Abstract: The present invention relates to novel lactose-derived compounds of general formula (I) and to their use as agents for stimulating the immune system of the skin and/or as immunoregulators, and for preparing a composition containing a cosmetically or pharmaceutically acceptable medium, intended in particular to prevent and/or limit the appearance of cutaneous immune imbalances, in particular related to environmental stresses.
Abstract: Solid forms of anhydrous (2S,3R,4R,5S,6R)-2-(4-chloro-3-(4-ethoxybenzyl)phenyl)-6-(methylthio)tetrahydro-2H-pyran-3,4,5-triol are disclosed, in addition to methods of their use in the treatment of various diseases and disorders.
Type:
Grant
Filed:
July 15, 2009
Date of Patent:
July 10, 2012
Assignee:
Lexicon Pharmaceuticals, Inc.
Inventors:
Susan Margaret De Paul, Anett Perlberg, Matthew Mangzhu Zhao
Abstract: A process of synthesizing a 5-azacytosine nucleoside, such as azacitidine and decitabine, comprises coupling a silylated 5-azacytosine with a protected D-ribofuranose of formula in the presence of a sulfonic acid catalyst.
Type:
Grant
Filed:
August 10, 2009
Date of Patent:
July 3, 2012
Assignee:
ScinoPharm Taiwan, Ltd.
Inventors:
Julian Paul Henschke, Xiaoheng Zhang, Lunghu Wang, Yung Fa Chen
Abstract: Methods for stabilizing ?-galactosidase, stabilizing ?-glucocerebrosidase, treating a glycolipid metabolic disorder caused by mutation of ?-galactosidase gene, treating a glycolipid metabolic disorder caused by mutation of ?-glucocerebrosidase gene, regenerating the activity of ?-galactosidase, regenerating the activity of ?-glucosidase, treating GM1 gangliosidosis, Morquio-B or Krabbe's disease, and treating Gaucher's disease, include administering a carba-sugar amine derivative represented by the following formula (1) or (2):
Abstract: This invention relates to the field of nucleic acid chemistry, more specifically to the field of compositions of matter that comprise triphosphates of modified 2?-deoxynucleosides and oligonucleotides that are formed when these are appended to the 3?-end of a primer, wherein said modifications comprise NH2 moiety attached to their 3?-hydroxyl group and a fluorescent species in a form of a tag affixed to the nucleobase via a linker that can be cleaved. Such compositions and their associated processes enable and improve the sequencing of oligonucleotides using a strategy of cyclic reversible termination, as outlined in U.S. Pat. No. 6,664,079. Most specifically, the invention concerns compositions of matter that are 5?-triphosphates of ribo- and 2?-deoxyribonucleosides carrying detectable tags and oligonucleotides that might be derived from them.
Type:
Grant
Filed:
March 23, 2009
Date of Patent:
July 3, 2012
Inventors:
Steven Albert Benner, Daniel Hutter, Nicole Aurora Leal, Fei Chen
Abstract: Aspects of the invention include 2? protected nucleoside monomers that are protected at the 2? site with thiocarbon protecting groups. Thiocarbon protecting groups of interest include thiocarbonate, thionocarbonate, dithiocarbonate groups, as well as thionocarbamate protecting groups. Aspects of the invention further include nucleic acids that include the protecting groups of the invention, as well as methods of synthesizing nucleic acids using the protecting groups of the invention.
Type:
Grant
Filed:
May 9, 2008
Date of Patent:
June 19, 2012
Assignee:
Agilent Technologies, Inc.
Inventors:
Douglas J. Dellinger, Agnieszka Sierzchala, John Turner, Joel Myerson, Zoltan Kupihar, Fernando Ferreira, Marvin H. Caruthers, Geraldine F. Dellinger
Abstract: Nucleotide monomers, polynucleotides, methods of making each, and methods of deprotecting each, are disclosed. An embodiment of the nucleotide monomer, among others, includes a nucleotide monomer having a heterobase protecting group selected from structures I through III as described herein. An embodiment of the polynucleotide, among others, includes a plurality of nucleotide moieties having a heterobase protecting group selected from one of structures I through III as described herein.
