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19th week of 2009 patent applcation highlights part 47
Patent application numberTitlePublished
20090118199SUBSTITUTED ACRYLAMIDE DERIVATIVE AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME - A pharmaceutical composition comprising a compound having Formula (I) or a pharmacologically acceptable salt thereof as an active ingredient:2009-05-07
20090118200Proline bis-amide orexin receptor antagonists - The present invention is directed to proline bis-amide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved.2009-05-07
20090118201BENZYLBENZENE DERIVATIVES AND METHODS OF USE - Provided are compounds having an inhibitory effect on sodium-dependent glucose cotransporter SGLT. The invention also provides pharmaceutical compositions, methods of preparing the compounds, synthetic intermediates, and methods of using the compounds, independently or in combination with other therapeutic agents, for treating diseases and conditions which are affected by SGLT inhibition.2009-05-07
20090118202COMPOSITIONS AND METHODS OF TREATING HYPERTENSION WITH TANNIN COMPLEXES - The present invention includes methods and compositions to ameliorate one or more symptom of hypertension through the inhibitor of an AT1 receptor by transcriptional down regulation of an angiotensin II type 1 receptor. The composition includes an effective amount of one or more tannic acids disposed in a pharmaceutically acceptable carrier.2009-05-07
20090118203Administration of agents inducing dopachrome tautomerase (TRP-2) expression for protecting hair follicle melanocytes - Agents inducing the expression of DOPAchrome tautomerase are administered, notably topically applied, to protect and/or regenerate the melanocytes of hair follicles, to promote the cyclic renewal of the follicular pigmentation unit, to prevent and/or limit and/or arrest the development of canities, and to maintain the natural pigmentation of gray or white head hair and/or body hair.2009-05-07
20090118204Methods and Compositions Related to Esculentoside A - Disclosed are compositions related to water soluble selective COX-2 inhibitors and methods of using the inhibitors (including Esculentoside A and derivatives thereof).2009-05-07
20090118205Antisense Oligonucleotides Directed to Ribonucleotide Reductase R2 and uses Thereof in the Treatment of Cancer - The present invention provides antisense oligonucleotides directed to a mammalian ribonucleotide reductase R2 gene and combinations of the antisense oligonucleotides with one or more chemotherapeutic agents for use in the treatment of cancer. 2009-05-07
20090118206RNA INTERFERENCE FOR THE TREATMENT OF GAIN-OF-FUNCTION DISORDERS - The present invention relates to the discovery of an effective treatment for a variety of gain-of-function diseases, in particular, Huntington's disease (HD). The present invention utilizes RNA Interference technology (RNAi) against polymorphic regions in the genes encoding various gain-of-function mutant proteins resulting in an effective treatment for the gain-of-function disease.2009-05-07
20090118207Use of apoptosis-specific eIF-5A siRNA to down regulate expression of proinflammatory cytokines to treat sepsis - The present invention relates to apoptosis specific eucaryotic initiation factor 5A (eIF-5A), referred to as apoptosis-specific eIF-5A or eIF5-A1, nucleic acids and polypeptides and methods for down regulating pro-inflammatory cytokines in a mammal by administering siRNA against eIF-5A1 to the mammal to treat/prevent sepsis and/or hemorrhagic shock.2009-05-07
20090118208Composition and methods of RNAI therapeutics for treatment of cancer and other neovascularization diseases - Compositions and methods are provided for treatment of diseases involving unwanted neovascularization (NV). The invention provides treatments that control NV through selective inhibition of pro-angiogenic biochemical pathways, including inhibition of the VEGF pathway gene expression and inhibition localized at pathological NV tissues. Tissue targeted nanoparticle compositions comprising polymer conjugates and nucleic acid molecules that induce RNA interference (RNAi) are provided. The nanoparticle compositions of the invention can be used alone or in combination with other therapeutic agents such as VEGF pathway antagonists. The compositions and methods can be used for the treatment of NV diseases such as cancer, ocular disease, arthritis, and inflammatory diseases.2009-05-07
20090118209Use of the slug gene as a genetic marker in functions mediated by SCF (stem cell factor) and applications - The Slug gene mediates the functions of SCF linking and its c-kit receptor which means that the Slug gene, the Slug gene's cDNA, Slug protein and/or drugs or substances that activate the expression of the Slug gene can be used as therapeutic agents in the mobilization of hematopoyetic stem cells for transplants or gene therapy, in the ex vivo expansion of hematopoyetic stem cells and/or in the treatment of masculine sterility problems.2009-05-07
20090118210Epididymal lipocalin gene and uses thereof - Isolated nucleic acids comprising a lipocalin gene promoter region, isolated nucleic acids comprising a human lipocalin gene, isolated nucleic acids encoding a lipocalin polypeptide, isolated lipocalin polypeptides, and uses thereof. The disclosed lipocalin nucleic acids and polypeptides can be used to generate a mouse model of male infertility, for drug discovery screens, and for therapeutic treatment of fertility-related conditions.2009-05-07
