In Same Chain As Carboxyl, Or Salt Thereof Patents (Class 562/443)
  • Publication number: 20150126707
    Abstract: A method for the synthesis of daptomycin or a daptomycin analogue is carried out on a resin to form a linear precursor followed by a serine ligation macrocyclization in solution. Daptomycin analogues can differ from daptomycin by substitution of amino acids residues and/or deletion or addition of amino acid residues. Daptomycin analogues can include a different fatty acid in the side arm of the daptomycin analogue.
    Type: Application
    Filed: November 6, 2013
    Publication date: May 7, 2015
    Applicant: THE UNIVERSITY OF HONG KONG
    Inventors: Xuechen Li, Hiu Yung Lam
  • Publication number: 20150025241
    Abstract: The present invention relates to an improved method for preparing dipeptidyl peptidase-IV inhibitor and intermediate. The present invention is able to reduce preparation costs by using low cost reagents on reaction and is able to be used in mass production by improving yield.
    Type: Application
    Filed: October 3, 2014
    Publication date: January 22, 2015
    Inventors: Woo Young KWAK, Heung Jae KIM, Jong Pil MIN, Tae Hyun YOON, Moohi YOO, Geun Gho LIM, Sun Ki CHANG
  • Patent number: 8921596
    Abstract: The present invention provides a simple and efficient method for synthesis of 4-[bis(2-chloroethyl)-amino]-L-phenylalanine hydrochloride. The process involves the treatment of 4-[bis(2-chloroethyl)-amino]-L-phenylalanine free base with hydrochloric acid in water followed by isolation of 4-[bis(2-chloroethyl)-amino]-L-phenylalanine hydrochloride of desired purity.
    Type: Grant
    Filed: March 15, 2011
    Date of Patent: December 30, 2014
    Assignee: Emcure Pharmaceuticals, Ltd.
    Inventors: Mukund Keshav Gurjar, Narendra Kumar Tripathy, Sandeep Anilrao Kotharkar, Pradip Nana Patil, Samit Satish Mehta
  • Publication number: 20140343314
    Abstract: The present invention provides novel compounds useful as proteasome inhibitors. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases.
    Type: Application
    Filed: August 1, 2014
    Publication date: November 20, 2014
    Inventors: Eric L Elliott, Abu J. Ferdous, Michael J. Kaufman, Sonja A. Komar, Debra L. Mazaik, Quentin J. Mccubbin, Phuong M. Nguyen, Vaithianathan Palaniappan, Raymond D. Skwierczynski, Nobel T. Truong, Csanad M. Varga, Peter N. Zawaneh
  • Publication number: 20140294796
    Abstract: The disclosure provides compositions and methods relating to aromatic-cationic peptides. The methods comprise administering to the subject an effective amount of an aromatic-cationic peptide to subjects in need thereof. For example, the peptides may be administered to subjects in need of a mitochondrial-targeted antioxidant.
    Type: Application
    Filed: December 5, 2012
    Publication date: October 2, 2014
    Inventors: D. Travis Wilson, Marc W. Andersen, Elizabeth Mead
  • Publication number: 20140249320
    Abstract: The present invention relates to pyrrolidin-2-ones according to the formula (1), or salts thereof, wherein R1 is hydrogen or a nitrogen protecting group, methods for their preparation and their use in the preparation of NEP-inhibitors, particularly in the preparation of N-(3-carboxyl-1-oxopropyl)-(4S)-(p-phenylphenylmethyl)-4-amino-(2R)-methyl butanoic acid ethyl ester or salt thereof.
    Type: Application
    Filed: March 25, 2014
    Publication date: September 4, 2014
    Inventors: David Hook, Thomas Ruch, Bernard Riss, Bernhard Wietfeld, Gottfried Sedelmeier, Matthias Napp, Markus Bänziger, Steven Hawker, Lech Ciszewski, Liladhar Murlidhar Waykole
  • Publication number: 20140243282
    Abstract: The present invention relates to novel drug conjugates, where in two drugs are linked together through an appropriate linker having at least two functional groups capable of forming covalent bond with drugs D1 and D2. The invention also relates to developing novel compositions, methods for their preparation and their use in treating various disease conditions.
