Spiro Patents (Class 549/264)
  • Publication number: 20150011776
    Abstract: Disclosed is a compound of formula 1, as shown below, where R1, R2, R3, R4, R5, R6 and R7 are as described herein. Also, disclosed is a process for the preparation of compounds of formula 1, and intermediates used therein. The compound of formula 1 can be useful for preparation of halichondrin analogs such as Eribulin.
    Type: Application
    Filed: December 24, 2012
    Publication date: January 8, 2015
    Inventors: Fabio E.S. Souza, Alena Rudolph, Ming Pan, Boris Gorin, Dino Alberico
  • Publication number: 20140323559
    Abstract: This invention provides for novel antiparasitic and pesticidal forms of moxidectin, including a long-acting polymeric implant. The resulting compounds may be used in veterinary compositions which are used in treating, controlling and preventing of endo- and ectoparasite infections in animals.
    Type: Application
    Filed: March 25, 2014
    Publication date: October 30, 2014
    Applicant: MERIAL LIMITED
    Inventors: Susan Mancini Cady, Baoqing Ma, Robert Clark Chapman, Chunhua Yang, Uday Jain
  • Publication number: 20140256619
    Abstract: The present invention relates to the use of avermectin derivative as a drug for the treatment of parasitic infections. The avermectin derivative is represented by the formula (I) wherein: (i) R1 is chosen from the group constituted of —CH(CH3)2, —CH(CH3)CH2CH3, or cyclohexyle, (ii) X represents —CH2CH2—, or —CH?CH—, (iii) R2 is chosen from the group constituted of or —OH group, (iv) R3 is OH or NOH, (v) represents a single bond when R3 is OH, or a double bond when R3 is NOH, as an inhibitor of a membrane-bound protein which transports exogenous compounds out of target cells.
    Type: Application
    Filed: October 18, 2012
    Publication date: September 11, 2014
    Inventors: Anne Lespine, Roger Prichard, Cecile Menez
  • Patent number: 8822528
    Abstract: This invention relates to novel polyether ionophores, formulations comprising same, and to methods of making and using these compounds and formulations for the treatment and/or prevention of parasitic infection in animals and humans. These compounds exhibit improved safety profiles and/or efficacies as compared to parent compounds.
    Type: Grant
    Filed: November 16, 2011
    Date of Patent: September 2, 2014
    Assignees: Merial Limited, Universite Claude Bernard Lyon 1, Centre National de la Recherche Scientifique (CNRS)
    Inventors: Jean Delaveau, Emile Vialle, Marc Lemaire, Stephane Pellet-Rostaing, Bruno Andrioletti
  • Patent number: 8765974
    Abstract: Disclosed is a method for producing a tetrahydropyran compound represented by general formula (5) shown in the scheme. Accordingly, a tetrahydropyran derivative is obtained in high yield and with high selectivity without using a highly toxic reagent, and an industrially useful method for producing a tetrahydropyran derivative and an intermediate thereof can be provided. In formulae (1) to (5), R1 and R2 each independently represent a hydrogen atom, a linear, branched, or cyclic alkyl group, or an aromatic group which may have a substituent, and R1 and R2may be combined to form an alkylene group, thereby forming a ring; and R3 and R4 each independently represent a hydrogen atom or a linear, branched, or cyclic alkyl group, and R3 and R4 may be combined to form an alkylene group, thereby forming a ring.
    Type: Grant
    Filed: April 14, 2010
    Date of Patent: July 1, 2014
    Assignee: Nissan Chemical Industries, Ltd.
    Inventors: Hirotaka Kawanami, Kana Yamaguchi, Shota Murase
  • Publication number: 20130345442
    Abstract: Methods and compositions are provided for the preparation of insecticidal compositions.
