Abstract: The present invention belongs to the field of biotechnology, recombinant protein production, molecular biology, microbiology and microbial genetics. It provides a modified eukaryotic cell that is modified to the effect that the modified eukaryotic cell is not able to provide an SSN6-like related protein or an SSN6-like protein that exerts its wildtype function and/or wildtype activity, the amount of SSN6-like related protein or of SSN6-like protein being present in the modified eukaryotic cell differs from the amount of SSN6-like related protein or of SSN6-like protein being present in its wildtype form, and/or essentially no SSN6-like related protein or SSN6-like protein is present in the modified cell. Additionally, the present invention provides a polynucleotide sequence comprising a modified ssn6-like related gene or modified ssn6-like gene, and a vector comprising said polynucleoptide.

Abstract: The present invention is directed to an injection syringe comprising an injectable composition, the composition comprising a penicillin, salt or prodrug thereof, one or more pharmaceutically acceptable excipients, and water, wherein the composition is free of a preservative agent. In other aspects, the invention relates to a process for producing the injection syringe, and a kit comprising the injection syringe.

Abstract: Disclosed is a method for producing a recombinant protein of interest, characterised in by the following steps: (a) providing a fusion protein comprising an Npro autoprotease moiety and a protein of interest moiety in inclusion bodies, (b) solubilising the fusion protein in the inclusion bodies by subjecting the inclusion bodies to a solubilisation buffer containing a detergent and wherein the solubilisation buffer contains no chaotropes or chaotropes in a concentration of less than 1.5 M urea (c) refolding the solubilised fusion protein and (d) allowing the fusion protein to be cleaved by the Npro autoprotease moiety under kosmotropic conditions, wherein the recombinant protein of interest is cleaved from the fusion protein, and (e) recovering the protein of interest.

Abstract: The present invention relates to a stable pharmaceutical composition comprising amorphous or crystalline linagliptin or a pharmaceutically acceptable salt of linagliptin, mannitol, copovidone, and magnesium stearate, processes for preparing the stable pharmaceutical composition, and a container comprising the stable pharmaceutical composition.

Abstract: A method for generating a flow profile of an inhalation device is described. The method comprises the step of measuring acoustic emissions induced by inhalation flow through the inhalation device. The method further comprises the step of detecting peak frequencies in the measured acoustic emissions and generating a flow profile based on the detected peak frequencies. A corresponding device is also described.

Abstract: The present invention relates to novel pharmaceutical compositions comprising Ledipasvir and Sofosbuvir as well as to methods for their preparation.

Abstract: The present invention relates to a hydrate of flibanserin, a process for its preparation and to a pharmaceutical composition comprising the hydrate. The invention further relates to the use of said pharmaceutical composition as a medicament in particular for the treatment of hypoactive sexual desire disorder (HSDD).

Abstract: Disclosed is a compound of formula 1, or a pharmaceutically acceptable salt thereof, where R1, R2, R3, R4, R5, R6, R7, R7?, R8, R9, R10, R11, R12 and R13 are as disclosed herein. Also, disclosed is a process for the preparation of the compound of formula 1, or a pharmaceutically acceptable salt thereof, and intermediates used therein. The compound of formula 1 can be used in the preparation of halichondrin analogs, such as Eribulin; and a process for its preparation from the compound of formula 1 is also disclosed.

Abstract: Amino acid residue misincorporations are necessarily found in sequence variants at low concentrations in admixture with expressed polypeptides, resulting from one or more base mismatches within codons susceptible to amino acid residue misincorporation during transcription and/or translation. The invention provides a method of optimizing the coding sequences of a polynucleotide that encodes a polypeptide, wherein at least one codon is susceptible to amino acid residue misincorporation. The method of the invention can be used to reverse-engineer an unknown coding sequence, which encodes the same polypeptide, but differs in said at least one codon from the known coding sequence. The method can further be used to alter the immunogenic potential of an expressed polypeptide. Thus, the invention is useful in engineering optimized polynucleotides encoding polypeptides.

Abstract: The present invention refers to the synthesis and intermediates of substituted bicyclic compounds by using a central 1H-pyrazolo[3,4-d]pyrimidine of formula (I), which is assembled starting from 4,6-dichloropyrimidine carboxylic acid. The invention in particular refers to the synthesis of the Bruton's tyrosine kinase (Btk) inhibitor 1-((R)-3-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one(ibrutinib) and its synthesis intermediates.

