Six-membered Hetero Ring Consists Of Sulfur, Nitrogen, And Carbon Patents (Class 544/3)
  • Patent number: 6881840
    Abstract: This relates to a dye represented by Formulae II and IIA below: wherein; R1 represents a hydrogen, an aryl group containing 6 to 14 carbon atoms, or an alkyl group containing 1 to 12 carbon atoms, R2 and R3 together form an aromatic, carbocyclic or heterocyclic ring system containing 6 to 14 atoms; X represents a sulfoxide (S?O), sulfone (SO2), or dicyanovinyl (C(CN)2) group; Y represents a sulfoxide (S?O), sulfone (SO2), carbonyl (C?O) or dicyanovinyl (C(CN)2) group; L1, L2, and L3 represent methine groups, wherein the methine groups may combine to form a 5- or 6-membered ring when m is equal to or >1; m is 0, 1, 2, or 3; W is an aryl group; and D is a moiety in conjugation with the X and Y groups.
    Type: Grant
    Filed: February 8, 2002
    Date of Patent: April 19, 2005
    Assignee: Eastman Kodak Company
    Inventors: Margaret J. Helber, Douglas M. Willis, John DiCillo
  • Patent number: 6869945
    Abstract: This application is directed to compounds useful as inhibitors of PDE4 in the treatment of diseases regulated by the activation and degranulation of eosinophils, especially asthma, chronic bronchitis, and chronic obstructuive pulmonary disease, of the formula: where Y is ?C(R1a)— or —[N?(O)k]— where k is 0 or 1; G1 is a saturated or unsaturated carbon ring system that is a 3- to 7-membered monocyclic, or that is a 7- to 12-membered, fused polycyclic; provided that G1 is not a discontinuous or restricted biaryl moiety as defined under G2; where optionally one carbon atom may be replaced by a heteroatom selected from N, O, and S; where optionally a second carbon atom thereof, and further optionally a third carbon atom thereof may be replaced by N; -G2 is a saturated or unsaturated carbon ring system that is a 3- to 7-membered monocyclic; or that is a 7- to 12-membered, fused polycyclic; or that is a 7- to 18-membered discontinuous or restricted biaryl moiety; wherein for each of the carbon ring systems re
    Type: Grant
    Filed: November 20, 2002
    Date of Patent: March 22, 2005
    Assignee: Pfizer Inc
    Inventors: Anthony Marfat, Michael William McKechney
  • Patent number: 6849623
    Abstract: Complex compounds or adducts of xanthine derivatives, for example propentofylline or pentoxyfylline, or phenazone derivatives, for example phenazone, propylphenazone and aminophenazone, and acesulfame-H, in which the components are present in a molar ratio of 1:1 or 1:2, have a pleasantly sweet taste and are suitable for numerous applications, for example in pharmaceuticals. The compounds can be prepared from the dissolved components by simple reaction.
    Type: Grant
    Filed: June 7, 2002
    Date of Patent: February 1, 2005
    Assignee: Nutrinova Nutrition Specialties & Food Ingredients GmbH
    Inventor: Andreas Burgard
  • Publication number: 20040254175
    Abstract: Novel compounds of formula (I), wherein D, W, X, Y, T and R1 have the meanings cited in claim 1, are inhibitors of coagulation factor Xa and can be used for the prophylaxis and/or therapy of thromboembolic diseases and in the treatment of tumors.
    Type: Application
    Filed: May 10, 2004
    Publication date: December 16, 2004
    Inventors: Dieter Dorsch, Bertram Cezanne, Christos Tsaklakidis, Werner Mederski, Johannes Gleitz, Christopher Barnes
  • Patent number: 6828276
    Abstract: There are described benzoylcyclohexanediones of the formula I, their preparation, and their use as herbicides and plant growth regulators. In this formula (I), C1, C2, C3 are cyclic radicals, X1 is a hetero atom, X2 is a chain of carbon atoms, L is a chain-like element, R1, R2, R3, R4, R5 are various radicals, and Y and Z are monoatomic bridge elements.
