Benzene Ring Bonded Directly To The Carbonyl Patents (Class 558/415)
  • Patent number: 6639093
    Abstract: The invention relates to the preparation of hydroxybenzoic benzyl esters by reacting benzyl chloride with hydroxybenzoic acids in the presence of one or more amides.
    Type: Grant
    Filed: April 5, 2002
    Date of Patent: October 28, 2003
    Assignee: Bayer Aktiengesellschaft
    Inventors: Pieter Ooms, Bernd-Ulrich Schenke
  • Patent number: 6630607
    Abstract: Aromatic methylidene compounds of the following general formula wherein R11 and R21 independently in each occurrence represent an unsubstituted or substituted alkyl or alkoxy group, a halogen, a cyano group or a nitro group, n11 and n21 are, respectively, an integer, R31 and R41 independently represent hydrogen, an unsubstituted or substituted alkyl group, an unsubstituted or substituted cycloalkyl group, an unsubstituted or substituted aromatic group, or an unsubstituted or substituted aromatic heterocyclic group and may join to complete a condensed ring, along with other types of aromatic methylidene compounds wherein the moieties attached to the naphthalene ring are attached to different positions of the ring. The preparation of the methylidene compounds is also described along with intermediate compounds and their preparation.
    Type: Grant
    Filed: January 24, 2002
    Date of Patent: October 7, 2003
    Assignee: Matsushita Electric Industrial Co., Ltd.
    Inventor: Mitsuru Hashimoto
  • Publication number: 20030176721
    Abstract: The invention relates to a method for the production of trifluoroethoxy-substituted benzoic acids, by reaction of a corresponding halogenated benzoic acid with trifluoroethanol in the solvent tetrahydrofuran, in the presence of a base and a copper salt, followed by an acidic work-up.
    Type: Application
    Filed: November 21, 2002
    Publication date: September 18, 2003
    Inventors: Kai Fabian, Steffen Enke, Herbert Tilly
  • Patent number: 6599861
    Abstract: Compounds of formula I wherein the substituents are defined as in claim 1, as well as the agronomically acceptable salts, isomers and enantiomers of these compounds, as well as the agronomically acceptable salts/N-oxides/isomers/enantiomers of these compounds, are eminently suitable for use as herbicides.
    Type: Grant
    Filed: June 21, 2001
    Date of Patent: July 29, 2003
    Assignee: Syngenta Participations AG
    Inventors: Jürgen Schaetzer, Alain De Mesmaeker, Shy-Fuh Lee
  • Publication number: 20030139390
    Abstract: Modulators of PPAR&ggr; activity are provided which are useful in pharmaceutical compositions and methods for the treatment of conditions such as type II diabetes and obesity.
    Type: Application
    Filed: July 30, 2002
    Publication date: July 24, 2003
    Applicant: Tularik Inc.
    Inventors: Lawrence R. McGee, Jonathan B. Houze, Steven M. Rubenstein
  • Publication number: 20030130537
    Abstract: The present invention relates to a process for preparing substituted benzoyl chlorides of the formula (1) 1
    Type: Application
    Filed: October 3, 2002
    Publication date: July 10, 2003
    Applicant: Clariant GmbH
    Inventors: Lars Bierer, Joachim Ritzer, Berthold Schiemenz, Thomas Wessel
  • Publication number: 20030130527
    Abstract: Method for the preparation of 1-(3-dimethylaminopropyl)-1-(4-fluorophenyl)-1,3-dihydroisobenzofuran-5-carbonitrile (citalopram) comprising the reaction of a compound of formula 1
    Type: Application
    Filed: February 24, 2003
    Publication date: July 10, 2003
    Applicant: ORION CORPORATION FERMION
    Inventors: Leif Hilden, Tuomas Huuhtanen, Petteri Rummakko, Arne Grumann, Pekka Pietikaeinen
  • Patent number: 6579993
    Abstract: Method for the preparation of 1-(3-dimethylaminopropyl)-1-(4-fluoro-phenyl)-1,3-dihydroisobenzofuran-5-carbonitrile (citalopram) comprising the reaction of a compound of formula wherein X is a halogen, with organometallic dimethylaminopropyl halide. Other aspects of the invention are new compounds of formula II and formula III and their preparation.
