Amide In Acid Moiety Patents (Class 560/41)
  • Patent number: 11192851
    Abstract: An object of the present invention is to provide a crystal of L-alanyl-L-glutamine having a low loose specific volume, and a method for producing the same. The present invention relates to a crystal of L-alanyl-L-glutamine in which the loose specific volume is 5.0 mL/g or less, and a method for producing the same.
    Type: Grant
    Filed: December 20, 2017
    Date of Patent: December 7, 2021
    Assignee: KYOWA HAKKO BIO CO., LTD.
    Inventor: Kazunari Fukumoto
  • Patent number: 10322182
    Abstract: The present invention is directed to novel lyophilized pharmaceutical preparations comprising a cytotoxic dipeptides such as melphalan flufenamide and one or more excipient(s) selected from the group comprising a polysorbate; a polyethylene glycol; ?-cyclodextrin; ocyclodextrin; hydroxypropyl-?-cyclodextrin; sulfobutylether-?-cyclodextrin; lactose; benzyl alcohol; disodium succinate; propylene glycol; Cremophor EL; Dimethyl sulfoxide; D-mannitol; Trehalose; Sucrose and an amino acid. This preparation may be further formulated and is useful in cancer therapy.
    Type: Grant
    Filed: August 1, 2016
    Date of Patent: June 18, 2019
    Assignee: ONCOPEPTIDES AB
    Inventors: Jack Spira, Fredrik Lehmann
  • Patent number: 10287316
    Abstract: The present invention provides a process for the production of compound (III) or a deprotected product thereof: comprising reacting compound (II) with chloroacetic acid, in the presence of a reducing agent; wherein PG is a protecting group and R is OH in a suitably protected form or (A). The invention further provides intermediate compounds formed in the process of the invention, and processes for the production of intermediate compounds.
    Type: Grant
    Filed: May 6, 2016
    Date of Patent: May 14, 2019
    Assignee: Oncopeptides AB
    Inventors: Niklas Håkan Wahlström, Johan Anders Wennerberg
  • Patent number: 9181175
    Abstract: The invention relates to a novel process, novel process steps and novel intermediates useful in the synthesis of pharmaceutically active compounds, in particular neutral endopeptidase (NEP) inhibitors.
    Type: Grant
    Filed: February 28, 2014
    Date of Patent: November 10, 2015
    Assignee: Zhejiang Jiuzhous Pharmaceutical Co., Ltd.
    Inventors: Guoliang Zhu, Lijun Yang, Ying Lin, Jie Ying
  • Patent number: 9035085
    Abstract: The present invention provides aryl ketone compounds and compositions containing them which facilitate the delivery of active agents. The aryl ketone compounds have the formula or a salt thereof, where n=1 to 9, and R1 to R5 are independently hydrogen, C1 to C4 alkyl, C1 to C4 alkoxy, C2 to C4 alkenyl, halogen, hydroxyl, —NH—C(O)—CH3, or —O—C6H5.
    Type: Grant
    Filed: March 10, 2008
    Date of Patent: May 19, 2015
    Assignee: EMISPHERE TECHNOLOGIES, INC.
    Inventors: Parshuram Rath, Maria Isabel Gomez-Orellana
  • Publication number: 20150126534
    Abstract: Covalent conjugation of an alpha amino acid ester to a modulator of the activity of a target intracellular enzyme or receptor, wherein the ester group of the conjugate is hydrolysable by one or more intracellular carboxylesterase enzymes to the corresponding acid, leads to accumulation of the carboxylic acid hydrolysis product in the cell and enables improved or more prolonged enzyme or receptor modulation relative to the unconjugated modulator.
