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| Number | Title | Issue Date |
| 8188124 | Talarazole metabolites Novel metabolites of talarazole of formula (I) have been isolated and characterized, wherein R═H, OH, OSO3H or O-gly; R1, ═H, OH, OSO3H, O-gly or =0; and gly=a glucuronate, or a pharmaceutically acceptable salt thereof. These com... | 05/29/2012 |
| 8183269 | Process for the preparation of rufinamide The present invention relates to a process for the preparation of rufinamide of formula I, which process comprises: (i) reacting a 2,6-difluorobenzylhalide of formula II, wherein X is chloride, bromide or iodide, with an azide to obtain 2-(azidomethyl)-1,3-difluorob... | 05/22/2012 |
| 8178077 | Drug development target protein and target gene, and method of screening The present invention provides novel target proteins and target genes for drug discovery, and the means that enable the development of novel drugs using the same. More particularly, the present invention provides NCS proteins and genes thereof; screening methods for... | 05/15/2012 |
| 8114896 | Method and composition for potentiating an opiate analgesic Composition and methods of treating pain and reducing or reversing tolerance to opiate analgesics are disclosed. The composition and method utilize an opiate analgesic and an endothelin antagonist as active agents to treat pain in mammals, including humans. ... | 02/14/2012 |
| 8110588 | 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 div... | 02/07/2012 |
| 8106077 | Compounds and methods for modulating FXR Compounds of formula (I) wherein variables are as defined herein and their pharmaceutical compositions and methods of use are disclosed as useful for treating dyslipidemia and related diseases. ... | 01/31/2012 |
| 8088801 | Aryloazol-2-yl cyanoethylamino compounds, method of making and method of using thereof The present invention relates to novel aryloazol-2-yl-cyanoethylamino derivatives of formula (I): wherein R3, R4, R5, R6, R7, P, Q, V, W, X, Y, Z and a are as defined i... | 01/03/2012 |
| 8088802 | N-phenylarylsulfonamide compound, pharmaceutical composition comprising the compound as active ingredient, synthetic intermediate for the compound and process for its preparation An N-phenylarylsulfonylamide compound of formula (I) (R1 is COOH etc.; R2 is hydrogen, methyl, etc.; R3 and R4 are a combination of methyl and methyl, etc.; R5 is isopr... | 01/03/2012 |
| 8076362 | Crystal modification A of 1-(2,6-difluorobenzyI)-1 H-1,2,3-triazole-4-carboxamide and dosage forms and formulations thereof The invention relates to dosage forms and formulations comprising the novel crystal modification A of the compound I-(2,6-difluorobenzyl)-I H-I,2,3-triazole-4-carboxamide, wherein crystal modification A is characterized by characteristic lines with interplanar spaci... | 12/13/2011 |
| 8039494 | Compositions and methods for treating diseases of the nail Methods and compositions for treating disorders of the nail and nail bed. Such compositions contain a vehicle in which all components of the composition are dissolved, suspended, dispersed, or emulsified, a non-volatile solvent, a wetting agent, and a pharmaceutical... | 10/18/2011 |
| 8017635 | Phenylalkyl substituted heteroaryl derivatives Certain novel phenylalkyl substituted azole derivatives have unexpected insecticidal activity. These compounds are represented by formula I: where A, B, D, E, G, a, b, c, d, and R through R11, inclusively, are folly described herein. In addition, composit... | 09/13/2011 |
| 8003673 | Daptomycin for the treatment of biofilm and catheter salvage Daptomycin can be used for biofilm treatment (particularly central venous catheter salvage for S. epidermidis infected catheters). Catheter salvage with daptomycin shows rapid cidality, activity against stationary phase bacteria, and penetration and activity ... | 08/23/2011 |
| 7977361 | Nitro-imidazole hypoxia imaging agent The present invention relates to novel radioactively labeled bioreducible tracers of Formula I useful for detecting hypoxic tumors or ischemic tissue in vivo. In one embodiment, the tracers consist of a 2-nitroimidazole moiety, a triazole, metabolically stable linke... | 07/12/2011 |
