Entries |
Document | Title | Date |
20080207643 | Composition for Treating Hyperlipaemia - The present invention provides a composition for treating hyperlipemia, which comprises the first active component acipimox, and the second active component atorvastatin, or the pharmaceutically acceptable salt, ester or solvate thereof. Weight ratio of the first to the second active component is (10-80):1. The composition is in the form of tablets, capsules, granules, pills or dropping pills. The combination of acipimox and atorvastatin is shown to have remarkably synergistic effect in decreasing serum total cholesterol, serum triglyceride and low density lipoprotein-cholesterol. Furthermore, in comparison with the combination of acipimox and pravastatin or the combination of acipimox and lorvastatin, the combination of acipimox and atorvastatin is shown to have more remarkable lipid decreasing effect, and have more advantageous effect of increasing high density lipoprotein-cholesterol. | 08-28-2008 |
20080207644 | Therapeutic materials and methods - Disclosed are methods for treating various cancers. Methods encompass the administration of an mTOR inhibitor in combination with a second drug selected from an ImiD, a PDE4 inhibitor, a p38 MAP kinase inhibitor, a xanthine anticytokine, a dual TACE/MMP inhibitor and a proteasome inhibitor. | 08-28-2008 |
20080221126 | Use of Hdac Inhibitors for the Treatment of Myeloma - The present invention relates to the use of an HDAC inhibitor, especially an HDAC inhibitor of formula I, | 09-11-2008 |
20080242680 | AGENT FOR THE PROPHYLAXIS OR TREATMENT OF NEURODEGENERATIVE DISEASE - The present invention provides a novel and useful agent for the prophylaxis or treatment of neurodegenerative diseases. Particularly, the present invention provides an agent for the prophylaxis or treatment of a neurodegenerative disease, which contains a compound represented by the following formula (I) as an active ingredient: | 10-02-2008 |
20080249109 | PYRAZINOYLGUANIDINE COMPOUNDS FOR USE AS TASTE MODULATORS - The present invention relates to blocking salt taste using compounds of Formula I as defined herein. | 10-09-2008 |
20080293740 | METHOD OF TREATING ACID-SENSING ION CHANNEL MEDIATED PAIN, COUGH SUPPRESSION, AND CENTRAL NERVOUS SYSTEM DISORDERS - The present invention provides a variety of methods of treatment of acid-sensing ion channel (ASIC) mediated pain, cough, and central nervous system disorders by ASICs inhibition with a series of pyrazinoylguanidine compounds represented by formula (I) as defined herein. | 11-27-2008 |
20080293741 | Tricyclo Substituted Amides as Glucokinase Modulators - Compounds of Formula (I): (I) or pharmaceutically acceptable salts thereof, are useful in the prophylactic and therapeutic treatment of hyperglycemia and diabetes. | 11-27-2008 |
20080293742 | Novel N-(Fluoro-Pyrazinyl)-Phenylsulfonamides as Modulators of Chemokine Receptor Ccr4 - The invention provides N-(fluoro-pyrazinyl)-phenylsulfonamides of formula (I) wherein R | 11-27-2008 |
20090018145 | Compositions and their use as anti-tumor agents - The present invention provides novel compounds and pharmaceutical compositions thereof, as well as methods for using the compounds and pharmaceutical compositions for treating tumors. Examples of specific tumor types that the compounds may be used to treat include, but are not limited to sarcomas, melanomas, neuroblastomas, carcinomas (including but not limited to lung, renal cell, ovarian, liver, bladder, and pancreating carcinomas) and mesotheliomas. | 01-15-2009 |
20090018146 | Combination Therapy with Triterpenoid Compounds and Proteasome Inhibitors - The present invention provides therapeutic compositions comprising a natural triterpenoid and a proteasome inhibitor. These compositions will be particularly useful in the treatment of malignancies and inflammation. The present invention also provides methods of treating a subject having a malignancy or an inflammatory disorder comprising administering to the subject a natural triterpenoid and a proteasome inhibitor. | 01-15-2009 |
20090023751 | COMPOUNDS THAT PROTECT AGAINST SENSORY HAIR CELL DEATH - The present invention provides methods of identifying compounds that protect against ototoxicity induced by one or more noxious stimuli, and methods of treating an individual with compounds identified using the present screening methods. Also provided are compounds demonstrated to have otoprotective effects. | 01-22-2009 |
20090062308 | METHODS OF USING SODIUM CHANNEL BLOCKERS - The present invention relates to use of a compound represented by formula (I): | 03-05-2009 |
20090062309 | Therapeutic compositions for the treatment of cardiovascular diseases and methods for use therefor - A pharmaceutical composition comprising an effective amount of at least one (a) an effective amount of at least one 3,5-diamino-6-chloro-N-(diaminomethylene) pyrazinecarboxamide monohydrochloride, dihydrate derivative comprising pirazinoylguanidine, benzamil, dichlorobenzamil, 5-(N,N-dimethyl)-Amiloride, 5-(N-ethyl-N-isopropyl)-Amiloride, (N,N-hexamethylene)-Amiloride, 5-(N-methyl-N-isobutyl)-Amiloride, and Amiloride citrate; (b) an effective amount of a calcium increasing agent; and (c) a pharmaceutically acceptable excipient. Methods are provided for treating a cardiovascular disease (CVD) in a patient diagnosed as having CVD or at risk for developing CVD, the method comprising administering to a subject in need of such treatment a therapeutically effective amount of at least one of 3,5-diamino-6-chloro-N-(diaminomethylene) pyrazinecarboxamide monohydrochloride, dihydrate and/or a derivative thereof. | 03-05-2009 |
