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Plural hetero atoms in the polycyclo ring system

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514 - Drug, bio-affecting and body treating compositions

514001000 - DESIGNATED ORGANIC ACTIVE INGREDIENT CONTAINING (DOAI)

514183000 - Heterocyclic carbon compounds containing a hetero ring having chalcogen (i.e., O,S,Se or Te) or nitrogen as the only ring hetero atoms DOAI

514277000 - Hetero ring is six-membered consisting of one nitrogen and five carbon atoms

514336000 - Additional hetero ring containing

514337000 - The additional hetero ring is one of the cyclos in a polycyclo ring system

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Entries
DocumentTitleDate
20100063099ADENYLYL CYCLASES AS NOVEL TARGETS FOR THE TREATMENT OF INFECTION BY EUKARYOTIC PATHOGENS - The present invention relates to a method of preventing or treating a disease caused by infection by a eukaryotic pathogen, wherein the method comprises administering an effective amount of a modulator of a eukaryotic pathogen's adenylyl cyclase. The invention also provides pharmaceutical compositions useful for preventing or treating a disease, with the compositions containing a therapeutically effective amount of a modulator of a eukaryotic pathogen's adenylyl cyclase. The invention also provides screening methods for identifying selective modulators of a eukaryotic pathogen's adenylyl cyclase that do not substantially modulate an adenylyl cyclase of the subject. The invention also provides methods for culturing eukaryotic pathogens and methods for inducing the pathogenic state in vitro.03-11-2010
20090215830Multiple ppi dosage form - Herein provided are dosage forms (variously referred to as “formulations”) comprising a PPI that is released from the dosage form as a first and a second dose. Each dose of PPI is present in an amount sufficient to raise the plasma levels of the PPI to at least 100 ng/ml.08-27-2009
20100022596EPOTHILONE ANALOGUES - The invention relates to analogues of epothilones, uses and methods of making the same.01-28-2010
20110195999NOVEL ANTIFUNGAL AGENT CONTAINING HETEROCYCLIC COMPOUND - The present invention provides an antifungal agent represented by the formula:08-11-2011
20110195998PEST CONTROL AGENT - Disclosed is a compound usable as a pest control agent and has excellent pest control activity. A compound represented by formula (I) has excellent pest control activity. The compound or an agriculturally or horticulturally acceptable salt thereof is thus useful as a pest control agent.08-11-2011
20100087488Physiologically Acceptable Salts of 3-[(2--1-methyl-1H-benzimidazol-5-carbonyl)-pyridin-2-yl-amino]-propionic acid ethyl ester - The invention relates to new salt forms of the active substance ethyl 3-[(2-{[4-(hexyloxycarbonylamino-imino-methyl)-phenylamino]-methyl}-methyl-1H-benzimidazole-5-carbonyl)-pyridin-2-yl-amino]-propionate.04-08-2010
20100113528OXADIAZOLE SUBSTITUTED INDAZOLE DERIVATIVES FOR USE AS SPHINGOSINE 1-PHOSPHATE (S1P) AGONISTS - The present invention provides compounds of formula (I) or salts thereof:05-06-2010
20100113524Prodrugs of proton pump inhibitors including the (1h-pyrrol-1-yl)-1h-benzimidazole moiety - The compounds of the formulas (I), (II), (III) and (IV), where the symbols are as defined in the specification are prodrugs of proton pump inhibitors. The R05-06-2010
201000760263-AMINO-INDAZOLE OR 3-AMINO-4,5,6,7-TETRAHYDRO-INDAZOLE DERIVATIVES - This invention relates to novel indazole derivatives of formula I:03-25-2010
20100076027INDAZOLE OR 4,5,6,7-TETRAHYDRO-INDAZOLE DERIVATIVES - This invention relates to novel indazole or 4,5,6,7-tetrahydro-indazole derivatives of formula I03-25-2010
20100076025PROCESS FOR SOLVENT REMOVAL FROM OMEPRAZOLE SALTS - The present invention relates to a process for removing an organic solvent from a salt of omeprazole, in particular a magnesium salt of omeprazole, a composition comprising a salt of omeprazole, in particular a magnesium salt of omeprazole obtainable by such a process, and pharmaceutical compositions comprising said composition or a salt of omeprazole, in particular a magnesium salt of omeprazole, in particular where omeprazole is S-omeprazole.03-25-2010
20120245203METHODS FOR TREATING HEARTBURN AND/OR PREVENTING GASTRIC BLEEDING OR HEMORRHAGE IN PATIENTS RECEIVING CLOPIDOGREL THERAPY - The present invention relates to methods of treating heartburn in a patient receiving clopidogrel therapy. In another aspect, the present invention relates to methods of preventing gastric bleeding or hemorrhage in patients receiving clopidogrel therapy.09-27-2012
20130085163Pyripyropene Derivative Having ACAT2 Inhibiting Activity and Stable to Metabolizing Enzymes - A compound effective in prevention and treatment of arteriosclerosis with a mechanism different from that of statin drugs has the following formula or a pharmaceutically acceptable salt, solvate, or hydrate thereof:04-04-2013
20130035358Bis Aromatic Compounds for Use as LTC4 Synthase Inhibitors - There is provided compounds of formula I,02-07-2013
20130040994Methods of Treatment Using Allosteric Processing Inhibitors for Matrix Metalloproteinases - The present invention includes a crystal comprising a complex of the pro form of a matrix metalloprotease (proMMP) and a small-molecule allosteric processing inhibitor that inhibits that activation of the proMMP, methods for identifying small-molecule allosteric processing inhibitors that inhibit the activation of a proMMP, and methods of treatment using small-molecule allosteric processing inhibitors that inhibit the activation of a proMMP. The present invention relates to the crystal structure of a complex of proMMP9 bound to a small-molecule allosteric processing inhibitor that inhibits activation of proMMP9. The invention further relates to the use of the methods and the crystal and related structural information for designing, selecting and/or optimizing small-molecule allosteric processing inhibitors that inhibit activation of proMMP9 and proMMP9 homologues. The present invention also relates to the use of small-molecule allosteric processing inhibitors for the treatment of diseases mediated by inappropriate matrix metalloproteinase (MMP) activity.02-14-2013
20130040993FUNGICIDE HYDROXIMOYL-HETEROCYCLES DERIVATIVES - The present invention relates to hydroximoyl-heterocycle derivatives, their process of preparation, their use as fungicide active agents, particularly in the form of fungicide compositions, and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions.02-14-2013
20130079374TRICYCLIC COMPOUND AND PHARMACEUTICAL USE THEREOF - The present invention provides a compound represented by the formula03-28-2013
20120264785Fluoro-substituted 3,5-dicyano-4-(1H-indazol-5-yl)-2,6-dimethyl-1,4-dihydropyridine derivatives and methods of use thereof - The present invention relates to novel fluoro-substituted 3,5-dicyano-4-(1H-indazol-5-yl)-2,6-dimethyl-1,4-dihy-dropyridine derivatives having protein tyrosine kinase inhibitory activity, to a process for the manufacture thereof and to the use thereof for the treatment of c-Met-mediated diseases or c-Met-mediated conditions, particularly cancer and other proliferative disorders.10-18-2012
20100105738EXTENDED RELEASE FORMULATIONS OF A PROTON PUMP INHIBITOR - The invention provides extended release formulations of proton pump inhibitor, such as an extended release formulation of rabeprazole, comprising an amount of rabeprazole between 30 and 90 mg rabeprazole and having an AUC of between 900 and 1750 ng*hr/mL and other properties.04-29-2010
20100105739MODULATORS OF ATP-BINDING CASSETTE TRANSPORTERS - Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.04-29-2010
20080214619Business method to treat and/or prevent a gastric acid disorder with a proton pump inhibitor (PPI) and a cholinergic agonist to induce rapid onset of PPI action with or without food - Pharmaceutical proton pump inhibitor (PPI) medications and methods are disclosed for preventing and/or treating gastrointestinal disorders characterized by abnormalities in gastric acid secretion at anytime of the day or night without the need for food effect or to be taken with food. The medications comprise a PPI and a cholinergic agonist for inducing rapid onset of PPI action, for increasing the duration of PPI efficacy and for optimizing clinical PPI effectiveness that may be administered at any time of the day or night without food or on an empty stomach, and possibly on an as-needed or on demand basis. In carrying out the methods, a PPI and cholinergic agonist may be administered together as a single unitary dose in the form of a liquid or solid, or administered together, but separately as either liquids or solids or a combination thereof. Preferably, an oral solid dosage form of the present invention allows for release of a proton pump inhibitor at a pH of about 5 or higher, e.g., pH about 5.5, 6, 6.5 or 7, followed by release of a cholinergic agonist within between about 10 minutes and about 60 minutes, preferably within about 15 minutes and about 30 minutes, after release of the proton pump inhibitor from the dosage form, so that it can be administered at any time of the day or night independent of food or food effect. It is believed that the methods and compositions of the present invention will increase the duration of PPI efficacy by between at least about 5 fold and about 10 fold or even about 20 fold, as compared to the duration of PPI efficacy derived from current PPI dosage forms administered alone and without food or a food effect. Kits comprising a PPI, a cholinergic agonist and optionally an antacid are disclosed, such as kits containing each drug in conventional and commercially available dry or liquid dosage forms for simultaneous or concomitant administration or in dry dosage forms to provide for the easy preparation of a liquid composition from the dry dosage forms. These new medications and methods will simplify the traditional continuous PPI regimen and improve patient compliance.09-04-2008
20100093806PHOSPHODIESTERASE 4 INHIBITORS, INCLUDING AMINOINDAZOLE AND AMINOBENZOFURAN ANALOGS - PDE4 inhibition is achieved by novel compounds, e.g., aminoindazole and aminobenzofuran analogs. The compounds of the present invention are of Formulas I and II:04-15-2010
20090176839FORMULATIONS OF 3-(6-(1-(2,2-DIFLUOROBENZO[D][1,3]DIOXOL-5-YL) CYCLOPROPANECARBOXAMIDO)-3-METHYLPYRIDIN-2-YL)BENZOIC ACID - The present invention relates to formulations of 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid, pharmaceutical packs or kits thereof, and methods of treatment therewith.07-09-2009
20130045994PYRIDINE DERIVATIVE - The present invention relates to a novel pyridine derivative or a pharmacologically acceptable ester thereof, or a pharmacologically acceptable salt of the derivative or ester, which has an excellent hypoglycemic effect or treats and/or prevents the onset of a disorder of carbohydrate or lipid metabolism or a disease mediated by peroxisome proliferator-activated receptor (PPAR) γ. A compound represented by the general formula (I):02-21-2013
