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| Number | Title | Issue Date |
| 8080668 | Thiazoles derivatives as AMPK activator The present application provides novel thiazole derivatives that are useful as activators of Adenosine 5′-Monophosphate-Activated Protein Kinase and pharmaceutical compositions containing such compounds. ... | 12/20/2011 |
| 8080559 | 5(S)-(2′-hydroxyethoxy)-20(S)-camptothecin and its preparation and use for the treatment of cancer A 5(S)-(2′-hydroxyethoxy)-20(S)-camptothecin diasterisomer is described which is a better inhibitor of topoisomerase I than either the diastereoisomeric mixture 5(RS)-(2′-hydroxyethoxy)-20(S)-camptothecin, or the 5(R)-(2′-hydroxyethoxy)-20(S)-camptothecin dias... | 12/20/2011 |
| 8063074 | Polymorphic forms of esomeprazole sodium Polymorphic crystalline Forms J, K, L, M, and N of esomeprazole sodium. ... | 11/22/2011 |
| 8058438 | Eszopiclone process Eszopiclone is prepared by reacting zopiclone with an enatiomerically pure di-p-toluoyl tartaric acid, recovering a solid salt, and reacting a solid salt with a base. Zopiclone is prepared by reacting 6-(5-chloropyrid-2-yl)-5-hydroxy-7-oxo-5,6-dihydropyrrolo[3,4-b]-... | 11/15/2011 |
| 8053000 | Compositions for drug delivery Substantially non-porous polymeric microparticles comprising a hydrophobic polymer and a plasticizer, and containing therein a bioactive or bioinactive agent. ... | 11/08/2011 |
| 8049021 | Process for the preparation of fluorotetraene There is provided a process for preparing 21-acetyloxy-6-alpha-fluoro-pregna-1,4,9(11),16-tetraene-3,20-dione compound of Formula I, which comprises reacting 21-acetyloxy-pregna-1,3,5,9(11),16-pentaene-3-oxo acetate with a fluorinating agent. ... | 11/01/2011 |
| 8039619 | Process for preparing (2R,3S/2S,3R)-2-(2,4-difluorophenyl)-3-(5-fluoropyrimidin-4-yl)-1-(1H-1,2,4-triazol-1-yl)butan-2-ol Voriconazole is prepared by a process comprising condensing 1-(2,4-difluorophenyl)-2-(1H-1,2,4-triazole-1-yl)ethanone with 4-chloro-6-ethyl-5-fluoropyrimidine, in a ketone, ether, aliphatic hydrocarbon, or aromatic hydrocarbon solvent, to give (2R,3S/2S,3R)-3-(4-chl... | 10/18/2011 |
| 8013181 | Preparation of rivastigmine and its salts There are provided processes for making rivastigmine. In one embodiment, the process includes reacting S-(−)-[1-(3-hydroxyphenyl)ethyl]dimethylamine with N-ethyl-N-methyl carbamoyl chloride in the presence of an organic base to obtain a free base of rivastigmine. | 09/06/2011 |
| 8008340 | 3-arylthioindole-2-carboxamide derivatives and analogs thereof as inhibitors of casein kinase I A method for inhibiting casein kinase Iε activity, comprising administering to said patient a therapeutically effective amount of a compound of formula I. its stereoisomer, enantiomer, racemate, ta... | 08/30/2011 |
| 8008328 | Methods for the treatment of diabetes-associated dyslipdemia Methods for the treatment of insulin resistance, diabetes, and/or diabetes associated dyslipidemia by administering niacin and meloxicam are disclosed. ... | 08/30/2011 |
| 8003820 | Process for preparing bisphosphonic acids A process for preparing a bisphosphonate compound comprises reacting a carboxylic acid with a phosphonating agent, in a cresol solvent. ... | 08/23/2011 |
| 7989463 | Biccyclic compounds as GATA modulators Novel bicyclic compounds of the formula (I), stereoisomers, and/or pharmaceutically acceptable salts of the novel bicyclic compounds, and/or pharmaceutically acceptable salts of the stereoisomers of the novel bicyclic compounds are provided. Additionally, methods of... | 08/02/2011 |
| 7977478 | Polymorphic forms of vardenafil Crystalline polymorphic forms of vardenafil and vardenafil hydrochloride, and processes for preparing them. ... | 07/12/2011 |
| 7943781 | Process for preparing telmisartan A process comprising cyclizing 3-amino-4-butyramido-5-methylbenzoic acid to form 2-n-propyl-4-methyl-benzimidazole-6-carboxylic acid. ... | 05/17/2011 |
