| 01st week of 2009 patent applcation highlights part 54 |
| Patent application number | Title | Published |
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| 20090005309 | SUBSTITUTED PIPERIDINES - Disclosed herein are substituted piperidine-based muscarinic receptor modulators of Formula I, process of preparation thereof, pharmaceutical compositions thereof, and methods of use thereof. | 2009-01-01 |
| 20090005310 | (En) Pharmaceutical Composition for Treating Haemorrhagic Shock and its Consecutive Symptoms - The invention is concerned with the use of a peptide comprising the N-terminal sequence | 2009-01-01 |
| 20090005311 | LACTOBACILLUS ACIDOPHILUS NUCLEIC ACIDS ENCODING FRUCTO-OLIGOSACCHARIDE UTILIZATION COMPOUNDS AND USES THEREOF - Fructooligosaccharide (FOS)-related protein nucleic acid molecules and polypeptides and fragments and variants thereof are disclosed in the current invention. In addition, FOS-related fusion proteins, antigenic peptides, and anti-FOS-related antibodies are encompassed. The invention also provides recombinant expression vectors containing a nucleic acid molecule of the invention and host cells into which the expression vectors have been introduced. Methods for producing the polypeptides of the invention and methods for their use are further disclosed. | 2009-01-01 |
| 20090005312 | NOVEL GLP-1 ANALOGUES LINKED TO ALBUMIN-LIKE AGENTS - Novel GLP-1 agonists which are protracted by coupling to a protraction protein. | 2009-01-01 |
| 20090005313 | ACTIVATABLE CLOSTRIDIAL TOXINS - Compositions comprising activatable recombinant neurotoxins and polypeptides derived therefrom. The invention also comprises nucleic acids encoding such polypeptides, and methods of making such polypeptides and nucleic acids. | 2009-01-01 |
| 20090005314 | Compositions and Methods for Modulating Pgc-1Alpha to Treat Neurological Diseases and Disorders - The present invention provides methods for modulating mitochondrial function, modulating lesion formation in the brain, modulating neurite growth, modulating neuronal degeneration, and treating and preventing neurological diseases or disorders comprising modulating the expression or activity of PGC-1α. The present invention also provides an animal, e.g., transgenic mouse, in which the PGC-1α gene is misexpressed. Methods for identifying compounds which are capable of treating or preventing a neurological disease or disorder are also described. | 2009-01-01 |
| 20090005315 | Vip Fragments and Methods of Use - The invention relates to composition comprising a pharmaceutically effective amount of one or more functional vasoactive intestinal peptide (VIP) fragments, and the use of those compositions in the treatment of fibrosis, hypertension and other disorders. | 2009-01-01 |
| 20090005316 | ALPHA-CONOTOXIN MII ANALOGS - The invention relates to novel conopeptides and/or novel uses of conopeptides. The conopeptides of the invention are analogs of α-Conotoxin MII that are selective for α6-containing nAChRs as described herein. | 2009-01-01 |
| 20090005317 | Methods for treating a corneal disorder and promoting skin wound healing - A method for treating a corneal disorder or for promoting skin wound healing comprising administering to a patient in need thereof a composition containing pharmaceutically effective amounts of (i) a first peptide comprising an amino acid sequence containing the following consecutive amino acids: Ser-Ser-Ser-Arg (SEQ ID NO: 1), or an analog thereof or a pharmaceutically acceptable salt thereof and (ii) a second peptide comprising an amino acid sequence containing the following consecutive amino acids with a terminal —NH | 2009-01-01 |
| 20090005318 | CONTROLLED RELEASE COMPOSITION AND METHOD OF PRODUCING THE SAME - A controlled release composition containing a physiologically active substance in high content, suppressing the initial excess release, and achieving a stable release speed over a long period of time is provided. | 2009-01-01 |
| 20090005319 | TOPICAL COMPOSITIONS FOR DELAYING EJACULATION AND METHODS OF USING THE SAME - A method, composition, and kit for topical application of a composition to a male penis to delay premature ejaculation during intercourse without adversely affecting response in a female partner are disclosed. The method includes applying to the penis a topical composition immediately prior to intercourse. The composition includes an effective amount of a vasodilator agent and a desensitizing agent such as an acetyl dipeptide-1 cetyl ester. | 2009-01-01 |
| 20090005320 | COMPOSITIONS COMPRISING AMINO ACID BICARBONATE AND METHODS OF USE THEREOF - The invention relates to compositions comprising one or more ionic salts, each of said ionic salts consisting of a bicarbonate anion and a cation selected from the group consisting of an amino acid, an amino acid derivative, a di-peptide and a tri-peptide, and to methods of making and using said compositions. | 2009-01-01 |
| 20090005321 | Phenylazetidinone Derivatives - Various azetidinone derivatives are described, as are pharmaceutical compositions containing these compounds and methods of treatment of diseases using these compounds. Other embodiments are also described. | 2009-01-01 |
