The Spiro Includes The Lactone Ring Patents (Class 549/265)
  • Patent number: 10920265
    Abstract: Provided is a compound that comprises the structure: where SIG is a signaling molecule and R3 is a formyl, a succinyl, a methyl succinyl, or a myristoyl. Also provided is a kit is provided that comprises the above compound, with instructions for determining the presence of the enzyme. Additionally, a method is provided for determining whether a sample has an enzyme that removes a succinyl, a methyl succinyl, a formyl, or a myristoyl moiety from an ?-amino of a lysine. Also provided is a method of determining whether a molecule inhibits an enzyme that removes a succinyl, a methyl succinyl, a formyl, or a myristoyl moiety from an ?-amino of a lysine.
    Type: Grant
    Filed: March 30, 2020
    Date of Patent: February 16, 2021
    Assignee: Enzo Life Sciences, Inc.
    Inventors: Konrad T. Howitz, Zhongda Zhang, Anne Kisielewski, Elizabeth Dale, Wayne Forrest Patton
  • Patent number: 10648013
    Abstract: Provided is a compound that comprises the structure: where SIG is a signaling molecule and R3 is a formyl, a succinyl, a methyl succinyl, or a myristoyl. Also provided is a kit is provided that comprises the above compound, with instructions for determining the presence of the enzyme. Additionally, a method is provided for determining whether a sample has an enzyme that removes a succinyl, a methyl succinyl, a formyl, or a myristoyl moiety from an ?-amino of a lysine. Also provided is a method of determining whether a molecule inhibits an enzyme that removes a succinyl, a methyl succinyl, a formyl, or a myristoyl moiety from an ?-amino of a lysine.
    Type: Grant
    Filed: April 18, 2019
    Date of Patent: May 12, 2020
    Assignee: Enzo Life Sciences, Inc.
    Inventors: Konrad T. Howitz, Zhongda Zhang, Anne Kisielewski, Elizabeth Dale, Wayne Forrest Patton
  • Patent number: 10308974
    Abstract: Provided is a compound that comprises the structure: where SIG is a signaling molecule and R3 is a formyl, a succinyl, a methyl succinyl, or a myristoyl. Also provided is a kit is provided that comprises the above compound, with instructions for determining the presence of the enzyme. Additionally, a method is provided for determining whether a sample has an enzyme that removes a succinyl, a methyl succinyl, a formyl, or a myristoyl moiety from an ?-amino of a lysine. Also provided is a method of determining whether a molecule inhibits an enzyme that removes a succinyl, a methyl succinyl, a formyl, or a myristoyl moiety from an ?-amino of a lysine.
    Type: Grant
    Filed: April 3, 2018
    Date of Patent: June 4, 2019
    Assignee: Enzo Life Sciences, Inc.
    Inventors: Konrad T. Howitz, Zhongda Zhang, Anne Kisielewski, Elizabeth Dale, Wayne Forrest Patton
  • Patent number: 9963734
    Abstract: Provided is a compound that comprises the structure: where SIG is a signaling molecule and R3 is a formyl, a succinyl, a methyl succinyl, or a myristoyl. Also provided is a kit is provided that comprises the above compound, with instructions for determining the presence of the enzyme. Additionally, a method is provided for determining whether a sample has an enzyme that removes a succinyl, a methyl succinyl, a formyl, or a myristoyl moiety from an ?-amino of a lysine. Also provided is a method of determining whether a molecule inhibits an enzyme that removes a succinyl, a methyl succinyl, a formyl, or a myristoyl moiety from an ?-amino of a lysine.
    Type: Grant
    Filed: March 21, 2017
    Date of Patent: May 8, 2018
    Assignee: Enzo Life Sciences, Inc.
    Inventors: Konrad T. Howitz, Zhongda Zhang, Anne Kisielewski, Elizabeth Dale, Wayne Forrest Patton
  • Patent number: 9879203
    Abstract: The present invention concerns a process for the preparation of an oxidized terpenes fraction which proved to be particularly useful in the preparation of sandalwood oil building blocks.
    Type: Grant
    Filed: November 16, 2015
    Date of Patent: January 30, 2018
    Assignee: Firmenich SA
    Inventors: Oliver Knopff, Fabien Fonteny
  • Publication number: 20150141603
    Abstract: The invention provides novel organometallic complexes useful as olefin metathesis catalysts. The complexes have an N-heterocyclic carbene ligand and a chelating carbene ligand associated with a Group 8 transition metal center. The molecular structure of the complexes can be altered so as to provide a substantial latency period. The complexes are particularly useful in catalyzing ring closing metathesis of acyclic olefins and ring opening metathesis polymerization of cyclic olefins.
