Class / Patent application number | Description | Number of patent applications / Date published |
514302000 | Ring oxygen in the bicyclo ring system | 58 |
20080262029 | Acid and Base Salt Forms of Gaboxadol - The present invention is directed to novel acid salt forms and base salt forms of the compound gabaoxadol (4,5,6,7-tetrahydroisoxazolo[5,4-c]pyridin-3-ol) and hydrates, solvates and polymorphic forms thereof. The invention is further concerned with pharmaceutical compositions containing the salt forms as an active ingredient, methods for treatment of disorders susceptible to amelioration by GABAA receptor agonism with the salt forms, and processes for the preparation of the salt forms. | 10-23-2008 |
20080269278 | Treatment of Impaired Respiratory Function with Gaboxadol - The present invention relates to a method for treating impaired respiratory function in a human patient suffering from sleep apnea, such as central sleep apnea or obstructive sleep apnea, comprising administering to said patient an effective amount of gaboxadol per day. | 10-30-2008 |
20080269279 | Substituted furo[2,3-B] pyridine derivatives as cannabinoid-1 receptor modulators - Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, Alzheimer's disease, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson's disease, movement disorders, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, the treatment of obesity or eating disorders, as well as the treatment of asthma, constipation, chronic intestinal pseudo-obstruction, cirrhosis of the liver, non-alcoholic fatty liver disease (NAFLD), non-alcoholic steatohepatitis (NASH), and the promotion of wakefulness. | 10-30-2008 |
20080306108 | Substituted Pyridoxines As Anti-Platelet Agents - Compounds with antiplatelet aggregation characteristics for the treatment of cardiovascular and cardiovascular related disease, are described. The methods are directed to administering pharmaceutical compositions comprising a pyridoxine analogue. | 12-11-2008 |
20090018157 | Chemical compounds - Compounds of Formula (I) wherein: R | 01-15-2009 |
20090048288 | METHOD OF TREATING STRESS-MEDIATED DEPRESSION - The present invention relates to a method for the treatment of depression comprising administering a therapeutically effective amount of gaboxadol to a patient, wherein the level of one or more inflammatory markers in said patient is increased or abnormal. The present invention also relates to a method for the treatment of stress-mediated depression comprising administering a therapeutically effective amount of gaboxadol to a patient, wherein the level of one or more inflammatory markers is increased or abnormal in said patient. The present invention also relates to a method for the treatment of depression or the amelioration of one or more depressive symptoms comprising administering a therapeutically effective amount of gaboxadol to a patient, wherein the clinical presentation of one or more symptoms of depression are the physiological effect of a general medical condition. Furthermore the present also relates to a method for testing the therapeutic effectiveness of a compound in the treatment of depression or reducing the symptoms of depression comprising measuring the amount of one or more inflammatory markers in a sample from a patient before said compound is administered to the patient and comparing with the amount of said one or more inflammatory markers in a sample from the same patient after administration of said compound to the patient. | 02-19-2009 |
20090076068 | IMIDAZOPYRIDIN-2-ONE DERIVATIVES AS INHIBITORS OF LIPASES AND PHOSPHOLIPASES - The present invention relates to imidazopyridin-2-one derivatives of the formula I with the definitions specified in the description, to their pharmaceutically usable salts and to their use as medicaments. | 03-19-2009 |
20090099227 | G-Protein Coupled Receptor Agonists - Compounds of Formula (I) or pharmaceutically acceptable salts or N-oxides thereof, are agonists of GPR116 and are useful for the treatment of obesity, and for the treatment of diabetes. | 04-16-2009 |
