22nd week of 2011 patent applcation highlights part 41 |
Patent application number | Title | Published |
20110130341 | METHOD AND KIT FOR DETECTION OF CANCER, AND THERAPEUTIC AGENT FOR CANCER - The object aims to comprehensively analyze miRNA that undergoes epigenetic silencing in cancer to identify miRNA associated with cancer, elucidate the role of the identified miRNA in cancer, and develop a novel method for detecting cancer and a novel therapeutic agent for cancer both of which relate to the miRNA. Disclosed is a method for detecting cancer in a subject, which comprises detecting methylated CpG in a CpG island located in a promoter region of a microRNA 34b gene and/or a microRNA 34c gene in a biological sample collected from the subject. Also disclosed is a therapeutic agent for cancer, which comprises a nucleic acid encoding a BTG4 gene or BTG4, or comprises a nucleic acid encoding a miR-34b gene and/or an miR-34c gene or miR-34b and/or miR-34c. | 2011-06-02 |
20110130342 | PEPTIDE HOMING TO BRAIN TUMORS - The present invention relates to a peptide, which specifically homes to the intracranial, early stage astrocytoma model that grows as islets and harbors co-opted tumor vessels in the brain. The peptide finds its use in targeted delivery of therapeutic substances to invasive brain cancer or metastatic brain lesions as such and in combination with conventional therapies, such as surgery and radiation, and anti-angiogenic therapies, and as a tool in diagnosis of, e.g., invasive brain cancer or metastatic brain lesions. | 2011-06-02 |
20110130343 | IMMUNITY-INDUCING AGENT AND METHOD FOR DETECTION OF CANCER - An immunity-inducing agent comprising as an effective ingredient(s) at least one polypeptide selected from the following polypeptides, the polypeptide(s) having an immunity-inducing activity/activities, or as an effective ingredient(s) a recombinant vector(s) which comprise(s) a polynucleotide(s) encoding the polypeptide(s) and is/are capable of expressing the polypeptide(s) in vivo can be used for therapy and/or prophylaxis of cancer: (a) a polypeptide consisting essentially of not less than 7 consecutive amino acids in any one of the amino acid sequences shown in the odd number IDs of SEQ ID NOs:3 to 95 in SEQUENCE LISTING; (b) a polypeptide having a sequence identity of not less than 90% with the polypeptide (a) and consisting essentially of not less than 7 amino acids; and (c) a polypeptide comprising the polypeptide (a) or (b) as a partial sequence thereof. Further, since the above polypeptide(s) react(s) with antibodies existing specifically in serum of a cancer patient, it is possible to detect cancer in a living body by measuring the antibodies in a sample. | 2011-06-02 |
20110130344 | TIGHT JUNCTION PROTEIN MODULATORS AND USES THEREOF - The invention provides tight junction protein modulators, compositions comprising the same, and uses thereof. In particular, the invention provides tight junction protein modulators that modulate the second extracellular loop of tight junction proteins, such as occludin or claudin. | 2011-06-02 |
20110130345 | ALPHA CONNEXIN C-TERMINAL (ACT) PEPTIDES FOR TREATING AGE-RELATED MACULAR DEGENERATION - Provided herein are compositions and methods for use in treating or preventing macular degeneration in a subject. | 2011-06-02 |
20110130346 | PEPTIDE CONJUGATES FOR DELVERY OF BIOLOGICALLY ACTIVE COMPOUNDS - A construct comprising a cell delivery peptide covalently attached to a biologically active compound suitable for delivery of said biologically active compound into cells, wherein optionally the cells are cardiac muscle, skeletal muscle, smooth muscle or contractile cells. | 2011-06-02 |
20110130347 | IDENTIFICATION OF NEW SPLICE-VARIANTS OF G-PROTEIN COUPLED RECEPTOR EP3 AND USES THEREOF - The present invention is directed to a polynucleotide sequence of the novel G-Protein Coupled Receptors EP3-11 OR EP3-12. The present invention provides polynucleotide sequences comprising the nucleic acid sequence SEQ ID NO: 20 or SEQ ID NO: 21 or nucleic acid sequences that hybridize to SEQ ID NO: 20 or SEQ ID NO: 21 or its complimentary strand having at least 40% sequence identity. The invention also provides the human EP3-11 or EP3-12 as targets for the identification of compounds useful for the treatment and prevention of cardiovascular diseases, inflammation, reproduction disorders and cancer as a result of relative quantification of the mRNA distribution in different human tissues by expression profiling. The invention also provides assays for the identification of compounds modulating EP3-11 or EP3-12. | 2011-06-02 |
20110130348 | KINETICALLY EFFICIENT SUBSTRATE FOR LIPOIC ACID LIGASE - The invention provides methods for identifying and optimizing peptide substrates for enzymes such as lipoic acid ligase (Lp1A). | 2011-06-02 |
20110130349 | Compounds and Methods for Treating Toll-Like Receptor 2-Related Diseases and Conditions - The present invention relates to compounds and methods useful in the prevention or treatment of diseases or conditions associated with Toll-like receptor 2 activation. | 2011-06-02 |
20110130350 | SYNTHESIS SCHEME FOR LACOSAMIDE - The present invention is concerned with an improved method of producing (R)-2-acetamido-N-benzyl-3-methoxypropionamide (lacosamide) comprising the 0-methylation of a compound of formula (I) to produce a compound of formula (II) in a single step reaction. | 2011-06-02 |
20110130351 | GLYCOLIPID FRACTION FROM CYANOBACTERIA FOR TREATMENT OF DISEASES OF THE ORAL CAVITY - The present invention relates to the preparation and use of a glycolipid fraction from | 2011-06-02 |
