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| Number | Title | Issue Date |
| 8173652 | Isoxazole-isoxazoles and isoxazole-isothiazoles The present invention is concerned with isoxazole-isoxazoles and isoxazole-isothiazoles of formula I, having affinity and selectivity for GABA A α5 receptor, their manufacture, pharmaceutical compositions containing them and their use as cognitive enhancers or for ... | 05/08/2012 |
| 8163747 | Acid addition salts, hydrates and polymorphs of 5-(2,4-dihydroxy-5-isopropyl-phenyl)-4-(4-morpholin-4-ylmethyl-phenyl)-isoxazole-3-carboxylic acid ethylamide and formulations comprising these forms The present invention relates to new salt forms of 5-(2,4-dihydroxy-5-isopropyl-phenyl)-4-(4-morpholin-4-ylmethyl-phenyl)-isoxazole-3-carboxylic acid ethylamide, in particular the mesylate, hydrochloride, tartrate, phosphate and hemi fumarate salt thereof; to crysta... | 04/24/2012 |
| 8148374 | Modulators of pharmacokinetic properties of therapeutics The present application provides for a compound of Formula IV, or a pharmaceutically acceptable salt, solvate, and/or ester thereof, compositions containing such compounds, therapeutic methods that include the administratio... | 04/03/2012 |
| 8138185 | 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 composit... | 03/20/2012 |
| 8138184 | Isoxazole derivatives and pharmaceutical compositions comprising the same An isoxazole derivative is provided. The isoxazole derivative has following formula: wherein R1, R2, R3, R4 and R5, independently, include hydr... | 03/20/2012 |
| 8129378 | Substituted oxazolidinones and their use in the field of blood coagulation The invention relates to the field of blood coagulation. Novel oxazolidinone derivatives of the general formula (I) processes for their preparation and their use as medicinally active compounds for the prophylaxis and/or tr... | 03/06/2012 |
| 8101609 | Processes for the preparation of rivaroxaban and intermediates thereof This invention provides a process for the preparation of S-Rivaroxaban and/or R-Rivaroxaban comprising reacting, in the presence of a first base, a compound of Formula 9: with a compound of Formula 8: | 01/24/2012 |
| 8088771 | Cycloalkylidene and heterocycloalkylidene inhibitor compounds The present invention provides a compound of general Formula (I) having histone deacetylase (HDAC) inhibitory activity, a pharmaceutical composition comprising the compound, and a method useful to treat diseases using the compound. | 01/03/2012 |
| 8088770 | Modulators of pharmacokinetic properties of therapeutics The present application provides for a compound of Formula IV: or a pharmaceutically acceptable salt, solvate, and/or ester thereof, compositions containing such compounds, therapeutic methods that include the administratio... | 01/03/2012 |
| 8030303 | Salt of morpholine compound (2S)-[4-(Carboxymethyl)thiazol-2-ylthio]-N-{[4-(3,4-dichlorobenzyl)morpholin-2-yl]methyl}acetamide hydrobromide and a crystal thereof, which resist easy weight change caused by vapor sorption as compared to a free form, and are superior as drug substances of pharmac... | 10/04/2011 |
| 8012971 | Therapeutic agent for chronic obstructive pulmonary disease Disclosed is a method for the prevention and/or treatment of a chronic obstructive pulmonary disease by administrating a 5-membered cyclic compound represented by the formula below: or a pharmaceutically acceptable salt of ... | 09/06/2011 |
| 7994166 | Pyrrolidinone benzenesulfonamide derivatives as modulators of ion channels for the treatment of pain The present invention relates to pyrrolidinone benzenesulfonamide derivatives useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions i... | 08/09/2011 |
| 7989450 | Functionalized diarylisoxazoles inhibitors of ciclooxygenase Isoxazole derivatives, in particular diarylisoxazole derivatives inhibitors of cyclooxygenase (COX), in particular cyclooxygenase-1 (COX-1), their pharmaceutical compositions, the process for their preparation and their use for the chemoprevention and treatment of i... | 08/02/2011 |