20090076031 | DEUTERIUM-ENRICHED BORTEZOMIB - The present application describes deuterium-enriched bortezomib, pharmaceutically acceptable salt forms thereof, and methods of treating using the same. | 03-19-2009 |
20090076032 | Derivatives of 18Beta-Glycyrrhetinic Acid - The present invention relates to novel derivatives of 18β-glycyrrhetinic acid and methods of synthesising the derivatives. Also included within the scope of the present invention are pharmaceutical compositions comprising the derivatives of the present invention and medical uses of the derivatives, including their use in inhibiting enzymes such as retinol dehydrogenases. The present invention also relates to methods of treating diseases, such as hyperproliferative diseases, neoplasms, cancers and photoageing. | 03-19-2009 |
20090099204 | Amide derivative, insecticide containing the same and method for application thereof as insecticide - The present invention is to provide a compound represented by the general formula (1) exhibiting a high insecticidal effect and an insecticide comprising the compound as an active ingredient. | 04-16-2009 |
20090118306 | Novel use of liver X receptor agonists - The present invention generally relates to a novel therapeutical use of liver X receptor (LXR) agonsits. More specifically, the present invention relates to the use of LXR agonist for the preparation of a medicament useful for the treatment and/or the prevention of a disease associated with beta cells degeneration, such as diabetes, and a method for increasing ex vivo viability of pancreatic islet cells, comprising contacting said islet cells with a LXR agonist. | 05-07-2009 |
20090118307 | Aryl Sulfonamides - Compounds are provided that act as potent antagonists of the CCR9 receptor, and which have been further confirmed in animal testing for inflammation, one of the hallmark disease states for CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR9-mediated diseases, and as controls in assays for the identification of CCR9 antagonists. | 05-07-2009 |
20090156616 | THERAPEUTIC AGENTS - The present invention relates to compounds of formula (I) and processes for preparing such compounds, their use in the treatment of obesity, psychiatric and neurological disorders, to methods for their therapeutic use and to pharmaceutical compositions containing them. | 06-18-2009 |
20090170876 | Novel 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 | 07-02-2009 |
20090192172 | 2-Alkyl-Cycloalk(en)yl-Carboxamides - Novel 2-alkylcycloalk(en)ylcarboxamides of the formula (I) | 07-30-2009 |
20090192173 | ANTI-TUBERCULAR DRUGS: COMPOSITIONS AND METHODS - Methods and compositions for treating disease caused by infectious agents, particularly tuberculosis. In particular, methods and compositions comprising substituted ethylene diamines for the treatment of infectious diseases are provided. In one embodiment, these methods and compositions are used for the treatment of mycobacterial infections, including, but not limited to, tuberculosis. In certain embodiments, the present invention comprises compositions comprising novel substituted ethylene diamine compounds further comprising antitubercular agents such as rifampicin, isoniazid, pyrazinamide and ethambutol. | 07-30-2009 |
20090270420 | METHODS FOR INHIBITING CARDIAC PAI-1 - The invention relates to methods of inhibiting cardiac PAI-1 by administering a PAI-1 antagonist. | 10-29-2009 |
20090270421 | INHIBITORS OF FATTY ACID AMIDE HYDROLASE - Potent inhibitors of fatty acid amide hydrolase (FAAH) are constructed having K | 10-29-2009 |
20090286809 | Preventives or remedies for alzheimer's disease, or amyloid protein fibril-formation inhibitors, which include a nitrogen-containing heteroaryl compound - The present invention relates to preventives or remedies for Alzheimer's disease, or to amyloid protein fibril-formation inhibitors, which include as an active ingredient a compound of general formula (I) below or a pharmacologically permitted salt thereof; and also to nitrogen-containing heteroaryl derivatives having specific substituents, or pharmacologically permitted salts thereof, which are valuable as preventives or remedies for Alzheimer's disease, or as amyloid protein fibril-formation inhibitors: | 11-19-2009 |
20090298853 | Carbamoyl Compounds as DGAT1 Inhibitors 190 - DGAT-1 inhibitor compounds of formula (I), pharmaceutically-acceptable salts and pro-drugs thereof are described, together with pharmaceutical compositions, processes for making them and their use in treating, for example, obesity | 12-03-2009 |
20090312348 | USE OF SODIUM BLOCKERS FOR AN EARLY THERAPY OF OBSTRUCTIVE LUNG DISEASES - The present invention relates to a blocker of sodium channels in cell membranes, particularly in membranes of epithelial cells of organs belonging to the respiratory tract to be used as the pharmaceutically active ingredient in a medicament for treating an obstructive lung disease in a patient. | 12-17-2009 |
20090318473 | 5,6-BISARYL-2-PYRIDINE-CARBOXAMIDE DERIVATIVES, PREPARATION AND APPLICATION THEREOF IN THERAPEUTICS AS UROTENSIN II RECEPTOR ANTAGONISTS - The present invention relates to derivatives of 5,6-bisaryl-2-pyridine-carboxamide, their preparation and their application in therapeutics as antagonists of urotensin II receptors. | 12-24-2009 |