    Type: Application
    Filed: August 21, 2013
    Publication date: December 26, 2013
    Applicant: Bayer CropScience LP
    Inventors: Hong ZHU, Jorge JIMENEZ, Colleen TAYLOR, Magalie GUILHABERT-GOYA, Jonathan MARGOLIS
  • Patent number: 8586112
    Abstract: The invention provides a process for the production of a substance or composition for the treatment, by therapy or prophylaxis, of parasitic infections, in particular malarial infections such as Plasmodium falciparum infections, of the human or animal body. The process comprises extracting the substance or composition from roots of the plant species Dicoma anomala, by an extraction using an organic solvent to obtain a liquid extract containing the substance or composition and removing the solvent from the liquid extract to leave a dried extract containing the substance or composition. The invention extends also to the use of the substance or composition in the manufacture of a medicament or preparation for such treatment of infections; to a substance or composition for use in such treatment of said infections; to compounds for use in such treatment of said infections; and to a method of treating said infections using such compounds.
    Type: Grant
    Filed: November 2, 2005
    Date of Patent: November 19, 2013
    Assignees: South African Medical Research Council, University of Cape Town
    Inventors: Motlalepula Gilbert Matsabisa, William Ernest Campbell, Peter Ian Folb, Peter John Smith
  • Publication number: 20130251647
    Abstract: The invention relates to new types of modulators of the cold menthol receptor TRPM8, to methods of modulating the TRPM8 receptor using these modulators; and in particular the use of the modulators for inducing a sensation of coldness; and also the articles and compositions produced using these modulators.
    Type: Application
    Filed: September 20, 2012
    Publication date: September 26, 2013
    Applicant: BASF SE
    Inventors: Thomas Subkowski, Claus Bollschweiler, Jens Wittenberg, Wolfgang Siegel, Ralf Pelzer
  • Publication number: 20130143956
    Abstract: This invention provides for novel antiparasitic and pesticidal forms of moxidectin, including a long-acting polymeric implant. The resulting compounds may be used in veterinary compositions which are used in treating, controlling and preventing of endo- and ectoparasite infections in animals.
    Type: Application
    Filed: November 30, 2012
    Publication date: June 6, 2013
    Applicant: Merial Limited
    Inventors: Susan Mancini Cady, Baoqing Ma, Robert Clark Chapman, Chunhua Yang, Uday Jain
  • Patent number: 8362170
    Abstract: Provided is a polymerizable compound represented by the following general formula (ca-1) or (cb-1): wherein the variables in the formulae are defined in the specification.
    Type: Grant
    Filed: June 18, 2012
    Date of Patent: January 29, 2013
    Assignee: FUJIFILM Corporation
    Inventors: Shuji Hirano, Kaoru Iwato, Hiroshi Saegusa, Yusuke Iizuka
  • Patent number: 8252877
    Abstract: Provided is a polymerizable compound represented by the following general formula (ca-1) or (cb-1): wherein the variables in the formulae are defined in the specification.
    Type: Grant
    Filed: December 11, 2009
    Date of Patent: August 28, 2012
    Assignee: FUJIFILM Corporation
    Inventors: Shuji Hirano, Kaoru Iwato, Hiroshi Saegusa, Yusuke Iizuka
  • Publication number: 20120128722
    Abstract: This invention relates to novel polyether ionophores, formulations comprising same, and to methods of making and using these compounds and formulations for the treatment and/or prevention of parasitic infection in animals and humans. These compounds exhibit improved safety profiles and/or efficacies as compared to parent compounds.
    Type: Application
    Filed: November 16, 2011
    Publication date: May 24, 2012
    Inventors: Jean Delaveau, Emile Vialle, Marc Lemaire, Stephane Pellet-Rostaing, Bruno Andrioletti
  • Publication number: 20120046476
    Abstract: Disclosed is a method for producing a tetrahydropyran compound represented by general formula (5) shown in the scheme. Accordingly, a tetrahydropyran derivative is obtained in high yield and with high selectivity without using a highly toxic reagent, and an industrially useful method for producing a tetrahydropyran derivative and an intermediate thereof can be provided. In formulae (1) to (5), R1 and R2 each independently represent a hydrogen atom, a linear, branched, or cyclic alkyl group, or an aromatic group which may have a substituent, and R1 and R2may be combined to form an alkylene group, thereby forming a ring; and R3 and R4 each independently represent a hydrogen atom or a linear, branched, or cyclic alkyl group, and R3 and R4 may be combined to form an alkylene group, thereby forming a ring.
