Abstract: The present invention relates to an apparatus for preparing polynucleotides on a solid support in a reactor comprising a column containing an immobilized solid support that is functionalized for polynucleotide synthesis. The solid support can be porous, and can be functionalized with a nucleoside or with a universal synthesis of polynucleotides.
Abstract: The invention provides methods for purifying carbohydrates, including oligosaccharides, nucleotide sugars, and related compounds, by use of ultrafiltration, nanofiltration and/or reverse osmosis. The carbohydrates are purified away from undesired contaminants such as compounds present in reaction mixtures following enzymatic synthesis or degradation of oligosaccharides.
Abstract: Probes labeled with 1,2-dioxetane precursors can be employed in a variety of assays. The probes may be nucleic acid, peptide nucleic acid, proteins including enzyme, antibody or antigen, steroid, carbohydrate, drug or non-drug hapten. The probe is provided with a 1,2-dioxetane precursor bound thereto, generally either covalently, or a strong ligand bond. The dioxetane precursor moiety is converted to a bound 1,2-dioxetane by exposure to singlet oxygen. These dioxetane (labels) either spontaneously decompose, or are induced to decompose by an appropriate trigger to release light. The trigger may be a change in pH temperature, or an agent which removes a protective group. Assay formats in which these 1,2-dioxetane labeled probes and referents may be used to include hybridization assays, immuno assays, gel-based assays and Capillary Zone Electrophoresis.
Abstract: The invention relates to compounds of the formula (I)
in which
R represents a radical
(CH2)mOn(X)YAr
in which m represents the number 0 or 1,
n represents the number 0 or 1,
X represents a radical (NH)a, CH2 or SO2, where a represents the number 0 or 1,
Y represents a radical (CH2)b—(CH═CH)c—(CH2)d, where c=0 or 1 and b+c+d ≦8,
Z represents a hydrogen or halogen atom,
Ar represents an optionally substituted aryl or heteroaryl radical and
W represents a hydrogen atom or an acyl radical, and their acid addition salts.
The compounds of the formula (1) have antibiotic properties.
Abstract: Aureobacterium barkerei strain KDO-37-2 (ATCC 49977) and KDO aldolase (EC 4.1.2.23) isolated therefrom are disclosed. The KDO aldolase is further disclosed to have a broad substrate specificity with respect to its reverse reaction, i.e. the condensation of aldoses with pyruvate to form a wide range of 2-keto-3-deoxy-onic acids, including 2-keto-3-deoxy-nonulosonic acid, 2-keto-3-deoxy-octulosonic acid, 2-keto-3-deoxy-heptulosonic acid, and 2-keto-3-deoxy-hexulosonic acid. In particular, 3-deoxy-D-manno-2-octulosonic acid (D-KDO), a vital component of lipopolysaccharides found in the bacterial outer membrane may be synthesized from D-arabinose and pyruvate in 67% yield. Additionally, protected forms of the KDO aldolase products, e.g. hexaacetyl 2-keto-3-deoxy-nonulosonic acid and pentaacetyl 2-keto-3-deoxy-octulosonic acid, may be decarboxylated to form the corresponding 2-deoxy-aldoses, e.g. 2-deoxy-octulose and 2-deoxy-heptulose respectively.
Abstract: The invention relates to a process for producing mixtures selectively enriched with either 1,1-GPM and 1,6-GPS from hydrogenated isomaltulose. The process involves dissolving hydrogenated isomaltulose at an elevated temperature, and subjecting the resulting solution to one or more cooling steps, wherein each cooling step utilizes a predetermined cooling rate over a predetermined temperature range.
Type:
Grant
Filed:
February 4, 1998
Date of Patent:
July 2, 2002
Assignee:
Sudzucker Aktiengesellschaft
Inventors:
Hanspeter Degelmann, Michael Gander, Jörg Kowalczyk, Markwart Kunz, Mohammad Munir, Matthias Schüttenhelm, Wolfgang Wach
Abstract: A combination of an agent which is a substrate for multidrug resistance related protein (MRP) and an inhibitor of MRP which is a nonsteroidal anti-inflammatory drug (NSAID) or a structural analogue thereof for simultaneous, sequential or separate use for increasing the potency of the substrate. The substrates include anti-cancer drugs and transition metal complexes. The combinations can be used to overcome the resistance to MRP substrates exhibited in many conditions, such as resistance to chemotherapy where patients have developed resistance, especially as a result of MRP over-expression to their chemotherapy.
