Carboxamides (i.e., Q-co-hnh, Wherein Q Is A Substituent Having Carbon Bonded Directly To The Carbonyl Or Is Hydrogen And Wherein Any Substituent Replacing One Or Both Hydrogens Shown Will Be Referred To As E) Patents (Class 564/123)
  • Patent number: 8722929
    Abstract: This invention provides compounds of formula A and formula B which are modulators of potassium ion channels and are useful for the treatment of seizure disorders.
    Type: Grant
    Filed: October 10, 2007
    Date of Patent: May 13, 2014
    Assignee: Valeant Pharmaceuticals International
    Inventors: Jean-Michel Vernier, Jianlan Song, Huanming Chen, Zhi Hong
  • Patent number: 8716527
    Abstract: Methods of treating or suppressing oxidative stress diseases including mitochondrial diseases, impaired energy processing disorders, neurodegenerative diseases and diseases of aging are disclosed, as well as compounds useful in the methods of the invention, such as 2- substituted-p-quinone derivatives as disclosed herein.
    Type: Grant
    Filed: March 4, 2009
    Date of Patent: May 6, 2014
    Assignee: Edison Pharmaceuticals, Inc.
    Inventors: Andrew W. Hinman, Kieron E. Wesson, Orion D. Jankowski, Paul Mollard, William D. Shrader, Christopher R. Cornell
  • Publication number: 20140120544
    Abstract: A method for nucleic acid isolation comprising: receiving a binding moiety solution within a process chamber; mixing the binding moiety solution with a biological sample, within the process chamber, in order to produce a moiety-sample mixture; incubating the moiety-sample mixture during a time window, thereby producing a solution comprising a set of moiety-bound nucleic acid particles and a waste volume; separating the set of moiety-bound nucleic acid particles from the waste volume; washing the set of moiety-bound nucleic acid particles; and releasing a nucleic acid sample from the set of moiety-bound nucleic acid particles. The method preferably utilizes a binding moiety comprising at least one of poly(allylamine) and polypropylenimine tetramine dendrimer, both of which reversibly bind and unbind to nucleic acids based upon environmental pH.
    Type: Application
    Filed: October 22, 2013
    Publication date: May 1, 2014
    Applicant: NeuMoDx Molecular, Inc.
    Inventors: Sundaresh Brahmasandra, Michelle Mastronardi, Elizabeth Craig, Maureen Carey
  • Publication number: 20140121217
    Abstract: The invention relates to compounds of structural formula (I): or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof, wherein A, Y, L, R1, W1 and W2 are defined herein. These compounds are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.
    Type: Application
    Filed: January 2, 2014
    Publication date: May 1, 2014
    Applicant: Synta Pharmaceuticals Corp.
    Inventors: Shoujun Chen, Lijun Sun, Jun Jiang, Yu Xie
  • Patent number: 8697912
    Abstract: The present invention relates to an N-(1-hydroxyethyl)carboxamide compound represented by formula (1) (in the formula, RA and RB represent independently from each other a hydrogen atom or an alkyl group having 1 to 4 carbon atoms except for a case where RA and RB represent a hydrogen atom at the same time) and a method for producing the same; a method for producing an N-(1-alkoxyethyl)carboxamide compound; a method for producing an N-vinyl carboxylic acid amide compound; and a method for producing an N-vinyl carboxylic acid amide (co)polymer. An N-(1-alkoxyethyl)carboxamide compound can be obtained by reacting N-(1-hydroxyethyl)carboxamide compound with alcohol in the presence of an acid catalyst, and an N-vinyl carboxylic acid amide compound, which is a monomer of the N-vinyl carboxylic acid amide (co)polymer, can be obtained by thermally decomposing or catalytically decomposing the N-(1-alkoxyethyl)carboxamide compound.
    Type: Grant
    Filed: January 5, 2010
    Date of Patent: April 15, 2014
    Assignee: Showa Denko K.K.
    Inventors: Keisuke Ohta, Syunichi Nagamatsu, Tetsuya Ishii
  • Publication number: 20140080802
    Abstract: The present invention relates to compounds of formula (I): or a pharmaceutically acceptable salt, hydrate, solvate, or prodrug thereof, wherein U, J, V, X, R2a, R2b, R2c, R5 and t are as described herein. The present invention relates generally to inhibitors of histone deacetylase and to methods of making and using them. These compounds are useful for promoting cognitive function and enhancing learning and memory formation. In addition, these compounds are useful for treating, alleviating, and/or preventing various conditions, including for example, neurological disorders, memory and cognitive function disorders/impairments, extinction learning disorders, fungal diseases and infections, inflammatory diseases, hematological diseases, and neoplastic diseases in humans and animals.
