Abstract: The invention relates to pyrrolone compounds of the formula (I) wherein X, R1, R2, R3, Ra, Rb, Rc and Rd are as defined in the specification. Furthermore, the present invention relates to processes and intermediates for making compounds of formula (I), to herbicidal compositions comprising these compounds and to methods of using these compounds to control plant growth.

Abstract: Disclosed are compositions for stabilizing a source of active halogen in aqueous solution. The compositions comprise (i) at least one substituted N-hydrogen compound, such as 5,5-dimethylhydantoin, and (ii) at least one additional nitrogen compound selected from ammonia, ammonium salts, and nitrogen compounds containing no carbon-hydrogen bonds, the molar ratio of (i) and (ii) being in the range of 50:1 to 0.02:1. Active halogen-containing aqueous solutions stabilized by the above compositions are particularly useful for controlling microbial and planktonic growth in aqueous systems such as process liquids in the pulping or papermaking industry. The compositions are also useful in reducing the corrosivity of halogen-containing solutions.

Abstract: The invention provides processes for preparing intermediates useful for preparing compounds of the formula: or a salt thereof, where R1-3 are as defined in the specification.

Abstract: Provided are compounds, pharmaceutical compositions and methods of treating or preventing disorders associated with NMDA receptor activity, including schizophrenia, Parkinson's disease, cognitive disorders, depression, neuropathic pain, stroke, traumatic brain injury, epilepsy, and related neurologic events or neurodegeneration. Compounds of the general Formulas A-J, and pharmaceutically acceptable salts, esters, prodrugs or derivatives thereof are disclosed.

Abstract: The present invention relates to novel nucleic acid molecules, called aptamers, that bind specifically to a small molecule fluorophore and thereby enhance the fluorescence signal of the fluorophore upon exposure to radiation of suitable wavelength. Molecular complexes formed between the novel fluorophores, novel nucleic acid molecules, and their target molecules are described, and the use of multivalent aptamer constructs as fluorescent sensors for target molecules of interest are also described.

Abstract: The invention provides processes for preparing intermediates useful for preparing compounds of the formula: or a salt thereof, where R1-3 are as defined in the specification.

Abstract: Preparation of new heterocyclic compounds characterized by 1,3-imidazolidine structure useful for stereoselective synthesis of optically pure key intermediates in 1?-methylcarbapenem production.

Abstract: Disclosed are novel compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R1, R2, R3, R4 and X are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of treating cognitive or neurodegenerative diseases such as Alzheimer's disease. Also disclosed are methods of treating a cognitive or neurodegenerative disease comprising administering to a patient I need of such treatment a combination of at least one compound of formula I and at least one compound selected from the group consisting of ?-secretase inhibitors other than those of formula I, HMG-CoA reductase inhibitors, gamma-secretase inhibitors, non-steroidal anti-inflammatory agents, N-methyl-D-aspartate receptor antagonists, cholinesterase inhibitors and anti-amyloid antibodies.

Abstract: The invention encompasses ureido substituted benzoic acid compounds, compositions comprising the compounds and methods for treating or preventing diseases associated with nonsense mutations of mRNA by administering these compounds or compositions.

Abstract: Disclosed is a method for producing precursors for 2-[18F]fluorophenylalanine and 6-[18F]fluoro-L-meta-tyrosine and the ?-methylated derivatives thereof, to the precursor, and to a method for producing 2-[18F]fluorophenylalanine and 6-[18F]fluoro-L-meta-tyrosine and the ?-methylated derivatives thereof from particular precursor. A compound of formula (3) is provided which enables an automated synthesis of L-3,4-dihydroxy-6-[18F]fluorophenylalanine and 6-[18F]fluoro-L-meta-tyrosine. The enantiomeric purity of the product is ?98%.

Abstract: The present invention relates to peptidomimetic compounds useful as protease inhibitors, particularly as serine protease inhibitors and more particularly as hepatitis C NS3 protease inhibitors; intermediates thereto; their preparation including novel steroselective processes to intermediates. The invention is also directed to pharmaceutical compositions and to methods for using the compounds for inhibiting HCV protease or treating a patient suffering from an HCV infection or physiological condition related to the infection. Also provided are pharmaceutical combinations comprising, in addition to one or more HCV serine protease inhibitors, one or more interferons exhibiting anti-HCV activity and/or one or more compounds having anti HCV activity and a pharmaceutically acceptable carrier, and methods for treating or preventing a HCV infection in a patient using the compositions. The present invention is also directed to a kit or pharmaceutical pack for treating or preventing HCV infection in a patient.

