Nitrogen Attached Indirectly To The Hetero Ring By Nonionic Bonding Patents (Class 549/451)
  • Patent number: 10017602
    Abstract: The present invention provides, among others, compounds of the following formula which can be used as degradable curing agents, methods for preparing the compounds, degradable polymers and reinforced composites, methods for degrading and recycling the polymers and composites.
    Type: Grant
    Filed: April 18, 2014
    Date of Patent: July 10, 2018
    Assignee: ADESSO AVANCED MATERIALS WUHU CO., LTD.
    Inventors: Bing Qin, Xin Li, Bo Liang
  • 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: 20150105559
    Abstract: Disclosed is a method for producing a compound having an amino group and/or a hydroxyl group from a substrate compound having an atomic group containing CO or CS by eliminating such atomic group. The substrate compound, having an atomic group containing CO or CS (for example, an amide, a carbamate, or the like), is allowed to react with a compound expressed by formula (I) below, at a temperature of 120° C. or lower, preferably in the presence of an ammonium salt, to eliminate such atomic group containing CO or CS. In formula (I) A may not be present, and in a case where A is present, A represents an alkyl group having 1 to 6 carbon atoms. H2N-A—NH2 (I) - - -.
    Type: Application
    Filed: March 4, 2013
    Publication date: April 16, 2015
    Applicant: Kyushu University, National University Corporation
    Inventors: Takashi Ohshima, Hiroyuki Morimoto, Yuhei Shimizu
  • Patent number: 8957097
    Abstract: The present invention is directed to hemi phorboxazole A: and its stereoisomers, as well as derivatives of hemi phorboxazole A of formula I: wherein ring A is aryl or a 5- or 6-membered heteroaryl optionally substituted with one or more of halogen, —OH, or —C1-6alkyl; and R is —CN, a 5- or 6-membered heteroaryl, or halogen; and the pharmaceutically acceptable salt forms thereof, in addition to methods of using these compounds.
    Type: Grant
    Filed: July 23, 2010
    Date of Patent: February 17, 2015
    Assignees: The Trustees Of The University Of Pennsylvania, The Regents Of The University Of California
    Inventors: Amos B. Smith, III, Zhuqing Liu, Anne-Marie L. Hogan, Doralyn S. Dalisay, Tadeusz F. Molinski
  • Patent number: 8952179
    Abstract: Industrial synthesis process for the compound of formula (I):
    Type: Grant
    Filed: December 11, 2013
    Date of Patent: February 10, 2015
    Assignee: Les Laboratories Servier
    Inventors: Nicolas Robert, Jean-Michel Lerestif, Jean-Pierre Lecouve, Marina Gaillard, Loic Meunier, Philippe Letellier, Mathieu Boiret
  • 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: 20140235872
    Abstract: The instant invention provides for novel cationic lipids that can be used in combination with other lipid components such as cholesterol and PEG-lipids to form lipid nanoparticles with oligonucleotides. It is an object of the instant invention to provide a cationic lipid scaffold that demonstrates enhanced efficacy along with lower liver toxicity as a result of lower lipid levels in the liver. The present invention employs low molecular weight cationic lipids with one short lipid chain to enhance the efficiency and tolerability of in vivo delivery of siRNA.
    Type: Application
    Filed: April 29, 2014
    Publication date: August 21, 2014
    Applicant: SIRNA THERAPEUTICS, INC.
    Inventors: Brian W. BUDZIK, Steven L. COLLETTI, Jennifer R. DAVIS, Ivory D. HILLS, Darla Danile SEIFRIED, Matthew G. STANTON
  • Patent number: 8785451
    Abstract: Disclosed are compounds of formula (IA), formula (IV) or formula (V), wherein the variables are as defined herein, and pharmaceutical compositions containing them which are useful for treating a subject with a proliferative disorder, such as cancer. The disclosed compounds and pharmaceutical compositions are also useful for treating disorders responsive to Hsp70 induction and/or natural killer induction.
