Plural Nitrogens In Alcohol Moiety Patents (Class 560/251)
  • Publication number: 20140315786
    Abstract: The present invention relates to targeting an intracellular enzyme for release of covalently linked bioactives which results in a synergistic effect between the bioactives. The present invention relates to the use of bioactives that are directly connected covalently or through a covalent molecular linker which have increased therapeutic activity when released as the free bioactives by intracellular enzymes as compared to when the bioactives are administered individually (i.e. not covalently linked). Further, methods are described of administering to patients in need thereof, bioactives as linked bioactives having increased therapeutic activity. Accordingly, this invention also relates to methods of treating patients for certain diseases.
    Type: Application
    Filed: March 16, 2012
    Publication date: October 23, 2014
    Applicant: Catabasis Pharmaceuticals, Inc.
    Inventors: Michael R. Jirousek, Jill C. Milne, David Carney, Jean E. Bemis, Chi B. Vu
  • Patent number: 8835494
    Abstract: Pro-drugs of 1-(2-halo-biphenyl-4-yl)alkanecarboxylic acids are useful for preventing and/or treating neurodegenerative diseases, improving cognitive function and treating cognitive impairment.
    Type: Grant
    Filed: April 3, 2013
    Date of Patent: September 16, 2014
    Assignee: Chiesi Farmaceutici S.p.A.
    Inventors: Bruno Pietro Imbimbo, Luca Raveglia
  • Publication number: 20140256998
    Abstract: Anti-agglomerants for gas hydrates, comprising alkoxylated and/or acylated non-quaternary nitrogen-containing compounds, method for inhibiting the agglomeration of gas hydrates in a conduit, and compositions comprising the gas hydrate anti-agglomerant, a corrosion inhibitor and/or a paraffin deposition inhibitor.
    Type: Application
    Filed: May 20, 2014
    Publication date: September 11, 2014
    Applicant: AKZO NOBEL N.V.
    Inventors: Martin HELLSTEN, Hans OSKARSSON
  • Publication number: 20140213788
    Abstract: The present invention relates to a process for the preparation of a compound of the general Formula (I), comprising: a) reacting a compound of the general Formula (II) with a compound of the Formula III R2COOH and a compound of the general Formula IV R3NC under such conditions that compound I is formed, wherein R1 represents a substituted or unsubstituted alkyl, alkenyl, alkynyl, aromatic or non-aromatic, mono-, di- or tricyclic, or heterocyclic structure, and R2 represents a substituted or unsubstituted alkyl, alkenyl, alkynyl, aromatic or non-aromatic, mono-, di- or tricyclic, or heterocyclic structure, and R3 represents a substituted or unsubstituted alkyl, alkenyl, or alkynyl structure. In further aspect the subject invention relates to the use of the the obtained products as intermediates for various peptidomimetics, and preferably as a building block in a convergent synthesis of prolyl dipeptide structures.
    Type: Application
    Filed: March 28, 2014
    Publication date: July 31, 2014
    Applicant: Vereniging voor Christelijk hoger onderwijs, wetenschappelijk onderzoek en patiëntenzorg
    Inventors: Eelco RUIJTER, Romano ORRU, Anass ZNABET, Marloes POLAK, Nicholas TURNER
  • Patent number: 8791246
    Abstract: An inventive substrate is provided which includes a substrate compound of formula A-B1-B2-B3-B4: wherein A is a sugar moiety; B1 is a linker moiety allowing the conjugation of moiety A and the remaining structure of the substrate; B2 is a linker moiety with a free reactive amino group so as to be available for reaction with carboxylic acids or detectable tags; B3 contains a permanently charged element such as a quaternary ammonium group so as to increase sensitivity for mass spectrometry analysis; and B4 of various carbon length conferring specificity amongst individual substrates in detection methods. Also provided is a molecule of the formula B1-B2-B3-B4, with similar structural characteristics to an enzymatic product produced by the action of a target enzyme on an inventive substrate. Further provided are methods for using inventive substrates for detecting enzymatic activity.
    Type: Grant
    Filed: April 3, 2012
    Date of Patent: July 29, 2014
    Assignee: PerkinElmer Health Sciences, Inc.
    Inventors: Blas Cerda, Mark Norman Bobrow
  • Publication number: 20140187617
    Abstract: Provided are compounds that are inhibitors of both rho kinase and of a monoamine transporter (MAT) act to improve the disease state or condition. Further provided are compositions comprising the compounds. Further provided are methods for treating diseases or conditions, the methods comprising administering compounds according to the invention. One such disease may be glaucoma for which, among other beneficial effects, a marked reduction in intraocular pressure (IOP) may be achieved.
    Type: Application
    Filed: December 23, 2013
    Publication date: July 3, 2014
    Applicant: AERIE PHARMACEUTICALS, INC.
