Patents Examined by Robert Gerstl
  • Bis-thiadiazole derivatives or salts thereof and agrohorticultural disease controller and method for using the same
    Patent number: 6313154
    Abstract: A bis-thiadiazole derivative represented by general formula (I): wherein R1 and R2 represent H, C1-C8 alkyl, halo C1-C4 alkyl, unsubstituted or substituted phenyl, 5- or 6-membered heterocycle containing 1 to 3 hetero atoms selected from O, S and N, or the like; X1 and X2 represent O or S; Y1 and Y2 represent O, S or —N(R3)—; R represents C0-C30 alkylene. —(C)a(R3)(R4)— (R3 and R4 represent H, halogen, OH, C1-C4 alkyl, halo C1-C4 alkyl or the like) or the like; and a is 0 to 30; or a salt thereof, and an agrohorticultural disease controller containing said derivative or salt as an active ingredient.
    Type: Grant
    Filed: March 26, 1999
    Date of Patent: November 6, 2001
    Assignee: Nihon Nohyaku Co., Ltd.
    Inventors: Kenji Tsubata, Takashi Shimaoka, Kazuhiro Takagi, Koji Baba, Sohkichi Tajima
  • Process for the preparation of prostaglandins
    Patent number: 6313341
    Abstract: A hydroxy-1-alkyne is reacted with a tin hydride compound, and the obtained (E,Z)-hydroxyvinylstannanes are separated to give the (E)-substance which is further converted to a vinylcopper complex shown by followed by the conjugate addition reaction with an &agr;, &bgr;-unsaturated cyclopentenone, and the deprotecting reaction is subsequently carried out to prepare a prostaglandin or an intermediate of prostaglandins easily, efficiently and industrially favorably.
    Type: Grant
    Filed: May 14, 1999
    Date of Patent: November 6, 2001
    Assignee: Fuji Yakuhin Kogyo Kabushiki Kaisha
    Inventors: Noriaki Murata, Atsunori Aramata, Tadashi Takeuchi
  • Succinoylamino hydroxyethylamino sulfonamides useful as retroviral protease inhibitors
    Patent number: 6313345
    Abstract: Succinoylamino hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
    Type: Grant
    Filed: October 18, 1999
    Date of Patent: November 6, 2001
    Assignee: G. D. Searle & Co.
    Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel Getman, Gary A. DeCrescenzo, John N. Freskos
  • Certain 5-alkyl-2-arylaminophenylacetic acids and derivatives
    Patent number: 6310099
    Abstract: Disclosed are the compounds of formula I wherein R is methyl or ethyl; R1 is chloro or fluoro; R2 is hydrogen or fluoro; R3 is hydrogen, fluoro, chloro, methyl, ethyl, methoxy, ethoxy or hydroxy; R4 is hydrogen or fluoro; and R5 is chloro, fluoro, trifluoromethyl or methyl; and pharmaceutically acceptable salts thereof, as selective COX-2 cyclooxygenase inhibitors; and pharmaceutically acceptable prodrug esters thereof.
    Type: Grant
    Filed: November 27, 2000
    Date of Patent: October 30, 2001
    Assignee: Novartis Ag
    Inventors: Roger A. Fujimoto, Leslie W. McQuire, Benjamin B. Mugrage, John H. van Duzer, Daqiang Xu
  • Hydroxamic and carboxylic acid derivatives having MMP and TNF inhibitory activity
    Patent number: 6310088
    Abstract: Compounds of formula (I) are useful therapeutic agents, by virtue of having MMP and TNF inhibitory activity.
    Type: Grant
    Filed: May 4, 2000
    Date of Patent: October 30, 2001
    Assignee: Darwin Discovery, Ltd.
    Inventors: Andrew Douglas Baxter, David Alan Owen, John Gary Montana, Elizabeth Jane Reed Nicholson
  • Isothiazole carboxylic acid amides
    Patent number: 6310005
    Abstract: Novel isothiazolecarboxamides of the formula in which R is as defined in the description, a plurality of processes for preparing the novel compounds and their use for protecting plants against attack by undesirable microorganisms.
