Abstract: Exemplary embodiments of this invention encompass a method for purifying a substantially crude stevioside, methods for preparing polymorphic and amorphous forms of stevioside, and the polymorphic and amorphous forms prepared therefrom.
Abstract: The invention provides esterified ?-galactosylceramides effective for cancer treatment and the like, and a medicament containing same. In particular, the invention relates to a compound represented by the formula (I): wherein R1 is a hydrocarbon group having a carbon number of 1 to 30, R2 is a hydrocarbon group having a carbon number of 1 to 20, R3 is a hydrogen atom or hydrocarbon group having a carbon number of 1 to 5, R4 and R5 are the same or different and each is a hydrogen atom or a hydrocarbon group having a carbon number of 1 to 5, or R4 and R5 in combination form a divalent hydrocarbon group having a carbon number of 1 to 5, and optionally form a ring structure together with the adjacent ethylenedioxy, or a salt thereof.
Abstract: Cleavable compositions that comprise a polar head, cleavable linker, and a hydrophobic tail; and methods for using them to isolate hydrophobic molecules.
Type:
Application
Filed:
November 15, 2010
Publication date:
September 8, 2011
Inventors:
Richard M. Caprioli, Ned A. Porter, Jeremy L. Norris
Abstract: The invention provides a surfactant and/or a cleaning composition comprising a microbially produced branched fatty alcohol or a derivative thereof. The invention also provides a household cleaning composition and a personal or pet care cleaning composition comprising a microbially produced branched fatty alcohol or a derivative thereof.
Abstract: A compound represented by the following general formula (I) or a salt thereof: wherein R1 represents a glycosyl group, a phosphate group, or a cyclic phosphate group bound to R2; R2 represents —CH2OH, —CHO, —CH2NH2, —CH2-amino acid residue, or —CH2—OPO2H; and R3 represents hydrogen atom, or —PO3H2, and a composition for cosmetics, medicaments, foodstuffs, and/or feeds containing the aforementioned compound or a salt thereof.
Abstract: The invention provides novel dye-labeled ribonucleotide analogs and methods for synthesizing those analogs. The compounds of the invention are especially useful for DNA sequencing by the polymerase chain reaction.
Type:
Grant
Filed:
January 25, 2010
Date of Patent:
August 23, 2011
Assignee:
Applied Biosystems, LLC
Inventors:
Peter Virgil Fisher, Shaheer Khan, Paolo Vatta
Abstract: Method for the production of C-aryl glucoside SGLT2 inhibitors useful for the treatment of diabetes and related diseases. and intermediates thereof. The C-aryl glucosides may be complexed with amino acid complex forming reagents.
Type:
Application
Filed:
April 25, 2011
Publication date:
August 18, 2011
Applicant:
BRISTOL-MYERS SQUIBB COMPANY
Inventors:
Prashant P. Deshpande, Bruce A. Ellsworth, Janak Singh, Theodor W. Denzel, Chiajen Lai, Gerard Crispino, Michael E. Randazzo, Jack Z. Gougoutas
Abstract: The present invention provides quinaldine-based semisquaraines, symmetrical and unsymmetrical squaraine dyes represented by the general formulae 1, 2 and 3 and/or pharmaceutically acceptable derivatives thereof as sensitizers for photodynamic therapeutical and industrial applications. These symmetrical and unsymmetrical squaraine dyes posses absorption which extends well into the photodynamic window (650-800 nm) and hence are useful for the treatment of deep seated tumors. The absorption of these dyes can be tuned by changing the substituents on the quinaldine moiety thereby enabling the development of a library of dyes which have absorption ranging from 650 to 800 nm. They also exhibited fluorescence emission in the long wavelength region making them useful as near infrared fluorescence sensors for the detection of tumors. These dyes are non-toxic in the dark and exhibit good photocytotoxicity.
Type:
Grant
Filed:
January 8, 2007
Date of Patent:
August 16, 2011
Assignee:
Council of Scientific and Industrial Research
Abstract: The present invention relates to a method of identifying a candidate therapeutic agent. The method comprises contacting a G-Protein Coupled Receptor (GPCR) with a compound of General Formula (I), or a pharmaceutically acceptable salt thereof determining whether the compound inhibits or effects signal transduction activity of the GPCR, wherein a compound that inhibits or effects the activity of the GPCR is a candidate therapeutic agent.
