KRASTEL, PHILIPP,LIECHTY, BRIGITTA-MARIA,SCHMITT, ESTHER,SCHREINER, ERWIN PAUL
申请号：
ES08803037
公开号：
ES2527298T3
申请日:
2008.08.14
申请国别(地区):
ES
年份:
2015
代理人:
摘要：
Cyclic depsypeptide having the structure of the formula (I): ** Formula ** in which the ester bond is between the carboxyl group of A7 and the hydroxyl group of A2, in which X and A1 are each independently optional , and in which X is any chemical residue； A1 is a conventional amino acid； A2 is threonine or serine or 5-methylhydroxyproline； A3 is a conventional non-basic amino acid or derivative thereof, or a non-conventional non-basic amino acid, in which the conventional non-basic amino acid derivative is selected from an O-alkyl, O-aryl, O-acyl, S- derivative alkyl, S-aryl, SS-alkyl, alkoxycarbonyl, O-carbonyl-alkoxy, carbonate, O-carbonyl-aryloxy, O-carbonylalkylamino, O-carbonyl-arylamino, N-alkyl, N-dialkyl, N-trialkylammonium, N- acyl, N-carbonyl-alkoxy, N-carbonylaryloxy, N-carbonyl-alkylamino, N-carbonyl-arylamino, N-sulfonylalkyl or N-sulfonylaryl； A4 is Ahp, dehydro-AHP or proline； A5 is isoleucine, leucine, phenylalanine, proline, threonine or valine； A6 is alanine, phenylalanine, tryptophan, tyrosine or a tyrosine derivative thereof, wherein the tyrosine derivative is selected from an O-alkyl, O-aryl, O-heteroaryl, O-acyl, O-PO3H derivative or O-SO3H or a derivative that is halogenated, in the ortho or meta position； A7 is leucine, isoleucine or valine； wherein the amide bond nitrogen atom between A5 and A6 may be substituted with a methyl； wherein Ahp is 3-amino-6-hydroxy-2-piperidone； or a pharmaceutically acceptable salt thereof, for use as a medicine to treat a calicrein-dependent disease 7.Depsipéptido cíclico que tiene la estructura de la fórmula (I):**Fórmula** en la que el enlace éster se encuentra entre el grupo carboxilo de A7 y el grupo hidroxilo de A2, en la que X y A1 son cada uno independientemente opcionales, y en la que X es cualquier residuo químico； A1 es un aminoácido convencional； A2 es treonina o serina o 5-metilhidroxiprolina； A3 es un aminoácido convencional no básico o derivado del mismo, o un aminoácido no convencional no básico