    Type: Grant
    Filed: January 30, 2002
    Date of Patent: June 17, 2003
    Assignee: Orion Corporation, Fermion
    Inventors: Leif Hilden, Tuomas Huuhtanen, Petteri Rummakko, Arne Grumann, Pekka Pietikaeinen
  • Patent number: 6569899
    Abstract: Aminobutylic acid derivatives of the formula (I) wherein the symbols are as defined in specification; and non-toxic salts thereof. Because of inhibiting matrix metalloproteinase, the compounds of the formula (I) are useful for prevention and/or treatment of diseases, for example, rheumatoid diseases, arthrosteitis, osteoarthritis, unusual bone resorption, osteoporosis, periodontitis, interstitial nephritis, arteriosclerosis, pulmonary emphysema, cirrhosis, cornea injury, cornea ulcer, metastasis, invasion or growth of tumor cells, autoimmune disease, disease caused by vascular emigration or infiltration of leukocytes, arterialization, multiple sclerosis, arota aneurysm, endometriosis, restenosis after PTCA, unstable angina, acute myocardial infarction, transient ischemic attack.
    Type: Grant
    Filed: October 5, 2001
    Date of Patent: May 27, 2003
    Assignee: Ono Pharmaceuticals Co., Ltd.
    Inventors: Kanji Takahashi, Tsuneyuki Sugiura
  • Publication number: 20030096992
    Abstract: The present invention relates to a method of preparing an alkylated salicylamide from a protected and activated salicylamide via a dicarboxylated salicylamide intermediate. The present invention also relates to dicarboxylic salicylamide delivery agent compounds for the delivery of active agents. Methods of administration are provided as well.
    Type: Application
    Filed: September 20, 2002
    Publication date: May 22, 2003
    Inventors: Joseph N. Bernadino, Doris C. O'Toole, William E. Bay
  • Patent number: 6566403
    Abstract: This invention relates to new compositions comprising predominantly one enantiomer of an N-acetonylbenzamide fungicide, methods of preparing N-acetonylbenzamides, and their use as fungicides.
    Type: Grant
    Filed: June 16, 1997
    Date of Patent: May 20, 2003
    Assignee: Dow AgroSciences LLC
    Inventors: Enrique Luis Michelotti, David Hamilton Young, Thomas Anthony McLaughlin
  • Publication number: 20030092747
    Abstract: The present invention relates to compounds of formula (I): 1
    Type: Application
    Filed: June 13, 2002
    Publication date: May 15, 2003
    Inventors: Heinrich Josef Schostarez, Robert Alan Chrusciel
  • Publication number: 20030092929
    Abstract: The present invention relates to 3-cyano-2,4,5-trifluorobenzoyl fluoride and to intermediates for its preparation and to the process for the preparation of 3-cyano-2,4,5-trifluoro-benzoyl fluoride, which starts from 5-fluoro-1,3-xylene (VIII); which is bichlorinated in the ring in the presence of a catalyst under ionic conditions to give 2,4-dichloro-5-fluoro-1,3-dimethylbenzene (VII). The latter is chlorinated in the side chains under free-radical conditions to give 2,4-dichloro-5-fluoro-3-dichloromethyl-1-trichloromethylbenzene (VI).
    Type: Application
    Filed: October 22, 2002
    Publication date: May 15, 2003
    Inventors: Albrecht Marhold, Peter Wolfrum
  • Patent number: 6562807
    Abstract: A novel class of compounds, which act to antagonize the action of the glucagon hormone on the glucagon receptor. Owing to their antagonizing effect of the glucagon receptor the compounds may be suitable for the treatment and/or prevention of any diseases and disorders, wherein a glucagon antagonistic action is beneficial, such as hyperglycemia, Type 1 diabetes, Type 2 diabetes, disorders of the lipid metabolism, such as dyslipidemia, and obesity.
    Type: Grant
    Filed: June 22, 2001
    Date of Patent: May 13, 2003
    Assignee: Novo Nordisk A/S
    Inventors: Anker Steen Jorgensen, Inge Thoger Christensen, Janos Tibor Kodra, Christian Sams, Carsten Behrens, Peter Madsen, Jesper Lau
  • Publication number: 20030088104
    Abstract: A novel achiral biaryl-type compound and a circular dichroism(CD) color fixing agent are provided. Furthermore, a method for determining an absolute configuration of a chiral compound is carried out by introducing the above achiral biaryl-type compound into the chiral compound.