Type:
Grant
Filed:
April 29, 1999
Date of Patent:
July 2, 2002
Assignee:
Dublin City University and Enterprise Ireland
Abstract: Compositions comprising a polysaccharide and a hydroxy-functional polyester are prepared by mixing the hydroxy-functional polyester and polysaccharide, modified polysaccharide or a naturally-occurring fiber or particulate filler and, optionally, other additives in a intensive mixer at a temperature and for a time sufficient to provide an intimate, well-dispersed mixture of the components.
Abstract: The present invention relates to evenly substituted polysaccharide derivatives having the general structure:
polysaccharide—O—R
wherein polysaccharide—O represents a substituted or unsubstituted polysaccharide unit and R is a substituent of a polysaccharide-OH group having either the structure
R=—A—B—
or the structure
R=—B—,
wherein A is a linear polyether chain having the following structure:
A=(—D—O—)n
wherein D denotes a linear aliphatic branched or unbranched chain having 2 to 12 C atoms, O represents an oxygen atom and n is a number equal to or greater than 1, and
B represents a substituted carbamic acid having the structure
wherein E denotes a linear or branched aliphatic chain having 1 to 18 C atoms.
Type:
Grant
Filed:
April 2, 1997
Date of Patent:
June 11, 2002
Assignee:
Wolff Walsrode AG
Inventors:
Jürgen Engelhardt, Joachim Simon, Hanns-Peter Müller, Rainhard Koch, Dirk-Jacques Dijkstra
Abstract: Methods for the regioselective alkylation at the 2′-hydroxy position over the 3′-hydroxy position of nucleosides and nucleoside analogs, forming 2′-O-ester modified compounds, are disclosed. Reduction and derivatization of the 2′-O-ester provides 2′-O-modified nucleosides and nucleoside analogs useful for the synthesis of oligomeric compounds having improved hybridization affinity and nuclease resistance.
Type:
Grant
Filed:
January 8, 1999
Date of Patent:
June 11, 2002
Assignee:
ISIS Pharmaceuticals, Inc.
Inventors:
Andrew M. Kawasaki, Allister S. Fraser, Muthiah Manoharan, P. Dan Cook, Thazha P. Prakash
Abstract: Heavily fluorinated sugar analogs of formula
wherein
R1 is selected from alkyl, alkenyl, aryl, —CH2—O-alkyl, —CH2—O-aryl, —CH2OPO3H, —CH2—O-carbohydrate, —CH2—NH-peptide, or —CH2—O-peptide;
wherein R2 is selected from hydroxy, —O-carbohydrate, —NH-peptide,
wherein
R3 is selected from H, halogen, lower alkyl, lower alkenyl, lower haloalkyl, lower haloalkenyl, amino, mono- or di-lower alkylamino;
wherein R4 is selected from amino, hydroxy, alkoxy, or halogen; and
wherein R5 is H or amino. The compounds of formula (I) are useful as antiviral and antineoplastic agents and the compounds of formula (II) are useful as plant growth inhibitors and herbicides.
Type:
Grant
Filed:
September 2, 1999
Date of Patent:
May 21, 2002
Assignee:
Board of Regents University of Nebraska-Lincoln
Abstract: Disclosed are derivatized malto-oligosaccharides and methods for the preparation thereof. In accordance with the disclosed invention, a malto-oligosaccharide is hydrogenated to thereby obtain a hydrogenated malto-oligosaccharide, and the resulting hydrogenated malto-oligosaccharide is derivatized, such as via oxidation, esterification, etherification, or enzymatic modification. The derivatization of such hydrogenated malto-oligosaccharides results in a surprisingly low level of a formation of by-products and products of degradation. In a particularly preferred embodiment of the invention, a mixture of malto-oligosaccharides is catalytically hydrogenated under reaction conditions suitable to substantially preserve the degree of polymerization (DP) profile of the mixture. The resulting malto-oligosaccharide mixture then is derivatized to form a derivatized malto-oligosaccharide mixture.
