Abstract: Enzymes mediating in the release of compounds characteristic of human malodour and in particular axillary malodour, and compounds that inhibit said enzymes having the general formula (I)
Type:
Application
Filed:
May 9, 2007
Publication date:
November 4, 2010
Applicant:
GIVAUDAN SA
Inventors:
Andreas Natsch, Gonzalo Acuna, Marie-Claude Fournie-Zaluski, Hans Gfeller
Abstract: The present invention relates to a process for preparing 2-fluoroacyl-3-aminoacrylic acid derivatives by reacting fluorinated carboxylic acids with dialkylaminoacrylic acid derivatives and acid halides.
Type:
Application
Filed:
December 16, 2008
Publication date:
October 28, 2010
Applicant:
BAYER CROPSCIENCE AG
Inventors:
Norbert Lui, Thomas Wollner, Jürgen Wieschmeyer, Michael Dockner, Jens-Dietmar Heinrich
Abstract: The present invention provides a method for the synthesis of ?2-amino acids. The method also provides methods yielding ?-substituted ?-amino aldehydes and ?-substituted ?-amino alcohols. The present method according to this invention allows for increased yield and easier purification using minimal chromatography or crystallization. The methods described herein are based on an aldehyde aminomethylation which involves a Mannich reaction between an aldehyde and a formaldehyde-derived N,O-acetal (iminium precursor) and a catalyst, such as, for example, L-proline or a pyrrolidine. The invention allows for large scale, commercial preparation of ?2-amino acids.
Type:
Grant
Filed:
March 26, 2007
Date of Patent:
October 26, 2010
Assignee:
Wisconsin Alumni Research Foundation
Inventors:
Yonggui Chi, Samuel H. Gellman, William C. Pomerantz, William S. Horne, Li Guo, Emily P. English
Abstract: The present invention provides prodrugs of GABA analogs, pharmaceutical compositions of prodrugs of GABA analogs and methods for making prodrugs of GABA analogs. The present invention also provides methods for using prodrugs of GABA analogs and methods for using pharmaceutical compositions of prodrugs of GABA analogs for treating or preventing common diseases and/or disorders.
Type:
Application
Filed:
July 1, 2010
Publication date:
October 21, 2010
Applicant:
XenoPort, Inc.
Inventors:
Mark A. Gallop, Kenneth C. Cundy, Cindy X. Zhou, Fayang G. Qiu, Fenmei Yao, Jia-Ning Xiang, Ian R. Ollmann
Abstract: A method of identifying a compound that modulates NCKX-mediated calcium ion exchange across a cell membrane, the method comprising the steps of providing an adherent cell, the cell membrane of which comprises a NCKX polypeptide or a functionally equivalent variant thereof, exposing the cell in suspension to a fluorescent calcium-sensitive dye, thereby causing intracellular uptake of the dye, settling the cell onto a solid support without allowing the cell to adhere to the solid support, exposing the cell to a test compound, exposing the cell to calcium and potassium ions, and measuring fluorescence from the intracellular calcium-sensitive dye after exposure of the cell to the test compound and the calcium and potassium ions, thereby to determine the rate and/or amount of calcium ion exchange across the cell membrane in the presence of the test compound.
Type:
Application
Filed:
November 11, 2008
Publication date:
September 30, 2010
Inventors:
Richard Martin Ogborne, Paul Petrus Marius Schnetkamp
Abstract: The present invention is directed in particular to dipeptide-like compounds derived from functionally substituted amino acids, having fatty acid chains bound thereto through amidification of the amine functional groups of said dipeptide-like compounds, one end portion of which bears an accessory functional side chain spacer, with the other end portion being an acid group either in neutral or charged state. Compounds of the present invention have immunomodulating properties like adjuvants, In addition, compounds of the invention can be grafted on a given antigen in order to modulate or tune the immune response or can be equally grafted on a pharmaceutical carrier to enhance the therapeutic effect or targeting thereof. Accordingly, compounds of the invention find use in human and veterinary medicine both as immunogens and diagnostic tools.
