Patents Examined by Paul J. Killos
  • Compounds having selective activity for retinoid X receptors, and means for modulation of processes mediated by retinoid X receptors
    Patent number: 6610883
    Abstract: Compounds, compositions, and methods for modulating processes mediated by Retinoid X Receptors using retinoid-like compounds which have activity selective for members of the subclass of Retinoid X Receptors (RXRs), in preference to members of the subclass of Retinoic Acid Receptors (RARs). Examples of such compounds are bicyclic benzyl, pyridinyl, thiophene, furanyl, pyrrole, and polyenoic acid derivatives including carbocyclic polyenoic acids. The disclosed methods employ compounds for modulating processes selectively mediated by Retinoid X Receptors.
    Type: Grant
    Filed: July 13, 1998
    Date of Patent: August 26, 2003
    Assignee: Ligand Pharmaceuticals, Inc.
    Inventors: Marcus F. Boehm, Richard A. Heyman, Lin Zhi, Chan Kou (Jack) Hwang, Steve White, Alex Nadzan
  • Poly(3-cyclopropyl-3-hydroxypropionate) and processes for its preparation and derivatives thereof
    Patent number: 6610878
    Abstract: Poly(3-cyclopropyl-3-hydroxypropionates) (I) which are useful for the preparation of vinylcyclopropane and cyclopropylacetylene are disclosed. Methods for the preparation of a variety of intermediates obtained from (I) such as 3-cyclopropyl-3-hydroxypropionic acid and esters and salts thereof, 3-cyclopropylacrylic acid, and vinylcyclopropane also are disclosed.
    Type: Grant
    Filed: April 11, 2000
    Date of Patent: August 26, 2003
    Assignee: Eastman Chemical Company
    Inventors: John Clark Hubbs, Theresa Sims Barnette, Neil Warren Boaz
  • Process for the preparation of contrast agents
    Patent number: 6610885
    Abstract: Process for the preparation of contrast agents The invention provides a process for the preparation of an N-alkyl-acylamino-phenyl-carboxylic acid or carboxylic acid derivative by liquid phase acylation and subsequent N-alkylation of a corresponding amino-phenyl-carboxylic acid (or carboxylic acid derivative), the improvement comprising the addition of an alkylating agent to a solution containing the reaction products of said acylation, to effect said N-alkylation.
    Type: Grant
    Filed: June 17, 1998
    Date of Patent: August 26, 2003
    Assignee: Amersham Health AS
    Inventors: Trygve Gulbrandsen, Odd Einar Ingvoldstad, Lars Terje Holmaas
  • Synthetic method of &agr;-ketol unsaturated fatty acids
    Patent number: 6605741
    Abstract: The present invention provides an efficient synthetic method of &agr;-ketol unsaturated fatty acid having a double bond at a &bgr;-position to the ketone group thereof. It comprises the steps of: preparing compound (4) by reacting monosubstituted acetylene (2) with epoxide (3); and preparing &agr;-ketol unsaturated fatty acid (1) from said compound (4) as shown in Reaction Formula 1: wherein R1 represents an alkyl group of 1-18 carbon atoms or an aliphatic hydrocarbon group of 2-18 carbon atoms having 1-5 double or triple bonds at given positions; R2 represents a protecting group for a hydroxyl group; R3 represents a protecting group for a carboxyl group; R is identical to R1 or, when R1 has one or more triple bonds, represents an aliphatic hydrocarbon group in which each triple bond of R1 is converted to a double bond; and A represents an alkylene group of 1-18 carbon atoms.
    Type: Grant
    Filed: April 10, 2002
    Date of Patent: August 12, 2003
    Assignee: Shiseido Co., Ltd.
    Inventors: Yoshihiro Yokokawa, Koji Kobayashi, Shosuke Yamamura
  • Fluorescent dyes for the labeling of biological substrates
    Patent number: 6605740
    Abstract: This invention provides a new class of squaraine dyes having moieties which serve for the covalent attachment to biological substrates and resulting in the fluorescent labeling of the substrates. The labeled substrates are intended for use in analytical techniques for the detection and measurement of biological and clinical compounds of interest.
