Chalcogen Bonded Directly To The Five-membered Hetero Ring By Nonionic Bonding Patents (Class 514/424)
-
Publication number: 20150051161Abstract: The present invention provides compositions and methods for detecting carboxymethyl-lysine (CML) and circulating receptor for advanced glycation end (RAGE) products, and methods for correlating CML and RAGE levels with age-related disease. In particular, serum CML and/or circulating receptor for advanced glycation end (RAGE) products can be used as a clinical biomarker in diagnostics to identify people who are at a higher risk of developing adverse ageing-related outcomes.Type: ApplicationFiled: April 10, 2014Publication date: February 19, 2015Applicant: THE JOHNS HOPKINS UNIVERSITYInventors: Richard David Semba, Luigi Ferruci, Edward G. Lakatta
-
Publication number: 20150037425Abstract: The present invention relates to pharmaceutical powders for inhalation produced by a method consisting of a first step of mixing particles of a force-controlling agent selected from a salt of a fatty acid with particles of one or more pharmacologically active materials and a second step of sieving or blending the powder with a carrier material.Type: ApplicationFiled: September 22, 2014Publication date: February 5, 2015Inventor: Rudi Mueller-Walz
-
Patent number: 8946446Abstract: The invention provides modulators for the orphan nuclear receptor RORy and methods for treating RORy mediated diseases by administrating these novel RORy modulators to a human or a mammal in need thereof. Specifically, the present invention provides pyrrolo sulfonamide compounds of Formula (1) and the enantiomers, diastereomers, tautomers, solvates and pharmaceutically acceptable salts thereof.Type: GrantFiled: April 13, 2012Date of Patent: February 3, 2015Assignee: Phenex Pharmaceuticals AGInventors: Christoph Steeneck, Olaf Kinzel, Christian Gege, Gerald Kleymann, Thomas Hoffmann
-
Publication number: 20150031670Abstract: Compounds of the formula (I), in which R1, R3, R5, R6, R7, R, X and Y have the meanings indicated in Claim 1, are inhibitors of methionine aminopeptidase and can be employed for the treatment of tumours.Type: ApplicationFiled: March 21, 2013Publication date: January 29, 2015Applicant: MERCK PATENT GmbHInventors: Timo Heinrich, Frank Zenke, Mireille Krier, Manja Friese-Hamim, Jeyaprakashnarayanan Seenisamy
-
Patent number: 8940776Abstract: A compound is represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof. A pharmaceutical composition comprises a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. A method of treating a subject in need thereof comprises administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. The subject has type 2 diabetes; renal hypertrophy or hyperplasia associated with diabetic nephropathy; Tay-Sachs; Gaucher's; or Fabry's disease. Methods of decreasing plasma TNF-?, lowering blood glucose levels, decreasing glycated hemoglobin levels, inhibiting glucosylceramide synthase, and lowering glycosphingolipid concentrations in a subject in need thereof respectively comprise administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof.Type: GrantFiled: August 27, 2012Date of Patent: January 27, 2015Assignee: Genzyme CorporationInventors: Craig Siegel, Cecilia M. Bastos, David J. Harris, Angeles Dios, Edward Lee, Richard Silva, Lisa M. Cuff, Mikaela Levine, Cassandra A. Celatka, Frederic Vinick, Thomas H. Jozefiak, Yibin Xiang, John Kane, Junkai Liao
-
Patent number: 8920846Abstract: A microcapsule in which a liquid droplet is coated with a resin, wherein in the droplet, a pesticidally active solid ingredient is suspended in a compound of formula (I), wherein R represents a C1-C5 alkyl group, is useful as a formulation of a pesticidally active solid ingredient.Type: GrantFiled: September 2, 2010Date of Patent: December 30, 2014Assignee: Sumitomo Chemical Company, LimitedInventors: Naoki Tsuda, Mayuko Ozawa
-