Abstract: The invention provides processes for preparing intermediates useful for preparing compounds of the formula: or a salt thereof, where R1-3 are as defined in the specification.

Abstract: Phenyliodonium ylide derivatives substituted with electron donating as well as electron withdrawing groups on the aromatic ring are shown for use as precursors in aromatic nucleophilic substitution reactions. The iodonium ylide group is substituted by nucleophiles such as halide ions to provide the corresponding haloaryl derivatives. No-carrier-added [F-18]fluoride ion exclusively substitutes the iodonium ylide moiety in these derivatives and provides high specific activity F-18 labeled fluoro derivatives. Protected L-dopa-6-iodonium ylide derivative have been synthesized as a precursors for the preparation of no-carrier-added 6-[F-18]fluoro-L-dopa. The iodonium ylide group in this L-dopa.derivative is nucleophilically substituted by no-carrier-added [F-18]fluoride ion to provide a [F-18]fluoro intermediates which upon acid hydrolysis yielded 6-[F-18]fluoro-L-dopa.

Abstract: Provided are compounds, pharmaceutical compositions and methods of treating or preventing disorders associated with NMDA receptor activity, including schizophrenia, Parkinson's disease, cognitive disorders, depression, neuropathic pain, stroke, traumatic brain injury, epilepsy, and related neurologic events or neurodegeneration. Compounds of the general Formulas A-J, and pharmaceutically acceptable salts, esters, prodrugs or derivatives thereof are disclosed.

Abstract: The present invention relates to a phosphodiesterase type III (PDE III) inhibitor and/or Ca2+- sensitizing agent or a pharmaceutically acceptable derivative thereof for the treatment of a patient suffering from hypertrophic cardiomyopathy (HCM). According to another aspect the present invention relates to the use of a PDE III inhibitor and/or Ca2+-sensitizing agent for the preparation of a medicament for the treatment of a patient suffering from HCM.

Abstract: The invention pertains to a compound generating an acid of the formula I or II, for instance corresponding sulfonium and iodonium salts, as well as corresponding sulfonyloximes wherein X is CH2 or CO; Y is O, NR4, S, O(CO), O(CO)O, O(CO)NR4, OSO2, O(CS), or O(CS)NR4; R1 is for example C1-C18alkyl, C1-C10haloalkyl, C2-C12alkenyl, C4-C30cycloalkenyl, phenyl-C1-C3-alkyl, C3-C30cycloalkyl, C3-C30cycloalkyl-C1-C18alkyl, interrupted C2-C18alkyl, interrupted C3-C30cycloalkyl, interrupted C3-C30cycloalkyl-C1-C18alkyl, interrupted C4-C30cycloalkenyl, phenyl, naphthyl, anthracyl, phenanthryl, biphenylyl, fluorenyl or heteroaryl, all unsubstituted or are substituted; or R1 is NR12R13; R2 and R3 are for example C3-C30cycloalkylene, C3-C30cycloalkyl-C1-C18alkylene, C1-C18alkylene, C1-C10haloalkylene, C2-C12alkenylene, C4-C30cycloalkenylene, phenylene, naphthylene, anthracylene, phenanthrylene, biphenylene or heteroarylene; all unsubstituted or substituted; R4 is for example C3-C30cycloalkyl, C3-C30cycloalkyl-C1-C18al

Abstract: A preparation method of (4S,5R)-semiester in which cycloanhydride conducts enantioselective ring-opening with alcohol in the presence of 9-epiquininurea. With this method, (4S,5R)-semiester is prepared at room temperature with high yield and high stereoselectivity.

Abstract: The objective of the present invention is to provide an optically active imidazolidinone derivative widely usable for synthesizing an optically active amino acid, a method of easily producing the derivative, and a method of easily producing an optically active amino acid by using the derivative. The objective can be achieved by producing an optically active amino acid using a novel optically active imidazolidinone derivative represented by a general formula (3) and the like. According to the method of the present invention, an optically active imidazolidinone derivative can be obtained by preferential crystallization from a mixture of isomers of the imidazolidinone derivative. Therefore, an optically active amino acid can be easily and stereoselectively produced without cumbersome procedures required for the conventional methods, such as resolution of diastereomers, synthesis from an optically active amino acid and resolution of isomers by silica gel column chromatography.

