Abstract: [Objective] The present invention provides a compound having an SGLT1 and/or SGLT2 inhibitory activity which is usable as an agent for the prevention or treatment of diabetes, postprandial hyperglycemia, impaired glucose tolerance, diabetic complications, obesity or the like. [Means to Solve the Problem] It is a 1-substituted-7-(?-D-glycopyranosyloxy)(aza)-indole compound represented by the general formula (I), a prodrug thereof, or a pharmaceutically acceptable salt thereof, or a hydrate or solvate thereof: wherein R1 represents a halogen atom or the like; n represents j an integer number from 0 to 3; R2 represents a hydrogen atom or the like; X represents a carbon atom which a hydrogen atom or the like binds to, or a nitrogen atom; Q represents an alkylene group or an alkenylene group each of which may have an oxygen atom or a sulfur atom in the chain; and A represents an aryl or heteroaryl group which may have a substituent.

Abstract: Problem: To provide compounds which have an anticoagulation effect based on their ability to inhibit the activated blood coagulation factor X and are useful as coagulation inhibitors or agents for prevention or treatment for diseases caused by thrombi or emboli. Means for Solution: Benzene derivatives or their salts having a characteristic chemical structure with a phenol ring and a benzene ring bonding to each other via an amide bond, in which the phenol ring further bonds to a benzene ring or a heteroaryl ring via an amide bond. They have an excellent effect of inhibiting the activated blood coagulation factor X, and especially have an excellent oral activity.

Abstract: The present invention relates to monosaccharide derivatives as anti-inflammatory agents. The compounds disorder herein can be useful for inhibition and prevention of inflammation and associated pathologies including inflammatory and autoimmune diseases such as bronchial asthma, rheumatoid arthritis, type I diabetes, multiple sclerosis, allograft rejection, psoriasis, inflammatory bowel disease, ulcerative colitis, acne, atherosclerosis, cancer, pruritis and allergic rhinitis. Pharmacological compositions containing compounds disclosed herein and the methods of treating bronchial asthma, chronic obstructive pulmonary disease, rheumatoid arthritis, multiple sclerosis, type I diabetes, psoriasis, allograft rejection, inflammatory bowel disease, ulcerative colitis, acne, atherosclerosis, cancer, pruritis, allergic rhinitis and other inflammatory and/or autoimmune disorders, using the compounds are also provided.

Abstract: Synthetic ligand compounds and methods of differentiating between Shiga toxin 1 and Shiga toxin 2 are disclosed herein. Another embodiment includes a kit for differentiating between Shiga toxin 1 and Shiga toxin 2. Assay systems and methods for providing an assay are also provided for herein.

Abstract: The present invention provides novel pyrrolo[2,1-c][1,4]benzodiazepine-glycoside prodrug of general formula 1a-b, useful as selective anticancer agents. The present invention also provides a process for the preparation of novel pyrrolo[2,1-c][1,4]benzodiazepine-glycoside prodrugs of general formula 1a-b. This invention also provides activation of these produgs by E. coli ? galactosidase and envisaged that these molecules are toxic to human cancer cell lines in the presence of the enzyme E. coli ?-galactosidase. The prodrugs 1a and 1b were also found to be toxic to human cancer HepG2 cells even in the absence of the E. coli ?-galactosidase. The toxic effect of the molecules when activated was similar to that of the parent molecules 6a and 6b, respectively.

Abstract: The present invention relates to processes for the production of 4-biphenylylazetidin-2-one derivatives of formula

Abstract: Derivatives of PSAs are synthesised, in which a reducing and/or non-reducing end terminal sialic acid unit is transformed into a N-hydroxysuccinimide (NHS) group. The derivatives may be reacted with substrates, for instance substrates containing amine or hydrazine groups, to form non-cross-linked/crosslinked polysialylated compounds. The substrates may, for instance, be therapeutically useful drugs, peptides or proteins or drug delivery systems.

