The Hetero Ring Is Five-membered Patents (Class 514/158)
  • Patent number: 10568895
    Abstract: This document provides methods and materials involved in treating cardiovascular conditions such as calcific aortic valve stenosis. For example, methods and materials for using sGC agonists or a combination of sGC agonists and PDE5A inhibitors to reduce calcification of heart valves and/or vessels or to slow progression of aortic sclerosis to calcific aortic valve stenosis are provided.
    Type: Grant
    Filed: February 7, 2019
    Date of Patent: February 25, 2020
    Assignee: Mayo Foundation for Medical Education and Research
    Inventors: Jordan D. Miller, Bin Zhang
  • Patent number: 10471045
    Abstract: Provided herein are compounds, derivatives thereof, composition comprising one or more of said compounds and derivatives, and methods for prevention and/or treatment of microbial infections and/or related diseases or conditions. The present compounds and/or derivatives thereof can be represented by Formula (I): The present methods include administering to a subject an effective amount of one or more compounds of Formula (I). In one embodiment, said microbial infections are bacterial infections. More specifically, said bacterial infections are staphylococcal infections.
    Type: Grant
    Filed: July 22, 2018
    Date of Patent: November 12, 2019
    Assignee: The University of Hong Kong
    Inventors: Yi Tsun Richard Kao, Peng Gao, Xuechen Li, Ming Liu
  • Patent number: 10413552
    Abstract: A method of treating a medulloblastoma in a mammal is provided comprising administering to the mammal a compound having the following general formula (1): wherein X is selected from the group consisting of hydrogen, hydroxyl (—OH), halogen, thio (—SH), sulfanyl (—SR), sulfinyl (—SOR), sulfonyl (—SO2R), carboxyl (—COOH), carbonyl (COOR), nitro (—NO2), nitroso (—NOR), amino (NH2), NHR, NRR1, cyano (—CN) and isocyano (—NC), wherein R and R1 are independently C1-C5 branched or unbranched lower alkyl; and Y is a 5- or 6-membered unsaturated ring, optionally substituted, or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: June 17, 2016
    Date of Patent: September 17, 2019
    Assignee: The Hospital for Sick Children
    Inventors: James Rutka, Claudia Faria
  • Patent number: 10238669
    Abstract: This document provides methods and materials involved in treating cardiovascular conditions such as calcific aortic valve stenosis. For example, methods and materials for using sGC agonists or a combination of sGC agonists and PDE5A inhibitors to reduce calcification of heart valves and/or vessels or to slow progression of aortic sclerosis to calcific aortic valve stenosis are provided.
    Type: Grant
    Filed: September 12, 2017
    Date of Patent: March 26, 2019
    Assignee: Mayo Foundation for Medical Education and Research
    Inventors: Jordan D. Miller, Bin Zhang
  • Patent number: 10214538
    Abstract: The present invention provides a process for the preparation of darunavir or solvates or a pharmaceutically acceptable salt thereof substantially free of bisfuranyl impurities, particularly darunavir propionate solvate. The present invention also provides a process for preparation amorphous darunavir using the darunavir propionate solvate.
    Type: Grant
    Filed: July 15, 2016
    Date of Patent: February 26, 2019
    Assignee: Laurus Labs Ltd.
    Inventors: Kameswar R. Chivukula, Venkata R. Murthy, Venkata S. Indukuri, Seeta R. Gorantla
  • Patent number: 10179142
    Abstract: T-lymphocyte invasion and metastases (Tiam-1) has been identified as a marker and anti-cancer drug target for therapy of metastatic bone cancer in individuals afflicted with prostate cancer. The present disclosure provides methods and compounds for inhibiting metastases by disrupting Tiam-1 expression and activity. One particularly preferred compound comprises a disulfomanide of the formula.
