Class / Patent application number | Description | Number of patent applications / Date published |
514230800 | Chalcogen bonded directly to ring carbon of 1,4-oxazine ring | 69 |
20080214535 | Amorphous Aprepitant Coprecipitates - A coprecipitate comprising amorphous aprepitant and a pharmaceutically acceptable carrier is prepared by rapidly removing solvent from a solution containing aprepitant and the carrier. | 09-04-2008 |
20080275036 | Prevention and treatment of cardiac conditions - The present invention provides a method of treating conditions associated with iron and calcium overload comprising administering an effective amount of dexrazoxane or a non-dexrazoxane compound of formula (IA), (IB), or (IC) or a pharmaceutically acceptable salt, tautomer, or stereoisomer thereof. | 11-06-2008 |
20090018126 | 4-Aminophenylmorpholinone Derivatives and Their Preparation - The invention relates to novel aminophenylmorpholinone derivates (I) | 01-15-2009 |
20090069313 | Novel MAO-A inhibitors - The present invention provides a new medical use for the compounds of the formula (I), their derivatives, analogs, tautomeric forms, stereoisomers, polymorphs, hydrates, solvates, pharmaceutically acceptable salts and compositions, metabolites and prodrugs thereof, as MAO-A inhibitors. Also included is a method for prophylaxis and treatment of mental disorders such as depression, in a mammal, comprising administering an effective amount of a compound of formula (I). These compounds are also effective in treating a disease, condition or disorder such as weight loss, obesity, bulimia, depression, bipolar disorders, psychoses, schizophrenia, behaviors, alcoholism, tobacco abuse, memory loss, Alzheimer's disease, dementia of aging, seizure disorders, epilepsy, attention deficit disorder, and Parkinson's disease, which is modulated by a cannabinoid receptor antagonist. | 03-12-2009 |
20090131420 | Novel Heterocyclic Analogs of Biphenyl Ethers - The present invention relates to novel compounds of formula (I) and their pharmaceutically acceptable salts and compositions. The present invention more particularly provides novel heterocyclic analogs of biphenyl ethers of the general formula (I). | 05-21-2009 |
20090203683 | BICYCLIC HETEROCYCLES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM, THEIR USE, AND PROCESSES FOR PREPARING THEM - A compound of formula (I) | 08-13-2009 |
20090239857 | TRIAMINE DERIVATIVE - An object of the present invention is to provide a novel compound which has a potent inhibitory effect on FXa and exhibits an excellent antithrombotic effect when orally administered. The present invention provides a compound represented by the following general formula (1): | 09-24-2009 |
20100048548 | IMINO-OXAZOLIDINES AND USE THEREOF - The present invention relates to novel iminooxazolidines, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and also to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular thromboembolic disorders. | 02-25-2010 |
20100063043 | SUBSTITUTED 2-OXO-3-PHENYL-5-CARBONYLAMINOMETHYL-1, 3-OXAZOLINES AND THEIR USE AS ANTICOAGULANT AND ANTITHROMBOTICS - The invention relates to the field of blood coagulation, more particularly, to novel compounds of general formula (I), | 03-11-2010 |
20100125070 | Bupropion Metabolites and Methods of Their Synthesis and Use - Methods and compositions are disclosed which utilize metabolites of bupropion for treating disorders ameliorated by inhibition of neuronal monoamine reuptake. Such disorders include, but are not limited to, sexual dysfunction, affective disorders, cerebral function disorders, cigarette smoking, and incontinence. Methods of making optically pure bupropion metabolites are also disclosed. | 05-20-2010 |
20100144727 | Oxazolidine and Morpholine Carboxamide Derivatives as P2X7 Modulators - The present invention relates to a compound of formula (I): | 06-10-2010 |
