Double Bonded Divalent Chalcogen Containing Patents (Class 544/54)
  • Patent number: 7314932
    Abstract: Methods for minimizing the formation of thioamide compounds using decoy agents during reactions, such as thionations of carbonyl compounds containing nitrite groups, are provided.
    Type: Grant
    Filed: April 7, 2005
    Date of Patent: January 1, 2008
    Assignee: Wyeth
    Inventor: Bogdan Kazimierz Wilk
  • Patent number: 7223754
    Abstract: The invention relates to methods of using Cav2.2 subunit calcium channel modulators, particularly thiazolidinone, oxazolidinone, and imidazolone derivatives, to treat lower urinary tract and related disorders.
    Type: Grant
    Filed: November 17, 2004
    Date of Patent: May 29, 2007
    Assignee: Dynogen Pharmaceuticals, Inc.
    Inventors: Matthew Oliver Fraser, Karl Bruce Thor, Edward C. Burgard
  • Patent number: 7183275
    Abstract: The present invention relates to 2-imino-1,3-thiazine derivatives, in specific, 2-imino-1,3-thiazine derivatives having a selective antagonistic activity or agonistic activity to a cannabinoid type 2 receptor and their pharmaceutical use.
    Type: Grant
    Filed: October 26, 2004
    Date of Patent: February 27, 2007
    Assignee: Shionogi Co., Ltd.
    Inventors: Koji Hanasaki, Takami Murashi, Hiroyuki Kai
  • Patent number: 7166590
    Abstract: A compound of the formula (I): [wherein R1 is (substituted) alkyl, alkoxy, phenyl, hetero ring etc.; A is bond, CO, SO2; R2 is H, (substituted) alkyl etc.; D is alkylene etc.; E is COO, OCO, O, S, SO, SO2 etc.; R3 is (substituted) alkyl, carbocyclic ring, hetero ring; J is O, NR16 (R16 is H, substituted alkyl); R4 is (substituted) alkyl, carbocyclic ring, hetero ring.] or non-toxic salt thereof, and an N-type calcium channel blocker comprising it as an active ingredient. The compounds of the formula (I) possess an inhibitory action on N-type calcium channel, so they are useful as agent for the prevention and/or treatment of cerebral infarct, transient ischemic attack, encephalomyelopathy after cardiac operation, spinal angiopathy, hypertension with stress, neurosis or epilepsy etc. or agent for the treatment of pain.
    Type: Grant
    Filed: May 28, 2002
    Date of Patent: January 23, 2007
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Takuya Seko, Masashi Kato
  • Patent number: 7094778
    Abstract: This invention relates to compounds which are generally muscarinic M2/M3 receptor antagonists and which are represented by Formula I: wherein X, Y, and Z are O, S or NR5, and the other substituents are as defined in the specification; and prodrugs, individual isomers, racemic or non-racemic mixtures of isomers, and pharmaceutically acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds and methods for their use as therapeutic agents.
    Type: Grant
    Filed: October 14, 2003
    Date of Patent: August 22, 2006
    Assignee: Syntex (U.S.A.) LLC
    Inventors: Charles Alois Dvorak, Lawrence Emerson Fisher, Keena Lynn Green, Ralph New Harris, III, Hans Maag, Anthony Prince, David Bruce Repke, Russell Stephen Stabler
  • Patent number: 7015217
    Abstract: The present application describes novel cyclic sulfone derivatives of formula I: or pharmaceutically acceptable salt or prodrug forms thereof, which are useful as inhibitors of matrix metalloproteinases (MMP), TNF-? converting enzyme (TACE), aggrecanase, or a combination thereof. In formula I, A is selected from —COR5, —CO2H, —CO2R6, —C(O)NHOH, —C(O)NHOR5, —C(O)NHOR6, —NHRa, —N(OH)COR5, —N(OH)CHO, —SH, —CH2SH, —S(O)(?NH)Ra, —S(?NH)2Ra, —SC(O)Ra, —PO(OH)2, and —PO(OH)NHRa; B is a thiomorpholine ring; X is absent or is CR3R4; and Ua, Xa, Ya, Za, R1, R2, Rb, and q are defined in the present specification.
    Type: Grant
    Filed: October 7, 2002
    Date of Patent: March 21, 2006
    Assignee: Bristol-Myers Squibb Company
    Inventors: Jingwu Duan, Chu-Biao Xue
  • Patent number: 6936606
    Abstract: Disclosed are novel cathepsin S, K, F, L and B reversible inhibitory compounds of the formulas (Ia) and (Ib) where R1, R2, R3, R4, R5, R6, R8, R9 and X are defined herein. The compounds are useful for treating autoimmune and other diseases.
