Oxy In Acid Moiety Patents (Class 560/39)
  • Patent number: 10875826
    Abstract: Disclosed are improved methods for the synthesis of N-(8-[2-hydroxybenzoyl]-amino) caprylic acid. Certain compounds have been found useful for preventing the formation of a colored impurity when included in an ester hydrolysis reaction. Conducting ester hydrolysis in anaerobic conditions has also been found to minimize the formation of the color impurity. Also disclosed are improved methods for synthesizing the sodium salt of N-(8-[2-hydroxybenzoyl]-amino) caprylic acid.
    Type: Grant
    Filed: August 30, 2007
    Date of Patent: December 29, 2020
    Assignee: Emisphere Technologies, Inc.
    Inventors: William Elliot Bay, Joseph Norman Bernadino, George Frederick Klein, Yi Ren, Pingsheng Zhang
  • Patent number: 9133096
    Abstract: The present invention relates to improved processes for the production of 2-amino-2-[2-(4-C2-20alkyl-phenyl)ethyl]propane-1,3-diols, and to compounds for use therein.
    Type: Grant
    Filed: November 8, 2013
    Date of Patent: September 15, 2015
    Assignee: Novartis AG
    Inventor: Gottfried Sedelmeier
  • Publication number: 20150141615
    Abstract: The invention relates to a method or process for the chemical manufacture of depsipeptides of the formula I employing an aldehyde acetal intermediate, wherein the symbols have the meaning defined in the description, to new intermediates and their manufacture, as well as related invention embodiments.
    Type: Application
    Filed: January 14, 2015
    Publication date: May 21, 2015
    Applicant: NOVARTIS AG
    Inventors: Murat ACEMOGLU, Heribert HELLSTERN, Bernard RISS, Christian SPRECHER
  • 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: 20150057451
    Abstract: The present invention provides organic molecules and methods thereof for reactions between organoboron reagents and double bonds, such as imines or carbonyls, to stereoselectively provide chiral products including amines and alcohols, entities useful for the preparation of biologically active molecules.
    Type: Application
    Filed: March 1, 2013
    Publication date: February 26, 2015
    Inventors: Amir H. Hoveyda, Daniel L. Silverio, Tatiana Pilyugina, Sebastian Torker, Daniel Robbins
  • Patent number: 8940919
    Abstract: A compound represented by the following general formula (1), and a method for producing the compound represented by the general formula (1), the method comprising: reacting together a compound represented by the following general formula (2), a compound represented by the following general formula (3), and a compound represented by the following general formula (4): wherein R1 represents any of a protective group of a carboxyl group, and a hydrogen atom, R2 and R3 each independently represent any of a protective group of an amino group, and a hydrogen atom, and R4 represents any of a protective group of a carboxyl group, and a hydrogen atom.
    Type: Grant
    Filed: September 4, 2013
    Date of Patent: January 27, 2015
    Assignee: Microbial Chemistry Research Foundation
    Inventors: Masakatsu Shibasaki, Kenzo Yamatsugu
  • Publication number: 20150011630
    Abstract: The present invention relates to new dihydroxyphenyl modulators of neurotransmitter levels, pharmaceutical compositions thereof, and methods of use thereof.
    Type: Application
    Filed: July 8, 2014
    Publication date: January 8, 2015
    Inventors: David S. Goldstein, Courtney Holmes, Rudolf-Geisbert Alken, Frank Schneider, Chengzhi Zhang
  • Patent number: 8927659
    Abstract: The invention provides biocompatible resorbable polymers, comprising monomer units having formula (I), formula (II), formula (III) or formula (IV). The polymers degrade over time when implanted in the body, and are useful as components of implantable medical devices.
    Type: Grant
    Filed: April 22, 2013
    Date of Patent: January 6, 2015
    Assignee: TYRX, Inc.
