Entries |
Document | Title | Date |
20080207707 | ARYL-SUBSTITUTED HETEROCYCLES, PROCESS FOR THEIR PREPARATION AND THEIR USE AS MEDICAMENTS - The invention relates to substituted aryl-substituted heterocycles and to the physiologically tolerated salts and physiologically functional derivatives thereof, to process for their preparation and to their use as medicaments. | 08-28-2008 |
20080227833 | OXA- AND THIADIAZOLES AND THEIR USE AS METALLOPROTEINASE INHIBITORS - Compounds formula (IA) or (IB), wherein W represents HO(C═O)—, HONH(C═O)— or H(C═O)N(OH)—; X represents —O— or —S—; and R | 09-18-2008 |
20080227834 | DERIVATIVES OF 2-AMINOTHIAZOLES AND 2-AMINO-OXAZOLES, PROCESSES FOR THEIR PREPARATION AND THEIR USE AS PHARMACEUTICAL COMPOSITIONS - The present invention relates to derivatives of 2-aminothiazoles and 2-aminooxazoles in all its stereoisomeric forms, enantiomeric forms and mixtures in any ratio, and its physiologically acceptable salts and tautomeric forms showing peroxisome proliferators activator receptor (PPAR) delta agonist activity. These compounds are compounds of the formula I, | 09-18-2008 |
20080255210 | OXADIAZOLINE LIGANDS FOR MODULATING THE EXPRESSION OF EXOGENOUS GENES VIA AN ECDYSONE RECEPTOR COMPLEX - The present invention relates to non-steroidal ligands for use in nuclear receptor-based inducible gene expression system, and a method to modulate exogenous gene expression in which an ecdysone receptor complex comprising: a DNA binding domain; a ligand binding domain; a transactivation domain; and a ligand is contacted with a DNA construct comprising: the exogenous gene and a response element; wherein the exogenous gene is under the control of the response element and binding of the DNA binding domain to the response element in the presence of the ligand results in activation or suppression of the gene. | 10-16-2008 |
20080255211 | Oxadiazole Compounds - A compound of formula (I): | 10-16-2008 |
20080255212 | OXADIAZOLONES AND DERIVATIVES THEREOF AS PEROXISOME PROLIFERATOR - ACTIVATED RECEPTOR (PPAR) DELTA AGONISTS - The invention relates to oxadiazolones and to their physiologically acceptable salts and physiologically functional derivatives showing peroxisome proliferator activator receptor (PPAR) delta agonist activity comprising compounds of formula I, | 10-16-2008 |
20080262051 | Triazole derivatives which are SMO antagonists - The present invention provides a method for the treatment or prevention of conditions which can be ameliorated by Smo antagonism, which method comprises administration to a patient in need thereof of an effective amount of a compound of formula I or a composition comprising a compound of formula I: | 10-23-2008 |
20080262052 | METHODS FOR THE TREATMENT OF METABOLIC AND GLUCOSE UTILIZATION DISORDERS THROUGH THE ADMINISTRATION OF OXADIAZOLONES AND DERIVATIVES THEREOF AS PEROXISOME PROLIFERATOR - ACTIVATED RECEPTOR (PPAR) DELTA AGONISTS - The invention relates to oxadiazolones and to their physiologically acceptable salts and physiologically functional derivatives showing PPARdelta agonist activity. | 10-23-2008 |
20080269302 | Macrocyclic Tertiary Amine Beta-Secretase Inhibitors for the Treatment of Alzheimer's Disease - The present invention is directed to macrocyclic tertiary amine compounds represented by general formula (I) | 10-30-2008 |
20080275093 | Diuretic Compounds Comprising Heterocyclic Nitric Oxide Donor Groups, Compositions and Methods of Use - The invention describes novel diuretic compounds comprising at least one heterocyclic nitric oxide donor group, or pharmaceutically acceptable salts thereof, and novel composition comprising at least one diuretic compound comprising at least one heterocyclic nitric oxide donor group, and optionally, at least one nitric oxide enhancing compound and/or at least one therapeutic agent. The invention also provides novel compositions and kits comprising at least one diuretic compound of the invention comprising at least one heterocyclic nitric oxide donor group, and optionally, at least one nitric oxide enhancing compound and/or at least one therapeutic agent. The invention also provides methods for (a) treating conditions resulting from excessive water and/or electrolyte retention; (b) treating cardiovascular diseases; (c) treating renovascular diseases; (d) treating diabetes; (e) treating diseases resulting from oxidatives stress; (f) treating endothelial dysfunctions; (g) treating diseases caused by endothelial dysfunctions; (h) treating cirrhosis; (j) treating pre-eclampsia; (k) treating osteoporosis; (l) treating nephropathy; (m) treating peripheral vascular diseases; (n) treating portal hypertension; (o) treating central nervous system disorders; and (p) treating sexual dysfunctions. The heterocyclic nitric oxide donors are preferably furoxans, sydnonimines, oxatriazole-5-ones and/or oxatriazole-5-imines. | 11-06-2008 |
20080293783 | OXADIAZOLYL-PHENOXYALKYLISOXAZOLES, COMPOSITIONS THEREOF AND METHODS FOR THEIR USE AS ANTI-PICORNAVIRAL AGENTS - Oxadiazolyl-phenoxyalkylisoxazoles and pharmaceutically acceptable salts thereof, compositions comprising oxadiazolyl-phenoxyalkylisoxazole compounds or pharmaceutically acceptable salts thereof and methods for using oxadiazolyl-phenoxyalkylisoxzazole compounds or pharmaceutically acceptable salts thereof as anti-picornaviral agents are described herein. The methods include using pleconaril as a prodrug for conversion to anti-picornaviral compounds in vivo. | 11-27-2008 |
20080306124 | Polycyclic Oxadiazoles or I Soxazoles and Their Use as Sip Receptor Ligands - Disclosed are polycyclic compounds of formula I | 12-11-2008 |
20080306125 | Compounds and Methods for Modulating Fx-Receptors - Compounds of formula. wherein variables are as defined herein and their pharmaceutical compositions and methods of use are disclosed as useful for treating dyslipidemia and related diseases. | 12-11-2008 |
20080312299 | Imidazole Derivatives as Fructose-1,6-Bisphosphatase Inhibitors and Pharmaceutical Compositions Containing Them - Imidazole derivatives of formula (I) wherein R | 12-18-2008 |
20080319030 | SYDNONIMINES - SPECIFIC DOPAMINE REUPTAKE INHIBITORS AND THEIR USE IN TREATING DOPAMINE RELATED DISORDERS - Derivatives of Sydnonimine and its analogues, which bind selectively to dopamine transporter (DAT) proteins are useful for treating and delaying the progression of disorders and illnesses that are alleviated by inhibiting dopamine reuptake. | 12-25-2008 |
20090012132 | Pharmaceutical Package - The present invention relates to a pharmaceutical package including a pharmaceutical preparation containing 2-ethoxy-1-{[2′-(5-oxo-4,5-dihydro-1,2,4-oxadiazol-3-yl)biphenyl-4-yl]methyl}-1H-benzimidazole-7-carboxylic acid (5-methyl-2-oxo-1,3-dioxol-4-yl)methyl or 2-cyclopropyl-1-{[2′-(5-oxo-4,5-dihydro-1,2,4-oxadiazol-3-yl)biphenyl-4-yl]methyl}-1H-benzimidazole-7-carboxylic acid (5-methyl-2-oxo-1,3-dioxol-4-yl)methyl or a salt thereof, and a desiccant. According to the present invention, a pharmaceutical package having a decreased uncomfortable odor is provided. | 01-08-2009 |
20090018172 | DIPHENYLUREA DERIVATIVES AND THEIR USE AS CHLORIDE CHANNEL BLOCKERS OR BKCa CHANNEL MODULATORS - The present invention relates to novel diphenylurea derivatives useful as chloride channel blockers or BK | 01-15-2009 |
20090030049 | MEDICAMENT FOR GENITAL HERPES - [PROBLEMS] To provide a medicament useful for the treatment of genital herpes after the development of lesions. | 01-29-2009 |
20090036503 | Triazole Derivatives as Inhibitors of 11-Beta-Hydroxysteroid Dehydrogenase-1 - Triazole derivatives of structural formula I are selective inhibitors of the 11β-hydroxysteroid dehydrogenase-1. The compounds are useful for the treatment of diabetes, such as noninsulin-dependent diabetes (NIDDM), hyperglycemia, obesity, insulin resistance, dyslipidemia, hyperlipidemia, hypertension, Metabolic Syndrome, and other symptoms associated with NIDDM. | 02-05-2009 |
20090042954 | 2-(Aryl)Azacyclylmethyl Carboxylates, Sulfonates, Phosphonates, Phosphinates and Heterocycles as S1p Receptor Antagonists - The present invention encompasses compounds of Formula I: | 02-12-2009 |
20090042955 | BICYCLIC SPHINGOSINE 1-PHOSPHATE ANALOGS - Compounds that have agonist activity at one or more of the S1P receptors are provided. The compounds are sphingosine analogs that, after phosphorylation, can behave as agonists at S1P receptors. | 02-12-2009 |
