Patents Issued in January 14, 2003
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Patent number: 6506866Abstract: Disclosed is a novel ethylene copolymer by copolymerizing an ethylene and at least one comonomer selected from a compound represented by the formula H2C═CHR wherein R is an alkyl group or an aryl group, and a diene, by slurry polymerization process in the presence of a solid catalyst system comprising a support, a transition metal compound and an activator capable of converting the transition metal compound into a catalytically active transition metal complex. The produced copolymer has a density of from 0.870 to 0.Type: GrantFiled: May 16, 1997Date of Patent: January 14, 2003Assignee: Dow Global Technologies Inc.Inventors: Grant B. Jacobsen, Fumio Matsushita, Lee Spencer, Peter L. Wauteraerts
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Patent number: 6506867Abstract: Elastic ethylene polymers are disclosed which have processability similar to highly branched low density polyethylene (LDPE), but the strength and toughness of linear low density polyethylene (LLDPE). The polymers have processing indices (PI's) less than or equal to 70 percent of those of a comparative linear ethylene polymer and a critical shear rate at onset of surface melt fracture of at least 50 percent greater than the critical shear rate at the onset of surface melt fracture of a traditional linear ethylene polymer at about the same I2 and Mw/Mn. The novel polymers can also have from about 0.01 to about 3 long chain branches/1000 total carbons and have higher low/zero shear viscosity and lower high shear viscosity than comparative linear ethylene polymers. The novel polymers can also be characterized as having a melt flow ratio, I10/I2, ≧5.63, a molecular weight distribution, Mw/Mn, defined by the equation: Mw/Mn≦(I10/I2)−4.Type: GrantFiled: October 18, 2000Date of Patent: January 14, 2003Assignee: The Dow Chemical CompanyInventors: Shih-Yaw Lai, John R. Wilson, George W. Knight, James C. Stevens
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Patent number: 6506868Abstract: The present invention provides a partial condensate of glycidyl ether group-containing alkoxysilane which is obtainable by dealcoholization reaction between glycidol and a partial condensate of alkoxysilane, compositions comprising the same and preparation methods thereof. Further, the present invention provides an alkoxy-containing silane-modified polyimide resin, alkoxy-containing silane-modified polyamide-imide resin and alkoxy-containing silane-modified phenol resin which are modified with the partial condensate of glycidyl ether group-containing alkoxysilane, and preparation methods thereof.Type: GrantFiled: March 7, 2001Date of Patent: January 14, 2003Assignee: Arakawa Chemical Industries, Ltd.Inventors: Hideki Goda, Shoji Takeda, Tetsuji Higashino
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Patent number: 6506869Abstract: A one-pack type epoxy resin composition is desclosed. The composition comprises a low-viscosity epoxy resin and an acid anhydride hardener, and has a viscosity of 250 P or less at 25° C. The hardener is an imide oligomer comprising an imide unit and having an acid anhydride group at the terminal thereof. The imide unit is represented by formula I: wherein A represents an asymmetric aromatic tetracarboxylic dianhydride residue or alicyclic tetracarboxylic dianhydride residue; and B represents a diaminopolysiloxane residue.Type: GrantFiled: September 25, 2001Date of Patent: January 14, 2003Assignee: Ube Industries, Ltd.Inventors: Hiroaki Yamaguchi, Masafumi Kohda
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Patent number: 6506870Abstract: Disclosed is a substantially chlorine-free polycarbonate resin for use in the production of a substrate for an optical information medium, which is produced by transesterification reaction and which comprises a plurality of aromatic polycarbonate main chains, each comprising recurring units each independently represented by formula (1): wherein the polycarbonate main chains collectively contain therein at least one heterounit (A) of formula (2): and at least one heterounit (B) of formula (3): wherein the sum of the amounts of (A) and (B) is from 0.03 to 0.3 mole %, based on the total molar amount of units (1), and the amount of (A) is at least 50 mole %, based on the total molar amount of (A) and (B), the weight average molecular weight of the polycarbonate resin being from 13,000 to 18,000.Type: GrantFiled: April 27, 2000Date of Patent: January 14, 2003Assignee: Asaki Kasei Kabushiki KaishaInventors: Hiroshi Hachiya, Shinya Kawasoe