Publication number: 20140377190Abstract: Compositions, methods and systems are provided for pulmonary or nasal delivery of two or more active agents via a metered dose inhaler. In one embodiment, the compositions include a suspension medium, active agent particles, and suspending particles, in which the active agent particles and suspending particles form a co-suspension within the suspension medium.Type: ApplicationFiled: April 21, 2014Publication date: December 25, 2014Applicant: Pearl Therapeutics, Inc.Inventors: Reinhard Vehring, Michael Steven Hartman, David Lechuga-Ballesteros, Adrian Edward Smith, Vidya B. Joshi, Sarvajna Dwivedi
-
Publication number: 20140371290Abstract: Salts of glycopyrrolate, including solid forms and formulations such as topicals thereof, are disclosed. Methods of making glycopyrrolate salts, including formulations such as topicals thereof, and methods of treating hyperhidrosis with salts of glycopyrrolate, and formulations such as topicals thereof, are disclosed.Type: ApplicationFiled: August 29, 2014Publication date: December 18, 2014Applicant: DERMIRA, INC.Inventors: John Allan STATLER, Anthony Adrian SHAW, Delphine Caroline IMBERT, Jennifer Leigh NELSON, Patricia ANDRES, Lisa Lynn McQUEEN, Stephan Xander Mattheus BOERRIGTER, Jon Gordon SELBO, Mark Christopher ANDRES
-
Publication number: 20140364479Abstract: The invention concerns a method for preparing glycopyrronium chloride, and its use in pharmaceutical applications.Type: ApplicationFiled: August 27, 2014Publication date: December 11, 2014Applicant: Chiesi Farmaceutici S.p.A.Inventors: Fausto PIVETTI, Monica Bocchi, Emanuele Ferrari
-
Publication number: 20140343083Abstract: Pyrrolidine derivatives which are inhibitors of acetyl-CoA carboxylase(s) and their use in the treatment of obesity and type-2 diabetes. An exemplary compound is 2-(4-(1-[5-Chloro-6-(2-hydroxy-2-methyl-propoxy)-pyrimidin-4-yl]-(R)-pyrrolidin-3-yloxy)-phenyl)-N-cyclopropyl-propionamide.Type: ApplicationFiled: May 12, 2014Publication date: November 20, 2014Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Niklas HEINE, Martin FLECK, Bernd NOSSE, Gerald Juergen ROTH
-
Publication number: 20140341979Abstract: The present invention relates, for example, to a liposome, which can be a basic liposome, a transferrin-conjugated liposome, or a pH-sensitive liposome, which encapsulates a compound that specifically inhibits the activity of a protein prenyltransferase, such as a RabGGTase and/or a GGTase I. The liposomes can be used as anti-cancer therapeutics including as part of methods for treating cancer, in assays, and in kits.Type: ApplicationFiled: July 30, 2014Publication date: November 20, 2014Inventors: Fuyuhiko Tamanoi, Jie Lu, Kohei Yoshimura, Ohyun Kwon, Hannah Fiji, Masaru Watanabe
-
Publication number: 20140343070Abstract: A proton pump inhibitor containing a compound represented by the formula (I) wherein X and Y are the same or different and each is a bond or a spacer having 1 to 20 carbon atoms in the main chain, R1 is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group, R2, R3 and R4 are the same or different and each is a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted thienyl group, an optionally substituted benzo[b]thienyl group, an optionally substituted furyl group, an optionally substituted pyridyl group, an optionally substituted pyrazolyl group, an optionally substituted pyrimidinyl group, an acyl group, a halogen atom, a cyano group or a nitro group, R5 and R6 are the same or different and each is a hydrogen atom or an optionally substituted hydrocarbon group, which has a superior proton pump action and shows an antiulcer activity and the like after conversion to a proton pump inhibitor in the body, or a salt thereof, or a prodrug theType: ApplicationFiled: August 1, 2014Publication date: November 20, 2014Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Masahiro Kajino, Atsushi Hasuoka, Naoki Tarui, Terufumi Takagi
-
