Entries |
Document | Title | Date |
20080234258 | Dihydroxyanthraquinones and Their Use - A compound of formula (1) | 09-25-2008 |
20080261967 | Modulators of Central Nervous System Neurotransmitters - Disclosed are agents having pharmacological activity against cellular receptors and intracellular signaling, particularly receptors and signaling pathways of central nervous system (CNS) neurotransmitters. Also disclosed are related methods and compositions for the treatment or prevention of diseases or disorders using the agents. | 10-23-2008 |
20080287430 | Furan Compounds Useful As Ep1 Receptor Antagonists - Compounds of formula (I) or a pharmaceutically acceptable derivative thereof | 11-20-2008 |
20080293711 | Chemokine receptor modulators - The invention provides compounds of Formula (I) | 11-27-2008 |
20090012075 | Fluorinated Arylamide Derivatives - The present invention relates to a novel class of fluorinated arylamide derivatives. The instant compounds can be used to treat cancer. The fluorinated arylamide derivatives can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases. The present invention further provides pharmaceutical compositions comprising the hydroxamic acid derivatives and safe dosing regimens of these pharmaceutical compositions, which are easy to follow, and which result in a therapeutically effective amount of the hydroxamic acid derivatives in vivo. | 01-08-2009 |
20090036439 | 3-ARYL-4-HYDROXYFURANONE COMPOUNDS AND THE HUMAN AND ANIMAL HEALTH USE THEREOF - The present invention provides a compound of formula I and the use thereof for the inhibition of bacterial cell wall biosynthesis and for the therapeutic treatment of bacterial infection or disease in a patient in need thereof. The present invention also provides the use of the formula I compound for the control of ecto- or endoparasites in homeothermic animals. | 02-05-2009 |
20090054427 | AMINOBENZYL-SUBSTITUTED CYCLIC SULFONES USEFUL AS BACE INHIBITORS - The invention relates to novel heterocyclic compounds of the formula | 02-26-2009 |
20090105239 | 2-PYRIDINE DERIVATIVES AS INHIBITORS OF NEUTROPHILE ELASTASE - The invention provides compounds of formula wherein R | 04-23-2009 |
20090105240 | Methods for treating leukemia and myelodysplastic syndrome, and methods for identifying agents for treating same - The present disclosure relates to methods for treating leukemia, pre-leukemic conditions, as well as myelodysplastic syndrome and acute myelogenous leukemia. The present disclosure further relates to compounds that can be used for treating leukemia, pre-leukemic conditions, as well as myelodysplastic syndrome and acute myelogenous leukemia. The present disclosure also relates to methods for identifying compounds that can be used for treating leukemia, pre-leukemic conditions, as well as myelodysplastic syndrome. | 04-23-2009 |
20090118269 | Methods for Treating Spinal Muscular Atrophy Using Tetracycline Compounds - Methods for using tetracycline compounds for the treatment of spinal muscular atrophy are described. | 05-07-2009 |
20090131421 | Compounds for proteasome enzyme inhibition - Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Ntn) hydrolases. The activities of those Ntn having multiple activities can be differentially inhibited by the compounds described. For example, the chymotrypsin-like activity of the 20S proteasome may be selectively inhibited with the inventive compounds. The peptide-based compounds include an epoxide or aziridine, and functionalization at the N-terminus. Among other therapeutic utilities, the peptide-based compounds are expected to display anti-inflammatory properties and inhibition of cell proliferation. | 05-21-2009 |
20090163487 | N-HYDROXYLSULFONAMIDE DERIVATIVES AS NEW PHYSIOLOGICALLY USEFUL NITROXYL DONORS - The invention relates to N-hydroxylsulfonamide derivatives that donate nitroxyl (HNO) under physiological conditions and are useful in treating and/or preventing the onset and/or development of diseases or conditions that are responsive to nitroxyl therapy, including heart failure and ischemia/reperfusion injury. Novel N-hydroxylsulfonamide derivatives release NHO at a controlled rate under physiological conditions, and the rate of HNO release is modulated by varying the nature and location of functional groups on the N-hydroxylsulfonamide derivatives. | 06-25-2009 |
20090186884 | Diaminopropanol Renin Inhibitors - Described are diaminopropanols of which are orally active and bind to renin to inhibit its activity. They are useful in the treatment or amelioration of diseases associated with elevated levels of renin activity or in the treatment of aspartic protease mediated disorders. Also described is a method for the use of the diaminopropanols in ameliorating or treating renin related disorders in a subject in need thereof. | 07-23-2009 |