    Type: Application
    Filed: October 28, 2013
    Publication date: March 20, 2014
    Inventors: Edward Holson, Florence Fevrier Wagner, Michel Weiwer, Li-Huei Tsai, Stephen Haggarty, Yan-Ling Zhang
  • Patent number: 8673982
    Abstract: This invention relates to certain ceramide-analogues of FTY720 (2-amino-2-[2-(4-octylphenyl)ethyl]propane-1,3-diol; fingolimod). In particular, the present invention relates to pharmaceutical compositions comprising these compounds, as well as processes for their preparation and their use in the treatment of autoimmune conditions, such as multiple sclerosis.
    Type: Grant
    Filed: February 23, 2010
    Date of Patent: March 18, 2014
    Assignee: Novartis AG
    Inventors: Volker Brinkmann, Guido Jordine, Markus Zollinger, Claudia Sayer
  • Patent number: 8664274
    Abstract: Compounds, methods and pharmaceutical compositions for treating viral infections, by administering certain novel sulfonyl semicarbazides, carbonyl semicarbazides, semicarbazides, ureas and related compounds in therapeutically effective amounts are disclosed. Methods for preparing the compounds and methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment and prophylaxis of viral infections such as caused by hemorrhagic fever viruses is disclosed, i.e., including but not limited to, Arenaviridae (Junin, Machupo, Guanarito, Sabia, Lassa, Tacaribe, Pinchinde, and VSV), Filoviridae (ebola and Marburg viruses), Flaviviridae (yellow fever, omsk hemorrhagic fever and Kyasanur Forest disease viruses), and Bunyaviridae (Rift Valley fever).
    Type: Grant
    Filed: July 6, 2011
    Date of Patent: March 4, 2014
    Assignee: Siga Technologies, Inc.
    Inventors: Dongcheng Dai, Tove Bolken, Dennis E. Hruby, Thomas R. Bailey
  • Patent number: 8658697
    Abstract: Compounds, methods and pharmaceutical compositions for treating viral infections, by administering certain novel sulfonyl semicarbazides, carbonyl semicarbazides, semicarbazides, ureas and related compounds in therapeutically effective amounts are disclosed. Methods for preparing the compounds and methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment and prophylaxis of viral infections such as caused by hemorrhagic fever viruses is disclosed, i.e., including but not limited to, Arenaviridae (Junin, Machupo, Guanarito, Sabia, Lassa, Tacaribe, Pinchinde, and VSV), Filoviridae (ebola and Marburg viruses), Flaviviridae (yellow fever, omsk hemorrhagic fever and Kyasanur Forest disease viruses), and Bunyaviridae (Rift Valley fever).
    Type: Grant
    Filed: October 26, 2010
    Date of Patent: February 25, 2014
    Assignee: Siga Technologies, Inc.
    Inventors: Dongcheng Dai, Tove Bolken, Dennis E. Hruby, Thomas R. Bailey
  • Patent number: 8653002
    Abstract: The present invention relates to aqueous suspension concentrate formulation for plant protection comprising: 2-chloro-5-[3,6-dihydro-3-methyl-2,6-dioxo-4-(trifluoromethyl)-1-(2H)pyrimidinyl]-4-fluoro-N-[[methyl(1-methylethyl)amino]sulfonyl]benzamide in the form of its crystalline anhydrate; at least one non-ionic surfactant selected from polyoxyethylene-polyoxy-C3-C4-alkylene block copolymers; at least one anionic surfactant comprising at least one arylsulfonate group; and water; wherein the pH value of the formulation is in the range of 3 to 7.
    Type: Grant
    Filed: August 26, 2010
    Date of Patent: February 18, 2014
    Assignee: BASF SE
    Inventors: Michael Krapp, Wolfgang Gregori, Klaus Kolb, Bernd Sievernich, Heidi Emilia Saxell, Joerg Steuerwald, Steven Bowe, Rex Liebl, Terrance M. Cannan
  • Patent number: 8642658
    Abstract: Compounds, methods, uses, compositions, kits and packages for the prevention and/or treatment of neural injury or a neurodegenerative disease, based on the use of a retinoic acid derivative, such as fenretinide, and/or analogs, derivatives, pro-drugs, precursors thereof, and/or salts thereof, are described.