    Type: Grant
    Filed: March 13, 2001
    Date of Patent: October 30, 2001
    Assignee: Bayer Aktiengesellschaft
    Inventors: Lutz Assmann, Hans-Ludwig Elbe, Dietmar Kuhnt, Gerd Hänssler, Karl-Heinz Kuck, Yoshinori Kitagawa, Haruko Sawada, Haruhiko Sakuma
  • 3-Cyano-3-(3,4-disubstituted) phenylcyclohexyl-1-carboxylates
    Patent number: 6300372
    Abstract: Novel 3-cyano-3-(3,4-disubstituted)phenylcyclohexyl-1-carboxylates or derivatives thereof and their corresponding cyclohexenyl analogs are described herein. These compounds inhibit the production of Tumor Necrosis Factor and are useful in the treatment of disease states mediated or exacerbated by TNF production. These compounds are also useful mediating or inhibiting the enzymatic or catalytic activity of phosphodiesterase IV and are therefore useful in treating diseases in need of mediation or inhibition thereof.
    Type: Grant
    Filed: January 30, 1996
    Date of Patent: October 9, 2001
    Assignee: SmithKline Beecham Corporation
    Inventors: Siegfried B. Christensen, IV, Cornelia Jutta Forster
  • Azoles for treatment of fungal infections
    Patent number: 6300353
    Abstract: Azole derivatives of the formula I wherein R14, R15 are each independently hydrogen or fluorine, T is a group of the formula: wherein R9 is pyrrolidinyl or a group A—NH—B—, A is hydrogen or straight-chain or branched C1-C5 alkyl; B is straight-chain or branched C1-C4 alkylene, —CH2—CONH—CH2 or —CH2CH2CH2—CH(NH2); and X− is a pharmaceutically acceptable anion; and pharmaceutically acceptable salts of said compounds, and hydrates and solvates of the compounds of formula I and the salts thereof can be used in the production of medicaments for treating fungal infections and mycoses.
    Type: Grant
    Filed: March 5, 1999
    Date of Patent: October 9, 2001
    Assignee: Basilea Pharmaceutica AG, a Swiss Company
    Inventors: Tadakatsu Hayase, Shigeyasu Ichihara, Yoshiaki Isshiki, Pingli Liu, Jun Ohwada, Toshiya Sakai, Nobuo Shimma, Masao Tsukazaki, Isao Umeda, Toshikazu Yamazaki
  • Thiazole derivatives
    Patent number: 6297266
    Abstract: Compounds of formula (I) as well as pharmaceutically usable salts and esters thereof, wherein R1, R2 and R3 have the significance described in the specification, inhibit the binding of adhesive proteins to the surface of different types of cell and accordingly influence cell-cell and cell-matrix interactions. They can be used in the form of pharmaceutical preparations in the control or prevention of neoplasms, tumor metastasizing, tumor growth, osteoporosis, Paget's disease, diabetic retinopathy, macular degeneration, restenosis following vascular intervention, psoriasis, arthritis, fibrosis, kidney failure as well as infections caused by viruses, bacteria or fungi.
    Type: Grant
    Filed: October 19, 1999
    Date of Patent: October 2, 2001
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Leo Alig, Kurt Hilpert, Thomas Weller
  • Artemisinin analogs having antimalarial antiproliferative and antitumor activities and chemoselective methods of making the same
    Patent number: 6297272
    Abstract: Methods for producing novel artemisinin analogs and artemisinin dimers having antimalarial, antiproliferative and antitumor activities are described herein. These novel artemisinin analogs and artemisinin dimers have the following structure or diastereomers thereof, having antimalarial, and antiproliferative and antitumor activities wherein, the monomers of the present invention are formed when n is 1 and R is alkyl, cycloalkyl, heteroalkyl, heterocycloalkyl, alkenyl, alkynyl, aryl or heteroaryl. The dimers of the present invention are formed when n is 2 and R is a linker including, but not limited to, alkyl, cycloalkyl, heteroalkyl, heterocycloalkyl, alkenyl, alkynyl, aryl or heteroaryl.
