology Corporation
Abstract: The present invention relates to a compound of Formula (I): or a pharmaceutically acceptable salt thereof, corresponding pharmaceutical compositions, compound preparation and treatment methods directed to bacterial infections and inhibition of bacterial peptide deformylase (PDF) activity.
Inventors:
Kelly M. Aubart, Andrew B. Benowitz, Yuhong Fang, James Hoffman, Joseph M. Karpinski, Andrew Nicholson Knox, Xiangmin Liao, Donghui Qin, Dongchuan Shi, Jared T. Spletstoser
Abstract: The present invention provides a process for the synthesis of substituted phenoxymethylpropionic acid and related compounds. The compounds are useful for inhibiting the formation of AGEs (Advanced Glycation End Products).
Abstract: Provided herein are compositions and methods for the treatment and analysis of neurological disorders. In particular, provided herein are small molecules targeted to amyloid-? (A?) or metal-A? species for the treatment, diagnosis, or study of neurological conditions such as Alzheimer's disease (AD) and other diseases and conditions.
Type:
Application
Filed:
November 30, 2012
Publication date:
November 13, 2014
Inventors:
Mi Hee Lim, Katayoun Saatchi, Urs Hafeli, Joo-Yong Lee
Abstract: Provided is a method of treating or preventing age-related macular degeneration (AMD) in a patient subject to, or symptomatic of the disease, wherein the method comprises restoring normal lysosomal pH (pHL), or acidifying an abnormally elevated pHL, thus decreasing or preventing a damaging accumulation of lipofuscin or waste products in the retinal pigment epithelium (RPE) cells of the eye of the patient. Further, this method is achieved by modulating the action of the P2X7 and/or P2Y12 receptors of the RPE cells, specifically decreasing the acidity (pHL) of the RPE lysosomes by administering selected receptor antagonists affecting the action of the P2X7 and/or P2Y12 receptors of the RPE. Methods for selecting and quantifying the effectiveness of drugs to restore pHL and determine outer segment clearance rates is also provided using a high through-put screening protocol.
Abstract: This invention provides a family of compounds that inhibit Class II fructose 1,6-bisphosphate aldolase (FBA), which is implicated in the pathogenic activity of a broad range of bacterial and parasitic agents. The compounds were identified by empirical testing, and provide a basis for further derivatization and optimization of 8-hydroxyquinoline-2-carboxylic acid and related compounds. Crystal structure shows that the compounds don't bind directly to the catalytic site of the enzyme, and so are not defined simply as substrate analogs. Instead, they create a pocket by induced fit, resulting a powerful and specific inhibitory effect on FBA activity.
Type:
Application
Filed:
May 8, 2014
Publication date:
November 13, 2014
Applicants:
Colorado Seminary, Which Owns and Operates The University Of Denver, Regis University
Inventors:
Scott Dusan Pegan, Kateri Ahrendt, Glenn C. Capodagli, Bryan Cowen
Abstract: Disclosure is provided for carbamate compounds that prevent, remove and/or inhibit the formation of biofilms, compositions including these compounds, devices including these compounds, and methods of using the same.
Abstract: The present specification discloses honeybee repellents exhibiting repellent properties similar to 2-heptanone, compositions comprising such repellents, uses to repel a honeybee from a mammal, location, plant, structure treated of such repellents, and methods of treating a mammal, location, plant, structure by applying such repellents.
Type:
Application
Filed:
May 3, 2014
Publication date:
November 6, 2014
Applicant:
INSCENT, INC.
Inventors:
Daniel F. Woods, Spiros Dimitratos, Robin W. Justice
Abstract: The invention relates to N-hydroxysulfonamide derivatives that donate nitroxyl (HNO) under physiological conditions and are useful in treating and/or preventing the onset and/or development of diseases or conditions that are responsive to nitroxyl therapy, including heart failure and ischemia/reperfusion injury. Novel N-hydroxysulfonamide derivatives release NHO at a controlled rate under physiological conditions, and the rate of HNO release is modulated by varying the nature and location of functional groups on the N-hydroxysulfonamide derivatives.
Type:
Grant
Filed:
October 3, 2013
Date of Patent:
December 30, 2014
Assignees:
The Johns Hopkins University, Cardioxyl Pharmaceuticals, Inc.
Inventors:
John P. Toscano, Frederick Arthur Brookfield, Andrew D. Cohen, Stephen Martin Courtney, Lisa Marie Frost, Vincent Jacob Kalish