06th week of 2010 patent applcation highlights part 45 |
Patent application number | Title | Published |
20100035810 | ADIPONECTIN PRODUCTION ENHANCER - The present invention relates to an adiponectin production enhancer comprising sericin as an active ingredient, and to a pharmaceutical composition and food and drink comprising sericin. These are effective in the prevention and/or amelioration of various diseases caused by reduction of blood adiponectin level such as arteriosclerosis, fatty liver and diabetes associated with obesity. The enhancer, the pharmaceutical composition and the food and drink according to the invention have excellent adiponectin production enhancing effects as well as high safety and are expected to be broadly applied to a variety of pharmaceutical preparations and food and drink. | 2010-02-11 |
20100035811 | Phosphoinositide Modulation For The Treatment Of Neurodegenerative Diseases - The present invention relates to the use of agents that inhibit the toxic effects of amyloid oligomers by increasing intracellular levels of phosphoinositol 4-phosphate (PI(4)P, or “PIP”) and/or phosphotidylinositol 4,5-biphosphate (PI(4,5)P2 or “PIP2”), the use of such agents for the treatment of neurodegenerative diseases, methods of treating neurodegenerative diseases by administration of agents which alter lipid metabolism, and methods of identifying agents which alter the association of presenilins with γ-secretase and lipid rafts. | 2010-02-11 |
20100035812 | Modified Bovine G-CSF Polypeptides And Their Uses - Modified bovine G-CSF polypeptides and uses thereof are provided. | 2010-02-11 |
20100035813 | RECOMBINANT E-SELECTIN MADE IN INSECT CELLS - The inventive features include recombinant mammalian E-selectin peptides, nucleic acids encoding said peptides, vectors and cells having these nucleic acids, and methods of making the peptides. Further inventive features include methods of treating diseases and conditions associated with inflammation using recombinant mammalian E-selectin peptides to induce mucosal tolerance to E-selectin. | 2010-02-11 |
20100035814 | N-Terminal Pegylated Prolactin Receptor Molecules - The invention is concerned with N-terminally pegylated polypeptides capable of binding to the prolactin receptor. Such polypeptides may for instance be N-terminally pegylated antagonists of the prolactin receptor, such as for instance prolactin variants. | 2010-02-11 |
20100035815 | SKIN WOUND HEALING COMPOSITIONS AND METHODS OF USE THEREOF - A wound healing composition comprising an amount of heat shock protein effective to promote wound healing and a method thereof to apply the composition. A preferred heat shock protein is either full-length hsp90α or the middle domain plus the charged sequence of hsp90α. The composition is topically applied to skin wounds, covering the outer surface of the wound. The heat shock protein acts by promoting migration of both human epidermal keratinocyte and dermal fibroblasts to the wound in order to close, heal, and remodel the wound. | 2010-02-11 |
20100035816 | MEDICAMENT COMPRISING A PEPTIDE EXTRACT OF AVOCADO, WHICH IS INTENDED FOR THE TREATMENT AND PREVENTION OF ILLNESSES THAT ARE LINKED TO AN IMMUNE SYSTEM DEFICIENCY OR OXIDATIVE STRESS OR SKIN AGEING OR DRY SKIN - The invention relates to a medicament which comprises a peptide extract of avocado and which can also comprise a composition containing D-mannoheptulose an/or perseitol, such as a water-soluble extract of avocado sugars, and/or a peptide extract of lupine. The inventive medicament is intended for the treatment and/or prevention of illnesses that are linked to an alteration in innate and/or acquired immunity, through an increase in the production of anti-microbial peptides, preferably hBD-2, without inducing inflammatory reactions, irritations or intolerances. | 2010-02-11 |
20100035817 | METHOD FOR THE PRODUCTION OF CONJUGATES OF INSULIN-LIKE GROWTH FACTOR-1 AND POLY(ETHYLENE GLYCOL) - The present invention relates to a fusion protein comprising IGF-I or an IGF-I variant N-terminally linked to the C-terminus of a propeptide. The invention relates also to a method involving the use of the aforementioned fusion protein in the production of a lysine-PEGylated IGF-I or IGF-I variant. The method comprises the steps of cultivating a prokaryotic host cell comprising an expression vector containing a nucleic acid encoding the fusion protein and causing the cell to express the fusion protein, recovering and PEGylating said fusion protein, cleaving said PEGylated fusion protein with IgA protease, and recovering lysine-PEGylated IGF-I or IGF-I variant. The invention relates also to a lysine-PEGylated IGF-I or IGF-I variant produced using the above method. In addition, the invention relates to a method for treating a neurodegenerative disorders like Alzheimer's Disease using the lysine-PEGylated IGF-I or IGF-I variant and a composition comprising the lysine-PEGylated IGF-I or IGF-I variant. | 2010-02-11 |
20100035818 | OPTIMIZED EXPRESSION OF HPV 52 L1 IN YEAST - Synthetic DNA molecules encoding the HPV 52 L1 protein are provided. Specifically, the present invention provides polynucleotides encoding HPV 52 L1 protein, wherein said polynucleotides are codon-optimized for high level expression in a yeast cell. In alternative embodiments of the invention, the nucleotide sequence of the synthetic molecule is altered to eliminate transcription termination signals that are recognized by yeast. The synthetic molecules may be used to produce HPV 52 virus-like particles (VLPs), and to produce vaccines and pharmaceutical compositions comprising the HPV 52 VLPs. The vaccines of the present invention provide effective immunoprophylaxis against papillomavirus infection through neutralizing antibody and cell-mediated immunity and may also be useful for treatment of existing HPV infections. | 2010-02-11 |