Abstract: Aminoglycoside-polyamines are disclosed along with methods of use thereof in displacement chromatography and as DNA-binding ligands. The aminoglycoside-polyamines are derivatives of carbohydrates, such as sugars, amino sugars, deoxysugars, glycosides, nucleosides and their substituted counterparts. The subject polyamines possess a group in place of at least one hydrogen atom of at least one hydroxyl group of the carbohydrate compound. In these compounds R1 is an alkyl group or an azaalkyl group, and R2 is a primary or secondary amino group.

Abstract: This invention provides estrogen receptor modulators of formula I, having the structure wherein Q, Q2, R1, R2, R2a, R3, R3a, and X as defined in the specification, or a pharmaceutically acceptable salt thereof.

Abstract: The present invention makes available, inter alia, methods and reagents for modulating smoothened-dependent pathway activation. In certain embodiments, the subject methods can be used to counteract the phenotypic effects of unwanted activation of a hedgehog pathway, such as resulting from hedgehog gain-of-function, ptc loss-of-function or smoothened gain-of-function mutations.

Abstract: The present invention provides glucopyranosyloxypyrazole derivatives represented by the general formula: wherein R represents a hydrogen atom, a lower alkyl group or a group forming a prodrug; one of Q and T represents a group represented by the general formula: (wherein P represents a hydrogen atom or a group forming a prodrug), while the other represents a lower alkyl group or a halo(lower alkyl) group; R2 represents a hydrogen atom, a lower alkyl group, a lower alkoxy group, a lower alkylthio group, a halo(lower alkyl) group or a halogen atom; and with the proviso that P does not represent a hydrogen atom when R represents a hydrogen atom or a lower alkyl group, or pharmaceutically acceptable salts thereof, which exert an inhibitory activity in human SGLT2 and have an improved oral absorption, and therefore are useful as agents for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, diabetic complications or obesity, and pharmaceutically acceptable salts thereo

Abstract: Fluorescent glycosides containing aromatic hydrocarbon groups are useful in labelling and detection methods for a wide array of chemical and biological molecules. Assembly of multiple analogs to form “polyfluors” affords fluorescence properties that are different from the properties of the component analogs. This allows for the design and use of combinatorial libraries of molecules displaying widely varying fluorescence colors.

Abstract: The invention relates to the compound of the formula (A) and also to its physiologically acceptable salts. The compound is suitable as, for example, a hypolipidemic.

Abstract: 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.

Abstract: Design and synthesis of a novel library of compounds comprising a spacer with an attachment element on one terminus and a recognition element on the other terminus is presented. The library of compounds can be attached to a solid support and used as an integral component of sensors and biosensors or the library of compounds can be used as antiviral drugs or to isolate pathogens from complex mixtures for further analysis.

Abstract: A photolabile compound, an oligomer probe array, and a substrate for oligomer probe array comprising the same, and a manufacturing method of the same are disclosed.

Abstract: The present invention provides nitrogen-containing fused-ring derivatives represented by the following general formula, or pharmaceutically acceptable salts thereof, or prodrugs thereof, which exhibit an excellent inhibitory activity in human SGLT and are useful as agents for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, postprandial hyperglycemia, impaired glucose tolerance, diabetic complications or obesity, in the formula R1 represent H, an optionally substituted alkyl group, an alkenyl group, etc.; R2 represent H, a halogen atom or an alkyl group; R3 and R4 represent H, OH, a halogen atom, an optionally substituted alkyl group, etc.; Y represents CH or N; Q represents alkylene, alkenylene, etc.; ring A represents an aryl group or a heteroaryl group; G represents a group represented by the following general formula (G-1) or (G-2) (in which E1 represents H, F or OH; and E2 represents H, F, a methyl group, etc.

