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27th week of 2009 patent applcation highlights part 57
Patent application numberTitlePublished
20090170795Kit of parts designed for implementing an antitumoral or antiviral treatment in a mammal - The present invention relates to a kit of parts comprising a nucleic acid sequence encoding a permease and a drug comprising one nucleobase moiety or a precursor thereof. The present invention further relates to a kit of parts comprising a precursor of a drug comprising a gene coding a permease and a nucleic acid sequence comprising a suicide gene. The present invention also relates to a vector comprising a gene coding a permease and a suicide gene.2009-07-02
20090170796Histone Demethylation Mediated By The Nuclear Amine Oxidase Homolog LSD1 - LSD1, a homolog of nuclear amine oxidases, functions as a histone demethylase and transcriptional co-repressor. LSD1 specifically demethylates histone H3 lysine 4, which is linked to active transcription. Lysine demethylation occurs via an oxidation reaction that generates formaldehyde. Importantly, RNAi inhibition of LSD1 causes an increase in H3 lysine 4 methylation and concomitant de-repression of target genes, suggesting that LSD1 represses transcription via histone demethylation. The results thus identify a histone demethylase conserved from 2009-07-02
20090170797Hunk, a snfi-related kinase essential for mammary tumor metastasis - This invention relates generally to a novel serine/threonine protein kinase, specifically to hormonally up-regulated, neu-tumor-associated kinase (HUNK); and to the role of HUNK in tumor metastasis, primary tumor development, and the prediction of tumor behavior.2009-07-02
20090170798Highly safe intranasally administrable gene vaccines for treating alzheimer's disease - An objective of the present invention is to provide a safe and effective vaccine therapy for Alzheimer's disease. A minus strand RNA viral vector carrying amyloid gene was constructed, and administered intranasally to 24- to 25-months-old APP transgenic mice. The level of serum anti-A 42 antibody was determined and showed to be markedly higher than the control. The results of histological investigation showed that the administration of a vector of the present invention markedly reduced senile plaques in all of the frontal lobe, parietal lobe, and hippocampus. The brain A level was also markedly reduced. Furthermore, the administration of a vector of the present invention did not result in lymphocyte infiltration in the central nervous system.2009-07-02
20090170799MODULATION OF C-REACTIVE PROTEIN EXPRESSION - Compounds, compositions and methods are provided for modulating the expression of C-reactive protein. The compositions comprise oligonucleotides, targeted to nucleic acid encoding C-reactive protein. Methods of using these compounds for modulation of C-reactive protein expression and for diagnosis and treatment of disease associated with expression of C-reactive protein are provided.2009-07-02
20090170800GENETIC CONSTRUCTS AND COMPOSITIONS COMPRISING RRE AND CTE AND USES THEREOF - Genetic constructs that comprise a coding sequence for HIV-1 Rev, and a coding sequence for a desired protein are disclosed. Compositions that comprise at least two nucleic acid molecules in which at least one nucleic acid molecule comprises a coding sequence for HIV-1 Rev, and at least one nucleic acid molecule comprises a coding sequence for a desired protein are disclosed. In such genetic constructs and compositions comprising nucleic acid molecules, the coding sequence for the desired protein comprises at least a portion of coding sequence for an HIV structural protein that includes an RRE and at least one CTE. Methods of inducing an immune response against an immunogen in an individual, methods of delivering proteins to an individual and methods of producing proteins are also disclosed.2009-07-02
20090170801METHODS OF TREATMENT OF CARDIOVASCULAR AND CEREBROVASCULAR DISEASES WITH FUCOIDAN - A method for treating an ischemic cardiovascular or cerebrovascular disease comprising administrating to a patient in the need of such treatment a pharmaceutical composition comprising fucoidan.2009-07-02
20090170802METHOD FOR PRODUCING POLYMERS - The invention relates to a method for producing polymers, in particular synthetic nucleic acid double strands of optional sequence, comprising the steps: 2009-07-02
