Tue, 26 May 2015 08:00:00 EDTThe invention relates to the use of compounds comprising at least one 2-(1H-tetrazol-5-yl)pyridine unit, of formula (I) below: as ligands for lanthanides and, more especially, as organic chromophores for complexing these elements. It also relates to lanthanide complexes using these compounds as complexing organic chromophores, and to new compounds containing one or more 2-(1H-tetrazol-5-yl)pyridine units, which are useful as ligands for lanthanides and, in particular, as organic chromophores for complexing these elements.Applications: photonics and optoelectronics, especially for forming light-emitting devices such as electroluminescent diodes; biology, as for example for the preparation of luminescent probes.
Tue, 26 May 2015 08:00:00 EDTThe process of the present invention relates to a method for the synthesis of a 1,4-diphenylazetidinone of formula (VIII) by using novel oxime intermediates.
Tue, 26 May 2015 08:00:00 EDTThe present invention provides novel porphyrin derivatives represented by the general formula 1 and/or pharmaceutically acceptable derivatives thereof as NIR sensitizers for photodynamic therapeutic and diagnostic, biological and industrial applications. These porphyrin derivatives possess absorption (400-700 nm) and emission (600-750 nm) in the regions where biological chromophores do not absorb and hence are ideal candidates for application as NIR PDT agents and fluorescence sensors for medicinal applications in biology. The substituents like hydroxyl and glycolic units on these dyes render them amphiphilicity thereby improving their solubility in the aqueous media and cellular uptake and localization. These dyes show no toxicity in the dark and are highly selective towards tumor cells and stain nucleus very rapidly. Accordingly, these porphyrin derivatives are extremely useful as NIR PDT fluorescence sensors in photodynamic therapeutic and diagnostic, biological and industrial applications.
Tue, 26 May 2015 08:00:00 EDTInhibitors of HCV replication of formula (I) and the N-oxides, salts, and stereoisomers, whereineach dashed line represents an optional double bond;X is N, CH and where X bears a double bond it is C;R1 is —OR7, —NH—SO2R8;R2 is hydrogen, and where X is C or CH, R2 may also be C1-6alkyl;R3 is hydrogen, C1-6alkyl, C1-6alkoxyC1-6alkyl, C3-7cycloalkyl;R4 is aryl or Het; n is 3, 4, 5, or 6;R5 is halo, C1-6alkyl, hydroxy, C1-6alkoxy, phenyl, or Het;R6 is C1-6alkoxy, or dimethylamino;R7 is hydrogen; aryl; Het; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl, aryl or with Het;R8 is aryl; Het; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl, aryl or with Het;aryl is phenyl optionally substituted with one, two or three substituents;Het is a 5 or 6 membered saturated, partially unsaturated or completely unsaturated heterocyclic ring containing 1 to 4 heteroatoms selected from nitrogen, oxygen and sulfur, and being optionally substituted with one, two or three substituents; pharmaceutical compositions containing compounds (I) and processes for preparing compounds (I). Bioavailable combinations of the inhibitors of HCV of formula (I) with ritonavir are also provided.
Tue, 26 May 2015 08:00:00 EDTThe present invention is concerned with novel antifungal 5,6-dihydro-4H-pyrrolo-[1,2-a][1,4]benzodiazepines and 6H-pyrrolo[1,2-a][1,4]benzodiazepines substituted with bicyclic benzene derivatives of Formula (I) wherein R1, R2, R3, R4, R5, R6 and R7 have the meaning defined in the claims. The compounds according to the present invention are active mainly against dermatophytes and systemic fungal infections. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.
Tue, 26 May 2015 08:00:00 EDTThe present invention is concerned with novel antifungal 5,6-dihydro-4H-pyrrolo-[1,2-a][1,4]benzodiazepines and 6H-pyrrolo[1,2-a][1,4]benzodiazepines of Formula (I) wherein R1, R2, R3, R4, R5 and R6 have the meaning defined in the claims. The compounds according to the present invention are active mainly against dermatophytes and systemic fungal infections. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.
Tue, 26 May 2015 08:00:00 EDTThe present invention provides compounds of the formula: which are useful as inhibitors of PHD and pharmaceutical compositions thereof.
Tue, 26 May 2015 08:00:00 EDTStable noribogaine salt ansolvates are useful for preparing pharmaceutical compositions and for alleviating nociceptive pain in a patient. Such ansolvates can be prepared by slurrying solvated forms, preferably MeOH solvated noribogaine hydrochloride in EtOH/water.