    Type: Grant
    Filed: August 30, 2001
    Date of Patent: December 7, 2004
    Assignee: Aventis CropScience GmbH
    Inventors: Thomas Seitz, Andreas van Almsick, Lothar Willms, Hermann Bieringer, Thomas Auler, Hubert Menne
  • Patent number: 6787522
    Abstract: Compounds of formula (I) are antibacterials: wherein: R1 represents hydrogen, or C1-C6 alkyl or C1-C6 alkyl substituted by one or more halogen atoms; R2 represents a group R10—(X)n—(ALK)m— wherein R10 represents hydrogen, or a C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, cycloalkyl, aryl, or heterocyclyl group, any of which may be unsubstituted or substituted by (C1-C6)alkyl, (C1-C6)alkoxy, hydroxy, mercapto, (C1-C6)alkylthio, amino, halo (including fluoro, chloro, bromo and iodo), trifluoromethyl, cyano, nitro, —COOH, —CONH2, —COORA, —NHCORA, —CONHRA, —NHRA, —NRARB, or —CONRARB wherein RA and RB are independently a (C1-C6)alkyl group, and ALK represents a straight or branched divalent C1-C6 alkylene, C2-C6 alkenylene, or C2-C6 alkynylene radical, and may be interrupted by one or more non-adjacent —NH—, —O— or —S— linkages, X represents —NH—, —O— or —S—, an
    Type: Grant
    Filed: April 30, 2002
    Date of Patent: September 7, 2004
    Assignee: British Biotech Pharmaceuticals
    Inventors: Michael George Hunter, Raymond Paul Beckett, John Martin Clements, Mark Whittaker, Stephen John Davies, Lisa Marie Pratt, Zoe Marie Spavold, Steven Launchbury
  • Patent number: 6759544
    Abstract: Complex compounds containing acesulfame have good antimicrobial action, in particular antibacterial action, and are distinguished by the fact that they are complex compounds of metallic elements such as zinc, copper, silver, or nonmetallic quaternary ammonium cations, such as the cetylpyridinium cation, with acesulfame. The invention also relates to a process for preparing the compounds and their use in the oral hygiene sector.
    Type: Grant
    Filed: June 7, 2002
    Date of Patent: July 6, 2004
    Assignee: Nutrinova Nutrition Specialties & Food Ingredients GmbH
    Inventor: Andreas Burgard
  • Patent number: 6753425
    Abstract: A processing composition for silver halide photographic light-sensitive materials, comprises a bis[2,6-diaminotriazin-4-yl]arylenediamine derivative having at least one of a sulfonic acid group, a carboxylic group and a hydroxyl group within the molecule. This processing composition can be applied to a color developer, a bleaching agent, a fixing agent, a bleach-fixing agent and a stabilizing agent and also to a processing agent in a concentration on use, a concentrated processing agent and a solid processing agent.
    Type: Grant
    Filed: April 16, 2003
    Date of Patent: June 22, 2004
    Assignee: Fuji Photo Film Co., Ltd.
    Inventors: Yasufumi Nakai, Keizo Kimura, Masashi Ogiyama
  • Publication number: 20040094749
    Abstract: The invention relates to a method for producing a phenothiazine granulate with a narrow particle size distribution. At least 98% pure phenothiazine in liquid form is pressed through a device provided with boreholes and a frequency is applied to said liquid phenothiazine. The liquid phenothiazine discharged through the boreholes enters a cooling medium having a temperature of between −196 and +120° C. The drops of liquid phenothiazine thus produced are brought to a temperature below melting point and are optionally solidified in another post-cooling area. Optionally, fine-grain particles or coarse-grained particles thus formed can be subsequently removed by appropriate methods. The bulk density of the obtained phenothiazine granulates ranges more particularly from 720-780 kg/m3.
    Type: Application
    Filed: August 11, 2003
    Publication date: May 20, 2004
    Inventors: J?uuml;rgen Beyer, Dietmar Breier, Gunther Effenberger, Michael Roos, Jens Ruppert, Olaf Just, Detlef Wehle
  • Publication number: 20040092512
    Abstract: The invention provides compound of the Formula: 1
    Type: Application
    Filed: November 6, 2003
    Publication date: May 13, 2004
    Applicant: Roche Palo Alto LLC
    Inventors: Hans Maag, Meng Sui, Shu-Hai Zhao
  • Patent number: 6627629
    Abstract: The present application describes modulators of CCR3 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases.
    Type: Grant
    Filed: June 29, 2001
    Date of Patent: September 30, 2003
    Assignee: Bristol-Myers Squibb Pharma
    Inventors: Soo S. Ko, James R. Pruitt, Dean A. Wacker, Douglas G. Batt
  • Publication number: 20030176668
    Abstract: A C-nitroso compound having a molecular weight ranging from about 225 to about 1,000 (from about 225 to about 600 for oral administration) on a monomeric basis wherein a nitroso group is attached to a tertiary carbon, which is obtained by nitrosylation of a carbon acid having a pKa less than about 25, is useful as an NO donor. When the compound is obtained from a carbon acid with a pKa less than about 10, it provides vascular relaxing effect when used at micromolar concentrations and this activity is potentiated by glutathione to be obtained at nanomolar concentrations. When the compound is obtained from a carbon acid with a pKa ranging from about 15 to about 20, vascular relaxing effect is obtained at nanomolar concentrations without glutathione. The compound is preferably water-soluble and preferably contains a carbon alpha to the nitrosylated carbon which is part of a ketone group.