| 7973061 | Anaplastic lymphoma kinase modulators and methods of use The present invention relates to compounds of the Formula I, wherein L, X, Y, Z, R1, R2, R3 and R4 are defined herein. The invention also provides methods of using the compounds for inhibition of kinases, more specifically... | 07/05/2011 |
| 7964621 | Thioamide compounds, method of making and method of using thereof The present invention relates to novel thioamide derivatives of formula (I) and formula (Ia): wherein, R3, R4, R5, R6, R7, P, Q, T, V, W, X, Y, Z, a, m and n are as def... | 06/21/2011 |
| 7960417 | Benzazole potentiators of metabotropic glutamate receptors The present invention is directed to benzazole compounds which are potentiators of metabotropic glutamate receptors, including the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamat... | 06/14/2011 |
| 7960416 | Stable emulsion composition An emulsion composition comprising (1) a compound (I) represented by the formula (I) wherein each symbol is as defined in the specification (2) an anionic synthetic phospholipid in a proportion of about 0.0001 about 5% (W/V) relative to the composition in total, and... | 06/14/2011 |
| 7943644 | Stabilization of iodine-containing biocides by means of special azole compounds Specific azole compounds are outstandingly suitable for stabilizing iodine-containing biocides in industrial materials, more particularly in paints based on alkyd resin. ... | 05/17/2011 |
| 7906539 | Imidazoles and triazoles, their preparation, and their use as pharmaceutical compositions The present invention relates to imidazoles and triazoles of general formula wherein R1 to R4 and X are defined as in claims 1 to 8, the tautomers, the enantiomers, the diastereomers, the... | 03/15/2011 |
| 7897625 | Carbamoylbenzotriazole derivatives as inhibitors of lipases and phospholipases The invention relates to carbamoylbenzotriazole derivatives of general formula (I), which are defined as cited in the description, to their pharmaceutically applicable salts and to their use as medicaments. ... | 03/01/2011 |
| 7893096 | Use of small molecule compounds for immunopotentiation The invention provides immunostimulatory compositions comprising a small molecule immuno-poteniator (SMIP) compound and methods of administration thereof. Also provided are methods of administering a SMIP compound in an effective amount to enhance the immune respons... | 02/22/2011 |
| 7868028 | Guanidine compounds as anesthetics and for treatment of nervous system disorders Novel guanidine compounds having the formula in which R1, R2 and R4 are as defined, are effective as sodium channel blockers in neuronal mammalian cells and as anesthetics and/or analgesics,... | 01/11/2011 |
| 7851491 | Modified bio-related substance, process for producing the same, and intermediate A modified bio-related substance, wherein at least one poly(alkylene glycol)oxy group represented by the following formula (1) is combined in a molecule: wherein R is a hydrocarbon group having 1 to 24 carbon atoms, OA... | 12/14/2010 |
| 7838542 | Bicyclic compositions and methods for modulating a kinase cascade The invention relates to compounds of the class of 2-carboxamide substituted indoles and methods for modulating one or more components of a kinase cascade. The compounds of the invention are useful for osteoporosis, hepatitis B, opthalmic disease, diabetes, athroscl... | 11/23/2010 |
| 7834038 | Methods for preparing nonpeptidic oligomers from amino acids The present invention relates to nonpeptidic oligomers. Methods for preparing nonpeptidic oligomers from amino acids by replacing the amide bond with heterocyclic rings are also disclosed. ... | 11/16/2010 |
| 7807699 | Dimeric pyrrolidine amide-containing small molecule apoptosis promoters The invention provides small molecule mimics of the Smac peptide that are dimer- or dimer-like compounds having two amide-containing domains connected by a linker. These compounds are useful to promote apoptosis. The invention includes pharmaceutical compositions co... | 10/05/2010 |
