Chalcogen Double Bonded Directly To A Ring Carbon Of The Hetero Ring Which Is Adjacent To The Ring Nitrogen (e.g., Laurolactam, Etc.) Patents (Class 540/451)
  • Patent number: 9624176
    Abstract: A method for preparing caprolactam by using a microreactor under Lewis acid catalysis, wherein a hydroxyl group in a cyclohexanone oxime is activated to obtain a cyclohexanone oxime sulfonates intermediate, then rearranged under Lewis acid catalysis to prepare the caprolactam. The method of this invention has a simple process and a high operation safety and selectivity, the reaction condition is mild, an efficient reaction can take place even at room temperature, the reaction time is short, the conversion of the cyclohexanone oxime can reach 100% within a short time, the selectivity of the caprolactam can reach 99%, the energy consumption is greatly reduced in the premise of maintaining a high yield, and the production cost is reduced, being an efficient and green and environmentally friendly method of for synthesizing the caprolactam.
    Type: Grant
    Filed: June 24, 2016
    Date of Patent: April 18, 2017
    Assignee: NANJING TECH UNIVERSITY
    Inventors: Kai Guo, Xin Li, Zheng Fang, Kai Zhang, Qi Yu, Pingkai Ouyang
  • Patent number: 8927569
    Abstract: A class of macrocyclic compounds of formula (I), wherein R1, R3, R4, Ra, Rb, A, Z, Y, X, M, W, n and m are defined herein, that are useful as inhibitors of viral proteases, particularly the hepatitis C virus (HCV) NS3 protease, are provided. Also provided are processes 5 for the synthesis and use of such macrocyclic compounds for treating or preventing HCV infection.
    Type: Grant
    Filed: July 17, 2008
    Date of Patent: January 6, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Steven Harper, Vincenzo Summa, Nigel J. Liverton, John A. McCauley, John W. Butcher, Marcello Di Filippo, Maria Emilia Di Francesco, Marco Ferrara, Joseph J. Romano, Michael T. Rudd
  • Patent number: 8871753
    Abstract: The present invention relates to macrocyclic compounds of Formula I: or pharmaceutically acceptable salts thereof or quaternary ammonium salts thereof wherein constituent members are provided hereinwith, as well as their compositions and methods of use, which are JAK/ALK inhibitors useful in the treatment of JAK/ALK-associated diseases including, for example, inflammatory and autoimmune disorders, as well as cancer.
    Type: Grant
    Filed: April 23, 2009
    Date of Patent: October 28, 2014
    Assignee: Incyte Corporation
    Inventors: Andrew Paul Combs, Richard B. Sparks, Eddy W. Yue, Hao Feng, Michael Jason Bower, Wenyu Zhu
  • Publication number: 20140114062
    Abstract: A method for producing a high purity, high quality amide compound, particularly a lactam. An amount of each of a halide, an aldehyde compound, an alcohol compound and a nitrile compound contained in a solution recycled into an oxime-forming step is controlled to an amount of 0.4 mol % or less based on the ketone as a starting material. One or more of a ketone, an oxime and an amide compound are purified by hydrogenation and/or crystallization for eliminating impurities containing a double bond. A content of impurities having a cyclic bridge structure is controlled using a cycloalkanone purified by recrystallization.
    Type: Application
    Filed: December 27, 2013
    Publication date: April 24, 2014
    Applicant: Ube Industries, Ltd.
    Inventors: Junichi Kugimoto, Joji Kawai, Kazuo Yamato, Masahide Okada, Tsunemi Sugimoto, Hiroshi Matsumoto
  • Publication number: 20140114061
    Abstract: A method for producing a high purity, high quality amide compound, particularly a lactam. An amount of each of a halide, an aldehyde compound, an alcohol compound and a nitrile compound contained in a solution recycled into an oxime-forming step is controlled to an amount of 0.4 mol % or less based on the ketone as a starting material. One or more of a ketone, an oxime and an amide compound are purified by hydrogenation and/or crystallization for eliminating impurities containing a double bond. A content of impurities having a cyclic bridge structure is controlled using a cycloalkanone purified by recrystallization.
    Type: Application
    Filed: December 27, 2013
    Publication date: April 24, 2014
    Applicant: Ube Industries, Ltd.
    Inventors: Junichi Kugimoto, Joji Kawai, Kazuo Yamato, Masahide Okada, Tsunemi Sugimoto, Hiroshi Matsumoto
  • Patent number: 8703936
    Abstract: Provided are modified cycloalkyne compounds; and methods of use of such compounds in modifying biomolecules. Embodiments include a cycloaddition reaction that can be carried out under physiological conditions. The cycloaddition reaction involves reacting a modified cycloalkyne with an azide moiety on a target biomolecule, generating a covalently modified biomolecule. The selectivity of the reaction and its compatibility with aqueous environments provide for its application in vivo and in vitro.
