Oxy In Acid Moiety Patents (Class 560/29)
  • Patent number: 9447024
    Abstract: A novel process for the preparation of (R)-2-acetamido-N-benzyl-3-methoxypropionamide (Lacosamide) is described. It comprises reacting N-acetyl-D-serine methyl ester with benzylamine catalyzed by a non-nucleophilic base to obtain (R)-2-acetamido-2-N-benzyl-3-hydroxy propionamide followed by its methylation.
    Type: Grant
    Filed: October 16, 2015
    Date of Patent: September 20, 2016
    Assignee: Divi's Laboratories Limited
    Inventors: Satchandra Kiran Divi, Mysore Aswatha Narayana Rao, Shaik Nowshuddin
  • Publication number: 20150133541
    Abstract: A novel phenylcarbamate compound and a pharmaceutical composition containing the same are provided. More specifically, a novel phenylcarbamate compound, a composition for muscle relaxation containing the phenylcarbamate compound as an active ingredient, and a method of muscle relaxation comprising administering a therapeutically effective amount of the phenylcarbamate compound, are provided.
    Type: Application
    Filed: January 13, 2015
    Publication date: May 14, 2015
    Inventor: Yong Moon Choi
  • Patent number: 9012497
    Abstract: The present invention relates to the cosmetic, dermatological or therapeutic use of certain cyclohexyl carbamate compounds of formula (I) given below, preferably as anti-cellulite actives.
    Type: Grant
    Filed: May 25, 2010
    Date of Patent: April 21, 2015
    Assignee: Symrise AG
    Inventors: Imke Meyer, Heiko Oertling, Nadine Hillebrand, Claudia Gömann, Rahim Brodhage
  • Publication number: 20150094457
    Abstract: Disclosed herein are non-natural amino acids and polypeptides that include at least one non-natural amino acid, and methods for making such non-natural amino acids and polypeptides. The non-natural amino acids, by themselves or as a part of a polypeptide, can include a wide range of possible functionalities, but typical have at least one oxime, carbonyl, dicarbonyl, and/or hydroxylamine group. Also disclosed herein are non-natural amino acid polypeptides that are further modified post-translationally, methods for effecting such modifications, and methods for purifying such polypeptides. Typically, the modified non-natural amino acid polypeptides include at least one oxime, carbonyl, dicarbonyl, and/or hydroxylamine group. Further disclosed are methods for using such non-natural amino acid polypeptides and modified non-natural amino acid polypeptides, including therapeutic, diagnostic, and other biotechnology uses.
    Type: Application
    Filed: May 29, 2014
    Publication date: April 2, 2015
    Applicant: Ambrx, Inc.
    Inventors: Zhenwei MIAO, Junjie Liu, Thea Norman, Russell Driver
  • Publication number: 20150065711
    Abstract: Disclosed are linear discrete PEG constructs, which can be created and produced in a precise and reproducible way. Key to being able to do these things, where x in the discrete PEGx can vary from about 2 to about 64, is that the processes used to make each linear portion is controlled to give essentially one oligomer/one compound. Having a variable length linear discrete PEG construct that is (a) primarily an linear discrete PEG construct with diagnostic or therapeutic groups attached along a chain of attachment cores, which is attached to a preferential locator; (b) is an m-discrete PEG as the terminal construct on the linear portion, and “hidden”; (c or linear discrete PEG with a terminus group that can be either negatively or positively charged, or neutral; and any of the discrete PEG portions can be designed to be cleaved after entering the cell.
    Type: Application
    Filed: August 15, 2014
    Publication date: March 5, 2015
    Applicant: EquIP, LLC
    Inventor: Paul D. Davis
  • Publication number: 20150038733
    Abstract: Disclosed is a method of the synthesis of ramalin. It comprises reacting a glutamic acid derivative, which is prepared using alkylchloroformate, with a hydrazine salt compound, which is prepared from hydroxy aniline, whether protected or not. The synthesis method allows ramalin, excellent in antioxidant and anti-inflammatory activity, to be simply synthesized at stable yield even without use of a highly toxic solvent such as DMF. In addition, the method is cost competitive, and provides ramalin at high efficiency, thus enabling the mass production of ramalin.
