Entries |
Document | Title | Date |
20080207710 | Insulin Secretagogue Drugs - Demanded is an insulin secretagogue that alleviates side effects, such as acceleration of obesity and cells so as not to be detrimental to insulin secretion β capability. The invention provides an insulin secretagogue agent not only dependent on glucose but also responsive to elevated blood sugar levels, comprising an effective amount of a substance having the activity of PPAR δ activation. This insulin secretagogue simultaneously exerts anti-obesity activity, serum cholesterol reducing activity useful for the treatment and prevention of arteriosclerosis, etc. and insulin resistance ameliorating activity. | 08-28-2008 |
20080207711 | Method for treating an ID2-related disorder - Described herein is a method of treating an ID2-related disorder comprising administering to a patient in need thereof an ID2 inhibitor or derivative thereof. | 08-28-2008 |
20080221179 | SUBSTITUTED PHENOXY AMINOTHIAZOLONES as estrogen related receptor-alpha modulators - The present invention relates to compounds of Formula (I), | 09-11-2008 |
20080262054 | Pharmaceutical Composition Containing Thiazolidinedione Compound - [OBJECT] To provide a pharmaceutical composition containing a thiazolidinedione compound and having superior solubility. | 10-23-2008 |
20080275094 | 5-(1,3-Diaryl-1H-Pyrazol-4-1 Methylene)-Thiazolidine-2,4-Dione Derivatives Useful as Anticancer Agent - The present invention relates to a 5-(1,3-diaryl-1H-pyrazol-4-ylmethylene)-thiazolidine-2,4-dione derivative or its pharmaceutically acceptable salts thereof, a method for preparing the same and an anticancer agent composition comprising the same as an active ingredient. | 11-06-2008 |
20080280962 | NOVEL THIAZOLIDIN-4-ONE DERIVATIVES - The invention relates to pharmaceutical compositions containing at least one thiazolidin-4-one derivative to prevent or treat disorders associated with an activated immune system. Furthermore, the invention relates to novel thiazolidin-4-one derivatives notably for use as pharmaceutically active compounds. Said compounds particularly act also as immunosuppressive agents. | 11-13-2008 |
20080306126 | Peroxisome proliferator activated receptor treatment of hyperhomocysteinemia and its complications - A method of lowering homocysteine level of an individual and of reducing the vascular pathology associated therewith, by administering a ligand of the peroxisome proliferator activate receptor gamma. The peroxisome proliferator activated receptor preferably may be rosiglitazone. | 12-11-2008 |
20090018173 | Method for controlling the yeast-to-filamentous growth transition in fungi - A method for controlling yeast-to-filamentous growth transition in fungi comprising contacting a fungal cell with an anti-fungal small molecule in an amount effective to reduce or inhibit the yeast-to-filamentous growth transition, wherein the anti-fungal small molecule is 5-(p-Bromobenzylidine)-α-isopropyl-4-oxo-2-thioxo-3-thiozolidineacetic acid or an analog thereof. A method for treating fungal infections comprising contacting one or more fungal cells with an anti-fungal small molecule in an amount effective to control the fungal infection, wherein the anti-fungal small molecule is 5-(p-Bromobenzylidine)-α-isopropyl-4-oxo-2-thioxo-3-thiozolidineactic acid or an analog thereof. | 01-15-2009 |
20090054505 | THERAPEUTIC OXAZOLIDINONES AND THIAZOLIDINONES - Disclosed herein is a compound represented by a formula | 02-26-2009 |
20090088462 | Pharmaceutical Composition for Enhancing Adiponectin Production - Method for treatment of a human patient having hypoadiponectinemia. 5-[4-(6-methoxy-1-methyl-1H-benzimidazol-2-ylmethoxy)benzyl]thiazolidine-2,4-dione or a pharmacologically salt thereof is administered in an amount effective to raise the level of adiponectine in said patient. | 04-02-2009 |
20090111859 | Substituted biphenyl GPR40 modulators - The present invention provides compounds useful, for example, for treating metabolic disorders in a subject. Such compounds have the general formula I: | 04-30-2009 |
20090124675 | INHIBITORS OF ANTI-APOPTOTIC PROTEINS - Various compounds comprising a thiazolidine ring are described as well as the use of such compounds to inhibit at least one BCL-2 protein family member. One of the compounds described has the structure the structure A, | 05-14-2009 |
20090124676 | SUBSTITUTED CYCLOPENTANES HAVING PROSTAGLANDIN ACTIVITY - Disclosed herein are compounds having a formula: | 05-14-2009 |
20090137644 | RHODANINE COMPOSITIONS FOR USE AS ANTIVIRAL AGENTS - This invention describes compounds and pharmaceutical compositions useful as inhibitors of ubiquitination. The compounds and compositions of the invention are useful as inhibitors of the biochemical pathways of organisms in which ubiquitination is involved. In particular, the compounds and compositions are useful for treating diseases caused by viruses such as poxviruses and retroviruses. The invention further provides for methods of treating smallpox, Herpes virus and HIV infection in patients using the compounds and compositions of the invention. | 05-28-2009 |
20090143446 | THIAZOLIDINONE AMIDES, THIAZOLIDINE CARBOXYLIC ACID AMIDES, METHODS OF MAKING, AND USES THEREOF - Substituted thiazolidinone carboxylic acid amides and substituted thiazolidine carboxylic acid amides according to formulae (I) and (II) are disclosed | 06-04-2009 |
20090163560 | THERAPEUTIC N-ARYL OR N-HETEROARYL PYRAZOLIDINE AND PYRAZOLIDINONE DERIVATIVES - A compound having a structure | 06-25-2009 |
20090258914 | Inhibitor of Anti-Apoptotic Proteins - A compound having the structure A is described as well as the use of such compounds to inhibit at least one BCL-2 protein family member. | 10-15-2009 |