    Type: Grant
    Filed: February 20, 2009
    Date of Patent: February 4, 2014
    Assignee: Royal Institution for the Advancement of Learning/McGill University
    Inventors: Danuta Radzioch, Samuel David, Ruben Lopez-Vales, Thomas Skinner
  • Patent number: 8618169
    Abstract: Compounds, compositions and methods are provided which are useful in the treatment of conditions such as central or peripheral nervous system disorders through the modulation of potassium ion flux through voltage-dependent potassium channels and/or depressing cortical and/or peripheral neuron activity are disclosed. Novel derivatives of N-phenylanthranilic acid are also disclosed.
    Type: Grant
    Filed: March 20, 2012
    Date of Patent: December 31, 2013
    Assignee: Ramot at Tel-Aviv University Ltd.
    Inventors: Bernard Attali, Asher Peretz
  • Patent number: 8614251
    Abstract: The invention provides a new crystalline form of agomelatine, preparation and use thereof. The X-ray powder diffraction diagram of the agomelatine crystalline form shows main peaks at the diffraction angles 2? 11.13°, 11.82°, 17.49°, 18.29°, 19.48°, 19.72°, 20.50°, 21.76°, 22.54°, 22.97°, 24.56°, 25.36°, 27.16° and 31.93°. Said new crystalline form is characterized by high purity, stability and good reproducibility, and thus is advantageous for the pharmaceutical formulation. In addition, the stability and solubility of said crystalline form are also superior over the several existing crystalline forms.
    Type: Grant
    Filed: March 9, 2010
    Date of Patent: December 24, 2013
    Assignee: Les Laboratories Servier
    Inventors: Hanbin Shan, Peng Zhang, Zhedong Yuan, Xudong Jiang, Yu Huang, Hubo Wang, Xufeng Cao, Xingdong Cheng, Xiong Yu
  • Publication number: 20130256228
    Abstract: This disclosure describes draw solution compositions for FO processes which increase the available membrane area for permeation and are also amenable to reconcentration with standard techniques, such as membrane filtration and evaporative technologies. The composition are comprised of a water soluble draw solute having surface active properties, i.e., a surfactant.
    Type: Application
    Filed: March 14, 2013
    Publication date: October 3, 2013
    Inventors: Upen J. Bharwada, Isaac V. Farr
  • Publication number: 20130245065
    Abstract: The present invention relates to processes for the preparation of quinoline-3-carboxamide derivatives, such as sodium 5-chloro-3-(ethylphenylcarbamoyl)-1-methyl-2-oxo-1,2-dihydroquinolin-4-olate (Laquinimod sodium). The present invention further relates to intermediates formed in such processes.
    Type: Application
    Filed: November 28, 2011
    Publication date: September 19, 2013
    Applicant: MAPI PHARMA LTD.
    Inventors: Ehud Marom, Michael Mizhiritskii, Shai Rubnov
  • Patent number: 8536229
    Abstract: The invention provides compounds of formula I wherein n, A, R, R?, R?, RO, X and Y are as defined in the description, and their preparation. The compounds of formula I are useful as pharmaceuticals.
    Type: Grant
    Filed: September 22, 2011
    Date of Patent: September 17, 2013
    Assignee: Novartis AG
    Inventors: Fabrizio Gasparini, Yves Auberson, Silvio Ofner, Terance W Hart, Kaspar Zimmerman
  • Patent number: 8536355
    Abstract: Disclosed herein is a process for producing Dialkyl substituted fatty acids amides. More particularly the present invention provides a process for producing pure form of N,N-dimethylamide of aliphatic carboxylic acids, wherein the aliphatic carboxylic acid is Octanoic Acid and Hexanoic Acid. The disclosed process comprises condensing Alkanoyl Chloride with dilute solution of Dialkylamine at a temperature of about 8 to 12° C. and isolating the crude by salting out the reaction mixture employing Sodium Chloride and distilling the same under vacuum.
    Type: Grant
    Filed: September 22, 2005
    Date of Patent: September 17, 2013
    Inventors: Ramachandran Radhakrishnan, Sisir K. Adhikari
  • Publication number: 20130224790
    Abstract: The invention includes a compound represented by the following structural formula: wherein is described herein. The compounds of the invention are useful in staining embryonic stem cells.