    Type: Grant
    Filed: August 8, 2013
    Date of Patent: April 22, 2014
    Assignee: The Regents of the University of California
    Inventors: John C. Jewett, Carolyn R. Bertozzi, Ellen May Sletten, Chelsea G. Gordon
  • Publication number: 20140093450
    Abstract: Described is a pretargeting method, and related kits, for targeted medical imaging and/or therapeutics, wherein use is made of abiotic reactive chemical groups that exhibit bio-orthogonal reactivity towards each other. The invention involves the use of [4+2] inverse electron demand (retro) Diels-Alder chemistry in providing the coupling between a Pre-targeting Probe and an Effector Probe. To this end one of these probes comprises an electron-deficient tetrazine or other suitable diene, and the other an E-cyclooctene which has a flattened structure as a result of the position of at least two exocyclic bonds.
    Type: Application
    Filed: May 7, 2012
    Publication date: April 3, 2014
    Applicant: KONINKLIJKE PHILIPS N.V.
    Inventors: Marc Stefan Robillard, Johan Lub, Raffaella Rossin, Sandra Martina Van Ben Bosch, Ronny Mathieu Versteegen
  • Publication number: 20130261296
    Abstract: Catalytic complexes including a metal atom having anionic ligands, at least one nucleophilic carbene ligand, and an alkylidene, vinylidene, or allenylidene ligand. The complexes are highly stable to air, moisture and thermal degradation. The complexes are designed to efficiently carry out a variety of olefin metathesis reactions.
    Type: Application
    Filed: January 25, 2013
    Publication date: October 3, 2013
    Inventors: Steven P. NOLAN, Jinkun HUANG
  • Patent number: 8519122
    Abstract: Provided are modified cycloalkyne compounds; and methods of use of such compounds in modifying biomolecules. Embodiments include a cycloaddition reaction that can be carried out under physiological conditions. The cycloaddition reaction involves reacting a modified cycloalkyne with an azide moiety on a target biomolecule, generating a covalently modified biomolecule. The selectivity of the reaction and its compatibility with aqueous environments provide for its application in vivo and in vitro.
    Type: Grant
    Filed: February 10, 2011
    Date of Patent: August 27, 2013
    Assignee: The Regents of the University of California
    Inventors: John C. Jewett, Carolyn Ruth Bertozzi, Ellen May Sletten, Chelsea Gloria Gordon
  • Publication number: 20130116240
    Abstract: Provided is an agent for the treatment or prophylaxis of inflammatory diseases, allergic diseases, autoimmune diseases, transplant rejection or the like. A compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof, or a solvate thereof: wherein each symbol is as described in the specification.
    Type: Application
    Filed: September 26, 2012
    Publication date: May 9, 2013
    Applicant: JAPAN TOBACCO INC.
    Inventor: Japan Tobacco Inc.
  • Patent number: 8399658
    Abstract: A process for purifying laurolactam by means of integrated connection of distillation and crystallization is provided. The crystallization is performed as a solution or melt crystallization. The process reduces thermal stress applied to the laurolactam stream and improved yields are obtained. Raw materials are recovered and recycled in the production sequence.
    Type: Grant
    Filed: November 22, 2010
    Date of Patent: March 19, 2013
    Assignee: Evonik Degussa GmbH
    Inventors: Axel Hengstermann, Ralf Meier, Daniel Demicoli, Martin Roos, Bernd Guenzel, Frank Huebner
  • Publication number: 20120323000
    Abstract: The present invention relates generally to olefin metathesis. In some embodiments, the present invention provides methods for Z-selective ring-closing metathesis.
    Type: Application
    Filed: June 1, 2012
    Publication date: December 20, 2012
    Applicants: TRUSTEES OF BOSTON COLLEGE, MASSACHUSETTS INSTITUTE OF TECHNOLOGY
    Inventors: Amir H. Hoveyda, Miao Yu, Chenbo Wang, Richard R. Schrock
  • Patent number: 8278322
    Abstract: The present invention relates to macrocyclic compounds of formula (I) that are useful as inhibitors of the hepatitis C virus (HCV) NS3 protease, their synthesis, and their use for treating or preventing HCV infections.
    Type: Grant
    Filed: July 28, 2006
    Date of Patent: October 2, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: M. Katharine Holloway, Nigel J. Liverton, John A. McCauley, Michael T. Rudd, Joseph P. Vacca, Steven W. Ludmerer, David B. Olsen
  • Patent number: 8178520
    Abstract: The present invention relates to macrocyclic compounds of formula (I): wherein W, n, R1, Ra, Rb, R3, R4, M, Z, ring A and ring B are defined herein, and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising them, and their use for the treatment or prevention of infection by hepatitis C virus.
