Oxy Patents (Class 562/465)
  • Publication number: 20010039365
    Abstract: A method and composition are disclosed for the hydroxylation of aromatic substrates in the presence of oxygen, hydrogen, and a catalyst. In a preferred embodiment, benzene is oxidized to phenol in the presence of oxygen, a vanadium catalyst, and hydrogen. The method is economical, safe, and amenable to commercial scale-up.
    Type: Application
    Filed: January 16, 2001
    Publication date: November 8, 2001
    Inventor: Terence Michael Barnhart
  • Publication number: 20010034450
    Abstract: Compounds of general formula (1): 1
    Type: Application
    Filed: March 5, 2001
    Publication date: October 25, 2001
    Inventors: Rikki Peter Alexander, Graham John Warrellow
  • Patent number: 6242635
    Abstract: A process for producing a 2-aralkyl-3-hydroxypropionic acid (or its ester), comprising the steps of: reacting a 3-hydroxy-2-methylene-3-arylpropionic acid ester, easily obtained by the reaction of an arylaldehyde with an acrylic acid ester, with an acid anhydride to form a 2-aralkylidene-3-acyloxypropionic acid ester; subjecting the same to hydrolysis or alcoholysis; and reducing the resulting 2-aralkylidene-3-hydroxypropionic acid or its ester. The reduction step may be conducted in the presence of a base.
    Type: Grant
    Filed: September 18, 1998
    Date of Patent: June 5, 2001
    Assignee: Ajinomoto Co., Inc.
    Inventors: Takayuki Suzuki, Takayuki Hamada, Kunisuke Izawa
  • Patent number: 6096920
    Abstract: Palladium-catalyzed arylation of an olefin (e.g., ethylene) with an aromatic halide (e.g., 2-bromo-6-methoxynaphthalene, m-bromobenzophenone, or 4-isobutyl-1-bromobenzene) is conducted in specified media. After a special acid or base phase separation procedure, palladium-catalyzed carbonylation of the olefinically-substituted aromatic intermediate is conducted in specified media using CO and water or an alcohol to form arylalkylcarboxylic acid or ester or substituted arylalkylcarboxylic acid or ester (e.g., racemic 2-(6-methoxy-2-naphthyl)propionic acid, 2-(3-benzoylphenyl)propionic acid, or 2-(4-isobutylphenyl)propionic acid). Catalyst recovery procedures enabling recycle of catalyst residues and efficient recovery of amine hydrogen halide scavenger and solvent used in the arylation reaction are described, as well as novel, highly efficient methods of conducting the carbonylation reaction.
    Type: Grant
    Filed: July 8, 1998
    Date of Patent: August 1, 2000
    Assignee: Albemarle Corporation
    Inventors: Robert H. Allen, R. Carl Herndon, Jr., Kannappan C. Chockalingam, W. Dirk Klobucar, Gary D. Focht, Tse-Chong Wu, Gary D. Heidebrecht, Joseph D. McLean, Yaping Zhong, Thorsten W. Brockmann, Ronny W. Lin, William J. Layman, Jr., Ranjit K. Roy
  • Patent number: 6066763
    Abstract: A process for preparing .alpha.-hydroxy acids by heating ammonium salts of .alpha.-hydroxy acids of general formula (I), removing the formed ammonia and water, adding water to the residue, and heating the obtained mixture, wherein R is hydrogen, C.sub.1 -C.sub.6 alkyl, alkyl(C.sub.1 -C.sub.6)thioalkyl (C.sub.1 -C.sub.6), phenyl or the like. This process is freed from the problem of disposal of by-products such as ammonium bisulfate and makes it possible to prepare a free .alpha.-hydroxy acid from an ammonium salt thereof economically and in a high yield.
    Type: Grant
    Filed: August 25, 1998
    Date of Patent: May 23, 2000
    Assignee: Nippon Soda Co., Ltd.
    Inventor: Koichi Hayakawa
  • Patent number: 6001877
    Abstract: The phenylalkan(en)oic acids of the formula: ##STR1## as defined herein, posses an antagonistic activity on leukotriene B.sub.4.
    Type: Grant
    Filed: May 20, 1998
    Date of Patent: December 14, 1999
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Mitoshi Konno, Takahiko Nakae, Nobuyuki Hamanaka
  • Patent number: 5998642
    Abstract: A method of inhibiting parasitic activity is disclosed in which the biosynthesis, structure and/or function of the glycosyl phosphatidylinositol (GPI) anchor of said parasite may be affected by incorporating into said GPI anchor selected analogs of myristic acid containing various heteroatoms, substituents and unsaturated bonds, including ester-containing analogs, ketocarbonyl-containing analogs, sulfur-containing analogs, double bond- and triple bond-containing analogs, aromatic moiety-containing analogs, nitrated analogs and halogenated analogs.