20090264483 | METHODS OF USING PPAR-gamma AGONISTS AND CASPASE-DEPENDENT CHEMOTHERAPEUTIC AGENTS FOR THE TREATMENT OF CANCER - This invention relates to compositions and methods utilizing a caspase-dependent chemotherapeutic drug and a PPARy-agonist, such as VP-16 or Taxol as the chemotherapeutic drug and troglitazone or pioglitazone as the PPARy agonist, for the treatment of cancer, including glioblastoma multiforme. The present invention demonstrates that PPAR agonists work with caspase-dependent chemotherapeutic drugs to increase the cytotoxic effects of these drugs in glioma cells. | 10-22-2009 |
20090275625 | NOVEL THIAZOLIDIN 4-ONE DERIVATIVES - The invention relates to pharmaceutical compositions containing at least one thiazolidin-4-one derivative to prevent or treat disorders associated with an activated immune system. Furthermore, the invention relates to novel thiazolidin-4-one derivatives notably for use as pharmaceutically active compounds. Said compounds particularly act also as immunosuppressive agents. | 11-05-2009 |
20090291992 | ANDROGEN RECEPTOR-ABLATIVE AGENTS - Compounds of the thiazolidinedione family are provided and shown to be effective androgen receptor ablative agents that can be used in methods of treating or preventing cancer or precancer, including prostate cancer. Also provided are methods of treating or preventing cancer by administering a therapeutically effective amount of one of the androgen receptor ablative agents to a subject in need of such treatment. | 11-26-2009 |
20090312376 | 5-(4-METHANESULFONYL-PHENYL)-THIAZOLE DERIVATIVES FOR THE TREATMENT OF ACUTE AND CHRONIC INFLAMMATORY DISEASES - The invention relates to a compound of formula (I): | 12-17-2009 |
20100010056 | TREATMENT FOR NICOTINE-INDUCED LUNG DISEASE USING PEROXISOME PROLIFERATOR-ACTIVATED RECEPTOR GAMMA AGONISTS - This invention provides pertains to the discovery that that nicotine interrupts molecular signaling between endodermal and mesodermal cells of the lung alveolus. Treatment of the lung with specific molecular agents (e.g., PPAR gamma agonists) can prevent and/or reverse the injury caused by nicotine. | 01-14-2010 |
20100076037 | Methods of Treating Neuropathic Pain with Agonists of PPAR-gamma - Embodiments of the invention relate to the treatment of neuropathic pain in mammals. Embodiments of the invention include methods for treating neuropathic pain as well as methods for preparing medicaments used in the treatment of mammalian pain. Preferably, methods of the invention comprise the use of PPARgamma agonists for the treatment of mammalian pain. | 03-25-2010 |
20100130571 | CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR PROTEIN INHIBITORS AND USES THEREOF - The invention provides compositions, pharmaceutical preparations and methods for inhibition of cystic fibrosis transmembrane conductance regulator protein (CFTR) that are useful for the study and treatment of CFTR-mediated diseases and conditions. The compositions and pharmaceutical preparations of the invention may comprise one or more thiazolidinone compounds, and may additionally comprise one or more pharmaceutically acceptable carriers, excipients and/or adjuvants. The methods of the invention comprise, in certain embodiments, administering to a patient suffering from a CFTR-mediated disease or condition, an efficacious amount of a thiazolidinone compound. In other embodiments the invention provides methods of inhibiting CFTR that comprise contacting cells in a subject with an effective amount of a thiazolidinone compound. In addition, the invention features a non-human animal model of CFTR-mediated disease which model is produced by administration of a thiazolidinone compound to a non-human animal in an amount sufficient to inhibit CFTR. | 05-27-2010 |
20100130572 | CYTOSKELETAL ACTIVE COMPOUNDS, COMPOSITION AND USE - The present invention is directed to synthetic cytoskeletal active compounds that are related to natural Latrunculin A or Latrunculin B. The present invention is also directed to pharmaceutical compositions comprising such compounds and a pharmaceutically acceptable carrier. The invention is additionally directed to a method of preventing or treating diseases or conditions associated with actin polymerization. In one embodiment of the invention, the method treats increased intraocular pressure, such as primary open-angle glaucoma. The method comprises administering to a subject a therapeutically effective amount of a cytoskeletal active compound of Formula I or II, wherein said amount is effective to influence the cytoskeleton, for example by inhibiting actin polymerization. | 05-27-2010 |
20100160395 | CYCLOPROPYL COMPOUNDS - A compound of the formula: | 06-24-2010 |
20100179200 | 2-OXOTHIAZOLIDINE 4-CARBOXYLIC ACID COMPOUNDS FOR PROMOTING DESQUAMATION OF THE SKIN - 2-oxothiazolidine-4-carboxylic acid compounds having the structural formula (I): | 07-15-2010 |
20100204288 | Heteroaryl-Ureas and Their Use as Glucokinase Activators - This invention relates to compounds of formula (I) | 08-12-2010 |
20100216852 | METHODS FOR SCREENING ANTIMICROBIAL AND ANTIVIRAL COMPOUNDS AND USES THEREOF - The invention features compounds that have antibacterial activity, their use for the treatment of bacterial infections, screening methods that use whole animals or plant seedlings to identify compounds that inhibit a pathogen in the animal or plant, and screening methods to identify compounds that increase the lifespan of an organism. | 08-26-2010 |
20100216853 | Methods and Compositions for Modulating P300/CBP Activity - The present invention relates to a method for identifying compounds that modulate the activity of p300/CBP. Compounds of the invention are identified by designing or screening for a compound which binds to at least one amino acid residue of the newly identified lysine-CoA inhibitor binding site, L1 loop, electronegative pocket, or electronegative groove of the HAT domain of p300/CBP and testing the compound for its ability to modulate the activity of p300/CBP. Compositions and methods for preventing or treating diseases or disorders associated with p300/CBP are also provided as is a method for producing a semi-synthetic HAT domain. | 08-26-2010 |