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Patent number: 6506871Abstract: Extrusion of a mixture of an ester-substituted diaryl carbonate, such as bis(methyl salicyl) carbonate, a dihydroxy aromatic compound such as bisphenol A and a transesterification catalyst such as tetrabutylphosphonium acetate (TBPA) affords polycarbonate having a weight average molecular weight of greater than 20,000 daltons. The extruder is equipped with one or more vacuum vents to remove by-product ester-substituted phenol. Similarly, a precursor polycarbonate having ester-substituted phenoxy endgroups, for example methyl salicyl endgroups, when subjected to extrusion affords a polycarbonate having a significantly increased molecular weight relative to the precursor polycarbonate. The reaction to form a higher molecular weight polycarbonate may be catalyzed by residual transesterification catalyst present in the precursor polycarbonate, or by a combination of any residual catalyst and an additional catalyst such as TBPA introduced in the extrusion step.Type: GrantFiled: June 12, 2002Date of Patent: January 14, 2003Assignee: General Electric CompanyInventors: Norberto Silvi, Patrick Joseph McCloskey, James Day, Mark Howard Giammattei
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Patent number: 6506872Abstract: A novel polycyanoaryl ether exhibiting excellent heat-resistance, hydrolysis-resistance and weatherability, as well as industrially high general-purpose properties, and the method for the production thereof is to be provided. The polycyanoaryl ether of this invention is represented by the formula (1): wherein R1 stands for a substituted or unsubstituted alkyl group of 1 to 12 carbon atoms, a substituted or unsubstituted alkoxy group of 1 to 12 carbon atoms, a substituted or unsubstituted alkylamino group of 1 to 12 carbon atoms, a substituted or unsubstituted alkylthio group of 1 to 12 carbon atoms, a substituted or unsubstituted aryl group of 6 to 20 carbon atoms, a substituted or unsubstituted aryloxy group of 6 to 20 carbon atoms, a substituted or unsubstituted arylamino group of 6 to 20 carbon atoms, or a substituted or unsubstituted arylthio group of 6 to 20 carbon atoms; R2 stands for a divalent organic group; and n stands for a degree of polymerization.Type: GrantFiled: April 25, 2001Date of Patent: January 14, 2003Assignee: Nippon Shokubai Co., Ltd.Inventors: Kunio Kimura, Yuhiko Yamashita, Yasunori Okumura, Shoji Ito
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Patent number: 6506873Abstract: The present invention relates to a fibrous material which includes a plurality of polylactide containing fibers. The plurality of polylactide containing fibers can be considered low shrinkage or high shrinkage. The plurality of polylactide containing fibers are considered low shrinkage fibers if they provide a boiling water shrinkage propensity of less than about 20%. The plurality of polylactide containing fibers are considered high shrink fibers if they provide an average fiber boiling water shrinkage propensity of greater than about 10% and a heat of fusion of less than about 25 J/g. The invention additionally relates to the use of an extrusion process to provide low shrinkage fibers and high shrinkage fibers. The invention further relates to the use of these fibers in desirable products.Type: GrantFiled: May 4, 1998Date of Patent: January 14, 2003Assignee: Cargill, IncorporatedInventors: Christopher Michael Ryan, Nancy Uzelac Buehler, Scott Louis Gessner, Andrea Lee Brosch
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Patent number: 6506874Abstract: IGF-I and insulin variants are provided that selectively bind to IGFBP-1 or IGFBP-3. These agonist variants are useful, for example, to improve the half-lives of IGF-I and insulin, respectively.Type: GrantFiled: November 28, 2000Date of Patent: January 14, 2003Assignee: Genentech, Inc.Inventors: Yves Dubaquie, Henry Lowman
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Patent number: 6506875Abstract: The invention teaches peptide epitopes which bind to HLA-Cw3 and HLA-Cw6 molecules on the surface of cells. The peptides are useful diagnostically and therapeutically, as are DNA molecules which encode them, and the cytolytic T lymphocytes specific to the HLA/peptide complexes. Also a feature of the invention is a method for identifying relevant molecules such as those described herein, in a system that uses stimulation and restimulation using different viral vectors.Type: GrantFiled: September 26, 2000Date of Patent: January 14, 2003Assignee: Ludwig Institute for Cancer ResearchInventors: Sacha Gnjatic, Lloyd J. Old, Yasuhiro Nagata, Elke Jager, Yao-Tseng Chen, Alexander Knuth
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Patent number: 6506876Abstract: The present invention provides compounds of the formula Ar1—Q—Ar2—Y—R—Z and pharmaceutically acceptable salts thereof wherein Ar1 and Ar2 are optionally substituted aryl moieties, Z is an optionally substituted nitrogen-containing moiety which may be an acyclic, cyclic or bicyclic amine or an optionally substituted monocyclic or bicyclic nitrogen-containing heteroaromatic moiety; Q is a linking group capable of linking two aryl groups; R is an alkylene moiety; Y is a linking moiety capable of linking an aryl group to an alkylene moiety and wherein Z is bonded to R through a nitrogen atom. The compounds and pharmaceutical compositions of the present invention are useful in the treatment of inflammatory diseases which are mediated by LTB4 production, such as psoriasis, ulcerative colitis, IBD and asthma.Type: GrantFiled: October 11, 1994Date of Patent: January 14, 2003Assignee: G.D. Searle & Co.Inventors: Nizal Samuel Chandrakumar, Barbara Baosheng Chen, Michael Clare, Bipinchandra Nanubhai Desai, Stevan Wakefield Djuric, Stephen Hermann Docter, Alan Frank Gasiecki, Richard Arthur Haack, Chi-Dean Liang, Julie Marion Miyashiro, Thomas Dale Penning, Mark Andrew Russell, Stella Siu-tzyy Yu