    Type: Grant
    Filed: August 20, 2007
    Date of Patent: July 22, 2014
    Assignee: Synta Pharmaceuticals Corp.
    Inventors: Keizo Koya, Lijun Sun, Shoujun Chen, Jun Jiang
  • Publication number: 20140150380
    Abstract: Disclosed are compounds of formula (1) and (2) and/or E/E-, E/Z- or Z/Z geometrical isomer forms thereof; wherein R1-R5, R1-R11 and A are defined as in description. The compounds are used as UV absorbers for protecting household products from photolytic and oxidative degradation, as plastic additives, preferably for food and pharmaceutical packaging applications, for preventing photo-degradation of food by incorporation of the compounds of formula (1?) and/or (2?) into transparent food containers, for protection of UV-A sensitive drugs from photo-degradation by incorporation of UV absorber in transparent blister foils or transparent pharmacy containers, as additives for photographic and printing applications, as additives for electronic applications and protecting the ingredients in agriculture applications.
    Type: Application
    Filed: July 19, 2012
    Publication date: June 5, 2014
    Inventors: Barbara Winkler, Dietmar Hueglin, Kai Eichin, Larissa Ehrsam, Xavier Marat, Hervé Richard, ILona Marion Kienzle, Ute Schroeder
  • Publication number: 20140138661
    Abstract: The present invention relates to crosslinkable compounds, to the crosslinked compounds obtained from these compounds, and to processes for the preparation thereof. The invention is furthermore directed to the use of these compounds in electronic devices and to the corresponding electronic devices themselves.
    Type: Application
    Filed: June 29, 2012
    Publication date: May 22, 2014
    Applicant: MERCK PATENT GmbH
    Inventors: Aurélie Ludemann, Alice Julliart, Anna Hayer, Anja Gerhard, Dominik Joosten, Holger Heil, Fabrice Eckes
  • Publication number: 20140094616
    Abstract: Compound (1) or a salt that is useful as an intermediate for the production of a medicine, an agrochemical or the like can be produced by a process including the following steps: (A) reacting an aldehyde (2) with nitromethane to produce a nitroaldehyde; (B) reacting the nitroaldehyde with an alcohol to produce a nitroacetal; (C) reducing the nitroacetal to produce an aminoacetal; (D) protecting an amino group in the aminoacetal to produce a protected aminoacetal; (E) treating the protected aminoacetal with an acid and subsequently with a base and then reacting the resultant product with a cyanating agent to produce a nitrile; (F) hydrolyzing the nitrile to produce a protected amino acid; and (G) substituting a group R5 in the protected amino acid by a hydrogen atom and protecting a carboxyl group therein.
    Type: Application
    Filed: May 17, 2012
    Publication date: April 3, 2014
    Applicant: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventors: Tetsuya Ikemoto, Leopold Mpaka Lutete, Toshiaki Aikawa
  • Publication number: 20140066408
    Abstract: This invention provides, but is not limited to, novel oleanolic acid derivatives having the formula: wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds, methods and intermediates useful for making the compounds, and methods of using the compounds and compositions.
    Type: Application
    Filed: January 14, 2013
    Publication date: March 6, 2014
    Applicant: REATA PHARMACEUTICALS, INC.
    Inventor: REATA PHARMACEUTICALS, INC.
  • Publication number: 20130338210
    Abstract: A method for delivering a nucleic acid to a cell can include exposing sample cells to a composition which includes charged lipids.
    Type: Application
    Filed: December 7, 2010
    Publication date: December 19, 2013
    Applicant: ALNYLAM PHARMACEUTICALS, INC.