20100222399 | Thiazolidinedione Analogues For The Treatment Of Hypertension - The present invention relates to thiazolidinedione analogues that are useful for treating hypertension, diabetes, and inflammatory diseases. Formula (I), wherein: each of R | 09-02-2010 |
20100249201 | 3-3-Di-Substituted-Oxindoles As Inhibitors of Translation Initiation - Compositions and methods for inhibiting translation using 3-(5-tert-Butyl-2-Hydroxy-phenyl)-3-phenyl-1,3-dihydro-indol-2-one and/or its derivatives are provided. Compositions, methods and kits for treating (1) cellular proliferative disorders, (2) non-proliferative, degenerative disorders, (3) viral infections, and/or (4) disorders associated with viral infections, using 3-(5-tert-butyl-2-hydroxy-phenyl)-3-phenyl-1,3-dihydro-indol-2-one and/or its derivatives are described. | 09-30-2010 |
20100298390 | INHIBITION OF LETHAL FACTOR PROTEASE ACTIVITY FROM ANTHRAX TOXIN - The present invention provides compounds that efficiently and specifically inhibit lethal factor (LF) protease activity of anthrax toxin. | 11-25-2010 |
20100305174 | Novel Heterocyclic Derivatives - The present invention relates to novel heterocyclic derivatives of formula (I) and their pharmaceutically acceptable salts, their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their hydrates, their solvates, their pharmaceutically acceptable salts, their pharmaceutical compositions, and their prodrugs thereof. The present invention more particularly provides novel compounds of the general formula (1). | 12-02-2010 |
20100305175 | PHARMACEUTICAL LATRUNCULIN FORMULATIONS - The present invention relates to an aqueous pharmaceutical formulation comprising at least one latrunculin and the formulation does not contain a substantial amount of dimethyl sulfoxide. In one embodiment, the present invention is directed to an aqueous pharmaceutical formulation comprising at least one latrunculin in an amount of 0.001-2% w/v, a non-ionic surfactant in an amount of 0.01-2% w/v, and a tonicity agent to maintain a tonicity between 200-400 mOsm/kG, at a pH between 4 to 8, wherein the latrunculin, the surfactant, and the tonicity agent are compatible in the formulation, and the formulation does not contain a substantial amount of dimethyl sulfoxide. The formulation is stable for at least six month at refrigerated temperature. The present invention further provides a method of reducing intraocular pressure, a method of treating glaucoma, a method of inhibiting wound healing after trabeculectomy, and a method of inhibiting angiogenesis. | 12-02-2010 |
20110021581 | DOSING REGIMEN FOR A SELECTIVE S1P1 RECEPTOR AGONIST - The present invention relates to a dosing regimen for a selective S1P | 01-27-2011 |
20110060019 | HETEROARYL-UREAS AND THEIR USE AS GLUCOKINASE ACTIVATORS - This invention relates to compounds of formula (I) | 03-10-2011 |
20110065761 | METHODS OF TREATING NERVE-RELATED VISION DISORDERS - This invention provides reagents and methods for delivering insulin, insulinomimetic agents, and the like to a vertebrate eye via subconjunctival routes, sub-Tenon's routes, or intravitreal routes for treatment of nerve-related vision disorders such as diabetic retinopathy, and formulations useful in the practice of the disclosed methods | 03-17-2011 |
20110086895 | THIAZOLIDINEDIONE ENERGY RESTRICTION-MIMETIC AGENTS - A method of inhibiting glycolysis in a subject by administering a pharmaceutical composition including a thiazolidinedione derivative to the subject is described. The thiazolidinedione derivatives are effective energy restriction mimetic agents, and can therefore be used to treat or prevent cancer in a subject, treat metabolic disorder, or increase the longevity of a subject. Various thiazolidinedione derivatives are also suitable for activating adenosine phosphate-activated protein kinase or inhibiting IL-6 expression. | 04-14-2011 |
20110092555 | Thiazolidinedione compound - A compound which is 5-{4-[(6-methoxy-1-methyl-1H-benzimidazol-2-yl)methoxy]benzyl}thiazolidine-2,4-dione hydrochloride, in crystal form wherein a powder x-ray diffraction pattern obtained by irradiation with a Cu Kα line shows main peaks at interplanar spacings d=14.29, 7.12, 5.34, 4.97, 4.74, 3.95, 3.85, 3.75, 3.55, 3.51, 3.15, 2.84, 2.76, 2.52 and 2.37. | 04-21-2011 |
20110124692 | CRYSTALLINE FORMS OF THIAZOLIDINEDIONE COMPOUND AND ITS MANUFACTURING METHOD - Thiazolidinedione compound crystalline forms useful as a bulk material for the manufacture of a peroxisome proliferator-activated receptor (PPAR) γ activator or an anticancer pharmaceutical composition are provided, which are hydrate crystalline forms of 5-(4-{[6-(4-amino-3,5-dimethylphenoxy)-1-methyl-1-H-benzimi dazol-2-yl]methoxy}benzyl)-1,3-thiazolidine-2,4-dione represented by Formula (I) below and of its dihydrochloride. | 05-26-2011 |
20110136880 | Latrunculin-Based Macrolides and Their Uses - Latrunculin derivatives are disclosed, as are anti-invasive and cytotoxic uses for latrunculins and latrunculin derivatives, and semisyntheses of latrunculin derivatives. The latrunculins and latrunculin derivatives are useful, for example, in treating cancers. | 06-09-2011 |
20110152329 | Use of Epothilone Derivatives for the Treatment of Hyperparathyroidism - The present invention relates to a method of treating a warm-blooded animal, especially a human, having hyperparathyroidism comprising administering to said animal a therapeutically effective amount of an epothilone derivative of formula I | 06-23-2011 |
20110166191 | 3-(2-amino-ethyl)-5-(3-cyclohexyl-propylidene)-thiazolidine-2,4-dione and its derivatives as multiple signaling pathway inhibitors and for the treatment of cancer - 3-(2-amino-ethyl)-5-(3-cyclohexyl-propylidene)-thiazolidine-2,4-dione and derivatives thereof are provided for use as dual inhibitors of the Raf/MEK/ERK and PI3K/Akt pathways and for use in the treatment of cancer. | 07-07-2011 |
