35th week of 2012 patent applcation highlights part 43 |
Patent application number | Title | Published |
20120220533 | MODULATING NEUROMUSCULAR JUNCTION DENSITY CHANGES IN BOTULINUM-TOXIN TREATED TISSUE - A method may include administering botulinum toxin to a tissue of a patient and administering a neuropeptide of the CRF family to the tissue of the patient. In some examples, the botulinum toxin is periodically administered to the tissue of the patient and/or the neuropeptide of the CRF family is periodically administered to the tissue of the patient. The periods with which the botulinum toxin and the neuropeptide of the CRF family are administered may be the same or may be different. In some examples, the botulinum toxin and the neuropeptide of the CRF family are administered to the tissue at substantially the same time, while in other embodiments, the botulinum toxin and the neuropeptide of the CRF family are administered to the tissue at different times. | 2012-08-30 |
20120220534 | BIOMARKER FOR NEURODEGENERATION IN NEUROLOGICAL DISEASE - The present invention provides a method of detecting or diagnosing a neurodegenerative disease or condition in a subject. Further aspects of the invention provide a method of monitoring a subject over a period of time to detect the development or progress of a neurodegenerative disease or condition. Methods of treating, detecting or diagnosing a neurodegenerative disease or condition in a subject are also provided. | 2012-08-30 |
20120220535 | CYCLIC-GLUR6 ANALOGS, METHODS OF TREATMENT AND USE - A composition which is reversible inhibitor of at least one neuron-specific PDZ domain | 2012-08-30 |
20120220536 | USE OF ENDOSTATIN PEPTIDES FOR THE TREATMENT OF FIBROSIS - C-terminal endostatin polypeptides are disclosed herein. In some embodiments, these polypeptides include or consist of (1) at least at least 40 consecutive amino acids of the amino acid sequence set forth as amino acids 133-180 of SEQ ID NO: 2, SEQ ID NO: 13 or SEQ ID NO: 4; (2) at least 40 consecutive amino acids of the amino acid sequence set forth as amino acids 133-180 of SEQ ID NO: 2, SEQ ID NO: 13 or SEQ ID NO: 4 with at most 5 amino acid substitutions, (3) the amino acid sequence set forth as amino acids 133-180 of SEQ ID NO: 2, SEQ ID NO: 13 or SEQ ID NO: 4; or (4) the amino acid sequence set forth as amino acids 133-180 of SEQ ID NO: 2, SEQ ID NO: 13 or SEQ ID NO: 4 with at most 5 amino acid substitutions; wherein the polypeptide has anti-fibrotic activity and wherein the polypeptide does not comprise amino acids 1-92 of SEQ ID NO: 2, SEQ ID NO: 13 or SEQ ID NO: 4. Polynucleotides encoding these polypeptide, host cells transformed with the polynucleotides, and methods of using these polypeptides and polynucleotides are disclosed. Uses of these polypeptide, polynucleotides and expression vectors include the treatment of fibrosis in a subject. Thus, methods are provided for treating fibrosis, including fibrosis of the skin and/or the lung. | 2012-08-30 |
20120220537 | 9-AMINOACRIDINE DERIVATIVES, THEIR PREPARATION AND USES - N-substituted 9-aminoacridine and bis-acridino derivatives containing electron-withdrawing groups (EWG) or electron-donating groups (EDG), including amino acid residues, and one-pot methods for their synthesis are disclosed. The derivatives are potential candidates for cancer treatment. | 2012-08-30 |
20120220538 | LUNASIN-CONTAINING COMPLEX AND PURIFICATION OF LUNASIN FROM PLANTS - A method of purifying lunasin or a lunasin-containing complex produced in a plant includes providing a plant material from the plant, and isolating the lunasin-containing complex from the plant material, and/or releasing lunasin from the lunasin-containing complex. A composition for treating a cancer or an inflammation-related disease in a subject includes a lunasin-containing complex. A composition for treating a cancer or an inflammation-related disease in a subject includes a lunasin polypeptide and/or a lunasin-containing complex; and curcumin, wherein the combination of the a lunasin polypeptide or lunasin-containing complex and the curcumin has a synergistic effect. A method for treating a cancer or an inflammation-related disease includes administering a composition including a lunasin-containing complex, or a lunasin polypeptide and/or a lunasin-containing complex, and curcumin. | 2012-08-30 |