    Type: Application
    Filed: September 26, 2014
    Publication date: May 21, 2015
    Inventors: Thay UNG, Yann SCHRODI, Mark S. TRIMMER, Andrew HEJL, Daniel SANDERS, Robert H. GRUBBS
  • Patent number: 9018394
    Abstract: The invention is a method for efficiently producing an aromatic compound by an intramolecular cyclization reaction, the aromatic compound having a ring structure that includes a nitrogen atom or oxygen atom. An aromatic compound composed of tert-butyl-2-(3-oxo-3-phenylpropyl)phenyl carbamate or another aniline derivative or the like, or an aromatic compound composed of 3-(1-hydroxynaphthalene-2-yl)propionic acid or another naphthol derivative or the like is made to react in a system to which an oxidizing agent and a quaternary ammonium salt represented by general formula (1) are fed. In the formula, X is an iodine atom; and R1, R2, R3 and R4 are each independently a C1-30 hydrocarbon group in which some hydrogen atoms are optionally substituted with halogen atoms, or R1 and R2 may be combine to form a divalent organic group bonded to a nitrogen atom, and R3 and R4 may combine to form a divalent organic group bonded to a nitrogen atom.
    Type: Grant
    Filed: February 2, 2012
    Date of Patent: April 28, 2015
    Assignee: National University Corporation Nagoya University
    Inventors: Kazuaki Ishihara, Uyanik Muhammet
  • Patent number: 9000216
    Abstract: An optically active spirolactone compound is highly enantioselectively produced by using an iodoarene derivative which can be synthesized easily and which is not racemized easily. A hypervalent iodine compound precursor (iodoarene derivative) which was able to be designed flexibly was synthesized from 2,6-dihydroxyiodoarene by using 1,2-aminoalcohol as a chiral source in short steps, a hypervalent iodine compound was prepared in a reaction system (in situ) by using a catalyst quantity of the resulting precursor in the presence of a stoichiometric quantity of m-CPBA, and a spirolactonization reaction of 3-(1-hydroxy-2-naphthyl)propionic acid was induced. As a result, a corresponding spirolactone compound was obtained at a high enantiomeric excess.
    Type: Grant
    Filed: March 6, 2012
    Date of Patent: April 7, 2015
    Assignee: National University Corporation Nagoya University
    Inventors: Kazuaki Ishihara, Muhammet Uyanik, Takeshi Yasui
  • Publication number: 20150064620
    Abstract: A photoacid generator compound has formula (1) wherein n is zero or 1; and R1-R6 are each independently hydrogen, halogen, or unsubstituted or substituted C1-20 linear or branched alkyl, C1-20 cycloalkyl, C6-20 aryl, C3-20 heteroaryl, or an acid-generating group having the structure *?L-Z?M+] wherein L is an unsubstituted or substituted C1-50 divalent group; Z? is a monovalent anionic group; and M+ is an iodonium or sulfonium cation. Geminal R groups can combine to form a ring with the carbon to which they are attached, as long as no more than two such rings are formed. At least one of R1-R6 includes the acid-generating group or two germinal R groups combine to form the acid-generating group. Also described are a photoresist composition incorporating the photoacid generator compound, a coated substrate including a layer of the photoresist composition, and a method of forming an electronic device using a layer of the photoresist composition.
    Type: Application
    Filed: August 28, 2013
    Publication date: March 5, 2015
    Applicant: ROHM AND HAAS ELECTRONIC MATERIALS LLC
    Inventors: Irvinder Kaur, Emad Aqad, Cong Liu, Cheng Bai Xu
  • Publication number: 20150057238
    Abstract: Certain compounds, or pharmaceutically acceptable salts or prodrugs thereof, are provided herein. Also provided are pharmaceutical compositions comprising at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of KMO activity are described, which comprise administering to such patients an amount of at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include neurodegenerative disorders such as Huntington's disease.
    Type: Application
    Filed: March 13, 2013
    Publication date: February 26, 2015
    Inventors: Leticia M. Toledo-Sherman, Celia Dominguez, Michael Prime, William Leonard Mitchell, Peter Johnson, Naomi Went
  • Patent number: 8946124
    Abstract: The invention relates to novel compounds of the formula (I) in which W, X, Y, Z, A, B, D and G have the meanings given above, to a plurality of processes and intermediates for their preparation, and to their use as pesticides and/or herbicides and/or fungicides. The invention also relates to selective herbicidal compositions comprising, firstly, the halogen-substituted spirocyclic ketoenols and, secondly, a crop plant compatibility-improving compound. The present invention furthermore relates to the boosting of the action of crop protection compositions comprising, in particular, halogen-substituted spirocyclic ketoenols, through the addition of ammonium salts or phosphonium salts and optionally penetrants, to the corresponding compositions, to processes for producing them and to their application in crop protection as pesticides and/or fungicides and/or for preventing unwanted plant growth. The invention also relates to substituted 3-(biphenyl-3-yl)-8,8-difluoro-4-hydroxy-1-azaspiro[4.
