Abstract: This invention provides caspase inhibitors of formula I: wherein Z is oxygen or sulfur; R1is hydrogen, —CHN2, R, CH2OR, CH2SR, or —CH2Y; Y is an electronegative leaving group; R2 is CO2H, CH2CO2H, or esters, amides or isosteres thereof; R3 is a group capable of fitting into the S2 subsite of a caspase enzyme; R4 and R5 are taken together with the intervening nitrogen to form heterocyclic ring and R is as described in the specification. The compounds are effective inhibitors of apoptosis and IL-1? secretion.

Abstract: A composition and use thereof for the prophylaxis or treatment of Alzheimer's disease, motor neurone disease, Lewy body disease, Pick's disease or progressive supranuclear palsy. The composition includes an agent which modulates or inhibits tau-tau association and which does not inhibit tau-tubulin binding. In the method the agent is administered to an individual in order to achieve the desired therapeutic effect. Preferably the agent which is administered is a phenothiazine compound.

Abstract: The invention features a method for treating a patient having a cancer or other neoplasm by administering to the patient two compounds simultaneously or within 14 days of each other in amounts sufficient to treat the patient.

Abstract: The present invention provides pharmaceutical compositions including a sedating antihistamine and a stimulant, and methods of use thereof. The stimulant reduces the sedation caused by the antihistamine, thereby allowing potent, but sedating, antihistamines to be used effectively.

Abstract: Photochemical demethylation reactions in solutions of thiazine dyes, in which the dye molecules act as both sensitizer and substrate, are reduced by quenching triple-state dye molecules, returning them to the unreactive around state.

Abstract: Novel chemical conjugates of psychotropic drugs and organic acids, uses thereof in the treatment of psychotic and/or proliferative disorders and diseases and as chemosensitizing agents, and their syntheses are disclosed. The organic acids are selected to reduce side effects induced by the psychotropic drugs and/or to exert an anti-proliferative activity.

Abstract: Pharmaceutical compositions contain a surfactant and one or more active ingredients selected from among anti-infective agents, anti-inflammatory agents, anti-mucolytic agents, antihistamines, antiseptics, combinations of antibiotics and combinations of these agents. The compositions are formulated for aerosol administration to treat chronic sinusitis or nasal polyps.

Abstract: The present invention relates to the combination of cyamemazine and an atypical neuroleptic, or a pharmaceutically acceptable salt thereof, and to the use thereof in the treatment of schizophrenia, and in particular of acute episodes of schizophrenia.

Abstract: The present invention relates to a phenothiazinium compound of Formula (I): 1

Abstract: Disclosed is the preparation and pharmaceutical use of substituted arylalcanoic acid derivatives of Formula I, wherein ring A, ring B, R1, R2, R3, R4, R5, X, Alk1, Alk2, Ar1, and Ar2 are as defined in the specification. These compounds, as selective agonists activating peroxisome proliferator-activated receptors (PPAR), in particularly the RXR/PPARalpha, RXR/PPARgamma, and RXR/PPARdelta heterodimers, are useful in the treatment and/or prevention of type 2 diabetes and associated metabolic syndrome such as hypertension, obesity, insulin resistance, hyperlipidemia, hyperglycemia, hypercholesterolemia, atherosclerosis, coronary artery disease, and other cardiovascular disorders with improved side effects profile commonly associated with conventional PPARgamma agonists.

Abstract: A vasectomy procedure is performed using a vas irrigation solution having a spermicidal agent that (a) acts to reduce the viability of downstream sperm following a vasectomy procedure and (b) has been established as safe and non-toxic in humans when administered by intravenous or other routes of injection for the treatment of other conditions. Preferred spermicidal agents are methylene blue and diltiazem. A kit having a pair of single-use, pre-filled injection devices is also disclosed.

Abstract: The present invention relates to new heterocyclic derivatives having an inhibitory activity on calpains and/or a trapping activity on reactive oxygen species, of formula in which A, X, Y, R1, R2 and Het represent variable groups. The invention also relates to their preparation methods, the pharmaceutical preparations containing them and their use for therapeutic purposes, in particular as inhibitors of calpains and/or traps of reactive oxygen species, selectively or non-selectively.

Abstract: Disclosed are compounds of the formula and the pharmaceutically acceptable salts thereof wherein R, Ar, A, n, R1 and R2 are defined herein. These compounds are highly selective agonists, antagonists or inverse agonists for GABAA brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAA brain receptors and are therefore useful in the diagnosis and treatment of anxiety, depression, Down Syndrome, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory. Pharmaceutical compositions, including packaged pharmaceutical compositions, are also disclosed.

Abstract: N-(imino)amines and their preparation and their use as NO synthase inhibitors and selective or non-selective traps for a reactive oxygen species.

