SANDOZ AG Patent applications |
Patent application number | Title | Published |
20160017403 | QUANTIFICATION OF MISFOLDED TNFR2:FC - The present invention is directed to methods for determining the relative amount of wrongly disulphide bridged TNFR2:Fc in a sample of TNFR2:Fc, a fusion protein which is used in a variety of therapeutic applications. In addition, the invention pertains to a method for purifying TNFR2:Fc using said method for determining the percentage of wrongly disulphide bridged TNFR2:Fc, and to TNFR2:Fc compositions obtained thereby. | 01-21-2016 |
20150274732 | PREPARATION OF ERTAPENEM INTERMEDIATES - The present invention relates to the preparation of compounds, in particular to the preparation of compounds which may be used as intermediates for the preparation of antibiotics, preferably carbapenem antibiotics, more preferably ertapenem, and salts thereof. | 10-01-2015 |
20150266841 | Novel Crystalline Form Of Vortioxetine Hydrobromide - The present invention is directed to a crystalline compound comprising a hydrobromide acid (HBr) salt of a compound of formula (I) (1-{2[2,4-dimethylphenyl)sulfanyl]phenyl}piperazine, INN: vortioxetine), having an XRPD pattern with characteristic peaks (expressed in 2θ±0.2° 2θ (CuKα radiation)) at 5.5°, 14.8°, 16.7° and 20.0° and processes for obtaining the same. | 09-24-2015 |
20150245995 | Stable Quick Dissolving Dosage Form Comprising Amoxicillin and Clavulanic Acid - A quick dissolving pharmaceutical formulation is disclosed. In one embodiment, the formulation includes at least the following components: (1) from about 35 to about 50 weight percent amoxicillin or a pharmaceutically acceptable salt thereof; (2) from about 2.0 to about 12 weight percent clavulanic acid or a pharmaceutically acceptable salt thereof; (3) from about 30 to about 40 weight percent mannitol; (4) from about 2 to about 7 weight percent crospovidone; (5) from about 0.5 to about 2.0 weight percent colloidal silicon dioxide; and (6) from about 2.0 to about 5.0 weight percent sodium stearyl fumarate. A method for making a quick dissolving pharmaceutical tablet is also disclosed. | 09-03-2015 |
20150183824 | SYNTHESIS OF TELAPREVIR AND BOCEPREVIR, OR PHARMACEUTICALLY ACCEPTABLE SALTS OR SOLVATES AS WELL AS INTERMEDIATE PRODUCTS THEREOF INCLUDING beta-AMINO ACIDS PREPARED VIA MUKAIYAMA ALDOL ADDITION - The invention relates to synthetic routes for preparing telaprevir and boceprevir, and its intermediates as well as peptides other than telaprevir. The synthetic routes are based on a Mukaiyama aldol addition reaction of a silyl enol ether or an enolate with an imine. The invention also refers to novel intermediates for preparing telaprevir/boceprevir or other peptides. | 07-02-2015 |
20150147781 | METHOD FOR PRODUCING A RECOMBINANT PROTEIN OF INTEREST - Disclosed is a method for producing a recombinant protein of interest, characterised in by the following steps: (a) providing a fusion protein comprising an N | 05-28-2015 |
20150080435 | PHARMACEUTICAL COMPOSITION CONTAINING CRYSTALLINE SORAFENIB TOSYLATE - The present invention relates to an oral solid dosage form, in particular a tablet, comprising sorafenib tosylate polymorphic form III. | 03-19-2015 |
20150073138 | NOVEL PROCESS FOR PREPARING CEFTAROLINE FOSAMIL - The present invention relates to a novel process for preparing ceftaroline fosamil as well as to a intermediates of this process. | 03-12-2015 |
20150038727 | METHOD FOR PREPARING SILODOSIN - The present invention relates to a process for preparing silodosin with high optical purity up to 99.9% enantiomeric excess (e.e.) or above. The process makes use of a method step, in which the enantiomers contained in a racemic mixture of a compound represented by the general formula V: wherein * denotes the asymmetric center, R | 02-05-2015 |
20140336179 | ACETONE SOLVATE OF IVABRADINE HYDROCHLORIDE - The present invention relates to a novel solvate of ivabradine hydrochloride, a process of its preparation and its use for the preparation of specific polymorphic forms of ivabradine hydrochloride. | 11-13-2014 |
20140329989 | PREPARATION OF MICAFUNGIN INTERMEDIATES - The present invention relates to the preparation of compounds, in particular to the preparation of compounds of formula (I), which may be used with a compound of formula (VI), or a salt thereof as intermediates for the preparation of antifungal agents, preferably micafungin (MICA) or a salt thereof. | 11-06-2014 |