    Inventors: Arikha Moses, Satish Pulapura, Arthur Schwartz, Qing Ge, Irene Shatova
  • Patent number: 8901169
    Abstract: In one aspect, the invention relates to compounds having the formula: where R1-R5 and X 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: Grant
    Filed: March 4, 2014
    Date of Patent: December 2, 2014
    Assignee: Theravance Biopharma R&D IP, LLC
    Inventors: Erik Fenster, Melissa Fleury, Adam D. Hughes
  • Patent number: 8900796
    Abstract: The present invention provides an acid generator generates a sulfonic acid represented by the following general formula (1) in response to high-energy beam or heat: To provide a novel acid generator which is suitably used as an acid generator for a resist composition, which solves the problems of LER and a depth of focus and can be effectively and widely used particularly without degradation of a resolution, a chemically amplified resist composition using the same, and a patterning process.
    Type: Grant
    Filed: February 15, 2013
    Date of Patent: December 2, 2014
    Assignee: Shin-Etsu Chemical Co., Ltd.
    Inventors: Masaki Ohashi, Tomohiro Kobayashi, Masayoshi Sagehashi
  • Publication number: 20140350286
    Abstract: A method for making a number (N) of samples react under the same reaction conditions, wherein the samples have a solution where the phase state of a reaction solvent changes in a reversible manner between a two-phase solution state and a uniform solution state when the temperature fluctuates over or under a certain constant temperature, and the processes are carried out sequentially in the following steps: (A) the constant container heating step of heating a number of reaction containers simultaneously and maintaining the reaction containers at a predetermined temperature; (B) the sample heating step of putting a sample in each heated reaction container and of maintaining a two-phase solution at a predetermined temperature; (C) the reaction step of stirring the sample that has been heated to the predetermined temperature so as to gain a uniform solution, which is maintained for a predetermined period of time; (D) the cooling step of cooling the uniform solution without cooling the reaction container after the
    Type: Application
    Filed: August 13, 2014
    Publication date: November 27, 2014
    Applicant: Japan Science and Technology Agency
    Inventor: Kazuhiro CHIBA
  • Publication number: 20140342989
    Abstract: A first aspect of the invention is a compound (sometimes also referred to herein as an “active agent” or “active compound”) of Formula Ia, or more particularly Formula Ib: or a pharmaceutically acceptable salt or prodrug thereof. Compositions thereof and methods of using the same (e.g. for the treatment of a neurological disease) are also described.
    Type: Application
    Filed: July 31, 2014
    Publication date: November 20, 2014
    Inventors: Harold L. Kohn, Christophe Salome, Elise Salome-Grosjean
  • Publication number: 20140343138
    Abstract: 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: Application
    Filed: February 14, 2014
    Publication date: November 20, 2014
    Applicant: THERAVANCE BIOPHARMA R&D IP, LLC
    Inventors: Adam D. Hughes, Erik Fenster, Melissa Fleury, Roland Gendron, Edmund J. Moran
  • Publication number: 20140336368
    Abstract: A multimodal contrast and radiopharmaceutical agent for an imaging and a targeted therapy guided by imaging.
    Type: Application
    Filed: November 18, 2011
    Publication date: November 13, 2014
    Applicants: CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE, UNIVERSITE DE STRASBOURG, HOSPICES CIVILS DE LYON
    Inventors: Delphine Felder-Flesch, Claire Billotey, Giuseppe Lamanna, Marc Janier, David Kriza
  • Publication number: 20140308666
    Abstract: 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: Application
    Filed: April 10, 2014
    Publication date: October 16, 2014
    Applicant: LIFE TECHNOLOGIES CORPORATION
    Inventors: Parul ANGRISH, Zhiwei YANG, Jonathan WANG
  • Publication number: 20140303232
    Abstract: This invention provides for a compound of formula (I): or a pharmaceutically acceptable salt thereof, wherein R1-R4, L and X are defined herein. The compounds of formula (I) and pharmaceutically acceptable salts thereof are cationic lipids useful in the delivery of biologically active agents to cells and tissues.
