Nitrogen Containing Patents (Class 514/471)
The nitrogen bonded directly to the hetero ring (Class 514/472)
  • SMALL MOLECULE INHIBITORS OF BOTULINUM NEUROTOXINS
    Publication number: 20110294848
    Abstract: The invention provides potent quinolinol-based BoNT/A small-molecule inhibitors of botulinum neurotoxins, in particular of Clostridium botulinum serotype A neurotoxins. The invention also provides methods of using these small-molecule inhibitors to inhibit infections by Clostridium botulinum, as well as, methods of preventing infections by Clostridium botulinum through materials that may be ingested.
    Type: Application
    Filed: May 28, 2009
    Publication date: December 1, 2011
    Inventors: Virginia I. Roxas-Duncan, Leonard A. Smith, Nizamettin Gul, John H. Cardellina, II, Rebecca C. Vieira, Susan M. Ensel, David C.H. Yang, Istvan J. Enyedy, Sivanesan Darkshanamurthy, Salimuddin Shah
  • Sphingosine-1-Phosphate Receptor Antagonists
    Publication number: 20110288076
    Abstract: This disclosure relates to sphingosine-1-phosphate (S1P) receptor antagonists, compositions comprising the S1P receptor antagonists and methods for using and processes for making the S1P receptor antagonists. In particularly, this disclosure relates to sphingosine-1-phosphate 1 (S1P1) receptor antagonists, compositions comprising the S1P1 receptor antagonist and methods for using the S1P1 receptor antagonist, such as in the treatment of cancer, and processes for making the S1P1 receptor antagonists.
    Type: Application
    Filed: October 16, 2009
    Publication date: November 24, 2011
    Applicant: EXELIXIS, INC.
    Inventors: Mohamed Abdulkader Ibrahim, Joon Won Jeong, Henry William Beecroft Johnson, Patrick Kearney, James W. Leahy, Gary L. Lewis, Robin Tammie Noguchi, John M. Nuss
  • SURGICAL COMPOSITIONS CONTAINING SIGMA-RECEPTOR AGONISTS
    Publication number: 20110288101
    Abstract: One aspect of the present invention relates to aqueous surgical compositions comprising a sigma-1 receptor agonist. Another aspect of the present invention relates to methods of irrigating ocular tissues during an ophthalmic surgical procedure such as cataract surgery. Such methods comprise bathing the ocular tissues with a composition comprising a sigma-1 receptor agonist.
    Type: Application
    Filed: May 20, 2011
    Publication date: November 24, 2011
    Applicant: ALCON RESEARCH, LTD.
    Inventors: Lixin Wang, Marcia Danielle Ong, Chi-Chun Tsai, Michael Hartzer
  • SULFONYL CONTAINING COMPOUNDS AS CYSTEINE PROTEASE INHIBITORS
    Publication number: 20110281879
    Abstract: The present invention is directed to compounds that are inhibitors of cysteine proteases, in particular, cathepsins B, K, L, F, and S and are therefore useful in treating diseases mediated by these proteases. The present invention is directed to pharmaceutical compositions comprising these compounds and processes for preparing them.
    Type: Application
    Filed: January 12, 2011
    Publication date: November 17, 2011
    Applicant: ViroBay, Inc.
    Inventor: Craig Mossman
  • Histone deacetylases inhibitors
    Patent number: 8058273
    Abstract: New inhibitors of histone deacetylases having antitumor activity, and the process of preparation thereof are herein described. These compounds belong to the structural formula (I) where R1 is a linear or branched chain containing at least two conjugated double bonds, A is an optionally substituted phenyl or pyridyl ring, Ar is an aryl or heteroaryl group, and R3 is hydrogen or alkoxyalkyl. The application also describes the use of said compounds in the treatment of diseases associated to the deregulation of histone deacetylases activity, such as tumors, as well as the relevant pharmaceutical compositions for administration to patients requiring said treatment.
    Type: Grant
    Filed: June 1, 2010
    Date of Patent: November 15, 2011
    Assignee: DAC S.R.L.
    Inventors: Saverio Minucci, Pier Giuseppe Pelicci, Antonello Mai, Marco Ballarini, Gaetano Gargiulo, Silvio Massa
  • SMALL MOLECULE INHIBITORS OF NADS, NAMNAT, AND NMNAT
    Publication number: 20110275635
    Abstract: Small molecule inhibitors of bacterial nicotinamide adenine dinucleotide synthetase (NADs), bacterial nicotinic acid mononucleotide adenylyltransferase (NaMNAT), and human nicotinamide mononucleotide adenylyltransferase (NMNAT) are provided, as well as methods of making and using the inhibitors.
