| Entries |
| Document | Title | Date |
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| 20090054501 | AZOLE COMPOUNDS USED AS TUBERCULOSTATIC AND LEISHMANICIDE AGENTS - This invention refers to new 1,2,3-triazole and imidazole compounds included in the families of compounds represented by general formula VIII. | 02-26-2009 |
| 20090069390 | DEUTERIUM-ENRICHED RUFINAMIDE - The present application describes deuterium-enriched rufinamide, pharmaceutically acceptable salt forms thereof, and methods of treating using the same. | 03-12-2009 |
| 20090105313 | Preventive or therapeutic agent for keratoconjunctival disorder - An object of the present invention is to provide a new medicinal use of 2-phenyl-1,2-benzisoselenazol-3(2H)-one or a salt thereof. 2-Phenyl-1,2-benzisoselenazol-3(2H)-one or a salt thereof exhibits an excellent prevention and improvement effect in corneal disorder models, and is therefore useful as a preventive or therapeutic agent for a keratoconjunctival disorder such as dry eye, superficial punctate keratopathy, corneal epithelial defects, corneal erosion, corneal ulcer, conjunctival epithelial defects, keratoconjunctivitis sicca, superior limbic keratoconjunctivitis, filamentary keratoconjunctivitis, keratitis or conjunctivitis. | 04-23-2009 |
| 20090105314 | Pharmaceutical Agent - The present invention provides an agent for the prophylaxis or treatment of complications after coronary-artery bypass surgery or cardiac diseases, autoimmune diseases, central nervous system diseases, inflammatory diseases, sepsis, severe sepsis or septic shock in a patient who undergoes coronary-artery bypass surgery, which comprises a compound represented by the formula (I): | 04-23-2009 |
| 20090163559 | Estrogen receptor modulators - The present invention relates to compounds and derivatives thereof, their synthesis, and their use as estrogen receptor modulators. The compounds of the instant invention are ligands for estrogen receptors and as such may be useful for treatment or prevention of a variety of conditions related to estrogen functioning including: bone loss, bone fractures, osteoporosis, metastatic bone disease, Paget's disease, periodontal disease, cartilage degeneration, endometriosis, uterine fibroid disease, hot flashes, increased levels of LDL cholesterol, cardiovascular disease, impairment of cognitive functioning, age-related mild cognitive impairment, cerebral degenerative disorders, restenosis, gynecomastia, vascular smooth muscle cell proliferation, obesity, incontinence, inflammation, inflammatory bowel disease, irritable bowel syndrome, sexual dysfunction, hypertension, retinal degeneration and cancer, in particular of the breast, uterus and prostate. | 06-25-2009 |
| 20090239913 | Process for the treatment and prevention of diseases caused by fungi - The subject invention is directed to the treatment of infections caused by fungi which are resistant to standard antifungal drugs such as fluconazole. The treatment method involves administering to the sufferer an effective amount of an agent that suppresses the activity of the fungal (H+)-ATPase pump (Pma1p). Such agents may take the form of: a) 2-phenyl-1,2-benzisoselenazol-3(2H)-one, commonly referred to as ebselen and depicted by Formula I, or b) 2-phenyl-1,2-benzisoselenazol-3(2H)-one 1-oxide, commonly referred to as ebselen se-oxide and depicted by Formula II, or pharmaceutically acceptable salts thereof. Opportunistic fungal infections include those which are systemic and those which are superficial and are caused by species of fungi belonging to the genus | 09-24-2009 |
| 20090253756 | Indole Amide Derivatives as EP4 Receptor Antagonists - The invention is directed to indole amide derivatives as EP4 receptor antagonists useful for the treatment of EP4 mediated diseases or conditions, such as acute and chronic pain, osteoarthritis, rheumatoid arthritis and cancer. Pharmaceutical compositions and methods of use are also included. | 10-08-2009 |