Type:
Grant
Filed:
December 21, 2000
Date of Patent:
September 21, 2010
Assignee:
OM Pharma
Inventors:
Jacques Bauer, Olivier Richard Martin, Sylvain Rodriguez
Abstract: A method of fractionating biomass, by permeability conditioning biomass suspended in a pH adjusted solution of at least one water-based polar solvent to form a conditioned biomass, intimately contacting the pH adjusted solution with at least one non-polar solvent, partitioning to obtain an non-polar solvent solution and a polar biomass solution, and recovering cell and cell derived products from the non-polar solvent solution and polar biomass solution. Products recovered from the above method. A method of operating a renewable and sustainable plant for growing and processing algae.
Type:
Application
Filed:
March 10, 2010
Publication date:
September 16, 2010
Inventors:
Thomas J. Czartoski, Robert Perkins, Jorge L. Villanueva, Glenn Richards
Abstract: Devices, compositions, and methods are described which provide a tubular nanostructure targeted to a lipid bilayer membrane. The targeted tubular nanostructure can have a surface region configured to pass through a lipid bilayer membrane of a cell, a hydrophobic surface region flanked by two hydrophilic surface regions configured to form a pore in a lipid bilayer membrane of a cellular organelle, and at least one ligand configured to bind one or more cognates on the lipid bilayer membrane of the cellular organelle. The target cell can be, for example, a tumor cell, an infected cell, or a diseased cell in a subject. The tubular nanostructure can form a pore in the lipid bilayer membrane of the cellular organelle, e.g., mitochondria, which can permit transit or translocation of at least one compound across the membrane and cause cell death of the target cell.
Type:
Application
Filed:
January 30, 2009
Publication date:
September 16, 2010
Inventors:
Mahalaxmi Gita Bangera, Ed Harlow, Roderick A. Hyde, Muriel Y. Ishikawa, Edward K.Y. Jung, Eric C. Leuthardt, Nathan P. Myhrvold, Dennis J. Rivet, Elizabeth A. Sweeney, Clarence T. Tegreene, Lowell L. Wood, JR., Victoria Y.H. Wood
Abstract: The present invention relates to an improved process for the synthesis of Ibandronate sodium of formula (I). The present invention also provides novel processes for the synthesis of 3-[N-(methylpentyl)amino]propionic acid (III).
Abstract: Alpha, omega-difunctional aldaramides, in particular diaminoaldaramides, dihydroxyaldaramides, bis(alkoxycarbonylalkyl)aldaramides, and bis(carboxyalkyl)aldaramides, and processes for preparing the aldaramides are provided.
Type:
Grant
Filed:
January 31, 2008
Date of Patent:
September 7, 2010
Assignee:
E. I. du Pont de Nemours and Company
Inventors:
Mark Allen Andrews, Henry Keith Chenault, Garret D. Figuly
Abstract: The invention provides a new enantioselective process for the preparation of (S)-pregabalin, or a pharmaceutical acceptable addition acid salt comprising: acid hydrolysis of the dioxolan ring of a chiral compound of general formula (I) to obtain compound of general formula (II); oxidation of compound (II) to obtain a compound of general formula (III) and transforming compound (III) into compound of general formula (IV); subjecting compound (IV) to basic hydrolysis to obtain a compound of general formula (V) which is reduced to obtain enantiomerically pure S-pregabalin. The invention also provides new chiral intermediates involved in the process.
Type:
Application
Filed:
July 17, 2008
Publication date:
August 5, 2010
Applicant:
LABORATORIOS DEL DR. ESTEVE, S.A.
Inventors:
Rosa M. Ortuno, Sandra Izquierdo, Helmut Heinrich Buschmann, Antoni Torrens Jover, Monica Garcia Lopez
Abstract: One aspect of the present invention relates to a method for the kinetic resolution of racemic and diastereomeric mixtures of chiral compounds. The critical elements of the method are: a non-racemic chiral tertiary-amine-containing catalyst; a racemic or diastereomeric mixture of a chiral substrate, e.g., a cyclic carbonate or cyclic carbamate; and a nucleophile, e.g., an alcohol, amine or thiol. A preferred embodiment of the present invention relates to a method for achieving the kinetic resolution of racemic and diastereomeric mixtures of derivatives of ?- and ?-amino, hydroxy, and thio carboxylic acids. In certain embodiments, the methods of the present invention achieve dynamic kinetic resolution of a racemic or diastereomeric mixture of a substrate, i.e.
