The Hetero Ring Is Five-membered Patents (Class 514/158)
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Publication number: 20110312921Abstract: The present invention relates to N-heterocyclic sulphonamide compounds, in particular pyrazole sulphonamide compounds, and their use as N-myristoyl transferase inhibitors.Type: ApplicationFiled: August 29, 2009Publication date: December 22, 2011Inventors: Stephen Brand, Paul Wyatt, Stephen Thompson, Victoria Smith, Tracy Bayliss, Justin Harrison, Neil Norcross, Laura Cleghorn, Ian Gilbert, Ruth Brenk
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Publication number: 20110301128Abstract: Compounds, compositions and methods for modulating the activity of receptors are provided. In particular compounds and compositions are provided for modulating the activity of receptors and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder directly or indirectly related to the activity of the receptors.Type: ApplicationFiled: August 22, 2011Publication date: December 8, 2011Applicant: EXELIXIS, INC.Inventors: Lynne Canne Bannen, Jeff Chen, Lisa Esther Dalrymple, Brenton T. Flatt, Timothy Patrick Forsyth, Xiao-Hui Gu, Morrison B. Mac, Larry W. Mann, Grace Mann, Richard Martin, Raju Mohan, Brett Murphy, Michael Charles Nyman, William C. Stevens, Tie-Lin Wang, Yong Wang, Jason H. Wu
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Publication number: 20110301129Abstract: Controlled release oral dosage forms are provided for the continuous, sustained administration of a pharmacologically active agent to the upper gastrointestinal tract of a patient in whom the fed mode as been induced. The majority of the agent is delivered, on an extended release basis, to the stomach, duodenum and upper regions of the small intestine, with drug delivery in the lower gastrointestinal tract and colon substantially restricted. The dosage form comprises a matrix of a biocompatible, hydrophilic, erodible polymer with an active agent incorporated therein, wherein the polymer is one that both swells in the presence of water and gradually erodes over a time period of hours, with swelling and erosion commencing upon contact with gastric fluid, and drug release rate primarily controlled by erosion rate.Type: ApplicationFiled: June 3, 2011Publication date: December 8, 2011Applicant: DEPOMED, INC.Inventors: BRET BERNER, JENNY LOUIE-HELM
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Publication number: 20110300137Abstract: The present application discloses the use of the anti-malarial drug lumefantrine and related compounds in the treatment of cancer.Type: ApplicationFiled: June 1, 2011Publication date: December 8, 2011Inventor: Douglas Tyler McKenzie
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Publication number: 20110286993Abstract: The present invention concerns a method for modulating the enzymatic activity of an enzyme, wherein said enzyme interacts with BMP, said method comprising the step of administering or inducing Hsp70, or a functional fragment or variant thereof, in a form suitable for allowing interaction between BMP and Hsp70, or said functional fragment or variant thereof, and thereby modulating the enzymatic activity of an enzyme interacting with BMP.Type: ApplicationFiled: June 26, 2009Publication date: November 24, 2011Inventors: Thomas Kirkegaard Jensen, Marja Helena Jaattela
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Publication number: 20110269723Abstract: The invention relates to novel spill resistant formulations comprising either a weak base or a weak acid as the pharmaceutical ingredient, a liquid base, a clay and a water soluble cellulose ether. The clay and cellulose ether allow for a broader pH range into which the pharmaceutically active agent may be dispersed or dissolved, and therefore allows for easier preparation and formulation of the pharmaceutical composition.Type: ApplicationFiled: July 12, 2011Publication date: November 3, 2011Applicant: Taro Pharmaceuticals U.S.A., Inc.Inventors: Satish ASOTRA, Xiaoli Wang, Zoltan Bodor