    Type: Grant
    Filed: April 2, 2001
    Date of Patent: August 12, 2003
    Inventor: Spyros Theodoropulos
  • Bicyclic enamide derivatives
    Patent number: 6603041
    Abstract: Enamide derivatives of formula (1) are described: wherein R1 is a group Ar1L2Ar2Alk- in which Ar1 is an optionally substituted aromatic or heteroaromatic group, L2 is a covalent bond or a linker atom or group, Ar2 is an optionally substituted arylene or heteroarylene group and Alk is a chain —CH2—CH(R)—, —CH═C(R)— or  in which R is a carboxylic acid (—CO2H) or a derivative or biostere thereof; R2 is a hydrogen atom or a C1-6alkyl group; X is an O or S atom or the group NR30 group; j and k is each zero or the integer 1 or 2 provided that the sum of j and k is zero or the integer 1 or 2; Cy1 is an optionally substituted cycloaliphatic, heterocycloaliphatic, aromatic or heteroaromatic group; and the salts, solvates, hydrates and N-oxides thereof.
    Type: Grant
    Filed: September 5, 2001
    Date of Patent: August 5, 2003
    Assignee: Celltech R & D Limited
    Inventors: Timothy John Norman, John Robert Porter, John Clifford Head, Andrew James Ratcliffe
  • Anhydride stabilization
    Patent number: 6603042
    Abstract: Disclosed herein are compositions comprising organic anhydrides having a reduced tendency to discolor with time, even when held at elevated temperatures for extended times. The compositions are produced by mixing at least one acid halide and various derivatives of hydroxy carboxylic acids with an anhydride to form a homogenous solution. Also disclosed is a process for preparing the compositions.
    Type: Grant
    Filed: August 20, 2002
    Date of Patent: August 5, 2003
    Assignee: Huntsman Petrochemical Corporation
    Inventor: Henry C. Brown
  • Method for producing catalysts containing metal nanoparticles on a porous support, especially for gas phase oxidation of ethylene and acetic acid to form vinyl acetate
    Patent number: 6603038
    Abstract: The invention relates to a method for producing a catalyst containing one or several metals from the group of metals comprising the sub-groups Ib and VIIIb of the periodic table on porous support particles, characterized by a first step in which one or several precursors from the group of compounds of metals from sub-groups Ib and VIIIb of the periodic table is or are applied to a porous support, and a second step in which the porous, preferably nanoporous support to which at least one precursor has been applied is treated with at least one reduction agent, to obtain the metal nanoparticles produced in situ in the pores of said support.
    Type: Grant
    Filed: April 28, 2000
    Date of Patent: August 5, 2003
    Assignee: Celanese Chemicals Europe GmbH
    Inventors: Alfred Hagemeyer, Uwe Dingerdissen, Klaus Kuhlein, Andreas Manz, Roland Fischer
  • Partially protected novel trisphenols and process for production thereof
    Patent number: 6603029
    Abstract: The invention provides a partially protected trisphenol having the general formula (I) wherein R1 is an alkyl group of 1-4 carbons or an alkoxyl group of 1-4 carbons, R2 is an alkyl group of 1-6 carbons or a cycloalkyl group of 5 or 6 carbons, X1 is a hydrogen atom, an alkoxycarbonylmethyl group wherein the alkyl group has 1-4 carbons, an alkoxycarbonyl group wherein the alkyl group has 1-4 carbons or a tetrahydropyranyl group, X2 is a hydrogen atom, an alkoxycarbonylmethyl group wherein the alkyl group has 1-4 carbons, an alkoxycarbonyl group wherein the alkyl group has 1-4 carbons or a tetrahydropyranyl group, provided that when X1 is a hydrogen atom, X2 is not a hydrogen atom, and when X2 is a hydrogen atom, X1 is not a hydrogen atom; and m is an integer of 0, 1 or 2, and n is an integer of 0, 1, 2 or 3.
    Type: Grant
    Filed: December 18, 2000
    Date of Patent: August 5, 2003
    Assignee: Honshu Chemical Industry Co., Ltd.
