Patent ID: 6939946
Filing Date: 2005-09-06
Classification: A61K,A61P,C07K,Y02A

Abstract:
1. A process for modifying a cyclic peptide ring nucleus comprising the steps of: (i) providing a cyclic peptide compound comprising a peptide unit having a γ-hydroxyl group; (ii) opening the ring of said cyclic peptide compound to provide a first linear peptide wherein said peptide unit having a γ-hydroxyl group is the N-terminus peptide unit of said first linear peptide; (iii) cleaving-off said peptide unit having a γ-hydroxyl group to provide a second linear peptide; (iv) attaching at least one amino acid, dipeptide unit or synthetic unit to said second linear peptide to produce a third linear peptide; (v) cyclizing said third linear peptide to produce a modified cyclic peptide compound having a modified ring nucleus; wherein said modified cyclic peptide compound is represented by formula I or II: wherein R is an alkyl group, an alkenyl group, an alkynyl group, an aryl group, or heteroaryl group; R2 is —H or —CH R3 is —H, —CH R4 is —H or —OH; R5 is —OH, —OPO R6 is —H or —OSO R7 is —CH (Y) is represented by the following formula wherein A is —CH where j is 1 or 2 and Z is an amino group, alkylamino group, or piperidyl amino group; and B is a substituted or unsubstituted C1 to C6 alkyl group; W is a hydrogen or C(O)R where R is as defined above; and pharmaceutically acceptable salts, esters or hydrates thereof.