    Inventors: Muthiah Manoharan, Khallanthottathil G. Rajeev, Muthusamy Jayaraman, David Butler, Mamta Kapoor, Rajesh Kumar Kainthan
  • Publication number: 20130261320
    Abstract: The present invention relates to the preparation of (R)—N-(3,4-difluoro-2-(2-fluoro-4-iodophenylamino)-6-methoxyphenyl)-1-(2,3-dihydroxypropyl)cyclopropane-1-sulfonamide and (S)—N-(3,4-difluoro-2-(2-fluoro-4-iodophenylamino)-6-methoxyphenyl)-1-(2,3-dihydroxypropyl)cyclopropane-1-sulfonamide.
    Type: Application
    Filed: April 23, 2013
    Publication date: October 3, 2013
    Applicant: ARDEA BIOSCIENCES, INC.
    Inventors: Andreas MADERNA, Jean Michel VERNIER
  • Publication number: 20130211103
    Abstract: Disclosed herein are methods and intermediates useful in the preparation of macrolides, e.g., compounds of formula (IV) wherein R1-R12 are as defined herein.
    Type: Application
    Filed: January 3, 2013
    Publication date: August 15, 2013
    Applicant: EISAI R&D MANAGEMENT CO., LTD.
    Inventor: EISAI R&D MANAGEMENT CO., LTD.
  • Publication number: 20120309819
    Abstract: The present application discloses an acid labile lipophilic molecular conjugate of cancer chemotherapeutic agents and methods for reducing or substantially eliminating the side effects of chemotherapy associated with the administration of a cancer chemotherapeutic agent to a patient in need thereof.
    Type: Application
    Filed: June 5, 2012
    Publication date: December 6, 2012
    Inventors: James D. McChesney, John T. Henri, Sylesh Kumar Venkataraman, Mahesh Kumar Gundluru
  • Publication number: 20120283450
    Abstract: This invention provides novel compounds comprising the following anti-inflammatory pharmacore: wherein X, R1 and R2 are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds, methods and intermediates useful for making the compounds, and methods of using the compounds and compositions.
    Type: Application
    Filed: July 18, 2012
    Publication date: November 8, 2012
    Inventors: Eric Anderson, Gary L. Bolton, Deborah A. Ferguson, Xin Jiang, Robert M. Kral, JR., Patrick M. O'Brien, Melean Visnick
  • Publication number: 20120208996
    Abstract: Process for the synthesis of ivabradine of formula (I): and addition salts thereof with a pharmaceutically acceptable acid.
    Type: Application
    Filed: February 9, 2012
    Publication date: August 16, 2012
    Applicant: LES LABORATOIRES SERVIER
    Inventors: Jean-Louis PEGLION, Aimée DESSINGES
  • Publication number: 20120178946
    Abstract: The present invention relates to the preparation of (R)-N-(3,4-difluoro-2-(2-fluoro-4-iodophenylamino)-6-methoxyphenyl)-1-(2,3-dihydroxypropyl)cyclopropane-1-sulfonamide and (S)-N-(3,4-difluoro-2-(2-fluoro-4-iodophenylamino)-6-methoxyphenyl)-1-(2,3-dihydroxypropyl)cyclopropane-1-sulfonamide.
    Type: Application
    Filed: July 10, 2010
    Publication date: July 12, 2012
    Applicant: ARDEA BIOSCIENCES ,INC.
    Inventors: Andreas Maderna, Jean-Michel Vernier
  • Publication number: 20120130092
    Abstract: It is possible to produce oseltamivir safely and stably in large quantities by using as a starting material tartaric acid, mannitol or arabinose, via dihydroxyhexenoic acid ester of the formula (4c).
    Type: Application
    Filed: December 6, 2011
    Publication date: May 24, 2012
    Inventors: Teruhiko Ishikawa, Seiki Saito, Takayuki Kudoh, Kotaro Suto, Hironori Nishiuchi, Makoto Okada, Masatoshi Taniguchi
  • Publication number: 20120115862
    Abstract: The present invention relates to compounds of the formula I wherein R1, R2, R3, R4, X and Y have the meanings given in the description. The compounds have an action which is immunomodulating and inhibits or regulates the release of IL-1? and/or TNF-?. They can therefore be used for treatment of diseases connected with a disturbance in the immune system.
