| Class / Patent application number | Description | Number of patent applications / Date published |
|---|
| 514230200 | Ring nitrogen shared by two of the cyclos | 58 |
| 20130045971 | INDUCED HYPOTHERMIA - Sudden cardiac arrest is treated by reducing blood temperature from about 37° C. to 33° C., following resuscitation, by injecting hypothermia inducing drugs such as a cannabinoid type into the patient's body, preferably in combination with physical surface body cooling. | 02-21-2013 |
| 20080214534 | (1,10B-Dihydro-2-(Aminoalkyl-Phenyl)-5H-Pyrazolo[1,5-C][1,3]Benzoxazin-5-Yl)Phenyl Methanone Derivatives as Hiv Viral Replication Inhibitors - The present invention relates to 5H-pyrazolo[1,5-c][1,3]benzoxazin-5-yl)phenyl methanone derivatives as inhibitors of the viral replication of the HIV virus, processes for their preparation as well as pharmaceutical compositions, their use as medicines, and diagnostic kits comprising them. The present invention also concerns combinations of the present HIV inhibitors with other anti-retroviral agents. It further relates to their use in assays as reference compounds or as reagents. The compounds of the present invention are useful for preventing or treating infection by HIV and for treating AIDS. | 09-04-2008 |
| 20130029977 | Fused substituted aminopyrrolidine derivative - A quinolone synthetic antibacterial agent having excellent properties as a medicine is provided, which has strong antibacterial activity not only to Gram-negative bacteria but also to Gram-positive cocci that have low sensitivity to quinolone antibacterial agents, and which exhibits high safety and excellent pharmacokinetics. A compound represented by the formula (I) or a salt thereof, or a hydrate thereof. Specifically, a quinolone derivative of the formula (I) wherein substituents R6 and R7 taken together with the carbon atoms to which they are bonded form a cyclic structure which may contain an oxygen atom as a ring constituent atom, the cyclic structure forming a 5-4, 5-5, or 5-6 fused bicyclic pyrrolidinyl substituent, the substituent being bonded to a quinolone mother skeleton Q containing a pyridobenzoxazine structure. | 01-31-2013 |
| 20130040943 | TRICYCLIC PYRIDYL-VINYL PYRROLES AS PAR1 INHIBITORS - This disclosure relates to compounds of formula I: | 02-14-2013 |
| 20130096109 | PYRIDONE DERIVATIVE HAVING INTEGRASE INHIBITORY ACTIVITY - An object of the present invention is to provide a novel integrase inhibitor. The present invention relates to a novel compound having an antiviral effect, more specifically, a pyridone derivative having HIV integrase inhibitory activity, and a medicament containing the same, in particular, an anti-HIV agent. The compound of the present invention has integrase inhibitory activity and/or cell proliferation inhibitory activity against viruses, in particular, HIV and drug-resistant strains thereof. Thus, the compound is useful in preventing or treating various diseases, viral infections (for example, AIDS), and the like in which integrase participates. | 04-18-2013 |
| 20090270379 | QUINOLONE DERIVATIVES USEFUL AS ANTIBACTERIAL AGENTS - The present invention is directed to quinolone derivatives, useful as antimicrobial compounds, pharmaceutical compositions comprising said derivatives and the use of said derivatives and pharmaceutical compositions as antimicrobial agents against pathogenic microorganisms, particularly against resistant microbes | 10-29-2009 |
| 20090270378 | NOVEL TETRAHYDROPYRIDOTHIOPHENES - Compounds of a certain formula (I), in which Ra and Rb have the meanings indicated in the description, are novel effective compounds with anti-proliferative and/or apoptosis inducing activity. | 10-29-2009 |