    Type: Application
    Filed: March 26, 2012
    Publication date: February 5, 2015
    Applicant: KOREA INSTITUTE OF OCEAN SCIENCE AND TECHNOLOGY
    Inventors: Joung Han Yim, Il Chan Kim, Dockyu Kim, Se Jong Han, Hyoung Seok Lee, Hari Datta Bhattarai, Tai Kyoung Kim, Keun Sik Kim
  • Publication number: 20140309424
    Abstract: The invention describes novel direct synthesis methods for converting a precursor into a PET-tracer with a 18F-fluoromethoxy-group. The invention is also directed to novel and stable precursors for the direct radiosynthesis of protected derivatives of O—([18F]Fluoromethyl)tyrosines.
    Type: Application
    Filed: June 29, 2012
    Publication date: October 16, 2014
    Applicant: PIRAMAL IMAGING SA
    Inventors: Thomas Brumby, Keith Graham, Martin Kruger
  • Publication number: 20140296334
    Abstract: The invention relates to (among other things) N-optionally substituted aryl-2-oligomer-3-alkoxypropionamides and compositions comprising the same. A compound of the invention, when administered by any of a number of administration routes, exhibits one or more advantages over corresponding compounds lacking the oligomer.
    Type: Application
    Filed: October 14, 2011
    Publication date: October 2, 2014
    Inventors: Jennifer Riggs-Sauthier, Wen Zhang
  • Publication number: 20140275008
    Abstract: Provide herein are compounds and pharmaceutical compositions suitable as modulators of hemoglobin, methods and intermediates for their preparation, and methods for their use in treating disorders mediated by hemoglobin and disorders that would benefit from tissue and/or cellular oxygenation.
    Type: Application
    Filed: March 15, 2013
    Publication date: September 18, 2014
    Inventors: Qing Xu, Zhe Li
  • Patent number: 8829226
    Abstract: A new compound is provided, which is used for preparing lacosamide. A novel method for preparing lacosamide is also provided. During the reaction, iodomethane and silver oxide that are cost expensive are not used, nor a Pd-c catalyst is used, so the production cost is low, the raw materials and accessory materials are cheap and easily available, and the process is simple, so that industrial production is easy to realize; and moreover, the yield is high, and good economic efficiency can be achieved.
    Type: Grant
    Filed: January 28, 2011
    Date of Patent: September 9, 2014
    Assignee: Zhejiang Jiuzhou Pharmaceutical Co., Ltd
    Inventors: Xianyi Zhang, Shaoqing Ge, Daqing Che
  • Publication number: 20140249216
    Abstract: The instant application describes novel compounds that modulate (in particular, inhibit) Sirt2, with structures according to Formulas (1) and (2) provided herein. The invention is also directed to pharmaceutical compositions thereof, methods of treatment (i.e., cancer and neurodegenerative disease) by administration of the modulating compounds, assay methods for finding modulators of Sirt2, and kits for practicing the assay method.
    Type: Application
    Filed: October 5, 2012
    Publication date: September 4, 2014
    Applicant: CORNELL UNIVERSITY
    Inventors: Hening Lin, Bin He
  • Patent number: 8802704
    Abstract: The invention relates to oxadiazole compounds of formula I. The compounds are useful e.g. in the treatment of autoimmune disorders, such as multiple sclerosis.
    Type: Grant
    Filed: March 29, 2010
    Date of Patent: August 12, 2014
    Assignee: Merck Serono SA
    Inventors: Anna Quattropani, Cyril Montagne, Wolfgang Sauer, Stefano Crosignani, Agnès Bombrun
  • Patent number: 8748650
    Abstract: A method for production of an N-carboxy amino acid anhydride with efficiency is provided. The method for production of an N-carboxy amino acid anhydride includes a step of reaction of an amino acid organic salt compound with a carbonic acid diester.
    Type: Grant
    Filed: August 26, 2009
    Date of Patent: June 10, 2014
    Assignee: JSR Corporation
    Inventors: Takeshi Endo, Koichi Koga, Atsushi Sudo
  • Publication number: 20140116293
    Abstract: The present invention relates to a cellulose acetate film for optical compensation and a retardation enhancer used therein, and relates to a cellulose acetate film which has a high retardation value in the thickness direction (Rth).
    Type: Application
    Filed: June 20, 2012
    Publication date: May 1, 2014
    Applicant: SK INNOVATION CO., LTD.