20090042948Physiologically acceptable salts of 3--1-methyl-1H-benzimidazol-5-carbonyl)-pyridin-2-yl-amino]-propionic acid ethyl ester - The invention relates to new, physiologically acceptable salts of the active substance ethyl 3-[(2-{[4-(hexyloxycarbonylamino-imino-methyl)-phenylamino]-methyl}-1-methyl-1H-benzimidazole-5-carbonyl)-pyridin-2-yl-amino]-propionate.02-12-2009
20090042945Benzo[d]isoxazol-3-yl-amine Compounds and Their Use as Vanilloid Receptor Ligands - The present invention relates to substituted benzo[d]isoxazol-3-yl-amine compounds, methods for their production, medicaments containing these compounds and the use of these compounds to produce medicaments.02-12-2009
20110015234INDAZOLE DERIVATIVES - The invention is concerned with novel indazole derivatives of formula (I)01-20-2011
20110015233Stable Pharmaceutical Omeprazole Formulation for Oral Administration - The present invention is directed to a pharmaceutical solution or syrup formulation for oral administration comprising; omeprazole, a solubilizing agent, a sweetening agent, a flavoring agent, and an antioxidant.01-20-2011
20110065755STABLE R(+)-LANSOPRAZOLE AMINE SALT AND A PROCESS FOR PREPARING THE SAME - A stable R-(+)-lansoprazole alkylamine salt and a process for preparing the salt.03-17-2011
200902704576,11-BICYCLOLIDES: BRIDGED BIARYL MACROLIDE DERIVATIVES - The present invention discloses compounds of formula I, or pharmaceutically acceptable salts, esters, or prodrugs thereof:10-29-2009
20100280077Process for Preparation of Stable Amorphous R-Lansoprazole - A process for preparing stable amorphous R-(+)-lansoprazole comprising optically resolving racemic lansoprazole by the formation of host-guest inclusion complexes by selectively and reversibly including chiral guest molecules in the lansoprazole.11-04-2010
20130065927FORMS OF DEXLANSOPRAZOLE AND PROCESSES FOR THE PREPARATION THEREOF - Provided is dexlansoprazole propylene glycolate hydrate. Polymorphic forms thereof are also provided. The dexlansoprazole propylene glycolate hydrate maybe such that the propylene glycol component is present in approximately equal proportions of (R) absolute configuration and (S) absolute configuration, or present in predominantly (R) absolute configuration, or predominantly (S) absolute configuration. Salts of dexlansoprazole are also provided. In particular, crystalline dexlansoprazole isopropylammonium salt and crystalline MTBE solvate of dexlansoprazole t-butylammonium salt are provided. Pharmaceutical formulations comprising dexlansoprazole propylene glycolate hydrate are also provided. Furthermore, processes for preparation of dexlansoprazole propylene glycolate hydrate are provided.03-14-2013
20110021571ACYLOXYALKYL CARBAMATE PRODRUGS, METHODS OF SYNTHESIS AND USE - The disclosures herein relate generally to acyloxyalkyl carbamate prodrugs of (±)-4-amino-3-(4-chlorophenyl)butanoic acid and analogs thereof, pharmaceutical compositions thereof, methods of making prodrugs of (±)-4-amino-3-(4-chlorophenyl)butanoic acid and analogs thereof, methods of using prodrugs of (±)-4-amino-3-(4-chlorophenyl)butanoic acid and analogs thereof, and pharmaceutical compositions thereof for treating or preventing common diseases and/or disorders such as spasticity and/or acid reflux disease. The disclosures herein also relate to acyloxyalkyl carbamate prodrugs of (±)-4-amino-3-(4-chlorophenyl)butanoic acid and analogs thereof which are suitable for oral administration and to sustained release oral dosage forms thereof.01-27-2011
20100087489Phenyl and Benzodioxinyl Substituted Indazoles Derivatives - A compound of formula Ia:04-08-2010
20080293773Amorphous Esomeprazole Hydrate - The present invention relates to a novel amorphous form of esomeprazole hydrate, to a process for its preparation and to a pharmaceutical composition containing it. Thus, tetrahydrofuran and water are added to esomeprazole potassium salt at 25-30 C, cooled to 20 C and then the pH is adjusted to 7.5-8.0 with acetic acid. The reaction mass is cooled to 5 C, stirred for 2 to 3 hours at 0-5 C, filtered the mass, washed with chilled mixture of water and tetrahydrofuran (2:1), and again washed with water. The wet cake is dried at 30-35 C under vacuum to reach the moisture content to 25-30%. The solid is again dried in rotovapour at 25-30 C under nitrogen atmosphere to give amorphous esomeprazole hydrate.11-27-2008
20080287503CARBAMOYLBENZOTRIAZOLE DERIVATIVES AS INHIBITORS OF LIPASES AND PHOSPHOLIPASES - The invention relates to carbamoylbenzotriazole derivatives of general formula (I), which are defined as cited in the description, to their pharmaceutically applicable salts and to their use as medicaments.11-20-2008
20100160380Therapeutic Salt Compositions and Methods - Therapeutic salt compositions and methods are disclosed herein.06-24-2010
20080275089Compositions and methods to treat gastrointestinal disorders - The invention provides safe and effective methods for treating and preventing dysphagia, lower esophageal mucosal rings, esophageal strictures, achalasia, gastric mucosal injuries, and bacterial infections. The methods comprise administering at least one proton pump inhibitor, optionally in combination with antibacterial compounds. In one embodiment, the proton pump inhibitor is rabeprazole, a pharmaceutically acceptable salt thereof and/or a stereoisomer thereof.11-06-2008
20110294854SUBSTITUTED OCTAHYDROCYCLOPENTA[c]PYRROLES AS CALCIUM CHANNEL MODULATORS - The present application relates to calcium channel inhibitors containing compounds of formula (I)12-01-2011
20100305163PHARMACEUTICAL FORMULATIONS COMPRISING NSAID AND PROTON PUMP INHIBITOR DRUGS - Aspects of the invention relate to pharmaceutical formulations comprising an NSAID and acid reducer drug for therapeutic purposes, and methods of preparing the same. Further aspects of the invention relate to fixed dose pharmaceutical formulations comprising naproxen, or pharmaceutically acceptable salts thereof, and esomeprazole, or pharmaceutically acceptable salts thereof.12-02-2010
20110281917Substituted Benzimidazoles for the Treatment of Astrocytomas - The present invention relates to the use of BENZIMIDAZOLE DERIVATIVES for the preparation of a drug for the treatment of astrocytomas.11-17-2011
20090042946METHOD AND KIT FOR CONTROLLING BLEEDING - Methods and kits for controlling bleeding from a disrupted blood vessel, wherein a vanilloid receptor agonist is administered to the site of the disruption of the blood vessel in a quantity sufficient to control the bleeding.02-12-2009
20110301201DABIGATRAN FOR PERCUTANEOUS INTERVENTIONAL CARDIAC CATHETERISATION - The invention relates to a new use of dabigatran etexilate of formula (I) optionally in the form of the pharmaceutically acceptable salts thereof, and new medicament formulations which may be used for this purpose.12-08-2011
20090221646CRYSTALLINE SOLVATE OF OMEPRAZOLE SODIUM - The present invention belongs to the field of pharmaceutical industry and relates to novel crystalline omeprazole sodium ethanol solvate and to the process for its preparation, which acts as intermediary compound to the processes for its conversion into different crystalline forms, first of all to a known omeprazole sodium form A, with low amount of residual solvents, i.e. less than 0.5% by weight of residual solvent.09-03-2009
20130023568Benzimidazole Derivatives And Their Pharmaceutical Compositions And Uses - The present invention relates to benzimidazole derivatives and their pharmaceutical compositions and uses, specifically to benzimidazole derivatives of Formula (I), or their stereoisomer, pharmaceutically acceptable salt or solvates thereof, in which R01-24-2013
20090298884Esomeprazole Strontium Salt, Process For Its Preparation and Pharmaceutical Compositions Containing Same - A strontium salt of esomeprazole is provided. A process for preparing a strontium salt of esomeprazole is also provided comprising reacting esomeprazole free base or a sodium, potassium or lithium salt of esomeprazole with a strontium source in one or more solvents.12-03-2009
20090209592INHIBITORS OF THE GASTRIC H+, K+-ATPASE WITH ENHANCED THERAPEUTIC PROPERTIES - Chemical syntheses and medical uses of novel inhibitors of the gastric H08-20-2009
20110288130BACTERIAL THIOREDOXIN REDUCTASE INHIBITORS AND METHODS FOR USE THEREOF - The mechanism of action of Ebselen differentiates between bacterial and mammalian thioredoxin reductase (TrxR). It displays fast oxidation of mammalian Trx and via the NADPH-TrxR catalyzed turnover of ebselen selenol with hydrogen peroxide, and therefore are mammalian antioxidants. Ebselen, and its diselenide, are strong competitive inhibitors of 11-24-2011
20100035933Kits, Recloseable Containers, Blanks And Methods Of Treatment - Kits include a recloseable container and an inner container housed within the recloseable container. The recloseable container can include a front wall and a front flap operable to transition between an open position and a closed position, wherein the front flap releasably engages the front wall when in the closed position. Methods of treatment which utilize the kits are also disclosed. Blanks for the recloseable container are also disclosed.02-11-2010
200900992363-Amino-1-arylpropyl indoles and AZA-substituted indoles and uses thereof - The present invention provides compounds of the formula:04-16-2009
20090099235Pyrazolopyrrolidines as Inhibitors of Gamma Secretase - The invention provides compounds of Formula I04-16-2009
20100113527CRYSTALLINE FORMS OF DEXLANSOPRAZOLE - Provided are crystalline forms of dexLansoprazole, as well as processes for the preparation thereof.05-06-2010
20100113525PEST CONTROL COMPOSITION - Disclosed is a pest control composition comprising at least one pyripyropene derivative of formula (I) or agriculturally and horticulturally acceptable salt thereof and at least one other pest control agent as active ingredients. The combined use of the two ingredients can provide a better insecticidal effect.05-06-2010
20100120863AMINOTETRAHYDROPYRANS AS DIPEPTIDYL PEPTIDASE-IV INHIBITORS FOR THE TREATMENT OR PREVENTION OF DIABETES - The present invention is directed to novel substituted aminotetrahydropyrans of structural formula I which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.05-13-2010
20100087490Dosage Units of 3-(6-(1-(2,2-Difluorobenzo[D] [1,3] Dioxol-5-YL) Cyclopropanecarboxamido)-3-Methylpyridin-2-YL)Benzoic Acid - The present invention relates to formulations of 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid in Form I, pharmaceutical packs or kits thereof, and methods of treatment therewith.04-08-2010
20090306143Derivatives of N-(heteroaryl)-1-heteroaryl-1H-indole-2-carboxamides, preparation thereof and therapeutic use thereof - The invention relates to compounds of formula (I):12-10-2009
20120108637Fused Bicyclic-Substituted Amines as Histamine-3 Receptor Ligands - Compounds of formula (I)05-03-2012
20090036493Benzimidazole Derivatives and Their Use for Modulating the GABA Alpha Receptor Complex - This invention relates to novel benzimidazole derivatives, pharmaceutical compositions containing these compounds, and methods of treatment therewith.02-05-2009
20110172276CARBOXAMIDE COMPOUND AND USE OF THE SAME - A carboxamide compound represented by the formula (I):07-14-2011
20090203743SMALL MOLECULE ENTRY INHIBITORS - The present invention concerns the compounds having the formula08-13-2009