    Type: Application
    Filed: February 26, 2002
    Publication date: May 8, 2003
    Applicant: KANAZAWA UNIVERSITY
    Inventors: Tomihisa Ohta, Shinzo Hosoi
  • Publication number: 20030078428
    Abstract: Phenylamino benzhydroxamic acid derivatives of formula (I) where R1, R2, R3, R4, R5, and R6 are hydrogen or substituent groups such as alkyl, and where R7 is hydrogen or an organic radical, are potent inhibitors of MEK and, as such, are effective in treating cancer and other proliferative diseases such as psoriasis and restenosis.
    Type: Application
    Filed: June 4, 2002
    Publication date: April 24, 2003
    Inventors: Stephen Douglas Barrett, Alexander James Bridges, Annette Marian Doherty, David Thomas Dudley, Alan Robert Saltiel, Haile Tecle
  • Patent number: 6541670
    Abstract: A compound of the general formula I wherein R1 represents a substituent selected from the group consisting of halogen, hydroxy, mercapto, trifluoromethyl, amino, (C1-C3)alkyl, (C2-C3)olefinic group, (C1-C3)alkoxy, (C1-C3)alkylthio, (C1-C6)alkylamino, (C1-C3)alkoxycarbonyl, cyano, —CONH2, phenyl, and nitro; R2 represents one or more, same or different substituents selected from the group consisting of hydrogen, halogen, hydroxy, mercapto, trifluoromethyl, amino, (C1-C3)alkyl, (C2-C3)olefinic group, (C1-C3)alkoxy, (C1-C3)alkylthio, (C1-C6)alkylamino, (C1-C3)alkoxycarbonyl, cyano, —CONH2, phenyl, and nitro; R3 represents one or more, same or different substituents selected from the group consisting of hydrogen, halogen, hydroxy, mercapto, trifluoromethyl, cyano, carboxy, carbamoyl, (C1-C10)alkyl, (C2-C10)olefinic group, (C3-C8)monocyclic hydrocarbon group, (C1-C10)alkoxy, (C1-C10)alkylthio, (C1-C10)alkoxycarbonyl, and phenyl; R4 represents hydrogen, (C1-C6)alkyl, (C2-C6)olefinic
    Type: Grant
    Filed: March 20, 2001
    Date of Patent: April 1, 2003
    Assignee: Leo Pharmaceutical Products Ltd. A/S
    Inventor: Erik Rytter Ottosen
  • Publication number: 20030060651
    Abstract: Benzoylcyclohexanedione derivatives of the formula (I) and their use as herbicides are described.
    Type: Application
    Filed: April 4, 2002
    Publication date: March 27, 2003
    Inventors: Thomas Seitz, Andreas van Almsick, Lothar Willms, Thomas Auler, Herman Bieringer, Hubert Menne
  • Publication number: 20030055287
    Abstract: The present invention provides a phthalic acid diamide derivative represented by the general formula (I) 1
    Type: Application
    Filed: January 4, 2002
    Publication date: March 20, 2003
    Inventors: Masanori Tohnishi, Hayami Nakao, Eiji Kohno, Tateki Nishida, Takashi Furuya, Toshiaki Shimizu, Akira Seo, Kazuyuki Sakata, Shinsuke Fujioka, Hideo Kanno
  • Publication number: 20030022934
    Abstract: The invention relates to novel phenoxyphenyl alkanesulphonates, processes for their preparation, their use for producing medicaments for the treatment and/or prophylaxis of diseases, in particular for the treatment of states of pain and neurodegenerative disorders
    Type: Application
    Filed: September 26, 2001
    Publication date: January 30, 2003
    Inventors: Markus Heil, Heinrich Meier, Paul Naab, Arnd Voerste, Jean-Marie-Viktor De Vry, Dirk Denzer, Frank Mauler, Klemens Lustig, Jan-Bernd Lenfers
  • Patent number: 6485799
    Abstract: A aniline derivative represented by general formula (1) wherein R and R′ represent independently each other alkyl with 1 to 10 carbon, alkoxyalkyl with 1 to 10 carbon, or hydrogen; x represents cyano, halogen, haloalkyl, haloalkyloxy, or 2-cyanoethynyl; Y represents fluorine or hydrogen; na and nc represent independently each other 0 or 1; Za, Zb, and Zc represent independently each other a single bond, 1,2-ethylene, carbonyloxy, or oxymethylene; ring A1 represents 1,4-phenylene in which hydrogen may be substituted by fluorine; ring A2 and ring A3 represent independently each other 1,4-cyclohexylene, 1,4-phenylene in which hydrogen may be substituted by fluorine, or 1,3-pyrimidine-2,5-diyl.