Tue, 26 May 2015 08:00:00 EDTThis disclosure is directed to fused tetracyclic pyrido[4,3-b>]indole and pyrido[3,4-b]indole derivatives. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.
Tue, 26 May 2015 08:00:00 EDTCompounds of Formula I and methods for treating metabolic disorders are disclosed.
Tue, 26 May 2015 08:00:00 EDTThis invention relates to novel compounds which are inhibitors of acyl coenzymeA: diacylglycerol acyltransferase 1 (DGAT-1), to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy for the prevention or treatment of diseases related to DGAT-1 dysfunction or where modulation of DGAT-1 activity may have therapeutic benefit including but not limited to obesity, obesity related disorders, hypertriglyceridemia, hyperlipoproteinemia, chylomicronemia, dyslipidemia, non-alcoholic steatohepatitis, diabetes, insulin resistance, metabolic syndrome, hepatitis C virus infection and acne or other skin disorders.
Tue, 19 May 2015 08:00:00 EDT25-desacetyl rifaximin or a pharmaceutically acceptable salt thereof is provided. Methods of treatment of bowl related disorders using isolated and/or purified 25-desacetyl rifaximin or a pharmaceutically acceptable salt thereof are also provided.
Tue, 19 May 2015 08:00:00 EDTThe invention concerns the production of quinoline compounds containing sulfonic acid groups, the said quinoline compounds and their conversion into dyes containing sulfonic acid groups. The dyes according to the invention are used especially to label analytes, for example to label biomolecules.
Tue, 19 May 2015 08:00:00 EDTThe present invention relates to Rifaximin polymorphic, salt, hydrate, and amorphous forms, to their use in medicinal preparations and to therapeutic methods using them.
Tue, 19 May 2015 08:00:00 EDTThe invention pertains to compound of Formula (I) wherein X, Y, Z, R1, R2, R3, R4, A and A′ are as described hereinabove. Formula (I) and (II) compounds can be used in pharmaceutical compositions, useful for the treatment of diseases.
Tue, 19 May 2015 08:00:00 EDTThe invention relates to 17-(1′-propenyl)-17-3′-oxidoestra-4-en-3-one derivatives with the general chemical formula I, where the residues Z, R4, R6a, R6b, R7, R15, R16a, R16b and R18 have the meanings stated in Claim 1, and their solvates, hydrates and salts, including all stereoisomers of these compounds. The invention further relates to the use of these derivatives for the production of a medicinal product for oral contraception and for the treatment of pre-, peri- and postmenopausal complaints and medicinal products that contain said derivatives, and in particular application in the aforementioned indications. The derivatives according to the invention have a progestational and in preferred cases additionally an antimineralocorticoid and neutral to slightly androgenic action.
Tue, 19 May 2015 08:00:00 EDTAn object is to overcome the drawbacks of conventional blue phthalocyanine pigments upon the formation of images, and to develop a blue pigment that can satisfactorily exhibit a greenish blue color high in chroma and excellent in colorfulness, brightness, dispersibility, hue, tinting power and the like and that is applicable to various image recording methods. The object can be achieved by a greenish blue pigment, which exhibits a greenish blue hue of high chroma and contains a pigment represented by the following formula (I): wherein the number, m, of substituent phthalimidomethyl group(s) is in a range of 1.0≦m≦5.0, and the number, n, of a substituent sulfonic group R1 is in a range of 0.05≦n≦1.0.
Tue, 12 May 2015 08:00:00 EDTThis invention relates to: (a) compounds and salts thereof that, inter alia, treat pain; (b) intermediates useful for the preparation of such compounds and salts; (c) compositions comprising such compounds and salts; (d) methods for preparing such intermediates, compounds, salts, and compositions; (e) methods of use of such compounds, salts, and compositions; and (f) kits comprising such compounds, salts, and compositions.
Tue, 12 May 2015 08:00:00 EDTThis invention relates to novel pyrazolopyrimidines and their use as metabotropic glutamate 5 receptor antagonists (mGlu5 receptor antagonists), pharmaceutical compositions containing the same, and methods of using the same as agents for treatment or amelioration of mGlu5 receptor mediated disorders.