    Inventors: Won Yeob Kim, Min Joung Im, Seung Eon Lee, Hyo Shin Kwak, Myoung Lae Kim, Yong Gyun Cho
  • Publication number: 20140116292
    Abstract: The present invention relates to a cellulose acetate film used for optical compensation and a retardation enhancer used therein, and relates to a cellulose acetate film which has a high retardation value in the thickness direction (Rth).
    Type: Application
    Filed: June 20, 2012
    Publication date: May 1, 2014
    Applicant: SK INNOVATION CO., LTD.
    Inventors: Won Yeob Kim, Min Joung Im, Seung Eon Lee, Myoung Lae Kim, Yong Gyun Cho, Sang Yeup Lee, Ki Yup Kim
  • Patent number: 8710098
    Abstract: A group of amino substituted benzoyl derivatives, their preparation and their use. The screening and research on an antiviral drug with hA3G/Vif as a target point proves that the 3-amino benzoyl derivatives not only have the combined activity for the hA3G/Vif, but also have a function of inhibiting replication of viruses. The present invention provides the possible breakthrough progress for the problem of HIV drug resistance, thereby providing a novel clinical antiviral drug which has higher efficiency.
    Type: Grant
    Filed: September 28, 2009
    Date of Patent: April 29, 2014
    Assignee: Institute of Medicinal Biotechnology Chinese Academy of Medical Science
    Inventors: Jian-Dong Jiang, Liyan Yu, Shan Cen, Zhuorong Li, Yanping Li, Jian Xu
  • Publication number: 20140114075
    Abstract: A process for the preparation in high yields and purity of the compound 6-(7-((1-aminocyclopropyl)methoxy)-6-methoxyquinolin-4-yloxy)-N-methyl-1-naphthamide of formula (I) and of the pharmaceutically acceptable salts thereof is described. The process has various advantages over those previously described, in particular it avoids the use of acyl azide intermediates and their Curtius rearrangement. Novel intermediates useful for the preparation of compound (I) are also described.
    Type: Application
    Filed: December 23, 2013
    Publication date: April 24, 2014
    Applicant: EOS ETHICAL ONCOLOGY SCIENCE S.p.A. in abbreviated form EOS S.p.A.
    Inventors: Silvano SPINELLI, Valeria LIVI
  • Patent number: 8669285
    Abstract: The present invention provides novel cycloalkylmethylamine analogs, and methods of preparing cycloalkylmethylamine analogs. The present invention also provides methods of using cycloalkylmethylamine analogs and compositions of cycloalkylmethylamine analogs. The pharmaceutical compositions of the compounds of the present invention can be advantageously used for treating and/or preventing obesity and obesity related co-morbid indications.
    Type: Grant
    Filed: April 19, 2013
    Date of Patent: March 11, 2014
    Assignee: Reviva Pharmaceuticals, Inc.
    Inventors: Laxminarayan Bhat, Seema Rani Bhat
  • Patent number: 8642780
    Abstract: The present invention relates to N-carbomethoxy-N-methoxy-(2-chloromethyl)-aniline compounds of the formula I, wherein: n is 0, 1, 2 or 3, each R1 is independently selected from halogen, C1-C4-alkyl, C1-C4-haloalkyl, C1-C4-alkoxy or C1-C4-haloalkoxy. The invention also relates to processes and intermediates for preparing such compounds of formula I. The invention furthermore relates to processes for preparing 2-(pyrazol-3?-yloxymethylene)-anilides in which compounds of formula I are applied as precursors.
    Type: Grant
    Filed: March 17, 2011
    Date of Patent: February 4, 2014
    Assignee: BASF SE
    Inventors: Maximilian Dochnahl, Bernd Mueller
  • Publication number: 20140018549
    Abstract: Compounds of Formula I are useful for the treatment of anxiety disorders such as generalized anxiety disorder (GAD), panic attack, post traumatic stress disorder (PTSD), obsessive compulsive disorder (OCD) and social phobias, wherein: A is chosen from: aryl or heteroaryl, A being optionally substituted with up to 5 independently-selected groups R8; R1 is chosen from: alkyl or haloalkyl; R2 is chosen from: H, C(O)R6, C(O)OR6, SO2R6 or C(O)NR6R7; R3, R4 and R5 are independently chosen from: H or alkyl; R6 and R7 are independently chosen from: H or alkyl; and R8 is chosen from: OH, CN, halo, alkyl, alkoxy, haloalkyl, haloalkoxy, C(O)R6, C(O)OR6, SO2R6 or C(O)NR6R7.