20090048310 | AGENT FOR PREVENTION/TREATMENT OF DISEASE CAUSED BY ACYCLOVIR-RESISTANT HERPESVIRUS - [Problems] To provide an agent useful for the prevention or treatment of various diseases associated with the infection with acyclovir-resistant viruses of the family Herpesviridae, specifically various infectious caused by herpes viruses, such as varicella associated with varicella-zoster virus infection, herpes zoster associated with recurrent infection with latent varicella-zoster virus, and herpes labialis, herpes encephalitis and genital herpes associated with HSV-1 and HSV-2 infection, and the like. | 02-19-2009 |
20090048311 | Compostions and Methods for Controlling Nematodes - Compositions and processes for controlling nematodes are described herein, e.g., nematodes that infest plants or animals. The compounds include oxazoles, oxadiazoles and thiadiazoles. | 02-19-2009 |
20090054502 | Benzimidazole Derivative and Use as Angiotensin II Antagonist - The present invention provides (5-methyl-2-oxo-1,3-dioxol-4-yl)methyl 2-cyclopropyl-1-{[2′-(5-oxo-4,5-dihydro-1,2,4-oxadiazol-3-yl)biphenyl-4-yl]methyl}-1H-benzimidazole-7-carboxylate represented by the formula: | 02-26-2009 |
20090069391 | Benzothiophene hydroxamic acid derivatives - The present invention relates to a novel class of hydroxamic acid derivatives. The hydroxamic acid compounds can be used to treat cancer. The hydroxamic acid compounds 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 are also 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. | 03-12-2009 |
20090093528 | METHODS FOR PROMOTING COMPOSITE TISSUE REGENERATION AND USES THEREOF - The present invention provides a use and method for GM284 to promote the regeneration of a bodily structure, comprised of a composite tissue in a subject. Additionally, the present invention provides a use and method for GM284 to promote composite tissue regeneration in a subject. The present invention further provides a use and method for GM284 to promote the regeneration of cells of a composite tissue in a subject. Finally, the present invention provides a use and method for GM284 to treat an injury to a composite tissue in a subject in need of such treatment. | 04-09-2009 |
20090105315 | PHENYL-CYCLOALKYL AND PHENYL-HETEROCYCLIC DERIVATIVES AS S1P RECEPTOR AGONISTS - Compounds that have agonist activity at one or more of the S1P receptors are provided. The compounds are sphingosine analogs that, after phosphorylation, can behave as agonists at S1P receptors. | 04-23-2009 |
20090111858 | Novel Alpha-(N-Sulfonamido)Acetamide Compound as an Inhibitor of Beta Amyloid Peptide Production - The present invention provides a novel alpha-(N-sulfonamido)acetamide compound, its pharmaceutical composition, processes thereof and a method for the treatment of Alzheimer's disease and other conditions associated with β-amyloid peptide. | 04-30-2009 |
20090124672 | ALDH-2 INHIBITORS IN THE TREATMENT OF PSYCHIATRIC DISORDERS - Disclosed are isoflavone derivatives having the structure of Formula I | 05-14-2009 |
20090137642 | 2-Acylaminothiazole Derivatives - The Invention relates to compounds of the formula I, wherein the variables are as defined in the claims, for use as a medicament. The compounds are A | 05-28-2009 |
20090149513 | Compositions of an Orally Active 1,2,4-Oxadiazole for Nonsense Mutation Suppression Therapy - The present invention relates to specific doses of and dosing regimens for using a 1,2,4-oxadiazole benzoic acid compound in treating or preventing diseases associated with nonsense mutations. In particular, the invention relates to specific doses and dosing regimens for the use of 3-[5-(2-fluoro-phenyl)-[1,2,4]oxadiazol-3-yl]-benzoic acid in mammals having diseases associated with nonsense mutations. | 06-11-2009 |
20090149514 | OXADIAZOLINE LIGANDS FOR MODULATING THE EXPRESSION OF EXOGENOUS GENES VIA AN ECDYSONE RECEPTOR COMPLEX - The present invention relates to methods to use non-steroidal ligands in nuclear receptor-based inducible gene expression system to modulate exogenous gene expression in which an ecdysone receptor complex comprising: a DNA binding domain; a ligand binding domain; a transactivation domain; and a ligand is contacted with a DNA construct comprising: the exogenous gene and a response element; wherein the exogenous gene is under the control of the response element and binding of the DNA binding domain to the response element in the presence of the ligand results in activation or suppression of the gene. | 06-11-2009 |
20090149515 | Treatments for the control of schistosomiasis - A method for controlling schistosome parasites in a mammal comprising delivering an effective amount of an agent for silencing TGR activity in the parasites. | 06-11-2009 |
20090182021 | Tricyclic Beta-Secretase Inhibitors for the Treatment of Alzheimer's Disease - The present invention is directed to tricyclic compounds which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved. | 07-16-2009 |
20090197926 | BENZIMIDAZOLES AND THEIR USE FOR THE TREATMENT OF DIABETES - Compounds of formula (I), or salts thereof, which inhibit acetyl CoA (acetyl coenzyme A):diacylglycerol acyltransferase (DGAT1) activity are provided, | 08-06-2009 |
20090203752 | COMPOUNDS FOR NONSENSE SUPPRESSION, AND METHODS FOR THEIR USE - The present invention relates to methods, compounds, and compositions for treating or preventing diseases associated with nonsense mutations in an mRNA by administering the compounds or compositions of the present invention. More particularly, the present invention relates to methods, compounds, and compositions for suppressing premature translation termination associated with a nonsense mutation in an mRNA. | 08-13-2009 |
20090215839 | SYDNONIMINES-SPECIFIC DOPAMINE REUPTAKE INHIBITORS AND THEIR USE IN TREATING DOPAMINE RELATED DISORDERS - Derivatives of Sydnonimine and its analogues, which bind selectively to dopamine transporter (DAT) proteins are useful for treating and delaying the progression of disorders and illnesses that are alleviated by inhibiting dopamine reuptake. | 08-27-2009 |
20090239915 | Substituted 2-phenyl-benzimidazoles and their use as pharmaceuticals - The present invention relates to derivatives of 2-phenyl-benzimidazoles of the formula I, | 09-24-2009 |
20090247591 | SUBSTITUTED CYCLOHEXYLDIAMINES - The invention relates to compounds that have an affinity to the μ-opioid receptor and the ORL 1-receptor, methods for their production, medications containing these compounds and the use of these compounds for the treatment of pain or other conditions. | 10-01-2009 |
20090253759 | TETRALIN ANALOGS HAVING SPHINGOSINE 1-PHOSPHATE AGONIST ACTIVITY - Tetralin analogs that have agonist activity at one or more of the S1P receptors are provided. The compounds are sphingosine analogs, which, after phosphorylation, can behave as agonists at S1P receptors. | 10-08-2009 |
20090253760 | HYDRINDANE ANALOGS HAVING SPHINGOSINE 1-PHOSPHATE RECEPTOR AGONIST ACTIVITY - Hydrindane analogs that have agonist activity at one or more of the S | 10-08-2009 |
20090253761 | BENZOCYCLOHEPTYL ANALOGS HAVING SPHINGOSINE 1-PHOSPHATE RECEPTOR ACTIVITY - Benzocycloheptyl analogs that have agonist activity at one or more of the S1P receptors are provided. The compounds are sphingosine analogs, which, after phosphorylation, can behave as agonists at S1P receptors. | 10-08-2009 |
20090258913 | Triazole Derivatives as Inhibitors of 11-Beta-Hydroxysteroid Dehydrogenase-1 - Triazole derivatives of structural formula I are selective inhibitors of the 11β-hydroxysteroid dehydrogenase-1. The compounds are useful for the treatment of diabetes, such as noninsulin-dependent diabetes (NIDDM), hyperglycemia, obesity, insulin resistance, dyslipidemia, hyperlipidemia, hypertension, Metabolic Syndrome, and other symptoms associated with NIDDM. | 10-15-2009 |
20090264481 | Compounds, Compositions and Methods Comprising Oxadiazole Derivatives - The present invention relates to compositions and methods for treating a disease in an animal, which disease is responsive to inhibiting of functional cystic fibrosis transmembrane conductance regulator (CFTR) polypeptide by administering to a mammal in need thereof an effective amount of a compound defined herein (including those compounds set forth in Table 1 or encompassed by formula I, II, or III) or compositions thereof, thereby treating the disease. The present invention particularly, relates to a method of treating diarrhea and polycystic kidney disease. | 10-22-2009 |