    Inventors: Mitchell A. deLong, Jill Marie Sturdivant, Susan M. Royalty
  • Patent number: 8765810
    Abstract: The present invention is directed to compounds that are allosteric inhibitors of tumor necrosis factor receptor I, compositions comprising such compounds, and methods of using such compounds and compositions thereof in the treatment of TNF-? mediated conditions.
    Type: Grant
    Filed: October 18, 2012
    Date of Patent: July 1, 2014
    Assignees: The Trustees Of The University Of Pennsylvania, Cephalon, Inc.
    Inventors: Mark I. Greene, Ramachandran Murali, Xin Cheng, Raphael Ottenbrite, Yingxin Xiaio
  • Patent number: 8686145
    Abstract: The present invention relates to a process for the preparation of a compound of the general Formula (I), comprising: a) reacting a compound of the general Formula (II) with a compound of the Formula III R2COOH and a compound of the general Formula IV R3NC under such conditions that compound I is formed, wherein R1 represents a substituted or unsubstituted alkyl, alkenyl, alkynyl, aromatic or non-aromatic, mono-, di- or tricyclic, or heterocyclic structure, and R2 represents a substituted or unsubstituted alkyl, alkenyl, alkynyl, aromatic or non-aromatic, mono-, di- or tricyclic, or heterocyclic structure, and R3 represents a substituted or unsubstituted alkyl, alkenyl, or alkynyl structure. In further aspect the subject invention relates to the use of the obtained products as intermediates for various peptidomimetics, and preferably as a building block in a convergent synthesis of prolyl dipeptide structures.
    Type: Grant
    Filed: September 16, 2010
    Date of Patent: April 1, 2014
    Assignee: Vereniging Voor Christelijk Hoger Onderwijs, Wetenschappelijk Onderzoek en Patientenzorg C/O Technology Transfer Officer VU & Vumc
    Inventors: Eelco Ruijter, Romano Orru, Anass Znabet, Marloes Polak, Nicholas Turner
  • Patent number: 8673980
    Abstract: This invention relates to the field of biologically active compounds and specifically to closthioamides, pharmaceutical compositions comprising these compounds, and their use as antibiotic, antifungal, and/or cytotoxic agent.
    Type: Grant
    Filed: November 2, 2010
    Date of Patent: March 18, 2014
    Assignee: Leibniz-Institut fuer Naturstoff-Forschung und Infektionsbiologie
    Inventors: Swantje Behnken, Hans-Martin Dahse, Christian Hertweck, Keishi Ishida, Thorger Lincke, Martin Roth, Florian Kloss
  • Publication number: 20130267592
    Abstract: Pro-drugs of 1-(2-halo-biphenyl-4-yl)alkanecarboxylic acids are useful for preventing and/or treating neurodegenerative diseases, improving cognitive function and treating cognitive impairment.
    Type: Application
    Filed: April 3, 2013
    Publication date: October 10, 2013
    Applicant: Chiesi Farmaceutici S.p.A.
    Inventors: Bruno Pietro IMBIMBO, Luca Raveglia
  • Publication number: 20130217753
    Abstract: The invention provides amphiphilic macromolecules that are useful for delivering nucleic acids to cells and that are useful as delivery agents for gene therapy.
    Type: Application
    Filed: March 13, 2013
    Publication date: August 22, 2013
    Applicant: Rutgers, the State University of New Jersey
    Inventor: Rutgers, the State University of New Jersey
  • Publication number: 20130177986
    Abstract: The disclosed islet isolation method comprises: an injection step of injecting a preservation solution into the pancreatic duct of an excised pancreas; a preservation step of immersing the pancreas into an immersion fluid for preservation; a digestion step of breaking down the pancreas to provide pancreatic tissue; and a purification step of immersing the pancreatic tissue in a purification solution to provide islets. The digestion step consists of: an enzyme injection step of injecting an enzyme solution containing a digestion enzyme into the pancreas; a digestion initiation step of activating the digestion enzyme; a digestion termination step of inactivating the digestion enzyme; and a collection step of collecting the broken-down pancreatic tissue.
    Type: Application
    Filed: July 13, 2011
    Publication date: July 11, 2013
    Inventors: Masahiro Tanemura, Yoshiki Sawa, Akira Myouri, Toshinori Ito, Masaki Mori, Yuichiro Doki
  • Publication number: 20130096092
    Abstract: Disclosed are inhibitors of retroviral growth of formula (I), that are useful in treatment of retroviral infections such as HIV. Also disclosed are a composition comprising a pharmaceutically acceptable carrier and at least one compound or salt of the invention, a method for inactivating a virus, a method for dissociating a metal ion from a zinc finger-containing protein, and a method for inhibiting the transmission of a virus.
