Abstract: The present invention provides a substance which strongly inhibits human ?-amylase and is effective for the prevention and treatment of hyperglycemia, for example, diabetes and the diseases caused thereby, and an ?-amylase inhibitor and a prophylactic or therapeutic agent for hyperglycemia containing the said substance as active principle. Maltoligosaccharide derivatives represented by the following formula: (wherein n is an integer of 0 to 2; m is an integer of 0 to 2; and X represents a hydrogen atom or a hydrophobic group) or their hydrates or physiologically acceptable salts are provided, and they are contained as active principle to prepare an ?-amylase inhibitor and a prophylactic or therapeutic agent for hyperglycemia such as diabetes.

Abstract: Compounds represented by the formula 1: A is selected from the group consisting of wherein each R individually is H or acyl, Y is X, N3, NH2, monoalkylamino, or dialkylamino; Z is O or S; and X is selected from the group consisting of hydrogen, halo, hydroxy, alkoxy, alkyl, haloalkyl, alkenyl, haloalkenyl, alkynyl, amino, monoalkylamino, dialkylamino, thioaryl, thioalkyl, allylamino, cyano and nitro; tautomers thereof; and pharmaceutically acceptable salts thereof are provided along with methods for their fabrication. Various of these compounds can be used as anticancer agents, or antiviral agents or to inhibit DNA replication.

Abstract: Methods and compositions for treating or ameliorating diseases and other conditions, such as infectious diseases, autoimmune diseases and allergies are provided. The methods employ cyclic AGPs for selectively stimulating immune responses in animals and plants.

Abstract: Highly hydrophilic indole and benzoindole derivatives that absorb and fluoresce in the visible region of light are disclosed. These compounds are useful for physiological and organ function monitoring. Particularly, the molecules of the invention are useful for optical diagnosis of renal and cardiac diseases and for estimation of blood volume in vivo.

Abstract: Sugar-modified SIN-1 compositions are provided. The compositions are useful for generating NO in response to hydrolytic activity of a glycosidase specific for the O-glycosidic bond between the sugar and SIN-1 moieties. Pharmaceutical compositions containing the sugar-modified SIN-1 compositions and methods of using the compositions are also provided.

Abstract: Purpurin-carbohydrate conjugates and their method of preparation and use for treatment of cancer cells. The conjugates have the general formula: wherein R6 and R7 taken together are ?NR11 or are independently —OR11, where at least one R11 is preferably a mono or polysaccharide moiety and R1-R8 are various groups formed from carbon and hydrogen and optionally oxygen and nitrogen where R3 and R4 may together from a covalent bond.

Abstract: The subject invention discloses materials and methods for the design, synthesis, and biochemical evaluation of chromogenic substrate compounds for sialidases of bacterial, viral, protozoa, and vertebrate (including humans) origin. These compounds are based upon N-acetylneuraminic acid glycosides. In particular, this invention provides a novel class of these compounds as chromogenic substrates of these sialidases which yield chromogenic products after reactions catalyzed by sialidase take place. Also provided are methods of making these substrate compounds, methods of diagnosis and prognosis of sialidase related diseases using these substrate compounds.

Abstract: The subject invention discloses materials and methods for the design, synthesis, and biochemical evaluation of chromogenic substrate compounds for sialidases of bacterial, viral, protozoa, and vertebrate (including humans) origin. In particular, this invention provides a novel class of effective compounds as chromogenic substrates of these sialidases which yield chromogenic products after reactions catalyzed by sialidase take place. Also provided are methods of making these substrate compounds, methods of diagnosis and prognosis of sialidase related diseases using these substrate compounds.

Abstract: This invention provides novel substrate compounds that selectively inhibit the proliferation of pathological cells, for example, pathological calls that endogenously overexpress a target enzyme that confers resistance to biologic and chemotherapeutic agents. The enzyme acts on a substrate compound to 1) convert it to a cellular toxin and/or 2) release a toxic byproduct. In one embodiment, the activity of the target enzyme has been greatly enhanced in a target cell as a result of loss of tumor suppressor function and/or selection resulting from previous exposure to chemotherapy. In another embodiment, the pathological cell contains a target enzyme that is an expression product of an infectious agent in the cell. Further provided by this invention is a method for treating a subject by delivering to the subject a prodrug as described herein. The prodrugs of this invention may be used alone or in combination with other chemotherapeutics or alternative anti-cancer therapies such as radiation.