20080207697Use of Epothilones in the Treatment of Neuronal Connectivity Defects Such as Schizophrenia and Autism - The present invention is about the use of at least one epothilone or derivative thereof as an active ingredient for manufacturing a medicament for use in the treatment of disease(s) involving a neuronal connectivity defect, such as schizophrenia or autism.08-28-2008
20100113526Process for the Preparation of Esomeprazole Magnesium Dihydrate - A process for preparing Form A of (S)-5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridinyl)-methyl]sulfinyl]-1H-benzimidazole magnesium dihydrate, processes for preparing various intermediates useful in the preparation of Form A of (S)-5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridinyl)-methyl]sulfinyl]-1H-benzimidazole magnesium dihydrate and a novel polymorphic Form II of 5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridinyl)-methyl]thio]-1H-benzimidazole.05-06-2010
20080275090AMINO-BENZAZOLES AS P2Y1 RECEPTOR INHIBITORS WITH PYRIDINE RING AND HETEROCYCLIC COMPONENTS - The present invention provides novel amino-benzazoles and analogues thereof, which are selective inhibitors of the human P2Y11-06-2008
20090170904Substituted benzimidazoles and methods of their use - New substituted benzimidazole compounds, compositions, and methods of inhibition of kinase activity associated with tumorigenesis in a human or animal subject are provided. In certain embodiments, the compounds and compositions are effective to inhibit the activity of at least one serine/threonine kinase or receptor tyrosine kinase. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a serine/threonine kinase- or receptor tyrosine kinase-mediated disorder, such as cancer.07-02-2009
20080306118Process for the crystallization of (R) - or (S) - Lansoprazole - The present invention relates to a production method of a crystal of (R)-lansoprazole or (S)-lansoprazole, which includes crystallization at a temperature of about 0° C. to about 35° C. from a C12-11-2008
20080207698Novel Compounds 569 - The present invention provides compounds of formula (I)08-28-2008
20110207780Therapeutic Salt Compositions and Methods - Therapeutic salt compositions and methods are disclosed herein.08-25-2011
20090264473Novel Crystalline Forms of Antidiabetic Compounds - A novel crystalline anhydrate of the free acid and a crystalline anhydrous besylate salt of a selective PPAR gamma partial agonist which has a fused bicyclic aromatic group attached to an oxypropanoic acid moiety are stable and non-hygroscopic. The compounds are suitable for preparing pharmaceutical formulations for the treatment of type 2 diabetes, hyperglycemia, obesity, and dyslipidemia.10-22-2009
20080269298Benzimidazol-1-YL-thiophene compounds for the treatment of cancer - The present invention provides compounds of formula (I):10-30-2008
20090163551Compositions and Methods for Treating Diseases - This invention relates to methods for treating, preventing and/or managing gastric injury, e.g., NSAID-induced gastric injury in a subject including administering to the subject tegaserod, alone or in combination with a proton pump inhibitor. Also provided are compositions and kits for use in methods of the invention.06-25-2009
20090030044Crystal of Salt of Benzimidazole Compound - A crystal of a salt of 2-[[[3-methyl-4-(2,2,2-trifluoroethoxy)-2-pyridinyl]methyl]sulfinyl]-1H-benzimidazole which is useful as a medicine, and use of the crystal.01-29-2009
20110207779PROCESS FOR THE PREPARATION OF ESOMEPRAZOLE MAGNESIUM - The present invention relates to a process for the preparation of esomeprazole magnesium containing R-isomer greater than about 0.1% by wt. In particular, the present invention relates to a process for the preparation of esomeprazole magnesium dihydrate containing R-isomer greater than about 0.1% by wt.08-25-2011
20090163553BENZIMIDAZOLE COMPOUND CRYSTAL - A novel crystal of (R)-2-[[[3-methyl-4-(2,2,2-trifluoroethoxy)-2-pyridinyl]methyl]sulfinyl]-1H-benzimidazole or a salt thereof of the present invention is useful for an excellent antiulcer agent.06-25-2009
20090163552CARBOXYL- OR HYDROXYL-SUBSTITUTED BENZIMIDAZOLE DERIVATIVES - This invention relates to novel carboxyl- or hydroxyl-substituted benzimidazole derivatives of formula (I)06-25-2009
20090137634Pest control agents - Disclosed is a composition for use as a pest control agent, comprising a compound represented by formula (I) or an agriculturally and horticulturally acceptable salt thereof as active ingredient and an agriculturally and horticulturally acceptable carrier:05-28-2009
20090137633Stable pharmaceutical composition of rabeprazole - The present invention relates to a method of preparing a stable pharmaceutical composition of rabeprazole. The preparation may be used as an injectable dosage form in the treatment of severe gastric ulcers.05-28-2009
20090005422BACTERIAL THIOREDOXIN REDUCTASE INHIBITORS AND METHODS FOR USE THEREOF - The mechanism of action of Ebselen differentiates between bacterial and mammalian thioredoxin reductase (TrxR). It displays fast oxidation of mammalian Trx and via the NADPH-TrxR catalyzed turnover of ebselen selenol with hydrogen peroxide, and therefore are mammalian antioxidants. Ebselen, and its diselenide, are strong competitive inhibitors of 01-01-2009
20090176838Cyclourea Compounds as Calcium Channel Blockers - The invention relates to cyclourea compounds of Formula I: or a pharmaceutically acceptable salt or solvate thereof, wherein R07-09-2009
200803190222-Pyridyl substituted imidazoles as ALK5 and/or ALK4 inhibitors - 2-pyridyl-substituted imidazoles and their use in inhibiting ALK 5 and/or ALK 4 receptors is disclosed.12-25-2008
20110230523TRANSCRIPTION FACTOR MODULATING COMPOUNDS AND METHODS OF USE THEREOF - Substituted benzoimidazole compounds useful as anti-infectives that decrease resistance, virulence, or growth of microbes are provided. Methods of making and using substituted benzoimidazole compounds, as well as pharmaceutical preparations thereof, in, e.g., reducing antibiotic resistance and inhibiting biofilms.09-22-2011
20090197920METHODS AND COMPOSITIONS FOR MODULATING CALCIUM CHANNELS - The present invention relates to methods and compositions for modulating calcium channels. In particular, the present invention provides methods and compositions for modulating (e.g., disrupting) Cav1.3a calcium channels for research and therapeutic methods (e.g., treating dopaminergic diseases and conditions).08-06-2009
20090197919Novel Method for Preparation of Ammonium Salts of Esomeprazole - The present invention relates to a process for the preparation of quartenary ammoniumsalts of esomeprazole. Further, the present invention also relates to the use quartenary ammoniumsalts of esomeprazole for the treatment of gastrointestinal disorders, pharmaceutical compositions containing them as well as the quartenary ammoniumsalts of esomeprazole, as such.08-06-2009
20120289550COMPOSITION COMPRISING A COMBINATION OF OMEPRAZOLE AND LANSOPRAZOLE, AND A BUFFERING AGENT, AND METHODS OF USING SAME - The present disclosure relates to pharmaceutical compositions comprising omeprazole, lansoprazole and sodium bicarbonate. Methods of using such compositions are also provided11-15-2012
20120289549NEW HEXAHYDROPYRROLOIMIDAZOLONE COMPOUNDS - The invention provides novel compounds having the general formula (I),11-15-2012
20110224260CATECHOL-BASED DERIVATIVES FOR TREATING OR PREVENTING DIABETICS - The present invention provides a catechol-based derivative and a pharmaceutical acceptable salt therefrom and a solvate therefrom. A pharmaceutical composition for preventing or treating diabetes and ischemia, comprising a catechol-based derivative of formula (I) and at least one selected from the group consisting of a pharmaceutical excipient, a diluent and a carrier.09-15-2011
20090082404BENZIMIDAZOLES - Novel compounds of the formula I in which R03-26-2009
20080262043Solid Crystalline Form of Pantoprazole Free Acid, Salts Derived Therefrom and Process for Their Preparation - The invention relates, in general, to a new solid crystalline form of pantoprazole free acid (denominated “Form III”), salts derived therefrom (e.g., pantoprazole sodium and pantoprazole sodium sesquihydrate) and methods for producing the same. The invention further includes formulating pantoprazole free acid Form III, salts derived therefrom (e.g., pantoprazole sodium and pantoprazole sodium sesquihydrate) and/or in vivo cleavable prodrugs thereof (collectively “the compounds of the invention”) into readily usable dosage units for the therapeutic treatment (including prophylactic treatment) of mammals, including humans.10-23-2008
20090093522Freeze-dried pantoprazole preparation and pantoprazole injection - Lyophilized pantoprazole preparations which are obtainable by freeze-drying of an aqueous solution of pantoprazole, ethylenediamine tetraacetic acid and/or a suitable salt thereof, and sodium hydroxide and/or sodium carbonate are disclosed. The preparations have advantageous properties when reconstituted for injection.04-09-2009
20090209593NOVEL ANTIBACTERIAL AGENTS - This invention relates to novel macrolides, to the preparation of novel macrolides, to the use of such novel macrolides for preventing, treating, or ameliorating various conditions, and to the use of such novel macrolides as antibacterial agents.08-20-2009
20090209591Pharmaceutical product for injection - The present invention is related to a pharmaceutical product for injection comprising a container including a closure suitable for preparations for injection, the container containing an acid labile proton pump inhibitor, a salt thereof, a solvate of the acid labile proton pump inhibitor or a salt thereof, wherein the container and closure are made of material which essentially does not release zinc ions.08-20-2009
20090221645Dihydroimidazothiazole Derivatives - Compounds of formula (I) or pharmaceutically acceptable salts thereof, exhibit 5-HT09-03-2009
20090258909Novel Benzimidazole Derivatives Useful as Selective Androgen Receptor Modulators (SARMS) - The present invention is directed to novel benzimidazole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the androgen receptor.10-15-2009
200902537503-INDAZOLYL-4-PYRIDYLISOTHIAZOLES - The present invention provides 3-indazoyl-4-pyridylisothiazoles or a pharmaceutically acceptable salt thereof, pharmaceutical compositions thereof, and methods of using the same, as well as processes for preparing the same, and intermediates thereof.10-08-2009
20090258907COMPOUNDS USEFUL AS INHIBITORS OF ROCK KINASES - Disclosed herein are compounds of formula (I) or pharmaceutical acceptable salts thereof,10-15-2009
20100160382ANTI-ACID PHARMACEUTICAL COMPOSITION IN POWDER FORM AND PROCESS FOR MAKING IT - An anti-acid pharmaceutical composition for the rapid and prolonged neutralization of gastric acidity with mucosa-protecting activity in powder form to prepare, by dispersion in water, a pharmaceutical solution or suspension for oral use characterized in that the composition includes sodium alginate; an anti-acid soluble agent or a combination of anti-acids; an inhibitor of proton pump; diluent and sweetening agents, wherein a) at least 30% of sodium alginate present in the formulation along with the total of the inhibitor of proton pump are homogeneously distributed over the surface of the total soluble anti-acid agent [or] of the combination of anti-acids of the composition; and b) the rest, about 70%, of sodium alginate present in the formulation contains a percentage of humidity of less than 2%.06-24-2010