    Type: Application
    Filed: December 12, 2011
    Publication date: August 28, 2014
    Inventor: Satish Reddy Kallam
  • Patent number: 8809578
    Abstract: The present invention relates to a novel compound having excellent antioxidant activity, isolated from Ramalina terebrata, and more particularly to a novel compound, RAMALIN™, having excellent antioxidant activity, isolated from the Antarctic lichen Ramalina terebrata, a method for preparing the RAMALIN™, and a pharmaceutical composition, a functional food and a functional cosmetic composition, which contain the RAMALIN™ as an active ingredient. The RAMALIN™ according to the invention has significantly excellent antioxidant effects compared to commercially available antioxidants, and thus can be widely used in agents for treating oxidation-related diseases, anti-aging functional foods, functional cosmetic products for skin whitening and wrinkle reduction, etc.
    Type: Grant
    Filed: November 10, 2009
    Date of Patent: August 19, 2014
    Assignee: Korea Ocean Research and Development Institute
    Inventors: Joung Han Yim, Hong Kum Lee, Hari Datta Bhattarai, Paudel Babita, Il Chan Kim, Soon Gyu Hong, Doc Kyu Kim, Yoo Kyung Lee, Sung Gu Lee, Hyun Cheol Oh
  • Publication number: 20140221361
    Abstract: Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, C-19 modified triterpenoids that possess unique antiviral activity are provided as HIV maturation inhibitors, as represented by compounds of Formulas I and II: These compounds are useful for the treatment of HIV and AIDS.
    Type: Application
    Filed: February 4, 2014
    Publication date: August 7, 2014
    Inventors: Jacob Swidorski, Brian Lee Venables, Zheng Liu, Ny Sin, Nicholas A. Meanwell, Alicia Regueiro-Ren
  • Patent number: 8791295
    Abstract: A method of producing a purified optically active 4-amino-3-(substituted phenyl)butanoic acid compound which is characterized by comprising a step of making a crude optically active 4-amino-3-(substituted phenyl)butanoic acid compound contact an organic acid in the presence of water.
    Type: Grant
    Filed: September 22, 2008
    Date of Patent: July 29, 2014
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Kazuo Murakami, Masahiro Takeda, Hirofumi Kato
  • Patent number: 8791294
    Abstract: The invention relates to a process for the stereoselective preparation of amino acid derivatives, comprising a hydrogenation reaction of the compound of formula (III), alternatively its enantiomer, wherein R is (C1-C8)-alkyl; followed by a hydrolysis reaction to obtain L-mesityl alanine, alternatively its enantiomer D-mesityl alanine and, optionally, subjecting said compound to an amino group protection reaction, particularly as Fmoc. It also comprises Fmoc-L- or Fmoc-D-mesityl alanine as products per se, useful as intermediates in preparing peptides or peptide analogs with therapeutic or biological activity.
    Type: Grant
    Filed: November 19, 2008
    Date of Patent: July 29, 2014
    Assignee: BCN Peptides, S.A.
    Inventors: Llorenç Rafecas Jane, Antoni Riera Escale, Rosario Ramon Albalate, Monica Alonso Xalma
  • Publication number: 20140179897
    Abstract: The present invention relates to the crystal structures of dolastatin 16, dolamethylleuine and dolaphenvaline. The present invention also relates to processes for preparing dolamethylleuine and dolaphenvaline. The present invention further relates to computer readable medium with crystal structural data and/or information stored thereon.
    Type: Application
    Filed: April 25, 2012
    Publication date: June 26, 2014
    Inventors: George R. Pettit, Thomas Smith, Jun-Ping Xu, Delbert Herald
  • Patent number: 8716520
    Abstract: Novel method for synthesis of optically pure (S)-(?)-1,1?-bi-2-naphthol and/or (R)-(+)-1,1?-bi-2-naphthol via resolution of racemic (RS)-1,1?-bi-2-naphthol through formation of co-crystal with optically active derivatives of ?-amino acids.