    Type: Application
    Filed: March 7, 2014
    Publication date: October 9, 2014
    Applicant: NOVARTIS AG
    Inventors: Jeremy Lee BARYZA, Rohan Eric John BECKWITH, Keith BOWMAN, Crystal BYERS, Tanzina FAZAL, Gabriel Grant GAMBER, Cameron Chuck-munn LEE, Ritesh Bhanudasji TICHKULE, Chandra VARGEESE, Shuangxi WANG, Laura Ellen West, Thomas ZABAWA, Junping ZHAO
  • Publication number: 20140296354
    Abstract: Described herein are the one-pot synthesis and characterization of a library of low molecular weight peptoid compounds that are able to form gels at room temperature. The compounds are synthesized from biologically-based starting materials, are biocompatible, and are resistant to degradation by proteases and peptidases.
    Type: Application
    Filed: April 1, 2014
    Publication date: October 2, 2014
    Applicant: OLD DOMINION UNIVERSITY RESEARCH FOUNDATION
    Inventors: Guijun WANG, Hari P. R. MANGUNURU
  • Publication number: 20140296335
    Abstract: The present invention relates to the use of a pharmaceutically effective amount of an short-acting calcium channel blocking compound to treat ischemic heart conditions, cardiac arrhythmias, hypertensive crisis in an emergency room setting, hypertension before, during, or after surgery, no-reflow phenomenon following reperfusion, and diseases associated with decreased skeletal muscle blood flow. The invention also relates to pharmaceutical compositions formulated for use in such methods and to kits for such methods.
    Type: Application
    Filed: June 16, 2014
    Publication date: October 2, 2014
    Inventors: Martin P. MAGUIRE, Elise Rioux, Harry J. Leighton
  • Publication number: 20140256730
    Abstract: Compounds represented by formulae I, II, III, and IV including pro-drugs for treprostinil and prostacyclin analogs. Uses include treatment of pulmonary hypertension (PH) or pulmonary arterial hypertension (PAH). The structures of the compounds can be adapted to the particular application for a suitable treatment dosage. Transdermal applications can be used.
    Type: Application
    Filed: January 13, 2014
    Publication date: September 11, 2014
    Applicant: Corsair Pharma, Inc.
    Inventors: Cyrus K. BECKER, Jürg R. PFISTER, Gwenaella RESCOURIO, Meenakshi S. VENKATRAMAN, Xiaoming ZHANG
  • Publication number: 20140249244
    Abstract: The present invention relates to polymer, homo- or copolymer or oligomer for the photoalignment of liquid crystals, especially for the planar orientation of liquid crystals, comprising a main chain and a side chain, wherein the side chain and/or main chain comprises a polar group, compositions thereof, and its use for optical and electro optical devices, especially liquid crystal devices (LCDs).
    Type: Application
    Filed: September 28, 2012
    Publication date: September 4, 2014
    Applicant: ROLIC AG
    Inventors: Sabrina Chappellet, Jean-Francois Eckert, Mohammed Ibn-Elhaj, Frederic Lincker, Satish Palika, Hubert Seiberle, Qian Tang, Eva Veenstra
  • Patent number: 8822527
    Abstract: 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: Grant
    Filed: October 16, 2012
    Date of Patent: September 2, 2014
    Assignee: Biotheryx, Inc.
    Inventors: Kyle W. H. Chan, Frank Mercurio, David I. Stirling
  • Patent number: 8809571
    Abstract: The present invention relates to improved processes for the production of 2-amino-2-[2-(4-C2-20-alkyl-phenyl)ethyl]propane-1,3-diols, and to compounds for use therein.
