Plural Chalcogens Bonded Directly To The Five-membered Hetero Ring By Nonionic Bonding Patents (Class 514/425)
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Patent number: 8664259Abstract: New, oil-based suspension concentrates composed of at least one room-temperature-solid compound of the formula (I?), at least one penetrant, at least one vegetable oil, at least one nonionic surfactant and/or at least one anionic surfactant, and optionally one or more additives from the groups of the emulsifiers, foam inhibitors, preservatives, antioxidants, colorants and/or inert filler materials, a process for producing these suspension concentrates, and their use for applying the active substances comprised.Type: GrantFiled: March 4, 2005Date of Patent: March 4, 2014Assignee: Bayer CropScience AGInventors: Reiner Fischer, Udo Reckmann, Ronald Vermeer
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Patent number: 8664255Abstract: The present invention provides aryl- or heteroaryl-diketo acid compounds effective to inhibit an activity of a Mycobacterial malate synthase enzyme or to inhibit a malate synthase activity in other bacteria having the enzyme. The compounds may be phenyl- naphthyl-, or thienyl-substituted diketo acids and carboxylate derivatives thereof. Also provided are methods of treating tuberculosis or other pathophysiological conditions associated with a malate synthase enzyme with the inhibitory compounds and methods of in silico design of the inhibitory compounds. In addition, the present invention provides the inhibitory compounds designed by this method. Furthermore, three-dimensional X-ray crystal structures of the Mycobacterial malate synthase complexed with the inhibitory compounds are provided. Further still a method for stabilizing an aromatic or heteroaromatic diketo acid or its prodrug or close analog in solution by derivatizing at least the ortho position on the aromatic ring is provided.Type: GrantFiled: October 20, 2009Date of Patent: March 4, 2014Assignee: The Texas A&M University SystemInventors: Joel S. Freundlich, James C. Sacchettini, Inna V. Kriger, Thomas R. Ioerger, Vijay Gawandi
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Patent number: 8658690Abstract: Disclosed herein are isolated compounds or pharmaceutically acceptable salts thereof, which exhibit immunostimulatory or anti-inflammatory effects. The compounds are isolated from the fruiting body of A. camphorata in a solid culture. Also disclosed are methods of stimulating immune responses and/or treating an inflammatory disorder with these compounds and pharmaceutical compositions including the compounds or pharmaceutically acceptable salts thereof.Type: GrantFiled: February 16, 2012Date of Patent: February 25, 2014Assignee: Well Shine Biotechnology Development Co., Ltd.Inventors: Yueh-Hsiung Kuo, Bi-Fong Lin
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Publication number: 20140045689Abstract: The present invention relates to the use of 3,4-disubstituted pyrrole 2,5-diones of the formula I as defined in the description for controlling phytopathogenic fungi. Further the invention relates to novel compounds of the formula I.Type: ApplicationFiled: April 19, 2012Publication date: February 13, 2014Inventors: Richard Riggs, Jochen Dietz, Wassilios Grammenos, Bernd Mueller, Jan Klaas Lohmann, Nadege Boudet, Ian Robert Craig, Egon Haden, Jurith Montag
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Patent number: 8629084Abstract: The invention relates to novel iodophenyl-substituted cyclic ketenols of the formula (I) in which CKE, J, X and Y are as defined above, to a plurality of processes and intermediates for their preparation and to their use as pesticides and/or herbicides, and also to selective herbicidal compositions comprising firstly iodophenyl-substituted cyclic ketonols of the formula (I) and secondly at least one crop plant compatibility-improving compound.Type: GrantFiled: September 13, 2005Date of Patent: January 14, 2014Assignee: Bayer CropScience AGInventors: Reiner Fischer, Thomas Bretschneider, Kerstin Ilg, Stefan Lehr, Dieter Feucht, Olga Malsam, Udo Reckmann, Guido Bojack, Christian Arnold, Thomas Auler, Martin Jeffrey Hills, Heinz Kehne, Waltraud Hempel, Erich Sanwald
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Publication number: 20140011772Abstract: The present invention relates to compositions and methods for the treating and empirically investigating conditions associated with neuronal dysfunction (e.g., chronic pain, epileptic neuronal activity). In particular, the present invention provides compositions and methods for using flufenamic acid in the treatment and empirical investigation of conditions associated with neuronal dysfunction (e.g., chronic pain, epileptic neuronal activity).Type: ApplicationFiled: June 13, 2013Publication date: January 9, 2014Applicant: NORTHWESTERN UNIVERSITYInventors: Marco Martina, A. Vania Apkarian