    Type: Grant
    Filed: September 4, 2014
    Date of Patent: January 15, 2019
    Assignee: THE ARIZONA BOARD OF REGENTS ON BEHALF OF THE UNIVERSITY OF ARIZONA
    Inventors: Emmanuelle Meuillet, Sylvestor Moses, Shuxing Zhang
  • Patent number: 10016379
    Abstract: A method of treatment for third spacing is provided. The method includes identifying an adverse factor, which includes conditions causing an increase in vascular permeability resulting in third spacing. The method also includes diagnosing the patient with third spacing, which can include third spacing of fluids, materials, or both. The patient is treated with a therapeutically effective amount of a non-increased vascular permeability modifier loop diuretic, such as a non-sulfonamide loop diuretic like ethacrynic acid or ethacrynate sodium.
    Type: Grant
    Filed: March 10, 2016
    Date of Patent: July 10, 2018
    Inventor: Robin L. Webb
  • Patent number: 9540351
    Abstract: Provided herein are pharmaceutically acceptable salts of 3,5-diaminopyrazoles, for example, pharmaceutically acceptable salts of compounds of Formula IA, that are useful for modulating regulated-in-COPD kinase activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a RC kinase-mediated disorder, disease, or condition.
    Type: Grant
    Filed: September 17, 2014
    Date of Patent: January 10, 2017
    Assignee: Axikin Pharmaceuticals, Inc.
    Inventors: Tai Wei Ly, Erik Dean Raaum
  • Patent number: 9234178
    Abstract: The present invention provides a method for increasing the expression of MAFA in cells expressing markers characteristic of the pancreatic endocrine lineage comprising the steps of culturing the cells expressing markers characteristic of the pancreatic endocrine lineage in medium comprising a sufficient amount of a cyclin-dependant kinase inhibitor to cause an increase in expression of MAFA.
    Type: Grant
    Filed: October 23, 2009
    Date of Patent: January 12, 2016
    Assignee: Janssen Biotech, Inc.
    Inventors: Alireza Rezania, Benjamin Fryer
  • Publication number: 20150148318
    Abstract: A method of inhibiting the growth of cancer cells is disclosed in which cancer cells that contain an enhanced amount relative to non-cancerous cells of one or more of phosphorylated mTOR, Akt1, ERK2 and serine2152-phosphorylated filamin A are contacted with an FLNA-binding effective amount of a compound or a pharmaceutically acceptable salt thereof that binds to the pentapeptide of filamin A (FLNA) of SEQ ID NO: 1 and exhibits at least about 60 percent of the FITC-labeled naloxone binding amount when present at a 10 ?M concentration and using unlabeled naloxone as the control inhibitor at the same concentration. A compound that binds to the FLNA pentapeptide preferably also contains at least four of the six pharmacophores of FIGS. 19-24.
    Type: Application
    Filed: September 26, 2014
    Publication date: May 28, 2015
    Inventors: Hoau-Yan Wang, Lindsay Burns Barbier
  • Publication number: 20150141383
    Abstract: There is disclosed crystalline darunavir hydrate substantially free of any non-aqueous solvent.
    Type: Application
    Filed: January 30, 2015
    Publication date: May 21, 2015
    Inventors: Manjinder Singh PHULL, Dharmaraj Ramachandra RAO, Rajendra Narayanrao KANKAN
  • Publication number: 20150141382
    Abstract: The present invention relates to novel solvates of Darunavir of Formula I.
    Type: Application
    Filed: January 11, 2013
    Publication date: May 21, 2015
    Inventors: Anand Gopalkrishna Kamat, Naga Trinadhachari Ganala, Venkata Balaji Boddu, Joseph Prabahar Koilpillai, Sivakumaran Meenaakshisunderam
  • Publication number: 20150105351
    Abstract: The present invention is directed to novel nanomolar and picomolar inhibitors of HIV reverse transcriptase, pharmaceutical compositions therefrom and methods for inhibiting reverse transcriptase and treating HIV infections, especially included drug resistant strains of HIV-1 and HIV-2 and/or secondary disease states and/or conditions which occur as a consequence of HIV infection.