    Type: Application
    Filed: January 8, 2010
    Publication date: November 10, 2011
    Applicant: THE UAB RESEARCH FOUNDATION
    Inventors: Wayne J. Brouillette, Christie G. Brouillette, Whitney B. Moro
  • Synergistic active compound combinations
    Publication number: 20110275583
    Abstract: Novel active compound combinations comprising compounds of the formula (I) and compounds of the formula (II) have very good insecticidal and acaricidal properties.
    Type: Application
    Filed: April 28, 2011
    Publication date: November 10, 2011
    Applicant: Bayer CropScience AG
    Inventors: Thomas BRETSCHNEIDER, Heike HUNGENBERG, Martin Füsslein
  • N-Acylthiourea and N-Acylurea Inhibitors of the Hedgehog Protein Signalling Pathway
    Publication number: 20110275663
    Abstract: The present invention relates to the use of acylthiourea or acylurea derivatives for the treatment of pathologies involving a tissue dysfunction associated with a deregulation of the Hedgehog protein signalling pathway, and also to novel acylthiourea or acylurea derivatives as such, to their use as a medicinal product, and to pharmaceutical compositions containing them.
    Type: Application
    Filed: April 16, 2009
    Publication date: November 10, 2011
    Inventors: Martial Ruat, Hélène Faure, Elisabeth Traiffort, Angèle Schoenfelder, André Mann, Maurizio Taddei, Antonio Solinas, Fabrizio Manetti
  • Heteroaryl Diamide Compounds Useful as MMP-13 Inhibitors
    Publication number: 20110275625
    Abstract: Disclosed are compounds and compositions of the formula (I) as described herein which are inhibitors of MMP-13. Also disclosed are methods of using and making compounds of the formula (I).
    Type: Application
    Filed: November 5, 2009
    Publication date: November 10, 2011
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Neil Alexander Farrow, Donghong Amy Gao, Alexander Heim-Riether, Shuang Liang, Sabine Schlyer, Lana Louise Smith Keenan, Steven John Taylor, Bernd Wellenzohn, Dieter Wiedenmayer, Zhaoming Xiong, Qiang Zhang
  • SPILL RESISTANT FORMULATIONS CONTAINING CLAYS
    Publication number: 20110269723
    Abstract: 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: Application
    Filed: July 12, 2011
    Publication date: November 3, 2011
    Applicant: Taro Pharmaceuticals U.S.A., Inc.
    Inventors: Satish ASOTRA, Xiaoli Wang, Zoltan Bodor
  • METHODS OF TREATING ULCERATIVE COLITIS
    Publication number: 20110263601
    Abstract: Methods are disclosed for treating ulcerative colitis and related diseases and disorders, which comprise inhibiting tryptophan hydroxylase (TPH) in patients in need thereof.
    Type: Application
    Filed: October 25, 2010
    Publication date: October 27, 2011
    Inventors: Philip Manton Brown, Qingyun Liu, Brian Zambrowicz
  • PHARMACEUTICAL FORMULATION FOR USE IN HIV THERAPY
    Publication number: 20110262533
    Abstract: The invention discloses a formulation prepared by granulating at least one anti-retro viral drug and at least one pharmaceutically acceptable additive, using an organic solvent; milling the product; finally processing the milled product to form tablets or capsules.
    Type: Application
    Filed: June 10, 2011
    Publication date: October 27, 2011
    Inventors: Kiran Kumar Narsaiah VELAVENI, Sanjay Deshraj Verma, Akhilesh Ashok Dixit, Abhijit Mukund Deshmukh, Sanjeev Meharchand Sethi
  • NOVEL BRADYKININ B1-ANTAGONISTS
    Publication number: 20110263626
    Abstract: The present invention relates to compounds of general formula I wherein n, R1, R2, R3, R4, R5, R6, R7 and R8 are defined as stated hereinafter, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with organic or inorganic acids or bases, which have valuable properties, the preparation thereof, the pharmaceutical compositions containing the pharmacologically effective compounds, the preparation thereof and the use thereof.
