05th week of 2012 patent applcation highlights part 54 |
Patent application number | Title | Published |
20120028940 | FUNCTIONALLY SELECTIVE AZANITRILE ALPHA-2C ADRENORECEPTOR AGONISTS - In its many embodiments, the present invention provides a novel class of azanitrile compounds as inhibitors of α2C adrenergic receptor agonists, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the α2C adrenergic receptors using such compounds or pharmaceutical compositions. | 2012-02-02 |
20120028941 | Pharmaceutical Product Comprising a P38 Kinase Inhibitor and a Second Active Ingredient - The invention provides a pharmaceutical product, kit or composition comprising a first active ingredient which is N-Cyclopropyl-3-fluoro-4-methyl-5[3-[[1-[2-[2-(methylamino)ethoxy]phenyl]cyclopropyl]amino]-2-oxo-1(2H)-pyrazinyl]-benzamide or a salt thereof, and a second active ingredient selected from: a non-steroidal Glucocorticoid Receptor (GR Receptor) Agonist; an antioxidant; a β2 adrenoceptor agonist; a CCR1 antagonist; a chemokine antagonist (not CCR1); a corticosteroid; a CRTh2 antagonist; a DPI antagonist; an Histone Deacetylase activator; an IKK2 kinase inhibitor; a COX inhibitor; a lipoxygenase inhibitor; a leukotriene receptor antagonist; a MABA compound; an MPO inhibitor; a muscarinic antagonist; a PDE4 inhibitor; a PPARγ agonist; a protease inhibitor; a Statin; a thromboxane antagonist; a vasodilator; or, an ENAC blocker (Epithelial Sodium-channel blocker); and its use in the treatment of respiratory disease. | 2012-02-02 |
20120028942 | Medicinal Cream Made Using Neomycin Sulphate, Betamethasone Valerate, And Chitosan, And A Process To Make The Same - The present invention is directed to a composition for treating bacterial skin infections & skin inflammation, along with skin rejuvenation. More particularly, the present invention relates to a pharmaceutical cream comprising a biopolymer, a corticosteroid and an antibacterial active ingredient. It discloses a composition for treating bacterial skin infections & skin inflammation, along with skin rejuvenation containing a) a biopolymer in the form of chitosan, b) a combination of active pharmaceutical ingredients (APIs), neomycin sulphate & betamethasone valerate used in treating bacterial skin infections & skin inflammations, c) a cream base containing primary and secondary emulsifiers, waxy materials, co-solvents, acids, preservatives, buffering agents, anti oxidants, chelating agents, and humectants and d) water. The active ingredients, namely chitosan, a corticosteroid Betamethasone Valerate, and an antibacterial agent Neomycin Sulphate, are incorporated in cream base for use in treating bacterial skin infections and skin inflammation due to allergy & itching, & wounds on human skin involving contacting human skin with the above identified composition. | 2012-02-02 |
20120028943 | Medicinal Cream Made Using Fluticasone Propionate And Chitosan And A Process To Make The Same - The present invention relates to a composition for treating skin inflammation, along with skin rejuvenation. More particularly, the present invention relates to a pharmaceutical cream comprising a biopolymer, and a corticosteroid. It discloses a composition for treating skin inflammation, along with skin rejuvenation containing a) a biopolymer in the form of chitosan, b) an active pharmaceutical ingredient (API) composition in the form of fluticasone propionate, used in treating skin inflammation c) a cream base containing primary and secondary emulsifiers, waxy materials, co-solvents, acids, preservatives, buffering agents, anti oxidants, chelating agents, and humectants and d) water. The active ingredients, namely chitosan, and a corticosteroid in the form of fluticasone propionate, are incorporated in cream base for use in treating skin inflammation due to allergy & itching & wounds on human skin involving contacting human skin with the above identified composition. | 2012-02-02 |
20120028944 | CYCLODEXTRIN NANOTECHNOLOGY FOR OPHTHALMIC DRUG DELIVERY - The invention provides an ophthalmic composition which is an aqueous suspension comprising drug, cyclodextrin and water, the composition having an aqueous phase of from about 0.1% (w/v) to about 90% (w/v) of the drug in solution, as dissolved free drug and as dissolved drug/cyclodextrin complex(es), and a solid phase of from about 10% (w/v) to about 99.9% (w/v) of the drug as solid drug/cyclodextrin particles, suspended in the aqueous phase; the size of the solid particles being from about 10 nm to about 1 mm, the drug/cyclodextrin particles being capable of dissolving in aqueous tear fluid within 24 hours of application to the eye surface. The aqueous eye suspension can be in the form of eye drops, eye gel or eye mist. Further, the invention provides a method for treating a condition of the posterior segment and/or anterior segment of the eye comprising applying to the eye surface, in an amount which delivers to said segment or segments a therapeutically effective amount of a drug suitable for treating said condition, an ophthalmic composition which is as defined above. Nasal compositions and methods and ophthalmic and nasal compositions in powder form are also provided. | 2012-02-02 |
