Patents Examined by Ba K. Trinh
  • &bgr;-lactams, methods for the preparation of taxanes, and sidechain-bearing taxanes
    Patent number: 6350887
    Abstract: Novel &bgr;-lactams finding utility as intermediates in the preparation of sidechain-bearing taxanes such as taxol and taxol derivatives. The present invention also relates to novel methods of coupling &bgr;-lactams to form such sidechain-bearing taxanes, and to novel sidechain-bearing taxanes.
    Type: Grant
    Filed: May 12, 1995
    Date of Patent: February 26, 2002
    Assignee: Bristol-Myers Squibb Company
    Inventors: John K. Thottathil, Ivan D. Trifunovich, David J. Kucera, Wen-Sen Li
  • Catalytic asymmetric epoxidation
    Patent number: 6348608
    Abstract: A compound and method for producing an enantiomerically enriched epoxide from an olefin using a chiral ketone and an oxidizing agent is disclosed.
    Type: Grant
    Filed: April 6, 1999
    Date of Patent: February 19, 2002
    Inventor: Yian Shi
  • Method for oxidizing an organic compound having at least one C-C double bond
    Patent number: 6348607
    Abstract: In a process for oxidizing an organic compound containing at least one C—C double bond, or a mixture of two or more thereof, which comprises the step (II) below: (II) reaction of the organic compound or the mixture of two or more thereof with a medium comprising molecular oxygen in the presence of a heterogeneous catalyst, the medium further comprises carbon monoxide (CO).
    Type: Grant
    Filed: April 16, 2001
    Date of Patent: February 19, 2002
    Assignee: BASF Aktiengesellschaft
    Inventors: Ulrich Müller, Georg Heinrich Grosch, Bernd Stein, Norbert Rieber
  • Stabilization of taxane-containing dispersed systems
    Patent number: 6348215
    Abstract: The invention provides a method of stabilizing a taxane in a dispersed system, which method comprises exposing the taxane to a molecule which improves physical stability of the taxane in the dispersed system. By improving physical stability of the taxane in the dispersed system, higher taxane content can be achieved. The invention thus further provides a stable taxane-containing liposome preparation comprising a liposome containing one or more taxanes present in the liposome in an amount of less than 20 mol % total taxane to liposome, wherein the liposome is suspended in a glycerol:water composition having at least 30% glycerol.
    Type: Grant
    Filed: October 6, 2000
    Date of Patent: February 19, 2002
    Assignee: The Research Foundation of State University of New York
    Inventors: Robert M. Straubinger, Sathyamangalam V. Balasubramanian
  • Process for producing (2R, 3S)-3-amino-1, 2-oxirane
    Patent number: 6348615
    Abstract: A process for producing (2R, 3S)-3-amino-4-phenylbutane-1,2-epoxide compounds which comprises treating a (2S, 3S)-3-amino-1-halo-2-hydroxy-4-phenylbutane compound or a (2S, 3S)-3-amino-4-phenylbutane-1,2-epoxide with a carboxylic acid quaternary ammonium salt or a carboxylic acid metal salt a quaternary ammonium salt and a quaternary ammonium salt, to give a (2S, 3S)-1-acyloxy-3-amino-2-hydroxy-4-phenylbutane compound, further treating the same with a sulfonic acid halide in the presence of an organic base to give a (2S, 3S)-1-acyloxy-3-amino-2-sulfonyloxy-4-phenylbutane compound, furthermore treating said compound with an inorganic base. An intermediate for the production of an HIV protease inhibitor can be produced from L-phenylalanine.
    Type: Grant
    Filed: May 11, 2001
    Date of Patent: February 19, 2002
    Assignee: Kaneka Corporation
    Inventors: Kazumi Okuro, Kenji Inoue
  • Water soluble analogs and prodrugs of paclitaxel
    Patent number: 6344571
    Abstract: The invention relates to water soluble antitumor analogs of paclitaxel of formula (I) wherein R1=C(O)CH2CH(OH)COOX, R2=H, C(O)CH2CH(OH)COOX, X=H, Li, Na or any other pharmaceutically acceptable counterion, as well as to a pharmaceutical composition comprising an antineoplastically effective amount of such analogs as an active ingredient.
    Type: Grant
    Filed: February 21, 2001
    Date of Patent: February 5, 2002
    Assignee: Pharmachemie B.V.
    Inventors: Peter H. G. Wiegerinck, Duncan Sperling, Lesly Braamer, Eric W. P. Damen, Johan W. Scheeren, Dick de Vos
  • Aryl or heteroaryl amides of tetrahydronaphthalene, chroman, thichroman and 1,2,3,4-tetrahydroquinolinecarboxlic acids, having an electron withdrawing substituent in the aromatic or heteroaromatic moiety, having retinoid-like biological activity
    Patent number: 6342602
    Abstract: Compounds of the formula wherein the symbols have the meaning defined in the specification have retinoid-like biological activity.
