Abstract: The application relates to novel amino alcohols of the general formula (I) where R, R1, R2, R3, R4, R5 and R6 each have the definitions illustrated in detail in the description, to a process for their preparation and to the use of these compounds as medicines, in particular as renin inhibitors.

Abstract: A transdermal delivery system (TDS) for administering at least one active agent through the skin. The system has a first electrode, a second electrode, and a matrix located between the first and second electrodes. The TDS contains at least one active agent which is either alkaline or acidic. The system is configured such that when applying a voltage to the electrodes, the pH of the matrix, in the case of an alkaline active agent, does not exceed the pH of the active agent and, in case of an acidic active agent, does not fall below the pH of the active agent.

Abstract: A pharmaceutical composition of a pharmaceutically acceptable trospium salt, with upon administration to a human patient generates an average steady state blood levels of trospium with a minimum (Cmin) and maximum (Cmax) blood levels of about 0.5-2.5 ng/ml and about 2.0-6.0 ng/ml, respectively.

Abstract: Methods and compositions useful in the treatment or prevention of lysosomal storage diseases, such as Pompe's disease, Fabry's disease, Gaucher's disease, and Niemann-Pick disease, are provided. The treatment includes administering to a subject a farnesyl transferase inhibitor compound. The treatment may also include enzyme replacement therapy or gene therapy.

Abstract: The present invention relates to compounds of formula (I) wherein n represents 0, 1, 2, 3, 4 or 5, R represents independent from each other hydroxyl, cyano, nitro, halogen, alkyl, alkoxy alkylcarbonyl, alkoxycarbonyl, alkylamine, dialkylamine, alkylcarbonylamine, alkylcarbamate Y represents one of the following groups: (Ia) in free base or acid addition salt form, to processes for their production, to pharmaceutical compositions comprising them and their use in the manufacture of a medicament for the treatment and/or delay of progression of psychotic and neurodegenerative disorders.

Abstract: A pharmaceutical composition of a pharmaceutically acceptable trospium salt, with upon administration to a human patient generates an average steady state blood levels of trospium with a minimum (Cmin) and maximum (Cmax) blood levels of about 0.5-2.5 ng/ml and about 2.0-6.0 ng/ml, respectively.

Abstract: Patients susceptible to or suffering from disorders, such as central nervous system disorders, which are characterized by an alteration in normal neurotransmitter release, such as dopamine release (e.g., Parkinsonism, Parkinson's Disease, Tourette's Syndrome, attention deficient disorder, or schizophrenia), are treated by administering a compound of Formulas 1 or 2, as described herein. The compounds of Formulas 1 and 2 are also useful for treating pain, and treating drug addiction, nicotine addiction, and/or obesity. The compounds can exist as individual stereoisomers, racemic mixtures, diastereomers and the like.

Abstract: The present invention relates to 1-aza-bicycloalkyl derivatives of Formula (I) wherein the substituents are as defined in the specification and to processes for their production to pharmaceutical compositions comprising them and to their use in the manufacture of a medicament for the treatment and/or delay of progression of psychotic and nemodegenerative disorders.

Abstract: Disclosed is a preparation for transnasal application, which has improved fluidability. Specifically disclosed is a preparation for transnasal application, which comprises at least a complex comprising: a fluidability-improving component comprising a first crystalline cellulose (A) having specified powder properties, tricalcium phosphate (B) having specified powder properties, and a second crystalline cellulose (C) having specified powder properties or a starch (D) having specified powder properties; and a physiologically active substance.

Abstract: A dermal or transdermal therapeutic system comprising a reservoir that contains at least one active substance, an active substance-permeable membrane which delimits the active-substance reservoir, and a closing layer. The closing layer is impermeable to the active substance at a temperature lying below the skin temperature while being permeable at skin temperature and above.

Abstract: The invention provides methods and compositions for treating conditions mediated by various kinases wherein derivatives of urea compounds are employed. The invention also provides methods of using the compounds and/or compositions in the treatment of a variety of diseases and unwanted conditions in subjects.

Abstract: A pharmaceutical composition for transdermal delivery comprising one or more physiologically active agents; one or more dermal penetration enhancers; and a volatile pharmaceutically acceptable carrier comprising a volatile solvent; and wherein the physiologically active agent and dermal penetration enhancer form an amorphous deposit upon evaporation of the volatile carrier, said amorphous deposit forming a reservoir within the stratum corneum; and (A) wherein the composition has a release rate profile of physiologically active agent so as to provide a ratio of the maximum concentration (Cmax) to the average concentration (Cavg) for the physiologically active agent over the dosage interval within the range of 1 to 10.

Abstract: Disclosed are N-{[(1S,4S,6S)-3-(2-pyridinylcarbonyl)-3-azabicyclo [4.1.0]hept-4-yl]methyl}-2-heteroarylamine derivatives and their use as pharmaceuticals.

