SPETZLER, JANE,SCHÄFFER, LAUGE,LAU, JESPER,KODRA, JÁNOS TIBOR,MADSEN, KJELD,GARIBAY, PATRICK WILLIAM,KOFOED, JACOB,RUNGE, STEFFEN,THØGERSEN, HENNING,PETTERSSON, INGRID
申请号：
ES08803802
公开号：
ES2550363T3
申请日:
2008.09.05
申请国别(地区):
ES
年份:
2015
代理人:
摘要：
A GLP-1 analog that is GLP-1 (7-35) (SEQ ID No. 1) modified having the sequence of formula (I) ** Formula ** in which Xaa7 is L-histidine, D-histidine, desamino-histidine, 2-amino-histidine, β-hydroxy-histidine, homohistidine, Nα-acetylhistidine, α-fluoromethyl-histidine, α-methyl-histidine, 3-pyridylalanine, 2-pyridylalanine or 4-pyridylalanine； Xaa8 is Ala, Gly, Val, Leu, Ile, Lys, Aib, (1-aminocyclopropyl) carboxylic acid, (1-aminocyclobutyl) carboxylic acid, (1-aminocyclopentyl) carboxylic acid, (1-aminocyclohexyl) carboxylic acid, ( 1-aminocycloheptyl) carboxylic or (1-aminocyclooctyl) carboxylic acid； Xaa9 is Glu or a derivative of Glu such as alpha, alpha-dimethyl-Glu； Xaa16 is Val or Leu； Xaa18 is Ser, Lys, Cys or Arg； Xaa20 is Leu, Lys or Cys； Xaa23 is Gln, Glu, Lys, Cys or Arg； Xaa24 is Ala or Asn； Xaa25 is Ala or Val； Xaa27 is Glu, Ala or Leu； Xaa30 is Ala, Glu, Lys, Arg or is absent； Xaa31 is Trp, Lys, Cys or is absent； Xaa33 is Val, Lys, Cys or is absent； Xaa34 is Lys, Glu, Asn, Arg, Cys or is absent； Xaa35 is Gly, Aib or is absent； R is amide or absent； provided that if Xaa30, Xaa31, Xaa32, Xaa33 or Xaa34 is absent then each amino acid residue in the 3 'direction is also absent； and where the GLP-1 analog has a total of 2, 3, 4, 5, 6, 7, 8 or 9 amino acid substitutions compared to GLP-1 (7-35).Un análogo de GLP-1 que es GLP-1(7-35) (SEQ ID Nº 1) modificado que tiene la secuencia de fórmula (I)**Fórmula** en la que Xaa7 es L-histidina, D-histidina, desamino-histidina, 2-amino-histidina, ß-hidroxi-histidina, homohistidina, N&alpha；-acetilhistidina, &alpha；-fluorometil-histidina, &alpha；-metil-histidina, 3-piridilalanina, 2-piridilalanina o 4-piridilalanina； Xaa8 es Ala, Gly, Val, Leu, Ile, Lys, Aib, ácido (1-aminociclopropil) carboxílico, ácido (1-aminociclobutil) carboxílico, ácido (1-aminociclopentil) carboxílico, ácido (1-aminociclohexil) carboxílico, ácido (1-aminocicloheptil) carboxílico o ácido (1-aminociclooctil) carboxílico； Xaa9 es Glu o un deri