    Type: Grant
    Filed: September 27, 2002
    Date of Patent: August 30, 2005
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Younes Bekkali, Denice Mary Spero, Sanxing Sun, David S. Thomson, Yancey D. Ward, Erick R. R. Young, Eugene R. Hickey, Weimin Liu, Usha R. Patel
  • Patent number: 6818640
    Abstract: It is found out that compounds represented by general formula (I) bind selectively to cannabinoid 2 receptor (CB2R) and thus exhibit CB2R antagonism or CB2R agonis wherein R1 represents optionally substituted alkylene; R2 represents hydrogen, alkyl, a group represented by the formula —C(═R5)—R6 (wherein R5 represents O or S; and R6 represents alkyl, alkoxy, alkylthio, etc.) or a group represented by the formula SO2R7 (wherein R7 represents allyl, etc.); m is an integer of from 0 to 2; and A represents optionally substituted aryl, etc.
    Type: Grant
    Filed: February 26, 2002
    Date of Patent: November 16, 2004
    Assignee: Shionogi & Co., Ltd.
    Inventors: Koji Hanasaki, Takami Murashi, Hiroyuki Kai
  • Patent number: 6794406
    Abstract: The invention relates to new indole derivatives, processes for their preparation, and their use in medicaments.
    Type: Grant
    Filed: December 21, 2001
    Date of Patent: September 21, 2004
    Assignee: Bayer Aktiengesellschaft
    Inventors: Helmut Haning, Michael Woltering, Gunter Schmidt, Hilmar Bischoff, Axel Kretschmer, Verena Vöhringer, Christiane Faeste
  • 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: 6673804
    Abstract: A compound of the formula (I) or a pharmacologically acceptable salt, ester or other derivative thereof: R1 is H or NHOH. R2 is H, optionally substituted alkyl, cycloalkyl or a group —AR6. A is an alkylene which may be optionally interrupted by O, —S(O)m— or —N(R9). R6 is a group (II), (III), (IV) X is O, S, —N(R10)—, —C(R11)(R12)—. Y is O, CO, —S(O)n—, —N(R10)—, —C(R11)(R12)—. Each of R7 and R8 is H, alkyl, COOH, optionally substituted alkyl, etc. Each of R9, R10, R11, and R12 is H, alkyl, etc. Each of m and n is 0 to 2. R3 is H, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted alkenyl, optionally substituted alkynyl. R4 is optionally substituted (hetero)arylene. R5 is optionally substituted alkyl, optionally substituted (hetero)aryl. These compounds have matrixmetalloproteinase—13 inhibitory activity and aglycanase inhibitory activity.
    Type: Grant
    Filed: October 2, 2000
    Date of Patent: January 6, 2004
    Assignee: Sankyo Company, Limited
    Inventors: Tomio Kimura, Shoujiro Miyazaki, Keiji Ueda, Kazuhiko Tanzawa, Shigeru Ushiyama, Wataru Takasaki
  • Patent number: 6670359
    Abstract: The present invention relates to new new piperidyl- or piperazinyl-substituted dihydro-2H-1-benzopyran derivatives compound having the formula (I) wherein X is N or CH; Y is NR2CH2, CH2NR2, NR2CO, CONR2, NR2SO2 or NR2CONR2 wherein R2 is H or C1-C6 alkyl; R1 is H, C1-C6 alkyl or C3-C6 cycloalkyl; R3 is C1-C6 alkyl, C3-C6 cycloalkyl or (CH2)n-aryl, wherein aryl is phenyl or a heteroaromatic ring containing one or two heteroatoms selected from N, O and S and which may be mono- or di-substituted with R4 and/or R5; and n is 0-4; as (R)-enantiomers, (S)-enantiomers or a racemate in the form of a free base or a pharmaceutically acceptable salt or solvate thereof, a process for their preparation, pharmaceutical compositions containing said therapeutically active compounds and to the use of said active compounds.
    Type: Grant
    Filed: November 1, 2002
    Date of Patent: December 30, 2003
    Assignee: AstraZeneca AB
    Inventors: Stefan Berg, Martin Nylöf, Svante Ross, Seth-Olov Thorberg
  • Publication number: 20030232984
    Abstract: The method of this invention prepares acylated cyclic compounds by contacting phenyl esters as acylating agents with cyclic compounds in the presence of a cyanide or fluoride catalyst.