| 20090275619 | Amide Substituted Indazole and Benzotriazole Derivatives as Poly(ADP-Ribose)Polymerase (PARP) Inhibitors - The present invention relates to compounds of formula (I) and pharmaceutically acceptable salts or tautomers thereof which are inhibitors of poly (ADP-ribose) polymerase (PARP) and thus useful for the treatment of cancer, inflammatory diseases, reperfusion injuries, ischemic conditions, stroke, renal failure, cardiovascular diseases, vascular diseases other than cardiovascular diseases, diabetes, neurodegenerative diseases, retroviral infection, retinal damage or skin senescence and UV-induced skin damage, and as chemo- or radiosensitizers for cancer treatment. | 11-05-2009 |
| 20090306153 | SYNTHESIS AND USE OF NOVEL INHIBITORS AND INACTIVATORS OF PROTEIN ARGININE DEIMINASES - In one embodiment of the present disclosure, an inactivator of protein arginine deiminase 4 is disclosed. The inactivator includes: (I) and x includes F; Cl, and H, y includes OH and NH | 12-10-2009 |
| 20090326015 | COMPOUNDS WITH EMBEDDED BENZOPYRAN MOTIF FOR CORE STRUCTURES AND PREPARATION METHOD THEREOF - The present invention relates to a compound having benzopyran core, a preparation method of the derivatives by liquid phase synthesis and solid phase synthesis through diversity-oriented synthesis, and an anticancer agent comprising the compound that exhibit excellent cytotoxicity against cancer cells. | 12-31-2009 |
| 20100016381 | STABLE EMULSION COMPOSITION - The present invention provides an emulsion composition comprising (A) a compound stable in an acidic range, and (B) a buffer, wherein the pH is adjusted from about 3.7 to about 5.5. | 01-21-2010 |
| 20100029724 | SCREENING METHOD - The present invention provides a method of screening for a therapeutic drug for diabetes or a nerve system disease, including using ferrochelatase, and a ferrochelatase activator containing a compound represented by the formula: | 02-04-2010 |
| 20100029725 | RESISTANCE MANAGEMENT STRATEGIES - Insect refuge strategies are described for the management of insect resistance development. The present invention relates generally to the control of pests that cause damage to crop plants, and in particular to corn plants, by their feeding activities directed to root damage, and more particularly to the control of such plant pests by exposing target pests to seeds or mixtures of seeds having multiple different modes of action. The first one or more transgenes and the second one or more transgenes are each, respectively, insecticidal to the same target insect but have different modes of action, and bind either semi-competitively or non-competitively to different binding sites in the target pest. In addition, the treatment of such seed with a chemical or peptide-associated pesticide prior to planting the seed is also disclosed. | 02-04-2010 |
| 20100029726 | CYCLOHEXANESULFONYL DERIVATIVES AS GLYT1 INHIBITORS TO TREAT SCHIZOPHRENIA - The present invention provides compounds of formula I: | 02-04-2010 |
| 20100120873 | PROPHYLACTIC OR THERAPEUTIC AGENT FOR AGE-RELATED MACULAR DEGENERATION - An object of the present invention is to find a novel medicinal use of 2-phenyl-1,2-benzisoselenazol-3(2H)-one or a salt thereof. 2-Phenyl-1,2-benzisoselenazol-3(2H)-one or a salt thereof exhibits an excellent inhibitory effect on neovascularization in the choroid and also has a protective effect on retinal pigment epithelial cell damage, and therefore is useful as a prophylactic or therapeutic agent for age-related macular degeneration. | 05-13-2010 |
| 20100130565 | THIOAMIDE COMPOUNDS, METHOD OF MAKING AND METHOD OF USING THEREOF - The present invention relates to novel thioamide derivatives of formula (I) and formula (Ia): | 05-27-2010 |
| 20100168188 | Estrogen Receptor Modulators - The present invention relates to compounds and derivatives thereof, their synthesis, and their use as estrogen receptor modulators. The compounds of the instant invention are ligands for estrogen receptors and as such may be useful for treatment or prevention of a variety of conditions related to estrogen functioning including: bone loss, bone fractures, osteoporosis, metastatic bone disease, Paget's disease, periodontal disease, cartilage degeneration, endometriosis, uterine fibroid disease, hot flashes, increased levels of LDL cholesterol, cardiovascular disease, impairment of cognitive functioning, cerebral degenerative disorders, restenosis, gynecomastia, vascular smooth muscle cell proliferation, obesity, incontinence, inflammation, inflammatory bowel disease, sexual dysfunction, hypertension, retinal degeneration and cancer, in particular of the breast, uterus and prostate. | 07-01-2010 |