20090118212METHODS FOR PRODUCING AND USING IN VIVO PSEUDOTYPED RETROVIRUSES - The present invention provides novel pseudotyped retroviral vectors that can transduce human and other cells. Vectors are provided that are packaged efficiently in packaging cells and cell lines to generate high titer recombinant virus stocks expressing novel envelope glycoproteins. The present invention further relates to compositions for gene therapy.2009-05-07
20090118213RNA ANTAGONIST COMPOUNDS FOR THE INHIBITION OF APO-B100 EXPRESSION - Oligonucleotides directed against the Apo-B100 gene are provided for modulating the expression of Apo-B100. The compositions comprise oligonucleotides, particularly antisense oligonucleotides, targeted to nucleic acids encoding the Apo-B100. Methods of using these compounds for modulation of Apo-B100 expression and for the treatment of diseases associated with either overexpression of Apo-B100, expression of mutated Apo-B100 or both are provided. Examples of diseases are cancer such as lung, breast, colon, prostate, pancreas, lung, liver, thyroid, kidney, brain, testes, stomach, intestine, bowel, spinal cord, sinuses, bladder, urinary tract or ovaries cancers. The oligonucleotides may be composed of deoxyribonucleosides or a nucleic acid analogue such as for example locked nucleic acid or a combination thereof.2009-05-07
20090118214Compositions for conferring tolerance to viral disease in social insects, and the use thereof - Compositions and methods for reducing susceptibility to infectious disease in bees using RNA interference technology, and more particularly, prevention and treatment of viral infections in honeybees such as Israel acute paralysis virus (IAPV) by feeding of pathogen-specific dsRNA. Further, multiple-pathogen specific dsRNA is disclosed.2009-05-07
20090118215Bioresorbable Controlled-Release Composition - A novel method for the preparation of a highly densified and at least partly, preferably fully or almost fully hydrated ceramic for use in the preparation of a pharmaceutical composition notably for controlled-release of one or more therapeutically, prophylactically and/or diagnostically active substance. The method involves a concomitant step of hydrating and densifying a bioresorbable and hydratable ceramic such as calcium sulphate. The invention also relates to compositions comprising such a highly densified ceramic. The pharmaceutical composition is useful for targeted and controlled local prolonged release of active substances, e.g. anti-cancer agents, whereby the spectrum and severity of side effects are minimized due to an optimized local concentration-time profile.2009-05-07
20090118216ANAPLASTIC LYMPHOMA KINASE (ALK) AS ONCOANTIGEN FOR LYMPHOMA VACCINATION - Use of intracytoplasmatic domain of Anaplastic Lymphoma Kinase (ALK) protein and/or a nucleic acid molecule encoding for the intracytoplasmatic domain of Anaplastic Lymphoma Kinase (ALK) protein, of any species, for the preparation of a medicament, preferably a vaccine, for the treatment and/or prevention of a tumor in a subject, preferably a lymphoma.2009-05-07
20090118217Genetic polymorphisms associated with myocardial infarction, methods of detection and uses thereof - The present invention is based on the discovery of genetic polymorphisms that are associated with myocardial infarction. In particular, the present invention relates to nucleic acid molecules containing the polymorphisms, variant proteins encoded by such nucleic acid molecules, reagents for detecting the polymorphic nucleic acid molecules and proteins, and methods of using the nucleic acid and proteins as well as methods of using reagents for their detection.2009-05-07
20090118218Biocompatible Hydrogels - A biocompatible macromer composition is provided which includes a first polymer possessing a first nucleoside, and a second polymer possessing a second nucleoside that is complementary to the first nucleoside and capable of undergoing base pairing with the first nucleoside. The biocompatible macromer composition can be used as an adhesive or sealant in human and/or animal medical applications.2009-05-07
20090118219FLEA GABA RECEPTOR SUBUNIT NUCLEIC ACID MOLECULES - The present invention relates to flea GABA receptor subunit nucleic acid molecules; to flea GABA receptor subunit proteins encoded by such nucleic acid molecules; to antibodies raised against such proteins; and to compounds that inhibit the activity of such proteins. The present invention also includes methods to obtain such proteins, nucleic acid molecules, antibodies, and inhibitory compounds. The present invention also includes therapeutic compositions comprising such proteins, nucleic acid molecules, antibodies and inhibitory compounds, particularly those that specifically inhibit flea GABA receptor subunit activity, as well as the use of such therapeutic compositions to treat animals.2009-05-07
20090118220SUBSTITUTED ADENINES AND THE USES THEREOF - This invention relates to compounds of Formula I:2009-05-07
20090118221METHOD OF TREATING ARRHYTHMIAS - Methods are provided for treating arrhythmia in a manner that minimizes undesirable side effects, comprising administration of a therapeutically effective minimal dose of an A2009-05-07