20100173944HELICOBACTER PYLORI ERADICATING AGENT HAVING INHIBITORY ACTIVITY ON GASTRIC ACID SECRETION - Disclosed are: a compound which is stable in an acid, has an antibacterial effect against a bacterium 07-08-2010
20100160381RAF Inhibitors for the Treatment of Thyroid Cancer - The invention relates to the use of an Raf inhibitor for the manufacture of pharmaceutical compositions for the treatment of thyroid cancer, more specifically papillary thyroid cancer (PTC); the use of a Raf inhibitor in the treatment of thyroid cancer, more specifically PTC; a method of treating warm-blooded animals including mammals, especially humans, suffering from thyroid cancer, more specifically PTC, by administering to a said animal in need of such treatment a dose effective against said disease of an Raf inhibitor. The invention also relates to the use of a Raf inhibitor in combination with a platin compound for the treatment of thyroid cancer, more specifically papillary thyroid cancer.06-24-2010
20090048302Methods and compositions for the treatment of conditions related to gastric acid secretion - A method comprising orally administering to a mammal a proton pump inhibitor, or a pharmaceutically acceptable prodrug thereof, and a compound which modulates the activity of the MRP2 or other transporter proteins involved in efflux of a proton pump inhibitor or a prodrug, is disclosed herein, said method being effective for the prevention or treatment of a disease or condition related to gastric acid secretion. This method applied to compounds which both inhibit and stimulate MRP2 activity or activity of other transporter proteins involved in efflux of a proton pump inhibitor or a prodrug.02-19-2009
20100184807Methods to inhibit tumor cell growth by using proton pump inhibitors - Methods of treating one or more growth deregulated cells are disclosed: An effective amount of a pharmaceutical composition including a proton pump inhibitor is administered thereby treating a growth deregulated cell outside of the gastric lumen of a subject.07-22-2010
20090143438Novel Pyridine Derivative Having Anti-Helicobacter Pylori Activity - The object is to provide an excellent pharmaceutical having an anti-06-04-2009
20130123305FUNGICIDE HYDROXIMOYL-TETRAZOLE DERIVATIVES - The present invention relates to hydroximoyl-tetrazole derivatives of formula (I), their process of preparation, their use as fungicide active agents, particularly in the form of fungicide compositions and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions.05-16-2013
20100227889Benzimidazole Derivatives - A compound of formula (I) or a pharmaceutically acceptable salt or prodrug ester thereof: wherein R, X and Y are as disclosed in the specification, suitable for the treatment of osteoporosis.09-09-2010
20100222391BENZIMIDAZOLE COMPOUND CRYSTAL - A novel crystal of (R)-2-[[[3-methyl-4-(2,2,2-trifluoroethoxy)-2-pyridinyl]methyl]sulfinyl]-1H-benzimidazole or a salt thereof of the present invention is useful for an excellent antiulcer agent.09-02-2010
20100216844Carboxamide compounds and their use as calpain inhibitors - The present invention relates to novel carboxamide compounds and their use as a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity and to a method for the therapeutic and/or prophylactic treatment by administering an effective amount of at least one of these carboxamide compounds.08-26-2010
20100227890POLYMORPHS OF ESOMEPRAZOLE SALTS - The present invention relates to a high assayed esomeprazole magnesium dihydrate substantially free of its trihydrate form. The present invention further provides an improved and commercially viable process for preparation of high assayed esomeprazole magnesium dihydrate substantially free of its trihydrate form. The present invention also provides an improved process for preparation of pure amorphous esomeprazole magnesium. The present invention further provides an improved and commercially viable process for preparation of substantially enantiomerically pure esomeprazole in neutral form or as a pharmaceutically acceptable salt or as its solvates including hydrates. The present invention also provides solid form of esomeprazole calcium salt, its polymorphs (form 1, form 2 and amorphous form) and processes for their preparation thereof.09-09-2010
20100227891THRESHOLD BLOOD OMEPRAZOLE CONCENTRATION IS 50 NG/ML FOR THE MAINTENANCE OF INTRAGASTRIC PH OF AT LEAST 4.0 AFTER ORAL DOSING WITH CMA-OMEPRAZOLE, AGN 201904-Z - Dosage forms of sodium {4-[5-Methoxy-2-(4-methoxy-3,5-dimethyl-pyridin-2-ylmethanesulfinyl)-benzoimidazole-1-sulfonyl]-phenoxy}-acetate, and methods of use of the dosage forms are disclosed herein.09-09-2010
201002407071,3,5-TRISUBSTITUTED TRIAZOLE DERIVATIVE - The present invention relates to 2-[3-(2,2-Difluoro-benzo[1,3]dioxol-5-ylamino)-5-(2,6-dimethyl-pyridin-4-yl)-[1,2,4]triazol-1-yl]-N-ethyl-acetamide and analogues or pharmaceutically acceptable salts thereof, processes for preparing them, pharmaceutical compositions containing them and their use in therapy.09-23-2010
20100144796NEW POLYMORPHS OF ETHYL 3-[(2-{[4-(HEXYLOXYCARBONYLAMINO-IMINO- METHYL)-PHENYLAMINO]-METHYL-1-METHYL-1H-BENZIMIDAZOLE-5-CARBONYL) -PYRIDIN-2-YL-AMINO]-PROPIONATE - The invention relates to new polymorphs of the active substance ethyl 3-[(2-{[4-(hexyloxycarbonylamino-imino-methyl)-phenylamino]-methyl}-1-methyl-1H-benzimidazole-5-carbonyl)-pyridin-2-yl-amino]-propionate, the preparation thereof and the use thereof as pharmaceutical compositions.06-10-2010
20100144795TREATMENT OF ATTENTION-DEFICIT/HYPERACTIVITY DISORDER - 3-(5,6-Dichloro-pyridin-3-yl)-1S,5S-3,6-diazabicyclo[3.2.0]heptane and salts thereof are effective nicotinic receptor agonist compounds that demonstrated pharmacological effect for symptoms associated with attention-deficit/hyperactivity disorder.06-10-2010
20110112147INDAZOLONE ANALOGS AS GLYCOGEN SYNTHASE ACTIVATORS - Provided herein are compounds of the formula (I):05-12-2011
20100222390Methods and Compositions for the Intravenous Administration of Compounds Related to Proton Pump Inhibitors - Disclosed herein are liquid compositions comprising a therapeutically effective concentration of a prodrug of a sulfonyl-containing proton pump inhibitor, wherein said compositions have a pH of from 3 to 7.3. Solid compositions related thereto are also disclosed. Methods of delivering a proton pump related thereto are also disclosed. Compositions comprising a second therapeutically active agent are also disclosed herein.09-02-2010
20120142737PHARMACEUTICAL COMPOSITIONS OF A NON-ENTERIC COATED PROTON PUMP INHIBITOR WITH A CARBONATE SALT AND BICARBONATE SALT COMBINATION - A method for treating gastric acid disorders with a non-enteric coated proton pump inhibitor in a pharmaceutically acceptable carrier including a bicarbonate salt of a Group IA metal and a carbonate salt of a Group IA metal; and a pharmaceutical composition of a non-enteric coated proton pump inhibitor in a pharmaceutically acceptable carrier including a bicarbonate salt of a Group IA metal and a carbonate salt of a Group IA metal are disclosed. A presently preferred proton pump inhibitor is lansoprazole, a presently preferred bicarbonate salt is sodium bicarbonate, and a presently preferred carbonate salt is sodium carbonate. The composition is a fast-acting formulation which reduces the undesirable belching associated with proton pump inhibitor formulations that contain high doses of sodium bicarbonate.06-07-2012
20120142738Pharmaceutical composition for treating dermatological autoimmune diseases - There is proposed a pharmaceutical composition for treating dermatological autoimmune diseases, comprising a proton pump inhibitor.06-07-2012
20090258908Crystalline S-Omeprazole Strontium Hydrate, Method For Preparing Same, And Pharmaceutical Composition Containing Same - This invention provides a crystalline S-omeprazole strontium hydrate for the prevention or treatment of gastric acid-related diseases, which has high optical purity, theremostability, solubility and nonhygroscopicity, a method for preparing same, and a pharmaceutical composition containing same.10-15-2009
20090170905SOLID FORMS OF 3-(6-(1-(2,2-DIFLUOROBENZO[D][1,3]DIOXOL-5-YL) CYCLOPROPANECARBOXAMIDO)-3-METHYLPYRIDIN-2-YL)BENZOIC ACID - The present invention relates to a substantially crystalline and free solid state form of 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid (Form I), pharmaceutical compositions thereof, and methods of treatment therewith.07-02-2009
20110118317Use of epothilones in the treatment of neuronal connectivity defects such as schizophrenia and autism - The present invention is about the use of at least one epothilone or derivative thereof as an active ingredient for manufacturing a medicament for use in the treatment of disease(s) involving a neuronal connectivity defect.05-19-2011
20090069384THIENOPYRROLES USEFUL IN THE TREATMENT OF INFLAMMATION - There is provided compounds of formula I: wherein the dotted lines, U5 V5 X03-12-2009
20110015232Pyrrolydine Derivatives as IAP Inhibitors - The present invention relates to novel IAP inhibitor compounds of: Formula (I).01-20-2011
20110039895PROLYL HYDROXYLASE INHIBITORS - The invention described herein relates to certain benzimidazol-4-ylcarboxamide derivatives of formula (I)02-17-2011
20130190358NOVEL ORALLY ADMINISTERED DABIGATRAN FORMULATION - The invention relates to a new medicament formulation of the active substance dabigatran etexilate of formula I07-25-2013
20110086883NOVEL BENZIMIDAZOLE DERIVATIVES USEFUL AS SELECTIVE ANDROGEN RECEPTOR MODULATORS (SARMS) - The present invention is directed to novel benzimidazole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the androgen receptor.04-14-2011
20110086884BARIUM SALT OF BENZIMIDAZOLE DERIVATIVE - The invention relates to crystalline barium salt of (S)-omeprazole, which is (S)-5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridinyl)-methyl]sulfinyl]-1H-benzimidazole. The invention also relates to processes for preparing crystalline barium salt of (S)-omeprazole and pharmaceutical compositions that include the crystalline barium salt of (S)-omeprazole so prepared.04-14-2011
20110086882PYRAZOLOTHIAZOLE COMPOUND - A compound represented by the formula (I) or pharmacologically acceptable salt thereof exhibits an excellent CRF receptor antagonism04-14-2011
20090203741CRYSTALS OF BENZOXADIAZOLE DERIVATIVE - Object Provided are β-form crystal, γ-form crystal, and α-form crystal of a benzoxadiazole derivative, wherein a uniform crystal having sufficient qualities can be obtained with high reproducibility, and they can be anytime supplied as crystals of drug substance for use in producing pharmaceuticals, are particularly suitable for mass synthesis in industrial production, hardly exhibit hygroscopicity and have particularly excellent photo-resistance.08-13-2009