20120220539 | CONOTOXIN PEPTIDES - The present invention relates conotoxin peptides that are analogs of the α-contoxin peptide RgIA. These conotoxin peptides block the α9α10 subtype of the nicotinic acetylcholine receptor (nAChR) and can be used for treating pain, such as neuropathic pain and inflammatory pain, inflammatory disorders, such as rheumatic diseases, and in the treatment of breast cancer. | 2012-08-30 |
20120220540 | SYNBODIES TO AKT1 - The present application provides synbodies against AKT1 differing in amino acid sequence, conjugation chemistry, linker/scaffold, or adjunct moiety. The synbodies are useful for diagnosis and treatment of cancer and as research reagents. | 2012-08-30 |
20120220541 | USE OF YEAST PEPTIDE HYDROLYSATE AS AN ACTIVE AGENT FOR STRENGTHENING HAIR - The invention concerns the use of a composition comprising at least one yeast ( | 2012-08-30 |
20120220542 | PEGYLATED C-PEPTIDE - The present invention relates to modified forms of C-peptide, and methods for their use. In one aspect, the modified forms of C-peptide comprise PEGylated C-peptide derivatives comprising at least one PEG group attached to the N-terminus, which exhibit superior pharmacokinetic and biological activity in vivo. | 2012-08-30 |
20120220543 | Treatment of Glaucoma and Other Retinopathies with Gangliosides - A method of treating or preventing a retinopathy such as glaucoma in a human patient in need thereof comprising administering one or more gangliosides to the patient. | 2012-08-30 |
20120220544 | Ganglioside Transmucosal Formulations - A transmucosal formulation comprising a ganglioside and a mucosal absorption enhancer, as well as a method of treating or preventing Parkinson's disease in a human patient in need thereof comprising parenterally administering such a transmucosal formulation to said patient. | 2012-08-30 |
20120220545 | COUMARIN COMPOUNDS AS MELANOGENESIS MODIFIERS AND USES THEREOF - Provided are coumarin compounds of formula I, for example, robustic acid methyl ether, and the use of such compounds and compositions thereof to modulate (e.g., inhibit) melanogenesis and pigmentation. | 2012-08-30 |
20120220546 | COMPOSTIONS DESIGNED FOR THE INHIBITION AND/OR BLOCKING OF THE EPITHELIAL/MESENCHYMAL TRANSITION - 5′-methylthioadenosine (MTA) is described as a compound that is susceptible to inhibiting and/or blocking the epithelial-mesenchymal transition (EMT), a process whereby epithelial cells become mesenchymal cells. | 2012-08-30 |
20120220547 | FOOD FORMULATION COMPRISING GLYCOGEN - The present invention relates to a food formulation for the controlled release of glucose comprising glycogen and at least one other edible component, as well the use of glycogen for its preparation. | 2012-08-30 |
20120220548 | Compositions and methods for treatment of virus-associated cancer cells - Compositions, methods and kits are provided for treating a cancer, tumor or pre-cancerous tissue condition resistant to a chemotherapeutic agent, the tissue condition having one or more proteins or tumorigenesis markers induced by, upregulated by or otherwise associated with virus exposure. A marker may be a receptor for, or may operatively regulate production or use of hyuronan, for example by mediating a hyaluronan-associated signal path or affecting expression of a protein or signaling pathway of the diseased tissue. A treatment composition includes a competitor of hyaluronan interactions and further includes or is co-administered with a drug, e.g., a chemotherapy agent to which the virus-associated condition would be resistant absent the hyaluronan or competitor. | 2012-08-30 |
20120220549 | Pituitous Silicone Fluids - Fluid compositions are disclosed containing a branched organopolysiloxane and a carrier fluid. The branched organopolysiloxane is obtainable by reacting an organohydrogencyclosiloxane and an alkenyl terminated polydiorganosiloxane. The disclosed fluid compositions possess pituitous rheological properties. | 2012-08-30 |
20120220550 | PYRAZOLE DERIVATIVES, PREPARATION METHOD THEREOF, AND COMPOSITION FOR PREVENTION AND TREATMENT OF OSTEOPOROSIS CONTAINING SAME - The present invention provides pyrazole derivative compounds and pharmaceutically acceptable salts thereof. The compounds of the present invention have an excellent effect of preventing and treating osteoporosis. | 2012-08-30 |
20120220551 | PHOSPHORUS CONTAINING COMPOUNDS AS PROTEIN KINASE INHIBITORS - The present invention relates to compounds represented by formula (I), which can modulate the activity of protein kinases. The invention also relates to a composition containing a compound of formula (I), and a method for synthesizing and using such compound for preventing or treating ALK or cMet mediated disorders or conditions. | 2012-08-30 |