    Type: Grant
    Filed: March 10, 2010
    Date of Patent: May 6, 2014
    Assignee: Lupin Limited
    Inventors: Bhairab Nath Roy, Girij Pal Singh, Piyush Suresh Lathi, Rangan Mitra
  • Publication number: 20140113842
    Abstract: Betaine surfactants of formula (I) and preparation methods and uses thereof are provided. The surfactant can decrease the interfacial surface tension of crude oil till 10?3 mN/m, have the capabilities of antiheating (130° C.), antimineralizing and antidiluting, and can be used in the field of tertiary oil recovery.
    Type: Application
    Filed: March 11, 2011
    Publication date: April 24, 2014
    Applicant: PetroChina Company Limited
    Inventors: Chunde Liu, Shiyi Yuan, Demin Wang, Xinmin Song
  • Publication number: 20140099696
    Abstract: Microspheres are produced by contacting a solution of a macromolecule or small molecule in a solvent with an antisolvent and a counterion, and chilling the solution. The microspheres are useful for preparing pharmaceuticals, nutraceuticals, cosmetic products and the like of defined dimensions.
    Type: Application
    Filed: April 30, 2013
    Publication date: April 10, 2014
    Applicant: Ansun Biopharma, Inc.
    Inventors: Michael P. Malakhov, Fang Fang
  • Publication number: 20140100357
    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 aromatic amine 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 alkylated amine 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: August 23, 2013
    Publication date: April 10, 2014
    Applicant: Ambrx, Inc.
    Inventors: Zhenwei Miao, Junjie Liu, Thea Norman
  • Patent number: 8664426
    Abstract: The present invention relates to compounds of formula I and II, which are functionalized amino acids, and polymers formed from the same. Polymers formed from the functionalized amino acids are expected to have controllable degradation profiles, enabling them to release an active component over a desired time range. The polymers are also expected to be useful in a variety of medical applications.
    Type: Grant
    Filed: July 25, 2013
    Date of Patent: March 4, 2014
    Assignee: Bezwada Biomedical, LLC
    Inventor: Rao S Bezwada
  • Publication number: 20140051858
    Abstract: The present disclosure relates to a preparation method for powder of a carbamic acid derivative, which includes reacting a liquid amine derivative with carbon dioxide at a temperature in a range of from about ?30° C. to about 500° C. at a pressure in a range of from about 0.3 MPa to about 100 MPa. In addition, the present disclosure relates to a reduction method for powder of a carbamic acid derivative to a liquid amine derivative and carbon dioxide, which includes dissolving powder of the carbamic acid derivative prepared in a solvent; refluxing the carbamic acid derivative at a temperature in a range of from about 30° C. to about 100° C.; and evaporating the solvent.
    Type: Application
    Filed: August 14, 2013
    Publication date: February 20, 2014
    Applicant: Sogang University Research Foundation
    Inventors: Nam Hwi HUR, Byeong No LEE
  • Patent number: 8653136
    Abstract: Compositions based on amino acids are described, for improving the myocardial ventricular function in patients suffering from diabetes, particularly but not exclusively II type diabetes. The compositions according to the invention comprise up to 75% of the branched chain amino acids leucine, isoleucine and valine, as active ingredients. Preferably, the compositions also comprise, as further active ingredients, up to 50% of threonine and lysine. Other essential amino acids are preferably also provided, in particular methionine, phenylalanine, histidine, tryphtophan, as well as non essential amino acids, in particular tyrosine and/or cyst(e)ine (i.e., cystine and cysteine). Other amino acids can be added, provided that their sum is in a percentage being lower than 20% with respect to the other active ingredients, and less than 10% for each single amino acid.
    Type: Grant
    Filed: April 17, 2008
    Date of Patent: February 18, 2014
    Assignee: Determinants of Metabolism Research Laboratory S.R.L.
    Inventors: Franco Conti, Francesco Saverio Dioguardi
  • Patent number: 8637620
    Abstract: The invention relates to a process for preparing a polymeric material doped with metal elements, comprising a step of polymerization of at least one monomer comprising at least one ethylenic function, said monomer being complexed with a metal element. Use of the materials obtained by means of this process as catalysts, or luminescent or magnetic materials, or as elements for laser targets.
