Patents Examined by John Kight
  • Patent number: 6172221
    Abstract: A back extraction process in which beta-lactam antibiotics or clavulanic acid is extracted from an organic solvent phase into an aqeous medium phase, using a mixing region in which the phases are mixed rapidly under high turbulence and shear stress.
    Type: Grant
    Filed: August 27, 1997
    Date of Patent: January 9, 2001
    Assignee: SmithKline Beecham p.l.c.
    Inventor: Simon Ruddick
  • Patent number: 6172233
    Abstract: Compounds of structure (2) are prepared by reaction of an arecoline analogue of structure(4) with an organometallic compound containing an X-substituted phenyl group, such as a compound of structure (3). Suitably the compound of structure (3) is a Grignard reagent, where M is magnesium and Y is a halogen atom, or M may be a Group II metal and Y is a halogen atom or a second X-substituted phenyl group. When structure (3) is a Grignard reagent, the reaction is carried out either in a suitable non-ether solvent, typically a hydrocarbon or a non-reactive chlorinated hydrocarbon, or in a mixture of such a solvent with diethyl ether. Compounds of structure (2) are important intermediates in the preparation of inter alia paroxetine.
    Type: Grant
    Filed: January 15, 1998
    Date of Patent: January 9, 2001
    Assignee: SmithKline Beecham plc
    Inventor: Neal Ward
  • Patent number: 6172222
    Abstract: This invention concerns the treatment of smooth muscle spasticity or excess muscle contraction such as urge urinary incontinence with a compound of the formula wherein: R1 and R2 are independently straight chain alkyl of 1 to 6 carbon atoms, branched alkyl of 3 to 6 carbons atoms, or cycloalkyl of 3 to 6 carbons atoms where R1 and R2 may be substituted by F, Cl, Br, I, OH, NH2, cyano, C1-C6 alkoxy, C1-C6alkylthio, COOH or COOC1-C6 alkyl; R3 is an aryl or heteroaryl as defined herein, optionally substituted with 0 to 4 groups selected independently from C1-C6 alkyl, C1-C6 alkoxy, cyano, F, Cl, Br, C1-C6 alkylthio, CO2R1, CONH2, OH, NH2, and NO2; n is 0 or 1; R4 is a straight chain alkyl group of 1 to 10 carbons atoms, a branched alkyl of 3 to 10 carbons, or a cycloalkyl of 3 to 10 carbons; and all crystalline forms and the pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: June 7, 1999
    Date of Patent: January 9, 2001
    Assignee: American Home Products Corporation
    Inventors: Adam Matthew Gilbert, Zhen-jia Chen
  • Patent number: 6169092
    Abstract: 3-Urea-pyridofurans and -pyridothiophenes are prepared by reacting appropriately substituted 3-amino-pyridofurans or -pyridothiophenes with isocyanates or isothiocyanates. The 3-urea-pyridofurans and -pyridothiophenes can be used as active ingredients in medicaments, particularly in medicaments for the treatment of acute and chronic inflammatory processes.
    Type: Grant
    Filed: January 5, 1999
    Date of Patent: January 2, 2001
    Assignee: Bayer Aktiengesellschaft
    Inventors: Gabriele Br{umlaut over (a)}unlich, Mazen Es-Sayed, R{umlaut over (u)}diger Fischer, Rolf Henning, Burkhard Fugmann, Stephan Schneider, Michael Sperzel, Graham Sturton, Mary Fitzgerald, Barbara Briggs, Arnel Concepcion
  • Patent number: 6166075
    Abstract: This invention relates to new antiestrogens of the general formula ##STR1## in which the substituents have the meanings that are explained in more detail in the description.The new compounds are a) pure antiestrogens or b) antiestrogens with partial estrogenic action (tissue-selective estrogens).Based on these properties, the new compounds are suitable for the production of pharmaceutical agents: in the case of a), for example, for the treatment of breast cancer; in the case of b), for example, for hormone replacement therapy.