| 20090012072 | FLUOROQUINOLONE COMPOSITIONS - The invention relates to pharmaceutical compositions comprising (i) a fluoroquinolone, (ii) a salt formed between a carboxylate anion and a divalent metal cation, (iii) a liquid comprising an organic solvent selected from the group consisting of glycerol, propylene glycol, glycerol formal, and (iv) optionally water. The invention further relates to methods of treating or preventing a condition in an animal comprising administering to the animal in need thereof a pharmaceutical composition of the invention. | 01-08-2009 |
| 20130123249 | NOVEL BENZOXAZINE OXAZOLIDINONE COMPOUNDS, PREPARATION METHODS AND USES THEREOF - Novel benzoxazine oxazolidinone compounds, preparation methods and uses thereof are disclosed, which belong to the field of pharmacy. More specifically, novel benzoxazine oxazolidinone compounds represented by the following general formula (I), preparation methods and uses thereof in preparing medicament for treating infectious diseases, especially infectious diseases caused by multi-drug resistant bacteria, are disclosed. | 05-16-2013 |
| 20100184755 | PROTEIN KINASE C INHIBITORS AND USES THEREOF - This disclosure concerns compounds which are useful as inhibitors of protein kinase C (PKC) and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of PKC. This disclosure also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes. | 07-22-2010 |
| 20100022524 | TRICYCLIC TETRAHYDROQUINOLINE ANTIBACTERIAL AGENTS - The invention includes tetrahydroquinoline and related compounds of formula I, and pharmaceutical compositions thereof, that exhibit useful antibacterial activity against a wide range of human and veterinary pathogens. | 01-28-2010 |
| 20110172219 | CYANOAMINOQUINOLONES AND TETRAZOLOAMINOQUINOLONES AS GSK-3 INHIBITORS - Provided herein are aminoquinolones and pharmaceutically acceptable derivatives thereof. In certain embodiments, provided herein are compounds, compositions and methods for treating, preventing or ameliorating GSK-3 mediated diseases. | 07-14-2011 |
| 20080280893 | SUBSTITUTED-DIHYDRO[1,4]OXAZINO[2,3,4-hi]INDAZOLE DERIVATIVES AS 5-HYDROXYTRYPTAMINE-6 LIGANDS - The present invention provides a compound of formula I and the use thereof for the treatment of a central nervous system disorder related to or affected by the 5-HT6 receptor. | 11-13-2008 |
| 20120295898 | Antiviral Therapy - The present invention relates to combinations of compounds comprising HIV integrase inhibitors and other therapeutic agents. Such combinations are useful in the inhibition of HIV replication, the prevention and/or treatment of infection by HIV, and in the treatment of AIDS and/or ARC. | 11-22-2012 |
| 20120295899 | BENZYLPYRROLIDINONE DERIVATIVES AS MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY - The present application describes modulators of MCP-1 or CCR-2 of formula | 11-22-2012 |
| 20110269751 | HETEROCYCLIC NITROGENOUS OR OXYGENOUS COMPOUNDS WITH INSECTICIDAL ACTIVITY FORMED FROM DIALDEHYDES AND THEIR PREPARATION AND USES THEREOF - The heterocyclic nitrogenous or oxygenous compounds of formula (A), (B), (C) or (D) formed from dialdehydes, their optical isomers, cis- and trans- isomers, or agrochemically acceptable salts, their preparation methods, agrochemical compositions comprising the compounds and the uses thereof are provided. The compounds and their derivatives have high insecticidal activities to several farming and forestry pests including homoptera and lepidoptera pests, such as aphis, fulgorid, whitefly, leafhopper, common thrips, cotton bollworm, cabbage caterpillar, cabbage moth, cotton leafworm, armyworm and so on. | 11-03-2011 |
| 20090163485 | HETEROARYL DERIVATIVES AS OREXIN RECEPTOR ANTAGONISTS - The present invention relates to compounds of formula | 06-25-2009 |