    Type: Application
    Filed: August 28, 2008
    Publication date: October 27, 2011
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Norbert Hauel, Angelo Ceci, Enzo Cereda, Henri Doods, Ingo Konetzki, Juergen Mack, Henning Priepke, Annette Schuler-metz, Rainer Walter
  • New Compounds
    Publication number: 20110263556
    Abstract: This invention relates to compounds of formula I, their use as inhibitors of the microsomal prostaglandin E2 synthase-1 (mPGES-1), pharmaceutical compositions containing them, and their use as medicaments for the treatment and/or prevention of inflammatory diseases and associated conditions such as inflammatory/nociceptive pain. A, M, R1, R2, R7, Ra, Rb, Q3, Q4, Q6, Z2, Z4, Z5, Z6 and W have meanings given in the description.
    Type: Application
    Filed: October 20, 2010
    Publication date: October 27, 2011
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Henning PRIEPKE, Henri DOODS, Raimund KUELZER, Roland PFAU, Dirk STENKAMP, Robert ROENN, Benjamin PELCMAN
  • Squaramide derivatives as CXCR2 antagonist
    Publication number: 20110251206
    Abstract: The present invention relates to compounds of formula (I) wherein X, R1, R2, R3, R4 and R5 are as defined herein, which are useful for treating diseases which respond to CXCR2 receptor mediators. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.
    Type: Application
    Filed: June 21, 2011
    Publication date: October 13, 2011
    Inventors: Urs Baettig, Anne-Marie D'Souza, Peter Hunt, Neil John Press, Simon James Watson
  • MELT-COATED PHARMACEUTICAL COMPOSITION WITH FAST RELEASE
    Publication number: 20110250244
    Abstract: The present invention relates to a process for producing a solid, coated pharmaceutical composition by a melt coating process. The process is adapted to provide a solid, coated pharmaceutical composition by melt coating, which has a fast release.
    Type: Application
    Filed: December 17, 2009
    Publication date: October 13, 2011
    Applicant: Losan Pharma GmbH
    Inventors: Peter Kraahs, Stefanie Bold, Lars Fahsel
  • Modulators of G Protein-Coupled Receptor 88
    Publication number: 20110251196
    Abstract: The present disclosure is generally directed to compounds which can modulate G-protein coupled receptor 88, compositions comprising such compounds, and methods for modulating G-protein coupled receptor 88.
    Type: Application
    Filed: October 5, 2010
    Publication date: October 13, 2011
    Inventors: Carolyn Diane Dzierba, Richard A. Hartz, Yingzhi Bi, Vijay T. Ahuja, Joanne J. Bronson, Kenneth Carson, Giovanni Cianchetta, Michael Green, David Kimball, S. Roy Kimura, Soojin Kwon, John E. Macor, Yulian Zhang, Greg Zipp
  • SUBSTITUTED AMIDO PHENOXYBENZAMIDES
    Publication number: 20110237592
    Abstract: The present invention relates to substituted amido phenoxybenzamide compounds of general formula (I): in which A, R1, R2, R3, R4, R5, R6, R7, R8, R9 and n are as defined in the claims, to pharmaceutical compositions and combinations containing said compounds, to methods of preparing said compounds, and to the use of said compounds or compositions for treating hyper-proliferative and/or angiogenesis disorders, as a sole agent or in combination with other active ingredients.
    Type: Application
    Filed: October 29, 2009
    Publication date: September 29, 2011
    Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFT
    Inventors: Ingo Hartung, Marion Hitchcock, Knut Eis, Florian Puhler
  • TREATMENT OF OBSTRUCTIVE SLEEP APNEA SYNDROME WITH A COMBINATION OF A CARBONIC ANHYDRASE INHIBITOR AND AN ADDITIONAL ACTIVE AGENT
    Publication number: 20110224196
    Abstract: This invention relates generally to methods and pharmaceutical formulations useful in treating patients suffering from obstructive sleep apnea syndrome (OSAS). Treatment of OSAS is effected by administering a carbonic anhydrase inhibitor to the patient in combination with at least one additional active agent. Examples of additional active agents include modafinil, eszopiclone, zolpidem, zaleplon, and phentermine.
    Type: Application
    Filed: January 7, 2011
    Publication date: September 15, 2011
    Applicant: Vivus, Inc.
    Inventors: Leland F. Wilson, Peter Tam, Thomas Najarian, Charles H. Bowden
  • SUBSTITUTED HYDROXAMIC ACIDS AND USES THEREOF
    Publication number: 20110212969
    Abstract: This invention provides compounds of formula (I): wherein ring A, X1, X2, X3, R2, R4b, R10, and G have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention, and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.
    Type: Application
    Filed: February 25, 2011
    Publication date: September 1, 2011
    Applicant: Millennium Pharmaceuticals, Inc.