    Type: Application
    Filed: March 24, 2003
    Publication date: December 18, 2003
    Inventor: Paul Walter Wojtkowski
  • Patent number: 6656911
    Abstract: The present invention relates to certain substituted oxadiazole, thiadiazoles and triazole peptoids which are useful as inhibitors of serine proteases. Compounds of the invention are useful for treating, for example, adult respiratory distress syndrome, septic shock, and myocardial ischemia-reperfusion injury.
    Type: Grant
    Filed: April 18, 2002
    Date of Patent: December 2, 2003
    Assignee: Cortech, Inc.
    Inventors: Albert Gyorkos, Lyle W Spruce
  • Patent number: 6642180
    Abstract: The present invention relates to novel biphenyl-substituted cyclic ketoenols of the formula (I) in which W represents hydrogen, halogen, alkyl, alkoxy, alkenyloxy, halogenoalkyl, halogenoalkoxy, halogenoalkenyloxy, nitro or cyano, X represents halogen, alkyl, alkoxy, alkenyloxy, alkylthio, alkylsulphinyl, alkylsulphonyl, halogenoalkyl, halogenoalkoxy, halogenoalkenyloxy, nitro, cyano or in each case optionally substituted phenyl, phenoxy, phenylthio, phenylalkoxy or phenylalkylthio, Y represents in each case optionally substituted cycloalkyl, aryl or hetaryl, Z represents hydrogen, halogen, alkyl, alkoxy, halogenoalkyl or halogenoalkoxy, CKE represents one of the groups  in which A, B, D, L, M, Q1, Q2, Q3, Q4, Q5 and Q6 are as defined in the description, to preparation and to their use as pesticides and herbicides.
    Type: Grant
    Filed: January 25, 2002
    Date of Patent: November 4, 2003
    Assignee: Bayer Aktiengesellschaft
    Inventors: Reiner Fischer, Alan Graff, Thomas Bretschneider, Christoph Erdelen, Mark Wilhelm Drewes, Dieter Feucht
  • Publication number: 20030176418
    Abstract: The present invention relates to tetrahydroquinoline compounds as muscarinic receptor agonists; compositions comprising the same; methods of inhibiting an activity of a muscarinic receptor with said compounds; methods of treating a disease condition associated with a muscarinic receptor using said compounds; and methods for identifying a subject suitable for treatment using said compounds.
    Type: Application
    Filed: December 23, 2002
    Publication date: September 18, 2003
    Inventors: Niels Skjaerbaek, Kristian Norup Koch, Bo Lennart Mikael Friberg, Bo-Ragnar Tolf
  • Publication number: 20030171219
    Abstract: The invention relates to new phenyl-substituted cyclic ketoenols of the formula (I) 1
    Type: Application
    Filed: September 19, 2002
    Publication date: September 11, 2003
    Inventors: Folker Lieb, Hermann Hagemann, Arno Widdig, Michael Ruther, Reiner Fischer, Thomas Bretschneider, Christoph Erdelen, Ulrike Wachendorff-Neumann, Hans-Joachim Santel, Markus Dollinger, Alan Graff, Norbert Mencke, Andreas Turberg, Peter Dahmen
  • Publication number: 20030171368
    Abstract: The disclosure is directed to compounds of the formula (I) 1
    Type: Application
    Filed: February 6, 2002
    Publication date: September 11, 2003
    Inventors: Werner Seitz, Andreas Kling, Herve Geneste, Thomas Subkowski, Claudia Graef, Wilfried Hornberger
  • Patent number: 6605608
    Abstract: The present invention relates to the compounds of the formula (I) and salts thereof (all the symbols are the same meanings as described in the specification). The compounds of the formula (I) possess inhibitory activity of N-type calcium channel, so they are useful as drug for prevention and/or treatment of cerebral infarct, transient ischemic attack, encephalomyelopathy after cardiac operation, spinal angiopathy, hypertension with stress, neurosis, epilepsy, asthma and pollakiuria etc. or agent for the treatment of pain.