    Type: Grant
    Filed: February 14, 2012
    Date of Patent: February 3, 2015
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Thomas Bretschneider, Reiner Fischer, Stefan Lehr, Elmar Gatzweiler, Ulrich Görgens, Isolde Häuser-Hahn, Ines Heinemann, Arnd Voerste
  • Patent number: 8940859
    Abstract: 1,3-Dipole-functional compounds (e.g., azide functional compounds) can be reacted with certain alkynes in a cyclization reaction to form heterocyclic compounds. Useful alkynes (e.g., strained, cyclic alkynes) and methods of making such alkynes are also disclosed. The reaction of 1,3-dipole-functional compounds with alkynes can be used for a wide variety of applications including the immobilization of biomolecules on a substrate.
    Type: Grant
    Filed: March 13, 2012
    Date of Patent: January 27, 2015
    Assignee: University of Georgia Research Foundation, Inc.
    Inventors: Geert-Jan Boons, Jun Guo, Xinghai Ning, Margaretha Wolfert
  • Publication number: 20140378344
    Abstract: Fluorescent dyes useful for preparing fluorescent metal ion indicators, the fluorescent indicators themselves, and the use of the fluorescent indicators for the detection, discrimination and quantification of metal cations are provided.
    Type: Application
    Filed: August 4, 2014
    Publication date: December 25, 2014
    Inventors: Zhenjun Diwu, Haitao Guo, Ruogu Peng, Qin Zhao, Jixiang Liu, Jinfang Liao
  • Publication number: 20140308696
    Abstract: Reaction-based fluorscent probes are provided which detect, for example, biologically important sulfane sulfur species (persulfide, polysulfide, and elemental sulfur) in, for example, complex and living systems. The probes are high in selectivity and sensitivity to sulfane sulfurs. Moreover, probes are suitable for bioimaging sulfane sulfurs in living cells.
    Type: Application
    Filed: April 11, 2014
    Publication date: October 16, 2014
    Applicant: Washington State University
    Inventors: Ming Xian, Wei Chen
  • Patent number: 8828678
    Abstract: A compound comprising the structure: (SIG)-(SI-MOD)m. is provided in which SIG is a signaling molecule, SI is a self-immolative structure bound to SIG such that SIG has a reduced signal relative to the signal of SIG without SI, MOD is a moiety bound to SI that is subject to modification by an activator, and m is an integer from 1 to about 10. When MOD is modified by an activator, SI is destabilized and self-cleaved from SIG such that SIG generates an increased signal. Also provided are methods of determining whether a sample comprises an activator such as a nitroreductase, and methods of determining whether a mammalian cell is hypoxic using a compound of the formula (SIG)-(SI-MOD)m.
    Type: Grant
    Filed: November 16, 2010
    Date of Patent: September 9, 2014
    Assignee: Enzo Life Sciences, Inc.
    Inventors: Maciej Szczepanik, Irina V. Lebedeva, Yuejun Xiang, Praveen Pande, Wayne Forrest Patton
  • Patent number: 8822528
    Abstract: This invention relates to novel polyether ionophores, formulations comprising same, and to methods of making and using these compounds and formulations for the treatment and/or prevention of parasitic infection in animals and humans. These compounds exhibit improved safety profiles and/or efficacies as compared to parent compounds.
    Type: Grant
    Filed: November 16, 2011
    Date of Patent: September 2, 2014
    Assignees: Merial Limited, Universite Claude Bernard Lyon 1, Centre National de la Recherche Scientifique (CNRS)
    Inventors: Jean Delaveau, Emile Vialle, Marc Lemaire, Stephane Pellet-Rostaing, Bruno Andrioletti
  • Publication number: 20140212328
    Abstract: Embodiments herein generally relate to the use, devices, and compounds for generating singlet oxygen. In some embodiments, the singlet oxygen can be used for fluid purification and/or sterilization.
    Type: Application
    Filed: July 24, 2012
    Publication date: July 31, 2014
    Applicant: EMPIRE TECHNOLOGY DEVELOPMENT LLC
    Inventors: William Brenden Carlson, Gregory David Phelan
  • Patent number: 8786181
    Abstract: The present invention relates to a blend comprising; a) at least one polymer or copolymer or a mixture of a plurality of polymers and/or copolymers which contain a main chain and a side chain, where at least one side chain contains a structural unit of the following formula (I), the symbols and indices used here are as defined below; b) at least one host molecule which has electron- or hole-transporting functionality, and c) at least one emitter molecule.