20100035819 | METHOD OF PROMOTING SKIN COLLAGEN PRODUCTION - It is intended to provide a skin collagen production promoter, foods and drinks for promoting skin collagen production and cosmetics for promoting skin collagen production which are useful in preventing skin chapping, wrinkles, worsening in skin fitness, etc. Namely, a skin collagen production promoter, foods and drinks for promoting skin collagen production and cosmetics for promoting skin collagen production which contain as the active ingredient(s) a milk-origin basic protein fraction and/or a basic peptide fraction obtained by digesting the above-described basic protein fraction with a protein digesting enzyme such as pepsin or pancreatin. The above basic protein fraction and basic peptide fraction have an effect of increasing skin collagen level. | 2010-02-11 |
20100035820 | AMIDATED DOPAMINE NEURON STIMULATING PEPTIDES FOR CNS DOPAMINERGIC UPREGULATION - The present invention relates to novel proteins, referred to herein as amidated glial cell line-derived neurotrophic factor (GDNF) peptides (or “Amidated Dopamine Neuron Stimulating peptides (ADNS peptides)”), that are useful for treating brain diseases and injuries that result in dopaminergic deficiencies. | 2010-02-11 |
20100035821 | Amide Linkage Cyclic Natriuretic Peptide Constructs - Cyclic constructs which bind to a natriuretic peptide receptor and include a plurality of amino acid residues, at least one amino acid surrogate of formula I: | 2010-02-11 |
20100035822 | PROLINE-RICH PEPTIDES, PHARMACEUTICAL COMPOSITION, USE OF ONE OR MORE PEPTIDES AND METHOD OF TREATMENT - The present invention provides oligopeptides with amino acid sequences comprised in set forth in SEQ ID NO 1 to 18, capable of binding to diverse targets, generating increase and sustenance to nitric oxide (NO) production in mammalian cells, potentiate the argininosuccinate synthase activity of animal cells and/or increase the intracellular bivalent calcium ion in animal cells. Also disclosed are pharmaceutical compositions of one or more peptides described in the present invention. The invention further relates to the use of these peptides. | 2010-02-11 |
20100035823 | LIGANDS OF SH3 DOMAINS - Provided are compounds that bind to SH3 domains. Also provided are combinatorial libraries for discovering such compounds. Methods of identifying a compound that binds to an SH3 domain are also provided. Methods of inhibiting an activity of a protein comprising an SH3 domain are additionally provided. Additionally provided are methods of inhibiting the activity of a protein comprising an SH3 domain and methods of treating a mammal having a deleterious condition that is mediated by a protein comprising an SH3 domain. The use of a compound that binds to the SH3 domain of a protein kinase in the manufacture of a medicament for the treatment of a deleterious condition in a mammal that is dependent on a protein kinase for induction or severity are also provided. | 2010-02-11 |
20100035824 | Synergistic Pharmaceutical Composition - The invention relates to pharmaceutical compositions containing an isoflavone or isoflavone glycoside or a pharmaceutically acceptable salt or solvate of said isoflavone or isoflavone glycoside as an active substance. Also disclosed are uses of such pharmaceutical compositions. | 2010-02-11 |
20100035825 | Treatment Of Disease By Inducing Cell Apoptosis - The present invention relates generally to the treatment and prevention of diseases characterized by excess cell proliferation and/or activation. In particular, the present invention provides compositions and methods to suppress the activation and/or proliferation of various cells. In some preferred embodiments, the present invention provides compositions and methods to suppress the activation and/or proliferation of mesenchymally derived cells (including, but not limited to hepatic stellate cells), as well as cells with abnormal growth characteristics. In some particularly preferred embodiments, the present invention provides compositions and methods to inhibit or eliminate fibrosis. In alternative preferred embodiments, the present invention provides compositions and methods to induce fibrosis. In still further embodiments, the present invention provides methods and compositions to treat and/or prevent cancer. | 2010-02-11 |
20100035827 | Multivalent metal salts of boronic acids - Salts of a pharmaceutically acceptable divalent metal and an organoboronic acid drug. Examples of such metals are calcium, magnesium and zinc. The organoboronic acid drug may be a boropeptide protease inhibitor. The salts may be formulated in oral dosage form. | 2010-02-11 |
20100035828 | MILK OLIGOSACCHARIDE FOR STIMULATING THE IMMUNE SYSTEM - The present invention relates to methods and nutritional compositions for stimulating the immune system, particularly in subjects with an impaired immune system such as 5 infants, said method comprising administering a composition comprising sheep milk and/or short chain oligosaccharides. | 2010-02-11 |
20100035829 | METHOD OF TREATING INTRAUTERINE INFLAMMATION - A method of treating intrauterine inflammation in a subject associated with intrauterine bacterial infection includes administering to the subject a therapeutically effective amount of a toll-like receptor 4 antagonist. The therapeutically effective amount administered to the subject is an amount effective in reducing intrauterine inflammation in the subject. | 2010-02-11 |
