Patents Examined by T. A. Solola
  • Process for preparing benzothiophenecarboxamide derivatives
    Patent number: 6465662
    Abstract: A process for preparing a compound having PGD2 antagonism represented by the formula (I), or a pharmaceutically acceptable salt or hydrate thereof, which process comprises reacting an amino alcohol of the formula (II) or its salt with a compound of the formula (III) or its reactive derivative, oxidizing the product with halo oxoacid in the presence of 2,2,6,6-tetramethylpiperidine-1-oxyls, reacting the product with an ylide under the conditions for Wittig reaction, and optionally deprotecting the product.
    Type: Grant
    Filed: April 29, 2002
    Date of Patent: October 15, 2002
    Assignee: Shionogi & Co., Ltd.
    Inventors: Tsunetoshi Honma, Yoshiharu Hiramatsu
  • Halogen promoted multi-metal oxide catalyst
    Patent number: 6461996
    Abstract: A catalyst comprising a promoted mixed metal oxide is useful for the vapor phase oxidation of an alkane or a mixture of an alkane and an alkene to an unsaturated carboxylic acid and for the vapor phase ammoxidation of an alkane or a mixture of an alkane and an alkene to an unsaturated nitrile.
    Type: Grant
    Filed: August 10, 2001
    Date of Patent: October 8, 2002
    Assignee: Rohm and Haas Company
    Inventors: Sanjay Chaturvedi, Anne Mae Gaffney, Scott Han, Michele Doreen Heffner, Ruozhi Song
  • Process for preparing benzothiophenecarboxamide derivatives
    Patent number: 6462241
    Abstract: A process for preparing a compound having PGD2 antagonism represented by the formula (I), or a pharmaceutically acceptable salt or hydrate thereof, which process comprises reacting an amino alcohol of the formula (II) or its salt with a compound of the formula (III) or its reactive derivative, oxidizing the product with halo oxoacid in the presence of 2,2,6,6-tetramethylpiperidine-1-oxyls, reacting the product with an ylide under the conditions for Wittig reaction, and optionally deprotecting the product.
    Type: Grant
    Filed: April 29, 2002
    Date of Patent: October 8, 2002
    Assignee: Shionogi & Co., Ltd.
    Inventors: Tetsuo Okada, Makoto Kakinuma
  • Beta-amino acid nitrile derivatives as cathepsin K inhibitors
    Patent number: 6462076
    Abstract: The present invention relates to beta-amino acid nitrile derivatives and pharmaceutically acceptable salts and/or pharmaceutically acceptable esters thereof. The compounds are cysteine protease inhibitors useful for the treatment of diseases associated with cysteine proteases, such as osteoporosis, osteoarthritis, rheumatoid arthritis, tumor metastasis, glomerulonephritis, atherosclerosis, myocardial infarction, angina pectoris, instable angina pectoris, stroke, plaque rupture, transient ischemic attacks, amaurosis fugax, peripheral arterial occlusive disease, restenosis after angioplasty and stent placement, abdominal aortic aneurysm formation, inflammation, autoimmune disease, malaria, ocular fundus tissue cytopathy and respiratory disease.
    Type: Grant
    Filed: June 1, 2001
    Date of Patent: October 8, 2002
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Tobias Gabriel, Michael Pech, Rosa Maria Rodriguez Sarmiento
  • Gambogic acid, analogs and derivatives as activators of caspases and inducers of apoptosis
    Patent number: 6462041
    Abstract: The present invention is directed to gambogic acid, analogs and derivatives thereof, represented by the general Formulae I-III: wherein R1-R5 are defined herein. The present invention also relates to the discovery that compounds having Formula I-III are activators of caspases and inducers of apoptosis. Therefore, the activators of caspases and inducers of apoptosis of this invention can be used to induce cell death in a variety of clinical conditions in which uncontrolled cell growth and spread of abnormal cells occurs.
    Type: Grant
    Filed: February 1, 2000
    Date of Patent: October 8, 2002
    Assignee: Cytovia, Inc.
    Inventors: Sui Xiong Cai, Han-Zhong Zhang, Yan Wang, Ben Tseng, Shailaja Kasibhatla, John A. Drewe
  • Process for the purification of propylene oxide
    Patent number: 6462209
    Abstract: Process for improving the quality of a propylene oxide contaminated with poly(propylene oxide), which process comprises the steps of: (a) contacting the liquid propylene oxide with an adsorbent consisting of magnesium silicate and/or calcium silicate under such conditions that the amount of poly(propylene oxide) is reduced to the desired level, and (b) recovering the purified propylene oxide product.
    Type: Grant
    Filed: September 14, 2001
    Date of Patent: October 8, 2002
    Assignee: Shell Oil Company
    Inventors: Johannes Gerhardus Joseph Beckers, Johannes Jozias Blom
  • Substituted &agr;, &bgr;-anellated butyrolactones
    Patent number: 6462074
    Abstract: The present invention relates to novel substituted (&agr;,&bgr;-fused butyrolactones, to processes for their preparation and to their use for the prevention and/or treatment of disorders caused by hyper- or hypofunction of the glutamatergic system, in particular of cerebral ischaemias, craniocerebral trauma, states of pain or CNS-mediated spasms.