20090170803ADJUNCTIVE TREATMENT OF BIOLOGICAL DISEASES - The present invention provides a therapeutic method for treating biological diseases that includes the administration of an effective amount of a suitable antibiotic agent, antifungal agent or antiviral agent in conjunction with an A2009-07-02
20090170804PIRFENIDONE/TOLL-LIKE RECEPTOR (TLR) AGONIST COMPOSITIONS AND METHODS FOR USING THEM TO STIMULATE PRODUCTION OF GRANULOCYTE COLONIZING STIMULATING FACTOR (G-CSF) - The invention disclosed herein relates to compositions and methods for treating subjects suffering from or at risk of developing neutropenia. In some embodiments, the methods comprise administering to a subject suffering from or at risk of developing neutropenia, an effective amount of pirfenidone and one or more toll-like receptor (TLR) agonists.2009-07-02
20090170805ANTI-MICROBIAL AGENTS AND USES THEREOF - Many pathogens, including 2009-07-02
20090170806COMBINATION OF ALOVUDINE AND ZIDOVUDINE IN A MOLAR RATIO OF 1:100 TO 1:350 - Co-administration of alovudine and zidovudine at ratios considerably in excess of the prior art completely or substantially abolishes the mitochondrial toxicity of alovudine in mitochondrial DNA depletion experiments. The invention thus provides pharmaceutical compositions comprising alovudine and zidovudine in a molar ratio in the range 1:100 to 1:350 and methods for the treatment or prophylaxis of multiply resistant HIV comprising the simultaneous or consequential administration of alovudine and zidovudine in the characteristic molar ratio.2009-07-02
20090170807Methods and means for producing hyaluronan - The present invention relates to fungal cells and fungi which synthesize hyaluronan and to methods for preparing such fungi, and also to methods for preparing hyaluronan with the aid of these fungal cells or fungi. Furthermore, the present invention relates to the use of fungi for preparing hyaluronan and to food or feed which comprises hyaluronan.2009-07-02
20090170808ORAL AGENT FOR IMPROVING AND PROTECTING THE FUNCTION OF JOINT COMPRISING HYALURONIC ACID-PHOSPHOLIPID COMPLEXES - The present invention relates to an oral formulation comprising a hyaluronic acid-phospholipid complex, and to use of a hyaluronic acid-phospholipid complex for the manufacture of a joint function-improving and protecting agent for oral administration which can alleviate the arthritic symptoms in patients with arthritic conditions, increase the concentration of hyaluronic acid in synovial fluid, improve the lubrication of joints, as well as maintain and enhance the normal functions of joints.2009-07-02
20090170809Pectic Polysaccharides Isolated from Fruit Pods of Okra - The invention relates to a method for producing a high molecular weight pectin-like polysaccharide from fruit pods of okra. The high molecular weight pectin-like polysaccharide, when dissolved in a buffer, exhibit viscoelastic properties, and is very useful in applications such as ophthalmic surgery, dermatology and orthopedics.2009-07-02
20090170810METHODS OF TREATMENT OF CARDIOVASCULAR AND CEREBROVASCULAR DISEASES WITH LOW MOLECULAR WEIGHT FUCOIDAN - A method for treating an ischemic cardiovascular or cerebrovascular disease comprising administrating to a patient in the need of such treatment a pharmaceutical composition comprising low molecular weight fucoidan.2009-07-02
20090170811Composition for treatment of a detached retina and method of prodution thereof - The present invention relates to a composition for use in the treatment of a detached retina, comprising an oil and an additive capable of increasing the extensional viscosity of the oil. The present invention also relates to a method and kit of parts for producing the composition.2009-07-02
20090170812Transcription factor modulating compounds and methods of use thereof - Substituted benzoimidazole compounds useful as anti-infectives that decrease resistance, virulence, or growth of microbes are provided. Methods of making and using substituted benzoimidazole compounds, as well as pharmaceutical preparations thereof, in, e.g., reducing antibiotic resistance and inhibiting biofilms.2009-07-02
20090170813Hypophosphorous Acid Derivatives and their Therapeutical Applications - Hypophosphorous acid derivatives having Formula (I) wherein .M is a [C(R3,R4)]n1-C(E,COOR1,N(H,Z)) group, or an optionally substituted Ar—CH(COOR1,N(H,Z)) group, or an a, β, or a β, g-cyclic amino acid; .R2009-07-02
200901708147,8-BICYCLOAKYL-CHROMAN DERIVATIVES - 7,8-Bicyclic-chroman derivatives of Formula I:2009-07-02