Type:
Grant
Filed:
March 23, 2006
Date of Patent:
June 19, 2012
Assignees:
Agilent Technologies, Inc., The Regents of the University of Colorado
Inventors:
Douglas J. Dellinger, Zoltan Timar, Agnieszka Sierzchala, Geraldino Dellinger, Marvin H. Caruthers
Abstract: The synthesis and biochemical utility of modified oligonucleotides containing diphosphodiester internucleotide linkages. The synthesis of these compounds was carried out using diphosphitylating reagents. Oligonucleotides containing diphosphate diester bridges wherein said oligonucleotides are synthesized via a solid-phase synthesis strategy to form modified oligonucleotides. Diphosphitylating, triphosphitylating, tetraphosphitylating, ?-triphosphitylating, bifunctional diphosphitylating, bifunctional triphosphitylating, and bifunctional tetraphosphitylating reagents wherein, the phosphorus atoms are linked together through oxygen, sulfur, amino, or methylene groups and/or are substituted with chlorine, diisopropylamine and cyanoethoxy groups.
Type:
Grant
Filed:
January 10, 2008
Date of Patent:
June 5, 2012
Assignee:
Board of Governors for Higher Education, State of Rhode Island and Providence Plantation
Abstract: The present invention relates a processing method for nano-miniaturizing chitosan of modifying property, which degrades the chitosan of high molecular weight down to the chitosan of middle and low molecular weight, then primarily nano-miniaturizes the interim chitosan by quaternary ammonium salt/synthesis, finally yield the nano-miniaturized chitosan of modified property by sol-gel method to have features in good biocompatibility and bioactivity to be served as additive material in products of cosmetics, medical treatment, hygiene, health care, biomedicine, agriculture, textile, food and so like so that not only the antiseptic, moisture-retentive and deodorizing capabilities can be promoted but also the processing cost can be reduced due to easiness of the mass production.
Abstract: Ionic liquids and cellulose ester compositions and processes for producing ionic liquids and cellulose esters. Cellulose esters can be produced by esterifying cellulose in a reaction medium comprising one or more ionic liquids. Cellulose esters prepared via the methods of the present invention can be contacted with at least one bleaching agent to produce bleached cellulose esters having a ?E value of less than 30.
Type:
Grant
Filed:
August 11, 2008
Date of Patent:
May 29, 2012
Assignee:
Eastman Chemical Company
Inventors:
Charles Michael Buchanan, Norma Lindsey Buchanan
Abstract: [Problems] A derivative of a nucleic acid antimetabolite is demanded which can show a higher therapeutic effect at a lower dose. [Means for Solving Problems] Disclosed is a high molecular weight derivative a nucleic acid antimetabolite, which is characterized by comprising a high molecular weight compound comprising a polyethylene glycol moiety and a polymer moiety having a carboxyl group in a side chain and a nucleoside derivative which can act as a nucleic acid antimetabolite, wherein the nucleoside derivative is bound to the carboxyl group in the side chain of the high molecular weight compound via a highly hydrophobic linker.
Abstract: Novel avermectin derivatives of the formula (I) in which —C22R1-A-C23R2, R3, R4 and R5 have the meanings given in the description, processes for preparing these compounds and their use for controlling animal pests, and also novel intermediates and their preparation.
Type:
Grant
Filed:
August 8, 2007
Date of Patent:
May 22, 2012
Assignee:
Bayer Cropscience AG
Inventors:
Peter Jeschke, Gunter Karig, Robert Velten, Reiner Fischer, Olga Malsam, Ulrich Görgens, Christian Arnold, Erich Sanwald, Achim Harder, Andreas Turberg
Abstract: The invention relates to Purine Derivatives; compositions comprising an effective amount of a Purine Derivative; and methods for reducing an animal's rate of metabolism, protecting an animal's heart against myocardial damage during cardioplegia; or for treating or preventing a cardiovascular disease, a neurological disorder, an ischemic condition, a reperfusion injury, obesity, a wasting disease, or diabetes, comprising administering an effective amount of a Purine Derivative to an animal in need thereof.