20120220552 | (THIO)MORPHOLINE DERIVATIVES AS S1P MODULATORS - The present disclosure relates to (thio)morpholine derivatives of the formula (I) | 2012-08-30 |
20120220553 | THE USE OF LPA FOR ENCOURAGING PREGNANCY, AND FERTILITY AGENT - The objective is to find compounds which have an activity to improve the success rate of pregnancy and implantation in blastocyst transfer in mammals, to provide a method of producing and using the compounds, and to provide a pregnancy-promoting agent. Disclosed is a pregnancy-promoting agent containing one or more lysophosphatidic acids selected from the group consisting of LPA-C16:0, LPA-C16:1, LPA-C18:0, LPA-C18:1 and LPA-C18:2. | 2012-08-30 |
20120220554 | Combretastatins for Prevention of Posterior Capsule Opacification - Methods and compositions for the treatment and prevention of posterior capsular opacification are provided. The method comprises administering a therapeutically effective amount of a combretastatin to a subject suffering from or at risk of developing posterior capsule opacification. | 2012-08-30 |
20120220555 | Methods of Simultaneously Treating Ocular Rosacea and Acne Rosacea - A method for simultaneously treating ocular rosacea and acne rosacea in a human in need thereof comprising administering systemically to said human a tetracycline compound in an amount that is effective to treat ocular rosacea and acne rosacea but has substantially no antibiotic activity. | 2012-08-30 |
20120220556 | DROSPIRENONE FOR HORMONE REPLACEMENT THERAPY - A pharmaceutical composition comprising as a first active ingredient an estrogen, such as estradiol or estradiol valerate, in sufficient amounts to treat disorders and symptoms associated with deficient endogenous levels of estrogen in women, and as a second active ingredient 6β,7β;15β;16β-dimethylene-3-oxo-17α-preg-4-ene-21,17-carbolactone (drospirenone, DRSP) in sufficient amounts to protect the endometrium from the adverse effects of estrogen is useful for, amongst others, treating peri-menopausal, menopausal and post-menopausal women. This composition may be used for hormone replacement therapy and may be administered as a multi-phased pharmaceutical preparation. This combination therapy may comprise continuous, sequential or interrupted administration, or combinations thereof, of DRSP and estrogen, each optionally in micronized form. | 2012-08-30 |
20120220557 | LIQUID PROPELLANT-FREE FORMULATION COMPRISING AN ANTIMUSCARINIC DRUG - Liquid, propellant-free pharmaceutical formulation for administration by nebulization which comprising an antimuscarinic drug as active ingredient are useful for the prevention and/or treatment of a wide range of conditions including respiratory disorders. | 2012-08-30 |
20120220558 | Methods of Treating Hormone-Related Conditions Using Thio-Oxindole Derivatives - The present invention provides methods of inducing contraception which includes delivering to a female a composition containing a compound of formula I, or tautomers thereof, in a regimen which involves delivering one or more of a selective estrogen receptor modulator, wherein formula I is: | 2012-08-30 |
20120220559 | Controlled Release and Taste Masking Oral Pharmaceutical Composition - Controlled release and taste masking compositions containing one or more active principles inglobated in a three-component matrix structure, i.e. a structure formed by successive amphiphilic, lipophilic or inert matrices and finally inglobated or dispersed in hydrophilic matrices. The use of a plurality of systems for the control of the dissolution of the active ingredient modulates the dissolution rate of the active ingredient in aqueous and/or biological fluids, thereby controlling the release kinetics in the gastrointestinal tract. | 2012-08-30 |
20120220560 | STEROID TETROL SOLID STATE FORMS - The invention relates to solid state forms of androst-5-ene-3β,7β,16α,17β-tetrol, formulations containing or prepared from such solid state forms and use of these materials for modulating unwanted inflammation including acute and chronic non-productive inflammation. The formulations can be used to prevent, treat or slow the progression of conditions related to autoimmunity and metabolic disorders such as arthritis, multiple sclerosis, ulcerative colitis, Type 1 diabetes and Type 2 diabetes. | 2012-08-30 |