    Type: Grant
    Filed: December 15, 1997
    Date of Patent: December 7, 1999
    Assignee: Washington University
    Inventors: Jeffrey I. Gordon, George W. Gokel, Paul T. Englund
  • Patent number: 5990342
    Abstract: A surfactant, an emusifier for emulsion polymerization, a dispersant for suspension polymerization and a modifier for modification of resin properties are disclosed, each of these agents being comprised of a novel compound having a dibasic carboxyl group. The compound is represented by Formula (1)[X--O--(R.sup.1 O).sub.m --OC--R.sup.2 --COO].sub.y M (1)where M is a hydrogen atom, a metal atom or a quaternary nitrogen-containing group, y is equal to the valence of M, R.sup.1 is at least one hydrocarbon group, R.sup.2 is a moiety of a dibasic acid or a moiety of its anhydride, m is 0 or an integer of 1 to 1,000, and X is a hydrocarbon group having at least one polymerizable double bond of carbon--ncarbon which may contain an oxygen atom and a fluorine atom.
    Type: Grant
    Filed: July 16, 1996
    Date of Patent: November 23, 1999
    Assignee: Asahi Denka Kogyo K.K.
    Inventors: Masahide Tsuzuki, Kaoru Komiya
  • Patent number: 5945561
    Abstract: Certain novel substituted (5,6)-dihydroanthracenyl compounds of the general formula ##STR1## wherein A, n, p, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7 and R.sub.8 are as defined in the specification exhibit retinoid-like properties and are particularly useful in the prevention of post-surgical adhesions.
    Type: Grant
    Filed: April 24, 1998
    Date of Patent: August 31, 1999
    Assignee: Bristol-Myers Squibb Company
    Inventors: John E. Starrett, Jr., Kenneth M. Tramposch, Xina Nair, Peter R. Reczek, Anna Ericsson, Anne Marinier, Alain Martel, Fred C. Zusi
  • Patent number: 5942623
    Abstract: The invention relates to a process for the preparation of 2-(pyrid-2-yloxymethyl)phenylacetates of formula (I) useful as intermediates for agricultural pesticides, which comprises reacting a 2-pyridine of formula (II), wherein L is a leaving group and A, D and m are as defined in the description with a compound MO--CH.sub.2 R where M is a metal atom and R is the residue of a metal salt of phenylacetic acid. It also includes the compounds MO--CH.sub.2 R, a process for their preparation and a "one-pot" process for the preparation of 2-(pyrid-2-yloxymethyl) phenylacetates from 3-isochromanone.
    Type: Grant
    Filed: February 19, 1998
    Date of Patent: August 24, 1999
    Assignee: ZENECA Limited
    Inventors: Alfred Glyn Williams, Gordon Richard Munns, Paul Anthony Worthington
  • Patent number: 5935985
    Abstract: We proposed a novel compound having an activity of PGI.sub.2 receptor agonist.A phenoxyacetic acid derivative of the formula ##STR1## A is --C(R.sup.1).dbd.N.about.OR.sup.2, --CH(R)NH--OR.sup.2, --COE, --SO.sub.2 E, --CH.sub.2 --NR.sup.3 --Y, --Z--NR.sup.3 --CONR.sup.4 R.sup.5, --CH.sub.2 --OR.sup.6, --CO.sub.2 R.sup.6, --CH.sub.2 --O.about.N.dbd.CR.sup.7 R.sup.8, --CH.sub.2 --O--NHCHR.sup.7 R.sup.8, substituted by imidazolyl(methyl), pyrazolylmethyl, oxazolyl(methyl), thioxazolyl, isoxazolyl, isothiazolyl, oxadiazolyl, triazolylmethyl;T is alkylene, alkenylene, etc.;D is --CO.sub.2 R.sup.10, --CONR.sup.11 R.sup.12 ;E is (substitution) amino, hydradino;Y is substituted (thio) carbonyl, substituted sulfonyl;Z is --CH.dbd.N--, --CH.sub.2 NR.sup.3 --;R.sup.1, R.sup.3, R.sup.10 --R.sup.13 is each H or alkyl, etc.;R.sup.2, R.sup.4 --R.sup.9 is each H, alkyl or alkyl substituted by phenyl or hetero ring ,etc. and non-toxic salts thereof, non-toxic acid addition salts thereof, possess an agonistic on PGI.sub.
    Type: Grant
    Filed: September 8, 1997
    Date of Patent: August 10, 1999
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Nobuyuki Hamanaka, Kanji Takahashi, Hidekado Tokumoto
  • Patent number: 5929117
    Abstract: Cyano and carboxy derivatives of substituted styrenes are inhibitors of tumor necrosis factor .alpha., nuclear factor .kappa.B, and phosphodiesterase and can be used to combat cachexia, endotoxic shock, retrovirus replication, asthma, and inflammatory conditions. A typical embodiment is 3,3-bis-(3,4-dimethoxyphenyl)acrylonitrile.