20100035830 | Iron-Carbohydrate Complex Compounds - The invention provides an iron-carbohydrate complex compound which is characterized by a content of iron(II). The invention also provides processes for the preparation of the iron-carbohydrate complex compound and the use thereof for treatment of iron deficiency anaemias. | 2010-02-11 |
20100035831 | ANTI-WRINKLE AGENT AND ADAM INHIBITOR - Disclosed is an anti-wrinkle agent for ameliorating a wrinkle (particularly a fine wrinkle) developed when the barrier function is decreased by dryness and the like. Also disclosed is an ADAM inhibitor. The anti-wrinkle agent or the ADAM inhibitor comprises an alkyl glucoside represented by the general formula: (1) [wherein R represents a linear or branched alkyl group having 1 to 18 carbon atoms] or a salt thereof. | 2010-02-11 |
20100035832 | Macrolides - This invention relates to a novel class of antibiotic agents, more specifically to macrolides comprising an oxazolidinone structure, their preparation, pharmaceutical compositions containing them, their use and methods of treatment using them. | 2010-02-11 |
20100035833 | ANTIBIOTIC MACROCYCLE COMPOUNDS AND METHODS OF MNAUFACTURE AND USE THEREOF - The invention encompasses an active metabolite of the 18-membered macrocyclic antimicrobial agents, specifically, a metabolite of tiacumicin B and in certain embodiments, R-Tiacumicin B or and its related compounds. In particular, the invention encompasses a compound that acts as a potent antibiotic agent for the treatment of bacterial infections, specifically GI infections caused by toxin producing strains of | 2010-02-11 |
20100035834 | NOVEL 1,4-BENZOTHIEPIN-1, 1-DIOXIDE DERIVATIVES WITH IMPROVED PROPERTIES METHOD FOR PRODUCING THE SAME, DRUGS CONTAINING SAID COMPOUNDS AND THE USE THEREOF - This invention relates to Novel 1,4-benzothiepin-1,1-dioxide derivatives with improved properties, method for producing the same, drugs containing said compounds and use thereof. | 2010-02-11 |
20100035835 | NUCLEOSIDE ARYL PHOSPHORAMIDATES FOR THE TREATMENT OF RNA-DEPENDENT RNA VIRAL INFECTION - The present invention provides nucleoside aryl phosphoramidates of structural formula (I) which are precursors to inhibitors of RNA-dependent RNA viral polymerase. These compounds are precursors to inhibitors of RNA-dependent RNA viral replication and are useful for the treatment of RNA-dependent RNA viral infection. They are particularly useful as precursors to inhibitors of hepatitis C virus (HCV) NS5B polymerase, as precursors to inhibitors of HCV replication, and/or for the treatment of hepatitis C infection. The invention also describes pharmaceutical compositions containing such nucleoside aryl phosphoramidates alone or in combination with other agents active against RNA-dependent RNA viral infection, in particular HCV infection. Also disclosed are methods of inhibiting RNA-dependent RNA polymerase, inhibiting RNA-dependent RNA viral replication, and/or treating RNA-dependent RNA viral infection with the nucleoside aryl phosphoramidates of the present invention. | 2010-02-11 |
20100035836 | BICYCLIC NUCLEOSIDES AND NUCLEOTIDES AS THERAPEUTIC AGENTS - The present disclosure relates to the use and methods of manufacture of bicyclic nucleosides and nucleotides for the treatment and prevention of infectious and proliferative diseases, including microbial infections and cancer. | 2010-02-11 |
20100035837 | THERAPEUTIC OR PROPHYLACTIC AGENT FOR VASOCONSTRICTION - An object of the present invention is to provide an agent for treating or preventing vasospasm. An object of the present invention is to provide an agent for treating or preventing cerebral vasospasm as well as arterial vasospasm. Further, an object of the present invention is to provide an agent for treating or preventing cerebral ischemia and cerebral infarction. | 2010-02-11 |
20100035838 | Cross-linked polysaccharide gels - The present invention relates to a process for preparing a cross-linked polysaccharide gel comprising contacting a polysaccharide with a cross-linking agent and a masking agent to form a cross-linked polysaccharide gel having resistance to degradation under physiological conditions. | 2010-02-11 |
20100035839 | MEROCYANINE DERIVATIVES - Disclosed are merocyanine derivatives which correspond to the formula (I), wherein L | 2010-02-11 |
20100035840 | PESTICIDAL COMPOSITION COMPRISING FOSETYL-ALUMINIUM, PROPAMOCARB-HCL AND AN INSECTICIDE SUBSTANCE - The present invention relates to a pesticide composition intended for protecting plants, crops or seeds against phyto-pathogenic fungi or damaging insects, and the corresponding methods of treatment using the said composition. More precisely, the subject of the present invention is a pesticide composition based on fosetyl-Al, propamocarb-HCl, an insecticide active substance and optionally a further fungicide active substance. | 2010-02-11 |
20100035841 | INHIBITORS OF TYROSINE KINASES AND USES THEREOF - Disclosed herein are compounds that inhibit the activity of particular tyrosine kinases. Methods for the preparation of such compounds are disclosed. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the compounds disclosed, alone or in combination with other therapeutic agents, for the treatment of tyrosine kinase-mediated diseases or conditions or tyrosine kinase-dependent diseases or conditions are provided. | 2010-02-11 |