    Type: Application
    Filed: August 26, 2011
    Publication date: August 29, 2013
    Applicants: AGENCY FOR SCIENCE, TECHNOLOGY AND RESEARCH, NATIONAL UNIVERSITY OF SINGAPORE
    Inventors: Young-Tae Chang, Sung Chan Lee, Nam Young Kang
  • Publication number: 20130216486
    Abstract: The present invention provides synthetic routes for preparing various isomers of cyclohexane-based coolants, such as menthyl esters and menthanecarboxamide derivatives, in particular those substituted at the amide nitrogen, for example with an aromatic ring or aryl moiety. Such structures have high cooling potency and long lasting sensory effect, which make them useful in a wide variety of consumer products. One synthetic route involves a copper catalyzed coupling of a primary menthanecarboxamide with an aryl halide, such reaction working best in the presence of potassium phosphate and water. Using this synthetic route, specific isomers can be prepared including the menthanecarboxamide isomer having the same configuration as l-menthol and new isomers such as a neoisomer having opposite stereochemistry at the carboxamide (C-1) position. The neoisomer unexpectedly has potent and long lasting cooling effect.
    Type: Application
    Filed: March 20, 2013
    Publication date: August 22, 2013
    Applicant: The Procter & Gamble Company
    Inventor: The Procter & Gamble Company
  • Patent number: 8513307
    Abstract: Novel N-phenylacetamide compounds of formula (I): and cosmetic and pharmaceutical compositions containing same are useful for treating disorders of the sebaceous gland, e.g., acne, or have cosmetic applications.
    Type: Grant
    Filed: March 5, 2010
    Date of Patent: August 20, 2013
    Assignee: Galderma Research & Development
    Inventor: Thibaud Portal
  • Patent number: 8513431
    Abstract: Disclosed is a method for preparing a compound of Formula 1 wherein R1 is CHX2, CX3, CX2CHX2 or CX2CX3; each X is independently Cl or F; Z is optionally substituted phenyl; and Q is phenyl or 1-naphthalenyl, each optionally substituted as defined in the disclosure; comprising contacting a compound of Formula 2 with hydroxylamine in the presence of a base. The present invention also relates to novel compounds of Formula 2, useful as starting materials for the aforedescribed method.
    Type: Grant
    Filed: July 9, 2012
    Date of Patent: August 20, 2013
    Assignee: E.I. du Pont de Nemours and Company
    Inventors: Gary David Annis, Brenton Todd Smith
  • Publication number: 20130197226
    Abstract: The present invention features pharmaceutical compositions and methods of using the pharmaceutical compositions for treating left ventricular diastolic dysfunction. In particular, the pharmaceutical compositions include an apolipoprotein complex comprising a lipid fraction and a protein fraction.
    Type: Application
    Filed: July 19, 2011
    Publication date: August 1, 2013
    Inventors: Jean-Claude Tardif, David Busseuil, Éric Rhéaume
  • Publication number: 20130197257
    Abstract: A process for the preparation of a compound of formula (I): which is useful as an intermediate in the preparation of pharmaceutically active compounds.
    Type: Application
    Filed: March 14, 2013
    Publication date: August 1, 2013
    Applicant: Hoffmann-La Roche Inc.
    Inventor: Hoffmann-La Roche Inc.
  • Publication number: 20130190296
    Abstract: Provided are small-molecule Trp-p8 modulators, including Trp-p8 agonists and Tip-p8 antagonists, and compositions comprising small-molecule Trp-p8 agonists as well as methods for identifying and characterizing novel small-molecule Trp-p8 modulators and methods for decreasing viability and/or inhibiting growth of Trp-p8 expressing cells, methods for activating Trp-p8-mediated cation influx, methods for stimulating apoptosis and/or necrosis, and related methods for the treatment of diseases, including cancers such as lung, breast, colon, and/or prostate cancers as well as other diseases, such as benign prostatic hyperplasia, that are associated with Trp-p8 expression.
    Type: Application
    Filed: November 20, 2012
    Publication date: July 25, 2013
    Applicant: Dendreon Corporation
    Inventor: Dendreon Corporation
  • Patent number: 8492588
    Abstract: The present invention relates to benzyloxyanilide derivatives having the following structural formula: The compounds of the present invention are useful for the treatment and prevention of diseases and disorders which are affected by activation or modulation of potassium ion channels. One such condition is seizure disorders.