    Type: Application
    Filed: January 17, 2003
    Publication date: September 18, 2003
    Inventors: Jonathan S. Stamler, Eric J. Toone
  • Patent number: 6608070
    Abstract: This invention provides a compound of the following formula: or the pharmaceutically acceptable salts thereof wherein Z is OH, C1-6 alkoxy, —NR2R3 or heterocycle; Q is selected from the following: (a) an optionally substituted phenyl, (b) an optionally substituted 6-membered monocyclic aromatic group containing one, two, three or four nitrogen atom(s), (c) an optionally substituted 5-membered monocyclic aromatic group containing one heteroatom selected from O, S and N and optionally containing one, two or three nitrogen atom(s) in addition to said heteroatom, (d) an optionally substituted C3-7 cycloalkyl and (e) an optionally substituted benzo-fuzed heterocycle; R1 is hydrogen, C1-4 alkyl or halo; R2 and R3 are independently hydrogen, OH, C1-4 alkoxy, C1-4 alkyl or C1-4 alkyl substituted with halo, OH, C1-4 alkoxy or CN; X is independently selected from H, halo, C1-4 alkyl, halo-substituted C1-4 alkyl, OH, C1-4 alkoxy, halo-substituted C1-4 alkoxy, C1-4 alkylthio, NO2, NH2, di-(C1-4 al
    Type: Grant
    Filed: July 28, 1999
    Date of Patent: August 19, 2003
    Inventors: Kazunari Nakao, Rodney William Stevens, Kiyoshi Kawamura, Chikara Uchida, Hiroki Koike, Stephane Caron
  • Patent number: 6596716
    Abstract: The present invention relates to the potentiation of glutamate receptor function using certain 2-propane-sulphonamide derivatives. It also relates to novel 2-propane-sulphonamide derivatives, to processes for their preparation and to pharmaceutical compositions containing them.
    Type: Grant
    Filed: July 25, 2001
    Date of Patent: July 22, 2003
    Assignee: Eli Lilly and Company
    Inventors: Tracey E McKennon, Paul L Ornstein, Edward C. R. Smith, Hamideh Zarrinmayeh, Dennis M Zimmerman
  • Patent number: 6559155
    Abstract: Pyrimidones of formula (I) are inhibitors of the enzyme LpPLA2 and thereof use in treating inter alia atherosclerosis, in which: R1 is COOH or a salt thereof, COOR10, CONR11R12, CN or CH2OH; R2 is a mono- or bicyclic aromatic ring system or a mono- or bicyclic heteroaromatic ring system; R3 is C1-20alkyl, C3-6cycloalkyl, C3-6cycloalkylC1-5alkyl, C1-10alkoxyC1-10alkyl, or an aromatic or heteroaromatic ring system; W is SO2 or a bond; X is O or S; and Y is a group of the formula A1—A2—A3 in which A1 and A3 each represent a bond or a straight chain or branched alkylene group, said alkylene group(s) containing a total of 1 to 10 carbon atoms and A2 represents a bond or O, S, SO, SO2, CO, C═CH2, CONH, NHCO, CR15R16, CH═CH or C═C, providing that when A2 is O, S, SO, SO2 or CONH, A3 contains at least two carbon atoms linking the A2 group and the CH2 group in formula (I).
    Type: Grant
    Filed: February 21, 2001
    Date of Patent: May 6, 2003
    Assignee: SmithKline Beecham p.l.c.
    Inventors: Colin Andrew Leach, Stephen Allan Smith
  • Publication number: 20030065172
    Abstract: Acesulfame-K is a widely used sweetener in food and beverage. It is prepared by using the substituted sodium phenoxide or substituted phenol as the starting substance to synthesize the following three intermediates: a substituted phenoxide sulfonylchloride(I), a substituted phenoxide sulfonylamide(II) and an acetoacetamide-N-sulfonyl-substituted phenoxide(III). Particularly, II was prepared by using the liquid or gaseous ammonia to react with I under the action of some catalysts in a reaction column. III was prepared by using II to react with diketene. Acesulfame-K was prepared by ring-closure in III with methanol solution of KOH or K2CO3.