20100035842 | Amino alcohol compounds or phosphonic acid derivatives thereof - A compound having a formula II(a): | 2010-02-11 |
20100035843 | METHODS FOR ATTENUATING ALLERGEN-INDUCED AIRWAY HYPERREACTIVITY USING CD1D DEPENDENT ANTAGONISTS - The present invention is directed to a method of inhibiting allergen-induced airway CD1d activation by administering a composition containing a moiety that blocks CD1d activation. Methods of the invention are useful for treatment and prevention of air-way hyperactivity caused by an allergen, and results in the attenuation of CD1d-restricted immune responses, including treatment of hay fever and asthma are due to air-way hyperactivity, and for systemic administration to attenuate ongoing immune responses. Preferably, these compositions are in a form intended for administration via nasal passages or directly inhaled to the air-ways. | 2010-02-11 |
20100035844 | PESTICIDE COMPOSITION COMPRISING PROPAMOCARB-FOSETYLATE AND AN INSECTICIDALLY ACTIVE SUBSTANCE - The present invention relates to a pesticide composition intended for protecting plants, crops or seeds against phyto-pathogenic fungi or damaging insects, and the corresponding methods of treatment using the said composition. More precisely, the subject of the present invention is a pesticide composition based on propamocarb-fosetylate, an insecticide active substance and optionally a further fungicide active substance. | 2010-02-11 |
20100035845 | TIGECYCLINE FORMULATIONS - The invention is directed to a frozen pharmaceutical formulation suitable for administration to a subject parenterally, comprising a therapeutically effective amount of tigecycline and an agent selected from the group consisting of lactose, dextrose, glucose, mannose, sucrose, ribose, xylose and a combination thereof, wherein the formulation in a pre-frozen state at about 22° C. or in an unfrozen state at about 22° C. has a pH in the range of from 4.0 to 5.5. Preferably, the formulation is suitable for storage at or below about −20° C. over a period of at least about 2 months, preferably 6 months, more preferably 26 months. Alternatively, the formulation is suitable for storage at about 22° C. over a period of about 24 hours. | 2010-02-11 |
20100035846 | METHOD FOR THE TREATMENT OF ACNE AND CERTAIN DOSAGE FORMS THEREOF - An oral dosage form, including 65 mg of minocycline, an amount of lactose monohydrate, and an amount of hydroxypropylmethylcellulose. The hydroxypropylmethylcellulose is hydroxypropylmethylcellulose that is about 8.9±0.2% hydroxypropoxylated. An oral dosage form, including 115 mg of minocycline, an amount of lactose monohydrate, and an amount of hydroxypropylmethylcellulose. The hydroxypropylmethylcellulose is hydroxypropylmethylcellulose that is about 8.9±0.2% hydroxypropoxylated. | 2010-02-11 |
20100035847 | GENES FOR BIOSYNTHESIS OF TETRACYCLINE COMPOUNDS AND USES THEREOF - The invention relates to genetically engineered cells, and to proteins and genes useful in the production of tetracycline compounds, to methods of producing tetracycline compounds, and to tetracyclines thereby produced. The present invention is based on the cloning and heterologous expression of genes encoding the chelocardin biosynthetic pathway. | 2010-02-11 |
20100035848 | THERAPY FOR DISORDERS OF THE PROXIMAL DIGESTIVE TRACT - A method for managing or treating an inflammatory, erosive, dyspeptic or reflux disorder of the proximal digestive tract of a subject comprises administering to the subject a therapeutically effective amount of an ACE2 inhibitor. A therapeutic combination, useful to treat any disease or condition in which an NSAID is indicated, comprises an NSAID in an anti-inflammatory, analgesic or antipyretic effective amount and a gastroprotective agent that comprises an ACE2 inhibitor in an amount effective to protect mucosal surfaces of the proximal digestive tract from erosion or ulceration induced by the NSAID. | 2010-02-11 |
20100035849 | NOVEL METHYLENEDIOXY PHENOLIC COMPOUNDS AND THEIR USE TO TREAT DISEASE - The present invention provides novel methylenedioxy phenolic compounds and their derivatives, methods of making them and methods of using them to treat or prevent cardiovascular disease, vascular disease and/or inflammatory disease, as well as Type I and Type II Diabetes and Dyslipidemia patients at risk for hypertension, stroke, cardiovascular and renal disease. | 2010-02-11 |
20100035850 | METHOD OF TREATMENT FOR INFLAMMATORY BOWEL DISEASE - The present invention provides methods of treating inflammatory bowel disease comprising administering to a subject in which remission has not been achieved after a first treatment of about 4-8 weeks of 5-ASA (mesalamine or 5-ASA), a further daily dose greater than about 4 g of 5-ASA in controlled release form to achieve a favorable response to treatment. | 2010-02-11 |
20100035851 | AGENT FOR IMPROVING INSULIN RESISTANCE - To inhibit production of adipocytokines, in particular, adipocytokines that elicit insulin resistance and to prevent onset of pathosis caused by the insulin resistance, or improve the pathosis, the present invention provides an agent or a food or drink which contains a compound having a cyclolanostane skeleton, or an organic solvent extract, a hot water extract of a plant of the family Liliaceae or Gramineae, or a fraction thereof which contains the compound as an active ingredient. | 2010-02-11 |