20090264482 | CHEMICAL COMPOUNDS - This invention relates to non-steroidal compounds that are modulators of androgen receptor, and also to the methods for the making and use of such compounds. | 10-22-2009 |
20090270463 | AMIDO DERIVATIVES-CONTAINED PHARMACEUTICAL COMPOSITION - The present invention relates to a pharmaceutical composition containing a solid dispersion comprising an amide derivative or a salt thereof and a water-soluble polymer, wherein the pharmaceutical composition is not prepared by a melting method. The pharmaceutical composition contains the solid dispersion having an improved oral absorption, properties suitable for formulation, and an excellent stability. | 10-29-2009 |
20090270464 | Benzimidazole derivative and use as a II receptor antagonist - The present invention relates to a compound represented by the formula (I) | 10-29-2009 |
20090275620 | SUBSTITUTED 5- PHENYLAMINO- 1, 3, 4-OXADIAZOL-2-YLCARBONYLAMINO-4-PHENOXY-CYCLOHEXANE CARBOXYLIC ACID AS INHIBITORS OF ACETYL COENZYME A DIACYLGLYCEROL ACYLTRANSFERASE - Compounds of formula (I), or salts thereof, which inhibit acetyl CoA (acetyl coenzyme A):diacylglycerol acyltransferase (DGAT1) activity are provided, | 11-05-2009 |
20090275621 | 1, 3, 4-OXADIAZOL-2-ONES AS PPAR DELTA MODULATORS AND THEIR USE THEREOF - The present invention is directed to 1,3,4-oxadiazalones, compounds of formula I and their pharmaceutically acceptable salts stereoisomers, tautomers, or solvates thereof. Novel compounds include those of formula I, in which radicals are as defined herein. | 11-05-2009 |
20090286837 | Oxadiazole compounds as urokinase inhibitors - The present invention relates to novel compounds which inhibit urokinase-plasminogen activator (uPA), have a high bioavailability and can be administered orally, and to their use as therapeutic active substances for the treatment of disorders associated with urokinase and/or urokinase receptor, for example tumours and metastasis. The invention relates in particular to compounds containing oxadiazole groups. | 11-19-2009 |
20090291990 | OXADIAZOLYL-PHENOXYALKYLISOXAZOLES, COMPOSITIONS THEREOF AND METHODS FOR THEIR USE AS ANTI-PICORNAVIRAL AGENTS - Oxadiazolyl-phenoxyalkylisoxazoles and pharmaceutically acceptable salts thereof, compositions comprising oxadiazolyl-phenoxyalkylisoxazole compounds or pharmaceutically acceptable salts thereof and methods for using oxadiazolyl-phenoxyalkylisoxzazole compounds or pharmaceutically acceptable salts thereof as anti-picornaviral agents are described herein. The methods include using pleconaril as a prodrug for conversion to anti-picornaviral compounds in vivo. | 11-26-2009 |
20090291991 | ISOINDOLINE COMPOUNDS AND METHODS OF THEIR USE - Novel isoindoline compounds are disclosed. Methods of treating, preventing and/or managing cancer, diseases and disorders associated with, or characterized by, undesired angiogenesis, and diseases and disorders mediated by PDE 4, using the compounds are also disclosed. | 11-26-2009 |
20090298894 | AMINO ACID COMPOUNDS - [Problem] To provide novel compounds that are S1P1 receptor agonists and exhibit an immunosuppressive activities by inducing lymphocyte sequestration in secondary lymphoid tissues. In addition, to provide a pharmaceutical agent which comprises the compounds as an effective component, in particular to provide a therapeutic and/or prophylactic agent for an autoimmune disease and the like. | 12-03-2009 |
20090326016 | FUNGICIDAL N-CYCLOALKYL-CARBOXAMIDE DERIVATIVES - The present invention relates to N-cycloalkyl-thiocarboxamide or N-cycloalkyl-N-substituted carboximidamide derivatives of formula (I) wherein A and B represent a 5-membered heterocyclyl groups, T represents an oxygen, sulphur or amino derivatives, Z | 12-31-2009 |
20090326017 | PAIN-RELIEVING COMPOSITIONS AND USES THEREFOR - This invention discloses compositions and methods for inducing, promoting or otherwise facilitating pain relief. More particularly, the present invention discloses the use of sub-normovasodilatory doses of nitric oxide donors in the therapeutic management of vertebrate animals including humans, for the prevention or alleviation of pain, especially neuropathic pain. According to some embodiments of the present invention, nitric oxide donors are administered by any suitable route so as to provide concentrations of NO that are about ½ to 10 | 12-31-2009 |
20100010053 | COMPOUNDS - The present invention relates to novel oxadiazole derivatives having pharmacological activity, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders. | 01-14-2010 |
20100016382 | PHARMACEUTICAL COMPOSITION - The present invention provides a solid pharmaceutical composition superior in the stability and dissolution property, wherein the drug dissolution property of a solid dosage form containing a fat and oil-like substance having a low melting point is improved. | 01-21-2010 |
20100016383 | 4-(3,3-DIHALO-ALLYLOXY)PHENOL DERIVATIVES HAVING PESTICIDAL PROPERTIES - Compounds of formula | 01-21-2010 |
20100022604 | PROPHYLACTIC OR THERAPEUTIC AGENT FOR ALOPECIA - Disclosed is a novel therapeutic agent which is useful for the prevention or treatment of alopecia. Specifically disclosed is a prophylactic or therapeutic agent for alopecia, which comprises 1-[2-((2S)-2-{5-[(3,4-dimethoxyphenoxy)methyl]-1,2,4-oxadiazol-3-yl}pyrrolidin-1-yl)-1,1-difluoro-2-oxoethyl]-3,3,5,5-tetramethylcyclohexanol as an active ingredient. | 01-28-2010 |
20100029727 | 1, 3, 4 -OXADIAZOLE DERIVATIVES AS DGAT1 INHIBITORS - Compounds of formula (I), or salts thereof, which inhibit acetyl CoA (acetyl coenzyme A):diacylglycerol acyltransferase (DGAT1) activity are provided, | 02-04-2010 |
20100029728 | PHOSPHODIESTERASE INHIBITORS - The present invention relates to phosphodiesterase (PDE) type IV selective inhibitors. Compounds disclosed herein can be useful in the treatment of CNS diseases, AIDS, asthma, arthritis, bronchitis, chronic obstructive pulmonary disease (COPD), psoriasis, allergic rhinitis, shock, atopic dermatitis, Crohn's disease, adult respiratory distress syndrome (ARDS), eosinophilic granuloma, allergic conjunctivitis, osteoarthritis, ulcerative colitis and other inflammatory diseases especially in humans. Processes for the preparation of disclosed compounds, pharmaceutical compositions containing the disclosed compounds, and their use as PDE type IV selective inhibitors, are provided. | 02-04-2010 |
20100029729 | COMPOUNDS - The present invention relates to novel oxadiazole derivatives having pharmacological activity, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders. | 02-04-2010 |
20100035943 | Oxa-and thiadiazoles and their use as metalloproteinase inhibitors - Compounds formula (IA) or (IB), wherein W represents HO(C═O)—, HONH(C═O)— or H(C═O)N(OH)—; X represents —O— or —S—; and R | 02-11-2010 |
20100041722 | ORGANIC COMPOUNDS - The present invention provides a compound of formula I: | 02-18-2010 |
20100048648 | Thiophene derivatives as S1P1/EDGE1 receptor agonists - The invention relates to novel thiophene derivatives, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunomodulating agents. | 02-25-2010 |
20100063115 | 5-(1,3,4-OXADIAZOL-2-YL)-1H-INDAZOLE AND 5-(1,3,4-THIADIAZOL-2-YL)-1H-INDAZOLE DERIVATIVES AS SGK INHIBITORS FOR THE TREATMENT OF DIABETES - Novel aminoindazolylurea derivatives of the formula (I), in which L, X, Y, R | 03-11-2010 |
20100087495 | PHENYL DERIVATIVES AND THEIR USE AS IMMUNOMODULATORS - The invention relates to phenyl derivatives of formula (I), their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunomodulating agents. | 04-08-2010 |
20100120874 | HETEROCYCLIC GAMMA SECRETASE MODULATORS - The invention relates to methods for the treatment of Alzheimer's disease, cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica and Down syndrome which comprise administering a therapeutically effective amount of a compound of formula I | 05-13-2010 |
20100130567 | MEDICAL AGENT FOR PREVENTION OR TREATMENT OF ALZHEIMER 'S DISEASE - A method of treating or preventing Alzheimer's disease or mild cognitive impairment which is an early state of cognitive impairment including Alzheimers' disease by administering a pharmacologically effective amount of an angiotensin II receptor blocker. A method of improving cerebral circulation or cerebral blood flow disorder by administering a pharmacologically effective amount of an angiotensin II receptor blocker. A method of treating or preventing amyloid β-induced brain disfunction by administering a pharmacologically effective amount of an angiotensin II receptor blocker. | 05-27-2010 |
