Abstract: 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, etc. It is a 1-substituted-3-(?-D-glycopyranosyl) nitrogen-containing heterocyclic compound represented by the general formula (I), a prodrug thereof, or a pharmaceutically acceptable salt thereof, or a hydrate or a solvate thereof; an SGLT inhibitor containing the same; a pharmaceutical composition containing the same and a combination pharmacy of them. In the formula, A represents an alkylene group or alkenylene group; B represents a single bond, —O—, —S— or —NH—; C represents an optionally substituted aryl or heteroaryl group; Q independently represents a carbon atom which a hydrogen atom or a substituent binds to, or a nitrogen atom.

Abstract: This invention provides compositions of matter that, when incorporated into an oligonucleotide, present to a complementary strand in a Watson-Crick pairing geometry a pattern of hydrogen bonds that is different from the pattern presented by adenine, guanine, cytosine, and thymine. Most specifically, this invention discloses and claims compositions of matter that present the same hydrogen bonding patterns as the isocytidine and isoguanosine nucleobases, but do not have unfavorable tautomeric forms, do not become disassociated from their sugar, and do not make major groove interactions, as much, as easily, or as strongly as isocytidine and isoguanosine.

Abstract: The present invention provides nitrogen-containing fused cyclic 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 one of R1 and R4 represents a group represented by the following general formula (S) (in which R5 and R6 represent H, OH, a halogen atom, etc.; Q represents an alkylene group etc.; and ring A represents an aryl group etc.), and the other represents H, OH, an amino group, etc.; R2 and R3 represent H, OH, an amino group, a halogen atom, and an optionally substituted alkyl group, etc.; A1 represents O, S, etc.

Abstract: The present invention relates to C-Glycosylisoflavones having alkylaminoalkoxyl substituent and pharmaceutically acceptable salts thereof, a process for the preparation thereof, pharmaceutical compositions comprising an effective amount of a compound of the formula (I), and to the use of these compounds or compositions for the treatment or prevention of cardio- and cerebrovascular diseases, in particular for the treatment of various cardiocerebral hypoxic-ischemic diseases, for the treatment or prevention of diabetes mellitus and complications thereof, and for the treatment or prevention of chemical poisoning, in particular alcoholism.

Abstract: The instant invention provides for compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer.

Abstract: This invention relates to the field of nucleic acid chemistry, more specifically to the field of compositions and processes that can bind to nucleic acids, including compositions and processes that by doing so have use in the capture, detection and sequencing of nucleic acids, and most specifically to nucleoside analogs that incorporate nucleobase analogs that are able to bind to different natural nucleobases with nearly equal affinity, and therefore display a degree of ambiguity, or universality, in their binding pattern. Such nucleobase analogs, when incorporated into oligonucleotides, allow the oligonucleotides to bind with nearly equal affinity and/or melting temperature, to a complementary strand, template the synthesis of oligonucleotide from primers that have a distribution of sequences, and support the sequencing of oligonucleotides. Thus, these have use in human diagnostics, especially when polymorphisms are present in a population.

Abstract: Compounds represented by the formula: and pharmaceutically acceptable salts thereof and prodrugs thereof; wherein R1 is H, CH3, C2H5, C3H7 R2 is H, CH3, C2H5, C3H7, CH?CH2, CH2—OH, CH2F, CF3 R?2 is H, OH, NH2, NH-alkyl, F, N3, OCH3, O—C(O)CH(NH2)alkyl R3 is H, CH3, C2H5, C3H7 R?3 is H, OH, NH2, NH-alkyl, F, N3, OCH3, O—C(O)CH(NH2)alkyl R4 is H, CH3, C2H5, C3H7 At least one of R2, R3, or R4has to be other than H, when X?NH in B R6 is H, CH3, C2H5, R7 is selected from H, alkyl, alkenyl, aryl, acyloxyalkyl, and pivaloyloxyalkyl, aminoacids, CH2CH2SC(O)alkyl; and B is represented by the following structure: X is independently NR6, O, S, R8 and R9 independently is H, NH2, OH, SH, F, Cl, Br, I, aryl, heterocycle, alkyl, alkene, alkyne, S-alkyl, S-aryl, S(O)-alkyl, SO2-alkyl, SO2NH2, SO2NH-alkyl, SO2NH-aryl, NH-alkyl, NH-aryl, N(alkyl)2, N(aryl)2, O-alkyl, O-aryl, O-heterocycle, NH-(CH2)n-aryl, NH—C(O)-alkyl, NH—C(O)-aryl are useful for inhibiting viral RNA polymerases and treating patients