    Type: Grant
    Filed: December 22, 2000
    Date of Patent: August 12, 2003
    Assignee: Ono Pharmaceutical Co., Ltd
    Inventors: Takuya Seko, Masashi Kato
  • Publication number: 20030144504
    Abstract: The present invention relates to new compounds of the formula (I) 1
    Type: Application
    Filed: July 18, 2002
    Publication date: July 31, 2003
    Inventors: Reiner Fischer, Thomas Bretschneider, Hermann Hagemann, Folker Lieb, Michael Ruther, Arno Widdig, Peter Dahmen, Markus Dollinger, Christoph Erdelen, Hans-Joachim Santel, Ulrike Wachendorff-Neumann, Alan Graff, Wolfram Andersch
  • Publication number: 20030109521
    Abstract: This invention relates aryl substituted thiazolidinones of Formula I: 1
    Type: Application
    Filed: July 16, 2002
    Publication date: June 12, 2003
    Applicant: Euro-Celtique, S.A.
    Inventors: Qun Sun, Donald J. Kyle
  • 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: 20030045432
    Abstract: The present invention relates to new compounds of the formula (I) 1
    Type: Application
    Filed: December 11, 2001
    Publication date: March 6, 2003
    Inventors: Reiner Fischer, Thomas Bretschneider, Hermann Hagemann, Folker Lieb, Norbert Lui, Michael Ruther, Arno Widdig, Christoph Erdelen, Ulrike Wachendorff-Neumann, Hans-Joachim Santel, Markus Dollinger, Peter Dahmen, Norbert Mencke, Andreas Turberg
  • Patent number: 6485868
    Abstract: The invention relates to an electrolyte for an electrochemical device. This electrolyte includes 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 electrolyte has high heat resistance and hydrolysis resistance as compared with conventional electrolytes.
    Type: Grant
    Filed: July 25, 2000
    Date of Patent: November 26, 2002
    Assignee: Central Glass Company, Limited
    Inventors: Shoichi Tsujioka, Hironari Takase, Mikihiro Takahashi
  • Patent number: 6469000
    Abstract: Disclosed are compounds which are inhibitors of metalloproteases having the following structure: where Ar, W, X, Y, Z, R1 and R2 have the meanings described in the specification and optical isomers, diastereomers, and enantiomers thereof or a pharmaceutically-acceptable salt, or biohydrolyzable amides, esters, or imides thereof. Also disclosed are pharmaceutical compositions and methods of treating diseases, disorders and conditions characterized by unwanted metalloprotease activity using these compounds or pharmaceutical compositions.
    Type: Grant
    Filed: August 29, 2000
    Date of Patent: October 22, 2002
    Assignee: The Procter & Gamble Co.
    Inventors: Stanislaw Pikul, Kelly Lynn McDow-Dunham, Neil Gregory Almstead, Biswanath De, Michael George Natchus, Yetunde Olabisi Taiwo
  • Publication number: 20020123491
    Abstract: Compound represented by the structural formula 1
    Type: Application
    Filed: December 14, 2000
    Publication date: September 5, 2002
    Inventors: Neng-Yang Shih, Ho-Jane Shue, Gregory A. Reichard, Sunil Paliwal, David J. Blythin, John J. Piwinski, Dong Xiao, Xiao Chen
  • Patent number: 6410482
    Abstract: (Het)Arylsulfonylureas having an imino function, their preparation, and their use as herbicides and plant growth regulators Compounds of the formula (I) and salts thereof in which A is a (hetero)aromatic or heterocyclic bridge linked to the group SO2 by a direct bond, or via O, S, NH, CH2 or via alkylated NH or alkylated methylene, B is a group having an imino-containing fragment N═C—N, N═C—S, N═C—O or N═C—C which is linked to A by one of the nitrogen atoms of the fragment, R═H or an aliphatic radical, W═O or S and X, Y and Z are as defined in claim 1 are suitable as herbicides and plant growth regulators. The preparation is carried out for example similarly to known processes via novel intermediates of the formula (XII) (cf.
    Type: Grant
    Filed: May 13, 1997
    Date of Patent: June 25, 2002
    Assignee: Hoechst Schering AgrEvo GmbH
    Inventors: Gerhard Schnabel, Lothar Willms, Klaus Bauer, Hermann Bieringer, Christopher Rosinger
  • 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: 6395730
    Abstract: Certain thiazolidinone and metathiazanone compounds, as described, are useful as potassium channel inhibitors and are especially useful for the treatment of cardiac arrhythmias and other diseases, conditions and disorders.