20100144728 | Oxazolidinone For The Treatment And Prophylaxis Of Pulmonary Hypertension - The present invention relates to the use of factor Xa inhibitors, especially of oxazolidinones of the formula (I), for the treatment and/or prophylaxis of pulmonary hypertension, and to the use thereof for the manufacture of medicaments for the treatment and/or prophylaxis of pulmonary hypertension. | 06-10-2010 |
20100152178 | IMIDAZOLE DERIVATIVES - A CB2 receptor modulator comprising an imidazole derivative represented by the general formula (I): | 06-17-2010 |
20100184756 | Herbicide Composition for Lawn - A herbicide composition for lawn characterized by containing iodosulfuron-methyl or its salt, and at least 1 kind of herbicidal compound selected from the group consisting of oxaziclomefone, fentrazamide, oxadiargyl, ethoxysulfuron, cafenstrole, indanofan, asulam, fenoxaprop, clethodim, ethofumesate, tribenuron-methyl, metsulfuron-methyl, thifensulfuron-methyl, bromoxynil, MCPA, 2,4-D, dicamba as effective components. | 07-22-2010 |
20100197680 | LACTAM-SUBSTITUTED DICARBOXYLIC ACIDS AND USE THEREOF - The present application relates to novel lactam-substituted dicarboxylic acid derivatives, processes for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for producing medicaments for the treatment and/or prophylaxis of diseases, especially for the treatment and/or prevention of cardiovascular disorders. | 08-05-2010 |
20100210637 | HETEROARYLOXY NITROGENOUS SATURATED HETEROCYCLIC DERIVATIVE - Provided are compounds of a formula (I) and their pharmaceutically-acceptable salts: | 08-19-2010 |
20100210638 | MODULATORS 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. | 08-19-2010 |
20100261720 | HETEROCYCLIC COMPOUND AND PHARMACEUTICAL COMPOSITION THEREOF - The present invention provides a heterocyclic compound represented by General Formula (1): | 10-14-2010 |
20100273789 | AMINOACYL PRODRUGS - The present application relates to prodrug derivatives of 5-chloro-N-({(5S)-2-oxo-3-[2-fluoro-4-(3-oxomorpholin-4-yl)phenyl]-1,3-oxazolidin-5-yl}methyl)thiophene-2-carboxamide, processes for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for the manufacture of medicaments for the treatment and/or prophylaxis of diseases, especially of thromboembolic disorders. | 10-28-2010 |
20100273790 | PROCESSES FOR THE PREPARATION OF RIVAROXABAN AND INTERMEDIATES THEREOF - This invention provides a process for the preparation of S-Rivaroxaban and/or R-Rivaroxaban comprising reacting, in the presence of a first base, a compound of Formula 9: | 10-28-2010 |
20100292230 | Aminoacyl prodrug derivatives and medicaments for treatment of thromboembolic disorders - The present application relates to prodrug derivatives of 5-chloro-N-({(5S)-2-oxo-3-[4-(3-oxomorpholin-4-yl)phenyl]-1,3-oxazolidin-5-yl}methyl)thiophene-2-carboxamide, processes for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for the manufacture of medicaments for the treatment and/or prophylaxis of diseases, especially of thromboembolic disorders. | 11-18-2010 |
20100305116 | Compounds Comprising a Cyclobutoxy Group - The present invention relates to compounds comprising a cyclobutoxy group, processes for preparing them, phar-maceutical compositions comprising said compounds and their use as pharmaceuticals. | 12-02-2010 |
20110003804 | Oxazolidinones For the Treatment and/or Prophylaxis of Heart Failure - The present invention relates to the use of selective inhibitors of coagulation factor Xa, in particular of oxazolidinones of the formula (I), for the treatment and/or prophylaxis of heart failure and/or disorders related to heart failure as well as their use for the preparation of pharmaceutical drugs for the treatment and/or prophylaxis of heart failure and/or disorders related to heart failure. | 01-06-2011 |
20110009402 | Cyclic Inhibitors of 11Beta-Hydroxysteroid Dehydrogenase 1 - The invention relates to novel compounds of the Formula Ik, Im | 01-13-2011 |