    Type: Application
    Filed: July 25, 2002
    Publication date: April 3, 2003
    Inventors: Nianshou Tian, Haiming Liu
  • Patent number: 6531539
    Abstract: The invention is directed to organosilicon compounds of the general formula prepared by reacting triazine compounds with functional groups (e.g., chlorine) and corresponding compounds (e.g., mercapto). The organosilicon compounds can be used in rubber mixtures.
    Type: Grant
    Filed: April 5, 2001
    Date of Patent: March 11, 2003
    Assignee: Degussa AG
    Inventors: Roland Krafczyk, Rudolf Michel, Jörg Münzenberg, Hans-Detlef Luginsland
  • Patent number: 6525099
    Abstract: The present invention provides certain N-substituted sulfonamide derivatives useful for potentiating glutamate receptor function in a mammal and therefore, useful for treating a wide variety of conditions, such as psychiatric and neurological disorders.
    Type: Grant
    Filed: January 23, 2001
    Date of Patent: February 25, 2003
    Assignee: Eli Lilly and Company
    Inventors: Macklin Brian Arnold, Winton Dennis Jones, Paul Leslie Ornstein, Hamideh Zarrinmayeh, Dennis Michael Zimmerman
  • Publication number: 20030023084
    Abstract: Complex compounds containing acesulfame have good antimicrobial action, in particular antibacterial action, and are distinguished by the fact that they are complex compounds of metallic elements such as zinc, copper, silver, or nonmetallic quaternary ammonium cations, such as the cetylpyridinium cation, with acesulfame. The invention also relates to a process for preparing the compounds and their use in the oral hygiene sector.
    Type: Application
    Filed: June 7, 2002
    Publication date: January 30, 2003
    Inventor: Andreas Burgard
  • Publication number: 20030017993
    Abstract: Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.
    Type: Application
    Filed: November 16, 2001
    Publication date: January 23, 2003
    Inventors: Eugene D. Thorsett, Christopher M. Semko, Dimitrios Sarantakis, Michael A. Pleiss, Anthony Kreft, Andrei W. Konradi, Francine S. Grant, Darren B. Dressen, Susan Ashwell, Reinhardt Bernhard Baudy, Louis John Lombardo
  • 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
  • Publication number: 20030008865
    Abstract: Complex compounds or adducts of xanthine derivatives, for example propentofylline or pentoxyfylline, or phenazone derivatives, for example phenazone, propylphenazone and aminophenazone, and acesulfame-H, in which the components are present in a molar ratio of 1:1 or 1:2, have a pleasantly sweet taste and are suitable for numerous applications, for example in pharmaceuticals. The compounds can be prepared from the dissolved components by simple reaction.
    Type: Application
    Filed: June 7, 2002
    Publication date: January 9, 2003
    Inventor: Andreas Burgard
  • Patent number: 6500818
    Abstract: Compounds having the following formula wherein L, M, R2, R3, R4, R5, R6, R7, X1 and X2 are as defined in the specification, pharmaceutically-acceptable salt thereof, useful for treating depression, anxiety, asthma, rheumatoid arthritis, Alzheimer's disease, cancer, schizophrenia, oedema, allergic rhinitis, inflammation, pain, gastrointestinal-hypermotility, emesis, Huntington's disease, psychoses, hypertension, migraine, bladder hypermotility, or urticaria, compositions including such compounds and processes for making such compounds.
    Type: Grant
    Filed: March 30, 2001
    Date of Patent: December 31, 2002
    Assignee: Astrazeneca AB
    Inventors: Peter Robert Bernstein, Robert Frank Dedinas, Cyrus John Ohnmacht, Keith Russell
  • Publication number: 20020193312
    Abstract: Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.
    Type: Application
    Filed: November 15, 2001
    Publication date: December 19, 2002
    Inventors: Eugene D. Thorsett, Christopher M. Semko, Dimitrios Sarantakis, Michael A. Pleiss, Anthony Kreft, Andrei W. Konradi, Francine S. Grant, Darren B. Dressen, Susan Ashwell, Reinhardt Bernhard Baudy, Louis John Lombardo
  • Patent number: 6495686
    Abstract: Disclosed are compounds of the formula: wherein Ar, R1, R2, R3, W, X, Y, and Z are substituents as defined herein, which compounds are highly selective partial agonists or antagonists at human CRF1 receptors and are useful in the diagnosis and treatment of treating stress related disorders such as post traumatic stress disorder (PTSD) as well as depression, headache and anxiety.
    Type: Grant
    Filed: February 23, 2001
    Date of Patent: December 17, 2002
    Assignee: Neurogen Corporation
    Inventor: Taeyoung Yoon
  • Patent number: 6420360
    Abstract: The present invention provides a compound of formula I These compounds are useful as antibiotic agents.
