Boron, Phosphorus, Heavy Metal Or Aluminum Containing Patents (Class 536/17.1)
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Publication number: 20100221269Abstract: The invention provides functionalized monosaccharides and disaccharides suitable for use in synthesizing a lipid A derivative, as well as methods for synthesizing and using a synthetic lipid A derivative.Type: ApplicationFiled: September 5, 2008Publication date: September 2, 2010Applicant: UNIVERSITY OF GEORGIA RESEACH FOUNDATION, INCInventor: Geert-Jan Boons
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Publication number: 20100152429Abstract: Disclosed are a sodium salt represented by the average formula (I) below, and a method for producing such a sodium salt. (In the formula, m1, n1, m2 and n2 independently represent 0 or a positive number not greater than 2, while satisfying m1+n1=2, m2+n2=2, 0<m1+m2<4 and 0<n1+n2<4.) Also disclosed is a decomposition suppression method which makes a sodium salt represented by average formula (I) coexist with a sodium salt represented by the general formula (IV) below. This method enables improvement of long-term stability of a sodium salt represented by general formula (IV).Type: ApplicationFiled: November 21, 2007Publication date: June 17, 2010Applicant: Eisai R&D Management Co., Ltd.Inventors: Shin Sakurai, Ken Furukawa, Kimihiro Matsuo, Kenichi Tagami
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Publication number: 20100093654Abstract: Tetrasubstituted glucopyranosylated benzene derivatives of general formula (I) as defined according to claim 1, including the tautomers, the stereoisomers thereof, the mixtures thereof and the salts thereof. The compounds according to the invention are suitable for the treatment of metabolic disorders.Type: ApplicationFiled: February 20, 2008Publication date: April 15, 2010Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Frank Himmelsbach, Matthias Eckhardt, Peter Eickelmann, Leo Thomas
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Publication number: 20100076183Abstract: A nucleoside monomer that is protected by a thionocarbamate protecting group is provided, as well as a method for making a polynucleotide that uses the same. Also provided is a polynucleotide synthesis method that employs a diamine to deprotect a protected polynucleotide.Type: ApplicationFiled: May 14, 2009Publication date: March 25, 2010Inventors: Douglas J. Dellinger, Joel Myerson, Agnieszka Sierzchala, Geraldine F. Dellinger, Zoltan Timar
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Publication number: 20100075321Abstract: A labeled compound is so designed that an aromatic tertiary amine compound is bondable with a biomolecule. One of S1 and S2 contains a group bound with a molecular chain 10 (e.g. an oligonucleotide) capable of binding with a biomolecule or a reactive group covalently binding with a reactive group present in the biomolecule, n is 0 or 1, R3 is a phenyl group or a naphthyl group, Ar1 is a phenylene group or a naphthylene group, and Ar2 is any of a phenylene group, a naphthylene group, an anthrylene group, and a phenanthrene group. The detection of a fluorescence emitted by excitation of the labeled compound bound to a biomolecule ensures the biomolecule being detected at high sensitivity and a high SN ratio.Type: ApplicationFiled: August 21, 2009Publication date: March 25, 2010Applicant: SONY CORPORATIONInventor: Mari Ichimura
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Publication number: 20100069312Abstract: The invention provides prophylactic and therapeutic applications of select aminoalkyl glucosamine phosphate (AGP) compounds in autoimmune diseases.Type: ApplicationFiled: April 18, 2008Publication date: March 18, 2010Applicant: Universite Libre de BruxellesInventors: Stanislas Goriely, Dominique De Wit, Michel Goldman, Sophie Detienne, Jean-Marc Brulet
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Publication number: 20100048492Abstract: The present invention relates to a pharmaceutical composition comprising at least one compound of formula (I): or one of its pharmaceutically acceptable salts in which R1, R2 and R3 are independently a hydrogen or an R7—CO— group where R7 is an alkyl, alkene or alkyne group, linear, branched or cyclic, comprising 2 to 24 carbon atoms; R4 is a hydrogen atom or a mannosyl group substituted in position 6 by an R6 residue chosen from the group comprising a hydrogen atom and an R7—CO— group; and R5 is chosen from the group comprising a hydrogen atom, a mono-, di-, tri-, tetra- and penta-mannosyl; and the use of such a composition for manufacturing a medication intended for the prevention or treatment of an illness associated with the over-expression of TNF and/or IL-12 in a subject.Type: ApplicationFiled: November 20, 2007Publication date: February 25, 2010Inventors: Valérie Quesniaux Ryffel, Germain Puzo, Jérôme Nigou, Martine Gilleron
