Patents Examined by John Kight
  • Patent number: 6090168
    Abstract: The present application relates to a series of novel sulfonic acid metal cation salts of the formula ##STR1## which are useful intermediates to prepare antifolate 5-substituted pyrrolo[2,3-d]pyrimidines. The present invention also relates to a novel process for preparing the sulfonic acid metal cation salts and to a novel process for preparing aldehydes of the formula ##STR2## from the corresponding sulfonic acid metal cation salts.
    Type: Grant
    Filed: October 6, 1999
    Date of Patent: July 18, 2000
    Assignee: Eli Lilly and Company
    Inventors: Douglas Patton Kjell, Brian James Slattery, Charles Jackson Barnett
  • Patent number: 6090571
    Abstract: Novel heterocyclic compounds which generate chemiluminescence on reaction with a phosphatase enzyme are provided as well as a process for their preparation and intermediates useful therein. The compounds comprise a nitrogen, oxygen or sulfur-containing heterocyclic ring system bearing an exocyclic carbon-carbon double bond. The double bond is further substituted at the distal carbon with a phosphate group and an oxygen or sulfur atom-containing group.Novel compositions further comprising a cationic aromatic compound (CAC) in addition to the heterocyclic phosphate compound are provided. The addition of the CAC in the composition greatly increases the production of chemiluminescence and provides improved detection sensitivity. Compositions further comprising an anionic surfactant and a non-ionic surfactant provide additional improvements in detection sensitivity.
    Type: Grant
    Filed: July 21, 1999
    Date of Patent: July 18, 2000
    Assignee: Lumigen, Inc.
    Inventors: Hashem Akhavan-Tafti, Zahra Arghavani, Renuka DeSilva
  • Patent number: 6087367
    Abstract: The present invention provides the compound having the structure: ##STR1## wherein each of R.sub.1 and R.sub.2 are independently the same as or different from each other; when R.sub.1 and R.sub.2 are the same, each is a substituted or unsubstituted arylamino, cycloalkylamino, pyridineamino, piperidino, 9-purine-6-amine, or thiozoleamino group; when R.sub.1 and R.sub.2 are different, R.sub.1 =R.sub.3 --N--R.sub.4, wherein each of R.sub.3 and R.sub.4 are independently the same as or different from each other and are a hydrogen atom, a hydroxyl group, a substituted or unsubstituted, branched or unbranched alkyl, alkenyl, cycloalkyl, aryl, alkyloxy, aryloxy, arylalkyloxy, or pyridine group, or R.sub.3 and R.sub.4 bond together to form a piperidine group and R.sub.2 is a hydroxylamino, hydroxyl, amino, alkylamino, dialkylamino or alkyloxy group; and n is an integer from about 4 to about 8.
    Type: Grant
    Filed: May 18, 1999
    Date of Patent: July 11, 2000
    Assignees: Sloan-Kettering Institute for Cancer Research, The Trustees of Columbia University in the City of New York
    Inventors: Ronald Breslow, Paul A. Marks, Richard A. Rifkind, Branko Jursic
  • Patent number: 6087346
    Abstract: The invention relates to methods for the treatment of central nervous system disorders, neurological disorders, gastrointestinal disorders, drug abuse, angina, migraine, hypertension and depression by administering a pharmaceutical composition comprising an effective amount of certain sigma receptor ligands to a patient in need of such treatment. The invention further relates to novel sigma receptor ligands having high binding to the sigma receptor and pharmaceutical compositions thereof.
    Type: Grant
    Filed: February 21, 1996
    Date of Patent: July 11, 2000
    Assignees: Cambridge Neuroscience, Inc., Virginia Commonwealth University
    Inventors: Richard A. Glennon, James B. Fischer
  • Patent number: 6083977
    Abstract: Novel trienoic retinoid compounds having activity for retinoic acid receptors and retinoid X receptors are provided. Also provided are pharmaceutical compositions incorporating such compounds and methods for their use.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: July 4, 2000
    Assignee: Ligand Pharmaceuticals Incorporated
    Inventors: Marcus F. Boehm, Lin Zhang, Alex M. Nadzan
  • Patent number: 6080780
    Abstract: Methods of treating anxiety with flavonoid compounds according to Formula (I) and dimers thereof, compounds of Formula (I) and dimers thereof, use of compounds of Formula (I) and pharmaceutical formulations comprising flavonoids of Formula (I) and dimers thereof.
    Type: Grant
    Filed: July 8, 1998
    Date of Patent: June 27, 2000
    Assignee: University of Strathclyde
    Inventors: Alejandro Constantino Paladini, Jorge Horacio Medina
  • Patent number: 6080782
    Abstract: Compounds of formula I are selective cyclic nucleotide phosphodiesterase (PDE) inhibitors (namely of type IV). They and pharmaceutical compositions in which they are active ingredients are useful as bronchial therapeutics, for elimination of erectile dysfunction and for treatment of disorders, particularly those of inflammatory nature. The compounds are distinguished by low toxicity, good enteral absorption (high bioavailability), a great therapeutic breadth and the absence of significant side effects.
