Abstract: The present invention describes novel nitrosated and/or nitrosylated nonsteroidal antiinflammatory compounds, and novel compositions comprising at least one nitrosated and/or nitrosylated nonsteroidal antiinflammatory compound, and, optionally, at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase. The present invention also provides methods for treating, preventing and/or reducing inflammation, pain, and fever; decreasing or reversing the gastrointestinal, renal and other toxicities resulting from the use of nonsteroidal antiinflammatory drugs; treating and/or preventing gastrointestinal disorders; treating inflammatory disease states and disorders; and treating and/or preventing ophthalmic diseases or disorders.

Abstract: Among its several embodiments, the present invention provides an improved process for the preparation of tetrahydrobenzothiepine-1,1-dioxide compounds; the provision of a process for preparing a diastereomeric mixture of tetrahydrobenzothiepine-1,1-dioxide compounds from a single diastereomer of such compounds; the provision of a process for the preparation of 3-bromo-2-substituted propionaldehyde compounds; and the provision of a process for the preparation of 3-thio-2-substituted propionaldehyde compounds.

Abstract: Etoposide analogs such as 4′-O-demethyl-4&bgr;-[4″-(methyl-L-tyrosine-N-carbonyl)-anilino]-4-desoxy-podophyllotoxin (12) and 4′-O-demethyl-4&bgr;-[4″-(methyl-L-tryptophan-N-carbonyl)-anilino]-4-desoxypodophyllotoxin (13) are described, along with pharmaceutical formulations containing the same, methods of use thereof, and intermediates and methods of making the same.

Abstract: The present invention provides combinations of cardiovascular therapeutic compounds for the prophylaxis or treatment of cardiovascular disease including hypercholesterolemia, atherosclerosis, or hyperlipidemia. Combinations disclosed include an ileal bile acid transport inhibitor combined with a bile acid sequestrant.

Abstract: The present invention of compounds of formula (I) 1

Abstract: The present invention relates to cyclic sulfone moiety-containing hydroxyethylamine protease inhibitor compounds and pharmaceutical or method of use therefor, particularly as an inhibitor of HIV protease.

Abstract: The invention provides compounds of formula as described in the claims, or an optical isomer, diastereomer or enantiomer thereof, or a pharmaceutically-acceptable salt, or biohydrolyzable amide, ester, or imide thereof are useful as inhibitors of metalloproteases. Also disclosed are pharmaceutical compositions and methods of treating diseases, disorders and conditions characterized by metalloprotease activity using these compounds or the pharmaceutical compositions containing them.

Abstract: The present invention offers a tracheal smooth muscle relaxant containing the compound represented by the following formula (1) or pharmacologically acceptable salt thereof as an effective ingredient.

Abstract: The present invention pertains, at least in part, to novel 7-substituted tetracycline compounds. These tetracycline compounds can be used to treat numerous tetracycline compound-responsive states, such as bacterial infections and neoplasms, as well as other known applications for minocycline and tetracycline compounds in general, such as blocking tetracycline efflux and modulation of gene expression.

Abstract: The present invention relates to methods for preparing macrocyclic products having 9 or more ring atoms by ring-closing diyne metathesis of suitable diyne substrates. The diyne substrates can be converted into cycloalkynes or into cycloalkadiynes by cyclodimerization, depending on the particular reaction conditions. Any alkyne metathesis catalyst can be used as the catalyst, regardless of whether said catalysts are heterogeneously or homogeneously present in the reaction medium. The preferred catalysts or pre-catalysts are transition metal alkylidyne complexes, transition metal compounds which form alkylidyne complexes under the reaction conditions, and transition metal compounds with metal-metal triple bonds. The method can be carried out with numerous functional groups, solvents, and additives.

Abstract: The present invention relates to compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, A, X, T, Q, Z, U, Y, Ar, p and n are as defined in the specification. These compounds are useful in the treatment and/or prevention of conditions mediated by nuclear receptors, in particular the Peroxisome Proliferator-Activated Receptors (PPAR).

Abstract: Compounds of formula (I) are antibacterial agents wherein: R3 and R4, taken together with the carbon atoms to which they are respectively attached, form an optionally substituted saturated carbocyclic or heterocyclic ring of 5 to 16 atoms, which may be benz-fused or fused to a second optionally substituted saturated carbocyclic or heterocyclic ring of 5 to 16 atoms; and R1 and R2 are as defined in the specification.