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Publication number: 20100009902Abstract: The present invention provides conjugates between a substrate, e.g., peptide, glycopeptide, lipid, etc., and a modified saccharyl fragment bearing a modifying group such as a water-soluble polymer, therapeutic moiety or a biomolecule. The conjugates are linked via the enzymatic conversion of the activated modified saccharyl fragment into a glycosyl linking group that is interposed between and covalently attached to the substrate and the modifying group. The conjugates are formed from substrates by the action of a sugar transferring enzyme, e.g., a glycosyltransferase. For example, when the substrate is a peptide, the enzyme conjugates a modified saccharyl fragment moiety onto either an amino acid or glycosyl residue of the peptide. Also provided are pharmaceutical formulations that include the conjugates. Methods for preparing the conjugates are also within the scope of the invention.Type: ApplicationFiled: January 6, 2006Publication date: January 14, 2010Applicant: NEOSE TECHNOLOGIES, INC.Inventor: Shawn DeFrees
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Patent number: 7635762Abstract: The present invention provides luminescent metal ion complexes for use in a wide range of biological and chemical studies. The luminescent metal ion complexes of the invention comprise a metal ion chelating component covalently bound to a carrier molecule. Also provided are methods of making and using the luminescent metal ion complexes.Type: GrantFiled: October 21, 2003Date of Patent: December 22, 2009Assignee: Biosearch Technologies, Inc.Inventors: Ronald M. Cook, Matt Lyttle, Mary Katherine Johansson
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Publication number: 20090312531Abstract: One aspect of the present invention relates to a double-stranded oligonucleotide comprising at least one ligand tethered to an altered or non-natural nucleobase. In certain embodiments, the non-natural nucleobase is difluorotolyl, nitropyrrolyl, or nitroimidazolyl. In certain embodiments, the ligand is a steroid or aromatic compound. In certain embodiments, only one of the two oligonucleotide strands comprising the double-stranded oligonucleotide contains a ligand tethered to an altered or non-natural nucleobase. In certain embodiments, both of the oligonucleotide strands comprising the double-stranded oligonucleotide independently contain a ligand tethered to an altered or non-natural nucleobase. In certain embodiments, the oligonucleotide strands comprise at least one modified sugar moiety. Another aspect of the present invention relates to a single-stranded oligonucleotide comprising at least one ligand tethered to an altered or non-natural nucleobase.Type: ApplicationFiled: July 31, 2009Publication date: December 17, 2009Applicant: ALNYLAM PHARMACEUTICALS, INC.Inventors: Muthiah MANOHARAN, Kallanthottathil G. RAJEEV, Jie XIA
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Publication number: 20090285844Abstract: A method is provided for identifying, isolating, and producing htrB mutants of gram-negative bacterial pathogens. The method comprises mutating the htrB gene of a gram-negative bacterial pathogen so that there is a lack of a functional htrB protein, resulting in a mutant that lacks one or more secondary acyl chains contained in the wild type gram-negative bacterial pathogen, and displays substantially reduced toxicity as compared to the wild type strain. Also, the present invention provides methods for using a vaccine formulation containing the htrB mutant, the endotoxin isolated therefrom, or the endotoxin isolated therefrom which is then conjugated to a carrier protein, to immunize an individual against infections caused by gram-negative bacterial pathogens by administering a prophylactically effective amount of the vaccine formulation.Type: ApplicationFiled: March 30, 2009Publication date: November 19, 2009Inventors: Michael A. Apicella, Melvin G. Sunshine, Na-Gyong Lee, Rasappa Arumugham, Bradford W. Gibson
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Publication number: 20090270339Abstract: A lyophilized unit dose form containing about 2 g of glufosfamide is useful in treatment of cancer and other hyper-proliferative diseases.Type: ApplicationFiled: June 4, 2007Publication date: October 29, 2009Inventor: Mike Li
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Patent number: 7605136Abstract: Conjugates of epothilones and epothilone derivatives (as effectors) with suitable saccharides or saccharide derivatives (as recognition units) are described. Their production is carried out by the recognition units being reacted with suitable linkers, and the compounds that are produced are conjugated to the effectors. The pharmaceutical use of the conjugates for treating proliferative or angiogenesis-associated processes is described.Type: GrantFiled: December 5, 2003Date of Patent: October 20, 2009Assignee: Bayer Schering Pharma AGInventors: Klaus Bosslet, Holger Hess-Stumpp, Jens Hoffmann, Ulrich Klar, Andrea Rotgeri