    Type: Grant
    Filed: November 18, 1997
    Date of Patent: June 27, 2000
    Assignee: BYK Gulden Lomberg Chemische Fabrik GmbH
    Inventors: Wolf-Rudiger Ulrich, Thomas Martin
  • Patent number: 6080865
    Abstract: Methyl-5-(3-methyl piperidino)pentanamines of general formula ##STR1## in which one of the two radicals R.sup.1, R.sup.2 is hydrogen and the other methyl, are produced by two-stage hydrogenation from 2-methyl glutaronitrile. The compounds are suitable as catalysts in the production of polyurethanes.
    Type: Grant
    Filed: October 20, 1997
    Date of Patent: June 27, 2000
    Assignee: Lonza AG
    Inventors: Josef Heveling, Andreas Gerhard
  • Patent number: 6077956
    Abstract: The invention relates to a process for preparing 1,2,3,6-tetrahydro-2,2,6,6-tetramethylpyridine from 4-hydroxy-2,2,6,6-tetramethylpiperidine in which 4-hydroxy-2,2,6,6-tetramethylpiperidine is dehydrated at elevated temperature in the gas phase over a solid acid catalyst.
    Type: Grant
    Filed: July 24, 1998
    Date of Patent: June 20, 2000
    Assignee: Huels Aktiengesellschaft
    Inventors: Manfred Kaufhold, Udo Jegelka
  • Patent number: 6075145
    Abstract: Catalyst compositions based on amorphous partially dehydrated zirconium hydroxide which are doped with from 0.01 to 20 atom percent of copper and/or from 0.01 to 20 atom percent of nickel, in each case based on zirconium, and have a specific surface area by the BET method of at least 50 m.sup.2 /g. The catalyst compositions are suitable, in particular, as the catalyst in hydrogen transfer reactions, such as, the Meerwein-Ponndorf-Verley reduction or the Oppenauer oxidation. The preparation of 3-hydroxyquinuclidine of the formula: ##STR1## involves reaction of quinuclidin-3-one with a secondary alcohol in the presence of the amorphous partially dehydrated zirconium hydroxide.
    Type: Grant
    Filed: March 6, 1998
    Date of Patent: June 13, 2000
    Assignee: Lonza AG
    Inventors: Josef Heveling, David Laffan, Alain Wellig
  • Patent number: 6071912
    Abstract: This invention is directed to benzamidine derivatives substituted by amino acid and hydroxy acid derivatives which are useful as anti-coagulants. This invention is also directed to pharmaceutical compositions containing the compounds of the invention, and methods of using the compounds to treat disease-states characterized by thrombotic activity.
    Type: Grant
    Filed: September 9, 1999
    Date of Patent: June 6, 2000
    Assignee: Berlex Laboratories, Inc.
    Inventors: Monica Kochanny, Raju Mohan, Michael M. Morrissey, Howard P. Ng, Weiya Yun
  • Patent number: 6071928
    Abstract: The present invention relates to compounds of formula (I), wherein R is C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkylC.sub.1-4 alkyl, which groups are optionally substituted by hydroxy, C.sub.1-4 alkoxy or NR.sup.a R.sup.b, where R.sup.a and R.sup.b each independently repesent hydrogen or C.sub.1-4 alkyl; or R is C.sub.1-4 alkyl substituted by Ar, and optionally further substituted by one or both of R.sup.4 and R.sup.5 ; R.sup.1, R.sup.2 and R.sup.3 represent a variety of substituents; R.sup.9 and R.sup.10 are each hydrogen, halogen, C.sub.1-6 alkyl, CH.sub.2 OR.sup.c, oxo, CO.sub.2 R.sup.a or CONR.sup.a R.sup.b where R.sup.c represents hydrogen, C.sub.1-6 alkyl or phenyl; X is --CH.sub.2, or --CH.sub.2 CH.sub.2 --; Y is --CH--, --CH.sub.2 --, --CH.sub.2 CH-- or --CH.sub.2 CH.sub.2 --, with the proviso that the sum total of carbon atoms in X+Y is 2 or 3; and when Y is --CH-- or --CH.sub.
    Type: Grant
    Filed: December 16, 1998
    Date of Patent: June 6, 2000
    Assignee: Merck Sharp & Dohme, Ltd.
    Inventors: Neil Roy Curtis, Ian Thomas Huscroft, Janusz Jozef Kulagowski, Christopher John Swain
  • Patent number: 6071927
    Abstract: The present invention relates to certain spiro-piperdine derivatives which are tachykinnin antagonists and are useful, for example, in the treatment or prevention of pain, inflammation, migraine, emesis and postherpetic neuralgia.
    Type: Grant
    Filed: December 16, 1998
    Date of Patent: June 6, 2000
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Raymond Baker, Neil Roy Curtis, Jason Matthew Elliott, Timothy Harrison, Gregory John Hollingworth, Philip Stephen Jackson, Janusz Jozef Kulagowski, Eileen Mary Seward, Christopher John Swain, Brian John Williams
  • Patent number: 6071965
    Abstract: The present invention relate to phosphinic alkanoic acid derivatives that inhibit N-Acetylated .alpha.-Linked Acidic Dipeptidase (NAALADase) enzyme activity, pharmaceutical compositions comprising the same, and methods of using the same to inhibit NAALADase activity and to treat glutamate abnormalities and prostate diseases.