20090170815ALENDRONATE ORAL LIQUID FORMULATIONS - The invention features an oral pharmaceutical solution comprising a therapeutically effective amount of alendronate or a salt thereof and a pharmaceutically acceptable liquid carrier. The solution is substantially free from degradation products, with the proviso that the solution has no buffer and no complexing agent. The oral solution avoids the difficulties in swallowing tablets of the prior art. Moreover, the oral solution is surprisingly stable without the use of buffering systems and complexing agents of the prior art.2009-07-02
20090170816COMBINATION COMPRISING SQUALENE, A PHOSPHOLIPID AND AN OMEGA 3 FATTY ACID FOR THE TREATMENT OF CANCER - Pharmaceutical composition which comprises squalene or its pharmaceutically acceptable derivatives; at least one phospholipid, its salts or pharmaceutically acceptable derivatives; and at least one omega-3 fatty acid, its salts or pharmaceutically acceptable derivatives. Use of the composition in the preparation of a drug designed for the prophylaxis, treatment and/or improvement of cancer symptoms in mammals. The invention also relates to a fodder for animals such as dogs and cats which comprises the composition.2009-07-02
20090170817CORROSION INHIBITION - The present invention relates to a method of preventing or alleviating the problems associated with corrosion and to novel formulations for use in such a method.2009-07-02
20090170818(20S)-23,23-Difluoro-Methylene-19-Nor-Bishomopregnacalciferol-Vitamin D Analogs - This invention discloses (20S)-23,23-difluoro-2-methylene-19-nor-bishomopregnacalciferol-vitamin D analogs, and specifically (20S)-23,23-difluoro-1α-hydroxy-2-methylene-19-nor-bishomopregnacalciferol, and pharmaceutical uses therefor. This compound exhibits pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as an anti-cancer agent and for the treatment of skin diseases such as psoriasis as well as skin conditions such as wrinkles, slack skin, dry skin and insufficient sebum secretion. This compound also has little, if any, calcemic activity and therefore may be used to treat autoimmune disorders or inflammatory diseases in humans as well as renal osteodystrophy. This compound may also be used for the treatment or prevention of obesity.2009-07-02
20090170819(20R)-23,23-Difluoro-2-Methylene-19-Nor-Bishomopregnacalciferol-Vitamin D Analogs - This invention discloses (20R)-23,23-difluoro-2-methylene-19-nor-bishomopregnacalciferol-vitamin D analogs, and specifically (20R)-23,23-difluoro-1 α-hydroxy-2-methylene-19-nor-bishomopregnacalciferol, and pharmaceutical uses therefor. This compound exhibits pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as an anti-cancer agent and for the treatment of skin diseases such as psoriasis as well as skin conditions such as wrinkles, slack skin, dry skin and insufficient sebum secretion. This compound also has little, if any, calcemic activity and therefore may be used to treat autoimmune disorders or inflammatory diseases in humans as well as renal osteodystrophy. This compound may also be used for the treatment or prevention of obesity.2009-07-02
200901708202-Methylene-(20S,25R)-19,26-Dinor-Vitamin D Analogs - This invention discloses 2-methylene-(20S,25R)-19,26-dinor-vitamin D analogs, and specifically 2-methylene-(20S,25R)-19,26-dinor-1α,25-dihydroxyvitamin D2009-07-02
200901708212-Methylene-(20S,25S)-19,26-Dinor-Vitamin D Analogs - This invention discloses 2-methylene-(20S,25S)-19,26-dinor-vitamin D analogs, and specifically 2-methylene-(20S,25S)-19,26-dinor-1α,25-dihydroxyvitamin D2009-07-02
200901708222-Methylene-20-Methyl-19,24,25,26,27-Pentanor-Vitamin D Analogs - This invention discloses 2-methylene-20-methyl-19,24,25,26,27-pentanor-vitamin D analogs, and specifically 2-methylene-20-methyl-1α-hydroxy-19,24,25,26,27-pentanor-vitamin D2009-07-02
20090170823Dosage Regimens and Pharmaceutical Compositions and Packages for Emergency Contraception - The present invention is directed to dosage regimens for emergency contraception using nonsteroidal progestins and pharmaceutical compositions and packages thereof. Such regimens are useful for females in need of emergency contraception.2009-07-02
20090170824Diarylsulfones as 5-HT2A Antagonists - Compounds of formula I:2009-07-02
20090170825BETA-LACTAMYLALKANOIC ACIDS FOR TREATING PREMENSTRUAL DISORDERS - 0-lactamyl alkanoic acids are described. Methods for treating various premenstrual disorders using or more O-lactamyl alkanoic acids are also described.2009-07-02