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Publication number: 20090239814Abstract: The present invention provides iRNA agents comprising at least one subunit of the formula (I): wherein: A and B are each independently for each occurrence O, N(RN) or S; X and Y are each independently for each occurrence H, OH, a hydroxyl protecting group, a phosphate group, a phosphodiester group, an activated phosphate group, an activated phosphite group, a phosphoramidite, a solid support, —P(Z?)(Z?)O-nucleoside, —P(Z?)(Z?)O-oligonucleotide, a lipid, a PEG, a steroid, a lipophile, a polymer, —P(Z?)(Z?)O-Linker-OP(Z??)(Z??)O-oligonucleotide, a nucleotide, an oligonucleotide, —P(Z?)(Z?)-formula (I), —P(Z?)(Z?)— or -Linker-R; R is LG, -Linker-LG, or has the structure shown below: LG is independently for each occurrence a carbohydrate, e.g.Type: ApplicationFiled: December 4, 2008Publication date: September 24, 2009Applicant: ALNYLAM PHARMACEUTICALS, INC.Inventors: Muthiah Manoharan, Kallanthottathil G. Rajeev, Jayaprakash K. Narayanannair, Martin Maier
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Publication number: 20090206245Abstract: It is an object of the present invention to provide a novel mass spectrometry method which overcomes the conventional problems mentioned above, which can analyze at a high sensitivity and high accuracy a chemical reaction on a surface of a self-organized membrane bound to a metal, and which can be applied to analysis of structures of a sugar chain in future. According to the present invention, a method for performing mass spectrometry of sulfur atom-containing derivatives of an organic residue, characterized in that the method includes ionizing a metal-organic residue complex into the derivatives, wherein the complex has the organic residue bound through a sulfur atom to the metal is provided, thereby solving the above problems.Type: ApplicationFiled: March 29, 2005Publication date: August 20, 2009Applicant: Shionogi CO., LtdInventors: Noriko Nagahori, Kenichi Niikura, Shinichiro Nishimura
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Patent number: 7547755Abstract: A (co)polycarbonate the molecular structure of which contains units derived from bisphenols conforming to formulae (1a1) and (1b1) in which R1 independently of one another represents hydrogen or a C1-C10-alkyl and R2 represents C1-C10-alkyl, or phenyl or benzyl in each case unsubstituted or substituted by at least one member selected from the group consisting of hydrogen and C1-C10-alkyl radical. The (co)polycarbonate exhibits relatively high glass transition temperature and improved adhesion to metals.Type: GrantFiled: September 24, 2007Date of Patent: June 16, 2009Assignee: Bayer Material Science AGInventor: Helmut-Werner Heuer
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Publication number: 20090130717Abstract: A microorganism represented by a strain K04-0144 belonging to Streptomyces sp. having ability to produce K04-0144 substance is cultured in the medium, and the isolated K04-0144A substance, K04-0144B substance and K04-0144C substance therefrom have strong antibacterial activities against Gram-positive bacteria including methicillin-resistant Streptococcus aureus (MRSA), consequently these are useful as the therapeutic agents for infectious disease caused by MRSA as well as infectious diseases caused by multidrug including ?-lactam antibiotics resistant bacteria. Further, similarly, since the novel K04-0144D substance isolated from the cultured liquid has the action for enhancing the effect of ?-lactam antibiotics, which are utilized as the antibacterial agents, in combination with them, it is useful as the therapeutic agent for infectious diseases caused by methicillin-resistant Staphylococcus aureus (MRSA) and multidrug including ?-lactam antibiotics resistant bacteria.Type: ApplicationFiled: May 16, 2006Publication date: May 21, 2009Inventors: Satoshi Omura, Hiroshi Tomoda, Yong-pil Kim, Hideaki Hanaki, Atsuko Matsumoto, Yoko Takahashi
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Publication number: 20090062214Abstract: A compound having excellent macrophage activity inhibitory action, which is represented by the general following formula: wherein Q represents an oxygen atom, a C1-C3 alkylene group, a —O-Alk- group or a —O-Alk-O— group (in which Alk is a C1-C3 alkylene group), R1 represents a C1-C20 alkanoyl group which may be substituted, a C3-C20 alkenoyl group which may be substituted or a C3-C20 alkynoyl group which may be substituted, R2, R3 and R4, which may be the same or different, represent a hydrogen atom, a C1-C20 alkyl group which may be substituted, a C2-C20 alkenyl group which may be substituted, a C2-C20 alkynyl group which may be substituted, a C1-C20 alkanoyl group which may be substituted, a C3-C20 alkenoyl group which may be substituted or a C3-C20 alkynoyl group which may be substituted, R5 represents a hydrogen atom, a halogen atom, a hydroxyl group, a C1-C6 alkoxy group which may be substituted, a C2-C6 alkenyloxy group which may be substituted or a C2-C6 alkynyloxy group which may be substitutedType: ApplicationFiled: January 7, 2005Publication date: March 5, 2009Inventors: Masao Shiozaki, Takaichi Shimozato