| 20090005322 | Physiologically- Active Composition Based on Collagen - The present invention concerns a physiologically active composition which contains an enzymatically hydrolysed collagen as the active component I and at least one component of the non-vitamin type having anti-oxidative and/or anti-inflammatory properties as the active component II. Collagen of animal origin that is soluble in cold water comes into particular consideration as component I and a fermentation broth or a plant extract comes into particular consideration as component II. This composition which is designed in particular as a food supplement or functional food can be used to prevent inflammatory and/or degenerative symptoms in particular with a chronic course such as for example arthritis and arthroses or to successfully treat these symptoms. The claimed composition can be used above all by professional, leisure and recreational athletes who suffer in particular from strained joint functions. | 2009-01-01 |
| 20090005323 | Cathepsin K Inhibitors and Obesity - This invention relates to the treatment of obesity, the treatment of obesity related disorders, prevention of weight gam, prevention of weight regain or for weight maintenance by the use of a cathepsin K inhibitor as active ingredient, alone or in conjunction with other anti-obesity agents The invention also relates to the pharmaceutical compositions comprising cathepsin K inhibitor as active ingredient, pharmaceutically acceptable carriers or excipients, and optionally one or more anti-obesity agents. | 2009-01-01 |
| 20090005324 | Biologically active extract from dendrobium plant, use thereof and process for preparing the same - A substance having the following formula is provided. | 2009-01-01 |
| 20090005325 | Ketolide Derivatives as Antibacterial Agents - Provided herein are ketolide derivatives, which can be used as antibacterial agents. Compounds described herein can be used for treating or preventing conditions caused by or contributed to by gram positive, gram negative or anaerobic bacteria, more particularly against, for example, | 2009-01-01 |
| 20090005326 | SINGLE DOSE ROXITHROMYCIN - The invention relates to a method of treating a bacterial infection in an animal by administering a single dose of roxithromycin. | 2009-01-01 |
| 20090005327 | ESSENTIAL N-3 FATTY ACIDS IN CARDIAC IN SUFFICIENCY AND HEART FAILURE THERAPY - The present invention concerns a method of therapeutic prevention and treatment of a heart disease chosen from cardiac insufficiency and heart failure including the administration of an essential fatty acid containing a mixture of eicosapentaenoic acid ethyl ester (EPA) and docosahexaenoic acid ethyl ester (DHA), either alone or in combination with another therapeutic agent. | 2009-01-01 |
| 20090005328 | METHODS OF MODULATING TUBULIN DEACETYLAST ACTIVITY - The present invention provides methods for identifying agents that modulate a level or an activity of tubulin deacetylase polypeptide, as well as agents identified by the methods. The invention further provides methods of modulating tubulin deacetylase activity in a cell. The invention further provides methods of modulating cellular proliferation by modulating the activity of tubulin deacetylase. | 2009-01-01 |
| 20090005329 | NUCLEIC ACID BASED LADDER COPOLYMERS - The present invention relates to a copolymer termed a ladder copolymer because it has two backbones that serve as legs/sides of a ladder structure. These two backbones, one of which is a nucleic acid or nucleic acid-like polymer, are linked together as the legs/sides of a ladder are linked together by the rungs. | 2009-01-01 |
| 20090005330 | Methods and Compositions to Inhibit P2x7 Receptor Expression - Methods and compositions for the downregulation of P2X7 receptor expression or activity are disclosed. Preferred compositions comprise siNA. The methods and compositions are useful in the treatment of diseases characterised by increased 112X7 receptor activity, such as neuronal degeneration, Alzheimer's disease, inflammatory diseases, and some cancers. | 2009-01-01 |
| 20090005331 | AChE antisense oligonucleotide as an anti-inflammatory agent - Disclosed is a novel use for AChE antisense oligonucleotides as anti-inflammatory agents, wherein said oligonucleotides are preferably as denoted by SEQ ID NO:1, SEQ ID NO:2 and SEQ ID NO:7. Methods of treatment of inflammatory conditions, as well as fever, and particularly inflammation-associated neuropathies such as Guillain-Barré Syndrome, are described. | 2009-01-01 |
| 20090005332 | Compositions and Methods for Modulating Gene Expression Using Self-Protected Oligonucleotides - The present invention is directed to novel nucleic acid molecules which include a region complementary to a target gene and one or more self-complementary regions, and the use of such nucleic acid molecules and compositions comprising the same to modulate gene expression and treat a variety of diseases and infections. | 2009-01-01 |
