| Class / Patent application number | Description | Number of patent applications / Date published |
|---|
| 514119000 | C(=O)N containing | 39 |
| 20080312191 | Novel Urokinase Inhibitors - The present invention relates to novel compounds with inhibitory activity towards urokinase plasminogen activator (uPA); to methods for preparation of said uPA inhibitor compounds; to pharmaceutical compositions comprising said uPA inhibitor compounds; to the use of said uPA inhibitor compounds as a medicament and the use of said uPA inhibitor compounds for the preparation of a medicament for the treatment of conditions chosen from the group comprising cancer, tumour growth, tumour invasion, tumour metastasis, diabetic retinopathy, hemorrhagic atherosclerosis and inflammatory conditions, such as rheumatoid arthritis and psoriasis. | 12-18-2008 |
| 20090005349 | THERAPEUTIC USES OF GLUTATHIONE MIMICS - A prodrug having antioxidant activity, including a phosphorylated compound having a thiol group. A method of treating oxidative stress by administering a prodrug of a phosphorylated compound including a thiol group, removing a phosphate group of the prodrug, and treating oxidative stress. A method of increasing bioavailability of a thiol compound by creating a prodrug by phosphorylating a thiol compound, administering the prodrug, preventing first pass metabolism of the prodrug, removing a phosphate group from the prodrug, and providing active drug to a site in need of therapy from oxidative stress. A method of preventing radiation damage to healthy tissue by administering a prodrug comprising a phosphorylated compound including a thiol group, removing a phosphate group of the prodrug to provide active drug, and preventing radiation damage to healthy tissue. | 01-01-2009 |
| 20090054378 | IMMUNOMODULATORY COMPOUNDS AND TREATMENT OF DISEASES RELATED TO AN OVERPRODUCTION OF INFLAMMATORY CYTOKINES - Method of using immunomodulatory compounds for treating diseases related to an overproduction of inflammatory cytokines, including diseases selected from asthma, atopic dermatitis, allergic rhinitis, prostatitis, inflammatory bowel disease, diabetes, and rhumatoid arthritis, the compounds being of general formula (I): | 02-26-2009 |
| 20090124582 | Acyloxyalkyl Carbamate Prodrugs, Methods of Synthesis, and Use - Acyloxyalkyl carbamate prodrugs of 3-aminopropylphosphonous acid, 3-aminopropylphosphinic acid, and analogs thereof, pharmaceutical compositions comprising acyloxyalkyl carbamate prodrugs of 3-aminopropylphosphonous acid, 3-aminopropylphosphinic acid, and analogs thereof, methods of making prodrugs of 3-aminopropylphosphonous acid, 3-aminopropylphosphinic acid, and analogs thereof, methods of using prodrugs of 3-aminopropylphosphonous acid, 3-aminopropylphosphinic acid, and analogs thereof and pharmaceutical compositions thereof for treating or preventing diseases or disorders such as spasticity or gastroesophageal reflux disease are disclosed. Acyloxyalkyl carbamate prodrugs of 3-aminopropylphosphonous acid, 3-aminopropylphosphinic acid, and analogs thereof and sustained release oral dosage forms thereof, which are suitable for oral administration, are also disclosed. | 05-14-2009 |
| 20090137531 | Aryl Amide Sphingosine 1- - The present invention provides compounds that have antagonist activity at the S1P | 05-28-2009 |
| 20090203651 | USE OF SPHINGOLIPIDS IN THE TREATMENT AND PREVENTION OF TYPE 2 DIABETES MELLITUS, INSULIN RESISTANCE AND METABOLIC SYNDROME - The present invention relates to the use of sphingolipids for the preparation of a food item, a food supplement and/or a medicament for the treatment and/or prevention of insulin resistance, diabetes mellitus type 2 and/or Metabolic Syndrome. In particular, the invention relates to the use of a sphingolipid with the general formula (I): | 08-13-2009 |
| 20090209495 | USE OF EDG RECEPTOR BINDING AGENTS IN CANCER - Provided is a method for treating solid tumors, e.g. tumor invasiveness, and particularly inhibiting or controlling deregulated angiogenesis, using a sphingosine- | 08-20-2009 |