Abstract: The invention provides a method for labeling an analyte comprising a primary amino group, the method comprising: a. a labeling process comprising reacting the analyte with a dialdehyde in the presence of a label, wherein the label bears a charge, and b. an analysis process comprising subjecting the labeled analyte to MS, preferably LC-MS-MS. Herein, preferably, the labeling process comprises reacting an analyte with a dialdehyde, wherein the dialdehyde carries a label bearing a charge, to provide a labeled analyte carrying the charge. The present invention also provides a labeling method to provide a labeled analyte carrying a charge, wherein the labeling method comprises a labeling process comprising reacting an analyte with a dialdehyde, wherein the analyte comprises a primary amino group and wherein the dialdehyde carries a label bearing the charge. The dialdehyde is preferably an aromatic dialdehyde, most preferably an aromatic 1,2- or 1,3-dicarboxaldehyde.
Type:
Application
Filed:
March 19, 2008
Publication date:
July 22, 2010
Inventors:
Thomas Ivo Franciscus Huber Cremers, Lutske Aafke Anna de Jong, Wijnand Sjoerd Faber
Abstract: One aspect of the present invention relates to compounds for delivering chemotherapeutic agents to cancerous cells to reduce discomfort and deleterious side effects associated with systemic administration of such agents. Another aspect of the invention relates to methods of treating a subject with cancer by administering a therapeutically effective amount of a chemotherapeutic agent that predominately targets cancerous cells over healthy cells. Additionally, one aspect of the present invention relates to methods of inhibiting the life-cycle of a cancerous cell, as well preparing a chemotherapeutic prodrug.
Abstract: Disclosed is an absorbent for separation of carbon dioxide from mixed gases, comprising a mixture of i) a compound of the chemical formula 1 having one or more groups of three functional groups consisting of amino group attached to a tertiary carbon atom; carboxylate group; and hydroxyl group respectively, in a molecule, or a compound of the chemical formula 2 having one or more groups of two functional groups consisting of amino group attached to a quarternary carbon atom; and carboxylate group respectively in a molecule, and ii) an amine compound which promotes the reaction. The absorbent for separation of carbon dioxide of the present invention is advantageous economically, since its efficiency is excellent due to larger unit absorption amount of carbon dioxide, and the energy required for regeneration can be reduced due to the relatively wider difference of absorption amounts with temperature.
Type:
Grant
Filed:
December 27, 2006
Date of Patent:
July 20, 2010
Assignee:
Korea Electric Power Corporation
Inventors:
Jae Goo Shim, Jun Han Kim, Kyung Ryong Jang, Chung Kul Ryu, Hee Moon Eum, Hyun Soo Lim
Abstract: The invention relates to a method for the synthesis of amino acids/esters of general formula NH2—(CH2)n—COOR in which n is an integer between 5 and 14, and R is either H or an alkyl radical including from 1 to 4 carbon atoms, from natural long-chain mono-unsaturated fatty acids or esters including at least 10 adjacent carbon atoms per molecule, said method comprising: first converting, if necessary, said natural long-chain fatty acid or ester into a monounsaturated fatty acid/ester of general formula R1—(CH2)m—CH?CH—(CH2)p—COOR in which R1 is H, CH3 or a COOR radical, m is an integer between 0 and 14 and p is an integer between 2 and 11, then submitting the latter to a crossed catalytic metathesis reaction with a compound of formula R2—CH?CH—R3 in which R2 is either H or CN and R3 is CN or CH2NH2, provided that if R2 is CN, R3 can be only CN, and finally converting the resulting product of the general formula R3—CH?CH—(CH2)p—COOR into an amino-acid, either by hydrogenation, or by hydrogenation of the triple t
Abstract: Specific, highly potent 2-oxo-amide based inhibitors of phospholipase A2 (PLA2) activity are provided. A role for PLA2 activity in spinally mediated inflammatory processes is established, and a method for treating hyperalgesia and other inflammatory conditions associated with PLA2 activity is provided.
Type:
Grant
Filed:
March 7, 2003
Date of Patent:
June 29, 2010
Assignee:
The Regents of the University of California
Inventors:
Edward Dennis, Tony Yaksh, Karin Killermann Lucas, Camilla Svensson, David A. Six, George Kokotos, Violetta Constantinou-Kokotou
Abstract: A method is provided for quantifying endogenous sphingolipids in a biological system. The method includes preparing one or more isotope labeled amino acids; introducing the isotope labeled amino acids into a biological system; extracting and separating a sphingolipid-containing fraction from the biological system; and quantifying the amount of endogenous sphingolipids in the biological system. The isotope-labeled amino acid may include a non-essential amino acid, and the method may further include adding an amino acid synthesis inhibitor into the biological system. Systems and kits for quantifying endogenous sphingolipids also are disclosed.