    Type: Application
    Filed: October 8, 2014
    Publication date: April 16, 2015
    Inventors: William L. Jorgensen, Karen S. Anderson
  • Publication number: 20150094284
    Abstract: A series of S-triazolyl ?-mercaptoacetanilides having general structure (1) are provided, where Q is CO2H, CONR2, SO3H, or SO2NR2. The compounds inhibit several variants of the reverse transcriptase of HIV, and are useful in the treatment of HIV infections.
    Type: Application
    Filed: December 3, 2014
    Publication date: April 2, 2015
    Inventors: Jean-Luc GIRARDET, Yung-Hyo KOH, Martha DE LA ROSA, Esmir GUNIC, Zhi HONG, Stanley LANG, Woo-Hong KIM
  • Publication number: 20150079155
    Abstract: This invention concerns a liposome comprising lipids and at least one active ingredient, wherein at least one of the lipids is a cationic lipid; said liposome exhibiting a net positive charge at physiological conditions at which said liposome preferentially adheres to monocytes in freshly drawn blood when compared to adherence to granulocytes, T-lymphocytes, B-lymphocytes and/or NK cells in freshly drawn blood, to a lipid-based pharmaceutical composition comprising said liposomes and their use in monocytic associated prophylaxis, treatment or amelioration of a condition such as cancer, an infectious disease, an inflammatory disease, an autoimmune disease or allergy.
    Type: Application
    Filed: March 14, 2013
    Publication date: March 19, 2015
    Inventors: Simon Skjøde Jensen, Thomas Lars Andresen, Jonas Rosager Henriksen, Pia Thermann Johansen
  • Publication number: 20150072958
    Abstract: Various embodiments of the present invention relate to, among other things, compounds and methods of using those compounds to treat an HIV infection. The compounds of the various embodiments of the present invention provide, among other things, therapeutic agents having enhanced penetration capability across the blood-brain barrier, such that they can enter the CNS to treat an HIV-1 infection in the CNS.
    Type: Application
    Filed: September 10, 2014
    Publication date: March 12, 2015
    Inventors: Arun K. Ghosh, Hiroaki Mitsuya, Sofiya Yashchuk
  • Publication number: 20150072959
    Abstract: Substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed.
    Type: Application
    Filed: November 13, 2014
    Publication date: March 12, 2015
    Inventors: Dane Goff, Jing Zhang, Catherine Sylvain, Rajinder Singh, Sacha Holland, Jiaxin Yu, Thilo J. Heckrodt, Pingyu Ding
  • Publication number: 20150065431
    Abstract: The present invention provides methods of reducing cutaneous scar formation by treating a cutaneous wound with a composition comprising a therapeutic agent that is a sodium channel blocker and/or an inhibitor of the Nax/SCN7A pathway. The present invention also provides wound cover components impregnated with such compositions, kits composed of such compositions with a wound dressing or sterile wipe, and mixtures of such compositions with a topical component (e.g., cream, ointment, or gel) suitable for application to a cutaneous wound. The present invention also provides compositions, kits, devices, and methods for treating skin conditions (e.g., dermatitis, psoriasis, or other skin conditions) with such compositions and devices. Examples of such therapeutic agents include, but are not limited to, an inhibitor of a gene or protein selected from: ENac, COX-2, PGE2, PI3K, PKB, Nax Prss8, IL-1?, IL-8, SAPK, Erk gene, p38 gene, PAR2, S100A8, S100A9, S100A12.