Tue, 12 May 2015 08:00:00 EDTA composition having BACE 1 inhibitory activity containing a compound represented by the formula (I): wherein ring A is an optionally substituted carbocyclic group or an optionally substituted heterocyclic group;E is lower alkylene;X is S, O, or NR1;R1 is a hydrogen atom or lower alkyl;R2a, R2b, R3a, R3b, R4a, and R4b, is each independently a hydrogen atom, halogen, or hydroxyl etc.;n and m are each independently an integer of 0 to 3;n+m is an integer of 0 to 3;R5 is a hydrogen atom or substituted lower alkyl;its pharmaceutically acceptable salt or a solvate thereof.
Tue, 12 May 2015 08:00:00 EDTSubstituted indazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification; the compounds of the invention may be useful in therapy in the treatment of diseases associated with a deregulated protein kinase activity, like cancer.
Tue, 12 May 2015 08:00:00 EDTIn certain embodiments, the invention is directed to composition comprising stable particles comprising ganaxolone, wherein the volume weighted median diameter (D50) of the particles is from about 50 nm to about 500 nm.
Tue, 05 May 2015 08:00:00 EDTThe invention relates to pharmaceutically acceptable salts of amphiphilic photosensitizing agents which have a water solubility of at least 0.5 mg/ml and to their use in methods of photochemical internalization. Such salts may be formed from a pharmaceutically acceptable base, for example an organic amine such as an amino alcohol, or from a pharmaceutically acceptable acid, for example a sulphonic acid or a sulphonic acid derivative. Due to their increased water solubility, such salts are particularly suitable for use in the preparation of parenteral pharmaceutical preparations, e.g. for use as solutions for injection or infusion.
Tue, 05 May 2015 08:00:00 EDTThe present invention provides a novel process for the preparation of 7-chloro-2,3,4,5-tetrahydro-1H-1-benzazepin-5-one. The present invention also provides an improved process for the preparation of 7-chloro-1-(2-methyl-4-nitrobenzoyl)-5-oxo-2,3,4,5-tetrahydro-1H-1-benzazepine. The present invention further provides an improved process for the preparation of 7-chloro-1-[2-methyl-4-[(2-methylbenzoyl)amino]benzoyl]-5-oxo-2,3,4,5-tetrahydro-1H-1-benzazepine.
Tue, 05 May 2015 08:00:00 EDTThis disclosure concerns a new family of phosphorus-containing compounds of Formula (I): and pharmaceutically acceptable derivatives thereof. Compositions containing such compounds and uses thereof are also provided.
Tue, 05 May 2015 08:00:00 EDTProvided is a method for purifying rocuronium bromide, which comprises: formulating crude rocuronium bromide to be purified into an aqueous solution, distilling off excess residue solvents at reduced pressure, absorbing by adding active carbon or silica gel, then filtrating, quick freezing the filtrate into ice, and then lyophilizing to obtain rocuronium bromide.
Tue, 05 May 2015 08:00:00 EDTThe present invention relates to a benzodiazepine compound of formula (I), processes for its preparation, pharmaceutical compositions containing such a compound and to its use in therapy.
Tue, 05 May 2015 08:00:00 EDTInhibitors of HCV replication of formula (I) and the N-oxides, salts, or stereoisomers thereof, wherein the dashed line, X, R1, R2, R3, R4, R5, R6, and R7 have defined meanings; the preparation thereof; compositions containing compounds of formula (I), including bioavailable combinations with ritonavir; and the pharmaceutical uses thereof.
Tue, 28 Apr 2015 08:00:00 EDTA method for preparing temsirolimus, the method including: using a substituted aromatic aldehyde to protect 2,2-dimethylol propionic acid to produce intermediate II; carrying out reaction between the intermediate II and 2,4,6-trichlorobenzoyl chloride; carrying out condensation reaction between a resulting product and rapamycin to produce intermediate III; and finally using sulfuric acid to remove a protecting group from the intermediate III to yield temsirolimus.
Tue, 28 Apr 2015 08:00:00 EDTA macrocycle based on β-diketimines, a process for preparing the inventive macrocycle, an uncharged macrocyclic dimetallic complex based on the inventive macrocycle, and a process for preparing the uncharged macrocyclic dimetallic complex, the use of the uncharged macrocyclic dimetallic complex as a polymerization catalyst in the polymerization of carbon dioxide with one or more epoxides, a process for preparing polycarbonates by reacting carbon dioxide with one or more epoxides in the presence of the inventive uncharged macrocyclic dimetallic complex, and a polycarbonate prepared by the process according to the invention.