Type:
Application
Filed:
December 23, 2009
Publication date:
June 24, 2010
Applicant:
FLORIDA STATE UNIVERSITY RESEARCH FOUNDATION
Inventors:
Mark R. Emmett, Huan He, Alan G. Marshall
Abstract: A polyurethane resin is synthesized from a compound represented by the following Formula (1), a polymerizable composition includes the polyurethane resin, a planographic printing plate precursor includes a photosensitive layer including the composition, and a method produces a diol compound that can be used as a raw material of the polyurethane resin. In Formula (1), R1 and R2 each independently represent a single bond or an alkylene group optionally having a substituent, R3 represents a hydrogen atom or an alkyl group, R4 represents a hydrogen atom or an alkyl group, and A represents a divalent or higher linking group, provided that R1 and R2 are not both a single bond.
Abstract: The present invention relates to a whole cell catalytic system for the preparation of an enantiomerically enriched ?-amino acid from a corresponding hydantoin wherein hydantoinase, L-carbamoylase and hydantoin racemase are coexpressed in a recombinant micro-organism wherein the genes coding for these three enzymes are located on a single replicon. The present invention further relates to the use of such a whole cell catalytic system according in the preparation of an enantiomerically enriched L-?-amino acid from a corresponding hydantoin.
Type:
Application
Filed:
December 4, 2007
Publication date:
June 10, 2010
Inventors:
Monika Rusnak-Müller, Oliver May, Petrus Johannes Hermsen, Henricus Martinus Maria Gerardus Straatman, Wolfgang Skranc, Wilhelmus Hubertus Joseph Boesten, Dannis Heemskerk, Ben De Lange, Georgios Sarakinos
Abstract: A novel method of an amidocarbonylation reaction among an aldehyde compound, an amide compound, and carbon monoxide, which comprises using a palladium-supporting crosslinked-polymer composition containing palladium clusters having a major-axis length of 20 nm or shorter to conduct the amidocarbonylation reaction. Thus, an N-acyl-?-amino acid can be more efficiently and selectively synthesized in a dean reaction system. Also provided is a catalyst for use in the method.
Abstract: The present disclosure relates to methods of rational genome mining. A method may include narrowing the number of clones that would otherwise need to be screened and/or identifying a gene with a desired catalytic activity. The disclosure also relates to a nitrile hydrolase from Bradyrhizobium japonicum USDA110 first identified by rational genome mining. In addition, the disclosure relates to nitrilase bll6402 and catalytically active variants capable of converting an ?-hydroxy nitriles, a ?-hydroxy nitrile and/or an ?,?-dinitrile to a carboxylic acid.
Type:
Application
Filed:
June 9, 2009
Publication date:
June 3, 2010
Inventors:
Dunming Zhu, Ling Hua, Edward R. Biehl, Chandrani Mukherjee
Abstract: The present invention is directed to a regio- and stereoselective bioconversion of selected aliphatic dinitriles into corresponding cyanocarboxylic acids. More particularly, the present invention provides methods for the conversion of 2-isobutyl-succinonitrile into (S)-3 cyano-5-methylhexanoic acid, which is a useful intermediate in the synthesis of (S)-3(aminomethyl)-5-methylhexanoic acid (pregabalin). Pregabalin can be used for treating certain cerebral diseases, for example, in the treatment and prevention of seizure disorders, pain, and psychotic disorders.
Type:
Grant
Filed:
April 1, 2005
Date of Patent:
June 1, 2010
Assignee:
Pfizer, Inc.
Inventors:
Michael P. Burns, Justin K. Weaver, John Wing Wong
Abstract: The present invention provides nucleic acids encoding B7-related factors that modulate the activation of immune or inflammatory response cells, such as T-cells. Also provided are expression vectors and fusion constructs comprising nucleic acids encoding B7-related polypeptides, including BSL1, BSL2, and BSL3. The present invention further provides isolated B7-related polypeptides, isolated fusion proteins comprising B7-related polypeptides, and antibodies that are specifically reactive with B7-related polypeptides, or portions thereof. In addition, the present invention provides assays utilizing B7-related nucleic acids, polypeptides, or peptides. The present invention further provides compositions of B7-related nucleic acids, polypeptides, fusion proteins, or antibodies that are useful for the immunomodulation of a human or animal subject.
