Of Carboxylic Acid Ester Patents (Class 564/134)
  • Patent number: 9162973
    Abstract: A method for preparing a compound of Formula 1 comprising contacting a compound of Formulae 2 and 3 in the presence of a palladium source, a ligand, a base and carbon monoxide wherein R1, R2, X and R3 are as defined in the disclosure. A method for preparing a compound of Formula 5 wherein R1, R2, R3, R4, R5, R6 and Z are as defined in the disclosure, using a compound of Formula 1 characterized by preparing a compound of Formula 1 by the method disclosed above or using a compound of Formula 1 prepared by the method above.
    Type: Grant
    Filed: September 16, 2014
    Date of Patent: October 20, 2015
    Assignee: E I DU PONT DE NEMOURS AND COMPANY
    Inventors: Sigridur Soley Kristjansdottir, Rafael Shapiro, Matthew Richard Oberholzer
  • Patent number: 9006488
    Abstract: A solvent-free mechanical process of reacting amine compounds with acetylating agents resulting in amides such as acetaminophen is described.
    Type: Grant
    Filed: March 20, 2014
    Date of Patent: April 14, 2015
    Inventors: Muhammad Amin, Muhammad S. Iqbal
  • Patent number: 9006486
    Abstract: The present disclosure generally relates to a new process for the preparation of high purity 5-nitro-isophthalamide compounds, which are useful as intermediates for the preparation of imaging agents, such as iodinated x-ray contrast imaging agents like ioversol, iohexyl and iopamidol.
    Type: Grant
    Filed: January 7, 2014
    Date of Patent: April 14, 2015
    Assignee: Liebel-Flarsheim Company LLC
    Inventor: James R. Meyer
  • Patent number: 8962885
    Abstract: The invention relates to new ?-hydroxyalkylamides, to a method for production of same and to the use of same.
    Type: Grant
    Filed: March 10, 2011
    Date of Patent: February 24, 2015
    Assignee: Evonik Degussa GmbH
    Inventors: Werner Grenda, Emmanouil Spyrou, Thomas Weihrauch, Christoph Lammers, Holger Loesch, Klaus Behrendt
  • Publication number: 20150051410
    Abstract: Novel processes for the preparation of a compound of Formula I-2 substantially free of the 5,6-trans isomer: wherein R2, R3 and R4 are as defined in the specification are provided. Novel intermediates for the preparations of isomer free Prostaglandins and derivatives thereof are also provided.
    Type: Application
    Filed: August 15, 2013
    Publication date: February 19, 2015
    Applicant: CHIROGATE INTERNATIONAL INC.
    Inventors: Shih-Yi Wei, Yu-Chih Yeh, Min-Kuan Hsu, Li-Ta Kao
  • Patent number: 8946478
    Abstract: Provided are a benzamide derivative as shown in formula (I) or a pharmaceutically acceptable salt thereof, and the preparation method and use thereof for preparing a medicine for treating cancer, wherein the group definitions of formula (I) are as set out in the description.
    Type: Grant
    Filed: November 3, 2011
    Date of Patent: February 3, 2015
    Assignee: Zhejiang Hisun Pharmaceutical Co., Ltd.
    Inventors: Hua Bai, Xuyang Zhao, Yongxiang Gong, Jinqing Zhong, Qifeng Zhu, Xiaoyu Liu, Lifei Liu, Qixian Zhou
  • Patent number: 8946476
    Abstract: The present patent application relates to an alternative process for the preparation of amino derivatives. In particular, the present application relates to an improved process for the manufacture of Lacosamide (LCM), (R)-2-acetamido-N-benzyl-3-methoxypropion-amide, which is useful as an anticonvulsive drug. In a particular aspect, the present invention relates to a process of manufacture of optically enriched (R)-2-acetamido-N-benzyl-3-methoxypropion-amide (I) comprising resolution of 2-acetamido-N-benzyl-3-methoxypropion-amide (II).
