Patents Examined by John Kight
  • Patent number: 6231873
    Abstract: A cosmetic composition on an external treatment agent containing microcapsules, with an average particle size of 0.1 to 2000 &mgr;m, enclosing a hydrophobic component, wherein the microcapsules are composed of a gelatin film swollen with water.
    Type: Grant
    Filed: December 22, 1997
    Date of Patent: May 15, 2001
    Assignee: Shiseido Company, LTD
    Inventors: Akira Noda, Michihiro Yamaguchi, Masanori Aizawa, Yoshimaru Kumano
  • Patent number: 6229018
    Abstract: A process for the preparation of nicotinic acid by the direct oxidation of &bgr;-picoline in the gas phase, wherein water and &bgr;-picoline are fed separately to the catalyst bed and the catalyst is based on a titanium dioxide support which has been prepared by the sulfate method and has a high specific surface area and a vanadium oxide content of from 5 to 50 %.
    Type: Grant
    Filed: August 31, 1999
    Date of Patent: May 8, 2001
    Assignee: Degussa Aktiengesellschaft
    Inventors: Dieter Heinz, Wolfgang Hölderich, Steffen Krill, Wolfgang Böck, Klaus Huthmacher
  • Patent number: 6225316
    Abstract: The invention relates to compounds of the formula wherein R is hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl; R1 is hydrogen or halogen; or R and R1 may be together —CH═CH—CH═CH—; R2 is hydrogen, halogen, trifluoromethyl, lower alkoxy or cyano; R3 is hydrogen, lower alkyl or form a cycloalkyl group; R4 is hydrogen, —N(R5)2, —N(R5)S(O)2-lower alkyl, —N(R5)C(O)R5 or a cyclic tertiary amine of the group R5 is, independently from each other, hydrogen, C3-6-cycloalkyl, benzyl or lower alkyl; R6 is hydrogen, hydroxy, lower alkyl, —N(R5)CO-lower alkyl, hydroxy-lower alkyl, cyano, —CHO or a 5- or 6 membered heterocyclic group, optionally bonded via an alkylene group, X is —C(O)N(R5)—, —(CH2)mO—, —(CH2)mN(R5)—, —N(R5)C(O)—, or —N(R5)(CH2)m—; n is 0-4; and m is 1 or 2; and to pharmaceutically acceptable acid addition salts thereof.
    Type: Grant
    Filed: February 16, 2000
    Date of Patent: May 1, 2001
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Michael Bös, Guido Galley, Thierry Godel, Torsten Hoffmann, Walter Hunkeler, Patrick Schnider, Heinz Stadler
  • Patent number: 6225481
    Abstract: Robustaflavone, intermediates and analogues thereof and a method for synthesizing the same are provided. The method involves constructing apigenin ethers containing functionalities at the 6- and 3′-positions which could be cross-coupled using transition metal catalysis. The method also involves development of a regioselective iodination of an apigenin derivative at the 6-position, formation of an apigenin 3′-boronate using a palladium-catalyzed exchange of the corresponding 3′-iodide with a diboron reagent. Finally, Suzuki coupling to form the sterically congested 6-3′″ biaryl bond of robustaflavone provides access to the desired biflavanoid system. Robustaflavone intermediates and analogues may be used to prepare analogues of other biflavanoids such as hinokifavone, rhusflavone and succedaneaflavone.
    Type: Grant
    Filed: August 21, 1998
    Date of Patent: May 1, 2001
    Assignee: Advanced Life Sciences, Inc.
    Inventors: David E. Zembower, Heping Zhang, Michael T. Flavin, Yuh-Meei Lin
  • Patent number: 6225473
    Abstract: Disclosed is a method for producing (−)cis-3-hydroxy-1-methyl-4-(2,4,6-trimethoxyphenyl)-piperidine characterised in that 1-methyl-piperidine-4-one is converted into hydrobromide, subsequently transformed with bromine into 3(R,S)-bromine-1-methyl-4-oxo-pyridine-hydrobromide and reacted with 1,3,5-trimethoxyphenyl to form 3(R,S)-bromine-1-methyl-4-(2,4,6-trimethoxyphenyl)-1,2,3,6-tetrahydro-pyridine-hydrobromide. By stirring the reaction solution into an organic solvent, 3(R,S)-bromine-1-methyl-4-(2,4,6-trimethoxyphenyl)-1,2,3,6-tetrahydro-pyridine-hydrobromide is initially isolated as a solid and subsequently the product is mixed with water and converted into 3(R,S)-hydroxy-1-methyl-4-(2,4,6-trimethoxyphenyl)-1,2,3,6-tetrahydro-pyridine by means of stirring.
