Inventors list

Assignees list

Classification tree browser

Top 100 Inventors

Top 100 Assignees


Chalcogen attached directly to the six-membered hetero ring by nonionic bonding

Subclass of:

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

514279000 - Polycyclo ring system having the six-membered hetero ring as one of the cyclos

514299000 - Bicyclo ring system having the six-membered hetero ring as one of the cyclos

514311000 - Quinolines (including hydrogenated)

Patent class list (only not empty are listed)

Deeper subclasses:

Entries
DocumentTitleDate
20130045989STABILIZED CRYSTAL OF 2-ETHYL-3,7-DIMETHYL-6-(4-(TRIFLUOROMETHOXY)PHENOXY)QUINOLINE-4-YL METHYL CARBONATE, PROCESS FOR PRODUCING THE CRYSTAL, AND AGRICULTURAL CHEMICAL COMPOSITION COMPRISING THE CRYSTAL - An objective of the present invention is to provide a crystal of 2-ethyl-3,7-dimethyl-6-(4-(trifluoromethoxy)phenoxy)quinoline-4-yl methyl carbonate having stable physicochemical properties.02-21-2013
20130072522Process for Making Modulators of Cystic Fibrosis Transmembrane Conductance Regulator - The invention provides a process for the preparation of a compound of Formula 1,03-21-2013
20130030016QUINOLINE DERIVATIVES AS ANTIBACTERIAL AGENTS - Method of treating a bacterial infection other than a Mycobacterial infection, using a compound of formula (Ia) or (Ib)01-31-2013
20090042933Derivatives of 4-(2-amino -1-hydroxyethyl)phenol as agonists of the Beta2 adrenergic receptor - A compound of formula (I) or a pharmaceutically-acceptable salt, solvate or stereoisomer thereof wherein R02-12-2009
20130030017QUINOLINE DERIVATIVES AS ANTIBACTERIAL AGENTS - Method of treating a bacterial infection other than a Mycobacterial infection, using a compound of formula (Ia) or (Ib)01-31-2013
20100016352COMPOUNDS AND METHODS FOR TREATING ESTROGEN RECEPTOR-RELATED DISEASES - Provided herein in certain embodiments are compounds, pharmaceutical compositions and methods for modulating the functions of estrogen receptor alpha 36, for preventing and/or treating diseases mediated by estrogen receptor alpha 36, for preventing and/or treating osteoporosis, for inducing cell death and/or inhibiting cell proliferation and for preventing and/or treating diseases involving abnormal cell proliferation such as cancers.01-21-2010
20120184579Quinolines and Their Therapeutic Use - Compounds of formula (I) are CRTH2 ligands, useful in the treatment of, for example, asthma and COPD wherein: R07-19-2012
20090176826COMBINATION DRUG CONTAINING PROBUCOL AND A TETRAZOLYLALKOXY-DIHYDROCARBOSTYRIL DERIVATIVE WITH SUPEROXIDE SUPRESSANT EFFECTS - This invention relates to a combination drug comprising a combination of a tetrazolylalkoxy-dihydrocarbostyril derivative of the formula:07-09-2009
20090143426Synthesis of 1,3,6-trisubstituted-2-carboxyquinol-4-ones as selective ET A antagonists and their use as medicaments - The invention discloses the composition and preparation of various 1,3,6-trisubstituted-2-carboxy-quinol-4-ones of the formula 1 where R is H, alkyl, haloalkyl or hydroxyalkyl, R′ is alkyl, nitro, halogen or NR06-04-2009
20100087481ORAL PHARMACEUTICAL FORMULATIONS FOR ANTIDIABETIC COMPOUNDS - Oral pharmaceutical preparations of salts and polymorphs of a compound useful in the treatment of inflammatory and metabolic conditions and diseases are provided herein. The oral pharmaceutical preparation is useful for the treatment or prevention of conditions and disorders associated with energy homeostasis such as type II diabetes, lipid metabolism, adipocyte differentiation and inflammation.04-08-2010
20130085158SOLID FORMS OF 3-(6-(1-(2,2-DIFLUOROBENZO[D][1,3]DIOXOL-5-YL) CYCLOPROPANECARBOXAMIDO)-3-METHYLPYRIDIN-2-YL)BENZOIC ACID - The present invention relates to a substantially a solid form of 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid (Compound 1, Solvate Form A and Compound 1, HCl Salt Form A), processes for making such forms, pharmaceutical compositions thereof, and methods of treatment therewith.04-04-2013
200902475785-HYDROXYMETHYL-OXAZOLIDIN-2-ONE-DERIVATIVES AND THEIR USES AS ANTIBACTERIALS - The invention relates to novel chimeric antibiotics of formula I10-01-2009
201300409891-CYCLOPROPYL-8-METHYL-7-[5-METHYL-6-(METHYLAMINO)-3-PYRIDINYL]-4-OXO-1,4-- DIHYDRO-3-QUINOLINECARBOXYLIC ACID SALTS - There is provided a salt of 1-cyclopropyl-8-methyl-7-[5-methyl-6-(methylamino)-3-pyridinyl]-4-oxo-1,4-dihydro-3-quinolinecarboxylic acid selected from the group consisting of citrate, hemi-fumarate, maleate, L-tartrate, mesylate, hydrochloride, potassium, and sodium salts.02-14-2013
20130079367SOLID FORMS OF N-[2,4-BIS(1,1-DIMETHYLETHYL)-5-HYDROXYPHENYL]-1,4-DIHYDRO-4-OXOQUINOLINE- -3-CARBOXAMIDE - The present invention relates to solid state forms of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide (Compound 1), pharmaceutical compositions thereof and methods therewith.03-28-2013
20090264464ANTITUMOR AGENT FOR UNDIFFERENTIATED GASTRIC CANCER - The present invention relates to a therapeutic agent represented by the General formula (I), or a pharmacologically acceptable salt thereof, or a solvate of the compound or the salt thereof:10-22-2009
20100105728DIHYDRO-[1H]-QUINOLIN-2-ONE DERIVATIVES AS RXR AGONISTS FOR THE TREATMENT OF DYSLIPIDEMIA, HYPERCHOLESTEROLEMIA AND DIABETES - The present invention relates to compounds of Formula (I),04-29-2010
20090131474SCREENING METHODS FOR PROTEIN KINASE B INHIBITORS EMPLOYING VIRTUAL DOCKING APPROACHES AND COMPOUNDS AND COMPOSITIONS DISCOVERED THEREBY - The present invention describes an improved method for screening compounds for activity in inhibiting the enzymatic activity of Akt1 protein kinase, also known as Protein Kinase B, an enzyme that is believed to play a key role in the inhibition of apoptosis and thus in the etiology of cancer and other conditions, including neurodegenerative diseases. In general, the method comprises: (1) providing a plurality of compounds suspected of having Akt1 kinase inhibitory activity; (2) modeling the docking of each of the plurality of the compounds with a target binding site derived from the crystal structure of a ternary complex involving Akt1, a nonhydrolyzable ATP analogue, and a peptide substrate derived from a physiological AKT substrate such that the protein active site is defined including those residues within a defined distance from the nonhydrolyzable ATP analogue; (3) ranking the docked compounds by goodness of fit; (4) further selecting compounds from compounds high ranked by goodness of fit in docking by using one or more screening criteria; (5) optionally, visually analyzing structures of compounds selected in step (4) to remove any compounds with improbable docking geometry; and (6) experimentally testing the selected compounds from step (4) or step (5), if step (5) is performed, to determine their inhibitory activity against Akt1 in order to select compounds with Akt1 inhibitory activity. The invention also encompasses pharmaceutical compositions including compounds whose inhibitory activity against Akt1 is discovered by the screening method, as well as methods of use of the pharmaceutical compositions to treat cancer and other conditions.05-21-2009
20100069434Compositions of n-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline- -3-carboxamide - Pharmaceutical compositions including N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide (Compound 1) and methods of using such compositions are described herein.03-18-2010
20090042935NOVEL IV FORMULATION OF TIPIFARNIB - This invention concerns compositions of tipifarnib, mannitol, and hydroxypropyl-β-cyclodextrin and, suitable for intravenous (IV) administration. The invention further concerns the use of such formulation and processes for preparing such formulations and methods of treating by administering said formulations.02-12-2009
20090042932ANTIMICROBIAL PARENTERAL FORMULATION - This invention relates to a parenteral formulation containing an effective amount of the compound of the following formula I:02-12-2009
20100137361Tetrahydro-Quinolinylurea Derivatives - This invention relates to tetrahydro-quinolinylurea derivatives and salts thereof which are useful as active ingredients of pharmaceutical preparations.06-03-2010
20100267768PROCESS FOR MAKING MODULATORS OF CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR - The invention provides a process for the preparation of a compound of Formula 1,10-21-2010
20130090354Pharmaceutical Compositions and Administrations Thereof - The present invention relates to the use of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide, solids forms, and pharmaceutical compositions thereof for the treatment of CFTR mediated diseases, particularly cystic fibrosis, in patients possessing specific genetic mutations.04-11-2013
20110015224COMBINATION OF A CARBOSTYRIL AND CARNITINE - The present invention relates to a medicament for treating occlusive and/or ischemic vascular disorder comprising a carbostyril derivative and carnitine.01-20-2011
20130065920PHARMACEUTICAL COMPOSITION FOR THE PREVENTION OR TREATMENT OF OSTEOARTHRITIS CONTAINING REBAMIPIDE AS AN ACTIVE INGREDIENT - The present invention provides a pharmaceutical composition for preventing or treating osteoarthritis comprising rebamipide as an active ingredient and a pharmaceutically acceptable carrier. The pharmaceutical composition may be for oral administration, for example an oral solid dosage form of a tablet or capsule form. The pharmaceutical composition may be formulated into a unit dosage form suitable for orally administering rebamipide in a dose ranging from 0.5 to 50 mg/kg, preferably from 0.6 to 6 mg/kg.03-14-2013
20130065921PTEN INHIBITOR OR MAXI-K CHANNELS OPENER - A new PTEN opener or a new opener of a large conductance Ca03-14-2013
20130065922NOVEL AMIDES AS FUNGICIDES - Compounds of the general formula (I), wherein the substituents are as defined in claim 03-14-2013
20110021561QUINOLINE COMPOUND AND PHARMACEUTICAL COMPOSITION, PREPARATION METHOD AND USES THEREOF - The present invention discloses a quinoline compound represented by the formula A or pharmaceutically acceptable solvate, optical isomer or polymorph thereof,01-27-2011
20090247576ANTI-TUMOR AGENT FOR MULTIPLE MYELOMA - The object of the invention is to provide a pharmaceutical composition and a therapeutic method which can exert their effects with higher efficiency on a living organism having at least one cell selected from the group consisting of a cell overexpressing FGFR3, a cell that has a t(4;14) translocation and a cell expressing mutant FGFR3. The compound represented by General Formula (I), a pharmacologically acceptable salt thereof or a solvate thereof can exert their effects with higher efficiency on a living organism having at least one cell selected from the group consisting of a cell overexpressing FGFR3, a cell that has a t(4;14) translocation and a cell expressing mutant FGFR3.10-01-2009
20120115904COMPOUNDS HAVING ANTIPARASITIC OR ANTI-INFECTIOUS ACTIVITY - Compounds of formula I:05-10-2012
20090012119FLUOROALKYLPYRROLIDINE DERIVATIVE - This invention relates to a compound represented by the following formula (1):01-08-2009