    Type: Application
    Filed: October 7, 2014
    Publication date: May 7, 2015
    Inventors: Alan Hornsby Davidson, Alan Hastings Drummond, Lindsey Ann Needham
  • Patent number: 9023974
    Abstract: A polyimide demonstrates low coefficient of hygroscopic expansion and low water absorption coefficient when used as an insulation film. The polyimide is derived from a tetracarboxylic acid dianhydride containing ester group expressed by the general formula below, and a polyester imide precursor: wherein R is independent and represents a straight or branched-chain alkyl group with 1 to 6 carbon atoms or straight or branched-chain alkoxyl group with 1 to 6 carbon atoms, n is an integer of 0 to 4, and m is an integer of 2 to 4, but wherein, if m =2, n is an integer of 1 to 4.
    Type: Grant
    Filed: January 28, 2008
    Date of Patent: May 5, 2015
    Assignee: Honshu Chemical Industry Co., Ltd.
    Inventor: Masatoshi Hasegawa
  • Patent number: 9018255
    Abstract: The subject of the present invention are novel esters of (acyloxymethyl)acrylamide, a pharmaceutical composition containing them and their use in the production of drugs for the prophylaxis or treatment of oncogenic diseases and diseases connected with increased cell proliferation.
    Type: Grant
    Filed: October 16, 2011
    Date of Patent: April 28, 2015
    Assignees: Instytut Chemii Organicznej Polskiej Akademii Nauk, Warszawski Uniwersytet Medyczny
    Inventors: Ryszard Ostaszewski, Szymon Klossowski, Izabela Ziuzia, Angelika Szokalska, Marta Swiech, Jakub Golab
  • Patent number: 9012677
    Abstract: The present invention relates to the discovery of new class of hydrolysable amino acid derivatives and absorbable polyester amides, polyamides, polyepoxides, polyureas and polyurethanes prepared therefrom. The resultant absorbable polymers are useful for drug delivery, tissue engineering, tissue adhesives, adhesion prevention, bone wax formulations, medical device coatings, stents, stent coatings, highly porous foams, reticulated foams, wound care, cardiovascular applications, orthopedic devices, surface modifying agents and other implantable medical devices. In addition, these absorbable polymers should have a controlled degradation profile.
    Type: Grant
    Filed: November 14, 2014
    Date of Patent: April 21, 2015
    Assignee: Bezwada Biomedical, LLC
    Inventor: Rao S Bezwada
  • Publication number: 20150073173
    Abstract: The invention relates to compounds of the formula to a process for making same and to the use of the products in the solid phase peptide synthesis. The compounds of formula I are versatile peptide intermediates for the solid phase peptide synthesis (SPPS) of peptide drugs which comprise a Glu-fatty alkyl side chain building block attached to a Lys-part of the peptide chain.
    Type: Application
    Filed: November 12, 2014
    Publication date: March 12, 2015
    Applicant: HOFFMANN-LA ROCHE INC.
    Inventor: Kurt Puentener
  • Publication number: 20150073172
    Abstract: The invention relates to a method for the synthesis of a compound according to formula I comprising the following steps: a) reacting a Dane salt according to formula II and a Dane salt according to formula III with a coupling reagent; b) adding a diamine according to formula IV to the reaction mixture; and c) adding an acid to the reaction mixture to adjust the pH value of the reaction to <7; wherein L represents a C2-C20 alkyl group, a C6-C20 aryl group, or a C7-C20 alkylaryl group; R1 and R2 can be identical or different and represent a hydrogen atom, a C1-C4 alkyl group, a C1-C4 hydroxyalkyl group, a C1-C4 thioether group, a C6-C20 aryl group, a C7-C26) alkylaryl group, a C7-C20 alkylhydroxyaryl group, a C4-C20 alkylheteroaryl group with 1 to 4 heteroatoms; or a C1-C4 alkylcarboxylic moiety, which may be an acid, an amide, or which may be esterified with a C1-C6 alkyl group or a C7-C20 alkylaryl group; R3 represents a C1-C4 alkyl group; R4 represents a hydrogen atom, or a C1-C4 alkyl group; R5 represent
    Type: Application
    Filed: May 13, 2013
    Publication date: March 12, 2015
    Inventors: Martin Bindl, Roland Herrmann, Gunter Knaup
  • Publication number: 20150065586
    Abstract: The present invention relates to the discovery of new class of hydrolysable amino acid derivatives and absorbable polyester amides, polyamides, polyepoxides, polyureas and polyurethanes prepared therefrom. The resultant absorbable polymers are useful for drug delivery, tissue engineering, tissue adhesives, adhesion prevention, bone wax formulations, medical device coatings, stents, stent coatings, highly porous foams, reticulated foams, wound care, cardiovascular applications, orthopedic devices, surface modifying agents and other implantable medical devices. In addition, these absorbable polymers should have a controlled degradation profile.
