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Nitrogen attached indirectly to the six-membered hetero ring by nonionic bonding

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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

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Entries
DocumentTitleDate
20100267779Novel Compounds and Methods of Using Them - Described herein are novel HDAC inhibitors, formulations containing them and methods of using them. In some embodiments, the HDAC inhibitors possess specific stereochemistry. In other embodiments, the compounds described herein are used in the treatment or prevention of histone deacetylase mediated disorders.10-21-2010
20100056585N-(2-Aminophenyl)-4-[N-(Pyridine-3-yl)-Methoxycarbonyl-Aminomethyl]-Benzam- ide (MS-275) Polymorph B - The crystalline Polymorph B of N-(2-aminophenyl)-4-[N-(pyridine-3-yl)methoxy-carbonyaminomethyl]benzamide (MS-275) of formula I03-04-2010
20090192202ANDROGEN MODULATORS - The present invention is directed to a new class of 4-cyano-phenoxy-alkyl carboxyl derivatives and to their use as androgen receptor modulators. Other aspects of the invention are directed to the use of these compounds to decrease excess sebum secretions and to stimulate hair growth.07-30-2009
20110196001METHOD TO CONTROL INSECTS RESISTANT TO COMMON INSECTICIDES - N-Substituted sulfoximines are effective at controlling insects resistant to common insecticides.08-11-2011
20130030026ALKYNYL PHENYL DERIVATIVE COMPOUNDS FOR TREATING OPHTHALMIC DISEASES AND DISORDERS - Provided are alkynyl phenyl derivative compounds, pharmaceutical compositions thereof, and methods of treating ophthalmic diseases and disorders, such as age-related macular degeneration and Stargardt's Disease, using said compounds and compositions.01-31-2013
20130079376PYRIDYL-2-METHYLAMINO COMPOUNDS, COMPOSITIONS AND USES THEREOF - Compounds are provided according to formula I:03-28-2013
20130079377Aryl or N-heteroaryl Substituted Methanesulfonamide Derivatives as Vanilloid Receptor Ligands - The invention relates to aryl or N-heteroaryl substituted methanesulfonamide derivatives as vanilloid receptor ligands, to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseases and/or disorders.03-28-2013
20100324103Substituted Enaminocarbonyl Compounds - The present application relates to substituted enaminocarbonyl compounds of the formula (I)12-23-2010
20100041717N-((3-BENZYL)-2,2-(BIS-PHENYL)-PROPAN-1-AMINE DERIVATIVES AS CETP INHIBITORS FOR THE TREATMENT OF ATHEROSCLEROSIS AND CARDIOVASCULAR DISEASES - Compounds of formula (Ia) and (Ib), wherein A, B, C, R02-18-2010
20100041716NITROXIDES FOR USE IN TREATING OR PREVENTING HYPERCHOLESTEROLEMIA - Pharmaceutical compositions are provided that are useful in treating hypercholesterolemia. The compositions comprise a pharmaceutically acceptable carrier, and an effective therapeutic or prophylactic amount of a nitroxide antioxidant that alters the expression of one or more genes related to hypercholesterolemia. Methods are also provided for the use of the pharmaceutical compositions in the treatment or prevention of hypercholesterolemia. In a preferred embodiment, the nitroxide antioxidant is Tempol (4-hydroxy-2,2,6,6-tetramethylpiperidine-1-oxyl).02-18-2010
20090156650COMPOSITION THAT COMPRISES AT LEAST ONE OXIME AND ITS USE IN THERAPEUTICS - This invention relates to a medication, a pharmaceutical composition. and method for the treatment of respiratory poisoning in animals and humans caused by organophosphorus compounds, whereby said medication and said pharmaceutical composition comprise at least one oxime and one blocker of organic cation transporters (OCT).06-18-2009
20080312298Methods for Identification of Modulators of Carm1 Methyl Transferase Activity - This invention relates to CARM1, CARM1 binding pockets, or CARM1-like binding pockets. The invention relates to a computer comprising a data storage medium encoded with the structure coordinates of such binding pockets. The invention also relates to methods of using the structure coordinates to solve the structure of homologous proteins or protein complexes. The invention relates to methods of using the structure coordinates to screen for and design compounds that bind to CARM1 protein, complexes of CARM1 protein, homologs thereof, or CARM1-like protein or protein complexes. The invention also relates to crystallizable compositions and crystals comprising a CARM1 protein or homologs thereof. The invention also relates to methods of identifying binders of CARM1 proteins. The invention also relates to methods for determining the intracellular activity of CARM1 methyltransferase and methods for identifying an agent that inhibits the intracellular activity of CARM1 methyltransferase.12-18-2008
20100144801MUSCARINIC RECEPTOR ANTAGONISTS - The present invention generally relates to muscarinic receptor antagonists of formula I, which are useful, among other uses, for the treatment of various diseases of the respiratory, urinary and gastrointestinal systems mediated through muscarinic receptors. The invention also relates to the process for the preparation of disclosed compounds, pharmaceutical compositions containing the disclosed compounds, and the methods for treating diseases mediated through muscarinic receptors. Formula (I) wherein Het: is heterocyclyl or heteroaryl X: O, S or NR1 and the other substituents are defined as in the claims.06-10-2010
20090124671TRPV1 ANTAGONISTS - The present invention relates to compounds of formula (I)05-14-2009
20100069447BENZAMIDE DERIVATIVES AND USES RELATED THERETO - Benzamide derivatives of formulae I and II, and pharmaceutically acceptable salts, solvates, stereoisomers, and prodrugs thereof, and pharmaceutical compositions comprising the same, are described and have therapeutic utility, particularly in the treatment of diabetes, obesity, and related conditions and disorders:03-18-2010