20090012118Kynurenic Acid Amide Derivatives as Nr2b Receptor Antagoni - The new kynurenic acid amide derivatives of formula (I): and optical antipodes, racemates and the salts thereof are highly effective and selective antagonists of NMDA receptor, and moreover most of the compounds are selective antagonist of NR2B subtype of NMDA receptor.01-08-2009
20110319446BICYCLO[2.2.1]HEPT-7-YLAMINE DERIVATIVES AND THEIR USES - Compounds of formula (I) have muscarinic M3 receptor modulating activity;12-29-2011
20130018071Solid Forms of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline- -3-carboxamide - The present invention relates to solid state forms of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide (Compound 1), pharmaceutical compositions thereof and methods therewith.01-17-2013
20100010039POLYMORPHIC CRYSTAL FORM OF A INDAN-2-YLAMINO-HYDROXYETHYL-QUINOLINONE MALEATE DERIVATIVE AS BETA-ADRENOCEPTOR AGONIST - New polymorphic crystal form of (R)-5-[2-(5,6-diethyl-indan-2-ylamino)-1-hydroxyethyl]-8-hydroxy-1H-quinolin-2-one maleate designated crystal form Qalpha that is useful in the treatment of inflammatory or obstructive airways diseases. A method for preparing crystal form Qalpha is also described.01-14-2010
20090105299c-MET MODULATORS AND METHODS OF USE - The present invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. More specifically, the invention provides quinazolines and quinolines which inhibit, regulate, and/or modulate kinase receptor, particularly c-Met, KDF, c-Kit, flt-3 and flt-4, signal transduction pathways related to the changes in cellular activities as mentioned above, compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions. The present invention also provides methods for making compounds as mentioned above, and compositions which contain these compounds.04-23-2009
201200102395-CHLORO-4-HYDROXY-1-METHYL-2-OXO-N-PHENYL-1,2-DIHYDROQUINOLINE-3-CARBOXAM- IDE, SALTS AND USES THEREOF - The subject invention provides 5-chloro-4-hydroxy-1-methyl-2-oxo-N-phenyl-1,2-dihydroquinoline-3-carboxamide, its salts and uses.01-12-2012
20090099230Solid forms of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline- -3-carboxamide - Solid forms of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide are described herein, including crystalline forms thereof.04-16-2009
20100113515PTEN INHIBITOR OR MAXI-K CHANNELS OPENER - A new PTEN opener or a new opener of a large conductance Ca05-06-2010
20100113514FUSED HETEROCYCLIC COMPOUNDS AS ION CHANNEL MODULATORS - The present invention relates to sodium channel inhibitors of Formula :05-06-2010
20120142729KAT ll INHIBITORS - The present invention relates to compounds 3-amino-1-hydroxy-2-oxo-1,2,3,4-tetrahydroquinoline-7-carbonitrile, 3-amino-1-hydroxy-7-(2-methoxyethoxy)-3,4-dihydroquinolin-2(1H)-one, and 3-amino-1-hydroxy-7-[(1S)-2-methoxy-1-methylethoxy]-3,4-dihydroquinolin-2(1H)-one, including racemic mixtures and resolved enantiomers thereof, to pharmaceutically acceptable salts thereof, and to the treatment of cognitive deficits associated with schizophrenia and other psychiatric, neurodegenerative and/or neurological disorders in mammals, including humans.06-07-2012
20100234421SUBSTITUTED 3-AMINO-2-MERCAPTOQUINOLINES AS KCNQ2/3 MODULATORS - The invention relates to substituted 3-amino-2-mercaptoquinolines, to processes for their preparation, to medicaments containing these compounds and to the use of these compounds in the preparation of medicaments.09-16-2010
20100120850Quinoline Derivatives, Pharmaceutical Compositions Comprising Them, and Their Use in Treating Central Nervous System and Peripheral Diseases - Compounds of Formula (I) wherein R05-13-2010
20100120852AROYL-PIPERIDINE DERIVATIVES AND METHOD OF TREATING DISORDERS INDUCED BY SUBSTANCE P - The invention relates to a method of administering N-(3,5-bis-trifluoromethyl-benzoyl)-2-benzyl-4-(quinoloylamino)-piperidines of the formula05-13-2010
20090298875A Combination of Compounds, Which Can be Used in the Treatment of Respiratory Diseases, Especially Chronic Obstructive Pulmonary Disease (COPD) and Asthma - The present invention provides pharmaceutical compositions comprising a β12-03-2009
20100249183THERAPEUTIC USE OF N-(ARYLALKYL)-1H-PYRROLOPYRIDINE-2-CARBOXAMIDE DERIVATIVES - The invention concerns therapeutic use of compounds of general formula (I), wherein n, the pyrrolopyridine ring, X09-30-2010
20100249182AMINOQUINOLINE DERIVATIVES, PREPARATION METHOD THEREOF AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME - Provided are a novel aminoquinoline compound represented by Formula 1 or a pharmaceutically acceptable salt thereof, preparation method thereof, and a pharmaceutical composition for preventing or treating cutaneous cancer, comprising the aminoquinoline compound or pharmaceutically acceptable salt thereof. Since the compound of Formula 1 exhibits excellent anti-proliferative effect on melanoma tumor cells, it is useful for preventing or treating cutaneous cancer.09-30-2010
20120108632PRENYLTRANSFERASE INHIBITORS FOR OCULAR HYPERTENSION CONTROL AND THE TREATMENT OF GLAUCOMA - The invention concerns in one embodiment a method of treating glaucoma or elevated intraocular pressure comprising administering a pharmaceutically effective amount of a composition comprising at least one prenyltransferase inhibitor. In another embodiment, the invention concerns a composition for the treatment of elevated intraocular pressure and glaucoma comprising a pharmaceutically effective amount of a prenyltransferase inhibitor.05-03-2012
20120108631Sulfonamides for the Modulation of PKM2 - The invention relates to sulfonamide compounds and methods for activating PKM2. The compounds and methods are useful in treating or preventing a disease or disorder selected from cancer, cell proliferative disorder, inflammatory disorder, metabolic disorder, and immune system disorder.05-03-2012
20090247577PYRROLIDINE DERIVATIVES USEFUL AS BACE INHIBITORS - Novel 3-mono-, 3,4-di- and 3,4,4,-tri-substituted pyrrolidine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (disorder) that depends on the activity of beta-secretase and/or the generation of beta-amyloid and the subsequent aggregation into oligomers and fibrils; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on the activity of beta-secretase and/or the generation of beta-amyloid and the subsequent aggregation into oligomers and fibrils; pharmaceutical formulations comprising a said substituted pyrrolidine compound, and/or a method of treatment comprising administering a said substituted pyrrolidine compound. The substituted pyrrolidine compounds are especially of the formula I,10-01-2009
20110172268MECHANISM-BASED SMALL-MOLECULE PARASITE INHIBITORS - Methods for preventing or treating an Apicomplexan parasite infection in a patient administering to a patient in need thereof an effective amount of a compound of Formulas I-IV.07-14-2011
20080207687Quinoline Derivatives as Antibacterial Agents - Use of a compound for the manufacture of a medicament for the treatment of a bacterial infection provided that the bacterial infection is other than a Mycobacterial infection, said compound being a compound of formula (I)08-28-2008
20110172269ANTIOXIDANT COMBINATIONS FOR USE IN FEED RATIONS TO INCREASE MILK PRODUCTION AND MILK FAT - The present invention provides a combination of antioxidants that effectively stabilize different types of fats utilized in a ruminant diet. When included in a ruminant feed ration or water source, the antioxidant combination typically increases nutrient digestion, such as fiber and protein, improves rumen fermentation, improves microbial growth, improves microbial efficiency, increases milk production and/or milk fat, improves antioxidant status of the ruminant, and attenuates the negative effects of some fats in the ruminant animal.07-14-2011
20090281141MACROCYCLIC INHIBITORS OF HEPATITIS C VIRUS - Inhibitors of HCV replication of formula (I)11-12-2009
20090281140Macrocyclic inhibitors of hepatitis c virus - Inhibitors of HCV replication of formula (I)11-12-2009
20090042934Sulfonyl-Quinoline Derivatives - The present invention relates to new mGluR1 and mGluR5 receptor subtype preferring ligands of formula (I) and/or salts and/or hydrates and/or solvates and/or polymorphs thereof. The invention also relates to processes and intermediates for their preparation, to pharmaceutical compositions containing these compounds and to their use in treatment and/or prevention of conditions which require modulation of mGluR1 and mGluR5 receptors.02-12-2009
20090298876MODULATORS OF ATP-BINDING CASSETTE TRANSPORTERS - The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.12-03-2009
20100280070NOVEL TETRAHYDROQUINOLINES AS AROMATASE INHIBITORS - The invention relates to synthesis and biological screening of novel tetrahydroquinolines of formula (I), their derivatives, their stereoisomers, their pharmaceutically acceptable salts and pharmaceutically acceptable compositions containing them for aromatase inhibition: (I). The present invention also relates to a process for the preparation of the novel tetrahydroquinolines, their derivatives, their stereoisomers, their pharmaceutically acceptable salts and pharmaceutically acceptable compositions containing them. These compounds are useful in for aromatase inhibition, particularly in the treatment and/or prevention of cancer, particularly breast cancer, more particularly hormone dependent breast cancer.11-04-2010
20090156636THERAPEUTIC AGENT FOR GLOMERULAR DISEASE - The present invention relates to a preventive and/or therapeutic agent for a glomerular disease containing, as active ingredients pitavastatin or a salt thereof and candesartan cilexetil or a salt thereof. The agent of the present invention exhibits an excellent effect in the prevention and/or therapy of a glomerular disease.06-18-2009
20090170896c-Met modulators and methods of use - The present invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. More specifically, the invention provides quinazolines and quinolines which inhibit, regulate, and/or modulate kinase receptor, particularly c-Met, KDF, c-Kit, flt-3 and flt-4, signal transduction pathways related to the changes in cellular activities as mentioned above, compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions. The present invention also provides methods for making compounds as mentioned above, and compositions which contain these compounds.07-02-2009
20130217724N-ETHYL-N-PHENYL-1,2-DIHYDRO-4,5-DI-HYDROXY-1-METHYL-2-OXO-3-QUINOLINECARB- OXAMIDE, PREPARATION AND USES THEREOF - The subject invention provides a pharmaceutical composition containing laquinimod or a pharmaceutically acceptable salt thereof, and a compound of N-ethyl-N-phenyl-1,2-dihydro-4,5-di-hydroxy-1-methyl-2-oxo-3-quinolinecarboxamide or a salt thereof.08-22-2013