20090118222NOVEL PYRIMIDINE NUCLEOSIDE COMPOUND OR ITS SALT - A novel pyrimidine nucleoside compound represented by the following formula (1):2009-05-07
20090118223Novel 2'-c-methyl and 4'c-methyl nucleoside derivatives - Novel 2′-C-methyl nucleoside 5′-monophosphate and 4′-C-methyl nucleoside 5′-monophosphate derivatives, stereoisomers, and pharmaceutically acceptable salts or prodrugs thereof, their preparation, and their uses for the treatment of hepatitis C viral infection are described.2009-05-07
20090118224AGENT AGAINST PSYCHOSOCIAL STRESSES - To provide a novel anti-psychosocial stress agent which is highly safety and can be continuously taken, more particularly, a novel anti-psychosocial stress agent which prevents or alleviates psychosocial stress.2009-05-07
200901182251-Methyl Nicotinamide and Derivatives for Treatment of Gastric Injury - The present invention is directed to nicotinamide derivatives, and their use in treating gastrointestinal disorders.2009-05-07
20090118226INTESTINAL EOSINOPHIL-SUPPRESSING COMPOSITION - To promote the growth of human beings or animals, prevent the onset of diarrhea and prevent or ameliorate various diseases, it is intended to provide a substance which has an effect of decreasing eosinophils in the intestinal tract and a feed comprising the same as a feed additive. Namely, an intestinal eosinophil-suppressing composition which contains an ▪-linked galactooligosaccharide as the active ingredient. When added in an amount of from 0.01 to 10% by weight, in terms of the saccharide, to an animal feed, this composition is useful in providing an intestinal eosinophil-suppressing feed.2009-05-07
20090118227CAROTENOID-CONTAINING COMPOSITIONS AND METHODS - The present invention is directed to carotenoid compositions and methods for inhibiting the growth of pathogenic bacteria or for preventing or treating bacterial infections in subjects by administration of an effective amount of astaxanthin and beta-carotene.2009-05-07
20090118228CAROTENOID-CONTAINING COMPOSITIONS AND METHODS - The present invention is directed to methods for improving optical or skin health in a subject comprising administering to the subject a combination of lutein, zeaxanthin, lycopene, and beta-carotene.2009-05-07
20090118229CAROTENOID-CONTAINING COMPOSITIONS AND METHODS - The present invention is directed to carotenoid-containing compositions and methods for improving bone or respiratory health in a subject comprising administering to the subject a combination of lycopene, beta-carotene, and beta-cryptoxanthin.2009-05-07
20090118230FUCOSE CONTAINING PROTEOGLYCAN OR ACIDIC GLYCAN AND THEIR PHARMACEUTICAL USE - A class of proteoglycans containing fucosylated acidic glycans, e.g., as produced by marine sponges and sea urchin embryos, have been found to stimulate selective proliferation of mammalian natural killer (NK) cells and γδT cells. These compounds are useful as pharmaceuticals, particularly as immunostimulants, e.g., in the treatment of cancer and viral infections.2009-05-07
20090118231Pectin-modified resistant starch, a composition containing the same and method for preparing resistant starch - This invention relates to a pectin-modified resistant starch prepared by cross-linking starch with pectin by pectinesterase reaction. Such resistant starch is low amylase digestible and thus is useful in food products, including nutritional supplements, to reduce calorie content and increase fiber content. This invention also relates to a composition containing the resistant starch and a process for the preparation of the same.2009-05-07
20090118232INDOLES, 1H-INDAZOLES, 1,2-BENZISOXAZOLES, 1,2-BENZOISOTHIAZOLES, AND PREPARATION AND USES THEREOF - The present invention relates generally to the field of ligands for nicotinic acetylcholine receptors (nACh receptors), activation of nACh receptors, and the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain. Further, this invention relates to novel compounds (indazoles and benzothiazoles), which act as ligands for the α7 nACh receptor subtype, methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.2009-05-07
20090118233Heterocyclic compounds having inhibitory activity against HIV integrase - A heterocyclic compound of the formula (I):2009-05-07
20090118234Novel phosphonic acid compounds as inhibitors of serine proteases - The present invention is directed to phosphonic acid compounds useful as serine protease inhibitors, compositions thereof and methods for treating inflammatory and serine protease mediated disorders.2009-05-07
20090118235Novel phosphonic acid compounds as inhibitors of serine proteases - The present invention is directed to phosphonic acid compounds useful as serine protease inhibitors, compositions thereof and methods for treating inflammatory and serine protease mediated disorders.2009-05-07
20090118236Novel Phosphorus-Containing Thyromimetics - The present invention relates to compounds of phosphonic acid containing T3 mimetics, stereoisomers, pharmaceutically acceptable salts, co-crystals, and prodrugs thereof and pharmaceutically acceptable salts and co-crystals of the prodrugs, as well as their preparation and uses for preventing and/or treating metabolic diseases such as obesity, NASH, hypercholesterolemia and hyperlipidemia, as well as associated conditions such as atherosclerosis, coronary heart disease, impaired glucose tolerance, metabolic syndromex and diabetes.2009-05-07