    Type: Application
    Filed: June 10, 2011
    Publication date: April 18, 2013
    Applicants: Health and Human Services
    Inventors: Daniel Appella, Ettore Appella, John K. Inman, Lisa M. Miller Jenkins, Ryo Hayashi, Deyun Wang
  • Publication number: 20130072562
    Abstract: The present invention is directed to compounds that are allosteric inhibitors of tumor necrosis factor receptor I, compositions comprising such compounds, and methods of using such compounds and compositions thereof in the treatment of TNF-? mediated conditions.
    Type: Application
    Filed: October 18, 2012
    Publication date: March 21, 2013
    Applicants: CEPHALON, INC., THE TRUSTEES OF THE UNIVERSITY OF PENNSYVANIA
    Inventors: The Trustees Of The University Of Pennsyvania, Cephalon, Inc.
  • Publication number: 20130040389
    Abstract: The present invention relates to non-steroidal ligands for use in nuclear receptor-based inducible gene expression system, and a method to modulate exogenous gene expression in which an ecdysone receptor complex comprising: a DNA binding domain; a ligand binding domain; a transactivation domain; and a ligand is contacted with a DNA construct comprising: the exogenous gene and a response element; wherein the exogenous gene is under the control of the response element and binding of the DNA binding domain to the response element in the presence of the ligand results in activation or suppression of the gene.
    Type: Application
    Filed: September 5, 2012
    Publication date: February 14, 2013
    Applicant: Intrexon Coporation
    Inventors: Robert Eugene HORMANN, David W. Potter, Orestes Chortyk, Colin M. Tice, Glenn Richard Carlson, Andrew Meyer, Thomas R. Opie
  • Publication number: 20120330015
    Abstract: The present invention relates to a process for the preparation of a compound of the general Formula (I), comprising: a) reacting a compound of the general Formula (II) with a compound of the Formula III R2COOH and a compound of the general Formula IV R3NC under such conditions that compound I is formed, wherein R1 represents a substituted or unsubstituted alkyl, alkenyl, alkynyl, aromatic or non-aromatic, mono-, di- or tricyclic, or heterocyclic structure, and R2 represents a substituted or unsubstituted alkyl, alkenyl, alkynyl, aromatic or non-aromatic, mono-, di- or tricyclic, or heterocyclic structure, and R3 represents a substituted or unsubstituted alkyl, alkenyl, or alkynyl structure. In further aspect the subject invention relates to the use of the obtained products as intermediates for various peptidomimetics, and preferably as a building block in a convergent synthesis of prolyl dipeptide structures.
    Type: Application
    Filed: September 16, 2010
    Publication date: December 27, 2012
    Applicant: Vereniging voor Christelijk hoger onderwijs, wetenschappelijk onderzoek en patientenzorg
    Inventors: Eelco Ruijter, Romano Orru, Anass Znabet, Marloes Polak, Nicholas Turner
  • Publication number: 20120270940
    Abstract: This invention relates to the field of biologically active compounds and specifically to closthioamides, pharmaceutical compositions comprising these compounds, and their use as antibiotic, antifungal, and/or cytotoxic agent.
    Type: Application
    Filed: November 2, 2010
    Publication date: October 25, 2012
    Applicant: LELBUIZ-INSTITUT FUR NATURSTOFF-FORSCHUNG UND INFE
    Inventors: Swantje Behnken, Hans-Martin Dahse, Christian Hertweck, Keishi Ishida, Thorger Lincke, Martin Roth, Florian Kloss
  • Publication number: 20120197015
    Abstract: The present invention is directed to providing epoxycarboxamide compounds, azide compounds and amino alcohol compounds which serve as manufacturing intermediates that can lead to useful ?-ketoamide compounds, and the present invention is also is directed to processes for preparing ?-ketoamide compounds using the intermediates. The epoxycarboxamide compounds, azide compounds and amino alcohol compounds are represented by the following formulae: wherein R1, R2, R3, R4 and R5, as well as subvariables for one or more of R1, R2, R3, R4 and R5 are as defined herein.
    Type: Application
    Filed: December 14, 2011
    Publication date: August 2, 2012
    Applicant: Seikagaku Kogyo Kabushiki Kaisha d/b/a Seikagaku Corporation
    Inventors: Nobuo KOBAYASHI, Tsuneo Koji, Takashi Fujita, Tomofumi Nishimura, Akihiko Hosoda
  • Patent number: 8202679
    Abstract: An oxime ester compound of formula (I) useful as a photopolymerization initiator. A photopolymerization initiator having the oxime ester compound as an active ingredient is activated through efficient absorption of light of long wavelength, e.g., 405 nm or 365 nm, to exhibit high sensitivity. In formula (I), R1 and R2 are each R11, OR11, COR11, SR11, CONR12R13, or CN; R11, R12, and R13 are each hydrogen, a C1-C20 alkyl group, C6-C30 aryl group, a C7-C30 arylalkyl group, or a C2-C20 heterocyclic group; R3 and R4 are each R11, OR11, SR11, COR11, CONR12R13, NR12COR11, OCOR11, COOR11, SCOR11, OCSR11, COSR11, CSOR11, CN, halogen, or a hydroxyl group; a and b is each 0 to 4; X is oxygen, sulfur, selenium, CR31R32, CO, NR33, or PR34; and R31, R32, R33, and R34 each have the same meaning as R1.