    Type: Grant
    Filed: July 24, 2000
    Date of Patent: November 26, 2002
    Assignee: Chisso Corporation
    Inventors: Atsuko Fujita, Norio Tamura, Hiroyuki Tekeuchi, Fusayuki Takeshita, Nobumasa Nakamura, Etsuo Nakagawa
  • Publication number: 20020161237
    Abstract: Compounds of formula 1 and 1-1, 1
    Type: Application
    Filed: January 5, 2001
    Publication date: October 31, 2002
    Inventors: Nader Fotouhi, Paul Gillespie, Robert William Guthrie, Sherrie Lynn Pietranico-Cole, Weiya Yun
  • Publication number: 20020147204
    Abstract: A compound of the formula: 1
    Type: Application
    Filed: March 26, 2002
    Publication date: October 10, 2002
    Applicant: Sumitomo Pharmaceuticals Company, Limited
    Inventors: Kazuhito Ikeda, Tohru Tatsuno, Hiroki Ogo, Toshio Nishihara, Tatsuya Fujibayashi, Ryu Nagata
  • Patent number: 6441177
    Abstract: Tertiary amines of the formula wherein A1, A2, A3, A4, M, p, T and Q are as defined herein, and acid addition salts thereof, have antimycotic and cholesterol-lowering activity.
    Type: Grant
    Filed: December 16, 1999
    Date of Patent: August 27, 2002
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Johannes Aebi, Henrietta Dehmlow, Jacques Himber, Synèse Jolidon, Hans Lengsfeld, Olivier Morand, Gérard Schmid, Yu-Hua Ji
  • Patent number: 6433211
    Abstract: A process for producing a cyanobenzoic acid compound, a cyanobenzamide compound, an alkyl cyanobenzoate compound, and a cyanobenzoyl chloride compound, which are useful intermediates for a variety of chemicals such as pharmaceuticals, agrochemicals, liquid crystals, and monomers for functional polymers. One nitrile group of an easily available phthalonitrile compound is selectively hydrolyzed to thereby produce a cyanobenzamide compound with high selectivity and yield. The cyanobenzamide compound thus-produced is transformed under acidic conditions into a cyanobenzoic acid compound and a cyanobenzoate ester compound without the cyano group of the benzene ring being damaged.
    Type: Grant
    Filed: September 24, 1999
    Date of Patent: August 13, 2002
    Assignee: Showa Denko Kabushiki Kaisha
    Inventors: Hiroshi Yasuda, Haruaki Ito, Takashi Tani, Kimitaka Ohshiro, Makoto Saito, Sumio Soya, Kuniomi Marumo
  • Patent number: 6410794
    Abstract: Improved processes for preparation of tetralones in high enantiomeric purity centers on resolution using simulated moving bed chromatography of a racemic tetralone derivative. Resolution is effected with high enantiomeric purity, and subsequent reactions of the desired tetralone derivative enantiomer performed with high optical specificity to maintain enantiomeric purity. The undesired enantiomer may be racemized and recycled to the resolution phase to avoid loss.
    Type: Grant
    Filed: November 3, 2000
    Date of Patent: June 25, 2002
    Assignee: UOP LLC
    Inventors: Herman A. Zinnen, Mark J. Gattuso
  • Patent number: 6407267
    Abstract: A method for the preparation of citalopram comprising reaction of a compound of Formula (IV), wherein R is C1-6 alkyl, acyl, C1-6 alkylsulfonyl or arylsulfonyl, with 3-(N,N-dimethylamino)-propyl magnesium halide, to prepare citalopram.
    Type: Grant
    Filed: June 25, 2001
    Date of Patent: June 18, 2002
    Assignee: H. Lundbeck A/S
    Inventors: Michael Harold Rock, Hans Petersen, Peter Ellegaard
  • Patent number: 6407288
    Abstract: The present invention discloses novel naphthylsalicylanilides of the general formula wherein W is a substituted or unsubstituted naphthyl ring. The substitution on W includes replacing one or more —H with —OH, alkyl, O-alkyl, branched alkyl, or cycloalkyl, containing 1-6 carbon atoms or combinations thereof. Y is a substituted or unsubstituted phenyl ring or substituted or unsubstituted naphthyl ring. The substitution for Y includes replacement of one or more —H atoms with CN, CF3, NO2, methoxy, benzoyl, phenoxy, phenoxymethyl or combinations thereof. These compounds are useful as antibacterial against gram negative and gram positive bacteria and as antiinflammatory agents.