Abstract: This invention relates to a compound and the use of the compound of the formula wherein R1, R2, R3, R4 and R5 are as defined in the description, A signifies —CH═CH— or —C≡C—; and B signifies wherein R6 to R26, X and Y are as defined in the specification or a pharmaceutically acceptable salt thereof, for use in pharmaceutical compositions for the treatment or prevention of mGluR5 receptor mediated disorders.

Abstract: This invention provides potent inhibitors of glycosyltransferases. The glyscosyltransferase inhibitors are useful for inhibiting the synthesis of glycosides. Accordingly, the glycosyltransferase inhibitors find use, for example, in the modulation of biological processes that involve glycoside-mediated cell adhesion.

Abstract: The present invention relates to compounds of the general formula (I) The compounds are useful in the treatment and/or prevention of conditions mediated by clear receptors, in particular the Peroxisome Proliferator-Activated Receptors (PPAR).

Abstract: A method for preventing adverse effects associated with the use of a medical device in a patient by introducing into the patient a device of which at least a portion includes a prophylactic or therapeutic amount of a nitric oxide adduct. The nitric oxide adduct can be present in a matrix coating on a surface of the medical device; can be coated per se on a surface of the medical device; can be directly or indirectly bound to reactive sites on a surface of the medical device; or at least a portion of the medical device can be formed of a material, such as a polymer, which includes the nitric oxide adduct. Also disclosed is a method for preventing adverse effects associated with the use of a medical device in a patient by introducing the device during a medical procedure and before or during said procedure locally administering a nitric oxide adduct to the site of contact of said device with any internal tissue.

Abstract: The reduced or “leuco” forms of certain pharmaceutical compounds can be produced and/or stabilised by mixing the unreduced compounds or the reduced compounds, respectively, with acid and a sulphydryl compound, especially a sulphur-containing amino acid, or peptide or derivative of such an amino acid.

Abstract: This invention relates to the use of a CYP2D6 inhibitor in combination with a drug having CYP2D6 catalyzed metabolism, wherein the drug and the CYP2D6 inhibitor are not the same compound; and pharmaceutical compositions for said use.

Abstract: Compounds of formula (I) 1

Abstract: Inhibition of RNA function, and treatment or control of diseases or conditions, e.g. infectious diseases such as viruses and viral infections (including HIV) and microbial infections, by the contacting of the RNA with a compound having a central or core structure comprising three fused rings containing from 12 to 15 ring atoms, the central ring including at least one heteroatom selected from nitrogen, oxygen and sulfur, the atoms of the three-ring core structure being optionally substituted with substituents such as halogens, cyano, and/or various substituted or unsubstituted aliphatic and/or heteroaliphatic moieties, or contacting the RNA with yohimbine, usnic acid or N-{4-[2,5-Dioxo-1-(4-trifluoromethoxy-phenyl)-pyrrolidin-3-yl]-phenyl}-2,2,2-trifluoro-acetamide. Preferred compounds are various phenothiazines, including both known and novel compounds.

Abstract: The present invention provides a compound of the formula (I) and pharmaceutically acceptable salts having useful antiviral activity against viruses of the herpes family. In said formula, X=O, (CH2)m, S, SO, SO2, NH, NR8 or a chemical bond; Y=O, (CH2)m, S, SO, SO2, NH, NR8; Z=NH, O, NR8, S, SO, SO2. The remaining substituents are described in the specification.

Abstract: The present invention relates to the use of the dye methylene blue (MB) or a related compound to prevent or reverse an exaggerated hemodynamic reaction in animals in need thereof, including humans. More specifically, the present invention concerns the use of MB or a related compound to prevent or reverse hypotension, unstable angina, myocardial infarction or shock caused by the concomitant ingestion of a phosphodiesterase inhibitor, such as sildenafil citrate, and a NO-donor, such as L-arginine, or an organic nitrate, such as nitroglycerin.

Abstract: A pharmacological composition includes an anti-histaminic in spray formulation that reduces symptomatic skin itching of skin without substantially eliciting weight gain or sedation in the patient when the composition is sprayed onto the area of skin at a dosage of at least 10 mg/ml over a period of at least 10 applications. Particularly contemplated anti-histaminic include hydroxyzine and ketotifen.

Abstract: Antimicrobial compositions containing a singlet oxygen-generating agent and a lubricant exhibit very effective antimicrobial activity against a variety of organisms, including Gram-positive bacteria, Gram-negative bacteria, fungi and yeast. The compositions have particular utility as beverage container lubricants. The passage of a container along a conveyor is antimicrobially lubricated by applying a lubricant to at least a portion of the container-contacting surface of the conveyor or to at least a portion of the conveyor-contacting surface of the container and generating singlet oxygen in situ. This method provides effective control of microbes on a beverage conveyor line, at rates comparable to purely chemical biocidal systems.