    Type: Application
    Filed: November 14, 2014
    Publication date: March 5, 2015
    Inventor: Rao S. Bezwada
  • Publication number: 20150023878
    Abstract: The compounds of the invention are inhibitors of excitatory amino acid transporters (EAAT) that penetrate the blood-brain barrier to access the central nervous system. The compounds of the invention follow the structural formula: or a salt, ester or prodrug thereof, wherein X is a halogen, such as fluorine, or a radionuclide, such as fluorine-18. The compounds and methods described herein can be used for the treatment of, e.g., neurodegenerative disorders (e.g., amyotrophic lateral sclerosis), ischemia, spinal cord injury, and traumatic brain injury in a patient (e.g., a human). The invention further provides compounds and methods for the synthesis and use of radiographic tracers to diagnose and follow the progression of such disorders.
    Type: Application
    Filed: March 5, 2013
    Publication date: January 22, 2015
    Inventors: John M. Gerdes, Richard J. Bridges, Syed K. Ahmed, Sarjubhai Patel
  • Patent number: 8901341
    Abstract: The present invention relates to the discovery of new class of hydrolysable amino acid derivatives and absorbable polyester amides, polyamides, polyepoxides, polyureas and polyurethanes prepared therefrom. The resultant absorbable polymers are useful for drug delivery, tissue engineering, tissue adhesives, adhesion prevention, bone wax formulations, medical device coatings, stents, stent coatings, highly porous foams, reticulated foams, wound care, cardiovascular applications, orthopedic devices, surface modifying agents and other implantable medical devices. In addition, these absorbable polymers should have a controlled degradation profile.
    Type: Grant
    Filed: May 3, 2013
    Date of Patent: December 2, 2014
    Assignee: Bezwada Biomedical, LLC
    Inventor: Rao S. Bezwada
  • Publication number: 20140296240
    Abstract: The present invention provides a compound of formula I?; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R5, B1, X and n are defined herein. The invention also relates 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: Application
    Filed: June 17, 2014
    Publication date: October 2, 2014
    Inventors: Gary Mark COPPOLA, Yuki IWAKI, Rajeshri Ganesh KARKI, Toshio KAWANAMI, Gary Michael KSANDER, Muneto MOGI, Robert SUN
  • Publication number: 20140296559
    Abstract: This invention relates to a novel process for the synthesis of R-biphenylalaninol and to intermediate compounds that are formed in the process according to the invention, i.e. novel intermediates useful in the synthesis of R-biphenylalaninol. The in vention also relates to R-biphenylalaninol, The process according to the invention, the intermediates to of R-biphenylalaninol and of R-biphenylalaninol are all useful in the synthesis of pharmaceutically active compounds.
    Type: Application
    Filed: August 16, 2012
    Publication date: October 2, 2014
    Applicants: DSM FINE CHEMICALS AUSTRIA NFG. GMBH & CO KG, DSM IP ASSETS B.V.