20090118324 | MAPK/ERK KINASE INHIBITORS - Compounds are provided for use with MEK that comprise: | 05-07-2009 |
20090131468 | Bis-(Sulfonylamino) Derivatives in Therapy 065 - The invention provides compounds of formula | 05-21-2009 |
20090203731 | TREATMENT OF DEPRESSION AND OTHER AFFECTIVE DISORDERS - The present invention relates to use of gaboxadol for preparing a pharmaceutical composition for treating depression. Moreover, it relates to the use of gaboxadol for the preparation of a pharmaceutical composition to be used in combination with a serotonin reuptake inhibitor, or any other compound which causes an elevation in the level of extracellular serotonin. | 08-13-2009 |
20090281138 | Bis-(Sulfonylamino) Derivatives in Therapy 066 - The invention provides compounds of formula | 11-12-2009 |
20100048610 | CARBINOL DERIVATIVES HAVING CYCLIC LINKER - [Object] To provide a novel LXRβ agonist that is useful as a preventative and/or therapeutic agent for atherosclerosis; arteriosclerosis such as those resulting from diabetes; dyslipidemia; hypercholesterolemia; lipid-related diseases; inflammatory diseases that are caused by inflammatory cytokines; skin diseases such as allergic skin diseases; diabetes; or Alzheimer's disease. | 02-25-2010 |
20100081686 | Pyridone derivatives having a binding activity to the cannabinoid type 2 recepter - It was found that the compound having a binding activity to the cannabinoid type 2 receptor represented by the formula (I): | 04-01-2010 |
20100093787 | TREATMENT OF IMPAIRED RESPIRATORY FUNCTION WITH GABOXADOL - The present invention relates to a method for treating impaired respiratory function in a human patient suffering from sleep apnea, such as central sleep apnea or obstructive sleep apnea, comprising administering to said patient an effective amount of gaboxadol per day. | 04-15-2010 |
20100120839 | PYRAZOLES USEFUL IN THE TREATMENT OF INFLAMMATION - There is provided compounds of formula I, | 05-13-2010 |
20100210681 | AQUEOUS PHARMACEUTICAL COMPOSITION - The present invention relates to an aqueous pharmaceutical composition comprising 1-(2-dimethylaminoethyl)-3-((2R,4aS,5R,10bS)-5-phenyl-9-trifluoromethyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-2-ylmethyl)urea as active compound, to a liquid pharmaceutical composition which is suitable for the preparation of the aqueous pharmaceutical composition, and to a process for the preparation of the compositions. | 08-19-2010 |
20100234419 | SUBSTITUTED 3-AMINOISOXAZOLOPYRIDINES AS KCNQ2/3 MODULATORS - The invention relates to substituted 3-aminoisoxazolopyridines, 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 |
20100331358 | TETRAHYDROFUROPYRIDONES - The present invention relates to Tetrahydrofuropyridones compounds useful as HIF prolyl hydroxylase inhibitors to treat anemia and like conditions. | 12-30-2010 |
20110039883 | AZOLOPYRIDIN-2-ONE DERIVATIVES AS LIPASE AND PHOSPHOLIPASE INHIBITORS - The present invention provides compounds which have an inhibitory effect on hormone-sensitive lipase or endothelial lipase. The compounds of the invention are azolopyridin-2-one derivatives of the general formula I | 02-17-2011 |
20110046175 | BENZOFURAN CANNABINOID COMPOUNDS AND RELATED METHODS OF USE - Furanopyridine cannabinoid analog compounds of the formula I are disclosed. | 02-24-2011 |
20110046176 | FURANOPYRIDINE CANNABINOID COMPOUNDS AND RELATED METHODS OF USE - Furanopyridine cannabinoid analog compounds of the formula I are disclosed. | 02-24-2011 |
20110053974 | CARBOXYLIC ACID COMPOUND - To find a therapeutic agent and/or a preventive agent for diabetes mellitus or the like having excellent activity and safety. A compound represented by the following general formula (I), or a pharmacologically acceptable salt thereof. In the formula, X represents ═C(R5)- or ═N—; Y represents —O— or —NH—; L represents a bond or a substitutable C1-C3 alkylene group; M represents a substitutable C3-C10 cycloalkyl group, a substitutable C6-C10 aryl group, or a substitutable heterocyclic group; R | 03-03-2011 |