Abstract: Disclosed are compositions and methods capable of facilitating the detection and measurement of poly(ADP-ribose)polymerases (PARP enzymes). PARP enzyme activity can be monitored using a novel calorimetric substrate, ADP-ribose-para-nitrophenol. The substrate can be synthesized from beta nicotinamide adenine dinucleotide (?-NAD+) and para-nitrophenol. In an embodiment, a continuous assay was developed to detect and kinetically monitor activity for PARP enzymes such as PARP-1, tankyrase-1 (PARP-5), and VPARP (PARP-4). The compositions and methods are particularly useful in the screening and identification of specific PARP inhibitors.

Abstract: 4-Biarylyl-1-phenylazetidin-2-ones useful for the treatment of hypercholesterolemia are disclosed. The compounds are of the general formula in which represents an aryl or heteroaryl residue; Ar represents an aryl residue; U is a two to six atom chain; and the R's represent substituents.

Abstract: The present invention provides glucopyranosyloxypyrazole derivatives represented by the general formula: wherein R represents a hydrogen atom, a lower alkyl group or a group forming a prodrug; one of Q and T represents a group represented by the general formula: (wherein P represents a hydrogen atom or a group forming a prodrug), while the other represents a lower alkyl group or a halo(lower alkyl) group; R2 represents a hydrogen atom, a lower alkyl group, a lower alkoxy group, a lower alkylthio group, a halo(lower alkyl) group or a halogen atom; and with the proviso that P does not represent a hydrogen atom when R represents a hydrogen atom or a lower alkyl group, or pharmaceutically acceptable salts thereof, which exert an inhibitory activity in human SGLT2 and have an improved oral absorption, and therefore are useful as agents for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, diabetic complications or obesity, and pharmaceutically acceptable salts there

Abstract: A compound having SGLT1 and/or SGLT2 inhibitory activity which is usable as an agent for the prevention or treatment of diabetes, postprandial hyperglycemia, impaired glucose tolerance, diabetic complications, obesity, etc. It is a 1-(?-D-glycopyranosyl)-3-substituted nitrogen-containing heterocyclic compound represented by the general formula (I), a prodrug, or a pharmaceutically acceptable salt thereof, or a hydrate or solvate thereof; an SGLT inhibitor containing the same; a pharmaceutical composition containing the same and a medicinal use thereof. In the formula, ring A represents optionally substituted aryl or heteroaryl; Q1 to Q5 independently represent a carbon atom having a hydrogen atom or substituent bonded thereto or a nitrogen atom; E represents a single bond, alkylene, —O—, —S— or —NH—; and R represents methyl, ethyl, fluoromethyl or hydroxymethyl.

Abstract: The present invention relates to glucopyranosyloxy-pyrazoles of general formula wherein R1 to R6 and R7a, R7b, R7c are defined as in claim 1, the tautomers, the stereoisomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids, which have valuable pharmacological properties, particularly an inhibitory effect on sodium-dependent glucose cotransporter SGLT, the use thereof for the treatment of diseases, particularly metabolic disorders such as diabetes, and the preparation thereof.

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.

Abstract: Compounds and pharmaceutical compositions comprising them are disclosed that may be useful for the treatment of diseases and disorders such as diabetes and obesity.

Abstract: The invention relates to novel derivatives of morphine-6-glucuronide, the preparation method thereof and the uses of same in therapy, for example, as analgesics.

Abstract: Compounds having the formula (I): wherein A represents a group such as a cyclic group, R1 and R2 represent groups such as alkyl groups or hydroxymethyl groups, and n represents 1 or 2, or pharmacologically acceptable salts thereof or pharmacologically acceptable esters thereof have superior activity and stability, and are useful for the treatment and/or prevention of diabetes mellitus, or the like.

Abstract: The present invention relates to processes for preparing the compounds of general formula I, wherein the groups R1 to R6 and R7a, R7b, R7c are defined according to claim 1. Furthermore the present invention relates to processes for preparing educts and intermediates in the above processes and to intermediates as such.