20110130352 | THE USE OF THE EFFECTIVE FRACTION OF ALKALOIDS FROM MULBERRY TWIG IN PREPARING HYPOGLYCEMIC AGENTS - The present invention relates to an effective fraction of alkaloids and the effective fraction is prepared from mulberry twig and its active ingredients are a composition of alkaloids. Determined by HPLC, the percentage of the total alkaloids are 50% or more by weight in the effective fraction and the percentage of the compound 1-deoxynojirimycin is 30% or more by weight in the total alkaloids. The effective fraction of the invention is prepared as the following steps: the mulberry twig is extracted by solvents, and the extract is precipitated by alcohol precipitation or flocculation to remove the impurities, and then concentrated, purified by resin chromatography. The present invention also relates to a pharmaceutical composition containing the said effective fraction of alkaloids and to the use of the effective fraction of alkaloids according to claim | 2011-06-02 |
20110130353 | HIGHLY PURIFIED ANTIENDOTOXIN COMPOUND - The invention provides compositions containing a highly purified antiendotoxin compound and methods of preparing and using such compositions. | 2011-06-02 |
20110130354 | SULFATED OLIGOSACCHARIDE DERIVATIVES - The invention relates to compounds which are polysulfated oligosaccharide derivatives having activity as inhibitors of heparan sulfate-binding proteins and inhibitors of the enzyme heparanase; methods for the preparation of the compounds; compositions comprising the compounds, and use of the compounds and compositions thereof for the antiangiogenic, antimetastatic, anti-inflammatory, antimicrobial, anticoagulant and/or antithrombotic treatment, lowering of blood triglyceride levels and inhibition of cardiovascular disease of a mammalian subject. | 2011-06-02 |
20110130355 | USE OF SOPHORICOSIDE IN THE MANUFACTURE OF MEDICAMENTS - The present invention relates to the use of sophoricoside for the prevention and/or the treatment of articular cartilage degeneration or osteoarthritis in post-menopausal women. It is effective and has no side-effects on uterus, breasts and the like as animal-derived estrogen does. It is easy to be extracted and the source thereof is abundant. Therefore, it has a promising marketing prospect. | 2011-06-02 |
20110130356 | MORPHINE AND MORPHINE PRECURSORS - Methods and materials related to the use of morphine, morphine precursors (e.g., reticuline), and inhibitors of morphine synthesis or activity to treat diseases, to reduce inflammation, or to restore normal function are provided. | 2011-06-02 |
20110130357 | Aminoglycosides: Synthesis and Use as Antifungals - The present invention relates to novel aminoglycoside analogs having certain substituents at the 6 position of ring III which exhibit improved antifungal activity but possess minimal antibacterial properties. The compounds of the present invention are analogues of kanamycin B and kanamycin A. Also provided are methods of synthesizing and methods of using the compounds of the present invention. The compounds of the present invention are useful in treating or preventing fungal disease. | 2011-06-02 |
20110130358 | METHOD FOR TRANSDIFFERENTIATION OF BODY TISSUES - The invention relates to methods for transdifferentiation of body tissues which can be used to generate specific cell types needed for regenerating organs or body parts, following cellular degeneration, injury or amputation. The present invention also describes the use of tissue transdifferentiation for treating cancer and autoimmune diseases. | 2011-06-02 |
20110130359 | METHODS FOR PREVENTING OR REDUCING NEUROTOXICITY ASSOCIATED WITH ADMINISTERING DPD INHIBITORS IN COMBINATION WITH 5-FU AND 5-FU PRODRUGS - Methods for improved administration and dosing of DPD inhibitors in combination with 5-FU and/or 5-FU prodrugs are provided, comprising first administering to a patient in need thereof a DPD inhibitor that substantially eliminates activity of the enzyme in both nervous and non-nervous tissues within the patient and thereafter administering 5-FU or a 5-FU prodrug, wherein the level of 5-FU or 5-FU generated from a prodrug is in substantial excess of DPD inhibitor in the patient. | 2011-06-02 |
20110130360 | PREVENTING OR REDUCING OXIDATIVE STRESS OR OXIDATIVE CELL INJURY - A water-insoluble cellulose derivative, such as ethyl cellulose is useful for preventing or reducing oxidative stress or oxidative cell injury in tissues of an animal and in particular for influencing the level Stearoyl-CoA Desaturase-1 (SCD1) gene expression or ATP synthase mitochondrial F1 complex assembly factor 1 (ATPAF1) gene expression in non-adipose tissues of the animal. | 2011-06-02 |
20110130361 | SILICON DERIVATIVES AS HISTONE DEACETYLASE INHIBITORS - The present invention relates to a novel class of Silicon derivatives. The Silicon compounds can be used to treat cancer. The Silicon compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases. The present invention further provides pharmaceutical compositions comprising the Silicon derivatives and safe dosing regimens of these pharmaceutical compositions, which are easy to follow, and which result in a therapeutically effective amount of the Silicon derivatives in vivo. | 2011-06-02 |
20110130362 | A2B ADENOSINE RECEPTOR ANTAGONISTS - Disclosed are novel compounds that are A | 2011-06-02 |
20110130363 | BENZOPYRAN AND BENZOXEPIN PI3K INHIBITOR COMPOUNDS AND METHODS OF USE - Benzopyran and benzoxepin compounds of Formulas I and II, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formulas I and II for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed. | 2011-06-02 |