20140303184 | PROCESS FOR THE PREPARATION OF A CHIRAL COMPOUND - The present invention relates to a process for the preparation of a compound of formula (V), in particular posaconazole, wherein said process comprises the steps of (1) providing a mixture comprising a compound of formula (IV), a protic solvent system, and a suitable base; and (2) heating the mixture of (1) to obtain a mixture comprising the compound of formula (V). | 10-09-2014 |
20140294962 | METHOD OF PREPARING POLYMORPHIC PURE FORM A OF BAZEDOXIFENE ACETATE - The present invention provides a reliable process for the preparation of polymorphic pure form A of Bazedoxifene x acetate. In addition, the present invention relates to a process of wet granulation of polymorphic pure form A of Bazedoxifene x acetate. The present invention also relates to pharmaceutical compositions comprising polymorphic pure form A of Bazedoxifene x acetate as well as to the use of cyclic ethers for the preparation of such pharmaceutical composition. | 10-02-2014 |
20140294756 | Long-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 the non-glycosylated recombinant human G-CSF and sorbital 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 and then increased in temperature to a temperature within the range of from 2° C. to 8° C. for a period of time adjusted to allow the composition to thaw and to obtain a liquid composition having a G-CSF content of at least 95% of the G-CSF content of the original composition. | 10-02-2014 |
20140213784 | METHOD FOR THE PREPARATION OF SUBSTITUTED OXAZOLIDINONES - The present invention relates to methods for the preparation of a compound having the formula (X). Individual reaction steps as well as intermediates are additionally claimed. | 07-31-2014 |
20140200252 | CRYSTAL 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. | 07-17-2014 |
20140194356 | AQUEOUS FORMULATION COMPRISING AT LEAST A NEUTRAL SALT AND A BIOPHARMACEUTICAL PROTEIN - The present invention is related to a pharmaceutically acceptable aqueous formulation comprising at least a neutral salt and a biopharmaceutical protein, wherein the concentration ratio between the biopharmaceutical protein and the neutral salt is in the range of ≧0.7 and ≦5. | 07-10-2014 |
20140170702 | METHOD FOR PRODUCING A RECOMBINANT PROTEIN OF INTEREST - Disclosed is a method for producing a recombinant protein of interest, the method being characterised in by the following steps:
| 06-19-2014 |
20140170701 | METHOD FOR PRODUCING A RECOMBINANT PROTEIN OF INTEREST - Disclosed is a method for producing a recombinant protein of interest which is characterised by the following steps:
| 06-19-2014 |
20140163083 | NOVEL CRYSTALLINE SALTS OF ASENAPINE - Crystalline Asenapine salts of tartaric acid or succinic acid, wherein the salts are e.g. selected from the group consisting of Asenapine D, L-tartrate hydrate form A, Asenapine D, L-tartrate hydrate form B, Asenapine D, L-tartrate anhydrous form, Asenapine succinate form X, Asenapine succinate form, and Asenapine succinate form II are described as well as related pharmaceutical compositions and related treatment of psychotic diseases or disorders. | 06-12-2014 |
20140135353 | CRYSTALLINE SODIUM SALT OF AN HIV INTEGRASE INHIBITOR - A crystalline sodium salt of a compound of formula I (INN: Raltegravir) | 05-15-2014 |
20140128444 | NOVEL CRYSTALLINE SALTS OF ASENAPINE WITH ORGANIC DI-ACIDS AND TRI-ACIDS - Novel crystalline salts of Asenapine (I) with organic di-acids and tri-acids and to methods of their preparation are disclosed along with related pharmaceutical compositions and methods of treating psychotic diseases or disorders. | 05-08-2014 |
20140121259 | NOVEL CRYSTALLINE ASENAPINE HYDROCHLORIDE SALT FORMS - Novel crystalline HCl salts of Asenapine, methods of their preparation and related pharmaceuticals and treatments are disclosed. | 05-01-2014 |
20140121225 | POLYMORPH OF LINAGLIPTIN BENZOATE - The present invention relates to a novel polymorph of Linagliptin benzoate and to methods for its preparation. Furthermore the present invention relates to the use of the novel polymorph for the preparation of a medicament. In addition the present invention relates to pharmaceutical compositions comprising an effective amount of the novel polymorph of Linagliptin benzoate. | 05-01-2014 |
20140081016 | REGIOSELECTIVE ACYLATION OF RAPAMYCIN AT THE C-42 POSITION - The invention refers to the selective acylation of Rapamycin at the 42-position (I) with an acylating agent of the formula (II) wherein R | 03-20-2014 |