20090186885 | THERAPEUTIC COMPOUNDS - Disclosed herein is a compound according to one of the formulas | 07-23-2009 |
20090192151 | THERAPEUTIC AMIDES AND RELATED COMPOUNDS - Disclosed herein are compounds useful in treating glaucoma, inflammatory bowel disease, the stimulation of hair growth, and the stimulation of the conversion of vellus hair to terminal hair. The compounds themselves are herein. | 07-30-2009 |
20090239858 | THERAPEUTIC AMIDES - Compounds comprising | 09-24-2009 |
20090270385 | SUBSTITUTED ARYLCYCLOPENTENES AS THERAPEUTIC AGENTS - Compounds comprising | 10-29-2009 |
20090270386 | THERAPEUTIC COMPOUNDS - Compounds comprising | 10-29-2009 |
20090270387 | SUBSTITUTED ARYLCYCLOPENTENES AS THERAPEUTIC AGENTS - Compounds comprising | 10-29-2009 |
20090275575 | BENZOPHENONE DERIVATIVES USEFUL FOR INHIBITING FORMATION OF MICROTUBULE - Disclosed herein are novel benzophenone derivatives represented by formula I, a pharmaceutically acceptable salt thereof, a hydrate thereof or a solvate thereof, a pharmacological composition containing the same, and a use of the composition as therapeutic drugs. The benzophenone derivatives have an inhibition activity of microtubule formation and can be used to treat a normal proliferative state of a malignant tumor by killing the actively proliferating cells. | 11-05-2009 |
20090312316 | NOVEL COMPOUNDS - The present invention relates to derivatives of borrelidin that are useful in medicine, e.g. in the treatment of cancer or B-cell malignancies, or other diseases in which angiogenesis contributes to the pathology including ophthalmic disorders such as diabetic retinopathy as well as age related macular degeneration (AMD), corneal neovascularisation and retinopathy or prematurity. The present invention also provides methods for the production of these compounds and their use in medicine, in particular in the treatment and/or prophylaxis of cancer or B-cell malignancies and other diseases in which angiogenesis is implicated in the pathogenic process. | 12-17-2009 |
20100022527 | BIPHENYL SUBSTITUTED SPIROTETRONIC ACIDS AND THEIR USE FOR THE TREATMENT OF RETROVIRAL DISEASES - The present invention relates to novel substituted spirotetronic acids (I) in which R | 01-28-2010 |
20100041649 | INHIBITORS OF PAPILLOMA VIRUS - A compound of formula (I) or its enantiomers or diastereoisomers thereof: | 02-18-2010 |
20100105673 | SUBSTITUTED AMINOFURANONES AND THEIR USE - The present invention relates to novel substituted aminofurans, to methods for their preparation, to their use in the treatment and/or prophylaxis of diseases as well as their use in the manufacture of medical products for the treatment and/or prophylaxis of diseases, in particular retroviral disorders, in humans and/or animals. | 04-29-2010 |
20100125071 | CXC-CHEMOKINE RECEPTOR LIGANDS - The present invention relates to compounds of formula (I) with the substituents as defined herein, and uses thereof. | 05-20-2010 |
20100137298 | Biaryl Sulfonamides and Methods for Using Same - The present invention relates to biaryl sulfonamides and their use as, for example, metalloproteinase inhibitors. | 06-03-2010 |
20100311738 | Pharmaceutical Composition For The Parenteral Administration Of Ultrashort-Effective Beta-Adrenoreceptor Antagonists - The present invention relates to a pharmaceutical composition in the form of a storage-stable solution for the parenteral administration of ultrashort-effective β-adrenoreceptor antagonists, comprising a) an ultrashort-effective β-adrenoreceptor antagonist and/or a pharmaceutically acceptable salt thereof, b) water, and c) a cyclodextrin and/or a functional cyclodextrin derivative. The composition according to the invention has high stability, even without the presence of additional adjuvants. | 12-09-2010 |
20110021517 | ANTITUMOR COMBINATION COMPRISING A MORPHOLINYL ANTHRACYCLINE DERIVATIVE AND DEMETHYLATING AGENTS - The present invention provides a combination of a morpholinyl anthracycline derivative, in particular a methoxy morpholino doxorubicin derivative, or a pharmaceutically acceptable salt thereof, and a demethylating agent, having an antineo-plastic effect. Also provided is the use of the said combinations in the treatment or prevention of metastasis, in the treatment of tumors, as well for reversing the resistance in cells resistant to such a methoxy morpholino doxorubicin derivative. | 01-27-2011 |