20120220561 | OXADIAZOLE INHIBITORS OF LEUKOTRIENE PRODUCTION - The present invention relates to compound of formula (I): | 2012-08-30 |
20120220562 | Anti-Viral Compounds - Compounds effective in inhibiting replication of Hepatitis C virus (“HCV”) are described. This invention also relates to processes of making such compounds, compositions comprising such compounds, and methods of using such compounds to treat HCV infection. | 2012-08-30 |
20120220563 | Substituted piperidines - The invention relates to novel substituted piperidines, to processes for preparation thereof, to the use thereof for treatment and/or prophylaxis of diseases and to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases, especially of cardiovascular disorders and tumour disorders. | 2012-08-30 |
20120220564 | SELECTIVE CALCIUM CHANNEL MODULATORS - Methods and compounds effective in ameliorating conditions characterized by unwanted calcium channel activity, particularly unwanted T-type calcium channel activity are disclosed using a series of compounds containing N-acylated cyclic amines linked to an aπl ring as shown in formula (I). | 2012-08-30 |
20120220565 | PYRIDYL-AMINE FUSED AZADECALIN MODULATORS - The present invention provides a novel class of pyridyl-amine fused azadecalin compounds and methods of using the compounds as glucocorticoid receptor modulators. | 2012-08-30 |
20120220566 | Antimicrobial Compounds and Methods of Making and Using the Same - The present invention relates generally to the field of antimicrobial compounds and to methods of making and using them. These compounds are useful for treating, preventing, and reducing the risk of microbial infections in humans and animals. | 2012-08-30 |
20120220567 | BENZO-FUSED OXAZEPINE COMPOUNDS AS STEAROYL-COENZYME A DELTA-9 DESATURASE INHIBITORS - The present invention relates to certain 4,5-dihydro-3H-spiro[benzo[b]-[1,4]oxazepine compounds of the Formula (I) or a pharmaceutically acceptable salt thereof, wherein R | 2012-08-30 |
20120220568 | Histamine-3 Receptor Antagonists - This invention is directed to a compound of formula I, | 2012-08-30 |
20120220569 | FUSED HETEROCYCLIC RING DERIVATIVE AND USE THEREOF - The present invention provides a fused heterocycle derivative having a strong Smo inhibitory activity, and use thereof. | 2012-08-30 |
20120220570 | FUSED HETEROCYCLIC RING DERIVATIVE AND USE THEREOF - The present invention provides a fused heterocycle derivative having a strong Smo inhibitory activity, and use thereof. | 2012-08-30 |
20120220571 | HIV INTEGRASE INHIBITORS - Compounds of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: (I), wherein X is O or N(R3); and R1, R2, R3 and Y are defined herein. The compounds are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset or progression of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se (or as hydrates or solvates thereof) or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines. | 2012-08-30 |
20120220572 | TRICYCLIC INHIBITORS OF KINASES - The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, | 2012-08-30 |
20120220573 | Benzodiazepine Bromodomain Inhibitor - The present invention relates to a benzodiazepine compound of formula (I), processes for its preparation, pharmaceutical compositions containing such a compound and to its use in therapy. | 2012-08-30 |
20120220574 | METHODS OF UTILIZING ARYLPIPERAZINE DERIVATIVES - The present invention provides arylpiperazine derivatives which can be advantageously used for treating schizophrenia and related psychoses such as acute manic, bipolar disorder, autistic disorder, and depression. | 2012-08-30 |
20120220575 | N-SUBSTITUTED OXAZINOPTERIDINES AND OXAZINOPTERIDINONES - Disclosed are compounds of Formula 1, | 2012-08-30 |
20120220576 | Novel Heterocyclic Derivatives - The invention relates to novel heterocyclic compounds of the formula | 2012-08-30 |
20120220577 | GLYCINE B ANTAGONISTS - The invention relates to naphthalene derivatives as well as their pharmaceutically acceptable salts. The invention further relates to a process for the preparation of such compounds. The compounds of the invention are glycine B antagonists and are therefore useful for the control and prevention of various disorders, including neurological disorders. | 2012-08-30 |