    Type: Grant
    Filed: May 11, 2007
    Date of Patent: May 15, 2012
    Assignee: Istituto di Ricerche di Biologia Molecolare P. Angeletti SpA
    Inventors: Maria Emilia Di Francesco, Emanuela Nizi, Paola Pace, Vincenzo Summa
  • Publication number: 20120039848
    Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
    Type: Application
    Filed: August 11, 2011
    Publication date: February 16, 2012
    Inventors: Yao-Ling Qiu, Xiaowen Peng, Ce Wang, Yat Sun Or
  • Publication number: 20110306599
    Abstract: Provided is an agent for the treatment or prophylaxis of inflammatory diseases, allergic diseases, autoimmune diseases, transplant rejection or the like. A compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof, or a solvate thereof: wherein each symbol is as described in the specification.
    Type: Application
    Filed: November 24, 2010
    Publication date: December 15, 2011
    Applicant: JAPAN TOBACCO INC.
    Inventors: Teruhiko INOUE, Tetsudo KAYA, Shinichi KIKUCHI, Koji MATSUMURA, Ritsuki MASUO, Motoya SUZUKI, Michihide MAEKAWA
  • Publication number: 20110237791
    Abstract: A 2-pyridone compound represented by the formula [1]: {wherein in the formula [1], the ring represented by A represents a benzene ring or a pyridine ring, X represents any of the structures represented by the formulas [3] shown below: V represents a single bond or a lower alkylene group, and W represents a single bond, an ether bond or a lower alkylene group (wherein the lower alkylene group may contain an ether bond)}, a tautomer or stereoisomer of the compound, a pharmaceutically acceptable salt thereof, or a solvate thereof is a compound that has an excellent GK activating effect and is useful as a pharmaceutical.
    Type: Application
    Filed: April 6, 2011
    Publication date: September 29, 2011
    Applicants: TAISHO PHARMACEUTICAL CO., LTD, NISSAN CHEMICAL INDUSTRIES, LTD.
    Inventors: Takanori KAWAGUCHI, Kengo WATATANI, Keiko FUSEGI, Masahiro BOHNO, Hajime ASANUMA, Shoichi KURODA, Yudai IMAI, Tomomichi CHONAN, Nagaaki SATO, Shigeru TOKITA, Shigetada SASAKO, Takumi OKADA, Keishi HAYASHI, Shin ITOH, Noriko SAITO, Rui JIBIKI, Seishi ISHIYAMA, Hirofumi OTA
  • Publication number: 20110224337
    Abstract: The present invention relates to a process for purifying an N-alkyllactam which comprises contacting N-alkyllactams with carbon. The present invention also relates to mixtures comprising poly(vinylidene fluodride) (PVDF) and N-alkyllactams, in which the N-alkyllactams have been purified by contacting the N-alkyllactam as well as a method for their production. The present invention also relates to the use of said mixtures in processing PVDF for applications in which improved color is a quality requirement.
    Type: Application
    Filed: November 18, 2009
    Publication date: September 15, 2011
    Applicant: BASF SE
    Inventors: Yoshihisa Fujii, Kanno Hiroyasu
  • Publication number: 20110124855
    Abstract: A process for purifying laurolactam by means of integrated connection of distillation and crystallization is provided. The crystallization is performed as a solution or melt crystallization. The process reduces thermal stress applied to the laurolactam stream and improved yields are obtained. Raw materials are recovered and recycled in the production sequence.
    Type: Application
    Filed: November 22, 2010
    Publication date: May 26, 2011
    Applicant: EVONIK DEGUSSA GMBH
    Inventors: Axel HENGSTERMANN, Ralf Meier, Daniel Demicoli, Martin Roos, Bernd Guenzel, Frank Huebner
  • Patent number: 7947677
    Abstract: Compounds of formula I: (wherein variables A1, A2, A3, A4, A5, A6, A7, B1, B2, B3, B4, D1, D2, E1, E2, E3, E4, E5, G1, G2, J, K, T, U, V, W, X, Y and Z are as described herein) which are antagonists of CGRP receptors and which are useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.