| 20090005333 | REDUCING CULLING IN HERD ANIMALS GROWTH HORMONE RELEASING HORMONE (GHRH) - One aspect of the current invention is a method of decreasing an involuntary cull rate in farm animals, wherein the involuntary cull results from infection, disease, morbidity, or mortality. Additionally, milk production, animal welfare, and body condition scores are improved by utilizing methodology that administers the isolated nucleic acid expression construct encoding a GHRH or functional biological equivalent to an animal through a parenteral route of administration. Following a single dose of nucleic acid expression vector, animals are healthier and effects are demonstrated long term without additional administration(s) of the expression construct. | 2009-01-01 |
| 20090005334 | Nucleic acid derivatives - A compound which comprises a backbone having a plurality of chiral carbon atoms, the backbone bearing a plurality of ligands each being individually bound to a chiral carbon atom of the plurality of chiral carbon atoms, the ligands including one or more pair(s) of adjacent ligands each containing a moiety selected from the group consisting of a naturally occurring nucleobase and a nucleobase binding group, wherein moieties of the one or more pair(s) are directly linked to one another via a linker chain; building blocks for synthesizing the compound; and uses of the compound, particularly in antisense therapy. | 2009-01-01 |
| 20090005335 | COMPOUNDS FOR THE MODULATION OF BETA-CATENIN EXPRESSION - The invention relates to oligomer compounds (oligomers), which target beta-catenin mRNA in a cell, leading to reduced expression of beta-catenin. Reduction of beta-catenin expression is beneficial for a range of medical disorders, such as hyperproliferative disorders, such as cancer. The invention provides therapeutic compositions comprising oligomers and methods for modulating the expression of beta-catenin using said oligomers, including methods of treatment. | 2009-01-01 |
| 20090005336 | Use of the microRNA miR-1 for the treatment, prevention, and diagnosis of cardiac conditions - Among >300 miRNAs known to date, miR-1 is considered muscle-specific. Here we show that that miR-1 overexpressed in individuals with coronary artery disease, and when overexpressed, it exacerbated arrhythmogenesis in both infarcted and normal hearts of rats whereas elimination of miR-1 by its antisense inhibitor relieved it. MiR-1 rendered slowed conduction and depolarized membrane by post-transcriptionally repressing KCNJ2 and GJA1 genes, likely accounting for its arrhythmogenic potential. Thus, miR-1 may have important pathophysiological functions in heart, being a novel antiarrhythmic target useful in the treatment and prevention of various cardiac pathologies. | 2009-01-01 |
| 20090005337 | Pde11a Mutations in Adrenal Disease - The invention provides previously uncharacterized variants of PDE11A that are correlated with a newly discovered form of Cushing Syndrome that presents at a young age. The invention also provides methods useful to research, screen for, treat, or prevent diagnose the disease using the PDE11A variants, as well as other methods relating thereto. | 2009-01-01 |
| 20090005338 | Carbonyl-substituted titanocenes - A medicament containing a compound of the following formulas (Ia) and (Ib): | 2009-01-01 |
| 20090005339 | Methods of Treating Ear Infections - Methods of treating and/or preventing otitis media in a subject are provided. Methods of treating and/or preventing otitis externa are also provided. | 2009-01-01 |
| 20090005340 | Bioactive Agents Produced By Submerged Cultivation of a Basidiomycete Cell - The invention in one aspect is directed to a method for cultivating a Basidiomycete cell in liquid culture medium, said method comprising the steps of providing a Basidiomycete cell capable of being cultivated in a liquid growth medium, and cultivating the Basidiomycete cell under conditions resulting in the production intracellularly or extracellularly of one or more bioactive agent(s) selected from the group consisting of oligosaccharides, polysaccharides, optionally glycosylated peptides or polypeptides, oligonucleotides, polynucleotides, lipids, fatty acids, fatty acid esters, secondary metabolites such as polyketides, terpenes, steroids, shikimic acids, alkaloids and benzodiazepine, wherein said bioactive agent comprises one or more desirable activities, such as anti-tumour activity, immune stimulating activity, and enhancement of survival of an individual. | 2009-01-01 |
| 20090005341 | PROCESS FOR THE PREPARATION OF N-ACYL-(EPI)K5-AMINE-O-SULFATE-DERIVATIVES AND PRODUCTS THUS OBTAINED - A new method is described for the oversulfation of (epi)K5-N-sulfates to obtain (epi)K5-amine-O-oversulfates at extremely high degree of sulfation and for the transformation of these intermediates into new N-acyl-(epi)K5-amine-O-oversulfates basically free of activity on the coagulation parameters and useful in the cosmetic or pharmaceutical field. Also described are pharmaceutical compositions containing, as one of their active ingredients, an (epi)K5-amine-O-oversulfate. | 2009-01-01 |