    Type: Grant
    Filed: August 11, 1997
    Date of Patent: July 27, 1999
    Assignee: Celgene Corporation
    Inventors: George W. Muller, Mary Shire
  • Patent number: 5874460
    Abstract: Compounds of the formula ##STR1## where W is (CH.sub.2).sub.n where n is 1 or 2, or n is 0 and W represents lower alkyl groups attached to each oxygen;m is an integer between 1 and 8;R.sub.1 is COOH or a pharmaceutically acceptable salt thereof, COOR.sub.4, CONR.sub.5 R.sub.6, CONR.sub.5 SO.sub.2 R.sub.7, CH.sub.2 OH, CH.sub.2 OR.sub.7, CH.sub.2 O--COR.sub.7, CH.sub.2 O--CONR.sub.5,R.sub.7, CH.sub.2 OCOOR.sub.7, CH.sub.2 NH.sub.2, CH.sub.2 NR.sub.5 R.sub.6, etc. where R.sub.4 is an alkyl group, or a cycloalkyl group, or R.sub.4 is phenyl or lower alkylphenyl, R.sub.5 and R.sub.6 independently are hydrogen, an alkyl group, etc., R.sub.7 is alkyl of 1 to 10 carbons, phenyl or lower alkylphenyl, R.sub.8 is lower alkyl, and R.sub.9 is divalent alkyl radical of 2-5 carbons, R.sub.10 is an alkyl OR cycloalkyl containing 1 to 5 carbons;R.sub.2 is H, COR.sub.7, R.sub.7, CO--OR.sub.7, CO--NR.sub.5,R.sub.7, PO(OH)OR.sub.7, PO(OR.sub.7).sub.2, POR.sub.7 OH, or POR.sub.7 (OR.sub.7) ;R.sub.
    Type: Grant
    Filed: June 9, 1998
    Date of Patent: February 23, 1999
    Assignee: Allergan Sales Inc.
    Inventors: Robert M. Burk, David F. Woodward
  • Patent number: 5863926
    Abstract: The present invention relates to novel 4,4-(disubstituted)cyclohexan-1-carboxylate monomers and related compounds, pharmaceutical compositions containing these compounds, and their use in treating allergic and inflammatory diseases and for inhibiting the production of Tumor Necrosis Factor (TNF).
    Type: Grant
    Filed: October 6, 1997
    Date of Patent: January 26, 1999
    Assignee: SmithKline Beecham Corporation
    Inventors: Siegfried B. Christensen, IV, Joseph M. Karpinski, M. Dominic Ryan, Paul E. Bender
  • Patent number: 5859295
    Abstract: This invention relates to canvanine analogs, their pharmaceutical compositions, and a method for treatment of cancer, particularly pancreatic cancer.
    Type: Grant
    Filed: June 18, 1996
    Date of Patent: January 12, 1999
    Assignee: University of Kentucky Research Foundation
    Inventors: Peter A. Crooks, Gerald A. Rosenthal
  • Patent number: 5817862
    Abstract: The invention relates to a process for the preparation of cinnamic acid derivatives which involves reacting chlorinated aromatic compounds and acrylic acid derivatives in the presence of palladium catalysts.
    Type: Grant
    Filed: August 22, 1996
    Date of Patent: October 6, 1998
    Assignee: Merck Patent Gesellschaft mit Beschrankter Haftung
    Inventors: Eike Poetsch, Volker Meyer, Ulrich Heywang, Rainer Christ, Jurgen Seubert
  • Patent number: 5783593
    Abstract: The present invention provides a compound of the formula ##STR1## which inhibit squalene synthetase and cholesterol biosynthesis and are useful in the treatment of e.g., hyperlipidaemia, atherosclerosis, or fungal infections, processes for the preparation of the compounds of the invention, intermediates useful in these processes, and pharmaceutical compositions containing the compounds.
    Type: Grant
    Filed: April 29, 1996
    Date of Patent: July 21, 1998
    Assignee: Abbott Laboratories
    Inventors: William R. Baker, Saul H. Rosenberg, Anthony K. L. Fung, Todd W. Rockway, Stephen A. Fakhoury, David S. Garvey, B. Gregory Donner, Stephen J. O'Connor, Rajnandan N. Prasad, Wang Shen, David M. Stout, Gerard M. Sullivan
  • Patent number: 5777160
    Abstract: This invention relates to certain 1,4,4-(trsubstituted)cyclohex-1-ene dimers and rlated compounds which are useful in treating allergic and inflammatory diseases and for inhibiting the production of Tumor Necrosis Factor (TNF).
    Type: Grant
    Filed: June 23, 1997
    Date of Patent: July 7, 1998
    Assignee: SmithKline Beecham Corporation
    Inventors: Siegfried B. Christensen, IV, Joseph M. Karpinski
  • Patent number: 5777176
    Abstract: The present invention relates to novel dimers of 4.4-(disubstituted)cyclohexan-1-ol dimers and delated compounds, pharmaceutical compositions containing these compounds, and their use in treating allergic and inflammatory diseases and for inhibiting the production of Tumor Necrosis Factor (TNF).