20090118237Carisoprodol, Phenytoin and Fosphenytoin Articles and Methods - A method of using carisoprodol, phenytoin or fosphenytoin comprises informing a user that co-administration of carisoprodol with phenytoin or fosphenytoin results in an increase in free phenytoin blood levels, a decrease in total phenytoin levels, or both. In another embodiment, a method of using carisoprodol, phenytoin or fosphenytoin comprises informing a user that when co-administering carisoprodol with phenytoin or fosphenytoin, the level of free phenytoin in a patient serum should be monitored, the level of total phenytoin should be monitored, or both. Also included are methods and articles of manufacture.2009-05-07
20090118238DEUTERIUM-ENRICHED ALENDRONATE - The present application describes deuterium-enriched alendronate sodium, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.2009-05-07
20090118239Amorphous and crystalline forms of ibandronate disodium - Provided are amorphous and crystalline forms of ibandronate disodium, as well as processes for the preparation thereof.2009-05-07
20090118240LOCAL TREATMENT OF NEUROFIBROMAS - A method for treating a neurofibroma, e.g. dermal neurofibroma, a subdermal neurofibroma, or a superficial plexiform neurofibroma, in a subject in need of such treatment is disclosed. The method comprises locally applying a composition to a neurofibroma either topically or intralesionally. This method does not encompass systemic administration of the composition to the subject to have an effect on the neurofibromas. Compositions useful for such treatments and methods of preparing the compositions are disclosed.2009-05-07
20090118241BIOABSORBABLE POLYMER COMPOSITIONS EXHIBITING ENHANCED CRYSTALLIZATION AND HYDROLYSIS RATES - A bimodal bioabsorbable polymer composition. The composition includes a first amount of a bioabsorbable polymer polymerized so as to have a first molecular weight distribution; a second amount of said bioabsorbable polymer polymerized so as to have a second molecular weight distribution having a weight average molecular weight between about 10,000 to about 50,000 Daltons, the weight average molecular weight ratio of said first molecular weight distribution to said second molecular weight distribution is at least about two to one; wherein a substantially homogeneous blend of said first and second amounts of said bioabsorbable polymer is formed in a ratio of between about 50/50 to about 95/5 weight/weight percent. Also disclosed are a medical device, a method of making a medical device and a method of melt blowing a semi-crystalline polymer blend.2009-05-07
20090118242Injectable capsaicin with non-steroidal anti-inflammatory adjunctive agent - Disclosed in certain embodiments is a method for relieving pain at a site in a human or animal in need thereof, comprising administering by injection or infiltration, a dose of a capsaicinoid and coadministering an effective amount of a NSAID to decrease an undesired effect of the capsaicinoid.2009-05-07
20090118243Compositions and methods for the treatment of ophthalmic conditions - The invention relates to methods of treating ophthalmic conditions comprising administering a compound of formula A, a compound of any one of formulae 1-49, a lipoxin compound, or an oxylipin compound.2009-05-07
20090118244BENZODIAZEPINONE COMPOUNDS USEFUL IN THE TREATMENT OF SKIN CONDITIONS - The present invention provides a family of benzodiazepinone compounds and pharmaceutical compositions thereof. The present invention also provides methods of treating certain skin conditions, e.g., atopic dermatitis, rosacea, or psoriasis, by administering a benzodiazepinone and methods of reducing the proliferation of keratinocyte cells by exposing such cells to a benzodiazepinone.2009-05-07
20090118245MEDICAMENT - The present invention relates to a medicament which contains as the active ingredient combination at least one gestagen with a contraceptive action as the sole hormone component and at least one insulin sensitiser, which medicament is in particular suitable for preventing or treating pathological disorders which are caused by polycystic ovary syndrome (PCOS).2009-05-07
20090118246Therapeutic ophthalmic compositions containing retinal friendly recpients and related methods - Pharmaceutical compositions suitable for administration into the interior of an eye of a person or animal are described. The present compositions include one or more components which are effective in providing a reduced toxicity relative to existing intraocular ophthalmic compositions. The present compositions include one or more therapeutic agents in amounts effective in providing a desired therapeutic effect when placed in an eye, and one or more retinal friendly excipients that have a reduced toxicity relative to benzyl alcohol or polysorbate 80. In certain compositions, the excipient component of the compositions comprises one or more cyclodextrins or cyclodextrin derivatives. Methods of using the compositions to treat ocular conditions are also described.2009-05-07