    Type: Grant
    Filed: October 14, 2011
    Date of Patent: July 22, 2014
    Assignees: Merck Patent GmbH, Fraunhofer-Gesellschaft Forschung E.V.
    Inventors: Thomas Eberle, Rémi Manouk Anémian, Manuel Thesen, Hartmut Krueger, Armin Wedel, Beatrice Salert, Stefanie Kreissl
  • Publication number: 20140163094
    Abstract: The present invention relates to specific beta-lactone compounds and compositions thereof for the treatment of infections, such as, e.g., infections with bacteria or infections with protozoa, in particular infections with Gram-positive and/or Gram-negative bacteria and of infectious diseases caused by or related to Gram-positive and/or Gram-negative bacteria, and to the modulation of virulence of Gram-positive and/or Gram-negative bacteria or of protozoa by specific beta-lactone compounds. The invention further relates to the use of the compounds or compositions for preventing or eliminating biofilms.
    Type: Application
    Filed: September 16, 2013
    Publication date: June 12, 2014
    Inventors: Stephan A. Sieber, Thomas Bottcher
  • Patent number: 8722574
    Abstract: There are described thermal imaging members and thermal imaging methods utilizing unsymmetrical rhodamine compounds. The rhodamine color-forming compounds exhibit a first color when in a crystalline form and a second color, different from the first color, when in an amorphous form.
    Type: Grant
    Filed: April 27, 2012
    Date of Patent: May 13, 2014
    Assignee: Zink Imaging, Inc.
    Inventors: Michael P Filosa, Stephen J. Telfer, John L Marshall, Richard M Allen, John M Hardin
  • Publication number: 20140039202
    Abstract: Disclosed is a method for separating and purifying Ginkgolide C from root bark of ginkgo.
    Type: Application
    Filed: February 24, 2012
    Publication date: February 6, 2014
    Inventors: Jun He, Jichuan Kang, Jianian Yang, Yixin Qian
  • Publication number: 20130338371
    Abstract: The invention is a method for efficiently producing an aromatic compound by an intramolecular cyclization reaction, the aromatic compound having a ring structure that includes a nitrogen atom or oxygen atom. An aromatic compound composed of tert-butyl-2-(3-oxo-3-phenylpropyl)phenyl carbamate or another aniline derivative or the like, or an aromatic compound composed of 3-(1-hydroxynaphthalene-2-yl)propionic acid or another naphthol derivative or the like is made to react in a system to which an oxidizing agent and a quaternary ammonium salt represented by general formula (1) are fed. In the formula, X is an iodine atom; and R1, R2, R3 and R4 are each independently a C1-30 hydrocarbon group in which some hydrogen atoms are optionally substituted with halogen atoms, or R1 and R2 may be combine to form a divalent organic group bonded to a nitrogen atom, and R3 and R4 may combine to form a divalent organic group bonded to a nitrogen atom.
    Type: Application
    Filed: February 2, 2012
    Publication date: December 19, 2013
    Applicant: National University Corporation Nagoya University
    Inventors: Kazuaki Ishihara, Uyanik Muhammet
  • Publication number: 20130338364
    Abstract: An optically active spirolactone compound is highly enantioselectively produced by using an iodoarene derivative which can be synthesized easily and which is not racemized easily. A hypervalent iodine compound precursor (iodoarene derivative) which was able to be designed flexibly was synthesized from 2,6-dihydroxyiodoarene by using 1,2-aminoalcohol as a chiral source in short steps, a hypervalent iodine compound was prepared in a reaction system (in situ) by using a catalyst quantity of the resulting precursor in the presence of a stoichiometric quantity of m-CPBA, and a spirolactonization reaction of 3-(1-hydroxy-2-naphthyl)propionic acid was induced. As a result, a corresponding spirolactone compound was obtained at a high enantiomeric excess.
    Type: Application
    Filed: March 6, 2012
    Publication date: December 19, 2013
    Applicant: NATIONAL UNIVERSITY CORPORATION NAGOYA UNIVERSITY
    Inventors: Kazuaki Ishihara, Muhammet Uyanik, Takeshi Yasui
  • Publication number: 20130324580
    Abstract: The present invention is in the field of pharmaceuticals and chemical industries. In particular, the present invention relates to new anticancer agents based on miliusane compounds. The present invention also includes its preparation and application method for treating cancer.
    Type: Application
    Filed: March 15, 2013
    Publication date: December 5, 2013
    Applicant: HONG KONG BAPTIST UNIVERSITY
    Inventor: Hongjie ZHANG
  • Publication number: 20130245269
    Abstract: The present invention describes tripodal catechol derivatives with an adamantyl basic framework for the functionalisation of surfaces, methods for their production and use. The remaining fourth bridgehead position is easily suitable to be further functionalised via so-called click reactions, by way of example with biomolecules, dyes, radiomarkers, polyethylene glycol or active agents.