    Type: Grant
    Filed: June 23, 1997
    Date of Patent: July 7, 1998
    Assignee: SmithKline Beecham Corporation
    Inventors: Siegfried B. Christensen, IV, Joseph M. Karpinski
  • Patent number: 5746998
    Abstract: A radiographic imaging agent including a plurality of block copolymers forming a micelle, the block copolymers including a hydrophilic polymer linked to a hydrophobic polymer, and the hydrophobic polymer including a backbone incorporating radiopaque molecules via covalent bonds.
    Type: Grant
    Filed: August 8, 1996
    Date of Patent: May 5, 1998
    Assignee: The General Hospital Corporation
    Inventors: Vladimir P. Torchilin, Vladimir S. Trubetskoy, Gerald L. Wolf, G. Scott Gazelle
  • Patent number: 5716624
    Abstract: Novel pharmaceutically/cosmetically-active polyaromatic propynyl compounds have the structural formula (1): ##STR1## in which X is one of the radicals: ##STR2## and are useful for the treatment of a wide variety of disease states, whether human or veterinary, for example dermatological, rheumatic, respiratory, cardiovascular and ophthalmological disorders, as well as for the treatment of mammalian skin and hair conditions/disorders.
    Type: Grant
    Filed: December 15, 1994
    Date of Patent: February 10, 1998
    Assignee: C.I.R.D. Galderma
    Inventor: Jean-Michel Bernardon
  • Patent number: 5705703
    Abstract: Catechol derivatives of the formula ##STR1## wherein Ra, Rb and Rc have the significance given herein. the ester and ether derivatives thereof which are hydrolyzable under physiological conditions and the pharmaceutically acceptable salts thereof are described and possess valuable pharmacological properties. In particular, they inhibit the enzyme catechol-O-methyltransferase (COMT), a soluble, magnesium-dependent enzyme which catalyses the transference of the methyl group of S-adenosylmethionine to a catechol substrate, whereby the corresponding methyl ethers are formed. Suitable substrates which can be O-methylated by COMT and which can thus be deactivated are, for example, extraneuronal catecholamines and exogeneously-administered therapeutically active substances having a catechol structure.Formula Ia above embraces not only compounds which form part of the invention, but also known compounds: the compounds which form part of the invention can be prepared according to known methods.
    Type: Grant
    Filed: January 21, 1997
    Date of Patent: January 6, 1998
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Karl Bernauer, Janos Borgulya, Hans Bruderer, Mose Da Prada, Gerhard Zurcher
  • Patent number: 5698711
    Abstract: This invention is directed to the pharmaceutical use of phenyl compounds, which are linked to an aryl moiety by various linkages, for inhibiting tumor necrosis factor. The invention is also directed to the compounds, their preparation and pharmaceutical compositions containing these compounds. Furthermore, this invention is directed to the pharmaceutical use of the compounds for inhibiting cyclic AMP phosphodiesterase.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: December 16, 1997
    Assignee: Rhone-Poulenc Rorer Limited
    Inventor: Malcolm Norman Palfreyman
  • Patent number: 5698733
    Abstract: Disclosed are 9-deoxyprostaglandins which are useful in the treatment of glaucoma and ocular hypertension. Some of these 9-deoxyprostaglandins are novel. Also disclosed are ophthalmic, pharmaceutical compositions comprising such prostaglandins.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: December 16, 1997
    Assignee: Alcon Laboratories, Inc.
    Inventors: Mark R. Hellberg, Thomas R. Dean, Paul W. Zinke, Robert D. Selliah, John E. Bishop
  • Patent number: 5684168
    Abstract: .beta.-phenylisiserine-(2R,3S), salts and preparation thereof through the action of ammonia on .beta.-phenylglycidic-(2R,3R) acid and its use in the preparation of taxane derivatives of general formula: ##STR1## wherein R is hydrogen or --COCH.sub.3 ;and R.sub.1 is phenyl or --O--C(CH.sub.3).sub.3.
    Type: Grant
    Filed: April 10, 1995
    Date of Patent: November 4, 1997
    Assignee: Rhone-Poulenc Rorer S.A.
    Inventors: Jean-Pierre Duchesne, Max Ferraro
  • Patent number: 5650533
    Abstract: The invention relates to 4-substituted isoxazole derivatives of formula I: ##STR1## wherein R, R.sup.1, R.sup.2, Q and n have the meaning defined in the description which possess valuable herbicidal properties.
    Type: Grant
    Filed: June 2, 1995
    Date of Patent: July 22, 1997
    Assignee: Rhone-Poulenc Agriculture Ltd.