Abstract: Novel compounds of formula I: 1

Abstract: The reduced (or ‘leuco’) forms of certain pharmaceutically active compounds can be used for the treatment or pro-phylaxis methaemoglobinaemia or of a disease or disorder associated with or resulting from oxidative stress, such as Alzheimer's disease, motor neurone disease, Lewy Body disease, Pick's disease, Progressive Supranuclear Palsy, ischaemia, myocardial infarction, acute lung injury, stroke, Parkinson's disease or haemolysis and anaemia in acute falciparum malaria.

Abstract: This invention relates to a stable, sterilized, purified composition having a polymer matrix and a therapeutically effective amount of a drug, wherein the drug can be used to prevent or treat drug-induced, alcohol-induced, biologically-induced, trauma-induced or pain-induced nausea, vomiting, dizziness and other adverse effects arising from but not limited to motion sickness, cancer therapy, and pregnancy. In particular, the polymer matrix may be conformable to topical application on animal skin.

Abstract: A phenothiazine, acridan, acridone oxime, acridone hydrazone and dibenzodiazepine derivative represented by formula (I) 1

Abstract: The invention provides a novel heterocyclic ring condensed benzothiazine compound which is effective for prevention or remedy of disease, in which histamine, leukotriene and the like participate. The heterocyclic ring condensed benzothiazine compound of the present invention or a pharmacologically acceptable salt thereof is effective for prevention or remedy of disease, in which a chemical mediator, such as histamine, leukotriene and the like, participate, for example, asthma, allergic coryza, atopic dermatitis, hives, hay fever, gastrointestinal allergy, food allergy and the like.

Abstract: This invention relates to new compounds, pharmaceutical compositions and diagnostic kits comprising such compounds, and methods of using such compounds for inhibiting NAALADase enzyme activity, detecting diseases where NAALADase levels are altered, effecting neuronal activity, effecting TGF-&bgr; activity, inhibiting angiogenesis, and treating glutamate abnormalities, diabetic neuropathy, pain, compulsive disorders, prostate diseases, cancers and glaucoma.

Abstract: This invention provides ocular formulations comprising an ocular drug and a carboxylic acid in an amount sufficient to maintain the pH of the formulation from about 4.5 to about 7.5. The ocular drug may be a dopamine antagonist and the acid may be lactic acid, citric acid or tartaric acid. In some aspects, the pH of the formulation is about 5.5 The ocular formulations of this invention provide enhanced bioavailability which results in increased drug concentrations across the cornea and in the eye ball, i.e., aqueous humor and intraocular organs and chambers. Moreover, the present formulations are non-irritating when applied topically and have a shelf-life of at least fourteen days at 25° C. Methods are also provided to increase ocular blood flow by using present ocular formulations comprising dopamine antagonists or other drugs for the prevention and treatment of ocular hypertension, glaucoma, ischemic retinopathy and age-related macular degeneration (AMD).

Abstract: A transdermal or transmucosal pharmaceutical administration form for treating nicotine dependency or for disaccustoming smokers, comprising nicotine, a nicotine salt, a nicotine derivative or a nicotinergic substance in combination with at least one further active substance is characterized in that as additional active substance(s) it comprises at least one substance which acts on the central nervous system.

Abstract: The present invention discloses dye-sulfenate derivatives and their bioconjugates for dual phototherapy of tumors and other lesions. The compounds of the present invention may contain either a mixture of Type 1 and Type 2 agents or a single entity that integrates both units in the same molecules. The compounds are designed to produce both Type 1 and Type 2 phototherapeutic effect at once using dual wavelength light source that will produce singlet oxygen and free radicals at the lesion of interest.

Abstract: A bio-spectral imaging system and methods for in situ diagnosis of a disease state in biological tissue or cells of a living organism are provided. In one form, a method includes applying to the tissue or cells in situ a biological stain composition that includes at least one metachromatic dye; performing a spectral analysis to obtain at least one spectrum of the stained tissue or cells; comparing the spectrum with spectra from a library of spectra of similarly stained reference tissue or cells that have been categorized as diseased or non-diseased; and correlating the spectrum to a disease state. The system and methods may be used to diagnose, for example, pre-cancer and/or cancer, as well as diseases caused by various microorganisms. Methods for creating a library of spectra, methods for monitoring the efficiency of photodynamic therapy of diseased biological tissue or cells in vivo, as well as methods for improving the efficiency of photodynamic therapy are also provided.

