Oxy Patents (Class 562/444)
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Patent number: 8541397Abstract: 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: GrantFiled: February 5, 2013Date of Patent: September 24, 2013Assignee: Allergan, Inc.Inventors: Santosh C. Sinha, Smita Bhat, Evelyn Corpuz, Ken Chow, Wenkui K. Fang, Wha-Bin Im
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Publication number: 20130245074Abstract: Provided is a levodopa prodrug that overcomes the problems attributed to the blood kinetics of levodopa such as large number of doses and the incidence of side effects due to frequent dosing. (2S)-2-Amino-3-(3,4-bis((2-(benzoyloxy)-2-methylpropanoyl)oxy)phenyl)propanoic acid, a salt thereof, or a solvate thereof is a levodopa prodrug, and provides a flat blood concentration-time profile of levodopa through oral administration, and therefore is useful as a preventive and/or therapeutic agent for Parkinson's disease and/or Parkinson's syndrome that overcomes the problems associated with pharmaceutical preparations of levodopa.Type: ApplicationFiled: December 1, 2011Publication date: September 19, 2013Applicant: ONO PHARMACEUTICALS CO., LTD.Inventors: Masaya Kokubo, Koji Yano
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Publication number: 20130224318Abstract: The present invention describes methods for improving the appearance of skin, particularly, treating, ameliorating, preventing, delaying, and/or improving one or more signs of excess accumulation and/or production of subcutaneous fat, such as cellulite, and conditions related thereto, by topically applying compositions comprising Carnitine Palmitoyl Transferase-1 (CPT-1) modulators, optionally with other anti-lipid agents; and also describes compositions and methods for treating, preventing and improving the appearance of skin, particularly, treating, preventing, ameliorating, reducing and/or eliminating loss of subcutaneous fat in the skin, wherein the compositions include natural plant constituents that stimulate lipid synthesis.Type: ApplicationFiled: February 26, 2013Publication date: August 29, 2013Applicant: Avon Products, Inc.Inventor: Avon Products, Inc.
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Patent number: 8519175Abstract: 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: GrantFiled: October 8, 2012Date of Patent: August 27, 2013Assignee: Bezwada Biomedical, LLCInventor: Rao S Bezwada
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Publication number: 20130217651Abstract: The present invention relates to novel phenoxy derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.Type: ApplicationFiled: February 20, 2013Publication date: August 22, 2013Applicant: ALLERGAN, INC.Inventor: ALLERGAN, INC.
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Publication number: 20130203830Abstract: The invention is related to compounds for prevention of cell injury or protection of cells. The compounds are involved in the maintenance or the increase of hydrogen sulphide in cells, which results in a protection of the cells or the prevention of cell injury. The compounds of the invention can be used in cell culture and tissue culture techniques. They can also be used in several medical conditions such as ischemia, reperfusion and hypothermia, or for preserving organs which are used for transplantation.Type: ApplicationFiled: April 18, 2011Publication date: August 8, 2013Applicant: SULFATEQ B.V.Inventors: Fatemeh Talaei, Robert Henk Henning, Adrianus C. Van der Graaf
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Patent number: 8497302Abstract: Method for the microbiological production of cinnamoyl amide derivatives of amino acids, certain products that result therefrom and uses thereof, especially as antioxidants.Type: GrantFiled: June 5, 2009Date of Patent: July 30, 2013Assignee: Institut de Recherche pour le DevelopmentInventor: Jean Lorquin
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Publication number: 20130184447Abstract: A metal coordination complex of a biologically active moiety and a metal is disclosed. The complex confers to the biologically active moiety an improved performance which can include potency, stability, absorbability, targeted delivery, and combinations thereof.Type: ApplicationFiled: March 5, 2013Publication date: July 18, 2013Applicant: SYNTHONICS, INC.Inventor: SYNTHONICS, INC.
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Publication number: 20130150331Abstract: 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: ApplicationFiled: February 5, 2013Publication date: June 13, 2013Applicant: ALLERGAN, INC.Inventor: ALLERGAN, INC.