    Type: Grant
    Filed: October 2, 2001
    Date of Patent: June 18, 2002
    Assignee: The Research Foundation of State University of New York
    Inventors: Robert A. Coburn, Richard T. Evans, Robert J. Genco
  • Publication number: 20020072500
    Abstract: The present invention relates to a class of compounds represented by the Formula I.
    Type: Application
    Filed: September 26, 2001
    Publication date: June 13, 2002
    Inventors: Thomas Rogers, Thomas D. Penning, Lan Jiang, Balekudru Devadas, Peter Ruminiski, Jennifer VanCamp, Chester Yuan
  • Patent number: 6372693
    Abstract: The invention relates to 2-(3-alkenylbenzoyl)cyclohexane-1,3-diones of the formula I where the variables have the following meanings: R1, R2 are hydrogen, nitro, halogen, cyano, thiocyanato, alkyl, haloalkyl, alkoxyalkyl, alkenyl, alkynyl, —OR6, —OCOR7, —OSO2R7, —SH, —S(O)nR8, —SO2OR6, —SO2NR6R9, —NR9SO2R7 or —NR9COR7; R3 is hydrogen, halogen, alkyl, haloalkyl, alkoxy, alkenyl, alkynyl; R4, R5 are hydrogen, nitro, halogen, cyano, thiocyanato, alkyl, haloalkyl, cycloalkyl, alkenyl, cycloalkenyl, alkynyl, alkoxy, alkylthio, haloalkoxy, —COR10, —CO2R10, —COSR10, —CONR10R11, —C(R12)═NR13, —PO(OR10)(OR11); unsubstituted or substituted alkyl, heterocyclyl, heterocyclylalkyl, phenyl, phenylalkyl, hetaryl or hetarylalkyl; or R4 and R5 together form an alkanediyl chain which can be substituted and/or can be interrupted by a hetero atom; Q is an unsubstituted or substituted cyclohexane-1,3-dione ring wh
    Type: Grant
    Filed: November 2, 1999
    Date of Patent: April 16, 2002
    Assignee: BASF Aktiengesellschaft
    Inventors: Ernst Baumann, Wolfgang von Deyn, Stefan Engel, Regina Luise Hill, Uwe Kardorff, Guido Mayer, Martina Otten, Michael Rack, Joachim Rheinheimer, Matthias Witschel, Karl-Otto Westphalen, Ulf Misslitz, Helmut Walter
  • Patent number: 6369273
    Abstract: The use of a compound of the formula (I): wherein: ring C is phenyl or carbon-linked heteroaryl selected from pyridyl, pyrazinyl, pyrimidinyl and pyridazinyl; and wherein said phenyl or heteroaryl is substituted as defined herein; A—B is selected from NHCO, OCH2, SCH2, NHCH2, trans-vinylene, and ethynylene; R1 is linked to ring C at a carbon ortho to the position of A—B attachment and is defined herein; n is 1 or 2; R2 and R3 are alkyl, haloalkyl or together from cycloalkyl or halocycloalkyl as defined herein; in the manufacture of a medicament for use in the elevation of PDH activity in warm-blooded animals such as humans is described. Salts and esters of compounds of formula (I) are also described.
    Type: Grant
    Filed: August 2, 2000
    Date of Patent: April 9, 2002
    Assignee: AstraZeneca AB
    Inventor: Roger J Butlin
  • Publication number: 20020040158
    Abstract: The present invention relates to a process for preparing substituted benzoyl chlorides of the formula (1) 1
    Type: Application
    Filed: July 26, 2001
    Publication date: April 4, 2002
    Applicant: Clariant GmbH
    Inventors: Lars Bierer, Joachim Ritzer, Berthold Schiemenz, Thomas Wessel
  • Publication number: 20020032178
    Abstract: Salicylic acid derivatives of the formula I, 1
    Type: Application
    Filed: July 2, 2001
    Publication date: March 14, 2002
    Inventors: Andreas Gypser, Thomas Grote, Joachim Rheimheimer, Ingo Rose, Oliver Cullmann, Markus Gewehr, Wassilios Grammenos, Jordi Tormo i Blasco, Bernd Muller, Hubert Sauter, Eberhard Ammermann, Siegfried Strathmann, Gisela Lorenz, Reinhard Stierl
  • Patent number: 6355490
    Abstract: The present invention relates to a process of coding and identifying individual members of a chemical combinatorial library synthesized on a plurality of solid supports which undergo mix and split synthesis. The process provides for tagging the solid supports with a coding identifier that is attached to the solid support and which can be decoded by infrared or raman spectroscopy when directly attached to the support.