| 7939513 | Tetracycline derivatives as antibacterial agents In accordance with one aspect, the present invention provides a compound of general formula (I), its stereoisomers thereof and/or its pharmaceutically acceptable salts thereof, which have antibacterial activity; with methods of treating infectious diseases in warm b... | 05/10/2011 |
| 7935841 | Bisphospholanes for use as catalysts in asymmetric reactions The invention concerns an enantiomerically enriched compound of formula (1) or the opposite enantiomer thereof wherein each of Ar1—Ar4 represent the same or different aromatic groups of up to 20 carb... | 05/03/2011 |
| 7919633 | Process for preparation of celecoxib There is provided a process for preparation of celecoxib by reacting 4,4,4-trifluoro-1-[4-(methyl)phenyl]butane-1,3-dione with 4-sulphonamidophenylhydrazine or its salt in a solvent medium that contains an alkyl ester. There is also provided a process for the purifi... | 04/05/2011 |
| 7879889 | Therapeutic use of acylaminothiazole derivatives The present invention discloses and claims therapeutic uses of a compound corresponding to the general formula (I): Wherein, X, R1, R2, R3, R4, R5, R5′, R | 02/01/2011 |
| 7875646 | Derivatives of N-[(1,5-diphenyl-1H-pyrazol-3-yl)methyl] sulfonamide, their preparation and their application in therapeutics The present invention relates to compounds corresponding to the formula (I): In which R1, R2, R3, R4 and R5 are as described herein. The invention also relates to the m... | 01/25/2011 |
| 7868007 | Triazolopyridine carboxamide derivatives, preparation thereof and therapeutic use thereof The invention relates to the triazolopyridine carboxamide derivatives of general formula (I): Wherein X, A, R1 and R2 are as defined herein. The invention further relates to preparation methods and the... | 01/11/2011 |
| 7863279 | Triazolopyridine carboxamide derivatives and triazolopyrimidine carboxamide derivatives, preparation thereof and therapeutic use thereof The invention relates to the triazolopyridine carboxamide derivatives and triazolopyrimidine carboxamide derivatives of general formula (I): Wherein X, A, R1 and R2 are as defined herein. The invention... | 01/04/2011 |
| 7838547 | Aryl-substituted polycyclic amines, method for the production thereof, and use thereof as a medicament The invention relates to aryl-substituted polycyclic amines of formula I, especially bicyclic amines, and to the physiologically tolerated salts and physiologically functional derivatives thereof; where the symbols and radi... | 11/23/2010 |
| 7824919 | Method for analyzing activated polyethylene glycol compounds A chemical analysis method for the determination of RO(CH2CH2O)nH, RO(C2H4O)nA, and AO(C2H4O)nA in a mixture thereof, wherein R is an alkyl group, A is a functional gr... | 11/02/2010 |
| 7816484 | Method for making polyethylene glycol carbonates A method for preparing a polyalkylene glycol carbonate is disclosed comprising reacting a hydroxyl functional polyalkylene glycol and a reagent selected from carbonates and chloroformates in the presence of an aromatic solvent and an amine. ... | 10/19/2010 |
| 7803763 | Method of purifying preproinsulin The invention relates to a method for the chromatographic purification of preproinsulins, in which higher molecular weight substances are removed from an aqueous solution of preproinsulin by a first chromatography on an anion exchanger in flow-through mode and a sub... | 09/28/2010 |
| 7795289 | Use of acylaminothiazole derivatives as therapeutic agents This invention discloses and claims a method of treatment of a disease as defined herein using a compound conforming to the general formula (I): Wherein R1, R2, R′2, R3, R4... | 09/14/2010 |
| 7786104 | N-(aminoheteroaryl)-1H-indole-2-carboxamide derivatives, and preparation and therapeutic application thereof The invention concerns compounds of general formula (I): Wherein n, X1, X2, X3, X4, Y, Z, Z1, Z2, Z3 and Z4 are as defined herein. The ... | 08/31/2010 |