Tue, 28 Apr 2015 08:00:00 EDTThe present invention is directed to methods for preparation of a composition comprising mixed crystalline polymorphs rifaximin α and rifaximin β. For example, practice of a method of the invention can provide the composition comprising mixed crystalline polymorphs rifaximin α and rifaximin β wherein the rifaximin β is present in about 3-12% (w/w) or is present in about 5-8% (w/w). The composition comprising mixed crystalline polymorphs rifaximin α and rifaximin β is prepared by dissolving raw rifaximin in a water-soluble organic solvent, for example ethanol, at reflux, then adding water to achieve a final mixed solvent of about 7:3 (v/v) solvent to water ratio, then cooling to 35-40° C. until crystallization commences, then further cooling with stirring to 0° C., then recovery of the crystallized material, and drying to a water content of between 2.5% and 5.0%, to provide the composition comprising mixed crystalline polymorphs rifaximin α and rifaximin β. The composition is suitable for medicinal use, such as in treatment of infections of the gastrointestinal tract.
Tue, 28 Apr 2015 08:00:00 EDTChemical entities that are bufalin derivatives, pharmaceutical compositions and methods of treatment of cancer are described.
Tue, 28 Apr 2015 08:00:00 EDTPorphyrin compounds are provided. The compounds may further comprise a fused polycyclic aromatic hydrocarbon or a fused heterocyclic aromatic. Fused polycyclic aromatic hydrocarbon s and fused heterocyclic aromatics may extend and broaden absorption, and modify the solubility, crystallinity, and film-forming properties of the porphyrin compounds. Additionally, devices comprising porphyrin compounds are also provided. The porphyrin compounds may be used in a donor/acceptor configuration with compounds, such as C60.
Tue, 21 Apr 2015 08:00:00 EDTThe invention relates to a method for producing manganese complex compounds of the general formula (1), wherein M, X, L, z, Y and q are defined as in claim 1. The method is characterized by the following steps: a) reacting one or more bivalent metal salts with the ligand L in water as the solvent to form a coordination compound from the one or more bivalent metal salt and the ligand L, the one or more bivalent metal salts being selected from bivalent manganese salts and iron salts and at least one bivalent metal salt being a bivalent manganese salt, b) oxidizing the coordination compound of step a) with an oxidant while at the same time maintaining a pH of 11 to 14, to transform the metal M from the bivalent to the trivalent and/or tetravalent form, c) reducing the pH of the reaction mixture to a pH of 4 to 9 and removing any metal oxides or metal hydroxides of the metal M formed and d) adding, at a pH of 4 to 9, a salt of the formula MezYq, wherein Me represents an alkali metal ion, ammonium ion or an alkanol ammonium ion, and Y, z and q are defined as in formula (1).
Tue, 21 Apr 2015 08:00:00 EDTDisclosed is a method of preparing an amino acid ester of maytansinol by reacting maytansinol with an N-carboxyanhydride of an amino acid (NCA) in the presence of a drying agent. Also disclosed is an improved method of preparing an amino acid ester of maytansinol in which a nucleophile is added to the reaction mixture after completion of the reaction between maytansinol and an N-carboxyanhydride of an amino acid.
Tue, 21 Apr 2015 08:00:00 EDTProvided is a crystalline form E of ertapenem sodium. Further provided is a method for preparing a crystalline form E of ertapenem sodium, characterized by using an aqueous ertapenem sodium solution at a low concentration as a raw material. The crystalline form E can be easily filtered and dried, the properties in the drying process are stable, and the purity of the crystal is high and can be up to 98.5% or higher.
Tue, 21 Apr 2015 08:00:00 EDTA method to produce uretonimine-modified isocyanate composition comprises Providing an organic isocyanate composition having two or more isocyanate groups;Reacting, in the presence of a suitable catalyst, said polyisocyanate composition to form uretonimine-modified isocyanate composition comprising carbodiimide groups and uretonimine groups;terminating said reacting by the addition of an amount of oxalic acid mono alkyl ester halide.
Tue, 21 Apr 2015 08:00:00 EDTCompounds of formula I: or salts thereof are disclosed. Also disclosed are pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I and therapeutic methods for treating a Retroviridae viral infection including an infection caused by the HIV virus.
