Abstract: The present invention relates to substituted pyrazoles, compositions containing such compounds and methods of treatment The compounds are glucagon receptor antagonists and thus are useful for treating, preventing or delaying the onset of type 2 diabetes mellitus.

Abstract: The present invention relates to a compound of the formula (1): wherein R1 is group of the formula (2): (wherein X is nitrogen atom or C(R5), Y is nitrogen atom or C(R6), R5 and R6 are each independently hydrogen atom, etc.) etc., m is 1 to 6, L1 is single bond, etc., R2 is hydrogen atom, substituted or unsubstituted alkyl group, etc., R3 is hydrogen atom, etc., L2 is single bond, etc., R4 is hydrogen atom, substituted or unsubstituted aryl group, etc., or pharmaceutically acceptable salt thereof, being useful for preventing or treating Alzheimer's disease.

Abstract: The present invention pertains to certain compounds of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A serotonin receptor. Compounds and pharmaceutical compositions thereof are directed to methods useful in the treatment of platelet aggreagation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, blood clot formation, asthma or symptoms thereof, agitation or a symptom thereof, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorder, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, and sleep disorders, sleep disorders, diabetic-related disorders, progressive multifocal leukoencephalopathy and the like.

Abstract: The invention relates to non-peptidic molecules which modulate, especially inhibit, the interaction of protein kinase A (PKA) and A kinase anchor proteins (AKAP) and to a host or target organism that comprises said non-peptidic compounds or recognition molecules directed to said compounds, such as e.g. antibodies or chelating agents. The invention also relates to a pharmaceutical agent, especially for use in the treatment of diseases that are associated with a disturbance of the cAMP signal path, especially insipid diabetes, hypertonia, pancreatic diabetes, duodenal ulcer, asthma, heart failure, obesity, AIDS, edema, hepatic cirrhosis, schizophrenia and others. The invention also relates to the use of the inventive molecules.

Abstract: The present invention is directed to 2-phenyl-indole compounds, their preparation, pharmaceutical compositions containing these compounds, and their pharmaceutical use in treating a patient suffering from a PGD2-mediated disorder including, but not limited to, allergic disease (such as allergic rhinitis, allergic conjunctivitis, atopic dermatitis, bronchial asthma and food allergy), systemic mastocytosis, disorders accompanied by systemic mast cell activation, anaphylaxis shock, bronchoconstriction, bronchitis, eczema, urticaria diseases accompanied by itch (such as atopic dermatitis and urticaria), diseases (such as cataract, retinal detachment, inflammation, infection and sleeping disorders) which are generated secondarily as a result of behavior accompanied by itch (such as scratching and beating), inflammation, chronic obstructive pulmonary diseases, ischemic reperfusion injury, cerebrovascular accident, chronic rheumatoid arthritis, pleurisy, ulcerative colitis and the like.

Abstract: Disclosed is a compound useful as a type I 11?hydroxysteroid dehydrogenase inhibitor. A compound represented by the formula: a pharmaceutically acceptable salt or solvate thereof, wherein R1 is optionally substituted alkyl or the like, one of R2 and R4 is a group of formula: —Y—R5, wherein Y is —O— or the like, R5 is substituted alkyl (the substituent is optionally substituted cycloalkyl or the like), optionally substituted branched alkyl or the like, the other of R2 and R4 is hydrogen or optionally substituted alkyl, R3 is a group of formula: —C(?O)-Z-R6, wherein Z is —NR7— or —NR7—W—, R6 is optionally substituted cycloalkyl or the like, R7 is hydrogen or optionally substituted alkyl, W is optionally substituted alkylene, X is ?N— or the like, with the proviso that compounds wherein R2 is 2-(morphorino)ethoxy, R3 is N-(1-adamantyl)carbamoyl and R1 is benzyl are excluded.

Abstract: Disclosed herein is a compound having a structure or a pharmaceutically acceptable salt, or a prodrug thereof. Therapeutic methods, compositions, and medicaments related thereto are also disclosed.

Abstract: The present invention discloses novel compounds of Formula (I), or pharmaceutically acceptable salts thereof, which have glucagon receptor antagonist or inverse agonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula (I) as well as methods of using them to treat diabetic and other glucagon related metabolic disorders, and the like.

Abstract: The present invention discloses monomers of structure (IV) wherein “X” is an alkyl, aryl, or oligoether group, and “R” is an alkyl, aryl, or oligoether group that is chemically bonded to the N1 or N2 position of each of the tetrazole rings. The monomers of the present invention are suitable as binders in energetic compositions.