    Type: Application
    Filed: September 7, 2011
    Publication date: September 19, 2013
    Applicant: JUSTUS-LIEBIG-UNIVERSITA GIESSEN
    Inventors: Wolfgang Maison, Faiza Khalil, Elisa Franzmann
  • Publication number: 20130231385
    Abstract: The present invention includes bis- and tris-benzamide compounds that block AR signaling and have anticancer activity. Uses for these compounds, and pharmaceutical compositions containing the same, also are provided.
    Type: Application
    Filed: May 27, 2011
    Publication date: September 5, 2013
    Applicant: The Board of Regents of the University of Texas Systems
    Inventors: Jung-Mo Ahn, Ganesh Raj
  • Publication number: 20130216951
    Abstract: A radiation-sensitive resin composition includes a polymer, an acid generating agent, and an organic solvent. The polymer includes a first structural unit derived from a compound represented by a formula (1), and a second structural unit derived from a compound represented by a formula (2). R1 represents an organic group having a valency of (a+2) that represents a ring structure having 3 to 8 carbon atoms together with the carbon atom constituting a lactone ring. R2 represents a fluorine atom, a hydroxyl group, an organic group having 1 to 20 carbon atoms or the like.
    Type: Application
    Filed: March 29, 2013
    Publication date: August 22, 2013
    Applicant: JSR CORPORATION
    Inventor: JSR Corporation
  • Publication number: 20130196362
    Abstract: Provided herein are improved fluorogenic compounds and probes that can be used as reagents for measuring, detecting and/or screening peroxynitrite. The fluorogenic compounds of the invention can produce fluorescence colors, such as green, yellow, red, or far-red. Also provided herein are fluorogenic compounds for selectively staining peroxynitrite in the mitochondria of living cells. Provided also herein are methods that can be used to measure, directly or indirectly, the presence and/or amount of peroxynitrite in chemical samples and biological samples such as cells and tissues in living organisms. Also provided are high-throughput screening methods for detecting or screening peroxynitrite or compounds that can increase or decrease the level of peroxynitrite in chemical and biological samples.
    Type: Application
    Filed: January 30, 2013
    Publication date: August 1, 2013
    Applicant: THE UNIVERSITY OF HONG KONG
    Inventor: THE UNIVERSITY OF HONG KONG
  • Publication number: 20130130289
    Abstract: The present invention provides compounds and methods for assaying redox state of metabolically active cells and methods for assaying enzyme activity and/or metabolite level by coupling to redox defining co-factor NAD(P)/NAD(P)H measurement.
    Type: Application
    Filed: August 31, 2012
    Publication date: May 23, 2013
    Applicant: PROMEGA CORPORATION
    Inventors: Helene A. BENINK, James J. CALI, Sarah DUELLMAN, Dieter KLAUBERT, Donna LEIPPE, Martha O'BRIEN, John SHULTZ, Jolanta VIDUGIRIENE, Wenhui ZHOU, Mary SOBOL
  • Patent number: 8426127
    Abstract: It is an object of the present invention to provide an on-off type fluorescent compound used in gene analyses, which is highly stable and highly sensitive, and which enables amplification of a trace amount of gene signal and observation thereof. The present invention provides a compound represented by the following formula (1) or (2): wherein R1 represents an alkyl group containing 1 to 6 carbon atoms, an amino group, an amide group optionally having a protecting group or a substituent, a halogen atom, or a hydrogen atom; R2 independently represents an alkyl group containing 1 to 6 carbon atoms, a halogen atom, or a hydrogen atom; R3 represents an alkyl group containing 1 to 6 carbon atoms, an aryl group, or a hydrogen atom; R4 represents a group containing an oxygen atom, or a hydrogen atom, wherein R3 may bind to R4 to form a ring.
    Type: Grant
    Filed: December 19, 2007
    Date of Patent: April 23, 2013
    Assignee: Riken
    Inventors: Hiroshi Abe, Yoshihiro Ito, Jin Wang, Kazuhiro Furukawa
  • Publication number: 20130040935
    Abstract: 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: Application
    Filed: February 8, 2011
    Publication date: February 14, 2013
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Ningshu Liu, Kai Thede, Philip Lienau, Arne Scholz, Christoph-Stephan Hilger, Ulf Bömer, Maher Najjar, Knut Eis, Reiner Fischer, Wahed Ahmed Moradi
  • Patent number: 8362170
    Abstract: Provided is a polymerizable compound represented by the following general formula (ca-1) or (cb-1): wherein the variables in the formulae are defined in the specification.