    Type: Application
    Filed: April 25, 2013
    Publication date: January 16, 2014
    Applicant: NPS Pharmaceuticals, Inc.
    Inventor: NPS Pharmaceuticals, Inc.
  • Patent number: 8609882
    Abstract: The invention relates to a process for the preparation of N-protected ?-aminoaldehydes by deacetalization of the acetal functional group of corresponding N-protected ?-aminoacetals using formic acid.
    Type: Grant
    Filed: April 2, 2008
    Date of Patent: December 17, 2013
    Assignee: Clariant Speciality Fine Chemicals (France)
    Inventors: Muriel Albalat, Géraldine Primazot, Didier Wilhelm, Jean-Claude Vallejos
  • Publication number: 20130331568
    Abstract: The invention provides compounds of formula I wherein n, A, R, R?, R?, R0, X and Y are as defined in the description, and their preparation. The compounds of formula I are useful as pharmaceuticals.
    Type: Application
    Filed: August 15, 2013
    Publication date: December 12, 2013
    Applicant: Novartis AG
    Inventors: Fabrizio Gasparini, Yves Auberson, Silvio Ofner, Terance W. Hart, Kaspar Zimmermann
  • Patent number: 8598386
    Abstract: The present invention relates to a method for producing (R)-2-acetamido-N-benzyl-3-methoxypropionamide (lacosamide), by methylation of (R)-2-acetamino-2-N-benzyl-3-hydroxy-propionamide (V), in which the methylation is carried out at a temperature below 20° C.
    Type: Grant
    Filed: October 17, 2011
    Date of Patent: December 3, 2013
    Assignee: Euticals GmbH
    Inventors: Richard Wisdom, Joerg Jung, Andreas Meudt
  • Publication number: 20130316985
    Abstract: A pharmaceutical composition including at least one compound of the Formulas (I), (II), or (III), or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof, as defined herein. Also disclosed is a method of treatment of diseases which are pathophysiologically related to GPR35, the GPR35-hERG signaling complex, or both, as defined herein.
    Type: Application
    Filed: May 20, 2013
    Publication date: November 28, 2013
    Applicant: Corning Incorporated
    Inventors: Huayun Deng, Ye Fang
  • Publication number: 20130296551
    Abstract: A 7-membered heterocyclic compound having the formula (I), or its salt, or a solvate thereof with a chymase inhibitory action and useful for the prevention or treatment of various diseases, in which chymase is involved: a method for producing the same, and a pharmaceutical composition useful for the prevention or treatment of diseases, in which chymase is involved, including the compound of having the formula (I), or its pharmaceutically acceptable salt, or a solvate thereof are provided.
    Type: Application
    Filed: July 3, 2013
    Publication date: November 7, 2013
    Inventors: Tsuyoshi MUTO, Taisaku Tanaka, Hiroshi Maruoka, Seiichi Imajo, Yoshiaki Tomimori
  • Publication number: 20130281453
    Abstract: Serine hydrolases are implicated in malconditions such as cancer, central nervous system disorders, cardiovascular disorders, obesity, and metabolic disorders. Many serine hydrolases expressed in proteomic libraries are of unknown function in vivo. Compounds identified through library versus library screening can be used for treatment of malconditions associated with the specific serine hydrolase KIAA1363 (also known as AADACL1). A library of inhibitors of KIAA1363 was prepared and candidate compounds were identified as a potent inhibitors having submicromolar IC50 values. An exemplary compound of the invention was shown to be an effective inhibitor of prostate cancer pathogenesis. Other inhibitory compounds of the invention comprising fluorophore groups are shown to be effective in spatial and temporal localization of the serine hydrolase in cells and tissues.
    Type: Application
    Filed: October 21, 2011
    Publication date: October 24, 2013
    Applicant: The Scripps Research Institute
    Inventors: Benjamin Cravatt, Daniel Nomura, Jae W. Chang, Raymond E. Moellering, Dan Bachovehin, Weiwei Li
  • Publication number: 20130231386
    Abstract: The present invention provides novel cycloalkylmethylamine analogs, and methods of preparing cycloalkylmethylamine analogs. The present invention also provides methods of using cycloalkylmethylamine analogs and compositions of cycloalkylmethylamine analogs. The pharmaceutical compositions of the compounds of the present invention can be advantageously used for treating and/or preventing obesity and obesity related co-morbid indications.