    Type: Grant
    Filed: June 9, 1999
    Date of Patent: December 26, 2000
    Assignee: Schering Aktiengesellschaft
    Inventors: Ulrich Klar, Rolf Bohlmann, Karsten Parczyk, Karl-Heinrich Fritzemeier, Monika Lessl, Rosemarie Lichtner
  • Patent number: 6166215
    Abstract: A process for producing the compound [I] or a salt thereof having excellent pesticidal activity as shown in the following schema.
    Type: Grant
    Filed: September 8, 1999
    Date of Patent: December 26, 2000
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Hideki Uneme, Hitoshi Ishizuka
  • Patent number: 6166004
    Abstract: There are described compounds of formula I*, ##STR1## wherein R.sub.1 is lower alkoxycarbonyl,R.sub.2 is secondary or tertiary lower alkyl or lower alkylthio-lower alkyl,R.sub.3 is phenyl that is unsubstituted or substituted by one or more lower alkoxy radicals, or C.sub.4 -C.sub.8 cycloalkyl,R.sub.4 is phenyl or cyclohexyl each substituted in the 4-position by unsaturated heterocyclyl that is bonded by way of a ring carbon atom, has from 5 to 8 ring atoms, contains from 1 to 4 hetero atoms selected from nitrogen, oxygen, sulfur, sulfinyl (--SO--) and sulfonyl (--SO.sub.2 --) and is unsubstituted or substituted by lower alkyl or by phenyl-lower alkyl,R.sub.5, independently of R.sub.2, has one of the meanings mentioned for R.sub.2, andR.sub.6, independently of R.sub.1, is lower alkoxycarbonyl,or salts thereof, provided that at least one salt-forming group is present.The compounds are inhibitors of retroviral aspartate protease and can be used, for example, in the treatment of AIDS.
    Type: Grant
    Filed: September 20, 1999
    Date of Patent: December 26, 2000
    Assignee: Novartis Finance Corporation
    Inventors: Alexander Fassler, Guido Bold, Hans-Georg Capraro, Marc Lang, Satish Chandra Khanna
  • Patent number: 6166069
    Abstract: This invention provides compounds of Formula I having the structure ##STR1## wherein: A, B, R1, R2, R3, R4, R5, and R6 are as defined in the specification,or a pharmaceutically acceptable salt thereof, which are useful in treating metabolic disorders related to insulin resistance or hyperglycemia.
    Type: Grant
    Filed: May 10, 1999
    Date of Patent: December 26, 2000
    Assignee: American Home Products Corporation
    Inventors: Michael S. Malamas, Jay E. Wrobel, Arlene J. Dietrich, Zenan Li, Iwan Gunawan
  • Patent number: 6166040
    Abstract: Pharmaceutical compounds of the formula: ##STR1## in which n is 1 to 6, m is 1 or 2 and p is 1 or 2, R.sup.1 and R.sup.2 are each hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, HO--C.sub.1-4 alkyl, C.sub.1-4 alkoxy-C.sub.1-4 alkyl, C.sub.1-4 alkylthio, halo, optionally substituted phenyl, optionally substituted phenyl-C.sub.1-4 alkyl, or R.sup.1 and R.sup.2 together with the carbon atom to which they are attached form a C.sub.3-6 cycloalkyl group, >C.dbd.O, C.dbd.NOR' where R' is hydrogen or C.sub.1-4 alkyl,R.sup.3, R.sup.4 and R.sup.5 are each hydrogen, halo, nitro, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 alkyl-CO--, where m is 0, 1 or 2, R'R"N--SO.sub.2 --, --COOR', --CONR'R", --NR'R", --N(OR')COOR", --COR', --NHSO.sub.2 R', where R' and R' are each hydrogen or C.sub.1-4 alkyl,R.sup.6 and R.sup.7 are each hydrogen or C.sub.1-4 alkyl,X is oxygen or sulphur,the dotted line represents an optional double bond, and the fluorine atom is attached at the 6- or 7-position; and salts thereof.