    Type: Grant
    Filed: June 18, 2012
    Date of Patent: January 29, 2013
    Assignee: FUJIFILM Corporation
    Inventors: Shuji Hirano, Kaoru Iwato, Hiroshi Saegusa, Yusuke Iizuka
  • Publication number: 20120322974
    Abstract: 1,3-Dipole-functional compounds (e.g., azide functional compounds) can be reacted with certain alkynes in a cyclization reaction to form heterocyclic compounds. Useful alkynes (e.g., strained, cyclic alkynes) and methods of making such alkynes are also disclosed. The reaction of 1,3-dipole-functional compounds with alkynes can be used for a wide variety of applications including the immobilization of biomolecules on a substrate.
    Type: Application
    Filed: March 13, 2012
    Publication date: December 20, 2012
    Applicant: University of Georgia Research Foundation, Inc.
    Inventors: GEERT-JAN BOONS, Jun Guo, Xinghai Ning, Margaretha Wolfert
  • Publication number: 20120308481
    Abstract: Radio-opaque biodegradable compositions are formed by modifying terminal groups of synthetic and natural biodegradable polymers such as polylactones with iodinated moieties. The biodegradable property of the compositions renders them suitable for use in medical field such as drug delivery, imaging. Compounds disclosed in this invention exist as neat liquid. Certain compositions disclosed in this invention form hydrophobic iodine rich domains when dissolved in water, such domains provide better contrasting properties as well as ability to dissolve hydrophobic bioactive drugs. Certain iodinated moieties disclosed in the invention are capable of cross linking natural proteins in situ in presence of suitable catalysts and co-catalysts.
    Type: Application
    Filed: August 16, 2012
    Publication date: December 6, 2012
    Applicant: PATHAK HOLDINGS LLC
    Inventors: Chandrashekhar P. Pathak, Sanjay M. Thigle
  • Publication number: 20120301401
    Abstract: This invention relates to A crown ether of formula (I) wherein m is 4, 5, 6, 7, or 8 and i is, independently for each occurrence, 1 or 2; each occurrence of R1 and R2 is independently selected from hydrogen; linear or branched and substituted or unsubstituted C1 to C10 alkyl, alkenyl and alkinyl; and substituted or unsubstituted aryl with up to 10 ring atoms; or R1 and R2 together form an oxo group; at least one occurrence in the crown ether of R1, R2 and the carbon to which R1 and R2 are attached, said carbon being bound directly to an ether oxygen of formula (I), form together a group of formula (II) wherein L is a linker which is absent or selected from a covalent bond and (CR5R6)n, each occurrence of R5 and R6 being independently selected from hydrogen; linear or branched and substituted or unsubstituted C1 to C10 alkyl, alkenyl and alkinyl; and substituted or unsubstituted aryl with up to 10 ring atoms, n being 1, 2 or 3; X and Y, independently from each other, are selected from O and S; Z, indep
    Type: Application
    Filed: November 25, 2010
    Publication date: November 29, 2012
    Applicant: ARISGEN SA
    Inventors: Paolo Botti, Sylvie Tchertchian, Doriane Theurillat
  • Publication number: 20120301880
    Abstract: Alkyl amine dyes, oligonucleotide probes prepared from the alkyl amine dyes, phosphoramidites and solid supports prepared from the alkyl amine dyes, and methods of labeling biological agents using the alkyl amine dyes.
    Type: Application
    Filed: May 29, 2012
    Publication date: November 29, 2012
    Applicant: BLOOD CELL STORAGE, INC.
    Inventors: Michael W. Reed, Robert O. Dempcy
  • Publication number: 20120270836
    Abstract: The present invention relates to compositions and methods for the treatment of Alzheimer's disease and related disorders. More specifically, the present invention relates to novel combinatorial therapies of Alzheimer's disease and related disorders. In particular, the invention concerns compounds which, alone or in combination(s), can effectively modulate synapse function and/or angiogenesis and/or cell stress response. The invention also relates to methods of producing a drug or a drug combination for treating Alzheimer's disease and to methods of treating Alzheimer's disease or a related disorder.
    Type: Application
    Filed: May 2, 2012
    Publication date: October 25, 2012
    Applicant: PHARNEXT
    Inventors: Daniel Cohen, Ilya Chumakov, Serguei Nabirochkin
  • Patent number: 8252877
    Abstract: Provided is a polymerizable compound represented by the following general formula (ca-1) or (cb-1): wherein the variables in the formulae are defined in the specification.
    Type: Grant
    Filed: December 11, 2009
    Date of Patent: August 28, 2012
    Assignee: FUJIFILM Corporation
    Inventors: Shuji Hirano, Kaoru Iwato, Hiroshi Saegusa, Yusuke Iizuka
  • Patent number: 8247579
    Abstract: The present invention relates to novel spirocyclic tetronic acid derivatives of the formula (I) in which R1, R2 and R3 have the meanings given in the description, to a plurality of processes for their preparation and to their use as pesticides.