| 20080261964 | Substituted quinolones II - The invention relates to substituted quinolones of formula (I) and to methods for their preparation as well as their use for the production of medicaments for the treatment and/or prophylaxis of diseases, especially for use as antiviral agents, in particular against cytomegaloviruses. | 10-23-2008 |
| 20090221565 | NOVEL 7-SUBSTITUTED 3-CARBOXY-OXADIAZINO-QUINOLONE DERIVATIVES, THEIR PREPARATION AND THEIR APPLICATION AS ANTI-BACTERIALS - A subject of the invention is the compounds of formula (I): | 09-03-2009 |
| 20090048242 | (1,10B-DIHYDRO-2-(AMINOALKYL-PHENYL)-5H-PYRAZOLO[1,5 C][1,3]BENZOXAZIN-5-YL)PHENYL METHANONE DERIVATIVES AS HIV VIRAL REPLICATION INHIBITORS - The present invention relates to 5H-pyrazolo[1,5-c][1,3]benzoxazin-5-yl)phenyl methanone derivatives as inhibitors of the viral replication of the HIV virus, processes for their preparation as well as pharmaceutical compositions, their use as medicines, and diagnostic kits comprising them. The present invention also concerns combinations of the present HIV inhibitors with other anti-retroviral agents. It further relates to their use in assays as reference compounds or as reagents. The compounds of the present invention are useful for preventing or treating infection by HIV and for treating AIDS. | 02-19-2009 |
| 20100273787 | KYNURENINE-AMINOTRANSFERASE INHIBITORS - Compounds of formula (I): prodrug derivatives and/or pharmaceutically acceptable salt thereof, selectively inhibit the enzyme kynurenine aminotransferase, thereby reducing the synthesis of kynurenic acid. The compounds are used for the treatment of psychiatric and neurological diseases which benefit from an increase in glutamatergic and/or cholinergic neurotransmission, such as schizophrenia, depression, bipolar illness, anxiety and Alzheimer's disease. Furthermore, the compounds of the invention are useful for stimulating attention, memory and other cognitive processes in normal individuals of any age, including children, adolescents and the elderly. Additionally, the compounds of the invention are also useful for treatment of patients suffering from malaria by preventing parasite gametogenesis and fertility based on reduction of xanthurenic acid formation from its bioprecursor 3-hydroxy kynurenine. | 10-28-2010 |
| 20100216781 | mTOR KINASE INHIBITORS FOR ONCOLOGY INDICATIONS AND DISEASES ASSOCIATED WITH THE mTOR/PI3K/AKT PATHWAY - Provided herein are Heteroaryl Compounds having the following structure: | 08-26-2010 |
| 20090042873 | TRICYCLIC N-HETEROARYL-CARBOXAMIDE DERIVATIVES CONTAINING A BENZIMIDAZOLE UNIT, METHOD FOR PREPARING SAME AND THEIR THERAPEUTIC USE - The invention concerns tricyclic N-heteroarylcarboxamide derivatives containing a benzimidazole unit of general formula (I): | 02-12-2009 |
| 20100144726 | NOVEL INDOLIC DERIVATIVES, THEIR PREPARATION PROCESSES AND THEIR USES IN PARTICULAR AS ANTIBACTERIALS - The invention relates to the use of at least one compound of the formula (I), | 06-10-2010 |
| 20120035166 | METHODS OF TREATING A PULMONARY BACTERIAL INFECTION USING FLUOROQUINOLONES - Disclosed herein are methods of treating a pulmonary bacterial infection comprising bacteria growing under anaerobic conditions using a fluoroquinolone antibiotic. The fluoroquinolone antibiotic may, for example, be levofloxacin or ofloxacin. Also disclosed are methods of inhibiting bacteria growing under anaerobic conditions by exposing the bacteria to an amount of fluoroquinolone antibiotic effective to inhibit growth of said bacteria. | 02-09-2012 |
| 20120245161 | INDOLYL-PIPERIDINYL BENZYLAMINES AS BETA-TRYPTASE INHIBITORS - The present invention discloses and claims a series of substituted indolyl-piperidinyl benzylamines of the formula | 09-27-2012 |