20090036494Administration of Pharmaceuticals - A new administration regimen giving an extended plasma concentration profile of a H02-05-2009
20100063100MODULATORS OF ALDEHYDE DEHYDROGENASE ACTIVITY AND METHODS OF USE THEREOF - The present invention provides compounds that function as modulators of aldehyde dehydrogenase activity; and pharmaceutical compositions comprising the compounds. The present invention provides therapeutic methods involving administering a subject compound, or a subject pharmaceutical composition.03-11-2010
20110178131Compounds Which Have Activity At M1 Receptor And Their Uses In Medicine - Compounds of formula (I) or a salt thereof are provided:07-21-2011
20110178130MACROCYCLIC UREA AND SULFAMIDE DERIVATIVES AS INHIBITORS OF TAFIa - The invention relates to compounds of the formula (I) which are inhibitors of activated thrombin-activable fibrinolysis inhibitor. The compounds of the formula I are suitable for producing medicaments for prophylaxis, secondary prevention and treatment of one or more disorders associated with thromboses, embolisms, hypercoagulability or fibrotic changes.07-21-2011
20100056580NOVEL CRYSTALLINE SALT FORM OF AN ANTIDIABETIC COMPOUND - A novel crystalline anhydrous toluenesulfonic acid salt form of a selective PPAR gamma partial agonist which has a fused bicyclic aromatic group attached to an oxypropanoic acid moiety is stable and non-hygroscopic. The crystalline salt form is useful for making pharmaceutical formulations for the treatment of type 2 diabetes, hyperglycemia, obesity, and dyslipidemia.03-04-2010
20090215831INHIBITORS OF THE GASTRIC H+, K+-ATPASE WITH ENHANCED THERAPEUTIC PROPERTIES - Chemical syntheses and medical uses of novel inhibitors of the gastric H08-27-2009
20100063101NEW BENZIMIDAZOLE DERIVATIVES - The invention is concerned with novel benzimidazole derivatives of formula (I)03-11-2010
20110077273NEW BENZIMIDAZOLE DERIVATIVES - The present invention relates to compounds of formula (I),03-31-2011
20110071194Chemical Compounds 572 - Compounds of formula (I):03-24-2011
20100004291LIQUID DOSAGE FORMS OF NON-ENTERICALLY COATED ACID-LABILE DRUGS - Provided herein are formulations of acid labile drugs, such as proton pump inhibitors (PPI). The formulations comprise a PPI and a liquid vehicle typically having a pH greater than 6.5 and a viscosity sufficient to maintain a uniform suspension of the PPI for 15 minutes.01-07-2010
20120122933Compounds - The present invention relates to a novel crystalline form of esomeprazole sodium salt. Further, the present invention also relates to the use of the novel crystalline form for the treatment of gastrointestinal disorders, pharmaceutical compositions containing it as well as processes for the preparation of the novel crystalline form.05-17-2012
20080275091COMPOSITIONS AND METHODS FOR TREATING NOCTURNAL ACID BREAKTHROUGH AND OTHER RELATED DISORDERS - The present invention relates to, inter alia, pharmaceutical compositions comprising an acid labile proton pump inhibitor and a buffering agent; to methods for manufacture of such compositions, and to use of such compositions in treating and preventing diseases and/or disorders.11-06-2008
20080242703Pharmaceutical compositions for the treatment of hearing loss - The present invention provides a pharmaceutical composition for the treatment of hearing loss. The pharmaceutical composition of the present invention comprises a proton pump inhibitor (PPI), and is useful to decreasing acute or chronic hearing loss of patients related to the mutation or degenerative dysfunction of SLC26A4 gene.10-02-2008
20120277268SOLID FORMS OF 3-(6-(1-(2,2-DIFLUOROBENZO[D][1,3]DIOXOL-5-YL) CYCLOPROPANECARBOXAMIDO)-3-METHYLPYRIDIN-2-YL)BENZOIC ACID - The present invention relates to a substantially crystalline and free solid state form of 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid (Form I), pharmaceutical compositions thereof, and methods of treatment therewith.11-01-2012
20120277269METHOD FOR TREATING OR PREVENTING THROMBOSIS USING DABIGATRAN ETEXILATE OR A SALT THEREOF WITH IMPROVED EFFICACY OVER CONVENTIONAL WARFARIN THERAPY - A method for preventing stroke in a patient suffering from atrial fibrillation, wherein the patient has no risk factors for major bleeding events, the method comprising administering to the patient 150 mg b.i.d. of dabigatran etexilate, optionally in the form of a pharmaceutically acceptable salt thereof.11-01-2012
20080214618Gastric Therapies Amd Compositions Therefor - 1. A composition, in one or more parts, for the treatment of gastric and/or duodenal 09-04-2008
20100286209VINYL INDAZOLYL COMPOUNDS - The present invention provides vinyl indazolyl compounds useful in the treatment of cancer.11-11-2010
20100324095PHARMACEUTICAL COMPOSITION FOR INHIBITING AMYLOID-BETA PROTEIN ACCUMULATION - The present invention provides: a pharmaceutical composition for inhibiting amyloid-β protein accumulation comprising a compound of the formula (I) or a pharmaceutically acceptable salt thereof as an active ingredient; a method for inhibiting amyloid-β protein accumulation, comprising a step of administering an effective amount of the compound of the formula (I) or a pharmaceutically acceptable salt thereof to a mammal which may be diagnosed with an amyloid-β protein-related disease; and so on.12-23-2010
20120071514BENZOXAZOLONE DERIVATIVES AS ALDOSTERONE SYNTHASE INHIBITORS - The present invention provides a compound of formula I;03-22-2012
20100069441ANTIMICROBIAL INDOLINE COMPOUNDS FOR TREATMENT OF BACTERIAL INFECTIONS - The present invention provides indoline heterocyclic compounds of the following formula I:03-18-2010
20110190352USE OF DABIGATRANETEXILATE FOR TREATING PATIENTS WITH PULMONARY HYPERTENSION - The invention relates to a new use of dabigatran etexilate of formula (I), optionally in the form of the pharmaceutically acceptable salts thereof, as well as new medicament formulations which may be used for this purpose.08-04-2011
20110190351Benzoimidazole Derivatives and Glycogen Synthase Kinase-3 Beta Inhibitors Containing the Same - Benzoimidazole Derivatives are provided. The compounds of the present invention are useful for Glycogen Synthase Kinase-3 Beta Inhibitors.08-04-2011
20100016370PROCESS FOR THE PREPARATION OF ESOMEPRAZOLE MAGNESIUM IN A STABLE FORM - There is provided a process for preparing purified esomeprazole magnesium, comprising the steps of: providing esomeprazole magnesium; contacting said esomeprazole magnesium with a non-solvent comprising an aqueous component up to a maximum content defined by water saturation in the non-solvent; and recovering purified esomeprazole magnesium formed from the contacting step. The process is particularly suitable to obtain esomeprazole magnesium dihydrate, especially form A. The esomeprazole magnesium obtained is remarkably pure, stable and is resistant to form interchangeability.01-21-2010
20100016369AMINOTETRAHYDROINDAZOLOACETIC ACIDS - The invention is concerned with the compounds of formula I:01-21-2010
20080269297Process for the Preparation of Esomeprazole Non-Salt Form - The present invention relates to a new process for the preparation of new crystal modifications of esomeprazole non-salt form. Further, the present invention also relates to the use of said new crystal modifications for the treatment of gastrointestinal disorders, pharmaceutical compositions containing them as well as the crystal modifications, as such.10-30-2008
20100093805METHOD OF TREATING AMBLYOPIA - The present invention relates to a method of treating or alleviating the symptoms of amblyopia. It is based on the discovery that repeated administration of a specific drug, which is known to be clinically active to treat depression in humans, results in improved vision of the amblyopic eye.04-15-2010
20090203742BROADSPECTRUM 2-AMINO-BENZOTHIAZOLE SULFONAMIDE HIV PROTEASE INHIBITORS - The present invention relates to the use of 2-amino-benzothiazoles, having the formula08-13-2009
20090111856Parenteral Formulation Comprising Proton Pump Inhibitor Sterilized in its Final Container by Ionizing Radiation - The present invention relates to a stable sterilized parenteral formulation comprising an acid susceptible proton pump inhibitor. The formulation, a solid formulation comprising the acid susceptible proton pump inhibitor and optionally pharmaceutically acceptable excipients, has been sterilized in its final container by ionizing radiation. The container may consist of several compartments and separately contains a suitable solvent, which is sterilized, i.e. radiated, at the same time as the solid formulation. Alternatively, the suitable solvent is sterilized separately or aseptically manufactured. The solid formulation is dissolved in a suitable solvent before being administered to the patient, i.e. being prepared ex tempore. The present invention also relates to the prepared sterilized parenteral formulation, the stable solid formulation, processes for obtaining said parenteral formulation and the solid formulation as well as to the therapeutic uses thereof.04-30-2009
20110046184SOLID STATE FORMS OF RACEMIC ILAPRAZOLE - The invention relates to crystalline forms of racemic ilaprazole, 2[[(4-methoxy-3-methyl-2-pyridinyl)-methyl]sulfinyl]-5-(1H-pyrrol-1-yl) 1H-Benzimidazole. The invention also relates to a pharmaceutical composition for inhibiting gastric acid secretion comprising a crystalline Form of ilaprazole according to the invention in an amount effective to inhibit gastric acid secretion and a pharmaceutically acceptable carrier. The invention also provides methods of treatment for various acid-related gastrointestinal (GI) disorders.02-24-2011
20090042947PHARMACOLOGICALLY ACTIVE COMPOUNDS CONTAINING SULFUR - Disclosed herein is a method for the production of disulfide compounds of the formula (I) PAC-S02-12-2009
20100286208Novel polymorph of esomeprazole potassium and process for its preparation - Disclosed is a novel potassium salt of esomeprazole in polymorph form X, which can be used in pharmaceutical compositions. Processes for preparing polymorph form X of esomeprazole potassium are also provided.11-11-2010
20110306640DABIGATRAN IN TUMOUR THERAPY - The invention relates to the use of dabigatran etexilate of Formula (I) optionally in the form of the pharmaceutically acceptable salts thereof, as well as new medicament formulations for the treatment of tumours.12-15-2011
20100010046PHARMACEUTICAL FORMULATION FOR PARENTERAL ADMINISTRATION - Parenteral formulations comprising ketorolac, and a compound of formula II wherein R is hydrogen or lower alkyl. Such formulations are used for the treatment and prevention of pain.01-14-2010
20110082174SOLID STATE FORMS OF RACEMIC ILAPRAZOLE - The invention relates to crystalline forms of racemic ilaprazole, 2[[(4-methoxy-3-methyl-2-pyridinyl)-methyl]sulfinyl]-5-(1H-pyrrol-1-yl) 1H-Benzimidazole. The invention also relates to a pharmaceutical composition for inhibiting gastric acid secretion comprising a crystalline Form of ilaprazole according to the invention in an amount effective to inhibit gastric acid secretion and a pharmaceutically acceptable carrier. The invention also provides methods of treatment for various acid-related gastrointestinal (GI) disorders.04-07-2011
