Novartis Ag

Degussa Aktiengesellschaft

Other

Matthias Kittelmann

Maria-Regina Kula

Oreste Ghisalba

Ulrich Hassiepen

Christian Wandrey

Udo Kragl

Kurt Laumen

Paula Walser-Volken

Teresa Klein

A method of inhibiting dipeptidyl peptidase-IV comprising administering to a mammal in need of such treatment a therapeutically effective amount of a compound of formulae (I A), (I B), (X A), (X B), (Y A) or (Y or B), wherein R' represents and R&#x2033; represents hydrogen, hydroxy, C-Calkoxy, C-C-alkanoyloxy, or RRN&#x2014;CO&#x2014;O&#x2014;, where Rand Rindependently are C-Calkyl or phenyl which is unsubstituted or substituted by a substitutent selected from C-Calkyl, C-Calkoxy, halogen and trifluoromethyl and where Radditionally is hydrogen; or Rand Rtogether represent C-Calkylene,in free form or in form of a pharmaceutically acceptable acid addition salt.

Organic compounds

The present invention relates to a compound The instant invention relates to a compound of formulae (I A), (I B), (X A), (X B), (Y A) or (Y B),  Compounds of formulae (I A), (I B), (X A), (X B), (Y A) or (Y B) inhibit DPP-IV (dipeptidyl-peptidase-IV) activity. They are therefore indicated for use as pharmaceuticals in inhibiting DPP-IV and in the treatment of conditions mediated by DPP-IV, such as non-insulin-dependent diabetes mellitus, arthritis, obesity, osteoporosis and further conditions of impaired glucose tolerance.

The invention belongs to the field of biotechnology. It concerns a biocatalyst, i.e. a dead or living microorganism or a polypeptide, preferably in isolated form, which exhibits acylase enzymatic activity without lipase- or esterase-activity. The biocatalyst is capable of stereoselectively hydrolysing a racemic acylamide which has an aliphatic acyl residue and which is not a derivative of a natural amino acid.

Biocatalysts with amine acylase activity

The invention relates to a process for the production of cytidine 5'-monophosphosialic acids which comprises reacting a sialic acid with cytidine 5'-triphosphate in the presence of a cell extract of a naturally occurring microorganism having cytidine 5'-monophospho-N-acetylneuraminic acid synthetase activity, the extract optionally having been subjected to one purification step.

Process for the production of activated sialic acids

A novel N-Acetyl-2,3-didehydroaminoacid-acylase is obtained by cultivating Zoogloea ramigera DSM 4306. The new enzyme can be used in a coupled enzyme system with an L-Leucinedehydrogenase for the enzymatic conversion of N-Acetyl-2,3-didehydroleucine to L-Leucine, D- or L-tryptophylglycine to D- or L-tryptophaneamide and glycine, as well as other tryptophanedipeptides to tryptophaneamides and free amino acids.

Method of using N-acetyl-2,3-Didehydroleucine acylase for the

A novel N-Acetyl-2,3-didehydroaminoacid-acylase is obtained by cultivating Zoogloea ramigera DSM 4306. The new enzyme can be used in a coupled enzyme system with an L-Leucinedehydrogenase for the enzymatic conversion of N-Acetyl-2,3-didehydroleucine to L-Leucine, D- or L-tryptophylglycine to D- or L- tryptophaneamide and glycine, as well as other tryptophanedipeptides to tryptophaneamides and free amino acids.

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Freiburg, Germany

Matthias Kittelmann