    Type: Grant
    Filed: December 25, 2007
    Date of Patent: June 19, 2012
    Assignee: Adeka Corporation
    Inventors: Daisuke Sawamoto, Nobuhide Tominaga
  • Publication number: 20120095124
    Abstract: The present invention relates to an aminimide compound having a structure represented by the following general formula (I) in the molecule thereof, relates to a curable composition using the aminimide compound and relates to a method for curing the composition; in which R0 represents a hydrogen atom, an alkyl group which may have an optional substituent, an aryl group which may have an optional substituent, or a heterocyclic residue which may have an optional substituent. R1, R2 and R3 each independently represent a hydrogen atom, or an optional substituent. However, at least two of R1, R2 and R3 may bond to each other to form a cyclic structure.
    Type: Application
    Filed: June 16, 2010
    Publication date: April 19, 2012
    Applicant: Three Bond Co., Ltd.
    Inventor: Manabu Kirino
  • Publication number: 20120065176
    Abstract: It is reported herein that certain muscle diseases and conditions, including forms of muscular dystrophy, are characterized by impaired insulin-dependent signaling in the muscle tissue, in essence, a form of insulin resistance. The present disclosure relates to therapeutic agents, compositions and methods for treating a muscle disease or condition characterized by impaired insulin-dependent signaling by targeting components of the defective insulin signaling pathway. The disease or condition may be treated by administering a therapeutic agent that activates the insulin signaling pathway, in particular, therapeutic agents that act post-insulin receptor to modulate intracellular effector molecules. An exemplary modulator is metformin. Metformin may be administered alone or may be co-administered with another therapeutic agent for treating the muscle disease or condition, such as a corticosteroid.
    Type: Application
    Filed: May 18, 2010
    Publication date: March 15, 2012
    Inventors: Lynn Megeney, Carol Evans, Abdelmalik Slassi
  • Publication number: 20110269689
    Abstract: High penetration compositions (HPC) of a parent compound, which are capable of crossing biological barriers with high penetration efficiency. The HPCs are capable of being converted to parent drugs or parent drug-related compounds such as metabolites after crossing one or more biological barriers and thus can render treatments for the conditions that the parent drugs or parent drug-related compounds can. Additionally, the HPCs are capable of reaching areas that their parent drugs or parent drug-related compounds may not be able to access or to render a sufficient concentration at the target areas HPCs of NSAIA, for example, have demonstrated indications such as treating hair loss. A HPC can be administered to a subject through various administration routes, e.g., locally delivered to an action site of a condition with a high concentration or systematically administered to a biological subject and enter the general circulation with a faster rate.
    Type: Application
    Filed: December 4, 2009
    Publication date: November 3, 2011
    Inventor: Chongxi Yu
  • Publication number: 20110136827
    Abstract: The invention provides certain bis-acylated hydroxylamine derivative compounds, pharmaceutical compositions and kits comprising such compounds, and methods of using such compounds or pharmaceutical compositions. In particular, the invention provides methods of using such compounds or pharmaceutical compositions for treating, preventing, or delaying the onset and/or develop of a disease or condition. In some embodiments, the disease or condition is selected from cardiovascular diseases, ischemia, reperfusion injury, cancerous disease, pulmonary hypertension and conditions responsive to nitroxyl therapy.
    Type: Application
    Filed: December 7, 2010
    Publication date: June 9, 2011
    Inventors: John P. Toscano, Art Sutton, Vincent J. Kalish, Frederick Arthur Brookfield, Stephen Martin Courtney, Lisa Marie Frost
  • Publication number: 20110118116
    Abstract: The present invention relates to azolin-2-ylamino compounds of formula (I), wherein A is a radical of the formulae (A.1) or (A.2), wherein * denotes the binding site and wherein the indices and variables are as defined in the description. The present invention relates as well as to the precursor compounds thereof, which are both useful for combating animal pests selected from insects, arachnids and nematodes. The invention also relates to methods for controlling and/or combating such animal pests by using these compounds, to methods of protecting crops and plant propargation material, and further also to seeds and agricultural and veterinary composition comprising said compounds.
