Patents Examined by Mukund J. Shah
  • Patent number: 6514966
    Abstract: NPY antagonists, methods of using such NPY antagonists and pharmaceutical compositions containing such NPY antagonists. The NPY antagonists are useful for the treatment of NPY mediated disease/conditions including obesity.
    Type: Grant
    Filed: January 4, 2001
    Date of Patent: February 4, 2003
    Assignee: Pfizer Inc.
    Inventors: Richard L. Elliott, Richard F. Hank, Marlys Hammond
  • Patent number: 6515159
    Abstract: An S,S-ethylenediamine-N,N′-disuccinic acid iron alkali salt which contains a lactam compound represented by the following general formula (1): wherein M is an ammonium ion or an alkali metal ion, and an ethylenediaminemonosuccinic acid represented by the following general formula (2): wherein M is an ammonium ion or an alkali metal ion, in an amount of 7 wt % or less, respectively.
    Type: Grant
    Filed: August 17, 2001
    Date of Patent: February 4, 2003
    Assignee: Mitsubishi Rayon Co., Ltd.
    Inventors: Toshitake Yamakawa, Haruo Sakai
  • Patent number: 6515168
    Abstract: The present invention relates to an energy and effluent saving process for the production of N-phosphonomethyl iminodiacetic acid (PMIDA), an intermediate in the preparation of glyphosate. An alkali metal salt of iminodiacetic acid is reacted with phosphorous acid and a strong mineral acid, or a source thereof to form iminodiacetic phosphite and the alkali metal salt of the strong mineral acid. After removal of the latter salt, the iminodiacetic phosphite is converted to PMIDA by reaction with formaldehyde. PMIDA is recovered and the solution remaining can be recycled in the process.
    Type: Grant
    Filed: March 19, 2001
    Date of Patent: February 4, 2003
    Assignees: Crop Protection Holdings SDN BHD, Agriguard Limited
    Inventor: Brian Parker
  • Patent number: 6511991
    Abstract: The present invention relates to nitric oxide-releasing amidine- and enamine-derived diazeniumdiolates, compositions comprising such compounds, methods of using such compounds and compositions, and to a method for the preparation of nitric oxide-releasing amidine and enamine derived diazeniumdiolates via the direct reaction of nitric oxide with amidines and enamines, and to a method of converting amines into such compounds.
    Type: Grant
    Filed: April 3, 2001
    Date of Patent: January 28, 2003
    Assignee: The United States of America as represented by the Department of Health and Human Services
    Inventors: Joseph A. Hrabie, Larry K. Keefer
  • Patent number: 6511975
    Abstract: A compound of the formula (I) wherein R1 and R2 is a substituted or unsubstituted aryl group, or a substituted or unsubstituted heteroaryl group. A is CH2, CO or SO2. B is a single bond, alkylene or alkenylene. D is O or S. E is alkylene or alkenylene. wherein G is a substituted or unsubstituted cycloalkene ring, or a substituted cycloalkane ring. Ar is a substituted or unsubstituted aryl ring, or a substituted or unsubstituted heteroaryl ring. R3 is alkyl. n is 1-3. The invention includes a pharmacologically acceptable salt, ester or other derivative of a compound of the formula (I). The invention also provides pharmaceutical compositions and methods of treating specified diseases utilizing a compound of formula (I).
    Type: Grant
    Filed: July 13, 2000
    Date of Patent: January 28, 2003
    Assignee: Sankyo Company, Limited
    Inventors: Takahide Nishi, Takeshi Yamaguchi, Yukiko Iio, Toshiyasu Takemoto, Katsuyoshi Nakajima
  • Patent number: 6511987
    Abstract: Disclosed are compounds of the formula: and the pharmaceutically acceptable salts thereof, wherein W, Q, X, X1, Y and Z are as defined herein. These compounds bind with high selectivity and/or high affinity to the benzodiazepine site of GABAA receptors and are therefore useful in the treatment of central nervous system (CNS) diseases and as probes for the localization of GABAA receptors in tissue samples. Also disclosed are intermediates useful in the preparation of these compounds.
    Type: Grant
    Filed: November 10, 2000
    Date of Patent: January 28, 2003
    Assignee: Neurogen Corporation
    Inventors: Jun Yuan, Pamela Albaugh, Kenneth Shaw, Alan Hutchinson
  • Patent number: 6509328
    Abstract: The present invention is a compound of formula wherein X is an ethynediyl group, R1, R2 and R3 are as defined in the specification.
    Type: Grant
    Filed: October 13, 2000
    Date of Patent: January 21, 2003
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Geo Adam, Alexander Alanine, Erwin Goetschi, Vincent Mutel, Thomas Johannes Woltering
  • Patent number: 6509498
    Abstract: The invented process produces sorbic acid or its salt through the decomposition of a polyester obtained from ketene and aldehyde, and includes the step of treating a solution containing-sorbic acid or its salt with a chemically activated carbon, which sorbic acid or its salt is produced by the decomposition of the polyester. The treatment with activated carbon is performed, for example, at pH ranging from 5.8 to 7.5 at temperatures ranging from 30° C. to 80° C. The invented process can efficiently remove colored substances and can easily yield a high quality sorbic acid having a satisfactory hue in a high yield.