    Inventors: David Alan Roberts, Susan Mary Cramp, Derek Ian Wallis, Jean-Paul Bulot
  • Patent number: 5637759
    Abstract: Novel organic compounds and metal ion-containing amino acid chelates are described which are useful in solid phase synthesis of polypeptides and as magnetic resonance imaging (MRI) enhancing agents. The present invention also relates to a convenient and straightforward method to synthesize a metal-ligating amino acid suitable as MRI enhancing agents or for introducing a strong metal binding site at any chosen position in a peptide. Some compounds are designed to be compatible with N-.alpha.-Fmoc peptide synthesis strategy, and can easily be prepared on large scale. Thus, flexible linkers of different lengths and containing various structures can be placed between the .alpha.-carbon backbone of peptides and metal binding moieties. These peptides will provide a variety of affinity cleaving reagents which can be directed against protein or nucleic acid targets. Therefore, these molecules can serve as an important tool to study protein folding, protein-protein and protein-nucleic acid interactions.
    Type: Grant
    Filed: July 30, 1992
    Date of Patent: June 10, 1997
    Assignee: The Regents of the University of California
    Inventors: John E. Hearst, Tariq M. Rana, Matt Ban
  • Patent number: 5631293
    Abstract: Amino acid-substituted benzoylguanidines, a process for their preparation, their use as a medicament or diagnostic agent and a medicament containing themBenzoylguanidines of the formula I ##STR1## in which the radicals R(1) to R(5) have the meanings given in the description, are described. They are prepared by reacting a compound of the formula II ##STR2## in which R(1) to R(5) and L have the meanings given in the description, with guanidine. The compound I is suitable for the preparation of cardiovascular medicaments.
    Type: Grant
    Filed: September 8, 1995
    Date of Patent: May 20, 1997
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Heinz-Werner Kleemann, Hans-Jochen Lang, Jan-Robert Schwark, Andreas Weichert, Wolfgang Scholz, Udo Albus
  • Patent number: 5599975
    Abstract: A compound selected from those of formula (I): ##STR1## wherein A, X, Y, Z, R, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are as defined in the description.This compound or its physiologically tolerable salts may be used therapeutically as platelet anti-aggregation agent.
    Type: Grant
    Filed: October 27, 1994
    Date of Patent: February 4, 1997
    Assignee: Adir Et Compagnie
    Inventors: Ren e Gree, Ali M. Hachem, Danielle Gree, Yves Le Floc'h, Yves Rolland, Serge Simonet, Tony Verbeuren
  • Patent number: 5567410
    Abstract: A radiographic imaging agent including a plurality of block copolymers forming a micelle, the block copolymers including a hydrophilic polymer linked to a hydrophobic polymer, and the hydrophobic polymer including a backbone incorporating radiopaque molecules via covalent bonds.
    Type: Grant
    Filed: June 24, 1994
    Date of Patent: October 22, 1996
    Assignee: The General Hospital Corporation
    Inventors: Vladimir P. Torchilin, Vladimir S. Trubetskoy, Gerald L. Wolf, G. Scott Gazelle
  • Patent number: 5527947
    Abstract: This invention relates to an improved process for the manufacture of cinnamate compounds, particularly sunscreen agents, useful in cosmetic skin and hair care formulations. The process comprises: (a) dissolving a water insoluble C.sub.1 to C.sub.4 alkoxy benzaldehyde and a C.sub.1 to C.sub.4 alkyl acetate in a common hydrocarbon solvent; (b) reacting the resulting solution in the presence of a strong alkali metal-containing base under mild conditions to form a mixture containing the corresponding C.sub.1 to C.sub.4 alkyl C.sub.1 to C.sub.4 alkoxy cinnamate, the alkali metal salt of the enol corresponding to the C.sub.1 to C.sub.4 alkyl C.sub.1 to C.sub.4 alkoxy cinnamate, the alkali metal salt of a C.sub.1 to C.sub.4 alkoxycinnamic acid, and a C.sub.1 to C.sub.4 alkanol; (c) acidifying the resulting mixture with from about 0.5 to about 1 mole of a strong polybasic acid per mole of base to release acetic acid, to convert the alkali metal salt of the C.sub.1 to C.sub.
    Type: Grant
    Filed: December 19, 1994
    Date of Patent: June 18, 1996
    Assignee: ISP Van Dyk Inc.
    Inventors: Anatoly Alexander, Ratan K. Chaudhuri
  • Patent number: 5489447
    Abstract: A description is given of carrier-bound compounds of the formula I ##STR1## in which R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 independently of one another are hydrogen, halogen, nitro, cyano, CF.sub.3, C.sub.1 -C.sub.15 alkyl, C.sub.5 -C.sub.12 cycloalkyl, C.sub.2 -C.sub.15 alkenyl, C.sub.1 -C.sub.12 haloalkyl, C.sub.1 -C.sub.12 alkoxy, C.sub.1 -C.sub.12 alkylthio, C.sub.6 -C.sub.10 aryl, C.sub.6 -C.sub.10 aryloxy, C.sub.7 -C.sub.12 arylalkyl, --CO.sub.2 R.sub.6, --COR.sub.6 or ##STR2## in which at least one of the radicals R.sub.1 to R.sub.5 is hydrogen, halogen or C.sub.1 -C.sub.15 alkyl, and, in addition, the radicals R.sub.1 and R.sub.2, R.sub.2 and R.sub.3, R.sub.3 and R.sub.4 or R.sub.4 and R.sub.5 together with the carbon atoms to which they are attached form a benzo or cyclohexenyl ring,R.sub.6 is C.sub.1 -C.sub.20 alkyl, C.sub.2 -C.sub.20 alkyl which is interrupted by oxygen, sulfur or >N--R.sub.9 ; or is C.sub.7 -C.sub.12 arylalkyl,R.sub.7 and R.sub.