    Inventors: Petrus Johannes Hermsen, Peter Hans Ermann, Peter Hans Riebel, Michael Wolberg, Andreas Hendrikus Maria De Vries
  • 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: 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
  • Patent number: 8822534
    Abstract: The present invention provides a compound of formula I?; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R5, B1, X and n are defined herein. The invention also relates 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: Grant
    Filed: November 29, 2012
    Date of Patent: September 2, 2014
    Assignee: Novartis AG
    Inventors: Yuki Iwaki, Rajeshri Ganesh Karki, Gary Michael Ksander
  • Patent number: 8822679
    Abstract: A compound useful as a building block for the manufacture of various compounds is represented by Formula A or D. In Formula A and D, z is 0 or 1; Q is a heteroatom; R1 through R11 and Ra through Rf are each independently hydrogen, a substituted or unsubstituted hydrocarbyl group, a substituted or unsubstituted heteroatom containing hydrocarbyl group, or a functional group; d, e and f are each independently 0 or greater; each of A, B and D is independently a carbon atom or a heteroatom; and two or more of R1 though R11, Ra through Rf and Y optionally combine to form a ring. In some embodiments, R8 and R9 combine to form a carbonyl group. In some embodiments, R2 and Y combine to form a ring with the Q atom. In some embodiments, the ring includes at least one double bond.
    Type: Grant
    Filed: June 22, 2012
    Date of Patent: September 2, 2014
    Assignee: California Institute of Technology
    Inventors: Brian M Stoltz, Scott C. Virgil, David E White, Taiga Yurino, Yiyang Liu, Douglas C Behenna, Douglas Duquette, Christian Eidamshaus
  • Publication number: 20140228323
    Abstract: The present invention provides a compound of formula I; or a pharmaceutically acceptable salt thereof, wherein R1, R2 and R3 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 pharmaceutical composition of the compounds of the invention and a combination of pharmacologically active agents and a compound of the invention.
    Type: Application
    Filed: February 12, 2014
    Publication date: August 14, 2014
    Applicant: NOVARTIS AG
    Inventors: David Weninger BARNES, Scott Louis COHEN, Dean Franklin Rigel
  • Publication number: 20140179947
    Abstract: The invention relates to a novel process, novel process steps and novel intermediates useful in the synthesis of pharmaceutically active compounds, in particular neutral endopeptidase (NEP) inhibitors.
    Type: Application
    Filed: February 28, 2014
    Publication date: June 26, 2014
    Inventors: Guoliang Zhu, Lijun Yang, Ying Lin, Jie Ying
  • Patent number: 8703990
    Abstract: The invention relates to a novel process, novel process steps and novel intermediates useful in the synthesis of pharmaceutically active compounds, in particular neutral endopeptidase (NEP) inhibitors.
    Type: Grant
    Filed: January 12, 2010
    Date of Patent: April 22, 2014
    Assignee: Zhejiang Jiuzhous Pharmaceutical Co., Ltd.
    Inventors: Guoliang Zhu, Lijun Yang, Ying Lin, Jie Ying
  • Patent number: 8673974
    Abstract: The present invention provides a compound of formula I; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, A1, X, X1, s 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 pharmaceutical composition of the compounds of the invention and a combination of pharmacologically active agents and a compound of the invention.
    Type: Grant
    Filed: November 11, 2011
    Date of Patent: March 18, 2014
    Assignee: Novartis AG
    Inventors: Gary Mark Coppola, Rajeshri Ganesh Karki, Toshio Kawanami
  • 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
  • Patent number: 8664391
    Abstract: The present invention relates to compounds of formula (I) that have CYP450 inhibiting properties and are useful as boosting agents when used with HIV treatments. These compounds are represented by formula including the salts and stereoisomeric forms thereof, wherein R1 is 5-thiazolyl or 3-pyridinyl; R2 is iso-butyl, 2,2-dimethylpropyl; 2-hydroxy-2-methyl-propyl or cyclohexylmethyl; R3 is phenyl optionally substituted with one or more halogens, trifluoromethyl, C1-6-alkyl or C1-6-alkoxy wherein optionally two of said alkoxy groups are be linked to each other to form a 5 or 6-membered ring; heteroaryl; C3-7cycloalkyl optionally substituted with one or more halogens; C1-6alkyl optionally substituted with heteroaryl; —O—CH2— (heteroaryl). As boosting agents they are able to increase at least one of the pharmacokinetic variables of certain drugs when co-administered, or improve the bioavailability of certain drugs.