    Type: Grant
    Filed: May 26, 2000
    Date of Patent: January 21, 2003
    Assignee: Daicel Chemical Industries, Ltd.
    Inventors: Akira Yamashita, Mitsuhiro Kouno
  • Patent number: 6509354
    Abstract: 3-Arylphenyl sulfide derivatives represented by general formula (I): (wherein R is a C2-C6 alkyl group, a C2-C6 alkenyl group, a C2-C6 alkynyl group or the like, B0 to B2 and B3 are hydrogen atoms, halogen atoms, cyano groups, C1-C4 haloalkyl groups or the like, n is 0, 1 or 2, and Ar is a phenyl ring, a pyridine ring, a thiophene ring, a pyrazole ring or the like), and insecticides and miticides containing the 3-arylphenyl sulfide derivatives as an active ingredient.
    Type: Grant
    Filed: October 27, 2000
    Date of Patent: January 21, 2003
    Assignees: Kumiai Chemical Industry Co., Ltd., Ihara Chemical Industry Co., Ltd.
    Inventors: Keiji Toriyabe, Nobuo Takefuji, Minoru Itou, Tetsuya Hirade, Kiyotoshi Nishiyama, Mitsuharu Asahida, Yasunobu Maeda, Nobuhide Wada, Toyokazu Fujisawa, Hiroyuki Yano, Masaaki Komatsu, Osamu Tada
  • Patent number: 6506756
    Abstract: The present invention discloses novel substituted imidazole compounds which have dual histamine-H1 and H3 receptor antagonist activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such imidazoles as well as methods of using them to treat allergy, inflammatory and CNS-related diseases and others.
    Type: Grant
    Filed: September 18, 2001
    Date of Patent: January 14, 2003
    Assignee: Schering Corporation
    Inventors: Neng-Yang Shih, Daniel M. Solomon, John J. Piwinski, Andrew T. Lupo, Jr., Michael J. Green
  • Patent number: 6506932
    Abstract: A method for oxidizing an aromatic compound possesssing at least one alkyl substituent by using a catalyst avoids containing a corrosive bromine ion, remains stably without being decomposed even in an oxidizing atmospherfe, and permits reclamation is provided. An aromatic compound possessing at least one alkyl substituent is oxidized by using a catalyst which has at least one kind of element selected from the group consisting of phosphorus, silicon, and germanium as a hetero atom and at least one kind of element selected from the group consisting of molybdenum, tungsten, vanadium, and niobium as a poly atom and comprises a heteropoly-oxometalate anion possessing two defective structure site and at least one kind of element selected from the group of elements of Periods 4˜6 of Groups IB, VA,VIIA, and VIII in the Periodic Table of the Elements.
    Type: Grant
    Filed: November 7, 2001
    Date of Patent: January 14, 2003
    Assignee: Nippon Shokubai Co., Ltd.
    Inventors: Yasutaka Sumida, Masahiro Wada, Noritaka Mizuno
  • Patent number: 6506768
    Abstract: The present invention concerns the compounds of formula the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein R1 is hydrogen, optionally substituted C1-6alkyl, aryl; R2 is each independently a halogen, hydroxy, C1-6alkyl, C1-6alkyloxy or nitro; n is 0, 1, 2 or 3; Alk is C1-6alkanediyl; D is an optionally substituted saturated or unsaturated nitrogen containing heterocycle; and aryl is optionally substituted phenyl; having a great therapeutic breadth. It further relates to their use as a medicine, their preparation as well as compositions containing them.
    Type: Grant
    Filed: August 15, 2001
    Date of Patent: January 14, 2003
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Ludo Edmond Josephine Kennis, Josephus Carolus Mertens
  • Patent number: 6506758
    Abstract: A compound of formula (I): or a salt thereof, or a solvate thereof, wherein: A represents an optionally substituted aryl group or an optionally substituted heterocyclyl group; Ra represents —CO—NRsRt wherein Rs and Rt each independently represent hydrogen, alkyl, substituted alkyl, optionally substituted alkenyl, optionally substituted aryl, optionally substituted arylalkyl, optionally substituted heterocyclyl or an optionally substituted heterocyclylalkyl group, or Rs and Rt together with the nitrogen to which they are attached form a heterocyclyl group; R1 and R2 each independently represents hydrogen, hydroxy, amino, alkoxy, optionally substituted aryloxy, optionally substituted benzyloxy, alkylamino, dialkylamino, halo, trifluoromethyl, trifluoromethoxy, nitro, alkyl, carboxy, carbalkoxy, carbamoyl, alkylcarbamoyl, or R1 and R2 together represent methylenedioxy, carbonyldioxy or carbonyldiamino; and R3 represents hydrogen, alkanoyl, alkyl, aminoalkyl, hydroxyalkyl, carbox
    Type: Grant
    Filed: October 11, 2001
    Date of Patent: January 14, 2003
    Assignees: SmithKline Beecham Laboratoires Pharmceutiques, SmithKline Beecham SpA
    Inventors: Stefania Gagliardi, Guy Marguerite Marie Gerard Nadler, Pietro A T Novella
  • Patent number: 6506743
    Abstract: Compounds of formula wherein A is an unsubstituted or substituted aromatic or non-aromatic, monocyclic or bicyclic heterocyclic radical wherein a ring nitrogen atom may have been replaced by a group R1 is hydrogen or C1-C3alkyl; R2 is hydrogen or C1-C3alkyl; R3 is hydrogen, an unsubstituted or substituted C1-C3-C6alkyl, C6cycloalkyl, C2-C6alkenyl or C2-C6alkynyl group, or C(═O)—R5, R5 is C1-C4alkyl, C1-C4alkoxy, an unsubstituted or substituted phenyl, phenoxy or benzyloxy group, or N(R6)2, each R6, independently of the other, is hydrogen, C1-C4alkyl or unsubstituted or substituted phenyl, X is CH—NO2, N—CN or N—NO2 and n is from 1 to 3, in free form or in salt form, and, where appropriate, tautomers of those compounds and the salts thereof, can be used as agrochemical active ingredients and can be prepared in a manner known per se.