    Type: Grant
    Filed: June 20, 1994
    Date of Patent: February 6, 1996
    Assignee: Ciba-Geigy Corporation
    Inventors: Andreas Kramer, Adalbert Braig
  • Patent number: 5476944
    Abstract: The present invention relates to derivatives of cyclic phenolic thioethers of the formula: ##STR1## and the pharmaceutically acceptable salts thereof, which are inhibitors or stimulators of superoxide generation, and which may also inhibit cyclooxygenase and/or 5-lipoxygenase, to pharmaceutical compositions containing one or more of these compounds in combination with a pharmaceutically-acceptable carrier, and to medical methods of treatment employing these compounds.
    Type: Grant
    Filed: May 19, 1994
    Date of Patent: December 19, 1995
    Assignee: G. D. Searle & Co.
    Inventors: Richard A. Partis, Richard A. Mueller, Francis J. Koszyk, Richard M. Weier
  • Patent number: 5458678
    Abstract: There are described novel alkaline earth metal salts, transition metal salts and transition metal complexes of compounds of the formula I ##STR1## in which R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are, independently of one another, hydrogen, halogen, nitro, cyano, CF.sub.3, C.sub.1 -C.sub.15 alkyl, C.sub.5 -C.sub.12 cycloalkyl, C.sub.2 -C.sub.15 alkenyl, C.sub.1 -C.sub.12 haloalkyl, C.sub.1 -C.sub.12 alkoxy, C.sub.1 -C.sub.12 alkylthio, C.sub.6 -C.sub.10 aryl which is unsubstituted or substituted by C.sub.1 -C.sub.4 alkyl; C.sub.6 -C.sub.10 aryloxy which is unsubstituted or substituted by C.sub.1 -C.sub.4 alkyl; C.sub.7 -C.sub.12 arylalkyl which is unsubstituted or substituted on the aryl radical by from 1 to 3 C.sub.1 -C.sub.4 alkyl groups; --CO.sub.2 R.sub.6, --COR.sub.6 or ##STR2## where at least one of the radicals R.sub.1 to R.sub.5 is hydrogen, halogen or C.sub.1 -C.sub.15 alkyl, in addition the radicals R.sub.1 and R.sub.2, R2 and R.sub.3, R.sub.3 and R.sub.4 or R.sub.4 and R.sub.
    Type: Grant
    Filed: April 4, 1994
    Date of Patent: October 17, 1995
    Assignee: Ciba-Geigy Corporation
    Inventors: William P. Armstrong, Adalbert Braig, Markus Frey, Andreas Kramer
  • Patent number: 5446198
    Abstract: The present invention relates to the novel compound 4-hydroxy-2,3,5-trifluorobenzoic acid and to a process for preparing this novel substance by reacting 2,3,4,5-tetrafluorobenzoic acid at elevated temperature with a basic compound dissolved and/or suspended in water, adding, if desired, a fluoride scavenger, bringing the resulting reaction mixture to a pH of 0 to 6 by addition of an acid, and isolating the 4-hydroxy-2,3,5-trifluorobenzoic acid formed.
    Type: Grant
    Filed: December 15, 1993
    Date of Patent: August 29, 1995
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Ralf Pfirmann, Rainer Wingen
  • Patent number: 5426210
    Abstract: An adduct of cinnamic acid and glycerin represented by the following general structural formula (1); ##STR1## (In the general structural formula (1) above, G represents 1 mole of glycerin and e represents average mole number of addition and at least 1. R represents hydrogen or fatty chain. n and k are identified by that (n+k) is 1 to 3, and n and k are 0 to 3 respectively. X represents hydrogen, ion, fatty chain or Gm, and the G represents 1 mole of glycerin, m represents average number of addition and at least 1.), an ultraviolet ray absorbent and an external preparation for skin containing the same.The adduct of cinnamic acid and glycerin according to the present invention have excellent capability to absorb ultraviolet rays as well as high water solubility.
    Type: Grant
    Filed: March 5, 1993
    Date of Patent: June 20, 1995
    Assignee: Shiseido Co., Ltd.