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Publication number: 20140005248Abstract: The present invention relates to novel compounds of formula (I): wherein X is selected from hydrogen, a halogen, or a substituent. and R is selected from hydrogen, a halogen, phenyl , aryl as specified and Y is selected from H, hydroxy, as specified and R1 is selected from H, methyl , alkyl, C1-18 straight, branched or cyclic, saturated, unsaturated and aromatic hydrocarbyl groups, which aromatic groups may be heterocyclic, cyclic or acyclic and which may optionally be substituted by alkyl, alkynyloxycarbonyl, aryl, benzyl, arlyoxy, arylcarbonyl, aryloxycarbonyl, sulphur equivalents of said oxy, carbonyl and oxycarbonyl moieties, and oxo as specified. The invention also relates to their uses as CCK receptor ligands and CCK antagonists and their medicinal applications.Type: ApplicationFiled: July 2, 2012Publication date: January 2, 2014Inventors: Padijarethakkal N Balaram, Pornthip Lattmann
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Publication number: 20140005176Abstract: Provided herein are 2-phenoxy- and 2-phenylsulfonamide derivatives with CCR3 antagonistic activity. These compounds are useful for the treatment of diseases associated with CCR3 activity, including but not limited to, atopic dermatitis, allergic rhinitis, rheumatoid arthritis, Grave's disease, HIV infection, Alzheimer's disease, atherosclerosis and other inflammatory and/or immunological disorders.Type: ApplicationFiled: August 26, 2013Publication date: January 2, 2014Applicant: AXIKIN PHARMACEUTICALS, INC.Inventors: Yingfu Li, Kevin Bacon, Hiromi Sugimoto, Keiko Fukushima, Kentaro Hashimoto, Makiko Marumo, Toshiya Moriwaki, Noriko Nunami, Naoki Tsuno, Klaus Urbahns, Nagahiro Yoshida
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Publication number: 20130324514Abstract: The present invention relates to compounds of general formula I, wherein the groups R1, R2, R3, m and n are defined as in claim 1, which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2. Furthermore, the invention relates to novel intermediates, useful for the synthesis of compounds of formula I.Type: ApplicationFiled: May 22, 2013Publication date: December 5, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Dieter HAMPRECHT, Sara FRATTINI, Iain LINGARD, Stefan PETERS
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Publication number: 20130316906Abstract: The invention relates to novel compounds of the formula (I) in which R1, R2, R3, R4, R5, Y, Q and G have the meanings given above, to a plurality of processes and intermediates for their preparation and to their use as herbicides and/or pesticides. Moreover, the invention relates to selective herbicidal compositions comprising, firstly, the phenyl-substituted bicyclooctane-1,3-dione derivates and, secondly, a crop plant compatibility-improving compound. The present invention furthermore relates to increasing the activity of crop protection compositions comprising in particular phenyl-substituted bicyclooctane-1,3-dione derivates by adding ammonium salts or phosphonium salts and, if appropriate, penetrants, to the corresponding compositions, to processes for their preparation and to their use in crop protection as pesticides and/or for preventing unwanted plant growth.Type: ApplicationFiled: October 28, 2011Publication date: November 28, 2013Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Alfred Angermann, Stefan Lehr, Guido Bojack, Reiner Fischer, Isolde Häuser-hahn, Ines Heinemann, Elmar Gatzweiler, Christopher Hugh Rosinger, Arnd Voerste, Dieter Feucht
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Publication number: 20130315981Abstract: The present invention is a method of increasing lipolysis in an adipose tissue of a mammal comprising delivering to macrophages at the adipose tissue of the mammal an effective amount of an agent which reduces the concentration of macrophages at the adipose tissue of the mammal, thereby increasing lipolysis in the adipose tissue of the mammal.Type: ApplicationFiled: June 22, 2011Publication date: November 28, 2013Applicant: The Trustees of Columbia University in the City of New YorkInventors: Anthony W. Ferrante, JR., Aliki Kosteli
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Publication number: 20130296398Abstract: The invention relates to the use of cannabidiol (CBD), at a dose of greater than 300 mg/day, in combination with a standard anti-epileptic drug (SAED) which acts via sodium or calcium channels, for use in the treatment of epilepsy. The SAED is preferably one which•modifies low-threshold or transient neuronal calcium currents,or•reduces high-frequency neuronal firing and sodium-dependent action potentials and enhances GABA effects. Preferred SAEDs are ethosuximide and valproate.Type: ApplicationFiled: January 3, 2012Publication date: November 7, 2013Applicants: Otsuka Pharmaceutical Co., Limited, GW Pharma LimitedInventors: Ben Whalley, Claire Williams, Gary Stephens
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Publication number: 20130281507Abstract: The invention relates to compounds of formula (I): The invention likewise relates to a cosmetic method for depigmenting, lightening and/or whitening keratin materials, more particularly the skin, that utilizes these compoundsType: ApplicationFiled: November 23, 2011Publication date: October 24, 2013Applicant: L'OREALInventor: Xavier Marat
