Carbonyl Of -coo- Group Bonded Directly To A Ring Patents (Class 544/172)
  • Patent number: 10745433
    Abstract: The invention relates to compounds for inhibiting a cancer cell or a virus. Particularly, the invention provides compounds for inhibiting, treating and/or preventing cancer and Zika virus.
    Type: Grant
    Filed: January 12, 2017
    Date of Patent: August 18, 2020
    Assignee: Taipei Medical University
    Inventors: Yun Yen, Jing-Ping Liou, Yun-Ru Liu
  • Publication number: 20150148347
    Abstract: A compound of formula I, wherein the groups R1, R2, R3, X, m, and n are defined as in claim 1, which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2. Furthermore, the invention relates to novel intermediates, useful for the synthesis of compounds of formula I.
    Type: Application
    Filed: November 25, 2014
    Publication date: May 28, 2015
    Inventors: Iain LINGARD, Dieter HAMPRECHT
  • Publication number: 20150072984
    Abstract: Chemical entities that are curcumin derivatives, pharmaceutical compositions and methods of treatment of cancer are described.
    Type: Application
    Filed: August 29, 2012
    Publication date: March 12, 2015
    Inventor: Xiangping Qian
  • Publication number: 20140275008
    Abstract: Provide herein are compounds and pharmaceutical compositions suitable as modulators of hemoglobin, methods and intermediates for their preparation, and methods for their use in treating disorders mediated by hemoglobin and disorders that would benefit from tissue and/or cellular oxygenation.
    Type: Application
    Filed: March 15, 2013
    Publication date: September 18, 2014
    Inventors: Qing Xu, Zhe Li
  • 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
  • Patent number: 8748598
    Abstract: Analogs of 3-O-acetyl-11-keto-beta-boswellic acid and their method of preparation are presented. The analogs may be used as anti-inflammatory and anti-cancer agents. The compounds inhibit 5-lipoxygenase enzyme and various cell lines related to inflammation as well as to cancer showing a significantly better efficacy when compared to the normal boswellic acids. The analogs are capable of controlling and treating various inflammatory diseases and cancers.
    Type: Grant
    Filed: September 30, 2011
    Date of Patent: June 10, 2014
    Assignee: Laila Nutraceuticals
    Inventors: Ganga Raju Gokaraju, Rama Raju Gokaraju, Venkata Subbaraju Gottumukkala, Trimurtulu Golakoti, Krishanu Sengupta
  • Patent number: 8697335
    Abstract: A radiation-sensitive resin composition includes a compound, a resin and a radiation-sensitive acid generator. The compound has a structure in which a group represented by a following formula (1) is bound to a nitrogen atom. The resin has an acid-dissociative dissolution-controlling group and has a property such that alkali solubility of the resin increases by an action of an acid. In the formula (1), Y is a monovalent group having 5 to 20 carbon atoms, and “*” represents a bonding hand with the nitrogen atom. In the formula (i), R1, R2 and R3 each independently represent a linear or branched alkyl group having 1 to 4 carbon atoms or a monovalent alicyclic hydrocarbon group having 4 to 12 carbon atoms, or R1 and R2 are linked with each other to form a bivalent alicyclic hydrocarbon group, and “*” represents a bonding hand with the oxygen atom.
    Type: Grant
    Filed: January 17, 2012
    Date of Patent: April 15, 2014
    Assignee: JSR Corporation
    Inventors: Kazuo Nakahara, Mitsuo Sato
  • Publication number: 20130267699
    Abstract: The invention provides heterocyclic compounds with quaternary centers and methods of preparing compounds. Methods include the method for the preparation of a compound of Formula (II): comprising treating a compound of Formula (I): with a transition metal catalyst and under alkylation conditions as valence and stability permit.
    Type: Application
    Filed: March 12, 2013
    Publication date: October 10, 2013
    Inventors: Brian M. Stoltz, Scott C. Virgil, David E. White, Taiga Yurino, Yiyang Liu, Douglas C. Behenna, Douglas Duquette, Christian Eidamshaus
  • Publication number: 20130261122
    Abstract: The present invention is directed to novel substituted bicyclic aromatic compounds useful as S-nitrosoglutathione reductase (GSNOR) inhibitors, pharmaceutical compositions comprising such compounds, and methods of making and using the same.