20120196894NOVEL TRPA1 ANTAGONISTS - The present invention relates to compositions and methods that modulate at least one TRP family member. Specifically, the present invention relates to novel TRPA1 antagonists and their use in the treatment of pain such as chronic inflammatory and neuropathic pain. Compounds that can modulate one or more TRPA1 functions are useful in many aspects including, but not limited to, maintaining calcium homeostasis; maintaining sodium homeostasis; modulating intracellular calcium levels; modulating membrane polarization (membrane potential); modulating cation levels; and/or treating or preventing diseases, disorders, or conditions associated with calcium homeostasis, sodium homeostasis, calcium or sodium dyshomeostasis, or membrane polarization/hyperpolarization (including hypo and hyperexcitability), and/or treating or preventing diseases, disorders, or conditions associated with regulation or misregulation of TRPA1 expression or function. The present invention further relates to methods and compositions that antagonize both a function of TRPA1 and a function of one or more additional TRP channels.08-02-2012
20120035212(L)-Malate salt of N-(4-phenyl)-N'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide - Disclosed are malate salts of N-(4-{[6,7-bis(methyloxy)-quinolin-4-yl]oxy}phenyl)-N′-(4-fluorophenyl)cyclopropane-02-09-2012
20090163545Method For Altering The Lifespan Of Eukaryotic Organisms - A method for altering the lifespan of a eukaryotic organism. The method comprises the steps of providing a lifespan altering compound, and administering an effective amount of the compound to a eukaryotic organism, such that the lifespan of the organism is altered. In one embodiment, the compound is identified using the DeaD assay.06-25-2009
20090137627Method for Treating Chronic Pain - A method for the treatment of chronic pain in a mammal is provided. The method comprises administering to a mammal (e.g., a human) suffering from chronic pain a pain relieving amount of a diarylureido-dihalokynurenate compound. Preferred diarylureido-dihalokynurenate compounds are esters (e.g., ethyl esters). Particularly preferred are diphenylureido-dichlorokynurenate compounds.05-28-2009
20090137626Pharmaceutical Composition Containing PPARgamma Agonist - [Object] To provide a highly safe method for treating diabetes that demonstrates superior effects and is capable of inhibiting adverse side effects.05-28-2009
20080319009Methylene-bridged selective androgen receptor modulators and methods of use thereof - This invention provides a class of androgen receptor targeting agents (ARTA). The agents define a new subclass of compounds, which are selective androgen receptor modulators (SARM). Several of the SARM compounds have been found to have an unexpected androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor. Other SARM compounds have been found to have an unexpected antiandrogenic activity of a nonsteroidal ligand for the androgen receptor. The SARM compounds, either alone or as a composition, are useful for a) male contraception; b) treatment of a variety of hormone-related conditions, for example conditions associated with Androgen Decline in Aging Male (ADAM), such as fatigue, depression, decreased libido, sexual dysfunction, erectile dysfunction, hypogonadism, osteoporosis, hair loss, anemia, obesity, sarcopenia, osteopenia, osteoporosis, benign prostate hyperplasia, alterations in mood and cognition and prostate cancer; c) treatment of conditions associated with Androgen Decline in Female (ADIF), such as sexual dysfunction, decreased sexual libido, hypogonadism, sarcopenia, osteopenia, osteoporosis, alterations in cognition and mood, depression, anemia, hair loss, obesity, endometriosis, breast cancer, uterine cancer and ovarian cancer; d) treatment and/or prevention of acute and/or chronic muscular wasting conditions; e) preventing and/or treating dry eye conditions; f) oral androgen replacement therapy; g) decreasing the incidence of, halting or causing a regression of prostate cancer; and/or h) inducing apoptosis in a cancer cell.12-25-2008
20080319008Compounds Having Activity in Increasing Ion Transport by Mutant-Cftr and Uses Thereof - The invention provides compositions, pharmaceutical preparations and methods for increasing activity (e.g., ion transport) of the mutant cystic fibrosis transmembrane conductance regulator protein (mutant-CFTR), e.g., ΔF508 CFTR, G551D-CFTR, G1349D-CFTR, or D1152H-CFTR, that are useful for the treatment of cystic fibrosis (CF). The compositions and pharmaceutical preparations of the invention may comprise one or more phenylglycine-containing compounds or sulfonamide-containing compounds of the invention, or an analog or derivative thereof.12-25-2008
20100004282TREATMENT OF ANTIBIOTIC-RESISTANT BACTERIA INFECTION - This invention relates to a method of treating infection by methicillin-nonsusceptibale bacteria, vancomycin-nonsusceptibale bacteria, penicillin-nonsusceptibale bacteria, clarithromycin-nonsusceptibale bacteria, or metronidazole-nonsusceptibale bacteria by administering to a subject in need thereof an effective amount of a compound of the following formula:01-07-2010
20090239904COMPOUNDS HAVING BETA2 ADRENERGIC RECEPTOR AGONIST AND MUSCARINIC RECEPTOR ANTAGONIST ACTIVITY - This invention provides compounds of formula I:09-24-2009
20130217725Macrocyclic Inhibitors Of Hepatitis C Virus - Inhibitors of HCV replication of formula (I)08-22-2013
20090023773COMPOSITIONS AND METHODS FOR MODULATING GATED ION CHANNELS - Disclosed are compounds that modulate the activity of the gated ion channels. Compounds that modulate these gated ion channels are useful in the treatment of diseases and disorders related to pain, inflammation, the neurological system, the gastrointestinal system and genitourinary system. Preferred compounds include compounds of the Formulae 1, 2, 3, 4, and 5.01-22-2009
20090023774Pyridine analogs as C5A antagonists - The present invention provides novel compounds of Formula I which are antagonists of the C5a receptor. Compounds of the present invention are useful for the treatment of various C5a-mediated diseases and disorders; accordingly the present invention provides a method for the treatment of C5a-mediated diseases using the novel compounds described herein, as well as pharmaceutical compositions containing them.01-22-2009
20090062337Treatment of Microbial Infections - The present invention provides methods for treating various microbial infections using a compound of the formula:03-05-2009
20110230520NITRATE DERIVATIVES OF CILOSTAZOL FOR THE TREATMENT OF VASCULAR AND METABOLIC DISEASES - Nitrate derivatives of cilostazol are described. They have superior properties and clinical advantages compared to cilostazol in the treatment of vascular and metabolic diseases.09-22-2011
20080262034LIPOIC ACID DERIVATIVES - Lipoic acid derivatives and pharmaceutical formulations containing lipoic acid derivatives are useful in the treatment and prevention of disease characterized by disease cells that are sensitive to lipoic acid derivatives.10-23-2008
20090209580ANTITUMOR AGENT FOR THYROID CANCER - The objective of the present invention is to provide a pharmaceutical composition and a therapeutic method that are specifically effective against at least one disease selected from multiple endocrine neoplasia, type IIA, multiple endocrine neoplasia, type IIB, familial medullary thyroid carcinoma, thyroid carcinoma, papillary thyroid carcinoma, sporadic medullary thyroid carcinoma, Hirschsprung disease, pheochromocytoma, parathyroid hyperplasia and mucosal neuromas of the gastrointestinal tract.08-20-2009
20090221635QUINOLINYL AND BENZOTHIAZOLYL MODULATORS - Compounds, compositions and methods are provided that are useful in the treatment or prevention of a condition or disorder mediated by PPARγ. In particular, the compounds of the invention modulate the function of PPARγ. The subject methods are particularly useful in the treatment and/or prevention of diabetes, obesity, hypercholesterolemia, rheumatoid arthritis and atherosclerosis.09-03-2009
20090253739Amine Derivatives - The invention relates to compounds of formula (1)10-08-2009
20090048293METHODS FOR TREATING BACILLUS INFECTION - The present invention provides compositions and methods for detecting, treating, and preventing microbial infection, especially infection caused by 02-19-2009
20090048295SUBSTITUTED 5,6,7,8-TETRAHYDROQUINOLINE DERIVATIVES, COMPOSITIONS, AND METHODS OF USE THEREOF - Substituted 5,6,7,8-tetrahydroquinoline derivatives, which are C502-19-2009
20090048296HIGH CONCENTRATION LOCAL ANESTHETIC FORMULATIONS - A transdermal topical anesthetic formulation, which can be used to ameliorate or inhibit neuropathic pain, has been developed. In the preferred embodiment, the topical anesthetic is a local anesthetic such as lidocaine, most preferably lidocaine free-base in a gel, and the dosage of the local anesthetic is effective in the painful area or immediately adjacent areas, to ameliorate or eliminate the pain. High concentration of local anesthetic in solution in the carrier is used to drive rapid release and uptake of the drug. Relief is typically obtained for a period of several hours.02-19-2009
20090048294HIF-1 ALPHA ACTIVATING AGENT - The present invention relates to a HIF-1α activator containing clioquinol and its derivatives as an active ingredient. Clioquinol and its derivatives of the invention inhibit HIF-1α (hypoxia-inducible factor-1α) ubiquitination in normoxic cells and thus accumulate HIF-1α. In the meantime, CQ inhibits FIH-I activity and thereby induces transcription activity of the accumulated HIF-1α, resulting in the induction of expressions of HIF-1α target genes VEGF (vascular endothelial growth factor) and EPO (erythropoietin). Therefore, clioquinol and its derivatives can be effectively used as a therapeutic agent for ischemic disease.02-19-2009
20100184804METHODS FOR THE PREVENTION OR TREATMENT OF BACTERIAL AND FUNGAL INFECTIONS - The present invention features improved methods for treating, stabilizing, or preventing a bacterial or a fungal infection in a plant or an animal, such as a mammal. In particular, these methods involve the use of a compound, that is controlled by MvfR, and that affects the expression of an MvfR protein or that promotes its modification or inactivation, or a compound produced by 07-22-2010
20110060005TREATMENT OF MITOCHONDRIAL DISORDERS USING A FARNESYL TRANSFERASE INHIBITOR - Methods and pharmaceutical compositions comprising a low dose of a farnesyl transferase inhibitor useful in the treatment of proteinopathies and mitochondrial disorders are provided. These low doses are below the doses used in oncological treatments for which these compounds were initially designed. The treatment includes administering to a subject an amount of a farnesyl transferase inhibitor, wherein the amount administered is sufficient to stimulate mitophagy in said subject. Treatments in accordance with the present invention may also include an acetylcholinesterase inhibitor, an activator of neurotrophic receptors, an NMDA anatagonist, an amyloid deposit inhibitor, an antipsychotic agent, an antidepressant, an anxiolytic, or an antioxidant.03-10-2011
20130123301CRYSTALLINE SALTS OF QUINOLINE COMPOUNDS AND METHODS FOR PREPARING THEM - A stable solid pharmaceutical composition consisting essentially of an effective amount of a crystalline salt of formula (II)05-16-2013
20090076075QUINOLINE DERIVATIVES - The invention concerns quinoline derivatives of Formula I03-19-2009