    Inventors: Taiichi Shiomi, Sachiko Miyagi, Toru Masuda
  • Compounds and methods for the inhibition of the expression of VCAM-1
    Patent number: 6602914
    Abstract: This invention is in the area of methods and compositions for the inhibition of the expression of VCAM-1 and, in particular, for the treatment of diseases mediated by VCAM-1, including cardiovascular and inflammatory diseases.
    Type: Grant
    Filed: April 2, 2002
    Date of Patent: August 5, 2003
    Assignee: AtheroGenics, Inc.
    Inventor: Charles Q. Meng
  • Unsaturated oxyalkylene esters and uses thereof
    Patent number: 6599937
    Abstract: The invention relates to methods of modulating gene expression in a hematopoietic cell or augmenting hematopoiesis in a host, as well as methods of treating, preventing, or ameliorating disorders affecting hematopoiesis level in a host, by administering to the host or the hematopoietic cell an effective amount of a compound of formula (I).
    Type: Grant
    Filed: September 25, 2000
    Date of Patent: July 29, 2003
    Assignee: Beacon Laboratories, Inc.
    Inventors: Edward Neiss, Bernard Loev
  • Cleavable, water-soluble surfactants
    Patent number: 6600076
    Abstract: The present invention provides a novel class of water-soluble cleavable surfactants and methods for utilizing these surfactants.
    Type: Grant
    Filed: October 12, 1999
    Date of Patent: July 29, 2003
    Assignees: The Regents of the University of California, Wisconsin Alumni Research Foundation
    Inventors: Nicholas L. Abbott, Lana I. Jong
  • Derivatives of phenyl 4-aminosalicylate and method of making the same
    Patent number: 6600063
    Abstract: The present invention relates to novel antimycobacterial compounds and in particular to antimycobacterial compounds comprised of derivatives of phenyl 4-aminosalicylate. This invention further relates to methods for their preparation, to their use as therapeutic agents and to pharmaceutical compositions containing them. The novel methods of the invention yield derivatives of phenyl 4-aminosalicylate on a multi-gram scale and in high purity for subsequent biological evaluation in drug discovery.
    Type: Grant
    Filed: October 23, 2000
    Date of Patent: July 29, 2003
    Assignee: Board of Trustees of Wellesley College
    Inventor: Michael J. Hearn
  • Methods for making 2-(&ohgr;-alkoxycarbonylalkanoyl)-4-butanolide, ester of &ohgr;-hydroxy-(&ohgr;-3)-ketoaliphatic acid, and derivatives thereof
    Patent number: 6600070
    Abstract: In industrial production of &ohgr;-hydroxyaliphatic acid being an important intermediate for large cyclic lactone-based perfumes, using dicarboxylate ester which is inexpensive and readily obtainable, a method, with high yield and improved selectively, for making a 2-(&ohgr;-alkoxycarbonylalkanoyl)-4-butanolide and an alkaline metal salt thereof, an ester of &ohgr;-hydroxy-(&ohgr;-3)-ketoaliphatic acid as a novel compound and a derivative thereof, and a method for making the same are provided.
    Type: Grant
    Filed: November 29, 2001
    Date of Patent: July 29, 2003
    Assignee: Soda Aromatic Co., Ltd.
    Inventors: Hideaki Takaoka, Sigeru Wada, Nobuhiko Ito, Akio Hasebe, Shinzo Imamura, Hideo Muraoka
  • Matrix metalloproteinase inhibitors
    Patent number: 6600057
    Abstract: The present invention provides compounds that are effective in treating disorders caused by the enzymatic activity of matrix metalloproteinases. These disorders include, but are not limited to, rheumatoid arthritis, osteoarthritis, periodontal disease, aberrant angiogenesis, tumor invasion and metastasis, corneal ulceration, and in complications of diabetes. The present invention is also is useful for treating wounds.
    Type: Grant
    Filed: December 29, 2000
    Date of Patent: July 29, 2003
    Assignee: Kimberly-Clark Worldwide, Inc.