20130090359METHOD FOR TREATING A TRPV1-MEDIATED DISEASE - A method for treating a TRPV1-mediated disease by administering to a patient a therapeutically effective amount of a compound or a salt thereof having the following formula [I]:04-11-2013
20090088460Administration of E-3[3-[N-(4-methoxybenzenesulfonyl)-N-isopropylamino]phenyl]-3-(3-pyridyl- )propenohydroxamic acid for preventing and/or treating inflammatory cutaneous pathologies/afflictions - Inflammatory cutaneous pathologies/afflictions, e.g., eczema or psoriasis, are prevented and/or treated by administering to a subject in need of such treatment, a thus effective amount of E-3-[3-[N-(4-methoxybenzenesulfonyl)-N-isopropylamino]phenyl]-3-(3-pyridyl)propenohydroxamic acid of formula (I):04-02-2009
20090306152COOLING COSMETIC OR DERMATOLOGICAL PREPARATIONS COMPRISING (1R,2S,5R)-2-ISOPROPYL-5-METHYL-N-(2-(PYRIDIN-2-YL)ETHYL)-CYCLOHEXANE CARBOXAMIDE AND/OR (1R,2S,5R)-N-(4-CYANOMETHYL-PHENYL)-2-ISOPROPYL-5-METHYLCYCLOHEXANE CARBOXAMIDE IN COMBINATION WITH MENTHOXYPROPANEDIOL - A cooling topical cosmetic or dermatological preparation which comprises (1R,2S,5R)-2-isopropyl-5-methyl-N-(2-(pyridin-2-yl)ethyl)cyclohexane carboxamide and/or (1R,2S,5R)-N-(4-cyanomethyl-phenyl)-2-isopropyl-5-methylcyclohexane carboxamide, in combination with menthoxypropanediol.12-10-2009
20090093526INHIBITION OF P38 KINASE USING SYMMETRICAL AND UNSYMMETRICAL DIPHENYL UREAS - This invention relates to the use of a group of aryl ureas in treating cytokine mediated diseases and proteolytic enzyme mediated diseases, and pharmaceutical compositions for use in such therapy.04-09-2009
20130059894PESTICIDAL COMPOSITION AND ITS USE - A composition comprising a carboxamide compound represented by following formula (I), wherein R03-07-2013
20090076097DEUTERIUM-ENRICHED ATAZANAVIR - The present application describes deuterium-enriched atazanavir, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.03-19-2009
20090247590Indane amides - The invention relates to novel compounds and processes for their preparation and their use for preparing medicaments for the treatment of disorders, especially hyper-proliferative disorders.10-01-2009
20120115914Treatment Methods Employing Histamine H3 Receptor Antagonists, Including Betahistine - Methods of treating depression, binge eating disorder, narcolepsy, excessive daytime sleepiness, substance use disorders, and Prader Willi syndrome, disorders characterized at least in part by hypocortisolemia and decreased activity of the hypothalamic-pituitary-adrenal (HPA) axis, and disorders related to disturbances in circadian rhythm, comprising the step of administering an effective amount of a histamine type 3 (H05-10-2012
20120115913Ethanamine Compounds and Methods of Using the Same - The present invention is directed to ethanamine compounds, pharmaceutical compositions comprising the same, and methods of treating depression by administering the ethanamine compound.05-10-2012
20100041718PESTICIDAL COMPOSITIONS - A pesticidal composition comprising a pesticide, an ammonium salt, and a nonionic surfactant, is provided.02-18-2010
20120238605OTAMIXABAN FOR TREATMENT OF ELDERLY AND RENAL IMPAIRED NON-ST ELEVATION MYOCARDIAL INFARCTION PATIENTS - The invention relates to the use of (2R,3R)-2-(3-carbamimidoyl-benzyl)-3-[4-(1-oxy-pyridin-4-yl)benzoylamino]-butyric acid methyl ester or a pharmaceutically acceptable salt thereof, for the preparation of a medicament for use in non-ST elevation myocardial infarction, said treatment comprising administering a therapeutically effective amount of (2R,3R)-2-(3-Carbamimidoyl-benzyl)-3-[4-(1-oxy-pyridin-4-yl)benzoylamino]-butyric acid methyl ester or a pharmaceutically acceptable salt thereof to a human patient, who is elderly and/or shows renal insufficiency and/or has a low body weight.09-20-2012
20110124689PROCESS FOR PREPARING ATAZANAVIR BISULFATE AND NOVEL FORMS - A process is provided for preparing the HIV protease inhibitor atazanavir bisulfate wherein a solution of atazanavir free base is reacted with concentrated sulfuric acid in an amount to react with less than about 15% by weight of the free base, seeds of Form A crystals of atazanavir bisulfate are added to the reaction mixture, and as crystals of the bisulfate form, additional concentrated sulfuric acid is added in multiple stages at increasing rates according to a cubic equation, to effect formation of Form A crystals of atazanavir bisulfate.05-26-2011
20100204284HETERO-SUBSTITUTED ACETANILIDE DERIVATIVES AS ANALGESIC AGENTS - Hetero-substituted acetanilide derivatives are disclosed as analgesic agents. The compounds of the invention are useful in methods for treating a disease or condition in a mammal characterized by pain and/or fever.08-12-2010
20080319029Bifenthrin/Acetamiprid Compositions for Control of General Household Pests - The present invention relates to an insecticidal composition of bifenthrin and acetamiprid with significantly improved knockdown and mortality characteristics when applied to general household pests.12-25-2008
20090298892Treatment Methods Employing Histamine H3 Receptor Antagonists, Including Betahistine - Methods of treating depression, binge eating disorder, narcolepsy, excessive daytime sleepiness, substance use disorders, and Prader Willi syndrome, disorders characterized at least in part by hypocortisolemia and decreased activity of the hypothalamic-pituitary-adrenal (HPA) axis, and disorders related to disturbances in circadian rhythm, comprising the step of administering an effective amount of a histamine type 3 (Bb) receptor antagonist, such as betahistine or its pharmaceutically acceptable salts, or its metabolites to an individual.12-03-2009
20090176845SUBSTITUTED 2-AMINOTETRALIN DERIVATIVES AS SELECTIVE ALPHA 2B AGONIST - Substituted 2-aminotetralin derivatives as selective alpha 2B agonists includes a compound represented by Formula 1:07-09-2009