20090099237Methods of treating inflammatory diseases - Methods relating to selective inhibitors of the casein kinase 1 isoforms that are useful for the treatment of inflammatory diseases are presented.04-16-2009
20120041030PYRIDINE THIO DERIVATIVE, AND PHARMACEUTICAL COMPOSITION WHICH CONTAINS SAME AND HAS ANTI-HELICOBACTER PYLORI ACTION - Disclosed are a novel pyridine thio derivative, and a pharmaceutical composition using the novel pyridine thio derivative, particularly a pharmaceutical composition having selective antibacterial activity against 02-16-2012
20100331371METHYL-BENZIMIDAZOLE DERIVATIVES - The invention is concerned with novel substituted benzimidazole derivatives of formula (I)12-30-2010
20120065233TYROSINE KINASE INHIBITORS - The present disclosure relates to the field of tyrosine kinase enzyme inhibition, in particular anaplastic lymphoma kinase (ALK) inhibition using novel small molecules. Provided are compounds capable to modulate ALK activity, compositions that comprise the compounds, and methods of using the compounds for the treatment or prevention of diseases or conditions that are characterized by ALK activity or expression.03-15-2012
20100016368AMINOTETRAHYDROINDAZOLOACETIC ACIDS - The invention is concerned with the compounds of formula I:01-21-2010
20080214620NOVEL INHIBITORS OF GLUTAMINYL CYCLASE - The present invention relates to compounds of formula (I), combinations and uses thereof for disease therapy,09-04-2008
20110028518DEXLANSOPRAZOLE PROCESS AND POLYMORPHS - Processes for the preparation of dexlansoprazole, an amorphous form of dexlansoprazole, a solid dispersion of amorphous dexlansoprazole and a pharmaceutically acceptable carrier, and processes for their preparation. Also provided are crystalline compounds 2-[(R)-[(4-chloro-3-methyl-2-pyridinyl)methyl]sulfinyl]-1H-benzimidazole and 2-[(R)-[(4-nitro-3-methyl-2-pyridinyl)methyl]sulfinyl]-1H-benzimidazole, and methods for their preparation.02-03-2011
20090076089DEUTERIUM-ENRICHED PANTOPRAZOLE - The present application describes deuterium-enriched pantoprazole, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.03-19-2009
20120046319PROCESS FOR THE PREPARATION OF ENANTIOMERICALLY ENRICHED PROTON PUMP INHIBITORS - The invention discloses a process for the preparation of compounds having structures typical for proton pump inhibitors in enantiomerically enriched form by using particular metal catalysts in an enantioselective oxidation step. Also disclosed are useful further processes and pure intermediate and subsequently final products.02-23-2012
20120010248Mitochondrial Aldehyde Dehydrogenase-2 Modulators and Methods of Use Thereof - The present invention provides compounds that function as modulators of mitochondrial aldehyde dehydrogenase-2 (ALDH2) activity; and pharmaceutical compositions comprising the compounds. The present invention provides therapeutic methods involving administering a subject compound, or a subject pharmaceutical composition. The present invention further provides assays for identifying agonists of ALDH2.01-12-2012
20090182014INSECTICIDAL COMPOSITIONS COMPRISING COMPOUNDS HAVING INHIBITORY ACTIVITY VERSUS ACYL COA: CHOLESTEROL ACYLTRANSFERASE OR SALTS THEREOF AS EFFECTIVE INGREDIENTS - The present invention relates to insecticidal compositions comprising compounds having an inhibitory activity versus acyl CoA: cholesterol acyltransferase (ACAT) or salts thereof as effective ingredients. The compounds having inhibitory activity versus ACAT have an excellent insecticidal effect by inhibiting sterol metabolism in noxious insects. Therefore, the compounds of the present invention can be used as safe and effective insecticides.07-16-2009
20110166183PROCESS FOR PREPARATION OF ESOMEPRAZOLE SODIUM OF HIGH CHEMICAL PURITY AND NEW FORMS OF ESOMEPRAZOLE SODIUM - A process for preparing esomeprazole sodium comprises the steps of providing a solution of esomeprazole sodium in a solvent constituted mainly of methanol or only of methanol; and carrying out precipitation or crystallisation of esomeprazole sodium from said solution. Esomeprazole sodium is preferably obtained from pure form of neutral racemate through chiral chromatography using methanol-based mobile phase, and a subsequent reaction with sodium source. Novel crystal and semicrystal forms of esomeprazole sodium can be provided repeatedly and in physically stable and highly pure form.07-07-2011
20090062347DEUTERIUM-ENRICHED AXITINIB - The present application describes deuterium-enriched axitinib, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.03-05-2009
20110046183CRYSTAL OF BENZIMIDAZOLE COMPOUND - Provided is a crystal of (R)-2-[[[3-methyl-4-(2,2,2-trifluoroethoxy)-2-pyridinyl]methyl]sulfinyl]-1H-benzimidazole showing an X-ray powder diffraction pattern having characteristic peaks at interplanar spacings (d) of 10.06±0.2, 8.70±0.2, 6.57±0.2, 5.59±0.2 and 4.00±0.2 Angstroms. The present invention provides a stable antiulcer drug superior in the absorbability.02-24-2011
20110046182EFFICIENT ASPIRIN PRODRUGS - Aspirin is one of the most widely used drugs in the treatment of inflammation, pain and fever. It has more recently found application in the prevention of heart attacks and stroke and is being studied as a cancer chemopreventative agent. Despite its value aspirin continues to be underutilized because it causes gastric bleeding. The technology under development potentially removes this problem. It is designed to reduce contact between the drug and the intestinal lining. An isosorbide aspirinate prodrug compound is thus provided. The compound has the general structure as shown in general formula (I) wherein Y is a C02-24-2011
20110092546SUBSTITUTED BENZIMIDAZOLES FOR NEUROFIBROMATOSIS - The present invention relates to the use of BENZIMIDAZOLE DERIVATIVES for the preparation of a drug for the treatment of neurofibromatosis.04-21-2011
20110092545Compounds, Compositions and Methods for Stabilizing Transthyretin and Inhibiting Transthyretin Misfolding - Compounds, compositions and methods are provided for stabilizing transthyretin and for treating, preventing, or ameliorating one or more symptoms of transthyretin mediated diseases. In one embodiment, the compounds are benzoxazoles and related compounds.04-21-2011
20100093804 NOVEL CRYSTALLINE FORM OF LANSOPRAZOLE - The present invention relates to a novel and stable crystalline polymorph of lansoprazole, a process for its preparation and to a pharmaceutical composition comprising it. Thus, for example, lansoprazole crude is dissolved in methanol at 20-30° C. followed by stirring and the solution is cooled to 0-10° C. The resulting solution is stirred for 1 hour to 1 hour 30 minutes at 0-10° C., the solid is filtered and then dried to give lansoprazole crystalline form III.04-15-2010
20090131481Transcription Factor Modulating Compounds and Methods of Use Thereof - Substituted benzimidazole compounds useful as anti-infectives that decrease resistance, virulence, or growth of microbes are provided. Methods of using substituted benzimidazole compounds, in, e.g., reducing virulence and infectivity, inhibiting biofilms and treating bacterial infections are also provided.05-21-2009
20090131482METHYL-BENZIMIDAZOLE DERIVATIVES - The invention is concerned with novel substituted benzimidazole derivatives of formula (I)05-21-2009
20110184024Pharmaceutical Composition Containing Esomeprazole - The present invention relates to esomeprazole free base or its alkali salt-containing composition which stability is improved and is easy to manufacture.07-28-2011
20100173945Compounds with nootropic action, their preparation, pharmaceutical compositions containing them, and use thereof - Described herein are new bicyclic arylimidazolones having nootropic action (i.e., protecting and stimulating cerebral functions), analgesic action and anti hyperalgesic action; also described is the process for their preparation and pharmaceutical compositions comprising them, useful for the treatment of cognitive deficits, and of various types of pain.07-08-2010
20100173946BENZIMIDAZOLYLIDENE PROPANE-1,3-DIONE DERIVATIVE OR SALT THEREOF - Compounds useful as GnRH receptor antagonists are provided. The present inventors have further examined propane-1,3-dione derivatives and confirmed as a result that a propane-1,3-dione having 2-(1,3-dihydro-2H-benzimidazol-2-ylidene), or a compound which has benzene or thiophene ring substituted with a group derived from 1-hydroxymethyl, shows excellent availability, in addition to its excellent GnRH receptor antagonism, thereby accomplishing the invention. Since the compound of the invention shows excellent availability, in addition to its strong GnRH receptor antagonism, it can be expected that it exerts superior drug effect in the living body, and it is useful for the treatment of sex hormone dependent diseases such as prostate cancer, breast cancer, endometriosis, uterine leiomyoma, benign prostatic hypertrophy and the like. In addition, since the compound of the invention is excellent in metabolic stability in human and also is less in drug interaction, it has more desirable properties as a medicament to be used for the aforementioned diseases.07-08-2010
20100173947New Indications for Direct Thrombin Inhibitors - The invention relates to new indications for direct thrombin inhibitors such as dabigatran etexilate in the CNS and other fields.07-08-2010
20120252847NOVEL FORM OF S-OMEPRAZOLE - The present invention relates to a novel form of the (−)-enantiomer of 5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridinyl)-methyl]sulfinyl]-110-04-2012
20120252848LIQUID DOSAGE FORMS OF NON-ENTERICALLY COATED ACID-LABILE DRUGS - Provided herein are formulations of acid labile drugs, such as proton pump inhibitors (PPI). The formulations comprise a PPI and a liquid vehicle typically having a pH greater than 6.5 and a viscosity sufficient to maintain a uniform suspension of the PPI for 15 minutes.10-04-2012
20120214846HEXAHYDROCYCLOPENTYL[F]INDAZOLE PYRIDYL ETHANOLS AND DERIVATIVES THEREOF AS SELECTIVE GLUCOCORTICOID RECEPTOR MODULATORS - The present invention encompasses compounds of Formula (I): or pharmaceutically acceptable salts or hydrates thereof, which are useful as selective glucocorticoid receptor ligands for treating a variety of autoimmune and inflammatory diseases or conditions. Pharmaceutical compositions and methods of use are also included.08-23-2012
201202148472-[1-PHENYL-5-HYDROXY-4a-SUBSTITUTED-HEXAHYDROCYCLOPENTA[F]INDAZOL-5-YL]ET- HYL PHENYL DERIVATIVES AS GLUCOCORTICOID RECEPTOR LIGANDS - The present invention encompasses compounds of Formula I: or pharmaceutically acceptable salts or hydrates thereof, which are useful as selective glucocorticoid receptor ligands for treating a variety of autoimmune and inflammatory diseases or conditions. Pharmaceutical compositions and methods of use are also included.08-23-2012
20100273831FLUORO ALKYL SUBSTITUTED BENZIMIDAZOLE CANNABINOID AGONISTS - The present invention is related to novel benzimidazole compounds of formula (I) having cannabinoid receptor agonistic properties, pharmaceutical compositions comprising these compounds, chemical processes for preparing these compounds and their use in the treatment of diseases linked to the mediation of the cannabinoid receptors in animals, in particular humans.10-28-2010