| 20090005342 | Composition Having Blood Pressure Reducing and/or Elevation Suppressing Effect and Food and Drink Containing the Same - The present invention regards the composition having a blood pressure reducing and/or elevation suppressing effect comprising a mannose-based oligosaccharide mass comprising 1 to 10 molecules of monosaccharides linked together, said molecules mainly comprising mannose. It is the object of the present invention to provide an economical and simple food and drink which has an excellent blood pressure reducing and/or elevation suppressing effect without changing ordinary eating habits much, and a composition ingestible with a food and drink which effectively uses waste resources such as coffee extraction residues. | 2009-01-01 |
| 20090005343 | B-CYCLODEXTRIN DERIVATIVES AND THEIR USE AGAINST ANTHRAX LETHAL TOXIN - The invention provides low molecular weight compounds that block the pore formed by protective antigen and inhibit anthrax toxin action. Structures of the compounds are derivatives of β-cyclodextrin. Per-substituted alkylamino derivatives displayed inhibitory activity, and they were protective against anthrax lethal toxin action at low micromolar concentrations. Also, the addition of one of the alkylamino derivatives to the bilayer lipid membrane with multiple PA channels caused a significant decrease in membrane conductance. Thus, the invention also provides methods for protection against anthrax toxicity. | 2009-01-01 |
| 20090005344 | Compounds and Methods of Use Thereof - Imidazole and benzimidazole boronic acid compounds, analogs thereof, and pharmaceutical formulations are described, along with methods of use thereof for inhibiting inflammatory cytokines such as tumor necrosis factor alpha (TNF-α) in a subject in need thereof. | 2009-01-01 |
| 20090005345 | Detoxification of Shellfish - The present invention relates to the detoxification of bivalves and other shellfish. More particularly, the invention relates to a feed composition and a method for detoxifying shellfish, and the use of a surface-active agent for the detoxification of bivalves and other shellfish. | 2009-01-01 |
| 20090005346 | Azacytosine Derivatives Useful as Antiviral Agents - The present invention provides 5-azacytosine derivatives with antiviral activity, specifically having viral replication inhibiting properties, more particularly in DNA viruses such as pox-, papilloma- and herpes viruses in humans. The invention also provides pharmaceutical compositions comprising such 5-azacytosine derivatives as active ingredients in combination with pharmaceutically acceptable carriers, which are useful for the treatment of subjects suffering from viral infections. | 2009-01-01 |
| 20090005347 | DRUG FOR THE TREATMENT OF OSTEONECROSIS AND FOR THE MANAGEMENT OF PATIENTS AT RISK OF DEVELOPING OSTEONECROSIS - A bisphosphonate for the treatment of osteonecrosis and/or osteonecrosis dissecans. The drug may further be used to prevent the onset of osteonecrosis and/or osteonecrosis dissecans and any complications associated with both diseases. | 2009-01-01 |
| 20090005348 | Compounds Having Cytokine Modulating Properties - A method of modulating one or more immuno-regulatory cytokines, such as pro-inflammatory and/or anti-inflammatory cytokines, comprising administering to a subject a therapeutically effective amount of one or more phosphate derivatives of one or more hydroxy chromans, or complexes thereof. | 2009-01-01 |
| 20090005349 | THERAPEUTIC USES OF GLUTATHIONE MIMICS - A prodrug having antioxidant activity, including a phosphorylated compound having a thiol group. A method of treating oxidative stress by administering a prodrug of a phosphorylated compound including a thiol group, removing a phosphate group of the prodrug, and treating oxidative stress. A method of increasing bioavailability of a thiol compound by creating a prodrug by phosphorylating a thiol compound, administering the prodrug, preventing first pass metabolism of the prodrug, removing a phosphate group from the prodrug, and providing active drug to a site in need of therapy from oxidative stress. A method of preventing radiation damage to healthy tissue by administering a prodrug comprising a phosphorylated compound including a thiol group, removing a phosphate group of the prodrug to provide active drug, and preventing radiation damage to healthy tissue. | 2009-01-01 |