20100010012 | GLUTAMATE AGGRECANASE INHIBITORS - The present invention relates to modulators of metalloproteinase activity. | 01-14-2010 |
20100056546 | SULFONYLUREA INHIBITORS OF ATP-SENSITIVE POTASSIUM CHANNELS - The present invention relates to new sulfonylurea inhibitors of ATP-sensitive potassium channels, pharmaceutical compositions thereof, and methods of use thereof. | 03-04-2010 |
20100087447 | PHARMACEUTICAL COMPOSITION COMPRISING PYRAZINE DERIVATIVE, AND METHOD OF USING PYRAZINE DERIVATIVE IN COMBINATION - Disclosed is a pharmaceutical composition comprising a pyrazine derivative represented by the general formula: | 04-08-2010 |
20100144759 | NOVEL N-(FLUORO-PYRAZINYL)-PHENYLSULFONAMIDES AS MODULATORS OF CHEMOKINE RECEPTOR CCR4 - The invention provides N-(fluoro-pyrazinyl)-phenylsulfonamides of formula (I) | 06-10-2010 |
20100152204 | TREATMENT FOR SPINAL MUSCULAR ATROPHY - A method of treating spinal muscular atrophy. The method includes administering an effective amount of composition including a sodium-proton exchanger inhibitor and a pharmaceutically acceptable carrier or salt, to a subject with spinal muscular atrophy to ameliorate a symptom of spinal muscular atrophy. | 06-17-2010 |
20100160343 | HETEROARYL, HETEROCYCLIC AND ARYL COMPOUNDS WHICH INHIBIT LEUKOCYTE ADHESION MEDIATED BY VLA-4 - Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis. | 06-24-2010 |
20100168133 | USE OF SUBSTITUTED QUINOLINE DERIVATIVES FOR THE TREATMENT OF DRUG RESISTANT MYCOBACTERIAL DISEASES - The present invention relates to the use of a substituted quinoline derivative for the preparation of a medicament for the treatment of an infection with a drug resistant | 07-01-2010 |
20100261735 | FUNGICIDAL COMPOSITION CONTAINING ACID AMIDE DERIVATIVE - Conventional many fungicidal compositions have had practical problems such that either a preventive effect or a curing effect is inadequate, the residual effect tends to be inadequate, or the controlling effect against plant diseases tends to be inadequate depending upon the application site, and a fungicidal composition to overcome such problems has been desired. The present invention provides a fungicidal composition containing an acid amide derivative of the formula (I) or a salt thereof, as an active ingredient: | 10-14-2010 |
20100267746 | ALIPHATIC PYRAZINOYLGUANIDINE SODIUM CHANNEL BLOCKERS WITH BETA AGONIST ACTIVITY - The present invention provides sodium channel blockers possessing beta-adrenergic receptor agonist activity. | 10-21-2010 |
20100324071 | NOVEL GLUCOKINASE ACTIVATORS AND METHODS OF USING SAME - Compounds are provided which are activators of the enzyme glucokinase and thus are useful in treating diabetes and related diseases, which compounds have the structure | 12-23-2010 |
20110003832 | 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. | 01-06-2011 |
20110009426 | 5,6-BISARYL-2-PYRIDINE-CARBOXAMIDE DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC APPLICATION THEREOF AS UROTENSIN II RECEPTOR ANTAGONISTS - The present invention relates to 5,6-bisaryl-2-pyridinecarboxamides, to their preparation and to their therapeutic use as urotensin II receptor antagonists. | 01-13-2011 |
20110015211 | FIBROSIS INHIBITOR - [Object] The main object of the present invention is to provide a fibrosis inhibitor. | 01-20-2011 |
20110053958 | MODULATORS OF THE PROSTACYCLIN (PGI2) RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO - The present invention relates to amide derivatives of Formula (XIIIa) and pharmaceutical compositions thereof that modulate the activity of the PGI2 receptor. Compounds of the present invention and pharmaceutical compositions thereof are directed to methods useful in the treatment of: pulmonary arterial hypertension (PAH); idiopathic PAH; familial PAH; PAH associated with a collagen vascular disease, a congenital heart disease, portal hypertension, HIV infection, ingestion of a drug or toxin, hereditary hemorrhagic telangiectasia, splenectomy, pulmonary veno-occlusive disease (PVOD) or pulmonary capillary hemangiomatosis (PCH); PAH with significant venous or capillary involvement; platelet aggregation; coronary artery disease; myocardial infarction; transient ischemic attack; angina; stroke; ischemia-reperfusion injury; restenosis; atrial fibrillation; blood clot formation in an angioplasty or coronary bypass surgery individual or in an individual suffering from atrial fibrillation; atherosclerosis; atherothrombosis; asthma or a symptom thereof; a diabetic-related disorder such as diabetic peripheral neuropathy, diabetic nephropathy or diabetic retinopathy; glaucoma or other disease of the eye with abnormal intraocular pressure; hypertension; inflammation; psoriasis; psoriatic arthritis; rheumatoid arthritis; Crohn's disease; transplant rejection; multiple sclerosis; systemic lupus erythematosus (SLE); ulcerative colitis; ischemia-reperfusion injury; restenosis; atherosclerosis; acne; type 1 diabetes; type 2 diabetes; sepsis; and chronic obstructive pulmonary disorder (COPD). | 03-03-2011 |
20110071164 | ERG CHANNEL OPENERS FOR THE TREATMENT OF CARDIAC ARRHYTHMIAS - This invention relates to the use of ERG channel openers for the treatment of cardiac arrhythmias, and to the use of specific compounds for such treatment. In a separate aspect the invention provides novel compounds useful as ERG channel openers. | 03-24-2011 |