20100035852 | COMPOSITIONS AND METHODS FOR TREATING INFLAMMATORY CONDITIONS OF THE BOWEL - The present invention provides compositions and methods for treating inflammatory conditions (e.g., of the bowel). In particular, the present invention provides methods of treating (e.g., therapeutically and/or prophylactically treating) inflammatory conditions (e.g., of the bowel), compositions useful for such methods (e.g., antagonists and/or inhibitors of angiotensin II (AngII) receptor Type 1 | 2010-02-11 |
20100035853 | METHOD FOR PREVENTING OR TREATING CISPLATIN-INDUCED NEPHROTOXICITY - Provided is a method for preventing or treating cisplatin induced nephrotoxicity, which comprises administering a patient who is receiving cisplatin a therapeutically effective amount of an aldosterone blocker such as eplerenone or spironolactone. | 2010-02-11 |
20100035854 | DRY POWDER FORMULATIONS - A dry powder suitable for inhalation in a dry powder inhaler, the powder comprising a carrier, an active agent and at least 0.5% by weight of magnesium stearate, the powder being further characterized in that the less than 10% of the surface of the carrier material is covered with particles of magnesium stearate. The invention is also directed to a method of making dry powders by blending together the ingredients mentioned in a diffusion blender for a period time that is less than 60 minutes. | 2010-02-11 |
20100035855 | Method for treating or preventing a cardiovascular disease or condition utilizing estrogen receptor modulators based on APOE allelic profile of a mammalian subject - A method for treating cardiovascular disease in a mammalian subject includes providing to the subject at least one treatment regimen including at least one estrogen receptor modulator, wherein the at least one treatment regimen is determined based on the APOE allelic profile in the subject, and based on the steroid hormone levels prior to disease diagnosis and on current steroid hormone levels in the subject. | 2010-02-11 |
20100035856 | Beta-LACTAM-CONTAINING FORMULATIONS WITH INCREASED STABILITY IN AQUEOUS SOLUTION - The invention relates to novel formulations for dissolution in water which contain a β-lactam antibiotic and urea and whose pH after dissolution of the formulation in water is in the range of from 4.5 to 8. The formulations are suitable in particular for the treatment of bacterial diseases in animals. | 2010-02-11 |
20100035857 | ANTI-HYPERCHOLESTEROLEMIC COMPOUNDS - This invention provides cholesterol absorption inhibitors of Formula I:I and the pharmaceutically acceptable salts thereof. The compounds are useful for lowering plasma cholesterol levels, particularly LDL cholesterol, and for treating and preventing atherosclerosis and atherosclerotic disease events. | 2010-02-11 |
20100035858 | Novel Compositions and Methods for Binding and Inhibiting 5-HT4 Receptor - The present invention relates to compositions that bind to 5-HT4 receptors and inhibit proliferation of activated lymphocytes. The invention also provides methods for inhibiting proliferation and inducing cell death in activated immune cells, as well methods for treating diseases associated with activated immune cells by administering 5-HT4 receptor ligands. | 2010-02-11 |
20100035859 | TREATMENT OF PROTEIN AGGREGATION DISEASES - A method of treatment for the prevention or therapy of a protein aggregation disease includes the administration in combination of a first active medicament and a second active medicament, wherein the first active medicament is active to impede aggregation of amyloid protein and the second active medicament is active to disaggregate previously formed aggregates of amyloid protein. | 2010-02-11 |
20100035860 | INHIBITORS OF PROTEIN TYROSINE PHOSPHATASE FOR THE PROMOTION OF PHYSIOLOGICAL CARDIAC HYPERTROPHY - The invention relates to the use of protein tyrosine phosphatase inhibitors for the promotion of physiological cardiac hypertrophy and the treatment of pathological cardiac hypertrophy. | 2010-02-11 |
20100035861 | Meptazinol Biligand Derivatives and/or their Salts, Preparation Method and Uses Thereof - The present invention belongs to pharmaceutical field. It relates to a novel family of bivalent (−)-meptazinol compounds and/or their salts, as well as the preparation and utilization of the compounds in the treatment of neurodegenerative disorders and dementias such as Alzheimer's Disease (AD). In the present invention, bivalent (−)-meptazinol compounds were synthesized, from the starting material (−)-meptazinol, successively by N-demethylation forming (−)-nor-meptazinol and then by acylation with α,ω-alkanediacyl dihalides or alkylation with α,ω-dihaloalkanes. Results from in vitro cholinesterase inhibiting test and AChE-induced Aβ aggregation test demonstrated that the bivalent (−)-meptazinol compounds and/or their salts were novel bivalent inhibitors of both ACHE and Aβ aggregation. The most potent compound inhibited both ACHE and BCHE at nM level, which was 10000 and 1500 times more potent than (−)-MEP hydrochloride, respectively. It inhibited ACHE-induced Aβ aggregation by a factor of 2 compared with propidium. | 2010-02-11 |
20100035862 | NOVEL AZA-CYCLIC INDOLE-2-CARBOXAMIDES AND METHODS OF USE THEREOF - The invention relates to aza-cyclic-indole-2-carboxamide derivatives, compositions comprising such compounds, and methods of preventing or treating conditions and disorders using such compounds and compositions. | 2010-02-11 |
20100035863 | 2 Amino-Pyrimidine Derivatives As H4 Receptor Antagonists, Processes For Preparing Them And Their Use In Pharmaceutical Compositions - The present invention concerns novel 2 amino pyrimidine derivatives of formula (I), processes for preparing them, pharmaceutical compositions containing them and their use as harmaceuticals. | 2010-02-11 |
