ANE derivatives with novel bridging

Details ANE derivatives with novel bridging ANE derivatives with novel bridging

1988-12-15

1990-01-02

Schain, Howard E.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Peptide containing doai

530324, 530325, 530326, C07K 700, C07K 502, C07K 708

Patent

active

048913588

ABSTRACT:
Disclosed herein are derivatives of atrial natriuretic peptides wherein the exocyclic N-terminal peptide segment is deleted and the two cysteinyl residues (at positions 105 and 121) of the natural sequence are replaced with a trivalent unit, --NHCH(CO--)--Q--X--Y--CH.sub.2 CH.sub.2 CO-- wherein Q is methylene, ethylene or CR'R" wherein R' and R" each independently is lower alkyl, X is oxy or thio, and Y is methylene or des-Y. The derivatives may be optionally substituted at various positions including positions 106, 107 and 124. The derivatives possess ANF-like activity and are indicated for treating hypertension and for treating pathological conditions resulting from an imbalance of body fluids and electrolytes.

REFERENCES:
patent: 4670540 (1987-06-01), Sakakibara
patent: 4721704 (1988-01-01), Chang et al.
patent: 4757048 (1988-07-01), Lewichi et al.
patent: 4764504 (1988-08-01), Johnson et al.
A. DeBold et al., Life Sciences, 28, 89 (1981).
M. G. Currie et al., Science 221, 71 (1983).
M. Cantin and J. Genest, Endocrine Reviews, 6, 107 (1985).

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