    Type: Grant
    Filed: October 13, 2000
    Date of Patent: May 28, 2002
    Assignees: Icagen, Inc., Eli Lilly and Company
    Inventors: Michael F. Gross, Neil A. Castle, Jose S. Mendoza
  • 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
  • Publication number: 20020022575
    Abstract: The present invention relates to new compounds of the formula (I) 1
    Type: Application
    Filed: April 20, 2001
    Publication date: February 21, 2002
    Inventors: Reiner Fischer, Thomas Bretschneider, Hermann Hagemann, Folker Lieb, Michael Ruther, Arno Widdig, Peter Dahmen, Markus Dollinger, Christoph Erdelen, Hans-Joachim Santel, Ulrike Wachendorff-Neumann, Alan Graff, Wolfram Andersch
  • Publication number: 20020004503
    Abstract: A compound of the formula: 1
    Type: Application
    Filed: April 18, 2001
    Publication date: January 10, 2002
    Inventors: Hing Leung Sham, Daniel W. Norbeck, Xiaoqi Chen, David A. Betebenner, Dale J. Kempf, Thomas R. Herrin, Gondi N. Kumar, Stephen L. Condon, Arthur J. Cooper, Daniel A. Dickman, Steven M. Hannick, Lawrence Kolaczkowski, Patricia A. Oliver, Daniel J. Plata, Peter J. Stengel, Eric J. Stoner, Jieh-Heh J. Tien, Jih-Hua Liu, Ketan M. Patel
  • Patent number: 6268311
    Abstract: 1-Amino-3-benzyluracils I (X=oxygen, sulfur; R1=C1-C4-haloalkyl; R2=H, halogen; R3, R7=H, CN, SCN, halogen, C1-C4-haloalkyl, C1-C4-haloalkoxy, C1-C4-haloalkylthio; R4=H, CN, SCN, halogen, C1-C4-alkyl, C1-C4-haloalkyl, C1-C4-alkoxy, C1-C4-haloalkoxy, C1-C4-haloalkylthio, C1-C6-alkylaminocarbonyl; R5=H, CN, NO2, halogen, OH, C1-C4-alkoxy, NH2, C1-C6-alkyl-amino; R6=H, CN, NO2, halogen, OH, C1-C4-alkoxy, NH2, C1-C6-alkyl-amino, CHO) and their salts are used as herbicides and for the desiccation/defoliation of plants.
    Type: Grant
    Filed: March 17, 1998
    Date of Patent: July 31, 2001
    Assignee: BASF Aktiengesellschaft
    Inventors: Olaf Menke, Ralf Klintz, Gerhard Hamprecht, Elisabeth Heistracher, Peter Schäfer, Cyrill Zagar, Norbert Götz, Karl-Otto Westphalen, Ulf Misslitz, Helmut Walter
  • 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: 6172060
    Abstract: Disclosed are nitrosated and/or nitrosylated phosphodiesterase inhibitors having the formula NOn-PDE inhibitor where n is 1 or 2. The invention also provides compositions comprising such compounds in a pharmaceutically acceptable carrier. The invention also provides a composition comprising a therapeutically effective amount of an phosphodiesterase inhibitor (PDE inhibitor), which can optionally be substituted with at least one NO or NO2 moiety, and one to ten fold molar excess of a compound that donates, transfers or releases nitrogen monoxide as a charged species, i.e., nitrosonium (NO+) or nitroxyl (NO−), or as the neutral species, nitric oxide (NO•) or which stimulates endogenous EDRF production. The invention also provides compositions comprising such compounds in a pharmaceutically acceptable carrier. The invention also provides methods for treating sexual dysfunctions in males and females.
    Type: Grant
    Filed: February 10, 1999
    Date of Patent: January 9, 2001
    Assignee: NitroMed, Inc.
    Inventors: David S. Garvey, Inigo Saenz de Tejada
  • Patent number: 6156794
    Abstract: A method of using a compound of formula (I) wherein R.sup.1, R.sup.2, R.sup.3, X and n have any of the meanings defined in the specification, to antagonize glutamate binding, or to treat glutamate-related disorders is provided. Novel compounds, intermediates and pharmaceutical compositions are also provided.
    Type: Grant
    Filed: September 13, 1999
    Date of Patent: December 5, 2000
    Inventors: Morris Faiman, John V. Schloss, Jang-Yen Wu
  • Patent number: 6114327
    Abstract: The present application provides a series of benzimidazole compounds of formula I: ##STR1## which inhibit the growth of picornaviruses, such as rhinoviruses (bovine and human), enteroviruses such as polioviruses, coxsackieviruses of the A and B groups, or echo virus, cardioviruses such as encephalomyocarditis (EMC), apthoviruses such as foot and mouth disease virus, and flaviviruses such as hepatitis C virus and bovine viral diarrhea virus.Such compounds are also useful as intermediates for preparing additional benzimidazole antiviral compounds.