20100137381 | ACETAMIDE DERIVATIVES AS POTASSIUM CHANNEL MODULATORS - This invention relates to novel acetamide derivatives that are found to be potent modulators of ion channels, in particular potassium channels and chloride channels, and, as such, are valuable candidates for the treatment of diseases or disorders as diverse as those which are responsive to the modulation of potassium channels. | 06-03-2010 |
20100173958 | COMPOUNDS FOR THE INHIBITION OF DGAT1 ACTIVITY - Compounds of formula (I), or salts thereof, which inhibit acetyl CoA(acetyl coenzyme A):diacylglycerol acyltransferase (DGAT1) activity are provided, | 07-08-2010 |
20100184813 | CHEMICAL COMPOUNDS 553 - DGAT-1 inhibitor compounds of formula (I) and pharmaceutically-acceptable salts thereof are described, together with pharmaceutical compositions, processes for making them and their use in treating, for example, obesity | 07-22-2010 |
20100190832 | Mechanism-based inhibitors of transthyretin amyloidosis: studies with biphenyl ethers and structural templates - Transthyretin (TTR), a tetrameric thyroxine (T4) carrier protein, is associated with a variety of amyloid diseases. Derivative of biphenyl ethers (BPE), which are shown to interact with a high affinity to its T4 binding site thereby preventing its aggregation and fibrillogenesis. They prevent fibrillogenesis by stabilizing the tetrameric ground state of transthyretin. Two compounds (2-(5-mercapto-[1,3,4]oxadiazol-2-yl)-phenol and 2,3,6-trichloro-N-(4H-[1,2,4]triazol-3-yl) exhibit the ability to arrest TTR amyloidosis. The dissociation constants for the binding of BPEs and compound 11 and 12 to TTR correlate with their efficacies of inhibiting amyloidosis. They also have the ability to inhibit the elongation of intermediate fibrils as well as show nearly complete (>90%) disruption of the preformed fibrils. Biphenyl ethers and compounds 11 and 12 as very potent inhibitors of TTR fibrillization and inducible cytotoxicity. | 07-29-2010 |
20100216851 | 1,2,4-OXADIAZOLE BENZOIC ACID COMPOSITIONS AND THEIR USE IN BIOASSAYS - Novel 1,2,4-oxadiazole benzoic acid compounds, methods of using and pharmaceutical compositions comprising an 1,2,4-oxadiazole benzoic acid derivative are disclosed. The methods include methods of treating or preventing a disease ameliorated by modulation of premature translation termination or nonsense-mediated mRNA decay, or ameliorating one or more symptoms associated therewith. | 08-26-2010 |
20100222398 | 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 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. | 09-02-2010 |
20100234435 | CYCLOALKYLAMINO ACID DERIVATIVES - The invention relates to compounds of formula I | 09-16-2010 |
20100240717 | NOVEL THIOPHENE DERIVATIVES AS S1P1/EDG1 RECEPTOR AGONISTS - The invention relates to thiophene derivatives of formula (I)/their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunosuppressive agents wherein: A represents *—CO—CH═CH—, *—CO—CH | 09-23-2010 |
20100240718 | NOVEL HETEROARYL-SUBSTITUTED ACETONE DERIVATIVE, SUITABLE FOR INHIBITING PHOSPHOLIPASE A2 - The present invention relates to novel heteroaryl-substituted acetone derivatives inhibiting the enzyme phospholipase A2, and pharmaceutical agents comprising said compounds. | 09-23-2010 |
20100240719 | NOVEL ALPHA-(N-SULFONAMIDO)ACETAMIDE COMPOUNDS INCORPORATING DEUTERIUM AS INHIBITORS OF BETA AMYLOID PEPTIDE PRODUCTION - The present disclosure provides novel deuterated alpha-(N-sulfonamido)acetamide compounds, their pharmaceutical composition, processes thereof and a method for the treatment of Alzheimer's disease, head trauma, traumatic brain injury, and/or dementia pugilistica and/or other conditions associated with β-amyloid peptide. | 09-23-2010 |
20100249198 | (R)-4-(HETEROARYL) PHENYLETHYL DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM - The present invention relates to a novel class of (R)-4-(heteroaryl)phenylpropionic derivatives of formula (I), useful in the inhibition of the chemotactic activation induced by the fraction C5a of complement. Said compounds are useful in the treatment of pathologies depending on the chemotactic activation of neutrophils and monocytes induced by the fraction C5a of the complement. In particular, the compounds of the invention are useful in the treatment of autoimmune hemolytic anemia (AIHA), psoriasis, bullous pemphigoid, rheumatoid arthritis, ulcerative colitis, acute respiratory distress syndrome, idiopathic fibrosis, glomerulonephritis and in the prevention and treatment of injury caused by ischemia and reperfusion. | 09-30-2010 |
20100261766 | Phenyl-Oxetanyl-Derivatives - Novel organic compounds are described and claimed which may in particular be useful in the treatment of diseases being triggered by the (human) autoimmune system. | 10-14-2010 |
20100261767 | OXADIAZOLE DERIVATIVES FOR USE AS S1P1 AGONISTS IN THE TREATMENT OF AUTOIMMUNE AND INFLAMMATORY DISORDERS - The present invention relates to novel oxadiazole derivatives having pharmacological activity, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders. | 10-14-2010 |
20100261768 | Bioavailable Compositions of Amorphous Alpha-(N-Sulfonamido)Acetamide Compound - Amorphous solid dispersion compositions containing (2R)-2-[[(4-chlorophenyl)sulfonyl][[2-fluoro-4-(1,2,4-oxadiazol-3-yl)phenyl]methyl]amino]-5,5,5-trifluoropentanamide and either polyvinylpyrrolidone-vinyl acetate or hydroxypropylmethylcellulose acetate succinate are provided for tabletting. | 10-14-2010 |
20100280082 | Metabotropic Glutamate Receptor Oxadiazole Ligands and Their Use as Potentiators - Compounds of Formula (I) wherein R | 11-04-2010 |
20100280083 | NOVEL CATECHOL DERIVATIVE, PHARMACEUTICAL COMPOSITION CONTAINING THE SAME, USE OF THE CATECHOL DERIVATIVE, AND USE OF THE PHARMACEUTICAL COMPOSITION - The present invention provides compounds represented by general formula (I): | 11-04-2010 |
20100292282 | SYNTHESIS AND CRYSTALLINE FORMS OF CB-1 ANTAGONIST/INVERSE AGONIST - The present invention relates to a process for producing crystalline 3-[(1S)-1-(1-{(S)-(4-chlorophenyl)[3-(5-oxo-4,5-dihydro-1,3,4-oxadiazol-2-yl)phenyl]methyl}azetidin-3-yl)-2-fluoro-2-methyl-propyl]-5-fluorobenzonitrile, and novel salts, solvates, hydrates and polymorphs thereof. | 11-18-2010 |
20100292283 | NOVEL PHENYL-ACETAMIDE AND PHENYL-PROPIONAMIDE DERIVATIVES USEFUL AS POTASSIUM CHANNEL MODULATORS - This invention relates to novel phenyl-acetamide and phenyl-propionamide derivatives that are found to be potent modulators of potassium channels and, as such, are valuable candidates for the treatment of diseases or disorders as diverse as those which are responsive to the modulation of potassium channels. | 11-18-2010 |
20100298388 | SUBSTITUTED BENAMIDINES AS ANTIBACTERIAL AGENTS - Compounds of formula (IA) or (IB) have antibacterial activity: wherein W is ═C(H)— or ═N—; R | 11-25-2010 |
20100324104 | 1,2,3-TRIAZOLES AS 11-BETA HYDROXYSTEROID DEHYDROGENASE TYPE I INHIBITORS - Novel compounds are provided which are 11-beta-hydroxysteroid dehydrogenase type I inhibitors. 11-beta-hydroxysteroid dehydrogenase type I inhibitors are useful in treating, preventing, or slowing the progression of diseases requiring 11-beta-hydroxysteroid dehydrogenase type I inhibitor therapy. These novel compounds of formula (I): or stereoisomers or pharmaceutically acceptable salts thereof, wherein R | 12-23-2010 |
20110039899 | Gabapentin for the Treatment of Overactive Bladder, Stress Incontinence and BPH - Use of an alpha-2-delta ligand, or a pharmaceutically acceptable derivative thereof, for the manufacture of a medicament for the treatment of LUTS, other than urinary incontinence, associated with OAB and/or BPH. | 02-17-2011 |