| 20090005350 | CYCLOOXYGENASE-2 SELECTIVE INHIBITORS, COMPOSITIONS AND METHODS OF USE - The invention describes novel cyclooxygenase 2 (COX-2) selective inhibitors and novel compositions comprising at least one cyclooxygenase 2 (COX-2) selective inhibitor, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or at least one therapeutic agent. The invention also provides novel kits comprising at least one COX-2 selective inhibitor, optionally nitrosated and/or nitrosylated, and, optionally, at least one nitric oxide donor, and/or, optionally, at least one therapeutic agent. The novel cyclooxygenase 2 selective inhibitors of the invention can be optionally nitrosated and/or nitrosylated. The invention also provides methods for treating inflammation, pain and fever; for treating and/or improving the gastrointestinal properties of COX-2 selective inhibitors; for facilitating wound healing; for treating and/or preventing renal and/or respiratory toxicity; for treating and/or preventing other disorders resulting from elevated levels of cyclooxygenase-2; and for improving the cardiovascular profile of COX-2 selective inhibitors. | 2009-01-01 |
| 20090005351 | Hormone replacement therapy - This invention relates to methods and pharmaceutical compositions for providing hormone replacement therapy in perimenopausal, menopausal, and postmenopausal women through the continuous administration of combinations of conjugated estrogens and medroxyprogesterone acetate. | 2009-01-01 |
| 20090005352 | Prodrugs of Propofol, Compositions and Uses Thereof - The present invention provides propofol prodrugs, methods of making propofol prodrugs, pharmaceutical compositions of propofol prodrugs and methods of using propofol prodrugs and pharmaceutical compositions thereof to treat or prevent diseases or disorders such as migraine headache pain and post-chemotherapy or post-operative surgery nausea and vomiting. | 2009-01-01 |
| 20090005353 | Non-Anilinic Derivatives of Isothiazol-3(2H)-one 1,1-Dioxides as Liver X Receptor Modulators - The present invention relates to certain novel compounds of the formula (I) | 2009-01-01 |
| 20090005354 | New Amino Derivatives and Their Use as Pharmaceuticals - The present invention provides for compounds of formula (I): | 2009-01-01 |
| 20090005355 | Piperidine Compound and Process for Preparing the Same - The present invention is to provide a piperidine compound represented by the formula [I]: | 2009-01-01 |
| 20090005356 | SUBSTITUTED PYRROLOPYRIDINES AND PYRAZOLOPYRIDINES AS KINASE MODULATORS - Provided herein are substituted pyrrolopyridine heterocycles and substituted pyrazolopyridine heterocycles, pharmaceutical compositions comprising said heterocycles and methods of using said heterocycles in the treatment of disease. The heterocycles disclosed herein function as kinase modulators and have utility in the treatment of diseases such as cancer, allergy, asthma, inflammation, obstructive airway disease, autoimmune diseases, metabolic disease, infection, CNS disease, brain tumor, obesity, asthma, hematological disorder, degenerative neural disease, cardiovascular disease, or disease associated with angiogenesis, neovascularization, or vasculogenesis. | 2009-01-01 |
| 20090005357 | Pharmacological Treatment for Sleep Apnea - The present invention relates generally to pharmacological methods for the prevention of amelioration of sleep-related breathing disorders via administration of agents or combinations of agents that possess serotonin-related pharmacological activity. | 2009-01-01 |
| 20090005358 | Compositions and methods for treating medical conditions - The invention features methods, compositions, and kits for the treatment of pain or pruritus in a patient. In one embodiment, the methods, compositions, and kits of the invention provide for a combination therapy including a tricyclic compound and a tetra-substituted pyrimidopyrimidine. | 2009-01-01 |
| 20090005359 | Heterocyclic Compounds Useful as RAF Kinase Inhibitors - The present invention provides compounds useful as inhibitors of Raf protein kinase. The present invention also provides compositions thereof, and methods of treating Raf-mediated diseases. | 2009-01-01 |
| 20090005360 | Modified release preparations containing oxcarbazepine and derivatives thereof - Controlled-release preparations of oxcarbazepine and derivatives thereof for once-a-day administration are disclosed. The inventive compositions comprise solubility- and/or release enhancing agents to provide tailored drug release profiles, preferably sigmoidal release profiles. Methods of treatment comprising the inventive compositions are also disclosed. | 2009-01-01 |
| 20090005361 | Combination of Organic Compounds - The present invention relates to a combination, such as a combined preparation or pharmaceutical composition, respectively, comprising a therapeutic agent acting on the renin-angiotensin system (RAS) or a pharmaceutically acceptable salt thereof and comprising at least one CB1 antagonist, or a pharmaceutically acceptable salt thereof. The present invention furthermore relates to the use of such a combination for the prevention of, delay of progression of, treatment of diseases and disorders that may be modulated by action on the renin-angiotensin system (RAS), appetency disorders or substance abuse disorders. | 2009-01-01 |