    Type: Grant
    Filed: May 11, 1999
    Date of Patent: December 26, 2000
    Assignee: Eli Lilly and Company Limited
    Inventors: John Fairhurst, Peter Thaddeus Gallagher, Martin Victor Miles, William Martin Owton, Colin William Smith
  • Patent number: 6162919
    Abstract: A process for preparing the d-threo isomer of methylphenidate hydrochloride comprising converting d,l-threo methylphenidate hydrochloride to the free base form in a first step, resolving the free base prepared in the first step with (R)-(-)-1,1'-binaphthyl-2,2'-diyl hydrogen phosphate to obtain the phosphate salt enriched with the d-threo isomer of methylphenidate in a second step, basifying the phosphate salt to obtain the free base form of the d-threo isomer of methylphenidate in a third step, converting the free base to the hydrochloride salt form of the d-threo isomer of methylphenidate in high optical purity in a fourth step, and recrystallizing the hydrochloride salt form to obtain the desired d-threo isomer in a higher optical purity. An alternative embodiment relates to the preparation of the d-threo isomer of methylphenidate hydrochloride utilizing the hydrochloride salt form of the racemic mixture of threo-methylphenidate directly.
    Type: Grant
    Filed: December 3, 1998
    Date of Patent: December 19, 2000
    Assignee: Novartis AG
    Inventors: Mahavir Prashad, Bin Hu
  • Patent number: 6162479
    Abstract: Safe, effective first-pass inhibiting compounds and citrus-derived substances are provided. Formulations containing the compounds are also provided as are methods for inhibiting the first pass effect.
    Type: Grant
    Filed: December 7, 1999
    Date of Patent: December 19, 2000
    Assignee: Bioavailability Systems, LLC
    Inventor: James W. Harris
  • Patent number: 6162924
    Abstract: A process for preparing a halohydrin of a water-miscible olefin comprising: reacting a water-miscible olefin in water with a compound of the formula (I) ##STR1## wherein R.sub.1 and R.sub.2 independently represent a branched or unbranched, substituted or unsubstituted, lower alkyl having from 1 to 5 carbons and X is a halogen, to thereby form the halohydrin of the water-miscible olefin.
    Type: Grant
    Filed: April 9, 1999
    Date of Patent: December 19, 2000
    Assignee: Eastman Chemical Company
    Inventor: Neil W. Boaz
  • Patent number: 6162807
    Abstract: This invention is directed to monocyclic N-heterocyclics which are substituted by acyclic or cyclic thio derivatives which are useful as anti-coagulants. This invention is also directed to pharmaceutical compositions containing the compounds of the invention, and methods of using the compounds to treat disease-states characterized by thrombotic activity.
    Type: Grant
    Filed: January 11, 2000
    Date of Patent: December 19, 2000
    Assignee: Berlex Laboratories, Inc.
    Inventors: Monica J. Kochanny, Michael M. Morrissey, Howard P. Ng
  • Patent number: 6159985
    Abstract: The subject invention involves compounds having the structure: wherein the C.sub..alpha. --N.sub..beta. and C.sub.5 -C.sub.6 bonds are independently single or double bonds, R1 is selected from alkyl, aryl, and heterocycle; R2-R13 are independently selected from hydrogen and other substituents; and pharmaceutically-acceptable salts thereof. The subject invention also involves pharmaceutical compositions containing such compounds, and methods for treating or preventing diseases and disorders using such compounds.
    Type: Grant
    Filed: September 21, 1999
    Date of Patent: December 12, 2000
    Assignee: The Procter & Gamble Company
    Inventors: Song Liu, David Edward Portlock, Schwe Fang Pong
  • Patent number: 6159996
    Abstract: Polycyclic thiazolidin-2-ylidene amines and their physiologically tolerable salts and physiologically functional derivatives of the formula I ##STR1## in which the radicals have the meanings indicated, and their physiologically tolerable salts and a process for their preparation are described. The compounds are suitable, for example, as anorectics.
