Abstract: The present invention refers to a process for preparing granules or particles comprising afatinib dimaleate, comprising the steps of providing afatinib dimaleate and at least one pharmaceutically acceptable excipient, and preparing granules or particles involving the use of at least one solvent selected from organic solvent and water, wherein all pharmaceutically acceptable excipients used in the process for preparing granules or particles have neutral or acidic properties, and wherein afatinib dimaleate has a solubility of at least 5 mg/ml in said at least one solvent. The present invention further refers to granules or particles comprising afatinib dimaleate that are prepared according to this process. Additionally, the present invention refers to a process for preparing a pharmaceutical composition comprising afatinib dimaleate, as well as to an adsorbate comprising afatinib dimaleate.

Abstract: The present invention relates to a pharmaceutical composition containing a stable polymorph of rifaximin and a wicking agent as well as a method of preparing the same.

Abstract: A process for preparing a compound of formula (I) or a salt thereof, the process comprising providing a compound of formula (III) wherein PG is an inert electron withdrawing hydroxyl protecting group, reacting the compound of formula (III) with a fluorinating agent, obtaining a compound of formula (II) and deprotecting the compound of formula (II).

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: The present invention relates to a highly convergent method for the synthesis and purification of ceftolozane and intermediates starting from 7-aminocephaiosporanic acid (7-ACA).

Abstract: The present invention relates to a process for the preparation of carbamoylamino pyrazole derivatives using diacetoxyiodobenzene (PhI(OAc)2) in combination with a non-nucleophilic base.

Abstract: A process for preparing a compound of formula (I) or a salt thereof, the process comprising providing a compound of formula (III) wherein PG is an inert electron withdrawing hydroxyl protecting group, reacting the compound of formula (III) with a fluorinating agent, obtaining a compound of formula (II) and deprotecting the compound of formula (II).

Abstract: The present invention refers to the synthesis and intermediates of substituted bicyclic compounds, which are used as a masked form of acrylamides and 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: A solid pharmaceutical composition comprising a solid composition, wherein the solid com-position comprises sofosbuvir and at least one pharmaceutically acceptable matrix compound, wherein at least 99 weight-% of the sofosbuvir comprised in the solid composition are present in amorphous form, at least 99 weight-% of the solid composition consist of the sofosbuvir and the at least one matrix compound, wherein the solid composition contains the sofosbuvir in an amount of at least 25 weight-%, or at least 30 weight-%, or at least 35 weight-%, or at least 40 weight-% or at least 50 weight-% or at least 55 weight-% or preferably at least 5 weight-% based on the combined weight of the sofosbuvir and the at least one matrix com-pound, wherein in the adsorption-desorption isotherm of the at least one pharmaceutically acceptable matrix compound, the desorption mass difference minus the adsorption mass dif-ference at 75% relative humidity and 25° C. is less than 0.

Abstract: The present invention provides novel methods of cell disruption and release of biomolecules from a cell. The invention comprises the use of positively and/or negatively charged microparticles comprising ground resin. It is particularly useful for purification of biomolecules from cell culture.

Abstract: The present invention relates to processes, process steps and intermediates useful in the asymmetric bisamidation of malonic ester derivatives wherein the new processes, process steps and intermediates are, for example, useful in the preparation of asymmetric malonic acid bisanilides such as cabozantinib.

Abstract: The present invention relates to crystalline forms of cabozantinib phosphoric acid salt and cabozantinib hydrochloric acid salt and to a method for their preparation. Furthermore, the invention relates to pharmaceutical compositions comprising said crystalline forms and their use as anti-cancer medicaments. Cabozantinib, i.e. N-{4-[(6,7-dimethoxy-4-quinolinyl)oxy]phenyl}-N?-(4-fluorophenyl)-1,1-cyclopropanedicarboxamide is represented by the chemical structure: Formula.

Abstract: The present invention relates to a process for the preparation of a compound of formula (A), Further, the present invention relates to the respective compound (A) as such and to its use in the preparation of antifungal agent.

Abstract: The present invention relates to crystalline form C of avibactam sodium and to a process for its preparation. The invention also concerns a pharmaceutical composition comprising form C and one or more antibacterial agents, wherein at least one antibacterial agent is a beta-lactam antibiotic. The pharmaceutical composition of the present invention can be used as medicament, in particular for treatment and/or prevention of bacterial infections.

Abstract: The present invention relates to a pharmaceutical composition containing rifaximin in the form of two different polymorphs as well as a method of preparing the same.

Abstract: A process for preparing a nucleoside phosphoramidate, in particular to a process for preparing sofosbuvir, wherein a phosphoramidate derivative is used as starting material.

Abstract: The present invention relates to a solid dispersion comprising, preferably consisting of, naloxegol salts in amorphous form and at least one pharmaceutically acceptable matrix compound and wherein the matrix compound is (i) an organic polymer, or (ii) a silicon-based inorganic adsorbent. Further, the present invention also relates to a process for preparing a solid dispersion comprising naloxegol in amorphous form and at least one pharmaceutically acceptable matrix compound, as well as to a solid dispersion obtained or obtainable by said process. Further, the present invention relates to a pharmaceutical composition comprising such solid dispersion as well as a pharmaceutical composition for use as p-opioid antagonists.

Abstract: The present invention relates to crystalline forms of cabozantinib succinate (Form A) and cabozantinib acetate (Form A-1) and to pharmaceutical compositions comprising said crystalline forms and their use as anti-cancer medicaments.

Abstract: The present invention relates to crystalline forms of cabozantinib phosphoric acid salt and cabozantinib hydrochloric acid salt and to a method for their preparation. Furthermore, the invention relates to pharmaceutical compositions comprising said crystalline forms and their use as anti-cancer medicaments. Cabozantinib, i.e. N-{4-[(6,7-dimethoxy-4-quinolinyl)oxy]phenyl}-N?-(4-fluorophenyl)-1,1-cyclopropanedicarboxamide is represented by the chemical structure: Formula.

Abstract: 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, R1 is a protecting group, and R2 is cyano or carbamoyl, are separated.