| 7803822 | Triazole derivative and use thereof The present invention relates to a thrombin receptor antagonist containing a compound represented by the formula (I) wherein R1a, R1b and R2 are each a hydrogen atom, an optionally substitut... | 09/28/2010 |
| 7781462 | Compounds for the treatment of proliferative disorders The invention relates to compounds of structural formula (I): or a pharmaceutically acceptable salt, solvate, clathrate, and prodrug thereof, wherein Ra, Rb, and R2 ... | 08/24/2010 |
| 7750028 | Crystal modifications of 1-(2,6-difluorobenzyl)-1H-1, 2,3-triazole-4-carboxamide The invention relates to the novel modifications B and C of the compound 1-(2,6-difluorobenzyl)-1H-1,2,3-triazole-4-carboxamide of the formula its use and pharmaceutical preparations comprising this crystal modifications. | 07/06/2010 |
| 7728016 | Substituted 5-membered ring compounds and their use Compound of a compound of formula (I) or a salt, N-oxide, hydrate or solvate thereof, in the preparation of a composition for inhibition of HSP90 activity: wherein ring A is an aromatic or non-aromatic carbocyclic or heterocyclic ring having 5 ring atoms, for exampl... | 06/01/2010 |
| 7709508 | Estrogen receptor modulators The present invention relates to compounds and derivatives thereof, their synthesis, and their use as estrogen receptor modulators. The compounds of the instant invention are ligands for estrogen receptors and as such may be useful for treatment or prevention of a v... | 05/04/2010 |
| 7696237 | Agents for combating plant pests The present invention relates to compositions for controlling plant pests containing the compound of formula (I) in a mixture with fungicidally active compounds. ... | 04/13/2010 |
| 7691886 | Benzimidazole derivatives as raf kinase inhibitors The present invention relates to benzimidazole derivatives of formula I, the use of the compounds of formula I as inhibitors of one or more kinases, the use of the compounds of formula I for the manufacture of a pharmaceutical compositions and methods of treatment, ... | 04/06/2010 |
| 7687526 | Benzo-fused compounds for use in treating metabolic disorders The present invention provides compounds useful, for example, for treating metabolic disorders in a subject. Such compounds have the general formula I: where the definitions of the variables | 03/30/2010 |
| 7659293 | α-Amino-N-hydroxy-acetamide derivatives The invention relates to α-amino-N-hydroxy-acetamide derivatives of formula I, wherein R is di-lower alkyl amino, 1,2,3-triazol-1-yl, 1,2,3-triazol-2-yl or 1,2,4-triazol-4-yl, m represents an integer from 1 up to and in... | 02/09/2010 |
| 7652043 | WNT pathway antagonists Aromatic compounds for treating various diseases and pathologies are disclosed. The methods use of such compounds are also provided. Accordingly, the present invention makes available methods and compositions for inhibiting aberrant growth states in cells having Wnt... | 01/26/2010 |
| 7629369 | N-phenylarylsulfonamide compound, pharmaceutical composition comprising the compound as active ingredient, synthetic intermediate for the compound and process for its preparation An N-phenylarylsulfonylamide compound of formula (I) (R1 is COOH etc.; R2 is hydrogen, methyl, etc.; R3 and R4 are a combination of methyl and methyl, etc.; R5 is isopr... | 12/08/2009 |
| 7598279 | Neurotherapeutic azole compounds Azole compounds containing carbamoyl group and pharmaceutically useful salts thereof are described. The compounds are effective anticonvulsants which are used in the treatment of disorders of the central nervous system, especially as anxiety, depression, convulsion,... | 10/06/2009 |
| 7538128 | Dipeptidyl peptidase IV inhibitors, process for their preparation and compositions containing them The present invention relates to novel compounds useful as dipeptidyl peptidase IV (DPP-IV) inhibitors of the formula: wherein X, Y, a, R1, and R2 are as defined herein. ... | 05/26/2009 |
| 7531560 | Anti-cytokine heterocyclic compounds Disclosed are compounds of formula (I) which inhibit production of cytokines involved in inflammatory processes and are thus useful for treating diseases and pathological conditions involving inflammation such as chronic in... | 05/12/2009 |