| 20090253658 | Fat Accumulation Inhibitor - To provide a fat accumulation inhibitor and a food or drink for inhibiting fat accumulation, a visceral fat accumulation inhibitor and a food or drink for inhibiting visceral fat accumulation, or an agent for accelerating increase and/or inhibiting decrease of an adiponectin concentration in blood and a food or drink for accelerating increase and/or inhibiting decrease of an adiponectin concentration in blood. | 10-08-2009 |
| 20090281066 | Treatment of proliferative disorders with amino-substituted (E)-2,6- dialkoxystyryl 4-substituted benzylsulfones - Methods of treating cancer using compounds according to Formula (I) are disclosed herein, wherein X, X | 11-12-2009 |
| 20090286759 | ACYLOXYALKYL CARBAMATE PRODRUGS, METHODS OF SYNTHESIS AND USE - Acyloxyalkyl carbamate prodrugs of 3-aminopropylphosphinic acid and analogs thereof, methods of making acyloxyalkyl carbamate prodrugs of 3-aminopropylphosphinic acid and analogs thereof, methods of using acyloxyalkyl carbamate prodrugs of 3-aminopropylphosphinic acid and analogs thereof, and pharmaceutical compositions comprising acyloxyalkyl carbamate prodrugs 3-aminopropylphosphinic acid and analogs thereof for treating diseases or disorders such as mild cognitive impairment, cognitive impairment associated with Alzheimer's disease Alzheimer's disease, depression, anxiety, and epilepsy are disclosed. Acyloxyalkyl carbamate prodrugs of 3-aminopropylphosphinic acid and analogs thereof, which are suitable for oral administration and sustained release oral dosage forms are also disclosed. | 11-19-2009 |
| 20090312291 | AGENT FOR PREVENTING INFECTION - An agent for preventing an infection with an influenza virus or a food or drink for preventing infection with an influenza virus is provided. It is the agent for preventing an infection with an influenza virus and a food or drink for preventing an infection with an influenza virus, which comprises a fat globule membrane component as an active ingredient. It is the agent for preventing an infection with an influenza virus and a food or drink for preventing an infection with an influenza virus, which comprises a sphigosine-containing phospholipid and/or a derivative thereof, particularly sphingomyelin, as an active ingredient. | 12-17-2009 |
| 20100022482 | aSMase inhibitors - The present invention relates to compounds of formula | 01-28-2010 |
| 20100113397 | SYNTHESIS OF OSELTAMIVIR CONTAINING PHOSPHONATE CONGENERS WITH ANTI-INFLUENZA ACTIVITY - Novel phosphonate compounds are described. The compounds have activity as neuraminidase inhibitors against wild-type and H274Y mutant of H1N1 and H5N1 viruses. The present disclosure also provides an enantioselective synthetic route to known neuraminidase inhibitors oseltamivir and the anti-flu drug Tamiflu®, as well as novel phosphonate compounds, via D-xylose. Another efficient and flexible synthesis of Tamiflu and the highly potent neuraminidase inhibitor Tamiphosphor was also achieved in 11 steps and >20% overall yields from the readily available fermentation product (1S-cis)-3-bromo-3,5-cyclohexadiene-1,2-diol. Most of the reaction intermediates were obtained as crystals without tedious purification procedures. The key transformations include an initial regio- and stereoselective bromoamidation of a bromoarene cis-dihydrodiol, as well as the final palladium-catalyzed carbonylation and phosphonylation. | 05-06-2010 |
| 20100152140 | Method of Cancer Treatment with Naphthol Analogs - In one embodiment, the present invention relates to a method of treating a cancer characterized by overexpression of cyclic adenosine monophosphate response element-binding protein (CREB) or phosphorylated CREB (p-CREB) by administering to a patient suffering from the cancer a pharmaceutically-effective amount of a composition comprising a compound selected from the group consisting of 2-{1-[3-(Amidinothio)propyl]-1H-indol-3-yl}-3-(1-methylindol-3-yl)maleimide, naphthol analogs having the structure (I), wherein R | 06-17-2010 |