    Type: Grant
    Filed: October 7, 2008
    Date of Patent: January 28, 2014
    Assignee: Commissariat A l'Energie Atomique et aux Energies Alternatives
    Inventors: Alexia Balland Longeau, Louis Moreau, Jérôme Thibonnet, Emilie Velasquez
  • Patent number: 8624022
    Abstract: The present invention relates to novel aniline derivatives and their use in therapy, in particular their use in the treatment of fungal infections.
    Type: Grant
    Filed: October 7, 2011
    Date of Patent: January 7, 2014
    Assignee: UCB Pharma, S.A.
    Inventors: Andrew David Carr, Judi Charlotte Neuss, Michael Glen Orchard, David William Porter
  • Patent number: 8519175
    Abstract: The present invention relates to compounds of formula I and II, which are functionalized amino acids, and polymers formed from the same. Polymers formed from the functionalized amino acids are expected to have controllable degradation profiles, enabling them to release an active component over a desired time range. The polymers are also expected to be useful in a variety of medical applications.
    Type: Grant
    Filed: October 8, 2012
    Date of Patent: August 27, 2013
    Assignee: Bezwada Biomedical, LLC
    Inventor: Rao S Bezwada
  • Publication number: 20130204033
    Abstract: Antiproliferative compounds having a structure represented by formula (II), where n, R1, R2, R3, R4, and R5 are as defined herein, can be used to treat tumors, optionally when conjugated to a ligand such as an antibody:
    Type: Application
    Filed: January 29, 2013
    Publication date: August 8, 2013
    Applicant: Medarex, Inc.
    Inventor: Medarex, Inc.
  • Publication number: 20130196433
    Abstract: Methods for enhancing cellular uptake of cargo molecules by boronating the cargo molecule, particularly with one or more phenylboronic acid groups. Cellular uptake includes at least partial uptake into the cytosol. Boronation includes ligating, crosslinking or otherwise bonding one or more phenylboronic acids substituted to contain a reactive group to a cargo molecule. Boronation also includes ligating, crosslinking or otherwise bonding a phenylboronated oligopeptide to a cargo molecule. The phenylboronate groups are optionally conjugated to the cargo molecule via linking moieties that can be selectively cleaved, such cleavable linkers can allow the phenylboronate groups to be removed from the cargo molecule after the boronated cargo molecule is introduced into the cell. The invention includes certain phenylboronates which are boronation reagents, certain boronated oligopeptides and certain boronated peptides and proteins.
    Type: Application
    Filed: January 18, 2013
    Publication date: August 1, 2013
    Inventors: Ronald T. Raines, Gregory Ellis, Michael Palte
  • Patent number: 8476286
    Abstract: Use of compound of formula (I), wherein, is, or, and wherein the symbols are as defined, or a pharmaceutically-acceptable and -cleavable ester, or acid addition salt thereof, for the preparation of a medicament for promoting the release of parathyroid hormone, e.g. for preventing or treating bone conditions which are associated with increased calcium depletion or resorption or in which stimulation of bone formation and calcium fixation in the bone is desirable.
    Type: Grant
    Filed: June 14, 2002
    Date of Patent: July 2, 2013
    Assignee: Novartis AG
    Inventors: René Beerli, Ruben A Tommasi, Sven Weiler, Leo Widler
  • Publication number: 20130158275
    Abstract: The invention relates to a new process for producing useful intermediates for the manufacture of NEP inhibitors or prodrugs thereof, in particular NEP inhibitors comprising -amino- -biphenyl- -methylalkanoic acid, or acid ester, backbone, such as N-(3-carboxyl-1-oxopropyl)-(4S)-(p-phenylphenylmethyl)-4-amino-(2R)-methyl butanoic acid ethyl ester or salt thereof.
    Type: Application
    Filed: August 22, 2011
    Publication date: June 20, 2013
    Applicant: NOVARTIS AG
    Inventors: David Hook, Bernhard Riss, Jianguang Zhou, Yunzhong Li, Erhard Bappert
  • Publication number: 20130150331
    Abstract: The present invention relates to novel alkyne and alkene derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
    Type: Application
    Filed: February 5, 2013
    Publication date: June 13, 2013
    Applicant: ALLERGAN, INC.
    Inventor: ALLERGAN, INC.