    Inventors: Christopher Blackburn, Kenneth M. Gigstad, Sean J. Harrison, He Xu
  • NOVEL BRIDGED CYCLIC COMPOUNDS AS HISTONE DEACETYLASE INHIBITORS
    Publication number: 20110212943
    Abstract: Provided herein are novel bridged cyclic derivatives of the general formula (I), their analogs, tautomeric forms, stereoisomers, polymorphs, solvates, intermediates, pharmaceutically acceptable salts, pharmaceutical compositions, metabolites and prodrugs thereof. These compounds can inhibit HDACs and are useful as therapeutic or ameliorating agent for diseases that are involved in cellular growth such as malignant tumors, autoimmune diseases, skin diseases, infections, inflammation, neurode-generative disorders etc.
    Type: Application
    Filed: October 14, 2009
    Publication date: September 1, 2011
    Applicant: ORCHID RESEARCH LABORATORIES LIMITED
    Inventors: Gopalan Balasubramanian, Ponpandian Thanasekaran, Sridharan Rajagopal, Bharathimohan Kuppusamy, Virendra Kachhadia, Vignesh Radhakrishnan, Sivasudar Velaiah, Shridhar Narayanan, Mandar Bhonde, Praveen Rajendran, Sriram Rajagopal
  • 3,4-Di-Substituted Cyclobutene-1,2-Diones as CXC-Chemokine Receptor Ligands
    Publication number: 20110213029
    Abstract: There are disclosed compounds of the formula or a pharmaceutically acceptable salt or solvate thereof which are useful for the treatment of chemokine-mediated diseases such as acute and chronic inflammatory disorders and cancer.
    Type: Application
    Filed: May 6, 2011
    Publication date: September 1, 2011
    Applicants: Schering Corporation, Pharmacopeia Drug Discovery
    Inventors: Arthur G. Taveras, Cynthia J. Aki, Richard W. Bond, Jianping Chao, Michael Dwyer, Johan A. Ferreira, Jianhua Chao, Younong Yu, John J. Baldwin, Bernd Kaiser, Ge Li, J. Robert Merritt, Purakkattle J. Biju, Kingsley H. Nelson, JR., Laura L. Rokosz, Gaifa Lai, James P. Jakway, Minglang Wu, Evan A. Hecker, Daniel Lundell, Jay S. Fine
  • PHARMACEUTICAL FORMULATIONS AND METHODS OF USE WHICH COMBINE NON-STEROIDAL ANTI-INFLAMMATORY COMPOUNDS WITH ANIT-HYPERTENSIVE COMPOUNDS
    Publication number: 20110207724
    Abstract: An oral dosage form of a non-steroidal anti-inflammatory drug (NSAID) is rendered safer for extended or chronic use for anti-inflammatory, analgesic or antipyretic therapy by combining it with an antihypertensive drug. The antihypertensive drug acts prophylactically to inhibit or reduce NSAID-induced hypertension and by so doing the adverse cardiovascular side effects of NSAIDs, such as high blood pressure, heart attack, stroke, opththamologic complications, and death, when NSAIDs are used repetitively over an extended period of time for reducing inflammation or in pain management.
    Type: Application
    Filed: May 22, 2009
    Publication date: August 25, 2011
    Inventors: Peter C. Hoyle, Paul Waymack
  • Use of Carboxamides on Cultivated Plants
    Publication number: 20110203018
    Abstract: The present invention relates to a method of controlling pests and/or increasing the health of a plant as compared to a corresponding control plant by treating the cultivated plant, parts of a plant, seed, or their locus of growth with a carboxamide compound.
    Type: Application
    Filed: October 21, 2009
    Publication date: August 18, 2011
    Applicant: BASF SE
    Inventors: Markus Gewehr, Dirk Voeste, Juergen Logemann, Maarten Hendrik Stuiver, Pilar Puente, Robert John Gladwin
  • INHIBITORS OF THE SHIGA TOXINS TRAFFICKING THROUGH THE RETROGRADE PATHWAY
    Publication number: 20110201601
    Abstract: The present invention relates to the use of compounds of general formula (I) and (II) for the preparation of a drug for preventing and/or treating disorders caused by Shiga toxins and related toxins.