| 7985750 | Substituted oxazolidinone derivatives This invention relates to novel compounds that are substituted oxazolidinones derivatives and pharmaceutically acceptable salts thereof. More specifically, this invention relates to novel oxazolidinones compounds that are derivatives of rivaroxaban. The invention al... | 07/26/2011 |
| 7960380 | Non-anilinic derivatives of isothiazol-3(2H)-one 1,1-dioxides as liver X receptor modulators The present invention relates to certain novel compounds of the formula (I) to processes for preparing such compounds, to their the utility in modulation of nuclear hormone receptors Liver X Receptor (LXR) α (NR1H3) and/or β (NR1H2) and in treating and/or preventi... | 06/14/2011 |
| 7960379 | Therapeutic compounds Compounds comprising or a pharmaceutically acceptable salt or a prodrug thereof, are disclosed, wherein J1, J2, B, Y, A and D are as described. Methods, compositions, and medicaments related th... | 06/14/2011 |
| 7956055 | Substituted gamma lactams as therapeutic agents A compound having the formula or a pharmaceutically acceptable salt or a prodrug thereof is disclosed herein. Y, A, U, and B are as described herein. Methods, compositions, and medicaments related to these compounds... | 06/07/2011 |
| 7935700 | Morpholine compound A compound represented by the formula (1) wherein ring A is aryl optionally having substituent(s) and the like; ring B is arylene optionally having substituent(s) and the like; m=0-2; n=1-5; X is a bond and the like; Y is a... | 05/03/2011 |
| 7816355 | Processes for the preparation of rivaroxaban and intermediates thereof This invention provides a process for the preparation of S-Rivaroxaban and/or R-Rivaroxaban comprising reacting, in the presence of a first base, a compound of Formula 9: with a compound of Formula 8: | 10/19/2010 |
| 7790720 | Compounds comprising an oxazole or thiazole moiety, processes for making them, and their uses The present invention relates to compounds comprising an oxazole or thiazole moiety of formula (I), processes for preparing them, pharmaceutical compositions comprising said compounds and their uses as H3-receptor ligands, Formula (I), wherein, A1 | 09/07/2010 |
| 7786117 | Therapeutic substituted thiazolidinones, oxazolidinones, and related compounds Compounds comprising or a pharmaceutically acceptable salt or a prodrug thereof, are disclosed, wherein J, B, Y, G and A are as described. Methods, compositions, and medicaments related thereto are also di... | 08/31/2010 |
| 7723333 | Non-anilinic derivatives of isothiazol-3(2H)-one 1,1-dioxides as liver X receptor modulators The present invention relates to certain novel compounds of the formula (I) to processes for preparing such compounds, to their the utility in modulation of nuclear hormone receptors Liver X Receptor (LXR) α (NR1H3) and/or... | 05/25/2010 |
| 7671051 | Inhibitors of 11-β-hydroxy steroid dehydrogenase type 1 The present invention relates to compounds with the formula (I) and also to pharmaceutical compositions comprising the compounds, as well as to the use of the compounds in medicine and for the preparation of a medicament whic... | 03/02/2010 |
| 7608619 | Substituted oxazole compounds with analgesic activity Substituted oxazole derivatives corresponding to formula I: a method for producing such compounds, pharmaceutical compositions containing such compounds, and the use of such compounds to treat pain, depression, urinary inco... | 10/27/2009 |
| 7592339 | Substituted oxazolidinones and their use in the field of blood coagulation The invention relates to the field of blood coagulation. Novel oxazolidinone derivatives of the general formula (I) processes for their preparation and their use as medicinally active compounds for the prophylaxis and/or tr... | 09/22/2009 |
| 7585860 | Substituted oxazolidinones and their use in the field of blood coagulation The invention relates to the field of blood coagulation. Novel oxazolidinone derivatives of the general formula (I) processes for their preparation and their use as medicinally active compounds for the prophylaxis and/or tr... | 09/08/2009 |