| 20110124606 | SENSE-IMPROVING AGENT - Disclosed are: a sense-improving agent which comprises, as an active ingredient, a phospholipid or a sphingosine-containing phospholipid and/or a derivative thereof, particularly a sphingomyelin, and which has an effect of improving the dulling of senses at a periphery when ingested orally or directly applied to the skin; and a sense-improving food, beverage, feed or cosmetic comprising the sense-improving agent. The phospholipid to be used may be a chemically synthesized phospholipid or a naturally occurring phospholipid, preferably a phospholipid derived from an edible material such as soybean and egg yolk, particularly preferably a phospholipid derived from milk. | 05-26-2011 |
| 20110212926 | WATER-SOLUBLE ACETAMINOPHEN ANALOGS - The present invention provides water-soluble acetaminophen prodrugs and formulations which may be suitable for parenteral administration. Methods of treating a disease or condition responsive to acetaminophen (such as fever and/or pain) using the acetaminophen prodrugs, as well as kits, unit dosages, and combinations with additional pharmaceutical agent(s) are also provided. | 09-01-2011 |
| 20110212927 | CARBONATE PRODRUGS AND METHODS OF USING THE SAME - The present invention provides carbonate prodrugs which comprise a carbonic phosphoric anhydride prodrug moiety attached to the hydroxyl or carboxyl group of a parent drug moiety. The prodrugs may provide improved physicochemical properties over the parent drug. Also provided are methods of treating a disease or condition that is responsive to the parent drug using the carbonate prodrugs, as well as kits and unit dosages. | 09-01-2011 |
| 20110306578 | USE OF ORGANOPHOSPHORUS COMPOUNDS FOR THE THERAPEUTIC AND PROPHYLACTIC TREATMENT OF INFECTIONS - Use of organophosphorus compounds of general Formula (I) | 12-15-2011 |
| 20120108551 | OPHTHALMIC COMPOSITIONS - The present invention relates to compositions that may alleviate symptoms of ocular stress, as well as methods of their production, use, and storage compositions. The compositions comprise at least one ocular epithelial cell associating group and at least one hydrophilic group. In one embodiment the at least one ocular epithelial cell associating group and at least one hydrophilic group are substituents on a conjugated polyaromatic core. | 05-03-2012 |
| 20120178721 | IMMUNOMODULATORY COMPOUNDS AND TREATMENT OF DISEASES RELATED TO AN OVERPRODUCTION OF INFLAMMATORY CYTOKINES - Method of using immunomodulatory compounds for treating diseases related to an overproduction of inflammatory cytokines, including diseases selected from asthma, atopic dermatitis, allergic rhinitis, prostatitis, inflammatory bowel disease, diabetes, and rheumatoid arthritis, the compounds being of general formula (I): | 07-12-2012 |
| 20120202777 | C-Linked Hydroxamic Acid Derivatives Useful As Antibacterial Agents - The present invention is directed to a new class of hydroxamic acid derivatives of Formula I, | 08-09-2012 |
| 20120252764 | COMPOSITIONS AND METHODS FOR PROTECTING CELLS FROM TOXIC EXPOSURES - The present invention provides compositions and methods for protecting cells and tissues from damage associated with therapeutic treatments of cancers and other diseases and conditions where reactive oxygen species are produced. The present invention also provides compositions useful as research reagents. | 10-04-2012 |
| 20120270843 | PESTICIDE COMPOSITION COMPRISING PROPAMOCARB-FOSETYLATE AND AN INSECTICIDALLY ACTIVE SUBSTANCE - The present invention relates to a pesticide composition intended for protecting plants, crops or seeds against phyto-pathogenic fungi or damaging insects, and the corresponding methods of treatment using the said composition. More precisely, the subject of the present invention is a pesticide composition based on propamocarb-fosetylate, an insecticide active substance and optionally a further fungicide active substance. | 10-25-2012 |
| 20130065861 | COMPOUNDS (CYSTEIN BASED LIPOPEPTIDES) AND COMPOSITIONS AS TLR2 AGONISTS USED FOR TREATING INFECTIONS, INFLAMMATIONS, RESPIRATORY DISEASES ETC. - The invention provides a novel class of compounds viz. generally lipopeptides like Pam3CSK4, immunogenic compositions and pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with Toll-Like Receptors 2. In one aspect, the compounds are useful as adjuvants for enhancing the effectiveness a vaccine. | 03-14-2013 |
