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SANDOZ AG

SANDOZ AG Patent applications
Patent application numberTitlePublished
20120136015PROCESS FOR PREPARATION OF ENDOTHELIAL RECEPTOR ANTAGONIST (BOSENTAN) - The present invention relates to processes for the preparation of an endothelial receptor antagonist. The present invention particularly relates to synthesis of 4-tert-butyl-N-[6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)-2-(2-pyrimidinyl)-4-pyrimidinyl]benzene sulfonamide (bosentan).05-31-2012
20120122993PHARMACEUTICAL COMPOSITION CONTAINING 1H-INDEN-1-AMINE, 2,3-DIHYDRO-N-2-PROPYNYL-(1R)-, METHANESULFONATE - A pharmaceutical composition comprising as an active ingredient a therapeutically effective amount of R(+)-N-propargyl-1-aminoindan mesylate thereof, and less than 50% by weight of hexahydric sugar alcohols.05-17-2012
20120116070METHOD FOR THE PRODUCTION OF CEFTOBIPROLE MEDOCARIL - The present invention relates to a method for the production of organic compounds, in particular sodium (6R,7R)-7-[(Z)-2-(5-amino-[1,2,4]thiadiazol-3-yl)-2-hydroxyimino-acetylamino]-8-oxo-3-[(E)-(R)-1′-(5-methyl-2-oxo-[1,3]-dioxol-4-ylmethoxycarbonyl)-2-oxo-[1,3′]bipyrrolidinyl-3-ylidenemethyl]-5-thia-1-aza-bicyclo[4.2.0]oct-2-ene-2-carboxylate (ceftobiprole medocaril), and compounds of the general formula (1) and of the general formula (2), the compounds themselves and intermediates in the production according to the invention.05-10-2012
20120108807METHOD FOR THE PRODUCTION OF CEFTOBIPROLE MEDOCARIL - The present invention relates to a method for the production of organic compounds, in particular sodium (6R,7R)-7-[(Z)-2-(5-amino-[1,2,4]thiadiazol-3-yl)-2-hydroxyimino-acetylamino]-8-oxo-3-[(E)-(R)-1′-(5-methyl-2-oxo-[1,3]-dioxol-4-ylmethoxycarbonyl)-2-oxo-[1,3′]bipyrrolidinyl-3-ylidenemethyl]-5-thia-1-aza-bicyclo[4.2.0]oct-2-ene-2-carboxylate (ceftobiprole medocaril), and compounds of the general formula (1) and of the general formula (2), the compounds themselves and intermediates in the production according to the invention.05-03-2012
20120107869ORGANIC COMPOUNDS - Disclosed is a method for the production of a heterologous polypeptide of interest with a homogenous N-terminus, using a fusion polypeptide comprising the polypeptide of interest and N-terminally thereto a polypeptide exhibiting autoproteolytic function, said method comprising the steps of a) binding of the fusion polypeptide in a soluble, autoproteolytically inactive form by an affinity chromatography system, b) refolding of the fusion polypeptide, thereby activating the autoproteolytic function of the fusion polypeptide and causing cleavage of the heterologous polypeptide of interest, and c) subsequently eluting the heterologous polypeptide of interest, wherein said steps are conducted on one affinity chromatography system.05-03-2012
20120101277CRYSTALLINE FORM OF POSACONAZOLE - The present invention relates to crystalline form II-S, its preparation and its use to prepare other crystalline forms of posaconazole, in particular crystalline form IV of posaconazole.04-26-2012
20120088808CRYSTAL FORMS OF SAXAGLIPTIN - The present invention relates to novel polymorphic forms of Saxagliptin Hydrochloride. The present invention also relates to methods of making polymorphic forms of Saxagliptin Hydrochloride.04-12-2012
20120042613Long-Term Storage of Non-Glycosylated Recombinant Human G-CSF - The present invention provides a method for stable long-term storage of non-glycosylated recombinant human G-CSF, wherein an aqueous acetate or glutamate buffered G-CSF composition containing non-glycosylated recombinant human G-CSF and sorbitol is cooled to a temperature of −15° C. or below to obtain a frozen G-CSF composition, which frozen composition is then stored in the frozen state. The temperature of the frozen G-CSF composition is later increased to a temperature within the range of from 2° C. to 8° C. for a time selected to allow the G-CSF composition to thaw and to obtain a liquid G-CSF composition having a G-CSF content of at least 95% of the G-CSF content of the original composition.02-23-2012
20120022025CRYSTALLINE FORM C OF TIGECYCLINE DIHYDROCHLORIDE AND METHODS FOR ITS PREPARATION - The present invention relates to crystalline form C of Tigecycline dihydrochloride and to methods for the preparation of the same. Furthermore the present invention relates to the use of crystalline form C of Tigecycline dihydrochloride as an intermediate for the preparation of an anti-infective medicament. Moreover the present invention relates to pharmaceutical compositions comprising crystalline form C of Tigecycline dihydrochloride in an effective amount and to the use of crystalline form C of Tigecycline dihydrochloride as an anti-infective medicament.01-26-2012