20110082156 | FATTY ACID ACIPIMOX DERIVATIVES AND THEIR USES - The invention relates to fatty acid acipimox derivatives; compositions comprising an effective amount of a fatty acid acipimox derivative; and methods for treating or preventing an metabolic disease comprising the administration of an effective amount of a fatty acid acipimox derivative. | 04-07-2011 |
20110105531 | COMPOSITIONS AND METHODS FOR IDENTIFICATION OF SUBSPECIES CHARACTERISTICS OF MYCOBACTERIUM TUBERCULOSIS - The present invention provides compositions, kits and methods for rapid genotyping of strains of | 05-05-2011 |
20110105532 | Haloalkyl-substituted amides as insecticides and acaricides - The present invention relates to halogen-substituted amide derivatives of the general formula (I) | 05-05-2011 |
20110112114 | INHIBITORS OF SERINE PROTEASES, PARTICULARLY HEPATITIS C VIRUS NS3 PROTEASE - The present invention relates to compounds, methods and pharmaceutical compositions for inhibiting proteases, particularly serine proteases, and more particularly HCV NS3 proteases. The compounds, and the compositions and methods that utilize them, can be used, either alone or in combination to inhibit viruses, particularly HCV virus. | 05-12-2011 |
20110136831 | N-2-(Hetero)Arylethylcarboxamide Derivative, and Pest-Controlling Agent Comprising the Same - An N-2-(hetero)arylethylcarboxamide derivative represented by the formula (I) | 06-09-2011 |
20110136832 | Promoting Cycling of ApoE4 Isoform - Cycling of ApoE4 isoform is promoted in a person in need thereof by contacting the person with an effective amount of a pharmaceutically-acceptable modulator of intracellular ApoE4 transport vesicle pH. | 06-09-2011 |
20110166161 | HETEROCYCLIC CARBOXAMIDE COMPOUNDS - This invention relates to novel heterocyclic carboxamide derivatives and salts thereof. More particularly, it relates to novel heterocyclic carboxamide derivatives and salts thereof which act as a ROCK inhibitor, to a pharmaceutical composition comprising the same and to a method of using the same therapeutically in the treatment and/or prevention of ROCK-related disease. | 07-07-2011 |
20110178102 | SIR2 REGULATION - Compounds are disclosed which inhibit SIR2 base exchange more than deacetylation, thus enhancing SIR2 deacetylation activity. Methods of using the compounds for enhancing SIR2 deacetylation activity and increasing longevity of an organism are also disclosed. Methods for screening for compounds that enhance SIR2 deacetylation activity and increase longevity of an organism are additionally disclosed. | 07-21-2011 |
20110178103 | THERAPEUTIC AGENT FOR CHRONIC RENAL FAILURE - The present invention aims to provide a therapeutic agent for chronic renal failure, comprising as an effective ingredient a compound represented by General Formula (1) or a pharmaceutically acceptable salt thereof. That is, the present invention provides provision of a drug comprising as an effective ingredient a compound represented by General Formula (1) or a pharmaceutically acceptable salt thereof, which drug is useful not only for amelioration of renal function, but also for amelioration of anemia, activation of SOD and excretion of uremic substances. | 07-21-2011 |
20110183998 | HETEROCYCLIC COMPOUNDS, PROCESSES FOR THEIR PREPARATION, MEDICAMENTS COMPRISING THESE COMPOUNDS, AND THE USE THEREOF - Heterocyclic derivatives, processes for their preparation, medicaments comprising these compounds, and the use thereof. The invention relates to compounds of the formula I in which the radicals R1, R2, R3, R4, W, A, B, D, E, G, L, M, R, T and Y have the stated meanings, and to the physiologically tolerated salts thereof. The compounds are suitable for example for the treatment of the metabolic syndrome, insulin resistance, obesity and diabetes. | 07-28-2011 |
20110195979 | COMPOUNDS FOR THE TREATMENT AND PREVENTION OF INFLUENZA - A compound of formula (I) | 08-11-2011 |
20110218208 | 2-HETEROCYCLYLAMINOALKYL-(P-QUINONE) DERIVATIVES FOR TREATMENT OF OXIDATIVE STRESS DISEASES - Methods of treating or suppressing oxidative stress disorders including mitochondrial diseases, impaired energy processing disorders, neurodegenerative diseases and diseases of aging are disclosed, as well as compounds useful in the methods of the invention, such as 2-heterocyclylaminoalkyl-(p-quinone) derivatives. | 09-08-2011 |
20110218209 | NUTRIENT DELIEVRY DRUG COMPOSITION - The present invention is a hypoallergenic nutrient delivery drug composition, that includes an active drug, a binder with non-genetically engineered and non-chemically treated starches and food powders, a filler with non-genetically engineered and non-chemically treated vegetable powder and/or extracts and a non-genetically engineered and non-chemically treated fruit powder and/or extract and a preservative that includes non-genetically engineered and non-chemically treated fruit juice, fruit oil and vitamins. There is also a sustained nutrient drug delivery composition that includes non-genetically engineered and non-chemically treated oils, starches and vegetable powders and/or extracts and fruit powder and/or extracts. There is also a broad spectrum nutrient delivery drug composition that includes non-genetically engineered and non-chemically treated pepper and oil mixtures or extracts. | 09-08-2011 |
20110230501 | PHARMACEUTICAL COMPOSITIONS FOR THE TREATMENT OF DIABETES MELLITUS - Disclosed herein is a pharmaceutical composition comprising Hydroxychloroquine or its pharmaceutically acceptable salt and at least one antidiabetic compound, useful in the treatment of diabetes mellitus. | 09-22-2011 |