| 20130102570 | PROPHYLACTIC AGENT OR THERAPEUTIC AGENT FOR DIABETES OR OBESITY - A medicament having an excellent CaSR agonist action which enables the prevention or treatment of diabetes or obesity is provided by a composition comprising the compound represented by general formula (I) as defined, or a salt thereof. | 04-25-2013 |
| 20130178446 | METHOD FOR DECREASING SEBUM PRODUCTION - The present invention is directed to the topical application of the malonamide ACAT inhibitors described by Formula I. Other aspects of the invention are directed to topical formulations of these diamides, their use to treat sebaceous gland disorders and their use to alleviate oily skin. | 07-11-2013 |
| 20140107079 | Beta-hydroxy-gamma-aminophosphonates for Treating Immune Disorders - The present disclosure provides methods of treating, ameliorating, or preventing immune disorders, allergic disorders, or inflammatory disorders, or combinations thereof, or providing hepatoprotection in subject. In one aspect, the method comprises administering to a subject a therapeutically effective amount of a β-hydroxy-γ-aminophosphonate or β-amino-γ-aminophosphonate. | 04-17-2014 |
| 20140235592 | SUBSTITUTED 6-METHOXY-4-AMINO-N-PHENYL-2-NAPHTAMIDES AS SPHINGOSINE RECEPTOR MODULATORS - The present invention relates to substituted 6-methoxy-4-amino-N-phenyl-2-naphtamides derivatives, processes for preparing them, pharmaceutical compositions to containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors. | 08-21-2014 |
| 20140303122 | CASR AGONISTS - By searching various kinds of compounds having CaSR agonistic activity, the present invention provides CaSR agonistic agents, pharmaceutical compositions, preventive or therapeutic agents for diarrhea and kokumi-imparting agents each of which comprise the compound. More specifically, the present invention provides CaSR agonistic agents, pharmaceutical compositions, preventive or therapeutic agents for diarrhea and kokumi-imparting agents each of which comprise a glutamic acid derivative having CaSR agonistic activity or pharmaceutically acceptable salts thereof. | 10-09-2014 |
| 20140309195 | SMALL MOLECULES THAT PROMOTE SKIN REGENERATION - Provided herein are small molecules for the induction of fibroblast proliferation and increased secretion or production of proteins. The small molecules described herein can be used for the promotion of skin regeneration. Also provided herein are methods for promoting skin regeneration and wound healing. | 10-16-2014 |
| 20140364398 | C-Linked Hydroxamic Acid Derivatives Useful As Antibacterial Agents - The present invention is directed to a new class of hydroxamic acid derivatives, their use as LpxC inhibitors, and more specifically their use to treat bacterial infections. | 12-11-2014 |
| 20140378418 | COMPOUNDS FOR INHIBITING 1-DEOXY-D-XYLULOSE-5-PHOSPHATE REDUCTOISOMERASE - In particular, the compound is effective to inhibit Dxr in | 12-25-2014 |
| 20150133405 | Methods - The present invention relates to the use of selective aquaporin inhibitors, e.g., of aquaporin-4 or aquaporin-2, e.g., certain phenylbenzamide compounds, for the prophylaxis, treatment and control of aquaporin-mediated conditions, e.g., diseases of water imbalance, for example edema (particularly edema of the brain and spinal cord, e.g., following trauma or ischemic stroke, as well as the edema associated with glioma, meningitis, acute mountain sickness, epileptic seizures, infections, metabolic disorders, hypoxia, water intoxication, hepatic failure, hepatic encephalopathy, diabetic ketoacidosis, abscess, eclampsia, Creutzfeldt-Jakob disease, and lupus cerebritis, as well as edema consequent to microgravity and/or radiation exposure, as well as edema consequent to invasive central nervous system procedures, e.g., neurosurgery, endovascular clot removal, spinal tap, aneurysm repair, or deep brain stimulation, as well as retinal edema), as well as hyponatremia and excess fluid retention, and diseases such as epilepsy, retinal ischemia and other diseases of the eye associated with abnormalities in intraocular pressure and/or tissue hydration, myocardial ischemia, myocardial ischemia/reperfusion injury, myocardial infarction, myocardial hypoxia, congestive heart failure, sepsis, and neuromyelitis optica, as well as migraines, as well as to novel assays for identifying aquaporin inhibitors. | 05-14-2015 |