    Type: Grant
    Filed: November 1, 2001
    Date of Patent: July 16, 2002
    Assignee: Pharmacia & Upjohn Company
    Inventors: David John Anderson, Jackson B. Hester, Jr.
  • Patent number: 6416762
    Abstract: The present invention provides structure-based combinatorial libraries of compounds containing the functional group minima of picornaviruses including poliovirus and rhinovirus. The libraries can be used to screen for therapeutical antiviral compounds, e.g., anti-picornaviral capsid-binding compounds.
    Type: Grant
    Filed: December 11, 1998
    Date of Patent: July 9, 2002
    Assignee: President and Fellows of Harvard College
    Inventors: Diane M. Joseph-McCarthy, Lyle D. Isaacs, George M. Whitesides, Martin Karplus, James M. Hogle, James Li-wen Cheh
  • Patent number: 6416922
    Abstract: The present invention related to an azomethine dye precursor represented by the following general formula (1) and the image-forming material and image-forming method using the azomethine dye precursor: wherein Ar represents an aryl group or a heterocyclic group which may each have a substituent; X represents a bivalent group linking a carbon atom and a nitrogen atom; and Cp represent a coupler residue which may or may not form a ring.
    Type: Grant
    Filed: January 29, 2001
    Date of Patent: July 9, 2002
    Assignee: Fuji Photo Film Co., Ltd.
    Inventors: Hiroshi Sato, Masatoshi Yumoto, Yoshimitsu Arai, Hirotaka Matsumoto
  • Patent number: 6407098
    Abstract: The application relates to novel heterocycloalkenes, to a number of processes for their preparation and to their use as fungicide.
    Type: Grant
    Filed: October 31, 2000
    Date of Patent: June 18, 2002
    Assignee: Bayer Aktiengesellschaft
    Inventors: Bernd-Wieland Krüger, Ulrich Heinemann, Herbert Gayer, Lutz Assmann, Ralf Tiemann, Thomas Seitz, Gerd Hänssler, Klaus Stenzel, Stefan Dutzmann
  • Patent number: 6407232
    Abstract: The invention relates an ionic metal complex represented by the general formula (1): wherein M is an element of groups 3-15 of the periodic table; Aa+ represents a metal ion, onium ion or proton; X1 represents O, S or NR5R6; each of R1 and R2 independently represents H, a halogen, a C1-C10 alkyl group or C1-C10 halogenated alkyl group; R3 represents a C1-C10 alkylene group, C1-C10 halogenated alkylene group, C4-C20 aryl group or C4-C20 halogenated aryl group; R4 represents a halogen, C1-C10 alkyl group, C1-C10 halogenated alkyl group, C4-C20 aryl group, C4-C20 halogenated aryl group or X2R7; X2 represents O, S or NR5R6; each of R5 and R6 represents H or a C1-C10 alkyl group; and R7 represents a C1-C10 alkyl group, C1-C10 halogenated alkyl group, C4-C20 aryl group or C4-C20 halogenated aryl group. The ionic metal complex can be used as a supporting electrolyte for electrochemical devices, a polymerization catalyst of polyolefins and so forth, or a catalyst for organic synthesis.
    Type: Grant
    Filed: July 25, 2000
    Date of Patent: June 18, 2002
    Assignee: Central Glass Company, Limited
    Inventors: Shoichi Tsujioka, Hironari Takase, Mikihiro Takahashi
  • Patent number: 6383230
    Abstract: The invention relates to novel monobenzenic dyes including at least one cationic group Z, Z chosen from quaternized aliphatic chains, aliphatic chains including at least one quaternized saturated ring and aliphatic chains including at least one quaternized unsaturated ring, to their use as oxidation-dye precursors for the oxidation-dyeing of keratin fibers, to dye compositions containing them and to oxidation-dyeing processes using them.
    Type: Grant
    Filed: January 18, 2000
    Date of Patent: May 7, 2002
    Assignee: L'Oreal
    Inventors: Alain Genet, Alan Lagrange
  • Patent number: 6365587
    Abstract: The present application describes novel substituted aryl hydroxamic acids of formula I: or pharmaceutically acceptable salt forms thereof, wherein ring A is a 5-8 membered ring containing from 0-1 additional heteroatoms selected from N, O, and S, which are useful as metalloprotease inhibitors.
    Type: Grant
    Filed: May 13, 1999
    Date of Patent: April 2, 2002
    Inventors: Matthew E. Voss, Carl P. Decicco, Ruth R. Wexler
  • Patent number: 6348459
    Abstract: The present invention provides a compound of formula I These compounds are useful as antibiotic agents.