20110301178 | PYRAZINYL CARBOXAMIDES AS FUNGICIDES - This present disclosure is related to the field of pyrazine carboxamides and their derivatives and the use of these compounds as fungicides. | 12-08-2011 |
20110301179 | NAPHTHAMIDES AS ANTICANCER AGENTS - A compound (particularly useful for inhibiting cancer) according to formula I: | 12-08-2011 |
20110319427 | USE OF 5AHQ AND BORTEZOMIB FOR THE TREATMENT OF HEMATOLOGICAL DISEASES - The disclosure provides methods and compositions for treating hematological malignancies. In particular, the disclosure provides methods and compositions for treating leukemia, lymphoma and multiple myeloma using bortezomit and 5AHQ (5-ammo-8-hydroxyqumolme) and related compounds that bind non-competitively to an alpha unit of 2OS proteasome and inhibit proteasome activity Kits and commercial packages are also disclosed | 12-29-2011 |
20120010221 | TABLET AND GRANULATED POWDER CONTAINING 6-FLUORO-3-HYDROXY-2-PYRAZINECARBOXAMIDE - Disclosed is a useful tablet which contains a high quantity of 6-fluoro-3-hydroxy-2-pyrazinecarboxamide or a salt thereof; has a size that is easy to ingest; has superior release characteristics; and has a hardness that can withstand film coating, packaging, and transportation. | 01-12-2012 |
20120065214 | COMPOUNDS AND THEIR USES 708 - The present invention relates to pyrazinone derivatives of formula (I): | 03-15-2012 |
20120108611 | 5, 6-BISARYL-2-PYRIDINE-CARBOXAMIDE DERIVATIVES, PREPARATION AND APPLICATION THEREOF IN THERAPEUTICS AS UROTENSIN II RECEPTOR ANTAGONISTS - The present invention relates to derivatives of 5,6-bisaryl-2-pyridine-carboxamide, their preparation and their application in therapeutics as antagonists of urotensin II receptors. | 05-03-2012 |
20120149718 | Amido Compounds - Compounds of the formula I: | 06-14-2012 |
20120157476 | OXIME COMPOUNDS - The present invention relates to compounds of the formula | 06-21-2012 |
20120165343 | Glucagon Receptor Modulators - The present invention provides a compound of Formula (I) | 06-28-2012 |
20120178765 | NOVEL GLUCOKINASE ACTIVATORS AND PROCESSES FOR THE PREPARATION THEREOF - The present invention provides an amide derivative having a stilbene or 1,2-diphenylethane moiety within the molecule thereof, a process for the preparation thereof, and a pharmaceutical composition comprising the same. The amide derivative of the present invention activates glucokinase remarkably, and therefore they can be usefully applied for treating glucokinase-mediated diseases, such as hyperglycemia and diabetes. | 07-12-2012 |
20120190693 | Reverse Amide Compounds As Protein Deacetylase Inhibitors And Methods Of Use Thereof - The present invention relates to novel “reverse amide” compounds comprising a zinc chelator group, and the use of such compounds in the inhibition of HDAC6 and in the treatment of various diseases, disorders or conditions related to HDAC6. | 07-26-2012 |
20120214821 | Lipidomic Biomarkers of Diabetes - The invention, in some aspects, relates to methods for predicting a subject's risk of developing a glucose-related metabolic disorder, e.g., diabetes. In some aspects, the invention relates to methods for selecting and monitoring a treatment for a glucose-related metabolic disorder, e.g., diabetes. | 08-23-2012 |
20120214822 | N-CYCLOPROPYL-3-FLUORO-5-[3-[[1-[2-[2- [(2-HYDROXETHYL)AMINO] ETHOXY]PHENYL] CYCLOPROPYL] AMINO]-2-OXO- 1 (2H)-PYRAZINYL]-4-METHYL-BENZAMIDE, OR PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF AND THEIR USES - The present invention relates to pyrazinone derivatives of formula (I): | 08-23-2012 |
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. | 08-30-2012 |
20130005742 | Substituted Diphenylpyrazine Derivatives - This invention relates to novel substituted diphenylpyrazines and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a PGI | 01-03-2013 |
20130012523 | PYRAZINONE DERIVATIVES, PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF AND THEIR USES - The present invention relates to pyrazinone derivatives of formula (I): | 01-10-2013 |
20130172367 | 2-Alkyl-Cycloalk(en)yl-Carboxamides | 07-04-2013 |
20130178482 | 3,5-DIAMINO-6-CHLORO-N-(N-(4-(4-(2-(HEXYL(2,3,4,5,6-PENTAHYDROXYHEXYL)AMIN- O)ETHOXY)PHENYL)BUTYL) CARBAMIMIDOYL)PYRAZINE-2-CARBOXAMIDE - The present invention relates to the compound of the formula: | 07-11-2013 |
20130184293 | COMPOSITIONS AND METHODS FOR TREATING DIABETES AND NEUROPSYCHOLOGICAL DYSFUNCTION - The present invention relates to compositions and methods for treating diabetes mellitus, neuropsychological and neurological disorders in a particular group of patient. More specifically, the invention relates to methods of treating diabetes mellitus, neuropsychological and neurological disorders in patients having defective potassium channels. The invention may be used in human subjects, particularly adults or children, and is appropriate to treat various neurological disorders. | 07-18-2013 |
20130217706 | MODULATORS OF THE PROSTACYCLIN (PGI2) RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO - The present invention relates to amide derivatives of Formula (XIIIa) and pharmaceutical compositions thereof that modulate the activity of the PGI2 receptor. Compounds of the present invention and pharmaceutical compositions thereof are directed to methods useful in the treatment of: pulmonary arterial hypertension (PAH); idiopathic PAH; familial PAH; PAH associated with a collagen vascular disease; and other diseases. | 08-22-2013 |