20110130364 | PYRROLOPYRIDINE DERIVATIVES SUBSTITUTED WITH CYCLIC AMINO GROUP - An object of the present invention is to provide an antagonist against CRF receptors which is effective as a therapeutic or prophylactic agent for diseases in which CRF is considered to be involved, such as depression, anxiety, Alzheimer's disease, Parkinson's disease, Huntington's chorea, eating disorder, hypertension, gastric diseases, drug dependence, epilepsy, cerebral infarction, cerebral ischemia, cerebral edema, cephalic external wound, inflammation, immunity-related diseases, alopecia, irritable bowel syndrome, sleep disorders, epilepsy, dermatitides, schizophrenia, etc. This problem can be solved with a pyrrolopyrimidine or pyrrolopyridine derivative substituted with a cyclic amino group represented by formula [I] below which has a high affinity for CRF receptors and is effective against diseases in which CRF is considered to be involved. | 2011-06-02 |
20110130365 | Fluorinated Heteroaryls - The present invention provides Formula (1A) XN O R 3 HN R 5 O R 4 R 2 R 1 (1A) 5 compounds that act as glucokinase activators; pharmaceutical compositions thereof; and methods of treating diseases, disorders, or conditions mediated by the glucokinase enzyme, where X, R 1, R 2, R 3, R 4, and R 5 are as described herein. | 2011-06-02 |
20110130366 | FOSAPREPITANT DIMEGLUMINE INTERMEDIATE, NEUTRAL FOSAPREPITANT, AND AMORPHOUS FOSAPREPITANT DIMEGLUMINE AND PROCESSES FOR THEIR PREPARATIONS - The present invention generally relates to a process for the preparation of fosaprepitant dimeglumine intermediate and its use in the preparation of fosaprepitant dimeglumine; to a neutral form of fosaprepitant in a solid state and processes for the preparation thereof; and to a stable amorphous fosaprepitant dimeglumine, having a stability at temperatures of about 2° C. to about 8° C. and at a relative humidity below at least 60%; and a process for the preparation thereof. | 2011-06-02 |
20110130367 | Combination Therapy for Treating Proliferative Diseases - The present invention relates generally to new chemical combinations and methods for their use in the treatment of proliferative diseases and in particular cancer. | 2011-06-02 |
20110130368 | DERIVATIVES OF 4- OR 5-AMINOSALICYLIC ACID - The present invention provides new derivatives of 4- or 5-aminosalicylic acid, and a pharmaceutical composition containing these derivatives of 4- or 5-aminosalicylic acid as active ingredients, useful for the treatment of intestinal diseases such as inflammatory bowel disease (IBD) and irritable bowel syndrome (IBS) and for the prevention/treatment of colon cancer. More particularly, these derivatives comprise a hydrogen sulfide releasing moiety linked via an azo, an ester, an anhydride, a thioester or an amide linkage to a molecule of 4- or 5-aminosalicylic acid. Furthermore, the present invention provides a process for preparing these compounds and their use for treating IBD and IBS and the prevention/treatment of colon cancer. | 2011-06-02 |
20110130369 | USE OF FTS FOR THE TREATMENT OF MYOCARDIAL ISCHEMIA/REPERFUSION INJURY - Disclosed are methods for reducing the extent of myocardial ischemia/reperfusion injury, comprising administering to a human prior to reperfusion of the ischemic myocardium or pre-angioplasty, coronary artery bypass surgery, or thrombolytic therapy an effective amount of FTS, or various analogs thereof, or a pharmaceutically acceptable salt thereof. Methods of treating ischemia/reperfusion injury, comprising administering to a human after reperfusion of the ischemic myocardium or post-angioplasty, coronary artery bypass surgery, or thrombolytic therapy an effective amount of FTS, or various analogs thereof, or a pharmaceutically acceptable salt thereof are also disclosed. | 2011-06-02 |
20110130370 | Pharmaceutical composition comprising a strontium salt, vitamin D and A cyclodextrin - A pharmaceutical composition comprising a strontium salt, vitamin D and a cyclodextrin. | 2011-06-02 |
20110130371 | C-ring-substituted pregn-4-ene-21,17-carbolactones, and pharmaceutical preparations comprising the same - The present invention relates to C-ring-substituted pregn-4-ene-21,17-carbolactones of the general formula I | 2011-06-02 |
20110130372 | COMPOSITION COMPRISING ESTRONE AND HYDROCORTISONE FOR USE IN THE TOPICAL TREATMENT OF BALDNESS - The present invention relates to a composition comprising an association of active substances for use in the topical treatment of baldness, particularly of male pattern and female pattern androgenetic alopecia. | 2011-06-02 |
20110130373 | METHODS FOR ADMINISTRATION AND FORMULATIONS FOR THE TREATMENT OF REGIONAL ADIPOSE TISSUE - Provided herein are pharmaceutical formulations, methods, and systems for treating regional fat deposits and fat-related conditions and indications. Methods comprise administering a pharmaceutical formulation consisting essentially of a long-acting beta-2 adrenergic receptor agonist, for example, salmeterol, suitable for subcutaneous administration. Methods further comprise administering a pharmaceutical formulation that is suitable for subcutaneous injection comprising: (a) a lipophilic long-acting selective beta-2 adrenergic receptor agonist and/or glucocorticosteroid, or a salt, optical isomer, racemate, solvate, or polymorph thereof; and (b) at least one subcutaneously acceptable inactive ingredient. | 2011-06-02 |