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Patent number: 8455681Abstract: The present invention is directed to Mannich condensation product sequestering agents or mixtures of Mannich condensation product sequestering agents for use in fuels and lubricating oils. The present invention is also directed to a process for preparing the Mannich condensation product sequestering agents. The present invention is also directed to a product formed by combining, under reaction conditions, a polyisobutyl-substituted hydroxyaromatic compound, an aldehyde, an amino acid or ester thereof, and an alkali metal base to form the Mannich condensation product sequestering agent. The present invention is also directed to a lubricating oil composition, a lubricating oil concentrate, a fuel composition, and a fuel concentrate having the Mannich condensation product sequestering agents of the present invention.Type: GrantFiled: May 9, 2012Date of Patent: June 4, 2013Assignee: Chevron Oronite Company LLCInventors: James J. Harrison, Kenneth D. Nelson
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Publication number: 20130109710Abstract: The spiro compound represented by the following general formula [Ia], its pharmaceutically acceptable salt or a solvate thereofType: ApplicationFiled: September 14, 2012Publication date: May 2, 2013Applicant: JAPAN TOBACCO INC.Inventors: Takashi Shimada, Hiroshi Ueno, Kazuhiro Tsutsumi, Kouichi Aoyagi, Tomoyuki Manabe, Shin-Ya Sasaki, Susumu Katoh
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Publication number: 20130109639Abstract: In one aspect, the invention relates to compounds having the formula: where R1-R6, a, b, and Z are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.Type: ApplicationFiled: November 1, 2012Publication date: May 2, 2013Inventors: Adam D. HUGHES, Erik FENSTER, Melissa FLEURY, Roland GENDRON
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Patent number: 8431733Abstract: 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: GrantFiled: March 11, 2009Date of Patent: April 30, 2013Assignee: Virobay, Inc.Inventor: Jeffrey Dener
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Publication number: 20130102649Abstract: Disclosed herein are substituted biaryl alkyl amide compounds, methods of synthesizing substituted biaryl alkyl amide compounds and methods of treating diseases and/or conditions with substituted biaryl alkyl amide compounds.Type: ApplicationFiled: October 16, 2012Publication date: April 25, 2013Applicant: BioTheryX, Inc.Inventor: BioTheryX, Inc.
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Patent number: 8410052Abstract: The invention is directed to a method of administering pharmaceutical compositions comprising peptide drugs such as a calcitonin in combination with one or more oral delivery agents, together with an amount of a liquid, and method of treatment of disorders responsive to the action of peptide drugs such as a calcitonin employing such method of administration so as to enhance the oral bioavailability of a calcitonin. The methods of the invention increase the oral absorption and systemic bioavailability of peptide drugs, such as a calcitonin.Type: GrantFiled: February 29, 2008Date of Patent: April 2, 2013Assignee: Novartis AGInventor: Yatindra Joshi
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Patent number: 8404663Abstract: 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: GrantFiled: November 28, 2011Date of Patent: March 26, 2013Assignee: Allergan, Inc.Inventors: Santosh C. Sinha, Smita S. Bhat, Evelyn G. Corpuz, Ken Chow, Wenkui K. Fang, Wha-Bin Im
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Publication number: 20130071439Abstract: Methods of treating or reducing biofilms, treating a biofilm-related disorder, and preventing biofilm formation using D-amino acids are described.Type: ApplicationFiled: January 10, 2011Publication date: March 21, 2013Applicant: PRESIDENT AND FELLOWS OF HARVARD COLLEGEInventors: Richard Losick, Jon Clardy, Roberto Kolter, Illana Kolodkin-Gal, Diego Romero, Shugeng Cao
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Publication number: 20130041176Abstract: Methods of analyzing glatiramer acetate (GA) to assess secondary structure, for example, alpha helical content and/or random coil content thereof are provided as are methods for preparing a composition comprising GA and methods for identifying a copolymer as GA.Type: ApplicationFiled: October 12, 2012Publication date: February 14, 2013Applicant: MOMENTA PHARMACEUTICALS, INC.Inventor: MOMENTA PHARMACEUTICALS, INC.