20110319867METHOD AND DEVICE FOR ORAL APPLICATION OF A COMPOSITION - The invention relates to a device for oral application of a composition. The device comprises recess having an outer rim encompassing the recess. Within the recess, a composition is arranged. The composition comprises a gelling agent and an active agent. A cover member is attached to the rim and completely covers the recess. Thus, the cover member, together with the recess, retains the composition within the recess. The cover member has an outer surface opposed to an inner surface adjoining the recess. In order to allow preparation of the composition by adding water without the risk of losing some of the composition during preparation, the cover member comprises one or more openings for providing fluidic connection between the inner surface and the outer surface. Through this opening, water can enter for preparing the composition meanwhile the cover retains all composition within the recess. The invention further relates to a method for manufacturing the device. The solid composition is introduced into the recess and the cover member is attached to the rim. The method further comprises to provide the cover member with one or more openings. The openings are adapted for providing fluidic connection between the inner surface and the outer surface of the cover member.12-29-2011
20110306764CRYSTALLINE FORM OF AN ORGANIC COMPOUND - The present invention is directed to a crystalline form of 2-[6-[3(R)-aminopiperidin-1-yl]-3-methyl-2,4-dioxo-1,2,3,4-tetrahydropyrimidin-1-ylmethyl]-benzonitrile, a process for the preparation of said crystalline form and the use thereof in the manufacture of a pharmaceutical composition.12-15-2011
20110190502PROCESS FOR THE PREPARATION OF S-CLOPIDOGREL - A process for the preparation of (S)-Clopidogrel free base or a pharmaceutically acceptable salt thereof by the racemization of the undesired (R)-Clopidogrel in the presence of a suitable base followed by resolution with camphor sulfonate salt and further treatment with an inorganic acid to yield the title compound.08-04-2011
20110178340IMPROVED PROCESS FOR THE PRODUCTION OF BIMATOPROST - The present invention relates to a process for the purification of crude bimatoprost to obtain pure bimatoprost comprising a chromatography, preferably a chromatography using an achiral stationary phase and an eluent comprising an alcohol and an apolar solvent; and crystallisation of the product obtained the chromatography to obtain pure bimatoprost.07-21-2011
20110174653CAPSULE WITH SOLUBLE BLOCKING ELEMENT - The invention relates to a capsule comprising an inlet and an outlet connected by a passage, in which a dissolvable blocking element and a composition to be orally administered are arranged. The blocking element is fluid permeable and, in a non-dissolved condition, is arranged in the passage to block delivery of the composition to an outlet of the passage. The invention further relates to a method for releasable sealing a capsule comprising a composition to be orally administered, comprising the steps of providing the composition chamber in a passage and filling composition into the composition chamber. The passage formed by the capsule is occluded with a blocking element and the blocking element comprises dissolvable material and has a fluid permeable structure.07-21-2011
20110165636PROCESS FOR THE STEREOSELECTIVE ENZYMATIC HYDROLYSIS OF 5-METHYL-3-NITROMETHYL-HEXANOIC ACID ESTER - The present invention relates to processes for the preparation of 5-methyl-3-nitromethyl-hexanoic acid ester and its salts. Also disclosed are processes for the preparation of 5-methyl-3-nitromethyl-hexanoic acid salt and a process for the preparation of 3-(aminomethyl)-5-methylhexanoic acid. (S)-5-Methyl-3-nitromethyl-hexanoic acid or (R)-5-methyl-3-nitromethyl-hexanoic acid in enantioenriched form or enantiopure form as well as salts thereof, (S)-5-methyl-3-nitromethyl-hexanoic acid ester or (R)-5-methyl-3-nitromethyl-hexanoic acid ester in enantioenriched form or enantiopure form and a compound, namely Formula (XIII), in racemic form, enantioenriched form or enantiopure form are also disclosed.07-07-2011
20110137035PREPARATION OF MICROBIOLOGICALLY PRODUCED ERGOT ALKALOIDS - The present invention relates to a method for preparing microbiologically produced ergot alkaloids of the following formula (I), comprising the step of: a) extracting the fermentation product occurring during the biological production, said product containing at least one ergot alkaloid of formula (I), at a pH of 8-14 using an extractant with a solubility in water of 0.2 g/100 g of water to 25 g/100 g water at 20° C., wherein the amount of extractant is sufficient to form a 2-phase system together with the fermentation product.06-09-2011