20090170826Acid Addition Salt of Optically Active Dihydropyridine Derivative - There is provided an excellent medicine for treating or preventing hypertension or the like. A specific acid addition salt of (R)-2-amino-1,4-dihydro-6-methyl-4-(3-nitrophenyl)-3,5-pyridinedicarboxylic acid 3-(1-diphenyl-methylazetidin-3-yl) ester 5-isopropyl ester is useful as a medicine for treating or preventing hypertension or the like.2009-07-02
20090170827Acid Addition Salt of Dihydropyridine Derivative - There is provided an excellent medicine for treating or preventing hypertension or the like. A specific acid addition salt of 2-amino-1,4-dihydro-6-methyl-4-(3-nitrophenyl)-3,5-pyridinedicarboxylic acid 3-(1-diphenylmethylazetidin-3-yl)ester 5-isopropyl ester is useful as a medicine for treating or preventing hypertension or the like.2009-07-02
20090170828Azetidine Derivatives as Inhibitors of Stearoyl-Coenzyme a Delta-9 Desaturase - Azetidine derivatives 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; obesity; diabetes; neurological disease; metabolic syndrome; insulin resistance; liver steatosis; and non-alcoholic steatohepatitis. (I)2009-07-02
20090170829Carboxamide, Sulfonamide and Amine Compounds and Methods for Using The Same - Disclosed are carboxamide, sulfonamide and amine compounds, as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure2009-07-02
20090170830Tricyclic Beta-Secretase Inhibitors for the Treatment of Alzheimer's Disease - The present invention is directed to tricyclic compounds of formula (I)2009-07-02
20090170831SUBSTITUTED LACTAMS AS INHIBITORS OF ABETA PROTEIN PRODUCTION - Field of the Invention This invention relates to novel lactams of Formula (I):2009-07-02
20090170832HETEROCYCLIC COMPOUNDS HAVING TYPE I 11beta HYDROXYSTEROID DEHYDROGENASE INHIBITORY ACTIVITY - Disclosed is a compound useful as a type I 11βhydroxysteroid dehydrogenase inhibitor.2009-07-02
20090170833PYRAZOLYL DERIVATIVES, PREPARATION PROCESS AND INTERMEDIATES OF THIS PROCESS AS MEDICINAL PRODUCTS AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM - The present invention relates to the novel derivatives of formula (I) in which2009-07-02
20090170834Fused Pyrimidones and Thiopyrimidones, and Uses Thereof - Compounds represented by Structural Formula (I):2009-07-02
20090170835ISOINDOLINE DERIVATIVES - Provided is a novel isoindoline compound of the formula (I):2009-07-02
20090170836NEW INHIBITORS OF HISTONE DEACETYLASE - This invention comprises the novel compounds of formula (I)2009-07-02
20090170837METHODS FOR TREATING RAS DRIVEN CANCER IN A SUBJECT - The invention relates to the discovery that the dibenzodiazepinone analogues have growth inhibiting activities on tumorigenic cells that are driven by expression of RAS or mutated RAS. Thus the invention includes methods for inhibiting the activity of RAS using dibenzodiazepinone analogues; methods for inhibiting the growth of a RAS driven cancer cell using dibenzodiazepinone analogues; methods for inhibiting the growth of a RAS driven cancer using dibenzodiazepinone analogues; and methods for treating a subject having a RAS driven cancer using dibenzodiazepinone analogues.2009-07-02
20090170838Bicycloheteroaryl compounds as P2X7 modulators and uses thereof - Bicycloheteroaryl compounds are disclosed that have a formula represented by the following:2009-07-02
20090170839AEROSOL FORMULATION FOR INHALATION CONTAINING AN ANTICHOLINERGIC AGENT - The invention relates to specific aqueous aerosol formulations that are devoid of propellant, containing one or more anticholinergic agents of formula (1), in which X represents an anion, and containing at least one pharmacologically compatible organic acid and optionally additional pharmacologically compatible adjuvants and/or complexing agents. The cation of formula (1′) is contained in the preparation at a concentration of between 830.22 and 904.2 mg per 100 ml of medicament preparation.2009-07-02
20090170840NS1 protein inhibitors - The present invention generally relates to compounds to treat viral infections and methods of their use. In particular, compounds of the present invention inhibit the activity of NS1 protein, thereby mitigating viral infection and, in particular, influenza virus infection. Accordingly, NS1 protein inhibitors and methods of treatment that employ such inhibitors are contemplated by the present invention.2009-07-02
20090170841Styrenyl Derivative Compounds for Treating Ophthalmic Diseases and Disorders - The present invention relates generally to compositions and methods for treating neurodegenerative diseases and disorders, particularly ophthalmic diseases and disorders. Provided herein are styrenyl derivative compounds, including but not limited to stilbene derivative compounds, and compositions comprising these compounds, that are useful for treating and preventing ophthalmic diseases and disorders, including age-related macular degeneration (AMD) and Stargardt's Disease.2009-07-02