20120028945 | 5-Beta, 14-Beta-Androstane Derivatives Useful For The Treatment Of Proteinuria, Glomerulosclerosis And Renal Failure - Compound of formula (I), wherein the symbol have the meaning reported in the text; for preparing a medicament for the prevention and/or treatment of proteinuria, glomerulosclerosis or renal failure. | 2012-02-02 |
20120028946 | TESTOSTERONE GEL AND METHOD OF USE - The present invention relates to an improved transdermal hydroalcoholic testosterone gel formulation that provides, among other things, a desirable pharmacokinetic hormone profile, and methods of use. | 2012-02-02 |
20120028947 | Ophthalmic Compositions - An aqueous ophthalmic composition comprising loteprednol etabonate, and polyacryclic acid. The composition has a viscosity in the range from about 300 cp to about 1500 cp, and a total concentration of cations of less than about 50 mM. The ophthalmic composition is used to treat patients suffering from allergic conjunctivitis, and includes instructing a person suffering from ocular itching resulting from allergic conjunctivitis to administer once or twice daily in the form of one or more eye drops the aqueous ophthalmic composition described. | 2012-02-02 |
20120028948 | TESTOSTERONE GEL AND METHOD OF USE - The present invention relates to an improved transdermal hydroalcoholic testosterone gel formulation that provides, among other things, a desirable pharmacokinetic hormone profile, and methods of use. | 2012-02-02 |
20120028949 | Rapidly Disintegrating Tablet - The present invention relates to rapidly disintegrating tablets intended to be used as orodispersible tablets or dispersible tablets. They are ingested either by dispersing directly in the mouth or in water. The tablets include silicified microsrystalline cellulose. They are especially suitable for antibiotics. These tablets are also suitable for use in pediatric patients in the age above 3 years. For pediatric patients under 3 years the same tablets can be used as dispersible tablets. Rapidly disintegrating tablets which contain amoxicillin and clavulanic acid are also described. | 2012-02-02 |
20120028950 | Substituted heterocyclylbenzylpyrazoles and use thereof - The present application relates to novel substituted 1-[3-(heterocyclyl)benzyl]-1H-pyrazole derivatives, to processes for preparation thereof, to use thereof for treatment and/or prevention of diseases and to use thereof for production of medicaments for treatment and/or prevention of diseases, more particularly for treatment and/or prevention of hyperproliferative and angiogenic diseases and those diseases which arise from metabolic adaptation to hypoxic states. Such treatments can be effected in the form of monotherapy or else in combination with other medicaments or further therapeutic measures. | 2012-02-02 |
20120028951 | PYRIDAZINONE COMPOUNDS - The present invention provides a compound which has the effect of PDE inhibition, and which is useful as a medicament for preventing or treating schizophrenia or so on. A compound of formula (I | 2012-02-02 |
20120028952 | 5-ALKYNYL-PYRIMIDINES - The present invention encompasses compounds of general formula (1) | 2012-02-02 |
20120028953 | Azetidine Derivatives - Compounds of formula (I) are inhibitors of fatty acid amide hydrolase, (FAAH), and which are useful in the treatment of diseases or medical conditions which benefit from inhibition of FAAH activity, such as anxiety, depression pain, inflammation, and eating, sleep, neurodegenerative and movement disorders: Formula (I) Wherein Ar | 2012-02-02 |
20120028954 | Substituted Pyridine, Pyridazine, Pyrazine And Pyrimidine Compounds And Methods For Using The Same - Disclosed are substituted pyridine compounds as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure | 2012-02-02 |
20120028955 | BICYCLIC MGLUR5 POSITIVE ALLOSTERIC MODULATORS AND METHODS OF MAKING AND USING SAME - In one aspect, the invention relates to bicyclic mGluR5 positive allosteric modulators, for example 6-(phenylethynyl)-3,4-dihydroisoquinolin-1(2H)-one, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention. | 2012-02-02 |
20120028956 | BICYCLIC MGLUR5 POSITIVE ALLOSTERIC MODULATORS AND METHODS OF MAKING AND USING SAME - In one aspect, the invention relates to bicyclic mGluR5 positive allosteric modulators, for example 6-(phenylethynyl)-3,4-dihydroisoquinolin-1(2H)-one, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention. | 2012-02-02 |
20120028957 | Inhibitors Of The Influenza A Virus M2 Proton Channel - Provided are compounds that are capable of modulating the activity of the influenza A virus via interaction with the M2 transmembrane protein. Also provided are methods for treating an influenza A-affected disease state or infection comprising administering a composition comprising one or more compounds that have been identified as being capable of interaction with the M2 protein. | 2012-02-02 |