Abstract: The present invention provides combinations of cardiovascular therapeutic compounds for the prophylaxis or treatment of cardiovascular disease including hypercholesterolemia, atherosclerosis, or hyperlipidemia. Combinations disclosed include an ileal bile acid transport inhibitor combined with a cholesteryl ester transfer protein (CETP) inhibitor.

Abstract: The invention provides compounds of the formula: 1

Abstract: The present invention provides a method for treating pain using an atypical antipsychotic compound.

Abstract: Composition in the form of an aqueous solution, useful for disinfecting hard surfaces comprises: a) from 0.0005% to 20% by weight of peracetic acid, b) from 0.001% to 45% by weight of acetic acid, c) from 0.001% to 35% by weight of hydrogen peroxide, d) from 0.0001% to 2% by weight of at least one compound of formula (I) (R1)(R2)(R3)N→O  (I) e) if desired, up to 2.5% by weight of at least one nonionic surfactant, and wherein f) the weight ratio between the compound of formula (I) and the peracetic acid is less than or equal to 1, and in that g) the weight ratio between the nonionic surfactant and the peracetic acid is less than or equal to 0.2.

Abstract: Matrix metalloproteinases (MMPs) are a group of enzymes that have been implicated in the pathological destruction of connective tissue and basement membranes. These zinc containing endopeptidases consist of several subsets of enzymes including collagenases, stromelysins and gelatinases. TNF-&agr; converting enzyme (TACE), a pro-inflmatory cytokine, catalyzes the formation of TNF-&agr; from membrane bound TNF-&agr; precursor protein. It is expected that small molecule inhibitors of MMPs and TACE therefore have the potential for treating a variety of disease states.

Abstract: Substituted benzothiepine 1,1-dioxide derivatives of formula I: in which R1, R2, R3, R4, R5 and Z have the meanings indicated, and their physiologically tolerable salts and physiologically functional derivatives and a process for their preparation are described. The compounds are suitable, for example, as hypolipidemics.

Abstract: The present invention relates to compounds of the general formula (I) 1

Abstract: The effect of HIV components on lymphocytes, as exemplified by peripheral blood mononuclear cells (PBMC) in retarding their proliferation can be reversed by inhibiting the PKA/cAMP pathway. By using protocols which inhibit this pathway, the ability of lymphocytes to proliferate can be restored. The restoration of this pathway is useful in reversing the effects of HIV infection.

Abstract: Provided are novel benzothiepines, derivatives, and analogs thereof; pharmaceutical compositions containing them; and methods of using these compounds and compositions in medicine, particularly in the prophylaxis and treatment of hyperlipidemic conditions such as those associated with atherosclerosis or hypercholesterolemia, in mammals. Also provided are compositions and methods for combination therapy employing ileal bile acid transport inhibitors and HMG Co-A reductase inhibitors for the treatment of hyperlipidemic conditions.

Abstract: The invention relates to water-dispersible granules of a pesticidally active main component of sufficiently high melting point, a liquid pesticidal active substance or pesticidal active substance of low melting point and/or which is not sufficiently biologically active in the solid state, in dissolved form, a solvent or solvent mixture with low volatility, and, if appropriate, further additives or adjuvants. The granules are prepared from an aqueous suspoemulsion of the components by removing the water, for example in a fluidized-bed drier. The novel granules are distinguished by an outstanding spontaneous dispersibility and a good biological activity of the formulations prepared from them.

Abstract: The invention is directed to 1,4-dithiin- and 1,4-dithiepin-1,1,4,4-tetroxide derivatives useful as galanin receptor antagonists for treating disorders of the central nervous system. Pharmaceutical compositions comprising the compounds of the present invention and methods of treating conditions such as an eating disorder, obesity, bulimia nervosa, anorexia nervosa, binge eating, diabetes, dyslipidemia, hypertension, memory loss, sleep disturbances, pain, depression, anxiety, Alzheimer's disease, senile dementia, cerebral hemorrhage, or diarrhea are also described.

Abstract: The invention relates to compounds of formula I 1

Abstract: Provided are novel benzothiepines, derivatives, and analogs thereof; pharmaceutical compositions containing them; and methods of using these compounds and compositions in medicine, particularly in the prophylaxis and treatment of hyperlipidemic conditions such as those associated with atherosclerosis or hypercholesterolemia, in mammals.