    Type: Grant
    Filed: January 9, 2008
    Date of Patent: August 21, 2012
    Assignee: Bayer Cropscience AG
    Inventors: Reiner Fischer, Thomas Bretschneider, Hubertus Schulte, Gerhard Krautstrunk, Christian Arnold, Erich Sanwald
  • Publication number: 20120183948
    Abstract: Provided is a compound that comprises the structure: where SIG is a signaling molecule and R3 is a formyl, a succinyl, a methyl succinyl, or a myristoyl. Also provided is a kit is provided that comprises the above compound, with instructions for determining the presence of the enzyme. Additionally, a method is provided for determining whether a sample has an enzyme that removes a succinyl, a methyl succinyl, a formyl, or a myristoyl moiety from an ?-amino of a lysine. Also provided is a method of determining whether a molecule inhibits an enzyme that removes a succinyl, a methyl succinyl, a formyl, or a myristoyl moiety from an ?-amino of a lysine.
    Type: Application
    Filed: January 13, 2011
    Publication date: July 19, 2012
    Applicant: ENZO LIFE SCIENCES, INC. C/O ENZO BIOCHEM, INC.
    Inventors: Konrad T. Howitz, Zhongda Zhang, Anne Kisielewski, Elizabeth Dale, Wayne Forrest Patton
  • Patent number: 8222288
    Abstract: The invention relates to small molecules which function as inhibitors of the interaction between p53 and MDM2. The invention also relates to the use of these compounds for inhibiting cell growth, inducing cell death, inducing cell cycle arrest and/or sensitizing cells to additional agent(s).
    Type: Grant
    Filed: June 14, 2010
    Date of Patent: July 17, 2012
    Assignee: The Regents of the University of Michigan
    Inventors: Shaomeng Wang, Dongguang Qin, Jianyong Chen, Shanghai Yu
  • Publication number: 20120178927
    Abstract: The invention relates to novel cycloalkylphenyl-substituted cyclic ketoenols of the formula (I) in which J, X, Y, m and CKE are as defined above, to processes and intermediates for their preparation and to their use as pesticides and/or herbicides. Moreover, the invention relates to selective herbicidal compositions comprising, firstly, the cycloalkylphenyl-substituted cyclic ketoenols and, secondly, a crop plant compatibility-improving compound. The invention furthermore relates to increasing the activity of crop protection compositions comprising compounds of the formula (I) by adding ammonium or phosphonium salts and, if appropriate, penetrants.
    Type: Application
    Filed: July 12, 2011
    Publication date: July 12, 2012
    Applicant: Bayer CropScience AG
    Inventors: Reiner FISCHER, Thomas BRETSCHNEIDER, Stefan LEHR, Dieter FEUCHT, Eva-Maria FRANKEN, Olga MALSAM, Alfred ANGERMANN, Guido BOJACK, Christian ARNOLD, Martin Jeffery HILLS, Heinz KEHNE, Christopher Hugh ROSINGER
  • Publication number: 20120172575
    Abstract: 1,3-Dipole-functional compounds (e.g., azide functional compounds) can be reacted with certain alkynes in a cyclization reaction to form heterocyclic compounds. Useful alkynes (e.g., strained, cyclic alkynes) and methods of making such alkynes are also disclosed. The reaction of 1,3-dipole-functional compounds with alkynes can be used for a wide variety of applications including the immobilization of biomolecules on a substrate.
    Type: Application
    Filed: March 13, 2012
    Publication date: July 5, 2012
    Applicant: University of Georgia Research Foundation, Inc.
    Inventors: GEERT-JAN BOONS, Jun Guo, Xinghai Ning, Margaretha Wolfert
  • Patent number: 8203007
    Abstract: The invention described herein provides a novel lactide monomer derivative and process for preparing the lactide monomer derivative. The monomer derivative of the invention is bifunctional in nature, and can be employed a variety of efficient synthesis processes to prepare various polymers. Further, the bifunctional monomer derivative can be used to prepare various intermediate-stage compounds and polymers, which in turn can be used to synthesize other compounds, polymers, copolymers and composites. The lactide monomer derivative has a bifunctional norbornene spiro lactide structure, spiro[6-methyl-1,4-dioxane-2,5-dione-3,2?-bicyclo[2.2.1]hept[5]ene], and structure as follows: and stereoisomers thereof. The lactide monomer derivative is bifunctional in that either 1) the norbornene ring, 2) lactide ring, or 3) both, can be opened and used in polymer synthesis for the backbone or the reactive branch for other polymeric syntheses.