Abstract: wherein when Y is  or heteroaryl; A is —O(CH2)m, S, —NH(CH2)m, or (CH2)n where n is 0-3 and m is 0-2; and R1 to R6 are as defined herein. A method is also provided for treating diabetes and related diseases employing an SGLT2 inhibiting amount of the above compound alone or in combination with one, two or more other antidiabetic agents, and/or one, two or more hypolipidemic agents.

Abstract: The present invention discloses new and novel substituted anthracyclines with modified alkyl-aromatic ring substitutions on the C-3′ of the sugar moiety or modified or unmodified alkyl-aromatic ring substitutions at the C-4′ of the sugar moiety. It also discloses novel methods for the preparation of sugar substrates and methods for the preparation of anthracycline antibiotics. These anthracycline analogs show high cytotoxicity in vitro against several tumor cell lines.

Abstract: The present invention relates to a novel endogenous compound 2-amino-3-[2-(&agr;-mannopyranosyl)indole-3-yl]propionic acid; to a method for testing a biological function by quantitating 2-amino-3-[2-(&agr;-mannopyranosyl)indole-3-yl]propionic acid in a collected biological sample and determining the biological function based on the quantitated values; to an antibody specifically reactive with 2-amino-3-[2-(&agr;-mannopyranosyl)indole-3-yl]propionic acid; to a hybridoma that produces the antibody; to a method for immunologically quantitating 2-amino-3-[2-(&agr;-mannopyranosyl)indole-3-yl]propionic acid in a sample by using the antibody; and to a process for producing a 2-amino-3-[2-(&agr;-mannopyranosyl)indole-3-yl]propionic acid derivative.

Abstract: Maltoligosaccharide derivatives represented by the general formula: wherein n is an integer of 0 to 3 and X is a hydrogen atom or a hydrophobic group) or their hydrates or physiologically acceptable salts, and an &agr;-amylase inhibitor and a prophylactic or therapeutic agent for hyperglycemia such as diabetes containing them as an active ingredient.

Abstract: Processes for the preparation of 3′,4′-cyclic acetals of pentopyranosylnucleosides, in which the pentopyranosyl nucleoside is reacted with an aldehyde, ketone, acetal, or ketal under reduced pressure of less than about 500 mbar.

Abstract: This invention provides compounds containing a 2-deoxy-2-amino-&bgr;-D-glucopyranose (glucosamine) glycosidically linked to an cyclic aminoalkyl (aglycon) group. The invention further provides methods for inducing an immune response using the compounds of the present invention in the presence or absence of an antigen. In addition, methods for treating disease with the compounds of the present invention with or without an antigen are also provided in this invention.

Abstract: An SGLT2 inhibiting compound is provided having the formula A method is also provided for treating diabetes and related diseases employing an SGLT2 inhibiting amount of the above compound alone or in combination with another antidiabetic agent or other therapeutic agent.

Abstract: Branched hydrazone linkers for linking a targeting ligand such as an antibody to a therapeutically active drug. The point of branching is at a polyvalent atom and the number of drugs increases by a factor of two for each generation of branching. A preferred drug is doxorubicin.

Abstract: The subject invention discloses materials and methods for the design, synthesis, and biochemical evaluation of chromogenic substrate compounds for sialidases of bacterial, viral, protozoa, and vertebrate (including humans) origin. In particular, this invention provides a novel class of effective compounds as chromogenic substrates of these sialidases which yield chromogenic products after reactions catalyzed by sialidase take place. Also provided are methods of making these substrate compounds, methods of diagnosis and prognosis of sialidase related diseases using these substrate compounds.

Abstract: The present invention relates to glycoconjugates of 20(S)-camptothecin, in which a 3-O-methylated &bgr;-L-fucose unit is linked to the 20-hydroxyl group of a camptothecin derivative via a thiourea-modified peptide spacer. The invention furthermore relates to processes for the preparation of the compounds according to the invention and to their use as medicaments, in particular in connection with oncoses.

Abstract: A series of 2-(Purin-9-yl)-tetrahydrofuran-3,4-diol derivatives with broad anti-inflammatory properties which inhibit leukocyte recruitment and activation and which are agonists of the adenosine 2a receptor are described.