    Type: Application
    Filed: April 14, 2010
    Publication date: February 23, 2012
    Inventors: Hirotaka Kawanami, Kana Yamaguchi, Shota Murase
  • Publication number: 20100152401
    Abstract: Provided is a polymerizable compound represented by the following general formula (ca-1) or (cb-1): wherein the variables in the formulae are defined in the specification.
    Type: Application
    Filed: December 11, 2009
    Publication date: June 17, 2010
    Applicant: FUJIFILM CORPORATION
    Inventors: Shuji HIRANO, Kaoru IWATO, Hiroshi SAEGUSA, Yusuke IIZUKA
  • Publication number: 20090304832
    Abstract: The invention provides a process for the production of a substance or composition for the treatment, by therapy or prophylaxis, of parasitic infections, in particular malarial infections such as Plasmodium falciparum infections, of the human or animal body. The process comprises extracting the substance or composition from roots of the plant species Dicoma anomala, by an extraction using an organic solvent to obtain a liquid extract containing the substance or composition and removing the solvent from the liquid extract to leave a dried extract containing the substance or composition. The invention extends also to the use of the substance or composition in the manufacture of a medicament or preparation for such treatment of infections; to a substance or composition for use in such treatment of said infections; to compounds for use in such treatment of said infections; and to a method of treating said infections using such compounds.
    Type: Application
    Filed: November 2, 2005
    Publication date: December 10, 2009
    Inventors: Motlalepula Gilbert Matsabisa, William Ernest Campbell, Peter Ian Folb, Peter John Smith
  • Patent number: 7576124
    Abstract: Safe, effective first-pass inhibiting compounds and citrus-derived substances are provided. Formulations containing the compounds are also provided as are methods for their preparation and for inhibiting the first pass effect.
    Type: Grant
    Filed: May 11, 2007
    Date of Patent: August 18, 2009
    Assignee: Bioavailability Systems, L.L.C.
    Inventor: James W. Harris
  • Patent number: 7576123
    Abstract: Compositions, methods, etc. for addressing the first-pass effect.
    Type: Grant
    Filed: April 4, 2007
    Date of Patent: August 18, 2009
    Assignee: Bioavailability Systems, L.L.C.
    Inventor: James W. Harris
  • Publication number: 20080300134
    Abstract: A compound of the formula (I) wherein the bond between carbon atoms 22 and 23 indicated with a broken line is a single or double bond, n is 0, 1 or 2, R1 represents, for instance, a C1-C12alkyl group, R2 represents, for instance, R15 group, R3 represents, for instance, R2 group, R4 represents, for instance, a chemical constituent, R5 represents, for instance, hydrogen, and R6 represents, for instance, R16 group; wherein R15 represents, for instance, unsubstituted or mono- to pentasubstituted C1-C6alkyl group, and R16 represent, for instance, hydrogen, or R15; and if appropriate, an E/Z isomer and/or diastereoisomer and/or tautomer of the compound of formula (I), in each case in free form or in salt form. Such compounds have been found to have pesticidal properties.
    Type: Application
    Filed: August 19, 2005
    Publication date: December 4, 2008
    Applicant: SYNGENTA CROP PROTECTION, INC.
    Inventors: Ottmar Franz Hueter, Thomas Pitterna, Pierre Jung, Fiona Murphy Kessabi, Laura Quaranta
  • Patent number: 7378534
    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: August 29, 2005
    Date of Patent: May 27, 2008
    Assignee: Bioavailability Systems, LLC.