20130217707 | TREATING ATTENTION DEFICIT HYPERACTIVITY DISORDER WITH NHE INHIBITORS - The present invention relates to a method of treating attention deficit hyperactivity disorder in a subject. This method includes selecting a subject with attention deficit hyperactivity disorder and administering to the selected subject a sodium/hydrogen exchanger inhibitor under conditions effective to treat the subject for attention deficit hyperactivity disorder. Methods of identifying compounds suitable to treat attention deficit hyperactivity disorder are also disclosed. | 08-22-2013 |
20130217708 | MEGLUMINE SALT OF 6-FLUORO-3-HYDROXY-2-PYRAZINE CARBOXAMIDE - A preparation replete with a meglumine salt of 6-fluoro-3-hydroxy-2-pyrazine carboxamide has superior solubility, and is useful as a preparation for injection. | 08-22-2013 |
20130231351 | SIR2 REGULATION - Compounds are disclosed which inhibit SIR2 base exchange more than deacetylation, thus enhancing SIR2 deacetylation activity. Methods of using the compounds for enhancing SIR2 deacetylation activity and increasing longevity of an organism are also disclosed. Methods for screening for compounds that enhance SIR2 deacetylation activity and increase longevity of an organism are additionally disclosed. | 09-05-2013 |
20130252974 | 5,6-BISARYL-2-PYRIDINE-CARBOXAMIDE DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC APPLICATION THEREOF AS UROTENSIN II RECEPTOR ANTAGONISTS - The present invention relates to 5,6-bisaryl-2-pyridinecarboxamides, to their preparation and to their therapeutic use as urotensin II receptor antagonists. | 09-26-2013 |
20130261133 | Therapeutic Compounds for Protozoal and Microbial Infections and Cancer - The compounds of the invention exhibit antiprotozoal, antimicrobial, and anticancer properties that are useful for the treatment or prevention of infections or cancer in a patient (e.g., a human). For example, the compounds and methods described herein can be used for the treatment or prevention of protozoal infections such as leishmaniasis, malaria, and | 10-03-2013 |
20130281464 | BIGUANIDE DERIVATIVE COMPOUND - Provided is a novel compound which simultaneously inhibits both NMDA receptors and ASIC1a, which are associated with neurodegenerative disease and so on, and thus is useful for the prevention and treatment of various nervous system diseases. A biguanide derivative represented by the following general formula (1), a salt thereof, or a hydrate of the derivative or the salt: | 10-24-2013 |
20130303548 | INDICATION FOR USE OF NIACIN (NICOTINIC ACID) FOR TREATMENT, PREVENTION AND REVERSAL OF FATTY LIVER DISEASE - Niacin prevents and/or reverses the development of experimental hepatic steatosis, deposition of triglycerides in liver and serum of individuals, deposition of total cholesterol in liver and serum in individuals, and inhibit liver lipid peroxidation and oxidative stress in individuals at risk of developing fatty liver disease or NAFLD. In cultured human hepatocytes, niacin inhibits alcohol-induced fat accumulation. | 11-14-2013 |
20130324559 | DENDRIMER LIKE AMINO AMIDES POSSESSING SODIUM CHANNEL BLOCKER ACTIVITY FOR THE TREATMENT OF DRY EYE AND OTHER MUCOSAL DISEASES - Sodium channel blockers represented by the formula: | 12-05-2013 |
20140011817 | COMPOSITION FOR REDUCING NERVOUS SYSTEM INJURY AND METHOD OF MAKING AND USE THEREOF - This application discloses a composition comprising an amiloride and/or an amiloride analog which can be used for reducing nerve injury or nervous system injury in a subject. The formulation of such composition is also disclosed. The application further directs to methods for treating nerve injury or nervous system injury by administering to the subject a therapeutically effective amount of a pharmaceutical composition comprising amiloride, an amiloride analog or a pharmaceutically acceptable salt thereof. | 01-09-2014 |
20140031372 | CICLETANINE IN COMBINATION WITH ORAL ANTIDIABETIC AND/OR BLOOD LIPID-LOWERING AGENTS AS A COMBINATION THERAPY FOR DIABETES AND METABOLIC SYNDROME - Preferred embodiments of the present invention are related to novel therapeutic drug combinations and methods for treating and/or preventing complications in patients with diabetes and/or metabolic syndrome. More particularly, aspects of the present invention are related to using a combination of cicletanine and an oral antidiabetic agent for treating and/or preventing complications (including microalbuminuria, nephropathies, retinopathies and other complications) in patients with diabetes or metabolic syndrome. | 01-30-2014 |
20140073651 | BENZAMIDE DERIVATIVES AS P2X7 RECEPTOR ANTAGONISTS - The invention relates to benzamide derivatives of formula (I), | 03-13-2014 |
20140107133 | 3,5-DIAMINO-6-CHLORO-N-(N-(4-(4-(2-(HEXYL(2,3,4,5,6-PENTAHYDROXYHEXYL)AMIN- O)ETHOXY)PHENYL)BUTYL)CARBAMIMIDOYL)PYRAZINE-2-CARBOXAMIDE - The present invention relates to the compound of the formula: | 04-17-2014 |
20140142117 | REVERSE AMIDE COMPOUNDS AS PROTEIN DEACETYLASE INHIBITORS AND METHODS OF USE THEREOF - The present invention relates to novel “reverse amide” compounds comprising a zinc chelator group, and the use of such compounds in the inhibition of HDAC6 and in the treatment of various diseases, disorders or conditions related to HDAC6. | 05-22-2014 |
20140142118 | CHEMICALLY AND METABOLICALLY STABLE DIPEPTIDE POSSESSING POTENT SODIUM CHANNEL BLOCKER ACTIVITY - A very stable, selective and renally safe sodium channel blocker represented by the formula: The invention also includes a variety of compositions, combinations and methods of treatment using this inventive sodium channel blocker. | 05-22-2014 |