20090118247Therapeutic ophthalmic compositions containing retinal friendly excipients and related methods - Pharmaceutical compositions suitable for administration into the interior of an eye of a person or animal are described. The present compositions include one or more components which are effective in providing a reduced toxicity relative to existing intraocular ophthalmic compositions. The present compositions include one or more therapeutic agents in amounts effective in providing a desired therapeutic effect when placed in an eye, and one or more retinal friendly excipients that have a reduced toxicity relative to benzyl alcohol or polysorbate 80. In certain compositions, the excipient component of the compositions comprises one or more cyclodextrins or cyclodextrin derivatives. Methods of using the compositions to treat ocular conditions are also described.2009-05-07
200901182483-Alpha-hydroxy 21-n-heteroaryl-pregnane derivatives for modulation of brain excitability and a process for the production thereof - The invention relates to a novel multi step process of making compounds of Formula I:2009-05-07
20090118249DHEAS INHALATION COMPOSITIONS - The present invention provides compositions for aqueous suspension comprising DHEAS and a divalent cation. The suspension in combination with a nebulizer or nasal pump spray can be administers as an aerosol for the treatment of respiratory diseases and conditions. The present invention also provides methods for making compositions in form of aqueous suspension of DHEA and divalent cations.2009-05-07
20090118250PHARMACEUTICAL COMPOSITION - A pharmaceutical composition comprising: (A) an androgen; (B) a cyclic enhancer of the type used in the compositions and methods claimed by U.S. Pat. No. 5,023,252 to Hsieh; and (C) a thickening agent; including, for example, a composition in which the cyclic enhancer is a macrocyclic ester or a macrocyclic ketone; the use of the composition to treat a condition, for example, male hypogonadism, in a patient by applying the composition to the membrane of the patient; and a method for making the composition.2009-05-07
20090118251PHARMACEUTICAL COMPOSITION - A pharmaceutical composition comprising: (A) an androgen; (B) a cyclic enhancer of the type used in the compositions and methods claimed by U.S. Pat. No. 5,023,252 to Hsieh; and (C) a thickening agent; including, for example, a composition in which the cyclic enhancer is a macrocyclic ester or a macrocyclic ketone; the use of the composition to treat a condition, for example, male hypogonadism, in a patient by applying the composition to the membrane of the patient; and a method for making the composition.2009-05-07
20090118252PHARMACEUTICAL COMPOSITION - A pharmaceutical composition comprising: (A) an androgen; (B) a cyclic enhancer of the type used in the compositions and methods claimed by U.S. Pat. No. 5,023,252 to Hsieh; and (C) a thickening agent; including, for example, a composition in which the cyclic enhancer is a macrocyclic ester or a macrocyclic ketone; the use of the composition to treat a condition, for example, male hypogonadism, in a patient by applying the composition to the membrane of the patient; and a method for making the composition.2009-05-07
20090118253COMPOSITIONS AND METHODS FOR TREATING DYSFUNCTIONAL UTERINE BLEEDING - The subject matter of the instant invention is pertinent to the field of hormone therapy. More specifically, the subject matter of the instant invention concerns methods of treating dysfunctional uterine bleeding. The instant invention is also relevant to the treatment and/or prevention of anemia in patients with dysfunctional uterine bleeding. Compositions for practicing the methods, comprising progesterone antagonists are also disclosed. Embodiments of the instant invention also disclose methods for identifying new selective progesterone receptor modulators for practicing disclosed methods of treatment.2009-05-07
20090118254HISTAMINE H3 RECEPTOR AGENTS, PREPARATION AND THERAPEUTIC USES - The present invention discloses novel compounds of Formula I or pharmaceutically acceptable salts thereof which have histamine-H3 receptor antagonist or inverse agonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I as well as methods of using these compositions to treat obesity, cognitive deficiencies, narcolepsy, and other histamine H3 receptor-related diseases.2009-05-07
20090118255Crp Lowering Agent - The present invention provides a novel drug which is useful as a preventive and/or therapeutic agent for various diseases involved in elevation of CRP level, in particular, inflammatory disease and cancer comprising a compound having inhibitory activity against squalene synthase or a salt thereof, or a prodrug thereof.2009-05-07
20090118256CHRONOTHERAPEUTIC DILTIAZEM FORMULATIONS AND THE ADMINISTRATION THEREOF - A method of treating or preventing myocardial ischemia in a patient in need thereof comprising administration of a controlled-release Galenical preparation of pharmaceutically acceptable Diltiazem including the pharmaceutically acceptable salts thereof, suitable for evening dosing every 24 hours containing from about 180 mg to about 420 mg of the form of Diltiazem associated with excipients to provide controlled (sustained) release of the form of Diltiazem for providing a Cmax of diltiazem in the blood at between about 10 hours and about 17 hours after administration, the preparation comprising the form of Diltiazem in oral sustained-release dosage form in which the Diltiazem is adapted to be released after administration over a prolonged period of time and exhibits when given to humans (i) a higher bioavailability when given at night compared to when given in the morning without food according to FDA guidelines or criteria and (ii) bioequivalence when given in the morning with and without food according to the same FDA guidelines or criteria.2009-05-07