    Type: Grant
    Filed: September 4, 1997
    Date of Patent: March 12, 2002
    Inventors: Jill Edie Hochlowski, Thomas J. Sowin, Daniel W. Norbeck, Anne-Laure Marie Grillot, Rolf E. Swenson
  • Patent number: 6346518
    Abstract: The present invention is concerned with the stereoisomeric forms of itraconazole (X=Cl) and saperconazole (X=F), which may be represented by the formula and the pharmaceutically acceptable acid addition salt forms thereof, processes for preparing said stereoisomeric forms, the complexes thereof with cyclodextrin derivatives, pharmaceutical compositions comprising said complexes and methods of preparing said complexes and pharmaceutical compositions.
    Type: Grant
    Filed: January 26, 1995
    Date of Patent: February 12, 2002
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Jan Heeres, Jean Louis Mesens, Jozef Peeters
  • Publication number: 20020015805
    Abstract: The invention relates to a fluoro-substituted alkenyl compound represented by formula (1) 1
    Type: Application
    Filed: May 22, 2001
    Publication date: February 7, 2002
    Inventors: Yasuhiro Haseba, Shuichi Matsui, Hiroyuki Takeuchi, Yasuhiro Kubo, Etsuo Nakagawa
  • Publication number: 20020016491
    Abstract: A method of selectively controlling undesirable vegetation in crops by using a postemergent application of an herbicidally effective amount of a metal chelate of a 2-(substituted benzoyl)-1,3-cyclohexanedione compound to the locus of such undesirable vegetation.
    Type: Application
    Filed: May 28, 1999
    Publication date: February 7, 2002
    Inventors: HERBERT B. SCHER, JINLING CHEN
  • Publication number: 20020016347
    Abstract: Heteroaryl aminobenzophenones of general formula I inhibit interleukin-1&bgr; and TNF-&agr; and may therefore be useful in the therapy of inflammatory diseases and conditions.
    Type: Application
    Filed: May 21, 2001
    Publication date: February 7, 2002
    Inventor: Anne Marie Horneman
  • Patent number: 6329399
    Abstract: Novel amine derivatives having an excellent antimycotic effect represented by general formula (1) below and salts thereof are provided. [in the formula (1, R1 represents a C1-5 alkyl group which may be halogenated, R2 represents 4-(1,1-dimethylalkyl)benzyl group, 4-(1-methyl-phenylethyl)benzyl group, 1-or 2-naphthylmethyl group, or a hydrocarbon group having 3,3-dimethyl-1-butynyl group or a phenyl group at its terminal and 1 to 3 double bonds; R3 represents oxygen atom or a methylene group which may be substituted by a C1-4 alkyl group; and R4 represents 1-or 2 naphthyl group or a phenyl group which may be substituted.
    Type: Grant
    Filed: May 18, 2000
    Date of Patent: December 11, 2001
    Assignee: Pola Chemical Industries, Inc.
    Inventors: Takao Itoh, Takuji Nakashima, Akira Nozawa, Kouji Yokoyama, Hiroyuki Takimoto, Masayuki Yuasa, Yukio Kawazu, Toshimitsu Suzuki, Toshiro Majima
  • Patent number: 6329551
    Abstract: A phenylenediamine derivative represented by following formula (I) or (II): wherein R1 and R2 each represents a hydrogen atom, a lower alkyl group, or a lower alkoxy group; R3 represents a hydrogen atom or a methyl group; R4 represents a methyl group or an ethyl group; and n and m each is 1, 2, or 3; wherein R1 and R2 each represents a hydrogen atom, a lower alkyl group, a lower alkoxy group, or a cyano group; and n and m each is 1, 2, or 3, is disclosed. These phenylenediamine derivatives are effectively used as antioxidants for rubbers, which scarcely cause vanishing by evaporation or a thermal denaturation even under a high-temperature condition of 150° C. or higher.