    Type: Grant
    Filed: August 4, 2000
    Date of Patent: January 29, 2002
    Assignee: Allergan Sales, Inc.
    Inventors: Min Teng, Tien T. Duong, Roshantha A. Chandraratna
  • Glycidyl ester adducts having increased glass transition temperatures
    Patent number: 6342615
    Abstract: The invention provides for a purified glycidyl ester product prepared from neo acids wherein said ester product is recovered as a light fraction from a glycidyl ester reaction product composition that has been subjected to conditions of temperature and vacuum in a thin film, short pass distillation evaporator, said purified glycidyl ester product further characterized that its polymerizable reaction product with methacrylic acid has a higher effective glass transition temperature as compared with the polymerizable reaction product with methacrylic acid of said glycidyl ester reaction product composition prior to purification.
    Type: Grant
    Filed: May 8, 2000
    Date of Patent: January 29, 2002
    Assignee: ExxonMobil Chemicals Patents Inc.
    Inventors: Richard William Ryan, Gerald G. McGlamery, Jr., Ralph Martin Kowalik, Michael J. Keenan
  • C2 substituted phenyl taxane derivatives and pharmaceutical compositions containing them
    Patent number: 6339164
    Abstract: Taxane derivatives having alternative C2 substituents.
    Type: Grant
    Filed: December 16, 1999
    Date of Patent: January 15, 2002
    Assignee: Florida State University
    Inventors: Robert A. Holton, Chunlin Tao
  • Taxanes having an alkyl substituted side-chain and pharmaceutical compositions containing them
    Patent number: 6335362
    Abstract: Taxane derivatives having an alkyl substituted C13 side chain.
    Type: Grant
    Filed: June 5, 1995
    Date of Patent: January 1, 2002
    Assignee: Florida State University
    Inventors: Robert A. Holton, Ki-byung Chai, Hamid Idmoumaz, Hossain Nabizadeh, Yukio Suzuki
  • Chromatographic separation method of paclitaxel and cephalomannin
    Patent number: 6333419
    Abstract: A method for separating paclitaxel from cephalomannin and other related compounds by obtaining a starting material that contains paclitaxel and cephalomannin; dissolving the starting material in any one of a number of particularly defined solvents such as butyl formate and butyl acetate to form a mixture; subjecting the mixture to column chromatography to obtain an eluted fraction of paclitaxel, an eluted fraction of cephalomannin and a residue; and separately drying the paclitaxel and cephalomannin fractions to obtain separate crystalline forms of paclitaxel and cephalomannin, respectively.
    Type: Grant
    Filed: November 28, 2000
    Date of Patent: December 25, 2001
    Assignee: Indena SpA
    Inventors: Bruno Gabetta, Gianfranco Zini
  • Ureido and thioureido derivatives of 4-amino-2(5H)-furanones and 4-amino-2(5H)-thiophenones as antitumor agents
    Patent number: 6333346
    Abstract: The present invention relates to ureido and thioureido derivatives of 4-amino-2(5H)-furanones and 4-amino-2(5H0-thiophenones for the treatment of tumors.
    Type: Grant
    Filed: June 2, 2000
    Date of Patent: December 25, 2001
    Assignee: Roche Diagnostics GmbH
    Inventors: Ernesto Menta, Nicoletta Pescalli, Marco Conti, Gerd Zimmerman
  • Taxoids, their preparation and pharmaceutical compositions containing them
    Patent number: 6331635
    Abstract: New taxoids of general formula (I): their preparation and pharmaceutical compositions containing them. The new products of general formula (I) in which Z represents a radical of general formula (II): display noteworthy antitumour and antileukaemic properties.
    Type: Grant
    Filed: April 28, 1998
    Date of Patent: December 18, 2001
    Assignee: Aventis Pharma S.A.
    Inventors: Hervé Bouchard, Jean-Dominique Bourzat, Alain Commerçon
  • Tetraphosphonate bicyclic trisanhydrides
    Patent number: 6326490
    Abstract: Disclosed are novel bicyclic tris(anhydride)s useful as intermediates in the synthesis of biolologically active compounds, and the compounds which may be synthesized from such intermediates.
    Type: Grant
    Filed: October 10, 1997
    Date of Patent: December 4, 2001
    Assignee: Pharmasset, Ltd.
    Inventors: Krzysztof W. Pankiewicz, Krystyna Lesiak, Kyoichi A. Watanabe
  • Method of producing expoxides in the gaseous phase
    Patent number: 6323349
    Abstract: A method for epoxidation of olefins with 2 to 6 C atoms, especially propene, with hydrogen peroxide in the gas phase at a temperature below 250° C. The reaction is carried out by bringing a gas mixture containing the olefin, hydrogen peroxide and water into contact with the catalyst from the series of compounds of an element of the 4th to the 6th subgroup of the periodic table or of arsenic or selenium and molecular sieves in the absence of a liquid phase. Titanium-containing molecular sleeves are preferred catalysts.