    Type: Grant
    Filed: March 17, 2009
    Date of Patent: August 19, 2014
    Assignee: Novartis AG
    Inventor: Gottfried Sedelmeier
  • Patent number: 8802659
    Abstract: 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: Grant
    Filed: August 5, 2010
    Date of Patent: August 12, 2014
    Assignee: 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
  • 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
  • Publication number: 20140213620
    Abstract: In recognition of the need to develop novel therapeutic agents, the present invention provides novel histone deacetylase inhibitors. These compounds include an ester bond making them sensitive to deactivation by esterases. Therefore, these compounds are particularly useful in the treatment of skin disorders. When the compounds reaches the bloodstream, an esterase or an enzyme with esterase activity cleaves the compound into biologically inactive fragments or fragments with greatly reduced activity Ideally these degradation products exhibit a short serum and/or systemic half-life and are eliminated rapidly. These compounds and pharmaceutical compositions thereof are particularly useful in treating cutaneous T-cell lymphoma, neurofibromatosis, psoriasis, hair loss, skin pigmentation, and dermatitis, for example. The present invention also provides methods for preparing compounds of the invention and intermediates thereto.
    Type: Application
    Filed: July 17, 2013
    Publication date: July 31, 2014
    Inventors: James Elliot Bradner, Ralph Mazitschek
  • Publication number: 20140213813
    Abstract: The invention relates to novel compounds of the formula (I), in which W, X, Y, Z and CKE are each as defined above, to several methods and intermediates for preparation thereof and to the use thereof as pesticides and/or herbicides. The invention also relates to selective herbicidal compositions which comprise firstly haloalkylmethyleneoxyphenyl-substituted ketoenols and secondly a compound which improves crop plant compatibility. The present invention further relates to the enhancement of the action of crop protection compositions comprising especially haloalkylmethyleneoxyphenyl-substituted ketoenols, by the addition of ammonium or phosphonium salts and optionally penetration enhancers, to the corresponding compositions, to methods for production thereof and to the use thereof in crop protection as insecticides and/or acaricides and/or for preventing undesired plant growth.
    Type: Application
    Filed: July 22, 2013
    Publication date: July 31, 2014
    Applicant: Bayer Intellectual Property GmbH
    Inventors: Reiner FISCHER, Thomas BRETSCHNEIDER, Stefan LEHR, Eva-Maria FRANKEN, Olga MALSAM, Arnd VOERSTE, Ulrich GORGENS, Jan DITTGEN, Dieter FEUCHT, Isolde HAUSER-HAHN, Christopher Hugh ROSINGER, Alfred Angermann
  • Publication number: 20140213814
    Abstract: A process for extraction of a peptide from a reaction mixture resulting from a peptide coupling reaction, the reaction mixture containing the peptide and a polar aprotic solvent selected from N,N-dimethylformamide, N,N-dimethylacetamide and N-methyl-2-pyrrolidone, whereby the process includes a step a) and a step b): step a) including the addition of a component a1) and a component a2), whereby component a1) is toluene and component a2) is water, to the reaction mixture, so that a biphasic system with an organic layer and an aqueous layer is obtained; step b) including the subsequent separation of the organic layer containing the peptide from the aqueous layer. In an embodiment, a combination of toluene and an organic solvent 1 selected from n-heptane, 2-methyltetrahydrofuran, ethylacetate, isopropylacetate, acetonitrile and tetrahydrofuran is used for the process for extraction. The extraction step is preferably used in a process for preparation of a peptide in liquid phase.
    Type: Application
    Filed: June 14, 2012
    Publication date: July 31, 2014
    Applicants: LONZA BRAINE S.A., LONZA LTD
    Inventors: Didier Monnaie, Luciano Forni, Mathieu Giraud
  • Patent number: 8791159
    Abstract: A compound having an ability to bind to an SIP receptor and represented by formula (I), a salt thereof, a solvate thereof or a prodrug thereof is useful for prevention and/or treatment of rejection of transplantation, graft-versus-host disease, autoimmune disease, allergic disease and the like: wherein ring A is a cyclic group; ring B is a cyclic group which may have substituent(s); X is a spacer having 1 to 8 atoms in its main chain, etc.; Y is a spacer having 1 to 10 atoms in its main chain, etc.; n is 0 or 1, wherein when n is 0, m is 1 and R1 is a hydrogen atom or a substituent, and wherein when n is 1, m is 0 or an integer of 1 to 7 and R1 is a substituent, and wherein m is 2 or more, R1s are the same or different.