    Inventor: Stephen Quirk
  • Enhancement of the efficacy of benzoylbenzenes
    Patent number: 6596775
    Abstract: The invention relates to method for the enhancement of the activity and/or systemicity of fungicidal compositions containing at least one benzoylbenzene of formula I wherein R1 through R7, m and n are as defined in claim 1, with the aid of one or more adjuvants selected from the group consisting of (a) alkylpolyglycosides, alkenyl succinic acid derivatives, dialkyl sulfosuccinates, polyvinylpyrrolidones, perfluoroalkyl acids derivatives, perfluoro(C3-20)alkyl esters of carboxylic acids, and mixtures thereof; (b) alkoxylated alcohols, amines or acids; (c) water-immiscible polar aprotic solvents; and to the use of such a composition as a fungicide.
    Type: Grant
    Filed: August 28, 2001
    Date of Patent: July 22, 2003
    Assignee: BASF Aktiengesellschaft
    Inventors: Michael Aven, Henry Van Tuyl Cotter
  • Fused bicyclic or tricyclic amino acids
    Patent number: 6596900
    Abstract: The compounds of the instant invention are bicyclic or tricyclic amino acids useful in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, pain, arthritis, neuropathological disorders, sleep disorders, visceral pain disorders, and gastrointestinal disorders. Processes for the preparation of the final products and intermediates useful in the process are included. Pharmaceutical compositions containing one or more of the compounds are also included.
    Type: Grant
    Filed: April 16, 2002
    Date of Patent: July 22, 2003
    Assignee: Pfizer Inc
    Inventors: David Clive Blakemore, Justin Stephen Bryans, Sophie Caroline Williams
  • Substituted cyclopentenes, their preparation and their use for chiral scaffolds
    Patent number: 6593489
    Abstract: 3,4-Disubstituted-1-cyclopentene compounds, in substantially enantiopure form, have the relative stereochemistry according to formula (1A) or (1B) including the opposite enantiomers thereof, wherein R1 is either COOX, wherein X is selected from the group consisting of alkyl, H, and a salt-forming cation, or CH2OH, whererin the hydroxy group is optionally protected; R2 is H or a protecting group; R3 is H or alkyl, and R4 is selected from the group consisting of H, alkoxy, alkyl, aryl, and aralkyl; or, in the case of formula (1A), R2 and R4 are linked to form an oxazolidonone ring. These compounds can be used to prepare a series of complementary stereochemcially varied cyclopentane scaffolds.
    Type: Grant
    Filed: September 11, 2000
    Date of Patent: July 15, 2003
    Assignee: ChirotechTechnology Limited
    Inventors: Mark Edward Brennan Smith, Nadine Derrien
  • Diflunisal esters and related compounds
    Patent number: 6593365
    Abstract: O-medium alkyl esters of diflunisal and related compounds are disclosed having anti-platelet activity, hydroxy radical scavenging properties, enhanced hepatic clearance and low ulcerogenic potential. These compounds have general formula (I) wherein n equals 3-13.
    Type: Grant
    Filed: October 12, 1999
    Date of Patent: July 15, 2003
    Assignee: The University of Queensland
    Inventors: Daniel Yung-Yu Hung, Michael Stephen Roberts
  • RXR modulators with improved pharmacologic profile
    Patent number: 6593493
    Abstract: The present invention provides a novel class of RXR modulator compounds that exhibit an improved pharmacologic profile relative to the profile of previously studied RXR modulators, including those that share common structural features with the presently claimed modulators. The present invention also provides synthetic methods for preparing these compounds as well as pharmaceutical compositions incorporating these novel compounds and methods for the therapeutic use of such compounds and pharmaceutical compositions.
    Type: Grant
    Filed: September 14, 2000
    Date of Patent: July 15, 2003
    Assignee: Ligand Pharmaceuticals, Inc.
    Inventors: Robert J. Ardecky, Marcus F. Boehm, Amy L. Faulkner, Lawrence G. Hamann, Todd K. Jones, Christopher M. Mapes, Pierre-Yves Michellys, John S. Tyhonas, Anthony W. Thompson, Jyun-Hung Chen