200901182574-(p-QUINONYL)-2-HYDROXYBUTANAMIDE DERIVATIVES FOR TREATMENT OF MITOCHONDRIAL DISEASES - Methods of treating or suppressing mitochondrial diseases, such as Friedreich's ataxia (FRDA), Leber's Hereditary Optic Neuropathy (LHON), mitochondrial myopathy, encephalopathy, lactacidosis, and stroke (MELAS), Kearns-Sayre Syndrome (KSS), are disclosed, as well as compounds useful in the methods of the invention, such as 4-(p-quinolyl)-2-hydroxybutanamide derivatives. Methods and compounds useful in treating other disorders such as amyotrophic lateral sclerosis (ALS), Huntington's disease, Parkinson's disease, and pervasive developmental disorders such as autism are also disclosed. Energy biomarkers useful in assessing the metabolic state of a subject and the efficacy of treatment are also disclosed. Methods of modulating, normalizing, or enhancing energy biomarkers, as well as compounds useful for such methods, are also disclosed.2009-05-07
20090118258COMBINATION THERAPY COMPRISING ANGIOTENSIN CONVERTING ENZYME INHIBITORS AND VASOPRESSIN RECEPTOR ANTAGONISTS - The present invention relates to certain pharmaceutical compositions containing at least one vasopressin receptor antagonist and at least one angiotensin converting enzyme (ACE) inhibitor and methods for preparing these compounds, compositions, intermediates and derivatives thereof and for the treatment of vasopressin and/or angiotensin converting enzyme mediated disorders.2009-05-07
20090118259PHARMACEUTICAL USE OF SUBSTITUTED AMIDES - The use of substituted amides for modulating the activity of 11-hydroxysteroid dehydrogenase type 1 (11HSD1) and the use of these compounds as pharmaceutical compositions, are described. Also a novel class of substituted amides, their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments are described. The present compounds are modulators and more specifically inhibitors of the activity of 11HSD1 and may be useful in the treatment, prevention and/or prophylaxis of a range of medical disorders where a decreased intracellular concentration of active glucocorticoid is desirable.2009-05-07
20090118260ARYL- AND HETEROARYL-SUBSTITUTED TETRAHYDROBENZAZEPINES AND USE THEREOF TO BLOCK REUPTAKE OF NOREPINEPHRINE, DOPAMINE, AND SEROTONIN - The compounds of the present invention are represented by the following aryl- and heteroaryl-substituted tetrahydrobenzazepine and dihydrobenzazapine derivatives having formulae I(A-E) and formula (II):2009-05-07
20090118261QUINAZOLINONE DERIVATIVES AND THEIR USE AS B-RAF INHIBITORS - The invention relates to chemical compounds of the formula (I): or pharmaceutically acceptable salts thereof, which possess B Raf inhibitory activity and are accordingly useful for their anti cancer activity and thus in methods of treatment of the human or animal body. The invention also relates to processes for the manufacture of said chemical compounds, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments of use in the production of an anti-cancer effect in a warm blooded animal such as man.2009-05-07
20090118262Non-Aqueous Water-Miscible Materials as Vehicles for Drug Delivery - A pharmaceutical composition includes at least one pharmaceutical component having a low aqueous solubility and at least one non-aqueous water-miscible material. Such a pharmaceutical composition is useful in providing a therapeutically meaningful amount of such pharmaceutical component at a target tissue. The pharmaceutical composition is particularly suitable for administration to or into an ocular environment to treat or control an ocular disease, disorder, or condition.2009-05-07
20090118263Novel Adenine Compound - An adenine compound represented by the formula (1): (1) [wherein A2009-05-07
20090118264Medicament having neovascularization promoting action - Methods of use of medicaments having neovascularization promoting action, which medicaments comprise a retinoid antagonist such as 4-(5H-7,8,9,10-tetrahydro-5,7,7,10,10-pentamethylbenzo[e]naphtho[2,3-b][1-,4]diazepin-13-yl)benzoic acid as an active ingredient.2009-05-07
20090118265NOVEL 1,4-DIAZA-BICYCLO[3.2.2]NONANE DERIVATIVES AND THEIR MEDICAL USE - This invention relates to novel 1,4-diaza-bicyclo[3.2.2]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.2009-05-07
20090118266NOVEL 1,4-DIAZA-BICYCLO[3.2.2]NONYL OXADIAZOLYL DERIVATIVES AND THEIR MEDICAL USE - This invention relates to novel 1,4-diaza-bicyclo[3.2.2]nonyl oxadiazolyl derivatives and their use in the manufacture of pharmaceutical compositions. The compounds of the invention are found to be cholinergic ligands at the nicotinic acetylcholine receptors.2009-05-07
20090118267INDANES - Compounds of the formula (I), in which R2009-05-07
20090118268OMEGA-CARBOXY ARYL SUBSTITUTED DIPHENYL UREAS AS p38 KINASE INHIBITORS - This invention relates to the use of a group of aryl ureas in treating p38 mediated diseases, and pharmaceutical compositions for use in such therapy.2009-05-07
20090118269Methods for Treating Spinal Muscular Atrophy Using Tetracycline Compounds - Methods for using tetracycline compounds for the treatment of spinal muscular atrophy are described.2009-05-07
20090118270PHOSPHODIESTERASE 4 INHIBITORS - PDE4 inhibition is achieved by novel compounds, e.g., N-substituted diarylamine analogs. The compounds of the present invention are of Formulas I-III:2009-05-07