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Publication number: 20110269722Abstract: The invention provides the compounds of formula (I) or pharmaceutically acceptable salts thereof. The invention also provides pharmaceutical compositions comprising one or more compounds of formula I or intermediates thereof and one more of pharmaceutically acceptable carriers, vehicles or diluents. The invention further provides methods of preparation and methods of use of prodrugs including NO-releasing prodrugs, double prodrugs and mutual prodrugs comprising the compounds of formula I.Type: ApplicationFiled: December 23, 2010Publication date: November 3, 2011Inventor: Apparao Satyam
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Publication number: 20110269677Abstract: The invention provides protease inhibitors that are chemically modified by covalent attachment of a water-soluble oligomer. A conjugate of the invention, when administered by any of a number of administration routes, exhibits characteristics that are different from the protease inhibitors not attached to the water-soluble oligomer.Type: ApplicationFiled: March 12, 2008Publication date: November 3, 2011Applicant: Nektar TherapeuticsInventors: Jennifer Riggs-Sauthier, Lin Cheng, Tacey X. Viegas, Xuyuan Gu, Franco J. Duarte, Wen Zhang
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Publication number: 20110263544Abstract: The present invention comprises a compound for the prevention and/or treatment of cardiovascular diseases, nephropathy, fibrosis, primary aldosteronism or edema. The compound is of the following general formula (I): wherein R1 represents a C1-C3 alkyl group; R2 represents a hydroxy-C1-C4 alkyl group and the like; R3 represents a halogeno group, a halogeno-C1-C3 alkyl group and the like; R4 represents a hydrogen atom, a halogeno group and the like, —R5 represents a sulfamoyl group or a C1-C3 alkylsulfonyl group; R6 represents a hydrogen atom, a halogeno group and the like] or an N-oxide, atropisomer of the foregoing, or pharmaceutically acceptable salt of the foregoing.Type: ApplicationFiled: October 7, 2009Publication date: October 27, 2011Applicants: DAIICHI SANKYO COMPANY, LIMITED, EXELIXIS, INC.Inventors: John Nuss, Matthew Williams, Raju Mohan, Richard Martin, Tie-Lin Wang, Hiroyuki Tsuruoka, Kazumasa Aoki, Masatoshi Honzumi, Yusuke Asoh, Keiji Saito, Tsuyoshi Homma
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Publication number: 20110263542Abstract: The present invention relates, in general to treatment of pain comprising administering an alpha-2 adrenergic agonist and an endothelin antagonist, wherein administration of the agents acts as an analgesic and ameliorates pain in a subject.Type: ApplicationFiled: July 28, 2008Publication date: October 27, 2011Applicant: ENGOGENXInventor: Anil Gulati
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Publication number: 20110263543Abstract: Biphenyl compounds of Formula (I) and Formula (II), and their pharmaceutically acceptable salts or solvates or prodrugs, their pharmaceutical compositions, their use and process of preparation are provided. Compounds of Formula (I) and Formula (II) are disclosed to exhibit anti-inflammatory properties.Type: ApplicationFiled: August 24, 2009Publication date: October 27, 2011Inventors: Rajiv R. Sakhardande, Vithal Kulkarni, Nilesh Wagh, Manmohan Nimbalkar, Suhas M. Nadkarni
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Publication number: 20110257111Abstract: This invention relates to novel hydroxyethylamino sulfonamides and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a compound with the ability to act as an HIV (human immunodeficiency virus) protease inhibitor.Type: ApplicationFiled: October 23, 2009Publication date: October 20, 2011Inventors: Scott L. Harbeson, Carig E. Masse
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Publication number: 20110257134Abstract: The present invention relates to co-crystals of tramadol and co-crystal formers selected from NSAIDs, processes for preparation of the same, their uses in pharmaceutical formulations, and for the treatment of various disorders, including pain.Type: ApplicationFiled: October 16, 2009Publication date: October 20, 2011Applicant: LABORATORIOS DEL DR. ESTEVE, S.A.Inventors: Helmut Heinrich Buschmann, Lluis Sola Carandell, Jordi Benet Buchholz, Jordi Carles Ceron Bertran, Carlos Ramon Plata Salaman, Nicolas Tesson