20120028958 | 5-ALKYNYL-PYRIMIDINES - The present invention encompasses compounds of general formula (1) | 2012-02-02 |
20120028959 | DIHYDROOROTATE DEHYDROGENASE INHIBITORS - The invention relates to compounds of formula (I) wherein R | 2012-02-02 |
20120028961 | 6 Substituted 2, 3,4,5 Tetrahydro-1H-Benzo[d]Azepines as 5-HT2c Receptor Agonist - The present invention provides 6-substituted 2,3,4,5-tetrahydro-1H-benzo[d]azepines of Formula I as selective 5-HT | 2012-02-02 |
20120028962 | FUSED HETEROCYCLIC RING COMPOUND - A compound represented by the following formula or a salt thereof, which has an GPR119 agonist action, is useful for the prophylaxis or treatment of diabetes, obesity and the like, and shows superior efficacy: | 2012-02-02 |
20120028963 | NOVEL HYDROXAMATE DERIVATIVE, A PRODUCTION METHOD FOR THE SAME, AND A PHARMACEUTICAL COMPOSITION COMPRISING THE SAME - The present invention relates to hydroxamate derivatives, isomers thereof, pharmaceutically acceptable salts thereof, hydrates thereof, or solvates thereof, the use thereof for preparing pharmaceutical compositions, pharmaceutical compositions containing the same, a method of treating disease using the compositions, and a method for preparing the hydroxamate derivatives. | 2012-02-02 |
20120028964 | PHARMACEUTICAL COMBINATION - The present invention relates to a pharmaceutical combination for the treatment of schizophrenia and acute manic episodes associated with bipolar disorders, which comprises a compound which is active on a trace amine-associated receptor 1 (TAAR1 agonist) and an antipsychotic drug. This combination can reduce metabolic side effects which appear if using an antipsychotic drug alone. | 2012-02-02 |
20120028965 | COMPOUNDS USEFUL AS PROTEIN KINASE INHIBITORS - The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions. | 2012-02-02 |
20120028966 | PROTEIN KINASE INHIBITORS - In one aspect, the invention provides compounds of Formula I | 2012-02-02 |
20120028967 | NOVEL DIAZA-BICYCLONONYL-PYRIMIDINYL DERIVATIVES AND THEIR MEDICAL USE - This invention relates to novel 1,4-diaza-bicyclo[3.2.2]nonyl pyrimidine derivatives and their use in the manufacture of pharmaceutical compositions. The compounds of the invention are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances. | 2012-02-02 |
20120028968 | NOVEL DIBENZOFURANYL-OXADIAZOLYL-DIAZABICYCLONONANE DERIVATIVES AND THEIR MEDICAL USE - This invention relates to novel dibenzofuranyl-oxadiazolyl-diazabicyclononane derivatives and their use in the manufacture of pharmaceutical compositions. The compounds of the invention are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances. | 2012-02-02 |
20120028969 | BICYCLIC ACETYL-COA CARBOXYLASE INHIBITORS AND USES THEREOF - The present invention provides compounds of formula (I); | 2012-02-02 |
20120028970 | HETEROARYLTHIOMETHYL PYRIDINE DERIVATIVE - The present invention relates to a compound represented by a formula (I): wherein X is a group represented by or the like; Y is a group represented by or the like; and Ar | 2012-02-02 |
20120028971 | OXO-HETEROCYCLICALLY SUBSTITUTED ALKYL CARBOXYLIC ACIDS AND USE THEREOF - The present application relates to novel alkylcarboxylic acids having an oxo-substituted azaheterocyclic partial structure, to processes for their preparation, to their use for the treatment and/or prevention of diseases, and to their use for producing medicaments for the treatment and/or prevention of diseases, especially for the treatment and/or prevention of cardiovascular disorders. | 2012-02-02 |
20120028972 | BIOMARKER ASSAYS FOR DETECTING OR MEASURING INHIBITION OF TOR KINASE ACTIVITY - Provided herein are methods for detecting and/or measuring the inhibition of TOR kinase activity in a subject and uses associated therewith. | 2012-02-02 |
20120028973 | NITROIMIDAZOOXAZINES AND THEIR USES IN ANTI-TUBERCULAR THERAPY - The present invention relates to novel nitroimidazooxazines, to their preparation, and to their use as drugs for treating | 2012-02-02 |
20120028974 | TRIAZOLOPYRIDINES AS PHOSPHODIESTERASE INHIBITORS FOR TREATMENT OF DERMAL DISEASES - The present invention relates to a compound according to formula I, wherein R | 2012-02-02 |
20120028975 | SUBSTITUTED TRIAZOLOPYRIDINES AND ANALOGS THEREOF - The present invention relates to substituted triazolopyridines and analogs thereof, the use of the compounds as phosphodiesterase 10 (PDE10) inhibitors for the treatment of PDE10-modulated disorders, to pharmaceutical compositions comprising the compounds. | 2012-02-02 |
20120028976 | PHARMACOKINETICALLY-BASED DOSING REGIMENTS OF A THROMBIN RECEPTOR ANTAGONIST - Dosing regimens based on the pharmacokinetic characteristics of a thrombin receptor antagonist are disclosed. In some embodiments, the dosing regimens result in mean plasma concentrations. Also disclosed are methods of treating acute coronary syndrome and peripheral arterial disease, and of effecting secondary prevention, by orally administering thrombin receptor antagonists according to such dosing regimens. | 2012-02-02 |