    Inventor: James W. Harris
  • Patent number: 7316884
    Abstract: A 5-methylene-1,3-dioxolan-4-one derivative and a monomer and copolymer thereof and a resist composition containing the polymer or copolymer where the 5-methylene-1,3 -dioxolan-4-one derivative is of formula (1): wherein R1 represents a bridged cyclic hydrocarbon group containing 4 to 16 carbon atoms, or a linear or branched alkyl group containing 1 to 6 carbon atoms which has a bridged cyclic hydrocarbon group containing 4 to 16 carbon atoms as a substituent; R2 represents a hydrogen atom, or a linear or branched alkyl group containing 1 to 6 carbon atoms; or R1 and R2 represent a bridged cyclic hydrocarbon group containing 4 to 16 carbon atoms together with the carbon atom to which they are bound, provided that the alkyl group and the bridged cyclic hydrocarbon group may have at least one substituent selected from a group consisting of a linear or branched alkyl group containing 1 to 6 carbon atoms which may be optionally substituted, a hydroxy group, a carboxy group, an acyl group containing 2 to 6 car
    Type: Grant
    Filed: October 22, 2002
    Date of Patent: January 8, 2008
    Assignee: Mitsubishi Rayon Co., Ltd.
    Inventors: Ryuichi Ansai, Yoshihiro Kamon, Tadayuki Fujiwara, Hideaki Kuwano, Atsushi Ootake, Hikaru Momose
  • Patent number: 7314942
    Abstract: Alpha-methylenelactone is produced from butyrolactone and valerolactone by the addition of formaldehyde in a supercritical fluid.
    Type: Grant
    Filed: January 7, 2003
    Date of Patent: January 1, 2008
    Assignee: E. I. duPont de Nemours & Co.
    Inventors: Keith W. Hutchenson, Leo E. Manzer
  • Patent number: 7232915
    Abstract: An improved process for the preparation of cis-1,3-diols is described where a beta hydroxy ketone is treated with a trialkylborane or dialkylalkoxyborane or a mixture of a trialkylborane and a dialkylalkoxyborane followed by recovery and reuse of the alkylborane species to convert additional beta hydroxy ketone to the cis-1,3-diol.
    Type: Grant
    Filed: April 29, 2005
    Date of Patent: June 19, 2007
    Assignee: Warner-Lambert Company
    Inventors: Robert Lee Bosch, Richard Joseph McCabe, Thomas Norman Nanninga, Robert Joseph Stahl
  • Patent number: 7230027
    Abstract: Compositions, methods, etc. for addressing the first-pass effect.
    Type: Grant
    Filed: March 16, 2005
    Date of Patent: June 12, 2007
    Assignee: Bioavailability Systems, L.L.C.
    Inventor: James W. Harris
  • Patent number: 6808724
    Abstract: The present invention relates to a novel compound isolated from Artemisia Sylvatica, expressed by the formula 1, a method of isolation, and its use thereof, and more particularly to a novel compound isolated from Artemisia Sylvatica, a method of isolation, and its use in inhibiting farnesyl transferase activity, which is essential for activating Ras oncogene, and repressing cancer cell growth.
    Type: Grant
    Filed: January 28, 2003
    Date of Patent: October 26, 2004
    Assignee: Korea Research Institute of Bioscience and Biotechnology
    Inventors: Byoung-Mog Kwon, Kwang-Hee Son, Dong-Choi Han, Jong-Han Kim, Hyun-Mi Kang, Sun Bok Jeon
  • Patent number: 6716832
    Abstract: The present invention relates to novel arylphenyl-substituted cyclic ketoenols of the formula (I): in which X represents halogen, alkyl, alkoxy, alkenyloxy, alkylthio, alkylsulphinyl, alkylsulphonyl, halogenalkyl, halogeno-alkoxy, halogenoalkenyloxy, nitro, cyano or in each case optionally substituted phenyl, phenoxy, phenylthio, phenyl-alkoxy or phenylalkylthio, Y represents in each case optionally substituted cycloalkyl, aryl or hetaryl, Z represents hydrogen, halogen, alkyl, alkoxy, alkenyloxy, halogenoalkyl, halogenoalkoxy, halogenoalkenyloxy, nitro or cyano, CKE represents one of the groups: in which A, B, D, G and Q1 to Q6 are each as defined in the description, to a plurality of processes for their preparation and to their use as pesticides and herbicides.