20090076073THERAPEUTIC AMIDES - The invention provides compounds of the formula:03-19-2009
20090076072DEUTERIUM-ENRICHED TAFENOQUINE - The present application describes deuterium-enriched tafenoquine, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.03-19-2009
20100144787Quinolines and Their Therapeutic Use - Compounds of formula (I) are CRTH2 ligands, useful in the treatment of, for example, asthma and COPD wherein: R06-10-2010
20100144786QUINOLINE DERIVATIVES AS CRTH2 RECEPTOR LIGANDS - Specific quinoline derivatives are CRTH2 antagonists, useful in the treatment of conditions having an inflammatory component.06-10-2010
20100222381Cyclopentathiophene/cyclohexathiophene DNA methyltransferase inhibitors - Compounds represented by Formula (I):09-02-2010
20080275082Pharmaceutical Composition - A novel pharmaceutical composition comprising the NK11-06-2008
20090111851Antimicrobial Quinolones, Their Compositions and Uses - Compounds having the general structure:04-30-2009
20090111850Amino-Substituted Ethylamino Beta2 Adrenergic Receptor Agonists - The invention provides novel β04-30-2009
20120142730USE OF LAQUINIMOD FOR REDUCING FATIGUE, IMPROVING FUNCTIONAL STATUS, AND IMPROVING QUALITY OF LIFE IN MULTIPLE SCLEROSIS PATIENTS - The subject invention provides methods for reducing or inhibiting progression of the level of fatigue in a multiple sclerosis human patient, for improving or inhibiting deterioration of the functional status of a multiple sclerosis human patient, and for improving or inhibiting deterioration of the general health of a multiple sclerosis human patient, comprising orally administering to the human patient laquinimod or a pharmaceutically acceptable salt thereof. The subject invention also provides a method for providing neuroprotection to a human subject, the method comprising orally administering to the human subject laquinimod or a pharmaceutically acceptable salt thereof.06-07-2012
20130137722SOLID FORMS OF N-(4-(7-AZABICYCLO[2.2.1]HEPTAN-7-YL)-2-TRIFLUOROMETHYL)PHENYL)-4-OXO-5-(- TRIFLUOROMETHYL)-1,4-DIHYDROQUINOLINE-3-CARBOXAMIDE - The present invention relates to substantially crystalline and solid state forms of N-(4-(7-azabicyclo[2.2.1]heptan-7-yl)-2-(trifluoromethyl)phenyl)-4-oxo-5-(trifluoromethyl)-1,4-dihydroquinoline-3-carboxamide (Form A-HCl, Form B, Form B-HCl, or any combination of these forms), pharmaceutical compositions thereof, and methods of treatment therewith.05-30-2013
20130137723CRYSTAL OF ANTI-BACTERIAL COMPOUND - It is intended to provide a salt of a compound and crystals thereof useful as a therapeutic and/or preventive agent for infectious diseases which has wide and excellent antibacterial activity and has excellent safety.05-30-2013
20090069372ANTITUMOR AGENTS - The invention provides compounds of formula I:03-12-2009
20110212993MEDICAMENT FOR TREATING GLAUCOMA COMPRISING AS AN ACTIVE INGREDIENT CYCLODEXTRIN-CLATHRATE COMPOUND OF CILOSTAZOL - The invention relates to an ophthalmic medicament for treating glaucoma which comprises a clathrate compound prepared by dissolving cilostazol or a salt thereof in a cyclodextrin.09-01-2011
20110034509Beta-2-Adrenoreceptor Agonists - Compounds of formula02-10-2011
20110039887CARBOSTYRIL DERIVATIVES INCLUDING CILOSTAZOL FOR TREATING FATTY LIVER - The invention relates to a medicament for preventing and/or treating fatty liver which comprises as an active ingredient cilostazol or a pharmaceutically acceptable salt thereof.02-17-2011
20110118308CRYSTALS OF LAQUINIMOD SODIUM, AND PROCESS FOR THE MANUFACTURE THEREOF - Disclosed is a process for the preparation of laquinimod sodium which removes the impurities after the salt formation step, thus resulting in crystals of higher purity as well as crystals having improved crystalline characteristics.05-19-2011
20110118309USE OF HDAC INHIBITORS FOR THE TREATMENT OF HODGKIN'S DISEASE - The present invention relates to the use of an HDAC inhibitor, especially an HDAC inhibitor of formula (I):05-19-2011
20100197728CRYSTALLINE FORM OF A QUINOLINONE-CARBOXAMIDE COMPOUND - The invention provides a crystalline hydrochloride salt of 1-isopropyl-2-oxo-1,2-dihydroquinoline-3-carboxylic acid {(1S,3R,5R)-8-[(R)-2-hydroxy-3-(methanesulfonyl-methyl-amino)propyl]-8-azabicyclo[3.2.1]oct-3-yl}amide or a solvate thereof. The invention also provides pharmaceutical compositions comprising such crystalline salt forms, methods of using such crystalline salt forms to treat diseases associated with 5-HT08-05-2010
20100184803Treatment of Lysosomal Storage Diseases - Methods and compositions useful in the treatment or prevention of lysosomal storage diseases, such as Pompe's disease, Fabry's disease, Gaucher's disease, and Niemann-Pick disease, are provided. The treatment includes administering to a subject a farnesyl transferase inhibitor compound. The treatment may also include enzyme replacement therapy or gene therapy.07-22-2010
20090326008NF-kappa B Inhibitor - The present invention provides an NF-κB inhibitor. The NF-κB inhibitor of the present invention contains a carbostyril compound represented by General Formula (1)12-31-2009
20100048621MEDICAMENT FOR TREATING CHRONIC OBSTRUCTIVE PULMONARY DISEASE - The invention relates to a medicament for treating chronic obstructive pulmonary disease comprising as active ingredients a carbostyril derivative of formula (1): wherein A is a lower alkylene group, R is a cycloalkyl group, the bonding between 3- and 4-positions of the carbostyril skeleton is a single bond or a double bond, or a salt thereof; and probucol.02-25-2010
20100069435METHOD OF SELECTIVELY INTRODUCING AMINO SUBSTITUENT - Provided are a technique for position-selectively introducing an amino group into a difluorobenzoic acid, a novel process for producing a quinolonecarboxylic acid derivative serving as an antibacterial agent, and intermediates in the production. The process comprises treating a compound represented by formula (6):03-18-2010
20110098318FARNESYL PROTEIN TRANSFERASE INHIBITORS FOR TREATING BREAST CANCER - The present invention relates to the use of farnesyl protein transferase inhibitors for preparing pharmaceutical compositions for treating advanced breast cancer.04-28-2011
20100130548BIPHENYL DERIVATIVES AS MODULATORS OF VOLTAGE GATED ION CHANNELS - Biphenyl derivatives useful as ion channel antagonists are disclosed herein. The compositions thereof are useful for treating or relieving pain-related conditions.05-27-2010
20110077269DERIVATIVES FOR MODULATION OF ION CHANNELS - Sulfonamide derivatives act as ion channel antagonists. The compositions are useful for treating or relieving pain-related conditions.03-31-2011
20120202848THERAPY OF AUTOIMMUNE COLITIS USING A TIP60 INHIBITOR - This invention is in the fields of immunology and autoimmunity. More particularly it concerns methods of treating patients with compounds which are useful agents for inhibiting the functions of TIP60 in the treatment of an individual suffering, for example, from ulcerative colitis and other irritable bowel diseases.08-09-2012
20100120849Compositions for Treating Hyperproliferative Vascular Disorders and Cancers - The present invention relates to a pharmaceutical composition for preventing or treating hyperproliferative vascular disorders, and a pharmaceutical anticancer composition comprising the compound represented by the Formula 1. The present compounds exhibit IC05-13-2010
20080249129Compositions and Methods for Treatment of Protein Misfolding Diseases - Disclosed are compounds and conditions that either suppress or enhance toxicity in yeast cells expressing alpha synuclein or huntingtin. These compounds and conditions can be used in the development of compositions that suppress toxicity, fibril formation, and/or diseases mediated at least in part by alpha synuclein or huntingtin.10-09-2008
20130165479ANTAGONISTS OF THE TRPV1 RECEPTOR AND USES THEREOF - The present application is directed to compounds that are TRPV1 antagonictc and have formula (I)06-27-2013
20110251235STABLE LAQUINIMOD PREPARATIONS - The invention relates to a pharmaceutical composition comprising a pharmaceutically acceptable salt of N-ethyl-N-phenyl-1,2,-dihydro-4-hydroxy-5-chloro-1-methyl-2-oxoquinoline-3-carboxamide, N-methylglucamine, and a pharmaceutically acceptable carrier.10-13-2011
20090030038Novel 8-Sulfonylamino-3 Aminosubstituted Chroman or Tetrahydronaphtalene Derivatives Modulating the 5Ht6 Receptor - The present invention relates to new compounds of formula I. (I) wherein R01-29-2009
20120122921PROCESS FOR MAKING MODULATORS OF CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR - The invention provides a process for the preparation of a compound of Formula 1,05-17-2012
20120122922COMPOSITIONS OF N-[2,4-BIS(1,1-DIMETHYLETHYL)-5-HYDROXYPHENYL]-1,4-DIHYDRO-4-OXOQUINOLINE- -3-CARBOXAMIDE - Pharmaceutical compositions including N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide (Compound 1) and methods of using such compositions are described herein.05-17-2012
200901434274-Oxoquinoline derivatives - This invention relates to novel compounds that are 4-oxoquinoline derivatives and pharmaceutically acceptable salts thereof. More specifically, this invention relates to novel 4-oxoquinoline derivatives that are derivatives of elvitegravir. This invention also provides pyrogen-free compositions comprising one or more compounds of this invention and a carrier, and the use of the disclosed compounds and compositions in methods of treating diseases and conditions that are beneficially treated by administering an HIV integrase inhibitor, such as elvitegravir.06-04-2009
20080242700Methods and Compositions for Selectin Inhibition - The present teachings relate to compounds of formula I:10-02-2008
20080306110Alkylnitrile Quinolines as Nk-3 Receptor Ligands - Compounds of Formula I12-11-2008
20080214605Alkyl Sulfoxide Quinolines as Nk-3 Receptor Ligands - Compounds of Formula I09-04-2008
20080214604Medicinal Composition - A pharmaceutical composition comprising: an active ingredient consisting of 4-(3-chloro-4-(cyclopropylaminocarbonyl)aminophenoxy)-7-methoxy-6-quinolinecarboxamide, salt thereof, or solvate of the foregoing; and (i) a compound, a 5% (w/w) aqueous solution or suspension of which has a pH of 8 or more, and/or (ii) silicic acid, salt thereof, or solvate of the foregoing is a highly stable pharmaceutical composition, wherein under humidified and heated storage conditions, the decomposition of said compound is sufficiently reduced, or the gelation on the surface of the pharmaceutical composition is sufficiently inhibited.09-04-2008
20080255191BENZYLIMIDAZOLYL SUBSTITUTED 2-QUINOLINE AND QUINAZOLINE DERIVATIVES FOR USE AS FARNESYL TRANSFERASE INHIBITORS - This invention comprises the novel compounds of formula (I)10-16-2008
20080255192Methods and Compositions for Selectin Inhibition - The present teachings relate to novel compounds of formula I:10-16-2008
200802551908-Cyanoquinolonecarboxylic Acid Derivative - To provide a quinolone antibacterial drug and a therapeutic agent for infectious diseases, which exhibit potent antibacterial activity on Gram-positive and Gram-negative bacteria and which is highly safe.10-16-2008