    Type: Grant
    Filed: May 29, 2012
    Date of Patent: July 23, 2013
    Assignee: Valeant Pharmaceuticals International
    Inventors: Jim Zhen Wu, Jean-Michel Vernier, Huanming Chen, Jianlan Song
  • Patent number: 8481593
    Abstract: The invention relates to the use of para-coumaric acid or para-hydroxycinnamic acid derivatives in cosmetic or dermatological compositions, specifically to the use of at least one compound derived from para-coumaric acid having a general formula (I) below: in which, especially, Z represents an oxygen or an —NH— group; X and Y are identical and each represent a CH or CH2 group, as an active principle with depigmenting, free-radical-scavenging and/or antiinflammatory activity. The invention also relates to the use of the above compounds for cosmetic care or for the preparation of a pharmaceutical composition, especially for depigmenting an area of skin, having antiradical and/or antiinflammatory activity.
    Type: Grant
    Filed: June 3, 2011
    Date of Patent: July 9, 2013
    Assignees: BASF Beauty Care Solutions S.A.S., Universite Joseph Fourier-Grenoble 1
    Inventors: Sabrina Okombi, Delphine Rival, Ahcene Boumendjel, Anne-Marie Mariotte, Eric Perrier
  • Publication number: 20130172388
    Abstract: Cannabionid receptor-2 inverse antagonists include compounds represented by Formula IV, or a pharmaceutically acceptable salt thereof: wherein: R1 and R2 are independently H, alkyl, or alkenyl; R3 is alkyl, alkenyl, aryl, aralkyl, aralkenyl, heterocyclyl, heterocyclylalkyl, heteroaryl, heteroarylalkyl; R4 and R5 are independently a bond, alkylenyl, or alkenylenyl; each R6 and R7 is independently selected from the group consisting of OH, F, Cl, Br, I, (C1-C6)alkyl, alkoxy, amino, COOH, CONH2, SO3H, PO3H2, CN, SH, NO2 and CF3; and p and q are independently 0, 1, 2, 3, 4, or 5. Such compounds may be used to treat osteoporosis or multiple myeloma.
    Type: Application
    Filed: December 14, 2012
    Publication date: July 4, 2013
    Applicant: University of Pittsburgh -- Of the Commonwealth System of Higher Education
    Inventor: University of Pittsburgh -- Of the Commonwealth System of Higher Education
  • Patent number: 8471063
    Abstract: Described herein are peptide derivatives and peptidomimetics as inhibitors for transglutaminases, methods for their preparation, pharmaceutical compositions containing said compounds as well as uses of said transglutaminase inhibitors in particular for the treatment of coeliac disease and transglutaminase dependent diseases.
    Type: Grant
    Filed: November 8, 2007
    Date of Patent: June 25, 2013
    Assignee: Zedira GmbH
    Inventor: Kai Oertel
  • Patent number: 8471051
    Abstract: One aspect of the present invention relates to a method for the transition metal (e.g., Cu(I)) mediated amidation of C—H bonds using electron-rich aliphatic azides. In certain embodiments, the methods are useful for the C—H insertion of nitrenes generated and stabilized by a ?-diketiminato metal catalyst. In certain embodiments, said nitrenes are generated from organoazides, or by oxidation of the corresponding amine. Another aspect of the present invention relates to olefin aziridination using said ?-diketiminato metal catalysts. In addition, the methods of the present invention include stereoselective C—H bond aminations and olefin aziridinatons. In certain embodiments, the methods are conducted in an aerobic environment. In certain embodiments, the present invention relates to the use of O2 as an oxidant, wherein water is the byproduct of oxidation; this fact avoids the generation of toxic byproducts and renders the methods atom economical.
    Type: Grant
    Filed: December 5, 2007
    Date of Patent: June 25, 2013
    Assignee: Georgetown University
    Inventor: Timothy H. Warren
  • Patent number: 8460635
    Abstract: Synthetic peptidomimetic derivatives and phenyl group derivatives of Fenretinide (4-HPR) are disclosed, as are their uses as therapeutic, diagnostic and imaging agents for cancer and other diseases.
    Type: Grant
    Filed: March 11, 2009
    Date of Patent: June 11, 2013
    Assignee: Albert Einstein College of Medicine of Yeshiva University
    Inventors: Ganjam V. Kalpana, Bhaskar C. Das
  • Publication number: 20130131124
    Abstract: The present invention relates to O-CYCLOPROPYLCYCLOHEXYL-CARBOXANILIDES derivatives of formula (I); their process of preparation, their use as fungicide, particularly in the form of fungicide compositions, and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions.