20110130374 | Small Pyrimidine Derivatives and Methods of Use Thereof - Provided are pyrimidine derivatives which are ubiquitination inhibitors that inhibit the ubiquitin ligase activity, particularly of POSH polypeptides, and are useful for the treatment of cancer, angiogenesis disorders, and inflammatory disorders. | 2011-06-02 |
20110130375 | NEW NO-RELEASING STEROIDS FOR THE TREATMENT OF RETINA AND MACULA LUTEA DISEASES - The invention relates to compounds of general formula (I) and pharmaceutically acceptable salts or stereoisomers thereof | 2011-06-02 |
20110130376 | NEW NO RELEASING STEROIDS DERIVATIVES - The invention relates to compounds of general formula (I) and pharmaceutically acceptable salts or stereoisomers thereof | 2011-06-02 |
20110130377 | SUBSTITUTED ARYLOXAZOLES AND THEIR USE - The present application relates to novel substituted aryloxazole derivatives, a method for the production thereof, the use thereof for the treatment and/or prophylaxis of diseases and the use thereof for the production of drugs for the treatment and/or prophylaxis of diseases, preferably for the treatment and/or prevention of cardiovascular and metabolic disorders. | 2011-06-02 |
20110130378 | EZETIMIBE PROCESS AND COMPOSITION - The present invention describes a process for producing ezetimibe (EZT) from a protected compound, including a step of deprotecting the 4-(p-hydroxyphenyl) protection group by catalytic hydrogenation, wherein the catalyst is used in an amount of 0.7 wt.-% or lower, relative to the weight of the compound used for the deprotection reaction. After carrying out a step of deprotection reaction, the process preferably comprises: (a) the reaction product is dissolved or extracted in ethyl acetate, and (b) the ethyl acetate solution is washed with an aqueous salt solution. The invention further describes a process for obtaining pure EZT, wherein raw EZT is dissolved in a solvent at a concentration of lower than 0.1 g/ml, and a crystallization step is carried out from this solution. These measures, respectively alone and particularly in combination contribute to attain ezetimibe (EZT) free of critical impurities described herein, and thus to use exceptionally pure ezetimibe (EZT) to be formulated into a pharmaceutical composition together with a pharmaceutically acceptable carrier or excipient. | 2011-06-02 |
20110130379 | PIPERAZINE DERIVATIVES USED AS CAV2.2 CALCIUM CHANNEL MODULATORS - The present invention relates to novel piperazine derivatives (I); to processes for their preparation; to pharmaceutical compositions containing the derivatives; and to the use of the derivatives in therapy to treat diseases for which blocking the Ca | 2011-06-02 |
20110130380 | Heteroaryl Kinase Inhibitors - The present invention provides compounds of Formula (I): | 2011-06-02 |
20110130381 | SMALL MOLECULE INHIBITORS OF PLASMODIUM FALCIPARUM DIHYDROOROTATE DEHYDROGENASE - Inhibitors of dihydroorotate dehydrogenase (DHODH) for the | 2011-06-02 |
20110130382 | MODULATORS OF 5-HT RECEPTORS AND METHODS OF USE THEREOF - The present application relates to 1,2,3,4,4a,5,6,7-octahydropyrazino[1,2-a][1,4]benzodiazepine, 1,2,3,4,4a,5,6,7-octahydropyrazino[1,2-a][1,5]benzodiazepine, 2,3,4,4a,5,6,7,11b-octahydro-1H-pyrido[3,4-d][2]benzazepine, 1,2,3,4,4a,5,6,7-octahydropyrazino[1,2-a][1]benzazepine, 1,2,3,4,4a,5-hexahydro-7H-pyrazino[1,2-a][4,1]benzoxazepine, and 2,3,4,4a,5,6-hexahydro-1H-pyrazino[2,1-d][1,5]benzoxazepine, and 5,6,7,7a,8,9,10,11-octahydropyrazino[1,2-d]pyrido[3,2-b][1,4]diazepine derivatives of formula (I) | 2011-06-02 |
20110130383 | Use of Ion Channel Modulators in the Prophylaxis and Treatment of Inflammatory and Immunological Diseases - Use of compounds of general formula (1) and pharmacologically acceptable salts and prodrugs thereof: Formula (1) wherein A and B are CH | 2011-06-02 |
20110130384 | AMIDE COMPOUND - The present invention aims to provide a prophylactic or therapeutic agent for schizophrenia and the like, containing the compound of the present invention having a GPR52 agonist activity. A compound represented by the following formula (I) or a salt thereof: | 2011-06-02 |
20110130385 | Bicyclic Heterocylic Derivatives and Methods of Use - The present invention relates to novel bicyclic heterocycle derivatives, pharmaceutical compositions comprising the bicyclic heterocycle derivatives and the use of these compounds for treating or preventing allergy, an allergy-induced airway response, congestion, a cardiovascular disease, an inflammatory disease, a gastrointestinal disorder, a neurological disorder, a metabolic disorder, obesity or an obesity-related disorder, diabetes, a diabetic complication, impaired glucose tolerance or impaired fasting glucose. R | 2011-06-02 |
20110130386 | DNA-PK INHIBITORS - A compound of formula (I) wherein: R1 and R2 are independently selected from hydrogen, an optionally substituted C | 2011-06-02 |
20110130387 | SIRTUIN MODULATING COMPOUNDS - Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent. | 2011-06-02 |
20110130388 | PROPHYLACTIC OR THERAPEUTIC AGENT FOR AXIAL MYOPIA - Since high myopia increases the risks of retinal detachment, myopic chorioretinal atrophy, myopic choroidal neovascularization, glaucoma, and cataract, establishment of prophylaxis against the progress of myopia is desired. However, at present, there is no effective prophylaxis or therapy for axial myopia, which is considered to cause high myopia. The present invention, which was completed based on the finding that Rho kinase inhibitors have an inhibitory action on axial length extension, provides a prominently effective prophylactic or therapeutic agent comprising a Rho kinase inhibitor as an active ingredient for axial myopia. | 2011-06-02 |