    Type: Application
    Filed: October 9, 2009
    Publication date: May 10, 2012
    Inventors: Stefan Laufer, Wolfgang Albrecht
  • Publication number: 20120058144
    Abstract: The present invention provides lipids that are advantageously used in lipid particles for the in vivo delivery of therapeutic agents to cells. In particular, the invention provides lipids having the following structures XIV or XVII.
    Type: Application
    Filed: November 10, 2009
    Publication date: March 8, 2012
    Applicant: ALNYLAM PHARMACEUTICALS, INC.
    Inventors: Muthiah Manoharan, Kallanthottathil G. Rajeev, Muthusamy Jayaraman, David Butler, Jayaprakash K. Narayanannair, Marco A. Ciufolini
  • Publication number: 20120027796
    Abstract: The present invention provides lipids that are advantageously used in lipid particles for the in vivo delivery of therapeutic agents to cells. In particular, the invention provides lipids having the following structures: (Formula (I) or (XXXV)).
    Type: Application
    Filed: November 10, 2009
    Publication date: February 2, 2012
    Applicant: ALNYLAM PHARMACEUTICALS, INC.
    Inventors: Muthiah Manoharan, Kallanthottathil G. Rajeev, David Butler, Jayaprakash K. Narayanannair, Muthusamy Jayaraman, Laxmab Eltepu
  • Publication number: 20110294830
    Abstract: The present invention provides a nitrogen-containing compound represented by formula (I1) (in formula (I1), R0 represents a nitro group or the like, Z represents an optionally substituted aryl group or the like, R3 represents a hydrogen atom or the like, Y represents a nitro group or the like, n represents an integer of 0 to 3, D represents an optionally substituted 5-membered to 8-membered hydrocarbon ring group or heterocyclic group having or not having a substituent other than substituent X, X represents a group represented by formula (II-1) (in formula (II-1), R1 and R2 respectively and independently represent a hydrogen atom or the like), A represents a carbon atom or the like, n1 represents an integer of 0 to 2) or a salt thereof, and an insecticide, miticide, sanitary insect pest control agent, or harmful organism control agent including as an active ingredient thereof the nitrogen-containing compound or the salt thereof.
    Type: Application
    Filed: February 5, 2010
    Publication date: December 1, 2011
    Applicant: Nippon Soda Co., Ltd.
    Inventors: Jyun Iwata, Masahiro Kawaguchi, Akiko Mizui
  • Publication number: 20110263879
    Abstract: A zwitterionic phosphonium salt of Formula I: wherein n is 0 or 1; R is H or SO3; R? is selected from the group consisting of C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, C3-C10 cycloalkyl, phenyl, substituted phenyl, benzyl and C1-C10 alkoxy-carbonyl; R? is CX3 when n is O; and X is selected from the group consisting of F, Cl, Br and I. The zwitterionic phosphonium salts are useful reagents for the preparation of alkenes and acetals from the corresponding aldehyde.
    Type: Application
    Filed: July 29, 2009
    Publication date: October 27, 2011
    Applicant: THE HONG KONG POLYTECHNIC UNIVERSITY
    Inventors: Tak-Hang Chan, Congde Huo, Xun He
  • Publication number: 20110256175
    Abstract: The present invention provides superior compositions and methods for the delivery of therapeutic agents to cells. In particular, these include novel lipids and nucleic acid-lipid particles that provide efficient encapsulation of nucleic acids and efficient delivery of the encapsulated nucleic acid to cells in vivo. The compositions of the present invention are highly potent, thereby allowing effective knock-down of specific target proteins at relatively low doses. In addition, the compositions and methods of the present invention are less toxic and provide a greater therapeutic index compared to compositions and methods previously known in the art.