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Patent number: 8546419Abstract: The present invention relates to conjugate comprising a carrier substituted with one or more occurrences of a moiety having the structure: wherein each occurrence of M is independently a modifier having a molecular weight ?10 kDa; denotes direct of indirect attachment of M to linker LM; and each occurrence of LM is independently an optionally substituted succinamide-containing linker, whereby the modifier M is directly or indirectly attached to the succinamide linker through an amide bond, and the carrier is linked directly or indirectly to each occurrence of the succinamide linker through an ester bond. In another aspect, the invention provides compositions comprising the conjugates, methods for their preparation, and methods of use thereof in the treatment of various disorder, including, but not limited to cancer.Type: GrantFiled: July 19, 2012Date of Patent: October 1, 2013Assignee: The General Hospital CorporationInventors: Mikhail I. Papisov, Alexander Yurkovetskiy
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Patent number: 8530426Abstract: The invention relates to topical use of at least one UGT inducer for the preparation of a cosmetic or dermopharmaceutical composition comprising a dermatologically acceptable carrier to protect and/or enhance the state of the skin and prevent and/or treat imperfections of the skin.Type: GrantFiled: April 25, 2005Date of Patent: September 10, 2013Assignee: Sederma SASInventors: Karl Lintner, Claire Mas Chamberlin
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Publication number: 20130231323Abstract: Disclosed are compounds of formulae (I), (II), and (II)I: and pharmaceutically acceptable salts thereof, wherein the variables, R, R1, R2, R3, R101, L, D, Q, Y, X, and Z are defined herein. These compounds are useful for treating Gram-negative bacteria infections.Type: ApplicationFiled: September 6, 2011Publication date: September 5, 2013Applicant: DUKE UNIVERSITYInventors: Pei Zhou, Eric J. Toone
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Publication number: 20130225649Abstract: The present invention relates to compounds from Antrodia cinnamomea. The present invention also relates to a composition and a method for treating or prophylaxis of hepatitis C virus (HCV) or human immunodeficiency virus (HIV) infection.Type: ApplicationFiled: October 17, 2012Publication date: August 29, 2013Applicant: SIMPSON BIOTECH CO., LTD.Inventor: SIMPSON BIOTECH CO., LTD.
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Patent number: 8518985Abstract: The invention relates to novel compounds of the formula (I), in which W, X, Y, Z and CKE are each as defined above, to several methods and intermediates for preparation thereof and to the use thereof as pesticides and/or herbicides. The invention also relates to selective herbicidal compositions which comprise firstly haloalkylmethyleneoxyphenyl-substituted ketoenols and secondly a compound which improves crop plant compatibility. The present invention further relates to the enhancement of the action of crop protection compositions comprising especially haloalkylmethyleneoxyphenyl-substituted ketoenols, by the addition of ammonium or phosphonium salts and optionally penetration enhancers, to the corresponding compositions, to methods for production thereof and to the use thereof in crop protection as insecticides and/or acaricides and/or for preventing undesired plant growth.Type: GrantFiled: March 11, 2010Date of Patent: August 27, 2013Assignee: Bayer CropScience AGInventors: Reiner Fischer, Thomas Bretschneider, Stefan Lehr, Eva-Maria Franken, Olga Malsam, Arnd Voerste, Ulrich Gorgens, Jan Dittgen, Dieter Feucht, Isolde Hauser-Hahn, Christopher Hugh Rosinger, Alfred Angermann
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Patent number: 8507537Abstract: The present invention relates to novel trifluoromethoxyphenyl-substituted tetramic acid derivatives of the formula (I), in which J, X, Y, A, B, D and G have the meanings given above, to a number of processes for their preparation, and to their use as pesticides and/or herbicides. The invention further provides selective herbicidal compositions which comprise, firstly, trifluoromethoxyphenyl-substituted tetramic acid derivatives and, secondly, a crop plant compatibility-improving compound. The invention further relates to the boosting of the action of crop protection compositions comprising compounds of the formula (I) through the additions of ammonium salts or phosphonium salts and optionally penetrants.Type: GrantFiled: October 13, 2007Date of Patent: August 13, 2013Assignee: Bayer CropScience AGInventors: Reiner Fischer, Stefan Lehr, Christian Arnold, Thomas Auler, Jan Dittgen, Dieter Feucht, Eva-Maria Franken, Waltraud Hempel, Martin Jeffrey Hills, Heinz Kehne, Peter Losel, Olga Malsam, Christopher Hugh Rosinger, Erich Sanwald, Ulrich Gorgens, Stefan Antons, Wolfgang Ebenbeck, Axel Pleschke, Marielouise Schneider, Ralf Wischnat
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Publication number: 20130197059Abstract: The invention relates to compounds of formula I: wherein R1, R2, and n are defined in the detailed description and claims. In particular, the present invention relates to the compounds of formula I for use in the manufacture and delivery of conjugated moieties such as small molecules, peptides, nucleic acids, fluorescent moieties, and polymers which are linked to LFA-1 integrin antagonists to target cells expressing LFA-1.Type: ApplicationFiled: January 24, 2013Publication date: August 1, 2013Applicant: Hoffmann-La Roche Inc.Inventor: Hoffmann-La Roche Inc.