    Type: Grant
    Filed: October 30, 2000
    Date of Patent: February 19, 2002
    Assignee: Pharmacia and Upjohn Company
    Inventors: David John Anderson, Jackson B. Hester, Jr.
  • Patent number: 6313072
    Abstract: The novel compounds of formula I: (A, B, R1, R2, R3, X and m are defined in the specification) show selective herbicidal activity. The new compounds can be prepared according to known methods and can be used as herbicides in agriculture and related fields.
    Type: Grant
    Filed: February 18, 1999
    Date of Patent: November 6, 2001
    Assignee: American Cyanamid Company
    Inventors: Stephen Scheiblich, Thomas Maier, Axel Kleemann, Helmut Siegfried Baltruschat
  • Patent number: 6271235
    Abstract: HIV protease inhibitors, obtainable by chemical synthesis, inhibit or block the biological activity of the HIV protease enzyme, causing the replication of the HIV virus to terminate. These compounds, as well as pharmaceutical compositions that contain these compounds and optionally other anti-viral agents as active ingredients, are suitable for treating patients or hosts infected with the HIV virus, which is known to cause AIDS.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: August 7, 2001
    Assignee: Agouron Pharmaceuticals, Inc.
    Inventors: Bruce A. Dressman, James E. Fritz, Stephen W. Kaldor, Vincent J. Kalish, Siegfried Heinz Reich, Michael J. Rodriguez, Timothy A. Shepherd, John H. Tatlock, Louis Nickolaus Jungheim
  • Patent number: 6265583
    Abstract: The present invention relates to cyclic sulfone moiety-containing hydroxyethylamine protease inhibitor compounds and pharmaceutical or method of use therefor, particularly as an inhibitor of HIV protease.
    Type: Grant
    Filed: October 22, 1998
    Date of Patent: July 24, 2001
    Assignees: G. D. Searle & Co., Monsanto Company
    Inventors: Deborah E. Bertenshaw, Daniel Getman, Robert M. Heintz, John J. Talley, Kathryn L. Reed, Robert Alan Chrusciel, Michael Clare
  • Patent number: 6232309
    Abstract: Insecticidal heterocyclic compounds of the formula: wherein A represents a five-membered or six-membered heteroaryl group containing one to three hetero atoms selected from the group consisting of S, O and N, said heteroaryl group being unsubstituted or substituted by a halogen atom or C1-4 alkyl group, Z represents a three-membered straight chain, each member being selected from the group consisting of CH2—, O, S and N—R2 with at least one of said three members being O, S or N—R2; E represents CH2, O, S or N—R2, wherein R2 represents a hydrogen atom, a C1-4 alkyl group, a C1-4 alkoxy group or the group wherein R3 represents a hydrogen atom or halogen atom, X represents CH or N, Y represents a nitro group or cyano group, and R1 represents a hydrogen atom or methyl group.
    Type: Grant
    Filed: May 22, 2000
    Date of Patent: May 15, 2001
    Assignee: Nihon Bayer Agrochem K.K.
    Inventors: Kozo Shiokawa, Shinichi Tsuboi, Koichi Moriya, Katsuhiko Shibuya
  • Patent number: 6217856
    Abstract: A description is given of symmetrical triazine derivatives of formula (1), wherein R1 and R2 are each independently of the other hydrogen; C1-C12alkyl, C1-C12alkoxy; and R3 is C1-C12alkyl; or C1-C12alkoxy. The easily accessible triazine derivatives are suitable for protecting ultraviolet-sensitive materials, in particular skin and hair of humans and animals, from the harmful effects of UV radiation.
    Type: Grant
    Filed: May 17, 1999
    Date of Patent: April 17, 2001
    Assignee: Ciba Specialty Chemicals Corporation
    Inventors: Thomas Ehlis, Dietmar Hüglin, Helmut Luther
  • Patent number: 6217848
    Abstract: Dye-peptide conjugates useful for diagnostic imaging and therapy are disclosed. The dye-peptide conjugates include several cyanine dyes with a variety of bis- and tetrakis(carboxylic acid) homologues. The small size of the compounds allows more favorable delivery to tumor cells as compared to larger molecular weight imaging agents. The various dyes are useful over the range of 350-1300 nm, the exact range being dependent upon the particular dye. Use of dimethylsulfoxide helps to maintain the fluorescence of the compounds. The molecules of the invention are useful for diagnostic imaging and therapy, in endoscopic applications for the detection of tumors and other abnormalities and for localized therapy, for photoacoustic tumor imaging, detection and therapy, and for sonofluorescence tumor imaging, detection and therapy.