20120220578 | GUM RESIN AS A CARRIER FOR TOPICAL APPLICATION OF PHARMACOLOGICALLY ACTIVE AGENTS - Described are pharmacological compositions comprising a gum resin; a pharmacologically active agent and a topically acceptable volatile solvent for the gum resin and active agent. Also described are methods for the transdermal or transmucosal delivery of a pharmacologically active agent using such compositions. | 2012-08-30 |
20120220579 | METHODS OF UTILIZING ARYLPIPERAZINE DERIVATIVES - The present invention provides arylpiperazine derivatives which can be advantageously used for treating schizophrenia and related psychoses such as acute manic, bipolar disorder, autistic disorder, and depression. | 2012-08-30 |
20120220580 | PREPARATION OF CAROTENOID DERIVATIVES AND THEIR APPLICATIONS - Compounds having the structure of general formula I or pharmaceutically acceptable salts thereof which are derivatives of fucoxanthin and fucoxanthol are disclosed. A preparation method of the compound and its use in weight reducing are also disclosed. | 2012-08-30 |
20120220581 | IMIDAZO[1,2-b]PYRIDAZINE DERIVATIVES AND THEIR USE AS PDE10 INHIBITORS - The present invention relates to novel imidazo[1,2-b]pyridazine derivatives which are inhibitors of the phosphodiesterase 10 enzyme (PDE10) and which are useful for the treatment or prevention of neurological, psychiatric and metabolic disorders in which the PDE10 enzyme is involved. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes to prepare such compounds and compositions, to the use of such compounds or pharmaceutical compositions for the prevention or treatment of neurological, psychiatric and metabolic disorders and diseases. | 2012-08-30 |
20120220582 | IMIDAZOPYRAZINE SYK INHIBITORS - Certain imidazopyrazines and pharmaceutical compositions thereof are provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are provided. Also provided are methods for determining the presence or absence of Syk kinase in a sample. | 2012-08-30 |
20120220583 | SUBSTITUTED HYDROXYETHYL AMINE COMPOUNDS AS BETA-SECRETASE MODULATORS AND METHODS OF USE - The present invention comprises a new class of compounds useful for the modulation of Beta-secretase activity and for the treatment of diseases, including Alzheimer's disease (AD) and related CNS conditions, mediated thereby. In one embodiment, the compounds have a general Formula I | 2012-08-30 |
20120220584 | HETEROCYCLIC COMPOUNDS AND METHODS OF USE - Heterocyclic compounds derived from benzotriazine, triazines, triazoles and oxadiazoles are disclosed. The methods of synthesis and of use of such heterocyclic compounds are also provided. | 2012-08-30 |
20120220585 | HETEROCYCLIC COMPOUNDS AND THEIR USES - Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110δ activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute Lymphoblastic leukaemia (T-ALL) B-cell Acute Lymphoblastic leukaemia (B-ALL) Non Hodgkins Lymphoma (NHL) B-cell lymphoma and solid tumors, such as breast cancer. | 2012-08-30 |
20120220586 | HETEROCYCLIC COMPOUNDS AND THEIR USES - Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110δ activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute Lymphoblastic leukaemia (T-ALL) B-cell Acute Lymphoblastic leukaemia (B-ALL) Non Hodgkins Lymphoma (NHL) B-cell lymphoma and solid tumors, such as breast cancer. | 2012-08-30 |
20120220587 | PYRIDINYLIMIDAZOLONE DERIVATIVES FOR THE INHIBITION OF PI3 KINASES - Compounds of the formula (I), in which X | 2012-08-30 |
20120220588 | QUINAZOLINE COMPOUNDS - Disclosed are compounds having the formula: wherein R | 2012-08-30 |
20120220589 | HETEROCYCLIC COMPOUNDS FOR THE INHIBITION OF PASK - Disclosed herein are new heterocyclic compounds and compositions and their application as pharmaceuticals for the treatment of disease. Methods of inhibiting PAS Kinase (PASK) activity in a human or animal subject are also provided for the treatment of diseases such as diabetes mellitus. | 2012-08-30 |
20120220590 | NOVEL COMPOUNDS AS MODULATORS OF GLUCOCORTICOID RECEPTORS - Compounds of formula (I) and pharmaceutical compositions containing them are described. The use of the compounds and compositions are also described. | 2012-08-30 |
20120220591 | PYRIMIDONE COMPOUNDS - A pyrimidone derivative represented by general formula (I) or a pharmaceutically acceptable salt thereof: | 2012-08-30 |
20120220592 | 2-PHENYLETHYLAMINO DERIVATIVES AS CALCIUM AND/OR SODIUM CHANNEL MODULATORS - 2-Phenylethylamino substituted carboxamide derivatives and their use as sodium and/or calcium channel modulators useful in preventing, alleviating and curing a wide range of pathologies are presented. | 2012-08-30 |