    Type: Grant
    Filed: November 14, 2006
    Date of Patent: May 24, 2011
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Ian M. Bell, Craig A. Stump, Cory R. Theberge, Steven N. Gallicchio, C. Blair Zartman, Harold G. Selnick
  • Publication number: 20100324257
    Abstract: The present invention relates to a cell, which has been genetically modified relative to its wild type, so that in comparison with its wild type it is able to produce more ?-aminocarboxylic acids, more ?-aminocarboxylic acid esters or more lactams derived from ?-aminocarboxylic acids, starting from carboxylic acids or carboxylic acid esters. Furthermore, the present invention relates to a method for the production of a genetically modified cell, the cells obtainable by this method, a method for the production of ?-aminocarboxylic acids, of ?-aminocarboxylic acid esters or of lactams derived from ?-aminocarboxylic acids, the ?-aminocarboxylic acids, ?-aminocarboxylic acid esters or lactams derived from ?-aminocarboxylic acids obtainable by this method, a method for the production of polyamides based on ?-aminocarboxylic acids or based on lactams and the polyamides obtainable by this method.
    Type: Application
    Filed: December 12, 2008
    Publication date: December 23, 2010
    Applicant: EVONIK DEGUSSA Gmbh
    Inventors: Andreas Karau, Volker Sieber, Thomas Haas, Harald Haeger, Katrin Grammann, Bruno Buehler, Lars Blank, Andreas Schmid, Guido Jach, Bernd Lalla, Andreas Mueller, Katrin Schullehner, Peter Welters, Thorsten Eggert, Andrea Weckbecker
  • Patent number: 7807826
    Abstract: The present invention provides a method for purifying laurolactam from a crude lactam mixture. In the method of the present invention, laurolactam is selectively crystallized by melt crystallization with controlled cooling of the crude lactam mixture.
    Type: Grant
    Filed: October 2, 2008
    Date of Patent: October 5, 2010
    Assignee: Evonik Degussa GmbH
    Inventors: Axel Hengstermann, Ralf Meier, Bernd Günzel, Martin Roos, Stephan Schäflein, Bernd-Holger Modrow
  • Publication number: 20100113460
    Abstract: Disclosed are compounds having the ability to inhibit cytochrome P450 2A6, 2A13, and/or 2B6 and tobacco products comprising them. Also disclosed are pharmaceutical compositions comprising them.
    Type: Application
    Filed: March 20, 2008
    Publication date: May 6, 2010
    Applicant: Givaudan SA
    Inventors: Boris Schilling, Wolf D. Woggon, Antoinette Chougnet, Thierry Granier, Georg Frater, Andreas Hanhart
  • Patent number: 7666861
    Abstract: The present invention is directed to synthetic cytoskeletal active compounds that are related to natural Latrunculin A or Latrunculin B. The present invention is also directed to pharmaceutical compositions comprising such compounds and a pharmaceutically acceptable carrier. The invention is additionally directed to a method of preventing or treating diseases or conditions associated with actin polymerization. In one embodiment of the invention, the method treats increased intraocular pressure, such as primary open-angle glaucoma. The method comprises administering to a subject a therapeutically effective amount of a cytoskeletal active compound of Formula I or II, wherein said amount is effective to influence the cytoskeleton, for example by inhibiting actin polymerization.
    Type: Grant
    Filed: December 4, 2007
    Date of Patent: February 23, 2010
    Assignee: Inspire Pharmaceuticals, Inc.
    Inventors: John W. Lampe, Robert Plourde, Jr., Jin She, Jason L. Vittitow, Paul S. Watson, Michael T. Crimmins, David J. Slade
  • Patent number: 7652003
    Abstract: Disclosed are novel compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R1, R2, R3, n and X are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of treating cognitive or neurodegenerative diseases such as Alzheimer's disease. Also disclosed are methods of treating a cognitive or neurodegenerative disease comprising administering to a patient I need of such treatment a combination of at least one compound of formula I and at least one compound selected from the group consisting of ?-secretase inhibitors other than those of formula I, HMG-CoA reductase inhibitors, gamma-secretase inhibitors, non-steroidal anti-inflammatory agents, N-methyl-D-aspartate receptor antagonists, cholinesterase inhibitors and anti-amyloid antibodies.
    Type: Grant
    Filed: July 26, 2005
    Date of Patent: January 26, 2010
    Assignee: Schering-Plough Corporation
    Inventors: Andrew W Stamford, Ying Huang, Guoqing Li, Corey O Strickand, Johannes H. Voigt
  • Publication number: 20090306367
    Abstract: The present invention is directed to a process for preparing amides. In particular, the process is directed to a process performable on the industrial scale, in which a ketoxime can be converted to a cyclic or acyclic amide by means of a Beckmann rearrangement using 2,4,6-trichloro-1,3,5-triazine as a catalyst in a nonpolar organic solvent.
