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    • 4. 发明申请
    • ATRIAL PEPTIDE DERIVATIVES
    • ATRIAL肽衍生物
    • WO1990014362A1
    • 1990-11-29
    • PCT/US1990002917
    • 1990-05-23
    • ABBOTT LABORATORIESLUCAS, Scott, D.ROCKWAY, Todd, W.DAVIDSEN, Steven, K.THOMAS, A., MitchellVON GELDERN, Thomas, W.
    • ABBOTT LABORATORIES
    • C07K07/08
    • C07K14/58A61K38/00
    • The present invention provides novel peptides which exhibit useful hypotensive, natriuretic, diuretic, renovasodilating, reno-protective, smooth muscle relaxant, and vasorelaxant activities. The novel atrial peptides of the instant invention are encompassed by formula (I) or a pharmaceutically acceptable salt, ester or amide thereof, wherein R is selected from hydrogen, AcetylArg, Aha, Arg, Cit, His, Lys, Orn and Ser-Ser; R is a sulfur-containing group; R is a hydrophobic amino acid or dipeptide; R is a dipeptide spacer or a tripeptide of the formula X-Y, where X is a dipeptide spacer and Y is a basic amino acid; R is a hydrophobic amino acid; R is a peptide of up to three amino acids; R is selected from Cha, Phe, Cha-Arg, Phe-Arg, (D)Phe-Arg, Phe-(D)Arg, Phe Arg, Leu-Arg, Ala-Arg, Arg and Gly-Ala; and R is a sulfur-containing group.
    • 本发明提供了具有有用的低血压,利尿钠,利尿剂,改善释放,肾保护,平滑肌松弛剂和血管舒张活性的新型肽。 本发明的新型心房肽包括式(I)或其药学上可接受的盐,酯或酰胺,其中R 1选自氢,乙酰基氨基,氨基,Arg,Cit,His,Lys,Orn和 丝氨酸 - 丝氨酸; R 2是含硫基团; R 3是疏水性氨基酸或二肽; R 4是二肽间隔物或式X-Y的三肽,其中X是二肽间隔物,Y是碱性氨基酸; R 5是疏水性氨基酸; R 6是多至三个氨基酸的肽; R 7选自Cha,Phe,Cha-Arg,Phe-Arg,(D)Phe-Arg,Phe-(D)Arg,Phe> Arg,Leu-Arg,Ala-Arg,Arg和Gly -翼; R 8为含硫基团。