    Type: Grant
    Filed: May 2, 2002
    Date of Patent: April 6, 2004
    Assignee: Bayer Aktiengesellschaft
    Inventors: Folker Lieb, Reiner Fischer, Alan Graff, Udo Schneider, Thomas Bretschneider, Christoph Erdelen, Wolfram Andersch, Mark-Wilhelm Drewes, Markus Dollinger, Ingo Wetcholowsky, Randy Allen Myers
  • Patent number: 6693092
    Abstract: The present invention relates to novel arylphenyl-substituted cyclic ketoenols of the formula (I) in which X represents halogen, alkyl, alkoxy, alkenyloxy, alkylthio, alkylsulphinyl, alkylsulphonyl, halogenoalkyl, halogenoalkoxy, halogenoalkenyloxy, nitro, cyano or in each case optionally substituted phenyl, phenoxy, phenylthio, phenylalkoxy or phenylalkylthio, Y represents in each case optionally substituted cycloalkyl, aryl or hetaryl, W and Y independently of one another each represent hydrogen, halogen, alkyl, alkoxy, alkenyloxy, halogenoalkyl, halogenoalkoxy, halogenoalkenyloxy, nitro or cyano, CKE represents one of the groups  in which A, B, D, G and Q1 to Q6 are each as defined in the description, to a plurality of processes for their preparation and to their use as pesticides and herbicides.
    Type: Grant
    Filed: May 9, 2002
    Date of Patent: February 17, 2004
    Assignee: Bayer Aktiengesellschaft
    Inventors: Folker Lieb, Reiner Fischer, Alan Graff, Udo Schneider, Thomas Bretshneider, Christoph Erdelen, Wolfram Andersch, Mark Wilhelm Drewes, Markus Dollinger, Ingo Wetcholowsky, Randy Allen Myers
  • Patent number: 6660766
    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: July 30, 2001
    Date of Patent: December 9, 2003
    Assignee: Bioavailability Systems, LLC
    Inventor: James W. Harris
  • Patent number: 6605595
    Abstract: Avermectin derivatives represented by the general formula (I) or salts thereof: wherein —X----Y— represents —CH═CH—, —CH2—C(═O)—, —CH2—CH2—, or —CH2—CH(R13)—; for example, 1) when —X----Y— represents —CH═CH—, R1 represents (R11)(R12)C [wherein R11 represents a substituted or unsubstituted lower alkyl group; a formyl group; a lower alkoxylcarbonyl group etc.
    Type: Grant
    Filed: February 11, 2002
    Date of Patent: August 12, 2003
    Assignee: The Kitasato Institute
    Inventors: Satoshi Omura, Toshiaki Sunazuka, Andreas Turberg, Georg von Samson-Himmelstjerna, Olaf Hansen, Achim Harder
  • Publication number: 20030139601
    Abstract: Compounds of formula (I) and salts thereof: 1
    Type: Application
    Filed: October 22, 2002
    Publication date: July 24, 2003
    Applicant: SANKYO COMPANY, LIMITED
    Inventors: Akio Saito, Yoko Sugiyama, Toshimitsu Toyama, Toshihiko Nanba
  • Publication number: 20030099910
    Abstract: The present invention relates to a photochromic spirobenzopyran compound of the formula (1) and its derivatives, a spirobenzopyran group having unsaturated terminal groups, a polymer prepared therefrom, a method for the production thereof, a composition comprising said spirobenzopyran or said spirobenzopyran group-containing polymer and a photochromic switch film using the same: 1
    Type: Application
    Filed: August 24, 1999
    Publication date: May 29, 2003
    Inventors: EUN-KYOUNG KIM, YUN-KI CHOI, SAM-ROK KEUM
  • Publication number: 20030027063
    Abstract: A three dimensional optical data storage and retrieval system that includes a three dimensional optical data storage medium and an apparatus for providing access to data stored on the medium. The data storage medium includes an optical data storage material which either a low molecular weight or polymeric glassy solid that are capable of undergoing multi-photon excitation that are energetically different in the write and read cycles. The optical data storage materials provide substantially higher storage capacities relative to conventional materials, and show high robustness in that written and stored data can undergo multiple read cycles without erasure or overwriting. An apparatus for data recording and accessing stored data on the medium includes a controllable variable energy photo-emitting excitation source and an emission photo-detector.