  • Patent number: 8445706
    Abstract: An unnatural amino acid including a phosphate mimicking group for mimicking a phosphate group in phosphoamino acids and a protein phosphatase modifying group for covalently binding protein phosphatases. A probe for detecting disease including a phosphate mimicking group for mimicking a phosphate group in phosphoamino acids and a protein phosphatase modifying group for covalently binding protein phosphatases. A method for detecting the presence of disease by administering the unnatural amino acid, binding the unnatural amino acid with a phosphatase, detecting a signal, and detecting the presence of disease. A method of identifying a known protein phosphatase, and a method of identifying an unknown protein phosphatase. A method of making the unnatural amino acid.
    Type: Grant
    Filed: September 1, 2009
    Date of Patent: May 21, 2013
    Assignee: Board of Trustees of Northern Illinois University
    Inventor: Kui Shen
  • Patent number: 8431733
    Abstract: The present invention relates to a process for the preparation of (2S,3S)-3-amino-N-cyclopropyl-2-hydroxyalkanamides, and their use in the preparation of HCV inhibitors and cathepsin inhibitors.
    Type: Grant
    Filed: March 11, 2009
    Date of Patent: April 30, 2013
    Assignee: Virobay, Inc.
    Inventor: Jeffrey Dener
  • Publication number: 20130035487
    Abstract: The present invention relates to non-steroidal ligands for use in nuclear receptor-based inducible gene expression system, and a method to modulate exogenous gene expression in which an ecdysone receptor complex comprising: a DNA binding domain; a ligand binding domain; a transactivation domain; and a ligand is contacted with a DNA construct comprising: the exogenous gene and a response element; wherein the exogenous gene is under the control of the response element and binding of the DNA binding domain to the response element in the presence of the ligand results in activation or suppression of the gene.
    Type: Application
    Filed: September 5, 2012
    Publication date: February 7, 2013
    Applicant: Intrexon Corporation
    Inventors: Robert Eugene HORMANN, David W. Potter, Orestes Chortyk, Colin M. Tice, Glenn Richard Carlson, Andrew Meyer, Thomas R. Opie
  • Publication number: 20120329846
    Abstract: Disclosed is an agent for use in the treatment or prevention of inflammatory bowel disease. Also disclosed is an agent for inhibiting the production of TNF-?. A therapeutic or prophylactic agent for inflammatory bowel disease comprising at least one amino acid selected from the group consisting of lysine, histidine, phenylalanine, methionine, tryptophan, glutamine, glycine, cysteine, cystine and threonine, the amino acid being administered at a dose of 0.1 to 4000 mg/kg per day; and a TNF-? production inhibitor comprising an amino acid selected from the group consisting of histidine, phenylalanine and tryptophan, the amino acid being administered at a dose of 0.1 to 4000 mg/kg per day.
    Type: Application
    Filed: March 27, 2012
    Publication date: December 27, 2012
    Applicant: Ajinomoto Co., Inc.
    Inventors: Hideki Matsumoto, Tomohisa Okutsu, Tomoko Takeda, Hideki Suzuki, Tetsuo Yano, Masaki Hashimoto, Miho Ono, Manabu Suzuki
  • Publication number: 20120321560
    Abstract: This invention relates to a chemistry branch, particularly to the field of compounds' organic synthesis that belongs to the aromatic bicyclic or naphthalene category, used in the detection of amyloid sheets. These new naphthalene derivatives have a general formula: Wherein R represents mutually independent groups. In I: R1:-alkylenyl-C(O)NH-alkylenyl-R3, -alkylenyl-C(O)O—R4, R3:—COOH, —OH, —SH, —NH2, -alkyl-NH-alkyl-N-dithiocarbamate alkaline earth metal salts, R4: H, succinimidyl group, R2: —H,-alkyl. In II: R1: -alkyl, -alkylenyl-halide-alkylenyl-hydroxyl-alkylenyl-O-aryl, —O-alkylsulfonate alkylenyl, R2: -halide-alkylenyl-O-aryl, -alkylenyl-O-alkylsulfonate, -alkylenyl-halide-, —CH(O), —HC?C(CN)2, —HC?CHNO2, -alkylenyl-NH2, -alkylenyl-NH-alkyl, -alkylenyl-alkyl-N-dithiocarbamate alkaline salts. The terms “alkyl” and “alkylenyl” refer to linear or branched aliphatic chains, preferably from 1 to 4 carbon atoms and the term halide to fluorine, bromine or iodine.