    Type: Grant
    Filed: December 31, 1997
    Date of Patent: June 6, 2000
    Assignee: Guilford Pharmaceuticals Inc.
    Inventors: Paul F. Jackson, Weixing Li, Keith M. Maclin, Kevin L. Tays, Takashi Tsukamoto, Barbara S. Slusher
  • Patent number: 6071953
    Abstract: Chromans of formula I ##STR1## with the meanings of R(A), R(B) and R(1) to R(8) stated in the specification are suitable for producing a medicament for blocking the K.sup.+ channel that is opened by cyclic adenosine monophosphate (cAMP); also for producing medicaments for inhibiting gastric acid secretion; for the treatment of ulcers of the stomach and the intestinal region, in particular the duodenum, for the treatment of reflux esophagitis, for the treatment of diarrheal disorders, for the treatment and prevention of all types of arrhythmias, including atrial, ventricular and supraventricular arrhythmias, for controlling reentry arrhythmias and for preventing sudden heart death as a result of ventricular fibrillation.
    Type: Grant
    Filed: February 19, 1998
    Date of Patent: June 6, 2000
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Hans Jochen Lang, Joachim Brendel, Uwe Gerlach, Klaus Weidmann
  • Patent number: 6071954
    Abstract: The invention encompasses the novel compound of Formula I useful in the treatment of cyclooxygenase-2 mediated diseases. ##STR1## The invention also encompasses certain pharmaceutical compositions for treatment of cyclooxygenase-2 mediated diseases comprising compounds of Formula I.
    Type: Grant
    Filed: March 13, 1998
    Date of Patent: June 6, 2000
    Assignee: Merk Frosst Canada, Inc.
    Inventors: Yves LeBlanc, Patrick Roy, Serge Leger, Erich Grimm, Zhaoyin Wang
  • Patent number: 6066642
    Abstract: The present invention provides certain novel compounds, compositions, and a method of treating a mammal by blocking its adenosine receptors comprising administering at least one compound of the present invention. Examples of the present inventive compounds include certain flavonoids of formulae (I) and (II), wherein R.sub.1 to R.sub.4 are as defined in the description, and M is --CH(OH)--CH(R.sub.2)-- or --C(OH).dbd.C(R.sub.2)-- and R.sub.1, R.sub.2 are as defined in the description; or dihydropyridines of formula (III), wherein R.sub.2 to R.sub.6 are as defined in the description; or pyridines of formula (IV), wherein R.sub.2 to R.sub.6 are as defined in the description, or triazoloquinazolines of formula (V), wherein R.sub.1 and R.sub.2 are as defined in the description; and their derivatives, or pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: December 7, 1998
    Date of Patent: May 23, 2000
    Assignee: The United States of America as represented by the Department of Health and Human Services
    Inventors: Kenneth A. Jacobson, Ji-Long Jiang, Yong-Chul Kim, Yishai Karton, Albert M. Van Rhee
  • Patent number: 6063940
    Abstract: A 1-bromoalkylbenzene derivative is prepared by reacting a phenylalkene derivative with hydrogen bromide in the presence of a non-polar solvent. The phenylalkene derivative is prepared by reacting an alkenyl halide with metal magnesium to form a Grignard reagent, and then reacting the Grignard reagent with a benzyl halide derivative. An allyl Grignard reagent is prepared by reacting continuously an allyl halide derivative with metal magnesium in an organic solvent, in which the allyl halide derivative and metal magnesium are continuously added to the reaction system and the allyl Grignard reagent formed is continuously removed from the reaction system. The processes provide the intended compounds in high yields, high selectivities and high purities.
    Type: Grant
    Filed: February 13, 1997
    Date of Patent: May 16, 2000
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Hiroaki Fujishima, Yasunobu Miyamoto, Masayoshi Minai, Tsutomu Matsumoto, Hideki Ushio, Takayuk Higashii
  • Patent number: 6063927
    Abstract: Piperidine compounds, processes for preparing them, pharmaceutical compositions comprising them and their use in therapy are disclosed.
    Type: Grant
    Filed: April 23, 1999
    Date of Patent: May 16, 2000
    Assignee: SmithKline Beecham plc
    Inventors: Andrew Simon Craig, Alan David Jones, Deirdre O'Keeffe, Neal Ward
  • Patent number: 6063938
    Abstract: Disclosed is a process for producing .epsilon.-caprolactone which comprises distilling a reaction mixture obtained by oxidation of cyclohexanone to separate impurities, wherein .epsilon.-caprolactone separated in a rectifying column is contacted with an oxygen-containing gas and then distilled. Thereby, a high quality of .epsilon.-caprolactone of in which no coloration occurs during long time preservation can be produced by industrial advantages.
    Type: Grant
    Filed: July 25, 1997
    Date of Patent: May 16, 2000
    Assignee: Mitsubishi Gas Chemical Company, Inc.
    Inventors: Kazuo Tanaka, Kengi Nakaya, Atsushi Ohkoshi, Hideaki Fujita