Patent number: 8889889Abstract: Crosslinked polymers, methods for their preparation and use, are described in which the crosslinked polymers are formed from at least two polymer precursors, one of which is designed, upon degradation of the crosslinked polymer, to release the second polymer precursor in its original, unmodified chemical form.Type: GrantFiled: April 15, 2013Date of Patent: November 18, 2014Assignee: Confluent Surgical, Inc.Inventors: Rachit Ohri, Phillip Blaskovich, Joshua Kennedy, Steven L. Bennett, Arthur Driscoll
-
Publication number: 20140336227Abstract: Compounds, pharmaceutical compositions of general formula (I) or (I?) or a pharmaceutically acceptable salt thereof, and methods for treating an inflammatory disorder: wherein: z is 1, 2 or 4; X is —CO—Yk—(R1)n; k is 0 or 1; Y is a cycloalkyl or polycycloalkyl, cycloalkenyl or polycycloalkenyl group; each R1 is a branched chain alkyl group; n is any integer from 1 to m, where m is the maximum number of substitutions permissible on the cyclo-group Y; and the compound comprises an amino lactam ring linked to an alkyl group —Yk—(R1)n by an amide group, wherein the carbon atom in the alkyl group at the 2-position relative to the carbon atom of the amide carbonyl is linked to each of the carbon atom of the amide carbonyl and three other carbon atoms by a single bond, and wherein the 2-position carbon atom has essentially tetrahedral bond angles.Type: ApplicationFiled: November 4, 2013Publication date: November 13, 2014Applicant: CAMBRIDGE ENTERPRISE LIMITEDInventors: David J Grainger, David John Fox
-
Patent number: 8883844Abstract: There is provided compositions and methods for the treatment of respiratory conditions such as pulmonary hypertension and sickle-cell disease in a patient in need thereof. The composition and method are for treating a patient in need thereof by inhalation of a composition containing amino acid ester compounds comprising at least one nitric oxide releasing group and pharmaceutical salts thereof.Type: GrantFiled: September 22, 2011Date of Patent: November 11, 2014Assignee: Nitrogenix Inc.Inventor: Michael Farber
-
Patent number: 8877800Abstract: The present invention concerns methods useful in treating a subject having diarrhea-predominant IBS (IBS-D) by administering N-methyl-N-[(1S)-1-phenyl-2-((3S)-3-hydroxypyrrolidin-1-yl)ethyl]-2,2-diphenylacetamide and/or a pharmaceutically acceptable salt thereof to the subject.Type: GrantFiled: November 5, 2010Date of Patent: November 4, 2014Assignee: Tioga Pharmaceuticals, Inc.Inventor: Allen Mangel
-
Patent number: 8877251Abstract: The present invention relates to methods of making a powder for inhalation comprising a first step of mixing particles of a force-controlling agent selected from the group consisting of phospholipids, titanium dioxide, aluminum dioxide, silicon dioxide, starch, and salts of fatty acids, with particles of one or more pharmacologically active materials, wherein the mixing is achieved by one or more of the processes of sieving, mixing or blending, and wherein the mixing results in the particles of the force-controlling agent being disposed on the surface of the particles of the one or more pharmacologically active materials as either a particulate coating or as a continuous or discontinuous film.Type: GrantFiled: September 5, 2012Date of Patent: November 4, 2014Assignee: Jagotec AGInventor: Rudi Mueller-Walz
-
Publication number: 20140323424Abstract: Described herein are assays, kits and methods for treating mood disorders by testing for one or more polymorphisms in a specific group of genes and for analyzing the results of polymorphism testing; the genes included may converge in one or more signaling pathways, and may be epigenetic. The genes are included based on the relationships of the proteins encoded by the genes in the context of particular signaling pathways and provide a diagnostically relevant nexus. Also described herein are methods of presenting the data collected by the screen, including methods of delivering interpretive comments and/or treatment guidance based on the results of the genetic screening either individually or based on the genetic composition of particular clusters of genes which may be related to each other. Importantly, drugs which modulate these genetic disturbances are described for targeted therapeutic use based upon companion diagnostic method.Type: ApplicationFiled: July 7, 2014Publication date: October 30, 2014Inventor: Jay L. LOMBARD