    Type: Grant
    Filed: October 7, 2009
    Date of Patent: March 4, 2014
    Assignee: Janssen R&D Ireland Ltd
    Inventors: Tim Hugo Maria Jonckers, Wim Bert Griet Schepens, Geerwin Yvonne Paul Haché, Beate Sabine Hallenberger, Jennifer Chiyomi Sasaki, Judith Eva Baumeister, Gerben Albert Van 'T Klooster
  • Publication number: 20140031230
    Abstract: An object of the present invention is to provide an auxin biosynthesis inhibitor superior to L-AOPP. The object can be attained by a compound represented by general formula (I): wherein, R1 to R5 and X are the same as defined in the specification or a salt or solvate thereof.
    Type: Application
    Filed: February 28, 2012
    Publication date: January 30, 2014
    Inventors: Yukihisa Shimada, Ko Kikuzato, Megumi Narukawa, Tadao Asami, Kazuo Soeno
  • Patent number: 8637696
    Abstract: The invention provides novel compounds and methods to carry out organocatalytic Michael additions of aldehydes to nitroethylene catalyzed by a proline derivative to provide ?-substituted-?-nitroaldehydes. The reaction can be rendered enantioselective when a chiral pyrrolidine catalyst is used, allowing for Michael adducts in nearly optically pure form (e.g., 96-99% e.e.). The Michael adducts can bear a single substituent or dual substituents adjacent to the carbonyl. The Michael adducts can be efficiently converted to protected ?2-amino acids, which are essential for systematic conformational studies of ?-peptide foldamers.
    Type: Grant
    Filed: September 17, 2012
    Date of Patent: January 28, 2014
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Samuel Helmer Gellman, Yonggui Chi, Li Guo
  • Publication number: 20130331595
    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 12, 2013
    Publication date: December 12, 2013
    Applicant: Millennium Pharmaceuticals, Inc.
    Inventors: Edward J. Olhava, Mihaela Diana Danca
  • Publication number: 20130324678
    Abstract: Provide is a method capable of effectively improving a rejection of a permeable membrane without remarkably reducing a permeation flux, even if the membrane is seriously degraded. The method for improving a rejection of a permeable membrane supplies an aqueous solution (excluding an aqueous solution having a pH of 7 or less) containing a compound having an amino group and a molecular weight of 1,000 or less through the permeable membrane (amino-treatment step). Since the low molecular weight amino compound is supplied through the permeable membrane, degraded portions of the membrane can be restored without remarkably reducing the permeation flux thereof, and the rejection thereof can be effectively improved.
    Type: Application
    Filed: March 5, 2012
    Publication date: December 5, 2013
    Applicant: KURITA WATER INDUSTRIES LTD
    Inventors: Takahiro Kawakatsu, Tetsuya Aoki
  • Publication number: 20130324717
    Abstract: This invention relates to polymerizable ultraviolet light absorbers and yellow colorants and their use in ophthalmic lenses. In particular, this invention relates to polymerizable ultraviolet light absorbing methane compounds and yellow compounds of the methine and anthraquinone classes that block ultraviolet light and/or violet-blue light transmission through ophthalmic lenses.
    Type: Application
    Filed: August 5, 2013
    Publication date: December 5, 2013
    Inventors: Jason Clay Pearson, Max Allen Weaver, Jean Carroll Fleischer, Gregory Allan King
  • Publication number: 20130317102
    Abstract: The subject of the present invention are novel esters of (acyloxymethyl)acrylamide, a pharmaceutical composition containing them and their use in the production of drugs for the prophylaxis or treatment of oncogenic diseases and diseases connected with increased cell proliferation.