20100273830NOVEL INSECTICIDES - An insecticidal compound of formula (I) in which G10-28-2010
20100010047Isotopically substituted proton pump inhibitors - The invention relates to compounds of formula 101-14-2010
20100292276BENZIMIDAZOLE DERIVATIVES USEFUL AS TRP M8 RECEPTOR MODULATORS - The present invention is directed to benzimidazole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by TRP M8 (transient receptor potential M8 channel). More particularly, the compounds of the present invention are useful in the treatment of inflammatory pain, inflammatory hyperalgesia, inflammatory hypersensitivity condition, neuropathic pain, neuropathic cold allodynia, inflammatory somatic hyperalgesia, inflammatory visceral hyperalgesia, cardiovascular disease aggravated by cold, anxiety and depression.11-18-2010
20120220634Taxane Compounds, Compositions And Methods - The present invention provides a method for the preparation of orally available pentacyclic taxane compounds, as well as intermediates useful in their preparation.08-30-2012
201200835133-Substituted-8-Substituted-3H-Imidazo[5,1-d][1,2,3,5]tetrazin-4-one Compounds and Their Use - The present invention pertains generally to the field of therapeutic compounds, and more specifically to 3-substituted-8-substituted-3H-imidazo[5,1-d][1,2,3,5]tetrazin-4-one compounds of the following formula, wherein -A and —B are as defined herein (collectively referred to herein as 38TM compounds):04-05-2012
20120083511CRYSTALLINE (R)-(E)-2-(4-(2-(5-(1-(3,5-DICHLOROPYRIDIN-4-YL)ETHOXY)-1H-INDAZOL-3-YL)V- INYL)-1H-PYRAZOL-1-YL)ETHANOL - The present invention provides crystalline (R)-(E)-2-(4-(2-(5-(1-(3,5-dichloropyridin-4-yl)ethoxy)-1H-indazol-3-yl)vinyl)-1H-pyrazol-1-yl)ethanol useful in the treatment of cancer.04-05-2012
20120225909INDAZOLE ANALOG - [Objective] To provide a drug that selectively stimulates the β3-adrenergic receptors, particularly a drug capable of preferentially stimulating the β3-adrenergic receptors over the α1-adrenergic receptors. This drug can be used in the treatment and prevention of diabetes, obesity, hyperlipidemia, depression, cholelithiasis, diseases caused by biliary hyperkinesia, diseases caused by hyperfunction of the gastrointestinal tract, interstitial cystitis, overactive bladder or urinary incontinence, diseases associated with decreased lacrimation, and the like.09-06-2012
20080287502Transdermal Administration of Proton Pump Inhibitors - A method and composition for the transdermal administration of proton pump inhibitors such as substituted pyridyl methylsulfinyl benzimidazoles, and in particular, omeprazole, lansoprazole, esomeprazole, pantoprazole and raberprazole. The method and composition include the use of a hydroxide-releasing agent as a permeation enhancer to increase the flux of the protein pump inhibitor through a patient's skin or mucosal tissues and optionally also include the use of a carrier such as 1,3-butanediol, dipropylene glycol, and hexylene glycol.11-20-2008
20120270905FLUORINATED 2,6-DIALKYL-3,5-DICYANO-4-(1H-INDAZOL-5-YL)-1,4-DIHYDROPYRIDINES AND METHODS OF USE THEREOF - The present invention relates to novel fluorinated 2,6-dialkyl-3,5-dicyano-4-(1H-indazol-5-yl)-1,4-dihydropyridine derivatives having protein tyrosine kinase inhibitory activity, to a process for the manufacture thereof and to the use thereof for the treatment of c-Met-mediated diseases or c-Met-mediated conditions, particularly cancer and other proliferative disorders.10-25-2012
20120322830Cyclourea Compounds as Calcium Channel Blockers - The invention relates to cyclourea compounds of Formula I: or a pharmaceutically acceptable salt or solvate thereof, wherein R12-20-2012
20100234430METHODS AND PHARMACEUTICAL FORMULATIONS FOR PROTECTING PHARMACEUTICAL COMPOUNDS FROM ACIDIC ENVIRONMENTS - Methods and pharmaceutical compositions for protecting pharmaceutical compounds (or drugs) in acidic environments are provided. Methods of treatment using formulations capable of protecting pharmaceutical compounds in acidic environments are also provided. Formulations provided generally comprise a therapeutically effective amount of at least one pharmaceutical compound, and a pharmaceutically acceptable protectant. The pharmaceutically acceptable protectant of the invention generally comprises a water-soluble acid neutralizer, and a water-insoluble acid neutralizer.09-16-2010
20090298885METHYLENE UREA DERIVATIVES - The present invention relates to methylene urea derivatives of formula (I), the use of the compounds of formula (I) as inhibitors of raf-kinase, the use of the compounds of formula (I) for the manufacture of a pharmaceutical composition and a method of treatment, comprising administering said pharmaceutical composition to a patient.12-03-2009
20100204279Therapeutic Salt Compositions and Methods - Therapeutic salt compositions and methods are disclosed herein.08-12-2010
20100168181BENZIMIDAZOLE AMIDO DERIVATIVES, THEIR MANUFACTURE AND USE AS PHARMACEUTICAL AGENTS - Objects of the present invention are the compounds of formula (I) their pharmaceutically acceptable salts, enantiomeric forms, diastereoisomers and racemates, the preparation of the above-mentioned compounds, medicaments containing them and their manufacture, as well as the use of the above-mentioned compounds in the control or prevention of illnesses such as cancer.07-01-2010
20110306641NOVEL 2,6-SUBSTITUTED-3-NITROPYRIDINE DERIVATIVE, METHOD FOR PREPARING SAME, AND PHARMACEUTICAL PREPARATION INCLUDING SAME - The present invention relates to a novel 2,6-substituted-3-nitropyridine derivative compound, a method for preparing same, a pharmaceutical composition for prevention and treatment of osteoporosis including same, applications of same for preparing the therapeutic agent of osteoporosis prevention and treatment, and a method for prevention and treatment of osteoporosis using same. The 2,6-substituted-3-nitropyridine derivative compound of the present invention effectively increases osteoblast activity and also inhibits the formation of osteoclasts, so that it may be usefully used for the prevention and treatment of osteoporosis.12-15-2011
20110319450BENZIMIDAZOLE COMPOUND CRYSTAL - A novel crystal of (R)-2-[[[3-methyl-4-(2,2,2-trifluoroethoxy)-2-pyridinyl]methyl]sulfinyl]-1H-benzimidazole or a salt thereof of the present invention is useful for an excellent antiulcer agent.12-29-2011
20120101131Aminotetrahydroindazoloacetic Acids - The invention is concerned with the compounds of formula I:04-26-2012
20100168180Novel Compounds - A compound for use in the treatment of proliferative disorders, such as cancer, having the following formula:07-01-2010
20130018074NEW COMPOUNDS - The present invention provides organic compounds of the following structure; A-L1-B—C-D-L2-E that are useful for treating or preventing conditions or disorders associated with DGAT1 activity in animals, particularly humans.01-17-2013
201300235662-(1,2-BENZISOXAZOL-3-YL)BENZYLAMINE DERIVATIVES - The invention relates to 2-(1,2-benzisoxazol-3-yl)benzylamine derivatives having the general Formula (I) wherein R01-24-2013
20130023567Novel Compounds - A compound for use in the treatment of proliferative disorders, such as cancer, having the following formula:01-24-2013
20080255200SUBSTITUTED BENZIMIDAZOLES - Disclosed herein are substituted benzimidazole-based proton pump modulators of Formula I, processes of preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.10-16-2008
20080255199Compounds Useful for the Synthesis of S- and R-Omeprazole and a Process for Their Preparation - The present invention relates to an improved method for the synthesis of the (S)- or (R)-enantiomer of omeprazole, characterized in that 2-[[(4-X-3,5-dimethylpyridin-2-yl)methyl]thio]-5-methoxy-1H-benzimidazole or 2-[[(4-X-3,5-dimethyl-1-ox-idopyridin-2-yl) methyl]thio]-5-methoxy-1H-benzimidazole, wherein X is a leaving group, is oxidized into the corresponding sulphoxide which is obtained as a crystalline compound. Recrystallisation of the thus obtained sulphoxide results in a compound of enhanced chemical and optical purity, which is subsequently transformed into the (S)- or (R)-enantiomer of omeprazole.10-16-2008
20130172389BENZIMIDAZOLE DERIVATIVES AS SELECTIVE BLOCKERS OF PERSISTENT SODIUM CURRENT - The present invention is directed to a compound of Formula I07-04-2013
20080234327DIHYDROINDAZOLE COMPOUNDS USEFUL IN TREATING IRON DISORDERS - This invention is directed to compounds of formula (I):09-25-2008
20080234326Novel Salts of Pantoprazole and (S) - Pantoprazole - The invention relates to pantoprazole and (S)-pantoprazole salts and to medicaments comprising these compounds.09-25-2008
20080234325Novel Methods Using Pyridine Derivatives - The invention provides methods of treating and preventing asthma, laryngitis, symptomatic gastroesophageal reflux disease, pregnancy-induced gastroesophageal reflux disease, noncardiac chest pains, coughing, apnea, dyspepsia, inflammatory bowel disease, irritable bowel syndrome, gastritis, stress ulcers, bleeding peptic ulcers, acute gastrointestinal bleeding, infectious enteritis, collagenous colitis, lymphocytic colitis, chronic diarrhea in immunocompromised patients, esophageal ulcers in immunocompromised patients, idiopathic gastric acid hypersecretion, gastroparesis, gastrointestinal motility disorders, Zollinger-Ellison syndrome, short bowel syndrome, emesis, regurgitation, early satiety, chronic sore throat, abdominal pain, abdominal bloating, nausea, sour stomach, diarrhea, constipation, bacterial infections, refractory ulcers, gastrointestinal disorders induced by NSAIDs, Barrett's esophagus, gastrointestinal disorders caused by steroids, gastrointestinal disorders induced by cholinergic compounds, and fungal or viral-induced ulcers in the gastrointestinal tract by administering a therapeutically effective amount of at least one of the pyridine derivatives of the invention to a patient in need thereof. The invention also provides on demand relief of symptoms associated with gastroesophageal reflux disease (GERD), and provides relief from symptoms caused by the consumption of excessive amounts of food and/or alcohol by administering a therapeutically effective amount of at least one of the pyridine derivatives of the invention to a patient in need thereof. The invention also provides methods for treating parasitic infections, such as malaria, by administering a therapeutically effective amount of at least one of the pyridine derivatives of the invention to a patient in need thereof. In preferred embodiments, the pyridine derivative of the invention is rabeprazole, a pharmaceutically acceptable salt thereof, or a stereoisomer thereof.09-25-2008
20080227822SUBSTITUTED THIENOPYRROLE CARBOXYLIC ACID AMIDES, PYRROLOTHIAZOLE CARBOXYLIC ACID AMIDES, AND RELATED ANALOGS AS INHIBITORS OF CASEIN KINASE I - The present invention comprises methods for the treatment of central nervous system diseases and disorders including mood disorders and sleep disorders through the administration of compounds of formula (I) and formula (II)09-18-2008