20110196004 | CRYSTALLINE FORMS OF (R) -5-[3-CHLORO-4-(2,3-DIHYDROXY-PROPOXY)-BENZ [Z] YLIDENE] -2-( [Z]-PROPYLIMINO) -3-0-TOLYL-THIAZOLIDIN-4-ONE - The invention relates to crystalline forms of (R)-5-[3-chloro-4-(2,3-dihydroxy-propoxy)-benz[Z]ylidene]-2-([Z]-propylimino)-3-o-tolyl-thiazolidin-4-one, processes for the preparation thereof, pharmaceutical compositions containing said crystalline forms, and their use as compounds improving vascular function and as immunomodulating agents, either alone or in combination with other active compounds or therapies. | 08-11-2011 |
20110230529 | BENZAMIDE GLUCOKINASE ACTIVATORS - The present invention relates to N-heteroaryl-benzamides of the formula (I), pharmaceutical compositions comprising the same, and methods of using the same. The N-heteroaryl-benzamides are useful as glucokinase activators. | 09-22-2011 |
20110263664 | Inhibitors of PIM-1 Protein Kinases, Compositions and Methods for Treating Prostate Cancer - The disclosure relates to inhibitors of Pim-1 and/or Pim-2 protein kinase, to compositions comprising one or more inhibitors of Pim-1 and/or Pim-2 protein kinase, and to methods for treating cancer. | 10-27-2011 |
20110275681 | NOVEL SOLID FORMS OF EPALRESTAT - The invention relates to novel crystalline salts of 5-[(1Z,2E)-2-methyl-3-phenylpropenylidene]-4-oxo-2-thioxo-3-thiazolidineacetic acid and a novel betaine cocrystal of 5-[(1Z,2E)-2-methyl-3-phenylpropenylidene]-4-oxo-2-thioxo-3-thiazolidineacetic acid. The preparation and characterization of the novel crystalline salts and cocrystal according to various embodiments of the invention is described. The invention also relates to pharmaceutical compositions containing the novel crystalline salts and cocrystal and the therapeutic use of the novel crystalline salts and cocrystal to treat and/or prevent various conditions, including treating and/or preventing diabetic complications, inhibiting aldose reductase, and affording cardioprotection in patients who may be non-diabetic. | 11-10-2011 |
20110275682 | NOVEL CHOLINE COCRYSTAL OF EPALRESTAT - The invention relates to a novel choline cocrystal of 5-[(1Z,2E)-2-methyl-3-phenylpropenylidene]-4-oxo-2-thioxo-3-thiazolidineacetic acid. The preparation and characterization of the novel choline cocrystal according to various embodiments of the invention is described. The invention also relates to pharmaceutical compositions containing the novel choline cocrystal and the therapeutic use of the novel choline cocrystal to treat and/or prevent various conditions, including treating and/or preventing diabetic complications, treating and/or preventing homocystinuria reducing levels of homocysteine in blood serum, inhibiting aldose reductase, and affording cardioprotection in non-diabetic patients. | 11-10-2011 |
20110281921 | NOVEL ANTI-BIOFILM AGENTS - Novel agents exhibiting anti-biofilm formation activity while being non-cytotoxic are provided, as well as methods of using the same, either per se or conjugated to a polymer, for preventing and/or reducing the formation of microbial biofilms and/or for disrupting microbial biofilms. The novel agents described herein include thiazolidine-2,4-diones (TZDs), pyrrolidine-2,5-diones (PYDs), imidazolidine-2,4-diones or oxazolidine-2,4-diones, substituted by an alkyl having 7-20 carbon atoms in its backbone chain. | 11-17-2011 |
20110313007 | USE OF METFORMIN IN COMBINATION WITH A GLUCOKINASE ACTIVATOR AND COMPOSITIONS COMPRISING METFORMIN AND A GLUCOKINASE ACTIVATOR - The present invention provides uses of a glucokinase activator in combination with metformin. Uses include treating type 2 diabetes, lowering blood glucose, improving insulin sensitivity, enhancing phosphorylation of glucose, and improving the therapeutic effectiveness of metformin. The invention also provides pharmaceutical compositions that comprise a GK activator and metformin. The invention also provides a salt formed between metformin and a GK activator. | 12-22-2011 |
20110313008 | PENTAFLUOROSULPHOLANE-CONTAINING ANTIDIABETIC COMPOUNDS - This invention provides for certain pentafluorosulpholane-containing compounds of the formula or a pharmaceutically acceptable salt, ester, solvate or prodrug thereof, wherein the variables are defined herein; the inventive compounds are agonists of the G-protein coupled receptor 40 (GPR40, also known as free fatty acid receptor FFAR). This invention further relates to pharmaceutical compositions containing these compounds, and the use of these compounds to regulate insulin levels in a mammal. The compounds may be used, for example in the prevention and treatment of Type 2 diabetes mellitus and in the prevention and treatment of conditions related to Type 2 diabetes mellitus, such as insulin resistance, obesity and lipid disorders. | 12-22-2011 |
20120004271 | USE OF VAGINALLY-ADMINISTERED INSULIN SENSITIZING AGENTS - Use of vaginal insulin sensitising agents for the prevention and/or treatment of hyperandrogenism and/or polycystic ovary syndrome and/or related disorders. | 01-05-2012 |
20120010255 | Compounds and Methods for Regulating Integrins - The application describes small molecules capable of modulating activity of beta2 family of integrins, such as integrin CD11b/CD18 (also known as Mac-1, CR3 and αMβ2). Such compounds may be used in certain embodiments for treating a disease or condition, such as inflammation, immune-related disorders, cancer, ischemia-reperfusion injury, stroke, neointimal thickening associated with vascular injury, wound-healing, organ transplantation and cardiovascular disease, among others. | 01-12-2012 |
20120010256 | INHIBITORS OF 11-BETA-HYDROXY STEROID DEHYDROGENASE TYPE 1 - The present invention relates to compounds with the formula (I), (II), (III) or (IV): | 01-12-2012 |