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Publication number: 20130190377Abstract: The present invention relates to novel lactams of formulae (I) and (II). The present invention further relates to the use of these compounds in the treatment of microbial infections and microbial contamination of surfaces, particularly infections and surface contaminations characterised by biofilm formation. Further provided are compounds of formula (I) and (II) substituted with acrylate or methacrylate groups and their attachment to surfaces or polymers to inhibit microbial contamination.Type: ApplicationFiled: January 24, 2007Publication date: July 25, 2013Applicant: BIOSIGNAL LIMITEDInventors: Naresh Kumar, George Iskander
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Publication number: 20130184321Abstract: The present invention relates to an Attention deficit and hyperactivity disorder (ADHD) mouse model and a screening method for a composition for the prevention and treatment of attention deficit disease. The mouse model constructed by inserting cobalt wire in the right side of the frontal lobe is very useful as the ADHD mouse model, and the said ADHD mouse model can be effectively used for the screening of an agent for the treatment of attention deficit disease since the mouse demonstrated brain wave with low frequency, hyperactivity, and cognitive impairment, which are characteristic symptoms of attention deficit disease, when ethosuximide, one of T-type calcium channel blockers, was administered. Therefore, the composition comprising a T-type calcium channel blocker was also confirmed to be effectively used for the prevention and treatment of attention deficit disease.Type: ApplicationFiled: January 21, 2011Publication date: July 18, 2013Applicant: KOREA ADVANCED INSTITUTE OF SCIENCE AND TECHNOLOGYInventors: Daesoo Kim, Jeongjin Kim
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Publication number: 20130150281Abstract: A cascade carrier linked prodrug is described comprising a biologically active moiety and a masking group having at least one nucleophile and being distinct from the carrier.Type: ApplicationFiled: February 5, 2013Publication date: June 13, 2013Applicant: Ascendis Pharma GmbHInventor: Ascendis Pharma GmbH
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Publication number: 20130143858Abstract: The invention relates to compounds according to Formula I: or a pharmaceutically acceptable salt thereof, wherein m, n, R1, R2, R3, R4, R5, x and y are as defined herein. Compounds according to Formula I are pharmacologically effective as potassium channel inhibitors, in particular inhibitors of the acetylcholine operated inward rectifying potassium channel current (i.e. IKACh blockers), and are believed to be useful in the treatment of cardiac arrhythmias, in particular supraventricular tacharrhythmias, such as atrial fibrillation and atrial flutter.Type: ApplicationFiled: January 28, 2013Publication date: June 6, 2013Applicant: ASTRAZENECA ABInventor: AstraZeneca AB
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Publication number: 20130129772Abstract: The present invention relates to a method of preventing or ameliorating the symptoms of arthritis or preventing or ameliorating cartilage destruction or chondrocyte death in a subject suffered from arthritis, comprising administrating the subject an effective amount of an active component selected from a compound, a mixture, and a mycelium prepared from Antrodia cinnamomea.Type: ApplicationFiled: November 19, 2012Publication date: May 23, 2013Applicant: SIMPSON BIOTECH CO., LTD.Inventors: Wei-Tso Chia, Chia-Chin Sheu
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Publication number: 20130109735Abstract: Salacinol and ponkoranol homologues, derivatives thereof and methods of synthesizing and using said homologies and derivatives. The derivatives include stereoisomers, de-O-sulfonated compounds and congeners of the naturally occurring homologues. Some of the derivatives exhibit enhanced glucosidase inhibitory bioactivity in comparison to the naturally occurring compounds which have been isolated from Salacia reticulata.Type: ApplicationFiled: December 1, 2010Publication date: May 2, 2013Applicant: SIMON FRASER UNIVERSITYInventors: Brian Mario Pinto, Sankar Mohan, Ravindranath Nasi, Jayakanthan Kumarasamy, Razieh Eskarandi