| 20150299230 | Novel Prodrugs And Methods Of Use Thereof - The invention relates to compounds of use as targeted cytotoxic agents and methods of use thereof. In particular, the invention relates to prodrugs that are substantially resistant to human AKR1C3 enzyme metabolism, methods of cell ablation using said compounds and methods of treatment of cancer and other hyperproliferative disorders using said compounds. | 10-22-2015 |
| 20150313853 | ANTI-HIV COMPOUND AND PREPARATION METHOD AND USE THEREOF - The present invention relates to the technical field of chemically synthesized drugs, in particular to an anti-HIV drug or prodrug and preparation method and uses thereof. The compound or prodrug compound of the present invention has a structural formula as represented by formula I. The compounds have anti-HIV-1 and anti-HIV-2 virus activity, and have a C8166 therapeutic index as high as 2081.59 and an H9 therapeutic index as high as 303.03. Furthermore, the compounds have high solubility up to 1290-2845.5 μg/ml in an aqueous solution, and can be formulated into an oral formulation. | 11-05-2015 |
| 20150342967 | METHODS - The present invention relates to the use of selective aquaporin inhibitors, e.g., of aquaporin-4 or aquaporin-2, e.g., certain phenylbenzamide compounds, for the prophylaxis, treatment and control of aquaporin-mediated conditions, e.g., diseases of water imbalance, for example edema (particularly edema of the brain and spinal cord, e.g., following trauma or ischemic stroke, as well as the edema associated with glioma, meningitis, acute mountain sickness, epileptic seizures, infections, metabolic disorders, hypoxia, water intoxication, hepatic failure, hepatic encephalopathy, diabetic ketoacidosis, abscess, eclampsia, Creutzfeldt-Jakob disease, and lupus cerebritis, as well as edema consequent to microgravity and/or radiation exposure, as well as edema consequent to invasive central nervous system procedures, e.g., neurosurgery, endovascular clot removal, spinal tap, aneurysm repair, or deep brain stimulation, as well as retinal edema), as well as hyponatremia and excess fluid retention, and diseases such as epilepsy, retinal ischemia and other diseases of the eye associated with abnormalities in intraocular pressure and/or tissue hydration, myocardial ischemia, myocardial ischemia/reperfusion injury, myocardial infarction, myocardial hypoxia, congestive heart failure, sepsis, and neuromyelitis optica, as well as migraines, as well as to novel assays for identifying aquaporin inhibitors. | 12-03-2015 |
| 20160095318 | ANTIMICROBIAL COMPOSITION - An antimicrobial composition includes benzalkonium chloride in an amount of 0.06% w/w to 0.19% w/w and cocamidopropyl PG-dimonium chloride phosphate in an amount of 0.6% w/w to 1.9% w/w. The composition also includes propylene glycol in an amount of 0.4% w/w to 1.2% w/w and triethylene glycol in an amount of 0.1% w/w to 0.3% w/w. A polysorbate is included in an amount of 0.02% w/w to 0.08% w/w and water in an amount of 96.0% w/w to 99.0% w/w. | 04-07-2016 |
| 20160159851 | INHIBITORS OF THE FARNESOID X RECEPTOR AND USES IN MEDICINE - Disclosed are inhibitors of the farnesoid X receptor, for example of formula (I), wherein R | 06-09-2016 |
| 20220133753 | COMPOSITIONS AND METHODS USEFUL FOR TREATING DISEASES CHARACTERIZED BY INSUFFICIENT PANTOTHENATE KINASE ACTIVITY - Methods and pharmaceutical compositions for use in treating diseases associated with insufficient activity of the pantothenate kinase enzyme (e.g., CASTOR diseases) are disclosed. The methods and compositions involve an effective amount of an active derivative of 4′-phosphopantetheine. | 05-05-2022 |