    Type: Grant
    Filed: October 22, 1999
    Date of Patent: September 5, 2000
    Assignee: Eli Lilly and Company
    Inventors: Steven Eugene Dunlap, Louis Nickolaus Jungheim, Mark Joseph Tebbe, Gilbert Thomas Voy, John Arnold Werner
  • Patent number: 6048824
    Abstract: Compounds of formula (I), 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 ##STR2## R.sub.1 is hydrogen or C.sub.1 -C.sub.3 alkyl; R.sub.2 is hydrogen or C.sub.1 -C.sub.3 alkyl; R.sub.3 is hydrogen, an unsubstituted or substituted C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 cycloalkyl C.sub.2 -C.sub.6 alkenyl or C.sub.2 -C.sub.6 alkynyl group, or C(.dbd.O)--R.sub.5, R.sub.5 is C.sub.1 -C.sub.4 alkyl C.sub.1 -C.sub.4 alkoxy, an unsubstituted or substituted phenyl, phenoxy or benzyloxy group, or N(R.sub.6).sub.2, each R.sub.6, independently of the other, is hydrogen, C.sub.1 -C.sub.4 alkyl or unsubstituted or substituted phenyl, X is CH--NO.sub.2, N--CN or N--NO.sub.2 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: November 22, 1995
    Date of Patent: April 11, 2000
    Assignee: Novartis Corporation
    Inventors: Peter Maienfisch, Jozef Gonda, Olivier Jacob, Laurenz Gsell
  • Patent number: 6048999
    Abstract: This invention provides sweetener blends comprising N-[N-(3,3-dimethylbutyl)-L-.alpha.-aspartyl]-L-phenylalanine 1-methyl ester and another sweetener. The sweetener blends of this invention exhibit isobole synergy.
    Type: Grant
    Filed: January 25, 1999
    Date of Patent: April 11, 2000
    Assignee: The NutraSweet Company
    Inventors: Laurie L. Pajor, Kernon M. Gibes
  • Patent number: 6008223
    Abstract: Compounds of formula I ##STR1## wherein Q.sup.1, Q.sup.2, Q.sup.3, and Q.sup.4 have any of the meanings given in the specification, their N-oxides, and their pharmaceutically acceptable salts are nonpeptide antagonists of SP and NKA are useful for the treatment of asthma, etc. Also disclosed are pharmaceutical compositions, processes for preparing the compounds of formula I and intermediates.
    Type: Grant
    Filed: January 20, 1998
    Date of Patent: December 28, 1999
    Assignee: Zeneca Limited
    Inventors: Peter R. Bernstein, Scott C. Miller
  • Patent number: 5965565
    Abstract: The present invention is directed to certain piperidines, pyrrolidines, and hexahydro-1H-azepines of the general structural formula: ##STR1## wherein B is selected from: ##STR2## and R.sup.1, R.sup.1a, R.sup.2a, R.sup.3a, R.sup.3b, R.sup.4, R.sup.4a, R.sup.4b, R.sup.4c, R.sup.5, D, X, Y, n, x and y are as defined herein. These compounds promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to treat physiological or medical conditions characterized by a deficiency in growth hormone secretion, such as short stature in growth hormone deficient children, and to treat medical conditions which are improved by the anabolic effects of growth hormone. Growth hormone releasing compositions containing such compounds as the active ingredient thereof are also disclosed.
    Type: Grant
    Filed: December 11, 1997
    Date of Patent: October 12, 1999
    Assignee: Merck & Co., Inc.
    Inventors: Meng H. Chen, Zhijian Lu, Ravi Nargund, Arthur A. Patchett, James R. Tata, Lihu Yang, Mu Tsu Wu
  • Patent number: 5861380
    Abstract: The present invention relates to certain substituted oxadiazole, thiadiazole and triazole peptoids which are useful as inhibitors of human neutrophil elastase (HNE) for the treatment of HNE-mediated processes implicated in conditions such as adult respiratory distress syndrome, septic shock and multiple organ failure. A series of studies also have indicated the involvement HNE in myocardial ischemia-reperfusion injury, emphysema. HNE-mediated processes are implicated in other conditions such as arthritis, periodontal disease, glomerulonephritis, dermatitis, psoriasis, cystic fibrosis, chronic bronchitis, atherosclerosis, Alzheimer's disease, organ transplantation, corneal ulcers, and invasion behavior of malignant tumors.