    Type: Application
    Filed: July 14, 2009
    Publication date: May 19, 2011
    Inventors: Ronan Le Vezouet, Markus Kordes, Ralph Paulini, Deborah L. Culbertson
  • Publication number: 20110071056
    Abstract: Methods and compositions are provided that include degradable gemini surfactants including degradable gemini surfactants. Methods of use include subterranean operations, especially those involving the placement of resin systems, formation of emulsions (e.g., emulsified acids, emulsified fracturing fluids, drilling fluids, etc.), and in the formation of surfactant gelled fluids. Such treatments include, but are not limited to, drilling, stimulation treatments (e.g., fracturing treatments, acidizing treatments), and completion operations (e.g., sand control treatments like gravel packing).
    Type: Application
    Filed: September 24, 2009
    Publication date: March 24, 2011
    Inventors: Rajesh K Saini, Narongsak Tonmukayakul, Thomas D. Welton, Jason E. Bryant, Sherry G. Gaskins
  • Publication number: 20110014699
    Abstract: Embodiments of the present disclosure provide for prostratin analogs, bryostatin analogs, prodrugs of prostratin and prostratin analogs, methods of making prostratin analogs, and methods of making prodrugs of prostratin and prostratin analogs, methods of use of prostratin analogs, bryostatin analogs, and prodrugs thereof, and the like.
    Type: Application
    Filed: July 20, 2010
    Publication date: January 20, 2011
    Inventors: Paul A. Wender, Lars V. Heumann, Rainer Kramer, Carolyn Gauntlett, Elizabeth Mieuli, Dennis Fournogerakis, Pierre-Luc Boudreault, Adam Schrier, Brian DeChristopher
  • Publication number: 20110008634
    Abstract: A rust inhibitor usable for metal surface coating includes, as an effective component, a compound containing a chelate group, and a long chain alkyl group and/or a cyclic alkyl group, which are bonded by an ester bond or other bonds.
    Type: Application
    Filed: July 2, 2009
    Publication date: January 13, 2011
    Applicants: AUTONETWORKS TECHNOLOGIES, LTD., SUMITOMO WIRING SYSTEMS, LTD., SUMITOMO ELECTRIC INDUSTRIES, LTD., KYUSHU UNIVERSITY
    Inventors: Tatsuya Hase, Makoto Mizoguchi
  • Patent number: 7851505
    Abstract: The current invention provides novel thiotungstate derivatives, methods of making novel thiotungstate derivatives, pharmaceutical compositions of novel thiotungstate derivatives, methods of using novel thiotungstate derivatives to treat diseases associated with aberrant vascularization, copper metabolism disorders and obesity and methods of using pharmaceutical compositions of thiotungstate derivatives to treat diseases associated with aberrant vascularization, copper metabolism disorders, neurodegenerative disorders, obesity or NF-?B dysregulation.
    Type: Grant
    Filed: May 27, 2004
    Date of Patent: December 14, 2010
    Assignee: Attenuon, LLC
    Inventors: Robert J. Ternansky, Patricia L. Gladstone, Amy L. Allan, Melissa L. P. Price, Andrew Mazar
  • Publication number: 20100249262
    Abstract: An oxime ester compound of formula (I) useful as a photopolymerization initiator. A photopolymerization initiator having the oxime ester compound as an active ingredient is activated through efficient absorption of light of long wavelength, e.g., 405 nm or 365 nm, to exhibit high sensitivity. In formula (I), R1 and R2 are each R11, OR11, COR11, SR11, CONR12R13, or CN; R11, R12, and R13 are each hydrogen, a C1-C20 alkyl group, C6-C30 aryl group, a C7-C30 arylalkyl group, or a C2-C20 heterocyclic group; R3 and R4 are each R11, OR11, SR11, COR11, CONR12R13, NR12COR11, OCOR11, COOR11, SCOR11, OCSR11, COSR11, CSOR11, CN, halogen, or a hydroxyl group; a and b is each 0 to 4; X is oxygen, sulfur, selenium, CR31R32, CO, NR33, or PR34; and R31, R32, R33, and R34 each have the same meaning as R1.
    Type: Application
    Filed: December 25, 2007
    Publication date: September 30, 2010
    Applicant: ADEKA CORPORATION
    Inventors: Daisuke Sawamoto, Nobuhide Tominaga
  • Publication number: 20100222583
    Abstract: Transition metal complexes include a diazaphosphacycle of formula III and a transition metal. The phosphorus atom of the diazaphosphacycle is bonded to the transition metal and the diazaphosphacycle of formula III has the following structure where the variables have the values set forth herein.