| 20100227899 | Process for the treatment of bacterial infections using 2-phenyl-1,2-benzisoselenazol-3(2H)-one 1-oxide - The subject invention demonstrates a novel antibacterial activity for 2-phenyl-1,2-benzisoselenazol-3(2H)-one 1-oxide, commonly referred to as ebselen se-oxide, and is directed to the treatment of bacterial infections by administration of an effective amount of said compound. Bacterial infections include those infections which are either systemic or superficial in nature. The treatment is intended for a variety of animals, such as premature neonates to adult humans. Administration of ebselen se-oxide to treat superficial bacterial infections may be performed by a topical application, such as via an ointment, a spray, a cream, a mouth wash, an eye drop solution, an ear drop solution, a soap, a gel, or a lotion. In addition, an antibacterial capsule can be administered orally or intravaginally. Administration of ebselen se-oxide to treat systemic bacterial infections may be performed by an intravenous route, a rectal route, an intranasal route, an oral route, an intramuscular route, or by inhalation. Administration of said compound may also be achieved via aerosol, which can be generated by a nebulizer. Ebselen se-oxide may be administered alone, or with a carrier such as dimethylsulfoxide (DMSO), an alcohol, or other suitable carrier. The effective daily amount of ebselen se-oxide is from about 1 μg/kg to 10 mg/kg of body weight. | 09-09-2010 |
| 20100240715 | Apoptosis promoters - Disclosed are compounds which inhibit the activity of anti-apoptotic protein family members, compositions containing the compounds and uses of the compounds for preparing medicaments for treating diseases during which occurs expression one or more than one of an anti-apoptotic protein family member. | 09-23-2010 |
| 20110028522 | FULLERENE THERAPIES FOR INFLAMMATION - Described herein are methods for treating inflammatory disorders. The methods comprise administering to a subject in need thereof a therapeutically effective amount of a synthetically modified fullerene. | 02-03-2011 |
| 20110034523 | CRYSTALLINE FORMS OF RUFINAMIDE - Disclosed is a crystalline form of rufinamide selected from:
| 02-10-2011 |
| 20110060017 | NOVEL 1,2,3-TRIAZOLE DERIVATIVES USEFUL AS MODULATORS OF NICOTINIC ACETYLCHOLINE RECEPTORS - This invention relates to novel 1,2,3-triazole derivatives, which are found to be modulators of the nicotinic acetyl-choline receptors. Due to their pharmacological profile, the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances. | 03-10-2011 |
| 20110118321 | CARBAMOYLBENZOTRIAZOLE DERIVATIVES AS INHIBITORS OF LIPASES AND PHOSPHOLIPASES - The invention relates to carbamoylbenzotriazole derivatives of general formula (I), which are defined as cited in the description, to their pharmaceutically applicable salts and to their use as medicaments. | 05-19-2011 |
| 20110172278 | COMPOUNDS AND METHODS FOR MODULATING G PROTEIN-COUPLED RECEPTORS - The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with or mediated by G protein-coupled receptors, in particular G protein-coupled receptor 120. | 07-14-2011 |
| 20110201656 | NOVEL DIPHENYL 1,2,3-TRIAZOLE DERIVATIVES USEFUL AS MODULATORS OF NICOTINIC ACETYLCHOLINE RECEPTORS - This invention relates to novel diphenyl 1,2,3-triazole derivatives, which are found to be modulators of the nicotinic acetylcholine receptors. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances. | 08-18-2011 |
| 20110201657 | AMIDE SUBSTITUTED INDAZOLE AND BENZOTRIAZOLE DERIVATIVES AS POLY(ADP-RIBOSE)POLYMERASE (PARP) INHIBITORS - The present invention relates to compounds of formula (I) and pharmaceutically acceptable salts or tautomers thereof which are inhibitors of poly (ADP-ribose) polymerase (PARP) and thus useful for the treatment of cancer, inflammatory diseases, reperfusion injuries, ischemic conditions, stroke, renal failure, cardiovascular diseases, vascular diseases other than cardiovascular diseases, diabetes, neurodegenerative diseases, retroviral infection, retinal damage or skin senescence and UV-induced skin damage, and as chemo- or radiosensitizers for cancer treatment. | 08-18-2011 |