    Type: Grant
    Filed: July 21, 2000
    Date of Patent: May 1, 2001
    Assignee: Aventis Pharma Deutschland GmbH
    Inventors: Gerhard Breipohl, Jürgen Michalowsky
  • Patent number: 6225477
    Abstract: This invention relates to a method of improving the catalytic performance of palladium or ruthenium, rhenium-on-carbon hydrogenation catalysts operating in aqueous media where loss of soluble rhenium may result in rapid catalytic failure. A rhenium-containing hydrogenation catalyst comprised of rhenium on a support material is regenerated by first treating the catalyst with aqueous perrhenic acid or potassium perrhenate followed by treating the catalyst under reducing conditions at elevated temperature and pressure. Treatment of the catalyst as described replenishes dispersed fresh finely divided rhenium which enhances the activity of the catalyst while at the same time allowing the operations to be carried out in situ in the hydrogenation reactor or in a side stream reactor with significant savings in reducing reactor down time and precious metal expenses.
    Type: Grant
    Filed: February 4, 1998
    Date of Patent: May 1, 2001
    Assignee: E. I. du Pont de Nemours and Company
    Inventors: Richard Edward Ernst, John Byrne Michel, Daniel Campos
  • Patent number: 6224734
    Abstract: The invention provides novel mepiquat plant growth regulator compositions which have improved hygroscopicity and corrosion characteristics. The novel mepiquat plant growth regulator compositions of the invention can be readily prepared from technical mepiquat chlorid inter alia by electrochemical ion exchange processes or by quaternization of N-methylpiperidine with dimethylcarbonate as starting material.
    Type: Grant
    Filed: September 22, 1999
    Date of Patent: May 1, 2001
    Assignees: BASF Aktiengesellschaft, BASF Corporation
    Inventors: Reiner Kober, David G. Hobbs, Scott W. Gibson, Kenneth Eugene Fersch, Wilhelm Rademacher, Jörg Botzem, Markus Frede, Matthias Dernbach, Reimer Göttsche, Reinhard Dötzer
  • Patent number: 6218541
    Abstract: A method for obtaining purified bisbenzylisoquinoline alkaloids from the roots of Stephania Tetrandra involves obtaining, from the roots of Stephania Tetrandra, a precipitate comprising tetrandrine, fangchinoline and compounds which constitute impurities, contacting the precipitate with chloroform to form a chloroform solution in which tetrandrine and fangchinoline is dissolved, separating the chloroform solution containing dissolved tetrandrine and fangchinoline from undissolved impurities, removing chloroform from the chloroform solution to obtain a chloroform extract solid having an enriched tetrandrine and fangchinoline content relative to the precipitate, contacting the chloroform extract solid with cool benzene to form a combination comprising undissolved fangchinoline and a benzene solution in which tetrandrine is dissolved, separating the benzene solution from the undissolved fangchinoline from the first solid, removing benzene from the first benzene solution to form a benzene extract which comprises
    Type: Grant
    Filed: June 28, 1999
    Date of Patent: April 17, 2001
    Assignee: CBA, International, Inc.
    Inventor: Zhishuang Wang
  • Patent number: 6218429
    Abstract: A compound of the formula: wherein R1 is an optionally substituted hydrocarbon, amino or heterocyclic group; R2 is H or an optionally substituted hydrocarbon group; R3 is H or an optionally substituted hydrocarbon or heterocyclic group; X is CHR4, NR4, O or S in which R4 is H or an optionally substituted hydrocarbon group; Y is C, CH or N; ring A is optionally substituted 5- to 7-membered ring; ring B is an optionally substituted benzene ring; and m is 1 to 4, or a salt thereof, a process for producing it, an intermediate for the production and a pharmaceutical composition comprising it are provided.