-
Publication number: 20140323519Abstract: This invention relates to novel heterocyclic compounds that are useful for treating cancer and other cellular proliferative diseases and/or disorders associated with B-Raf activity. The compounds of the invention may be illustrated by the Formula (I).Type: ApplicationFiled: April 20, 2012Publication date: October 30, 2014Applicant: MERCK SHARP & DOHME CORP.Inventors: M. Arshad Siddiqui, Lianyun Zhao, Amit K. Mandal
-
Publication number: 20140315972Abstract: The invention relates to a compound (RS)-2-(2-oxo-4-phenylpyrrolidin-1-yl)acetamide having modulatory activity with a commensurate effect, to a pharmaceutical substance (RS)-2-(2-oxo-4-phenylpyrrolidin-1-yl)acetamide containing: 2-(2-oxo-4-phenylpyrrolidin-1-yl)acetamide—no less than 99.0% and no more than 100.5% on dry basis, individual related impurities individually or in total—no more than 0.2%; residual amounts of organic solvents individually or in total—no more than 3000 ppm. The invention also relates to a method for producing the pharmaceutical substance differing in that the obtained raw materials are subjected to purification, crystallization and stabilization of the compound by processing it with demineralized (distilled) water, and the isothermal crystallization from propanol followed by drying. The invention also relates to compositions for internal and external application. The invention provides higher efficacy, safety, stability and width of therapeutic application.Type: ApplicationFiled: September 20, 2012Publication date: October 23, 2014Inventors: Valentina Ivanovna Akhapkina, Roman Vitalyevich Akhapkin
-
Publication number: 20140315905Abstract: Novel substituted benzamide based inhibitors, their use in therapy, pharmaceutical compositions comprising the compounds, the use of said compounds in the manufacture of medicaments, and therapeutic methods comprising the administration of said compounds are described. The present compounds modulate the activity of 11?-hydroxysteroid dehydrogenase type 1 (11?HSD1) and are accordingly useful in the treatment of diseases in which such a modulation is beneficial, such as the metabolic syndrome.Type: ApplicationFiled: July 2, 2014Publication date: October 23, 2014Inventor: Soren Ebdrup
-
Publication number: 20140314685Abstract: Ion channel modulating compounds are disclosed. The compounds of the present invention may be incorporated in compositions and kits. The present invention also discloses a variety of in vitro and in vivo uses for the compounds and compositions, including the treatment of arrhythmia and the production of analgesia and local anesthesia.Type: ApplicationFiled: November 15, 2013Publication date: October 23, 2014Applicant: Cardiome Pharma Corp.Inventors: Gregory N. Beatch, Bertrand M.C. Plouvier, Tao Sheng, Michael J.A. Walker, Richard A. Wall, Sandro L. Yong, Jeff Jiqun Zhu, Alexander B. Zolotoy
-
Publication number: 20140308214Abstract: The present invention relates to pharmaceutical compositions for inhalation comprising glycopyrrolate, a beta2-agonist, and optionally an inhaled corticosteroid; to a process for preparing such compositions and to the use of such compositions for the prevention and/or treatment of respiratory, inflammatory or obstructive airway disease.Type: ApplicationFiled: February 17, 2012Publication date: October 16, 2014Applicant: CIPLA LIMITEDInventors: Geena Malhotra, Shrinivas Madhukar Purandare
-