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Publication number: 20110256129Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic protein family members, compositions containing the compounds and uses of the compounds for preparing medicaments for treating diseases during which occurs expression one or more than one of an anti-apoptotic protein family member.Type: ApplicationFiled: April 25, 2011Publication date: October 20, 2011Inventors: Milan Bruncko, Hong Ding, Steven Elmore, Aaron Kunzer, Christopher L. Lynch, William McClellan, Cheol-Min Park, Andrew Petros, Xiaohong Song, Xilu Wang, Noah Tu, Michael Wendt, Alexander Shoemaker, Michael Mitten
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Publication number: 20110245208Abstract: A method of combating a somatosensory disorder in a subject, comprising administering to the subject an effective amount of a composition comprising bupranolol and/or pharmaceutically acceptable derivative(s) thereof. Compositions useful for such administration are described, including salts, esters, solvates, etc. of tert-butyl[3-(2-chloro-5-methylphenoxy)-2-hydroxypropyl]amine, in which such salt, ester, solvate, etc. compound is in enantiomeric excess or homoenantiomeric in the R isomer thereof, or is formulated with racemic mixtures of the R and S stereoisomers of the salts, esters, solvates, etc. of tert-butyl[3-(2-chloro-5-methylphenoxy)-2-hydroxypropyl]amine. Combination therapy compositions of opioid receptor agonists and such compounds are also described. A method is disclosed of referential genotypic screening of candidate subjects in connection with therapeutic intervention using the compositions of the disclosure to combat the somatosensory disorder.Type: ApplicationFiled: March 30, 2011Publication date: October 6, 2011Applicant: ALGYNOMICS INC.Inventors: Luda Diatchenko, William Maixner
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Publication number: 20110237554Abstract: Inhibitors of NKCC1, such as bumetanide, when coadministered with inhibitors of GABA transaminase, such as vigabatrin, attenuate both the retinal toxicity and the intramyelinic edema.Type: ApplicationFiled: March 22, 2011Publication date: September 29, 2011Inventor: Frances E. Jensen
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Publication number: 20110195940Abstract: Provided herein (among other things) are protease inhibitor compounds having enhanced features, along with methods for administering such compounds. For example, the subject compounds can be administered without concomitant administration of a CYP3A4 inhibitor, have increased therapeutic index and/or increased potency, and are low-resistance inducing in nature. Exemplary potent HIV protease inhibitors are mono-m-PEG3-atazanavir, mPEGn-N-darunavir (wherein n is 3 or 5), mPEGn-NHCO-saquinavir (wherein n is 5 or 7), and di-mPEG3-atazanavir.Type: ApplicationFiled: September 17, 2009Publication date: August 11, 2011Applicant: Nektar TherapeuticsInventors: C. Simone Jude-Fishburn, Laurie A. Vander Veen, Timothy A. Riley
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Publication number: 20110195939Abstract: HIV-protease inhibitors, particularly saquinavir, showed strong anticancer activity but numerous side effects limited its application. In order to overcome its toxicity original compounds were modified by covalent attachment of NO. The efficacy of parental and NO-modified drug was compared in vitro and in vivo. Anticancer activities of NO-modified saquinavir (Saq-NO) was monitored in vitro using assay for cell viability, proliferation, necrotic, autophagic and apoptotic cell death, differentiation, expression of intracellular molecules such as cyclin D3, p53 and Akt. Antitumor properties and toxicity of the compound was estimated in vivo. Saq-NO abrogated the viability of large spectrum of human and rodent tumor cell lines with IC50 significantly lower than parental drug and expressed strong antimelanoma action in vivo. In contrast to saquinavir, there was no detectable toxicity against primary cells in vitro and in vivo.Type: ApplicationFiled: July 30, 2009Publication date: August 11, 2011Applicant: GANIAL IMMUNOTHERAPEUTICS INC.Inventors: Ferdinando Nicoletti, Yousef Al-Abed, Gianni Garotta
