Abstract: This invention relates to an oligonucleotide comprising one or more abasic nucleoside monomers of formula V: These monomers are useful for modifying of oligonucleotides at one or more positions. This invention also relates to a method of inhibiting the expression of a target gene in a cell. The method comprises contacting the cell with an oligonucleotide having one or more of the above formula (V).

Abstract: A pharmaceutical composition includes a pharmaceutical polysaccharide and phenylephrine hydrochloride. The ratio of said polysaccharide to phenylephrine hydrochloride is sufficient to dilute the composition such that phenylephrine hydrochloride is stable at high temperature and humidity.

Abstract: The present invention relates to a new class of diazepine-derivatives as chelating agents for paramagnetic metal ions, the process for their preparation, and use of such paramagnetic complexes as contrast agents, particularly suitable for Magnetic Resonance Imaging (MRI) analysis.

Abstract: Functionally-modified oligonucleotide analogues comprising modified intersubunit linkages and/or modified 3? and/or 5?-end groups are provided. The disclosed compounds are useful for the treatment of diseases where inhibition of protein expression or correction of aberrant mRNA splice products produces beneficial therapeutic effects.

Abstract: Disclosed is a method for highly efficiently obtaining an optically active alcohol from a carbonyl compound highly enantioselectively. Also disclosed is a ligand used in such a method. Specifically, an optically active alcohol is obtained by reacting a carbonyl compound and an organozinc compound by using a ligand (L) shown below.

Abstract: The present invention provides a benzazepine compound that can maintain for a long period of time the blood level of tolvaptan enabling to provide the desired pharmaceutical effects. The benzazepine compound of the present invention is represented by general formula (1) wherein R1 represents a —CO—(CH2)n—COR2 group (wherein n is an integer of 1 to 4, and R2 is (2-1) a hydroxy group; (2-2) a lower alkoxy group optionally substituted with a hydroxy group, a lower alkanoyl group, a lower alkanoyloxy group, a lower alkoxycarbonyloxy group, a cycloalkyloxycarbonyloxy group, or 5-methyl-2-oxo-1,3-dioxol-4-yl; or (2-3) an amino group optionally substituted with a hydroxy-lower alkyl group), or the like.

Abstract: The present invention provides a benzoazepine compound represented by following general formula (1): or a salt thereof, wherein R represents a hydrogen atom, a hydroxy group optionally protected with a protecting group, etc., R1 represents a hydrogen atom or hydroxy-protecting group, and X represents an oxygen atom or a sulfur atom. The benzoazepine compound of the present invention and salts thereof have high solubility in water, and can be suitably used for injections.

Abstract: Immunopotentiators can be adsorbed to insoluble metal salts, such as aluminium salts, to modify their pharmacokinetics, pharmacodynamics, intramuscular retention time, and/or immunostimulatory effect. Immunopotentiators are modified to introduce a moiety, such as a phosphonate group, which can mediate adsorption. These modified compounds can retain or improve their in vivo immunological activity even when delivered in an adsorbed form.

Abstract: The present invention provides novel compounds and ligands that are useful in transition metal catalyzed cross-coupling reactions. For example, the compounds and ligands of the present invention are useful in palladium or gold catalyzed cross-coupling reactions.

Abstract: Disclosed herein are phosphate esters of noribogaine and dihydronoribogaine, and esters and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising such compounds, and the methods of their use, including in the treatment of addiction and/or pain.

Abstract: The present application provides novel pyrimido-pyridazinone compounds and methods for preparing and using these compounds. These compounds are useful in treating inflammation in patients by administering one or more of the compounds to a patient. In one embodiment, the novel pyrimido-pyridazinone compound is of Formula (I) and R1 and R2 are defined herein.

Abstract: Compounds of Formula I and methods for treating metabolic disorders are disclosed.

Abstract: The present invention provides a benzoazepine compound represented by following general formula (1): or a salt thereof, wherein R represents a hydrogen atom, a hydroxy group optionally protected with a protecting group, etc., R1 represents a hydrogen atom or hydroxy-protecting group, and X represents an oxygen atom or a sulfur atom. The benzoazepine compound of the present invention and salts thereof have high solubility in water, and can be suitably used for injections.

Abstract: A class of compounds that inhibit Hepatitis C Virus (HCV) is disclosed, along with compositions containing the compound, and methods of using the composition for treating individuals infected with HCV.