Abstract: Compounds of formula (I): wherein Ar, X, R1, R2, R3 and R4 are as defined herein. The compounds are useful as reverse transcriptase inhibitors against wild type and single or double mutant strains of HIV.

Abstract: A novel class of compounds, which act to antagonize the action of the glucagon hormone on the glucagon receptor. Owing to their antagonizing effect of the glucagon receptor the compounds may be suitable for the treatment and/or prevention of any glucagon-mediated conditions and diseases such as hyperglycemia, Type 1 diabetes, Type 2 diabetes and obesity.

Abstract: The invention provides small molecule mimics of the Smac peptide that are dimer-like or trimer-like compounds having two or three amide-containing domains connected by a linker. These compounds are useful to promote apoptosis. The invention includes pharmaceutical compositions comprising such compounds and methods to use them to treat conditions including cancer and autoimmune disorders.

Abstract: Compounds of formula (I): wherein Ar, X, R1, R2, R3 and R4 are as defined herein. The compounds are useful as reverse transcriptase inhibitors against wild type and single or double mutant strains of HIV.

Abstract: A salt molten at room temperature that does not contain any organic solvent, excelling in stability; and a display device that is improved in the durability in high-temperature environment by virtue of the use thereof. There is provided a salt molten at room temperature characterized by being composed of a silver salt and any of compounds of the following general formula (I) or general formula (II).

Abstract: The present invention provides a cleaning agent for cleaning a semiconductor device having copper wiring on the surface thereof following a chemical mechanical polishing process in a production process of a semiconductor device, including a compound represented by the following formula (I): X1-L—X2??formula (I) wherein, in formula (I), X1 and X2 each independently represent a monovalent substituent formed by removing one hydrogen atom from a heterocycle containing at least one nitrogen atom, and L represents a divalent linking group; and provides a cleaning method using the cleaning agent.

Abstract: Disclosed herein are novel compositions and methods for treating or preventing a variety of disorders and conditions associated with lipid metabolism. The methods generally include administering to a patient in need thereof a therapeutically effective amount of a pharmaceutical composition comprising one or more fibric acid or statin derivative compositions alone or in combination with one or more lipid altering agents and/or PDE inhibitors.

Abstract: The present invention relates to a compound of the general formula (1): wherein, Y is a methylene group, and the like; A is an optionally substituted heterocyclic group, and the like; B is an optionally substituted heterocyclic group, and the like; R1 is an optionally substituted alkyl group, wherein the alkyl group further may optionally be substituted by an optionally substituted homocyclic group, and the like; and R2 is an optionally substituted amino group, and the like; or a pharmaceutically acceptable derivative thereof, which has an inhibitory activity against cholesteryl ester transfer protein (CETP), thereby being useful for prophylaxis and/or treatment of arteriosclerotic diseases, hyperlipemia or dyslipidemia, and the like.

Abstract: An organophotoreceptor that includes: (a) a charge transport material having the formula wherein A is selected from heterocyclic groups, naphthyl group, alkylsulfonylphenyl, stilbenyl or the group X, wherein X is represented by the formula B is selected from hydrogen, alkyl group, and an aryl group, with the proviso that when A is naphthyl, B is naphthyl; or where R1 is selected from the group consisting of N-pyrrolyl, N-pyrazolyl, N-tetrazolyl, N-indolyl, N-carbazolyl, N-triazolyl, N-imidazolyl, N-benzimidazolyl, N-indazolyl, and N-benzotriazolyl group, and R3 is a 9-fluorenone group. (b) a charge generating compound; and (c) an electrically conductive substrate.

Abstract: The present invention is directed to compounds which are potentiators of metabotropic glutamate receptors, including the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.

Abstract: The present invention relates to a silver halide color photographic light-sensitive material wherein at least one of light-sensitive silver halide emulsion layers includes a silver halide emulsion having a silver chloride content of at least 95 mol % and a silver iodide content of 0.05 mol % to 0.75 mol % and/or a silver bromide content of 0.05 mol % to 4.00 mol % and further at least one compound represented by the following formula (I): X-(L)n-Y ??Formula (I) wherein X represents a group adsorptive to a silver halide, L represents a divalent connecting group comprising one of an atom and an atomic group including at least one of a carbon atom, a nitrogen atom, a sulfur atom and an oxygen atom, Y denotes a reducible group and n denotes an integer of 0 or 1.