    Type: Grant
    Filed: June 4, 1999
    Date of Patent: April 17, 2001
    Assignee: Mallinckrodt Inc.
    Inventors: Samuel Achilefu, Richard Bradley Dorshow, Joseph Edward Bugaj, Raghavan Rajagopalan
  • Patent number: 6180086
    Abstract: The sensitivity and specificity of the optical modality can be enhanced by the use of highly absorbing dyes as contrast agents. Novel cyanine dyes that absorb and emit light in the near infrared region of electromagnetic spectrum are disclosed. These dyes are useful for imaging, diagnosis and therapy of various diseased states. Particularly, the molecules of the invention are useful for optical diagnostic imaging and therapy, in endoscopic applications for the detection of tumors and other abnormalities, for localized therapy, for photoacoustic tumor imaging, detection and therapy, and for sonofluorescence tumor imaging, detection and therapy.
    Type: Grant
    Filed: January 18, 2000
    Date of Patent: January 30, 2001
    Assignee: Mallinckrodt Inc.
    Inventors: Samuel Achilefu, Raghavan Rajagopalan, Richard B. Dorshow, Joseph E. Bugaj
  • Patent number: 6162915
    Abstract: Chlorosulfonyl substituted aromatic heterocyclic compounds, such as 2-chlorosulfonyl[1,2,4]triazolo[1,5-c]pyrimidine compounds, were prepared in good yield by chloroxidation of di(aromatic heterocyclyl) disulfide compounds in a medium containing water, a water-immiscible organic solvent, and a phase transfer catalyst, such at tetrabutylammonium chloride.
    Type: Grant
    Filed: June 25, 1998
    Date of Patent: December 19, 2000
    Assignee: Dow AgroSciences LLC
    Inventors: Douglas L. Pearson, Jimmy J. Tai, Timothy J. Adaway
  • Patent number: 6057120
    Abstract: The invention concerns the use of redox-active compounds for the production of detection reagents for a method for the determination of an analyte as well as reagent kits that contain these redox-active compounds. In addition new redox-active compounds are disclosed.
    Type: Grant
    Filed: September 22, 1997
    Date of Patent: May 2, 2000
    Assignee: Roche Diagnostics GmbH
    Inventors: Dieter Heindl, Rupert Herrmann, Joachim Hones, Hans-Peter Josel, Martina Junius-Comer, Hartmut Merdes, Axel Schmidt, Ernst Selbertinger
  • Patent number: 6004950
    Abstract: The invention encompasses the novel compound of Formula I as well as a method of treating cyclooxygenase-2 mediated diseases comprising administration to a patient in need of such treatment of a non-toxic therapeutically effective amount of a compound of Formula I. ##STR1## The invention also encompasses certain pharmaceutical compositions for treatment of cyclooxygenase-2 mediated diseases comprising compounds of Formula I.
    Type: Grant
    Filed: September 11, 1998
    Date of Patent: December 21, 1999
    Assignee: Merck Frosst Canada, Inc.
    Inventors: Richard Friesen, Daniel Dube, Denis Deschenes
  • Patent number: 5955461
    Type: Grant
    Filed: December 12, 1997
    Date of Patent: September 21, 1999
    Assignee: Schering Aktiengesellschaft
    Inventors: Andreas Huth, Lechoslaw Turski
  • Patent number: 5908852
    Abstract: A class of 1,3,5-substituted pyrazoles is described for the treatment of inflammation, including treatment of pain and disorders such as arthritis. Compounds of particular interest are of Formula I ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as described herein; or a pharmaceutically-acceptable salt thereof.
    Type: Grant
    Filed: May 30, 1996
    Date of Patent: June 1, 1999
    Assignee: G. D. Searle & Co.
    Inventors: John J Talley, Donald J Rogier, Jr., Thomas D. Penning, Stella S Yu
  • Patent number: 5861138
    Abstract: Novel ligands for use in MRI contrast agents and which have the formula ##STR1## wherein R.sub.1 -R.sub.14, M", l, m, and n are defined herein.
    Type: Grant
    Filed: November 20, 1996
    Date of Patent: January 19, 1999
    Assignee: Hoechst Celanese Corp.