| 20090005362 | Compositions Comprising Antihistamines or Mast Cell Stabilizers, and Methods of Making and Using Same - Compositions comprise: (a) a material selected from the group consisting of antihistamines, stabilizers, salts thereof, and combinations thereof; and (b) a vasoconstrictor, decongestant, or a salt thereof, provided when the material consists of an antihistamine or a salt thereof, at least one antihistamine other than ketotifen and salts thereof is present. In certain embodiments, the compositions have a pH maintainable at about 5 or less during storage. The compositions can be used to treat, alleviate or ameliorate ocular allergic conditions. | 2009-01-01 |
| 20090005363 | Organic Compounds - The present invention relates to novel nicotinic acid derivatives, of formula (I) | 2009-01-01 |
| 20090005364 | Azole Derivatives With Antimuscarinic Activity - The present invention relates to compounds of formula (I) wherein R1, R2, x, X, Y and B are as defined in the description for the treatment of muscarinic acetylcholine receptor mediated diseases, in particular M3 muscarinic receptor mediated diseases. | 2009-01-01 |
| 20090005365 | THERAPEUTIC PYRAZOLONAPHTHYRIDINE DERIVATIVES - The invention provides a novel chemical series of formula I, as well as methods of use thereof for binding to the benzodiazepine site of the GABA | 2009-01-01 |
| 20090005366 | DEUTERIUM-ENRICHED OLANZAPINE - The present application describes deuterium-enriched olanzapine, pharmaceutically acceptable salt forms thereof, and methods of treating using the same. | 2009-01-01 |
| 20090005368 | Ethanol or 1,2-Ethanediol Cyclohexyl Antibiotic Derivatives - The invention relates to antibiotic ethanol or 1,2-ethanediol cyclohexyl derivatives of formula (I) wherein R1 represents (C | 2009-01-01 |
| 20090005369 | Oxazolidinone Compounds and Compositions and Methods Related Thereto - The invention provides new oxazolidinones of formula (I), where R1, R2, R3 and R4 are independently selected from H, F and Cl; A is certain heterocycles optionally substituted; X is selected from O, S, NR8 and CR8R9; R8 and R9 having different meanings; Y is selected from O, S, SO, SO2, NO, NR11 and CR11R12; R11 and R12 having different meanings; and n is selected from 0 and 1. It also provides different processes for the preparation of such compounds. Oxazolidinones compounds of formula (I) are active against Gram-positive and some Gram-negative human and veterinary pathogens with a weak monoamine oxidase (MAO) inhibitory activity. They are useful for the treatment of bacterial infections. | 2009-01-01 |
| 20090005370 | ISOXAZOLE-IMIDAZOLE DERIVATIVES - The present invention is concerned isoxazole-imidazole derivatives having affinity and selectivity for GABA A α5 receptor binding site, their manufacture, pharmaceutical compositions containing them and their use for enhancing cognition or for the treatment of cognitive disorders like Alzheimer's disease. In particular, the present invention is concerned with aryl-isoxazol-4-yl-imidazole derivatives of formula I | 2009-01-01 |
| 20090005371 | Substituted Fused [1,2]Imidazo[4,5-C] Ring Compounds and Methods - Fused [1,2]imidazo[4,5-c] ring compounds, e.g., fused [1,2]imidazo[4,5-c]quinolines and [1,2]imidazo[4,5-c]naphthyridines, with a substituent, e.g., a substituted alkoxy substituent, at the 6, 7, 8, or 9-position, pharmaceutical compositions containing the compounds, intermediates, methods of making and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are disclosed. | 2009-01-01 |
| 20090005372 | Triazolophthalazines - The compounds of formula I | 2009-01-01 |
| 20090005373 | SUBSTITUTED SULFONAMIDO-MACROCYCLES AS TIE2 INHIBITORS AND SALTS THEREOF, PHARMACEUTICAL COMPOSITIONS COMPRISING SAME, METHODS OF PREPARING SAME AND USES OF SAME - The invention relates to substituted sulfonamido-macrocycles according to the general formula (I): | 2009-01-01 |
| 20090005374 | IMIDAZOPYRIDINYL THIAZOLYL HISTONE DEACETYLASE INHIBITORS - A compound of general Formula (I) having histone deacetylase (HDAC) and/or CDK inhibitory activity, a pharmaceutical composition comprising the compound, and a method useful to treat diseases using the compound. | 2009-01-01 |
| 20090005375 | ACETYL COENZYME A CARBOXYLASE INHIBITORS - The present invention relates to acetyl coenzyme-A carboxylase (“ACC”) inhibiting compounds of the formula | 2009-01-01 |
| 20090005376 | 1-Alkoxy 1H-Imidazo Ring Systems and Methods - Imidazo-containing compounds (e.g., imidazonaphthyridines, imidazopyridines, imidazoquinolines, and imidazote-trahydroquinolines) with an alkoxy substituent at the 1-position, pharmaceutical compositions containing the compounds and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are disclosed. | 2009-01-01 |
| 20090005377 | Pyrazolopyridine Derivates - New compounds of formula (I) and the salts thereof, wherein the meanings for the various substituents are as disclosed in the description, are useful as p38 kinase inhibitors. | 2009-01-01 |
| 20090005378 | PYRROLO-PYRIDINE KINASE MODULATORS - The present invention provides novel pyrrolo-pyridine kinase modulators and methods of using the novel pyrrolo-pyridine kinase modulators to treat diseases mediated by kinase activity. | 2009-01-01 |
| 20090005379 | Azaindole-2-Carboxamide Derivatives - The present invention relates to compounds of formula (I) wherein R | 2009-01-01 |