20110288135Fast Dissolving Tablet - The present invention relates to processes for the preparation of tablets which dissolve rapidly in the mouth and provide an excellent mouthfeel. The tablets of the invention comprise a compound which melts at about 37° C. or lower, have a low hardness, high stability and generally comprise few insoluble disintegrants which may cause a gritty or chalky sensation in the mouth. Convenient and economically feasible processes by which the tablets of the invention may be produced are also provided.11-24-2011
20100035941METHODS FOR INCREASING BLOOD FLOW AND/OR PROMOTING TISSUE REGENERATION - Methods for increasing blood flow and/or regenerating tissue using compounds which bind to the chemokine receptor CXCR4 are disclosed. Preferred embodiments of such compounds are of the formula Z-linker-Z′) wherein Z is a cyclic polyamine containing 9-32 ring members of which 2-8 are nitrogen atoms, said nitrogen atoms separated from each other by at least 2 carbon atoms, and wherein said heterocycle may optionally contain additional heteroatoms besides nitrogen and/or may be fused to an additional ring system; or Z is of the formula (I) wherein A comprises a monocyclic or bicyclic fused ring system containing at least one N and B is H or an organic moiety of 1-20 atoms; Z′ may be embodied in a form as defined by Z above, or alternatively may be of the formula —N(R)—(CR02-11-2010
20100267780BICYCLIC ARYL AND HETEROARYL RECEPTOR MODULATORS - Compounds of formula (I) or pharmaceutically acceptable salts thereof, are opioid receptor modulators, e.g. mu-opioid receptor antagonists, neutral antagonists or inverse agonists, and are useful inter alia for the treatment of obesity.10-21-2010
20090149511Administration of an Inhibitor of HDAC and an mTOR Inhibitor - Methods of treating patients with an HDAC inhibitor and an mTOR inhibitor are provided.06-11-2009
20100120872ORGANIC COMPOUNDS AND THEIR USES - The present application describes organic compounds that are useful for the treatment, prevention and/or amelioration of human diseases.05-13-2010
20100249197CARBAMIC ACID COMPOUNDS COMPRISING AN AMIDE LINKAGE AS HDAC INHIBITORS - This invention pertains to certain active carbamic acid compounds which inhibit HDAC activity and which have the formula (1) wherein: A is an aryl group; Q09-30-2010
20120071520CRYSTALLINE PHASES OF 2'--BIPHENYL-2-CARBOXYLIC ACID (2-PYRIDIN-3-YL-ETHYL)-AMIDE - The present invention relates to polymorphic forms and solvates of 2′-{[2-(4-methoxy-phenyl)-acetylamino]-methyl]}-biphenyl-2-carboxylic acid (2-pyhdin-3-yl-ethyl)-amide, processes for their preparation and their use, in particular for the preparation of medicaments.03-22-2012
20090281150Compound 249 - A pharmaceutical depot comprising (i) N-{5-[(cyclopropylamino)carbonyl]-2-methylphenyl}-3-fluoro-11-12-2009
20090281149Amine Derivative Compounds for Treating Ophthalmic Diseases and Disorders - Provided are amine derivative compounds, pharmaceutical compositions thereof, and methods of treating ophthalmic diseases and disorders, such as age-related macular degeneration and Stargardt's Disease, using said compounds and compositions.11-12-2009
20090291989ISOTHIOCYANATE COMPOUNDS, PHARMACEUTICAL COMPOSITIONS, AND USES THEREOF - Provided herein are compositions of matter and pharmaceutical compositions thereof, for use in inhibiting the growth of various microbial pathogens, including bacteria, fungi, protozoa, and viral pathogens. Also provided herein are methods of treating microbial diseases/infections and cancer with the compositions. The compositions are additionally useful in wood preservation and food preservation by inhibition of microbial growth.11-26-2009
20100113536 HALOALKYLSULFONE SUBSTITUTED COMPOUNDS USEFUL FOR TREATING OBESITY AND DIABETES - The present invention relates to novel compounds of formula [I], wherein R05-06-2010
20090170909ALPHA KETOAMIDE COMPOUNDS AS CYSTEINE PROTEASE INHIBITORS - The present invention is directed to compounds that are inhibitors of cysteine proteases, in particular, cathepsins B, K, L, F, and S and are therefore useful in treating diseases mediated by these proteases. The present invention is directed to pharmaceutical compositions comprising these compounds and processes for preparing them.07-02-2009
20080221176Chemical Compounds - This invention relates to compounds that are modulators of the liver X receptors (LXRs), and also to the methods for the making and use of such compounds.09-11-2008
20090264480TRPA1 ANTAGONISTS - Compounds of formula (I)10-22-2009
20090264479Papain Family Cysteine Protease Inhibitors for the Treatment of Parasitic Diseases - Several parasites responsible for mammalian diseases are dependent on cysteine protease for various life-cycle functions. Inhibition of these proteases can be useful in the treatment of these parasitic diseases, including toxoplasmosis, malaria, African trypanosomiasis, Chagas disease, leishmaniasis or schistosomiasis.10-22-2009
20090182020SUBSTITUTED BIS(HETERO)AROMATIC N--ETHYLPROPIOLAMIDES AND USE THEREOF FOR PRODUCTION OF MEDICAMENTS - The present invention relates to substituted bis(hetero)aromatic N-ethylpropiolamides, methods for the production thereof, medicaments containing these compounds and the use thereof for the production of medicaments.07-16-2009
20090088459NOVEL BIARYL SULFONAMIDE DERIVATIVES - The invention is concerned with novel biaryl sulfonamide derivatives of formula (I)04-02-2009
20090182019Histone deacetylase inhibitors - The present invention provides novel HDAC inhibitors and methods of treating diseases using the same.07-16-2009
20090326014Use of 5-ht7 receptor agonists for the treatment of pain - The present invention refers to the use of 5-HT12-31-2009
20090054500Composition and methods useful in preventing cardiac hypertrophy - The present invention is directed to compositions and methods that can be used for preventing the hypertrophy of cardiac cells. The compositions and methods involve the use of compounds that lead to an increase in the cellular activity of the transcription factor CHF1.02-26-2009
20090005426PHARMACEUTICALLY ACTIVE SULFONYL HYDRAZIDE DERIVATIVES - Sulfonyl hydrazide compounds according to formula I01-01-2009