    Type: Grant
    Filed: January 12, 1999
    Date of Patent: October 2, 2001
    Assignees: Hauser, Inc., Johns Hopkins University
    Inventors: Gary H. Posner, Hardwin O'Dowd, Suji Xie, Theresa A. Shapiro, Christopher Murray
  • Process for the preparation of 1,2,4-thiadiazoles
    Patent number: 6297384
    Abstract: 3-[N′-(benzoyl)thioureido]-5-substituted-1,2,4-thiadiazoles are debenzoylated in an aqueous KOH solution. This process provides the 5-substituted-3-thioureido-1,2,4-thiadiazoles in unexpectedly high yield and purity as compared to similar processes employing NaOH.
    Type: Grant
    Filed: December 21, 1999
    Date of Patent: October 2, 2001
    Assignee: The Procter & Gamble Company
    Inventor: Joseph K. Agyin
  • Reverse hydroxamate inhibitors of matrix metalloproteinases
    Patent number: 6294573
    Abstract: Compounds having the formula are matrix metalloproteinase inhibitors. Also disclosed are matrix metalloproteinase-inhibiting compositions and methods of inhibiting matrix metalloproteinase in a mammal.
    Type: Grant
    Filed: January 27, 2000
    Date of Patent: September 25, 2001
    Assignee: Abbott Laboratories
    Inventors: Michael L. Curtin, Yujia Dai, Steven K. Davidsen, Joseph F. Dellaria, Jr., Alan S. Florjancic, Jianchun Gong, Yan Guo, Howard R. Heyman, James H. Holms, Michael R. Michaelides, Jamie R. Stacey, Douglas H. Steinman, Carol K. Wada, Lianhong Xu
  • 3-aryl alkenyl-1,2,4-oxadiazole derivatives and their use as parasiticides for animals
    Patent number: 6291492
    Abstract: The invention relates to new 3-aryl-alkenyl-1,2,4 -oxadiazole derivatives of the formula (I) in which R1, R2, R3, R4, R5, R6, Y, m and n have the meanings given in the description, to a plurality of processes for their preparation, and to their use as pesticides.
    Type: Grant
    Filed: July 11, 1996
    Date of Patent: September 18, 2001
    Assignee: Bayer Aktiengesellschaft
    Inventors: Peter Jeschke, Ulrike Wachendorff-Neumann, Christoph Erdelen, Norbert Mencke, Andreas Turberg
  • Compounds and methods of use for treatment of neurogenic inflammation
    Patent number: 6291501
    Abstract: The subject invention pertains to compounds which are useful as antiinflammatory agents and to compositions containing such compounds as active ingredients. The novel uses of the compounds relate to the anti-neurogenic inflammatory properties of the disclosed bis-heterocyclic compounds. Specifically exemplified herein are dragmacidin f, topsentin d, and topsentin e, and their salts, analogs, and derivatives.
    Type: Grant
    Filed: February 19, 1999
    Date of Patent: September 18, 2001
    Assignees: Harbor Branch Oceanographic Institution, Inc., Regents of the University of California
    Inventors: Amy E. Wright, Shirley A. Pomponi, Robert S. Jacobs
  • Certain 5-alkyl-2-arylaminophenylacetic acids and derivatives
    Patent number: 6291523
    Abstract: Disclosed are the compounds of formula I wherein R is methyl or ethyl; R1 is chloro or fluoro; R2 is hydrogen or fluoro; R3 is hydrogen, fluoro, chloro, methyl, ethyl, methoxy, ethoxy or hydroxy; R4 is hydrogen or fluoro; and R5 is chloro, fluoro, trifluoromethyl or methyl; and pharmaceutically acceptable salts thereof, as selective COX-2 cyclooxygenase inhibitors; and pharmaceutically acceptable prodrug esters thereof.