Abstract: Patients susceptible to or suffering from disorders, such as central nervous system disorders, which are characterized by an alteration in normal neurotransmitter release, such as dopamine release (e.g., Parkinsonism, Parkinson's Disease, Tourette's Syndrome, attention deficient disorder, or schizophrenia), are treated by administering a compound of Formulas 1 or 2, as described herein. The compounds of Formulas 1 and 2 are also useful for treating pain, and treating drug addiction, nicotine addiction, and/or obesity. The compounds can exist as individual stereoisomers, racemic mixtures, diastereomers and the like.

Abstract: Disclosed herein are methods of enhancing the stability of a sustained pharmaceutical composition comprising an active agent and a polymer and methods of preparing such pharmaceutical compositions with enhanced stability.

Abstract: The main goals of the invention are to develop the long-term release of Granisetron injection implant composition with biodegradable polymer and to develop relative processing. Granisetron is mixed with different biodegradable polymers, and then hot melt extrusion technique with different diameter, temperature, rate of extrusion and holding time is applied to make implant. In vitro dissolution of the Granisetron injection implant composition shows the component continued release of the drug for over 7 days.

Abstract: The present invention provides a most suitable prodrug of a cinnamide compound. The prodrug is represented by Formula (I) wherein Ra and Rb each denote a C1-6 alkyl group or the like; Xa denotes a methoxy group or a fluorine atom; Y denotes a phosphono group or the like; and A denotes a cyclic lactam derivative.

Abstract: Herein disclosed is a method of rescuing gonadotropin-releasing hormone receptor (GnRHR) mutants with IN3 or a mimetic thereof. IN3 significantly rescues 11 missense mutations as assessed by radioligand binding and by IP production. Such rescue occurred despite widely disparate loci along the receptor. In addition, many altered GnRH receptors (terminally truncated, internal deletions, or lacking the ability to form bridges to form tertiary structure) were rescued with IN3.

Abstract: Methods are provided for treating a subject for a fertility condition. In accordance with the subject methods, at least a portion of a subject's autonomic nervous system is modulated to increase the sympathetic activity/parasympathetic activity ratio in a manner that is effective to treat the subject for the condition. Embodiments of the subject invention include modulating a subject's autonomic nervous system using electrical energy and/or one or more pharmacological agents. The subject methods find use in the treatment of a variety of different fertility conditions. Also provided are kits for use in practicing the subject methods.

Abstract: Ampoules made of plastics material and containing 0.5 to 5 ml of a pharmaceutical formulation are sealed, together with an oxygen scavenger, within a pouch.

Abstract: The specific compounds of this list: {7-cyano-2-methyl-1-[4-(morpholine-4-sutfonyl)benzyl]indolizin-3-yl}acetic acid, {1-(3-chloro-4-ethanesulfonylbenzyl)-7-cyano-2-methylindolizin-3-yl}acetic acid, {1-[3-chloro4-(morpholine-4-sulfonyl)benzyl]-7-cyano-2-methylindolizin-3-yl}acetic acid, {1-(3-chloro-4-ethanesulfonylphenylsulfanyl)-7-cyano-2-methylindolizin-3-yl}acetic acid, {1-[3-chloro-4-(morpholine-4-sutfonyl)phenylsutfanyl]-7-cyano-2-methylindolizin-3-yl}acetic acid, {7-cyano-1-(6-fluoroquinolin-2-ylmethyl)-2-methylindolizin-3-yl}acetic acid are ligands of the CRTH2 receptor and are useful in the treatment of respiratory diseases.

Abstract: A pharmaceutical or cosmetic carrier or composition for topical application characterized by rheological properties which render the carrier or composition semi-solid at rest and a liquid upon application of shear forces thereto. The composition or carrier are prepared by mixing 1-25 percent of a solidifying agent and 75-99 percent of a hydrophobic solvent, by weight, wherein at least one of them has therapeutic or cosmetic benefits, in the presence or absence of a biologically active substance.

Abstract: Provided are methods and compositions for the treatment of a sexual dysfunction such as premature ejaculation. In certain embodiments, a NMDA antagonist (e.g., dextromethorphan) is administered to a subject in combination with tramadol or a tramadol derivative to treat premature ejaculation. In certain embodiments, a capsaicinoid (e.g., capsaicin) and/or a phosphodiesterase type V inhibitor (e.g., sildenafil citrate) are further administered to the subject. Pharmaceutical preparations such as tablets and capsules are provided.

Abstract: The present invention relates to compounds of formula (I) wherein n represents 0, 1, 2, 3, 4 or 5 R represents independent from each other hydroxyl, cyano, nitro, halogen, alkyl, alkoxy alkylcarbonyl, alkoxycarbonyl, alkylamine, dialkylamine, alkylcarbonylamine, alkylcarbamate Y represents one of the following groups: in free base or acid addition salt form, to processes for their production, their use as pharmaceuticals and to pharmaceutical compositions comprising them.