    Type: Application
    Filed: May 5, 2010
    Publication date: September 2, 2010
    Inventors: Clark R. Landis, Wiechang Jin, Jonathan S. Owen, Thomas P. Clark
  • Publication number: 20100207078
    Abstract: The present invention provides novel compositions suitable for use in an intermolecular photodeprotection reaction scheme. Such compositions include a chromophore compound and a second compound having a photocleavable group bonded to a protected functional group. Novel compounds which can used in intramolecular photodeprotection are also provided. These compounds have a chromophore moiety bonded to a photocleavable group, which itself is bonded to a protected group. The compounds and compositions disclosed herein can be used in two-photon and multi-photon excitation.
    Type: Application
    Filed: July 12, 2007
    Publication date: August 19, 2010
    Inventors: Seth Marder, Stephen Barlow, Joseph Perry, Jing Wang
  • Patent number: 7763747
    Abstract: Bis- and tris-dihydroxyaryl compounds and their methylenedioxy analogs and pharmaceutically acceptable esters, their synthesis, pharmaceutical compositions containing them, and their use in the treatment of amyloid diseases, especially A? amyloidosis, such as observed in Alzheimer's disease, IAPP amyloidosis, such as observed in type 2 diabetes, and synucleinopathies, such as observed in Parkinson's disease, and the manufacture of medicaments for such treatment.
    Type: Grant
    Filed: November 4, 2008
    Date of Patent: July 27, 2010
    Assignee: Proteotech, Inc.
    Inventors: Alan D. Snow, Beth P. Nguyen, Gerardo M. Castillo, Virginia J. Sanders, Thomas P. Lake, Lesley Larsen, Rex T. Weavers, Stephen D. Lorimer, David S. Larsen, David L. Coffen, Charlotte Coffen, legal representative
  • Publication number: 20100167927
    Abstract: The invention relates to substituted amino-thiourea compounds of formula (I), to the enantiomers, diastereomers and salts thereof and to compositions comprising such compounds. The invention also relates to the use of the substituted amino-thiourea compounds, of their salts or of compositions comprising them for combating animal pests. Furthermore the invention relates also to methods of applying such compounds. The substituted amino-thiourea compounds are defined by the following formula (I): wherein A, B, R1, R2, R3, R4, R5.1, R5.2 and R6 are defined as in the description.
    Type: Application
    Filed: May 13, 2008
    Publication date: July 1, 2010
    Applicant: BASF SE
    Inventors: Christopher Koradin, Markus Kordes, Ernst Baumann, Ronan Le Vezouet, Deborah L. Culbertson
  • Publication number: 20090114879
    Abstract: The present invention relates to the use of a specific group of alkoxylated and/or acylated non-quaternary nitrogen-containing compounds as anti-agglomerants for gas hydrates. The anti-agglomerants are surface-active non-quaternary nitrogen-containing compounds with 1-5 nitrogen atoms, which compounds have at least one hydrophobic group with 6-24 carbon atoms, and where the hydrophobic group is connected to the remainder of the molecule by an amine moiety, an ether moiety or an amide moiety, provided that when the hydrophobic group is connected by means of an amide moiety to the remainder of the molecule, the compounds must contain a total of at least two nitrogen atoms, and optionally contain 1-12 —CH2CH2O— groups and/or 1-6 hydroxyalkyl groups with 3-4 carbon atoms; and which compounds have at least one C2-C3 acyl group and/or at least one hydroxyalkyl group with 3-4 carbon atoms; or a salt thereof.
    Type: Application
    Filed: March 16, 2007
    Publication date: May 7, 2009
    Applicant: AKZO NOBEL N.V.
    Inventors: Martin Hellsten, Hans Oskarsson
  • Patent number: 7459585
    Abstract: The present invention provides an AP-1 activation inhibitor, NF-kappa B activation inhibitor, inflammatory cytokine production inhibitor, matrix metalloprotease production inhibitor, inflammatory cell adhesion molecule expression inhibitor, anti-inflammatory agent, antirheumatic agent, immunosuppressant, cancer metastasis inhibitor, remedy for arteriosclerosis and antiviral agent which contain the benzene derivative of the following general formula (I) or a pharmaceutically acceptable salt thereof as an active ingredient.
    Type: Grant
    Filed: March 24, 2005
    Date of Patent: December 2, 2008
    Assignee: Ajinomoto Co., Inc.
    Inventors: Yukio Iino, Kohichi Fujita, Takashi Tsuji, Ariko Kodaira, Kenji Takehana, Tsuyoshi Kobayashi, Takashi Yamamoto
  • Patent number: 7320998
    Abstract: The present invention provides carbohydrate analogs of the formula: wherein X is CH2, O, or NH, and R1-8 are independently H, a short hydrocarbon, a substituted amine, an alcohol, a substituted ether, a substituted amide, a substituted ketone, a substituted carboxylic acid, a short peptide, or a short oligosaccharide, Y is H, a short hydrocarbon, a short peptide, or a short oligosaccharide, and R9 is H, a short hydrocarbon, a substituted amine, an alcohol, a substituted ether, a substituted amide, a substituted ketone, a carboxylic acid, a short peptide, or a short oligosaccharide.