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Publication number: 20090054353Abstract: The present invention relates, as medicaments, to the ?-D-mannopyranosyl-1 phosphate derivatives of formulae I, II and III: (where each group R11 to R14, R21 to R24, R31 to R34 is H or an OH-protective group, and R and R? are defined as indicated in the description), which can be used as cellular sources of Man-1 P, against the CDG-I syndrome and in particular the CDG-Ia syndrome. The invention also relates to these derivatives as industrial products and to their method of preparation.Type: ApplicationFiled: February 27, 2007Publication date: February 26, 2009Inventors: Christine Gravier-Pelletier, Renaud Hardre, Amira Khaled, Yves Le Merrer
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Publication number: 20080312424Abstract: The invention provides methods and compositions for the rapid and sensitive detection of post-translationally modified proteins, and particularly of those with post-translational glycosylations. The methods can be used to detect O-GlcNAc posttranslational modifications on proteins on which such modifications were undetectable using other techniques. In one embodiment, the method exploits the ability of an engineered mutant of ?-1,4-galactosyltransferase to selectively transfer an unnatural ketone functionality onto O-GlcNAc glycosylated proteins. Once transferred, the ketone moiety serves as a versatile handle for the attachment of biotin, thereby enabling detection of the modified protein. The approach permits the rapid visualization of proteins that are at the limits of detection using traditional methods. Further, the preferred embodiments can be used for detection of certain disease states, such as cancer, Alzheimer's disease, neurodegeneration, cardiovascular disease, and diabetes.Type: ApplicationFiled: June 15, 2007Publication date: December 18, 2008Applicant: INVITROGEN CORPORATIONInventors: Linda Hseih-Wilson, Nelly Khidekel, Hwan-Ching Tai, Sabine Arndt
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Publication number: 20080249037Abstract: The present invention is directed to synthetic molecules having biological activity similar to PIM (acyl glycerol phosphatidylinositol manno-oligosacccharide) activity, for use in the treatment and prevention of inflammatory or immune cell mediated diseases or disorders.Type: ApplicationFiled: November 18, 2004Publication date: October 9, 2008Inventors: Gurmit Singh-Gill, David Samuel Larsen, Jeremy David Jones, Wayne Bruce Severn, Jacquie Lucille Harper, Gavin Painter
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Publication number: 20080194494Abstract: The invention relates to a chemical genus of 4-biarylyl-1-phenylazetidin-2-ones useful for the treatment of hypercholesterolemia and other disorders, having general formula: Pharmaceutical compositions and methods for treating cholesterol- and lipid-associated diseases are also disclosed.Type: ApplicationFiled: April 26, 2006Publication date: August 14, 2008Applicant: MICROBIA, INC.Inventors: Eduardo J. Martinez, John Jeffrey Talley, Regina Lundrigan
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Publication number: 20080177049Abstract: In preparing a glycoside compound from (a) a furanose compound or pyranose compound, and (b) an alcohol compound, a process for preparing a glycoside compound in which glycosidic bond locates selectively trans form relative to C-2 hydroxyl group, the process comprising using a furanose compound wherein the hydroxyl at the 2-position may have a substituent protected with a group A, or a pyranose compound which may have a substituent wherein R2 and R3 are the same or different and are each alkyl having 1 to 4 carbon atoms or aryl having or not having a substituent, or R2 and R3 are combined to form alkylene having 2 to 4 carbon atoms (the alkylene may be substituted with alkyl having 1 to 4 carbon atoms, or may have intervening phenylene), and m and n are each an integer of 0 or 1.Type: ApplicationFiled: February 20, 2006Publication date: July 24, 2008Inventor: Shigeru Yamago