    Type: Application
    Filed: December 16, 2011
    Publication date: October 3, 2013
    Applicant: N30 Pharmaceuticls, Inc.
    Inventors: Xicheng Sun, Jian Qiu, Adam Stout
  • Publication number: 20130144057
    Abstract: (Meth)acrylic acid ester, which contains one or more partial structures each represented by the following formula 1 in a molecule thereof, wherein the partial structure is a urethane structure which does not have a hydrogen atom directly bonded to a nitrogen atom of the following formula 1: where the nitrogen atom is not bonded to a hydrogen atom.
    Type: Application
    Filed: November 28, 2012
    Publication date: June 6, 2013
    Inventor: Mitsunobu MORITA
  • Publication number: 20130102780
    Abstract: The present disclosure provides processes for the N-dealkylation of tertiary amines and the use of transition metal catalysts to prepare tertiary N-allyl amine derivatives and secondary amine derivatives thereof. The tertiary amines can be alkaloids and, more particularly, the tertiary amines can be opioids. In specific embodiments, the present disclosure provides methods for use in processes for the synthesis of naloxone and naltrexone from oripavine.
    Type: Application
    Filed: December 11, 2012
    Publication date: April 25, 2013
    Applicant: Rhodes Technologies
    Inventor: Rhodes Technologies
  • Publication number: 20130089624
    Abstract: The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula I: wherein the variables are as defined herein. Additionally, the present invention also relates to novel processes for the production of various morpoholine based intermediates.
    Type: Application
    Filed: September 28, 2012
    Publication date: April 11, 2013
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: Jean-Damien Charrier, Stephen Clinton Young, Christopher John Davis, John Studley
  • Publication number: 20130012701
    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: Application
    Filed: June 22, 2012
    Publication date: January 10, 2013
    Applicant: 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: 20120196852
    Abstract: The invention is directed towards novel naphthoquinone and naphthothiazole compounds, and methods of treating disorders related to MetAP, including tuberculosis and bacterial infection, using various naphthoquinone, hydroxyquinonline, and naphthothiazole compounds.
    Type: Application
    Filed: August 5, 2010
    Publication date: August 2, 2012
    Applicant: THE JOHNS HOPKINS UNIVERSITY
    Inventors: Jun O. Liu, Omonike Arike Olaleye, Shridhar Bhat
  • Publication number: 20120035176
    Abstract: Analogs of 3-O-acetyl-11-keto-beta-boswellic acid and their method of preparation are presented. The analogs may be used as anti-inflammatory and anti-cancer agents. The compounds inhibit 5-lipoxygenase enzyme and various cell lines related to inflammation as well as to cancer showing a significantly better efficacy when compared to the normal boswellic acids. The analogs are capable of controlling and treating various inflammatory diseases and cancers.
    Type: Application
    Filed: September 30, 2011
    Publication date: February 9, 2012
    Inventors: Ganga Raju Gokaraju, Rama Raju Gokaraju, Venkata Subbaraju Gottumukkala, Trimurtulu Golakoti, Krishanu Sengupta
  • Patent number: 8105504
    Abstract: Organic materials which possess outstanding stability to oxidative, thermal or light-induced degradation comprise as stabilizers at least one compound of the formula (I) wherein the general symbols are as defined in claim 1. The compounds of formula I are especially useful as stabilizers for protecting polymers and lubricants against oxidative, thermal or light-induced degradation and as scavengers for oxidized developer in color photographic material.
    Type: Grant
    Filed: August 22, 2005
    Date of Patent: January 31, 2012
    Assignee: BASF SE
    Inventors: Michèle Gerster, Peter Nesvadba
  • Publication number: 20110288057
    Abstract: The invention relates to the use of and mainly novel compounds of the formula I wherein the moieties are as defined in the description, which are useful as farnesyl pyrophosphate synthase modulators and e.g. in the treatment of proliferative diseases.