20120028977 | Subunit Selective NMDA Receptor Potentiators For The Treatment Of Neurological Conditions - Provided are compounds, pharmaceutical compositions and methods of treating or preventing disorders associated with NMDA receptor activity, including schizophrenia, Parkinson's disease, cognitive disorders, depression, neuropathic pain, stroke, traumatic brain injury, epilepsy, and related neurologic events or neurodegeneration. Compounds of the general Formulas A-J, and pharmaceutically acceptable salts, esters, prodrugs or derivatives thereof are disclosed. | 2012-02-02 |
20120028978 | SUBSTITUTED BICYCLIC HCV INHIBITORS - Provided herein are compounds, pharmaceutical compositions and combination therapies for treatment of hepatitis C. | 2012-02-02 |
20120028979 | 2-(PIPERIDIN-1-YL)-4-HETEROCYCLYL-THIAZOLE-5-CARBOXYLIC ACID DERIVATIVES AGAINST BACTERIAL INFECTIONS - Compounds of formula (I) and their pharmaceutically acceptable salts are described. Processes for their preparation, pharmaceutical compositions containing them, their use as medicaments and their use in the treatment of bacterial infections are also described. | 2012-02-02 |
20120028980 | USE OF NK-1 RECEPTOR ANTAGONISTS IN MANAGEMENT OF VISCERAL PAIN - Methods for managing visceral pain in mammalian subjects are described, in which a NK-1 receptor antagonist is administered to the subject before, during or after administration of general anesthesia. The methods and uses of NK-1 receptor antagonists described herein provide improved visceral pain management and MAC reduction when used with volatile anesthetics for general anesthesia. | 2012-02-02 |
20120028981 | Kinase Knockdown Via Electrophilically Enhanced Inhibitors - Provided herein are electrophilically enhanced kinase inhibitors. Also provided herein are methods of making and utilizing the same. | 2012-02-02 |
20120028982 | 2-AMINO-BICYCLO[3.1.0]HEXANE-2, 6-DICARBOXYLIC ESTER DERIVATIVE - A drug effective for the treatment and prevention of psychiatric disorders such as schizophrenia, anxiety and related ailments thereof, depression, bipolar disorder and epilepsy. The drug antagonizes the action of group II metabotropic glutamate receptors and shows high activity in oral administration. A 2-amino-bicyclo[3.1.0]hexane-2,6-dicarboxylic ester derivative represented by formula [I] | 2012-02-02 |
20120028983 | NOVEL COMPOUND HAVING 3-HETEROARYLPYRIMIDIN-4-(3H)-ONE STRUCTURE AND PHARMACEUTICAL PREPARATION CONTAINING SAME - Disclosed is a compound which has both an angiotensin-II receptor antagonistic activity and a PPARγ activation activity and is useful as a prophylactic and/or therapeutic agent for hypertension, heart diseases, angina pectoris, cerebrovascular disorders, cerebral circulatory disorders, ischemic peripheral circulatory disorders, renal diseases, arteriosclerosis, inflammatory diseases, type-2 diabetes, diabetic complications, insulin resistance syndrome, syndrome X, metabolic syndrome and hyperinsulinemia. [In the formula, A represents a 5- to 10-membered heteroaryl group; R | 2012-02-02 |
20120028984 | Compound Useful As A c-MET Inhibitor - The present invention relates to a c-Met inhibitor (disclosed herein) or a pharmaceutically acceptable salt thereof useful in treating cancer mediated by activity of c-Met receptors. | 2012-02-02 |
20120028985 | COMBINATIONAL THERAPY FOR TREATING AUTOIMMUNE DISEASE - The present invention relates to the treatment and prevention of immunological and inflammatory disorders with a compound of formula (I) in combination with methotrexate, | 2012-02-02 |
20120028986 | 2-HETEROARYL-PYRROLO [3,4-C]PYRROLE DERIVATIVES, AND USE THEREOF AS SCD INHIBITORS - The invention relates to compounds of the formula (I), where the groups R1, M, A, B, D, L, and R have the specified meanings, and to the physiologically compatible salts thereof. The compounds are suitable, for example, for treating metabolic syndrome, insulin resistance, obesity, and diabetes. | 2012-02-02 |
20120028987 | Bicyclic Benzamides of 3-Or-4-Substituted 4-(Aminomethyl)-Piperidine Derivatives - The present invention of compounds of formula (I) | 2012-02-02 |
20120028988 | USE OF PYRIDAZINONE COMPOUND FOR CONTROL OF HARMFUL ARTHROPOD PESTS - Since a pyridazinone compound shown by formula (I) has an activity for controlling arthropod pests, the pyridazinone compound is effective for a use for controlling arthropod pests. | 2012-02-02 |
20120028989 | 6-(3-AZA-BICYCLO[3.1.0]HEX-3-YL)-2-PHENYL-PYRIMIDINES - The present invention relates to 6-(3-aza-bicyclo[3.1.0]hex-3-yl)-2-phenyl-pyrimidine derivatives and their use as P2Y | 2012-02-02 |