Abstract: Protecting groups derived from a halogenated coumarin group, a quinoline-2-one group, a xanthene group, a thioxanthene group, a selenoxanthene group, or an anthracene group are described. The protecting groups is photolabile and can be removed by irradiating the group with light, such as flash photolysis with ultraviolet radiation or pulsed infrared radiation.

Abstract: Benzimidazole derivatives useful for treating or preventing viral infections such as those caused by herpes viruses or in the treatment of restenosis following surgical techniques. Methods of preparing these benzimidazole derivatives and pharmaceutical compositions containing them are described.

Abstract: The invention relates to a method of potentiating cell damage in a target cell population by administering a “restraining agent” and concomitantly or subsequently applying a “targeted cytotoxic insult.” The restraining agent is administered at a concentration and under conditions sufficient to retard, but not to arrest, the progress of the target cell population through the cell cycle, a concept termed “dynamic retardation.” With such a mechanism, all the cells intended for damage by the targeted cytotoxic insult are likely to cycle into the relevant interval of vulnerability (target interval) within the cell cycle, resulting in a larger number of susceptible cells, and the time period during which those cells are vulnerable to the action of a given targeted cytotoxic insult is increased, resulting in a higher probability and percentage of cell killing.

Abstract: The present invention relates to simplified synthesis, new carbohydrate-based products and practical use of different carbohydrate-based products. Examples of these are (Gal&agr;1-3Gal), GlcNAc&bgr;1-3Gal, &agr;- or &bgr;-glycosides thereof, Gal&agr;1-3Gal- containing tri-, or higher oligosaccharides, &agr;- or &bgr;-glycosides thereof, GlcNAc&bgr;1-3Gal containing tri-, tetra-, or higher oligosaccharides, and derivatives and/or &agr;- or &bgr;-glycosides thereof, Gal&agr;1-3GalGlcNAc&bgr;1-3Gal, &agr;- or &bgr;-glycosides thereof, Gal&agr;1-3Gal&bgr;1-4GlcNAc&bgr;1-3Gal&bgr;1-4Glc, or other higher oligosaccharides containing the Gal&agr;1-3Gal-structure, &agr;- or &bgr;-glycosides thereof, modified carbohydrates, di-, tri-, oligo-, or polyfunctional products containing carbohydrate structures, and the use of the products for synthesis, affinity purification, diagnostic applications and therapy.

Abstract: SGLT2 inhibiting compounds are provided having the formula where R1, R2, and R2a are independently hydrogen, OH, OR5, lower alkyl, CF3, OCHF2, OCF3, SR5i or halogen, or two of R1, R2 and R2a together with the carbons to which they are attached can form an annelated five, six or seven membered carbocycle or heterocycle; R3 and R4 are independently hydrogen, OH, OR5a, OAryl, OCH2Aryl, lower alkyl, cycloalkyl, CF3, —OCHF2, —OCF3, halogen, —CN, —CO2R5b, —CO2H, —COR6b, —CH(OH)R6c, —CH(OR5h)R6d, —CONR6R6a, —NHCOR5c, —NHSO2R5d, —NHSO2Aryl, Aryl, —SR5e, —SOR5f, —SO2R5g, —SO2Aryl, or a five, six or seven membered heterocycle, or R3 and R4 together with the carbons to which they are attached form an annelated five, six or seven membered carbocycle or heterocycle; R5, R5a, R5b, R5c, R5d, R5e, R5f, R5g, R5h and R5i are independently lower alkyl; R6, R6a, R6b, R6c and R6d are independently hydrogen, alkyl,

Abstract: The use of carbohydrate derivatives in or for making a topical composition for promoting skin exfoliation is disclosed. The use of said composition of controlling intrinsic and extrinsic skin ageing, as well as a non-therapeutic skin treatment method for skin exfoliation, are also disclosed.

Abstract: Substituted benzothiepine 1,1-dioxide derivatives of formula I: 1

Abstract: The present invention is directed to novel ketomethylene group-containing inhibitors of cysteine or serine proteases. Methods for the use of the protease inhibitors are also described.