Patent number: 8859590Abstract: Inhibitors of BACE1 and compositions containing them are described. Use of the inhibitors and compositions containing them to treat Alzheimer's disease are described.Type: GrantFiled: December 4, 2009Date of Patent: October 14, 2014Assignee: Purdue Research FoundationInventor: Arun K. Ghosh
-
Patent number: 8859610Abstract: Salts of glycopyrrolate, including solid forms thereof are herein disclosed. Methods of making glycopyrrolate salts and methods of treating hyperhidrosis with salts of glycopyrrolate are disclosed.Type: GrantFiled: September 11, 2013Date of Patent: October 14, 2014Assignee: Dermira, Inc.Inventors: John Allan Statler, Anthony Adrian Shaw, Delphine Caroline Imbert, Jennifer Leigh Nelson, Patricia Andres, Lisa Lynn McQueen, Stephan Xander Mattheus Boerrigter
-
Publication number: 20140303101Abstract: This invention pertains to dental care compositions with antimicrobial benefits. In particular, the invention provides for compositions of oral tissue-adherent salts that release biocidal ions on a controlled release basis and thereby provide and maintain an essentially uniform concentration of biocidal ions above the MBC or MIC of the target bacteria at the site of application in the mouth for an extended period of time. The compositions are useful for treating or preventing oral diseases resulting from bacteria, fungal or yeast infections, such as caries, gingivitis, periodontal disease and candidiasis.Type: ApplicationFiled: June 25, 2014Publication date: October 9, 2014Inventors: Anthony Errol Winston, Richard F. Stockel, Anthony Joseph Sawyer
-
Publication number: 20140296317Abstract: The invention relates to the 5S,4R-enantiomer of 2-(5-methyl-2-oxo-4-phenyl-pyrrolidin-1-yl)-acetamide with cognition enhancing activity of high pharmacological value and to its preparation method which includes the synthesis of 5S-methyl-4R-phenylpyrrolidin-2-one, its N-alkylation with ethyl haloacetate and the treatment of intermediate ethyl 2-(5S-methyl-2-oxo-4R-phenyl-pyrrolidin-1-yl)-acetate with ammonia.Type: ApplicationFiled: June 16, 2014Publication date: October 2, 2014Inventors: Ivars KALVINS, Antons LEBEDEVS, Aleksandrs CERNOBROVIJS, Maija DAMBROVA, Liga ZVEJNIECE, Maksims VORONA, Grigorijs VEINBERGS
-
Patent number: 8846742Abstract: The present invention relates to compounds that may be used to inhibit activation of protein kinase G (“PKG”). It is based, at least in part, on the discovery of the tertiary structure of PKG and the identification of molecules that either bind to the active site of PKG and/or are analogs of balanol.Type: GrantFiled: February 14, 2007Date of Patent: September 30, 2014Assignee: The Trustees of Columbia University in the City of New YorkInventors: Richard Ambron, Ying-Ju Sung, Jeremy Greenwood, Leah Frye, Shi-Xian Deng, Yuli Xie, Donald W. Landry
-
Patent number: 8840923Abstract: Slow-release excipients which comprise an association of at least one glycogen and at least one alginate with an alkaline-earth metal salt are useful for the preparation of slow-release pharmaceutical formulations.Type: GrantFiled: December 23, 2008Date of Patent: September 23, 2014Assignee: Aziende Chimiche Riunite Angelini Francesco A.C.R.A.F. S.p.A.Inventors: Vincenzo Russo, Elisa Liberati, Nicola Cazzolla, Leonardo Marchitto, Lorella Ragni
-
Publication number: 20140271862Abstract: A high dose rapidly dispersing three-dimensionally printed dosage form comprising a high dose of levetiracetam in a porous matrix that disperses in water within a period of less than about 10 seconds is disclosed. Also disclosed are methods of preparing the dosage form and of treating a condition, disease or disorder that is therapeutically responsive to levetiracetam.Type: ApplicationFiled: May 15, 2014Publication date: September 18, 2014Applicant: APRECIA PHARMACEUTICALS COMPANYInventors: Jules JACOB, Norman COYLE, Thomas G. WEST, Donald C. MONKHOUSE, Henry L. SURPRENANT, Nemichand B. JAIN