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Publication number: 20110183944Abstract: Compositions for controlled release of one or more therapeutic agents where the composition is essentially free of excipients are disclosed. In particular, compositions comprising a HMG-CoA reductase inhibitor, particularly simvastatin, and a NSAID, such as a COX-2 inhibitor, particularly celecoxib, in which greater than 90% of the weight of the composition is made up of the HMG-CoA reductase inhibitor and NSAID are provided.Type: ApplicationFiled: January 27, 2011Publication date: July 28, 2011Inventors: Paul Ashton, Hong Guo, Jianbing Chen, Tadeusz Cynkowski, Grazyna Cynkowska
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Publication number: 20110182869Abstract: This invention relates to products comprising antibiotics or probiotics and the use thereof for the treatment of gut motility disorders such as irritable bowel syndrome (IBS).Type: ApplicationFiled: July 14, 2009Publication date: July 28, 2011Inventors: Jan Knol, Kaouther Ben Amor, Richèle Deodata Wind
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Publication number: 20110166110Abstract: The present invention provides a novel class of fused ring azadecalin compounds and methods of using the compounds as glucocorticoid receptor modulators.Type: ApplicationFiled: March 11, 2011Publication date: July 7, 2011Applicant: Corcept Therapeutics, Inc.Inventors: Robin D. Clark, Nicholas C. Ray, Paul M. Blaney, Christopher A. Hurley, Karen Williams
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Publication number: 20110105440Abstract: The present invention is directed to hexahydrocyclopentylf]indazole carboxamides and derivatives thereof as selective glucocorticoid receptor ligands useful for treating a variety of autoimmune and inflammatory diseases or conditions. Pharmaceutical compositions and methods of use are also included.Type: ApplicationFiled: February 24, 2009Publication date: May 5, 2011Inventors: William P. Dankulich, Mildred L. Kaufman, Danielle M. McMaster, Robert S. Meissner, Helen J. Mitchell
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Publication number: 20110082117Abstract: 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: ApplicationFiled: July 27, 2010Publication date: April 7, 2011Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Esther Martinborough, Lev T.D. Fanning, Urvi Sheth, Dean Wilson, Andreas P. Termin, Timothy D. Neubert, Nicole Hilgraf, Tara Leanne Hampton, Tara Whitney, Aarti Sameer Kawatkar, Danielle Lehsten, Dean Stamos, Jinglan Zhou, Vijayalaksmi Arumugam, Corey Anderson
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Publication number: 20110064677Abstract: This invention provides new lipoxin analogs, compositions containing analogs, and methods of using these compounds and compositions for treating and preventing oral inflammation, including gingivitis, periodontitis, and other forms of periodontal disease. The invention also provides for methods of treating and preventing oral inflammation, including gingivitis, periodontitis, and other forms of periodontal disease with compositions containing COX-2 inhibitors. Further, the invention provides methods for preventing systemic diseases beyond theoral cavity that are related to periodontal disease using the composition containing lipoxin analogs, COX-2 inhibitors, or both.Type: ApplicationFiled: September 28, 2010Publication date: March 17, 2011Applicants: TRUSTEES OF BOSTON UNIVERSITY, BRIGHAM AND WOMEN'S HOSPITAL, INC., UNIVERSITY OF SOUTHERN CALIFORNIAInventors: Thomas E. Van Dyke, Nicos A. Petasis, Charles N. Serhan
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Publication number: 20110021467Abstract: The invention relates to methods of treating or preventing malaria which comprises administering to a patient in need thereof, an effective amount of a 1H-indazole-3-carboxamide derivative of general formula (I), in the form of a base or of an addition salt with an acid, or in the form of a hydrate or of a solvate of said base or acid addition salt.Type: ApplicationFiled: October 1, 2010Publication date: January 27, 2011Applicant: Sanofi-AventisInventors: Hugues D'ORCHYMONT, Laurent Fraisse, André Zimmermann
