Abstract: The invention relates to a novel synthesis route towards R-biphenylalaninol and to the intermediates applied in this synthesis route. The process according to the invention and the intermediate compounds are useful in the synthesis of pharmaceutically active compounds.

Abstract: The present invention relates to a composition, such as a coating composition, comprising a peptide linked to a lubricant, wherein the peptide is cleavable by one or more proteinases present in tear fluid. The invention further relates to an ocular device comprising said composition, such as a preformed contact lens.

Abstract: This invention relates to a novel process for the synthesis of R-biphenylalaninol and to intermediate compounds that are formed in the process according to the invention, i.e. novel intermediates useful in the synthesis of R-biphenylalaninol. The invention also relates to R-biphenylalaninol, The process according to the invention, the intermediates to of R-biphenylalaninol and of R-biphenylalaninol are all useful in the synthesis of pharmaceutically active compounds.

Abstract: This invention relates to a novel process for the synthesis of R-biphenylalaninol and to intermediate compounds that are formed in the process according to the invention, i.e. novel intermediates useful in the synthesis of R-biphenylalaninol. The in vention also relates to R-biphenylalaninol, The process according to the invention, the intermediates to of R-biphenylalaninol and of R-biphenylalaninol are all useful in the synthesis of pharmaceutically active compounds.

Abstract: The invention relates to a process for the preparation of compounds that are important building blocks in convergent synthesis routes to 2(S),4(S),5(S),7(S)-2,7-dialkyl-4-hydroxy-5-amino-8-aryl-octanoyl amides or pharmaceutically acceptable salts thereof, such as the compound Aliskiren, and to a process for the preparation of these octanoyl amides, comprising reacting said building block.

Abstract: The present invention relates to a whole cell catalytic system for the preparation of an enantiomerically enriched ?-amino acid from a corresponding hydantoin wherein hydantoinase, L-carbamoylase and hydantoin racemase are coexpressed in a recombinant micro-organism wherein the genes coding for these three enzymes are located on a single replicon. The present invention further relates to the use of such a whole cell catalytic system according in the preparation of an enantiomerically enriched L-?-amino acid from a corresponding hydantoin.

Abstract: The invention relates to a process for racemising an enantiomer-enriched Schiff base of a primary amino acid amide with a strong base that is chemically reactive towards water. The reaction is conducted in an organic solvent. Preferably a metal alkoxide, a metal alkyl, a metal amide, or a metal hydride, in particular a metal alkoxide is applied as the strong base. As the Schiff base preferably N-benzylidene primary amino acid amide is used, with the primary amino acid amide preferably being derived from an aliphatic primary amino acid amide, for example tertiary-leucine amide. As organic solvent use is preferably made of an aromatic hydrocarbon, a cyclic, aliphatic hydrocarbon or a ether, in particular an aromatic hydrocarbon is applied. The invention may also be applied for the racemisation of an enantiomer-enriched primary amino acid amide.

Abstract: The invention relates to a process for racemising an enantiomer-enriched Schiff base of a primary amino acid amide with a strong base that is chemically reactive towards water. The reaction is conducted in an organic solvent. Preferably a metal alkoxide, a metal alkyl, a metal amide, or a metal hydride, in particular a metal alkoxide is applied as the strong base. As the Schiff base preferably N-benzylidene primary amino acid amide is used, with the primary amino acid amide preferably being derived from an aliphatic primary amino acid amide, for example tertiary-leucine amide. As organic solvent use is preferably made of an aromatic hydrocarbon, a cyclic, aliphatic hydrocarbon or a ether, in particular an aromatic hydrocarbon is applied. The invention may also be applied for the racemisation of an enantiomer-enriched primary amino acid amide.