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Publication number: 20130034497Abstract: This invention relates to derivatives of Iodine-labeled homoglutamic acids and glutamic acids and their analogues suitable for labeling or already labeled by Iodine, methods of preparing such compounds, compositions comprising such compounds, kits comprising such compounds or compositions and uses of such compounds, compositions or kits for diagnostic imaging or radiotherapy.Type: ApplicationFiled: November 15, 2010Publication date: February 7, 2013Applicant: PIRAMAL IMAGING SAInventors: Heribert Schmitt-Willich, Niels Böhnke, Norman Koglin, Andre Müller, Holger Siebeneicher, Matthias Friebe
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Publication number: 20130018194Abstract: This invention relates to octahydro-binaphthol derivatives, which can recognize amino acids and amino alcohols enantioselectively and transform L-amino acids into D-amino acids and optically resolve amino acids or amino alcohol with high efficiency.Type: ApplicationFiled: April 1, 2011Publication date: January 17, 2013Applicants: AMINOLUX, INC, EWHA UNIVERSITY-INDUSTRY COLLABORATION FOUNDATIONInventor: Kwan-Mook Kim
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Patent number: 8349893Abstract: This invention relates to novel 4-trimethylammoniobutyrates of the formula wherein A1, R1, m and n are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds inhibit carnitine palmitoyl transferase (CPT) activity, in particular CPT2 activity, and can be used as medicaments.Type: GrantFiled: April 28, 2009Date of Patent: January 8, 2013Assignee: Hoffmann-La Roche Inc.Inventors: Mirjana Andjelkovic, Simona M. Ceccarelli, Odile Chomienne, Patrizio Mattei
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Publication number: 20130005782Abstract: This invention relates generally to integrin ligand discovery and to a method of integrin ligand discovery base upon induction of ligand-induced epitopes. Such ligands have the potential to be active agent as anti-inflammatory, anti-angiogenesis and/or anti-thrombotic agents and for the treatment of integrin mediated diseases and/or conditions.Type: ApplicationFiled: March 23, 2011Publication date: January 3, 2013Inventors: Alexandre Chigaev, Larry A. Sklar
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Patent number: 8344177Abstract: The invention relates to portable albumin binders, which are useful for improving the pharmacokinetic properties of diagnostic or therapeutic agents, in particular increasing the blood circulations time and/or the tissue penetration capacity of such agents.Type: GrantFiled: November 2, 2007Date of Patent: January 1, 2013Assignee: Philochem AGInventors: Dario Neri, Christoph Dumelln
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Publication number: 20120322066Abstract: This disclosure relates to novel detergents for use in various procedures including, for example, nucleic acid amplification reactions such as polymerase chain reaction (PCR). Methods for preparing the modified detergents are also described.Type: ApplicationFiled: June 8, 2012Publication date: December 20, 2012Applicant: Life Technologies CorporationInventors: Parul Angrish, Zhiwei Yang, Jonathan Wang
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Publication number: 20120308588Abstract: In one aspect, the invention relates to compounds having the formula: where R1, R2, R3, a, R4, R5, and R6 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.Type: ApplicationFiled: May 18, 2012Publication date: December 6, 2012Applicant: THERAVANCE, INC.Inventors: Melissa Fleury, Roland Gendron, Adam D. Hughes, Jane Schmidt
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Patent number: 8323688Abstract: The present invention relates to dosage forms of human growth hormone, the use of an absorption enhancer to allow absorption of human growth hormone into the systemic circulation in a biologically active form, in particular after oral administration, as well as the use of oral dosage forms comprising human growth hormone and an absorption enhancer for the treatment of human growth hormone deficiencies and disorders associated therewith.Type: GrantFiled: August 28, 2007Date of Patent: December 4, 2012Assignee: Novartis AGInventors: Moise Azria, Yatindra Joshi, Rosario Lobrutto, Linda Mindeholm, Ashish B Patel
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Publication number: 20120296113Abstract: The present invention generally refers to a process for the preparation of L-thyroxine derivatives. More in particular, the present invention relates to a iodination reaction of an aromatic derivative with an appropriate iodinating agent, so to afford the related iodinated compound as disodium salt, which may represent a useful intermediate for the synthesis of the L-thyroxine mono-sodium salt, and the free form thereof.Type: ApplicationFiled: December 17, 2010Publication date: November 22, 2012Applicant: BRACCO IMAGING S.P.A.Inventors: Carlo Felice Viscardi, Enrico Cappelletti, Laura Galimberti, Sonia Gazzetto, Loredana Sini