20080262048CONTROL OF PARASITES IN ANIMALS BY THE USE OF NOVEL TRIFLUOROMETHANESULFONANILIDE OXIME ETHER DERIVATIVES - Novel trifluoromethanesulfonanilide oxime ether compounds useful for controlling endo and/or ectoparasites in the environment are provided, together with methods of making the same, and methods of using the inventive compounds to treat parasite infestations in vivo or ex vivo.10-23-2008
20090203749AGENT FOR CONTROL OF DEGRANULATION REACTION AND CYTOKINE PRODUCTION - To provide an agent capable of controlling the degranulation reaction and/or cytokine production of mast cell and the like. The present invention provides an agent for controlling a degranulation reaction and an agent for controlling a cytokine production, comprising a substance capable of controlling an intracellular zinc ion concentration, particularly, a zinc ion, a zinc ion chelator, an agent for controlling the expression and/or function of a zinc ion-requiring protein, or an agent for controlling the expression and/or function of a zinc ion transporter, as an active ingredient.08-13-2009
20090253755N-[(PYRIDIN-2-YL) METHOXY] BENZAMIDE DERIVATIVES AND RELATED COMPOUNDS AS FUNGICIDES - A compound of general formula (I):10-08-2009
20090221652COMBINATIONS OF METFORMIN AND MEGLITINIDE - Methods of treating glucose related disorders, for example by administering a meglitinide such as mitiglinide, repaglinide, or nateglinide, optionally in combination with a biguanide such as metformin, are described herein.09-03-2009
20100184812MUTUAL PRODRUGS AND METHODS TO TREAT CANCER - Mutual prodrugs comprising retinoids and histone deacetylase inhibitors, methods for production of the mutual prodrugs, and methods of treatment comprising administration of the mutual prodrugs. The retinoids include all-trans retinoic acid, 13-cis retinoic acid, and retinoic acid analogs that have a substitution at C-4. Further, the mutual prodrugs of the present invention can be used as therapeutic agents for the treatment of cancer and dermatological diseases and conditions. Pharmaceutical compositions comprising the mutual prodrugs.07-22-2010
20130123307METHOD TO CONTROL INSECTS RESISTANT TO COMMON INSECTICIDES - N-Substituted sulfoximines are effective at controlling insects resistant to common insecticides.05-16-2013
20100227898NOVEL MICROBIOCIDES - Compounds of the formula (I) in which the substituents are as defined in claim 09-09-2010
20100227897Composition for Controlling Colorado Potato Beetles - The present invention relates to an insecticidal composition suitable for use in controlling Colorado potato beetles comprising zeta-cypermethrin and a second insecticide selected from the group consisting of acetamiprid and fipronil.09-09-2010
20100222397Use of Succinate Dehydrogenase Inhibitors For Controlling Powdery Mildew Primary Infections - The present invention relates to the use of succinate dehydrogenase Inhibitors for controlling powdery mildew primary infections in crops and to a method for controlling those primary infections.09-02-2010
20100240713AROMATIC AND HETEROAROMATIC COMPOUNDS USEFUL IN TREATING IRON DISORDERS - This invention is directed to compounds of formula (I), wherein m, formula (II), R09-23-2010
20080312297Substituted Oxyguanidines - The present application relates to new substituted oxyguanidines of structure (I)12-18-2008
200900760962-Pyridinylcycloalkylbenzamide derivatives and their use as fungicides - A compound of general formula (I):03-19-2009
20100144802Small Molecule Inhibitors for Immune Modulation - Methods of treating immunosuppression by administering a therapeutic amount of a tryphostin compound of the formula:06-10-2010
20100144803INSECTICIDAL N-SUBSTITUTED (6-HALOOALKYLPYRIDIN-3-YL)-ALKYL SULFOXIMINES - N-Substituted (6-haloalkylpyridin-3-yl)alkyl sulfoximines are effective at controlling insects.06-10-2010
20100204283PESTICIDE COMPOSITION POTENTIATED IN EFFICACY AND METHOD FOR POTENTIATING EFFICACY OF PESTICIDAL ACTIVE INGREDIENTS - The present invention provides a pesticide composition comprising a pesticidal active ingredient and a compound represented by chemical formula (I) or chemical formula (II)08-12-2010
20130137731ETHANAMINE COMPOUNDS AND METHODS OF USING THE SAME - The present invention is directed to ethanamine compounds, pharmaceutical compositions comprising the same, and methods of treatingh depression by administering the ethanamine compound.05-30-2013
200900365012-Cyclopenten-1-One Oxime Derivatives Inhibiting Production of TNF-Alpha - 2-cyclopenten-1-one oxime derivatives represented by Formula (I), or pharmaceutically acceptable salts thereof inhibit the production of TNF-α or PDE4, and therefore show therapeutic effect in inflammatory or immunological disorders mediated through TNF-α or PDE4.02-05-2009
20080249142HYDROXYBENZOATE SALTS OF METANICOTINE COMPOUNDS - Patients susceptible to or suffering from conditions and disorders, such as central nervous system disorders, are treated by administering to a patient in need thereof compositions that are hydroxybenzoate salts of E-metanicotine-type compounds. The formation of hydroxybenzoate salts of the E-metanicotine compounds is also useful in purifying the E-metanicotine compounds, as the hydroxybenzoate salts tend to crystallize out, leaving impurities such as Z-metanicotine compounds, and compounds where the double bond has migrated, in solution. If desired, the hydroxybenzoate salts can be converted to either the free base (the E-metanicotine compound) or to another pharmaceutically acceptable salt form.10-09-2008
20090291988Reversible Inhibitors of Monoamine Oxidase A and B - The instant invention relates to compounds of formula I, diagrammed below, wherein R3, E, D and Y are defined in the application, which are useful as reversible inhibitors of monoamine oxidase-B and/or monoamine oxidase-A, and therefore useful to treat or prevent neurological diseases or conditions in mammals, preferably humans.11-26-2009