20110046188 | COMPOSITIONS COMPRISING NOVEL PPAR LIGANDS AND ANTI-HYPERLIPEMIC AGENTS - Methods are provided for treating or preventing conditions comprising hypertension and dyslipidemia using antihyperlipemic agents and compounds that antagonize the angiotensin II type 1 (AT1) receptor, function as partial or full activators of peroxisome proliferator activated receptors (PPARs) and lower triglycerides or elevate blood HDL-cholesterol. Compositions are provided for treating or preventing conditions comprising hypertension and dyslipidemia, comprising antihyperlipemic agents which lower triglycerides and inhibit cholesterol synthesis such as statins, and compounds that antagonize or block the angiotensin II type 1 (AT1) receptor, activate PPARs and lower triglycerides or elevate blood HDL-cholesterol such as sartans. | 02-24-2011 |
20110071199 | Thiophenyl Sulfonamides for the Treatment of Alzheimer's Disease - There is provided a series of novel α-(N-sulfonamido)acetamide compounds of the Formula (I) | 03-24-2011 |
20110077277 | ORGANIC COMPOUNDS - The present invention provides compounds of the following structure; | 03-31-2011 |
20110086893 | OXA- AND THIADIAZOLES AND THEIR USE AS METALLOPROTEINASE INHIBITORS - Compounds formula (IA) or (IB), wherein W represents HO(C═O)—, HONH(C═O)— or H(C═O)N(OH)—; X represents —O— or —S—; and R | 04-14-2011 |
20110190355 | HETEROCYCLIC INDAZOLE DERIVATIVES - Novel heterocyclic indazole derivatives of the formula (I), in which L, Q, R, X, Y, R | 08-04-2011 |
20110196002 | DIACYLGLYCEROL ACYLTRANSFERASE INHIBITORS - The present invention relates to isoxazole, thiazole and oxidiazole derivatives, processes for their preparation, pharmaceutical compositions containing them and their use as medicaments, in particular to the use of these compounds in the prevention and treatment of diseases or disorders mediated by diacylglycerol acyltransferase (DGAT), particularly DGAT1. | 08-11-2011 |
20110201658 | Pharmaceutical package - The present invention relates to a pharmaceutical package including a pharmaceutical preparation containing 2-ethoxy-1-{[2′-(5-oxo-4,5-dihydro-1,2,4-oxadiazol-3-yl)biphenyl-4-yl]methyl}-1H-benzimidazole-7-carboxylic acid (5-methyl-2-oxo-1,3-dioxol-4-yl)methyl or 2-cyclopropyl-1-{[2′-(5-oxo-4,5-dihydro-1,2,4-oxadiazol-3-yl)biphenyl-4-yl]methyl}-1H-benzimidazole-7-carboxylic acid (5-methyl-2-oxo-1,3-dioxol-4-yl)methyl or a salt thereof, and a desiccant. According to the present invention, a pharmaceutical package having a decreased uncomfortable odor is provided. | 08-18-2011 |
20110201659 | AGENT FOR PREVENTING OR TREATING ZOSTER-ASSOCIATED PAIN - The present invention relates to a pharmaceutical composition and method for preventing or treating a zoster-associated pain. The inventors found that an N-{2-[(4-substituted phenyl)amino]-2-oxoethyl}tetrahydro-2H-thiopyran-4-carboxamide compound useful as a varicella-zoster virus (VZV) unexpectedly has the effect to prevent an irreversible nerve degeneration accompanied by herpes virus infection, and therefore is also useful as an agent for preventing or treating zoster-associated pain, and thus accomplished the present invention. | 08-18-2011 |
20110207784 | OXADIAZOLE-2-OXIDES AS ANTISCHISTOSOMAL AGENTS - The invention provides 1,2,5-oxadiazole-containing compounds of Formula (I), wherein R | 08-25-2011 |
20110257232 | BIPHENYL OXADIAZOLE DERIVATIVES AS SPHINGOSINE-1-PHOSPHATE RECEPTORS MODULATORS - The present invention relates to novel biphenyl oxadiazole derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors. | 10-20-2011 |
20110263661 | 3-(4-((1H-IMIDAZOL-1-YL)METHYL)PHENYL)-5-ARYL-1,2,4-OXADIAZOLE DERIVATIVES AS SPHINGOSINE-1 PHOSPHATE RECEPTORS MODULATORS - Substituted 3-(4-((1H-imidazol-1-yl)methyl)phenyl)-5-phenyl-1,2,4-oxadiazole derivatives which are useful as sphingosine-1-phosphate modulators and useful for treating a wide variety of disorders associated with modulation of sphingosine-1-phosphate receptors. | 10-27-2011 |
20110275680 | NOXEL OXIME DERIVATIVES OF 3, 5-SECO-4-NOR-CHOLESTANE, PHARMACEUTICAL COMPOSITIONS CONTAINING SAME, AND METHOD FOR PREPARING SAME - The invention relates to novel chemical compounds, in particular oxime derivatives of 3,5-seco-4-nor-cholestane, to the application thereof as drugs, in particular cytoprotective drugs, and more particularly as neuroprotective, cardioprotective and/or hepatoprotective drugs. | 11-10-2011 |
20110288137 | SYDNONIMINES-SPECIFIC DOPAMINE REUPTAKE INHIBITORS AD THEIR USE IN TREATING DOPAMINE RELATED DISORDERS - Derivatives of Sydnonimine and its analogues, which bind selectively to dopamine transporter (DAT) proteins are useful for treating and delaying the progression of disorders and illnesses that are alleviated by inhibiting dopamine reuptake. | 11-24-2011 |
20110301208 | VIRAL AND FUNGAL INHIBITORS - Novel classes of viral and fungal inhibitors are disclosed. These compounds are useful in treating, preventing, and/or ameliorating viral infections such as, for example, Hepatitis C Virus, West Nile Virus, Dengue Virus, and Japanese Encephalitis Virus, and fungal infections such as, for example, candidiasis. | 12-08-2011 |
20120004270 | Selective Androgen Receptor Modulators - This invention provides compounds as described herein or pharmaceutically acceptable salte thereof, pharmaceutical compositions comprising a compound as described herein or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable excipient, methods of modulating the androgen receptor using the compounds or compositions described herein, methods of treating diseases beneficially treated by an androgen receptor modulator (e.g., sarcopenia, prostate cancer, contraception, type 2 diabetes related disorders or diseases, anemia, depression, and renal disease) using the compounds and compositions described herein and processes for making compounds described herein and intermediates useful in the preparation of same. | 01-05-2012 |
20120015988 | Sulfone Compounds Which Modulate The CB2 Receptor - Compounds which modulate the CB2 receptor are disclosed. Compounds according to the invention bind to and are agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain. | 01-19-2012 |
20120015989 | LINKED MYC-MAX SMALL MOLECULE INHIBITORS - Provided herein are compounds and compositions for interfering with the association of Myc and Max. These compounds and compositions are useful in methods for inhibiting growth or proliferation of a cell. Methods of inhibiting growth or proliferation of a cell comprise contacting the cell with an amount of a compound that interferes with Myc and Max association effective to inhibit growth or proliferation of the cell. | 01-19-2012 |
20120015990 | TASPASE1 INHIBITORS AND THEIR USES - Provided herein are small molecule inhibitors of Taspase1 and methods of using the small molecule inhibitors of Taspase1 to treat neoplasm in subjects in need thereof. | 01-19-2012 |
20120015991 | POLYCYCLIC ANTAGONISTS OF LYSOPHOSPHATIDIC ACID RECEPTORS - Described herein are compounds that are antagonists of lysophosphatidic receptor(s). Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists, alone and in combination with other compounds, for treating LPA-dependent or LPA-mediated conditions or diseases. | 01-19-2012 |
20120022119 | HETEROCYCLIC ANTAGONISTS OF PROSTAGLANDIN D2 RECEPTORS - Described herein are heteroaryl compounds that are antagonists of PGD | 01-26-2012 |
20120035226 | OXADIAZOLE DERIVATIVES - The invention relates to oxadiazole compounds of formula I. The compounds are useful e.g. in the treatment of autoimmune disorders, such as multiple sclerosis. | 02-09-2012 |
20120077854 | COMPOSITIONS AND METHODS FOR MODULATING RETINOL BINDING TO RETINOL BINDING PROTEIN 4 (RBP4) - The present invention relates to compositions and methods for modulating retinol binding to retinol binding protein 4 (RBP4). In particular, the present invention provides compounds having Formula (1) or (2) (Formulae (1), (2)); wherein R | 03-29-2012 |
20120142745 | NOVEL PHENYL OXADIAZOLE DERIVATIVES AS SPHINGOSINE 1-PHOSPHATE (S1P) RECEPTOR MODULATORS - The present invention relates to novel phenyl oxadiazole derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors. | 06-07-2012 |
20120172401 | BENZIMIDAZOLE DERIVATIVE AND USE AS ANGIOTENSIN II ANTAGONIST - The present invention provides (5-methyl-2-oxo-1,3-dioxol-4-yl)methyl 2-cyclopropyl-1-{[2′-(5-oxo-4,5-dihydro-1,2,4-oxadiazol-3-yl)biphenyl-4-yl]methyl}-1H-benzimidazole-7-carboxylate represented by the formula: | 07-05-2012 |
20120202856 | SUBSTITUTED BENZIMDAZOLE DERIVATIVES USEFUL AS TRPM8 RECEPTOR MODULATORS - The present invention is directed to benzimidazole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by TRP M8, including for example, inflammatory pain, inflammatory hyperalgesia, inflammatory hypersensitivity condition, neuropathic pain, neuropathic cold allodynia, inflammatory somatic hyperalgesia, inflammatory visceral hyperalgesia, cardiovascular disease aggravated by cold and pulmonary disease aggravated by cold. | 08-09-2012 |