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Patent number: 6506877Abstract: The present invention relates to the discovery, identification and characterization of nucleotides that encode Ob receptor (ObR), a receptor protein that participates in mammalian body weight regulation. The invention encompasses obR nucleotides, host cell expression systems, ObR proteins, fusion proteins, polypeptides and peptides, antibodies to the receptor, transgenic animals that express an obR transgene, or recombinant knock-out animals that do not express the ObR, antagonists and agonists of the receptor, and other compounds that modulate obR gene expression or ObR activity that can be used for diagnosis, drug screening, clinical trial monitoring, and/or the treatment of body weight disorders, including but not limited to obesity, cachexia and anorexia.Type: GrantFiled: December 28, 1995Date of Patent: January 14, 2003Assignee: Millennium Pharmaceuticals, Inc.Inventors: Louis A Tartaglia, Robert I Tepper, Janice A Culpepper
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Patent number: 6506878Abstract: HMTMF81 polypeptides and polynucleotides and methods for producing such polypeptides by recombinant techniques are disclosed. Also disclosed are methods for utilizing HMTMF81 polypeptides and polynucleotides in the design of protocols for the treatment of infections such as bacterial, fungal, protozoan and viral infections, particularly infections caused by HIV-1 or HIV-2; pain; cancers; anorexia; bulimia; asthma; Parkinson's disease; acute heart failure; hypotension; hypertension; urinary retention; osteoporosis; angina pectoris; myocardial infarction; ulcers; asthma; allergies; benign prostatic hypertrophy; and psychotic and neurological disorders, including anxiety, schizophrenia, manic depression, delirium, dementia, severe mental retardation and dyskinesias, such as Huntington's disease or Gilles dela Tourett's syndrome, among others and diagnostic assays for such conditions.Type: GrantFiled: June 5, 2000Date of Patent: January 14, 2003Assignee: Smithkline Beecham CorporationInventors: Catherine E. Ellis, Wendy Halsey, Ganesh M. Sathe, Robert S. Ames, James J. Foley, Henry M. Sarau, Jon Chambers
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Patent number: 6506879Abstract: A substantially endotoxin-free ApoA or ApoE is produced by recombinant DNA technique, suitably in E. coli. Medicaments and methods for treatment of atherosclerosis or cardiovascular diseases employ ApoA or ApoE purified by a process comprising contacting a first aqueous solution comprising ApoA or ApoE and endotoxins with a matrix comprising an immobilized compound with an end group comprising two or three nitrogen atoms bonded to a carbon atom for attaching the endotoxins to the matrix, and subsequently treating the matrix comprising the immobilized compound with a second aqueous solution comprising a surfactant for releasing the ApoA or ApoE while the endotoxins remain attached to the matrix.Type: GrantFiled: November 22, 1999Date of Patent: January 14, 2003Assignee: Esperion Therapeutics, Inc.Inventors: Hans Ageland, Lena Romander
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Patent number: 6506880Abstract: The present invention provides novel synthetic apolipoprotein E (ApoE)-mimicking peptides wherein the receptor binding domain of apolipoprotein E is covalently linked to 18A, the well characterized lipid-associating model class A amphipathic helical peptide. Such peptides enhance low density lipoprotein (LDL) and very low density lipoprotein (VLDL) binding to and degradation b y fibroblast or HepG2 cells. Also provided are possible applications of the synthetic peptides in lowering human plasma LDL/VLDL cholesterol levels, thus inhibiting atherosclerosis.Type: GrantFiled: March 7, 2000Date of Patent: January 14, 2003Assignee: The UAB Research FoundationInventor: Gattadahalli M. Anantharamaiah
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Patent number: 6506881Abstract: Humanized antibody molecules (HAMs) are described having specificity for human milk fat globule and having an antigen binding site wherein at least one of the complementarity determining regions (CDRs) of the variable domains is derived from the mouse monoclonal antibody CTMO1 and the remaining immunoglobulin-derived parts of the HAM are derived from a human immunoglobulin. The HAMs may be chimeric humanized antibodies or CDR-grafted humanized antibodies and are preferably produced by recombinant DNA techniques. The HAMs are useful for in vivo diagnosis and therapy.Type: GrantFiled: May 25, 1995Date of Patent: January 14, 2003Assignee: Celltech R&D LimitedInventors: John Robert Adair, Raymond John Owens, Terence Seward Baker, Alan Howard Lyons