    Type: Application
    Filed: June 17, 2009
    Publication date: August 18, 2011
    Applicants: COMMISSAR. A L'ENERG. ATOM. ET AUX ENERG. ALTERN., INSTITUT CURIE, CENTRE NAT DE LA RECHERCHE SCIENTIFIQUE
    Inventors: Daniel Gillet, Julien Barbier, Ludger Johannes, Bahne Stechmann, Siau-Kun Bai
  • SULFONAMIDE COMPOUNDS OR SALTS THEREOF
    Publication number: 20110201616
    Abstract: [Object] A compound which is useful as an EP1 receptor antagonist is provided. [Means for Solution] The present inventors investigated EP1 receptor antagonists, and confirmed that a compound having a sulfonamide structure, in which the nitrogen atom of the sulfonamide structure is substituted with 2-fluoropropyl group, 3-fluoro-2-methylpropyl group or the like, has a potent EP1 receptor antagonistic action, thereby completing the present invention. The sulfonamide compound of the present invention has a potent EP1 receptor antagonistic action and can be used as an agent for preventing and/or treating a lower urinary tract symptom or the like.
    Type: Application
    Filed: June 22, 2009
    Publication date: August 18, 2011
    Applicant: Astellas Pharma Inc.
    Inventors: Hideki Kubota, Issei Tsukamoto, Kazunori Kamijo, Koji Kato, Yuta Fukuda, Hidenori Azami
  • DUAL-ACTING THIOPHENE, PYRROLE, THIAZOLE AND FURAN ANTIHYPERTENSIVE AGENTS
    Publication number: 20110178101
    Abstract: In one aspect, the invention relates to compounds having the formula: wherein: Ar, Z, R3, R4 and R5 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
    Type: Application
    Filed: January 18, 2011
    Publication date: July 21, 2011
    Inventors: Paul R. Fatheree, Robert Murray McKinnell
  • Hydroxamic Acid Derivatives Useful as Antibacterial Agents
    Publication number: 20110178042
    Abstract: The invention relates to a compound of formula (I): or a pharmaceutically acceptable salt thereof, thereof, wherein: G is a group of formula (II); and pharmaceutically acceptable salts, prodrugs, hydrates, or solvates, thereof, wherein A, B. L1-L4 A, B, R1-R4 and m are as defined herein. The invention also relates to pharmaceutical compositions comprising the compounds of formula (I) and their use in treating a bacterial infection.
    Type: Application
    Filed: September 1, 2009
    Publication date: July 21, 2011
    Applicant: Pfizer Inc.
    Inventors: Matthew F. Brown, Charles F. Donovan, Edmund L. Eilsworth, Denton W. Hoyer, Timothy A. Johnson, Manjinder S. Lall, Chris Lim-Berakis, Sean T. Murphy, Debra A. Sherry, Clarke B. Taylor, Joseph S. Warmus
  • GASTRORETENTIVE DRUG DELIVERY SYSTEM, PREPARATION METHOD AND USE THEREOF
    Publication number: 20110171275
    Abstract: A gastroretentive drug delivery system is provided. Said system comprises a hollow vesicle and a drug-containing layer which surrounds the hollow vesicle. Said hollow vesicle preferably has a single chamber structure. The size in maximal diameter direction of said hollow vesicle is preferably 0.5-3.5 cm. The gastroretentive drug delivery system preferably contains an isolating layer and/or waterproofing layer between the hollow vesicle and the layer containing drug.
    Type: Application
    Filed: November 4, 2008
    Publication date: July 14, 2011
    Applicant: TEAM ACADEMY OF PHARMACEUTICAL SCIENCE
    Inventors: Qingwei Jiang, Junli Zheng, Wenbin Yang, Quanzhi Liu
  • AQUAPORIN MODULATORS AND METHODS OF USING THEM FOR THE TREATMENT OF EDEMA AND FLUID IMBALANCE
    Publication number: 20110172195
    Abstract: Compounds, including 3-carboxy aryl sulfonamide compounds, which agonize or antagonize aquaporin channels and methods of using them to treat disorders or diseases mediated by aquaporins.
    Type: Application
    Filed: March 15, 2011
    Publication date: July 14, 2011
    Applicant: ARIZONA BOARD OF REG. ON BEHALF OF THE UNIV. OF AZ
    Inventors: Gary A. Flynn, Andrea J. Yool, Elton Rodrigues Migliati, Leslie S. Ritter
  • Inhibitors of plasma kallikrein
    Patent number: 7977380
    Abstract: The present invention provides compounds that inhibit the activity of plasma kallikrein (PK) and methods of preventing and treating the formation of thrombin during or after a PK dependent disease or condition, for example, after fibrinolysis treatment.
    Type: Grant
    Filed: November 20, 2009
    Date of Patent: July 12, 2011
    Assignee: Activesite Pharmaceticals, Inc.