| 20110230527 | CASPASE INHIBITORS AND USES THEREOF - This invention provides novel caspase inhibitors useful for prophylaxis or treatment of a number of pathologies, including, for example, Huntington's disease. In certain embodiments the inhibitors include inhibitors of casepase-3 and/or casepase-6. | 09-22-2011 |
| 20110269803 | AZOLE COMPOUNDS USED AS TUBERCULOSTATIC AND LEISHMANICIDE AGENTS - This invention refers to new 1,2,3-triazole and imidazole compounds included in the families of compounds represented by general formula VIII. | 11-03-2011 |
| 20120010254 | COMPOUNDS AND METHODS FOR TREATMENT OF INFLUENZA - The present invention provides in part a compound of Formula (I) or a pharmaceutically-acceptable salt or stereoisomer thereof: where R | 01-12-2012 |
| 20120022118 | COMPOUNDS FOR THE TREATMENT OF PROLIFERATIVE DISORDERS - The invention relates to compounds of structural formula (I): | 01-26-2012 |
| 20120041040 | FUNCTIONALIZED 4- AND 5-VINYL SUBSTITUTED REGIOISOMERS OF 1, 2, 3-TRIAZOLES VIA 1, 3-DIPOLAR CYCLOADDITION AND POLYMERS THEREOF - The present invention provides novel functionalized mixtures 4- and 5-vinyl substituted regioisomers of 1,2,3-triazoles via 1,3-dipolar cycloaddition. Functionalized alkyne moieties with a terminal alcoholic functionality are reacted with functionalized organic moieties with a terminal leaving group and an azide to provide an alcoholic functionalized mixture of 4- and 5-substituted regioisomers of 1,2,3-triazole moieties. The mixture may be converted to a wide variety of useful functionalized mixtures of 4- and 5-vinyl substituted regioisomers of 1,2,3-triazole moieties, which in turn can be converted to a wide variety of useful polymers The novel alcoholic functionalized mixtures of 4- and 5-substituted regioisomers can be separated by chromatography to provide the purified 4- and 5-alcoholic functionalized substituted 1,2,3-triazole moieties. The novel compounds of the invention can be employed in a wide variety of compositions (Formulae (I), (II)); wherein R | 02-16-2012 |
| 20120149741 | TREATMENT OF DUCHENNE MUSCULAR DYSTROPHY - There are provided compounds of Formula (I) wherein three of A | 06-14-2012 |
| 20120232119 | METHOD FOR TREATING A KERATOCONJUNCTIVAL DISORDER - A method for treating a keratoconjunctival disorder, wherein the keratoconjunctival disorder comprises at least one disorder selected from the group consisting of a superficial punctate keratopathy, a corneal epithelial defect, corneal erosion, a corneal ulcer, a conjunctival epithelial defect, keratoconjunctivitis sicca, superior limbic keratoconjunctivitis, filamentary keratoconjunctivitis, keratitis and conjunctivitis, and wherein the method comprises orally administering from 3 mg/kg to 30 mg/kg per day of 2-phenyl-1,2-benzisoselenazol-3(2H)-one or a salt thereof to a patient in need thereof. | 09-13-2012 |
| 20120322837 | AMIDE COMPOUND AND MEDICINAL USE THEREOF - A compound of formula [I-W]: | 12-20-2012 |
| 20130045998 | PROCESS FOR PREPARING RUFINAMIDE INTERMEDIATE - The present invention refers to an improved method for the preparation of compound 1-(2,6-difluorobenzyl)-1H-1,2,3-triazole-4-carboxylic acid substantially free of its 3H-I isomer. The invention also refers to the use of said intermediate for the preparation of Rufinamide and for obtaining a new polymorphic form of Rufinamide, designed as Form R-5. The invention also refers to said new polymorph of Rufinamide, and to the composition containing it and its use as medicament. The new polymorph of Rufinamide shows good stability and appropriate physico-chemical properties for its manipulation on industrial scale. Polymorph Form R-5 will be suitable to use as pharmaceutical for the treatment of convulsions, especially for the treatment of epilepsy. | 02-21-2013 |