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Publication number: 20110003764Abstract: The present invention relates to a drug combination capable of conferring therapeutic benefits in the treatment of both AIDS and malaria. In particular, it relates to a drug combination including at least one quinolinic antimalarial compound such as chloroquine or hydroxychloroquine, and at least one inhibitor of the Human Immunodeficiency Virus (HIV) protease enzyme. This drug combination is capable of inhibiting the replication of both HIV and Plasmodium sp. It also relates to the direct antimalarial effects of the HIV PIs.Type: ApplicationFiled: May 26, 2009Publication date: January 6, 2011Inventor: Andrea Savarino
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Publication number: 20100305073Abstract: The present invention relates to compounds that have CYP450 inhibiting properties and are therefore useful as boosters of certain drugs, i.e. they are able to increase at least one of the pharmacokinetic variables of certain drugs when co-administered. The invention further provides the use of said compounds as improvers of the bioavailability of certain drugs. Methods for the preparation of the compounds of the invention and pharmaceutical compositions are also provided.Type: ApplicationFiled: December 5, 2008Publication date: December 2, 2010Inventors: Tim Hugo Maria Jonckers, Wim Bert Griet Schepens, Geerwin Yvonne Paul Haché, Beate Sabine Hallenberger, Jennifer Chiyomi Sasaki, Judith Eva Baumeister, Gerben Albert Van 'T Klooster
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Publication number: 20100249049Abstract: The present invention relates to an arylalkylamine compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof, a process for preparing the same, and use of the above-mentioned compound as an activating compound (CaSR agonist) of a Ca sensing receptor, a pharmaceutical composition containing the above-mentioned compound as an effective ingredient, etc.Type: ApplicationFiled: May 7, 2010Publication date: September 30, 2010Inventors: Hiroshi MIYAZAKI, Junko TSUBAKIMOTO, Kosuke YASUDA, Iwao TAKAMURO, Osamu SAKURAL, Tetsuya YANAGIDA, Yataka HISADA
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Patent number: 7786125Abstract: The present application is directed to therapeutic compounds, compositions, and methods for culturing neuronal cells and for preventing and the treatment of neurodegenerative diseases, such as Parkinson's disease and amyotrophic lateral sclerosis (ALS).Type: GrantFiled: April 7, 2009Date of Patent: August 31, 2010Inventor: Leu-Fen H. Lin
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Publication number: 20100210603Abstract: The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.Type: ApplicationFiled: September 11, 2009Publication date: August 19, 2010Inventors: Roger D. Tung, Mark A. Murcko, Govinda R. Bhisetti
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Publication number: 20100196368Abstract: New substituted benz-azole compounds, compositions and methods of inhibition of Raf kinase activity in a human or animal subject are provided. The new compounds compositions may be used either alone or in combination with at least one additional agent for the treatment of a Raf kinase mediated disorder, such as cancer.Type: ApplicationFiled: March 12, 2010Publication date: August 5, 2010Applicant: NOVARTIS VACCINES AND DIAGNOSTICS, INC.Inventors: Payman Amiri, Wendy Fantl, Teresa Hansen, Barry Haskell Levine, Christopher McBride, Daniel J. Poon, Savithri Ramurthy, Paul A. Renhowe, Cynthia M. Shafer, Sharadha Subramanian, Leonard Sung