    Type: Application
    Filed: April 3, 2007
    Publication date: December 10, 2009
    Applicant: EVONIK DEGUSSA GMBH
    Inventors: Martin Roos, Stephanie Schauhoff, Martin Trageser, Hans-Peter Krimmer
  • Patent number: 7579462
    Abstract: Efficient chemical processes for preparing high yields, purities, and different polymorphic forms of 17-allyl amino geldanamycin (17-AAG) and other ansamycins are described and claimed.
    Type: Grant
    Filed: September 18, 2002
    Date of Patent: August 25, 2009
    Assignee: Conforma Therapeutics Corporation
    Inventors: Lin Zhang, Marcus F. Boehm, Siead Zegar
  • Patent number: 7557118
    Abstract: A method for the preparation of a compound of general Formula: or pharmaceutically acceptable derivatives and salts, racemates, isomers and/or tautomers thereof comprising cyclizing an azomethine ylide of general Formula: wherein, A is a cyclic or non-cyclic group; Z is a carbon or a heteroatom; n is selected from 0, 1, 2 or 3; W, X and Y may be the same or different and each are selected from hydrogen; optionally substituted alkyl, alkenyl, alkynyl, amino, alkoxy, alkenoxy, alkynoxy, aryl, alkylthio, heterocyclyl; carboxy, carboxy ester, carboxamido, acyl, acyloxy, mercapto, halogen, nitro, sulfate, phosphate, cyano and optionally protected hydroxy; or W and X, together with the nitrogen and carbon atoms to which they are attached, form a saturated or unsaturated nitrogen containing heterocyclic group which may be optionally substituted or optionally fused to a saturated or unsaturated carbocyclic group, aryl group or heterocyclic group is provided.
    Type: Grant
    Filed: March 7, 2005
    Date of Patent: July 7, 2009
    Assignee: The Australian National University
    Inventors: Martin Gerhardt Banwell, Bernard Luke Flynn
  • Publication number: 20090170878
    Abstract: The invention relates to novel macrocyclic compounds of the formula in which all of the variables are as defined in the specification, in free base form or in acid addition salt form, to their preparation, to their use as medicaments and to medicaments comprising them.
    Type: Application
    Filed: July 19, 2007
    Publication date: July 2, 2009
    Inventor: Rainer Machauer
  • Publication number: 20090088567
    Abstract: The present invention provides a method for purifying laurolactam from a crude lactam mixture. In the method of the present invention, laurolactam is selectively crystallized by melt crystallization with controlled cooling of the crude lactam mixture.
    Type: Application
    Filed: October 2, 2008
    Publication date: April 2, 2009
    Applicant: EVONIK DEGUSSA GmbH
    Inventors: Axel Hengstermann, Ralf Meier, Bernd Guenzel, Martin Roos, Stephan Schaflein, Bernd-Holger Modrow
  • Publication number: 20080188651
    Abstract: Dictyostatin and its analogs show great promise as new anticancer agents. The present invention provides dictyostatin analogs, synthetic intermediates for the synthesis of dictyostatin analogs, and synthetic methods for the synthesis of such analogs and intermediates.
    Type: Application
    Filed: January 2, 2008
    Publication date: August 7, 2008
    Inventors: Dennis P. Curran, Youseung Shin, Jean-Hugues Fournier, John Mancuso, Billy W. Day, Arndt Bruckner, Yoshikazu Fukui
  • Patent number: 7402675
    Abstract: An amine ether of formula A wherein a is 1 or 2; and when a is 1, E is E?; when a is 2, E is L; E? is C1-C36 alkyl; C3-C18 alkenyl; C2-C18 alkinyl; C5-C18 cycloalkyl; C5-C18 cycloalkenyl; a radical of a saturated or unsaturated aliphatic bicyclic or tricyclic hydrocarbon of 7 to 12 carbon atoms; C2-C7alkyl or C3-C7alkenyl substituted by halogen; C7-C15 aralkyl or C7-C15 aralkyl substituted by C1-C4 alkyl or phenyl; or E? is a radical of formula (VII) as explained in claim 1; T? is tertiary C4-C18alkyl or phenyl, each of which are unsubstituted or substituted by halogen, OH, COOR21 or C(O)—R22; or T? is C5-C12cycloalkyl; C5-C12cycloalkyl which is interrupted by at least one O or —NR18—; a polycyclic alkyl radical having 7-18 carbon atoms, or the same radical which is interrupted by at least one O or —NR18—; or T? is —C(G1)(G2)-T?; or C1-C18alkyl or C5-C12cycloalkyl substituted by T? is hydrogen, halogen, NO2, cyano, or is a monovalent organic radical comprising 1-50 carbon atoms; or T? and T?