20100035864 | Diacylglycerol Acyltransferase Inhibitors - Provided herein are compounds of the formula (1): | 2010-02-11 |
20100035865 | Sulfonamides and Pharmaceutical Compositions Thereof - The invention is directed to a class of compounds, including the pharmaceutically acceptable salts of the compounds, having the structure of formula (I), as defined in the specification. The invention is also directed to compositions containing the compounds of formula (I). | 2010-02-11 |
20100035866 | NOVEL SUBSTITUTED-1, 1-DIOXO-BENZO[1,2,4]THIADIAZIN-3ONES, PREPARATION METHOD THEREOF, AND PHARMACEUTICAL COMPOSITION CONTAINING THE SAME - The present invention relates to compounds of substituted-1,1-dioxo-benzo[1,2,4]thiadiazin-3-ones acting as a 5HT6 receptor antagonist, a preparation method thereof, and a pharmaceutical composition containing the same for treatment of the central nervous system disorders. The compounds of substituted-1,1-dioxo-benzo[1,2,4]thiadiazin-3-ones according to the present invention have excellent binding affinity for the 5HT6 receptor and excellent selectivity for the 5HT6 receptor over other receptors. Also, the compounds reverse a disruption of PPI by apomorphine and don't show rotatod deficit in mice. Therefore the compounds according to the present invention may be valuably used for treatment of a 5HT6 receptor relating disorders. | 2010-02-11 |
20100035867 | Inhibitors of Cyclic Nucleotide Synthesis and Their Use for Therapy of Various Diseases - We disclose a method of inhibiting activity of adenylyl cyclase or guanylyl cyclase in a mammal by administering to the mammal an amount of a composition effective to inhibit the activity, wherein the composition contains at least one compound selected from the group consisting of structural formulae (Ia) and (Ib) and salts thereof, wherein R1 is —H or has the structure —C(═O)R8; R2 is ═O or has the structure —OC(═O)R9; and R3, R4, R5, R6, and R7 are each independently selected from the group consisting of —H, —NO | 2010-02-11 |
20100035868 | METHODS OF TREATMENT OF UTERINE PATHOLOGICAL CONDITIONS - A method of treating or preventing a pathological condition of the uterus in an individual the method comprising administering to the individual any one or more of an inhibitor of cyclooxygenase-2 (COX-2), an inhibitor of prostaglandin E synthase (PGES), or an EP2 or EP4 receptor antagonist. Typically, the pathological condition is uterine cancer, fibroids or endometriosis. | 2010-02-11 |
20100035869 | TARGETED NITROXIDE AGENTS - Provided herein are compositions and related methods useful for free radical scavenging, with particular selectivity for mitochondria. The compounds comprise a nitroxide-containing group attached to a mitochondria-targeting group. The compounds can be cross-linked into dimers without loss of activity. Also provided herein are methods, for preventing, mitigating and treating damage caused by radiation. The method comprises delivering a compound, as described herein, to a patient in an amount and dosage regimen effective to prevent, mitigate or treat damage caused by radiation. | 2010-02-11 |
20100035870 | Pyrimidin-4-yl-3, 4-Dihydro-2H-Pyrrolo[1,2A] Pyrazin-1-one Compounds - The present invention relates to compounds of formula (I), or pharmaceutically acceptable salts thereof, wherein Z is NR | 2010-02-11 |
20100035871 | BENZOXAZINE DERIVATIVES AND USES THEREOF - Compounds of formula (I) or pharmaceutically acceptable salts thereof are provided, wherein each of Z, X, R | 2010-02-11 |
20100035872 | PDE10 INHIBITORS AND RELATED COMPOSITIONS AND METHODS - Compounds that inhibit PDE10 are disclosed that have utility in the treatment of a variety of conditions, including (but not limited to) psychotic, anxiety, movement disorders and/or neurological disorders such as Parkinson's disease, Huntington's disease, Alzheimer's disease, encephalitis, phobias, epilepsy, aphasia, Bell's palsy, cerebral palsy, sleep disorders, pain, Tourette's syndrome, schizophrenia, delusional disorders, drug-induced psychosis and panic and obsessive-compulsive disorders. Pharmaceutically acceptable salts, stereoisomers, solvates and prodrugs of the compounds are also provided. Also disclosed are compositions containing a compound in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for inhibiting PDE10 in a warm-blooded animal in need of the same. | 2010-02-11 |
20100035873 | Diaryl Compounds and Uses Thereof - The invention relates to derivatives of a compound of formula I: | 2010-02-11 |
20100035874 | Organic compounds - There are described pyrazolo[5.1-b]oxazole derivatives useful as corticotropin releasing factor (CRF | 2010-02-11 |
20100035875 | TRIAZOLOPYRIDINE JAK INHIBITOR COMPOUNDS AND METHODS - A compound of Formula I, enantiomers, diasteriomers, tautomers or pharmaceutically acceptable salts thereof, wherein R | 2010-02-11 |
20100035876 | Use of a Kinase Inhibitor for the Treatment of Particular Resistant Tumors - The invention provides low molecular weight compounds, namely tetrahydropyrrolo[3,4-c]pyrazoles, showing a high affinity for the ATP pocket of ABL tyrosine kinase. These compounds are thus ATP-competitive tyrosine kinase inhibitors displaying a significant inhibitory potency also, and in particular, towards BCR-ABL inhibitor-resistant T315I ABL mutants. The compounds of the invention find a useful application in the treatment of BCR-ABL inhibitor-resistant ABL-mediated diseases, such as Imatinib-resistant chronic myelogenous leukemia. Moreover, the invention provides a screening method for the identification of compounds capable of binding the ATP pocket of a kinase protein, in particular of the T315I mutant ABL kinase. | 2010-02-11 |