20110112141CRYSTALS OF LAQUINIMOD SODIUM, AND PROCESS FOR THE MANUFACTURE THEREOF - Disclosed is a process for the preparation of laguinimod sodium which removes the impurities after the salt formation step, thus resulting in crystals of higher purity as well as crystals having improved crystalline characteristics.05-12-2011
20120302600STABLE LAQUINIMOD PREPARATIONS - The invention relates to a pharmaceutical composition comprising a pharmaceutically acceptable salt of N-ethyl-N-phenyl-1,2,-dihydro-4-hydroxy-5-chloro-1-methyl-2-oxoquinoline-3-carboxamide, N-methylglucamine, and a pharmaceutically acceptable carrier.11-29-2012
20100298375 MEDICAMENT COMPRISING A CARBOSTYRIL DERIVATIVE AND DONEPEZIL FOR TREATING ALZHEIMER'S DISEASE - The invention relates to a medicament for treating Alzheimer's disease comprising as active ingredients a carbostyril derivative of the general formula: wherein A is a lower alkylene group, R is a cycloalkyl group, the bonding between 3- and 4-positions of the carbostyril skeleton is a single bond or a double bond, or a salt thereof; and donepezil or a salt thereof.11-25-2010
20100324087COMBINED USE OF ANGIOGENESIS INHIBITOR AND TAXANE - The problems of the present invention are to find a pharmaceutical composition and a method for treating cancer that exhibit excellent anti-tumor effect. Excellent anti-tumor effect is achieved when 4-(3-chloro-4-(cyclopropylaminocarbonyl)aminophenoxy)-7-methoxy-6-quinolinecarboxamide, an analogous compound thereof, a pharmacologically acceptable salt thereof or a solvate thereof is used in combination with taxane.12-23-2010
20100324088Fused Pyridone M1 Receptor Positive Allosteric Modulators - The present invention is directed to fused pyridone compounds of formula (I) (I) that are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.12-23-2010
20100168162SELECTIVE INHIBITORS OF AKT AND METHODS OF USING SAME - The present invention describes an improved method for screening compounds for activity in inhibiting the enzymatic activity of Akt1 protein kinase, also known as Protein Kinase B, an enzyme that is believed to play a key role in the inhibition of apoptosis and thus in the etiology of cancer and other conditions, including neurodegenerative diseases. In general, the method comprises: (1) providing a plurality of compounds suspected of having Akt1 kinase inhibitory activity; (2) modeling the docking of each of the plurality of the compounds with a target binding site derived from the crystal structure of a ternary complex involving Akt1, a nonhydrolyzable ATP analogue, and a peptide substrate derived from a physiological AKT substrate such that the protein active site is defined including those residues within a defined distance from the nonhydrolyzable ATP analogue; (3) ranking the docked compounds by goodness of fit; (4) further selecting compounds from compounds high ranked by goodness of fit in docking by using one or more screening criteria; (5) optionally, visually analyzing structures of compounds selected in step (4) to remove any compounds with improbable docking geometry; and (6) experimentally testing the selected compounds from step (4) or step (5), if step (5) is performed, to determine their inhibitory activity against Akt1 in order to select compounds with Akt1 inhibitory activity. The invention also encompasses pharmaceutical compositions including compounds whose inhibitory activity against Akt1 is discovered by the screening method, as well as methods of use of the pharmaceutical compositions to treat cancer and other conditions.07-01-2010
20100168161DERIVATIVES OF 4-(2-AMINO-1-HYDROXYETHYL)PHENOL AS AGONISTS OF THE BETA2 ADRENERGIC RECEPTOR - The present relates to compounds of formula (I):07-01-2010
20110136863N-Heterocyclic M1 Receptor Positive Allosteric Modulators - The present invention is directed to compounds of formula (I) (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.06-09-2011
20110136861QUINOLONE INHIBITORS OF LIPOPROTEIN-ASSOCIATED PHOSPHOLIPASE A2 - The present invention relates to new quinolone inhibitors of lipoprotein-associated phospholipase A2 activity, pharmaceutical compositions thereof, and methods of use thereof.06-09-2011
20110190342GLYCINE B ANTAGONIST - The invention relates to quinoline derivatives as well as their pharmaceutically acceptable salts. The invention further relates to a process for the preparation of such compounds. The compounds of the invention are glycine B antagonists and are therefore useful for the control and prevention of various disorders, including neurological disorders.08-04-2011
20090197913SYNERGISTIC MODULATION OF FLT3 KINASE USING A FLT3 INHIBITOR AND A FARNESYL TRANSFERASE INHIBITOR - The invention is directed to a method of inhibiting FLT3 tyrosine kinase activity or expression or reducing FLT3 kinase activity or expression in a cell or a subject comprising the administration of a farnesyl transferase inhibitor and a FLT3 kinase inhibitor selected from compounds of Formula I′:08-06-2009
20100029715POLYMORPHIC FORMS OF A MACROCYCLIC INHIBITOR OF HCV - Provided are crystalline forms of the compound of formula (I), which is a macrocyclic inhibitor of HCV, processes for the preparation thereof, and pharmaceutical compositions comprising these crystalline forms.02-04-2010
20100029714AQUEOUS PHARMACEUTICAL SUSPENSIONS CONTAINING REBAMIPIDE AND MANUFACTURING PROCESS THEREOF - The invention provides a rebamipide-containing aqueous pharmaceutical suspension which can be prepared by a simple process and keep the dispersed fine-particle state of rebamipide stable without having the fine particle agglutinated. The rebamipide-containing aqueous pharmaceutical suspension of the invention is prepared by mixing polyvinyl alcohol and additionally a sodium salt compound with rebamipide.02-04-2010
20100022586BICYCLIC HETEROARYL INHIBITORS OF PDE4 - The present invention relates to compounds and methods which may be useful as inhibitors of phosphodiesterase 4 (PD E4) for the treatment or prevention of inflammatory diseases and other diseases involving elevated levels of cytokines and proinflammatory mediators.01-28-2010
20100022585BETA- AND GAMMA-AMINO-ISOQUINOLINE AMIDE COMPOUNDS AND SUBSTITUTED BENZAMIDE COMPOUNDS - Disclosed are beta and gamma-amino isoquinoline amide compounds and substituted benzamide compounds. In particular, the invention provides compounds that affect the function of kinases in a cell and that are useful as therapeutic agents or with therapeutic agents. The compounds of the invention are useful in the treatment of a variety of diseases and conditions including eye diseases such as glaucoma, cardiovascular diseases, and diseases characterized by abnormal growth, such as cancers. The invention further provides compositions containing the beta or gamma-amino isoquinoline amide compounds or substituted benzamide compounds.01-28-2010
20100160372TREATMENT OF PROTEINOPATHIES USING A FARNESYL TRANSFERASE INHIBITOR - Methods and pharmaceutical compositions comprising a low dose of a farnesyl transferase inhibitor useful in the treatment of proteinopathies are provided. These low doses are below the doses used in oncological treatments for which these compounds were initially designed. The treatment includes administering to a subject in need thereof a therapeutically effective amount of a farnesyl transferase inhibitor, wherein the amount is effective to inhibit the farnesylation of a non-Ras FTase substrate involved in the autophagy pathway without substantially affecting the farnesylation of Ras or other oncology related substrates. Treatments in accordance with the present invention may also include an acetylcholinesterase inhibitor, an activator of neurotrophic receptors, an NMDA antagonist, an amyloid deposit inhibitor, an antipsychotic agent, an antidepressant, an anxiolytic, or an antioxidant.06-24-2010
20100197727Quinoline Derivatives as Antibacterial Agents - Use of a compound for the manufacture of a medicament for the treatment of a bacterial infection provided that the bacterial infection is other than a Mycobacterial infection, said compound being a compound of formula (Ia) or (Ib)08-05-2010
201101523163,4-SUBSTITUTED PIPERIDINE DERIVATIVES AS RENIN INHIBITORS - The present invention relates to 3,4-substituted piperidinyl-based renin inhibitor compounds bearing at 4-position Isoqumolone and having the Formula (I): The invention further relates to pharmaceutical compositions containing said compounds, as well as their use in treating cardiovascular events and renal insufficiency.06-23-2011
20110306634Amorphous Salt of a Macrocyclic Inhibitor of HCV - The amorphous form of the sodium salt of the macrocyclic inhibitor of HCV of formula:12-15-2011
20100331363TREATMENT OF MITOCHONDRIAL DISORDERS USING A FARNESYL TRANSFERASE INHIBITOR - Methods and pharmaceutical compositions comprising a low dose of a farnesyl transferase inhibitor useful in the treatment of proteinopathies are provided. These low doses are below the doses used in oncological treatments for which these compounds were initially designed. The treatment includes administering to a subject an amount of a farnesyl transferase inhibitor, wherein the amount administered is sufficient to cause an improvement in mitochondrial health in said subject. Treatments in accordance with the present invention may also include an acetylcholinesterase inhibitor, an activator of neurotrophic receptors, an NMDA anatagonist, an amyloid deposit inhibitor, an antipsychotic agent, an antidepressant, an anxiolytic, or an antioxidant.12-30-2010
20100120851PRENYLTRANSFERASE INHIBITORS FOR OCULAR HYPERTENSION CONTROL AND THE TREATMENT OF GLAUCOMA - The invention concerns in one embodiment a method of treating glaucoma or elevated intraocular pressure comprising administering a pharmaceutically effective amount of a composition comprising at least one prenyltransferase inhibitor. In another embodiment, the invention concerns a composition for the treatment of elevated intraocular pressure and glaucoma comprising a pharmaceutically effective amount of a prenyltransferase inhibitor.05-13-2010
20100022587DERIVATIVES OF 2-PHENYL-3-HYDROXYQUINOLINE-4(1H)-ONE AND METHODS OF THEIR PREPARATION AND UTILIZATION - Derivatives of 2-phenyl-3-hydroxyquinoline-4(1H)-one of the general formula (II), where X represents a nitro group, amino group, and Y represents an atom of halogen, oxygen or sulphur substituted by C01-28-2010
20110034508Treatment of BDNF-related disorders using laquinimod - This application provides for a method of increasing brain-derived neurotrophic factor (BDNF) serum level in a human subject comprising periodically administering to the subject an amount of laquinimod or pharmaceutically acceptable salt thereof effective to increase BDNF serum level in the human subject. The method can further comprise periodically administering to the subject an amount of a second BDNF-increasing agent. This application also provides for a method for treating a human subject suffering from a BDNF-related disease comprising periodically administering laquinimod or a pharmaceutically acceptable salt thereof in an amount effective to treat the human subject. This application additionally provides for use of laquinimod in the manufacture of a medicament for increasing BDNF serum level in a human subject. This application further provides for a pharmaceutical composition comprising an amount of laquinimod effective for use in increasing BDNF serum level in a human subject. This application also provides for a pharmaceutical preparation comprising an amount of laquinimod and an amount of a second BDNF-increasing agent effective for use in increasing BDNF serum level in a human subject.02-10-2011