20110015191 | ORGANIC COMPOUNDS - Novel polymorph form III of Aprepitant and a method for preparation of novel form III is disclosed. New processes for the preparation of Aprepitant form II are disclosed. The processes involve transformation of form III to form II by heating in decalin and the precipitation of form II from a solvent or solvent mixture by cooling and/or addition of addition of seed crystals or an anti solvent. Solid dispersions containing Aprepitant form II in a suitable carrier are disclosed. A process for the preparation of the solid dispersion by evaporation of a solution of Aprepitant and the carrier in a suitable solvent is disclosed. Stable Aprepitant form II is disclosed. Further pharmaceutical compositions containing Aprepitant form II, III or solid dispersions containing Aprepitant form II in a suitable carrier are disclosed. A methanol solvate of Aprepitant is disclosed. | 01-20-2011 |
20110034453 | Aminoacyl Prodrug Derivatives and Medicaments for the Treatment of Thromboembolitic Disorders - The present application relates to prodrug derivatives of 5-chloro-N-({(5S)-2-oxo-3-[4-(3-oxomorpholin-4-yl)phenyl]-1,3-oxazolidin-5-yl}methyl)thiophene-2-carboxamide, processes for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for the manufacture of medicaments for the treatment and/or prophylaxis of diseases, especially of thromboembolic disorders. | 02-10-2011 |
20110046127 | Imidazopyridazines for Use as Protein Kinase Inhibitors - There is provided compounds of formula (I): wherein Z, M, R | 02-24-2011 |
20110053927 | NANOPARTICLE FORMATION VIA RAPID PRECIPITATION - The invention encompasses a method for making nano-sized particles of water-insoluble pharmaceuticals comprising: (1) dissolving the water-insoluble pharmaceutical in a water-miscible solvent, optionally with water and inactive pharmaceutical ingredients, to make a solution; (2) rapidly mixing the solution with an anti-solvent which creates a high level of supersaturation, wherein the anti-solvent is water with optional inactive pharmaceutical ingredients; (3) simultaneously applying energy to the resulting mixture during the mixing of solution and anti-solvent as nano-sized drug particles precipitate out and form a slurry mixture under supersaturation; and (4) optionally isolating the nano-sized particles of water-insoluble pharmaceuticals from the slurry mixture. | 03-03-2011 |
20110059958 | MORPHOLINONE COMPOUNDS AS FACTOR IXA INHIBITORS - The present invention provides a compound of Formula (I) | 03-10-2011 |
20110098289 | METHOD FOR TREATING OBESITY - The present invention relates generally to methods of treating obesity and minimizing metabolic risk factors associated therewith using, for example, zonisamide or other weight loss-promoting anti-convulsant either alone or in combination with bupropion or metabolites thereof or other compound that enhances the activity of norepinephrine and/or dopamine via uptake inhibition or other mechanism. | 04-28-2011 |
20110118251 | SPIROPIPERIDINE COMPOUNDS AS ORL-1 RECEPTOR ANTAGONISTS - An ORL-1 receptor antagonist of the formula: | 05-19-2011 |
20110118252 | SUBSTITUTED AMIDE DERIVATIVES AND METHODS OF USE - Selected compounds are effective for prophylaxis and treatment of diseases, such as HGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes. | 05-19-2011 |
20110118253 | 5-METHYL-1-(NAPHTHALEN-2-YL)-1H-PYRAZOLES USEFUL AS SIGMA RECEPTOR INHIBITORS - The invention relates to compounds having the formula (I): | 05-19-2011 |
20110160199 | Aralkyl Substituted Piperidine or Piperazine Derivatives and Their Use for Treating Schizophrenia - The present invention discloses an aralkyl substituted piperidine or piperazine derivative and the use of the derivative in preparation of medicaments for treating schizophrenia and correlative psychoneuroses. It is shown by pharmacological tests that the derivative of the present invention has better antischizophrenic effect and less toxicity. Said derivative is a free base or salt of the compound having the following general formula. | 06-30-2011 |