Abstract: The present invention provides a benzoazepine compound represented by following general formula (1): or a salt thereof, wherein R represents a hydrogen atom, a hydroxy group optionally protected with a protecting group, etc., R1 represents a hydrogen atom or hydroxy-protecting group, and X represents an oxygen atom or a sulfur atom. The benzoazepine compound of the present invention and salts thereof have high solubility in water, and can be suitably used for injections.

Abstract: The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.

Abstract: A class of compounds that inhibit Hepatitis C Virus (HCV) is disclosed, along with compositions containing the compound, and methods of using the composition for treating individuals infected with HCV.

Abstract: Disclosed is a method for highly efficiently obtaining an optically active alcohol from a carbonyl compound highly enantioselectively. Also disclosed is a ligand used in such a method. Specifically, an optically active alcohol is obtained by reacting a carbonyl compound and an organozinc compound by using a ligand (L) shown below.

Abstract: Immunopotentiators can be adsorbed to insoluble metal salts, such as aluminium salts, to modify their pharmacokinetics, pharmacodynamics, intramuscular retention time, and/or immunostimulatory effect. Immunopotentiators are modified to introduce a moiety, such as a phosphonate group, which can mediate adsorption. These modified compounds can retain or improve their in vivo immunological activity even when delivered in an adsorbed form.

Abstract: The present invention is directed to processes associated with the preparation of [2-(8,9-dioxo-2,6-diazabicyclo[5.2.0]non-1(7)-en-2-yl)ethyl]phosphonic acid (perzinfotel).

Abstract: This invention relates to methods and small molecules having a phosphate group that can be used to inhibit phosphate transport and to treat or prevent diseases that are related to disorders in the maintenance of normal serum phosphate levels.

Abstract: Compounds are provided which can be useful in reducing the activity of an angiotensin-converting enzyme and thus be used to treat or prevent a renin-angiotensin aldosterone system-related disorder. These compounds include lipoic acid derivatives such as prolyl lipoic acid and pipecolinyl lipoic acid, and other compounds, and these compounds are useful in treating hypertension, stroke, or other renin-angiotensin aldosterone system-related disorders in human or animal patients. Pharmaceutical compositions prepared using these compounds and methods of treatment using these compounds are also provided.

Abstract: The present invention provides compounds of Formula I and salts, hydrates, solvates, complexes, and prodrugs thereof. The present invention further provides methods for synthesizing compounds of Formula I. The invention additionally provides pharmaceutical compositions comprising the compounds of Formula I and methods of using the pharmaceutical compositions of Formula I to treat and prevent disorders and diseases associated with the RyR receptors that regulate calcium channel functioning in cells.

Abstract: The present invention provides a benzoazepine compound represented by following general formula (1): or a salt thereof, wherein R represents a hydrogen atom, a hydroxy group optionally protected with a protecting group, etc., R1 represents a hydrogen atom or hydroxy-protecting group, and X represents an oxygen atom or a sulfur atom. The benzoazepine compound of the present invention and salts thereof have high solubility in water, and can be suitably used for injections.

Abstract: The present invention provides a benzoazepine compound represented by following general formula (1): or a salt thereof, wherein R represents a hydrogen atom, a hydroxy group optionally protected with a protecting group, etc., R1 represents a hydrogen atom or hydroxy-protecting group, and X represents an oxygen atom or a sulfur atom. The benzoazepine compound of the present invention and salts thereof have high solubility in water, and can be suitably used for injections.

Abstract: The present invention provides a benzazepine compound that can maintain for a long period of time the blood level of tolvaptan enabling to provide the desired pharmaceutical effects. The benzazepine compound of the present invention is represented by general formula (1) wherein R1 represents a —CO—(CH2)n—COR2 group (wherein n is an integer of 1 to 4, and R2 is (2-1) a hydroxy group; (2-2) a lower alkoxy group optionally substituted with a hydroxy group, a lower alkanoyl group, a lower alkanoyloxy group, a lower alkoxycarbonyloxy group, a cycloalkyloxycarbonyloxy group, or 5-methyl-2-oxo-1,3-dioxo-4-yl; or (2-3) an amino group optionally substituted with a hydroxy-lower alkyl group), or the like.