20090118271Preventive or Therapeutic Agents for Pancreatic Cancer, Ovarian Cancer, or Liver Cancer Comprising a Novel Water-Soluble Prodrug - Preventive or therapeutic agents for pancreatic cancer, ovarian cancer, or liver cancer of the present invention comprise a water-soluble prodrug represented by formula 1 described below, or a pharmaceutically acceptable salt, or a hydrate or solvate of the prodrug or pharmaceutically acceptable salt,2009-05-07
20090118272BENZOTHIAZOLE AND AZABENZOTHIAZOLE COMPOUNDS USEFUL AS KINASE INHIBITORS - A compound of Formula (I)2009-05-07
20090118273Compounds and Compositions as Protein Kinase Inhibitors - The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of Abl, Bcr-Abl, Bmx, BTK, b-RAF, c RAF, CSK, cSRC, Fes, FGFR3, Flt3, IKKα, IKKβ, JNK1α1, JNK2α2, Lck, Met, MKK4, MKK6, p70S6K, PAK2, PDGFRα, PKA, PKCα, PKD2, ROCK-II, Ros, Rsk1, SAPK2α, SAPK2β, SAPK3, SAPK4, SGK, Syk, Tie2 and TrkB kinases.2009-05-07
20090118274MONOCYCLIC AMINOPROPYL TETRAHYDRO-PYRAZOLO-PYRIDINE MODULATORS OF CATHEPSIN S - Monocyclic aminopropyl tetrahydro-pyrazolo-pyridine compounds are described, which are useful as cathepsin S modulators. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by cathepsin S activity, such as psoriasis, pain, multiple sclerosis, atherosclerosis, and rheumatoid arthritis.2009-05-07
20090118275THIAZOLOPYRIMIDINE P13K INHIBITOR COMPOUNDS AND METHODS OF USE - Compounds of Formulas Ia and Ib, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula Ia and Ib for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.2009-05-07
20090118276THIENOPYRIMIDINES, THIENOPYRIDINES, AND PYRROLOPYRIMIDINES AS B-RAF INHIBITORS - The present invention relates to compounds of formula la:2009-05-07
200901182773 Unsubstituted N-(aryl- or heteroaryl)-pyrazolo[1,5-a]pyrimidines as Kinase Inhibitors - The invention relates to 3-unsubstituted N-(aryl- or heteroaryl)-pyrazolo[1,5-a]pyrimidine compounds, their use as kinase inhibitors, new pharmaceutical formulations comprising said compounds, said compounds for use in the diagnostic or therapeutic treatment of warm-blooded animals, especially humans, their use in the treatment of diseases or for the manufacture of pharmaceutical formulations useful in the treatment of diseases that respond to modulation of kinase, especially tie-2 kinase, activity, methods of treatment comprising administration of said compounds to a warm-blooded animal, especially a human, and processes for the manufacture of said compounds.2009-05-07
20090118278COMPOSITIONS USEFUL AS INHIBITORS OF GSK-3 - The present invention provides a compound of formula I:2009-05-07
20090118279COMPOUND CONTAINING BASIC GROUP AND USE THEREOF - The present invention relates to a compound represented by formula (I):2009-05-07
20090118280Compounds Which Potentiate AMPA Receptor and Uses Thereof in Medicine - Compounds of formula (I) and salts are provided:2009-05-07
20090118281Amino Alcohol Derivatives And Their Use As Renin Inhibitor - The application relates to novel amino alcohols of the general formula (I) where R, R2009-05-07
20090118282Compounds and methods for treatment of amyloid-beta-peptide related disorders - The present invention relates to compounds, preparation and uses thereof, particularly in the pharmaceutical industry. The present invention discloses novel compounds more particularly useful for the treatment of Alzheimer's disease and other similar diseases, and more specifically the inventive compounds modulate (in particular, inhibit) the level of amyloid-β peptide (Aβ) exhibited by cells or tissues; Aβ peptide is a major component of the amyloid plaques found in the brains of Alzheimer's sufferers. This invention also relates the use of these inhibitors to prevent, treat or ameliorate the symptoms of Alzheimer's disease or any Amyloid-β-Peptide Related Disorder.2009-05-07
20090118283Amide Derivatives as Kinase Inhibitors - The present invention relates to new AGC kinase inhibitors, in particular to compounds of Formula (I) or (II) or a stereoisomer tautomer, racemic, metabolite, pro- or predrug, salt, hydrate, or solvate thereof, wherein Ar2009-05-07
20090118284Novel compounds that are ERK inhibitors - Disclosed are the ERK inhibitors of formula 1.0:2009-05-07
20090118285USE OF KCNQ-OPENERS FOR TREATING OR REDUCING THE SYMPTOMS OF SCHIZOPHRENIA - The invention relates to a novel method for treating or reducing the symptoms of schizophrenia, said method comprising administering to a host in need thereof an effective amount of a compound able to selectively increase the ion flow through KCNQ potassium channels. Furthermore the invention relates to the use of selective KCNQ potassium channel openers for the preparation of a pharmaceutical composition for treating or reducing the symptoms of schizophrenia and related symptoms, disorders and diseases. Furthermore the invention relates to a method of screening for a compound, which is a selective KCNQ potassium channel opener and which is capable of having an anti-psychotic potential.2009-05-07
20090118286Heterobicyclic Acrylamides - Use of heterobicyclic acrylamides of the formula (I)2009-05-07
20090118287ORGANIC COMPOUNDS - The present invention provides a compound of formula (I):2009-05-07