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Patent number: 6506882Abstract: The invention relates to human TNF delta and TNF epsilon polypeptides, polynucleotides encoding the polypeptides, methods for producing the polypeptides, in particular by expressing the polynucleotides, and agonists and antagonists of the polypeptides. The invention further relates to methods for utilizing such polynucleotides, polypeptides, agonists and antagonists for applications, which relate, in part, to research, diagnostic and clinical arts.Type: GrantFiled: February 26, 2002Date of Patent: January 14, 2003Assignee: Human Genome Sciences, Inc.Inventors: Guo-Liang Yu, Jian Ni, Reiner Gentz, Patrick J. Dillon
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Patent number: 6506883Abstract: Humanized and chimeric monoclonal antibodies that recognize EGF-R and comprise an artificial sequence at least of the FRs of the heavy chain variable region of a human immunoglobulin. The humanized and monoclonal antibodies may comprise variable regions of non-human origin and constant regions of human origin with amino acid substitutions with the variable regions and/or framework regions. Use of the antibodies for therapeutical and diagnostic purposes is also disclosed.Type: GrantFiled: December 21, 1998Date of Patent: January 14, 2003Assignee: Centro de Inmunologia MolecularInventors: Christina Maria Meteo de Acosta del Rio, Rolando Pérez RodrÃguez, Ernesto Moreno FrÃas
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Patent number: 6506884Abstract: The invention concerns novel nucleic acid sequences and amino acid sequences of a novel variant of vascular endothelial growth factor (VEGF). The invention further concerns expression vectors and host cells containing said sequences as well as pharmaceutical compositions and detection methods using said sequences.Type: GrantFiled: March 6, 2000Date of Patent: January 14, 2003Assignee: Compugen Ltd.Inventors: Liat Mintz, Kinneret Savitzky, Sharon Engel
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Patent number: 6506885Abstract: Hybridoma cell lines have been generated which produce and secrete monoclonal antibodies which selectively bind to tilmicosin. These hybridomas may be obtained by using as an immunization agent or immunogen, 23-deoxo-23-demycinosyl tilmicosin which has been conjugated to an immunogenic carrier. The antibodies may be used to detect and/or quantify tilmicosin in biological samples. The monoclonal antibodies also may be incorporated into kits.Type: GrantFiled: September 27, 2001Date of Patent: January 14, 2003Assignee: The United States of America as represented by the Secretary of AgricultureInventor: Ross C. Beier
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Patent number: 6506886Abstract: Form II crystals of clarithromycin can be easily prepared by treating clarithromycin of different crystal forms with water or with a mixture of water and a water-immiscible organic solvent and isolating treated crystals by filtration.Type: GrantFiled: March 7, 2001Date of Patent: January 14, 2003Assignee: Hanmi Pharm. Co., Ltd.Inventors: Tae-Suk Lee, Ju-Cheol Lee, Kyoung-Ik Lee, Gwan-Sun Lee, Wan-Joo Kim
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Patent number: 6506887Abstract: The invention provides method for producing nucleic acid ligands that generate a signal, or cause a decrease in the level of a signal, in the presence of a target molecule or an environmental stimulus. The methods of the instant invention are collectively termed Conditional SELEX. The nucleic acid ligands of the instant invention are useful in any application where it is desirable to measure the concentration of a target molecule or detect and quantitate an environmental stimulus.Type: GrantFiled: July 29, 1999Date of Patent: January 14, 2003Assignee: SomaLogic, IncorporatedInventors: Jonathan Drew Smith, Larry Gold
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Patent number: 6506888Abstract: Novel nucleoside or nucleotide analogs comprising 2′-O-amino residues, processes for their synthesis and incorporation into polynucleotides.Type: GrantFiled: September 19, 2000Date of Patent: January 14, 2003Assignee: Ribozyme Pharmaceuticals, Inc.Inventors: Alexander Karpeisky, Leonid Beigelman
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Patent number: 6506889Abstract: The present invention relates to Ras suppressors, in particular the Ras suppressor SUR-8. The present invention provides isolated nucleotide sequence encoding SUR-8, isolated SUR-8 peptides, antibodies that specifically bind SUR-8, methods for the detection of SUR-8, methods for producing SUR-8 transgenic animals, non-human animals expressing SUR-8, and methods for screening compounds for the ability to alter SUR-8 associated signal transduction.Type: GrantFiled: May 19, 1998Date of Patent: January 14, 2003Assignee: University Technology CorporationInventors: Min Han, Derek Sieburth