20110130389 | FUMARATE SALT OF 4-BROMOPHENYL 1,4-DIAZABICYCLO[3.2.2]NONANE-4-CARBOXYLATE, CRYSTALLINE FORMS THEREOF, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF - Fumarate salt of 4-bromophenyl 1,4-diazabicyclo[3.2.2]nonane-4-carboxylate, crystalline forms thereof, methods of preparation thereof, and therapeutic use thereof. | 2011-06-02 |
20110130390 | Use of COX-2 Inhibitors for the Treatment of Schizophrenia, Delusional Disorders, Affective Disorders, Autism or Tic Disorders - The invention concerns the use of a COX-2 inhibitor for the treatment of psychiatric disorders such as schizophrenia, delusional disorders, affective disorders, autism or tic disorders, in particular chronic schizophrenic psychoses and schizoaffective psychoses, temporary acute psychotic disorders, depressive episodes, recurring depressive episodes, manic episodes and bipolar affective disorders. Moreover, the invention is concerned with the use of a COX-2 inhibitor, in particular celecoxib, in combination with a neuroleptic drug, in particular risperidone, or an antidepressant, for the treatment of psychiatric disorders such as schizophrenia, delusional disorders, affective disorders, autism or tic disorders. | 2011-06-02 |
20110130391 | UREIDO SUBSTITUTED BENZOIC ACID COMPOUNDS AND THEIR USE FOR NONSENSE SUPPRESSION AND THE TREATMENT OF DISEASE - The invention encompasses ureido substituted benzoic acid compounds, compositions comprising the compounds and methods for treating or preventing diseases associated with nonsense mutations of mRNA by administering these compounds or compositions. | 2011-06-02 |
20110130392 | Method of Administering a Methylene Blue - Curcumin Analog for the Treatment of Alzheimer's Disease - A method of administering a methylene blue-curcumin hybrid useful in treating or preventing Alzheimer's Disease. | 2011-06-02 |
20110130393 | INHIBITORS OF JANUS KINASES - The instant invention provides for compounds that inhibit the four known mammalian JAK kinases (JAK1, JAK2, JAK3 and TYK2). The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting the activity of JAK1, JAK2, JAK3 and TYK2 by administering the compound to a patient in need of treatment for myeloproliferative disorders or cancer. | 2011-06-02 |
20110130394 | PHARMACEUTICAL COMPOUNDS - The invention provides kinase inhibitor compounds of the formula (1): | 2011-06-02 |
20110130395 | P13K ISOFORM SELECTIVE INHIBITORS - 2-Morpholin-4-yl-9H-purine and 5-Morpholin-4-yl-3H-[1,2,3]triazolo[4,5-d]pyrimidine derivatives, especially those substituted by 6-heteroaryl, are unexpected PI3 kinase isoform selective inhibitors with good drug properties and are useful in treating disorders related to abnormal PI3K activities such as cancer, immune disorders, cardiovascular disease, viral infection, inflammation, metabolism/endocrine disorders and neurological disorders. | 2011-06-02 |
20110130396 | IMIDAZOTHIADIAZOLE DERIVATIVES - Novel imidazo[2,1-b][1,3,4]thiadiazole derivatives of formula (I) | 2011-06-02 |
20110130397 | PYRROLINONE COMPOUNDS AS INHIBITORS OF BACTERIAL PEPTIDYL TRNA HYDROLASE AND USES THEREOF - Provided herein are compounds that modulate the activity of a bacterial peptidyl tRNA hydrolase, including compositions and dosage forms comprising the compounds. Further provided herein are methods for preventing or inhibiting bacterial proliferation as well as methods for preventing, treating, and/or managing a bacterial infection using such compounds and compositions. | 2011-06-02 |
20110130398 | SPIROINDOLINONE PYRROLIDINES - There are provided compounds of the formula | 2011-06-02 |
20110130399 | Phthalazine Derivatives with Angiogenesis Inhibiting Activity - The invention relates to new phthalazine derivatives of formula I, | 2011-06-02 |
20110130400 | TRPV4 ANTAGONISTS - The present invention relates to diazabicyclo[2.2.1]hept-2-yl analogs, pharmaceutical compositions containing them and their use as TRPV4 antagonists. | 2011-06-02 |
20110130401 | NEW CHEMICAL COMPOUNDS - Compounds of general formula (1) | 2011-06-02 |
20110130402 | HETEROAROMATIC GLUCOKINASE ACTIVATORS - The present invention describes 2,3-di-substituted N-heteroaromatic propionamides, wherein the substitution at the 3-position is an optionally substituted phenyl ring and the substitution at the 2-position is an alkyl or cycloalkyl group; pharmaceutical compositions comprising the same; and, methods of using the same. The propionamides are glucokinase activators which increase insulin secretion for the treatment of type II diabetes. | 2011-06-02 |
20110130403 | PYRAZOLO [3, 4-B] PYRIDINE DERIVATIVES AS PHOSPHODIESTERASE INHIBITORS - The present invention relates to phosphodiesterase (PDE) type 4, phosphodiesterase (PDE) type 7 and dual PDE type 4/PDE type 7 inhibitors. Compounds disclosed hereinf having the structure of Formula I: can be useful in the treatment, prevention, inhibition or suppression of CNS diseases, for example, multiple sclerosis; various pathological conditions such as diseases affecting the immune system, including AIDS, rejection of transplant, auto-immune disorders such as T-cell related diseases, for example, rheumatoid arthritis; inflammatory diseases such as respiratory inflammation diseases including chronic obstructive pulmonary disease (COPD), asthma, bronchitis, allergic rhinitis, adult respiratory distress syndrome (ARDS) and other inflammatory diseases including but not limited to psoriasis, shock, atopic dermatitis, eosinophilic granuloma, allergic conjunctivitis, osteoarthritis; gastrointestinal inflammation diseases such as Crohn's disease, colitis, pancreatitis as well as different types of cancers including leukaemia; especially in humans. Processes for the preparation of disclosed compounds, pharmaceutical compositions containing the disclosed compounds and their use as PDE type 4, PDE type 7 and dual PDE t e 4/PDE t e 7 inhibitors are rovided. | 2011-06-02 |