20110028469 | Thiphene-2-Carboxamide Derivatives As Modulators of CCR9 Receptor - Provided are compounds of Formula (I) or of Formula (II) that are modulators of CCR9 receptor activity, compositions containing the compounds and methods of use of the compounds and compositions. In certain embodiments, provided are methods for treating or amelioratin diseases associated with modulation of CCR9 receptor activity. | 02-03-2011 |
20110046129 | 2-Phenylethylamino Derivatives as Calcium and/or Sodium Channel Modulators - 2-Phenylethylamino substituted carboxamide derivatives and their use as sodium and/or calcium channel modulators useful in preventing, alleviating and curing a wide range of pathologies are presented. | 02-24-2011 |
20110092496 | THIOPHENE COMPOUNDS AND THROMBOPOIETIN RECEPTOR ACTIVATORS - A compound represented by the formula (I) (wherein R | 04-21-2011 |
20110152255 | THERAPEUTIC COMPOUNDS - Compounds comprising formula (I) or a pharmaceutically acceptable salt thereof, are disclosed, wherein J, B, Y, and A are as described in claims | 06-23-2011 |
20110190286 | THERAPEUTICALLY ACTIVE CYCLOPENTANES - Disclosed herein are compounds having a formula: | 08-04-2011 |
20110212954 | ALPHA-LIPOIC ACID DERIVATIVES AND THEIR USE IN DRUG PREPARATION - The present invention concerns an enantiomer R of a compound of Formula (I), wherein X is —NH—R | 09-01-2011 |
20110224202 | PDE10 INHIBITORS AND RELATED COMPOSITIONS AND METHODS - Compounds that inhibit PDE10 are disclosed that have utility in the treatment of a variety of conditions, including (but not limited to) psychotic, anxiety, movement disorders and/or neurological disorders such as Parkinson's disease, Huntington's disease, Alzheimer's disease, encephalitis, phobias, epilepsy, aphasia, Bell's palsy, cerebral palsy, sleep disorders, pain, Tourette's syndrome, schizophrenia, delusional disorders, drug-induced psychosis and panic and obsessive-compulsive disorders. Pharmaceutically acceptable salts, stereoisomers, solvates and prodrugs of the compounds are also provided. Also disclosed are compositions containing a compound in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for inhibiting PDE10 in a warm-blooded animal in need of the same. | 09-15-2011 |
20110245243 | COMPOUNDS AND COMPOSITIONS AS CATHEPSIN S INHIBITORS - The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of Cathepsin S. | 10-06-2011 |
20110275625 | Heteroaryl Diamide Compounds Useful as MMP-13 Inhibitors - Disclosed are compounds and compositions of the formula (I) as described herein which are inhibitors of MMP-13. Also disclosed are methods of using and making compounds of the formula (I). | 11-10-2011 |
20110275626 | FORMULATION FOR ORAL TRANSMUCOSAL ADMINISTRATION OF ANALGESIC AND/OR ANTISPASMODIC MOLECULES - A formulation for oral transmucosal administration of at least one active principle with antispasmodic and/or analgesic effect, including the active principle in base form and/or in salt form, an aqueous alcohol solution titrating at least 35° alcohol by weight, the active principle being present in a state of stable and complete dissolution in the aqueous alcohol solution. Also, a method of preparing this formulation and its use for treating spastic crises. | 11-10-2011 |
20110301158 | ARYL CARBONYL DERIVATIVES AS THERAPEUTIC AGENTS - This invention relates to aryl carbonyl derivatives which are activators of glucokinase which may be useful for the management, treatment, control, or adjunct treatment of diseases, where increasing glucokinase activity is beneficial. | 12-08-2011 |
20120022059 | SUBSTITUTED FURANCARBOXAMIDES, AND USE THEREOF - The present invention relates to novel substituted furancarboxamides, methods for their production, their use for the treatment and/or prevention of diseases, as well as their use for the production of medicaments for the treatment and/or prophylaxis of diseases, especially retroviral diseases, in humans and/or animals. | 01-26-2012 |
20120088762 | COMPOUNDS FOR ENZYME INHIBITION - One aspect of the invention relates to inhibitors that preferentially inhibit immunoproteasome activity over constitutive proteasome activity. In certain embodiments, the invention relates to the treatment of immune related diseases, comprising administering a compound of the invention. In certain embodiments, the invention relates to the treatment of cancer, comprising administering a compound of the invention. | 04-12-2012 |