    Type: Application
    Filed: October 16, 2011
    Publication date: November 28, 2013
    Inventors: Ryszard Ostaszewski, Szymon Klossowski, Izabela Ziuzia, Angelika Szokalska, Marta Swiech, Jakub Golab
  • 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: 20130267714
    Abstract: Compounds of the formula (I) in the form of a mixture of predominantly one diastereomer or in the form of pure diastereomers, Z1-Q-P*R0R1??(I), wherein: Z1 is a C-bonded, secondary phosphine group of the formula —P(R)2, wherein R is a hydrocarbon radical or O-atom(s)-containing heterohydrocarbon radical having 1 to 18 carbon atoms and optionally substituted by C1-C6-alkyl, trifluoromethyl, C1-C6-alkoxy, trifluoromethoxy, (C1-C4-alkyl)2-amino, (C6H5)3Si, (C1-C12-alkyl)3Si or halogen; Q is selected from the group consisting of: (i) an optionally substituted achiral aromatic group, wherein the achiral aromatic group is bonded directly to Z1 through a carbon atom of the achiral aromatic group and bonded directly to P*R0R1 through a carbon atom of the achiral aromatic group, and (ii) an optionally substituted C1-C4-alkylene group; P* is a chiral phosphorus atom; R0 is methyl; and R1 is a C-bonded optically enriched or optically pure chiral, mono- or polycyclic, nonaromatic hydrocarbon ring; and prepar
    Type: Application
    Filed: April 26, 2013
    Publication date: October 10, 2013
    Inventors: Benoit PUGIN, Matthias LOTZ, Heidi LANDERT, Adrian WYSS, Raphael AARDOOM, Bjorn GSCHWEND, Andreas PFALTZ, Felix SPINDLER
  • Patent number: 8552204
    Abstract: Disclosed is a novel zinc cluster compound represented by general formula (1): Zn4O (OCOR)6 (RCOOH)n, wherein R represents an alkyl group which has 1 to 4 carbon atoms and may be substituted with a halogen atom, and n represents 0.1 to 1, and also disclosed are a method for producing the compound and a reaction using the compound.
    Type: Grant
    Filed: May 31, 2010
    Date of Patent: October 8, 2013
    Assignee: Takasago International Corporation
    Inventors: Yoshimasa Matsushima, Hideki Nara, Takahiro Fujiwara
  • Publication number: 20130244944
    Abstract: Provided herein are self-assembling compounds that can form ion channels in lipid bilayers or cell membranes and ion-channel-forming compositions comprising the self-assembling compounds. Also provided are methods of making and using the ion channels formed from a plurality of molecules of the self-assembling compounds. Further, provided are methods of treating or preventing conditions and diseases that are related to the dysfunction of ion channels, including chloride channels.
    Type: Application
    Filed: December 31, 2012
    Publication date: September 19, 2013
    Applicants: VERSITECH LIMITED, THE UNIVERSITY OF HONG KONG
    Inventors: Dan Yang, Xiang Li, Huiyan Zha
  • Publication number: 20130245133
    Abstract: The present invention relates to the discovery of new class of hydrolysable amino acid derivatives and absorbable polyester amides, polyamides, polyepoxides, polyureas and polyurethanes prepared therefrom. The resultant absorbable polymers are useful for drug delivery, tissue engineering, tissue adhesives, adhesion prevention, bone wax formulations, medical device coatings, stents, stent coatings, highly porous foams, reticulated foams, wound care, cardiovascular applications, orthopedic devices, surface modifying agents and other implantable medical devices. In addition, these absorbable polymers should have a controlled degradation profile.
    Type: Application
    Filed: May 3, 2013
    Publication date: September 19, 2013
    Applicant: BEZWADA BIOMEDICAL, LLC.
    Inventor: Rao S. BEZWADA
  • fD
    Publication number: 20130238118
    Abstract: The invention disclosed herein relates to methods and means for allocating, allotting, apportioning, dispensing, distributing, preparing, portioning, meting out and/or otherwise providing, controlling and/or regulating access to quantities of foods, beverages, and/or other substances. Various embodiments of the methods and means of the invention may be performed by and/or implemented in hardware, in software, by one or more entities, and/or by some combination of hardware, software and/or one or more entities.