    Type: Application
    Filed: August 27, 2014
    Publication date: March 5, 2015
    Inventors: Wei Xu, Seok Jong Hong, Robert D. Galiano, Thomas A. Mustoe
  • Publication number: 20150056300
    Abstract: The present disclosure generally relates to therapeutic nanoparticles. Exemplary nanoparticles disclosed herein may include about 0.1 to about 40 weight percent of a therapeutic agent and about 10 to about 90 weight percent a diblock poly(lactic) acid-poly(ethylene)glycol copolymer or a diblock poly(lactic)-co-poly(glycolic) acid-poly(ethylene)glycol copolymer, wherein the diblock poly(lactic) acid-poly(ethylene)glycol copolymer comprises poly(lactic) acid having a number average molecule weight of about 30 kDa to about 90 kDa or the diblock poly(lactic)-co-poly(glycolic) acid-poly(ethylene)glycol copolymer comprises poly(lactic)-co-poly(glycolic) acid having a number average molecule weight of about 30 kDa to about 90 kDa.
    Type: Application
    Filed: October 24, 2011
    Publication date: February 26, 2015
    Applicant: BIND Therapeutics, Inc.
    Inventors: David Dewitt, Maria Figueiredo, Hong Wang, Greg Troiano, Young-Ho Song
  • Publication number: 20150051177
    Abstract: Provided herein are novel compounds, pharmaceutical compositions for use, inter alia, in methods of reducing Wnt-mediated effects and treating cancer.
    Type: Application
    Filed: October 31, 2014
    Publication date: February 19, 2015
    Inventor: Darren Orton
  • Publication number: 20150018293
    Abstract: Compositions and methods for the treatment and control of various conditions in an animal which comprises administering to said animal an effective amount of a immediate release composition of about 0.5% to 50% wt/wt of active ingredient together with excipients to a total of about 100%, wherein said composition dissolves in a relatively short period of time, e.g., 75 seconds or less, 5 seconds or less, or 3 seconds or less, upon administration to said animal.
    Type: Application
    Filed: May 12, 2014
    Publication date: January 15, 2015
    Applicant: NEWMARKET PHARMACEUTICALS LLC
    Inventors: David ROCK, Mark RIDALL
  • Publication number: 20150011514
    Abstract: Pharmaceutical compositions are provided comprising one or more orally deliverable dose units, each comprising particulate celecoxib in an amount of about 10 mg to about 1000 mg in intimate mixture with one or more pharmaceutically acceptable excipients. The compositions are useful in treatment or prophylaxis of cyclooxygenase-2 mediated conditions and disorders.
    Type: Application
    Filed: September 23, 2014
    Publication date: January 8, 2015
    Inventors: Danchen Gao, Anthony J. Hlinak, Ahmad M. Mazhary, James E. Truelove, Margaret B. Vaughn
  • Publication number: 20150004239
    Abstract: The invention provides solid particles comprising: a) a solid core that comprises an active pharmaceutical agent and b) a coating of Compound 2: (2) or a pharmaceutically acceptable salt of thereof on the core, as well as compositions comprising such particles, and methods for treating diseases (e.g. HIV infection) with such particles.
    Type: Application
    Filed: January 11, 2013
    Publication date: January 1, 2015
    Inventors: Aaron J. Cullen, Richard Hung Chiu Yu
  • Patent number: 8921344
    Abstract: A method of increasing the bioavailability of 5-aminosalicylate compound by administration of an oral dosage form with food is provided, as well as an article of manufacture comprising an oral dosage form of 5-aminosalicylate compound in a suitable container and associated with printed labeling which describes the increased bioavailability of the medication in the container when taken with food.
    Type: Grant
    Filed: November 3, 2006
    Date of Patent: December 30, 2014
    Assignee: Salix Pharmaceuticals, Inc.
    Inventor: Lorin Johnson
  • Publication number: 20140357601
    Abstract: The present invention relates to methods of treating fibromyalgia, by administering a therapeutically-effective combination of an antiviral component and a COX-2 inhibitor component. The invention is further related to pharmaceutical compositions comprising a combination of a therapeutically-effective amount of the antiviral compound famciclovir and a therapeutically-effective amount of the COX-2 inhibitor celecoxib. The invention is also related to methods of treating functional somatic syndromes by administering a therapeutically-effective combination of famciclovir and celecoxib.