Abstract: The present invention concerns new phospholipid derivatives of nucleosides of the general formula (I) in which R1 represents a straight-chained or branched, saturated or unsaturated aliphatic residue with 9-14 carbon atoms which can optionally be substituted once or several times; R2 can represent a straight-chained or branched, saturated or unsaturated aliphatic residue with 8-12 carbon atoms which can optionally be substituted once or several times; m is 2 or 3; A can represent a methylene group or an oxygen; Nuc can be a nucleoside or a residue derived from a nucleoside derivative; and tautomers thereof and their physiologically tolerated salts of inorganic and organic acids and bases as well as pharmaceutical preparations containing these compounds.
Abstract: The invention provides a novel silicon-containing compound having an oxidation potential of 0.3 to 1.5 V on the basis of a standard hydrogen electrode, wherein at least one alkoxy group is bonded to a silicon atom and at least one aromatic amine group is also bonded to the silicon atom.
An organic electroluminescence device having excellent mechanical and electric contact between an electrode and an organic layer is also provided by treating the surface of an anode with using a surface-treating agent comprising the above silicon-containing compound.
Abstract: The present invention pertains to novel inhibitors of DNA glycosylases. The invention is based at least in part on the observation that specific substituted pyrrolidines, and analogs thereof, are capable of specifically inhibiting DNA glycosylases, e.g., as transition state analogs, and consequently are useful for modulation of DNA repair. Such compounds can, for example, be used for treating subjects having a disorder associated with excessive cell proliferation, such as in the treatment of various cancers. Furthermore, these glycosylase inhibitors can be used as anti-bacterial, anti-viral and anti-fungal agents.
Type:
Grant
Filed:
March 7, 1997
Date of Patent:
April 9, 2002
Assignee:
President and Fellows of Harvard College
Abstract: Provided are products including trihydroxystilbenes and glycosylated derivatives thereof. Also provided are compositions containing these products with an aqueous solvent, particularly and alcohol-water mixture, and reverse phase chromatographic methods for isolating and purifying the compositions from plant materials. The products have biological activity, including anti-tumor activity.
Type:
Grant
Filed:
December 21, 1998
Date of Patent:
March 26, 2002
Assignee:
Pure World Botanicals, Inc.
Inventors:
Bo Lin Zheng, Calvin Hyungchan Kim, Kan He, Qun Yi Zheng
Abstract: A process for deprotecting RNA alkylsilyl groups comprising, contacting the groups with a solution of anhydrous triethylamine-hydrogen fluoride (aHF-TEA) in triethylamine and N-methylpyrrolidine at between 60° C.-70° C. for 0.25-24 h.
Abstract: A subject of the invention is the compounds of formula (I):
R1=H, OH, alkyl, alkenyl or alkynyl optionally substituted or alkoxy,
R2=H, Hal,
R3=H, alkyl, Hal,
Rg and Rh: H, alkyl, aryl heterocycle,
R5=H or O-alkyl,
R6=alkyl or CH2—O-alkyl,
R7=H or alkyl.
The compounds of formula (I) have antibiotic properties.
Type:
Grant
Filed:
December 21, 1998
Date of Patent:
February 26, 2002
Assignee:
Aventis Pharma S.A.
Inventors:
Michel Klich, Patrick Laurin, Branislav Musicki, Laurent Schio
Abstract: Improved methods for the simultaneous production of dihydroxybenzene and dicarbinol from diisopropylbenzene are provided. These methods provide for continuous and simultaneous production of diisopropylbenzene dihydroperoxide (DHP) and diisopropylbenzene hydroxyhydroperoxide (HHP) using Karr Column extractors operated in series. A very high purity DHP-containing solution, the precursor to the dihydroxybenzene, can be produced according to the reported methods. A safe and efficient method for producing dicarbinol from HHP is also disclosed.
Type:
Grant
Filed:
February 24, 1998
Date of Patent:
February 26, 2002
Assignee:
Indspec Chemical Corporation
Inventors:
Raj B. Durairaj, Vaughn J. Romell, Michael N. Tackie, Thomas K. Volek
Abstract: This invention provides a method of killing tumor cells or microorganisms which comprises contacting the tumor cells or the microorganisms with an amount of nicotinamide adenine dinucleotide (NAD) or its analogs effective to increase clonogenic toxicity of cells. This invention also provides a method of killing tumor cells or microoganisms in a subject which comprises administering an amount of nicotinamide adenine dinucleotide or its analogs effective to increase clonogenic toxicity of cells to the subject.