20120088805 | COMPOUND HAVING DETRUSOR MUSCLE-CONTRACTING ACTIVITY AND URETHRAL SPHINCTER MUSCLE-RELAXING ACTIVITY - Since a compound represented by formula (I) wherein all of the symbols are the same as defined in the specification, a salt thereof, a solvate thereof, a prodrug thereof, a mixture with a diastereomer thereof in an arbitrary ratio, or a cyclodextrin clathrate thereof have a contracting activity of bladder detrusor and a relaxing activity of urethral sphincter, they can ameliorate bladder contraction dysfunction and/or urethral relaxation dysfunction, and for example, are effective for underactive bladder. Additionally, the compound of the present invention has little risk of side effects on the urinary system, the circulatory system and the digestive system, and exhibits excellent pharmacokinetics, such as oral absorbability etc. Therefore, the compound of the present invention is useful as a superior agent for preventing, treating and/or ameliorating underactive bladder. | 04-12-2012 |
20120115916 | OXAZOLE AND THIAZOLE DERIVATIVES AS ALX RECEPTOR AGONISTS - The invention relates to oxazole and thiazole derivatives of formula (I), wherein A, E, X, R | 05-10-2012 |
20120122939 | ALKYLSULFONYL-SUBSTITUTED THIAZOLIDE COMPOUNDS - A new class of alkylsulfonyl-substituted thiazolide compounds is described. These compounds show strong activity against hepatitis virus. | 05-17-2012 |
20120129896 | THIAZOLIDINEDIONE ANALOGUES FOR THE TREATMENT OF METABOLIC DISEASES - The present invention relates to thiazolidinedione analogues that are useful for treating hypertension, diabetes, and inflammatory diseases. | 05-24-2012 |
20120136033 | Small Molecule Antagonists of Phosphatidylinositol-3,4,5-Triphosphate (PIP3) and Uses Thereof - Disclosed are a new class of non-lipid small molecule inhibitors which interfere with the interaction between PIP3 and pleckstrin homology domains. These molecules target a broad range of PIP3-dependent signaling events in vitro and exert significant anti-tumor activity in vivo. The small molecule inhibitors of the invention can be used alone or together with tumor necrosis factor (TNF)-related apoptosis-inducing ligand (TRAIL) or other cancer medicament to treat cancer. Small molecule inhibitors of the invention act synergistically in combination with TRAIL in treating cancer. Pharmaceutical compositions and methods for treating cancer are provided. | 05-31-2012 |
20120136034 | FATTY ACIDS AS ANTI-INFLAMMATORY AGENTS - Compounds of formula I and their metabolites are potent mediators of an inflammatory response: (I) where a, b, c, d, e, f, V, W, X, Y, R | 05-31-2012 |
20120165375 | Urea Glucokinase Activators - This application relates to novel urea glucokinase activators and use of the compounds of the invention for preparation of a medicament for the treatment of various diseases, e.g. for the treatment of type 2 diabetes. Further encompassed is a pharmaceutical composition comprising a compound according to the invention and a process for preparing such. | 06-28-2012 |
20120252854 | CRYSTALLINE FORMS OF THIAZOLIDINEDIONE COMPOUND AND ITS MANUFACTURING METHOD - A crystalline form of a hydrate of a dihydrochloride 5-(4-{[6-(4-amino-3,5-dimethylphenoxy)-1-methyl-1-H-benzimidazol-2-yl]methoxy}benzyl)-1,3-thiazolidine-2,4-dione represented by the following formula: | 10-04-2012 |
20120258991 | METHOD OF TREATING A CANCER BY ADMINISTERING A SPECIFIED DRUG - A method of treating a cancer selected from the group consisting of breast cancer, pancreatic cancer, kidney cancer, prostate cancer, medulloblastoma, rhabdomyosarcoma, Ewing sarcoma, liposarcoma, multiple myeloma or leukemia. An effective amount of 5-(4-(6-(4-amino-3,5-dimethyl-phenoxy)-1-methyl-1H-benzimidazol-2-ylmethoxy)-benzyl)-thiazolidine-2,4-dione.dihydrochloride is administered to a patient having said cancer. | 10-11-2012 |
20120289557 | Protein Synthesis Required for Long-Term Memory is Induced by PKC Activation on Days Preceding Associative Learning - The present invention provides methods of contacting a protein kinase C (PKC) activator with a PKC activator in a manner sufficient to stimulate the synthesis of proteins sufficient to consolidate long-term memory. The present invention also provides methods of contacting a protein kinase C (PKC) activator with a PKC activator in a manner sufficient to downregulate PKC. | 11-15-2012 |
20120302612 | NOVEL THIAZOLIDIN-4-ONE DERIVATIVES - The invention relates to pharmaceutical compositions containing at least one thiazolidin-4-one derivative to prevent or treat disorders associated with an activated immune system. Furthermore, the invention relates to novel thiazolidin-4-one derivatives notably for use as pharmaceutically active compounds. Said compounds particularly act also as immunosuppressive agents. | 11-29-2012 |
20130085169 | METHODS AND COMPOSITIONS COMPRISING AMPK ACTIVATOR (METFORMIN/TROGLITAZONE) FOR THE TREATMENT OF MYOTONIC DYSTROPHY TYPE 1 (DM1) - The present invention relates to methods and compositions for the treatment of Myotonic Dystrophy type 1 (DM1) with an AMPK activator . | 04-04-2013 |
20130102645 | Methods and compositions for controlling vascularization in ophthalmological and dermatological diseases - A method for controlling vascularization in a patient's eye or skin includes administering to the patient's eye or skin a pharmaceutical composition having | 04-25-2013 |
20130143934 | AGENT FOR REGENERATION AND/OR PROTECTION OF NERVES - An EP2 agonist which may have an EP3 agonistic effect has an effect of regenerating and/or protecting nerves, and is therefore useful as a therapeutic agent for a disease of the peripheral nervous system, such as a lower or upper motor neuron disease, a nerve root disease, plexopathy, thoracic outlet compression syndrome, peripheral neuropathy, neurofibromatosis and neuromuscular transmission disease. An EP2 agonist which has an EP3 agonistic effect is a safe and effective agent for the regeneration and/or protection of nerves which has little influence on the circulatory system. | 06-06-2013 |
20130184318 | MODULATING COMPLIANCE OF TRABECULAR MESHWORK - The present invention provides methods of determining the effect of test agents on the compliance of trabecular meshwork (TM) tissue, at the level of the extracellular matrix (ECM) and/or cells within the TM. Agents that modulate (e.g., increase or decrease) compliance of the TM tissue find use. Agents that increase the compliance of ECM and TM cells within the TM find use in the treatment and prevention of eye disorders characterized by high intraocular pressure, e.g., glaucoma. | 07-18-2013 |