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Publication number: 20080076833Abstract: The present invention relates to phosphorylated polyphenols, preferably tannins that, unlike their unphosphorylated counterparts, do not suffer from relatively low stability, resulting in an activity that is relatively short in time, and/or that do not result in yellowing of materials therewith such as textiles or polymers. The present invention further relates to a simple, cheap and environmentally friendly way of preparing these compounds. The phosphorylation process of the invention can be extended to simple phenolic compounds as well, as long as these have at least one accessible hydroxyl group. The phosphorylated compounds according to the invention can be used as antioxidants, as radical scavengers, as complexating agents for metals and proteins, as antibacterials or antiallergenic compounds, and as agents to flock textile.Type: ApplicationFiled: September 14, 2004Publication date: March 27, 2008Applicant: AJINOMOTO OMNICHEM S.A.Inventors: Willy Van Brussel, Geert Schelkens, Patrick Ricquier
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Publication number: 20070293445Abstract: Stable solid, crystalline forms of elsamitrucin salts are provided that are useful in preparing anti-neoplastic parenteral formulations. Also provided are methods for treating neoplastic diseases in humans using parenteral formulations that include at least one stable elsamitrucin salt.Type: ApplicationFiled: June 15, 2006Publication date: December 20, 2007Applicant: SPECTRUM PHARMACEUTICALS, INC.Inventors: Ashok Gore, Fred Defesche, Hemant Joshi, Guru Reddy, Luigi Lenaz, Paul K. Isbester, Olga V. Lapina, Grant J. Palmer, Jonathon S. Salsbury
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Patent number: 7157432Abstract: Provided is a tetraphenylbacteriochlorin derivative represented by the formula (I): [wherein R1, R2, R3 and R4, independently from each other, are a residue of a monosaccharide represented by the formulae: (wherein, R is a hydrogen or a protecting group)], or its salt. The tetraphenylbacteriochlorin derivative or its salt has a large molar extinction coefficient at long wavelengths which are expected to have a high tissue-penetrating property, and exhibits high selectivity to tumor cells and hydrophilicity.Type: GrantFiled: September 7, 2005Date of Patent: January 2, 2007Assignees: San-Ei Gen F.F.I., Inc.Inventors: Shigenobu Yano, Toyoji Kakuchi, Yuji Mikata
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Patent number: 7112671Abstract: The present invention provides certain non-symmetric tripyrranes; that is, tripyrranes that do not contain a mirror plane of symmetry perpendicular to the plane containing the tripyrrane. Further, the invention includes texaphyrin compounds and sapphyrin compounds, as well as other polypyrrolic macrocycles, prepared using tripyrranes of Formula I as a precursor. These macrocycles are characterized by a tripyrrolic portion of the macrocyclic ring having substituents that cause the heterocycle to lack a plane of symmetry perpendicular to the plane of the macrocycle.Type: GrantFiled: August 28, 2001Date of Patent: September 26, 2006Assignee: Pharmacyclics, Inc.Inventors: Tarak D. Mody, Joshua Galanter
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Patent number: 7109323Abstract: The invention relates to the formulation of pharmaceutical compounds. More particularly, the invention provides stable, pharmaceutically acceptable compositions prepared from boronic acid compounds and methods for preparing the compositions. The invention also provides novel boronate ester compounds. The invention further provides boronic acid anhydride compounds useful in the methods of the invention.Type: GrantFiled: December 23, 2003Date of Patent: September 19, 2006Assignees: The United States of America as represented by the Department of Health and Human Services, Millennium Pharmaceutical, Inc.Inventors: Louis Plamondon, Louis Grenier, Julian Adams, Shanker Lal Gupta
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Patent number: 7105648Abstract: The invention relates to novel oligomers containing PNA units that are substituted by phosphite ester, phosphonic acid, or carbaborane functions and PNA monomers that are substituted by phosphite ester, phosphonic acid, or carbaborane functions, from which the novel oligomers are produced.Type: GrantFiled: March 3, 2000Date of Patent: September 12, 2006Assignee: Ugichem GmbHInventors: Holger Bock, Thomas Lindhorst
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Patent number: 7078519Abstract: Methods for forming structurally defined organosilicon carbohydrates are provided. Additionally, structurally defined organosilicon carbohydrates are provided. The structurally defined organosilicon carbohydrates may be formed by contacting a hydrolase enzyme with an organosilicon reactant and a carbohydrate reactant. The enzyme may catalyze the formation of an ester bond between carboxylic acid, ester, or amide functional groups of the organosilicon or carbohydrate reactant and alcohol functional groups of the carbohydrate or organosilicon reactant. The enzyme may catalyze the formation of an amide bond between carboxylic acid, ester, or amide functional groups of the organosilicon or carbohydrate reactant and amine functional groups of the carbohydrate or organosilicon reactant.Type: GrantFiled: August 15, 2003Date of Patent: July 18, 2006Assignees: Dow Corning Corporation, Polytechnic UniversityInventors: Kurt Friedrich Brandstadt, Thomas Howard Lane, Richard A. Gross