    Type: Grant
    Filed: September 10, 2010
    Date of Patent: July 29, 2014
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Shinji Nakade, Hirotaka Mizuno, Takeji Ono, Masashi Minami, Hiroshi Saga, Hiroshi Hagiya, Takaki Komiya, Hiromu Habashita, Haruto Kurata, Kazuhiro Ohtsuki, Kensuke Kusumi
  • Publication number: 20140194620
    Abstract: The present invention relates to a precursor of positron emission tomography (PET) radioactive medical supplies, a preparation method thereof, and an application thereof, and more specifically, to a precursor having a tetravalent organic salt leaving group, a preparation method, and a method for preparing desired PET radioactive medical supplies in a high radiochemical yield within a short preparation time by introducing 18F using the same through a single step. The precursor having a tetravalent organic salt leaving group of the present invention can simplify the known complex multistep preparation of radioactive medical supplies into a single step, can save production costs because an excessive amount of a phase transfer catalyst is not required, facilitates separation of a compound after reaction, and enables rapid reaction velocity. The features are appropriate for the mass production of PET radioactive medical supplies by an automated synthesis system.
    Type: Application
    Filed: May 11, 2012
    Publication date: July 10, 2014
    Applicant: FUTURECHEM CO., LTD.
    Inventors: Dae-Yoon Chi, Byoung-Se Lee, Chansoo Park, Min-Hyung Lee, Hyojin Cha, Woojin Cho, Heewon Kang, Kyunghun Kim
  • Publication number: 20140163042
    Abstract: Compounds of formula (I) are inhibitors of histone deacetylase activity, and are useful in the treatment of, for example, cancers, wherein R1 is a carboxylic acid group (—COOH), or an ester group which is hydrolysable by one or more intracellular carboxyesterase enzymes to a carboxylic acid group; R2 is the side chain of a natural or non-natural alpha amino acid; Y is a bond, —C(?O), —S(?O)2—, —C(?O)O—, —C(O)NR3—, —C(?S)—NR3, —C(?NH)NR3 or —S(?O)2NR3— wherein R3 is hydrogen or optionally substituted C1-C6 alkyl; L1 is a divalent radical of formula -(Alk1)m(Q)n(Alk2)p- wherein m, n and p are independently 0 or 1, Q is (i) an optionally substituted divalent mono- or bicyclic carbocyclic or heterocyclic radical having 5-13 ring members, or (ii), in the case where both m and p are 0, a divalent radical of formula —X2-Q1- or -Q1-X2— wherein X2 is —O—, S— or NRA— wherein RA is hydrogen or optionally substituted C1-C3 alkyl, and Q1 is an optionally substituted divalent mono- or bicyclic carbocyclic or heterocyclic r
    Type: Application
    Filed: February 13, 2014
    Publication date: June 12, 2014
    Applicant: Chroma Therapeutics Ltd.
    Inventors: Alan Hornsby Davidson, Sanjay Ratilal Patel, Francesca Ann Mazzei, Stephen John Davies, Alan Hastings Drummond, David Festus Charles Moffat, Kenneth William John Baker, Alastair David Graham Donald
  • Patent number: 8729257
    Abstract: This invention relates to a novel class of hybrid lipid compound based on pentaerythritol, their intermediates, preparation methods and uses thereof. Different kinds of functional groups such as alkyl chain, siloxane group, azobenzene, porphyrins, cholesterol, benzene ring and carboxyl were introduced into the four hydroxyl groups of pentaerythritol through chemical reaction to obtain the final hybrid lipid compounds based on pentaerythritol. Cerasomes prepared from such lipids have uniform size, silicate network surface, good stability and biocompatibility, and the leakage of drugs is not easy. The present liposome can be used as functional materials such as drugs or drug carriers, or used for optical storage and molecular devices, simulation, design and synthesis of artificial systems, nano-composite membrane materials and the removal of organic pollutants, etc., in addition, the preparation method of the present invention is simple, and it is easy for industrial production.