20090170842BRCA1-BASED BREAST OR OVARIAN CANCER PREVENTION AGENTS AND METHODS OF USE - A pharmaceutical composition for use in treating, inhibiting, and/or preventing breast and/or ovarian cancer can include: a molecule having a structure of one of Compounds 1-38, pharmaceutically acceptable salt thereof, or analog thereof, and a pharmaceutically acceptable carrier containing the compound. The pharmaceutically acceptable carrier can be configured for oral, systemic, transdermal, intranasal, suppository, parenteral, intramuscular, intravenous, or subcutaneous administration. The compound can be present in the composition in a therapeutically effective amount for treating, inhibiting, and/or preventing breast and/or ovarian cancer. Also, the compound can be present in a therapeutically effective amount for enhancing production of BRCA1.2009-07-02
20090170843(Poly) aminoacetamide derivatives of epipodophyllotoxin their process of preparation and their applications in therapeutics as anticancer agents - The present invention relates to novel podophyllotoxin derivatives substituted in the 4-position by a substituted (poly)aminoalkylaminoacetamide chain, to their process of preparation and to their use as medicament as anticancer agents.2009-07-02
20090170844Spiro Tetracyclic Compound - Disclosed is an anti-coagulant which has extremely excellent inhibitory effect on FXa and an extremely poor inhibitory effect on hERG channel, and can be administered through the oral route. Specifically, disclosed is a compound represented by the formula (I) or a pharmaceutically acceptable salt thereof.2009-07-02
20090170845USE OF IMIDAZO[2,1-b]-1,3,4-THIADIAZOLE-2-SULFONAMIDE COMPOUNDS TO TREAT NEUROPATHIC PAIN - Disclosed herein are methods and compositions for treating and/or prophylaxis of neuropathic pain in a subject. The methods comprise administering to the subject suffering from neuropathic pain, a therapeutically effective amount of a compound, according to Formula I:2009-07-02
20090170846INHIBITORS OF THE HIV INTEGRASE ENZYME - The present invention is directed to compounds of formula (I), and pharmaceutically acceptable salts and solvates thereof, their synthesis, and their use as modulators or inhibitors of the human immunodeficiency virus “HIV” integrase enzyme. Formula (I).2009-07-02
20090170847Imidazopyridine Derivatives Inhibiting Protein Kinase Activity, Method for the Preparation Thereof and Pharmaceutical Composition Containing Same - The inventive imidazopyridine derivative can be used in a pharmaceutical composition for preventing or treating diseases such as diabetes, obesity, dementia, cancer, and inflammation, since it can efficiently inhibit the activities of several protein kinases including glycogen synthase kinase-3 (GSK-3), aurora kinase, extracellular signal-regulated kinase (ERK), protein kinase B (AKT), and the likes, to control signal transductions thereof.2009-07-02
20090170848THIAZOLONES FOR USE AS PI3 KINASE INHIBITORS - Invented is a method of inhibiting the activity/function of PI3 kinases using substituted thiazolones. Also invented is a method of treating one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries by the administration of substituted thiazolones.2009-07-02
20090170849QUINAZOLINONE DERIVATIVES HAVING B-RAF INHIBITORY ACTIVITY - 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.2009-07-02
20090170850Cycloalkyl derivatives of 3-hydroxy-4-pyridinones - The present invention provides an cycloalkyl derivative of 3-hydroxy-4-pyridinone which is useful for the chelation of metal ions such as iron. Its preparation and use is described. In particular, the invention concerns the removal of iron in chemical and biological systems including chelating agents having the formula I2009-07-02
20090170851Chroman Compounds - Compounds according to Formula (I):2009-07-02
20090170852NOVEL PYRAZOLE-BASED HMG CoA REDUCTASE INHIBITORS - Novel compounds and pharmaceutical compositions useful as hypocholesterolemic and hypolipidemic agents are described. More specifically, potent inhibitors of the enzyme 3-hydroxy-3-methylglutaryl-coenzyme A reductase (“HMG CoA reductase”) are described. Methods of using such compounds and compositions to treat subjects, including humans, suffering from hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, atherosclerosis, Alzheimer's Disease, benign prostatic hypertrophy (BPH), diabetes and osteoporosis are also described.2009-07-02