20110130404 | QUINOXALINEDIONE DERIVATIVES - The present invention relates to compounds of formula (I) | 2011-06-02 |
20110130405 | SUBSTITUTED QUINAZOLINES AS BLOOD PLATELET LOWERING AGENTS - This invention relates to the discovery of 3-and 5-substituted analogues of the selective platelet lowering agent anagrelide with reduced potential for cardiovascular side-effects which should lead to improved patient compliance and safety in the treatment of myeloproliferative diseases. More specifically, the present invention relates to certain imidazoquinazoline derivatives which have the general formula (I) shown below wherein the meanings of the substituents are defined in claim 1 and which have utility as platelet lowering agents in humans. The compounds of the present invention function by inhibiting megakaryocytopoeisis and hence the formation of blood platelets. | 2011-06-02 |
20110130406 | PYRAZOLO-PYRIDINES AS TYROSINE KINASE INHIBITORS - Compounds of Formulas Ia and Ib, and stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting receptor tyrosine kinases and for treating disorders mediated thereby. Methods of using compounds of Formula Ia and Ib, and stereoisomers, geometric isomers, tautomers, solvates and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed. | 2011-06-02 |
20110130407 | ISOQUINOLINONE DERIVATIVES AS NK3 ANTAGONISTS - Isoquinolone derivatives of the general formula I are provided. The compounds are NK3 antagonists and useful for the treatment of e.g. psychosis and schizophrenia. | 2011-06-02 |
20110130408 | PIPERAZIN-1-YL-TRIFLUOROMETHYL-SUBSTITUTED-PYRIDINES AS FAST DISSOCIATING DOPAMINE 2 RECEPTOR ANTAGONISTS - The present invention relates to piperazin-1-yl-trifluoromethyl-substituted-pyridines that are fast dissociating dopamine 2 receptor antagonists, processes for preparing these compounds, pharmaceutical compositions comprising these compounds as an active ingredient. The compounds find utility as medicines for treating or preventing central nervous system disorders, for example schizophrenia, by exerting an antipsychotic effect without motor side effects. | 2011-06-02 |
20110130409 | SUBSTITUTED 1,2,3,4-TETRAHYDROCYCLOPENTA[B]INDOL-3-YL)ACETIC ACID DERIVATIVES USEFUL IN THE TREATMENT OF AUTOIMMUNE AND INFLAMMATORY DISORDERS - The present invention relates to certain substituted 1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetic acid derivatives of Formula (Ia) and pharmaceutically acceptable salts thereof, which exhibit useful pharmacological properties, for example, as agonists of the S1P1 receptor. Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the treatment of S1P1 receptor-associated disorders, for example, psoriasis, rheumatoid arthritis, Crohn's disease, transplant rejection, multiple sclerosis, systemic lupus erythematosus, ulcerative colitis, type I diabetes, acne, microbial infections or diseases and viral infections or diseases. | 2011-06-02 |
20110130410 | PROCESS FOR PREPARING METHYL METHYLCARBAMATE AND ITS PURIFICATION FOR USE AS PHARMACEUTICALLY ACTIVE COMPOUND - The present invention relates to a process for preparing methyl {4,6-diamino-2-[1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]pyrimidin-5-yl}methylcarbamate of the formula (I) | 2011-06-02 |
20110130411 | PROCESS FOR PREPARING METHYL CARBAMATE AND ITS PURIFICATION FOR USE AS PHARMACEUTICALLY ACTIVE COMPOUND - The present invention relates to processes for preparing methyl {4,6-diamino-2-[1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]pyrimidin-5-yl}carbamate, i.e. the compound of the formula (I) | 2011-06-02 |
20110130412 | Acyclic amine inhibitors of nucleoside phosphorylases and hydrolases - The invention relates to compounds of the general formula (I) which are inhibitors of purine nucleoside phosphorylases (PNPs) and/or nucleoside hydrolases (NHs). The invention also relates to the use of these compounds in the treatment of diseases and infections including cancer, bacterial infections, protozoal infections, and T-cell mediated disease and to pharmaceutical compositions containing the compounds. | 2011-06-02 |
20110130413 | SUBSTITUTED QUINAZOLINES - This invention relates to the discovery of prodrugs of substituted analogues of the selective platelet lowering agent anagrelide which have reduced potential for cardiovascular side-effects and which should therefore lead to improved patient compliance and safety in the treatment of myeloproliferative diseases. More specifically, the present invention relates to prodrugs of certain imidazoquinazoline derivatives which have the general formula (I) shown below wherein the substituents have the meanings defined in claim | 2011-06-02 |
20110130414 | NOVEL FUSED THIAZOLO AND OXAZOLO PYRIMIDINONES - The present invention relates to novel compounds, their pharmaceutically acceptable salts, and their isomers, stereoisomers, conformers, tautomers, polymorphs, hydrates and solvates. The present invention also encompasses pharmaceutically acceptable compositions of said compounds and process for preparing novel compounds. The invention further relates to the use of the above-mentioned compounds for the preparation of medicament for use as pharmaceuticals. | 2011-06-02 |