Type:
Grant
Filed:
October 10, 2003
Date of Patent:
August 9, 2011
Assignee:
Alchemia Limited
Inventors:
Wim Meutermans, Glang Le Thanh, Giovanni Abbenante, Gerald Tometzki, Judy Halliday, Johannes Zuegg
Abstract: The present invention relates to a skin-protecting composition for the damaged skin, comprising glycyrrhizin, quercetin, rosmarinic acid, madecassic acid, chamazulene, bicalein and emodin. The composition of the present invention has all of excellent antioxidant, anti-inflammatory, wound-healing and moisturizing effects, thereby being widely used in medicine, cosmetic material or the like for the purpose of protecting the easily infectable, damaged and dried skin.
Type:
Grant
Filed:
December 17, 2007
Date of Patent:
August 9, 2011
Assignee:
Biospectrum, Inc.
Inventors:
Deok Hoon Park, Jong Sung Lee, Kwang sun Jung
Abstract: The present invention includes as an active ingredient at least one biosurfactant, in particular mannosyl alditol lipid (such as MEL and MML) or triacylated mannosyl alditol lipid. This allows providing an activator and anti-aging agent that is excellent in activating and anti-aging effects on cells and that is safe enough to be used for a long time, and also providing cosmetics, quasi-drugs, drugs, and drinks and foods including the activator and the anti-aging agent as active ingredients. Further, the present invention provides MEL whose mannosyl erythritol skeleton in a molecular structure is 1-O-?-D-mannopyranosyl-meso-erythritol and a method for producing the MEL with use of a microorganism.
Type:
Grant
Filed:
February 9, 2009
Date of Patent:
August 2, 2011
Assignees:
Toyo Boseki Kabushiki Kaisha, National Institute of Advanced Industrial Science and Technology
Abstract: This invention is directed to polysaccharide based aerogels, related to herein as aeropolysaccharides (aerocellulose) and reinforced aeropolysaccharides, and preparation thereof by an environmentally friendly process.
Abstract: The invention relates to the preparation of phenolics derivatives by enzymatic condensation of phenolics selected among pyrocatechol or its derivatives with the glucose moiety of sucrose. The production of said phenolics derivatives is achieved with a glucosyltransferase (EC 2.4.1.5). These O-?-glucosides of selected phenolics are new, have a solubility in water higher than that of their parent polyphenol and have useful applications in cosmetic and pharmaceutical compositions, such as antioxidative, antiviral, antibacterial, immune-stimulating, antiallergic, antihypertensive, antiischemic, antiarrythmic, antithrombotic, hypocholesterolemic, antilipoperoxidant, hepatoprotective, anti-inflammatory, anticarcinogenic, antimutagenic, antineoplastic, anti-thrombotic and vasodilatory formulations, or in any other field of application.
Type:
Application
Filed:
March 21, 2011
Publication date:
July 28, 2011
Applicant:
LIBRAGEN
Inventors:
DANIEL AURIOL, Renaud Nalin, Patrick Robe, Fabrice Lefevre
Abstract: A method for preparing hexose derivatives comprises the steps of providing a silylated hexose, treating the silylated hexose with a first carbonyl compound in the presence of a catalyst to form an ketalized hexose, treating the ketalized hexose with a second carbonyl compound followed by treating with a first reductant to form an etherized hexose, and converting the etherized hexose into a target hexose derivative, which can be 2-alcohol hexose, 3-alcohol hexose, 4-alcohol hexose, or a 6-alcohol hexose. In particular, the present invention can prepare the hexose derivatives with highly regioselective scheme to protect individual hydroxyls of monosaccharide units and install an orthogonal protecting group pattern in a one-pot manner.
Abstract: There are disclosed herein antigenic structures useful in producing vaccines against and compounds helpful in combating diseases caused by the bacterium Moraxella catarrhalis. Disclosed are specific structures of the carbohydrate molecules derived from genetically engineered strains of Moraxella catarrhalis, which when presented appropriately to the immune system will facilitate a functional immune response to the target core oligosaccharide region.
Abstract: Sulfoquinovosylacyl propanediol compounds represented by formula (I): wherein R1 is an acyl residue of a fatty acid, Y is a number of 1, 2 or 3, and M represents a cation having a positive charge equal to Y and pharmaceutically acceptable salts thereof are effective for treating tumors.
Abstract: Engineered nucleotide compositions, having polymerase interacting components that improve the interactivity of the polymerase and the nucleotide, particularly for nucleic acid sequencing applications. Compositions include the interactive polymerases along with the nucleotide analogs. Kits, methods and systems are provided for analysis of nucleic acid synthesis reactions.