    Type: Grant
    Filed: November 6, 2009
    Date of Patent: February 3, 2015
    Assignee: UCB Pharma GmbH
    Inventors: Didier Bouvy, Alain Merschaert, Véronique Pinilla, Joerg Hamann, Ralf Kanzler, Antoine Thomas
  • Publication number: 20150005503
    Abstract: A method for preparing a compound of Formula 1 comprising contacting a compound of Formulae 2 and 3 in the presence of a palladium source, a ligand, a base and carbon monoxide wherein R1, R2, X and R3 are as defined in the disclosure. A method for preparing a compound of Formula 5 wherein R1, R2, R3, R4, R5, R6 and Z are as defined in the disclosure, using a compound of Formula 1 characterized by preparing a compound of Formula 1 by the method disclosed above or using a compound of Formula 1 prepared by the method above.
    Type: Application
    Filed: September 16, 2014
    Publication date: January 1, 2015
    Inventors: SIGRIDUR SOLEY KRISTJANSDOTTIR, RAFAEL SHAPIRO, MATTHEW RICHARD OBERHOLZER
  • Publication number: 20140371445
    Abstract: The present invention relates to a quinic acid derivative, preparation process of the same and pharmaceutical uses thereof. The quinic acid derivative has a quinic acid-like structure which binds to CD28, blocks T-cell signal 2 pathway via CD28, and suppresses T-cell activation. The C-1 carboxyl group, the C-3 hydroxyl group and the C-4 hydroxyl group of quinic acid are modified to attenuate the cytotoxicity of the quinic acid derivative. The preparation process of the quinic acid derivative comprises 2 steps of: treating quinic acid with the first reagent in the presence of the acid catalyst to form an immediate; and treating the immediate with the second reagent to from the quinic acid derivative. With the ability to suppress T-cell activation, the quinic acid derivative is used to treats an autoimmune disease, an allergy, transplant rejection or other related immune disorder.
    Type: Application
    Filed: June 13, 2013
    Publication date: December 18, 2014
    Inventors: HUEIH-MIN CHEN, CHUNG-MING SUN, CHIH-YU HUANG
  • Patent number: 8907130
    Abstract: The invention relates to novel ?-hydroxyalkylamides, to a method for their production and to the use thereof.
    Type: Grant
    Filed: March 10, 2011
    Date of Patent: December 9, 2014
    Assignee: Evonik Degussa GmbH
    Inventors: Werner Grenda, Emmanouil Spyrou, Thomas Weihrauch, Christoph Lammers, Holger Loesch, Klaus Behrendt
  • Patent number: 8901328
    Abstract: Disclosed is a method involving reacting a deprotonated mono- or dialkanol amine with one or more C4 to about C75 fatty acid monoalcohol esters.
    Type: Grant
    Filed: April 11, 2012
    Date of Patent: December 2, 2014
    Assignee: Chervon Oronite Company LLC
    Inventors: Yat Fan Suen, Sarah Liz Jensen
  • Patent number: 8822724
    Abstract: A carboxamide can be produced in a high yield by a method for producing a carboxamide, for example, represented by formula (4): (wherein R1 and R3 are as defined below), the method comprising a step of allowing a carboxylic acid ester represented by formula (1): (wherein R1 represents an optionally substituented C1-C20 hydrocarbon group or an optionally substituented C3-C20 heterocyclic group, and R2 represents an optionally substituented C1-C20 hydrocarbon group), an amine represented by formula (2): R3—NH2??(2) (wherein R3 represents a hydrogen atom or an optionally substituented C1-C20 hydrocarbon group), and a formamide compound represented by formula (3): (wherein R3 is as defined above) to react in the presence of a metal alkoxide.
    Type: Grant
    Filed: July 13, 2011
    Date of Patent: September 2, 2014
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Junichi Tomokawa, Takahiro Kimura, Norihiko Hirata
  • Patent number: 8809395
    Abstract: The present invention is directed to compounds, intermediates and methods for making valerenic acid and its derivatives as well as the use of such compounds as GABAA receptor ligands.