Abstract: This invention relates to novel 8-aza-bicyclo[3.2.1]octane derivatives useful as monoamine neurotransmitter re-uptake inhibitors. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.

Abstract: The present invention relates to 1-aza-bicycloalkyl derivatives of Formula (I) wherein the substituents are as defined in the specification and to processes for their production, their use as pharmaceuticals and to pharmaceutical compositions comprising them.

Abstract: The present invention relates to new methylindazole modulators of 5-HT3 receptor activity, pharmaceutical compositions thereof, and methods of use thereof.

Abstract: Composition and methods of treating pain and reducing or reversing tolerance to opiate analgesics are disclosed. The composition and method utilize an opiate analgesic and an endothelin antagonist as active agents to treat pain in mammals, including humans.

Abstract: Disclosed are compounds having the ability to inhibit cytochrome P450 2A6, 2A13, and/or 2B6 and tobacco products comprising them. Also disclosed are pharmaceutical compositions comprising them.

Abstract: The present invention discloses novel compounds, which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.

Abstract: The present invention is directed to novel substituted pyrroline compounds useful as kinase inhibitors and methods for treating or ameliorating a kinase mediated disorder.

Abstract: The present invention provides compounds and amyloid probes thereof that allow for an antemortem method of diagnosing AD and quantitating the extent or progression of amyloid deposits (plaques) by in vivo imaging of amyloid and/or amyloid deposits in the regions of the brain. Preferably, an amyloid probe of the invention can cross the blood-brain barrier and distinguish AD brain from normal brain. An amyloid probe can be administered to a patient in amounts suitable for in vivo imaging of amyloid deposits. Amyloid probes of the invention can also be used to detect and quantitate amyloid deposits in diseases including, without limitation, Down's syndrome, familial AD and homozygotes for the apolipoprotein E4 allele. In one aspect, the compounds may be used in the treatment or prophylaxis of diseases that include, without limitation, AD and type 2 diabetes mellitus.

Abstract: Compounds represented by formula I: or pharmaceutically acceptable salts and solvates thereof, wherein R1, X, Y, Y1, and Z are as defined herein, are useful for treating flaviviridae viral infections.

Abstract: Compounds of formula (I) are CRTH2 ligands, useful in the treatment of, inter alia, respiratory diseases: wherein R1 is fluoro, chloro, cyano or trifluoromethyl; R2 is hydrogen, fluoro or chloro; R3 is hydrogen, fluoro, chloro or trifluoromethyl; X is —CH2—, —S—, —S(?O)— or —S(?O)2—; one of Y and Y1 is hydrogen and the other is —C(?O)R4, or —S(?O)2R4, or —CR5R6OR7 or a heterocyclic group selected from furanyl, thienyl, pyrrolyl, oxazolyl, thiazolyl, imidazolyl, pyrazolyl, isoxazolyl, isothiazolyl, 1,2,3-oxadiazolyl, 1,2,4-oxadiazolyl, 1,3,4-oxadiazolyl, 1,2,5-oxadiazolyl, furazanyl, 1,2,3-triazolyl, 1,2,4-triazolyl, 1,2,3-thiadiazolyl, 1,2,5-thiadiazolyl, 1,3,4-thiadiazolyl, 1,2,4-thiadiazolyl, tetrazolyl, pyridinyl, pyridazinyl, pyrimidinyl, pyrazinyl, 1,2,4-triazinyl and 1,3,5-triazinyl any of which may be optionally substituted; R4 is an optionally substituted cyclic amino group having 5, 6 or 7 ring atoms which is linked to the carbonyl or sulfonyl through a ring nitrogen; R5 and R6 are independently hydr

Abstract: New stable compositions comprising the combination of a topically active vasoconstrictor and a topically active anticholinergic drug are disclosed. Preferably, the composition comprises ipratropium or a salt thereof in combination with xylometazoline hydrochloride and a salt thereof. Upon topically administering such compositions to a nasal mucosa in individuals suffering from the common cold the symptoms of rhinorrhea are significantly reduced.

Abstract: This invention relates to chromen-2-one derivatives useful as monoamine neurotransmitter re-uptake inhibitors. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.

Abstract: According to one aspect of the present invention, a dietary composition is provided. In at least one embodiment, the dietary composition comprises a therapeutically effective amount of an admixture including a caffeine ingredient and a vasodilator ingredient. In at least another embodiment, the admixture further includes an additive selected from the group consisting of taurine, rhodiola, green tea extract, dimethylethanolamine, inositol, vitamin C, one or more B vitamins, a flowing agent, citrulline malate, and combinations thereof. In certain particular embodiments, the caffeine ingredient includes dicaffeine malate. In certain other embodiments, the vasodilator ingredient includes diarginine malate.