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Patent number: 7723389Abstract: The invention provides pharmaceutical compositions for the treatment or prevention of the toxic effects of therapeutic agents and methods of treating or preventing such toxicity using a toxicity reducing amount of N-acetylcysteine either alone or in combination with a therapeutically effective amount or, to achieve its therapeutic advantages, an amount larger than what is customarily given as a therapeutically effective amount, of a therapeutic agent.Type: GrantFiled: November 4, 2002Date of Patent: May 25, 2010Assignee: The Board of Trustees of the Leland Stanford Junior UniversityInventors: Leonard A. Herzenberg, Leonore A. Herzenberg, Stephen C. De Rosa, James Andrus
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Patent number: 7671077Abstract: The present application is directed to therapeutic compounds, compositions, and methods for culturing neuronal cells and for preventing and the treatment of neurodegenerative diseases, such as Parkinson's disease and amyotrophic lateral sclerosis (ALS).Type: GrantFiled: July 19, 2004Date of Patent: March 2, 2010Inventor: Leu-Fen Hou Lin
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Patent number: 7625884Abstract: A method of increasing the bioavailability of balsalazide by administration of an oral dosage form with food is provided, as well as an article of manufacture comprising an oral dosage form of balsalazide 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: GrantFiled: October 23, 2007Date of Patent: December 1, 2009Assignee: Salix Pharmaceuticals, LtdInventor: Lorin Johnson
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Patent number: 7452872Abstract: A method of increasing the bioavailability of balsalazide by administration of an oral dosage form with food is provided, as well as an article of manufacture comprising an oral dosage form of balsalazide 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: GrantFiled: August 8, 2007Date of Patent: November 18, 2008Assignee: Salix Pharmaceuticals, Inc.Inventor: Lorin Johnson
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Patent number: 6518274Abstract: The invention relates to the use of cycloventabenzofuran derivatives for the production of a medicament for the treatment of nuclear factor of &kgr;B-dependent diseases.Type: GrantFiled: April 18, 2001Date of Patent: February 11, 2003Assignee: Bayer AktiengesellschaftInventors: Matthias Gehling, Jörg Baumgarten, Axel Kretschmer, Horst-Peter Antonicek, Peter Proksch, Bambang Wahyu Nugroho, Frank Bohnenstengel
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Publication number: 20010055565Abstract: The invention relates to a method of detecting concentrations of cyclooxygenase-2 in a mammal, the method comprising: administering to the mammal a diagnostically effective amount of a cyclooxygenase-2 selective agent, which is capable of being detected in vivo; and b) detecting the agent so the concentration of cyclooxygenase-2 is detected.Type: ApplicationFiled: January 9, 2001Publication date: December 27, 2001Applicant: G.D. Searle & Co.Inventors: Peter C. Isakson, Karen Seibert, John J. Talley
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Patent number: 6306842Abstract: In accordance with the present invention, there are provided conjugates of a combination of pharmacologically active agents (e.g., NSAIDs and selective COX-2 inhibitors). Invention conjugates provide a new class of pharmacologically active agents (e.g., anti-inflammatory agents) which provide the therapeutic benefits of both NSAIDs and selective COX-2 inhibitors, while causing a much lower incidence of side-effects then are typically observed with such agents due to the protective effects imparted by modifying the pharmacologically active agents as described herein.Type: GrantFiled: June 2, 2000Date of Patent: October 23, 2001Assignee: Medinox, Inc.Inventors: Ching-San Lai, Tingmin Wang
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Patent number: 6284752Abstract: New pharmaceutical compositions and pharmaceutical compositions comprising metal complexes have activity against diseases caused by or related to overproduction or localised high concentration of nitric oxide in the body.Type: GrantFiled: October 19, 1998Date of Patent: September 4, 2001Assignee: AnorMED Inc.Inventors: Michael J Abrams, Simon P Fricker, Barry A Murrer, Owen J Vaughan