    Type: Grant
    Filed: January 22, 2010
    Date of Patent: August 19, 2014
    Assignee: Valericon GmbH
    Inventors: Johann Mulzer, Jürgen Ramharter, Steffen Hering, Sophia Khom
  • Publication number: 20140213821
    Abstract: It is described a process for the opening of lactone or lactam rings useful in the synthesis of pharmaceutically active compounds and the intermediates thereof, particularly Aliskiren. It has found that by selecting a type of solvent it is possible to obtain excellent yields and high optical and chemical purity of the isolated products.
    Type: Application
    Filed: July 25, 2012
    Publication date: July 31, 2014
    Applicant: CHEMO IBERICA, S. A.
    Inventors: Luca Carcone, Domenico Magrone, Giuseppe Barreca, Marcello Rasparini, Huang Liming
  • Publication number: 20140200367
    Abstract: The present disclosure generally relates to a new process for the preparation of high purity 5-nitro-isophthalamide compounds, which are useful as intermediates for the preparation of imaging agents, such as iodinated x-ray contrast imaging agents like ioversol, iohexyl and iopamidol.
    Type: Application
    Filed: January 7, 2014
    Publication date: July 17, 2014
    Applicant: Mallinckrodt LLC
    Inventor: James R. Meyer
  • Patent number: 8680333
    Abstract: The invention relates to a process for the preparation of formamides by reacting aromatic amines with a formic acid ester in the presence of a catalyst, wherein the catalyst is a phosphorus-containing acid or a Lewis-acidic metal salt.
    Type: Grant
    Filed: December 1, 2010
    Date of Patent: March 25, 2014
    Assignee: BASF SE
    Inventors: Axel Franzke, Torsten Mattke, Julia Leschinski, Radwan Abdallah, Michael Bock, Robert Baumann, Eckhard Stroefer
  • Patent number: 8674133
    Abstract: The invention relates to a process for continuously preparing N-alkyl(meth)acrylamides by reacting alkyl(meth)acrylates with high-boiling amines. A catalyst activation and specific workup technique achieve product qualities which have not been achieved to date. In addition, very high space-time yields and overall yields can be achieved.
    Type: Grant
    Filed: March 3, 2010
    Date of Patent: March 18, 2014
    Assignee: Evonik Röhm GmbH
    Inventors: Bardo Schmitt, Wolfgang Klesse, Martina Ebert, Dirk Broell, Guido Protzmann, Joachim Knebel, Thomas Kehr, Hans-Gerhard Stadler, Gerhard Koelbl, Benedikt Laux
  • Patent number: 8637707
    Abstract: The present invention relates to a process for preparing substituted 2-aminobiphenyls and to a process for preparing (Het)arylamides of such 2-aminobiphenyls.
    Type: Grant
    Filed: July 3, 2009
    Date of Patent: January 28, 2014
    Assignees: BASF SE, Technische Universitaet Muenchen
    Inventors: Michael Keil, Michael Rack, Thomas Zierke, Markus Heinrich, Alexander Wetzel
  • Publication number: 20130345470
    Abstract: A process for producing high purity 3-hydroxypropionic acid from a fermentation cell broth is described. The 3-hydroxypropionic acid can be converted to a variety of products, such as acrylamide, 3-hydroxypropionic esters, acrylic esters, and 3-HP amide. This process features a high degree of product flexibility, limited or no solvent recycle, discrete waste streams, an efficient water removal process, and efficient recovery of products and solvents with proven and scalable equipment.
    Type: Application
    Filed: June 20, 2012
    Publication date: December 26, 2013
    Applicant: OPX Biotechnologies, Inc.
    Inventors: Robert Tengler, David DeCoster
  • Publication number: 20130338231
    Abstract: The invention provides compound of the general formula: in which each X independently represents a polymer chain; n represents an integer greater than 1; Q represents a linker; Y represents an amide group; and Z represents either —CH.(CH2L)2 or —C(CH2L)(?CH2), in which each L independently represents a leaving group. The compounds are useful reagents for the conjugation of polymers to proteins, the resulting conjugates being novel and also forming part of the invention.
    Type: Application
    Filed: June 17, 2013
    Publication date: December 19, 2013
    Inventors: Antony GODWIN, Stephen Brocchini
  • Publication number: 20130324688
    Abstract: The preparation of cyclohexadienes from one or more plant oils is disclosed. The cyclohexadiene can be used to form polymers or derivatized to form other monomers that can be used to form polymeric materials.