20110082171 | Medicaments and Methods for Inhibition of Scarring - Provided is the use of an agonist of a GABA | 04-07-2011 |
20110112137 | HIV PROTEASE INHIBITOR AND CYTOCHROME P450 INHIBITOR COMBINATIONS - Compositions and methods of treating viral infections are provided. More particularly, compositions including a combination of protease inhibitors and cytochrome p450 enzyme inhibitors are provided. Methods of using the compositions for treatment of diseases or disorders caused by a virus such as HIV infections are also provided. | 05-12-2011 |
20110178120 | HIV INTEGRASE INHIBITORS FROM PYRIDOXINE - The present invention relates to pyridoxine (vitamin B | 07-21-2011 |
20110301190 | POLYMORPHIC FORMS OF A GABAA AGONIST - The present invention is directed to novel polymorphic forms of the compound 4,5,6,7-tetrahydroisoxazolo[5,4-c]pyridin-3-ol hydrate (gaboxadol monohydrate). The invention is further concerned with pharmaceutical compositions containing the polymorphic forms as an active ingredient, methods for treatment of disorders susceptible to amelioration by GABAA receptor agonism with the polymorphic forms, and processes for the preparation of the polymorphic forms. | 12-08-2011 |
20120035207 | Use of GABAA Receptor Agonists for the Treatment of Hearing, Vestibular and Attention Disorders, Intention Tremor and Restless Leg Syndrome - The invention provides a method of treating a condition selected from hearing disorders, vestibular disorders, attention disorders, intention tremor and restless leg syndrome comprising administering to a human patient in need thereof a therapeutically effective amount of a compound which is an agonist at GABA | 02-09-2012 |
20120115901 | PORPHYRIN COMPOUNDS COMPRISING ONE OR MORE PYRIDONE MOIETIES - Various porphyrin compounds comprising one or more pyridone moieties, intermediates thereof, compositions thereof, and, methods of making and using thereof. | 05-10-2012 |
20120142724 | OXAZOLO[5-4-b]PYRIDIN-5-YL COMPOUNDS - The present invention provides oxazolo[5,4-b]pyridin-5-yl compounds useful in the treatment of cancer. | 06-07-2012 |
20120190709 | Indazolyl-substituted dihydroisoxa-zolopyridines and methods of use thereof - This invention relates to novel 4-(indazol-5-yl)-4,7-dihydroisoxazolo[5,4-b]pyridine derivatives having protein tyrosine kinase inhibitory activity, to a process for the manufacture thereof and to the use thereof for the treatment of c-Met-mediated diseases or c-Met-mediated conditions, particularly cancer and other proliferative disorders. | 07-26-2012 |
20120202845 | DIURETICS - A compound having the structure formula (I) or a pharmaceutically acceptable salt thereof, and methods of using the compounds for treating hypertension. | 08-09-2012 |
20120208838 | DIURETICS - A compound having the structure (I) wherein R is selected from the group consisting of 1) and 2), or a pharmaceutically acceptable salt thereof, and methods of using the compounds for treating hypertension. | 08-16-2012 |
20120289542 | CICLETANINE IN COMBINATION WITH ORAL ANTIDIABETIC AND/OR BLOOD LIPID-LOWERING AGENTS AS A COMBINATION THERAPY FOR DIABETES AND METABOLIC SYNDROME - Preferred embodiments of the present invention are related to novel therapeutic drug combinations and methods for treating and/or preventing complications in patients with diabetes and/or metabolic syndrome. More particularly, aspects of the present invention are related to using a combination of cicletanine and an oral antidiabetic agent for treating and/or preventing complications (including microalbuminuria, nephropathies, retinopathies and other complications) in patients with diabetes or metabolic syndrome. | 11-15-2012 |
20120316195 | ARYL-PYRIDINE DERIVATIVES AS ALDOSTERONE SYNTHASE INHIBITORS - The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein R | 12-13-2012 |