    Type: Application
    Filed: August 14, 2014
    Publication date: December 4, 2014
    Inventor: William L. Pridgen
  • Publication number: 20140357600
    Abstract: Described herein are compositions (e.g., a pharmaceutical composition) and methods for controlling the delivery of a therapeutic agent, and their use in the treatment and/or prevention of diseases and disorders.
    Type: Application
    Filed: June 6, 2014
    Publication date: December 4, 2014
    Applicant: CHEMIC LABORATORIES INC.
    Inventors: Joseph P. St. Laurent, Scott A. Goodrich, Gerald S. Jones, Jr.
  • Patent number: 8900565
    Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which inhibit the activity of histone deacetylase 8 (HDAC8). Also described herein are methods of using such HDAC8 inhibitors, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of HDAC8 activity.
    Type: Grant
    Filed: November 21, 2012
    Date of Patent: December 2, 2014
    Assignee: Pharmacyclics, Inc.
    Inventors: Joseph J. Buggy, Sriram Balasubramanian, Erik Verner, Vincent W. F. Tai, Chang-Sun Lee
  • Patent number: 8901108
    Abstract: This invention concerns arylsulfonyl pyrazoline carboxamidine derivatives as antagonists of 5-ht6 receptors, to methods for the preparation of these compounds and to novel intermediates useful for their synthesis.
    Type: Grant
    Filed: September 11, 2013
    Date of Patent: December 2, 2014
    Assignee: AbbVie Bahamas Limited
    Inventors: Arnold Van Loevezijn, Wouter I. Iwema Bakker, Axel Stoit, Agatha A. M. Rensink, Jennifer Venhorst, Martina A. W. Van Der Neut, Martin De Hann, Cornelis G. Kruse
  • Patent number: 8883766
    Abstract: In general, the invention relates to compounds useful as ion channel modulators. It has now been found that compounds of this invention, and pharmaceutically acceptable compositions thereof, are useful as inhibitors of voltage-gated sodium channels.
    Type: Grant
    Filed: April 27, 2012
    Date of Patent: November 11, 2014
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Esther Martinborough, Tim Neubert, Tara Whitney, Danielle Lehsten, Tara Hampton, Nicole Zimmermann, Andreas P. Termin
  • Patent number: 8841282
    Abstract: The present invention relates to pyrrolidinone benzenesulfonamides of the following formula: useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders, such as pain.
    Type: Grant
    Filed: August 15, 2013
    Date of Patent: September 23, 2014
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Dean Stamos, Esther Ann Martinborough, Nicole Hilgraf, Timothy Donald Neubert, Mehdi Numa, Tara Whitney, Aarti Sameer Kawatkar
  • Publication number: 20140243296
    Abstract: A treatment regimen and dosage form comprising ritonavir and darunavir and their use in the treatment of HIV infection.
    Type: Application
    Filed: October 5, 2012
    Publication date: August 28, 2014
    Applicant: JAGOTEC AG
    Inventors: Pascal Grenier, Guy Vergnault, Patricia Ibarra
  • Publication number: 20140242168
    Abstract: The present invention provides perorally administrable drug release systems and processes for producing perorally administrable systems having a drug-containing core and a sheath which surrounds the core and comprises a swellable shell and an elastic coating which surrounds at least the shell, the sheath having at least one orifice.