    Type: Grant
    Filed: July 14, 2000
    Date of Patent: October 8, 2002
    Assignee: Bayer Aktiengesellschaft
    Inventors: Andreas Stolle, Horst-Peter Antonicek, Stephen Lensky, Arnd Voerste, Thomas Müller, Jörg Baumgarten, Karsten von dem Bruch, Gerhard Müller, Udo Stropp, Ervin Horváth, Jean-Marie-Viktor de Vry, Rudy Schreiber
  • Oxazolidines as 5-HT2A-antagonists
    Patent number: 6462056
    Abstract: The invention relates to novel oxazolidine derivatives of the formula in which R1, R2 and R3 have the meanings stated in claim 1, their salts and processes for preparing the compounds according to the invention. The compounds of the formula I act as 5-HT2A antagonists with a 5-HT reuptake-inhibiting, antidepressant or anxiolytic effect and can be used to produce pharmaceuticals.
    Type: Grant
    Filed: August 25, 1999
    Date of Patent: October 8, 2002
    Assignee: Merck Patent Gesellschaft mit beschrankter Haftung
    Inventors: Henning Böttcher, Helmut Prücher, Hartmut Greiner, Gerd Bartoszyk, Christoph Seyfried
  • Radiolabeled farnesyl-protein transferase inhibitors
    Patent number: 6458935
    Abstract: The present invention is directed toward radiolabeled farnesyl-protein transferase inhibitor compounds which are useful to label FPTase in assays, whether cell-based, tissue-based or in whole animal. The tracers can also be used in competitive binding assays to obtain information on the interaction of unlabeled FTIs with FPTase.
    Type: Grant
    Filed: June 12, 2000
    Date of Patent: October 1, 2002
    Assignee: Merck & Co., Inc.
    Inventors: H. Donald Burns, Terence G. Hamill, Raymond E. Gibson
  • Amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors
    Patent number: 6458785
    Abstract: Selected amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.
    Type: Grant
    Filed: April 18, 2001
    Date of Patent: October 1, 2002
    Assignee: G. D. Searle
    Inventors: Daniel P Getman, Gary A. DeCrescenzo, John N. Freskos, Michael L. Vazquez, James A. Sikorski, Balekudru Devadas, Srinivasan Nagarajan, David L. Brown, Joseph J. McDonald
  • Pyran derivatives
    Patent number: 6455579
    Abstract: Disclosed are pyran derivatives, which have distinctive sensitivity to visible light and distinctive luminous ability. The derivatives are useful in photopolymerization, electroluminescence, and dye lasers, and are obtainable through a step of reacting a compound having a 4-cyanomethylene-2-methyl-4H-pyran skeleton with a compound having a 3-formylcoumarin skeleton.
    Type: Grant
    Filed: November 9, 2000
    Date of Patent: September 24, 2002
    Assignee: Kabushiki Kaisha Hayashibara Seibutsu Kagaku Kenkyujo
    Inventors: Makoto Satsuki, Akira Shinpo, Yasuyo Ooga, Sadaharu Suga, Atsushi Oda, Hiroshi Tada, Yoshikazu Sakaguchi
  • Process for preparing benzothiophenecarboxamide derivatives
    Patent number: 6455741
    Abstract: A process for preparing a compound having PGD2 antagonism represented by the formula (I), or a pharmaceutically acceptable salt or hydrate thereof, which process comprises reacting an amino alcohol of the formula (II) or its salt with a compound of the formula (III) or its reactive derivative, oxidizing the product with halo oxoacid in the presence of 2,2,6,6-tetramethylpiperidine-1-oxyls, reacting the product with an ylide under the conditions for Wittig reaction, and optionally deprotecting the product.
    Type: Grant
    Filed: April 29, 2002
    Date of Patent: September 24, 2002
    Assignee: Shionogi & Co., Ltd.
    Inventors: Tetsuo Okada, Makoto Kakinuma
  • Aminonitrile production
    Patent number: 6455724
    Abstract: Provided is a selective hydrogenation process for producing aminonitriles by contacting the corresponding dinitriles with a hydrogen-containing fluid in the presence of a hydrogenation catalyst, a solvent and an azide additive.
    Type: Grant
    Filed: October 2, 2001
    Date of Patent: September 24, 2002
    Assignee: E. I. du Pont de Nemours and Company
    Inventor: Alex Sergey Ionkin
  • Aminonitrile production
    Patent number: 6455723
    Abstract: Provided is a selective hydrogenation process for producing aminonitriles by contacting the corresponding dinitriles with a hydrogen-containing fluid in the presence of a hydrogenation catalyst, a solvent and divalent sulfur and selenium compounds.