20080227821N-SUBSTITUTED TRICYCLIC 3-AMINOPYRAZOLES AS ANTI-MITOTIC TUBULIN POLYMERIZATION INHIBITORS - The invention is directed to compounds having the following structures:09-18-2008
20080227820CYCLIC PHENYL-SUBSTITUTED INDAZOLS, A PROCESS FOR THEIR PRODUCTION AND THEIR USE AS ANTI-INFLAMMATORY AGENTS - The present invention relates to the compounds of formula I,09-18-2008
20130178500HEXAHYDROPYRROLO[3,4-b]PYRROLE DERIVATIVES, PREPARATION METHODS AND PHARMACEUTICAL USES THEREOF - Hexahydropyrrolo[3,4-b]pyrrole derivatives, preparation methods and pharmaceutical uses thereof are provided. Specifically, dipeptidyl peptidase IV inhibitors presented by following formula (I) are provided. Such compounds can be used for treating or preventing the diseases associated with dipeptidyl peptidase IV, such as diabetes, obesity and hyperlipemia. The compounds presented by formula (I) and pharmaceutically acceptable salts thereof, a method for preparing a pharmaceutical composition thereof and their uses in the manufacture of medicaments for treating or preventing the disease associated with dipeptidyl peptidase IV are provided.07-11-2013
20130203816PROLYL HYDROXYLASE INHIBITORS AND METHODS OF USE - The present disclosure relates to HIF-1α prolyl hydroxylase inhibitors, compositions which comprise the HIF-1α prolyl hydroxylase inhibitors described herein and to methods for controlling, inter alia, Peripheral Vascular Disease (PVD), Coronary Artery Disease (CAD), heart failure, ischemia, and anemia.08-08-2013
20110269798PRECURSOR PHASE AND USE THEREOF FOR PREPARING THE MAGNESIUM TETRAHYDRATE SALT OF AN OMEPRAZOLE ENANTIOMER - A precursor phase of the magnesium tetrahydrate salt of an omeprazole enantiomer, and also processes for preparing it and its use for the preparation of the magnesium tetrahydrate salt are described. Crystals of the magnesium tetrahydrate salt thus obtained, and their uses, especially in the synthesis of the dihydrate form A of the magnesium salt of the enantiomer or as medicament are also disclosed.11-03-2011
20110269799METHOD FOR TREATING OR PREVENTING THROMBOSIS USING DABIGATRAN ETEXILATE OR A SALT THEREOF WITH IMPROVED EFFICACY OVER CONVENTIONAL WARFARIN THERAPY - A method for preventing stroke in a patient suffering from atrial fibrillation, wherein the patient has no risk factors for major bleeding events, the method comprising administering to the patient 150 mg b.i.d. of dabigatran etexilate, optionally in the form of a pharmaceutically acceptable salt thereof.11-03-2011
20080200517CRYSTALLINE FORMS OF SOLVATED ILAPRAZOLE - The invention relates to crystalline forms of various solvates of ilaprazole, 2[[(4-methoxy-3-methyl-2-pyridinyl)-methyl]sulfinyl]-5-(1H-pyrrol-1-yl) 1H-Benzimidazole. The invention also relates to a pharmaceutical composition for inhibiting gastric acid secretion comprising crystalline ilaprazole hydrate according to the invention in an amount effective to inhibit gastric acid secretion and a pharmaceutically acceptable carrier. The invention also provides methods of treatment for various acid-related gastrointestinal (GI) disorders.08-21-2008
20080200516SOLID STATE FORMS OF RACEMIC ILAPRAZOLE - The invention relates to crystalline forms of racemic ilaprazole, 2[[(4-methoxy-3-methyl-2-pyridinyl)-methyl]sulfinyl]-5-(08-21-2008
20080200515SOLID STATE FORMS OF ENANTIOPURE ILAPRAZOLE - The invention relates to solid state forms of enantiopure ilaprazole, 2[[(4-methoxy-3-methyl-2-pyridinyl)-methyl]sulfnyl]-5-(1H-pyrrol-1-yl) 1H-Benzimidazole. The invention also relates to a pharmaceutical composition for inhibiting gastric acid secretion comprising a solid form of ilaprazole according to the invention in an amount effective to inhibit gastric acid secretion and a pharmaceutically acceptable carrier. The invention also provides methods of treatment for various acid-related gastrointestinal (GI) disorders such as those discussed above.08-21-2008
20080200514Indications for Direct Thrombin Inhibitors - The invention relates to new indications for direct thrombin inhibitors such as dabigatran etexilate in the CNS and other fields.08-21-2008
20110224259NOVEL INHIBITORS - The invention relates to novel heterocyclic derivatives as inhibitors of glutaminyl cyclase (QC, EC 2.3.2.5). QC catalyzes the intramolecular cyclization of N-terminal glutamine residues into pyroglutamic acid (5-oxo-prolyl, pGlu*) under liberation of ammonia and the intramolecular cyclization of N-terminal glutamate residues into pyroglutamic acid under liberation of water.09-15-2011
20110275676Triazole-substituted anthranilamides as pesticides - The present invention constitutes new, triazole-substituted anthranilamides of the general formula (I),11-10-2011
20110237628CYCLOPENTYL- AND CYCLOHEPTYLPYRAZOLES - This invention relates to novel cyclopentyl- and cycloheptylpyrazole derivatives of the formula I09-29-2011
20130150413BENZISOTHIAZOL-3(1H)-ONE-5-SULFONYL DERIVATIVES AS CHEMOKINE RECEPTOR MODULATORS - The present invention relates to novel benzisothiazol-3(1H)-one-5-sulfonyl derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.06-13-2013
20100298383NOVEL BENZIMIDAZOLE DERIVATIVES USEFUL AS SELECTIVE ANDROGEN RECEPTOR MODULATORS (SARMS) - The present invention is directed to novel benzimidazole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the androgen receptor.11-25-2010
20120283297OXADIAZOLE SUBSTITUTED INDAZOLE DERIVATIVES FOR USE AS SPHINGOSINE 1-PHOSPHATE 1 (S1P1) RECEPTOR AGONISTS - Oxadiazole substituted indazole derivatives of formula (I) or pharmaceutical salts thereof having pharmacological activity, processes for their preparation, pharmaceutical compositions containing them and their uses in the treatment of various disorders mediated by S1P1 receptors are disclosed.11-08-2012
20120283296PYRROLOPYRAZOLES FOR TREATING CNS DISORDERS - Provided herein are methods of utilizing PAK inhibitors for the treatment of CNS disorders.11-08-2012
20120283295INDAZOLE DERIVATIVES AND THEIR USE FOR BLOCKADING VOLTAGE DEPENDENT SODIUM CHANNELS - The invention provides an indazole derivative of formula (1), or a pharmaceutically acceptable salt or N-oxide thereof, wherein R11-08-2012
20110313002TRICYCLIC COMPOUNDS - The present invention provides novel compounds of formula I,12-22-2011
20110313001TRIAZOLE DERIVATIVES FOR TREATMENT OF ALZHEIMER'S DISEASE - According to the invention there is provided a compound of formula (I): (I) or a pharmaceutically acceptable salt or hydrate thereof; wherein the variables are as defined herein. The compounds selectively attenuate the production of Aβ42 and hence are useful in treatment of Alzheimer's disease and related conditions.12-22-2011
20130190359BRIDGED HETEROCYCLIC COMPOUNDS AND METHODS OF USE - This disclosure relates to new compounds that may be used to modulate a histamine receptor in an individual. Novel compounds are described, including new bridged heterocyclic [4,3-b]indole compounds. Pharmaceutical compositions are also provided. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.07-25-2013
20130190360Compositions Containing a Pyripyropene Insecticide and an Adjuvant - Pesticidal composition containing a pyripyropene insecticide and an adjuvant07-25-2013
20130190357COMPOSITIONS AND METHODS FOR ASSESSING AND TREATING A PRECURSOR LESION AND/OR ESOPHAGEAL CANCER - One aspect of the present disclosure relates to a method for predicting a subject's risk of developing an esophageal cancer, a precursor lesion, or both. One step of the method includes obtaining a biological sample from the subject. Next, the presence of at least one germline mutation is determined in the biological sample. The subject is at an increased risk of an esophageal cancer, a precursor lesion, or both, where the presence of at least one germline mutation is determined.07-25-2013
20120029026PYRIDINE DERIVATIVE - The present invention relates to a novel pyridine derivative or a pharmacologically acceptable ester thereof, or a pharmacologically acceptable salt of the derivative or ester, which has an excellent hypoglycemic effect or treats and/or prevents the onset of a disorder of carbohydrate or lipid metabolism or a disease mediated by peroxisome proliferator-activated receptor (PPAR) γ. A compound represented by the general formula (I):02-02-2012
20120046320BETA- AND GAMMA-DIKETONES AND GAMMA-HYDROXYKETONES AS WNT/BETA-CATENIN SIGNALING PATHWAY ACTIVATORS - The present invention discloses β-diketones, γ-diketones or γ-hydroxyketones or analogs thereof, that activate Wnt/β-catenin signaling and thus treat or prevent diseases related to signal transduction, such as osteoporosis and osteoarthropathy; osteogenesis imperfecta, bone defects, bone fractures, periodontal disease, otosclerosis, wound healing, craniofacial defects, oncolytic bone disease, traumatic brain injuries related to the differentiation and development of the central nervous system, comprising Parkinson's disease, strokes, ischemic cerebral disease, epilepsy, Alzheimer's disease, depression, bipolar disorder, schizophrenia; eye diseases such as age related macular degeneration, diabetic macular edema or retinitis pigmentosa and diseases related to differentiation and growth of stem cell, comprising hair loss, hematopoiesis related diseases and tissue regeneration related diseases.02-23-2012
20120083512PHARMACEUTICAL PRODUCT FOR INJECTION - The claimed subject matter is related to a pharmaceutical product for injection comprising a container including a closure suitable for preparations for injection, the container containing an acid labile proton pump inhibitor, a salt thereof, a solvate of the acid labile proton pump inhibitor or a salt thereof, wherein the container and closure are made of material which essentially does not release zinc ions.04-05-2012
20120095055HEXAHYDROCYCLOPENTYL[f]INDAZOLE 5-HYDROXYMETHYL ETHANOLS AND DERIVATIVES THEREOF AS SELECTIVE GLUCOCORTICOID RECEPTOR MODULATORS - The present invention encompasses compounds of Formula (I): or pharmaceutically acceptable salts or hydrates thereof, which are useful as selective glucocorticoid receptor ligands for treating a variety of autoimmune and inflammatory diseases or conditions. Pharmaceutical compositions and methods of use are also included.04-19-2012
20120095054POLYMORPHS OF ESOMEPRAZOLE SALTS - The present invention relates to a high assayed esomeprazole magnesium dihydrate substantially free of its trihydrate form. The present invention further provides an improved and commercially viable process for preparation of high assayed esomeprazole magnesium dihydrate substantially free of its trihydrate form. The present invention also provides an improved process for preparation of pure amorphous esomeprazole magnesium. The present invention further provides an improved and commercially viable process for preparation of substantially enantiomerically pure esomeprazole in neutral form or as a pharmaceutically acceptable salt or as its solvates including hydrates. The present invention also provides solid form of esomeprazole calcium salt, its polymorphs (form 1, form 2 and amorphous form) and processes for their preparation thereof.04-19-2012
20120095053AMINOTETRAHYDROINDAZOLOACETIC ACIDS - The invention is concerned with the compounds of formula I:04-19-2012

Patent applications in class Plural hetero atoms in the polycyclo ring system