    Type: Application
    Filed: April 9, 2013
    Publication date: December 5, 2013
    Inventor: Robert T. MATHERS
  • Patent number: 8586792
    Abstract: A process for the preparation of 4-iodo-3-nitrobenzamide free from the impurities formed due to nucleophilic substitution of the labile iodo group is disclosed.
    Type: Grant
    Filed: March 9, 2012
    Date of Patent: November 19, 2013
    Assignee: Divi's Laboratories Ltd.
    Inventors: Murali Krishna Prasad Divi, Mysore Aswatha Narayana Rao, Venkataramana Rajuri
  • Publication number: 20130225810
    Abstract: Provided are a benzamide derivative as shown in formula (I) or a pharmaceutically acceptable salt thereof, and the preparation method and use thereof for preparing a medicine for treating cancer, wherein the group definitions of formula (I) are as set out in the description.
    Type: Application
    Filed: November 3, 2011
    Publication date: August 29, 2013
    Applicant: Zhejiang Hisun Pharmaceutical Co., Ltd.
    Inventors: Hua Bai, Xuyang Zhao, Yongxiang Gong, Jinqing Zhong, Qifeng Zhu, Xiaoyu Liu, Lifei Liu, Qixian Zhou
  • Publication number: 20130172618
    Abstract: A process for the preparation of 4-iodo-3-nitrobenzamide free from the impurities formed due to nucleophilic substitution of the labile iodo group is disclosed.
    Type: Application
    Filed: March 9, 2012
    Publication date: July 4, 2013
    Applicant: DIVI'S LABORATORIES LIMITED
    Inventors: Murali Krishna Prasad Divi, Mysore Aswatha Narayana Rao, Venkataramana Rajuri
  • Publication number: 20130165507
    Abstract: The invention relates to novel guanidine derivatives in the cinnamic series of general formula (I): The invention also relates to the process for preparing said guanidine derivatives and also to synthetic intermediates. Finally, the invention relates to the use of the guanidine derivatives for the preparation of compositions with anti-glycation properties, especially in cosmetology.
    Type: Application
    Filed: September 6, 2011
    Publication date: June 27, 2013
    Applicant: PRODUITS CHIMIQUES AUXILIAIRES ET DE SYNTHESE
    Inventors: Sylvain Rault, Jean Charles Lancelot, Peggy Suzanne, Anne-Sophie Voisin-Chiret, Regis Pecquet, Jean-Christophe Joseph
  • Patent number: 8440860
    Abstract: A process for manufacturing dialkyl lactamide including reacting lactide and dialkylamine selected from one or more of dimethylamine, diethylamine, and methylethylamine to form a reaction mixture which includes dialkyl lactamide selected from N,N-dimethyl lactamide, N,N-diethyl lactamide, and N,N-methylethyl lactamide, N,N-dialkyl lactoyl lactamide, and dialkylamine, subjecting the reaction mixture to a separation step to form a product stream including N,N-dialkyl lactamide, a first recycle stream including dialkylamine and a second recycle stream including N,N-dialkyl lactoyl lactamide, feeding the recycle streams to the reaction step, and isolating the product stream. The process allows the manufacture of N,N-dimethyl lactamide, N,N-diethyl lactamide, and N,N-methylethyl lactamide on a commercial scale.
    Type: Grant
    Filed: September 30, 2009
    Date of Patent: May 14, 2013
    Assignee: Purac Biochem BV
    Inventor: Jan Van Krieken
  • Publication number: 20130092047
    Abstract: To provide a water/oil repellent agent and a water/oil repellent composition which are capable of imparting sufficient water/oil repellency to the surface of an article and which have low environmental impact. One comprising a reaction product obtained by reacting a fluorinated alcohol or amine having a polyfluoroalkyl moiety having at most 6 carbon atoms with a polyisocyanate compound, which is, when applied to an article, capable of imparting sufficient water/oil repellency, while presenting little environmental impact. When applied to an article, the water/oil repellent composition of the present invention is capable of imparting a high quality water/oil repellency to the article.