    Inventors: Sukanto Sinha, Tamie Jo Chilcote
  • BIARYL AMINO ACIDS AND THEIR USE IN DNA BINDING OLIGOMERS
    Publication number: 20110160192
    Abstract: Compounds of formula (I): Z?-CO-A-B—NH-Z (I) wherein: Z is H or an amino protecting group; Z? is OH, a protected or activated hydroxyl group or Cl; A is an optionally substituted C5-6 arylene group; and B is an optionally substituted C5-6 arylene group.
    Type: Application
    Filed: March 7, 2011
    Publication date: June 30, 2011
    Applicant: SPIROGEN LIMITED
    Inventors: Philip Wilson Howard, Geoffrey Wells
  • AGRICULTURAL CHEMICAL COMPOSITION AND FRUIT BAG
    Publication number: 20110159065
    Abstract: The present invention provides an agricultural chemical composition containing an agricultural chemical active ingredient A, a sorbitan fatty acid ester and a wax, and a production process thereof. In addition, the present invention provides an agricultural chemical sheet or a fruit bag in which the agricultural chemical composition is retained, and a production process thereof.
    Type: Application
    Filed: August 24, 2009
    Publication date: June 30, 2011
    Applicant: Nippon Soda Co., Ltd.
    Inventors: Kaoru Nishimura, Takao Iwasa
  • NOVEL AROMATIC COMPOUNDS AND THEIR USE IN MEDICAL APPLICATIONS
    Publication number: 20110152291
    Abstract: Pharmaceutical compositions comprising at least one compound of the formulas (Ia) or (Ib) and a pharmaceutically acceptable carrier wherein the symbols have the following meaning —X- is e.g. and Y being e.g. or the pharmaceutically acceptable salts can be applied to modulate the in-vitro and in-vivo binding processes mediated by E-, P- or L-selectin binding.
    Type: Application
    Filed: March 1, 2011
    Publication date: June 23, 2011
    Applicant: REVOTAR BIOPHARMACEUTICALS AG
    Inventors: Ewald M. AYDT, Remo Kranich, Anke S. Busemann
  • ACYLAMINO-SUBSTITUTED FUSED CYCLOPENTANECARBOXYLIC ACID DERIVATIVES AND THEIR USE AS PHARMACEUTICALS
    Publication number: 20110152290
    Abstract: The present invention relates to compounds of the formula I, wherein A, Y, Z, R3 to R6, R20 to R22 and R50 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. Specifically, they are inhibitors of the endothelial differentiation gene receptor 2 (Edg-2, EDG2), which is activated by lysophosphatidic acid (LPA) and is also termed as LPA1 receptor, and are useful for the treatment of diseases such as atherosclerosis, myocardial infarction and heart failure, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.
    Type: Application
    Filed: November 4, 2010
    Publication date: June 23, 2011
    Applicant: SANOFI-AVENTIS
    Inventors: Matthias SCHAEFER, Josef PERNERSTORFER, Dieter KADEREIT, Hartmut STROBEL, Werngard CZECHTIZKY, L. Charlie CHEN, Alena SAFAROVA, Aleksandra WEICHSEL, Marcel PATEK
  • COMPOSITION AND METHOD FOR INHIBITING NOROVIRUS INFECTION
    Publication number: 20110152263
    Abstract: A composition for use in inhibiting the binding of a Norovirus to the histo-blood group antigen on the surface of epithelia. The composition contains a therapeutically effective amount of a binding-inhibiting compound selected from Compounds 1 through 15, and at least one diluent, carrier or excipient. The Compounds competitively bind a Norovirus that has the capability of binding with the histo-blood group antigens of secretor blood type, including A, B, AB, and O blood types. The compositions can be administered to a human prior to or after infection by a Norovirus, to prevent or ameliorate an infection.
    Type: Application
    Filed: November 15, 2007
    Publication date: June 23, 2011
    Inventor: Xi JIANG
  • Method Of Controlling Soil Insects
    Publication number: 20110150957
    Abstract: The present invention relates to an insecticidal granular composition, comprising (a) at least one insecticide, selected from the group consisting of an enaminocarbonyl compound, a neonicotinoid, a tetronic acid derivative or a tetramic acid derivative compound, a carbamate compound, an organophosphate compound, a diamide compound, a pyrethroid compound and flonicamid; (b) optionally at least one moisture-retaining agent; and (c) vegetable meal.