Abstract: The present invention provides Bis-(1(2)H-tetrazol-5-YL)-amine compound, and safe and inexpensive methods for producing high quality Bis-(1(2)H-tetrazol-5-YL)-amine compound. Also provided are Bis-(1(2)H-tetrazol-5-YL)-amine intermediates, and methods for their preparation. The process of preparing Bis-(1(2)H-tetrazol-5-YL)-amine intermediate substantially combines dicyanamide salt, azide salt, solvent and acid at 40-70 C temperature. The process of preparing Bis-(1(2)H-tetrazol-5-YL)-amine anhydride and/or Bis-(1(2)H-tetrazol-5-YL)-amine monohydrate comprises heating the intermediate described above at ?75 C and adding a second acid.

Abstract: Lead-free primary explosives of the formula [MII(A)R(BX)S](CY)T, where A is 1,5-diaminotetrazole, and syntheses thereof are described. Substantially stoichiometric equivalents of the reactants lead to high yields of pure compositions thereby avoiding dangerous purification steps.

Abstract: Certain novel phenyl substituted cyclic urea derivatives have unexpected insecticidal activity. These compounds are represented by formula I: where A, B a, D, b, E, G, c, d, J, X and R through R10, inclusively, are fully described herein. In addition, compositions comprising an insecticidally effective amount of at least one compound of formula I, and optionally, an effective amount of at least one of a second compound, with at least one insecticidally compatible carrier are also disclosed; along with methods of controlling insects comprising applying said compositions to a locus where insects are present or are expected to be present.

Abstract: A novel compound, used for example, as a gas generating fuel, is defined as a compound having the structural formula of R3—R1—R2, wherein R1 is a urea group, R2 is a tetrazolyl group with a C—N bond to the urea group, and R3 may be defined as a non-tetrazolyl, triazolyl, heterocyclic, heterocyclic amine, aliphatic, aliphatic amine, aryl, alkyl, hydrogen, or nitrogen group linked to the free nitrogen on the urea group. A method of making the compound is also provided. A gas generating composition 12 containing the novel compound as a fuel, and an oxidizer is also provided. The novel compound may be contained within a gas generant composition 12, within a gas generator 10. The gas generator 10 may be contained within a gas generating system such as an airbag inflator 10 or seat belt assembly 150, or more broadly within a vehicle occupant protection system 180.

Abstract: A dibenzylamine compound represented by the formula (1) wherein R1 and R2 are each a C1-6 allyl group optionally substituted by halogen atoms and the like; R3, R4 and R5 are each a hydrogen atom, a halogen atom and the like, or R3 and R4 may form, together with carbon atoms bonded thereto, a homocyclic or heterocyclic ring optionally having substituent(s); A is —N(R7)(R8) and the like; ring B is an aryl group or a heterocyclic residue; R6 is a hydrogen atom, a halogen atom, a nitro group, a C1-6 allyl group and the like; n is an integer of 1 to 3, a prodrug thereof and a pharmaceutically acceptable salt thereof show selective and potent CETP inhibitory activity, and therefore, they can be provided as therapeutic or prophylactic agents for hyperlipidemia or arteriosclerosis and the like.

Abstract: The present invention provides compounds capable of binding to an Fc receptor and modulating Fc receptor activity comprising a core lipophilic group in the form of an Aryl zing substituted with a group rich in p-electrons. The invention further provides for a method of treating an autoimmune disease involving Fc receptor activity using such compounds. A method for obtaining a compound which modulates Fc receptor activity is also provided, the method comprising: (a) providing or designing compounds having structural characteristics to fit in the groove of the Fc?RIIa structure; and (b) screening the compounds for modulating activity on the Fc receptor.

Abstract: The invention is concerned with novel heteroarylacetamides of formula (I) Rd—C(O)—N(Re)—Rc—CH2—C(O)—N(Ra)(Rb)??(I) wherein Ra to Re are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit the coagulation factor Xa and can be used as medicaments.

Abstract: There are described cycloalkyl derivatives of the formula (I) R1—Y-A-B-D-E-F-G??(I) in which R1, Y, A, B, D, E, F and G have the meaning indicated herein, their preparation and their use as medicaments. The compounds according to the invention can be used as vitronectin receptor antagonists and as inhibitors of bone resorption.

Abstract: The present invention provides an improved phosphoramidite activator comprising a solution of 5-benzylmercaptotetrazole in acetonitrile and N-alkyimidazole. Further provided are improved methods of oligonucleotide synthesis wherein a phosphoramidite activator comprising a solution of 5-benzylmercaptotetrazole in acetonitrile and N-alkyimidazole is used to prepare internucleoside linkages.