    Type: Application
    Filed: October 9, 2009
    Publication date: October 20, 2011
    Applicants: THE UNIVERSITY OF BRITISH COLUMBIA, TEKMIRA PHARMACEUTICALS CORPORATION
    Inventors: Michael J. Hope, Sean C. Semple, Jianxin Chen, Thomas D. Madden, Pieter R. Cullis, Marco A. Ciufolini, Barbara Low Shoud Mui
  • Publication number: 20110223105
    Abstract: There is provided a compound of Formula and salts thereof wherein R1 is an imine or an alkylated imine, said imine or alkylated imine comprising a linear or branched alkyl group of length C1 to C5; R2 are each independently (a) an unsubstituted or substituted linear or branched alkyl group of chain length C1-7; (b) an aryl substituted alkyl group, wherein said aryl group is substituted, (c) an alkoxy substituted alkyl group, wherein said alkoxy group is substituted by a methoxy group or an alkoxy group substituted with an alkoxy group; or (d) an H atom; wherein said substituents in (a) and (b) are selected from hydroxy, alkoxy, acyloxy, alkoxycarbonyloxy, amino, aryl, nitro, oxo and fluoro groups. R3 and R4 are linear or branched alkyl groups of length C1 to C6 constituting a ketal or a cyclic ketal. The compounds claimed may be used for the manufacture of a medicament.
    Type: Application
    Filed: September 1, 2009
    Publication date: September 15, 2011
    Inventors: Leif A. Eriksson, Lennart Löfgren
  • Publication number: 20110117125
    Abstract: The present invention provides compositions and methods for the delivery of therapeutic agents to cells. In particular, these include novel lipids and nucleic acid-lipid particles that provide efficient encapsulation of nucleic acids and efficient delivery of the encapsulated nucleic acid to cells in vivo. The compositions of the present invention are highly potent, thereby allowing effective knock-down of specific target protein at relatively low doses. In addition, the compositions and methods of the present invention are less toxic and provide a greater therapeutic index compared to compositions and methods previously known in the art.
    Type: Application
    Filed: December 31, 2008
    Publication date: May 19, 2011
    Applicants: TEKMIRA PHARMACEUTICALS CORPORATION, THE UNIVERSITY OF BRITISH COLUMBIA, ALNYLAM PHARMACEUTICALS
    Inventors: Michael J. Hope, Sean C. Semple, Jianxin Chen, Thomas D. Madden, Barbara Mui, Pieter R. Cullis, Marco A. Ciufolini, Kim F. Wong, Muthiah Manoharan, Rajeev G. Kallanthottathil
  • Publication number: 20110102528
    Abstract: An embodiment of the composition contains any of compounds of the formula A-LG in which A represents any of residues of general formula (A-1) below and LG represents any of groups that are cleaved to generate acids of the formula A-H when acted on by an acid. The composition further contains at least one of a compound that generates an acid when exposed to actinic rays or radiation and a compound that generates an acid when heated.
    Type: Application
    Filed: October 28, 2010
    Publication date: May 5, 2011
    Applicant: FUJIFILM Corporation
    Inventors: Tomotaka TSUCHIMURA, Takeshi Kawabata, Takayuki Ito
  • Patent number: 7932252
    Abstract: The present invention relates to compounds that modulate various chemokine receptors. These compounds are useful for treating inflammatory and immune diseases.
    Type: Grant
    Filed: May 12, 2005
    Date of Patent: April 26, 2011
    Assignee: ChemoCentryx, Inc.
    Inventors: Solomon Ungashe, John Jessen Wright, Andrew Pennell
  • Publication number: 20100280252
    Abstract: The present invention provides bifunctional polymers, methods of preparing the same, and intermediates thereto. These compounds are useful in a variety of applications including the PEGylation of biologically active molecules. The invention also provides methods of using said compounds and compositions thereof.