Abstract: The current invention provides compounds having a structure according to Formulae 1, 2, 3, and 4: wherein the A-ring, B-ring, C-ring, m, n, R25, R50, and R51 are as described in the specification. The invention also provides pharmaceutical compositions comprising compounds of Formulae 1, 2, 3, and 4, as well as methods of treating cognitive disorders, such as Alzheimer's disease. The invention further provides intermediates useful in preparing the compounds of Formulae 1, 2, 3, and 4.

Abstract: The novel benzamide derivative represented by formula (1) and the novel anilide derivative represented by formula (13) of this invention has differentiation-inducing effect, and are, therefore, useful a therapeutic or improving agent for malignant tumors, autoimmune diseases, dermatologic diseases and parasitism. In particular, they are highly effective as an anticancer drug, specifically to a hematologic malignancy and a solid carcinoma.

Abstract: The present invention pertains to the use of a PKC inhibitor in the treatment of insulin-producing cell and tissue rejection, such as islet transplantation rejection or rejection of transdifferentiated insulin-producing hepatocytes.

Abstract: The objective of the present invention is to provide a tea polyphenol composition that has reduced bitterness and astringency while containing catechins with high purity. The present invention provides a tea polyphenol composition, (A) comprising 85% by weight to 95% by weight of catechins, (B) wherein the catechins contains epigallocatechin gallate and gallocatechin gallate at a ratio of 65% by weight to 80% by weight and (C) wherein the ratio given by (epigallocatechin gallate+gallocatechin gallate)/(epicatechin+catechin+epigallocatechin+gallocatechin+epicatechin gallate+catechin gallate) is from 2 to 4.

Abstract: The invention provides compounds of formula (I), and pharmaceutically acceptable salts thereof wherein: R1, R2, R3, R4, R5, R6, R7, X and X1 are as defined herein. These compounds are useful in the manufacture of medicaments for use in the prevention or treatment of a fungal disease. Compounds of formula (I), and agriculturally acceptable salts thereof, may also be used as agricultural fungicides.

Abstract: This invention relates to novel chromen-2-one derivatives useful as monoamine neurotransmitter re-uptake inhibitors. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.

Abstract: The invention relates to a hydrochloride salt of (1R,2R,3S,5S)-3-(3,4-dichlorophenyl)-2-[(methyloxy)methyl]-8-azabicyclo[3.2.1]octane, uses of the salt as a medicament in the treatment inter alia of disorders of the central nervous system and pharmaceutical compositions and dosage forms comprising the salt.

Abstract: The present invention relates to propellant-free aerosol formulations for inhalation containing ipratropium bromide and salbutamol.

Abstract: Disclosed herein is the use of a composition, containing isoflavone-containing soybean extract, L-carnitine, caffeine and arginine as active ingredients, for the treatment of obesity and diabetes. The disclosed composition contains isoflavone-containing soybean extract, carnitine, caffeine and arginine in the form of a mixture, and thus shows not only the effect of promoting lipolysis and fat burning, but also anti-obesity and anti-diabetic effects by increasing the expressions of adiponectin and Glut4 genes to restore insulin sensitivity.

Abstract: Sheet-like dosage forms that quickly dissolve or disintegrate in an aqueous environment, for the application of active agent combinations for the treatment of hypertension. The dosage forms contain at least two active agents that are suitable for the treatment of hypertension. The antihypertensive agents are selected from the group that encompasses beta receptor blockers, alpha receptor blockers, calcium antagonists, ACE inhibitors, AT1 antagonists, centrally acting antihypertensive agents, direct vasodilators, and diuretics. The use of active agent combinations according to the invention for the production of an oral dosage form for the treatment of high blood pressure, a method for the therapeutic treatment of hypertension, and a method for the production of a sheet-like dosage form are also disclosed.

Abstract: Disclosed are a method for controlling the elution of a drug from a stent and a drug-eluting stent capable of reducing the restenosis rate after therapy. A coating composition for a drug-eluting stent comprising an endothelin receptor antagonist and a copolymer of 2-methacryloyloxyethyl phosphorylcholine and n-butyl methacrylate. The elution of the endothelin receptor antagonist from the coating composition can be controlled by varying the ratio of 2-methacryloyloxyethyl phosphorylcholine to n-butyl methacrylate in the copolymer.

Abstract: A compound of formula (I) wherein R denotes another heterocylic residue and wherein Ra, Rb, Rc, Rd and Re, are as defined in the specification, processes for their production, their uses, in particular in transplantation, and pharmaceutical compositions containing them.

Abstract: The invention relates to tetrahydronaphthalene derivatives, process for their production and their use as anti-inflammatory agents.