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Patent number: 6506890Abstract: An automated nucleic acid compaction device for analyzing and compacting a nucleic acid complex into unimolecular nucleic acid particles. Broadly, the device includes a container support and agitation system; a measuring and testing system; and a dispensing system; all controlled by a control system. The control system controls the support and agitation system and the dispensing system based either on a predetermined formulation or by analysis of feedback data provided by the measuring and testing system. In a preferred embodiment, the device is a real-time measuring and mixing instrument operating in a closed loop system. The preferred embodiment also comprises a monitoring system including a submersible probe which is positioned in the batch solution to provide data to a controller. Once a desired level of nucleic acid compaction is reached, as detected by the monitoring system, the controller stops the dispensing and mixing agitating systems.Type: GrantFiled: November 28, 2000Date of Patent: January 14, 2003Inventors: Mark J. Cooper, Tomasz H. Kowalczyk, Murali Krishna Pasumarthy
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Patent number: 6506891Abstract: This invention provides cells containing recombinant polynucleotides coding for cell surface molecules that, when expressed in the cell, result in rejection of the cell by the host immune system. The invention also provides methods of using such cells, and capsules for delivery of biologically active molecules to a patient.Type: GrantFiled: January 16, 2001Date of Patent: January 14, 2003Assignee: Neurotech S.A.Inventors: Weng Tao, Shou Wong, William F. Hickey, Joseph P. Hammang, E. Edward Baetge
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Patent number: 6506892Abstract: A novel immunoregulatory factor, designated IL-X, is described which has been isolated from Mycoplasma. The subject invention also concerns polynucleotides which encode IL-X. IL-X protein is a growth factor for EBV transformed human B lymphocytes and for murine helper T lymphocytes. Also taught are methods of raising antibodies to IL-X, and cloning of IL-X.Type: GrantFiled: October 29, 1998Date of Patent: January 14, 2003Inventors: Andrew C. Webb, Beverly A. Blazar
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Patent number: 6506893Abstract: The present invention pertains to polynucleotides derived from staphylococcal genes encoding resistance to streptogramin A or to streptogramin B and chemically related compounds. This invention relates to the use of polynucleotides as oligonucleotide primers or probes for detecting Staphylococcal strains that are resistant to streptogramin A or to streptogramin B and related compounds in a biological sample. The present invention is directed to the full length coding sequences of the staphylococcal genes encoding for resistance to streptogramin A or to streptogramin B from Staphylococcus and to polypeptides expressed by these full length coding sequences. This invention relates to the use of the expressed polypeptides to produce specific monoclonal or polyclonal antibodies that serve as detection means in order to characterize any staphylococcal strain carrying genes encoding resistance to streptogramin A or to streptogramin B.Type: GrantFiled: December 20, 1999Date of Patent: January 14, 2003Assignee: Institut PasteurInventors: Névine El Solh, Jeanine Allignet
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Patent number: 6506894Abstract: A process for the synthesis in solution phase of a phosphorothioate triester is provided. The process comprises the solution phase coupling of an H-phosphonate with an alcohol in the presence of a coupling agent to form an H-phosphonate diester. The H-phosphonate diester is oxidized in situ with a sulfur transfer agent to produce the phosphorothioate triester. Preferably, the H-phosphonate and alcohol are protected nucleosides or oligonucleotides. Oligonucleotide H-phosphonates which can be used in the formation of phosphorothioate triesters are also provided.Type: GrantFiled: April 26, 2000Date of Patent: January 14, 2003Assignee: Avecia LimitedInventors: Colin Bernard Reese, Quanlai Song
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Patent number: 6506895Abstract: A photoactivatable nucleic acid derivative composition in which one or more photoreactive group(s) are bound to a natural or synthetic nucleic acid. The photoreactive groups can be bound to the nucleic acid before, during or after its formation, and can thereafter be activated in order to attach the nucleic acid to another molecule, e.g., to the surface of a solid support. Also described is a method of preparing such a composition, and a method of using such a composition to attach the nucleic acid to a another molecule, such as that provided by the surface of a substrate used to prepare a nucleic acid chip by photolithographic techniques.Type: GrantFiled: February 24, 1998Date of Patent: January 14, 2003Assignee: SurModics, Inc.Inventors: Patrick E. Guire, Melvin J. Swanson, Gary W. Opperman
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Patent number: 6506896Abstract: The invention relates to a pentopyranosylnucleoside of the formula (I) or of the formula (II) their preparation and use for the production of a therapeutic, diagnostic and/or electronic component.Type: GrantFiled: July 11, 2000Date of Patent: January 14, 2003Assignee: Nanogen Recognomics GmbHInventors: Christian Miculka, Norbert Windhab, Tilmann Brandstetter, Gerhard Burdinski