    Type: Grant
    Filed: June 8, 2009
    Date of Patent: June 19, 2012
    Assignee: Regents of the University of Minnesota
    Inventors: Feng Jing, Marc Hillmyer
  • Publication number: 20120129833
    Abstract: 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 diabetes, obesity, hyperlipidaemia, fatty livers and of disorders of the cardiovascular system.
    Type: Application
    Filed: August 19, 2011
    Publication date: May 24, 2012
    Applicant: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Ningshu LIU, Kai Thede, Philip Lienau, Arne Scholz, Maher Najjar, Ulf Bomer, Knut Eis, Reiner Fischer
  • Publication number: 20120128722
    Abstract: This invention relates to novel polyether ionophores, formulations comprising same, and to methods of making and using these compounds and formulations for the treatment and/or prevention of parasitic infection in animals and humans. These compounds exhibit improved safety profiles and/or efficacies as compared to parent compounds.
    Type: Application
    Filed: November 16, 2011
    Publication date: May 24, 2012
    Inventors: Jean Delaveau, Emile Vialle, Marc Lemaire, Stephane Pellet-Rostaing, Bruno Andrioletti
  • Publication number: 20120122136
    Abstract: Provided is a compound comprising the structure: (SIG)-(SI-MOD)m. In this compound, SIG is a signaling molecule, SI is a self-immolative structure bound to SIG such that SIG has a reduced signal relative to the signal of SIG without SI, MOD is a moiety bound to SI that is subject to modification by an activator, and m is an integer from 1 to about 10. With this compound, when MOD is modified by an activator, SI is destabilized and self-cleaved from SIG such that SIG generates an increased signal. Also provided is a method of determining whether a sample comprises an activator, using the above-described compound. Additionally provided is a method of determining whether a cell comprises a nitroreductase using the above-described compound where nitroreductase is the activator. Further provided is a method of determining whether a mammalian cell is hypoxic using the above-described compound where nitroreductase is the activator.
    Type: Application
    Filed: November 16, 2010
    Publication date: May 17, 2012
    Applicant: ENZO LIFE SCIENCES, INC., C/O ENZO BIOCHEM, INC.
    Inventors: Maciej Szczepanik, Irina V. Lebedeva, Yuejun Xiang, Praveen Pande, Wayne Forrest Patton
  • Patent number: 8148423
    Abstract: Provided herein are fluorophore compounds including rhodol and rhodamine compounds which can be used as fluorescent labels and/or fluorogenic probes and methods of making same. Provided also herein are methods that can be used to track, measure, detect, or screen biological species such as protein, DNA, enzyme, antibody, organelle, cell, tissue, drug, hormone, nucleotide, nucleic acid, polysaccharide or lipid in living organisms. Specifically, the methods include the steps of contacting any of the fluorophore compounds, rhodol compounds and rhodamine compounds disclosed herein with the biological species to form one or more fluorescent compounds, and measuring fluorescence properties of the fluorescent compounds. Provided also herein are high-throughput screening fluorescent methods for detecting or screening biological species.
    Type: Grant
    Filed: April 3, 2009
    Date of Patent: April 3, 2012
    Assignees: Versitech Limited, Morningside Ventures Limited
    Inventors: Dan Yang, Tao Peng
  • Patent number: 8138334
    Abstract: This invention concerns substituted oxa-diaza-spiro-[5.5]-undecanone derivatives having neurokinin antagonistic activity, in particular an NK1 antagonistic activity, an NK3 antagonistic activity, a combined NK1/NK2 antagonistic activity and a combined NK1/NK2/NK3 antagonistic activity, their preparation, compositions comprising them and their use as a medicine, in particular for the treatment and/or prophylaxis of schizophrenia, emesis, anxiety and depression, irritable bowel syndrome (IBS), circadian rhythm disturbances, pre-eclampsia, nociception, pain, in particular visceral and neuropathic pain, pancreatitis, neurogenic inflammation, asthma, chronic obstructive pulmonary disease (COPD) and micturition disorders such as urinary incontinence.
    Type: Grant
    Filed: March 3, 2006
    Date of Patent: March 20, 2012
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Frans Eduard Jenssens, Sophie Coupa, Alain Philippe Poncelet, Bruno Schoentjes
  • Patent number: RE44734
    Abstract: This invention relates to processes for the production of 3-oxo-pregnane-21,17-carbolactones of formula II as well as 3-oxo-pregn-4-ene-21,17-carbolactones of formula III by the metal-free oxidation of 17-(3-hydroxypropyl)-3,17-dihydroxyandrostanes of formula I In addition, the invention relates to the dichloromethane hemisolvate of 6B,7B;15?,16?-diethylene-3-oxo-17?-pregnan-5?-ol-21,17-carbolactone (IV) as such.
    Type: Grant
    Filed: May 12, 2011
    Date of Patent: January 28, 2014
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Carsten Seilz, Hartmut Seba