    Type: Grant
    Filed: August 17, 2004
    Date of Patent: July 22, 2008
    Assignee: Ciba Specialty Chemicals Corp.
    Inventors: Andreas Hafner, Hans Jürg Kirner, Franz Schwarzenbach, Paul Adriaan Van Der Schaaf, Peter Nesvadba
  • Patent number: 7323563
    Abstract: A method for the treatment of bacterial infections in humans and non-human mammals, which comprises inhibiting bacterial growth by administering to a subject an antibacterially effective dose of a compound of formula (I) or a pharmaceutically or veterinarily acceptable salt thereof:
    Type: Grant
    Filed: August 22, 2005
    Date of Patent: January 29, 2008
    Assignee: British Biotech Pharmaceuticals Ltd.
    Inventors: Michael George Hunter, Paul Raymond Beckett, John Martin Clements, Mark Whittaker, Zoe Marie Spavold
  • Patent number: 7320974
    Abstract: The present invention is directed to synthetic cytoskeletal active compounds that are related to natural Latrunculin A or Latrunculin B. The present invention is also directed to pharmaceutical compositions comprising such compounds and a pharmaceutically acceptable carrier. The invention is additionally directed to a method of preventing or treating diseases or conditions associated with actin polymerization. In one embodiment of the invention, the method treats increased intraocular pressure, such as primary open-angle glaucoma. The method comprises administering to a subject a therapeutically effective amount of a cytoskeletal active compound of Formula I or II, wherein said amount is effective to influence the cytoskeleton, for example by inhibiting actin polymerization.
    Type: Grant
    Filed: March 23, 2006
    Date of Patent: January 22, 2008
    Assignee: Inspire Pharmaceuticals, Inc.
    Inventors: John W. Lampe, Robert Plourde, Jr., Jin She, Jason L. Vittitow, Paul S. Watson, Michael T. Crimmins, David J. Slade
  • Publication number: 20070265184
    Abstract: Preparation of cyclododecatriene in a continuous or discontinuous process by trimerization of butadiene in the presence of a catalyst system and a solvent, the crude cyclododecatriene obtained being able to be isolated by means of distillation. The cyclooctadiene formed as by-product can likewise be isolated from the crude product.
    Type: Application
    Filed: March 20, 2007
    Publication date: November 15, 2007
    Applicant: DEGUSSA AG
    Inventors: Jurgen Herwig, Wilhelm Brugging, Martin Roos, Norbert Wilczok
  • Patent number: 7244594
    Abstract: A microbial method for the preparation of an epothilone containing a terminal hydroxyalkyl group, comprising contacting at least one epothilone having a terminal alkyl group with an enzyme or microorganism capable of catalyzing the selective hydroxylation of said alkyl group to a hydroxyalkyl group, and effecting said hydroxylation.
    Type: Grant
    Filed: March 23, 2004
    Date of Patent: July 17, 2007
    Assignee: Bristol-Myers Squibb Company
    Inventors: Wenying Li, James A. Matson, Xiaohua Huang, Kin Sing Lam, Grace A. McClure
  • Patent number: 7125893
    Abstract: This invention describes the new 6-alkenyl- and 6-alkinyl-epothilone derivatives of general formula I in which R1a, R1b, R2a, R3a, R3b, R4, R5, R6, R7, A, Y, D, E, G, Y and Z are as defined in the specification. The compounds are useful in treating malignant tumours, for example, ovarian, stomach, colon, breast, adeno-, head and neck carcinomas, acute lymphocytic and myelocytic leukemia. In addition, these compounds are suitable for anti-angiogenesis therapy as well as for treatment of chronic inflammatory diseases such as psoriasis and arthritis. Methods of use and preparation of the compounds are also described.
    Type: Grant
    Filed: May 1, 2000
    Date of Patent: October 24, 2006
    Assignee: Schering AG
    Inventors: Ulrich Klar, Wolfgang Schwede, Werner Skuballa, Bernd Buchmann, Jens Hoffmann, Rosemarie Lichtner
  • Patent number: 7122677
    Abstract: A NK1 antagonist having the formula (I), wherein Ar1 and Ar2 are optionally substituted phenyl or heteroaryl, X1 is an ether, thio or imino linkage, R4 and R5 are not both H or alkyl, and the remaining variables are as defined in the in the specification, useful for treating a number of disorders, including emesis, depression, anxiety and cough. Pharmaceuticals compositions. Methods of treatment and combinations with other agents are also disclosed.