| 20130096165 | COMPOUNDS AND METHODS FOR MODULATING G PROTEIN-COUPLED RECEPTORS - The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with or mediated by G protein-coupled receptors, in particular G protein-coupled receptor 120. | 04-18-2013 |
| 20130267568 | (1,2,3-Triazolyl)sulfonyl Derivatives - The invention relates to a compound of the formula | 10-10-2013 |
| 20130274298 | AZOLE COMPOUNDS USED AS TUBERCULOSTATIC AND LEISHMANICIDE AGENTS - This invention refers to new 1,2,3-triazole and imidazole compounds included in the families of compounds represented by general formula VIII. This invention also refers to a pharmaceutical composition comprising at least one of the azole compounds represented by the general formula VIII, to the use of such compositions and to methods of treatment or inhibition of tuberculosis and leishmaniasis. | 10-17-2013 |
| 20140011847 | CASPASE INHIBITORS AND USES THEREOF - This invention provides novel caspase inhibitors useful for prophylaxis or treatment of a number of pathologies, including, for example, Huntington's disease. In certain embodiments the inhibitors include inhibitors of casepase-3 and/or casepase-6. | 01-09-2014 |
| 20140107168 | G-QUADRUPLEX STABILISING AGENT - A compound of formula I | 04-17-2014 |
| 20140113941 | THIOLACTONE ANTIBIOTICS - This invention provides a compound having the structure | 04-24-2014 |
| 20140121248 | METALLOENZYME INHIBITOR COMPOUNDS - The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes. | 05-01-2014 |
| 20140200247 | Novel compositions and processes for preparing 5-amino or substituted amino 1,2,3-triazoles and triazoles orotate formulations - New polymorphs of 5-amino or substituted amino 1,2,3-triazole and substituted derivatives thereof, of orotates of the carboxyamidotriazoles, of formulations of the triazoles and orotic acid in the ratio of 1:1 to 1:4 (base:acid) and of safer processes of the preparation of the same are disclosed. The compounds are useful in the control and treatment of diseases including, but not limited to solid cancers, macular degeneration, retinopathy, chronic myeloid leukemia, AIDS and diseases which rely on aberrant signal transduction. The improved processes to prepare the orotate formulations use stable, efficient and safer starting azide intermediate materials in the synthesis of new polymorphs of carboxyamidotriazole. | 07-17-2014 |
| 20140296306 | AMIDE COMPOUND AND MEDICINAL USE THEREOF - A compound of formula [I-W]: | 10-02-2014 |
| 20140315961 | ARGININE METHYLTRANSFERASE INHIBITORS AND USES THEREOF - Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting arginine methyltransferase activity. Methods of using the compounds for treating arginine methyltransferase-mediated disorders are also described. | 10-23-2014 |
| 20150018395 | CHIMERIC SMALL MOLECULES FOR THE RECRUITMENT OF ANTIBODIES TO CANCER CELLS - The present invention relates to chimeric chemical compounds which are used to recruit antibodies to cancer cells, in particular, prostate cancer cells or metastasized prostate cancer cells. The compounds according to the present invention comprise an antibody binding terminus (ABT) moiety covalently bonded to a cell binding terminus (CBT) through a linker and optionally, a connector molecule. | 01-15-2015 |
| 20150133511 | N-ALKYLTRIAZOLE COMPOUNDS AS LPAR ANTAGONISTS - Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of inflammatory diseases and disorders such as, for example, pulmonary fibrosis . . . . | 05-14-2015 |
| 20150133512 | N-ARYLTRIAZOLE COMPOUNDS AS LPAR ANTAGONISTS - Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of inflammatory diseases and disorders such as, for example, pulmonary fibrosis. | 05-14-2015 |
| 20150352079 | SELECTIVE HISTONE DEACETYLASE 8 INHIBITORS - Described herein are compounds and pharmaceutical compositions containing such compounds, which inhibit the activity of histone deacetylase 8 (HDAC8). Also described herein are methods of using such HDAC8 inhibitors, alone and in combination with other compounds, for treating diseases or conditions that benefit from inhibition of HDAC8 activity | 12-10-2015 |
| 20190142799 | ASH1L INHIBITORS AND METHODS OF TREATMENT THEREWITH | 05-16-2019 |