Abstract: The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof: The compounds or salts modulate P2X7 receptor function and are capable of antagonizing the effects of ATP at the P2X7 receptor (P2X7 receptor antagonists). The invention also provides the use of such compounds or salts, or pharmaceutical compositions thereof, in the treatment or prevention of disorders/diseases mediated by the P2X7 receptor, for example pain, inflammation or a neurodegenerative disease, in particular pain such as inflammatory pain, neuropathic pain or visceral pain.

Abstract: The invention encompasses ureido substituted benzoic acid compounds, compositions comprising the compounds and methods for treating or preventing diseases associated with nonsense mutations of mRNA by administering these compounds or compositions.

Abstract: Preparation of new heterocyclic compounds characterised by 1,3-imidazolidine structure useful for stereoselective synthesis of optically pure key intermediates in 1?-methylcarbapenem production

Abstract: A compound of the formula is disclosed as an HIV protease inhibitor. Methods and compositions for inhibiting an HIV infection are also disclosed.

Abstract: Disclosed is a method for producing precursors for L-3,4-dihydroxy-6-[18F]fluorophenylalanine and 2-[18F]fluoro-L-tyrosine and the ?-methylated derivatives thereof, the precursor, and to a method for producing L-3,4-dihydroxy-6-[18F]fluorophenylalanine and 2-[18F]fluoro-L-tyrosine and the ?-methylated derivatives thereof from the precursor. A compound of formula (3) is provided which enables automated synthesis of L-3,4-dihydroxy-6-[18F]fluorophenylalanine and 2-[18F]fluoro-L-tyrosine. The enantiomeric purity of the product is ?98%.

Abstract: Disclosed is a method for producing precursors for 2-[18F]fluorophenylalanine and 6-[18F]fluoro-L-meta-tyrosine and the ?-methylated derivatives thereof, to the precursor, and to a method for producing 2-[18F]fluorophenylalanine and 6-[18F]fluoro-L-meta-tyrosine and the ?-methylated derivatives thereof from particular precursor. A compound of formula (3) is provided which enables an automated synthesis of L-3,4-dihydroxy-6-[18F]fluorophenylalanine and 6-[18F]fluoro-L-meta-tyrosine. The enantiomeric purity of the product is ?98%.

Abstract: Hexamethylphosphoramide (HMPA) was added to a reaction vessel containing (R)-1,1?-binaphthyl-2,2?-dithiol and potassium hydroxide. The vessel was purged with oxygen and stirred at 80° C. for 5 days under 7 atmospheres of oxygen. After being cooled to room temperature, the reaction product was purified to yield potassium (R)-1,1?-binaphthyl-2,2?-disulfonate. The (R)-1,1?-binaphthyl-2,2?-disulfonic acid obtained from the disulfonate and 2,6-diphenylpyridine were stirred in acetonitrile, and then the solvent was evaporated under reduced pressure. Subsequently, magnesium sulfate and distilled CH2Cl2 were added to the reaction product, and the mixture was stirred at room temperature for 30 minutes. The resulting solution was cooled to 0° C. Benzaldehyde imine whose nitrogen is protected with Cbz and subsequently acetyl acetone were dropped into the solution over a period of 1 hour. The resulting mixture was further stirred at 0° C. for 30 minutes.

Abstract: The present invention is to provide a process for preparing a synthetic intermediate of biotin which is industrially advantageous, and discloses a process for preparing a compound represented by the formula (I): 1 wherein R1 and R2 may be the same or different from each other, and each represents hydrogen atom, a benzyl group which may have a substituent(s) on the benzene ring, a benzhydryl group which may have a substituent(s) on the benzen ring, or a trityl group which may have a substituent(s) on the benzene ring, R3 represents cyano group, carboxyl group, an alkoxycarbonyl group, an alkylthiocarbonyl group, or a carbamoyl group which may have a substituent, or a salt thereof which comprises subjecting a compound represented by the formula (II-a): 2 wherein the symbols have the same meanings as defined above, or a salt thereof to ring transformation.

Abstract: The present invention provides compounds having formula (I): or pharmaceutically acceptable salts and N-oxides thereof, wherein the subscript m is an integer from 0-4; Ar is an optionally substituted aryl; B is an optionally substituted aryl; L1 is an optionally substituted linking group selected from the group consisting of C1-4 alkylene, C1-4 heteroalkylene, C2-4 alkenylene and —CH2N(Ru)X5—; and L2 is a bond or C1-3 alkylene. The compounds act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity.