    Type: Application
    Filed: August 26, 2009
    Publication date: June 23, 2011
    Applicant: Bayer CropScience AG
    Inventors: Wolfgang Wirth, Wolfgang Thielert, Heike Hungenberg, Jean-Pierre Trijau
  • ALCANOIC ACID AMIDES SUBSTITUTED BY SATURATED O-HETEROCYCLES
    Publication number: 20110144197
    Abstract: Compounds of the general formula (formula I) in which the meanings of the substituents R1 and R6 are as indicated in claim 1, have renin-inhibiting properties and can be used as medicines.
    Type: Application
    Filed: February 18, 2011
    Publication date: June 16, 2011
    Inventors: Peter Herold, Robert Mah, Vincenzo Tschinke, Stefan Stutz, Aleksandar Stojanovic, Stjepan Jelakovic, Christiane Marti
  • NOVEL PHLOROGLUCINOL DERIVATIVES HAVING SELECTIN LIGAND ACTIVITY
    Publication number: 20110142765
    Abstract: Pharmaceutical compositions comprising at least one compound of the formula (I) and a pharmaceutically acceptable carrier which is useful in a medicine wherein the symbols and substituents have the following meaning —X— is e.g. and Y being e.g. or the pharmaceutically acceptable salts, esters or amides and prodrugs can be applied to modulate the in-vitro and in-vivo binding processes mediated by E-, P- or selectin binding.
    Type: Application
    Filed: February 23, 2011
    Publication date: June 16, 2011
    Applicant: REVOTAR BIOPHARMACEUTICALS AG
    Inventors: Ewald M. AYDT, Remo Kranich
  • NOVEL CARBOXYLIC ACID ANALOGS AS GLYCOGEN SYNTHASE ACTIVATORS
    Publication number: 20110136792
    Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of metabolic diseases and disorders such as, for example, type II diabetes mellitus.
    Type: Application
    Filed: October 20, 2010
    Publication date: June 9, 2011
    Inventors: David Robert Bolin, Stuart Hayden, Yimin Qian, Kshitij Chhabilbhai Thakkar
  • DELIVERY OF H2 ANTAGONISTS
    Publication number: 20110135716
    Abstract: The present invention provides improved systems and methods for the local delivery of H2 antagonists. The inventive methods include topical administration of an effective amount of a H2 antagonist encapsulated in liposomes. In certain embodiments, the H2 antagonist, for example, Cimetidine, is encapsulated into paucilamellar liposomes, such as NOVASOME® microvesicles. Also provided are pharmaceutical compositions comprising liposome-encapsulated H2 antagonists. The methods and compositions of the present invention may be used to treat any disease state or condition where local administration of H2 antagonists is beneficial.
    Type: Application
    Filed: February 15, 2011
    Publication date: June 9, 2011
    Applicant: TRUSTEES OF BOSTON UNIVERSITY
    Inventors: Thomas E. Van Dyke, Michael Holick, Alpdogan Kantarci, Hatice Hasturk
  • Compressible-Coated Pharmaceutical Compositions and Tablets and Methods of Manufacture
    Publication number: 20110129530
    Abstract: There is provided a method for preparing a pharmaceutical composition comprising compressible coated, taste-masked and/or controlled-release coated drug-containing particles, rapidly-dispersing microgranules comprising a disintegrant and a sugar alcohol, a saccharide, or a mixture thereof, and other optional, pharmaceutically acceptable excipients wherein the orally disintegrating tablet (ODT) or rapidly dispersing tablet (RDT) composition having acceptable tableting, organoleptic, and pharmacokinetic properties.
    Type: Application
    Filed: November 30, 2010
    Publication date: June 2, 2011
    Applicant: EURAND, INC.
    Inventors: Gopi M. Venkatesh, Jin-Wang Lai, James M. Clevenger, Craig Kramer
  • USES OF CALPAIN INHIBITORS TO INHIBIT INFLAMMATION
    Publication number: 20110117106
    Abstract: Calpains target junctional components that normally seal the epithelium, forming tight junctions. This selective targeting by calpains facilitates the transmigration of leukocytes across the epithelium and into tissue spaces where they can cause inflammation. The present disclosure provides methods of using calpain inhibitors to prevent epithelial junction reorganization such that leukocyte transmigration is inhibited and accordingly, inflammation reduced or prevented. These methods can at least be used to reduce respiratory inflammation by preventing leukocyte accumulation in pulmonary airways.
    Type: Application
    Filed: March 6, 2009
    Publication date: May 19, 2011
    Inventor: Alice Prince
  • USE OF ANTI-BACTERIAL AGENTS FOR THE TREATMENT OF EPITHELIAL-RELATED CONDITIONS
    Publication number: 20110118265
    Abstract: Disclosed herein are methods of inactivating and/or decolonizing bacteria on a surface. The present invention also discloses methods for treatment of epithelial conditions caused or aggravated by bacteria, such as acne vulgaris, in a subject in need thereof. The present invention additionally discloses inventive compounds and compositions that exhibit anti-bacterial and/or anti-inflammatory effects.