20120184545 | HEART-SLOWING DRUG CONTAINING SHORT-ACTING BETA-BLOCKER AS TEH ACTIVE INGREDIENT - The present invention relates to an agent which slows down the heart rate which has an excellent controlling ability in diagnostic imaging comprising a short-acting β-blocker (e.g. landiolol hydrochloride or esmolol hydrochloride). The short-acting β-blocker has a property of slowing down the heart rate and it can temporarily suppress the tachycardia at diagnosis. According to the dose and the method of administration, it can control the period for the heart rate adjustment. Also, the present invention relates to a diagnostic imaging auxiliary comprising a short-acting β-blocker as active ingredient. | 07-19-2012 |
20120208807 | TOFA ANALOGS USEFUL IN TREATING DERMATOLOGICAL DISORDERS OR CONDITIONS - This invention is directed to analogs of 5-(tetradecyloxy)-2-furancarboxylic acid (TOFA) and their use in the treatment of dermatological disorders or conditions characterized by sebaceous gland hyperactivity, such as acne and oily skin, and other dermatological disorders and conditions. This invention is also directed to pharmaceutical compositions comprising analogs of TOFA and a pharmaceutically acceptable excipient for dermatological or oral administration. Formula (I) | 08-16-2012 |
20120258965 | N-HYDROXYLSULFONAMIDE DERIVATIVES AS NEW PHYSIOLOGICALLY USEFUL NITROXYL DONORS - The invention relates to N-hydroxylsulfonamide derivatives that donate nitroxyl (HNO) under physiological conditions and are useful in treating and/or preventing the onset and/or development of diseases or conditions that are responsive to nitroxyl therapy, including heart failure and ischemia/reperfusion injury. Novel N-hydroxylsulfonamide derivatives release NHO at a controlled rate under physiological conditions, and the rate of HNO release is modulated by varying the nature and location of functional groups on the N-hydroxylsulfonamide derivatives. | 10-11-2012 |
20120302561 | Compounds, Formulations, and Methods of Protein Kinase C Inhibition - The invention provides a method of inhibiting atypical protein kinase C (aPKC) comprising contacting an aPKC with a compound having a structure selected from the group consisting of structural formulas (I) to (IX). The invention further provides a method of inhibiting or reducing vascular permeability. The method comprising administering to a subject a composition comprising an amount of a compound having a structure selected from the group consisting of structural formulas (I) to (IX) effective to inhibit or reduce vascular permeability. A method of treating or preventing a disease or disorder characterized by abnormal vascular permeability, a method of inhibiting angiogenesis, a method of inhibiting cancer cell proliferation, a formulation, and a method of preparing a formulation also are provided. | 11-29-2012 |
20130040945 | CERTAIN CHEMICAL ENTITIES, COMPOSITIONS, AND METHODS - Chemical entities that are arctigenin derivatives, pharmaceutical compositions and methods of treatment of cancer are described. | 02-14-2013 |
20130123253 | MODULATORS OF CENTRAL NERVOUS SYSTEM NEUROTRANSMITTERS - Disclosed are agents having pharmacological activity against cellular receptors and intracellular signaling, particularly receptors and signaling pathways of central nervous system (CNS) neurotransmitters. Also disclosed are related methods and compositions for the treatment or prevention of diseases or disorders using the agents. | 05-16-2013 |
20130158022 | Acrylamide Compounds And Use Thereof For Inhibiting Apoptosis - The present invention relates to a compound of Formula I, or an isomer, pharmaceutically acceptable salt and solvate of the compound, and to a composition comprising the compound of Formula I, or the isomer, pharmaceutically acceptable salt and solvate thereof, and a pharmaceutically acceptable carrier, excipient or diluents. The present invention also relates to use of the compound of Formula I, or the isomer, pharmaceutically acceptable salt and solvate thereof for combating apoptosis, preventing or treating a disease or disorder associated with apoptosis; and especially use for protecting cardiomyocyte, and for preventing or treating a disease or disorder associated with cardiomyocyte apoptosis. | 06-20-2013 |
20130296315 | Use of Dithiine Derivatives in Crop Protection and the Protection of Materials - The present invention relates to the use of new and known dithiine derivatives for controlling unwanted microorganisms, more particularly phytopathogenic fungi, in crop protection, in the household and hygiene sector and in the protection of materials, and also to new dithiine derivatives, to processes for preparing them, to their use, and to crop protection compositions comprising these new dithiine derivatives. | 11-07-2013 |
20130331387 | HETEROARYL DERIVATIVES AS ALPHA7 NACHR MODULATORS - Disclosed is a compound of formula (I), wherein Z, m and R | 12-12-2013 |
