KRASTEL, Philipp,LIECHTY, Brigitta-Maria,MEINGASSNER, Josef Gottfried,SCHMITT, Esther,SCHREINER, Erwin Paul
申请号:
ES08803036
公开号:
ES2632392T3
申请日:
2008.08.14
申请国别(地区):
ES
年份:
2017
代理人:
摘要:
A cyclic depsypeptide having the structure of the formula (I): ** Formula ** wherein an ester bond is formed between a carboxyl group of A7 and a hydroxyl group of A2, wherein the acyl residue X is CH3CH2CH (CH3) CO or (CH3) 2CHCO, A1 is glutamine, glutamic acid, or a derivative thereof, selected from glutamic nitrile, alkyl ester of 1 to 12 carbon atoms of glutamic acid or aryl ester of 6 to 24 carbon atoms of glutamic acid, A2 is threonine, A3 is leucine, A4 is Ahp, where AHP is 3-amino-6-hydroxy-pipiridin-2-one, 3-amino-piperidin-2-one, proline, 5- hydroxyproline or a derivative thereof, selected from 3-amino-3,4-dihydro-1H-pyridin-2-one, ** Formula ** wherein R is selected from the group consisting of alkyl of 1 to 12 carbon atoms, alkenyl of 2 to 12 carbon atoms, alkynyl of 2 to 12 carbon atoms, haloalkyl of 1 to 12 carbon atoms, alkoxy (with 1 to 12 carbon atoms) alkyl (with 1 to 12 atoms of carbon), alkoxy (with 2 to 12 carbon atoms) alkoxyalkyl (with 1 to 12 carbon atoms) of 1 to 12 carbon atoms, hydroxyalkyl of 1 to 12 carbon atoms, phenyl and phenyl alkyl of 1 to 6 carbon atoms., A5 is isoleucine, A6 is tyrosine, N-Me-tyrosine or a derivative thereof, selected from N-Me-tyrosine where the OH group of the tyrosine or N-Me-tyrosine is OR, where R is selected from the group consisting of alkyl of 1 to 12 carbon atoms, alkenyl of 2 to 12 carbon atoms, alkynyl of 2 to 12 carbon atoms, haloalkyl of 1 to 12 carbon atoms, haloalkenyl of 2 to 12 atoms of carbon, haloalkynyl of 2 to 12 carbon atoms, alkoxycarbonyl of 1 to 12 carbon atoms, alkoxy (with 1 to 12 carbon atoms) carbonyl alkyl, alkylaminocarbonyl of 1 to 12 carbon atoms, wherein the alkyl, alkenyl moieties and alkynyl of the R groups may be unsubstituted or further substituted by aryl, arylalkyl from 2 to 12 carbon atoms, arylalkenyl of 2 to 12 carbon atoms or arylalkyl alkyl of 2 to 12 carbon atoms, heterocyclyl and heterocyclylalkyl of 1 to 12 carbon atoms, A7 is isoleucine or valine, or a pharmaceutica