    Type: Grant
    Filed: December 6, 1996
    Date of Patent: January 19, 1999
    Assignee: Cortech, Inc.
    Inventors: Albert Gyorkos, Lyle W. Spruce
  • Patent number: 5854241
    Abstract: Disclosed are pyrido?3,2,1-i,j!?3,1!benzoxazine compounds of the formula (I): ##STR1## wherein z represents a radical having the formula: ##STR2## wherein B represents --CH.sub.2 --, --O-- or a direct bond; and the other variables in formula (I) and Z are as described herein. The compounds have antibacterial properties and also disclosed are antibacterial compositions containing them and methods of using them to prevent or combat bacterial infections. Methods for preparing the compounds are also disclosed.
    Type: Grant
    Filed: January 3, 1997
    Date of Patent: December 29, 1998
    Assignee: Bayer Aktiengesellschaft
    Inventors: Werner Hallenbach, Thomas Himmler, Thomas Jaetsch, Burkhard Mielke, Klaus Dieter Bremm, Rainer Endermann, Franz Pirro, Michael Stegemann, Heinz-Georg Wetzstein
  • Patent number: 5847115
    Abstract: There is disclosed an azetidinone compound of the formula ?I!: ##STR1## wherein Ring B is a benzene ring which may have substituent(s), R.sup.1 is a hydroxy-substituted lower alkyl group which may have substituent(s), X is oxygen atom and the like, Y is oxygen atom and the like, and Z is a methylene group which may have substituent(s), which is useful as a synthetic intermediate of the 1 .beta.-methylcarbapenem-type antibacterial agent.
    Type: Grant
    Filed: November 1, 1996
    Date of Patent: December 8, 1998
    Assignee: Tanabe Seiyaku Co., Ltd.
    Inventors: Tameo Iwasaki, Kazuhiko Kondo
  • Patent number: 5840732
    Abstract: This invention provides a new condensed imidazole compound possessing inhibitory activity of adhesion molecule expression.This invention also provides a therapeutic and prophylactic agent for diabetic nephritis and/or autoimmune disease and an immunosuppressor for organ transplantation.
    Type: Grant
    Filed: December 6, 1996
    Date of Patent: November 24, 1998
    Assignee: Takeda Chemical Industries Ltd.
    Inventors: Muneo Takatani, Hitoshi Ikeda, Kyoko Iida, Hidenori Abe
  • Patent number: 5789404
    Abstract: 3-Substituted 1-arylindole compounds are provided having general formula (I) ##STR1## wherein Ar is an optionally substituted aryl group; X represents a divalent hydrocarbon group, methyleneoxy or -thioxo; R.sup.1 -R.sup.4 are hydrogen or other substituents; R.sup.5 is hydrogen, alkyl, alkenyl, etc.; R.sup.6 and R.sup.7 are independently hydrogen, alkyl, alkenyl, etc.; R.sup.8 is alkyl, alkenyl or R.sup.8 represents a group of formula 1a or 1b; wherein n is an integer from 2-8; W is O or S; U is N or CH; Z is (CH.sub.2).sub.m, m being 2 or 3, 1,2-phenylene optionally substituted with halogen or trifluoromethyl, CH.dbd.CH, COCH.sub.2 or CSCH.sub.2 ; V is O, S, CH.sub.2 or NR.sup.10, wherein R.sup.10 is hydrogen, alkyl, alkenyl, cycloalkyl, etc.; U.sup.1 is O, S, CH.sub.2 or a group NR.sup.11, wherein R.sup.11 is hydrogen, alkyl, alkenyl, etc.; and V.sup.1 is NR.sup.12 R.sup.13, OR.sup.14, SR.sup.15 or CR.sup.16 R.sup.17 R.sup.18, where R.sup.12 -R.sup.18 are as the R.sup.10 substituents; R.sup.