    Type: Grant
    Filed: July 9, 2004
    Date of Patent: January 22, 2008
    Assignee: Chymos Corporation
    Inventors: Stephen S. Rothman, Edmund J. Niedzinskl
  • Patent number: 7253210
    Abstract: This invention provides a class of androgen receptor targeting agents (ARTA). The agents define a new subclass of compounds, which are selective androgen receptor modulators (SARM). Several of the SARM compounds have been found to have an unexpected androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor. Other SARM compounds have been found to have an unexpected antiandrogenic activity of a nonsteroidal ligand for the androgen receptor.
    Type: Grant
    Filed: October 14, 2003
    Date of Patent: August 7, 2007
    Assignee: University of Tennessee Research Foundation
    Inventors: James T. Dalton, Duane D. Miller, Igor Rakov
  • Patent number: 7220781
    Abstract: Compounds of formula I in which R1, R2, R3, each X, L, Y, Cy, Lp, D and n have the meanings as set out in the specification, and corresponding compounds in which the unsubstituted or substituted amidine group is replaced with an unsubstituted or substituted aminomethyl group, are useful as serine protease inhibitors.
    Type: Grant
    Filed: January 8, 2004
    Date of Patent: May 22, 2007
    Assignee: Tularik Limited
    Inventors: John Walter Liebeschuetz, William Alexander Wylie, Bohdan Waszkowycz, Christopher William Murray, Andrew David Rimmer, Pauline Mary Welsh, Stuart Donald Jones, Jonathan Michael Ernest Roscoe, Stephen Clinton Young, Phillip John Morgan
  • Patent number: 7034015
    Abstract: The invention relates to a novel class of aminobenzophenones derivatives, to pharmaceutical preparations comprising said compounds, to dosage units of such preparations, to methods of treating patients comprising administering said compounds, and to the use of said compounds in the manufacture of pharmaceutical preparations.
    Type: Grant
    Filed: August 28, 2002
    Date of Patent: April 25, 2006
    Assignee: Leo Pharma A/S
    Inventors: Erik Rytter Ottosen, Anne Marie Horneman, Xifu Liang
  • Patent number: 6852738
    Abstract: A class of acyl sulfamides comprises compounds that are potent ligands for PPAR gamma and generally have antagonist or partial agonist activity. The compounds may be useful in the treatment, control or prevention of obesity, non-insulin dependent diabetes mellitus (NIDDM), hyperglycemia, dyslipidemia, hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, atherosclerosis, vascular restenosis, inflammation, and other PPAR gamma mediated diseases, disorders and conditions.
    Type: Grant
    Filed: January 25, 2002
    Date of Patent: February 8, 2005
    Assignee: Merck & Co., Inc.
    Inventors: A. Brian Jones, John J. Acton, III
  • Patent number: 6849626
    Abstract: The invention relates to semicarbazides of the general formula I where R1, R2, R3, R4 and I have the meaning indicated in claim 1. The compounds of the formula I can be employed as pharmaceutical active compounds in human and veterinary medicine, in particular for the control and prevention of thromboembolic disorders such as thrombosis, mycocardial infarct, arteriosclerosis, inflammation, apoplexy, angina pectoris, restenosis after angioplasty and intermittent claudication.
    Type: Grant
    Filed: August 21, 2001
    Date of Patent: February 1, 2005
    Assignee: Merck Patent GmbH
    Inventors: Werner Mederski, Horst Juraszyk, Dieter Dorsch, Christos Tsaklakidis, Johannes Gleiltz, Christopher Barnes
  • Patent number: 6767922
    Abstract: This invention relates to novel compounds of Formula (I) to (VII), and compositions thereof, useful in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).
    Type: Grant
    Filed: September 6, 2002
    Date of Patent: July 27, 2004
    Assignee: SmithKline Beecham Corporation
    Inventors: Katherine Louisa Widdowson, Qi Jin
  • Patent number: 6740682
    Abstract: The novel compound 3-amidinobenzoyl-D-phenylglycine-3-phenylanilide is useful as a serine protease inhibitor.