Type:
Grant
Filed:
March 26, 2009
Date of Patent:
July 5, 2011
Assignee:
Pacific Biosciences of California, Inc.
Inventors:
Gene Shen, Paul Peluso, Arkadusz Bibillo
Abstract: The invention concerns novel 1,2-dioxetane derivatives of general formula (I) as defined in the description, capable of emitting a detectable luminescent signal, their use in a method for detecting and/or quantizing a physical, chemical or biological, in particular enzymatic, phenomenon, as well as a kit for implementing said method.
Type:
Grant
Filed:
May 24, 2006
Date of Patent:
June 28, 2011
Assignees:
Quidd, Universite de Rouen
Inventors:
Pierre-Yves Renard, Anthony Romieu, Marc Massonneau
Abstract: Compounds and methods are provided for obtaining oligosaccharide mimics. More specifically, compounds and methods are described wherein oligosaccharide mimics are obtained by incorporating or substituting in a cyclohexane derivative.
Type:
Grant
Filed:
October 9, 2007
Date of Patent:
June 21, 2011
Assignee:
GlycoMimetics, Inc.
Inventors:
Beat Ernst, Daniel Schwizer, Arun K Sarkar, John L Magnani
Abstract: The present invention relates to antioxidative and hepatoprotective compositions, and more particularly to antioxidative and hepatoprotective compositions comprising diarylheptanoid compounds from Alnus japonica. The diarylheptanoid compounds from Alnus japonica include a compound selected from the group consisting of alusenone 1a, alusenone 1b, hirsutenone, hirsutanonol, oregonin, alnuside A, alnuside B, rubranoside B and rubranoside C. The antioxidative and hepatoprotective compositions have excellent antioxidative and hepatoprotective activities while having no side effects, and thus are useful for the prevention and treatment of oxidation-associated diseases and liver diseases.
Type:
Application
Filed:
May 6, 2010
Publication date:
June 16, 2011
Applicant:
RNL BIO CO., LTD.
Inventors:
Jeong Chan RA, Young Ho KIM, Dong Hwan SOHN
Abstract: A method for restructuring the epidermis with a composition, wherein said composition includes a polyol-glycoside and said polyol-glycoside is obtained by the acetalization of a polyol with a reducing sugar.
Type:
Application
Filed:
February 22, 2011
Publication date:
June 16, 2011
Applicant:
Societe D'Exploitation De Produits Pour Les Industries Chimiques (SEPPIC)
Abstract: Novobiocin analogues and pharmaceutical composition containing such compounds useful for the treatment and/or prevention of neurodegenerative disorders and autoimmune disorders.
Abstract: The object of the present invention is to provide a nucleoside or nucleotide having a 5-substituted-2-oxo(1H)pyridin-3-yl group as a base, as well as a method using the same. In one embodiment, the nucleoside or nucleotide of the present invention has a fluorescent dye selected from the group consisting of 5-FAM, 6-FAM, 5-TAMRA, 6-TAMRA, DANSYL, 5-HEX, 6-HEX, 5-TET, 6-TET, 5-ROX and 6-ROX or a quencher dye selected from the group consisting of DABCYL, BHQ1 and BHQ2, which is attached either directly or through a linker to the 5-position of the above base.
Abstract: This invention relates to processes for production of alkylamino glucosaminide phosphate compounds, and of disaccharide compounds, including various novel intermediates and intermediate processes. In one aspect, glycosyl halides are produced by reaction of an O-silyl glycoside with a dihalomethyl alkyl ether.
Abstract: The compounds of formula (I), wherein n is an integer from 0 to 4; R1 is a radical selected from the group consisting of H, CH3, CH2-CH3, C(CH3)3, COOH, CONH2 and C?CH; R2, R3, R4 and R5 are radicals independently selected from the group consisting of H, F, Cl, Br, (C1-C3)-alkoxyl and (C1-C4)-alkyl; and R6 is a radical selected from the group consisting of H, F, Cl, Br, (C1-C3)-alkoxyl, (C1-C4)-alkyl, R7, CH?CH—R7 and O—CH2—R7; wherein R7 is phenyl or phenyl mono- or independently di-substituted with F, Cl, Br, (C1-C3)-alkoxyl or (C1-C4)-alkyl, exhibit a similar chemotactic index to that of amygdalin (natural product whose chemotaxis profile is similar to that of peptide T) and, consequently, are useful for treating inflammatory and/or allergic dermatophathies, such as psoriasis, and are especially much less toxic than amygdalin.