| 20090005380 | CYCLOHEXYL DERIVATIVES - The present invention relates to compounds of formula I | 2009-01-01 |
| 20090005381 | METHODS OF TREATING SEROTONIN-MEDIATED DISEASES AND DISORDERS - Methods are disclosed for treating serotonin-mediated diseases and disorders, which comprise inhibiting tryptophan hydroxylase (TPH) in patients in need thereof. | 2009-01-01 |
| 20090005382 | METHODS OF USING AND COMPOSITIONS COMPRISING TRYPTOPHAN HYDROXYLASE INHIBITORS - Methods and compositions comprising tryptophan hydroxylase inhibitors are disclosed. Particular methods are directed at reducing or avoiding serotonin-mediated adverse effects associated with some drugs. | 2009-01-01 |
| 20090005383 | THYROID HORMONE ANALOGS - Provided herein are compounds of the formula (I): | 2009-01-01 |
| 20090005384 | Method for Producing Adsorptive Porous Body - The present invention relates to a method for producing a 2-benzyl-5-(4-chlorophenyl)-6-[4-(methylthio)phenyl]-2H-pyridazin-3-one adsorptive porous material characterized by treating a porous material with a halogen-containing organic solvent in which 2-benzyl-5-(4-chlorophenyl)-6-[4-(methylthio)phenyl]-2H-pyridazin-3-one is dissolved. The production method of the present invention is simple and easy, and the obtained adsorptive porous material is excellent in dissolution properties of 2-benzyl-5-(4-chlorophenyl)-6-[4-(methylthio)phenyl]-2H-pyridazin-3-one. | 2009-01-01 |
| 20090005385 | Treatment or Prevention of Cancer or Cardiovascular Disease with Methenyltetrahydrofolate Synthetases - The present invention relates to a method of screening test substances for chemotherapeutic activity or for efficacy in treating cardiovascular disease by providing one or more cells transformed with a nucleic acid molecule encoding methenyltetrahydrofolate synthetase, contacting the cells with test substance(s), and identifying those test substances which modulate methenyltetrahydrofolate synthetase expression as candidates for such therapeutic use. Another aspect of the present invention relates to a method of measuring folate status in a sample by measuring methenyltetrahydrofolate synthetase expression or activity and/or catecholamine activity in the sample, all of which are correlated to folate status in the sample. The present invention can also be used to treat or prevent cancer or cardiovascular disease in a subject by administering to the subject a substance which modulates methenyltetrahydrofolate synthetase expression or activity and/or catecholamine activity. | 2009-01-01 |
| 20090005386 | Methods for Modulating Ion Channels - In one embodiment, the invention provides an ion having the formula: (I) In another embodiment, the invention provides a method for modulating potassium, sodium, and cyclic nucleotide-modulated ion channels in a mammal in need thereof. In a further embodiment, the invention provides a method for modulating ligand-gated ion channels or transient receptor potential channels in a mammal in need thereof. The methods comprise administering an ion having the formula described above. | 2009-01-01 |
| 20090005387 | QUINOXALINYL MACROCYCLIC HEPATITIS C VIRUS SERINE PROTEASE INHIBITORS - The present invention relates to compounds, including compounds of Formula I, or a pharmaceutically acceptable salt, ester, or prodrug, thereof: | 2009-01-01 |
| 20090005388 | 3-Heteroaryl-3,9-Diazabicyclo[3.3.1]Nonane Derivatives as Nicotinic Acetylcholine Receptor Agonists - This invention relates to novel 3,9-diazabicyclo[3.3.1]nonane derivatives which are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances. | 2009-01-01 |
| 20090005389 | 2,5 Diaza-Bicyclo [2.2.1] Heptane Derivatives as Calcium Channel Blockers - 2,5-diaza-bicyclo[2.2.1]heptane derivatives represented by Formula (I), or pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by, sodium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, urinary incontinence, itchiness, allergic dermatitis, epilepsy, irritable bowel syndrome, depression, anxiety, multiple sclerosis, bipolar disorder and stroke, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds. | 2009-01-01 |
| 20090005390 | NOVEL QUINUCLIDINE DERIVATIVES AND THEIR USE - This invention relates to novel quinuclidine derivatives and their use as pharmaceuticals. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances. | 2009-01-01 |
| 20090005391 | Tricyclo Substituted Amides - Compounds of Formula (I) or pharmaceutically acceptable salts thereof, are useful in the prophylactic and therapeutic treatment of hyperglycemia and diabetes. | 2009-01-01 |
| 20090005392 | CRYSTAL OF 6-[4-(4-PYRIDYLAMINO) PHENYL]-4,5-DIHYDRO-3(2H-PYRIDAZINONE HYDROCHLORIDE TRIHYDRATE - The present invention provides crystals of 6-[4-(4-pyridylamino)phenyl]-4,5-dihydro-3(2H)-pyridazinone hydrochloride trihydrate useful as a medicament for therapeutic treatment of cardiac failure, and the like; and a pharmaceutical composition comprising said crystals as an active ingredient. | 2009-01-01 |