    Type: Application
    Filed: October 12, 2009
    Publication date: November 24, 2011
    Applicant: Novartis AG
    Inventors: Simona Cotesta, Joseph Fraser Glickman, Wolfgang Jahnke, Andreas Marzinzik, Silvio Ofner, Jean-Michel Rondeau, Thomas Zoller
  • Publication number: 20110152255
    Abstract: Compounds comprising formula (I) or a pharmaceutically acceptable salt thereof, are disclosed, wherein J, B, Y, and A are as described in claims 1-13. Methods, compositions, and medicaments related thereto are also disclosed, for treating baldness, glaucoma or inflammatory bowel diseases.
    Type: Application
    Filed: April 21, 2009
    Publication date: June 23, 2011
    Inventors: Yariv Donde, Jeremiah H. Nguyen
  • Publication number: 20110059972
    Abstract: 1,4 naphthoquinones derivatives, of formula (I) wherein A is selected from the following rings: their preparation and their application as antimalarial agents
    Type: Application
    Filed: March 25, 2009
    Publication date: March 10, 2011
    Applicant: CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE
    Inventors: Elisabeth Davioud-Charvet, Tobias Muller, Holger Bauer, R. Heiner Schirmer
  • Patent number: 7626042
    Abstract: A medicament having inhibitory activity against NF-?B activation which comprises as an active ingredient a substance selected from the group consisting of a compound represented by the following general formula (I) and a pharmacologically acceptable salt thereof, and a hydrate thereof and a solvate thereof: wherein X represents a connecting group whose number of atoms in a main chain is 2 to 5 (said connecting group may be substituted), “A” represents an acyl group which may be substituted, (provided that unsubstituted acetyl group and unsubstituted acryloyl group are excluded,) or a C1 to C6 alkyl group which may be substituted, or A may bind to connecting group X to form a cyclic structure which may be substituted, “E” represents an aryl group which may be substituted or a heteroaryl group which may be substituted, ring Z represents an arene which may have one or more substituents in addition to the group represented by formula —O-A wherein A has the same meaning as that defined above and the group repr
    Type: Grant
    Filed: June 5, 2003
    Date of Patent: December 1, 2009
    Assignee: Institute of Medicinal Molecular Design, Inc.
    Inventors: Susumu Muto, Akiko Itai
  • Publication number: 20090156804
    Abstract: The present invention relates to a production method of an optically active morpholine compound represented by the formula 10, which includes the following steps: wherein each symbol is as defined in the specification. The present invention also relates to a production method of an compound represented by the formula 55, which includes the following steps: wherein each symbol is as defined in the specification. According to the production method of the present invention, an optically active 2-aryl-substituted morpholine compound and 3-oxo-3-(pyrimidin-4-yl)propionate, which are important as starting materials for synthesizing 2-(2-arylmorpholin-4-yl)-1-methyl-1H-[4,4?]bipyrimidinyl-6-one having a tau protein kinase 1 inhibitory activity and useful as a therapeutic drug for Alzheimer's disease and the like, can be produced in a high yield by an industrially advantageous method.
    Type: Application
    Filed: July 21, 2006
    Publication date: June 18, 2009
    Applicants: MITSUBISHI TANABE PHARMA CORPORATION, SANOFI-AVENTIS
    Inventors: Masahiro Okuyama, Fumiaki Uehara, Hiroshi Iwamura, Kazutoshi Watanabe
  • Patent number: 7435851
    Abstract: The present invention provides substituted puleganic amides and compositions thereof, which are both useful as a topical treatment for skin, such as a repellant for insects and arthropods.
    Type: Grant
    Filed: September 29, 2006
    Date of Patent: October 14, 2008
    Assignee: E.I. du Pont de Nemours and Company
    Inventor: Mark A. Scialdone
  • Patent number: 7232821
    Abstract: Compounds of formula (I) or a pharmaceutically acceptable derivative thereof: wherein A, R1, R2, Rx, R8, R9 and n are as defined in the specification, a process for the preparation of such compounds, pharmaceutical compositions comprising such compounds and the use of such compounds in medicine.
    Type: Grant
    Filed: April 7, 2003
    Date of Patent: June 19, 2007
    Assignee: Glaxo Group Limited
    Inventors: Gerard Martin Paul Giblin, Adrian Hall, David Nigel Hurst, Ian Reginald Kilford, Xiao Qing Lewell, Alan Naylor, Riccardo Novelli
  • Patent number: 7195751
    Abstract: This invention pertains to methods, mixtures, kits and/or compositions for the determination of analytes by mass analysis using unique labeling reagents or sets of unique labeling reagents. The labeling reagents can be isomeric or isobaric and can be used to produce mixtures suitable for multiplex analysis of the labeled analytes.