    Type: Application
    Filed: July 6, 2012
    Publication date: August 28, 2014
    Applicant: LTS LOHMANN THERAPIE-SYSTEME AG
    Inventors: Christiane Schiller, Knut Seidlitz
  • Patent number: 8778628
    Abstract: An arylalkylamine compound is represented by the following formula [I-e] or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: June 17, 2013
    Date of Patent: July 15, 2014
    Assignee: Mitsubishi Tanabe Pharma Corporation
    Inventors: Hiroshi Miyazaki, Junko Okabe, Kosuke Yasuda, Iwao Takamuro, Osamu Sakurai, Tetsuya Yanagida, Yutaka Hisada
  • Patent number: 8748412
    Abstract: Provided herein are non-peptide GLP-1 receptor modulator compounds, for example, of Formula I, pharmaceutical compositions comprising such compounds, and processes of preparation thereof. Also provided are methods of their use for the treatment of a metabolic disorder.
    Type: Grant
    Filed: February 2, 2011
    Date of Patent: June 10, 2014
    Assignee: Argusina Bioscience Inc.
    Inventors: Jiayu Liao, Yufeng Hong, Yong Wang, Thomas W. Von Geldern, Kanyin E. Zhang
  • Publication number: 20140141089
    Abstract: The disclosure is directed to a nanoparticle comprising a porous framework core including a porous framework material and a compound, and a lipid layer disposed on the surface of the porous framework core.
    Type: Application
    Filed: February 11, 2010
    Publication date: May 22, 2014
    Applicant: Colorado School of Mines
    Inventor: Hongjun Liang
  • Publication number: 20140142070
    Abstract: This invention relates to solid oral dosage forms of the HIV inhibitor Darunavir and/or a pharmaceutically acceptable salt or solvate thereof, and combination formulations thereof.
    Type: Application
    Filed: July 6, 2012
    Publication date: May 22, 2014
    Applicant: Janssen R&D Ireland
    Inventors: Urbain Alfons C Delaet, Philip Erna H. Heyns, Eugeen Maria Jozef Jans, Roel Jos M. Mertens, Geert Van Der Avoort
  • Patent number: 8685947
    Abstract: Diuretic bioactivity profiles of phase inversion micronized furosemide and furosemide co-precipitated with Eudragit L100, and mixtures of those formulations with stock furosemide, reduced or eliminated the rapid spike in diuresis associated with immediate release formulations and maintained cumulative urine output. Of the formulations tested, each of a mixture of micronized furosemide with stock furosemide, and Eudragit L100 polymer with stock furosemide demonstrated optimal diuretic bioactivity profiles in subjects.
    Type: Grant
    Filed: August 25, 2011
    Date of Patent: April 1, 2014
    Assignee: Brown University
    Inventors: Edith Mathiowitz, Bryan Laulicht
  • Patent number: 8673886
    Abstract: The present invention is directed to the use of nifuratel, or a physiologically acceptable salt thereof, to treat infections caused by Atopobium species. The invention is further directed to the use of nifuratel to treat bacteriuria, urinary tract infections, infections of external genitalia in both sexes, as well as bacterial vaginosis, or mixed vaginal infections in women, when one or more species of the genus Atopobium are among the causative pathogens of those infections.
    Type: Grant
    Filed: April 19, 2010
    Date of Patent: March 18, 2014
    Assignee: Polichem SA
    Inventor: Federico Mailland
  • Publication number: 20140057879
    Abstract: The present invention relates to co-crystals of tramadol and co-crystal formers selected from NSAIDs/coxibs, processes for preparation of the same and their uses as medicaments or in pharmaceutical formulations, more particularly for the treatment of pain.
    Type: Application
    Filed: October 29, 2013
    Publication date: February 27, 2014
    Applicant: LABORATORIOS DEL DR. ESTEVE, S.A.
    Inventors: Carlos Ramon PLATA SALAMAN, Nicolas TESSON
  • Publication number: 20140038922
    Abstract: The present invention generally relates to protein signalling. In particular, compounds that inhibit the Wnt protein signalling pathway are disclosed. Such compounds may be used in the treatment of Wnt protein signalling-related diseases and conditions such as cancer, degenerative diseases, type II diabetes and osteopetrosis.
