Cyclic hexapeptides, their production and use

Details Cyclic hexapeptides, their production and use Cyclic hexapeptides, their production and use

1996-10-30

1999-09-07

Achutamurthy, Ponnathapura

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Peptide containing doai

514 9, 514 2, 530317, 530339, A61K 3812, C07K 764

Patent

active

059487542

ABSTRACT:
A cyclic hexapeptide represented by the formula: --R.sup.3)--! (I)
wherein A is a D-acidic-.alpha.-amino acid residue; Y is an acidic-.alpha.-amino acid residue; C is an L-.alpha.-amino acid residue; R.sup.1 is a group represented by the formula: ##STR1## wherein X.sup.1 and X.sup.2 are independently H, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, halogen or nitro, and may bind together to form a ring in cooperation with the adjacent carbon atom; R.sup.2 is C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkyl-C.sub.1-3 alkyl, C.sub.1-6 alkylthio-C.sub.1-3 alkyl, C.sub.3-7 cycloalkylthio-C.sub.1-3 alkyl, C.sub.1-5 alkoxy-C.sub.1-3 alkyl, C.sub.3-7 cycloalkoxy-C.sub.1-3 alkyl, C.sub.1-6 alkylthio, C.sub.3-7 cycloalkylthio, C.sub.1-5 alkoxy or C.sub.3-7 cycloalkoxy; R.sup.3 is H, C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, --COR.sup.4, --COOR.sup.5 or --CONHR.sup.6 ; when X.sup.1, X.sup.2 and R.sup.3 are all hydrogen atoms, R.sup.2 is not an isobutyl group, or a salt thereof, which exhibits excellent antagonistic action against endothelin receptors, particularly endothelin B receptors.

REFERENCES:
patent: 5114918 (1992-05-01), Ishikawa et al.
Kikuchi et al. "Cyclic Hexapeptide Endothelin Receptor Antagonists Highly Potent For Both Receptor Subtypes ET.sub.A and ET.sub.B ", Biochemical and Biophysical Research Communications, vol. 200:1708-1711, (1994).
Hirata et al., "Receptor Binding Activity and Cytosolic Free Calcium Response by Synthetic Endothelin Analogs in Cultured Rat Vascular Smooth Muscle Cells", Biochem. Biophysical Research Comm., vol. 160, No. 1, Apr. 1989, pp. 228-234.
Ihara et al., "Biological Profiles of Highly Potent Novel Endothelin Antagonists Selective for the ET.sub.A Receptor", Life Sciences, vol. 50, No. 4, (1992), pp. pp. 247-255.
Nakajima et al., "Structure-Activity Relationship of Endothelin: Importance of Charged Groups", Biochem. Biophysical Res. Comm., vol. 163, No. 1, (1989), pp. 424-429.
Kimura et al., "Structure-Activity Relationship of Endothelin: Importance of the C-Terminal Moiety", Biochem. Biophysical Res. Comm., vol. 156, No. 3, Nov. 1988, pp. 1182-1186.
Annette M. Doherty, "Endothelin: A New Challenge", Jour. of Med. Chem., vol. 35, No. 9, May 1992 pp. 1494-1508.

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