    Inventors: Wei-Jun Peng, Daniel A. Aguilar
  • Patent number: 5824677
    Abstract: Disclosed are compounds having a straight or branched aliphatic hydrocarbon structure of formula I: ##STR1## In formula I, n is an integer from one to four and m is an integer from four to twenty. Independently, R.sub.1 and R.sub.2 are hydrogen, a straight or branched chain alkyl, alkenyl or alkynyl of up to twenty carbon atoms in length or --(CH.sub.2).sub.w R.sub.5. If R.sub.1 or R.sub.2 is --(CH.sub.2).sub.w R.sub.5, w may be an integer from one to twenty and R.sub.5 may be an hydroxyl, halo, C.sub.1-8 alkoxyl group or a substituted or unsubstituted carbocycle or heterocycle. Alternatively, R.sub.1 and R.sub.2 may jointly form a substituted or unsubstituted, saturated or unsaturated heterocycle having from four to eight carbon atoms, N being a hetero atom of the resulting heterocyle. R.sub.3 may be either hydrogen or C.sub.13. In the compounds, a total sum of carbon atoms comprising R.sub.1 or R.sub.2, (CH.sub.2).sub.n and (CH.sub.2).sub.m does not exceed forty. R.sub.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: October 20, 1998
    Assignee: Cell Therapeutics, Inc.
    Inventors: J. Peter Klein, Gail E. Underiner, Anil M. Kumar
  • Patent number: 5744607
    Abstract: The invention is directed to glutamic acid and aspartic acid derivatives represented by formula (I): ##STR1## wherein R.sub.1 is selected from the group consisting of unsubstituted, mono- or di-substituted phenyl groups, unsubstituted, mono- or di-substituted phenylamino groups, a 2(beta)naphthyl group, and heterocyclic, monocyclic and dicyclic groups; R.sub.2 is selected from heterocyclic spiro groups, aminoalkyladamantyl groups, alkylamino groups, C.sub.4 -C.sub.10 cycloalkylamino groups and dicyclic amino groups (condensed); R.sub.3 is H, CH.sub.3 or C.sub.2 H.sub.5 ; A is a bond or a linear or branched alkylene group having from 1 to 4 carbon atoms; W is a tertiary amino group or a heterocyclic group; and r is 1 or 2. The compounds have a potent antagonistic effect on gastrin and cholecystokinin and can be used to treat diseases which are linked to imbalances in the physiological levels of gastrin, cholecystokinin or other biologically active polypeptides related thereto.
    Type: Grant
    Filed: October 18, 1996
    Date of Patent: April 28, 1998
    Assignee: Rotta Research Laboratorium S.p.A.
    Inventors: Francesco Makovec, Lucio C. Rovati, Luigi A. Rovati
  • Patent number: 5686486
    Abstract: The present invention relates to compounds of formula I which are 4-hydroxy-benzopyran-2-ones and 4-hydroxy-cycloalkyl?b!pyran-2-ones useful for inhibiting a retrovirus in a mammalian cell infected with said retrovirus. ##STR1## Wherein R.sub.10 and R.sub.
    Type: Grant
    Filed: August 4, 1995
    Date of Patent: November 11, 1997
    Assignee: Pharmacia & Upjohn Company
    Inventors: Paul Kosta Tomich, Michael John Bohanon, Steven Ronald Turner, Joseph Walter Strohbach, Suvit Thaisrivongs, Richard C. Thomas, Karen Rene Romines, Chih-Ping Yang, Paul Adrian Aristoff, Harvey Irving Skulnick, Paul D. Johnson, Ronald B. Gammill, Qingwei Zhang, Gordon L. Bundy, David John Anderson, Lee S. Banitt
  • Patent number: 5641783
    Abstract: Disclosed are compounds having a straight or branched aliphatic hydrocarbon structure of formula I: ##STR1## In formula I, n is an integer from one to four and m is an integer from four to twenty. Independently, R.sub.1 and R.sub.2 are hydrogen, a straight or branched chain alkyl, alkenyl or alkynyl of up to twenty carbon atoms in length or --(CH.sub.2).sub.w R.sub.5. If R.sub.1 or R.sub.2 is --(CH.sub.2).sub.w R.sub.5, w may be an integer from one to twenty and R.sub.5 may be an hydroxyl, halo, C.sub.1-8 alkoxyl group or a substituted or unsubstituted carbocycle or heterocycle. Alternatively, R.sub.1 and R.sub.2 may jointly form a substituted or unsubstituted, saturated or unsaturated heterocycle having from four to eight carbon atoms, N being a hetero atom of the resulting heterocycle. R.sub.3 may be either hydrogen or C.sub.1-3. In the compounds, a total sum of carbon atoms comprising R.sub.1 or R.sub.2, (CH.sub.2).sub.n and (CH.sub.2).sub.m does not exceed forty. R.sub.
    Type: Grant
    Filed: September 8, 1994
    Date of Patent: June 24, 1997
    Assignee: Cell Therapeutics, Inc.
    Inventors: J. Peter Klein, Gail E. Underiner, Anil M. Kumar