-
Publication number: 20140275087Abstract: The present invention relates to pyrrolidine derivatives of the formula (I), or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such pyrrolidine derivatives, and the use of such pyrrolidine derivatives for therapeutic purposes. The pyrrolidine derivatives are GlyT1 inhibitors.Type: ApplicationFiled: March 17, 2014Publication date: September 18, 2014Inventors: Wilhelm Amberg, Frauke Pohlki, Udo Lange, Ying X. Wang, Hongyu H. Zhao, Huan-Qiu Li, Jason T. Brewer, Irini Zanze, Justin Dietrich, Anil Vasudevan, Stevan W. Djuric, Yanbin Lao, Charles W. Hutchins
-
Publication number: 20140275037Abstract: Compounds, methods and pharmaceutical compositions for treating viral infections, by administering certain novel semicarbazides, sulfonyl carbazides, ureas and related compounds in therapeutically effective amounts are disclosed. Methods for preparing the compounds and methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment and prophylaxis of viral infections such as caused by hemorrhagic fever viruses is disclosed, i.e., including but not limited to Arenaviridae (Junin, Machupo, Guanavito, Sabia and Lassa), Filoviridae (ebola and Marburg viruses), Flaviviridae (yellow fever, omsk hemorrhagic fever and Kyasanur Forest disease viruses), and Bunyaviridae (Rift Valley fever).Type: ApplicationFiled: December 19, 2013Publication date: September 18, 2014Applicant: Siga Technologies, Inc.Inventors: Yijun Deng, Theodore J. Nitz, Thomas R. Bailey, Yanming Zhang, Sylvie Laquerre
-
Publication number: 20140275204Abstract: A method of treating hyperhidrosis in a mammalian subject comprising: a) providing a composition comprising a pharmaceutically acceptable vehicle and from about 1.0% to about 25% of a compound having the formula: and b) topically administering the composition to skin of an area of a mammalian subject suffering from hyperhidosis, before bedtime, such that, compared to untreated, baseline conditions, sweat production is reduced by at least about 25% for at least about six (6) hours.Type: ApplicationFiled: March 14, 2014Publication date: September 18, 2014Applicant: BODOR LABORATORIES, INC.Inventors: NICHOLAS S. BODOR, DAVID ANGULO
-
Publication number: 20140275086Abstract: The present invention relates to pyrrolidine derivatives of the formula (I), or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such pyrrolidine derivatives, and the use of such pyrrolidine derivatives for therapeutic purposes. The pyrrolidine derivatives are GlyT1 inhibitors.Type: ApplicationFiled: March 17, 2014Publication date: September 18, 2014Inventors: Wilhelm Amberg, Frauke Pohlki, Udo Lange, Ying X. Wang, Hongyu H. Zhao, Huan-Qiu Li, Jason T. Brewer, Irini Zanze, Justin Dietrich, Anil Vasudevan, Stevan W. Djuric, Yanbin Lao, Charles W. Hutchins
-
Publication number: 20140256702Abstract: In one aspect, the invention relates to compounds having the formula: where R1-R5 and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.Type: ApplicationFiled: March 4, 2014Publication date: September 11, 2014Applicant: THERAVANCE, INC.Inventors: Erik Fenster, Melissa Fleury, Adam D. Hughes
-
Publication number: 20140255491Abstract: Inhalation solutions for administration of muscarinic antagonists for the treatment of breathing disorders, such as COPD, are provided.Type: ApplicationFiled: March 11, 2014Publication date: September 11, 2014Applicant: SUNOVION RESPIRATORY DEVELOPMENT INC.Inventor: William GERHART
-
Patent number: 8829041Abstract: Compounds of formula (I) are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Also disclosed are pharmaceutical compositions comprising the histamine-3 receptor ligands, methods for using such compounds and compositions, and a process for preparing compounds within the scope of formula (I).Type: GrantFiled: June 22, 2007Date of Patent: September 9, 2014Assignee: AbbVie Inc.Inventors: Huaqing Liu, Lawrence A. Black, Youssef L. Bennani, Marlon D. Cowart