Abstract: The invention relates to a pharmaceutical composition consisting of ceftaroline fosamil acetic acid solvate and arginine, both having a specific particle size distribution, wherein said pharmaceutical composition is stable and does not segregate into an inhomogeneous mixture.

Abstract: The present invention relates to a method for obtaining recombinant granulocyte-colony stimulating factor (G-CSF), comprising at least one cation exchange chromatography and at least one hydrophobic interaction chromatography, wherein said two chromatographic steps are immediately consecutive in optional order. In particular, the present invention relates to a method for purifying G-CSF from a mixture of G-CSF and other proteins, comprising two cation exchange chromatography steps which are conducted before and after a hydrophobic interaction chromatography, respectively.

Abstract: A process comprising (i) providing a mixture comprising a compound of formula (I) or isomers, stereoisomers, diastereomers, enantiomers or salts thereof; (ii) subjecting the mixture provided in (i) to fluorinating conditions in the presence of a fluorination agent selected from the group consisting of diethylamino (difluoro) sulfonium tetrafluoroborate and difluoro(morpholino) sulfonium tetrafluoroborate obtaining a mixture comprising a compound of formula (II) or isomers, stereoisomers diastereomers, enantiomers or salts thereof; (iii) optionally subjecting the mixture obtained in (ii) to deprotection conditions, obtaining a mixture comprising the compound of formula (III) or isomers, stereoisomers, diastereomers, enantiomers or salts thereof.

Abstract: A tablet comprising a polymorphic form of crystalline sofosbuvir having a moisture stability of at least 95% in an amount of at least 40 weight-%.

Abstract: The present invention belongs to the field of pharmaceutical industry and relates to a dry pharmaceutical composition comprising Canagliflozin, as well as to a process for preparing the same. Such dry pharmaceutical composition is useful as a medicament, especially for the normalization of plasma glucose levels.

Abstract: The present invention provides new transcription termination signal sequences, especially a polynucleotide comprising at least two consecutive transcription termination signals, characterized in that 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.

Abstract: Edoxaban is factor X inhibitor useful for the treatment or the prevention of thrombosis or embolism. A pharmaceutical composition comprising Edoxaban, or a pharmaceutically acceptable salt thereof, a water soluble vinylpyrrolidone polymer selected from the group consisting of povidone and copovidone, and a cellulose ether, and not comprising a sugar alcohol, having good dissolution and bioavailability is provided. A process for its preparation, a dosage form comprising such composition, and the use of said pharmaceutical composition and dosage form as a medicament are also disclosed.

Abstract: A process for the preparation of a compound of formula (I) and of a acid salt (T) wherein R1 is selected from the group consisting of alkyl, aryl, cycloalkyl, heteroalkyl, heteroaryl and heterocycloalkyl, R2 and R3, are, independently of each other, selected from the group consisting of alkyl, aryl, cycloalkyl, heteroalkyl, heteroaryl and heterocycloalkyl, R4, R5, R6 and R7, are independently of each other, selected from the group consisting of H, alkyl, aryl, cycloalkyl, heteroalkyl, heteroaryl and heterocycloalkyl, and wherein the acid salt is a 2,3-Ditoluoyl tartaric acid salt, 2,3-Dibenzoyl tartaric acid salt, 2,3-Dianisoyl tartaric acid salt, 2,3-Dibenzoyl tartaric acid mono(dimethylamide) salt or a mixture of two or more thereof, wherein the tartaric acid salt (T) of the compound of formula (I) contains at least 90% by weight of the tartaric salt of the compound of formula (Ia) based on the total weight of the acid salt of the compound of formula (I).

Abstract: The present invention relates to an oral solid dosage form, in particular a tablet, comprising macitentan free base polymorphic form I.

Abstract: The present disclosure relates to polymorphic forms of the hydrochloride salt of ponatinib (“compound 1”) and to processes for the preparation of these polymorphic forms. The present disclosure also generally relates to a pharmaceutical composition comprising the forms, as well of methods of using the form(s) in the treatment of disorders associated with pathological cellular proliferation, such as neoplasms, and cancer.