    Type: Grant
    Filed: April 7, 2000
    Date of Patent: December 11, 2001
    Assignee: NOK Corporation
    Inventors: Seiji Nakagome, Akihiko Toda
  • Patent number: 6326507
    Abstract: Compounds and methods useful for chemopreventative treatment of diseases such as cancer, Alzheimer's disease, Parkinson's disease, inflammatory bowel diseases, and multiple sclerosis.
    Type: Grant
    Filed: June 17, 1999
    Date of Patent: December 4, 2001
    Assignee: Trustees of Dartmouth College
    Inventors: Gordon W. Gribble, Tadashi Honda, Michael B. Sporn, Nanjoo Suh
  • Publication number: 20010023300
    Abstract: The present invention relates to 3-cyano-2,4,5-trifluorobenzoyl fluoride and to intermediates for its preparation and to the process for the preparation of 3-cyano-2,4,5-trifluoro-benzoyl fluoride, which starts from 5-fluoro-1,3-xylene (VIII); which is bichlorinated in the ring in the presence of a catalyst under ionic conditions to give 2,4-dichloro-5-fluoro-1,3-dimethylbenzene (VII). The latter is chlorinated in the side chains under free-radical conditions to give 2,4-dichloro-5-fluoro-3-dichloromethyl-1-trichloromethylbenzene (VI).
    Type: Application
    Filed: March 21, 2001
    Publication date: September 20, 2001
    Inventors: Albrecht Marhold, Peter Wolfrum
  • Patent number: 6278013
    Abstract: Intermediates useful in the preparation of 8-cyano-1-cyclopropyl-7-(2,8-diazabicyclo[4.3.0]nonan-8-yl-6-fluorol,4-dihydro-4-oxo-3-quinolinecarboxylic acids of the following structures are claimed.
    Type: Grant
    Filed: November 21, 2000
    Date of Patent: August 21, 2001
    Assignee: Bayer Aktiengesellschaft
    Inventors: Stefan Bartel, Thomas Jaetsch, Thomas Himmler, Hans-Georg Rast, Werner Hallenbach, Ernst Heinen, Franz Pirro, Martin Scheer, Michael Stegemann, Hans-Peter Stupp, Heinz-Georg Wetzstein
  • Patent number: 6262292
    Abstract: The invention relates to (1) a process for producing a cyanobenzaldehyde compound by converting the aminomethyl group in a cyanobenzylamine compound into an aldehyde group using an oxidizing agent without impairing the cyano group, to (2) a process for producing a cyanobenzoyl halide compound by converting the aldehyde group in a cyanobenzaldehyde compound into an acid halide group without impairing the cyano group, and to (3) a process for producing a cyanobenzoic acid compound by reacting a cyanobenzaldehyde compound with a hypohalogenous compound. According to the present invention, cyanophenyl derivatives that are useful as an intermediate of medical preparations, agricultural chemicals, liquid crystals, functional high molecular monomers and the like can be produced efficiently from raw materials that are obtained without difficulty.
    Type: Grant
    Filed: June 30, 1999
    Date of Patent: July 17, 2001
    Assignee: Showa Denko K.K.
    Inventors: Hiroshi Yasuda, Kimitaka Ohshiro, Kaneo Nozawa, Kohei Morikawa
  • Patent number: 6229040
    Abstract: The present invention relates to 3-cyano-2,4,5-trifluorobenzoyl fluoride and to intermediates for its preparation and to the process for the preparation of 3-cyano-2,4,5-trifluoro-benzoyl fluoride, which starts from 5 fluoro-1,3-xylene (VIII); which is bichlorinated in the ring in the presence of a catalyst under ionic conditions to give 2,4-dichloro-5-fluoro-1,3 dimethylbenzene (VII). The latter is chlorinated in the side chains under free-radical conditions to give 2,4-dichloro-5-fluoro-3-dichloromethyl-1 trichloromethylbenzene (VI).