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Patent number: 8309754Abstract: 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: GrantFiled: December 24, 2011Date of Patent: November 13, 2012Assignee: Bezwada Biomedical, LLCInventor: Rao S Bezwada
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Publication number: 20120258063Abstract: An object is to provide an external preparation for skin preferably usable to prevent or ameliorate pigmentation. The object is achieved by providing a preventing or ameliorating agent for pigmentation, consisting of a compound represented by the following general formula (1), an isomer thereof, and/or a pharmacologically acceptable salt thereof, and an external preparation for skin containing the same as a component: [wherein R1 represents an unsubstituted aromatic group or an aromatic group having any substituent; R2 represents a hydrogen atom, a linear chain or branched chain alkyl group having a number of carbon atom or atoms of 1 to 4, or an acyl group having a linear or branched alkyl chain having a number of carbon atom or atoms of 1 to 4; and R3 represents a hydrogen atom or a linear chain or branched chain alkyl group having a number of carbon atom or atoms of 1 to 4.Type: ApplicationFiled: December 16, 2010Publication date: October 11, 2012Applicant: Pola Chemical Industries Inc.Inventors: Yuko Saitoh, Chihiro Kondo, Takashi Yamasaki
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Publication number: 20120253065Abstract: The present invention is directed to Mannich condensation product sequestering agents or mixtures of Mannich condensation product sequestering agents for use in fuels and lubricating oils. The present invention is also directed to a process for preparing the Mannich condensation product sequestering agents. The present invention is also directed to a product formed by combining, under reaction conditions, a polyisobutyl-substituted hydroxyaromatic compound, an aldehyde, an amino acid or ester thereof, and an alkali metal base to form the Mannich condensation product sequestering agent. The present invention is also directed to a lubricating oil composition, a lubricating oil concentrate, a fuel composition, and a fuel concentrate having the Mannich condensation product sequestering agents of the present invention.Type: ApplicationFiled: May 9, 2012Publication date: October 4, 2012Applicant: Chevron Oronite Company LLCInventors: James J. Harrison, Kenneth D. Nelson
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Publication number: 20120252830Abstract: The present invention provides a compound of formula I?; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, X and n are defined herein. The invention also relates to a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.Type: ApplicationFiled: June 7, 2012Publication date: October 4, 2012Applicant: NOVARTIS AGInventors: Gary Mark Coppola, Yuki Iwaki, Rajeshri Ganesh Karki, Toshio Kawanami, Gary Michael Ksander, Muneto Mogi, Robert Sun
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Publication number: 20120244627Abstract: Provided are methods of detecting the presence or amount of a dihydroxyvitamin D metabolite in a sample using mass spectrometry. The methods generally comprise associating an amine with a dihydroxyvitamin D metabolite in a sample, ionizing the adduct, and detecting the amount of the ion to determine the presence or amount of the vitamin D metabolite in the sample.Type: ApplicationFiled: October 19, 2010Publication date: September 27, 2012Applicant: Georgetown UniversityInventor: Steven J. Soldin
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Publication number: 20120203023Abstract: A novel process for the preparation of a phenylalanine derivative of formula (I):Type: ApplicationFiled: October 19, 2010Publication date: August 9, 2012Inventors: Joseph Paul Adams, Toru Kuroda, Hiroaki Matsumae, John Bryce Strachan, Nobuhiro Yagi
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Publication number: 20120190748Abstract: Formulations and delivery systems that include a thyroid hormone active agent consisting essentially of T4 should reduce fluctuations in delivery of thyroid hormone.Type: ApplicationFiled: August 3, 2010Publication date: July 26, 2012Inventor: Haren Treasurer
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Publication number: 20120190649Abstract: Compounds that have agonist activity at one or more of the S1P receptors are provided. The compounds are sphingosine analogs that, after phosphorylation, can behave as agonists at S1P receptors.Type: ApplicationFiled: August 5, 2010Publication date: July 26, 2012Applicant: BIOGEN IDEC MA INC.Inventors: Jermaine Thomas, Xiaogao Liu, Edward Yin-Shiang Lin, Guo Zhu Zheng, Bin Ma, Richard D. Caldwell, Kevin M. Guckian, Gnanasambandam Kumaravel, Arthur G. Taveras
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Publication number: 20120189546Abstract: This invention relates to novel cyclo alkyl compounds suitable for labeling by 18F, methods of preparing such a compound, compositions comprising such compounds, kits comprising such compounds or compositions and uses of such compounds, compositions or kits for diagnostic imaging by positron emission tomography (PET).Type: ApplicationFiled: July 9, 2010Publication date: July 26, 2012Applicant: BAYER PHARMA AKTIENGESELLSCHAFTInventors: Keith Graham, Heribert Schmitt-Willich, Dominic Franck