    Type: Application
    Filed: January 30, 2013
    Publication date: September 12, 2013
    Inventor: Alfred M. Haas
  • 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
  • Patent number: 8487109
    Abstract: The present invention relates to a process for the regioselective synthesis of compounds of the formula (I), wherein R1; R2; R3; R4; R5; J and W have the meanings indicated in the claims. The present invention provides an efficient and general palladium-catalyzed coupling process for aryl tosylates with terminal alkynes to a wide variety of substituted, multifunctional aryl-1-alkynes of the formula I.
    Type: Grant
    Filed: December 23, 2009
    Date of Patent: July 16, 2013
    Assignee: Sanofi
    Inventors: Omar Rkyek, Marc Nazare, Andreas Lindenschmidt, Matthias Urmann, Nis Halland, Jorge Alonso
  • Patent number: 8466081
    Abstract: Disclosed are halogenated amide esters that are suitable as internal electron donors in procatalyst compositions. Ziegler-Natta catalyst compositions containing the present procatalyst compositions exhibit improved catalyst activity and/or improved catalyst selectivity and produce propylene-based olefins with broad molecular weight distribution.
    Type: Grant
    Filed: February 24, 2011
    Date of Patent: June 18, 2013
    Assignee: Dow Global Technologies LLC
    Inventors: Linfeng Chen, Tak W. Leung, Tao Tao, Kuanqiang Gao, James X. Shu
  • Patent number: 8461372
    Abstract: The present invention relates to the discovery of new class of hydrolysable amino acid derivatives and absorbable polyester amides, polyamides, polyepoxides, polyureas and polyurethanes prepared therefrom. The resultant absorbable polymers are useful for drug delivery, tissue engineering, tissue adhesives, adhesion prevention, bone wax formulations, medical device coatings, stents, stent coatings, highly porous foams, reticulated foams, wound care, cardiovascular applications, orthopedic devices, surface modifying agents and other implantable medical devices. In addition, these absorbable polymers should have a controlled degradation profile.
    Type: Grant
    Filed: January 25, 2012
    Date of Patent: June 11, 2013
    Inventor: Rao S. Bezwada
  • Publication number: 20130109880
    Abstract: The present invention relates to novel phenyl-N-acyl derivatives of biogenic amines and amino acids of general formula (I) as cyclooxynease inhibitors, possessing analgetic and anti-inflammatory properties and devoid of side effects in particular ulcerogeneity and pro-spasmodic actions, as well as capability to potentiate effect of other analgetics, and possessing in addition antihypoxic, antidepressant and anti-Parkinsonistic action; as well as to the processes for the preparation novel and known phenyl-N-acyl derivatives of biogenic amines, to a pharmaceutical composition and to an agent comprising compounds of general formula (I) as well as to use thereof and a method of treating.
    Type: Application
    Filed: November 12, 2012
    Publication date: May 2, 2013
    Applicant: Obschestvo S Ogranichennoi Otvetstvennostiyu Pharmenterprises
    Inventor: Obschestvo S Ogranichennoi Otvetstvennostiyu
  • Patent number: 8415501
    Abstract: The present invention is directed to methods and compositions for making and using a new polymorph of cinacalcet hydrochloride.
    Type: Grant
    Filed: March 22, 2007
    Date of Patent: April 9, 2013
    Assignee: Amgen, Inc.
    Inventors: Belle B. Liu, Pengzu Zhou, Nina Cauchon
  • Publication number: 20130072519
    Abstract: Compounds of Formula I that inhibit microsomal triglyceride transfer protein (MTP) and/or apolipoprotein B (Apo B) secretion and their uses in the treatment of diseases linked thereto in animals are described herein.