20120316196 | Compounds Which Have Activity at M1 Receptor and Their Uses in Medicine - Compounds of formula (I) or a salt thereof are provided: | 12-13-2012 |
20120329827 | DERIVATIVES OF PYRIDOXINE FOR INHIBITING HIV INTEGRASE - The present invention relates to compounds of Formula I or pharmaceutically acceptable salts, solvates or formulations thereof. Compounds of Formula I inhibit HIV-integrase enzyme and are useful for preventing and treating of HIV infection and AIDS. | 12-27-2012 |
20130023557 | CARBOXYLIC ACID DERIVATIVES HAVING AN OXAZOLO[5,4-B]PYRIDINE RING - The invention therefore relates to compounds of the formula I | 01-24-2013 |
20130023558 | CARBOXYLIC ACID DERIVATIVES HAVING AN OXAZOLO[4,5-c]PYRIDINE RING - Carboxylic acid derivatives having an oxazolo[4,5-c]pyridine ring | 01-24-2013 |
20130079366 | Benzisoxazoles and Azabenzisoxazoles as MGLUR4 Allosteric Potentiators, Compositions, and Methods of Treating Neurological Dysfunction - Benzisoxazole and azabenzisoxazole compounds which are useful as allosteric potentiators/positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds, for example, in treating neurological and psychiatric disorders or other disease state associated with glutamate dysfunction. | 03-28-2013 |
20130090353 | NOXIOUS ARTHROPOD CONTROL COMPOSITION AND HETEROCYCLIC COMPOUND - A noxious arthropod controlling composition comprising a heterocyclic compound represented by the formula (1) [wherein, A | 04-11-2013 |
20130116275 | INHIBITORS OF HIF AND ANGIOGENESIS - Inhibitors of the Hypoxia Inducible Factor (HIF) and angiogenesis and their methods of use including the treatment of cancer, hypoxia related pathologies, disorders leading to ischemia, for example stroke and ischemic heart disease, and non-cancerous angiogenic diseases are provided. | 05-09-2013 |
20130150401 | NEW COMPOUNDS, PHARMACEUTICAL COMPOSITIONS AND USES THEREOF - The present invention relates to compounds of formula I, | 06-13-2013 |
20130158070 | CONJUGATES OF POLYUNSATURATED FATTY ACIDS AND AMINE-CONTAINING COMPOUNDS AND USES THEREOF - Novel chemical conjugates derived from unsaturated fatty acids and therapeutically active agents, are disclosed. The chemical conjugates are designed and characterized as COX-2 and/or 5-LOX inhibitors and are useful in the treatment of inflammatory diseases and disorders such as Alzheimer's disease, Parkinson's disease, asthma, osteoarthritis, rheumatoid arthritis, pain, primary dysmenorrhea, Crohn's disease and ulcerative colitis. | 06-20-2013 |
20130245063 | COMPOUNDS THAT MODULATE INTRACELLULAR CALCIUM - Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity. | 09-19-2013 |
20130331410 | 2,3-DIHYDROFURO[2,3-c]PYRIDIN-2-YLPIPERIDINE DERIVATIVES - The present invention relates to compounds of general formula I, | 12-12-2013 |
20130345255 | TRPV1 ANTAGONISTS - Disclosed herein are compounds of formula (I) or pharmaceutically acceptable salts, prodrugs, or combinations thereof, | 12-26-2013 |
20140275154 | Novel Compounds for the Treatment of Hepatitis C - The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV. | 09-18-2014 |
20140275155 | SUBSTITUTED BICYCLIC 1-CARBOXYLIC-ACID (BENZYL-CYANO-METHYL)-AMIDES INHIBITORS OF CATHEPSIN C - This invention relates to bicyclic 1-carboxylic-acid (benzyl-cyano-methyl)-amides of formula 1 | 09-18-2014 |
20140275156 | FLAVONOID COMPOUNDS, AND METHODS OF USE THEREOF - There is provided now flavonoid compounds, compositions containing these compounds, methods for their synthesis, and uses of these compounds. In particular, there is provided methods of preventing and or mitigating the damage caused by cell apoptosis or cell necrosis by administration of the novel flavonoid compounds. In some aspects, there is provided methods for inhibiting pro-apoptotic signalling kinases activity in a subject while regulating and activating extracelluar signal regulated kinase (ERK). | 09-18-2014 |