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Publication number: 20130102591Abstract: The invention provides compositions and methods for prevention, treatment, or management of pulmonary hypertension using piperidine, pyrrolidine, or azepane derivatives comprising one to four nitric oxide (NO) donor groups and a reactive oxygen species (ROS) degradation catalyst. The invention further provides a water dispersible powder comprising nanoparticles comprising said derivatives, as well as pharmaceutical compositions thereof and methods of use.Type: ApplicationFiled: January 26, 2011Publication date: April 25, 2013Inventors: Andrew Lurie Salzman, Shlomo Magdassi, Katrin Margulis-Goshen
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Publication number: 20130095110Abstract: The present invention is directed to KIAA1199, which is a novel factor involved in decomposition of hyaluronic acid, and to use thereof. More specifically, the invention is directed to a hyaluronic acid decomposition-promoting agent containing the KIAA1199 gene and a protein encoded by the gene; to a hyaluronic acid decomposition-inhibiting agent characterized by inhibiting the activity or expression thereof (including an siRNA or a monoclonal antibody); and to a method for screening a novel hyaluronic acid decomposition-controlling agent, in which the method contains employing the expression of KIAA1199 as an index.Type: ApplicationFiled: June 3, 2011Publication date: April 18, 2013Applicant: KAO CORPORATIONInventors: Hiroyuki Yoshida, Shintaro Inoue, Shingo Sakai, Aya Nagaoka
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Patent number: 8420694Abstract: A compound represented by the formula (I?): or a salt thereof, has a superior androgen modulating action, wherein R1, R2, R4 to R8, R10 and R11 are defined in the claim.Type: GrantFiled: August 6, 2008Date of Patent: April 16, 2013Assignee: Takeda Pharmaceutical Company LimitedInventor: Atsushi Hasuoka
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Patent number: 8420644Abstract: The present invention relates to the use of at least one compound of formula (I) below: or at least one of the pharmaceutically acceptable salts thereof, for the preparation of a medicament intended for the prevention or for the treatment of cerebral edemas.Type: GrantFiled: June 5, 2006Date of Patent: April 16, 2013Assignee: BiocodexInventors: Marie-Emmanuelle Le Guern, Philippe Girard, Jean-Marie Gillardin, Laurence Berthon-Cedille, Bernard Hublot
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Patent number: 8410024Abstract: The present invention relates to the use of new and known maleimide salts for controlling phytopathogenic fungi, and also to methods for controlling phytopathogenic fungi in crop protection, in the household and hygiene sectors and in materials protection, and also to crop protection compositions comprising these maleimide salts.Type: GrantFiled: March 4, 2011Date of Patent: April 2, 2013Assignee: Bayer Cropscience AGInventors: Thomas Seitz, Thomas Himmler, Jürgen Benting, Ulrike Wachendorff-Neumann
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Publication number: 20130071495Abstract: The present invention relates to an inhibitor of glycogen synthase kinase 3 (GSK-3) for use in a method of treating or preventing emphysema, a method of activating an emphysema cell, an activated emphysema cell obtained by this method for use in a method of treating or preventing emphysema, and a method of screening for a substance for treating or preventing emphysema.Type: ApplicationFiled: March 16, 2011Publication date: March 21, 2013Applicant: Helmholtz Zentrum Muenchen Deutsches Forschungszentrum fuer Gesundheit und Umwelt (GmbHInventors: Melanie Koenigshoff, Oliver Eickelberg
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Publication number: 20130065909Abstract: The invention relates to Fatty Acid Fumarate Derivatives; compositions comprising an effective amount of a Fatty Acid Fumarate Derivative; and methods for treating or preventing cancer, a metabolic disorder or neurodegenerative disorder comprising the administration of an effective amount of a Fatty Acid Fumarate Derivative.Type: ApplicationFiled: November 9, 2012Publication date: March 14, 2013Applicant: CATABASIS PHARMACEUTICALS, INC.Inventors: Jill C. Milne, Michael R. Jirousek, Jean E. Bemis, Chi B. Vu