20120238606 | AZILSARTAN ORGANIC AMINE SALTS, PREPARATION METHOD AND USE THEREOF - Azilsartan amine salts, their preparation and method of use are disclosed. Specifically, azilsartan amine salts represented by formula (I), their preparation, pharmaceutical compositions containing a therapeutically effective amount of the compounds and their use for treating hypertension are disclosed. | 09-20-2012 |
20120252853 | Positive allosteric modulators of nicotinic acetylcholine receptor - The present invention relates to compounds useful in therapy, to compositions comprising said compounds, and to methods of treating diseases comprising administration of said compounds. The compounds referred to are positive allosteric modulators (PAMs) of the nicotinic acetylcholine α7 receptor. | 10-04-2012 |
20120264792 | FURAZANOBENZIMIDAZOLES AS PRODRUGS TO TREAT NEOPLASTIC OR AUTOIMMUNE DISEASES - A compound of formula (II) | 10-18-2012 |
20120289555 | Novel S-Nitrosoglutathione Reductase Inhibitors - The present invention is directed to inhibitors of S-nitrosoglutathione reductase (GSNOR), pharmaceutical compositions comprising such GSNOR inhibitors, and methods of making and using the same. | 11-15-2012 |
20120329838 | NOVEL MODULATORS OF SPHINGOSINE PHOSPHATE RECEPTORS - Compounds that activate a sphingosine-1-phosphate receptor of the subtype 1 are provided. Certain compounds selectively activate the receptor subtype 1 in relation to the sphinogosine-1-phosphate receptor subtype 3. Uses and methods of inventive compounds for treatment of malconditions wherein activation, agonism, inhibition or antagonism of the S1P1 is medically indicated are provided. | 12-27-2012 |
20120329839 | NOVEL MODULATORS OF SPHINGOSINE PHOSPHATE RECEPTORS - Compounds that activate a sphingosine-1-phosphate receptor of the subtype 1 are provided. Certain compounds selectively activate the receptor subtype 1 in relation to the sphinogosine-1-phosphate receptor subtype 3. Uses and methods of inventive compounds for treatment of malconditions wherein activation, agonism, inhibition or antagonism of the S1P1 is medically indicated are provided. | 12-27-2012 |
20120329840 | NOVEL MODULATORS OF SPHINGOSINE PHOSPHATE RECEPTORS - Compounds that activate a sphingosine-1-phosphate receptor of the subtype 1 are provided. Certain compounds selectively activate the receptor subtype 1 in relation to the sphinogosine-1-phosphate receptor subtype 3. Uses and methods of inventive compounds for treatment of malconditions wherein activation, agonism, inhibition or antagonism of the S1P1 is medically indicated are provided. | 12-27-2012 |
20130035360 | NOVEL WATER SOLUBLE FUROXAN DERIVATIVES HAVING ANTITUMOR ACTIVITY - Water soluble compounds having a furoxan structure which are capable of inhibiting metabolic pathways involved in the development of the tumours are provided. The use of such compounds as a medicament in the therapy of the tumours and as an adjuvant in the immunotherapy protocols against neoplasms is also described. | 02-07-2013 |
20130116288 | Selective Androgen Receptor Modulators - This invention provides compounds of formulas I, Ia, Ib, Ic, Id, Ie, If or Ig or salts thereof, pharmaceutical compositions comprising a compound of formulas I, Ia, Ib, Ic, Id, If or Ig and a pharmaceutically acceptable excipient, methods of modulating the androgen receptor, methods of treating diseases beneficially treated by an androgen receptor modulator (e.g., sarcopenia, prostate cancer, contraception, type 2 diabetes related disorders or diseases, anemia, depression, and renal disease) and processes for making compounds of formulas I, Ia, Ib, Ic, Id, Ie, If or Ig and intermediates useful in the preparation of same. | 05-09-2013 |
20130116289 | 5-(BIPHENYL-4-YL)-3-PHENYL-1,2,4-OXADIAZOLYL DERIVATIVES AS LIGANDS ON THE SPHINGOSINE 1-PHOSPHATE(SIP)RECEPTORS - The present invention provides compounds of Formula (I), as selective S1P1 inhibitors, as well as their use for treating multiple sclerosis and other diseases. | 05-09-2013 |
20130131127 | METHOD OF USING DOPAMINE REUPTAKE INHIBITORS AND THEIR ANALOGS FOR TREATING DIABETES SYMPTOMS AND DELAYING OR PREVENTING DIABETES-ASSOCIATED PATHOLOGIC CONDITIONS - Method of using dopamine reuptake inhibitors, e.g., sydnonimine derivatives, for the management of diabetic symptoms and associated complications or conditions, such as hyperglycemia and diabetic neuropathy. | 05-23-2013 |
20130137733 | Di-Substituted Amides for Enhancing Glutamatergic Synaptic Responses - This invention relates to compounds, pharmaceutical compositions and methods for use in the prevention and treatment of cerebral insufficiency, including enhancement of receptor functioning in synapses in brain networks responsible for basic and higher order behaviors. These brain networks, which are involved in regulation of breathing, and cognitive abilities related to memory impairment, such as is observed in a variety of dementias, in imbalances in neuronal activity between different brain regions, as is suggested in disorders such as Parkinson's disease, schizophrenia, respiratory depression, sleep apneas, attention deficit hyperactivity disorder and affective or mood disorders, and in disorders wherein a deficiency in neurotrophic factors is implicated, as well as in disorders of respiration such as overdose of an alcohol, an opiate, an opioid, a barbiturate, an anesthetic, or a nerve toxin, or where the respiratory depression results form a medical condition such as central sleep apnea, stroke-induced central sleep apnea, obstructive sleep apnea, congenital hypoventilation syndrome, obesity hypoventilation syndrome, sudden infant death syndrome, Rett syndrome, spinal cord injury, traumatic brain injury, Cheney-Stokes respiration, Ondines curse, Prader-Willi's syndrome and drowning. In a particular aspect, the invention relates to compounds useful for treatment of such conditions, and methods of using these compounds for such treatment. | 05-30-2013 |
20130158080 | METHODS FOR TREATING HYPERTENSION IN BLACK PATIENTS - The present invention relates to methods of treating hypertension in a black patient using a therapeutically effective amount of a combination of an angiotensin II receptor blocker and chlorthalidone. | 06-20-2013 |
20130158081 | CRYSTALLINE FORMS OF 3-[5-(2-FLUOROPHENYL)-[1,2,4]OXADIAZOL-3-YL]-BENZOIC ACID - The present invention relates to crystalline forms of 3-[5-(2-fluorophenyl)-[1,2,4]oxadiazol-3-yl]-benzoic acid, pharmaceutical compositions and dosage forms comprising the crystalline forms, methods of making the crystalline forms and methods for their use for the treatment, prevention or management of diseases ameliorated by modulation of premature translation termination or nonsense-mediated mRNA decay. | 06-20-2013 |
20130217733 | ACYLBENZENE DERIVATIVE - Provided are compounds having an excellent hypoglycemic action and a β cell- or pancreas-protecting action or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition having an excellent therapeutic effect and/or prophylactic effect on type 1 diabetes, type 2 diabetes, and the like, which cause an increase in the blood sugar level due to abnormal sugar metabolism. A compound represented by general formula (I), or a pharmaceutically acceptable salt thereof, is disclosed. | 08-22-2013 |
20130225644 | MODIFIED LYSINE-MIMETIC COMPOUNDS - Lysine mimetic compounds having useful pharmacological activity such as antiarrhythmic activity and desirable bioavailability properties are disclosed. | 08-29-2013 |
20130253019 | LYSOPHOSPHATIDIC ACID RECEPTOR ANTAGONISTS FOR THE TREATMENT OF CONDITIONS OR DISEASES OF THE EYE - Described herein is the use of LPA1 antagonists in the treatment or prevention of diseases or conditions of the eye of a mammal. Also described are pharmaceutical compositions that include at least one LPA1 antagonist. | 09-26-2013 |