    Type: Grant
    Filed: January 19, 2001
    Date of Patent: November 27, 2001
    Assignee: Degussa-Huls Aktiengesellschaft
    Inventors: Rüdiger Schütte, Georg Markowz, Peter Esser, Torsten Balduf, Georg Thiele, Steffen Hasenzahl
  • Piperidine-4 sulphonamide compounds
    Patent number: 6323217
    Abstract: A compound of formula (I): wherein: R1 represents hydrogen or alkyl, R2a and R2b represent a group selected from hydrogen, halogen, alkyl, hydroxy, alkoxy, trihaloalkyl, cyano, nitro, amino, alkylamino and dialkylamino, R3 represents hydrogen or hydroxy, X represents oxygen or methylene, V represents an alkylene chain that is optionally unsaturated and optionally substituted, U represents a bond or an alkylene chain, W represents a group selected from aryl and heteroaryl, each of those groups being optionally substituted by one or more identical or different groups, its isomers, its hydrates, its solvates and addition salts thereof with a pharmaceutically acceptable acid. Medicinal products containing the same which are useful in the treatment of diseases or pathological conditions in which endothelial dysfunction is known.
    Type: Grant
    Filed: January 30, 2001
    Date of Patent: November 27, 2001
    Assignee: Adir et Compagnie
    Inventors: Jean-Louis Peglion, Aimée Dessinges, Christophe Poitevin, Jean-Paul Vilaine, Nicole Villeneuve, Catherine Thollon, Marie-Pierre Bourguignon
  • Suksdorfin analogs, compositions thereof, and methods for making and using thereof
    Patent number: 6319929
    Abstract: The present invention is directed to compounds that are analogs of the natural product suksdorfin. Compounds of the present invention include those having Formula IV: wherein R20 through R26, M and Z are defined herein. The invention is also directed to pharmaceutical compositions and methods of using these compositions for treating retroviral infections.
    Type: Grant
    Filed: December 8, 1998
    Date of Patent: November 20, 2001
    Assignees: The University of North Carolina at Chapel Hill, Panacos Pharmaceuticals, Inc.
    Inventors: Kuo-Hsiung Lee, Yoshiki Kashiwada, Li Huang, Thomas Tung-Ying Lee, Mark Cosentino, Jim Snider, Mark Manak, Lan Xie
  • Compounds for treatment of cardiac arrhythmia synthesis, and methods of use
    Patent number: 6316487
    Abstract: The subject invention pertains to novel compounds, and compositions comprising the compounds, for the treatment of cardiac arrhythmias. The subject invention further concerns a method of making the novel compounds. The novel compounds are rapidly metabolized analogs of amiodarone, having the distinct and advantageous characteristic of being metabolized to a less lipophilic compound. The new compounds can have particular utility for treating life-threatening ventricular tachyarrhythmias, especially in patients with congestive heart failure (CHF). The product can also provide effective management for ventricular arrhythmias and supraventricular arrhythmias, including atrial fibrillation and re-entrant tachyarrhythmias involving accessory pathways.
    Type: Grant
    Filed: October 6, 2000
    Date of Patent: November 13, 2001
    Assignee: Aryx Therapeutics
    Inventors: Pascal Druzgala, Peter G. Milner
  • Epoxidation catalyst and process
    Patent number: 6310224
    Abstract: In a process for the production of an oxirane compound by reaction of olefins, oxygen and hydrogen using a noble metal on titanium or vanadium silicalite catalyst the improvement wherein the catalyst is doped with a substantially non-reduced metal dopand.
    Type: Grant
    Filed: January 19, 2001
    Date of Patent: October 30, 2001
    Assignee: ARCO Chemical Technology, L.P.
    Inventor: Roger A. Grey
  • Synthesis of paclitaxel from baccatin III by protection of the 7-hydroxyl of baccatin III using a strong base and an electrophile
    Patent number: 6307071
    Abstract: Process for synthesizing paclitaxel by treating baccatin III with a strong base in a solvent, adding an electrophile to the solution to form a 7-O-protected baccatin III derivative, reacting the 7-O-protected baccatin III derivative with a protected paclitaxel sidechain in a solvent such that the protected paclitaxel sidechain is coupled to the 13-hydroxyl of the 7-O-protected baccatin III, and subsequently deprotecting the protected paclitaxel sidechain and the 7-O protecting group to form paclitaxel, and intermediates used therein.
    Type: Grant
    Filed: February 1, 2000
    Date of Patent: October 23, 2001
    Assignee: Bristol-Myers Squibb Company
    Inventor: Francis S. Gibson