    Type: Application
    Filed: December 4, 2012
    Publication date: April 18, 2013
    Applicant: Asahi Glass Company, Limited
    Inventor: Asahi Glass Company, Limited
  • Patent number: 8378061
    Abstract: Provided are films made from copolyesters having improved oil repellency as compared to conventional copolyesters. The copolyesters are derived from certain perfluorinated monomers.
    Type: Grant
    Filed: September 1, 2010
    Date of Patent: February 19, 2013
    Assignee: E.I. du Pont de Nemours and Company
    Inventors: Neville Everton Drysdale, Surbhi Mahajan, Kenneth Gene Moloy, Fredrik Nederberg, Joel M. Pollino, Joachim C. Ritter
  • Patent number: 8350099
    Abstract: Disclosed are fluorovinyl ether functionalized aromatic diesters and derivatives thereof. The compounds disclosed have utility as functionalized monomers and comonomers in polyesters, polyamides, and the like. It has been found that incorporation of the monomers into polymers provides improved soil resistance to shaped articles produced from the polymers.
    Type: Grant
    Filed: September 1, 2010
    Date of Patent: January 8, 2013
    Assignee: E I du Pont de Nemours and Company
    Inventors: Neville Everton Drysdale, Surbhi Mahajan, Kenneth Gene Moloy, Fredrik Nederberg, Joel M. Pollino, Joachim C. Ritter
  • Patent number: 8338644
    Abstract: A process for preparing N,N-dimethylacetamide (DMAC) by continuously reacting methyl acetate (MeOAc) with dimethylamine (DMA) in the presence of a basic catalyst, wherein MeOAc is used in the form of a methanolic solution which is obtained as a by-product in the preparation of polyTHF by transesterifying polyTHF diacetate with methanol.
    Type: Grant
    Filed: December 14, 2010
    Date of Patent: December 25, 2012
    Assignee: BASF SE
    Inventors: Horst Grafmans, Steffen Maas, Alexander Weck, Heinz Ruetter, Michael Schulz, Karl-Heinz Ross
  • Publication number: 20120258470
    Abstract: A mutant hydrolase optionally fused to a protein of interest is provided. The mutant hydrolase is capable of forming a bond with a substrate for the corresponding nonmutant (wild-type) hydrolase which is more stable than the bond formed between the wild-type hydrolase and the substrate. Substrates for hydrolases comprising one or more functional groups are also provided, as well as methods of using the mutant hydrolase and the substrates of the invention. Also provided is a fusion protein capable of forming a stable bond with a substrate and cells which express the fusion protein.
    Type: Application
    Filed: April 18, 2012
    Publication date: October 11, 2012
    Applicant: PROMEGA CORPORATION
    Inventors: Keith V. Wood, Dieter Klaubert, Georgyi V. Los, Robert F. Bulleit, Mark McDougall, Chad Zimprich
  • Publication number: 20120178783
    Abstract: This invention provides the compound having the structure wherein n is 1-10; X is C—R11 or N; wherein R11 is H, OH, SH, F, Cl, SO2R7, NO2, trifluoromethyl, methoxy, or CO—R7, wherein R7 is alkyl, alkenyl, alkynyl, C3-C8 cycloalkyl, or aryl; Z is R2 is H or NR3R4, wherein R3 and R4 are each independently H, C1-C6 alkyl, or C3-C8 cycloalkyl; R5 is OH or SH; and R6, R12, R13, and R14 are each independently H, OH, SH, F, Cl, SO2R15, NO2, trifluoromethyl, methoxy, or CO—R15, wherein R15 is alkyl, alkenyl, alkynyl, C3-C8 cycloalkyl, or aryl, or a salt of the compound, which is useful in the treatment of tumors.
    Type: Application
    Filed: March 21, 2012
    Publication date: July 12, 2012
    Inventors: John S. Kovach, Francis Johnson
  • Publication number: 20120165293
    Abstract: The presently disclosed subject matter provides a method of synthesizing prostaglandins and prostaglandin analogs comprising the ring closing metathesis of compounds of Formula (I). Also provided are novel compounds of Formula (I) and Formula (II). In addition to their use as synthetic intermediates in the presently disclosed methods, compounds of Formula (II) can be used as prostaglandin and/or prostaglandin analog prodrugs.