Tue, 14 Apr 2015 08:00:00 EDTThe invention relates to compounds of formula (I) wherein R1, R2, X1, X2, Y, Ra, Rb, Q have the meanings given in claim 1. The compounds are useful e.g. in the treatment of autoimmune disorders, such as multiple sclerosis and also in the treatment of cancer disorders.
Tue, 14 Apr 2015 08:00:00 EDTThe invention concerns a new process for the resolution of ivabradine and of intermediates of synthesis thereof.
Tue, 14 Apr 2015 08:00:00 EDTThe invention provides a process of preparing 4-amino-4-oxobutanoyl peptides and cyclic analogues thereof of Compound I and pharmaceutically acceptable salts thereof.
Tue, 14 Apr 2015 08:00:00 EDTThe present invention relates to an improved process for oxidizing 3-hydroxy-methyl-cephem derivatives to the corresponding 3-formyl-cephem derivatives. In particular this oxidation process is for the preparation of 7-[2-(5-amino-[1,2,4]thia-diazol-3-yl)-2-hydroxyimino-acetylamino]-3-formyl-8-oxo-5-thia-1-aza-bicyclo[4.2.0]oct-2-ene-2-carboxylic acid derivatives of formula (I) using a combination of a hypervalent iodine oxidizing agent of the type 10-I-3 such as bis(acetoxy)iodo-benzene (BAIB) and a catalyst such as 2,2,6,6-tetramethyl-1-piperidinyloxy (TEMPO). These compounds of formula (I) are intermediates in the synthesis of ceftobiprole.
Tue, 14 Apr 2015 08:00:00 EDTProvided herein is a method for the synthesis of cephalosporin antibiotic compounds comprising the conversion of a protected 7-amino group into a 7-carboxamide moiety in a single step.
Tue, 14 Apr 2015 08:00:00 EDTThe present invention is directed to novel organometallic complexes as catalysts for the reaction of compounds with isocyanate and hydroxyl functional groups to form urethane and/or polyurethane and the process employing such catalysts. More particularly, the present invention is directed to novel complexes of zinc(II) with substituted amidines. These novel catalysts are useful for the production of urethanes and polyurethanes which are important in many industrial applications.
Tue, 14 Apr 2015 08:00:00 EDTThe invention relates to novel oxindole derivatives of general formula (I), wherein the substituents R1, R2, A, B, and Y are defined as in claim 1. The invention further relates to medicaments containing said derivatives, and use thereof for the prevention and/or treatment of vasopressin-dependent diseases.
Tue, 14 Apr 2015 08:00:00 EDTDescribed herein are α3 or α2 or α2/α3 GABAergic receptor subtype selective ligands, pharmaceutical compositions, and methods of use of such ligands and compositions in treatment of anxiety disorders, epilepsy and schizophrenia with reduced sedative and ataxic side effects. In embodiments, such as α3 or α2 or α2/α3 GABAergic receptor subtype selective ligands lack ester linkages and may be thus relatively insensitive to hydrolysis by esterases.
Tue, 14 Apr 2015 08:00:00 EDTA compound represented by the formula (I) or a pharmaceutically acceptable salt thereof: wherein Z represents nitrogen atom or C—X; X represents hydrogen atom or fluorine atom; R1 is hydrogen atom or a C1-C3 alkyl group; L represents single bond or a C1-C6 alkylene group which may be substituted; Y represents single bond, sulfur atom, oxygen atom, NH, or the like; R2 represents hydrogen atom or a cyclic group which may be substituted, which is used for preventive and/or therapeutic treatment of a disease caused by abnormal activity of tau protein kinase 1 such as a neurodegenerative diseases (e.g. Alzheimer disease).
Tue, 14 Apr 2015 08:00:00 EDTThe present invention provides novel cephalotaxus esters, syntheses thereof, and intermediates thereto. The invention also provides pharmaceutical compositions comprising a compound of the present invention and methods of using said compounds or compositions in the treatment of proliferative diseases (e.g., benign neoplasm, cancer, inflammatory disease, autoimmune disease, diabetic retinopathy) and infectious disease. The invention further provides methods of using said compounds or compositions in the treatment of multidrug resistant cancer.
Tue, 14 Apr 2015 08:00:00 EDTCompounds of Formula (I), their preparation and use in preventing or treating bacterial infections are disclosed.
Tue, 07 Apr 2015 08:00:00 EDTThe present invention relates to a process for the preparation of pure meropenem trihydrate.