    Type: Grant
    Filed: August 25, 1998
    Date of Patent: September 18, 2001
    Assignee: Novartis AG
    Inventors: Roger A. Fujimoto, Leslie W. McQuire, Benjamin B. Mugrage, John H. van Duzer, Daqiang Xu
  • Small molecule inhibitors of rotamase enzyme activity
    Patent number: 6291510
    Abstract: This invention relates to neurotrophic compounds having an affinity for FKBP-type immunophilins, their preparation and use as inhibitors of the enzyme activity associated with immunophilin proteins, and particularly inhibitors of peptidyl-prolyl isomerase or rotamase enzyme activity.
    Type: Grant
    Filed: May 7, 1998
    Date of Patent: September 18, 2001
    Assignee: GPI NIL Holdings, Inc.
    Inventors: Gregory S. Hamilton, Joseph P. Steiner
  • Process for the preparation of chiral keto-heterocycles of basic amino acids
    Patent number: 6291678
    Abstract: A process for the preparation of novel keto heterocycle derivatives of basic natural and unnatural amino acids which affords products of high enantiomeric excess where a metalated heterocycle is reacted with N,O-dialkyl amide of an amino acid containing arylsulphonamide protected side chain amine in high chemical and optical yield as well as the novel compounds obtained by the process.
    Type: Grant
    Filed: December 11, 1998
    Date of Patent: September 18, 2001
    Assignee: Warner-Lambert Company
    Inventors: Kent A. Berryman, Annette M. Doherty, Jeremy J. Edmunds, Janet S. Plummer
  • Herbicidal compounds
    Patent number: 6291400
    Abstract: A compound of formula (I): or a salt, enamine or the like, acylate, sulphonate, carbamate or ether derivative thereof; wherein X, X1 and X2 are independently oxygen or sulphur, R1 is an optionally substituted heterocyclic or cycloalkyl group, and Y is an optionally substituted C2-C4 alkylene group which is optionally interposed by an oxygen atom, a group a group or an optionally mono-substituted nitrogen atom, wherein p is 0, 1 or 2, s is 0 or 1 and Rb is alkyl or alkoxy; provided that when X, X1 and X2 are oxygen, R1 is not pyridyl or pyrimidinyl. Processes for the preparation of these compounds and herbicidal compositions containing them are also described and claimed.
    Type: Grant
    Filed: May 27, 1999
    Date of Patent: September 18, 2001
    Assignee: Zeneca Limited
    Inventors: John E D Barton, David Cartwright, John M Cox, Glynn Mitchell, Charles G Carter, David L Lee, Francis H Walker, Frank X Woolard
  • Thiazolidinedione, oxazolidinedione and oxadiazolidinedione derivatives
    Patent number: 6288096
    Abstract: Novel thiazolidinedione, oxazolidinedione and oxadiazolidinedione derivatives, process for their manufacture, pharmaceutical preparations containing them and the use of the compounds in conditions associated with insulin resistance.
    Type: Grant
    Filed: June 25, 1998
    Date of Patent: September 11, 2001
    Assignee: AstraZeneca AB
    Inventors: Kjell Andersson, Maria Boije, Eva-Lotte Lindstedt, Bengt Ljung, Bo Nordén
  • Compounds
    Patent number: 6288095
    Abstract: A method is provided for the treatment and/or prophylaxis of cardiovascular diseases or eating disorders in a human or non-human mammal, which comprises administering to a human or non-human mammal in need thereof, an effective, non-toxic amount of a compound of formula (I): or a tautomeric form thereof and/or a pharmaceuticlaly acceptable salt thereof and/or a pharmaceutically acceptable solvate thereof, in which A1 represents a substituted or unsubstituted aromatic heterocyclyl group; R1 represents a hydrogen atom, an alkyl group, an acyl group, an aralkyl group, wherein the aryl moiety may be substituted or unsubstituted, or a substituted or unsubstituted aryl group; R2 and R3 each represent hydrogen, or R2 and R3 together represent a bond; A2 represents a benzene ring having in total up to five substituents; and n represents an integer in the range of from 2 to 6.
    Type: Grant
    Filed: December 19, 1994
    Date of Patent: September 11, 2001
    Assignee: Beecham Group p.l.c.
    Inventors: Richard Mark Hindley, Michael Antony Cawthorne