20100210684Amine salt of carbostyril derivative - The invention provides an amine salt of a carbostyril derivative formed from a carbostyril derivative represented by the formula (1) [wherein R is a halogen atom; the substituted position of the side chain is 3- or 4-position in the carbostyril skeleton; and the bonding between 3- and 4-positions of the carbostyril skeleton is a single bond or a double bond] and an amine; and the invention is useful as drugs for treating various diseases, especially as aqueous formulations due to the superior water solubility and the superior pharmacologic effects.08-19-2010
20090036485Quinoline derivatives - The invention concerns quinoline derivatives of Formula (I) or a pharmaceutically-acceptable salt, solvate or pro-drug thereof, wherein each of p, R02-05-2009
20120046313SILOXANE POLYMER CONTAINING TETHERED FLUOROQUINOLONE - A polymer that is a polysiloxane polymer has fluoroquinolone antibiotic groups, or pharmaceutically acceptable salts thereof, attached via linkers. The linkers may be hydrolytically labile thereby providing a manner of releasing the fluoroquinolone antibiotic from the polymer.02-23-2012
20120010238DEUTERATED N-ETHYL-N-PHENYL-1,2-DIHYDRO-4-HYDROXY-5-CHLORO-1-METHYL-2-OXOQ- UINOLINE-3-CARBOXAMIDE, SALTS AND USES THEREOF - The subject invention provides deuterated N-ethyl-N-phenyl-1,2-dihydro-4-hydroxy-5-chloro-1-methyl-2-oxoquinoline-3-carboxamide, its salts and uses.01-12-2012
20120010237COMPOUNDS HAVING ANTIPARASITIC OR ANTI-INFECTIOUS ACTIVITY - A method for inhibiting a parasitic or infectious disease in a subject, wherein the parasitic or infectious disease is selected from one caused by 01-12-2012
20090163544Use of NK-3 Receptor Antagonists for the Treatment of Nausea and Vomiting - This invention relates to the treatment or prevention of nausea and/or vomiting by the administration of a NK-3 receptor antagonist.06-25-2009
20110166179ANTIBACTERIAL QUINOLINE DERIVATIVES - The present invention relates to novel substituted quinoline derivatives according to the general formula (Ia) or formula (Ib):07-07-2011
20120015977QUINOLINONE DERIVATIVES USEFUL FOR THE TREATMENT OF CNS DISORDERS - The present invention relates to novel quinolinone derivatives (I), efficacious in animal models of CNS disorders and, as such, valuable candidates for the prevention or treatment of CNS (Central Nervous System) diseases or disorders. In other aspects the invention relates to pharmaceutical compositions comprising the quinolinone derivatives of the invention and to the use of these compounds for therapeutic applications.01-19-2012
20120059033Crystalline Salts of a Potent HCV Inhibitor - This invention relates to novel tris(hydroxymethyl)aminomethane, choline and N-methyl-D-glucamine salt forms of the following Compound (1) and methods for the preparation thereof, pharmaceutical compositions thereof, and their use in the treatment of Hepatitis C Viral (HCV) infection:03-08-2012
20090298874BACTERIAL ATP SYNTHASE BINDING DOMAIN - This invention provides an isolated mutant atpE protein and departing from said mutant atpE protein the identification of an ATPase binding domain. This invention also provides related nucleic acids, vectors, host cells, pharmaceutical compositions and articles of manufacture. This invention further provides methods for determining whether a test compound interacts with an atpE protein, i.e. with the ATPase binding domain of the present invention, as well as pharmaceuticals compositions comprising said test compound, in particular as antimicrobials, more particular as antimycobacterial agent, even more particular for treating tuberculosis in a subject.12-03-2009
20120071506METHODS FOR TREATING CNS DISORDERS WITH BICYCLO-SUBSTITUTED 2-IMIDAZOLINE AND 2-IMIDAZOLES - The present invention relates to a method for treating a disorder selected from depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder, stress-related disorders, psychotic disorders such as schizophrenia, neurological diseases such as Parkinson's disease, neurodegenerative disorders such as Alzheimer's disease, epilepsy, migraine, hypertension, substance abuse and metabolic disorders such as eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders which comprises administering to an individual a therapeutically effective amount of a compound of formula I03-22-2012
20120071505SUBSTITUTED PYRIDINE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS, AND METHODS OF USE TO TREAT OXIDATIVE STRESS - Substituted pyridine derivatives, methods of their preparation, pharmaceutical compositions comprising a substituted pyridine derivative, and methods of use in treating inflammation are provided. The substituted pyridine derivatives may control of the activity or the amount or both the activity and the amount of heme-oxygenase.03-22-2012
20120157492ANTIBIOTIC DRUG - This invention relates to a malic acid salt of (3S,5R)-7-[3-amino-5-methyl-piperidinyl]-1-cyclopropyl-1,4-dihydro-8-methoxy-4-oxo-3-quinolinecarboxylic acid. Also disclosed is a method of treating bacterial infection by an effective amount of this salt.06-21-2012
20120071504MODULATORS OF CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR - This invention relates to a compound of Formula I:03-22-2012
20120208843Method of Using GPR35 to Identify Metabolic-Stabilizing Compounds - The present invention relates to a method for identifying a metabolic stabilizing compound, comprising: a) contacting a candidate compound with GPR35, and b) determining whether GPR35 functionality is increased, wherein an increase in GPR35 functionality is indicative of the candidate compound being a metabolic stabilizing compound. The invention further relates to a method for treating or preventing a metabolic-related disorder, comprising administering to an individual in need thereof an effective amount of a GPR35 modulator.08-16-2012
20110105558EYE-DROP PREPARATION AND USE THEREOF - Disclosed is a technique for preventing the decomposition of latanoprost (a thermally unstable substance) contained in an eye-drop solution to stabilize the eye-drop solution. Specifically disclosed is an eye-drop preparation comprising latanoprost and carteolol hydrochloride. By adding carteolol hydrochloride to an eye-drop solution containing latanoprost which is a thermally unstable substance and is likely to be adhered on the surface of a container, it becomes possible to prevent the decomposition of latanoprost in the eye-drop solution and also prevent the loss of latanoprost caused by the adsorption of latanoprost on the surface of a container.05-05-2011
20110105557FARNESYL PROTEIN TRANSFERASE INHIBITOR COMBINATIONS WITH ANTIESTROGEN AGENTS - The present invention is concerned with combinations of a farnesyl transferase inhibitor and an antiestrogen agent for inhibiting the growth of tumor cells, useful in the treatment of cancer.05-05-2011
20100093792CRYSTALLINE FORMS OF A POTENT HCV INHIBITOR - This invention relates to novel crystalline forms of the following Compound (1), and the sodium salt thereof, and methods for the preparation thereof, pharmaceutical compositions thereof, and their use in the treatment of Hepatitis C Viral (HCV) infection:04-15-2010
20100093791Therapeutic Compositions - There is provided the use of a 5-HT04-15-2010
20120258983Pharmaceutical Composition and Administrations Thereof - The present invention relates to pharmaceutical compositions comprising a solid dispersion of N-[2,4-Bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide, methods of manufacturing pharmaceutical compositions of the present invention, and methods of administering pharmaceutical compositions of the present invention.10-11-2012
20120165372SOLID FORMS OF N-[2,4-BIS(1,1-DIMETHYLETHYL)-5-HYDROXYPHENYL]-1,4-DIHYDRO-4-OXOQUINOLINE- -3-CARBOXAMIDE - Solid forms of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide are described herein, including crystalline forms thereof.06-28-2012
20120165371SPIRO SUBSTITUTED COMPOUNDS AS ANGIOGENESIS INHIBITORS - The present invention relates to spiro (tetracarbon) substituted compound of Formula I, processes for their preparation, pharmaceutical compositions containing them as active ingredient, methods for the treatment of disease states associated with angiogenesis, such as cancers associated with protein tyrosine kinases, to their use as medicaments for use in the production of inhibition of tyrosine kinases reducing effects in warm-blooded animals such as humans.06-28-2012
20120165370QUINOLINE DERIVATIVES AS ANTI-CANCER AGENTS - Quinoline derivatives showing anticancer activities against cancer cell lines of hepatocellular carcinoma (Hep3B), lung carcinoma (A549), esophageal squamous cell carcinoma (HKESC-1, HKESC-4 and KYSE150). The quinoline derivatives have a backbone structure of the following formulas:06-28-2012
201201653693-SUBSTITUTED QUINOLINIUM AND 7H-INDOLO[2,3-c]QUINOLINIUM SALTS AS NEW ANTIINFECTIVES - The present invention relates to quinolinium antiinfective agents in which the qunolinium nucleus is fused to an indole ring or the qunolinium nucleus is linked to a cyclic structure through an opened indole or a benzothiophene or benzofuran ring. The compound is further substituted with various substituent groups.06-28-2012
20120136025QUINOLONE DERIVATIVE OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF - Disclosed are quinolone derivatives characterized in that these have lower alkyl, cycloalkyl or the like at the 1-position; —N(R05-31-2012
20100173939ANTIVIRAL COMPOUNDS - The present invention relates to macrocyclic compounds of formula (I) that are useful as inhibitors of hepatitis C virus (HCV) NS3 protease, their synthesis, and their use for treating or preventing HCV infection.07-08-2010
20120252840Method of Treating Cancer - This invention is directed to the treatment of cancer, particularly ocular melanoma, with a dual inhibitor of MET and VEGF such as Compound 1.10-04-2012
20120172395SLOW-RELEASE CILOSTAZOL TABLET HAVING AN IMPROVED ELUTION RATE AND MINIMAL SIDE EFFECTS - Provided is a slow-release tablet including cilostazol as a pharmacologically active component, which is efficacious in suppressing aggregation of blood platelets and promoting vascular relaxation by inhibiting phosphodiesterase types. The slow-release cilostazol tablet has an extended elution time so that the slow-release cilostazol tablet can be taken once daily for convenience of drug use, and minimizes the manifestation of headache which is one side effect caused when women, the elderly and children take conventional cilostazol preparations so that the convenience of drug use can be improved. Also, the slow-release cilostazol tablet exhibits a stable elution pattern with no variation in elution rate according to changes in pH in the stomach and intestines, as well as an effect of delaying the release of a drug, using a mixture of hydroxypropyl methylcellulose and a carbomer as a release-controlling polymer.07-05-2012