| 20090215762 | Siloxane polymer containing tethered levofloxacin - A polymer that is a polysiloxane polymer has Levofloxacin groups, or pharmaceutically acceptable salts thereof, attached via linkers. The linkers may be hydrolytically labile thereby providing a manner of releasing the Levofloxacin from the polymer. | 08-27-2009 |
| 20090029980 | C-7 Isoxazolinyl Quinolone / Naphthyridine Derivatives Useful as Antibacterial Agents - The present invention relates to C-7 isoxazolyl quinoline/naphthyridine derivatives useful as antimicrobial compounds, pharmaceutical compositions comprising said derivatives and the use of said derivatives and pharmaceutical compositions as antimicrobial agents against pathogenic microorganisms, particularly against resistant microbes. | 01-29-2009 |
| 20090029979 | 5-HTX MODULATORS - This invention relates to compounds which bind to serotonin receptors inside or outside the central nervous system, in particular compounds which bind to the 5-HT | 01-29-2009 |
| 20110053921 | HEXAHYDROOXAZINOPTERINE COMPOUNDS - The present invention provides mTOR inhibitors of the formula | 03-03-2011 |
| 20080221091 | Metalloprotease inhibitors containing a heterocyclic moiety - The present invention relates generally to pharmaceutical agents containing a heterocyclic moiety, and in particular, to heterocyclic metalloprotease inhibiting compounds. More particularly, the present invention provides a new class of heterocyclic MMP-13 inhibiting compounds with a modified benzoxazine moiety, that exhibit an increased potency and selectivity in relation to currently known MMP-13 inhibitors. | 09-11-2008 |
| 20110257167 | IDENTIFICATION OF LKB1 MUTATION AS A PREDICTIVE BIOMARKER FOR SENSITIVITY TO TOR KINASE INHIBITORS - Provided herein are methods for treating and/or preventing a cancer or a tumor syndrome in a patient, comprising administering an effective amount of a TOR kinase inhibitor to a patient having cancer or a tumor syndrome, characterized by a LKB1 and/or AMPK gene or protein loss or mutation. | 10-20-2011 |
| 20080280894 | DIHYDRO[1,4]OXAZINO[2,3,4-hi]INDAZOLE DERIVATIVES AS 5-HYDROXYTRYPTAMINE-6 LIGANDS - The present invention provides a compound of formula I and the use thereof for the treatment of a central nervous system disorder related to or affected by the 5-HT6 receptor. | 11-13-2008 |
| 20100298309 | TRICYCLIC TRIAZOLIC COMPOUNDS - The present invention relates to new tricyclic triazolic compounds having a high affinity for sigma-1 receptor as well as to the process for the preparation thereof, to composition comprising them and to their use as medicaments according to compounds of formula (I), Wherein R | 11-25-2010 |
| 20110263587 | REVERSIBLY HEAT-GELABLE AQUEOUS COMPOSITION - The present invention relates to a reversibly heat-gelable aqueous composition comprising a reversibly heat-gelable aqueous composition according to conventional technique, to which a thixotropic property-increasing substance is added. The thixotropic property-increasing substance is preferably at least one member selected from the group consisting of sugar alcohol, lactose, carmellose or pharmaceutically acceptable salts thereof and cyclodextrin. This composition can be stored at room temperature and accordingly, it is quite convenient for users to carry about the same. | 10-27-2011 |
| 20090156587 | Eye Medication Formulation with Antibacterial Agent - A formulation for administration to the eye has at least one pharmaceutical agent such as a mydriatic agent, a cycloplegic agent, an anesthetic or a non-steroidal anti-inflammation agent combined with an anti-bacterial agent and a suitable carrier. The formulation can be made for topical or intracameral administration to the eye. | 06-18-2009 |