20150025106 | THERMOGEL FORMULATION FOR COMBINATION DRUG DELIVERY - The invention provides a drug delivery system for a combination of therapeutic agents. The system includes a water soluble biodegradable ABA-type triblock copolymer that possesses thermosensitive gelation properties. The system can form a stable thermogel that includes a combination of therapeutic agents including, for example, rapamycin, paclitaxel, and 17-AAG. After administration to a subject, the drugs are released at a controlled rate from the thermogel, which biodegrades into non-toxic components. The polymer system can also function to increase the solubility and stability of drugs in the composition. | 01-22-2015 |
20150038527 | FUROPYRIDINE DERIVATIVES - Compounds of the formula I | 02-05-2015 |
20150087672 | AROMATIC RING COMPOUND - The present invention provides an aromatic ring compound having a melanin-concentrating hormone receptor antagonistic action and useful as an agent for the prophylaxis or treatment of obesity and the like. The present invention relates to a compound represented by the formula | 03-26-2015 |
20150352085 | METHODS OF INCREASING TONIC INHIBITION AND TREATING SECONDARY INSOMNIA - Methods of increasing tonic inhibition in a subject in need thereof, for example a subject with Fragile X syndrome or Angelman syndrome are disclosed. Methods of treating secondary insomnia in a subject with a neurodegenerative disease or disorder are also disclosed. The methods can include administering the subject an effective amount of 4,5,6,7-tetrahydroisoxazolo(5,4-c)pyridin-3-ol (THIP) or a derivative thereof, or a pharmaceutically acceptable salt thereof, increase tonic inhibition in neurons of the subject; to increase slow wave sleep (SWS) and/or slow wave activity (SWA), normalize sleep architecture, reduce secondary insomnia, increase non-rapid eye movement (NREM) sleep, increase sleep continuity, enhance delta activity within NREM, increase or improve total sleep time (TST), increase or improve sleep efficiency, reduce total time awake (TAA), reduce number of awakenings (NWA), reduce latency to persistent sleep (LPS), or to reduce wake after sleep onset (WASO), in the subject, or any combination thereof. | 12-10-2015 |
20160024103 | FUSED FURANS FOR THE TREATMENT OF HEPATITIS C - The disclosure provides compounds of formula I or II, including their salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV. | 01-28-2016 |
20160038469 | METHODS OF INCREASING TONIC INHIBITION AND TREATING SECONDARY INSOMNIA - Methods of increasing tonic inhibition in a subject in need thereof, for example a subject with Fragile X syndrome or Angelman syndrome are disclosed. Methods of treating secondary insomnia in a subject with a neurodegenerative disease or disorder are also disclosed. The methods can include administering the subject an effective amount of 4,5,6,7-tetrahydroisoxazolo(5,4-c)pyridin-3-ol (THIP) or a derivative thereof, or a pharmaceutically acceptable salt thereof, increase tonic inhibition in neurons of the subject; to increase slow wave sleep (SWS) and/or slow wave activity (SWA), normalize sleep architecture, reduce secondary insomnia, increase non-rapid eye movement (NREM) sleep, increase sleep continuity, enhance delta activity within NREM, increase or improve total sleep time (TST), increase or improve sleep efficiency, reduce total time awake (TAA), reduce number of awakenings (NWA), reduce latency to persistent sleep (LPS), or to reduce wake after sleep onset (WASO), in the subject, or any combination thereof. | 02-11-2016 |
20160060254 | THIAZOLE-BASED INHIBITORS OF SCAVENGER RECEPTOR BI - This application describes compounds and methods that can inhibit Scavenger receptor class B, type I (SR-BI) activity, which compounds and methods can used, for example, to mediate high-density lipoprotein (HDL) lipid uptake and treat hepatitis C viral infections. | 03-03-2016 |
20170233345 | SUBSTITUTED QUINOLINE-4-CARBOXAMIDES AND USE THEREOF | 08-17-2017 |