20130245017 | CRYSTALLINE FORM OF RIVAROXABAN DIHYDRATE - The present invention relates to a novel crystalline dihydrate of Rivaroxaban, processes for the preparation thereof, pharmaceutical compositions comprising said crystalline dehydrate and to processes for preparing and storing said pharmaceutical compositions. The invention also relates to a crystalline formic acid solvate of Rivaroxaban, processes for the preparation of crystalline Rivaroxaban formic acid solvate and to the use of said Rivaroxaban formic acid solvate in the manufacture of the crystalline dihydrate of Rivaroxaban. | 09-19-2013 |
20130211086 | PURIFICATION OF POSACONAZOLE AND OF POSACONAZOLE INTERMEDIATES - The present invention relates to a process for the preparation of a hydrogen chloride (HCl) salt of a compound of formula (I) wherein Y | 08-15-2013 |
20130210833 | PROCESS FOR THE PREPARATION OF CHIRAL TRIAZOLONES - A process for the preparation of a chiral compound, in particular posaconazole, wherein the process comprises mixing and reacting the compounds of formula (I) Y | 08-15-2013 |
20130203994 | PREPARATION OF POSACONAZOLE INTERMEDIATES - The present invention relates to process for the preparation of a chiral compound of formula (IX) or a salt thereof, wherein Y | 08-08-2013 |
20130203993 | PROCESS FOR THE PREPARATION OF CHIRAL HYDRAZIDES - The present invention relates to a process for the preparation of a chiral compound according to formula (V) wherein R | 08-08-2013 |
20130184457 | METHOD FOR THE PREPARATION OF RIVORAXABAN - The present invention relates to the use of a compound having the formula (II) for the preparation of a compound having the formula (V). Methods of preparing the compound having the formula (V) using the compound having the formula (II) are also described. Individual reaction steps as well as intermediates are additionally claimed. | 07-18-2013 |
20130164253 | Long-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 the non-glycosylated recombinant human G-CSF and sorbital 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 and then increased in temperature to a temperature within the range of from 2° C. to 8° C. for a period of time adjusted to allow the composition to thaw and to obtain a liquid composition having a G-CSF content of at least 95% of the G-CSF content of the original composition. | 06-27-2013 |
20130137734 | Polymorphs of an Active Pharmaceutical Ingredient - The present invention relates to crystalline form I of Febuxostat as well as to pharmaceutical compositions camprising crystalline form I as an active pharmaceutical ingredient. Furthermore the present invention relates to a further polymorphic form of Febuxostat designated as form II and to a novel solvate of Febuxostat. The present invention also relates to methods of making crystalline form I, form II and the novel solvate of Febuxostat. | 05-30-2013 |
20130059344 | TRANSCRIPTION TERMINATOR SEQUENCES - The present invention provides new transcription termination signal sequences, especially a polynucleotide comprising at least two consecutive transcription termination signals, characterized in that said consecutive transcription termination signals comprise at least a first and a second transcription termination signal that are at most 1000 nucleotides apart, and at least one of the termination signal has or encodes a RNA hairpin structure. | 03-07-2013 |
20130028940 | CASPOFUNGIN FORMULATIONS - The present invention relates to pharmaceutical compositions comprising a pharmaceutically acceptable salt of caspofungin as active ingredient being useful for the prevention and/or treatment of fungal infections. Said compositions additionally comprise specific bulking agents and small amounts or no amounts of an additional pH modifier and may be in a liquid or solid form, e.g. may be lyophilized compositions. Said compositions show good stability and reduced amounts of sub-visible particulate matter formed in solutions which are reconstituted from the lyophilized product. | 01-31-2013 |
20130012481 | CRYSTALLINE 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. | 01-10-2013 |
20120258493 | PROMOTER SEQUENCES - The present invention relates to new promoter sequences and uses thereof, in particular expression cassettes, vectors, and methods of expressing genes using the new promoters. | 10-11-2012 |