20120172394PHARMACEUTICAL COMPOSITION FOR PREVENTING OR TREATING RHEUMATOID ARTHRITIS, CONTAINING REBAMIPIDE - The present invention provides a pharmaceutical composition for preventing or treating rheumatoid arthritis comprising rebamipide as an active ingredient and a pharmaceutically acceptable carrier. The pharmaceutical composition may be for oral administration, for example an oral solid dosage form of a tablet or capsule form. The pharmaceutical composition may be formulated into a unit dosage form suitable for orally administering rebamipide in a dose ranging from 0.5 to 50 mg/kg, preferably from 0.6 to 6 mg/kg.07-05-2012
20120214841SOLID FORMS OF N-[2,4-BIS(1,1-DIMETHYLETHYL)-5-HYDROXYPHENYL]-1,4-DIHYDRO-4-OXOQUINOLINE- -3-CARBOXAMIDE - The present invention relates to solid state forms of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide (Compound 1), pharmaceutical compositions thereof and methods therewith.08-23-2012
20100048620COMPOSITION FOR TREATMENT OF UNDIFFERENTIATED GASTRIC CANCER - Disclosed are: a therapeutic agent, a kit and a treatment method for undifferentiated gastric cancer; and a pharmaceutical composition, a kit and a treatment method which are more effective on a living organism having at least one cell selected from the group consisting of a cell overexpressing FGFR2 and a cell expressing a mutant FGFR2. A combination of a FGFR2 inhibitor and a therapeutic substance for gastric cancer is more effective on undifferentiated gastric cancer. The combination of a FGFR2 inhibitor and a therapeutic substance for gastric cancer is more effective on a living organism having at least one cell selected from the group consisting of a cell overexpressing FGFR2 and a cell expressing a mutant FGFR2.02-25-2010
20100010040Triazol Derivatives Useful For The Treatment of Diseases - The invention relates to compounds of formula (1)01-14-2010
20100292271Quinoline Compounds Suitable for Treating Disorders that Respond to Modulation of the Serotonin-5-HT6 Receptor - The present invention relates to novel quinoline compounds of the formula (I) and to the salts thereof. The compounds possess valuable therapeutic properties and are particularly suitable, for treating diseases that respond to modulation of the serotonin 11-18-2010
20100292270TREATMENT OF CACHEXIA - The present invention provides a means for prevention and treatment of cachexia and other chronic illnesses including but not limited to the promotion of weight gain, reduction or prevention of weight loss by administration of a substance that both reduces the sensitivity of beta-adrenergic receptors and of 5-HT1a receptors. (S)-pindolol, (S)-propranolol, tertatolol or bopindolol are preferred for this purpose.11-18-2010
20120220626NOVEL QUINOLINE COMPOUND, AND COMPOSITION CONTAINING CENTIPEDE EXTRACT OR COMPOUNDS ISOLATED THEREFROM FOR PREVENTION AND TREATMENT OF CARDIOVASCULAR DISEASE - The present invention relates to a composition for the prevention and treatment of cardiovascular diseases containing the novel quinoline compound, the centipede extracts or compounds isolated from the extracts. The novel quinoline compound, the centipede extracts or a quinoline compound and a phenol compound isolated from the extracts of the invention exhibit excellent LDL-antioxidant activity, ACAT inhibiting activity, and anti-inflammatory activities, so that they can be included as an effective ingredient in a composition for the prevention and treatment of cardiovascular disease including hyperlipidemia, atherosclerosis, coronary heart disease, and myocardial infarction mediated by LDL-oxidation, cholesteryl ester synthesis and accumulation, and inflammation.08-30-2012
20120220625PHARMACEUTICAL COMPOSITION AND ADMINISTRATIONS THEREOF - The present invention relates to pharmaceutical compositions comprising a solid dispersion of N-[2,4-Bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide, methods of manufacturing pharmaceutical compositions of the present invention, and methods of administering pharmaceutical compositions of the present invention.08-30-2012
20110124682PHARMACEUTICAL COMPOSITION COMPRISING REBAMIPIDE - An object of the present invention is to provide a pharmaceutical composition containing rebamipide, which is unnecessary to be re-dispersed, has an enough transparency, and exhibits neutral to weakly acidic pH not to injure the keratoconjunctiva of a patient suffering from dry eye. The present pharmaceutical composition comprises (1) rebamipide, (2) an amino sugar, and (3) an buffer agent, which has no inorganic cation.05-26-2011
20090076074QUINOLINE DERIVATIVES - The invention concerns quinoline derivatives of Formula I03-19-2009
20120270899Compositions and Methods for Treating Cardiovascular Diseases - The present specification discloses pharmaceutical compositions, methods of preparing such pharmaceutical compositions, and methods and uses of treating a cardiovascular disease in an individual using such pharmaceutical compositions.10-25-2012
20100234422Sulfonylated Heterocycles Useful for Modulation of the Progesterone Receptor - Compounds of the following structure are provided, wherein n, R09-16-2010
20120277264ANTITHROMBOTIC AGENT - An object of the present invention is to provide an antithrombotic agent that has fewer side effects and that is highly effective. The present invention provides an antithrombotic agent comprising (±)-[2-[4-(3-ethoxy-2-hydroxypropoxy)phenylcarbamoyl]ethyl]dimethylsulfonium p-toluenesulfonate represented by Formula (1) as an active ingredient.11-01-2012
20100204272Compounds which have activity at M1 receptor and their uses in medicine - Compounds of formula (I) or a salt thereof are provided:08-12-2010
20100204271STABLE CRYSTAL OF 4-OXOQUINOLINE COMPOUND - Provision of a stabilized crystal of 6-(3-chloro-2-fluorobenzyl)-1-[(S)-1-hydroxymethyl-2-methylpropyl]-7-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylic acid (compound A). A crystal of compound A, which shows a particular X-ray powder diffraction pattern of a characteristic diffraction peaks at diffraction angles 2θ(°) as measured by X-ray powder diffractometry.08-12-2010
20100204270Quinoline Derivatives as Antibacterial Agents - Use of a compound for the manufacture of a medicament for the treatment of a bacterial infection provided that the bacterial infection is other than a Mycobacterial infection, said compound being a compound of formula (Ia) or (Ib) a pharmaceutically acceptable acid or base addition salt thereof, a stereochemically isomeric form thereof, a tautomeric form thereof or a N-oxide form thereof. Several of these compounds are also claimed as such. Further the combination of the above compounds with other antibacterial agents is described08-12-2010
20120329829Dopamine Transporter Inhibitors for Use in Treatment of Movement Disorders and Other CNS Indications - The invention provides a class of dopamine transporter inhibitors of formula (I) (DAS inhibitors), packaged pharmaceuticals comprising such inhibitors, and their uses treating, or the manufacturing medicaments for treating disease conditions, including Parkinson's disease, Hoehn and Yahr Staging of Parkinson's Disease. Unified Parkinson Disease Rating Scale (UPDRS), and Schwab and England Activities of Daily Living Scale. Related business methods such as marketing the inhibitors to healthcare providers are also provided.12-27-2012
201300125373,8-DIAMINOTETRAHYDROQUINOLINE DERIVATIVE - A method for treatment of a systemic wasting disease, by administering, to a subject in need thereof, an effective amount of a 3,8-diaminotetrahydroquinoline derivative represented by formula (Ia) (wherein X represents CH01-10-2013
20100130547SOLID FORMS OF N-(4-(7-AZABICYCLO[2.2.1]HEPTAN-7-YL)-2-(TRIFLUORORMETHYL)PHENYL)-4-OXO-5- -(TRIFLUOROMETHYL)-1,4-DIHYROQUINOLINE-3-CARBOXAMIDE - The present invention relates to solid state forms, for example, crystalline forms of N-(4-(7-azabicyclo[2.2.1]heptan-7-yl)-2-(trifluoromethyl)phenyl)-4-oxo-5-(trifluoromethyl)-1,4-dihydroquinoline-3-carboxamide, pharmaceutical compositions thereof, and methods therewith.05-27-2010
20100130546QUINOLONE COMPOUND AND PHARMACEUTICAL COMPOSITION - The present invention provides a quinolone compound represented by General Formula (1)05-27-2010
20110136862NOVEL TETRAMETHYL SUBSTITUTED PIPERIDINE DERIVATIVES AND THEIR USE AS MONOAMINE NEUROTRANSMITTER RE-UPTAKE INHIBITORS - This invention relates to novel tetramethyl substituted pipehdine derivatives useful as monoamine neurotransmitter re-uptake inhibitors. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.06-09-2011
20080255193Pharmaceutical Composition - A novel pharmaceutical composition comprising the NK10-16-2008
20080227811Spiro Substituted Compounds As Angiogenesis Inhibitors - The present invention relates to spiro (tetracarbon) substituted compound of Formula I, processes for their preparation, pharmaceutical compositions containing them as active ingredient, methods for the treatment of disease states associated with angiogenesis, such as cancers associated with protein tyrosine kinases, to their use as medicaments for use in the production of inhibition of tyrosine kinases reducing effects in warm-blooded animals such as humans.09-18-2008
20080221160SULFONYLATED HETEROCYCLES USEFUL FOR MODULATION OF THE PROGESTERONE RECEPTOR - Compounds of the following structure are provided, wherein n, R09-11-2008
20080221159Inhibitors of human immunodeficiency virus replication - Compounds of formula I:09-11-2008
20080221158Novel 14 and 15 Membered Ring Compounds - The present invention relates to 15-membered macrolides substituted at the 4″ position of formula (I)09-11-2008
20130178498BICYCLIC HETEROARYL INHIBITORS OF PDE4 - The present invention relates to compounds and methods which may be useful as inhibitors of phosphodiesterase 4 (PDE4) for the treatment or prevention of inflammatory diseases and other diseases involving elevated levels of cytokines and proinflammatory mediators.07-11-2013
20130178499Novel Substituted Quinoline Compounds as S-Nitrosoglutathione Reductase Inhibitors - The present invention is directed to novel quinoline compounds useful as S-nitrosoglutathione reductase (GSNOR) inhibitors, pharmaceutical compositions comprising such compounds, and methods of making and using the same.07-11-2013
20130143919PHARMACEUTICAL COMPOSITIONS AND ADMINISTRATIONS THEREOF - The present invention relates to pharmaceutical compositions comprising a compound of Formula I in combination with one or both of a Compound of Formula II and/or a Compound of Formula III. The invention also relates to solid forms and to pharmaceutical formulations thereof, and to methods of using such compositions in the treatment of CFTR mediated diseases, particularly cystic fibrosis.06-06-2013