    Type: Application
    Filed: July 13, 2010
    Publication date: June 28, 2012
    Inventors: George Petros Yiannikouros, Panos Kalaritis, Chaminda Priyapushpa Gamage, Stephenie Bosse Abernathy
  • Publication number: 20120157706
    Abstract: The invention provides methods and compositions for preparing lisdexamfetamine and salts thereof. More particularly, the invention provides, for example, methods of preparing lisdexamfetamine from D-amphetamine.
    Type: Application
    Filed: December 20, 2010
    Publication date: June 21, 2012
    Inventors: Michael J. Bauer, Gary Richard Callen, Judi Christine Humphrey, Todd Jeffrey Johnson, Matthew Wendell Schiesher
  • Patent number: 8193390
    Abstract: A process for preparing N,N-dimethylacetamide (DMAC) by continuously reacting methyl acetate (MeOAc) with dimethylamine (DMA) in the presence of a basic catalyst, wherein MeOAc is used in the form of a methanolic solution and the continuous distillative workup is effected in such a way that methanol and any other low boilers are initially removed overhead in a column A and the bottom effluent of column A is fed to a column B in which DMAC is removed via a side draw a purity of ?99.7% by weight.
    Type: Grant
    Filed: December 3, 2005
    Date of Patent: June 5, 2012
    Assignee: BASF SE
    Inventors: Horst Grafmans, Steffen Maas, Alexander Weck, Heinz Rütter, Michael Schulz, Karl-Heinz Roβ
  • Publication number: 20120095238
    Abstract: The invention relates to a continuous method for producing amides of aromatic carboxylic acids by reacting at least one carbonic acid ester of formula (I) R3—OOOR4, wherein R3 represents an optionally substituted aromatic hydrocarbon group with 5 to 100 carbon atoms and R4 represents a hydrocarbon group with 1 to 30 carbon atoms, with at least one amine of formula (II) HNR1R2, wherein R1 and R2 independently represent hydrogen or a hydrocarbon group with 1 to 100 C atoms, in a reaction tube the longitudinal axis of which extends in the direction of propagation of the microwaves of a monomode microwave applicator, under microwave irradiation to form carboxamide.
    Type: Application
    Filed: June 9, 2010
    Publication date: April 19, 2012
    Applicant: CLARIANT FINANCE (BVI) LIMITED
    Inventors: Matthias Krull, Roman Morschhaeuser
  • Publication number: 20120077959
    Abstract: Cobalt(II) complexes of the D2-symmetric chiral porphyrins are effective catalysts for asymmetric cyclopropanation reactions with succinimidyl diazoacetate. The Co-catalyzed reaction is suitable for various olefins, providing the corresponding cyclopropane succinimidyl esters in high yields and excellent diastereo- and enantio-selectivity.
    Type: Application
    Filed: February 16, 2010
    Publication date: March 29, 2012
    Inventors: X. Peter Zhang, Joshua V. Ruppel
  • Publication number: 20110313195
    Abstract: The invention relates to a process for continuously preparing N-alkyl(meth)acrylamides by reacting alkyl (meth)acrylates with high-boiling amines. A catalyst activation and specific workup technique achieve product qualities which have not been achieved to date. In addition, very high space-time yields and overall yields can be achieved.