    Type: Grant
    Filed: January 27, 2004
    Date of Patent: March 27, 2007
    Assignee: Applera Corporation
    Inventors: Darryl J. C. Pappin, Michael Bartlet-Jones
  • Patent number: 7034020
    Abstract: The present invention provides a series of compounds having structural formulas wherein n1 is 1 to 5, n2 is 1 to 4 and m is 1 to 3; X is O or NH; Y is CH2, O, S, NH, NR; R is selected from the group consisting a straight-chain aliphatic group, a branched-chain aliphatic group and an alicyclic group; wherein R? is selected from the group consisting of hydrogen, methyl and ethyl; when Y is O, n1 is not 1; and wherein X and R? are independently optionally substituted at C2, C3 or C4 in compounds of Fomula IV or a pharmaceutically acceptable salt thereof. Also provided is a method of inactivating antigen-specific T cells in a n individual.
    Type: Grant
    Filed: December 12, 2003
    Date of Patent: April 25, 2006
    Assignee: The University of Arkansas for Medical Science
    Inventors: Kathleen Gilbert, E. Kim Fifer
  • Patent number: 7002010
    Abstract: The instant invention discloses a process for the preparation of compounds of the formula I: wherein the general symbols are as defined in claim 1, which process comprises reacting a compound of formula II: wherein the general symbols are as defined in claim 1, with a compound of the formula III: wherein R5 is as defined in claim 1. The compounds of the formula II are new and useful as stabilizers for protecting organic materials, in particular synthetic polymers, reprographic materials or coating materials against oxidative, thermal or light-induced degradation.
    Type: Grant
    Filed: December 4, 2001
    Date of Patent: February 21, 2006
    Assignee: Ciba Specialty Chemicals Corporation
    Inventors: Dario Lazzari, Mirko Rossi, Giuseppe Veronesi, Nazzareno Ruggeri, Katharina Fritzsche, Adalbert Braig
  • Publication number: 20040209873
    Abstract: Arylcycloalkyl derivatives having branched side chains, processes for their preparation and their use as pharmaceuticals
    Type: Application
    Filed: February 27, 2004
    Publication date: October 21, 2004
    Applicant: Aventis Pharma Deutschland GmbH
    Inventors: Christian Stapper, Heiner Glombik, Eugen Falk, Jochen Goerlitzer, Dirk Gretzke, Stefanie Keil, Hans-Ludwig Schaefer, Wolfgang Wendler
  • Patent number: 6803370
    Abstract: Disclosed are certain alpha amino acid compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.
    Type: Grant
    Filed: July 20, 2001
    Date of Patent: October 12, 2004
    Assignees: Elan Pharmaceuticals, Inc., Wyeth
    Inventors: Andrei W. Konradi, Michael A. Pleiss, Eugene D. Thorsett, Susan Ashwell, Gregory S. Welmaker, Anthony Kreft, Dimitrios Sarantakis, Darren B. Dressen, Francine S. Grant, Christopher Semko, Ying-Zi Xu
  • Patent number: 6689882
    Abstract: A new improved process for synthesizing morpholinylbenzenes of the formula I by reacting morpholine of formula II with a substituted benzene of formula III, wherein morpholine is used as a reactant and as the only one solvent.
    Type: Grant
    Filed: November 12, 2002
    Date of Patent: February 10, 2004
    Assignee: AstraZeneca AB
    Inventor: Wei Tian
  • Patent number: 6602869
    Abstract: This invention relates to novel compounds of formula (I) wherein R1 represents a polymer, aryl or alkyl group, R2 represents a hydrogen atom, a halogen atom, a radical CN, CF3, OH, OCF3, COOH, R7, OR7 or OCOR7, R3 represents an aryl or alkyl halogen, R4 represents an alkyl radical. The invention also relates to a cosmetic composition comprising said compounds and to the use thereof to reduce and/or curb hair loss i.e. to increase and/or stimulate the growth of said hair.
    Type: Grant
    Filed: November 21, 2001
    Date of Patent: August 5, 2003
    Assignee: L'Oreal S.A.