    Type: Application
    Filed: April 19, 2013
    Publication date: September 5, 2013
    Applicant: Reviva Pharmaceuticals, Inc.
    Inventors: Laxminarayan BHAT, Seema Rani BHAT
  • Publication number: 20130211045
    Abstract: The present invention provides novel conformationally-defined macrocyclic compounds that have been demonstrated to be selective modulators of the ghrelin receptor (growth hormone secretagogue receptor, GHS-R1a and subtypes, isoforms and variants thereof). Methods of synthesizing the novel compounds are also described herein. These compounds are useful as agonists of the ghrelin receptor and as medicaments for treatment and prevention of a range of medical conditions including, but not limited to, metabolic and/or endocrine disorders, gastrointestinal disorders, cardiovascular disorders, obesity and obesity-associated disorders, central nervous system disorders, genetic disorders, hyperproliferative disorders and inflammatory disorders.
    Type: Application
    Filed: December 17, 2012
    Publication date: August 15, 2013
    Applicant: TRANZYME PHARMA INC.
    Inventor: TRANZYME PHARMA INC.
  • Publication number: 20130202652
    Abstract: A targeting lipid can have the formula (I) in which T4 is a targeting moiety. The targeting moiety can be chosen to favor the lipid being localized with a desired organ, tissue, cell, cell type or subtype, or organelle. The targeting moiety can include, for example, transferrin, anisamide, an RGD peptide, prostate specific membrane antigen (PSMA), fucose, an antibody, or an aptamer.
    Type: Application
    Filed: July 29, 2011
    Publication date: August 8, 2013
    Applicant: ALNYLAM PHARMACEUTICALS, INC.
    Inventors: Muthiah Manoharan, Kallanthottathil G. Rajeev, Narayanannair K. Jayaprakash
  • Patent number: 8492499
    Abstract: The invention relates to addition compounds which are obtainable by reacting a) one or more polyisocyanates containing uretdione groups with b) one or more compounds of the formula (I) Y—(XH)n??(I) with the proviso that at least 50% of the free isocyanate groups of component a) are reacted with the compounds of the formula (I) to give an intermediate which contains uretdione groups, and subsequently the intermediate is reacted with c) one or more compounds of the general formula (II) Z—NHRm??(II) with the proviso that all free NCO groups optionally still present and at least 20% of uretdione groups originally used are reacted with Z—(NHR)m. The invention further relates to the use of the addition compounds as dispersants and dispersion stabilizers, and to a process for preparing them.
    Type: Grant
    Filed: March 20, 2007
    Date of Patent: July 23, 2013
    Assignee: BYK-Chemie GmbH
    Inventors: Karlheinz Haubennestel, Stefan Moessmer, Wolfgang Pritschins, Thomas Launag
  • Publication number: 20130156710
    Abstract: The present invention relates to the cosmetic, dermatological or therapeutic use of certain cyclohexyl carbamate compounds of formula (I) given below, preferably as skin and/or hair lightening (whitening) actives. The invention further relates to compositions and cosmetic, dermatological or therapeutic products comprising one or more compounds of formula (I) suitable for lightening human skin and/or hair and corresponding methods.
    Type: Application
    Filed: May 25, 2010
    Publication date: June 20, 2013
    Applicant: SYMRISE AG
    Inventors: Gabriele Vielhaber, Heiko Oertling, Nicole Titze, Claudia Gömann, Rahim Brodhage
  • Publication number: 20130137710
    Abstract: The present invention relates to the cosmetic, dermatological or therapeutic use of certain cyclohexyl carbamate compounds of formula (I) given below, preferably as anti-cellulite actives.
    Type: Application
    Filed: May 25, 2010
    Publication date: May 30, 2013
    Applicant: SYMRISE AG
    Inventors: Imke Meyer, Heiko Oertling, Nadine Hillebrand, Claudia Gömann, Rahim Brodhage
  • Publication number: 20130116457
    Abstract: The present invention provides compounds and methods that can be used to convert the intermediate halomethyl ketones (HMKs), e.g., chloromethyl ketones, to the corresponding S,S- and R,S-diastereomers. More particularly, the present invention provides: (1) reduction methods; (2) inversion methods; and (3) methods involving the epoxidation of alkenes. Using the various methods of the present invention, the R,S-epoxide and the intermediary compounds can be prepared reliably, in high yields and in high purity.