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Patent number: 6506897Abstract: The invention relates to a method of preparing crystalline L-arabinose by extraction of sugar beet pulp, from which sugar has been extracted, in a strong alkaline solution, by hydrolysis of the obtained crude araban with a strong acid at an elevated temperature, by neutralization and filtration of the obtained solution, by chromatographic separation of the L-arabinose fraction, by purification of the obtained L-arabinose solution by means of cation and anion exchangers and adsorbent resins, and by recovering the pure L-arabinose as a crystalline product.Type: GrantFiled: October 30, 2000Date of Patent: January 14, 2003Assignee: Danisco Finland OyInventors: Juhani Antila, Vili Ravanko, Pertti Walliander
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Patent number: 6506898Abstract: Provided is a process for preparing an at least bis-carbamate functional 1,3,5-triazine by contacting an at least diamino-1,3,5-triazine, an acyclic organic carbonate and a base, as well as certain novel compositions producible thereby. Also provided are substantially halogen contamination free crosslinker compositions comprising the products obtainable by the process, and curable compositions based upon these crosslinkers.Type: GrantFiled: May 25, 1995Date of Patent: January 14, 2003Assignee: Cytec Technology Corp.Inventors: Lawrence A. Flood, Ram B. Gupta, Revathi Iyengar, David A. Ley, Vankatarao K. Pai
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Patent number: 6506899Abstract: Pigment dispersants prepared by reacting an isocyanate oligomer having an average functionality of at least three with a polyester or polyacrylate, a poly(ethylene glycol)alkyl ether, and a diamine having a primary amine and a tertiary amine have excellent stabilizing properties and offer a wide formulation latitude with a variety of solvent systems, including polar solvents and water, and are particularly useful as pigment dispersants for paints and coating applications.Type: GrantFiled: August 9, 1999Date of Patent: January 14, 2003Assignee: E. I. du Pont de Nemours and CompanyInventor: John A. Simms
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Patent number: 6506900Abstract: The invention relates to a new process for preparing a scopine ester useful as an intermediate in preparing (1&agr;,2&bgr;,4&bgr;,5&agr;,7&bgr;)-7-[(hydroxydi-2-thienylacetyl)oxy]-9,9-dimethyl-3-oxa-9-azoniatricyclo[3.3.1.02,4] nonane-bromide.Type: GrantFiled: August 19, 2002Date of Patent: January 14, 2003Assignee: Boehringer Ingelheim Pharma AGInventors: Rolf Banholzer, Manfred Graulich, Sven Luettke, Andreas Mathes, Helmut Meissner, Peter Specht, Wolfgang Broeder
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Patent number: 6506901Abstract: This invention provides compounds of Formula I having the structure wherein A, B, Z, R and R1 are as defined hereinbefore, or a pharmaceutically acceptable salt thereof, which are useful in treating or inhibiting metabolic disorders related to insulin resistance or hyperglycemia (typically associated with obesity or glucose intolerance), atherosclerosis, gastrointestinal disorders, neurogenetic inflammation, glaucoma, ocular hypertension and frequent urination; and are particularly useful in the treatment or inhibition of type II diabetes.Type: GrantFiled: July 12, 2001Date of Patent: January 14, 2003Assignee: WyethInventors: Robert John Steffan, Mark Anthony Ashwell, Jeffrey Claude Pelletier, William Ronald Solvibile, Edward Martin Matelan
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Patent number: 6506902Abstract: Provided is a method of synthesizing a compound of formula I, comprising: (a) reacting a compound of formula II wherein R1 and R2 are independently hydrogen, hydroxy(C1-C2)alkyl, or (C1-C2)alkyl with, a compound of formula III wherein R3, R4, and R5 are each independently of each other hydrogen, (C1-C3)alkyl, (C1-C3)alkoxy, or halogen; and X is a leaving group, in a solvent having a dielectric constant at 20° C. of at least 30 but no more than 40; and (b) obtaining the compound I.Type: GrantFiled: March 29, 2001Date of Patent: January 14, 2003Assignee: Alteon, Inc.Inventor: Dilip Wagle
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Patent number: 6506903Abstract: A process for the production of 4-thiazolylmethyl derivatives are provided. A process for the production of the compound represented by the formula (I): wherein R1 is hydrogen or halogen and Hal is halogen, which comprises reacting 4-methylthiazole with N-halosuccinimide in a solvent in the presence of a radical initiator.Type: GrantFiled: August 17, 2000Date of Patent: January 14, 2003Assignee: Shionogi & Co., Ltd.Inventors: Masaaki Uenaka, Masahiko Nagai, Naotake Kobayashi