20130274299 | Cognition Enhancing Compounds and Compositions, Methods of Making, and Methods of Treating - The invention relates generally to muscarinic agonists, which are useful for stimulating muscarine receptors, and treating cognitive disorders. Included among the muscarinic agonists disclosed herein are oxadiazole derivatives, compositions, and preparations thereof. Methods of synthesizing oxadiazole compounds also are provided. This disclosure also relates in part to compositions for enhancing cognitive function in subjects such as humans, the compositions comprising a muscarinic agonist or a pharmaceutically suitable form thereof. This disclosure relates in part to methods of treating animals such as humans by administering such compositions. | 10-17-2013 |
20130281495 | SYDNONIMINES-SPECIFIC DOPAMINE REUPTAKE INHIBITORS AND THEIR USE IN TREATING DOPAMINE RELATED DISORDERS - Derivatives of Sydnonimine and its analogues, which bind selectively to dopamine transporter (DAT) proteins are useful for treating and delaying the progression of disorders and illnesses that are alleviated by inhibiting dopamine reuptake. | 10-24-2013 |
20130289082 | Composition and Method for Treating a Neurodegenerative Event - Disclosed is an article of manufacture featuring a support with a therapeutically effective amount of at least one fatty acid amide hydrolase (FAAH) inhibitor therein. The article has several uses and advantages including use to increase levels of at least one neurotrophin in a subject in need of such treatment. Also disclosed is a method of increasing levels of the neurotrophin in an animal by administering to a subject in need thereof at least one FAAH inhibitor. | 10-31-2013 |
20130303577 | OXADIAZOLE DERIVATIVES AS SPHINGOSINE 1-PHOSPHATE (S1P) RECEPTOR MODULATORS - The present invention relates to novel oxadiazole derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors. | 11-14-2013 |
20130331419 | MINERALOCORTICOID RECEPTOR ANTAGONISTS - Disclosed are the compounds of the Formula (I) as well as pharmaceutically acceptable salts thereof, which are useful for treating aldosterone-mediated diseases. The processes for preparing compounds of the Formula (I), the use for the therapy and prophylaxis of the abovementioned diseases and for preparing pharmaceuticals for this purpose, and the pharmaceutical compositions which comprise compounds of the formula (I) are disclosed too. | 12-12-2013 |
20140005237 | USE OF ACETYLATED TUBULIN AS A BIOMARKER OF DRUG RESPONSE TO FURAZANOBENZIMIDAZOLES | 01-02-2014 |
20140024686 | USE OF GLU-TUBULIN AS A BIOMARKER OF DRUG RESPONSE TO FURAZANOBENZIMIDAZOLES - Use of glu-tubulin as a biomarker for predicting the response to a compound, preferably resistance of a disease such as cancer in a subject to said compound, wherein the compound is a furazanobenzimidazole compound of general formula (I). | 01-23-2014 |
20140088163 | C17-HETEROARYL DERIVATIVES OF OLEANOLIC ACID AND METHODS OF USE THEREOF - Disclosed herein are novel C17-heteroaryl derivatives of oleanolic acid, including those of the formula: | 03-27-2014 |
20140100251 | 1, 2, 4-OXADIAZOLES AZETIDINE DERIVATIVES AS SPHINGOSINE-1 PHOSPHATE RECEPTORS MODULATORS - The present invention relates to 1,2,4-oxadiazoles azetidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors. | 04-10-2014 |
20140113942 | PROCESS FOR THE PREPARATION AND PURIFICATION OF AZILSARTAN MEDOXOMIL - The present invention relates to process an improved process for the preparation of azilsartan medoxomil. In particular, the field of invention relates to a process for purification of azilsartan medoxomil. More particularly, the invention relates to an improved process for preparation of azilsartan medoxomil and its pharmaceutically acceptable salts. | 04-24-2014 |
20140135365 | 2-THIO-1,3,4-OXADIAZOLES AZETIDINE DERIVATIVES AS SPHINGOSINE-1 PHOSPHATE RECEPTORS MODULATORS - The present invention relates to 2-thio-1,3,4-oxadiazoles azetidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors. | 05-15-2014 |
20140135366 | ARYL OXADIAZOLE DERIVATIVES AS SPHINGOSINE 1-PHOSPHATE (S1P) RECEPTOR MODULATORS - The present invention relates to aryl oxadiazole derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors. | 05-15-2014 |
20140155440 | CYSTEINE AND CYSTINE BIOISOSTERES TO TREAT SCHIZOPHRENIA AND REDUCE DRUG CRAVINGS - The present invention provides cysteine and cystine bioisosteres for the treatment of schizophrenia and drug addiction. The invention further encompasses pharmaceutical compositions containing such bioisosteres and methods of using the bioisosteres for treatment of schizophrenia and drug addiction. | 06-05-2014 |
20140221436 | COMPOSITIONS FOR AN ORALLY ACTIVE 1,2,4-OXADIAZOLE FOR THE TREATMENT OF DISEASE - The present invention relates to specific doses of and dosing regimens for using a 1,2,4-oxadiazole benzoic acid compound in treating or preventing diseases associated with nonsense mutations. In particular, the invention relates to specific doses and dosing regimens for the use of 3-[5-(2-fluoro-phenyl)-[1,2,4]oxadiazol-3-yl]-benzoic acid in mammals having diseases associated with nonsense mutations. | 08-07-2014 |
20140221437 | N-HETERO-RING-SUBSTITUTED AMIDE DERIVATIVE - Compounds having an excellent hypoglycemic effect and β cell- or pancreas-preserving effects or pharmaceutically acceptable salts thereof, and a pharmaceutical composition having an excellent therapeutic effect and/or prophylactic effect on type 1 diabetes, type 2 diabetes, and the like, which cause hyperglycemia due to abnormal glucose metabolism. A compound represented by general formula (I), or a pharmaceutically acceptable salt thereof, is disclosed. | 08-07-2014 |
20140235679 | CRYSTALLINE FORMS OF 3-[5-(2-FLUOROPHENYL)-[1,2,4]OXADIAZOL-3-YL]-BENZOIC ACID - The present invention relates to crystalline forms of 3-[5-(2-fluorophenyl)-[1,2,4]oxadiazol-3-yl]-benzoic acid, pharmaceutical compositions and dosage forms comprising the crystalline forms, methods of making the crystalline forms and methods for their use for the treatment, prevention or management of diseases ameliorated by modulation of premature translation termination or nonsense-mediated mRNA decay. | 08-21-2014 |
20140275185 | Novel S-Nitrosoglutathione Reductase Inhibitors - The present invention is directed to inhibitors of S-nitrosoglutathione reductase (GSNOR), pharmaceutical compositions comprising such GSNOR inhibitors, and methods of making and using the same. | 09-18-2014 |
20140275186 | NOVEL NON-STEROIDAL COMPOUNDS AS ANDROGEN RECEPTOR MODULATORS - This invention relates to novel 4,5-dihydroisoxazoles and 4,5-dihydro[1,2,4]-oxadiazoles of formula (I), to their use as androgenic or antiandrogenic agents or androgen receptor modulators, and to methods of their preparation. | 09-18-2014 |
20140296307 | POTENT ANALOGUES OF THE C-MYC INHIBITOR 10074-G5 WITH IMPROVED CELL PERMEABILITY - The present invention relates compounds and compositions for interfering with the association of Myc and Max. These compounds and compositions are useful in methods for inhibiting growth or proliferation of a cell. Methods of inhibiting growth or proliferation of a cell comprise contacting the cell with an amount of a compound that interferes with Myc and Max association effective to inhibit growth or proliferation of the cell. The compounds exhibit increased inhibitory activity against c-Myc relative to the known c-Myc inhibitor small-molecule benzofurazan N-([1,1′-biphenyl]-2-yl)-7-nitrobenzo[c][1,2,5]oxadiazol-4-amine (10074-G5). | 10-02-2014 |
20140296308 | DRUGS FOR INHIBITING P38 AND USES THEREOF - The present invention relates to compounds with a benzoxadiazolyl amine structure which are capable of inhibiting the activation or the biological activity of p38 mitogen-activated protein kinase (MAPK) and the use thereof in the treatment of a disease that can be alleviated by means of inhibiting the activation or the biological activity of said p38 MAPK, for example, an inflammatory disease or a disease presenting with pain. | 10-02-2014 |
20140309265 | MACROCYCLIC COMPOUNDS FOR INHIBITION OF INHIBITORS OF APOPTOSIS - The invention relates generally to macrocyclic compounds and their therapeutic use. More particularly, the invention relates to macrocyclic compounds that modulate the activity of inhibitors of apoptosis (IAPs) and/or are useful in the treatment of medical conditions, such as cancer. | 10-16-2014 |
20140315962 | 1,2,5-Oxadiazoles As Inhibitors Of Indoleamine 2,3- Dioxygenase - The present invention is directed to 1,2,5-oxadiazole derivatives, and compositions of the same, which are inhibitors of indoleamine 2,3-dioxygenase and are useful in the treatment of cancer and other disorders, and to the processes and intermediates for making such 1,2,5-oxadiazole derivatives. | 10-23-2014 |