    Type: Grant
    Filed: May 10, 1999
    Date of Patent: April 17, 2001
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Shigenori Ohkawa, Osamu Uchikawa, Kohji Fukatsu, Masaomi Miyamoto
  • Patent number: 6218389
    Abstract: The invention provides compounds of formula as described in the claims, or an optical isomer, diastereomer or enantiomer thereof, or a pharmaceutically-acceptable salt, or biohydrolyzable amide, ester, or imide thereof are useful as inhibitors of metalloproteases. Also disclosed are pharmaceutical compositions and methods of treating diseases, disorders and conditions characterized by metalloprotease activity using these compounds or the pharmaceutical compositions containing them.
    Type: Grant
    Filed: July 31, 1998
    Date of Patent: April 17, 2001
    Assignee: The Procter & Gamble Co.
    Inventors: Neil Gregory Almstead, Roger Gunnard Bookland, Yetunde Olabisi Taiwo, Rimma Sandler Bradley, Rodney Dean Bush, Biswanath De, Michael George Natchus, Stanislaw Pikul
  • Patent number: 6211374
    Abstract: The present invention provides water-soluble, pyran-based photochromic compounds characterized by improved stability when in an open, excited configuration. The advantages of the present invention are provided, at least in part, by functionalizing a pyran-based photochromic compound with carboxylate functionality in such a way that the carboxylate and/or its counter ion have sufficient mobility to engage in intermolecular and intramolecular interactions. In preferred embodiments, such a mobile carboxylate and/or counter ion provided on one side of an open pyran ring is preferably capable of complexing with functionality on the other side of the open pyran ring, greatly stabilizing the open configuration.
    Type: Grant
    Filed: April 22, 1998
    Date of Patent: April 3, 2001
    Inventor: Joseph Thomas Ippoliti
  • Patent number: 6211378
    Abstract: An environmentally friendly process for the preparation of the 4-functionalized N—OR derivatives of 2,2,6,6-tetraalkylpiperidines involves the hydrogen peroxide of the corresponding N—H compound to form the corresponding N-oxyl derivative, reacting two equivalents of the N-oxyl compound with one equivalent of a compound having an allylic hydrogen, a benzylic hydrogen or an activated methine hydrogen to form one equivalent of the corresponding N—OH compound and one equivalent of the corresponding N—OR compound, and recycling the N—OH compound back to the corresponding N-oxyl compound using hydrogen peroxide or air.
    Type: Grant
    Filed: May 20, 1999
    Date of Patent: April 3, 2001
    Assignee: Ciba Specialty Chemicals Corporation
    Inventors: Joseph E. Babiarz, Stephen D. Pastor, Glen T. Cunkle
  • Patent number: 6207833
    Abstract: The invention relates to a single stage method for preparing 2-(quinolylthio)acetic acid and its salts by reacting 2-chloroquinoline and mercaptoacetic acid
    Type: Grant
    Filed: June 23, 2000
    Date of Patent: March 27, 2001
    Assignee: Loba Feinchemie AG
    Inventor: Herbert Koller
  • Patent number: 6207834
    Abstract: A process for producing piperidinecarboylic acid amide derivatives useful as serotonin antagonists, antithrombocytic agents or intermediates for them, which comprises the step of reacting a 2-oxazoline compound with a piperidine derivative in the presence of an acid is provided. This process is an industrially excellent process for producing piperidinecarboylic acid amide derivatives useful as serotonin antagonists, antithrombocytic agents or intermediates for them.
    Type: Grant
    Filed: October 12, 1999
    Date of Patent: March 27, 2001
    Assignee: Ajinomoto Co., Inc.
    Inventors: Isao Arai, Takashi Yamamoto, Hirokazu Naora
  • Patent number: 6207839
    Abstract: A process for reacting olefinic compounds, certain carboxylic reactants, and aldehydes or ketones and products prepared by the process. The compositions of the process are useful as intermediates for the preparation of additives for lubricants and fuels.