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Patent number: 6506904Abstract: A method of preparing N,N-disubstituted 3,3′-dithiodipropionamide of formula (2) is provided. In the method, 3-mercaptopropi-onamide of formula (4) reacts with an aqueous solution of amine to prepare N-substituted-3-mercaptopropionamide of formula (3) and N-substituted-3-mercaptopropionamide reacts with an aqueous solution of hydrogen peroxide. In addition, a method of preparing substituted 3-isothiazolone is provided.Type: GrantFiled: May 21, 2002Date of Patent: January 14, 2003Assignee: SK Chemicals Co., Ltd.Inventors: Seung-Hwan Kim, Jeong-Ho Park, Jin-Man Kim, Soon-Jong Hahn, Ki-Seong Choi, Myung-Ho Cho
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Patent number: 6506905Abstract: 3-(alk-2-ynyloxy)carbonyl-5-oxazolidine carboxylic acid and its analogs having a formula and wherein R1 is hydrogen, aryl, heteroaryl, alkyl, alkenyl, alkynyl, R2 and R3 are independently selected from hydrogen, alkyl, alkenyl, alkynyl, aryl, heteroaryl, R4 is hydrogen, alkyl, alkenyl, alkynyl, aryl, substituted aryl, heteroaryl, R5 and R6 independently selected from hydrogen, alkyl, alkenyl,alkynyl, arly, heteroaryl, alkoxy, alkeyloxy, alkynyloxy, aryloxy, heteroaryloxy.Type: GrantFiled: June 1, 2001Date of Patent: January 14, 2003Assignee: Dabur India LimitedInventors: Sharma Arun Prakash, Sarkar Subrata
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Patent number: 6506906Abstract: Small molecule polyamides that specifically bind with subnanomolar affinity to any predetermined sequence in the human genome with potential use in molecular biology and human medicine are described. Further, the designed compounds which target the minor groove of B-form double helical DNA offer a general approach for the control of gene-expression. Simple rules are disclosed which provide for rational control of the DNA-binding sequence specificity of synthetic polyamides containing N-methylpyrrole and N-methylimidazole amino acids. A series of molecular templates for polyamide design are disclosed which provide for small molecules which recognize predetermined DNA sequences with affinities and specificities comparable to sequence-specific DNA-binding proteins such as transcription factors. These design rule are applied to provide a polyamide for specific targeting of a predetermined 7 base pair sequence from a conserved HIV gene promoter at subnanomolar concentration.Type: GrantFiled: October 8, 1999Date of Patent: January 14, 2003Assignee: California Institute of TechnologyInventor: Peter B. Dervan
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Patent number: 6506907Abstract: There is provided a process for the production of a N-benzyl azetidine-2-carboxylic acid alkylphenyl, or alkyl, ester which process comprises the reaction of an optionally substituted alkylphenyl, or an optionally substituted alkyl, 2-bromo-4-chlorobutyrate with an optionally substituted benzylamine, which process may be used as part of an overall process for the production of azetidine-2-carboxylic acid.Type: GrantFiled: July 14, 2000Date of Patent: January 14, 2003Assignee: AstraZeneca ABInventors: Bo Lindqvist, Peter L. Sivertsen
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Patent number: 6506908Abstract: Processes are disclosed for preparing 3-hydroxymethylcyclopentanone compounds, which are useful as intermediates in the preparation of HIV chemokine CCR-5 receptor antagonists. A process is described in which the compounds are prepared by opening the cyclopropyl ring of a (1-alkoxycarbonyl-2-oxo)-trans-bicyclo[3.1.0]hexane compound by addition of a nucleophile to the cyclopropyl ring, and then decarboxylating the resulting 2-alkoxycarbonyl-3-(Nu-methyl)-cyclopentanone (Nu=the added nucleophilic group) via base solvolysis. Also described is a process for preparing the bicyclo[3.1.0]hexane precursors by the catalyzed cyclopropanation of a suitable alpha-diazo-beta-ketoester. The preparation of the alpha-diazo-beta-ketoesters and precursors thereto are also disclosed.Type: GrantFiled: April 20, 2001Date of Patent: January 14, 2003Assignee: Merck & Co., Inc.Inventors: Nobuyoshi Yasuda, Michael Palucki, Joann M. Um, David Alan Conlon, Barry M. Trost
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Patent number: 6506909Abstract: A method of synthesizing trimethylene carbonate is disclosed involving (a) reacting 1,3-propanediol and a compound chosen from phosgene and bis-chloroformates to form a polycarbonate intermediate having the structure: wherein n is at least 2; R1 is an end group chosen from H, R3-Cl, R3-OH and —C(O)Cl, where R3 is C1-C6 linear or branched alkyl and R2 is an end group chosen from —OCH2CH2CH2Cl, —OCH2CH2CH2OH and Cl; and (b) providing a combination of temperature and pressure corresponding to vapor phase conditions for trimethylene carbonate.Type: GrantFiled: December 20, 2001Date of Patent: January 14, 2003Assignee: PPG Industries Ohio, Inc.Inventors: Mark P. Bowman, Charles B. Kreutzberger
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Patent number: 6506910Abstract: A more practical synthesis for preparing discodermolide and structurally related analogues, novel compounds useful in the process and novel compounds prepared by the process.Type: GrantFiled: August 3, 2001Date of Patent: January 14, 2003Assignee: Novartis AGInventor: Frederick Ray Kinder, Jr.