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Patent number: 8207227Abstract: The inventors have discovered that the disodium salt of certain delivery agents has surprisingly greater efficacy for delivering active agents than the corresponding monosodium salt. Furthermore, the inventors have discovered that the disodium salts of these delivery agents form solvates with ethanol and hydrates with water. The delivery agents have the formula wherein R1, R2, R3, and R4 are independently hydrogen, halogen, C1-C4 alkyl, or C1-C4 alkoxy; and R5 is a substituted or unsubstituted C2-C16alkylene, substituted or unsubstituted C2-C16 alkenylene, substituted or unsubstituted C1-C12 alkyl(arylene), or substituted or unsubstituted aryl(C1-C12 alkylene). The hydrates and solvates of present invention also have surprisingly greater efficacy for delivering active agents, such as heparin and calcitonin, than their corresponding monosodium salts and free acids. The present invention provides an alcohol solvate, such as ethanol solvate, of a disodium salt of a delivery agent of the formula above.Type: GrantFiled: March 22, 2011Date of Patent: June 26, 2012Assignees: Emisphere Technologies, Inc., Novartis AGInventors: William E. Bay, Rajesh K. Agarwal, Kiran Chaudhary, Michael M. Goldberg, Joanne P. Corvino, Shingai Majuru, Moise Azria, Joseph Ault, Simon D. Bateman, Subash Patel, Joseph Sikora, Rebecca F. Yang, Joseph Zielinski
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Publication number: 20120142640Abstract: 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: ApplicationFiled: November 28, 2011Publication date: June 7, 2012Applicant: ALLERGAN, INC.Inventors: Santosh C. Sinha, Smita S. Bhat, Evelyn G. Corpuz, Ken Chow, Wenkui K. Fang, Wha-Bin Im
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Publication number: 20120142778Abstract: Method for the microbiological production of cinnamoyl amide derivatives of amino acids, certain products that result therefrom and uses thereof, especially as antioxidants.Type: ApplicationFiled: June 5, 2009Publication date: June 7, 2012Inventor: Jean Lorquin
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Publication number: 20120130122Abstract: The invention relates to novel 18F-labelled compounds which may be suitable for use as Positron Emission Tomography (PET) radiotracers, and to processes for preparation of such. The 18F-labelled compounds of the invention comprise a [18F]fluoroalkenyl group.Type: ApplicationFiled: January 27, 2012Publication date: May 24, 2012Applicant: HAMMERSMITH IMANET LIMITEDInventors: ERIK ARSTAD, EDWARD GEORGE ROBINS
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Patent number: 8173840Abstract: The present invention is directed to novel therapeutic compounds comprised of an amino acid bonded to a medicament or drug having a hydroxy, amino, carboxy or acylating derivative thereon. These high therapeutic index derivatives have the same utility as the drug from which they are made, and they have enhanced pharmacological and pharmaceutical properties. In fact, the novel drug derivatives of the present invention enhance at least one therapeutic quality, as defined herein. The present invention is also directed to pharmaceutical compositions containing same.Type: GrantFiled: January 30, 2006Date of Patent: May 8, 2012Assignee: Signature R&D Holdings, LLCInventor: V. Ravi Chandran
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Publication number: 20120095256Abstract: The present invention provides a process for producing Droxidopa or a pharmaceutically acceptable salt thereof comprising a step of reacting threo-N-phthaloyl-3-(3,4-dihydroxyphenyl)-L-serine represented by the formula (1) with methylamine, whereby a process for producing threo-3-(3,4-dihydroxyphenyl)-L-serine (common name: Droxidopa), which is useful as an agent for treatment of peripheral orthostatic hypotension or an agent for treatment of Parkinson's disease, with high production efficiency and without requiring troublesome operations.Type: ApplicationFiled: June 29, 2010Publication date: April 19, 2012Applicant: DAINIPPON SUMITOMO PHARMA CO.,LTD.Inventors: Toshikazu Yagi, Koji Koyama, Masanori Itoh
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Publication number: 20120053243Abstract: To provide a parakeratosis inhibitor, pore reducing agent and skin roughness preventing/ameliorating agent that exhibit capabilities of parakeratosis inhibition, pore reduction, skin roughness prevention/amelioration, etc., and further provide a skin preparation for external use having these capabilities. There are provide a parakeratosis inhibitor and a pore reducing agent each comprising at least one compound selected from the group consisting of a glycine derivative, an aminodicarboxylic acid derivative, an acylaminodicarboxylic acid derivative, a pyrrolidinecarboxylic acid derivative, a piperidinecarboxylic acid derivative, a hexamethyleneiminecarboxylic acid, a beta-alanine derivative and salts of these derivatives.Type: ApplicationFiled: November 7, 2011Publication date: March 1, 2012Applicant: SHISEIDO COMPANY, LTD.Inventors: Mikiko Kaminuma, Masaru Suetsugu, Toshii Iida, Shinji Inomata, Keiko Takada, Yuji Katsuta
