Abstract: The present invention is concerned with isoxazole-thiazole derivatives of formula I, having affinity and selectivity for GABA A ?5 receptor, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful as cognitive enhancer or for the therapeutic and/or prophylactic treatment of cognitive disorders like Alzheimer's disease.
Type:
Grant
Filed:
April 28, 2010
Date of Patent:
May 15, 2012
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Roland Jakob-Roetne, Matthew C. Lucas, Andrew Thomas
Abstract: Disclosed is a process for the manufacture of pseudo proline dipeptides of the formula wherein R1 is a side chain of an alpha amino acid, R2 is an amino protecting group and R3 and R4 are independently either hydrogen or C1-4-alkyl, and R5 is hydrogen or methyl starting from an amino acid derivative of the formula wherein R1 and R2 are as defined above. Pseudo proline dipeptides can be used as reversible protecting groups for Ser, Thr and Cys and thus are versatile tools in peptide chemistry.
Type:
Grant
Filed:
June 14, 2007
Date of Patent:
November 3, 2009
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Thomas Ammann, Stephan Goetzoe, Bernd Thern, Sandra Welz, Klaus-Juergen Wolter