Abstract: The present invention provides an improved method of preparing a 4,7-di-O-alkyl chromogenic ketoside of N-acetylneuraminic acid (Neu5Ac) for use in detecting influenza virus types A and B. The ketosides are substrates that are selectively cleaved by a neuraminidase on influenza virus, but not be neuraminidases found on other viruses or on bacteria. The synthesis is efficient and provides large quantities of the ketoside for commercial development. The synthesis includes a step of alkylating the 4- and 7-hydroxyl groups of a protected alkyl ester alkyl ketoside derivative of Neu5Ac by a process that comprises contacting the derivative with a composition comprising an alkyl halide to form a 4,7-di-O-alkyl protected alkyl ester alkyl ketoside derivative of Neu5Ac. The synthesis alternatively includes protecting the 8- and 9-hydroxyl groups of an alkyl ester alkyl ketoside derivative of Neu5Ac by forming an 8,9-epoxide protected alkyl ester alkyl ketoside derivative of Neu5Ac.

Abstract: The present invention relates to a novel class of glycoside indoles. More specifically, the present invention relates to a novel class of glycoside indoles isolated from Calanthe discolor Lindl. and derivatives thereof.

Abstract: A new class of N-linked Lewis and LacNAc analogs of are synthesized and shown to be effective inhibitors of human fucosyltransferases. In a high yielding reaction sequence the glucosamine derivative 1 was transformed to the 3-azido-2,3-dideoxy sugar 2e under excellent stereocontrol. The LacNAc analog 4d was synthesized as a single isomer in three steps starting from 2e. In a one pot procedure iminocyclitol 5 was transformed into aldehyde 6 and successfully used for reductive amination with 4c and 2f yielding trisaccharide 8a, and disaccharide 7a.

Abstract: The present invention provides fluorescent nucleosides carrying polycyclic aromatic hydrocarbons such as anthracene, phenanthrene, pyrene stilbene, tetracene or pentacene. The subject nucleosides may be synthesized using a C-glycosidic bond formation method employing organocadmium or organozinc derivatives of the aromatic compounds and coupling with a 1-&agr;-chlororibose or deoxyribose synthon. The &agr;-anomers of the coupling reaction may be epimerized to the &bgr;-anomers by acid-catalyzed equilibration. The fluorescent nucleosides act as DNA or RNA base analogs and can be incorporated into nucleic acids. Resultant fluorescently tagged nucleic acids are useful as probes for target nucleic acids in tissues, solutions or immobilized on membranes.

Abstract: A process for producing riboflavin glucoside comprises cultivating a microorganism belonging to the genus Bacillus, such as Bacillus brevis, Bacillus cereus, Bacillus circulans, Bacillus coagulans, Bacillus licheniformis, Bacillus megaterium, Bacillus pumilus or Bacillus subtilis, which is capable of producing riboflavin glucosides, in an aqueous medium containing a starch under aerobic conditions. Amongst the preferred strains are Bacillus subtilis RB50::[pRF69]60Ade+ and Bacillus subtilis RB50::[pRF69]60[pRF93]120Ade+. The so-produced riboflavin glucoside can be used as a more soluble substitute for riboflavin to prepare clear drinks and injection solutions.

Abstract: Process for regiospecific preparation of new 3-hydroxypyridine-4(1H)-one derivatives starting from monosaccharides or itols of general formula: in which R represents a radical, either saturated or not, branched or not, having carbon-atom groups, and having hetero-atoms or not, and Sub represents a saccharide derivative or an itol, either cyclic not, protected or not, the hydrocarbon skeleton of which is bound to the nitrogen atom of the pyridinone either directly or by the intermediary of a spacing group. The present invention is characterized in that the process comprises a first step of protection of the 3-hydroxy group of the pyranone derivative, a second basocatalyzed step of substitution of the intracyclic oxygen atom of the pyranone by the nitrogen atom of the amine function of the amino monosaccharide or amino itol, and a third step of de-protection of the 3-OH group of the pyridinone cycle and possibly of the OH groups of the glucide or itol residue.

Abstract: This invention provides a process for the preparation of a Eleutherobin derivative of the formula: wherein R1 is a hydrogen, ester, nitrile or C2H4—R wherein R4 is a carbohydrate, an alcohol an amine, an amide, an alkyne, or, R2 is a linear or branched alkyl moiety, R3 is an ester, an amide, a carbamate, an acetal compound,an ether or a urethane, R4 is a hydrogen or CH2,position C2 and C3 is cis or trans,position C8 is &agr; or &bgr; and a compound is produced having the structures: Additionally, this experiment provides a method for inhibiting growth of cancerous cells comprising contracting an amount of Eleutherobin derivative effective to inhibit the growth of said cells. Further provided is a method for treating cancer in a subject which comprises administering to the subject a therapeutically effective amount of the Eleutherobin derivative.