    Type: Grant
    Filed: July 12, 1999
    Date of Patent: December 12, 2000
    Assignee: Aventis Pharma Deutschland GmbH
    Inventors: Gerhard Jaehne, Karl Geisen, Hans Jochen Lang
  • Patent number: 6156763
    Abstract: Certain non-nucleoside compounds that will selectively inhibit telomerase by targeting the nucleic add structures, such as G-quadruplexes, that may be associated with human telomeres or telomerase have been identified. Inhibition of human telomerase by two perylenetetracarboxylic acid diimides and a carbocyanine has been demonstrated. .sup.1 H-NMR studies have evidenced the stabilization of a G-quadruplex by the perylenetetracarboxylic acid diimide compounds and provided evidence that these and structurally related compounds inhibit the telomerase enzyme by a mechanism consistent with interaction with G-quadruplex structures.
    Type: Grant
    Filed: February 4, 1999
    Date of Patent: December 5, 2000
    Assignee: Board of Regents, The University of Texas System
    Inventors: Sean M. Kerwin, Oleg Y. Fedoroff, Miguel Salazar, Laurence H. Hurley
  • Patent number: 6156754
    Abstract: The present invention relates to glycoconjugates of camptothecin derivatives in which at least one carbohydrate component is linked via suitable spacers with the A or B ring of a camptothecin derivative. The invention furthermore relates to processes for preparing the compounds according to the invention and to their use as medicaments, in particular in connection with cancer.
    Type: Grant
    Filed: March 24, 1999
    Date of Patent: December 5, 2000
    Assignee: Bayer Aktiengesellschaft
    Inventors: Hans-Georg Lerchen, Karsten von dem Bruch, Jorg Baumgarten, Michael Sperzel
  • Patent number: 6156784
    Abstract: Disclosed are compositions containing compounds of the formula (I) below wherein A,B,C,G,Q and R are defined herein. The compounds are useful as phosphotyrosine mimics that, when incorporated into an appropriate molecular structure, inhibit the binding of tyrosine kinase-dependent regulatory proteins to their native phosphotyrosine-containing ligands or receptors. Also disclosed are methods for preparing the compounds of the formula (I).
    Type: Grant
    Filed: December 7, 1999
    Date of Patent: December 5, 2000
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Rajashekhar Betageri, Jean-Marie Ferland, Montse Llinas-Brunet, Neil Moss, John R. Proudfoot
  • Patent number: 6152969
    Abstract: The present invention relates to the development of a coloring matter which has a moderately bluish magenta color and an excellent lightfastness and can provide a wide range of color tones in the visible range when used together with yellow and cyan inks. A water-base ink composition or the like is prepared by using a sulfonic acid derivative of an anthrapyridone compound represented by general formula (I) as a magenta dye, wherein R.sub.1 ' represents alkoxycarbonyl, carbonyl or benzoyl; R.sub.2 represents hydrogen or alkyl; and R.sub.3 and R.sub.4 represent each independently hydrogen, halogeno, alkyl or alkoxy.
    Type: Grant
    Filed: February 3, 1999
    Date of Patent: November 28, 2000
    Assignee: Nippon Kayaku Kabushiki Kaisha
    Inventors: Hiroyuki Matsumoto, Yasuo Shirasaki, Katsunori Fujii
  • Patent number: 6153724
    Abstract: Polymers and processes for synthesizing the polymers from .alpha.,.beta.-unsaturated lactones, particularly 2(5H)-furanone, and amines with side chains. The polymers are used as hydrogels, as polymers that can bind metals and form complexes that are soluble in organic solvents, as polymers useful as flocculants in water purification, as polymers useful on non-fouling surfaces for biofilm suppression, polymers for use on non-thrombogenic surfaces, and polymers with uses as thin conductive films for microchips and other electronic devices. The process is a polymerization reaction involving the cyclic .alpha.,.beta.-unsaturated lactone and a primary amine or primary ammonium compound.
    Type: Grant
    Filed: September 24, 1998
    Date of Patent: November 28, 2000
    Assignee: Board of Trustees Operating Michigan State University
    Inventor: Rawle I. Hollingsworth