20090062353Alkynyl phenyl derivative compounds for treating ophthalmic diseases and disorders - Provided are alkynyl phenyl derivative compounds, pharmaceutical compositions thereof, and methods of treating ophthalmic diseases and disorders, such as age-related macular degeneration and Stargardt's Disease, using said compounds and compositions.03-05-2009
20080200525PESTICIDALLY ACTIVE KETONE AND OXIME DERIVATIVES - Compounds of formula08-21-2008
20120277272Ethanamine Compounds and Methods of Using the Same - (S)-2-methyl-11-01-2012
20080214628Compounds Capable of Activating Cholinergic Receptors - Compounds incorporating aryl substituted olefinic amine are provided. Representative compounds are (4E)-N-methyl-5-(3-pyridyl)-4-penten-2-amine, (4E)-N-methyl-5-(5-pyrimidinyl)-4-penten-2-amine, (4E)-N-methyl-5-(5-methoxy-3-pyridyl)-4-penten-2-amine, (4E)-N-methyl-5-(6-amino-5-methyl-3-pyridyl)-4-penten-2-amine, (2R)-(4E)-N-methyl-5-(3-pyridyl)-4-penten-2-amine, (2R)-(4E)-N-methyl-5-(5-isopropoxy-3-pyridyl)-4-penten-2-amine, (4E)-N-methyl-5-(5-bromo-3-pyridyl)-4-penten-2-amine, (4E)-N-methyl-5-(5-ethoxy-3-pyridyl)-4-penten-2-amine, (2S)-(4E)-N-methyl-5-(3-pyridyl)-4-penten-2-amine, (4E)-N-methyl-5-(5-isopropoxy-3-pyridyl)-4-penten-2-amine and (2S)-(4E)-N-methyl-5-(5-isopropoxy-3-pyridyl)-4-penten-2-amine.09-04-2008
20110053992Novel Inhibitors of Proliferation and Activation of Signal Transducer and Activator of Transcription (STATS) - Pyridine compounds effective in modulation STAT3 and/or STAT5 activation are provided that are useful in the prevention and treatment of proliferative disease and conditions including cancer, inflammation and proliferative skin disorders.03-03-2011
20110053991Treatment of Histone Deacetylase Mediated Disorders - Provided herein are pharmaceutical agents, pharmaceutical compositions, methods of treatment, treatment regimens and kits for the treatment of histone deacetylase mediated disorders.03-03-2011
20120302611PESTICIDAL COMPOSITIONS AND RELATED METHODS - Pesticidal compositions that improve soil residual efficacy of sulfoxaflor are disclosed.11-29-2012
20100324102N-(3-PYRIDIN-2-YLPROPYL) BENZAMIDE DERIVATIVES AS FUNGICIDES - A compound of general formula (I)12-23-2010
20100179199Ethanamine Compounds and Methods of Using the Same 545 - The present invention is directed to ethanamine compounds, pharmaceutical compositions comprising the same, and methods of treating depression by administering the ethanamine compound.07-15-2010
20090318511SELECTIVE HYDROXAMATE BASED MMP INHIBITORS - The present invention provides a compound of formula (I):12-24-2009
20110201655PHARMACEUTICAL COMPOSITION IMPROVING INTESTINAL ABSORPTION - An object of the present invention is to provide a pharmaceutical composition that improves intestinal absorption of a compound having a structure represented by the general formula [1]. The composition containing a compound represented by the general formula [1] or a salt thereof and (b) a lipophilic substance improves intestinal absorption of the compound. In the formula, A represents —(NR08-18-2011
20100016379Terephthalamate Compounds and Compositions, and Their Use as HIV Integrase Inhibitors - Described herein are compounds having a terephthalamate structural feature. Also described herein, are methods of making such compounds, methods of using such compounds to modulate the activity of HIV integase, and pharmaceutical compositions and medicaments comprising such compounds. Also described herein are methods of using such compounds, pharmaceutical compositions and medicaments to treat and/or prevent and/or inhibit and/or ameliorate the pathology and/or symptomology of AIDS or infection with HIV.01-21-2010
20110003869Use of Succinate Dehydrogenase Inhibitors for Controlling Sclerotinia ssp. - The invention relates to the use of succinate dehydrogenase inhibitors, especially of fluopyram, for controlling 01-06-2011
200902037505-HT2C Receptor Agonists as Anorectic Agents - This invention relates to compounds which modulate receptors of the 5-HT2 family of receptors, and particularly to compounds which modulate 5-HT2C receptors. Compounds of the invention include agonists and selective agonists for the 5-HT2C receptor Compounds of the invention include selective agonists for the 5-HT2C receptor which exhibit significantly less or no agonist activity on the 5-HT2A receptor and/or the 5-HT2B receptor. Compounds of this invention are those of Formula I and pharmaceutically acceptable salts, esters and solvates (including hydrates) wherein variables are defined in the specification hereof.08-13-2009
20100305167Administration of an Inhibitor of HDAC - Methods of treating patients with SNDX-275 are provided.12-02-2010
20100016380TNF-alpha production inhibitors - A compound having the following formula01-21-2010
20120041037COMPOSITION THAT COMPRISES AT LEAST ONE OXIME AND ITS USE IN THERAPEUTICS - A medication, a pharmaceutical composition, and method for the treatment of respiratory poisoning in animals and humans caused by organophosphorus compounds, whereby said medication and said pharmaceutical composition comprise at least one oxime and one blocker of organic cation transporters (OCT).02-16-2012
20120041036SUBSTITUTED ACYLGUANIDINE DERIVATIVES (AS AMENDED) - An object of the present invention is to provide an excellent agent for treating or preventing dementia, schizophrenia based on serotonin 5-HT02-16-2012
20120041039AMINE DERIVATIVE COMPOUNDS FOR TREATING OPHTHALMIC DISEASES AND DISORDERS - Provided are amine derivative compounds, pharmaceutical compositions thereof, and methods of treating ophthalmic diseases and disorders, such as age-related macular degeneration and Stargardt's Disease, using said compounds and compositions.02-16-2012
20120041038AMINE DERIVATIVE COMPOUNDS FOR TREATING OPHTHALMIC DISEASES AND DISORDERS - Provided are amine derivative compounds, pharmaceutical compositions thereof, and methods of treating ophthalmic diseases and disorders, such as age-related macular degeneration and Stargardt's Disease, using said compounds and compositions.02-16-2012