Type:
Grant
Filed:
May 29, 2007
Date of Patent:
June 7, 2011
Assignee:
Universitat Politècnica De Catalunya
Inventors:
Pérez Gonzáles Juan Jesús, Amadeu Llebaria Soldevilla, Carmen Lagunas Arnal, Andrés Fernández Garcia
Abstract: The disclosure provides nucleotide analogs and methods of their use. Analogs of the invention comprise a reporter molecule (label) attached via the N4, N6, O4, or O6 position of the nitrogenous base portion of the analog. In a preferred embodiment, nucleotide analogs of the invention comprise a label attached to the nitrogenous base portion of the analog via a cleavable linker at the N4, O4, N6 or O6 position.
Abstract: The invention relates to compounds which are polysulfated oligosaccharide derivatives having activity as inhibitors of heparan sulfate-binding proteins and inhibitors of the enzyme heparanase; methods for the preparation of the compounds; compositions comprising the compounds, and use of the compounds and compositions thereof for the antiangiogenic, antimetastatic, anti-inflammatory, antimicrobial, anticoagulant and/or antithrombotic treatment, lowering of blood triglyceride levels and inhibition of cardiovascular disease of a mammalian subject.
Type:
Application
Filed:
December 3, 2010
Publication date:
June 2, 2011
Applicant:
Progen Pharmaceuticals Limited
Inventors:
Vito Ferro, Jon Krueger Fairweather, Tomislav Karoli, Ligong Liu
Abstract: Provided are an external preparation for skin and a wrinkle-reducing agent exhibiting an excellent effect of reducing wrinkles that develop particularly in an exposed site along with aging, and having high safety. The external preparation for skin and the wrinkle-reducing agent each contain an alkyl thioglycoside represented by the general formula (1): G-SR1 (1) (in the formula: G represents a sugar; R1 represents an alkyl group having 10 to 18 carbon atoms; and G and an SR1 group are bonded to each other via a ?-glycosidic bond).
Abstract: The invention relates to polysulfated glycosides of formula (I), the pharmaceutically acceptable salts thereof, as well as the pharmaceutical compositions containing these compounds as active ingredients. Furthermore the invention provides a method of preventing, treating or alleviating the symptoms of acute and chronic inflammatory disorders of the airways of mammals—including asthma and asthma-related pathologies.
Type:
Application
Filed:
January 25, 2011
Publication date:
May 19, 2011
Applicant:
Ivax Drug Research Institute Ltd.
Inventors:
János Kuszmann, István Kurucz, Gábor Medgyes, Nicholas Bodor
Abstract: The present invention relates to novel antineoplastic agents and cancer diagnostic agents that specifically target neo-plastic cells via the GLUT transportation system. More specifically, the invention relates to conjugates of 2-deoxyglucose, wherein a linker, which includes a covalent bond, is attached to 2-deoxyglucose at the 2 position, and the linker is attached to a therapeutic or diagnostic agent. The invention also relates to methods of treating tumor disease and methods of making the novel compounds of the present invention. The agents of the present invention are superior to previous agents as they are targeted via GLUT transporters.
Type:
Grant
Filed:
June 9, 2004
Date of Patent:
May 17, 2011
Assignee:
The Trustees of the University of Pennsylvania
Inventors:
Gang Zheng, Jerry D. Glickson, Britton Chance
Abstract: The present invention can provide a novel saccharide primer, which makes it possible to efficiently synthesize a sugar chain, and a method for using the primer. According to the present invention, the saccharide primer of the present invention is a saccharide primer having an alkenyl chain that has one or more double bonds in a position other than the alkyl chain terminal, and represented by the following general formula (I): Lac-O-Ck:m(n) ??General formula (I) In the general formula (I), Ck represents an alkenyl chain, m represents a total number of double bonds, and n represents a position of the double bond in the alkenyl chain. Here, k is preferably an integer in the range of 8 to 14, and particularly 12 or 13. In addition, when m is 1, n is an integer satisfying 1?n?k?2; and when m satisfies 2?m?k?1, n is a plurality of integers satisfying 1?n?k?1.
Abstract: The invention provides a tobramycin formulation for delivery by aerosolization in the form of additive-free, isotonic solution whose pH has been optimised to ensure adequate shelf-life at room temperature. Said formulation can be advantageously used for the treatment and prophylaxis of acute and chronic endobronchial infections, in particular those caused by the bacterium Pseudomonas aeruginosa associated to lung diseases such as cystic fibrosis.