20100035877 | METHODS AND COMPOSITIONS FOR TREATING PATHOLOGIES ASSOCIATED WITH BDNF SIGNALING - A method of treating ncm-neurødegenerative pathologies associated with derangement in brain-derived neurotrophic factor signaling in the brain stem includes administering to the subject an amount of at least one arnpakine effective to increase brain-derived neurotrophic factor nodose sensory neurons of the subject. | 2010-02-11 |
20100035878 | INHIBITORS OF C-JUN N-TERMINAL KINASES FOR THE TREATMENT OF NEURODEGENERATIVE DISORDERS RELATING TO APOPTOSIS AND/OR INFLAMMATION - The present invention provides novel compounds of formula I and their use in the inhibition of c-Jun N-terminal kinases. The present invention further provides the use of these compounds in medicine, in particular in the prevention and/or treatment of neurodegenerative disorders related to apoptosis and/or inflammation. | 2010-02-11 |
20100035879 | N-SULFONYLCARBOXIMIDAMIDE APOPTOSIS PROMOTERS - Compounds having the formula | 2010-02-11 |
20100035880 | SUBSTITUTED SULFONYLAMINOARYLMETHYL CYCLOPROPANECARBOXAMIDE AS VR1 RECEPTOR ANTAGONISTS - This invention provides a compound of the formula (I): | 2010-02-11 |
20100035881 | WRINKLE-IMPROVING AGENT - The invention provides a novel wrinkle-improving agent that has an effect of improving wrinkles, that does not entail problems of safety or pain even when applied to the skin, and that contains a very safe substance as an active component. A discovery was made that N-benzoyl-β-alanine, other specific β-alanine derivatives, and salts thereof have a wrinkle-improving effect, whereby a wrinkle-improving agent containing as an active component one, two, or more types of compounds selected from the group composed of these specific β-alanine derivatives and the salts thereof was developed. | 2010-02-11 |
20100035882 | INHIBITION OF PDE2A - The invention relates to the use of PDE2A inhibitors for the manufacture of a medicament for the treatment and/or prophylaxis of coronary diseases, especially stable and unstable angina pectoris, acute myocardial infarction, prophylaxis of myocardial infarction, heart failure, and high blood pressure and the sequelae of atherosclerosis, and vascular disorders, disorders of the kidney, especially renal failure, inflammatory disorders, erectile dysfunction and prevention of sudden heart death. | 2010-02-11 |
20100035883 | DIHYDROPYRIDOPHTHALAZINONE INHIBITORS OF POLY(ADP-RIBOSE)POLYMERASE (PARP) - A compound having the structure set forth in Formula (I) and Formula (II): | 2010-02-11 |
20100035884 | KINASE INHIBITOR - The invention is directed to a compound of formula (I): | 2010-02-11 |
20100035885 | COMPOSITIONS FOR MANIPULATING THE LIFESPAN AND STRESS RESPONSE OF CELLS AND ORGANISMS - Provided herein are methods and compositions for modulating the activity of sirtuin deacetylase protein family members; p53 activity; apoptosis; lifespan and sensitivity to stress of cells and organisms. Exemplary methods comprise contacting a cell with an activating compound, such as a flavone, stilbene, flavanone, isoflavone, catechin, chalcone, tannin or anthocyanidin; or an inhibitory compound, such as a sphingolipid, e.g., sphingosine. | 2010-02-11 |
20100035886 | PARENTERAL FORMULATIONS OF DOPAMINE AGONISTS - This invention relates to stable pharmaceutical compositions for parenteral administration comprising dopamine agonists and peripheral acting agents useful for treatment of metabolic disorders or key elements thereof. The parenteral dosage forms exhibit long stable shelf life and distinct pharmacokinetics. | 2010-02-11 |
20100035887 | THERAPEUTIC COMPOUNDS FOR BLOCKING DNA SYNTHESIS OF POX VIRUSES - This invention provides methods of inhibiting replication of a poxvirus by contacting a poxvirus with a compound having formula I, formula XXI, formula XXXII, or formula XLI which in turn reduce, inhibit, or abrogate poxvirus DNA polymerase activity and/or its interaction with its processivity factor. Formula I, formula XXI, formula XXXII, or formula XLI can be utilized to treat humans and animals suffering from a poxvirus infection. Pharmaceutical compositions for treating poxvirus infected subjects are also provided. | 2010-02-11 |
20100035888 | Diaryl Urea for Treating Pulmonary Hypertension - The present invention relates to pharmaceutical compositions for treating, preventing or managing pulmonary hypertension comprising 4{4-[3-(4-chloro-3-trifluoromethylphenyl)-ureido]-3-fluorophenoxy}-pyridine-2-carboxylic acid methylamide optionally combined with at least one additional therapeutic agent. | 2010-02-11 |
20100035889 | Use of PDE III Inhibitors For The Treatment of Asymptomatic (Occult) Heart Failure - The invention relates to the use of a phosphodiesterase type III (PDE III) inhibitor or Ca | 2010-02-11 |
20100035890 | USE OF RANOLAZINE FOR THE TREATMENT OF CARDIOVASCULAR DISEASES - Disclosed are methods for treating patients suffering from cardiovascular diseases comprising administering an intravenous (IV) infusion of ranolazine. In one embodiment, the IV infusion of ranolazine is followed by an orally administered sustained release ranolazine dosage formulation to maintain human ranolazine plasma levels at therapeutic levels in patients. | 2010-02-11 |
20100035891 | Pharmaceutically Active Compounds - Compounds of the formula (I): | 2010-02-11 |