20120004269Alkynyl Phenyl Derivative Compounds for Treating Ophthalmic Diseases and Disorders - Provided are alkynyl phenyl derivative compounds, pharmaceutical compositions thereof, and methods of treating ophthalmic diseases and disorders, such as age-related macular degeneration and Stargardt's Disease, using said compounds and compositions.01-05-2012
20090281151PESTICIDAL COMPOSITION COMPRISING A 2-PYRDILMETHYLBENZAMIDE DERIVATIVE AND AN INSECTICIDE COMPOUND - A composition comprising at least a pyridylmethylbenzamide derivative of general formula (I) (A) and an insecticide compound (B) in a (A)/(B) weight ratio of from 1/1000 to 1000/1; a composition further comprising an additional fungicidal compound and a method for preventively or curatively combating the pests and diseases of crops by using this composition.11-12-2009
20120010253Fungicidal compositions comprising Fluopyram and Metrafenone - Fungicidal compositions comprising as active components Fluopyram and Metrafenone in a synergistically effective amount, methods for controlling phytopathogenic harmful fungi using mixtures of Fluopyram and Metrafenone, the use of Fluopyram and Metrafenone for preparing such mixtures, and also compositions and seed comprising such mixtures.01-12-2012
20110166190METHODS OF TREATING MAMMALS WITH EUSTACHIAN TUBE DYSFUNCTIONS - The invention relates to methods of medically treating mammals with Eustachian tube dysfunctions, such as Ménière's disease, vertigo, Otitis Media (including Otitis Media with Effusion (OME), Acute Otitis Media (AOM) and Aerotitis Media (AM)) as well as other disorders which are characterized by ET dysfunction.07-07-2011
20120015987NOVEL POLYMORPH OF ATAZANAVIR SULFATE - The present invention provides a novel crystalline form of atazanavir sulfate, process for its preparation and to pharmaceutical composition containing it. In accordance with the present invention atazanavir sulfate was dissolved in methanol, to the solution was added ethyl acetate, the solid obtained was collected by filtration and dried to give atazanavir sulfate crystalline form H1.01-19-2012
20120208855AMINO-BENZOIC ACID DERIVATIVES FOR USE IN THE TREATMENT OF DIHYDROGENASE-RELATED DISORDERS - Provided herein is method of modulating, and in particular decreasing dihydroorotate dehydrogenase (DHODH) activity, as well as a method of treating a DHODH related disease or disorder.08-16-2012
20120309799BIGUANIDE DERIVATIVE, PREPARATION METHOD THEREOF, AND PHARMACEUTICAL COMPOSITION CONTAINING SAME AS AN ACTIVE INGREDIENT - A biguanide derivative compound with N4-N5 substitution, which is represented by Formula 1, or a pharmaceutically acceptable salt thereof, a method of preparing the same, and a pharmaceutical composition containing the same as an active ingredient are provided. The biguanide derivative may exhibit excellent effect on activation of AMPK and inhibition of cancer cell proliferation in a low dose, compared with conventional drugs, and thus, may be useful to treat diabetes mellitus, obesity, hyperlipidemia, hypercholesterolemia, fatty liver, coronary artery disease, osteoporosis, polycystic ovarian syndrome, metabolic syndrome, cancer, etc.12-06-2012
20120309798Tumour Treatment Agents and Method - N1-(3-Methoxypropyl)-2-(pyridylmethylidene)-hydrazine-1-carbothioamide (I) and its Cu12-06-2012
20120252852OTAMIXABAN FORMULATIONS WITH IMPROVED STABILITY - The invention relates to a pharmaceutical composition comprising methyl (2R,3R)-2-{3-[amino(imino)methyl]benzyl}-3-{[4-(1-oxidopyridin-4-yl)benzoyl]amino}butanoate or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable acidic reacting compound or to an aqueous solution or dispersion of the composition as well as a process for the preparation of the same, methods of using such compositions to treat subjects suffering from conditions which can be ameliorated by the administration of an inhibitor of Factor Xa.10-04-2012
20110105572CARBAMIC ACID COMPOUNDS COMPRISING AN AMIDE LINKAGE AS HDAC INHIBITORS - This invention pertains to certain active carbamic acid compounds which inhibit HDAC activity and which have the following formula:05-05-2011
20100093811HIV PROTEASE INHIBITORS - Compounds of Formula I are disclosed: (I), wherein X04-15-2010
20120316205OIL DISPERSION OF SULFOXIMINES FOR THE CONTROL OF INSECTS - The invention relates to oil dispersions of sulfoximine insecticides, such as sulfoxaflor, and methods of using these dispersions to control insects such as whitefly.12-13-2012
20100197742NEW FORMULATIONS AND USE THEREOF - A pharmaceutical formulation comprising one or more active pharmaceutical ingredients (APIs) suitable for intraoral uptake, that comprises cocoa powder, a process for manufacturing the formulation and use of the formulation for medical treatment.08-05-2010
20100048646N'-Cyano-N-Halogenalkylimidamide Derivatives - The present application relates to novel substituted N′-cyano-N-halogenalkylimidamide derivatives, to processes for their preparation and to their use for controlling animal pests, especially arthropods, in particular insects.02-25-2010
20100048647NEMATICIDAL AGENT COMPOSITION AND METHOD OF USING THE SAME - The present invention provides a nematocide containing, as an active ingredient, an N-2-(pyridyl)ethylcarboxamide derivative represented by the formula (I):02-25-2010
20100273836OXIME ETHER DERIVATIVE AND FUNGICIDE FOR AGRICULTURAL AND HORTICULTURAL USE - The present invention provides a novel oxime ether derivative represented by the following formula (I), or salt thereof, that can be industrially produced advantageously, and can function as a fungicide for agricultural and horticultural use that has reliable effects and can be used safely, and a fungicide for agricultural and horticultural use that contains at least one of these compounds as an active ingredient thereof. In addition, the present invention provides a novel ketone derivative that is a production intermediate of the oxime ether derivative.10-28-2010