Abstract: The present invention relates to the use of diaryl hepatonoid-based compounds of formula (1) for inhibiting viral activity. The diaryl hepatonoid-based compounds have an excellent effect of inhibiting viral activity, and thus will be useful as therapeutic agents against virus-related diseases.
Type:
Application
Filed:
June 4, 2009
Publication date:
May 5, 2011
Inventors:
Jeong Chan Ra, Young Ho Kim, Hyuk Joon Kwon, Huu Tung Nguyen
Abstract: The invention relates to: (i) the use of osyl derivatives of genkwanin and sakuranetin having formula (I) in (a) cosmetics or dermatology and (b) therapeutics; (ii) the use of novel derivatives having formula (I) as industrial products; and (iii) the production method thereof [Formula (I)], wherein symbol [Formula (II)] represents a single or double bond, R represents H or an osyl residue, particularly with structure S1 or s2 [Formula (III)], Z represents H, an alkyl group at C1-C4, acyl at C1-C5, monosaccharide or sulphate.
Type:
Grant
Filed:
March 11, 2005
Date of Patent:
May 3, 2011
Inventors:
Michel Prost, Jacqueline Ragot, Pierre Tubery
Abstract: Method for the production of C-aryl glucoside SGLT2 inhibitors useful for the treatment of diabetes and related diseases. and intermediates thereof. The C-aryl glucosides may be complexed with amino acid complex forming reagents.
Type:
Grant
Filed:
June 19, 2007
Date of Patent:
April 26, 2011
Assignee:
Bristol-Myers Squibb Company
Inventors:
Prashant P. Deshpande, Bruce A. Ellsworth, Janak Singh, Theodor W. Denzel, Chiajen Lai, Gerard Crispino, Michael E. Randazzo, Jack Z. Gougoutas
Abstract: An external preparation composition used for preventing or treating symptoms or diseases related to dermatopathy caused by dryness, UV rays and aging such as wrinkles and sags of the skin, pigmentation of the skin, skin roughness and coarse texture and skin diseases such as psoriasis, lichen, ichthyosis, keratosis, Darier's disease, pustulosis, acne, eczema and atopic dermatitis. The external preparation composition comprises at least one of acyl glucosamine derivatives represented by the following Formula (I): wherein R1, R2, R3, R4 and R5 are defined; and X is any one of groups represented by the following Formulas (A) to (C): wherein Y, n and R6 are also defined.
Abstract: The invention relates to compounds capable of releasing nitric oxide wherein the compounds comprise a saccharide and at least one nitric oxide-releasing diazeniumdiolate [N2O2] functional group, which is bonded directly to a carbon atom of the saccharide, and methods for preparing the same. The invention further comprises the treatment of biological disorders treatable by the administration of nitric oxide.
Type:
Grant
Filed:
October 16, 2006
Date of Patent:
April 19, 2011
Assignee:
The United States of America, as represented by the Secretary, Department of Health and Human Services
Abstract: The invention provides a high throughput, high purity, high yield system and method of isolating and purifying rebaudioside A (“Reb A”), with acceptable water solubility for all commercial uses, from commercially available Stevia rebaudiana starting material. The invention also provides a means of maximizing yields of 99+% purity Reb A based on the attributes of a given batch of Stevia starting material. The Reb A produced by the invention is water soluble, devoid of bitterness heretofore associated with rebaudioside sweeteners, non-caloric, and suitable for use as a reagent and as an ingredient in orally consumed products, e.g., as a sweetener, flavor enhancer, and flavor modifier.
Type:
Grant
Filed:
October 17, 2005
Date of Patent:
April 12, 2011
Assignee:
SGF Holdings, LLC
Inventors:
Mel Clinton Jackson, Gordon James Francis, Robert Gordon Chase
Abstract: Pharmaceutical formulations containing (i) an amphiphilic drug and (ii) a short-chain sphingolipid are described and provided herein along with methods of making and using same.
Type:
Grant
Filed:
November 11, 2004
Date of Patent:
March 29, 2011
Assignee:
Het Nederlands Kanker Instituut
Inventors:
Robert J. Veldman, Wim J. Van Blitterswijk, Marcel Verheij, Gerben A. Koning
Abstract: A method for increasing breast meat yield in avians by treating the poultry with an effective amount of natamycin. The effective amount of natamycin can be added to the avian's feed wither directly or in the form of a premix containing a carrier.