    Type: Grant
    Filed: October 15, 1999
    Date of Patent: May 8, 2001
    Assignee: Bayer Aktiengesellschaft
    Inventors: Albrecht Marhold, Peter Wolfrum
  • Patent number: 6211234
    Abstract: Compounds of formula (I) are described wherein R1 is hydrogen, -(lower alkyl)q(CO2R6 or OH), —CN, —C(R7)═NOR8, NO2, —O(lower alkyl)R9, —C≡C—R10, —CR11═C(R12)(R13), —C(═O)CH2C(═O)CO2H, —CO(R14), alkylthio, alkylsulphinyl, alkylsulphonyl, carbamoyl, thiocarbamoyl, substituted carbamoyl, substituted thiocarbamoyl, sulphamoyl or an optionally substituted nitrogen-containing ring, m, n, o and p are independently zero or 1 and R2, R3, R4 and R5 are various groups; and physiologically acceptable salts, N-oxides and prodrugs thereof. The compounds have endothelin antagonist activity and are useful as pharmaceuticals.
    Type: Grant
    Filed: June 27, 1997
    Date of Patent: April 3, 2001
    Assignee: Rhone-Poulenc Rorer Limited
    Inventors: Peter Charles Astles, Mark Francis Harper, Neil Victor Harris, Iain McFarlane McLay, Roger John Aitchison Walsh, Richard Alan Lewis, Christopher Smith, Barry Porter, Clive McCarthy
  • Patent number: 6153651
    Abstract: Ortho-substituted benzoylguanidines, process for their preparation, their use as a medicament or diagnostic, and medicament comprising them.Ortho-substituted benzoylguanidines of the formula I ##STR1## in which R(1) to R(4) have the meanings given in the claims, are suitable, as antiarrhythmic pharmaceuticals having a cardioprotective component, for the prophylaxis and treatment of infarction and for the treatment of angina pectoris. They also inhibit, in a preventive manner, the pathophysiological processes associated with the genesis of ischemically induced damage, in particular associated with the triggering of ischemically induced cardiac arrhythmias.
    Type: Grant
    Filed: February 28, 1997
    Date of Patent: November 28, 2000
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Udo Albus, Joachim Brendel, Heinz-Werner Kleemann, Hans Jochen Lang, Wolfgang Scholz, Jan-Robert Schwark, Andreas Weichert
  • Patent number: 6140528
    Abstract: The invention relates to intermediates to herbicidal compounds of formulae (Ia), (Ib) or (Ic): ##STR1##
    Type: Grant
    Filed: November 22, 1999
    Date of Patent: October 31, 2000
    Assignee: Rhone-Poulenc Agriculture Ltd
    Inventor: David William Hawkins
  • Patent number: 6040339
    Abstract: Compounds of formula (I): ##STR1## wherein: R.sup.1 is alkyl; R.sup.2a, R.sup.2b, R.sup.2c and R.sup.2d are the same or different and each is hydrogen, optionally substituted alkyl or various other organic groups; R.sup.3 is alkyl; R.sup.4 is a group of formula (II), (III), (IV), (V), (VI), (VII), (VIII) or (IX): ##STR2## wherein: A.sup.1 is a single bond, alkylene or alkenylene; A.sup.2 is or alkenylene; A.sup.3 is a single bond, alkyleneor alkenylene; R.sup.5a and R.sup.5b are the same or different and each is hydrogen, alkyl or various other groups; R.sup.6 is alkyl or phenyl; R.sup.7 is hydrogen or alkyl; R.sup.8 is alkyl or various other groups; and n is 0 and pharmaceutically acceptable salts thereof have valuable inhibitory activity against acyl-CoA: cholesterol acyl transferase.
    Type: Grant
    Filed: May 28, 1998
    Date of Patent: March 21, 2000
    Assignee: Sankyo Company, Limited
    Inventors: Akira Yoshida, Kozo Oda, Takashi Kasai, Kousei Shimada, Hiroshi Kogen, Ichiro Hayakawa, Sadao Ishihara, Teiichiro Koga, Eiichi Kitazawa, Taro Tokui
  • Patent number: RE37087
    Abstract: There are provided new alkane and alkoxyalkane derivatives of the general formula I in which R1, R2, R3, R4 and A have the meanings given in the description, processes for their preparation and insecticidal and acaricidal compositions containing these compounds.
    Type: Grant
    Filed: June 20, 1991
    Date of Patent: March 6, 2001
    Assignee: Schering Aktiengesellschaft
    Inventors: Helga Franke, Heinrich Franke, Hans-Rudolf Kruger, Hartmut Joppien, Dietrich Baumert, David Giles