| 7781590 | Piperidinylalkylcarbamate derivatives, methods for their preparation and the therapeutic use thereof as fatty acid amido hydrolase enzyme inhibitors The present invention comprises peridinylalkylcarbamate derivatives, methods for their preparation and the therapeutic use thereof as fatty acid amido hydrolase (FAAH) enzyme inhibitors. These derivatives exert various pharmacological activities by interacting, inte... | 08/24/2010 |
| 7781477 | Therapeutic use of -(1-Indolyl)-1-indole-2-carboxamide derivatives The invention relates to therapeutic use of compounds of general formula (I): in which X1, X2, X3, X4, X5, Z1, Z2, Z3, Z4 an... | 08/24/2010 |
| 7781471 | Diaryl triazolmethylamine derivatives, preparation and therapeutic use thereof The invention concerns compounds of formula (I): Wherein X, R1, R2, R3 and R4 are as described herein. The invention also concerns a method for preparing same and the therapeutic ... | 08/24/2010 |
| 7781440 | Use of substituted 2-pyrimidinyl-6,7,8,9-tetrahydropyrimido[1,2-] pyrimidin-4-one and 7-pyrimidinyl-2,3-dihydroimidazo[1,2-] pyrimidin-5(1)one derivatives The invention relates to use of a pyrimidone derivative represented by formula (I) or a salt thereof as therapeutic agents: Wherein m, n, p, X, Y, R1, R2, R3, R4 R5, are as defined herein. The invention specifically relates... | 08/24/2010 |
| 7777057 | Derivatives of dioxan-2-alkyl carbamates, preparation thereof and application thereof in therapeutics A compound corresponding to general formula (I): in which R1 represents a phenyl or naphthalenyl group optionally substituted with one or more halogen atoms or hydroxyl, cyano, nitro, (C1-C3... | 08/17/2010 |
| 7777042 | N-sulfonylpipecolic acid derivative FKBP binding composition and pharmaceutical use thereof A composition for binding FKBP proteins is disclosed, along with a method of treating conditions associated with neuronal degeneration, wherein said composition comprises a compound of formula I, wherein, R, R1, ... | 08/17/2010 |
| 7763636 | N-(arylalkyl)-1H-pyrrolopyridine-2-carboxamide derivatives, preparation and therapeutic use thereof The invention concerns compounds of general formula (I), wherein n, the pyrrolopyridine ring, X, Z1, Z2, Z3, Z4, Z5 and W are as defined herein. The invention also concer... | 07/27/2010 |
| 7759377 | Acylaminothiazole derivatives and use thereof as beta-amyloid inhibitors Compounds of formula (I) as defined herein: inhibit the formation of the β-amyloid peptide (β-A4) and are, therefore, useful in the treatment of pathologies in which a β-amyloid peptide (β-A4) formation inhibitor provid... | 07/20/2010 |
| 7759366 | Arylaminoaryl-alkyl-substituted imidazolidine-2,4-diones, process for preparing them, medicaments comprising these compounds, and their use This invention relates to arylaminoaryl-alkyl-substituted imidazolidone-2,4-diones of formula (I) and also to their physiologically tolerated salts: Wherein R, R′, R1 to R10, A, D, E, G, L and p are as defined herein. The... | 07/20/2010 |
| 7745467 | -(heteroaryl)-1-heteroarylalkyl-1-indole-2-carboxamide derivatives, preparation and therapeutic use thereof The invention concerns compounds of general formula (I), wherein n, X1, X2, X3, X4, Y and W are as defined herein. The invention also concerns a method for preparing said compound... | 06/29/2010 |
| 7741493 | Heterocyclic compounds as P2X7 ion channel blockers The present invention relates to a novel series of 4,5-diphenyl-2-amino-4,5-dihydro-imidazole derivatives of the formula II: wherein R, R1, R2, R3, R4, R5, X and Y are ... | 06/22/2010 |
| 7741491 | Diphenylamine-substituted salicylthiazole derivatives and related compounds as phosphotyrosine phosphatase 1B (PTB1B) inhibitors for using as blood-sugar decreasing active ingredients for treating diabetes The invention therefore relates to compounds of the formula I in which the variables are as defined in the specification, to pharmaceutical compositions containing them and to their use for therapeutically lowering blood gl... | 06/22/2010 |
| 7741363 | 3-Acylindole derivatives, preparation and therapeutic use thereof The invention relates to compounds of formula (I), wherein X, R1, R2, R3, R4 and R5 are as described herein. The invention also includes preparative methods for the pre... | 06/22/2010 |