20120028990 | 3 ARYL OR HETEROARYL-SUBSTITUTED INDOLE DERIVATIVE - A 3-aryl or heteroaryl-substituted indole derivative which is effective as a preventive or remedy for various diseases is provided. [Means for Resolution] A compound represented by a formula (I) or a pharmaceutically acceptable salt thereof is provided. In the formula, R1 represents a hydrogen atom, C1-6 alkyl et al; R2 represents a hydrogen atom, C1-6 alkyl et al; Z represents aryl or heteroaryl (with the proviso that imidazolyl is excluded); and W represents a group represented by the formula (w-1) or (w-2). In the formula, R3 represents C1-6 alkyl et al; Yl and Y2 both represent a hydrogen atom or Y1 and Y2 together form —CH2-CH2-; Q represents CH or N; Ar represents phenyl, furyl et al; R4 and R5 each independently represent a hydrogen atom or C1-6 alkyl or R4 and R5 together with the nitrogen atom form pyrrolidine et al. | 2012-02-02 |
20120028991 | PHARMACEUTICAL COMPOSITIONS CONTAINING DOPAMINE RECEPTOR LIGANDS AND METHODS OF TREATMENT USING DOPAMINE RECEPTOR LIGANDS - The present invention relates to pharmaceutical compositions containing dopamine receptor ligands and selective serotonin reuptake inhibitors and to methods of treating disorders such as schizophrenia, major depressive disorder and bipolar depression using combinations of dopamine receptor ligands and selective serotonin reuptake inhibitors. The present invention also relates to methods of treating depression using dopamine receptor ligands. | 2012-02-02 |
20120028992 | Pharmaceutical compositions for terminating acute episodes of cardiac arrhythmia, restoring sinus rhythm, preventing recurrence of cardiac arrhythmia and/or maintaining normal sinus rhythm in mammals - Disclosed are pharmaceutical compositions for and methods of preventing or treating acute and/or chronic cardiac arrhythmias in a mammal, including terminating acute episodes of cardiac arrhythmia, restoring normal sinus rhythm, preventing recurrence of cardiac arrhythmia and/or maintaining normal sinus rhythm, which contain a combination of 1-[2-[(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazine and 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazine. | 2012-02-02 |
20120028993 | Compounds Effective Against Cancer - The present invention describes a Composition, comprising one or more compounds selected from the group consisting of a) compound (I) which is ethacrynic acid bezafibrate, fenofibrate, and/or griseofulvin, b) compound (II), which is ciclopirox ciclopirox olamine, octopirox, and/or cinnarizine, c) mixtures of compound (I) and compound (II), or pharmaceutically acceptable derivatives thereof for the treatment of cancer. The present invention is further directed to the use of said compounds or a mixture of compounds for the manufacture of a medicament for the treatment of cancer and to the use of said compound in a method for treating cancers in animals and humans. | 2012-02-02 |
20120028994 | COMPOUNDS FOR THE REDUCTION OF BETA-AMYLOID PRODUCTION - The present disclosure provides a series of compounds of the formula (I) | 2012-02-02 |
20120028995 | NOVEL COMPOUNDS FOR MEDICAL USE AS PEPTIDASE EFFECTORS - The invention relates to compounds of general formula (I) as set forth in the claims as well as to the use of the compounds of the general formula (1) in the medical field, specifically for use in the suppression of DNA synthesis and inflammatory cytokine production as well as in the stimulation of anti-inflammatory cytokine production in vitro and in vivo. This abstract is neither intended to define the invention disclosed in this specification nor intended to limit the scope of the invention in any way. | 2012-02-02 |
20120028996 | NOVEL OXIME DERIVATIVES - The present invention relates to novel oxime derivatives of the general formula (I), their tautomeric forms, their stereoisomers, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, methods for their preparation, use of these compounds in medicine and the intermediates involved in their preparation. | 2012-02-02 |
20120028997 | PROKINETICIN 1 RECEPTOR ANTAGONISTS - The present invention relates to certain novel compounds of Formula (I): | 2012-02-02 |
20120028998 | CO-CRYSTAL OF ETRAVIRINE AND NICOTINAMIDE - Etravirine (TMC125) nicotinamide co-crystal, its preparation, and use in the treatment of HIV infection. | 2012-02-02 |
20120028999 | ADMINISTRATION OF TLR7 LIGANDS AND PRODRUGS THEREOF FOR TREATMENT OF INFECTION BY HEPATITIS C VIRUS - This invention relates to methods for treating or preventing hepatitis C virus infections in mammals using Toll-Like Receptor (TLR)7 ligands and prodrugs thereof. More particularly, this invention relates to methods of orally administering a therapeutically effective amount of one or more prodrugs of TLR7 ligands for the treatment or prevention of hepatitis C viral infection. Oral administration of these TLR7 immunomodulating ligands and prodrugs thereof to a mammal provides therapeutically effective amounts and reduced undesirable side effects. | 2012-02-02 |