20140148468 | SPECIFIC CARBOXAMIDES AS KCNQ2/3 MODULATORS - The invention relates to specific carboxamides, to processes for their preparation, to medicaments comprising these compounds and to the use of these compounds in the preparation of medicaments. | 05-29-2014 |
20140148469 | USE OF FORM-I CRYSTAL OF 2--N-(METHYLSULFONYL)ACETAMIDE - A main object of the present invention is to provide a novel crystal of 2-{4-[N-(5,6-diphenylpyrazin-2-yl)-N-isopropylamino]butyloxy}-N-(methylsulfonyl)acetamide (hereinafter referred to as “compound A”). A Form-I crystal of compound A shows diffraction peaks at 9.4 degrees, 9.8 degrees, 17.2 degrees and 19.4 degrees in the powder X-ray diffraction spectrum thereof. A Form-II crystal of compound A shows diffraction peaks at 9.0 degrees, 12.9 degrees, 20.7 degrees and 22.6 degrees in the powder X-ray diffraction spectrum thereof. A Form-III crystal of compound A shows diffraction peaks at 9.3 degrees, 9.7 degrees, 16.8 degrees, 20.6 degrees and 23.5 degrees in the powder X-ray diffraction spectrum thereof. | 05-29-2014 |
20140155414 | CRYSTALS OF 2- {4- [N- (5,6-DIPHENYLPYRAZIN-2-YL) -N-ISOPROPYLAMINO]BUTYLOXY}-N- (METHYLSULFONYL) ACETAMIDE - A main object of the present invention is to provide a novel crystal of 2-{4-[N-(5,6-diphenylpyrazin-2-yl)-N-isopropylamino]butyloxy}-N-(methylsulfonyl)acetamide (hereinafter referred to as “compound A”). A Form-I crystal of compound A shows diffraction peaks at 9.4 degrees, 9.8 degrees, 17.2 degrees and 19.4 degrees in the powder X-ray diffraction spectrum thereof. A Form-II crystal of compound A shows diffraction peaks at 9.0 degrees, 12.9 degrees, 20.7 degrees and 22.6 degrees in the powder X-ray diffraction spectrum thereof. A Form-III crystal of compound A shows diffraction peaks at 9.3 degrees, 9.7 degrees, 16.8 degrees, 20.6 degrees and 23.5 degrees in the powder X-ray diffraction spectrum thereof. | 06-05-2014 |
20140171447 | CHLORO-PYRAZINE CARBOXAMIDE DERIVATIVES WITH EPITHELIAL SODIUM CHANNEL BLOCKING ACTIVITY - This invention provides compounds of the formula I: | 06-19-2014 |
20140213598 | SUBSTITUTED CYANOANILINE COMPOUNDS, PREPARATION AND USE THEREOF - Disclosed is a substituted cyanoaniline compound or a salt thereof, wherein the compound has a structure represented by General Formula I. The compound of General Formula I has broad-spectrum fungicidal activity in the field of agriculture and effectively prevents against a variety of pathogens such as cucumber downy mildew, wheat powdery mildew, maize rust disease, rice blast and cucumber gray mold. In particular, even at a low dose, the compound effectively prevents and treats rice blast, cucumber gray mold, maize rust disease and cucumber downy mildew. Moreover, the raw materials for preparing the compounds are widely available and the synthesis method therefor is simple and convenient. | 07-31-2014 |
20140221397 | FIBROSIS INHIBITOR - [Object] The main object of the present invention is to provide a fibrosis inhibitor. | 08-07-2014 |
20150018374 | FUNGICIDAL PYRAZOLE MIXTURES - Disclosed is a fungicidal composition comprising (a) at least one compound selected from the compounds of Formula 1, N-oxides, and salts thereof, | 01-15-2015 |
20150099764 | DENDRIMER LIKE AMINO AMIDES POSSESSING SODIUM CHANNEL BLOCKER ACTIVITY FOR THE TREATMENT OF DRY EYE AND OTHER MUCOSAL DISEASES - Sodium channel blockers represented by the formula: | 04-09-2015 |
20150126527 | MODULATORS OF THE PROSTACYCLIN (PGI2) RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO - The present invention relates to amide derivatives of Formula (XIIIa) and pharmaceutical compositions thereof that modulate the activity of the PGI2 receptor. Compounds of the present invention and pharmaceutical compositions thereof are directed to methods useful in the treatment of: Pulmonary arterial hypertension (PAH); idiopathic PAH; familial PAH; PAH associated with a collagen vascular disease, a congenital heart disease, portal hypertension, HIV infection, ingestion of a drug or toxin, hereditary hemorrhagic telangiectasia, splenectomy, pulmonary veno-occlusive disease (PVOD) or pulmonary capillary hemangiomatosis (PCH); PAH with significant venous or capillary involvement; platelet aggregation; coronary artery disease; myocardial infarction; transient ischemic attack, angina; stroke; ischemia-reperfusion injury; restenosis; atrial fibrillation; blood clot formation in an angioplasty or coronary bypass surgery individual or in an individual suffering from atrial fibrillation; atherosclerosis; atherothrombosis; asthma or a symptom thereof; a diabetic-related disorder such as diabetic peripheral neuropathy, diabetic nephropathy or diabetic retinopathy; glaucoma or other disease of the eye with abnormal intraocular pressure; hypertension; inflammation; psoriasis; psoriatic arthritis; rheumatoid arthritis; Crohn's disease; transplant rejection; multiple sclerosis; systemic lupus erythematosus (SLE); ulcerative colitis; ischemia-reperfusion injury; restenosis; atherosclerosis; acne; type 1 diabetes; type 2 diabetes; sepsis; and chronic obstructive pulmonary disorder (COPD). | 05-07-2015 |
20150290189 | CHEMICALLY AND METABOLICALLY STABLE DIPEPTIDE POSSESSING POTENT SODIUM CHANNEL BLOCKER ACTIVITY - A very stable, selective and renally safe sodium channel blocker represented by the formula: | 10-15-2015 |