    Type: Grant
    Filed: October 2, 2001
    Date of Patent: September 24, 2002
    Assignee: E. I. du Pont de Nemours and Company
    Inventor: Alex Sergey Ionkin
  • Two-stage preparation of promoted V/Sb-oxide ammoxidation catalysts
    Patent number: 6451730
    Abstract: A process for the preparation of a promoted VSbOx catalyst comprising mixing a vanadium compound, at least a first portion of an antimony compound, and at least a portion of the support material to form a slurry, heating the slurry to remove the water, calcining the dried slurry to form a catalyst precursor, combining the catalyst precursor with a second aqueous sol containing the remaining portion of the support material and the remaining portion of the antimony compound to form a second slurry, drying the second slurry to remove the water and calcining the dried mixture to form the finished catalyst.
    Type: Grant
    Filed: June 27, 1997
    Date of Patent: September 17, 2002
    Assignee: The Standard Oil Company
    Inventors: Maria Strada Friedrich, Michael J. Seely, Dev Dhanaraj Suresh
  • Synthesis of dialkyl carbonates
    Patent number: 6452036
    Abstract: The invention generally concerns methods for the synthesis of dialkyl carbonates, and more specifically dimethyl carbonate (DMC) and diethyl carbonate (DEC). Methods according to the invention generally comprise reacting an alcohol or diol, a base and a halogen in the presence of an amine salt catalyst thereby forming a first intermediate. The first intermediate is reacted with carbon monoxide forming a second intermediate which then reacts with the alcohol or diol in the presence of the amine salt catalyst forming the dialkyl carbonate product.
    Type: Grant
    Filed: May 2, 2002
    Date of Patent: September 17, 2002
    Assignee: Jacam Chemicals, L.L.C.
    Inventors: Gene H. Zaid, Beth Ann Wolf
  • Process for preparing d,l-&agr;-tocopherol
    Patent number: 6452023
    Abstract: A process for the manufacture of d,l-&agr;-tocopherol by the acid-catalyzed condensation of trimethylhydroquinone with isophytol or phytol in ethylene or propylene carbonate or a mixture of both carbonates, or in a mixture of one or both of the carbonates and a non-polar solvent, comprises carrying out the condensation in the presence of at most 0.4 weight percent based on the weight of isophytol or phytol of 12-tungstophosphoric acid, 12-molybdophosphoric acid or 12-tungstosilicic acid. The product of the process is the most active and industrially important member of the vitamin E group.
    Type: Grant
    Filed: June 29, 1999
    Date of Patent: September 17, 2002
    Assignee: Roche Vitamins Inc.
    Inventors: Fabrice Aquino, Werner Bonrath
  • Process for extraction and purification of paclitaxel from natural sources
    Patent number: 6452024
    Abstract: A process for the extraction and purification of Paclitaxel from a natural source of taxanes, comprising extracting Paclitaxel with an organic solvent from a natural source of taxanes, and treating the raw material with a base or an acid to obtain a biomass by precipitation. The biomass is isolated and dried, and resin and natural pigments are removed. The biomass is then dissolved in acetone and at least one non-polar solvent is added, until a Paclitaxel-enriched oily phase is obtained. The Paclitaxel-enriched oily phase is then treated with a base or an acid to obtain a second biomass, which is recovered by precipitation and dried. A solution of the second biomass in a volatile solvent is chromatographically purified at least once and crystallized.
    Type: Grant
    Filed: May 26, 2000
    Date of Patent: September 17, 2002
    Assignee: Chaichem Pharmaceuticals International
    Inventors: Trung Bui-Khac, Nicolas Dupuis
  • Indolecarboxylic compounds and their use as pharmaceutical compounds
    Patent number: 6448285
    Abstract: The invention relates to the use, as active principle, in a physiologically acceptable medium, in a composition, of an effective amount of at least one compound of the indolecarboxylic family, this compound or these compositions being intended to treat disorders associated with overactivity of 5&agr;-reductase. These compounds or the compositions containing them are more particularly intended to treat androgen-dependent disorders such as seborrhoea and/or acne and/or hirsutism and/or androgenic alopecia. The invention also relates to novel compounds of the indolecarboxylic family and to compositions containing them.
    Type: Grant
    Filed: July 26, 1999
    Date of Patent: September 10, 2002
    Assignee: Societe L'Oreal S.A.
    Inventors: Bruno Bernard, Catherine Gerst, Jean-Baptiste Galey, Maria Dalko, Patrick Pichaud
  • Method of epoxidizing olefins
    Patent number: 6448418
    Abstract: A process is provided for the epoxidation of olefins with percarboxylic acid in a reaction mixture consisting of an aqueous phase and an organic phase, the percarboxylic acid being formed in situ in the aqueous phase from hydrogen peroxide and a carboxylic acid or a carboxylic anhydride, and the olefins being dissolved in an organic solvent in the organic phase, wherein the epoxidation is carried out in several steps, each step being carried out with a fresh aqueous phase and the aqueous phase being separated off after each step.
    Type: Grant
    Filed: April 25, 2001
    Date of Patent: September 10, 2002
    Assignee: BASF Aktiengesellschaft
    Inventor: Christian Ott