    Type: Grant
    Filed: July 19, 2010
    Date of Patent: May 20, 2014
    Assignee: Harbin Institute of Technology
    Inventors: Zhifei Dai, Xiaolong Liang, Xiuli Yue
  • Publication number: 20140128463
    Abstract: Disclosed are amide compounds, preparation method and uses thereof, specifically, the compounds represented by formula I or pharmaceutically acceptable salts, wherein R1, R2, R3, R4, R5, Q, X and n are defined as in the description. Also disclosed are a method for preparing the compounds of formula I, a composition containing the compounds, and the uses of the same in the preparation of medicaments for regulating blood lipid and/or preventing gallstone. The compounds of formula I disclosed in the present invention have stability in vitro, good solubility in the pharmaceutical organic solvents and favorable bioavailability in animals.
    Type: Application
    Filed: June 25, 2012
    Publication date: May 8, 2014
    Applicants: China State Institute of Pharmaceutic Industry, Shanghai Institute of Pharmaceutical Industry
    Inventors: Zhenpeng Yu, Gouping Wang, Zhen Zhang, Minyu Liu, Xiaoling Huang, Ying Liu, Lin Xiao, Li Cai, Xuejun Wu, Yifang Deng, Mianli Pan, Renhai Chen, Shenrong Tang, Quanhai Liu
  • Publication number: 20140100195
    Abstract: 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: Application
    Filed: October 5, 2012
    Publication date: April 10, 2014
    Inventors: Richard D. Caldwell, Kevin M. GUCKIAN, Gnanasambandam KUMARA VEL, Wen-Cherng LEE, Edward Yin-Shiang LIN, Xiaogao LlU, Bin MA, Daniel M. SCOTT, Zhan SHl, Jermaine THOMAS, Arthur G. TAVERAS, Guo Zhu ZHENG
  • Patent number: 8686184
    Abstract: 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: Grant
    Filed: May 18, 2012
    Date of Patent: April 1, 2014
    Assignee: Theravance, Inc.
    Inventors: Melissa Fleury, Roland Gendron, Adam D. Hughes, Jane Schmidt
  • Publication number: 20140088314
    Abstract: A chelating agent, a metal-chelate, and a contrast agent are provided, wherein the chelating agent comprises a compound of structure (I) wherein R1, R2, R3, R8, R7, R?7 R?1, R?2, R?3 and R8? are selected from a hydrogen, a protected C1-C3 hydroxyalkyl group, a C1-C3 alkyl group; R4 and R?4 are selected from a hydrogen, a hydroxyl group, a protected hydroxy group, a protected C1-C3 hydroxyalkyl group, a C1-C3 alkyl group; n is an integer between 0 and 4; R5 and R?5 are selected from a hydrogen, a protecting group selected from the group consisting of C1-C30 aliphatic radicals, C3-C30 cycloaliphatic radicals, C2-C30 aromatic radicals; R9 and R?9 are selected form a hydrogen or a protecting group selected from the group consisting of C1-C30 aliphatic radicals, C3-C30 cycloaliphatic radicals, C2-C30 aromatic radicals, m is an integer between 0 and 10; and at least one of R7 and R?7 is acidic group or a protected acidic group.
    Type: Application
    Filed: September 26, 2012
    Publication date: March 27, 2014
    Applicant: GENERAL ELECTRIC COMPANY
    Inventors: Brian James Grimmond, Michael James Rishel
  • Publication number: 20140079760
    Abstract: The present invention relates to polymers modified to increase their resorbability. In particular, the polymers of the invention have phenyl ester side chains which are good leaving groups and which thereby increase the resorption rate of the polymer relative to the same polymer, for example, bearing a comparable amount of an alkyl ester side chain. Such polymers are generally water insoluble, but when modified are able to solubilize drugs and upon degradation and resorption, release those in a physiological environment in a controlled and/or sustained manner.