20120252841Substituted 2-mercaptoquinoline-3-carboxamides as KCNQ2/3 modulators - The invention relates to substituted 2-mercaptoquinoline-3-carboxamides, methods for the preparation thereof, medicaments containing these compounds and the use of these compounds for the preparation of medicaments.10-04-2012
20110269794External Preparation for Athlete's Foot Treatment - External preparations for athlete's foot treatment capable of enhancing patient's compliance and capable of reducing the symptom of rubefaction, comprising an anti-trichophyton drug mixed with at least one compound selected from among 1-menthol, menthol analogue compounds and bactericidal compounds.11-03-2011
20130116280Fusion protein comprising C-terminal domain of RET protein and use thereof as a diagnosing marker - A fusion protein including N-terminal domain of a fusion partner at N-terminal and C-terminal domain of RET protein at C-terminal, a fusion gene encoding the fusion protein, and a use of the fusion protein or the fusion gene as a diagnosing marker for a cancer, are provided.05-09-2013
20130116279BICYCLIC HETEROARYL INHIBITORS OF PDE4 - The present invention relates to compounds and methods which may be useful as inhibitors of phosphodiesterase 4 (PDE4) for the treatment or prevention of inflammatory diseases and other diseases involving elevated levels of cytokines and proinflammatory mediators.05-09-2013
20130096157QUINOLINE DERIVATIVES AND USES OF THE SAME - Provided is a quinoline derivative of Chemical Formula (I):04-18-2013
20130096158Treatment Of Multiple Sclerosis With Combination Of Laquinimod And Fingolimod - This invention provides a method of treating a subject afflicted with multiple sclerosis or presenting a clinically isolated syndrome comprising administering to the subject laquinimod as an add-on therapy to or in combination with fingolimod. This invention also provides a package and a pharmaceutical composition comprising laquinimod and fingolimod for treating a subject afflicted with multiple sclerosis or presenting a clinically isolated syndrome. This invention also provides laquinimod for use as an add-on therapy or in combination with fingolimod in treating a subject afflicted with multiple sclerosis or presenting a clinically isolated syndrome. This invention further provides use of laquinimod and fingolimod in the preparation of a combination for treating a subject afflicted with multiple sclerosis or presenting a clinically isolated syndrome.04-18-2013
20130102631NOVEL MICROBIOCIDAL DIOXIME ETHER DERIVATIVES - The present invention provides compounds of formula (I) wherein R04-25-2013
20130102630Derivatives of the Aminated Hydroxyquinoline Class For Treating Cancers - The invention relates to compounds of the aminated hydroxyquinoline type capable of preventing the migration of metastases or tumoral cells. Such compounds are useful for treating cancers.04-25-2013
20130131107PHARMACEUTICAL COMPOSITIONS AND ADMINISTRATIONS THEREOF - The present invention relates to pharmaceutical compositions comprising a compound of Formulas I and II, optionally in combination with a Compound of Formula III and/or a Compound of Formula IV. The invention also relates to solid forms and to pharmaceutical formulations thereof, and to methods of using such compositions in the treatment of CFTR mediated diseases, particularly cystic fibrosis.05-23-2013
20100280069CONTROLLED RELEASE LOCAL ANESTHETIC FOR POST DENTAL SURGERY AND METHOD OF USE - The present invention relates to a method of delivering local anesthetic after dental extraction surgery. The present invention relates to packing the tooth socket with a tinned release local anesthetic which is coordinated with an initial local anesthetic and which lasts up to 5 days. The socket can be surgically sealed or the implant can act as the sealing means.11-04-2010
20130143918Solid Forms of (R)-1(2,2-Difluorobenzo[D][1,3]Dioxol-5-yl)-N-(1-(2,3-Dihydroxypropyl-6-F- luoro-2-(1-Hydroxy-2-Methylpropan-2-yl)-1H-Indol-5-yl)-Cyclopropanecarboxa- mide - The present invention relates to solid forms of (R)-1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)-N-(1-(2,3-dihydroxypropyl)-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)-1H-indol-5-yl)cyclopropanecarboxamide (Compound 1) in substantially crystalline form (Form A) or amorphous form, pharmaceutical compositions thereof, and methods of treatment therewith.06-06-2013
20100041697PNEUMONIA TREATMENT - This invention relates to a method of treating pneumonia by orally administering to a subject in need thereof a quinolone compound of formula (I), shown in the disclosure, at a daily dose of 2-30 mg/kg.02-18-2010
20080200503Macrocylic Inhibitors Of Hepatitis C Virus - Inhibitors of HCV of formula (I).08-21-2008
20110230519SOLID FORMS OF N-[2,4-BIS(1,1-DIMETHYLETHYL)-5-HYDROXYPHENYL]-1,4-DIHYDRO-4-OXOQUINOLINE- -3-CARBOXAMIDE - The present invention relates to solid state forms of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide (Compound 1), pharmaceutical compositions thereof and methods therewith.09-22-2011
20110251234MESYLATE SALT OF 5-(2--1-HYDROXYETHYL)-8-HYDROXYQUINOLIN-2(1H)-ONE AS AGONIST OF THE BETA2 ADRENERGIC RECEPTOR - The present disclosure relates to a mesylate salt of 5-(2-{[6-(2,2-difluoro-2-phenylethoxy)hexyl]amino}-1-hydroxyethyl)-8-hydroxyquinolin-2(1H)-one as well as pharmaceutical compositions comprising them, and their use in therapy as agonists of the β2 receptor.10-13-2011
20130150404BIPHENYL DERIVATIVES - This invention provides biphenyl derivatives of formula I:06-13-2013
201003176933,8-DIAMINOTETRAHYDROQUINOLINE DERIVATIVE - To provide a compound which has a potent agonistic activity on GHS-R and which is useful as a therapeutic agent for systemic wasting diseases such as cachexia.12-16-2010
20100317692Quinolone M1 Receptor Positive Allosteric Modulators - The present invention is directed to quinolone compounds of general formula (I)12-16-2010
20120283289CRYSTALLINE FORM OF A BIPHENYL COMPOUND - The invention provides a crystalline 1,2-ethanedisulfonic acid salt of biphenyl-2-ylcarbamic acid 1-[2-(2-chloro-4-{[(R)-2-hydroxy-2-(8-hydroxy-2-oxo-1,2-dihydroquinolin-5-yl)ethylamino]methyl}-5-methoxyphenylcarbamoyl)ethyl]piperidin-4-yl ester or a solvate thereof. This invention also provides pharmaceutical compositions comprising such a salt or prepared using such a salt; processes and intermediates for preparing such a salt; and methods of using such a salt to treat a pulmonary disorder.11-08-2012
20130184310TREATMENT OF LUPUS ARTHRITIS USING LAQUINIMOD - This invention provides a method of treating a subject afflicted with active lupus arthritis comprising periodically administering to the subject an amount of laquinimod or pharmaceutically acceptable salt thereof effective to treat the subject. This invention also provides laquinimod or pharmaceutically acceptable salt thereof for use in treating a subject afflicted with active lupus arthritis. This invention further provides a pharmaceutical composition comprising an amount of laquinimod or pharmaceutically acceptable salt thereof for use in treating a subject afflicted with lupus arthritis.07-18-2013
20110288123FORMULATIONS FOR THE TREATMENT OF ACUTE HERPES ZOSTER PAIN - The present invention provides compositions and methods that are useful for treatment of pain associated with acute herpes zoster. The aqueous compositions are non-stinging and non-irritating.11-24-2011
20110288122Pharmaceutical Compositions and Administrations Thereof - The present invention relates to the use of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide, solids forms, and pharmaceutical compositions thereof for the treatment of CFTR mediated diseases, particularly cystic fibrosis, in patients possessing specific genetic mutations.11-24-2011
20110288121Processes for Producing Modulators of Cystic Fibrosis Transmembrane Conductance Regulator - The present invention relates to the process for producing modulators of cystic fibrosis transmembrane conductance regulator (CFTR).11-24-2011
20110312995BRIDGED AND FUSED HETEROCYCLIC ANTIDIABETIC COMPOUNDS - This invention provides for certain bridged and fused heterocyclic compounds of the formula (I) or a pharmaceutically acceptable salt, ester solvate or prodrug thereof wherein: L is: (II) and the other variables are defined herein; the inventive compounds are agonists of the G-protein coupled receptor 40 (GPR40, also known as free fatty acid receptor FFAR). This invention further relates to pharmaceutical compositions containing these compounds, and the use of these compounds to regulate insulin levels in a mammal. The compounds may be used, for example in the prevention and treatment of Type 2 diabetes mellitus and in the prevention and treatment of conditions related to Type 2 diabetes mellitus, such as insulin resistance, obesity and lipid disorders.12-22-2011
20110312994BIPHENYL DERIVATIVES - This invention provides biphenyl derivatives of formula I:12-22-2011
20120029015Novel medical use of kynurenic acid, its precursors and derivatives - The invention relates to the use of kynurenic acid derivatives of general formula (I),02-02-2012
201200290145-(2--1-HYDROXYETHYL)-8-HYDROXYQUINOLIN-2 (1H)-ONE FOR THE TREATMENT OF LUNG FUNCTION - A compound which is a hydroxyquinolinone derivative of formula (I),02-02-2012
20130203806CILOSTAZOL COCRYSTALS AND COMPOSITIONS - The invention relates to improvements of the physiochemical and/or the pharmaceutical properties of cilostazol. Disclosed herein are several new compositions and cocrystals of cilostazol, including: a 1:1 cilostazol gentisic acid cocrystal, a 1:1:1 cilostazol gentisic acid H08-08-2013
20130203807USE OF LAQUINIMOD FOR TREATING CROHN'S DISEASE PATIENTS WHO FAILED FIRST-LINE ANTI-TNF THERAPY - This application provides for a method of treating a human patient afflicted with anti-TNFα refractory Crohn's disease, of treating a human patient afflicted with non-fibrostenotic Crohn's disease, and of treating a human patient whose Crohn's disease had not been surgically treated, the method comprising periodically administering to the patient an amount of laquinimod or pharmaceutically acceptable salt thereof effective to treat the patient. This application also provides for a method of inducing or maintaining clinical remission in a human patient afflicted with Crohn's disease comprising periodically administering to the patient an amount of laquinimod effective to induce or maintain clinical remission in the patient, which amount of laquinimod is less than 0.5 mg/day.08-08-2013
20130203808Drug for degradation and treatment of biofilms - The invention comprising decoquinate and one or both of a redox drug or macrolide drug for prophylaxis or treatment of certain biofilms and plaques in humans and animals.08-08-2013
20120077842QUINOLINE DERIVATIVE-CONTAINING PHARMACEUTICAL COMPOSITION - A pharmaceutical composition comprising a compound represented by the formula (I) or pharmaceutically acceptable salt thereof or solvate thereof; and a basic substance is excellent in dissolution, is stable even after a long term storage, and is useful as a preventive or therapeutic agent against a tumor:03-29-2012

Patent applications in class Chalcogen attached directly to the six-membered hetero ring by nonionic bonding