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Patent number: 6958319Abstract: The present invention provides stable compounds prepared from boronic acid and lyophilized compounds thereof of the formula (1): in which Z1 and Z2 are moieties derived from sugar. The invention also provides methods for preparing such compounds. Lyophilizing a mixture comprising a boronic acid compound and a moiety derived from sugar produces a stable composition that readily releases the boronic acid compound upon reconstitution in aqueous media.Type: GrantFiled: September 18, 2003Date of Patent: October 25, 2005Assignee: The United States of America as represented by the Department of Health and Human ServicesInventor: Shanker Lal Gupta
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Patent number: 6958389Abstract: Provided is a tetraphenylbacteriochlorin derivative represented by the formula (I): [wherein R1, R2, R3 and R4, independently from each other, are a residue of a monosaccharide represented by the formulae: (wherein, R is a hydrogen or a protecting group)], or its salt. The tetraphenylbacteriochlorin derivative or its salt has a large molar extinction coefficient at long wavelengths which are expected to have a high tissue-penetrating property, and exhibits high selectivity to tumor cells and hydrophilicity.Type: GrantFiled: September 6, 2001Date of Patent: October 25, 2005Assignees: San-Ei Gen F.F.I. Inc.Inventors: Shigenobu Yano, Toyoji Kakuchi, Yuji Mikata
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Patent number: 6906042Abstract: The invention provides micelles, pharmaceutical formulations comprising micells, solutions comprising micells, methods for preparing micells, methods for delivering micells to patients, and methods for treating sepsis, endotoxemia, septic shock and systemic inflamatory response syndrome in patients by adiministering micelles. The micelles comprises compounds of Forumala (A): wherein the substituents are as defined herein.Type: GrantFiled: February 20, 2001Date of Patent: June 14, 2005Assignee: Eisai Co., Ltd.Inventors: James McShane, Tori Arens, Kazuhiro Kaneko, Tomohiro Watanabe, Kazuhide Ashizawa
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Patent number: 6900181Abstract: The present invention concerns analogues of M6P for use in promoting the healing of wounds or fibrotic disorders with reduced scarring, together with methods for doing same.Type: GrantFiled: March 18, 2003Date of Patent: May 31, 2005Assignee: Renovo LimitedInventors: Mark W. J. Ferguson, Sarah G. Jones, Sally Freeman
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Patent number: 6861512Abstract: The geometric isomers of olefins and olefinic compounds are separated by means of liquid chromatography using a stationary phase comprising an organosilane with a pendant aliphatic functional group such as C18 and a mobile phase which includes an additive comprising alkanes and alkenes.Type: GrantFiled: March 1, 2001Date of Patent: March 1, 2005Assignee: Eisai Co., Ltd.Inventors: Lily Lu, John D. Orr
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Publication number: 20040138142Abstract: The invention relates to new carbohydrate derivatives of paclitaxel and docetaxel with increased solubility in water as compared to the parent compounds, paclitaxel and docetaxel These derivatives are produced from naturally occurring precursor molecules which upon hydrolysis yield these natural precursors and the original paclitaxel and docetaxel molecules. The present invention also related to the composition and the use of such derivatives for cancer therapy. These derivatives may also be used in antifungal or antiviral therapy.Type: ApplicationFiled: January 9, 2003Publication date: July 15, 2004Inventor: Michel Page
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Patent number: 6713446Abstract: The present invention provides stable compounds prepared from boronic acid and lyophilized compounds thereof of the formula (1): in which Z1 and Z2 are moieties derived from sugar. The invention also provides methods for preparing such compounds. Lyophilizing a mixture comprising a boronic acid compound and a moiety derived from sugar produces a stable composition that readily releases the boronic acid compound upon reconstitution in aqueous media.Type: GrantFiled: January 25, 2002Date of Patent: March 30, 2004Assignee: The United States of America as represented by the Secretary of the Department of Health and Human ServicesInventor: Shanker Lal Gupta