    Type: Application
    Filed: May 9, 2011
    Publication date: March 21, 2013
    Inventors: Edward Lee Conn, David Hepworth, Yingmei Qi, Benjamin Neil Rocke, Roger Benjamin Ruggeri, Yan Zhang
  • Patent number: 8394853
    Abstract: The present invention provides a compound of formula I?; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R5, B1, X and n are defined herein. The invention also relates 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: Grant
    Filed: May 27, 2010
    Date of Patent: March 12, 2013
    Assignee: Novartis AG
    Inventors: Gary Mark Coppola, Yuki Iwaki, Rajeshri Ganesh Karki, Toshio Kawanami, Gary Michael Ksander, Muneto Mogi, Robert Sun
  • Publication number: 20130059998
    Abstract: Amino acid-based poly(ester amide) (PEA) macromers (e.g., functional PEA macromers) and methods for preparing amino acid-based poly(ester amide) (PEA) macromers. The functional PEA macromers can comprise functional groups such as hydroxyl, amine, sulfonic acids, carboxyl, thiol and acryloyl at the two terminuses of the PEA macromers. The content of the terminal functional groups on the macromers can be precisely controlled by adjusting the molar ratio of reactive monomers. The resulting versatility of these new functional PEA macromers can be used to fabricate a wide range of PEAs and PEA hybrid derivatives with very different chemical, physical, mechanical, thermal and biological properties. The functional PEA macromers can also be polycondensed into forming block PEA polymers.
    Type: Application
    Filed: March 9, 2011
    Publication date: March 7, 2013
    Inventors: Chih-Chang Chu, Mingxiao Deng
  • Publication number: 20130030059
    Abstract: The invention relates to compounds that specifically bind a T1R1/T1R3 or T1R2/T1R3 receptor or fragments or sub-units thereof. The present invention also relates to the use of hetero-oligomeric and chimeric taste receptors comprising T1R1/T1R3 and T1R2/T1R3 in assays to identify compounds that respectively respond to umami taste stimuli and sweet taste stimuli. Further, the invention relates to the constitutive of cell lines that stably or transiently co-express a combination of T11 and T1R3; or T1R2 and T1R3; under constitutive or inducible conditions. The use of these cells lines in cell-based assays to identify umami and sweet taste modulatory compounds is also provided, particularly high throughput screening assays that detect receptor activity by use of fluorometric imaging.
    Type: Application
    Filed: March 12, 2012
    Publication date: January 31, 2013
    Inventors: Xiaodong Li, Lena Staszewski, Hong Xu
  • Publication number: 20130030210
    Abstract: The invention provides novel compounds and methods to carry out organocatalytic Michael additions of aldehydes to nitroethylene catalyzed by a proline derivative to provide ?-substituted-?-nitroaldehydes. The reaction can be rendered enantioselective when a chiral pyrrolidine catalyst is used, allowing for Michael adducts in nearly optically pure form (e.g., 96-99% e.e.). The Michael adducts can bear a single substituent or dual substituents adjacent to the carbonyl. The Michael adducts can be efficiently converted to protected ?2-amino acids, which are essential for systematic conformational studies of ?-peptide foldamers.
    Type: Application
    Filed: September 17, 2012
    Publication date: January 31, 2013
    Applicant: WISCONSIN ALUMNI RESEARCH FOUNDATION
    Inventors: Samuel Helmer GELLMAN, Yonggui CHI, Li GUO
  • Publication number: 20130023645
    Abstract: The present invention related to methods for forming dicarba bridges in organic compounds. This involves the use of a pair of complementary metathesisable groups on the organic compound, and subjecting the compound to cross-metathesis under microwave radiation conditions. In an alternative, the compounds containing a turn-induced group between the pair of cross metathesisable groups to facilitate the cross-metathesis.
    Type: Application
    Filed: April 23, 2012
    Publication date: January 24, 2013
    Inventors: Andrea Jane Robinson, William Roy Jackson, Jim Patel, Jomana Elaridi