    Type: Application
    Filed: November 26, 2013
    Publication date: March 20, 2014
    Applicant: TYRX Pharma, Inc.
    Inventors: Arthur Schwartz, Satish Pulapura, Sarita Nethula
  • 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: 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: 20140046087
    Abstract: A compound represented by the following general formula (1), and a method for producing the compound represented by the general formula (1), the method comprising: reacting together a compound represented by the following general formula (2), a compound represented by the following general formula (3), and a compound represented by the following general formula (4): wherein R1 represents any of a protective group of a carboxyl group, and a hydrogen atom, R2 and R3 each independently represent any of a protective group of an amino group, and a hydrogen atom, and R4 represents any of a protective group of a carboxyl group, and a hydrogen atom.
    Type: Application
    Filed: September 4, 2013
    Publication date: February 13, 2014
    Applicant: Microbial Chemistry Research Foundation
    Inventors: Masakatsu SHIBASAKI, Kenzo YAMATSUGU
  • Publication number: 20140046040
    Abstract: Methods and compositions for the selective derivatization of a oligohistidine-tagged recombinant protein. A modifying compound comprised of an imidazole reactive group, a linker, and a ligating group is contacted with the recombinant protein, and a cooperative bond forms between the ligating group and the oligohistidine tag in the presence of a metal cation, and a covalent bond forms between the imidazole reactive group and an imidazole ring of the oligohistidine tag followed by the concomitant separation of the imidazole reactive group from the linker. Addition of a metal chelator results in the dissociation of the ligating group and the oligohistidine tag.
    Type: Application
    Filed: August 8, 2013
    Publication date: February 13, 2014
    Applicant: CLARKSON UNIVERSITY
    Inventor: Artem Melman
  • Publication number: 20140039194
    Abstract: The invention provides synthetic processes and synthetic intermediates that can be used to prepare 4-oxoquinolone compounds having useful integrase inhibiting properties.
    Type: Application
    Filed: August 1, 2013
    Publication date: February 6, 2014
    Applicant: Gilead Sciences, Inc.
    Inventors: Dominika PCION, Carrie TOMASI, Mark Charles WHITCOMB, Eric D. DOWDY, Wenyi FU, Patricia MACLEOD
  • Publication number: 20140031577
    Abstract: The invention relates to novel compounds of the formula (I), in which W, X, Y, Z and CKE are each as defined above, to several methods and intermediates for preparation thereof and to the use thereof as pesticides and/or herbicides. The invention also relates to selective herbicidal compositions which comprise firstly haloalkylmethyleneoxyphenyl-substituted ketoenols and secondly a compound which improves crop plant compatibility. The present invention further relates to the enhancement of the action of crop protection compositions comprising especially haloalkylmethyleneoxyphenyl-substituted ketoenols, by the addition of ammonium or phosphonium salts and optionally penetration enhancers, to the corresponding compositions, to methods for production thereof and to the use thereof in crop protection as insecticides and/or acaricides and/or for preventing undesired plant growth.
    Type: Application
    Filed: July 22, 2013
    Publication date: January 30, 2014
    Applicant: Bayer Intellectual Property GmbH
    Inventors: Reiner FISCHER, Thomas BRETSCHNEIDER, Stefan LEHR, Eva-Maria FRANKEN, Olga MALSAM, Arnd VOERSTE, Ulrich GORGENS, Jan DITTGEN, Dieter FEUCHT, Isolde HAUSER-HAHN, Christopher Hugh ROSINGER
  • Patent number: 8637547
    Abstract: Compounds of formula (I) inhibit HDAC activity, wherein A, B and D independently represent ?C— or ?N—; W is a divalent radical —CH?CH— or CH2CH2—; R1 is a carboxylic acid group (—COOH), or an ester group which is hydrolysable by one or more intracellular carboxyesterase enzymes to a carboxylic acid group; R2 is the side chain of a natural or non-natural alpha amino acid; z is 0 or 1; and Y, L1, and X1 are as defined in the claims.