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Patent number: 6699835Abstract: The invention relates to the formulation of pharmaceutical compounds. More particularly, the invention provides stable, pharmaceutically acceptable compositions prepared from boronic acid compounds and methods for preparing the compositions. The invention also provides novel boronate ester compounds. The invention further provides boronic acid anhydride compounds useful in the methods of the invention.Type: GrantFiled: January 25, 2002Date of Patent: March 2, 2004Assignees: The United States of America as represented by the Department of Health and Human Services, Millennium Pharmaceuticals, Inc.Inventors: Louis Plamondon, Louis Grenier, Julian Adams, Shanker Lal Gupta
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Publication number: 20040023913Abstract: The invention relates to a pathogen-inactivating agent, as well as its use, whereby the agent contains an element that binds to nucleic acids of the pathogens, and a conjungate that destroys nucleic acid. The conjungate is created from a metal chelate complex, in which the metal can change between at least two oxidation levels. In particular, the agent can be used in physiological liquids, such as blood, or blood fractions for the inactivation of viruses.Type: ApplicationFiled: April 18, 2003Publication date: February 5, 2004Inventors: Hans-Juergen Neumann, Helmut Knoller
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Patent number: 6657057Abstract: The present invention provides an industrially excellent and novel process for producing methylcobalamin useful as medicines. Namely, it provides a process for producing methylcobalamin, which comprises the step of methylating cyanocobalamin or hydroxocobalamin in the presence of a reducing agent and a water-soluble methylating agent.Type: GrantFiled: May 23, 2002Date of Patent: December 2, 2003Assignee: Eisai Co., Ltd.Inventors: Yoshihiko Hisatake, Hiroshi Kuroda
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Patent number: 6630577Abstract: A reagent having the general formula of General Formula I: wherein group Z comprises a spacer selected from an aliphatic chain up to about 6 carbon equivalents in length, an unbranched aliphatic chain of from about 6 to 18 carbon equivalents in length with at least one of an intermediate amide and a disulfide moiety, and a polyethylene glycol chain of from about 3 to 12 carbon equivalents in length; wherein group R is an electrophilic or nucleophilic moiety suitable for reaction of the reagent with a biologically active species; and wherein group Q is one of nothing at all, an amide, a methyl amide, a methylene, an ether, a thioether, a methyl ether, and a methyl thioether moiety. Also, a conjugate, a bioconjugate and a method of conjugating.Type: GrantFiled: June 4, 2001Date of Patent: October 7, 2003Assignee: Prolinx, Inc.Inventors: Mark L. Stolowitz, Guisheng Li, Jean P. Wiley
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Patent number: 6624317Abstract: Compounds according to formula I: T1—L—T2 (I), wherein T1 is a taxoid group, preferably of Formula II: wherein R1 is C6H5; R2 is O; L is a linking group; and T2 is a substituent selected from the group consisting of epipodophyllotoxin, amsacrine, ellipticine, anthracycline antibiotic, mitoxantrone, and colchicine groups, and pharmaceutically acceptable salts thereof, are provided herein. The compounds are useful in, among other things, treating tumors or cancer in subjects in need thereof, inducing cellular differentiation, and inhibiting cellular mitosis.Type: GrantFiled: September 25, 2000Date of Patent: September 23, 2003Assignee: The University of North Carolina at Chapel HillInventors: Kuo-Hsiung Lee, Qian Shi, Kenneth F. Bastow, Hui-Kang Wang
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Patent number: 6620921Abstract: A &bgr;-D-glucofuranose compound which is 1,2,3,5,6-penta-O-propanoyl-&bgr;-D-glucofuranose, preferably in crystalline form, is prepared from D-glucose. The compound is prepared by reacting D-glucose with boric acid, or an equivalent thereof, followed by treatment with a propanoylating reagent, preferably propanoic anhydride. The compound is useful for the preparation of other compounds, such as glucofuranosides.Type: GrantFiled: September 19, 2002Date of Patent: September 16, 2003Assignee: Industrial Research LimitedInventors: Richard Hubert Furneaux, Phillip Martin Rendle, Ian Michael Sims
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Publication number: 20030171305Abstract: Provided is a tetraphenylbacteriochlorin derivative represented by the formula (I): 1Type: ApplicationFiled: March 7, 2003Publication date: September 11, 2003Inventors: Shigenobu Yano, Toyoji Kakuchi, Yuji Mikata