Abstract: Caspase activity and apoptosis are promoted using active, dimeric Smac peptide mimetics of the general formula M1-L-M2, wherein moieties M1 and M2 are monomeric Smac mimetics and L is a covalent linker. Target cancerous or inflammatory cells are contacted with an effective amount of an active, dimeric Smac mimetic, and a resultant increase in apoptosis of the target cells is detected. The contacting step may be effected by administering to a pharmaceutical composition comprising a therapeutically effective amount of the dimeric mimetic, wherein the individual may be subject to concurrent or antecedent radiation or chemotherapy for treatment of a neoproliferative pathology.

Abstract: The present invention encompasses compounds or Formula (I): as well as the pharmaceutically acceptable salts and hydrates thereof. The compounds are useful for treating immune mediated diseases and conditions, such as bone marrow, organ and tissue transplant rejection. Pharmaceutical compositions and methods of use are included.

Abstract: The present invention is directed to the field of substituted tetrazole synthesis and manufacture. More particularly, the present invention is directed to processes for preparing substituted tetrazoles and tetrazolate salts, such as sodium nitrotetrazolate and sodium cyanotetrazolate, using small scale and/or microreactor techniques. The use of the present techniques result in less hazardous and more efficient manufacturing processes.

Abstract: The invention relates to substituted N-cyclohexylheterocycles and to the physiologically tolerated salts and physiologically functional derivatives thereof, to processes for their preparation and to their use as medicaments. Compounds of the formula I, in which the radicals have the stated meanings, and the physiologically tolerated salts thereof, and process for their preparation are described. The compounds bring about for example a weight reduction in mammals and are suitable for example for the prevention and treatment of obesity and diabetes.

Abstract: The present invention encompasses compounds of Formula (I): as well as the pharmaceutically acceptable salts and hydrates thereof. The compounds are useful for treating immune mediated diseases and conditions, such as bone marrow, organ and tissue transplant rejection. Pharmaceutical compositions and methods of use are included.

Abstract: An organophotoreceptor that includes: (a) a charge transport compound having the formula where n is an integer between 2 and 6, inclusive; R1 is an aryl group; R2 is a sulfolanyl group; a pyrrolyl group; a tetrazolyl group; a benzotriazolyl group; a stilbenyl group; an alkylsulfonylphenyl group, an arylsulfonylphenyl; a pyrazolyl group; or group A, where A is with the proviso that when R2 is an alkylsulfonylphenyl group or an arylsulfonylphenyl, R1 may be hydrogen, an alkyl group, or an aryl group; X is an alkylene linking group as described in the specification; and Y is a bond, C, N, O, S, a —(CH2)p— group where p is an integer between 0 and 10, an aryl group, a cycloalkyl group, a cyclosiloxyl, a heterocyclic group, or a CR7 group where R7 is H, alkyl group, or aryl group; (b) a charge generating compound; and (c) an electrically conductive substrate.

Abstract: This invention relates to novel N-linked sulfonamides of N-heterocyclic carboxylic acid and carboxylic acid isosteres, their preparation, and use for treating neurological disorders including physically damaged nerves and neurodegenerative diseases, and for treating alopecia and promoting hair growth.

Abstract: The present invention provides indoles of Formula I: wherein R1 and R2 have any of the values defined therefor in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions, including inflammatory diseases, cardiovascular diseases, and cancers. Also provided are pharmaceutical compositions comprising one or more compounds of Formula I.

Abstract: The invention provides compounds, compositions and methods relating to novel arylsulfonanilide derivatives and their use as pharmacologically active agents. The compositions find particular use as pharmacological agents in the treatment of disease states, particularly cancer, psoriasis, vascular restenosis, infections, atherosclerosis and hypercholesterolemia, or as lead compounds for the development of such agents.

Abstract: The present invention relates to novel naphthalene derivatives of formula (I), wherein R1, R2, R3 and X are as defined in the description, and preparation thereof. The compounds of formula (I) are useful as pharmaceuticals.

Abstract: Ethylene derivatives of formula (I): where Q is an unsubstituted or substituted phenyl or heterocyclic group, especially a 4-thiazolyl, 1- or 3-pyrazolyl, 1,3-oxazol-4-yl, phenyl or pyridyl group; E is a substituent such as a cyano group; A is a substituent such as a 4-pyrazolyl or thiazolyl group; and B is a substituent such as an alkylcarbonyl group. Agricultural chemicals and agents for preventing the attachment of aquatic organisms containing one or more such ethylene derivatives.