    Type: Application
    Filed: February 17, 2010
    Publication date: November 4, 2010
    Applicant: Intezyne Technologies
    Inventors: Kurt Breitenkamp, Kevin N. Sill, Habib Skaff
  • Patent number: 7825126
    Abstract: Disclosed are (N)-methanocarba adenine nucleosides of the formula: as highly potent A3 adenosine receptor agonists, pharmaceutical compositions comprising such nucleosides, and a method of use of these nucleosides, wherein R1-R6 are as defined in the specification. These nucleosides are contemplated for use in the treatment a number of diseases, for example, inflammation, cardiac ischemia, stroke, asthma, diabetes, and cardiac arrhythmias. The invention also provides compounds that are agonists of both A1 and A3 adenosine receptors for use in cardioprotection.
    Type: Grant
    Filed: September 2, 2005
    Date of Patent: November 2, 2010
    Assignee: The United States of America as represented by the Department of Health and Human Services
    Inventors: Kenneth A. Jacobson, Bhalchandra V. Joshi, Susanna Tchilibon
  • Publication number: 20100267946
    Abstract: The present invention provides prodrugs of GABA analogs, pharmaceutical compositions of prodrugs of GABA analogs and methods for making prodrugs of GABA analogs. The present invention also provides methods for using prodrugs of GABA analogs and methods for using pharmaceutical compositions of prodrugs of GABA analogs for treating or preventing common diseases and/or disorders.
    Type: Application
    Filed: July 1, 2010
    Publication date: October 21, 2010
    Applicant: XenoPort, Inc.
    Inventors: Mark A. Gallop, Kenneth C. Cundy, Cindy X. Zhou, Fayang G. Qiu, Fenmei Yao, Jia-Ning Xiang, Ian R. Ollmann
  • Publication number: 20100104629
    Abstract: Cationic lipids, cationic lipid based drug delivery systems, ways to make them and methods of treating diseases using them are disclosed.
    Type: Application
    Filed: September 10, 2009
    Publication date: April 29, 2010
    Applicant: ABBOTT LABORATORIES
    Inventors: Prasad A. Dande, Todd M. Hansen, Robert D. Hubbard, Aparna V. Sarthy, Yu Shen, Lu Tian, Carol K. Wada, Xiaobin Zhao
  • Patent number: 7655649
    Abstract: The present invention is directed to compounds which contain substituted pyridazines and pyrimidines moieties which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for treating cancer comprising administration of the compounds of the invention.
    Type: Grant
    Filed: April 5, 2005
    Date of Patent: February 2, 2010
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Mark T. Bilodeau, Peter C. Chua, Nicholas D. P. Cosford, Jacob M. Hoffman, Johnny Yasuo Nagasawa
  • Publication number: 20090263407
    Abstract: Cationic lipids, cationic lipid based drug delivery systems, ways to make them and methods of treating diseases using them are disclosed.
    Type: Application
    Filed: April 16, 2009
    Publication date: October 22, 2009
    Applicant: ABBOTT LABORATORIES
    Inventors: Prasad A. Dande, Todd M. Hansen, Robert D. Hubbard, Carol K. Wada, Lu Tian, Xiaobin Zhao
  • Patent number: 7547716
    Abstract: A medicament for enhancing an effect of a cancer therapy based on a mode of action of DNA injury, which comprises as an active ingredient a compound represented by the general formula (I) or a physiologically acceptable salt thereof: wherein R represents an aryl-substituted alkyl group, an heteroaryl-substituted alkyl group, a cycloalkyl-substituted alkyl group, or a cyclic hydrocarbon group wherein said cyclic hydrocarbon group may be saturated, partly saturated, or aromatic; or Z may bind to R to form a cyclic structure, Z represents a hydrogen atom or a C1 to C6 alkyl group. The medicament enhanced the effect of the cancer therapy and decreases a dose of an anticancer agent and/or radiation, and therefore, can reduce side effects resulting from the cancer therapy.
    Type: Grant
    Filed: June 7, 2002
    Date of Patent: June 16, 2009
    Assignee: Institute of Medicinal Molecular Design, Inc.