Abstract: Compounds of formula (I) or pharmaceutically acceptable salts thereof are provided: wherein: A is alkylenyl of 1 to 4 carbon atoms, or alkenylenyl of 2 to 4 carbon atoms; R1 and R2 are, independently, hydrogen or a C5 to C7 aryl optionally substituted with 1 to 2 substituents, independently, selected from the group consisting of —C(O)R3, halogen, cyano, nitro, hydroxyl, C1-C6 alkyl, and C1-C6 alkoxy, with the proviso that at least one of R1 and R2 is not hydrogen; R3 is, independently, hydrogen, —OR4, alkyl, aryl, or heteroaryl; R4 is hydrogen, alkyl, aryl, or heteroaryl; R5 and R6 are, independently, hydrogen, alkyl, hydroxyl, alkoxy, or C5 to C7 aryl; wherein any R3 to R6 group having an aryl or heteroaryl moiety can optionally be substituted on the aryl or heteroaryl moiety with 1 to about 5 substituents, independently, selected from the group consisting of halogen, cyano, nitro, hydroxyl, C1-C6 alkyl, and C1-C6 alkoxy.

Abstract: Compounds of formula (I) or pharmaceutically acceptable salts thereof are provided where at least one of R2 or R3 is not hydrogen. The compounds of the present invention are N-methyl-D-aspartate (NMDA) receptor antagonists and are useful in treating a variety of conditions present in a mammal that benefit from inhibiting the NMDA receptor.

Abstract: The invention relates to novel compounds and methods of using them for modulating sleep.

Abstract: The present invention relates to substituted arylsulphonylaminomethyl-phosphonic acid derivatives of general formula wherein R, X, Y and Z are defined as in claim 1, the tautomers, enantiomers, diastereomers, mixtures thereof and salts thereof which have valuable pharmacological properties, particularly the suppression of the interaction of glycogen phosphorylase a with the GL subunit of glycogen-associated protein phosphatase 1 (PP1), and their use as pharmaceutical compositions.

Abstract: The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels and calcium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.

Abstract: A mutual prodrug of a MRA and a (?-agonist for formulation for delivery by aerosolization to inhibit pulmonary bronchoconstriction is described. The mutual prodrug is preferably formulated in a small volume solution (10-500 ?L) dissolved in a quarter normal saline having pH between 5.0 and 7.0 for the treatment of respiratory tract bronchoconstriction by an aerosol having mass median average diameter predominantly between 1 to 5?, produced by nebulization or by dry powder inhaler.

Abstract: The present invention provides a benzoazepine compound represented by following general formula (1): or a salt thereof, wherein R represents a hydrogen atom, a hydroxy group optionally protected with a protecting group, etc., R1 represents a hydrogen atom or hydroxy-protecting group, and X represents an oxygen atom or a sulfur atom. The benzoazepine compound of the present invention and salts thereof have high solubility in water, and can be suitably used for injections.

Abstract: The present invention refers to compounds that, in addition to enhancing the sensitivity to acetylcholine and choline, and their exogenous agonists, of neuronal cholinergic receptors and/or acting as cholinesterase inhibitors and/or neuroprotective agents, have enhanced blood-brain barrier permeability in comparison to their parent compounds. The compounds are derived (either formally by their chemical structure or directly by chemical synthesis) from natural compounds belonging to the class of amaryllidaceae alkaloids e.g., galantamine, narwedine and lycoramine, or from metabolites of said compounds. The compounds of the present invention can either interact as such with their target molecules, or they can act as “pro-drugs”, in the sense that after reaching their target regions in the body they are converted by hydrolysis or enzymatic attack to the original parent compound and react as such with their target molecules, or both. The compounds of this invention may be used as medicaments.

Abstract: The present invention provides a production method of an allylic amine represented by the formula (III): wherein R3 is as defined in the specification, which comprises reacting by an allylic alcohol represented by the formula (II): wherein R3 is as defined in the specification, with sulfamic acid, in the presence of a phosphoramidite ligand represented by the formula (I): wherein each symbol is as defined in the specification, and an iridium complex. According to the present invention, a primary allylic amine can be produced directly from an allylic alcohol, without use of an activator for an allylic alcohol and conversion of an allylic alcohol into an activated compound thereof.

Abstract: The invention encompasses a series of pyrimidinone compounds which inhibit HIV integrase and thereby prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS. The invention also encompasses intermediates useful for making the pyrimidone compounds. Additionally, pharmaceutical compositions and methods for treating those infected with HIV are encompassed.

Abstract: The invention is directed to compositions and methods useful for treating Central Nervous System (CNS) disorders. Furthermore, the invention provides compositions and methods of treating sleep disorders. More specifically, the invention is directed to the compositions and use of derivatized, histamine antagonists for the treatment of sleep disorders.

Abstract: The present invention provides methods for the preparation of {2-[(8,9)-dioxo-2,6-diaza-bicyclo[5.2.0]-non-1(7)-en-2-yl]ethyl}phosphonic acid, and esters thereof.