Type:
Grant
Filed:
August 4, 2008
Date of Patent:
May 22, 2012
Assignee:
Inotek Pharmaceuticals Corporation
Inventors:
Prakash Jagtap, Csaba Szabo, Andrew L. Salzman
Abstract: This invention defines novel compositions that can be used for clinical treatment of a class of chronic inflammatory diseases. Increased generation of carbonyl substances, namely aldehydes and ketones, occurs at sites of chronic inflammation and is common to the etiologies of all of the clinical disorders addressed herein. Such carbonyl substances are cytotoxic and additionally serve to perpetuate and disseminate the inflammatory process. This invention defines use of compositions, the orally administered required primary agents of which are primary amine derivatives of benzoic acid capable of covalently reacting with the carbonyl substances. p-Aminobenzoic acid (or PABA) is an example of the required primary agent of the present invention. PABA has a small molecular weight, is water-soluble, has a primary amine group which reacts with carbonyl-containing substances and is tolerated by the body in relatively high dosages for extended periods.
Abstract: The present invention provides a therapeutic method for treating an inflammatory response caused by a sickle cell crisis, comprising administration of an effective amount of an A2A adenosine receptor agonist. Optionally, the method includes administration of a type IV PDE inhibitor (e.g., rolipram).
Type:
Grant
Filed:
February 9, 2007
Date of Patent:
May 15, 2012
Assignee:
University of Virginia Patent Foundation
Inventors:
Joel M. Linden, Kori Wallace, Robert Alan Figler, Jayson M. Rieger
Abstract: The invention disclosed in this document is related to the field of pesticides and their use in controlling pests. A compound having the following structure is disclosed.
Type:
Grant
Filed:
February 11, 2009
Date of Patent:
May 15, 2012
Assignee:
Dow AgroSciences, LLC
Inventors:
Gary D. Crouse, Thomas C. Sparks, CaSandra L. McLeod, David A. Demeter, Kristy Bryan, Annette V. Brown, William H. Dent, III, Denise P. Cudworth, Jaime S. Nugent, Ricky Hunter, Jack G. Samaritoni
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.
Abstract: The present disclosure provides compositions and methods for treating, ameliorating, or relieving at least one symptom associated with loss of blood flow to the brain including, without limitation, ischemic stroke. Compositions of the disclosure may comprise a bile acid compound and a carbohydrate, wherein both materials remain in solution for all pH values of the solution within a selected range of pH values. Symptoms may include infarct volume, functional recovery, apoptosis, and/or eNOS expression.
Abstract: Disclosed are methods of treating cancer, inflammatory conditions, and/or infectious disease in an animal comprising: administering to the animal, a therapeutically effective amount of a heterocyclic compound. The animal is a mammal, preferably a human or a rodent.
Type:
Grant
Filed:
June 10, 2008
Date of Patent:
May 1, 2012
Assignee:
Nereus Pharmaceuticals, Inc.
Inventors:
Michael Palladino, Saskia Theodora Cornelia Neuteboom
Abstract: A compound of formula (A) or salt thereof: wherein each of R1, R2, and R3 independently represents hydrogen, alkyl, aryl, acyl, sulfonyl, or silyl; P represents hydrogen or a hydroxy protective group. This compound may be used an intermediate for making a 2-deoxy-2,2-difluoro-D-ribofuranosyl nucleosides, such as gemcitabine.
Type:
Grant
Filed:
August 31, 2009
Date of Patent:
May 1, 2012
Assignee:
ScnioPharm Taiwan Ltd.
Inventors:
Julian Paul Henschke, Yung Fa Chen, George Charles Schloemer