    Type: Application
    Filed: May 1, 2013
    Publication date: February 6, 2014
    Inventors: Lawrence LUM, Michael G. ROTH, Baozhi CHEN, Chuo CHEN, Michael E. DODGE, Wei TANG
  • Publication number: 20140038923
    Abstract: The present invention provides compounds and compositions, e.g., a series of compounds wherein a 1,5-biarylpyrazole group is conjugated to a urea group by a non-cleavable covalent chain, that are useful as dual COX-2/sEH inhibitors. The compounds disclosed herein have activity associated with the arachidonate cascade. The activity of these compounds was demonstrated using a lipopolysaccharide (LPS) induced model of pain in the rat. The compounds of the present invention demonstrated superior anti-allodynic activity as compared to the same dose of celecoxib, i.e., a COX-2 inhibitor, also as compared to the same dose of t-AUCB, i.e., a sEH inhibitor, and also as compared to the co-administered same dose of both celecoxib and t-AUCB. The dual inhibitors of the present invention demonstrate enhanced in vivo anti-allodynic activity in a nociceptive behavioral assay.
    Type: Application
    Filed: December 12, 2011
    Publication date: February 6, 2014
    Applicant: The Regents of the University of California
    Inventors: Bruce D. Hammock, Sung Hee Hwang, Karen Wagner, Christophe Morisseau, Aaron Wecksler, Guodong Zhang
  • Publication number: 20140030336
    Abstract: A pharmaceutical composition for the treatment or acute disorders is described. The composition comprises an essentially water-free, ordered mixture of at least one pharmaceutically active agent in the form of microparticles which are adhered to the surfaces of carrier particles which are substantially larger than the particles of the active agent or agents, and are essentially water-soluble, in combination with the bioadhesion and/or mucoadhesion promoting agent. The invention also relates to a method for preparing the composition and to the use of the composition for the treatment of acute disorders.
    Type: Application
    Filed: July 30, 2013
    Publication date: January 30, 2014
    Applicant: Orexo AB
    Inventors: Anders Pettersson, Christer Nystrom
  • Publication number: 20140024622
    Abstract: The present invention relates to pharmaceutical compositions comprising tramadol and celecoxib and their uses as medicaments or analgesics, more particularly for the treatment of severe to moderate pain with an inflammation component.
    Type: Application
    Filed: September 25, 2013
    Publication date: January 23, 2014
    Applicant: LABORATORIOS DEL DR. ESTEVE, S.A.
    Inventors: Enrique PORTILLO SALIDO, Sebastia VIDELA CES
  • Publication number: 20140018327
    Abstract: Disclosed is a compound of formula (I) wherein ‘a’ and R1-R5 are as described herein, as a modulator of nicotinic acetylcholine receptors particularly the ?7 subtype, in a subject in need thereof, as well as analogues, prodrugs, isotopically substituted analogs, metabolites, pharmaceutically acceptable salts, polymorphs, solvates, isomers, clathrates, and co-crystal thereofs, for use either alone or in combinations with suitable other medicaments, and pharmaceutical compositions containing such compounds and analogues. Also disclosed are a process of preparation of the compounds and the intended uses thereof in therapy, particularly in the prophylaxis and therapy of disorders such as Alzheimer's disease, mild cognitive impairment, senile dementia, and the like.
    Type: Application
    Filed: March 27, 2012
    Publication date: January 16, 2014
    Applicant: LUPIN LIMITED
    Inventors: Neelima Sinha, Gourhari Jana, Ajay Ramchandra Tilekar, Navnath Popat Karche, Venkata P. Palle, Rajender Kumar Kamboj
  • Publication number: 20140018326
    Abstract: Compounds of Formula I are disclosed: wherein L, A, R1, R2, R3A, R3B, R4A, R4B, R5, R6 and R7 are defined herein. The compounds encompassed by Formula I include compounds which are HIV protease inhibitors and other compounds which can be metabolized in vivo to HIV protease inhibitors. The compounds and their pharmaceutically acceptable salts are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
    Type: Application
    Filed: October 27, 2011
    Publication date: January 16, 2014
    Inventors: Oscar M. Moradei, Sheldon Crane, Daniel J. Mckay, Marie-Eve Lebrun, Vouy Linh Truong
  • Publication number: 20140011775
    Abstract: This invention concerns arylsulfonyl pyrazoline carboxamidine derivatives as antagonists of 5-ht6 receptors, to methods for the preparation of these compounds and to novel intermediates useful for their synthesis.