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Patent number: 6262040Abstract: The invention relates to compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein R, R1, and R2, are as defined herein. The invention further relates to pharmaceutical compositions containing, and methods of using, the compounds of formula (I), or acceptable salts thereof, for the inhibition of phosphodiesterase (PDE) type IV or the production of tumor necrosis factor (TNF) in a mammal. The invention also relates to intermediates that are useful in the preparation of the compounds of formula (I).Type: GrantFiled: March 4, 1999Date of Patent: July 17, 2001Assignee: Pfizer IncInventor: Anthony Marfat
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Patent number: 6004948Abstract: Compounds of the formula (I) in which A is oxygen, sulphur or NH; B is a group of the formula (IIa) or (IIb); and the other variables have the meaning given in claim 1, may be used as inhibitors of the enzyme cyclooxygenase II ##STR1##Type: GrantFiled: September 3, 1998Date of Patent: December 21, 1999Assignee: Nycomed Austria GmbHInventors: Heinz Blaschke, Peter Kremminger, Michael Hartmann, Harald Fellier, Jorg Berg, Thomas Christoph, Franz Rovenszky, Dagmar Stimmeder
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Patent number: 5958910Abstract: The invention is concerned with the use of sulfonamide derivatives of the general formula ##STR1## wherein R Signifies lower-alkyl, phenyl, benzyl, naphthyl, pyridyl or thienyl, optionally substituted by one or more lower-alkyl, lower-alkoxy, lower-alkyl carbonyl-amino, halogen, cycloalkyl, nitro, amino, methylenedioxy, phenoxy or benzyloxy substituents, and the aromatic rings, can, in turn, be substituted by nitro, halogen or amino,R.sup.1 -R.sup.4 signify hydrogen, halogen, hydroxy, lower-alkyl, nitro, cyano, amino, lower-alkoxy, benzyloxy, trifluoromethyl or phenyl, optionally substituted by one or more lower-alkyl, trifluoromethyl, nitro, amino or hydroxy substituents, and wherein R.sup.1 and R.sup.2 or R.sup.2 and R.sup.Type: GrantFiled: November 20, 1998Date of Patent: September 28, 1999Assignee: Hoffmann-La Roche Inc.Inventors: Andrea Cesura, Stephan Rover
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Patent number: 5753688Abstract: A class of pyrazolyl benzenesulfonamide compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula I: ##STR1## or a pharmaceutically-acceptable salt thereof.Type: GrantFiled: September 27, 1995Date of Patent: May 19, 1998Inventors: John J. Talley, Thomas D. Penning, Paul W. Collins, Donald J. Rogier, Jr., James W. Malecha, Julie M. Miyashiro, Stephen R. Bertenshaw, Ish K. Khanna, Matthew J. Graneto, Roland S. Rogers, Jeffery S. Carter
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Patent number: 5547975Abstract: A class of benzopyranopyrazolyl derivatives is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula I ##STR1## wherein A is --(CH.sub.2).sub.m --X--(CH.sub.2).sub.n --; wherein X is S(O).sub.p or O; wherein m is 0 or 1; wherein n is 0 or 1; wherein p is 0 or 1; wherein B is selected from phenyl and five and six membered heteroaryl; wherein R.sup.1 is selected from lower haloalkyl, cyano, formyl, lower alkoxycarbonyl, lower alkoxy, lower N-alkylaminocarbonyl, N-phenylaminocarbonyl, lower N,N-dialkylaminocarbonyl and lower N-alkyl-N-phenylaminocarbonyl; wherein R.sup.2 is phenyl substituted at a substitutable position with a radical selected from lower alkylsulfonyl and sulfamyl; and wherein R.sup.Type: GrantFiled: September 20, 1994Date of Patent: August 20, 1996Inventors: John J. Talley, Stephen R. Bertenshaw, Matthew J. Graneto, Donald J. Rogier
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Patent number: 5273970Abstract: The antibacterial substance baquiloprim (2,4-diamino-5-[8-dimethylamino-7-methyl-5-quinolylmethyl]pyrimidine) is shown to be active against protozoal infections, e.g. toxoplasmosis. Preferably the baquiloprim is administered together with a sulphonamide.Type: GrantFiled: January 3, 1991Date of Patent: December 28, 1993Assignee: Coopers Animal Health LimitedInventor: Nicholas McHardy