    Inventors: Susumu Muto, Masayuki Komukai, Akiko Itai
  • Publication number: 20080275098
    Abstract: The present invention comprises novel substituted 2-aminoimidazoles of formula I, processes for their preparation, pharmaceutical compositions thereof, and methods for their use in the treatment of disorders of the central nervous system, cardiovascular disorders, stroke and pulmonary disorders, urinary disorders such as acute or chronic renal failure, disorders of biliary function, respiratory disorders such as snoring or sleep apnea. wherein the substitutents R1-R8 are further defined herein.
    Type: Application
    Filed: July 14, 2008
    Publication date: November 6, 2008
    Applicant: SANOFI-AVENTIS DEUTSCHLAND GMBH
    Inventors: Uwe HEINELT, Hans-Jochen LANG, Armin HOFMEISTER, Klaus WIRTH, Hans-Willi JANSEN
  • Publication number: 20080268518
    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: October 26, 2007
    Publication date: October 30, 2008
    Applicant: AMBRX, INC.
    Inventors: Zhenwei MIAO, Junjie LIU, Thea NORMAN, Russell DRIVER
  • Publication number: 20080268519
    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: October 26, 2007
    Publication date: October 30, 2008
    Applicant: AMBRX, INC.
    Inventors: Zhenwei MIAO, Junjie LIU, Thea NORMAN, Russell DRIVER
  • Publication number: 20080182968
    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: October 17, 2007
    Publication date: July 31, 2008
    Applicant: AMBRX, INC.
    Inventors: Zhenwei MIAO, Junjie LIU, Thea NORMAN, Russell DRIVER
  • Patent number: 7273856
    Abstract: Described herein are compounds of formula (I) useful as antagonists of tachykinins in general, and in particular of neurokinin A; and the pharmaceutical formulations comprising the compounds of formula (I)
    Type: Grant
    Filed: October 28, 2002
    Date of Patent: September 25, 2007
    Assignee: Menarini Ricerche S.P.A.
    Inventors: Alessandro Sisto, Valerio Caciagli, Maria Altamura, Alessandro Giolitti, Valentina Fedi, Antonio Guidi, Danilo Giannotti, Nicholas Harmat, Rossano Nannicini, Franco Pasqui, Carlo Alberto Maggi
  • Patent number: 7205320
    Abstract: PDE4 inhibition is achieved by novel compounds, e.g., N-substituted aniline and diphenylamine analogs. The compounds of the present invention are of Formula I: wherein R1, R2, R3 and R4 are as defined herein.
    Type: Grant
    Filed: January 12, 2004
    Date of Patent: April 17, 2007
    Assignee: Memory Pharmaceuticals Corp.
    Inventors: Richard A. Schumacher, William F. Brubaker, Michael De Vivo, Hans-Jürgen Ernst Hess, Allen Hopper, Ashok Tehim, Ruiping Liu, Axel Unterbeck
  • Patent number: 7041345
    Abstract: The invention relates to chiral compounds of formula (I) wherein Y1, Y2, Y3, Y4, X1, X2, X3 and X4 have the meaning given in claim 1, to liquid crystalline mixtures comprising at least one chiral compound of formula (I), to chiral linear or crosslinked liquid crystalline polymers obtainable by polymerizing a polymerizable mixture comprising at least one chiral compound of formula (I), to the use of chiral compounds of formula (I) and mixtures and polymers obtained thereof in liquid crystal displays, active and passive optical elements, adhesives, synthetic resins with anisotropic mechanical properties, cosmetic and pharmaceutical compositions, diagnostics, liquid crystal pigments, for decorative and security applications, nonlinear optics, optical information storage or as chiral dopants, and to a liquid crystal display comprising a mixture comprising at least one chiral compound of formula (I)
    Type: Grant
    Filed: June 25, 2001
    Date of Patent: May 9, 2006
    Assignee: Merck Patent GmbH
    Inventors: Peer Kirsch, Andreas Tangerbeck, Detlef Pauluth, Joachim Krause, Michael Heckmeier, Kazuaki Tarumi
  • Patent number: 7034015
    Abstract: The invention relates to a novel class of aminobenzophenones derivatives, to pharmaceutical preparations comprising said compounds, to dosage units of such preparations, to methods of treating patients comprising administering said compounds, and to the use of said compounds in the manufacture of pharmaceutical preparations.