20100035892 | METHOD FOR ASSEMBLING HIGH-PURITY CHEMICAL LIBRARIES, COMPOUNDS SUPPRESSING ACETYL COENZYME A CARBOXYLASE ACTIVITIES DISCOVERED BY SAME - The present disclosure provides novel compounds of the formula (I): | 2010-02-11 |
20100035893 | TRIAZOLOPYRIDINE CARBOXAMIDE DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF - The invention relates to the triazolopyridine carboxamide derivatives of general formula (I): | 2010-02-11 |
20100035894 | Aqueous liquid preparation having improved intraocular gatifloxacin penetration - An object is to provide an ophthalmic aqueous preparation excellent in the retention of gatifloxacin in a tear fluid and the preparation of gatifloxacin into an aqueous humor and a conjunctiva. Another object is to prevent the formation of any precipitate and the reduction in viscosity in the aqueous liquid preparation. An aqueous liquid preparation comprising gatifloxacin, a pharmacologically acceptable salt thereof or a hydrate of gatifloxacin or the salt and at least 0.15 w/v % of xanthan gum enables to improve the retention and penetration of gatifloxacin. When at least 0.2 w/v % of sodium chloride is added to the aqueous liquid preparation, the formation of any precipitate and the reduction in viscosity in the aqueous liquid preparation can be prevented. | 2010-02-11 |
20100035895 | 2-AMINOCARBONYL-PYRIDINE DERIVATIVES - The present invention relates to 2-aminocarbonyl-pyridine derivatives of Formula (I) and their use as P2Y | 2010-02-11 |
20100035896 | Combination of N-(3-methoxy-5-methylpyrazin-2-yl)-2-(4-[1,3,4-oxadiazol-2-yl]phenyl)pyri- dine-3-sulphonamide and an anti-mitotic cytotoxic agent - A combination, comprising N-(3-methoxy-5-methylpyrazin-2-yl)-2-(4-[1,3,4-oxadiazol-2-yl]phenyl)pyridine-3-sulphonamide and an anti-mitotic cytotoxic agent. | 2010-02-11 |
20100035897 | Pyridine, pyrimidine and pyrazine derivatives as gpcr agonists - Compounds of formula (I): R | 2010-02-11 |
20100035898 | Organic compounds - There are described cyclohexyl amide derivatives useful as corticotropin releasing factor (CRF | 2010-02-11 |
20100035899 | 5,7-DISUBSTITUTED[1.3]THIAZOLO[4,5-d]PYRIMIDIN-2(3H)-AMINE DERIVATIVES AND THEIR USE IN THERAPY - There are disclosed novel 5-substituted 7-amino-[1,3]thiazolo[4,5-d]pyrimidine derivatives of formula (I) wherein R | 2010-02-11 |
20100035900 | 6-Arylmethyl-substituted pyrazolopyrimidines - The invention relates to novel 6-arylmethyl-substituted pyrazolopyrimidines, process for their preparation and their use for producing medicaments for improving perception, concentration, learning and/or memory. | 2010-02-11 |
20100035901 | ADENINE DERIVATIVE AS INHIBITORS OF HSP90 FOR THE TREATMENT OF CANCER - The invention provides a compound which is (a) an amino acid derivative of formula (I) or a tautomer thereof, or (b) a pharmaceutically acceptable salt, N-oxide, hydrate or solvate thereof: wherein R | 2010-02-11 |
20100035902 | 5-ARYL-SUBSTITUTED DIHYDROPYRIDOPYRIMIDINES AND DIHYDROPYRIDAZINES AND USE THEREOF AS MINERAL CORTICOID ANTAGONISTS - The present application relates to novel aryl-substituted heterobicyclic compounds, a process for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for the manufacture of medicaments for the treatment and/or prophylaxis of diseases, especially cardiovascular disorders. | 2010-02-11 |
20100035903 | PYRROLO[2,3-D]PYRIMIDINE COMPOUNDS - A compound of the formula | 2010-02-11 |
20100035904 | PHENOBARBITAL SALTS; METHODS OF MAKING; AND METHODS OF USE THEREOF - Disclosed are new phenobarbital salts, methods of preparation, and uses thereof. | 2010-02-11 |
20100035905 | Hydrates of 2-chloro-5-[3,6-dihydro-3-methyl-2,6-dioxo-4-(trifluoromethyl)-1-(2H)-pyr- imidinyl]-4-fluoro-N-[[methyl(1-methylethyl)amino]sulfonyl]benzamide - The present invention relates to hydrates of 2-chloro-5-[3,6-dihydro-3-methyl-2,6-dioxo-4-(trifluoromethyl)-1-(2H)pyrimidinyl]-4-fluoro-N-[[methyl(1-methylethyl)amino]-sulfonyl]benzamide. The invention also relates to a process for the preparation of these hydrates and to plant protection formulations which comprise hydrates of the phenyluracil I. | 2010-02-11 |
20100035906 | Dipyridyl-dihydropyrazolones and their use - The present application relates to novel dipyridyl-dihydropyrazolones, processes for their preparation, their use for treatment and/or prophylaxis of diseases and their use for the preparation of medicaments for treatment and/or prophylaxis of diseases, in particular cardiovascular and hematological diseases and kidney diseases, and for promoting wound healing. | 2010-02-11 |
20100035907 | NEW 2,4-DIANILINOPYRIMIDINES, PREPARATION THEREOF AS DRUGS, PHARMACEUTICAL COMPOSITIONS AND USE THEREOF ESSENTIALLY AS IKK INHIBITORS - The disclosure relates to a compound of formula (I): | 2010-02-11 |
20100035908 | SUBSTITUTED ACETOPHENONES USEFUL AS PDE4 INHIBITORS - The present invention relates to a compound according to formula: (I); wherein X | 2010-02-11 |
20100035909 | NOVEL SUBSTITUTED DIAZA-SPIRO-PYRIDINONE DERIVATIVES FOR USE IN MCH-1 MEDIATED DISEASES - The present invention concerns aryl and heteroaryl substituted diaza-spiro-pyridinone derivatives having antagonistic melanin-concentrating hormone (MCH) activity, in particular MCH-1 activity according to the general Formula (I) | 2010-02-11 |
20100035910 | Process for the Preparation of Quaternary N-Alkyl Morphinan Alkaloid Salts - An improved process for the N-alkylation of tertiary morphinan alkaloid bases to form the corresponding quaternary morphinan alkaloid derivatives. | 2010-02-11 |