    Type: Application
    Filed: July 12, 2002
    Publication date: February 6, 2003
    Applicant: The Trustees of Boston College
    Inventors: John T. Fourkas, Christopher E. Olson, Michael J.R. Previte
  • Patent number: 6500960
    Abstract: Modified PKS gene clusters which produce novel polyketides in an efficient system in a host cell or in a cell free extract are described. The novel polyketides result from the incorporation of diketides of the formula wherein A is a moiety that activates the diketide, and at least one of R1 and R2 is a substituent other than that natively occurring in the diketide normally processed by the modified PKS cluster. The polyketides may also be glycosylated to provide antibiotics.
    Type: Grant
    Filed: May 14, 1999
    Date of Patent: December 31, 2002
    Assignees: Stanford University (Board of Trustees of the Leland Stanford Junior University), Brown University Research Foundation
    Inventors: Chaitan Khosla, Rembert Pieper, Guanglin Luo, David E. Cane, Camilla Kao
  • Patent number: 6486195
    Abstract: The most thermodynamically stable crystalline form of the benzoic acid salt of 4″-deoxy-4″-epi-methylamino avermectin B1a/B1b as the hemihydrate is obtained by crystallization from organic solvents containing a controlled amount of water.
    Type: Grant
    Filed: January 20, 1995
    Date of Patent: November 26, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Raymond Cvetovich, James A. McCauley, Richard Demchak, Richard J. Varsolona
  • Publication number: 20020173473
    Abstract: The invention relates to compounds of the general formula 1
    Type: Application
    Filed: November 26, 2001
    Publication date: November 21, 2002
    Inventor: Thomas Goebel
  • Patent number: 6476066
    Abstract: Safe, effective first-pass inhibiting compounds and citrus-derived substances are provided. Formulations containing the compounds are also provided as are methods for their preparation and for inhibiting the first pass effect.
    Type: Grant
    Filed: February 27, 2001
    Date of Patent: November 5, 2002
    Assignee: Bioavailability Systems, L.L.C.
    Inventor: James W. Harris
  • Patent number: 6410590
    Abstract: The present invention relates to novel derivatives of Andrographolide, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, and their pharmaceutically acceptable solvates. The novel derivatives of Andrographolide have the general formula (I) The andrographolide derivatives represented by general formula (I) are useful for treating cancer, HSV, HIV, psoriasis, restonosis, atherosclerosis, other cardiovascular disorders, and can be used as antiviral, antimalarial, antibacterial, hepatoprotective, and immunomodulating agents and for treatment of other metabolic disorders.
    Type: Grant
    Filed: February 1, 2001
    Date of Patent: June 25, 2002
    Assignee: Dr. Reddy's Research Foundation
    Inventors: Srinivas Nanduri, Sriram Rajagopal, Sairam Pothukuchi, Sunilkumar Bhadramma Kochunarayana Pillai, Ranjan Chakrabarti
  • Patent number: 6388099
    Abstract: The heterologous expression of the OlePKS in Streptomyces lividans, produces 8,8a-deoxyoleandolide, an aglycone precursor of oleandomycin. The co-expression with DEBS in S. lividans of the P450 monooxygenase OleP produces 8,8a-dihydroxy-6-deoxyerythonolide B and other derivatives that are precursors to important macrolide antibiotics.
    Type: Grant
    Filed: January 23, 2001
    Date of Patent: May 14, 2002
    Assignee: Kosan Biosciences, Inc.