20110172222 | Oxazolidinones for the Treatment of Inflammatory Conditions of the Gastrointestinal Tract - The present invention relates to the use of selective inhibitors of coagulation factor Xa, in particular of oxazolidinones of the formula (I), for the treatment and/or prophylaxis of inflammatory conditions of the gastrointestinal tract such as inflammatory bowel disease (IBD) and celiac disease and/or disorders related to inflammatory bowel disease (IBD) and/or celiac disease such as thromboembolic events (including e.g. pulmonary embolism (PE), arterial and venous thrombosis, myocardial infarction, stroke) as well their use for the preparation of pharmaceutical drugs for the treatment and/or prophylaxis of inflammatory bowel disease (IBD) and/or celiac disease and/or disorders related to inflammatory bowel disease (IBD) and/or celiac disease such as thromboembolic events. | 07-14-2011 |
20110172223 | Substituted Aryl Sulfone Derivatives as Calcium Channel Blockers - A series of substituted aryl sulfone derivatives represented by Formula I, or pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by, calcium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, urinary incontinence, itchiness, allergic dermatitis, epilepsy, diabetic neuropathy, irritable bowel syndrome, depression, anxiety, multiple sclerosis, sleep disorder, bipolar disorder and stroke, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds. | 07-14-2011 |
20110230478 | 4-Alkyl-substituted diaminopyrimidines - Use of 4-alkyl-substituted diaminopyrimidines of the formula (I) as fungicide | 09-22-2011 |
20110237578 | AMIDE COMPOUNDS, COMPOSITIONS AND USES THEREOF - Compounds are provided according to formula (I), where A, B, W, X′, L, R | 09-29-2011 |
20110245242 | Heterocyclically Substituted Anilinopyrimides - Heterocyclically substituted anilinopyrimidines of the formula (I) | 10-06-2011 |
20110263591 | 2-HETEROARYL CARBOXAMIDES - The invention relates to novel 2-heteroaryl carboxamides and to the use thereof for producing medicaments for the treatment and/or prophylaxis of diseases and for improving perception, concentration, learning and/or memory. | 10-27-2011 |
20110281860 | USE OF QUINAZOLINE DERIVATIVES FOR THE TREATMENT OF VIRAL DISEASES - The present invention relates to the use of quinazoline derivatives, which show EGFR inhibitory activity, for the prevention and/or treatment of virus-induced diseases, preferably virus induced respiratory diseases and exacerbation in chronic airway diseases such as COPD or asthma. | 11-17-2011 |
20120088761 | AMINOACYL PRODRUG DERIVATIVES AND MEDICAMENTS FOR THE TREATMENT OF THROMBOEMBOLITIC DISORDERS - The present application relates to prodrug derivatives of 5-chloro-N-({(5S)-2-oxo-3-[4-(3-oxomorpholin-4-yl)phenyl]-1,3-oxazolidin-5-yl}methyl)thiophene-2-carboxamide, processes for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for the manufacture of medicaments for the treatment and/or prophylaxis of diseases, especially of thromboembolic disorders. | 04-12-2012 |
20120094994 | FUNCTIONALIZED AMINO ACIDS AND ABSORBABLE POLYMERS THEREFROM - The present invention relates to compounds of formula I and II, which are functionalized amino acids, and polymers formed from the same. | 04-19-2012 |
20120184544 | SUBSTITUTED BENZAMIDE DERIVATIVES AS GLUCOKINASE (GK) ACTIVATORS - The present invention relates to substituted benzamide derivatives of the general Formula I and their pharmaceutically acceptable salts, pharmaceutically acceptable solvates, enantiomers, diastereomers, prodrugs, metabolites, and polymorphs and can be useful for treating disease states mediated by glucokinase. Compounds disclosed herein can be used for reducing blood glucose levels and for increasing insulin secretion for treating type II diabetes. The invention also relates to processes for the preparation of the compounds of invention, pharmaceutical compositions containing the compounds, and their use. | 07-19-2012 |