Abstract: The present invention provides C-purine nucleoside analogs and certain derivatives thereof which are inhibitors of RNA-dependent RNA viral polymerase. These compounds are inhibitors RNA-dependent RNA viral replication and are useful for the treatment of RNA-dependent RNA viral infection. They are particularly useful as inhibitors of hepatitis C virus (HCV) NS5B polymerase, as inhibitors of HCV replication, and/or for the treatment of hepatitis C infection. The invention also describes pharmaceutical compositions containing such C-nucleoside compounds alone or in combination with other agents active against RNA-dependent RNA viral infection, in particular HCV infection. Also disclosed are methods of inhibiting RNA-dependent RNA polymerase, inhibiting RNA-dependent RNA viral replication, and/or treating RNA-dependent RNA viral infection with the C-nucleoside compounds of the present invention.

Abstract: The invention provides methods for treating hepatitis C viral infections and related viral infections, as well as compounds and compositions that are useful for treating such infections.

Abstract: 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, etc. It is a 1-substituted-3-(?-D-glycopyranosyl) nitrogen-containing heterocyclic compound represented by the general formula (I), a prodrug thereof, or a pharmaceutically acceptable salt thereof, or a hydrate or a solvate thereof; an SGLT inhibitor containing the same; a pharmaceutical composition containing the same and a combination pharmacy of them. In the formula, A represents an alkylene group or alkenylene group; B represents a single bond, —O—, —S— or —NH—; C represents an optionally substituted aryl or heteroaryl group; Q independently represents a carbon atom which a hydrogen atom or a substituent binds to, or a nitrogen atom.

Abstract: The present invention relates to the use of the compound according to formula (I), below for the treatment of tumors, cancer and hyperproliferative diseases, among other conditions or disease states: Where X is H or F; R1 and R2 are independently H, an acyl group, a C1-C20 alkyl or ether group, a phosphate, diphosphate, triphosphate or a phosphodiester group, a (A) or (B) group; Where Nu is a radical of a biologically active compound such as an anticancer, antiviral or antihyperproliferative compound such that an amino group or hydroxyl group from said biologically active agent forms a phosphate, phosphoramidate, carbonate or urethane group with the adjacent moiety; each R8 is independently H, or a C1-C20 alkyl or ether group, preferably a C1-C12 alkyl group; k is 0-12, preferably, 0-2; and pharmaceutically acceptable salts thereof.

Abstract: Novel synthetic monomers that have the capacity to be assembled into defined oligomers which bind with sequence specificity to duplex Watson-Crick DNA via a triple helix motif are provided.

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 C-glycoside derivatives and salts thereof, wherein B ring is bonded to A ring via —X— and A ring is directly bonded to the glucose residue, and it is usable as a Na+-glucose cotransporter inhibitor, especially for a therapeutic and/or preventive agent for diabetes such as insulin-dependent diabetes (type 1 diabetes) and insulin-independent diabetes (type 2 diabetes), as well as diabetes related diseases such as an insulin-resistant diseases and obesity.

Abstract: This invention relates to substituted fused heterocyclic C-glycosides, compositions containing them, and methods of using them, for example, for the treatment or prophylaxis of diabetes and Syndrome X.

Abstract: The present invention relates to dideoxynucleoside analog compounds containing a dideoxy ribofuranosyl moiety that exhibit selective anti-viral activity coupled with substantially low toxicity toward the host cells. In particular, the compounds according to the present invention show potent inhibition of the replication of the human immunodeficiency virus (HIV), while remaining substantially inert toward host cell DNA. Compounds according to the present invention exhibit primary utility as agents for inhibiting the growth or replication of retroviruses, particularly HIV. The compounds of the invention comprise a (2,3?-dideoxy-?-ribofuranosyl) ring coupled to a heterocyclic nucleobase that lacks an “O2 carbonyl”, that enables them to selectively react with and inhibit viral reverse transcriptase, while remaining substantially unreactive toward human DNA polymerases.