20110124893ANTIBIOTIC COMPOUNDS - The present invention relates to the new crystalline solid form XI of Tigecycline and a process of preparing the same. Form XI of Tigecycline is particularly suitable for the isolation of Tigecycline in the last step of the synthesis of Tigecycline. Further the present invention relates to a process of preparing amorphous Tigecycline by spray drying form XI or another crystalline form of Tigecycline.05-26-2011
20110124575METHOD FOR PROCESSING MICROBIOLOGICALLY PRODUCED CYCLIC OLIGOPEPTIDES - The present invention relates to a method for processing microbiologically produced, non-polar, cyclic oligopeptides comprising the step of a) extracting the entire fermentation broth incident to the microbiological production process using a liquid extractant that contains ether and is immiscible with water, wherein the amount of extractant is sufficient to form a two-phase system together with the total fermentation broth, and novel solvates of cyclosporin A and methyl-t-butyl ether.05-26-2011
20110105772CRYSTALLINE FORMS OF TIGECYCLINE HYDROCHLORIDE - The present invention relates to crystalline forms A and B of Tigecycline hydrochloride and to methods for the preparation of the same. Furthermore the present invention relates to the use of crystalline forms A and B of Tigecycline hydrochloride as intermediates for the formulation of an anti-infective medicament. Moreover the present invention relates to pharmaceutical compositions comprising crystalline form A of Tigecycline hydrochloride in an effective amount and to the use of crystalline form A of Tigecycline hydrochloride as anti-infective medicament.05-05-2011
20110105525PHARMACEUTICAL COMPOSITIONS CONTAINING A CRYSTALLINE FORM OF POSACONAZOLE - The present invention relates to a pharmaceutical composition comprising crystalline form Y of posaconazole. The pharmaceutical composition can be used to treat or prevent fungal infections.05-05-2011
20110065722A CRYSTALLINE FORM OF POSACONAZOLE - The present invention relates to crystalline form IV of posaconazole and pharmaceutical compositions comprising the same. The pharmaceutical composition can be used to treat or prevent fungal infections.03-17-2011
20110045531METHOD FOR PRODUCING A RECOMBINANT PROTEIN ON A MANUFACTURING SCALE - A method for producing a protein of interest on a manufacturing scale is based on integration, by homologous recombination, of the DNA encoding the protein of interest into a bacterial cell genome at a pre-selected site. The manufacturing scale production of recombinant proteins is in the fed-batch mode, semi-continuous or in a chemostat.02-24-2011
20110040078PROCESS FOR THE PRODUCTION OF TELITHROMYCIN - The present invention relates to a process for the preparation of erythromysin derivatives, in particular telithromycin of formula (I) and its pharmaceutically acceptable salts, providing the isolated intermediates in crystalline form of superior stability and purity.02-17-2011
20110015191ORGANIC COMPOUNDS - Novel polymorph form III of Aprepitant and a method for preparation of novel form III is disclosed. New processes for the preparation of Aprepitant form II are disclosed. The processes involve transformation of form III to form II by heating in decalin and the precipitation of form II from a solvent or solvent mixture by cooling and/or addition of addition of seed crystals or an anti solvent. Solid dispersions containing Aprepitant form II in a suitable carrier are disclosed. A process for the preparation of the solid dispersion by evaporation of a solution of Aprepitant and the carrier in a suitable solvent is disclosed. Stable Aprepitant form II is disclosed. Further pharmaceutical compositions containing Aprepitant form II, III or solid dispersions containing Aprepitant form II in a suitable carrier are disclosed. A methanol solvate of Aprepitant is disclosed.01-20-2011
20110009648Carbonyl Asymmetric Alkylation - This invention relates to processes and intermediates for the stereoselective alkylation of carbonyl groups. The invention in particular allows the stereoselective preparation of the antidepressant drug escitalopram. It has been found that boric or boronic acid derivatives are useful bridging elements for the attachment of a chiral group to a compound containing a carbonyl group to be alkylated. The said borates and boronates are thus useful in a process for the asymmetric alkylation of a carbonyl group in a compound containing a carbonyl group and an anchor group capable of reacting with a boric or boronic acid derivative. The asymmetric alkylation can be carried out by admixing the compound containing a carbonyl group to be alkylated and the anchor group capable of reacting with a boric or boronic acid derivative with a boric or boronic acid derivative, adding a chiral alcohol, and adding an organometallic compound. After the alkylation reaction, the borate and boronate can be easily removed by hydrolysis.01-13-2011
20110009629PREPARATION OF MORPHOLINE DERIVATIVES - This invention relates to processes and intermediates for the stereoselective morpholine derivatives. The invention in particular allows the stereoselective preparation of the drugs aprepitant and fosaprepitant.01-13-2011