20120214806 | 3-AMINO-5-PHENYL-5,6-DIHYDRO-2H-[1,4]OXAZINES - The present invention relates to 3-Amino-5-phenyl-5,6-dihydro-2H-[1,4]oxazines of formula I | 08-23-2012 |
20120252801 | ANTIFUNGAL COMPOUNDS - The present invention relates to a series of novel compounds which have been shown to possess antifungal activity. The invention therefore relates to the new compounds, methods for their preparation, pharmaceutical compositions comprising them and to the compounds for use as a medicament, more in particular antifungal medicament. | 10-04-2012 |
20120258964 | 2-HETEROARYL CARBOXAMIDES - The invention relates to novel 2-heteroaryl carboxamides and to the use thereof for producing medicaments for the treatment and/or prophylaxis of diseases and for improving perception, concentration, learning and/or memory. | 10-11-2012 |
20120289502 | IMIDAZOLE DERIVATIVES - A CB2 receptor modulator comprising an imidazole derivative represented by the general formula (I): | 11-15-2012 |
20130123252 | 2,3,5-Trisubstituted Thiophene Compounds and Uses Thereof - The present invention provides a compound of formula I: | 05-16-2013 |
20130131056 | POSITIVE ALLOSTERIC MODULATORS (PAM) - The present invention relates to phenylethynyl compounds of formula I | 05-23-2013 |
20130178469 | NOVEL ANTIVIRAL AGENTS - The present invention provides a compound of Formula I or a pharmaceutically acceptable derivative, salt or prodrug thereof. Further provided is a method of treatment or prophylaxis of a viral infection in a subject comprising administering to said subject an effective amount of a compound of Formula I or a pharmaceutically acceptable derivative, salt or prodrug thereof. A pharmaceutical composition or medicament comprising a compound of Formula I is also provided | 07-11-2013 |
20130203751 | SUBSTITUTED 8-ALKOXY-2-AMINOTETRALIN DERIVATIVES, AND USE THEREOF - The present application relates to novel substituted 8-alkoxy-2-aminotetraline derivatives, to processes for their preparation, to their use for the treatment and/or prevention of diseases and to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of cardiovascular disorders. | 08-08-2013 |
20130237535 | FATTY ACID SYNTHASE INHIBITORS - This invention relates to the use of spirocyclic piperidine derivatives for the modulation, notably the inhibition of the activity or function of fatty acid synthase (FAS). Suitably, the present invention relates to the use of spirocyclic piperidines in the treatment of cancer. | 09-12-2013 |
20130252949 | APREPITANT L-PROLINE COMPOSITION AND COCRYSTAL - A 1:1:1 aprepitant L-proline H | 09-26-2013 |
20130317016 | Aprepitant Injectable Formulations - An aqueous stable and ready-to-use formulation of aprepitant is prepared. Especially preferred formulations comprise a synergistic combination of a co-solvent and a surfactant and may further include a secondary co-solvent. Among other advantages of contemplated formulations, aprepitant is dissolved at high concentrations and remains dissolved and stable, even over prolonged periods of time. | 11-28-2013 |
20130338156 | IMIDAZOPYRIDIN-2-ONE DERIVATIVES - A compound represented by formula (I) having mTOR inhibitory activity or a pharmacologically acceptable salt thereof. | 12-19-2013 |
20130345213 | SUBSTITUTED MORPHOLINES AS MODULATORS FOR THE CALCIUM SENSING RECEPTOR - Compounds of Formula (I) along with processes for their preparation that are useful for treating, managing and/or lessening the diseases, disorders, syndromes or conditions associated with the modulation of calcium sensing (CaSR) receptors. Methods of treating, managing and/or lessening the diseases, disorders, syndromes or conditions associated with the modulation of calcium sensing (CaSR) receptors of Formula (I). | 12-26-2013 |