Abstract: Disclosed are novel bicyclic tris(anhydride)s useful as intermediates in the synthesis of biologically active compounds, and the compounds which may be synthesized from such intermediates.

Abstract: C-nucleosides are synthesized by a method in which a sugar is derivatized in a single step to provide a heterocycle at the C1 position, and then the heterocycle is aromatized in another single step. In one class of preferred embodiments a cyano sugar is converted into thiocarboxamide, and subsequently condensed to form an azole ring. In a second class of preferred embodiments a cyano sugar is condensed with an amino acid to provide the azole ring. In a third class of preferred embodiments a halo sugar is condensed with a preformed heterocycle to provide the azole ring.

Abstract: The present invention provides 2-aminopyridine and 2-pyridone C-nucleosides and oligonucleotides containing the subject nucleosides. The nucleosides are useful in the preparation of the subject oligonucleotides. The oligonucleotides are useful in oligonucleotide-based diagnosis and separation through triplex binding.

Abstract: The invention provides nucleosides of formulae (I), (II), (V) and (VII) as described in the specification which possess antiviral and anticancer activity. Treatment of breast cancer is a preferred embodiment.

Abstract: The present invention provides 2-aminopyridine and 2-pyridone C-nucleosides and oligonucleotides containing the subject nucleosides. The nucleosides are useful in the preparation of the subject oligonucleotides. The oligonucleotides are useful in oligonucleotide-based diagnosis and separation through triplex binding.

Abstract: A method for synthesizing C-glycosides of ulosonic acids such as Neu5Ac, by which diastereocontrolled synthesis of &agr;-C-glycosides of ulosonic acids is attained is disclosed. In the method of the present invention, an ulosonic acid sulfone or phosphite is reacted with an aldehyde or ketone compound in the presence of a lanthanide metal halide.

Abstract: Provided is an artificial nucleic acid which has a double-stranded structure made of two oligonucleotides, where the oligonucleotide has in a sugar-phosphate backbone structure thereof a sugar moiety having a group having a metal-coordinating site, and the two oligonucleotides are bound together through a metal complex structure formed by coordination of the metal-coordinating site to a metal ion. Also provided is a nucleotide useful for synthesizing the artificial nucleic acid.

Abstract: Disclosed are novel bicyclic tris(anhydride)s useful as intermediates in the synthesis of biolologically active compounds, and the compounds which may be synthesized from such intermediates.

Abstract: Compounds of the formula I 1

Abstract: The present invention relates, in general, to a nucleoside base and, in particular, to a universal, photocleavable nucleoside base. The invention further relates to oligonucleotides comprising such a base.

Abstract: Novel nucleoside analogs, such as 3-(&bgr;-D-Ribofuranosyl)-2-fluoropyridine, 3-(&bgr;-D-Ribofuranosyl)-pyridin-2-one, 3-(&bgr;-D-Ribofuranosyl)-pyridin-2-(4-nitrophenylethyl)-one, 3-(&agr;-D-Ribofuranosyl)-2-fluoropyridine, 5-(&bgr;-D-Ribofuranosyl)-2-bromopyridine, 5-(&agr;-D-Ribofuranosyl)-2-bromopyridine, 5-(&bgr;-D-Ribofuranosyl)-pyridin-2-one, 5-(&agr;-D-Ribofuranosyl)-pyridin-2-one, 5-(&bgr;-D-Ribofuranosyl)-2-aminopyridine, 5-(&bgr;-D-Ribofuranosyl)-pyridin-2-(4-nitrophenylethyl)-one, and 5-(&agr;-D-Ribofuranosyl)-2-aminopyridine; process for their synthesis and incorporation into polynucleotides.

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: This invention pertains to nucleoside analogs that have antiviral activity and improved metabolic stability, compositions comprising them, and methods of antiviral treatment employing them. More particularly, this invention pertains to imidazo[1,2-a]pyridine C-nucleosides, as exemplified by compounds such as imidazo[l,2-a]pyridine C5-nucleosides and imidazo[1,2-a]pyridine C3-nucleosides, and may be represented by formula (I), wherein exactly one of Q3 and Q5 is a sugar-like moiety; exactly one of Q3 and Q5 is —H; and Q2, Q6, Q7 and Q8 are independently imidazo[1,2-a]pyridine substituents, such as —H, —F, —Cl, —Br and —I.