20090170853NOVEL INHIBITORS OF KINASES - The present invention provides compounds of formula I,2009-07-02
20090170854New Use - The present invention relates to a new use of certain pharmaceutically active compounds in the treatment and/or prevention of medicament induced gastric ulcer. More particularly the invention is directed to the use of said compounds, and pharmaceutically acceptable salts thereof, for the treatment and/or prevention of NSAID (non-steroidal antiinflammatory drugs) induced gastric ulcer as well as a pharmaceutical composition in the unit dosage form for the prevention of NSAID induced gastric ulcer in a mammal comprising an NSAID together with a 6-carboxamido-imidazo[1,2-a]pyridine compounds. Other pharmaceutically active compounds used in the present invention comprises COX-2 inhibitors, NO-NSAIDs and bisphosphonates.2009-07-02
20090170855HIV INHIBITING 3,4-DIHYDRO-IMIDAZO[4,5-B]PYRIDIN-5-ONES - HIV inhibitory compounds of formula:2009-07-02
20090170856HETEROCYCLIC ANTIVIRAL COMPOUNDS - Compounds of formula I, wherein R2009-07-02
20090170857Method for healing a wound using a direct vasodilator - A method for healing a wound comprising the step of topically administering a wound healing composition to a wounded area, wherein the wound healing composition comprises a first medicament characterized as a direct vasodilator and pharmaceutically acceptable salts thereof.2009-07-02
20090170858Methods and Compositions Containing Natural Folates for Protecting Against Radiation Damage - Disclosed are methods for protecting a subject from harmful effects of ionizing radiation. The method includes administering to the subject an effective amount of at least one reduced folate. Also disclosed are radioprotective compositions that include a first radioprotective agent and a second radioprotective agent, where the first radioprotective agent is a reduced folate. Methods for protecting a subject from harmful effects of ultraviolet radiation are also disclosed.2009-07-02
20090170859Viral Polymerase Inhibitors - An enantiomer, diastereoisomer or tautomer of a compound, represented by formula I:2009-07-02
20090170860Use of PARP-1 Inhibitors - A method for improving the cytotoxic effect of Ecteinascidin-743 (ET-743) or an analog thereof on a tumor cell population in a patient the method including administering to the patient, sequentially or simultaneously, a therapeutically effective combination of a composition including ET-743 and an amount of a composition including a PARP-1 inhibitor effective to increase the cytotoxic effect of ET-743 on the tumor cell population. Anti-tumor compositions containing a therapeutically effective amount of ET-743 and an amount of a PARP-1 inhibitor effective to increase the tumor cytotoxicity of the ET-743 are also presented.2009-07-02
20090170861Pyridazinone Derivatives Useful as Glucan Synthase Inhibitors - In its many embodiments, the present invention provides -substituted pyridazinone compounds as glucan synthase inhibitors, methods of preparing such compounds, pharmaceutical including one or more of such compounds, methods of preparing pharmaceutical formulations including one or more such compounds or one or more such compounds along with other antifungal agents, and methods of treatment, prevention, inhibition, or amelioration of one or more fungal infections associated with glucan synthase using such compounds or pharmaceutical compositions.2009-07-02
20090170862USE OF C-KIT INHIBITORS FOR THE TREATMENT OF MYELOMA - The present invention relates to the use of a c-kit inhibitor, especially a c-kit inhibitor of formula I,2009-07-02
20090170863Acylated Spiropiperidine Derivatives as Melanocortin-4 Receptor Modulators - Certain novel N-acylated spiropiperidine derivatives are ligands of the human melanocortin receptor(s) and, in particular, are selective ligands of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the modulation of MC-4R, such as obesity, diabetes, nicotine addiction, alcoholism, sexual dysfunction, including erectile dysfunction and female sexual dysfunction.2009-07-02
20090170864Diacylglycerol Acyltransferase Inhibitors - Provided herein are compounds of the formula (I):2009-07-02