20120220593 | Substituted 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: | 2012-08-30 |
20120220594 | METHODS FOR TREATING CANCER IN PATIENTS HAVING IGF-1R INHIBITOR RESISTANCE - A method for treating cancer comprising identifying a mammal that overexpresses breast cancer resistance protein; and administering to said mammal a pharmaceutical composition comprising a therapeutically effective amount of ixabepilone. In one aspect, the mammal is not administered an agent that is susceptible to breast cancer resistance protein overexpression resistance. In another aspect, the cancer is a solid tumor. | 2012-08-30 |
20120220595 | Deuterated Tyrosine Kinase Inhibitors - Compounds of Formula I, as shown below and defined herein: enriched in deuterium, and pharmaceutically acceptable salts thereof, synthesis, intermediates, formulations, and methods of disease treatment therewith, including cancers mediated at least in part by IGF-1R and/or IR. | 2012-08-30 |
20120220596 | CYSTEINE AND CYSTINE PRODRUGS TO TREAT SCHIZOPHRENIA AND REDUCE DRUG CRAVINGS - The present invention provides cysteine and cystine prodrugs for the treatment of schizophrenia and drug addiction. The invention further encompasses pharmaceutical compositions containing prodrugs and methods of using the prodrugs and compositions for treatment of schizophrenia and drug addiction. | 2012-08-30 |
20120220597 | L-MALATE SALTS OF 6-(5-CHLORO-2-PYRIDYL)-5-[(4-METHYL-1-PIPERAZINYL)CARBONYLOXY]-7-OXO-6,7-- DIHYDRO-5H-PYRROLO[3,4-B]PYRAZINE - A novel L-malate salt of (6-(5-chloro-2-pyridyl)-5-[(4-methyl-1-piperazinyl)carbonyloxy]-7-oxo-6,7-dihydro-5H-pyrrolo[3,4-b]pyrazine) is provided. | 2012-08-30 |
20120220598 | Besylate Salts of 6-(5-Chloro-2-Pyridyl)-5-[(4 Methyl-1-Piperazinyl)Carbonyloxy]-7-oxo-6, 7-dihydro-5H-Pyrrolo[3,4-b]Pyrazine - A novel besylate salt of (6-(5-chloro-2-pyridyl)-5-[(4-methyl-1-piperazinyl)carbonyloxy]-7-oxo-6,7-dihydro-5H-pyrrolo[3,4-b]pyrazine) is provided. | 2012-08-30 |
20120220599 | AZA-BICYCLOALKYL ETHERS AND THEIR USE AS ALPHA7-NACHR AGONISTS - The present invention relates to 1-aza-bicycloalkyl derivatives of formula I, | 2012-08-30 |
20120220600 | N-Oxide of 3-(2,6-dichloro-3,5-dimethoxy-phenyl) -1--1-methyl-urea - An N-oxide of 3-(2,6-Dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea, pharmaceutically acceptable salts thereof, compositions including the compound and its pharmaceutically acceptable salts, and methods of preparing the compound and the compositions (such as, for example, by oxidizing 3-(2,6-Dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea with an oxidizing agent) are described. Further described herein are methods of using the compound and compositions of the present technology, alone and in combination with other suitable agents, to treat various diseases, including but not limited to, those that can be prevented, inhibited or ameliorated by inhibition of kinase activity selected from FGFR1, FGFR2, FGFR3 or FGFR4. | 2012-08-30 |
20120220602 | CYSTEINE PROTEASE INHIBITORS - Compounds of the formula II: | 2012-08-30 |
20120220603 | SUBSTITUTED HETEROCYCLIC DERIVATIVES FOR THE TREATMENT OF PAIN AND EPILEPSY - Compounds of formula (I) which are useful in ameliorating conditions characterized by unwanted sodium and/or calcium channel activity, particularly unwanted Na | 2012-08-30 |
20120220604 | PIPERAZINYL-ALKYL-BENZOIMIDAZOL-2-ONE DERIVATIVES AND THEIR USE AS MONOAMINE NEUROTRANSMITTER RE-UPTAKE INHIBITORS - The present application discloses novel piperazinyl-alkyl-benzoimidazol-2-one derivatives useful as monoamine neurotransmitter re-uptake inhibitors. In other aspects the invention discloses the use of these compounds in a method for therapy, and pharmaceutical compositions comprising the compounds of the invention. | 2012-08-30 |
20120220605 | OXOPIPERAZINE DERIVATIVES FOR THE TREATMENT OF PAIN AND EPILEPSY - Compounds of formula (I) which are useful in ameliorating conditions characterized by unwanted sodium and/or calcium channel actrvrh, particularly Na | 2012-08-30 |
20120220606 | NEW CAPPED PYRAZINOYLGUANIDINE SODIUM CHANNEL BLOCKERS - The present invention relates to sodium channel blockers. The present invention also includes a variety of methods of treatment using these inventive sodium channel blockers. | 2012-08-30 |