    Type: Application
    Filed: September 11, 2013
    Publication date: January 9, 2014
    Applicant: Abbott Healthcare Products B.V.
    Inventors: Arnold van Loevezijn, Wouter I. Iwema Bakker, Axel Stoit, Agatha A.M. Rensink, Jennifer Venhorst, Martina A.W. Van Der Neut, Martin De Hann, Cornelis G. Kruse
  • Publication number: 20140004177
    Abstract: The present invention generally relates to the transdermal delivery of various compounds. In some aspects, transdermal delivery may be facilitated by the use of a hostile biophysical environment. One set of embodiments provides a composition for topical delivery comprising a COX-2 inhibitor and/or a salt thereof, and optionally, a hostile biophysical environment and/or a nitric oxide donor. In some cases, the composition may be stabilized using a combination of a stabilization polymer (such as xanthan gum, KELTROL® BT and/or KELTROL® RD), propylene glycol, and a polysorbate surfactant such as Polysorbate 20, which combination unexpectedly provides temperature stability to the composition, e.g., at elevated temperatures such as at least 40° C. (at least about 104° F.), as compared to compositions lacking one or more of these.
    Type: Application
    Filed: December 29, 2011
    Publication date: January 2, 2014
    Applicant: Strategic Science & Technologies, LLC
    Inventor: Eric T. Fossel
  • Publication number: 20140005150
    Abstract: 3,4-diarylpyrazole derivatives of formula (I) as defined in the specification, and pharmaceutically acceptable salts thereof, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer.
    Type: Application
    Filed: August 20, 2013
    Publication date: January 2, 2014
    Applicant: NERVIANO MEDICAL SCIENCES S.R.L.
    Inventors: Maurizio Pulici, Fabio Zuccotto, Gabriella Traquandi, Sonia Biondaro, Paolo Trifiro', Alessandra Badari, Stefano Nuvoloni, Giovanni Cervi, Chiara Marchionni, Michele Modugno
  • Publication number: 20130345181
    Abstract: The present invention relates to the use of certain pyrrolopyridineamino derivatives (hereinafter referred to as “PPA derivatives”), particularly 1H-pyrrolo[3,2-c]pyridine-6-amino derivatives, to inhibit the spindle checkpoint function of Monospindle 1 (Mps1—also known as TTK) kinases either directly or indirectly via interaction with the Mps kinase itself. In particular, the present invention relates to PPA derivatives for use as therapeutic agents for the treatment and/or prevention of proliferative diseases, such as cancer. The present invention also relates to processes for the preparation of the PPA derivatives, and pharmaceutical compositions comprising them.
    Type: Application
    Filed: March 14, 2012
    Publication date: December 26, 2013
    Applicant: CANCER RESEARCH TECHNOLOGY LIMITED
    Inventors: Vassilios Bavetsias, Butrus Atrash, Sébastien Gaston André Naud, Peter William Sheldrake, Julian Blagg
  • Publication number: 20130338119
    Abstract: The present invention relates to heterocyclic derivatives useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.
    Type: Application
    Filed: August 15, 2013
    Publication date: December 19, 2013
    Applicant: Vertex Pharmaceuticals Incorporated
    Inventors: Dean Stamos, Esther Ann Martinborough, Nicole Hilgraf, Timothy Donald Neubert, Mehdi Numa, Tara Whitney, Aarti Sameer Kawatkar