Abstract: The present invention relates to peptidomimetic compounds useful as protease inhibitors, particularly as serine protease inhibitors and more particularly as hepatitis C NS3 protease inhibitors; intermediates thereto; their preparation including novel steroselective processes to intermediates. The invention is also directed to pharmaceutical compositions and to methods for using the compounds for inhibiting HCV protease or treating a patient suffering from an HCV infection or physiological condition related to the infection. Also provided are pharmaceutical combinations comprising, in addition to one or more HCV serine protease inhibitors, one or more interferons exhibiting anti-HCV activity and/or one or more compounds having anti HCV activity and a pharmaceutically acceptable carrier, and methods for treating or preventing a HCV infection in a patient using the compositions. The present invention is also directed to a kit or pharmaceutical pack for treating or preventing HCV infection in a patient.

Abstract: The invention relates to a salt of an ACE inhibitor dicarboxylic acid with an organic amine and/or an alkali compound, a transdermal therapeutic system comprising the salt, and a method of producing the transdermal therapeutic system.

Abstract: Imidazole derivatives, compositions containing them, methods of preparing them, including regioselective scale-up synthetic methods, and methods of using them.

Abstract: Insecticidal sulfoximines are produced efficiently and in high yield by the oxidation of the corresponding sulfilimine with ruthenium tetraoxide or an alkali metal permanganate.

Abstract: Compounds of formula (I): (A)m·(B)n??(I) wherein A represents an angiotensin-converting enzyme inhibitor compound containing at least one salt-forming basic function, B represents a compound containing at least one salt-forming acid function and at least one NO donor group, m represents the number of acid functions of B that have been converted to a salt and n represents the number of basic functions of A that have been converted to a salt, the bond or bonds between A and B being of the ionic type. Medicinal products containing the same which are useful in treating cardiovascular pathologies.

Abstract: The invention describes compositions and kits comprising at least qrie organic nitric oxide enhancing salt of an angiotensin converting enzyme inhibitor, and, optionally, at least one nitric oxide enhancing compound and/or at least one therapeutic agent. The invention also provides methods for (a) treating cardiovascular diseases; (b) treating renovascular diseases; (c) treating diabetes; (d) treating diseases resulting from oxidative stress; (e) treating endothelial dysfunctions; (f) treating diseases caused by endothelial dysfunctions; (g) treating cirrhosis; (h) treating pre-eclampsia; Q) treating osteoporosis; (k) treating nephropathy; (l) treating peripheral vascular diseases; (m) treating portal hypertension; (n) treating ophthalmic disorders; (o) treating metabolic syndrome; and (p) treating hyperlipidemia.

Abstract: Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are generally monocyclic and bicyclic compounds and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated diseases, and as controls in assays for the identification of competitive CCR1 antagonists.

Abstract: The invention relates to new substituted imidazoles of general formula wherein R1 to R3 and X are defined as claims, the tautomers, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, and processes for preparing them and their use as intermediates for preparing pharmaceutical compositions or pesticides.

Abstract: The present invention is directed to compounds of the formula or pharmaceutically acceptable salts, prodrug, solvate or optical isomer thereof, pharmaceutical compositions containing same and use thereof for treating diseases linked to disregulated cell proliferation or to disregulated protein kinase.

Abstract: The invention relates to novel 2-Oxy, 2-Amino, and 2-Thio-imidazole compounds of formula (I): wherein all variables are as herein defined, pharmaceutical compositions containing the compounds and methods of using them in the treatment of neurological disorders and other disorders and conditions mediated by the histamine H3 receptor.

Abstract: The present invention relates to methods for the synthesis of chiral non-racemic products, e.g., enantiomerically-enriched hemiesters, from prochiral starting materials, e.g., meso anhydrides. The present invention also relates to catalysts for the aforementioned methods, and methods for synthesizing these catalysts.

Abstract: The present invention relates to novel trifluorobutenyl imidazole thioether derivatives of the following formula (I) wherein R1 represents hydrogen or halogen, R2 represents hydrogen, halogen or alkoxycarbonyl, R3 represents hydrogen, alkyl, alkenyl, cycloalkyl or aralkyl, and n represents 0,1 or 2, with the proviso that R1, R2 and R3 do not all represent hydrogen at the same time, to a process for their preparation and to their use as nematicides.

Abstract: The invention relates to a method for selectively dissociating cyclic carboxylic acid anhydrides. According to the inventive method, a chiral amino alcohol with a tertiary amino group that may have a partially or completely bridged structure is used as the chiral auxiliary reagent.