Abstract: Phenothiazine and its derivatives products are provided with a minimal level of fines or dust as a result of forming such products in prill form. The prills are generally spherical. Also provided is a method for reducing the level of powder in phenothiazine product which includes forming the phenothiazine product in prill form such that the prills have a generally spherical shape. The prill product achieves improved handling, flowability and dissolution times, while minimizing the generation of phenothiazine fines and dust, and the problems associated with worker exposure, irritation and sensitization to such fines and dust.

Abstract: The invention concerns novel N-(iminomethyl)amine derivatives comprising in their skeleton the aminophenylamine, oxodiphenylamine, carbazole, phenazine, phenoxazine or oxodiphenyl motif, their use as medicines and pharmaceutical compositions containing them. The invention concerns in particular the following compounds: -4-{[2-thienyl(imino)methyl]amino}-N-[2-(phenylamino)phenyl]-benzenebutanamide; -4-{[2-thienyl(imino)methyl]amino}-N-[4-(phenylamino)phenyl]-benzenebutanamide; -N-′[4-(10H-phenothiazin-2-yloxy)phenyl]-2-thiophenecarboximidamide; -4-(4-{[amino(2-thienyl)methylidene]amino}phenyl)-N-(10H-phenothiazin-3-ylH)butanamide; -3-[(3-{[amino(2-thienyl)methylidene]amino}-benzyl)amino]-N-(4-anilinophenyl)propanamide; -N′-(4-{2-[(10H-phenothiazin-3-ylmethyl)amino]ethyl}phenyl-2-thiophene carboximidamide.

Abstract: Kappa-opioid agonists prevent the impairment of renal function otherwise caused by the combination of gaseous anesthesia and surgery or severe trauma. Not only do these agents preserve renal function and maintain urine output, they also maintain plasma electrolyte concentration and osmolality by reducing renal loss of sodium and potassium when compared to other diuretic agents. The preservation of urine flow as well as the ability to retain body sodium, potassium, calcium, and osmolality during surgery or severe trauma under gaseous anesthesia are novel and unique properties associated only with kappa opioid agonists. To date, no other clinically-used diuretic agent has been shown to provide constant urine flow, or to retain electrolytes during anesthesia and surgery. The kappa opioid agonists may be used in surgical patients with normal cardiovascular function, but are particularly useful in patients with compromised cardiovascular and/or renal function.

Abstract: The invention provides methods and compositions for enhancing the bioavailability of a drug in a subject. The present invention also provides methods and compositions for treating or preventing hepatic injury in a subject in need thereof. The invention further provides methods for identifying hydrophobic peptides, e.g., &bgr;-amyloid peptide derivatives, which are useful in enhancing bioavailability of a drug in a subject.

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

Abstract: This invention herein describes a method of facilitating the entry of drugs into cells and tissues at physiologically protected sites at pharmicokinetically useful levels and also a method of targeting drugs to specific organelles within the cell. This polar lipid/drug conjugate targeting invention embodies an advance over other drug targeting methods known in the prior art, because the invention provides drug concentrations in such physiologically protected sites that can reach therapeutically-effective levels after administration of systemic levels much lower than are currently administered to achieve a therapeutic dose. This technology is appropriate for use with psychotropic, neurotropic and neurological drugs, agents and compounds, for rapid and efficient introduction of such agents across the blood-brain barrier.

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

Abstract: Phenothiazine and its derivatives products are provided with a minimal level of fines or dust as a result of forming such products in prill form. The prills are generally spherical. Also provided is a method for reducing the level of powder in phenothiazine product which includes forming the phenothiazine product in prill form such that the prills have a generally spherical shape. The prill product achieves improved handling, flowability and dissolution times, while minimizing the generation of phenothiazine fines and dust, and the problems associated with worker exposure, irritation and sensitization to such fines and dust.

Abstract: A phenothiazine, acridan, acridone oxime, acridone hydrazone and dibenzodiazepine derivative represented by formula (I) 1

Abstract: This invention relates to a pharmaceutical composition for angiotensin II-mediated diseases, which comprises a compound having angiotensin II antagonistic activity of the formula wherein R1 is H or an optionally substituted hydrocarbon residue; R2 is an optionally esterified carboxyl group; R3 is a group capable of forming an anion or a group convertible thereinto; X is a covalent bond between the 2 phenyl rings or a spacer having a chain length of 1 to 2 atoms as the linear moiety between the adjoining phenylene group and phenyl group; n is 1 or 2; the ring A is a benzene ring having 1 or 2 optional substituents in addition to R2; and Y is a bond, —O—, —S(O)m- (wherein m is 0, 1 or 2) or —N(R4)— (wherein R4 is H or an optionally substituted alkyl group), or a pharmaceutically acceptable salt thereof in combination with a compound having diuretic activity or a compound having calcium antagonistic activity.

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

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

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

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