20120220607 | COMPOSITIONS AND METHODS FOR TREATMENT AND PREVENTION OF HYPERURICEMIA RELATED HEALTH CONSEQUENCES - Disclosed herein are methods of delaying the onset or treating diabetes that comprises administering a uric acid lowering agent. The inventors have made the remarkable discovery that elevated uric acid levels are not a corollary to insulin resistance, but rather a primary mediator of insulin resistance. Specifically exemplified are methods that involve administering to a patient susceptible to development of diabetes a composition comprising a uric acid lowering agent in a regimen that maintains serum uric acid levels below at least 5.5 mg/dl, or below at least 5.2 mg/dl. | 2012-08-30 |
20120220608 | METHOD OF PREVENTING AND TREATING HEPATIC DISEASE USING A2B ADENOSINE RECEPTOR ANTAGONISTS - The invention is related to methods of preventing and treating hepatic fibrosis using A | 2012-08-30 |
20120220609 | 5-HYDROXYPYRIMIDINE-4-CARBOXAMIDE DERIVATIVE - The present invention provides a compound which enhances the production of erythropoietin. The present invention provides a compound represented by formula (1): | 2012-08-30 |
20120220610 | INHIBITIONS OF GLUTAMINASE C - The present invention relates to a method of reducing the production of glutamate from glutamine by glutaminase C in a cell or tissue. The method involves inhibiting glutaminase C activity in the cell or tissue under conditions effective to reduce production of glutamate from glutamine. Compounds for carrying out this method are also disclosed. | 2012-08-30 |
20120220611 | 1,3-BENZOXAZOLYL DERIVATIVES AS KINASE INHIBITORS - Compounds of the formula I, the preparation and use thereof for the preparation of a medicament for the treatment of diseases, in particular tumours and/or diseases that are caused, mediated and/or propagated by angiogenesis. Compounds of the formula I are effective inhibitors of tyrosine kinases, in particular TIE-2 and VEGFR, and of Raf kinases. (I) | 2012-08-30 |
20120220612 | PHARMACEUTICAL COMPRISING PPAR AGONIST - An object of the present invention is to provide an agent for promoting proliferation of a meibomian gland epithelial cell and a corneal epithelial cell, as well as provide an agent for treating an ocular disease such as meibomian gland dysfunction or evaporative dry eye. | 2012-08-30 |
20120220613 | METHOD FOR DETERMINING SENSITIVITY TO AN ANTICANCER AGENT - To provide a marker for determining sensitivity of a patient to an anti-cancer agent, and novel cancer therapeutic means employing the marker. | 2012-08-30 |
20120220614 | SUBSTITUTED BIARYL DERIVATIVES AND METHODS OF USE THEREOF - The present invention relates to Substituted Biaryl Derivatives, compositions comprising a Substituted Biaryl Derivative, and methods of using the Substituted Biaryl Derivatives for treating or preventing obesity, diabetes, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of GPR119 in a patient. | 2012-08-30 |
20120220615 | SUBSTITUTED INDOLYL ALKYL AMINO DERIVATIVES AS NOVEL INHIBITORS OF HISTONE DEACETYLASE - This invention comprises the novel compounds of formula (I) | 2012-08-30 |
20120220616 | NOVEL SPIROPIPERIDINE COMPOUNDS - A compound of the formula: or a pharmaceutically acceptable salt thereof as well as a pharmaceutical composition, and a method for treating diabetes. | 2012-08-30 |
20120220617 | Fluorescent Perylene Derivatives for Direct Detection of Heparin - The invention relates to a perylene diimide derivative and to an in vitro method for preparing the same. In addition, the invention relates to a method for detecting heparin in a sample using perylene diimide derivatives, wherein the interaction of the perylene diimide derivative with heparin modulates the intensity of the fluorescent signal of the mixture compared to the solution. The invention also comprises a diagnostic kit for detecting heparin in a sample in vitro, comprising the perylene diimide derivative, as well as the use of the perylene diimide derivative for neutralizing the anticoagulant activity of heparin. | 2012-08-30 |
20120220618 | ANTICANCER AGENT SENSITIVITY-DETERMINING MARKER - To provide a marker for determining sensitivity of a patient to an anti-cancer agent, and novel cancer therapeutic means employing the marker. | 2012-08-30 |
20120220619 | Rapamycin Derivative or an Impdh Inhibitor for Treating Polycystic Kidney Disease - A method for treating polycystic kidney disease, comprising administering to a subject in need thereof a therapeutical effective amount of an inosine-5′-monophosphate dehydrogenase inhibitor or a rapamycin derivative. | 2012-08-30 |