    Type: Grant
    Filed: August 12, 1996
    Date of Patent: August 4, 1998
    Assignee: H. Lundbeck A/S
    Inventors: Kim Andersen, Jens Kristian Perregaard
  • Patent number: 5760033
    Abstract: A compound represented by the chemical formula ?1!: ##STR1## wherein Z is oxygen or sulfur, Y is halogen, optionally substituted alkyl, optionally substituted alkoxycarbonyl, optionally substituted alkoxy, S(O).sub.p r.sup.1 wherein p denotes an integer from 0 to 2, r.sup.1 is optionally substituted alkyl, nitro, cyano or optionally substituted amino, m denotes an integer from 1 to 3, R.sub.1, R.sub.2 and R.sub.4 are same or different one another and each independently hydrogen, optionally substituted alkyl or optionally substituted phenyl, R.sub.3 is alkyl, alkenyl, aralkyl, cycloalkyl, phenyl, naphthyl, pyridyl, furyl or thienyl, those which substituents can be further optionally substituted by halogen, hydroxy, optionally substituted alkyl or the like, and a chemical agent for controlling pests.
    Type: Grant
    Filed: August 25, 1995
    Date of Patent: June 2, 1998
    Inventors: Yasuo Yamada, Takashi Kishimoto, Michihiko Matsuda, Renpei Hatano, Takao Iwasa, Makio Yano
  • Patent number: 5739130
    Abstract: Heterotricyclic derivatives of the formula: ##STR1## wherein R.sup.1 is hydrogen, lower alkyl, lower alkoxy, lower alkylthio, halogen, nitro, amino or protected amino,R.sup.2 is hydroxy, protected hydroxy, halogen, amino or protected amino,R.sup.3 is hydrogen or an organic group,R.sup.4 is hydrogen or lower alkyl,R.sup.8 is hydrogen or lower alkyl, and--Z-- is --O-- or a group of the formula: ##STR2## (in which n is 0, 1 or 2), and pharmaceutically acceptable salts thereof which are useful as a medicament.
    Type: Grant
    Filed: September 4, 1996
    Date of Patent: April 14, 1998
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Masaaki Matsuo, Kiyoshi Tsuji, Katsuya Nakamura, Glen W. Spears
  • Patent number: 5686454
    Abstract: The invention is directed to a series of novel compounds of the formula ##STR1## where Y is carbonyl or sulfonyl; R.sup.7 and R.sup.8 are alkyl, or R.sup.7 and R.sup.8, together with the carbon to which they are attached, form a C.sub.3-6 carbocyclic ring; R.sup.9 and R.sup.10 are each independently selected from hydrogen, hydroxyl, oximido, methyl, carboxyl, carboxyalkyl, unsubstituted or substituted alkoxycarbonyl, alkylcarbonyloxyalkyl, cyanoalkyl, hydroxyalkyl or unsubstituted amino; R.sup.11 is hydrogen, oxo, --N(R.sup.12)--CO--R.sup.13 or --CO--N(R.sup.14)--R.sup.15 ; R.sup.12 is hydrogen or unsubstituted or substituted alkyl; R.sup.13 is alkoxyl, unsubstituted or substituted heterocyclic rings selected from ##STR2## or unsubstituted or substituted alkyl; and R.sup.14 and R.sup.15 are each independently selected from hydrogen or unsubstituted or substituted alkyl. The Y moiety cannot be bonded to the camphor ring at the 3 or 6 positions.
    Type: Grant
    Filed: January 16, 1996
    Date of Patent: November 11, 1997
    Assignee: Merck & Co., Inc.
    Inventors: Mark G. Bock, Doug W. Hobbs
  • Patent number: RE39130
    Abstract: Novel heterocyclic compounds of the formula wherein, R1 represents a hydrogen atom or an alkyl group, A represents an ethylene group which may be substituted by alkyl or a trimethylene group which may be substituted by alkyl, X represents an oxygen or sulfur atom or the group in which R2 represents a hydrogen atom of an optionally substituted alkyl, an alkenyl, an alkynyl or an acyl group, and R3 represents a hydrogen atom or an alkyl group, and Z represents an optionally substituted 5- or 6-membered heterocyclic group which contains at least two hetero atoms selected from oxygen, sulfur and nitrogen atoms, or an optionally substituted 3- or 4-pyridyl group. The above defined novel heterocyclic compounds of formula (I) exhibit powerful insecticidal properties.
    Type: Grant
    Filed: June 6, 1994
    Date of Patent: June 13, 2006
    Assignee: Bayer Cropscience K.K.
    Inventors: Kozo Shiokawa, Shinichi Tsuboi, Shinzo Kagabu, Shoko Sasaki, Koichi Moriya, Yumi Hatori