    Type: Application
    Filed: March 3, 2010
    Publication date: December 22, 2011
    Inventors: Bardo Schmitt, Wolfgang Klesse, Martina Ebert, Dirk Broell, Guido Protzmann, Joachim Knebel, Thomas Kehr, Hans-Gerhard Stadler, Gerhard Koelbl, Benedikt Laux
  • Publication number: 20110295036
    Abstract: The present invention relates to a method for synthesizing a pharmaceutically acceptable acid addition salt of (1S, 2R)-milnacipran comprising the following successive steps: (a) reaction of phenylacetonitrile and of (R)-epichlorhydrin in the presence of a base containing an alkaline metal, followed by a basic treatment, and then by an acid treatment in order to obtain a lactone; (b) reaction of said lactone with MNEt2, wherein M represents an alkaline metal, or with NHEt2 in the presence of a Lewis acid-amine complex, in order to obtain an amide-alcohol; (c) reaction of said amide-alcohol with thionyl chloride in order to obtain a chlorinated amide; (d) reaction of said chlorinated amide with a phthalimide salt in order to obtain a phthalimide derivative; (e) hydrolysis of the phthalimide group of said phthalimide derivative in order to obtain (1S, 2R)-milnacipran, and (f) salification of (1S, 2R)-milnacipran in a suitable solvent system in the presence of a pharmaceutically acceptable acid.
    Type: Application
    Filed: January 29, 2010
    Publication date: December 1, 2011
    Applicant: PIERRE FABRE MEDICAMENT
    Inventors: Marc Nicolas, Paul Hellier, Catherine Diard, Laurent Subra
  • Publication number: 20110280803
    Abstract: The present invention provides a method for the synthesis of radioiodinated compounds which is advantageous over prior art methods. Using a hydrazine or an aminoxy in place of a primary amine for indirect radioiodination facilitates a much quicker reaction thus reducing reaction time and increasing the yield. In addition, where there are primary amines in the molecule to be radioiodinated, such as the N-terminus of a peptide or lysine residues, reaction at the hydrazine or aminoxy is greatly favoured.
    Type: Application
    Filed: January 29, 2010
    Publication date: November 17, 2011
    Applicant: GE HEALTHCARE UK LIMITED
    Inventors: Michelle Avory, Jane Brown, Peter Brian Iveson
  • Publication number: 20110245494
    Abstract: The present invention includes methods/processes and intermediates for preparing compounds having structural Formula (I): wherein X is alkyl, substituted alkyl, alkenyl, substituted alkenyl, heteroalkyl, substituted heteroalkyl, heteroalkenyl, or substituted heteroalkenyl.
    Type: Application
    Filed: July 29, 2009
    Publication date: October 6, 2011
    Applicant: SENOMYX, INC.
    Inventors: Catherine Tachdjian, Donald S. Karanewsky, Xiao-Qing Tang, Qing Chen, Peter Leeming, Tayyab Rashid, Daniel Levin
  • Publication number: 20110237678
    Abstract: A compound of general formula (I). A process for preparing this compound. A fungicidal composition comprising a compound of general formula (I). A method for treating plants by applying a compound of general formula (I) or a composition comprising it.
    Type: Application
    Filed: April 26, 2011
    Publication date: September 29, 2011
    Applicant: BAYER CROPSCIENCE AG
    Inventors: Darren MANSFIELD, Pierre-Yves COQUERON, Heiko RIECK, Philippe DESBORDES, Alain VILLIER, Marie-Claire GROSJEAN-COURNOYER, Pierre GENIX
  • Publication number: 20110224459
    Abstract: The invention relates to new ?-hydroxyalkylamides, to a method for production of same and to the use of same.
    Type: Application
    Filed: March 12, 2010
    Publication date: September 15, 2011
    Applicant: EVONIK DEGUSSA GmbH
    Inventors: Werner Grenda, Emmanouil Spyrou
  • Publication number: 20110218353
    Abstract: Disclosed are fluorovinyl ether functionalized aromatic diesters and derivatives thereof. The compounds disclosed have utility as functionalized monomers and comonomers in polyesters, polyamides, and the like. It has been found that incorporation of the monomers into polymers provides improved soil resistance to shaped articles produced from the polymers.
    Type: Application
    Filed: September 1, 2010
    Publication date: September 8, 2011
    Applicant: E.I. DU PONT DE NEMOURS AND COMPANY
    Inventors: Neville Everton Drysdale, Surbhi Mahajan, Kenneth Gene Moloy, Fredrik Nederberg, Joel M. Pollino, Joachim C. Ritter
  • Publication number: 20110212943
    Abstract: Provided herein are novel bridged cyclic derivatives of the general formula (I), their analogs, tautomeric forms, stereoisomers, polymorphs, solvates, intermediates, pharmaceutically acceptable salts, pharmaceutical compositions, metabolites and prodrugs thereof. These compounds can inhibit HDACs and are useful as therapeutic or ameliorating agent for diseases that are involved in cellular growth such as malignant tumors, autoimmune diseases, skin diseases, infections, inflammation, neurode-generative disorders etc.