Type:
Application
Filed:
February 7, 2008
Publication date:
May 20, 2010
Inventors:
Glen E. Mikesell, Henry Shen, Han Chang, Joshua N. Finger, Guchen Yang, Robert James Peach
Abstract: A metal chelating composition having the formula: wherein Q is a carrier; S1 is a spacer; L is -A-T-CH(X)— or —C(?O)—; A is an ether, thioether, selenoether, or amide linkage; T is a bond or substituted or unsubstituted alkyl or alkenyl; X is —(CH2)kCH3, —(CH2)kCOOH, —(CH2)kSO3H, —(CH2)kPO3H2, —(CH2)kN(J)2, or —(CH2)kP(J)2, preferably —(CH2)kCOOH or —(CH2)kSO3H; k is an integer from 0 to 2; J is hydrocarbyl or substituted hydrocarbyl; Y is —COOH, —H, —SO3H, —PO3H2, —N(J)2, or —P(J)2, preferably, —COOH; Z is —COOH, —H, —SO3H, —PO3H2, —N(J)2, or —P(J)2, preferably, —COOH; and i is an integer from 0 to 4, preferably 1 or 2.
Type:
Grant
Filed:
March 1, 2006
Date of Patent:
May 4, 2010
Assignee:
Sigma-Aldrich Co.
Inventors:
William K. Kappel, Vankatappa Viswanatha, Handong Li, Richard J. Mehigh, John G. Dapron
Abstract: An antidepressant containing, as an active ingredient, at least one compound selected from a branched amino acid, a pharmaceutically acceptable salt thereof and a derivative thereof.
Abstract: This invention relates to polypeptides having aldolase activity, including pyruvate activity such as, without limitation, HMG and/or KHG aldolase activity, polynucleotides encoding these polypeptides, and methods of making and using these polynucleotides and polypeptides. In some embodiments, the invention is directed to polypeptides having aldolase activity, including pyruvate activity such as, without limitation, HMG and/or KHG aldolase activity, including thermostable and thermotolerant activity, and polynucleotides encoding these enzymes, and making and using these polynucleotides and polypeptides. The polypeptides in accordance with the invention can be used in a variety of pharmaceutical, agricultural and industrial contexts.
Type:
Application
Filed:
March 7, 2007
Publication date:
April 15, 2010
Inventors:
David P. Weiner, Lishan Zhao, Peter Luginbuhl, Ellen Burke, Toby H. Richardson, Paula M. Hicks
Abstract: The invention encompasses processes for the synthesis of (S)-(+)-3-(aminomethyl)-5-methylhexanoic acid, (S)-Pregabalin, and intermediates of (S)-Pregabalin.
Type:
Application
Filed:
October 19, 2009
Publication date:
April 1, 2010
Inventors:
Vinod Kumar Kansal, Brijnath P. Chaurasia, V. Govardhan Rao, Anand Prakash Tiwari
Abstract: The invention relates to pure (R)-CMH and to the optical resolution of CMH-racemate, a key intermediate in the synthesis of (S)-Pregabalin. The invention also relates to the process for optically purifying (R)-CMH and to the process for isolating (S)-CMH from the mother liquor.
Type:
Grant
Filed:
August 14, 2007
Date of Patent:
March 16, 2010
Assignee:
Teva Pharmaceutical Industries Ltd.
Inventors:
Lilach Hedvati, Ziv Dee-Noor, Claude Singer, Gideon Pilarski
Abstract: The present invention is directed toward compositions comprising carbon nanotubes (CNTs) that are sidewall-functionalized with amino acid groups, and to amino acid compositions comprising carbon nanotubes. The present invention is also directed to simple and relatively inexpensive methods for the preparation of such compositions. Such compositions are expected to greatly extend the bio-medical applications of CNTs.