    Inventors: Mikiko Kato, Reiji Miyahara, Keiichi Uehara, Sadaki Takata
  • Patent number: 5414108
    Abstract: The subject matter of the invention is a process for the preparation of carboxylic acids and derivatives of them of the general formula ##STR1## wherein R means hydrogen, or a C.sub.1-4 alkyl or a (C.sub.1-5 alkoxy)carbonyl group,R.sub.1 is as defined in claim 1,R.sub.7 stands for hydrogen or a C.sub.1-7 alkyl group andR.sub.8 means hydrogen or a carboxyl group.
    Type: Grant
    Filed: August 11, 1992
    Date of Patent: May 9, 1995
    Assignee: Biogal Gyogyszergrar
    Inventors: Gyorgy Toth, Janos Balint, Klara Elek nee Herczik, Zsuzsanna Moricz nee Garai, Eva Mudra nee Kantor
  • Patent number: 5395964
    Abstract: Preparation process for a hydroxyphenylacetic acid of formula (I): ##STR1## where R.dbd.H, alkyl or alkoxyl as well as its salts, in which the corresponding free or salified hydroxymandelic acid of formula (II): ##STR2## in which R has the meaning given previously and M.dbd.H, K or an ammonium group is reacted in an aqueous medium, at a temperature greater than or equal to 50.degree. C., with formic acid in the presence of catalytic quantities of an oxygenated derivative of sulphur having a degree of oxidation from 2 to 4, in order to obtain the hydroxyphenylacetic acid of formula (I) which is isolated or, if desired, is salified according to the usual methods and the hydroxyphenylacetic acid thus obtained.
    Type: Grant
    Filed: May 19, 1994
    Date of Patent: March 7, 1995
    Assignee: Societe Francaise Hoechst
    Inventors: Jean-Claude Vallejos, Yani Christidis
  • Patent number: 5395918
    Abstract: The invention describes new biphenyl dianhydrides, and new polyimides and copolyimides made from the dianhydrides. The synthesized polyimides exhibit significantly enhanced solubility when the biphenyl dianhydrides are substituted, particularly at the 2 and 2' positions on the phenyl rings.
    Type: Grant
    Filed: April 21, 1994
    Date of Patent: March 7, 1995
    Assignee: The University of Akron
    Inventors: Frank W. Harris, Sheng-Hsien Lin
  • Patent number: 5391817
    Abstract: Certain novel biaryl compounds are effective phospholipase A.sub.2 (PLA.sub.2) inhibitors.
    Type: Grant
    Filed: December 21, 1993
    Date of Patent: February 21, 1995
    Assignee: Bristol-Myers Squibb
    Inventors: Dane Springer, Bing-Yu Luh, Katharine M. Greene, Joanne J. Bronson, Muzammil M. Mansuri
  • Patent number: 5360819
    Abstract: A release tag reagent suitable for use in the chemical analysis of a substance to be detected, which substance contains reactive groups, such as for, but not limited to gas phase detection groups, which reagent comprises three covalently bonded groups: a signal group which on release provides a ketone signal compound to be detected, a release group which may be cleaved to release the ketone signal group, which release group contains, for example, a vic glycol or an olefin group and a reactivity group which is reactive with a reactive group of the substance to be detected.
    Type: Grant
    Filed: March 11, 1985
    Date of Patent: November 1, 1994
    Assignee: Northeastern University
    Inventor: Roger W. Giese
  • Patent number: 5350872
    Abstract: The subject matter of the invention is a process for the preparation of carboxylic acids and derivatives of them of the general formula ##STR1## wherein R means hydrogen, or a C.sub.1-4 alkyl or a (C.sub.1-5 alkoxy)carbonyl group,R.sub.1 is as defined in claim 1,R.sub.7 stands for hydrogen or a C.sub.1-7 alkyl group andR.sub.8 means hydrogen or a carboxyl group,by reacting a 1,3-dioxane-4,6-dione derivative of the general formula ##STR2## wherein R.sub.9 stands for a C.sub.1-4 alkyl group or a phenyl group, optionally monosubstituted by halogen andR.sub.10 stands for hydrogen or a C.sub.1-5 alkyl group orR.sub.9 and R.sub.10 together form a pentamethylene group,and an aldehyde or ketone of the general formula ##STR3## in the presence of formic acid.
    Type: Grant
    Filed: October 29, 1993
    Date of Patent: September 27, 1994
    Assignee: Biogal Gyogyszergrar
    Inventors: Gyorgy Toth, Janos Balint, Klara Elek nee Herczik, Zsuzsanna Moricz nee Garai, Eva Mudra nee Kantor
  • Patent number: 5344970
    Abstract: A ruthenium-phosphite complex having the formula ##STR1## wherein a is from 1 to 3; b is 1 or 2; c is from 0 to 3; and R is hydrogen, alkyl, aryl, halo, amino, acetylamino, or sulfo; and X is ##STR2## where R.sub.1, R.sub.2, and R.sub.3 are the same or different and are hydrogen or C.sub.1 to C.sub.6 linear or branched alkyl.This complex can be used to effect the reduction of unsaturated organic compounds or, when comprised of ligands having optical activity, can be used as the catalyst for effecting the asymmetric reduction of unsaturated organic compounds.