20110130415 | PROTEIN KINASE C INHIBITORS AND USES THEREOF - This disclosure concerns compounds which are useful as inhibitors of protein kinase C (PKC) and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of PKC. This disclosure also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes. | 2011-06-02 |
20110130416 | PHARMACEUTICAL COMPOSITION FOR TREATING HYPERTENSION AND METABOLIC SYNDROME AND USE THEREOF - The present invention provides a pharmaceutical composition comprising the following active ingredients: 1) amlodipine or a pharmaceutically acceptable salt thereof, 2) pioglitazone or a pharmaceutically acceptable salt thereof, and 3) rosuvastatin or a pharmaceutically acceptable salt thereof. The present invention also provides use of the pharmaceutical composition in preparing a medicament for treating hypertension or metabolic syndrome. The pharmaceutical composition of the present invention can treat hypertension or metabolic syndrome, while effectively controlling the incidence of associated cardiovascular diseases and more potently improving survival prognosis in hypertensive patients. When blood pressure is lowered to desired level, the risk factors such as cardiovascular diseases are rectified, metabolic disorders and prognosis of patients are improved, and survival rate of hypertensive patients is raised. | 2011-06-02 |
20110130417 | NEW AZACYCLIC DERIVATIVES - Compounds of formula (I) | 2011-06-02 |
20110130418 | SUBSTITUTED PHENYLENEDIAMINES AS INHIBITORS OF THE INTERACTION BETWEEN MDM2 AND P53 - The present invention provides compounds of formula (I), their use as an inhibitor of a p53-MDM2 interaction as well as pharmaceutical compositions comprising said compounds of formula (I). | 2011-06-02 |
20110130419 | NOVEL SALT OF ISOQUINOLINE COMPOUND AND CRYSTAL THEREOF - The invention provides a salt of (R)-3-[2-(2-hydroxymethylpyrrolidin-1-yl)ethyl]-5-methyl-2H-isoquinolin-1-one and a crystal thereof. (R)-3-[2-(2-Hydroxymethylpyrrolidin-1-yl)ethyl]-5-methyl-2H-isoquinolin-1-one monophosphate is a compound which is chemically stable, has high solubility, and shows less weight change due to humidity as compared to a free form and monohydrochloride dihydrate, and is superior as a bulk drug for pharmaceutical products. | 2011-06-02 |
20110130420 | ISOQUINOLINONE DERIVATIVES AS NK3 ANTAGONISTS - Isoquinolone derivatives of the general formula Ik″ are provided. The compounds are NK3 antagonists and useful for the treatment of e.g. psychosis and schizophrenia. | 2011-06-02 |
20110130421 | Methods and Compositions for the Treatment of Chronic Renal Hypertension - Methods and compositions for the treating chronic renal hypertension in a subject comprising administering a therapeutically effective amount of at least one nitroxide-containing composition to the subject, particularly 4-hydroxy-2,2,6,6-tetramethyl-1-piperidine-1-oxyl (Tempol). | 2011-06-02 |
20110130422 | BIPHENYL COMPOUNDS USEFUL AS MUSCARINIC RECEPTOR ANTAGONISTS - This invention provides compounds of formula I: | 2011-06-02 |
20110130423 | Compounds Which Have Activity At M1 Receptor And Their Uses In Medicine - Compounds of formula (I) and salts thereof are provided: | 2011-06-02 |
20110130424 | SUBSTITUTED PHENYLPIPERIDINES WITH SEROTONINERGIC ACTIVITY AND ENHANCED THERAPEUTIC PROPERTIES - Chemical syntheses and medical uses of novel inhibitors of the uptake of monoamine neurotransmitters and pharmaceutically acceptable salts and prodrugs thereof, for the treatment and/or management of psychotropic disorders, anxiety disorder, generalized anxiety disorder, depression, post-traumatic stress disorder, obsessive-compulsive disorder, panic disorder, hot flashes, senile dementia, migraine, hepatopulmonary syndrome, chronic pain, nociceptive pain, neuropathic pain, painful diabetic retinopathy, bipolar depression, obstructive sleep apnea, psychiatric disorders, premenstrual dysphoric disorder, social phobia, social anxiety disorder, urinary incontinence, anorexia, bulimia nervosa, obesity, ischemia, head injury, calcium overload in brain cells, drug dependence, and/or premature ejaculation are described. | 2011-06-02 |
20110130426 | Novel Sulphonamide Derivatives as Glucocorticoid Receptor Modulators for the Treatment of Inflammatory Diseases - A compound of formula (I) or a pharmaceutically acceptable salt thereof; compositions comprising them, processes for preparing them and their use in medical therapy (for example modulating the glucocorticoid receptor in a warm blooded animal). | 2011-06-02 |
20110130427 | PESTICIDAL COMPOSITION - To improve the controlling effects of anthranilamide compounds against pests. A pesticidal composition comprising, as active ingredients, an anthranilamide compound or its salt, and a polyoxyalkylene phosphoric acid ester surfactant, and a method for controlling a pest by using such a composition, are provided. Further, a method for improving the pesticidal effects of an anthranilamide compound or its salt, as an active ingredient, by means of a polyoxyalkylene phosphoric acid ester surfactant, is provided. | 2011-06-02 |
20110130428 | Sublingual Compositions Comprising (2S) - (4E) -N-Methyl-5- (3- (5-Isopropoxypyridin) YL)-4-Penten-2-Amine - The present invention relates to sublingual compositions comprising (2S)-(4E)-N-methyl-5-(3-(5-iso-propoxypyridin)yl)-4-penten-2-amine or pharmaceutically acceptable salts thereof, to the preparation of said compositions and the use of thereof in therapy. | 2011-06-02 |