    Type: Application
    Filed: June 1, 2011
    Publication date: May 23, 2013
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Jörg Nico Greul, Jürgen Benting, Peter Dahmen, Ulrike Wachendorff-Neumann
  • Patent number: 8445541
    Abstract: Methods for concomitant administration of colchicine together with one or more second active agents, e.g., verapamil, are disclosed. Such methods reduce the dangers commonly associated with such concomitant administration and provide additional benefits. Methods of notifying health care practitioners and patients regarding appropriate dosing for concomitant administration of colchicine together with second active agents are also provided.
    Type: Grant
    Filed: April 24, 2012
    Date of Patent: May 21, 2013
    Assignee: Takeda Pharmaceuticals U.S.A., Inc.
    Inventor: Matthew W. Davis
  • Publication number: 20130121909
    Abstract: A method of purification and modification of carbon nanoproduct involves forcing a mixture of the dehydrated air or oxygen or ozone or any combination thereof through the carbon nanoproduct under pressure up to 0.8 MPa accompanied by mixing of the carbon nanoproduct and heating in the temperature range from +20 to +550° C. This abstract is not to be considered limiting, since other embodiments may deviate from the features described in this abstract.
    Type: Application
    Filed: December 18, 2012
    Publication date: May 16, 2013
    Inventors: Igor Leonidovich Petrov, Yuriy Alekseevich Skryabin, Olga Alexander Shenderova
  • Patent number: 8440722
    Abstract: Methods for concomitant administration of colchicine together with one or more second active agents, e.g., verapamil, are disclosed. Such methods reduce the dangers commonly associated with such concomitant administration and provide additional benefits. Methods of notifying health care practitioners and patients regarding appropriate dosing for concomitant administration of colchicine together with second active agents are also provided.
    Type: Grant
    Filed: April 24, 2012
    Date of Patent: May 14, 2013
    Assignee: Takeda Pharamceuticals U.S.A., Inc.
    Inventor: Matthew W. Davis
  • Patent number: 8440721
    Abstract: Methods for concomitant administration of colchicine together with one or more second active agents, e.g., ketoconazole and ritonavir, are disclosed. Such methods reduce the dangers commonly associated with such concomitant administration and provide additional benefits. Methods of notifying health care practitioners and patients regarding appropriate dosing for concomitant administration of colchicine together with second active agents are also provided.
    Type: Grant
    Filed: July 18, 2011
    Date of Patent: May 14, 2013
    Assignee: Takeda Pharmaceuticals U.S.A., Inc.
    Inventor: Matthew W. Davis
  • Patent number: 8426643
    Abstract: The present invention provides synthetic routes for preparing various isomers of cyclohexane-based coolants, such as menthyl esters and menthanecarboxamide derivatives, in particular those substituted at the amide nitrogen, for example with an aromatic ring or aryl moiety. Such structures have high cooling potency and long lasting sensory effect, which make them useful in a wide variety of consumer products. One synthetic route involves a copper catalyzed coupling of a primary menthanecarboxamide with an aryl halide, such reaction working best in the presence of potassium phosphate and water. Using this synthetic route, specific isomers can be prepared including the menthanecarboxamide isomer having the same configuration as l-menthol and new isomers such as a neoisomer having opposite stereochemistry at the carboxamide (C-1) position. The neoisomer unexpectedly has potent and long lasting cooling effect.
    Type: Grant
    Filed: August 14, 2009
    Date of Patent: April 23, 2013
    Assignee: The Procter & Gamble Company
    Inventors: Kenneth Edward Yelm, Gregory Mark Bunke, John Christian Haught
  • Publication number: 20130090452
    Abstract: A process for reacting formaldehyde cyanohydrin (FACH) with ethylenediamine (EDA) in a reactor with limited backmixing at a temperature in the range from 20 to 120° C., wherein the residence time in the reactor is 300 seconds or less.
    Type: Application
    Filed: August 30, 2012
    Publication date: April 11, 2013
    Applicant: BASF SE
    Inventors: Hermann Luyken, Sebastian Ahrens, Gordon Brasche, Jens Baldamus, Robert Baumann, Randolf Hugo, Stephanie Jaegli, Johann-Peter Melder, Jörg Pastre, Boris Buschhaus
  • Publication number: 20130090453
    Abstract: A process for preparing TETA and/or DETA by hydrogenating EDDN and/or EDMN with hydrogen in the presence of a catalyst, which comprises preparing EDDN and/or EDMN from FA, HCN and EDA in the presence of toluene as a solvent and performing the hydrogenation in suspension mode in the presence of THF.