20120253038 | PROCESSES FOR THE SYNTHESIS OF BAZEDOXIFENE ACETATE AND INTERMEDIATES THEREOF - Efficient processes for the synthesis of pharmaceutically useful compounds such as (1-[4-(2-azepan-1-yl-ethoxy)-benzyl]-2-(4-hydroxy-phenyl)-3-methyl-1H-indol-5-ol acetic acid commonly known as bazedoxifene acetate (Formula IX) using cyanomethoxybenzyl halides of Formula III, where X=Halogens e.g., Cl, F, Br, I; G=Any electron donating or electron withdrawing substituent. | 10-04-2012 |
20120232266 | REDUCTION OF ORGANIC COMPOUNDS WITH LOW AMOUNTS OF HYDROGEN - The present invention relates to a process for the reaction of a compound with hydrogen wherein the reaction is conducted using a hydrogen-containing gas comprising up to about 10 vol. % hydrogen and at least about 90 vol. % of an inert gas and wherein the compound to be reacted with hydrogen is provided in a liquid phase. The process of the present invention is particularly suitable for hydrogenation and hydrogenolysis reactions. | 09-13-2012 |
20120165548 | PROCESS FOR THE PREPARATION OF INDOLINE DERIVATIVES AND THEIR INTERMEDIATES THEREOF - Processes for the preparation of Silodosin and its intermediates comprising reductive amination of compound of Formula (VIII) with a compound of Formula (VII) or a compound of Formula (XV) in a suitable solvent using a reducing agent. | 06-28-2012 |
20120142693 | CRYSTALLINE COMPOUND OF 7-[(3R)-3-AMINO-1-OXO-4-(2, 4, 5-TRIFLUORPHENYL)BUTYL]-5, 6, 7, 8-TETRAHYDRO-3-(TRI FLUORMETHYL)-1, 2, 4 -TRIAZOLO[4,3-A]PYRAZIN - A crystalline compound of 7-[(3R)-3-amino-1-oxo-4-(2,4,5-trifluorophenyl)butyl]-5,6,7,8-tetrahydro-3-(trifluoromethyl)-1,2,4-triazolo[4,3-a]pyrazine (INN: Sitagliptin) of formula 1 | 06-07-2012 |
20120136015 | PROCESS 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 |
20120122993 | PHARMACEUTICAL 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 |
20120116070 | METHOD 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 |
20120108807 | METHOD 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 |
20120107869 | ORGANIC 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 |
20120101277 | CRYSTALLINE 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 |
20120088808 | CRYSTAL 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 |
20120042613 | Long-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 |
20120022025 | CRYSTALLINE 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 |
20110319867 | METHOD 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 |
20110306764 | CRYSTALLINE 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 |
20110190502 | PROCESS 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 |
20110178340 | IMPROVED 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 |
20110174653 | CAPSULE 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 |
20110165636 | PROCESS 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 |
20110137035 | PREPARATION 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 |
20110124893 | ANTIBIOTIC 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 |
20110124575 | METHOD 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 |
20110105772 | CRYSTALLINE 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 |
20110105525 | PHARMACEUTICAL 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 |
20110065722 | A 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 |
20110045531 | METHOD 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 |
20110040078 | PROCESS 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 |
20110015191 | ORGANIC 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 |
20110009648 | Carbonyl 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 |
20110009629 | PREPARATION 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 |
20100151035 | PHARMACEUTICAL 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 |
20100063473 | DEVICE 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 |
20100010239 | Process 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 PGF | 01-14-2010 |
20090203069 | Organic 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 |
20090186865 | Lyophilization 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 |
20090162897 | Promoter 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 |
20090149508 | Process 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 |
20090099370 | Crystalline 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 |
20080319162 | Process 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 |
20080280841 | Amorphous 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 |
20080207583 | Process 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 (C | 08-28-2008 |