Abstract: The present invention provides methods for preparing LPS antagonist lipodisaccharide B1287 and stereoisomers thereof, which compounds are useful as in the prophylactic and affirmative treatment of endotoxemia including sepsis, septicemia and various forms of septic shock. Also provided are synthetic intermediates useful for implementing the inventive methods.
Abstract: Oligonucleotide probes containing two labels are provided and are useful in hybridization assays. The probes can also contain a minor groove binding group.
Type:
Grant
Filed:
January 6, 2010
Date of Patent:
March 1, 2011
Assignee:
Elitech Holding B.V.
Inventors:
Michael W. Reed, Eugeny Alexander Lukhtanov, Alexander A. Gall, Robert O. Dempcy, Nicolaas M. J. Vermeulen
Abstract: Novel enzymes and novel enzymatic pathways for the pyruvate-based synthesis of shikimate or at least one intermediate thereto or derivative thereof, nucleic acids encoding the enzymes, cells transformed therewith, and kits containing said enzymes, cells, or nucleic acid. A KDPGal aldolase is used to perform condensation of pyruvate with D-erythrose 4-phosphate to form 3-deoxy-D-arabino-heptulosonate-7-phosphate (DAHP); a 3-dehydroquinate synthase is used to convert the DAHP to 3-dehydroquinate (DHQ); DHQ dehydratase can then convert DHQ to the key shikimate intermediate, 3-dehydroshikimate.
Type:
Application
Filed:
July 20, 2010
Publication date:
February 24, 2011
Applicant:
BOARD OF TRUSTEES OPERATING MICHIGAN UNIVERSITY
Abstract: 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:
Grant
Filed:
July 31, 2009
Date of Patent:
February 22, 2011
Assignee:
Alnylam Pharmaceuticals, Inc.
Inventors:
Muthiah Manoharan, Kallanthottathil G. Rajeev, Jie Xia
Abstract: A process for preparing a bioabsorbable sheet preparation holding thrombin is provided. A process for preparing a bioabsorbable sheet preparation holding thrombin which comprises immersing a bioabsorbable sheet consisting of polyglycolic acid in a thrombin solution containing thrombin as an active ingredient, glycerol as a softening agent, Tween 80 as a permeating agent, and optionally histidine and trehalose as a stabilizing agent followed by drying to hold thrombin on said bioabsorbable sheet, and a bioabsorbable sheet preparation holding thrombin prepared by said process.
Type:
Application
Filed:
April 15, 2009
Publication date:
February 17, 2011
Applicant:
THE CHEMO-SERO-THERAPEUTIC RESEARCH INSTITUTE
Abstract: Pyrazole derivatives represented by the general formula: wherein R1 represents H, an optionally substituted C1-6 alkyl group etc.; one of Q and T represents a group selected from the following groups: and the other represents —(CH2)n—Ar wherein Ar represents a substituted C6-10 aryl group, etc., and n represents 0 to 2, R represents an optionally substituted C3-8 cycloalkyl group, etc., pharmaceutically acceptable salts thereof or prodrugs thereof, which exhibit an excellent inhibitory activity in human 1,5-anhydroglucitol/fructose/mannose transporter and are useful as agents for the prevention, inhibition of progression or treatment of a disease associated with the excess uptake of at least a kind of carbohydrates from glucose, fructose and mannose or a disease associated with hyperglycemia and pharmaceutical compositions comprising the same, pharmaceutical uses thereof, and intermediates for production thereof.
Abstract: Methods are described for the preparation of combinatorial libraries of potentially biologically active disaccharide compounds. These compounds are variously functionalized, with a view to varying lipid solubility size, function an other properties, with the particular aim of discovering novel drug or drug-like compounds, or compounds with useful properties. The invention provides intermediates, processes and synthetic strategies for the solution or solid phase synthesis of disaccharides, variously functionalized about the sugar ring, including the addition of aromaticity and charge, and the placement of pharmaceutically useful groups and isosteres.
Type:
Grant
Filed:
April 24, 2003
Date of Patent:
January 25, 2011
Assignee:
Alchemia Limited
Inventors:
Wim Meutermans, Michael West, George Adamson, Giang Thanh Le, Nicholas B. Drinnan, Giovanni Abbenante, Bernd Becker, Matthias Grathwohl, Premraj Rajaratnam, Gerald Tometzki