    Type: Application
    Filed: June 7, 2012
    Publication date: May 9, 2013
    Applicant: Aerojet Fine Chemicals LLC
    Inventors: Aslam A. Malik, Todd E. Clement, Hasan Palandoken, James Robinson, III, Joy A. Stringer
  • Publication number: 20130102794
    Abstract: The present invention provides an alternative synthesis of N-substituted aminotetralines comprising resolution of N-substituted aminotetralins of formula (II), wherein R1, R2 and R3 are as defined for compound of formula (I).
    Type: Application
    Filed: June 24, 2011
    Publication date: April 25, 2013
    Applicant: UCB PHARMA GMBH
    Inventors: Celal Ates, Arnaud Schule, Magali Palacio, Paul Deutsch, David Vasselin, Nicolas Carly, Ganesh Phadtare, Swapnil Yerande, Jean-Pierre Delatinne, Maria Luisa Escudero Hernandez, Veronique Pinilla
  • Publication number: 20130096317
    Abstract: The embodiments described herein provide a reduction of an aldehyde or a ketone, such as a Meerwein-Ponnorf-Verley (MPV) reaction of an aldehyde or ketone. In some embodiments, the reaction occurs in the presence of Al[OC(CH3)3]. In some embodiments, the reaction occurs in the presence of an aprotic solvent. In some embodiments, the aldehyde or ketone is an amino aldehyde or an amino ketone wherein the amine is group is protected such that the nitrogen of the amine has no proton. Other embodiments related to compositions and compounds related to the reduction reaction, or to the preparation or use of the aldehyde, the ketone, or the resulting alcohol.
    Type: Application
    Filed: November 12, 2010
    Publication date: April 18, 2013
    Applicants: GEORGIA TECH RESEARCH CORPORATION, AMERICAN PACIFIC CORPORATION
    Inventors: Charles L. Liotta, Pamela Pollet, Kristen Kitagawa Fisher, William Dubay, Joy Stringer
  • Publication number: 20130066102
    Abstract: A new compound is provided, which is used for preparing lacosamide. A novel method for preparing lacosamide is also provided. During the reaction, iodomethane and silver oxide that are cost expensive are not used, nor a Pd-c catalyst is used, so the production cost is low, the raw materials and accessory materials are cheap and easily available, and the process is simple, so that industrial production is easy to realize; and moreover, the yield is high, and good economic efficiency can be achieved.
    Type: Application
    Filed: January 28, 2011
    Publication date: March 14, 2013
    Applicant: ZHEJIANG JIUZHOU PHARMACEUTICAL CO., LTD
    Inventors: Xianyi Zhang, Shaoqing Ge, Daqing Che
  • Patent number: 8362300
    Abstract: The present invention provides addition compounds, which suitable as dispersants and as dispersion stabilizers, and to the salts of the said compounds. The invention further provides processes for preparing these addition compounds, to their use as dispersants and dispersion stabilizers for organic and inorganic pigments and also fillers in organic and aqueous systems, and to pulverous or fibrous solids coated with such dispersants and intended for incorporation into liquid systems.
    Type: Grant
    Filed: May 6, 2005
    Date of Patent: January 29, 2013
    Assignee: BYK-Chemie GmbH
    Inventors: Wolfgang Pritschins, Udo Krappe, Karlheinz Haubennestel, Andrea Esser
  • Publication number: 20130005986
    Abstract: The present invention relates to N-carbomethoxy-N-methoxy-(2-chloromethyl)-aniline compounds of the formula I, wherein: n is 0, 1, 2 or 3, each R1 is independently selected from halogen, C1-C4-alkyl, C1-C4-haloalkyl, C1-C4-alkoxy or C1-C4-haloalkoxy. The invention also relates to processes and intermediates for preparing such compounds of formula I. The invention furthermore relates to processes for preparing 2-(pyrazol-3?-yloxymethylene)-anilides in which compounds of formula I are applied as precursors.