Abstract: The invention relates to substituted benzo(b)thiepine-1,1-dioxide derivatives and to the acid addition salts thereof. The invention relates to compounds of formula (I), wherein R1, R2, R3, R4, R5 and Z have the cited descriptions, to the physiologically compatible salts, to physiologically functional derivatives, and to a method for the production thereof. The compounds are suited, for example, as hypolipidemic agents.

Abstract: Compounds of the formula (I) are disclosed which are dual fibrinogen receptor and vitronectin receptor antagonists and are useful in the treatment of atherosclerosis, in the prevention of restenosis and in the prevention of tumor metastasis and tumor growth: 1

Abstract: Provided are compounds of formula (I) 1

Abstract: A sulfonic acid compound of a cyclic phenol sulfide represented by formula (1): (wherein X represents a hydrogen atom, a hydrocarbon group, or an acyl group; M represents a hydrogen atom, an alkyl group, a metal, ammonium, (lower-alkyl)ammonium, (lower-alkanol)ammonium, a nitrogen-containing heterocyclic group, or an amino acid residue; Z represents Sm, SO, or SO2; m is an integer of from 1 to 7; and n is an integer of from 4 to 12, with the proviso that the plural X's, M's and Z's are each the same or different, and at least one of the plural M's is neither a hydrogen atom nor an alkyl group), or a salt thereof; a composition for separating and recovering an organic halogen compound or a monocyclic aromatic compound, comprising a cyclic phenol sulfide or a salt thereof, and a carrier; and a pharmaceutical composition a cyclic phenol sulfide or a pharmaceutically acceptable salt, and a carrier.

Abstract: The invention provides compounds of the formula: wherein the ring A is an optionally substituted benzene ring; R1 is an optionally substituted non-aromatic heterocyclic group; R2 and R3 are independently hydrogen atom or an optionally substituted hydrocarbon group; n is an integer of 0-3; or salts thereof, which are useful as medicines having an osteogenesis promoting effect and chondrogensis promoting effect. The present invention relates to an amine compound having an excellent effect of inhibiting production and/or secretion of amyloid-b protein, a production and use thereof. Especially, it is effective for preventing and/or treating, for example, neurodegenerative diseases, amyloid angiopathy, neurological disorders caused by cerebrovascular disorders, and so forth.

Abstract: A compound of the formula: wherein R1 is hydrogen or halogen, R2 is hydroxy, acyl(lower)alkoxy, hydroxy(lower)alkyl, lower alkoxy(lower)alkyl, lower alkylthio(lower)alkyl, mono(or di or tri)halo(lower)alkyl, (ethoxycarbonyl)amino, sulfamoylamino, (dimethylsulfamoyl)amino, N,N-di(lower)alkylamino(lower)alkyl, hydroxyimino(lower)alkyl, lower alkoxyimino(lower)alkyl, acyl, lower alkoxycarbonyl, carbamoyl, di(lower)alkylcarbamoyl, (amino(lower)alkyl)carbamoyl, N,N-di(lower)alkylamino(lower)alkylcarbamoyl, guanidinocarbonyl, morpholinylsulfonyl, sulfamoyl, lower alkylsulfamoyl, (lower alkylsulfonyl)(lower)alkyl, guanidinocarbonyl(lower)alkenyl, lower alkylthio, cyano, acyl(lower)alkyl, acyl(lower)alkenyl, aryl which has one or more substituent(s) or a heterocyclic group which has one or more substituent(s), and X is —O—, or a salt thereof.

Abstract: Methods of using prostaglandin agonists for the reduction of intraocular pressure, and accordingly glaucoma.

Abstract: This invention provides the methodology and agents for treating any disease or clinical condition which is at least partly the result of endoplasmic reticulum-associated retention of proteins. Thus, the methods and agents of the present invention provide for the release of normally retained proteins from the endoplasmic reticulum. The present invention is particuarly useful for treating any disease or clinical condition which is at least partly the result of endoplasmic reticulum-associated retention or degradation of mis-assembled or mis-folded proteins.

Abstract: Method and compositions for treating a patient having a neurological disease or disorder, such as stroke, head trauma, spinal cord injury, spinal cord ischemia, ischemia- or hypoxia-induced nerve cell damage, epilepsy, anxiety, neuropsychiatric or cognitive deficits due to ischemia or hypoxia such as those that frequently occur as a consequence of cardiac surgery under cardiopulmonary bypass, or neurodegenerative diseases such as Alzheimer's Disease, Huntington's Disease, Parkinson's Disease, or amyotrophic lateral sclerosis (ALS).