| 7585859 | PDE4B inhibitors and uses therefor Compounds active on phosphodiesterase PDE4B are provided. Also provided herewith are compositions useful for treatment of PDE4B-mediated diseases or conditions, and methods for the use thereof. ... | 09/08/2009 |
| 7582629 | Derivatives of isothiazol-3(2)-one 1,1-dioxides as liver X receptor modulators The present invention relates to certain novel compounds of the formula (I) to processes for preparing such compounds, to their the utility in modulation of nuclear hormone receptors Liver X Receptor (LXR) α (NR1H3) and/or β (NR1H2) and in treating and/or preventi... | 09/01/2009 |
| 7429588 | Crystalline isoxazole derivative and medical preparation thereof Crystalline 3-[(1S)-1-(2-fluorobiphenyl-4-yl)ethyl]-5-{[amino(morpholin-4-yl)methylene]amino}-isoxazole that exhibits the following angle of diffraction (2θ) and relative intensity in a powder X-ray diffraction pattern, is very easy to handle and stable in a proces... | 09/30/2008 |
| 7407976 | Thiazoles and oxazoles useful as modulators of ATP-Binding Cassette transporters The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to meth... | 08/05/2008 |
| 7361676 | Solid preparation containing single crystal form There are provided a solid preparation containing a single crystal of 2-(3-cyano-4-isobutyloxyphenyl)-4-methyl-5-thiazolecarboxylic acid, an excipient and a disintegrating agent, and a method for producing the same. ... | 04/22/2008 |
| 7354919 | Isoxazole compositions useful as inhibitors of ERK Described herein are compounds that are useful as protein kinase inhibitors, especially inhibitors of ERK, having the formula: where A, B, R1, R2, T and Ht are described in the specification. The compo... | 04/08/2008 |
| 7348348 | Aryl-link-aryl substituted thiazolidine-dione and oxazolidine-dione as sodium channel blockers Aryl-link-aryl thiazolidine-dione and aryl-link-aryl oxazolidine-dione compounds are sodium channel blockers; pharmaceutical compositions that include an effective amount of the aryl-link-aryl thiazolidine-dione and aryl-link-aryl oxazolidine-dione compounds and a p... | 03/25/2008 |
| 7332602 | Pyridyl substituted heterocycles useful for treating or preventing HCV infection The present invention relates to pyridyl substituted heterocycles and hydro isomers thereof and pharmaceutical compositions thereof that inhibit replication and/or proliferation of HCV virus. The present invention also relates to the use of the pyridyl heterocycles ... | 02/19/2008 |
| 7329765 | Benzothiophene compounds having antiinfective activity Benzothiophene compounds such as are DNA binding compounds exhibiting antibacterial activity. ... | 02/12/2008 |
| 7304050 | Antibacterial agents Compounds of formula I and methods for their preparation are disclosed. Further disclosed are methods of making biologically active compounds of formula I as well as pharmaceutically acceptable compositions comprising compounds of formula I. Compounds of formula I a... | 12/04/2007 |
| 7291614 | Processes for the preparation of linezolid intermediate The present invention provides improved methods of converting R—N-(4-morpholiyl-3-fluorophenyl)-2-oxo-5-oxazolidinyl-methyl azide (III) to the intermediate S—N-(4-morpholinyl-3-fluorophenyl)-2-oxo-5-oxazolidinyl-methyl amine (II) that involve the production of f... | 11/06/2007 |
| 7282501 | Modulators of peroxisome proliferator activated receptors (PPAR) The present invention is directed to a compound of formula I, and pharmaceutically acceptable salts, solvates, hydrates or stereoisomer thereof, which are useful in treating Syndrome X, Type II diabetes, hyperglycemia, hyperlipidemia, obesity, coagaulopathy, hyperte... | 10/16/2007 |
| 7271289 | Biphenylcarboxylic amide derivatives as p38 kinase inhibitors Compounds of formula (I): or pharmaceutically acceptable derivatives thereof, and their use as pharmaceuticals, particularly as p38 kinase inhibitors. ... | 09/18/2007 |
| 7259171 | Di and trifluoro-triazolo-pyridines anti-inflammatory compounds The present invention relates to novel triazolo-pyridines of the formula I wherein R1 is fluoro; s is an integer from two to three; R2 is (C3-C6)cycloalkyl ... | 08/21/2007 |