    Type: Application
    Filed: November 12, 2010
    Publication date: May 19, 2011
    Inventors: Jeffry B. Stock, Maxwell Stock
  • INHIBITOR OF PLASMINOGEN ACTIVATOR INHIBITOR-1
    Publication number: 20110112140
    Abstract: The present invention relates to a novel compound having plasminogen activator inhibitor-1 (PAI-1) inhibitory activity, and a PAI-1 inhibitor comprising the compound as an active ingredient. The present invention further relates to a pharmaceutical composition that has an inhibitory action on PAI-1 activity and is useful in the prevention and treatment of various diseases whose onset is associated with PAI-1 activity. The novel compound is represented by the following general formula. Each symbol is defined as those in the specification.
    Type: Application
    Filed: March 31, 2009
    Publication date: May 12, 2011
    Applicant: RENASCIENCE CO., LTD.
    Inventors: Toshio Miyata, Nagahisa Yamaoka, Hidehiko Kodama, Kenji Murano
  • INDANE DERIVATIVES AS AMPA RECEPTOR MODULATORS
    Publication number: 20110092539
    Abstract: The present invention relates to a heterocyclic derivative according to formula (I); wherein the variables are defined as in the specification, or to a pharmaceutically acceptable salt or solvate thereof. The present invention also relates to a pharmaceutical composition comprising said heterocyclic derivatives and to their use in therapy, for instance in the treatment or prevention of psychiatric diseases where an enhancement of synaptic responses mediated by AMPA receptors is required, including schizophrenia, depression and Alzheimer's disease.
    Type: Application
    Filed: June 3, 2009
    Publication date: April 21, 2011
    Inventors: Jonathan Gillespie, Craig Jamieson, Zoran Rankovic
  • Isoxazoline compounds having MIF antagonist activity
    Patent number: 7928130
    Abstract: Methods of use and pharmaceutical compositions for a genus of low molecular weight compounds comprising optionally substituted isoxazoline ring systems that act as inhibitors of MIF (macrophage migration inhibitory factor) are disclosed. Specifically, the compounds are useful for treating a variety of diseases involving inflammatory activity or pro-inflammatory cytokine responses, such as autoimmune diseases (including rheumatoid arthritis, insulin-dependent diabetes, multiple sclerosis, graft versus host disease, lupus syndromes), asthma, arthritis, ARDS, psoriasis, interleukin-2 toxicity, proliferative vascular disease, and various forms of sepsis and septic shock, and other conditions characterized by underlying MIF responses including, for instance, tumor growth and neovascularization (angiogenesis).
    Type: Grant
    Filed: January 27, 2009
    Date of Patent: April 19, 2011
    Assignee: Cytokine PharmaSciences, Inc.
    Inventor: Yousef Al-Abed
  • FATTY ACID ACIFRAN DERIVATIVES AND THEIR USES
    Publication number: 20110082202
    Abstract: The invention relates to fatty acid acifran derivatives; compositions comprising an effective amount of a fatty acid acifran derivative; and methods for treating or preventing an metabolic disease comprising the administration of an effective amount of a fatty acid acifran derivative.
    Type: Application
    Filed: October 5, 2010
    Publication date: April 7, 2011
    Inventors: Jill C. Milne, Michael R. Jirousek, Jean E. Bemis, Chi B. Vu
  • Uses of neuraminidase inhibitors in infectious diseases
    Patent number: 7910620
    Abstract: The present invention relates to methods of decreasing the infectivity, morbidity and rate of mortality, in treating diseases associated with a variety of pathogenic organisms, specifically diseases involving one or more pathogens that require neuraminidase as a virulence factor. In addition, the present invention uses biology based therapy to treat neuraminidase dependent infections or diseases dependent on sialic acid metabolism.
    Type: Grant
    Filed: April 22, 2005
    Date of Patent: March 22, 2011
    Inventor: Jack J. Broadhurst, III
  • ?- and ?- amino acid hydroxyethylamino sulfonamides useful as retroviral protease inhibitors
    Patent number: RE42889
    Abstract: ?- and ?-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
    Type: Grant
    Filed: April 23, 2007
    Date of Patent: November 1, 2011
    Assignee: G.D. Searle LLC
    Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, John N. Freskos, Robert M. Heintz, Deborah E. Bertenshaw