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Publication number: 20030166581Abstract: The invention encompasses novel salts of topiramate, and pharmaceutically acceptable polymorphs, solvates, hydrates, dehydrates, co-crystals, anhydrous, or amorphous forms thereof, as well as pharmaceutical compositions and pharmaceutical unit dosage forms containing the same. In particular, the invention encompasses pharmaceutically acceptable salts of topiramate, including without limitation topiramate sodium, topiramate lithium, topiramate potassium, or polymorphs, solvates, hydrates, dehydrates, co-crystals, anhydrous, and amorphous forms thereof. The invention further encompasses novel co-crystals or complexes of topiramate, as well as pharmaceutical compositions comprising them. The invention also encompasses methods of treating or preventing a variety of diseases and conditions including, but not limited to, seizures, epileptic conditions, tremors, cerebral function disorders, obesity, neuropathic pain, affective disorders, tobacco cessation, migraines, and cluster headache.Type: ApplicationFiled: November 18, 2002Publication date: September 4, 2003Inventors: Orn Almarsson, Julius Remenar, Matthew L. Peterson
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Patent number: 6600026Abstract: The present invention relates to the use of self-assembled monolayers with mixtures of conductive oligomers and insulators to detect target analytes.Type: GrantFiled: May 6, 1999Date of Patent: July 29, 2003Assignee: Clinical Micro Sensors, Inc.Inventor: Changjun Yu
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Publication number: 20030099968Abstract: A semiconductor nanocrystal compound is described which is capable of linking to one or more affinity molecules. The compound comprises (1) one or more semiconductor nanocrystals capable of, in response to exposure to a first energy, providing a second energy, and (2) one or more linking agents, having a first portion linked to the one or more semiconductor nanocrystals and a second portion capable of linking to one or more affinity molecules. One or more of these semiconductor nanocrystal compounds are linked to one or more affinity molecules to form a semiconductor nanocrystal probe capable of bonding with one or more detectable substances in a material being analyzed, and capable of, in response to exposure to a first energy, providing a second energy.Type: ApplicationFiled: May 24, 2002Publication date: May 29, 2003Inventors: Shimon Weiss, Marcel Bruchez, Paul Alivisatos
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Patent number: 6566339Abstract: The present invention concerns analogues of M6P for use in promoting the healing of wounds or fibrotic disorders with reduced scarring, together with methods for doing same.Type: GrantFiled: September 1, 2000Date of Patent: May 20, 2003Assignee: Renovo LimitedInventors: Mark William James Ferguson, Sarah Glenys Moore, Sally Freeman
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Patent number: 6486129Abstract: The present invention relates to compounds of formula (1), wherein R1 is phenyl, naphthyl, 1,2,3,4-tetrahydronaphthyl, (iso)quinolinyl, tetrahydro(iso)quinolinyl, 3,4-dihydro-1H-isoquinolinyl, chromanyl or the camphor group, which groups may optionally be substituted with one or more substitutents selected from (1-8C)alkyl or (1-8C)alkoxy; R2 and R3 are independently H or (1-8C)alkyl; R4 is (1-8C)alkyl or (3-8C)cycloalkyl; or R3 and R4 together with the nitrogen atom to which they are bonded are a nonaromatic (4-8)membered ring optionally containing another heteroatom, the ring optionally being substituted with (1-8C)alkyl or SO2-(1-8C)alkyl; Q is a spacer having a chain length of 10 to 70 atoms; and Z is a negatively charged oligosaccharide residue comprising two to six monosaccharide units, the charge being compensated by positively charged counterions; or a pharmaceutically acceptable salt thereof or a prodrug thereof.Type: GrantFiled: December 18, 2000Date of Patent: November 26, 2002Assignees: Akzo Nobel N.V., University LeidenInventors: Cornelia Maria Tromp, Johannes Egbertus Maria Basten, Constant Adriaan Anton van Boeckel, Rogier Christian Buijsman
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Publication number: 20020165369Abstract: The invention relates to novel platinum-based compounds for labeling biomolecules. Platinum based labeling compounds according to the invention irreversibly attach to a target biomolecule via coordination of a platinum (II) metal center with N or S atoms on the target biomolecule. The invention relates to the novel compounds themselves, methods of making the platinum-based labeling compounds, probes labeled with such compounds, methods of making such labeled probes, and kits comprising the novel platinum-based labeling compounds and/or probes labeled with them. The invention also relates to methods of using probes labeled with platinum-based labeling compounds of the invention, particularly array and microarray hybridization methods.Type: ApplicationFiled: March 1, 2002Publication date: November 7, 2002Applicant: StratageneInventors: Jeffrey Braman, Haoqiang Huang