20100151035PHARMACEUTICAL COMPOSITIONS OF POORLY SOLUBLE DRUGS - The present invention relates to a stable pharmaceutical composition of a poorly water-soluble drug with a view to increasing its solubility and bioavailability. The present invention relates to a solid dispersion of a poorly water-soluble drug.06-17-2010
20100063473DEVICE FOR THE ORAL APPLICATION OF A SUBSTANCE - A device for oral application of a substance, comprising an inner tube surrounding a first volume an outer tube surrounding a second volume, the second volume comprising a cavity section adjoining an inlet opening of the outer tube being adapted for containing the substance, a separation area arranged in the second volume, the separation area adjoining the cavity section and the first volume, and a selective connecting passage between the cavity section and a pressure compensation space to selectively enable a flow of the substance from the cavity section though the first volume. A kit-of-parts, comprises the inventive device a predefined amount of a substance being contained in a receptacle or the cavity section, and instructions for the use of the substance. Methods for filling the inventive device as well as to a method for oral application using the inventive device are provided.03-11-2010
20100010239Process for the Production of Prostaglandins and Prostaglandin Analogs - The present invention relates to an improved process for the production of prostaglandins and prostaglandin analogs. In particular, this invention relates to the production of prostaglandins of the PGF01-14-2010
20090203069Organic compounds - Disclosed is a method for the production of a heterologous polypeptide of interest with a homogenous N-terminus, using a fusion polypeptide comprising the polypeptide of interest and N-terminally thereto a polypeptide exhibiting autoproteolytic function, said method comprising the steps of a) binding of the fusion polypeptide in a soluble, autoproteolytically inactive form by an affinity chromatography system, b) refolding of the fusion polypeptide, thereby activating the autoproteolytic function of the fusion polypeptide and causing cleavage of the heterologous polypeptide of interest, and c) subsequently eluting the heterologous polypeptide of interest, wherein said steps are conducted on one affinity chromatography system.08-13-2009
20090186865Lyophilization Process - An improved process for the production of lyophilized Piperacillin alone or in combination with Tazobactam with improved pH adjustment, by degassing the solution of products to a controlled low carbon dioxide content prior to lyophilization.07-23-2009
20090162897Promoter Sequences - The present invention relates to methods for producing polypeptides or nucleic acids, in particular antisense RNA and hairpin RNA in filamentous fungi. The present invention also relates to isolated 06-25-2009
20090149508Process for the preparation of substituted phenyl ether compounds - A novel process for the preparation of a compound of the formula (II), which is useful as intermediate compound for the preparation of thiazolidinedione derivatives, such as rosiglitazone, pioglitazone, troglitazone and ciglitazone, is disclosed.06-11-2009
20090099370Crystalline Form of Perindopril Erbumine - The present invention relates to new crystalline form of the ACE inhibitor perindopril and processes for the preparation thereof.04-16-2009
20080319162Process and Intermediates for the Synthesis of Caspofungin - The present invention relates to novel processes for preparing certain aza cyclohexapeptide compounds, e.g. caspofungin, novel intermediates used in said processes and a process for preparing said intermediates. In particular, the intermediates have formula (II), wherein X is amino or substituted amino and contains a cyano/nitrile functionality.12-25-2008
20080280841Amorphous Telithromycin Compound - The present invention relates to stable amorphous 3-De[(2,6-dideoxy-3-C-methyl-3-O-methyl-α-L-ribohexopyranosyl)oxy]-11,12-dideoxy-6-O-methyl-3-oxo-12,11-[oxycarbonyl[[4-[4-(3-pyridinyl)-1H-imidazol-1-yl]butyl]imino]]erythromycin (telithromycin), methods for the preparation thereof, the use of stable amorphous telithromycin in the treatment of bacterial infections and to pharmaceutical compositions comprising stable amorphous telithromycin.11-13-2008
20080207583Process For Preparing Granulates Comprising Amoxicillin - A novel process for preparing a stable granulate, which comprises a mixture of amoxicillin trihydrate and amoxicillin sodium, by means of extrusion granulation of amoxicillin trihydrate with an aqueous solution of sodium hydroxide, sodium bicarbonate, sodium carbonate and mixture thereof or with an aqueous solution of sodium salt of (C08-28-2008

Patent applications by SANDOZ AG