20120220637Ophthalmologic Compositions And Use Mode Thereof - The invention concerns a pharmaceutical composition characterized in that it contains a combination of a parasympatholytic agent, a sympathomimetic agent and a local anaesthetic. Such a composition may be injected into the anterior chamber of the eye before a cataract operation or instilled on the eye before laser treatment.08-30-2012
20120225914TREATMENT OF SUNBURN USING ANALGESICS AND ANTIHISTAMINES - Combination compositions and kits comprising an analgesic and an antihistamine are provided as well as methods of use in treating sunburn.09-06-2012
20120225913TRYPSIN-LIKE SERINE PROTEASE INHIBITORS, AND THEIR PREPARATION AND USE - The invention relates to inhibitors of trypsin-like serine proteases of the general formula (I) which, as well as plasmin, also inhibit plasma kallikrein, and to their preparation and use as medicaments, preferably for treatment of blood loss, especially in the case of hyperfibrinolytic states, in organ transplants or heart surgery interventions, in particular with a cardiopulmonary bypass, or as a constituent of a fibrin adhesive.09-06-2012
20120225912NOVEL COLCHICINE DERIVATIVES, METHODS AND USES THEREOF - The invention relates to colchicine derivatives, methods and uses thereof for treatment of cancer. In certain embodiments, the colchicine derivative comprises a compound of Formula I:09-06-2012
20120190714ALPHA KETOAMIDE COMPOUNDS AS CYSTEINE PROTEASE INHIBITORS - The present invention is directed to compounds that are inhibitors of cysteine proteases, in particular, cathepsins B, K, L, F, and S and are therefore useful in treating diseases mediated by these proteases. The present invention is directed to pharmaceutical compositions comprising these compounds and processes for preparing them.07-26-2012
20100035940Cyclin Dependent Kinase Inhibitors - The invention relates to cyclin dependent kinase inhibitor compounds and methods of identifying and using them. The invention further relates to pharmaceutical compositions for treating cell proliferative disorders, especially cancer.02-11-2010
20100004297NOVEL HEXAFLUOROISOPROPANOL DERIVATIVES - The invention is concerned with novel hexafluoroisopropanol derivatives of formula (I)01-07-2010
20100204282Reverse indoles as 5-lipoxygenase-activating protein (FLAP) inhibitors - Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of 5-lipoxygenase-activating protein (FLAP). Also described herein are methods of using such FLAP modulators, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other leukotriene-dependent or leukotriene mediated conditions or diseases.08-12-2010
20120329837CATHEPSIN INHIBITORS FOR TREATING MICROGLIA-MEDIATED NEURON LOSS IN THE CENTRAL NERVOUS SYSTEM - The present invention concerns methods of using Cathepsin S inhibitors and compounds of Formula I that are inhibitors of cathepsin S in treating CNS disorders, diseases, and injuries, particularly neurodegenerative conditions. The present invention is directed to pharmaceutical compositions comprising these compounds for treating CNS disorders.12-27-2012
201202895544-DIMETHYLAMINOBUTYRIC ACID DERIVATIVES - This invention relates to novel 4-dimethylaminobutyric acid derivatives of the formula11-15-2012
20100130564SMALL MOLECULE INHIBITORS OF BCL6 - Provided are methods of inhibiting BCL6 repression in a mammalian cell. Also provided are methods of treating cancer in a mammal.05-27-2010
20120149740PHARMACEUTICAL DEPOT FOR N-{5-[(CYCLOPROPYLAMINO)CARBONYL]-2-METHYLPHENYL)-3-FLUORO-4-(PYRIDIN-2-Y- LMETHOXY)BENZAMIDE - A pharmaceutical depot comprising (i) N-{5-[(cyclopropylamino)carbonyl]-2-methylphenyl}-3-fluoro-4-(pyridin-2-ylmethoxy)benzamide, or a pharmaceutically-acceptable salt thereof, as a pharmaceutical agent (PA) and (ii) a polymer which degrades to create an acidic microclimate, wherein the PA is released from the polymer upon polymer degradation.06-14-2012
20120149739PHARMACEUTICAL DEPOT FOR N-{5-[(CYCLOPROPYLAMINO)CARBONYL]-2-METHYLPHENYL)-3-FLUORO-4-(PYRIDIN-2-Y- LMETHOXY)BENZAMIDE - A pharmaceutical depot comprising (i) N-{5-[(cyclopropylamino)carbonyl]-2-methylphenyl}-3-fluoro-4-(pyridin-2-ylmethoxy)benzamide, or a pharmaceutically-acceptable salt thereof, as a pharmaceutical agent (PA) and (ii) a polymer which degrades to create an acidic microclimate, wherein the PA is released from the polymer upon polymer degradation.06-14-2012
20120149738NOVEL INHIBITORS OF PROLIFERATION AND ACTIVATION OF SIGNAL TRANSDUCER AND ACTIVATORS OF TRANSCRIPTION (STATS) - Pyridine compounds effective in modulation STAT3 and/or STAT5 activation are provided that are useful in the prevention and treatment of proliferative disease and conditions including cancer, inflammation and proliferative skin disorders.06-14-2012
20120149737Therapeutic Aryl-Amido-Aryl Compounds and Their Use - The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain aryl-amido-aryl compounds of the following formula (for convenience, collectively referred to herein as “AAA compounds”), which, inter alia, are (selective) retinoic acid receptor α (RARα) agonists. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to (selectively) activate RARα, and in the treatment of diseases and conditions that are mediated by RARα, that are ameliorated by the activation of RARα, etc., including cognitive disorders, memory impairment, memory deficit, senile dementia, Alzheimer's disease, early stage Alzheimer's disease, intermediate stage Alzheimer's disease, late stage Alzheimer's disease, cognitive impairment, and mild cognitive impairment.06-14-2012
20120149736ENZYME INHIBITORS - Compounds of formula (I), inhibit HDAC activity: wherein A, B and D independently represent ═CH— or ═N—; W is —CH═CH— Or —CH06-14-2012
20130018078ADHESIVE MIXTURE FOR TRANSDERMAL DELIVERY OF HIGHLY PLASTICIZING DRUGS - Transdermal drug delivery patches and methods of their production are described. The patches can be made such that the accommodate highly plasticizing drugs such as selegiline and/or the use of protonated forms of various drugs.01-17-2013