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Patent number: 6506911Abstract: A novel 3-hydroxypyridin-4-one compound of formula I is provided wherein R is hydrogen or a group that is removed by metabolism in vivo to provide the free hydroxy compound, R1 is an aliphatic hydrocarbon group or an aliphatic hydrocarbon group substituted by a hydroxy group or a carboxylic acid ester, sulpho acid ester or a C1-6 alkoxy, C6-aryloxy or C7-10aralkoxy ether thereof, R3 is selected from hydrogen and C1-6 alkyl; and R4 is selected from hydrogen, C1-6 alkyl and a group as described for R2; characterised in that R2 is selected from groups (i) —CONH—R5 (ii) —CH2NHCO—R5 (iii) —SO2NH—R5 (iv) —CH2NHSO2—R5 (v) —CR6R6OR7 (viii) —CONHCOR5 wherein R5 is selected from hydrogen and optionally hydroxy, alkoxy, or aralkoxy substituted C1-3 alkyl, aryl and C7-13 aralkyl, R6 is independently selected from hydrogen, C1-13 alkyl, aryl and C7-13 aralkyl, and R7 is selected from hydrogen, C1-13 alkyl, aryl and C7Type: GrantFiled: September 4, 2001Date of Patent: January 14, 2003Assignee: BTG International LimitedInventors: Robert Charles Hider, Gary Stuart Tilbrook, Zudong Liu
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Patent number: 6506912Abstract: A method of modifying or altering the structured a 1&agr;-hydroxylated vitamin D compound to increase its biological activity by altering the conformational equilibrium of the A-ring to favor a chair conformation that presents the 1&agr;-hydroxyl in the axial orientation. This is accomplished by either locking the A-ring chair conformation in a geometry having an axially orientated 1&agr;-hydroxyl, or by the addition of one or more substituents to the A-ring which interact with other substituents in the molecule or on the A-ring to provide a driving force to the A-ring to adopt a chair conformation which presents the 1&agr;-hydroxyl in the axial orientation.Type: GrantFiled: October 31, 2001Date of Patent: January 14, 2003Assignee: Wisconsin Alumni Research FoundationInventors: Hector F. DeLuca, Rafal R. Sicinski
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Patent number: 6506913Abstract: A dimethylfurancarboxyanilide compound of the formula (I): wherein R1 and R2 are the same or different and each is hydrogen, (C2-C6)-alkyl, (C3-C6)-cycloalkyl, (C3-C6)-alkenyl, (C2-C6) alkynyl, (C1-C3)-halogenoalkyl, (C2-C6)-alkoxy, (C1-C6)-alkoxy-(C1-C6)-alkyl, cyano, substituted amide, (C1-C6)-alkoxy-carbonyl, benzoyl which is unsubstituted or has 1 to 2 substituents, benzoylamino which is unsubstituted or has 1 to 2 substituents; (C2-C6)-alkanoylamino, (C3-C6)-cycloalkylcarbonylamino, benzyl which is unsubstituted or has 1 to 2 substituents, phenyl which is unsubstituted or has 1 to 2 substituents, or (C1-C6)-alkoxycarbonyl-(C2-C5)-alkenylene; and R1 and R2 do not both represent hydrogen at the same time. A wood preservative containing the dimethylfurancarboxyanilide compound as an active ingredient. A method of preserving wood by applying the dimethylfurancarboxyanilide compound to wood.Type: GrantFiled: October 24, 2001Date of Patent: January 14, 2003Assignee: Sankyo Company, LimitedInventors: Kiyoshi Konishi, Toshiaki Yanai, Akio Saito
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Patent number: 6506914Abstract: A process for producing an oxirane compound by reacting an olefin with hydroperoxides in the presence of a catalyst wherein said catalyst is obtained by gelling a silicon compound of the following formula (1) (silicon compound (1)), a silicon compound of the following formula (2) (silicon compound (2)) and a titanium compound in water, alcohol solvent or mixed solvent of water and alcohol, removing a solvent in the resulted gel by extraction with supercritical fluid, then, performing drying and silylation treatment: Si(OR1)4 (1) (R2)mSi(OR3)4−m (2) (R1, R2 and R3 independently represent a hydrocarbon group having 1 to 20 carbon atoms. m represents an integer of 1 or 2.Type: GrantFiled: May 31, 2002Date of Patent: January 14, 2003Assignee: Sumitomo Chemical Company, LimitedInventors: Junpei Tsuji, Carsten Stocker
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Patent number: 6506915Abstract: Processes for the stereospecific synthesis of coenzyme Q10, ubiquinone, are disclosed; a total synthetic procedure using geraniol as the starting material. The process of the invention results in high yields of isometrically pure ubiquinone. The synthetic coenzyme Q10 can be used as an antioxidant, a nutritional supplement and as a pharmaceutical in treating many conditions.Type: GrantFiled: June 14, 2001Date of Patent: January 14, 2003Inventor: Daniel David West