20090118288N-Benzyl-Morpholine Derivatives as Modulators of the Chemokine Receptor - The present invention provides a compound of a formula (I): wherein the variables are defined herein; to a process for preparing such a compound; and to the use of such a compound in the treatment of a chemokine (such as CCR3) mediated disease state.2009-05-07
20090118289(Biphenyl) Carboxylic Acids and Derivatives Thereof - The present invention relates to compounds having the general formula (I) with the definitions of A, X, R2009-05-07
20090118290Indoleacetic acid and indenacetic acid derivatives as therapeutic agents with reduced gastrointestinal toxicity - The presently disclosed subject matter provides derivatives of non-steroidal anti-inflammatory drugs (NSAIDs) that are characterized by substantially reduced cyclooxygenase inhibiting activity, yet retain the ability to interact with and modulate the activities of other polypeptides such as the class of peroxisome proliferators-activated receptors (PPARs) and γ-secretase. Also provided are methods of using the derivatives to treat pathological disorders.2009-05-07
20090118291Histone deacetylase inhibitors - This invention relates to hydroxamic acid derivatives having a carbamate linkage, that are inhibitors of histone deacetylase (HDAC), and are useful in the prevention and/or treatment of cellular proliferative diseases, for example cancer, autoimmune, allergic and inflammatory diseases, diseases of the central nervous system (CNS) such as neurodegenerative diseases, and in the prevention and/or treatment of restenosis.2009-05-07
20090118292CYTOKINE INHIBITORS - A compound of Formula I:2009-05-07
20090118293METHODS FOR REDUCING HOSPITALIZATIONS RELATED TO HEART FAILURE - The invention provides methods for (a) prolonging time to hospitalization for heart failure; (b) prolonging time to first hospitalization for heart failure; (c) reducing the total number of days a patient with heart failure spends in the hospital for heart failure for a single hospital stay (i.e., reducing the duration of a single hospital stay for a patient with heart failure); (d) reducing the total number of days a patient spends in the hospital for heart failure for multiple hospital stays; (e) reducing the number of hospital admissions for heart failure; and (f) reducing mortality and reducing hospitalizations for heart failure (e.g., the total number of days in the hospital and/or the number of hospital visits) in a patient in need thereof comprising administering to the patient a therapeutically effective amount of (i) a hydralazine compound or pharmaceutically acceptable salt thereof, (ii) isosorbide dinitrate and/or isosorbide mononitrate, and (iii) optionally at least one compound selected from the group consisting of angiotensin converting enzyme inhibitors, β-adrenergic antagonists, angiotensin II antagonists, aldosterone antagonists, cardiac glucosides (digitalis), and diuretic compounds.2009-05-07
20090118294COMPOSITIONS AND METHODS RELATED TO HEART FAILURE - The invention provides methods for reducing the total number of days a patient with heart failure spends in the hospital for heart failure for a single hospital stay (i.e., reducing the duration of a single hospital stay for a patient with heart failure); reducing the total number of days a patient spends in the hospital for heart failure for multiple hospital stays (i.e., two or more hospital stays); reducing the number of hospital admissions for heart failure; and reducing mortality and reducing hospitalizations for heart failure (e.g., the total number of days in the hospital and/or the number of hospital visits); by administering to a patient a therapeutically effective amount of (i) a hydralazine compound or pharmaceutically acceptable salt thereof, (ii) isosorbide dinitrate and/or isosorbide mononitrate, and (iii) optionally at least one angiotensin converting enzyme inhibitors, β-adrenergic antagonists, angiotensin II antagonists, aldosterone antagonists, cardiac glucosides (digitalis), or diuretic compounds.2009-05-07
20090118295CHEMICAL COMPOUNDS - The use of a compound of formula I wherein Y is a single bond, C═O, C═S or S(O)2009-05-07
20090118296Heteroaromatic Compounds As Inhibitors Of Stearoyl-Coenzyme A Delta-9 Desaturase - Heteroaromatic compounds of structural formula (I) are selective inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD1) relative to other known stearoyl-coenzyme A desaturases. The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease; atherosclerosis; lipid disorders; obesity; diabetes; neurological disease; metabolic syndrome; insulin resistance; and fatty liver disease.2009-05-07
20090118297POLYMORPHS OF DASATINIB AND PROCESS FOR PREPARATION THEREOF - Provided is dasatinib, solvates thereof and their crystalline forms, methods for their preparation, and pharmaceutical compositions thereof.2009-05-07
20090118298Octahydropentalene compounds as chemokine receptor antagonists - The present invention is directed to novel compounds of Formula (I)2009-05-07
20090118299AGENT FOR PREVENTION OR TREATMENT OF GLAUCOMA - There is Provided an Agent for Prevention of glaucoma or an agent for prevention or treatment of ocular hypertension, with a potent ocular hypotensive effect and prolonged duration thereof. An agent for prevention or treatment of glaucoma comprising a Rho kinase inhibitor and a carbonic anhydrase inhibitor in combination.2009-05-07
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