-
Patent number: 8822692Abstract: The present invention relates to new diterpenoid derivatives of formula (I), processes for their preparation, and to pharmaceutical compositions containing them for the treatment of cardiovascular disorders, urinary incontinence, asthma, or Alzheimer's disease and/or to prevent obstructive vascular lesions consequently to arteriotomy and/or angioplasty, and to prevent organ damage in hypertensive patients.Type: GrantFiled: July 26, 2013Date of Patent: September 2, 2014Assignee: Sigma-Tau Industrie Farmaceutiche Riunite, S.p.A.Inventors: Alberto Cerri, Mauro Gobbini, Marco Torri, Patrizia Ferrari, Mara Ferrandi, Giuseppe Bianchi
-
Patent number: 8822496Abstract: The present invention relates to therapeutic combinations comprising (a) Compound (1), or a pharmaceutically acceptable salt thereof, as herein described, (b) an interferon alfa and (c) ribavirin and particular regimens for administering this combination. Compound (1) is a selective and potent inhibitor of the HCV NS3 serine protease. The present invention also relates to methods of using such therapeutic combinations for treating HCV infection or alleviating one or more symptoms thereof in a patient.Type: GrantFiled: October 27, 2010Date of Patent: September 2, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Carla Haefner, Gerhard Steinmann, Jerry O. Stern, Chan-Loi Yong
-
Publication number: 20140243341Abstract: Antiviral protease inhibitors, including peptidyl aldehydes, peptidyl ?-ketoamides, peptidyl bisulfite salts, and peptidyl heterocycles, are disclosed, along with related antiviral compounds, and methods of using the same to treat or prevent viral infection and disease. The compounds possess broad-spectrum activity against viruses that belong to the picornavirus-like supercluster, which include important human and animal pathogens including noroviruses, enteroviruses, poliovirus, foot-and-mouth disease virus, hepatitis A virus, human rhinovirus (cause of common cold), human coronavirus (another cause of common cold), transmissible gastroenteritis virus, murine hepatitis virus, feline infectious peritonitis virus, and severe acute respiratory syndrome coronavirus.Type: ApplicationFiled: September 27, 2012Publication date: August 28, 2014Inventors: Kyeong-Ok Chang, Yunjeong Kim, William C. Groutas, Duy Hua, Linda J. Saif
-
Publication number: 20140243396Abstract: Imidazoquinolines, as set forth in formula (I), are useful for inhibiting growth or proliferation of mucoepidermoid carcinoma cells. The therapeutic and prophylactic treatments provided by this invention are practiced by administering to a patient in need thereof an amount of a compound of formula (I) that is effective to inhibit growth or proliferation of the mucoepidermoid carcinoma cells.Type: ApplicationFiled: September 27, 2012Publication date: August 28, 2014Inventors: James D. Griffin, Lizi Wu, Jie Chen
-
Publication number: 20140242122Abstract: Salts of glycopyrrolate, including solid forms thereof are herein disclosed. Methods of making glycopyrrolate salts and methods of treating hyperhidrosis with salts of glycopyrrolate are disclosed.Type: ApplicationFiled: September 11, 2013Publication date: August 28, 2014Applicant: Dermira, Inc.Inventors: John Allan STATLER, Anthony Adrian SHAW, Delphine Caroline IMBERT, Jennifer Leigh NELSON, Patricia ANDRES, Lisa Lynn McQUEEN, Stephan Xander Mattheus BOERRIGTER
-
Patent number: 8815935Abstract: The present invention is directed to novel compounds. These compounds can be useful in inhibiting the activity of protein prenyltransferases including GGTase I and/or RabGGTase. The compounds can also be used as anti-cancer therapeutics including as part of methods for treating cancer, in assays, and in kits.Type: GrantFiled: September 13, 2012Date of Patent: August 26, 2014Assignee: The Regents of the University of CaliforniaInventors: Ohyun Kwon, Fuyuhiko Tamanoi, Hannah Fiji, Masaru Watanabe