| 20110053922 | Spiro (Piperidine-4,2'-Pyrrolidine)-1-(3,5-Trifluoromethyl Phenyl) Methylcarboxamides As NK1 Tachikynin Receptor Antagonists - Compounds of formula (I) or a pharmaceutically acceptable salt thereof | 03-03-2011 |
| 20110118247 | 2-Methyl-5-Imino-Benzo[D][1,3]Oxazin[5-B]Pyrazole Compound, Preparation and Use Thereof - The present invention disclosed compound 2-methyl-5-imino-benzo[d][1,3]oxazin[5-b]pyrazole and preparation method and uses thereof. The compound 2-methyl-5-imino-benzo[d][1,3]oxazin[5-b]pyrazole of the present invention has the following structure of formula (II), wherein the compound or pharmaceutically acceptable salts thereof can be used for preparing the drugs for treatment or prevention of cardiovascular diseases. | 05-19-2011 |
| 20080221090 | HCV NS5B Inhibitors - The invention encompasses compounds of Formula I as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV. | 09-11-2008 |
| 20110166131 | SUBSTITUTED PYRROLIDINE DERIVATIVE - A quinolone antibacterial compound, or a salt or hydrate of the compound, for the treatment of infectious diseases, which exhibit potent antibacterial activity and higher selective toxicity against Gram-positive and Gram-negative bacteria, which do not cause side effects (e.g., convulsion), which exhibit higher safety, and which has a structure of formula (I): | 07-07-2011 |
| 20120022056 | FUSED TRICYCLIC DERIVATIVES FOR THE TREATMENT OF PSYCHOTIC DISORDERS - Compounds of formula (I) wherein R | 01-26-2012 |
| 20090192147 | [a]-FUSED INDOLE COMPOUNDS, THEIR USE AS mTOR KINASE AND PI3 KINASE INHIBITORS, AND THEIR SYNTHESES - The invention relates to [a]-fused indole compounds of the Formula II, | 07-30-2009 |
| 20120028972 | BIOMARKER ASSAYS FOR DETECTING OR MEASURING INHIBITION OF TOR KINASE ACTIVITY - Provided herein are methods for detecting and/or measuring the inhibition of TOR kinase activity in a subject and uses associated therewith. | 02-02-2012 |
| 20120108582 | Fused substituted aminopyrrolidine derivative - A quinolone synthetic antibacterial agent having excellent properties as a medicine is provided, which has strong antibacterial activity not only to Gram-negative bacteria but also to Gram-positive cocci that have low sensitivity to quinolone antibacterial agents, and which exhibits high safety and excellent pharmacokinetics. A compound represented by the formula (I) or a salt thereof, or a hydrate thereof. Specifically, a quinolone derivative of the formula (I) wherein substituents R6 and R7 taken together with the carbon atoms to which they are bonded form a cyclic structure which may contain an oxygen atom as a ring constituent atom, the cyclic structure forming a 5-4, 5-5, or 5-6 fused bicyclic pyrrolidinyl substituent, the substituent being bonded to a quinolone mother skeleton Q containing a pyridobenzoxazine structure. | 05-03-2012 |
| 20110092494 | Tricyclic Tetrahydroquinoline Antibacterial Agents - The invention includes tetrahydroquinoline and related compounds of formula I, and pharmaceutical compositions thereof, that exhibit useful antibacterial activity against a wide range of human and veterinary pathogens. | 04-21-2011 |
| 20120316158 | OPHTHALMIC SOLUTION FOR TREATING OCULAR INFECTION COMPRISING LEVOFLOXACIN OR SALT THEREOF OR SOLVATE OF THE SAME, METHOD FOR TREATING OCULAR INFECTION, LEVOFLOXACIN OR SALT THEREOF OR SOLVATE OF THE SAME, AND USE THEREOF - Instillation of a 1.5% (w/v) levofloxacin ophthalmic solution three times a day, which is the dosage or dose regimen of the present invention, has features to cure bacterial conjunctivitis in a shorter time than instillation of a 0.5% (w/v) ophthalmic solution three times a day, which is the conventional dosage or dose regimen, and not to increase