20140364464 | CRYSTALLINE FORMS OF AZILSARTAN MEDOXOMIL POTASSIUM AND PREPARATION AND USES THEREOF - The present invention relates to the field of pharmaceutical chemistry. Disclosed herein is a crystalline form of azilsartan medoxomil potassium, which is substantially pure. The crystalline form is crystalline form A, form B, form C, form D, form E, form F, form G, form H, form I, form J, form K or form L. The substantially pure crystalline forms of azilsartan medoxomil potassium of the invention generally have good properties such as high solubility, high bioavailability, good stability, long shelf life and good antistatic property. The crystalline forms of azilsartan medoxomil potassium generally exhibit an excellent performance in reducing clinical systolic blood pressure (SBP) and average 24-hour SBP. Disclosed herein are methods of preparing the substantially pure crystalline forms of azilsartan medoxomil potassium, pharmaceutical compositions comprising the crystalline forms, and preparation methods and uses thereof. | 12-11-2014 |
20140371279 | CRYSTALLINE FORMS OF AZILSARTAN AND PREPARATION AND USES THEREOF - The present invention relates to the field of pharmaceutical chemistry. Disclosed herein is a crystalline form of azilsartan, which is substantially pure. The crystalline form is crystalline form A, form B, form C, form D, form E, form F, form G, form H, form I, form J or form K. The substantially pure crystalline forms of azilsartan of the invention generally have good properties such as high solubility, high bioavailability, good stability, long shelf life and good antistatic property. The crystalline forms of azilsartan generally exhibit an excellent performance in reducing clinical systolic blood pressure (SBP) and average 24-hour SBP. Disclosed herein are methods of preparing the substantially pure crystalline forms of azilsartan, pharmaceutical compositions comprising the crystalline forms, and preparation methods and uses thereof. | 12-18-2014 |
20150011594 | BIN1 EXPRESSION AS A MARKER OF CANCER - Provided are methods for screening a subject for cancer. The methods involve obtaining a blood sample from the subject and determining a level of Bridging Integrator 1 (BIND isoforms comprising exon 12a in the sample. Optionally, the method involves determining a level of 12a+/13− BIN isoform (comprising exon 12a but lacking exon 13) in the sample. An elevated level of 12a+ (e.g., 12a+/13−) BIN1 isoforms in the blood sample indicates the subject has cancer. Also provided are methods for determining efficacy of a cancer therapy in a subject and methods of treating cancer. Isolated antibodies that selectively bind human 12a+ BIN1 are also provided as well as kits for determining 12a+/13− BIN1 isoforms. | 01-08-2015 |
20150031730 | FUNGICIDAL 3-[(1,3-THIAZOL-4-YLMETHOXYIMINO)(PHENYL)METHYL]-2-SUBSTITUTED-- 1,2,4-OXADIAZOL-5(2H)-ONE DERIVATIVES - The present invention relates to 3-[(1,3-thiazol-4-ylmethoxyimino)(phenyl)methyl]-2-substituted-1,2,4-oxadiazol-5(2H)-one derivatives of formula (I), their process of preparation, their use as fungicide active agents, particularly in the form of fungicide compositions, and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions. | 01-29-2015 |
20150073024 | 1,2,4-Oxadiazole Derivatives as Immunomodulators - The present invention relates to 1,2,4-oxadiazole and 1,2,4-thiadiazole compounds as therapeutic agents capable of inhibiting the programmed cell death 1 (PD1) signaling pathway. The invention also refers to derivatives of the therapeutic agents. The invention also encompasses the use of the said therapeutic agents and derivatives for treatment of disorders via immunopotentiation comprising inhibition of immunosuppressive signal induced due to PD-1, PD-L1, or PD-L2 and therapies using them. | 03-12-2015 |
20150141474 | CYCLIC ETHER DGAT1 INHIBITORSCYCLIC ETHER DGAT1 INHIBITORS - The invention relates to compounds of formula (I): useful for treating disorders mediated by acyl coA-diacylglycerol acyl transferase 1 (DGAT1), e.g. metabolic disorders. The invention also provides methods of treating such disorders, and compounds and compositions etc. for their treatment. | 05-21-2015 |
20150148384 | A-RING EPOXIDIZED TRITERPENOID-BASED ANTI-INFLAMMATION MODULATORS AND METHODS OF USE THEREOF - Disclosed herein are novel A-ring epoxidized triterpenoid compounds and derivatives thereof, including those of the formula (I), wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits, and articles of manufacture comprising such compounds. Methods and intermediates useful for making the compounds, and methods of using the compounds, for example as antioxidant inflammation modulators, and compositions thereof are also provided. | 05-28-2015 |
20150291574 | NOVEL POLYMORPHS OF AZILSARTAN - The present invention provides a novel crystalline Form of azilsartan acid, process for its preparation and pharmaceutical compositions comprising it. The present invention also provides a novel crystalline Form of azilsartan medoxomil potassium, process for its preparation and pharmaceutical compositions comprising it. | 10-15-2015 |
20150315178 | PLASMINOGEN ACTIVATOR INHIBITOR-1 INHIBITORS AND METHODS OF USE THEREOF - The invention relates to plasminogen activator-1 (PAI-1) inhibitor compounds and uses thereof in the treatment of any disease or disorder associated with elevated PAI-1. The invention includes, but is not limited to, the use of such compounds to prevent or reduce thrombosis and fibrosis, to promote thrombolysis, and to modulate lipid metabolism and treat diseases or disorders associated with elevated PAI-1, cholesterol, or lipid levels. | 11-05-2015 |
20160002214 | ANTICANCER AGENT AND PROCESS FOR THE PREPARATION THEREOF - The present invention provides a compound of general formula A for use as a potential anticancer agent against human cancer cell lines and a process for the preparation thereof. | 01-07-2016 |
20160007607 | FUNGICIDAL 3--OXADIAZOLONE DERIVATIVES | 01-14-2016 |
20160008328 | Stable Pharmaceutical Package Comprising Azilsartan Medoxomil | 01-14-2016 |
20160045478 | Novel S-Nitrosoglutathione Reductase Inhibitors - The present invention is directed to inhibitors of S-nitrosoglutathione reductase (GSNOR), pharmaceutical compositions comprising such GSNOR inhibitors, and methods of making and using the same. | 02-18-2016 |
20160101087 | METHODS FOR DOSING AN ORALLY ACTIVE 1,2,4-OXADIAZOLE FOR NONSENSE MUTATION SUPPRESSION THERAPY - The present invention relates to specific doses of and dosing regimens for using a 1,2,4-oxadiazole benzoic acid compound in treating or preventing diseases associated with nonsense mutations. In particular, the invention relates to specific doses and dosing regimens for the use of 3-[5-(2-fluoro-phenyl)-[1,2,4]oxadiazol-3-yl]-benzoic acid in mammals having diseases associated with nonsense mutations. | 04-14-2016 |
20160185730 | DRUG FOR INHIBITING AGGREGATION OF PROTEINS INVOLVED IN DISEASES LINKED TO PROTEIN AGGREGATION AND/OR NEURODEGENERATIVE DISEASES - The present invention relates to a compound represented by formula (E). The present invention also relates to a compound represented by the formula (E) for use in the treatment or prevention of diseases linked to protein aggregation and/or neurodegenerative diseases. Moreover, the present invention relates to pharmaceutical and diagnostic compositions comprising the compound of the invention as well as to a kit. Furthermore, the present invention relates to a method of imaging deposits of aggregated protein. A kit for preparing a detectably labelled compound of the present invention is also disclosed. | 06-30-2016 |
20160193189 | CRYSTALLINE FORMS OF 3-[5-(2-FLUOROPHENYL)-[1,2,4]OXADIAZOL-3-YL]-BENZOIC ACID FOR THE TREATMENT OF DISEASE | 07-07-2016 |
20160199356 | Cognition Enhancing Compounds and Compositions, Methods of Making, and Methods of Treating | 07-14-2016 |
20160199357 | METHODS FOR THE PRODUCTION OF FUNCTIONAL PROTEIN FROM DNA HAVING A NONSENSE MUTATION AND THE TREATMENT OF DISORDERS ASSOCIATED THEREWITH | 07-14-2016 |
20180021303 | BKCA CHANNEL ACTIVATOR FOR TREATING MUSCULAR DISORDER | 01-25-2018 |
20190142806 | MODULATORS OF THE INTEGRATED STRESS PATHWAY | 05-16-2019 |
20190144402 | 1,2,4-Oxadiazole Derivatives as Immunomodulators | 05-16-2019 |