Abstract: Novel aromatic fluoroglycoside derivatives, medicaments containing these compounds, and the use thereof. The invention relates to substituted aromatic fluoroglycoside derivatives of the formula I in which the radicals have the stated meanings, and their physiologically tolerated salts and process for their preparation. The compounds are suitable for example as antidiabetics.

Abstract: The present invention provides pyrazole-O-glycoside derivatives represented by the following formulae, used as a diabetic medicine

Abstract: The present invention is directed to compounds comprising a 2,3-diphenylquinoxaline moiety which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for treating cancer comprising administration of the compounds of the invention.

Abstract: The present invention provides glucopyranosyloxypyrazole derivatives represented by the general formula: wherein R1 is a hydrogen atom or a hydroxyalkyl group; one of Q and T is a group represented by the general formula; the other is an optionally substituted alkyl group or a cycloalkyl group; and R2 is a halogen atom, a hydroxy group, an optionally substituted alkyl group, an optionally substituted alkoxy group, an alkylthio group, a group of the general formula: -A-R3 wherein A is a single bond, an oxygen atom, a methylene group, an ethylene group, —OCH2— or —CH2O—; and R3 is a cycloalkyl group, a heterocycloalkyl group, an optionally substituted aryl group, an optionally substituted tiazolyl group or an optionally substituted pyridyl group, pharmaceutically acceptable salts thereof or prodrugs thereof, which exert an excellent inhibitory activity in human SGLT1, and therefore are useful as drugs for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, diabetic

Abstract: The present invention provides glucopyranosyloxypyrazole derivatives represented by the general formula: wherein one of Q and T represents a group represented by the general formula: while the other represents a lower alkyl group or a halo(lower alkyl) group; R1 represents a hydrogen atom, an optionally substituted lower alkyl group, a lower alkenyl group, a cyclic lower alkyl group, etc.; R2 represents a hydrogen atom, an optionally substituted lower alkyl group, a lower alkoxy group, a lower alkenyl group, a cyclic lower alkyl group, a cyclic lower alkoxy group, etc., which exert an excellent inhibitory activity in human SGLT2, and therefore are useful as drugs for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, diabetic complications or obesity, pharmaceutically acceptable salts thereof or prodrugs thereof, production intermediates thereof and pharmaceutical uses thereof.

Abstract: 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.

Abstract: Substituted indole-O-glucosides, compositions containing them, and methods of using them, for example for the treatment of diabetes and Syndrome X are disclosed.

Abstract: The present invention discloses compounds of formula I, or pharmaceutically acceptable salts, esters, or prodrugs thereof: which exhibit antibacterial properties. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject in need of antibiotic treatment. The invention also relates to methods of treating a bacterial infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The invention further includes process by which to make the compounds of the present invention.

Abstract: The present invention relates to anti-tumor compounds, compositions and methods.

Abstract: 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.

Abstract: A process for the production of dual-functional ion exchange resins from lignocellulosic agricultural material involving anionization of the lignocellulosic agricultural material with citric acid and then cationization of the lignocellulosic agricultural material with dimethyloldihydroxyethylene urea (DMDHEU) and choline chloride, or cationization of the lignocellulosic agricultural material with DMDHEU and choline chloride and then anionization of the lignocellulosic agricultural material with citric acid.

Abstract: This invention relates to to substituted benzimidazole-O-glucosides, benztriazole-O-glucosides, and benzimidazolone-O-glucosides, compositions containing them, and methods of using them, for example, for the treatment or prophylaxis of diabetes and Syndrome X.

Abstract: The present invention provides glucopyranosyloxypyrazole derivatives represented by the general formula: wherein one of Q and T represents a group represented by the general formula: while the other represents a lower alkyl group or a halo(lower alkyl) group; R1 represents a hydrogen atom, an optionally substituted lower alkyl group, a lower alkenyl group, a cyclic lower alkyl group, etc.; R2 represents a hydrogen atom, an optionally substituted lower alkyl group, a lower alkoxy group, a lower alkenyl group, a cyclic lower alkyl group, a cyclic lower alkoxy group, etc., which exert an excellent inhibitory activity in human SGLT2, and therefore are useful as drugs for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, diabetic complications or obesity, pharmaceutically acceptable salts thereof or prodrugs thereof, production intermediates thereof and pharmaceutical uses thereof.