20130018077ALKYNYL PHENYL DERIVATIVE COMPOUNDS FOR TREATING OPHTHALMIC DISEASES AND DISORDERS - Provided are alkynyl phenyl derivative compounds, pharmaceutical compositions thereof, and methods of treating ophthalmic diseases and disorders, such as age-related macular degeneration and Stargardt's Disease, using said compounds and compositions.01-17-2013
20110160252PHARMACEUTICAL COMPOSITIONS FOR TREATMENT OR PREVENTION OF HBV INFECTION - First, the present inventors assessed the effect of the compound represented by formula (III) below on Huh-7 cells infected with HBV, and demonstrated that the compound alone had an anti-HBV effect in vitro.06-30-2011
20110160251ANIMAL ECTOPARASITE CONTROL COMPOSITION - The present invention provides an animal ectoparasite control composition containing an insecticidal component and an adipate, and a method of controlling an animal ectoparasite which comprises administering an effective amount of the animal ectoparasite control composition to an animal.06-30-2011
20130172393PHENOXYALKYL PYRIDINIUM OXIME THERAPEUTICS FOR TREATMENT OF ORGANOPHOSPHATE POISONING - Phenoxyalkyl pyridinium oxime compounds for use in treating organophosphate poisoning.07-04-2013
20080249143NEW FORMULATIONS AND USE THEREOF - A pharmaceutical formulation comprising one or more active pharmaceutical ingredients (APIs) suitable for intraoral uptake, that comprises cocoa powder, a process for manufacturing the formulation and use of the formulation for medical treatment.10-09-2008
200802211774- PIRIDINYLMETHYLSULPHONAMIDE DERIVATIVE AS FUNGICIDAL PLANT PROTECTION AGENTS - Sulfonamides of the formula I09-11-2008
20080221175N-cyclohexyl benzamides and benzeneacetamides as inhibitors of 11-beta-hydroxysteroid dehydrogenases - The present invention provides N-cyclohexyl benzamide and benzeneacetamide compounds according to formula (I):09-11-2008
20080214627DIACYLHYDRAZINE LIGANDS FOR MODULATING THE EXPRESSION OF EXOGENOUS GENES IN MAMMALIAN SYSTEMS VIA AN ECDYSONE RECEPTOR COMPLEX - The present invention relates to non-steroidal ligands for use in nuclear receptor-based inducible gene expression system, and a method to modulate exogenous gene expression in which an ecdysone receptor complex comprising: a DNA binding domain; a ligand binding domain; a transactivation domain; and a ligand is contacted with a DNA construct comprising: the exogenous gene and a response element; wherein the exogenous gene is under the control of the response element and binding of the DNA binding domain to the response element in the presence of the ligand results in activation or suppression of the gene.09-04-2008
20130102642SYNERGISTIC PESTICIDAL MIXTURES - Synergistic pesticidal mixtures are provided.04-25-2013
20080200524Amide compounds as ion channel ligands and uses thereof - Compounds are disclosed that have a formula represented by the following:08-21-2008
20090023787TECHNETIUM-DIPYRIDINE COMPLEXES, AND METHODS OF USE THEREOF - One aspect of the invention relates to novel complexes of technetium (Tc) with various heteroaromatic ligands, e.g., pyridyl and imidazolyl ligands, and their use in radiopharmaceuticals for a variety of clinical diagnostic and therapeutic applications. Another aspect of the invention relates to novel pyridyl ligands that form a portion of the aforementioned complexes. Methods for the preparation of the technetium complexes are also described. Another aspect of the invention relates to novel pyridyl ligands based on derivatized lysine, alanine and bis-amino acids for conjugation to small peptides by solid phase synthetic methods. Additionally, the invention relates to methods for imaging regions of a mammal using the complexes of the invention.01-22-2009
20120283299Biguanide Derivative, A Preparation Method Thereof And A Pharmaceutical Composition Containing The Biguanide Derivative As An Active Ingredient - A biguanide derivative compound with N1-N5 substitution, which is represented by Formula 1, or a pharmaceutically acceptable salt thereof, a method of preparing the same, and a pharmaceutical composition containing the same as an active ingredient are provided. The biguanide derivative may exhibit excellent effect on activation of AMPKα and inhibition of cancer cell proliferation in a low dose, compared to conventional drugs, and thus, may be useful to treat diabetes mellitus, obesity, hyperlipidemia, hypercholesterolemia, fatty liver, coronary artery disease, osteoporosis, polycystic ovarian syndrome, metabolic syndrome, cancer, etc.11-08-2012
20130197041GABR-A2 DIAGNOSTIC - The present invention provides a method of selection of a patient, who is a candidate for treatment with an NMDA antagonist drug, such as (S)-1-phenyl-2-(pyridin-2-yl)ethanamine or ketamine, whereby to predict an increased or decreased likelihood of response to the NMDA antagonist. The invention provides a method for determining the sequence of GABR-A2 at any of four single nucleotide polymorphism (SNP) sites known as rs3756007, rs11503016, rs17537359 or rs1372472. The method also provides ARMS primers optimised for determining the sequence at these GABR-A2 SNPs and diagnostic kits comprising suitable primers or probes for determining the particular SNPs.08-01-2013
20130197042HDAC INHIBITORS - Compounds of formula (I) inhibit HDAC activity:08-01-2013
20130096164USE OF A 1-N-(HALO-3-PYRIDYLMETHYL)-N-METHYLAMINO-1-ALKYLAMINO-2-NITROETHY- LENE DERIVATIVE FOR PREPARING A TOPICAL VETERINARY PHARMACEUTICAL COMPOSITION FOR COMBATING EXTERNAL PARASITES - The present invention relates to the use, as active ingredient, of a 1-N-(halo-3-pyridylmethyl)-N-methylamino-1-alkylamino-2-nitroethylene derivative for preparing a veterinary pharmaceutical composition for topical application in the treatment of external parasites, in particular fleas, in domestic animals, in particular in dogs and cats, intended to be applied at least every 2 weeks.04-18-2013

Patent applications in class Nitrogen attached indirectly to the six-membered hetero ring by nonionic bonding