    Inventors: Jean-Baptiste Galey, Maria Dalko, Lionel Breton
  • Publication number: 20030096802
    Abstract: The compound of the formula (I) 1
    Type: Application
    Filed: July 15, 2002
    Publication date: May 22, 2003
    Applicant: ONO PHARMACEUTICAL CO., LTD.
    Inventors: Shuichi Ohuchida, Kazuo Kishimoto, Narito Tateishi, Hiroyuki Ohno
  • Publication number: 20030087934
    Abstract: The present invention relates to certain substituted polyketides of formula I, 1
    Type: Application
    Filed: August 5, 2002
    Publication date: May 8, 2003
    Inventors: Frederick R. Kinder, Kenneth W. Bair, Timothy M. Ramsey, Michael L. Sabio
  • Publication number: 20030078418
    Abstract: This invention relates to novel substituted succinic acid metallo-&bgr;-lactamase inhibitors which are useful potentiators of &bgr;-lactam antibiotics.
    Type: Application
    Filed: March 15, 2002
    Publication date: April 24, 2003
    Inventors: James M. Balkovec, Mark L. Greenlee, Steven H. Olson, Gregory P. Rouen
  • Publication number: 20030060624
    Abstract: The present invention relates to processes for the preparation of any of the intermediate 1,3-substituted indenes of the formulae (Ia), (Ib) and (Ic) or a mixture thereof: 1
    Type: Application
    Filed: April 17, 2002
    Publication date: March 27, 2003
    Inventor: Robert A. Singer
  • Publication number: 20030060465
    Abstract: Compounds of the formula: RC(O)O-spacer-OC(O)R′, wherein (i) RC(O)— is the acyl residue of an NSAID or other pharmaceutically active agent bearing a carboxylic acid function, (ii) spacer is Cn alkyl, (iii) n is from 1 to 6, and (iv) R′ is substituted or unsubstituted heteroaryl or heterocycle, and pharmaceutical compositions thereof.
    Type: Application
    Filed: December 18, 2001
    Publication date: March 27, 2003
    Inventor: Jamal A. Jilani
  • Publication number: 20020193594
    Abstract: The invention relates to a process for the preparation of carboxamides, in particular peptides, from an acid component in the form of a compound containing at least one carboxyl group and an amine component in the form of a compound containing at least one primary or secondary amino group, and its use.
    Type: Application
    Filed: March 27, 2002
    Publication date: December 19, 2002
    Inventors: Joachim Rudolph, Gunther Jung, Bernd Thern
  • Patent number: 6479518
    Abstract: The present invention is directed to certain novel compounds represented by structural formula I: or a pharmaceutically acceptable salt thereof, wherein R3, R5, R6, R7, R8, R11, R12, R13, Q, W, X, Y and Z are defined herein. The invention is also concerned with pharmaceutical formulations comprising these novel compounds as active ingredients and the use of the novel compounds and their formulations in the treatment of certain disorders. The compounds of this invention are tachykinin receptor antagonists and are useful in the treatment of psychiatric disorders including depression and anxiety.
    Type: Grant
    Filed: September 21, 2001
    Date of Patent: November 12, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Paul E. Finke, Laura C. Meurer, Sander G. Mills, Malcolm MacCoss, Hongbo Qi
  • Patent number: 6479491
    Abstract: The present invention relates to compounds of formula (I), any of it enantiomers, or any mixture thereof, or a pharmaceutically acceptable acid addition salt thereof, wherein R1, R2, R3, R4, R11, R12, R13, R14 and R15 each independently are hydrogen, alkyl, alkoxy, halogen, trifluoromethyl, nitro, cyano, amino, acyl, alkylamino, dialkylamino, aminocarbonyl, or acylamino; R5 is hydrogen, alkyl, alkoxyalkyl, or phenylalkyl; X is —CH2—Z—, Z—CH2—, NH—CO—, —CO—NH—, or —CH═CH—; wherein Z is O, S, CH2, or NH; Y is O, —CH2—W—, —W—CH2—; wherein W is O, or S; and n is 0, 1 or 2. The compounds are useful in the treatment of psychotic disorders.