    Type: Grant
    Filed: November 12, 2002
    Date of Patent: October 17, 2006
    Assignee: Scherig Corporation
    Inventors: Gregory A. Reichard, Sunil Paliwal, Neng-Yang Shih, Dong Xiao, Hon-Chung Tsui, Sapna Majmundar Shah, Cheng Wang, Michelle Laci Wrobleski
  • Patent number: 7026310
    Abstract: The invention relates to novel quinoline derivatives of the formula 1, to their preparation and to their use as medicaments, in particular for treating tumors.
    Type: Grant
    Filed: April 14, 2005
    Date of Patent: April 11, 2006
    Assignee: Zentaris GmbH
    Inventors: Peter Emig, Eckhard Günther, Jürgen Schmidt, Bernd Nickel, Bernhard Kutscher
  • Patent number: 6984734
    Abstract: The present invention provides an oxidative coupling procedure that allows efficient synthesis of novel cyclo[n]pyrrole macrocycles. Therefore, the present invention provides cyclo[n]pyrroles where n is 6, 7, 8, 9, 10, 11, or 12, and derivatives, multimers, isomers, and ion and neutral molecule complexes thereof as new compositions of matter. A protonated form of cyclo[n]pyrrole displays a gap of up to 700 nm between strong Soret and Q-like absorption bands in the electronic spectrum, demonstrating no significant ground state absorption in the visible portion of the electronic spectrum. Uses of cyclo[n]pyrroles as separation media, nonlinear optical materials, information storage media and infrared filters are provided.
    Type: Grant
    Filed: February 26, 2003
    Date of Patent: January 10, 2006
    Assignee: Board of Regents, The University of Texas System
    Inventors: Jonathan L. Sessler, Daniel Seidel, Frederic R. Bolze, Thomas Koehler
  • Patent number: 6962992
    Abstract: The invention describes crown ether chelators, including crown ethers having the formula and aza-substituted and thia-substituted analogs thereof. These crown ethers are substituted by a dye moiety, a chemically reactive group, a conjugated substance, or a combination thereof. Chelators that are substituted by fluorescent dyes are particularly useful as indicators for metal cations, particularly Na+ and K+ ions, and particularly where binding of the target ion results in a change in the fluorescence properties of the indicator that can be correlated with the ion concentration. Methods are provided for utilizing reactive groups on the chelators for conjugation to dyes, lipids and polymers and methods for enhancing entry of the indicators into living cells.
    Type: Grant
    Filed: December 19, 2001
    Date of Patent: November 8, 2005
    Assignee: Molecullar Probes, Inc.
    Inventors: Vladimir V. Martin, Kyle R. Gee, Richard P. Haugland, Zhenjun Diwu
  • Patent number: 6936447
    Abstract: Autoinducer molecules, e.g., N-(3-oxododecanoyl)homoserine lactone, for Pseudomonas aeruginosa are described. The molecules regulate gene expression in the bacterium. Therapeutic compositions and therapeutic methods involving analogs and/or inhibitors of the autoinducer molecules also are described. The molecules are useful for treating or preventing infection by Pseudomonas aeruginosa.
    Type: Grant
    Filed: April 3, 2000
    Date of Patent: August 30, 2005
    Assignees: University of Iowa Research Foundation, University of Rochester, Ithaca College
    Inventors: James P. Pearson, Kendall M. Gray, Luciano Passador, Kenneth D. Tucker, Anatol Eberhard, Barbara H. Iglewski, Everett P. Greenberg
  • Patent number: 6906188
    Abstract: A method for making epothilones and epothilone analogs is described, as are novel compounds made by the method. Exemplary novel compounds include those according to the formula: With respect the formula, G is selected from the group consisting of R2 substituents independently are selected from the group consisting of H and lower alkyl groups; Z is selected from the group consisting of the halogens and —CN; M is selected from the group consisting of O and NR3; R3 is selected from the group consisting of H, lower alkyl, R4CO, R4OCO, and R4SO2; R4 is selected from the group consisting of H, lower alkyl, and aryl; T is selected from the group consisting of CH2, CO, HCOH and protected derivatives thereof; W is H or OR; and X and Y independently are selected from the group consisting of O, NH, S, CO, and C.