20140187545 | Pyrazolopyrimidine Derivatives As PI3 Kinase Inhibitors - PI3Kβ selective compounds having the structure | 07-03-2014 |
20140235629 | HETEROCYCLIC COMPOUNDS AS MDM2 INHIBITORS FOR THE TREATMENT OF CANCER - The present invention provides MDM2 inhibitor compounds of Formula I or II, or the pharmaceutically acceptable salts thereof, | 08-21-2014 |
20140275061 | SUBSTITUTED TETRAHYDROISOQUINOLINE COMPOUNDS AS FACTOR XIA INHIBITORS - The present invention provides compounds of Formula (I): or stereoisomers, pharmaceutically acceptable salts thereof, wherein all of the variables are as defined herein. These compounds are inhibitors of factor XIa and/or plasma kallikrein which may be used as medicaments. | 09-18-2014 |
20140336187 | METHODS FOR TREATING LEISHMANIASIS - Methods are provided to inhibit proliferation of | 11-13-2014 |
20150141416 | HYDROXYBUPROPION ANALOGUES FOR TREATING DRUG DEPENDENCE - The invention provides hydroxybupropion analogues capable of inhibiting the reuptake of one or more monoamines and/or acting as antagonists at nicotinic acetylcholine receptors. The compounds may selectively bind to one or more monoamine transporters, including those for dopamine, norepinephrine, and serotonin and/or may selectively bind to one or more nicotinic acetylcholine receptor subtypes. Such compounds may be used to treat conditions that are responsive to modification of monoamine levels and/or antagonism of nicotinic acetylcholine receptors, including drug dependency, depression, and obesity. | 05-21-2015 |
20150315200 | SUBSTITUTED TETRAHYDROISOQUINOLINE COMPOUNDS AS FACTOR XIA INHIBITORS - The present invention provides compounds of Formula (I): | 11-05-2015 |
20150329562 | Factor IXa Inhibitors - The present invention provides a compound of Formula (I) | 11-19-2015 |
20150336943 | NOVEL BENZODIOXANE-PIPERIDINE DERIVATIVES AND THEIR THERAPEUTIC APPLICATIONS FOR TREATING NEUROPSYCHIATRIC DISORDERS - The present invention concerns benzodioxane-piperidine with general formula I: | 11-26-2015 |
20150352120 | USE OF NK-1 RECEPTOR ANTAGONISTS FOR TREATING HYPOMAGNESEMIA, NEUROGENIC INFLAMMATION, AND CARDIAC DYSFUNCTION ASSOCIATED WITH EGFR-BLOCKING DRUGS - The present disclosure provides methods for alleviating or preventing the negative physiological side effects associated with the administration of EGFR blocking therapeutics. The disclosure provides, inter alia, methods for treating or preventing: hypomagnesemia, cardiac dysfunction, and skin lesions, which are induced by EGFR blocking drugs, by administering an NK-1 receptor antagonist. | 12-10-2015 |
20160082013 | EMULSION FORMULATIONS OF APREPITANT - Disclosed herein are novel pharmaceutical formulations of aprepitant suitable for parenteral administration including intravenous administration. Also included are formulations including both aprepitant and dexamethasone sodium phosphate. The pharmaceutical formulations are stable oil-in-water emulsions for non-oral treatment of emesis and are particularly useful for treatment of subjects undergoing highly emetogenic cancer chemotherapy. | 03-24-2016 |
20160120870 | THE PROCESS FOR THE PREPARATION OF A PHARMACEUTICAL COMPOSITION COMPRISING RIVAROXABAN - The present invention relates to a process for the preparation of a pharmaceutical composition comprising rivaroxaban, wherein the process comprises a step of milling a mixture comprising rivaroxaban and at least one hydrophilic binder. | 05-05-2016 |
20160137626 | BICYCLIC AROMATIC CARBOXAMIDE COMPOUNDS USEFUL AS PIM KINASE INHIBITORS - The present disclosure describes bicyclic aromatic carboxamide derivatives, as well as their compositions and methods of use. The compounds inhibit the activity of the Pim kinases, and are useful in the treatment of diseases related to the activity of Pim kinases including, e.g., cancer and other diseases. | 05-19-2016 |