20130237573 | 4-SUBSTITUTED-3-BENZYLOXY-BICYCLO[3.1.0]HEXANE COMPOUNDS AS mGluR 2/3 ANTAGONISTS - A mGlu2/3 receptor antagonist of the formula: | 09-12-2013 |
20130296386 | SMALL MOLECULE RNASE INHIBITORS AND METHODS OF USE - Small molecule inhibitors of bacterial ribonuclease (e.g., RnpA) and methods for their synthesis and use are described herein. The methods of using the compounds include treating and preventing microbial infections and inhibiting bacterial ribonuclease. | 11-07-2013 |
20130310431 | USES FOR SUBSTITUTED 2-AMINO-THIAZOLONES IN TREATING ALZHEIMER'S DISEASE - The invention provides 11-β-hydroxysteroid dehydrogenase type 1 enzyme (11βHSD1) inhibitors, such as a compound of the formula: (A), its hydroxy and keto metabolites, and pharmaceutically acceptable salts thereof, for treating cognitive disorders, including age-related cognitive disorders, such as Alzheimer's Disease. Also provided are methods and uses for inhibiting 11βHSD1 and for reducing the concentration or preventing the elevation of concentration of cortisol in the brain of a subject by administering the compound of the formula (A); its hydroxy and keto metabolites, and pharmaceutically acceptable salts thereof. | 11-21-2013 |
20130310432 | NOVEL THIAZOLIDIN-4-ONE-DERIVATIVES - The invention relates to pharmaceutical compositions containing at least one thiazolidin-4-one derivative to prevent or treat disorders associated with an activated immune system. Furthermore, the invention relates to novel thiazolidin-4-one derivatives notably for use as pharmaceutically active compounds. Said compounds particularly act also as immunosuppressive agents. | 11-21-2013 |
20130345267 | METHODS AND COMPOSITIONS FOR MODULATING P300/CBP ACTIVITY - The present invention relates to a method for identifying compounds that modulate the activity of p300/CBP. Compounds of the invention are identified by designing or screening for a compound which binds to at least one amino acid residue of the newly identified lysine-CoA inhibitor binding site, L1 loop, electronegative pocket, or electronegative groove of the HAT domain of p300/CBP and testing the compound for its ability to modulate the activity of p300/CBP. Compositions and methods for preventing or treating diseases or disorders associated with p300/CBP are also provided as is a method for producing a semi-synthetic HAT domain. | 12-26-2013 |
20130345268 | Methods and Compositions for the Treatment of RAS Associated Disorders - The instant disclosure relates to compositions that may be useful as therapeutic agents for the treatment of disorders associated or caused by Ras deregulation or dysregulation, for example, disorders associated with alterations in the NF1 gene such as neurofibromatosis type I, fungal infections such as those caused by | 12-26-2013 |
20140051734 | Treatment of Type 2 Diabetes With a Combination of DPIV Inhibitor and Metformin or Thiazolidinedione - This invention relates to a therapeutic method for glycaemic control, in particular to a method for the treatment of Pi-type 2 diabetes, comprising the administration of a DPIV inhibitor together with metformin or a thiazolidinedione | 02-20-2014 |
20140187594 | DIPHENYL ETHER COMPOUNDS FOR THE TREATMENT OF LIVER, LUNG DISORDERS, DIABETIC COMPLICATIONS AND CARDIOVASCULAR DISEASES - Described herein are compounds of formula (I), their derivatives, analogs, tautomeric forms, stereoisomers, polymorphs, hydrates, solvates, pharmaceutically acceptable salts and compositions, metabolites and prodrugs thereof, for use in treating liver diseases such as non-alcoholic fatty liver disease (NAFLD) and non-alcoholic steatohepatitis (NASH), and other fibrotic diseases of the liver; diabetic complications such as macro (ischemic heart disease, cerebrovascular disease and peripheral vascular disease) and micro (cataract, retinopathy nephropathy neuropathy, maculopathy and glaucoma) vascular complication; and cardiovascular diseases such as atherosclerosis, restenosis, hypertension, vasospasm, and cardiac hypertrophy; and lung disorders and lung fibrosis. | 07-03-2014 |
20140187595 | Methods and Compositions Comprising AMPK Activator (Metformin/Troglitazone) for the Treatment of Myotonic Dystrophy Type 1 (DM1) - The present invention relates to methods and compositions for the treatment of Myotonic Dystrophy type 1 (DM1) with an AMPK activator . | 07-03-2014 |
20140221438 | NOVEL SOLID FORMS OF EPALRESTAT - The invention relates to novel crystalline salts of 5-[(1Z,2E)-2-methyl-3-phenylpropenylidene]-4-oxo-2-thioxo-3-thiazolidineacetic acid and a novel betaine cocrystal of 5-[(1Z,2E)-2-methyl-3-phenylpropenylidene]-4-oxo-2-thioxo-3-thiazolidineacetic acid. The preparation and characterization of the novel crystalline salts and cocrystal according to various embodiments of the invention is described. The invention also relates to pharmaceutical compositions containing the novel crystalline salts and cocrystal and the therapeutic use of the novel crystalline salts and cocrystal to treat and/or prevent various conditions, including treating and/or preventing diabetic complications, inhibiting aldose reductase, and affording cardioprotection in patients who may be non-diabetic. | 08-07-2014 |
20140235681 | Combination therapy for glaucoma - Disclosed herein is method of treating glaucoma or ocular hypertension comprising administering a prostaglandin agonist and a second therapeutically active agent to a mammal in need thereof, wherein said second therapeutically active agent is selected from: β-Blockers, Adrenergic Agonists, non-selective adrenergic agonists, α | 08-21-2014 |
