Patent ID: 6013627
Filing Date: 2000-01-11
Classification: A61K,A61P,C07K,C12N,C12R

Abstract:
A cyclopeptolide of formula I ##STR25## wherein: A is an .alpha.-hydroxy-substituted butyric acid residue optionally .gamma.-substituted by R.sub.6, which represents CN, COOR.sub.2, CONR.sub.3 R.sub.4, COR.sub.5, CSNH.sub.2 or alkyl, which may be substituted by azido, halogen, alkoxy, optionally protected hydroxy or amino, vinyl, which may be substituted by alkyl, halogen or CN, cycloalkyl, tetrazolyl or --C.tbd.CH, wherein R.sub.2 represents hydrogen or optionally arylsubstituted alkyl, R.sub.3 and R.sub.4 are the same or different and represent hydrogen or alkyl or form together with the nitrogen a 3- to 6-membered ring optionally containing a second heteroatom, and R.sub.5 represents hydrogen or lower alkyl,B is an .alpha.-amino-.gamma.-methyl-substituted octanoic acid residue;R.sub.1 is hydrogen or methyl;C is a tryptophan or N-methyl-tryptophan residue of formula VI ##STR26## wherein R.sub.8 represents hydrogen, alkoxy, alkyl or benzyl, R.sub.9 represents hydrogen or halogen, R.sub.10 represents hydrogen or methyl and ---- represents a single or double bond,X is an .alpha.-amino-substituted (C.sub.2 to C.sub.14) carboxylic acid residue, andY is an .alpha.-amino- or N-methyl-.alpha.-amino substituted (C.sub.2 to C.sub.10) carboxylic acid residue.