20150307445 | Novel Compounds as Diacylglycerol Acyltransferase Inhibitors - This invention relates to novel compounds which are inhibitors of acyl coenzymeA: diacylglycerol acyltransferase 1 (DGAT-1), to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy for the prevention or treatment of diseases related to DGAT-1 dysfunction or where modulation of DGAT-1 activity may have therapeutic benefit including but not limited to obesity, obesity related disorders, hypertriglyceridemia, hyperlipoproteinemia, chylomicronemia, dyslipidemia, non-alcoholic steatohepatitis, diabetes, insulin resistance, metabolic syndrome, hepatitis C virus infection and acne or other skin disorders. | 10-29-2015 |
20150329517 | TETRAHYDRONAPHTHYL(THIO) CARBOXAMIDES - The present invention relates to novel tetrahydronaphthyl(thio) carboxamides, to processes for preparing these compounds, to compositions comprising these compounds, and to the use thereof as biologically active compounds, especially for control of harmful microorganisms in crop protection and in the protection of materials | 11-19-2015 |
20150343059 | RADIOSENSITIZER COMPOUNDS FOR USE IN COMBINATION WITH RADIATION - Disclosed herein are radiosensitizer compounds useful in combination with radiation therapy, e.g., a synergistic combination therapy for the treatment of cancer and other disorders. The radiosensitizer compounds have the general formula I: wherein A represents an aromatic core; at least one of R | 12-03-2015 |
20150368231 | N-SUBSTITUTED-5-SUBSTITUTED PHTHALAMIC ACIDS AS SORTILIN INHIBITORS - The present invention is directed to N-substituted-5-substituted phthalamic acids which of formula (A). The compounds are considered useful for the treatment of diseases treatment of a neurodegenerative disease, psychiatric disease, motorneuron disease, peripheral neuropathies, pain, neuroinflammation or atherosclerosis such as Alzheimer's disease and Parkinson's disease. | 12-24-2015 |
20150376145 | STABLE SODIUM CHANNEL BLOCKERS - A very stable, selective and renally safe sodium channel blocker represented by the formula: | 12-31-2015 |
20160039750 | Bioavailable Diacylhydrazine Ligands for Modulating the Expression of Exogenous Genes via an Ecdysone Receptor Complex - The present invention relates to non-steroidal ligands for use in nuclear receptor-based inducible gene expression system, and a method to modulate exogenous gene expression in which an ecdysone receptor complex comprising: a DNA binding domain; a ligand binding domain; a transactivation domain; and a ligand is contacted with a DNA construct comprising: the exogenous gene and a response element; wherein the exogenous gene is under the control of the response element and binding of the DNA binding domain to the response element in the presence of the ligand results in activation or suppression of the gene. | 02-11-2016 |
20160100579 | NEMATICIDAL N-(2-SUBSTITUTED 2-PHENYLETHYL)CARBOXAMIDES AND N-(2-SUBSTITUTED 2-PHENYLETHYL)-THIOCARBOXAMIDES - The present invention relates to the use of known and novel N-(2-substituted 2-phenylethyl)carboxamides and N-(2-substituted 2-phenylethyl)thiocarboxamides, for the control of plant damaging nematodes in agriculture and further relates to novel N-(2-substituted 2-phenylethyl)carboxamides and N-(2-substituted 2-phenylethyl)thiocarboxamides, processes and intermediate compounds for their preparation, their use as nematicides and their use as anthelmintics against endoparasites in animals and humans, compositions containing such compounds and methods for the control of nematodes and helminths. | 04-14-2016 |
20160115119 | alpha-SUBSTITUTED GLYCINAMIDE DERIVATIVE - The present invention is to provide a novel α-substituted glycinamide derivative, or a pharmaceutically acceptable salt thereof, a pharmaceutical composition comprising the same, and a pharmaceutical use thereof. | 04-28-2016 |
20160143908 | COMPOSITION FOR REDUCING NERVOUS SYSTEM INJURY AND METHOD OF MAKING AND USE THEREOF - This application discloses a composition comprising an amiloride and/or an amiloride analog which can be used for reducing nerve injury or nervous system injury in a subject. The formulation of such composition is also disclosed. The application further directs to methods for treating nerve injury or nervous system injury by administering to the subject a therapeutically effective amount of a pharmaceutical composition comprising amiloride, an amiloride analog or a pharmaceutically acceptable salt thereof. | 05-26-2016 |
20160165890 | PLANT DISEASE CONTROL COMPOSITION AND ITS USE | 06-16-2016 |
20160184304 | COMPOSITION FOR REDUCING NERVOUS SYSTEM INJURY AND METHOD OF MAKING AND USE THEREOF - This application discloses a composition comprising an amiloride and/or an amiloride analog which can be used for reducing nerve injury or nervous system injury in a subject. The formulation of such composition is also disclosed. The application further directs to methods for treating nerve injury or nervous system injury by administering to the subject a therapeutically effective amount of a pharmaceutical composition comprising amiloride, an amiloride analog or a pharmaceutically acceptable salt thereof. | 06-30-2016 |
20160250213 | FORMULATIONS OF AZAINDOLE COMPOUNDS | 09-01-2016 |
20160251353 | INHIBITORS OF INFLUENZA VIRUSES REPLICATION | 09-01-2016 |
20180021333 | METHODS AND PHARMACEUTICAL COMPOSITIONS FOR THE TREATMENT OF EBOLA VIRUS DISEASE | 01-25-2018 |
20190144397 | Crystalline Form of Selexipag | 05-16-2019 |