    Type: Grant
    Filed: December 22, 1993
    Date of Patent: September 6, 1994
    Assignee: Albemarle Corporation
    Inventor: Charles H. Kolich
  • Patent number: 5332857
    Abstract: Variously substituted 3,5-dihydroxy-6,8-nonadienoic acids and esters, are blood cholesterol lowering agents and so are useful in the prevention and treatment of cardiovascular diseases such as atherosclerosis.
    Type: Grant
    Filed: July 6, 1992
    Date of Patent: July 26, 1994
    Assignee: Pfizer Inc.
    Inventors: Peter A. McCarthy, Frederick J. Walker
  • Patent number: 5306833
    Abstract: Process for obtaining an arylacetic acid of general formula (I):Ar--CHR--COOH (I)in which R=H, C.sub.1 -C.sub.4 alk, Ar=2-thienyl, 3-thienyl, 1-naphthyl, 2-naphthyl, 1-(2-methoxy naphthyl), 3,4-methylenedioxy phenyl or phenyl of general formula (II): ##STR1## in which R.sub.1 =H, OH or C.sub.1 -C.sub.4 alkoxy, R.sub.2 =H, C.sub.1 -C.sub.4 alk, C.sub.1 -C.sub.4 alkoxy or OH, as well as their alkali metal salts, by reaction in a solvent of the corresponding arylglycolic acid of general formula (III):Ar-CR(OH)--COOH (III)or one of its alkali metal salts with a hydrogen donor agent chosen from the group constituted by: formic acid, or one of its alkali metal salts, phosphonic acid, phosphinic acid, or one of their alkali metal salts, in the presence of a hydrogen transfer catalyst, which if desired is isolated or salified, and use for the preparation of certain acids of formula (I).
    Type: Grant
    Filed: February 3, 1993
    Date of Patent: April 26, 1994
    Assignee: Societe Francaise Hoechst
    Inventors: Jean-Claude Vallejos, Yani Christidis
  • Patent number: 5288750
    Type: Grant
    Filed: January 31, 1991
    Date of Patent: February 22, 1994
    Assignee: Orion-yhtyma Oy
    Inventors: Pentti Pohto, Paivi A. Aho, Reijo J. Backstrom, Erkki J. Honkanen, Inge-Britt Y. Linden, Erkki A. O. Nissinen
  • Patent number: 5283352
    Abstract: Catechol compounds of formula I ##STR1## where R.sub.1, R.sub.2, R.sub.3 and X are as described herein are effective Catechol-O-methyltransferase inhibitors.
    Type: Grant
    Filed: December 7, 1992
    Date of Patent: February 1, 1994
    Assignee: Orion-yhtyma Oy
    Inventors: Reijo J. Backstrom, Kalevi E. Heinola, Erkki J. Honkanen, Seppo K. Kaakkola, Pekka J. Kairisalo, Inge-Britt Y. Linden, Pekka I. Mannisto, Erkki A. O. Nissinen, Pentti Pohto, Aino K. Pippuri, Jarmo J. Pystynen
  • Patent number: 5279759
    Abstract: Alpha-(p-alkoxybenzylidene) carboxylic acids are used as color stabilizers, processing aids and whiteners for soap.
    Type: Grant
    Filed: December 9, 1992
    Date of Patent: January 18, 1994
    Assignee: Henkel Corporation
    Inventors: Louis Rebrovic, Alan C. Kilbarger
  • Patent number: 5254728
    Abstract: Complexes containing S(+)-ibuprofen, method for the production of these complexes and pharmaceutical preparations containing these complexes are described.
    Type: Grant
    Filed: November 15, 1991
    Date of Patent: October 19, 1993
    Assignee: Medice Chem.-pharm. Fabrik Putter GmbH & Co. KG
    Inventor: Henrich H. Paradies
  • Patent number: 5250325
    Abstract: Coating composition comprising:A) an organic film-forming binder; andB) a corrosion-inhibiting amount of a water-insoluble salt of i) a carboxylic acid having the formula (I): ##STR1## and ii) a base selected from a) a cation of Group Ib, IIa, IIb, IIIa, IIIb, IVa, IVb, Va, VIa, VIIa or VIIIa of the Periodic Table of Elements, b) an amine of formula II: ##STR2## c) a guanidine of formula III:R.sub.7 --N.dbd.C(NH.sub.2).sub.2 IIId) an amidine of formula IV:R.sub.7 --C(.dbd.NH)NH.sub.2 IVor e) melamine.
    Type: Grant
    Filed: January 21, 1993
    Date of Patent: October 5, 1993
    Assignee: Ciba-Geigy Corporation
    Inventors: Emyr Phillips, William P. Armstrong