Patent ID: 6943145
Filing Date: 2005-09-13
Classification: A61K,C07K

Abstract:
1. A quaternary salt of the formula wherein: X R R or one of R the depicted ring system is a pyridinium, quinolinium or isoquinolinium ion; “spacer” is an L-amino acid unit or a di- or tripeptide consisting of 2 or 3 L-amino acid units, the N-terminal amino acid of said spacer being bonded to the depicted carbonyl carbon via an amide bond; and “peptide” is a peptide having 2 to 20 amino acid units having growth factor inhibitory activity which is octreotide or lanreotide, wherein the N-terminal phenylalanine or napthylalanine of said peptide is bonded to the C-terminal amino acid of said spacer via a peptide bond, and wherein the C-terminal threonine of said peptide: (a) has a C-terminal carboxyl group —COOH which has been replaced with a —COOR (b) has a C-terminal —CH (c) has a C-terminal —CONH (d) has a C-terminal —CONH (e) has a C-terminal —CH with the provisos that: (1) when the C-terminal amino acid is as defined in (a), (b) or (c) above, the side chain —NH (2) when the C-terminal amino acid is as defined in (d) or (e) above, then the side chain —NH