Abstract: The invention relates to pharmaceutical compositions comprising an aldose reductase inhibitor and an ACE inhibitor, and their use in the treatment of diabetic complications such as diabetic neuropathy, diabetic retinopathy and diabetic nephropathy.

Abstract: Method for controlling harmful organisms in genetically modified cotton plants which contain a gene derived from Bacillus thuringiensis which encodes and expresses an insecticidally active protein, which comprises applying an insecticisally effective amount of one or more compounds from the following groups and a-f, described herein, to the plants, to their seeds or propagation stock and/or to the area in which they are cultivated. The method according to the invention makes it possible to reduce the application rate of crop protection agents which act synergistically with the transgenic plants, and also to increase and widen the efficacy of the transgenic plants, and therefore offers both economical and ecological advantages.

Abstract: Novel derivatives of prostaglandin compounds of the F-series (PGF), specifically macrocyclic internal 1,15-lactones of fluprostenol and related PGF analogs, such as cloprostenol or latanoprost. The novel analogs can be formulated into ophthalmic solutions and topically applied for the treatment of the increased intraocular pressure caused by glaucoma and the reduction of ocular hypertension.

Abstract: Spirohydantoin compounds and their pharmaceutically acceptable salts are disclosed. The synthesis of these compounds and their use as alpha 1a adrenergic receptor antagonists is also described. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds are typically selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia can be achieved.

Abstract: The present invention describes novel nitrosated and/or nitrosylated nonsteroidal antiinflammatory compounds, and novel compositions comprising at least one nitrosated and/or nitrosylated nonsteroidal antiinflammatory compound, and, optionally, at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase. The present invention also provides methods for treating, preventing and/or reducing inflammation, pain, and fever; decreasing or reversing the gastrointestinal, renal and other toxicities resulting from the use of nonsteroidal antiinflammatory drugs; treating and/or preventing gastrointestinal disorders; treating inflammatory disease states and disorders; and treating and/or preventing ophthalmic diseases or disorders.

Abstract: Aqueous endosulfan microcapsule dispersions in which the dispersed microcapsules comprise endosulfan, an organic solvent or solvent mixture and a capsule-forming material based on isocyanate prepolymers and the aqueous phase which represents the dispersion medium comprises surfactants, a water-soluble inorganic salt with or without other formulation aids, which include a relatively small amount of capsule-forming material, and a process for their preparation.

Abstract: This invention concerns the compounds of formula (I), the N-oxide forms, the pharmaceutically acceptable addition salts and the stereoisomeric forms thereof, wherein n is zero to 6; p and q are zero to 4; r is zero to 5; R1 and R2 each independently are hydrogen; optionally substituted C1-6alkyl; C1-6alkylcarbonyl; halomethylcarbonyl; or R1 and R2 taken together with the nitrogen atom to which they are attached may form a morpholinyl ring or an optionally substituted heterocycle; each R3 and R4 independently are halo, cyano, hydroxy, halomethyl, halomethoxy, carboxyl, nitro, amino, mono- or di(C1-6alkyl)amino, C1-6alkylcarbonylamino, aminosulfonyl, mono- or di(C1-6alkyl)aminosulfonyl, C1-6alkyl, C1-6alkyloxy, C1-6alkylcarbonyl, C1-6alkyloxycarbonyl; each R5 independently is C1-6alkyl, cyano or halomethyl; X is CR6R7, NR8, O, S, S(═O) or S(═O)2; aryl is optionally substituted phenyl; provided that the compound is other than (±)-3,3a,8,12b-tetrahydro-N-methyl-2H-dibenzo[3

Abstract: Provided are novel benzothiepines, derivatives, and analogs thereof; pharmaceutical compositions containing them; and methods of using these compounds and compositions in medicine, particularly in the prophylaxis and treatment of hyperlipidemic conditions such as those associated with atherosclerosis or hypercholesterolemia, in mammals. Also provided are compositions and methods for combination therapy employing ileal bile acid transport inhibitors and EG Co-A reductase inhibitors for the treatment of hyperlipidemic conditions.

Abstract: Compounds of general formula (I) wherein R4 is an ester or thioester group and R, R1, R2, and R3 are as specified in the description, inhibit monocyte and/or macrophage and/or lymphocyte activation and lymphocyte proliferation.