20090170865Treatment of Prostate Cancer with Angiogenesis-Targeting Quinazoline-Based Anti-Cancer Compounds - Provided is a method of inhibiting the growth of prostate cancer cells comprising administering an effective amount of DZ-50 (2-[4-biphenyl-4-sulfonyl)-piperazin-1-yl]-6,7-diisopropoxyquinazolin-4-yl-amine) to a patient in need thereof. In another aspect, a method is provided for inhibiting the initiation of prostate cancer comprising administering an effective amount of DZ-50 to a patient in need thereof. In yet another aspect, a method is provided for inhibiting the formation of a prostate tumor-derived metastatic lesion comprising administering an effective amount of DZ-50 to a patient in need thereof. In any of the aforementioned methods, a quinazoline-based drug which induces apoptosis of a prostate cancer cell may be coadministered with DZ-50. Also provided is a composition comprising DZ-50, a quinazoline-based drug which induces apoptosis of a prostate cancer cell, and a pharmaceutically acceptable carrier.2009-07-02
20090170866MOESIN, CAVEOLIN 1 AND YES ASSOCIATED PROTEIN 1 AS PREDICTIVE MARKERS OF RESPONSE TO DASATINIB IN BREAST CANCERS - The invention described herein relates to methods and compositions useful in the diagnosis, treatment and management of cancers that express particular genes, including the moesin, caveolin 1, and/or yes-associated protein 1 genes.2009-07-02
20090170867TRPV1 ANTAGONISTS INCLUDING SULFONAMIDE SUBSTITUENT AND USES THEREOF - The invention relates to compounds of formula IA′2009-07-02
20090170868TRPV1 ANTAGONISTS INCLUDING DIHYDROXY SUBSTITUENT AND USES THEREOF - The invention relates to compounds of formula IA2009-07-02
20090170869PIPERAZINE DERIVATIVE HAVING AFFINITY FOR THE HISTAMINE H3 RECEPTOR - The present invention relates to 1-(1-methylethyl)-4-{[4-(tetrahydro-2H-pyran-4-yloxy)phenyl]carbonyl}piperazine2009-07-02
20090170870AMIDINE-CONTAINING COMPOUNDS USEFUL AS MUSCARINIC RECEPTOR ANTAGONISTS - The invention relates to compounds of formula I:2009-07-02
20090170871IL-8 Receptor Antagonists - This invention relates to novel compounds and compositions thereof, useful in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).2009-07-02
20090170872Compounds and Their Pharmaceutical Use - The present invention relates to novel compounds of the general formula (I), their analogs, their stereoisomers, their polymorphs, their hydrates, their solvates, their pharmaceutically acceptable salts and compositions. The present invention more particularly provides novel compounds of the general formula (I).2009-07-02
20090170873Pyrazole-substituted arylamides as P2X3 and P2X2/3 antagonists - Compounds of the formula I:2009-07-02
20090170874Triazole-substituted arylamides as P2X3 and P2X2/3 antagonists - Compounds of the formula I:2009-07-02
20090170875COMPOUNDS FOR THE TREATMENT OF INFLAMMATORY DISORDERS - This invention relates to compounds of the Formula (I):2009-07-02
20090170876Novel Topical Formulations of Flucytosine - The invention relates to topical formulations of flucytosine which demonstrate a clear advantage over currently available therapeutic regimens for the treatment and maintenance of fungal infections, particularly vulvovaginal candidiasis. The invention provides compositions which solve the long-standing need for antimicrobial agents which treat effectively resistant strains of 2009-07-02
200901708775,6-Trimethylenepyrimidin-4-one compounds - Pyrimidone compounds of formula (I):2009-07-02
20090170878MACROCYCLIC COMPOUNDS USEFUL AS BACE INHIBITORS - The invention relates to novel macrocyclic compounds of the formula2009-07-02
200901708796,9-Disubstituted Purine Derivatives and Their Use as Cosmetics and Cosmetic Compositions - Certain 6,9-disubstituted purine derivatives and their pharmaceutically acceptable salts are provided. These 6,9-disubstituted purine derivatives and their pharmaceutically acceptable salts are useful in compositions for treating mammalian cells, and especially human skin cells, in order to ameliorate the adverse effects of aging, treat skin disease states, treat immunological responses resulting from or associated with inflammation, and the like.2009-07-02
20090170880Methods and Means for the Treatment of Cancer - Provided are Breast Cancer Resistance Protein (BCRP) inhibitors, P-glycoprotein (P-gp) inhibitors and chemotherapeutic agents for use in the treatment of cancer by combination therapy of the BCRP inhibitor and/or P-gp inhibitor with the chemotherapeutic agent. The chemotherapeutic agent is an imidazotetrazine, e.g. temozolomide.2009-07-02
20090170881NEW INHIBITORS OF HISTONE DEACETYLASE - This invention comprises the novel compounds of formula (I)2009-07-02
20090170882Methods and compositions - Compounds, compositions and methods relating to kinesin inhibition are described herein.2009-07-02