Abstract: Substituted indazole-O-glucosides, compositions containing them, and methods of using them, for example for the treatment of diabetes and Syndrome X are disclosed.

Abstract: The present invention provides glucopyranosyloxypyrazole derivatives represented by the general formula: wherein R represents a hydrogen atom, a lower alkyl group or a group forming a prodrug: one of Q and T represents a group represented by the general formula: (wherein P represents a hydrogen atom or a group forming a prodrug), while the other represents a lower alkyl group or a halo(lower alkyl) group; R2 represents a hydrogen atom, a lower alkyl group, a lower alkoxy group, a lower alkylthio group, a halo(lower alkyl) group or a halogen atom; and with the proviso that P does not represent a hydrogen atom when R represents a hydrogen atom or a lower alkyl group, or pharmaceutically acceptable salts thereof, which exert an inhibitory activity in human SGLT2 and have an improved oral absorption, and therefore are useful as agents for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, diabetic complications or obesity, and pharmaceutically acceptable salts thereo

Abstract: The present invention provides methods of treating diabetes and associated conditions by administering a composition including at least one sterol or 5?-stanol absorption inhibitor or compositions or therapeutic combinations including: (a) at least one antidiabetic medication; and (b) at least one sterol or 5?-stanol absorption inhibitor.

Abstract: This invention provides analogs of eleutherobin and the eleuthesides modified at the C-11 position or comprising an epoxide functionality from C-11 to C-12. C-11 to C-12 is an ideal location for conjugating functional moieties to the eleutherobin pharmacophore without significant loss of antimitotic activity. Moieties that may be conjugated at C-11 include those intended to increase the solubility of the pharmacophore, to facilitate drug formulation, or to facilitate in vivo delivery or targeting.

Abstract: The present invention provides compositions, therapeutic combinations and methods including: (a) at least one hormone replacement therapy composition; and (b) at least one sterol absorption inhibitor which can be useful for treating vascular conditions in post-menopausal women and lowering plasma levels of sterols or 5?-stanols.

Abstract: The present invention provides methods for the treatment of obesity using sterol or 5?-stanol absorption inhibitors and compositions and therapeutic combinations including sterol or 5?-stanol absorption inhibitors and at least one obesity control medication.

Abstract: In accordance with the present invention, there is provided pregabalin lactose conjugate compounds. Also provided as part of the present invention is a novel method of central nervous system disorders or diseases including seizure disorders, pain, depression, anxiety, sleep disorders, consumptive disorders, psychosis, tardive dyskinesia, Huntington's disease, or Parkinson's disease in a subject by administering to the subject a pharmaceutically effective amount of a pregabalin lactose conjugate.

Abstract: The reactivity of a number of p-methylphenyl thioglycoside (STol) donors which are either fully protected or have one hydroxyl group exposed has been quantitatively determined by HPLC in conjunction with the development of a broadly applicable approach for a facile one-pot synthesis of oligosaccharides. The influence on reactivity of the structural effects of different monosaccharide cores and different protecting groups on each glycoside donor is characterized and quantified. In addition, a correlation between glycosyl donor reactivity and the chemical shift of the anomeric proton by 1 H NMR has been established. A database of thioglycosides as glycosyl donors has been created using this reactivity data. The utility is demonstrated by the easy and rapid one-pot assembly of various linear and branched oligosaccharide structures.

Abstract: The present invention provides pyrazole-O-glycoside derivatives represented by the following formulae, used as a diabetic medicine.

Abstract: Compounds of the formula I, in which R1, R2, R3, R4, R5, and R6 have the meanings given in the description, and their physiologically acceptable salts. The compounds are suitable for use, for example, as hypolipidemics.