20120029000 | PROCESS FOR THE PREPARATION OF ALOGLIPTIN - The present invention is based on the discovery of a process for preparing pyrimidin-dione compounds, especially alogliptin and its derivatives, which comprises the reaction of a urea derivative of formula (VIII) with a malonic acid or its derivatives to form intermediates of formulae (VII) or (VII-A), which are subsequently converted to a compound of formula (II) upon introduction of a leaving group X. Compound (II) then reacts with an amine to form compound (I), which is optionally converted to its salts of formula (IV). | 2012-02-02 |
20120029001 | METHOD OF TREATMENT OF NEPHROGENIC DIABETES INSIPIDUS - Nephrogenic diabetes insipidus is treated with statins. | 2012-02-02 |
20120029002 | BENZIMIDAZOLE AND PYRAZOLOPYRIDINE DERIVATIVES FOR TREATING AND/OR PREVENTING CARDIOVASCULAR DISEASES - The present application relates to novel fused, heteroatom-bridged pyrazole and imidazole derivatives, to processes for their preparation, to their use, alone or in combination, 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. | 2012-02-02 |
20120029003 | GALECTIN-3 AND STATIN THERAPY - Described herein are materials and methods for predicting and monitoring a heart failure patient's physiological response to treatment with a statin. More specifically, the present invention relates to the endogenous protein galectin-3 and its use as a predictor of response to treatment with 3-hydroxy-3-methylglutaryl coenzyme-A reductase inhibitors, or statins. | 2012-02-02 |
20120029004 | NOVEL AMINOPYRIDINE DERIVATIVES HAVING AURORA A SELECTIVE INHIBITORY ACTION - The present invention relates to a compound of Formula (I): wherein: R | 2012-02-02 |
20120029005 | SPIPERONE DERIVATIVES AND METHODS OF TREATING DISORDERS - Described herein are spiperone derivative compounds which have been found to be useful in methods of stimulating CaCC and treating disorders (or symptoms thereof) associated with CaCC including cystic fibrosis, wherein a compound of the invention is administered to a subject. | 2012-02-02 |
20120029006 | Cis-tetrahydro-spiro(cyclohexane-1,1'-pyrido[3,4-b]indole)-4-amine Compounds - Cis-tetrahydro-spiro(cyclohexane-1,1′-pyrido[3,4-b]indole)-4-amine compounds which act on the nociceptin/ORL-1 receptor system as well as on the μ-opioid receptor system and which are distinguished in particular by selective effectiveness in the treatment of chronic pain, such as inflammatory pain, visceral pain, tumour pain, and neuropathic pain, without at the same time developing pronounced effectiveness against acute, nociceptive pain. | 2012-02-02 |
20120029007 | MORPHINAN COMPOUNDS - This invention relates to novel morphinan compounds and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a σ | 2012-02-02 |
20120029008 | CRYSTALLINE AND AMORPHOUS FORMS OF NALBUPHINE HYDROCHLORIDE - The present invention is directed to novel crystalline and amorphous forms of nalbuphine hydrochloride. | 2012-02-02 |
20120029009 | Tacrolimus For Improved Treatment Of Transplant Patients - An extended release oral dosage form comprising as active substance tacrolimus or a pharmaceutically active analogue thereof for a once daily immunosuppressive treatment of a patient in need thereof, preferable a kidney or liver transplant patient. The dosage form releases the active substance over an extended period of time. It also provides improved pharmacokinetic parameters due to an extended and constant in vivo release including substantial decreased peak concentrations, despite increased bioavailability, substantial extended times for maximal concentration, and higher minimal concentrations when compared with conventional immediate release dosage forms and a recent modified release tacrolimus dosage form. | 2012-02-02 |
20120029010 | METHOD TO USE COMPOSITIONS HAVING ANTIDEPRESSANT ANXIOLYTIC AND OTHER NEUROLOGICAL ACTIVITY AND COMPOSITIONS OF MATTER - The sponges were collected from a variety of locations in the Florida Keys and separated based on morphology and color. The samples were identified as three species, two of which are well known: | 2012-02-02 |
20120029011 | NOVEL NITROGEN-CONTAINING HETEROARYL COMPOUNDS AND METHODS OF USE THEREOF - The present invention relates to compounds suitable for use in mediating hypoxia inducible factor and for treating erythropoietin-associated conditions by increasing endogenous erythropoietin in vitro and in vivo. | 2012-02-02 |
20120029012 | 5, 6, or 7-SUBSTITUTED -3-(HETERO) ARYLISOQUINOLINAMINE DERIVATIVES AND THERAPEUTIC USE THEREOF - The present invention relates to 5, 6, or 7-substituted-3-(hetero)arylisoquinolinamine derivatives represented by general formula D, their pharmacologically acceptable salts thereof, and compositions containing such compounds. Methods for treating hyperproliferative disorders by administering the compounds are also included. | 2012-02-02 |
20120029013 | DERIVATIVES OF AMINOCYCLOBUTANE OR AMINOCYCLOBUTENE, THEIR METHOD OF PREPARATION AND THEIR USE AS MEDICAL PRODUCTS - The present invention concerns compounds of general formula (1), where in:—-a- is a single or double bond, Ar is an aromatic group, substituted or unsubstituted, R1 and R2 each independently or together are: a hydrogen atom or C | 2012-02-02 |