20140249191 | Compositions for Controlling Vascularization in Ophthalmological and Dermatological Diseases - A treatment method for controlling vascularization in a patient's eye or skin includes administering to the patient's eye or skin a pharmaceutical composition having formula (I) or a pharmaceutically acceptable salt, hydrate, enantiomer, diastereomer, racemate or mixtures of stereoisomers thereof. wherein the patient has a disease or disorder associated with vascularization in the eye or skin or wherein said patient is at risk for developing a disease or disorder associated with vascularization of the eye or skin. | 09-04-2014 |
20140296309 | MODIFIED RELEASE COMPOSITIONS OF EPALRESTAT OR A DERIVATIVE THEREOF AND METHODS FOR USING THE SAME - Modified release pharmaceutical compositions of epalrestat are provided. Methods of manufacturing the tablets and treating various diseases and conditions, including diabetes and diabetic complications, by administering the modified release compositions to patients in need thereof are also provided. | 10-02-2014 |
20140303217 | DOSING REGIMEN FOR A SELECTIVE S1P1 RECEPTOR AGONIST - The present invention relates to a dosing regimen for a selective S1P | 10-09-2014 |
20140303218 | Nitrogen Mustard Derivatives - The disclosure includes compounds of Formula (1): wherein X | 10-09-2014 |
20140315964 | DOSING REGIMEN FOR A SELECTIVE S1P1 RECEPTOR AGONIST - The present invention relates to a dosing regimen for a selective S1P | 10-23-2014 |
20140364465 | THIAZOLIDINEDIONE DERIVATIVES, PREPARATION THEREOF AND USE THEREOF IN CANCER TREATMENT - The present invention relates to thiazolidinedione derivatives, to the processes for preparing same and to the therapeutic use thereof for preventing or treating cancer, and more specifically breast cancer. These compounds are of formula (I) and exhibit, at a concentration of 100 μM, a hepatocyte viability preferably greater than 60%, preferably greater than 80% and more preferentially greater than 85%. | 12-11-2014 |
20140371280 | Method of treating diabetic peripheral neuropathy through amendment of pre-neuronal diabetic coagulative micro-angiopathy and neuronal deficiency of mitochondrial ATP production, and through induction of neuronal regeneration - DPN is an intractable and tormenting neurovascular and dermal disorder. | 12-18-2014 |
20150031733 | TETRAZOLINONE COMPOUNDS AND ITS USE - The present invention provides a compound having an excellent efficacy for controlling pests. A tetrazolinone compound of a formula (1): [wherein, R1 represents an C6-C16 aryl group, an C1-C12 alkyl group, a C3-C12 cycloalkyl group or an adamantyl group, etc., which each optionally be substituted; R2 represents a hydrogen atom, an C1-C12 alkyl group, or a halogen atom, etc.; R4 and R5 represent independently of each other a hydrogen atom or an C1-C3 alkyl group, etc.; R6, R7, R8 and R9 represent independently of each other a hydrogen atom, a halogen atom, an C1-C12 alkyl group, a C1-C12 haloalkyl group, an C2-C12 alkenyl group, a C3-C12 cycloalkyl group, an C1-C12 alkoxy group or a C1-C12 haloalkoxy group, etc.; X and Y represent independently of each other a sulfur atom or an oxygen atom; Q represents an oxygen atom or a sulfur atom; and R10 represents an C1-C6 alkyl group, etc.] shows an excellent controlling efficacy on pests. | 01-29-2015 |
20150051255 | GLUCOSE TRANSPORTER INHIBITORS - Thiazolidinedione compounds and pharmaceutically acceptable salts thereof are described. The compounds can be used in methods of treating cancer in a subject by administering to the subject a therapeutically effective amount of the compound. The compounds can also be used in methods of inhibiting glucose uptake in a cell by contacting the cell with the compound. | 02-19-2015 |
20150057319 | NOVEL CHOLINE COCRYSTAL OF EPALRESTAT - The invention relates to a novel choline cocrystal of 5-[(1Z,2E)-2-methyl-3-phenylpropenylidene]-4-oxo-2-thioxo-3-thiazolidineacetic acid. The preparation and characterization of the novel choline cocrystal according to various embodiments of the invention is described. The invention also relates to pharmaceutical compositions containing the novel choline cocrystal and the therapeutic use of the novel choline cocrystal to treat and/or prevent various conditions, including treating and/or preventing diabetic complications, treating and/or preventing homocystinuria reducing levels of homocysteine in blood serum, inhibiting aldose reductase, and affording cardioprotection in non-diabetic patients. | 02-26-2015 |
20150073025 | METHOD FOR IDENTIFYING DISEASE RISK FACTORS - Provided herein is a method for identifying a genetic variant that is associated with development of a condition of interest (e.g., Alzheimer's disease), and genetic variants so identified. Methods of treatment with an active agent (e.g., with a particular active agent and/or at an earlier age) is also provided, upon detecting a genetic variant described herein. In some embodiments, the genetic variant is a deletion/insertion polymorphism (DIP) of the TOMM40 gene. Kits for determining if a subject is at increased risk of developing late onset Alzheimer's disease is also provided. Kits for determining if a subject is responsive to treatment for a condition of interest with an active agent are further provided. | 03-12-2015 |
20150105435 | COMPOUNDS AND METHODS FOR REGULATING INTEGRINS - A method of treating inflammation, by administering an effective amount of a β2 integrin agonist to a patient, and reducing inflammation. A method of treating cancer, by administering an effective amount of a β2 integrin agonist to a patient, and reducing tumor growth. A method of treating a patient exposed to radiation, by administering an effective amount of a β2 integrin agonist to the patient after radiation exposure, and mitigating the effects of radiation exposure in the patient. A method of preventing effects of radiation, by administering an effective amount of a β2 integrin agonist to the patient prior to radiation exposure, and preventing the effects of radiation exposure on the patient. A method of treating acquired bone marrow failure (BMF), by administering an effective amount of a β2 integrin agonist to a patient. Methods of improving the health of damaged vasculature in a patient and activating β2 integrins. | 04-16-2015 |