Type:
Application
Filed:
January 18, 2005
Publication date:
February 25, 2010
Inventors:
Valery N. Khabashesku, Haiqing Peng, John L. Margrave, Mary Lou Margrave
Abstract: The present invention discloses an optically active quarternary ammonium salt having axial asymmetry and a method for producing an ?-amino acid and a derivative thereof using the same. The optically active quarternary ammonium salt having axial asymmetry of the present invention is a chiral phase-transfer catalyst that has a simple structure and that can be produced in a smaller number of process steps. The compound of the present invention is very useful as a phase-transfer catalyst in the synthesis of an ?-alkyl-?-amino acid and a derivative thereof as well as an ?,?-dialkyl-?-amino acid and a derivative thereof. Therefore, the compound of the present invention can be used in the development of novel foods and pharmaceuticals.
Abstract: This invention relates to certain biphenyl amino acid compounds, compositions, and methods for treating or preventing obesity and related diseases.
Type:
Application
Filed:
July 31, 2006
Publication date:
January 21, 2010
Applicant:
Bayer Healthcare LLC
Inventors:
Roger A. Smith, Derek Lowe, Tatiana Shelekhin, Georgiy Bondar, Philip Coish, Stephen J. O'Connor
Abstract: Disclosed herein are biomarkers for determining gamma radiation exposure by an animal or human. The biomarkers include 3-hydroxy-2-methylbenzoic acid 3-O-sulfate, N-hexanoylglycine, ?-thymidine, taurine, xanthine, xanthosine, 2?-deoxyuridine, 2?-deoxycytidine, 2?-deoxyxanthosine, or any salt, ion, or combination thereof. Also disclosed are methods for determining gamma radiation exposure by an animal or human, which include the step of measuring the amount of one or more biomarkers specific to gamma radiation in the biological fluid and correlating the amount of said biomarkers to the amount of gamma radiation exposure by the animal or human. Systems for determining gamma radiation exposure by an animal or human and methods of treating an animal or human for gamma radiation exposure are also disclosed.
Type:
Application
Filed:
May 15, 2008
Publication date:
December 24, 2009
Inventors:
Jeffrey R. Idle, Frank J. Gonzalez, John B. Tyburski, Kristopher W. Krausz, Andrew David Patterson
Abstract: Raney copper which is doped with at least one metal from the group comprising iron and/or noble metals is used as a catalyst in the dehydrogenation of alcohols.
Type:
Grant
Filed:
June 1, 2007
Date of Patent:
December 15, 2009
Assignee:
Degussa AG
Inventors:
Daniel Ostgard, Jörg Sauer, Andreas Freund, Monika Berweiler, Matthias Höpp, Rudolf Vanheertum, Walther Girke
Abstract: Conjugates of a gamma-aminobutyric acid (GABA) compound or a glycine compound and an analgesic drug are disclosed. Further disclosed are pharmaceutical compositions containing these conjugates and uses thereof in the treatment of CNS-associated diseases or disorders, optionally in combination with a psychotropic drug.
Type:
Application
Filed:
July 17, 2007
Publication date:
December 10, 2009
Applicants:
Ramot At Tel Aviv University Ltd., Bar-IIan University, BioLine RX Ltd.
Inventors:
Abraham Nudelman, Ada Rephaeli, Irit Gil-Ad, Abraham Weizman, Ran Lifshitz, IIan Winkler
Abstract: Disclosed are materials and methods for preparing optically active ?-amino acids of Formula 1, which bind to the alpha-2-delta (?2?) subunit of a calcium channel.
Type:
Application
Filed:
July 31, 2009
Publication date:
December 3, 2009
Inventors:
Margaret Claire Evans, Lloyd Charles Franklin, Lorraine Michelle Murtagh, Thomas Norman Nanninga, Bruce Allen Pearlman, James Edward Saenz, Niamh Josephine Willis
Abstract: The present invention relates to a novel process for the preparation of ?-amino acids, such as (±)-3-(aminomethyl)-5-methyl-hexanoic acid 1, which is a key intermediate in the preparation of the potent anticonvulsant pregabalin, (S)-(+)-3-(aminomethyl)-5-methyl-hexanoic acid 2.
Type:
Application
Filed:
July 12, 2007
Publication date:
November 19, 2009
Applicants:
Generics [UK] Limited, Merck Development Centre Private Limited
Inventors:
Abhay Gaitonde, Chitra Valdya, P. Khairnar
Abstract: The present invention provides a chiral phase-transfer catalyst of the following formula (I): The compound (I) can be produced by reacting a 2,2?-dimethylene bromide-1,1?-biphenyl derivative, which can be produced through comparatively small number of steps, with an easily available secondary amine.