20120029014 | 5-(2--1-HYDROXYETHYL)-8-HYDROXYQUINOLIN-2 (1H)-ONE FOR THE TREATMENT OF LUNG FUNCTION - A compound which is a hydroxyquinolinone derivative of formula (I), | 2012-02-02 |
20120029015 | Novel medical use of kynurenic acid, its precursors and derivatives - The invention relates to the use of kynurenic acid derivatives of general formula (I), | 2012-02-02 |
20120029016 | Indoles Useful in the Treatment of Inflammation - There is provided compounds of formula I, wherein ring R | 2012-02-02 |
20120029017 | PECTIN-CONTAINING JELLY FORMULATION - There is disclosed a technique for making a jelly formulation comprising pectin slide out of a container easily (improving the slidability of the jelly formulation) when taking the formulation out of the container to prevent the formulation from remaining in the container. The jelly formulation of the present invention comprises a drug, pectin, divalent metal ions, and polyoxyethylene polyoxypropylene glycol. | 2012-02-02 |
20120029018 | 9-SUBSTITUTED PHENANTHRENE BASED TYLOPHORINE DERIVATIVES - The present invention provides compounds of Formula I: compositions containing the same, and methods of use thereof such as for the treatment of cancer. | 2012-02-02 |
20120029019 | POLYMORPHIC FORMS OF 3-(4-AMINO-1-OXO-1,3 DIHYDRO-ISOINDOL-2-YL)-PIPERIDINE-2,6-DIONE - Polymorphic forms of 3-(4-amino-1-oxo-1,3 dihydro-isoindol-2-yl)-piperidine-2,6-dione are disclosed. Compositions comprising the polymorphic forms, methods of making the polymorphic forms and methods of their use are also disclosed. | 2012-02-02 |
20120029020 | POLYMORPHIC FORMS OF 3-(4-AMINO-1-OXO-1,3 DIHYDRO-ISOINDOL-2-YL)-PIPERIDINE-2,6-DIONE - Polymorphic forms of 3-(4-amino-1-oxo-1,3 dihydro-isoindol-2-yl)-piperidine-2,6-dione are disclosed. Compositions comprising the polymorphic forms, methods of making the polymorphic forms and methods of their use are also disclosed. | 2012-02-02 |
20120029021 | Nitroxide Free Radical Synergized Antineoplastic Agents - Nitroxide free radicals attached to antineoplastic agents can synergize their potencies to cancer cells. This invention relates to any antineoplastic agents and their derivatives chemically attached with nitroxide free radicals, such as TEMPO and its radical derivatives. This invention also relates to precursors of such compounds, as well as the products formed from the adducts after administration. | 2012-02-02 |
20120029022 | Potent Non-Urea Inhibitors Of Soluble Epoxide Hydrolase - The present invention relates to compounds that exhibit vasodilatory and anti-inflammatory effects by inhibiting the activity of soluble epoxide hydrolase (sEH). The present invention is also directed to methods of identifying such compounds, and use of such compounds for the treatment of diseases related to dysfunction of vasodilation, inflammation, and/or endothelial cells. In particular non-limiting embodiments, components of the invention may be used to treat hypertension. | 2012-02-02 |
20120029023 | HETEROCYCLES SUBSTITUTED PYRIDINE DERIVATIVES AND ANTIFUNGAL AGENT CONTAINING THEREOF - An object of the present invention is to provide an antifungal agent which has excellent antifungal effects and is superior in terms of its physical properties, safety and metabolic stability. According to the present invention, there is disclosed a compound represented by the following formula (I), or a salt thereof: | 2012-02-02 |
20120029024 | SPOT-ON PESTICIDE COMPOSITION - A spot-on pesticide composition for animals, specifically mammals, including dogs and cats, which composition comprises a combination of active components, including fipronil and a pyrethroid, and optionally an insect growth regulator, in doses and proportions which are parasiticidally effective against a variety of insects and pests, and in a formulation which is convenient for local application to the animal's skin, preferably localized over a small surface area. | 2012-02-02 |
20120029025 | SPOT-ON PESTICIDE COMPOSITION - A spot-on pesticide composition for animals, specifically mammals, including dogs and cats, which composition comprises a combination of active components, including fipronil and a pyrethroid, and optionally an insect growth regulator, in doses and proportions which are parasiticidally effective against a variety of insects and pests, and in a formulation which is convenient for local application to the animal's skin, preferably localized over a small surface area. | 2012-02-02 |
20120029026 | PYRIDINE 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): | 2012-02-02 |
20120029027 | N-[(6-AZA-BICYCLO[3.2.1]OCT-5-YL)-ARYL-METHYL]-HETEROBENZAMIDE DERIVATIVES, PREPARATION THEREOF, AND THERAPEUTIC USE OF SAME - The invention relates to a compound of the general formula (I), where: R is a hydrogen atom or a group selected from the (C | 2012-02-02 |