    Inventor: Robert McDaniel
  • Patent number: 6387948
    Abstract: 8-Acetylarteminolide of the formula (I) having inhibitory activities against farnesyl-protein transferase(FPTase), a progression of the cell cycle and angiogenesis may be useful for the prevention and treatment of various cancers and angiogenesis-related diseases:
    Type: Grant
    Filed: June 17, 2000
    Date of Patent: May 14, 2002
    Assignee: Korea Research Institute of Bioscience and Biotechnology
    Inventors: Byoung-Mog Kwon, Kwang-Hee Son, Ha-Won Jeong, Seung-Ho Lee, Mi-Young Han, Hyun-Mi Kang, Hyae-Kyeong Kim, Soo-Ik Chang
  • Patent number: 6372781
    Abstract: Spirolaxine, the compound of formula (I) wherein R is H, and the novel compounds of formula (I) wherein R is (C1-C5) alkyl or CH3(CH2)nCO and n is 1, 2, 3 or 4 are useful in treating gastroduodenal diseases such as gastric ulcers, duodenal ulcers and gastric cancer caused by Helicobacter pylori. Spirolaxine and spirolaxine methyl ether are isolated from the fermentation of Sporotrichum pruinosum ATCC 74278. Spirolaxine and the compounds of formula (I) are also useful in combination with H2 antagonist, colloidal bismuth subcitrate and other antibiotics.
    Type: Grant
    Filed: June 7, 2000
    Date of Patent: April 16, 2002
    Assignee: Pfizer Inc.
    Inventors: Mark A. Guadliana, Liang H. Huang, Takushi Kaneko, Paul C. Watts
  • Patent number: 6362168
    Abstract: Compounds of the formula: wherein X represents a single or a double bond; R1 is H or OH; provided that when X is a single bond, R1 is H or OH, and when X is a double bond, R1 is absent; R2 is H, C1-C8 alkyl, C2-C8 alkenyl, C2-C8 alkynyl, alkoxy-alkyl or alkylthioalkyl containing from 1 to 6 carbon atoms in each alkyl or alkoxy group, wherein any of said alkyl, alkoxy alkenyl or alkynyl groups may be substituted by one or more halo atoms; or a C3-C8 cycloalkyl or C5-C8 cycloalkenyl group, either of which may be substituted by methylene or one or more C1-C4 alkyl groups or halo atoms; or a 3 to 6 membered oxygen or sulphur containing heterocyclic ring which may be saturated, or fully or partially unsaturated and which may be substituted by one or more C1-C4 alkyl groups or halo atoms; or a group of the formula SR5 wherein R5 is C1-C8 alkyl, C2-C8 alkenyl, C2-C8 alkynyl, C3-C8 cycloalkyl, C5-C8 cycloalkenyl, phenyl or substituted phenyl wherein the substituent is C1-C4 alkyl, C1-C4 alkoxy or
    Type: Grant
    Filed: June 5, 1995
    Date of Patent: March 26, 2002
    Assignee: Pfizer Inc.
    Inventors: Christopher J. Dutton, Stephen P. Gibson, Shih-Jen E. Lee
  • Patent number: 6355810
    Abstract: Disclosed are multibinding compounds which inhibit 3-hydroxy-3-methylglutaryl coenzyme A reductase (HMG-COA reductase), the rate limiting enzyme in cholesterol biosynthesis. The multibinding compounds of this invention containing from 2 to 10 ligands covalently attached to one or more linkers. Each ligand is a moiety capable of binding to HMG-CoA reductase and the distance between ligands is at least 10 Å. The multibinding compounds of this invention are useful in the treatment and prevention of hypercholesterolemia, hyperlipidemia, atherosclerosis and the like.
    Type: Grant
    Filed: June 4, 1999
    Date of Patent: March 12, 2002
    Assignee: Advanced Medicine, Inc.
    Inventors: John H. Griffin, Michael R. Leadbetter, Donald E. Schmidt, Jr.