200901708833-ARYLPHENYL SULFIDE DERIVATIVE AND INSECTICIDE AND MITICIDE - 3-Arylphenyl sulfide derivatives represented by general formula (I):2009-07-02
20090170884FUNGICIDAL ACTIVE SUBSTANCE COMBINATION - Active compound combinations comprising an oxime ether derivative of the formula (I)2009-07-02
20090170885NAPHTHYRIDINE DERIVATIVES AS POTASSIUM CHANNEL MODULATORS - This invention provided compounds of formula I2009-07-02
20090170886ANDROGEN MODULATORS - The present invention is directed to a new class of benzonitriles and to their use as androgen receptor modulators. Other aspects of the invention are directed to the use of these compounds to decrease excess sebum secretions and to stimulate hair growth.2009-07-02
20090170887Novel indazole derivative having spiro ring structure in side chain - An object of the present invention is to create a novel indazole derivative having a spiro ring structure in a side chain, which is useful as a pharmaceutical, and to find a new pharmacological activity of the derivative. The present invention compound is represented by the general formula [I] and has an excellent Rho kinase inhibitory activity. In the formula, the ring X represents a benzene ring or a pyridine ring; R2009-07-02
20090170888Antipruritic Agent for Pruritus Caused by Multiple Sclerosis - An antipruritic against pruritus caused by multiple sclerosis is disclosed. The antipruritic comprises as an effective ingredient an κ opioid receptor agonist compound having a 4,5-epoxymorphinan skeleton and having a specific chemical structure, such as Compound 1 having the following structure:2009-07-02
20090170889USE OF FINASTERIDE, DUTASTERIDE AND RELATED COMPOUNDS FOR THE PREVENTION OR TREATMENT OF NEUROLOGICALLY-ASSOCIATED DISORDERS - The present invention relates to new pharmaceutical uses of 4-azasteroid compounds, in particular of Finasteride/Dutasteride/Dutasteride and Dutasteride, particularly preferred of Finasteride/Dutasteride/Dutasteride, and its pharmaceutically acceptable derivatives, and combinations comprising said compounds. The invention also features generally the use of a modulator compound of neuroprotective conditions via beta subunits of shaker-type voltage-gated potassium channels and/or via members of solute carriers family 25, in particular Aralar (member 12) and adenine-nucleotide translocators 1 & 2 (member 4 & 5) and/or via a 4-nitrophenylphosphatase domain and non-neuronal SNAP25-like protein homolog 1 (NIPSNAP 1) as a neuroprotective medicament, particularly as a medicament for the prevention and/or treatment of neurological diseases such as dementia, Parkinson, Alzheimer, schizophrenia or epilepsy. The demonstrated inhibition of the MPTP appears to constitute a novel principle applicable to all pathological conditions which have underlying excitotoxic/mitochondrial mechanisms, like: amyotrophic lateral sclerosis, Alzheimer's disease, depression, epilepsy, multiple sclerosis, pain, Parkinson's disease, schizophrenia, traumatic brain and spinal chord injury, stroke and other ischemic conditions in the brain.2009-07-02
20090170890METHOHDS OF INHIBITING VIRAL INFECTION - A method of inhibiting viral infection in a mammal in need of same, includes administering an effective amount of at least one of the compounds of FGI-103 which are represented by 273, 365 and 510 either prophylactically to prevent viral infection, or therapeutically following viral infection. These compounds appear to selectively inhibit Caspase 8 as a method of preventing infective viral particle release. They can be administered IV, IP, orally or via other conventional administration routes. The compounds are highly effective, requiring relatively low dosages on the order of 1 ng/kg-200 mg/kg of body weight.2009-07-02
20090170891Niacin Receptor Agonists, Compositions Containing Such Compounds and Methods of Treatment - The present invention encompasses compounds of Formula I:2009-07-02
200901708923-Hydroxy-6-phenylphenanthridines as pde4 inhibitors - The compounds of formula I2009-07-02
20090170893NOVEL HYDRATE FORM - The present invention relates to a novel hydrate form of moxifloxacin monohydrochloride, processes for preparing the form, pharmaceutical compositions comprising the form and uses of the form and compositions.2009-07-02
20090170894UREA DERIVATIVES OF TROPANE, THEIR PREPARATION AND THEIR THERAPEUTIC APPLICATION - The present invention is related to a compound of formula (I)2009-07-02
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