    Type: Application
    Filed: April 17, 2010
    Publication date: December 20, 2012
    Inventors: Marquiza Sablón Carrazana, Chryslaine Rodriguez-Tanty, Alejandro Perera Pintado, Suchitil Rivera Marrero, Rafaela Perez Perera, Rosa Maria López Barroso, Anais Prats Capote, Hermán Vélez Castro, Carlos Serafin Pérez Martínez, Pedro Valdés Sosa
  • Publication number: 20120316361
    Abstract: Novel method for synthesis of optically pure (S)-(?)-1,1?-bi-2-naphthol and/or (R)-(+)-1,1?-bi-2-naphthol via resolution of racemic (RS)-1,1?-bi-2-naphthol through formation of co-crystal with optically active derivatives of ?-amino acids.
    Type: Application
    Filed: March 10, 2010
    Publication date: December 13, 2012
    Applicant: Lupin Limited
    Inventors: Bhairab Nath Roy, Girij Pal Singh, Piyushi Suresh Lathi, Rangan Mitra
  • Patent number: 8309754
    Abstract: The present invention relates to compounds of formula I and II, which are functionalized amino acids, and polymers formed from the same. Polymers formed from the functionalized amino acids are expected to have controllable degradation profiles, enabling them to release an active component over a desired time range. The polymers are also expected to be useful in a variety of medical applications.
    Type: Grant
    Filed: December 24, 2011
    Date of Patent: November 13, 2012
    Assignee: Bezwada Biomedical, LLC
    Inventor: Rao S Bezwada
  • Patent number: 8293926
    Abstract: The present invention provides a method of producing a compound (IIa) or a compound (IIb), provides a method of producing a compound (IIIa) or a compound (IIIb), provides a method of producing a compound (Va) or its salt or a compound (Vb) or its salt, provides a method of producing a compound (IIIa) or a compound (IIIb), further, provides a method of producing a compound (Va) or its salt or a compound (Vb) or its salt including these production methods.
    Type: Grant
    Filed: December 8, 2006
    Date of Patent: October 23, 2012
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Junichi Yasuoka, Shoji Fukuyo, Tetsuya Ikemoto
  • Publication number: 20120264825
    Abstract: The invention provides compounds which are -amino acid hydrogen peroxide solvates, wherein the side chain of the -amino acid has no basic nitrogen. A process for preparing the compounds and uses thereof are also described.
    Type: Application
    Filed: May 6, 2010
    Publication date: October 18, 2012
    Inventors: Ovadia Lev, Petr Prikhodchenko
  • Patent number: 8273793
    Abstract: Disclosed is a method for producing precursors for 2-[18F]fluorophenylalanine and 6-[18F]fluoro-L-meta-tyrosine and the ?-methylated derivatives thereof, to the precursor, and to a method for producing 2-[18F]fluorophenylalanine and 6-[18F]fluoro-L-meta-tyrosine and the ?-methylated derivatives thereof from particular precursor. A compound of formula (3) is provided which enables an automated synthesis of L-3,4-dihydroxy-6-[18F]fluorophenylalanine and 6-[18F]fluoro-L-meta-tyrosine. The enantiomeric purity of the product is ?98%.
    Type: Grant
    Filed: November 21, 2008
    Date of Patent: September 25, 2012
    Assignee: Forschungszentrum Juelich GmbH
    Inventors: Franziska Wagner, Johannes Ermert, Heinrich Hubert Coenen
  • Patent number: 8269008
    Abstract: The present invention relates to novel compounds capable of modulating the stability and/or activity of hypoxia inducible factor (HIF) by inhibiting the activity of at least one HIF hydroxylase enzyme.
    Type: Grant
    Filed: December 2, 2008
    Date of Patent: September 18, 2012
    Assignee: FibroGen, Inc.