Abstract: The invention provides novel compounds and methods to carry out organocatalytic Michael additions of aldehydes to nitroethylene catalyzed by a proline derivative to provide ?-substituted-?-nitroaldehydes. The reaction can be rendered enantioselective when a chiral pyrrolidine catalyst is used, allowing for Michael adducts in nearly optically pure form (e.g., 96-99% e.e.). The Michael adducts can bear a single substituent or dual substituents adjacent to the carbonyl. The Michael adducts can be efficiently converted to protected ?2-amino acids, which are essential for systematic conformational studies of ?-peptide foldamers.
Type:
Application
Filed:
March 23, 2009
Publication date:
October 22, 2009
Applicant:
WARF - Wisconsin Alumni Research Foundation
Inventors:
Samuel Helmer Gellman, Yonggui Chi, Li Guo
Abstract: The present invention is directed to a method for ?N-methylation of amino acids suitable for on-resin methylation, compatible with Fmoc/tBu SPPS, and compatible with amino acids bearing protected or unprotected nucleophilic side-chains, notably Arg(Pbf), Met, Cys, and Trp. The present invention is further directed to a compound of Formula I wherein m, n, X and Y are defined as described herein.
Abstract: The invention is directed to methods of making organic compounds by metathesis and hydrocyanation. The method of the invention may be used, for example, to make industrial important organic compounds such as diacids, diesters, acid-amines, acid-alcohols, acid-nitriles, ester-amines, ester-alcohols, and ester-nitriles.
Type:
Application
Filed:
April 10, 2009
Publication date:
October 15, 2009
Inventors:
Timothy W. Abraham, Hiroki Kaido, Choon Woo Lee, Richard L. Pederson, Yann Schrodi, Michael John Tupy, Alexandre A. Pletnev
Abstract: Disclosed are materials and methods for preparing optically active ?-amino acids of Formula 1, which bind to the alpha-2-delta (?2?) subunit of a calcium channel.
Type:
Application
Filed:
June 27, 2005
Publication date:
October 1, 2009
Inventors:
Brian G Conway, Thomas Norman Nanninga, Hiafeng Wu, Garrett S. Hoge, Bruce Allen Pearlman, Derick Dale Winkle
Abstract: Chiral selectors having ?-unsubstituted ?-amino acid derivatives of the structure: a stationary phase for separating substance mixtures containing the chiral selector, and processes for separating mixtures of chiral substances, including enantiomers, and especially enantiomers of substances selected from ?-amino acids and derivatives thereof, ?-amino acids and ?-hydroxy acids are provided.
Type:
Application
Filed:
March 10, 2009
Publication date:
September 17, 2009
Applicant:
EVONIK DEGUSSA GmbH
Inventors:
Franz-Rudolf Kunz, Peter Richter, Stefan Merget, Roland Singer, Thomas Mueller
Abstract: The present invention relates to a method for the production of at least one nonvolatile microbial metabolite in solid form by sugar-based microbial fermentation, in which process a microorganism strain which produces the desired metabolites is grown using a sugar-containing liquid medium with a monosaccharide content of more than 20% by weight based on the total weight of the liquid medium, and the volatile constituents of the fermentation liquor are subsequently largely removed, the sugar-containing liquid medium being prepared by: a1) milling selected starch feedstock from cereal grains; and a2) liquefying the millbase in an aqueous liquid in the presence of at least one starch-liquefying enzyme, followed by saccharification using at least one saccharifying enzyme, where, for liquefaction purposes, at least a portion of the millbase is liquefied by continuous or batchwise addition to the aqueous liquid.
Type:
Application
Filed:
September 6, 2006
Publication date:
September 10, 2009
Applicant:
BASF SE
Inventors:
Stephan Freyer, Markus Pompejus, Oskar Zelder, Markus Lohscheidt, Matthias Boy, Edzard Scholten
Abstract: The present invention relates to a novel process for preparing alkoxyamines from a nitroxide and a dithiocarbamate by photolysis reaction. This process, which does not generate effluent containing metals, may be carried out in batch or in continuous mode and takes place at a lower temperature than the known processes for synthesizing alkoxyamines.
Abstract: This invention provides compounds having excellent antitumor activity, which are represented by the following formulae in which R1, R2, R3, m, n and R4 have the significations as given in the specification.