    Type: Application
    Filed: March 17, 2011
    Publication date: January 3, 2013
    Applicant: BASF SE
    Inventors: Maximilian Dochnahl, Bernd Mueller
  • Patent number: 8344173
    Abstract: A cyclotriphosphazene represented by Formula 1 prepared by introducing a dendritic tetrapeptide and a hydrophilic polyethylene glycol into a cyclotriphosphazene ring, a method of preparing the same, and a drug carrier including the cyclotriphosphazene of Formula 1. The compound according to the present invention may form a strong molecular hydrogel in a very low concentration of 2 w/w % or less. Furthermore, the hydrogel prepared using the compound of Formula 1 exhibits biodegradability, thermosensitivity at around body temperature, biocompatibility with protein drugs, and an easy way to prepare along with a sustained release property without any burst effect in the early stage of release. Therefore, the present cyclotriphosphazene molecular hydrogel may be efficiently used as a drug carrier for a sustained release of a drug, particularly, a protein drug.
    Type: Grant
    Filed: April 28, 2009
    Date of Patent: January 1, 2013
    Assignee: CnPharm Co., Ltd.
    Inventors: Youn Soo Sohn, Yong Joo Jun, Sung Mo Choi
  • Publication number: 20120302759
    Abstract: The invention relates to a method for preparing a combretastatin derivative (I) or (II), said method including the following steps: triaryl(3,4,5-trimethoxybenzyl)phosphonium halide P3 (III), wherein Ar denotes an aryl group selected from among phenyl or thienyl, is reacted with P2 having formula (IV) or P?2 having formula (V) so as to respectively obtain the compound P4 or P?4, which have formulas (VI) and (VII), respectively; then, during a step for deprotection in the presence of an acid and/or a base, the compound having P4 or P?4 leads, after an optional purification step, to the compound having formula (I) or (II).
    Type: Application
    Filed: June 4, 2012
    Publication date: November 29, 2012
    Applicant: C/O SANOFI
    Inventors: Pascal BESSE, Eric DIDIER, Nicolas TREMAUDEUX
  • Publication number: 20120288444
    Abstract: The present invention is directed single diasteromers of 4-fluoroglutamine having a diastereomeric excess of at least 80%. Methods of preparing the single diastereomers are also described, as well as methods of using the single diastereomers of radiolabeled 4-fluoroglutamine as imaging agent is also described.
    Type: Application
    Filed: August 13, 2010
    Publication date: November 15, 2012
    Applicant: THE TRUSTEES OF THE UNIVERSITY OF PENNSYLVANIA
    Inventors: Hank F. Kung, Craig B. Thompson, Wenchao Qu, Karl Ploessl
  • Publication number: 20120283466
    Abstract: A new compound is provided, which is used for preparing lacosamide. A novel method for preparing lacosamide is also provided. During the reaction, iodomethane and silver oxide that are cost expensive are not used, nor a Pd-c catalyst is used, so the production cost is low, the raw materials and accessory materials are cheap and easily available, and the process is simple, so that industrial production is easy to realize; and moreover, the yield is high, and good economic efficiency can be achieved.
    Type: Application
    Filed: June 29, 2012
    Publication date: November 8, 2012
    Applicant: ZHEJIANG JIUZHOU PHARMACEUTICAL CO., LTD.
    Inventors: Xianyi ZHANG, Shaoqing GE, Daqing CHE
  • Publication number: 20120226066
    Abstract: The present invention is directed to novel macrocyclic compounds of formula (I) and their pharmaceutically acceptable salts, hydrates or solvates: wherein R1, R2, R3, R4, R5, R6, n1, m, p Z1, Z2, and Z3 are as describe in the specification. The invention also relates to compounds of formula (I) which are antagonists of the motilin receptor and are useful in the treatment of disorders associated with this receptor and with or with motility dysfunction.
    Type: Application
    Filed: March 5, 2012
    Publication date: September 6, 2012
    Inventors: Eric Marsault, Luc Ouellet, Hamid R. Hoveyda
  • Publication number: 20120226067
    Abstract: The present invention is directed to novel macrocyclic compounds of formula (I) and their pharmaceutically acceptable salts, hydrates or solvates: wherein R1, R2, R3, R4, R5, R6 , n1, m, p Z1, Z2, and Z3 are as describe in the specification. The invention also relates to compounds of of formula (I) which are antagonists of the motilin receptor and are useful in the treatment of disorders associated with this receptor and with or with motility dysfunction.