    Inventors: Michael P. Arend, Heng Cheng, Lee A. Flippin, Danny Ng, Eric D. Turtle, Min Wu
  • Publication number: 20120189600
    Abstract: The present invention relates to compositions and methods for treating neurodegenerative diseases. In some embodiments, the present invention provides compositions for treating and preventing presbycusis.
    Type: Application
    Filed: March 21, 2012
    Publication date: July 26, 2012
    Applicant: MARINE BIO CO., LTD.
    Inventor: Shinichi Someya
  • Patent number: 8217137
    Abstract: The present invention is directed to a series of new compounds, combining the unique properties of fullerenes and bio-active amino acid residues, and to methods for making such compounds. The present invention is directed toward fullerene-based amino acids, and to amino acid residues, peptide chains, proteins, and polypeptides made from such fullerene-based amino acids. The present invention is further directed to amino acid residues, peptide chains, proteins, and polypeptides comprising such fullerene-based amino acids and into which such fullerene-based amino acids have been incorporated. Exemplary compounds have been prepared, and these compounds have been characterized and confirmed with infrared (IR) spectroscopy, nuclear magnetic resonance (NMR) spectroscopy, mass spectrometry (MS), etc.
    Type: Grant
    Filed: January 14, 2005
    Date of Patent: July 10, 2012
    Assignee: William Marsh Rice University
    Inventors: Andrew R. Barron, Jianzhong Yang
  • Patent number: 8211333
    Abstract: Certain poly(oxyalkylene) colorants are disclosed along with method of preparation thereof. A method of using these colorants as fluorescent security taggants is also disclosed.
    Type: Grant
    Filed: February 22, 2011
    Date of Patent: July 3, 2012
    Assignee: Sun Chemical Corp.
    Inventors: Russell Schwartz, Don DeRussy, Dan Gloster, Steve Postle, Rakesh Vig, Ewell Cook, Tatiana Romanova
  • Publication number: 20120142916
    Abstract: The present invention relates to pyrrolidin-2-ones according to the formula (1), or salts thereof, wherein R1 is hydrogen or a nitrogen protecting group, methods for their preparation and their use in the preparation of NEP-inhibitors, particularly in the preparation of N-(3-carboxyl-1-oxopropyl)-(4S)-(p-phenylphenylmethyl)-4-amino-(2R)-methyl butanoic acid ethyl ester or salt thereof.
    Type: Application
    Filed: December 21, 2011
    Publication date: June 7, 2012
    Inventors: David Hook, Thomas Ruch, Bernhard Riss, Bernhard Wietfeld, Gottfried Sedelmeier, Matthias Napp, Markus Bänziger, Steven Hawker, Lech Ciszewski, Liladhar Murtidhar Waykole
  • Publication number: 20120141590
    Abstract: Microspheres are produced by contacting a solution of a macromolecule or small molecule in a solvent with an antisolvent and a counterion, and chilling the solution. The microspheres are useful for preparing pharmaceuticals, nutraceuticals, cosmetic products and the like of defined dimensions.
    Type: Application
    Filed: September 30, 2011
    Publication date: June 7, 2012
    Inventors: Michael Malakhov, Fang Fang
  • Publication number: 20120116117
    Abstract: The present invention provides a simple and efficient method for synthesis of 4-[bis (2-chloroethyl)-amino]-L-phenylalanine hydrochloride. The process involves the treatment of 4-[bis(2-chloroethyl)-amino]-L-phenylalanine free base with hydrochloric acid in water followed by isolation of 4-[bis(2-chloroethyl)-amino]-phenylalanine hydrochloride of desired purity.
    Type: Application
    Filed: March 15, 2011
    Publication date: May 10, 2012
    Inventors: MUKUND KESHAV GURJAR, Narendra Kumar Tripathy, Sandeep Anilrao Kotharkar, Pradip Nana Patil, Samit Satish Mehta
  • Publication number: 20120071664
    Abstract: Disclosed are ?-amino acids that are unsubstituted in the ? position; that are substituted in the ? position with an aryl group; that are substituted in the ? position with an aryl group; that bear two substituents in the ? position; and/or that are substituted in the ? and ? positions with groups which, together with the carbon atoms at the ? and ? positions, form a ring. Also disclosed are methods for making the above-mentioned ?-amino acids and other ?-amino acids which involve providing an ?,?-unsaturated imide; converting the ?,?-unsaturated imide to a 2-substituted-isoxazolidin-5-one; and converting the 2-substituted-isoxazolidin-5-one to a ?-amino acid.