    Type: Grant
    Filed: November 13, 2000
    Date of Patent: November 12, 2002
    Assignee: Neurosearch A/S
    Inventors: Oskar Axelsson, Dan Peters, Jorgen Scheel-Kruger, Elsebet Ostergaard Nielsen
  • Publication number: 20020055509
    Abstract: Disclosed are a series of phenylalanine derivatives, to compositions containing them, to processes for their preparation, and to their use in medicine.
    Type: Application
    Filed: July 20, 2001
    Publication date: May 9, 2002
    Inventors: Andrei W. Konradi, Michael A. Pleiss, Eugene D. Thorsett, Susan Ashwell, Gregory S. Welmaker, Anthony Kreft, Dimitrios Sarantakis, Darren B. Dressen, Francine S. Grant, Christopher Semko, Ying-Zi Xu
  • Patent number: 6200972
    Abstract: This invention relates to neurotrophic low molecular weight, small molecule heterocyclic esters and amides having an affinity for FKBP-type immunophilins, and their use as inhibitors of the enzyme activity associated with immunophilin proteins, particularly peptidyl-prolyl isomerase, or rotamase, enzyme activity.
    Type: Grant
    Filed: February 23, 1998
    Date of Patent: March 13, 2001
    Assignee: GPI NIL Holdings, Inc.
    Inventors: Jia-He Li, Gregory S. Hamilton
  • Patent number: 6093823
    Abstract: The invention pertains to a process for the continuous production of basic cyclic optically active .alpha.-amino acids of general formula (I) by continuous racemate splitting via diastereomeric salt pairs with re-racemisation of the residual amino acid or amino acid derivative in the mother liquid with the aid of an optically active acid.
    Type: Grant
    Filed: March 24, 1998
    Date of Patent: July 25, 2000
    Assignee: Degussa Aktiengesellschaft
    Inventors: Matthias Kottenhahn, Klaus Stingl, Karlheinz Drauz
  • Patent number: 6037498
    Abstract: This invention relates to novel compounds of general formula (I) ##STR1## wherein R.sup.1 represents an organic group, R.sup.2 represents a hydrogen atom or an organic group, and the asterisk denotes that the group R.sup.1 is predominantly in the R- or S-configuration such that the compound is in substantially enantiomerically pure form. The compounds are a useful source of chiral nucleophiles, e.g. undergoing stereoselective Michael addition to .alpha.,.beta.-unsaturated carboxylic acid derivatives.
    Type: Grant
    Filed: August 12, 1996
    Date of Patent: March 14, 2000
    Assignee: Oxford Asymmetry International PLC
    Inventors: Stephen Graham Davies, Mario Eugenio Cosamino Polywka, David Roy Fenwick, Frank Reed
  • Patent number: 5955608
    Abstract: Novel processes for producing benzothiophenes employing ethylene carbonate or propylene carbonate are provided.
    Type: Grant
    Filed: January 30, 1998
    Date of Patent: September 21, 1999
    Assignee: Eli Lilly and Company
    Inventor: Douglas P. Kjell
  • Patent number: 5917086
    Abstract: A method for the purification of a keto acid having the general formula ##STR1## wherein R1 and R2 independently represent a straight or branched chain alkyl of 1-18 carbon atoms, a cycloalkyl of 4-8 carbon atoms or a phenyl both of which may be substituted by at least one substituent selected from the group consisting of halogen atoms and alkyls having 1-4 carbon atoms, an aralkyl of 7-10 carbon atoms, alkoxyalkyl having 2-20 carbon atoms, tetrahydrofuryl alkyl, alkylcarboxy alkyl, alkyl carboxy benzyl, or R1 and R2 together with the adjacent nitrogen atom may form a heterocyclic ring, or one of R.sub.1 and R.sub.2 is hydrogen, which comprises slurrying the keto acid with an alcohol solvent, maintaining the slurry at elevated temperature in a sealed vessel until the Rhodamine impurity has dissolved, cooling and isolating the pure keto acid by filtration.
    Type: Grant
    Filed: January 9, 1998
    Date of Patent: June 29, 1999
    Assignee: Ciba Specialty Chemicals Corporation
    Inventors: James Philip Taylor, John Barry Henshall, John Whitworth
  • Patent number: 5885984
    Abstract: Aminocyclohexylester compounds, including thioesters, are disclosed. The compounds of the present invention may be incorporated in compositions and kits. The present invention also discloses a variety of in vitro and in vivo uses for the compounds and compositions, including the blockade of ion channels and the treatment of arrhythmias.