    Type: Grant
    Filed: November 19, 2001
    Date of Patent: May 25, 2004
    Assignee: Tularik Limited
    Inventor: John Walter Liebeschuetz
  • Publication number: 20040063786
    Abstract: The present invention is related to new vanilloid analogues containing resiniferatoxin pharmacophores, pharmaceutical compositions that have such analogues, and their uses as vanilloid receptor agonists and potent analgesics. The present invention provides a pharmaceutical composition for preventing, alleviating or treating pain, acute pain, chronic pain, neuropathic pain, post-operative pain, migraine, arthralgia, neutopathies, nerve injury, diabetic neuropathy, neurodegeneration, neurotic skin disorder, stroke, urinary bladder hypersensitiveness, irritable bowel syndrome, a respiratory disorder such as asthma or chronic obstructive pulmonary disease, irritation of skin, eye or mucous membrane, fervescence, stomach-duodenal ulcer, inflammatory bowel disease, inflammatory disease or urgent urinary incontinence.
    Type: Application
    Filed: December 18, 2002
    Publication date: April 1, 2004
    Inventor: Jee Woo Lee
  • Patent number: 6703379
    Abstract: The present invention provides an AP-1 activation inhibitor, NF-kappa B activation inhibitor, inflammatory cytokine production inhibitor, matrix metalloprotease production inhibitor, inflammatory cell adhesion molecule expression inhibitor, anti-inflammatory agent, antirheumatic agent, immunosuppressant, cancer metastasis inhibitor, remedy for arteriosclerosis and antiviral agent which contain the benzene derivative of the following general formula (I) or a pharmaceutically acceptable salt thereof as an active ingredient.
    Type: Grant
    Filed: March 12, 2001
    Date of Patent: March 9, 2004
    Assignee: Ajinomoto Co., Inc.
    Inventors: Yukio Iino, Kohichi Fujita, Takashi Tsuji, Ariko Kodaira, Kenji Takehana, Tsuyoshi Kobayashi, Takashi Yamamoto
  • Publication number: 20030092746
    Abstract: Compounds of Formula I are antagonists of VLA-4 and/or &agr;4&bgr;7, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds may be formulated into pharmaceutical compositions and are suitable for use in the treatment of AIDS-related dementia, allergic conjunctivitis, allergic rhinitis, Alzheimer's disease, asthma, atherosclerosis, autologous bone marrow transplantation, certain types of toxic and immune-based nephritis, contact dermal hypersensitivity, inflammatory bowel disease including ulcerative colitis and Crohn's disease, inflammatory lung diseases, inflammatory sequelae of viral infections, meningitis, multiple sclerosis, multiple myeloma, myocarditis, organ transplantation, psoriasis, pulmonary fibrosis, restenosis, retinitis, rheumatoid arthritis, septic arthritis, stroke, tumor metastasis, uveititis, and type I diabetes.
    Type: Application
    Filed: May 21, 2001
    Publication date: May 15, 2003
    Inventors: William K. Hagmann, Stephen E. DeLaszlo, Theodore Kamenecka, Malcolm MacCoss
  • Patent number: 6534542
    Abstract: Compounds of formula (i) and of formula (ii) wherein the symbols have the meaning disclosed in the specification, specifically or selectively modulate &agr;2B and/or &agr;2C adrenergic receptors in preference over &agr;2A adrenergic receptors, and as such are useful for alleviating chronic pain and allodynia and have no or only minimal cardivascular and/or sedatory activity.
    Type: Grant
    Filed: February 27, 2001
    Date of Patent: March 18, 2003
    Assignee: Allergen Sales, Inc.
    Inventors: Ken Chow, Daniel W. Gil, Wenkui Ken Fang, Michael E. Garst
  • Patent number: 6444702
    Abstract: The present invention provides novel aminoadamantane derivatives, methods of making the derivatives, compositions including the novel aminoadamantane derivatives, and methods for the treatment and prevention of neurological diseases using the derivatives and compositions.
    Type: Grant
    Filed: February 22, 2000
    Date of Patent: September 3, 2002
    Assignee: NeuroMolecular, Inc.
    Inventors: Yuqiang Wang, Wenqing Ye, James W. Larrick, Jonathan S. Stemler, Stuart A. Lipton
  • Patent number: 6323227
    Abstract: This invention relates to compounds of formula which inhibit Factor Xa, to pharmaceutical compositions containing the compounds, and to the use of the compounds for the treatment of patients suffering from conditions which can be ameliorated by the administration of an inhibitor of Factor Xa.
    Type: Grant
    Filed: February 26, 1999
    Date of Patent: November 27, 2001
    Assignee: Aventis Pharmaceuticals Products Inc.
    Inventors: Scott I. Klein, Kevin R. Guertin, Alfred P. Spada, Heinz W. Pauls, Yong Gong, Daniel G. McGarry
  • Patent number: 6225334
    Abstract: The invention concerns novel glyoxylic acid derivatives, a process for their preparation and their use as pesticides.
    Type: Grant
    Filed: January 11, 1999
    Date of Patent: May 1, 2001
    Assignee: Bayer Aktiengesellschaft
    Inventors: Thomas Seitz, Klaus Stenzel, Ulrike Wachendorff-Neumann