    Type: Application
    Filed: September 20, 2011
    Publication date: March 22, 2012
    Applicant: NDSU Research Foundation
    Inventors: Mukund P. SIBI, Craig P. Jasperse, Prabagaran Narayanasamy, Sandeep R. Ghorpade
  • Publication number: 20120029188
    Abstract: The present invention relates to novel aniline derivatives and their use in therapy, in particular their use in the treatment of fungal infections.
    Type: Application
    Filed: October 7, 2011
    Publication date: February 2, 2012
    Applicant: UCB Pharma S.A.
    Inventors: Andrew David Carr, Judi Charlotte Neuss, Michael Glen Orchard, David William Porter
  • Patent number: 8097754
    Abstract: Provided are syntheses of (S)-(+)-3-(aminomethyl)-5-methylhexanoic acid, (S)-Pregabalin via a chiral intermediate of the following formula 4 wherein Ar is a C6-10 aromatic group, R is a straight or branched C1-4 alkyl, ester, or carboxylic acid, and R1 is a straight or branched C1-5 alkyl, aralkyl, or substituted aralkyl.
    Type: Grant
    Filed: March 24, 2008
    Date of Patent: January 17, 2012
    Assignee: Teva Pharmaceutical Industries Ltd.
    Inventors: Vinod Kumar Kansal, Brijnath P. Chaurasia, Anand Prakash Tiwari, Shivaji Haribhau Shelke
  • Publication number: 20120010161
    Abstract: The present invention relates to compounds of azapeptide or azapeptidomimetic type of formula (I): in which R1, R2, R3, X1, X2, X3, X4 and Y are as defined in claim 1, to pharmaceutical compositions containing them and to such compounds as adjuvant for an anticancer or anti-infectious medicament.
    Type: Application
    Filed: January 25, 2010
    Publication date: January 12, 2012
    Applicants: CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE, UNIVERSITE CLAUDE BERNARD LYON I
    Inventor: Joelle Paris
  • Patent number: 8022173
    Abstract: The present invention herein provides a combination of stable isotope-labeled aliphatic amino acids, which permits the structural analysis of a high molecular weight protein, in particular, a high molecular weight protein whose molecular weight exceeds 60 kDa. This is a combination of stable isotope-labeled amino acids which is characterized in that arginine (Arg), glutamine (Gln), glutamic acid (Glu), lysine (Lys), methionine (Met) and proline (Pro) satisfy the following requirements concerning the labelling pattern: (b) one of the methylene hydrogen atoms of at least one of the methylene groups is deuterated and the both of the two methylene hydrogen atoms of at least one of the methylene groups are likewise deuterated; and (d) when they each have a methyl group, the hydrogen atoms of the methyl group except for one of the same are deuterated, or the methyl group is completely deuterated.
    Type: Grant
    Filed: August 26, 2008
    Date of Patent: September 20, 2011
    Assignee: Japan Science and Technology Agency
    Inventors: Masatsune Kainosho, Tsutomu Terauchi
  • Publication number: 20110218342
    Abstract: Disclosed are ?-amino acids that are unsubstituted in the ? position; that are substituted in the ? position with an aryl group; that are substituted in the ? position with an aryl group; that bear two substituents in the ? position; and/or that are substituted in the ? and ? positions with groups which, together with the carbon atoms at the ? and ? positions, form a ring. Also disclosed are methods for making the above-mentioned ?-amino acids and other ?-amino acids which involve providing an ?,?-unsaturated imide; converting the ?,?-unsaturated imide to a 2-substituted-isoxazolidin-5-one; and converting the 2-substituted-isoxazolidin-5-one to a ?-amino acid.
    Type: Application
    Filed: July 21, 2004
    Publication date: September 8, 2011
    Inventors: Mukund P. Sibi, Craig P. Jasperse, Prabagaran Narayanasamy, Sandeep R. Ghorpade