20140135321 | SMALL MOLECULE INHIBITORS OF HIV PROTEASES - Described herein are compounds, compositions, and methods for treating HIV and related diseases. | 05-15-2014 |
20140194416 | N-HYDROXYLSULFONAMIDE DERIVATIVES AS NEW PHYSIOLOGICALLY USEFUL NITROXYL DONORS - The invention relates to N-hydroxylsulfonamide derivatives that donate nitroxyl (HNO) under physiological conditions and are useful in treating and/or preventing the onset and/or development of diseases or conditions that are responsive to nitroxyl therapy, including heart failure and ischemia/reperfusion injury. Novel N-hydroxylsulfonamide derivatives release NHO at a controlled rate under physiological conditions, and the rate of HNO release is modulated by varying the nature and location of functional groups on the N-hydroxylsulfonamide derivatives. | 07-10-2014 |
20140343049 | DIHYDROFURAN DERIVATIVES AS INSECTICIDAL COMPOUNDS - The present invention relates to compounds of formula (IA) wherein Q | 11-20-2014 |
20150025068 | BISARYLSULFONAMIDES USEFUL IN THE TREATMENT OF INFLAMMATION AND CANCER - A compound of formula (I), useful for the treatment of cancer, inflammation and inflammatory disorders, and a pharmaceutical composition containing the compound. | 01-22-2015 |
20150025069 | TOFA ANALOGS USEFUL IN TREATING DERMATOLOGICAL DISORDERS OR CONDITIONS - This invention is directed to analogs of 5-(tetradecyloxy)-2-furancarboxylic acid (TOFA) and their use in the treatment of dermatological disorders or conditions characterized by sebaceous gland hyperactivity, such as acne and oily skin, and other dermatological disorders and conditions. This invention is also directed to pharmaceutical compositions comprising analogs of TOFA and a pharmaceutically acceptable excipient for dermatological or oral administration. | 01-22-2015 |
20150307512 | SYNTHESIS OF FR901464 AND ANALOGS WITH ANTITUMOR ACTIVITY - The present invention provides novel analogs of FR901464, as well as an improved methodology for preparing FR901464 and its analogs. These compounds display an anti-cancer activity and are candidates for therapies against a number of disease states associated with dysfunctional RNA splicing. | 10-29-2015 |
20150336880 | N-HYDROXYLSULFONAMIDE DERIVATIVES AS NEW PHYSIOLOGICALLY USEFUL NITROXYL DONORS - The invention relates to N-hydroxylsulfonamide derivatives that donate nitroxyl (HNO) under physiological conditions and are useful in treating and/or preventing the onset and/or development of diseases or conditions that are responsive to nitroxyl therapy, including heart failure and ischemia/reperfusion injury. Novel N-hydroxylsulfonamide derivatives release NHO at a controlled rate under physiological conditions, and the rate of HNO release is modulated by varying the nature and location of functional groups on the N-hydroxylsulfonamide derivatives. | 11-26-2015 |
20160038445 | ACRYLAMIDE COMPOUNDS AND USE THEREOF FOR INHIBITING APOPTOSIS - The present invention relates to a compound of Formula I, or an isomer, pharmaceutically acceptable salt and solvate of the compound, and to a composition comprising the compound of Formula I, or the isomer, pharmaceutically acceptable salt and solvate thereof, and a pharmaceutically acceptable carrier, excipient or diluents. The present invention also relates to use of the compound of Formula I, or the isomer, pharmaceutically acceptable salt and solvate thereof for combating apoptosis, preventing or treating a disease or disorder associated with apoptosis; and especially use for protecting cardiomyocyte, and for preventing or treating a disease or disorder associated with cardiomyocyte apoptosis. | 02-11-2016 |
20160074411 | USE OF LANDIOLOL HYDROCHLORIDE IN THE LONG-TERM TREATMENT OF TACHYARRHYTHMIAS - The invention provides a new use of landiolol hydrochloride for persistent reduction of the heart rate during the administration period of landiolol hydrochloride in the treatment of a human suffering from tachycardia, tachyarrhythmia or elevated blood pressure, wherein landiolol hydrochloride is administered at a constant dose of more than 5 μg/kg/min, specifically of at least 10 μg/kg/min for a period of at least 2 hours and wherein the heart rate and/or blood pressure of said patient are persistently reduced during the administration period compared to the heart rate and/or blood pressure before treatment and no overshooting effect occurs after termination of said administration. | 03-17-2016 |
20190142812 | 5-SUBSTITUTED 2-(MORPHOLIN-4-YL)-1,7-NAPHTHYRIDINES | 05-16-2019 |
20190142833 | ARYLQUINAZOLINES | 05-16-2019 |