20110130429 | PYRIDINES FOR TREATING INJURED MAMMALIAN NERVE TISSUE - Embodiments of the present disclosure provide a novel pyridine, pharmaceutical compositions comprising such pyridine, and the use of such compositions in treating injured mammalian nerve tissue, including but not limited to an injured spinal cord. In at least one embodiment of the method, the method comprises the step of administering to the mammal in need thereof with a pharmaceutical composition, or pharmaceutically acceptable salt, comprising 4-aminopyridine-3-methanol. | 2011-06-02 |
20110130430 | Materials Having Embedded Insecticides And Additives - The present invention concerns polymeric material containing at least an embedded insecticidally active ingredient and an additive, which are released at room temperature. It similarly concerns materials produced from this polymer, for example in the form of self-supporting film/sheet, threads, wovens, fabrics, textiles, nets, curtains and pellets. The invention further concerns processes for producing such polymeric material and also the use of the self-supporting film/sheet, threads, wovens, fabrics, textiles and nets and curtains produced from the material for protecting humans, animals and plants and buildings, machines and packaging against arthropods, particularly for controlling insects. | 2011-06-02 |
20110130431 | Compounds Which Modulate The CB2 Receptor - Compounds of formula (I) | 2011-06-02 |
20110130432 | Heterocyclic Carboxamides For Use As Thrombin Inhibitors - This invention relates to novel pharmaceutically useful compounds of formula (I), in particular compounds that are competitive inhibitors of trypsin-like serine proteases, especially thrombin, their use as medicaments, pharmaceutical compositions containing them and synthetic routes to their production. Formula (I) | 2011-06-02 |
20110130433 | Hepatitis C Virus Inhibitors - This disclosure concerns novel compounds of Formula (I) as defined in the specification and compositions comprising such novel compounds. These compounds are useful antiviral agents, especially in inhibiting the function of the NS5A protein encoded by Hepatitis C virus (HCV). Thus, the disclosure also concerns a method of treating HCV related diseases or conditions by use of these novel compounds or a composition comprising such novel compounds. | 2011-06-02 |
20110130434 | MODIFIED RELEASE RAMIPRIL COMPOSITIONS AND USES THEREOF - The invention relates to a modified release pharmaceutical composition comprising ramipril or pharmaceutically acceptable salts thereof and pharmaceutically acceptable excipient(s) wherein pharmaceutical composition is bioequivalent to conventional immediate release formulation of ramipril administered twice daily. The invention further relates to a modified release pharmaceutical composition comprising: an immediate release component comprising ramipril or pharmaceutically acceptable salts thereof and a modified release component comprising ramipril or pharmaceutically acceptable salts thereof. The invention further relates to the process for the preparation of modified release pharmaceutical composition of ramipril. | 2011-06-02 |
20110130435 | TIME-RELEASED MEDICATION FOR APPLYING TO CRUSTACEAN OVARIAN DEVELOPMENT - A time-released medication for applying to crustacean ovarian development comprises a covering oil and a serotonin-related reagent. The covering oil is coated with the serotonin-related reagent and provides a sustainable releasing effect for the serotonin-related reagent. The serotonin-related reagent is selected from a group of serotonin, a precursor of serotonin, a derivative of serotonin and an agonist of serotonin. The coating relationship between the serotonin-related reagent and the covering oil makes them become a time-released medication. | 2011-06-02 |
20110130436 | CASPASE INHIBITORS AND USES THEREOF - This invention provides novel compounds, and pharmaceutically acceptable derivatives thereof, that are useful as caspase inhibitors. These compounds have the general formula I: | 2011-06-02 |
20110130437 | SALT FORMS OF A 6-FLUORO-1,2-DIHYDRO-2-OXO-3H-INDOL-3-YLIDENE DERIVATIVE, PROCESS FOR THEIR MANUFACTURE AND PHARMACEUTICAL COMPOSITIONS CONTAINING SAME - The present invention relates to salt forms of the compound 4-[(Z)-[[4-[(dimethylaminoJmethyllphenyllaminolCe-fluoro-1,2-dihydro2-oxo-3H-indol-3-ylidene)methyl]-benzenepropanoic acid which are suitable for pharmaceutical development and to a process for their manufacture. | 2011-06-02 |
20110130438 | ANILINE ANALOGS AS GLYCOGEN SYNTHASE ACTIVATORS - Provided herein are compounds of the formula (I): | 2011-06-02 |
20110130439 | CYCLOPENTANE HEPTAN(ENE)OIC ACID, 2-HETEROARYLALKENYL DERIVATIVES AS THERAPEUTIC AGENTS - A compound comprising | 2011-06-02 |
20110130440 | NON-NATURAL RIBONUCLEOTIDES, AND METHODS OF USE THEREOF - One aspect of the present invention relates to modified nucleosides and oligonucleotides comprising such modified nucleosides. Another aspect of the invention relates to a method of inhibiting the expression of a gene in call, the method comprising (a) contacting an oligonucleotide of the invention with the cell; and (b) maintaining the cell from step (a) for a time sufficient to obtain degradation of the mRNA of the target gene. | 2011-06-02 |
20110130441 | OLIGOMERIC COMPOUNDS HAVING AT LEAST ONE NEUTRALLY LINKED TERMINAL BICYCLIC NUCLEOSIDES - The present disclosure describes oligomeric compounds having at least one bicyclic nucleoside attached to the 3′ or 5′ termini by a neutral internucleoside linkage and methods of using the oligomeric compounds. In some embodiments, the oligomeric compounds provided herein hybridize to a portion of a target RNA resulting in loss of normal function of the target RNA. | 2011-06-02 |