    Type: Grant
    Filed: September 14, 2007
    Date of Patent: January 28, 2014
    Assignee: Chroma Therapeutics Ltd.
    Inventors: Alan Hornsby Davidson, David Charles Festus Moffat, Francesca Ann Day, Alistair David Graham Donald
  • Patent number: 8624051
    Abstract: This invention relates to a “one pot” process for the preparation of isoserine derivatives in high diastereoselective way. The process according to the invention includes the steps of reacting a protected glycidic acid with imines to yield isoserines protected both at the —OH and at the —COOH groups, deprotection of the obtained intermediates to isoserines or isoserine 1-4C— alkyl esters. Pure threo derivatives as the main isomer are obtained.
    Type: Grant
    Filed: April 13, 2011
    Date of Patent: January 7, 2014
    Assignee: Indena S.p.A.
    Inventors: Gabriele Fontana, Maria Luisa Gelmi, Federico Gassa
  • Publication number: 20130345462
    Abstract: The present invention provides a compound useful as a synthetic intermediate for an anti-HIV agent having an integrase inhibitory activity, a production method thereof, and a production method of an anti-HIV agent using the synthetic intermediate. Specifically, the present invention provides, for example, compounds represented by the formulas (6), (7-1), (7-2) and (8): wherein R is a fluorine atom or a methoxy group, R1 is a C1-C4 alkyl group, R2 is a hydroxyl-protecting group, and X2 is a halogen atom, a production method thereof, and a production method of an anti-HIV agent using the synthetic intermediate.
    Type: Application
    Filed: January 14, 2013
    Publication date: December 26, 2013
    Applicant: JAPAN TOBACCO INC.
    Inventor: JAPAN TOBACCO INC.
  • Patent number: 8586536
    Abstract: In one aspect, the invention relates to compounds having the formula: where R1-R6, a, b, and X 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: Grant
    Filed: December 14, 2011
    Date of Patent: November 19, 2013
    Assignee: Theravance, Inc.
    Inventors: Roland Gendron, Melissa Fleury, Adam D. Hughes
  • Publication number: 20130281705
    Abstract: Compounds useful for the treatment of various metabolic disorders, such as insulin resistance syndrome, diabetes, hyperlipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis, are disclosed.
    Type: Application
    Filed: June 18, 2013
    Publication date: October 24, 2013
    Inventor: Shalini SHARMA
  • Patent number: 8563714
    Abstract: The present invention relates to bridged spiro[2.4]heptane derivatives of formula (I), wherein W, Y, Z, R1 and R2 are as defined in the description, their preparation and their use as pharmaceutically active compounds as ALX receptor and/or FPRL2 agonists for the treatment of inflammatory and obstructive airways diseases.
    Type: Grant
    Filed: May 17, 2010
    Date of Patent: October 22, 2013
    Assignee: Actelion Pharmaceuticals Ltd.
    Inventors: Daniel Bur, Olivier Corminboeuf, Sylvaine Cren, Corinna Grisostomi, Xavier Leroy, Sylvia Richard-Bildstein
  • Patent number: 8558023
    Abstract: A process for preparing an enantiomerically enriched cycloalkene-substituted alanine compound having the structure: by asymmetrically hydrogenating a dehydro amino acid compound having the structure: in a suitable reaction media in the presence of a catalyst having a transition metal moiety complexed to a chiral phosphine ligand to prepare enantiomerically enriched cycloalkene substituted alanine compounds having the structure of Formula (IA) or (IB), which are key intermediates for the ACE inhibitors ramipril and perindolpril:
    Type: Grant
    Filed: April 20, 2011
    Date of Patent: October 15, 2013
    Assignee: Chiral Quest, Inc.
    Inventors: Zijun Liu, Sanhui Lin, Wenge Li, Jingyang Zhu, Xinjun Liu, Xiaojuan Zhang, Hui Lu, Fei Xiong, Zhongwei Tian
  • 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