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Publication number: 20130065850Abstract: Alterations of certain metabolite concentrations and fluxes that occur in response to viral infection are described. Host cell enzymes in the involved metabolic pathways are selected as targets for intervention; i.e., to restore metabolic flux to disadvantage viral replication, or to further derange metabolic flux resulting in “suicide” of viral-infected cells (but not uninfected cells) in order to limit viral propagation. While any of the enzymes in the relevant metabolic pathway can be selected, pivotal enzymes at key control points in these metabolic pathways are preferred as candidate antiviral drug targets. Inhibitors of these enzymes are used to reverse, or redirect, the effects of the viral infection. Drug candidates are tested for antiviral activity using screening assays in vitro and host cells, as well as in animal models. Animal models are then used to test efficacy of candidate compounds in preventing and treating viral infections. The antiviral activity of enzyme inhibitors is demonstrated.Type: ApplicationFiled: April 3, 2012Publication date: March 14, 2013Applicant: THE TRUSTEES OF PRINCETON UNIVERSITYInventors: Josh MUNGER, Bryson BENNETT, Thomas SHENK, Joshua RABINOWITZ
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Publication number: 20130065834Abstract: Methods of modulating proteasome activity, increasing life span and neurogenesis are provided herein.Type: ApplicationFiled: July 25, 2012Publication date: March 14, 2013Applicant: SALK INSTITUTE FOR BIOLOGICAL STUDIESInventors: David Vilchez, Andrew Dillin
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Publication number: 20130059900Abstract: A crystal form I of (S)-4-hydroxy-2-oxo-1-pyrrolidine acetamide, or named (S)-oxiracetam, is provided, which is characterized by a powder x-ray diffraction pattern that exhibits data of d-values versus the relative intensities as: 7.075(M), 5.355(S), 5.092(S), 4.590(M), 4.325(M), 4.259(S), 4.041(VS), 3.808(M), 3.542(M), 3.445(M), 3.393(M), 2.972(M), 2.914(S). A method for preparing a crystal form I of (S)-oxiracetam is also provided, which includes preparing the crude product and crystallizing A use of the crystal form I of (S)-oxiracetam in the manufacture of a medicament for preventing and treating memory dysfunction is also provided. Accordingly, the crystal form I of (S)-oxiracetam prepared by the method has high purity of more than 99.3% based on the percentages of the mass, with better efficacy than (S)-oxiracetam for preventing or treating memory dysfunction.Type: ApplicationFiled: September 8, 2010Publication date: March 7, 2013Inventors: Chao You, Hua Feng, Qi Pang, Lei Ye, Yuying Chen, Zuyuan Rong, Lei Jin, Nan Xu, Fei Li, Bo Li
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Patent number: 8389565Abstract: Methods for synthesizing Salacinol, its stereoisomers, and analogues, homologues and other derivatives thereof potentially useful as glycosidase inhibitors. In some embodiments the compounds of the invention may have the general formula (I) or (II): The synthetic schemes may comprise reacting a cyclic sulfate with a 5-membered ring sugar containing a heteroatom (X). The heteroatom preferably comprises sulfur, selenium, or nitrogen. The cyclic sulfate and ring sugar reagents may be readily prepared from carbohydrate precursors, such as D-glucose, L-glucose, D-xylose and L-xylose. The target compounds are prepared by opening of the cyclic sulfates by nucleophilic attack of the heteroatoms on the 5-membered ring sugars. The resulting heterocyclic compounds have a stable, inner salt structure comprising a heteroatom cation and a sulfate anion. The synthetic schemes yield various stereoisomers of the target compounds.Type: GrantFiled: March 2, 2006Date of Patent: March 5, 2013Assignee: Simon Fraser UniversityInventors: Brian Mario Pinto, Blair D. Johnston, Ahmad Ghavami, Monica Gabriela Szczepina, Hui Liu, Kashinath Sadalapure, Henrik H. Jensen, Nag Sharwan Kumar, Ravindranath Nasi
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Publication number: 20130040935Abstract: The invention relates to 5?-biphenyl-substituted cyclic ketoenols for therapeutic purposes, to pharmaceutical compositions and to their use in therapy, in particular for the prophylaxis and therapy of tumour disorders.Type: ApplicationFiled: February 8, 2011Publication date: February 14, 2013Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Ningshu Liu, Kai Thede, Philip Lienau, Arne Scholz, Christoph-Stephan Hilger, Ulf Bömer, Maher Najjar, Knut Eis, Reiner Fischer, Wahed Ahmed Moradi
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Publication number: 20130035635Abstract: The present invention relates to a prodrug or a pharmaceutically acceptable salt thereof, comprising a drug linker conjugate D-L, wherein D being a biologically active moiety containing an aromatic hydroxyl group is conjugated to one or more polymeric carriers via secondary carbamate-containing linkers L. Such carrier-linked prodrugs achieve drug releases with therapeutically useful half-lives. The invention also relates to pharmaceutical compositions comprising said prodrugs and their use as medicaments.Type: ApplicationFiled: January 21, 2011Publication date: February 7, 2013Applicant: ASCENDIS PHARMA A/SInventors: Harald Rau, Torben Lessmann