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Publication number: 20120022024Abstract: This disclosure relates to compositions and methods including for the inhibition, prevention, and/or treatment of microbial infections, including infections from such pathogens as Staphylococcus aureus.Type: ApplicationFiled: July 21, 2011Publication date: January 26, 2012Applicant: The Board of Trustees of the University of IllinoisInventors: Eric Oldfield, Yongcheng Song
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Publication number: 20120015443Abstract: Chiral selectors having ?-unsubstituted ?-amino acid derivatives of the structure: a stationary phase for separating substance mixtures containing the chiral selector, and processes for separating mixtures of chiral substances, including enantiomers, and especially enantiomers of substances selected from ?-amino acids and derivatives thereof, ?-amino acids and ?-hydroxy acids are provided.Type: ApplicationFiled: September 23, 2011Publication date: January 19, 2012Applicant: EVONIK DEGUSSA GmbHInventors: Franz-Rudolf Kunz, Peter Richter, Stefan Merget, Roland Singer, Thomas Mueller
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Publication number: 20120010292Abstract: The invention relates to novel forms of 4-({(4-carboxybutyl)[2-(2-{[4-(2-phenyl-ethyl)benzyl]oxy}phenyl)ethyl]amino}methyl)benzoic acid, in particular to the modification I, to processes for their preparation, to medicaments comprising them and to their use for fighting diseases.Type: ApplicationFiled: December 4, 2009Publication date: January 12, 2012Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFTInventors: Alfons Grunenberg, Franz-Josef Mais, Katharina Tenbieg, Birgit Keil
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Publication number: 20120004183Abstract: This invention provides compositions and methods for producing translational components that expand the number of genetically encoded amino acids in eukaryotic cells. The components include orthogonal tRNAs, orthogonal aminoacyl-tRNA synthetases, pairs of tRNAs/synthetases and unnatural amino acids. Proteins and methods of producing proteins with unnatural amino acids in eukaryotic cells are also provided.Type: ApplicationFiled: June 23, 2011Publication date: January 5, 2012Applicant: The Scripps Research InstituteInventors: Alexander Deiters, T. Ashton Cropp, Jason W. Chin, J. Christopher Anderson, Peter G. Schultz
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Publication number: 20110312911Abstract: Glucagon receptor antagonist compounds are disclosed. The compounds are useful for treating type 2 diabetes and related conditions. Pharmaceutical compositions and methods of treatment are also included.Type: ApplicationFiled: February 3, 2010Publication date: December 22, 2011Inventors: Roman Kats-Kagan, Christian P. Stevenson, Xibin Liao, Qinghong Fu, Emma R. Parmee, Songnian Lin
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Publication number: 20110313154Abstract: A method for preparing a phenylalanine derivative having a quinazoline-dione ring represented by the following formula (1) or a pharmaceutically acceptable salt thereof, comprising the following steps (a), (b) and (c): (a) reacting an acyl phenylalanine derivative represented by the following formula (2): with a carbonyl group-introducing reagent and a specific anthranilic acid derivative to thus form the corresponding carboxy-asymmetric urea derivative; (b) converting the carboxy-asymmetric urea derivative into the corresponding quinazoline-dione derivative in the presence of a carboxyl group-activating agent: (c) if desired, substituting an N-alkyl group for the hydrogen atom bonded to the nitrogen atom present in the quinazoline-dione ring of the quinazoline-dione derivative using an N-alkylation agent and then deprotecting the resulting product, when the substituent R3? which is a group corresponding to R3 is protected.Type: ApplicationFiled: August 26, 2011Publication date: December 22, 2011Applicant: AJINOMOTO CO., INC.Inventors: Noriyasu KATAOKA, Kotaro OKADO, Tatsuhiro YAMADA, Koichi FUJITA, Tamotsu SUZUKI, Tatsuya OKUZUMI, Masayuki SUGIKI, Akinori TATARA
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Publication number: 20110288174Abstract: The invention relates to novel forms of 4-({(4-carboxybutyl) [2-(2-{[4-(2-phenylethyl)benzyl]oxy}phenyl)ethyl]amino}methyl)benzoic acid, in particular to the monohydrate in form A, to processes for their preparation, to medicaments comprising them and to their use for fighting diseases.Type: ApplicationFiled: December 8, 2009Publication date: November 24, 2011Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFTInventors: Alfons Grunenberg, Franz-Josef Mais, Katharina Tenbieg, Birgit Keil