Abstract: The present invention provides trichloroethyl-sulfonylurea-containing compounds that inhibit glycing transporters, pharmaceutical compositions comprising such compounds, methods for using such compounds for inhibiting glycine transporters and methods for using such compounds for the treatment of disease states in which glycine is involved.

Abstract: This invention relates to novel processes for preparing heteroaryl-substituted urea compounds of formula (I): which are useful for treating diseases and pathological conditions involving inflammation such as chronic inflammatory disease. X, Ar, L, Q and are described herein.

Abstract: An N-containing five-membered ring compound of formula (I) wherein all symbols are the same as described in the specification, and a non-toxic salt thereof. The compound of formula (I) has an inhibitory activity against cysteine protease and therefore it is useful as an agent for the prophylaxis and/or treatment of inflammatory diseases, diseases induced by apoptosis, diseases induced by disorders of immune responses, autoimmune diseases, diseases induced by decomposition of proteins which compose organism, shock, circulatory system disorders, blood coagulation systems disorders, malignant tumors, acquired immune deficiency syndrome (AIDS) and AIDS-related complex (ARC), parasitic diseases, nerve degeneration diseases, pulmonary disorders, bone resorption diseases, endocrinesthenia, etc.

Abstract: The present invention provides benzo[b]thiophenes of Formula I: 1

Abstract: TNF-&agr; inhibitors containing a heterocyclic compound having angiotensin II antagonistic activity which are useful as preventives/remedies for inflammatory diseases, etc.

Abstract: The present invention provides benzo[b]thiophenes of Formula I: 1

Abstract: The present invention provides benzo[b]thiophenes of Formula I: 1

Abstract: The invention relates to novel tetrazolinone derivatives of general formula (I) wherein R1 represents halogen, C1-4 alkyl, C1-4 haloalkyl, C1-4 alkoxy, C1-4 alkylthio, C1-4 alkylsulfonyl, C1-4 alkylsulfonyloxy, C2-5 alkoxycarbonyl, C2-6 alkoxyalkyl, C2-6 alkylthioalkyl, nitro or cyano, R2 represents a hydrogen atom, C1-6 alkyl, C3-6 cycloalkyl which may be optionally substituted with halogen, or C1-3 alkyl, C1-4 haloalkyl or phenyl which may be optionally substituted with halogen, or C1-3 aklyl, C1-4 haloalkyl or nitro, m represents 0, 1 or 2, n represents 0 or 1, Q represents one of the groups which are mentioned in the description. The invention further relates to their use as herbicides and a process together with the intermediates for their preparation.

Abstract: A benzimidazole compound or a salt thereof which has an inhibitory action of forming of macrophages and is useful as an active ingredient of an orally available medicament for preventive and/or therapeutic treatment of arteriosclerosis, which is represented by the formula (I): wherein, R1 represents one or more functional groups on the benzene ring selected from the group consisting of hydrogen atom, a halogen atom, a lower alkyl group and a lower alkoxy group; R2 represents hydrogen atom, an alkyl group or an acyl group; L represents a C4-C8 alkylene group or an ethyleneoxy linking group represented as (CH2CH2O)nCH2CH2 wherein n represents 1 or 2; X represents O or NH; Y represents S or a single bond; and Q represents a 5- or 6-membered heterocyclic group which may have a functional group on the ring.

Abstract: The instant invention relates to novel tetrazole derivatives of the formula (I) wherein R1 represents halogen, methyl, ethyl, halomethyl, methoxy, ethoxy, C1-2 haloalkoxy, methylthio, ethylthio, C1-3 alkylsulfonyl, methylsulfonyloxy, ethylsulfonyloxy, nitro or cyano, R2 represents C1-6 alkyl, C3-6 cycloalkyl which may be optionally substituted with halogen or C1-3 alkyl, C1-4 haloalkyl, C2-6 alkenyl, or phenyl which may be optionally substituted with halogen, C1-3 alkyl, C1-4 haloalkyl, C2-6 alkenyl, or phenyl which may be optionally substituted with halogen, C1-3 alkyl, C1-2 haloalkyl or nitro, m represents 0, 1 or 2, two R1 s may be identical or different, in case m represents 2, n represents 1 or 2, Q represents one the cyclic groups which are mentioned in the specification, to intermediates and several processes for their preparation, to their use as herbicides and to novel compositions containing them.