    Type: Application
    Filed: March 5, 2012
    Publication date: September 6, 2012
    Inventors: Eric Marsault, Luc Ouellet, Hamid R. Hoveyda
  • Publication number: 20120220784
    Abstract: The present invention provides an efficient and scalable process to prepare the compound of formula 4 by reduction of the corresponding ?-acyloxy sulfides.
    Type: Application
    Filed: February 24, 2012
    Publication date: August 30, 2012
    Applicant: ScinoPharm Singapore PTE, Ltd.
    Inventors: JyhHsiung Liao, LungHuang Kuo
  • Patent number: 8247594
    Abstract: A compound of formula (I), wherein A1, A2, A3, A4, R1, R2, R3, G1, G2, G3 and Q are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of formula (I), to insecticidal, acaricidal, molluscicidal and nematicidal compositions comprising them and to methods of using them to combat and control insect, acarine, mollusc and nematode pests.
    Type: Grant
    Filed: February 26, 2008
    Date of Patent: August 21, 2012
    Assignee: Syngenta Crop Protection LLC
    Inventors: Pierre Joseph Marcel Jung, Christopher Richard Ayles Godfrey, William Lutz, Peter Maienfisch, André Denis Stoller, Werner Zambach
  • Patent number: 8222314
    Abstract: Urethane acrylates of the general Formula (I), corresponding salts, solvates or solvates of a salt thereof: wherein R1, R2, R3, R4 and R5 each independently represent a substituent selected from the group consisting of hydrogen, halogens, C1-6-alkyls, trifluoromethyl, C1-6-alkylthios, C1-6-alkylselenos, C1-6-alkyltelluros, and nitro groups, with the proviso that at least one of R1, R2, R3, R4 and R5 is not hydrogen; R6 and R7 each independently represent a substituent selected from the group consisting of hydrogen and C1-6-alkyls; and A represents a saturated or unsaturated or linear or branched C1-6-alkyl radical or a polyalkylene oxide radical having 2-6 ethylene oxide or propylene oxide units; processes for producing and methods of using the same.
    Type: Grant
    Filed: August 7, 2009
    Date of Patent: July 17, 2012
    Assignee: Bayer MaterialScience AG
    Inventors: Thomas Roelle, Friedrich-Karl Bruder, Thomas Fäcke, Marc-Stephan Weiser, Dennis Hönel
  • Publication number: 20120178805
    Abstract: Provided are various compounds of Formula (I): Also provided are pharmaceutical compositions comprising the above compounds. Additionally, methods of inhibiting macrophage migration inhibitory factor (MIF) activity in a mammal are provided, as are methods of treating or preventing inflammation in a mammal. Further provided are methods of treating a mammal having sepsis, septicemia, and/or endotoxic shock. Also provided are methods of treating a mammal having an autoimmune disease, and methods of treating a mammal having a tumor.
    Type: Application
    Filed: March 13, 2012
    Publication date: July 12, 2012
    Inventor: Yousef Al-Abed
  • Publication number: 20120178957
    Abstract: The present invention relates to Sitagliptin intermediate and preparation method and use thereof. The method comprises reacting compound of formula (II) and trifluorobromobenzene with a Grignard reagent by a Grignard reaction to obtain a compound of formula (I). Compound of formula (I) is a new intermediate compound for the synthesis of Sitagliptin. Compound of formula (I) can be easily used for preparing another important intermediate compound of formula (V) for the synthesis of Sitagliptin.
    Type: Application
    Filed: September 25, 2010
    Publication date: July 12, 2012
    Inventors: Guoliang Zhu, Jian Zhang, Lljun Yang, Qingdan Yao, Jie Ying
  • Publication number: 20120171117
    Abstract: The present invention provides a process for [18F]-fluorination of biomolecules containing a primary amino group such as proteins and peptides and in particular of peptides. The invention further provides reagents for this process, in particular 18F-labelled prosthetic groups for use in the preparation as well as non-labelled intermediates useful in the preparation of the [18F]-labelled prosthetic groups. [18F]-labelled compounds useful as radiopharmaceuticals, specifically for use in Positron Emission Tomography (PET) are also provided.
    Type: Application
    Filed: March 8, 2012
    Publication date: July 5, 2012
    Applicant: HAMMERSMITH IMANET LIMITED
    Inventors: ERIK ARSTAD, MATTHIAS EBERHARD GLASER