    Type: Grant
    Filed: February 27, 1997
    Date of Patent: March 23, 1999
    Assignee: University of British Columbia
    Inventors: Bernard A. MacLeod, Michael J. A. Walker, Richard A. Wall
  • Patent number: 5869663
    Abstract: The invention relates to compounds of the formula ##STR1## in which: A is a divalent radical selected from:A.sub.1) --O--CO--A.sub.2) --CH.sub.2 --O--CO--A.sub.3) --O--CH.sub.2 --CO--A.sub.4) --O--CH.sub.2 --CH.sub.2 --A.sub.5) --N(R.sub.1)--CO--A.sub.6) --N(R.sub.1)--CO--CO--A.sub.7) --N(R.sub.1)--CH.sub.2 --CH.sub.2 --A.sub.8) --O--CH.sub.2 --in which:R.sub.1 is a hydrogen or a (C.sub.1 -C.sub.4)-alkyl; andAm is a nitrogen-containing heterocycle.
    Type: Grant
    Filed: March 18, 1997
    Date of Patent: February 9, 1999
    Assignee: Sanofi
    Inventors: Xavier Emonds-Alt, Isabelle Grossriether, Patrick Gueule, Vincenzo Proietto, Didier Van Broeck
  • Patent number: 5852193
    Abstract: The invention relates to intermediates and processes for producing benzothiophenes employing hydroxylamines.
    Type: Grant
    Filed: April 29, 1998
    Date of Patent: December 22, 1998
    Assignee: Eli Lilly and Company
    Inventor: Erik Christopher Chelius
  • Patent number: 5783697
    Abstract: Vinyl carbamate compounds are prepared by reacting appropriate secondary amines with carbon dioxide and acetylenically unsaturated compounds in the presence of a compound of a metal from the platinum group, in particular a ruthenium compound, with either one of the two process steps (a) and (b) or, preferably, both being carried out:(a) the acetylene compound is reinjected during the reaction;(b) the reaction is carried out in the presence of a tertiary amine.
    Type: Grant
    Filed: January 21, 1997
    Date of Patent: July 21, 1998
    Assignee: BASF Aktiengesellschaft
    Inventors: Marc Heider, Jochem Henkelmann, Michael Karcher, Thomas Ruhl
  • Patent number: 5777162
    Abstract: Described herein are compounds of Formula (XX) and Formula (XXIV), shown below, and processes of making same. ##STR1## wherein p is 0 ##STR2## wherein p is 1, and Y is chlorine or bromine.
    Type: Grant
    Filed: November 12, 1996
    Date of Patent: July 7, 1998
    Assignee: Zeneca Limited
    Inventors: Ian Richard Matthews, Christopher Richard Ayles Godfrey, John Martin Clough
  • Patent number: 5756817
    Abstract: The present invention relates to a racemic or enantiomerically enriched O-carbamoyl-phenylalaninol compound represented by the following structural formula V and pharmaceutically acceptable salts thereof to treat diseases of the central nervous system: ##STR1## wherein Ph is a phenyl group as described as follows: ##STR2## wherein R is a member selected from the group consisting of hydrogen, lower alkyl of 1 to 8 carbon atoms, halogen selected from F, Cl, Br and I, alkoxy containing 1 to 3 carbon atoms, nitro, hydroxy, trifluoromethyl, and thioalkoxy containing 1 to 3 carbon atoms, and x is an integer from 1 to 3, with the proviso that R is the same or different when x is 2 or 3, R.sup.1 and R.sup.2 may be the same or different from each other and are independently selected from the group consisting of hydrogen, lower alkyl of 1 to 8 carbon atoms, aryl, arylalkyl, cyclic propyl and 5 to 7-membered aliphatic cyclic compounds, and R.sup.1 and R.sup.
    Type: Grant
    Filed: October 7, 1996
    Date of Patent: May 26, 1998
    Assignee: Yukong Limited
    Inventors: Yong Moon Choi, Dong Il Han, Yong Kil Kim, Hun Woo Shin, Jeong-Han Park