-
Publication number: 20140236226Abstract: The present invention relates to shape memory polymers (SMP) and especially to shape memory polymer containing a water soluble non-reactive plasticiser and to uses thereof.Type: ApplicationFiled: October 5, 2012Publication date: August 21, 2014Applicants: Smith & Nephew PLC, University of BradfordInventors: Malcolm Brown, Horacio Montes de Oca Balderas, Michael Andrew Hall, Phillip Caton-Rose, Phillip David Coates, Glen Thompson
-
Patent number: 8809283Abstract: The invention relates to methods and compositions for inhibiting proteasome activity using cinnamate compounds. These cinnamate compounds can be formulated for topical or systemic use for skin disorders such as psoriasis.Type: GrantFiled: May 19, 2006Date of Patent: August 19, 2014Assignee: Natuderm, LLCInventor: Jack Arbiser
-
Publication number: 20140228330Abstract: This invention provides a pharmaceutical composition comprising a eutectic composition of two pharmacologically active ingredients for delivery to the lung by inhalation. This invention also provides a pharmaceutical composition comprising a eutectic composition of two pharmacologically active ingredients for the treatment of respiratory disease.Type: ApplicationFiled: August 8, 2012Publication date: August 14, 2014Inventors: Graham Ruecroft, Dipesh Parikh
-
Patent number: 8802719Abstract: Methods of preparing (+)-1,4-dihydro-7-[(3S,4S)-3-methoxy-4-(methylamino)-1-pyrrolidinyl]-4-oxo-1-(2-thiazolyl)-1,8-naphthyridine-3-carboxylic acid are disclosed. Also provided are pharmaceutical compositions comprising (+)-1,4-dihydro-7-[(3S,4S)-3-methoxy-4-(methylamino)-1-pyrrolidinyl]-4-oxo-1-(2-thiazolyl)-1,8-naphthyridine-3-carboxylic acid, and methods of treatment using such compositions.Type: GrantFiled: July 11, 2013Date of Patent: August 12, 2014Assignee: Sunesis Pharmaceuticals, Inc.Inventors: Anantha Sudhakar, Tamilarasan Subramani, Mohamed Shiek Mohamed Mujeebur Rahuman, Ramar Subbiah
-
Publication number: 20140221330Abstract: An objective of the present invention is to provide a novel NDM (New Delhi metallo-?-lactamase) inhibitor that functions as a drug for restoring the antibacterial activity of ?-lactam antibiotics that have been inactivated as a result of decomposition by NDM.Type: ApplicationFiled: July 26, 2012Publication date: August 7, 2014Inventors: Akihiro Morinaka, Kazunori Maebashi, Takashi Ida, Muneo Hikida, Mototsugu Yamada, Takao Abe
-
Publication number: 20140221383Abstract: Compounds having the structures of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis: In the compounds of Formula I, B or R2 is a phenyl group which has an ortho aryl, heterocyclic, benzoheterocyclic or benzocycloalkyl substituent, and one other position on the 5-membered ring has an aromatic, heterocyclic, cycloalkyl, benzoheterocyclic or benzocycloalkyl substituent connected directly to the ring or attached to the ring through a —CH2—.Type: ApplicationFiled: April 14, 2014Publication date: August 7, 2014Applicant: Merck Sharp & Dohme Corp.Inventors: Amjad Ali, Joann M. Napolitano, Qiaolin Deng, Zhijian Lu, Peter J. Sinclair, Gayle E. Hallet, Christopher F. Thompson, Nazia Quraishi, Cameron J. Smith, Julianne A. Hunt, Adrian A. Dowst, Yi-Heng Chen, Hong Li
-
Publication number: 20140219995Abstract: Organic compounds showing the ability to inhibit effector toxin secretion or translocation mediated by bacterial type III secretion systems are disclosed. The disclosed type III secretion system inhibitor compounds are useful for combating infections by Gram-negative bacteria such as Salmonella spp., Shigella flexneri, Pseudomonas spp., Yersinia spp., enteropathogenic and enteroinvasive Escherichia coli, and Chlamydia spp. having such type III secretion systems.Type: ApplicationFiled: July 13, 2012Publication date: August 7, 2014Applicant: MICROBIOTIX, INC.Inventors: Donald T. Moir, Daniel Aiello, Norton P. Peet, John D. Williams, Matthew Torhan