    Type: Grant
    Filed: August 28, 2002
    Date of Patent: April 25, 2006
    Assignee: Leo Pharma A/S
    Inventors: Erik Rytter Ottosen, Anne Marie Horneman, Xifu Liang
  • Patent number: 6936627
    Abstract: The invention describes novel nitrosated and/or nitrosylated H2 receptor antagonist compounds, and novel compositions comprising at least one H2 receptor antagonist compound that is optionally substituted with at least one NO and/or NO2 group, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase and/or at least one nonsteroidal antiinflammatory drug, antacid, bismuth-containing reagent or anti-viral agent.
    Type: Grant
    Filed: October 29, 2002
    Date of Patent: August 30, 2005
    Assignee: NitroMed, Inc.
    Inventors: David S. Garvey, L. Gordon Letts, Chia-En Lin, Tiansheng Wang
  • Patent number: 6861561
    Abstract: The invention relates to substituted aromatic polycyclic tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases.
    Type: Grant
    Filed: September 26, 2002
    Date of Patent: March 1, 2005
    Assignee: G. D. Searle & Co.
    Inventors: James A. Sikorski, Richard C. Durley, Mark A. Massa, Jane L. Wang, Deborah A. Mischke, Barry L. Parnas, Melvin L. Rueppel
  • Patent number: 6825231
    Abstract: The application discloses substituted norbornylamino derivatives, processes for their preparation, their use as medicaments or diagnostics and a medicament comprising them Substituted norbornylamino derivatives having exo-configured nitrogen and an endo-fused five-membered ring of the formula I, or having exo-configured nitrogen and an exo-fused five-membered ring of the formula I a in which R1, R2, R3, R4, R5, A, B, S1, and S2 are as defined in the claims, are highly suitable for use as antihypertensive agents, for reducing or preventing ischemically induced damage, for use as medicaments for surgical interventions for the treatment of ischemias of the nervous system, of stroke and cerebral edema, of shock, of impaired respiratory drive, for the treatment of snoring, as laxatives, as agents against ectoparasites, for the prevention of the formation of biliary calculus, as antiatherosclerotics, as agents against late diabetic complications, carcinomatous disorders, fibrotic disorders, endot
    Type: Grant
    Filed: December 12, 2000
    Date of Patent: November 30, 2004
    Assignee: Aventis Pharma Deutschland GmbH
    Inventors: Uwe Heinelt, Hans-Jochen Lang, Heinz-Werner Kleemann, Jan-Robert Schwark, Klaus Wirth, Hans-Willi Jansen
  • Publication number: 20040192954
    Abstract: The compound O-(2-[18F]fluoroethyl)-L-tyrosine has proven to be particularly suitable for positron emission tomography and has already been tested in clinical practice. Until now, the compound has been prepared according to a relatively laborious method (Wester H. J. et al., J. Nucl. Med. 1999; 40: 205-212).
    Type: Application
    Filed: May 24, 2004
    Publication date: September 30, 2004
    Inventor: Kurt Hamacher
  • Patent number: 6649652
    Abstract: A methods of treating an infection comprises administering a therapeutically effective amount of a compound described by the Formula (I)
    Type: Grant
    Filed: July 30, 2002
    Date of Patent: November 18, 2003
    Assignees: The University of North Carolina at Chapel Hill, Georgia State University Research Foundation, Inc.
    Inventors: David W. Boykin, M. Syed Rahmathullah, Richard R. Tidwell, James E. Hall