Peptide, production and use thereof

Details Peptide, production and use thereof Peptide, production and use thereof

1992-12-17

1997-03-25

Robinson, Douglas W.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Peptide containing doai

530329, 530330, 514 18, A61K 3800, C07K 700, C07K 706, C07K 510

Patent

active

056144970

ABSTRACT:
A peptide represented by the formula: ##STR1## wherein R.sub.1 represents an oil-soluble group; R.sub.2 and R.sub.5 represent a hydrogen atom or a lower alkyl group; R.sub.3 represents an aliphatic group which may have O or S; R.sub.4 represents a heterocyclic-substituted lower alkyl group; R.sub.6 represents a hydrogen atom, a lower alkyl group or an aromatic cyclic group; X represents a group having an aromatic ring; n represents an integer of 0 or more and m represents an integer of 2 or more, or a salt thereof exhibits a marked endothelin receptor-antagonistic action, and the peptide [I] is pharmaceutically useful as a therapeutic agent for hypertension, cardiovascular disease and renal disease, for instance.

REFERENCES:
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patent: 5352659 (1994-10-01), Wakimasu et al.
patent: 5430022 (1995-07-01), Hemmi et al.
patent: 5444152 (1995-08-01), Ishikawa et al.
patent: 5470833 (1995-11-01), Ishikawa et al.
patent: 5494897 (1996-02-01), Ishikawa et al.
patent: 5496928 (1996-03-01), Ishikawa et al.
Stein et al. J. Of Medicinal Chemistry, vol. 37, No. 3, pp. 329-331.
Doherty, J. of Medicinal Chemistry, vol. 35, No. 9, May 1, 1992.
Eur. J. Pharmacol. 221:77 (1992), "Protective Effect of a Selective Endothelin Receptor Antagonist in Ischemic Acute Renal Failure in Rats".
J. Pharm. Exper. Therap., 270:728 (1994), "A New Endothelin Receptor Antagonist Shows Long-Lasting Inhibition of Endothelin-Mediated Blood Pressure Responses in Rats".
Ihara, et al, Life Sciences, vol. 50, pp. 247-255, 1992.
Fukuroda, Life Sciences, vol. 50, pp. 107-112, 1992.

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