  • Patent number: 6355441
    Abstract: Chemiluminescent 1,2-dioxetane compounds capable of producing light energy when decomposed, substantially stable at room temperature, represented by the formulas I or II:
    Type: Grant
    Filed: July 28, 1999
    Date of Patent: March 12, 2002
  • Publication number: 20020019544
    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: Application
    Filed: July 30, 2001
    Publication date: February 14, 2002
    Applicant: BIOAVAILABILITY SYSTEMS, LLC
    Inventor: James W. Harris
  • Patent number: 6309687
    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: August 24, 2000
    Date of Patent: October 30, 2001
    Inventor: James W. Harris
  • Patent number: 6281361
    Abstract: Dibenzonaphthyrone of formula (I) wherein A1 and A2 independently of each other are unsubstituted or mono- to tetra-substituted o-C6-C18arylene, with the proviso that formula (I) does not represent a dibenzonaphthyrone of the formula The invention further relates to processes for the preparation thereof, to the use thereof for colouring/pigmenting high-molecular-weight organic material and to substance compositions comprising dibenzonaphthyrones.
    Type: Grant
    Filed: March 29, 1999
    Date of Patent: August 28, 2001
    Assignee: Ciba Specialty Chemicals Corp.
    Inventors: Peter Nesvadba, Joachim Jandke
  • Patent number: 6255337
    Abstract: First-pass effective substances derived from citrus.
    Type: Grant
    Filed: May 27, 1999
    Date of Patent: July 3, 2001
    Assignee: Bioavailability Systems, L.L.C.
    Inventor: James W. Harris
  • Patent number: 6248776
    Abstract: Safe, effective first-pass inhibiting compounds and citrus-derived substances are provided. Formulations containing the compounds are also provided as are methods for their preparation and for inhibiting the first pass effect.
    Type: Grant
    Filed: February 17, 1999
    Date of Patent: June 19, 2001
    Assignee: Bioavailability Systems, L.L.C.
    Inventor: James W. Harris
  • Patent number: 6239073
    Abstract: Disclosed are compositions and methods for promoting plant growth. The compounds are cyclopropyl-, cyclobutyl-, and cyclopentyl-substituted brassinosteroids having high growth promoting ability. They may be used alone or in combination with other plant growth regulating agents.
    Type: Grant
    Filed: November 4, 1999
    Date of Patent: May 29, 2001
    Assignee: Exelixis Plant Sciences, Inc.
    Inventors: Thomas G. Back, Richard P. Pharis, Suanne K. Nakajima
  • Patent number: 6174710
    Abstract: Spirolaxine, the compound of formula (I) wherein R is H, and the novel compounds of formula (I) wherein R is (C1-C6)alkyl or CH3(CH2)nCO and n is 1, 2, 3 or 4 are useful in treating gastroduodenal diseases such as gastric ulcers, duodenal ulcers and gastric cancer caused by Helicobacter pylori. Spirolaxine and spirolaxine methyl ether are isolated from the fermentation of Sporotrichum pruinosum ATCC 74278. Spirolaxine and the compounds of formula (I) are also useful in combination with H2 antagonist colloidal bismuth subcitrate and other antibiotics.
    Type: Grant
    Filed: January 16, 1997
    Date of Patent: January 16, 2001
    Assignee: Pfizer Inc.
    Inventors: Mark A. Guadliana, Liang H. Huang, Takushi Kaneko, Paul C. Watts
  • Patent number: 6124477
    Abstract: The present inventor has discovered chemical compounds which inhibit the first-pass effect of orally administered drugs in humans; that phototoxic low molecular weight furocoumarins and certain ether-substituted furocoumarins that are naturally present in citrus extracts, juices, byproducts, etc. may be removed therefrom or reduced in concentration without destroying the first-pass effect inhibiting compounds therein, and a method for preparing citrus-based compositions using only FDA or USP acceptable reagents.
    Type: Grant
    Filed: December 30, 1997
    Date of Patent: September 26, 2000
    Assignee: Bioavailability Systems, LLC
    Inventor: James W. Harris