20120220620 | Antitubercular alkaloid - A derivative of β-carboline alkaloid harmine, 10,12-diheptanoyl-11-hydroxy-3-methyl-β-carboline, prepared by a Friedel-Crafts acylation of harmine is reported as a novel potent antitubercular drug. | 2012-08-30 |
20120220621 | ANTI-CANCER COMPOUND AND PHARMACEUTICAL COMPOSITION CONTAINING THE SAME - The invention relates to a compound of formula (I), more specifically in the levorotatory form (1 | 2012-08-30 |
20120220622 | HETEROCYCLIC DERIVATIVES | 2012-08-30 |
20120220623 | THE ENANTIOMER OF TENATOPRAZOLE AND THE USE THEREOF IN THERAPY - This invention relates to optically active substances of tenatoprazole, (+) and (−)-5-methoxy-2-{(4-methoxy-3,5-dimethyl-2-pyridyl)methyl]sulfinyl}-1H-imidazo[4,5-b]pyridine. The compound and pharmaceutical compositions thereof are useful for anti-ulcer agent. | 2012-08-30 |
20120220624 | PYRAZOLO [3,4-B] PYRIDIN-4-ONE KINASE INHIBITORS - The present invention is directed to novel kinase inhibitors of general formula (I) and pharmaceutically acceptable salts thereof, and to the use of the kinase inhibitors of general formula (I) for treating diseases or disorders in which tau phosphorylation and cell cycle regulation is implicated, such as Alzheimer's Disease and cancer. | 2012-08-30 |
20120220625 | PHARMACEUTICAL COMPOSITION AND ADMINISTRATIONS THEREOF - The present invention relates to pharmaceutical compositions comprising a solid dispersion of N-[2,4-Bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide, methods of manufacturing pharmaceutical compositions of the present invention, and methods of administering pharmaceutical compositions of the present invention. | 2012-08-30 |
20120220626 | NOVEL QUINOLINE COMPOUND, AND COMPOSITION CONTAINING CENTIPEDE EXTRACT OR COMPOUNDS ISOLATED THEREFROM FOR PREVENTION AND TREATMENT OF CARDIOVASCULAR DISEASE - The present invention relates to a composition for the prevention and treatment of cardiovascular diseases containing the novel quinoline compound, the centipede extracts or compounds isolated from the extracts. The novel quinoline compound, the centipede extracts or a quinoline compound and a phenol compound isolated from the extracts of the invention exhibit excellent LDL-antioxidant activity, ACAT inhibiting activity, and anti-inflammatory activities, so that they can be included as an effective ingredient in a composition for the prevention and treatment of cardiovascular disease including hyperlipidemia, atherosclerosis, coronary heart disease, and myocardial infarction mediated by LDL-oxidation, cholesteryl ester synthesis and accumulation, and inflammation. | 2012-08-30 |
20120220627 | Substituted 2-amino-quinoline-3-carboxamides as KCNQ2/3 modulators - The invention relates to substituted 2-amino-quinoline-3-carboxamides, to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseases and/or disorders. | 2012-08-30 |
20120220628 | TABLETS COMPRISING A TASTE MASKING AGENT - The present invention is directed to a tablet comprising at least one bitter tasting and/or mucosa numbness causing pharmaceutically active compound; and at least one zinc salt. In addition, the present invention relates to the use of a zinc salt to reduce or mask the bitter taste of or the numbness of the mucosa caused by pharmaceutically active compounds. | 2012-08-30 |
20120220629 | ASYMMETRIC UREAS AND MEDICAL USES THEREOF - Disclosed are compounds, compositions and methods for the prevention and/or treatment of diseases which are pathophysiologically mediated by the ghrelin receptor. The compounds have the general formula (I): | 2012-08-30 |
20120220630 | PRUCALOPRIDE ORAL SOLUTION - The present invention is concerned with an oral aqueous solution comprising prucalopride or pharmaceutically acceptable acid addition salts thereof having good organoleptic properties. | 2012-08-30 |
20120220631 | USE OF 5H-THIOENO(3,4-c)PYRROLE-4,6-DIONE DERIVATIVES AS TUMOR NECROSIS FACTOR INHIBITOR - A method of treating or curing a disease caused by or associated with elevated levels of TNF in a patient including administering to the patient 5H-thioeno(3,4-c)pyrrole-4,6-dione derivatives. | 2012-08-30 |
20120220632 | Methods For Treatment of Fabry Disease - Provided are in vitro and in vivo methods for determining whether a patient with Fabry disease will respond to treatment with a specific pharmacological chaperone. | 2012-08-30 |
20120220633 | PIPERIDINE DERIVATIVES AS HUMAN PAPILLOMA VIRUS INHIBITORS - HPV inhibitors with formula (I) where G | 2012-08-30 |