    Type: Application
    Filed: August 31, 2012
    Publication date: April 11, 2013
    Applicant: BASF SE
    Inventors: Hermann Luyken, Sebastian Ahrens, Gordon Brasche, Jens Baldamus, Robert Baumann, Randolf Hugo, Stephanie Jaegli, Johann-Peter Melder, Jõrg Pastre, Boris Buschhaus
  • Patent number: 8415396
    Abstract: Stable ultrapure colchicine compositions comprising ultrapure colchicine and a pharmaceutically acceptable excipient are described. The compositions can be tablets. Methods for preparing such compositions and methods of use are also disclosed. Methods of treating gout flares with colchicine compositions are also disclosed.
    Type: Grant
    Filed: April 20, 2012
    Date of Patent: April 9, 2013
    Assignee: Takeda Pharmaceuticals U.S.A., Inc.
    Inventors: Matthew W. Davis, Hengsheng Feng
  • Patent number: 8415395
    Abstract: Stable ultrapure colchicine compositions comprising ultrapure colchicine and a pharmaceutically acceptable excipient are described. The compositions can be tablets. Methods for preparing such compositions and methods of use are also disclosed. Methods of treating gout flares with colchicine compositions are also disclosed.
    Type: Grant
    Filed: April 19, 2012
    Date of Patent: April 9, 2013
    Assignee: Takeda Pharmaceuticals U.S.A., Inc.
    Inventors: Matthew W. Davis, Hengsheng Feng
  • Publication number: 20130085286
    Abstract: A process for preparing amines of the formula (II) R1—NH—CH2—CH2—NH2??(II) in which R1 is hydrogen or radicals of the formula x is integers from zero to two, by reacting nitriles of the formula (I) R2—NH—CH2—CN??(I) in which R2 is hydrogen or radicals of the formula and R3 is the NC— or H2N—CH2- radicals and x is integers from zero to two, with hydrogen in the presence of a catalyst in suspension mode or in a fixed bed, wherein the space velocity on the catalyst, based on the catalyst surface area, is 10?6 to 10?4 kg of nitrile of the formula (I) per m2 of catalyst surface area and hour, the catalyst surface area being determined by the BET method.
    Type: Application
    Filed: August 31, 2012
    Publication date: April 4, 2013
    Applicant: BASF SE
    Inventors: Hermann Luyken, Sebastian Ahrens, Gordon Brasche, Jens Baldamus, Robert Baumann, Randolf Hugo, Stephanie Jaegli, Johann-Peter Melder, Jõrg Pastre, Boris Buschhaus
  • Patent number: 8410247
    Abstract: Water soluble reagents and methods for the formation of an amide bond between a phosphinothioester and an azide in an aqueous medium. The phosphinothioester is generated using a water-soluble phosphinothiol reagent. This reaction allows formation of an amide bond between a wide variety of chemical species including amino acids, peptides or protein fragments in an aqueous solution. Of particular interest, this reaction allows for the formation of an amide bond in a physiological setting. In a specific embodiment, this invention provides reagents and methods for peptide ligation in an aqueous medium. The reaction eliminates the need for a cysteine residue and is traceless leaving no residual atoms in the ligated peptide product.
    Type: Grant
    Filed: August 24, 2009
    Date of Patent: April 2, 2013
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Ronald T. Raines, Annie Tam, Matthew B. Soellner
  • Publication number: 20130079492
    Abstract: A process for preparing EDDN and/or EDMN by conversion of FA, HCN and EDA, the reaction being effected in the presence of water, and, after the conversion, water being depleted from the reaction mixture in a distillation column, which comprises performing the distillation in the presence of an organic solvent which has a boiling point between water and EDDN and/or EDMN at the distillation pressure existing in the column or which forms a low-boiling azeotrope with water.
    Type: Application
    Filed: August 30, 2012
    Publication date: March 28, 2013
    Applicant: BASF SE
    Inventors: Hermann Luyken, Sebastian Ahrens, Gordon Brasche, Jens Baldamus, Robert Baumann, Randolf Hugo, Stephanie Jaegli, Johann-Peter Melder, Jörg Pastre, Boris Buschhaus
  • Publication number: 20130079556
    Abstract: The invention provides a method for producing amides via the reaction of aldehydes and amines with oxygen adsorbed on a metallic silver or silver alloy catalyst.