    Type: Application
    Filed: October 14, 2009
    Publication date: September 1, 2011
    Applicant: ORCHID RESEARCH LABORATORIES LIMITED
    Inventors: Gopalan Balasubramanian, Ponpandian Thanasekaran, Sridharan Rajagopal, Bharathimohan Kuppusamy, Virendra Kachhadia, Vignesh Radhakrishnan, Sivasudar Velaiah, Shridhar Narayanan, Mandar Bhonde, Praveen Rajendran, Sriram Rajagopal
  • Publication number: 20110178339
    Abstract: A process for manufacturing dialkyl lactamide including reacting lactide and dialkylamine selected from one or more of dimethylamine, diethylamine, and methylethylamine to form a reaction mixture which includes dialkyl lactamide selected from N,N-dimethyl lactamide, N,N-diethyl lactamide, and N,N-methylethyl lactamide, N,N-dialkyl lactoyl lactamide, and dialkylamine, subjecting the reaction mixture to a separation step to form a product stream including N,N-dialkyl lactamide, a first recycle stream including dialkylamine and a second recycle stream including N,N-dialkyl lactoyl lactamide, feeding the recycle streams to the reaction step, and isolating the product stream. The process allows the manufacture of N,N-dimethyl lactamide, N,N-diethyl lactamide, and N,N-methylethyl lactamide on a commercial scale.
    Type: Application
    Filed: September 30, 2009
    Publication date: July 21, 2011
    Applicant: PURAC BIOCHEM B.V.
    Inventor: Jan Van Krieken
  • Publication number: 20110137056
    Abstract: The present invention relates to compounds useful as pharmaceutical intermediates, to processes for preparing the intermediates, to intermediates used in the processes, and to the use of the intermediates in the preparation of pharmaceuticals. In particular, the present invention concerns enantiomerically pure trans-cyclopropane carboxylic acid derivatives, processes for preparing the carboxylic acid derivatives and their use in preparing pharmaceuticals.
    Type: Application
    Filed: November 30, 2010
    Publication date: June 9, 2011
    Applicant: ASTRAZENECA AB
    Inventors: Jean-Paul Dejonghe, Koen Peeters, Marc Renard
  • Publication number: 20110137047
    Abstract: The present invention relates to a novel manufacturing process and novel intermediates useful in the synthesis of pharmaceutically active compounds, especially rennin inhibitors such as Aliskiren. The invention describes a preparation of enantiomerically pure 8-aryloctanoic acids of general formula I from readily available key intermediate, chiral cis-diacid of formula II, aziridine of formula XI and a monocyclic compound of formula III.
    Type: Application
    Filed: October 15, 2010
    Publication date: June 9, 2011
    Applicant: CarboDesign LLC
    Inventor: Milan Soukup
  • Publication number: 20110092715
    Abstract: A process for reacting, in the presence of a particular calcium containing catalyst, an amine having an active hydrogen and one or more of a fatty acid ester or a fatty acid.
    Type: Application
    Filed: October 16, 2009
    Publication date: April 21, 2011
    Inventors: Upali Weerasooriya, John Boorem, Brian Hodle, Aaron Boorem, Peter Radford, Howard Stevenson, G. Gerald Barr
  • Publication number: 20110021820
    Abstract: The present invention relates to the preparation of compounds of formula (I) derived from arylacetic acid comprising two phenol functions and an amide function, which have free-radical scavenging and antioxidant properties and which are soluble in lipid media. These compounds can be used as cosmetic and pharmaceutical preparations for the prevention of biological degradations caused by free radicals.
    Type: Application
    Filed: March 6, 2009
    Publication date: January 27, 2011
    Applicant: CATALYS SAS
    Inventors: Guy Adrian, Patrick Bigot