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Patent number: 8367065Abstract: The present invention provides single chain antibody-directed polymeric prodrugs containing multifunctional linkers. Methods of making the polymeric delivery systems and methods of treating mammals using the same are also disclosed.Type: GrantFiled: March 12, 2009Date of Patent: February 5, 2013Assignee: Enzon Pharmaceuticals, Inc.Inventors: Hong Zhao, Prasanna Reddy, Maria Belen Rubio
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Publication number: 20120321727Abstract: Disclosed are edible formulations, for example, edible films and gummi confectioneries, that mask the taste of semen. The films and confectioneries include a composition that upon activation in the oral cavity provides a lasting taste masking effect that endures for up to 20 minutes. The composition includes a film former or gelling agent, an effective amount of a protein masker, and an effective amount of a bitter masker. The composition may also include a flavoring agent, sweetening agents, and sensates.Type: ApplicationFiled: April 25, 2012Publication date: December 20, 2012Applicant: ACME SPECIALTY PRODUCTS, LLCInventors: Robert J. Windschauer, Teresa T. Virgallito
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Publication number: 20120309811Abstract: The invention relates to a compound having structure (I), which acts as a non-competitive specific inhibitor of P-glycoprotein (P-gp for “Pleiotropic glycoprotein”) and which can be used as a drug, particularly for improving the effectiveness of chemotherapy treatments. The invention is therefore suitable for use in the medical field, particularly for the chemotherapeutic treatment of cancers or infections.Type: ApplicationFiled: October 5, 2010Publication date: December 6, 2012Applicants: UNIVERSITE CLAUDE BERNARD - LYON 1, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE - CNRS -Inventors: Ophelie Arnaud, Ali Koubeissi, Laurent Ettouati, Joelle Paris, Attilio Di Peetro, Pierre Falson
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Publication number: 20120289535Abstract: The present invention relates to conjugate comprising a carrier substituted with one or more occurrences of a moiety having the structure: wherein each occurrence of M is independently a modifier having a molecular weight ?10 kDa; denotes direct of indirect attachment of M to linker LM; and each occurrence of LM is independently an optionally substituted succinamide-containing linker, whereby the modifier M is directly or indirectly attached to the succinamide linker through an amide bond, and the carrier is linked directly or indirectly to each occurrence of the succinamide linker through an ester bond. In another aspect, the invention provides compositions comprising the conjugates, methods for their preparation, and methods of use thereof in the treatment of various disorder, including, but not limited to cancer.Type: ApplicationFiled: July 19, 2012Publication date: November 15, 2012Applicant: The General Hospital CorporationInventors: Mikhail I. Papisov, Alexander Yurkovetskiy
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Publication number: 20120277193Abstract: Combinations of compounds are provided that produce a synergistic effect when administered.Type: ApplicationFiled: September 20, 2010Publication date: November 1, 2012Applicant: PRESIDENT AND FELLOWS OF HARVARD COLLEGEInventors: Frederick P. Roth, Murat Cokol, Hon Nian Chua
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Publication number: 20120258997Abstract: The invention is related to the new application of selected derivatives of 2-pyrrolidone to inhibition of protein glycation and to prevention and treatment of diabetes complications, such as atherosclerosis, nephropathy, retinopathy, cataract or neuropathy.Type: ApplicationFiled: October 23, 2010Publication date: October 11, 2012Inventors: Rafal Olszanecki, Beata Bujak-Gizycka, Ryszard Korbut, Mariusz Gajda
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Patent number: 8283477Abstract: The present invention relates to a method of preparing N-substituted maleimide in high purity and high yield, wherein, unlike a conventional method of preparing N-substituted maleimide after preparing N-substituted maleamic acid, an organic solvent, an acid catalyst, a dehydration co-catalyst and a stabilizer are added into a reactor without separately preparing N-substituted maleamic acid, and then a primary amine is added into the reactor to form an amine salt, maleic anhydride is added into the reactor, and the resulting mixture is subjected to a dehydration-cyclization reaction, wherein water produced during the reaction is azeotropically distilled with the organic solvent so as to effectively suppress formation of a maleimide polymer.Type: GrantFiled: June 24, 2009Date of Patent: October 9, 2012Assignee: Korea Kumho Petrochemical Co., Ltd.Inventors: Jin-Eok Kim, Seung-il Kim, Han-Jin Kwag