20120029028 | Compositions and methods for treating hyperlipidemias - The present invention is directed to a composition and method for the treatment of hyperlipidemias by targeting Microsomal triglyceride transfer protein (MTP). In particular, the present invention is directed to a combination of at least one MTP inhibitor and at least one lipid-lowering agent, both in an amount effective to treat hyperlipidemias. | 2012-02-02 |
20120029029 | SUBSTITUTED THIAZOL-2-YLAMINE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS, AND METHODS OF USE AS 11-BETA HSD1 MODULATORS - The present invention is directed to substituted thiazol-2-ylamine derivatives and pharmaceutically acceptable salts thereof that inhibit 11βHSD1 and that may be useful in the treatment of diseases in which modulation or inhibition of 11βHSD1 is beneficial or where a reduction in intracellular glucorticoid levels is desirable. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases, disorders, or conditions in which modulation or inhibition of 11βHSD1 is beneficial or where a reduction in intracellular glucorticoid levels is desirable. | 2012-02-02 |
20120029030 | METHOD FOR CUSTOMIZED DISPENSING OF VARIABLE DOSE DRUG COMBINATION PRODUCTS FOR INDIVIDUALIZING OF THERAPIES - Generally the method involves identifying the concentration of each of two or more active therapeutics tailored to treat a particular patient's unique metabolism and one or more diseases, communicating that information to a producer who has multiple fixed or variable concentrations of each active available, where the producer then combines the individual concentrations of each active into single units such as a tablets or pills, and distributes those indirectly or directly to the patient. | 2012-02-02 |
20120029031 | METADOXINE FOR USE AS INHIBITOR OF HEPATIC FIBROSIS - The use of metadoxine in the treatment of hepatic fibrosis is described. Metadoxine can be orally and/or parenterally administered at a dosage comprised between 50 and 1000 mg per dose, preferably between 300 and 600 mg per dose. In the in vitro study, metadoxine results effective at lower concentrations with respect to those that are obtained in the plasma after oral administration at the doses recommended for conventional pathology. | 2012-02-02 |
20120029032 | MATRIX-TYPE SUSTAINED RELEASE PREPARATION CONTAINING BASIC ADDITIVE - Disclosed is a matrix-type sustained release preparation containing a basic drug unstable against an acid as an active pharmaceutical ingredient, wherein the decomposition of the basic drug unstable against the acid can be prevented and therefore the pH-dependent release can be reduced. A hardly water-soluble basic normal salt is added to a matrix-type sustained release preparation containing a basic drug that is unstable against an acid. | 2012-02-02 |
20120029033 | SPOT-ON PESTICIDE COMPOSITION - A spot-on pesticide composition for animals, specifically mammals, including dogs and cats, which composition comprises a combination of active components, including fipronil and a pyrethroid, and optionally an insect growth regulator, in doses and proportions which are parasiticidally effective against a variety of insects and pests, and in a formulation which is convenient for local application to the animal's skin, preferably localized over a small surface area. | 2012-02-02 |
20120029034 | Novel calcium salts of Compound as Anti-Inflammatory, Immunomodulatory and Anti-Proliferatory Agents - The present invention relates to calcium salts of compounds of the general formula (I) | 2012-02-02 |
20120029035 | COMPOSITIONS AND METHODS FOR EXTENDED THERAPY WITH AMINOPYRIDINES - Disclosed herein are methods and compositions related to use of aminopyridines, such as 4-aminopyridine, for use in a therapeutically effective manner for patients with a demyelinating condition, such as multiple sclerosis. | 2012-02-02 |
20120029036 | PHARMACEUTICAL COMPOSITIONS COMPRISING PYRIDYL CYANOGUANIDINE, PROCESS FOR PREPARING THE SAME AND USE THEREOF - Disclosed are a composition comprising a pyridyl cyanoguanidine and a cyclodextrin, a cyclodextrin derivative and/or a surfactant with solubilization, process for preparing the same and use thereof. | 2012-02-02 |
20120029037 | ANIMAL ECTOPARASITE-CONTROLLING AGENT - The present invention provides an animal ectoparasite-controlling agent containing as an active ingredient a hydrazide compound represented by the formula (1) | 2012-02-02 |
20120029038 | ANIMAL ECTOPARASITE-CONTROLLING AGENT - The present invention provides an animal ectoparasite-controlling agent containing as an active ingredient a hydrazide compound represented by the formula (1) | 2012-02-02 |
20120029039 | ANIMAL ECTOPARASITE-CONTROLLING AGENT - The present invention provides an animal ectoparasite-controlling agent containing as an active ingredient a hydrazide compound represented by the formula (1) | 2012-02-02 |
20120029040 | ANIMAL ECTOPARASITE-CONTROLLING AGENT - The present invention provides an animal ectoparasite-controlling agent containing as an active ingredient a hydrazide compound represented by the formula (1) | 2012-02-02 |