    Type: Grant
    Filed: December 11, 2001
    Date of Patent: January 14, 2003
    Assignee: Syngenta Investment Corporation
    Inventors: Peter Maienfisch, Jozef Gonda, Olivier Jacob, Laurenz Gsell
  • Patent number: 6503910
    Abstract: Compounds of the formula (B)2N—X—(CH2)n—CR1R2—CO—Y  (I) have therapeutic utility as inhibitors of metalloproteinases etc.
    Type: Grant
    Filed: August 11, 2000
    Date of Patent: January 7, 2003
    Assignee: Darwin Discovery Ltd.
    Inventors: Andrew Douglas Baxter, David Alan Owen, Robert John Watson, John Gary Montana
  • Patent number: 6503949
    Abstract: Disclosed is a novel class of compounds of formula (I) wherein V, A, Y, Z, R1, E, X and D are as defined in the specification. These compounds act to antagonize the action of the glucagon hormone on the glucagon receptor. Owing to their antagonizing effect of the glucagon receptor, the compounds are suitable for treating or preventing glucagon-mediated conditions and diseases such as hyperglycemia, Type 1 diabetes, Type 2 diabetes and obesity.
    Type: Grant
    Filed: May 16, 2000
    Date of Patent: January 7, 2003
    Assignee: Noro Nordisk A/S
    Inventors: Jesper Lau, Peter Madsen, Christian Sams, Carsten Behrens, Josef Vagner, Inge Thøger Christensen, Behrend Frederik Lundt, Ulla Grove Sidelmann, Henning Thøgersen, Anthony L. Ling, Michael Bruno Plewe, Larry Kenneth Truesdale, Shenghua Shi
  • Patent number: 6504047
    Abstract: The present invention is directed towards compounds of the general formula (I) (I) are important intermediates for the preparation of pharmaceuticals. Further intermediates, process for the preparation of (I) and use thereof.
    Type: Grant
    Filed: April 25, 2001
    Date of Patent: January 7, 2003
    Assignee: Degussa AG
    Inventor: Günter Knaup
  • Patent number: 6503908
    Abstract: There is provided compounds of formula I, wherein R1, R2, R3 and Het1 have meanings given in the description, which are useful in the curative and prophylactic treatment of medical conditions for which inhibition of a cyclic guanosine 3′,5′-monophosphate phosphodiesterase (e.g. cGMP PDE5) is desired.
    Type: Grant
    Filed: October 6, 2000
    Date of Patent: January 7, 2003
    Assignee: Pfizer Inc
    Inventor: Graham Nigel Maw
  • Patent number: 6504028
    Abstract: The present invention relates to a process for forming polymer conjugates which are useful as enzyme inhibitors. The process of the present invention comprises the steps of: a) reacting a polymer or copolymer alcohol to form a chloroformate; b) combining a substituted or unsubstituted anthranilic acid comprising an enzyme interaction attenuating unit; and a base catalyst wherein the base catalyst is a supported base catalyst, to form a substrate reactive admixture; and c) adding to said chloroformate formed in step (a) said substrate reactive admixture formed in step (b) to form a benzoxazin-4-one conjugate.
    Type: Grant
    Filed: June 26, 2001
    Date of Patent: January 7, 2003
    Assignee: The Procter & Gamble Co.
    Inventors: Renae Dianna Fossum, Todd Laurence Underiner
  • Patent number: 6503905
    Abstract: The present invention relates to compounds of the formula I, wherein Z1, Z2, X, Q, R1, R2 and R3 are defined as in the specification, pharmaceutical compositions containing such compounds the use of such compounds to treat neurological and gastrointestinal disorders.
    Type: Grant
    Filed: August 6, 1999
    Date of Patent: January 7, 2003
    Assignee: Pfizer Inc
    Inventors: Spiros Liras, Martin P. Allen, Barbara E. Segelstein