20150111933 | Deuterated Thiazolidinone Analogues as Agonists for Follicle Stimulating Hormone Receptor - The present invention relates to deuterated thiazolidinone analogues as agonists for follicle stimulating hormone receptor and their use for treating fertility disorders. | 04-23-2015 |
20150133514 | PROTEIN DISULFIDE ISOMERASE INHIBITING ANTICANCER AGENTS - Protein disulfide isomerase inhibitors according to formula I | 05-14-2015 |
20150297570 | SMALL MOLECULE INHIBITORS OF MALT1 - MALT1 cleavage activity is linked to the pathogenesis of activated B-cell-like diffuse large B-cell lymphoma (ABC-DLBCL), a chemo-resistant form of DLBCL. We developed a MALT1 activity assay and identified chemically diverse MALT1 inhibitors. A selected lead compound MI-2 featured direct binding to MALT1 and suppression of its protease function. MI-2 concentrated within human ABC-DLBCL cells and irreversibly inhibited cleavage of MALT1 substrates. This was accompanied by suppression of NF- | 10-22-2015 |
20150306074 | FATTY ACIDS AS ANTI-INFLAMMATORY AGENTS - Compounds of formula I and their metabolites are potent mediators of an inflammatory response: | 10-29-2015 |
20150352070 | METHODS OF TREATING DISEASES ASSOCIATED WITH HIGH-FAT DIET AND VITAMIN A DEFICIENCY USING RETINOIC ACID RECEPTOR AGONISTS - This invention relates to pharmaceutical composition and methods of using vitamin A and/or RARB agonist for the treatment or prevention of diseases or conditions associated with high fat diet and/or vitamin deficiency. After smoking, high fat diet is said to be the second most lethal habit, causing 300,000 deaths each year in the U.S. alone. High fat diet leads to many health problems, including obesity, stroke, cancer, high blood pressure, diabetes, osteoarthritis, rheumatoid arthritis, multiple sclerosis, heart disease, and diseases in other organs such as liver and kidney. | 12-10-2015 |
20160015816 | SOLID COMPOSITIONS COMPRISING A GLUCOKINASE ACTIVATOR AND METHODS OF MAKING AND USING THE SAME - The invention relates to solid compositions comprising {2-[3-cyclohexyl-3-(trans-4-propoxy-cyclohexyl)-ureido]-thiazol-5-ylsulfanyl}-acetic acid, and methods of making and using such solid compositions. | 01-21-2016 |
20160024071 | INHIBITORS OF LRRK2 KINASE ACTIVITY - The present invention provides compounds having a structure according to Formula I. The invention further provides pharmaceutical compositions including the compounds of the invention and methods of making and using the compounds and compositions of the invention, e.g., in the treatment and prevention of various disorders, such as Parkinson's disease. | 01-28-2016 |
20160045607 | ESTROGEN-RELATED RECEPTOR ALPHA BASED PROTAC COMPOUNDS AND ASSOCIATED METHODS OF USE - The present invention relates to bifunctional compounds, which find utility as modulators of targeted ubiquitination, especially inhibitors of a variety of polypeptides and other proteins which are degraded and/or otherwise inhibited by bifunctional compounds according to the present invention. In particular, the present invention is directed to compounds, which contain on one end a VHL ligand which binds to the ubiquitin ligase and on the other end a moiety which binds a target protein such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of that protein. The present invention exhibits a broad range of pharmacological activities associated with compounds according to the present invention, consistent with the degradation/inhibition of targeted polypeptides. | 02-18-2016 |
20160051521 | Thiazolidinediones of Omega-3 Polyunsaturated Acids as New Insulin Sensitizers for Treating Type2 Diabetes - The present invention relates to thiazolidinedione derivatives of omega-3 fatty acids as insulin sensitizers, and their use in treating Type2 diabetes, obesity, hypertriglyceridemia, cardiovascular diseases, metabolic diseases, inflammation, renal anemia, and/or Alzheimer's disease: and for modulating activity of peroxisome proliferator-activated receptors (PPARs). | 02-25-2016 |
20160130240 | ARYL SULFIDE DERIVATIVES AND ARYL SULFOXIDE DERIVATIVES AS ACARICIDES AND INSECTICIDES - The present invention relates to aryl sulfoxide derivatives, to the use thereof as acaricides and insecticides for controlling animal pests and to processes and intermediates for preparation thereof. The aryl sulfide and aryl sulfoxide derivatives have the general structure (I) | 05-12-2016 |
20160151336 | COMPOUNDS AND METHODS FOR REGULATING INTEGRINS | 06-02-2016 |
20160159758 | 3-(2-AMINO-ETHYL)-ALKYLIDENE)-THIAZOLIDINE-2,4-DIONE AND 1-(2-AMINO-ETHYL)-ALKYLIDENE-1,3-DIHYDRO-INDOL-2-ONE DERIVATIVES AS SELECTIVE SPHINGOSINE KINASE 2 INHIBITORS - 3-(2-amino-ethyl)-5-[3-(4-substituted-phenyl)-alkylidene)-thiazolidine-2,4-dione and 1-(2-amino-ethyl)-3-alkylidene-1,3-dihydro-indol-2-one and derivatives thereof are provided for use as selective SphK2 inhibitors and for use in the treatment of human diseases, such as cancer. | 06-09-2016 |
20160176859 | High-Throughput Assay for Identifying Small Molecules that Modulate AMP-activated Protein Kinase (AMPK) | 06-23-2016 |
20160184277 | Use of Metformin in Combination with a Glucokinase Activator and Compositions Comprising Metformin and a Glucokinase Activator - The present invention provides uses of a glucokinase activator in combination with metformin. Uses include treating type 2 diabetes, lowering blood glucose, improving insulin sensitivity, enhancing phosphorylation of glucose, and improving the therapeutic effectiveness of metformin. The invention also provides pharmaceutical compositions that comprise a GK activator and metformin. The invention also provides a salt formed between metformin and a GK activator. | 06-30-2016 |
20160250194 | Methods of Making and Using Thioxothiazolidine and Rhodanine Derivatives as HIV-1 and JSP-1 Inhibitors | 09-01-2016 |