the rate of occurrence of side effects. Curing the ocular infection in a short time leads to shortening of the duration of exposure of the ocular-infection-causing bacterium to levofloxacin. Therefore, the levofloxacin ophthalmic solution in the dosage or dose regimen of the present invention is eventually expected to suppress emergence of the resistant bacterium resulting from the long-term use of the levofloxacin ophthalmic solution in the conventional dosage or dose regimen. In addition, it is confirmed that the levofloxacin ophthalmic solution in the dosage or dose regimen of the present invention directly inhibits the ocular-infection-causing bacterium such as | 12-13-2012 |
| 20120129846 | GAMMA SECRETASE MODULATORS - In its many embodiments, the present invention provides a novel class of heterocyclic compounds of the formula: as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the central nervous system using such compounds or pharmaceutical compositions. | 05-24-2012 |
| 20100204217 | TREATMENT FOR LEUKEMIA AND IDIOPATHIC APLASTIC ANEMIA - A process for treating a patient with leukemia or an aplastic anemia having cells with inclusions that stain with anti- | 08-12-2010 |
| 20120178748 | HETEROARYL COMPOUNDS AND METHODS OF USE THEREOF - Provided herein are heteroaryl compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. In one embodiment, the compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as CNS disorders and metabolic disorders, including, but not limited to, e.g., neurological disorders, psychosis, schizophrenia, obesity, and diabetes. | 07-12-2012 |
| 20100292227 | INHIBITORS OF HUMAN IMMUNODEFICIENCY VIRUS REPLICATION - Compounds of formula I: | 11-18-2010 |
| 20120220575 | N-SUBSTITUTED OXAZINOPTERIDINES AND OXAZINOPTERIDINONES - Disclosed are compounds of Formula 1, | 08-30-2012 |
| 20110003802 | Bridged N-Cyclic Sulfonamido Inhibitors of Gamma Secretase - The invention provides N-cyclic sulfonamido compounds and salts of Formula I: | 01-06-2011 |
| 20110003801 | BENZIMIDAZOLE DERIVATIVES USEFUL AS TRPM8 CHANNEL MODULATORS - Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: | 01-06-2011 |
| 20110003800 | BENZIMIDAZOLE DERIVATIVES USEFUL AS TRPM8 CHANNEL MODULATORS - Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: | 01-06-2011 |
| 20120094989 | 5-HT RECEPTOR MODULATING COMPOUNDS - The present invention relates to compounds having 5-hydroxytryptamine receptor modulating activity, in particular compounds having an acidic moiety held distant from the 5-HT pharmacophore by a rigid linker group, to compositions containing such compounds and methods of treatment using them. Such compounds have an increased affinity for the 5-HT receptor and a reduced hERG effect. Certain compounds of the invention further exhibit an angiotensin II receptor modulating activity. Claimed are compounds of formula (I): HT-L-A. HT is a 5-HT receptor modulating moiety containing a basic nitrogen atom; A is an acid moiety; L is a linker moiety. | 04-19-2012 |
| 20100234367 | 7-CYCLOALKYLAMINOQUINOLONES AS GSK-3 INHIBITORS - Provided herein are aminoquinolones of formula I and compositions containing the compounds. The compounds and compositions provided herein are useful in the prevention, amelioration or treatment of GSK-3 inhibitors mediated diseases. | 09-16-2010 |
| 20110275621 | HIV INTEGRASE INHIBITORS - Tricyclic compounds of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: | 11-10-2011 |
| 20120329790 | Dentinal Drug Delivery Composition - The present invention is a dentinal drug delivery composition composed of cationic and/or neutral porous particles containing an effective amount of a therapeutic agent and a method for using the same to provide a dental treatment. | 12-27-2012 |