    Type: Application
    Filed: January 25, 2011
    Publication date: March 28, 2013
    Inventors: Robert J. Madix, Ling Zhou, Bingjun Xu, Cynthia M. Friend, Cassandra G. Freyschlag
  • Publication number: 20130060002
    Abstract: A process is disclosed for separating the output from the reaction of EDDN or EDMN with hydrogen in the presence of THF, a catalyst, TETA or DETA, water, and optionally organic compounds having higher and lower boiling points than TETA or DETA. Hydrogen is removed, and the output is supplied to a distillation column DK1 in which an azeotrope, optionally comprising organic compounds with a boiling point lower than TETA or DETA, is removed from the top. A product comprising TETA or DETA is removed from the bottom and passed cinto a distillation column DK2, removing THF. A stream comprising TETA or DETA passes from the bottom of DK2. The DK1 azeotrope is condensed. Phase separation is induced by the addition of an organic solvent essentially immiscible with water, and the mixture is separated. The organic phase is recycled into DK1 and the water phase is discharged.
    Type: Application
    Filed: August 30, 2012
    Publication date: March 7, 2013
    Applicant: BASF SE
    Inventors: Hermann Luyken, Sebastian Ahrens, Gordon Brasche, Jens Baldamus, Robert Baumann, Randolf Hugo, Stephanie Jaegli, Johann-Peter Melder, Jörg Pastre, Boris Buschhaus
  • Publication number: 20130053417
    Abstract: The invention provides a compound that is a CETP activity inhibitor. The compound can increase HDL and at the same time decrease LDL through selective inhibition of CETP activity, the invention also provides for the use of the compound to prevent or treat atherosclerosis or hyperlipidemia.
    Type: Application
    Filed: March 21, 2012
    Publication date: February 28, 2013
    Applicant: JAPAN TOBACCO INC.
    Inventors: Hisashi Shinkai, Kimiya Maeda, Hiroshi Okamoto
  • Publication number: 20130053584
    Abstract: A process for reacting ethylenediamine-formaldehyde adduct (EDFA) and/or ethylene-diamine-monoformaldehyde adduct (EDMFA) with hydrogen cyanide (HCN) in a reactor with limited backmixing at a temperature in the range from 20 to 120° C., wherein the residence time in the reactor is 300 seconds or less.
    Type: Application
    Filed: August 30, 2012
    Publication date: February 28, 2013
    Applicant: BASF SE
    Inventors: Hermann Luyken, Sebastian Ahrens, Gordon Brasche, Jens Baldamus, Robert Baumann, Randolf Hugo, Stephanie Jaegli, Johann-Peter Melder, Jörg Pastre, Boris Buschhaus
  • Publication number: 20130053536
    Abstract: A process for preparing EDDN and/or EDMN by a) conversion of FA, HCN and EDA, the conversion being effected in the presence of water, b) depleting water from the reaction mixture obtained in stage a), and c) treating the mixture from stage b) with an absorbent in the presence of an organic solvent, wherein the adsorbent is a solid acidic adsorbent.
    Type: Application
    Filed: August 30, 2012
    Publication date: February 28, 2013
    Applicant: BASF SE
    Inventors: Hermann Luyken, Sebastian Ahrens, Gordon Brasche, Jens Baldamus, Robert Baumann, Randolf Hugo, Stephanie Jaegli, Johann-Peter Melder, Jörg Pastre, Boris Buschhaus
  • Publication number: 20130041101
    Abstract: The present invention is directed to a composition comprising an amide moiety containing polyol wherein the amide moiety is formed by the reaction of an amine reactive compound with an amine containing compound.
    Type: Application
    Filed: August 9, 2011
    Publication date: February 14, 2013
    Applicant: Huntsman International LLC
    Inventors: Steve Diamanti, Howard P. Klein
  • Publication number: 20130035500
    Abstract: A method of preparing functionalized graphene, comprises treating graphene with an alkali metal in the presence of an electron transfer agent and coordinating solvent, and adding a functionalizing compound. The method further includes quenching unreacted alkali metal by addition of a protic medium, and isolating the functionalized graphene.
    Type: Application
    Filed: August 4, 2011
    Publication date: February 7, 2013
    Applicant: BAKER HUGHES INCORPORATED
    Inventor: Anil K. Sadana