| 20090005393 | Pyridine and Pyrimidine Derivatives as Inhibitors of Histone Deacetylase - This invention comprises the novel compounds of formula (I) | 2009-01-01 |
| 20090005394 | Endothelin receptor antagonists - This invention relates to novel endothelin receptor antagonists, derivatives, acceptable acid addition salts, solvates, hydrates and polymorphs thereof. The invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by compounds that block the endothelin signaling pathway that leads to vasoconstriction and in particular those diseases or conditions beneficially treated by endothelin receptor antagonists. | 2009-01-01 |
| 20090005395 | SILDENAFIL N-OXIDE AS PRODRUG - Embodiments of the present invention relate to a compound of formula (1 | 2009-01-01 |
| 20090005396 | Use of Pyrazolyl-Pyrimidine Derivatives in the Treatment of Pain - This invention relates to the use of a pyrazolyl-pyrimidine of the formula (I). n=0, 1, 2 or 3 (I) in the manufacture of a medicament for use in the treatment or prophylaxis of pain. and to their pharmaceutical formulations and to their methods of use. | 2009-01-01 |
| 20090005397 | Substituted Oxindol Derivatives and Medicaments Containing the Same - The invention relates to novel oxindol derivatives of general formula (1) wherein the substituents A, B, R | 2009-01-01 |
| 20090005398 | Methods For The Treatment of Central Nervous System Tumors - Methods for the treatment of primary and secondary central nervous system tumors in a mammal which comprise administration of a benzimidazole thiophene compound are provided. | 2009-01-01 |
| 20090005399 | Substituted Imidazo[2,1-b]thiazole Compounds and Uses Thereof - Substituted imidazo[2,1-b]thiazole compounds corresponding to formula I, | 2009-01-01 |
| 20090005400 | Biologically Active Aphrocallistin Compounds - The subject invention provides novel compositions of biologically active compounds which can advantageously be used in blocking cellular proliferation and/or treatment of cancer. | 2009-01-01 |
| 20090005401 | Novel Compounds - This invention relates to a novel group of 8-Alkyl/Aryl-4-aryl-2-N-(alkylamino)-N″-substituted-N′-cyanoguanidino-8H-pyrido[2,3-d]pyrimidin-7-one compounds, processes for the preparation thereof, the use thereof in treating CSBP/p38 kinase mediated diseases and pharmaceutical compositions for use in such therapy. | 2009-01-01 |
| 20090005402 | Medicine containing pyrimidine derivative - A drug for central diseases which contains a compound represented by general formula (I), or a pharmacologically acceptable salt thereof, as active component | 2009-01-01 |
| 20090005403 | Alkinyl-Oxypyrimidines Used in the Form of Pesticides - The invention relates to compounds of the formula (I), | 2009-01-01 |
| 20090005404 | Pyridylsulfonamido pyrimidines for treating diabetic nephropathy - The present invention relates to the use of a compound of formula (I) wherein R | 2009-01-01 |
| 20090005405 | COMPOSITIONS AND METHODS FOR TREATING AND PREVENTING DERMATOSES - The invention encompasses protectant agents including uracil or a metabolite thereof that effectively prevent and/or treat the cutaneous toxicities and dermatological side-effects associated with chemotherapeutic agents. Additionally, and surprisingly compositions including uracil or a metabolite thereof are effective for treating or preventing various dermatoses. | 2009-01-01 |
| 20090005406 | Cancer Treatment Method - The present invention relates to a method of treating cancer in a mammal by administration of pyrimidine derivatives. In particular, the method relates to a method of treating cancer by administration of 5-[[4-[(2,3-Dimethyl-2H-indazol-6-yl)methylamino]-2-pyrimidinyl]amino]-2-methylbenzenesulfonamide or a salt or solvate thereof. | 2009-01-01 |
| 20090005407 | PARTICULATE (3'-CHLOROBIPHENYL-4-YL)(1-(PYRIMIDIN-2-YL)PIPERIDIN-4-YL)METHANONE AND METHODS OF ITS USE - Particulate (3′-chlorobiphenyl-4-yl)(1-(pyrimidin-2-yl)piperidin-4-yl)methanone is disclosed. Also disclosed are pharmaceutical formulations and dosage forms comprising particulate (3′-chlorobiphenyl-4-yl)(1-(pyrimidin-2-yl)piperidin-4-yl) and methods of their use. | 2009-01-01 |
| 20090005408 | PROCESS FOR THE PRODUCTION OF AN ABUSE-PROOFED DOSAGE FORM - The present invention relates to a process for the production of abuse-proofed, thermoformed dosage forms containing, apart from one or more active ingredients with potential for abuse and optionally physiologically acceptable auxiliary substances, at least one synthetic or natural polymer with a breaking strength of at least 500 N. | 2009-01-01 |
| 20090005409 | Pyrrolo[3,2-C] Pyrdine Derivatives and Processes for the Preparation Thereof - The present invention provides novel pyrrolo[3,2-c]pyridine derivatives or pharmaceutically acceptable salts thereof, processes for the preparation thereof, and compositions comprising the same. The pyrrolo[3,2-c]pyridine derivatives or pharmaceutically acceptable salts thereof of the present invention have excellent proton pump inhibition effects and possess the ability to attain a reversible proton pump inhibitory effect. | 2009-01-01 |