Abstract: The invention provides novel thiazoles bearing 3-pyridyl or 4-isoquinilinyl substituents, and pharmaceutical compositions thereof. The invention also provides methods of using compounds of the invention and pharmaceutical compositions thereof as inhibitors of lyases, e.g., the 17a-hydroxylase-C17,20 enzyme. The invention further provides methods for treating cancer in a subject, comprising administering to the subject a compound of the invention or a pharmaceutical composition thereof. The cancer can be, e.g., prostate cancer or breast cancer.

Abstract: A novel achiral biaryl-type compound and a circular dichroism(CD) color fixing agent are provided. Furthermore, a method for determining an absolute configuration of a chiral compound is carried out by introducing the above achiral biaryl-type compound into the chiral compound.

Abstract: There is provided a process for preparing a pharmacologically acceptable salt of N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanyl-amino acid which comprises condensing an amino acid and N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanine.N-carboxyanhydride under basic condition, carrying out decarboxylation under between neutral and acidic condition to obtain N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanyl-amino acid, and forming a pharmacologically acceptable salt thereof, wherein the production of a by-product (3): is suppressed by carrying out in an aqueous liquid a series of operations till formation of the pharmacologically acceptable salt or till isolation of the pharmacologically acceptable salt. The present invention enables to prepare the pharmacologically acceptable salt of N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanyl-amino acid having high quality, in a commercial scale with high yield and economical efficiency.

Abstract: A composition comprising: (a) from 0.1% to 20% of at least one compound comprising: (i) a five-, six-, or seven-membered ring containing a thiourea functional group; and (ii) at least one of (A) a carbocyclic ring system fused to the five-, six-, or seven-membered ring; and (B) an aryl, aralkyl, C4-C22 alkyl or C4-C22 alkenyl group attached to a ring carbon atom of the five-, six-, or seven-membered ring; and (b) a lubricating oil.

Abstract: A new class of imidazolines as 4-position acids or esters with very potent anti-inflammatory as well as antimicrobial activity is described. The synthesis of these imidazolines includes a multicomponent reaction applicable to a combinatorial synthetic approach. The combination of these two key characteristics provides an effective therapeutic drug in the treatment of septic shock as well as many other inflammatory (arthritis and asthma) and infectious disorders. The use of this novel class of non-steroidal agents as anti-inflammatory agents (for the treatment of asthma, etc.), antibacterial agents, and antiseptic agents is described. The compounds are also useful in the treatment of tumors (such as cancers). The imidazolines are potent inhibitors of the transcription factor NF-&kgr;B as well as potent activity against the Gram (+) bacterium. The compositions are also useful for treating autoimmune diseases and for inhibiting rejection of organ and tissue transplants.

Abstract: A new class of imidazolines as 4-position acids or esters with very potent anti-inflammatory as well as antimicrobial activity is described. The synthesis of these imidazolines includes a multicomponent reaction applicable to a combinatorial synthetic approach. The combination of these two key characteristics provides an effective therapeutic drug in the treatment of septic shock as well as many other inflammatory (arthritis and asthma) and infectious disorders. The use of this novel class of non-steroidal agents as anti-inflammatory agents (for the treatment of asthma etc.), antibacterial agents and antiseptic agents is described. The compounds are also useful in the treatment of tumors (such as cancers). The imidazolines are potent inhibitors of the transcription factor NF-&kgr;B as well as potent activity against the Gram (+) bacterium B. subtillus and B. cereus with MIC values in the range of 50 &mgr;m/mL.

Abstract: The invention relates to compounds of formula (I) in which the symbols have the meanings given in the claims. Said compounds are inhibitors of the sodium-dependent bicarbonate/chloride ion exchanger which can be used as medicines for the prophylaxis or treatment of a wide range of diseases, for example the treatment and/or prophylaxis of myocardial infarction, angina pectoris, diseases caused by ischaemia, impaired respiration, cardiac ischaemia, ischaemia of the peripheral and central nervous system and stroke, ischaemia of the peripheral organs and limbs and diseases in which cell proliferation is a primary or secondary cause, in the treatment of shock, during surgical interventions and organ transplants or for preserving and storing transplants to be used in surgical interventions.

Abstract: The present invention relates generally to a novel class of imidazolidinones of Formula (I): 1

Abstract: The present invention is directed to peptidomimetic macrocyclic compounds which inhibit prenyl-protein transferase and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting prenyl-protein transferase and the prenylation of the oncogene protein Ras.

Abstract: Compounds of the formula: are disclosed which have activity as inhibitors of binding between VCAM-1 and cells expressing VLA-4. Such compounds are useful for treating diseases whose symptoms and/or damage are related to the binding of VCAM-1 to cells expressing VLA-4.