Abstract: Compounds of formula (I) or pharmaceutically acceptable salts thereof are provided: wherein: A is alkylenyl of 1 to 4 carbon atoms, or alkenylenyl of 2 to 4 carbon atoms; R1 and R2 are, independently, hydrogen or a C5 to C7 aryl optionally substituted with 1 to 2 substituents, independently, selected from the group consisting of —C(O)R3, halogen, cyano, nitro, hydroxyl, C1-C6 alkyl, and C1-C6 alkoxy, with the proviso that at least one of R1 and R2 is not hydrogen; R3 is, independently, hydrogen, —OR4, alkyl, aryl, or heteroaryl; R4 is hydrogen, alkyl, aryl, or heteroaryl; R5 and R6 are, independently, hydrogen, alkyl, hydroxyl, alkoxy, or C5 to C7 aryl; wherein any R3 to R6 group having an aryl or heteroaryl moiety can optionally be substituted on the aryl or heteroaryl moiety with 1 to about 5 substituents, independently, selected from the group consisting of halogen, cyano, nitro, hydroxyl, C1-C6 alkyl, and C1-C6 alkoxy.

Abstract: Compounds of formula (I) or pharmaceutically acceptable salts thereof are provided where at least one of R2 or R3 is not hydrogen. The compounds of the present invention are N-methyl-D-aspartate (NMDA) receptor antagonists and are useful in treating a variety of conditions present in a mammal that benefit from inhibiting the NMDA receptor.

Abstract: The invention encompasses a series bicyclic pyrimidinone compounds of Formula I which inhibit HIV integrase and prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS.

Abstract: Phosphine compounds represented by the following formula (1): 1

Abstract: The present invention relates to compounds of Formula (I): wherein A1 is methylene, ethylene or propylene group and A2 is N or CR5, or stereoisomeric forms, stereoisomeric mixtures, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of HCV NS3 protease, and to pharmaceutical compositions and diagnostic kits comprising the same, and methods of using the same for treating viral infection or as an assay standard or reagent.

Abstract: The present invention provides a compound having sPLA2 inhibiting activity. The compound represented by the formula (I): wherein R1 is (a) C1 to C20 alkyl, C2 to C20 alkenyl, C2 to C20 alkynyl, carbocyclic groups, heterocyclic groups or the like; R2 is CONH2 or CONHNH2; one of R3 and R4 is —(L2)-(acidic group) wherein L2 is a group connecting with an acid group and the length of the connecting groups 1 to 5 atoms, and the other is a hydrogen atom; its prodrug, their pharmaceutically acceptable salt, or solvate thereof.

Abstract: Novel compounds having activity as non-covalent inhibitors of urokinase and having activity in reducing or inhibiting blood vessel formation are provided. These compounds have at a group having a guanidino moiety or derivative thereof. These compounds are useful in vitro for monitoring plasminogen activator levels and in vivo in treatment of conditions which are ameliorated by inhibition of or decreased activity of urokinase and in treating pathologic conditions wherein blood vessel formation is related to a pathologic condition.

Abstract: The present invention relates to compounds of formula (I) wherein R1 and R2 are independently selected from C1-6alkyl; one of R4 and R5 is a group of formula (IA): R3, R6, R7, R8, R9, R10 and R11 and the other of R4 and R5 are as defined within, pharmaceutically acceptable salts, solvates, solvates of such salts and prodrugs thereof and there use as ileal bile acid transport (IBAT) inhibitors for the treatment of hyperlipidaemia. Processes for their manufacture and pharmaceutical compositions containing them are also described.

Abstract: A water-soluble reference standard is useful for immunoassays of a lipophilic drugs.

Abstract: Novel phospholipid derivatives of the General Formula I: 1

Abstract: The present invention relates to compounds of the formula I,

Abstract: Chiral ligands and transition metal complexes based on such chiral ligands useful in asymmetric catalysis are disclosed. The chiral ligands include chiral C1-C6 TunaPhos ligands. The ruthenium TunaPhos complex reduces ketones to the corresponding alcohols with 95-99.6% enantioselectivity. The transition metal complexes of the chiral ligands are useful in asymmetric reactions such as asymmetric hydrogenation, hydride transfer, hydrosilylation, hydroboration, hydrovinylation, hydroformylation, hydrocarboxylation, isomerization, allylic alkylation, cyclopropanation, Diels-Alder reaction, Heck reaction, isomerization, Aldol reaction, Michael addition and epoxidation reactions.