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Patent number: 5258374Abstract: Furosemide ##STR1## is used as medicament for the treatment of allergic conjunctivitis; it is dropped into the conjunctival fornix of the eye.Type: GrantFiled: July 18, 1991Date of Patent: November 2, 1993Assignee: Hoechst AktiengesellschaftInventor: Sebastiano Bianco
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Patent number: 5135924Abstract: Systemic bacterial infections caused by aerobic and anaerobic organisms in companion animals such as dogs can be treated effectively and conveniently by the oral administration on a once a day basis of an antibacterial combination of ormetoprim and a sulfonamide, the activity of which is potentiated by ormetoprim. Various dosage forms are possible, including concentrates for addition to the feed or drinking water, as well as boluses, tablets, pastes, solutions, and suspensions for administration directly to the animals.Type: GrantFiled: September 24, 1990Date of Patent: August 4, 1992Assignee: Hoffmann-La Roche Inc.Inventors: Wallace E. Brandt, Lyle J. Hanson, Gianpaolo Maestrone
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Patent number: 5096897Abstract: Substituted antithrombotic substituted cycloalkano[b]-dihydroindole- and -indole-sulphonamides for treatment of thromboses, thromboembolisms, ischaemias, asthma and allergies, of the formula ##STR1## in which R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are hydrogen or other radicals,X is aryl, alkyl or CF.sub.3,m and Z each is 1, 2, 3 or 4,n is 0, 1 or 2,A is a bond or --NH--, andY is OH, alkoxy, aryloxy, amino or sulphonylamine, with the proviso that, in all cases, two of the substituents R.sup.1 -R.sup.4 are other than hydrogen in the event that m represents the number 2 and Y represents the hydroxyl group,or a salt thereof.Type: GrantFiled: March 28, 1991Date of Patent: March 17, 1992Assignee: Bayer AktiengesellschaftInventors: Horst Boshagen, Ulrich Muller, Ulrich Rosentreter, Erwin Bischoff, Volker-Bernd Fiedler, Elisabeth Perzborn, Joachim Hutter, Peter Norman, Nigel J. Cuthbert, Hilary P. Francis, Marie G. McKenniff
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Patent number: 5039670Abstract: Substituted antithrombotic substituted cycloalkano[b]-dihydroindole- and -indole-sulphonamides for treatment of thromboses, thromboembolisms, ischemias, asthma and allergies, of the formula ##STR1## in which R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are hydrogen or other radicals,X is aryl, alkyl or CF.sub.3,m and Z each is 1,2,3 or 4,n is 0, 1 or 2,A is a bond or --NH--, andY is OH, alkoxy, aryloxy, amino or sulphonylamine, with the proviso that, in all cases, two of the substituents R.sup.1 -R.sup.4 are other than hydrogen in the event that m represents the number 2 and Y represents the hydroxyl group,or a salt thereof.Type: GrantFiled: October 17, 1990Date of Patent: August 13, 1991Assignee: Bayer AktiengesellschaftInventors: Horst Boshagen, Ulrich Muller, Ulrich Rosentreter, Erwin Bischoff, Volker-Bernd Fiedler, Elisabeth Perzborn, Joachim Hutter, Peter Norman, Nigel J. Cuthbert, Hilary P. Francis, Marie G. McKenniff
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Patent number: 4985417Abstract: Method and formulation useful in treatment of glaucoma in a mammal wherein an effective amount of an active water soluble carbonic anhydrase inhibitor is administered, said inhibitor being a compound having the formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein R.sup.1 is selected from the group consisting of H, NH.sub.2 CH.sub.2 --, --CH(Me)NH.sub.2, --CH(NH.sub.2)CHMe.sub.2, --CH(NH.sub.2)CH.sub.2 CHMe.sub.2, --CH(NH.sub.2)CH(Me)CH.sub.2 Me, 2-pyrrolidinyl residues wherein the R.sup.1 CO-- constitutes an .alpha.-aminoacyl group, N-acetylaminoacyl derivatives and the corresponding dipeptidyl radicals wherein R.sup.1 CO-- is a dipeptidyl residue containing two amino acid residues of the formula where R.sup.1 is --CHR.sup.7 NHCOCHR.sup.8 NH.sub.2, R.sup.6 NHCHR.sup.5 --, ##STR2## and R.sup.6 NHCH.sub.2 CHR.sup.5 --; R.sup.2 is selected from the group consisting of H, alkyl having from 1 to 6 carbon atoms, alkenyl having from 2 to 6 carbon atoms, and cycloalkyl;R.sup.Type: GrantFiled: May 2, 1989Date of Patent: January 15, 1991Inventors: Seymour F. Trager, G. Michael Blackburn