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Patent number: 8278345Abstract: The present invention relates to compounds of formula (I), combinations and uses thereof for disease therapy, R1 represents heteroaryl, -carbocyclyl-heteroaryl, -alkenylheteroaryl or -alkylheteroaryl; R2 represents hydrogen; halogen; alkenyl; alkynyl; -alkenylaryl; -alkenylheteroaryl; alkyl, which may optionally be substituted by one or more groups selected from halogen, hydroxyl, alkoxy-, -thioalkyl, —C(O)OH and —C(O)O-alkyl; carbocyclyl, which may optionally be substituted by one or more groups selected from alkyl, halogen, hydroxyl, alkoxy-, -thioalkyl, —C(O)OH and —C(O)O-alkyl; -alkylcarbocyclyl; -alkylheterocyclyl; aryl; heteroaryl; heterocyclyl; -alkylaryl; -alkyl(aryl)2, -alkylheteroaryl; -aryl-heteroaryl; -heterocyclyl-aryl; -aryl-aryl; -heteroaryl-aryl; -heteroaryl-heteroaryl, and —C(O)R4; R3 represents halogen; alkyl optionally substituted by one or more groups selected from halogen, hydroxyl, alkoxy, thioalkyl, —C(O)OH and —C(O)O-alkyl; aryl; heteroaryl; —C(O)R5; R4 and R5 independently repreType: GrantFiled: November 8, 2007Date of Patent: October 2, 2012Assignee: Probiodrug AGInventors: Michael Thormann, Michael Altmstetter, Andreas Treml, Ulrich Heiser, Mirko Buchholz, Andre J. Niestroj
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Patent number: 8273787Abstract: Activated cytotoxic compounds are described for attachment to targeting molecules for the treatment of a mammalian disease condition which comprise, an activator, a spacer linker, a linker (e.g., self-immolative), and a cytotoxic drug selected from the group consisting of AMINO-SUBSTITUTED (E)-2,6-DIALKOXYSTYRYL 4-SUBSTITUTED BENZYLSULFONES, AMINO-AND-HYDROXY SUBSTITUTED STYRYLSULFONANILIDES, and SUBSTITUTED PHENOXY- AND PHENYLTHIO-STYRYLSULFONE DERIVATIVES. Activated cytotoxic compound attached to a targeting molecule are described wherein the targeting molecule is selected from the group consisting essentially of an antibody, a receptor, a ligand, a cytokine, a hormone, and a signal transduction molecule. The invention is further directed to a method of treatment of disease conditions.Type: GrantFiled: September 14, 2007Date of Patent: September 25, 2012Assignee: Onconova Therapeutics, IncInventors: Stanley C Bell, Glenn Fegley, Stephen Cosenza, Jodie Duke, Reddy E Premkumar, Reddy M. V. Ramana
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Publication number: 20120237615Abstract: The present invention provides O-nitro compounds, pharmaceutical compositions of O-nitro compounds and methods of using O-nitro compounds and/or pharmaceutical compositions thereof to treat or prevent diseases or disorders characterized by abnormal cell proliferation, such as cancer, inflammation, cardiovascular disease and autoimmune disease.Type: ApplicationFiled: May 30, 2012Publication date: September 20, 2012Applicants: RADIORX, INC., C/O INTERWEST VENTURE PARTNERS, ALLIANT TECHSYSTEMS INC.Inventors: Mark D. Bednarski, Lynn M. Oehler, Susan Knox, Louis Cannizzo, Kirstin Warner, Robert Wardle, Stephen Velarde, Shoucheng Ning
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Patent number: 8217182Abstract: A cyclic polycarboxylic acid anhydride, a polycarboxylic acid, or a mixture of them is allowed to react with hydroxylamine or a salt thereof in an organic solvent under dewatering conditions to yield a corresponding cyclic N-hydroxyimide compound. The cyclic polycarboxylic acid anhydride can be, for example, succinic anhydride or glutaric anhydride. The polycarboxylic acid can be, for example, succinic acid, glutaric acid, or adipic acid. In this process, the reaction is preferably carried out using an organic solvent capable of undergoing azeotropy with water as all or part of a reaction solvent while removing water from the reaction system by azeotropy with the organic solvent. This process produces a cyclic N-hydroxyimide compound in a good yield from any of a cyclic polycarboxylic acid anhydride and a polycarboxylic acid.Type: GrantFiled: July 28, 2009Date of Patent: July 10, 2012Assignee: Daicel Chemical Industries, LTD.Inventor: Yasuteru Kajikawa