    Type: Grant
    Filed: August 5, 1998
    Date of Patent: March 27, 2001
    Assignee: The Lubrizol Corporation
    Inventor: Mark R. Baker
  • Patent number: 6204274
    Abstract: The present invention provides compounds of the formula (1): wherein R1 and R2 each independently represent hydrogen, hydroxy, F, Cl, Br, I, CN, 1 to 6 carbon alkyl, 1 to 6 carbon alkoxy, nitro, CF3 and phenyloxy or benzyloxy, in which the aromatic ring can be optionally substituted by from 1 to 3 groups selected from C1-C6 alkoxy (preferably OMe), F, Cl, Br, I, and CF3; R3 and R4 are each independently a hydrogen, a 1 to 6 carbon alkyl or a CH2Ph in which the phenyl ring can be optionally substituted by from 1 to 3 groups selected from C1-C6 alkoxy (preferably OMe), F, Cl, Br, I, and CF3; Y is selected from CH2 or CH and, X is selected from a group represented by N, CR3, CHR3, CHCH; or a pharmaceutically acceptable salt thereof, as well as pharmaceutical compositions and methods of using the compounds to treat central nervous system disorders, such as depression, anxiety, drug withdrawal, eating and sexual disorders and other conditions for which serotonin reuptake inhibitors are used.
    Type: Grant
    Filed: April 23, 1999
    Date of Patent: March 20, 2001
    Assignee: American Home Products Corporation
    Inventors: Michael G. Kelly, Young H. Kang
  • Patent number: 6204257
    Abstract: The present invention is directed to novel water-soluble prodrugs of aliphatic or aromatic hindered hydroxyl group containing pharmaceuticals.
    Type: Grant
    Filed: August 7, 1998
    Date of Patent: March 20, 2001
    Assignee: Universtiy of Kansas
    Inventors: Valentino J. Stella, Jan J. Zygmunt, Ingrid Gunda Georg, Muhammad S. Safadi
  • Patent number: 6200996
    Abstract: Compounds of the formula: are useful in treating disease conditions mediated by TNF-&agr; such as rheumatoid arthritis, osteoarthritis, sepsis, AIDS, ulcerative colitis, multiple sclerosis, Crohn's disease and degenerative cartilage loss.
    Type: Grant
    Filed: January 27, 2000
    Date of Patent: March 13, 2001
    Assignee: American Cyanamid Company
    Inventors: Jeremy I. Levin, James M. Chen, Frances C. Nelson
  • Patent number: 6197961
    Abstract: At least one of a Rh catalyst, a Pd catalyst or a Ru catalyst is used as a catalyst in preparing the salt of &ggr;-(piperidyl)-butyric acid (2) by hydrogenating the salt of &ggr;-(pyridyl)butyric acid (1) [preferably the salt of &ggr;-(pyridyl)butyric acid (1) obtained in the undermentioned steps (a) and (b) and containing not more than 3% by weight of salt of bis(pyridylethyl)acetic acid (3)] in a solvent in the presence of a catalyst: (a) reacting the vinylpyridine (4) with the diester of malonic acid (5) in the presence of a base to give the 2-(pyridylethyl)malonic acid diester (6), and (b) hydrolyzing and decarboxylating the 2-(pyridylethyl)malonic acid diester (6) obtained in the step (a) in an acidic aqueous solution to give the salt of &ggr;-(pyridyl)butyric acid (1).
    Type: Grant
    Filed: June 4, 1998
    Date of Patent: March 6, 2001
    Assignee: Koei Chemical Co., Ltd.
    Inventors: Toshito Sakai, Masayo Nagaoka, Ken Kanno
  • Patent number: 6197978
    Abstract: A process for the manufacture of the racemic compound of the formula (I), its R-enantiomer (formula R-(I)) and its S-enantiomer (formula S-(I)), and pharmaceutically acceptable salts and/or solvates thereof, as well as new intermediates obtained and used in the process.
    Type: Grant
    Filed: May 6, 1998
    Date of Patent: March 6, 2001
    Assignee: Astra Aktiebolag
    Inventors: Sverker Hanson, Lars Johansson, Daniel D. Sohn