    Type: Grant
    Filed: January 29, 2003
    Date of Patent: June 14, 2005
    Assignee: State of Oregon acting by and through the State Board of Higher Education on behalf of Oregon State University
    Inventors: James David White, Kurt Frederick Sundermann, Rich Garrett Carter
  • Patent number: 6900328
    Abstract: An amine ether of formula (A) wherein a is 1 or 2; and when a is 1, E is E?; when a is 2, E is L; E? is C1-C36 alkyl; C3-C18 alkenyl; C2-C18 alkinyl; C5-C18 cycloalkyl; C5-C18 cycloalkenyl; a radical of a saturated or unsaturated aliphatic bicyclic or tricyclic hydrocarbon of 7 to 12 carbon atoms; C2-C7alkyl or C3-C7alkenyl substituted by halogen; C7-C15aralkyl or C7-C15 aralkyl substituted by C1-C4 alkyl or phenyl; or E? is a radical of formula (VII) as explained in claim 1; T? is tertiary C4-C18alkyl or phenyl, each of which are unsubstituted or substituted by halogen, OH, COOR21 or C(O)—R22; or T? is C5-C12cycloalkyl; C5-C12cacloalkyl which is interrupted by at least one O or —NR18—; a polycyclic alkyl radical having 7-18 carbon atoms, or the same radical which is interrupted by at least one O or —NR18—; or T? is —C(G1)(G2)—T?; or C1-C18alkyl or C5-C12cycloalkyl substituted by F(I)T? is hydrogen, halogen, NO2, cyano, or is a monovalent organic radical comprising 1-50 carbon atoms; or T? and T? together for
    Type: Grant
    Filed: May 17, 2001
    Date of Patent: May 31, 2005
    Assignee: Ciba Specialty Chemicals Corporation
    Inventors: Andreas Hafner, Hans Jürg Kirner, Franz Schwarzenbach, Paul Adriaan Van Der Schaaf, Peter Nesvadba
  • Patent number: 6890921
    Abstract: This invention relates to a series of arylsubstituted piperazines, of Formula I pharmaceutical compositions containing them and intermediates used in their manufacture. The compounds of the invention selectively inhibit binding to the ?-1a adrenergic receptor, a receptor which has been implicated in benign prostatic hyperplasia. As such the compounds are potentially useful in the treatment of this and other disease.
    Type: Grant
    Filed: March 15, 2000
    Date of Patent: May 10, 2005
    Assignee: Ortho-McNeil Pharmaceutical, Inc.
    Inventors: Linda Jolliffe, William Murray, Virginia Pulito, Allen Reitz, Xiaobing Li, Linda Mulcahy, Cynthia Maryanoff, Frank Villani
  • Patent number: 6852713
    Abstract: Lactam derivatives of the general formula are disclosed. Pharmaceutical compositions containing the compounds and methods for their use are also disclosed.
    Type: Grant
    Filed: April 16, 2003
    Date of Patent: February 8, 2005
    Assignee: Adolor Corporation
    Inventors: Roland E. Dolle, Paul Anson Tuthill
  • Patent number: 6790953
    Abstract: The present invention relates to novel ether compounds, compositions comprising ether compounds, and methods useful for treating and preventing cardiovascular diseases, dyslipidemias, dysproteinemias, and glucose metabolism disorders comprising administering a composition comprising an ether compound. The compounds, compositions, and methods of the invention are also useful for treating and preventing Alzheimer's Disease, Syndrome X, peroxisome proliferator activated receptor-related disorders, septicemia, thrombotic disorders, obesity, pancreatitis, hypertension, renal disease, cancer, inflammation, and impotence. In certain embodiments, the compounds, compositions, and methods of the invention are useful in combination therapy with other therapeutics, such as hypocholesterolemic and hypoglycemic agents.
    Type: Grant
    Filed: July 26, 2002
    Date of Patent: September 14, 2004
    Assignee: Esperion Therapeutics, Inc.
    Inventors: Jean-Louis Henri Dasseux, Carmen Daniela Oniciu
  • Publication number: 20040132997
    Abstract: Compounds represented by the following structure (I), acid-addition salts and prodrugs are disclosed: 1
    Type: Application
    Filed: September 25, 2003
    Publication date: July 8, 2004
    Inventors: Scott C. Mitchell, Benjamin Nicholson
  • Patent number: 6747021
    Abstract: The present invention provides antitumor methods, formulations, and compounds comprising a cryptophycin.
    Type: Grant
    Filed: July 26, 2001
    Date of Patent: June 8, 2004
    Assignees: Eli Lilly and Company, Wayne State University, University of Hawaii
    Inventors: Thomas Hughes Corbett, Richard Elliott Moore, Jian Liang
  • Patent number: RE47539
    Abstract: Convenient methods of preparing aza-dibenzocyclooctynes are disclosed herein. Aza-dibenzocyclooctynes attached to a surface are also disclosed herein. Aza-dibenzocyclooctynes can be reacted with azides to form heterocyclic compounds. Such reactions can be useful in a wide variety of applications including, for example, labeling surfaces.
    Type: Grant
    Filed: December 16, 2016
    Date of Patent: July 30, 2019
    Assignee: UNIVERSITY OF GEORGIA RESEARCH FOUNDATION, INC.
    Inventors: Vladimir V. Popik, Alexander Kuzmin, Andrei Polukhtine