Abstract: The invention relates to compounds of the formula in which: A is a divalent radical selected from: A1) —O—CO— A2) —CH2—O—CO— A3) —O—CH2—CO— A4) —O—CH2—CH2— A5) —N(R1)—CO— A6) —N(R1)—CO—CO— A7) —N(R1)—CH2—CH2— A8) —O—CH2— in which: R1 is a hydrogen or a (C1-C4)-alkyl; and Am is a nitrogen-containing heterocycle.

Abstract: A liquid pharmaceutical formulation comprising a) 2 to 7% w/v of Zotepine; b) 0.5 to 35% w/v of an organic acid selected from the group consisting of ascorbic acid, citric acid, fumaric acid, glutaric acid, lactic acid, malic acid, sorbic acid and tartaric acid; c) 15 to 60% v/v of ethanol and d) a liquid diluent to 100%; which may be used as drops or in a drink.

Abstract: This invention is to provide a compound of the formula: wherein R1 is an optionally substituted 5- to 6-membered ring; the ring A is an optionally substituted 6- to 7-membered ring; the ring B is an optionally substituted benzene ring; n is an integer of 1 or 2; Z is a chemical bond or a divalent group; R2 is (1) an optionally substituted amino group in which a nitrogen atom may form a quaternary ammonium, (2) an optionally substituted nitrogen-containing heterocyclic ring group which may contain a sulfur atom or an oxygen atom as ring constituting atoms and wherein a nitrogen atom may form a quaternary ammonium, (3) a group binding through a sulfur atom or (4) a group of the formula:  wherein k is 0 or 1, and when k is 0, a phosphorus atom may form a phosphonium; and R5 and R6 are independently an optionally substituted hydrocarbon group, an optionally substituted hydroxy group or an optionally substituted amino group, and R5 and R6 may bind to each other to form a cy

Abstract: Substituted benzothiepine 1,1-dioxide derivatives of formula I: in which R1, R2, R3, R4, R5 and Z have the meanings indicated, and their physiologically tolerable salts and physiologically functional derivatives and a process for their preparation are described. The compounds are suitable, for example, as hypolipidemics.

Abstract: This invention relates to an insecticidal and miticidal composition which contains as active ingredients chlorfenapyr in combination with one or more compounds selected from the group consisting of benzoepin, nereistoxin-type insecticidal agents and diafenthiuron.

Abstract: The present invention provides tricyclic compounds which are useful for the treatment of pollakiuria and urinary incontinence and which are represented by general formula (I): (wherein R1 represents hydrogen, substituted or unsubstituted lower alkyl, etc.; X1—X2—X3 represents CR5═CR6—CR7═CR8 (wherein R5, R6, R7 and R8, which may be the same or different, each represents hydrogen, substituted or unsubstituted lower alkyl, hydroxy, substituted or unsubstituted lower alkoxy, etc.), N(O)m═CR5—CR6═CR7 (wherein R5, R6 and R7 have the same significances as defined above, and m represents 0 or 1), S—CR7═CR8 (wherein R7 and R8 have the same significances as defined above), etc.

Abstract: This invention concerns the compounds of formula (I), the N-oxide forms, the pharmaceutically acceptable addition salts and the stereoisomeric forms thereof, wherein n is zero to 6; p and q are zero to 4; r is zero to 5; R1 and R2 each independently are hydrogen; optionally substituted C1-6alkyl; C1-6alkylcarbonyl; halomethylcarbonyl; or R1 and R2 taken together with the nitrogen atom to which they are attached may form a morpholinyl ring or an optionally substituted heterocycle; each R3 and R4 independently are halo, cyano, hydroxy, halomethyl, halomethoxy, carboxyl, nitro, amino, mono- or di(C1-6alkyl)amino, C1-6alkylcarbonylamino, aminosulfonyl, mono- or di(C1-6alkyl)aminosulfonyl, C1-6alkyl, C1-6alkyloxy, C1-6alkylcarbonyl, C1-6alkyloxycarbonyl; each R5 independently is C1-6alkyl, cyano or halomethyl; X is CR6R7, NR8, O, S, S(═O) or S(═O)2; aryl is optionally substituted phenyl; provided that the compound is other than (±)-3,3a,8,12b-tetrahydro-N-methyl-2H-dibenzo[3